Abstract: Sulfonium compounds represented by the formula ##STR1## have anticancer activity, immunostimulant activity and the like, and useful as the active components of drugs and agricultural chemicals.
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: Pharmaceutical compounds of the general formula ##STR1## and non-toxic pharmaceutically-acceptable salts thereof wherein R.sup.1 is inter alia alkyl, cycloalkyl, aralkyl, or certain pyridyl or phenyl radicals, and with provisoR.sup.2 is selected from hydrogen, lower alkyl, lower alkoxy, amino, hydroxyl, halogen, carboxyl, amido, and --CON(lower alkyl).sub.2. Methods of preparing these compounds are described. The compounds exhibit analgesic, anti-inflammatory, hyperglycemic and/or hypoglycemic activity.
Type:
Grant
Filed:
August 18, 1980
Date of Patent:
July 6, 1982
Assignee:
Canadian Patents & Development Limited
Inventors:
Edward E. Knaus, Linda A. Corleto, Kinfe Redda
Abstract: Penicillin compounds and methods for the production thereof are described, said penicillin compounds being represented by the formula (I) ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 each represents hydrogen, a lower alkyl group, a halogen atom, a lower alkoxy group, a hydroxyl group, or a substituted or unsubstituted phenylalkoxy group except that R.sub.1, R.sub.2, and R.sub.3 cannot all represent hydrogen simultaneously; R.sub.4 represents hydrogen or a lower alkyl group; and R.sub.5 represents hydrogen or a hydroxyl group.
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: Iminobenzyl dihydropyridines of the formula ##STR1## wherein, each R is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl, sulfonamido, halogen, alkoxy, alkenyloxy, alkynyloxy, cyano, hydroxy, acyloxy, nitro, amino, alkylmercapto, alkylamino, alkanoylamino, carbalkoxyamino, carboxy, methanesulfonyl, carbalkoxy or trifluoromethyl;each R.sub.4 is lower alkoxy;each R.sub.2 is lower alkyl;and R.sub.3 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclic or ##STR2## wherein R is as previously defined; have anti-hypertensive activity.
Abstract: Derivatives of benzoylphenoxyalkanoic acids corresponding to the formula: ##STR1## wherein: X represents for example a halogen, R.sup.1 and R.sup.2 represent for example alkyl groups, R represents for example an aminoacid; and the salts thereof are new products showing antilipaemic and anticholesterolemic pharmacological activity.
Type:
Grant
Filed:
February 21, 1980
Date of Patent:
October 20, 1981
Assignee:
Alpha Farmaceutici S.p.A.
Inventors:
Valerio Borzatta, Manlio Cristofori, Mauro Morotti, Giuseppe Mascellani
Abstract: Novel substituted (3-loweralkylamino-2-R.sub.1 O-propoxy)pyridines, their pharmaceutically acceptable salts, certain intermediates and their preparation are disclosed. These pyridines have pharmaceutically useful properties such as .beta.-adrenergic blocking activity.
Abstract: A compound of the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each represents a member selected from the group consisting of hydrogen and nicotinoyl, with the proviso that R.sub.1, R.sub.2 and R.sub.3 do not all simultaneously represent hydrogen, and the nontoxic acid addition salts thereof.
Abstract: The invention provides 4-pyridone-3-carboxylic acids and derivatives thereof together with a method for their preparation. Also included in the invention are compositions containing said 4-pyridone-3-carboxylic acids and derivatives and the use of said compounds and compositions as antibacterial and/or antifungal agents or for animal growth promotion or improved feed utilization.
Type:
Grant
Filed:
February 1, 1979
Date of Patent:
August 18, 1981
Assignee:
Bayer Aktiengesellschaft
Inventors:
Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
Abstract: Novel alkylene glycol derivatives of the formula (1) ##STR1## in which R.sup.1 is the hydrogen atom, an alkyl group having 1-4 C-atoms or an aryl group, R.sup.2 is the hydrogen atom or an alkyl group having 1-4 C-atoms, R.sup.3 is the hydrogen atom or a group of the formula ##STR2## in which Z is an alkyl residue, an optionally substituted aryl residue or a heterocyclic residue and R.sup.4 is a residue of the formula ##STR3## in which R.sup.5 is the hydrogen atom or chlorine atom, or the methyl group, exhibit an advantageous activity in regard of lowering the cholesterol and triglyceride level in the blood. Production of the novel derivatives by reduction of the corresponding acids, or by reacting a phenol of the formula ##STR4## and an alcohol of the formula ##STR5## optionally with subsequent esterification, is described.
Type:
Grant
Filed:
April 23, 1979
Date of Patent:
June 23, 1981
Assignee:
Siegfried AG
Inventors:
Kurt Thiele, Quazi Ahmed, Ulrich Jahn, Rudolf Adrian
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: This invention concerns a two-step process for the preparation of ethylene from mixture of carbon monoxide and hydrogen (commonly known as synthesis gas) by reaction of said carbon monoxide/hydrogen mixtures with a carboxylic acid in the presence of one or more ruthenium catalyst complexes to form an ethyl ester of said carboxylic acid coreactant, followed by pyrolysis of said ethyl ester intermediate to ethylene.
Abstract: Novel taurine derivatives of general formula (I) ##STR1## (wherein R.sup.1 is nicotinoyl, 3,4,5-trimethoxybenzoyl or acetylsalicyloyl and R.sup.2 is as defined for R.sup.1 or is --CH.sub.2 CH.sub.2 OR.sup.1) have antilipemic and choleretic activities. The compound in which R.sup.2 .dbd.--CH.sub.2 CH.sub.2 OR.sup.1 and R.sup.1 is acetylsalicyloyl exhibits high antiinflammatory, analgesic and antipyretic activity and is essentially free of the unfavorable effect of acetylsalicylic acid on the stomach.
Abstract: Iodopropargyl derivatives of formula:IC.tbd.CCH.sub.2 OR[wherein R represents an alkanoyl group (which may be unsubstituted or have one or more halogen, cyano, substituted or unsubstituted .alpha.
Abstract: In this disclosure, the synthesis of alkyl and aryl esters of substituted 2-anilino-3-pyridinecarboxylic acids is described. This preparation is performed reacting a previously obtained alkyl or aryl ester of 2-chloro-3-pyridinecarboxylic acid, with 3,2 or 3-substituted aniline.
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: N-substituted .omega.-aminoalkanoyl-.omega.-aminoalkanoic acids and their pharmacologically-acceptable salts (with a base) are useful, e.g., in pharmaceutical-composition form for the treatment or prophylaxis of diseases which are based on inadequate performance of the pancreas, the bile and/or the liver. The compounds are prepared, e.g., by reacting an N-(mono- or di-substituted) .omega.-amino-alkanoic acid with an N-(unsubstituted or monosubstituted) .omega.-aminoalkanoic acid.
Abstract: A highly selective oxidation process for preparing pyridin-carboxylic acids from pyridine compounds nucleus substituted with alkyl groups, through a carbon-carbon bond, and oxidizable to carboxyl, and from hydrosoluble hexavalent chromium compounds, in the presence of an acid.Particularly described is the oxidation of beta-picoline with sodium bichromate to obtain the sodium salt of nicotinic acid and 99.5% pure free acid, respectively.
Abstract: Soft quaternary surface active agents having the formula: ##STR1## wherein >N represents a tertiary open chain or cyclic aliphatic amine; wherein >N represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.20 open chain or cyclo alkyl group, a C.sub.1 -C.sub.20 alkoxyalkyl group, a C.sub.1 -C.sub.20 acyloxyalkyl group, a C.sub.1 -C.sub.20 haloalkyl group, a C.sub.1 -C.sub.20 carboxyalkyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O--C.sub.1 -C.sub.4 alkyl group, an O--C.sub.1 -C.sub.8 acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.1 represents a C.sub.9 -C.sub.22 straight or branched alkyl group, a --(CH.sub.2).sub.n -- ##STR2## group, wherein R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each selected from the group consisting of a hydrogen atom, a methyl group or an ethyl group, a C.sub.0 -C.sub.
Abstract: Labile quaternary ammonium salts of the following formula (I) and (II) are provided: ##STR1## wherein ##STR2## represents a tertiary aliphatic amine; wherein ##STR3## represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.8 open chain or cyclo alkyl group, a C.sub.1 -C.sub.8 alkoxyalkyl group, a C.sub.1 -C.sub.8 acyloxyalkyl group, a C.sub.1 -C.sub.8 haloalkyl group, a C.sub.1 -C.sub.8 carboxyalkyl group, a C.sub.2 -C.sub.8 alkenylphenyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O-lower alkyl (C.sub.1 -C.sub.4) group, an O-acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.1 which may be the same or different, represents any member defined by R above with the proviso that R.sub.
Abstract: Chromone compounds carrying a pyridyl substituent at the 2-position are disclosed, such as, for instance, 6-carboxy-2-(2'-pyridyl)-chromone. The disclosed compounds are useful in the treatment of allergies.
Type:
Grant
Filed:
September 16, 1977
Date of Patent:
April 10, 1979
Assignee:
Carlo Erba S.p.A.
Inventors:
Gianfederico Doria, Piernicola Giraldi, Francesco Lauria, Maria L. Corno, Piero Sberze, Marcello Tibolla
Abstract: The process for the production of 2-chloronicotinic acid from nicotinic acid-N-oxide, characterized in that the 2-chloronicotinic acid chloride is distilled off from the reaction mixture and the distillate is allowed to flow into water at a temperature of 40.degree. to 100.degree. C. The 2-chloronicotinic acid chloride is hydrolized to the 2-chloronicotinic acid, which precipitates in a pure white crystalline form.
Abstract: A treatment to alleviate the symptoms of psoriasis consisting of topical application of a cream, ointment or lotion containing, as the principal active ingredient, one or more 6-substituted nicotinamides and or 2-substituted pyrazinamides is disclosed. The therapeutic composition may include a single member of the above active ingredients present in a total amount of from 0.01 to 5 percent by weight of the total composition, or a plurality thereof present in a preferred concentration range of from 0.02 to 2 percent by weight of the total composition. Topical application of the therapeutic composition in a cream, ointment, or a water or alcohol solution has been found to achieve from substantial to complete remissions of psoriasis in humans.