Abstract: Provided is a process for preparation and/or purification of clavulanic acid or a pharmaceutically acceptable salt or ester thereof including removing solids from a clavulanic acid containing fermentation broth by microfiltration to form a first filtrate, further removing solids from the first filtrate by ultrafiltration to form a second filtrate, concentrating the second filtrate by removal of water, and treating the concentrated second filtrate to isolate clavulanic acid or a pharmaceutically acceptable salt or ester thereof.
Type:
Grant
Filed:
August 14, 2000
Date of Patent:
August 14, 2001
Assignee:
LEK Pharmaceutical and Chemical Co. D. D.
Abstract: Provided is a process for preparation and/or purification of clavulanic acid or a pharmaceutically acceptable salt or ester thereof including removing solids from a clavulanic acid containing fermentation broth by microfiltration to form a first filtrate, further removing solids from the first filtrate by ultrafiltration to form a second filtrate, concentrating the second filtrate by removal of water, and treating the concentrated second filtrate to isolate clavulanic acid or a pharmaceutically acceptable salt or ester thereof, characterized in that the first filtrate is filtered using an ultrafiltration membrane having a molecular weight cut-off of 10 to 30 kD and a permeate flow rate of 10 to 30 lm.sup.-2 h.sup.-1.
Abstract: The present invention provides a process for making a compound having a structure according to Formula (I) ##STR1## wherein A.sup.1, A.sup.2 and A.sup.3 are independently carbon or nitrogen and R.sup.1, R.sup.3, R.sup.4 and R.sup.6 are known quinolone substituents; and wherein one of R.sup.1, R.sup.3 or R.sup.6 may be a lactam-containing moiety;or a protected form, salt, pharmaceutically-acceptable salt, biohydrolyzable ester, or solvate thereof;the process comprising reacting one or more organosilicon compounds with a compound having a structure according to Formula (II) ##STR2## wherein A.sup.1, A.sup.2 and A.sup.3, R.sup.1, R.sup.3, R.sup.4 and R.sup.6 as described above; wherein one of R.sup.1, R.sup.3 or R.sup.6 may be a lactam-containing moiety; and X is a leaving group;or a protected form, salt, biohydrolyzable ester, or solvate thereof.
Type:
Grant
Filed:
November 14, 1996
Date of Patent:
December 30, 1997
Assignee:
The Procter & Gamble Company
Inventors:
Jared Lynn Randall, Jane Ellen Godlewski
Abstract: .beta.-Lactam derivatives and analogs are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
Type:
Grant
Filed:
July 16, 1987
Date of Patent:
January 10, 1989
Assignee:
Merck & Co., Inc.
Inventors:
Paul E. Finke, Morris Zimmerman, James B. Doherty, Bonnie M. Ashe, Conrad P. Dorn
Abstract: A compound having the formula (I): ##STR1## is described, together with salts thereof and an enzymatic process for converting such compounds into clavulanic acid.A process for the preparation of the compound of formula (I) and its salts is disclosed, together with intermediates for use therein. This process involves the use of a novel enzyme system to effect the desired cyclization, which enzyme system is preferably derived from a micro-organism, in particular a species of Streptomyces.
Type:
Grant
Filed:
August 27, 1986
Date of Patent:
January 3, 1989
Assignee:
Beecham Group plc
Inventors:
Stefan R. Woroniecki, Stephen W. Elson, Keith H. Baggaley
Abstract: A compound of formula I ##STR1## or a salt or ester thereof. Processes for the preparation of these compounds and the use of these compounds in the preparation of further bicyclic compounds are also disclosed.
Abstract: The compounds of the formula (II): ##STR1## or pharmaceutically acceptable salts or esters thereof wherein A is a hydrogen atom or an esterifying radical; X is an alkyl group of 1-12 carbon atoms optionally substituted by a hydroxy, amino, acylamino of C.sub.1-6 alkoxy group, which substituents are not on the carbon atom adjacent to the nitrogen atom; or a C.sub.5-7 cycloalkyl group; or a phenylalkyl group wherein the carbon atom content of the alkyl part is 1-6 and the phenyl part is optionally substituted with a fluorine, bromine, chlorine, C.sub.1-6 alkyl, or C.sub.1-6 alkoxy; with the proviso that when X represents an optionally substituted phenylalkyl group and A represents C.sub.1-3 alkyl, then the --CO.sub.2 A group is attached to the alkyl part of the phenylalkyl group; have been found to be .beta.-lactamase inhibitors and antibacterial agents. Their preparation and use is described.
Type:
Grant
Filed:
April 13, 1983
Date of Patent:
March 24, 1987
Assignee:
Beecham Group p.l.c.
Inventors:
Brian P. Clarke, John B. Harbridge, Irene Stirling
Abstract: A compound of formula I ##STR1## or a salt or ester thereof. Processes for the preparation of these compounds and the use of these compounds in the preparation of further bicyclic compounds are also disclosed.