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PE20090058A1 - Compuestos carboxamida heterociclicos como inhibidores de la actividad akt - Google Patents

Compuestos carboxamida heterociclicos como inhibidores de la actividad akt

Info

Publication number
PE20090058A1
PE20090058A1 PE2008000249A PE2008000249A PE20090058A1 PE 20090058 A1 PE20090058 A1 PE 20090058A1 PE 2008000249 A PE2008000249 A PE 2008000249A PE 2008000249 A PE2008000249 A PE 2008000249A PE 20090058 A1 PE20090058 A1 PE 20090058A1
Authority
PE
Peru
Prior art keywords
alkyl
inhibitors
carboxamide compounds
heterocyclic carboxamide
akt activity
Prior art date
Application number
PE2008000249A
Other languages
English (en)
Inventor
Mark Andrew Seefeld
Meagan B Route
Dirk A Heerding
Simon Peace
Dennis S Yamashita
Kenneth C Mcnulty
Original Assignee
Smithkline Beecham Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39682107&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20090058(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of PE20090058A1 publication Critical patent/PE20090058A1/es

Links

Classifications

    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/12—Ketones
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Immunology (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A COMPUESTOS DE CARBOXAMIDA HETEROCICLICOS DE FORMULA (I), EN DONDE R41Y R42 SON INDEPENDIENTEMENTE H, UN GRUPO DE FORMULA a), HALOGENO, ALQUILO(C1-C4), ALQUILOXI(C1-C4), OPCIONALMENTE SUSTITUIDOS, FURANO, TIOFENO, ENTRE OTROS; R43 ES H, ALQUILO(C1-C4), ALQUILOXI(C1-C4), ENTRE OTROS; R44 ESTA AUSENTE O ES -(CR60R61)mAR; R45 ES H O ALQUILO(C1-C4); R20 ES H O ALQUILO(C1-C4), E HIDROXI; X ES O, S Y NR49, DONDE R49 ES H O ALQUILO(C1-C4); n ES DE 0 A 2 Y ESTE RESTO SI ES APLICABLE ESTA SUSTITUIDO CON HIDROXIALQUILO(C1-C4). SON SELECCIONADOS N-[2-AMINO-1-(FENILMETIL)ETIL]-4-BROMO-5-(1-METHYL-1H-PIRAZOL-5-IL)-2-FURANOCARBOXAMIDA, N-[2-AMINO-1-(FENILMETIL)ETIL]-5-(1-METIL-1H-PIRAZOL-5-IL)-2-TIENOCARBOXAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON INHIBIDORES DE LA ACTIVIDAD DE LA PROTEINA QUINASA B (PKB O AKT), SIENDO UTILES EN EL TRATAMIENTO DE CANCER Y ARTRITIS
PE2008000249A 2007-02-07 2008-02-05 Compuestos carboxamida heterociclicos como inhibidores de la actividad akt PE20090058A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US88858607P 2007-02-07 2007-02-07

Publications (1)

Publication Number Publication Date
PE20090058A1 true PE20090058A1 (es) 2009-04-03

Family

ID=39682107

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008000249A PE20090058A1 (es) 2007-02-07 2008-02-05 Compuestos carboxamida heterociclicos como inhibidores de la actividad akt

Country Status (35)

Country Link
US (7) US8410158B2 (es)
EP (1) EP2117523B1 (es)
JP (3) JP4723677B2 (es)
KR (3) KR20140140570A (es)
CN (1) CN101646427B (es)
AR (1) AR066184A1 (es)
AU (1) AU2008213694B2 (es)
BR (1) BRPI0807146B8 (es)
CA (1) CA2678255C (es)
CL (1) CL2008000348A1 (es)
CO (1) CO6220930A2 (es)
CR (1) CR10995A (es)
CY (1) CY1115535T1 (es)
DK (1) DK2117523T3 (es)
DO (1) DOP2009000196A (es)
EA (1) EA018038B1 (es)
ES (1) ES2501518T3 (es)
HK (1) HK1132676A1 (es)
HR (1) HRP20140790T1 (es)
IL (1) IL200212A (es)
JO (1) JO3134B1 (es)
MA (1) MA31167B1 (es)
MX (2) MX367398B (es)
MY (1) MY164480A (es)
NZ (1) NZ579177A (es)
PE (1) PE20090058A1 (es)
PL (1) PL2117523T3 (es)
PT (1) PT2117523E (es)
SG (1) SG193678A1 (es)
SI (1) SI2117523T1 (es)
TW (2) TWI507194B (es)
UA (1) UA102992C2 (es)
UY (1) UY30892A1 (es)
WO (1) WO2008098104A1 (es)
ZA (1) ZA200905363B (es)

Families Citing this family (110)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7625890B2 (en) 2005-11-10 2009-12-01 Smithkline Beecham Corp. Substituted imidazo[4,5-c]pyridine compounds as Akt inhibitors
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
JP5581219B2 (ja) 2008-01-25 2014-08-27 ミレニアム ファーマシューティカルズ， インコーポレイテッド チオフェンおよびホスファチジルイノシトール３−キナーゼ（ｐｉ３ｋ）阻害薬としてのその使用
US20100048524A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
US9394333B2 (en) 2008-12-02 2016-07-19 Wave Life Sciences Japan Method for the synthesis of phosphorus atom modified nucleic acids
MA32998B1 (fr) * 2009-01-30 2012-01-02 Glaxosmithkline Llc Chlorhydrate de n-{(1-s)-2-amino-1-[(3-fluorophényl) méthyl]éthyl}-5-chloro-4-(4-chloro-1-methyl-1h-pyrazol-5-yl)-2-thiophènecarboxamide cristallin
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
CA2750935A1 (en) 2009-01-30 2010-08-12 Millennium Pharmaceuticals, Inc. Heteroaryls and their use as pi3k inhibitors
EP2393827B1 (en) 2009-02-05 2015-10-07 Tokai Pharmaceuticals, Inc. Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
RU2612521C2 (ru) 2009-07-06 2017-03-09 Онтории, Инк. Новые пролекарства нуклеиновых кислот и способы их применения
MX2012003546A (es) * 2009-09-23 2012-09-07 Glaxosmithkline Llc Combinacion.
US20120283278A1 (en) * 2009-09-23 2012-11-08 Melissa Dumble Combination
US8835450B2 (en) * 2009-10-08 2014-09-16 Glaxosmithkline Llc Combination of inhibitor of B-Raf and an inhibitor of Akt in the treatment of cancer
EP2485594B1 (en) * 2009-10-08 2015-01-07 GlaxoSmithKline LLC Combination
WO2011060380A1 (en) * 2009-11-14 2011-05-19 The Regents Of The University Of California Pik3ca mutation status and sash1 expression predicts synergy between lapatinib and an akt inhibitor in her2 positive breast cancer
BR112012024380A2 (pt) 2010-03-25 2015-09-15 Glaxosmithkline Llc compostos químicos
MX355038B (es) 2010-03-30 2018-03-28 Verseon Corp Compuestos aromáticos multisustituidos como inhibidores de trombina.
WO2011146710A1 (en) 2010-05-21 2011-11-24 Glaxosmithkline Llc Combination
WO2011150044A1 (en) * 2010-05-26 2011-12-01 Glaxosmithkline Llc Combination
US8859768B2 (en) 2010-08-11 2014-10-14 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9062038B2 (en) 2010-08-11 2015-06-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US8796271B2 (en) 2010-08-11 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
EP2620428B1 (en) 2010-09-24 2019-05-22 Wave Life Sciences Ltd. Asymmetric auxiliary group
EA201390539A1 (ru) 2010-10-13 2013-09-30 Милленниум Фармасьютикалз, Инк. Гетероарилы и их применение
TWI505828B (zh) 2010-12-20 2015-11-01 葛蘭素史克智慧財產（第二）有限公司 新穎醫藥組成物
SG191724A1 (en) 2011-01-11 2013-08-30 Glaxosmithkline Llc Combination
US20120184562A1 (en) 2011-01-19 2012-07-19 Kin-Chun Luk 1,6- and 1,8-naphthyridines
US20120184548A1 (en) 2011-01-19 2012-07-19 Romyr Dominique Carboxylic acid aryl amides
US20120184542A1 (en) 2011-01-19 2012-07-19 Kevin Anderson Pyrido pyrimidines
US8362023B2 (en) 2011-01-19 2013-01-29 Hoffmann-La Roche Inc. Pyrazolo pyrimidines
US8673905B2 (en) 2011-03-17 2014-03-18 Hoffmann-La Roche Inc. Imidazo pyrazines
WO2012177925A1 (en) 2011-06-21 2012-12-27 The Board Institute, Inc. Akt inhibitors for treating cancer expressing a magi3 - akt3 fusion gene
JP6128529B2 (ja) 2011-07-19 2017-05-17 ウェイブ ライフ サイエンシズ リミテッドＷａｖｅ Ｌｉｆｅ Ｓｃｉｅｎｃｅｓ Ｌｔｄ． 官能化核酸の合成のための方法
EP2793880A4 (en) * 2011-12-23 2015-06-24 Millennium Pharm Inc HETEROARYLE AND USES THEREOF
PE20142356A1 (es) * 2012-04-24 2015-01-30 Glaxosmithkline Intellectual Property (N 2) Limited Metodo de tratamiento de las dermatosis sensibles a los esteroides
KR101835401B1 (ko) 2012-07-13 2018-03-08 신 니뽄 바이오메디칼 라보라토리즈, 엘티디. 키랄 핵산 어쥬번트
WO2014012081A2 (en) 2012-07-13 2014-01-16 Ontorii, Inc. Chiral control
CN104684893B (zh) 2012-07-13 2016-10-26 日本波涛生命科学公司 不对称辅助基团
CA2884848C (en) 2012-09-28 2017-08-22 Pfizer Inc. Benzamide and heterobenzamide compounds
JP6251277B2 (ja) 2012-10-16 2017-12-20 ヤンセン ファーマシューティカ エヌ．ベー． ＲＯＲ−ガンマ−ｔのフェニル結合キノリニルモジュレーター
SG11201502369XA (en) 2012-10-16 2015-05-28 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of ror-gamma-t
WO2014062655A1 (en) 2012-10-16 2014-04-24 Janssen Pharmaceutica Nv HETEROARYL LINKED QUINOLINYL MODULATORS OF RORyt
CA2889051A1 (en) * 2012-10-22 2014-05-01 Glaxosmithkline Llc Combination
JP6232443B2 (ja) 2012-11-30 2017-11-15 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ 新規な医薬組成物
CA2897559A1 (en) 2013-01-09 2014-07-17 Glaxosmithkline Intellectual Property (No.2) Limited Combination
EP2961747B1 (en) 2013-02-27 2017-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
CA2904170A1 (en) 2013-03-14 2014-09-25 University Of Maryland, Baltimore Androgen receptor down-regulating agents and uses thereof
MX373646B (es) * 2013-03-15 2020-04-02 Verseon Corp Halogeno-pirazoles como inhibidores de trombina.
PT2968297T (pt) 2013-03-15 2019-01-10 Verseon Corp Compostos aromáticos multissubstituídos como inibidores da serina protease
KR20160104612A (ko) 2013-07-26 2016-09-05 업데이트 파마 인코포레이트 비산트렌의 치료 효과 개선용 조성물
MX2016001901A (es) 2013-08-12 2016-10-13 Tokai Pharmaceuticals Inc Biomarcadores para tratamiento de trastornos neoplasicos usando terapias dirigidas con andrógeno.
EP3052097A1 (en) * 2013-10-01 2016-08-10 Novartis AG Combination
AU2014330780B2 (en) 2013-10-01 2017-05-25 Novartis Ag Enzalutamide in combination with Afuresertib for the treatment of cancer
WO2015057629A1 (en) 2013-10-15 2015-04-23 Janssen Pharmaceutica Nv ALKYL LINKED QUINOLINYL MODULATORS OF RORyt
US10555941B2 (en) 2013-10-15 2020-02-11 Janssen Pharmaceutica Nv Alkyl linked quinolinyl modulators of RORγt
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
US9284308B2 (en) 2013-10-15 2016-03-15 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of RORγt
BR112016008258A2 (pt) 2013-10-15 2017-10-10 Janssen Pharmaceutica Nv moduladores de ror?t de quinolinila
US9403816B2 (en) 2013-10-15 2016-08-02 Janssen Pharmaceutica Nv Phenyl linked quinolinyl modulators of RORγt
WO2015056180A1 (en) 2013-10-15 2015-04-23 Glaxosmithkline Intellectual Property (No.2) Limited Indoline derivatives as inhibitors of perk
US9328095B2 (en) 2013-10-15 2016-05-03 Janssen Pharmaceutica Nv Heteroaryl linked quinolinyl modulators of RORgammat
CA2926313A1 (en) 2013-10-15 2015-04-23 Kristi A. Leonard Secondary alcohol quinolinyl modulators of roryt
MY176489A (en) 2013-12-24 2020-08-12 Bristol Myers Squibb Co Novel tricyclic compounds as anticancer agents
US10149905B2 (en) 2014-01-15 2018-12-11 Shin Nippon Biomedical Laboratories, Ltd. Chiral nucleic acid adjuvant having antitumor effect and antitumor agent
WO2015108047A1 (ja) 2014-01-15 2015-07-23 株式会社新日本科学 免疫誘導活性を有するキラル核酸アジュバンド及び免疫誘導活性剤
JPWO2015108046A1 (ja) 2014-01-15 2017-03-23 株式会社新日本科学 抗アレルギー作用を有するキラル核酸アジュバンド及び抗アレルギー剤
EP3094728B1 (en) 2014-01-16 2022-03-09 Wave Life Sciences Ltd. Chiral design
MX2016011674A (es) * 2014-03-12 2017-04-27 Novartis Ag Combinacion que comprende un inhibidor de btk y un inhibidor de akt.
CN104926801B (zh) 2014-03-22 2019-06-04 浙江大学 取代氮杂环类衍生物、含其的药物组合物及其在抗肿瘤中的应用
EP3125920B1 (en) 2014-04-04 2020-12-23 Del Mar Pharmaceuticals Dianhydrogalactitol, diacetyldianhydrogalactitol or dibromodulcitol to treat non-small-cell carcinoma of the lung and ovarian cancer
MA39999A (fr) 2014-06-06 2015-12-10 Res Triangle Inst Agonistes du récepteur de l'apeline (apj) et leurs utilisations
US10189810B2 (en) 2014-09-17 2019-01-29 Verseon Corporation Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
WO2016059602A2 (en) 2014-10-16 2016-04-21 Glaxo Group Limited Methods of treating cancer and related compositions
TW201630907A (zh) 2014-12-22 2016-09-01 必治妥美雅史谷比公司 ＴＧＦβＲ拮抗劑
SI3261639T1 (sl) 2015-02-27 2023-01-31 Verseon International Corporation Substituirane pirazolne spojine kot zaviralci serinskih proteaz
WO2017037578A2 (en) 2015-08-28 2017-03-09 Novartis Ag Combination therapy
WO2017098421A1 (en) 2015-12-08 2017-06-15 Glaxosmithkline Intellectual Property Development Limited Benzothiadiazine compounds
KR20180090852A (ko) 2015-12-09 2018-08-13 리써치 트라이앵글 인스티튜트 개선된 아펠린 수용체(apj) 효능제 및 이의 용도
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
WO2017153952A1 (en) 2016-03-10 2017-09-14 Glaxosmithkline Intellectual Property Development Limited 5-sulfamoyl-2-hydroxybenzamide derivatives
CN109311908B (zh) * 2016-06-16 2021-05-07 哈尔滨珍宝制药有限公司 作为Akt抑制剂的二氢吡唑氮杂卓类化合物
EP3526209B1 (en) * 2016-10-12 2025-04-16 Research Triangle Institute Heterocyclic apelin receptor (apj) agonists and uses thereof
KR20190090824A (ko) 2016-12-01 2019-08-02 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 암을 치료하는 방법
CN107011377B (zh) * 2017-05-03 2019-02-26 南通书创药业科技有限公司 一种β-羰基磷酸酯的制备方法
CA3068936A1 (en) 2017-07-05 2019-01-10 Novartis Ag Novel pharmaceutical composition
TW201922721A (zh) 2017-09-07 2019-06-16 英商葛蘭素史克智慧財產發展有限公司 化學化合物
WO2019053617A1 (en) 2017-09-12 2019-03-21 Glaxosmithkline Intellectual Property Development Limited CHEMICAL COMPOUNDS
ES2943092T3 (es) 2017-12-13 2023-06-08 Harbin Zhenbao Pharmaceutical Co Ltd Sal que sirve como inhibidor de Akt y cristal de la misma
US20210300939A1 (en) 2018-07-23 2021-09-30 Signalrx Pharmaceuticals, Inc. Single Molecule Compounds Providing Multi-Target Inhibition of BTK and Other Proteins and Methods of Use Thereof
EP3866807A1 (en) 2018-10-16 2021-08-25 F. Hoffmann-La Roche AG Use of akt inhibitors in ophthalmology
US20220033775A1 (en) 2018-11-05 2022-02-03 Iovance Biotherapeutics, Inc. Expansion of tils utilizing akt pathways inhibitors
IL310831A (en) 2018-11-30 2024-04-01 Glaxosmithkline Ip Dev Ltd Compounds useful in curing HIV
US20220040324A1 (en) 2018-12-21 2022-02-10 Daiichi Sankyo Company, Limited Combination of antibody-drug conjugate and kinase inhibitor
CN110031626A (zh) * 2019-04-02 2019-07-19 浙江理工大学 一种用于胃肠道间质肿瘤迁移的标志物ack1及其应用
WO2021018941A1 (en) 2019-07-31 2021-02-04 Glaxosmithkline Intellectual Property Development Limited Methods of treating cancer
CN114080225A (zh) 2019-08-08 2022-02-22 来凯有限公司 治疗癌症的方法
EP4021450A1 (en) 2019-08-26 2022-07-06 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
WO2021118924A2 (en) 2019-12-12 2021-06-17 Ting Therapeutics Llc Compositions and methods for the prevention and treatment of hearing loss
US12014835B2 (en) 2020-02-19 2024-06-18 Vanderbilt University Methods for evaluating therapeutic benefit of combination therapies
EP4125840A1 (en) 2020-03-27 2023-02-08 Som Innovation Biotech, S.A. Compounds for use in the treatment of synucleinopathies
CN111592531B (zh) * 2020-06-23 2023-08-15 上海鲲博玖瑞医药科技发展有限公司 福瑞塞替的制备方法
CN111620860B (zh) * 2020-06-23 2023-02-03 济南健丰化工有限公司 一种福瑞塞替的制备方法
WO2022069554A1 (de) 2020-10-01 2022-04-07 Bayer Aktiengesellschaft Verfahren zur herstellung von 4-bromfuran-2-carboxylaten
CN119013022A (zh) 2022-03-14 2024-11-22 来凯有限公司 癌症的组合治疗
WO2023187037A1 (en) 2022-03-31 2023-10-05 Astrazeneca Ab Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer
AR129423A1 (es) 2022-05-27 2024-08-21 Viiv Healthcare Co Compuestos útiles en la terapia contra el hiv
WO2024083716A1 (en) 2022-10-17 2024-04-25 Astrazeneca Ab Combinations of a serd for the treatment of cancer
WO2024100236A1 (en) 2022-11-11 2024-05-16 Astrazeneca Ab Combination therapies for the treatment of cancer
TW202448458A (zh) 2023-06-02 2024-12-16 美商亞文納營運公司 雌激素受體降解劑與ａｋｔ抑制劑之組合

Family Cites Families (178)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1030415A (zh) 1987-02-20 1989-01-18 山之内制药株式会社 饱和的杂环碳酰胺衍生物和它的制备方法
ES2005163A6 (es) 1987-04-14 1989-03-01 Lilly S A E Un procedimiento para la produccion de derivados de tiofen-2-carboxamida.
PT90001B (pt) 1988-03-16 1994-06-30 Zambeletti Spa L Processo para a preparacao de derivados heterociclicos de etilenodiamina
DE3810848A1 (de) 1988-03-30 1989-10-19 Boehringer Ingelheim Kg Neue 2,3,4-substituierte imidazole und 3,4,5-substituierte 1,2,4-triazole, ihre herstellung und verwendung
DE3927483A1 (de) 1989-08-19 1991-02-21 Boehringer Ingelheim Kg Neue substituierte heterocyclische fuenfringe, ihre herstellung und verwendung
US5258357A (en) 1989-10-07 1993-11-02 Basf Aktiengesellschaft Carboxamides, their preparation and their use as herbicides
DE3933573A1 (de) * 1989-10-07 1991-04-18 Basf Ag Carbonsaeureamide, verfahren zu ihrer herstellung und ihre verwendung als herbizide
US6645969B1 (en) 1991-05-10 2003-11-11 Aventis Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
US5559235A (en) 1991-10-29 1996-09-24 Glaxo Wellcome Inc. Water soluble camptothecin derivatives
GB9201755D0 (en) 1992-01-28 1992-03-11 British Bio Technology Compounds
US5595872A (en) 1992-03-06 1997-01-21 Bristol-Myers Squibb Company Nucleic acids encoding microsomal trigyceride transfer protein
US5342947A (en) 1992-10-09 1994-08-30 Glaxo Inc. Preparation of water soluble camptothecin derivatives
EP0667773A4 (en) 1992-10-14 1996-09-25 Merck & Co Inc FIBRINOGEN RECEPTOR ANTAGONISTS.
EP0665833B1 (en) 1992-10-23 1999-07-14 MERCK SHARP & DOHME LTD. Dopamine receptor subtype ligands
FR2707295A1 (fr) 1993-06-07 1995-01-13 Rhone Poulenc Agrochimie Fongicides pyrazoles substitués en position 3 par un hétérocycle.
DE69418045T2 (de) * 1993-08-06 1999-10-07 Smithkline Beecham P.L.C., Brentford Amidderivate als 5ht1d rezeptor antagonisten
US5739135A (en) * 1993-09-03 1998-04-14 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
US5491237A (en) 1994-05-03 1996-02-13 Glaxo Wellcome Inc. Intermediates in pharmaceutical camptothecin preparation
US5668148A (en) * 1995-04-20 1997-09-16 Merck & Co., Inc. Alpha1a adrenergic receptor antagonists
JP3964478B2 (ja) 1995-06-30 2007-08-22 エーザイ・アール・アンド・ディー・マネジメント株式会社 ヘテロ環含有カルボン酸誘導体及びそれを含有する医薬
US5846990A (en) * 1995-07-24 1998-12-08 Bristol-Myers Squibb Co. Substituted biphenyl isoxazole sulfonamides
AU6870396A (en) 1995-08-02 1997-02-26 J. Uriach & Cia S.A. New pyrimidone derivatives with antifungal activity
JPH10507205A (ja) * 1995-08-02 1998-07-14 ホータ．ウリアッヒ イ シイア．エセ．アー． 抗真菌活性を有する新規カルボンアミド
USRE39088E1 (en) * 1995-08-22 2006-05-02 Japan Tobacco, Inc. Amide compounds and use of the same
US6001866A (en) * 1995-10-05 1999-12-14 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
US5972980A (en) 1995-10-05 1999-10-26 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
AU6966696A (en) 1995-10-05 1997-04-28 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
US5942544A (en) * 1996-02-22 1999-08-24 Dupont Pharmaceuticals Company α-branched anilines, toluenes, and analogs thereof as factor Xa inhibitors
JP2001509131A (ja) 1996-04-03 2001-07-10 メルク エンド カンパニー インコーポレーテッド ファルネシルプロテイントランスフェラーゼの阻害剤
AU706150B2 (en) 1996-04-03 1999-06-10 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0891357A1 (en) 1996-04-03 1999-01-20 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997036897A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0891333A1 (en) 1996-04-03 1999-01-20 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU706497B2 (en) 1996-04-03 1999-06-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP2000507593A (ja) 1996-04-03 2000-06-20 メルク エンド カンパニー インコーポレーテッド ファルネシル―タンパク質トランスフェラーゼ阻害剤
EP0891351A1 (en) 1996-04-03 1999-01-20 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0891339A1 (en) 1996-04-03 1999-01-20 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AUPO163896A0 (en) * 1996-08-14 1996-09-05 Resmed Limited Determination of respiratory airflow
WO1998037068A1 (en) * 1997-02-21 1998-08-27 Bristol-Myers Squibb Company Benzoic acid derivatives and related compounds as antiarrhythmic agents
US5998336A (en) 1997-02-26 1999-12-07 The Board Of Trustees Of The Leland Stanford Junior University Ceramic/metal and A15/metal superconducting composite materials exploiting the superconducting proximity effect and method of making the same
US6359134B1 (en) 1997-05-30 2002-03-19 Takeda Chemical Industries, Ltd. Sulfonamide derivatives, their production and use
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
DE19744026A1 (de) 1997-10-06 1999-04-08 Hoechst Marion Roussel De Gmbh Pyrazol-Derivate, ihre Herstellung und ihre Verwendung in Arzneimitteln
AU751139B2 (en) * 1997-10-13 2002-08-08 Astellas Pharma Inc. Amide derivative
KR100349385B1 (ko) 1997-12-12 2002-08-24 유로-셀티크 소시에떼 아노뉨 2-티오크산틴으로부터 얻어진 3-치환 아데닌
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
AUPP433398A0 (en) 1998-06-25 1998-07-16 Australian National University, The Compounds and processes
US6192967B1 (en) * 1998-10-19 2001-02-27 Sunny En Liung Huang Collapsible auto shade
US6130333A (en) * 1998-11-27 2000-10-10 Monsanto Company Bicyclic imidazolyl derivatives as phosphodiesterase inhibitors, pharmaceutical compositions and method of use
GB9827882D0 (en) 1998-12-17 1999-02-10 Smithkline Beecham Plc Novel compounds
DE19904396A1 (de) 1999-02-04 2000-08-10 Bayer Ag Substituierte Pyrazolbenzylamin-Derivate
DE19904397A1 (de) 1999-02-04 2000-08-10 Bayer Ag Verwendung von Pyrazol-Carbonsäureamiden
JP2000256358A (ja) 1999-03-10 2000-09-19 Yamanouchi Pharmaceut Co Ltd ピラゾール誘導体
HUP0203338A2 (hu) 1999-04-13 2003-03-28 Abbott Gmbh & Co. Kg Integrin receptor ligandumok
JP2003500383A (ja) 1999-05-24 2003-01-07 コア・セラピューティクス，インコーポレイテッド 第Ｘａ因子阻害剤
CA2374646A1 (en) 1999-05-24 2000-11-30 Cor Therapeutics, Inc. Inhibitors of factor xa
JP2001247569A (ja) 1999-08-12 2001-09-11 Japan Tobacco Inc ピロリジン誘導体又はピペリジン誘導体及びその医薬用途
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
EP1235807A1 (en) 1999-11-24 2002-09-04 Millennium Pharmaceuticals, Inc. B-amino acid-, aspartic acid- and diaminopropionic-based inhibitors of factor xa
EP1162196A4 (en) 1999-12-27 2003-04-16 Japan Tobacco Inc COMPOUNDS WITH JOINED CYCLES AND THEIR USE AS MEDICAMENTS
US6770666B2 (en) 1999-12-27 2004-08-03 Japan Tobacco Inc. Fused-ring compounds and use thereof as drugs
EP1207864A2 (en) 2000-02-05 2002-05-29 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of erk
EP1196390A2 (en) 2000-02-05 2002-04-17 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of erk
CZ20013540A3 (cs) * 2000-02-05 2002-03-13 Vertex Pharmaceuticals Incorporated Deriváty pyrazolu jako inhibitory ERK a farmaceutický prostředek, který je obsahuje
WO2001064642A2 (en) 2000-02-29 2001-09-07 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
GB0011098D0 (en) 2000-05-08 2000-06-28 Black James Foundation Pharmaceutical compositions comprising protpn pump inhibitors and gastrin/cholecystokinin receptor ligands
WO2001087287A2 (en) 2000-05-19 2001-11-22 Applied Research Systems Ars Holding N.V. Use of pyrazole derivatives for treating infertility
US6589195B1 (en) * 2000-05-26 2003-07-08 Orthomerica Products, Inc. Modular adjustable prophylactic hip orthosis and adduction/abduction joint
US6599926B2 (en) * 2000-06-23 2003-07-29 Bristol-Myers Squibb Company Heteroaryl-phenyl substituted factor Xa inhibitors
AU2001277143A1 (en) 2000-07-24 2002-02-05 Davide Riccardo Grassetti Inhibition of mutagenic effects of carcinogens
GB0018758D0 (en) * 2000-07-31 2000-09-20 Smithkline Beecham Plc Novel use and compunds
JO2654B1 (en) * 2000-09-04 2012-06-17 شركة جانسين فارماسوتيكا ان. في Multiple aryl caroxa amides are useful as lipid - lowering agents
JP4267920B2 (ja) * 2001-01-26 2009-05-27 中外製薬株式会社 代謝調節剤として有用なマロニル−ＣｏＡ脱炭酸酵素阻害剤
CA2445568A1 (en) * 2001-04-27 2002-11-07 Vertex Pharmaceuticals Incorporated Triazole-derived kinase inhibitors and uses thereof
DE10223912A1 (de) * 2001-06-28 2003-01-16 Merck Patent Gmbh TN- und STN-Flüssigkristallanzeigen
US20030015823A1 (en) * 2001-07-18 2003-01-23 Hydranautics Method for forming a thick section, thermoset, solid casting
CA2456192A1 (en) * 2001-08-03 2003-02-13 Qing Tang Pyrazole-derived kinase inhibitors and uses thereof
EP1423380B1 (en) * 2001-08-03 2010-12-15 Vertex Pharmaceuticals Incorporated Pyrazole-derived kinase inhibitors and uses thereof
EP1419161A1 (en) * 2001-08-24 2004-05-19 PHARMACIA & UPJOHN COMPANY Substituted-heteroaryl-7-aza 2.2.1]bicycloheptanes for the treatment of disease
CA2458661A1 (en) * 2001-09-27 2003-04-03 Applied Research Systems Ars Holding N.V. Methods of increasing endogenous testosterone levels
US6794252B2 (en) * 2001-09-28 2004-09-21 Texas Instruments Incorporated Method and system for forming dual work function gate electrodes in a semiconductor device
WO2003035619A1 (en) 2001-10-25 2003-05-01 Merck & Co., Inc. Tyrosine kinase inhibitors
US6897208B2 (en) * 2001-10-26 2005-05-24 Aventis Pharmaceuticals Inc. Benzimidazoles
WO2003039529A1 (en) * 2001-11-07 2003-05-15 4Sc A.G. Selective antibacterial agents
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
JP4656838B2 (ja) * 2002-02-06 2011-03-23 バーテックス ファーマシューティカルズ インコーポレイテッド Ｇｓｋ−３の阻害剤として有用なヘテロアリール化合物
US7335779B2 (en) 2002-03-08 2008-02-26 Quonova, Llc Modulation of pathogenicity
GB0206860D0 (en) * 2002-03-22 2002-05-01 Glaxo Group Ltd Compounds
GB0206861D0 (en) * 2002-03-22 2002-05-01 Glaxo Group Ltd Medicaments
CA2480856A1 (en) 2002-04-05 2003-10-23 Merck & Co., Inc. Substituted aryl amides
BR0309556A (pt) * 2002-04-26 2005-02-09 Pfizer Prod Inc Inibidores de metaloproteinase pirimidina-2,4,6-triona
US7470543B2 (en) * 2002-06-05 2008-12-30 Nerviano Medical Sciences S.R.L. Methods for identifying ligands using competitive binding 1H NMR experiments
GB0216224D0 (en) * 2002-07-12 2002-08-21 Glaxo Group Ltd Compounds
US20060122234A1 (en) * 2002-08-02 2006-06-08 Argenta Discovery Limited Substituted thienyl-hydroxamic acids as histone deacetylase inhibitors
EP1536790A2 (en) * 2002-08-09 2005-06-08 AstraZeneca AB Oxadiazoles as modulators of metabotropic glutamate receptor-5
AU2003265395A1 (en) * 2002-08-14 2004-03-03 Ppd Discovery, Inc. Prenylation inhibitors and methods of their synthesis and use
US6649638B1 (en) * 2002-08-14 2003-11-18 Ppd Discovery, Inc. Prenylation inhibitors and methods of their synthesis and use
DE60333762D1 (de) 2002-08-23 2010-09-23 Novartis Vaccines & Diagnostic Pyrrolverbindungen als glykogen synthase kinase 3 inhibitoren
DE10239443A1 (de) 2002-08-28 2004-03-11 Boehringer Ingelheim International Gmbh Blockiervorrichtung für ein Sperrspannwerk mit federbetätigtem Abtrieb
EP1398029A1 (en) * 2002-09-10 2004-03-17 LION Bioscience AG NR3B1 nuclear receptor binding 3-substituted pyrazole derivatives
WO2004054515A2 (en) 2002-12-13 2004-07-01 Smithkline Beecham Corporation Thrombopoietin mimetics
JP2006511583A (ja) 2002-12-20 2006-04-06 ファルマシア・コーポレーション マイトジェン活性化プロテインキナーゼ−活性化プロテインキナーゼ−２を阻害するための非環式ピラゾール化合物
CA2515235A1 (en) * 2003-02-10 2004-08-19 Bayer Healthcare Ag Bis(hetero)aryl carboxamide derivatives for use as pgi2 antagonists
WO2004072018A1 (ja) 2003-02-12 2004-08-26 Takeda Pharmaceutical Company Limited アミン誘導体
US7223788B2 (en) * 2003-02-14 2007-05-29 Sanofi-Aventis Deutschland Gmbh Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
EP1599447A1 (en) * 2003-02-28 2005-11-30 Galderma Research & Development, S.N.C. Ligands that modulate lxr-type receptors
US7517887B2 (en) 2003-04-09 2009-04-14 General Atomics Reversible inhibitors of S-adenosyl-L-homocysteine hydrolase and uses thereof
TW200512195A (en) * 2003-04-21 2005-04-01 Elan Pharm Inc Benzamide 2-hydroxy-3-diaminoalkanes
JP4716996B2 (ja) * 2003-05-26 2011-07-06 武田薬品工業株式会社 スルホピロール
MXPA05013645A (es) * 2003-06-20 2006-02-24 Galderma Res & Dev Nuevos compuestos moduladores de los receptores de tipo ppar gama y su utilizacion en composiciones cosmeticas o farmaceuticas.
DE10331305A1 (de) 2003-07-10 2005-02-17 Siemens Ag Kommunikationssystem, Peer-to-Peer-Nachrichten-Filter-Rechner und Verfahren zum Verarbeiten einer Peer-to-Peer-Nachricht
FR2857666B1 (fr) 2003-07-15 2005-08-26 Oreal Composition tinctoriale comprenant a titre de coupleur un derive du furane et nouveaux derives du furane
ATE492278T1 (de) 2003-07-23 2011-01-15 Synta Pharmaceuticals Corp Verbindungen gegen entzündungen und immun- relevante verwendungen
WO2005019200A2 (en) 2003-08-14 2005-03-03 Icos Corporation Aryl piperidine derivatives as vla-1 integrin antagonists and uses thereof
EP1660487B1 (en) 2003-08-15 2008-03-19 Vertex Pharmaceuticals Incorporated Pyrrole compositions useful as inhibitors of c-met
WO2005019182A1 (en) 2003-08-20 2005-03-03 Bayer Healthcare Ag Pyrazolylmethylbenzamide derivatives as p2xt-receptor antagonists
US20070004771A1 (en) * 2003-10-06 2007-01-04 Glaxo Group Limited Preparation of 1,6,7-trisubstituted azabenzimidazoles as kinase inhibitors
EP1689393A4 (en) * 2003-10-06 2008-12-17 Glaxo Group Ltd PREPARATION OF 1,7-DISUBSTITUTED AZABENZIMIDAZOLES AS KINASE INHIBITORS
EP1684762A4 (en) 2003-11-13 2009-06-17 Ambit Biosciences Corp UREA DERIVATIVES AS MODULATORS OF KINASE
RU2006121990A (ru) 2003-11-21 2007-12-27 Эррэй Биофарма Инк. (Us) Ингибиторы протеинкиназ акт
US8652089B2 (en) 2004-01-19 2014-02-18 Arthrex, Inc. System for distending body tissue cavities by continuous flow irrigation
WO2005074642A2 (en) 2004-01-30 2005-08-18 Smithkline Beecham Corporation Chemical compounds
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005081954A2 (en) 2004-02-25 2005-09-09 Wyeth Inhibitors of protein tyrosine phosphatase 1b
WO2005099200A1 (en) * 2004-03-30 2005-10-20 Matsushita Electric Industrial Co., Ltd. Content relay server, content relay system, content relay method, and program using the same
RU2006138036A (ru) * 2004-03-30 2008-05-10 Чирон Корпорейшн (Us) Производные замещенного тиофена в качестве противораковых средств
WO2005097765A1 (en) 2004-03-31 2005-10-20 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
JP2005336172A (ja) 2004-04-26 2005-12-08 Japan Tobacco Inc 腎虚血再灌流障害治療又は予防薬
TW200600492A (en) * 2004-05-18 2006-01-01 Achillion Pharmaceuticals Inc Substituted aryl acylthioureas and related compounds; inhibitors of viral replication
AU2005247610A1 (en) * 2004-05-29 2005-12-08 7Tm Pharma A/S Substituted thiazoleacetic as crth2 ligands
JP2008503490A (ja) * 2004-06-17 2008-02-07 センジェント・セラピューティクス・インコーポレイテッド チロシンホスファターゼの三置換窒素調節物質
AU2005260689B2 (en) * 2004-06-30 2012-05-10 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of protein kinases
US7671077B2 (en) * 2004-07-19 2010-03-02 Leu-Fen Hou Lin Neuroprotective small organic molecules, compositions and uses related thereto
US20060019967A1 (en) 2004-07-21 2006-01-26 Su-Ying Wu SARS CoV main protease inhibitors
US20060019968A1 (en) * 2004-07-24 2006-01-26 Laboratorios Dr. Esteve S.A. Use of compounds active on the sigma receptor for the treatment of neuropathic pain
US7269099B2 (en) 2004-07-30 2007-09-11 Bolt Technology Corporation Air gun
JP2006066488A (ja) * 2004-08-25 2006-03-09 Mitsubishi Electric Corp 半導体受光素子およびその製造方法
US7365385B2 (en) * 2004-08-30 2008-04-29 Micron Technology, Inc. DRAM layout with vertical FETs and method of formation
US20060043513A1 (en) * 2004-09-02 2006-03-02 Deok-Hoon Kim Method of making camera module in wafer level
TW200616969A (en) 2004-09-17 2006-06-01 Tanabe Seiyaku Co Imidazole compound
US20060062453A1 (en) * 2004-09-23 2006-03-23 Sharp Laboratories Of America, Inc. Color highlighting document image processing
WO2006043518A1 (ja) 2004-10-18 2006-04-27 Santen Pharmaceutical Co., Ltd. 神経疾患治療剤
JP2006120339A (ja) 2004-10-19 2006-05-11 Matsushita Electric Ind Co Ltd 高周波加熱電源装置
TW200619843A (en) 2004-10-20 2006-06-16 Sumitomo Bakelite Co Semiconductor wafer and semiconductor device
DE102004051277A1 (de) * 2004-10-21 2006-04-27 Merck Patent Gmbh Heterocyclische Carbonylverbindungen
DE102004054666A1 (de) 2004-11-12 2006-05-18 Bayer Cropscience Gmbh Substituierte Pyrazol-3-carboxamide, Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren
JP2008520732A (ja) 2004-11-23 2008-06-19 ワイス ゴナドトロピン放出ホルモン受容体アンタゴニスト
WO2006058879A1 (en) * 2004-11-30 2006-06-08 Neurosearch A/S Novel diazabicyclic aryl derivatives as cholinergy ligands
SE527990C2 (sv) 2004-12-06 2006-08-01 Mora Of Sweden Ab Isborr
CN101141957A (zh) 2005-02-03 2008-03-12 Irm责任有限公司 作为ppar调节剂的化合物和组合物
JP2006232707A (ja) 2005-02-23 2006-09-07 Japan Tobacco Inc 癌転移抑制剤
US20080207760A1 (en) 2005-04-11 2008-08-28 Achillion Pharmaceuticals, Inc. Pharmaceutical Compositions For and Methods of Inhibiting Hcv
WO2006116355A1 (en) * 2005-04-22 2006-11-02 Kalypsys, Inc. Ortho-terphenyl inhibitors of p38 kinase and methods of treating inflammatory disorders
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
WO2006136829A2 (en) 2005-06-21 2006-12-28 Astex Therapeutics Limited Pyrazole derivatives and their use as pka and pkb modulators
US20060288588A1 (en) 2005-06-22 2006-12-28 Frank Morabito Garden tool
US8541461B2 (en) * 2005-06-23 2013-09-24 Astex Therapeutics Limited Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators
WO2006136637A2 (es) * 2005-06-24 2006-12-28 Eloy Antonio Martinez Albal Implante dental de corona rotatoria
WO2006138744A2 (en) * 2005-06-24 2006-12-28 Genelabs Technologies, Inc. Heteroaryl derivatives for treating viruses
BRPI0612287A8 (pt) 2005-06-27 2019-01-22 Exelixis Inc composição para uso farmacêutico no tratamento de doenças através da medicina nuclear e métodos de uso e para modulação de atividade de receptor nuclear
CN100494167C (zh) 2005-08-02 2009-06-03 天津大学 抗乙肝病毒的叔胺氧化物及制备方法和制备药物的应用
GB0518237D0 (en) 2005-09-07 2005-10-19 Angeletti P Ist Richerche Bio Therapeutic compounds
WO2007052843A1 (ja) 2005-11-04 2007-05-10 Takeda Pharmaceutical Company Limited 複素環アミド化合物およびその用途
US7838676B2 (en) * 2005-11-21 2010-11-23 Amgen Inc. Beta-secretase modulators and methods of use
US8163749B2 (en) 2005-12-14 2012-04-24 Bristol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
EP1968568A4 (en) 2005-12-22 2011-04-13 Glaxosmithkline Llc HEMMER OF NUTS ACTIVITY
CA2634787C (en) * 2005-12-23 2014-10-21 Smithkline Beecham Corporation Azaindole inhibitors of aurora kinases
AR056882A1 (es) 2006-02-01 2007-10-31 Bayer Cropscience Sa Derivados del fungicida n- cicloalquil- bencil- amida
NZ570847A (en) 2006-02-28 2011-10-28 Helicon Therapeutics Inc Therapeutic compounds
JP2007277230A (ja) 2006-03-15 2007-10-25 Tanabe Seiyaku Co Ltd 医薬組成物
EP2518063B1 (en) 2006-12-21 2017-02-01 Sloan-Kettering Institute For Cancer Research Pyridazinones and furan-containing compounds
JP2010513530A (ja) 2006-12-22 2010-04-30 エンサイシブ・ファーマシューティカルズ・インコーポレイテッド Ｃ３ａ受容体の調節剤およびその使用方法
EP2114388B1 (en) 2007-02-07 2015-05-20 GlaxoSmithKline LLC Inhibitors of akt activity
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
WO2008121685A1 (en) 2007-03-28 2008-10-09 Smithkline Beecham Corporation Methods of use for inhibitors of akt activity
EP2134175A4 (en) 2007-03-29 2012-01-11 Glaxosmithkline Llc HAMMER OF ACT ACTIVITY

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