Benzene Ring Bonded Directly To Urea Nitrogen Patents (Class 514/596)
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Patent number: 6608066Abstract: The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treating or prophylaxis of undesired thrombosis.Type: GrantFiled: October 27, 2000Date of Patent: August 19, 2003Assignee: Sunol Molecular CorporationInventors: Jin-An Jiao, Lawrence K. Luepschen, Esperanza L. Nieves, Hing C. Wong, Dean P. Taylor
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Patent number: 6593362Abstract: This invention relates to pharmaceutical compositions and methods of using non-peptidic cyclophilin-binding compounds in medical conditions involving breakdown of mitochondrial energy metabolism induced by calcium overload, in treating alopecia and promoting hair growth, in treating infections with filarial and helmintic parasites, and in treating and preventing infections with the human immunodeficiency virus.Type: GrantFiled: May 21, 2001Date of Patent: July 15, 2003Assignee: Guilford Pharmaceuticals Inc.Inventors: Joseph P. Steiner, Gregory S. Hamilton
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Publication number: 20030130309Abstract: Disclosed are methods of treating certain cytokine mediated diseases or conditions using novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein.Type: ApplicationFiled: July 1, 2002Publication date: July 10, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Neil Moss, John Robinson Regan
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Publication number: 20030114517Abstract: A novel class of compounds such as antagonists of the neuropeptide Y Y5 receptor, methods of making such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more diseases associated with the neuropeptide Y Y5 receptor are disclosed.Type: ApplicationFiled: March 12, 2002Publication date: June 19, 2003Inventors: William J. Greenlee, Ying Huang, Joseph M. Kelly, Stuart W. McCombie, Andrew W. Stamford, Yusheng Wu
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Publication number: 20030100608Abstract: Disclosed are compounds of the formula (I) shown below which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds.Type: ApplicationFiled: May 24, 2002Publication date: May 29, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Eugene R. Hickey
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Patent number: 6566304Abstract: The invention relates to use of (a) compounds of phosphorus containing at least partly lipophilic organic radicals together with (b) urea and/or urea derivatives in selected quantity ratios of (a) to (b) as a soil additive for biologically controlling plant-parasitic soil nematodes by strengthening the correspondingly antagonistic soil potential, more particularly by strengthening the growth of antagonistic and/or nematicidal rhizosphere bacteria and/or corresponding mycorrhiza strains—and at the same time strengthening the growth of cultivated plants in soil. The multicomponent mixtures which strengthen bacterial growth are preferably introduced into the region of the plant roots in the form of an aqueous preparation using plant-compatible emulsifiers before and/or during plant growth. Components (a) and (b) are used in such quantity ratios that the ratio by weight of C to N is no higher than 6:1 and preferably no higher than 5:1.Type: GrantFiled: February 6, 2001Date of Patent: May 20, 2003Assignee: Cognis Deutschland GmbHInventors: Doris Bell, Bettina Kopp-Holtwiesche, Stephan Von Tapavicza
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Patent number: 6548539Abstract: Compounds of the general structure according to Formula (I) wherein R1 is selected from alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, and heterocycloalkyl; R2 is selected from alkyl, alkenyl, alkyny, heteroalkyl, haloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, and heterocycloalkylalkyl; R3 is selected from aryl, heteroaryl, cycloalkyl, and heterocycloalkyl; W is selected from Ch2, O and S; n is 0 to about 3: X is selected from S or O; Y, if present, is selected from a bond, aryl, NH, NR, O or S, where R3 is selected from hydrogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, and heterocycloalkylalkyl; and Z, if present, can represent a bond or is selected from lower alkyl, O or S are disclosed. Also disclosed are uses of such compounds for treating a variety of disease conditions, including cancer.Type: GrantFiled: March 5, 2002Date of Patent: April 15, 2003Assignee: Avalon PharmaceuticalsInventors: Stanislaw Pikul, Daniel R. Soppet, Paul E. Young
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Patent number: 6541473Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.Type: GrantFiled: September 17, 2001Date of Patent: April 1, 2003Assignee: Warner Lambert CompanyInventors: Stuart E. Bradley, Eric W. Collington, Matthew C. Fyfe, William T. Gattrell, Joanna V. Geden, Peter J. Murray, Martin J. Procter, Robert J. Rowley, Jonathan G. Williams
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Patent number: 6538031Abstract: A method of successfully controlling sea lice in commercial fish farming, in an efficient and environmentally friendly way, with the compounds named in claim 1, preferably by injection, and a method of automating this type of control, are described.Type: GrantFiled: November 20, 2000Date of Patent: March 25, 2003Assignee: Novartis Animal Health US, Inc.Inventor: Hariolf Schmid
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Publication number: 20030055009Abstract: This invention relates to pharmaceutical compositions and methods of using non-peptidic cyclophilin-binding compounds in medical conditions involving breakdown of mitochondrial energy metabolism induced by calcium overload, in treating alopecia and promoting hair growth, in treating infections with filarial and helmintic parasites, and in treating and preventing infections with the human immunodeficiency virus.Type: ApplicationFiled: May 21, 2001Publication date: March 20, 2003Inventors: Joseph P. Steiner, Gregory S. Hamilton
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Patent number: 6531506Abstract: The invention provides compounds that inhibit epoxide hydrolase in therapeutic applications for treating hypertension. A preferred class of compounds for practicing the invention have the structure shown by Formula I wherein Z is oxygen or sulfur, W is carbon phosphorous or sulfur, X and Y is each independently nitrogen, oxygen, or sulfur, and X can further be carbon, at least one of R1-R4 is hydrogen, R2 is hydrogen when X is nitrogen but is not present when X is sulfur or oxygen, R4 is hydrogen when Y is nitrogen but is not present when Y is sulfur or oxygen, R1 and R3 is each independently C1-C20 substituted or unsubstituted alkyl, cycloalkyl, aryl, acyl, or heterocyclic.Type: GrantFiled: November 21, 2000Date of Patent: March 11, 2003Assignee: Regents of the University of CaliforniaInventors: Deanna L. Kroetz, Darryl C. Zeldin, Bruce D. Hammock, Christophe Morisseau
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Patent number: 6531499Abstract: Peptoid compounds of Formula I and Formula II are disclosed The compounds are useful in the treatment of matrix metalloproteinase-mediated disorders.Type: GrantFiled: July 23, 2001Date of Patent: March 11, 2003Assignee: Wisconsin Alumni Research FoundationInventors: Donald T. Witiak, Paul J. Bertics, Yingsheng Zhang
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Patent number: 6500864Abstract: Novel disulfide derivatives useful for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The disulfide derivatives act as mast cell stabilizers.Type: GrantFiled: May 22, 2002Date of Patent: December 31, 2002Assignee: Alcon Universal Ltd.Inventors: Zixia Feng, Mark R. Hellberg, Steven T. Miller
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Patent number: 6492419Abstract: A topically acceptable aqueous pour-on formulation adapted for localized external application to an animal, which format includes an effective amount of a water insoluble insect growth regulator (IGR), a suspending agent, a surfactant or mixture of surfactants, and an aqueous carrier.Type: GrantFiled: August 15, 2000Date of Patent: December 10, 2002Assignee: Schering-Plough Animal Health Corp.Inventor: Stanley Shepherd
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Publication number: 20020183315Abstract: The present invention discloses compounds useful in treating or preventing IMPDH-associated disorders, such as transplant rejection and autoimmune diseases, having the formula (I), 1Type: ApplicationFiled: May 23, 2002Publication date: December 5, 2002Inventors: Edwin J. Iwanowicz, Katerina Leftheris, Chunjian Liu, Toomas Mitt, Scott H. Watterson
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Publication number: 20020165275Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins, and to pharmaceutical compositions comprising one or more of the said compounds. The invention further relates to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders.Type: ApplicationFiled: January 25, 2002Publication date: November 7, 2002Inventors: Yong-Qian Wu, Sergei Belyakov, Gregory S. Hamilton, David Limburg, Joseph P. Steiner, Mark Vaal, Ling Wei, Douglas Wilkinson
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Publication number: 20020165223Abstract: Compounds represented by structural formula I 1Type: ApplicationFiled: September 12, 2001Publication date: November 7, 2002Inventors: William J. Greenlee, Ying Huang, Joseph M. Kelly, Stuart W. McCombie, Andrew W. Stamford, Yusheng Wu
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Publication number: 20020161040Abstract: Use of at least one aminophenol derivative of formula (I) below: 1Type: ApplicationFiled: April 19, 2002Publication date: October 31, 2002Applicant: L'OREALInventors: Michel Philippe, Remy Tuloup, Christian Blaise
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Patent number: 6469067Abstract: An active ingredient combination for the simultaneous control of ecto- and endoparasites, especially mites, ticks and nematodes, on productive livestock, domestic animals and pets, is described, which comprises the active ingredients (1) 1-[4-chloro-3-(3-chloro-5-trifluoromethyl-2-pyridyloxy)phenyl]-3-(2,6-difluorobenzoyl)urea and (2) a compound of formula (i) wherein R1 is hydrogen or one of radicals R2 is —CH(CH3)—CH3, —CH(CH3)—C2H5, —C(CH3)═CH—CH(CH3)2 or cyclohexyl; R3 is hydrogen or hydroxy if the bond between atoms 22 and 23 represents a double bond, or is hydrogen or the group ═N—O—CH3 if a single bond is present between atoms 22 and 23; and R4 is HO— or HO—N═, in free form or in the form of a physiologically acceptable salt.Type: GrantFiled: November 20, 2000Date of Patent: October 22, 2002Assignee: Novartis AGInventors: Jacques Bouvier, Catherine Kolly
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Publication number: 20020151586Abstract: The invention is directed to acylphenylurea derivatives and their physiologically tolerated salts and physiologically functional derivatives.Type: ApplicationFiled: June 8, 2001Publication date: October 17, 2002Inventors: Elisabeth Defossa, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Heinz Baringhaus
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Patent number: 6458998Abstract: Compounds of formula I are useful for treating conditions associated with hyperglycemia, especially Type II diabetes. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.Type: GrantFiled: May 25, 2000Date of Patent: October 1, 2002Assignee: Telik, Inc.Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum
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Publication number: 20020137774Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: July 19, 2001Publication date: September 26, 2002Applicant: BAYER CORPORATIONInventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
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Publication number: 20020128321Abstract: This invention relates to novel compounds and a novel use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: May 31, 2001Publication date: September 12, 2002Applicant: SmithKline Beecham CorporationInventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge
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Publication number: 20020115722Abstract: Disclosed herein are &bgr;-tubulin inhibitors of formula I, prodrugs thereof and therapeutically acceptable salts thereof, 1Type: ApplicationFiled: December 22, 2000Publication date: August 22, 2002Inventors: Rene C. Gaudreault, Jean Legault
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Publication number: 20020107282Abstract: The invention relates to a composition containing at least one aminophenol derivative and at least one isoflavonoid. These combinations of active agents show synergism in the depigmentation and/or bleaching of the skin.Type: ApplicationFiled: November 13, 2001Publication date: August 8, 2002Applicant: L'OREALInventors: Veronique Chevalier, Dang-Man Pham
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Patent number: 6423854Abstract: Use of at least one aminophenol derivative of formula (I) below: in which: R represents a hydrogen atom or a radical —COR2, wherein R2 represents a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon or alkoxy radical; R1 is a radical of formula (a), (b) or (c) below: (a) —CO—NR3R4 (b) —CO—O—R5 (c) —SO2—R5 wherein R3 represents a hydrogen atom or a linear or branched, saturated or unsaturated, optionally hydroxylated, C1 to C6 hydrocarbon radical, R4 represents a hydrogen atom or a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon radical, and R5 represents a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon radical, in a depigmenting and/or bleaching cosmetic composition for human skin, body hairs or head hair; compositions comprising the derivatives of formula (I) and a process forType: GrantFiled: June 21, 1999Date of Patent: July 23, 2002Assignee: L'OrealInventors: Michel Philippe, Remy Tuloup, Christian Blaise
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Publication number: 20020082255Abstract: The invention is directed to physiologically active compounds of general formula (I): 1Type: ApplicationFiled: November 2, 2001Publication date: June 27, 2002Inventor: Paul Robert Eastwood
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Publication number: 20020061927Abstract: Methods of treating a person suffering from HIV protease inhibitor-induced metabolic disorders such as lipodystrophy, hypertriglyceridemia, insulin resistance, hyperglycemia, diabetes and ketoacidosis, comprise treatment with an insulin receptor activating compound, optionally in conjunction with insulin. In general, any insulin receptor activating compound is suitable for the practice of the invention; and preferred compounds are disclosed.Type: ApplicationFiled: October 11, 2001Publication date: May 23, 2002Inventors: Prasad V.V.S.V. Manchem, Robert T. Lum, Steven R. Schow
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Patent number: 6391917Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.Type: GrantFiled: April 19, 2001Date of Patent: May 21, 2002Assignee: ZymoGenetics, Inc.Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
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Publication number: 20020058709Abstract: Novel disulfide derivatives useful for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The disulfide derivatives act as mast cell stabilizers.Type: ApplicationFiled: April 25, 2001Publication date: May 16, 2002Applicant: Alcon Universal Ltd.Inventors: Zixia Feng, Mark R. Hellberg, Steven T. Miller
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Patent number: 6387906Abstract: The present invention concerns novel compounds of formula a N-oxide form, a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, wherein n is zero, 1, 2 or 3; X is N or CH; each R1 independently is halo, nitro, cyano, amino, hydroxy, C1-4alkyl, C1-4alkyloxy or trifluoromethyl; R2 is hydrogen; C3-7alkenyl; C3-7alkynyl, aryl; C3-7cycloalkyl; optionally substituted C1-6alkyl R3 and R4 each independently are hydrogen, C1-6alkyl, C3-7cycloalkyl or aryl; or R3 and R4 taken together form a bivalent radical —R3—R4— of formula: wherein R5a, R5b, R5c, R5d each independently are hydrogen, C1-6alkyl or aryl; and aryl is optionally substituted phenyl; as antifungals; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: January 7, 2000Date of Patent: May 14, 2002Inventors: Lieven Meerpoel, Jan Heeres, Frank Christopher Odds, Hugo Florent Adolf Vanden Bossche, Louis Jozef Elisabeth Van der Veken
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Publication number: 20020037928Abstract: The present invention provides pharmaceutical compositions and methods for the treatment of diabetes mellitus using combination therapy. The compositions relate to a compound of Formula I and an antidiabetic agent such as sulfonylureas, biguanides, glitazones, &agr;-glucosidase inhibitors, potassium channel antagonists, aldose reductase inhibitors, glucagon antagonists, activators of RXR, insulin therapy or other anti-obesity agent. The methods include the administration of the combination of compound of Formula I with antidiabetic agent where the two components are delivered in a simultaneous manner, where the compound of Formula I is administered first, followed by the antidiabetic agent, as well as wherein the antidiabetic agent is delivered first followed by the compound of Formula I.Type: ApplicationFiled: May 2, 2001Publication date: March 28, 2002Inventors: Juan C. Jaen, Jin-Long Chen
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Patent number: 6362229Abstract: The present invention relates generally to the fields of bacteriology and mycology. More particularly, the present invention provides novel inhibitors of multidrug transport proteins that may be used in combination with existing antibacterial agent and/or antifungal agents to increase the toxic effects of the antimicrobial agents. More specifically, the present invention provides methods and compositions for enhancing the antibacterial action of fluoroquinolones by administering fluoroquinolones in combination with an inhibitor of multidrug transporters and of enhancing the antifungal action of azole antifungal agents by administering an azole antifungal agent in combination with an inhibitor of multidrug transporters. Compositions comprising indole, urea, quinoline or aromatic amide based inhibitors also are disclosed.Type: GrantFiled: August 17, 2000Date of Patent: March 26, 2002Assignee: Influx, Inc.Inventors: Penelope N. Markham, Debbie C. Mulhearn, Alexander A. Neyfakh, David Crich, Mohamad-Rami Jaber, Michael E. Johnson
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Publication number: 20020035114Abstract: The invention relates to compounds of formula (I):Type: ApplicationFiled: August 8, 2001Publication date: March 21, 2002Inventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, Francois Lefoulon, Gerald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
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Patent number: 6355662Abstract: Compounds of Formula (1.0.0): are described wherein A is for example aryl, heteroaryl or heterocyclyl, Y is preferably —C(═O)—; B is independently selected from a group of moieties, the most preferred of which are those of partial Formulas (1.1.2) and (1.1.6): and E is a single bond; oxygen; 1,1-cyclopropyl; C(CH3)2; CF2; or a bridging moiety of partial Formula (1.9.0): where R1a is hydrogen when R1 has the meaning of a mono-valent substituent; and R1a is a single bond when R1 has the meaning of a di-valent substituent. Said compounds are useful in methods of treating or preventing an inflammatory, autoimmune or respiratory diseases by inhibiting cell adhesion and consequent or associated pathogenic processes subsequently mediated by VLA-4.Type: GrantFiled: October 26, 1999Date of Patent: March 12, 2002Assignee: Pfizer IncInventors: Allen Jacob Duplantier, Anthony John Milici, Louis Stanley Chupak
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Aminobenzoic acid derivatives having anti-tumorigenic activity, methods of making and using the same
Publication number: 20020022747Abstract: Haloacetoamido, benzoic acid derivatives having anti-tumorigenic activity. Examples of the haloacetoamido, benzoic acid derivatives include 3-chloroacetoamido, benzoylurea, 3-bromoacetoamido, benzoylurea, 3-iodoacetoamido, benzoylurea, ethyl-3-chloroacetoamido, benzoate, ethyl-3-bromoacetoamido, benzoate and ethyl-3-iodoacetoamido, benzoate. Intermediates for synthesizing the derivatives, along with method of making and using the derivatives, are also provided.Type: ApplicationFiled: August 29, 2001Publication date: February 21, 2002Inventors: George J. Bekesi, Jian-Dong Jiang, Imre Weisz, John Roboz, James F. Holland -
Publication number: 20020016350Abstract: This invention relates to a series of substitituted amino acids of Formula I 1Type: ApplicationFiled: August 10, 2001Publication date: February 7, 2002Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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Patent number: 6344476Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases other than cancer and proteolytic enzyme mediated diseases other than cancer, and pharmaceutical compositions for use in such therapy.Type: GrantFiled: May 22, 1998Date of Patent: February 5, 2002Assignee: Bayer CorporationInventors: Gerald Ranges, William Scott, Michael Bombara, Deborah Rauner, Aniko Redman, Roger Smith, Holger Paulsen, David Gunn, Jinshan Chen, Joel Renick
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Patent number: 6337350Abstract: Derivatives of aryl and heterocyclic ureido and aryl and heterocyclic carboxamido phenoxy isobutyric acids have been found to inhibit the nonenzymatic glycation of proteins which often results in formation of advanced glycation endproducts and crosslinks. Many other phenoxyisobutyric acid derivatives as well as certain other compounds as set out in this disclosure also have been found to inhibit the nonenzymatic glycation of proteins. The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences.Type: GrantFiled: April 5, 2000Date of Patent: January 8, 2002Assignee: City of HopeInventors: Samuel Rahbar, Iraj Lalezari
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Publication number: 20010046997Abstract: Chemical structures have been identified which allosterically modify pyrvate kinase and inhibit enzymatic activity. These compounds can be used as pharmaceuticals in the treatment of a wide variety of diseases and disorders where influencing metabolic processes is beneficial, such as the glycolytic pathway, all pathways which use ATP as an energy source, and all pathways which involve 2,3-diphosphoglycerate related to the delivery of oxygen by modifying hemoglobin's oxygen affinity, treatments of tumor and cancer and Alzheimer's disease (AD).Type: ApplicationFiled: March 7, 2001Publication date: November 29, 2001Inventors: Donald J. Abraham, Changging Wang, Richmond Danso-Danquah, James C. Burnett, Gajanan S. Joshi, Steven J. Hoffman
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Patent number: 6316503Abstract: The invention provides compounds, compositions and methods for modulating the effects of LXR in a cell. The compounds and compositions are useful both as diagnostic indicators of LXR function and as pharmacologically active agents. The compounds and compositions find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.Type: GrantFiled: March 14, 2000Date of Patent: November 13, 2001Assignee: Tularik Inc.Inventors: Leping Li, Julio C. Medina, Kevin Lustig, Bei Shan, Hirohiko Hasegawa, Serena T. Cutler, Jiwen Liu, Liusheng Zhu
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Publication number: 20010031763Abstract: This invention relates to substituted bis-acridines and related compounds which are ligands, in particular, antagonists of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, atherosclerosis, psoriasis, autoimmune disease such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted bis-acridines and related compounds which are CCR5 receptor antagonists. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor ligands may be useful in the treatment of HIV infection.Type: ApplicationFiled: April 11, 2001Publication date: October 18, 2001Applicant: SmithKline Beecham CorporationInventors: William E. Bondinell, Valerie A. Reader, Thomas Wen Fu Ku
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Publication number: 20010016605Abstract: N-4-Chlorobenzyl-N-cyclopentyl-N′-phenyl-urea of the formula 1Type: ApplicationFiled: January 10, 2001Publication date: August 23, 2001Inventors: Heinz-Wilhelm Dehne, Irene Zens, Astrid Mauler-Machnik
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Patent number: 6271261Abstract: Novel IL-8 receptor antagonists and methods of using them are provided.Type: GrantFiled: December 17, 1998Date of Patent: August 7, 2001Assignee: SmithKline Beecham CorporationInventor: Katherine L Widdowson
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Patent number: 6262113Abstract: The present invention relates to novel compounds and a novel use of phenyl ureas in the treatment of disease states mediated by the chemokine Interleukin-8 (IL-8).Type: GrantFiled: August 14, 1998Date of Patent: July 17, 2001Assignee: SmithKline Beecham CorporationInventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
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Patent number: 6255351Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.Type: GrantFiled: September 30, 1999Date of Patent: July 3, 2001Assignee: ZymoGenetics, Inc.Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
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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: 6221913Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.Type: GrantFiled: January 20, 1999Date of Patent: April 24, 2001Assignee: ZymoGenetics, Inc.Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
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Patent number: 6214880Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: September 21, 1999Date of Patent: April 10, 2001Assignee: Tularik Inc.Inventor: Jonathan B. Houze
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Patent number: 6214881Abstract: The present invention relates to the novel use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (I-8).Type: GrantFiled: February 9, 1999Date of Patent: April 10, 2001Assignee: SmithKline Beecham CorporationInventor: Jia-Ning Xiang