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51. 发明专利

PL341652A1 DERIVATIVES OF TRIAZOLOPYRIDAZINE AS LIGANDS FOR GABA RECEPTORS 未知
公开(公告)号：PL341652A1
公开(公告)日：2001-04-23
申请号：PL34165299
申请日：1999-01-13
申请人： MERCK SHARP & DOHME
发明人： CARLING WILLIAM ROBERT , CASTRO PINEIRO JOSE LUIS , COLLINS IAN JAMES , GUIBLIN ALEXANDER RICHARD , HARRISON TIMOTHY , MADIN ANDREW , MOORE KEVIN WILLIAM , RUSSELL MICHAEL GEOFFREY NEIL , SCOTT GAYLE , STREET LESLIE JOSEPH
IPC分类号： A61K31/5025 , A61P25/00 , A61P25/08 , A61P25/22 , A61P43/00 , C07D487/04 , A61K31/50
摘要： A class of substituted 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a fluoro-substituted phenyl ring at the 3-position and a heteroaryl-methoxy moiety at the 6-position, are selective ligands for GABAA receptors, in particular having high affinity for the alpha2 and/or alpha3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

52. 发明专利

AU2306500A Triazolo-pyridazine derivatives as ligands for gaba receptors 未知
公开(公告)号：AU2306500A
公开(公告)日：2000-08-29
申请号：AU2306500
申请日：2000-02-02
申请人： MERCK SHARP & DOHME
发明人： CARLING WILLIAM ROBERT , MITCHINSON ANDREW , RUSSELL MICHAEL GEOFFREY NEIL , STREET LESLIE JOSEPH
IPC分类号： A61K31/5025 , A61P25/00 , A61P25/08 , A61P25/22 , C07B61/00 , C07D487/04 , C07F7/18

53. 发明专利

AU6219999A Pyrazolo-triazine derivatives as ligands for gaba receptors 未知
公开(公告)号：AU6219999A
公开(公告)日：2000-05-08
申请号：AU6219999
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： A61K31/53 , C07D487/04

54. 发明专利

AU2065799A Triazolo-pyridazine derivatives as ligands for gaba receptors 未知
公开(公告)号：AU2065799A
公开(公告)日：1999-08-09
申请号：AU2065799
申请日：1999-01-13
申请人： MERCK SHARP & DOHME
发明人： CARLING WILLIAM ROBERT , PINEIRO JOSE LUIS CASTRO , COLLINS IAN JAMES , GUIBLIN ALEXANDER RICHARD , HARRISON TIMOTHY , MADIN ANDREW , MOORE KEVIN WILLIAM , RUSSELL MICHAEL GEOFFREY NEIL , SCOTT GAYLE , STREET LESLIE JOSEPH
IPC分类号： A61K31/5025 , A61P25/00 , A61P25/08 , A61P25/22 , A61P43/00 , C07D487/04 , A61K31/50
摘要： A class of substituted 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a fluoro-substituted phenyl ring at the 3-position and a heteroaryl-methoxy moiety at the 6-position, are selective ligands for GABAA receptors, in particular having high affinity for the alpha2 and/or alpha3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

55. 发明专利

CA2315763A1 TRIAZOLO-PYRIDAZINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 未知
公开(公告)号：CA2315763A1
公开(公告)日：1999-07-29
申请号：CA2315763
申请日：1999-01-13
申请人： MERCK SHARP & DOHME
发明人： CARLING WILLIAM ROBERT , STREET LESLIE JOSEPH , HARRISON TIMOTHY , CASTRO PINEIRO JOSE LUIS , MOORE KEVIN WILLIAM , SCOTT GAYLE , COLLINS IAN JAMES , MADIN ANDREW , RUSSELL MICHAEL GEOFFREY NEIL , GUIBLIN ALEXANDER RICHARD
IPC分类号： A61K31/5025 , A61P25/00 , A61P25/08 , A61P25/22 , A61P43/00 , C07D487/04 , C07D237/00 , C07D249/00 , A61K31/50
摘要： A class of substituted 1,2,4-triazolo4,3-b!pyridazine derivatives, possessing a fluoro-substituted phenyl ring at the 3-position and a heteroaryl-methoxy moiety at the 6-position, are selective ligands for GABA A receptors, in particular having high affinity for the .alpha.2 and/or .alpha.3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

57. 发明专利

AU1449997A Diazabicyclo-octane derivatives as 5-ht receptor ligands 未知
公开(公告)号：AU1449997A
公开(公告)日：1997-08-22
申请号：AU1449997
申请日：1997-01-21
申请人： MERCK SHARP & DOHME
发明人： PINEIRO JOSE LUIS CASTRO , RUSSELL MICHAEL GEOFFREY NEIL
IPC分类号： A61P25/06 , C07D521/00 , C07D487/04 , A61K31/40
摘要： PCT No. PCT/GB97/00181 Sec. 371 Date Sep. 28, 1998 Sec. 102(e) Date Sep. 28, 1998 PCT Filed Jan. 21, 1997 PCT Pub. No. WO97/28162 PCT Pub. Date Aug. 7, 1997Compounds having formula I, or pharmaceutically acceptable salts or prodrugs thereof: are selective agonists of the 5-HT1D alpha receptor and are useful in the treatment of migraine and associated conditions.

58. 发明专利

ES2291043T3 DERIVADOS DE PIRAZOLOTRIAZINA COMO LIGANDOS PARA RECEPTORES DE GABA. 未知
公开(公告)号：ES2291043T3
公开(公告)日：2008-02-16
申请号：ES99949224
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
摘要： Un compuesto de fórmula I, o una sal del mismo en la que Z representa halógeno; o alquilo C1-6, cicloalquilo C3-7, cicloalquenilo C4-7, bicicloalquilo C6-8, arilo, heterocicloalquilo C3-7, heteroarilo o dialquil C1-6-amino, pudiendo estar opcionalmente sustituido cualquiera de dichos grupos; R1 representa cicloalquilo C3-7, fenilo, furilo, tienilo, piridinilo o pirazinilo, pudiendo estar opcionalmente sustituido cualquiera de dichos grupos; y R2 representa cicloalquil C3-7-alquilo C1-6, arilalquilo C1-6 o heteroarilalquilo C1-6, pudiendo estar opcionalmente sustituido cualquiera de dichos grupos; en los que arilo es fenilo o naftilo; heteroarilo es piridinilo, quinolinilo, isoquinolinilo, piridazinilo, pirimidinilo, pirazinilo, quinoxalinilo, furilo, benzofurilo, dibenzofurilo, tienilo, benzotienilo, pirrolilo, indolilo, pirazolilo, indazolilo, oxazolilo, isoxazolilo, tiazolilo, isotiazolilo, imidazolilo, bencimidazolilo, oxadiazolilo, tiadiazolilo, triazolilo, tetrazolilo, [1, 2, 4]triazolo[1, 5-a]piridinilo, 5, 6, 7, 8-tetrahidro[1, 2, 4]triazolo[1, 5-a]piridinilo o 5, 6, 7, 8-tetrahidro[1, 2, 4]triazolo[1, 5-a]pirazinilo; y los sustituyentes opcionales son alquilo C1-6, arilalquilo C1-6, piridilalquilo C1-6, halógeno, haloalquilo C1-6, dihaloalquilo C1-6, trifluorometilo, ciano, cianoalquilo C1-6, hidroxi, hidroximetilo, alcoxi C1-6, cicloalquil C3-7-alcoxi C1-6, cianoalcoxi C1-6, cicloalcoxi C3-7, amino, aminoalquilo C1-6, dialquil C1-6-aminoalquilo C1-6, dialquil C1-6-aminocarbonilalquilo C1-6, N-alquil C1-6-piperidinilo, pirrolidinilalquilo C1-6, piperazinilalquilo C1-6, morfolinilalquilo C1-6, dialquil C1-6-morfolinilalquilo C1-6 e imidazolilalquilo C1-6.

59. 发明专利

AU2001244398B2 Pyrazolo-triazine derivatives as ligands for gaba receptors 未知
公开(公告)号：AU2001244398B2
公开(公告)日：2005-08-25
申请号：AU2001244398
申请日：2001-04-04
申请人： MERCK SHARP & DOHME
发明人： CARLING WILLIAM ROBERT , STREET LESLIE JOSEPH , RUSSELL MICHAEL GEOFFREY NEIL , MITCHINSON ANDREW
IPC分类号： A61K31/53 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07B61/00 , C07D487/04 , C07D253/00 , C07D231/00 , A61K031/53
摘要： A class of substituted pyrazolo[1,5-d][1,2,4]triazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 7-position, an alkyl group at the 4-position, and a substituted alkoxy moiety at the 2-position, are selective ligands for GABAA receptors, in particular having high affinity for the alpha2 and/or alpha3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

60. 发明专利

CA2484162A1 IMIDAZO-TRIAZINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 未知
公开(公告)号：CA2484162A1
公开(公告)日：2003-11-13
申请号：CA2484162
申请日：2003-05-01
申请人： MERCK SHARP & DOHME
发明人： STREET LESLIE JOSEPH , RUSSELL MICHAEL GEOFFREY NEIL , GOODACRE SIMON CHARLES , HALLETT DAVID JAMES , BETTATI MICHELA , CHAMBERS MARK STUART
IPC分类号： A61K31/53 , A61P1/08 , A61P1/14 , A61P13/10 , A61P15/00 , A61P21/02 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/16 , C07D487/04 , A61K31/4188
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 GABAA receptors, in particular having good affinity for the .alpha.2 and/or .alpha.3 and/or .alpha.5 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.

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