公开(公告)号：NZ250652A

公开(公告)日：1995-10-26

申请号：NZ25065294

申请日：1994-01-10

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 ,  C07C215/88 ,  C07C219/32

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：NO950999L

公开(公告)日：1995-09-18

申请号：NO950999

申请日：1995-03-15

Applicant: HOFFMANN LA ROCHE

Inventor： GODEL THIERRY ,  HUNKELER WALTER ,  STADLER HEINZ ,  WIDMER ULRICH

IPC: A61K31/41 ,  A61K31/55 ,  A61K31/5517 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  A61P43/00 ,  C07D487/02 ,  C07D487/04 ,  C07D495/12 ,  C07D495/14 ,  C07D498/14

Abstract: Aminomethyl-substd. oxadiazolyl-imidazodiazepines of formula (I) and their addn salts are new: A and C atoms alpha and beta form a gp of formula e.g. (A ):Q = a gp. of formula e.g. (Q ):R , R = H; lower alkyl,etc.;or NR R = 5-8 membered heterocycle opt. contg. a further hetero atom or carrying a fused benzene ring; R = H and R = lower alkyl; or R +R = H; halo;etc.; and C atom gamma has the S configuration when R is other than H.

公开(公告)号：NO950999A

公开(公告)日：1995-09-18

申请号：NO950999

申请日：1995-03-15

Applicant: HOFFMANN LA ROCHE

Inventor： GODEL THIERRY ,  HUNKELER WALTER ,  STADLER HEINZ ,  WIDMER ULRICH

IPC: A61K31/41 ,  A61K31/55 ,  A61K31/5517 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  A61P43/00 ,  C07D487/02 ,  C07D487/04 ,  C07D495/12 ,  C07D495/14 ,  C07D498/14

CPC classification number: C07D487/04 ,  C07D495/14

公开(公告)号：NO950999D0

公开(公告)日：1995-03-15

申请号：NO950999

申请日：1995-03-15

Applicant: HOFFMANN LA ROCHE

Inventor： GODEL THIERRY ,  HUNKELER WALTER ,  STADLER HEINZ ,  WIDMER ULRICH

IPC: A61K31/41 ,  A61K31/55 ,  A61K31/5517 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  A61P43/00 ,  C07D487/02 ,  C07D487/04 ,  C07D495/12 ,  C07D495/14 ,  C07D498/14 ,  C07D

Abstract: Aminomethyl-substd. oxadiazolyl-imidazodiazepines of formula (I) and their addn salts are new: A and C atoms alpha and beta form a gp of formula e.g. (A ):Q = a gp. of formula e.g. (Q ):R , R = H; lower alkyl,etc.;or NR R = 5-8 membered heterocycle opt. contg. a further hetero atom or carrying a fused benzene ring; R = H and R = lower alkyl; or R +R = H; halo;etc.; and C atom gamma has the S configuration when R is other than H.

公开(公告)号：CZ8694A3

公开(公告)日：1994-08-17

申请号：CZ8694

申请日：1994-01-14

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

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：HU9400056D0

公开(公告)日：1994-05-30

申请号：HU9400056

申请日：1994-01-10

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

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：NO924829A

公开(公告)日：1993-06-21

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: A61K31/40 ,  A61K20060101 ,  A61K31/403 ,  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

CPC classification number: C07D209/60

公开(公告)号：UY23524A1

公开(公告)日：1993-06-11

申请号：UY23524

申请日：1992-12-18

Applicant: HOFFMANN LA ROCHE

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

IPC: A61P25/00 ,  A61K20060101 ,  A61K31/40 ,  A61K31/405 ,  A61P25/28 ,  C07D20060101 ,  C07D209/00 ,  C07D209/04 ,  C07D209/08 ,  C07D209/56 ,  C07D209/60 ,  C07D209/90

Abstract: Se describe un procedimiento para la preparación de derivados de cis-2,3,3a,4,5,9b-hexahidro-1H-benzo[b] indol, de fórmula general I (figura 1) en donde R1 significa un radical de la fórmula -O-CO-NR4-R5; R2 significa n-propilo, entre otras posibilidades; de isómeros trans o mezclas isoméricas cis-trans correspondientes y de sus sales farmacéuticamente utilizables. Como ejemplo no limitante: (+)-cis-3-(2-ciclohexiletil)-2,3,3a,4,5,9b-hexahidro-1H-benzo[e]indol-6-ildimetilcarbamato. Se usa en el tratamiento o profilaxis de trastornos cognoscitivos y demencia senil (especialmente enfermedad de Alzheimer) y para la mejora de capacidad de memoria.

公开(公告)号：CA2299139C

公开(公告)日：2011-03-29

申请号：CA2299139

申请日：2000-02-23

Applicant: HOFFMANN LA ROCHE

Inventor： BOS MICHAEL ,  BRANCA QUIRICO ,  GALLEY GUIDO ,  GODEL THIERRY ,  HOFFMANN TORSTEN ,  HUNKELER WALTER ,  SCHNIDER PATRICK ,  STADLER HEINZ

IPC: C07D213/82 ,  A61K20060101 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/444 ,  A61K31/455 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/00 ,  A61P9/00 ,  A61P11/00 ,  A61P11/06 ,  A61P19/02 ,  A61P25/00 ,  A61P25/04 ,  A61P25/28 ,  A61P25/30 ,  A61P27/02 ,  A61P29/00 ,  A61P43/00 ,  C07D20060101 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/63 ,  C07D213/65 ,  C07D213/74 ,  C07D213/75 ,  C07D213/78 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: The present invention relates to compounds of the general formula (see formula I) wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; or R and R1, when adjacent, may be together -CH=CH-CH=CH-; R2 and R2' are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R2 and R2', when adjacent, may be together -CH=CH-CH-CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R3 and R3' are each hydrogen, lower alkyl or together with the carbon to which they are attached form a cycloalkyl group; R4 is hydrogen, -N(R)2, -N(R5)(CH2)n OH, -N(R5)S(O)2-lower alkyl, -N(R5)S(O)2--phenyl, -N=CH-N(R5)2, -N(R5)C(O)R5 or a cyclic tertiary amine of the group (see formula II) or the group (see formula III); R5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, -(CH2)n COO-lower alkyl, -N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)n O(CH2)n OH, -CHO or a 5-or 6--membered heterocyclic group, wherein said 5- or 6-membered heterocyclic group is optionally bonded via an alkylene group, X is -C(O)N(R5)-, -(CH2)m O-, -(CH2)m N(R5)-, -N(R5)C(O)-, or -N(R)(CH2)m-; n is 0-4; and m is 1 or 2; with the proviso that the compound is other than 2-(3,5-Bis-trifluoromethyl-phenyl)-N--methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide, and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I show a high affinity to the NK-1 receptor. They may be used for the treatment of diseases, which relate to NK-1 receptor antagonists.

公开(公告)号：PT1394150E

公开(公告)日：2011-02-17

申请号：PT03026298

申请日：2000-02-15

Applicant: HOFFMANN LA ROCHE

Inventor： STADLER HEINZ ,  HUNKELER WALTER ,  QUIRICO BRANCA DR ,  GALLEY GUIDO ,  BOES MICHAEL ,  HOFFMANN TORSTEN ,  SCHNIDER PATRICK ,  GODEL THIERRY

IPC: C07D213/82 ,  A61K20060101 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/444 ,  A61K31/455 ,  A61K31/496 ,  A61P1/00 ,  A61P9/00 ,  A61P11/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/28 ,  A61P25/30 ,  A61P27/02 ,  A61P29/00 ,  A61P43/00 ,  C07D20060101 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/63 ,  C07D213/65 ,  C07D213/74 ,  C07D213/75 ,  C07D213/78 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14