Abstract: The present invention a process for the preparation of a compound of the formula (X) useful as precursor for the A-ring in taxanes ##STR1## wherein R' is an ##STR2## in which R" is a linear, branched or cyclic alkyl group of 1 to 10 carbon atoms. The invention further relates to the novel compound (X) and to novel intermediates in said process.
Abstract: This invention relates to novel processes for synthesizing intermediates in the preparation of N-aryl and N-heteroarylamide inhibitors of the enzyme acyl coenzyme A: cholesterol acyltransferase (ACAT), and to novel intermediates used in such processes.
Abstract: Perhydro-5,5-8a-trimethyl-2-naphthalenone is prepared by acid cyclization of carboxylic esters of formula ##STR1## having a double bond in one of the positions indicated by the dotted lines and wherein symbol R designates a C.sub.1 -C.sub.6 alkyl radical, X stands for a monovalent radical of formula P(O)(OR.sup.1).sub.2 or C(O)R.sup.2, R.sup.1 represents a C.sub.1 -C.sub.6 alkyl group and R.sup.2 is either a linear or branched alkyl group or a substituted or unsubstituted phenyl radical, and wherein the wavy line represents a C--C bond of cis or trans configuration, or of formula ##STR2## wherein the wavy lines and symbol R are defined as above, and R.sup.0 represents a C.sub.3 -C.sub.6 alkyl radical, preferably branched, followed by basic decarboxylation of the obtained product.
Type:
Grant
Filed:
July 27, 1994
Date of Patent:
September 26, 1995
Assignee:
Firmenich SA
Inventors:
Roger L. Snowden, Cyril Mahaim, Dana P. Simmons
Abstract: The present invention relates to novel potassium channel agonists which are useful in activating the calcium activated Maxi-K potassium channel in mammalian neuronal and smooth muscle tissue. The claimed compounds are of the general formula: ##STR1## In addition, a novel microbiological process for producing the claimed compounds is described.
Type:
Grant
Filed:
December 13, 1993
Date of Patent:
March 21, 1995
Assignee:
Merck & Co., Inc.
Inventors:
Maria L. Garcia, Robert A. Giacobbe, Otto D. Hensens, Gregory J. Kaczorowski, Seok H. Lee, Owen B. McManus, Deborah L. Zink
Abstract: This invention relates to a novel ester which presents as (CF 1) and a method for the production of the same as well as a process for hydrolysis and a method for the determination of an optical purity using this ester, and the object thereof is to provide an intermediate for the synthesis or various natural products, which has high stability, and the optical purity of which can readily be determined, according to the esterification of 1-oxo-5-hydroxymethyl-2-cyclohexene which is unstable to acids and alkalis.
Abstract: This invention relates to compounds of structural formula (I) isolated from an aerobic fermentation of Trichoderma viride MF5628, ATCC 74084: ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents. These compounds are also potent antifungal agents. Additionally, they inhibit farnesyl protein transferase and farnesylation of the oncogene protein Ras and are thus useful in treating cancer. This invention also relates to a process for obtaining compounds of structural formula (I).
Type:
Grant
Filed:
February 9, 1993
Date of Patent:
November 15, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Guy H. Harris, Deborah Zink, E. Tracy T. Jones, Yu L. Kong
Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 independently are hydrogen, lower alkyl of 1 to 6 carbons, halogen or lower alkoxy of 1 to 6 carbons; R.sub.5 and R.sub.5 ' independently are hydrogen or lower alkyl of 1 to 6 carbons; Y is oxygen or sulfur; Z is n-alkyl having 2 to 10 carbons, cyclo or branch-chained alkyl of 3 to 10 carbons, and straight chain alkenyl having 2 to 10 carbons, or cyclo or branched chained alkenyl of 3 to 10 carbons, and the Z-Y substituent is in a 1,2 (ortho) or 1,3 (meta) position on the phenyl ring relative to the ethene moiety; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3 to 6 carbons, cycloalkyl having 3 to 6 carbons, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.
Abstract: Poly(oxyalkylene) hydroxyaromatic ethers having the formula: ##STR1## or a fuel-soluble salt thereof; where n is an integer from 5 to 100; x is an integer from 0 to 10; R.sub.1 and R.sub.2 are each independently hydrogen, hydroxy, lower alkyl having 1 to 6 carbon atoms, or lower alkoxy having 1 to 6 carbon atoms; R.sub.3 and R.sub.4 are each independently hydrogen or lower alkyl having 1 to 6 carbon atoms; R.sub.5 is an acyl group of the formula: ##STR2## wherein y is 1, 2 or 3; R.sub.6 is a divalent hydrocarbyl radical, when y is 1, a trivalent hydrocarbyl radical, when y is 2, or tetravalent hydrocarbyl radical, when y is 3, said hydrocarbyl radicals having 1 to about 20 carbon atoms; and each Z is independently selected from the group consisting of: ##STR3## where each R.sub.7 is independently alkyl having 1 to 30 carbon atoms, phenyl, aralkyl having 7 to 36 carbon atoms or alkaryl having 7 to 36 carbon atoms.
Abstract: Compounds of the formula ##STR1## in which R is hydrogen or hydroxyl, R.sub.1 is alkyl, alkoxy, amino or aryl, and R.sub.2 is hydrocarbylcarbonyl or hydrocarbylsulfonyl, are highly suitable for stabilizing magenta couplers in photographic materials.
Type:
Grant
Filed:
June 15, 1992
Date of Patent:
December 28, 1993
Assignee:
Ciba-Geigy Corporation
Inventors:
David G. Leppard, David H. Steinberg, Henri Dubas
Abstract: An isocarbacyclin derivative represented by the following formula [VII'] ##STR1## wherein A represents, a hydrocarbylcarboxylate group, a carboxymethoxycarbonyl group, an amide group, an acyloxymethyl group or a hydroxymethyl group; R.sup.4 represents H, a methyl group or a vinyl group; R.sup.5 represents a (substituted)alkyl group, a phenyl group, a phenoxy group or a cycloalkyl group; R.sup.e22 and R.sup.e32 represent H or a hydroxyprotecting group; n is 0 or 1;and a pharmaceutically acceptable salt thereof.
Abstract: Optically active cyclopentenols are here disclosed which are represented by the formula (I) ##STR1## (wherein R is a hydrogen atom or an acyl group having 2 to 15 carbon atoms, and the sign * denotes a chiral carbon atom).The optically active cyclopentenols can be prepared by a process which comprises the step of carrying out a transesterification between (.+-.
Abstract: The invention provides organosilicon compounds of the formula: ##STR1## in which: n is 1, 2 or 3;each R, which may be identical or different, is a monovalent organic group which contains a carbon-carbon double bond and from 2 to 10 carbon atoms;each R.sub.1, which may be identical or different, is a straight or branched alkyl radical optionally substituted by one or more halogen atoms or cyano groups; an aryl radical or an alkylaryl radical optionally substituted by one or more halogen atoms;R.sub.2 is a straight or branched divalent alkylene or alkylidene radical possessing up to 4 carbon atoms;X is a divalent radical consisting of, or containing, at least one hetero-atom selected from oxygen, sulphur and nitrogen atoms, the radical being attached to the radical R.sub.2 via a said hetero-atom;G is an organic radical of valency (m+1) possessing from 1 to 30 carbon atoms;m is 1, 2 or 3;and each Y, which may be identical or different, is a functional group selected from: --NO.sub.