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1. 发明授权

EP0434095B1 Phenylacetonitrilealkylaminoalkyl-ortho-substituted aryl compounds as immunosuppressives 失效
标题翻译：苯基乙腈烷基氨基烷基 - 邻位取代的芳基化合物作为免疫抑制剂
公开(公告)号：EP0434095B1
公开(公告)日：1994-02-02
申请号：EP90125245.2
申请日：1990-12-21
申请人： G.D. Searle & Co.
发明人： Liang, Chi-Dean , McKearn, John P. , Farah, John M. Jr. , Mueller, Richard A.
IPC分类号： C07C255/43 , A61K31/275
CPC分类号： C07C255/43

2. 发明公开

EP0434095A1 Phenylacetonitrilealkylaminoalkyl-ortho-substituted aryl compounds as immunosuppressives 失效
标题翻译：苯基丙酮烷基氨基烷基 - （邻位取代基）-Arylverbindungen als Immunosupressoren。
公开(公告)号：EP0434095A1
公开(公告)日：1991-06-26
申请号：EP90125245.2
申请日：1990-12-21
申请人： G.D. Searle & Co.
发明人： Liang, Chi-Dean , McKearn, John P. , Farah, John M. Jr. , Mueller, Richard A.
IPC分类号： C07C255/43 , A61K31/275
CPC分类号： C07C255/43
摘要： A class of substituted phenylacetonitrilealkylaminoalkyl-ortho-substituted aryl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases. Compounds of particular interest are of the formula

wherein m is one or two; wherein n is a number selected from one to five, inclusive; wherein R¹ is selected from hydrido, alkyl, hydroxyalkyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkenyl and alkynyl; wherein R⁶ is selected from loweralkyl;
wherein each of R⁸, R⁹, R¹⁰ and R¹² through R¹⁶ is independently selected from hydrido, hydroxy, alkyl, hydroxyalkyl, alkoxy, alkenyl, alkynyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonylalkenyl, alkylaminocarbonyl and alkoxyalkyl; with the proviso that at least one of R¹² and R¹⁶ must be selected from hydroxy, alkyl, hydroxyalkyl, alkoxy, alkenyl, alkynyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonylalkenyl, alkylaminocarbonyl and alkoxyalkyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类具有免疫抑制特性的取代苯基乙腈烷基氨基烷基邻位取代芳基化合物。该类化合物可用于减少移植器官的受体排斥和治疗自身免疫性或炎性疾病。特别感兴趣的化合物具有式CHEM，其中m是一个或两个; 其中n是选自1至5的数字，包括1和5; 其中R 1选自氢，烷基，羟基烷基，环烷基，环烷基烷基，烷氧基烷基，烯基和炔基; 其中R 6选自低级烷基; 其中R 8，R 9，R 1和R 2至R 6中的每一个独立地选自氢，羟基，烷基，羟基烷基，烷氧基，烯基，炔基，烷基羰基，烷氧基羰基，烷基羰基烯基，烷基氨基羰基和烷氧基烷基; 条件是R 1和R 2中的至少一个必须选自羟基，烷基，羟基烷基，烷氧基，烯基，炔基，烷基羰基，烷氧基羰基，烷基羰基烯基，烷基氨基羰基和烷氧基烷基; 或其互变异构体或其药学上可接受的盐。

3. 发明公开

EP0204309A3 Substituted N-benzyl-4(benzhydryl) piperidines 失效
标题翻译：取代的N-BENZYL-4（苯甲酰基）哌啶
公开(公告)号：EP0204309A3
公开(公告)日：1988-09-14
申请号：EP86107507
申请日：1986-06-03
申请人： G.D. Searle & Co.
发明人： Rorig, Kurt Joachim , Djuric, Steven Wakefield , Fowler, Kerry Wallace , Liang, Chi-Dean
IPC分类号： C07D211/94 , A61K31/445 , C07D211/14 , C07D211/18
CPC分类号： C07D211/94 , C07D211/14 , C07D211/18 , Y02P20/582
摘要： The invention relates to compounds of the formula:
and the pharmaceutically acceptable salts thereof wherein Ar are the same or different and represent phenyl or halogen substituted phenyl; R is selected from lower alkoxy, or di (lower alkyl) amino; R 1 is selected from hydrogen, lower alkoxy-carbonyl, carboxy, or lower alkylaminocarbonyl; and n is 0 or 1 provided that when R is hydrogen n is 1. Said compounds are useful cardiovascular agents.

4. 发明授权

EP0219813B1 Bicyclo-substituted phenylacetonitrile derivatives 失效
标题翻译：双羟基取代的苯乙酮衍生物
公开(公告)号：EP0219813B1
公开(公告)日：1989-08-16
申请号：EP86114319.6
申请日：1986-10-16
申请人： G.D. Searle & Co.
发明人： Liang, Chi-Dean
IPC分类号： C07C121/78 , A61K31/275
CPC分类号： C07C255/00

5. 发明授权

EP0183216B1 N-(Aralkoxybenzyl)-4(benzhydryl) piperidines 失效
标题翻译： N-（ARALKOXYBENZYL）-4（BENZHYDRYL）PIPERIDINES
公开(公告)号：EP0183216B1
公开(公告)日：1989-07-19
申请号：EP85114929.4
申请日：1985-11-25
申请人： G.D. Searle & Co.
发明人： Rorig, Kurt Joachim , Liang, Chi-Dean , Hamilton, Robert Wallis
IPC分类号： C07D211/14 , C07D211/18 , A61K31/445
CPC分类号： C07D211/18 , C07D211/14

6. 发明公开

EP0219813A1 Bicyclo-substituted phenylacetonitrile derivatives 失效
标题翻译：苯并噻唑酮。
公开(公告)号：EP0219813A1
公开(公告)日：1987-04-29
申请号：EP86114319.6
申请日：1986-10-16
申请人： G.D. Searle & Co.
发明人： Liang, Chi-Dean
IPC分类号： C07C121/78 , A61K31/275
CPC分类号： C07C255/00
摘要： The invention relates to compounds of the formula:
which are useful cardiovascular agents.
摘要翻译：本发明涉及下式的化合物：，它们是有用的心血管药。 [R

7. 发明公开

EP0183216A1 N-(Aralkoxybenzyl)-4(benzhydryl) piperidines 失效
标题翻译：的N- Aralkoxybenzyl-4-二苯甲基 - 哌啶。
公开(公告)号：EP0183216A1
公开(公告)日：1986-06-04
申请号：EP85114929.4
申请日：1985-11-25
申请人： G.D. Searle & Co.
发明人： Rorig, Kurt Joachim , Liang, Chi-Dean , Hamilton, Robert Wallis
IPC分类号： C07D211/14 , C07D211/18 , A61K31/445
CPC分类号： C07D211/18 , C07D211/14
摘要： The invention relates to compounds of the formula:
which are useful cardiovascular agents. BACKGROUND OF THE INVENTION
The present invention provides novel compounds of formula I

8. 发明公开

EP1221441A2 LTA4 Hydrolase inhibitors 失效
标题翻译： LTA4水解酶抑制剂
公开(公告)号：EP1221441A2
公开(公告)日：2002-07-10
申请号：EP02006764.1
申请日：1995-10-10
申请人： G.D. SEARLE & CO.
发明人： Chandrakumar, Nizal Samuel , Chen, Barbara Baosheng , Clare, Michael , Desai, Bipinchandra Nanubhai , Djuric, Steven Wakefield , Docter, Stephan Hermann , Gasiecki, Alan Frank , Haack, Richard Arthur , Liang, Chi-Dean , Miyashiro, Julie Marion , Penning, Thomas Dale , Russell, Mark Andrew , Yu, Stella Siu-tzyy
IPC分类号： C07D295/08 , C07D295/22 , C07D277/34 , C07D209/12 , C07D417/12 , A61K31/33 , C07C217/16 , C07D213/30 , C07D401/12 , C07D211/46 , A61P43/00 , C07C237/06 , C07D215/14 , C07D211/62 , C07D451/02 , C07C229/12 , C07D295/20 , C07D333/16 , C07D207/16 , C07D491/04 , C07D277/24
CPC分类号： C07D295/185 , C07C217/16 , C07C229/12 , C07C237/06 , C07D277/24 , C07D295/088 , C07D295/215 , C07D295/26
摘要： The present invention provides compounds of the formula Ar 1 -Q-Ar 2 -Y-R-Z and pharmaceutically acceptable salts thereof wherein Ar 1 and Ar 2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB 4 production, such as proriasis, ulcerative colitis, IBD and asthma.
摘要翻译：本发明提供式Ar 1 -Q-Ar 2 -YRZ的化合物及其药学上可接受的盐，其中Ar 1和Ar 2是任选取代的芳基，Z是任选取代的含氮部分，其可以是无环，环状或双环胺或任选取代的单环或双环含氮杂芳基部分; Q是能够连接两个芳基的连接基团; R是亚烷基部分; Y是能够将芳基连接到亚烷基部分并且其中Z通过氮原子与R键合的连接部分。本发明的化合物和药物组合物可用于治疗由LTB4产生介导的炎性疾病，例如胎盘is is，溃疡性结肠炎，IBD和哮喘。

9. 发明公开

EP0204309A2 Substituted N-benzyl-4(benzhydryl) piperidines 失效
标题翻译：取代的N-苄基-4-（二苯甲基） - 哌啶。
公开(公告)号：EP0204309A2
公开(公告)日：1986-12-10
申请号：EP86107507.5
申请日：1986-06-03
申请人： G.D. Searle & Co.
发明人： Rorig, Kurt Joachim , Djuric, Steven Wakefield , Fowler, Kerry Wallace , Liang, Chi-Dean
IPC分类号： C07D211/94 , A61K31/445 , C07D211/14 , C07D211/18
CPC分类号： C07D211/94 , C07D211/14 , C07D211/18 , Y02P20/582
摘要： The invention relates to compounds of the formula:
and the pharmaceutically acceptable salts thereof wherein Ar are the same or different and represent phenyl or halogen substituted phenyl; R is selected from lower alkoxy, or di (lower alkyl) amino; R 1 is selected from hydrogen, lower alkoxy-carbonyl, carboxy, or lower alkylaminocarbonyl; and n is 0 or 1 provided that when R is hydrogen n is 1.
Said compounds are useful cardiovascular agents.

10. 发明公开

EP0194665A1 beta-Adrenergic receptor agonist alkylaminoalkyl pyridinemethanol derivatives 失效
标题翻译：烷基氨基烷基吡啶甲醇助剂alsβ-adrenerge Rezeptor-Agonisten。
公开(公告)号：EP0194665A1
公开(公告)日：1986-09-17
申请号：EP86103291.0
申请日：1986-03-12
申请人： G.D. Searle & Co.
发明人： Liang, Chi-Dean , Walsh, Gerald Michael
IPC分类号： C07D213/30 , C07D213/38 , A61K31/44
CPC分类号： C07D213/38
摘要： The invention relates of α-[(1-methytethy)amino)-methyl]-3-pyridinemethanol of the formula
and pharmaceutically acceptable salts thereof as well as pharmaceutical compositions containing said compounds, which possess valuable long-acting β-adrenergic receptor agonist activity.
摘要翻译：本发明涉及下式的α - [（1-甲基乙基氨基） - 甲基] -3-吡啶甲醇及其药学上可接受的盐，以及含有所述化合物的药物组合物，其具有有价值的长效β-肾上腺素能受体激动剂活性。

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