Abstract: Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## the amido ester moiety of which is in the L-configuration, and pharmaceutically acceptable salts thereof are disclosed.
Type:
Grant
Filed:
September 2, 1986
Date of Patent:
July 7, 1987
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Wasyl Halczenko, George Hartman, Steven M. Pitzenberger
Abstract: Products of formula (I) ##STR1## in which R=C.sub.6-18 aromatic or alkylaromatic of valency z, R'=H, C.sub.1-16 alkyl or phenyl, A=CH.sub.2 or CH.sub.2 --O-- and, in the latter case, R'.noteq.H, x=1-8, y=1-20, z=1-3 and T denotes one or more anionic groups or a mixture of anionic groups and non-ionic groups are disclosed.These compounds are prepared by the reaction of a phenol R(OH).sub.z with an epoxide ##STR2## and an epihalogenohydrin ##STR3## in which X=Cl or Br, this being followed by replacement of X with one or more hydrophilic groupsThese compounds can be used as surface-active agents.
Abstract: Vinyl ether monomers of the formula ##STR1## wherein n is 0 or 1 and R is CH.sub.3 or C.sub.2 H.sub.5, precursors thereto, and copolymers with, e.g., tetrafluoroethylene, are provided. The copolymers are useful as electrical insulation and as the sheath portion of optical fibers, and can be converted to known ion exchange polymers having carboxylic groups which are useful, e.g., in the form of permionic membrane for separating the compartments of a chloralkali cell. The vinyl ether monomers can also be converted to vinyl ether monomers which contain carboxylate functional groups, which in turn can be copolymerized to useful copolymers.
Abstract: The present invention relates to methods for the preparation of anilinofumarate, a useful intermediate in the preparation of quinoline-2,3-dicarboxylic acid and in the preparation of 2-(2-imidazolin-z-yl) quinoline-3-carboxylic acid herbicidal agents.
Abstract: Crystalline salts of (R,S)-pivaloyloxyethyl esters of (S)-3-(3,4-dihydroxyphenyl)-2-methylalanine and processes for their preparation are disclosed.
Abstract: Synthesis gas is produced by the partial oxidation of a feedstock comprising petroleum coke and/or heavy liquid hydrocarbonaceous fuel containing sulfur and having an ash that contains nickel, vanadium and a comparatively high level of silicon. An iron and calcium-containing additive is introduced into the reaction zone along wth the feed. Separate portions of the additive (i) combine with a portion of the nickel, calcium and sulfur to generate a liquid phase washing agent that collects and transports out of the gas generator a portion of the vanadium-containing oxide laths and spinels and other ash components; and (ii) combine with a portion of the nickel, calcium and silicon to generate a liquid oxide-silicate phase that fluxes e.g. dissolves substantially all of the remaining portion of said vanadium-containing oxide laths and spinels and other ash components.
Abstract: Polythioalkanecarboxylic products of formula: ##STR1## in which R.sub.1 =C.sub.6-30 aromatic or alkylaromatic radical; R.sub.2 =C.sub.4 -C.sub.18 alkyl; A=C.sub.1-3 alkylene; M=H, alkali metal or alkaline earth metal, an ammonium ion or a substituted ammonium ion; z=1-6; m=1-10; n=1-20; and u=zero or 1 are disclosed.A process of preparation comprising, in a first stage, reacting an alcohol or phenol of formula R.sub.1 (OH) .sub.z (II) with an epihalogenohydrin of formula ##STR2## in which X=Cl or Br, in the presence of a Lewis acid, to give the intermediates of the formula: ##STR3## and in a second stage, the two compounds of formulae R.sub.2 SH (V) and HS--A--COOH (VI), in which R.sub.2 and A have the meanings indicated above, are reacted simultaneously or successively with the compound of the formula (IV) is also disclosed.The compounds of the formula (I) are used in cosmetic compositions.
Abstract: Synthesis gas is produced by the partial oxidation of a feedstock comprising petroleum coke and/or heavy liquid hydrocarbonaceous fuel containing sulfur and having an ash that contains nickel, vanadium and a comparatively low level of silicon. An iron-containing additive is introduced into the reaction zone along with the feed. The additive combines with at least a portion of the nickel constituents and sulfur found in the feedstock to produce a liquid phase washing agent that collects and transports at least a portion of the vanadium-containing oxide laths and spinels and other ash components out of the reaction zone. In another embodiment, a minor amount of an additional material selected from the group of elements consisting of magnesium, chromium and mixtures thereof is included in the iron-containing additive. In still another embodiment, the iron-containing additive is uniformly dispersed in petroleum coke having a nickel and vanadium-containing ash.
Abstract: A method for preparing an important stereo-specific intermediate in the synthesis of prostaglandin analogs is disclosed. Said intermediate is (+)S-2-hydroxy-2-methyl-hexanoic acid and is prepared via an asymmetric halolactonization reaction utilizing L-proline as the chiral agent.
Abstract: Disclosed is a method for preparation of alkoxymethylene compounds, especially methoxymethylene compounds, from substituted or unsubstituted acetic acid alkyl esters, especially methyl esters, from the corresponding hydroxymethylene compounds or their alkali salts, by reaction with excess alkanol, especially methanol, in the presence of HCl and a water-binding agent. Preferred are water-binding agents which form stable reaction products with water.
Abstract: Diphenylazomethine derivatives of formula (I) ##STR1## wherein R.sub.1 is hydrogen or methyl and R.sub.2 is an --OH,--OM (M=alkaline metal or alkaline earth metal), --NH.sub.2 or --O(C.sub.1-4 alkyl) group, and which are in the form of cis or trans isomers or mixtures thereof, have central nervous system activity and can be used as antidepressants and anticonvulsants.
Abstract: This invention is concerned with new .beta.-[2-(halogenobenzyl)-phenoxy]-ylamine derivatives of the general formula ##STR1## wherein R represents a C.sub.1 -C.sub.8 -alkyl group having a linear or branched hydrocarbon chain,R.sub.1 and R.sub.2, which may identical or different, represent each a C.sub.1 -C.sub.4 -alkyl-group, andAr represents a polychlorophenyl group of the formula ##STR2## (in which Y.sub.1 is 4-Cl, Y.sub.2 is H or Cl, and Y.sub.3 is H or Cl, at least one of the Y.sub.2 and Y.sub.3 being Cl); and their addition salts.These new compounds are useful as pharmaceuticals.
Type:
Grant
Filed:
November 27, 1984
Date of Patent:
April 21, 1987
Assignee:
Institut de Recherches Chimiques et Biologiques Appliquees (I.R.C.E.B.A)
Abstract: A process for the preparation of 5,6-dialkoxyanthranilic acids is described. The 5,6-dialkoxyanthranilic acids are useful in the preparation of substituted quinazolinediones which are active cardiotonic agents.
Abstract: An aqueous dispersion of unreacted particulate petroleum coke substantially comprising carbon and containing a small amount of ash substantially comprising vanadium constituents and other materials from a process for the partial oxidation of petroleum coke to produce synthesis gas is mixed with a K.sup.+ amyl xanthate vanadium collection agent and a frothing agent. After pH adjustment, if necessary, the mixture is subjected to aeration with or without mechanical agitation in a froth flotation zone. About 70 to 95 wt. % of the unconverted particulate petroleum coke particles (basis carbon) float in the froth layer that is formed. The remainder of the unconverted petroleum coke comprising coarser particles is suspended in a bottom aqueous dispersion on which the froth layer floats. In addition, selective separation of the vanadium constituents in the unconverted petroleum coke ash takes place.
Type:
Grant
Filed:
April 26, 1985
Date of Patent:
April 14, 1987
Assignee:
Texaco Inc.
Inventors:
Stephen R. Vasconcellos, Mitri S. Najjar, James R. Pascoe
Abstract: Carbonamides are prepared from carboxylic acids and ammonia in the presence of a catalytic amount of a hydrated oxide.Preferably a hydrated titanium-, zirconium- or tin oxide in an amount between 0.05 to 10% by weight is used. The hydrated oxide contains at least 4% of water.
Type:
Grant
Filed:
July 3, 1984
Date of Patent:
April 7, 1987
Assignee:
Internationale Octrooi Maatschappij "Octropa" B.V.
Inventors:
Teunis Eikelboom, John A. Rand, Pieter M. van Dijk
Abstract: A simple single step process for preparing alkyl and substituted alkyl esters of amino acids is described. The products are bioactive compounds including compounds useful as antihypertensive agents.
Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: W are selected from the group consisting of:the groups R.sup.5 --CO-- and R.sup.5 --CS-- wherein: R.sup.5 is selected from alkenyl, alkynyl, benzyl, phenyl, substituted alkyl, substituted alkenyl, substituted alkynyl, substituted benzyl, substituted phenyl and the acetal, hemiacetal, oxime, imine and Schiff base derivatives of the group R.sup.5 --CO--;the groups Y--CO-- and Y--CS-- wherein Y is selected from hydroxy, mercapto, alkylthio and the groups MO-- and MS-- wherein M is an organic or an inorganic cation;the groups R.sup.6 R.sup.7 NCO-- and R.sup.6 R.sup.7 NCS-- wherein R.sup.6 and R.sup.7 are independently selected from hydrogen, alkyl, substituted alkyl, alkanoyl, carboxy, alkoxycarbonyl, alkylsulfonyl, benzoyl, benzenesulfonyl, substituted benzoyl, substituted benzenesulfonyl, or R.sup.6 and R.sup.
Type:
Grant
Filed:
July 2, 1984
Date of Patent:
March 24, 1987
Assignee:
ICI Australia Limited
Inventors:
Keith G. Watson, Graham J. Bird, Graeme J. Farquharson
Abstract: The invention is directed to a process for the production of monoperoxydicarboxylic acids and their alkali or alkaline earth metals by reacting the corresponding anhydride with hydrogen peroxide in an organic solvent which dissolves the corresponding peracid and in the presence of an anion exchanger.
Abstract: Provided herein is a butanediol of the formula: ##STR1## wherein R is an alkyl group containing 5-21 carbon atoms or an alkenyl group containing 5-21 carbon atoms and which contains 1-2 unsaturated bonds. The present invention also contemplates a method of preparing such compounds and the use of such compounds as an anti-tumor agent for treating tumors.