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1. 发明申请

WO2004089911A1 PYRAZOLE DERIVATIVES AS GAMMA-SECRETASE INHIBITORS USEFUL IN THE TREATMENT OF ALZHEIMER’S DISEASE 审中-公开
标题翻译：用作治疗阿尔茨海默病的GAMMA-分泌酶抑制剂的吡唑衍生物
公开(公告)号：WO2004089911A1
公开(公告)日：2004-10-21
申请号：PCT/GB2004/001452
申请日：2004-04-01
申请人： MERCK SHARP & DOHME LIMITED , BETTATI, Michela , CHAMBERS, Mark, Stuart , HUNT, Peter, Alan , JONES, Philip , MACLEOD, Angus, Murray , SZEKERES, Helen, Jane , TEALL, Martin, Richard
发明人： BETTATI, Michela , CHAMBERS, Mark, Stuart , HUNT, Peter, Alan , JONES, Philip , MACLEOD, Angus, Murray , SZEKERES, Helen, Jane , TEALL, Martin, Richard
IPC分类号： C07D231/12
CPC分类号： C07D231/12 , C07D401/04 , C07D401/06 , C07D409/12
摘要： The compounds of formula (I): inhibit gamma-secretase and hence are of utility in the treatment or prevention of Alzheimer's disease.
摘要翻译：式（I）化合物：抑制γ-分泌酶，因此可用于治疗或预防阿尔茨海默氏病。

2. 发明申请

WO2003048132A1 IMIDAZOPYRIDINES, PYRIMIDINES AND TRIAZINES FOR ENHANCING COGNITION AS GABA-A ALPHA 5 RECEPTOR SUBTYPE LIGANDS 审中-公开
标题翻译：用于增强作为GABA-ALPHA 5受体亚型配体的认知的咪唑吡啶，嘧啶和三嗪
公开(公告)号：WO2003048132A1
公开(公告)日：2003-06-12
申请号：PCT/GB2002/005337
申请日：2002-11-27
申请人： MERCK SHARP & DOHME LIMITED , BETTATI, Michela , CHAMBERS, Mark, Stuart , HUMPHRIES, Alexander, Charles , JONES, Philip , LEWIS, Richard, Thomas , MAXEY, Robert, James , SZEKERES, Helen, Jane , TEALL, Martin, Richard
发明人： BETTATI, Michela , CHAMBERS, Mark, Stuart , HUMPHRIES, Alexander, Charles , JONES, Philip , LEWIS, Richard, Thomas , MAXEY, Robert, James , SZEKERES, Helen, Jane , TEALL, Martin, Richard
IPC分类号： C07D235/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides a pharmaceutical composition providing a compound of formula I or a pharmaceutically acceptable salt thereof in a pharmaceutically acceptable excipient: (I), in which: X and Y independently represent CH or N, with the proviso that if X is CH then Y is also CH; R 1 represents hydrogen, 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; V and W are independently selected from H, halogen, C -1-6 alkyl, OH and C -1-6 alkoxy; Z represents H, halogen, CN, NO 2 , CF 3 , OCF 3 , CF 2 H, SCF 3 , R 2 , OR 3 , SR 3 , (CH 2 )pN(R 3 ) 2 , O(CH 2 )pN(R 3 ) 2 , SO 2 R 2 , SO 2 N(R 3 ) 2 , COR 4 , CO 2 R 3 , CON(R 3 ) 2 , NHCOR 4 , NR 1 (CH 2 ) n heteroaryl or O(CH 2 ) n heteroaryl the heteroaryl is optionally substituted by one, two or three groups chosen from C 1-6 alkyl, benzyl, (CH 2 )pN(R 3 ) 2 , halogen and CF 3 , R 1 is C 1-6 alkyl, where n is 1 or 2 and p is 0, 1 or 2; with the proviso that at least one of V, W and Z is other than H; R 2 represents C 1-6 alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkylC 1-4 alkyl, C 2-6 alkenyl, C 2-6 alkynyl or heteroaryl, any of which may bear a substituent selected from halogen, CN, NO 2 , CF 3 , OCF 3 , CF 2 H, SCF 3 , OH, C 1-4 alkoxy, C 1-4 alkoxycarbonyl, amino, C 1-4 alkylamino, or di(C 1-4 alkyl)amino; R 3 represents H or R 2 ; or two R 3 groups bonded to the same nitrogen atom may complete a 5-7 membered nonaromatic heterocyclic ring; and R 4 represents R 3 or heteroaryl; the compounds are ligands for GABA-A receptors containing the alpha 5 subtype and thus are useful for enhancing cognition in individuals suffering from conditions such as Alzheimer's Disease.
摘要翻译：本发明提供在药学上可接受的赋形剂中提供式I化合物或其药学上可接受的盐的药物组合物：其中：X和Y独立地表示CH或N，条件是如果X是CH则 Y也是CH; R 1表示氢，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 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 或CR = NOR ; R a和R b独立地表示氢，烃或杂环基; V和W独立地选自H，卤素，C 1-6烷基，OH和C 1-6烷氧基; Z表示H，卤素，CN，NO 2，CF 3，OCF 3，CF 2 H，SCF 3，R 2，OR 3，SR 3，（CH 2）pN（R 3）2，O（CH 2）p N （R 3）2，SO 2 R 2，SO 2 N（R 3）2，COR 4，CO 2 R 3，CON（R 3）2，NHCOR 4，NR 1 （CH2）杂芳基或O（CH2）杂芳基，杂芳基任选被一个，两个或三个选自C 1-6烷基，苄基，（CH 2）pN（R 3）2，卤素和CF 3，R 1，是C 1-6烷基，其中n是1或2，p是0,1或2; 条件是V，W和Z中的至少一个不是H; R 2表示C 1-6烷基，C 3-6环烷基，C 3-6环烷基C 1-4烷基，C 2-6烯基，C 2-6炔基或杂芳基，其中任何一个可以带有选自卤素，CN，NO 2，CF 3，OCF 3，CF 2 H，SCF 3，OH ，C 1-4烷氧基，C 1-4烷氧基羰基，氨基，C 1-4烷基氨基或二（C 1-4烷基）氨基; R 3表示H或R 2; 或两个与相同氮原子键合的R 3基团可以完成5-7元非芳族杂环; 并且R 4表示R 3或杂芳基; 该化合物是含有α5亚型的GABA-A受体的配体，因此可用于增强患有诸如阿尔茨海默氏病等疾病的个体的认知。

3. 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。

4. 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。

5. 发明申请

WO2004072045A1 SUBSTITUTED QUINOLINE-4-CARBOXYLIC HYDRAZIDES AS NK-2/NK-3 RECEPTOR LIGANDS 审中-公开
标题翻译：作为NK-2 / NK-3受体配体的取代的喹啉-4-羧氧基水杨酸
公开(公告)号：WO2004072045A1
公开(公告)日：2004-08-26
申请号：PCT/GB2004/000415
申请日：2004-02-03
申请人： MERCK SHARP & DOHME LIMITED , CHAMBERS, Mark, Stuart , JONES, Philip , MACLEOD, Angus, Murray
发明人： CHAMBERS, Mark, Stuart , JONES, Philip , MACLEOD, Angus, Murray
IPC分类号： C07D215/52
CPC分类号： C07D215/52
摘要： The present invention discloses a compound of formula (I): wherein: R 1 is an aryl or heteroaryl ring; R 2 is hydroxy, C 1-6 alkoxy, C 1-6 alkyl, amino, NR'R" or C 1-6 alkyl-NR'R" where R' and R" are independently chosen from hydrogen and C 1-4 alkyl and where R' and R", together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing 3-7 membered heterocycle optionally containing a further nitrogen atom and optionally substituted by NR'R" as defined above or R 2 is C 1-6 alkoxy substituted by NR'R" as defined above; R 3 is hydrogen or C 1-6 alkyl; R 4 is hydrogen, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, C 3-8 cycloalkyl, aryl or aryl C 1-6 alkyl; R 5 is hydrogen, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, C 3-8 cycloalkyl, aryl, aryl C 1-6 alkyl or C 1-6 alkoxycarbonyl; or R 4 and R 5 , together with the nitrogen atom to which they are attached, form a C 3 -C 10 mono- or bicyclic saturated ring; X and Y are independently chosen from hydrogen, hydroxy, nitro, amino, cyano, CF 3 , halogen and C 1-4 alkyl; or a pharmaceutically acceptable salt thereof; as NK-2/NK-3 ligands for treating schizophrenia, COPD, asthma or irritable bowel syndrome.
摘要翻译：本发明公开了式（I）的化合物：其中：R 1是芳基或杂芳基环; R 2是羟基，C 1-6烷氧基，C 1-6烷基，氨基，NR'R“或C 1-6烷基-NR'R”，其中R'和R“独立地选自氢和C 1-4烷基，其中R'和R“与它们所连接的氮原子一起形成任选地含有另外的氮原子并且任选被如上定义的NR'R”所取代的饱和含氮3-7元杂环或R 2 >如上定义的被NR'R“取代的C 1-6烷氧基; R 3是氢或C 1-6烷基; R 4是氢，C 1-8烷基，C 2-8烯基，C 2-8炔基，C 3-8环烷基，芳基或芳基C 1-6烷基; R 5是氢，C 1-8烷基，C 2-8烯基，C 2-8炔基，C 3-8环烷基，芳基，芳基C 1-6烷基或C 1-6烷氧基羰基; 或R 4和R 5与它们所连接的氮原子一起形成C 3 -C 10单环或双环饱和环; X和Y独立地选自氢，羟基，硝基，氨基，氰基，CF 3，卤素和C 1-4烷基; 或其药学上可接受的盐; 作为用于治疗精神分裂症，COPD，哮喘或肠易激综合征的NK-2 / NK-3配体。

6. 发明申请

WO2002076983A1 IMIDAZO-PYRIMIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
标题翻译：作为GABA受体配体的咪唑并吡啶衍生物
公开(公告)号：WO2002076983A1
公开(公告)日：2002-10-03
申请号：PCT/GB2002/001354
申请日：2002-03-19
申请人： MERCK SHARP & DOHME LIMITED , BLACKABY, Wesley, Peter , CASTRO PINEIRO, Jose, Luis , CHAMBERS, Mark, Stuart , GOODACRE, Simon, Charles , HALLETT, David, James , JONES, Philip , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , MAXEY, Robert, James , MOORE, Kevin, William , STREET, Leslie, Joseph
发明人： BLACKABY, Wesley, Peter , CASTRO PINEIRO, Jose, Luis , CHAMBERS, Mark, Stuart , GOODACRE, Simon, Charles , HALLETT, David, James , JONES, Philip , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , MAXEY, Robert, James , MOORE, Kevin, William , STREET, Leslie, Joseph
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/519
摘要： A class of imidazo[1,2-α]pyrimidine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, are selective ligands for GABA A receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类通过任选取代的五元或六元杂芳环在3-位上被取代的咪唑并[1,2-a]嘧啶衍生物，是GABA A受体的选择性配体，特别是对α2具有良好的亲和力和/或α3和/或α5亚基，因此有益于治疗和/或预防中枢神经系统的不利条件，包括焦虑，抽搐和认知障碍。

7. 发明申请

WO2003093272A1 IMIDAZO-TRIAZINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
标题翻译：咪达唑啶衍生物作为GABA受体的配体
公开(公告)号：WO2003093272A1
公开(公告)日：2003-11-13
申请号：PCT/GB2003/001888
申请日：2003-05-01
申请人： MERCK SHARP & DOHME LIMITED , BETTATI, Michela , CHAMBERS, Mark, Stuart , GOODACRE, Simon, Charles , HALLETT, David, James , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph
发明人： BETTATI, Michela , CHAMBERS, Mark, Stuart , GOODACRE, Simon, Charles , HALLETT, David, James , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A class of 7-phenylimidazo[1,2- b ][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a -NH- linkage, and substituted on the phenyl ring by one or two further substituents as defined herein, being selective ligands for GABA A receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类7-苯基咪唑并[1,2-b] [1,2,4]三嗪衍生物，其在苯环的间位被任选取代的被氧原子连接或桥连的芳基或杂芳基取代或-NH-键，并且在苯环上被如本文所定义的一个或两个另外的取代基取代，是GABA A受体的选择性配体，特别是对α2和/或α3和/或其α5亚基具有良好的亲和力。因此在治疗和/或预防中枢神经系统的不利条件方面有益，包括焦虑，抽搐和认知障碍。

8. 发明申请

WO2003093273A1 IMIDAZO-TRIAZINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
标题翻译：咪达唑啶衍生物作为GABA受体的配体
公开(公告)号：WO2003093273A1
公开(公告)日：2003-11-13
申请号：PCT/GB2003/001957
申请日：2003-05-01
申请人： MERCK SHARP & DOHME LIMITED , CHAMBERS, Mark, Stuart , GOODACRE, Simon, Charles , HALLETT, David, James , MAXEY, Robert, James , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph
发明人： CHAMBERS, Mark, Stuart , GOODACRE, Simon, Charles , HALLETT, David, James , MAXEY, Robert, James , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A class of imidazo[1,2 b ][1,2,4]triazine derivatives, substituted at the 7-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABA A receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类由任选取代的五元或六元杂芳环在7-位取代的咪唑并[1,2b] [1,2,4]三嗪衍生物是GABA 受体的选择性配体，特别是对α2和/或α3和/或α5亚基具有良好亲和力，因此在治疗和/或预防中枢神经系统的不良状况（包括焦虑，惊厥和认知障碍）方面是有益的。

9. 发明申请

WO2006097766A1 ARYLSULFONYL BENZYL ETHERS AS 5-HT2A ANTAGONISTS 审中-公开
公开(公告)号：WO2006097766A1
公开(公告)日：2006-09-21
申请号：PCT/GB2006/050048
申请日：2006-03-08
申请人： MERCK SHARP & DOHME LIMITED , CHAMBERS, Mark, Stuart , GILLIGAN, Myra , HUMPHRIES, Alexander, Charles , MERCHANT, Kevin, John
发明人： CHAMBERS, Mark, Stuart , GILLIGAN, Myra , HUMPHRIES, Alexander, Charles , MERCHANT, Kevin, John
IPC分类号： A61K31/10 , A61K31/44 , C07C317/14 , C07D213/71 , A61P25/00 , A61K31/166 , A61K31/18 , A61K31/277 , A61K31/415 , A61K31/4164 , A61K31/4184 , A61K31/4196 , A61K31/426 , C07D213/80 , C07D213/82
CPC分类号： C07D213/80 , A61K31/10 , A61K31/166 , A61K31/18 , A61K31/277 , A61K31/415 , A61K31/4164 , A61K31/4184 , A61K31/4196 , A61K31/426 , A61K31/44 , C07C317/22 , C07C317/44 , C07D213/71 , C07D213/82 , C07D231/12 , C07D233/64 , C07D235/06 , C07D249/08 , C07D277/26 , C07D401/04
摘要： Compounds of formula (I) are potent and selective antagonists of the 5-HT 2A receptor, and hence are useful in treatment of various CNS disorders.
摘要翻译：式（I）化合物是5-HT 2A 2A受体的有效和选择性拮抗剂，因此可用于治疗各种CNS疾病。

10. 发明申请

WO2002074773A1 IMIDAZO-PYRIMIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
标题翻译：作为GABA受体配体的咪唑并吡啶衍生物
公开(公告)号：WO2002074773A1
公开(公告)日：2002-09-26
申请号：PCT/GB2002/001352
申请日：2002-03-19
申请人： MERCK SHARP & DOHME LIMITED
发明人： CHAMBERS, Mark, Stuart , GOODACRE, Simon, Charles , HALLETT, David, James , JENNINGS, Andrew , JONES, Philip , LEWIS, Richard, Thomas , MOORE, Kevin, William , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph , SZEKERES, Helen, Jane
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A class of 3-phenylimidazo[1,2-a]pyrimidine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a -NH- linkage, and further substituted on the phenyl ring by alkyl, trifluoromethyl, alkoxy or one or two halogen atoms, especially fluoro, are selective ligands for GABAA receptors, in particular having good affinity for the a2 and/or a3 and/or a5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类3-苯基咪唑并[1,2-a]嘧啶衍生物，其在苯环的间位被被氧原子或-NH-键直接连接或桥连的任意取代的芳基或杂芳基取代，并且在苯环上被烷基，三氟甲基，烷氧基或一个或两个卤素原子，特别是氟取代，是GABA A受体的选择性配体，特别是对其a2和/或a3和/或a5亚基具有良好的亲和力，因此在治疗和/或预防中枢神经系统的不良状况（包括焦虑，抽搐和认知障碍）方面是有益的。

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