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公开(公告)号:BRPI0921348A2
公开(公告)日:2019-09-24
申请号:BRPI0921348
申请日:2009-11-03
Applicant: HOFFMANN LA ROCHE
Inventor: ANJA LIMBERG , ERWIN GOETSCHI , KARLHEINZ BAUMANN , SYNESE JOLIDON , THOMAS LUEBBERS
IPC: C07D401/12 , A61K31/4178 , C07D413/12 , C07D417/12
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公开(公告)号:BRPI0413497B1
公开(公告)日:2017-12-19
申请号:BRPI0413497
申请日:2004-08-02
Applicant: HOFFMANN LA ROCHE
Inventor: EMMANUEL PINARD , HENRI STALDER , MATTHIAS HEINRICH NETTEKOVEN , ROBERT NARQUIZIAN , ROGER DAVID NORCROSS , SYNESE JOLIDON
IPC: A61K31/495 , A61K31/497 , A61P25/28 , C07D213/74 , C07D213/85 , C07D239/42 , C07D241/20 , C07D251/42 , C07D257/04 , C07D263/32 , C07D271/06 , C07D295/192 , C07D309/12
Abstract: "piperazina com ou que substitui grupo de fenila e seu uso como inibidores de glyt1". a presente invenção refere-se a compostos de fórmula (i) em que os substituintes são descritos nas reivindicação 1. os compostos podem ser empregados no tratamento de doenças com base no inibidor de captação de glicina, tais como psicoses, dor, disfunção neurodegenerativa em memória e aprendizado, esquizofrenia, demência e outras doenças nas quais os processos cognitivos são prejudicados, tais como distúrbios do déficit de atenção ou doença de alzheimer.
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公开(公告)号:CL2009000023A1
公开(公告)日:2010-05-07
申请号:CL2009000023
申请日:2009-01-08
Applicant: HOFFMANN LA ROCHE
Inventor: ERWIN GOETSCHI , SYNESE JOLIDON , HELMUT JACOBSEN , ALEXANDER FLOHR , KARLHEINZ BAUMANN , THOMAS LUEBBERS
IPC: A61K31/428 , A61P9/00 , A61P25/00 , A61P25/28 , C07D233/60 , C07D249/08 , C07D263/32 , C07D277/60 , C07D401/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/052
Abstract: Compuestos derivados de heterociclos de nitrógeno y azufre, moduladores de beta-amiloide; procedimiento de preparación; composición farmacéutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de Alzheimer, angiopatía amiloide cerebral, hemorragia cerebral, demencia multiinfarto, demencia pugilística o Síndrome de Down.
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公开(公告)号:ZA905740B
公开(公告)日:1991-04-24
申请号:ZA905740
申请日:1990-07-20
Applicant: HOFFMANN LA ROCHE
Inventor: GUERRY PHILIPPE , PHILIPPE GUERRY , JOLIDON SYNESE , SYNESE JOLIDON , ZURFLUEH RENE , RENE ZURFLUEH
IPC: C07C225/16 , A61K20060101 , A61K31/13 , A61K31/135 , A61K31/138 , A61K31/395 , A61P31/10 , C07C20060101 , C07C49/84 , C07C213/02 , C07C213/08 , C07C217/18 , C07C217/20 , C07C217/22 , C07C217/46 , C07D20060101 , C07D205/04 , C07D295/088 , A61K , C07C , C07D
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公开(公告)号:JO2605B1
公开(公告)日:2011-11-01
申请号:JOP20030116
申请日:2003-09-18
Applicant: HOFFMANN LA ROCHE
Inventor: HANS IDING , SYNESE JOLIDON , DANIELA KRUMMENACHER , ROSA MARIA RODRIGUEZ SARMIENTO , ANDREW WILLIAM THOMAS , BEAT WIRZ , WOLFGANG WOSTL , RENE WYLER
IPC: A61K31/4015 , A61P25/16 , A61P25/28 , C07D207/26 , C07D207/273 , C07D207/277 , C07D401/04
Abstract: Racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of a disease which is mediated by a monoamine oxidase B inhibitor, in particular Alzheimer’s diseases and senile dementia
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公开(公告)号:JO2604B1
公开(公告)日:2011-11-01
申请号:JOP20030115
申请日:2003-09-18
Applicant: HOFFMANN LA ROCHE
Inventor: HANS IDING , SYNESE JOLIDON , DANIELA KRUMMENACHER , ROSA MARIA RODRIGUEZ SARMIENTO , ANDREW WILLIAM THOMAS , BEAT WIRZ , WOLFGANG WOSTL , RENE WYLER
IPC: A61K31/4015 , A61P25/16 , A61P25/28 , C07D207/26 , C07D207/273 , C07D207/277 , C07D401/04
Abstract: Racemic or enantiomerically pure 4- pyrrolidino derivatives, processes for their preparation , pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, in particular which is mediated by monoamine oxidase B inhibitors, in particular Alzheimer’s diseases or senile dementia.
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公开(公告)号:CL2009000380A1
公开(公告)日:2010-09-21
申请号:CL2009000380
申请日:2009-02-19
Applicant: HOFFMANN LA ROCHE
Inventor: ERWIN GOETSCHI , SYNESE JOLIDON , HELMUT JACOBSEN , ALEXANDER FLOHR , KARLHEINZ BAUMANN , THOMAS LUEBBERS
IPC: A61K31/506 , A61P25/00 , A61P25/28 , C07D207/04 , C07D233/64 , C07D239/42 , C07D403/14 , C07D413/14
Abstract: Compuestos derivados de heterociclos, moduladores de beta-amiloide; proceso de preparación; composición farmacéutica; y uso en el tratamiento de la Enfermedad de Alzheimer, angioplastia cerebral amiloide, demencia multiinfarto, Síndrome de Down, entre otras.
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公开(公告)号:JO2541B
公开(公告)日:2010-09-05
申请号:JO200358
申请日:2003-05-28
Applicant: HOFFMANN LA ROCHE
Inventor: SYNESE JOLIDON , ROSA MARIA RODRIGUEZ SARMIENTO , ANDREW WILLIAM THOMAS , & X C;RENE WYLER
Abstract: This invention relates to N-acylamino aryl derivatives of the general formula (I), wherein R is halogen, halogen-(C1-C6)-alkyl, cyano, C1-C6-alkoxy or halogen-(C1-C6)-alkoxy; R , R , R and R independently from each other are selected from the group consisting of hydrogen, (C1-C6)-alkyl, halogen, halogen-(C1-C6)-alkyl, hydroxy, C1-C6-alkoxy or -CHO; R is hydrogen or C1-C3-alkyl; R , R independently from each other are selected from the group consisting of hydrogen, C1-C6-alkyl, C1-C6-alkoxy or -COO(C1-C6)alkyl; or R and R form together with the C-atom to which they are attach a C3-C7-cycloalkyl ring; R is -CO-NR R ; -COO(C1-C6)-alkyl, -CN, -NR2 or -NHC(O)R; R and R independently from each other are selected from the group consisting of hydrogen, C1-C6-alkyl, NH2 or hydroxy; R is hydrogen or C1-C6-alkyl; n is 0, 1, 2 or 3. X is -CHRO, -OCHR, -CH2S-, -SCH2-, -CH2CH2-, -CH=CH- or -C=C-; and to pharmaceutically active acid addition salts thereof. It has been found that the compounds of general formula (I) are selective monoamine oxidase B inhibitors and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B inhibitors, for example for the treatment of Alzheimer's disease or senile dementia.
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公开(公告)号:ZA200705469B
公开(公告)日:2008-11-26
申请号:ZA200705469
申请日:2007-07-04
Applicant: HOFFMANN LA ROCHE
Inventor: SYNESE JOLIDON , DAVID NORCROSS ROGER , ROBERT NARQUIZIAN , EMMANUEL PINARD
IPC: A61K20090101 , A61P20090101 , C07D20090101
Abstract: The present invention relates to compounds of formula I wherein R 1 , R 2 , R 3 , X, X 1 , and n are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. These compounds are good inhibitors of the glycine transporter 1 (GlyT-1) for the treatment CNS disorders, such as schizophrenia, cognitive impairment, and Alzheimer's disease.
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公开(公告)号:ZA200705472B
公开(公告)日:2008-09-25
申请号:ZA200705472
申请日:2007-07-04
Applicant: HOFFMANN LA ROCHE
Inventor: SYNESE JOLIDON , DAVID NORCROSS ROGER , ROBERT NARQUIZIAN , EMMANUEL PINARD
IPC: A61K20090101 , A61P20090101 , C07D20090101
Abstract: The present invention relates to compounds of formula I wherein R 1 , R 2 , X 1 , and X 2 are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. Such compounds are inhibitors of the glycine transporter 1 (GlyT-1) and can be used in the treatment of schizophrenia, cognitive impairment, and Alzheimer's disease.
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