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公开(公告)号:MX9704352A
公开(公告)日:1997-12-31
申请号:MX9704352
申请日:1997-06-12
Applicant: HOFFMANN LA ROCHE
Inventor: CIVELLI OLIVIER , MARTIN JAMES RICHARD , MONSMA FREDERICK , MOREAU JEAN-LUC , NOTHACKER HANS-PETER , REINSCHEID RAINER
IPC: G01N33/53 , A61K38/00 , A61K38/10 , A61P25/08 , A61P25/20 , A61P25/26 , G01N33/15 , G01N33/566 , G01N33/94 , A61B05/00
Abstract: La presente invencion se refiere a un método de escrutinio de un compuesto terapéuticamente util basado en el ensayo de agonista del receptor LC132 en un ensayo de escrutinio para transtornos neurologicos y/o psiquiátricos. Más específicamente, el método de escrutinio se basa en poner en contacto un receptor LC132 con un agente que se sospecha que es un agonista de la funcion del receptor LC132, seguido de la deteccion de la union y/o de la actividad agonista del compuesto, y seguido del ensayo de un agente con actividad agonista LC132 en un ensayo de escrutinio de actividad antiepiléptica, anticonvulsionante y/o ansiolítica.
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公开(公告)号:AU2485397A
公开(公告)日:1997-12-18
申请号:AU2485397
申请日:1997-06-12
Applicant: HOFFMANN LA ROCHE
Inventor: CIVELLI OLIVIER , MARTIN JAMES RICHARD , MONSMA FREDERICK , MOREAU JEAN-LUC , NOTHACKER HANS-PETER , REINSCHEID RAINER
IPC: G01N33/53 , A61K38/00 , A61K38/10 , A61P25/08 , A61P25/20 , A61P25/26 , G01N33/15 , G01N33/566 , G01N33/94 , G01N33/68
Abstract: The present invention relates to a method of screening for a therapeutically useful compound which comprises testing an LC132 receptor agonist in a screening assay for psychiatric and/or neurological disorders. More particularly, the screening method is based on contacting an LC132 receptor with an agent suspected of being an agonist of the LC132 receptor function, followed by the detection of the binding and/or the agonist activity of the compound and then testing of an agent with LC132 agonist activity in an antiepileptic, anticonvulsant or anxiolytic screening assay.
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公开(公告)号:MA26470A1
公开(公告)日:2004-12-20
申请号:MA24950
申请日:1998-01-28
Applicant: HOFFMANN LA ROCHE
Inventor: ADAM GEO , CESURA ANDREA , GALLEY GUIDO , JENCK FRANCOIS , MONSMA FREDERICK , ROEVER STEPHAN , WICHMANN JUERGEN
IPC: C07D233/04 , A61K31/00 , A61K31/41 , A61K31/435 , A61K31/438 , A61K31/445 , A61K31/55 , A61K51/02 , A61P3/04 , A61P3/12 , A61P9/00 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D215/58 , C07D305/14 , C07D471/00 , C07D471/10 , C07D498/00 , C07D233/00 , A61K31/40 , A61K31/415
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公开(公告)号:PT856514E
公开(公告)日:2001-10-31
申请号:PT98100970
申请日:1998-01-21
Applicant: HOFFMANN LA ROCHE
Inventor: ROVER STEPHAN , WICHMANN JURGEN , ADAM GEO , CESURA ANDREA , GALLEY GUIDO , JENCK FRANCOIS , MONSMA FREDERICK
IPC: C07D233/04 , A61K31/00 , A61K31/41 , A61K31/435 , A61K31/438 , A61K31/445 , A61K31/55 , A61K51/02 , A61P3/04 , A61P3/12 , A61P9/00 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D215/58 , C07D305/14 , C07D471/00 , C07D471/10 , C07D498/00 , A61K31/44
Abstract: The present invention relates to compounds of the formula wherein R and R are, independently from each other, hydrogen, lower alkyl, lower alkoxy or halogen; R is phenyl, optionally substituted by lower alkyl,CF3, lower alkoxy or halogen; and R is hydrogen, lower alkyl, lower alkenyl, -C(O)-lower alkyl, -C(O)-phenyl, lower alkyl-C(O)-phenyl, lower alkylen-C(O)O-lower alkyl, lower alkantriyl-di-C(O)O-lower alkyl, hydroxy-lower alkyl, lower alkyl-O-lower alkyl, lower alkyl-CH(OH)CF3, phenyl or benzyl, R and R are, independently from each other, hydrogen, phenyl, lower alkyl or di-lower alkyl or may form together a phenyl ring, and R and one of R or R may form together a saturated or unsaturated 6 membered ring, A is a 4 - 7 membered saturated ring which may contain a heteroatom such as O or S, and to pharmaceutically acceptable acid addition salts thereof which are agonists and/or antagonists of the OFQ receptor.
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公开(公告)号:DK0856514T3
公开(公告)日:2001-09-17
申请号:DK98100970
申请日:1998-01-21
Applicant: HOFFMANN LA ROCHE
Inventor: ADAM GEO , CESURA ANDREA , GALLEY GUIDO , JENCK FRANCOIS , MONSMA FREDERICK , ROEVER STEPHAN , WICHMANN JUERGEN
IPC: C07D233/04 , A61K31/00 , A61K31/41 , A61K31/435 , A61K31/438 , A61K31/445 , A61K31/55 , A61K51/02 , A61P3/04 , A61P3/12 , A61P9/00 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D215/58 , C07D305/14 , C07D471/00 , C07D471/10 , C07D498/00 , A61K31/44
Abstract: The present invention relates to compounds of the formula wherein R and R are, independently from each other, hydrogen, lower alkyl, lower alkoxy or halogen; R is phenyl, optionally substituted by lower alkyl,CF3, lower alkoxy or halogen; and R is hydrogen, lower alkyl, lower alkenyl, -C(O)-lower alkyl, -C(O)-phenyl, lower alkyl-C(O)-phenyl, lower alkylen-C(O)O-lower alkyl, lower alkantriyl-di-C(O)O-lower alkyl, hydroxy-lower alkyl, lower alkyl-O-lower alkyl, lower alkyl-CH(OH)CF3, phenyl or benzyl, R and R are, independently from each other, hydrogen, phenyl, lower alkyl or di-lower alkyl or may form together a phenyl ring, and R and one of R or R may form together a saturated or unsaturated 6 membered ring, A is a 4 - 7 membered saturated ring which may contain a heteroatom such as O or S, and to pharmaceutically acceptable acid addition salts thereof which are agonists and/or antagonists of the OFQ receptor.
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公开(公告)号:SI0856514T1
公开(公告)日:2001-08-31
申请号:SI9830035
申请日:1998-01-21
Applicant: HOFFMANN LA ROCHE
Inventor: ADAM GEO , CESURA ANDREA , GALLEY GUIDO , JENCK FRANCOIS , MONSMA FREDERICK , ROEVER STEPHAN , WICHMANN JUERGEN
IPC: C07D233/04 , A61K31/00 , A61K31/41 , A61K31/435 , A61K31/438 , A61K31/445 , A61K31/55 , A61K51/02 , A61P3/04 , A61P3/12 , A61P9/00 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D215/58 , C07D305/14 , C07D471/00 , C07D471/10 , C07D498/00 , A61K31/44
Abstract: The present invention relates to compounds of the formula wherein R and R are, independently from each other, hydrogen, lower alkyl, lower alkoxy or halogen; R is phenyl, optionally substituted by lower alkyl,CF3, lower alkoxy or halogen; and R is hydrogen, lower alkyl, lower alkenyl, -C(O)-lower alkyl, -C(O)-phenyl, lower alkyl-C(O)-phenyl, lower alkylen-C(O)O-lower alkyl, lower alkantriyl-di-C(O)O-lower alkyl, hydroxy-lower alkyl, lower alkyl-O-lower alkyl, lower alkyl-CH(OH)CF3, phenyl or benzyl, R and R are, independently from each other, hydrogen, phenyl, lower alkyl or di-lower alkyl or may form together a phenyl ring, and R and one of R or R may form together a saturated or unsaturated 6 membered ring, A is a 4 - 7 membered saturated ring which may contain a heteroatom such as O or S, and to pharmaceutically acceptable acid addition salts thereof which are agonists and/or antagonists of the OFQ receptor.
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公开(公告)号:EA001357B1
公开(公告)日:2001-02-26
申请号:EA199800108
申请日:1998-01-30
Applicant: HOFFMANN LA ROCHE
Inventor: ADAM GEO , CECURA ANDREA , GALLEY GUIDO , JENCK FRANCOIS , MONSMA FREDERICK , ROEVER STEPHAN , WICHMANN JUERGEN
IPC: C07D233/04 , A61K31/00 , A61K31/41 , A61K31/435 , A61K31/438 , A61K31/445 , A61K31/55 , A61K51/02 , A61P3/04 , A61P3/12 , A61P9/00 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D215/58 , C07D305/14 , C07D471/00 , C07D471/10 , C07D498/00
Abstract: ВзаявкеописанысоединенияформулыгдеRи Rкаждыйнезависимодруготдругаобозначаетводород, C-Cалкил, C-Cалкоксиилигалоген;Rобозначаетфенил, необязательнозамещенный C-Cалкилом, CF, C-Cалкоксигруппойилигалогеном; иRобозначаетводород, C-Cалкил, C-Cалкенил, -С(O)-C-Cалкил, -С(O)-фенил, C-Cалкил-С(O)-фенил, C-Cалкилен-C(O)O-C-Caлкил, C-Cалкантриил-ди-С(O)O-(C-C)алкил, гидрокси-C-Cалкил, C-Cалкил-О-C-Cалкил, C-Cалкил-СН(ОН)CF, фенилилибензил;Rи Rкаждыйнезависимодруготдругаобозначаетводород, фенил, C-Cалкилилиди-C-CалкилилимогутвместеобразовыватьфенильноекольцоиRиодиниз Rили Rмогутвместеобразовыватьнасыщенноеилиненасыщенное 6-членноекольцо;Аобозначает 4-7-членноенасыщенноекольцо, котороеможетсодержатьгетероатом, такой, какО или S;иихфармацевтическиприемлемыекислотно-аддитивныесоли, которыеявляютсяагонистамии/илиантагонистами OFQ-рецептора.
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公开(公告)号:HU9701032A2
公开(公告)日:1998-08-28
申请号:HU9701032
申请日:1997-06-11
Applicant: HOFFMANN LA ROCHE
Inventor: CIVELLI OLIVIER , MARTIN JAMES RICHARD , MONSMA FREDERICK , MOREAU JEAN-LUC , NOTHACKER HANS-PETER , REINSCHEID RAINER
IPC: G01N33/53 , A61K38/00 , A61K38/10 , A61P25/08 , A61P25/20 , A61P25/26 , G01N33/15 , G01N33/566 , G01N33/94
Abstract: The present invention relates to a method of screening for a therapeutically useful compound which comprises testing an LC132 receptor agonist in a screening assay for psychiatric and/or neurological disorders. More particularly, the screening method is based on contacting an LC132 receptor with an agent suspected of being an agonist of the LC132 receptor function, followed by the detection of the binding and/or the agonist activity of the compound and then testing of an agent with LC132 agonist activity in an antiepileptic, anticonvulsant or anxiolytic screening assay.
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公开(公告)号:ID19773A
公开(公告)日:1998-07-30
申请号:ID980073
申请日:1998-01-22
Applicant: HOFFMANN LA ROCHE
Inventor: ADAM GEO , CESURA ANDREA , GALLEY GUIDO , JENCK FRANCOIS , MONSMA FREDERICK , ROVER STEPHAN , WICHMANN JURGEN
IPC: C07D233/04 , A61K31/00 , A61K31/41 , A61K31/435 , A61K31/438 , A61K31/445 , A61K31/55 , A61K51/02 , A61P3/04 , A61P3/12 , A61P9/00 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D215/58 , C07D305/14 , C07D471/00 , C07D471/10 , C07D498/00
Abstract: The present invention relates to compounds of the formula wherein R and R are, independently from each other, hydrogen, lower alkyl, lower alkoxy or halogen; R is phenyl, optionally substituted by lower alkyl,CF3, lower alkoxy or halogen; and R is hydrogen, lower alkyl, lower alkenyl, -C(O)-lower alkyl, -C(O)-phenyl, lower alkyl-C(O)-phenyl, lower alkylen-C(O)O-lower alkyl, lower alkantriyl-di-C(O)O-lower alkyl, hydroxy-lower alkyl, lower alkyl-O-lower alkyl, lower alkyl-CH(OH)CF3, phenyl or benzyl, R and R are, independently from each other, hydrogen, phenyl, lower alkyl or di-lower alkyl or may form together a phenyl ring, and R and one of R or R may form together a saturated or unsaturated 6 membered ring, A is a 4 - 7 membered saturated ring which may contain a heteroatom such as O or S, and to pharmaceutically acceptable acid addition salts thereof which are agonists and/or antagonists of the OFQ receptor.
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公开(公告)号:HU9800138D0
公开(公告)日:1998-03-30
申请号:HU9800138
申请日:1998-01-26
Applicant: HOFFMANN LA ROCHE
Inventor: ADAM GEO , CESURA ANDREA , GALLEY GUIDO , JENCK FRANCOIS , MONSMA FREDERICK , ROEVER STEPHAN , WICHMANN JUERGEN
IPC: C07D233/04 , A61K31/00 , A61K31/41 , A61K31/435 , A61K31/438 , A61K31/445 , A61K31/55 , A61K51/02 , A61P3/04 , A61P3/12 , A61P9/00 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D215/58 , C07D305/14 , C07D471/00 , C07D471/10 , C07D498/00
Abstract: The present invention relates to compounds of the formula wherein R and R are, independently from each other, hydrogen, lower alkyl, lower alkoxy or halogen; R is phenyl, optionally substituted by lower alkyl,CF3, lower alkoxy or halogen; and R is hydrogen, lower alkyl, lower alkenyl, -C(O)-lower alkyl, -C(O)-phenyl, lower alkyl-C(O)-phenyl, lower alkylen-C(O)O-lower alkyl, lower alkantriyl-di-C(O)O-lower alkyl, hydroxy-lower alkyl, lower alkyl-O-lower alkyl, lower alkyl-CH(OH)CF3, phenyl or benzyl, R and R are, independently from each other, hydrogen, phenyl, lower alkyl or di-lower alkyl or may form together a phenyl ring, and R and one of R or R may form together a saturated or unsaturated 6 membered ring, A is a 4 - 7 membered saturated ring which may contain a heteroatom such as O or S, and to pharmaceutically acceptable acid addition salts thereof which are agonists and/or antagonists of the OFQ receptor.
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