Abstract: 4'-Deoxyvincristine, 4'-deoxy-1-formylleurosidine and the corresponding 4-desacetyl derivatives, useful in inhibiting the growth of experimental tumors.
Abstract: Carbamoylalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene of 1 to 6 carbons; R.sub.2 and R.sub.3 are independently selected from hydrogen and straight chain alkyl of 1 to 4 carbons, or R.sub.2 is hydrogen and R.sub.3 is branched chain alkyl of 3 or 4 carbons, phenyl, benzyl or phenethyl, or R.sub.2 and R.sub.3 taken together with N atom to which they are attached form ##STR3## R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.6 is hydrogen or lower alkyl; R.sub.7 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR4## or certain heterothio groups; are disclosed.
Abstract: A new compound with a nucleus containing a benzo-fused carbocyclic .beta.-lactam system is disclosed. The compound has antibacterial activity against B. subtilis.
Abstract: A series of 5-endo-(quinoline-carbonyloxy)-,(benzothiophene-carbonyloxy)- and (quinoxaline-carbonyloxy)-N[amino-(lower)alkyl]bicyclo[2.2.1]-heptane-2,3- di-endo-carboxylic acid imides has been found to possess excellent prophylactic and therapeutic activity as anti-arrhythmic agents.
Type:
Grant
Filed:
August 19, 1976
Date of Patent:
February 13, 1979
Assignee:
Bristol-Myers Company
Inventors:
Ronald L. Buchanan, John T. Woolever, Alex M. Jelenevsky
Abstract: 7-[D-.alpha.-(4-hydroxy-1,5-naphthyridine-3-carboxyamido)-.alpha.-phenyl (and p-hydroxyphenyl) acetamido]-3-carbamoyloxymethyl-3-cephem-4-carboxylic acids were synthesized and found to have potent antibacterial activity in vitro especially against many strains of Pseudomonas aeruginosa.
Type:
Grant
Filed:
June 9, 1977
Date of Patent:
February 6, 1979
Assignee:
Bristol-Myers Company
Inventors:
Takayuki Naito, Jun Okumura, Masahisa Oka
Abstract: Novel 1,2-dihydro-2-oxoquinol-4-ylalkanoic acid derivatives bearing a variety of substituents on the quinoline nucleus but including, at position 1, an aromatic radical linked directly or through a C.sub.1-4 -alkylene or a C.sub.2-4 -alkenylene radical. Representative compounds of the invention are 1-(3,4-dichlorobenzyl)-3-methyl-1,2-dihydro-2-oxoquinol-4-ylacetic acid and .alpha.-(1-benzyl-1,2-dihydro-2-oxoquinol-4-yl)propionic acid. The compounds possess anti-inflammatory or analgesic properties, or are inhibitors of the enzyme aldose reductase.
Type:
Grant
Filed:
September 12, 1977
Date of Patent:
February 6, 1979
Assignee:
Imperial Chemical Industries Limited
Inventors:
David R. Brittain, Edward D. Brown, Walter Hepworth, Gilbert J. Stacey
Abstract: 2-Keto-6,7,8,9-tetrahydro-2H-pyrano(3,2-g)-quinoline and 2-keto-9-methyl-,8,9-tetrahydro-2H-pyrano(3,2-g)-quinoline, compounds useful as laser dyes, are prepared from 7-hydroxy-1,2,3,4-tetrahydroquinoline.
Type:
Grant
Filed:
March 29, 1976
Date of Patent:
February 6, 1979
Assignee:
The United States of America as represented by the Secretary of the Navy
Inventors:
Peter R. Hammond, Erhard J. Schimitschek, John A. Trias
Abstract: Novel organic amide compounds which are N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
Type:
Grant
Filed:
October 27, 1977
Date of Patent:
January 30, 1979
Assignee:
Warner-Lambert
Inventors:
James S. Kaltenbronn, Theodore H. Haskell, Leonard Doub
Abstract: A series of novel 7-(D-.alpha.-acylaminoarylacetamido)-.DELTA..sup.3 -cephem derivatives have been prepared wherein the acyl moiety contains an epoxy group immediately adjacent to the carbonyl carbon atom. These compounds are useful as antibacterial agents for the treatment of diseases caused by Gram-negative and Gram-positive bacteria. Preferred members include 7-[D-.alpha.-(cis-2-carboxyoxiran-3-carboxamido)phenylacetamido]-3-(1-meth yl-1,2,3,4-tetrazol-5-ylthiomethyl)-.alpha..sup.3 -cephem-4-carboxylic acid and 7-[D-.alpha.-(cis-2-carboxyoxiran-3-carboxamido)phenylacetamido]cephalospo ranic acid. Alternate methods of preparation are provided for these compounds and the principal synthetic route is described in detail.
Abstract: Cyclic nitrile carbonate-containing compounds having the structural formula: ##STR1## wherein T is O, S, or NR"'; R and R' are organic radicals; R" is hydrogen, halogen or an organic radical and R"' is hydrogen or an organic radical are prepared by reacting a cyclic nitrile carbonate-containing chloroformate having the structural formula: ##STR2## with a nucleophilic compound having the structural formula: ##STR3## wherein T, R, R', R" and R"' are as defined above, under conditions such that the TH group will react with the chloroformate group, but no reaction will occur involving either the cyclic nitrile carbonate group or the ##STR4## group. The novel compounds of the invention are useful in the preparation of crosslinkable polymers.
Abstract: Cephalosporin compounds substituted in the 7-position with a hydroxy-halo substituted .alpha.-aminophenylacetamido group and in the 3-position with a heterocyclicthiomethyl group are prepared by 7-acylation. The products are antibacterial agents.
Abstract: Novel 7.alpha.-methoxy-cephalosporins and non-toxic salts thereof, which contain a di-oxo-piperazinylcarbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds.
Abstract: Cyanoalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene or ##STR3## R.sub.2 is phenyl, 2-thienyl, or 3-thienyl; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.5 is hydrogen or lower alkyl; R.sub.6 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR4## or certain heterothio groups; are disclosed. These compounds are useful as antibacterial agents.
Abstract: A novel ester of 7-acylamido-3-methyl-cepham-4-carboxylic acid derivative and a process for the preparation thereof which comprises reacting penicillin sulfoxide ester with the metal halide, and a novel 7-acylamido-3-methyl-cepham-4-carboxylic acid derivative and a process for the preparation thereof which comprises reacting penicillin sulfoxide ester with the metal halide and decomposing the resultant in a reductive atmosphere.
Abstract: Compounds of the formula: ##STR1## wherein the symbols X each represent hydrogen or methoxy, R represents hydrogen or carboxymethyl, the symbols R.sub.1 each represent hydrogen or together represent a valency bond and the symbols R.sub.2 each represent hydrogen or together represent a valency bond, the pair of symbols R.sub.2 having the same significance as the pair of symbols R.sub.1, and when the symbols R.sub.1 and R.sub.2 represent hydrogen the symbol X also represents hydrogen, are new compounds possessing antiviral activity.
Type:
Grant
Filed:
May 18, 1977
Date of Patent:
December 5, 1978
Assignee:
Rhone-Poulenc Industries
Inventors:
Jean-Louis Fabre, Daniel Farge, Claude James
Abstract: This invention relates to novel amides of 4-hydroxy-6H-thieno[2,3-b]thiopyran-5-carboxylic acid-7,7-dioxide having the Formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl; R.sub.2 is hydrogen, lower alkyl or aryl; Ar is aryl or heterocyclic; to the pharmaceutically acceptable salts thereof; and to processes for their preparation. The compounds of this invention exhibit antiinflammatory activity.
Type:
Grant
Filed:
December 27, 1977
Date of Patent:
November 28, 1978
Assignee:
Warner-Lambert Company
Inventors:
Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes
Abstract: N-Propylnorapomorphine dialkanoate, dibenzoate and dicyclopropanecarboxylate esters and acid-addition salts thereof, having anti-parkinson activity, are prepared by reaction of N-propylnorapomorphine with a respective alkanoyl, benzoyl or cyclopropanecarbonyl halide or corresponding acid anhydride in the presence of an acid acceptor.
Abstract: Novel chemical compounds of the formula: ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, phenyl, alkali metal, or an amine cation;X and Y can be the same or different and are selected from the group consisting of hydrogen, alkyl or from one to six carbon atoms, inclusive, cycloalkyl of 5 or 6 carbon atoms, inclusive, phenyl, hydroxyl, alkoxy having from one to three carbon atoms, inclusive, halogen, trifluoromethyl, cyano, carboxyamide and ##STR2## where Q is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, alkali metal, and an amine cation, with the proviso that whereR is hydrogen, alkali metal or an amine cation, then Q is the same as R, and whereR is phenyl or alkyl from one to three carbon atoms, then Q is phenyl or alkyl from one to three carbon atoms; andZ is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, and phenyl.
Type:
Grant
Filed:
August 5, 1976
Date of Patent:
November 21, 1978
Assignee:
The Upjohn Company
Inventors:
Charles M. Hall, Herbert G. Johnson, John B. Wright