R Contains Benzene Ring Patents (Class 514/615)
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Patent number: 6809090Abstract: N-(imino)amines and their preparation and their use as NO synthase inhibitors and selective or non-selective traps for a reactive oxygen species.Type: GrantFiled: July 1, 2003Date of Patent: October 26, 2004Inventors: Dennis Bigg, Pierre-Etienne Chabrier de Lassauniere, Serge Auvin, Jeremiah Harnett, Gérard Ulibarri
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Patent number: 6800660Abstract: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ═O or ═S.Type: GrantFiled: July 10, 2002Date of Patent: October 5, 2004Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono
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Publication number: 20040152769Abstract: Prodrugs having a hydrolyzable carbamate moiety, compositions including the prodrugs, methods of preparing the prodrugs and methods of treatment using the prodrugs are disclosed. The prodrug has the formula DC(X)XR, where D is a biologically active agent, X is O, S or NR′, and R is a moiety that modifies various properties of the biologically active agent. The biologically active agent either includes a functional group such as an amide, thioamide, imide, thioimide, urea, thiourea, carbamate, thiocarbamate, sulfonamide, or sulfonimide group, or includes a hydroxy, amine, carboxylic acid or thiol group that is modified to include such a group. An NH group from the biologically active agent can be coupled to an activated form the C(X)XR moiety to form the prodrugs described herein. Relative to a conventional carbamate group, the presence of the additional carbonyl or sulfonyl group makes the carbamate group more susceptible to hydrolysis.Type: ApplicationFiled: November 7, 2003Publication date: August 5, 2004Inventors: Nnochiri Nkem Ekwuribe, Jennifer Riggs-Sauthier, Tatyana A. Dyakonov
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Patent number: 6696472Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenoxy-N-phenyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: February 24, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20040005354Abstract: Oral trimethobenzamide compositions and methods for treating and controlling nausea and/or vomiting are disclosed in warm blooded animals, especially humans including children. The oral trimethobenzamide compositions and methods of the present invention are at least as effective as a 200 mg intramuscular (I.M.) trimethobenzamide HCl injectable formulation. In addition, an oral composition containing about 300 mg of trimethobenzamide HCl is uniquely approximately bioequivalent to a 200 mg intramuscular (I.M.) trimethobenzamide HCl injectable formulation. The oral pediatric trimethobenzamide compositions and methods of the present invention are believed to be at least as effective as a 200 mg intramuscular (I.M.) trimethobenzamide HCl injectable formulation when administered at a dose of about 100 mg. In addition, an oral pediatric composition containing about 120 mg of trimethobenzamide HCl is believed to be uniquely approximately bioequivalent to a 200 mg intramuscular (I.M.Type: ApplicationFiled: February 6, 2003Publication date: January 8, 2004Applicant: King Pharmaceuticals, Inc.Inventors: Jefferson J. Gregory, Robert G. Bruns, Dean R. Cirotta, Thomas K. Rogers, Charles L. Pamplin
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Patent number: 6673777Abstract: There is disclosed a method for treating diseases and disorders involving T cell activation and HIV-infection, using the p38 mitogen activated protein kinase (MAPK) signaling pathway as a target for intervention. There is further disclosed a use for guanylhydrazone-substituted compounds to treat diseases and disorders related to T cell activation and HIV-infection.Type: GrantFiled: November 2, 2000Date of Patent: January 6, 2004Assignee: Cytokine PharmaSciences, Inc.Inventors: Kevin J. Tracey, Pamela Cohen, Michael Bukrinsky, Helena Schmidtmayerova
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Patent number: 6670394Abstract: This invention relates to a method for the prophylaxis of or for treating COPD by administering a PDE4 inhibitor which has a defined therapeutic ratio.Type: GrantFiled: August 31, 2001Date of Patent: December 30, 2003Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Mary S. Barnette, Theodore J. Torphy
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Publication number: 20030225126Abstract: The present invention relates generally to the field of bacteriology. More particularly, the present invention provides methods and compositions for increasing the effectiveness of existing antibacterial agents and methods of overcoming bacterial resistance. Specifically, the invention provides methods of enhancing the action of an antibacterial agent by use of an antibiotic potentiator. Compositions of antibiotic potentiators including an acyl hydrazide, an oxy amide, and an 8-hydroxy quinoline also are disclosed.Type: ApplicationFiled: March 23, 2001Publication date: December 4, 2003Applicant: Influx, Inc.Inventors: Penelope N. Markham, Debbie C. Mulhearn, Ekaterina A. Klyachko, Alexander A. Neyfakh, David Crich, Mohamed-Rami Jaber, Michael E. Johnson
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Patent number: 6653321Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.Type: GrantFiled: July 28, 2000Date of Patent: November 25, 2003Assignee: Telik, Inc.Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
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Publication number: 20030212068Abstract: 1Type: ApplicationFiled: April 28, 2003Publication date: November 13, 2003Applicant: ASTRAZENECA ABInventors: Dearg S. Brown, George R. Brown
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Publication number: 20030195258Abstract: Disclosed is a compound represented by the Structural Formula (I): 1Type: ApplicationFiled: January 15, 2003Publication date: October 16, 2003Applicant: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono
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Patent number: 6620840Abstract: N-(imino)amines and their preparation and their use as NO synthase inhibitors and selective or non-selective traps for a reactive oxygen species.Type: GrantFiled: September 26, 2002Date of Patent: September 16, 2003Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Dennis Bigg, Pierre-Etienne Chabrier de Lassauniere, Serge Auvin, Jeremiah Harnett, Gérard Ulibarri
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Publication number: 20030149103Abstract: The present invention provides functionalized cyclopropane compounds that have pesticidal and/or TMOF activity. The pesticidal compounds and other compounds of the present invention are usefully employed in the control of pests, particularly insect pests such as mosquitoes, which ingest blood.Type: ApplicationFiled: December 13, 2001Publication date: August 7, 2003Inventor: Russell J. Linderman
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Publication number: 20030105078Abstract: The invention relates to novel diphenyl derivatives, to processes for their preparation and to their use in medicaments.Type: ApplicationFiled: February 26, 2002Publication date: June 5, 2003Inventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Christiane Faeste, Hilmar Bischoff, Axel Kretschmer, Verena Vohringer, Peter Ellinghaus
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Patent number: 6528685Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.Type: GrantFiled: October 19, 1999Date of Patent: March 4, 2003Assignees: Teva Pharmaceutical Industries, Ltd., Technion Research and Development Foundation, Ltd.Inventors: Sasson Cohen, Yaacov Herzig, Ruth Levy, Mitchell Shirvan, Jeff Sterling, Alex Veinberg, Moussa B. H. Youdim, John P. M. Finberg
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Patent number: 6489363Abstract: Pharmaceutical compositions of modafinil compounds, and pharmaceutical, non-aqueous compositions of modafinil compounds in organic solvents are disclosed, along with their use in the treatment of diseases.Type: GrantFiled: October 10, 2001Date of Patent: December 3, 2002Assignee: Cephalon, Inc.Inventors: Martin J. Jacobs, Bradley T. McIntyre, Piyush R. Patel
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Patent number: 6468982Abstract: Methods of prophylactic and therapeutic immunization of an individual against pathogen infection, diseases associated with hyperproliferative cells and autoimmune diseases are disclosed. The methods comprise the steps of administering to cells of an individual, a nucleic acid molecule that comprises a nucleotide sequence that encodes a protein which comprises at least one epitope that is identical or substantially similar to an epitope of a pathogen antigen, a hyperproliferative cell associated protein or a protein associated with autoimmune disease respectively. In each case, nucleotide sequence is operably linked to regulatory sequences to enable expression in the cells. The nucleic acid molecule is free of viral particles and capable of being, expressed in said cells. The cells may be contacted cells with a cell stimulating agent. Methods of prophylactically and therapeutically immunizing an individual against HIV are disclosed.Type: GrantFiled: June 23, 1997Date of Patent: October 22, 2002Assignees: The Trustees of the University of Pennsylvania, The Wistar InstituteInventors: David B. Weiner, William V. Williams, Bin Wang
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Patent number: 6436421Abstract: The present invention relates to pesticide compositions. In particular, the present invention relates to pesticide compositions comprising a pesticide and a redispersible polymer and to a method for controlling agricultural pests by applying to the pest or the locus of the pest a pesticide composition comprising a pesticide and a redispersible polymer.Type: GrantFiled: February 27, 1998Date of Patent: August 20, 2002Assignee: ?Rohm and Haas CompanyInventors: Frederick James Schindler, Yili Guo, Gregory C. Pierce, James Allen Quinn
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Patent number: 6433017Abstract: In accordance with the present invention, there are provided amphiphilic polyamine compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.Type: GrantFiled: February 28, 2001Date of Patent: August 13, 2002Assignee: Gene Therapy Systems, Inc.Inventors: Philip L. Felgner, Xiang Gao, Jing Ling
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Patent number: 6410600Abstract: The invention relates to novel azines, to a process for their preparation and to their use as fungicides.Type: GrantFiled: October 19, 2000Date of Patent: June 25, 2002Assignee: Bayer AktiengesellschaftInventors: Dirk Backhaus, Bernd-Wieland Krüger, Peter Gerdes, Herbert Gayer, Martin Vaupel, Klaus Stenzel
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Patent number: 6376548Abstract: This invention relates to enhanced propertied pesticides which can be used as fungicides, herbicides, insecticides, rodenticides or biocides, compositions comprising enhanced propertied pesticides, and the method of use of enhanced propertied pesticides and their compositions. It has been found that certain pesticidal compounds can be substituted with a moiety which comprises a substituent which enhances or changes the properties of the pesticidal compound. Additionally, some of the compounds of this invention may comprise two pesticidal components which can be different from one another. The invention relates also to pesticidal compositions comprising a pesticidal compound of this invention and an pesticidally acceptable carrier as well as methods of controlling a pest comprising applying a pesticidally effective amount of a composition comprising a compound of this invention and a pesticidally acceptable carrier to the pest, to the locus of the pest or to the growth medium of said pest.Type: GrantFiled: January 28, 2000Date of Patent: April 23, 2002Assignee: Rohm and Haas CompanyInventors: Mark Joseph Mulvihill, Steven Howard Shaber
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Patent number: 6369111Abstract: The invention relates to novel substituted oximes, to a process for their preparation and to their use as fungicides.Type: GrantFiled: May 30, 2001Date of Patent: April 9, 2002Assignee: Bayer AktiengesellschaftInventors: Dirk Backhaus, Herbert Gayer, Stefan Hillebrand, Peter Gerdes, Martin Vaupel, Astrid Mauler-Machnik
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Patent number: 6369108Abstract: A method for treating COPD is disclosed comprising administering compounds of Formula (I) wherein the terms R1, R3, X, X2 and Z are herein defined.Type: GrantFiled: June 28, 2000Date of Patent: April 9, 2002Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Theodore Torphy
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Publication number: 20020035157Abstract: The present invention relates to a pharmaceutical composition comprising a nitrate vasodilator and a compound of formula I.Type: ApplicationFiled: March 7, 2001Publication date: March 21, 2002Inventor: Gary McCleane
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Patent number: 6348499Abstract: Amphiphilic polyamide compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.Type: GrantFiled: November 24, 1999Date of Patent: February 19, 2002Assignee: Gene Therapy Systems, Inc.Inventors: Philip L. Felgner, Xiang Gao, Jing Ling
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Publication number: 20010044151Abstract: This invention relates to an improved method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The improvement resides in a select group of non-steroid ligands which show improved activity over known ligands.Type: ApplicationFiled: April 12, 2001Publication date: November 22, 2001Inventors: Glenn Richard Carlson, Dean Ervin Cress, Tarlochan Singh Dhadialla, Robert Eugene Hormann, Dat Phat Le
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Patent number: 6319894Abstract: There is disclosed a complex and a combination of the glycosylated polypeptide fetuin and a therapeutically active small molecule compound having a net positive charge at physiological pH. The presence of fetuin as a drug complex or in combination with the therapeutically active small molecule compound enhances therapeutic activity of the small molecule compound. The present invention further provides a means for screening for therapeutically active small molecule compounds by means of binding to fetuin.Type: GrantFiled: January 8, 1997Date of Patent: November 20, 2001Assignee: The Picower Institute for Medical ResearchInventors: Kevin Tracey, Haichao Wang
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Patent number: 6300519Abstract: There are described compounds of formula I*, wherein R1 is lower alkoxycarbonyl, R2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C4-C8cycloalkyl, R4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, suffinyl (—SO—) and sulfonyl (—SO2—) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R5, independently of R2, has one of the meanings mentioned for R2, and R6, independently of R1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.Type: GrantFiled: November 23, 1999Date of Patent: October 9, 2001Assignee: Novartis Finance CorporationInventors: Alexander Fässler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
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Patent number: 6271263Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.Type: GrantFiled: March 2, 1999Date of Patent: August 7, 2001Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Benjamin Sklarz, Ramy Lidor, Eliezer Bahar, Yaacov Herzig, Jeff Sterling, Alex Veinberg
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Patent number: 6248787Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 6, 1995Date of Patent: June 19, 2001Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 6242494Abstract: A class of substituted b-amino acids are potent inhibitor of methionine aminopeptidase type 2 (MetAP2) and are thus useful in inhibiting angiogenesis and disease conditions which depend upon angiogenesis for their development such as diabetic retinopathy, tumor growth, and conditions of inflammation. Pharmaceutical compounds containing the compounds and methods of inhibiting methionine aminopeptidase-2, and angiogenesis are also disclosed.Type: GrantFiled: April 30, 1999Date of Patent: June 5, 2001Assignee: Abbott LaboratoriesInventors: Richard A. Craig, Jack Henkin, Megumi Kawai, Linda M. Lynch, Jyoti Patel, George S. Sheppard, Jieyi Wang
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Patent number: 6221915Abstract: The present invention relates to a pharmaceutical composition comprising a nitrate vasodilator and a compound of formula I:Type: GrantFiled: March 30, 1999Date of Patent: April 24, 2001Inventor: Gary McCleane
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Patent number: 6172108Abstract: Compounds of formula (I): R—NH—A—CO—NH—NH—(W)n—Z (I) wherein: n is 0 or 1, W represents —CO— or S(O)r wherein r is 0, 1 or 2, Z represents a group selected from aryl, arylalkyl, heteroaryl and heteroarylalkyl, each optionally substituted, R represents a grouping selected from: Z1—T—CO—, Z1—O—T—CO—, Z1—T—O—CO—, Z1—T—S(O)q— wherein Z1, T and q are as defined in the description, A represents alkylene, alkenylene or alkynylene each having from 3 to 8 carbon atoms, alkylenecycloalkylene, cycloalkylenealkylene, alkylenecycloalkylenealkylene, alkylenearylene, arylenealkylene, alkylenearylenealkylene a grouping wherein B1 is as defined in the description, or A forms with the adjacent nitrogen atom a grouping as defined in the description, and medicinal products containing the same which are useful as Neuropeptide Y receptorType: GrantFiled: December 16, 1999Date of Patent: January 9, 2001Assignee: Adir et CompagnieInventors: Antonio Monge Vega, Ignacio Aldana Moraza, Daniel-Henri Caignard, Jacques Duhault, Jean Boutin, Odile Dellazuana
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Patent number: 6143728Abstract: There is disclosed a method for treating diseases and disorders involving T cell activation and HIV-infection, using the p38 mitogen activated protein kinase (MAPK) signaling pathway as a target for intervention. There is further disclosed a use for guanylhydrazone-substituted compounds to treat diseases and disorders related to T cell activation and HIV-infection.Type: GrantFiled: November 14, 1997Date of Patent: November 7, 2000Assignee: The Picower Institute for Medical ResearchInventors: Kevin J. Tracey, Pamela Cohen, Michael Bukrinsky, Helena Schmidtmayerova
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Patent number: 6130248Abstract: This invention relates to compositions for and methods of treating, preventing or ameliorating cancer and other proliferative diseases as well as methods of inducing wound healing, treating cutaneous ulcers, treating gastrointestinal disorders, treating blood disorders such as anemias, immunomodulation, enhancing recombinant gene expression, treating insulin-dependent patients, treating cystic fibrosis patients, inhibiting telomerase activity, treating virus-associated tumors, especially EBV-associated tumors, augmenting expression of a tumor suppressor gene and inducing tolerance to an antigen. The methods of the invention use tricarboxylic acid substituted oxyalkyl esters.Type: GrantFiled: December 30, 1996Date of Patent: October 10, 2000Assignees: Bar-ILAn University, Mor Research Applications, Ltd., Beacon Laboratories, Inc.Inventors: Abraham Nudelman, Ada Rephaeli
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Patent number: 6124356Abstract: A fungicidal compound of formula (I): or a stereoisomer thereof, wherein A is CH or N, B is OCH.sub.3 or NHCH.sub.3, E is --NR.sup.1 --C(CH.sub.3).dbd.N-- or --N.dbd.C(CH.sub.3)--NR.sup.1 --, R.sup.1 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl or optionally substitute benzyl, R.sup.2 is H, C.sub.1-4 alkyl, halo(C.sub.1-4)alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl, and R.sup.3 is optionally substituted aryl or optionally substituted heterocyclyl.Type: GrantFiled: January 6, 1999Date of Patent: September 26, 2000Assignee: Zeneca LimitedInventors: George Tseriotis, Ian Henry Aspinall, Paul Anthony Worthington
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Patent number: 6077869Abstract: This invention relates to the use of compounds of formula I as selective COX-2 inhibitors and antiinflammatory agents: ##STR1## wherein: X and Y are selected from hydrogen, halogen, alkyl, nitro, amino or other oxygen and sulfur containing functional groups such as hydroxy, methoxy and methylsulfonyl.Type: GrantFiled: October 20, 1999Date of Patent: June 20, 2000Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Zhihua Sui, Michael Wachter
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Patent number: 6077866Abstract: Novel benzophenonehydrazone derivatives represented by the formula (I): ##STR1## wherein, R.sup.1 is halogen; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is cyano, optically substituted C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-4 alkynyl, C.sub.1-4 alkyl-carbonyl or C.sub.1-4 alkoxy-thiocarbonyl; R.sup.4 is hydrogen, phenyl, optionally substituted C.sub.1-6 alkyl, optionally substituted C.sub.2-8 alkenyl, --CO--R.sup.8, --CO--O--R.sup.9 or ##STR2## R.sup.5 is hydrogen, formyl, phenyl, optionally substituted C.sub.1-8 alkyl, optionally substituted C.sub.2-8 alkenyl, optionally substituted C.sub.3-8 alkynyl, optionally substituted C.sub.1-8 alkyl-arbonyl, optionally substituted C.sub.1-6 alkyl-oxalyl, optionally substituted C.sub.1-8 alkoxy-carbonyl, optionally substituted C.sub.1-8 alkoxy-oxalyl, optionally substituted C.sub.3-8 cycloalkyl-carbonyl, optionally substituted C.sub.2-8 alkenyl-carbonyl or optionally substituted benzoyl; R.sup.6 is hydrogen or halogen; R.sup.7 is hydrogen, halogen or C.sub.Type: GrantFiled: May 10, 1996Date of Patent: June 20, 2000Assignee: Nihon Bayer Agrochem K.K.Inventors: Yoshinori Kitagawa, Katsuaki Wada, Yoshiko Kyo, Yuichi Otsu, Yumi Hattori, Toru Obinata, Takahisa Abe, Katsuhiko Shibuya, Wolfram Andersch
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Patent number: 6075044Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.Type: GrantFiled: July 17, 1998Date of Patent: June 13, 2000Assignee: The Regents of the University of CaliforniaInventors: Ching C. Wang, John Somoza, Jon P. Page, Ronaldus Marcellus Alphonsus Knegtel, Irwin D. Kuntz, Connie M. Oshiro, A. Geoffrey Skillman
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Patent number: 6043282Abstract: Azinooxime ethers of the formula I ##STR1## (X=NOCH.sub.3, CHOCH.sub.3, CHCH.sub.3 ; Y=O, NZ, where Z=H, alkyl; R.sup.1 =H, alkyl; R.sup.2 =cyano, nitro, trifluoromethyl, halogen, alkyl, alkoxy; m=0, 1, 2, it being possible for the radicals R.sup.2 to be different if m=2; R.sup.3 =H, cyano, alkyl, haloalkyl, alkoxy, cycloalkyl; R.sup.4, R.sup.5, R.sup.6 =indepedently of one another H, unsubst. or subst. alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl), and their salts, processes and intermediates for their preparation and their use for controlling harmful fungi and animal pests.Type: GrantFiled: July 29, 1998Date of Patent: March 28, 2000Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Klaus Oberdorf, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Bernd Muller, Ruth Muller, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6028110Abstract: A pharmaceutical or veterinary composition comprising a compound of formula I ##STR1## wherein X is a --CO.sub.2 H group and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 are as defined in the specification, or a salt, hydrate or solvate thereof, and a pharmaceutically or veterinarily acceptable excipient or carrier. A method of treatment of diseases or conditions mediated by MMPs in mammals, such as rheumatoid arthritis, osteoarthritis, periodontitis, gingivitis, corneal ulceration or tumour invasion by secondary means, by administering to the mammal an effective amount of the composition.Type: GrantFiled: November 22, 1996Date of Patent: February 22, 2000Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Andrew Miller, Raymond Paul Beckett, Fionna Mitchell Martin, Mark Whittaker
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Patent number: 6022900Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 6, 1995Date of Patent: February 8, 2000Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 6013671Abstract: This invention relates to insecticidal compositions comprising one or more substituted N,N'-dibenzoyl-N'-tert-alkyl-hydrazines and diethyl maleate which exhibit improved activity as insecticides when compared to compositions without diethylmaleate.Type: GrantFiled: January 19, 1999Date of Patent: January 11, 2000Assignee: Rohm and Haas CompanyInventors: Dat Phat Le, Guy Julius Smagghe
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Patent number: 6013836Abstract: This invention relates to N'-substituted-N,N'-disubstitutedhydrazines of formula I ##STR1## wherein X and X' are independently O, S, or NR; A' and B' are independently substituted or unsubstituted aryl or aromatic heterocycle; wherein F is alkyl, alkenyl, or aralkyl; and wherein E is a tertiary carbon containing organic radical having a total of at least four carbon and halogen atoms but not more than six halogen atoms, or a non-tertiary carbon containing non-haloalkyl organic or organometallic radical having at least five atoms other than hydrogen, oxygen and halogen which are useful as insecticides, compositions containing those compounds, methods of producing the compounds, and methods of their use. More particularly, the invention relates to insect growth regulating compounds and compositions, and methods of using such compounds and compositions. Compounds of the present invention are particularly suitable for controlling plant-destructive insects in crops of cultivated plants, ornamentals and forestry.Type: GrantFiled: May 22, 1995Date of Patent: January 11, 2000Assignee: Rohm and Haas CompanyInventors: Adam Chi-Tung Hsu, Harold Ernest Aller, Dat Phat Le, Donald Wesley Hamp, Barry Weinstein, Raymond August Murphy
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Patent number: 6008255Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 6, 1995Date of Patent: December 28, 1999Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 6005009Abstract: Methods of inhibiting fibrosis comprising administering certain pyridoxal benzoyl hydrazones or analogs thereof are disclosed. Preferred hydrazones are pyridoxal benzoyl hydrazone, 3-hydroxyisonicotinaldehyde benzoyl hydrazone and salicylaldehyde benzoyl hydrazone. The methods are useful in treating fibrosing disorders, including dermal fibrosing disorders, fibrosis of internal organs and fibrotic conditions of the eye.Type: GrantFiled: March 20, 1997Date of Patent: December 21, 1999Assignee: Duke UniversityInventors: Saood Murad, Sheldon R. Pinnell, Huanshu Yang
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Patent number: 5990171Abstract: The invention concerns hydrazonoacetic acid amides of general formula (I), a process for producing them, and the use of the said amides as pesticides. In the formula shown, the following meanings apply: A stands for a simple bond or optionally substituted alkylene; Q stands for oxygen or sulphur, R.sup.1 stands for optionally substituted cycloalkyl, cycloalkenyl, aryl or heterocyclyl; R.sup.2 stands for hydrogen or optionally substituted alkyl, cycloalkyl, cycloalkenyl, aryl or heterocyclyl; R.sup.3 and R.sup.4 are identical or different and each stand for hydrogen or optionally substituted alkyl or cycloalkyl; R.sup.2 and R.sup.3 together with the nitrogen atom to which they are bound form an optionally substituted heterocyclyl ring; R.sup.5 stands for optionally substituted cycloalkyl, cycloalkenyl, aryl or heterocyclyl.Type: GrantFiled: September 25, 1997Date of Patent: November 23, 1999Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Klaus Stenzel
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Patent number: 5981505Abstract: Methods of inducing genetic material into cells of an individual and compositions and kits for practicing the same are disclosed. The methods comprise the steps of contacting cells of an individual with a polynucleotide function enhancer and administering to the cells, a nucleic acid molecule that is free of retroviral particles. The nucleic acid molecule comprises a nucleotide sequence that encodes a protein that comprises at least one epitope that is identical or substantially similar to an epitope of a pathogen antigen or an antigen associated with a hyperproliferative or autoimmune disease, a protein otherwise missing from the individual due to a missing, non-functional or partially functioning gene, or a protein that produces a therapeutic effect on an individual. Methods of prophylactically and therapeutically immunizing an individual against HIV are disclosed. Pharmaceutical compositions and kits for practicing methods of the present invention are disclosed.Type: GrantFiled: November 26, 1997Date of Patent: November 9, 1999Assignees: The Trustees of The University of Pennsylvania, The Wistar InstituteInventors: David B. Weiner, William V. Williams, Bin Wang
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Patent number: 5932616Abstract: The present invention provides the compound having the structure: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8.Type: GrantFiled: April 4, 1994Date of Patent: August 3, 1999Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia Univerisity in the City of New YorkInventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind, Branko Jursic
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Patent number: 5919816Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.Type: GrantFiled: October 17, 1997Date of Patent: July 6, 1999Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Thomas J. Dodd