EE05405B1 - Kinaasi inhibiitoritena toimivad bitskloprasoolid, nende valmistamismeetod, kasutamine ja neid sisaldavad farmatseutilised kompositsioonid - Google Patents

Kinaasi inhibiitoritena toimivad bitskloprasoolid, nende valmistamismeetod, kasutamine ja neid sisaldavad farmatseutilised kompositsioonid

Info

Publication number
EE05405B1
EE05405B1 EEP200300054A EEP200300054A EE05405B1 EE 05405 B1 EE05405 B1 EE 05405B1 EE P200300054 A EEP200300054 A EE P200300054A EE P200300054 A EEP200300054 A EE P200300054A EE 05405 B1 EE05405 B1 EE 05405B1
Authority
EE
Estonia
Prior art keywords
clopazoles
bit
acting
preparation
pharmaceutical compositions
Prior art date
Application number
EEP200300054A
Other languages
English (en)
Estonian (et)
Inventor
Fancelli Daniele
Pittal� Valeria
Varasi Mario
Original Assignee
Pharmacia Italia S.P.A.
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
Family has litigation
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=EE05405(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pharmacia Italia S.P.A. filed Critical Pharmacia Italia S.P.A.
Publication of EE200300054A publication Critical patent/EE200300054A/xx
Publication of EE05405B1 publication Critical patent/EE05405B1/xx

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Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/28—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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00—Libraries per se, e.g. arrays, mixtures
EEP200300054A 2000-08-10 2001-07-25 Kinaasi inhibiitoritena toimivad bitskloprasoolid, nende valmistamismeetod, kasutamine ja neid sisaldavad farmatseutilised kompositsioonid EE05405B1 (et)

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
EE200300054A EE200300054A (et) 2004-12-15
EE05405B1 true EE05405B1 (et) 2011-04-15

Family

ID=24549630

Family Applications (1)

Application Number Title Priority Date Filing Date
EEP200300054A EE05405B1 (et) 2000-08-10 2001-07-25 Kinaasi inhibiitoritena toimivad bitskloprasoolid, nende valmistamismeetod, kasutamine ja neid sisaldavad farmatseutilised kompositsioonid

Country Status (29)

Country Link
US (3) US7541354B2 (ru)
EP (1) EP1320531B1 (ru)
JP (2) JP4555547B2 (ru)
KR (1) KR100904157B1 (ru)
CN (2) CN1447810A (ru)
AR (1) AR034137A1 (ru)
AT (1) ATE480539T1 (ru)
AU (2) AU8765401A (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
NZ524475A (en) * 2000-08-10 2004-11-26 Pharmacia Italia S 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
MY138268A (en) 2002-05-15 2009-05-29 Janssen Pharmaceutica Nv N-substituted tricyclic 3-aminopyrazoles as inhibitors for the treatment of cell proliferative disorders
CA2486101C (en) * 2002-05-17 2009-07-07 Pharmacia Italia S.P.A. Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
MXPA05000629A (es) * 2002-07-17 2005-04-25 Pharmacia Italia Spa Derivados de pirazol heterobiciclico como inhibidores de cinasa.
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
MXPA05000947A (es) * 2002-07-25 2005-05-16 Pharmacia Italia Spa Biciclo-pirazoles activos como inhibidores de cinasa, procedimiento para su preparacion y composiciones farmaceuticas que los contienen.
WO2004013146A1 (en) * 2002-07-25 2004-02-12 Pharmacia Italia S.P.A Condensed heterocyclic pyrazole derivatives as kinase inhibitors
UA81790C2 (ru) * 2002-12-19 2008-02-11 Фармация Италия С.П.А. Замещенные пиролопиразольные производные как ингибиторы киназы
US20070037790A1 (en) * 2003-03-11 2007-02-15 Francesca Abrate Bicyclo-pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
ME00142B (me) 2003-05-22 2010-10-10 Nerviano Medical Sciences Srl Derivati pirazolo-hinazolina, postupci za njihovo dobijanje i njihova upotreba kao inhibitora kinaze
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.
US20050043346A1 (en) * 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
MXPA06001556A (es) * 2003-08-08 2006-05-15 Pharmacia Italia Spa Derivados activos de pirimidilpirrol como inhibidores de la cinasa.
AU2004276341B2 (en) * 2003-09-23 2011-04-14 Vertex Pharmaceuticals Incorporated Pyrazolopyrrole derivatives as protein kinase inhibitors
US7592466B2 (en) 2003-10-09 2009-09-22 Abbott Laboratories Ureas having antiangiogenic activity
WO2005061519A1 (en) 2003-12-19 2005-07-07 Takeda San Diego, Inc. Kinase inhibitors
JPWO2005063241A1 (ja) * 2003-12-26 2007-07-19 小野薬品工業株式会社 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
US7550598B2 (en) 2004-08-18 2009-06-23 Takeda Pharmaceutical Company Limited Kinase inhibitors
US7713973B2 (en) 2004-10-15 2010-05-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
ATE495742T1 (de) * 2004-10-27 2011-02-15 Janssen Pharmaceutica Nv Tetrahydro pyridinyl pyrazole cannabinoid modulatoren
US20060128710A1 (en) * 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
AU2005323797B2 (en) * 2005-01-10 2009-07-09 Pfizer Inc. Pyrrolopyrazoles, potent kinase inhibitors
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
WO2007009898A1 (en) 2005-07-19 2007-01-25 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
TW200736255A (en) * 2005-12-01 2007-10-01 Elan Pharm Inc 5-(Substituted)-pyrazolopiperidines
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
US7968583B2 (en) 2005-12-12 2011-06-28 Nerviano Medical Sciences S.R.L. Substituted pyrrolo-pyrazole derivatives active as kinase inhibitors
US7618982B2 (en) 2005-12-19 2009-11-17 Nerviano Medical Sciences S.R.L. Heteroarylpyrrolopyridinones active as kinase inhibitors
PT1979356E (pt) * 2005-12-21 2013-11-21 Pfizer Prod Inc Carbonilaminopirrolopirazolos, inibidores potentes de cinase
US7504513B2 (en) 2006-02-27 2009-03-17 Hoffman-La Roche Inc. Thiazolyl-benzimidazoles
WO2007099166A1 (en) * 2006-03-03 2007-09-07 Nerviano Medical Sciences S.R.L. Pyrazolo-pyridine derivatives active as kinase inhibitors
ES2442491T3 (es) * 2006-03-03 2014-02-11 Nerviano Medical Sciences S.R.L. Biciclopirazoles activos como inhibidores de cinasa
US20070213378A1 (en) * 2006-03-10 2007-09-13 Lymphosign Inc. Compounds for modulating cell proliferation, compositions and methods related thereto
WO2007146136A2 (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
JP2010505962A (ja) 2006-10-09 2010-02-25 武田薬品工業株式会社 キナーゼ阻害剤
WO2008043745A1 (en) * 2006-10-11 2008-04-17 Nerviano Medical Sciences S.R.L. Substituted pyrrolo-pyrazole derivatives as kinase inhibitors
EP2073807A1 (en) 2006-10-12 2009-07-01 Astex Therapeutics Limited Pharmaceutical combinations
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
CA2677572C (en) * 2007-02-07 2012-12-18 Pfizer Inc. 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
AU2008237660B2 (en) 2007-04-12 2011-12-22 Pfizer Inc. 3-amido-pyrrolo [3, 4-C] pyrazole-5 (1H, 4H, 6H) carbaldehyde derivatives as inhibitors of protein kinase C
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
WO2010009985A2 (en) 2008-07-24 2010-01-28 Nerviano Medical Sciences S.R.L. Therapeutic combination comprising an aurora kinase inhibitor and antiproliferative agents
US9974844B2 (en) * 2008-11-17 2018-05-22 The Regents Of The University Of Michigan Cancer vaccine compositions and methods of using the same
JP2012512223A (ja) 2008-12-18 2012-05-31 エフ．ホフマン−ラ ロシュ アーゲー チアゾリル−ベンズイミダゾール類
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
US9180127B2 (en) 2009-12-29 2015-11-10 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
RU2652638C2 (ru) 2010-12-17 2018-04-28 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Замещенные пиразолхиназолиновые производные в качестве ингибиторов киназы
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
KR20140027366A (ko) 2011-05-04 2014-03-06 포르마 티엠, 엘엘씨. Nampt의 억제를 위한 신규 화합물 및 조성물
EP3569598A1 (en) 2011-11-17 2019-11-20 Dana Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
JP5992054B2 (ja) 2011-11-29 2016-09-14 ノバルティス アーゲー ピラゾロピロリジン化合物
UY34591A (es) 2012-01-26 2013-09-02 Novartis Ag Compuestos de imidazopirrolidinona
US9365576B2 (en) 2012-05-24 2016-06-14 Novartis Ag Pyrrolopyrrolidinone compounds
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
CA2890359A1 (en) * 2012-11-07 2014-05-15 Zucai SUO Substituted gemcitabine aryl amide analogs and treatment methods using same
EP2948453B1 (en) 2013-01-22 2017-08-02 Novartis AG Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the p53/mdm2 interaction
EP2948451B1 (en) 2013-01-22 2017-07-12 Novartis AG Substituted purinone compounds
WO2014191894A1 (en) 2013-05-27 2014-12-04 Novartis Ag Imidazopyrrolidinone derivatives and their use in the treatment of disease
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
AU2014272700B2 (en) 2013-05-28 2016-12-01 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives and their use in the treatment of disease
EA028175B1 (ru) 2013-05-28 2017-10-31 Новартис Аг Производные пиразолопирролидин-4-она в качестве ингибиторов вет и их применение при лечении заболевания
ES2676734T3 (es) 2013-10-18 2018-07-24 Syros Pharmaceuticals, Inc. Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas
AU2014337044A1 (en) 2013-10-18 2016-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
KR20160086930A (ko) 2013-11-21 2016-07-20 노파르티스 아게 피롤로피롤론 유도체 및 bet 억제제로서의 그의 용도
JP2017516853A (ja) 2014-05-23 2017-06-22 ミングサイト ファーマシューティカルズ，インク． 自己免疫性疾患の処置
CN107074887B (zh) 2014-10-31 2020-12-22 宇部兴产株式会社 取代二氢吡咯并吡唑化合物
JP6854762B2 (ja) * 2014-12-23 2021-04-07 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド サイクリン依存性キナーゼ７（ｃｄｋ７）の阻害剤
RU2742305C2 (ru) 2014-12-30 2021-02-04 Новира Терапьютикс, Инк. Производные и способы лечения инфекций гепатита в
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
JP6861166B2 (ja) 2015-03-27 2021-04-21 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド サイクリン依存性キナーゼの阻害剤
LT3302448T (lt) * 2015-06-04 2024-02-12 Aurigene Oncology Limited Pakeisti heterociklilo dariniai kaip cdk inhibitoriai
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
RU2765718C1 (ru) * 2015-06-15 2022-02-02 Убе Индастриз, Лтд. Замещенное производное дигидропирролопиразола
CA2996978A1 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
EP3478692B1 (en) 2016-06-29 2020-06-17 Novira Therapeutics Inc. Oxadiazepinone derivatives and their use in the treatment of hepatitis b infections
WO2018005883A1 (en) 2016-06-29 2018-01-04 Novira Therapeutics, Inc. Diazepinone derivatives and their use in the treatment of hepatitis b infections
WO2018047081A1 (en) 2016-09-09 2018-03-15 Novartis Ag Compounds and compositions as inhibitors of endosomal toll-like receptors
MX2019004685A (es) 2016-10-24 2019-08-21 Astrazeneca Ab Derivados de 6,7,8,9-tetrahidro-3h-pirazolo[4,3f] isoquinolina utiles en el tratamiento del cancer.
MX2019008438A (es) 2017-01-30 2019-10-30 Astrazeneca Ab Moduladores del receptor de estrogeno.
WO2018222601A1 (en) 2017-05-31 2018-12-06 Chemocentryx, Inc. 5-5 FUSED RINGS AS C5a INHIBITORS
WO2018222598A1 (en) 2017-05-31 2018-12-06 Chemocentryx, Inc. 6-5 FUSED RINGS AS C5a INHIBITORS
US10435429B2 (en) 2017-10-03 2019-10-08 Nucorion Pharmaceuticals, Inc. 5-fluorouridine monophosphate cyclic triester compounds
WO2019072942A1 (en) 2017-10-11 2019-04-18 F. Hoffmann-La Roche Ag BICYCLIC COMPOUNDS FOR USE AS INHIBITORS OF KINASE RIP1
SG11202003746UA (en) * 2017-11-02 2020-05-28 Aicuris Gmbh & Co Kg Novel, highly active pyrazolo-piperidine substituted indole-2-carboxamides active against the hepatitis b virus (hbv)
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
EP3728203B1 (en) * 2017-12-22 2024-03-13 ChemoCentryx, Inc. DIARYL SUBSTITUTED 6,5-FUSED RING COMPOUNDS AS C5aR INHIBITORS
US11427550B2 (en) 2018-01-19 2022-08-30 Nucorion Pharmaceuticals, Inc. 5-fluorouracil compounds
EP3773563A4 (en) 2018-04-02 2021-12-29 ChemoCentryx, Inc. Prodrugs of fused-bicyclic c5ar antagonists
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
WO2020100944A1 (ja) 2018-11-14 2020-05-22 宇部興産株式会社 ジヒドロピロロピラゾール誘導体
AU2019413694A1 (en) * 2018-12-28 2021-06-10 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
WO2021133601A1 (en) * 2019-12-24 2021-07-01 Dana-Farber Cancer Institute, Inc. The combination of cyclin dependent kinase 7 inhibitor and immunotherapy for treatment of cancer
WO2021216427A1 (en) 2020-04-21 2021-10-28 Ligand Pharmaceuticals, Inc. Nucleotide prodrug compounds
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
CA2166721C (en) * 1993-07-06 1999-07-27 Allen Jacob Duplantier Bicyclic tetrahydro pyrazolopyridines
US5508300A (en) * 1994-01-14 1996-04-16 Pfizer Inc. Dihydro pyrazolopyrroles, compositions and use
NZ292991A (en) * 1994-10-20 1999-02-25 Pfizer Bicyclic tetrahydropyrazolopyridines that are selective inhibitors of phosphodiesterase (pde) type iv or the production of tnf and pharmaceutical compositions containing them
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
US6008230A (en) * 1995-10-16 1999-12-28 Fujisawa Pharmaceutical Co., Ltd. Quinoline compounds as H+ -ATPases
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
NZ524475A (en) * 2000-08-10 2004-11-26 Pharmacia Italia S 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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