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公开(公告)号:JO2495B1
公开(公告)日:2009-10-05
申请号:JOP20030009
申请日:2003-02-02
Applicant: HOFFMANN LA ROCHE
Inventor: GEO ADAM , ERWIN GOETSCHI , JUERGEN WICHMANN , THOMAS JOHANNES WOLTERING
Abstract: The invention relates to dihydro-benzo[b][1,4] diazepin-2-one derivatives of the general formula wherein R1, R2, X and Y are as defined in the specification and R3 is a six-membered aromatic heterocycle containing 1 to 3 nitrogen atoms or a pyridine-N-oxide as further defined in the specification. The invention further relates to medicaments containing these compounds, a process for their preparation as well as their use for preparation of medicaments for the treatment or prevention of acute and/or chronic neurological disorders.
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公开(公告)号:JO2273B
公开(公告)日:2005-04-07
申请号:JO200233
申请日:2002-04-10
Applicant: HOFFMANN LA ROCHE
Inventor: MUTEL VINCENT , WICHMANN JUERGEN , GEO ADAM , ERWIN GOETSCHI , THOMAS JOHANNES WOLTERING
IPC: C07D243/28 , A61K31/5513 , A61P1/06 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/34 , A61P25/36 , A61P43/00 , C07D401/04 , C07D403/10 , C07D403/14 , C07D413/10 , C07D417/10
CPC classification number: C07D401/04 , C07D403/10 , C07D403/14 , C07D417/10
Abstract: This invention Is concerned with dihydro-benzo [b][1 .4] diazepin-2-one derivatives of the general formula . Wherein RI, R2, R3 and Y are as defined in the specification. The invention further relates to rnedlcaments containing these compounds, a process for their preparation as well as their use for preparation of medicaments for the treatment or prevention of acute and/or chronic neurological disorders
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公开(公告)号:JO2236B1
公开(公告)日:2004-10-07
申请号:JOP20000049
申请日:2000-04-13
Applicant: HOFFMANN LA ROCHE
Inventor: MUTEL VINCENT , VIEIRA ERIC , WICHMANN JURGEN , KONARD BLEICHER , THOMAS JOHANNES WOLTERING
Abstract: The present invention relates to compounds of formula Wherein R1 signifies hydrogen or lower alkyl R2.R3 signify, independently from each other, hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl X signifies O,S or two hydrogen, atoms not forming a bridge A1/A2 signify, independently from each other, phenyl or a 6-membered heterocycle containing 1 or 2 nitrogen atoms B is a group of formula Wherein R3 signifies lower alkyl, lower alkenyl, lower alkinyl, benzyl, lower alkyl- cycloalkyl, lower alkyl- cyano, lower alkyl- pyridinyl, lower alkyl-lower, lower alkoxy-phenyl, lower alkyl-phenyl, which is optionally substituted by lower alkoxy, or phenyl, which is optionally substituted by lower alkoxy, or lower alkyl-thienyl, cycloalkyl, lower alkyl- trifluoromethyl, or lower alkyl – morpholinyl, Y signifies –O,S or a bond Z signifies O.or S Or B is a -5- membered heterocyclic group of formula Wherein R4 and R5 signifies hydrogen, lower alkyl, lower alkoxy, cyclohexyl, lower alkyl- cyclohexyl or trifluoromethyl, with the proviso that at least one of R4 or R5 has to be hydrogen as well as to their pharmaceutically acceptable salts These compounds may be used in the control or prevention of acute and or chronic neurological disorders such as restricted brain function caused by bypass operations or transplants, poor blood supply to the brain, spinal cord injuries, head injuries, hypoxia caused by pregnancy, cardiac arrest, hypoglycaemia, alheimer’s disease, huntington’s chorea, Als, dementia caused by AIDS , eye injuries, retinopathy, cognitive disorders, memory deficits, schizophrenia, idiopathic parkinsonism or parkinsonism caused by medicaments as well as conditions which lead to glutamate deficiency functions, such as e’g, muscle spasms, convulsions, migraine, urinary incontinence, nicotine addiction, psychoses, opiate addition, anxiety, vomiting , acute and chronic pain, dyskinesia and depression
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公开(公告)号:TR199801367A3
公开(公告)日:1999-02-22
申请号:TR9801367
申请日:1998-07-14
Applicant: F. HOFFMANN-LA ROCHE AG
Inventor: GEO ADAM , SABINE KOLCZEWSKI , VINCENT MUTEL , JUERGEN WICHMANN , THOMAS JOHANNES WOLTERING
IPC: A61K31/00 , C07D239/22 , A61K31/505 , A61K31/519 , A61P1/08 , A61P9/00 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P27/02 , A61P43/00 , C07D239/00 , C07D239/40 , C07D277/00 , C07D513/04
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公开(公告)号:BRPI0609719B8
公开(公告)日:2021-05-25
申请号:BRPI0609719
申请日:2006-03-14
Applicant: HOFFMANN LA ROCHE
Inventor: ERWIN GOETSCHI , JUERGEN WICHMANN , SILVIA GATTI MCARTHUR , THOMAS JOHANNES WOLTERING , WYLIE SOLANG PALMER
IPC: C07D471/04 , A61K31/4745 , A61K31/5025 , A61K31/519 , A61P25/00 , C07D487/04
Abstract: derivados de acetilenil-pirazol-pirimidina como antagonistas de mgbur2, bem como processo para a preparação, composição farmacêutica e emprego dos mesmos. a presente invenção refere-se aos compostos da fórmula (1): um processo para a fabricação dos mesmos, seu emprego para a preparação de medicamentos para tratar distúrbios do cns e composições farmacêuticas contendo-os, em que r¹ a r³, a, m, l, e, g, e j são como definidos na descrição e reivindicações.
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16.
公开(公告)号:BRPI0709633B1
公开(公告)日:2020-03-03
申请号:BRPI0709633
申请日:2007-03-19
Applicant: HOFFMANN LA ROCHE
Inventor: ERWIN GOETSCHI , JUERGEN WICHMANN , SILVIA GATTI MCARTHUR , THOMAS JOHANNES WOLTERING
IPC: C07D213/34 , A61K31/444 , A61K31/506 , A61P25/00 , C07D233/96 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/14 , C07D407/04 , C07D409/10 , C07D409/14 , C07D413/04 , C07D413/14
Abstract: derivados de piridina e pirimidina como antagonistas de mgiur2. a presente invenção refere-se a compostos de fórmula (i), um processo para a fabricação destes, seu uso para a preparação de medicamentos para tratar distúrbios do cns e composições farmacêuticas contendo-os: em que a, b, x, y, r^ 1^, r^ 2^, r^ 3^ e r^ 4^ são como definido na descrição e reivindicações.
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公开(公告)号:JO2495B
公开(公告)日:2009-10-05
申请号:JO20039
申请日:2003-02-02
Applicant: HOFFMANN LA ROCHE
Inventor: GEO ADAM , ERWIN GOETSCHI , JUERGEN WICHMANN , THOMAS JOHANNES WOLTERING
Abstract: The invention relates to dihydro-benzo[b][1,4] diazepin-2-one derivatives of the general formula wherein R1, R2, X and Y are as defined in the specification and R3 is a six-membered aromatic heterocycle containing 1 to 3 nitrogen atoms or a pyridine-N-oxide as further defined in the specification. The invention further relates to medicaments containing these compounds, a process for their preparation as well as their use for preparation of medicaments for the treatment or prevention of acute and/or chronic neurological disorders.
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公开(公告)号:JO2299B1
公开(公告)日:2005-09-12
申请号:JOP20000170
申请日:2000-10-11
Applicant: HOFFMANN LA ROCHE
Inventor: MUTEL VINCENT , GOETSCHI ERWIN , ALANINE ALEXANDER , GEO ADAM , THOMAS JOHANNES WOLTERING
IPC: A61K31/55 , A61K31/551 , A61K31/5513 , A61P1/08 , A61P3/08 , A61P9/08 , A61P13/02 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/34 , A61P25/36 , A61P27/02 , A61P29/02 , A61P43/00 , C07D243/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/10 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/08 , C07D409/14 , C07D413/10 , C07D417/02 , C07D417/04 , C07D417/06 , C07D417/10 , C07D417/14
Abstract: The present invention relates to compounds of general formula (I) wherein R is phenyl; pyridine; thiophenyl or thiazolyl, which are optionally substituted. The compounds according to the present invention can be used for treating or preventing acute and/or chronic neurological disorders such as psychosis, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficits.
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公开(公告)号:JO2299B
公开(公告)日:2005-09-12
申请号:JO2000170
申请日:2000-10-11
Applicant: HOFFMANN LA ROCHE
Inventor: MUTEL VINCENT , GOETSCHI ERWIN , ALANINE ALEXANDER , GEO ADAM , THOMAS JOHANNES WOLTERING
IPC: A61K31/55 , A61K31/551 , A61K31/5513 , A61P1/08 , A61P3/08 , A61P9/08 , A61P13/02 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/34 , A61P25/36 , A61P27/02 , A61P29/02 , A61P43/00 , C07D243/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/10 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/08 , C07D409/14 , C07D413/10 , C07D417/02 , C07D417/04 , C07D417/06 , C07D417/10 , C07D417/14
CPC classification number: C07D401/04 , C07D243/12 , C07D403/10 , C07D405/06 , C07D413/10 , C07D417/06 , C07D417/10
Abstract: The present invention relates to compounds of general formula (I) wherein R is phenyl; pyridine; thiophenyl or thiazolyl, which are optionally substituted. The compounds according to the present invention can be used for treating or preventing acute and/or chronic neurological disorders such as psychosis, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficits.
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公开(公告)号:JO2285B
公开(公告)日:2005-09-12
申请号:JO200232
申请日:2002-04-10
Applicant: HOFFMANN LA ROCHE
Inventor: MUTEL VINCENT , WICHMANN JUERGEN , GEO ADAM , ERWIN GOETSCHI , THOMAS JOHANNES WOLTERING
IPC: C07D243/12 , A61K31/551 , A61K31/5513 , A61P25/00 , A61P25/18 , A61P25/28 , A61P43/00 , C07D401/04 , C07D403/04 , C07D403/10 , C07D403/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14
CPC classification number: C07D401/04 , C07D403/10 , C07D403/14 , C07D417/10
Abstract: This invention is concerned with dihydro-benzo [b] [1,4] diazepin-2-one derivatives of the general formula: Wherein RI, R2, R3, X and Y are as defined in the specification. The invention further relates to med medicaments containing there compounds, a process for their preparations as well as their use for preparation of medicaments for the treatment for the treatment or prevention of acute and/or chronic neurological disorders
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