公开(公告)号：ZA975561B

公开(公告)日：1997-12-29

申请号：ZA975561

申请日：1997-06-23

Applicant: HOFFMANN LA ROCHE

Inventor： BOES MICHAEL ,  GODEL THIERRY ,  RIEMER CLAUS ,  SLEIGHT ANDREW

IPC: A61K20060101 ,  A61K31/18 ,  C07C20060101 ,  C07C311/21 ,  C07C311/37 ,  C07D20060101 ,  C07D213/72 ,  C07D239/28 ,  C07C ,  A61K ,  C07D

公开(公告)号：BR9509711A

公开(公告)日：1997-09-30

申请号：BR9509711

申请日：1995-11-08

Applicant: HOFFMANN LA ROCHE

Inventor： BUETTELMANN BERND ,  GODEL THIERRY

IPC: A61K31/00 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5513 ,  A61K31/5517 ,  A61P21/00 ,  A61P21/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/08 ,  A61P25/20 ,  A61P25/22 ,  A61P43/00 ,  C07D487/04 ,  C07D487/14 ,  C07D495/14 ,  C07D495/22

Abstract: PCT No. PCT/EP95/04393 Sec. 371 Date Apr. 22, 1997 Sec. 102(e) Date Apr. 22, 1997 PCT Filed Nov. 8, 1995 PCT Pub. No. WO96/15129 PCT Pub. Date May 23, 1996The invention is concerned with basically-substituted imidazodiazepinones of the formula: I wherein A and the two carbon atoms denoted by alpha and beta together signify: (A1) Q signifies one of the residues: (Q1) (Q2) (Q3) R1 and R2 each signify hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower hydroxyalkyl, lower alkoxy-lower alkyl, (C3-C6)-cycloalkyl, (C3-C6)-cycloalkyl-lower alkyl, amino-lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl or aryl-lower alkyl or together with the nitrogen atom signify a 5- to 8-membered heterocycle optionally containing a further hetero atom or a fused benzene ring; R3 signifies hydrogen and R4 signifies lower alkyl or R3 and R4 together signify a di- or trimethylene group and; R5 and R6 each signify hydrogen, halogen, trifluoromethyl, lower alkoxy or nitro; with the carbon atom denoted by gamma having the S-configuration when R3 is different from hydrogen, and pharmaceutically acceptable acid addition salts thereof. These compounds can be used as anxiolytic and/or anticonvulsant and/or muscle relaxant and/or sedative-hypnotic active substances.

公开(公告)号：HU9701096D0

公开(公告)日：1997-08-28

申请号：HU9701096

申请日：1997-06-25

Applicant: HOFFMANN LA ROCHE

Inventor： BOES MICHAEL ,  GODEL THIERRY ,  RIEMER CLAUS ,  SLEIGHT ANDREW

IPC: A61K31/63 ,  A61K31/18 ,  A61K31/325 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/44 ,  A61K31/505 ,  A61P25/00 ,  C07C311/21 ,  C07C311/38 ,  C07C311/44 ,  C07D209/08 ,  C07D213/76 ,  C07D239/48 ,  C07D239/50 ,  C07D239/69 ,  C07D403/04

Abstract: Use of sulphonamide compounds of formula (I) is claimed for treatment of central nervous disorders. Z = a group of formula (a)-(e); R = H, NH2, lower alkylamino, dialkylamino or alkyl, or halo or CF3; R = H or lower alkyl; R = H, NH2, lower alkylamino, dialkylamino, alkyl or alkoxy, or halo or CF3; R = NH2 or halo, or lower alkylamino, dialkylamino, alkyl or alkoxy; R = H or halo, or lower alkylamino, dialkylamino or alkoxy; R = lower alkyl, alkylamino, dialkylamino or alkoxy, or halo or CF3; R = NH2, lower alkylamino, dialkylamino, alkoxy or alkylsulphanyl, SH, pyrrolidin-1-yl or azetidin-1-yl; R = NH2, lower alkylamino, dialkylamino, alkoxy or alkylsulphanyl, benzylamino, halo, pyrrolidin-1-yl or azetidin-1-yl; R , R = lower alkoxy or alkylamino; R = H or halo; R = H or lower alkyl; and provided that R and R are not both OCH3.

公开(公告)号：NO972983D0

公开(公告)日：1997-06-26

申请号：NO972983

申请日：1997-06-26

Applicant: HOFFMANN LA ROCHE

Inventor： BOES MICHAEL ,  GODEL THIERRY ,  RIEMER CLAUS ,  SLEIGHT ANDREW

IPC: A61K31/63 ,  A61K31/18 ,  A61K31/325 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/44 ,  A61K31/505 ,  A61P25/00 ,  C07C311/21 ,  C07C311/38 ,  C07C311/44 ,  C07D209/08 ,  C07D213/76 ,  C07D239/48 ,  C07D239/50 ,  C07D239/69 ,  C07D403/04

Abstract: Use of sulphonamide compounds of formula (I) is claimed for treatment of central nervous disorders. Z = a group of formula (a)-(e); R = H, NH2, lower alkylamino, dialkylamino or alkyl, or halo or CF3; R = H or lower alkyl; R = H, NH2, lower alkylamino, dialkylamino, alkyl or alkoxy, or halo or CF3; R = NH2 or halo, or lower alkylamino, dialkylamino, alkyl or alkoxy; R = H or halo, or lower alkylamino, dialkylamino or alkoxy; R = lower alkyl, alkylamino, dialkylamino or alkoxy, or halo or CF3; R = NH2, lower alkylamino, dialkylamino, alkoxy or alkylsulphanyl, SH, pyrrolidin-1-yl or azetidin-1-yl; R = NH2, lower alkylamino, dialkylamino, alkoxy or alkylsulphanyl, benzylamino, halo, pyrrolidin-1-yl or azetidin-1-yl; R , R = lower alkoxy or alkylamino; R = H or halo; R = H or lower alkyl; and provided that R and R are not both OCH3.

公开(公告)号：AT150001T

公开(公告)日：1997-03-15

申请号：AT93121161

申请日：1993-12-31

Applicant: HOFFMANN LA ROCHE

Inventor： GODEL THIERRY ,  GUTKNECHT EVA-MARIA

IPC: C07C211/19 ,  A61K31/13 ,  A61K31/135 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P37/00 ,  C07C213/00 ,  C07C215/42 ,  C07C215/52 ,  C07C215/70 ,  C07C217/60 ,  C07C219/24 ,  C07D213/64 ,  C07C215/44 ,  C07C233/18

Abstract: Compounds of the general formula in which R and R each denote hydrogen or lower alkyl optionally substituted by aryl or C3-6-cycloalkyl; R and R either both denote or both denote halogen, or one denotes hydrogen and the other denotes halogen, hydroxyl, lower alkoxy, aryloxy or amino and R denotes hydrogen or - if no primary or secondary amino group(s) is (are) present - denotes alkanoyl, and pharmaceutically utilisable salts of compounds of the formula (I) with acids have useful pharmacodynamic properties as non-competitive NMDA antagonists such that they can be used as neuroprotectives. These compounds are novel, with the exception of rac-cis-4b-(2-aminoethyl)-4b,5,6,7,8,8a,9,10-octahydrophenanthren-8a-o l.

公开(公告)号：HRP921448A2

公开(公告)日：1996-10-31

申请号：HRP921448

申请日：1992-12-18

Applicant: HOFFMANN LA ROCHE

Inventor： BRUDERER HANS ,  GODEL THIERRY ,  IMHOF RENE ,  JAKOB-ROETNE ROLAND

IPC: A61K20060101 ,  A61K31/40 ,  A61K31/405 ,  C07D20060101 ,  C07D209/00 ,  C07D209/04 ,  C07D209/08 ,  C07D209/56 ,  C07D209/60

公开(公告)号：NO179325C

公开(公告)日：1996-09-18

申请号：NO924829

申请日：1992-12-14

Applicant: HOFFMANN LA ROCHE

Inventor： BRUDERER HANS ,  GODEL THIERRY ,  IMHOF RENE ,  JAKOB-ROETNE ROLAND

IPC: A61K20060101 ,  A61K31/403 ,  A61K31/40 ,  A61K31/405 ,  A61K31/435 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/535 ,  A61P25/28 ,  C07D20060101 ,  C07D209/00 ,  C07D209/04 ,  C07D209/08 ,  C07D209/56 ,  C07D209/60 ,  C07D209/90 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D413/04 ,  C07D413/06

Abstract: cis-2,3,3a,4,5,9b-Hexahydro-1H-benz[e]indole derivatives of the general formula in which R denotes a radical of the formula -O-CO-NR R , R denotes lower alkyl, lower cycloalkyl or lower alkyl substituted by lower cycloalkyl, aryl, aroyl, aroylamino, amino or by a cyclic amino, amide or imide group, R denotes hydrogen or lower alkyl, R denotes lower alkyl and R denotes hydrogen or lower alkyl, corresponding trans isomers or cis/trans isomer mixtures and pharmaceutically utilizable acid addition salts thereof are novel and are distinguished by useful therapeutic properties. They are particularly suitable for the treatment or prophylaxis of cognitive disorders and senile dementia (especially Alzheimer's disease) and for the improvement of memory power.

公开(公告)号：NO179325B

公开(公告)日：1996-06-10

申请号：NO924829

申请日：1992-12-14

Applicant: HOFFMANN LA ROCHE

Inventor： BRUDERER HANS ,  GODEL THIERRY ,  IMHOF RENE ,  JAKOB-ROETNE ROLAND

IPC: A61K20060101 ,  A61K31/403 ,  A61K31/40 ,  A61K31/405 ,  A61K31/435 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/535 ,  A61P25/28 ,  C07D20060101 ,  C07D209/00 ,  C07D209/04 ,  C07D209/08 ,  C07D209/56 ,  C07D209/60 ,  C07D209/90 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D413/04 ,  C07D413/06

Abstract: cis-2,3,3a,4,5,9b-Hexahydro-1H-benz[e]indole derivatives of the general formula in which R denotes a radical of the formula -O-CO-NR R , R denotes lower alkyl, lower cycloalkyl or lower alkyl substituted by lower cycloalkyl, aryl, aroyl, aroylamino, amino or by a cyclic amino, amide or imide group, R denotes hydrogen or lower alkyl, R denotes lower alkyl and R denotes hydrogen or lower alkyl, corresponding trans isomers or cis/trans isomer mixtures and pharmaceutically utilizable acid addition salts thereof are novel and are distinguished by useful therapeutic properties. They are particularly suitable for the treatment or prophylaxis of cognitive disorders and senile dementia (especially Alzheimer's disease) and for the improvement of memory power.

公开(公告)号：CA2204030A1

公开(公告)日：1996-05-23

申请号：CA2204030

申请日：1995-11-08

Applicant: HOFFMANN LA ROCHE

Inventor： GODEL THIERRY ,  BUETTELMANN BERND

IPC: A61K31/55 ,  C07D487/04 ,  C07D487/14 ,  C07D495/14

Abstract: The invention is concerned with basically-substituted imidazodiazepines of general formula (I). These compounds can be used as anxiolytic and/or anticonvulsant and/or muscle relaxant and/or sedative-hypnotic active substances.

公开(公告)号：ZA9504024B

公开(公告)日：1995-11-24

申请号：ZA9504024

申请日：1995-05-17

Applicant: HOFFMANN LA ROCHE

Inventor： BUETTELMANN BERND ,  GROSS LAURENCE ,  RIEMER CLAUS ,  GODEL THIERRY ,  NEIDHART MARIE-PAULE HEITZ ,  WYLER RENE

IPC: A61K20060101 ,  C07D20060101 ,  C07D ,  A61K