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1.发明授权
公开(公告)号：US5798442A
公开(公告)日：1998-08-25
申请号：US426547
申请日：1995-04-21
申请人： Michel Gallant , Marc Labelle , Yves Gareau , Donald W. Nicholson
发明人： Michel Gallant , Marc Labelle , Yves Gareau , Donald W. Nicholson
CPC分类号： C12N9/6475 , C07K5/0205 , C07K5/1021 , A61K38/00
摘要： Compounds having the formula I: R.sup.1 COAA.sup.1 AA.sup.2 AA.sup.3 NHY are inhibitors of apopain, an enzyme involved in the process of apoptosis. These compounds are useful as research tools as well as in the treatment of any condition in which reduced apoptosis would be beneficial, including immune deficiency syndromes (including AIDS), type I diabetes, pathogenic infections, cardiovascular and neurological injury, alopecia, aging, Parkinson's disease and Alzheimer's disease.
摘要翻译： 具有式I的化合物：R1COAA1AA2AA3NHY是凋亡过程的抑制剂，其是参与凋亡过程的酶。 这些化合物可用作研究工具以及用于治疗减少细胞凋亡有益的任何病症，包括免疫缺陷综合征（包括AIDS），I型糖尿病，致病性感染，心血管和神经损伤，脱发，衰老，帕金森病 疾病和阿尔茨海默病。
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2.发明授权Method for identifying inhibitors for apopain based upon the crystal structure of the apopain: Ac-DEVD-CHO complex 失效基于脱辅酶A的晶体结构鉴定胭脂蛋白的抑制剂的方法：Ac-DEVD-CHO复合物
公开(公告)号：US5834228A
公开(公告)日：1998-11-10
申请号：US800007
申请日：1997-02-13
申请人： Joseph W. Becker , Donald W. Nicholson , Jennifer Rotonda , Nancy A. Thornberry , Kimberly M. Fazil , Michel Gallant , Yves Gareau , Marc Labelle , Erin P. Peterson , Dita M. Rasper , Rejean Ruel , John P. Vaillancourt
发明人： Joseph W. Becker , Donald W. Nicholson , Jennifer Rotonda , Nancy A. Thornberry , Kimberly M. Fazil , Michel Gallant , Yves Gareau , Marc Labelle , Erin P. Peterson , Dita M. Rasper , Rejean Ruel , John P. Vaillancourt
CPC分类号： C12N9/6475 , C12Q1/37 , G01N2333/96466
摘要： The apopain:Ac-DEVD-CHO complex has been crystallized and its structure determined by x-ray crystallography. Based upon this crystal structure of the complex, a method for identifying inhibitors of apopain is presented which comprises designing putative inhibitors having specific contacts with apopain, making the putative inhibitors, and testing the putative inhibitors for their ability to inhibit apopain.
摘要翻译： 脱辅酶A-DEVD-CHO复合物已经结晶，其结构通过X射线晶体学测定。 基于复合物的这种晶体结构，提出了一种用于鉴定胭脂蛋白的抑制剂的方法，其包括设计具有与脯氨酸具有特异性接触的推定的抑制剂，制备推定的抑制剂，并测试推定的抑制剂以抑制胭脂蛋白的能力。
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3.发明授权Method of treatment using phenyl and biaryl derivatives as prostaglandin E inhibitors and compounds useful therefore 失效使用苯基和联芳基衍生物作为前列腺素E抑制剂和因此有用的化合物的治疗方法公开(公告)号：US06627656B2
公开(公告)日：2003-09-30
申请号：US09840942
申请日：2001-04-24
申请人： Michel Gallant , Nicolas Lachance , Marc Labelle , Robert Zamboni , Helene Juteau , Yves Gareau , Patrick Lacombe
发明人： Michel Gallant , Nicolas Lachance , Marc Labelle , Robert Zamboni , Helene Juteau , Yves Gareau , Patrick Lacombe
IPC分类号： A61K3121
CPC分类号： C07D213/64 , C07C57/38 , C07C59/68 , C07D213/55 , C07D333/24 , C07D333/34 , C07D409/12
摘要： This invention encompasses a method for the treatment or prevention of prostaglandin mediated diseases comprising administering to a mammalian patient a compound of formula I: in an amount that is effective to treat or prevent said prostaglandin mediated disease. Novel compounds are also disclosed.
摘要翻译： 本发明包括用于治疗或预防前列腺素介导的疾病的方法，包括向哺乳动物患者施用式I化合物：以有效治疗或预防所述前列腺素介导的疾病的量。 还公开了新的化合物。
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公开(公告)号：US5532237A
公开(公告)日：1996-07-02
申请号：US388929
申请日：1995-02-15
申请人： Michel Gallant , Yves Gareau , Daniel Guay , Marc Labelle , Petpiboon Prasit
发明人： Michel Gallant , Yves Gareau , Daniel Guay , Marc Labelle , Petpiboon Prasit
IPC分类号： C07D401/06 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/495 , A61K31/535 , A61P11/00 , A61P25/00 , A61P27/02 , A61P27/06 , A61P27/14 , A61P29/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D209/10 , C07D209/12 , C07D209/14 , C07D209/26 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06
CPC分类号： C07D209/14 , C07D209/26
摘要： Disclosed are indole derivatives having activity on the cannabinoid receptors and the methods of their preparation. The compounds are useful for lowering ocular intra ocular pressure and treating glaucoma because of the activity on the cannabinoid receptor.
摘要翻译： 公开了具有对大麻素受体的活性的吲哚衍生物及其制备方法。 由于大麻素受体的活性，这些化合物可用于降低眼内压和治疗青光眼。
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公开(公告)号：US5750539A
公开(公告)日：1998-05-12
申请号：US475139
申请日：1995-06-07
申请人： Yves Gareau , Claude Dufresne , Marc Labelle , James Yergey , Xin Xu , Deborah Nicoll-Griffith , Nathalie Chauret , Laird Trimble
发明人： Yves Gareau , Claude Dufresne , Marc Labelle , James Yergey , Xin Xu , Deborah Nicoll-Griffith , Nathalie Chauret , Laird Trimble
IPC分类号： C07D215/14 , A61K31/44 , A61K31/47 , A61P1/16 , A61P7/00 , A61P9/08 , A61P9/10 , A61P11/08 , A61P13/02 , A61P15/00 , A61P29/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D215/18 , C07D495/04 , C07D215/12
CPC分类号： C07D495/04 , C07D215/18
摘要： Compounds of Formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
摘要翻译： 式I的化合物：我是白三烯的作用的拮抗剂。 这些化合物可用作抗哮喘，抗过敏，抗炎和细胞保护剂。 它们也可用于治疗心绞痛，脑痉挛，肾小球肾炎，肝炎，内毒素血症，葡萄膜炎和同种异体移植排斥。
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公开(公告)号：US5472964A
公开(公告)日：1995-12-05
申请号：US260592
申请日：1994-06-16
申请人： Robert N. Young , Marc Labelle , Yves Leblanc , Yi B. Xiang , Cheuk K. Lau , Claude Dufresne , Yves Gareau
发明人： Robert N. Young , Marc Labelle , Yves Leblanc , Yi B. Xiang , Cheuk K. Lau , Claude Dufresne , Yves Gareau
IPC分类号： C07D513/04 , A61K31/44 , A61K45/06 , A61P11/06 , A61P27/02 , A61P29/00 , A61P37/08 , A61P43/00 , C07D491/04 , C07D491/048 , C07D495/04 , A61K31/435
CPC分类号： C07D491/04 , C07D495/04 , C07D513/04
摘要： Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
摘要翻译： 具有式I的化合物：I是白三烯的作用的拮抗剂。 这些化合物可用作抗哮喘，抗过敏，抗炎和细胞保护剂。 它们也可用于治疗心绞痛，脑痉挛，肾小球肾炎，肝炎，内毒素血症，葡萄膜炎和同种异体移植排斥。
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公开(公告)号：US06211197B1
公开(公告)日：2001-04-03
申请号：US09411505
申请日：1999-10-04
申请人： Michel Belley , Marc Labelle , Nicholas Lachance , Michel Gallant , Nathalie Chauret , Laird A. Trimble , Chun Li
发明人： Michel Belley , Marc Labelle , Nicholas Lachance , Michel Gallant , Nathalie Chauret , Laird A. Trimble , Chun Li
IPC分类号： A61K31192
CPC分类号： C07D257/04 , C07C59/64 , C07C59/66 , C07C59/68 , C07C62/34 , C07C309/10 , C07C311/51 , C07C323/60 , C07C323/62 , C07D215/18 , C07D215/36 , C07D285/135 , C07D307/79 , C07D317/60 , C07D333/28 , C07D333/34
摘要： Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed. The compounds are represented by formula II: Ar1—W—Ar2—X—Q II The compounds of the invention are structurally different from NSAIDs and opiates, and are antagonists of the pain and inflammatory effects of E-type prostaglandins.
摘要翻译： 公开了用于治疗前列腺素介导的疾病的化合物和方法及其某些药物组合物。 化合物由式II表示：本发明的化合物在结构上不同于NSAID和阿片剂，并且是E型前列腺素的疼痛和炎症作用的拮抗剂。
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公开(公告)号：US20170369444A1
公开(公告)日：2017-12-28
申请号：US15129351
申请日：2015-03-30
发明人： Marc Labelle , Rui Zhang , Cuthbert D. Martyr , Neerja Saraswat , Thomas Boesen
IPC分类号： C07D213/79 , C07D471/04 , C07D417/12 , C07D405/12 , C07D237/24 , C07D401/12 , C07D401/06 , C07D239/28 , C07D487/04 , C07D409/12
CPC分类号： C07D213/79 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K45/06 , C07D213/38 , C07D213/48 , C07D213/56 , C07D237/24 , C07D239/28 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D417/12 , C07D471/04 , C07D487/04 , A61K2300/00
摘要： Compounds of the form in which Q is selected from —COOH—CH═NR12, —W, —CH2NHR13, —CH=0 and —CH(OR17)2 capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer and formulations and methods of use of such compounds.
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公开(公告)号：US08426358B2
公开(公告)日：2013-04-23
申请号：US13087261
申请日：2011-04-14
申请人： Frank Kayser , Marc Labelle , Bei Shan , Jian Zhang , Mingyue Zhou
发明人： Frank Kayser , Marc Labelle , Bei Shan , Jian Zhang , Mingyue Zhou
CPC分类号： C12N9/1029 , A61K31/497 , A61K38/45 , C07D403/12 , C07D417/12
摘要： The invention provides compounds, pharmaceutical compositions and methods for treating atherosclerosis, inflammation, thrombosis and other conditions and for decreasing or prevention of accumulation of cholesterol in a subject by modifying LCAT polypeptide.
摘要翻译： 本发明提供了通过改变LCAT多肽来治疗动脉粥样硬化，炎症，血栓形成和其它病症并降低或预防受试者胆固醇积聚的化合物，药物组合物和方法。
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公开(公告)号：US20050043330A1
公开(公告)日：2005-02-24
申请号：US10928784
申请日：2004-08-26
申请人： Michelle Browner , David Clark , Timothy Cushing , Xiaolin Hao , Ronald Hawley , Xiao He , Juan Jaen , Sharada Labadie , Marie-Louise Smith , Francisco Talamas , Nigel Walker , Marc Labelle
发明人： Michelle Browner , David Clark , Timothy Cushing , Xiaolin Hao , Ronald Hawley , Xiao He , Juan Jaen , Sharada Labadie , Marie-Louise Smith , Francisco Talamas , Nigel Walker , Marc Labelle
IPC分类号： A61K31/4709 , A61K31/4745 , A61K31/5377 , A61P3/10 , A61P17/06 , A61P19/02 , A61P29/00 , A61P31/04 , A61P35/00 , A61P43/00 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/04 , C07D471/04 , C12N15/25 , C12N15/28 , A61K31/519 , A61K31/517 , C07D487/02 , C07D43/02
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D417/04 , C07D471/04
摘要： Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic and cell proliferative conditions or diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism and cell proliferation. The subject compounds contain fused carbocyclic or heterocyclic rings.
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