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1. 发明授权

US06506876B1 LTA4 hydrolase inhibitor pharmaceutical compositions and methods of use 失效
标题翻译： LTA4水解酶抑制剂药物组合物和使用方法
公开(公告)号：US06506876B1
公开(公告)日：2003-01-14
申请号：US08321184
申请日：1994-10-11
申请人： Nizal Samuel Chandrakumar , Barbara Baosheng Chen , Michael Clare , Bipinchandra Nanubhai Desai , Stevan Wakefield Djuric , Stephen Hermann Docter , Alan Frank Gasiecki , Richard Arthur Haack , Chi-Dean Liang , Julie Marion Miyashiro , Thomas Dale Penning , Mark Andrew Russell , Stella Siu-tzyy Yu
发明人： Nizal Samuel Chandrakumar , Barbara Baosheng Chen , Michael Clare , Bipinchandra Nanubhai Desai , Stevan Wakefield Djuric , Stephen Hermann Docter , Alan Frank Gasiecki , Richard Arthur Haack , Chi-Dean Liang , Julie Marion Miyashiro , Thomas Dale Penning , Mark Andrew Russell , Stella Siu-tzyy Yu
IPC分类号： A01N4340
CPC分类号： A61K31/445 , A61K31/138 , A61K31/192 , A61K31/197 , A61K31/216 , A61K31/381 , A61K31/40 , A61K31/44 , A61K31/4468 , A61K31/4535 , A61K31/454 , A61K31/46
摘要： The present invention provides compounds of the formula Ar1—Q—Ar2—Y—R—Z and pharmaceutically acceptable salts thereof wherein Ar1 and Ar2 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 LTB4 production, such as psoriasis, ulcerative colitis, IBD and asthma.
摘要翻译：本发明提供式Ar1-Q-Ar2-YRZ的化合物及其药学上可接受的盐，其中Ar1和Ar2是任选取代的芳基部分，Z是任选取代的含氮部分，其可以是无环的，环状的或双环的胺，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，例如牛皮癣，溃疡性结肠炎，IBD和哮喘。

2. 发明授权

US06451852B2 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：US06451852B2
公开(公告)日：2002-09-17
申请号：US09766722
申请日：2001-01-22
申请人： Chi-Dean Liang , John P. McKearn , John M. Farah, Jr. , Richard A. Mueller
发明人： Chi-Dean Liang , John P. McKearn , John M. Farah, Jr. , Richard A. Mueller
IPC分类号： A61K31277
CPC分类号： C07C255/43
摘要： A class of substituted phenylacetonitrile-alkylaminoalkyl-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的苯基乙腈 - 烷基氨基烷基邻位取代的芳基化合物。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是一种或两种; 其中n是选自1至5的数字，包括1和5; 其中R1选自氢化，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R8，R9，R10和R12至R16各自独立地选自氢，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R12和R16中的至少一个必须选自羟基，烷基，羟烷基，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. 发明授权

US4264517A Alkylphenyl 5Z,8Z,11Z,14Z,17Z-eicosapentaenoates 失效
标题翻译：烷基苯基5Z，8Z，11Z，14Z，17Z-二十碳五烯酸酯
公开(公告)号：US4264517A
公开(公告)日：1981-04-28
申请号：US88502
申请日：1979-10-26
申请人： Chi-Dean Liang
发明人： Chi-Dean Liang
IPC分类号： C07C69/587 , A61K31/23 , A61P1/04 , A61P7/04 , C07C51/09 , C09F5/08 , C11C3/00
CPC分类号： C07C51/09
摘要： Alkylphenyl 5Z,8Z,11Z,14Z,17Z-eicosapentaenoates having platelet aggregation inhibiting and antisecretory activity and methods of preparation thereof are disclosed.
摘要翻译：公开了具有血小板聚集抑制和抗分泌活性的烷基苯基5Z，8Z，11Z，14Z，17Z-二十碳五烯酸酯及其制备方法。

4. 发明授权

US5486539A Method of using phenylacetonitrilealkylaminoalkyl-ortho-substituted aryl compounds as immunosuppressives 失效
标题翻译：使用苯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的方法
公开(公告)号：US5486539A
公开(公告)日：1996-01-23
申请号：US204121
申请日：1994-03-01
申请人： Chi-Dean Liang , John P. McKearn , John M. Farah, Jr. , Richard A. Mueller
发明人： Chi-Dean Liang , John P. McKearn , John M. Farah, Jr. , Richard A. Mueller
IPC分类号： C07C255/43 , A61K31/275
CPC分类号： C07C255/43
摘要： A class of substituted phenylacetonitrile-alkylaminoalkyl-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 ##STR1## wherein m is one or two; wherein n is a number selected from one to five, inclusive; wherein R.sup.1 is selected from hydrido, alkyl, hydroxyalkyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkenyl and alkynyl; wherein R.sup.6 is selected from loweralkyl; wherein each of R.sup.8, R.sup.9, R.sup.10 and R.sup.12 through R.sup.16 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 R.sup.12 and R.sup.16 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的苯基乙腈 - 烷基氨基烷基邻位取代的芳基化合物。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下式：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R1选自氢化，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R8，R9，R10和R12至R16各自独立地选自氢，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R12和R16中的至少一个必须选自羟基，烷基，羟烷基，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。

5. 发明授权

US4404144A Unsaturated analogs of .beta.-alkyl-.beta.-hydroxy glutaric acid and esters thereof 失效
标题翻译： β-烷基-β-羟基戊二酸的不饱和类似物及其酯
公开(公告)号：US4404144A
公开(公告)日：1983-09-13
申请号：US327821
申请日：1981-12-07
申请人： Chi-Dean Liang
发明人： Chi-Dean Liang
IPC分类号： C07C17/16 , C07C49/255 , C07C59/42 , C07D339/08 , C07C69/675 , C07C49/175 , C07C59/185 , C07C59/245 , C07C59/58 , C07C59/76 , C07C69/732
CPC分类号： C07C17/16 , C07C45/567 , C07C49/255 , C07C59/42 , C07C69/732 , C07C69/734 , C07D339/08
摘要： This invention relates to .beta.-Alkyl-.beta.-Hydroxy Glutaric acid .differential. ester derivatives which are useful as anti-hyperlipoproteinemia agents.
摘要翻译：本发明涉及可用作抗高脂蛋白血症药物的β-烷基-β-羟基戊二酸衍生物衍生物。

6. 发明授权

US3972907A Anti-hyperlipidemic fatty acids and esters 失效
标题翻译：抗高血脂脂肪酸和酯类
公开(公告)号：US3972907A
公开(公告)日：1976-08-03
申请号：US561646
申请日：1975-03-24
申请人： John S. Baran , Chi-Dean Liang
发明人： John S. Baran , Chi-Dean Liang
IPC分类号： C07C17/093 , C07C57/03 , C07C309/73 , C11C3/02
CPC分类号： C07C309/73 , C07C17/093 , C07C57/03
摘要： 2,2-Dialkylated arachidonic acid and esters are prepared from the alkyl esters of arachidonic acid by treatment with the appropriate alkyl iodide. The compounds so produced are useful as pharmacological agents in view of their ability to inhibit lipogenesis.
摘要翻译： 2,2-二烷基化花生四烯酸和酯由花生四烯酸的烷基酯通过用合适的烷基碘处理制备。考虑到它们抑制脂肪生成的能力，所产生的化合物可用作药理学试剂。

7. 发明授权

US6162823A LTA.sub.4 hydrolase inhibitors 失效
标题翻译： LTA4水解酶抑制剂
公开(公告)号：US6162823A
公开(公告)日：2000-12-19
申请号：US815700
申请日：1997-03-12
申请人： Thomas Dale Penning , Stella Siu-tzyy Yu , James Malecha , Chi-Dean Liang , Mark Andrew Russell
发明人： Thomas Dale Penning , Stella Siu-tzyy Yu , James Malecha , Chi-Dean Liang , Mark Andrew Russell
IPC分类号： C07C311/51 , C07D333/16 , A61K31/38 , A61K31/18 , C07C303/00 , C07D333/22
CPC分类号： C07D333/16 , C07C311/51 , C07C2601/02
摘要： The present invention provides compounds having the of the formula I: ##STR1## and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.
摘要翻译：本发明提供具有式I化合物及其药学上可接受的盐和立体异构体，其可用于治疗由LTB4产生介导的炎性疾病，例如牛皮癣，溃疡性结肠炎，IBD和哮喘。

8. 发明授权

US5723492A LTA4 hydrolase inhibitor pharmaceutical compositions and methods of use 失效
公开(公告)号：US5723492A
公开(公告)日：1998-03-03
申请号：US469606
申请日：1995-06-06
申请人： Nizal Samuel Chandrakumar , Barbara Baosheng Chen , Michael Clare , Bipinchandra Nanubhai Desai , Stevan Wakefield Djuric , Stephen Hermann Docter , Alan Frank Gasiecki , Richard Arthur Haack , Chi-Dean Liang , Julie Marion Miyashiro , Thomas Dale Penning , Mark Andrew Russell , Stella Siu-tzyy Yu
发明人： Nizal Samuel Chandrakumar , Barbara Baosheng Chen , Michael Clare , Bipinchandra Nanubhai Desai , Stevan Wakefield Djuric , Stephen Hermann Docter , Alan Frank Gasiecki , Richard Arthur Haack , Chi-Dean Liang , Julie Marion Miyashiro , Thomas Dale Penning , Mark Andrew Russell , Stella Siu-tzyy Yu
IPC分类号： C07D295/08 , A61K31/135 , A61K31/138 , A61K31/192 , A61K31/195 , A61K31/197 , A61K31/215 , A61K31/216 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61K31/4535 , A61K31/454 , A61K31/46 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61K31/5375 , A61K31/695 , A61P29/00 , A61P43/00 , C07D207/14 , C07D207/16 , C07D209/12 , C07D211/58 , C07D211/62 , C07D213/38 , C07D215/12 , C07D235/08 , C07D277/24 , C07D295/18 , C07D307/42 , C07D307/81 , C07D307/85 , C07D311/58 , C07D317/54 , C07D333/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D473/08 , C07D491/052 , C07D491/107 , A61K31/24
CPC分类号： A61K31/445 , A61K31/138 , A61K31/192 , A61K31/197 , A61K31/216 , A61K31/381 , A61K31/40 , A61K31/44 , A61K31/4468 , A61K31/4535 , A61K31/454 , A61K31/46
摘要： The present invention provides compounds of the formula Ar.sup.1 --Q--Ar.sup.2 --Y--R--Z and pharmaceutically acceptable salts thereof wherein Ar.sup.1 and Ar.sup.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.sub.4 production, such as psoriasis, ulcerative colitis, IBD and asthma.

9. 发明授权

US4600710A .beta.-Adrenergic receptor agonist alkylaminoalkyl pyridinemethanol derivatives 失效
标题翻译： β-肾上腺素能受体激动剂烷基氨基烷基吡啶甲醇衍生物
公开(公告)号：US4600710A
公开(公告)日：1986-07-15
申请号：US711899
申请日：1985-03-14
申请人： Chi-Dean Liang , Gerald M. Walsh
发明人： Chi-Dean Liang , Gerald M. Walsh
IPC分类号： A61K31/44 , A61K31/4406 , A61K31/4418 , A61K31/443 , A61P11/16 , A61P25/02 , C07D213/38 , C07D405/04
CPC分类号： C07D213/38
摘要： .beta.-Adrenergic receptor site activation by novel pyridinemethanol derivatives and pharmaceutical compositions and methods of use thereof are described.
摘要翻译：描述了通过新型吡啶甲醇衍生物和药物组合物及其使用方法的β-肾上腺素能受体位点活化。

10. 发明授权

US4499289A Octahydronapthalenes 失效
标题翻译：八氢萘
公开(公告)号：US4499289A
公开(公告)日：1985-02-12
申请号：US549534
申请日：1983-11-07
申请人： John S. Baran , Chi-Dean Liang
发明人： John S. Baran , Chi-Dean Liang
IPC分类号： C07C15/24 , C07C17/093 , C07C29/00 , C07C43/196 , C07C43/23 , C07C43/315 , C07C45/51 , C07C45/56 , C07C69/732 , C07D309/30 , C07D339/06 , C07F7/18
CPC分类号： C07F7/1856 , C07C17/093 , C07C29/00 , C07C309/00 , C07C43/196 , C07C43/23 , C07C43/315 , C07C45/513 , C07C45/567 , C07D309/30 , C07D339/06 , C07C2102/28
摘要： The invention relates to octahydronapthalenes which are useful in antiatherosclerotic agents.
摘要翻译：本发明涉及可用于抗动脉粥样硬化剂的八氢萘。

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