Abstract: 7.beta.-[2-Amino-2-(benzothien-4,5,6, and 7-yl)acetylamino]-3-substituted-3-cepham-4-carboxylic acids and 7.beta.-[2-amino-2-(2,3-dihydrobenzothien-4,5,6, and 7 yl)acetylamino]-3H- or 3-substituted-3-cephem-4-carboxylic acids (1), e.g. 7.beta.-[2-amino-2-(benzothien-4-yl)acetylamino]-3-methyl-3-cephem-4-carbo xylic acid, are orally effective antibiotics. Also provided are benzothienyl oximino compounds, the corresponding 2,3-dihydro compounds (2) useful as intermediates to (1) and as antibiotics, as well as 7.beta.-(2,2-dialkyl-5-oxo-4-benzothienyl-1-imidazolidinyl)-3H-(3-substitu ted)-3-cephem-4-carboxylic acids and the corresponding 2,3-dihydro compounds (3) useful as antibiotics, and prepared with (1) by condensation with ketones. Pharmaceutical formulations of antibiotic compounds (1), (2), and (3) are provided.
Abstract: Cephalosporins of the formula ##STR1## wherein R is hydrogen, sodium, potassium or certain ester groups; R.sub.1 is in the .alpha.-configuration and is hydrogen or methoxy; R.sub.2 is hydrogen, ##STR2## X is hydrogen, ##STR3## R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl, ##STR4## --(CH.sub.2).sub.n --N--(lower alkyl).sub.2 ; R.sub.6 is hydrogen, sodium, or potassium; n is an integer from 1 to 4; are disclosed. These compounds are useful as anti-bacterial agents.
Type:
Grant
Filed:
March 12, 1984
Date of Patent:
February 26, 1985
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Hermann Breuer, Uwe D. Treuner, Theodor Denzel
Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently lower alkyl having from 1 to 4 carbon atoms; and R.sup.3 is lower alkyl having from 1 to 6 carbon atoms, lower cycloalkyl having from 3 to 6 carbon atoms optionally substituted with methyl or ethyl, lower alkoxyalkyl having up to a total of 8 carbon atoms or lower alkylthioalkyl having up to a total of 8 carbon atoms are insecticidal.
Abstract: In the synthesis of calcium leucovorin (calcium 5-formyl-5,6,7,8-tetrahydrofolate), the use of an amine base in the conversion of anhydroleucovorin (5,10-methenyl-5,6,7,8-tetrahydrofolic acid) to leucovorin unexpectedly results in a pure (USP) product directly from the reaction mixture.
Type:
Grant
Filed:
December 22, 1980
Date of Patent:
February 19, 1985
Assignee:
Burroughs Wellcome Co.
Inventors:
James C. Wisowaty, Roy A. Swaringen, David A. Yeowell
Abstract: This invention relates to novel compounds useful as intermediates in the preparation of cephalosporin compounds of antibacterial activity, having the formula ##STR1## wherein R.sup.1 is a group of the formula ##STR2## in which X is sulfur, oxygen or substituted or unsubstituted imino, andR.sup.2 is hydrogen or a saturated or unsaturated aliphatic hydrocarbon residue,a derivative at the carboxy group thereof and salt thereof.
Abstract: Highly active substantially pure Z-isomers of cephalosporins are produced by the following synthesis: ##STR1## in which R.sup.1, R.sup.4 and R.sup.5 ae various organic radicals,R.sup.2 is alkoxycarbonyl,Y is Cl, Br or --O--SO.sub.2 --R.sup.5, andX is a conventional cephalosporin substituent.Many of the intermediates are new, especially in pure Z-form.
Abstract: Compounds of the formula: ##STR1## wherein X is oxygen or sulfur; R.sup.1 and R.sup.2 are independently lower alkyl having from 1 to 4 carbon atoms; and R.sup.3 is lower alkyl having from 1 to 6 carbon atoms, lower cycloalkyl having from 3 to 6 carbon atoms optionally substituted with methyl or ethyl, lower alkoxyalkyl having up to a total of 8 carbon atoms or lower alkylthioalkyl having up to a total of 8 carbon atoms are insecticidal.
Abstract: This invention relates to novel cephem compounds, of antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 is carboxy (C.sub.1 -C.sub.6) alkyl or esterified carboxy (C.sub.1 -C.sub.6) alkyl,R.sup.2 is carboxy or an esterified carboxy group, andR.sup.3 is (C.sub.1 -C.sub.6) alkanoylamino, (C.sub.1 -C.sub.6) alkanesulfonyl, triazolylthio, tetrazolylthio having (C.sub.1 -C.sub.6) alkyl, pyridazinylthio having (C.sub.1 -C.sub.6) alkyl, thiadiazolylthio having (C.sub.1 -C.sub.6) alkyl, triazolopyridazinylthio or tetrazolopyridazinylthio, and pharmaceutically acceptable salts thereof.
Abstract: Disclosed are 2-(pyridinyl)-1,2,4-triazolo[1,5-a]pyrimidines and derivatives which are effective in increasing cardiac contractility. These compounds are useful in the treatment of congestive heart failure preferably by oral or parenteral administration.
Abstract: Cephalosporin derivatives of the formula: ##STR1## wherein R.sub.1 is methyl or ethyl and R.sub.2 is a straight-chain or branched alkyl group of 5 to 7 carbon atoms, and their pharmaceutically acceptable salts, which are effective as orally administrable antibiotic agents against both gram-positive- and negative-bacteria, and the production and compositions thereof, are proposed.
Abstract: A 1-(N-substituted carbamoyl)-5-fluorouracil derivative represented by the following general formula: ##STR1## R is a 4-alkoxycyclohexyl group-containing radical which is 2,3,4-trimethoxycyclohexcylethyl, 2,3,4-trimethoxycyclohexyl, 2,4-dimethoxycyclohexylmethyl, 3,4-dimethoxycyclohexylethyl, 2,4-dimethoxycyclohexyl, 2,4,5-trimethoxycyclohexyl, 3,4-dimethoxycyclohexylmethyl, 3,4,5-trimethoxycyclohexyl, 4-ethoxycyclohexyl or 4-ethoxycyclohexylmethyl. The compounds are carcinostatic agents. The compounds are used in a therapeutically effective amount in the presence of a carrier.
Abstract: A novel process for the preparation of thioethers comprising reacting a silylated thiol of the formulaR--S--SiR.sub.1 R.sub.2 R.sub.3 Iwherein R is an organic group and R.sub.1, R.sub.2 and R.sub.3 are individually selected from the group consisting of alkyl of 1 to 4 carbon atoms with an organic halide, sulfate or sulfonate in the presence of hexamethylphosphoric triamide as a solvent or co-solvent preferably under neutral conditions in aprotic solvents at a temperature between 0.degree. and 150.degree. C.
Type:
Grant
Filed:
March 7, 1983
Date of Patent:
January 29, 1985
Assignee:
Gist-Brocades N.V.
Inventors:
Cornelis A. Bruynes, Theodorus K. Jurriens
Abstract: The invention relates to complex salts of N-cyclohexyl-piperazino-acetamides or propionamides with dihydroxy aluminum-.alpha.-hydroxy-carboxylates, a process for preparing them and the use thereof as antiulcer-antisecretive-buffering drugs.
Abstract: Preparation of pharmaceutical composition comprising, treatment of human and animal diseases with, and compound of, 3,7-disubstituted-3-cephem-4-carboxylic acid.
Abstract: A cephalosporin derivative of the formula: ##STR1## in which R.sup.0 is a hydrogen atom or a methyl radical, R.sup.1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art; R.sup.2 is any one of the C-4 substituents from antibacterially-active cephalosporins known in the art; R.sup.3 is a hydrogen atom or a 1-6C alkoxy or 1-6C alkylthio radical; X.sup.1 is a sulphur or oxygen atom, a CH.sub.2 radical or a radical of the formula NR.sup.7 in which R.sup.7 is a hydrogen atom, a 1-6C alkyl, formyl or benzyl radical; X.sup.2 is a nitrogen atom or a radical of the formula N.sup..sym. -R.sup.7 ; R.sup.4 and R.sup.7, and R.sup.5 and R.sup.6 are a variety of substituents which are described in the specification; and the pharmaceutically-acceptable acid- or base-addition salts thereof. Pharmaceutical compositions, manufacturing processes and intermediates are also described.
Type:
Grant
Filed:
December 22, 1981
Date of Patent:
January 8, 1985
Assignees:
Imperial Chemical Industries PLC, ICI Pharma
Abstract: A process for preparing a 4-amino-5-dialkoxymethylpyrimidine derivative of the formula: ##STR1## which comprises reacting a propanenitrile derivative represented by the formula (I) or the novel compound represented by formula (II): ##STR2## with an amidine of the formula: ##STR3## wherein R.sup.1 to R.sup.6 are as defined in the specification. Also disclosed is a process for making the novel compounds of formula (II).
Abstract: These are described compounds of formula (I) ##STR1## or an acid addition salt thereof; in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, halogen, C.sub.1-4 haloalkyl, nitro, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio or phenylsulphonyl; in which R.sup.5 is a group of the formula ##STR2## where R.sup.7 is hydrogen or C.sub.1-6 alkyl, R.sup.8 is hydrogen or C.sub.1-4 alkyl and n is 0 or 1, provided that when R.sup.7 is hydrogen n is 0; and in which R.sup.6 is attached to the 1, 2 or 3 position of the triazole ring and is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, phenyl, benzyl or acyl. These compounds are pharmaceutically active and are especially useful in the treatment of disorders of the central nervous system. They are prepared by reacting an amine of formula R.sup.
Type:
Grant
Filed:
October 13, 1983
Date of Patent:
January 8, 1985
Assignee:
Lilly Industries Limited
Inventors:
Jiban K. Chakrabarti, Terrence M. Hotten, David J. Steggles