RU2015125575A - Композиции и способы для лечения злокачественной опухоли - Google Patents
Композиции и способы для лечения злокачественной опухоли Download PDFInfo
- Publication number
- RU2015125575A RU2015125575A RU2015125575A RU2015125575A RU2015125575A RU 2015125575 A RU2015125575 A RU 2015125575A RU 2015125575 A RU2015125575 A RU 2015125575A RU 2015125575 A RU2015125575 A RU 2015125575A RU 2015125575 A RU2015125575 A RU 2015125575A
- Authority
- RU
- Russia
- Prior art keywords
- wee1
- patient
- pharmaceutically acceptable
- acceptable salt
- inhibitor
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims 14
- 201000011510 cancer Diseases 0.000 title claims 9
- 239000000203 mixture Substances 0.000 title 1
- 101000621390 Homo sapiens Wee1-like protein kinase Proteins 0.000 claims 21
- 102100023037 Wee1-like protein kinase Human genes 0.000 claims 21
- 239000003112 inhibitor Substances 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 11
- 239000013068 control sample Substances 0.000 claims 8
- 230000014509 gene expression Effects 0.000 claims 8
- 101000687968 Homo sapiens Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase Proteins 0.000 claims 3
- 102100024262 Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase Human genes 0.000 claims 3
- 230000003211 malignant effect Effects 0.000 claims 3
- 239000000523 sample Substances 0.000 claims 3
- 101100520515 Homo sapiens PKMYT1 gene Proteins 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000013610 patient sample Substances 0.000 claims 2
- 206010000830 Acute leukaemia Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000092 prognostic biomarker Substances 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/43—Enzymes; Proenzymes; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
- C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
- C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
- C12Q1/6886—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
- G01N33/573—Immunoassay; Biospecific binding assay; Materials therefor for enzymes or isoenzymes
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q2600/00—Oligonucleotides characterized by their use
- C12Q2600/106—Pharmacogenomics, i.e. genetic variability in individual responses to drugs and drug metabolism
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q2600/00—Oligonucleotides characterized by their use
- C12Q2600/158—Expression markers
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/90—Enzymes; Proenzymes
- G01N2333/91—Transferases (2.)
- G01N2333/91005—Transferases (2.) transferring one-carbon groups (2.1)
- G01N2333/91011—Methyltransferases (general) (2.1.1.)
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Medicinal Chemistry (AREA)
- Analytical Chemistry (AREA)
- Pathology (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Wood Science & Technology (AREA)
- Genetics & Genomics (AREA)
- Zoology (AREA)
- Epidemiology (AREA)
- Biotechnology (AREA)
- Physics & Mathematics (AREA)
- Microbiology (AREA)
- Biochemistry (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- General Engineering & Computer Science (AREA)
- Biophysics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Cell Biology (AREA)
- Food Science & Technology (AREA)
- General Physics & Mathematics (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (22)
1. Способ лечения пациента, у которого диагностирована злокачественная опухоль, ассоциированная с киназой WEE1, ингибитором WEE1, включающий:
(a) измерение уровня экспрессии гена PKMYT1 в биологическом образце, содержащем злокачественные клетки, полученном от указанного пациента, и в контрольном образце;
(b) определение того, является ли уровень экспрессии гена в указанном образце от пациента более высоким или более низким, чем уровень экспрессии в указанном контрольном образце;
(c) отбор указанного пациента для лечения ингибитором WEE1, где уровень прогностического биомаркера из указанного образца пациента является более низким, чем в контрольном образце; и
(d) введение ингибитора WEE1 выбранному пациенту.
2. Способ по п. 1, где указанный контрольный образец получают от одного или нескольких индивидуумов, которые не имеют заболевания или у которых не была диагностирована злокачественная опухоль, ассоциированная с киназой WEE1.
3. Способ по п. 1, где указанный ингибитор WEE1 представляет собой WEE1-1, или его фармацевтически приемлемую соль, или WEE1-2 или его фармацевтически приемлемую соль.
4. Способ по п. 3, где указанный ингибитор WEE1 представляет собой WEE1-1 или его фармацевтически приемлемую соль.
5. Способ по п. 3, где указанный ингибитор WEE1 представляет собой WEE1-2 или его фармацевтически приемлемую соль.
6. Способ лечения пациента со злокачественной опухолью, чувствительного к лечению ингибитором WEE1, включающий:
(a) измерение уровня экспрессии гена PKMYT1 в биологическом образце, содержащем злокачественные клетки, полученном от указанного пациента, и в контрольном образце;
(b) определение того, является ли уровень экспрессии гена в указанном образце от пациента более высоким или более низким, чем уровень экспрессии в указанном контрольном образце;
(c) идентификацию указанного чувствительного пациента для лечения ингибитором WEE1, где уровень PKMYT1 в указанном образце пациента является более низким, чем в контрольном образце; и
(d) введение ингибитора WEE1 чувствительному пациенту.
7. Способ по п. 6, где указанный контрольный образец получен от одного или двух индивидуумов, которые не имеют заболевания или у которых не диагностирована злокачественная опухоль, ассоциированная с киназой WEE1.
8. Способ по п. 6, где указанный ингибитор WEE1 представляет собой WEE1-1 или его фармацевтически приемлемую соль, или WEE1-2 или его фармацевтически приемлемую соль.
9. Способ по п. 8, где указанный ингибитор WEE1 представляет собой WEE1-1 или его фармацевтически приемлемую соль.
10. Способ по п. 8, где указанный ингибитор WEE1 представляет собой WEE1-2 или его фармацевтически приемлемую соль.
11. Способ по п. 6, где указанная злокачественная опухоль представляет собой злокачественную опухоль, ассоциированную с киназой WEE1, выбранную из группы, состоящей из рака молочной железы, рака легкого, рака поджелудочной железы, рака толстого кишечника, рака яичника, острого лейкоза, хронического лимфоцитарного лейкоза, хронического миелоцитарного лейкоза и лимфомы Ходжкина.
12. Способ лечения пациента со злокачественной опухолью, ассоциированной с киназой WEE1, нуждающегося в лечении, включающий введение терапевтически эффективного количества ингибитора WEE1, где ингибитор WEE1 представляет собой WEE1-1 или его фармацевтически приемлемую соль, или WEE1-2 или его фармацевтически приемлемую соль, и где злокачественные клетки указанного пациента, подлежащего лечению, характеризуются низкой экспрессией PKMYT1.
13. Способ по п. 12, где ингибитор WEE1 представляет собой WEE1-1 или его фармацевтически приемлемую соль.
14. Набор для идентификации пациента со злокачественной опухолью, чувствительного к лечению ингибитором WEE1, включающий выявление средства, способного выявлять продукт экспрессии PKMYT1, в биологическом исследуемом образце.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261730795P | 2012-11-28 | 2012-11-28 | |
| US61/730,795 | 2012-11-28 | ||
| PCT/US2013/071377 WO2014085216A1 (en) | 2012-11-28 | 2013-11-22 | Compositions and methods for treating cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2015125575A true RU2015125575A (ru) | 2017-01-10 |
| RU2660349C2 RU2660349C2 (ru) | 2018-07-05 |
Family
ID=50828365
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2015125575A RU2660349C2 (ru) | 2012-11-28 | 2013-11-22 | Композиции и способы для лечения злокачественной опухоли |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US9655899B2 (ru) |
| EP (1) | EP2925888B1 (ru) |
| JP (1) | JP6290237B2 (ru) |
| KR (1) | KR102161331B1 (ru) |
| AU (1) | AU2013352568B2 (ru) |
| BR (1) | BR112015012295A8 (ru) |
| CA (1) | CA2892361A1 (ru) |
| CY (1) | CY1119676T1 (ru) |
| DK (1) | DK2925888T3 (ru) |
| ES (1) | ES2651347T3 (ru) |
| HR (1) | HRP20180002T1 (ru) |
| HU (1) | HUE035662T2 (ru) |
| LT (1) | LT2925888T (ru) |
| ME (1) | ME02925B (ru) |
| MX (1) | MX363243B (ru) |
| NO (1) | NO2941224T3 (ru) |
| PL (1) | PL2925888T3 (ru) |
| PT (1) | PT2925888T (ru) |
| RS (1) | RS56680B1 (ru) |
| RU (1) | RU2660349C2 (ru) |
| SI (1) | SI2925888T1 (ru) |
| SM (1) | SMT201700595T1 (ru) |
| WO (1) | WO2014085216A1 (ru) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| PT3495367T (pt) | 2012-06-13 | 2020-11-12 | Incyte Holdings Corp | Compostos tricíclicos substituídos como inibidores de fgfr |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| MX393494B (es) | 2013-04-19 | 2025-03-24 | Incyte Holdings Corp | Heterociclos biciclicos como inhibidores de los receptores del factor de crecimiento de fibroblastos (fgfr). |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| CR20170390A (es) | 2015-02-20 | 2017-10-23 | Incyte Holdings Corp | Heterociclos biciclicos como inhibidores de fgfr |
| WO2017078752A1 (en) * | 2015-11-06 | 2017-05-11 | The Penn State Research Foundation | Compositions and methods relating to cancer |
| US10280348B2 (en) * | 2017-01-31 | 2019-05-07 | Prc-Desoto International, Inc. | Low density aerospace compositions and sealants |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CA3078945A1 (en) | 2017-10-09 | 2019-04-18 | Nuvation Bo Inc. | Heterocyclic compounds and uses thereof |
| US11299493B2 (en) | 2017-10-09 | 2022-04-12 | Nuvation Bio Inc. | Heterocyclic compounds and uses thereof |
| US11174257B2 (en) | 2018-05-04 | 2021-11-16 | Incyte Corporation | Salts of an FGFR inhibitor |
| WO2019213544A2 (en) | 2018-05-04 | 2019-11-07 | Incyte Corporation | Solid forms of an fgfr inhibitor and processes for preparing the same |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| EP3952878A4 (en) * | 2019-04-09 | 2023-01-04 | Nuvation Bio Inc. | HETEROCYCLIC COMPOUNDS AND THEIR USES |
| WO2020210377A1 (en) * | 2019-04-09 | 2020-10-15 | Nuvation Bio Inc. | Heterocyclic compounds and uses thereof |
| KR20210150476A (ko) | 2019-04-09 | 2021-12-10 | 누베이션 바이오 인크. | 헤테로시클릭 화합물 및 그의 용도 |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076602A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| JP2023505258A (ja) | 2019-12-04 | 2023-02-08 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての三環式複素環 |
| PE20221504A1 (es) | 2019-12-04 | 2022-09-30 | Incyte Corp | Derivados de un inhibidor de fgfr |
| JP2023507799A (ja) * | 2019-12-20 | 2023-02-27 | リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー | 組み合わせ |
| CA3165468A1 (en) * | 2019-12-20 | 2021-06-24 | Recurium Ip Holdings, Llc | Combinations |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| KR20230017167A (ko) * | 2020-04-01 | 2023-02-03 | 엔진 바이오사이언시즈 피티이. 엘티디. | 암을 치료하기 위한 방법 및 조성물 |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法 |
| CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| CN113735863A (zh) * | 2021-09-29 | 2021-12-03 | 武汉九州钰民医药科技有限公司 | Wee1抑制剂adavosertib的制备工艺 |
| PT118269A (pt) | 2022-10-20 | 2024-04-22 | Univ Aveiro | Pkmyt1 for use in regenerative medicine |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (393)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3126375A (en) | 1964-03-24 | Chioacyl | ||
| US2789118A (en) | 1956-03-30 | 1957-04-16 | American Cyanamid Co | 16-alpha oxy-belta1, 4-pregnadienes |
| US2990401A (en) | 1958-06-18 | 1961-06-27 | American Cyanamid Co | 11-substituted 16alpha, 17alpha-substituted methylenedioxy steroids |
| US3048581A (en) | 1960-04-25 | 1962-08-07 | Olin Mathieson | Acetals and ketals of 16, 17-dihydroxy steroids |
| US3749712A (en) | 1970-09-25 | 1973-07-31 | Sigma Tau Ind Farmaceuti | Triamcinolone acetonide esters and process for their preparation |
| SE378110B (ru) | 1972-05-19 | 1975-08-18 | Bofors Ab | |
| US3996359A (en) | 1972-05-19 | 1976-12-07 | Ab Bofors | Novel stereoisomeric component A of stereoisomeric mixtures of 2'-unsymmetrical 16,17-methylenedioxy steroid 21-acylates, compositions thereof, and method of treating therewith |
| SE378109B (ru) | 1972-05-19 | 1975-08-18 | Bofors Ab | |
| US4319039A (en) | 1979-06-15 | 1982-03-09 | Merck & Co., Inc. | Preparation of ammonium salt of hypocholesteremic fermentation product |
| US4294926A (en) | 1979-06-15 | 1981-10-13 | Merck & Co., Inc. | Hypocholesteremic fermentation products and process of preparation |
| US4231938A (en) | 1979-06-15 | 1980-11-04 | Merck & Co., Inc. | Hypocholesteremic fermentation products and process of preparation |
| US4444784A (en) | 1980-08-05 | 1984-04-24 | Merck & Co., Inc. | Antihypercholesterolemic compounds |
| DK149080C (da) | 1980-06-06 | 1986-07-28 | Sankyo Co | Fremgangsmaade til fremstilling af derivater af ml-236b-carboxylsyre |
| JPS5889191A (ja) | 1981-11-20 | 1983-05-27 | Sankyo Co Ltd | ３−ヒドロキシ−ｍｌ−２３６ｂ誘導体の製造法 |
| US5354772A (en) | 1982-11-22 | 1994-10-11 | Sandoz Pharm. Corp. | Indole analogs of mevalonolactone and derivatives thereof |
| US4911165A (en) | 1983-01-12 | 1990-03-27 | Ethicon, Inc. | Pliabilized polypropylene surgical filaments |
| US4683202A (en) | 1985-03-28 | 1987-07-28 | Cetus Corporation | Process for amplifying nucleic acid sequences |
| US4681893A (en) | 1986-05-30 | 1987-07-21 | Warner-Lambert Company | Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis |
| US5525464A (en) | 1987-04-01 | 1996-06-11 | Hyseq, Inc. | Method of sequencing by hybridization of oligonucleotide probes |
| US5202231A (en) | 1987-04-01 | 1993-04-13 | Drmanac Radoje T | Method of sequencing of genomes by hybridization of oligonucleotide probes |
| US4885314A (en) | 1987-06-29 | 1989-12-05 | Merck & Co., Inc. | Novel HMG-CoA reductase inhibitors |
| US4782084A (en) | 1987-06-29 | 1988-11-01 | Merck & Co., Inc. | HMG-COA reductase inhibitors |
| US4820850A (en) | 1987-07-10 | 1989-04-11 | Merck & Co., Inc. | Process for α-C-alkylation of the 8-acyl group on mevinolin and analogs thereof |
| US5030447A (en) | 1988-03-31 | 1991-07-09 | E. R. Squibb & Sons, Inc. | Pharmaceutical compositions having good stability |
| US5700637A (en) | 1988-05-03 | 1997-12-23 | Isis Innovation Limited | Apparatus and method for analyzing polynucleotide sequences and method of generating oligonucleotide arrays |
| US4916239A (en) | 1988-07-19 | 1990-04-10 | Merck & Co., Inc. | Process for the lactonization of mevinic acids and analogs thereof |
| EP0360390A1 (en) | 1988-07-25 | 1990-03-28 | Glaxo Group Limited | Spirolactam derivatives |
| GB8822228D0 (en) | 1988-09-21 | 1988-10-26 | Southern E M | Support-bound oligonucleotides |
| US5290946A (en) | 1988-10-13 | 1994-03-01 | Sandoz Ltd. | Processes for the synthesis of 3-(substituted indolyl-2-yl)propenaldehydes |
| US5118853A (en) | 1988-10-13 | 1992-06-02 | Sandoz Ltd. | Processes for the synthesis of 3-disubstituted aminoacroleins |
| MX18467A (es) | 1988-11-23 | 1993-07-01 | Pfizer | Agentes terapeuticos de quinuclidinas |
| US4929437A (en) | 1989-02-02 | 1990-05-29 | Merck & Co., Inc. | Coenzyme Q10 with HMG-CoA reductase inhibitors |
| US5164372A (en) | 1989-04-28 | 1992-11-17 | Fujisawa Pharmaceutical Company, Ltd. | Peptide compounds having substance p antagonism, processes for preparation thereof and pharmaceutical composition comprising the same |
| US5189164A (en) | 1989-05-22 | 1993-02-23 | Sandoz Ltd. | Processes for the synthesis of syn-(E)-3,5-dihydroxy-7-substituted hept-6-enoic and heptanoic acids and derivatives and intermediates thereof |
| US5547839A (en) | 1989-06-07 | 1996-08-20 | Affymax Technologies N.V. | Sequencing of surface immobilized polymers utilizing microflourescence detection |
| US5424186A (en) | 1989-06-07 | 1995-06-13 | Affymax Technologies N.V. | Very large scale immobilized polymer synthesis |
| US5143854A (en) | 1989-06-07 | 1992-09-01 | Affymax Technologies N.V. | Large scale photolithographic solid phase synthesis of polypeptides and receptor binding screening thereof |
| US5242974A (en) | 1991-11-22 | 1993-09-07 | Affymax Technologies N.V. | Polymer reversal on solid surfaces |
| US5744101A (en) | 1989-06-07 | 1998-04-28 | Affymax Technologies N.V. | Photolabile nucleoside protecting groups |
| US5527681A (en) | 1989-06-07 | 1996-06-18 | Affymax Technologies N.V. | Immobilized molecular synthesis of systematically substituted compounds |
| US6551784B2 (en) | 1989-06-07 | 2003-04-22 | Affymetrix Inc | Method of comparing nucleic acid sequences |
| FI94339C (fi) | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi |
| DE3924454A1 (de) | 1989-07-24 | 1991-02-07 | Cornelis P Prof Dr Hollenberg | Die anwendung von dna und dna-technologie fuer die konstruktion von netzwerken zur verwendung in der chip-konstruktion und chip-produktion (dna chips) |
| PH27357A (en) | 1989-09-22 | 1993-06-21 | Fujisawa Pharmaceutical Co | Pyrazole derivatives and pharmaceutical compositions comprising the same |
| FI97540C (fi) | 1989-11-06 | 1997-01-10 | Sanofi Sa | Menetelmä terapeuttisesti käyttökelpoisten, aromaattisesti substituoitujen piperidiini- ja piperatsiinijohdannaisten valmistamiseksi |
| FR2654726B1 (fr) | 1989-11-23 | 1992-02-14 | Rhone Poulenc Sante | Nouveaux derives de l'isoindolone et leur preparation. |
| FR2654725B1 (fr) | 1989-11-23 | 1992-02-14 | Rhone Poulenc Sante | Nouveaux derives de l'isoindolone, leur preparation et les compositions pharmaceutiques qui les contiennent. |
| EP0430881A3 (en) | 1989-11-29 | 1991-10-23 | Ciba-Geigy Ag | Photochromic compounds, process for their preparation and their use |
| GB8929070D0 (en) | 1989-12-22 | 1990-02-28 | Fujisawa Pharmaceutical Co | Peptide compounds,processes for preparation thereof and pharmaceutical composition comprising the same |
| US5232929A (en) | 1990-11-28 | 1993-08-03 | Pfizer Inc. | 3-aminopiperidine derivatives and related nitrogen containing heterocycles and pharmaceutical compositions and use |
| WO1991009844A1 (en) | 1990-01-04 | 1991-07-11 | Pfizer Inc. | Substance p antagonists |
| US5321032A (en) | 1990-02-15 | 1994-06-14 | Fujisawa Pharmaceutical Co., Ltd. | Peptide compounds and pharmaceutical compositions thereof |
| US5288644A (en) | 1990-04-04 | 1994-02-22 | The Rockefeller University | Instrument and method for the sequencing of genome |
| US5420245A (en) | 1990-04-18 | 1995-05-30 | Board Of Regents, The University Of Texas | Tetrapeptide-based inhibitors of farnesyl transferase |
| JPH072740B2 (ja) | 1990-06-01 | 1995-01-18 | フアイザー・インコーポレイテツド | ３―アミノ―２―アリールキヌクリジン |
| JP2514137B2 (ja) | 1990-07-23 | 1996-07-10 | フアイザー・インコーポレイテツド | キヌクリジン誘導体 |
| WO1994004494A1 (en) | 1992-08-13 | 1994-03-03 | Warner-Lambert Company | Tachykinin antagonists |
| BR9106905A (pt) | 1990-09-28 | 1993-08-17 | Pfizer | Analogos de anel condensado de heterociclos nao aromaticos contendo nitrogenio |
| GB9023116D0 (en) | 1990-10-24 | 1990-12-05 | Fujisawa Pharmaceutical Co | Peptide compounds,processes for preparation thereof and pharmaceutical composition comprising the same |
| US5177080A (en) | 1990-12-14 | 1993-01-05 | Bayer Aktiengesellschaft | Substituted pyridyl-dihydroxy-heptenoic acid and its salts |
| EP0498069B1 (en) | 1990-12-21 | 1995-10-25 | Fujisawa Pharmaceutical Co., Ltd. | New use of peptide derivative |
| JPH0733385B2 (ja) | 1991-01-10 | 1995-04-12 | フアイザー・インコーポレイテツド | 物質ｐの拮抗薬としてのｎ−アルキルキヌクリジニウム塩 |
| ATE154354T1 (de) | 1991-02-11 | 1997-06-15 | Merck Sharp & Dohme | Azabicyclische verbindungen, diese enthaltende pharmazeutische zubereitungen und ihre therapeutische verwendung |
| ES2065175T3 (es) | 1991-03-01 | 1995-02-01 | Pfizer | Derivados de 1-azabiciclo(3.2.2)nonan-3-amina. |
| US5747469A (en) | 1991-03-06 | 1998-05-05 | Board Of Regents, The University Of Texas System | Methods and compositions comprising DNA damaging agents and p53 |
| JPH0794440B2 (ja) | 1991-03-26 | 1995-10-11 | フアイザー・インコーポレイテツド | 置換ピペリジンの立体選択的製造 |
| FR2677361A1 (fr) | 1991-06-04 | 1992-12-11 | Adir | Nouveaux peptides et pseudopeptides, derives de tachykinines, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| FR2676053B1 (fr) | 1991-05-03 | 1993-08-27 | Sanofi Elf | Nouveaux composes dialkylenepiperidino et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| FR2676055B1 (fr) | 1991-05-03 | 1993-09-03 | Sanofi Elf | Composes polycycliques amines et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| FR2676447B1 (fr) | 1991-05-17 | 1993-08-06 | Rhone Poulenc Rorer Sa | Nouveaux derives du thiopyranopyrrole et leur preparation. |
| FR2676443B1 (fr) | 1991-05-17 | 1993-08-06 | Rhone Poulenc Rorer Sa | Nouveaux derives de perhydroisoindole et leur preparation. |
| FR2676442B1 (fr) | 1991-05-17 | 1993-08-06 | Rhone Poulenc Rorer Sa | Nouveau derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent. |
| FR2676446B1 (fr) | 1991-05-17 | 1993-08-06 | Rhone Poulenc Rorer Sa | Nouveaux derives du thiopyranopyrrole, leur preparation et les compositions pharmaceutiques qui les contiennent. |
| WO1992020661A1 (en) | 1991-05-22 | 1992-11-26 | Merck & Co., Inc. | N, n-diacylpiperazines |
| CA2109415C (en) | 1991-05-22 | 1998-12-29 | Fumitaka Ito | Substituted 3-aminoquinuclidines |
| JPH0733386B2 (ja) | 1991-05-31 | 1995-04-12 | フアイザー・インコーポレイテツド | キヌクリジン誘導体 |
| GB9113219D0 (en) | 1991-06-19 | 1991-08-07 | Fujisawa Pharmaceutical Co | Peptide compound,processes for preparation thereof and pharmaceutical composition comprising the same |
| PL170516B1 (en) | 1991-06-20 | 1996-12-31 | Pfizer | Method of obtaining novel derivatives of fluoroalkoxy benzylaminic compounds of piperidine |
| TW202432B (ru) | 1991-06-21 | 1993-03-21 | Pfizer | |
| US5288730A (en) | 1991-06-24 | 1994-02-22 | Merck Sharp & Dohme Limited | Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy |
| ATE133657T1 (de) | 1991-07-05 | 1996-02-15 | Merck Sharp & Dohme | Aromatische verbindungen, diese enthaltende pharmazeutische zusammensetzungen und ihre therapeutische anwendung |
| EP0536817A1 (en) | 1991-07-05 | 1993-04-14 | MERCK SHARP & DOHME LTD. | Azabicyclic compounds as tachykinin antagonists |
| US5472978A (en) | 1991-07-05 | 1995-12-05 | Merck Sharp & Dohme Ltd. | Aromatic compounds, pharmaceutical compositions containing them and their use in therapy |
| WO1993001165A2 (en) | 1991-07-10 | 1993-01-21 | Merck Sharp & Dohme Limited | Aromatic compounds, compositions containing them and their use in therapy |
| US5495047A (en) | 1991-07-10 | 1996-02-27 | Merck, Sharp & Dohme (Ltd.) | Fused tricyclic compounds, pharmaceutical compositions containing them and their use in therapy |
| MY110227A (en) | 1991-08-12 | 1998-03-31 | Ciba Geigy Ag | 1-acylpiperindine compounds. |
| EP0600952B1 (en) | 1991-08-20 | 1996-04-17 | MERCK SHARP & DOHME LTD. | Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them |
| PT533280E (pt) | 1991-09-20 | 2001-01-31 | Glaxo Group Ltd | Novas utilizacoes medicas para antagonistas de taquiquinina |
| DE69232588T2 (de) | 1991-09-26 | 2002-08-22 | Pfizer Inc., New York | Kondensierte trizyklische, stickstoffenthaltende Verbindungen als Substanz P Rezeptor Antagonisten |
| JP2553020B2 (ja) | 1991-11-07 | 1996-11-13 | 吉富製薬株式会社 | キヌクリジン化合物およびその医薬用途 |
| CA2123403C (en) | 1991-11-12 | 2002-02-05 | Brian T. O'neill | Acyclic ethylenediamine derivatives as substance p receptor antagonists |
| US5384261A (en) | 1991-11-22 | 1995-01-24 | Affymax Technologies N.V. | Very large scale immobilized polymer synthesis using mechanically directed flow paths |
| US5412087A (en) | 1992-04-24 | 1995-05-02 | Affymax Technologies N.V. | Spatially-addressable immobilization of oligonucleotides and other biological polymers on surfaces |
| US5324633A (en) | 1991-11-22 | 1994-06-28 | Affymax Technologies N.V. | Method and apparatus for measuring binding affinity |
| EP0545478A1 (en) | 1991-12-03 | 1993-06-09 | MERCK SHARP & DOHME LTD. | Heterocyclic compounds as tachykinin antagonists |
| HU217629B (hu) | 1991-12-12 | 2000-03-28 | Novartis Ag. | Eljárás fluvasztatint tartalmazó stabilizált gyógyszerkészítmények előállítására |
| GB9200535D0 (en) | 1992-01-10 | 1992-02-26 | Fujisawa Pharmaceutical Co | New compound |
| GB9201179D0 (en) | 1992-01-21 | 1992-03-11 | Glaxo Group Ltd | Chemical compounds |
| US5328927A (en) | 1992-03-03 | 1994-07-12 | Merck Sharpe & Dohme, Ltd. | Hetercyclic compounds, processes for their preparation and pharmaceutical compositions containing them |
| JP2656702B2 (ja) | 1992-03-23 | 1997-09-24 | ファイザー製薬株式会社 | ペプチド性キヌクリジン |
| WO1993020236A1 (en) | 1992-04-03 | 1993-10-14 | Applied Biosystems, Inc. | Probe composition and method |
| FR2689888B1 (fr) | 1992-04-10 | 1994-06-10 | Rhone Poulenc Rorer Sa | Nouveaux derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent. |
| JPH07505648A (ja) | 1992-04-15 | 1995-06-22 | メルク シヤープ エンド ドーム リミテツド | アザサイクリック化合物 |
| GB2266529A (en) | 1992-05-01 | 1993-11-03 | Merck Sharp & Dohme | Tetrahydroisoquinoline derivatives |
| DE69331190T2 (de) | 1992-05-18 | 2002-04-18 | Pfizer Inc., New York | Überbrückte azabicyclische derivate als substanz p antagonisten |
| GB9211193D0 (en) | 1992-05-27 | 1992-07-08 | Merck Sharp & Dohme | Therapeutic agents |
| CA2099233A1 (en) | 1992-06-29 | 1993-12-30 | Conrad P. Dorn | Morpholine and thiomorpholine tachykinin receptor antagonists |
| US5637699A (en) | 1992-06-29 | 1997-06-10 | Merck & Co., Inc. | Process for preparing morpholine tachykinin receptor antagonists |
| US5719147A (en) | 1992-06-29 | 1998-02-17 | Merck & Co., Inc. | Morpholine and thiomorpholine tachykinin receptor antagonists |
| WO1994001402A1 (en) | 1992-07-13 | 1994-01-20 | Merck Sharp & Dohme Limited | Heterocyclic amide derivatives as tachykinin derivatives |
| CA2140343A1 (en) | 1992-07-17 | 1994-02-03 | Sean M. Sullivan | Method and reagent for treatment of animal diseases |
| GB2268931A (en) | 1992-07-22 | 1994-01-26 | Merck Sharp & Dohme | Azabicyclic tachykinin-receptor antagonists |
| AU675447B2 (en) | 1992-07-28 | 1997-02-06 | Merck Sharp & Dohme Limited | Carboxamidomethyl piperidine and analogues |
| GB2269170A (en) | 1992-07-29 | 1994-02-02 | Merck Sharp & Dohme | Azatricyclic tachykinin antagonists |
| WO1994003429A1 (en) | 1992-07-31 | 1994-02-17 | Merck Sharp & Dohme Limited | Substituted amines as tachykinin receptor antagonists |
| JPH07506379A (ja) | 1992-08-04 | 1995-07-13 | ファイザー・インコーポレーテッド | 物質ｐ受容体アンタゴニストとしての３−ベンジルアミノ−２−フェニル−ピペリジン |
| GB9216911D0 (en) | 1992-08-10 | 1992-09-23 | Merck Sharp & Dohme | Therapeutic agents |
| PT655996E (pt) | 1992-08-19 | 2002-04-29 | Pfizer | Benzilaminas substituidas contendo heterociclicos nao aromaticos contendo azoto |
| US5387595A (en) | 1992-08-26 | 1995-02-07 | Merck & Co., Inc. | Alicyclic compounds as tachykinin receptor antagonists |
| NO179904C (no) | 1992-09-04 | 1997-01-08 | Takeda Chemical Industries Ltd | Kondenserte heterocykliske forbindelser og deres anvendelse |
| US5563161A (en) | 1992-09-10 | 1996-10-08 | Merck Sharp & Dohme Ltd. | Alcohols and ethers with aromatic substituents as tachykinin-antagonists |
| GB9220286D0 (en) | 1992-09-25 | 1992-11-11 | Merck Sharp & Dohme | Therapeutic agents |
| JP2656699B2 (ja) | 1992-10-21 | 1997-09-24 | ファイザー製薬株式会社 | 置換ベンジルアミノキヌクリジン |
| GB9222262D0 (en) | 1992-10-23 | 1992-12-09 | Merck Sharp & Dohme | Therapeutic agents |
| GB9222486D0 (en) | 1992-10-26 | 1992-12-09 | Merck Sharp & Dohme | Therapeutic agents |
| JP2656700B2 (ja) | 1992-10-28 | 1997-09-24 | ファイザー製薬株式会社 | 置換キヌクリジン誘導体 |
| CA2146767A1 (en) | 1992-10-28 | 1994-05-11 | Timothy Harrison | 4-arylmethyloxymethyl piperidines as tachykinin antagonists |
| US5554501A (en) | 1992-10-29 | 1996-09-10 | Beckman Instruments, Inc. | Biopolymer synthesis using surface activated biaxially oriented polypropylene |
| US5554627A (en) | 1992-10-30 | 1996-09-10 | Merck, Sharp & Dohme Ltd. | Tachykinin antagonists |
| US5503980A (en) | 1992-11-06 | 1996-04-02 | Trustees Of Boston University | Positional sequencing by hybridization |
| CA2149242C (en) | 1992-11-12 | 1998-08-04 | Fumitaka Ito | Quinuclidine derivative for treatment of inflammatory and gastrointestinal disorders |
| US5261188A (en) | 1992-11-23 | 1993-11-16 | The Standard Products Company | Belt weatherstrip with bulb |
| JP2722279B2 (ja) | 1992-12-10 | 1998-03-04 | ファイザー・インク． | アミノメチレンで置換した非芳香族複素環式化合物及びサブスタンスｐのアンタゴニストとしての使用 |
| US5604260A (en) | 1992-12-11 | 1997-02-18 | Merck Frosst Canada Inc. | 5-methanesulfonamido-1-indanones as an inhibitor of cyclooxygenase-2 |
| AU682838B2 (en) | 1992-12-14 | 1997-10-23 | Merck Sharp & Dohme Limited | 4-aminomethyl/thiomethyl/sulfonylmethyl-4-phenylpiperidines as tachykinin receptor antagonists |
| GB9226581D0 (en) | 1992-12-21 | 1993-02-17 | Merck Sharp & Dohme | Therapeutic agents |
| EP0604181A1 (en) | 1992-12-21 | 1994-06-29 | Eli Lilly And Company | Antitumor compositions and method of treatment |
| GB9300051D0 (en) | 1993-01-04 | 1993-03-03 | Merck Sharp & Dohme | Therapeutic agents |
| DE69406903T2 (de) | 1993-01-15 | 1998-04-09 | Monsanto Co | 3,4-diarylthiophene und analoga davon, sowie deren verwendung als entzündungshemmende mittel |
| EP0610793A1 (en) | 1993-02-08 | 1994-08-17 | Takeda Chemical Industries, Ltd. | Tetracyclic morpholine derivatives and their use or analgesics |
| EP0683767B1 (en) | 1993-02-18 | 1998-06-03 | MERCK SHARP & DOHME LTD. | Azacyclic compounds, compositions containing them and their use as tachykinin antagonists |
| AU6140694A (en) | 1993-02-22 | 1994-09-14 | Merck Sharp & Dohme Limited | Aromatic compounds, compositions containing them and their use in therapy |
| WO1994019357A1 (en) | 1993-02-23 | 1994-09-01 | Merrell Dow Pharmaceuticals Inc. | Farnesyl:protein transferase inhibitors as anticancer agents |
| US5298627A (en) | 1993-03-03 | 1994-03-29 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
| AU6226494A (en) | 1993-03-04 | 1994-09-26 | Pfizer Inc. | Spiroazacyclic derivatives as substance p antagonists |
| US5409944A (en) | 1993-03-12 | 1995-04-25 | Merck Frosst Canada, Inc. | Alkanesulfonamido-1-indanone derivatives as inhibitors of cyclooxygenase |
| DE4311230C2 (de) | 1993-04-02 | 1996-12-19 | Mannesmann Ag | Nicht-spurgebundenes Fahrzeug mit Elektromotor |
| CA2118985A1 (en) | 1993-04-02 | 1994-10-03 | Dinesh V. Patel | Heterocyclic inhibitors of farnesyl protein transferase |
| US5496833A (en) | 1993-04-13 | 1996-03-05 | Merck Sharp & Dohme Limited | Piperidine tachykinin receptor antagonists |
| JP3424174B2 (ja) | 1993-05-06 | 2003-07-07 | メレルダウファーマス−ティカルズ インコーポレイテッド | タキキニン拮抗剤として有用な置換ピロリジン−３−イル−アルキル−ピペリジン類 |
| EP0698015A1 (en) | 1993-05-14 | 1996-02-28 | Genentech, Inc. | Preparation of n-cyanodithioimino-carbonates and 3-mercapto-5-amino-1h-1,2,4-triazole |
| US5602098A (en) | 1993-05-18 | 1997-02-11 | University Of Pittsburgh | Inhibition of farnesyltransferase |
| IL109646A0 (en) | 1993-05-19 | 1994-08-26 | Pfizer | Heteroatom substituted alkyl benzylamino-quinuclidines |
| US5380738A (en) | 1993-05-21 | 1995-01-10 | Monsanto Company | 2-substituted oxazoles further substituted by 4-fluorophenyl and 4-methylsulfonylphenyl as antiinflammatory agents |
| WO1994029309A1 (en) | 1993-06-07 | 1994-12-22 | Merck & Co., Inc. | Spiro-substituted azacycles as neurokinin antagonists |
| US5436265A (en) | 1993-11-12 | 1995-07-25 | Merck Frosst Canada, Inc. | 1-aroyl-3-indolyl alkanoic acids and derivatives thereof useful as anti-inflammatory agents |
| GB9602877D0 (en) | 1996-02-13 | 1996-04-10 | Merck Frosst Canada Inc | 3,4-Diaryl-2-hydroxy-2,5- dihydrofurans as prodrugs to cox-2 inhibitors |
| US5474995A (en) | 1993-06-24 | 1995-12-12 | Merck Frosst Canada, Inc. | Phenyl heterocycles as cox-2 inhibitors |
| US5837832A (en) | 1993-06-25 | 1998-11-17 | Affymetrix, Inc. | Arrays of nucleic acid probes on biological chips |
| EP0634402A1 (en) | 1993-07-14 | 1995-01-18 | Takeda Chemical Industries, Ltd. | Isochinolinone derivatives, their production and use |
| CA2167198C (en) | 1993-07-15 | 1999-03-16 | Kunio Satake | Benzylaminoquinuclidines |
| GB9315808D0 (en) | 1993-07-30 | 1993-09-15 | Merck Sharp & Dohme | Therapeutic agents |
| TW365603B (en) | 1993-07-30 | 1999-08-01 | Rhone Poulenc Rorer Sa | Novel perhydroisoindole derivatives, their preparation and pharmaceutical compositions which contain them |
| GB9317987D0 (en) | 1993-08-26 | 1993-10-13 | Glaxo Group Ltd | Chemical compounds |
| WO1995007908A1 (en) | 1993-09-17 | 1995-03-23 | Pfizer Inc. | Heteroarylamino and heteroarylsulfonamido substituted 3-benzylaminomethyl piperidines and related compounds |
| DE69433744T2 (de) | 1993-09-17 | 2004-10-14 | Pfizer Inc. | 3-amino-5-carboxy-substituierte piperidine und 3-amino-4-carboxy-substituierte pyrrolidine als tachykinin-antagonisten |
| IS4208A (is) | 1993-09-22 | 1995-03-23 | Glaxo Group Limited | 3-(tetrazólýl-benzyl)amínó-piperadidín afleiður |
| WO1995008542A1 (fr) | 1993-09-22 | 1995-03-30 | Kyowa Hakko Kogyo Co., Ltd. | Inhibiteur de la farnesyl-transferase |
| US5719148A (en) | 1993-10-15 | 1998-02-17 | Schering Corporation | Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases |
| US5721236A (en) | 1993-10-15 | 1998-02-24 | Schering Corporation | Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
| IL111235A (en) | 1993-10-15 | 2001-03-19 | Schering Plough Corp | Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them |
| US5661152A (en) | 1993-10-15 | 1997-08-26 | Schering Corporation | Tricyclic sulfonamide compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
| ES2164716T3 (es) | 1993-10-15 | 2002-03-01 | Schering Corp | Compuestos triciclicos de carbamato utiles para inhibir la funcion de la proteina-g y para el tratamiento de enfermedades proliferativas. |
| IL111257A0 (en) | 1993-10-15 | 1994-12-29 | Schering Corp | Tricyclic sulfonamide compounds useful for inhibition of g-protein function and for treatment of proliferative diseases |
| US5472672A (en) | 1993-10-22 | 1995-12-05 | The Board Of Trustees Of The Leland Stanford Junior University | Apparatus and method for polymer synthesis using arrays |
| US5470710A (en) | 1993-10-22 | 1995-11-28 | University Of Utah | Automated hybridization/imaging device for fluorescent multiplex DNA sequencing |
| AU682906B2 (en) | 1993-10-25 | 1997-10-23 | Parke, Davis & Company | Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase |
| US6156501A (en) | 1993-10-26 | 2000-12-05 | Affymetrix, Inc. | Arrays of modified nucleic acid probes and methods of use |
| WO1995011880A1 (en) | 1993-10-27 | 1995-05-04 | Merck Sharp & Dohme Limited | Substituted amides as tachykinin antagonists |
| US5429807A (en) | 1993-10-28 | 1995-07-04 | Beckman Instruments, Inc. | Method and apparatus for creating biopolymer arrays on a solid support surface |
| US5344991A (en) | 1993-10-29 | 1994-09-06 | G.D. Searle & Co. | 1,2 diarylcyclopentenyl compounds for the treatment of inflammation |
| US5783593A (en) | 1993-11-04 | 1998-07-21 | Abbott Laboratories | Inhibitors of squalene synthetase and protein farnesyltransferase |
| CA2152822A1 (en) | 1993-11-04 | 1995-05-11 | William R. Baker | Cyclobutane derivatives as inhibitors of squalene synthetase and protein farnesyltransferase |
| AU681454B2 (en) | 1993-11-05 | 1997-08-28 | Warner-Lambert Company | Substituted DI- and tripeptide inhibitors of protein:farnesyl transferase |
| US6403577B1 (en) | 1993-11-17 | 2002-06-11 | Eli Lilly And Company | Hexamethyleneiminyl tachykinin receptor antagonists |
| US5466823A (en) | 1993-11-30 | 1995-11-14 | G.D. Searle & Co. | Substituted pyrazolyl benzenesulfonamides |
| IT1271462B (it) | 1993-12-03 | 1997-05-28 | Menarini Farma Ind | Antagonisti delle tachichinine,procedimento per la loro preparazione e loro impiego in formulazioni farmaceutiche. |
| US5484799A (en) | 1993-12-09 | 1996-01-16 | Abbott Laboratories | Antifungal dorrigocin derivatives |
| IL111960A (en) | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| CA2176130A1 (en) | 1993-12-21 | 1995-06-29 | Thomas Alan Crowell | Non-peptide tachykinin receptor antagonists |
| JP3071467B2 (ja) | 1993-12-29 | 2000-07-31 | メルク シヤープ エンド ドーム リミテツド | 置換モルホリン誘導体およびその治療剤としての使用 |
| CN1046515C (zh) | 1993-12-29 | 1999-11-17 | 辉瑞大药厂 | 二氮杂双环神经激肽拮抗剂 |
| DE69504300T2 (de) | 1994-01-13 | 1999-04-29 | Merck Sharp & Dohme Ltd., Hoddesdon, Hertfordshire | Gem-bissubstituierte azazyclische tachykinin-antagonisten |
| US5728716A (en) | 1994-01-28 | 1998-03-17 | Merck Sharp & Dohme Limited | Aralkylamino substituted azacyclic therapeutic agents |
| US5393790A (en) | 1994-02-10 | 1995-02-28 | G.D. Searle & Co. | Substituted spiro compounds for the treatment of inflammation |
| US5631734A (en) | 1994-02-10 | 1997-05-20 | Affymetrix, Inc. | Method and apparatus for detection of fluorescently labeled materials |
| GB9402688D0 (en) | 1994-02-11 | 1994-04-06 | Merck Sharp & Dohme | Therapeutic agents |
| US5610165A (en) | 1994-02-17 | 1997-03-11 | Merck & Co., Inc. | N-acylpiperidine tachykinin antagonists |
| TW385308B (en) | 1994-03-04 | 2000-03-21 | Merck & Co Inc | Prodrugs of morpholine tachykinin receptor antagonists |
| WO1995024612A1 (de) | 1994-03-07 | 1995-09-14 | International Business Machines Corporation | Verfahren und vorrichtung zur schnellen interpolation von zwischenwerten aus periodischen phasenverschobenen signalen und zur erkennung von defekten in einem drehkörper |
| FI963597L (fi) | 1994-03-15 | 1996-11-14 | Eisai Co Ltd | Isoprenyylitransferaasi-inhibiittoreita |
| FR2718136B1 (fr) | 1994-03-29 | 1996-06-21 | Sanofi Sa | Composés aromatiques aminés, procédé pour leur obtention et compositions pharmaceutiques les contenant. |
| AU1615895A (en) | 1994-03-31 | 1995-10-12 | Bristol-Myers Squibb Company | Imidazole-containing inhibitors of farnesyl protein transferase |
| US5523430A (en) | 1994-04-14 | 1996-06-04 | Bristol-Myers Squibb Company | Protein farnesyl transferase inhibitors |
| US5610145A (en) | 1994-04-15 | 1997-03-11 | Warner-Lambert Company | Tachykinin antagonists |
| CZ104795A3 (en) | 1994-04-29 | 1996-02-14 | Lilly Co Eli | Benzimidazole derivative, process of its preparation, its use for preparing a pharmaceutical preparation and the pharmaceutical composition containing thereof |
| EP0758329A1 (en) | 1994-05-05 | 1997-02-19 | MERCK SHARP & DOHME LTD. | Morpholine derivatives and their use as antagonists of tachikinins |
| MX9605128A (es) | 1994-05-07 | 1997-08-30 | Boehringer Ingelheim Kg | Nuevos derivados de aminoacidos, procedimientos para su preparacion y composiciones farmaceuticas que contienen estos compuestos. |
| US5510510A (en) | 1994-05-10 | 1996-04-23 | Bristol-Meyers Squibb Company | Inhibitors of farnesyl protein transferase |
| US5571639A (en) | 1994-05-24 | 1996-11-05 | Affymax Technologies N.V. | Computer-aided engineering system for design of sequence arrays and lithographic masks |
| US5563255A (en) | 1994-05-31 | 1996-10-08 | Isis Pharmaceuticals, Inc. | Antisense oligonucleotide modulation of raf gene expression |
| EP0764163B1 (en) | 1994-06-06 | 2001-10-10 | Warner-Lambert Company | Tachykinin (nk 1) receptor antagonists |
| CA2150992A1 (en) | 1994-06-10 | 1995-12-11 | Philip Arthur Hipskind | Cyclohexyl tachykinin receptor antagonists |
| CN1150419A (zh) | 1994-06-10 | 1997-05-21 | 罗纳-布朗克罗莱尔股份有限公司 | 新的法呢基转移酶抑制剂、其制法及其药物组合物 |
| US5807522A (en) | 1994-06-17 | 1998-09-15 | The Board Of Trustees Of The Leland Stanford Junior University | Methods for fabricating microarrays of biological samples |
| US5571792A (en) | 1994-06-30 | 1996-11-05 | Warner-Lambert Company | Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase |
| CN1067067C (zh) | 1994-07-12 | 2001-06-13 | 伊莱利利公司 | 杂环速激肽受体拮抗物 |
| CA2154116A1 (en) | 1994-07-22 | 1996-01-23 | Philip Arthur Hipskind | 1-aryl-2-acetamidopentanone derivatives for use as tachykinin receptor antagonists |
| GB9415996D0 (en) | 1994-08-08 | 1994-09-28 | Merck Sharp & Dohme | Therapeutic agents |
| GB9415997D0 (en) | 1994-08-08 | 1994-09-28 | Merck Sharp & Dohme | Therapeutic agents |
| WO1996005529A1 (en) | 1994-08-09 | 1996-02-22 | Micron Optics, Inc. | Temperature compensated fiber fabry-perot filters |
| TW432061B (en) | 1994-08-09 | 2001-05-01 | Pfizer Res & Dev | Lactams |
| CA2155448A1 (en) | 1994-08-11 | 1996-02-12 | Katerina Leftheris | Inhibitors of farnesyl protein transferase |
| AU3192395A (en) | 1994-08-11 | 1996-03-07 | Banyu Pharmaceutical Co., Ltd. | Substituted amide derivative |
| AU3192495A (en) | 1994-08-12 | 1996-03-07 | Banyu Pharmaceutical Co., Ltd. | N,n-disubstituted amic acid derivative |
| PT777659E (pt) | 1994-08-15 | 2001-09-28 | Merck Sharp & Dohme | Derivados de morfolina e sua utilizacao como agentes terapeuticos |
| DE4429506B4 (de) | 1994-08-19 | 2007-09-13 | Degussa Gmbh | Verfahren zur Extraktion natürlicher Carotinoid-Farbstoffe |
| DE4429653C2 (de) | 1994-08-20 | 1997-04-03 | Anton Dr More | Konverter und Verfahren zum Frischen von Metallschmelzen insbesondere von Roheisen zu Stahl |
| HU221434B (en) | 1994-08-25 | 2002-10-28 | Merrell Pharma Inc | Substituted piperidines, pharmaceutical compositions containing them and their use |
| ATE158568T1 (de) | 1994-08-29 | 1997-10-15 | Akzo Nobel Nv | Verfahren zur herstellung von quaternären diestern |
| GB9417956D0 (en) | 1994-09-02 | 1994-10-26 | Merck Sharp & Dohme | Therapeutic agents |
| GB9418545D0 (en) | 1994-09-15 | 1994-11-02 | Merck Sharp & Dohme | Therapeutic agents |
| US5457107A (en) | 1994-09-16 | 1995-10-10 | Merck & Co., Inc. | Polymorphic form of a tachykinin receptor antagonist |
| CA2198382A1 (en) | 1994-09-30 | 1996-04-11 | Novartis Ag | 1-acyl-4-aliphatylaminopiperidine compounds |
| TW397825B (en) | 1994-10-14 | 2000-07-11 | Novartis Ag | Aroyl-piperidine derivatives |
| US5556752A (en) | 1994-10-24 | 1996-09-17 | Affymetrix, Inc. | Surface-bound, unimolecular, double-stranded DNA |
| FR2725986B1 (fr) | 1994-10-21 | 1996-11-29 | Adir | Nouveaux derives de piperidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| EP0709375B1 (en) | 1994-10-25 | 2005-05-18 | AstraZeneca AB | Therapeutic heterocycles |
| GB9421709D0 (en) | 1994-10-27 | 1994-12-14 | Zeneca Ltd | Therapeutic compounds |
| EP0714891A1 (en) | 1994-11-22 | 1996-06-05 | Eli Lilly And Company | Heterocyclic tachykinin receptor antagonists |
| JP4319251B2 (ja) | 1994-11-22 | 2009-08-26 | エヌエックスピー ビー ヴィ | 半導体素子を有し導体トラックが形成されている基板が接着層により結合されている支持本体を有する半導体装置 |
| FR2727411B1 (fr) | 1994-11-30 | 1997-01-03 | Rhone Poulenc Rorer Sa | Nouveaux derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent |
| CA2204144A1 (en) | 1994-12-09 | 1996-06-13 | Francis J. Tinney | Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase |
| PE38997A1 (es) | 1994-12-13 | 1997-10-02 | Novartis Ag | Antagonista de taquicinina |
| GB9426103D0 (en) | 1994-12-23 | 1995-02-22 | Merck Sharp & Dohme | Therapeutic agents |
| EA000164B1 (ru) | 1995-01-09 | 1998-10-29 | Магла Интернэшнл Лтд. | Состав для печати изображения на поверхности изделия из каучукового латекса, способ печати изображения и изделия из каучукового латекса |
| AU4437896A (en) | 1995-01-12 | 1996-07-31 | Glaxo Group Limited | Piperidine derivatives having tachykinin antagonist activity |
| JP3929069B2 (ja) | 1995-01-12 | 2007-06-13 | ユニバーシティ オブ ピッツバーグ | プレニルトランスフェラーゼの阻害剤 |
| FR2729390A1 (fr) | 1995-01-18 | 1996-07-19 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
| FR2729951B1 (fr) | 1995-01-30 | 1997-04-18 | Sanofi Sa | Nouveaux composes heterocycliques, procede pour leur preparation et compositions pharmaceutiques en contenant |
| FR2730492B1 (fr) | 1995-02-09 | 1997-03-14 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
| FR2730491B1 (fr) | 1995-02-09 | 1997-03-14 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
| US5633272A (en) | 1995-02-13 | 1997-05-27 | Talley; John J. | Substituted isoxazoles for the treatment of inflammation |
| GB9505491D0 (en) | 1995-03-18 | 1995-05-03 | Merck Sharp & Dohme | Therapeutic agents |
| GB9505492D0 (en) | 1995-03-18 | 1995-05-03 | Merck Sharp & Dohme | Therapeutic agents |
| US5554641A (en) | 1995-03-20 | 1996-09-10 | Horwell; David C. | Nonpeptides as tachykinin antagonists |
| GB9505692D0 (en) | 1995-03-21 | 1995-05-10 | Glaxo Group Ltd | Chemical compounds |
| EP0733632B1 (en) | 1995-03-24 | 2003-06-04 | Takeda Chemical Industries, Ltd. | Cyclic compounds, their production and use as tachykinin receptor antagonists |
| US5684013A (en) | 1995-03-24 | 1997-11-04 | Schering Corporation | Tricyclic compounds useful for inhibition of g-protein function and for treatment of proliferative diseases |
| US5700806A (en) | 1995-03-24 | 1997-12-23 | Schering Corporation | Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
| IL117580A0 (en) | 1995-03-29 | 1996-07-23 | Merck & Co Inc | Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them |
| US5565568A (en) | 1995-04-06 | 1996-10-15 | Eli Lilly And Company | 2-acylaminopropanamides as tachykinin receptor antagonists |
| CA2217351C (en) | 1995-04-07 | 2003-03-18 | Schering Corporation | Carbonyl-piperazinyl and piperidinyl compounds which inhibit farnesyl protein transferase |
| IL117798A (en) | 1995-04-07 | 2001-11-25 | Schering Plough Corp | Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them |
| US5891872A (en) | 1995-04-07 | 1999-04-06 | Schering Corporation | Tricyclic compounds |
| US5712280A (en) | 1995-04-07 | 1998-01-27 | Schering Corporation | Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
| JP3950170B2 (ja) | 1995-04-13 | 2007-07-25 | アベンティス・ファーマスーティカルズ・インコーポレイテッド | タキキニン受容体アンタゴニスト活性を有する新規な置換されたピペラジン誘導体 |
| US5831115A (en) | 1995-04-21 | 1998-11-03 | Abbott Laboratories | Inhibitors of squalene synthase and protein farnesyltransferase |
| US5624711A (en) | 1995-04-27 | 1997-04-29 | Affymax Technologies, N.V. | Derivatization of solid supports and methods for oligomer synthesis |
| IL118101A0 (en) | 1995-05-03 | 1996-09-12 | Abbott Lab | Inhibitors of farnesyltransferase |
| HUP9900822A3 (en) | 1995-05-25 | 1999-11-29 | Fujisawa Pharmaceutical Co | Piperazine derivatives, process for producing them, pharmaceutical compositions containing them and method for treating tachykinin-mediated diseases |
| US5545531A (en) | 1995-06-07 | 1996-08-13 | Affymax Technologies N.V. | Methods for making a device for concurrently processing multiple biological chip assays |
| US5919780A (en) | 1995-06-16 | 1999-07-06 | Warner Lambert Company | Tricyclic inhibitors of protein farnesyltransferase |
| GB9513121D0 (en) | 1995-06-28 | 1995-08-30 | Merck Sharp & Dohme | Therapeutic agents |
| GB9513118D0 (en) | 1995-06-28 | 1995-08-30 | Merck Sharp & Dohme | Therapeutic agents |
| GB9513117D0 (en) | 1995-06-28 | 1995-08-30 | Merck Sharp & Dohme | Therapeutic agents |
| JP3042894B2 (ja) | 1995-07-07 | 2000-05-22 | ファイザー製薬株式会社 | サブスタンスｐアンタゴニストとしての置換ベンゾラクタム化合物 |
| FR2736641B1 (fr) | 1995-07-10 | 1997-08-22 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
| AT402617B (de) | 1995-07-11 | 1997-07-25 | Datacon Schweitzer & Zeindl Gm | Anlage zum automatisierten, hermetischen anlage zum automatisierten, hermetischen verschliessen von gehäusen verschliessen von gehäusen |
| FR2736638B1 (fr) | 1995-07-12 | 1997-08-22 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
| CH690163A5 (fr) | 1995-07-28 | 2000-05-31 | Symphar Sa | Dérivés gem-diphosphonates substitués utiles en tant qu'agents anti-cancers. |
| US5569588A (en) | 1995-08-09 | 1996-10-29 | The Regents Of The University Of California | Methods for drug screening |
| TW340842B (en) | 1995-08-24 | 1998-09-21 | Pfizer | Substituted benzylaminopiperidine compounds |
| US5661028A (en) | 1995-09-29 | 1997-08-26 | Lockheed Martin Energy Systems, Inc. | Large scale DNA microsequencing device |
| US6020343A (en) | 1995-10-13 | 2000-02-01 | Merck Frosst Canada, Inc. | (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors |
| JP2002534955A (ja) | 1995-10-18 | 2002-10-15 | メルク エンド カンパニー インコーポレーテッド | シクロペンチルタキキニン受容体アンタゴニスト |
| DE19541283A1 (de) | 1995-11-06 | 1997-05-07 | Boehringer Ingelheim Kg | Neue Aminosäurederivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
| AU7597596A (en) | 1995-11-06 | 1997-05-29 | University Of Pittsburgh | Inhibitors of protein isoprenyl transferases |
| GB9523244D0 (en) | 1995-11-14 | 1996-01-17 | Merck Sharp & Dohme | Therapeutic agents |
| US6288237B1 (en) | 1995-11-17 | 2001-09-11 | Gesellschaft Fur Biotechnologische Forschung Mbh (Gbf) | Epothilons C and D, preparation and compositions |
| CA2238081A1 (en) | 1995-11-22 | 1997-05-29 | S. Jane Desolms | Inhibitors of farnesyl-protein transferase |
| AU715558B2 (en) | 1995-11-23 | 2000-02-03 | Merck Sharp & Dohme Limited | Spiro-piperidine derivatives and their use as tachykinin antagonists |
| GB9524157D0 (en) | 1995-11-25 | 1996-01-24 | Pfizer Ltd | Therapeutic agents |
| HU224225B1 (hu) | 1995-12-01 | 2005-06-28 | Sankyo Co. Ltd. | Tachikinin receptor antagonista hatású heterociklusos vegyületek, ezek előállítási eljárása és alkalmazásuk gyógyszerkészítmények előállítására |
| ATE215541T1 (de) | 1995-12-08 | 2002-04-15 | Janssen Pharmaceutica Nv | (imidazol-5-yl)methyl-2-chinolinoderivate als farnesyl protein transferase inhibitoren |
| GB9525296D0 (en) | 1995-12-11 | 1996-02-07 | Merck Sharp & Dohme | Therapeutic agents |
| US6022963A (en) | 1995-12-15 | 2000-02-08 | Affymetrix, Inc. | Synthesis of oligonucleotide arrays using photocleavable protecting groups |
| WO1997023478A1 (en) | 1995-12-22 | 1997-07-03 | Schering Corporation | Tricyclic amides useful for inhibition of g-protein function and for treatment of proliferative diseases |
| AU1529997A (en) | 1996-01-16 | 1997-08-11 | Warner-Lambert Company | Substituted histidine inhibitors of protein farnesyltransferase |
| US6673927B2 (en) | 1996-02-16 | 2004-01-06 | Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. | Farnesyl transferase inhibitors |
| US5744349A (en) * | 1996-03-05 | 1998-04-28 | Washington University | DNA sequences encoding human Myt1 kinase |
| CA2249601A1 (en) | 1996-04-03 | 1997-10-23 | Thorsten E. Fisher | Inhibitors of farnesyl-protein transferase |
| PT1288206E (pt) | 1996-04-12 | 2008-11-14 | Searle Llc | Derivados de benzenossulfonamida substituídos como pró-fármacos de inibidores de cox-2 |
| IL126833A0 (en) | 1996-05-22 | 1999-08-17 | Warner Lambert Co | Inhibitors of protein farnesyl transferase |
| CA2260216A1 (en) | 1996-07-15 | 1998-01-22 | Bristol-Myers Squibb Company | Thiadioxobenzodiazepine inhibitors of farnesyl protein transferase |
| US5861419A (en) | 1996-07-18 | 1999-01-19 | Merck Frosst Canad, Inc. | Substituted pyridines as selective cyclooxygenase-2 inhibitors |
| US6020194A (en) * | 1996-10-04 | 2000-02-01 | California Institute Of Technology | DNA encoding a Myt1 polypeptide |
| CA2273083C (en) | 1996-12-03 | 2012-09-18 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| AU6013998A (en) | 1996-12-30 | 1998-07-31 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| WO1998029119A1 (en) | 1996-12-30 | 1998-07-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| ATE252387T1 (de) | 1998-11-23 | 2003-11-15 | Novartis Pharma Gmbh | Verwendung von staurosporine derivaten zur behandlung von okularen neovaskularen erkrankungen |
| IL144578A0 (en) | 1999-01-29 | 2002-05-23 | Imclone Systems Inc | Antibodies specific to kdr and uses thereof |
| GB9904387D0 (en) | 1999-02-25 | 1999-04-21 | Pharmacia & Upjohn Spa | Antitumour synergistic composition |
| AU4972900A (en) | 1999-04-08 | 2000-11-14 | Arch Development Corporation | Use of anti-vegf antibody to enhance radiation in cancer therapy |
| US6077674A (en) | 1999-10-27 | 2000-06-20 | Agilent Technologies Inc. | Method of producing oligonucleotide arrays with features of high purity |
| ES2275657T3 (es) | 2000-03-20 | 2007-06-16 | MERCK SHARP & DOHME LTD. | Derivados de bicicloalquilo puenteados sulfonamido sustituidos. |
| GB0012671D0 (en) | 2000-05-24 | 2000-07-19 | Merck Sharp & Dohme | Therapeutic agents |
| GB0025173D0 (en) | 2000-10-13 | 2000-11-29 | Merck Sharp & Dohme | Therapeutic agents |
| ES2248397T3 (es) | 2000-11-02 | 2006-03-16 | MERCK SHARP & DOHME LTD. | Sulfamidas como inhibidores de la gamma-secretasa. |
| UA74849C2 (en) | 2000-11-17 | 2006-02-15 | Lilly Co Eli | Lactam |
| GB0108591D0 (en) | 2001-04-05 | 2001-05-23 | Merck Sharp & Dohme | Therapeutic agents |
| GB0108592D0 (en) | 2001-04-05 | 2001-05-23 | Merck Sharp & Dohme | Therapeutic agents |
| WO2002083139A1 (en) | 2001-04-10 | 2002-10-24 | Merck & Co., Inc. | Inhibitors of akt activity |
| US6958334B2 (en) | 2001-04-10 | 2005-10-25 | Merck & Co., Inc. | Inhibitors of Akt activity |
| AU2002251266A1 (en) | 2001-04-10 | 2002-10-28 | Merck Sharp And Dohme Limited | Inhibitors of akt activity |
| AU2002307163B2 (en) | 2001-04-10 | 2006-06-29 | Merck & Co., Inc. | A method of treating cancer |
| CA2442270C (en) | 2001-04-10 | 2009-09-08 | Merck & Co., Inc. | Inhibitors of akt activity |
| GB0119152D0 (en) | 2001-08-06 | 2001-09-26 | Merck Sharp & Dohme | Therapeutic agents |
| WO2003013526A1 (en) | 2001-08-08 | 2003-02-20 | Merck & Co. Inc. | Anticoagulant compounds |
| WO2003018543A1 (en) | 2001-08-21 | 2003-03-06 | Merck Sharp & Dohme Limited | Novel cyclohexyl sulphones |
| AU2002332122A1 (en) | 2001-10-15 | 2003-04-28 | The Medstar Research Institute | Modulation of akt-dependent response to prevent restenosis |
| EP1442132A2 (en) | 2001-10-26 | 2004-08-04 | Novartis AG | Methods for the treatment of osteoarthritis and compositions thereof |
| JP2005511581A (ja) | 2001-11-07 | 2005-04-28 | メルク エンド カムパニー インコーポレーテッド | 有糸分裂キネシン阻害剤 |
| ES2291543T3 (es) | 2001-12-06 | 2008-03-01 | MERCK & CO., INC. | Inhibicion de kinesina mitotica. |
| CA2468156A1 (en) | 2001-12-06 | 2003-06-19 | Merck & Co., Inc. | Azolopyrimidinone compounds and their use |
| JP2005515208A (ja) | 2001-12-06 | 2005-05-26 | メルク エンド カムパニー インコーポレーテッド | 有糸分裂性キネシン阻害剤 |
| US20050107404A1 (en) | 2001-12-06 | 2005-05-19 | Fraley Mark E. | Mitotic kinesin inhibitors |
| EP1458726B1 (en) | 2001-12-06 | 2009-07-15 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| JP4399269B2 (ja) | 2002-03-08 | 2010-01-13 | メルク エンド カムパニー インコーポレーテッド | 有糸分裂性キネシン阻害薬 |
| WO2003086403A1 (en) | 2002-04-08 | 2003-10-23 | Merck & Co., Inc. | Inhibitors of akt activity |
| US7223738B2 (en) | 2002-04-08 | 2007-05-29 | Merck & Co., Inc. | Inhibitors of Akt activity |
| WO2003086404A1 (en) | 2002-04-08 | 2003-10-23 | Merck & Co., Inc. | Fused quinoxaline derivatives as inhibitors of akt activity |
| WO2003084473A2 (en) | 2002-04-08 | 2003-10-16 | Merck & Co., Inc. | Method of treating cancer |
| CA2481229C (en) | 2002-04-08 | 2010-09-21 | Merck & Co., Inc. | Substituted pyrazine inhibitors of akt |
| GB0209991D0 (en) | 2002-05-01 | 2002-06-12 | Merck Sharp & Dohme | Therapeutic agents |
| GB0209995D0 (en) | 2002-05-01 | 2002-06-12 | Merck Sharp & Dohme | Therapeutic agents |
| WO2003093252A1 (en) | 2002-05-01 | 2003-11-13 | Merck Sharp & Dohme Limited | Heteroaryl substituted spirocyclic sulfamides for inhibition of gamma secretase |
| GB0209997D0 (en) | 2002-05-01 | 2002-06-12 | Merck Sharp & Dohme | Therapeutic agents |
| CA2483627A1 (en) | 2002-05-23 | 2003-12-04 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| WO2004039774A2 (en) | 2002-05-23 | 2004-05-13 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| AU2003276005B2 (en) | 2002-06-14 | 2009-01-15 | Merck Sharp & Dohme Corp. | Mitotic kinesin inhibitors |
| CA2487489C (en) | 2002-06-14 | 2010-11-23 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| GB0223040D0 (en) | 2002-10-04 | 2002-11-13 | Merck Sharp & Dohme | Therapeutic compounds |
| GB0223038D0 (en) | 2002-10-04 | 2002-11-13 | Merck Sharp & Dohme | Therapeutic compounds |
| GB0223039D0 (en) | 2002-10-04 | 2002-11-13 | Merck Sharp & Dohme | Therapeutic compounds |
| EP1556052A4 (en) | 2002-10-18 | 2006-11-02 | Merck & Co Inc | MITOTIC KINESINE HEMMER |
| JP2006507299A (ja) | 2002-10-30 | 2006-03-02 | メルク エンド カムパニー インコーポレーテッド | Ａｋｔ活性の阻害薬 |
| US20040102360A1 (en) | 2002-10-30 | 2004-05-27 | Barnett Stanley F. | Combination therapy |
| GB0225475D0 (en) | 2002-11-01 | 2002-12-11 | Merck Sharp & Dohme | Therapeutic agents |
| GB0225474D0 (en) | 2002-11-01 | 2002-12-11 | Merck Sharp & Dohme | Therapeutic agents |
| CA2508346A1 (en) | 2002-12-06 | 2004-06-24 | Pharmacia Corporation | Mitoneet polypeptide from mitochondrial membranes, modulators thereof, and methods of using the same |
| AU2003297230B2 (en) | 2002-12-20 | 2009-11-26 | Merck Sharp & Dohme Corp. | Mitotic kinesin inhibitors |
| WO2004058700A2 (en) | 2002-12-20 | 2004-07-15 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| GB0308318D0 (en) | 2003-04-10 | 2003-05-14 | Merck Sharp & Dohme | Therapeutic agents |
| ATE461179T1 (de) | 2003-04-24 | 2010-04-15 | Merck Sharp & Dohme | Hemmer der akt aktivität |
| JP2006524254A (ja) | 2003-04-24 | 2006-10-26 | メルク エンド カムパニー インコーポレーテッド | Ａｋｔ活性の阻害剤 |
| WO2004096135A2 (en) | 2003-04-24 | 2004-11-11 | Merck & Co., Inc. | Inhibitors of akt activity |
| AU2004233828B2 (en) | 2003-04-24 | 2009-05-28 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| WO2004101539A1 (en) | 2003-05-16 | 2004-11-25 | Merck Sharp & Dohme Limited | Cyclic sulfonamides for inhibition of gamma-secretase |
| CA2527533A1 (en) | 2003-06-12 | 2004-12-29 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| US7454431B2 (en) | 2003-07-17 | 2008-11-18 | At&T Corp. | Method and apparatus for window matching in delta compressors |
| GB0318447D0 (en) | 2003-08-05 | 2003-09-10 | Merck Sharp & Dohme | Therapeutic agents |
| KR100536215B1 (ko) | 2003-08-05 | 2005-12-12 | 삼성에스디아이 주식회사 | 플라즈마 디스플레이 패널 |
| US7307085B2 (en) | 2003-08-13 | 2007-12-11 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| JP4773961B2 (ja) | 2003-08-15 | 2011-09-14 | メルク・シャープ・エンド・ドーム・コーポレイション | 有糸分裂キネシン阻害薬 |
| AR045342A1 (es) | 2003-08-15 | 2005-10-26 | Merck & Co Inc | Inhibidores de quinesina mitotica |
| JP2007502775A (ja) | 2003-08-15 | 2007-02-15 | メルク エンド カムパニー インコーポレーテッド | 有糸分裂キネシン阻害剤 |
| CN1835756A (zh) | 2003-08-15 | 2006-09-20 | 默克公司 | 有丝分裂驱动蛋白抑制剂 |
| WO2005030731A1 (en) | 2003-09-24 | 2005-04-07 | Merck Sharp & Dohme Limited | Gamma-secretase inhibitors |
| US7294640B2 (en) | 2004-02-06 | 2007-11-13 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| WO2005100344A1 (en) | 2004-04-09 | 2005-10-27 | Merck & Co., Inc. | Inhibitors of akt activity |
| EP1737861A4 (en) | 2004-04-09 | 2010-04-28 | Merck Sharp & Dohme | HEMMER OF ACT ACTIVITY |
| CA2597456A1 (en) | 2005-02-14 | 2006-08-31 | Merck & Co., Inc. | Inhibitors of akt activity |
| CN101155588A (zh) | 2005-04-12 | 2008-04-02 | 默克公司 | Akt活性的抑制剂 |
| KR100959771B1 (ko) | 2005-06-10 | 2010-05-28 | 머크 샤프 앤드 돔 코포레이션 | Ａｋｔ 활성의 억제제 |
| WO2007076129A2 (en) | 2005-12-23 | 2007-07-05 | Nanostring Technologies, Inc. | Nanoreporters and methods of manufacturing and use thereof |
| AR060635A1 (es) | 2006-04-27 | 2008-07-02 | Banyu Pharma Co Ltd | Derivados de 1,2-dihidro-3h-pirazolo[3,4-d]pirimidin-3-ona, composiciones farmaceuticas que los comprenden y su uso en el tratamiento del cancer |
| EP2155752B1 (en) * | 2007-04-25 | 2018-09-19 | Merck Sharp & Dohme Corp. | Polymorph of dihydropyrazolopyrimidinone derivative as weel kinase.inhibitor |
| CN101784551A (zh) | 2007-06-15 | 2010-07-21 | 万有制药株式会社 | 二环苯胺衍生物 |
| ES2430053T3 (es) * | 2008-06-12 | 2013-11-18 | Merck Sharp & Dohme Corp. | Procedimiento para producir derivados de bicicloanilina |
| ES2524161T3 (es) | 2009-09-15 | 2014-12-04 | Merck Sharp & Dohme Corp. | Preparación de formas hemihidratadas cristalinas de dihidropirazolopirimidinona |
| BR112013011918A2 (pt) * | 2010-11-16 | 2020-08-25 | Array Biopharma, Inc | inibidor de chk1, composição farmacêutica e kit compreendendo o referido inibidor |
| WO2013039854A1 (en) * | 2011-09-15 | 2013-03-21 | Merck Sharp & Dohme Corp. | Compositions and methods for treating cancer |
-
2013
- 2013-11-22 SM SM20170595T patent/SMT201700595T1/it unknown
- 2013-11-22 HU HUE13858495A patent/HUE035662T2/en unknown
- 2013-11-22 DK DK13858495.8T patent/DK2925888T3/en active
- 2013-11-22 BR BR112015012295A patent/BR112015012295A8/pt not_active Application Discontinuation
- 2013-11-22 ES ES13858495.8T patent/ES2651347T3/es active Active
- 2013-11-22 MX MX2015006729A patent/MX363243B/es unknown
- 2013-11-22 KR KR1020157013523A patent/KR102161331B1/ko active Active
- 2013-11-22 EP EP13858495.8A patent/EP2925888B1/en active Active
- 2013-11-22 WO PCT/US2013/071377 patent/WO2014085216A1/en active Application Filing
- 2013-11-22 RU RU2015125575A patent/RU2660349C2/ru active
- 2013-11-22 RS RS20171325A patent/RS56680B1/sr unknown
- 2013-11-22 PT PT138584958T patent/PT2925888T/pt unknown
- 2013-11-22 SI SI201330904T patent/SI2925888T1/en unknown
- 2013-11-22 US US14/646,518 patent/US9655899B2/en active Active
- 2013-11-22 HR HRP20180002TT patent/HRP20180002T1/hr unknown
- 2013-11-22 JP JP2015544142A patent/JP6290237B2/ja active Active
- 2013-11-22 CA CA2892361A patent/CA2892361A1/en active Pending
- 2013-11-22 ME MEP-2017-295A patent/ME02925B/me unknown
- 2013-11-22 LT LTEP13858495.8T patent/LT2925888T/lt unknown
- 2013-11-22 PL PL13858495T patent/PL2925888T3/pl unknown
- 2013-11-22 AU AU2013352568A patent/AU2013352568B2/en active Active
-
2014
- 2014-01-02 NO NO14735382A patent/NO2941224T3/no unknown
-
2017
- 2017-11-30 CY CY20171101258T patent/CY1119676T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR102161331B1 (ko) | 2020-09-29 |
| HRP20180002T1 (hr) | 2018-02-09 |
| PL2925888T3 (pl) | 2018-03-30 |
| MX2015006729A (es) | 2015-08-14 |
| HK1209798A1 (en) | 2016-04-08 |
| EP2925888B1 (en) | 2017-10-25 |
| HUE035662T2 (en) | 2018-05-28 |
| US20160008361A1 (en) | 2016-01-14 |
| RS56680B1 (sr) | 2018-03-30 |
| AU2013352568B2 (en) | 2019-09-19 |
| EP2925888A1 (en) | 2015-10-07 |
| ME02925B (me) | 2018-04-20 |
| RU2660349C2 (ru) | 2018-07-05 |
| JP2016500110A (ja) | 2016-01-07 |
| NO2941224T3 (ru) | 2018-07-28 |
| LT2925888T (lt) | 2018-01-10 |
| AU2013352568A1 (en) | 2015-04-30 |
| CA2892361A1 (en) | 2014-06-05 |
| CY1119676T1 (el) | 2018-04-04 |
| US9655899B2 (en) | 2017-05-23 |
| SI2925888T1 (en) | 2018-02-28 |
| SMT201700595T1 (it) | 2018-03-08 |
| MX363243B (es) | 2019-03-14 |
| JP6290237B2 (ja) | 2018-03-07 |
| ES2651347T3 (es) | 2018-01-25 |
| BR112015012295A8 (pt) | 2023-03-14 |
| KR20150088257A (ko) | 2015-07-31 |
| EP2925888A4 (en) | 2016-05-11 |
| PT2925888T (pt) | 2017-12-13 |
| DK2925888T3 (en) | 2017-12-18 |
| WO2014085216A1 (en) | 2014-06-05 |
| BR112015012295A2 (pt) | 2017-07-11 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2015125575A (ru) | Композиции и способы для лечения злокачественной опухоли | |
| Zhou et al. | Increased expression of long-noncoding RNA ZFAS1 is associated with epithelial-mesenchymal transition of gastric cancer | |
| JP2016500110A5 (ru) | ||
| Zhen et al. | CircHMGCS1 promotes hepatoblastoma cell proliferation by regulating the IGF signaling pathway and glutaminolysis | |
| Yu et al. | IFITM1 promotes the metastasis of human colorectal cancer via CAV-1 | |
| Ries et al. | miR-186, miR-3651 and miR-494: potential biomarkers for oral squamous cell carcinoma extracted from whole blood | |
| Lv et al. | miRNA expression patterns in chemoresistant breast cancer tissues | |
| Zhou et al. | Tumor invasion and metastasis regulated by microRNA-184 and microRNA-574-5p in small-cell lung cancer | |
| Chen et al. | Comprehensive analysis of circular RNA profiling in AZD9291‐resistant non‐small cell lung cancer cell lines | |
| Pang et al. | miR-497 as a potential serum biomarker for the diagnosis and prognosis of osteosarcoma | |
| JP2017503481A5 (ru) | ||
| Sakabe et al. | Expression of cancer stem cell-associated DKK1 mRNA serves as prognostic marker for hepatocellular carcinoma | |
| Qu et al. | Long non-coding RNA ROR is a novel prognosis factor associated with non-small-cell lung cancer progression | |
| Su et al. | Ionizing radiation promotes advanced malignant traits in nasopharyngeal carcinoma via activation of epithelial-mesenchymal transition and the cancer stem cell phenotype | |
| Xie et al. | Overexpression of SPAG9 correlates with poor prognosis and tumor progression in hepatocellular carcinoma | |
| Lai et al. | DEPTOR expression negatively correlates with mTORC1 activity and tumor progression in colorectal cancer | |
| Lv et al. | Identification of miR-146b-5p in tissues as a novel biomarker for prognosis of gallbladder carcinoma | |
| Chen et al. | Effect of AKT inhibition on epithelial‑mesenchymal transition and ZEB1‑potentiated radiotherapy in nasopharyngeal carcinoma | |
| WO2017217807A3 (ko) | Nckap1을 유효성분으로 포함하는 대장암 진단 또는 대장암 전이 예후 예측용 바이오마커 조성물 | |
| Luan et al. | MiR-769-5p functions as an oncogene by down-regulating RYBP expression in gastric cancer. | |
| Karihtala et al. | Expression levels of microRNAs miR-93 and miR-200a in pancreatic adenocarcinoma with special reference to differentiation and relapse-free survival | |
| Renhua et al. | 165P: Long noncoding RNA LUCAT1 is associated with poor prognosis in human non-small cell lung cancer and affects cell proliferation via regulating p21 and p57 expression | |
| Hua et al. | An integrated pan-cancer analysis of identifying biomarkers about the EGR family genes in human carcinomas | |
| Hong et al. | Construction of a ferroptosis scoring system and identification of LINC01572 as a novel ferroptosis suppressor in lung adenocarcinoma | |
| Zhang et al. | LncRNA DQ786243 expression as a biomarker for assessing prognosis in patients with gastric cancer |