AR067413A1 - Compuestos heterociclicos que contienen ciclopenta[d]pirimidina inhibidores de proteinquinasas akt, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de las mismas para el tratamiento de enfermedades hiperproliferativas, tales como cancer - Google Patents

Compuestos heterociclicos que contienen ciclopenta[d]pirimidina inhibidores de proteinquinasas akt, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de las mismas para el tratamiento de enfermedades hiperproliferativas, tales como cancer

Info

Publication number
AR067413A1
AR067413A1 ARP080102885A ARP080102885A AR067413A1 AR 067413 A1 AR067413 A1 AR 067413A1 AR P080102885 A ARP080102885 A AR P080102885A AR P080102885 A ARP080102885 A AR P080102885A AR 067413 A1 AR067413 A1 AR 067413A1
Authority
AR
Argentina
Prior art keywords
alkyl
phenyl
membered
troliferative
tiperiferative
Prior art date
Application number
ARP080102885A
Other languages
English (en)
Original Assignee
Genentech Inc
Array Biopharma Inc
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
Application filed by Genentech Inc, Array Biopharma Inc filed Critical Genentech Inc
Publication of AR067413A1 publication Critical patent/AR067413A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Virology (AREA)
  • Psychology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)

Abstract

Reivindicacion 1: Un compuesto de la formula (1) y sus enantiomeros y sales, donde: G es fenilo, naftaleno, un heteroarilo de 5-6 miembros o un heteroarilo bicíclico de 9-10 miembros, donde el fenilo, naftaleno, o heteroarilo de 5-6 miembros o heteroarilo bicíclico de 9-10 miembros están opcionalmente sustituidos con uno a cuatro grupos Ra; R1 y R1a se seleccionan, de manera independiente, de H, Me, Et, -CH=CH2, -CH2OH, CF3, CHF2 o CH2F; R2 es H, -OH, -OMe o F; R2a es H, Me o F, o R2 y R2a son oxo; R3es H, Me, Et, o CF3; R4 es H, heterociclo de 4-6 miembros, ciclopropilmetilo o alquilo C1-4 opcionalmente sustituido con F, -OH o -Oalquilo C1-3; R5 y R5a se seleccionan, de manera independiente, de H y alquilo C1-4; o R5 y R5a junto con el átomo al cual están unidos forman un grupo carbonilo, un cicloalquilo de 5-6 miembros o un heterociclo de 5-6 miembros, donde el heterociclo tiene un heteroátomo de oxigeno; cada Ra es, de manera independiente, halogeno, alquilo C1-6, cicloalquilo C3-6, -O-alquilo C1-6, CF3, -OCF3, Salquilo C1-6, CN, fenilo, -OCH2-fenilo, NH2, -NO2, -NH-alquilo C1-6, -N-(alquilo C1-6)2, piperidina, pirrolidina, pirazol piridina, 2-aminopiridina, CH2F, CHF2, -OCH2F, -OCHF2, -OH, -SO2alquilo C1-6, C(O)NH2, C(O)NHalquilo C1-6 y C(O)N(alquilo C1-6)2 y j es 1 o 2; y cuando j es 2, el carbono de anillo de j opuesto a NR4 puede ser reemplazado con un heteroátomo O.
ARP080102885A 2007-07-05 2008-07-03 Compuestos heterociclicos que contienen ciclopenta[d]pirimidina inhibidores de proteinquinasas akt, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de las mismas para el tratamiento de enfermedades hiperproliferativas, tales como cancer AR067413A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US94813807P 2007-07-05 2007-07-05
US2008808P 2008-01-09 2008-01-09

Publications (1)

Publication Number Publication Date
AR067413A1 true AR067413A1 (es) 2009-10-07

Family

ID=40076864

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080102885A AR067413A1 (es) 2007-07-05 2008-07-03 Compuestos heterociclicos que contienen ciclopenta[d]pirimidina inhibidores de proteinquinasas akt, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de las mismas para el tratamiento de enfermedades hiperproliferativas, tales como cancer

Country Status (20)

Country Link
US (1) US8618097B2 (es)
EP (1) EP2170863B1 (es)
JP (2) JP5628028B2 (es)
KR (2) KR101650956B1 (es)
CN (2) CN103396409B (es)
AR (1) AR067413A1 (es)
AU (1) AU2008272830B8 (es)
BR (1) BRPI0813999A2 (es)
CA (1) CA2692502C (es)
CO (1) CO6251283A2 (es)
CR (1) CR11229A (es)
EC (1) ECSP109937A (es)
ES (1) ES2551352T3 (es)
HK (1) HK1147255A1 (es)
MA (1) MA31679B1 (es)
NZ (1) NZ582692A (es)
RU (1) RU2486181C2 (es)
SG (1) SG185274A1 (es)
TW (1) TWI450720B (es)
WO (1) WO2009006567A2 (es)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2526948A1 (en) 2006-09-20 2012-11-28 Aerie Pharmaceuticals, Inc. RHO kinase inhibitors
US8455513B2 (en) 2007-01-10 2013-06-04 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
CN101959887B (zh) 2008-01-08 2013-07-31 阵列生物制药公司 作为激酶抑制剂的吡咯并吡啶
EP2240483B8 (en) * 2008-01-09 2013-04-03 Array Biopharma, Inc. Pyrimidyl cyclopentanes as akt protein kinase inhibitors
ES2392014T3 (es) 2008-01-09 2012-12-03 Array Biopharma, Inc. Pirazolopiridinas como inhibidores de la cinasa
ES2401685T3 (es) * 2008-01-09 2013-04-23 Array Biopharma, Inc. Pirimidil ciclopentano hidroxilado como inhibidor de la proteína quinasa AKT
US8329709B2 (en) 2008-01-09 2012-12-11 Genentech, Inc. 5H-cyclopenta[D]pyrimidines as AKT protein kinase inhibitors
KR101624753B1 (ko) 2008-01-09 2016-05-26 어레이 바이오파마 인크. Akt 단백질 키나제 저해물질로서의 수산화된 피리미딜 시클로펜탄
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
EP3053913B1 (en) 2009-05-01 2018-03-07 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
MX2012011887A (es) 2010-04-16 2012-11-30 Genentech Inc Foxo 3a como biomarcador predictivo para la eficacia del inhibidor de la via de quinasa pi3k/akt.
JP6293655B2 (ja) 2011-04-01 2018-03-14 ジェネンテック, インコーポレイテッド 癌治療に対する感受性を予測するためのバイオマーカー
PL2858989T3 (pl) 2012-05-17 2020-11-16 Genentech, Inc. Amorficzna postać inhibującego AKT związku pirymidynylo-cyklopentanu, kompozycje oraz ich sposoby
CN104662015B (zh) 2012-06-20 2017-03-29 诺华股份有限公司 补体途径调节剂及其用途
WO2014130923A2 (en) 2013-02-25 2014-08-28 Genentech, Inc. Methods and compositions for detecting and treating drug resistant akt mutant
US20140275160A1 (en) 2013-03-15 2014-09-18 Aerie Pharmaceuticals, Inc. Combination therapy
AU2015414743B2 (en) * 2015-11-17 2019-07-18 Alcon Inc. Process for the preparation of kinase inhibitors and intermediates thereof
US9643927B1 (en) 2015-11-17 2017-05-09 Aerie Pharmaceuticals, Inc. Process for the preparation of kinase inhibitors and intermediates thereof
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
JP6907319B2 (ja) 2016-08-31 2021-07-21 アエリエ ファーマシューティカルズ インコーポレイテッド 眼科用組成物
EP3609871A4 (en) 2017-03-31 2021-01-06 Aerie Pharmaceuticals, Inc. ARYL CYCLOPROPYL-AMINO-ISOQUINOLINYL AMIDE COMPOUNDS
US11472799B2 (en) * 2018-03-06 2022-10-18 Icahn School Of Medicine At Mount Sinai Serine threonine kinase (AKT) degradation / disruption compounds and methods of use
KR20240095318A (ko) * 2018-04-04 2024-06-25 아비나스 오퍼레이션스, 인코포레이티드 단백질분해 조절제 및 연관된 사용 방법
CA3112391A1 (en) 2018-09-14 2020-03-19 Aerie Pharmaceuticals, Inc. Aryl cyclopropyl-amino-isoquinolinyl amide compounds
CN117677614A (zh) * 2021-12-17 2024-03-08 中国医药研究开发中心有限公司 具有akt激酶抑制活性的杂环化合物及其制备方法和医药用途

Family Cites Families (102)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3885035A (en) 1972-04-05 1975-05-20 Sandoz Ag Method for treating arrhythmia by using 1,4-bis(4 quinazolinyl) piperazines
US3956495A (en) 1973-10-30 1976-05-11 Eli Lilly And Company 2,4-Diaminoquinazolines as antithrombotic agents
US3966936A (en) 1974-02-21 1976-06-29 Pfizer Inc. Piperazino quinazoline bronchodilators
US4060615A (en) 1976-02-18 1977-11-29 Mead Johnson & Company 2-Piperazinyl-6,7-dimethoxyquinazolines
JPS562968A (en) 1979-06-21 1981-01-13 Mitsubishi Yuka Yakuhin Kk Novel pyrimidine derivative
JPS6270A (ja) 1985-03-07 1987-01-06 Sankyo Co Ltd シクロペンタ〔d〕ピリミジン誘導体
MX19185A (es) 1989-01-20 1993-12-01 Pfizer Procedimiento para preparar 3-(1,2,5,6-tretrahidropiridil)-pirrolopiridinas.
WO1994007890A1 (en) 1992-10-05 1994-04-14 Ube Industries, Ltd. Pyrimidine compound
EP0710654A4 (en) 1993-07-23 1996-08-28 Green Cross Corp TRIAZOLE DERIVATIVE AND ITS PHARMACEUTICAL USE
GB9416189D0 (en) 1994-08-10 1994-09-28 Merck Sharp & Dohme Therapeutic agents
EP0775120B1 (en) 1994-08-13 2003-06-04 Yuhan Corporation Novel pyrimidine derivatives and processes for the preparation thereof
US5525625A (en) 1995-01-24 1996-06-11 Warner-Lambert Company 2-(2-Amino-3-methoxyphenyl)-4-oxo-4H-[1]benzopyran for treating proliferative disorders
US7125880B1 (en) 1995-06-06 2006-10-24 Pfizer Inc. Corticotropin releasing factor antagonists
ZA979961B (en) 1996-11-15 1999-05-05 Lilly Co Eli 5-HT1F agonists
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
WO1999001426A1 (en) 1997-07-01 1999-01-14 Warner-Lambert Company 4-bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as mek inhibitors
CA2290509A1 (en) 1997-07-01 1999-01-14 Warner-Lambert Company 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as mek inhibitors
US6310060B1 (en) 1998-06-24 2001-10-30 Warner-Lambert Company 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors
US6506798B1 (en) 1997-07-01 2003-01-14 Warner-Lambert Company 4-Arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective MEK inhibitors
US6821963B2 (en) 1997-07-01 2004-11-23 Warner-Lambert Company 4-Bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors
US6423716B1 (en) 1998-03-31 2002-07-23 Kyowa Hakko Kogyo Co., Ltd. Nitrogenous heterocyclic compounds
DE19853278A1 (de) 1998-11-19 2000-05-25 Aventis Pharma Gmbh Substituierte 4-Amino-2-aryl-cyclopenta[d]pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate
US6696440B1 (en) 1999-01-07 2004-02-24 Warner-Lambert Company Treatment of asthma with MEK inhibitors
WO2000040237A1 (en) 1999-01-07 2000-07-13 Warner-Lambert Company Antiviral method using mek inhibitors
ES2251851T3 (es) 1999-01-13 2006-05-01 Warner-Lambert Company Llc Acidos sulfohidroxamicos y sulfohidroxamatos y su uso com inhibidores mek.
CA2348236A1 (en) 1999-01-13 2000-07-20 Stephen Douglas Barrett 4-arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective mek inhibitors
ATE309205T1 (de) 1999-01-13 2005-11-15 Warner Lambert Co Benzenesulfonamid-derivative und ihre verwendung als mek-inhibitoren
US6545030B1 (en) 1999-01-13 2003-04-08 Warner-Lambert Company 1-heterocycle substituted diarylamines
CA2355470C (en) 1999-01-13 2008-09-30 Warner-Lambert Company Benzoheterocycles and their use as mek inhibitors
EP1150950A2 (en) 1999-01-13 2001-11-07 Warner-Lambert Company Anthranilic acid derivatives
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
TR200200205T2 (tr) 1999-07-16 2002-06-21 Warner-Lambert Company MEK inhibitörleri kullanılarak kronik ağrının tedavi edilmesi
TR200200204T2 (tr) 1999-07-16 2002-11-21 Warner-Lambert Company MEK inhibitörleri kullanılarak kronik ağrının tedavi edilmesi.
AU5786000A (en) 1999-07-16 2001-02-05 Warner-Lambert Company Method for treating chronic pain using mek inhibitors
IL147150A0 (en) 1999-07-16 2002-08-14 Warner Lambert Co Method for treating chronic pain using mek inhibitors
BR0109188A (pt) 2000-03-15 2003-03-18 Warner Lambert Co Diarilaminas 5-amida substituìdas como inibidores de mex
EP1301472B1 (en) 2000-07-19 2014-03-26 Warner-Lambert Company LLC Oxygenated esters of 4-iodo phenylamino benzhydroxamic acids
PL360699A1 (en) 2000-08-25 2004-09-20 Warner-Lambert Company Llc. Process for making n-aryl-anthranilic acids and their derivatives
US6638926B2 (en) 2000-09-15 2003-10-28 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
WO2002044166A1 (en) 2000-11-02 2002-06-06 Astrazeneca Ab Substituted quinolines as antitumor agents
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
EP1383747B1 (en) 2001-04-30 2008-02-20 Glaxo Group Limited Fused pyrimidines as antagonists of the corticotropin releasing factor (crf)
WO2003022214A2 (en) 2001-09-06 2003-03-20 Millennium Pharmaceuticals, Inc. Piperazine and homopiperazine compounds
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
TW200306819A (en) * 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
JP2005526076A (ja) 2002-03-13 2005-09-02 アレイ バイオファーマ、インコーポレイテッド Mek阻害剤としてのn3アルキル化ベンズイミダゾール誘導体
EP3000810B1 (en) 2002-03-13 2017-07-19 Array Biopharma, Inc. N3 alkylated benzimidazole derivative as mek inhibitor
US7235537B2 (en) 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
AU2003230802B2 (en) 2002-04-08 2007-08-09 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
CA2481241C (en) 2002-04-08 2010-07-27 Merck & Co., Inc. Fused quinoxaline derivatives as inhibitors of akt activity
JP4394959B2 (ja) 2002-04-08 2010-01-06 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
AU2003223467B2 (en) 2002-04-08 2007-10-04 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
JP2005534632A (ja) 2002-05-10 2005-11-17 ニューロクライン バイオサイエンセズ, インコーポレイテッド メラノコルチンレセプターリガンドとしての置換ピペラジン
US20040102360A1 (en) 2002-10-30 2004-05-27 Barnett Stanley F. Combination therapy
AU2003284981B2 (en) 2002-10-30 2009-05-28 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
GB0308208D0 (en) 2003-04-09 2003-05-14 Glaxo Group Ltd Chemical compounds
WO2004096130A2 (en) 2003-04-24 2004-11-11 Merck & Co., Inc. Inhibitors of akt activity
EP1646615B1 (en) 2003-06-06 2009-08-26 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as modulators of atp-binding cassette transporters
EP1663994B1 (en) 2003-08-05 2012-03-07 Vertex Pharmaceuticals Incorporated Tetrahydroquinazoline compounds as inhibitors of voltage-gated ion channels
EP1656354B1 (en) 2003-08-12 2007-09-26 F.Hoffmann-La Roche Ag Tetrahydroquinazoline derivatives as cfr antagonists
JPWO2005026126A1 (ja) 2003-09-09 2006-11-16 小野薬品工業株式会社 Crf拮抗剤および二環式複素環化合物
US20050182061A1 (en) 2003-10-02 2005-08-18 Jeremy Green Phthalimide compounds useful as protein kinase inhibitors
KR101223914B1 (ko) * 2003-11-21 2013-01-18 어레이 바이오파마 인크. Akt 단백질 키나제 억제제
CA2563699C (en) 2004-04-23 2014-03-25 Exelixis, Inc. Kinase modulators and method of use
WO2005113762A1 (en) 2004-05-18 2005-12-01 Pfizer Products Inc. CRYSTAL STRUCTURE OF PROTEIN KINASE B-α (AKT-1) AND USES THEREOF
US20060025074A1 (en) 2004-07-30 2006-02-02 Chih-Ming Liang Bluetooth-based headset
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
GB0419161D0 (en) 2004-08-27 2004-09-29 Novartis Ag Organic compounds
TWM266655U (en) 2004-09-23 2005-06-01 Blueexpert Technology Corp Bluetooth earphone device capable of wirelessly receiving and transmitting stereo sound signal and digital information signal
TW200621257A (en) * 2004-10-20 2006-07-01 Astellas Pharma Inc Pyrimidine derivative fused with nonaromatic ring
UY29177A1 (es) 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
JP5274842B2 (ja) * 2004-12-28 2013-08-28 エグゼリクシス, インコーポレイテッド 免疫疾患、炎症疾患および増殖疾患の処置のためのセリン−スレオニンキナーゼモジュレーター(p70S6K、Akt−1およびAkt−2)としての[1H−ピペラゾ[3,4−d]ピリミジン−4−イル]−ピペラジンまたは[1H−ピペラゾ[3,4−d]ピリミジン−4−イル]−ピペラジン化合物
US20090111805A1 (en) 2005-02-24 2009-04-30 Pfizer Inc. Bicyclic heteroaromatic derivatives useful as anticancer agents
CN101189239A (zh) * 2005-04-28 2008-05-28 休普基因公司 蛋白激酶抑制剂
CN101228161B (zh) 2005-05-20 2012-10-10 沃泰克斯药物股份有限公司 适用作蛋白激酶抑制剂的吡咯并吡啶类
CA2610888C (en) 2005-06-10 2011-02-08 Merck & Co., Inc. Inhibitors of akt activity
AR054485A1 (es) 2005-06-21 2007-06-27 Cancer Rec Tech Ltd ARIL-ALQUILAMINAS Y HETEROARIL-ALQUILAMINAS COMO INHIBIDORES DE PROTEINA QUINASA A Y B, UN PROCESO PARA SU PREPARACION, COMPOSICIONES FARMACEUTICAS QUE LAS CONTIENEN Y SU USO EN LA FABRICACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO O PROFILAXIS DE ENFERMEDADES ORIGINADAS EN EL CRECIMIENTO ANORMAL DE LA
JP2009511528A (ja) 2005-10-13 2009-03-19 グラクソ グループ リミテッド Syk阻害物質としてのピロロピリミジン誘導体群
US20090253687A1 (en) 2005-12-28 2009-10-08 Shoji Fukumoto Fused Heterocyclic Compounds and Their Use as Mineralocorticoid Receptor Ligands
JP2009534454A (ja) 2006-04-25 2009-09-24 アステックス、セラピューティックス、リミテッド 医薬化合物
RU2008152171A (ru) 2006-07-05 2010-08-10 Интермьюн, Инк. (Us) Новые ингибиторы вирусной репликации гепатита с
WO2008003697A1 (en) 2006-07-06 2008-01-10 Glaxo Group Limited Substituted n-phenylmethyl -5-oxo-proline-2-amides as p2x7-receptor antagonists and their methods of use
US7910747B2 (en) 2006-07-06 2011-03-22 Bristol-Myers Squibb Company Phosphonate and phosphinate pyrazolylamide glucokinase activators
UA95641C2 (en) 2006-07-06 2011-08-25 Эррей Биофарма Инк. Hydroxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors
GB0613518D0 (en) 2006-07-06 2006-08-16 Phytopharm Plc Chemical compounds
EP2049500B1 (en) * 2006-07-06 2011-09-07 Array Biopharma, Inc. Cyclopenta [d] pyrimidines as akt protein kinase inhibitors
WO2008006025A1 (en) * 2006-07-06 2008-01-10 Array Biopharma Inc. Dihydrofuro pyrimidines as akt protein kinase inhibitors
US8063050B2 (en) * 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
WO2008012635A2 (en) 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents
US8329159B2 (en) * 2006-08-11 2012-12-11 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7659270B2 (en) * 2006-08-11 2010-02-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
JP5228912B2 (ja) * 2006-09-08 2013-07-03 三菱瓦斯化学株式会社 高血圧改善剤
US7741347B2 (en) * 2007-05-17 2010-06-22 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
SI2173723T1 (sl) * 2007-07-05 2011-12-30 Array Biopharma Inc Pirimidil ciklopentani kot inhibitorji AKT-protein-kinaze
US8629171B2 (en) * 2007-08-08 2014-01-14 Bristol-Myers Squibb Company Crystalline form of methyl ((1S)-1-((25)-2-(5-(4'-(2-((25)-1((2S)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)-2-pyrrolidinyl)-1H-imidazol-2-yl)-1-pyrrolidinyl)carbonyl)-2-methylpropyl)carbamate dihydrochloride salt
US8329709B2 (en) * 2008-01-09 2012-12-11 Genentech, Inc. 5H-cyclopenta[D]pyrimidines as AKT protein kinase inhibitors
ES2401685T3 (es) * 2008-01-09 2013-04-23 Array Biopharma, Inc. Pirimidil ciclopentano hidroxilado como inhibidor de la proteína quinasa AKT
KR101624753B1 (ko) * 2008-01-09 2016-05-26 어레이 바이오파마 인크. Akt 단백질 키나제 저해물질로서의 수산화된 피리미딜 시클로펜탄
US7704992B2 (en) * 2008-02-13 2010-04-27 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7906655B2 (en) * 2008-08-07 2011-03-15 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2010096462A1 (en) * 2009-02-17 2010-08-26 Enanta Pharmaceuticals, Inc Linked diimidazole derivatives
DK2430014T3 (en) * 2009-05-13 2015-11-30 Gilead Pharmasset Llc Anti-viral compounds

Also Published As

Publication number Publication date
CN103396409B (zh) 2015-03-11
JP2010532386A (ja) 2010-10-07
KR101650956B1 (ko) 2016-08-24
CN101801955B (zh) 2013-05-08
US20110015204A1 (en) 2011-01-20
CN101801955A (zh) 2010-08-11
ECSP109937A (es) 2010-03-31
RU2486181C2 (ru) 2013-06-27
NZ582692A (en) 2012-05-25
TW200902013A (en) 2009-01-16
JP5628028B2 (ja) 2014-11-19
RU2010103813A (ru) 2011-08-10
AU2008272830A1 (en) 2009-01-08
CO6251283A2 (es) 2011-02-21
JP2014028842A (ja) 2014-02-13
WO2009006567A3 (en) 2009-03-19
MA31679B1 (fr) 2010-09-01
CA2692502C (en) 2016-03-01
BRPI0813999A2 (pt) 2019-10-01
SG185274A1 (en) 2012-11-29
CN103396409A (zh) 2013-11-20
ES2551352T3 (es) 2015-11-18
AU2008272830B8 (en) 2013-12-12
HK1147255A1 (en) 2011-08-05
WO2009006567A2 (en) 2009-01-08
EP2170863A2 (en) 2010-04-07
US8618097B2 (en) 2013-12-31
AU2008272830B2 (en) 2013-12-05
CR11229A (es) 2010-02-09
TWI450720B (zh) 2014-09-01
EP2170863B1 (en) 2015-09-02
CA2692502A1 (en) 2009-01-08
KR20100044819A (ko) 2010-04-30
KR20150089099A (ko) 2015-08-04

Similar Documents

Publication Publication Date Title
AR067413A1 (es) Compuestos heterociclicos que contienen ciclopenta[d]pirimidina inhibidores de proteinquinasas akt, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de las mismas para el tratamiento de enfermedades hiperproliferativas, tales como cancer
AR085960A1 (es) 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2
AR060903A1 (es) Derivados de 1,2,3,4-tetrahidro-quinolina como inhibidores de cetp
PE20130376A1 (es) [1,8]naftiridinas sustituidas por 2,4-diarilo como inhibidores de quinasas para uso contra el cancer
AR060489A1 (es) Derivados del acido benzoazepin - oxi- acetico como agonistas de ppar - delta usados para aumentar hdl- c, reducir ldl-c y reducir colesterol
AR085489A1 (es) Derivados de triazolopiridinas, composiciones farmaceuticas que los contienen, proceso para prepararlos, intermediarios de dicho proceso y uso de los mismos para el tratamiento de enfermedades autoinmunes e inflamatorias
PE20190336A1 (es) Nuevos derivados de amonio, un proceso para su preparacion y composiciones farmaceuticas que los contienen
AR073406A1 (es) Aminodihidrotiazinas fusionadas con tetrahidropiranos,inhibidoras de bace1 y de la produccion de abeta amiloide, composiciones farmaceuticas que las contienen y usos de las mismas para el tratamiento de enfermedades neurodegenerativas,tales como alzheimer.
AR085316A1 (es) Derivados de pirrolo[2,3-b]piridina, utiles para la modulacion de quinasas
AR087760A1 (es) Heterociclilaminas como inhibidores de pi3k
AR078228A1 (es) Inhibidores de cyp17
AR070136A1 (es) Pirimidil ciclopentanos como inhibidores de la akt proteina quinasa
AR088226A1 (es) Derivados piperidinicos heterociclicos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades neurodegenerativas
PE20130188A1 (es) Pirrolidinonas heteroaromaticas fusionadas como inhibidores de syk
AR087591A1 (es) Derivados de ciclohexil azetidina como inhibidores de jak
AR075635A1 (es) N-alcoxiamidas de 6-(fenil sustituido)-4-aminopicolinatos y 2-(fenil sustituido)-6-amino-4-pirimidina carboxilatos, su uso como herbicidas selectivos para las cosechas y proceso de preparacion de dichos compuestos
EA201170099A1 (ru) Замещенные пиримидин-4-оновые производные
AR087288A1 (es) Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a
AR087328A1 (es) Derivados de imidazo[1,2-b]piridazina e imidazo[4,5-b]piridina como inhibidores de jak
AR078786A1 (es) Derivados de la cromenona
AR107042A1 (es) Inhibidores de la tirosina quinasa de bruton y métodos de su uso
AR076008A1 (es) Derivados de hidroximetil-isoxazol moduladores de receptores gaba a, composiciones farmaceuticas que los contienen, metodo para prepararlos y uso de los mismos para el tratamiento del alzheimer y otros trastornos cognitivos.
PE20142081A1 (es) Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodo de uso de los mismos
AR086100A1 (es) Compuestos de cromenona y composiciones farmaceuticas que los contienen
AR100810A1 (es) Inhibidores de fosfatidilinositol 3-quinasa

Legal Events

Date Code Title Description
FB Suspension of granting procedure