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 trombinaInfo
- 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
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
- C07D241/38—Heterocyclic 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
- C07D241/40—Benzopyrazines
- C07D241/44—Benzopyrazines 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
-
- 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
- A61K31/495—Heterocyclic 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
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic 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
- C07D211/08—Heterocyclic 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
- C07D211/10—Heterocyclic 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
- C07D211/14—Heterocyclic 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
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/06—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 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.
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)
| 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)
| 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 |
-
1998
- 1998-12-15 KR KR1020007010842A patent/KR20010042298A/ko not_active Withdrawn
- 1998-12-15 HU HU0101470A patent/HUP0101470A3/hu unknown
- 1998-12-15 BR BR9815785-0A patent/BR9815785A/pt not_active Application Discontinuation
- 1998-12-15 AU AU19179/99A patent/AU1917999A/en not_active Abandoned
- 1998-12-15 PL PL98343321A patent/PL343321A1/xx not_active Application Discontinuation
- 1998-12-15 EP EP98963961A patent/EP1068190A1/en not_active Withdrawn
- 1998-12-15 WO PCT/US1998/026704 patent/WO1999050254A1/en not_active Ceased
- 1998-12-15 JP JP2000541158A patent/JP2002509923A/ja active Pending
- 1998-12-15 CA CA002319554A patent/CA2319554C/en not_active Expired - Fee Related
- 1998-12-15 IL IL13765598A patent/IL137655A0/xx unknown
-
1999
- 1999-03-30 ZA ZA9902447A patent/ZA992447B/xx unknown
-
2000
- 2000-08-03 US US09/601,606 patent/US6410536B1/en not_active Expired - Fee Related
- 2000-08-18 IS IS5589A patent/IS5589A/is unknown
- 2000-09-20 NO NO20004697A patent/NO20004697D0/no unknown
-
2002
- 2002-01-04 US US10/038,006 patent/US6916805B2/en not_active Expired - Fee Related
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. |