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1. 发明申请

WO2005047246A1 NOVEL 1, 3-DISUBSTITUTED AZETIDINE DEIVATIVES FOR USE AS 5HT2A RECEPTOR LIGANDS 审中-公开
标题翻译：用作5HT2A受体配体的新一代，3 - 取代的AZETIDINE DEIVA
公开(公告)号：WO2005047246A1
公开(公告)日：2005-05-26
申请号：PCT/GB2004/004627
申请日：2004-11-02
申请人： MERCK SHARP & DOHME LIMITED , CHAMBERS, Mark, Stuart , CURTIS, Neil, Roy , MACLEOD, Angus, Murray , MAXEY, Robert, James , SZEKERES, Helen, Jane
发明人： CHAMBERS, Mark, Stuart , CURTIS, Neil, Roy , MACLEOD, Angus, Murray , MAXEY, Robert, James , SZEKERES, Helen, Jane
IPC分类号： C07D205/04
CPC分类号： C04B35/632 , C07D205/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07D409/06 , C07D413/06 , C07D417/06 , C07D417/14 , C07D495/04
摘要： Compounds of formula (I): are antagonists of the human 5-HT 2A receptor, and hence useful in treatment or prevention of a variety of neurological conditions.
摘要翻译：式（I）化合物：是人类5-HT 2A受体的拮抗剂，因此可用于治疗或预防各种神经病症。

2. 发明申请

WO2003048118A1 5-HT7 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 5-HT7受体拮抗剂
公开(公告)号：WO2003048118A1
公开(公告)日：2003-06-12
申请号：PCT/GB2002/005396
申请日：2002-11-29
申请人： MERCK SHARP & DOHME LIMITED , CURTIS, Neil, Roy , HUNT, Peter, Alan , KULAGOWSKI, Janusz, Jozef
发明人： CURTIS, Neil, Roy , HUNT, Peter, Alan , KULAGOWSKI, Janusz, Jozef
IPC分类号： C07C311/20
CPC分类号： C07D295/135 , C07C311/20 , C07C2601/08 , C07C2601/10 , C07D211/14 , C07D211/18 , C07D211/34 , C07D211/46 , C07D211/70 , C07D217/04 , C07D333/34 , C07D409/12
摘要： Substituted carbocyclic sulphonamide derivatives of formula (I), in which n is 0 or 1 and the other variables are as defined in the clains, are selective 5-HT 7 receptor antagonists and are thereby effective in the treatment of a variety of neurological conditions, including depression and sleep disorders.
摘要翻译：取代的式（I）的碳环磺酰胺衍生物，其中n为0或1，其他变量如在该位上所定义的选择性的5-HT 7受体拮抗剂，因此有效治疗各种神经病症，包括抑郁症和睡眠障碍。

3. 发明申请

WO1998024439A1 USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING SEVERE ANXIETY DISORDERS 审中-公开
标题翻译：使用NK-1受体拮抗剂治疗严重的恶心病
公开(公告)号：WO1998024439A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006683
申请日：1997-11-25
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , CURTIS, Neil, Roy , ELLIOTT, Jason, Matthew , HARRISON, Timothy , HOLLINGWORTH, Gregory, John , JACKSON, Philip, Stephen , KULAGOWSKI, Janusz, Jozef , RUPNIAK, Nadia, Melanie , SEWARD, Eileen, Mary , SWAIN, Christopher, John , WILLIAMS, Brian, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： A61K31/535
CPC分类号： A61K31/661 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675 , C07D211/56 , C07D491/10
摘要： The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist in a medicament adapted for oral administration for the treatment or prevention of severe anxiety disorders without concomitant therapy with other anti-anxiety agents, methods of treatment using such an NK-1 receptor antagonist and pharmaceutical compositions comprising it.
摘要翻译：本发明提供口服活性的长效中枢神经系统渗透性NK-1受体拮抗剂在适于口服给药以治疗或预防严重焦虑症的药物中的用途，而不与其他抗焦虑剂并用治疗，方法使用这种NK-1受体拮抗剂的治疗剂和包含它的药物组合物。

4. 发明申请

WO1998001450A1 SPIRO-PIPERIDINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译：螺旋哌啶衍生物及其作为治疗剂的用途
公开(公告)号：WO1998001450A1
公开(公告)日：1998-01-15
申请号：PCT/GB1997001710
申请日：1997-06-24
申请人： MERCK SHARP & DOHME LIMITED , CURTIS, Neil, Roy , HUSCROFT, Ian, Thomas , KULAGOWSKI, Janusz, Jozef , SWAIN, Christopher, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D491/107
CPC分类号： C07D491/10 , A61K31/438
摘要： The present invention relates to compounds of formula (I), wherein R is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C3-7cycloalyklC1-4alkyl, which groups are optionally substituted by hydroxy, C1-4alkoxy or NR R , where R and R each independently represent hydrogen or C1-4alkyl; or R is C1-4alkyl substituted by Ar, and optionally further substituted by one or both of R and R ; R , R and R represent a variety of substituents; R and R are each hydrogen, halogen, C1-6alkyl, CH2OR , oxo, CO2R or CONR R where R represents hydrogen, C1-6alkyl or phenyl; X is -CH2, or -CH2CH2-; Y is -CH=, -CH2-, -CH2CH= or -CH2CH2-, with the proviso that the sum total of carbon atoms in X+Y is 2 or 3; and when Y is -CH= or -CH2CH=, the broken line is a double bond; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
摘要翻译：本发明涉及式（I）化合物，其中R为C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，该基团任选被羟基，C 1-4烷氧基或NR 其中R a和R b各自独立地表示氢或C 1-4烷基; 或R为被Ar取代的C 1-4烷基，且任选进一步被R 4和R 5中的一个或两个取代; R 1，R 2和R 3代表各种取代基; R 9和R 10各自为氢，卤素，C 1-6烷基，CH 2 OH，氧代，CO 2 R a或CONR a R b，其中R e表示氢，C 1-6烷基或苯基; X是-CH 2或-CH 2 CH 2 - ; Y是-CH =，-CH 2 - ， - CH 2 CH =或-CH 2 CH 2 - ，条件是X + Y中的碳原子总数为2或3; 当Y为-CH =或-CH 2 CH =时，虚线为双键; 或其药学上可接受的盐。该化合物特别用于治疗或预防疼痛，炎症，偏头痛，呕吐和带状疱疹后神经痛。

5. 发明申请

WO1998024447A1 USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING COGNITIVE DISORDERS 审中-公开
标题翻译：使用NK-1受体拮抗剂治疗认知障碍
公开(公告)号：WO1998024447A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006940
申请日：1997-11-25
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , CURTIS, Neil, Roy , ELLIOTT, Jason, Matthew , HARRISON, Timothy , HOLLINGWORTH, Gregory, John , JACKSON, Philip, Stephen , KULAGOWSKI, Janusz, Jozef , RUPNIAK, Nadia, Melanie , SEWARD, Eileen, Mary , SWAIN, Christopher, John , WILLIAMS, Brian, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： A61K31/535
CPC分类号： A61K31/661 , A61K31/00 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675 , C07D211/56 , C07D491/10
摘要： The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist for the manufacture of a medicament adapted for oral administration for the treatment or prevention of cognitive disorders, methods of medical treatment using such an NK-1 receptor antagonist and pharmaceutical compositions comprising it.
摘要翻译：本发明提供口服活性的长效CNS渗透剂NK-1受体拮抗剂在制备适于口服给药以治疗或预防认知障碍的药物中的用途，使用这种NK- 1受体拮抗剂和包含它的药物组合物。

6. 发明申请

WO1998024444A1 USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING SUBSTANCE USE DISORDERS 审中-公开
标题翻译：使用NK-1受体拮抗剂治疗物质使用障碍
公开(公告)号：WO1998024444A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006690
申请日：1997-11-25
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , CURTIS, Neil, Roy , ELLIOTT, Jason, Matthew , HARRISON, Timothy , HOLLINGWORTH, Gregory, John , JACKSON, Philip, Stephen , KULAGOWSKI, Janusz, Jozef , RUPNIAK, Nadia, Melanie , SEWARD, Eileen, Mary , SWAIN, Christopher, John , WILLIAMS, Brian, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： A61K31/535
CPC分类号： A61K31/661 , A61K31/00 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675 , C07D211/56 , C07D491/10 , Y10S514/81 , Y10S514/811 , Y10S514/812 , Y10S514/813
摘要： The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist for the manufacture of a medicament adapted for oral administration for the treatment or prevention of substance use disorders, methods of treatment using such a NK-1 receptor antagonist and pharmaceutical compositions comprising the same.
摘要翻译：本发明提供口服活性的长效CNS渗透剂NK-1受体拮抗剂在制备适于口服给药以治疗或预防物质使用障碍的药物中的用途，使用这种NK- 1受体拮抗剂和包含其的药物组合物。

7. 发明申请

WO1998024442A1 USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING SEXUAL DYSFUNCTION 审中-公开
标题翻译：使用NK-1受体拮抗剂治疗性功能障碍
公开(公告)号：WO1998024442A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006687
申请日：1997-11-25
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , CURTIS, Neil, Roy , ELLIOTT, Jason, Matthew , HARRISON, Timothy , HOLLINGWORTH, Gregory, John , JACKSON, Philip, Stephen , KULAGOWSKI, Janusz, Jozef , RUPNIAK, Nadia, Melanie , SEWARD, Eileen, Mary , SWAIN, Christopher, John , WILLIAMS, Brian, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： A61K31/535
CPC分类号： A61K31/445 , A61K9/2018 , A61K31/5375
摘要： The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist for the manufacture of a medicament adapted for oral administration for the treatment or prevention of sexual dysfunctions, methods of treatment using such an NK-1 receptor antagonist and pharmaceutical compositions comprising it.
摘要翻译：本发明提供了口服活性的长效CNS渗透剂NK-1受体拮抗剂在制备适于口服给药以治疗或预防性功能障碍的药物中的用途，使用这种NK-1 受体拮抗剂和包含它的药物组合物。

8. 发明申请

WO1996005200A1 TETRAHYDROPYRIDINYLMETHYL DERIVATIVES OF PYRROLO[2,3-b]PYRIDINE 审中-公开
标题翻译：吡咯并[2,3-b]吡啶的四氢吡啶并咪唑衍生物
公开(公告)号：WO1996005200A1
公开(公告)日：1996-02-22
申请号：PCT/GB1995001820
申请日：1995-08-01
申请人： MERCK SHARP & DOHME LIMITED , CURTIS, Neil, Roy , KULAGOWSKI, Janusz, Jozef , LEESON, Paul, David , RIDGILL, Mark, Peter
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： A class of pyrrolo[2,3-b]pyridine derivatives of formula (I), wherein Q represents a moiety of formula Qa or Qb, are ligands for dopamine receptor subtypes within the body, in particular the dopamine D4 receptor subtype and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, including schizophrenia.
摘要翻译：一类式（I）的吡咯并[2,3-b]吡啶衍生物，其中Q表示式Qa或Qb的部分是体内多巴胺受体亚型的配体，特别是多巴胺D4受体亚型，因此可用于治疗和/或预防多巴胺系统疾病，包括精神分裂症。

9. 发明申请

WO2006059149A8 ARYLSULFONYLNAPHTHALENE DERIVATIVES AS 5HT2A ANTAGONISTS 审中-公开
标题翻译：作为5HT2A拮抗剂的芳基磺酰基萘乙烯衍生物
公开(公告)号：WO2006059149A8
公开(公告)日：2006-11-02
申请号：PCT/GB2005050215
申请日：2005-11-28
申请人： MERCK SHARP & DOHME , CHAMBERS MARK STUART , CURTIS NEIL ROY , GANCIA EMANUELA , GILLIGAN MYRA , HUMPHRIES ALEXANDER CHARLES , LADDUWAHETTY TAMARA , MAXEY ROBERT JAMES , MERCHANT KEVIN JOHN
发明人： CHAMBERS MARK STUART , CURTIS NEIL ROY , GANCIA EMANUELA , GILLIGAN MYRA , HUMPHRIES ALEXANDER CHARLES , LADDUWAHETTY TAMARA , MAXEY ROBERT JAMES , MERCHANT KEVIN JOHN
IPC分类号： C07C317/14 , A61K31/10 , A61K31/275 , A61K31/4409 , A61K31/47 , A61P25/00 , C07C311/08 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/42 , C07C317/44 , C07C323/65 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/71 , C07D215/36 , C07D215/60 , C07D233/54 , C07D241/12 , C07D249/06 , C07D249/08 , C07D249/18 , C07D261/08 , C07D271/10 , C07D277/26 , C07D333/34 , C07D401/12 , C07D471/02 , C07D471/04 , C07D473/38
CPC分类号： C07D401/12 , C07C311/08 , C07C317/14 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/42 , C07C317/44 , C07C323/65 , C07C2601/04 , C07D213/61 , C07D213/64 , C07D213/70 , C07D215/36 , C07D215/60 , C07D233/64 , C07D241/12 , C07D249/06 , C07D249/08 , C07D249/18 , C07D261/08 , C07D271/10 , C07D277/26 , C07D333/34 , C07D471/04 , C07D473/38
摘要： Compounds of formula (I) are potent and selective 5-HT 2A antagonists, useful in treatment of a variety of adverse conditions of the CNS.
摘要翻译：式（I）化合物是有效的和选择性的5-HT 2A拮抗剂，可用于治疗CNS的各种不利条件。

10. 发明申请

WO2005047247A1 NOVEL1,3-DISUBSTITUTED AZETIDINE DERIVATIVES FOR USE AS 5HT2A RECEPTOR LIGANDS 审中-公开
标题翻译：用作5HT2A受体配体的新型1,3取代的AZETIDINE衍生物
公开(公告)号：WO2005047247A1
公开(公告)日：2005-05-26
申请号：PCT/GB2004/004631
申请日：2004-11-02
申请人： MERCK SHARP & DOHME LIMITED , CHAMBERS, Mark, Stuart , CURTIS, Neil, Roy , MACLEOD, Angus, Murray , MAXEY, Robert, James , SZEKERES, Helen, Jane
发明人： CHAMBERS, Mark, Stuart , CURTIS, Neil, Roy , MACLEOD, Angus, Murray , MAXEY, Robert, James , SZEKERES, Helen, Jane
IPC分类号： C07D205/04
CPC分类号： C04B35/632 , C07D205/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07D409/06 , C07D413/06 , C07D417/06 , C07D417/14 , C07D495/04
摘要： Compounds of formula (I): are antagonists of the human 5-HT 2A receptor, and hence are useful in treatment or prevention of a variety of neurological conditions.
摘要翻译：式（I）化合物：是人5-HT 2A受体的拮抗剂，因此可用于治疗或预防各种神经病症。

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