Abstract: As new medicaments notably in the field of stomatology, the phenolic esters of eugenol and N-heteroaryl carboxylic acids including their N-oxides, and notably eugenyl nicotinate, picolinate and N-oxynicotinate and their pharmaceutical forms are disclosed.A new long acting form of local antalgesic is disclosed having a resorbable solid or doughy support which is impregnated with the active principle. The support may be for instance made of gelatin sponge.
Abstract: The present invention relates to compounds which are derivatives of 1,4-dihydropyridine-3-carbothiol acids of the formula: ##STR1## wherein R is hydrogen, an alkyl, aryl, heteryl;R' is a lower alkyl, aralkyl;R" is an alkoxy, alkylthio, aralkylthio;R"' is methyl;R"'+R" is phenylene (ortho-).The compounds of the present invention reveal a coronarodilating activity, and are useful in medicine.
Type:
Grant
Filed:
October 28, 1980
Date of Patent:
April 20, 1982
Inventors:
Brigita A. Vigante, Yan-Voldemar Y. Ozol, Rasma O. Vitolin, Gunta O. Silenietse, Agris A. Kimenis, Gunar Y. Dubur
Abstract: Novel hypolipidemic nicotinates and related esters, being phenoxy organic compounds, are disclosed, as well as pharmaceutical compositions thereof and method of treating hyperlipidemia therewith.
Type:
Grant
Filed:
January 5, 1981
Date of Patent:
March 23, 1982
Assignee:
Merz & Co.
Inventors:
Arthur Scherm, Dezsoe Peteri, Klaus Hummel
Abstract: The invention relates to a process for the production of 1,4-dihydropyridinecarboxylic acid compounds which involves hydrolysis, under alkaline conditions and in a temperature range from 10.degree. to 100.degree. C., of an ester group which contains an electron-attracting group. The invention also includes novel compounds made according to the invention as well as compositions containing said novel compounds. Also included in the invention are methods for the use of said compounds and compositions. The compounds obtained according to the process of the invention are useful because of their circulation-influencing action and are also useful as intermediates for the preparation of compounds having circulation-influencing action.
Abstract: 1,4-dihydropyridine derivatives of the general formula ##STR1## having vasodilating and anti-hypertensive activity, processes for preparing same, and pharmaceutical compositions thereof for treating cardiovascular diseases.
Abstract: The invention relates to a novel process and novel intermediates useful in the preparation of sympathomimetic amines. The pharmacologically useful final products, which are acyl derivatives of mono- and dihydroxy aromatic amines (e.g., catechol amines) can be prepared in optically active or racemic form by reacting the corresponding mono- or dihydroxy aromatic amine with a reagent capable of forming the N-tert-butoxycarbonyl derivative thereof; reacting the novel intermediate thus obtained with an acyloxymethyl chloride to afford the corresponding novel mono- or diacylated N-protected aromatic amine; and removing the N-protecting group therefrom.
Abstract: Aromatic acids having the following formula ##STR1## have been found to be effective plant growth regulants especially for the treatment of corn plants.
Type:
Grant
Filed:
August 9, 1978
Date of Patent:
April 14, 1981
Assignee:
Monsanto Company
Inventors:
Frederic G. Bollinger, John J. D'Amico, Dale J. Hansen
Abstract: Prostan-1-ol esters and intermediates for their preparation are described; the former compounds exhibit improved organ specificity and a longer duration of activity at lower dosages than the corresponding non-esterified prostaglandins and are useful, inter alia, in triggering abortion, inducing labor and regulating the menstrual cycle.
Type:
Grant
Filed:
March 2, 1978
Date of Patent:
March 17, 1981
Assignee:
Schering Aktiengesellschaft
Inventors:
Werner Skuballa, Bernd Raduchel, Helmut Vorbruggen, Walter Elger, Olaf Loge, Eckehard Schillinger
Abstract: The present invention relates to compounds which are derivatives of 1,4-dihydropyridine-3-carbothiol acids of the formula: ##STR1## wherein R is hydrogen, an alkyl, aryl, heteryl;R' is a lower alkyl, aralkyl;R" is an alkoxy, alkylthio, aralkylthio;R"' is methyl;R'"+R" is phenylene (ortho-).The compounds of the present invention reveal a coronarodilating activity, and are useful in medicine.
Type:
Grant
Filed:
March 19, 1979
Date of Patent:
February 24, 1981
Inventors:
Brigita A. Vigante, Yan-Voldemar Y. Ozol, Rasma O. Vitolin, Gunta O. Silenietse, Agris A. Kimenis, Gunar Y. Dubur
Abstract: The invention concerns novel 1-benzyl-1,2,5,6-tetrahydropyridine-3-carboxylic acid derivatives of the formula: ##STR1## wherein R.sup.1 is hydroxy, amino, (1-4C)alkylamino, di-[(1-4C)alkyl]amino, benzyloxy optionally substituted by halogeno, or (1-6C)alkoxy optionally substituted by (1-4C)alkoxy, morpholino or di-[(1-4C)alkyl]amino; and benzene ring A bears one or two substituents selected from halogeno, (1-4C)alkyl, cyano, carboxamido, trifluoromethyl and hydroxy; and their pharmaceutically acceptable salts; together with pharmaceutical compositions thereof; and analogy processes for their manufacture.The compounds of formula I are inhibitors of the aggregation of blood platelets and may be of application in the treatment or prophylaxis of thrombosis or occlusive vascular disease. A representative compound of the invention is 1-(2-chlorobenzyl)-1,2,5,6-tetrahydropyridine-3-carboxylic acid.
Abstract: The present invention relates to derivatives of 1,4-dihydropyridine and, more specifically, to 2,6-dimethyl-3,5-dimethoxycarbonyl-4-(o-difluoromethoxyphenyl)-1,4-dihydro pyridine of the formula: ##STR1## This compound features a clearly pronounced hypotensive activity while being low-toxic, wherefore it can be used in medicine for treating hypertensive disease.
Type:
Grant
Filed:
January 5, 1979
Date of Patent:
August 26, 1980
Inventors:
Valeria V. Kastron, Rasma O. Vitolin, Jury A. Fialkov, Svetlana V. Shelyazhenko, Gunar Y. Dubur, Agris A. Kimenis, Lev M. Yagupolsky
Abstract: Substituted furopyridinones and furopyrazinones which are useful as color formers in pressure-sensitive carbonless duplicating systems and thermal marking systems are prepared by reacting diphenylamines with substituted benzoyl (or 3-indolylcarbonyl)pyridinecarboxylic acids and substituted benzoyl (or 3-indolylcarbonyl)pyrazinecarboxylic acids, respectively.
Abstract: This disclosure describes esters of 4-(monoalkylamino)benzoic acids with hydroxyalkanoic acids and derivatives, phenols, or 3-pyridinols useful as hypolipidemic agents.
Abstract: Novel diphenyl and loweralkyl substituted diphenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful because of their low toxicity, and as such are advantageously included as the active agent in surgical scrubs, antibacterial soaps, as preservatives in cosmetic preparations, and the like. They also can be used for topical treatment of dermatological conditions having a bacterial origin or implication such as Acne vulgaris.
Type:
Grant
Filed:
December 3, 1976
Date of Patent:
October 23, 1979
Assignee:
Merck & Co., Inc.
Inventors:
Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
Abstract: The invention relates to new dihydropyridines which are substituted by an amino group in at least one of the 2- and 6-positions, by a sulphur-containing substituent in the 3-position, by a cyclic substituent in the 4-position and by a carbonyl substituent in the 5-position. The new dihydropyridines are particularly useful as agents which influence the circulatory system. Also included in the invention are procedures for preparation of the new dehydropyridines, compositions containing them and methods for their use.
Type:
Grant
Filed:
August 26, 1977
Date of Patent:
July 24, 1979
Assignee:
Bayer Aktiengesellschaft
Inventors:
Egbert Wehinger, Friedrich Bossert, Horst Meyer, Gerhard Franckowiak, Wulf Vater, Arend Heise, Stanislav Kazda, Kurt Stoepel