[go: up one dir, main page]

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)
  • 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)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Virology (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 (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 (xx)
EP (1) EP1320531B1 (xx)
JP (2) JP4555547B2 (xx)
KR (1) KR100904157B1 (xx)
CN (2) CN1447810A (xx)
AR (1) AR034137A1 (xx)
AT (1) ATE480539T1 (xx)
AU (2) AU2001287654B2 (xx)
BR (1) BR0113176A (xx)
CA (1) CA2416527C (xx)
CY (1) CY1110914T1 (xx)
CZ (1) CZ2003591A3 (xx)
DE (1) DE60143041D1 (xx)
DK (1) DK1320531T3 (xx)
EA (1) EA006381B1 (xx)
EE (1) EE05405B1 (xx)
ES (1) ES2349762T3 (xx)
HU (1) HU229824B1 (xx)
IL (2) IL153997A0 (xx)
MX (1) MXPA03001169A (xx)
MY (1) MY148632A (xx)
NO (1) NO325530B1 (xx)
NZ (1) NZ524475A (xx)
PE (1) PE20020274A1 (xx)
PL (1) PL213199B1 (xx)
PT (1) PT1320531E (xx)
SK (1) SK1882003A3 (xx)
WO (1) WO2002012242A2 (xx)
ZA (1) ZA200301813B (xx)

Families Citing this family (116)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60143041D1 (de) * 2000-08-10 2010-10-21 Pfizer Italia Srl Bizyklische pyrazole wirksam als kinase inhibitoren, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische zubereitungen
US20030195192A1 (en) * 2002-04-05 2003-10-16 Fortuna Haviv Nicotinamides having antiangiogenic activity
MXPA04011320A (es) 2002-05-15 2005-08-16 Johnson & Johnson 3-aminopirazoles triciclicos n-sustituidos como inhibidores del receptor del factor de crecimiento derivado de plaquetas.
JP4751063B2 (ja) * 2002-05-17 2011-08-17 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活性のアミノインダゾール誘導体、それらの調製方法、及びそれらを含む薬学的組成物
MXPA05000629A (es) * 2002-07-17 2005-04-25 Pharmacia Italia Spa Derivados de pirazol heterobiciclico como inhibidores de cinasa.
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
US20060135508A1 (en) * 2002-07-25 2006-06-22 Manuela Villa Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
WO2004013146A1 (en) * 2002-07-25 2004-02-12 Pharmacia Italia S.P.A Condensed heterocyclic pyrazole derivatives as kinase inhibitors
UA81790C2 (uk) 2002-12-19 2008-02-11 Фармация Италия С.П.А. Заміщені піролопіразольні похідні як інгібітори кінази
EP1608364A1 (en) * 2003-03-11 2005-12-28 Pharmacia Italia S.p.A. 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
BRPI0413438A (pt) * 2003-08-08 2006-10-17 Pharmacia Italia Spa derivados de pirimidilpirrol ativos como inibidores de cinase
JP2007506787A (ja) * 2003-09-23 2007-03-22 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼインヒビターとしてのピラゾロピロール誘導体
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
EP1698335A4 (en) * 2003-12-26 2007-08-01 Ono Pharmaceutical Co AGENT FOR PREVENTING AND / OR TREATING DISEASES INVOLVING A MITOCHONDRIAL BENZODIAZEPINE RECEPTOR
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
ATE479687T1 (de) 2004-10-15 2010-09-15 Takeda Pharmaceutical Kinaseinhibitoren
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
WO2006072831A1 (en) 2005-01-10 2006-07-13 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
BRPI0613045A2 (pt) * 2005-07-15 2010-12-14 Hoffmann La Roche aminas cÍclicas fundidas a heteroarila
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
US7968583B2 (en) 2005-12-12 2011-06-28 Nerviano Medical Sciences S.R.L. Substituted pyrrolo-pyrazole derivatives active as kinase inhibitors
EP1968976A1 (en) * 2005-12-12 2008-09-17 NERVIANO MEDICAL SCIENCES S.r.l. Substituted pyrazolo [4,3-c] pyridine derivatives active as kinase inhibitors
US7618982B2 (en) 2005-12-19 2009-11-17 Nerviano Medical Sciences S.R.L. Heteroarylpyrrolopyridinones active as kinase inhibitors
DK1979356T3 (da) * 2005-12-21 2013-11-18 Pfizer Prod Inc Carbonylaminopyrrolopyrazoler, kraftige kinaseinhibitorer
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
JP5250432B2 (ja) * 2006-03-03 2013-07-31 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として活性なビシクロピラゾール
WO2007106391A1 (en) * 2006-03-10 2007-09-20 Lymphosign Inc. Compounds for modulating cell proliferation, compositions and methods related thereto
AU2007258527A1 (en) * 2006-06-12 2007-12-21 Merck Sharp & Dohme Corp. 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
GEP20135728B (en) 2006-10-09 2013-01-25 Takeda Pharmaceuticals Co Kinase inhibitors
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
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
AP2009004958A0 (en) 2007-02-07 2009-08-31 Pfizer 3-amino-pyrrolo [3,4-C] pyrazole - 5 (1H, 4H, 6H) carbaldehyde derivatives as PKC inhibitors
US8293762B2 (en) 2007-02-27 2012-10-23 Nerviano Medical Sciences S.R.L. Isoquinolinopyrrolopyridinones active as kinase inhibitors
US8114871B2 (en) * 2007-04-12 2012-02-14 Pfizer Inc. 3-amido-pyrrolo[3,4-C]pyrazole-5(1H,4H,6H) carbaldehyde derivatives
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
ES2415907T3 (es) 2008-07-24 2013-07-29 Nerviano Medical Sciences S.R.L. Combinación terapéutica que comprende un inhibidor de cinasas aurora y agentes antiproliferativos
CA2743904A1 (en) 2008-11-17 2010-05-20 The Regents Of The University Of Michigan Cancer vaccine compositions and methods of using the same
CA2745596A1 (en) 2008-12-18 2010-10-28 F. Hoffmann-La Roche Ag Thiazolyl-benzimidazoles
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
EP2937345B1 (en) 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
WO2012020227A1 (en) 2010-08-11 2012-02-16 Centro Nacional De Investigaciones Oncologicas (Cnio) Tricyclic compounds for use as kinase inhibitors
WO2012080990A1 (en) 2010-12-17 2012-06-21 Nerviano Medical Sciences S.R.L. Substituted pyrazolo-quinazoline derivatives as kinase inhibitors
CN102134243A (zh) * 2011-03-04 2011-07-27 中国医学科学院医药生物技术研究所 具有抗肿瘤活性的双环氨基吡唑类衍生物
US8771682B2 (en) 2011-04-26 2014-07-08 Technische Universtität Dresden Methods and compositions for reducing interleukin-4 or interleukin-13 signaling
CN103717574B (zh) * 2011-05-04 2017-02-22 福马Tm有限责任公司 用于抑制nampt的新化合物和组合物
EP3569598A1 (en) 2011-11-17 2019-11-20 Dana Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
WO2013080141A1 (en) 2011-11-29 2013-06-06 Novartis Ag Pyrazolopyrrolidine compounds
US8815926B2 (en) 2012-01-26 2014-08-26 Novartis Ag Substituted pyrrolo[3,4-D]imidazoles for the treatment of MDM2/4 mediated diseases
WO2013175417A1 (en) 2012-05-24 2013-11-28 Novartis Ag Pyrrolopyrrolidinone compounds
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent 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
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 (en) 2013-01-22 2014-07-31 Novartis Ag Substituted purinone compounds
WO2014115080A1 (en) 2013-01-22 2014-07-31 Novartis Ag Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the p53/mdm2 interaction
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
CA2912986A1 (en) 2013-05-28 2014-12-04 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease
PL3004112T3 (pl) 2013-05-28 2018-02-28 Novartis Ag Pochodne pirazolo-pirolidyn-4-onu oraz ich zastosowanie w leczeniu choroby
ES2676734T3 (es) 2013-10-18 2018-07-24 Syros Pharmaceuticals, Inc. Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
AU2014351413B2 (en) 2013-11-21 2017-06-01 Novartis Ag Pyrrolopyrrolone derivatives and their use as BET inhibitors
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
AU2015371251B2 (en) * 2014-12-23 2020-06-11 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
WO2016109684A2 (en) * 2014-12-30 2016-07-07 Novira Therapeutics, Inc. Derivatives and methods of treating hepatitis b infections
CN104530045A (zh) * 2015-01-14 2015-04-22 中国药科大学 吡唑并[4,3-c]四氢吡啶类c-Met激酶抑制剂及其制备方法和用途
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
AU2016272908B2 (en) 2015-06-04 2021-05-06 Aurigene Oncology Limited Substituted heterocyclyl derivatives as CDK inhibitors
US10702527B2 (en) 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
EP3309163A4 (en) 2015-06-15 2019-01-09 UBE Industries, Ltd. SUBSTITUTED DIHYDROPYRROLO PYRAZOL DERIVATIVE
CA2996978A1 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
EP3478683B1 (en) 2016-06-29 2021-07-21 Novira Therapeutics Inc. Diazepinone derivatives and their use in the treatment of hepatitis b infections
WO2018005881A1 (en) 2016-06-29 2018-01-04 Novira Therapeutics, Inc. Oxadiazepinone derivatives and their use in the treatment of hepatitis b infections
CA3031585A1 (en) 2016-09-09 2018-03-15 Novartis Ag Compounds and compositions as inhibitors of endosomal toll-like receptors
JOP20190090B1 (ar) 2016-10-24 2023-03-28 Astrazeneca Ab مشتقات 9،8،7،6-رابع هيدرو-3h-بيرازولو [4،3-f]أيزوكينولين مفيدة في علاج السرطان
SI3494116T1 (sl) 2017-01-30 2020-02-28 Astrazeneca Ab Modulatorji receptorja estrogena
WO2018222598A1 (en) 2017-05-31 2018-12-06 Chemocentryx, Inc. 6-5 FUSED RINGS AS C5a INHIBITORS
MA48800A (fr) 2017-05-31 2020-04-08 Chemocentryx Inc Cycles 5-5 fusionnés utilisés en tant qu'inhibiteurs de c5a
US10435429B2 (en) 2017-10-03 2019-10-08 Nucorion Pharmaceuticals, Inc. 5-fluorouridine monophosphate cyclic triester compounds
MX2020003439A (es) 2017-10-11 2020-07-29 Hoffmann La Roche Compuestos biciclicos para usarse como inhibidores de cinasa de la proteina 1 de interaccion con receptores (rip1).
KR20200083552A (ko) * 2017-11-02 2020-07-08 아이쿠리스 게엠베하 운트 코. 카게 B형 간염 바이러스 (hbv)에 활성인 신규 고활성 피라졸로-피페리딘 치환된 인돌-2-카르복스아미드
AU2018388657C1 (en) 2017-12-22 2023-03-23 Chemocentryx, Inc. Diaryl substituted 5,5-fused ring compounds as C5aR inhibitors
SG11202005791QA (en) * 2017-12-22 2020-07-29 Chemocentryx Inc DIARYL SUBSTITUTED 6,5-FUSED RING COMPOUNDS AS C5aR INHIBITORS
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
AR114464A1 (es) 2018-04-02 2020-09-09 Chemocentryx Inc PROFÁRMACOS DE ANTAGONISTAS DE C5aR BICÍCLICOS FUSIONADOS
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 (en) 2018-11-14 2023-11-22 UBE Corporation Dihydropyrrolopyrazole derivative
AU2019413694B2 (en) * 2018-12-28 2025-03-20 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
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
CA3143349A1 (en) 2019-07-17 2021-01-21 Nucorion Pharmaceuticals, Inc. Cyclic deoxyribonucleotide compounds
EP4010336B1 (en) * 2019-08-05 2025-04-02 Dana-Farber Cancer Institute, Inc. Degraders of cyclin-dependent kinase 7 (cdk7) and uses thereof
EP4081527A4 (en) * 2019-12-24 2024-01-10 Dana-Farber Cancer Institute, Inc. COMBINATION OF A CYCLIN-DEPENDENT KINASE-7 INHIBITOR AND IMMUNOTHERAPY FOR THE TREATMENT OF CANCER
CN115605492B (zh) 2020-04-21 2025-09-16 配体制药股份有限公司 核苷酸前药化合物
EP4138787A1 (en) 2020-04-24 2023-03-01 Astrazeneca AB Pharmaceutical formulations
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
EP0707585A1 (en) * 1993-07-06 1996-04-24 Pfizer Inc. 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
ID26328A (id) 1997-12-22 2000-12-14 Bayer Ag Penghambat raf kinase menggunakan urea heterosiklik tersubstitusi aril dan heteroaril
DE60143041D1 (de) * 2000-08-10 2010-10-21 Pfizer Italia Srl Bizyklische pyrazole wirksam als kinase inhibitoren, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische zubereitungen
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 (en) * 2005-12-12 2008-09-17 NERVIANO MEDICAL SCIENCES S.r.l. Substituted pyrazolo [4,3-c] pyridine derivatives active as kinase inhibitors

Also Published As

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

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
EE200200409A (et) 1,3-dihüdro-2H-indool-2-ooni derivaadid, nende valmistamismeetod ja neid sisaldavad farmatseutilised kompositsioonid
HUP0300565A3 (en) 8-quinolinxanthine and 8-isoquinolinxanthine derivatives as pde 5 inhibitors, their use, process for their preparation and pharmaceutical compositions containing them
HUP0300434A3 (en) Oxazole derivatives and their uses as tyrosine kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
HUP0200355A2 (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
NO20032733L (no) Difenylazetidinonderivater, fremgangsmåte for deres fremstilling, legemidler som inneholder disse forbindelsene og deres anvendelse
EE200100484A (et) Bitsüklilised heterotsüklilised ühendid, neid ühendeid sisaldavad farmatseutilised kompositsioonid,ja nende valmistamise meetodid
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
EE200300254A (et) Heterotsüklilised ühendid, millel on antibakteriaalne toime, nende valmistamismeetod ja neid sisaldavad farmatseutilised kompositsioonid
NO20042805L (no) Nye forbindelser og deres anvendelse innen medisin, fremgangsmate for deres fremstilling og farmaoytiske sammensetninger som inneholder dem
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
NO20026154D0 (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