BR0210532A - Derivados de naftil benzofurano como inibidores do inibidor-1 de ativador de plasminogênio (pai-1) - Google Patents

Derivados de naftil benzofurano como inibidores do inibidor-1 de ativador de plasminogênio (pai-1)

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Publication number
BR0210532A
BR0210532A BR0210532-2A BR0210532A BR0210532A BR 0210532 A BR0210532 A BR 0210532A BR 0210532 A BR0210532 A BR 0210532A BR 0210532 A BR0210532 A BR 0210532A
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Brazil
Prior art keywords
aryl
heteroaryl
alkyl
substituted
cycloalkyl
Prior art date
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BR0210532-2A
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English (en)
Inventor
Hassan Mahmoud Elokdah
Geraldine Ruth Mcfarlane
Scott Christian Mayer
David Leroy Crandall
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Wyeth Corp
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Publication of BR0210532A publication Critical patent/BR0210532A/pt

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    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • 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
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    • A61P35/00—Antineoplastic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/80—Radicals substituted by oxygen atoms

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Furan Compounds (AREA)

Abstract

"DERIVADOS DE NAFTIL BENZOFURANO COMO INIBIDORES DO INIBIDOR-1 DE ATIVADOR DE PLASMINOGêNIO (PAI-1)". A presente invenção provê compostos que agem como inibidores do inibidor-1 (PAI-1) de ativador de plasminogênio de fórmula (1), onde: R, R~ 1~, R~ 2~ e R~ 3~ são H, alquila, cicloalquila, -CH~ 2~-(cicloalquila), alcanoíla, halo, hidróxi, arila, arila substituída, heteroarila, heteroarila substituída, perfluoralquila, alcóxi, amino, -NH(alquila), -N(alquila)~ 2~, ou perfluoralcóxi; R~ 4~ é H, alquila, perfluoralquila, arila, arila substituída, heteroarila, heteroarila substituída, alquenila, alquenil-arila, arila, -CH~ 2~CR~ 5~, -CH(OH)R~ 5~, -C(O)R~ 5~, -CH(SH)R~ 5~, ou -G(S)R~ 5~; R~ 5~ é H, alquila, perfluoralquila, arila, arila substituída, heteroarila, heteroarila substituída, alquenila, alquenil-arila; R~ 6~ é H, alquila, cicloalquila, -CH~ 2~-cicloalquila, alquilarila, arila, arila substituída, heteroarila, ou heteroarila substituída; n é um número inteiro de 0-6; A é COOH, ou um imitador de ácido; ou sua forma de sal, ou éster farmaceuticamente aceitável, bem como composições farmacêuticas e métodos usando esses compostos para tratar, ou prevenir condições resultantes de distúrbios fibrinolíticos, tal como trombose da veia profunda e doença cardíaca coronária, e fibrose pulmonar, e processos para a preparação de tais compostos.
BR0210532-2A 2001-06-20 2002-06-18 Derivados de naftil benzofurano como inibidores do inibidor-1 de ativador de plasminogênio (pai-1) BR0210532A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US29970201P 2001-06-20 2001-06-20
PCT/US2002/019231 WO2003000671A1 (en) 2001-06-20 2002-06-18 Naphthyl benzofuran derivatives as inhibitors of plasminogen activator inhibitor-1 (pai-1)

Publications (1)

Publication Number Publication Date
BR0210532A true BR0210532A (pt) 2004-06-22

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ID=23155895

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BR0210532-2A BR0210532A (pt) 2001-06-20 2002-06-18 Derivados de naftil benzofurano como inibidores do inibidor-1 de ativador de plasminogênio (pai-1)

Country Status (10)

Country Link
US (1) US6599925B2 (pt)
EP (1) EP1401822A1 (pt)
JP (1) JP4476624B2 (pt)
CN (1) CN1308320C (pt)
AR (1) AR036100A1 (pt)
BR (1) BR0210532A (pt)
CA (1) CA2449844A1 (pt)
MX (1) MXPA03011400A (pt)
TW (1) TWI240723B (pt)
WO (1) WO2003000671A1 (pt)

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US7259182B2 (en) * 2002-12-10 2007-08-21 Wyeth Aryl, aryloxy, and aklyloxy substituted 1H-indol-3-yl glyoxylic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
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ATE331709T1 (de) * 2002-12-10 2006-07-15 Wyeth Corp Substituierte 3-carbonyl-1-yl essigsäure derivate als plasminogen aktivator inhibitor(pai-1) inhibitoren
BR0316583A (pt) * 2002-12-10 2005-10-04 Wyeth Corp Derivados de ácido acético 3-alquil e 3-arilalquil 1h-indol-1-il substituìdo como inibidores do inibidor-1 do ativador do plasminogênio (pai-1)
US7332521B2 (en) * 2003-09-25 2008-02-19 Wyeth Substituted indoles
US7265148B2 (en) * 2003-09-25 2007-09-04 Wyeth Substituted pyrrole-indoles
US7534894B2 (en) * 2003-09-25 2009-05-19 Wyeth Biphenyloxy-acids
US7141592B2 (en) * 2003-09-25 2006-11-28 Wyeth Substituted oxadiazolidinediones
US7342039B2 (en) * 2003-09-25 2008-03-11 Wyeth Substituted indole oximes
US7420083B2 (en) * 2003-09-25 2008-09-02 Wyeth Substituted aryloximes
US7268159B2 (en) * 2003-09-25 2007-09-11 Wyeth Substituted indoles
US7446201B2 (en) * 2003-09-25 2008-11-04 Wyeth Substituted heteroaryl benzofuran acids
US7582773B2 (en) * 2003-09-25 2009-09-01 Wyeth Substituted phenyl indoles
US7351726B2 (en) * 2003-09-25 2008-04-01 Wyeth Substituted oxadiazolidinediones
US7442805B2 (en) * 2003-09-25 2008-10-28 Wyeth Substituted sulfonamide-indoles
US7163954B2 (en) 2003-09-25 2007-01-16 Wyeth Substituted naphthyl benzothiophene acids
US7411083B2 (en) 2003-09-25 2008-08-12 Wyeth Substituted acetic acid derivatives
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EP1781641A1 (en) * 2004-08-23 2007-05-09 Wyeth Pyrrolo-naphthyl acids as pai-1 inhibitors
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TW200744585A (en) * 2006-02-27 2007-12-16 Wyeth Corp Inhibitors of PAI-1 for treatment of muscular conditions
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AU2007307597A1 (en) 2006-10-12 2008-04-17 Institute Of Medicinal Molecular Design. Inc. Carboxylic acid derivatives
CA2703494A1 (en) 2007-10-23 2009-04-30 Institute Of Medicinal Molecular Design, Inc. Inhibitor of pai-1 production
WO2009125606A1 (ja) 2008-04-11 2009-10-15 株式会社医薬分子設計研究所 Pai-1阻害剤
US8633245B2 (en) * 2008-04-11 2014-01-21 Institute Of Medicinal Molecular Design, Inc. PAI-1 inhibitor
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EP2959898A1 (en) * 2009-05-05 2015-12-30 Sloan-Kettering Institute for Cancer Research 4,5-DIOXO-NAPHTHO[1,2-b]FURANS AS SELECTIVE PEPTIDE DEFORMYLASE INHIBITORS
CN102850451B (zh) * 2011-06-29 2014-05-07 辽宁诺康生物制药有限责任公司 具有抑制纤溶酶活性的重组textilinin-1及其制备方法和应用
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CN106890324A (zh) * 2015-12-18 2017-06-27 深圳瑞健生命科学研究院有限公司 一种预防和治疗糖尿病肾病的方法
WO2018107702A1 (zh) 2016-12-15 2018-06-21 深圳瑞健生命科学研究院有限公司 一种治疗糖尿病的新方法
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EP1401822A1 (en) 2004-03-31
JP2004534824A (ja) 2004-11-18
CN1543456A (zh) 2004-11-03
US6599925B2 (en) 2003-07-29
MXPA03011400A (es) 2004-04-05
JP4476624B2 (ja) 2010-06-09
TWI240723B (en) 2005-10-01
CA2449844A1 (en) 2003-01-03
US20030018067A1 (en) 2003-01-23
WO2003000671A1 (en) 2003-01-03
AR036100A1 (es) 2004-08-11
CN1308320C (zh) 2007-04-04

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