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1. 发明申请

WO2006043064A1 PIPERIDINES AND RELATED COMPOUNDS FOR TREATMENT OF ALZHEIMER'S DISEASE 审中-公开
标题翻译：治疗阿尔茨海默病的药代动力学及相关化合物
公开(公告)号：WO2006043064A1
公开(公告)日：2006-04-27
申请号：PCT/GB2005/004040
申请日：2005-10-20
申请人： MERCK SHARP & DOHME LIMITED , HANNAM, Joanne, Clare , KULAGOWSKI, Janusz, Jozef , MADIN, Andrew , RIDGILL, Mark, Peter , SEWARD, Eileen, Mary
发明人： HANNAM, Joanne, Clare , KULAGOWSKI, Janusz, Jozef , MADIN, Andrew , RIDGILL, Mark, Peter , SEWARD, Eileen, Mary
IPC分类号： C07D211/34 , C07D211/60 , C07D211/62 , C07D471/08 , C07D401/06 , C07D207/08 , C07D241/04 , A61K31/451 , A61K31/496 , A61K31/40 , A61P25/28
CPC分类号： C07D471/08 , C07D207/08 , C07D211/34 , C07D211/60 , C07D211/62 , C07D241/04 , C07D401/06
摘要： Compounds of formula (I), selectively inhibit production of Aβ (1-42) and hence are useful in treatment or prevention of disease assocaited with deposition of β -amyloid in the brain.
摘要翻译：式（I）化合物选择性地抑制Aβ的产生（1-42），因此可用于治疗或预防脑中沉淀β-淀粉样蛋白的疾病。

2. 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。

3. 发明申请

WO1996029328A1 MORPHOLINE DERIVATIVES, COMPOSITIONS CONTAINING THEM AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译：吗啉衍生物，它们的组合物及其作为治疗剂的用途
公开(公告)号：WO1996029328A1
公开(公告)日：1996-09-26
申请号：PCT/GB1996000587
申请日：1996-03-13
申请人： MERCK SHARP & DOHME LIMITED , HAWORTH, Karen, Elizabeth , OWEN, Simon, Neil , SEWARD, Eileen, Mary
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： The present invention relates to compounds of formula (I), wherein R and R represent hydrogen, halogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, C1-6alkoxy, C1-4alkyl substituted by a hydroxy or C1-4alkoxy group, OCF3, hydroxy, trifluoromethyl, trimethylsilyl, nitro, CN, SR , SOR , SO2R , COR , CO2R or CONR R , where R and R are each independently hydrogen or C1-4alkyl; R , R and R represent hydrogen, halogen, C1-6alkyl, C1-6alkoxy substituted by a C1-4alkoxy group, or trifluoromethyl; R represents C1-6alkyl, optionally substituted by oxo, substituted by a 5-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, oxadiazole and thiadiazole, wherein each heteroaromatic ring is substituted at the available carbon atom by a group of the formula: ZNR R . The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.
摘要翻译：本发明涉及式（I）化合物，其中R 1和R 4表示氢，卤素，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，C 1 C 1-6烷氧基，被羟基或C 1-4烷氧基取代的C 1-4烷基，OCF 3，羟基，三氟甲基，三甲基甲硅烷基，硝基，CN，SR a，SOR a，SO 2 R a， a>或CONR a R b，其中R a和R b各自独立地为氢或C 1-4烷基; R 2，R 3和R 5表示氢，卤素，C 1-6烷基，被C 1-4烷氧基取代的C 1-6烷氧基或三氟甲基; R 6表示任选被氧代取代的，被选自恶唑，噻唑，异恶唑，异噻唑，恶二唑和噻二唑的5元杂芳环取代的C 1-6烷基，其中每个杂芳环在可用碳原子上被一个基团取代式：ZNR 7 R 8。该化合物特别用于治疗疼痛，炎症，偏头痛和呕吐。

4. 发明申请

WO2010136491A1 BICYCLIC INDOLE-PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE 审中-公开
标题翻译：用于P110 DELTA选择性的双相吲哚吡啶PI3K抑制剂化合物及其使用方法
公开(公告)号：WO2010136491A1
公开(公告)日：2010-12-02
申请号：PCT/EP2010/057244
申请日：2010-05-26
申请人： F. HOFFMANN-LA ROCHE AG , CASTANEDO, Georgette , GOLDSTEIN, David, Michael , KONDRU, Rama, K. , LUCAS, Matthew, C. , PALMER, Wylie, Solang , PRICE, Stephen , SAFINA, Brian , SAVY, Pascal, Pierre, Alexandre , SEWARD, Eileen, Mary , SUTHERLIN, Daniel, P. , SWEENEY, Zachary, Kevin
发明人： CASTANEDO, Georgette , GOLDSTEIN, David, Michael , KONDRU, Rama, K. , LUCAS, Matthew, C. , PALMER, Wylie, Solang , PRICE, Stephen , SAFINA, Brian , SAVY, Pascal, Pierre, Alexandre , SEWARD, Eileen, Mary , SUTHERLIN, Daniel, P. , SWEENEY, Zachary, Kevin
IPC分类号： C07D487/04 , C07D495/04 , C07D513/04 , A61K31/519 , A61K31/52 , A61P37/00
CPC分类号： C07D495/04 , C07D487/04 , C07D513/04
摘要： Formula I (Ia and Ib) compounds wherein (i) X 1 is N and X 2 is S, (ii) X 1 is CR 7 and X 2 is S, (iii) X 1 is N and X 2 is NR 2 , (iv) X 1 is CR 7 and X 2 is O, or (v) X 1 is CR 7 and X 2 is NR 2 , including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PBK, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译：式（I）和（Ib）化合物，其中（i）X1为N，X2为S，（ii）X1为CR7，X2为S，（iii）X1为N，X2为NR2，（iv）X1为CR7和X2 是O，或（v）X1是CR7，X2是NR2，包括立体异构体，互变异构体，代谢物和药学上可接受的盐，可用于抑制PBK的δ同种型，以及用于治疗脂质激酶介导的疾病，例如炎症，免疫学，和癌症。公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

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

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。

9. 发明申请

WO1998024443A1 USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING BIPOLAR DISORDERS 审中-公开
标题翻译：使用NK-1受体拮抗剂治疗双极性疾病
公开(公告)号：WO1998024443A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006688
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 bipolar disorder without concomitant therapy with other antidepressant or anti-anxiety agents, methods of treatment using such an 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渗透性NK-1受体拮抗剂用于制造适于口服给药以治疗或预防双相情感障碍而不伴随其它抗抑郁药或抗焦虑治疗的药物的用途药剂，使用这种NK-1受体拮抗剂的治疗方法和包含其的药物组合物。

10. 发明申请

WO1998024441A1 USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING MAJOR DEPRESSIVE DISORDERS WITH ANXIETY 审中-公开
标题翻译： NK-1受体拮抗剂用于治疗主要恶性疾病的药物
公开(公告)号：WO1998024441A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006686
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 major depressive disorder with anxiety without concomitant therapy with other anti-depressant or anti-anxiety agents, 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受体拮抗剂用于制造适于口服给药以治疗或预防焦虑症的重度抑郁障碍的药物的用途，抑制剂或抗焦虑剂，使用这种NK-1受体拮抗剂的治疗方法和包含其的药物组合物。

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