Abstract: 4-Aroylethnyl-1-piperidinobutyrophenone derivatives and pharmaceutically acceptable salts thereof of the following general structure: ##STR1## wherein R is hydrogen, alkyl, alkoxy, halogen or trifluoromethyl; and R' is hydrogen or halogen, are useful as antipsychotic agents. The novel compounds are produced by aldol condensation of an acetophenone with a protected 4-(4-formyl-1-piperidino)-butyrophenone.
Abstract: Compounds having the formula ##STR1## wherein A is a bond or C.sub.1-4 alkylene; R.sup.1, R.sup.2 and R.sup.3 are independently a halogen atom, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, CF.sub.3, SCF.sub.3 or OCF.sub.3 ; R.sup.4 is a hydrogen atom or C.sub.1-4 alkyl; and n, m and q are independently an integer from 0 to 3; and pharmaceutically acceptable acid addition salts thereof, are useful for the treatment of gastrointestinal hypersecretion.
Abstract: An improved denture adhesive contains a particular amount of a specified ratio of sodium carboxymethylcellulose and poly(ethylene oxide) in a mineral oil base.
Type:
Grant
Filed:
April 17, 1980
Date of Patent:
July 28, 1981
Assignee:
Richardson-Merrell Inc.
Inventors:
Dadi J. Dhabhar, Allen Heyd, Nicholas F. Schmidt
Abstract: Compounds of the following general formula are irreversible inhibitors of pancreatic elastase: ##STR1## wherein M is hydroxy, lower alkoxy, benzyloxy or --NY.sub.1 Y.sub.2 wherein each of R.sub.4 and R.sub.5 is hydrogen or lower alkyl; R is CF.sub.3, CHF.sub.2 or CH.sub.2 F; R.sub.1 is straight or branched lower alkyl; R.sub.2 is defined the same as R.sub.1 or is benzyl; R.sub.30 is CHO, carbobenzoxy, tert-butoxycarbonyl, benzoyl or lower alkanoyl; X is pro, ala or leu and Y and Z together form a single bond; or Y-X is ala-pro, ala-ala or ala-leu and Z forms a single bond; and Z-Y-X is ala-ala-pro, ala-ala-ala or pro-ala-leu.
Type:
Grant
Filed:
June 16, 1980
Date of Patent:
July 7, 1981
Assignee:
Richardson-Merrell Inc.
Inventors:
Philippe Bey, Brian W. Metcalf, Jeffrey S. Wiseman
Abstract: A method of inducing sedation in a patient comprises administering to a patient in which sedation is desired an amount effective for inducing sedation of a compound of the formula ##STR1## wherein R is H, or C.sub.1-5 or 7 -straight or branched chain alkyl:R.sub.1 is H, C.sub.1-5 or 7 -straight or branched chain alkyl or allyl;R.sub.2 is phenyl or phenyl substituted with F, Cl, Br, NO.sub.2, C.sub.1-5 straight or branched chain alkyl, C.sub.1-5 straight or branched chain alkoxy, 2,4-di-Cl, 2,4-di-F or 2,4-di-Br, with the proviso that when the phenyl group is monosubstituted with F, the F atom is not in the o-position; andR.sub.3 is H or C-1-5 straight or branched chain alkyl, with the proviso that when R.sub.3 is straight or branched chain alkyl, R.sub.2 is unsubstituted phenyl; ora pharmaceutically acceptable acid addition salt thereof.
Abstract: Novel antisecretory compounds of the formula: ##STR1## wherein R is ##STR2## and pharmaceutically acceptable salts, diasteriomers and individual optical isomers thereof.
Type:
Grant
Filed:
March 26, 1979
Date of Patent:
April 7, 1981
Assignee:
Richardson-Merrell Inc.
Inventors:
Albert A. Carr, Hsien C. Cheng, Stephen W. Horgan, James K. Woodward
Abstract: Derivatives of 2-hydroxy-5-(1-hydroxy-2-piperazinylethyl)benzoic acid are prepared which are useful for their blocking action on .alpha. and .beta.-adrenergic receptors. In addition, these compounds are useful as spasmolytic and antihypertensive agents.
Abstract: Novel compounds of the following formula: ##STR1## wherein R.sub.1 is hydrogen or hydroxy; R.sub.2 is hydrogen; or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ; n is an integer of from 1 to 5; R.sub.3 is --CH.sub.3, --CH.sub.2 OH, --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; and each of A and B is hydrogen or hydroxy; with the provisos that at least one of A or B is hydrogen and one of A or B is other than hydrogen when R.sub.3 is --CH.sub.3 ; and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
April 10, 1979
Date of Patent:
March 3, 1981
Assignee:
Richardson-Merrell Inc.
Inventors:
Albert A. Carr, Joseph E. Dolfini, George J. Wright
Abstract: Pharmaceutically useful compounds of the following formula: ##STR1## wherein R.sub.1 represents hydrogen or hydroxy; R.sub.2 represents hydrogen; or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ; n is a positive whole integer of from 1 to 5; R.sub.3 is --CH.sub.3, --CH.sub.2 OH, --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; and A and B are individually hydrogen or hydroxy; with the provisos that at least one of A or B is hydrogen and one of A or B is other than hydrogen when R.sub.3 is --CH.sub.3 ; and pharmaceutically acceptable acid addition salts thereof.
Type:
Grant
Filed:
April 10, 1979
Date of Patent:
March 3, 1981
Assignee:
Richardson-Merrell Inc.
Inventors:
Albert A. Carr, Joseph E. Dolfini, George J. Wright
Abstract: Novel compounds of the formula ##STR1## wherein n is an integer of from 2 to 5, R is hydrogen, alkyl, alkoxy, halogen or trifluoromethyl, R.sub.1 is hydrogen, alkyl, alkoxy or halogen, X is carbonyl, hydroxymethylene or methylene, and Z is carbonyl or hydroxymethylene and their pharmaceutically acceptable acid addition salts are useful as antipsychotic agents having a low potential for extrapyramidal side effects. The novel compounds are prepared from novel intermediates of formula ##STR2## or their salts wherein R and X have the meanings defined above.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is H or NH.sub.2 ;R.sub.2 is C.sub.1-6 straight or branched chain alkyl; --CH.sub.2 OH; --(CH.sub.2).sub.n --O--(CH.sub.2).sub.m --CH.sub.3 ; phenyl; or --(CH.sub.2).sub.p NH.sub.2 ;n is 1-3;m is 0-3; andp is 1-5;and the pharmaceutically acceptable acid addition salts of those compounds of basic character, have antisecretory activity.
Abstract: Compounds of the Formula ##STR1## wherein R is H or C.sub.1-4 alkyl; R.sub.1 is H or C.sub.1-4 alkyl; and R.sub.2 is straight or branched chain alkyl of 10-20 carbon atoms, straight or branched chain alkenyl of 10-20 carbon atoms, straight or branched chain alkadienyl of 10-20 carbon atoms or straight or branched chain alkatrienyl of 10-20 carbon atoms and the pharmaceutically acceptable salts thereof, are useful as hypolipidemic agents.
Abstract: This invention is to the compound 5-[2-[[3-(1,3-benzodioxol-5-yl)-1-methylpropyl]amino]-1-hydroxyethyl]-2-me thoxybenzamide having the formula, ##STR1## pharmaceutically acceptable salts and individual optical isomers thereof, pharmaceutical compositions comprising as the active ingredient the compound of Formula 1 or salts or isomers thereof and the use of said compound, or salt or isomer thereof or pharmaceutical composition comprising same in the treatment of hypertension.