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21. 发明授权

US5455271A Tight-binding inhibitors of leukotriene A.sub.4 hydrolase 失效
标题翻译：白三烯A4水解酶的紧密结合抑制剂
公开(公告)号：US5455271A
公开(公告)日：1995-10-03
申请号：US079239
申请日：1993-06-17
申请人： Wei Yuan , Chi-Huey Wong , Bengt Samuelsson , Benito Munoz
发明人： Wei Yuan , Chi-Huey Wong , Bengt Samuelsson , Benito Munoz
IPC分类号： C07C215/28 , C07C217/62 , C07C225/16 , C07C229/34 , C07C229/38 , C07C237/20 , C07C323/29 , C07C327/42 , C07D233/54 , A61K31/24
CPC分类号： C07D233/64 , C07C215/28 , C07C217/62 , C07C225/16 , C07C229/34 , C07C229/38 , C07C237/20 , C07C323/29 , C07C327/42
摘要： Inhibitors of leukotriene A.sub.4 hydrolase are disclosed, corresponding to Formula I, below: ##STR1## wherein the depicted --NH.sub.2 group is in the (S) configuration; --W is --CH.sub.2 SH, --CH.sub.2 NH.sub.2 or C(.dbd.Z)--Y, wherein .dbd.Z is .dbd.O, or --H and --OH; and --Y is selected from the group consisting of (a) phenyl, (b) trifluoromethylphenyl, (c) carboxyphenyl, (d) benzyl, (e) C.sub.1 -C.sub.6 alkylenecarboxyl, (f) C.sub.1 -C.sub.6 alkyl, (g) C.sub.2 -C.sub.6 alkenyl, (h) C.sub.1 -C.sub.6 alkylenephenyl and (i) --C(.dbd.O)--X--R.sup.1 wherein X is O or NH and, R.sup.1 is selected from the group consisting of C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkylenecarboxyl, and benzyl; R.sup.2 is hydrogen, benzyloxy or 2-naphthylmethyloxy, and a pharmaceutically acceptable acid addition salt thereof. Inhibitors wherein --W is --CH.sub.2 SH, --CH.sub.2 NH.sub.2 or C(.dbd.Z)--Y wherein .dbd.Z is .dbd.O and --Y is --C(.dbd.O)--X--R.sup.1 are particularly preferred, as are those compounds wherein .dbd.Z is .dbd. O and --Y is selected from the group consisting of (a) phenyl, (b) trifluoromethylphenyl, (c) carboxyphenyl, (d) benzyl, (e) C.sub.1 -C.sub.6 alkylenecarboxyl, (f) C.sub.1 -C.sub.6 alkyl, (g) C.sub.2 -C.sub.6 alkenyl, (h) C.sub.1 -C.sub.6 alkylenephenyl. An inhibitor where --W is --CH.sub.2 SH, --CH.sub.2 NH.sub.2 or C(.dbd.Z)--Y wherein .dbd.Z is .dbd.O and --Y is --C(.dbd.O)--X--R.sup.1 is particularly preferred, as are those inhibitor compounds where .dbd.Z is .dbd.O and --Y is (a)--(h).
摘要翻译：公开了对应于下式I的白三烯A4水解酶的抑制剂：其中所述-NH 2基团为（S）构型; -W为-CH 2 SH，-CH 2 NH 2或C（= Z）-Y，其中= Z为= O或-H和-OH; 和（A）苯基，（b）三氟甲基苯基，（c）羧基苯基，（d）苄基，（e）C1-C6亚烷基羧基，（f）C1-C6烷基，（g）C2 -C 6烯基，（h）C 1 -C 6亚烷基苯基和（i）-C（= O）-X-R 1其中X是O或NH，并且R 1选自C 1 -C 6烷基，C 1 -C 6亚烷基羧基和苄基; R2是氢，苄氧基或2-萘基甲氧基，及其药学上可接受的酸加成盐。其中-W为-CH 2 SH，-CH 2 NH 2或C（= Z）-Y的抑制剂，其中= Z为= O，-Y为-C（= O）-X-R 1，其中= Z为（a）苯基，（b）三氟甲基苯基，（c）羧基苯基，（d）苄基，（e）C1-C6亚烷基羧基，（f）C1-C6烷基，（g ）C 2 -C 6烯基，（h）C 1 -C 6亚烷基苯基。其中-W是-CH 2 SH，-CH 2 NH 2或C（= Z）-Y的抑制剂，其中= Z是= O，-Y是-C（= O）-X-R 1，其中= Z为= O，-Y为（a） - （h）。

22. 发明授权

US07776891B2 VLA-4 antagonists 有权
标题翻译： VLA-4拮抗剂
公开(公告)号：US07776891B2
公开(公告)日：2010-08-17
申请号：US11659608
申请日：2005-08-12
申请人： Weichao Chen , Alec D. Lebsack , Benito Munoz , Shankar Venkatraman , Bowei Wang
发明人： Weichao Chen , Alec D. Lebsack , Benito Munoz , Shankar Venkatraman , Bowei Wang
IPC分类号： A61K31/44 , C07D401/02
CPC分类号： C07K5/06139 , C07K5/06191
摘要： Compounds of Formula (I) are antagonists of VLA-4, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of inflammatory bowel disease including ulcerative colitis and Crohn's disease, multiple sclerosis, asthma, and rheumatoid arthritis.
摘要翻译：式（I）化合物是VLA-4的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。这些化合物可以配制成药物组合物，并且适用于治疗包括溃疡性结肠炎和克罗恩病，多发性硬化，哮喘和类风湿性关节炎的炎性肠病。

23. 发明授权

US07495029B2 Prodrugs of (2R)-2-propyloctanoic acid for the treatment of stroke 失效
标题翻译：（2R）-2-丙基辛酸的前药用于治疗中风
公开(公告)号：US07495029B2
公开(公告)日：2009-02-24
申请号：US11667814
申请日：2005-11-10
申请人： Benito Munoz , Joseph E. Payne , Petpiboon Prasit , Thomas S. Reger , Nicholas D. Smith
发明人： Benito Munoz , Joseph E. Payne , Petpiboon Prasit , Thomas S. Reger , Nicholas D. Smith
IPC分类号： A61K31/235 , C07J71/00 , C07D311/80 , C07C381/00 , C07C69/02
CPC分类号： C07C69/24 , C07C53/128 , C07C257/14 , C07C317/46 , C07D217/02 , C07D311/80
摘要： Disclosed are prodrugs of (2R)-2-propyloctanoic acid, and pharmaceutical compositions comprising them, which may be effective in modulating multiple events in the biochemical cascade of stroke. Also disclosed are methods of treating patients who have had a stroke, or are at risk of stroke, by administering the compounds or compositions of the invention.
摘要翻译：公开了（2R）-2-丙基辛酸的前药和包含它们的药物组合物，其可有效调节中风生化级联中的多个事件。还公开了通过施用本发明的化合物或组合物来治疗患有中风或有卒中风险的患者的方法。

24. 发明申请

US20070142453A1 1-Alkyl-3-thio-substituted indole-2-alkynoic acids useful for the treatment of alzheimer's disease and related conditions 审中-公开
标题翻译：可用于治疗阿尔茨海默病和相关病症的1-烷基-3-硫代取代的吲哚-2-炔酸
公开(公告)号：US20070142453A1
公开(公告)日：2007-06-21
申请号：US10580286
申请日：2004-11-25
申请人： Dirk Beher , Michela Bettari , Ian Churcher , Benito Munoz , Petpiboon Prasit , Abdul Quddus , Nicholas Stock , Jonathan Wrigley
发明人： Dirk Beher , Michela Bettari , Ian Churcher , Benito Munoz , Petpiboon Prasit , Abdul Quddus , Nicholas Stock , Jonathan Wrigley
IPC分类号： A61K31/404 , C07D209/36
CPC分类号： C07D417/12 , A61K31/405 , C07D209/30 , C07D209/36 , C07D403/12
摘要： Compounds of formula I: modulate the activity of γ-secretase, and hence find use in treatment or prevention of Alzheimer's disease and related conditions.
摘要翻译：式I化合物：调节γ-分泌酶的活性，因此可用于治疗或预防阿尔茨海默病和相关病症。

25. 发明授权

US07105533B2 Fused heterobicyclo substituted phenyl metabotropic glutamate-5 modulators 失效
标题翻译：融合的异二环取代的苯基代谢型谷氨酸-5调节剂
公开(公告)号：US07105533B2
公开(公告)日：2006-09-12
申请号：US10527044
申请日：2003-09-09
申请人： Brian Thomas Campbell , Janet Lorraine Gunzer , Benito Munoz , Brian Andrew Stearns , Jean-Michel Andre Vernier , Bowei Wang
发明人： Brian Thomas Campbell , Janet Lorraine Gunzer , Benito Munoz , Brian Andrew Stearns , Jean-Michel Andre Vernier , Bowei Wang
IPC分类号： A61K31/4375 , A61K31/4439 , C07D471/02 , C07D487/02 , C07D513/02
CPC分类号： C07D513/04 , A61K31/137 , A61K31/222 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/485 , A61K45/06 , C07D401/10 , C07D471/04 , A61K2300/00
摘要： Phenyl compounds substituted with a fused-heterobicyclo moiety, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.
摘要翻译：被稠合 - 杂双环部分取代的苯基化合物是可用于治疗精神病和情绪障碍（例如精神分裂症，焦虑，抑郁和恐慌）以及治疗疼痛和其他疾病的mGluR5调节剂。

26. 发明授权

US6015879A Peptide and peptide analog protease inhibitors 失效
标题翻译：肽和肽类似物蛋白酶抑制剂
公开(公告)号：US6015879A
公开(公告)日：2000-01-18
申请号：US442662
申请日：1995-05-17
申请人： Ian Alexander McDonald , Elisabeth Albrecht , Benito Munoz
发明人： Ian Alexander McDonald , Elisabeth Albrecht , Benito Munoz
IPC分类号： A61K38/00 , A61K31/00 , A61P25/00 , A61P25/16 , A61P25/28 , C07C237/22 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/08 , C07K5/083 , A61K38/06
CPC分类号： C07K5/0808 , C07C237/22 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/06078 , C07K5/06139 , C07K5/06165 , C07K5/06191 , A61K38/00
摘要： Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided Among the compounds are those of formulae I and II: ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, cyclohexyl or cyclohexylmethyl; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 --(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; R.sub.B is preferbly iso-butyl; --R.sub.A =--(T).sub.m --(D).sub.m --R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is preferably an .alpha.-ketoester or .alpha.-ketoamide or aldehyde.
摘要翻译：提供化合物和化合物用于治疗以沉淀淀粉样蛋白为特征的疾病的方法在这些化合物中是式I和II的化合物：其中R 1优选为2-甲基丙烯，2-丁烯，环己基或环己基甲基; R2，R4和R8各自独立地是甲基或乙基; R3优选为异丁基或苯基; R5优选为异丁基; R6是H或甲基; R7-（Q）n优选为苄氧羰基或乙酰基; Q优选为-C（O） - ; RB优选为异丁基; -RA = - （T）m-（D）m -R 1，其中T优选为氧或碳，D优选为单不饱和C 3-4烯基为更优选的; 并且X优选为α-酮酯或α-酮酰胺或醛。

27. 发明授权

US5969100A Peptide, peptide analog and amino acid analog protease inhibitors 失效
公开(公告)号：US5969100A
公开(公告)日：1999-10-19
申请号：US403420
申请日：1995-03-13
申请人： Benito Munoz , Ian A. McDonald , Elisabeth Albrecht
发明人： Benito Munoz , Ian A. McDonald , Elisabeth Albrecht
IPC分类号： A61K38/00 , A61K31/00 , A61P25/00 , A61P25/16 , A61P25/28 , C07C237/22 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/08 , C07K5/083 , A61K38/06
CPC分类号： C07K5/0808 , C07C237/22 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/06078 , C07K5/06139 , C07K5/06165 , C07K5/06191 , A61K38/00
摘要： Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae (I), (II) and (III): ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, norleucine; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 --(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; R.sub.B is preferbly iso-butyl; R.sub.A =--(T).sub.m --(D).sub.m --R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is an alcohol, particularly a secondary alcohol.

28. 发明授权

US5863902A Methods of treating neurodegenerative disorders using protease inhibitors 失效
标题翻译：使用蛋白酶抑制剂治疗神经变性疾病的方法
公开(公告)号：US5863902A
公开(公告)日：1999-01-26
申请号：US444912
申请日：1995-05-18
申请人： Benito Munoz , Ian A. McDonald , Elisabeth Albrecht
发明人： Benito Munoz , Ian A. McDonald , Elisabeth Albrecht
IPC分类号： A61K38/00 , C07C237/22 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/083 , A61K38/05
CPC分类号： C07K5/0808 , C07C237/22 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/06078 , C07K5/06165 , C07K5/06191 , A61K38/00
摘要： Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae (I), (II) and (III): ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, norleucine; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 -(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; RB is preferbly iso-butyl; R.sub.A =--(T).sub.m --(D).sub.m --R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is an alcohol, particularly a secondary alcohol.
摘要翻译：提供了化合物和化合物用于治疗以沉淀淀粉样蛋白为特征的疾病的方法。其中R 1优选为2-甲基丙烯，2-丁烯，正亮氨酸;式（I），（II）和（III）的化合物为： R2，R4和R8各自独立地是甲基或乙基; R3优选为异丁基或苯基; R5优选为异丁基; R6是H或甲基; R7-（Q）n优选为苄氧羰基或乙酰基; Q优选为-C（O） - ; RB优选为异丁基; RA = - （T）m-（D）m -R 1，其中T优选为氧或碳，D优选为单不饱和C 3-4烯基; X是醇，特别是仲醇。

29. 发明授权

US5804560A Peptide and peptide analog protease inhibitors 失效
标题翻译：肽和肽类似物蛋白酶抑制剂
公开(公告)号：US5804560A
公开(公告)日：1998-09-08
申请号：US369422
申请日：1995-01-06
申请人： Ian Alexander McDonald , Elisabeth Albrecht , Benito Munoz
发明人： Ian Alexander McDonald , Elisabeth Albrecht , Benito Munoz
IPC分类号： A61K38/00 , A61K31/00 , A61P25/00 , A61P25/16 , A61P25/28 , C07C237/22 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/08 , C07K5/083 , A61K38/05
CPC分类号： C07K5/0808 , C07C237/22 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/06078 , C07K5/06139 , C07K5/06165 , C07K5/06191 , A61K38/00
摘要： Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae I and II: ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, cyclohexyl or cyclohexylmethyl; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 -(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; R.sub.B is preferbly iso-butyl; R.sub.A =--(T).sub.m--(D).sub.m--R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is preferably an .alpha.-ketoester or .alpha.-ketoamide or aldehyde.
摘要翻译：提供了化合物和化合物用于治疗以沉淀淀粉样蛋白为特征的疾病的方法。其中R 1优选为2-甲基丙烯，2-丁烯，环己基或环己基甲基;其中R 1优选为2-甲基丙烯，2-丁烯，环己基或环己基甲基; R2，R4和R8各自独立地是甲基或乙基; R3优选为异丁基或苯基; R5优选为异丁基; R6是H或甲基; R7-（Q）n优选为苄氧羰基或乙酰基; Q优选为-C（O） - ; RB优选为异丁基; RA = - （T）m-（D）m -R 1，其中T优选为氧或碳，D优选为单不饱和C 3-4烯基; 并且X优选为α-酮酯或α-酮酰胺或醛。

30. 发明申请

US20120022044A1 TRIAZOLE DERIVATIVES FOR TREATMENT OF ALZHEIMER'S DISEASE 有权
标题翻译：用于治疗阿尔茨海默病的三唑衍生物
公开(公告)号：US20120022044A1
公开(公告)日：2012-01-26
申请号：US13139830
申请日：2009-12-07
申请人： Christian Fischer , Joey Methot , Hua Zhou , Adam J. Schell , Benito Munoz , Alexey A. Rivkin , Sean P. Ahearn , Stephanie Chichetti , Rachel N. MacCoss , Sam Kattar , Matthew Christopher , Chaomin Li , Andrew Rosenau , William Colby Brown
发明人： Christian Fischer , Joey Methot , Hua Zhou , Adam J. Schell , Benito Munoz , Alexey A. Rivkin , Sean P. Ahearn , Stephanie Chichetti , Rachel N. MacCoss , Sam Kattar , Matthew Christopher , Chaomin Li , Andrew Rosenau , William Colby Brown
IPC分类号： A61K31/55 , C07D403/04 , C07D409/14 , A61P25/28 , C07D403/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D401/14 , C07D417/14
CPC分类号： A61K31/41 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of Aβ42 and hence are useful in treatment of Alzheimer's disease and related conditions.
摘要翻译：根据本发明，提供式I化合物或其药学上可接受的盐或水合物; 其中变量如本文所定义。这些化合物选择性地减弱A＆bgr的产生42，因此可用于治疗阿尔茨海默病和相关病症。

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