Plural Acyclic Nitrogens Bonded Directly To The Same Carbon Or Bonded Directly To Each Other Patents (Class 514/353)
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Publication number: 20030125354Abstract: Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q 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: October 15, 2002Publication date: July 3, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Ming-Hong Hao, Sanxing Sun
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Publication number: 20030125345Abstract: The present invention generally relates to nicotinic compounds, in the form of aryl substituted olefinic compounds, as well as pro-drug, N-oxide, metabolite and pharmaceutically acceptable salt forms thereof. Methods of modulating neurotransmitter release via administration of the compounds, pro-drugs, N-oxides and/or pharmaceutically acceptable salts are also disclosed.Type: ApplicationFiled: October 2, 2002Publication date: July 3, 2003Inventors: William S. Caldwell, Gary M. Dull, Balwinder S. Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared M. Wagner, Peter A. Crooks, Patrick M. Lippiello, Merouane Bencherif
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Publication number: 20030125331Abstract: Novel CycloHexenyl-Ethyl-Thiourea (CHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.Type: ApplicationFiled: October 22, 2002Publication date: July 3, 2003Applicant: Parker Hughes InstituteInventors: Fatih M. Uckun, Taracad K. Ventatachalam
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Publication number: 20030119882Abstract: The present invention relates to a solid pharmaceutical composition, comprisingType: ApplicationFiled: October 17, 2002Publication date: June 26, 2003Inventor: Markus Maegerlein
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Publication number: 20030119881Abstract: Compounds of the formula I: 1Type: ApplicationFiled: September 12, 2002Publication date: June 26, 2003Applicant: Medivir ABInventors: Christer Salhberg, Rolf Noreen, Marita Hogberg, Per Engelhardt
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Publication number: 20030109526Abstract: The present invention relates to azo amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: December 2, 2002Publication date: June 12, 2003Inventors: David Lauffer, Michael Mullican
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Patent number: 6576638Abstract: It is described the use of antagonists of neuro kynin receptors (NK-1; substance P receptors) in order to establish a new drug effective in the treatment of adenocarcinomas, such antagonists being one or more substances selected among those ones having the following features: pA2>6.0 both in human and in murine tissues, etherocyclic non peptidergic structures, antiangiogenic effects experimentally demonstrated onto the genito-urinary tract rumors induced via orthotopic drafts of human tumoral cells either in the genito-urinary apparatus of either immunodeficient rats or mice, decrease of the tumoral mass on tumors of the genito-urinary tract induced by orthotopic drafts of tumoral cells onto tissues of the genito-urinary tract of either immunodeficient rats or mice.Type: GrantFiled: May 13, 2002Date of Patent: June 10, 2003Assignee: Biopolis S.p.A.Inventors: Pierluigi Pompei, Maurizio Massi, Massimo Nabissi, Pier Luigi Sparapani
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Patent number: 6572848Abstract: Agonists of chlorine/potassium channel receptor, for example taurine, gamma-aminobutyric acid (GABA), isoguvacin, isonipecotic acid, 4,5,6,7-tetrahydroisoxazolo-(5,4-c)pyrid-3(2H)-one, a benzodiazepine, steroids, and cromakalim, pinacidil, nicorandil and minoxidil, are well suited for treating sensitive human skin and are especially useful for treating/eliminating skin itching, pruritus, tautness, tingling and/or erythema.Type: GrantFiled: April 28, 2000Date of Patent: June 3, 2003Assignee: Societe L'Oreal S.A.Inventors: Lionel Breton, Olivier De Lacharriere, Isabelle Nonotte
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Publication number: 20030100538Abstract: This invention pertains to substituted chalcones, specifically substituted 1-(4-methoxyphenyl)-3-(3,5-dimethoxyphenyl)prop-1-en-3-ones, which have therapeutic application, for example, as potent antiproliferative agents and antiinflammatory agents, and which have the formula (I) wherein: X is —H, —OH, —OC(═O)R3, —OS(═O)2OH, or —OP(═O)2(OH)2; Y is —H or a C1-4alkyl group; Z is —H or —OCH3; R1 is —H, a C1-4alkyl group, or C1-4fluoroalkyl group; R2 is —H, a C1-4alkyl group, or C1-4fluoroalkyl group; and, R3 is —H, a C1-6alkyl group, a C3-20 heterocyclyl group, or a C5-20aryl group; and pharmaceutically acceptable salts, esters, and protected forms thereof.Type: ApplicationFiled: September 26, 2002Publication date: May 29, 2003Inventors: Gerard Andrew Potter, Paul Crispin Butler, Elugba Wanogho
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Publication number: 20030092743Abstract: Compounds of the formula I: 1Type: ApplicationFiled: March 5, 2002Publication date: May 15, 2003Applicant: Medivir ABInventors: Christer Sahlberg, Dmitry Antonov, Hans Wallberg, Rolf Noreen
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Patent number: 6555561Abstract: This invention provides compounds of formula I having the structure Wherein substitutions at X, G, R1, R2, R3, R4, R5 are set forth in the specification.Type: GrantFiled: March 15, 2002Date of Patent: April 29, 2003Assignee: WyethInventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
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Patent number: 6552050Abstract: The present invention is directed to methods of using pro-NAD agents capable of enhancing the dermal and epidermal skin cell NAD content. These pro-NAD agents may be administered topically, orally, or parenterally to enhance DNA repair and other protective responses to DNA damage. The invention further relates to pharmaceutical compositions comprising pro-NAD agents that effectively elevate intracellular NAD content. Finally, the invention relates to the method of using the pro-NAD agents to treat disorders such as sunburn and other skin deterioration that results from DNA damage in skin cells.Type: GrantFiled: January 18, 2001Date of Patent: April 22, 2003Assignee: University of Kentucky Research FoundationInventors: Elaine L. Jacobson, Myron K. Jacobson
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Publication number: 20030045581Abstract: The present invention is directed to optionally substituted 4-substituted-1-(arylmethylidene)thiosemicarbazide, 4-substituted-1-(arylcarbonyl)thiosemicarbazide and analogs thereof, represented by the Formulae I and II: 1Type: ApplicationFiled: June 3, 2002Publication date: March 6, 2003Inventors: Sui Xiong Cai, Bao Ngoc Nguyen, John Drewe, P. Sanjeeva Reddy, Shailaja Kasibhatla, Azra Pervin
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Publication number: 20030045515Abstract: Pharmaceutical compositions comprising, as a first anti-neoplastic drug, cyanoguanidine IKK inhibitors, and in particular compounds of formula I 1Type: ApplicationFiled: May 21, 2002Publication date: March 6, 2003Inventors: Lise Binderup, Erik Bramm, Pernille-Julia Vig Hjarnaa, Karin Jexner Hamberg
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Patent number: 6525077Abstract: A compound of the formula is disclosed, the compound being suited for therapeutical uses. The invention also discloses compositions comprising said compound, methods of treatment involving administering said compound to a patient, and the use of said compound in the manufacture of medicaments.Type: GrantFiled: November 20, 2001Date of Patent: February 25, 2003Assignee: Leo Pharmaceutical Products Ltd. A/SInventors: Ernst Binderup, Pernille-Julia Vig Hjarnaa
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Patent number: 6511991Abstract: The present invention relates to nitric oxide-releasing amidine- and enamine-derived diazeniumdiolates, compositions comprising such compounds, methods of using such compounds and compositions, and to a method for the preparation of nitric oxide-releasing amidine and enamine derived diazeniumdiolates via the direct reaction of nitric oxide with amidines and enamines, and to a method of converting amines into such compounds.Type: GrantFiled: April 3, 2001Date of Patent: January 28, 2003Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Joseph A. Hrabie, Larry K. Keefer
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Patent number: 6503933Abstract: Compounds of formula (I) and salts thereof as phytopathogenic fungicides wherein A1 is substituted 2-pyridyl; A2 is optionally substituted phenyl; L is —(C═O)—, —SO2— or —(C═S)—; R1 is hydrogen, optionally substituted alkyl or acyl; and R2 is hydrogen or optionally substituted alkyl are useful phytopathogenic fungicides.Type: GrantFiled: September 21, 2000Date of Patent: January 7, 2003Assignee: Aventis CropScience UK LimitedInventors: Brian Anthony Moloney, David Hardy, Elizabeth Anne Saville-Stones
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Patent number: 6503948Abstract: A method for treating an organ donor prior to harvesting organ to reduce graft rejection in a recipient. An amount effective to reduce graft rejection of at least one compound selected from the group consisting of compounds having formulas I, II, III, IV, V, VI, and VII is administered to the organ donor: wherein Y is X is F or Cl; and the remaining groups are as defined in the specification.Type: GrantFiled: April 17, 2002Date of Patent: January 7, 2003Assignee: Southern Research InstituteInventors: Herbert M. Blatter, Donald R. Kahn, James R. Piper, John A. Secrist, III, Robert F. Struck, Carroll Temple
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Publication number: 20030004192Abstract: A method of modulating the level of activated, NF-&kgr;B in cells by contacting cells with a cyanoguanidine compound of general formula I 1Type: ApplicationFiled: May 24, 2002Publication date: January 2, 2003Inventors: Mogens Winkel Madsen, Lone Stengelshoj Olsen
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Publication number: 20020188011Abstract: The present invention relates to methods of treating viral or fungal infections using 3-aminopyridine-2-carboxyaldehyde thiosemicarbazone (3-AP) and 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP) and its prodrug forms and to pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: April 18, 2002Publication date: December 12, 2002Inventors: Ivan C. King, Terrance W. Doyle, Mario Sznol, Alan C. Sartorelli, Yung-Chi Cheng
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Patent number: 6492332Abstract: This invention relates to a method of inhibiting tumor cell adhesion, pain, and inflammation at a wound during a surgical procedure by delivering an irrigation solution containing a tumor cell anti-adhesion agent and a plurality of additional agents to an operative site during the surgical procedure. In addition, methods of inhibiting tumor cell attachment and implantation during a surgical procedure as well as inhibiting tumor metastasis during a surgical procedure are also provided.Type: GrantFiled: September 11, 2000Date of Patent: December 10, 2002Assignee: Omeros CorporationInventors: Gregory A. Demopulos, Pamela Pierce-Palmer, Jeffrey M. Herz, Darrell L. Tanelian
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Publication number: 20020177627Abstract: This patent discloses the use of poly-substituted isothiouronium salts (T1 where R1, R2, R3, R4=hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl, etc. and X−=Cl−, Br−, NO3−, CH3CO2−, or any other common anion), poly-substituted guanidinium salts (G1 where R1, R2, R3, R5, R6=hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl, etc. and X−=Cl−, Br, NO3−, CH3CO2−, or any other common anion), or mixtures of two or more of the above compounds, as the biocidal component of microbiocidal or anti-fouling formulations.Type: ApplicationFiled: June 28, 2002Publication date: November 28, 2002Applicant: RhoCraft Research Development, Ltd.Inventors: Thomas M. Fyles, Robert D. Rowe
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Publication number: 20020151568Abstract: The present invention is directed to derivatives of piperidinylethyl, phenoxyethyl, and fluorophenethyl bromopyridyl thioureas, which have been found to be effective non-nucleoside inhibitors (NNRTI) of NNI-resistant and multi-drug resistant human immunodeficiency virus (HIV)-1 reverse transcriptase (RT). The present invention is further directed to methods of using the above derivatives to treat patients with NNI-resistant or multi-drug resistant human immunodeficiency virus (HIV)-1.Type: ApplicationFiled: December 6, 2001Publication date: October 17, 2002Inventors: Fatih M. Uckun, Taracad K. Venkatachalam
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Publication number: 20020151545Abstract: Compounds of formula I and II, 1Type: ApplicationFiled: November 7, 2001Publication date: October 17, 2002Inventors: Gregory S. Bisacchi, James C. Sutton, Shung C. Wu
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Patent number: 6458816Abstract: The present invention relates to compounds according to the structure: Where R is H or CH3; R2 is phosphate which can be free acid or salt; R3 is H, F, Cl, Br, I, OCH3, OCF3 , CF3 or a C1-C3 alkyl group; R4 is H, F, Cl, Br, I, OCH3, OCF3 or CF3; and R5 and R6 are each independently H, F, Cl, Br, I, OCH3, OCF3 or CF3, with the proviso that when any two of R3, R4, R5 or R6 are other than H, the other two of R3, R4, R5 or R6 are H which may be used to treat neoplasia, including cancer.Type: GrantFiled: October 15, 2001Date of Patent: October 1, 2002Assignee: Vion Pharmaceuticals, Inc.Inventors: Terrence W. Doyle, Srinivasa Karra, Zujin Li, Xu Lin, John Mao, Qi Qiao, Yang Xu
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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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Patent number: 6451792Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.Type: GrantFiled: March 20, 2001Date of Patent: September 17, 2002Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
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Patent number: 6444691Abstract: The invention relates to 1,3-disubstituted ureas of general formula (I) where R1 is an aryl, R2 is nitro and/or amino, and X is oxygen and/or sulfur, and the method of preparing thereof which consists in treating aromatic amines with isocyanates. Isocyanates may be formed in situ and the reaction carried out in toluene, at 80° C. If the nitro group is formed, it is reduced with hydrogen in the presence of palladium catalyst to the amino group. The obtained 1,3-disubstituted ureas are inhibitors of the activity of the acyl co-enzyme A: cholesterol acyltransferase (ACAT) enzyme, and may be used to inhibit cholesterol esterification and absorption in hypercholesterolemia.Type: GrantFiled: July 10, 2000Date of Patent: September 3, 2002Assignee: Solvakofarma, a.s.Inventors: Vladi{acute over (m)}ir Oremus, VendelĂn {haeck over (S)}mahovskĂ˝, Viera Fáberová, Ivan KakalĂk, {haeck over (L)}udmila Schmidtová, Marián Zemánek
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Patent number: 6436944Abstract: This invention relates to the treatment of erectile dysfunction with a combination of (1) a compound selected from potassium channel openers, and (2) a compound selected from compounds which elevate cGMP levels. Sildenafil or a pharmaceutically acceptable salt thereof is preferred as the cGMP PDE elevator. Also included are compositions and kits comprising such impotence treating compounds.Type: GrantFiled: August 10, 2000Date of Patent: August 20, 2002Assignee: Pfizer Inc.Inventor: Murray C. Maytom
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Patent number: 6429317Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.Type: GrantFiled: September 5, 2000Date of Patent: August 6, 2002Assignee: Eli Lilly and CompanyInventors: Sean P. Hollinshead, Michael A. Staszak, John S. Ward, Joseph W. Wilson, Bret E. Huff, Philip F. Hughes, Jose S. Mendoza, Charles H. Mitch
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Patent number: 6403617Abstract: Compounds of the formula Useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, humanherpesviruses-6 and -7, and Kaposi herpesvirus.Type: GrantFiled: September 26, 2000Date of Patent: June 11, 2002Assignee: American Home Products Corp.Inventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
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Patent number: 6403619Abstract: The invention relates to the manipulation of enzymatic pathways, such as poly (ADP-ribose) polymerase pathways, which are dependent upon NAD as a substrate. By administering pro-NAD compounds, cell death caused by necrosis and/or apoptosis can be reduced. Further, by inhibiting one or more of these enzymes, the process of cell death can be accelerated, in conditions such as cancer, where acceleration of cellular necrosis and/or apoptosis is desired. Various inhibitors are described.Type: GrantFiled: April 14, 2000Date of Patent: June 11, 2002Assignee: University of Kentucky Research FoundationInventors: Elaine L. Jacobson, Myron K. Jacobson
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Patent number: 6395736Abstract: Compositions and methods for the treatment of anorectal disorders are provided in which certain combinations of NO donors, PDE inhibitors, superoxide (O2−) scavengers, &bgr;-adrenergic agonists, cAMP-dependent protein kinase activators, &agr;1-adrenergic antagonists, L-type Ca2+ channel blockers, estrogens, ATP-sensitive K+ channel activators and smooth muscle relaxants are used.Type: GrantFiled: December 13, 1999Date of Patent: May 28, 2002Assignee: Cellegy Pharmaceuticals, Inc.Inventors: Thomas P. Parks, Vivien Mak, Jung-Chung Lee, Charles Lee
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Publication number: 20020028837Abstract: Novel phenylethyl-thiourea (PHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.Type: ApplicationFiled: September 7, 2001Publication date: March 7, 2002Inventors: Fatih M. Uckun, Taracad K. Ventatachalam
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Publication number: 20020028836Abstract: Compounds of formula I: 1Type: ApplicationFiled: February 5, 2001Publication date: March 7, 2002Inventors: Robert J. Altenbach, Hao Bai, Jorge D. Brioni, William A. Carroll, Murali Gopalakrishnan, Robert J. Gregg, Mark W. Holladay, Peggy P. Huang, John F. Kincaid, Michael E. Kort, Philip R. Kym, John K. Lynch, Arturo Perez-Medrano, Henry Q. Zhang
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Patent number: 6337065Abstract: The present invention is directed to methods of using pro-NAD agents capable of enhancing the dermal and epidermal skin cell NAD content. These pro-NAD agents may be administered topically, orally, or parenterally to enhance DNA repair and other protective responses to DNA damage. The invention further relates to pharmaceutical compositions comprising pro-NAD agents that effectively elevate intracellular NAD content. Finally, the invention relates to the method of using the pro-NAD agents to treat disorders such as sunburn and other skin deterioration that results from DNA damage in skin cells.Type: GrantFiled: December 1, 1999Date of Patent: January 8, 2002Assignee: University of Kentucky Research FoundationInventors: Elaine L. Jacobson, Myron K. Jacobson
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Patent number: 6329349Abstract: Materials and methods for reducing or preventing ischemic damage of the heart are disclosed. A preferred embodiment of the invention comprises methods of sequential administration of a plurality of cardioprotective agents to patients suffering from ischernic damage or at risk for the same.Type: GrantFiled: April 24, 2000Date of Patent: December 11, 2001Assignees: Trustees of the University of Pennsylvania, The United States of America as represented by the Department of Health and Human ServicesInventors: Bruce T. Liang, Kenneth A. Jacobson
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Patent number: 6313148Abstract: Compounds antagonistic of the pain enhancing effects of prostaglandins are disclosed. The compounds comprise an optionally-substituted A ring with a —CH(R3)N(R2)B—R1 and —OD groups positioned in a 1,2 relationship to one another on ring carbon atoms. The 3-position ring-atom is not substituted. B is an optionally-substituted pyridyl ring and the group R1 is positioned on B in a 1,3 or 1,4 relationship with the —CH(R3)N(R2)B- linking group. R1, R2 and R3 and D can be a number of different organic or halogen moieties. N-oxides of —NR2 and S-oxides of sulphur containing rings are disclosed as are processes for the preparation of the compounds, intermediates in their preparation, pharmaceutical compositions containing them, and their use as therapeutic agents.Type: GrantFiled: April 3, 2000Date of Patent: November 6, 2001Assignee: Zeneca LimitedInventor: Gloria Anne Breault
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Publication number: 20010034342Abstract: The use of an N-substituted urea derivative for the manufacture of a medicament for the treatment of a condition where there is an advantage in inhibiting the NO synthase enzyme, in particular cerebral ischemia, and pharmaceutical formulations therefor are disclosed. Novel N-substituted urea derivatives and processes for the preparation thereof are also described.Type: ApplicationFiled: January 26, 2001Publication date: October 25, 2001Inventors: Jeffrey Alan Oplinger, Barry George Shearer, Eric Cleveland Bigham, Eric Steven Furfine, Edward Patrick Garvey
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Publication number: 20010033848Abstract: The present invention is directed to methods of using pro-NAD agents capable of enhancing the dermal and epidermal skin cell NAD content. These pro-NAD agents may be administered topically, orally, or parenterally to enhance DNA repair and other protective responses to DNA damage. The invention further relates to pharmaceutical compositions comprising pro-NAD agents that effectively elevate intracellular NAD content. Finally, the invention relates to the method of using the pro-NAD agents to treat disorders such as sunburn and other skin deterioration that results from DNA damage in skin cells.Type: ApplicationFiled: January 18, 2001Publication date: October 25, 2001Inventors: Elaine L. Jacobson, Myron K. Jacobson
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Patent number: 6300351Abstract: Novel compounds that are potent inhibitors of HIV reverse transcriptase (RT) are described in the invention. These novel compounds also inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The novel compounds of the invention include analogs and derivatives of phenethylthiazolylthiourea (PETT), of dihydroalkoxybenzyloxopyrimidine (DABO), and of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT). The invention additionally provides a composite HIV reverse-transcriptase (RT) nonnucleoside inhibitor (NNI) binding pocket constructed from a composite of multiple NNI-RT complexes The composite RT-NNI binding pocket provides a unique and useful tool for designing and identifying novel, potent inhibitors of reverse transcriptase.Type: GrantFiled: October 17, 2000Date of Patent: October 9, 2001Assignee: Parker Hughes InstituteInventors: Rakesh Vig, Chen Mao, Fatih A. Uckun
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Patent number: 6262090Abstract: Compounds of the formula wherein A is heteroaryl; R9-R12 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or R9 and R10 or R11 and R12 may be taken together to form aryl of 5 to 7 carbon atoms; W is O, NR6, or is absent; G is aryl or heteroaryl; and X is a bond X is a bond, —NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH)J; and J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6; or a pharmaceutical acceptable salt thereof, useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.Type: GrantFiled: November 22, 1999Date of Patent: July 17, 2001Assignee: American Home Products CorporationInventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
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Patent number: 6255323Abstract: A cyanoguanidine compound of the following formula: is disclosed. A cyanoguanidine compound of the present invention possess a high specificity for tumor cells. Also disclosed are methods for preparing a cyanoguanidine compound.Type: GrantFiled: April 7, 2000Date of Patent: July 3, 2001Assignee: Shionogi Bioresearch Corp.Inventors: Tai-Nang Huang, Guiqing Liang, Weimin Liu, Teresa Przewloka, Ming Shen, Shijie Zhang
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Patent number: 6251948Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.Type: GrantFiled: June 6, 1995Date of Patent: June 26, 2001Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of OregonInventors: Eckard Weber, John F. W. Keana
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Patent number: 6225305Abstract: The use of an N-substituted urea derivative for the manufacture of a medicament for the treatment of a condition where there is an advantage in inhibiting the NO synthase enzyme, in particular cerebral ischemia, and pharmaceutical formulations therefor are disclosed. Novel N-substituted urea derivatives and processes for the preparation thereof are also described.Type: GrantFiled: February 28, 2000Date of Patent: May 1, 2001Assignee: Glaxo Wellcome Inc.Inventors: Jeffrey Alan Oplinger, Barry George Shearer, Eric Cleveland Bigham, Eric Steven Furfine, Edward Patrick Garvey
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Patent number: 6225309Abstract: The invention concerns compounds of formula (I), wherein each of G1, G2 and G3 is CH or N; m is 1 or 2; R1 includes hydrogen, halogeno and 1-C)alkyl; M1 is a group of formula: NR2—L1—T1R3, in which R2 and R3 together form a (1-4C)alylene group, L1 includes (1-4C)alkylene, and T1 is CH or N; A may be a direct link; M2 is a group of the formula: (T2R4)rL2—T3R5 in which R is 0 or 1, each of T2 and T3 is CH or N, each of R4 and R5 is hydrogen or (1-4C)alkyl, or R4 and R5 together form a (1-4C)alkylene group, and L2 includes (1-4C)alkylene; M3 may be a direct link to X; X includes sulphonyl; and Q includes naphthyl and a heterocyclic moiety; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use as antithrombotic or anticoagulant agents.Type: GrantFiled: August 9, 1999Date of Patent: May 1, 2001Assignee: Zeneca LimitedInventors: Alan Wellington Faull, Andrew Stocker, Colette Marie Mayo, John Preston
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Patent number: 6218411Abstract: An agent for treating or ameliorating diabetic complications which contains at least one potassium channel activator as an active ingredient. The drug is expected to show a therapeutic or ameliorating action on diabetic complications such as retinopathy, neuropathy, nephropathy, peripheral circulation disorders, and skin ulcerations; it also proves effective in preventing, ameliorating, alleviating and gaining recovery from various symptoms and abnormalities caused by those diseases, as exemplified by blindness, proteinurea, pain, numbness, psychroesthesia, intermittent claudication and gangrene.Type: GrantFiled: February 8, 2000Date of Patent: April 17, 2001Assignee: Chugai Seiyaku Kabushiki KaishaInventor: Hiroshi Koga
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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
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Patent number: 6211242Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc. and represented by the general formula (I): wherein R1 is aryl optionally substituted with lower alkyl, etc., R2 is lower alkyl, etc., R3 is hydrogen, etc., R4 is aryl, etc., X is CH or N, and Y is CH or N, and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: January 30, 1998Date of Patent: April 3, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Keiji Hemmi, Hirokazu Tanaka
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Patent number: 6197797Abstract: The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine being in the 3- or 4-position, in which formula R1 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl nitro, amino, cyano, carboxy, or alkyl, alkoxy, or alkoxycarbonyl, the C-content of which can be from 1 to 4; X stands for a straight or branched C9-C20 carbon chain, saturated or unsaturated or Q—Ar—R; in which formula Ar stands for phenyl, Q stands for a C5-C20 divalent hydrocarbon radical which can be straight, branched, saturated or unsaturated and R stands for hydrogen or for one or more substituents which can be the same or different and are selected from the group consisting of: hydroxy, amino, halogen, trifluoromethyl, cyano, nitro, carboxy, carbamoyl, or alkyl, alkoxy, alkylthio, alkylamino, or alkoxycarbonyl, the C-content of which can be from 1 to 4; and pType: GrantFiled: November 26, 1999Date of Patent: March 6, 2001Assignee: Leo Pharmaceutical Products Ltd. A/S (Løvens kemiske Fabrik Produktionsaktieselskab)Inventors: Charlotte Schou, Erik Rytter Ottosen