Abstract: Disclosed are esters of substituted 8-hydroxy-1-phenyl-2,3,4,5-tetrahydro-1-H-3-benzazepines represented by the general formula I ##STR1## wherein X is chloro, bromo or trifluoromethyl; R.sub.1 is alkyl, aralkyl, aryl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, cycloalkylalkyl, alkoxycarbonylalkyl, cycloalkyl, 1-adamantyl, cycloalkoxyalkyl, alkoxy, aralkoxy, cycloalkoxy or aryloxy; and the pharmaceutically acceptable acid addition salts thereof. The compounds show neuroleptic, antidepressive and antiaggressive activity.
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: There are disclosed herein certain substituted imidazo[1,2-b]pyridazine compounds which are useful in the treatment of peptic ulcer diseases.
Abstract: There is disclosed the antibacterial 5R,6S,8R-6-(1-hydroxyethyl)-2-(2-[methylaminocarbonyl]-ethylthio)-penem-3- carboxylic acid, its pharmaceutically acceptable salts and esters as well as compositions containing them and methods for their use.
Abstract: There are disclosed certain alkali metal, alkaline earth metal, amine and amino acid salts of 3-(n-butyl)-4-hydroxy-1-phenyl-1,8-naphthyridine-2(1H)-one which, unlike the parent compound, are useful for orally treating chronic obstructive lung diseases such as asthma, bronchitis and the like.
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: An electrically heated hair curler or roller suitable for use in, for example, a hair setter contains therein a self-regulating heater comprised of a positive temperature coefficient (PTC) thermistor material. The PTC is in the shape of a flat pill or disc. There are no holes in the PTC, thus enabling it to maintain its integrity under stress. There are two cup shaped heat sinks, the bottoms of which rest against the flat faces of the PTC in electrical and heat conducting contact therewith. The heat sinks are held firmly against the PTC element by electrically conductive rivets or other connectors through holes in the bottoms of the heat sinks and depressions in the circumference of the PTC. A male positive electrical contact pin extends down from the inside face of the bottom of the lower heat sink. A negative electrical contact ring is around the pin and separated therefrom by a plastic insulating sleeve.
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: Disclosed is an improved process for the synthesis of 6-bromo-17,21-dihydroxy-3,11,20-trioxo-1,4,-pregnadienes 17,21-diesters. In particular, this invention relates to the conversion of 17,21-dihydroxy-3,11,20-trioxo-1,4-pregnadienes 17,21-diesters to 6-borom-17,21-dihyroxy-3,11,20-trioxo-1,4-pregnadienes-17-21-diesters via bromination under ionic conditions, e.g. bromine in acetic acid.
Type:
Grant
Filed:
December 27, 1982
Date of Patent:
April 3, 1984
Assignee:
Schering Corporation
Inventors:
Elliot L. Shapiro, Lawrence E. Finkenor
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: There is disclosed the antibacterial 5R,6S,8R-2-(1-methyl-2-imidazolylmethylthio)-6-(1-hydroxyethyl)penem-3-car boxylic acid, its pharmaceutically acceptable salts and esters as well as compositions containing them and methods for their use.
Type:
Grant
Filed:
January 17, 1983
Date of Patent:
March 6, 1984
Assignee:
Schering Corporation
Inventors:
Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace