Abstract: The compounds are pyridyl substituted aminoalkylthioureas and ureas which are inhibitors of H-2 histamine receptors. A compound of this invention is N-methyl-N'-[2-(2-pyridylmethylamino)ethyl]thiourea.
Type:
Grant
Filed:
October 29, 1975
Date of Patent:
April 19, 1977
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Graham John Durant, John Colin Emmett, Charon Robin Ganellin
Abstract: The method comprises administering to an animal a novel pharmaceutical composition containing a substituted-1-oxo-1H-2-benzothiopyran-3-carboxylic acid to inhibit antigen-antibody reaction in said animal. Representative of the compounds that can be used in the method are:1-Oxo-1H-2-benzothiopyran-3-carboxylic acid, andSodium 6-methoxy-1-oxo-1H-2-benzothiopyran-3-carboxylate.
Abstract: Substituted naphthoquinones of the formula (I) and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent alkyl, aryl, alkoxy, hydroxy, hydrogen or halogen or any two of the groups R.sub.1, R.sub.2, R.sub.3 and R.sub.4 taken together complete a carbocyclic ring, have useful anti-allergy activity in mammals.
Type:
Grant
Filed:
March 12, 1976
Date of Patent:
April 12, 1977
Assignee:
Beecham Group Limited
Inventors:
Barry Christian Charles Cantello, Derek Richard Buckle, Harry Smith
Abstract: A process for preparing pyridinium chloride salts of esters of 2-chloro-N-2-hydroxyethylacetamide in which no intermediates need be isolated is disclosed.
Abstract: The invention is predicated on the discovery that certain 1,4-disubstituted piperazines interact synergistically with certain known analgesics to antagonize or block the stimulus causing migraine. This effect is most pronounced when administering a mixture of 1-p-chlorobenzhydryl-4-p-(tertiary butyl)-benzyl-piperazine (buclizine) and N-acetyl-p-aminophenol (paracetamol) in the respective proportions by weight of from 1:20 to 1:200.
Abstract: Novel hydrogenated pyrimidine nucleosides and nucleotides are produced by catalytic hydrogenation, particularly in the presence of a rhodium catalyst. The novel compounds are specifically used to inhibit deaminating enzymes, which would inactivate cytosine arabinoside by conversion to uridine arabinoside. Cytosine arabinoside is used for its anti-viral, particularly anti-herpes and anticytotoxic activity in mammals and birds, as well as to destroy phages which interfere with the production of antibiotics. Novel formulations containing cytosine arabinoside and the hydrogenated pyrimidine nucleosides are advantageous to provide prolonged cytosine arabinoside effects.
Abstract: 6-(.alpha.-3-Acyl-ureidoacetamido)-penicillanic acids and pharmaceutically acceptable non-toxic salts thereof in which the hydrogen atom of the nitrogen atom present in the 3-position is substituted, are effective against Gram-positive and Gram-negative infections, particularly Klebsiella aerobacter infections.
Type:
Grant
Filed:
April 16, 1975
Date of Patent:
April 5, 1977
Assignee:
Bayer Aktiengesellschaft
Inventors:
Hans-Bodo Konig, Wilfried Schrock, Hans Disselnkotter, Karl Georg Metzer
Abstract: Substituted naphthoquinones of the formula (I) and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent alkyl, aryl, alkoxy, hydroxy, hydrogen or halogen or any two of the groups R.sub.1, R.sub.2, R.sub.3 and R.sub.4 taken together complete a carbocyclic ring, have useful anti-allergy activity in mammals.
Type:
Grant
Filed:
April 24, 1975
Date of Patent:
March 29, 1977
Assignee:
Beecham Group Limited
Inventors:
Barry Christian Charles Cantello, Derek Richard Buckle, Harry Smith
Abstract: Alkanoyl substituted benzoic acids and esters, e.g., p-pivaloyl ethyl benzoate, are prepared by oxidizing alkanoyl substituted toluene and reacting with lower alkanols and are useful as hypolipidemic, anti-obesity, and anti-diabetic agents.
Abstract: Pharmaceutical compositions comprising a substituted 3-cinnamoyl-2H-pyran-2,6(3H)-dione and methods of inhibiting the antigen-antibody reaction by administering said compositions. Certain of the 3-cinnamoyl-2H-pyran-2,6(3H)-diones are novel compounds per se.
Type:
Grant
Filed:
February 19, 1976
Date of Patent:
March 29, 1977
Assignee:
SmithKline Corporation
Inventors:
Lawrence William Chakrin, Kenneth Means Snader, Chester Rhodes Willis
Abstract: Certain compounds in which a carbon atom of a pyrrolidine or piperidine ring is bonded directly or through a methylene group to the nitrogen of a substituted benzamido group, and their pharmaceutically acceptable salts, are found to be active as antiarrhythmic agents.
Abstract: Substituted benzopyrano[3,4-c]pyridines having the following structural formula are disclosed: ##STR1## In the above formula, R.sub.1 R.sub.2 are hydrogen, a hydroxyl group or a lower alkoxyl group of from 1 to 6 carbon atoms; R.sub.3 is hydrogen or a lower alkyl group of from 1 to 6 carbon atoms and X is an oxygen atom, a sulfur atom, a methylene group or a nitrogen atom substituted by hydrogen, a lower alkyl group of from 1 to 6 carbon atoms or a lower alkanoyl group of from 1 to 6 carbon atoms. The compounds of this invention are prepared by reacting an R.sub.1, R.sub.2 -substituted phenol with a 3-carbethoxy-4-piperidone in the presence of an acid catalyst to give an intermediate R.sub.1, R.sub.2 -substituted benzopyrano[3,4-c] pyridine. N-aminoalkylbenzopyrano[3,4-c]pyridines are obtained by treating the benzopyrano[3,4-c]pyridine with an appropriately substituted alkyl halide. The compounds of this invention are useful as bronchodilators for the treatment of bronchial asthma.
Abstract: The present invention provides compounds of formula: ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, halog alkyl having from 1 to 6 carbon atoms, alcoxy having from 1 to 6 carbon atoms and alkylthio having from 1 to 6 carbon atoms,A taken separately is hydrogen and B is a radical with the formula ##STR2## , R.sub.3 being selected from the group consisting of hydrogen, halogen and alcoxy having from 1 to 6 carbon atoms, and A and B taken together form a radical --O--CH.sub.2 --, and the esters, N oxides and pharmacologically acceptable salts of the acids of Formula I.These compounds have analgesic and antiinflammatory properties.
Type:
Grant
Filed:
October 15, 1974
Date of Patent:
March 8, 1977
Assignee:
SERDEX - Societe d'Etudes, de Recherches, de Diffusion et d'Exploitation
Abstract: Composition and method for the prevention and treatment of syndromes caused by platelet-aggregation disorders wherein the active ingredient is a compound of the formula: ##STR1## wherein R is H or C.sub.1 -C.sub.4 alkyl and R.sub.1 is H, C.sub.1 -C.sub.4 alkyl or ##STR2## wherein n is 1 or 2, and R.sub.2 and R.sub.3 are H or C.sub.1 -C.sub.4 alkyl, or salts thereof.
Type:
Grant
Filed:
October 16, 1975
Date of Patent:
March 1, 1977
Assignee:
Carlo Erba
Inventors:
Pier Nicola Giraldi, Giuliano Nannini, Giovanni Riasoli, Anna Spelta, Aurelio Contone
Abstract: Benzoic acid amides characterized by the presence of a hydroxy or amino substituent in the phenyl ring, or an alkylated or acylated derivative thereof and by a heterocyclic group connected to the amide nitrogen atom through a hydrocarbon chain are antibacterial agents and in particular anti-tuberculosis agents. The compounds, of which N-[pyridyl-(2)-methyl]-2-hydroxybenzoic acid amide is a typical embodiment, are prepared by the reaction of an appropriately substituted benzoic acid, or derivative thereof, with an appropriate amine.
Type:
Grant
Filed:
April 2, 1975
Date of Patent:
February 1, 1977
Assignee:
Bayer Aktiengesellschaft
Inventors:
Karl Heinrich Mayer, Hans-Joachim Kabbe, Hinrich Otten
Abstract: Pharmaceutical compositions having anti-allergy activity in which the active anti-allergy agents are certain 3-nitro-.alpha.-pyridones and their pharmaceutically acceptable salts formulated in one or more pharmaceutically acceptable carriers.
Type:
Grant
Filed:
May 21, 1975
Date of Patent:
February 1, 1977
Assignee:
Beecham Group Limited
Inventors:
Derek Richard Buckle, Barrie Christian Charles Cantello, Harry Smith