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1.发明公开2-(PHENYL OR HETEROCYCLIC)-1H-PHENANTRHO[9,10-D]IMIDAZOLES AS MPGES-1 INHIBITORS 有权2-（苯基或杂环基）-1H- PHENANTRO [9,10，D〕咪唑ALS的mPGES-1抑制剂
公开(公告)号：EP1828143A1
公开(公告)日：2007-09-05
申请号：EP05823957.5
申请日：2005-12-15
发明人： CHAU, Anh , COTE, Bernard , DUCHARME, Yves , FRENETTE, Richard , FRIESEN, Richard , GAGNON, Marc , GIROUX, Andre , MARTINS, Evelyn , YU, Hongping , WU, Tom
IPC分类号： C07D235/02 , C07D403/04 , C07D401/04 , A61K31/4164 , A61K31/4439
CPC分类号： C07D401/14 , C07D235/02 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D413/06
摘要： The invention encompasses novel compounds of Formula I INSERT FORMULA I FROM CLAIM 1 or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.
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2.发明公开HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开杂芳族化合物AS硬脂酰 - 辅酶A-Δ9去饱和酶的抑制剂
公开(公告)号：EP1910352A1
公开(公告)日：2008-04-16
申请号：EP06761137.6
申请日：2006-07-18
发明人： BLACK, Cameron , DESCHENES, Denis , GAGNON, Marc , LACHANCE, Nicolas , LEBLANC, Yves , LEGER, Serge , LI, Chun, Sing , OBALLA, Renata, M.
IPC分类号： C07D417/14 , A61P3/06 , A61K31/501 , A61P3/10 , C07D413/14
CPC分类号： C07D413/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D417/14 , C07D471/04 , C07F9/65583
摘要： Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; lipid disorders; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and fatty liver disease.
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3.发明公开
公开(公告)号：EP1989187A1
公开(公告)日：2008-11-12
申请号：EP07719387.8
申请日：2007-02-22
发明人： CHAU, Anh , COTE, Bernard , DUCHARME, Yves , FRENETTE, Richard , FRIESEN, Richard , GAGNON, Marc , GIROUX, Andre , MARTINS, Evelyn , YU, Hongping , HAMEL, Pierre
IPC分类号： C07D235/02 , A61K31/4184
CPC分类号： C07D235/02 , C07D401/04 , C07D403/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04
摘要： The invention encompasses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.
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4.发明授权2-(PHENYL OR HETEROCYCLIC)-1H-PHENANTRHO[9,10-D]IMIDAZOLES AS MPGES-1 INHIBITORS 有权2-（苯基或杂环基）-1H- PHENANTRO [9,10，D〕咪唑ALS的mPGES-1抑制剂
公开(公告)号：EP1828143B1
公开(公告)日：2013-03-20
申请号：EP05823957.5
申请日：2005-12-15
发明人： CHAU, Anh , COTE, Bernard , DUCHARME, Yves , FRENETTE, Richard , FRIESEN, Richard , GAGNON, Marc , GIROUX, Andre , MARTINS, Evelyn , YU, Hongping , WU, Tom
IPC分类号： C07D235/02 , C07D403/04 , C07D401/04 , A61K31/4164 , A61K31/4439
CPC分类号： C07D401/14 , C07D235/02 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D413/06
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5.发明公开[1,2,3]TRIAZOLYL SUBSTITUTED QUINOLINES AND COUMARINS AS INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS 有权[1,2,3] - 三唑基 - 取代CHINO LINE AND AS香豆素白三烯生物合成抑制剂
公开(公告)号：EP2118093A1
公开(公告)日：2009-11-18
申请号：EP08714553.8
申请日：2008-02-05
发明人： DUCHARME, Yves , FRENETTE, Richard , FRIESEN, Richard , GAGNON, Marc , GAREAU, Yves , GRIMM, Erich, L. , JUTEAU, Helene , LALIBERTE, Sebastien , MACKAY, Bruce
IPC分类号： C07D405/06 , A61K31/4192 , A61K31/422 , A61K31/427 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61P11/06 , A61P29/00 , A61P37/08 , A61P9/10 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
CPC分类号： C07D401/06 , C07D401/14 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The instant invention provides compounds of Formula (I) which are leukotriene biosynthesis inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
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6.发明公开AZACYCLOALKANE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开作为硬脂酰辅酶A-9去饱和酶抑制剂的AZACYCLOALKANE衍生物
公开(公告)号：EP2076509A1
公开(公告)日：2009-07-08
申请号：EP07816009.0
申请日：2007-10-18
发明人： OBALLA, Renata M. , DESCHENES, Denis , GAGNON, Marc , LEBLANC, Yves , POWELL, David , RAMTOHUL, Yeeman K.
IPC分类号： C07D401/14 , A61K31/4545 , A61K31/501 , A61K31/506 , A61K31/53 , A61P3/04 , A61P3/06 , C07D413/14 , C07D417/14
CPC分类号： C07D413/14 , C07D401/14 , C07D417/14
摘要： Azacycloalkane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
摘要翻译： 结构式（I）的氮杂环烷烃衍生物相对于其他已知的硬脂酰辅酶A去饱和酶是硬脂酰 - 辅酶A-9去饱和酶（SCD1）的选择性抑制剂。 本发明化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 糖尿病; 神经疾病; 代谢综合征; 胰岛素抵抗; 和肝脂肪变性。
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7.发明公开CYCLIC AMINE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开环胺衍生物作为抑制剂硬脂酰辅酶A DELTA-9脱氢酶
公开(公告)号：EP2027121A1
公开(公告)日：2009-02-25
申请号：EP07719836.4
申请日：2007-05-22
发明人： LEBLANC, Yves , GAGNON, Marc
IPC分类号： C07D417/10 , A61K31/4523 , A61P3/00 , C07D413/10
CPC分类号： C07D413/10 , C07D417/10
摘要： Cyclic amine derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
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8.发明公开2-(PHENYL OR HETEROCYCLIC)-1H-PHENANTRHO(9,10-D)IMIDAZOLES AS MPGES-1 INHIBITORS 有权2-（苯基或杂环基）-1H-菲并（9,10-D）咪唑ALS的mPGES-1抑制剂
公开(公告)号：EP1954683A1
公开(公告)日：2008-08-13
申请号：EP06817652.8
申请日：2006-11-21
发明人： CHAU, Anh , COTE, Bernard , DUCHARME, Yves , FRENETTE, Richard , FRIESEN, Richard , GAGNON, Marc , GIROUX, Andre , MARTINS, Evelyn , YU, Hongping , WU, Tom
IPC分类号： C07D235/02 , A61K31/4184 , C07D401/04 , C07D401/06 , C07D405/06 , C07D413/06
CPC分类号： C07D235/02 , C07D235/18 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D413/04 , C07D413/06
摘要： The invention encompasses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.
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9.发明公开THIADIAZOLE SUBSTITUTED COUMARIN DERIVATIVES AND THEIR USE AS LEUKOTRIENE BIOSYNTHESIS INHIBITOR 有权噻二唑取代的香豆素衍生物及其作为白三烯生物合成抑制剂的用途
公开(公告)号：EP1869031A1
公开(公告)日：2007-12-26
申请号：EP06741360.9
申请日：2006-03-21
发明人： BLOUIN, Marc , GRIMM, Erich, L. , GAREAU, Yves , GAGNON, Marc , JUTEAU, Helene , LALIBERTE, Sebastien , MACKAY, Bruce , FRIESEN, Richard
IPC分类号： C07D413/12 , C07D417/12 , A61K31/4245 , A61P19/02 , A61K31/433
CPC分类号： C07D417/14 , C07D413/12 , C07D417/12
摘要： The instant invention provides compounds of Formula (Ia) which are leukotriene biosynthesis inhibitors, wherein X is O or S, Y is O, S, -NR6-CHR7- or -NR8-C(O)- and A is selected from 5-membered aromatic heterocyclic ring, 6-membered aromatic heterocyclic ring, naphthelenic or heterobicyclic aromatic ring system, phenyl and benzyl. A is optionally mono- or disubstituted. Compounds of Formula (Ia) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
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