Abstract: An improved process for the preparation of 4-methoxy-2'-{2-(1-methyl-2-piperidyl)ethyl}benzanilide has been developed. The process comprises essentially three steps starting with methyl anthranilate and 2-picoline and features a novel low-pressure hydrogenation sequence.
Abstract: Dihydro-M-4 and dihydro-IsoM-4 are new compounds which may be prepared by the catalytic hydrogenation of M-4 or IsoM-4 respectively. They, and their salts and esters (which may be prepared by conventional salification or esterification reactions with the parent dihydro-M-4 or dihydro-IsoM-4), are capable of inhibiting cholesterol biosynthesis in the liver and may be formulated, for therapeutic use, with conventional pharmaceutical carriers or diluents.
Abstract: Compounds of formula (I): ##STR1## (wherein R represents a group of formula ##STR2## and the corresponding ring-closed lactones, salts (especially alkali metal salts) and esters (especially C.sub.1 -C.sub.5 alkyl esters) thereof may be prepared by subjecting ML-236B, or ML-236B carboxylic acid or a salt or ester thereof to enzymatic hydroxylation, which may be effected by means of microorganisms of the genera Mucor, Rhizopus, Zygorynchus, Circinella, Actinomucor, Gongronella, Phycomyces, Martierella, Pycnoporus, Rhizoctonia, Absidia, Cunninghamella, Syncephalastrum and Streptomyces, or cell-free, enzyme-containing extracts from said microorganisms. The compounds are capable of inhibiting biosynthesis of cholesterol and are thus useful in the treatment of hypercholesteraemia.
Abstract: An improved process for preparation of 4,5-dichloro-1,2-dithia-cyclopenten-3-one of the formula ##STR1## by reacting hexachloroprene with sulphur at elevated temperatures, wherein the improvement comprises hydrolyzing by-product sulphur chlorides by conducting the reaction in the presence of water.
Abstract: 5,6-Epoxy-3,3,6-trimethyl-hept-1-en-4-one, a novel aliphatic epoxy-ketone, has been found to possess useful odor and flavor properties. It can be advantageously used as perfume and flavor-modifying ingredient.Perfume and flavor-modifying composition containing same and process for its preparation.
Type:
Grant
Filed:
April 22, 1982
Date of Patent:
May 8, 1984
Assignee:
Firmenich SA
Inventors:
Regula Naf, Anthony F. Morris, Ferdinand Naf
Abstract: A compound of formula (I): ##STR1## (called 6-methoxy-IsoML-236B lactone) and its corresponding free hydroxy-carboxylic acid and salts and esters of said acid may be prepared by the enzymatic alkoxylation of an ML-236B compound, preferably using a microorganism of the genus Syncephalastrum, Absidia or Cunninghamella, e.g. Absidia coerulea, or a cell-free enzyme-containing extract from said microorganism. If desired, the lactone or carboxylic acid may be converted by conventional salification or esterification techniques to the desired salt or ester. These compounds have the ability to inhibit the biosynthesis of cholesterol and are thus of value in the treatment of hypercholesteraemia, for which purpose they may be formulated as compositions in admixture with conventional pharmaceutical carriers or diluents.
Abstract: The invention relates to novel 4-(1H-azolylmethyl)-1,3-dioxolan-5-one derivatives of the formula I ##STR1## and to the production and use of these compounds. In formula I, R.sub.1 and R.sub.2 are unsubstituted or substituted alkyl or phenyl, or together form a 3- to 7-membered carbocyclic ring which is unsubstituted or substituted, A is an unsubstituted or substituted phenyl radical, and X is --CH.dbd. or --N.dbd.. The compounds of the formula I can be used in the form of appropriate compositions for regulating plant growth and/or for controlling and/or protecting plants from attack by phytopathogenic microorganisms.
Abstract: The invention concerns compounds of formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Ar represents an optionally substituted indolyl group; A represents a straight or branched chain alkylene or oxoalkylene group, each having 2-4 carbon atoms and R represents an optionally substituted aryl (including heteroaryl) group, which possess anti-hypertensive and psychotropic activity, and are useful in the treatment of high blood pressure or as anti-depressants.
Abstract: The present invention relates to chlorocitric acids of the formula ##STR1## and stereoisomers, optical antipodes and pharmaceutically acceptable salts thereof, to methods of preparation thereof, including intermediates involved therein, and to their use as anorectic agents for the treatment of obesity in mammals.
Type:
Grant
Filed:
August 7, 1981
Date of Patent:
April 17, 1984
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Robert W. Guthrie, Richard W. Kierstead, Francis A. Mennona, Ann C. Sullivan
Abstract: Novel ether, ester, urethane, thiourethane and carbonate derivatives of the ruminant growth promoters, M.139,603, M.139,603-adlehyde and oxime etc. derivatives thereof, all of which are effective in reducing the proportion of methane produced by ruminal fermentation, and increasing the proportion of propionic acid at the expense of acetic acid in the rumen contents; together with processes for their manufacture, compositions containing them, and their use in increasing growth and/or feed efficiency in ruminant animals.
Abstract: New 2-[4-(diphenylmethylene)-1-piperidinyl]-acetic acids and their amides, processes for the preparation thereof and therapeutic compositions. These compounds have the formula ##STR1## wherein Y=--OH or --NR.sub.1 R.sub.2, R.sub.1 and R.sub.2 =H, alkyl or phenyl; X=H, halogen or alkoxy; m=0, 1 or 2 and n=1 or 2.The 2-[4-(diphenylmethylene)-1-piperidinyl]-acetic acids are prepared by hydrolyzing the corresponding amide or lower alkyl ester, whereas the amides are prepared either by reacting a 4-(diphenylmethylene)-piperidine with an omega-haloacetamide, or by reacting an alkali metal salt of an omega-[4-diphenylmethylene)-1-piperidinyl]-alkanol (m=1 or 2) with a 2-haloacetamide, or by reacting a nitrogen compound (HNR.sub.1 R.sub.2) with a halide or alkyl ester of a 2-[4-(diphenylmethylene)-1-piperidinyl]-acetic acid.These compounds have in particular an antiallergic, spasmolytic, antihistaminic and broncholytic activity.
Abstract: Chlorine and tertiary alkanol dissolved in an inert organic solvent are reacted with calcium oxide in aqueous calcium chloride to produce tertiary alkyl hypochlorite which is recovered in the organic solvent and reacted with water and olefinically unsaturated compound to produce chlorohydrin and tertiary alkanol. Chlorohydrin and tertiary alkanol recovered in the organic solvent are contacted with calcium oxide in aqueous calcium chloride to produce the epoxy compound, and tertiary alkanol recovered in the organic solvent is recycled to hypochlorite production. Calcium chloride produced as by-product in the hypochlorite production and saponification is recovered as an aqueous solution having a calcium chloride concentration of at least 25 wt. % to provide calcium chloride in a usable form.
Abstract: N-Acylated N-phenyl-aminotetrahydro-2-furanones of the formula ##STR1## wherein R represents C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or halogen,R.sub.1 represents C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.4 -alkoxy or halogen,R.sub.2 represents hydrogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.4 -alkoxy or halogen,R.sub.3 represents hydrogen or methyl, with the total number of C atoms of the substituents R, R.sub.1, R.sub.2 and R.sub.3 in the phenyl ring not exceeding the number 8,R.sub.4 represents hydrogen or methyl, whileR.sub.5 represents one of the following groups: an alkythioalkyl or alkoxyalkyl group having 2 to 5 carbon atoms or an alkoxyalkoxymethyl group having a maximum of 6 carbon atoms, a 2-furanyl or 2-tetrahydrofuranyl group optionally substituted by halogen, a 1,2,4-triazolylmethyl group, a 1,2-pyrazolylmethyl group, or a group -CH.sub.2 -OR.sub.6 in which R.sub.6 represents a 5- or 6-membered heterocyclic having oxygen as the hetero atom are valuable fungicidal active substances.
Type:
Grant
Filed:
March 2, 1982
Date of Patent:
April 17, 1984
Assignee:
Ciba-Geigy Corporation
Inventors:
Walter Kunz, Wolfgang Eckhart, Adolf Hubele
Abstract: New bromoepoxy-cyclohexenes and their derivatives, which are starting compounds for units used to synthesize natural compounds, e.g. cyclitols or aminocyclitols.
Type:
Grant
Filed:
April 22, 1982
Date of Patent:
April 10, 1984
Assignee:
BASF Aktiengesellschaft
Inventors:
Horst Prinzbach, Reinhard Schwesinger, Reinhold Keller
Abstract: New cyclic carbonic acid derivatives of the formula ##STR1## in which R denotes either --CH.sub.2 OH, R.sup.1 then representing an alkyl radical having 1 to 4 C atoms, or ##STR2## R.sup.1 and R.sup.2 then independently of one another representing methyl or ethyl, or ##STR3## R.sup.1 and R.sup.5 then each representing an alkyl radical having 1 to 4 C atoms, or in whichR and R.sup.1 together denote ##STR4## wherein A represents the group ##STR5## or oxygen, a process for their preparation, and their use as copolymerization components in the preparation of polycarbonates.
Abstract: Totally synthetic analogs of the known inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase, compactin and mevinolin, are prepared from a chiral synthon derived from D-glucose which has the same chirality as the natural products.
Abstract: Esters of leukotriene A are conveniently prepared by reacting 9-oxo-5,6-trans-epoxynon-7(E)-enoates with 11-triphenylphosphoranylidene undec-6(Z),9(Z)-diene. Esters of leukotriene-A are useful intermediates in the synthesis of naturally occurring leukotrienes, which have been shown to be potent broncho-constricting substances. Novel intermediates to the esters of leukotriene A, 9-oxo-5,6-transepoxynon-7(E)-enoates and 7-oxo-5,6-trans-epoxyheptanoates, are disclosed.
Type:
Grant
Filed:
November 4, 1982
Date of Patent:
April 3, 1984
Assignee:
SmithKline Beckman Corporation
Inventors:
John G. Gleason, Charles M. Kinzig, Deborah L. Bryan
Abstract: The present invention relates to the novel trichothecenes, 12'-hydroxyverrucarin J and iso-satratoxin H, and a fermentation process for the production of said compounds.The invention also relates to pharmaceutical compositions comprising said compounds and methods for using said compositions.
Type:
Grant
Filed:
October 4, 1982
Date of Patent:
March 13, 1984
Assignee:
Warner-Lambert Company
Inventors:
Tim A. Smitka, Richard H. Bunge, James C. French, Russell J. Bloem
Abstract: A compound corresponding to formula (I): ##STR1## wherein X represents oxygen, sulphur or >N--R',R' representing hydrogen or an alkyl radical,R.sub.1 to R.sub.4, andR'.sub.1 to R'.sub.5 independently represent the following:a hydrogen or halogen atom,an alkyl, aryl, alkoxy, aryloxy or acyloxy radical,a hydroxy radical,an amino, mono-alkylamino or di-alkylamino radical,a hydroxyalkyl, aminoalkoxy, mono- or di-alkylaminoalkoxy radical,in the form of the d or l isomer, or in the form of a racemic mixture, is useful as a medicament.
Type:
Grant
Filed:
May 10, 1982
Date of Patent:
March 13, 1984
Assignee:
Pierre Fabre S.A.
Inventors:
Philippe Hatinguais, Jean-Francois Patoiseau, Gilbert Marcelon