Benzene Ring Containing Patents (Class 514/595)
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 6984647Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to ?-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.Type: GrantFiled: May 15, 2003Date of Patent: January 10, 2006Assignee: Janssen Pharmaceutica N.V.Inventors: Scott L. Dax, Michele Jetter, Mark McDonnell, James J. McNally, Mark Youngman
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Patent number: 6982285Abstract: 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: January 22, 2003Date of Patent: January 3, 2006Assignee: Novartis Animal Health US, Inc.Inventor: Hariolf Schmid
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Patent number: 6962945Abstract: The present invention provides N-aryloxypropanolyl-N?-phenethyl-urea derivatives of formula 3, method for their preparation and use thereof as potent appetite suppressants for treatment of obesity wherein R is selected from the group consisting of H, 2, 3 or 4-trifluoromethyl, 2, 3, or 4-chloro, 2, 3, or 4-bromo, 4-acetyl, 4-propionyl, 4-acetamido, 2,3 or 4 methoxy, 4 nitrile, 2,3 or 4-methyl, and 4 formyl and X is S or O.Type: GrantFiled: March 26, 2004Date of Patent: November 8, 2005Assignee: Council of Scientific and Industrial ResearchInventors: Kalpana Bhandari, Shipra Srivastava, Chandeshwar Nath
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Patent number: 6960588Abstract: Compounds of formula (I) in which M, B1, B2, B3, B4, B5, B6, A1, A2, A3, A4, A5, A6, K1 and K2 have the meanings as indicated in the description, are novel effective tryptase inhibitors.Type: GrantFiled: September 12, 2000Date of Patent: November 1, 2005Assignee: Altana Pharma AGInventor: Thomas Martin
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Patent number: 6900213Abstract: The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyl and A is a group of formula II, III, IV or V: An example is (3S,6S)-1-N-(7-phenylheptyl)-3-(4-(3,4,5-trimethoxyphenyl)benzyl)-4-N-methyl-6-methyl-2,5-dioxo-1,4-piperazine: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.Type: GrantFiled: July 21, 2003Date of Patent: May 31, 2005Assignee: Pharmacopeia Drug Discovery, Inc.Inventors: Tao Guo, Koc-Kan Ho, Edward McDonald, Roland Ellwood Dolle, Kurt W. Saionz, Steven G. Kultgen, Ruiyan Liu, Guizhen Dong, Peng Geng, Anton Egbert Peter Adang, Nicole Corine Renee Van Straten
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Patent number: 6872851Abstract: The invention concerns compounds of formula (I): R—A—R? wherein: A is as defined in the description; R represent, a group (V), wherein R?a and R?a are as defined in the description, or R forms with A a cyclic structure as defined in the description; R? represents a (CH2)t—R2 group wherein q, t, and R2 are as defined in the description. The invention is useful for preparing medicines.Type: GrantFiled: May 10, 1999Date of Patent: March 29, 2005Assignee: Les Laboratories ServierInventors: Daniel Lesieur, Frédérique Klupsch, Gérald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renard, Philippe Delagrange
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Patent number: 6852760Abstract: Compositions and methods of using the same for the treatment of diabetes and other disorders of glucose metabolism are provided. Compositions may include an anti-diabetic agent and one or more of a bioavailable source of chromium and vanadium.Type: GrantFiled: September 17, 1999Date of Patent: February 8, 2005Assignee: Akesis Pharmaceuticals, Inc.Inventors: Stuart A. Fine, Kevin J. Kinsella
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Patent number: 6852738Abstract: A class of acyl sulfamides comprises compounds that are potent ligands for PPAR gamma and generally have antagonist or partial agonist activity. The compounds may be useful in the treatment, control or prevention of obesity, non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, inflammation, and other PPAR gamma mediated diseases, disorders and conditions.Type: GrantFiled: January 25, 2002Date of Patent: February 8, 2005Assignee: Merck & Co., Inc.Inventors: A. Brian Jones, John J. Acton, III
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Patent number: 6822001Abstract: Combination therapies are provided for the treatment of proliferative disorders which use a pentafluorobenzenesulfonamide of formula I and an antineoplastic agent such as gemcitabine or paclitaxel.Type: GrantFiled: November 2, 2001Date of Patent: November 23, 2004Assignee: Tularik Inc.Inventors: Susan Schwendner, Pieter Timmermans, Jacqueline Walling
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Publication number: 20040209948Abstract: Disclosed are CCR8 inhibitors represented by Structural Formulas (I): 1Type: ApplicationFiled: December 23, 2003Publication date: October 21, 2004Applicant: Millennium Pharmaceuticals, Inc.Inventors: Bing Guan, Charles Minor, Mingshi Dai, Shomir Ghosh, Tracy J. Jenkins, Gang Li, Douglas F. Burdi, Robert A. Bennett
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Patent number: 6797731Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.Type: GrantFiled: March 12, 2003Date of Patent: September 28, 2004Assignee: Pfizer Inc.Inventors: 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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Publication number: 20040176443Abstract: Disclosed are diaryl piperazines and related compounds. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.Type: ApplicationFiled: March 12, 2004Publication date: September 9, 2004Applicant: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Alan Hutchison, Robert W. DeSimone, Kevin J. Hodgetts, James E. Krause, Geoffrey G. White
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Patent number: 6777572Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of renal failure.Type: GrantFiled: November 28, 2001Date of Patent: August 17, 2004Assignee: Pharmacia Corporation (of Pfizer Inc.)Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 6777561Abstract: Compounds of general formula I are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: June 1, 2000Date of Patent: August 17, 2004Assignee: AstraZeneca Canada Inc.Inventors: Daniel Delorme, Vlad Gregor, Edward Roberts, Eric Sun
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Publication number: 20040142982Abstract: Novel antagonists of ∝4&bgr;1 integrin and/or ∝4&bgr;7 integrin of the general Formula I: wherein R1, R2, R5, L1, L2, Rb, W and Z are as defined in any one of claims 1 to 13, A represents —CH— or a nitrogen atom, and p is from 0 to 4.Type: ApplicationFiled: February 23, 2004Publication date: July 22, 2004Inventors: Juan Miguel Jimenez Mayorga, Jordi Bach Tana, Jesus Maria Ontoria Ontoria, Eloisa Navarro Romero
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Publication number: 20040132786Abstract: The invention is directed to novel biaryl derivatives, to the uses of these compounds in various medicinal applications, including the treatment, prevention and control of proliferative diseases such as tumors, and to pharmaceutical compositions comprising these compounds. Compounds of the invention can be used to treat or prevent diseases or disorders that involve the activity of MIF-1 and/or adenosine kinase.Type: ApplicationFiled: December 18, 2003Publication date: July 8, 2004Applicant: IRM LLC, a Delaware Limited Liability CompanyInventors: Jason Chyba, Quinn Deveraux, Garret Hampton, Fred King
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Publication number: 20040097593Abstract: Novel acyl urea, thiourea, carbamate, thiocarbamate and related compounds are provided which are effective in inhibiting the cytokine-mediated inflammatory response in cultured cells, in ameliorating bone destruction in an animal model of arthritis and in lowering blood glucose levels in animal models of Type II diabetes mellitus. The compounds are disclosed as useful for a variety of treatments including the treatment of diabetes mellitus, insulin resistance, inflammation, inflammatory diseases, immunological diseases and cancer.Type: ApplicationFiled: May 7, 2003Publication date: May 20, 2004Inventors: Partha Neogi, Debedranath Dey, Joseph C. Fuller, Liang Chen, Ta-Kai Li
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Publication number: 20040082550Abstract: Tropolone derivatives represented by the formula (I), which have retinoid actions and are useful as active ingredients of medicaments [R1 to R4 represent hydrogen atom, an alkyl group, or an alkoxyl group; the ring represented by Ar represents an aryl ring or a heteroaryl ring; X represents a single bond, —N═N—, —CON(R5)—, —(C═C)nCON(R6)—, —N(R7)CON(R8)—, —SO2N(R9)—, —N(R10)— (R5 to R9 represent hydrogen atom or an alkyl group, n represents 1 to 3, R10 represents hydrogen atom, an alkyl group, or an acyl group), an alkylene group, an aryldiyl group, or a heterocyclic diyl group; Y represents hydrogen atom, —OR11 (R11 represents hydrogen atom, an alkyl group, or an acyl group), —NHR12 (R12 represents hydrogen atom, an alkyl group, an acyl group, or amino group), or a halogen atom.Type: ApplicationFiled: December 16, 2003Publication date: April 29, 2004Inventor: Hiroyuki Kagechika
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Publication number: 20040082626Abstract: Pharmaceutical compositions containing as an active ingredient compounds of the general formula (I), prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism:Type: ApplicationFiled: July 25, 2003Publication date: April 29, 2004Inventors: Hiroshi Takemoto, Masami Takayama, Yutaka Yoshida
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Publication number: 20040067927Abstract: The invention relates to novel compounds which are substituted alkyldiamino derivatives of formula (I). The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of formula (I) and especially their use as inhibitors of the plasmodium falciparum protease plasmepsin II or related aspartic proteases.Type: ApplicationFiled: November 7, 2003Publication date: April 8, 2004Inventors: Christoph Boss, Walter Fischli, Solange Meyer, Sylvia Richard-Bildstein, Thomas Weller
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Publication number: 20040044049Abstract: Compounds, compositions and methods for altering insulin secretion, particularly in the context of treatment of subjects having, or suspected of being at risk for having, diabetes mellitus.Type: ApplicationFiled: February 10, 2003Publication date: March 4, 2004Applicant: MitoKorInventors: Yazhong Pei, Soumitra S. Ghosh, Ian William James
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Publication number: 20040039040Abstract: Disclosed are novel urea derivatives and their medical uses, especially as adhesion molecule inhibitors useful for therapies of inflammatory diseases.Type: ApplicationFiled: March 14, 2003Publication date: February 26, 2004Inventors: Toshiya Takahashi, Takeshi Ishigaki, Miyuki Funahashi, Koji Taniguchi, Masayuki Kaneko, Mie Kainoh, Hiroyuki Meguro
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Patent number: 6696488Abstract: Novel (hydroxyethyl)ureas are described. These compounds are effective inhibitors of certain aspartyl proteases, notably secretases involved in the enzymatic cleavage of amyloid precursor protein (APP) to yield amyloid-&bgr; peptide. Methods are provided for administering the novel compounds to treat &bgr;-amyloid-associated diseases, notably Alzheimer's disease.Type: GrantFiled: August 10, 2001Date of Patent: February 24, 2004Assignee: The Brigham and Women's Hospital, Inc.Inventors: Michael S. Wolfe, Dennis J. Selkoe
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Publication number: 20040029903Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, a trihalomethylcarbonyl group, such as a trifluoromethylcarbonyl group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.Type: ApplicationFiled: May 21, 2003Publication date: February 12, 2004Applicant: Beacon Laboratories, Inc.Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman
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Publication number: 20040009227Abstract: This invention relates to novel porous materials that possess antiviral and/or antimicrobial properties. The invention encompasses a porous material having antiviral or antimicrobial properties-which is comprised of a porous substrate and an antiviral or antimicrobial agent. The invention also encompasses a process for making porous materials that possess antiviral and/or antimicrobial properties and the products of the process.Type: ApplicationFiled: April 8, 2003Publication date: January 15, 2004Applicant: Porex CorporationInventor: Li Yao
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Patent number: 6667414Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: November 28, 2001Date of Patent: December 23, 2003Assignee: Pharmacia CorporationInventors: Gunnar J. Hanson, John S. Baran
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Publication number: 20030207872Abstract: 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: January 11, 2002Publication date: November 6, 2003Applicant: 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: 20030203944Abstract: The present invention relates to an antagonist against vanilloid receptor and the pharmaceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fevescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.Type: ApplicationFiled: February 3, 2003Publication date: October 30, 2003Inventors: Young Ger Suh, Uh Taek Oh, Hee Doo Kim, Jee Woo Lee, Hyeung Geun Park, Young Ho Park, Jung Bum Yi
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Publication number: 20030199574Abstract: Methods for treating disorders of the eye and/or disorders of a nerve in a human or veterinary patient by delivering to the patient a therapeutically effective amount of a compound selected from the group of; urea, urea derivatives, thiourea, thiourea derivatives, guanidine, guanidine derivatives and compounds having General Formula I as set forth herein. For ophthalmic applications, the compound may be delivered by intravitreal injection such that the compound causes vitreal liquefaction, posterior vitreoretinal detachment and other affects.Type: ApplicationFiled: February 13, 2003Publication date: October 23, 2003Applicant: Vitreo-Retinal Technologies, Inc.Inventors: Vicken H. Karageozian, David Castillejos, John Park
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Patent number: 6635650Abstract: The invention relates to compounds of formula (I): A-G1-Cy-G2-Cy-G3-B (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: August 8, 2001Date of Patent: October 21, 2003Assignee: Les Laboratoires ServierInventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, François Lefoulon, Gérald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
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Publication number: 20030195202Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: ApplicationFiled: January 24, 2003Publication date: October 16, 2003Applicant: Vertex Pharmaceuticals IncorporatedInventors: David M. Armistead, Michael C. Badia, Guy W. Bemis, Randy S. Bethiel, Catharine A. Frank, Perry M. Novak, Steven M. Ronkin, Jeffrey O. Saunders
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Patent number: 6627774Abstract: Derivatives of N-deacetyl-thiocolchicine or of the isoster thereof of formula (I) wherein n is an integer from 0 to 8, Y is a CH2 group or, when n is 1, can also be a group of formula NH. Compounds of formula (I) have anti-proliferative activity.Type: GrantFiled: August 2, 2002Date of Patent: September 30, 2003Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Alessandro Pontiroli
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Publication number: 20030153596Abstract: The present invention relates to novel thiourca derivatives as a modulator for vanilloid receptor (VR) and the phar- maceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflam- matory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.Type: ApplicationFiled: July 9, 2002Publication date: August 14, 2003Inventors: Young Ger Suh, Uh Taek Oh, Hee Doo Kim, Jee Woo Lee, Hyeung Geun Park, Ok Hui Park, Yong Sil Lee, Young Ho Park, Yung Hyup Joo, Jin Kyu Choi, Kyung Min Lim, Sun Young Kim, Jin Kwan Kim, Hyun Ju Koh, Joo Hyun Moh, Yeon Su Jeong, Jung Bum Yi, Young Im Oh
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Patent number: 6602903Abstract: The invention relates to compounds of formula (I): and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: August 28, 2001Date of Patent: August 5, 2003Assignee: Les Laboratories ServierInventors: Gérald Guillaumet, Marie-Claude Viaud, Ahmed Mamai, Isabelle Charton, Pierre Renard, Caroline Bennejean, Béatrice Guardiola, Philippe Daubos
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Patent number: 6573284Abstract: Novel pro-drugs and assay reagents are provided which are useful as therapeutic agents especially for delivery and targetting therapeutically active agents to melanoma cells. The pro-drugs and assay reagents are substrates for tyrosinase and may be represented by the formula TyrX—B—ThrAg*. The compounds of formula TyrX—B—ThrAg* are capable of releasing a therapeutically active agent or assayable substance (ThrAg) at a desired location. TyrX— being a residue of an optionally substituted tyrosine analogue.Type: GrantFiled: June 14, 1999Date of Patent: June 3, 2003Inventors: Patrick Anthony Riley, Andrew Photiou, Tariq Hussain Khan, Helen Mary Osborn
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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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Publication number: 20030083333Abstract: Disclosed are novel 1,4-disubstituted benzo-fused compounds wherein G, X, L, Q, n and Y are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: ApplicationFiled: April 10, 2002Publication date: May 1, 2003Inventors: Pier Francesco Cirillo, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, Kristen Mueller, John Robinson Regan
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Publication number: 20030073720Abstract: Compounds of formula (I), in which M, A1, A2, K1 and K2 have the meanings as indicated in the description are novel active tryptase inhibitors.Type: ApplicationFiled: September 9, 2002Publication date: April 17, 2003Inventor: Thomas Martin
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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: 20030055111Abstract: Derivatives of N-deacetyl-thiocolchicine or of the isoster thereof of formula (I) 1Type: ApplicationFiled: August 2, 2002Publication date: March 20, 2003Inventors: Ezio Bombardelli, Alessandro Pontiroli
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Patent number: 6534501Abstract: 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: GrantFiled: March 7, 2001Date of Patent: March 18, 2003Assignees: Allos Therapeutics, Inc., Virginia Commonwealth UniversityInventors: Donald J. Abraham, Changging Wang, Richmond Danso-Danquah, James C. Burnett, Gajanan S. Joshi, Stephen J. Hoffman
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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: 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: 6528543Abstract: Glucokinase activating compounds of the formula wherein R1 and R2 are independently hydrogen, halo, amino, nitro, cyano, sulfonamido, lower alkyl, perfluoro-lower alkyl, lower alkyl thio, perfluoro-lower alkyl thio, lower alkyl sulfonyl, or perfluoro-lower alkyl sulfonyl; R3 is cycloalkyl having from 3 to 7 carbon atoms or lower alkyl having from 2 to 4 carbon atoms; R4 is hydrogen, lower alkyl, lower alkenyl, hydroxy lower alkyl, halo lower alkyl, R5 and R6 are hydrogen or lower alkyl; and n is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereofType: GrantFiled: March 21, 2000Date of Patent: March 4, 2003Assignee: Hoffman-La Roche Inc.Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Antonio Focella, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Publication number: 20030036532Abstract: The invention relates to the use of compounds of formula (I), wherein n=0-3; R1, R2=H, alkyl, aryl, heteroaryl, acyl; R3=H, halogen, alkyl, aryl, heteroaryl, arylalkyl, acyl, CN, NO2, R4—X—; R4=H, alkyl, aryl, heteroaryl, aralkyl, acyl; X=NH, O, S, SO2, NHSO2, OSO2, and A, B, C=organic groups. The inventive compounds are used for the prophylaxis and the therapeutic treatment of infectious processes, especially of infectious processes caused by parasites. The invention further relates to medicaments that contain the inventive compounds.Type: ApplicationFiled: August 23, 2002Publication date: February 20, 2003Inventors: Hassan Jomaa, Martin Schlitzer, Jochen Wiesner
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Patent number: 6514963Abstract: The present invention comprises methods and compositions for use in inhibiting egg production by parasitic trematode worms comprising administering to an individual in need thereof an effective amount of an agent which transiently inhibits the influx of calcium through a cell membrane calcium channel. Inhibition of egg production in the worms ameliorates many of the symptoms and pathology related to infection by trematode related diseases, including Schistosomiasis. The methods can also effect disease transmission by reducing the number of eggs released into the environment available to continue the worm life cycle.Type: GrantFiled: July 18, 2001Date of Patent: February 4, 2003Assignee: The Regents of the University of CaliforniaInventors: Mark Walter, Armand Kuris
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Publication number: 20030008881Abstract: The present invention relates to substituted phenylcyclohexanecarboxamides of the formula (I) 1Type: ApplicationFiled: August 30, 2001Publication date: January 9, 2003Inventors: Erwin Bischoff, Thomas Krahn, Stephan-Nicholas Muller, Holger Paulsen, Joachim Schuhmacher, Henning Steinhagen, Wolfgang Thielemann
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Publication number: 20030008884Abstract: The invention relates to compounds of formula (I), and also to salts thereof, which have fungicidal activities: 1Type: ApplicationFiled: August 6, 2001Publication date: January 9, 2003Applicant: Aventis CropScience S.A.Inventors: Vincent Gerusz, Darren James Mansfield, Jose Perez, David Tickle, Jean-Pierre Vors, Derek Baldwin, Thomas Lawley Hough, Dale Robert Mitchell
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Publication number: 20030004212Abstract: Described are cyclohexylamine derivatives of Formula I 1Type: ApplicationFiled: March 27, 2002Publication date: January 2, 2003Inventors: Russell Joseph DeOrazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer