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: New octapeptides having the formula X-R-Pro-His(benzyl)-His(benzyl)-R.sup.1 -Trp-D-Ala-Y wherein X is a protective group, R is Pro or Gln; R.sup.1 is Tyr(benzyl)-Ser(benzyl) or Ser(benzyl)-Pro and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino.
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: 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: Derivatives of amoxicillin having broad spectrum antibacterial activity are disclosed. In addition, the following methods for preparing the compounds are provided (a) reacting the free amino acid amoxicillin or the acid salt or silylated derivative thereof with a reactive derivative of 6-(4-pyridyl)-1,2-dihydro-2-oxonicotinic acid and (b) reacting the free amino acid 6-aminopenicillanic acid or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-(+)-N-(1,2-dihydro-2-oxonicotinyl)-2-(p-hydroyphenyl)glycine.
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 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: New hexapeptides having the formula X-Trp-His-(benzyl)-Ser(benzyl)-Tyr(benzyl)-Pro-Ala-Y wherein X is t-butoxycarbonyl or benzyloxycarbonyl and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino.
Abstract: New heptapeptides having the formula X-Ser(benzyl)-Tyr(benzyl)-Phe-Leu-Arg(R)-Pro-Gly-Y wherein X is a protective group, R is a protective group and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino.
Abstract: New hexapeptides having the formula X-Ser(benzyl)-Tyr(benzyl)-Ala-Leu-Arg-Pro-Y wherein X is t-butoxycarbonyl or benzyloxycarbonyl and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino.
Abstract: New heptapeptides having the formula X-R-His(benzyl)-His(benzyl)--R.sup.1 --R.sup.2 --Trp--Ala--Y wherein X is a protective group, R is Pro or Gln; R.sup.1 and R.sup.2 are Ser(benzyl) or Tyr(benzyl) and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)-amino.
Type:
Grant
Filed:
November 5, 1976
Date of Patent:
May 2, 1978
Assignee:
Parke, Davis & Company
Inventors:
Francis John Tinney, Ernest D. Nicolaides
Abstract: A method of producing a fluid absorbent web for the manufacture of disposable absorbent articles is provided, such as diapers, underpads, sanitary napkins or similar articles. The method includes the step of forming a uniform moving web of fiberized wood pulp having a central zone, applying hydrocolloid polymer particles onto the surface of the central zone, and distributing the applied particles into the body of the moving web by air pressure means. Apparatus for producing such articles is also provided featuring means for incorporating absorbent polymer particles within a central zone of a moving web of the matrix.
Abstract: New nonapeptides having the formula Prot Grp-R-Trp-Ser-Tyr-R.sub.2 -Leu-Arg-Pro-Gly-R.sub.3 ; salts thereof; wherein R is Gln, Gln (bzl), His (bzl), Ser (bzl), Pro, Leu, Tyr (bzl), Ile, Cys (bzl) or Phe, R.sub.2 is D-Phe, D-Ala, D-Leu, D-Trp, D-Tyr, D-Tyr (Me), D-Ser, D-Met, D-Arg, D-Val, D-His, D-Gln, D-Phs, D-Thr, D-Pro or D-Asn and R.sub.3 is NH.sub.2, NH(lower alkyl) or N-(lower alkyl).sub.2, methods for their production; certain peptide intermediates and their salts used in the production thereof; and the use of said nonapeptides as luteinizing hormone releasing factor antagonists.
Abstract: New hexapeptides having the formula X-R-Trp-His(benzyl)-Tyr(benzyl)-Ser(benzyl)-R.sup.1 -Ala-Y wherein X is t-butoxycarbonyl or benzyloxycarbonyl, R is a single bond, His, His(benzyl) or Gln; R.sup.1 is a single bond or Pro and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino with the proviso that the total number of amino acid units when R and R.sup.1 are combined is one.
Type:
Grant
Filed:
September 15, 1976
Date of Patent:
April 18, 1978
Assignee:
Parke, Davis & Company
Inventors:
Francis John Tinney, Ernest D. Nicolaides
Abstract: The present invention is concerned with improved dental semi-solid or paste-like elastomeric materials which have the capability of precise surface detail reproduction at ambient and body temperature. Such materials are prepared by treating liquid polysulfide with a synergistic accelerator system comprising a metallic peroxide, e.g., zinc peroxide, 2,2' dithiobisbenzothiazole and 2-mercaptobenzothiazole.
Abstract: The present invention relates to novel benzo(b)thiophene derivatives of the general formula: ##STR1## wherein Y represents a hydrogen or halogen atom; A represents a hydrogen atom or a phenyl group which may be substituted with a halogen atom or a lower alkoxy group; B represents a radical of the formula OR' or NR.sup.2 R.sup.3, wherein R' is an alkyl radical of 1 to 5 carbon atoms which may be substituted with hydroxy, lower alkoxy, phenyl or phenoxy groups or a cycloalkyl or phenyl group which may be substituted by lower alkoxy or halogen atoms; R.sup.2 and R.sup.3, which may be identical or different, represent, if identical, hydrogen, alkyl radicals of 1 to 5 carbon atoms which may be substituted by hydroxy, lower alkoxy, phenoxy, di-lower alkylamino, or phenyl groups; or, if R.sup.2 is hydrogen, R.sup.
Type:
Grant
Filed:
April 8, 1977
Date of Patent:
April 4, 1978
Assignee:
Warner-Lambert Company
Inventors:
Peter Johannes Stoss, Manfred Franz Reinhold Herrmann, Gerhard Satzinger
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