Abstract: This invention relates to a process for obtaining 10-deacetylbaccatin III from various parts of yew (Taxus sp.) by extraction with a suitable organic solvent of the aqueous solution obtained after treating the appropriate part of yew with water, followed by selective crystallization of 10-deacetylbaccatin III.
Abstract: Compounds of the formula ##STR1## in which R.sub.1 is halogen, C.sub.1 -C.sub.3 alkyl, halo-C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halo-C.sub.1 -C.sub.3 alkoxy or cyano and/or two substituents R.sub.1 which are bonded to adjacent C atoms of the phenyl ring together are --O--CH.sub.2 --O--; R.sub.2 is hydrogen, halogen or methyl;R.sub.3 is fluorine, chlorine, bromine or C.sub.1 -C.sub.3 alkyl; R.sub.4 is hydrogen or C.sub.1 -C.sub.3 alkyl;either R.sub.5 is hydrogen, C.sub.1 -C.sub.4 alkyl, ##STR2## --COCO--R.sub.8,--CO--R.sub.9 or S(O).sub.m --N(R.sub.10)--COO--R.sub.11 andR.sub.6 is C.sub.1 -C.sub.6 alkyl, halo-C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.6 alkenyl, halo-C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.5 alkynyl, halo-C.sub.3 -C.sub.5 alkynyl, C.sub.1 -C.sub.3 alkoxy-C.sub.1 -C.sub.3 alkyl, C.sub.3 -C.sub.6 cycloalkyl, unsubstituted or substituted phenyl; or R.sub.5 and R.sub.6 together are --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --; R.sub.7 is hydrogen, halogen or C.sub.1 -C.sub.3 alkyl; R.
Abstract: A method is disclosed for the production of .alpha.-APM.HCl by treating an F-.alpha.-AP derivative with a mixed solvent of methanol, hydrochloric acid and water, wherein the solubility of .alpha.-APM.HCl is lowered to increase the separation yield thereof.
Abstract: This invention relates to new ethanolamine derivatives having gut selective sympathomimetic and anti-pollakiuria activities and represented by the general formula [I]: ##STR1## wherein R.sup.1 is aryl or a heterocyclic group, each of which may be substituted with halogen, etc.,R.sup.2 is hydrogen, halogen, nitro, hydroxy, lower alkyl optionally substituted with acyl, lower alkenyl optionally substituted with acyl, lower alkoxy optionally substituted with acyl, or amino optionally substituted with acyl(lower)alkyl,R.sup.3 is hydrogen, an N-protective group, or lower alkyl optionally substituted with lower alkylthio,n is an integer of 0 to 3, anda heavy solid line means a single bond or a double bond,provided that when n is 1, then1) R.sup.1 is a condensed aromatic hydrocarbon group or a heterocyclic group, each of which may be substituted with halogen, etc.
Abstract: There are provided novel aminophosphonic acid derivatives of the general formula [I]: ##STR1## wherein n is an integer of 2 or 3; R.sup.1 is a phenyl, naphthyl, indolyl, benzothienyl, benzofuryl or benzoxazolyl group which may have 1 to 3 substituents selected from the group consisting of hydroxyl and lower alkyloxy groups, or a hydrogen atom; R.sup.2 is a lower alkyl group, a benzyl group, a 4-hydroxybenzyl group, a 3-indolylmethyl group or a .beta.-phenethyl group; and A is an optional residue of an amino acid selected from the group consisting of tryptophane, tyrosine, phenylalanine, homophenylalanine, naphthylalanine or N.sup..omega. -nitroarginine, and their pharmaceutically acceptable salts. The compounds according to the present invention and their pharmaceutically acceptable salts exhibit an inhibitory activity against endothelin-converting enzyme, and are expected to be useful as a drug treating various diseases with which endothelin is concerned.
Abstract: A process for producing an aromatic carbonate which comprises:reacting(a) an aromatic hydroxy compound with(b) carbon monoxide in the presence of(c) an oxidation agent,(d) a catalyst comprising a palladium compound or impregnated palladium catalyst,(e) a co-catalyst comprising a manganese compound, a cobalt compound or a copper compound, and(f) at least one nitrile compoundat a temperature of 20.degree. to 300.degree. C.
Abstract: This invention relates to a composition for and method of storing and using acetic acid or propionic acid, the composition comprising an alkali(ne earth) metal salt of acetic acid or propionic acid and an aliphatic carboxylic acid which has a pKa value lower than that of acetic acid or propionic acid respectively. When this composition is brought into contact with a solvent system capable of allowing ionisation of the salt and the aliphatic carboxylic acid, free acetic acid or propionic acid is released in situ. This method enables the free acids to be stored and released at the point of use thereby substantially reducing the risks of corrosion and unpleasant odors.
Abstract: A process for the preparation of an alkoxyalkanoic acid by reacting the corresponding alkoxyalkanol with a stable free radical nitroxide in the presence of a NO.sub.x -generating compound, a solvent and an oxidant, at a temperature in the range of from about 0.degree. C. to about 100.degree. C. and thereafter separating out the alkoxyalkanoic acid.
Abstract: An azole compound represented by the formula (I): ##STR1## wherein Ar is a substituted phenyl group;R.sup.1 and R.sup.2 independently are a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 may combine together to form a lower alkylene group;R.sup.3 is a group bonded through a carbon atom;R.sup.4 is a hydrogen atom or an acyl group;X is a nitrogen atom or a methine group; and nY and Z independently are a nitrogen atom or a methine group which may optionally be substituted with a lower alkyl group, or a salt thereof, which is useful for prevention and therapy of fungal infections of mammals as antifungal agent.
Abstract: A method is provided to improve the quality of recycle of certain residues by modifying the separation of alkanes and alkane-like materials and carbonyl-containing impurities from the recycle during the manufacture of acetic acid by the carbonylation of methanol. The improvement comprises operating a prior art stripper column in a reflux manner and partitioning the residue therefrom by the addition of water. The method also reduces the volume of disposal of potentially valuable recyclable reactants.
Type:
Grant
Filed:
April 26, 1993
Date of Patent:
December 6, 1994
Assignee:
Hoechst Celanese Corporation
Inventors:
George A. Blay, Madan Singh, Mark O. Scates, Wayne D. Picard
Abstract: A compound of the formula ##STR1## its pharmaceutically acceptable salts, and its pharmaceutically acceptable hydrolyzable esters for reducing sebum secretion and combatting acne as well as oral and topical compositions for use thereof.
Type:
Grant
Filed:
January 6, 1993
Date of Patent:
November 29, 1994
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Thomas I. Doran, Michael Rosenberger, Stanley S. Shapiro
Abstract: Dialkyl carbonates can be prepared by the reaction of carbon monoxide with alkyl nitrites in a continuous gas phase reaction, using a platinum group metal catalyst on an alumosilicate zeolite having acidic centers, preferably in the H.sup.+ form, as a support, which catalyst may optionally comprise additional material of a compound of antimony, bismuth, aluminum, copper, vanadium, niobium, tantalum, tin, iron, cobalt, nickel or a mixture of a plurality of these, and hydrogen halide being added in the course of the reaction intermittently or continuously. In this reaction, the dialkyl carbonates are formed with almost quantitative selectivity; the corresponding dialkyl oxalates cannot be detected in most cases.
Type:
Grant
Filed:
February 26, 1993
Date of Patent:
November 1, 1994
Assignee:
Bayer Aktiengesellschaft
Inventors:
Erich Wolters, Heinz Landscheidt, Alexander Klausener, Lothar Puppe
Abstract: The invention relates a process for the carbonylation of epoxides by reaction with carbon monoxide in the presence of a catalyst system containing a source of cobalt and a hydroxy substituted pyridine compound, whereby .beta.-propiolactones and/or derivatives thereof, such as .beta.-propiolactone polymers, .beta.-hydroxy carboxylic acids and esters, and .beta.-alkoxy carboxylic acids and esters, are produced.
Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
Abstract: An unsaturated ester monomer having the structure: ##STR1## wherein R.sup.1 is hydrogen or methyl; R.sup.2, R.sup.3 and R.sup.4 are each independently lower alkyl of 1 to about 4 carbons; and Z is nothing or is a divalent radical having 1 to about 20 carbons.
Abstract: A process for producing alkylene carbonates which comprises reacting urea and glycols described by the general formula RCH(OH) CH.sub.2 OH; wherein R represents hydrogen or an alkyl group containing 1 to 4 carbons, using a catalyst containing zinc, magnesium, lead or calcium at reduced pressures. The alkylene carbonates are produced with high yield easily using raw materials which are comparatively inexpensive with a mild reaction that does not involve explosive or hazardous materials.
Abstract: A catalytic process for alkylating an alkali metal selected from lithium, sodium and potassium with an alkyl halide containing 3 to 20 carbon atoms comprising conducting the reaction in the presence of a catalytic compound represented by the formula(RR.sup.1 R.sup.2 M.sup.a).sub.y A(R.sup.3).sub.xwherein R, R.sup.1 and R.sup.2 are independently selected from hydrogen, halogen, alkyl, alkenyl, cycloalkyl, and aryl groups, R.sup.3 is independently selected from alkyl groups containing 1 to 10 carbon atoms, alkylene groups containing 2 to 5 carbon atoms, aryl groups containing 6 to 18 carbon atoms, four to six-membered heterocyclic carbon containing groups containing one to two hetero atoms selected from oxygen, nitrogen, and sulfur; hydroxyalkyl, alkoxyalkyl and monoalkylaminoalkyl and dialkylaminoalkyl groups containing 2 to 13 carbon atoms; M.sup.
Type:
Grant
Filed:
March 23, 1993
Date of Patent:
August 23, 1994
Assignee:
FMC Corporation
Inventors:
Robert C. Morrison, Randy W. Hall, James A. Schwindeman, Conrad W. Kamienski, John F. Engel
Abstract: A process for the preparation of formic acid by the reaction of carbon monoxide with water at temperatures of from 100.degree. to 250.degree. C. and absolute from 100 to 350 bar, in which tertiary amines of the general formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 individually denote C.sub.1 -C.sub.14 alkyl, C.sub.3 -C.sub.8 cycloalkyl, aryl, and C.sub.7 -C.sub.16 aralkyl or together denote a 1,4-alkylene group or 1,5-alkylene group optionally mono- to tetra-substituted by C.sub.1 -C.sub.4 alkyl, provided that the total number of carbon atoms in R.sup.1, R.sup.2, and R.sup.3 is from 3 to 40,are added to the reaction mixture.
Abstract: Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid;R.sup.1 and R.sup.2 are independently alkyl, fluoroalkyl, cycloalkyl, aryl or aralkyl; andR.sup.3 is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, cyano, sulfonate, carboxamido, sulfonamido, CO.sub.2 -alkyl, CO.sub.2 -aryl or CO.sub.2 -aralkyl;are useful as contrast agents in x-ray imaging compositions and methods.
Abstract: Certain benzylphosphonic acid compounds, and their pharmaceutically-acceptable salts, are inhibitors of tyrosine kinase enzymes, and so are useful for the control of tyrosine kinase dependent diseases (e.g., cancer, atherosclerosis).