Abstract: Lactones of formula ##STR1## and their pharmacologically acceptable salts endowed with antioxiding and hypolipidaemic properties and that show the capability to prevent and/or to delay the oxidative modification of the lipoproteins by competing with the chain of propagation of the lipidic peroxidation by means of an effective scavenging of the peroxylic radicals. The compounds object of the present invention are useful in the treatment of the atherosclerosis and of many correlated vascular pathologies, like ischaemic cardiopathies (angina pectoris and myocardial infarction), cerebral thrombosis and peripheral arteriopathies, because the high plasma levels of lipids and the oxidative modifications of the low density lipoproteins (LDL) represent crucial events in the pathogenesis of the atherosclerosis.
Abstract: Compounds of formula (I): ##STR1## and salts and esters thereof have valuable anthelmintic, acaricidal and insecticidal activities. Methods of preparing the compounds are also provided.
Abstract: A lactone compound, useful as an osteogenetic accelerator, having the formula (I): ##STR1## wherein n is zero or 1 and m is zero or 1, provided that both n and m are not zero at the same time, or a stereoisomer thereof at the 23- and/or 25-positions or any mixture thereof and a production process thereof.
Abstract: Disclosed herein is a method for producing 4-hydroxy-5-methyl-3[2H]-furanone and new uses thereof.4-hydroxy-5-methyl-3[2H]-furanone may be extracted from the plants of Pinaceae species and may advantageously be used as an anti-oxidant or for whitening the skin. The compound or extracts containing same is not irritative to the skin and can safely be applied to the skin.
Type:
Grant
Filed:
December 12, 1994
Date of Patent:
February 11, 1997
Assignee:
Pacific Corporation
Inventors:
Yong C. Boo, Che O. Jeon, Byeong G. Lee, Kyung W. Ro, Eun J. Kim
Abstract: The present invention provides an integrated process for the production of propylene oxide from an alternate feedstream such as synthesis gas. In the process, propylene oxide is produced from a feedstream comprising hydrogen and a carbon oxide. A portion of the feedstream is passed to an oxygenate production zone to produce an oxygenate stream comprising methanol and dimethyl ether, and the oxygenate stream is passed to an olefin production zone containing a metal aluminophosphate catalyst to produce a propylene stream. The propylene stream is epoxidized with hydrogen peroxide which has been produced from hydrogen separated from a portion of the feedstream. The spent water stream produced by the epoxidation reaction is treated to remove heavy components and returned to the hydrogen peroxide production zone. The return of the unreacted propylene from the epoxidation reaction zone for its subsequent recovery and recycle permits a less complicated, lower energy propylene separation.
Abstract: The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and methods for treatment of certain cancers with these new compounds.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
February 4, 1997
Assignees:
The Research Foundation of State University of New York, Indena SpA Gruppo Inverni Della Beffa
Abstract: A compound of the formula ##STR1## in which: R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen atoms and groups of formula R.sup.3 --CO--, wherein R.sup.3 represents a group selected from the group consisting of unsubstituted alkyl groups having from 9 to 20 carbon atoms; substituted alkyl groups having from 10 to 20 carbon atoms; unsubstituted alkenyl groups having from 9 to 20 carbon atoms; substituted alkenyl group having from 10 to 20 carbon atoms; unsubstituted alkynyl groups having from 8 to 10 carbon atoms; and substituted alkynyl groups having from 8 to 10 carbon atoms wherein R.sup.1 and R.sup.2 are not both hydrogen atoms or acetyl groups. The compounds have antitumor activity.
Abstract: 3,4,6-trifluorophthalic acid is prepared in high yield by reaction of a 3,4,6-trichloro-N-substituted phthalimide with potassium fluoride at temperatures in the range of 200.degree. to 270.degree. C. in the absence of a catalyst to form the corresponding trifluoro-N-substituted phthalimide which, in turn, is hydrolyzed to form the 3,4,6-trifluorophthalic acid.
Type:
Grant
Filed:
June 18, 1993
Date of Patent:
January 21, 1997
Assignee:
Occidental Chemical Corporation
Inventors:
Neil J. O'Reilly, William S. Derwin, Henry C. Lin, Deanne M. Nowak
Abstract: Disclosed is a method of fluorescent detection of a nucleic acid. The method comprises contacting to the nucleic acid a bis-dicationic aryl furan compound, such as 2,5-bis[4-(4,5,6,7-tetrahydro-1H-1,3-diazepin-2-yl) phenyl] furan; 2,5-bis{[4-(N-isopropyl) amidino] phenyl}furan; and physiologically acceptable salts thereof, and exposing the nucleic acid to light at a frequency to induce fluorescence of the compound. A method for fluorescent detection of cytoskeleton elements, and novel bis-dicationic aryl furan compounds are also disclosed.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
January 14, 1997
Assignees:
Georgia State University Research Foundation, The University of North Carolina at Chapel Hill
Inventors:
Christine C. Dykstra, Richard R. Tidwell, David W. Boykin, W. David Wilson, Jaroslaw Spychala, Bijan P. Das, Arvind Kumar
Abstract: A bislactone compound represented by the general formula (I): ##STR1## wherein R.sub.1 and R.sub.2 each independently represent a hydrogen atom or an alkyl group having 6 or less carbon atoms, and R.sub.3, R.sub.4, R.sub.5 and R.sub.6 each independently represent a hydrogen atom, a hydroxy group or an alkyl group having 6 or less carbon atoms, which is useful as a stabilizer for polymers and as a raw material of a positive type resist:a process for producing the bislactone compound; anda positive resist composition comprising the bislactone compound.
Abstract: A method of providing adjuvant activity utilizing one or more of the components of propolis, such as the benzopyran phenol derivates, pinocembrin, pinobanksin-3-acetate and naringenin, and preferably using these three components combined.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
January 7, 1997
Assignees:
Michel Fockerman, Jasmine Fockerman Cederqvist
Abstract: Psoralen compound compositions are synthesized which have substitutions on the 4, 4', 5', and 8 positions of the psoralen, which yet permit their binding to nucleic acid of pathogens. Reaction conditions that photoactivate these bound psoralens result in covalent crosslinking to nucleic acid, thereby inactivating the pathogen. Higher psoralen binding levels and lower mutagenicity results in safer, more efficient, and reliable inactivation of pathogens. In addition to the psoralen compositions, the invention contemplates inactivating methods using the new psoralens.
Type:
Grant
Filed:
May 31, 1995
Date of Patent:
December 17, 1996
Assignee:
Steritech, Inc.
Inventors:
Susan Wollowitz, Stephen T. Isaacs, Henry Rapoport, Hans P. Spielmann
Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is (CR.sub.5 R.sub.6).sub.n, (CR.sub.5 R.sub.6).sub.n,-aryl, (CR.sub.5 R.sub.6).sub.n -heteroaryl, X-(CR.sub.5 R.sub.6).sub.n, X-(CR.sub.5 R.sub.6).sub.n -aryl or X-(CR.sub.5 R.sub.6).sub.n -heteroaryl wherein aryl and heteroaryl may be optionally substituted;X is 0 or NR.sub.5 ;R.sub.5 and R.sub.6 are independently H or lower alkyl;R.sub.2 is H, halo, lower alkyl or (CR.sub.5 R.sub.6).sub.n -aryl;R.sub.3 and R.sub.4 are independently H or alkyl;A is a D or L isomer of an amino acid selected from the group consisting of alanine, valine, leucine, isoleucine, proline, phenylalanine, glycine, tyrosine, methionine, asparagine, glutamine, aspartic acid, glutamic acid, lysine, arginine, histidine and .beta.-thienylalanine;Z is CH.sub.2 or O; andn is 0-4;pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1.beta.
Type:
Grant
Filed:
May 12, 1995
Date of Patent:
December 17, 1996
Assignee:
Sterling Winthrop Inc.
Inventors:
Roland E. Dolle, Todd L. Graybill, Gary J. Speier, Catherine P. Prouty, Stanley J. Schmidt
Abstract: Substantially pure compositions of matter selected from the group of cephalostatin 7, cephalostatin 8, and cephalostatin 9 having anti-neoplastic activity are disclosed.
Type:
Grant
Filed:
January 19, 1993
Date of Patent:
December 10, 1996
Assignee:
Arizona Board of Regents acting on behalf of Arizona State University
Abstract: 2-Chloro-5-(N-acyl-aminomethyl)pyridines can be prepared by hydrogenation of 2-chloro-5-cyanopyridine with hydrogen in an acylating agent using a hydrogenation catalyst.
Abstract: A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.
Abstract: The present invention relates to the epoxidation of olefins using cyclohexyl hydroperoxide as reactant, the improvement being using a secondary or tertiary alcohol such as cyclohexanol or tertiary butyl alcohol as a stabilizing agent during the epoxidation, the alcohol stabilizer being fed to the epoxidation reaction zone in an amount greater than 3 moles per mole of hydroperoxide fed to the epoxidation reaction zone.
Abstract: This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
Type:
Grant
Filed:
May 4, 1995
Date of Patent:
October 8, 1996
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Henry W. Pauls, Yong-Mi Choi, Dilip V. Amin