Abstract: The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.
Type:
Grant
Filed:
October 21, 1998
Date of Patent:
March 28, 2000
Assignee:
E. I. du Pont de Nemours and Company
Inventors:
Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
Abstract: This invention relates to a process for preparing perylene pigment compositions by reaction of(a) a perylene tetracarboxylic compound;(b) about 0.01 to about 20% by weight, relative to the perylene tetracarboxylic compound, of a non-pigmentary cyclic anhydride or imide of formula (I) ##STR1## wherein W is O or NR.sup.1 (where R.sup.1 is hydrogen, a metal, or optionally substituted alkyl, cycloalkyl, aralkyl, or aryl), R.sup.2, R.sup.3, and R.sup.4 are various combinations of substituents and/or fused-on rings, and the dotted line is an optional double bond representing R.sup.2 --C.dbd.C--R.sup.3 ;(c) ammonia or a primary alkyl, aralkyl, or aryl amine; optionally in the presence of(d) a solvent and/or(e) one or more dispersants.
Abstract: An ether is oxidized with oxygen under an oxidation catalyst comprising an imide compound (such as N-hydroxyphthalimide) or the imide compound and a co-catalyst to produce the corresponding chain or cyclic ester or anhydride. The co-catalyst may be a transition metal compound. The above process provides a process for oxidizing an ether by oxygen efficiently to produce the corresponding oxide (such as an ester, an hydride) with high conversion and selectivity.
Type:
Grant
Filed:
May 8, 1998
Date of Patent:
March 14, 2000
Assignees:
Daicel Chemical Industries, Ltd., Yasutaka Ishii
Abstract: This invention relates to an organomercapto Au(I) complex having the formula ##STR1## wherein M is a cationic counterion;SOL is a solubilizing group;A is a substituted or unsubstituted divalent organic linking group;and n is 1 to 4 and wherein the compound is symmetrical.It further relates to a method of manufacturing an organomercapto Au(I) complex comprising reacting an Au(I) complex with an organomercapto ligand and isolating the resulting organomercapto Au(I) complex from the reaction mixture.
Type:
Grant
Filed:
November 6, 1997
Date of Patent:
March 7, 2000
Assignee:
Eastman Kodak Company
Inventors:
Roger Lok, Weimar W. White, Brian P. Cleary
Abstract: Process for the production of alkoxycarbonyldipeptides intermediates in the synthesis of the lisinopril which comprises protecting both amino functions of the L-lysine with an alkoxycarbonyl group, subsequently making the N-carboxyanhydride of the N6-[alkoxycarbonyl]-L-lysine by treatment with thionyl chloride and making the desired alkoxycarbonyldipeptide by reaction with L-proline in alkaline medium.
Abstract: 4-Hydroxy-2-pyrrolidinone which is useful as a raw material of drugs can be produced rapidly and highly selectively in a high yield from an optically active or recemic 4-amino-3-hydroxybutylic acid derivative or a 4-azido-3-hydroxybutyric acid derivative by adding a base catalyst to the reaction system. 4-Hydroxy-2-pyrrolidinone having a high optical purity can be obtained by carrying out recrystallization of optically active 4-hydroxy-2-pyrrolidinone without using a poor solvent.
Abstract: Small diameter silicon carbide-containing fibers are provided in a bundle such as a fiber tow that can be formed into a structure where the radii of curvature is not limited to 10-20 inches. An aspect of this invention is directed to impregnating the bundles of fibers with the slurry composition to substantially coat the outside surface of an individual fiber within the bundle and to form a complex shaped preform with a mass of continuous fibers.
Type:
Grant
Filed:
December 30, 1996
Date of Patent:
February 15, 2000
Assignee:
General Electric Company
Inventors:
James D. Steibel, Gregory S. Corman, Robert C. Schikner, Andrew Szweda
Abstract: Compounds with fungicidal properties are presented having the formula ##STR1## wherein m and n are 0 or 1; X is hydrogen, halo, C.sub.1 -C.sub.4) alkyl or alkoxy; Z is (C.sub.1 -C.sub.12) alkyl or haloalkyl; R, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently hydrogen, a halogen, lower alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, arylcycloalkyl, or heterocyclyl, optionally substituted with one or more halogen atoms.
Type:
Grant
Filed:
December 3, 1998
Date of Patent:
February 8, 2000
Assignee:
Rohm and Haas Company
Inventors:
Ronald Ross, Ted Tsutomo Fujimoto, Steven Howard Shaber
Abstract: A process for the production of hydroxy-substituted oxazolidinones, particularly 5-hydroxyoxazolidinones, which are useful as intermediates in the synthesis of herbicidally active compounds, comprising treating a hydroxythiazolidinone with an oxidizing agent.
Type:
Grant
Filed:
July 28, 1998
Date of Patent:
February 8, 2000
Assignee:
ZENECA Limited
Inventors:
Glynn Mitchell, John Michael Cox, Shaheen Khatoon Vohra
Abstract: A melt-extrudable polymeric strand with enhanced tensile strength formed by extruding a melt-extrudable polymer while subjecting the a portion of the polymer to ultrasonic energy. The melt-extrudable polymeric strand has a tenacity which is from about 1.5 to about 3 times the tenacity of an otherwise identical strand not made by applying ultrasonic energy to a portion of the melt-extrudable polymer while the melt-extrudable polymer is extruded. Desirably, the strand has a tenacity within a range from about 0.3 to about 0.9 g/denier. In a method for making such a strand, a molten melt-extrudable polymer is extruded through a die assembly, ultrasonic energy is applied to a portion of the melt-extrudable polymer within the chamber and without applying ultrasonic energy to the die tip, while an extrusion exit orifice receives melt-extrudable polymer from an extrusion chamber, and the extruded polymer is attenuated to form a strand.
Abstract: The diphenyl-cyclopropene derivatives of the instant invention are kappa opioids useful in the treatment of pain, inflammation, Parkinsonism, dystonia, cerebral ischemia, diuresis, asthma, psoriasis, irritable bowel syndrome, and stroke.The compounds are K-agonists which are centrally acting and peripherally selective acting.
Abstract: A process is provided for the preparation of .alpha.-tocopherol. According to the process, a condensation reaction between trimethylhydroquinone and a specific phytol derivative or isophytol is conducted in the presence of any one of the following solvents:(i) a carbonate ester;(ii) a lower fatty acid ester represented by the following formula:R.sup.1 COOR.sup.2wherein R.sup.1 means a lower alkyl group having 1-4 carbon atoms and R.sup.2 means a lower alkyl group having 1-5 carbon atoms with the proviso that methyl acetate and ethyl acetate are excluded;(iii) a mixed solvent of a nonpolar solvent and a lower alcohol having 1-5 carbon atoms; and(iv) a mixed solvent of the nonpolar solvent and the lower fatty acid ester.
Abstract: Ingestible compounds which are substantially tasteless and which have been found to be effective reducers or eliminators of undesirable tastes for eatables.
Abstract: Novel products of formula (I), their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments. ##STR1## In the formula (I), the following substituents are among the preferred: Ar represents a substituted or condensed phenyl radical or a polycyclic or heterocyclic aromatic radical, R represents a radical of general formula --(CH.sub.2).sub.m --X.sub.1 --(CH.sub.2).sub.n --Z in which X.sub.1 =single bond, O, S; m=0, 1; n=0, 1, 2; it being possible for the CH.sub.2 radicals to be substituted; Z represents carboxyl, COOR.sub.6 (R.sub.6 =alkyl), CON(R.sub.7)(R.sub.8) (R.sub.7 =hydrogen or alkyl and R.sub.8 =hydrogen, hydroxyl, arylsulphonyl, heterocyclyl, optionally substituted amino, optionally substituted alkyloxy or optionally substituted alkyl), PO(OR.sub.9).sub.2 (R.sub.9 =hydrogen or alkyl), an --NH--CO--T (T=hydrogen or optionally substituted alkyl) radical, or elsea ##STR2## radical, R.sub.1 and R.sub.
Type:
Grant
Filed:
December 29, 1997
Date of Patent:
January 11, 2000
Assignee:
Rhone-Poulenc Rorer S.A.
Inventors:
Jean-Dominique Bourzat, Alain Commer.cedilla.on, Norbert Dereu, Patrick Mailliet, Fabienne Sounigo-Thompson, Jean-Paul Martin, Marc Capet, Michel Cheve
Abstract: A process for preparing glyoxal monoacetals of the formula I, ##STR1## where R.sup.1 and R.sup.2, which can be identical or different, are C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 alkenyl involves reacting a mixture of glyoxal and glyoxal bisacetals of the formula II, ##STR2## where R.sup.1 and R.sup.2 have the meaning given above, with an excess of an alcohol of the formula R.sup.1 OH or R.sup.2 OH or mixtures of these in the presence of an acid catalyst until reaction equilibrium is achieved.
Type:
Grant
Filed:
November 25, 1997
Date of Patent:
January 11, 2000
Assignee:
BASF Aktiengesellschaft
Inventors:
Carsten Groning, Jorg Therre, Gerd Kaibel, Klaus Ebel
Abstract: Ingestible compounds which are substantially tasteless and which have been found to be effective reducers or eliminators of undesirable tastes for eatables.
Abstract: The invention relates to derivatives of general formula I ##STR1## as defined in the description. The invention also relates to a process for their preparation and to their therapeutic use, in particular or the treatment of complaints associated with melatonin disorders, and pharmaceutical and cosmetic compositions comprising them.
Type:
Grant
Filed:
March 27, 1998
Date of Patent:
December 21, 1999
Assignee:
CEMAF and Laboratoires Besins Iscovesco S.A.
Inventors:
Jean-Bernard Fourtillan, Marianne Fourtillan, Jean-Claude Jacquesy, Marie-Paule Jouannetaud, Bruno Violeau, Omar Karam
Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
Type:
Grant
Filed:
July 22, 1998
Date of Patent:
December 21, 1999
Assignee:
Vertex Pharmaceuticals, Incorporated
Inventors:
Roger D. Tung, Mark A. Murcko, Govinda R. Bhisetti
Abstract: Activating groups for cyanine dyes used to label chain terminators in nucleotide sequencing, based on N-hydroxyphthalimide, are disclosed. From these activating groups, activated dyes of the present Invention are prepared which react with the derivitized nucleotide chain terminators to give a labeled chain terminator of the present Invention. The activating groups of the present Invention allow the dye-chain terminator reaction to occur at a much higher yield and with much greater selectivity for the mono-substituted product, compared with the prior art.