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31. 发明授权

US06762187B2 Retroviral protease inhibitors 失效
标题翻译：逆转录病毒蛋白酶抑制剂
公开(公告)号：US06762187B2
公开(公告)日：2004-07-13
申请号：US10245710
申请日：2002-09-18
申请人： John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Kathryn L. Reed , Ko-Chung Lin , John Nicholas Freskos , Michael Clare , Donald Joseph Rogier, Jr. , Robert M. Heintz , Michael L. Vazquez , Richard A. Mueller
发明人： John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Kathryn L. Reed , Ko-Chung Lin , John Nicholas Freskos , Michael Clare , Donald Joseph Rogier, Jr. , Robert M. Heintz , Michael L. Vazquez , Richard A. Mueller
IPC分类号： A61K314965
CPC分类号： C07D401/12 , C07D207/16 , C07D211/60 , C07D217/26
摘要： N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译：含有羟基胺化合物的N-杂环部分作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶抑制剂。

32. 发明授权

US06265583B1 Cyclic sulfone containing retroviral protease inhibitors 失效
公开(公告)号：US06265583B1
公开(公告)日：2001-07-24
申请号：US09177100
申请日：1998-10-22
申请人： Deborah E. Bertenshaw , Daniel Getman , Robert M. Heintz , John J. Talley , Kathryn L. Reed , Robert Alan Chrusciel , Michael Clare
发明人： Deborah E. Bertenshaw , Daniel Getman , Robert M. Heintz , John J. Talley , Kathryn L. Reed , Robert Alan Chrusciel , Michael Clare
IPC分类号： C07D28506
CPC分类号： C07D333/48 , C07D231/12 , C07D233/56 , C07D249/08 , C07D279/12 , C07D335/02 , C07D409/12
摘要： The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.

33. 发明授权

US6114381A Non-heterocyclic .beta.-phenyl-.alpha.-aminopropionic acid n-phenyl amides for treatment of neurotoxic injury 失效
标题翻译：用于治疗神经毒性损伤的非杂环β-苯基-α-氨基丙酸n-苯基酰胺
公开(公告)号：US6114381A
公开(公告)日：2000-09-05
申请号：US170784
申请日：1998-10-13
申请人： Barnett S. Pitzele , Nizal S. Chandrakumar , Michael Clare
发明人： Barnett S. Pitzele , Nizal S. Chandrakumar , Michael Clare
IPC分类号： A61K31/395 , A61K31/47 , C07C237/20 , C07D209/08 , C07D215/08 , C07D215/20 , C07D215/26 , C07D225/08 , A61K31/275 , A61K31/165 , C07C229/36 , C07C233/04
CPC分类号： C07D209/08 , A61K31/395 , A61K31/47 , C07C237/20 , C07D215/08 , C07D215/20 , C07D215/26 , C07D225/08
摘要： Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a .beta.-phenyl-.alpha.-aminopropionic acid N phenyl amide compound as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.5 is independently selected from hydrido, fluoro, chloro, bromo, methyl and ethyl; wherein R.sup.3 is selected from hydroxy, methoxy, ethoxy, methoxycarbonyloxy, ethoxycarbonyloxy, (2-methylpropoxy)carbonyloxy and (2-propenyloxy) carbonyloxy; wherein each of R.sup.6, R.sup.7 and R.sup.8 is hydrido; wherein each of R.sup.9 and R.sup.10 is independently selected from hydrido, methyl and ethyl; wherein R.sup.11 is one or more groups independently selected from hydrido, fluoro, chloro, hydroxy, methoxy, methyl and ethyl; or a tautomer or enantiomer therefor, or a pharmaceutically-acceptable salt or ester thereof.
摘要翻译：描述了治疗的化合物，组合物和方法以控制与缺氧或缺血相关的脑损伤，其通常在中风，心脏骤停或围产期窒息之后。该治疗包括施用β-苯基-α-氨基丙酸N苯基酰胺化合物作为拮抗剂，以抑制主要神经元兴奋性氨基酸受体位点的兴奋性毒性作用。最感兴趣的化合物是下式的化合物，其中R 1和R 5各自独立地选自氢，氟，氯，溴，甲基和乙基; 其中R3选自羟基，甲氧基，乙氧基，甲氧基羰基氧基，乙氧基羰基氧基，（2-甲基丙氧基）羰基氧基和（2-丙烯氧基）羰基氧基; 其中R6，R7和R8各自为氢; 其中R 9和R 10各自独立地选自氢，甲基和乙基; 其中R 11是一个或多个独立地选自氢，氟，氯，羟基，甲氧基，甲基和乙基的基团; 或其互变异构体或对映异构体，或其药学上可接受的盐或酯。

34. 发明授权

US5849784A Cyclic sulfone containing retroviral protease inhibitors 失效
公开(公告)号：US5849784A
公开(公告)日：1998-12-15
申请号：US556883
申请日：1995-11-02
申请人： Deborah E. Bertenshaw , Daniel Getman , Robert M. Heintz , John J. Talley , Kathryn L. Reed , Robert Alan Chrusciel , Michael Clare
发明人： Deborah E. Bertenshaw , Daniel Getman , Robert M. Heintz , John J. Talley , Kathryn L. Reed , Robert Alan Chrusciel , Michael Clare
IPC分类号： A61K31/38 , A61K31/381 , A61K31/382 , A61K31/415 , A61K31/425 , A61K31/4433 , A61K31/445 , A61K31/54 , A61P31/12 , A61P43/00 , C07D279/12 , C07D283/00 , C07D333/48 , C07D335/02 , C07D409/12 , C07D417/12 , C07D521/00
CPC分类号： C07D333/48 , C07D231/12 , C07D233/56 , C07D249/08 , C07D279/12 , C07D335/02 , C07D409/12
摘要： The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.

35. 发明授权

US5773646A Meta-substituted phenylene derivatives 失效
标题翻译：元取代亚苯衍生物
公开(公告)号：US5773646A
公开(公告)日：1998-06-30
申请号：US825086
申请日：1997-03-27
申请人： Nizal Chandrakumar , Barbara B. Chen , Helen Y. Chen , Michael Clare , Alan F. Gasiecki , Richard A. Haack , James W. Malecha , Peter G. Ruminski , Mark A. Russell
发明人： Nizal Chandrakumar , Barbara B. Chen , Helen Y. Chen , Michael Clare , Alan F. Gasiecki , Richard A. Haack , James W. Malecha , Peter G. Ruminski , Mark A. Russell
IPC分类号： A61K31/00 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/216 , A61K31/415 , A61K31/4164 , A61K31/4168 , A61K31/4184 , A61K31/496 , A61K31/505 , A61P1/00 , A61P1/02 , A61P19/00 , A61P19/08 , A61P19/10 , A61P27/00 , A61P27/02 , A61P35/00 , A61P43/00 , C07C45/67 , C07C49/796 , C07C205/35 , C07C205/45 , C07C205/56 , C07C205/57 , C07C257/16 , C07C257/18 , C07C259/18 , C07C275/42 , C07C279/18 , C07C279/24 , C07C279/28 , C07C311/46 , C07C311/47 , C07C317/42 , C07C317/44 , C07C323/44 , C07C323/56 , C07C335/16 , C07C335/22 , C07C335/32 , C07D223/06 , C07D233/50 , C07D233/88 , C07D235/30 , C07D239/14 , C07D311/18 , C07D311/20 , C07D405/12 , C07C241/00 , C07C205/00 , C07C229/00 , C07C321/00
CPC分类号： C07C45/673 , C07C205/35 , C07C205/45 , C07C205/56 , C07C205/57 , C07C257/16 , C07C259/18 , C07C275/42 , C07C279/18 , C07C279/24 , C07C279/28 , C07C311/46 , C07C311/47 , C07C317/42 , C07C323/44 , C07C335/16 , C07C335/22 , C07C335/32 , C07C49/796 , C07D223/06 , C07D233/50 , C07D233/88 , C07D235/30 , C07D239/14 , C07D311/18 , C07D311/20 , C07D405/12
摘要： The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物和选择性抑制或拮抗αvβ3整联蛋白的方法。

37. 发明授权

US4758675A 3-thiophene-substituted tyrosyl dipeptide amides 失效
标题翻译： 3-噻吩取代的酪氨酰二肽酰胺
公开(公告)号：US4758675A
公开(公告)日：1988-07-19
申请号：US14339
申请日：1987-02-13
申请人： Donald W. Hansen, Jr. , Barnett S. Pitzele , Robert W. Hamilton , Michael Clare
发明人： Donald W. Hansen, Jr. , Barnett S. Pitzele , Robert W. Hamilton , Michael Clare
IPC分类号： A61K38/00 , C07K5/065 , C07D333/22
CPC分类号： C07K5/06078 , A61K38/00
摘要： This invention relates to novel 3-thiophene-substituted tryosyl dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable addition salts thereof, wherein R.sup.1 is --OH, benzyloxy, or --OCH.sub.3 ; wherein R.sub.2 and R.sub.3 may be the same or different and represent lower alkyl of 1-6 carbon atoms; wherein R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl of 1-6 carbon atoms; wherein "v" represents an asymmetric carbon atom that may be racemic or that may have the D or L configuration; and wherein "w" represents an asymmetric carbon atom that has the D configuration. These compounds are useful as analgesic agents.
摘要翻译：本发明涉及下式的新型3-噻吩取代的甜蛋白二肽酰胺及其药学上可接受的加成盐，其中R1是-OH，苄氧基或-OCH3; 其中R2和R3可以相同或不同，代表1-6个碳原子的低级烷基; 其中R4，R5，R6，R7，R8和R9可以相同或不同，代表氢或1-6个碳原子的低级烷基; 其中“v”表示可以是外消旋的或可具有D或L构型的不对称碳原子; 并且其中“w”表示具有D构型的不对称碳原子。这些化合物可用作止痛剂。

38. 发明授权

US4757153A Sulfide, sulfinyl and sulfone dipeptide amides 失效
标题翻译：硫化物，亚磺酰基和砜二肽酰胺
公开(公告)号：US4757153A
公开(公告)日：1988-07-12
申请号：US882796
申请日：1986-07-14
申请人： Donald W. Hansen, Jr. , Daniel R. Pilipauskas , Michael Clare
发明人： Donald W. Hansen, Jr. , Daniel R. Pilipauskas , Michael Clare
IPC分类号： A61K38/00 , C07D333/20 , C07D333/38 , C07D333/48 , C07D335/02 , C07K5/065 , C07D337/00 , C07C103/00 , C07D331/04 , C07D333/36 , C07K7/12
CPC分类号： C07D333/48 , C07D333/20 , C07D333/38 , C07D335/02 , C07K5/06078 , A61K38/00
摘要： The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, lower alkoxy, --O(CH.sub.2).sub.n phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, and R.sup.9 may be the same or different and represent hydrogen, lower alkyl, cycloalkyl having 3 to 8 carbons, unsaturated lower alkyl, or --(CH.sub.2).sub.m cycloalkyl with the cycloalkyl having 3 to 8 carbons and m is 1 to 4; R.sup.10 is hydrogen or --(CH.sub.2).sub.p phenyl or with the phenyl optionally substituted with --NH.sub.2, --OH, halogen, --NO.sub.2, or lower alkyl or --(CH.sub.2).sub.p thienyl wherein p is 1 to 4; one of R.sup.7 or R.sup.8 is --(CH.sub.2).sub.f --S(O).sub.z --(CH.sub.2).sub.q --CH.sub.3 where f is 1 to 3 and q is 0 to 3, z is 0, 1 or 2 and the other is hydrogen or lower alkyl, or R.sup.7 and R.sup.8 together with carbon w is ##STR2## where x and y are independently 1 to 3 and z is 0, or 2. V represents an asymmetric carbon that may be recemic or have the D or L configuration; W represents an asymmetric carbon when R.sup.7 and R.sup.8 are not the same that may be recemic or have the D or L configuration.The compounds of this invention are useful as analgesic and/or antihypertensive agents.
摘要翻译：本发明涉及下式的新型取代的酪氨酸丙氨酸二肽酰胺及其药学上可接受的酸加成盐，其中R1是氢，低级烷基，羟基，低级烷氧基，-O（CH2）n-苯基，其中苯基任选被卤素，-NO 2，-CN，-NH 2或低级烷基，其中n为1至4; R2和R3表示低级烷基，卤素或低级烷氧基，或R2或R3中的任一个为氢，另一个为低级烷基，低级烷氧基或卤素; R 4，R 5，R 6和R 9可以相同或不同，表示氢，低级烷基，具有3-8个碳原子的环烷基，不饱和低级烷基或 - （CH 2）m环烷基，环烷基具有3至8个碳原子，m是1 到4; R 10是氢或 - （CH 2）p苯基或与-NH 2，-OH，卤素，-NO 2或低级烷基或 - （CH 2）p噻吩基取代的苯基，其中p为1至4; R 7或R 8中的一个为 - （CH 2）f S（O）z - （CH 2）q -CH 3，其中f为1至3，q为0至3，z为0,1或2，而另一个为氢或低级烷基或者R 7和R 8与碳w一起为，其中x和y独立地为1〜3，z为0或2.V表示可以是接受或具有D或L构型的不对称碳; 当R7和R8不相同时，W表示不对称碳，其可以是可接受的或具有D或L构型。本发明的化合物可用作镇痛药和/或抗高血压药。

39. 发明申请

US20070225291A1 Substituted Pyrazinone Compounds for the Treatment of Inflammation 审中-公开
标题翻译：用于治疗炎症的替代吡嗪酮化合物
公开(公告)号：US20070225291A1
公开(公告)日：2007-09-27
申请号：US10583782
申请日：2004-10-04
申请人： Mark Boys , Michael Clare , Mark Mitton-Fry
发明人： Mark Boys , Michael Clare , Mark Mitton-Fry
IPC分类号： C07D403/04
CPC分类号： C07D241/20 , C07D401/04
摘要： Kinase inhibitors of Formula (I): wherein X, Ra, Rb, Rc, and Rd are as defined herein, are disclosed.
摘要翻译：式（I）的激酶抑制剂：其中X，R a，R b，R c，R d和R d >如本文所定义。

40. 发明授权

US07211597B2 Substituted pyrazolyl compounds for the treatment of inflammation 失效
标题翻译：用于治疗炎症的取代的吡唑基化合物
公开(公告)号：US07211597B2
公开(公告)日：2007-05-01
申请号：US10247028
申请日：2002-09-19
申请人： Suzanne Metz , Michael Clare , Joyce Z. Crich , Timothy J. Hagen , Gunnar J. Hanson , He Huang , Stephen C. Houdek , Michael A. Stealey , Michael L. Vazquez , Richard M. Weier , Xiangdong Xu
发明人： Suzanne Metz , Michael Clare , Joyce Z. Crich , Timothy J. Hagen , Gunnar J. Hanson , He Huang , Stephen C. Houdek , Michael A. Stealey , Michael L. Vazquez , Richard M. Weier , Xiangdong Xu
IPC分类号： C07D491/052 , C07D471/04 , A61K31/4162 , A61K31/437 , A61K29/00
CPC分类号： C07D231/56 , C07D471/04 , C07D491/04 , C07D495/04 , C07D495/14
摘要： The present invention relates to compounds of Formula I: wherein A is (CH2)m-Q-(CH2)n, wherein each CH2 may be independently substituted with one or more substitution selected from the group consisting of: hydroxy, halo, alkoxy, lower alkyl, amino, aminoalkyl, alkylamino, alkenyl, and alkynyl; B is a 5 or 6 membered heteroaryl, or aryl, optionally saturated, or optionally substituted with R1, R2, or R12; X is selected from the group consisting of: N and C; and Y and Z are independently selected from the group consisting of: N, C, CH, CR3, S, and O; compositions comprising such compounds, intermediates thereof, methods of making such compounds, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
摘要翻译：本发明涉及式I的化合物：其中A是（CH 2）2 - （CH 2 CH 2）n 其中每个CH 2可以独立地被一个或多个选自以下的取代基取代：羟基，卤素，烷氧基，低级烷基，氨基，氨基烷基，烷基氨基，烯基和炔基; B是任选被饱和或任选被R 1，R 2或R 12取代的5或6元杂芳基或芳基; X选自：N和C; 且Y和Z独立地选自：N，C，CH，CR 3，S和O; 包含这些化合物的组合物，其中间体，制备此类化合物的方法，以及用于治疗癌症，炎症和炎症相关疾病如关节炎的方法。

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