Abstract: Compounds, compositions and methods of using the compounds of the formula as anti-allergics ##STR1## wherein X' is the same as X, X' is at the 3 or 4 position and is ##STR2##
Abstract: There is described the stereoselective total synthesis of novel .DELTA..sup.2,3 -1,4-morpholine-2-carboxylic acids possessing a fused .beta.-lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula ##STR1## wherein Z is halo, hydroxyl, etherified hydroxyl or hydroxyl esterified with a carboxylic acid residue or a sulfonic acid residue and X is amino, azido or acylamino. Also included in the invention are compounds of formula I in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds of formula I. The compounds of formula I are potent antibacterial agents or are of use as intermediates in the preparation of such antibacterial agents.
Type:
Grant
Filed:
August 19, 1976
Date of Patent:
January 10, 1978
Assignee:
Bristol-Myers Company
Inventors:
Marcel Menard, Gary M. F. Lim, Terry T. Conway
Abstract: Process for the manufacture of a heterocyclic compound of the formula I ##STR1## in which Y denotes a --CN, --COOR' or ##STR2## group, in which R' can be an optionally substituted alkyl or aryl radical and R" and R"' independently of one another can have the same meaning as R' or can be hydrogen or, conjointly with the nitrogen atom, can form a heterocyclic 5-membered or 6-membered ring and X denotes a --S-- or --O-- atom or a --NR"-- group and the ring A can carry non-ionic substituents or optionally substituted fused rings, wherein a nitrile of the formula IInc -- ch.sub.2 -- y (ii)is reacted, in organic solvents, with a lower alcohol of the formula IIIr -- oh (iii)using a molar ratio of nitrile to alcohol of 1:0.9 to 1:1.2, in the presence of an anhydrous strong acid at temperatures of -10.degree. to +40.degree.
Type:
Grant
Filed:
July 13, 1976
Date of Patent:
December 20, 1977
Assignee:
Ciba-Geigy AG
Inventors:
Peter Loew, Hansrudolf Schwander, Haukur Kristinsson
Abstract: N.sup.2 -alkoxynaphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis.