PE20020566A1 - DERIVADOS DE FENILACETAMIDO-PIRAZOLES COMO INHIBIDORES DE LA cdk/CICLINA QUINASA - Google Patents

DERIVADOS DE FENILACETAMIDO-PIRAZOLES COMO INHIBIDORES DE LA cdk/CICLINA QUINASA

Info

Publication number
PE20020566A1
PE20020566A1 PE2001001182A PE2001001182A PE20020566A1 PE 20020566 A1 PE20020566 A1 PE 20020566A1 PE 2001001182 A PE2001001182 A PE 2001001182A PE 2001001182 A PE2001001182 A PE 2001001182A PE 20020566 A1 PE20020566 A1 PE 20020566A1
Authority
PE
Peru
Prior art keywords
phenyl
cdk
cyclopropil
oxazolidin
propanamide
Prior art date
Application number
PE2001001182A
Other languages
English (en)
Inventor
Paolo Pevarello
Paolo Orsini
Gabriella Traquandi
Maria Gabriella Brasca
Raffaella Amici
Manuela Villa
Claudia Piutti
Mario Varasi
Antonio Longo
Original Assignee
Pharmacia & Upjohn 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
Priority claimed from US09/907,943 external-priority patent/US6455559B1/en
Application filed by Pharmacia & Upjohn Spa filed Critical Pharmacia & Upjohn Spa
Publication of PE20020566A1 publication Critical patent/PE20020566A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • 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
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings 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
    • C07D231/38Nitrogen atoms
    • C07D231/40Acylated on said nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Virology (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A DERIVADOS DE FENILACETAMIDO-PIRAZOLES DE FORMULA I DONDE R ES UN CICLOALQUILO C3-C5; R1 Y R2 SON H, HALOGENO, AMINO, HIDROXI, ALQUILO C1-C5, ENTRE OTROS; R3 EN POSICION 3 O 4 DEL ANILLO FENILO ES UN GRUPO DE FORMULA II REPRESENTANDO UN HETEROCICLICO QUE CONTIENE N CON 5 O 6 MIEMBROS; QUE CONTIENEN 1 Y 2 HETEROATOMOS ADICIONALES, IGUALES O DIFERENTES SELECCIONADOS ENTRE N, O, S; m ES 0-4; R4 ES HALOGENO, OH, ALQUILO C1-4, ALCOXI, ENTRE OTROS. UN COMPUESTO PREFERIDO ES (2S)-N-(5-CICLOPROPIL-1H-PIRAZOL-3-IL)-2-[4-(2-OXO-1,3-OXAZOLIDIN-3-IL)FENIL]PROPANAMIDA, N-(5-CICLOPROPIL-1H-PIRAZOL-3-IL)-2-[4-(2-OXO-1,3-OXAZOLIDIN-3-IL)FENIL]PROPANAMIDA, (2R)-N-(5-CICLOPROPIL-1H-PIRAZOL-3-IL)-2-[4-(2-OXO-1,3-OXAZOLIDIN-3-IL)FENIL]PROPANAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS MENCIONADOS TIENEN ACTIVIDAD INHIBITORIA DE LA cdk/CICLINA QUINASA Y SON UTILES COMO AGENTES ANTITUMORALES
PE2001001182A 2000-11-27 2001-11-27 DERIVADOS DE FENILACETAMIDO-PIRAZOLES COMO INHIBIDORES DE LA cdk/CICLINA QUINASA PE20020566A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25291100P 2000-11-27 2000-11-27
US09/907,943 US6455559B1 (en) 2001-07-19 2001-07-19 Phenylacetamido-pyrazole derivatives, process for their preparation and their use as antitumor agents

Publications (1)

Publication Number Publication Date
PE20020566A1 true PE20020566A1 (es) 2002-06-22

Family

ID=26942786

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2001001182A PE20020566A1 (es) 2000-11-27 2001-11-27 DERIVADOS DE FENILACETAMIDO-PIRAZOLES COMO INHIBIDORES DE LA cdk/CICLINA QUINASA

Country Status (10)

Country Link
US (1) US20040019046A1 (es)
EP (1) EP1345909A1 (es)
JP (1) JP2004517840A (es)
AR (1) AR035374A1 (es)
AU (1) AU2002215053A1 (es)
CA (1) CA2430151A1 (es)
MX (1) MXPA03004644A (es)
NZ (1) NZ525892A (es)
PE (1) PE20020566A1 (es)
WO (1) WO2002048114A1 (es)

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BR0315158A (pt) 2002-10-09 2005-08-16 Pfizer Prod Inc Compostos de pirazol para o tratamento de distúrbios neurodegenarativos
JP4398866B2 (ja) * 2002-10-18 2010-01-13 ビーエーエスエフ ソシエタス・ヨーロピア 1−フェニルピロリジン−2−オン−3−カルボキサミド
UA81790C2 (uk) * 2002-12-19 2008-02-11 Фармация Италия С.П.А. Заміщені піролопіразольні похідні як інгібітори кінази
CN1826343A (zh) 2003-05-22 2006-08-30 法玛西雅意大利公司 吡唑并-喹唑啉衍生物、它们的制备方法和它们作为激酶抑制剂的用途
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
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
US7244757B2 (en) * 2004-04-01 2007-07-17 Pfizer Inc Pyrazole-amine compounds for the treatment of neurodegenerative disorders
EP1763524A1 (en) * 2004-04-23 2007-03-21 Takeda San Diego, Inc. Indole derivatives and use thereof as kinase inhibitors
US7550598B2 (en) * 2004-08-18 2009-06-23 Takeda Pharmaceutical Company Limited Kinase inhibitors
US7713973B2 (en) 2004-10-15 2010-05-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
GB0507575D0 (en) * 2005-04-14 2005-05-18 Novartis Ag Organic compounds
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
JP2009535388A (ja) * 2006-05-03 2009-10-01 アストラゼネカ アクチボラグ ピラゾール誘導体、及びそのpi3k阻害薬としての使用
EP2223925A1 (en) * 2006-10-09 2010-09-01 Takeda Pharmaceutical Company Limited Kinase inhibitors
SG175609A1 (en) 2006-10-09 2011-11-28 Takeda Pharmaceutical Kinase inhibitors
CA2666116A1 (en) * 2006-10-16 2008-04-24 Novartis Ag Phenylacetamides useful as protein kinase inhibitors
CN102105148B (zh) 2008-07-24 2013-04-10 内尔维阿诺医学科学有限公司 包含aurora激酶抑制剂和抗肿瘤药的治疗组合
EP2651930B1 (en) * 2010-12-16 2015-10-28 Boehringer Ingelheim International GmbH Biarylamide inhibitors of leukotriene production
US8541576B2 (en) 2010-12-17 2013-09-24 Nerviano Medical Sciences Srl Substituted pyrazolo-quinazoline derivatives as kinase inhibitors
US8937071B2 (en) 2013-03-15 2015-01-20 Glaxosmithkline Intellectual Property Development Limited Compounds as rearranged during transfection (RET) inhibitors
JP2016516026A (ja) 2013-03-15 2016-06-02 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited Rearrangedduringtransfection(ret)キナーゼ阻害剤としてのピリジン誘導体
SG11201701694QA (en) * 2014-09-10 2017-04-27 Glaxosmithkline Ip Dev Ltd Pyridone derivatives as rearranged during transfection (ret) kinase inhibitors
BR112017004897A2 (pt) 2014-09-10 2017-12-12 Glaxosmithkline Ip Dev Ltd compostos inovadores como inibidores rearranjados durante a transfecção (ret)
MY190459A (en) 2015-06-04 2022-04-21 Aurigene Discovery Tech Ltd Substituted heterocyclyl derivatives as cdk inhibitors
MX2020004930A (es) 2017-11-14 2020-08-27 Merck Sharp & Dohme Compuestos de biarilo sustituido novedosos como inhibidores de indolamina 2,3-dioxigenasa (ido).
WO2019099294A1 (en) 2017-11-14 2019-05-23 Merck Sharp & Dohme Corp. Novel substituted biaryl compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
WO2020142559A1 (en) 2018-12-31 2020-07-09 Biomea Fusion, Llc Inhibitors of menin-mll interaction
CA3125350A1 (en) 2018-12-31 2020-07-09 Biomea Fusion, Llc Irreversible inhibitors of menin-mll interaction
US11180458B2 (en) 2019-11-12 2021-11-23 King Abdulaziz University Anticancer compounds, pharmaceutical compositions thereof, and a method of treating cancer
CN114702615A (zh) * 2021-01-01 2022-07-05 中国石油化工股份有限公司 负载型茂金属、含有其的催化剂、其制备和应用
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US6335342B1 (en) * 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
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US6455559B1 (en) * 2001-07-19 2002-09-24 Pharmacia Italia S.P.A. Phenylacetamido-pyrazole derivatives, process for their preparation and their use as antitumor agents
ES2281633T3 (es) * 2002-02-19 2007-10-01 Pfizer Italia S.R.L. Derivados triciclicos de pirazol, procedimiento para su preparacion y su uso como agentes antitumorales.

Also Published As

Publication number Publication date
MXPA03004644A (es) 2003-09-05
AU2002215053A1 (en) 2002-06-24
AR035374A1 (es) 2004-05-12
JP2004517840A (ja) 2004-06-17
US20040019046A1 (en) 2004-01-29
EP1345909A1 (en) 2003-09-24
CA2430151A1 (en) 2002-06-20
NZ525892A (en) 2004-11-26
WO2002048114A1 (en) 2002-06-20

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