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1. WO1996004282 - CARBAPENEM COMPOUNDS, COMPOSITIONS AND METHODS OF TREATMENT

Publication Number WO/1996/004282
Publication Date 15.02.1996
International Application No. PCT/US1995/010029
International Filing Date 25.07.1995
Chapter 2 Demand Filed 22.02.1996
IPC
C07D 477/20 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
477Heterocyclic compounds containing 1-azabicyclo heptane ring systems, i.e. compounds containing a ring system of the formula: , e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
10with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
12with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6
16with hetero atoms or carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 3
20Sulfur atoms
CPC
C07D 477/20
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
477Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula: , carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
10with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4 and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
12with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6
16with hetero atoms or carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 3
20Sulfur atoms
Y02P 20/55
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
20Technologies relating to chemical industry
50Improvements relating to the production of products other than chlorine, adipic acid, caprolactam, or chlorodifluoromethane, e.g. bulk or fine chemicals or pharmaceuticals
55Synthetic design, e.g. reducing the use of auxiliary or protecting groups
Applicants
  • MERCK & CO., INC. [US/US]; 126 East Lincoln Avenue Rahway, NJ 07065, US (AllExceptUS)
  • WADDELL, Sherman, T. [US/US]; US (UsOnly)
  • RATCLIFFE, Ronald, W. [US/US]; US (UsOnly)
  • BLIZZARD, Timothy, A. [US/US]; US (UsOnly)
  • WILDONGER, Kenneth, J. [US/US]; US (UsOnly)
  • WILKENING, Robert, R. [US/US]; US (UsOnly)
  • SZUMILOSKI, Sandra, P. [US/US]; US (UsOnly)
Inventors
  • WADDELL, Sherman, T.; US
  • RATCLIFFE, Ronald, W.; US
  • BLIZZARD, Timothy, A.; US
  • WILDONGER, Kenneth, J.; US
  • WILKENING, Robert, R.; US
  • SZUMILOSKI, Sandra, P.; US
Common Representative
  • MERCK & CO., INC.; 126 East Lincoln Avenue Rahway, NJ 07065, US
Priority Data
282,69329.07.1994US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) CARBAPENEM COMPOUNDS, COMPOSITIONS AND METHODS OF TREATMENT
(FR) COMPOSES DE CARBAPENEMS, COMPOSITIONS ET PROCEDES DE TRAITEMENT
Abstract
(EN)
Carbapenems of formula (I) are disclosed as MRSA active agents. R1 represents hydrogen or methyl; CO2M represents a carboxylic acid, a carboxylate anion with or without a pharmaceutically acceptable counterion, a pharmaceutically acceptable ester group or a carboxylic acid protected by a protecting group; P* represents hydrogen or a hydroxyl protecting group; Het represents a heterocyclic group which is uncharged or positively charged, containing no more than three positively charged atoms, and is selected from the group consisting of: (a) and (b) wherein $(1,3)$ represents the point of attachment to S; A represents O or S; and X, Y and Z independently represent CR, N or N+Ra.
(FR)
Cette invention concerne des carbapenems de formule (I) utilisés comme agents actifs contre le staphylocoque doré résistant à la méthiciline. Dans la formule (I) R1 représente hydrogène ou méthyle; CO2M représente un acide carboxylique avec ou sans un contre-ion pharmaceutiquement acceptable, un groupe ester pharmaceutiquement acceptable ou un acide carboxylique protégé par un groupe protecteur; P* représente hydrogène ou un groupe protecteur hydroxyle; Het représente un groupe hétérocyclique non chargé ou chargé positivement, ne contenant pas plus de trois atomes chargés positivement et sélectionné dans le groupe constitué par: (a) et (b), dans lesquels $(1,3)$ représente le point d'attache à S; A représente O ou S; et X, Y et Z représentent indépendamment CR, N ou N+Ra.
Also published as
Latest bibliographic data on file with the International Bureau