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1. 发明授权

US07309704B2 Heteroaryl urea neuropeptide Y Y5 receptor antagonists 有权
标题翻译：杂芳基脲神经肽Y Y5受体拮抗剂
公开(公告)号：US07309704B2
公开(公告)日：2007-12-18
申请号：US11210291
申请日：2005-08-24
申请人： Andrew Stamford , Youhao Dong , Stuart W. McCombie , Yusheng Wu
发明人： Andrew Stamford , Youhao Dong , Stuart W. McCombie , Yusheng Wu
IPC分类号： C07D239/24 , C07D403/04 , C07D403/12 , C07D403/14 , A61K31/506 , A61P3/04
CPC分类号： C07D401/12 , C07D213/75 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds represented by the structural Formula I: or a pharmaceutically acceptable salt thereof, which are useful for the treatment of metabolic and eating disorders such as obesity and hyperphagia, and for the treatment of diabetes and associated disorders.
摘要翻译：本发明涉及由结构式I表示的化合物或其药学上可接受的盐，其可用于治疗代谢和进食障碍如肥胖症和食欲过盛，以及用于治疗糖尿病和相关疾病。

2. 发明授权

US06982267B2 Heteroaryl urea neuropeptide Y Y5 receptor antagonists 有权
公开(公告)号：US06982267B2
公开(公告)日：2006-01-03
申请号：US10026651
申请日：2001-12-18
申请人： Andrew Stamford , Youhao Dong , Stuart W. McCombie , Yusheng Wu
发明人： Andrew Stamford , Youhao Dong , Stuart W. McCombie , Yusheng Wu
IPC分类号： C07D241/26 , C07D409/04 , A61K31/4965 , A61K31/497 , A61K3/04
CPC分类号： C07D401/12 , A61K31/4523 , A61K31/4535 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , A61K2300/00
摘要： The present invention relates to compounds represented by the structural Formula I: or a pharmaceutically acceptable salt thereof, which are useful for the treatment of metabolic and eating disorders such as obesity and hyperphagia, and for the treatment of diabetes and associated disorders.

3. 发明授权

US06946476B2 Heteroaryl urea neuropeptide Y Y5 receptor antagonists 有权
标题翻译：杂芳基脲神经肽Y Y5受体拮抗剂
公开(公告)号：US06946476B2
公开(公告)日：2005-09-20
申请号：US10177345
申请日：2002-06-20
申请人： Andrew Stamford , Youhao Dong , Stuart W. McCombie , Yusheng Wu
发明人： Andrew Stamford , Youhao Dong , Stuart W. McCombie , Yusheng Wu
IPC分类号： A61K31/4523 , A61K31/4535 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , C07D213/02 , A61K31/4418 , A61K31/4436 , A61P3/04 , C07D409/04
CPC分类号： C07D401/12 , C07D213/75 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds represented by the structural Formula I: or a pharmaceutically acceptable salt thereof, which are useful for the treatment of metabolic and eating disorders such as obesity and hyperphagia, and for the treatment of diabetes and associated disorders.
摘要翻译：本发明涉及由结构式I表示的化合物或其药学上可接受的盐，其可用于治疗代谢和进食障碍如肥胖症和食欲过盛，以及用于治疗糖尿病和相关疾病。

4. 发明授权

US06894063B2 Substituted urea neuropeptide Y Y5 Receptor antagonists 失效
标题翻译：取代的尿素神经肽Y Y5受体拮抗剂
公开(公告)号：US06894063B2
公开(公告)日：2005-05-17
申请号：US10096390
申请日：2002-03-12
申请人： William J. Greenlee , Ying Huang , Joseph M. Kelly , Stuart W. McCombie , Andrew W. Stamford , Yusheng Wu
发明人： William J. Greenlee , Ying Huang , Joseph M. Kelly , Stuart W. McCombie , Andrew W. Stamford , Yusheng Wu
IPC分类号： C07C275/30 , C07C311/07 , C07D211/58 , C07D211/96 , C07D401/04 , C07D401/06 , C07D409/12 , C07D409/14 , C07D417/04 , A61K31/445 , A61K31/41 , A61K31/435 , C07C281/00 , C07D421/00
CPC分类号： C07D401/04 , C07C275/30 , C07C311/07 , C07C2601/14 , C07D211/58 , C07D211/96 , C07D401/06 , C07D409/12 , C07D409/14 , C07D417/04
摘要： A novel class of compounds such as antagonists of the neuropeptide Y Y5 receptor, methods of making such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more diseases associated with the neuropeptide Y Y5 receptor are disclosed.
摘要翻译：一类新颖的化合物，例如神经肽Y Y5受体的拮抗剂，制备此类化合物的方法，含有一种或多种这类化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法，以及治疗，预防或改善方法公开了与神经肽Y Y5受体相关的一种或多种疾病。

5. 发明授权

US06451797B1 Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US06451797B1
公开(公告)日：2002-09-17
申请号：US09514935
申请日：2000-02-28
申请人： Joseph A. Kozlowski , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice
发明人： Joseph A. Kozlowski , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice
IPC分类号： A61K31501
CPC分类号： C07D401/12 , C07D211/58 , C07D405/14 , C07D409/12
摘要： Heterocyclic derivatives of di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula I (including all isomers, salts and solvates) wherein wherein one of Y and Z is —N— and the other is —N— or —CH—; X is —O—, —S—, —SO—, —SO2— or —CH2—; Q is R is alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R1, R2 and R3 are H or alkyl; R4 is alkyl, cyclolalkyl or R5 is H, alkyl, —C(O)alkyl, arylcarbonyl, —SO2alkyl, aryl-sulfonyl —C(O)Oalkyl, aryloxycarbonyl, —C(O)NH-alkyl or aryl-aminocarbonyl, wherein the aryl portion is optionally substituted; R6 is H or alkyl; and R7 is H, alkyl, hydroxyalkyl or alkoxyalkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of treatment are also disclosed.
摘要翻译：根据式I的二-N-取代哌嗪或1,4-二取代的哌啶化合物的杂环衍生物（包括所有异构体，盐和溶剂合物），其中Y和Z之一是-N-，另一个是-N-或 -CH-; X是-O - ， - S-，-SO-，-SO 2 - 或-CH 2 - ; Q是R是烷基，环烷基，任选取代的芳基或杂芳基; R 1和R 2是H或烷基; R 4 是烷基，环烷基或R 5是H，烷基，-C（O）烷基，芳基羰基，-SO 2烷基，芳基 - 磺酰基-C（O）O烷基，芳氧基羰基，-C（O）NH-烷基或芳基 - 氨基羰基，部分任选被取代; R 6是H或烷基; 和R 7是H，烷基，羟基烷基或烷氧基烷基; 是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。还公开了药物组合物和治疗方法。

6. 发明授权

US06391865B1 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：哌嗪衍生物可用作CCR5拮抗剂
公开(公告)号：US06391865B1
公开(公告)日：2002-05-21
申请号：US09562814
申请日：2000-05-01
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 , 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 , Eric Gilbert , Marc A. Labroli
IPC分类号： A01N5500
CPC分类号： A61K31/496 , A61K45/06 , C07D211/58 , C07D401/06 , 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：使用式5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，二苯基甲基或任选取代的苯基 - R 4是氢或烷基; R 6是氢，烷基或链烯基; R 4是氢或烷基; R 3是氢，烷基或烷氧基烷基，公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

7. 发明授权

US06387930B1 Piperidine derivatives useful as CCR5 antagonists 有权
标题翻译：哌啶衍生物可用作CCR5拮抗剂
公开(公告)号：US06387930B1
公开(公告)日：2002-05-14
申请号：US09562815
申请日：2000-05-01
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 , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin
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 , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin
IPC分类号： C07D40104
CPC分类号： C07D401/14 , C07D211/58 , C07D413/14 , C07D417/14
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein X is —C(R13)2—, —C(R13)(R19)—, —C(O)—, —O—, —NH—, —N(alkyl)—, R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is H, alkyl or alkenyl; R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl; R3 is optionally substituted phenyl, heteroaryl or naphthyl; R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2; R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and R5, R13, R14, R15 and R16 are hydrogen or alkyl 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X是-C（R 13）2 - ， - C（R 13）（R 19） - ， - C（O） - ， - O - N（烷基） - ，R是任选取代的苯基，吡啶基，噻吩基或萘基; R1是H，烷基或烯基; R2是任选取代的苯基，苯基烷基，杂芳基或杂芳基烷基，萘基，芴基或二苯基甲基; R 3是任选取代的苯基，杂芳基或萘基; R4是H，烷基，氟代烷基，环丙基甲基，-CH2CH2OH，-CH2CH2-O-烷基，-CH2C（O）-O-烷基，-CH2C（O）NH2，-CH2C（O）或-CH 2 C（O）-N（烷基）2; R 19是任选取代的苯基，杂芳基或萘基，环烷基，环烷基烷基或烷氧基烷基; 和R 5，R 13，R 14，R 15和R 16是氢或烷基，用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎性肠病，特应性皮炎，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拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

8. 发明授权

US6037352A Muscarinic antagonists 失效
公开(公告)号：US6037352A
公开(公告)日：2000-03-14
申请号：US195742
申请日：1998-11-19
申请人： Derek Lowe , Wei Chang , Joseph Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W Clader , Samuel Chackalamannil , Wang Yuguang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom
发明人： Derek Lowe , Wei Chang , Joseph Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W Clader , Samuel Chackalamannil , Wang Yuguang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom
IPC分类号： C07D295/08 , A61K31/335 , A61K31/357 , A61K31/36 , A61K31/365 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P25/28 , C07D211/14 , C07D211/22 , C07D211/24 , C07D211/26 , C07D211/32 , C07D211/58 , C07D211/62 , C07D239/34 , C07D257/04 , C07D271/06 , C07D295/02 , C07D295/03 , C07D295/084 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/12 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/14 , C07D295/145 , C07D295/15 , C07D307/33 , C07D309/12 , C07D317/28 , C07D317/62 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D211/00 , C07D211/08
CPC分类号： C07D211/20 , C07D211/22 , C07D211/24 , C07D211/32 , C07D211/58 , C07D213/643 , C07D213/65 , C07D213/68 , C07D237/14 , C07D239/34 , C07D239/38 , C07D257/04 , C07D277/34 , C07D295/03 , C07D295/088 , C07D295/092 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D295/26 , C07D307/33 , C07D333/20 , C07D335/02 , C07D405/12 , C07D405/14 , C07D409/14 , C07C2101/14
摘要： Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.

9. 发明授权

US5179093A Quinoline-diones 失效
标题翻译：喹啉二恶英
公开(公告)号：US5179093A
公开(公告)日：1993-01-12
申请号：US698204
申请日：1991-05-10
申请人： Adriano Afonso , Stuart W. McCombie , Jay Weinstein
发明人： Adriano Afonso , Stuart W. McCombie , Jay Weinstein
IPC分类号： C07D215/22 , C07D401/12
CPC分类号： C07D215/22 , C07D401/12
摘要： Compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein, R is H, halogen, (C.sub.1 -C.sub.6) alkyl, N(C.sub.1 -C.sub.6 alkyl/aryl).sub.2, OH, O--(C.sub.1 -C.sub.6) alkyl/aryl, CH.sub.2 OH, COOH, COO-alkyl/aryl, SO.sub.2 NH.sub.2, or SO.sub.2 NH (C.sub.1 -C.sub.6 alkyl/aryl);R.sub.1 is C.sub.1 -C.sub.6 alkyl, cycloalkyl, C.sub.2 -C.sub.6 alkenyl, heteroaryl, substituted heteroaryl, heterocycloalkyl, --CH.sub.2 -aryl, --CH.sub.2 -substituted aryl, --CH.sub.2 -heteroaryl, or --CH.sub.2 -substituted heteroaryl;R.sub.2 is H, C.sub.1 -C.sub.6 alkyl or aryl; ##STR2## is an aromatic ring or a heteroaromatic ring; and X is O or N-(alkyl/aryl/alkyl-aryl/alkoxylalkoxyaryl)are described. These compounds are useful as agents for treating viruses.
摘要翻译：式I的化合物或其药学上可接受的盐，其中R是H，卤素，（C 1 -C 6）烷基，N（C 1 -C 6烷基/芳基）2，OH，O-（C 1 -C 6）烷基芳基，CH 2 OH，COOH，COO-烷基/芳基，SO 2 NH 2或SO 2 NH（C 1 -C 6烷基/芳基）; R 1是C 1 -C 6烷基，环烷基，C 2 -C 6烯基，杂芳基，取代的杂芳基，杂环烷基，-CH 2 - 芳基，-CH 2 - 取代的芳基，-CH 2 - 杂芳基或-CH 2 - 取代的杂芳基; R2是H，C1-C6烷基或芳基; 是芳环或杂芳环; 并且X是O或N-（烷基/芳基/烷基 - 芳基/烷氧基烷氧基芳基）。这些化合物可用作治疗病毒的药剂。

10. 发明授权

US08114879B2 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：哌嗪衍生物可用作CCR5拮抗剂
公开(公告)号：US08114879B2
公开(公告)日：2012-02-14
申请号：US12055900
申请日：2008-03-26
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： A61K31/497 , C07D403/00
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; R1是氢或烷基; R 2是取代的苯基，取代的杂芳基，芴基，二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R4，R5和R7是氢或烷基; R6是氢，烷基或烯基; 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

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