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AR040580A1 - Derivados de pirazol heterobiciclico como inhibidores de la quinasa - Google Patents

Derivados de pirazol heterobiciclico como inhibidores de la quinasa

Info

Publication number
AR040580A1
AR040580A1 AR20030102551A ARP030102551A AR040580A1 AR 040580 A1 AR040580 A1 AR 040580A1 AR 20030102551 A AR20030102551 A AR 20030102551A AR P030102551 A ARP030102551 A AR P030102551A AR 040580 A1 AR040580 A1 AR 040580A1
Authority
AR
Argentina
Prior art keywords
group selected
heterobiciclic
aryl
compounds
optionally substituted
Prior art date
Application number
AR20030102551A
Other languages
English (en)
Inventor
Roberto Tonani
Simona Bindi
Daniele Fancelli
Valeria Pittala
Anello Matteo D
Original Assignee
Pharmacia Italia Spa
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
Application filed by Pharmacia Italia Spa filed Critical Pharmacia Italia Spa
Publication of AR040580A1 publication Critical patent/AR040580A1/es

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/42—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms with nitro or nitroso radicals directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

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

Abstract

Derivados de pirazol heterobicíclico como inhibidores de la quinasa, un procedimiento para su preparación y composiciones farmacéuticas que los comprenden; los compuestos de la presente pueden ser útiles en terapéutica, en el tratamiento de enfermedades asociadas con una actividad desregulada de la proteína quinasa, como por ejemplo el cáncer. Y una biblioteca combinatoria de compuestos. Reivindicación 1: Un compuesto de biciclo-pirazol de fórmula (1) caracterizado porque: X es un grupo seleccionado entre NR´ , O, S, SO, o SO2; cada uno de R y R1, siendo iguales o diferentes, es seleccionado independientemente entre H o un grupo opcionalmente sustituido seleccionado entre -R´, -COR´, COOR´, -CONHR´,-CONR´R", -SO2R´, -SO2NHR´ o -SO2NR´R"; en donde cada uno de R´y R", siendo iguales o diferentes, es seleccionado independientemente entre H o un grupo alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heterociclilo o arilo-alquilo C1-6, recto o ramificado, sustituido además opcionalmente; R2 es un grupo opcionalmente sustituido seleccionado entre -R´, -CH2OR´ y OR´, en donde R´ es como se definió más arriba; y las sales farmacéuticamente aceptables del mismo.
AR20030102551A 2002-07-17 2003-07-16 Derivados de pirazol heterobiciclico como inhibidores de la quinasa AR040580A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US39617402P 2002-07-17 2002-07-17

Publications (1)

Publication Number Publication Date
AR040580A1 true AR040580A1 (es) 2005-04-13

Family

ID=30115981

Family Applications (1)

Application Number Title Priority Date Filing Date
AR20030102551A AR040580A1 (es) 2002-07-17 2003-07-16 Derivados de pirazol heterobiciclico como inhibidores de la quinasa

Country Status (12)

Country Link
EP (1) EP1534716B1 (es)
JP (1) JP2006501191A (es)
AR (1) AR040580A1 (es)
AT (1) ATE393159T1 (es)
AU (1) AU2003254337A1 (es)
BR (1) BR0312722A (es)
CA (1) CA2492673A1 (es)
DE (1) DE60320560T2 (es)
ES (1) ES2304531T3 (es)
MX (1) MXPA05000629A (es)
TW (1) TWI284645B (es)
WO (1) WO2004007504A1 (es)

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TW200526204A (en) * 2004-02-03 2005-08-16 Pharmacia Italia Spa 1h-thieno[2,3-c]pyrazole derivatives useful as kinase inhibitors
DE602005023333D1 (de) 2004-10-15 2010-10-14 Takeda Pharmaceutical Kinaseinhibitoren
FR2878442B1 (fr) 2004-11-29 2008-10-24 Aventis Pharma Sa THIENO(2,3-c)PYRAZOLES SUBSTITUES, PROCEDE DE PREPARATION, COMPOSITIONS LES CONTENANT ET UTILISATION
FR2882751B1 (fr) 2005-03-04 2007-09-14 Aventis Pharma Sa Hydrazinocarbonyl-thieno[2,3-c]pyrazoles, procede de preparation, compositions les contenant et utilisation
ES2439918T3 (es) 2005-07-19 2014-01-27 Nerviano Medical Sciences S.R.L. Compuestos de 1H-tieno[2,3-c]-pirazol útiles como inhibidores de cinasas
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
JP2009534307A (ja) * 2006-03-30 2009-09-24 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 特定の耐性腫瘍の治療のためのキナーゼ阻害剤の使用
BRPI0710510A2 (pt) 2006-04-19 2011-08-16 Novartis Ag compostos indazol e processos para inibição de cdc7
US8119641B2 (en) 2006-05-31 2012-02-21 Nerviano Medical Sciences S.R.L. 1H-furo[3,2-C]pyrazole compounds useful as kinase inhibitors
SG158147A1 (en) 2006-10-09 2010-01-29 Takeda Pharmaceutical Kinase inhibitors
EP3162798B1 (en) 2007-09-28 2021-04-14 Takeda Pharmaceutical Company Limited 5-membered heterocyclic compound
EP2058315A1 (en) 2007-10-30 2009-05-13 Nerviano Medical Sciences S.r.l. 1H-Furo[3,2-C]Pyrazoles active as aurora kinase inhibitors
CA2830148C (en) 2011-03-31 2020-07-28 Sbi Biotech Co., Ltd. Novel furanone derivatives
MX2014010953A (es) 2012-03-16 2014-10-13 Hoffmann La Roche Metodos para tratamiento de melanoma con inhibidores pak1.
WO2015008234A1 (en) * 2013-07-17 2015-01-22 Glenmark Pharmaceuticals S.A. Bicyclic heterocyclic compounds as ror gamma modulators
US9974795B2 (en) 2014-01-31 2018-05-22 Carna Biosciences, Inc. Anticancer agent composition
WO2017144546A1 (en) 2016-02-23 2017-08-31 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of nasopharyngeal carcinoma
WO2019024809A1 (zh) * 2017-08-01 2019-02-07 正大天晴药业集团股份有限公司 作为RORγ抑制剂的双环化合物
US20220220480A1 (en) 2019-04-17 2022-07-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for treatment of nlrp3 inflammasome mediated il-1beta dependent disorders
WO2021118924A2 (en) 2019-12-12 2021-06-17 Ting Therapeutics Llc Compositions and methods for the prevention and treatment of hearing loss
WO2021198511A1 (en) 2020-04-03 2021-10-07 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for treatment of sars-cov-2 infection
WO2022008597A1 (en) 2020-07-08 2022-01-13 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical composition for the treatment of infectious diseases
CN113072562B (zh) * 2021-04-06 2022-01-14 山东大学 一种GSK-3β抑制剂及其制备方法与应用
WO2024261302A1 (en) 2023-06-22 2024-12-26 Institut National de la Santé et de la Recherche Médicale Nlrp3 inhibitors, pak1/2 inhibitors and/or caspase 1 inhibitors for use in the treatment of rac2 monogenic disorders

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US4140785A (en) * 1978-05-08 1979-02-20 E. I. Du Pont De Nemours And Company N-(benzothienopyrazol)amide antirhinoviral agents
US4420476A (en) * 1982-05-24 1983-12-13 Averst McKenna & Harrison, Inc. Benzofuro[3,2-c]pyrazol-3-amine derivatives
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WO2003051847A1 (en) * 2001-12-19 2003-06-26 Smithkline Beecham P.L.C. (1-h-indazol-3-yl) -amide derivatives as gsk-3 inhibitors

Also Published As

Publication number Publication date
MXPA05000629A (es) 2005-04-25
ES2304531T3 (es) 2008-10-16
DE60320560D1 (de) 2008-06-05
CA2492673A1 (en) 2004-01-22
WO2004007504A1 (en) 2004-01-22
EP1534716B1 (en) 2008-04-23
TWI284645B (en) 2007-08-01
ATE393159T1 (de) 2008-05-15
EP1534716A1 (en) 2005-06-01
BR0312722A (pt) 2005-05-10
AU2003254337A1 (en) 2004-02-02
JP2006501191A (ja) 2006-01-12
DE60320560T2 (de) 2008-12-11
TW200413389A (en) 2004-08-01

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