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.This is a division of application Ser. No. 611,282 filed Sept. 8, 1975.
Type:
Grant
Filed:
January 25, 1977
Date of Patent:
February 28, 1978
Assignee:
Warner-Lambert Company
Inventors:
David T. Connor, Patricia A. Young, Maximilian VON Strandtmann
Abstract: The present invention relates to compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen, halogen, hydroxy, lower alkoxy or lower alkyl, R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen or lower alkyl.These compounds, including their corresponding pharmaceutically acceptable salts, are useful in the management of allergic conditions such as hay fever and as a prophylactic in the treatment of bronchial asthma.
Type:
Grant
Filed:
August 2, 1976
Date of Patent:
February 28, 1978
Assignee:
Warner-Lambert Company
Inventors:
David T. Connor, Patricia A. Young, Max VON Strandtmann
Abstract: Substituted 3-(2-pyridinyl)-4(1H)-quinolinone N-oxides having the formula I: ##STR1## wherein R.sub.1 is hydrogen, halogen, lower alkyl, hydroxy or alkoxy; R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen or --CH.sub.2 OH; the dotted line indicates the possible presence of a double bond at the 2,3-position of the quinoline ring; the pharmaceutically acceptable acid addition salts thereof; and a process for the preparation thereof, are described. The compounds of the invention are useful for the treatment of hyperacidity and for the prevention of allergic and asthmatic reactions.
Type:
Grant
Filed:
June 25, 1976
Date of Patent:
February 28, 1978
Assignee:
Warner-Lambert Company
Inventors:
David T. Connor, Patricia A. Young, Maximilian VON Strandtmann
Abstract: A process for the conversion of the major antifungal antibiotic, acid S (ATCC NO. 25532) isolated from the fermentation of Polyangium cellulosum var. fulvum into the minor antibiotic, acid F, from the same fermentation is described wherein acid S is methylated with diazomethane to provide acid S methyl ester which is then oxidized with silver carbonate on celite to obtain the corresponding keto ester S, which is subsequently reduced with sodium borohydride to give a mixture of acid S methyl ester and acid F methyl ester. These esters are readily separated by preparative thin layer chromatography and the acid F methyl ester is hydrolyzed with sodium hydroxide solution to provide acid F.
Type:
Grant
Filed:
May 5, 1977
Date of Patent:
February 28, 1978
Assignee:
Warner-Lambert Company
Inventors:
David T. Connor, Maximilian VON Strandtmann
Abstract: This invention relates to a process for the preparation of 1-{[5-(4-hydroxy-2H-1,2-benzothiazin-3-yl)-1,2,4-oxadiazol-3-yl]methyl}eth anone S,S-dioxide (III), a novel intermediate useful in the preparation of the known anti-inflammatory agent, 4-hydroxy-3-(5-methyl-3-isoxazolylcarbamoyl)-2-methyl-2H-1,2-benzothiazine 1,1-dioxide (IV). According to the process of this invention, the saccharin compound, 2,3-dihydro-N-(5-methyl-3-isoxazolyl)-3-oxo-1,2-benzisothiazole-2-acetamid e 1,1-dioxide (I) is reacted with an alkali metal alkoxide of a lower alcohol in an inert solvent at temperatures below 30.degree. C. to form the benzenesulfonylglycineamide, alkyl 2-{[({[(5-methyl-3-isoxazolyl)amino]carbonyl}methyl)amino]sulfonyl}benzoat e (II), which is ring closed and rearranged by reaction with an alkali metal alkoxide of a lower alcohol in an inert solvent at temperatures of from 60.degree. to 70.degree. C. to form the desired oxadiazole compound III.
Type:
Grant
Filed:
February 10, 1976
Date of Patent:
February 28, 1978
Assignee:
Warner-Lambert Company
Inventors:
Arthur C. Fabian, Jerome D. Genzer, Charles Francis Kasulanis, John Shavel, Jr., Harold Zinnes
Abstract: Disclosed are novel benzo[g]Pyrido[2,1-b]-quinazolinones which are active as anti-allergy agents and thus have utility in the treatment of allergic reactions such as bronchial asthma.
Abstract: The present invention is concerned with novel tricyclic sulphoximides and with the preparation thereof. This family of compounds has been found to possess antihistominic, antitussive, antiinflammatory, sedative, and diuretic properties.
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:
June 16, 1976
Date of Patent:
February 28, 1978
Assignee:
Warner-Lambert Company
Inventors:
Wolf-Dieter Vigelius, Gerhard Satzinger, Manfred Herrmann
Abstract: A process is provided for producing intravenous immune globulin which comprises adsorbing plasminogen from blood of a selected mammalian species on L-lysine agarose, washing the adsorbate and eluting the purified plasminogen, converting the plasminogen to plasmin, and incubating a mixture of the plasmin and homospecific immune globulin having anticomplementary activity so as to reduce the anticomplementary activity, adsorbing excess plasmin present in the mixture, and recovering the immune globulin from the mixture.
Type:
Grant
Filed:
November 26, 1976
Date of Patent:
February 21, 1978
Assignee:
Parke, Davis & Company
Inventors:
Cyrill John Campbell, Daniel Ting Hsiu Liu
Abstract: New nonapeptides having the formula pGlu-D-Phe-Trp-Tyr(benzyl)-Ser(benzyl)-D-Ala-Leu-Orn-Pro-Y and Y is amino, lower alkylamino or di(lower alkyl)amino.
Abstract: 4-Aryl-1,6-dihydro-1,3,9-trimethylimidazo[1,2-a]-pyrazolo[4,3-f][1,4]-diaze pines; and acid-addition salts. The aryl group is phenyl, o-fluorophenyl, or o-chlorophenyl. The compounds are pharmacological agents, especially anticonvulsant and antianxiety agents. They can be produced by reacting a 7-(2-propynylamino)pyrazolo[3,4-e][1,4]diazepine with a strong anhydrous acid in the presence of a mercuric salt.
Abstract: New hexapeptides having the formula X-Pro-His(benzyl)-His(benzyl)-R-Trp-Ala-Y wherein X is t-butoxycarbonyl or benzyloxycarbonyl, R is Ser(benzyl) or Tyr(benzyl) and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino.
Abstract: A novel process for preparing 4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides is disclosed. The process involves the base catalyzed rearrangement of a saccharinacetamide of structure I to give II, ##STR1## wherein R.sup.1 is hydrogen or lower alkyl and R.sup.2 is lower alkyl, aryl or a heterocyclic ring selected from the group consisting of pyridyl, substituted-pyridyl, and thiazolyl. Compounds of the formula II have useful anti-inflammatory properties. In addition, they can be used as intermediate in the preparation of known anti-inflammatory agents.
Type:
Grant
Filed:
May 10, 1976
Date of Patent:
February 14, 1978
Assignee:
Warner-Lambert Company
Inventors:
Harold Zinnes, Neil A. Lindo, John Shavel, Jr.
Abstract: The present invention relates to 17-oxo-17-phenyl-prostaglandins having the following structural 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 hydrogen atom or a methyl or ethyl group, R.sup.2 and R.sup.3, which may be the same or different, each represent a hydrogen or halogen atom, a trifluoromethyl group or a straight- or branched-chain alkyl group containing from 1 to 3 carbon atoms, and R.sup.4 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.4 represents a hydrogen atom, non-toxic salts thereof.These compounds exhibit characteristic prostaglandin activity, e.g., abortifacient activity, stimulation activity on uterine contraction, and so on.
Abstract: 9-(5-O-Acyl-.beta.-D-arabinofuranosyl)adenine compounds and their production by reacting 9-(.beta.-D-arabinofuranosyl)adenine with a reactive derivative of an alkanoic acid. The compounds are useful as antiviral agents. The compounds are water-soluble and lipophilic, thereby being adaptable to a wide variety of pharmaceutical formulations.The present invention relates to new organic compounds that are useful in pharmacological agents and to a method for their production. More particularly, the invention relates to new 9-(5-O-acyl-.beta.-D-arabinofuranosyl)-adenine compounds that are represented by the formula ##STR1## where R is a straight chain alkanoyl group having from 2 to 8 carbon atoms or a branched chain alkanoyl group having 4 to 5 carbon atoms. Examples of alkanoyl groups represented by R are acetyl, propionyl, butyryl, pentanoyl, hexanoyl, octanoyl, 3-methylbutyryl, and 2,2-dimethylpropionyl.In accordance with the invention, 9-(5-O-acyl-.beta.
Type:
Grant
Filed:
May 17, 1976
Date of Patent:
January 17, 1978
Assignee:
Parke, Davis & Company
Inventors:
David Clarkston Baker, Theodore Herbert Haskell
Abstract: The present invention relates to compounds of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## B represents a single bond or a straight- or branched-chain alkylene group containing from 1 to 9 carbon atoms, W represents ethylene or trans-vinylene, X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, R represents a hydroxymethyl group or a grouping of the formula --COOR.sup.4, in which R.sup.4 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 hydrogen atom or a methyl or ethyl group and R.sup.3 represents a hydrogen or chlorine atom or a hydroxy group and cyclodextrin clathrates of such alcohols, acids and esters and, when R.sup.4 in the formula --COOR.sup.4 represents a hydrogen atom, non-toxic salts thereof, and intermediates therefor. These compounds exhibit characteristic prostaglandin-like activity.
Abstract: Oral pharmaceutical compositions comprising 3-phenoxy-pyridine or pharmaceutically acceptable acid-addition salts thereof and a pharmaceutical carrier. Methods for inducing psychostimulation by administering 3-phenoxypyridine or a pharmaceutically acceptable acid-addition salt thereof.
Abstract: This invention relates to substituted indolobenzoxazepines which act as central nervous system depressants and as such are useful as tranquillizers.
Abstract: Prostaglandin analogues of the formula: ##STR1## wherein X represents oxygen or sulphur, R.sup.1 and R.sup.2 each represent hydrogen or alkyl of from 1 to 3 carbon atoms, alkenyl of from 2 to 4 carbon atoms or trifluoromethyl, and the double bonds depicted in positions C.sub.5 -C.sub.6 and C.sub.13 -C.sub.14 are cis and trans respectively. These compounds are indicated in the treatment of impaired fertility, induction of labor or termination of pregnancy in females.