Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## wherein A represents C.sub.2 -C.sub.6 straight or branched chain alkylene group and R.sup.10 and R.sup.11 each independently represents optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, heterocyclyl, heterocyclyl-aliphatic, heteroaryl or heteroaraliphatic, or R.sup.10 and R.sup.11 taken together with the S.sup..sym. to which they are attached represent an optionally substituted sulfur-containing heterocyclic ring. Such derivatives are useful as potent antibacterial agents. Also disclosed are processes for the preparation of such derivatives.
Abstract: A novel antibiotic complex designated herein as BBM-1675 complex is produced by fermentation of certain novel strains of Actinomadura verrucosospora. The complex may be separated into two major components, BBM-1675 A.sub.1 and A.sub.2, and four minor components, BBM-1675 A.sub.3, A.sub.4, B.sub.1 and B.sub.2, and such components exhibit antimicrobial activity and also antitumor activity in certain mouse tumor systems.
Abstract: The dinalidixate and diphosphanilate salts of chlorhexidine possess antibacterial activity. They exhibit synergism as compared with comparable concentrations of chlorhexidine and the respective free acid. Synergistic compositions comprising a mixture of a chlorhexidine salt with phosphanilic acid or a salt of phosphanilic acid, or with nalidixic acid, or a salt of nalidixic acid are disclosed. Dermatological compositions of such novel salts, and all such mixtures, are provided.
Type:
Grant
Filed:
May 14, 1985
Date of Patent:
May 19, 1987
Assignee:
Bristol-Myers Company
Inventors:
Paul L. Warner, Jr., Grey B. Kornegay, George Redl
Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups; R.sup.5 represents either (a) an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical or (b) a divalent phenylene or C.sub.1 -C.sub.4 alkylene group joined to the ##STR2## ring so as to form a bridged polycyclic group; and ##STR3## represents a quaternized nitrogen-containing non-aromatic heterocycle. Such derivatives are useful as potent antibacterial agents.
Abstract: Novel carbapenem antibiotics are prepared in which the 2-substituent has the formula ##STR1## wherein n is 0, 1, 2, 3, m, is 1 or 2, and R is C.sub.1 -C.sub.6 alkyl, allyl, propargyl, carboxymethyl, cyanomethyl or aralkyl wherein the aryl moiety is phenyl or heteroaryl and the alkyl moiety is C.sub.1 -C.sub.6 alkyl, said heterocyclic ring containing the sulfonium group being optionally substituted at a ring carbon atom or atoms by one or two C.sub.1 -C.sub.6 alkyl groups.
Abstract: A label assembly includes machine readable indicia on the underside of the backing strip for verifying correspondence between identifying indicia on the label and the contents of a container before and/or during and/or after labeling of the container and is made by feeding a label layer/backing layer laminate web along a travel path and printing machine readable indicia on the underside of the backing layer and printing identifying indicia on the label layer.
Abstract: This invention relates to novel compositions of the antitumor agent [4'-9-(acridinylamino) methanesulfon-m-anisidide] (m-AMSA). The m-AMSA lactate salts in combination with Tween-80 provide a highly stable, ready to use aqueous product.
Abstract: A label assembly includes machine readable indicia on the underside of the backing strip for verifying correspondence between identifying indicia on the label and the contents of a container before and/or during and/or after labeling of the container and is made by feeding a label layer/backing layer laminate web along a travel path and printing machine readable indicia on the underside of the backing layer and printing identifying indicia on the label layer.
Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents a C.sub.1 -C.sub.6 straight or branched chain alkylene group; R.sup.5 represents an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radial and ##STR2## represents a nitrogen-containing aromatic heterocycle attached to the alkylene group A at a ring carbon atom and quaternized by substituent R.sup.5. Such derivatives are useful as potent antibacterial agents.
Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups and ##STR2## represents a quaternized nitrogen-containing aromatic heterocycle. Such derivatives are useful as potent antibacterial agents. Also disclosed are processes for the preparation of such derivatives and novel intermediates utilized in these processes.
Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups; R.sup.5 represents either (a) an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical or (b) a divalent phenylene or C.sub.1 -C.sub.4 alkylene group joined to the ##STR2## ring so as to form a bridged polycyclic group; and ##STR3## represents a quaternized nitrogen-containing non-aromatic heterocycle. Such derivatives are useful as potent antibacterial agents.
Abstract: There is disclosed a new crystalline form of 7-(dimethylaminomethylene)amino-9a-methoxymitosane having an infra-red spectrogram as disclosed in the drawing. This new crystalline form is characterized by substantially greater storage stability than amorphous 7-(dimethylaminomethylene)amino-9a-methoxymitosane.
Abstract: A novel stereocontrolled process is disclosed for converting 6-aminopenicillanic acid to an optically active azetidinone of the formula ##STR1## wherein R" is a hydroxy-protecting group by use of a 6,6-dihaloanhydropenicillin or 6,6-bis(phenylselenyl)anhydropenicillin intermediate.
Abstract: This invention relates to novel compositions of the antitumor agent [4'-9-(acridinylamino) methanesulfon-m-anisidide] (m-AMSA). The lactate salts of the m-AMSA composition in admixture with pyroglutamic acid provide a highly stable, highly water soluble product.
Abstract: Novel antitumor antibiotics designated herein as albacarcins M and V are produced by fermentation of Streptomyces albaduncas strain C-38291 (ATCC 39151). The new antibiotics possess antibacterial activity and also inhibit the growth of mammalian tumors such as P388 leukemia in mice.
Type:
Grant
Filed:
April 16, 1984
Date of Patent:
July 1, 1986
Assignee:
Bristol-Myers Company
Inventors:
James A. Matson, Robert W. Myllymaki, Terrence W. Doyle, James A. Bush
Abstract: A novel stereocontrolled process is disclosed for converting 6-aminopenicillanic acid to an optically active azetidinone of the formula ##STR1## wherein R" is a hydroxy-protecting group by use of a 6,6-dihaloanhydropenicillin or 6,6-bis(phenylselenyl)anhydropenicillin intermediate.
Abstract: Novel platinum(II) complexes of 1,2-diaminocyclohexane, 1-aminomethylcyclooctylamine and 1,2-diamino-2,4-dimethylpentane are provided. Such complexes are of use in inhibiting the growth of certain mammalian tumors.
Abstract: The compounds are of the class of 9-anilinoacridines, useful as antitumor agents and are analogs of m-AMSA. These compounds have the formula ##STR1## in which R.sup.1 is Br, Cl or CH.sub.3, and R.sup.2 is CH.sub.2 NHCH.sub.3, CH.sub.2 N(CHO)CH.sub.3 or CH.sub.2 NHCHO. Intermediate 3-substituted-9(10H)acridone-5-carboxylic acids are prepared by converting diphenylaminedicarboxylic acids via acyl chloride to dipiperidides, purifying the dipiperidides, treating said dipiperidides with phosphorous oxychloride in an inert organic solvent at a temperature in the range of about 70.degree. C. to 110.degree. C. to yield 9-acridine, subjecting said 9-acridine to mild acid hydroylsis to yield 9-acridone and thereafter hydroylzing said 9-acridones to the acid product.
Type:
Grant
Filed:
June 18, 1984
Date of Patent:
March 11, 1986
Assignee:
Bristol-Myers Company
Inventors:
Gerry Kavadias, Terrance W. Doyle, Elizabeth Janik, Richard A. Partyka
Abstract: This invention concerns novel water-soluble salts and compositions of the antitumor agent 4'-(9-acridinylamino) methanesulfon-m-anisidide (m-AMSA). More particularly, there are provided (1) the mono- and dipyroglutamate salts of m-AMSA and (2) compositions of m-AMSA with pyroglutamic acid. The novel salts and compositions provided enable m-AMSA to be administered as an aqueous solution without the necessity of using dimethylacetamide as a pharmaceutical vehicle.