Abstract: The invention is novel analogs of 9-cis-retinoic acid which are useful for the treatment and prevention of coronary artery disease and to protect against premature atherosclerosis by increasing HDL levels. The invention includes processes for preparing the novel 9-cis-retinoic acid analogs.
Type:
Grant
Filed:
November 14, 1995
Date of Patent:
October 19, 1999
Assignee:
American Cyanamid Company
Inventors:
Joseph William Epstein, Feng Ling Qing, Gary Harold Birnberg, Adam Matthew Gilbert
Abstract: A process for preparing a pharmaceutical composition which comprises admixing a compound of claim 1 or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
February 3, 1997
Date of Patent:
October 19, 1999
Assignee:
Fujisawa Pharmaceutical Co., Ltd.
Inventors:
Atsushi Kuno, Hiroaki Mizuno, Kumi Yamasaki, Yoshikazu Inoue
Abstract: A composition and method for the prevention or treatment of HIV-1 infection comprising an HIV-1 reverse transcriptase-inhibiting heterocyclyl carb(ox/thio)anilide compound, a second HIV-1 reverse transcriptase inhibitor compound which does not select for the same HIV-1 mutant strain or strains selected for by the heterocyclyl carb(ox/thio)anilide compound, and, optionally, a third HIV reverse transcriptase inhibitor compound.
Abstract: New compounds of the formula (A) ##STR1## a process for their preparation and their use in the manufacture of pharmaceutical preparations. The new compounds have both local anaesthetic and analgesic effect.
Abstract: A description is given of a process for stabilising an organic polymer against ozone in the ambient air, which comprises adding to the polymer as stabiliser a monomeric sterically hindered piperidine compound, or an oligomeric or polymeric sterically hindered piperidine compound containing one or several triazine units, or a secondary sterically hindered piperidine compound, the piperidine compound containing in any case at least one unit of formula I ##STR1## wherein G is hydrogen or methyl, and G.sub.1 and G.sub.2 are hydrogen, methyl or, taken together, oxygen.With this process it is possible to make a more accurate prediction of the service time of the polymer and it helps to avoid unnecessarily high dosages of the stabiliser.
Abstract: In a process for the catalytic hydrogenation of 2,5- and 2,3-dihydrofuran with hydrogen to give tetrahydrofuran, use is made of a catalyst in which a metal or a plurality of metals have been deposited by vapor deposition or sputtering on a metal wire mesh or a metal foil as support.
Type:
Grant
Filed:
May 22, 1998
Date of Patent:
October 12, 1999
Assignee:
BASF Aktiengesellschaft
Inventors:
Franz Josef Brocker, Rolf Fischer, Gerd Kaibel, Rolf Pinkos
Abstract: Processes and intermediates for preparing 2-substituted piperidines such as 2-substituted d-threo piperidines are provided. In preferred embodiments, the processes of the invention comprise the steps of reacting a 2-substituted pyridine with hydrogen in the presence of a catalyst in an alkanoic acid, and adding an alkyl alkanoate to the resulting mixture of threo and erythro 2-piperidine stereoisomers to precipitate alkanoate salts of the erythro stereoisomers preferentially with respect to alkanoate salts of the threo stereoisomers. The erythro salts then are reacted with aqueous base to form the corresponding mixture of erythro amide free bases, which are reacted with a suitable organic acid resolving agent in an alkyl alcohol solvent to form acid salts of the l-erythro stereoisomers preferentially with respect to the d-erythro stereoisomers.
Abstract: The present invention relates generally to methods and compositions for targeting the vasculature of solid tumors using immunological- and growth factor-based reagents. In particular aspects, antibodies carrying diagnostic or therapeutic agents are targeted to the vasculature of solid tumor masses through recognition of tumor vasculature-associated antigens, such as, for example, through endoglin binding, or through the specific induction of endothelial cell surface antigens on vascular endothelial cells in solid tumors.
Type:
Grant
Filed:
December 5, 1994
Date of Patent:
October 12, 1999
Assignee:
Board of Regents, The University of Texas System
Abstract: A triketone compound of the following formula: ##STR1## wherein Y.sup.1 is C.sub.1 to C.sub.4 alkyl, a halogen or a C.sub.1 to C.sub.4 haloalkyl; each of Y.sup.2 and Y.sup.3 is independently C.sub.1 to C.sub.4 alkyl; Y.sup.4 is hydrogen, C.sub.1 to C.sub.4 alkyl or a halogen; n is 0, 1 or 2; p is 0 or 1; each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently hydrogen, C.sub.1 to C.sub.4 alkyl or phenyl; or when p is 1, either R.sup.1 or R.sup.2 and either R.sup.3 or R.sup.4 optionally bond to each other to form an intramolecular double bond; and X is oxygen or sulfur. The triketone compound is useful as a herbicide to control a broad range of upland weeds at a low dosage without causing phytotoxicity on corn.
Abstract: The use of modified silicon dioxide as a catalyst support in catalytic reactions under hydrothermal conditions is described. The pore structure of the supports may be stabilized against hydrothermal reaction conditions by impregnating the catalyst supports with elements of Group IVB of the Periodic Tube of Elements.
Type:
Grant
Filed:
February 27, 1997
Date of Patent:
September 28, 1999
Assignee:
Degussa Huls Aktiengesellschaft
Inventors:
H. G. J. Lansink-Rotgerink, Heike Riedemann, Thomas Tacke, Helmfried Krause, Andreas Freund, Roland Burmeister, Peter Panster
Abstract: Disclosed is a process for the preparation of 2-butene-1,4-diol comprising contacting a mixture of water and 1,2-epoxy-3-butene with a catalyst comprising a metal halide, zeolite and a non-protic solvent.
Type:
Grant
Filed:
September 4, 1997
Date of Patent:
September 28, 1999
Assignee:
The Dow Chemical Company
Inventors:
Thomas J. Remans, Pierre A. Jacobs, Johan Martens, Dominicus A. G. van Oeffelen, Mathias H. G. Steijns
Abstract: New process for the preparation of ropivacaine hydrochloride monohydrate adapted for production in the plant, which process includes three steps.
Abstract: This invention presents novel methods for recovery of phosphoramidites from the waste products of oligonucleotide synthesis. The methods include reacting a tribromophenoxydichlorophosphorane with a H-phosphonate in the presence of an amine.
Type:
Grant
Filed:
December 27, 1996
Date of Patent:
September 21, 1999
Assignee:
Isis Pharmaceuticals, Inc.
Inventors:
Richard H. Griffey, Douglas L. Cole, Vasulinga Ravikumar
Abstract: A class of sulforhodamine labeling reagents capable of binding with a biomolecular species to produce a conjugate with fluorescent properties. The sulforhodamine labeling reagents have the structure: ##STR1## The group X is selected from an alkyl, an olefin, a monocyclic aliphatic saturated hydrocarbon, an aryl, or nothing at all. The group Y is selected from an amide, a substituted amide, or nothing at all. The group Z is selected from a monocyclic aliphatic hydrocarbon, an aryl, or an alkyl, as defined with respect to group X, a polyethylene glycol chain of the general form (CH.sub.2 CH.sub.2 O).sub.n, or nothing at all. The alkyl or polyethylene glycol chain may further have inert intermediate amide, ether, or disulfide functionalities. The group X, group Y, and group Z cannot all be nothing at all or non-existent. The group R is an electrophilic moiety suitable for conjugation of the fluorescent labeling reagent with a biomolecular species. Also disclosed is a method of making the reagents.
Abstract: 2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients.The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.
Abstract: A process is provided for preparing 14-hydroxynormorphinones having the formula: ##STR1## which comprises reacting normorphinones having the formula: ##STR2## wherein R is selected from the group consisting of lower alkyl of 1 to 7 carbon atoms, cycloalkyl-lower alkyl with 3-6 ring carbon atoms, benzyl and a substituted-benzyl having the formula: ##STR3## wherein Q and Q.sup.1 are individually selected from the group consisting of hydrogen, lower alkyl, trifluoromethyl, nitro, dialkylamino and cyano;R' is selected from the group consisting of R, 2-(4-morpholinyl)ethyl, benzyloxy carbonyl and R"C(O)-- wherein R" is lower alkyl of 1-4 carbon atoms;with hydrogen peroxide at a temperature of from about 15.degree. C. to about 70.degree. C. in the presence of an acid and an aqueous solvent system to solubilize the reactant for a period of time so as to form the 14-hydroxynormorphinones.
Type:
Grant
Filed:
July 16, 1998
Date of Patent:
September 14, 1999
Assignee:
Penick Corporation
Inventors:
Bao-Shan Huang, Yansong Lu, Ben-Yi Ji, Aris P Christodoulou
Abstract: The invention relates to a method for the stereoselective preparation of a hetero-bicyclic alcohol enantiomer, characterized in that a substantially pure enantiomer of the general formula ##STR1## is prepared from a compound of the general formula ##STR2## wherein the variable are as defined as in claim 1. The method comprises the following successive reaction steps:(i) reaction with a substantially enantiomerically pure compound of the general formula ##STR3## wherein Z, R.sub.3 and R.sub.4 are defined as in claim 1; (ii) subjection of the compound formed to a deprotection/ring-closure reaction;(iii) optionally deprotection of the hydroxy group of the ring-closed product.The invention further relates to enantiomerically pure intermediates, the preparation of these intermediates and the preparation of a starting compound.
Type:
Grant
Filed:
January 22, 1997
Date of Patent:
September 7, 1999
Assignee:
Duphar International Research B.V.
Inventors:
Nicolaas Buizer, Chris G. Kruse, Klara M. Schenk, Belal Shadid