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1. 发明申请

WO2004041826A8 IMIDAZOPYRAZINONES AND IMIDAZOTRIAZINONES DERIVATES AS GABA-A RECEPTOR ANXIOLYTIC 审中-公开
标题翻译：咪唑并吡嗪酮和咪达唑仑衍生物作为GABA-A受体拮抗剂
公开(公告)号：WO2004041826A8
公开(公告)日：2005-06-30
申请号：PCT/GB0304685
申请日：2003-10-29
申请人： MERCK SHARP & DOHME , CARLING WILLIAM ROBERT , CASTRO PINEIRO JOSE LUIS , GOODACRE SIMON CHARLES , HALLETT DAVID JAMES , STREET LESLIE JOSEPH
发明人： CARLING WILLIAM ROBERT , CASTRO PINEIRO JOSE LUIS , GOODACRE SIMON CHARLES , HALLETT DAVID JAMES , STREET LESLIE JOSEPH
IPC分类号： A61P25/00 , C07D487/04 , A61K31/4985 , A61K31/53
CPC分类号： C07D487/04
摘要： The present invention discloses a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein -U-V- represents -CH=CH-, or -CH2-CH2-, -N=CH- or -CH=N-; X represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a -NH- or -OCH2- linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrocarbon, a heterocyclic group, trifluoromethyl, -SO2R , -SO2NR R , -COR , -CO2R or -CONR R ; and R and R independently represent hydrogen, hydrocarbon or a heterocyclic group;pharmaceutical compositions comprising it; its use in methods of treatment; use of it in the manufacture of a medicament for treating and/or preventing anxiety; convulsions or a cognitive disorder; and methods of treatment using it.
摘要翻译：本发明公开了式I化合物或其药学上可接受的盐：（I）其中-U-V-表示-CH = CH-或-CH 2 -CH 2 - ， - N = CH-或-CH = N-; X 1表示氢，卤素，C 1-6烷基，三氟甲基或C 1-6烷氧基; X 2表示氢或卤素; Y表示化学键，氧原子或-NH-或-OCH2-键; Z表示任选取代的芳基或杂芳基; R 1表示烃，杂环基，三氟甲基，-SO 2 R a，-SO 2 NR a R b，-COR a，-CO 2 R a或-CONR a R b; R a和R b独立地表示氢，烃或杂环基;包含它的药物组合物; 其用于治疗方法; 在制备用于治疗和/或预防焦虑的药物中的用途; 抽搐或认知障碍; 和使用它的治疗方法。

2. 发明申请

WO2004065388A1 FLUOROIMIDAZOPYRIMIDINES AS GABA-A ALPHA 2/3 LIGANDS FOR DEPRESSION/ANXIETY 审中-公开
标题翻译：氟尿嘧啶嘧啶类作为GABA-A ALPHA 2/3用于抑制/抑制的配体
公开(公告)号：WO2004065388A1
公开(公告)日：2004-08-05
申请号：PCT/GB2004/000196
申请日：2004-01-21
申请人： MERCK SHARP & DOHME LIMITED , CARLING, William, Robert , GOODACRE, Simon, Charles , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph
发明人： CARLING, William, Robert , GOODACRE, Simon, Charles , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides a compound formula (I), or a pharmaceutically acceptable salt thereof: wherein W is phenyl or pyridyl; X 1 represents hydrogen, halogen, C 1-6 alkyl, trifluoromethyl or C 1-6 alkoxy; X 2 represents hydrogen or halogen; Y represents a chemical bond, an -NH- linkage or a group -OC n H 2n -; Z represents an optionally substituted aryl or heteroaryl group; R 1 represents hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, -OR a , -SR a , -SOR a , -SO 2 R a , -SO 2 NR a R b , NR a R b , -NR a COR b , -NR a CO 2 R b , -COR a , -CO 2 R a , -CONR a R b or Cr a =NOR b ; R a and R b independently represent hydrogen, hydrocarbon or a heterocyclic group; and n is zero, one, two or three; pharmaceutical compositions comprising it; its use in methods of treatment; use of it in the manufacture of medicaments to treat anxiety and/or depression; and methods of treatment for anxiety and/or depression using it.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐：其中W是苯基或吡啶基; X 1表示氢，卤素，C 1-6烷基，三氟甲基或C 1-6烷氧基; X 2表示氢或卤素; Y表示化学键，-NH-键或-OC n H 2n-基团; Z表示任选取代的芳基或杂芳基; R 1表示烃，杂环基，卤素，氰基，三氟甲基，硝基，-OR a，-SR a，-SOR a，-SO 2 R a，-SO 2 NR R a，-NR a R b，-NR a COR b，-NR a CO 2 R b，-COR a，-CO 2 R a，-CONR a R 或Cr = NOR ; R a和R b独立地表示氢，烃或杂环基; n为零，一，二或三; 包含它的药物组合物; 其用于治疗方法; 用于制造药物以治疗焦虑和/或抑郁症; 以及使用它的焦虑和/或抑郁症的治疗方法。

3. 发明申请

WO2003006464A1 (1,8) NAPHTHYRIDINES AS GABA LIGANDS, THEIR PHARMACEUTICAL COMPOSITIONS AND USES 审中-公开
标题翻译：（1,8）萘啶作为GABA配体，其药物组合物和用途
公开(公告)号：WO2003006464A1
公开(公告)日：2003-01-23
申请号：PCT/GB2002/003077
申请日：2002-07-03
申请人： MERCK SHARP & DOHME LIMITED , CARLING, William, Robert , MITCHINSON, Andrew , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph
发明人： CARLING, William, Robert , MITCHINSON, Andrew , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： A class of [1,8] naphthyridine analogues which are substituted in the 4-position by a substituted phenyl ring. These compounds are ligands for GABA A receptors and useful in the therapy of deleterious mental states such as anxiety.
摘要翻译：一类通过取代的苯环在4-位取代的[1,8]萘啶类似物。这些化合物是GABA A受体的配体，可用于治疗有害精神状态如焦虑症。

4. 发明申请

WO0138331A3 PYRAZOLO[1,5-D][1,2,4]TRIAZINES FOR ENHANCING COGNITION 审中-公开
标题翻译：吡唑并[1,5-D] [1,2,4]三嗪促进认知
公开(公告)号：WO0138331A3
公开(公告)日：2001-11-08
申请号：PCT/GB0004450
申请日：2000-11-22
申请人： MERCK SHARP & DOHME , BRYANT HELEN JANE , CARLING WILLIAM ROBERT , CHAMBERS MARK STUART , HOBBS SARAH CHRISTINE , JONES PHILIP , MACLEOD ANGUS MURRAY
发明人： BRYANT HELEN JANE , CARLING WILLIAM ROBERT , CHAMBERS MARK STUART , HOBBS SARAH CHRISTINE , JONES PHILIP , MACLEOD ANGUS MURRAY
IPC分类号： A61K31/53 , A61K31/5377 , A61P25/28 , C07D487/04 , C07D519/00
CPC分类号： C07D487/04
摘要： The present invention provides compounds of formula (I), or a salt thereof: wherein R represents halogen; or C1-6alkyl,C3-7cycloalkyl, C4-7cycloalkenyl, C6-8 bicycloalkyl, C6-10aryl, C3-7 heterocycloalkyl, heteroaryl or di(C1-6)alkylamino, any of which groups may be optionally substituted; L is O, S or NR where R is H, C1-6alkyl or C3-6cycloalkyl; W is: C1-6alkyl, C2-6alkenyl or C2-6alkynyl optionally substituted; X is NR R ; or X is a 5-membered or a 6-membered heteroaromatic ring the 5- or 6-membered heteroaromatic ring being optionally fused to a benzene or pyridine ring and the heteroaromatic ring being optionally substituted; Y is optionally branched C1-4alkylene optionally substituted by an oxo group or Y is a group (CH2)jO wherein the oxygen atom is nearest the group X and j is 2, 3 or 4; and Z represents a 5-membered or a 6-membered heteroaromatic ring any of which rings may be optionally substituted; pharmaceutical compositions containing them, their use in methods of treatment, and the use of them for manufacturing treatments for enhancing cognition, particularly in Alzheimer's Disease, and corresponding methods of treatment; the compounds are ligands and inverse agonists for the GABA-A alpha 5 receptor subtype.
摘要翻译：本发明提供了式（I）的化合物或其盐：其中R 1代表卤素; 或C1-6烷基，C3-7环烷基，C4-7环烯基，C6-8双环烷基，C6-10芳基，C3-7杂环烷基，杂芳基或二（C1-6）烷基氨基，其中任何基团可被任选取代; L是O，S或NR n，其中R n是H，C 1-6烷基或C 3-6环烷基; W为：任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基; X是NR 4 R 5; 或X为5元或6元杂芳族环，所述5或6元杂芳族环任选与苯或吡啶环稠合且所述杂芳族环任选被取代; Y是任选被氧代基团取代的支链C 1-4亚烷基或Y是基团（CH 2）j O，其中氧原子最接近基团X且j是2,3或4; Z代表5元或6元杂芳族环，其中任何一个环可以任选被取代; 含有它们的药物组合物，它们在治疗方法中的用途，以及它们用于制造用于增强认知，特别是在阿尔茨海默氏病中的治疗的用途以及相应的治疗方法; 该化合物是GABA-Aα5受体亚型的配体和反向激动剂。

5. 发明申请

WO1994026733A1 PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡嗪衍生物
公开(公告)号：WO1994026733A1
公开(公告)日：1994-11-24
申请号：PCT/GB1994000999
申请日：1994-05-09
申请人： MERCK SHARP & DOHME LIMITED , CARLING, William, Robert , COLLINS, Ian, James , LEESON, Paul, David , ROWLEY, Michael
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D409/14
摘要： A class of substituted pyrimidine derivatives are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment of disorders of the dopamine system, in particular schizophrenia.
摘要翻译：一类取代的嘧啶衍生物是体内多巴胺受体亚型的配体，因此可用于治疗多巴胺系统，特别是精神分裂症的病症。

6. 发明申请

WO2012051194A1 CYCLOSPORIN ANALOGS 审中-公开
标题翻译：环磷酰胺类似物
公开(公告)号：WO2012051194A1
公开(公告)日：2012-04-19
申请号：PCT/US2011/055791
申请日：2011-10-11
申请人： ALLERGAN, INC. , CARLING, William Robert , FRYDRYCH, Catherine Simone Victorire , GARST, Michael E. , STERN, Michael E. , SCHAUMBURG, Christopher S.
发明人： CARLING, William Robert , FRYDRYCH, Catherine Simone Victorire , GARST, Michael E. , STERN, Michael E. , SCHAUMBURG, Christopher S.
IPC分类号： C07K7/64
CPC分类号： C07K7/645 , A61K38/00 , C07K1/113
摘要： Disclosed herein are novel analogs of cyclosporin, pharmaceutical compositions containing them, and methods for their use in the treatment of dry eye and other conditions.
摘要翻译：本文公开了环孢菌素的新型类似物，含有它们的药物组合物及其用于治疗干眼症和其它病症的方法。

7. 发明申请

WO2006013393A3 QUINOLINE DERIVATIVES AS NEUROKININ RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2006013393A3
公开(公告)日：2006-02-09
申请号：PCT/GB2005/050120
申请日：2005-07-28
申请人： MERCK SHARP & DOHME LIMITED , CARLING, William Robert , ELLIOTT, Jason, Matthew , MEZZOGORI, Elena , RUSSELL, Michael, Geoffrey, Neil , WILLIAMS, Brian, John
发明人： CARLING, William Robert , ELLIOTT, Jason, Matthew , MEZZOGORI, Elena , RUSSELL, Michael, Geoffrey, Neil , WILLIAMS, Brian, John
IPC分类号： C07D215/52
摘要： The present invention relates to substituted quinoline-4-carboxylic acid hydrazides defined herein, pharmaceutical compositions comprising them and their use in treating diseases mediated by neurokinin-2 and/or neurokinin-3 (NK-3) receptors.

8. 发明申请

WO2004041826A1 IMIDAZOPYRAZINONES AND IMIDAZOTRIAZINONES DERIVATES AS GABA-A RECEPTOR ANXIOLYTIC 审中-公开
标题翻译：作为GABA-A受体ANXIOLYTIC的中等程度亚氨基和咪唑酮
公开(公告)号：WO2004041826A1
公开(公告)日：2004-05-21
申请号：PCT/GB2003/004685
申请日：2003-10-29
申请人： MERCK SHARP & DOHME LIMITED , CARLING, William, Robert , CASTRO PINEIRO, Jose, Luis , GOODACRE, Simon, Charles , HALLETT, David, James , STREET, Leslie, Joseph
发明人： CARLING, William, Robert , CASTRO PINEIRO, Jose, Luis , GOODACRE, Simon, Charles , HALLETT, David, James , STREET, Leslie, Joseph
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention discloses a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein -U-V- represents -CH=CH-, or -CH 2 -CH 2 -, -N=CH- or -CH=N-; X 1 represents hydrogen, halogen, C 1-6 alkyl, trifluoromethyl or C 1-6 alkoxy; X 2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a -NH- or -OCH 2 - linkage; Z represents an optionally substituted aryl or heteroaryl group; R 1 represents hydrocarbon, a heterocyclic group, trifluoromethyl, -SO 2 R a , -SO 2 NR a R b , -COR a , -CO 2 R a or -CONR a R b ; and R a and R b independently represent hydrogen, hydrocarbon or a heterocyclic group;pharmaceutical compositions comprising it; its use in methods of treatment; use of it in the manufacture of a medicament for treating and/or preventing anxiety; convulsions or a cognitive disorder; and methods of treatment using it.
摘要翻译：本发明公开了式I化合物或其药学上可接受的盐：（I）其中-U-V-表示-CH = CH-或-CH 2 -CH 2 - ， - N = CH-或-CH = N-; X 1表示氢，卤素，C 1-6烷基，三氟甲基或C 1-6烷氧基; X 2表示氢或卤素; Y代表化学键，氧原子或-NH-或-OCH2-键; Z表示任选取代的芳基或杂芳基; R 1表示烃，杂环基，三氟甲基，-SO 2 R a，-SO 2 NR a R b，-COR a，-CO 2 R a或-CONR a R b; R a和R b独立地表示氢，烃或杂环基;包含它的药物组合物; 其用于治疗方法; 在制备用于治疗和/或预防焦虑的药物中的用途; 惊厥或认知障碍; 和使用它的治疗方法。

9. 发明申请

WO1993011115A2 QUINOLONE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO1993011115A2
公开(公告)日：1993-06-10
申请号：PCT/GB1992002183
申请日：1992-11-25
申请人： MERCK SHARP & DOHME LIMITED , CARLING, William, Robert , LEESON, Paul, David , MOORE, Kevin, William , ROWLEY, Michael
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D215/22
CPC分类号： C07D215/227 , A61K31/47 , C07D215/42 , C07D215/50 , C07D401/06 , C07D413/06
摘要： A class of 2-(1H)-quinolone derivatives, substituted at the 3-position by an optionally substituted aryl substituent, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA receptor antagonist.
摘要翻译：在3-位被任选取代的芳基取代基取代的一类2-（1H） - 喹诺酮衍生物是NMDA受体的选择性非竞争性拮抗剂和/或是AMPA受体的拮抗剂，因此可用于治疗需要施用NMDA和/或AMPA受体拮抗剂的病症，如神经退行性疾病，抽搐或精神分裂症。

10. 发明申请

WO2012051193A1 CYCLOSPORIN ANALOGS 审中-公开
标题翻译： CYCLOSPORIN类似物
公开(公告)号：WO2012051193A1
公开(公告)日：2012-04-19
申请号：PCT/US2011/055788
申请日：2011-10-11
申请人： ALLERGAN, INC. , CARLING, William Robert , SCOWEN, David Arthur , GARST, Michael E. , STERN, Michael E. , SCHAUMBURG, Christopher S.
发明人： CARLING, William Robert , SCOWEN, David Arthur , GARST, Michael E. , STERN, Michael E. , SCHAUMBURG, Christopher S.
IPC分类号： C07K7/64
CPC分类号： A61K38/13 , C07K7/645
摘要： Disclosed herein are novel analogs of cyclosporin, pharmaceutical compositions containing them, and methods for their use in the treatment of dry eye and other conditions.
摘要翻译：本文公开了环孢菌素的新类似物，含有它们的药物组合物，以及它们用于治疗干眼症和其他疾病的方法。

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