PE20150666A1 - Inhibidores de serina/treonina cinasa - Google Patents
Inhibidores de serina/treonina cinasaInfo
- Publication number
- PE20150666A1 PE20150666A1 PE2014001344A PE2014001344A PE20150666A1 PE 20150666 A1 PE20150666 A1 PE 20150666A1 PE 2014001344 A PE2014001344 A PE 2014001344A PE 2014001344 A PE2014001344 A PE 2014001344A PE 20150666 A1 PE20150666 A1 PE 20150666A1
- Authority
- PE
- Peru
- Prior art keywords
- serine
- kinase inhibitors
- threonine kinase
- compounds
- hyperproliferative
- Prior art date
Links
Classifications
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La invencion describe compuestos de formula l: o estereoisomeros, tautomeros, profarmacos o sales farmaceuticamente aceptables de los mismos, en la que R1, R2, R3, R4, X1, X2, Y1 y Y2 se definen en la presente solicitud. Estos compuestos son activos como inhibidores de serina/treonina cinasa, por lo que son utiles en el tratamiento de enfermedades hiperproliferativas e inflamatorias.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261605523P | 2012-03-01 | 2012-03-01 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20150666A1 true PE20150666A1 (es) | 2015-05-06 |
Family
ID=47892024
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2014001344A PE20150666A1 (es) | 2012-03-01 | 2013-03-01 | Inhibidores de serina/treonina cinasa |
Country Status (37)
Country | Link |
---|---|
US (4) | US8697715B2 (es) |
EP (2) | EP2820009B1 (es) |
JP (2) | JP6068515B2 (es) |
KR (1) | KR102093526B1 (es) |
CN (2) | CN104507926B (es) |
AR (2) | AR090220A1 (es) |
AU (1) | AU2013225737B2 (es) |
BR (1) | BR112014021634B1 (es) |
CA (1) | CA2866086C (es) |
CL (1) | CL2014002301A1 (es) |
CO (1) | CO7081155A2 (es) |
CR (1) | CR20140413A (es) |
CY (1) | CY1120172T1 (es) |
DK (2) | DK3321262T3 (es) |
ES (2) | ES2857649T3 (es) |
HK (3) | HK1204323A1 (es) |
HR (2) | HRP20180591T1 (es) |
HU (2) | HUE053994T2 (es) |
IL (2) | IL234376A (es) |
LT (2) | LT3321262T (es) |
MX (1) | MX354675B (es) |
MY (1) | MY191936A (es) |
NO (1) | NO2945854T3 (es) |
NZ (1) | NZ700314A (es) |
PE (1) | PE20150666A1 (es) |
PH (3) | PH12015501654A1 (es) |
PL (2) | PL3321262T3 (es) |
PT (2) | PT2820009T (es) |
RS (2) | RS57097B1 (es) |
RU (1) | RU2650501C2 (es) |
SG (1) | SG11201405356QA (es) |
SI (2) | SI3321262T1 (es) |
SM (1) | SMT201800282T1 (es) |
TW (1) | TWI589569B (es) |
UA (1) | UA116774C2 (es) |
WO (1) | WO2013130976A1 (es) |
ZA (2) | ZA201406688B (es) |
Families Citing this family (38)
Publication number | Priority date | Publication date | Assignee | Title |
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BR112013021896A2 (pt) | 2011-02-28 | 2016-11-08 | Array Biopharma Inc | inibidores de serina/treonina cinase |
RU2014108140A (ru) | 2011-08-04 | 2015-09-10 | Эррэй Биофарма Инк. | Соединение на основе хинозолина в качестве ингибиторов серен-треониновых киназ |
JP6068515B2 (ja) | 2012-03-01 | 2017-01-25 | アレイ バイオファーマ、インコーポレイテッド | セリン/トレオニンキナーゼ阻害剤 |
MX363118B (es) * | 2012-05-03 | 2019-03-11 | Genentech Inc | Derivados de pirazol aminopirimidina como moduladores de cinasa 2 de repeticion rica en leucina (lrrk2). |
MX369989B (es) | 2012-08-27 | 2019-11-27 | Array Biopharma Inc | Inhibidores de serina/treonina cinasa para el tratamiento de enfermedades hiperproliferativas. |
AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
CA2884766A1 (en) | 2012-10-16 | 2014-04-24 | Daniel Jon Burdick | Serine/threonine kinase inhibitors |
WO2017156493A1 (en) | 2016-03-11 | 2017-09-14 | Denali Therapeutics Inc. | Compounds, compositions, and methods |
US9532987B2 (en) * | 2013-09-05 | 2017-01-03 | Genentech, Inc. | Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases |
SI3063143T1 (sl) | 2013-11-01 | 2018-09-28 | Novartis Ag, | Aminoheteroaril benzamidi kot inhibitorji kinaze |
BR112016012844B1 (pt) * | 2013-12-06 | 2023-01-10 | Genentech, Inc | Composto e composições farmacêuticas |
BR112016015235A2 (pt) * | 2013-12-30 | 2017-08-08 | Genentech Inc | Composto, composição farmacêutica, método de inibição da atividade da proteína quinase erk e método de tratamento |
WO2015103137A1 (en) | 2013-12-30 | 2015-07-09 | Array Biopharma Inc. | Serine/threonine kinase inhibitors |
MX2016012808A (es) | 2014-04-02 | 2017-01-05 | Intermune Inc | Piridinonas anti-fibroticas. |
TWI762806B (zh) | 2014-04-09 | 2022-05-01 | 美商建南德克公司 | 作為erk抑制劑之化合物 |
TWI704151B (zh) | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Erk抑制劑 |
WO2016106009A1 (en) | 2014-12-22 | 2016-06-30 | Eli Lilly And Company | Erk inhibitors |
CN106536522B (zh) * | 2015-06-03 | 2020-08-28 | 捷思英达医药技术(上海)有限公司 | 用于治疗银屑病的杂环化合物 |
WO2016192063A1 (en) * | 2015-06-03 | 2016-12-08 | Changzhou Jiekai Pharmatech Co. Ltd | Heterocyclic compounds as erk inhibitors |
ES2989326T3 (es) | 2015-10-21 | 2024-11-26 | Otsuka Pharma Co Ltd | Compuestos de benzolactama como inhibidores de la proteína cinasa |
EP3365335B1 (en) * | 2015-10-23 | 2024-02-14 | Array Biopharma, Inc. | 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2h)-one compounds as inhibitors of fgfr tyrosine kinases |
CR20180316A (es) | 2015-11-09 | 2018-10-05 | Astrazeneca Ab | Derivados de dihidroimidazopirazinona usados en el tratamiento del cáncer |
US11214565B2 (en) | 2015-11-20 | 2022-01-04 | Denali Therapeutics Inc. | Compound, compositions, and methods |
KR20180134347A (ko) | 2016-04-15 | 2018-12-18 | 제넨테크, 인크. | 암의 진단 및 치료 방법 |
UA126231C2 (uk) | 2016-06-16 | 2022-09-07 | Деналі Терапьютікс Інк. | Піримідин-2-іламіно-1н-піразоли як інгібітори lrrk2 для застосування при лікуванні нейродегенеративних захворювань |
GB201706327D0 (en) | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
CN111032656B (zh) * | 2017-08-22 | 2022-12-02 | 捷思英达医药技术(上海)有限公司 | 杂环化合物激酶抑制剂及其药物组合物和应用 |
CA3073073A1 (en) | 2017-09-08 | 2019-03-14 | F. Hoffmann-La Roche Ag | Diagnostic and therapeutic methods for cancer |
CN111433195B (zh) | 2017-11-24 | 2023-04-25 | 诺华股份有限公司 | 吡啶酮衍生物及其作为选择性alk-2抑制剂的用途 |
ES2936627T3 (es) * | 2018-02-08 | 2023-03-21 | Zhangzhou Pien Tze Huang Pharm | Compuesto de pirazina-2(1H)-cetona como inhibidor de FGFR |
EP3752200A1 (en) | 2018-02-13 | 2020-12-23 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
US12133841B2 (en) | 2018-05-22 | 2024-11-05 | Js Innomed Holdings Ltd. | Heterocyclic compounds as kinase inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof |
WO2020131627A1 (en) | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
WO2020192750A1 (zh) * | 2019-03-28 | 2020-10-01 | 江苏恒瑞医药股份有限公司 | 噻吩并杂环类衍生物、其制备方法及其在医药上的应用 |
CN113784970B (zh) * | 2019-05-15 | 2022-11-29 | 南京明德新药研发有限公司 | Erk抑制剂及其应用 |
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