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=google_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

Links

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
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 (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 (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 (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) AU8765401A (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 (111)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1320531E (pt) * 2000-08-10 2010-10-27 Pfizer Italia Srl Biciclo-pirazoles activos como inibidores da cinase, processo para a sua preparação e composições farmacêuticas compreendendo estes
US20030195192A1 (en) * 2002-04-05 2003-10-16 Fortuna Haviv Nicotinamides having antiangiogenic activity
BRPI0311179A2 (pt) 2002-05-15 2016-06-21 Janssen Pharmaceutica Nv 3-aminopirazóis tricíclicos n-substituídos como inibidores de receptor de pdfg
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.
CA2492673A1 (fr) * 2002-07-17 2004-01-22 Pharmacia Italia S.P.A. Derives de pyrazole heterobicycliques utilises comme inhibiteurs de kinase
WO2004013144A1 (fr) * 2002-07-25 2004-02-12 Pharmacia Italia Spa Bicyclo-pyrazoles actifs inhibiteurs de kinase, procede de preparation et compositions pharmaceutiques contenant ceux-ci
BR0312924A (pt) * 2002-07-25 2005-07-12 Pharmacia Italia Spa Biciclo-pirazóis ativos como inibidores de quinase, processo para sua preparação e composições farmacêuticas compreendendo os mesmos
JP4533138B2 (ja) * 2002-07-25 2010-09-01 ファイザー イタリア ソシエタ ア レスポンサビリタ リミタータ キナーゼ阻害剤としての縮環ヘテロ環式ピラゾール誘導体
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
GEP20094664B (en) 2003-05-22 2009-04-10 Nerviano Medical Sciences Srl Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
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
BRPI0413438A (pt) * 2003-08-08 2006-10-17 Pharmacia Italia Spa derivados de pirimidilpirrol ativos como inibidores de cinase
CA2539549A1 (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
WO2005061519A1 (fr) 2003-12-19 2005-07-07 Takeda San Diego, Inc. Inhibiteurs de kinase
EP1698335A4 (fr) * 2003-12-26 2007-08-01 Ono Pharmaceutical Co Agent pour prevenir et/ou de traiter des maladies faisant intervenir un recepteur de benzodiazepine mitochondrial
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
EP1812439B2 (fr) 2004-10-15 2017-12-06 Takeda Pharmaceutical Company Limited Inhibiteurs de kinase
KR20070074638A (ko) * 2004-10-27 2007-07-12 얀센 파마슈티카 엔.브이. 테트라하이드로 피리디닐 피라졸 카나비노이드 모듈레이터
US20060128710A1 (en) * 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
SI1838718T1 (sl) * 2005-01-10 2011-08-31 Pfizer Pirolopirazoli, zmogljivi inhibitorji kinaze
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
JP2009501187A (ja) * 2005-07-15 2009-01-15 エフ.ホフマン−ラ ロシュ アーゲー 新規なヘテロアリール縮合環式アミン
WO2007009898A1 (fr) 2005-07-19 2007-01-25 Nerviano Medical Sciences S.R.L. Composes 1h-thieno[2,3-c]pyrazole servant d'inhibiteurs de kinase
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
TW200736255A (en) * 2005-12-01 2007-10-01 Elan Pharm Inc 5-(Substituted)-pyrazolopiperidines
WO2007068637A1 (fr) * 2005-12-12 2007-06-21 Nerviano Medical Sciences S.R.L. Derives de pyrrolo-pyrazole substitues agissant comme inhibiteurs de kinase
WO2007068619A1 (fr) 2005-12-12 2007-06-21 Nerviano Medical Sciences S.R.L. Derives de pyrazolo[4,3-c]pyridine 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
MEP0808A (xx) * 2005-12-21 2010-02-10 Pfizer Prod Inc Karbonilamino pirolopirayoli, snažni inhibitori kinaza
US7504513B2 (en) 2006-02-27 2009-03-17 Hoffman-La Roche Inc. Thiazolyl-benzimidazoles
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
WO2007099171A2 (fr) 2006-03-03 2007-09-07 Nerviano Medical Sciences S.R.L. Bicyclopyrazoles actifs comme inhibiteurs de la kinase
US20070213378A1 (en) * 2006-03-10 2007-09-13 Lymphosign Inc. Compounds for modulating cell proliferation, compositions and methods related thereto
US20090281154A1 (en) * 2006-06-12 2009-11-12 Doherty James B Ophthalmic Compositions for Treating Ocular Hypertension
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
EA200970361A1 (ru) 2006-10-09 2010-02-26 Такеда Фармасьютикал Компани Лимитед Ингибиторы киназы
WO2008043745A1 (fr) * 2006-10-11 2008-04-17 Nerviano Medical Sciences S.R.L. Dérivés de pyrrolopyrazole substitués en tant qu'inhibiteurs de kinases
JP5528806B2 (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
EP2073807A1 (fr) 2006-10-12 2009-07-01 Astex Therapeutics Limited Combinaisons pharmaceutiques
JP5161245B2 (ja) * 2007-02-07 2013-03-13 ファイザー・インク PKC阻害剤としての3−アミノ−ピロロ[3,4−c]ピラゾール−5(1H,4H,6H)カルボアルデヒド誘導体
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
JP5683462B2 (ja) 2008-07-24 2015-03-11 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 オーロラキナーゼ阻害剤および抗増殖剤を含む治療用組み合わせ
WO2010057197A1 (fr) 2008-11-17 2010-05-20 The Regents Of The University Of Michigan Compositions de vaccins contre le cancer et leurs méthodes d’utilisation
EP2379543A2 (fr) 2008-12-18 2011-10-26 F. Hoffmann-La Roche AG Thiazolyl-benzimidazoles
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
AU2010343102B2 (en) 2009-12-29 2016-03-24 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
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
EP2614065B1 (fr) 2010-12-17 2017-04-19 Nerviano Medical Sciences S.r.l. Dérivés de pyrazolo-quinazoline substitués à titre d'inhibiteurs de kinases
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
BR112013028281A2 (pt) 2011-05-04 2017-01-10 Forma Tm Llc compostos e composições para inibição de nampt
AU2012340200B2 (en) 2011-11-17 2017-10-12 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
WO2013175417A1 (fr) 2012-05-24 2013-11-28 Novartis Ag Composés pyrrolopyrrolidinones
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
WO2014063061A1 (fr) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Petites molécules marquées de façon hydrophobe en tant qu'inducteurs de la dégradation de protéine
US9447137B2 (en) * 2012-11-07 2016-09-20 Nucorion Pharmaceuticals, Inc. Substituted gemcitabine aryl amide analogs
EP2948451B1 (fr) 2013-01-22 2017-07-12 Novartis AG Composés de purinone substitués
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
KR20160012194A (ko) 2013-05-27 2016-02-02 노파르티스 아게 이미다조피롤리디논 유도체 및 질환의 치료에서의 그의 용도
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
CA2912991A1 (fr) 2013-05-28 2014-12-04 Novartis Ag Derives de pyrazolo-pyrrolidin-4-one et leur utilisation dans le traitement de maladie
EP3004108B1 (fr) 2013-05-28 2017-10-18 Novartis AG Dérivés de pyrazolo-pyrrolidin-4-one comme des inhibiteurs de bet et leur utilisation dans le traitement d'une maladie
CA2927917C (fr) 2013-10-18 2022-08-09 Syros Pharmaceuticals, Inc. Composes heteroaromatiques utiles pour le traitement des maladies proliferatives
US10047070B2 (en) 2013-10-18 2018-08-14 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
CA2931249A1 (fr) 2013-11-21 2015-05-28 Novartis Ag Derives de pyrrolopyrrolone et leur utilisation en tant qu'inhibiteurs de proteines bet
AU2015263884B2 (en) 2014-05-23 2019-11-14 Mingsight Pharmaceuticals, Inc. Treatment of autoimmune disease
JP6690543B2 (ja) 2014-10-31 2020-04-28 宇部興産株式会社 置換ジヒドロピロロピラゾール化合物
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
WO2016109684A2 (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
EP3273966B1 (fr) 2015-03-27 2023-05-03 Dana-Farber Cancer Institute, Inc. Inhibiteurs de kinases cycline-dépendantes
CA2987552A1 (fr) * 2015-06-04 2016-12-08 Aurigene Discovery Technologies Limited Derives heterocyclyle substitues en tant qu'inhibiteurs de cdk
EP3307728A4 (fr) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. Thérapie d'association utilisant des inhibiteurs de transcription et des inhibiteurs de kinases
JP6787314B2 (ja) * 2015-06-15 2020-11-18 宇部興産株式会社 置換ジヒドロピロロピラゾール誘導体
JP7028766B2 (ja) 2015-09-09 2022-03-02 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
US10987359B2 (en) 2016-06-29 2021-04-27 Novira Therapeutics, Inc. Oxadiazepinone derivatives and methods of treating hepatitis B infections
US10975077B2 (en) 2016-06-29 2021-04-13 Novira Therapeutics, Inc. Diazepinone derivatives and their use in the treatment of hepatitis B infections
US10954233B2 (en) 2016-09-09 2021-03-23 Novartis Ag Compounds and compositions as inhibitors of endosomal toll-like receptors
SI3640251T1 (sl) 2016-10-24 2022-04-29 Astrazeneca Ab Derivati 6,7,8,9-tetrahidro-3H-pirazolo(4,3-f)izokinolina uporabni v zdravljenju raka
JOP20190183B1 (ar) 2017-01-30 2022-09-15 Astrazeneca Ab معدِلات مستقبلات الاستروجين
CN111032658B (zh) 2017-05-31 2022-12-20 凯莫森特里克斯股份有限公司 作为C5a抑制剂的5-5稠合环类
CN110997674B (zh) 2017-05-31 2022-12-20 凯莫森特里克斯股份有限公司 作为C5a抑制剂的6-5稠合环类
US10435429B2 (en) 2017-10-03 2019-10-08 Nucorion Pharmaceuticals, Inc. 5-fluorouridine monophosphate cyclic triester compounds
CN111201229B (zh) 2017-10-11 2024-08-23 豪夫迈·罗氏有限公司 用作rip1激酶抑制剂的二环化合物
US11236087B2 (en) * 2017-11-02 2022-02-01 Aicuris Gmbh & Co. Kg Highly active pyrazolo-piperidine substituted indole-2-carboxamides active against the hepatitis B virus (HBV)
CA3085946A1 (fr) 2017-12-22 2019-06-27 Chemocentryx, Inc. Composes cycliques condenses 6,5 a substitution diaryle, utilises en tant qu'inhibiteurs du c5ar
IL275516B2 (en) * 2017-12-22 2023-12-01 Chemocentryx Inc Ring compounds fused at the 5- and 6-position are diaryl-converted as C5AR inhibitors
US12110308B2 (en) 2018-01-10 2024-10-08 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
SG11202009588PA (en) 2018-04-02 2020-10-29 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
EP3885347B1 (fr) 2018-11-14 2023-11-22 UBE Corporation Dérivé de dihydropyrrolopyrazole
JP2022517740A (ja) * 2018-12-28 2022-03-10 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のインヒビターおよびそれらの使用
US12110311B2 (en) 2019-07-17 2024-10-08 Nucorion Pharmaceuticals, Inc. Cyclic deoxyribonucleotide compounds
AU2020414418A1 (en) * 2019-12-24 2022-07-21 Dana-Farber Cancer Institute, Inc. The combination of cyclin dependent kinase 7 inhibitor and immunotherapy for 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
RU2131876C1 (ru) * 1993-07-06 1999-06-20 Пфайзер Инк. Бициклические тетрагидропиразолпиридины или их фармацевтически приемлемые соли, фармацевтическая композиция, способ ингибирования фосфодиэстеразы, способ лечения
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
WO1997014681A1 (fr) * 1995-10-16 1997-04-24 Fujisawa Pharmaceutical Co., Ltd. Composes heterocycliques tels que des h+-atpases
GB9608435D0 (en) * 1996-04-24 1996-06-26 Celltech Therapeutics Ltd Chemical compounds
ES2155045T3 (es) * 1997-12-22 2007-02-01 Bayer Pharmaceuticals Corp. Inhibicion de la quinasa raf utilizando ureas heterociclicas sustituidas con arilo y heteroarilo.
PT1320531E (pt) * 2000-08-10 2010-10-27 Pfizer Italia Srl Biciclo-pirazoles activos como inibidores da cinase, processo para a sua preparação e composições farmacêuticas compreendendo estes
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
WO2007068619A1 (fr) * 2005-12-12 2007-06-21 Nerviano Medical Sciences S.R.L. Derives de pyrazolo[4,3-c]pyridine substitues agissant comme inhibiteurs de kinase

Also Published As

Publication number Publication date
CN102060857A (zh) 2011-05-18
WO2002012242A2 (fr) 2002-02-14
HUP0300741A2 (hu) 2003-11-28
IL153997A (en) 2014-01-30
EA006381B1 (ru) 2005-12-29
US20030171357A1 (en) 2003-09-11
DE60143041D1 (de) 2010-10-21
ZA200301813B (en) 2004-06-22
US20090221632A1 (en) 2009-09-03
CA2416527A1 (fr) 2002-02-14
AU2001287654B2 (en) 2006-12-14
IL153997A0 (en) 2003-07-31
KR20030027008A (ko) 2003-04-03
PL360663A1 (en) 2004-09-20
HU229824B1 (en) 2014-08-28
CZ2003591A3 (cs) 2003-06-18
EP1320531B1 (fr) 2010-09-08
PL213199B1 (pl) 2013-01-31
JP5185243B2 (ja) 2013-04-17
AR034137A1 (es) 2004-02-04
EA200300248A1 (ru) 2003-08-28
AU8765401A (en) 2002-02-18
EE200300054A (et) 2004-12-15
CA2416527C (fr) 2009-12-22
HUP0300741A3 (en) 2005-12-28
US8273765B2 (en) 2012-09-25
NO325530B1 (no) 2008-06-09
ES2349762T3 (es) 2011-01-11
CY1110914T1 (el) 2014-02-12
EP1320531A2 (fr) 2003-06-25
NZ524475A (en) 2004-11-26
MXPA03001169A (es) 2003-06-30
MY148632A (en) 2013-05-15
JP2010111677A (ja) 2010-05-20
PE20020274A1 (es) 2002-03-31
US7531531B2 (en) 2009-05-12
NO20030381L (no) 2003-02-24
PT1320531E (pt) 2010-10-27
BR0113176A (pt) 2003-06-17
US7541354B2 (en) 2009-06-02
SK1882003A3 (en) 2003-06-03
KR100904157B1 (ko) 2009-06-23
ATE480539T1 (de) 2010-09-15
WO2002012242A3 (fr) 2002-06-06
JP2004505977A (ja) 2004-02-26
DK1320531T3 (da) 2011-01-03
NO20030381D0 (no) 2003-01-24
JP4555547B2 (ja) 2010-10-06
US20070191386A1 (en) 2007-08-16
CN1447810A (zh) 2003-10-08

Similar Documents

Publication Publication Date Title
EE05405B1 (et) Kinaasi inhibiitoritena toimivad bitskloprasoolid, nende valmistamismeetod, kasutamine ja neid sisaldavad farmatseutilised kompositsioonid
EE200300259A (et) Mandelhappe derivaadid, nende valmistamise meetod, nende kasutamine trombiini inhibiitoritena ja neid sisaldavad ravimkoostised
EE05081B1 (et) Farmatseutilised kompositsioonid, mis sisaldavad 3-aminoasetidiini derivaate, 3-aminoasetidiini derivaadid ja nende valmistamise meetodid
HUP0301117A3 (en) Imidazole derivatives kinase inhibitors, their use, process for their preparation and pharmaceutical compositions containing them
HUP0204083A3 (en) 2-amino-nicotinamide derivatives and their use as vegf-receptor tyrosine kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
NO20024175L (no) Azetidinderivater, deres fremstilling og farmasöytiske preparater inneholdende forbindelsene
HUP0400908A3 (en) Pyrazole compounds useful as protein kinase inhibitors, their use and pharmaceutical compositions containing them
HUP0400194A3 (en) Imidazolidindion derivatives as metalloproteinase inhibitors, their use and pharmaceutical compositions containing them
EE04779B1 (et) 1,3-dihüdro-2H-indool-2-ooni derivaadid, nende valmistamismeetod ja neid sisaldavad farmatseutilised kompositsioonid
HUP0300434A3 (en) Oxazole derivatives and their uses as tyrosine kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
HUP0200355A3 (en) 4-aminopyrrolopyrimidines as kinase inhibitors, pharmaceutical compositions containing them and their use
EE200300475A (et) Türosiini kinaasi inhibiitorid, neid sisaldavad ravimkoostised ja nimetatud ühendid kasutamiseks haiguste ravis
EE200100484A (et) Bitsüklilised heterotsüklilised ühendid, neid ühendeid sisaldavad farmatseutilised kompositsioonid,ja nende valmistamise meetodid
NO20032733L (no) Difenylazetidinonderivater, fremgangsmåte for deres fremstilling, legemidler som inneholder disse forbindelsene og deres anvendelse
IL192937A0 (en) Pharmaceutical compositions containing beta-lapachone or derivatives or analogs thereof, and methods of using same
EE200300207A (et) Heterotsüklüülalküülpiperidiini derivaadid, nendevalmistamismeetodid ja farmatseutiline kompositsioon
HUP0400193A3 (en) Imidazolindion derivatives as metalloproteinase inhibitors, their use and pharmaceutical compositions containing them
NO20042805L (no) Nye forbindelser og deres anvendelse innen medisin, fremgangsmate for deres fremstilling og farmaoytiske sammensetninger som inneholder dem
EE200300254A (et) Heterotsüklilised ühendid, millel on antibakteriaalne toime, nende valmistamismeetod ja neid sisaldavad farmatseutilised kompositsioonid
DK1322158T3 (da) Farmaceutiske præparater med langvarig frigivelse, som indeholder metformin, og fremgangsmåde til fremstilling deraf
HUP0401499A3 (en) Indole derivatives as cox ii inhibitors, process for their preparation and pharmaceutical compositions containing them
HUP0204354A3 (en) Novel heterocyclic derivatives, preparation method and pharmaceutical compositions containing same and their use
AU2001277285A1 (en) Pyrazole-thiazole compounds, pharmaceutical compositions containing them, and methods of their use for inhibiting cyclin-dependent kinases
NO20026154L (no) Nye substituerte ftalider, fremgangsmåte for deres fremstilling og farmasöytiske sammensetninger inneholdende dem
EE05304B1 (et) Aminokinoliini derivaadid, meetod nende valmistamiseks, neid sisaldavad ravimkoostised ja nende kasutamine adenosiini A3-retseptori ligandidena

Legal Events

Date Code Title Description
GB1A Change in the ownership or in the address of the owner
MM4A Lapsed by not paying the annual fees

Effective date: 20140725