Abstract: In accordance with the present invention, methods are provided for the treatment of visual loss and other neurological dysfunctions in AIDS patients employing agents capable of blocking TNF expression in the central nervous system.
Type:
Grant
Filed:
March 26, 1992
Date of Patent:
June 9, 1998
Assignee:
University of Southern California
Inventors:
Alfredo A. Sadun, Parkash S. Gill, Pravin U. Dugel, Michele Madigan
Abstract: There are disclosed compounds of formula I,Ar--CH.sub.2 CH.sub.2 --NH--CR.sup.1 R.sup.2 --X--Y Iin whichAr represents a group, ##STR1## X represents a C.sub.1-12 alkylene chain optionally interrupted or terminated by one or more groups selected from --S(O).sub.n --, --O--, --C(Z)--, CR.sup.6 R.sup.7, phenylmethyne, --NR.sup.8 --, --CONH--, --NHCO-- and --NHCONH--,Y represents an optionally substituted aryl or cycloalkyl group,Z represents O or S,R.sup.1, R.sup.2, R.sup.5 and R.sup.9 each independently represent hydrogen or alkyl C.sub.1-6,R.sup.3 and R.sup.4 represent hydrogen, or R.sup.3 and R.sup.4 together form a group --S--, --NR.sup.9 -- or --CH.sub.2 --,R.sup.6 and R.sup.7 independently represent hydrogen, alkyl C.sub.1-6, fluoro, cyano, or CF.sub.3, provided that at least one of R.sup.6 and R.sup.7 is other than hydrogen,R.sup.8 represents hydrogen or alkyl C.sub.1-6, or when X is interrupted or terminated by more than one --NR.sup.8 -- group may together with another R.sup.8 group form the chain --CH.
Type:
Grant
Filed:
October 31, 1996
Date of Patent:
June 9, 1998
Assignee:
Astra Pharmaceuticals Limited
Inventors:
Roger V. Bonnert, Roger C. Brown, David R. Cheshire, Francis Ince, John Dixon
Abstract: Cis-epoxide compounds of formula (I-3) and pharmaceutically acceptable salts, hydrates and solvates thereof: ##STR1## wherein: R.sup.1 is a cycloalkyl, or arly-substituted lower alkyl group;K and J are independently a group having the formula of ##STR2## wherein R.sup.18 is a lower alkyl group optionally substituted with an aryl radical; X is O, NH, or N--CH.sub.3 ; and R.sup.19 is an aromatic hetercyclic sysstem containing a nitrogen atom in its ring, or a lower alkyl group optionally substituted with an aryl radical, or a hydrogen;G is an amino acid which is linked to K-- and ##STR3## by peptide bonds in formula (I-3); Q is an amino acid which is linked toby peptide bonds in formula (I-3), or a group having the formula ofwherein R.sup.20 is a lower alkyl group optionally substituted with an aromatic radical; and Y is CH.sub.2, O or NH; andr is 0 or 1, except that Q is a group having the formula ofr is 0.
Type:
Grant
Filed:
June 20, 1996
Date of Patent:
June 9, 1998
Assignee:
Lucky Limited
Inventors:
Sung Chun Kim, Nakyen Choy, Chang Sun Lee, Ho I. Choi, Jong Sung Koh, Heungsik Yoon, Chi Hyo Park, Sang Soo Kim, Young Chan Son
Abstract: Manufacturing method for hexafluorocyclobutene in which 1,2-dichlorohexafluorocyclobutane is dechlorinated using hydrogen in the presence of a metal oxide and/or silicon oxide catalyst. Manufacturing method for (Z)-1,2,3,3,4,4-hexafluorocyclobutane which carries out the hydrogen-adding reaction (hydrogen reduction) of the raw material, 1,2-dichlorohexafluorocyclobutane, in the presence of a rhodium catalyst, or which carries out vapor-phase hydrogen reduction of hexafluorocyclobutene in the presence of a palladium catalyst.Using this manufacturing method, hexafluorocyclobutene can easily be derived in a single step with high selectivity from 1,2-dichlorohexafluorocyclobutane which can be obtained readily and at a low cost. This method also produces a high yield of (Z)-1,2,3,3,4,4-hexafluorocyclobutane.
Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which A, R.sub.1, R'.sub.1, R.sub.2, R.sub.3 and n are as defined in the description, and medicinal product containing the same useful for treating a mammal afflicted with a disorder of the melatoninergic system.
Type:
Grant
Filed:
March 10, 1997
Date of Patent:
June 2, 1998
Assignee:
Adir et Compagnie
Inventors:
Daniel Lesieur, Veronique Leclerc, Patrick Depreux, Philippe Delagrange, Pierre Renard
Abstract: A preventive agent against adhesion of a marine organism comprising: at least one amine compound represented by the following formula (I): ##STR1## , wherein R is a C.sub.8-22 saturated or unsaturated aliphatic hydrocarbon group, R.sup.1 is hydrogen atom, aminopropyl, a C.sub.1-22 saturated aliphatic hydrocarbon or C.sub.2-22 unsaturated aliphatic hydrocarbon group, R.sup.2 is aminopropyl, a C.sub.1-8 saturated aliphatic hydrocarbon or C.sub.2-8 unsaturated aliphatic hydrocarbon group, provided that R.sup.1 is hydrogen atom or aminopropyl group when R.sup.2 is represents aminopropyl group, or a salt thereof; and at least one N-alkyl polyamine compound represented by the following formula (II):R--?NH(CH.sub.2).sub.3 !.sub.n --NH.sub.2 (II), wherein R is a C.sub.8-22 saturated or unsaturated aliphatic hydrocarbon group and n is an integer from 2 to 4, or a salt thereof in an amount of 0.1 to 9 parts by weight to one part by weight of the compound (I).
Abstract: A chemical warfare agent decontamination solution made up of about 30-45% of a quaternary ammonium complex containing benzyltrimethylammonium chloride and benzyltriethylammonium chloride dissolved in a solvent, such as water or glycol, is provided. This solution is a noncorrosive, nontoxic, nonflammable decontaminant, which may also be used to neutralize organophosphorus agricultural chemicals.
Type:
Grant
Filed:
March 13, 1996
Date of Patent:
June 2, 1998
Assignee:
The United States of America as represented by the Secretary of the Navy
Abstract: There is described a process for preparing 3-(2-thienylthio)butyric acid by converting a compound having the formula (III): ##STR1## wherein R is a straight chain or branched C.sub.1 to C.sub.4 alkyl group, whereby the production of 3-(3-thienylthio)butyric acid as a by-product which is the position isomer can be controlled to at most 0.1 mol %. 3-(2-Thienylthio)butyric acid is a useful compound as an intermediate for a medicinal compound.
Abstract: Substituted thiophenylalkenylcarboxylic acid guanidides, processes for their preparation, their use as a medicament or diagnostic, and a medicament containing them.There are described substituted thiophenylalkenylcarboxylic acid guanidides of the formula I ##STR1## in which R(1) to R(5) have the meanings given in the claims, which are outstandingly active antiarrhythmic pharmaceuticals having a cardioprotective component and are outstandingly suitable for infarct prophylaxis and infarct treatment and also for the treatment of angina pectoris, where they also inhibit or greatly reduce the pathophysiological processes in the formation of ischemically induced damage, in particular in the initiation of ischemically induced cardiac arrhythmias, in a preventive manner.
Type:
Grant
Filed:
February 11, 1997
Date of Patent:
May 26, 1998
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Jan-Robert Schwark, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Andreas Weichert, Udo Albus, Wolfgang Scholz
Abstract: An amide derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents a C.sub.1-40 hydrocarbon; R.sup.2 represents a C.sub.1-6 alkylene; R.sup.3 represents H, OH or alkoxyl; R.sup.4 represents a C.sub.1-39 hydrocarbon; R.sup.5 represents ##STR2## with the proviso that when R.sup.5 represents ##STR3## R.sup.3 does not represent OH; and a composition of the amide derivative for topical application to human skin. The composition improves the barrier function of the stratum corneum, providing improvement and prevention of dermatitis, skin roughness, or similar disorders.
Abstract: The present invention relates to a novel method for treating a mammal suffering from or susceptible to schizophrenia and schizophreniform diseases.
Type:
Grant
Filed:
January 29, 1996
Date of Patent:
May 19, 1998
Assignee:
Novo Nordisk A/S
Inventors:
Franklin Porter Bymaster, Harlan E. Shannon
Abstract: This invention relates to certain polyamine derivatives, to the methods and intermediates useful for their preparation, and to their use in treating diseases caused by infestation with a variety of parasitic protozoa.
Type:
Grant
Filed:
March 15, 1994
Date of Patent:
May 19, 1998
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
David M. Stemerick, Alan J. Bitonti, Michael L. Edwards, Peter P. McCann, Albert Sjoerdsma
Abstract: Aromatic bromomethyl compounds play a major role in the synthesis of active substances. They can be obtained in particularly pure form by the free-radical bromination of aromatic methyl compounds in the solvent chlorobenzene.
Abstract: A process for preparing a surfactant composition comprising reacting an N-alkylpolyhydroxyamine and an alkoxylated triglyceride of a fatty acid to produce a mixture of a polyhydroxy-fatty amide, an alkoxylated monoglyceride of a fatty acid, and an alkoxylated diglyceride of a fatty acid, the resulting mixture providing a water soluble surfactant composition.
Abstract: The compounds of formula I: ##STR1## wherein R.sup.1, R.sup.4 and R.sup.5 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, trifluoromethyl, amino, mono- or di-alkylamino, alkanamido, or alkanesulfonamido; or, R.sup.1 is defined as above and R.sup.4 and R.sup.5, taken together, are ortho substituted methylenedioxy, ethylenedioxy, or propylenedioxy; R.sup.2 and R.sup.3 are, independently, hydrogen or alkyl; n is 3 or 4; or pharmaceutically acceptable salts thereof, are useful in the treatment of depression and related disorders.
Abstract: Tetrahydrofurans tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.
Abstract: Compounds of Formula I are selective autoreceptor agonists useful in treating disease states involving hyperactivity of dopamine systems: ##STR1## in which X is --(CH.sub.2).sub.n --; n is 1-3; R.sub.1 is hydrogen, alkyl, hydroxyalkyl, cycloalkyl-methyl, bicyclo-alkylmethyl or --(CH.sub.2).sub.m YAr; where m is 0-4, Y is --CH.sub.2 --, and Ar is phenyl, halophenyl, alkylphenyl, dialkylphenyl or alkoxyphenyl; R.sub.2 is hydrogen or alkyl; R.sub.3 is hydrogen, halogen, alkyl, alkoxy or hydroxy; or a pharmaceutically acceptable salt thereof.
Abstract: Substituted 2-phenylpyridines I ##STR1## where substituents have the meaning described in the specification and their use as herbicides; for the desiccation/defoliation of plants.
Type:
Grant
Filed:
July 3, 1997
Date of Patent:
May 5, 1998
Assignee:
BASF Aktiengesellschaft
Inventors:
Peter Schafer, Gerhard Hamprecht, Elisabeth Heistracher, Ralf Klintz, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
Abstract: This invention discloses methods of using certain aryl-benzo?b!thiophene and benzo?b!furan compounds to block or inhibit cannabinoid receptors in mammals. It also discloses novel compounds which are antagonists of the cannabinoid receptors and also discloses pharmaceutical formulations which contain the compounds as an active ingredient.
Type:
Grant
Filed:
September 30, 1996
Date of Patent:
May 5, 1998
Assignee:
Eli Lilly and Company
Inventors:
George J. Cullinan, Kennan J. Fahey, Gary A. Koppel
Abstract: The invention relates to 4-substituted isoxazole derivatives of formula I: ##STR1## wherein R, R.sup.1, R.sup.2, Q and n have the meanings defined in the description, which possess valuable herbicidal properties.
Type:
Grant
Filed:
May 1, 1997
Date of Patent:
May 5, 1998
Assignee:
Rhone-Poulenc Agriculture Ltd.
Inventors:
David Alan Roberts, Susan Mary Cramp, Derek Ian Wallis, Jean-Paul Bulot