公开(公告)号：BRPI0709633B8

公开(公告)日：2021-05-25

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 composição farmacêutica e uso dos mesmos. 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.

公开(公告)号：JO2285B1

公开(公告)日：2005-09-12

申请号：JOP20020032

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

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

公开(公告)号：JO2273B1

公开(公告)日：2005-04-07

申请号：JOP20020033

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

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

公开(公告)号：HK1045683B

公开(公告)日：2006-02-03

申请号：HK02107101

申请日：2002-09-26

Applicant: F HOFFMANN-LA ROCHE AG [CH/CH]

Inventor： KONRAD BLEICHER ,  VINCENT MUTEL ,  ERIC VIEIRA ,  JURGEN WICHMANN ,  THOMAS JOHANNES WOLTERING

IPC: C07D20060101 ,  C07D295/08 ,  A61K20060101 ,  A61K31/325 ,  A61K31/352 ,  A61K31/381 ,  A61K31/382 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/4409 ,  A61K31/5375 ,  A61P20060101 ,  A61P25/00 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/34 ,  A61P27/02 ,  C07C20060101 ,  C07C233/90 ,  C07C233/91 ,  C07C271/64 ,  C07C333/10 ,  C07D213/00 ,  C07D213/30 ,  C07D213/60 ,  C07D213/61 ,  C07D263/48 ,  C07D271/00 ,  C07D271/06 ,  C07D271/07 ,  C07D271/10 ,  C07D271/113 ,  C07D295/088 ,  C07D311/84 ,  C07D333/16 ,  C07D335/12 ,  C07D335/14 ,  C07D409/12 ,  C07D413/12

公开(公告)号：JO2262B1

公开(公告)日：2004-10-07

申请号：JOP20000169

申请日：2000-10-10

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 ,  A61P9/00 ,  A61P9/10 ,  A61P13/00 ,  A61P21/02 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/34 ,  A61P25/36 ,  A61P27/02 ,  A61P43/00 ,  C07D243/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D491/056 ,  C07D491/113 ,  C07F7/10

Abstract: The present invention relates to compounds of general formula (I) wherein X is a single bond or an ethynediyl group, wherein, in case X is a single bond, R is halogen or phenyl which is optionally substituted with halogen, lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, or cyano; In case X is an ethynediyl group, R is phenyl, optionally substituted with halogen, lower alkyl, halo-lower alkyl, lower cycloalkyl, lower alkoxy or halo-lower alkoxy; R is a 5 or 6 membered aryl or heteroaryl 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

公开(公告)号：JO2262B

公开(公告)日：2004-10-07

申请号：JO2000169

申请日：2000-10-10

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 ,  A61P9/00 ,  A61P9/10 ,  A61P13/00 ,  A61P21/02 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/34 ,  A61P25/36 ,  A61P27/02 ,  A61P43/00 ,  C07D243/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D491/056 ,  C07D491/113 ,  C07F7/10

CPC classification number: C07D243/12

Abstract: The present invention relates to compounds of general formula (I) wherein X is a single bond or an ethynediyl group, wherein, in case X is a single bond, R is halogen or phenyl which is optionally substituted with halogen, lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, or cyano; In case X is an ethynediyl group, R is phenyl, optionally substituted with halogen, lower alkyl, halo-lower alkyl, lower cycloalkyl, lower alkoxy or halo-lower alkoxy; R is a 5 or 6 membered aryl or heteroaryl 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

公开(公告)号：BRPI0609719B1

公开(公告)日：2020-12-01

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.

公开(公告)号：MY176608A

公开(公告)日：2020-08-18

申请号：MYPI20030378

申请日：2003-02-05

Applicant: HOFFMANN LA ROCHE

Inventor： GEO ADAM ,  THOMAS JOHANNES WOLTERING ,  ERWIN GOETSCHI ,  JUERGEN WICHMANN

IPC: A61K31/5513 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10

Abstract: This invention relates to dihydro-benzo[b][l,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 heterocyde containing l 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.

公开(公告)号：MY126586A

公开(公告)日：2006-10-31

申请号：MYPI20001650

申请日：2000-04-18

Applicant: HOFFMANN LA ROCHE

Inventor： THOMAS JOHANNES WOLTERING ,  JURGEN WICHMANN ,  VINCENT MUTEL ,  ERIC VIEIRA ,  KONRAD BLEICHER

IPC: C07D295/08 ,  C07D335/14 ,  A61K31/325 ,  A61K31/352 ,  A61K31/381 ,  A61K31/382 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/4409 ,  A61K31/5375 ,  A61P25/00 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/34 ,  A61P27/02 ,  C07C233/90 ,  C07C233/91 ,  C07C271/64 ,  C07C333/10 ,  C07C333/16 ,  C07D213/00 ,  C07D213/30 ,  C07D213/60 ,  C07D213/61 ,  C07D263/48 ,  C07D271/00 ,  C07D271/06 ,  C07D271/07 ,  C07D271/10 ,  C07D271/113 ,  C07D295/088 ,  C07D311/84 ,  C07D333/16 ,  C07D335/12 ,  C07D409/12 ,  C07D413/12

Abstract: THE PRESENT INVENTION RELATES TO COMPOUNDS OF FORMULA WHEREIN R1 SIGNIFIES HYDROGEN OR LOWER ALKYL; R2, R2' 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 ALKONYL-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 ALKYLTRIFIUOROMETHYL 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 FORMULAS 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, ALZHEIMER'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 ADDICTION, ANXIETY, VOMITING, ACUTE AND CHRONIC PAIN, DYSKINESIA AND DEPRESSION.

公开(公告)号：MA26520A1

公开(公告)日：2004-12-20

申请号：MA25167

申请日：1998-07-14

Applicant: HOFFMANN LA ROCHE

Inventor： GEO ADAM ,  SABINE KOLCZEWSKI ,  VINCENT MUTEL ,  JURGEN WICHMANN ,  THOMAS JOHANNES WOLTERING

IPC: A61K31/00 ,  A61K31/505 ,  A61K31/519 ,  A61P1/08 ,  C07D239/22 ,  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 ,  C07D239/70 ,  C07D277/60 ,  A61K31/425