专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明授权

US06689765B2 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：可用作CCR5拮抗剂的哌嗪衍生物
公开(公告)号：US06689765B2
公开(公告)日：2004-02-10
申请号：US10061011
申请日：2002-01-30
申请人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
发明人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
IPC分类号： A61K31695
CPC分类号： C07D401/06 , A61K31/496 , A61K45/06 , C07D211/58 , C07D401/10 , C07D401/12 , C07D405/12 , C07D409/06 , C07D413/06 , A61K2300/00
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v, host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5，R 5和R 5独立地选自氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基， R 7为氢或烷基; R 6为氢，烷基或烯基;用于治疗HIV，实体器官移植排斥，移植物v，宿主病，关节炎，类风湿性关节炎，炎性肠病，特应性皮炎，公开了牛皮癣，哮喘，过敏或多发性硬化，以及新化合物，包含它们的药物组合物，以及本发明的CCR5拮抗剂与用于治疗可用于治疗炎性疾病的HIV或药物。

42. 发明授权

US06472394B1 MCH antagonists and their use in the treatment of obesity 失效
标题翻译： MCH拮抗剂及其在治疗肥胖中的应用
公开(公告)号：US06472394B1
公开(公告)日：2002-10-29
申请号：US10023371
申请日：2001-12-17
申请人： Brian A. McKittrick , Jing Su , John W. Clader , Shengjian Li , Guihau Guo
发明人： Brian A. McKittrick , Jing Su , John W. Clader , Shengjian Li , Guihau Guo
IPC分类号： C07D40106
CPC分类号： C07D401/06 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/454 , A61K31/4709 , A61K31/4965 , A61K31/517 , C07D211/34 , C07D405/06 , C07D413/06 , C07D417/06
摘要： Disclosed are compounds represented by structural formula I: or a pharmaceutically acceptable salt, ester or solvate thereof, wherein W is R1—CR3R12NR4C(O)— or R11C(O)NR4—; the dotted line is an optional double bond; X is —CHR8—, —C(O)—, or —C(═NOR9)—; Y is R1 is optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkyl-alkyl; R2 is optionally substituted aryl or heteroaryl; R3 is alkyl, aryl or heteroaryl; R4 and R12 are H or alkyl; R8 is H, alkyl or alkoxyalkyl; R9 is H, alkyl or arylalkyl; R10 is H, alkyl or aryl; R11 is or, when R2 is R6-heteroaryl or R10 is not H, R11 can also be R5-phenylalkyl; n is 1-3 and m is 1-5; and R14 is 1-3 substituents selected from H, alkyl, halogen, —OH, alkoxy and CF3; and pharmaceutical compositions containing the compounds and methods of using the compounds in the treatment of eating disorders and diabetes.
摘要翻译：公开了由结构式I表示的化合物：或其药学上可接受的盐，酯或溶剂合物，其中W为R 1 -CR 3 R 12 NR 4 C（O） - 或R 11 C（O）NR 4 - ;虚线为任选的双键; X为-CHR 8 - ， - （O） - 或-C（= NOR9） - ; Y是R 1是任选取代的环烷基，环烷基烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，杂环烷基或杂环烷基 - 烷基; R 2是任选取代的芳基或杂芳基; R 4是H，烷基或烷氧基烷基; R 9是H，烷基或芳基烷基; R 10是H，烷基或芳基; R 11是或者当R 2是R 6 - 杂芳基或R 10 不是H，R11也可以是R5-苯基烷基; n是1-3，m是1-5; R 14为1-3个选自H，烷基，卤素，-OH，烷氧基和CF 3的取代基;以及含有化合物的药物组合物和使用该化合物治疗进食障碍和糖尿病的方法。

43. 发明授权

US5939419A 2-benzyl-polycyclic guanine derivatives and process for preparing them 失效
标题翻译： 2-苄基 - 多环鸟嘌呤衍生物及其制备方法
公开(公告)号：US5939419A
公开(公告)日：1999-08-17
申请号：US507508
申请日：1995-08-23
申请人： Deen Tulshian , Brian A. McKittrick , Yan Xia , Samuel Chackalamannil
发明人： Deen Tulshian , Brian A. McKittrick , Yan Xia , Samuel Chackalamannil
IPC分类号： C07D239/54 , C07D473/40 , C07D487/14 , C07D487/20 , A61K31/505 , C07D491/22
CPC分类号： C07D487/14 , C07D239/54 , C07D473/40
摘要： Antihypertensive and bronchodilating compounds of the formula or a pharmaceutically acceptable salt thereof, and a process for preparing them are disclosed, wherein:R.sub.1, R.sub.2, R.sub.3, R.sup.a, R.sup.b and R.sup.c as defined in the disclosure;pharmaceutical compositions containing said compounds;methods of treatment using said compounds; anda process for preparing polycyclic guanines comprisinga) reducing a nitrosopyrimidine, and treating the reduced nitrosopyrimidine with an acylating reagent to give the amidopyrimidine;b) reacting the amidopyrimidine with a halogenating/cyclizing reagent to give a halopurine;c) reacting, in the presence of a base, the halopurine with an amine to give the substituted aminopurine; andd) closing the ring of the substituted aminopurine with a suitable dehydrating agent.
摘要翻译： PCT No.PCT / US94 / 01728 Sec。 371日期1996年11月26日 102（e）日期1996年11月26日PCT 1994年2月24日PCT公布。 WO94 / 19351 PCT出版物 1994年9月1日公开了下式的低血压和支气管扩张化合物或其药学上可接受的盐及其制备方法，其中：本发明中定义的R1，R2，R3，Ra，Rb和Rc; 含有所述化合物的药物组合物; 使用所述化合物的治疗方法; 以及制备多环鸟嘌呤的方法，包括a）还原亚硝基嘧啶，用酰化试剂处理还原的亚硝基嘧啶，得到酰胺嘧啶; b）使酰胺嘧啶与卤化/环化试剂反应得到卤代嘌呤; c）在碱的存在下使卤代嘌呤与胺反应，得到取代的氨基嘌呤; 和d）用合适的脱水剂封闭取代的氨基嘌呤的环。

44. 发明授权

US5631365A Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents 失效
标题翻译：用作降胆固醇药的羟基取代的氮杂环丁酮化合物
公开(公告)号：US5631365A
公开(公告)日：1997-05-20
申请号：US257593
申请日：1994-06-09
申请人： Stuart B. Rosenblum , Sundeep Dugar , Duane A. Burnett , John W. Clader , Brian A. McKittrick
发明人： Stuart B. Rosenblum , Sundeep Dugar , Duane A. Burnett , John W. Clader , Brian A. McKittrick
IPC分类号： A61K31/21 , A61K31/35 , A61K31/395 , A61K31/397 , A61K31/40 , A61P3/06 , A61P7/00 , A61P9/10 , C07D205/08
CPC分类号： C07D205/08 , Y02P20/55
摘要： A process for preparing compounds of the formula ##STR1## wherein R and R.sup.2 are independently --OH, --O(lower alkyl) or --0-benzyl and the remaining variables are as defined in the specification, comprising(a) treating with a strong base in an anhydrous organic solvent a lactone of the formula ##STR2## respectively, wherein Ar.sup.10 is Ar.sup.1 or a suitably protected hydroxy- or amino-substituted aryl, and R' and R.sup.2' are R and R.sup.2 as defined above or are suitably protected hydroxy groups;(b) reacting a product of step (a) with an imine of the formula ##STR3## wherein Ar.sup.20 and Ar.sup.30 are Ar.sup.2 or Ar.sup.3 or suitably protected hydroxy- or amino-substituted aryl;c) quenching the reaction with an acid; andd) removing protecting groups as necssary.
摘要翻译：制备式IMA化合物的方法其中R和R 2独立地是-OH，-O（低级烷基）或-O-苄基，其余的变量如说明书中所定义，包括（a）在无水有机溶剂中具有分子式为“IMAGE”的内酯的强碱，其中Ar10为Ar1或适当保护的羟基或氨基取代的芳基，R'和R2'为如上所定义的R和R 2，或者为适当保护的羟基; （b）使步骤（a）的产物与下式的亚胺反应：其中Ar 20和Ar 30是Ar 2或Ar 3或适当保护的羟基或氨基取代的芳基; c）用酸淬灭反应; 和d）去除保护基团。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式