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公开(公告)号：UY24865A1
公开(公告)日：2000-12-29
申请号：UY24865
申请日：1998-01-29
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: Compuestos de fórmula general (I), representada en la figura 1, y sales de adición de los mismos, en particular derivados de la 8-sustituida-1,3,8-triazospiro[4.5]-4-ona,donde: R1 y R2 son independientemente el uno del otro, hidrógeno, alquilo, alcoxi o halógeno; R3 es fenilo, alquilo opcionalmente sustituido, CF3, alcoxi o halógeno; A es un anillo saturado de 4 a 7 miembros; R5 y R6 son independientemente el uno del otro, hidrógeno, fenilo, alquilo o di-alquilo o juntos pueden formar un anillo fenilo, y R5 y uno de R1 y R2 pueden formar juntos un anillo saturado o no saturado de 6 miembros; cn la condición que dicho compuesto de fórmula general (I) no sea 8-(8-metoxi-1,2,3,4-tetrahidro-2-naftalenil)-1-fenil-1,3,8-triaza-spiro[4,5]decan-4-ona. Ejemplos no limitantes de compuestos de fórmula general (I): 8-(5,8-dicloro-1,2,3,4-tetrahidro-naftil-2)-3-metil-1-fenil-1,3,8-triaza-spiro[4,5]decan-4-ona; éster metílico de ácido [8-(5,8-dicloro-1,2,3,4-tetrahidro-naftil-2)-4-oxo-1-fenil-1,3,8-triaza-spiro[4,5]dec-3-il] acético. Se incluyen medicamentos que los contienen para el tratamiento de enfermedades relacionadas con el receptor de orfaniana FQ(OFQ), que incluye trastornos siquiátricos, neurológicos y fisiológicos; como por ejemplo trastornos de ansiedad y Alzheimer.
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公开(公告)号：AU719519B2
公开(公告)日：2000-05-11
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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13.发明专利
公开(公告)号：NZ328033A
公开(公告)日：1998-11-25
申请号：NZ32803397
申请日：1997-06-06
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 , C07K14/435
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：TR199800085A2
公开(公告)日：1998-08-21
申请号：TR9800085
申请日：1998-01-20
Applicant: HOFFMANN LA ROCHE
Inventor： ADAM GEO , CESURA ANDREA , GALLEY GUIDO , JENCK FRANCOIS , MONSMA FREDERICK , ROEVER 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 , C07D , A61K
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：CZ27398A3
公开(公告)日：1998-08-12
申请号：CZ27398
申请日：1998-01-29
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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Patent Agency Ranking
公开(公告)号：CA2226058A1
公开(公告)日：1998-07-30
申请号：CA2226058
申请日：1997-12-31
Applicant: HOFFMANN LA ROCHE
Inventor： JENCK FRANCOIS , MONSMA FREDERICK , GALLEY GUIDO , ADAM GEO , CESURA ANDREA , R VER 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 (see fig. I) wherein R1 and R2 are, independently from each other, hydrogen, lower alkyl, lower alkoxy or halogen; R3 is phenyl, optionally substituted by lower alkyl, CF3, lower alkoxy or halogen; and R4 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, R5 and R6 are, independently from each other, hydrogen, phenyl, lower alkyl or di-lower alkyl or may form together a phenyl ring, and R5 and one of R1 or R2 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：CZ179597A3
公开(公告)日：1998-03-18
申请号：CZ179597
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：HU9701032D0
公开(公告)日：1997-07-28
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：AU730147B2
公开(公告)日：2001-03-01
申请号：AU5280998
申请日：1998-01-29
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 , A61K31/395
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：SG71077A1
公开(公告)日：2000-03-21
申请号：SG1998000062
申请日：1998-01-07
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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