公开(公告)号：NZ214536A

公开(公告)日：1988-08-30

申请号：NZ21453685

申请日：1985-12-12

Applicant: HOFFMANN LA ROCHE

Inventor： HEBEISEN P

IPC: C07D499/04 ,  C07D205/08 ,  C07D277/20 ,  C07D277/32 ,  C07D277/40 ,  C07D417/12 ,  C07D499/10 ,  C07D499/64 ,  C07D499/70 ,  C07D501/04 ,  C07D501/20

Abstract: There is described a process for the manufacture of a compound of the formula IV wherein R1 is lower alkyl, lower alkanoyl, lower alkenyl or the group -CH2COOR2 or -C(CH3)2COOR2 and R2 is a readily cleavable group, by reacting a compound of the formula II wherein R is lower alkyl, with an alkali metal allylate and reacting the resulting compound of the formula I wherein M is an alkali metal atom, with a compound of the formula R1-X, wherein X is a leaving group. This process can be used to manufacture antimicrobially active mono- beta -lactam, cephalosporin and penicillin derivatives.

公开(公告)号：UY27097A1

公开(公告)日：2002-07-31

申请号：UY27097

申请日：2001-12-26

Applicant: HOFFMANN LA ROCHE ,  VERNALIS RES LTD

Inventor： MATTEI P ,  MIZRAHI J ,  KENNETT G A ,  RICHTER H ,  PLANCHER J M ,  BENTLEY J M ,  BICKERDIKE M J ,  HEBEISEN P ,  LIGHTOWLER S ,  ROEVER S ,  VICKERS S P ,  TAYLOR S ,  MORLEY T J

IPC: A61K31/365 ,  A61K31/407 ,  A61P1/00 ,  A61P1/14 ,  A61P1/18 ,  A61P3/04 ,  A61P3/10 ,  A61P5/48 ,  A61P7/12 ,  A61P9/10 ,  A61P11/00 ,  A61P15/10 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D487/04 ,  C07D471/04 ,  A61K31/4353

Abstract: La presente invención se refiere a compuestos químicos de fórmula (I), tanto como a sales farmacéuticamente utilizables, solvatos y esteres de los mismo, en donde R1 a R4 y n poseen el significado dado en la reivindicación 1. Pueden ser usados en forma de preparaciones farmacéuticas para el tratamiento o prevención de trastornos del sistema nervioso central, trastornos cardiovasculares, trastornos gastrointestinales, diabetes, obesidad y apnes durante el sueno.

公开(公告)号：UY27204A1

公开(公告)日：2002-09-30

申请号：UY27204

申请日：2002-03-12

Applicant: HOFFMANN LA ROCHE ,  VERNALIS RES LTD

Inventor： MATTEI P ,  RICHTER H ,  ROEVER S ,  TAYLOR S ,  MULLER M ,  HEBEISEN P

IPC: A61K31/337 ,  A61K31/4985 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P7/02 ,  A61P9/00 ,  A61P11/00 ,  A61P13/02 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32 ,  A61P29/00 ,  A61P43/00 ,  C07D487/04 ,  C07D487/02

Abstract: El presente invento se refiere a compuestos químicos de fórmula (I) así como sus sales, solvatos y ésteres farmacéuticamente aceptables, en donde R1 a R7 tienen el significado expuesto en la descripción y las reivindicaciones. Los compuestos pueden utilizarse en forma de preparados farmacéuticos para el tratamiento o prevención de trastornos del sistema nervioso central, lesión del sistema nervioso central, trastornos cardiovasculares, trastornos gastrointestinales, diabetes insipidus, diabetes tipo II, obesidad y apnea del sueno.

公开(公告)号：YU70888A

公开(公告)日：1989-12-31

申请号：YU70888

申请日：1988-04-08

Applicant: HOFFMANN LA ROCHE

Inventor： FURLENMEIER A ,  GOETSCHI E ,  HEBEISEN P ,  HOFHEIZ W ,  LINK H

IPC: C07D519/06 ,  A61K31/545 ,  A61P31/04 ,  C07D501/36 ,  C07D501/46 ,  C07D519/00 ,  C07D501/00

Abstract: Acyl derivatives of the formula I in which R is an acyl group, excluding those acyl groups of the formula in which A is a group of the formulae -NHCO-, -NHCONHCO-, -NHCOCH=CH-, wherein R6 is hydrogen or lower alkyl; R1 and R2 are hydrogen or a protecting group, X is hydrogen, halogen, lower alkoxy, nitro or -OR2, n is 1 or 2, R4 and R5 are hydrogen or together represent an additional bond and Z is a direct bond or carbonyl (where R4 and R5 both represent hydrogen) or a group of the formula -O-B- (where R4 and R5 together represent an additional bond) in which B is a straight-chain, branched or cyclic lower alkylene; and wherein R3 is a substituted bicyclic group of the formulae 7 5 NR7NNN+RE wherein R7 and R8 are independently hydrogen, lower alkyl or trifluoromethyl or, in formulae (a), (b), (e) and (f) together represent alkylene with 3 or 4 carbon atoms, and R', R'' and R''' are independently hydrogen, lower alkyl or lower cycloalkyl; wherein compounds of formula I in which R4 and R5 together represent an additional bond are present in the syn-isomeric form or as a mixture with the anti-isomeric form in which the syn-isomeric form predominates, as well as readily hydrolyzable esters and salts of these compounds and hydrates of the compounds of formula I or of their esters and salts. These compounds are useful as antibiotics.