Abstract: Disclosed are novel 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof.Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.
Type:
Grant
Filed:
November 27, 1990
Date of Patent:
July 21, 1992
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Abstract: Polytetrahydrofuran derivatives of the general formula ##STR1## where n is from 2 to 70, X is the bridge member --NH-- or --O-- and R.sup.1 and R.sup.4 are each hydrogen or various radicals.
Abstract: Aryl-sulfur pentafluorides of the formula I ##STR1## wherein R, A, Z, n, m and X.degree. have the meaning indicated in claim 1 are suitable for use as components of liquid-crystal phases for field-effect and/or bi-stability effect displays.
Type:
Grant
Filed:
December 27, 1989
Date of Patent:
October 8, 1991
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Volker Reiffenrath, Rudolf Eidenschink, Georg Weber
Abstract: Oligomeric carbonate dihydroxyaromatic-based chainstoppers are disclosed. One example of this type of chainstopper is a bisphenol A bischloroformate oligomer monocapped with phenol. These chainstoppers may be prepared by phosgenating a dihydroxyaromatic compound to terminate one or both of the terminal oxygen atoms with chlorocarbonyl groups, followed by reaction of the chlorocarbonyl-terminated material with a phenolic-type compound in the presence of an amine catalyst. The chainstoppers of the present invention are very useful in accurately controlling the molecular weight of polycarbonates formed by various processes, while also preventing the formation of undesirable by-products, such as diarylcarbonates.
Abstract: Disclosed are novel oxazolidinedione derivatives expressed by the following formula: ##STR1## (R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 being defined in the specification), a method of producing the derivatives and herbicides containing the derivatives as an active ingredient. Carbonate esters which are intermediates in the method of producing the oxazolidinedione derivatives are also disclosed.These novel derivatives exhibit excellent weed-killing activity for harmful weeds and low phytotoxicity for crops.
Type:
Grant
Filed:
January 31, 1989
Date of Patent:
January 8, 1991
Assignees:
Sagami Chemical Research Center, Chisso Corporation, Kaken Pharmaceutical Co. Ltd.
Abstract: The present invention relates to 3-aminomethyl derivatives of indane, dihydrobenzofurane, dihydrobenzothiophene, and indoline, acid addition salts thereof, isomers thereof, methods of preparation, pharmaceutical compositions and method of treating CNS-disorders such as schizophrenia, Parkinson's disease, depression, anxiety, migraine and senile dementia, or in the cure of cardiovascular diseases, by administering such a derivative.
Abstract: This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.
Type:
Grant
Filed:
March 12, 1987
Date of Patent:
June 12, 1990
Assignee:
Boehringer Mannheim GmbH
Inventors:
Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuhnle
Abstract: Liquid Crystal compounds represented by the following formula are disclosed. ##STR1## wherein R and R' are independently selected from alkyl groups containing 1.about.20 carbon atoms; X is --O--, --O--CO--O-- or direct bond; A.sub.1 and A.sub.2 are independently cyclic groups (such as phenylene and biphenylene), said cyclic groups may be substituted with 1.about.4 fluorine, chlorine or bromine atoms, or 1 or 2 substituent groups selected from the group consisting of cyano, nitro and trifluoromethyl groups; Y is --CO--O--, --O--CO--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.dbd.N--, --N.dbd.CH--, --N.dbd.N--, --CH.sub.2 S--, --SCH.sub.2 -- or direct bond; and * represents asymmetric atom providing optical activity.
Type:
Grant
Filed:
August 19, 1988
Date of Patent:
May 1, 1990
Assignees:
NEC Corporation, Sanyo Chemical Industries, Ltd.
Abstract: The present invention relates to aromatic derivatives of the formula: ##STR1## in which: n represents an integer between 2 and 10;R.sub.1 and R.sub.2 are identical or different and represent a cycloalkyl containing 3 to 6 carbon atoms or an alkyl containing from 1 to 6 carbon atoms which is unsubstituted or substituted by a phenyl or benzyl group; orR.sub.1 and R.sub.2, together with the nitrogen atom to which they are bonded, form a heterocycle selected from pyrrolidin-1-yl, piperidino, azepin-1-yl, hexamethyleneimino, 4-methylpiperidino, 4-benzylpiperidino, 4-phenylpiperidino, 1,2,3,4-tetrahydroisoquinol-2-yl, morpholino and imidazol-1-yl groups;R.sub.3 represents a hydrogen, a halogen, a methyl or a phenyl;R.sub.4 represents a hydrogen, a halogen or a methyl; or R.sub.3 and R.sub.4, taken together with the benzene ring to which they are bonded, form a naphth-1-yl or naphth-2-yl group;Y represents a direct bond, a methyleneoxy group, a methylenethio group or a vinylene group; andR.sub.
Abstract: This invention relates to a new one-step process for preparation of novel N-(acyloxyalkoxy)carbonyl derivatives useful as bioreversible prodrug moieties for drugs having a primary or secondary amine function thereon.
Abstract: The invention relates to a new process for preparing active esters or carboyxlic acids, which consists in reacting a carboxylic acid, in the presence of an agent for binding hydrohalic acid, with a carbonate of formula: ##STR1## in which R.sup.1 denotes either a radical of formula ##STR2## in which R.sup.3 and R.sup.4, which may be identical or different, are not hydrogen atoms and denote organic radicals which may be substituted or unsubstituted and saturated or unsaturated, and may or may not be bound to a polymer, and which can be joined together to form a hetero-cyclic system with the nitrogen, atom,or a substituted or unsubstituted aryl radical which may or may not be bound to a polymer,R.sup.2 denotes a hydrogen atom, an aliphatic or cycloaliphatic radical which may be substituted or unsubstituted and saturated or unsaturated, or a substituted or unsubstituted aromatic radical,and X denotes a halogen atom.This process is especially useful for the synthesis of active esters of N-protected amino acids.
Type:
Grant
Filed:
September 13, 1988
Date of Patent:
January 2, 1990
Assignee:
Societe Internationale Des Poudres et Explosifs
Abstract: The invention relates to new .alpha.-chlorinated carbonates characterized in that their formula is: ##STR1## in which X is a fluorine, chlorine or bromine atom and R.sup.1 is different from the ##STR2## group and represents; a substituted or non-substituted, saturated or unsaturated, aliphatic, araliphatic, primary, secondary, tertiary or cycloaliphatic radical.These .alpha.-chlorinated carbonates are prepared by the action of a compound of formula R.sup.1 OH on a chloroformate of formula: ##STR3## in a solvent medium in the presence of an acid scavenger which is added after the two preceding compounds.They are used to block the amine function of amino acids. The .alpha.-chlorinated carbonate and amino acid are reacted in a solvent medium at a temperature of -5.degree. to 100.degree. C. in the presence of an acid scavenger. Blocked amines are very useful in peptide synthesis.
Type:
Grant
Filed:
February 14, 1985
Date of Patent:
March 24, 1987
Assignee:
Societe Nationale des Poudres et Explosifs