Abstract: A method is disclosed for treatment of acute renal failure which comprises administering to a warm-blooded mammal manifesting acute renal failure a small but effective amount of zaprinast sufficient to effect acceleration of recovery from said acute renal failure.
Abstract: A method of inhibiting lentivirus is disclosed which comprises mammalian host susceptible to said lentivirus with a virally inhibitory effective amount of an O-acylated derivative of 1,5-dideoxy-1,5-imino-D-glucitol and their N-alkyl, N-acyl and N-aroyl derivatives in which from one to four of the free hydroxyl groups are O-acylated with carboxylic alkanoyl radicals selected from the group consisting of .omega.,.omega.,.omega.-trifluoroalkanoyl having from three to eight carbon atoms, carboxylic cycloalkanoyl groups having from four to eight carbon atoms and carboxylic acyclic alkanoyl groups having from two to ten carbon atoms, wherein the N-aroyl groups contain from 7 to 14 carbon atoms, the N-acyl groups contain from 4 to 8 carbon atoms and the N-alkyl groups contain from 1 to 14 carbon atoms.
Type:
Grant
Filed:
January 20, 1995
Date of Patent:
December 19, 1995
Inventors:
Richard A. Partis, Francis J. Koszyk, Richard A. Mueller
Abstract: A method is disclosed for inhibiting the biosynthesis of glycolipids in cells capable of producing glycolipids comprising subjecting said cells to a glycolipid inhibitory effective amount of an N-alkyl derivative of 1,5-dideoxy-1,5-imino-D-glucitol in which said alkyl contains from 2-8 carbon atoms.
Type:
Grant
Filed:
October 12, 1994
Date of Patent:
December 5, 1995
Assignee:
Monsanto Company
Inventors:
Frances M. Platt, Gabrielle R. Neises, Raymond A. Dwek, Terry D. Butters
Abstract: A cDNA clone having a base sequence for human tissue factor inhibitor (TFI) has been developed and characterized and the amino acid sequence of the TFI has been determined.
Type:
Grant
Filed:
July 15, 1993
Date of Patent:
November 14, 1995
Assignees:
Monsanto Company, Washington University
Inventors:
Tze-Chein Wun, Kuniko K. Kretzmer, George J. Broze, Jr.
Abstract: Novel 2-chloro and 2-bromo derivatives of 1,5-iminosugars are disclosed, especially such derivatives of 1,5-dideoxy-1,5-imino-D-glucitol. These compounds are useful inhibitors of glucosidase enzymes and also are useful as antiviral agents and as intermediates for the synthesis of other enzyme inhibitors and antiviral compounds.
Abstract: There is disclosed a method for providing for the coexpression of N-myristoyltransferase and a protein substrate for said N-myristoyltransferase in E. coli comprising introducing into E. coli a dual plasmid system comprising (A) the isopropyl-.beta.-D-thiogalactopyranoside-inducible tac promoter, the g10-L ribosome binding site, a NMT gene, the kanamycin resistance gene and the p15A origin of replication in operable sequence and (B) the recA promoter, the g10-L ribosome binding site, a mammalian gene, the ampicillin resistance gene and the Col E1 origin of replication in operable sequence. This allows production of mammalian N-myristoylproteins or proteins containing covalently linked analogs of myristate with altered physical-chemical properties.
Type:
Grant
Filed:
July 12, 1993
Date of Patent:
July 25, 1995
Assignee:
Washington University
Inventors:
Robert J. Duronio, Peter O. Olins, Jeffrey I. Gordon
Abstract: Novel derivatives of 1-deoxynojirimycin are disclosed which have amino or azido substituents at C-2 and/or C-3. These compounds are useful inhibitors of lentiviruses. Methods of chemical synthesis of these derivatives and intermediates therefor are also disclosed.
Type:
Grant
Filed:
October 17, 1994
Date of Patent:
July 25, 1995
Assignee:
G. D. Searle & Co.
Inventors:
Ish K. Khanna, Richard A. Mueller, Richard M. Weier
Abstract: A method of inhibiting lentivirus is disclosed which comprises mammalian host susceptible to said lentivirus with a virally inhibitory effective amount of an O-acylated derivative of 1,5-dideoxy-1,5-imino-D-glucitol and their N-alkyl, N-acyl and N-aroyl derivatives in which from one to four of the free hydroxyl groups are O-acylated with carboxylic alkanoyl radicals selected from the group consisting of .omega.,.omega.,.omega.-trifluoroalkanoyl having from three to eight carbon atoms, carboxylic cycloalkanoyl groups having from four to eight carbon atoms and carboxylic acyclic alkanoyl groups having from two to ten carbon atoms, wherein the N-aroyl groups contain from 7 to 14 carbon atoms, the N-acyl groups contain from 4 to 8 carbon atoms and the N-alkyl groups contain from 1 to 14 carbon atoms.
Type:
Grant
Filed:
December 21, 1993
Date of Patent:
May 2, 1995
Assignee:
G. D. Searle & Co.
Inventors:
Richard A. Partis, Francis J. Koszyk, Richard A. Mueller
Abstract: This invention discloses a method of treating cholera infection in a human by administering an effective amount of 1,5-dideoxy-1,5-imino-D-glucitol or a derivative thereof.
Type:
Grant
Filed:
May 13, 1993
Date of Patent:
March 21, 1995
Assignee:
Monsanto Company
Inventors:
Frances M. Platt, Gabrielle R. Neises, Raymond A. Dwek, Terry D. Butters
Abstract: Novel short peptides are disclosed that bind to the thrombospondin 1 receptor, which preferably have 5-13 amino acid residues which share the tripeptide Val-Val-Met and have the following sequences: RFYVVMWKQVTQS (Seq ID No. 1) and fragments thereof containing the minimal sequence RFYVVM, (Seq ID No. 3) and FIRVVMYEGKK (Seq ID No. 4) and fragments thereof containing the minimal sequence IRVVM (Seq ID No. 5).
Abstract: Azido-substituted fatty acid analogs which are useful in the fatty acid acylation of peptides and proteins and as antiviral agents are disclosed having the following chemical structure:Z--(CH.sub.2).sub.x COORwhereinZ=azido, tetrazolyl or triazolylR=H or C.sub.1 -C.sub.8 alkyl, andx=8-12.
Type:
Grant
Filed:
February 18, 1994
Date of Patent:
March 14, 1995
Assignee:
Washington University
Inventors:
Balekudru Devadas, Jeffrey I. Gordon, Steven P. Adams
Abstract: Novel derivatives of 1-deoxynojirimycin are disclosed which have amino or azido substituents at C-2 and/or C-3. These compounds are useful inhibitors of lentiviruses. Methods of chemical synthesis of these derivatives and intermediates therefor are also disclosed.
Type:
Grant
Filed:
December 20, 1993
Date of Patent:
February 21, 1995
Assignee:
G. D. Searle & Co.
Inventors:
Ish K. Khanna, Richard A. Mueller, Richard M. Weier
Abstract: Novel heptitol analogues of mannofuranose and their syntheses from .delta.-lactones of heptonic acids are disclosed. The novel heptitols are (A) 2,5-dideoxy-2,5-imino-D-glycero-D-talo-heptitol and (b) 1-amino-2,5-anydro-1-deoxy-D-glycero-D-talo-heptitol. These novel heptitol compounds are useful inhibitors of glycosidases.
Type:
Grant
Filed:
January 18, 1994
Date of Patent:
January 24, 1995
Assignee:
Monsanto Company
Inventors:
George W. J. Fleet, Bryan G. Winchester
Abstract: A method is disclosed for inhibiting nitric oxide formation in a warm blooded mammal afflicted with an acute or chronic inflammatory disease which comprises administering to said mammal an effective nitric oxide inhibitory amount of methyl-, or 1,1-dimethyl-, or amino-substituted guanidines.
Type:
Grant
Filed:
August 24, 1993
Date of Patent:
October 25, 1994
Assignee:
Washington University
Inventors:
Joseph R. Williamson, John A. Corbett, Michael L. McDaniel, Ronald G. Tilton
Abstract: Novel 2-alkyl carbinol derivatives of deoxynojirimycin (DNJ) and the chemical synthesis of these derivatives and intermediates therefor from DNJ and their method of inhibiting lentiviruses are disclosed.
Type:
Grant
Filed:
July 12, 1993
Date of Patent:
September 27, 1994
Assignee:
G. D. Searle & Co.
Inventors:
Ish K. Khanna, Richard A. Mueller, Richard M. Weier
Abstract: Novel tricyclic steriod analogs are disclosed which are 1H-benz[e]indene dodecahydro compounds that are useful for enhancing GABA-induced chloride currents at the GABA receptor/chloride ionophore complex and can be represented by the following structural formulas: ##STR1## wherein R.sub.1 =H or C.sub.1 -C.sub.4 alkyl or fluoroalkyl;R.sub.2 =H or C.sub.1 -C.sub.4 alkyl or fluoroalkyl, in which R.sub.1 and R.sub.2 can be the same or different;R.sub.3 =H or CH.sub.3 ;R.sub.4 =H or CH.sub.3, in which R.sub.3 and R.sub.4 can be the same or different;R.sub.5 =H;R.sub.6 =H;R.sub.5,R.sub.6 =.dbd.O(carbonyl);R.sub.7 =H;R.sub.8 =a hydrogen bond accepting group.R.sub.7,R.sub.8 =.dbd.O(carbonyl); andR'=an ester group.
Type:
Grant
Filed:
October 15, 1993
Date of Patent:
September 6, 1994
Assignee:
Washington University
Inventors:
Douglas F. Covey, Yuefei Hu, Charles F. Zorumski
Abstract: Novel inhibitors of retroviral protease, e.g., HIV protease, are provided which are peptides having from about 4 to about 8 amino acid residues and which are substrates for said protease derived from known cleavage sites and modified to contain an internal CH.sub.2 NH bond isostere.
Abstract: Novel derivatives of 1-deoxynojirimycin are disclosed which have thio or sulfinyl substituents at C-2 or C-3. These compounds are useful inhibitors of lentiviruses such as visna virus and human immunodeficiency virus. Methods of chemical synthesis of these derivatives and intermediates therefor are also disclosed.
Abstract: Azido-substituted fatty acid analogs which are useful in the fatty acid acylation of peptides and proteins and as antiviral agents are disclosed having the following chemical structure:Z--(CH.sub.2).sub.x COORwhereinZ=azido, tetrazolyl or triazolylR=H or C.sub.1 -C.sub.8 alkyl, andx=8-12.
Type:
Grant
Filed:
October 20, 1992
Date of Patent:
August 16, 1994
Assignee:
Washington University
Inventors:
Balekudru Devadas, Jeffrey I. Gordon, Steven P. Adams