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1. 发明申请

WO1997001553A1 PIPERIDINE AND MORPHOLINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译：哌啶和吗啉衍生物及其作为治疗剂的用途
公开(公告)号：WO1997001553A1
公开(公告)日：1997-01-16
申请号：PCT/GB1996001478
申请日：1996-06-20
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , ELLIOTT, Jason , STEVENSON, Graeme, Irvine , SWAIN, Christopher, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D403/14
CPC分类号： C07D401/14
摘要： The present invention provides compounds of formula (I), wherein R is a 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms selected from nitrogen, oxygen and sulphur, which group is optionally substituted; R is hydrogen, halogen, C1-6alkyl, C1-6alkoxy, CF3, OCF3, NO2, CN, SR , SOR , SO2R , CO2R , CONR R , C2-6alkenyl, C2-6alkynyl or C1-4alkyl substitued by C1-4alkoxy, where R and R each independently represent hydrogen or C1-4alkyl; R is hydrogen, halogen, C1-6alkyl, C1-6alkoxy substituted by C1-4alkoxy or CF3; R , R , R , R , R , A, X and Y are as defined in the specification; and m is zero or 1, and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
摘要翻译：本发明提供式（I）化合物，其中R 1是含有1,2,3或4个选自氮，氧和硫的杂原子的5-或6-元芳族杂环基，该基团任选被取代; R 2是氢，卤素，C 1-6烷基，C 1-6烷氧基，CF 3，OCF 3，NO 2，CN，SR a，SOR a，SO 2 R a，CO 2 R a，CONR C 1-6烷基，C 2-6炔基或被C 1-4烷氧基取代的C 1-4烷基，其中R a和R b各自独立地表示氢或C 1-4烷基; R 3是氢，卤素，C 1-6烷基，被C 1-4烷氧基或CF 3取代的C 1-6烷氧基; R 4，R 5，R 6，R 9a，R 9b，A，X和Y如说明书中所定义; 和m为0或1，及其药学上可接受的盐和前药。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。

2. 发明申请

WO1997001554A1 PIPERIDINE AND MORPHOLINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译：哌啶和吗啉衍生物及其作为治疗剂的用途
公开(公告)号：WO1997001554A1
公开(公告)日：1997-01-16
申请号：PCT/GB1996001477
申请日：1996-06-20
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , ELLIOTT, Jason , STEVENSON, Graeme, Irvine , SWAIN, Christopher, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D405/14
CPC分类号： C07D405/14
摘要： The present invention provides compounds of formula (I), wherein R is phenyl or a 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur, which aryl or heteroaryl group is optionally substituted; R is hydrogen, halogen, C1-6alkyl, C1-6alkoxy, CF3, OCF3, NO2, CN, SR , SOR , SO2R , CO2R , CONR R , C2-6alkenyl, C2-6alkynyl or C1-4alkyl substituted by C1-4alkoxy, where R and R each independently represent hydrogen or C1-4alkyl; R , R , R , R and R , A, X, and Y are as defined in the specification; the dotted line is an optional double bond; Q is oxygen, sulphur or -NH-; Q is -N=, -NH-, -CH= or -CH2-; and m is zero or 1; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
摘要翻译：本发明提供式（I）化合物，其中R 1为苯基或含有1,2,3或4个选自氮，氧和硫的杂原子的5或6元芳族杂环基，该芳基或杂芳基任选被取代; R 2是氢，卤素，C 1-6烷基，C 1-6烷氧基，CF 3，OCF 3，NO 2，CN，SR a，SOR a，SO 2 R a，CO 2 R a，CONR C 2-6烯基，C 2-6炔基或被C 1-4烷氧基取代的C 1-4烷基，其中R a和R b各自独立地表示氢或C 1-4烷基; R 4，R 5，R 6，R 9a和R 9b，A，X和Y如说明书中所定义; 虚线是可选的双键; Q 1是氧，硫或-NH-; Q 2是-N =，-NH-，-CH =或-CH 2 - ; m为0或1; 及其药学上可接受的盐和前药。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。

3. 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。

4. 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。

5. 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。

6. 发明申请

WO1998024445A1 USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING SCHIZOPHRENIC DISORDERS 审中-公开
标题翻译：使用NK-1受体拮抗剂治疗嗜酸性粒细胞减少症
公开(公告)号：WO1998024445A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006691
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 for the manufacture of a medicament adapted for oral administration for the treatment or prevention of schizophrenic disorders, methods of treatment using such a 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精神分裂症的药物中的用途，使用这种NK-1 受体拮抗剂和包含它的药物组合物。

7. 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。

8. 发明申请

WO1998024440A1 USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING STRESS DISORDERS 审中-公开
标题翻译：使用NK-1受体拮抗剂治疗应激障碍
公开(公告)号：WO1998024440A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006684
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 for the manufacture of a medicament adapted for oral administration for the treatment or prevention of stress disorders without concomitant therapy with other anti-stress agents, methods of treatment using such a 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受体拮抗剂用于制造适于口服给药以治疗或预防应激障碍的药物的用途，而不与其它抗应激剂并行治疗，使用这样的NK-1受体拮抗剂的治疗方法和包含它的药物组合物。

9. 发明申请

WO1997021702A1 3-BENZYLAMINOPYRROLIDINES AND -PIPERIDINES AS TACHYKININ RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为TACHYKININ受体拮抗剂的3-苄氧基吡啶和哌嗪
公开(公告)号：WO1997021702A1
公开(公告)日：1997-06-19
申请号：PCT/GB1996002998
申请日：1996-12-06
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , ELLIOTT, Jason , SWAIN, Christopher, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D403/12
摘要： The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein R is an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1,2,3 or 4 heteroatoms selected from nitrogen, oxygen and sulphur; R and R represent a variety of substituents; R is H or C1-6alkyl; R is H, halogen, C1-6alkyl, C1-6alkoxy substituted by C1-4alkoxy or CF3; R is H or C1-6alkyl; R is C1-6alkyl optionally substituted by a hydroxy group or the group -CO2R , where R is C1-6alkyl; R is halogen, C1-6alkyl, oxo, CO2R or CONR R ; m is zero or 1; n is 1 or 2; and q is zero, 1 or 2. 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）化合物或其药学上可接受的盐或前药，其中R 1为含有1,2,3或4个选自氮的杂原子的任选取代的5-或6-元芳族杂环基，氧和硫; R 2和R 4代表各种取代基; R 3是H或C 1-6烷基; R 5是H，卤素，C 1-6烷基，被C 1-4烷氧基或CF 3取代的C 1-6烷氧基; R 6a是H或C 1-6烷基; R 6b是任选被羟基或-CO 2 R c基团取代的C 1-6烷基，其中R c是C 1-6烷基; R 9是卤素，C 1-6烷基，氧代，CO 2 R a或CONR a R b; m为零或1; n为1或2; q为零，1或2.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。

10. 发明申请

WO1998024446A1 USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING MOVEMENT DISORDERS 审中-公开
标题翻译：使用NK-1受体拮抗剂治疗运动障碍
公开(公告)号：WO1998024446A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006692
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 antagonist for the manufacture of a medicament for oral administration for the treatment or prevention of movement disorders, methods of treatment using such a 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拮抗剂在制备用于口服给药以治疗或预防运动障碍的药物中的用途，使用这种NK-1受体拮抗剂的治疗方法和包含它的药物组合物。

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