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

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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

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)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200526204A (en) * 2004-02-03 2005-08-16 Pharmacia Italia Spa 1h-thieno[2,3-c]pyrazole derivatives useful as kinase inhibitors
WO2006044687A2 (en) 2004-10-15 2006-04-27 Takeda San Diego, Inc. Kinase inhibitors
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
EP1904503B1 (en) 2005-07-19 2013-11-06 Nerviano Medical Sciences S.R.L. 1h-thieno[2,3-c]-pyrazole compounds useful as kinase inhibitors
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
CA2648809A1 (en) 2006-04-19 2007-11-01 Novartis Ag Indazole compounds and methods for inhibition of cdc7
ATE478875T1 (de) * 2006-05-31 2010-09-15 Nerviano Medical Sciences Srl 1h-furoä3,2-cü pyrazolverbindungen, die sich als kinaseinhibitoren eignen
BRPI0719883A2 (pt) 2006-10-09 2015-05-05 Takeda Pharmaceutical Inibidores de quinase
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
USRE48140E1 (en) 2011-03-31 2020-08-04 Carna Biosciences, Inc. Furanone derivative
WO2013135745A1 (en) 2012-03-16 2013-09-19 F. Hoffmann-La Roche Ag Methods of treating melanoma with pak1 inhibitors
WO2015008234A1 (en) * 2013-07-17 2015-01-22 Glenmark Pharmaceuticals S.A. Bicyclic heterocyclic compounds as ror gamma modulators
JP6569908B2 (ja) 2014-01-31 2019-09-04 カルナバイオサイエンス株式会社 抗がん剤組成物
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
EP3663299B1 (en) * 2017-08-01 2023-03-08 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Bicyclic compound acting as ror gamma inhibitor
EP3956446A1 (en) 2019-04-17 2022-02-23 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for treatment of nlrp3 inflammasome mediated il-1beta dependent disorders
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

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EA006381B1 (ru) * 2000-08-10 2005-12-29 Фармация Италия С.П.А. Бициклопиразолы, активные в качестве ингибиторов киназы, способ их получения и включающие их фармацевтические композиции
AP2001002266A0 (en) * 2000-08-31 2001-09-30 Pfizer Prod Inc Pyrazole derivatives.
CA2422371C (en) * 2000-09-15 2010-05-18 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
AU2002353186A1 (en) * 2001-12-19 2003-06-30 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
EP1534716A1 (en) 2005-06-01
DE60320560T2 (de) 2008-12-11
JP2006501191A (ja) 2006-01-12
TWI284645B (en) 2007-08-01
ES2304531T3 (es) 2008-10-16
CA2492673A1 (en) 2004-01-22
DE60320560D1 (de) 2008-06-05
TW200413389A (en) 2004-08-01
EP1534716B1 (en) 2008-04-23
WO2004007504A1 (en) 2004-01-22
BR0312722A (pt) 2005-05-10
AU2003254337A1 (en) 2004-02-02
ATE393159T1 (de) 2008-05-15

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