SK1882003A3 - Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them - Google Patents

Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them Download PDF

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Publication number
SK1882003A3
SK1882003A3 SK188-2003A SK1882003A SK1882003A3 SK 1882003 A3 SK1882003 A3 SK 1882003A3 SK 1882003 A SK1882003 A SK 1882003A SK 1882003 A3 SK1882003 A3 SK 1882003A3
Authority
SK
Slovakia
Prior art keywords
pyrazol
dihydropyrrolo
tetrahydropyridine
acetyl
phenyl
Prior art date
Application number
SK188-2003A
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English (en)
Slovak (sk)
Inventor
Daniele Fancelli
Valeria Pittala
Mario Varasi
Original Assignee
Pharmacia Italia Spa
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=24549630&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=SK1882003(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pharmacia Italia Spa filed Critical Pharmacia Italia Spa
Publication of SK1882003A3 publication Critical patent/SK1882003A3/sk

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    • 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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
SK188-2003A 2000-08-10 2001-07-25 Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them SK1882003A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US63591400A 2000-08-10 2000-08-10
PCT/EP2001/008639 WO2002012242A2 (fr) 2000-08-10 2001-07-25 Bicyclo-pyrazoles actifs en tant qu'inhibiteurs de kinase, leur procede de preparation et compositions pharmaceutiques les contenant

Publications (1)

Publication Number Publication Date
SK1882003A3 true SK1882003A3 (en) 2003-06-03

Family

ID=24549630

Family Applications (1)

Application Number Title Priority Date Filing Date
SK188-2003A SK1882003A3 (en) 2000-08-10 2001-07-25 Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them

Country Status (29)

Country Link
US (3) US7541354B2 (fr)
EP (1) EP1320531B1 (fr)
JP (2) JP4555547B2 (fr)
KR (1) KR100904157B1 (fr)
CN (2) CN1447810A (fr)
AR (1) AR034137A1 (fr)
AT (1) ATE480539T1 (fr)
AU (2) AU2001287654B2 (fr)
BR (1) BR0113176A (fr)
CA (1) CA2416527C (fr)
CY (1) CY1110914T1 (fr)
CZ (1) CZ2003591A3 (fr)
DE (1) DE60143041D1 (fr)
DK (1) DK1320531T3 (fr)
EA (1) EA006381B1 (fr)
EE (1) EE05405B1 (fr)
ES (1) ES2349762T3 (fr)
HU (1) HU229824B1 (fr)
IL (2) IL153997A0 (fr)
MX (1) MXPA03001169A (fr)
MY (1) MY148632A (fr)
NO (1) NO325530B1 (fr)
NZ (1) NZ524475A (fr)
PE (1) PE20020274A1 (fr)
PL (1) PL213199B1 (fr)
PT (1) PT1320531E (fr)
SK (1) SK1882003A3 (fr)
WO (1) WO2002012242A2 (fr)
ZA (1) ZA200301813B (fr)

Families Citing this family (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2416527C (fr) * 2000-08-10 2009-12-22 Pharmacia Italia S.P.A. Bicyclo-pyrazoles actifs en tant qu'inhibiteurs de kinase, leur procede de preparation et compositions pharmaceutiques les contenant
US20030195192A1 (en) * 2002-04-05 2003-10-16 Fortuna Haviv Nicotinamides having antiangiogenic activity
AU2003234567A1 (en) 2002-05-15 2003-12-02 Janssen Pharmaceutica N.V. N-substituted tricyclic 3-aminopyrazoles as pdfg receptor inhibitors
WO2003097610A1 (fr) * 2002-05-17 2003-11-27 Pharmacia Italia S.P.A. Derives d'aminoindazole agissant comme inhibiteurs de kinase, methode d'obtention et compositions pharmaceutiques les renfermant
WO2004007504A1 (fr) * 2002-07-17 2004-01-22 Pharmacia Italia S.P.A. Derives de pyrazole heterobicycliques utilises comme inhibiteurs de kinase
MXPA05000945A (es) * 2002-07-25 2005-05-16 Pharmacia Italia Spa Biciclo-pirazoles activos como inhibidores de la cinasa, procedimientos para su preparacion y composiciones farmaceuticas que los contienen.
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
EP1530573B1 (fr) * 2002-07-25 2008-03-19 Pfizer Italia S.r.l. Inhibiteurs de kinases a base de derives de pyrazoles heterocycliques condenses
UA81790C2 (uk) * 2002-12-19 2008-02-11 Фармация Италия С.П.А. Заміщені піролопіразольні похідні як інгібітори кінази
BRPI0408486A (pt) * 2003-03-11 2006-04-04 Pharmacia Italia Spa derivados de biciclopirazol ativos como inibidores da cinase, processo para a sua preparação e composições farmacêuticas compreendendo-os
ES2436524T3 (es) 2003-05-22 2014-01-02 Nerviano Medical Sciences S.R.L. Derivados de pirazolo-quinazolina, procedimiento para su preparación y su uso como inhibidores de cinasas
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.
WO2005014572A1 (fr) * 2003-08-08 2005-02-17 Pharmacia Italia S.P.A. Derives de pyrimidylpyrrole pouvant etre utilises comme inhibiteurs de kinases
US20050043346A1 (en) * 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
WO2005030776A1 (fr) 2003-09-23 2005-04-07 Vertex Pharmaceuticals Incorporated Derives de pyrazolopyrrole utilises en tant qu'inhibiteurs de proteines kinases
US7592466B2 (en) 2003-10-09 2009-09-22 Abbott Laboratories Ureas having antiangiogenic activity
US7572914B2 (en) 2003-12-19 2009-08-11 Takeda Pharmaceutical Company Limited 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
WO2006023931A2 (fr) 2004-08-18 2006-03-02 Takeda San Diego, Inc. Inhibiteurs de kinase
EP1812439B2 (fr) 2004-10-15 2017-12-06 Takeda Pharmaceutical Company Limited Inhibiteurs de kinase
US20060089378A1 (en) * 2004-10-27 2006-04-27 Mingde Xia Tetrahydro-pyridinyl pyrazole cannabinoid modulators
US20060128710A1 (en) * 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
CA2593428C (fr) 2005-01-10 2012-04-17 Pfizer Inc. Pyrrolopyrazoles, puissants inhibiteurs de kinases
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
AU2006271781A1 (en) * 2005-07-15 2007-01-25 F. Hoffmann-La Roche Ag Novel heteroaryl fused cyclic amines
JP5303271B2 (ja) 2005-07-19 2013-10-02 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有用な１Ｈ−チエノ［２，３−ｃ］ピラゾール化合物
FR2889526B1 (fr) 2005-08-04 2012-02-17 Aventis Pharma Sa 7-aza-indazoles substitues, compositions les contenant, procede de fabrication et utilisation
WO2007023382A2 (fr) * 2005-08-25 2007-03-01 Pfizer Inc. Composes de pyrimidine amino pyrazole, puissants inhibiteurs de kinase
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
EA014906B1 (ru) * 2005-12-01 2011-02-28 Элан Фармасьютикалз, Инк. 5-(арилсульфонил)пиразолопиперидины
EP1968976A1 (fr) * 2005-12-12 2008-09-17 NERVIANO MEDICAL SCIENCES S.r.l. Derives de pyrazolo [4,3-c] pyridine substitues agissant comme inhibiteurs de kinase
WO2007068637A1 (fr) 2005-12-12 2007-06-21 Nerviano Medical Sciences S.R.L. Derives de pyrrolo-pyrazole substitues agissant comme inhibiteurs de kinase
US7618982B2 (en) 2005-12-19 2009-11-17 Nerviano Medical Sciences S.R.L. Heteroarylpyrrolopyridinones active as kinase inhibitors
MY151455A (en) * 2005-12-21 2014-05-30 Pfizer Prod Inc Carbonylamino pyrrolopyrazoles, potent kinase inhibitors
US7504513B2 (en) 2006-02-27 2009-03-17 Hoffman-La Roche Inc. Thiazolyl-benzimidazoles
EP1999131B1 (fr) 2006-03-03 2013-10-23 Nerviano Medical Sciences S.r.l. Bicyclopyrazoles actifs comme inhibiteurs de la kinase
WO2007099166A1 (fr) * 2006-03-03 2007-09-07 Nerviano Medical Sciences S.R.L. Dérives de pyrazolo-pyridine actifs en tant qu'inhibiteurs de la kinase
US20070213378A1 (en) * 2006-03-10 2007-09-13 Lymphosign Inc. Compounds for modulating cell proliferation, compositions and methods related thereto
WO2007146136A2 (fr) * 2006-06-12 2007-12-21 Merck & Co., Inc. Compositions ophtalmiques pour traiter une hypertension oculaire
WO2008017465A1 (fr) * 2006-08-10 2008-02-14 F. Hoffmann-La Roche Ag Dérivés de lactame bicycliques, leur fabrication et utilisation en tant qu'agents pharmaceutiques
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
JP5415271B2 (ja) * 2006-10-11 2014-02-12 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の置換ピロロ−ピラゾール誘導体
US8883790B2 (en) 2006-10-12 2014-11-11 Astex Therapeutics Limited Pharmaceutical combinations
US8916552B2 (en) 2006-10-12 2014-12-23 Astex Therapeutics Limited Pharmaceutical combinations
EA017937B1 (ru) 2007-02-07 2013-04-30 Пфайзер Инк. ПРОИЗВОДНЫЕ 3-АМИНОПИРРОЛО[3,4-c]ПИРАЗОЛ-5(1H,4H,6H)-КАРБАЛЬДЕГИДА В КАЧЕСТВЕ ИНГИБИТОРОВ РКС
EP2120933B1 (fr) 2007-02-27 2015-07-08 Nerviano Medical Sciences S.r.l. Isoquinolinopyrrolopyridinones actives utilisées comme inhibiteurs de kinase
CN101675052A (zh) * 2007-04-12 2010-03-17 辉瑞大药厂 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
EP2003129B1 (fr) 2007-06-11 2017-08-09 Nerviano Medical Sciences S.r.l. Dérivés de 1H-pyrido[3,4-B]indol-1-one et de 2,3,4,9-tétrahydro-1H-bêta-carbolin-1-one
EP2313097B1 (fr) 2008-07-24 2013-03-27 Nerviano Medical Sciences S.r.l. Combinaison thérapeutique renfermant un inhibiteur de la kinase aurora et des agents antiprolifératifs
CA2743904A1 (fr) 2008-11-17 2010-05-20 The Regents Of The University Of Michigan Compositions de vaccins contre le cancer et leurs methodes d'utilisation
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
EP2937345B1 (fr) 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Inhibiteurs de la kinase raf de type ii
WO2012020227A1 (fr) 2010-08-11 2012-02-16 Centro Nacional De Investigaciones Oncologicas (Cnio) Composés tricycliques destinés à être utilisés en tant qu'inhibiteurs de kinases
BR112013008527A2 (pt) 2010-12-17 2016-07-12 Nerviano Medical Sciences Srl derivados de pirazolo-quinazolina substituídos como inibidores de cinase
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
JP5978293B2 (ja) * 2011-05-04 2016-08-24 フォーマ ティーエム， エルエルシー． Ｎａｍｐｔを阻害するための新規な化合物および組成物
JP6106685B2 (ja) 2011-11-17 2017-04-05 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 Ｃ−ｊｕｎ−ｎ−末端キナーゼ（ｊｎｋ）の阻害剤
WO2013080141A1 (fr) 2011-11-29 2013-06-06 Novartis Ag Composés pyrazolopyrrolidine
UY34591A (es) 2012-01-26 2013-09-02 Novartis Ag Compuestos de imidazopirrolidinona
EP2855483B1 (fr) 2012-05-24 2017-10-25 Novartis AG Composés pyrrolopyrrolidinones
EP2909194A1 (fr) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibiteurs de cycline-dépendante kinase 7 (cdk7)
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
US9447137B2 (en) * 2012-11-07 2016-09-20 Nucorion Pharmaceuticals, Inc. Substituted gemcitabine aryl amide analogs
US9403827B2 (en) 2013-01-22 2016-08-02 Novartis Ag Substituted purinone compounds
WO2014115080A1 (fr) 2013-01-22 2014-07-31 Novartis Ag Composés pyrazolo[3,4-d]pyrimidinone utilisés en tant qu'inhibiteurs de l'interaction p53/mdm2
CN105209467B (zh) 2013-05-27 2018-06-08 诺华股份有限公司 咪唑并吡咯烷酮衍生物及其在治疗疾病中的用途
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
WO2014191911A1 (fr) 2013-05-28 2014-12-04 Novartis Ag Dérivés de pyrazolo-pyrrolidin-4-one et leur utilisation dans le traitement de maladie
AU2014272695B2 (en) 2013-05-28 2016-10-20 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives as BET inhibitors and their use in the treatment of disease
WO2015058126A1 (fr) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Composés hétéroaromatiques utiles dans le traitement de maladies prolifératives
AU2014337044A1 (en) 2013-10-18 2016-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
MX2016006667A (es) 2013-11-21 2016-07-26 Novartis Ag Derivados de pirrolo-pirrolona y su uso como inhibidores.
US9814716B2 (en) 2014-05-23 2017-11-14 Mingsight Pharmaceuticals, Inc. Treatment of autoimmune disease
US10131679B2 (en) 2014-10-31 2018-11-20 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)
WO2016109689A2 (fr) * 2014-12-30 2016-07-07 Novira Therapeutics, Inc. Dérivés et méthodes de traitement d'infections provoquées par le virus de l'hépatite b
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
CN107427521B (zh) 2015-03-27 2021-08-03 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
DK3302448T3 (da) 2015-06-04 2024-02-05 Aurigene Oncology Ltd Erstattede heterocyclylafledninger som cdk-inhibitore
CA2986441A1 (fr) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Therapie d'association utilisant des inhibiteurs de transcription et des inhibiteurs de kinases
AU2016281225B2 (en) 2015-06-15 2020-10-15 Ube Corporation Substituted dihydropyrrolopyrazole derivative
WO2017044858A2 (fr) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibiteurs de kinases cycline-dépendantes
TW201806956A (zh) 2016-06-29 2018-03-01 諾維拉治療公司 二氮呯酮衍生物及治療ｂ型肝炎感染之方法
CA3029566A1 (fr) 2016-06-29 2018-01-04 Novira Therapeutics, Inc. Derives de diazepinone et leur utilisation dans le traitement des infections par l'hepatite b
EP4059934B1 (fr) 2016-09-09 2026-07-29 Novartis AG Composés et compositions en tant qu'inhibiteurs de récepteurs de type toll endosomal
UA125824C2 (uk) 2016-10-24 2022-06-15 Астразенека Аб 6,7,8,9-ТЕТРАГІДРО-3H-ПІРАЗОЛО[4,3-f]ІЗОХІНОЛІНОВІ ПОХІДНІ, ЗАСТОСОВНІ В ЛІКУВАННІ РАКУ
CR20190379A (es) 2017-01-30 2019-10-21 Astrazeneca Ab Moduladores del receptor de estrógeno
JP7141129B2 (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５－５融合環
KR102638253B1 (ko) 2017-05-31 2024-02-16 케모센트릭스, 인크. C5a 억제제로서의 6-5 융합 고리
US10435429B2 (en) 2017-10-03 2019-10-08 Nucorion Pharmaceuticals, Inc. 5-fluorouridine monophosphate cyclic triester compounds
WO2019072942A1 (fr) 2017-10-11 2019-04-18 F. Hoffmann-La Roche Ag Composés bicycliques destinés à être utilisés en tant qu'inhibiteurs de la kinase rip1
MX2020004838A (es) * 2017-11-02 2020-10-16 Aicuris Gmbh & Co Kg Nuevas indol-2-carboxamidas sustituidas con pirazolopiperidina, de alta actividad, activas contra el virus de la hepatitis b (vhb).
MX2020006459A (es) 2017-12-22 2020-11-06 Chemocentryx Inc Compuestos de anillos fusionados 6,5 diaril sustituidos como inhibidores de c5ar.
MA51327A (fr) 2017-12-22 2021-05-26 Chemocentryx Inc Composés cycliques fusionnés en 5,5 à substitution diaryle, utilisés en tant qu'inhibiteurs du c5ar
AU2019207626B2 (en) 2018-01-10 2023-10-05 Nucorion Pharmaceuticals, Inc. Phosphor(n)amidatacetal and phosph(on)atalcetal compounds
US11427550B2 (en) 2018-01-19 2022-08-30 Nucorion Pharmaceuticals, Inc. 5-fluorouracil compounds
ES2993034T3 (en) 2018-04-02 2024-12-20 Chemocentryx Inc Prodrugs of fused-bicyclic c5ar antagonists
EP3810132A4 (fr) 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. Inhibiteurs de kinase de la famille taire et utilisations correspondantes
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
JP7530297B2 (ja) 2018-11-14 2024-08-07 Ｕｂｅ株式会社 ジヒドロピロロピラゾール誘導体
CN113164477A (zh) 2018-12-14 2021-07-23 达纳-法伯癌症研究所股份有限公司 C-jun-n-末端激酶的吡唑并吡啶抑制剂及其用途
EP3902542A4 (fr) * 2018-12-28 2022-09-07 Dana-Farber Cancer Institute, Inc. Inhibiteurs de la kinase dépendante des cyclines 7 et leurs utilisations
JP7675658B2 (ja) * 2019-04-30 2025-05-13 ヴァロ ヘルス インコーポレイテッド Ｕｓｐ３６の阻害
WO2021011692A1 (fr) 2019-07-17 2021-01-21 Nucorion Pharmaceuticals, Inc. Composés désoxyribonucléotidiques cycliques
CN114174281B (zh) 2019-08-05 2025-02-07 达纳-法伯癌症研究公司 细胞周期蛋白依赖性激酶7(cdk7)的降解剂及其用途
CA3166135A1 (fr) * 2019-12-24 2021-07-01 Dana-Farber Cancer Institute, Inc. Association d'un inhibiteur de kinase 7 dependante de cyclines et d'une immunotherapie pour le traitement du cancer
EP4143199B1 (fr) 2020-04-21 2025-11-19 Ligand Pharmaceuticals, Inc. Composés de promédicaments nucléotidiques
WO2021216431A1 (fr) 2020-04-21 2021-10-28 Ligand Pharmaceuticals, Inc. Composés de benzyloxy phosph(on)ate
PE20221838A1 (es) 2020-04-24 2022-11-29 Astrazeneca Ab Formulaciones farmaceuticas
US20210330653A1 (en) 2020-04-24 2021-10-28 Astrazeneca Ab Dosage Regimen for the Treatment of Cancer
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
CN1048015C (zh) * 1993-07-06 2000-01-05 美国辉瑞有限公司 双环四氢吡唑并吡啶类化合物
US5508300A (en) * 1994-01-14 1996-04-16 Pfizer Inc. Dihydro pyrazolopyrroles, compositions and use
PL319758A1 (en) * 1994-10-20 1997-08-18 Pfizer Bicyclic tetrahydropyrasole pyridines and their application as medicines
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
EP0876345B1 (fr) * 1995-10-16 2004-08-18 Fujisawa Pharmaceutical Co., Ltd. Composes heterocycliques tels que des h+-atpases
GB9608435D0 (en) * 1996-04-24 1996-06-26 Celltech Therapeutics Ltd Chemical compounds
NZ505845A (en) * 1997-12-22 2003-10-31 Bayer Ag Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
CA2416527C (fr) * 2000-08-10 2009-12-22 Pharmacia Italia S.P.A. Bicyclo-pyrazoles actifs en tant qu'inhibiteurs de kinase, leur procede de preparation et compositions pharmaceutiques les contenant
UA81790C2 (uk) * 2002-12-19 2008-02-11 Фармация Италия С.П.А. Заміщені піролопіразольні похідні як інгібітори кінази
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
EP1968976A1 (fr) * 2005-12-12 2008-09-17 NERVIANO MEDICAL SCIENCES S.r.l. Derives de pyrazolo [4,3-c] pyridine substitues agissant comme inhibiteurs de kinase

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