BR0312924A - Biciclo-pirazóis ativos como inibidores de quinase, processo para sua preparação e composições farmacêuticas compreendendo os mesmos - Google Patents

Biciclo-pirazóis ativos como inibidores de quinase, processo para sua preparação e composições farmacêuticas compreendendo os mesmos

Info

Publication number
BR0312924A
BR0312924A BR0312924-1A BR0312924A BR0312924A BR 0312924 A BR0312924 A BR 0312924A BR 0312924 A BR0312924 A BR 0312924A BR 0312924 A BR0312924 A BR 0312924A
Authority
BR
Brazil
Prior art keywords
preparation
pharmaceutical compositions
kinase inhibitors
pyrazoles
pyrazol
Prior art date
Application number
BR0312924-1A
Other languages
English (en)
Inventor
Manuela Villa
Francesca Abrate
Daniele Fancelli
Mario Varasi
Anna Vulpetti
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 BR0312924A publication Critical patent/BR0312924A/pt

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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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

Landscapes

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

Abstract

"BICICLO-PIRAZóIS ATIVOS COMO INIBIDORES DE QUINASE, PROCESSO PARA SUA PREPARAçãO E COMPOSIçõES FARMACêUTICAS COMPREENDENDO OS MESMOS". A presente invenção providencia um método para tratamento de doenças ocasionadas por uma atividade de proteína quinase alterada e associadas com essa atividade, compreendendo a administração a um mamífero em necessidade disto, de uma quantidade eficaz de um derivado pirazol-tetraidropiridina. A invenção também providencia pirazol-tetraidro piridinas específicos, uma biblioteca compreendendo pelo menos dois deles, um processo para sua preparação e a composições farmacêuticas que os contém, sendo úteis no tratamento de doenças ocasionadas por e/associadas com uma atividade de proteína quinase alterada, tal como câncer, distúrbios proliferativos celulares, infecções virais, doenças autoimune e distúrbios neurodegenerativos.
BR0312924-1A 2002-07-25 2003-07-01 Biciclo-pirazóis ativos como inibidores de quinase, processo para sua preparação e composições farmacêuticas compreendendo os mesmos BR0312924A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39812202P 2002-07-25 2002-07-25
PCT/EP2003/007000 WO2004014374A1 (en) 2002-07-25 2003-07-01 Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them

Publications (1)

Publication Number Publication Date
BR0312924A true BR0312924A (pt) 2005-07-12

Family

ID=31715671

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0312924-1A BR0312924A (pt) 2002-07-25 2003-07-01 Biciclo-pirazóis ativos como inibidores de quinase, processo para sua preparação e composições farmacêuticas compreendendo os mesmos

Country Status (8)

Country Link
US (1) US20060100233A1 (pt)
EP (1) EP1526852A1 (pt)
JP (1) JP2005536526A (pt)
AU (1) AU2003244632A1 (pt)
BR (1) BR0312924A (pt)
CA (1) CA2493625A1 (pt)
MX (1) MXPA05000947A (pt)
WO (1) WO2004014374A1 (pt)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
KR101151653B1 (ko) 2003-09-17 2012-06-28 얀센 파마슈티카 엔.브이. 융합된 헤테로사이클릭 화합물
WO2005030776A1 (en) 2003-09-23 2005-04-07 Vertex Pharmaceuticals Incorporated Pyrazolopyrrole derivatives as protein kinase inhibitors
JP2008516973A (ja) 2004-10-15 2008-05-22 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
CN101365700A (zh) * 2005-11-15 2009-02-11 沃泰克斯药物股份有限公司 可用作激酶抑制剂的氮杂吲唑
US20100120717A1 (en) 2006-10-09 2010-05-13 Brown Jason W Kinase inhibitors
AU2008256940A1 (en) * 2007-05-25 2008-12-04 Elan Pharmaceuticals, Inc. Pyrazolopyrrolidines as inhibitors of gamma secretase
US7741350B1 (en) 2009-01-28 2010-06-22 Cara Therapeutics, Inc. Bicyclic pyrazolo-heterocycles
JP6062633B2 (ja) 2009-01-28 2017-01-18 カラ セラピューティクス インコーポレイテッド 二環式ピラゾロ複素環類
EP2615916B1 (en) 2010-09-16 2017-01-04 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel erk inhibitors
EP2642998B1 (en) 2010-11-24 2020-09-16 The Trustees of Columbia University in the City of New York A non-retinoid rbp4 antagonist for treatment of age-related macular degeneration and stargardt disease
US9333202B2 (en) 2012-05-01 2016-05-10 The Trustees Of Columbia University In The City Of New York Non-retinoid antagonists for treatment of age-related macular degeneration and stargardt disease
US9096596B2 (en) 2013-03-14 2015-08-04 Janssen Pharmaceutica Nv P2X7 modulators
TWI644671B (zh) 2013-03-14 2018-12-21 比利時商健生藥品公司 Ｐ２ｘ７調節劑
US9938291B2 (en) 2013-03-14 2018-04-10 The Trustess Of Columbia University In The City Of New York N-alkyl-2-phenoxyethanamines, their preparation and use
US10053463B2 (en) 2013-03-14 2018-08-21 Janssen Pharmaceutica Nv Substituted [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
JO3509B1 (ar) 2013-03-14 2020-07-05 Janssen Pharmaceutica Nv معدلات p2x7
US10273243B2 (en) 2013-03-14 2019-04-30 The Trustees Of Columbia University In The City Of New York 4-phenylpiperidines, their preparation and use
WO2014152018A1 (en) 2013-03-14 2014-09-25 The Trustees Of Columbia University In The City Of New York Octahydrocyclopentapyrroles, their preparation and use
US9944644B2 (en) 2013-03-14 2018-04-17 The Trustees Of Columbia University In The City Of New York Octahydropyrrolopyrroles their preparation and use
EP3137168B1 (en) 2014-04-30 2022-01-05 The Trustees of Columbia University in the City of New York Substituted 4-phenylpiperidines, their preparation and use
EP3191492B1 (en) 2014-09-12 2019-01-09 Janssen Pharmaceutica NV P2x7 modulators
JP6771464B2 (ja) 2014-11-27 2020-10-21 ジェネンテック， インコーポレイテッド Ｃｂｐおよび／またはｅｐ３００インヒビターとしての、４，５，６，７−テトラヒドロ−１ｈ−ピラゾロ［４，３−ｃ］ピリジン−３−アミン化合物
KR20170118706A (ko) 2014-12-30 2017-10-25 노비라 테라퓨틱스, 인코포레이티드 B형 간염 감염을 치료하는 유도체 및 그 방법
CN104530045A (zh) * 2015-01-14 2015-04-22 中国药科大学 吡唑并[4,3-c]四氢吡啶类c-Met激酶抑制剂及其制备方法和用途
US10738035B2 (en) 2015-05-13 2020-08-11 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
EP3426245B1 (en) 2016-03-07 2022-12-14 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
WO2017205538A1 (en) 2016-05-24 2017-11-30 Genentech, Inc. Pyrazolopyridine derivatives for the treatment of cancer
EP3478692B1 (en) 2016-06-29 2020-06-17 Novira Therapeutics Inc. Oxadiazepinone derivatives and their use in the treatment of hepatitis b infections
CN114057739A (zh) 2016-06-29 2022-02-18 诺维拉治疗公司 二氮杂酮衍生物及其在治疗乙型肝炎感染中的用途
TW202244048A (zh) 2017-03-20 2022-11-16 美商佛瑪治療公司 作為丙酮酸激酶（ｐｋｒ）活化劑之吡咯并吡咯組成物
JP7221277B2 (ja) 2017-08-28 2023-02-13 エナンタ ファーマシューティカルズ インコーポレイテッド Ｂ型肝炎抗ウイルス剤
US10723733B2 (en) 2017-12-06 2020-07-28 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
WO2019143902A2 (en) 2018-01-22 2019-07-25 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
US10729688B2 (en) 2018-03-29 2020-08-04 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
BR112021005188A2 (pt) 2018-09-19 2021-06-08 Forma Therapeutics, Inc. tratamento de anemia falciforme com um composto de ativação de piruvato cinase r
US20230055923A1 (en) 2018-09-19 2023-02-23 Forma Therapeutics, Inc. Activating pyruvate kinase r
JP2022500466A (ja) 2018-09-21 2022-01-04 エナンタ ファーマシューティカルズ インコーポレイテッド 抗ウイルス剤としての官能化複素環
WO2020065613A1 (en) 2018-09-28 2020-04-02 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
MX2021003661A (es) 2018-09-28 2021-08-19 Janssen Pharmaceutica Nv Moduladores de la monoacilglicerol lipasa.
CN113166115A (zh) * 2018-10-05 2021-07-23 埃默里大学 单体和多聚体抗hbv药剂
AR116946A1 (es) 2018-11-02 2021-06-30 Aicuris Gmbh & Co Kg Derivados de urea 6,7-dihidro-4h-pirazolo[4,3-c]piridinas activas contra el virus de la hepatitis b (vhb)
JP2022507724A (ja) 2018-11-21 2022-01-18 エナンタ ファーマシューティカルズ インコーポレイテッド 抗ウイルス剤としての官能化複素環
WO2020247444A1 (en) 2019-06-03 2020-12-10 Enanta Pharmaceuticals, Inc, Hepatitis b antiviral agents
WO2020247575A1 (en) 2019-06-04 2020-12-10 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
US11760755B2 (en) 2019-06-04 2023-09-19 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
US11738019B2 (en) 2019-07-11 2023-08-29 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
WO2021055425A2 (en) 2019-09-17 2021-03-25 Enanta Pharmaceuticals, Inc. Functionalized heterocycles as antiviral agents
US11839663B2 (en) 2019-09-30 2023-12-12 Janssen Pharmaceutica Nv Radiolabelled MGL pet ligands
US11802125B2 (en) 2020-03-16 2023-10-31 Enanta Pharmaceuticals, Inc. Functionalized heterocyclic compounds as antiviral agents
WO2021191359A1 (en) 2020-03-26 2021-09-30 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK27383A (da) * 1982-02-17 1983-08-18 Lepetit Spa Fremgangsmaade til fremstilling af pyrazol(4,3-c)pyridiner
AU702105B2 (en) * 1994-10-20 1999-02-11 Pfizer Inc. Bicyclic tetrahydro pyrazolopyridines and their use as medicaments
EP1320531B1 (en) * 2000-08-10 2010-09-08 Pfizer Italia S.r.l. Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
CN1250544C (zh) * 2001-02-07 2006-04-12 奥索-麦克尼尔药品公司 吡啶并芳基苯基噁唑烷酮抗菌剂和相关组合物及方法
US20030073672A1 (en) * 2001-09-05 2003-04-17 Breitenbucher J. Guy Method for treating allergies using substituted pyrazoles

Also Published As

Publication number Publication date
MXPA05000947A (es) 2005-05-16
EP1526852A1 (en) 2005-05-04
WO2004014374A1 (en) 2004-02-19
JP2005536526A (ja) 2005-12-02
AU2003244632A1 (en) 2004-02-25
US20060100233A1 (en) 2006-05-11
CA2493625A1 (en) 2004-02-19

Similar Documents

Publication Publication Date Title
BR0312924A (pt) Biciclo-pirazóis ativos como inibidores de quinase, processo para sua preparação e composições farmacêuticas compreendendo os mesmos
BR0312913A (pt) Ativo de biciclo-pirazóis como inibidores de cinase, processo para sua preparação e composições farmacêuticas compreendendo o mesmo
BR0215063A (pt) Derivados de hidroxifenil-pirazol ativos como inibidores de cinase, processo para preparação dos mesmos e composições farmacêuticas compreendendo-os
BR122019010200B8 (pt) compostos de pirazol-quinazolina, seus sais, produtos ou kits e composições farmacêuticas
Wang et al. HSP27, 70 and 90, anti-apoptotic proteins, in clinical cancer therapy
BR0315988A (pt) Derivados de diidropirimido[4,5-d]pirimidinona substituìda por amino, sua produção e uso como agentes farmacêuticos
BRPI0407544A (pt) derivados de pirazol tetracìclicos como inibidores da cinase, processo para a sua preparação e composições farmacêuticas que os compreendem
BR0212841A (pt) Derivado ativo de aminoindazole como inibidores de cinase, processo para sua preparação e composições farmacêuticas que os contém
BR0313160A (pt) Composto, composição farmacêutica, métodos para tratar uma condição e um neoplasmo suscetìvel em um animal em um animal, processo para preparar um composto e uso de um composto
BR112014027181A2 (pt) derivados de benzamida para a inibição da atividade de abl1, abl2 e bcr-abl1
EA200400283A1 (ru) Производные аминофталазинона, активные как ингибиторы киназ, способ их получения и содержащие их фармацевтические композиции
BRPI0507375A (pt) derivados de 1h-tieno[2,3-c]pirazol úteis como inibidores de quinase
BR0009044A (pt) Composto, composição farmacêutica, método para tratar uma doença em um animal, uso de um composto, e, processo para fabricar um composto
BR9806870A (pt) Composto, processo para a profilaxia ou tratamento de uma condição clìnica em um mamìfero, formulação farmacêutica, e, uso de um composto e processo para preparar o mesmo.
BRPI0409624A (pt) 2-hidróxi-3-diaminoalcanos de benzamida
BR112014026383A2 (pt) derivados de benzamida para inibir a atividade de abl1, abl2 e bcr-abl1
BR0307819A (pt) Derivados de pirazol tricìclicos, processo para preparação dos mesmos como agentes antitumorais
BRPI0720588B8 (pt) derivados de pirazol-quinazolina substituídos, processo para sua preparação e seu uso como inibidores da quinase
BRPI0414111A (pt) inibidores heterocìclicos de mek e métodos de uso dos mesmos
BRPI0410477A (pt) composto ou um sal farmaceuticamente aceitável do mesmo, método para a profilaxia ou tratamento de uma condição quiral em um mamìfero, formulação farmacêutica, combinação, uso de um composto, e, processo para preparar um composto
BRPI0805826B8 (pt) compostos espiro-substituídos, composição farmacêutica e uso
BR0009043A (pt) Composto, composição farmacêutica, e, método de tratar uma doença em um animal em que a atividade da cisteìna protease contribui para a patologia e/ou sintomatologia da doença
BRPI0606313A2 (pt) derivados de 4-(1h-indol-3-il)-pirimidin-2-ilamina, processo para sua preparação e seu uso em terapia
BR0213233A (pt) Alcinos inibidores de metaloproteinase de matriz
EA200400289A1 (ru) Производные аминоизоксазола, активные в качестве ингибиторов киназы

Legal Events

Date Code Title Description
B08F Application fees: application dismissed [chapter 8.6 patent gazette]

Free format text: REFERENTE 6A., E 7A. 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 2064 DE 27/07/2010.