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BR9815785A - Quinoxalinonas como inibidores de protease de serina tal como fator xa e trombina - Google Patents

Quinoxalinonas como inibidores de protease de serina tal como fator xa e trombina

Info

Publication number
BR9815785A
BR9815785A BR9815785-0A BR9815785A BR9815785A BR 9815785 A BR9815785 A BR 9815785A BR 9815785 A BR9815785 A BR 9815785A BR 9815785 A BR9815785 A BR 9815785A
Authority
BR
Brazil
Prior art keywords
factor
quinoxalinones
thrombin
protease inhibitors
prodrugs
Prior art date
Application number
BR9815785-0A
Other languages
English (en)
Inventor
Danette Andrea Dudley
Jeremy John Edmunds
Original Assignee
Warner Lambert Co
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 Warner Lambert Co filed Critical Warner Lambert Co
Publication of BR9815785A publication Critical patent/BR9815785A/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40Benzopyrazines
    • C07D241/44Benzopyrazines 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 carbon atoms of the hetero ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/14Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Patente de Invenção: <B>"QUINOXALINONAS COMO INIBIDORES DE PROTEASE DE SERINA TAL COMO FATOR XA E TROMBINA"<D>. Esta invenção descreve quinoxalinonas de acordo com a Fórmula (I) ou seus estereoisómeros ou sais farmaceuticamente aceitáveis, ésteres, amidas ou pró-drogas, que mostram efeito de inibição sobre as proteases de serina tal como fator Xa, trombina e/ou fator VIIa. A invenção também descreve sais e pró-drogas dos compostos farmaceuticamente aceitáveis, composições farmaceuticamente aceitáveis compreendendo os compostos, seus sais ou pró-drogas, e métodos de uso deles como agentes terapêuticos para o tratamento ou prevenção de estados de doença em mamíferos caracterizados por trombose anormal.
BR9815785-0A 1998-03-31 1998-12-15 Quinoxalinonas como inibidores de protease de serina tal como fator xa e trombina BR9815785A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US8004298P 1998-03-31 1998-03-31
PCT/US1998/026704 WO1999050254A1 (en) 1998-03-31 1998-12-15 Quinoxalinones as serine protease inhibitors such as factor xa and thrombin

Publications (1)

Publication Number Publication Date
BR9815785A true BR9815785A (pt) 2000-12-05

Family

ID=22154891

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9815785-0A BR9815785A (pt) 1998-03-31 1998-12-15 Quinoxalinonas como inibidores de protease de serina tal como fator xa e trombina

Country Status (14)

Country Link
US (2) US6410536B1 (pt)
EP (1) EP1068190A1 (pt)
JP (1) JP2002509923A (pt)
KR (1) KR20010042298A (pt)
AU (1) AU1917999A (pt)
BR (1) BR9815785A (pt)
CA (1) CA2319554C (pt)
HU (1) HUP0101470A3 (pt)
IL (1) IL137655A0 (pt)
IS (1) IS5589A (pt)
NO (1) NO20004697D0 (pt)
PL (1) PL343321A1 (pt)
WO (1) WO1999050254A1 (pt)
ZA (1) ZA992447B (pt)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6291514B1 (en) 1998-02-09 2001-09-18 3-Dimensional Pharmaceuticals, Inc. Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors
AU3127900A (en) * 1998-12-23 2000-07-31 Du Pont Pharmaceuticals Company Thrombin or factor xa inhibitors
IL144560A0 (en) * 1999-02-09 2002-05-23 Dimensional Pharm Inc Heteroaryl amidine and guanidine derivatives and pharmaceutical compositions containing the same
SE9902202D0 (sv) * 1999-06-10 1999-06-10 Astra Ab Production of aggregates
AU2001234690A1 (en) 2000-02-01 2001-08-14 Cor Therapeutics, Inc. 2-(1h)-quinolone and 2-(1h)-quinoxalone inhibitors of factor xa
HUE025683T2 (hu) 2002-12-03 2016-04-28 Pharmacyclics Llc VIIA faktor inhibitor 2-(2-hidroxi-bifenil-3-il)-1H-benzoimidazol-5-karboxamidin-származékok
TWI289141B (en) 2003-03-11 2007-11-01 Hoffmann La Roche F. Ag. Quinolinone derivatives and uses thereof
CA2521621C (en) * 2003-04-15 2011-11-01 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
US7250447B2 (en) * 2003-05-20 2007-07-31 Genentech, Inc. Acylsulfamide inhibitors of factor VIIa
US7273886B2 (en) * 2003-05-20 2007-09-25 Genentech, Inc. Benzofuran inhibitors of factor VIIa
WO2005105098A2 (de) * 2004-05-05 2005-11-10 Immunopharm Aktiengesellschaft Präparat zur behandlung von krebs
DE102004023332A1 (de) * 2004-05-12 2006-01-19 Bayer Cropscience Gmbh Chinoxalin-2-on-derivate, diese enthaltende nutzpflanzenschützende Mittel und Verfahren zu ihrer Herstellung und deren Verwendung
BRPI0513386A (pt) * 2004-08-09 2008-05-06 Warner Lambert Co inibidores de reabsorção de norepinefrina de quinoxalinona para o tratamento de distúrbios do sistema nervoso central
EP1776964A4 (en) * 2004-08-11 2009-08-19 Kowa Co METHOD FOR THE PREVENTION AND TREATMENT OF BRAIN INFARC
AP2007003973A0 (en) * 2004-10-12 2007-07-30 Glenmark Pharmaceuticals Sa Novel dideptidyl peptidase IV inhibitors, pharmaceutical compositions containing them, and proces for their preparation
US7893066B2 (en) 2006-10-05 2011-02-22 Gilead Palo Alto, Inc. Pyridol[2,3-B]pyrazinones for use as stearoyl CoA desaturase inhibitors
WO2008043087A2 (en) 2006-10-05 2008-04-10 Cv Therapeutics, Inc. Bicyclic nitrogen-containing heterocyclic compounds for use as stearoyl coa desaturase inhibitors
US7662819B2 (en) 2007-04-09 2010-02-16 Gilead Palo Alto, Inc. Pteridinone derivatives for use as stearoyl CoA desaturase inhibitors
NZ580801A (en) * 2007-05-10 2012-09-28 Bristol Myers Squibb Co Aryl- and heteroaryl-substituted tetrahydrobenzo-1,4-diazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
JP5554709B2 (ja) 2007-08-31 2014-07-23 パーデュー、ファーマ、リミテッド、パートナーシップ 置換キノキサリンタイプピペリジン化合物とその使用
WO2009109258A1 (en) * 2008-03-05 2009-09-11 Merck Patent Gmbh Quinoxalinone derivatives as insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes
AU2009230130A1 (en) * 2008-03-26 2009-10-01 Daiichi Sankyo Company, Limited Hydroxyquinoxalinecarboxamide derivative
WO2009126123A1 (en) * 2008-04-10 2009-10-15 Cv Therapeutics Inc. Bicyclic nitrogen containing heterocyclic compounds for use as stearoyl coa desaturase inhibitors
WO2010010458A1 (en) 2008-07-21 2010-01-28 Purdue Pharma L.P. Substituted-quinoxaline-type bridged-piperidine compounds and the uses thereof
ES2613631T3 (es) 2010-12-22 2017-05-25 Purdue Pharma L.P. Compuestos de piperidina de tipo quinoxalina sustituidos con fósforo y usos de los mismos
JP2015501793A (ja) 2011-11-10 2015-01-19 オーエスアイ・ファーマシューティカルズ,エルエルシー ジヒドロプテリジノン類
JP2014533744A (ja) 2011-12-01 2014-12-15 パーデュー、ファーマ、リミテッド、パートナーシップ アゼチジン置換キノキサリンタイプピペリジン化合物とその使用
US9085561B2 (en) 2012-07-30 2015-07-21 Purdue Pharma L.P. Cyclic urea- or lactam-substituted quinoxaline-type piperidines as ORL-1 modulators
US9951038B2 (en) 2012-12-27 2018-04-24 Purdue Pharma L.P. Quinazolin-4(3H)-one-type piperidine compounds and uses thereof
US9040533B2 (en) 2012-12-27 2015-05-26 Purdue Pharma L.P. Oxime-substituted-quinoxaline-type piperidine compounds as ORL-1 modulators
US9090618B2 (en) 2012-12-27 2015-07-28 Purdue Pharma L.P. Substituted benzimidazole-type piperidine compounds and uses thereof
WO2014102588A2 (en) 2012-12-27 2014-07-03 Purdue Pharma L.P. Indole and indoline-type piperidine compounds and uses thereof
CN108137514A (zh) * 2015-07-30 2018-06-08 百时美施贵宝公司 芳基取代的二环杂芳基化合物
BR112018012934B1 (pt) * 2015-12-24 2023-11-07 The Regents Of The University Of California Reguladores cftr e métodos de uso dos mesmos
JP6938510B2 (ja) 2015-12-24 2021-09-22 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア Cftr制御因子及びこの使用方法
KR102723194B1 (ko) 2015-12-24 2024-10-28 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 Cftr 조절제 및 이의 사용 방법
DE102017005089A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substitulerte 3,4-Dihydrochinoxalin-2(1H)-one
DE102017005091A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one
AU2018321926B2 (en) 2017-08-24 2023-09-21 The Regents Of The University Of California Ocular pharmaceutical compositions
US20240287022A1 (en) * 2021-06-28 2024-08-29 Merck Sharp & Dohme Llc Il4i1 inhibitors and methods of use

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4082735A (en) 1976-04-26 1978-04-04 Syntex (U.S.A.) Inc. Novel immunological adjuvant compounds and methods of preparation thereof
US4082736A (en) 1976-04-26 1978-04-04 Syntex (U.S.A.) Inc. Novel immunological adjuvant compounds and methods of preparation thereof
JPS63145272A (ja) 1986-12-09 1988-06-17 Morishita Seiyaku Kk 4,5−ジヒドロ−6−(4−置換フエニル)−3(2h)−ピリダジノン誘導体
JPS63301874A (ja) * 1987-03-27 1988-12-08 Fujisawa Pharmaceut Co Ltd キノキサリン誘導体およびその製造法
JPH0276860A (ja) * 1987-10-05 1990-03-16 Toyo Jozo Co Ltd 6−置換アルコキシ−2−オキソ−1,2−ジヒドロキノキサリン誘導体
JPH01254348A (ja) 1988-04-01 1989-10-11 Matsushita Electric Ind Co Ltd 成形用型
HUT76640A (en) 1995-08-17 1997-10-28 Chinoin Gyogyszer Es Vegyeszet Compounds of pharmaceutical activity cyclic amide derivatives, pharmaceutical compositions containing them, process for producing them and their use
US6124291A (en) * 1996-06-18 2000-09-26 Warner-Lambert Company Pyrrolo[1,2-a]pyrazine-1,4-dione serine protease inhibitors
WO1998001428A1 (en) * 1996-07-08 1998-01-15 Du Pont Pharmaceuticals Company AMIDINOINDOLES, AMIDINOAZOLES, AND ANALOGS THEREOF AS INHIBITORS OF FACTOR Xa AND OF THROMBIN
TW472045B (en) * 1996-09-25 2002-01-11 Astra Ab Protein kinase C inhibitor compounds, method for their preparation, pharmaceutical composition thereof and intermediate used for their preparation
GB2324729B (en) 1997-04-30 2002-01-02 Bradford Hospitals Nhs Trust Lung treatment device

Also Published As

Publication number Publication date
AU1917999A (en) 1999-10-18
NO20004697L (no) 2000-09-20
IL137655A0 (en) 2001-10-31
US6410536B1 (en) 2002-06-25
CA2319554C (en) 2005-06-28
NO20004697D0 (no) 2000-09-20
KR20010042298A (ko) 2001-05-25
CA2319554A1 (en) 1999-10-07
IS5589A (is) 2000-08-18
JP2002509923A (ja) 2002-04-02
WO1999050254A1 (en) 1999-10-07
HUP0101470A3 (en) 2002-09-30
ZA992447B (en) 2000-10-10
US20020086866A1 (en) 2002-07-04
US6916805B2 (en) 2005-07-12
PL343321A1 (en) 2001-08-13
EP1068190A1 (en) 2001-01-17
HUP0101470A2 (hu) 2001-10-28

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Legal Events

Date Code Title Description
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B15K Others concerning applications: alteration of classification

Free format text: ALTERADA DE INT.CL.8: C07D 241/44, C07D 211/12, C07D 15/04, A61K 31/498, A61K 31/435, A61P 7/02

Ipc: C07D 241/44 (2008.04), C07D 211/12 (2008.04), C07C

B09B Patent application refused [chapter 9.2 patent gazette]

Free format text: INDEFIRO O PRESENTE PEDIDO DE PATENTE DE ACORDO COM ART. 8O DA LPI.

B09B Patent application refused [chapter 9.2 patent gazette]

Free format text: MANTIDO O INDEFERIMENTO UMA VEZ QUE NAO FOI APRESENTADO RECURSO DENTRO DO PRAZO LEGAL.