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1. 发明申请

WO0012505A3 TRIAZOLOPYRIDAZINE DERIVATIVES FOR TREATING ANXIETY AND ENHANCING COGNITION 审中-公开
标题翻译：用于治疗厌食症和增强感觉的三唑吡啶衍生物
公开(公告)号：WO0012505A3
公开(公告)日：2000-06-08
申请号：PCT/GB9902737
申请日：1999-08-20
申请人： MERCK SHARP & DOHME , LADDUWAHETTY TAMARA , MERCHANT KEVIN JOHN , STERNFELD FRANCINE , STREET LESLIE JOSEPH
发明人： MERCHANT KEVIN JOHN , STERNFELD FRANCINE , STREET LESLIE JOSEPH
IPC分类号： A61K31/5025 , A61P25/22 , A61P25/28 , C07D487/04 , A61K31/4985
CPC分类号： C07D487/04
摘要： A compound of formula (I), or a salt or prodrug thereof wherein: Z represents C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, aryl, C3-7 heterocycloalkyl, heteroaryl, di(C1-6)alkylamino or C6-12 bicycloalkyl, any of which groups may be optionally substituted; R represents an optionally substituted five-membered heteroaromatic ring selected from pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or R represents an optionally substituted six-membered heteroaromatic ring selected from pyridine, pyrazine, pyrimidine and pyridazine; and R represents cyano(C1-6)alkyl, hydroxy(C1-6)alkyl, C3-7 cycloalkyl(C1-6)alkyl, propargyl, C3-7 heterocycloalkylcarbonyl(C1-6)alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; its use in treating anxiety and pharmaceutical compositions comprising it; a subclass of compounds which are useful in enhancing cognition, such as Alzheimer's Disease, is also disclosed.
摘要翻译：式（I）化合物或其盐或前药，其中：Z表示C 1-6烷基，C 3-7环烷基，C 4-7环烯基，芳基，C 3-7杂环烷基，杂芳基，二（C 1-6）烷基氨基或 C 6-12双环烷基，其任何基团可以任选被取代; R 1表示选自吡咯，恶唑，噻唑，异恶唑，异噻唑，咪唑，吡唑，恶二唑，噻二唑，三唑和四唑的任选取代的五元杂芳环; 或R 1表示任选取代的六元杂芳环，其选自吡啶，吡嗪，嘧啶和哒嗪; 并且R 2表示氰基（C 1-6）烷基，羟基（C 1-6）烷基，C 3-7环烷基（C 1-6）烷基，炔丙基，C 3-7杂环烷基羰基（C 1-6）烷基， 6）烷基或杂芳基（C 1-6）烷基，其中任何基团可任选被取代; 其用于治疗焦虑症和包含它的药物组合物; 还公开了可用于增强认知的化合物的亚类，例如阿尔茨海默氏病。

2. 发明申请

WO03018546A3 TRICYCLIC PYRIDIN-2-ONE ANALOGUES AS LIGANDS FOR GABA-A RECEPTORS 审中-公开
标题翻译：三环吡啶-2-酮类似物作为GABA-A受体的配体
公开(公告)号：WO03018546A3
公开(公告)日：2003-07-17
申请号：PCT/GB0203703
申请日：2002-08-12
申请人： MERCK SHARP & DOHME , BOURRAIN SYLVIE , GOODACRE SIMON CHARLES , HALLETT DAVID JAMES , LEWIS RICHARD THOMAS , ROWLEY MICHAEL , STERNFELD FRANCINE , STREET LESLIE JOSEPH
发明人： BOURRAIN SYLVIE , GOODACRE SIMON CHARLES , HALLETT DAVID JAMES , LEWIS RICHARD THOMAS , ROWLEY MICHAEL , STERNFELD FRANCINE , STREET LESLIE JOSEPH
IPC分类号： A61P25/22 , C07D471/14 , C07D471/16
CPC分类号： C07D471/14
摘要： A class of selectively substituted fused tricyclic compounds based on a substituted pyridinone moiety are potent and functionally selective ligands for the alpha 2/ alpha 3 subunit of the human GABA-A receptor and are thereby effective in the treatment of anxiety.
摘要翻译：基于取代的吡啶酮部分的一类选择性取代的稠合三环化合物是人类GABA-A受体的α2/α3亚基的有效和功能选择性配体，并因此有效治疗焦虑症。

3. 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。

4. 发明专利

ES2198146T3 未知
公开(公告)号：ES2198146T3
公开(公告)日：2004-01-16
申请号：ES99940362
申请日：1999-08-20
申请人： MERCK SHARP & DOHME , LADDUWAHETTY TAMARA
发明人： MERCHANT KEVIN JOHN , STERNFELD FRANCINE , STREET LESLIE JOSEPH , LADDUWAHETTY TAMARA
IPC分类号： A61K31/5025 , A61P25/22 , A61P25/28 , C07D487/04 , A61K31/4985

5. 发明专利

DE69907923T2 未知
公开(公告)号：DE69907923T2
公开(公告)日：2004-02-12
申请号：DE69907923
申请日：1999-08-20
申请人： MERCK SHARP & DOHME , LADDUWAHETTY TAMARA
发明人： MERCHANT KEVIN JOHN , STERNFELD FRANCINE , STREET LESLIE JOSEPH , LADDUWAHETTY TAMARA
IPC分类号： A61K31/5025 , A61P25/22 , A61P25/28 , C07D487/04 , A61K31/4985

6. 发明专利

AT240333T 未知
公开(公告)号：AT240333T
公开(公告)日：2003-05-15
申请号：AT99940362
申请日：1999-08-20
申请人： MERCK SHARP & DOHME , LADDUWAHETTY TAMARA
发明人： MERCHANT KEVIN JOHN , STERNFELD FRANCINE , STREET LESLIE JOSEPH , LADDUWAHETTY TAMARA
IPC分类号： A61K31/5025 , A61P25/22 , A61P25/28 , C07D487/04 , A61K31/4985

7. 发明专利

DE69907923D1 未知
公开(公告)号：DE69907923D1
公开(公告)日：2003-06-18
申请号：DE69907923
申请日：1999-08-20
申请人： MERCK SHARP & DOHME , LADDUWAHETTY TAMARA
发明人： MERCHANT KEVIN JOHN , STERNFELD FRANCINE , STREET LESLIE JOSEPH , LADDUWAHETTY TAMARA
IPC分类号： A61K31/5025 , A61P25/22 , A61P25/28 , C07D487/04 , A61K31/4985

8. 发明专利

CA2288789C SUBSTITUTED 1,2,4-TRIAZOLO[3,4-A]PHTHALAZINE DERIVATIVES AS GABA ALPHA 5 LIGANDS 未知
公开(公告)号：CA2288789C
公开(公告)日：2009-07-21
申请号：CA2288789
申请日：1998-05-06
申请人： MERCK SHARP & DOHME
发明人： STERNFELD FRANCINE , MACLEOD ANGUS MURRAY , LADDUWAHETTY TAMARA , MERCHANT KEVIN JOHN , MOORE KEVIN WILLIAM , CARLING WILLIAM ROBERT , STREET LESLIE JOSEPH
IPC分类号： C07D487/04 , A61K31/5025 , A61P25/28 , A61P43/00
摘要： A compound of formula (I) wherein R1 is hydrogen, halogen or CN or a group CF3, OCF3, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy, each of which groups is unsubstituted or substituted with one or two halogen atoms or with a pyridyl or phenyl ring each of which rings may be unsubstituted or independently substituted by one or two halo-gen atoms or nitro, cyano, amino, methyl or CF3 groups; R2 is hydrogen, halogen or CN or a group CF3, OCF3, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy each of which groups is unsubstituted or substituted with one or two halogen atoms; L is O, S, or NR n where R n is H, C1-6alkyl or C3-6cycloalkyl; X is a five or six-membered optionally substituted heterocycle; Y is optionally branched C1-4alkylidene optionally substituted by an oxo group or Y is a gro up (CH2)j O wherein the oxygen atom is nearest the group X and j is 2, 3 or 4; Z is a five or six-membered optionally substituted heterocycle; or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising it, its use in medical treatment, processes for producing it and intermediates used in those processes are disclosed.

9. 发明专利

RS49746B SUPSTITUISANI DERIVAT TRIAZOLO- PIRADIZINA, FARMACEUTSKE SMEŠE KOJE SE SA NJIM PROIZVODE 未知
公开(公告)号：RS49746B
公开(公告)日：2008-04-04
申请号：YU77800
申请日：1999-06-15
申请人： MERCK SHARP & DOHME
发明人： CARLING WILLIAM ROBERT , DAVIES ANTONY JOHN MSD , PEARCE GARETH EDWARD STEPHEN , CASTRO PINEIRO JOSE LUIS , MADIN ANDREW , STREET LESLIE JOSEPH , COWDEN CAMERON JOHN MSD , MCCABE JAMES FRANCIS MSD
IPC分类号： C07D487/04 , A61K31/50 , A61K31/5025 , A61P25/00 , A61P25/22
摘要： 7-(1,1-Dimetiletil)-6-(2-etil-2H-1,2,4-triazol-3-ilmetoksi)-3-(2-fluorofenil)-1,2,4-triazolo[4,3-b]piridazin.Prijava sadrži još 5 zahteva.

10. 发明专利

DE69936998D1 未知
公开(公告)号：DE69936998D1
公开(公告)日：2007-10-11
申请号：DE69936998
申请日：1999-10-13
申请人： MERCK SHARP & DOHME
发明人： CARLING WILLIAM ROBERT , MITCHINSON ANDREW , MOORE KEVIN WILLIAM , RUSSELL MICHAEL GEOFFREY NEIL , SCOTT GAYLE , STREET LESLIE JOSEPH
IPC分类号： C07D487/04 , A61K31/53

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