公开(公告)号：CA1334196C

公开(公告)日：1995-01-31

申请号：CA518739

申请日：1986-09-22

Applicant: HOECHST AG

Inventor： SIEGEL HERBERT ,  KAMPE KLAUS-DIETER ,  ALPERMANN HANS G ,  GERHARDS HERMANN J ,  USINGER PATRICIA ,  SCHACHT ULRICH ,  LEVEN MARGRET ,  RAETHER WOLFGANG ,  DITTMAR WALTER ,  SACHSE BURKHARD

IPC: A61K31/41 ,  A61K31/415 ,  C07D233/60 ,  C07D233/64 ,  C07D249/08 ,  C07D521/00 ,  C07D233/56 ,  C07D405/06

Abstract: Arylmethylazoles of the formula I in which Aryl is (substituted) phenyl or naphthyl; Z is CH or N; R1 and Q are H or alkyl; R2 is H, alk(en)yl or alkynyl; R3 and R4 are H, alkyl or other hydrocarbons; or R3 and R4 together are a -(CH2)2-11 chain or a bridged -(CH2)4-5 chain, and their acid addition salts, stereoisomers and optically active enantiomers possess outstanding antimycotic and antidepressant activity. The compounds of the Formula I are obtained, inter alia, from arylmethylazoles II II which are reacted with a strong base and then with a carbonyl compound III 0=CR3R4; thereafter, the product is reacted with the protic acid or with an alkyl halide IV R2Hal. If desired, the products are converted to the acid addition salts, or the stereoisomers or optically active enantiomers are resolved.

公开(公告)号：FI87774C

公开(公告)日：1993-02-25

申请号：FI863795

申请日：1986-09-19

Applicant: HOECHST AG

Inventor： SIEGEL HERBERT ,  KAMPE KLAUS-DIETER ,  ALPERMANN HANS GEORG ,  GERHARDS HERMANN JOSEF ,  USINGER PATRICIA ,  SCHACHT ULRICH ,  LEVEN MARGRET ,  RAETHER WOLFGANG ,  DITTMAR WALTER ,  SACHSE BURKHARD

IPC: A61K31/41 ,  A61K31/415 ,  C07D233/60 ,  C07D233/64 ,  C07D249/08 ,  C07D521/00

公开(公告)号：NO170151C

公开(公告)日：1992-09-16

申请号：NO880973

申请日：1988-03-04

Applicant: HOECHST AG

Inventor： KAMPE KLAUS-DIETER ,  USINGER PATRICIA ,  SIEGEL HERBERT ,  ALPERMANN HANS GEORG ,  GERHARDS HERMANN JOSEF

IPC: A61K31/415 ,  A61P25/24 ,  A61P25/26 ,  A61P31/04 ,  C07D233/60 ,  C07D233/61 ,  C07D405/06 ,  C07D521/00

Abstract: 1-(1-Aryl-2-hydroxyethyl)-imidazoles and salts thereof, processes for the preparation thereof, medicaments containing these compounds, and the use thereof. The invention relates to 1-(1-aryl-2-hydroxyethyl)-imidazoles of the formula I I in which R1, R2, R3, Q, W, X and Y have the meanings specified, and also to medicaments based on these compounds, in particular those having an antimycotic and an antidepressive action.

公开(公告)号：DE3681544D1

公开(公告)日：1991-10-24

申请号：DE3681544

申请日：1986-09-12

Applicant: HOECHST AG

Inventor： SIEGEL HERBERT ,  KAMPE KLAUS-DIETER ,  ALPERMANN HANS GEORG ,  GERHARDS HERMANN JOSEF ,  USINGER PATRICIA ,  SCHACHT ULRICH ,  LEVEN MARGRET ,  RAETHER WOLFGANG ,  DITTMAR WALTER ,  SACHSE BURKHARD

IPC: A61K31/41 ,  A61K31/415 ,  C07D233/60 ,  C07D233/64 ,  C07D249/08 ,  C07D521/00

Abstract: Imidazole or 1,2,4-triazole derivs. of formula (I) and their acid-addn. salts and isomers are new. Ar = (a) phenyl substd. by W, X and Y, or (b) 1- or 2-naphthyl substd. by V and/or U; X = H, 1-4C alkyl, phenyl, F, Cl, Br, OH, 1-4C alkoxy, OAr, 1-4C alkylthio, NR5R'5, CF3 or OCH2Ar2; Ar1 = phenyl substd. by U; Ar2 = phenyl opt. substd. by 1 or 2 of F, Cl, OMe, OEt, and 1-3C alkyl; R5 and R'5 = 1-4C alkyl, or NR5R'5 = pyrrolidino, piperidino or morpholino; Y = H, 1-4C alkyl, F, Cl, Br, 1-4C alkoxy or 1-4C alkylthio; or X+Y = (CH2)x, OCH2CH2 or OCH2O in the 2,3 or 3,4 posn.; W = H, Me or OMe; V = 1-4C alkyl, phenyl, F, Cl, Br, OH, 1-4C alkoxy, 1-4C alkylthio, NR5R'5, benzyloxy or CF3; U = Me, F, Cl or OMe; Z = CH or N; R1 and Q = H or 1-4C alkyl; R2 = H, 1-4C alkyl, 3-5C alkenyl or 3-5C alkynyl; R3 and R4 = H or a 1-12C alkyl or other hydrocarbyl gp. opt. substd. or R3+R4 = (a) 2-11C linear alkylene or alkenylene and/or fused with 1 or 2 benzene rings opt. substd. or (b) 4-5C alkylene which is opt. substd. by 1-4C alkyl, OMe, CH2OMe or phenyl and is bridged by one or more 1-5C bridging gps. which may themselves be bridged, where one bridging gp. may contain a C=C bond and the bridged alkylene gp. may be fused with 1 or 2 benzene rings opt. substd.

公开(公告)号：PH24050A

公开(公告)日：1990-03-05

申请号：PH34277

申请日：1986-09-22

Applicant: HOECHST AG

Inventor： SIEGEL HERBERT ,  GERHARDS HERMANN JOSEF ,  SCHACHT ULRICH ,  DITTMAR WALTER ,  KAMPE KLAUS-DIETER ,  USINGER PATRICIA ,  LEVEN MARGARET ,  RAETHER WOLFGANG ,  SACHSE BURKHARD ,  ALPERMANN HANS GEORG

IPC: A61K31/41 ,  A61K31/415 ,  C07D233/60 ,  C07D233/64 ,  C07D249/08 ,  C07D521/00

Abstract: Arylmethylazoles of the formula I I in which Aryl is (substituted) phenyl or naphthyl; Z is CH or N; R1 and Q are H or alkyl; R2 is H, alk(en)yl or alkynyl; R3 and R4 are H, alkyl or other hydrocarbons; or R3 and R4 together are a -(CH2)2-11 chain or a bridged -(CH2)4-5 chain, and their acid addition salts, stereoisomers and optically active enantiomers possess outstanding antimycotic and antidepressant activity. They are obtained, inter alia, from arylmethylazoles II II which are reacted with a strong base and then with a carbonyl compound III O=CR3R4; thereafter, the product is reacted with the protic acid or with an alkyl halide IV R2Hal. If desired, the products are converted to the acid addition salts, or the stereoisomers or optically active enantiomers are resolved.

公开(公告)号：PT89537A

公开(公告)日：1989-10-04

申请号：PT8953789

申请日：1989-01-26

Applicant: HOECHST AG

Inventor： HENNING RAINER ,  HOCK FRANZ ,  STECHL JENS ,  USINGER PATRICIA ,  URBACH HANSJORG ,  RUGER WOLFGANG

IPC: C07D209/00 ,  C07K5/06

Abstract: (A) n-Octyl 2-alanyl-2-azabicyclo (3,3,0)octane-3- carboxylate derivs. of formula (Ia), in which all five chiral C atoms are in the S configuration, and their salts are new: R'2 = H or Et; R'3 = n-octyl. (B) Intermediates of formula (IX) and (X) in all-S isomer form are also new (see 'Preparation'). (C) ACE inhibitors (I) are used to prepare medicaments with psychotropic, esp. anxiolytic, activity. Pref (I) have min effective doses of 0.1-30 mg/kg in the 'lick-shock' and 'Geller-Seifter' conflict tests.

公开(公告)号：FI890370A

公开(公告)日：1989-07-28

申请号：FI890370

申请日：1989-01-25

Applicant: HOECHST AG

Inventor： RUEGER WOLFGANG ,  URBACH HANSJOERG ,  HENNING RAINER ,  STECHL JENS ,  USINGER PATRICIA ,  HOCK FRANZ

IPC: C12N9/99 ,  A61K31/405 ,  A61K31/47 ,  A61K31/55 ,  A61K38/00 ,  A61K38/55 ,  A61K45/06 ,  A61P25/18 ,  A61P25/20 ,  C07D209/52 ,  C07D223/10 ,  C07D223/16 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  C07K1/06 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K14/81 ,  A61K

Abstract: The invention relates to the use of angiotensin converting enzyme inhibitors as pharmaceuticals with a psychotropic, in particular anxiolytic, effect, to agents containing these and to the use thereof for the treatment or prophylaxis of disorders of the central nervous system, especially of anxiety states. … The invention furthermore relates to compounds of the formula … … in which R is hydrogen or ethyl and R is n-octyl, to processes for the preparation thereof, to agents containing these, and to the use thereof as pharmaceuticals.

公开(公告)号：PH26333A

公开(公告)日：1992-04-29

申请号：PH37894

申请日：1988-12-07

Applicant: HOECHST AG

Inventor： KAMPE KLAUS-DIETER ,  USINGER PATRICIA ,  SIEGEL HERBERT ,  GERHARDS HERMANN JOSEF ,  ALPERMANN HANS GEORG

IPC: C07D233/60

公开(公告)号：HUT53292A

公开(公告)日：1990-10-28

申请号：HU31589

申请日：1989-01-25

Applicant: HOECHST AG

Inventor： RUEGER WOLFGANG ,  URBACH HANSJOERG ,  HENNING RAINER ,  STECHL JENS ,  USINGER PATRICIA ,  HOCK FRANZ

IPC: A61K20060101 ,  A61K37/64

公开(公告)号：ZA8900574B

公开(公告)日：1989-09-27

申请号：ZA8900574

申请日：1989-01-25

Applicant: HOECHST AG

Inventor： RUEGER WOLFGANG ,  WOLFGANG RUEGER ,  URBACH HANSJOERG ,  HANSJOERG URBACH ,  HENNING RAINER ,  RAINER HENNING ,  STECHL JENS ,  JENS STECHL ,  USINGER PATRICIA ,  PATRICIA USINGER ,  HOCK FRANZ ,  FRANZ HOCK

IPC: A61K20060101 ,  A61K