PL364565A1 - Heterocykliczne inhibitory ERK2 oraz ich zastosowania - Google Patents

Heterocykliczne inhibitory ERK2 oraz ich zastosowania

Info

Publication number
PL364565A1
PL364565A1 PL02364565A PL36456502A PL364565A1 PL 364565 A1 PL364565 A1 PL 364565A1 PL 02364565 A PL02364565 A PL 02364565A PL 36456502 A PL36456502 A PL 36456502A PL 364565 A1 PL364565 A1 PL 364565A1
Authority
PL
Poland
Prior art keywords
erk2
heterocyclic inhibitors
heterocyclic
inhibitors
Prior art date
Application number
PL02364565A
Other languages
English (en)
Inventor
Jingrong Cao
Jeremy Green
Michael Hale
François Maltais
Judy Straub
Qing Tang
Alex Aronov
Original Assignee
Vertex Pharmaceuticals Incorporated
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 Vertex Pharmaceuticals Incorporated filed Critical Vertex Pharmaceuticals Incorporated
Publication of PL364565A1 publication Critical patent/PL364565A1/pl

Links

Classifications

    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
PL02364565A 2001-02-09 2002-02-08 Heterocykliczne inhibitory ERK2 oraz ich zastosowania PL364565A1 (pl)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US26781801P 2001-02-09 2001-02-09
US32876801P 2001-10-12 2001-10-12

Publications (1)

Publication Number Publication Date
PL364565A1 true PL364565A1 (pl) 2004-12-13

Family

ID=26952668

Family Applications (1)

Application Number Title Priority Date Filing Date
PL02364565A PL364565A1 (pl) 2001-02-09 2002-02-08 Heterocykliczne inhibitory ERK2 oraz ich zastosowania

Country Status (21)

Country Link
US (3) US6743791B2 (pl)
EP (1) EP1363906B1 (pl)
JP (2) JP4173738B2 (pl)
KR (1) KR100857732B1 (pl)
CN (1) CN100534991C (pl)
AP (1) AP2003002853A0 (pl)
AR (1) AR049239A1 (pl)
BR (1) BR0207114A (pl)
CA (1) CA2437767C (pl)
ES (1) ES2549677T3 (pl)
HU (1) HUP0304052A3 (pl)
IL (1) IL157131A0 (pl)
MX (1) MXPA03007049A (pl)
MY (1) MY130778A (pl)
NO (1) NO20033491L (pl)
NZ (1) NZ527251A (pl)
PE (1) PE20020971A1 (pl)
PL (1) PL364565A1 (pl)
RU (1) RU2300377C2 (pl)
TW (1) TWI309650B (pl)
WO (1) WO2002064586A2 (pl)

Families Citing this family (101)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6660731B2 (en) * 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
WO2002022605A1 (en) * 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7473691B2 (en) * 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6989385B2 (en) 2000-12-21 2006-01-24 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
GB0107901D0 (en) * 2001-03-29 2001-05-23 Cyclacel Ltd Anti-cancer compounds
ES2274035T3 (es) * 2001-06-01 2007-05-16 Vertex Pharmaceuticals Incorporated Compuestos de tiazol utiles como inhibidores de proteina quinasas.
TWI330183B (pl) * 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
ES2316756T3 (es) * 2002-01-10 2009-04-16 F. Hoffmann-La Roche Ag Uso de un inhibidor de gsk-3beta en la fabricacion de un medicamento para incrementar la formacion osea.
WO2003066629A2 (en) * 2002-02-06 2003-08-14 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors of gsk-3
US20040009981A1 (en) * 2002-03-15 2004-01-15 David Bebbington Compositions useful as inhibitors of protein kinases
US7304061B2 (en) * 2002-04-26 2007-12-04 Vertex Pharmaceuticals Incorporated Heterocyclic inhibitors of ERK2 and uses thereof
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
JP4307022B2 (ja) * 2002-07-05 2009-08-05 富士通マイクロエレクトロニクス株式会社 半導体装置の設計方法、半導体装置の設計プログラム及び半導体装置の設計装置
US7361665B2 (en) 2002-07-09 2008-04-22 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
CN1319968C (zh) 2002-08-02 2007-06-06 沃泰克斯药物股份有限公司 用作gsk－3的抑制剂的吡唑组合物
EP1571146A4 (en) * 2002-12-10 2010-09-01 Ono Pharmaceutical Co NITROGENIC HETEROCYCLIC COMPOUNDS AND THEIR MEDICAL USE
GB0229581D0 (en) * 2002-12-19 2003-01-22 Cyclacel Ltd Use
US7601718B2 (en) * 2003-02-06 2009-10-13 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
JP2006518381A (ja) * 2003-02-07 2006-08-10 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 プロテインキナーゼのインヒビターとして有用なヘテロアリール置換ピロール
US7456190B2 (en) * 2003-03-13 2008-11-25 Vertex Pharmaceuticals Incorporated Compositions useful as protein kinase inhibitors
CA2532965C (en) 2003-07-22 2013-05-14 Astex Therapeutics Limited 3, 4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators
GB0317127D0 (en) * 2003-07-22 2003-08-27 Astex Technology Ltd Pharmaceutical compounds
JP2007500178A (ja) * 2003-07-30 2007-01-11 サイクラセル・リミテッド プロテインキナーゼ阻害剤としてのピリジニルアミノ−ピリミジン誘導体
JP5164380B2 (ja) * 2003-10-21 2013-03-21 サイクラセル リミテッド ピリミジン−４−イル−３，４−チオン化合物及び治療におけるその使用
CA2547080A1 (en) * 2003-12-02 2005-07-28 Vertex Pharmaceuticals, Inc. Heterocyclic protein kinase inhibitors and uses thereof
US7592340B2 (en) * 2003-12-04 2009-09-22 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
EP1694686A1 (en) * 2003-12-19 2006-08-30 Takeda San Diego, Inc. Kinase inhibitors
US20050250829A1 (en) * 2004-04-23 2005-11-10 Takeda San Diego, Inc. Kinase inhibitors
WO2005105780A2 (en) * 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of rock and other protein kinases
AU2005245877B2 (en) * 2004-05-14 2010-06-03 Vertex Pharmaceuticals, Incorporated Prodrugs of pyrrolylpyrimidine ERK protein kinase inhibitors
UA84930C2 (ru) * 2004-05-14 2008-12-10 Вертекс Фармасьютикалс Инкорпорейтед Пиррольные соединения как ингибиторы протеинкиназ erk, их синтез и соответствующие промежуточные соединения
WO2006023931A2 (en) * 2004-08-18 2006-03-02 Takeda San Diego, Inc. Kinase inhibitors
EP1812439B2 (en) 2004-10-15 2017-12-06 Takeda Pharmaceutical Company Limited Kinase inhibitors
WO2006058120A1 (en) * 2004-11-22 2006-06-01 Vertex Pharmaceuticals Incorporated Bicyclic inhibitors or rho kinase
JP2008523103A (ja) * 2004-12-14 2008-07-03 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 Ｅｒｋプロテインキナーゼのピリミジンインヒビターおよびその使用
WO2006071644A1 (en) * 2004-12-23 2006-07-06 Vertex Pharmaceuticals Incorporated Selective inhibitors of erk protein kinases and uses therof
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
JP2008530193A (ja) * 2005-02-18 2008-08-07 アストラゼネカ アクチボラグ 化合物
ATE542814T1 (de) * 2005-08-18 2012-02-15 Vertex Pharma Pyrazinkinaseinhibitoren
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
US8080534B2 (en) * 2005-10-14 2011-12-20 Phigenix, Inc Targeting PAX2 for the treatment of breast cancer
GB0520955D0 (en) * 2005-10-14 2005-11-23 Cyclacel Ltd Compound
MX2008005814A (es) * 2005-11-03 2008-10-15 Vertex Pharma Aminopirimidinas utiles como inhibidores de cinasa.
US8546404B2 (en) 2005-12-13 2013-10-01 Merck Sharp & Dohme Compounds that are ERK inhibitors
KR101417136B1 (ko) * 2005-12-13 2014-08-07 머크 샤프 앤드 돔 코포레이션 Ｅｒｋ 억제제인 폴리사이클릭 인다졸 유도체 및 이를 포함하는 약제학적 조성물
JP2009528280A (ja) * 2006-02-16 2009-08-06 シェーリング コーポレイション Ｅｒｋインヒビターとしてのピロリジン誘導体
EP2223925A1 (en) * 2006-10-09 2010-09-01 Takeda Pharmaceutical Company Limited Kinase inhibitors
SG158147A1 (en) 2006-10-09 2010-01-29 Takeda Pharmaceutical Kinase inhibitors
CA2668429A1 (en) * 2006-11-02 2008-05-15 Vertex Pharmaceuticals Incorporated Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
RU2469034C2 (ru) * 2006-12-04 2012-12-10 Астразенека Аб Химические соединения
ES2347721T3 (es) * 2006-12-19 2010-11-03 Vertex Pharmaceuticals, Inc. Aminopirimidinas utiles como inhibidores de proteina quinasas.
EP2134709A1 (en) 2007-03-09 2009-12-23 Vertex Pharmaceuticals, Inc. Aminopyridines useful as inhibitors of protein kinases
EP2137183B1 (en) * 2007-03-09 2011-09-28 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
AU2008226457B2 (en) * 2007-03-09 2014-03-20 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
NZ580343A (en) 2007-04-13 2012-03-30 Vertex Pharma Aminopyrimidines useful as kinase inhibitors
JP5389785B2 (ja) 2007-05-02 2014-01-15 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 キナーゼ阻害剤として有用なチアゾールおよびピラゾール
CA2694381A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
MX2009011811A (es) * 2007-05-02 2010-01-14 Vertex Pharma Aminopirimidinas utiles como inhibidores de cinasa.
EP2164842A2 (en) * 2007-05-24 2010-03-24 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
MY148609A (en) * 2007-06-05 2013-05-15 Merck Sharp & Dohme Polycyclic indazole derivatives and their use as erk inhibitors for the treatment of cancer
CA2691417A1 (en) * 2007-06-18 2008-12-24 Schering Corporation Heterocyclic compounds and use thereof as erk inhibitors
BRPI0813629A2 (pt) * 2007-07-26 2018-07-10 Novartis Ag derivados de pirimidina úteis no tratamento de condições inflamatórias ou alérgicas
NZ582879A (en) * 2007-07-31 2012-03-30 Vertex Pharma Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof
HUE030912T2 (en) 2008-02-15 2017-06-28 Rigel Pharmaceuticals Inc Pyrimidine-2-amine compounds and their use as inhibitors of yak kinases
US8716483B2 (en) 2008-02-21 2014-05-06 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
KR101014351B1 (ko) 2008-08-04 2011-02-15 한국생명공학연구원 세포외 신호조절 키나제의 활성을 저해하는트리아졸릴-벤즈아미드 유도체 또는 이의 약학적으로허용가능한 염을 유효성분으로 함유하는 암 또는 심혈관계질환의 예방 또는 치료용 조성물
MX2011002312A (es) * 2008-09-03 2011-04-26 Vertex Pharma Co-cristales y formulaciones farmaceuticas que comprenden los mismos.
US20120077813A1 (en) 2009-04-15 2012-03-29 Astrazeneca Ab Imidazole Substituted Pyrimidines Useful in the Treatment of Glycogen Synthase Kinase-3 Related Disorders such as Alzheimer's Disease
JP2013147428A (ja) * 2010-04-27 2013-08-01 Dainippon Sumitomo Pharma Co Ltd 新規２−ヘテロアリール単環ピリミジン誘導体
MX360157B (es) * 2010-11-08 2018-10-24 Novartis Ag Uso de derivados de 2-carboxamida-cicloamino-urea en el tratamiento de enfermedades dependientes de egfr o de enfermedades que han adquirido resistencia a los agentes que tienen como objetivo los miembros de la familia egfr.
JP2014500254A (ja) * 2010-11-09 2014-01-09 セルゾーム リミティッド Ｔｙｋ２阻害剤としてのピリジン化合物およびそのアザ類似体
MX371331B (es) 2012-04-24 2020-01-27 Vertex Pharma Inhibidores de la proteina cinasa dependiente de acido desoxirribonucleico(adn-pk).
EP2890370B1 (en) * 2012-08-31 2019-10-09 The Regents of the University of California Agents useful for treating obesity, diabetes and related disorders
MX2015009952A (es) 2013-02-08 2015-10-05 Celgene Avilomics Res Inc Inhibidores de cinasas reguladas por señales extracelulares (erk) y sus usos.
ME03336B (me) 2013-03-12 2019-10-20 Vertex Pharma Inhibitori dnk-pk
WO2015002926A1 (en) 2013-07-02 2015-01-08 Bristol-Myers Squibb Company Tricyclic pyrido-carboxamide derivatives as rock inhibitors
AR096788A1 (es) 2013-07-02 2016-02-03 Bristol Myers Squibb Co Compuestos tricíclicos de carboxamida como inhibidores potentes de rock
CN112472699A (zh) 2013-07-26 2021-03-12 种族肿瘤学公司 改善比生群及衍生物的治疗益处的组合方法
KR102300576B1 (ko) 2013-09-10 2021-09-08 보드 오브 리전츠 더 유니버시티 오브 텍사스 시스템 절단된 선종성 결장 폴립증 (ａｐｃ) 단백질을 타겟화하는 치료제
JP6408569B2 (ja) 2013-10-17 2018-10-17 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ｄｎａ−ｐｋ阻害剤としての（ｓ）−ｎ−メチル−８−（１−（（２’−メチル−［４，５’−ビピリミジン］−６−イル）アミノ）プロパン−２−イル）キノリン−４−カルボキサミドおよびその重水素化誘導体の共結晶
CA2945263A1 (en) 2014-04-09 2015-10-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
EP3129025B1 (en) * 2014-04-09 2019-05-15 Genentech, Inc. Process for the manufacturing of medicaments
EP3179858B1 (en) 2014-08-13 2019-05-15 Celgene Car Llc Forms and compositions of an erk inhibitor
CN107849046B (zh) * 2015-06-03 2020-06-12 常州捷凯医药科技有限公司 作为erk抑制剂的杂环化合物
BR112017026159A2 (pt) * 2015-06-15 2018-08-14 Asana Biosciences, Llc inibidores heterocíclicos de erk1 e erk2 e seu uso no tratamento de câncer
EP3518931A4 (en) 2016-09-27 2020-05-13 Vertex Pharmaceuticals Incorporated METHOD FOR TREATING CANCER WITH A COMBINATION OF DNA-DAMAGING SUBSTANCES AND DNA-PK INHIBITORS
WO2019246121A1 (en) * 2018-06-18 2019-12-26 Duke University Compositions and methods for treating disorders characterized with aberrant ras/mapk signaling
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
CN109608444B (zh) * 2018-11-27 2022-02-11 中国药科大学 含异吲哚啉酮的erk抑制剂及其制备方法与用途
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
CA3150681A1 (en) 2019-08-14 2021-02-18 Incyte Corporation Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
US11851426B2 (en) 2019-10-11 2023-12-26 Incyte Corporation Bicyclic amines as CDK2 inhibitors
US20240285621A1 (en) * 2020-09-23 2024-08-29 Nerviano Medical Sciences S.R.L. Pyrazolyl-pyrimidine derivatives as kinase inhibitors
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
CN117209485A (zh) * 2023-08-31 2023-12-12 四川大学华西医院 一种具有抗肿瘤活性的嘧啶骨架类化合物及其制备方法和应用

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0727998B1 (en) * 1993-11-08 2004-01-21 Smithkline Beecham Corporation Oxazoles for treating cytokine mediated diseases
WO1997005878A1 (en) 1995-08-10 1997-02-20 Merck & Co., Inc. 2,5-substituted aryl pyrroles, compositions containing such compounds and methods of use
US5792778A (en) 1995-08-10 1998-08-11 Merck & Co., Inc. 2-substituted aryl pyrroles, compositions containing such compounds and methods of use
AU702887B2 (en) 1995-10-31 1999-03-11 Merck & Co., Inc. Substituted pyridyl pyrroles, compositions containing such compounds and methods of use
EP0946523A1 (en) * 1996-12-23 1999-10-06 Celltech Therapeutics Limited Fused polycyclic 2-aminopyrimidine derivatives, their preparation and their use as protein tyrosine kinase inhibitors
US6169086B1 (en) * 1997-01-27 2001-01-02 Daiichi Pharmaceutical Co., Ltd. Pyrazole derivatives
EP1017394B1 (en) * 1997-07-12 2005-12-07 Cancer Research Technology Limited Cyclin dependent kinase inhibiting purine derivatives
AU1924699A (en) 1997-12-19 1999-07-12 Smithkline Beecham Corporation Compounds of heteroaryl substituted imidazole, their pharmaceutical compositionsand uses
EP1077971A1 (en) 1998-05-14 2001-02-28 G.D. SEARLE & CO. 1,5-DIARYL SUBSTITUTED PYRAZOLES AS p38 KINASE INHIBITORS
WO1999065897A1 (en) * 1998-06-19 1999-12-23 Chiron Corporation Inhibitors of glycogen synthase kinase 3
AU6476599A (en) * 1998-11-03 2000-05-22 Novartis Ag Anti-inflammatory 4-phenyl-5-pyrimidinyl-imidazoles
WO2001074811A2 (en) * 2000-03-30 2001-10-11 Takeda Chemical Industries, Ltd. Substituted 1,3-thiazole compounds, their production and use
AU2002338642A1 (en) * 2001-04-13 2002-10-28 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases

Also Published As

Publication number Publication date
US7253187B2 (en) 2007-08-07
WO2002064586A3 (en) 2003-02-06
HU0304052D0 (en) 2004-01-28
RU2300377C2 (ru) 2007-06-10
ES2549677T3 (es) 2015-10-30
US6743791B2 (en) 2004-06-01
IL157131A0 (en) 2004-02-08
MXPA03007049A (es) 2003-11-18
JP2008163045A (ja) 2008-07-17
HUP0304052A3 (en) 2010-06-28
EP1363906B1 (en) 2015-07-15
WO2002064586A2 (en) 2002-08-22
CN100534991C (zh) 2009-09-02
KR100857732B1 (ko) 2008-09-10
NZ527251A (en) 2006-09-29
HUP0304052A2 (hu) 2004-04-28
AR049239A1 (es) 2006-07-12
AP2003002853A0 (en) 2003-09-30
BR0207114A (pt) 2004-02-25
PE20020971A1 (es) 2002-10-29
JP2004520402A (ja) 2004-07-08
NO20033491D0 (no) 2003-08-06
HK1062298A1 (en) 2004-10-29
RU2003127116A (ru) 2005-03-27
US20040229875A1 (en) 2004-11-18
CN1494541A (zh) 2004-05-05
MY130778A (en) 2007-07-31
CA2437767C (en) 2010-05-04
CA2437767A1 (en) 2002-08-22
US20030092714A1 (en) 2003-05-15
US20070265263A1 (en) 2007-11-15
JP4173738B2 (ja) 2008-10-29
NO20033491L (no) 2003-10-08
TWI309650B (en) 2009-05-11
KR20030074814A (ko) 2003-09-19
EP1363906A2 (en) 2003-11-26

Similar Documents

Publication Publication Date Title
HU0304052D0 (en) Heterocyclic inhibitors of erk2 and uses thereof
IL161258A0 (en) Heterocyclic compounds and methods of use
HUP0302650A3 (en) Fumaric and derivatives as nf-kappab inhibitors
AU2003237121A1 (en) Pyrrole derivatives as inhibitors of erk2 and uses thereof
AU2003251559A8 (en) Heterocyclic inhibitors of kinases
EP1383743A4 (en) DOUBLE INHIBITORS OF PDE 7 AND PDE 4
AU2003303128A8 (en) Inhibitors and methods of use thereof
PL353535A1 (en) Application of selective pde 10 inhibitor and application of papaverine
EP1549316A4 (en) HAMMER OF TFGbeta
IL157659A0 (en) New spirotricyclic derivatives and their use as phosphodiesterase-7 inhibitors
SI1534290T1 (sl) Novi inhibitorji kinaz
EP1474445A4 (en) ADIPONECTIN GLYCO-ISOFORMS, AND USES THEREOF
PL376575A1 (pl) Podstawione związki heterocykliczne oraz sposoby wykorzystania
PL373156A1 (pl) Związki i ich zastosowania do zmniejszania działania lipazy wrażliwej na hormony
EP1372654A4 (en) QUINOLINE INHIBITORS OF HYAK1 AND HYAK3 KINASES
IL159538A0 (en) 8/17 heterocyclic compounds and uses thereof as d-alanyl-d-alanine ligase inhibitors
AU8323701A (en) Inhibitors of p38
EP1613628A4 (en) REVERSIBLE INHIBITORS OF S-ADENOSYL-L-HOMOCYSTEIN HYDROLASE AND ITS USES
PL371217A1 (pl) Inhibitory integryny alfaVbeta6
AU2002337913A1 (en) Glycosulfopeptide inhibitors and methods of use thereof
AU2003210983A8 (en) Kinase inhibitors and methods of use thereof
PL369742A1 (pl) Inhibitory kinaz cyklinozależnych oraz związane znimi kompozycje i zastosowania
IL156776A0 (en) Inhibitors of cruzipain and other cysteine proteases
IL156775A0 (en) Cyclic 2-carbonylaminoketones as inhibitors of cruzipain and other cysteine proteases
AU2002306845A1 (en) Telomerase inhibitors and methods of their use

Legal Events

Date Code Title Description
REFS Decisions on refusal to grant patents (taken after the publication of the particulars of the applications)