公开(公告)号：BR8103216A

公开(公告)日：1982-02-16

申请号：BR8103216

申请日：1981-05-22

Applicant: HOFFMANN LA ROCHE

Inventor： STOHLER H ,  HOFHEINZ W

IPC: C07D233/92 ,  A61K31/415 ,  A61P33/10 ,  C07D233/91

Abstract: 2-Nitroimidazoles having filaricidal activity of the formula I wherein A is one of the groups -C(R3)=C(R1)(R2),-CHBr-CH2Br or -CH2-CCl=CH2; n is 1, 2, 3 or 4; R1 and R2 are hydrogen or C1-3-alkyl and R3 is hydrogen, C1-3-alkyl, chlorine or bromine, and processes for their preparation are described. The compounds of formula I and compounds of formula VII wherein R4 is -CH2-CH2OH, -CH2-CHOH-CH2OCH3, -CH2-CHOH-CH2OH or are useful in the treatment of filariasis is also described.

公开(公告)号：GR78269B

公开(公告)日：1984-09-26

申请号：GR830171525

申请日：1983-06-01

Applicant: HOFFMANN LA ROCHE

Inventor： FURLENMEIER A ,  HOFHEINZ W ,  HUBSCHVERLEN C N ,  ISENRING H-P

IPC: C07D205/085 ,  C07D263/48 ,  C07D277/20 ,  C07D403/12 ,  C07D405/04 ,  C07D413/12 ,  C07D417/12 ,  C07F7/08

公开(公告)号：NZ204387A

公开(公告)日：1986-12-05

申请号：NZ20438783

申请日：1983-05-27

Applicant: HOFFMANN LA ROCHE

Inventor： FURLENMEIER A ,  HOFHEINZ W ,  HUBSCHWERLEN C N ,  ISENRING H P

IPC: A61K31/397 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61P31/04 ,  C07D205/08 ,  C07D205/085 ,  C07D263/48 ,  C07D277/20 ,  C07D277/40 ,  C07D277/70 ,  C07D403/12 ,  C07D405/04 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07F7/08 ,  A61K31/395

Abstract: Antimicrobial 2-oxo-1-azetidinesulphonic acids of the formula in which H2N represents an amino-substituted thiazolyl group, R1 is lower alkyl which is substituted by carbamoyl, lower alkylsuphonyl, azido, piperidine-carbonyl, (hexahydro-1H-azepin-1-yl)carbonyl or lower alkynyl, and R2 is hydrogen or a lower organic group, typically, carbamoyloxymethyl.

公开(公告)号：NZ204386A

公开(公告)日：1986-12-05

申请号：NZ20438683

申请日：1983-05-27

Applicant: HOFFMANN LA ROCHE

Inventor： FURLENMEIER A ,  HOFHEINZ W ,  HUBSCHWERLEN C N ,  ISENRING H P

IPC: C07D205/085 ,  C07D263/48 ,  C07D277/20 ,  C07D403/12 ,  C07D405/04 ,  C07D413/12 ,  C07D417/12 ,  C07F7/08 ,  C07D277/00 ,  C07D213/00 ,  C07D233/00 ,  C07D263/00 ,  C07D285/00

公开(公告)号：DK470181A

公开(公告)日：1982-04-25

申请号：DK470181

申请日：1981-10-23

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM-MOLINA S ,  HOFHEINZ W

IPC: C07D499/87 ,  A61K31/43 ,  A61P43/00 ,  C07D499/00 ,  C07D499/86 ,  C07D499/861 ,  C07D499/897 ,  C07F9/6561 ,  C07D

Abstract: There are presented beta -lactams of the formula I wherein R1 is cyano or a group of the formula R4-CO- or R5-A-CO-, R2 is hydrogen, lower alkyl or halogen, R3 is hydrogen or a group readily cleavable by hydrolysis, n is the number 0, 1 or 2, R4 is hydrogen, hydroxy, lower alkoxy, lower alkyl, aryl or a group of the formula R5 is halogen, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, aryl, aryloxy, arylthio, arylsulphinyl, arylsulphonyl or di-(loweralkoxy)phoshinyl, R6 and R7 are lower alkyl and A is lower alkylene, and pharmaceutically acceptable salts of carboxylic acids of formula I with bases. The compounds exhibit pronounced beta -lactamase-inhibiting properties.

公开(公告)号：BR7602031A

公开(公告)日：1976-10-05

申请号：BR7602031

申请日：1976-04-02

Applicant: HOFFMANN LA ROCHE

Inventor： HOFHEINZ W

IPC: C07D233/94 ,  C07D233/92

公开(公告)号：NZ198672A

公开(公告)日：1985-05-31

申请号：NZ19867281

申请日：1981-10-16

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM-MOLINA S ,  HOFHEINZ W

IPC: C07D499/87 ,  A61K31/43 ,  A61P43/00 ,  C07D499/00 ,  C07D499/86 ,  C07D499/861 ,  C07D499/897 ,  C07F9/6561

Abstract: There are presented beta -lactams of the formula I wherein R1 is cyano or a group of the formula R4-CO- or R5-A-CO-, R2 is hydrogen, lower alkyl or halogen, R3 is hydrogen or a group readily cleavable by hydrolysis, n is the number 0, 1 or 2, R4 is hydrogen, hydroxy, lower alkoxy, lower alkyl, aryl or a group of the formula R5 is halogen, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, aryl, aryloxy, arylthio, arylsulphinyl, arylsulphonyl or di-(loweralkoxy)phoshinyl, R6 and R7 are lower alkyl and A is lower alkylene, and pharmaceutically acceptable salts of carboxylic acids of formula I with bases. The compounds exhibit pronounced beta -lactamase-inhibiting properties.

公开(公告)号：ZW8781A1

公开(公告)日：1981-12-16

申请号：ZW8781

申请日：1981-04-15

Applicant: HOFFMANN LA ROCHE

Inventor： HOFHEINZ W ,  STOHLER H

IPC: C07D233/92 ,  A61K31/415 ,  A61P33/10 ,  C07D233/91 ,  C07D ,  A61K

Abstract: 2-Nitroimidazoles having filaricidal activity of the formula I wherein A is one of the groups -C(R3)=C(R1)(R2),-CHBr-CH2Br or -CH2-CCl=CH2; n is 1, 2, 3 or 4; R1 and R2 are hydrogen or C1-3-alkyl and R3 is hydrogen, C1-3-alkyl, chlorine or bromine, and processes for their preparation are described. The compounds of formula I and compounds of formula VII wherein R4 is -CH2-CH2OH, -CH2-CHOH-CH2OCH3, -CH2-CHOH-CH2OH or are useful in the treatment of filariasis is also described.

公开(公告)号：AU7064081A

公开(公告)日：1981-11-26

申请号：AU7064081

申请日：1981-05-15

Applicant: HOFFMANN LA ROCHE

Inventor： HOFHEINZ W ,  STOHLER H

IPC: C07D233/92 ,  A61K31/415 ,  A61P33/10 ,  C07D233/91

Abstract: 2-Nitroimidazoles having filaricidal activity of the formula I wherein A is one of the groups -C(R3)=C(R1)(R2),-CHBr-CH2Br or -CH2-CCl=CH2; n is 1, 2, 3 or 4; R1 and R2 are hydrogen or C1-3-alkyl and R3 is hydrogen, C1-3-alkyl, chlorine or bromine, and processes for their preparation are described. The compounds of formula I and compounds of formula VII wherein R4 is -CH2-CH2OH, -CH2-CHOH-CH2OCH3, -CH2-CHOH-CH2OH or are useful in the treatment of filariasis is also described.