BRPI0411863A - derivados de pirazolil-indol como inibidores de cinase, processo para seu preparo e composições farmacêuticas compreendendo os mesmos - Google Patents

derivados de pirazolil-indol como inibidores de cinase, processo para seu preparo e composições farmacêuticas compreendendo os mesmos

Info

Publication number
BRPI0411863A
BRPI0411863A BRPI0411863-4A BRPI0411863A BRPI0411863A BR PI0411863 A BRPI0411863 A BR PI0411863A BR PI0411863 A BRPI0411863 A BR PI0411863A BR PI0411863 A BRPI0411863 A BR PI0411863A
Authority
BR
Brazil
Prior art keywords
preparation
pharmaceutical compositions
kinase inhibitors
indole derivatives
pyrazolyl
Prior art date
Application number
BRPI0411863-4A
Other languages
English (en)
Inventor
Daniela Gavina Berta
Barbara Forte
Sergio Mantegani
Mario Varasi
Paola Vianello
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 BRPI0411863A publication Critical patent/BRPI0411863A/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Virology (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

"DERIVADOS DE PIRAZOLIL-INDOL COMO INIBIDORES DE CINASE, PROCESSO PARA SEU PREPARO E COMPOSIçõES FARMACêUTICAS COMPREENDENDO OS MESMOS". A presente invenção refere-se a derivados de pirazolindol da fórmula (I), conforme definido na especificação, e sais farmaceuticamente aceitáveis dos mesmos, processo para seu preparo e composições farmacêuticas compreendendo os mesmos são descritos, os compostos da invenção podendo ser úteis em terapia, no tratamento de doenças associadas a uma atividade desregulada de cinase de proteína, tal como câncer.
BRPI0411863-4A 2003-07-08 2004-07-08 derivados de pirazolil-indol como inibidores de cinase, processo para seu preparo e composições farmacêuticas compreendendo os mesmos BRPI0411863A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US48540603P 2003-07-08 2003-07-08
PCT/EP2004/007479 WO2005005414A2 (en) 2003-07-08 2004-07-08 Pyrazolyl-indole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them

Publications (1)

Publication Number Publication Date
BRPI0411863A true BRPI0411863A (pt) 2006-08-08

Family

ID=34062075

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0411863-4A BRPI0411863A (pt) 2003-07-08 2004-07-08 derivados de pirazolil-indol como inibidores de cinase, processo para seu preparo e composições farmacêuticas compreendendo os mesmos

Country Status (7)

Country Link
US (1) US20050032869A1 (pt)
EP (1) EP1648884A2 (pt)
JP (1) JP2009501126A (pt)
BR (1) BRPI0411863A (pt)
CA (1) CA2531751A1 (pt)
MX (1) MXPA06000302A (pt)
WO (1) WO2005005414A2 (pt)

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TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
WO2005061519A1 (en) * 2003-12-19 2005-07-07 Takeda San Diego, Inc. Kinase inhibitors
US20050250829A1 (en) * 2004-04-23 2005-11-10 Takeda San Diego, Inc. Kinase inhibitors
WO2005118587A1 (en) * 2004-06-02 2005-12-15 Takeda Pharmaceutical Company Limited Indole derivative and use for treatment of cancer
EP1781653A1 (en) * 2004-07-05 2007-05-09 Astex Therapeutics Limited 3,4-disubstituted pyrazoles as cyclin dependent kinases (cdk) or aurora kinase or glycogen synthase 3 (gsk-3) inhibitors
US7550598B2 (en) * 2004-08-18 2009-06-23 Takeda Pharmaceutical Company Limited Kinase inhibitors
DE602005023333D1 (de) 2004-10-15 2010-10-14 Takeda Pharmaceutical Kinaseinhibitoren
KR101334511B1 (ko) 2004-12-30 2013-11-29 아스텍스 테라퓨틱스 리미티드 Ｃｄｋ, ｇｓｋ 및 오로라 키나아제의 활성을 조절하는피라졸 화합물
WO2006133885A1 (en) * 2005-06-15 2006-12-21 F. Hoffmann-La Roche Ag Tricyclic fused indole derivatives and their use as aurora kinase inhibitors
CN101287737A (zh) * 2005-08-12 2008-10-15 遗传技术研究公司 五环激酶抑制剂
US8119655B2 (en) * 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
CA2631871A1 (en) * 2005-12-16 2007-10-25 Genentech, Inc. Tetracyclic kinase inhibitors
WO2007077435A1 (en) * 2005-12-30 2007-07-12 Astex Therapeutics Limited Pharmaceutical compounds
EP2049119A2 (en) * 2006-06-29 2009-04-22 Astex Therapeutics Limited Pharmaceutical combinations of 1-cyclopropyl-3-[3-(5-morphoolin-4-ylmethyl-1h-benzoimidazol-2-yl)-1h-1-pyrazol-4-yl]-urea
US20110159111A1 (en) * 2006-06-29 2011-06-30 Astex Therapeutics Limited Pharmaceutical combinations
SG158147A1 (en) 2006-10-09 2010-01-29 Takeda Pharmaceutical Kinase inhibitors
EP2223925A1 (en) * 2006-10-09 2010-09-01 Takeda Pharmaceutical Company Limited Kinase inhibitors
US8168787B2 (en) 2006-11-16 2012-05-01 F.I.S. Fabbrica Italiana Sintetici S.P.A. Process for the preparation of imatinib and intermediates thereof
JP2009001541A (ja) * 2006-12-15 2009-01-08 Ishihara Sangyo Kaisha Ltd 新規ピラゾール化合物を中間体として用いるアントラニルアミド系化合物の製造方法
US8299070B2 (en) * 2009-11-25 2012-10-30 Japan Tobacco Inc. Indole compounds and pharmaceutical use thereof
CA2790284C (en) 2010-02-17 2019-01-08 Takeda Pharmaceutical Company Limited Thieno-pyrimidine compounds having cdc7 inhibitory activity
JP5859640B2 (ja) 2011-05-17 2016-02-10 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ブルトンチロシンキナーゼ阻害剤
CN104640850A (zh) * 2012-10-26 2015-05-20 霍夫曼-拉罗奇有限公司 3,4-二取代的1h-吡唑和4,5-二取代的噻唑的syk抑制剂
CN103044311B (zh) * 2012-12-26 2015-04-22 山东大学 一种多取代吲哚类化合物及其制备方法和应用
JP6912486B2 (ja) * 2016-02-19 2021-08-04 フェニックス モレキュラー デザインズ Ｒｓｋ阻害剤として有用なカルボキサミド誘導体
TWI752155B (zh) 2017-02-01 2022-01-11 德商菲尼克斯製藥股份有限公司 芳香烴受體(AhR)調節劑化合物
TWI674260B (zh) 2017-02-01 2019-10-11 德商菲尼克斯製藥股份有限公司 芳基烴受體(AhR)調節劑化合物
TW201835070A (zh) * 2017-02-21 2018-10-01 德商菲尼克斯製藥股份有限公司 芳香烴受體(AhR)調節劑化合物
WO2019100062A1 (en) 2017-11-20 2019-05-23 Ichan School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
CN111819193A (zh) 2018-01-05 2020-10-23 西奈山伊坎医学院 增加胰腺β细胞增殖的方法、治疗方法以及组合物
AU2019240065A1 (en) 2018-03-20 2020-09-24 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
EP3906028A4 (en) * 2018-12-31 2022-10-12 Icahn School of Medicine at Mount Sinai KINA INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE
KR20210126077A (ko) 2019-02-11 2021-10-19 피닉스 몰레큘라 디자인스 Rsk 억제제의 결정형
US11807644B2 (en) * 2020-05-12 2023-11-07 Pmv Pharmaceuticals, Inc. Methods and compounds for restoring mutant p53 function
WO2022204235A1 (en) * 2021-03-23 2022-09-29 Nido Biosciences, Inc. Bicyclic compounds as androgen receptor modulators
WO2023098699A1 (en) * 2021-12-01 2023-06-08 Nanjing Immunophage Biotech Co., Ltd Compounds and their uses as cd38 inhibitors

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BR0110302A (pt) * 2000-04-18 2003-01-14 Agouron Pharma Compostos de pirazol para inibição de proteìnas cinase, sal e pró-droga farmaceuticamente aceitável, metabólito farmaceuticamente ativo ou sal farmaceuticamente aceitável de metabólito, composição farmacêutica, método de tratamento de condição doentia em mamìferos mediada pela atividade de proteìna cinase, método de modulação ou inibição da atividade de um receptor de proteìna cinase
GB0102687D0 (en) * 2001-02-02 2001-03-21 Pharmacia & Upjohn Spa Oxazolyl-pyrazole derivatives active as kinase inhibitors,process for their preparation and pharmaceutical compositions comprising them
US20020198252A1 (en) * 2001-05-24 2002-12-26 Joseph Payack Process for the preparation of alkylamine substituted indoles
US20040242559A1 (en) * 2003-04-25 2004-12-02 Aventis Pharma S.A. Novel indole derivatives, preparation thereof as medicinal products and pharmaceutical compositions, and especially as KDR inhibitors

Also Published As

Publication number Publication date
US20050032869A1 (en) 2005-02-10
EP1648884A2 (en) 2006-04-26
MXPA06000302A (es) 2006-04-18
WO2005005414A2 (en) 2005-01-20
CA2531751A1 (en) 2005-01-20
WO2005005414A3 (en) 2005-04-21
JP2009501126A (ja) 2009-01-15

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Legal Events

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B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE AS 5A, 6A, 7A E 8A ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2159 DE 22/05/2012.