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：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：AU589684B2

公开(公告)日：1989-10-19

申请号：AU6299986

申请日：1986-09-22

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 ,  A61K31/445 ,  A61K31/535 ,  C07D405/06

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：HUT41744A

公开(公告)日：1987-05-28

申请号：HU399986

申请日：1986-09-19

Applicant: HOECHST AG

Inventor： SIEGEL HERBERT ,  KAMPE KLAUS-DIETER ,  ALPERMANN HANS ,  GERHARDS HERMANN ,  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: 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：ZA867189B

公开(公告)日：1987-05-27

申请号：ZA867189

申请日：1986-09-22

Applicant: HOECHST AG

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

IPC: C07D405/06 ,  A01N20060101 ,  A61K20060101 ,  A61K31/415 ,  A61P25/18 ,  A61P31/04 ,  C07D20060101 ,  C07D233/60 ,  C07D233/61 ,  C07D249/00 ,  C07D249/08 ,  C07D317/00 ,  C09D20060101 ,  C10M20060101 ,  C10N20060101 ,  C07D ,  A01N ,  A61K ,  C09D ,  C10M ,  C10N

公开(公告)号：AU6299986A

公开(公告)日：1987-03-26

申请号：AU6299986

申请日：1986-09-22

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 ,  C07D405/10 ,  A61K31/445 ,  A61K31/535

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：DK451686D0

公开(公告)日：1986-09-22

申请号：DK451686

申请日：1986-09-22

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 ,  C07D ,  A01N

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：ES2012526A6

公开(公告)日：1990-04-01

申请号：ES8801355

申请日：1988-05-03

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 ,  A01N43/50 ,  A61K31/45

Abstract: PROCEDIMIENTO PARA LA PREPARACION DE ARILMETILAZOLES SUSTITUIDOS DE FORMULA I

公开(公告)号：ES2002365A6

公开(公告)日：1988-08-01

申请号：ES8602081

申请日：1986-09-22

Applicant: HOECHST AG

Inventor： SIEGEL HERBERT ,  KAMPE KLAUSDIETER ,  ALPERMANN HANS GEORG ,  GERHARDS HERMANN JOSEF ,  USINGER PATRICIA ,  SCHACHT ULRICH ,  LEVEN MARGRET ,  RAETHER WOLFGANG

IPC: A61K31/41 ,  A61K31/415 ,  C07D233/60 ,  C07D233/64 ,  C07D249/08 ,  C07D521/00 ,  A01N43/50

Abstract: PROCEDIMIENTO PARA LA PREPARACION DE ARILMETILAZOLES SUSTITUIDOS DE FORMULA I DONDE ARIL SIGNIFICA FENILO O NAFTILO (SUSTITUIDO), Z ES CH O N, R1 Y Q SON H O ALQUILO, R2 ES H, ALQ(EN)ILO O ALQUINILO, R3 Y R4 SON H, ALQUILO U OTROS HIDROCARBUROS O SIGNIFICAN CONJUNTAMENTE UNA CADENA -(CH2)2-11- O UNA CADENA -(CH2)4-5- PUENTEADA, EN EL QUE SE HACE REACCIONAR UN COMPUESTO DE FORMULA II DONDE ARIL, R1, Z Y Q SON COMO ANTES, CON 1 O 2 EQUIVALENTES DE UNA BASE FUERTE, Y A CONTINUACION SE HACE REACCIONAR PRIMERO CON UN COMPUESTO CARBONILICO DE FORMULA III DON R3 Y R4 SON COMO ANTES, Y LUEGO CON UN ACIDO PROTOUVONIC O UN HALOGENURO DE ALQUILO DE FORMULA IV R2HALIV DONDE R2 ES COMO ANTES Y HAL ES CLORO, BROMO O YODO. LOS COMPUESTOA OBTENIDOS SON ESPECIALMENTE UTILES COMO ANTIMICOTICOS Y ANTIDEPRESIVOS.