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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

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Classifications

    • 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
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • 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
    • 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
    • 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
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34Heterocyclic 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
    • C07D307/56Heterocyclic 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
    • C07D307/68Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic 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
    • C07D333/26Heterocyclic 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
    • C07D333/38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic 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
    • C07D333/26Heterocyclic 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
    • C07D333/42Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Virology (AREA)
  • Communicable Diseases (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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EP1694686A1 (en) 2003-12-19 2006-08-30 Takeda San Diego, Inc. Kinase inhibitors
TW200526204A (en) * 2004-02-03 2005-08-16 Pharmacia Italia Spa 1h-thieno[2,3-c]pyrazole derivatives useful as kinase inhibitors
EP1778669A2 (en) 2004-08-18 2007-05-02 Takeda San Diego, Inc. 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
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
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
EP2010521A1 (en) 2006-04-19 2009-01-07 Novartis Ag Indazole compounds and methods for inhibition of cdc7
JP5303454B2 (ja) * 2006-05-31 2013-10-02 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有用な1h−フロ[3,2−c]ピラゾール化合物
EA200970361A1 (ru) 2006-10-09 2010-02-26 Такеда Фармасьютикал Компани Лимитед Ингибиторы киназы
US8334301B2 (en) 2007-09-28 2012-12-18 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
DK2692728T3 (en) 2011-03-31 2018-10-08 Carna Biosciences Inc UNKNOWN FURANONDERIVATE
BR112014020173A8 (pt) 2012-03-16 2017-07-11 Hoffmann La Roche Métodos para o tratamento de um melanoma, utilizações de um inibidor, composições, conjunto, método de inibição, método de identificação, método de ajuste do tratamento e invenção
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
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
CN114981298B (zh) 2019-12-12 2024-08-20 听治疗有限责任公司 用于预防和治疗听力损失的组合物和方法
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
WO2025078334A1 (en) 2023-10-09 2025-04-17 Institut National de la Santé et de la Recherche Médicale Combination of pak1 inhibitors and clk inhibitors for preventing resistance to chemotherapy in patients suffering from acute myeloid leukemia

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CZ2003468A3 (cs) * 2000-08-31 2004-05-12 Pfizeráproductsáinc Deriváty pyrazolu a jejich použití jako inhibitorů proteinkinázy
ES2242771T5 (es) * 2000-09-15 2011-10-14 Vertex Pharmaceuticals Incorporated Compuestos de pirazol útiles como inhibidores de proteína quinasas.
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
TW200413389A (en) 2004-08-01
ATE393159T1 (de) 2008-05-15
TWI284645B (en) 2007-08-01
WO2004007504A1 (en) 2004-01-22
DE60320560T2 (de) 2008-12-11
EP1534716B1 (en) 2008-04-23
CA2492673A1 (en) 2004-01-22
MXPA05000629A (es) 2005-04-25
AU2003254337A1 (en) 2004-02-02
EP1534716A1 (en) 2005-06-01
BR0312722A (pt) 2005-05-10
DE60320560D1 (de) 2008-06-05
JP2006501191A (ja) 2006-01-12
ES2304531T3 (es) 2008-10-16

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