EA200300248A1 - Бициклопиразолы, активные в качестве ингибиторов киназы, способ их получения и включающие их фармацевтические композиции - Google Patents

Бициклопиразолы, активные в качестве ингибиторов киназы, способ их получения и включающие их фармацевтические композиции

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Publication number
EA200300248A1
EA200300248A1 EA200300248A EA200300248A EA200300248A1 EA 200300248 A1 EA200300248 A1 EA 200300248A1 EA 200300248 A EA200300248 A EA 200300248A EA 200300248 A EA200300248 A EA 200300248A EA 200300248 A1 EA200300248 A1 EA 200300248A1
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EA
Eurasian Patent Office
Prior art keywords
bicyclopirasoles
active
receiving
pharmaceutical compositions
kinase inhibitors
Prior art date
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EA200300248A
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English (en)
Other versions
EA006381B1 (ru
Inventor
Даниеле Фанчелли
Валерия Питтала'
Марио Варази
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Фармация Италия С.П.А.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=24549630&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA200300248(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Фармация Италия С.П.А. filed Critical Фармация Италия С.П.А.
Publication of EA200300248A1 publication Critical patent/EA200300248A1/ru
Publication of EA006381B1 publication Critical patent/EA006381B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • 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
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • CCHEMISTRY; METALLURGY
    • C40COMBINATORIAL TECHNOLOGY
    • C40BCOMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00Libraries per se, e.g. arrays, mixtures

Abstract

Производные бициклопиразола формулы (I), как здесь указано, являются полезными для лечения заболеваний, связанных с протеинкиназами с нарушенной регуляцией.Отчет о международном поиске был опубликован 2002.06.06.
EA200300248A 2000-08-10 2001-07-25 Бициклопиразолы, активные в качестве ингибиторов киназы, способ их получения и включающие их фармацевтические композиции EA006381B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US63591400A 2000-08-10 2000-08-10
PCT/EP2001/008639 WO2002012242A2 (en) 2000-08-10 2001-07-25 Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them

Publications (2)

Publication Number Publication Date
EA200300248A1 true EA200300248A1 (ru) 2003-08-28
EA006381B1 EA006381B1 (ru) 2005-12-29

Family

ID=24549630

Family Applications (1)

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EA200300248A EA006381B1 (ru) 2000-08-10 2001-07-25 Бициклопиразолы, активные в качестве ингибиторов киназы, способ их получения и включающие их фармацевтические композиции

Country Status (29)

Country Link
US (3) US7541354B2 (ru)
EP (1) EP1320531B1 (ru)
JP (2) JP4555547B2 (ru)
KR (1) KR100904157B1 (ru)
CN (2) CN102060857A (ru)
AR (1) AR034137A1 (ru)
AT (1) ATE480539T1 (ru)
AU (2) AU2001287654B2 (ru)
BR (1) BR0113176A (ru)
CA (1) CA2416527C (ru)
CY (1) CY1110914T1 (ru)
CZ (1) CZ2003591A3 (ru)
DE (1) DE60143041D1 (ru)
DK (1) DK1320531T3 (ru)
EA (1) EA006381B1 (ru)
EE (1) EE05405B1 (ru)
ES (1) ES2349762T3 (ru)
HU (1) HU229824B1 (ru)
IL (2) IL153997A0 (ru)
MX (1) MXPA03001169A (ru)
MY (1) MY148632A (ru)
NO (1) NO325530B1 (ru)
NZ (1) NZ524475A (ru)
PE (1) PE20020274A1 (ru)
PL (1) PL213199B1 (ru)
PT (1) PT1320531E (ru)
SK (1) SK1882003A3 (ru)
WO (1) WO2002012242A2 (ru)
ZA (1) ZA200301813B (ru)

Families Citing this family (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU229824B1 (en) * 2000-08-10 2014-08-28 Pfizer Italia Srl Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
US20030195192A1 (en) * 2002-04-05 2003-10-16 Fortuna Haviv Nicotinamides having antiangiogenic activity
RS98804A (en) 2002-05-15 2006-10-27 Janssen Pharmaceutica N.V. N-substituted tricyclic 3-aminopyrazoles as pdfg receptor ihhibitors
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.
ATE393159T1 (de) * 2002-07-17 2008-05-15 Pfizer Italia Srl Heterobicyclische pyrazolderivate als kinaseinhibitoren
BR0312961A (pt) * 2002-07-25 2005-06-14 Pharmacia Italia Spa Derivados condensados heterociclicos de pirazol como inibidores de cinase
AU2003244632A1 (en) * 2002-07-25 2004-02-25 Pharmacia Italia S.P.A. Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
BR0312913A (pt) * 2002-07-25 2005-07-12 Pharmacia Italia Spa Ativo de biciclo-pirazóis como inibidores de cinase, processo para sua preparação e composições farmacêuticas compreendendo o mesmo
UA81790C2 (ru) * 2002-12-19 2008-02-11 Фармация Италия С.П.А. Замещенные пиролопиразольные производные как ингибиторы киназы
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
NZ543661A (en) 2003-05-22 2009-05-31 Nerviano Medical Sciences Srl Pyrazolo-quinazoline derivatives having antitumor activity and process for their preparation
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
AR045037A1 (es) * 2003-07-10 2005-10-12 Aventis Pharma Sa Tetrahidro-1h-pirazolo [3,4-c] piridinas sustituidas, composiciones que las contienen y su utilizacion.
CA2534496A1 (en) * 2003-08-08 2005-02-17 Ermes Vanotti Pyrimidylpyrrole derivatives active as kinase inhibitors
US20050043346A1 (en) * 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
WO2005030776A1 (en) 2003-09-23 2005-04-07 Vertex Pharmaceuticals Incorporated Pyrazolopyrrole derivatives as protein kinase inhibitors
US7592466B2 (en) 2003-10-09 2009-09-22 Abbott Laboratories Ureas having antiangiogenic activity
JP2007514759A (ja) 2003-12-19 2007-06-07 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
WO2005063241A1 (ja) * 2003-12-26 2005-07-14 Ono Pharmaceutical Co., Ltd. ミトコンドリアベンゾジアゼピン受容体介在性疾患の予防および/または治療剤
TW200526204A (en) * 2004-02-03 2005-08-16 Pharmacia Italia Spa 1h-thieno[2,3-c]pyrazole derivatives useful as kinase inhibitors
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
WO2006044687A2 (en) 2004-10-15 2006-04-27 Takeda San Diego, Inc. Kinase inhibitors
MX2007005071A (es) * 2004-10-27 2007-10-03 Johnson & Johnson Moduladores de canabinoide de tetrahidro-piridinilpirazol.
US20060128710A1 (en) * 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
DK1838718T3 (da) * 2005-01-10 2011-07-25 Pfizer Pyrrolopyrazoler, potente kinase inhibitorer
FR2880891B1 (fr) * 2005-01-19 2007-02-23 Aventis Pharma Sa Pyrazolo pyridines substituees, compositions les contenant, procede de fabrication et utilisation
PE20061119A1 (es) * 2005-01-19 2006-11-27 Aventis Pharma Sa PIRAZOLO PIRIDINAS SUSTITUIDAS COMO INHIBIDORES DE CINASAS FAK, KDR Y Tie
CN101223167B (zh) * 2005-07-15 2011-08-31 弗·哈夫曼-拉罗切有限公司 杂芳基稠合的环状胺
US7943654B2 (en) 2005-07-19 2011-05-17 Nerviano Medical Sciences S.R.L. 1H-thieno[2,3-c]pyrazole compounds useful as kinase inhibitors
FR2889526B1 (fr) 2005-08-04 2012-02-17 Aventis Pharma Sa 7-aza-indazoles substitues, compositions les contenant, procede de fabrication et utilisation
WO2007023382A2 (en) * 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
EP1957458A2 (en) * 2005-12-01 2008-08-20 Elan Pharmaceuticals Inc. 5-(arylsulfonyl)-pyrazolopiperidines
US7968583B2 (en) 2005-12-12 2011-06-28 Nerviano Medical Sciences S.R.L. Substituted pyrrolo-pyrazole derivatives active as kinase inhibitors
WO2007068619A1 (en) * 2005-12-12 2007-06-21 Nerviano Medical Sciences S.R.L. Substituted pyrazolo [4,3-c] pyridine derivatives active as kinase inhibitors
US7618982B2 (en) 2005-12-19 2009-11-17 Nerviano Medical Sciences S.R.L. Heteroarylpyrrolopyridinones active as kinase inhibitors
GEP20104974B (en) * 2005-12-21 2010-04-26 Pfizer Prod Inc Carbonylamino pyrrolopyrazoles, protent kinase inhibitors
US7504513B2 (en) 2006-02-27 2009-03-17 Hoffman-La Roche Inc. Thiazolyl-benzimidazoles
JP5250432B2 (ja) * 2006-03-03 2013-07-31 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として活性なビシクロピラゾール
WO2007099166A1 (en) * 2006-03-03 2007-09-07 Nerviano Medical Sciences S.R.L. Pyrazolo-pyridine derivatives active as kinase inhibitors
US20070213378A1 (en) * 2006-03-10 2007-09-13 Lymphosign Inc. Compounds for modulating cell proliferation, compositions and methods related thereto
CA2653903A1 (en) * 2006-06-12 2007-12-21 Merck & Co., Inc. Ophthalmic compositions for treating ocular hypertension
WO2008017465A1 (en) * 2006-08-10 2008-02-14 F. Hoffmann-La Roche Ag Bicyclic lactam derivatives, their manufacture and use as pharmaceutical agents
EA200970361A1 (ru) 2006-10-09 2010-02-26 Такеда Фармасьютикал Компани Лимитед Ингибиторы киназы
WO2008043745A1 (en) * 2006-10-11 2008-04-17 Nerviano Medical Sciences S.R.L. Substituted pyrrolo-pyrazole derivatives as kinase inhibitors
JP5528807B2 (ja) 2006-10-12 2014-06-25 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
US8916552B2 (en) 2006-10-12 2014-12-23 Astex Therapeutics Limited Pharmaceutical combinations
AP2009004958A0 (en) 2007-02-07 2009-08-31 Pfizer 3-amino-pyrrolo [3,4-C] pyrazole - 5 (1H, 4H, 6H) carbaldehyde derivatives as PKC inhibitors
JP5337717B2 (ja) 2007-02-27 2013-11-06 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として活性なイソキノリノピロロピリジノン
JP5404601B2 (ja) * 2007-04-12 2014-02-05 ファイザー・インク 新規な3−アミド−ピロロ[3,4−c]ピラゾール−5(1H,4H,6H)カルバルデヒド誘導体
EP2003129B1 (en) 2007-06-11 2017-08-09 Nerviano Medical Sciences S.r.l. 1H-Pyrido[3,4-B]indol-1-one and 2,3,4,9-Tetrahydro-1H-Beta-Carbolin-1-one Derivatives
CN102105148B (zh) 2008-07-24 2013-04-10 内尔维阿诺医学科学有限公司 包含aurora激酶抑制剂和抗肿瘤药的治疗组合
EP2376089B1 (en) * 2008-11-17 2018-03-14 The Regents of the University of Michigan Cancer vaccine compositions and methods of using the same
CN102256972A (zh) 2008-12-18 2011-11-23 霍夫曼-拉罗奇有限公司 噻唑基-苯并咪唑类
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
CA2784807C (en) 2009-12-29 2021-12-14 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
WO2012020227A1 (en) 2010-08-11 2012-02-16 Centro Nacional De Investigaciones Oncologicas (Cnio) Tricyclic compounds for use as kinase inhibitors
WO2012080990A1 (en) 2010-12-17 2012-06-21 Nerviano Medical Sciences S.R.L. Substituted pyrazolo-quinazoline derivatives as kinase inhibitors
CN102134243A (zh) * 2011-03-04 2011-07-27 中国医学科学院医药生物技术研究所 具有抗肿瘤活性的双环氨基吡唑类衍生物
US8771682B2 (en) 2011-04-26 2014-07-08 Technische Universtität Dresden Methods and compositions for reducing interleukin-4 or interleukin-13 signaling
CA2834746A1 (en) 2011-05-04 2012-11-08 Forma Tm, Llc Novel compounds and compositions for the inhibition of nampt
US9382239B2 (en) 2011-11-17 2016-07-05 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
US8969341B2 (en) 2011-11-29 2015-03-03 Novartis Ag Pyrazolopyrrolidine compounds
US8815926B2 (en) 2012-01-26 2014-08-26 Novartis Ag Substituted pyrrolo[3,4-D]imidazoles for the treatment of MDM2/4 mediated diseases
EP2855483B1 (en) 2012-05-24 2017-10-25 Novartis AG Pyrrolopyrrolidinone compounds
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
CN104955458A (zh) * 2012-11-07 2015-09-30 Z·索 取代的吉西他滨芳基酰胺类似物和使用所述类似物的治疗方法
EP2948453B1 (en) 2013-01-22 2017-08-02 Novartis AG Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the p53/mdm2 interaction
WO2014115077A1 (en) 2013-01-22 2014-07-31 Novartis Ag Substituted purinone compounds
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
JP6373978B2 (ja) 2013-05-27 2018-08-15 ノバルティス アーゲー イミダゾピロリジノン誘導体および疾患の処置におけるその使用
ES2650562T3 (es) 2013-05-28 2018-01-19 Novartis Ag Derivados de pirazolo-pirrolidin-4-ona y su uso en el tratamiento de enfermedades
ES2656471T3 (es) 2013-05-28 2018-02-27 Novartis Ag Derivados de pirazolo-pirrolidin-4-ona como inhibidores de BET y su uso en el tratamiento de enfermedades
CA2927917C (en) 2013-10-18 2022-08-09 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
US10047070B2 (en) 2013-10-18 2018-08-14 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
CA2931249A1 (en) 2013-11-21 2015-05-28 Novartis Ag Pyrrolopyrrolone derivatives and their use as bet inhibitors
ES2872338T3 (es) 2014-05-23 2021-11-02 Mingsight Pharmaceuticals Inc Tratamiento de enfermedades autoinmunitarias
EP3214086B1 (en) 2014-10-31 2021-09-22 Ube Industries, Ltd. Substituted dihydropyrrolopyrazole compound
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
US9518057B2 (en) * 2014-12-30 2016-12-13 Novira Therapeutics, Inc. Derivatives and methods of treating hepatitis B infections
CN104530045A (zh) * 2015-01-14 2015-04-22 中国药科大学 吡唑并[4,3-c]四氢吡啶类c-Met激酶抑制剂及其制备方法和用途
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
MY190459A (en) * 2015-06-04 2022-04-21 Aurigene Discovery Tech Ltd Substituted heterocyclyl derivatives as cdk inhibitors
EP3307728A4 (en) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. ASSOCIATION THERAPY USING TRANSCRIPTION INHIBITORS AND KINASE INHIBITORS
MX2017016030A (es) 2015-06-15 2018-08-01 Ube Industries Derivado de dihidropirrolopirazol sustituido.
WO2017044858A2 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
CA3029566A1 (en) 2016-06-29 2018-01-04 Novira Therapeutics, Inc. Diazepinone derivatives and their use in the treatment of hepatitis b infections
CA3029688A1 (en) 2016-06-29 2018-01-04 Novira Therapeutics, Inc. Oxadiazepinone derivatives and their use in the treatment of hepatitis b infections
PE20190732A1 (es) 2016-09-09 2019-05-23 Novartis Ag Compuestos y composiciones como inhibidores de los receptores endosomales tipo peaje
HUE057524T2 (hu) 2016-10-24 2022-05-28 Astrazeneca Ab 6,7,8,9-Tetrahidro-3H-pirazolo[4,3-f]izokinolin-származékok rák kezelésében való alkalmazásra
SI3494116T1 (sl) 2017-01-30 2020-02-28 Astrazeneca Ab Modulatorji receptorja estrogena
BR112019025230A2 (pt) 2017-05-31 2020-06-16 Chemocentryx, Inc. Anéis 5-5 fundidos como inibidores de c5a
JP7141130B2 (ja) 2017-05-31 2022-09-22 ケモセントリックス,インコーポレイティド C5a阻害剤としての6-5融合環
US10435429B2 (en) 2017-10-03 2019-10-08 Nucorion Pharmaceuticals, Inc. 5-fluorouridine monophosphate cyclic triester compounds
KR20200070297A (ko) 2017-10-11 2020-06-17 에프. 호프만-라 로슈 아게 Rip1 키나아제 억제제로서 사용하기 위한 이환형 화합물
EP3704119A1 (en) * 2017-11-02 2020-09-09 AiCuris GmbH & Co. KG Novel, highly active pyrazolo-piperidine substituted indole-2-carboxamides active against the hepatitis b virus (hbv)
MX2020006459A (es) * 2017-12-22 2020-11-06 Chemocentryx Inc Compuestos de anillos fusionados 6,5 diaril sustituidos como inhibidores de c5ar.
CN111788184B (zh) * 2017-12-22 2023-12-22 凯莫森特里克斯股份有限公司 用作C5aR抑制剂的二芳基取代的5,5-稠合环化合物
US11427550B2 (en) 2018-01-19 2022-08-30 Nucorion Pharmaceuticals, Inc. 5-fluorouracil compounds
JP7337833B2 (ja) 2018-04-02 2023-09-04 ケモセントリックス,インコーポレイティド 縮合二環式C5aRアンタゴニストのプロドラッグ
CN110878042B (zh) * 2018-09-05 2021-06-01 新发药业有限公司 一种n-取代基哌啶-3-酮的制备方法
US20220002303A1 (en) 2018-11-14 2022-01-06 Ube Industries, Ltd. Dihydropyrrolopyrazole derivative
US20220089611A1 (en) * 2018-12-28 2022-03-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
EP4081527A4 (en) * 2019-12-24 2024-01-10 Dana Farber Cancer Inst Inc COMBINATION OF A CYCLIN-DEPENDENT KINASE-7 INHIBITOR AND IMMUNOTHERAPY FOR THE TREATMENT OF CANCER
JP2023523415A (ja) 2020-04-21 2023-06-05 リガンド・ファーマシューティカルズ・インコーポレイテッド ヌクレオチドプロドラッグ化合物
CN115073471B (zh) * 2021-03-11 2023-03-21 沈阳药科大学 吡唑并四氢吡咯类衍生物、其制备方法和在医药上的应用
CN113563346A (zh) * 2021-08-19 2021-10-29 守恒(厦门)医疗科技有限公司 吡咯[3,4-c]并吡唑二酰胺类衍生物及其在抗肿瘤药物中的应用
CN115057860B (zh) * 2022-05-20 2024-02-09 四川大学华西医院 一种erk抑制剂及其制药用途

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3423414A (en) * 1966-01-13 1969-01-21 Ciba Geigy Corp Pyrazolopyridines
US3526633A (en) * 1968-03-06 1970-09-01 American Cyanamid Co Substituted 2,4,5,6-tetrahydropyrrolo(3,4-c)pyrazoles
US3947467A (en) * 1973-08-02 1976-03-30 Eli Lilly And Company 3-(5-Nitro-2-imidazolyl) pyrazoles
JPS5163193A (ja) * 1974-11-26 1976-06-01 Yoshitomi Pharmaceutical Tetorahidoropirazoropirijinkagobutsuno seizoho
BR9406946A (pt) * 1993-07-06 1996-08-06 Pfizer Tetra-hidro-pirazolpiridinas bicíclicas
US5508300A (en) * 1994-01-14 1996-04-16 Pfizer Inc. Dihydro pyrazolopyrroles, compositions and use
HUT77517A (hu) * 1994-10-20 1998-05-28 Pfizer Inc. Biciklusos tetrahidro-pirazolo-piridin-származékok, alkalmazásuk és ilyen vegyületeket tartalmazó gyógyászati készítmények
US5593997A (en) * 1995-05-23 1997-01-14 Pfizer Inc. 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors
JPH11514361A (ja) * 1995-10-16 1999-12-07 藤沢薬品工業株式会社 H+−ATPaseとしての複素環式化合物
GB9608435D0 (en) * 1996-04-24 1996-06-26 Celltech Therapeutics Ltd Chemical compounds
TR200002617T2 (tr) 1997-12-22 2000-11-21 Bayer Corporation Aril ve heteroaril sübstitüentli heterosiklik üreler kullanılarak RAF kinazın inhibe edilmesi
HU229824B1 (en) * 2000-08-10 2014-08-28 Pfizer Italia Srl Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
UA81790C2 (ru) * 2002-12-19 2008-02-11 Фармация Италия С.П.А. Замещенные пиролопиразольные производные как ингибиторы киназы
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
WO2007068619A1 (en) * 2005-12-12 2007-06-21 Nerviano Medical Sciences S.R.L. Substituted pyrazolo [4,3-c] pyridine derivatives active as kinase inhibitors

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