Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) or (II): ##STR1## and pharmaceutically acceptable salts thereof the compounds of the formula (II) in which R is hydrogen are disclosed.
Type:
Grant
Filed:
April 28, 1986
Date of Patent:
April 19, 1988
Assignee:
Merck & Co., Inc.
Inventors:
Byron H. Arison, Michael D. Greenspan, Joel B. Yudkovitz
Abstract: There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.
Type:
Grant
Filed:
May 14, 1985
Date of Patent:
April 5, 1988
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Wolfgang Grell, Gerhart Griss, Robert Sauter, Rudolf Hurnaus, Eckhard Rupprecht, Nikolaus Kaubisch, Joachim Kahling, Bernhard Eisele
Abstract: A method for producing .alpha.,.alpha.-dimethyl-.delta.-valerolactone which comprises carrying out the addition reaction of hydrogen bromide and 2,2-dimethyl-4-pentenoic acid in the presence or absence of a catalyst to synthesize 2,2-dimethyl-5-bromovaleric acid which is then subjected to ring-closure reaction by alkali treatment.
Type:
Grant
Filed:
October 16, 1986
Date of Patent:
March 29, 1988
Assignee:
Nitto Chemical Industry Co., Ltd.
Inventors:
Takeshi Inagaki, Tuyoshi Irie, Katsumi Nakamura, Denzi Sato
Abstract: A substance is provided which has strong enzyme inhibitory activity against thiol proteases such as papain, ficin, bromelain, etc. and which is represented by the following formula: ##STR1## (wherein R is a hydrogen atom or a hydroxyl group), its pharmaceutically acceptable salt or hydrate.
Abstract: Compounds of the formula ##STR1## are described wherein X is a C.sup.2-11 -alkyl group, optionally substituted by a protected hydroxy, protected oxo or protected carboxy group.
Abstract: A process for making highly pure cyclic esters by heating a copolymer of .alpha.-hydroxy acid or its ester on a thermally stable polyether core.
Abstract: The invention provides a process for epoxidizing an olefinic double bond in an olefinically-unsaturated compound by contact of a liquid phase mixture containing the olefinically-unsaturated compound, an aldehyde having at least two carbon atoms and a suitable solvent with molecular oxygen in the presence of a catalyst which is soluble in the reaction mixture and which comprises a praseodymium compound. The process has particularly advantageous application to oxidation of aldrin to dieldrin.
Abstract: The catalytic thermal depolymerization of polyesters to produce macrocyclic esters suitable for fragrance applications is carried out using an olefin polymer. High yields of the corresponding macrocyclic ester are produced at high rates while substantially eliminating reactor fouling and the formation of undesirable by-products. The depolymerization is most advantageously conducted using polyethylene.
Type:
Grant
Filed:
September 19, 1986
Date of Patent:
November 24, 1987
Assignee:
National Distillers and Chemical Corporation
Inventors:
Joseph Cahill, Jr., Herbert G. Rodenberg
Abstract: A method of preparing certain 2-halo-5-methylpyridines, useful as herbicide intermediates, is presented starting from acyclic pentenes. The pentene is difunctionalized, e.g., by making the epoxide, and is then reacted with a nitrogen source to close the ring. The nitrogen-containing 6-membered heterocycle may then be aromatized readily to produce the 2-halo-5-methylpyridine desired. Also part of the invention are novel acyclic and cyclic intermediates used in the process.
Abstract: A substituted trifluorooxetane of the formula: ##STR1## wherein R.sub.f is a C.sub.1 -C.sub.10 perfluoroalkyl group and n is 0, 1 or 2, which is useful as a solvent or a monomer.
Abstract: A glycidyl compound having the formula (I): ##STR1## wherein R is hydrogen atom or methyl group, p is an integer of 1 to 4 and Ar is aromatic hydrocarbon group selected from the group consisting of groups having the formula (II), (III) and (IV): ##STR2## wherein R.sup.1 R.sup.2 are the same or different and each is an alkyl group having 1 to 4 carbon atoms.The glycidyl compound can be cured by either heat, radical initiators or irradiation of ultraviolet rays and curing compounds prepared by using the glycidyl compound have high heat resistance and high surface hardness.
Abstract: Fatty acid esters of ascorbic acid are prepared by a process in which a homogeneous mixture of(a) ascorbic acid,(c) concentrated sulfuric acid having a concentration of not less than 96% and(c) a methyl or ethyl ester of a fatty acid of 12 to 18 carbon atomsis reacted at from 20.degree. to 50.degree. C.Using the novel process, the fatty acid esters of ascorbic acid, in particular ascorbyl palmitate, which are very desirable antioxidants are obtained by a procedure which is technically simpler and hence cheaper than the conventional processes, but in equally good yields.
Abstract: The present invention relates to new derivatives of (2,4,6-trimethoxyphenyl)-(3-piperidinopropyl)-ketone which are selected from the group consisting of:(i) (2,4,6-trimethoxyphenyl)-[3-(alkylpiperidino)-propyl)]-ketones of general formula: ##STR1## wherein R.sub.1 is CH.sub.3 or C.sub.2 H.sub.5 in 2- or 3-position of the piperidine ring, andR.sub.2 is H, CH.sub.3 or C.sub.2 H.sub.5 ; and(ii) their addition salts. These new derivatives are useful in therapeutics.
Abstract: This invention relates to 8-chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-[(substituted phenylsulfinyl)alkanoyl]hydrazides and 8-chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-[(substituted phenylsulfonyl)alkanoyl]hydrazides that are useful as prostaglandin antagonists and analgesic agents. This invention also relates to 8-chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-[(substituted phenylthio)alkanoyl]hydrazides that are useful as intermediates in the preparation of the corresponding sulfinyl and sulfonyl compounds.
Abstract: A process for the production of epichlorohydrin is disclosed which comprises reacting allyl chloride, chlorine and water to form an intermediate, then rapid conversion and separation of epichlorohydrin product; the epichlorohydrin-depleted reaction mixture is cooled and subjected to electrodialysis then reverse osmosis to concentrate and remove deleterious by-products, and at least a substantial portion of the resultant permeate is recycled to the reaction zone, thereby enabling reduced operating costs and/or improved yield.
Abstract: The invention relates to a process for the continuous preparation of trioxane, optionally together with cyclic formals, from an aqueous formaldehyde solution in the presence of acidic solid-bed catalysts, the reaction taking place without simultaneous evaporation.The process according to the invention can be carried out even at high formaldehyde concentrations without appreciable paraformaldehyde deposits.
Abstract: A composition comprising an aromatic polycarbonate branched or crosslinked with a residue of a compound of the formula ##STR1## wherein X, Y, X' and Y' are the same or different and are hydrogen or alkyl of one to about six carbon atoms, inclusive; W, W', Z and Z' are the same or different and are alkyl of one to about six carbon atoms, inclusive, and E is alkylene or alkylidene of two to about twelve carbon atoms, inclusive.
Abstract: Compounds of general formula ##STR1## in which R.sub.1, taken separately, denotes a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, andR.sub.2, taken separately, denotes a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or a phenylthio or phenylsulphonyl group, or alternativelyR.sub.1 and R.sub.2 together form an ethano bridge or, together with the two carbon atoms 8 and 9, form a fused benzene ring,R.sub.3 denotes a hydrogen atom or a methyl group andR.sub.4 denotes a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or a cation of a base which is acceptable in pharmacology, the group CH(R.sub.3)COOR.sub.4 being at position 2 or 3. have uses in treatment of inflammation, pain and undesirable platelet aggregation.
Abstract: The local anesthetic, L-N-n-propylpipecolic acid-2,6-xylidide, namely: ##STR1## This compound is prepared by chlorinating L-pipecolic acid to yield the acid chloride, namely L-pipecolic acid chloride. The acid chloride is then reacted with 2,6-xylidine to yield L-pipecolic acid-2,6-xylidide. The L-N-pipecolic acid-2,6-xylidide is then propylated to yield the L-N-n-propylpipecolic acid-2,6-xylidide, which is a potent local anesthetic for humans and is of relatively low toxicity.
Abstract: A fluoran compound represented by general formula (I): ##STR1## wherein R.sub.1 represents a straight or branched alkyl group having 1 to 8 carbon atoms, a cyclohexyl (C.sub.1 -C.sub.2) alkyl group, a cyclohexyl group, a phenyl group which may be substituted by chlorine, an alkoxyalkyl group, a benzyl group which may be substituted by chlorine, or a hydrogen atom;, R.sub.2 represents a hydrogen atom, a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a phenyl group which may be substituted by chlorine, a benzyl group which may be substituted by chlorine, a lower alkoxy group or a lower alkoxyalkyl group; R.sub.3 represents a hydrogen atom, a chlorine atom, a fluorine atom or a lower alkyl group having 1 to 4 carbon atoms; and n is 2.