BR9813926A - Substituição de bioisóstero de catecol por indazol em compostos terapeuticamente ativos - Google Patents

Substituição de bioisóstero de catecol por indazol em compostos terapeuticamente ativos

Info

Publication number
BR9813926A
BR9813926A BR9813926-6A BR9813926A BR9813926A BR 9813926 A BR9813926 A BR 9813926A BR 9813926 A BR9813926 A BR 9813926A BR 9813926 A BR9813926 A BR 9813926A
Authority
BR
Brazil
Prior art keywords
catechol
activity
indazole
replacement
compounds
Prior art date
Application number
BR9813926-6A
Other languages
English (en)
Inventor
Anthony Marfat
Original Assignee
Pfizer Prod Inc
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 Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of BR9813926A publication Critical patent/BR9813926A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • 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
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)

Abstract

Patente de Invenção: <B>"SUBSTITUIçãO DE BIOISóSTERO DE CATECOL POR INDAZOL EM COMPOSTOS TERAPEUTICAMENTE ATIVOS"<D>. São descritas composições de matéria terapeuticamente ativas e suas espécies membro, que compreendem compostos contendo indazol, em que os referidos compostos e a sua atividade farmacêutica resultam diretamente de uma substituição de bioisóstero catecol-por-indazol de um composto contendo catecol tendo a mesma atividade terapêutica, onde os referidos substituintes do não-catecol são os mesmos ou homólogos antes e depois da referida substituição, em que as referidas composições de matéria compreendem um composto de Fórmula (I¹) ou (I²): ou um seu sal farmaceuticamente aceitável, em que em uma modalidade preferida R^ C^ representa hidrogênio; R^ A^ representa ciclohexila; e R^ B^ representa etila. R~ a~ e R~ b~ representam cada um, individualmente e independentemente, hidrogênio ou substituintes do não-catecol dos referidos compostos, que resultam diretamente de uma substituição de bioisóstero catecol-por-indazol do referido composto contendo catecol tendo a referida atividade terapêutica, onde os referidos substituintes do não-catecol são os mesmos ou homólogos antes e depois da referida substituição, desde que R~ a~ e R~ b~ não possam representar ambos, ao mesmo tempo, hidrogênio. A atividade terapêutica envolvida pode compreender atividade inibidora da colinesterase, atividade <244>~ 1~-antagonista e <225>~ 1~-agonista adrenérgica, atividade inibidora de canal de cálcio, atividade antineoplásica, e atividade inibidora de fosfodiesterase do tipo IV.
BR9813926-6A 1997-11-04 1998-10-26 Substituição de bioisóstero de catecol por indazol em compostos terapeuticamente ativos BR9813926A (pt)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US6419897P 1997-11-04 1997-11-04
US6422997P 1997-11-04 1997-11-04
US6418797P 1997-11-04 1997-11-04
US6422897P 1997-11-04 1997-11-04
US6402497P 1997-11-04 1997-11-04
PCT/IB1998/001710 WO1999023077A1 (en) 1997-11-04 1998-10-26 Indazole bioisostere replacement of catechol in therapeutically active compounds

Publications (1)

Publication Number Publication Date
BR9813926A true BR9813926A (pt) 2000-09-19

Family

ID=27535645

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9813926-6A BR9813926A (pt) 1997-11-04 1998-10-26 Substituição de bioisóstero de catecol por indazol em compostos terapeuticamente ativos

Country Status (29)

Country Link
US (1) US6391872B1 (pt)
EP (1) EP1028946A1 (pt)
JP (1) JP2001521926A (pt)
CN (1) CN1284948A (pt)
AP (1) AP910A (pt)
AR (1) AR013746A1 (pt)
AU (1) AU754734B2 (pt)
BG (1) BG104450A (pt)
BR (1) BR9813926A (pt)
CA (1) CA2309150A1 (pt)
CZ (1) CZ20001621A3 (pt)
DZ (1) DZ2640A1 (pt)
EA (1) EA200000488A1 (pt)
HR (1) HRP20000253A2 (pt)
HU (1) HUP0004150A3 (pt)
ID (1) ID23921A (pt)
IL (1) IL135900A0 (pt)
IS (1) IS5465A (pt)
MA (1) MA26563A1 (pt)
NO (1) NO20002129L (pt)
NZ (1) NZ503918A (pt)
OA (1) OA11354A (pt)
PE (1) PE129199A1 (pt)
PL (1) PL340753A1 (pt)
SK (1) SK6252000A3 (pt)
TN (1) TNSN98200A1 (pt)
TR (1) TR200001234T2 (pt)
WO (1) WO1999023077A1 (pt)
YU (1) YU25000A (pt)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL340799A1 (en) * 1997-11-04 2001-02-26 Pfizer Prod Inc Therapeutically active compounds based on a substitution of indazole bioisoster for cathechol in pde 4 inhibitors
UA71971C2 (en) 1999-06-04 2005-01-17 Agoron Pharmaceuticals Inc Diaminothiazoles, composition based thereon, a method for modulation of protein kinases activity, a method for the treatment of diseases mediated by protein kinases
PE20010306A1 (es) * 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
US7141581B2 (en) 1999-07-02 2006-11-28 Agouron Pharmaceuticals, Inc. Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
TWI262914B (en) 1999-07-02 2006-10-01 Agouron Pharma Compounds and pharmaceutical compositions for inhibiting protein kinases
JP2001031549A (ja) * 1999-07-14 2001-02-06 Pola Chem Ind Inc 真皮コラーゲン線維束再構築剤及びそれを含有する化粧料
US6432979B1 (en) 1999-08-12 2002-08-13 American Cyanamid Company Method of treating or inhibiting colonic polyps and colorectal cancer
DE60031127T2 (de) * 1999-08-12 2007-02-01 Wyeth Holdings Corp. Nsaid und egfr kinase inhibitoren enthaltende pharmazeutische formulierung zur behandlung oder inhibierung von dickdarmpolypen und kolorektalem krebs
YU54202A (sh) 2000-01-18 2006-01-16 Agouron Pharmaceuticals Inc. Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije
HN2001000008A (es) 2000-01-21 2003-12-11 Inc Agouron Pharmaceuticals Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas, y su modo de empleo
US7005443B1 (en) * 2000-03-17 2006-02-28 Alcon, Inc. 5-Hydroxy indazole derivatives for treating glaucoma
AU2001249865A1 (en) 2000-04-18 2001-10-30 Agouron Pharmaceuticals, Inc. Pyrazoles for inhibiting protein kinase
DE60234510D1 (de) 2001-04-16 2010-01-07 Eisai R&D Man Co Ltd 1h-indazolverbindungen die jnk hemmen
AU2002337105B2 (en) 2001-09-19 2008-03-20 Takeda Gmbh Combination of a NSAID and a PDE-4 inhibitor
WO2003024456A1 (en) * 2001-09-20 2003-03-27 Eisai Co., Ltd. Methods for treating and preventing migraines
JP2005518097A (ja) * 2002-02-13 2005-06-16 コーニンクレッカ　フィリップス　エレクトロニクス　エヌ　ヴィ 集積半導体光学装置並びにこのような装置を製造する方法及び装置
US7108868B2 (en) 2002-03-22 2006-09-19 Unigen Pharmaceuticals, Inc. Isolation of a dual cox-2 and 5-lipoxygenase inhibitor from acacia
US7972632B2 (en) 2003-02-28 2011-07-05 Unigen Pharmaceuticals, Inc. Identification of Free-B-Ring flavonoids as potent COX-2 inhibitors
NZ535988A (en) 2002-04-30 2005-09-30 Unigen Pharmaceuticals Inc Formulation of a mixture of free-B-ring flavonoids and flavans as a therapeutic agent
US8034387B2 (en) 2002-04-30 2011-10-11 Unigen, Inc. Formulation of a mixture of free-B-ring flavonoids and flavans for use in the prevention and treatment of cognitive decline and age-related memory impairments
ES2309368T3 (es) 2002-12-02 2008-12-16 F. Hoffmann-La Roche Ag Derivados de indazol como antagonista del crf.
KR20050101551A (ko) 2003-02-14 2005-10-24 와이어쓰 5-하이드록시트립타민-6 리간드로서의헤테로사이클릴-3-설포닐인다졸
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
CA2521429A1 (en) * 2003-04-04 2004-10-21 Unigen Pharmaceuticals, Inc. Formulation of dual cycloxygenase (cox) and lipoxygenase (lox) inhibitors for mammal skin care
US6984652B2 (en) * 2003-09-05 2006-01-10 Warner-Lambert Company Llc Gyrase inhibitors
CA2557268A1 (en) 2004-02-27 2005-09-15 F. Hoffmann-La Roche Ag Indazole derivatives and pharmaceutical compositions containing them
US7844309B2 (en) * 2004-02-27 2010-11-30 Nokia Corporation Exchangeable keymat
KR100843526B1 (ko) 2004-02-27 2008-07-03 에프. 호프만-라 로슈 아게 피라졸의 접합 유도체
BRPI0508220A (pt) 2004-02-27 2007-07-17 Hoffmann La Roche derivados de pirazol heteroarila fundidos
US7601847B2 (en) 2004-10-26 2009-10-13 Wyeth Preparation and purification of 4-(indazol-3-yl)phenols
KR20070094747A (ko) * 2004-11-29 2007-09-21 워너-램버트 캄파니 엘엘씨 치료용 피라졸로［３,４-ｂ］피리딘 및 인다졸
AU2006291414A1 (en) * 2005-08-15 2007-03-22 Wyeth Azinyl-3-sulfonylindazole derivatives as 5-hydroxytryptamine-6 ligands
CN101282938A (zh) * 2005-08-15 2008-10-08 惠氏公司 作为5-羟色胺-6配体的经取代3-磺酰基吲唑衍生物
CN101243088B (zh) 2005-08-25 2011-06-29 霍夫曼-拉罗奇有限公司 p38 MAP激酶抑制剂及使用它的方法
WO2007029077A1 (en) * 2005-09-05 2007-03-15 Ranbaxy Laboratories Limited Substituted indazoles as inhibitors of phosphodiesterase type-iv
WO2007031838A1 (en) 2005-09-16 2007-03-22 Ranbaxy Laboratories Limited Substituted pyrazolo [3,4-b] pyridines as phosphodiesterase inhibitors
AU2006311942B2 (en) * 2005-11-03 2012-11-22 Allergan, Inc. Prostaglandins and analogues as agents for lowering intraocular pressure
US7645752B2 (en) 2006-01-13 2010-01-12 Wyeth Llc Sulfonyl substituted 1H-indoles as ligands for the 5-hydroxytryptamine receptors
CN101415685B (zh) 2006-01-31 2011-08-24 阿雷生物药品公司 激酶抑制剂及其使用方法
JP2009528363A (ja) 2006-02-28 2009-08-06 ヘリコン セラピューティクス，インコーポレイテッド Ｐｄｅ４インヒビターとしての治療用ピペラジン
WO2007120523A2 (en) * 2006-03-31 2007-10-25 Vitae Pharmaceuticals, Inc. 6-(aminoalkyl)indazoles
JP2009532471A (ja) * 2006-04-05 2009-09-10 ワイス ５−ヒドロキシトリプタミン−６リガンドとしてのスルホニル−３−ヘテロシクリルインダゾール誘導体
WO2007120596A1 (en) * 2006-04-12 2007-10-25 Wyeth DIHYDRO[1,4]DIOXINO[2,3-e]INDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS
US8012886B2 (en) * 2007-03-07 2011-09-06 Asm Assembly Materials Ltd Leadframe treatment for enhancing adhesion of encapsulant thereto
PT2124944E (pt) 2007-03-14 2012-05-17 Ranbaxy Lab Ltd Derivados de pirazolo[3,4-b]piridina como inibidores de fosfodiesterase
WO2011034217A1 (ja) * 2009-09-18 2011-03-24 株式会社Ｒｉｖｅｒｓｏｎ ポリフェノール誘導体及びそれの産生方法
JP2013526542A (ja) 2010-05-12 2013-06-24 アッヴィ・インコーポレイテッド キナーゼのインダゾール阻害薬
CN103709146B (zh) * 2014-01-15 2015-11-25 中国药科大学 一类含苯并咪唑结构的喹啉-4-胺衍生物、其制法及医药用途

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1989003385A1 (en) * 1987-10-13 1989-04-20 Yoshitomi Pharmaceutical Industries, Ltd. Fused pyrazole compounds, process for their preparation, and their medicinal use
EP0338087A4 (en) * 1987-10-13 1991-07-24 Yoshitomi Pharmaceutical Industries, Ltd. Fused pyrazole compounds, process for their preparation, and their medicinal use
US5593997A (en) * 1995-05-23 1997-01-14 Pfizer Inc. 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors
AP1147A (en) * 1996-05-03 2003-02-25 Pfizer Substituted indazole derivatives and related compounds.
AU724549B2 (en) * 1996-09-04 2000-09-28 Pfizer Inc. Indazole derivatives and their use as inhibitors of phosphodiesterase (PDE) type IV and the production of tumor necrosis factor (TNF)

Also Published As

Publication number Publication date
US6391872B1 (en) 2002-05-21
AR013746A1 (es) 2001-01-10
AP910A (en) 2000-12-05
AU754734B2 (en) 2002-11-21
SK6252000A3 (en) 2001-11-06
MA26563A1 (fr) 2004-12-20
AP9801375A0 (en) 1998-12-31
OA11354A (en) 2003-12-23
EP1028946A1 (en) 2000-08-23
CN1284948A (zh) 2001-02-21
AU9455298A (en) 1999-05-24
TNSN98200A1 (fr) 2005-03-15
JP2001521926A (ja) 2001-11-13
YU25000A (sh) 2003-12-31
NZ503918A (en) 2002-03-28
DZ2640A1 (fr) 2003-03-08
PE129199A1 (es) 1999-12-16
EA200000488A1 (ru) 2000-10-30
BG104450A (en) 2000-12-29
HUP0004150A3 (en) 2001-08-28
HRP20000253A2 (en) 2001-06-30
PL340753A1 (en) 2001-02-26
CZ20001621A3 (cs) 2001-08-15
TR200001234T2 (tr) 2000-08-21
CA2309150A1 (en) 1999-05-14
IS5465A (is) 2000-04-19
NO20002129L (no) 2000-07-03
NO20002129D0 (no) 2000-04-26
IL135900A0 (en) 2001-05-20
WO1999023077A1 (en) 1999-05-14
HUP0004150A2 (hu) 2001-05-28
ID23921A (id) 2000-05-25

Similar Documents

Publication Publication Date Title
BR9813926A (pt) Substituição de bioisóstero de catecol por indazol em compostos terapeuticamente ativos
NO20021328L (no) Pyrazolopyrimidier som terapeutiske midler
HK1062677A1 (en) 17Beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
BRPI0412219A (pt) composto, sal farmaceuticamente aceitável de um composto, composição farmacêutica, método para regular a transdução de sinal método para tratamento ou prevenção de uma doença
BR9909565A (pt) Derivados bicìclicos do ácido hidroxâmico
ES2145913T3 (es) Inhibidores de metaloproteasas.
NO20060981L (no) Pyridazinderivater og deres anvendelse som terapeutiske midler
BR0113448A (pt) Composto da fórmula ou um sal ou solvato deste ou um derivado destes fisiologicamente funcional, composição farmacêutica, uso do composto ou de um sal ou solvato deste ou de um derivado destes fisiologicamente funcional, e , métodos para tratar uma condição ou estado de doença mediados pela p38 quinase ou mediados pelas citoquinas, e mediados pela jnk quinase ou mediados pelas citoquinas, e ,para tratar duas ou mais condições ou doenças independentemente mediadas pela atividade da p38 e da jnk quinase
BRPI0508107A (pt) derivados de indazol e composições farmacêuticas contendo os mesmos
BR9814643A (pt) Inibidor de metaloprotease de ácido sulfona hidroxâmico aromático
MA26861A1 (fr) Inhibiteurs non peptidiques de la liaison cellulaire sous la dependance de vla-4 utiles dans le traitement des maladies inflammatoires, auto-immunes et respiratoires
BRPI0407618A (pt) derivados de tiazole amino substituidos com cicloalquilo contendo n e composições farmacêuticas para inibição da proliferação celular e métodos para a sua utilização
BR9809062A (pt) Inibidores da metaloproteinase, composições farmacêuticas comtendo os mesmos e seus usos farmacêuticos
BR0001292A (pt) Desfolhante
DK1263730T3 (da) Aminderivater til behandling af apoptose
HUP0001062A2 (hu) NAALADáz gátló hatású foszfinsavszármazékokat tartalmazó gyógyászati készítmények
HUP0102255A2 (hu) VLA-4 inhibitor hatású oMePUPA-V, ezt tartalmazó gyógyszerkészítmény és alkalmazása
SG147450A1 (en) Sustained release pharmaceutical compositions comprising aplindore and derivatives thereof
SE9901573D0 (sv) New compounds
BR0210285A (pt) Utilização de um composto, composto e composição farmacêutica
BR0315820A (pt) Inibidores de integrase de hiv, composições farmacêuticas e métodos para a sua utilização
MXPA04003611A (es) Piperidina- y piperazinacetaminas como inhibidores de la 17 beta-hidroxiesteroide deshidrogenasa tipo 3 para el tratamiento de enfermedades androgeno-dependientes.
BR9814376A (pt) Composto ou um pró-medicamento correspondente, ou um sal farmaceuticamente aceitável ou solvato de um tal composto ou um pró-medicamento deste, uso destes, composição farmacêutica, processo para o tratamento de um paciente humano ou animal não humano sofrendo de, ou sujeito a, condições que podem ser melhoradas pela admnistração de um inibidor da adesão celular mediada por &amp;4ß1, e, resina
NO308654B1 (no) Amid-derivater, fremgangsmÕter og mellomprodukter for fremstilling derav, deres anvendelse og farmasøytiske blandinger som inneholdende dem
ITMI20042475A1 (it) Uso di derivati tiazolidinonici come agenti terapeutici

Legal Events

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

Free format text: REFERENTE A 9A ANUIDADE.

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 PUBLICADO NA 1945 DE 15 - 04 - 2008.