BR0104424A - Composições de pirazol úteis como inibidores de erk - Google Patents

Composições de pirazol úteis como inibidores de erk

Info

Publication number
BR0104424A
BR0104424A BR0104424-9A BR0104424A BR0104424A BR 0104424 A BR0104424 A BR 0104424A BR 0104424 A BR0104424 A BR 0104424A BR 0104424 A BR0104424 A BR 0104424A
Authority
BR
Brazil
Prior art keywords
compositions useful
erk inhibitors
useful
compounds
inhibitors
Prior art date
Application number
BR0104424-9A
Other languages
English (en)
Inventor
Jeremy Green
Michael Mullican
Guy Bemis
Xiaoling Xie
Judith Straub
Qing Tang
Robert Mashall
Jingrong Cao
Michael Hale
Christopher Baker
Francois Maltais
James Janetka
Original Assignee
Vertex Pharma
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 Pharma filed Critical Vertex Pharma
Publication of BR0104424A publication Critical patent/BR0104424A/pt

Links

Classifications

    • 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • 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
    • A61P3/08Drugs 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
    • A61P31/12Antivirals
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • 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
    • A61P37/04Immunostimulants
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38Nitrogen atoms
    • 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
    • C07D403/04Heterocyclic 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
    • 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
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (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)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Gastroenterology & Hepatology (AREA)

Abstract

Patente de Invenção: "COMPOSIçõES DE PIRAZOL úTEIS COMO INIBIDORES DE ERK". Descritos aqui são os compostos que são úteis como inibidores de proteína quinase tendo a fórmula: (I) onde R^ 1-4^, Q, e T são descritos no relatório. Os compostos são úteis para o tratamento de estados de doença em mamíferos que são aliviados por um inibidor de proteína quinase, particularmente doenças tais como câncer, disfunções inflamatórias, restenose e doença cardiovascular.
BR0104424-9A 2000-02-05 2001-02-05 Composições de pirazol úteis como inibidores de erk BR0104424A (pt)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US18050600P 2000-02-05 2000-02-05
US19195600P 2000-03-24 2000-03-24
US24293500P 2000-10-24 2000-10-24
PCT/US2001/003911 WO2001057022A2 (en) 2000-02-05 2001-02-05 Pyrazole compositions useful as inhibitors of erk

Publications (1)

Publication Number Publication Date
BR0104424A true BR0104424A (pt) 2002-01-08

Family

ID=27391289

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0104424-9A BR0104424A (pt) 2000-02-05 2001-02-05 Composições de pirazol úteis como inibidores de erk

Country Status (19)

Country Link
US (4) US6528509B1 (pt)
EP (1) EP1200422A2 (pt)
JP (1) JP4783532B2 (pt)
KR (1) KR20010111298A (pt)
CN (1) CN1362953A (pt)
AU (1) AU782775B2 (pt)
BG (1) BG106054A (pt)
BR (1) BR0104424A (pt)
CA (1) CA2369504C (pt)
CZ (1) CZ20013540A3 (pt)
HK (1) HK1046276A1 (pt)
HU (1) HUP0202332A2 (pt)
IL (1) IL145757A (pt)
LT (1) LT4981B (pt)
NO (1) NO322745B1 (pt)
NZ (1) NZ514583A (pt)
SK (1) SK14082001A3 (pt)
TR (1) TR200103787T1 (pt)
WO (1) WO2001057022A2 (pt)

Families Citing this family (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6207665B1 (en) 1997-06-12 2001-03-27 Schering Aktiengesellschaft Piperazine derivatives and their use as anti-inflammatory agents
AU782775B2 (en) * 2000-02-05 2005-08-25 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of ERK
US6436915B1 (en) 2000-04-07 2002-08-20 Kinetek Pharmaceuticals, Inc. Pyrazole compounds
DK1308439T3 (da) * 2000-08-10 2009-01-12 Mitsubishi Tanabe Pharma Corp Prolinderivater og anvendelse af disse som lægemidler
US6660731B2 (en) * 2000-09-15 2003-12-09 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
US6495582B1 (en) * 2000-09-15 2002-12-17 Vertex Pharmaceuticals Incorporated Isoxazole compositions useful as inhibitors of ERK
EP1317448B2 (en) 2000-09-15 2011-05-04 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
JP2004509891A (ja) * 2000-09-22 2004-04-02 スミスクライン ビーチャム パブリック リミテッド カンパニー 抗糖尿病薬としてのピラゾロピリジンおよびピラゾロピリダジン
JP4160395B2 (ja) * 2000-12-21 2008-10-01 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インヒビターとして有用なピラゾール化合物
CA2437248A1 (en) 2001-02-02 2002-08-15 Takeda Chemical Industries, Ltd. Jnk inhibitor
DE60238620D1 (de) 2001-08-03 2011-01-27 Vertex Pharma Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung
DE60226154T2 (de) 2001-08-03 2009-05-20 Vertex Pharmaceuticals Inc., Cambridge Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung
AU2002333114B2 (en) 2001-11-30 2008-09-04 Qlt Inc. Hydrazonopyrazole derivatives and their use as therapeutics
EP1465610B1 (en) * 2002-01-10 2008-12-31 F. Hoffmann-La Roche Ag Use of a gsk-3beta inhibitor in the manufacture of a medicament for increasing bone formation
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
PL372198A1 (en) * 2002-02-06 2005-07-11 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors of gsk-3
DE60332604D1 (de) * 2002-03-15 2010-07-01 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
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
AU2003250701A1 (en) * 2002-07-31 2004-02-16 Wayne R. Danter Protein tyrosine kinase inhibitors
EP1532145B1 (en) * 2002-08-02 2006-09-13 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3
EP1388541A1 (en) * 2002-08-09 2004-02-11 Centre National De La Recherche Scientifique (Cnrs) Pyrrolopyrazines as kinase inhibitors
CA2542007C (en) * 2002-10-09 2010-06-29 Wayne R. Danter Protein tyrosine kinase inhibitors
JP2006516093A (ja) * 2002-10-23 2006-06-22 エクセリクシス, インク. 分枝形態形成のモディファイヤーとしてのcdkl1及び使用方法
KR20050104339A (ko) * 2002-12-20 2005-11-02 파마시아 코포레이션 비환식 피라졸 화합물
US20050019366A1 (en) * 2002-12-31 2005-01-27 Zeldis Jerome B. Drug-coated stents and methods of use therefor
WO2004072029A2 (en) * 2003-02-06 2004-08-26 Vertex Pharmaceuticals Incorporated Pyrazolopyridazines useful as inhibitors of protein kinases
WO2004078261A1 (en) * 2003-03-07 2004-09-16 The University Court Of The University Of Aberdeen Cannabinoid receptor inverse agonists and neutral antagonists as therapeutic agents for the treatment of bone disorders
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
WO2005012256A1 (en) 2003-07-22 2005-02-10 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
EP1656372B1 (en) 2003-07-30 2013-04-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
AU2004264440B2 (en) * 2003-08-15 2008-10-23 Vertex Pharmaceuticals Incorporated Pyrrole compositions useful as inhibitors of c-Met
DE10354060A1 (de) * 2003-11-19 2005-06-02 Merck Patent Gmbh Pyrrolderivate
CA2548172A1 (en) * 2003-12-04 2005-06-23 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
EP1694686A1 (en) 2003-12-19 2006-08-30 Takeda San Diego, Inc. Kinase inhibitors
US7488817B2 (en) * 2004-02-02 2009-02-10 The Trustees Of The University Of Pennsylvania Metal complex protein kinase inhibitors
US7462612B2 (en) 2004-03-26 2008-12-09 Vertex Pharmaceuticals Incorporated Pyridine inhibitors of ERK2 and uses thereof
JP2007533753A (ja) * 2004-04-23 2007-11-22 タケダ サン ディエゴ インコーポレイテッド インドール誘導体及びキナーゼ阻害剤としてのその使用
JP2008510734A (ja) * 2004-08-18 2008-04-10 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
ATE479687T1 (de) 2004-10-15 2010-09-15 Takeda Pharmaceutical Kinaseinhibitoren
FR2876582B1 (fr) * 2004-10-15 2007-01-05 Centre Nat Rech Scient Cnrse Utilisation de derives de pyrrolo-pyrazines pour la fabrication de medicaments pour le traitement de la mucoviscidose et de maladies liees a un defaut d'adressage des proteines dans les cellules
JP2008520745A (ja) * 2004-11-22 2008-06-19 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 Rhoキナーゼの二環式阻害剤
US8110573B2 (en) 2004-12-30 2012-02-07 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of CDK, GSK and aurora kinases
WO2006070202A1 (en) * 2004-12-30 2006-07-06 Astex Therapeutics Limited Pyrazole derivatives having kinase modulating activity
JP2008526723A (ja) * 2004-12-30 2008-07-24 アステックス、セラピューティックス、リミテッド Cdk、gsk及びオーロラキナーゼの活性を調節するピラゾール誘導体
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
TW200639163A (en) * 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
SG137989A1 (en) 2005-06-08 2008-01-28 Rigel Pharmaceuticals Inc Compositions and methods for inhibition of the JAK pathway
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
JP2007000061A (ja) * 2005-06-23 2007-01-11 Sumitomo Chemical Co Ltd 昆虫由来のc−Junアミノ末端リン酸化酵素活性に関わる有害生物の生理状態に変化を与える薬剤
JP2009504771A (ja) * 2005-08-18 2009-02-05 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 ピラジンキナーゼ阻害剤
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
JP5249771B2 (ja) * 2005-11-03 2013-07-31 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 キナーゼインヒビターとして有用なアミノピリミジン
NZ569087A (en) * 2005-12-13 2011-09-30 Schering Corp Polycyclic indazole derivatives that are ERK inhibitors
US8546404B2 (en) 2005-12-13 2013-10-01 Merck Sharp & Dohme Compounds that are ERK inhibitors
US8399442B2 (en) 2005-12-30 2013-03-19 Astex Therapeutics Limited Pharmaceutical compounds
ATE485268T1 (de) 2006-02-16 2010-11-15 Schering Corp Pyrrolidin-derivate als erk-hemmer
CA2642229C (en) 2006-02-24 2015-05-12 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
TW200800203A (en) 2006-03-08 2008-01-01 Astrazeneca Ab New use
JP5523829B2 (ja) 2006-06-29 2014-06-18 アステックス、セラピューティックス、リミテッド 複合薬剤
EA200970361A1 (ru) 2006-10-09 2010-02-26 Такеда Фармасьютикал Компани Лимитед Ингибиторы киназы
JP2010505961A (ja) * 2006-10-09 2010-02-25 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
JP2010509231A (ja) * 2006-11-02 2010-03-25 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阻害剤として有用なアミノピリジンおよびアミノピリミジン
MX2009006690A (es) * 2006-12-19 2009-07-31 Vertex Pharma Aminopirimidinas utiles como inhibidores de proteinas cinasas.
US8278337B2 (en) * 2006-12-20 2012-10-02 Merck Sharp & Dohme Substituted pyridines that are JNK inhibitors
EP2121681B1 (en) 2007-01-11 2015-04-15 Critical Outcome Technologies, Inc. Compounds and method for treatment of cancer
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
GB0702862D0 (en) * 2007-02-14 2007-03-28 Univ Aberdeen Therapeutic compounds
EP2134709A1 (en) 2007-03-09 2009-12-23 Vertex Pharmaceuticals, Inc. Aminopyridines useful as inhibitors of protein kinases
CA2680029A1 (en) * 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
ES2435997T3 (es) * 2007-03-09 2013-12-26 Vertex Pharmaceuticals, Inc. Aminopirimidinas útiles como inhibidores de las proteínas cinasas
WO2008124085A2 (en) * 2007-04-03 2008-10-16 Exelixis, Inc. Methods of using combinations of mek and jak-2 inhibitors
MX2009011059A (es) 2007-04-13 2009-11-26 Vertex Pharma Aminopirimidinas utiles como inhibidores de cinasas.
AU2008247594A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2008247595A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2008247592A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
AU2008257044A1 (en) * 2007-05-24 2008-12-04 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
JP2010530421A (ja) * 2007-06-18 2010-09-09 シェーリング コーポレイション 複素環化合物およびerk阻害剤としてのそれらの使用
CA2694499A1 (en) * 2007-07-31 2009-02-05 Vertex Pharmaceuticals Incorporated Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof
WO2009079797A1 (en) 2007-12-26 2009-07-02 Critical Outcome Technologies, Inc. Compounds and method for treatment of cancer
WO2009103032A1 (en) 2008-02-15 2009-08-20 Rigel Pharmaceuticals, Inc. Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases
MX2010009268A (es) 2008-02-21 2010-09-14 Schering Corp Compuestos que son inhibidores de erk.
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
NZ589315A (en) 2008-04-16 2012-11-30 Portola Pharm Inc 2,6-diamino-pyrimidin-5-yl-carboxamides as Spleen tryosine kinase (syk) or Janus kinase (JAK) inhibitors
JP2011518219A (ja) 2008-04-22 2011-06-23 ポートラ ファーマシューティカルズ, インコーポレイテッド タンパク質キナーゼの阻害剤
US8106039B2 (en) * 2008-04-30 2012-01-31 The Trustees Of The University Of Pennsylvania Metal complex phosphatidyl-inositol-3-kinase inhibitors
JP2011525931A (ja) * 2008-06-26 2011-09-29 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 Akt活性の阻害剤
EP2306825A4 (en) * 2008-06-26 2011-12-28 Glaxosmithkline Llc HAMMER OF ACT ACTIVITY
JP2011525930A (ja) * 2008-06-26 2011-09-29 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 Akt活性の阻害剤
EP2318406B1 (en) 2008-07-17 2016-01-27 Critical Outcome Technologies, Inc. Thiosemicarbazone inhibitor compounds and cancer treatment methods
KR20110050549A (ko) * 2008-09-03 2011-05-13 버텍스 파마슈티칼스 인코포레이티드 공-결정 및 이를 포함하는 제약 제제
BR112012002001A2 (pt) * 2009-07-28 2016-05-10 Rigel Pharmaceuticals Inc método para tratar uma doença e/ou distúrbio do olho, formulação farmacêutica, e, kit
BR112012017884A2 (pt) 2010-01-19 2019-09-24 Astrazeneca Ab composto, composição farmacêutica, uso de um composto, derivado de pirazina, métodos para o tratamento ou prevenção, para promoção óssea, e, para tratar lesões ósseas em cânceres
US8987272B2 (en) 2010-04-01 2015-03-24 Critical Outcome Technologies Inc. Compounds and method for treatment of HIV
US9102625B2 (en) 2010-11-01 2015-08-11 Portola Pharmaceuticals, Inc. Nicotinamides as JAK kinase modulators
US8877760B2 (en) 2011-11-23 2014-11-04 Portola Pharmaceuticals, Inc. Substituted pyrazine-2-carboxamide kinase inhibitors
WO2013109142A1 (en) 2012-01-16 2013-07-25 Stichting Het Nederlands Kanker Instituut Combined pdk and mapk/erk pathway inhibition in neoplasia
WO2013169858A1 (en) 2012-05-08 2013-11-14 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy
US9676756B2 (en) 2012-10-08 2017-06-13 Portola Pharmaceuticals, Inc. Substituted pyrimidinyl kinase inhibitors
WO2015041534A1 (en) 2013-09-20 2015-03-26 Stichting Het Nederlands Kanker Instituut P90rsk in combination with raf/erk/mek
US9629851B2 (en) 2013-09-20 2017-04-25 Stitching Het Nederlands Kanker Institut—Antoni Van Leeuwenhoek Ziekenhuis ROCK in combination with MAPK pathway
US20170027940A1 (en) 2014-04-10 2017-02-02 Stichting Het Nederlands Kanker Instituut Method for treating cancer
WO2015178770A1 (en) 2014-05-19 2015-11-26 Stichting Het Nederlands Kanker Instituut Compositions for cancer treatment
KR101600579B1 (ko) * 2014-06-25 2016-03-07 한국생명공학연구원 피라졸 아마이드 화합물 또는 이의 약학적으로 허용가능한 염을 유효성분으로 포함하는 암 예방 또는 치료용 약학적 조성물
JP7258460B2 (ja) 2015-01-30 2023-04-17 バイオメッド バレー ディスカバリーズ,インコーポレイティド C21H22Cl2N4O2の結晶形態
EP3355923B1 (en) 2015-10-01 2022-02-23 Stichting Het Nederlands Kanker Instituut- Antoni van Leeuwenhoek Ziekenhuis Histone deacetylase inhibitors for use in the treatment of drug resistant melanoma
JP6630844B2 (ja) * 2015-12-07 2020-01-15 蘇州信諾維医薬科技有限公司Suzhou Sinovent Pharmaceuticals Co., Ltd. 5員複素環式アミド系wnt経路阻害剤
WO2017099591A1 (en) 2015-12-07 2017-06-15 Stichting Het Nederlands Kanker Instituut-Antoni van Leeuwenhoek Ziekenhuis Treatment of inhibitor resistant braf-mutant cancers
WO2017204626A1 (en) 2016-05-24 2017-11-30 Stichting Het Nederlands Kanker Instituut-Antoni van Leeuwenhoek Ziekenhuis Combination therapy - combined map2k4/map3k1 and mek/erk inhibition
KR20210018915A (ko) * 2018-06-08 2021-02-18 베타 파머수티컬 컴퍼니 리미티드 Erk 억제제 및 이의 용도
US11795160B2 (en) 2019-02-22 2023-10-24 Insilico Medicine Ip Limited Kinase inhibitors
CN113518779B (zh) 2019-03-28 2024-03-15 江苏恒瑞医药股份有限公司 噻吩并杂环类衍生物、其制备方法及其在医药上的应用
AU2020251621A1 (en) 2019-03-29 2021-11-04 Jiangsu Hengrui Medicine Co., Ltd. Pyrroloheterocyclic derivative, preparation method therefor, and application thereof in medicine
US20220204512A1 (en) 2019-05-24 2022-06-30 Jiangsu Hengrui Medicine Co., Ltd. Substituted fused bicyclic derivative, preparation method therefor, and application thereof in medicines
CN116437915A (zh) 2020-09-29 2023-07-14 江苏恒瑞医药股份有限公司 一种吡咯并杂环类衍生物的晶型及其制备方法
TW202245753A (zh) 2021-02-24 2022-12-01 香港商英科智能有限公司 用於治療疾病之類似物

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2707295A1 (fr) * 1993-06-07 1995-01-13 Rhone Poulenc Agrochimie Fongicides pyrazoles substitués en position 3 par un hétérocycle.
JP3734180B2 (ja) * 1994-12-28 2006-01-11 エーザイ株式会社 新規ピラゾール誘導体
GB9608435D0 (en) * 1996-04-24 1996-06-26 Celltech Therapeutics Ltd Chemical compounds
AU7726898A (en) * 1997-05-22 1998-12-11 G.D. Searle & Co. Pyrazole derivatives as p38 kinase inhibitors
US6514977B1 (en) * 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
BR9809451A (pt) * 1997-05-22 2000-06-20 Searle & Co Pirazóis substituìdos com 3(5)-heteroarila como inibidores de quinase p38.
AU782775B2 (en) * 2000-02-05 2005-08-25 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of ERK

Also Published As

Publication number Publication date
US7056944B2 (en) 2006-06-06
IL145757A0 (en) 2002-07-25
US6593357B1 (en) 2003-07-15
SK14082001A3 (sk) 2002-03-05
NO20014837L (no) 2001-12-04
CA2369504C (en) 2009-01-06
WO2001057022A2 (en) 2001-08-09
JP4783532B2 (ja) 2011-09-28
NO322745B1 (no) 2006-12-04
NZ514583A (en) 2004-05-28
CN1362953A (zh) 2002-08-07
NO20014837D0 (no) 2001-10-04
HK1046276A1 (zh) 2003-01-03
CA2369504A1 (en) 2001-08-09
AU3672301A (en) 2001-08-14
US6699865B2 (en) 2004-03-02
JP2003522163A (ja) 2003-07-22
WO2001057022A3 (en) 2002-03-07
CZ20013540A3 (cs) 2002-03-13
AU782775B2 (en) 2005-08-25
US20040102506A1 (en) 2004-05-27
US20030040536A1 (en) 2003-02-27
HUP0202332A2 (en) 2002-10-28
IL145757A (en) 2007-12-03
LT2001103A (en) 2002-10-25
KR20010111298A (ko) 2001-12-17
US6528509B1 (en) 2003-03-04
BG106054A (en) 2002-06-28
EP1200422A2 (en) 2002-05-02
TR200103787T1 (tr) 2002-10-21
LT4981B (lt) 2003-01-27
US20030225151A1 (en) 2003-12-04

Similar Documents

Publication Publication Date Title
BR0104424A (pt) Composições de pirazol úteis como inibidores de erk
NO20031192D0 (no) Isoksazoler og deres anvendelse som inhibitorer av ERK
WO2001056993A3 (en) Pyrazole compositions useful as inhibitors of erk
DE60226154D1 (de) Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung
DE60238620D1 (de) Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung
MXPA03009846A (es) Derivados de triazol inhibidores de cinasa y usos de los mismos.
WO2002088090A3 (en) Pyrazole derived kinase inhibitors
BR0207114A (pt) Inibidores heterocìclicos de erk2 e seus usos
CY1114554T1 (el) Ινδαζολια, βενζοτριαζολια και ν-αναλογα αυτων ως αναστολεις p38 κινασης
MXPA03010961A (es) Compuestos de tiazol utiles como inhibidores de proteinas cinasas.
CY1109006T1 (el) Παραγωγα πουρινης ως αναστολεις κινασης
DE60214703D1 (de) Thiazolverbindungen, die sich als inhibitoren von proteinkinasen eignen
EA200300248A1 (ru) Бициклопиразолы, активные в качестве ингибиторов киназы, способ их получения и включающие их фармацевтические композиции
SE0101675D0 (sv) Novel composition
EA200300409A1 (ru) Пиримидин-2,4,6-трионовые ингибиторы металлопротеиназы
ATE353320T1 (de) Tricyclische proteinkinasehemmer
WO2003105840A3 (en) SPHINGOSINE KINASE INHIBITORS
WO2004030620A3 (en) Novel tyrosine kinase inhibitors
BRPI0407841A (pt) inibidores heterocìclicos de quinase
DE60329326D1 (de) Tace inhibitoren
BR9808923B1 (pt) processos para fazer compostos inibidores de ciclooxigenase-2, e, compostos intermediÁrios para fazer inibidores de ciclooxigenase-2.
TW200505906A (en) Selective mmp-13 inhibitors
NO20033921L (no) Inhibitor av monoaminopptak
ATE364037T1 (de) Tryptasehemmer
AR026515A1 (es) Compuestos bis-basicos como inhibidores de triptasa, procedimiento para su preparacion y su utilizacion como medicamentos

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 5A, 6A E 7A ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO PUBLICADO NA RPI 1963 DE 19.08.2008.