Abstract: Prostaglandin analogues of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, R.sup.1 represents a straight- or branched-chain alkyl group containing from 4 to 10 carbon atoms, and R.sup.2 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms and cyclodextrin clathrates of such acids and esters and, when R.sup.2 represents a hydrogen atom, non-toxic salts thereof, the bonds attaching the epidithio radical to the carbon atoms in the 9- and 11-positions in the grouping of formula VA being either botn in .alpha.-configuration or both in .beta.-configuration are disclosed.These compounds exhibit characteristic prostaglandin properties.
Abstract: The present invention is concerned with novel tricyclic sulphoximides and with the preparation thereof. This family of compounds has been found to possess antihistaminic, antitussive, antiinflammatory, sedative, and diuretic properties.
Type:
Grant
Filed:
August 31, 1976
Date of Patent:
August 29, 1978
Assignee:
Warner-Lambert Company
Inventors:
Peter Stoss, Gerhard Satzinger, Manfred Herrmann
Abstract: The present invention relates to 1-nor-2-amino carbamates derived from the antibiotic substance, designated acid S, produced by Polyangium cellulosum var. fulvum (ATCC No. 25532), and to processes for their production. The 1-nor-2-amino carbamates of acid S of this invention are useful as antifungal agents.
Type:
Grant
Filed:
February 4, 1977
Date of Patent:
August 15, 1978
Assignee:
Warner-Lambert Company
Inventors:
David T. Connor, Samuel M. Ringel, Maximilian VON Strandtmann
Abstract: 1-Substituted-2-(2-pyridinyl)ethanone N-oxides having the formula I or II: ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 and R.sub.3 are each hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, or benzyloxy; R.sub.4 is halogen, hydroxy, lower alkyl, lower alkoxy, benzyloxy, ortho-amino, ortho-lower alkylamino, ortho-alkanoylamino or ortho benzoylamino; and R.sub.5 is hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or benzyloxy; the pharmaceutically acceptable acid addition salts thereof, and a process for the preparation thereof, are described. The compounds of this invention are useful for the treatment of allergic conditions and for the treatment of hyperacidity.
Type:
Grant
Filed:
August 16, 1977
Date of Patent:
August 1, 1978
Assignee:
Warner-Lambert Company
Inventors:
David T. Connor, Patricia A. Young, Maximilian VON Strandtmann
Abstract: This invention relates to novel compounds of the pyrido-[2,1-b]quinazolin-one series and their methods of preparation. These compounds have utility as antiallergy agents.
Abstract: The present invention is concerned with new dibenzylglycolic acid derivatives and with the preparation thereof. These derivatives show an extraordinary anti-hypertensive and antisecretory profile.
Type:
Grant
Filed:
March 15, 1977
Date of Patent:
August 1, 1978
Assignee:
Warner-Lambert Company
Inventors:
Wolf-Dieter Vigelius, Gerhard Satzinger, Manfred Herrmann
Abstract: The present invention relates to aldehyde, oxime and phenylhydrazone derivatives of the novel antibiotic substance, acid S, produced by the organism Polyangium cellulosum var. fulvum (ATCC No. 25532) and to processes for their preparation. The aldehyde, oxime and phenylhydrazone derivatives of acid S of this invention are useful as antifungal agents.
Type:
Grant
Filed:
February 4, 1977
Date of Patent:
July 4, 1978
Assignee:
Warner-Lambert Company
Inventors:
David T. Connor, Samuel M. Ringel, Maximillian Von Strandtmann
Abstract: Novel 3-formylchromone derivatives are disclosed, substituted on the 5,6,7, or 8 positions by one or more of the following substituents: halogen, hydroxy, lower alkyl, lower alkoxy, lower acyl, lower acyloxy, or methylenedioxy. The corresponding 3-acetal or 3-hydrazone derivatives of the carboxaldehyde group are also disclosed. These compounds, and pharmaceutical compositions containing these compounds are useful for the treatment of allergic conditions and for the treatment of hyperacidity.
Type:
Grant
Filed:
June 19, 1974
Date of Patent:
July 4, 1978
Assignee:
Warner-Lambert Company
Inventors:
Sylvester Klutchko, Daniel Kaminsky, deceased, Maximilian VON Strandtmann
Abstract: This invention relates to 5,6-dihydro-4-oxo-4H-thieno[2,3-b]thiopyran-5-carboxamides of the Formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl; R.sub.2 is hydrogen, lower alkyl or aryl; and Ar is aryl or heterocyclic; their pharmaceutically acceptable salts and to processes for their preparation. The compounds of this invention exhibit antibacterial, antifungal and antiallergy activity.
Type:
Grant
Filed:
December 7, 1977
Date of Patent:
July 4, 1978
Assignee:
Warner-Lambert Company
Inventors:
Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes
Abstract: This invention relates to 5,6-dihydro-4-oxo-4H-thieno?2,3-b!thiopyran-5-carboxamides of the Formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl; R.sub.2 is hydrogen, lower alkyl or aryl; and Ar is aryl or heterocyclic; their pharmaceutically acceptable salts and to processes for their preparation. The compounds of this invention exhibit antibacterial, antifungal and antiallergy activity.
Type:
Grant
Filed:
December 7, 1977
Date of Patent:
June 27, 1978
Assignee:
Warner-Lambert Company
Inventors:
Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes
Abstract: This invention relates to 5,6-dihydro-4-oxo-4H-thieno[2,3-b]thiopyran-5-carboxamides of the Formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl; R.sub.2 is hydrogen, lower alkyl or aryl; and Ar is aryl or heterocyclic; their pharmaceutically acceptable salts and to processes for their preparation. The compounds of this invention exhibit antibacterial, antifungal and antiallergy activity.
Type:
Grant
Filed:
December 10, 1976
Date of Patent:
May 30, 1978
Assignee:
Warner-Lambert Company
Inventors:
Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes
Abstract: This invention relates to novel indolothiopyrones having the formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl or aryl; R.sub.2 is hydrogen or halogen; and R.sub.7 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, nitro-substituted-aryl, or .omega.-substituted lower alkyl wherein the substituent is: ##STR2## wherein R.sub.4 and R.sub.5 each represent hydrogen, lower alkyl, or together with the nitrogen atom, form a heterocyclic ring; and R.sub.6 is lower alkoxy or amino, and novel intermediates used in their preparation. The indolothiopyrones are prepared by reacting a 3-mercaptoindole with sodium propiolate or a substituted sodium propiolate followed by acidification to obtain an intermediate acid; the intermediate acid cyclizes in the presence of an acid catalyst to obtain the indolothiopyrone structure which may be additionally subjected to halogenation, alkylation or hydrolysis to obtain derivatives having the various substituent groups disclosed.
Abstract: The present invention is concerned with 11-oxo-1-benzoxepino[4,3-c]pyridines of Formula I: ##STR1## wherein R.sub.1 and R.sub.2 may be hydrogen, lower alkyl, cyano, carboxamido, carboxy, ethoxycarbonyl or tetrazolyl and R.sub.3 may be hydrogen, lower alkyl, halogen, hydroxy or lower alkoxy.These compounds are indicated in the management of allergic conditions such as bronchial asthma, hay fever and the like.
Type:
Grant
Filed:
February 14, 1977
Date of Patent:
May 30, 1978
Assignee:
Warner-Lambert Company
Inventors:
Sylvester Klutchko, Max VON Strandtmann
Abstract: The present invention relates to 15-cycloalkyl-prostaglandins of the formula: ##STR1## WHEREIN A represents a grouping of the formula: ##STR2## W represents ethylene or trans-vinylene, X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, R represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R.sup.1 represents a hydrogen atom or a methyl or ethyl group, R.sup.2 represents a straight- or branched-chain alkyl group containing from 2 to 8 carbon atoms or a phenyl group unsubstituted or substituted by an alkyl group containing from 1 to 3 carbon atoms, R.sup.3 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 3 carbon atoms, and n represents 4 or 5) and cyclodextrin clathrates of such acids and esters and, when R represents a hydrogen atom, non-toxic salts thereof.These new compounds exhibit characteristic prostaglandin-like activities.
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 10, 1976
Date of Patent:
April 4, 1978
Assignee:
Warner-Lambert Company
Inventors:
Jagadish C. Sircar, Stephen J. Kesten, Harold Zinnes