Abstract: Manufacture of 4-substituted oxazolinone-(5) compounds, which are intermediates for substituted aminoacids, by alkylation of 2-substituted or 3,4-disubstituted oxazolinone-(5) compounds in an aprotic solvent in the presence of a tertiary amine.
Type:
Grant
Filed:
August 5, 1980
Date of Patent:
July 13, 1982
Assignee:
BASF Aktiengesellschaft
Inventors:
Wolfgang Steglich, Rudolf Hurnaus, Peter Gruber, Boerries Kuebel
Abstract: 1-(Aralkoxyphenyl)-2 or 3-(bis-arylalkylamino)-alkanes, e.g. those of the formula: ##STR1## or therapeutically acceptable salts thereof are hypotensive and cardioactive agents.
Abstract: Described are compounds of the formula ##STR1## wherein ##STR2## wherein Z is hydrogen or loweralkyl, R.sub.5 and R.sub.6 may be the same or different and are hydrogen, loweralkyl or together are alkylene of 4 or 5 carbon atoms,R.sub.2 is hydrogen, halo, haloloweralkyl, loweralkyl, loweralkoxy, loweralkylthio or ##STR3## wherein R.sub.5 and R.sub.6 are previously defined, R.sub.3 is hydroxy, alkoxy, branched alkoxy, adamantyloxy, morpholino, amino or amino substituted by loweralkyl or alkylene of 4 or 5 carbon atoms,R.sub.4 is hydrogen or loweralkyl, andX.sub.1 and X.sub.2 are hydrogen, loweralkyl, halo or when substituted on adjacent carbon atoms of the benzene ring form a 1,3-butadienylene linkage, Y is oxygen or sulfur, and pharmaceutically acceptable salts thereof. The compounds are effective as diuretic agents in increasing urinary excretion.
Abstract: What are disclosed are a diagnostic agent for visualizing the hepatobiliary system which agent contains Technetium-99m-labelled (2,4,5-trimethylacetanilido)-iminodiacetate in a suitable solvent, and a process for the preparation of this diagnostic agent; chloroacetic acid-(2,4,5-trimethylanilide) as an intermediate product and a process for the preparation thereof; and (2,4,5-trimethylacetanilido)-iminodiacetate and a process for the preparation thereof.
Type:
Grant
Filed:
December 19, 1979
Date of Patent:
March 9, 1982
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Michael Molter, Gerhard Kloss, Eberhard Schickel
Abstract: Complexes of radiolabelled metals with N-(tri-substituted alkyl)-iminodiacetic acids or salts thereof having utility as radiopharmaceutical agents for monitoring the activity of an organ, their preparation and a method employing such complexes for externally monitoring the activity of an organ are disclosed.
Type:
Grant
Filed:
December 13, 1979
Date of Patent:
December 29, 1981
Assignee:
G. D. Searle & Co.
Inventors:
Patricia Frank, Stephen Kraychy, Ernest F. Le Von
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: Manufacture of 4-substituted oxazolinone-(5) compounds, which are intermediates for .alpha.-substituted aminoacids, by alkylation of 2-substituted or 3,4-disubstituted oxozolinone-(5) compounds in an aprotic solvent in the presence of a tertiary amine.
Type:
Grant
Filed:
March 29, 1978
Date of Patent:
April 28, 1981
Assignee:
BASF Aktiengesellschaft
Inventors:
Wolfgang Steglich, Rudolf Hurnaus, Peter Gruber, Boerries Kuebel
Abstract: 3-[4-(Disubstituted-amino)phenyl] or (9-julolidinyl)-3-(diphenylamino)phthalides useful as color formers in pressure-sensitive and thermal marking systems are prepared by reaction of 2-[4-(disubstituted-amino)benzoyl] or (9-julolidinyl-carbonyl)benzoic acids with diphenylamines.
Abstract: Compounds of the formula ##STR1## in which A is lower alkyl, or a substituted or unsubstituted phenyl, thienyl, furyl, indolyl or thiaindolyl radical, R, X.sub.4 and X.sub.5 are hydrogen or lower alkyl, Y is hydrogen, hydroxy, etherified hydroxy, substituted amino, or N-attached heterocyclyl, X.sub.0 is O or OCH.sub.2 CH.sub.2 O, R' represents hydrogen, lower alkyl or acetyl; and acid-addition salts thereof, are novel and useful in pharmacy as hypolipaemiant, hypocholosterolaemiant and cholagogic agents or in the preparation of such agents.
Abstract: 5-Substituted indan-2-carboxylic acids and functional derivatives thereof having inflammation-reducing properties have the general formula ##STR1## in which R is a phenyl, phenyl-lower alkenyl, phenyl-lower alkyl, phenyl substituted by at least one of the halogens, lower alkyl, lower alkoxy, acetamido, amino, lower dialkylamino, nitro, phenyl, lower alkylsulfonyl, lower dialkylaminosulfonyl and sulfamido, cyclohexyl, furyl, lower alkylfuryl, thienyl, halothienyl, lower alkylthienyl, or pyridyl group and R' is a hydroxyl, lower alkoxy, lower dialkylaminoalkoxy, cinnamoylamido lower alkoxy, 2-hydroxyethylamino, amino or lower dialkylaminoalkyl amino group. Besides the esters and amides, the functional derivatives of the acids include the pharmacologically acceptable salts of the above compounds. The compounds are also of low toxicity, have analgesic activity and exert an antipyretic effect.
Abstract: This disclosure describes 4-monoalkylaminophenyl carbinols (primary, secondary, and tertiary alcohols) and with derivatives and salts thereof useful as hypolipidemic and anti-atherosclerotic agents.
Abstract: Compounds of the formula ##STR1## in which A is lower alkyl, or a substituted or unsubstituted phenyl, thienyl, furyl, indolyl or thiaindolyl radical, R, X.sub.4 and X.sub.5 are hydrogen or lower alkyl, Y is hydrogen, hydroxy, etherified hydroxy, substituted amino, or N-attached heterocyclyl, X.sub.0 is O or OCH.sub.2 CH.sub.2 O, R' represents hydrogen, lower alkyl or acetyl; and acid-addition salts thereof, are novel and useful in pharmacy as hypolipaemiant, hypocholosterolaemiant and cholagogic agents or in the preparation of such agents.
Abstract: A method of treating mammals for allergy and anaphylactic reactions of a reagin or non-reagin mediated nature which comprises administering prophylactically to said mammal an anti-allergy or anaphylactic reaction effective amount of a compound of the formula ##STR1## Novel compositions are also claimed.
Abstract: Novel 2-amino-3-(5- and 6-)benzoylphenylacetic acids, esters and metal salts of the formula: ##STR1## wherein R is hydrogen or lower alkyl, R.sup.1 is hydrogen, lower-alkyl, sodium or potassium, R.sup.2 is hydrogen, halogen or lower alkoxy, X is hydrogen, lower alkyl, halogen, nitro or trifluoromethyl, Y is hydrogen, lower alkyl, halogen, nitro or trifluoromethyl, and Am is primary amino (--NH.sub.2) methylamino or dimethylamino. The compounds are prepared by hydrolysis of 4-(5- and 7-)benzoylindolin-2-ones to give the 2-amino-3-(5- and 6-)benzoylphenylacetic acids wherein amino is primary amino. The free acids are converted to the esters and metal salts. The calcium and magnesium salts are disclosed and are within the scope of the present invention. The compounds have anti-inflammatory activity, are effective in lowering the cholesterol levels in hyperlipemic rats and inhibit blood platelet aggregation.
Type:
Grant
Filed:
April 15, 1977
Date of Patent:
November 21, 1978
Assignee:
A. H. Robins Company, Incorporated
Inventors:
William J. Welstead, Jr., Henry W. Moran
Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## AND FUNCTIONAL DERIVATIVES THEREOF, ARE ANTI-INFLAMMATORY AGENTS.
Abstract: Pharmaceutical compositions having as the active agent a compound of the formula ##STR1## useful for preventing allergic manifestations in sensitized mammals and novel compounds.
Abstract: The invention relates to 3,4-Dihydro-2H-isoquinoline-1-ones and a process for preparing them.The compounds have an antiarrhythmic activity and are suitable for treating disturbance of the cardiac rhythm.