Abstract: Aminoketone-substituted coumarin sensitizers having tethered tertiary amino groups are described which have extremely good photosensitivity. The sensitizers of the instant invention have the formula: ##STR1## wherein R.sub.1 and R.sub.2 each represent an alkyl group having 1 to 6 carbon atoms, and R.sub.3 and R.sub.4 each represent hydrogen; or at least one of R.sub.1 and R.sub.3 or R.sub.2 and R.sub.4 together represent an alkylene group having 2 to 4 carbon atoms,R.sub.5 represents an alkyl group having 1 to 6 carbon atoms or H,R.sub.6 represents an alkylene group having 1 to 6 carbon atoms, andR.sub.7 and R.sub.8 each independently represent an alkyl group having 1 to 6 carbon atoms, both of R.sub.7 and R.sub.8 taken together represent an alkylene group having 4 to 6 carbon atoms, or R.sub.5 or R.sub.6 taken together with R.sub.7 or R.sub.8 represent a five, six, or seven membered heterocyclic ring group.
Type:
Grant
Filed:
February 3, 1995
Date of Patent:
July 9, 1996
Assignee:
Minnesota Mining and Manufacturing Company
Abstract: A condensed heterocyclic compound having a structure represented by formula (I): ##STR1## wherein the substituents are as defined in the specification herein.
Abstract: This invention provides improved synthetic processes for the preparation of hydroxy-protected cyclic urea compounds of Formula (IX), ##STR1## which are useful as intermediates for the preparation of cyclic urea human immunodeficiency virus (HIV) protease inhibitors, from N-protected aminoaldehydes. The processes of the present invention provide high yields, can be conducted on multikilogram scale, and eliminate the need for chromatographic purification of intermediates or final product.
Type:
Grant
Filed:
June 30, 1994
Date of Patent:
June 25, 1996
Assignee:
The DuPont Merck Pharmaceutical Company
Inventors:
Lilian A. Radesca, Gregory D. Harris, Edward K. W. Wat, Robert E. Waltermire
Abstract: The compound of the formula: ##STR1## where R.sub.1 and R.sub.5 are independently hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl, cyano, nitro, CO.sub.2 H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, cycloalkylalkyl, C.sub.3 -C.sub.8 cycloalkyloxy, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkylcarbonyloxy, C.sub.2 -C.sub.7 alkoxycarbonyl, mono- or di-alkylaminocarbonyl, tetrazolyl, --OH, --(CH.sub.2).sub.1-6 OH, --SH, --NH.sub.2 or --(CH.sub.2).sub.1-6 NR.sub.8 R.sub.9 where R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkoxycarbonyl and R.sub.9 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.3 and R.sub.4 are hydrogen or taken together with the carbon atoms to which they are attached form a double bond; R.sub.6 and R.sub.7 are independently H, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.
Type:
Grant
Filed:
May 23, 1995
Date of Patent:
June 18, 1996
Assignee:
American Home Products Corporation
Inventors:
Thomas J. Commons, Christa M. LaClair, Susan Christman
Abstract: New therapeutic agent of carboxymethylidenecycloheptimidazole derivatives and method for the manufacture thereof are disclosed, which are represented by the following formula or its alkali addition salts ##STR1## (wherein R.sub.1 represents a lower alkyl; R.sub.2 represents H or isopropyl group; R.sub.3 represent H, a lower alkyl or --C(CH.sub.3)H--OCOOR.sub.4 (R.sub.4 is a lower alkyl or cyclohexyl) and .dbd.CHCOOR.sub.3 is substituted group at 4 or 8 position; A represents ##STR2## These compounds are useful as anti-hypertensive, anti-congestive heart failure agents and intraocular pressure lowering agents.
Abstract: The invention relates to compounds of the formula (I) ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are, independently of one another, hydrogen, CF.sub.3, NO.sub.2, CN, halogen, --S(NSO.sub.2 CF.sub.3)CF.sub.3, (C.sub.1 -C.sub.4)-alkyl, phenyl, SO.sub.2 R.sup.5, COOR.sup.5, NR.sub.2.sup.5, where R.sup.5 is (C.sub.1 -C.sub.4)-alkyl, which can also be fluorinated, or phenyl, or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3 or R.sup.3 and R.sup.4 together form an aliphatic or aromatic ring which can also contain an oxygen, sulfur or nitrogen atom.The invention further provides a process for preparing the compounds of the formula (I), which comprises reacting compounds of the formula (II) ##STR2## where R.sup.1 to R.sup.4 are as defined above and X is hydrogen or an alkali metal, with elemental fluorine in the presence of an inert solvent and, if desired, an alkali metal fluoride at low temperatures.
Abstract: Ethylene glycol carbonate (EGC) can be isolated in purified form from contaminated material which contains impurities from the group comprising starting materials, by-products and/or catalysts of the preparation process in that the contaminated EGC is subjected to a fractional melt crystallization and the crystals of the purified EGC formed in this case are mechanically separated off from the remaining impurities dissolved in the residual melt.
Type:
Grant
Filed:
July 18, 1994
Date of Patent:
April 23, 1996
Assignee:
Bayer Aktiengesellschaft
Inventors:
Christine Mendoza-Frohn, Paul Wagner, Hans-Peter Wirges
Abstract: .beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is -O-, -S-, or -NR.sub.2 -, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.
Type:
Grant
Filed:
December 19, 1994
Date of Patent:
April 23, 1996
Assignee:
Warner-Lambert Company
Inventors:
Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
Abstract: A process for the preparation of 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride (terazosin hydrochloride dihydrate comprises the steps of reacting 4-amino-2-chloro-6,7-dimethoxy-quinazoline with N-(2-tetrahydrofuroyl)piperazine in an anhydrous polar organic solvent in the absence of an added acid scavenger to produce anhydrous 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride (Form IV) and thereafter converting the product of that step to 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)-piperazine hydrochloride dihydrate.
Type:
Grant
Filed:
October 18, 1994
Date of Patent:
April 2, 1996
Assignee:
Abbott Laboratories
Inventors:
Anthony Mannino, Rodger F. Henry, Wayne R. Heitmann, Bruce W. Horrom
Abstract: Phosphinic acid derivatives of the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, alkyl, alkenyl, alkenylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, carboxyalkyl, thioalkyl, alkoxythioalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl-substituted alkyl or heterocycloalkyl; or R.sub.1 and R.sub.2 form a cycloalkyl ring of 3-8 members and R.sub.3 and R.sub.4 are as defined; or R.sub.3 and R.sub.4 form a cycloalkyl ring of 3-7 members and R.sub.1 and R.sub.2 are as defined; or R.sub.1 and R.sub.2 together, and R.sub.3 and R.sub.4 together, each form a cycloalkyl ring;R.sub.5 is --OR.sub.9 or --NHR.sub.9, wherein R.sub.9 is hydrogen or alkyl;n is 0 or 1;A.sub.1 is p-aminobenzoyl or p-aminobenzenesulfonyl, or A.sub.1 and R.sub.5 together form a radical of an .alpha.-aminoacyl derivative; andR.sub.6 is phenylmethoxycarbonyl, arylcarbonyl, heteroarylcarbonyl or --A.sub.2 --R.sub.
Type:
Grant
Filed:
June 29, 1994
Date of Patent:
December 19, 1995
Assignee:
Schering Corporation
Inventors:
Brian A. McKittrick, Michael F. Czarniecki, Samuel Chackalamannil, Shin Chung, Shawn DeFrees, Andrew W. Stamford