Abstract: Disclosed are 6-(1'-hydroxyethyl)-2-[(1'R)-1'-aminoalkyl]penem-3-carboxylic acids and salts and esters thereof. The compounds are useful and potent antibacterial agents and can be formulated into a variety of forms suitable for oral, parenteral or topical use.
Abstract: Compounds of the formula ##STR1## wherein R is alkyl having 1 to 4 carbon atoms, one of Y and Z is a heterocyclic moiety, and the other of Y and Z is hydrogen, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms are useful as anthelmintics.
Abstract: Disclosed are 5,6-dihydro benzo[f]quinolines and derivatives which are effective in increasing cardiac contractility. These compounds are useful in the treatment of congestive heart failure.
Type:
Grant
Filed:
August 26, 1982
Date of Patent:
April 16, 1985
Assignee:
Schering Corporation
Inventors:
Elizabeth M. Smith, Ronald J. Doll, Bernard R. Neustadt
Abstract: Disclosed are triazolyl-substituted propane derivatives useful in the treatment of fungal diseases of humans and animals. Also disclosed are the processes for preparing the compounds, pharmaceutical compositions containing them, and the method of treating fungal diseases with said compounds.
Abstract: Disclosed are tricyclic lactams and derivatives which are effective in increasing cardiac contractility in humans. These compounds are useful in the treatment of congestive heart failure.
Type:
Grant
Filed:
June 16, 1983
Date of Patent:
October 2, 1984
Assignee:
Schering Corporation
Inventors:
Elizabeth M. Smith, Ronald J. Doll, Bernard R. Neustadt
Abstract: This invention relates to novel 3,20-dioxo-1,4-pregnadiene-17.alpha.-ol 17-aromatic heterocyclic carboxylates, to pharmaceutical formulations thereof, and their use in the treatment and control of inflammatory conditions.
Abstract: 3-Aralkyloxy-2,3-dihydro-2-(triazolylmethyl)benzo(b)thiophenes and related derivatives having antifungal, antibacterial, and antiprotozoal activity are prepared by the reaction of the corresponding 2,3-dihydro-3-hydroxy-2-(triazolylmethyl)benzo(b)thiophene or related derivative and an aralkyl halide.Preferred compounds are those where the aralkyl function is a hetercyclic aromatic, particularly 2-chloro-3-thenyl, and where the benzene nucleus is substituted by chlorine or fluorine.Pharmaceutical formulations comprising compounds of this invention are described, as well as the method for their use in treating microbial infections.
Type:
Grant
Filed:
July 29, 1982
Date of Patent:
August 28, 1984
Assignee:
Schering Corporation
Inventors:
Dinanath F. Rane, John J. Wright, Russell E. Pike
Abstract: 6-Substituted-hydrocarbon-2-(amino acid-thio)penem-3-carboxylic acids and congeners having useful antibacterial activity are disclosed. The compounds are prepared in a reaction sequence starting with a 4-acyloxy-2-azetidinone.
Abstract: There is disclosed a process for preparing 6-hydroxyethyl-2-alkylthio penem-3-carboxylates by a multi-step process comprising reacting an azetidinone having a protected hydroxy group at the 5 position with a diester of ketomalonic acid, chlorinating the resulting N-substituted azetidinone, removing the chlorine and OH protecting group, reacting the resulting compound with a silver salt to form a silver thio substituted at the 4 position of the azetidinone, cyclizing with a thiocarbonyl compound, then reacting the resulting penam with a fluoride to form a penam-penem tautomer, reacting the tautomer with a halide or ethylenically unsaturated compound followed by deprotecting the carboxyl at the 3 position to form the final penem product in high yield.
Type:
Grant
Filed:
March 30, 1982
Date of Patent:
April 17, 1984
Assignee:
Schering Corporation
Inventors:
Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace
Abstract: The novel antibiotic complex designated hazymicin consisting of eight components, is produced by a novel strain of Micromonospora herein designated Micromonospora echinospora var. challisensis SCC 1411. Also disclosed are the structures of the two components namely, Component 5 and Component 6.
Type:
Grant
Filed:
October 6, 1980
Date of Patent:
April 3, 1984
Assignee:
Schering Corporation
Inventors:
Jay A. Waitz, Joseph A. Marquez, Mahesh G. Patel, Ann C. Horan
Abstract: There are disclosed novel 23-demycinosyltylosin and derivatives thereof which have improved activity as antibiotics. Methods of preparation of the compounds are also disclosed.
Type:
Grant
Filed:
June 30, 1982
Date of Patent:
March 13, 1984
Assignee:
Schering Corporation
Inventors:
Ashit K. Ganguly, Yi-Tsung Liu, Alan K. Mallams
Abstract: Compounds of the formula ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. The compounds are useful as anthelmintics.
Abstract: There are disclosed 20-imino-20-deoxo-4"-acyl derivatives of the antibiotic tylosin which have higher serum levels and better absorption than the parent tylosins. Methods of preparation of the compounds are also disclosed.
Type:
Grant
Filed:
June 10, 1982
Date of Patent:
March 6, 1984
Assignee:
Schering Corporation
Inventors:
Ashit K. Ganguly, Allan K. Mallams, Yi-Tsung Liu
Abstract: This invention relates to 2,3-dihydro-2-(imidazolylmethyl)benzo(b)thiophenes, to intermediates useful in their preparation, and to processes for preparing said intermediates. Also included in the invention are pharmaceutical compositions and the method of use of the compounds as antifungal agents.
Type:
Grant
Filed:
March 3, 1982
Date of Patent:
February 14, 1984
Assignee:
Schering Corporation
Inventors:
Dinanath F. Rane, John J. Wright, Russell E. Pike
Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from hydrogen or lower alkyl; n is 1 or 0; A and B taken together with the carbons to which they are attached form an alkylene ring having six carbon atoms or A and B are hydrogen; and Z is ##STR2## The compounds are useful as hypertensive agents.
Type:
Grant
Filed:
March 8, 1982
Date of Patent:
February 14, 1984
Assignee:
Schering Corporation
Inventors:
Elizabeth M. Smith, Joseph T. Witkowski