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

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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

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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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Virology (AREA)
  • Vascular Medicine (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) 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 (117)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100904157B1 (ko) * 2000-08-10 2009-06-23 파마시아 이탈리아 에스.피.에이. 키나제 억제제로서 활성인 비사이클로-피라졸, 이의제조방법 및 이를 포함하는 약제학적 조성물
US20030195192A1 (en) * 2002-04-05 2003-10-16 Fortuna Haviv Nicotinamides having antiangiogenic activity
DE60326950D1 (de) 2002-05-15 2009-05-14 Janssen Pharmaceutica Nv N-substituierte tricyclische 3-aminopyrazole als pdgf rezeptorenhemmer
EP1506176B1 (fr) * 2002-05-17 2013-04-24 Pfizer Italia S.r.l. Derives d'aminoindazole agissant comme inhibiteurs de kinase, methode d'obtention et compositions pharmaceutiques les renfermant
JP2006501191A (ja) * 2002-07-17 2006-01-12 ファルマシア・イタリア・エス・ピー・エー キナーゼ阻害剤としてのヘテロ二環式ピラゾール誘導体
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
AU2003244649A1 (en) * 2002-07-25 2004-02-23 Pharmacia Italia Spa Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
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
CA2518395A1 (fr) * 2003-03-11 2004-09-23 Pharmacia Italia S.P.A. Derives de bicyclo-pyrazol ayant une action inhibitrice contre la kinase, procedes de preparation de ceux-ci et compositions pharmaceutiques les contenant
US7482354B2 (en) 2003-05-22 2009-01-27 Nerviano Medical Sciences S.R.L. Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
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
DE602004014163D1 (de) * 2003-08-08 2008-07-10 Pfizer Italia Srl Pyrimidylpyrrolderivate, die als kinaseinhibitoren wirken
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
WO2005063241A1 (fr) * 2003-12-26 2005-07-14 Ono Pharmaceutical Co., Ltd. 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
WO2006023931A2 (fr) 2004-08-18 2006-03-02 Takeda San Diego, Inc. Inhibiteurs de kinase
US7713973B2 (en) 2004-10-15 2010-05-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
ES2357776T3 (es) * 2004-10-27 2011-04-29 Janssen Pharmaceutica Nv Moduladores de cannabionoides de tetrahidro piridinil pirazol.
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
PE20061119A1 (es) * 2005-01-19 2006-11-27 Aventis Pharma Sa PIRAZOLO PIRIDINAS SUSTITUIDAS COMO INHIBIDORES DE CINASAS FAK, KDR Y Tie
FR2880891B1 (fr) * 2005-01-19 2007-02-23 Aventis Pharma Sa Pyrazolo pyridines substituees, compositions les contenant, procede de fabrication et utilisation
WO2007009883A1 (fr) * 2005-07-15 2007-01-25 F. Hoffmann-La Roche Ag Nouvelles amines cycliques fusionnés avec hétéroaryle
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 (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
AU2006320423B2 (en) * 2005-12-01 2012-06-21 Elan Pharmaceuticals, Inc. 5-(arylsulfonyl)-pyrazolopiperidines
JP5222731B2 (ja) * 2005-12-12 2013-06-26 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 キナーゼ阻害薬として活性な置換ピロロ−ピラゾール誘導体
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
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
ES2442491T3 (es) 2006-03-03 2014-02-11 Nerviano Medical Sciences S.R.L. Biciclopirazoles activos como inhibidores de cinasa
WO2007106391A1 (fr) * 2006-03-10 2007-09-20 Lymphosign Inc. Composés permettant de moduler la prolifération cellulaire, compositions et procédés les utilisant
AU2007258527A1 (en) * 2006-06-12 2007-12-21 Merck Sharp & Dohme Corp. 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
GEP20135728B (en) 2006-10-09 2013-01-25 Takeda Pharmaceuticals Co Kinase inhibitors
EP2089394B1 (fr) 2006-10-11 2011-06-29 Nerviano Medical Sciences S.r.l. Derives de pyrrolopyrazole substitues en tant qu'inhibiteurs de kinases
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
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
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
WO2008104475A1 (fr) 2007-02-27 2008-09-04 Nerviano Medical Sciences S.R.L. Isoquinolinopyrrolopyridinones actives utilisées comme inhibiteurs de kinase
CA2683695C (fr) 2007-04-12 2013-06-18 Pfizer Inc. Nouveaux derives de 3-amido-pyrrolo[3,4-c]pyrazole-5(1h,4h.6h) carbaldehyde
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
WO2010009985A2 (fr) 2008-07-24 2010-01-28 Nerviano Medical Sciences S.R.L. Combinaison thérapeutique renfermant un inhibiteur de la kinase aurora et des agents antiprolifératifs
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
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 (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
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
AR082888A1 (es) 2011-05-04 2013-01-16 Forma Therapeutics Inc Compuestos de piridina para la inhibicion de nampt
CA2856291C (fr) 2011-11-17 2020-08-11 Dana-Farber Cancer Institute, Inc. Inhibiteurs de la kinase c-jun-n-terminale (jnk)
WO2013080141A1 (fr) 2011-11-29 2013-06-06 Novartis Ag Composés pyrazolopyrrolidine
US8815926B2 (en) 2012-01-26 2014-08-26 Novartis Ag Substituted pyrrolo[3,4-D]imidazoles for the treatment of MDM2/4 mediated diseases
CN104321325B (zh) 2012-05-24 2016-11-16 诺华股份有限公司 吡咯并吡咯烷酮化合物
EP2909194A1 (fr) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibiteurs de cycline-dépendante 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
WO2014115077A1 (fr) 2013-01-22 2014-07-31 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
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
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
AU2014337122B2 (en) 2013-10-18 2019-01-03 Dana-Farber Cancer Institute, 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)
US9550796B2 (en) 2013-11-21 2017-01-24 Novartis Ag Pyrrolopyrrolone derivatives and their use as BET inhibitors
EP3145931B1 (fr) 2014-05-23 2021-03-31 Mingsight Pharmaceuticals, Inc. Traitement d'une maladie auto-immune
CA2966164C (fr) 2014-10-31 2023-10-17 Ube Industries, Ltd. Compose de dihydropyrrolopyrazole substitue
EP3236959B1 (fr) 2014-12-23 2025-09-24 Dana-Farber Cancer Institute, Inc. Inhibiteurs de la kinase cycline-dépendante 7 (cdk7)
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
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
EP3302448B1 (fr) * 2015-06-04 2023-10-25 Aurigene Oncology Limited Dérivés hétérocyclyle substitués en tant qu'inhibiteurs de cdk
US10702527B2 (en) 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
EP3309163A4 (fr) 2015-06-15 2019-01-09 UBE Industries, Ltd. Dérivé de dihydropyrrolopyrazole substitué
EP4019515A1 (fr) 2015-09-09 2022-06-29 Dana-Farber Cancer Institute, Inc. Inhibiteurs de kinases cycline-dépendantes
ES2817426T3 (es) 2016-06-29 2021-04-07 Novira Therapeutics Inc Derivados de oxadiazepinona y su uso en el tratamiento de infecciones por hepatitis B
MA45550A (fr) 2016-06-29 2019-05-08 Novira Therapeutics Inc Dérivés de diazépinone et leur utilisation dans le traitement des infections par l'hépatite b
CN115215886B (zh) 2016-09-09 2024-10-11 诺华股份有限公司 作为内体Toll样受体抑制剂的化合物及组合物
LT3640251T (lt) 2016-10-24 2022-03-10 Astrazeneca Ab 6,7,8,9-tetrahidro-3h-pirazolo[4,3-f]izochinolino dariniai, tinkami vėžio gydymui
MX2019008438A (es) 2017-01-30 2019-10-30 Astrazeneca Ab Moduladores del receptor de estrogeno.
ES2934507T3 (es) 2017-05-31 2023-02-22 Chemocentryx Inc Anillos fusionados en 5-5 como inhibidores 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
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
CN111527087A (zh) * 2017-11-02 2020-08-11 艾库里斯有限及两合公司 具有抗乙型肝炎病毒(hbv)活性的新的高活性的吡唑并-哌啶取代的吲哚-2-甲酰胺
MX2020006460A (es) * 2017-12-22 2020-11-06 Chemocentryx Inc Compuestos de anillo 5,5 fusionado sustituido con diarilo como inhibidores de c5ar.
US10828285B2 (en) 2017-12-22 2020-11-10 Chemocentryx, Inc. Diaryl substituted 6,5-fused ring compounds as C5aR inhibitors
KR102708995B1 (ko) 2018-01-10 2024-09-23 누코리온 파마슈티컬스, 인코포레이티드. 포스포르(포스포론)아미다타세탈 및 포스프(온)아탈세탈 화합물
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
JP7590185B2 (ja) 2018-06-25 2024-11-26 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 Taireファミリーキナーゼインヒビターおよびそれらの使用
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
AU2019413694B2 (en) * 2018-12-28 2025-03-20 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
WO2020223548A1 (fr) * 2019-04-30 2020-11-05 Integral Early Discovery, Inc. Inhibition de usp36
AU2020315394A1 (en) 2019-07-17 2022-02-17 Nucorion Pharmaceuticals, Inc. Cyclic deoxyribonucleotide compounds
JP7636388B2 (ja) * 2019-08-05 2025-02-26 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)の分解誘導剤およびその使用
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
EP4143199B1 (fr) 2020-04-21 2025-11-19 Ligand Pharmaceuticals, Inc. Composés de promédicaments nucléotidiques
CN115768778A (zh) 2020-04-21 2023-03-07 配体药物公司 苄氧基磷酸(膦酸)酯化合物
JP7719796B2 (ja) 2020-04-24 2025-08-06 アストラゼネカ・アクチエボラーグ 医薬製剤
IL297216A (en) 2020-04-24 2022-12-01 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
HUT74170A (en) * 1993-07-06 1996-11-28 Pfizer Bicyclic tetrahydro pyrazolopyridines
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
DE69633196D1 (de) * 1995-10-16 2004-09-23 Fujisawa Pharmaceutical Co Heterocyclische verbindungen als h+-atpasen
GB9608435D0 (en) * 1996-04-24 1996-06-26 Celltech Therapeutics Ltd Chemical compounds
DE69834842T2 (de) * 1997-12-22 2007-05-10 Bayer Pharmaceuticals Corp., West Haven Hemmung von raf-kinase unter verwendung von aryl- und heteroarylsubstituierten heterocyclischen harnstoffen
KR100904157B1 (ko) * 2000-08-10 2009-06-23 파마시아 이탈리아 에스.피.에이. 키나제 억제제로서 활성인 비사이클로-피라졸, 이의제조방법 및 이를 포함하는 약제학적 조성물
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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