MA29796B1 - Inhibiteurs de kinase - Google Patents

Inhibiteurs de kinase

Info

Publication number
MA29796B1
MA29796B1 MA30770A MA30770A MA29796B1 MA 29796 B1 MA29796 B1 MA 29796B1 MA 30770 A MA30770 A MA 30770A MA 30770 A MA30770 A MA 30770A MA 29796 B1 MA29796 B1 MA 29796B1
Authority
MA
Morocco
Prior art keywords
biohydrolysable
kinase inhibitors
solvate
arthritis
hydrate
Prior art date
Application number
MA30770A
Other languages
English (en)
Inventor
Jason W Brown
Sanjib Das
Qing Dong
Xianchang Gong
Stephen W Kaldor
Yan Liu
Bheema R Paraselli
Nicholas Scorah
Jeffrey A Stafford
Michael B Wallace
Original Assignee
Takeda San Diego 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 Takeda San Diego Inc filed Critical Takeda San Diego Inc
Publication of MA29796B1 publication Critical patent/MA29796B1/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/24—Antidepressants
    • 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
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems

Abstract

[0592] Composés, compositions pharmaceutiques, trousses et méthodes destinés à être utilisés avec des kinases, comprenant un composé choisi dans le groupe consistant en : dans laquelle les variables sont telles que définies ici.
MA30770A 2005-10-07 2008-03-19 Inhibiteurs de kinase MA29796B1 (fr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US72461905P 2005-10-07 2005-10-07

Publications (1)

Publication Number Publication Date
MA29796B1 true MA29796B1 (fr) 2008-09-01

Family

ID=37622078

Family Applications (1)

Application Number Title Priority Date Filing Date
MA30770A MA29796B1 (fr) 2005-10-07 2008-03-19 Inhibiteurs de kinase

Country Status (29)

Country Link
US (2) US8119655B2 (fr)
EP (2) EP1931669A1 (fr)
JP (1) JP5150878B2 (fr)
KR (1) KR20080051153A (fr)
CN (1) CN101356172B (fr)
AT (1) ATE495173T1 (fr)
AU (1) AU2006302135B2 (fr)
BR (1) BRPI0616950A2 (fr)
CA (1) CA2624610A1 (fr)
CR (1) CR9886A (fr)
CY (1) CY1111346T1 (fr)
DE (1) DE602006019651D1 (fr)
DK (1) DK2133349T3 (fr)
EA (1) EA015902B1 (fr)
ES (1) ES2358006T3 (fr)
GE (1) GEP20125368B (fr)
HK (1) HK1138842A1 (fr)
HR (1) HRP20110220T1 (fr)
IL (1) IL190306A0 (fr)
MA (1) MA29796B1 (fr)
MY (1) MY146989A (fr)
NO (1) NO20081564L (fr)
NZ (1) NZ566866A (fr)
PL (1) PL2133349T3 (fr)
PT (1) PT2133349E (fr)
RS (1) RS51897B (fr)
SI (1) SI2133349T1 (fr)
WO (1) WO2007044779A1 (fr)
ZA (1) ZA200802820B (fr)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE602005023333D1 (de) 2004-10-15 2010-10-14 Takeda Pharmaceutical Kinaseinhibitoren
WO2007038215A1 (fr) 2005-09-22 2007-04-05 Incyte Corporation Inhibiteurs tetracycliques de janus kinases
US8119655B2 (en) * 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
US20090326229A1 (en) * 2006-08-02 2009-12-31 Takeda Phamaceutical Company Limited Alpha-carboline derivatives and methods for preparation thereof
AU2007313961A1 (en) * 2006-10-09 2008-05-08 Takeda Pharmaceutical Company Limited Kinase inhibitors
US20100120717A1 (en) * 2006-10-09 2010-05-13 Brown Jason W Kinase inhibitors
EP2223925A1 (fr) * 2006-10-09 2010-09-01 Takeda Pharmaceutical Company Limited Inhibiteurs de kinase
JP5492565B2 (ja) * 2006-12-22 2014-05-14 インサイト・コーポレイション Ｊａｎｕｓキナーゼ阻害剤としての置換複素環
US8618121B2 (en) 2007-07-02 2013-12-31 Cancer Research Technology Limited 9H-pyrimido[4,5-B]indoles, 9H-pyrido[4',3':4,5]pyrrolo[2,3-D]pyridines, and 9H 1,3,6,9 tetraaza-fluorenes as CHK1 kinase function inhibitors
MX2010009513A (es) * 2008-02-28 2010-09-22 Takeda Pharmaceutical Composicion farmaceutica.
US20090312288A1 (en) * 2008-04-16 2009-12-17 Takeda Pharmaceutical Company Limited Kinase inhibitors
EP2283014A1 (fr) * 2008-04-16 2011-02-16 Takeda Pharmaceutical Company Limited Polymorphes de sel chlorhydrate de 5-(3-(éthylsulfonyl)phényl)-3,8-diméthyl-n-(1-méthylpipéridin-4-yl)-9h-pyridoý2,3-b¨indole-7-carboxamide et leurs procédés d'utilisation
EP2297145A2 (fr) * 2008-04-16 2011-03-23 Takeda Pharmaceutical Company Limited Polymorphes de 5-(3-(éthylsulfonyl)phényl)-3,8-diméthyl-n-(1-méthylpipéridin-4-yl)-9h-pyrido[2,3-b]indole-7-carboxamide et procédés d'utilisation associés
US8501765B2 (en) 2008-06-11 2013-08-06 Genentech, Inc. Diazacarbazoles and methods of use
AU2009258115B2 (en) * 2008-06-11 2015-01-29 Genentech, Inc. Diazacarbazoles and methods of use
AR072084A1 (es) * 2008-06-12 2010-08-04 Sanofi Aventis Derivados de azacarbolinas, su preparacion y su utilizacion terapeutica como inhibidores de las quinasas pim
DE102008052943A1 (de) 2008-10-23 2010-04-29 Merck Patent Gmbh Azaindolderivate
US8853391B2 (en) * 2008-12-18 2014-10-07 Merck Patent Gmbh Tricyclic azaindoles
FR2943674B1 (fr) * 2009-03-24 2013-02-22 Sanofi Aventis Derives d'azacarbolines,leur preparation et leur utilisation therapeutique
FR2950891B1 (fr) * 2009-10-06 2012-11-09 Sanofi Aventis Derives d'azacarbolines 9h-pyrrolo[2,3-b:5,4-c']dipyridine, leur preparation et leur utilisation therapeutique
SG174903A1 (en) * 2009-03-24 2011-11-28 Sanofi Sa 9h-pyrrolo[2,3-b: 5,4-c'] dipyridine azacarboline derivatives, preparation thereof, and therapeutic use thereof
FR2953838B1 (fr) * 2009-12-10 2012-02-24 Sanofi Aventis Derives de 9h-beta-carboline (ou 9h-pyridino[3,4-b]indole) trisubstitues, leur preparation et leur utilisation therapeutique
FR2953837B1 (fr) * 2009-12-10 2012-03-09 Sanofi Aventis Derives 9h-pyridino[3,4-b]indole disubstitues, leur preparation et leur utilisation therapeutique
US20110183938A1 (en) * 2009-12-16 2011-07-28 Genentech, Inc. 1,7-diazacarbazoles and methods of use
CN102372707B (zh) * 2010-08-16 2015-08-19 上海药明康德新药开发有限公司 6-甲基-4-溴-1,6-二氢吡咯[2,3-c]吡啶-7-酮的合成方法
CN104105696B (zh) 2011-11-09 2017-11-14 癌症研究技术有限公司 5‑(吡啶‑2‑基‑氨基)‑吡嗪‑2‑腈化合物及其治疗用途
DK2855448T3 (en) 2012-05-15 2017-05-01 Cancer Res Tech Ltd 5 - [[4 - [[MORPHOLIN-2-YL] METHYLAMINO] -5- (TRIFLUORMETHYL) -2-PYRIDYL] AMINO] PYRAZINE-2-CARBONITRIL AND THERAPEUTIC APPLICATIONS THEREOF
EP2810931B1 (fr) 2013-06-06 2018-04-25 Solvay SA Procédé de préparation d'anhydrides carboxyliques halogénés
WO2016126726A1 (fr) 2015-02-02 2016-08-11 Forma Therapeutics, Inc. Acides hydroxamiques bicycliques [4,6,0] en tant qu'inhibiteurs hdac6
US10239845B2 (en) 2015-02-02 2019-03-26 Forma Therapeutics, Inc. 3-aryl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors
WO2016187767A1 (fr) * 2015-05-25 2016-12-01 Hutchison Medipharma Limited Compositions pharmaceutiques et utilisation de celles-ci
US10555935B2 (en) 2016-06-17 2020-02-11 Forma Therapeutics, Inc. 2-spiro-5- and 6-hydroxamic acid indanes as HDAC inhibitors
PT3762368T (pt) 2018-03-08 2022-05-06 Incyte Corp Compostos de aminopirazina diol como inibidores de pi3k-y
WO2020010003A1 (fr) 2018-07-02 2020-01-09 Incyte Corporation DÉRIVÉS D'AMINOPYRAZINE UTILISÉS EN TANT QU'INHIBITEURS DE PI3K-γ
EP3837241A4 (fr) 2018-08-14 2022-05-18 Osteoqc Inc. COMPOSÉS ß-CARBOLINE FLUORÉS
EP3836923A4 (fr) * 2018-08-14 2022-05-18 Osteoqc Inc. Composés pyrrolo-dipyridine
US11773093B1 (en) 2023-01-19 2023-10-03 King Faisal University N-(pyrimido[2,3-b]indol-7-yl)acetamide compounds as antibacterial agents

Family Cites Families (302)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB828847A (en) 1956-12-14 1960-02-24 Ilford Ltd Improvements in or relating to cyanine dyes
FR1242962A (fr) 1959-08-25 1960-10-07 Kodak Pathe Nouveau procédé pour la préparation de colorants sensibilisateurs de la série des cyanines et des mérocyanines et produits obtenus
GB1268773A (en) 1968-03-15 1972-03-29 Glaxo Lab Ltd NOVEL alpha-CARBOLINE DERIVATIVES, THE PREPARATION THEREOF AND COMPOSITIONS CONTAINING THE SAME
US3710795A (en) 1970-09-29 1973-01-16 Alza Corp Drug-delivery device with stretched, rate-controlling membrane
GB1429184A (en) 1972-04-20 1976-03-24 Allen & Hanburys Ltd Physically anti-inflammatory steroids for use in aerosols
US4044126A (en) 1972-04-20 1977-08-23 Allen & Hanburys Limited Steroidal aerosol compositions and process for the preparation thereof
USRE28819E (en) 1972-12-08 1976-05-18 Syntex (U.S.A.) Inc. Dialkylated glycol compositions and medicament preparations containing same
JPS54110226A (en) * 1978-01-25 1979-08-29 Bayer Ag Dye
DE2844606A1 (de) 1978-10-13 1980-04-24 Bayer Ag Heterocyclische farbstoffe
US4328245A (en) 1981-02-13 1982-05-04 Syntex (U.S.A.) Inc. Carbonate diester solutions of PGE-type compounds
US4410545A (en) 1981-02-13 1983-10-18 Syntex (U.S.A.) Inc. Carbonate diester solutions of PGE-type compounds
US4358603A (en) 1981-04-16 1982-11-09 Syntex (U.S.A.) Inc. Acetal stabilized prostaglandin compositions
US4409239A (en) 1982-01-21 1983-10-11 Syntex (U.S.A.) Inc. Propylene glycol diester solutions of PGE-type compounds
GB9222253D0 (en) * 1992-10-23 1992-12-09 Celltech Ltd Chemical compounds
GB9304920D0 (en) * 1993-03-10 1993-04-28 Celltech Ltd Chemical compounds
CZ1598A3 (cs) * 1995-07-06 1998-04-15 Novartis Ag Pyrrolopyrimidiny a způsoby jejich přípravy
US7119174B2 (en) 1995-12-18 2006-10-10 Sugen, Inc. Diagnosis and treatment of AUR1 and/or AUR2 related disorders
US6716575B2 (en) * 1995-12-18 2004-04-06 Sugen, Inc. Diagnosis and treatment of AUR1 and/or AUR2 related disorders
IL124728A (en) 1995-12-18 2007-06-03 Sugen Inc AURORA – 1 and AURORA – 2 proteins
GB9707800D0 (en) 1996-05-06 1997-06-04 Zeneca Ltd Chemical compounds
ES2194213T3 (es) * 1996-08-09 2003-11-16 Boehringer Ingelheim Pharma Beta-carbolinas-4- sustituidas en calidad de inmunomoduladores.
GB9622363D0 (en) 1996-10-28 1997-01-08 Celltech Therapeutics Ltd Chemical compounds
GB9625184D0 (en) * 1996-12-04 1997-01-22 Celltech Therapeutics Ltd Chemical compounds
EP0946523A1 (fr) 1996-12-23 1999-10-06 Celltech Therapeutics Limited Derives polycyclique fondus de 2-aminopyrimidine, leur preparation et leur utilisation comme inhibiteurs de proteine tyrosine-kinase
GB9705361D0 (en) 1997-03-14 1997-04-30 Celltech Therapeutics Ltd Chemical compounds
DE69836220T2 (de) * 1997-08-15 2007-08-30 Hiroshima University Den zellzyklus regulierende proteine
DE69838172T2 (de) 1997-08-22 2008-04-10 Astrazeneca Ab Oxindolylchinazolinderivate als angiogenesehemmer
US7462605B2 (en) * 1998-01-23 2008-12-09 Celmed Oncology (Usa), Inc. Phosphoramidate compounds and methods of use
US6143480A (en) 1998-09-03 2000-11-07 Fuji Photo Film Co., Ltd. Leuco dye and image recording medium containing the same
US6706491B1 (en) * 1999-04-09 2004-03-16 The Board Of Trustees Of The University Of Illinois Reagents and methods for identifying and modulating expression of genes regulated by p21
US20050113460A1 (en) * 1999-04-30 2005-05-26 The Regents Of The University Of Michigan Compositions and methods relating to novel compounds and targets thereof
US6982265B1 (en) 1999-05-21 2006-01-03 Bristol Myers Squibb Company Pyrrolotriazine inhibitors of kinases
JP2003505064A (ja) 1999-07-21 2003-02-12 ユニバーシティー オブ マサチューセッツ キナーゼ遮断ポリペプチド及びその使用
JP4623483B2 (ja) 1999-08-23 2011-02-02 塩野義製薬株式会社 ｓＰＬＡ２阻害作用を有するピロロトリアジン誘導体
GB9922171D0 (en) 1999-09-21 1999-11-17 Zeneca Ltd Chemical compounds
KR20020032608A (ko) 1999-09-21 2002-05-03 다비드 에 질레스 퀴나졸린 화합물 및 이를 함유하는 제약 조성물
GB9922173D0 (en) 1999-09-21 1999-11-17 Zeneca Ltd Chemical compounds
DE60043349D1 (de) 1999-09-21 2009-12-31 Astrazeneca Ab Chinazolin-derivate und ihre verwendung als arzneimittel
JP2003511378A (ja) 1999-10-07 2003-03-25 アムジエン・インコーポレーテツド トリアジン系キナーゼ阻害薬
US6455525B1 (en) 1999-11-04 2002-09-24 Cephalon, Inc. Heterocyclic substituted pyrazolones
IL150388A0 (en) 1999-12-24 2002-12-01 Aventis Pharma Ltd Azaindoles
JP2003520855A (ja) * 2000-01-28 2003-07-08 アストラゼネカ アクチボラグ 化学的化合物
WO2001056993A2 (fr) 2000-02-05 2001-08-09 Vertex Pharmaceuticals Incorporated Compositions de pyrazole utiles en tant qu'inhibiteurs d'erk
CN1362953A (zh) * 2000-02-05 2002-08-07 沃泰克斯药物股份有限公司 用作erk抑制剂的吡唑组合物
EP1134221A1 (fr) 2000-03-15 2001-09-19 Aventis Pharma Deutschland GmbH Bêta-carbolines substituées comme inhibiteurs de lkB kinase
AU2001237418B2 (en) * 2000-03-15 2007-01-11 Sanofi-Aventis Deutschland Gmbh Substituted beta-carbolines with ikb-kinase inhibiting activity
EP1209158A1 (fr) 2000-11-18 2002-05-29 Aventis Pharma Deutschland GmbH Bêta-carbolines subtituées
JP2001294772A (ja) 2000-04-10 2001-10-23 Fuji Photo Film Co Ltd 着色組成物、インクジェット用インク及びインクジェット記録方法
JP2001302667A (ja) * 2000-04-28 2001-10-31 Bayer Ag イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体
US6555329B2 (en) * 2000-06-09 2003-04-29 Boehringer Ingelheim International Gmbh Method for identifying compounds altering higher-order chromatin-dependent chromosome stability
US6335342B1 (en) 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
EP1299381B1 (fr) 2000-06-28 2008-05-07 AstraZeneca AB Derives de la quinazoline substitues et leur utilisation comme inhibiteurs
AU2002222933A1 (en) 2000-07-13 2002-01-30 Millennium Pharamaceuticals, Inc. Inhibitors of factor xa
US20050009876A1 (en) * 2000-07-31 2005-01-13 Bhagwat Shripad S. Indazole compounds, compositions thereof and methods of treatment therewith
PL213199B1 (pl) 2000-08-10 2013-01-31 Pharmacia Italia Spa Zwiazek bicyklo-pirazolowy, sposób wytwarzania go, jego kompozycja farmaceutyczna, oraz kombinatoryczna biblioteka chemiczna
US6352858B1 (en) * 2000-09-11 2002-03-05 Isis Pharmaceuticals, Inc. Antisense modulation of BTAK expression
AU2001292670A1 (en) 2000-09-15 2002-03-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
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
US6610677B2 (en) * 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6613776B2 (en) * 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
MXPA03004644A (es) * 2000-11-27 2003-09-05 Pharmacia Italia Spa Derivados de fenilacetamdia-pirazol y su uso como agentes antitumorales.
US6455559B1 (en) 2001-07-19 2002-09-24 Pharmacia Italia S.P.A. Phenylacetamido-pyrazole derivatives, process for their preparation and their use as antitumor agents
HUP0302553A3 (en) 2000-11-28 2009-03-30 Pfizer Prod Inc Salts of a isothiazole-4-carboxamide and process for their preparation and use for the preparation of anti-hyperproliferation agents
FR2818278B1 (fr) 2000-12-20 2003-02-28 Sod Conseils Rech Applic Inhibiteurs de kinases dependantes des cyclines (cdk) et de la glycogene synthase kinase-3 (gsk-3)
AU2509602A (en) * 2000-12-20 2002-07-01 Sod Conseils Rech Applic Cyclin-dependent kinase (CDK) and glycolene synthase kinase-3 (GSK-3) inhibitors
MXPA03005606A (es) 2000-12-21 2003-10-06 Vertex Pharma Compuestos de pirazol utiles como inhibidores de la proteina cinasa.
GB0102687D0 (en) 2001-02-02 2001-03-21 Pharmacia & Upjohn Spa Oxazolyl-pyrazole derivatives active as kinase inhibitors,process for their preparation and pharmaceutical compositions comprising them
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
US6864255B2 (en) 2001-04-11 2005-03-08 Amgen Inc. Substituted triazinyl amide derivatives and methods of use
IL157933A0 (en) * 2001-05-14 2004-03-28 Pfizer Prod Inc Tartrate salts of 5,8,14-triazatetracyclo [10.3.1.02,11.04,9] -hexadeca-2(11),3,5,7,9-pentaene and pharmaceutical compositions thereof
US20050090498A1 (en) * 2001-05-24 2005-04-28 Kiyohiro Samizu 3-Quinolin-2(1h)-ylideneindolin-2-one derivative
US20030208067A1 (en) 2001-05-30 2003-11-06 Cao Sheldon Xiaodong Inhibitors of protein kinase for the treatment of disease
US6762179B2 (en) * 2001-05-31 2004-07-13 Vertex Pharmaceuticals Incorporated Thiazole compounds useful as inhibitors of protein kinase
DE60214703T2 (de) * 2001-06-01 2007-09-13 Vertex Pharmaceuticals Inc., Cambridge Thiazolverbindungen, die sich als inhibitoren von proteinkinasen eignen
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
CN1701114A (zh) 2001-06-22 2005-11-23 宝洁公司 用于亲脂流体体系的织物护理组合物
GB0115393D0 (en) 2001-06-23 2001-08-15 Aventis Pharma Ltd Chemical compounds
WO2003008365A2 (fr) 2001-07-19 2003-01-30 Pharmacia Italia S.P.A. Derives de phenylacetamido-thiazole, leur procede de preparation et leur utilisation en tant qu'agents antitumoraux
WO2003009852A1 (fr) 2001-07-24 2003-02-06 Merck & Co., Inc. Inhibiteurs de tyrosine kinase
WO2003012046A2 (fr) 2001-07-27 2003-02-13 The Regents Of The University Of California Polymorphisme du gene stk15 (stk6) et methodes de determination du risque de cancer
WO2003011287A1 (fr) 2001-08-03 2003-02-13 Vertex Pharmaceuticals Incorporated Derives de pyrazole comme inhibiteurs de gsk-3
IL159926A0 (en) * 2001-08-06 2004-06-20 Pharmacia Italia Spa Aminoisoxazole derivatives active as kinase inhibitors
US20030073692A1 (en) * 2001-08-07 2003-04-17 Pharmacia & Upjohn S.P.A. Amino-phthalazinone derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
US6927293B2 (en) 2001-08-30 2005-08-09 Merck & Co., Inc. Tyrosine kinase inhibitors
US6806272B2 (en) * 2001-09-04 2004-10-19 Boehringer Ingelheim Pharma Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
JP2005507922A (ja) 2001-09-19 2005-03-24 ファルマシア・コーポレイション 炎症の治療のための置換されたインダゾール化合物
CA2460939C (fr) * 2001-09-19 2008-07-29 Pharmacia Corporation Composes de pyrazolyl substitues pour le traitement de l'inflammation
JP2005506983A (ja) 2001-09-19 2005-03-10 ファルマシア・コーポレーション 炎症の治療のための置換ピラゾリル化合物
JP2005507892A (ja) * 2001-09-19 2005-03-24 ファルマシア・コーポレーション 炎症の治療のための置換されたピラゾリルベンゼンスルファミド化合物
ES2380054T3 (es) 2001-09-26 2012-05-08 Pfizer Italia S.R.L. Derivados de aminoindazol activos como inhibidores de quinasas, procedimientos para su preparación, y composiciones farmacéuticas que los contienen
GB0124299D0 (en) 2001-10-10 2001-11-28 Astrazeneca Ab Crystal structure of enzyme and uses thereof
WO2003032997A1 (fr) 2001-10-17 2003-04-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Derives pyrimidine, agent pharmaceutique contenant ces composes, utilisation et procede de fabrication de ces composes
US20040010027A1 (en) 2001-12-17 2004-01-15 Pharmacia & Upjohn Spa Hydroxphenyl-pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical comositions comprising them
SE0104340D0 (sv) 2001-12-20 2001-12-20 Astrazeneca Ab New compounds
CN100491372C (zh) 2001-12-24 2009-05-27 阿斯特拉曾尼卡有限公司 作为欧若拉激酶抑制剂的取代喹唑啉衍生物
IL162734A0 (en) 2002-02-01 2005-11-20 Ariad Gene Therapeutics Inc Phosphorus-containing compounds & uses thereof
FR2836914B1 (fr) * 2002-03-11 2008-03-14 Aventis Pharma Sa Indazoles substitues, compositions les contenant, procede de fabrication et utilisation
EP1485100B1 (fr) 2002-03-15 2010-05-05 Vertex Pharmaceuticals Incorporated Azinylaminoazoles utilises comme inhibiteurs de proteine kinases
EP1485381B8 (fr) 2002-03-15 2010-05-12 Vertex Pharmaceuticals Incorporated Azolylaminoazines en tant qu'inhibiteurs de proteines kinases
AU2003220300A1 (en) * 2002-03-15 2003-09-29 Binch, Hayley Compositions useful as inhibitors of protein kinases
ATE468336T1 (de) * 2002-03-15 2010-06-15 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
SE0200979D0 (sv) 2002-03-28 2002-03-28 Astrazeneca Ab New compounds
AU2003230802B2 (en) 2002-04-08 2007-08-09 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
WO2003087395A2 (fr) 2002-04-15 2003-10-23 Inserm Procedes d'identification d'agents antitumoraux inhibiteurs des interactions de rasgap avec la kinase aurora
US7304061B2 (en) * 2002-04-26 2007-12-04 Vertex Pharmaceuticals Incorporated Heterocyclic inhibitors of ERK2 and uses thereof
EP1549318B1 (fr) 2002-05-01 2010-02-17 Vertex Pharmaceuticals Incorporated Structure cristalline de la proteine aurora-2 et poches de liaison associees
MXPA04011417A (es) 2002-05-17 2005-02-14 Pharmacia Italia Spa Derivados de aminoindazol activos como inhibidores de cinasa, procedimiento para su preparacion y composiciones farmaceuticas que los comprenden.
CA2486933A1 (fr) 2002-05-31 2003-12-11 Yamanouchi Pharmaceutical Co., Ltd. Derive tetrahydropyrane
US6989451B2 (en) * 2002-06-04 2006-01-24 Valeant Research & Development Heterocyclic compounds and uses thereof
FR2840905B1 (fr) 2002-06-12 2006-07-07 Centre Nat Rech Scient Anticorps monoclonal anti-aurora-a, son procede d'obtention, et ses utilisations dans le diagnostic et le traitement des cancers
AU2002311176A1 (en) 2002-06-12 2003-12-31 Axia Biosciences, Inc. Chfr protein-catalyzed polyubiquitination of aurora kinase a and aurora kinase b
EP1515949B1 (fr) 2002-06-14 2007-03-14 Merck & Co., Inc. Inhibiteurs de kinesine mitotique
MY141867A (en) * 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
WO2004005283A1 (fr) 2002-07-09 2004-01-15 Vertex Pharmaceuticals Incorporated Imidazoles, oxazoles et thiazoles presentant des activites d'inhibition des proteines kinases
AU2003253880A1 (en) 2002-07-15 2004-02-02 Sugen, Inc. Novel kinases
CA2492673A1 (fr) 2002-07-17 2004-01-22 Pharmacia Italia S.P.A. Derives de pyrazole heterobicycliques utilises comme inhibiteurs de kinase
AU2003244649A1 (en) 2002-07-25 2004-02-23 Pharmacia Italia Spa Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
ATE389658T1 (de) 2002-07-25 2008-04-15 Pfizer Italia Srl Heterocyclische kondensierte pyrazolderivate als kinaseinhibitoren
US20060100233A1 (en) 2002-07-25 2006-05-11 Manuela Villa Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
NZ538715A (en) * 2002-08-14 2007-07-27 Vertex Pharma Protein kinase inhibitors and uses thereof
ES2293015T3 (es) * 2002-09-23 2008-03-16 Schering Corporation Imidazopirazinas como inhibidores de cinasas dependientes de ciclinas.
US20040157804A1 (en) 2002-10-16 2004-08-12 Gilead Sciences, Inc. Pre-organized tricyclic integrase inhibitor compounds
AU2003286711A1 (en) 2002-10-25 2004-05-13 Vertex Pharmaceuticals Incorporated Indazolinone compositions useful as kinase inhibitors
US20040102360A1 (en) * 2002-10-30 2004-05-27 Barnett Stanley F. Combination therapy
GB0226583D0 (en) 2002-11-14 2002-12-18 Cyclacel Ltd Compounds
US6909001B2 (en) 2002-12-12 2005-06-21 Pharmacia Corporation Method of making tricyclic aminocyanopyridine compounds
UA81790C2 (uk) 2002-12-19 2008-02-11 Фармация Италия С.П.А. Заміщені піролопіразольні похідні як інгібітори кінази
WO2004056812A1 (fr) 2002-12-23 2004-07-08 Astrazeneca Ab Derives de 4-(pyridin-4-ylamino)-quinazoline utilises comme agents anticancereux
CA2508921A1 (fr) 2002-12-24 2004-07-15 Astrazeneca Ab Composes de quinazoline
KR101010299B1 (ko) 2002-12-24 2011-01-25 아스트라제네카 아베 포스포노옥시 퀴나졸린 유도체 및 이의 약학적 용도
JP2006512387A (ja) 2002-12-24 2006-04-13 アストラゼネカ アクチボラグ 化合物
CL2004000016A1 (es) 2003-01-21 2005-04-15 Wyeth Corp Compuesto derivado de cloruro de 4-amino-2-butenoilo o una sal farmaceuticamente aceptable del mismo; procedimiento para preparar dicho compuesto, util como intermediario en la sintesis de compuestos inhibidores de proteina quinasa tirosina.
WO2004067516A1 (fr) 2003-01-30 2004-08-12 Boehringer Ingelheim Pharmaceuticals, Inc. Derives de 2,4-diaminopyrimidine utiles en tant qu'inhibiteurs de l'enzyme pkc-theta
WO2004070062A2 (fr) 2003-02-04 2004-08-19 Wyeth Compositions et techniques de diagnostic et de traitement de cancers
CA2513716A1 (fr) 2003-02-14 2004-08-26 Applied Research Systems Ars Holding N.V. Derives de piperazine-2-carboxamide
MXPA05008688A (es) 2003-02-17 2005-10-05 Pharmacia Italia Spa Derivados tetraciclicos de pirazol como inhibidores de la cinasa, procedimiento para su preparacion y composiciones farmaceuticas que los comprenden.
WO2004076454A1 (fr) 2003-02-26 2004-09-10 Boehringer Ingelheim Pharma Gmbh & Co Kg Dihydropteridinones, prodede de production et utilisation de ces dernieres comme medicaments
US6861422B2 (en) * 2003-02-26 2005-03-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
AR050920A1 (es) 2003-03-07 2006-12-06 Astrazeneca Ab Enantiomeros de heterociclos fusionados seleccionados y usos de los mismos
JP2006519816A (ja) 2003-03-11 2006-08-31 ファルマシア・イタリア・ソシエタ・ペル・アツィオーニ キナーゼ阻害剤として活性なビシクロピラゾール誘導体、それらの製造方法、及びそれらを含んでなる医薬組成物
DE602004024374D1 (de) 2003-03-13 2010-01-14 Vertex Pharma Zusammensetzungen zur verwendung als protein-kinase-inhibitoren
US7223766B2 (en) 2003-03-28 2007-05-29 Scios, Inc. Bi-cyclic pyrimidine inhibitors of TGFβ
EP1608652A1 (fr) 2003-03-31 2005-12-28 Vernalis (Cambridge) Limited Composes pyrazolopyrimidines et leur utilisation en medecine
WO2004090106A2 (fr) 2003-04-04 2004-10-21 Vertex Pharmaceuticals Incorporated Structures cristallines de complexes proteiques humains de la pim-1 kinase et poches de liaison de ces structures, et leurs utilisations dans la conception de medicaments
EA009121B1 (ru) * 2003-04-09 2007-10-26 Миллениум Фармасьютикалз, Инк. Бета-карболины, применяемые для лечения воспалительных заболеваний
JP2006522789A (ja) * 2003-04-11 2006-10-05 グレンマーク・ファーマシューティカルズ・エス・エー 炎症性およびアレルギー性障害の治療に有用な新規な複素環式化合物；それらの調製方法および医薬組成物
ES2301981T3 (es) 2003-04-16 2008-07-01 Astrazeneca Ab Derivados de quinazolina para el tratamiento del cancer.
WO2004096129A2 (fr) 2003-04-24 2004-11-11 Merck & Co., Inc. Inhibiteurs de l'activite de l'akt
US7579355B2 (en) 2003-04-24 2009-08-25 Merck & Co., Inc. Inhibitors of Akt activity
WO2004096130A2 (fr) 2003-04-24 2004-11-11 Merck & Co., Inc. Inhibiteurs de l'activite akt
DE602004023838D1 (de) 2003-04-24 2009-12-10 Merck & Co Inc Hemmer der akt aktivität
US20040242559A1 (en) 2003-04-25 2004-12-02 Aventis Pharma S.A. Novel indole derivatives, preparation thereof as medicinal products and pharmaceutical compositions, and especially as KDR inhibitors
EP1622684A4 (fr) 2003-05-01 2007-07-25 Univ Michigan Compositions et procedes de recherche de nouveaux composes et leurs cibles
DE602004029242D1 (en) 2003-05-01 2010-11-04 Bristol Myers Squibb Co Pyrazolamidverbindungen
US20050125852A1 (en) 2003-05-09 2005-06-09 Sugen, Inc. Novel kinases
US7482354B2 (en) 2003-05-22 2009-01-27 Nerviano Medical Sciences S.R.L. Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
US7345046B2 (en) * 2003-05-30 2008-03-18 Chiron Corporation Heteroaryl-fused pyrimidinyl compounds as anticancer agents
US20060135541A1 (en) 2003-06-02 2006-06-22 Astrazeneca Ab (3-((Quinazolin-4-yl) amino)-1h-pyrazol-1-yl)acetamide derivatives and related compounds as aurora kinase inhibitors for the treatment of proliferative diseases such as cancer
TW200505452A (en) 2003-06-17 2005-02-16 Astrazeneca Ab Chemical compounds
ATE458735T1 (de) * 2003-06-20 2010-03-15 Novartis Vaccines & Diagnostic Pyridino[1,2-a pyrimidin-4-onverbindungen als mittel gegen krebs
WO2005009348A2 (fr) 2003-06-25 2005-02-03 Ariad Pharmaceuticals, Inc. Derives de purine substitues
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
PL1641775T3 (pl) 2003-07-03 2009-07-31 Euro Celtique Sa Pochodne 2-pirydynoalkin użyteczne do leczenia bólu
AU2003304266A1 (en) 2003-07-03 2005-01-21 Cambridge University Technical Services Ltd Use of aurora kinase inhibitors for reducing the resistance of cancer cells
GB0315657D0 (en) 2003-07-03 2003-08-13 Astex Technology Ltd Pharmaceutical compounds
US20050032869A1 (en) 2003-07-08 2005-02-10 Pharmacia Italia S.P.A. Pyrazolyl-indole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
GB0315966D0 (en) 2003-07-08 2003-08-13 Cyclacel Ltd Compounds
US7141568B2 (en) * 2003-07-09 2006-11-28 Pfizer Italia S.R.L. Pyrrolo[3,4-c]pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
WO2005016252A2 (fr) 2003-07-11 2005-02-24 Ariad Gene Therapeutics, Inc. Macrocycles contenant du phosphore
US7449465B2 (en) 2003-07-16 2008-11-11 Janssen Pharmaceutica, N.V. Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors
NZ545058A (en) 2003-07-16 2008-05-30 Janssen Pharmaceutica Nv Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors
AU2004261400A1 (en) 2003-07-21 2005-02-10 Laboratoires Serono Sa Alkynyl aryl carboxamides
US20050101623A1 (en) * 2003-07-23 2005-05-12 Pharmacia Corporation Beta-carboline compounds and analogues thereof as mitogen-activated protein kinase-activated protein kinase-2 inhibitors
EP2067776A1 (fr) 2003-07-24 2009-06-10 Euro-Celtique S.A. Composes de piperidine et compositions pharmaceutiques les contenant
US20050026984A1 (en) * 2003-07-29 2005-02-03 Aventis Pharma S.A. Substituted thieno [2,3-c] pyrazoles and their use as medicinal products
US7619059B2 (en) 2003-07-29 2009-11-17 Life Technologies Corporation Bimolecular optical probes
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
BRPI0412347A (pt) 2003-07-30 2006-09-05 Cyclacel Ltd 2-aminofenil-4-fenilpiridinas como inibidores de quinase
US7094791B2 (en) 2003-07-31 2006-08-22 Avalon Pharmaceuticals, Inc. Derivatives of 3-hydroxy-pyrrole-2,4-dicarboxylic acid and uses thereof
US20050043346A1 (en) * 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
US7279575B2 (en) * 2003-08-08 2007-10-09 Pfizer Italia S.R.L. Pyrimidylpyrrole derivatives active as kinase inhibitors
AU2004267094A1 (en) 2003-08-20 2005-03-03 Vertex Pharmaceuticals Incorporated (4 -amino -1,2, 5-oxadiazol-4-yl) -hetxiroaromatic compounds useful as protein kinase inhibitors
AR045595A1 (es) 2003-09-04 2005-11-02 Vertex Pharma Composiciones utiles como inhibidores de proteinas quinasas
WO2005026155A1 (fr) 2003-09-12 2005-03-24 Applied Research Systems Ars Holding N.V. Benzoxazole acétonitriles
MXPA06002964A (es) 2003-09-16 2006-06-14 Astrazeneca Ab Derivados de quinazolina como inhibidores de cinasa de tirosina.
WO2005026156A1 (fr) 2003-09-16 2005-03-24 Astrazeneca Ab Derives de quinazoline
US20070032513A1 (en) 2003-09-16 2007-02-08 Hennequin Laurent F A Quinazoline derivatives
EP1670422A4 (fr) 2003-09-17 2007-08-01 Sunesis Pharmaceuticals Inc Identification d'inhibiteurs de kinase
KR20070064414A (ko) 2003-09-17 2007-06-20 이코스 코포레이션 세포 증식 제어를 위한 ｃｈｋ1 억제제의 용도
EP1664046B1 (fr) 2003-09-19 2009-06-17 Gilead Sciences, Inc. Composes d'aza-quinolinol phosphonate inhibiteurs de l'integrase
US20050085531A1 (en) * 2003-10-03 2005-04-21 Hodge Carl N. Thiophene-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof
CN1897950A (zh) 2003-10-14 2007-01-17 惠氏公司 稠合芳基和杂芳基衍生物及其使用方法
ATE437872T1 (de) 2003-10-14 2009-08-15 Univ Arizona Proteinkinaseinhibitoren
BRPI0415390A (pt) 2003-10-14 2006-12-12 Pharmacia Corp compostos de pirazinona substituìda para o tratamento da inflamação
KR20060123164A (ko) 2003-10-17 2006-12-01 아스트라제네카 아베 암 치료에 사용하기 위한 4-(피라졸-3-일아미노)피리미딘유도체
AU2004285745A1 (en) 2003-10-21 2005-05-12 Cyclacel Limited Pyrimidin-4-YL-3, 4-thione compounds and their use in therapy
WO2005037797A1 (fr) 2003-10-21 2005-04-28 Pharmacia Corporation Composes d'uree de pyrazole substituee utiles dans le traitement d'inflammations
JP2007509126A (ja) 2003-10-23 2007-04-12 ファルマシア・コーポレーション 炎症の治療のためのピリミジン化合物
WO2005044270A1 (fr) 2003-11-04 2005-05-19 4Sc Ag Derives de l'oxadiazolopyrazine utilises comme composes pharmaceutiquement actifs
JP5095216B2 (ja) 2003-11-14 2012-12-12 ローラス セラピューティクス インコーポレーテッド アリールイミダゾールおよびその抗癌剤としての使用
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
CA2546360A1 (fr) * 2003-11-19 2005-06-09 Signal Pharmaceuticals, Llc Procedes de traitement de maladies et de troubles par le ciblage de kinases multiples
FR2864084B1 (fr) 2003-12-17 2006-02-10 Aventis Pharma Sa Nouveaux derives organophosphores des indazoles et leur utilisation comme medicaments
EP1713814A1 (fr) 2003-12-17 2006-10-25 SGX Pharmaceuticals, Inc. Composes a fusion pyrazolo bicycliques utilises comme modulateurs de proteine kinases
GB0330043D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions comprising them
GB0330042D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions them
WO2005071419A2 (fr) 2004-01-16 2005-08-04 Ipsogen Etablissement de profils d'expression de proteines et prognose du cancer du sein
CN1910183A (zh) 2004-01-23 2007-02-07 希龙公司 四氢咔啉化合物作为抗癌药
TW200526204A (en) 2004-02-03 2005-08-16 Pharmacia Italia Spa 1h-thieno[2,3-c]pyrazole derivatives useful as kinase inhibitors
FR2865934B1 (fr) * 2004-02-05 2006-05-05 Sanofi Synthelabo Utilisation de derives d'indolizine 1,2,3 substitues, inhibiteurs des fgfs, pour la preparation de medicaments utiles pour le traitement de maladies liees a une angiogenese pathologique choroidienne
GB0402653D0 (en) 2004-02-06 2004-03-10 Cyclacel Ltd Compounds
TW200536536A (en) * 2004-02-25 2005-11-16 Schering Corp Pyrazolotriazines as kinase inhibitors
EP1730124A4 (fr) 2004-03-26 2009-04-01 Amphora Discovery Corp Composes et compositions a base de triazoles et leurs applications
PL2332940T3 (pl) 2004-03-30 2013-03-29 Vertex Pharma Azaindole użyteczne jako inhibitory JAK i innych kinaz białkowych
BRPI0509580A (pt) 2004-03-30 2007-11-27 Pfizer Prod Inc combinações de inibidores de transdução de sinal
FR2868421B1 (fr) 2004-04-01 2008-08-01 Aventis Pharma Sa Nouveaux benzothiazoles et leur utilisation comme medicaments
AU2005249380C1 (en) 2004-04-23 2012-09-20 Exelixis, Inc. Kinase modulators and methods of use
US20050250829A1 (en) 2004-04-23 2005-11-10 Takeda San Diego, Inc. Kinase inhibitors
TW200538453A (en) 2004-04-26 2005-12-01 Bristol Myers Squibb Co Bicyclic heterocycles as kinase inhibitors
WO2005105777A1 (fr) 2004-05-05 2005-11-10 Pharmacia & Upjohn Company Llc Composes d'amide a substitution de thiophene pour le traitement de l'inflammation.
AU2005245386B2 (en) 2004-05-07 2008-11-27 Amgen Inc. Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer
EP2719698B1 (fr) 2004-05-14 2016-10-05 Millennium Pharmaceuticals, Inc. Procédés pour la préparation d'inhibiteurs de l'aurora kinase
JP4812763B2 (ja) 2004-05-18 2011-11-09 ライジェル ファーマシューティカルズ， インコーポレイテッド シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途
EP1598343A1 (fr) 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH Dérivés de 2-arylaminopyrimidines comme des inhibiteurs de PLK
WO2005113550A1 (fr) 2004-05-20 2005-12-01 Mitsubishi Pharma Corporation Dérivé d'aminopyrimidine et utilisation médicinale de celui-ci
EP1753723B1 (fr) 2004-05-21 2008-08-13 Novartis Vaccines and Diagnostics, Inc. Dérivés de quinolinone substituée en tant qu"inhibiteurs de kinésine mitotique
JP2008500057A (ja) 2004-05-27 2008-01-10 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 Ｉｍｐｄｈ経路の阻害をモニタリングするためのバイオマーカー
WO2005118587A1 (fr) 2004-06-02 2005-12-15 Takeda Pharmaceutical Company Limited Dérivé d’indole et usage pour le traitement du cancer
EP1781293A1 (fr) 2004-06-04 2007-05-09 Amphora Discovery Corporation Composes a base de quinoleine et d'isoquinoleine presentant une activite d'inhibition d'enzymes utilisant de l'atp et compositions et utilisations de ceux-ci
FR2871158A1 (fr) 2004-06-04 2005-12-09 Aventis Pharma Sa Indazoles substitues, compositions les contenant, procede de fabrication et utilisation
BRPI0511065A (pt) 2004-06-04 2007-12-26 Pfizer Prod Inc método para tratar crescimento de célula anormal
EP1773807A2 (fr) 2004-06-14 2007-04-18 Takeda San Diego, Inc. Inhibiteurs de kinase
CA2568756A1 (fr) 2004-06-15 2005-12-29 Astrazeneca Ab Quinazolones substitues en tant qu'agents anticancereux
KR101170925B1 (ko) 2004-06-18 2012-08-07 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 암 치료용 키네신 방추 단백질 (ｋｓｐ) 억제제로서의ｎ-(1-(1-벤질-4-페닐-1ｈ-이미다졸-2-일)-2,2-디메틸프로필)벤자미드 유도체 및 관련 화합물
DE102004029784A1 (de) * 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel
EP1765820A4 (fr) 2004-06-23 2010-07-21 Irm Llc Composes et compositions utilises en tant qu'inhibiteurs des proteines kinases
CA2570552A1 (fr) 2004-06-28 2006-01-05 Altana Pharma Ag Pyrimidines 4,6-disubstituees et leur utilisation comme inhibiteurs des proteines kinases
US7253167B2 (en) 2004-06-30 2007-08-07 Bristol-Myers Squibb Company Tricyclic-heteroaryl compounds useful as kinase inhibitors
JP2008505089A (ja) 2004-07-01 2008-02-21 メルク　エンド　カムパニー　インコーポレーテッド 有糸***キネシン阻害剤
TW200616974A (en) 2004-07-01 2006-06-01 Astrazeneca Ab Chemical compounds
CA2571824A1 (fr) 2004-07-01 2006-01-19 Merck & Co., Inc. Inhibiteurs de kinesine mitotique
WO2006003440A1 (fr) 2004-07-05 2006-01-12 Astex Therapeutics Limited Pyrazoles 3,4-disubstitutes servant d'inhibiteurs de kinases cyclines dependantes (cdk), ou de kinases aurora ou de glycogene syntases 3 (gsk-3)
CA2571937A1 (fr) 2004-07-08 2006-02-09 Boehringer Ingelheim Pharmaceuticals, Inc. Derives de pyrimidine utiles comme inhibiteurs de la pkc-theta
WO2006005941A1 (fr) 2004-07-12 2006-01-19 Istituto Di Ricerche Di Biologia Molecolare P Angeletti S.P.A. Derives amidiques inhibiteurs de l'histone deacetylase
EP1768956A1 (fr) 2004-07-12 2007-04-04 Istituto di Richerche di Biologia Molecolare P. Angeletti S.p.A. Derives amide en tant qu'inhibiteurs d'histone deacetylase
DE102004034623A1 (de) 2004-07-16 2006-02-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 6-Formyl-tetrahydropteridine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
JP2008506714A (ja) 2004-07-16 2008-03-06 サネシス ファーマシューティカルズ， インコーポレイテッド オーロラキナーゼインヒビターとして有用なチエノピリミジン
WO2006012624A2 (fr) 2004-07-21 2006-02-02 The Regents Of The University Of California Agents de reticulation fondes sur un mecanisme
WO2006008545A2 (fr) 2004-07-22 2006-01-26 Astex Therapeutics Limited Composes pharmaceutiques
CN101023082A (zh) 2004-07-22 2007-08-22 阿斯利康(瑞典)有限公司 用于治疗和预防癌症的稠合嘧啶酮类
US7361763B2 (en) 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
EP1782315A4 (fr) 2004-07-30 2009-06-24 Rosetta Inpharmatics Llc Pronostic de patients atteints d'un cancer du sein
BRPI0514094A (pt) 2004-08-02 2008-05-27 Osi Pharm Inc composto, composição, e, método de tratamento de distúrbio hiperproliferativo
US20060141549A1 (en) 2004-08-03 2006-06-29 Sudipta Mahajan Cell-based kinase assay
WO2006023083A1 (fr) 2004-08-12 2006-03-02 Merck & Co., Inc. Inhibiteurs de kinesine mitotiques
ES2401138T3 (es) 2004-08-13 2013-04-17 Genentech, Inc. Inhibidores basados en tiazol de enzimas que usan ATP
JP2008510013A (ja) 2004-08-18 2008-04-03 メルク エンド カムパニー インコーポレーテッド 有糸***キネシン阻害剤
AU2005277587A1 (en) 2004-08-18 2006-03-02 Merck Sharp & Dohme Corp. Mitotic kinesin inhibitors
EP1778669A2 (fr) 2004-08-18 2007-05-02 Takeda San Diego, Inc. Inhibiteurs de kinase
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
EP1784175A4 (fr) 2004-08-23 2009-07-22 Merck & Co Inc Inhibiteurs de l'activite de akt
JP2008510770A (ja) 2004-08-26 2008-04-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｐｌｋ阻害剤としての新規プテリジノン
MY191349A (en) 2004-08-27 2022-06-17 Bayer Pharmaceuticals Corp New pharmaceutical compositions for the treatment of hyper-proliferative disorders
JP2008510771A (ja) 2004-08-27 2008-04-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ジヒドロプテリジノン、その製造方法および医薬薬剤としてのその使用
WO2006026597A2 (fr) 2004-08-30 2006-03-09 Smithkline Beecham Corporation Nouvelles compositions et procedes de traitement
GB0419416D0 (en) 2004-09-01 2004-10-06 Inst Of Ex Botany Ascr 4-Arylazo-3,5-Diamino-Pyrazole compounds and use thereof
CN101010303A (zh) 2004-09-01 2007-08-01 阿斯利康(瑞典)有限公司 喹唑啉酮衍生物和它们作为b－raf抑制剂的用途
AR050926A1 (es) 2004-09-03 2006-12-06 Astrazeneca Ab Derivados de benzamida como inhibidores de la histonadesacetilasa(hdac)
US7608622B2 (en) 2004-09-24 2009-10-27 Janssen Pharmaceutica Nv Imidazo[4,5-b]pyrazinone inhibitors of protein kinases
TW200624431A (en) 2004-09-24 2006-07-16 Hoffmann La Roche Phthalazinone derivatives, their manufacture and use as pharmaceutical agents
CA2581375A1 (fr) 2004-09-27 2006-04-06 Kosan Biosciences Incorporated Inhibiteurs de kinases specifiques
US20060069101A1 (en) 2004-09-27 2006-03-30 Kim Kyoung S Prodrugs of protein tyrosine kinase inhibitors
JP5002460B2 (ja) 2004-10-04 2012-08-15 ミレニアム ファーマシューティカルズ， インコーポレイテッド タンパク質キナーゼインヒビターとして有用なラクタム化合物
FR2876377B1 (fr) 2004-10-11 2007-03-16 Univ Claude Bernard Lyon Nouveaux derives de 9h-pyrido[2,3-b]indole, leur procede de preparation, ainsi que les compositions pharmaceutiques contenant de tels composes
NZ554017A (en) 2004-10-12 2010-06-25 Astrazeneca Ab [(Quinazolin-4-yloxy)phenyl]acetamide derivatives
WO2006040568A1 (fr) 2004-10-15 2006-04-20 Astrazeneca Ab Quinoxalines en tant qu'inhibiteurs b-raf
WO2006050076A1 (fr) 2004-10-29 2006-05-11 Janssen Pharmaceutica, N.V. Composes de pyrrolyle fusionnes substitues par pyrimidinyle et utiles dans le traitement des troubles induits par la kinase
NZ554441A (en) 2004-10-29 2009-07-31 Banyu Pharma Co Ltd Novel aminopyridine derivatives having aurora A selective inhibitory action
US7795259B2 (en) 2004-11-22 2010-09-14 Vertex Pharmaceuticals Incorporated Pyrrolopyrazines and pyrazolopyrazines useful as inhibitors of protein kinases
GB0427917D0 (en) 2004-12-21 2005-01-26 Astrazeneca Ab Chemical compounds
ITPI20040099A1 (it) 2004-12-24 2005-03-24 Maurizio Pacini Sistema di realizzazione di tappeto erboso mediante micro-plantule preradicate
WO2006070198A1 (fr) 2004-12-30 2006-07-06 Astex Therapeutics Limited Derives pyrazoliques modulant l'activite des kinases cdk, gsk et aurora
EP1836199A1 (fr) 2004-12-30 2007-09-26 Astex Therapeutics Limited Derives de thiazole et isothiazole modulant l'activite des kinases cdk, gsk et aurora
EP2395000A1 (fr) 2004-12-30 2011-12-14 Astex Therapeutics Limited Composés de benzimidazole régulant l' activite de kinases CDK, GSK et aurora
GB0500492D0 (en) 2005-01-11 2005-02-16 Cyclacel Ltd Compound
GB0504475D0 (en) 2005-03-04 2005-04-13 Astrazeneca Ab Chemical compounds
GB0504474D0 (en) 2005-03-04 2005-04-13 Astrazeneca Ab Chemical compounds
FR2882751B1 (fr) 2005-03-04 2007-09-14 Aventis Pharma Sa Hydrazinocarbonyl-thieno[2,3-c]pyrazoles, procede de preparation, compositions les contenant et utilisation
FR2884821B1 (fr) 2005-04-26 2007-07-06 Aventis Pharma Sa Pyrrolopyridines substitues, compositions les contenant, procede de fabrication et utilisation
GB0509224D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Inhibitors of intracellular enzymatic activity
GB0509227D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Intracellular enzyme inhibitors
GB0509223D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Enzyme inhibitors
US7541367B2 (en) 2005-05-31 2009-06-02 Janssen Pharmaceutica, N.V. 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders
WO2006131552A1 (fr) 2005-06-09 2006-12-14 Boehringer Ingelheim International Gmbh Alpha-carbolines comme inhibiteurs de cdk-1
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
US20090326229A1 (en) * 2006-08-02 2009-12-31 Takeda Phamaceutical Company Limited Alpha-carboline derivatives and methods for preparation thereof
EP2081930A2 (fr) 2006-10-09 2009-07-29 Takeda San Diego, Inc. Inhibiteurs de kinases
EP2223925A1 (fr) * 2006-10-09 2010-09-01 Takeda Pharmaceutical Company Limited Inhibiteurs de kinase
AU2007313961A1 (en) 2006-10-09 2008-05-08 Takeda Pharmaceutical Company Limited Kinase inhibitors
US20100120717A1 (en) * 2006-10-09 2010-05-13 Brown Jason W Kinase inhibitors
US20090312288A1 (en) * 2008-04-16 2009-12-17 Takeda Pharmaceutical Company Limited Kinase inhibitors

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ATE495173T1 (de) 2011-01-15
ES2358006T3 (es) 2011-05-04
WO2007044779A1 (fr) 2007-04-19
DE602006019651D1 (de) 2011-02-24
EA200800725A1 (ru) 2009-02-27
US20070117816A1 (en) 2007-05-24
EP2133349A1 (fr) 2009-12-16
EP1931669A1 (fr) 2008-06-18
KR20080051153A (ko) 2008-06-10
IL190306A0 (en) 2009-09-22
AU2006302135B2 (en) 2012-05-17
US8119655B2 (en) 2012-02-21
CY1111346T1 (el) 2015-08-05
RS51897B (en) 2012-02-29
CA2624610A1 (fr) 2007-04-19
DK2133349T3 (da) 2011-03-28
EP2133349B1 (fr) 2011-01-12
SI2133349T1 (sl) 2011-05-31
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US8318939B2 (en) 2012-11-27
PL2133349T3 (pl) 2011-08-31
MY146989A (en) 2012-10-15
CR9886A (es) 2008-08-01
CN101356172B (zh) 2012-06-13
EA015902B1 (ru) 2011-12-30
HK1138842A1 (en) 2010-09-03
AU2006302135A1 (en) 2007-04-19
AU2006302135A2 (en) 2009-12-17
ZA200802820B (en) 2010-02-24
CN101356172A (zh) 2009-01-28
PT2133349E (pt) 2011-03-17
NZ566866A (en) 2011-12-22
BRPI0616950A2 (pt) 2009-11-24
JP5150878B2 (ja) 2013-02-27
US20100190816A1 (en) 2010-07-29
HRP20110220T1 (hr) 2011-04-30
NO20081564L (no) 2008-07-02

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