Plural Acyclic Nitrogens Bonded Directly To The Same Carbon Or Bonded Directly To Each Other Patents (Class 514/353)
  • Publication number: 20030125354
    Abstract: 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: Application
    Filed: October 15, 2002
    Publication date: July 3, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Ming-Hong Hao, Sanxing Sun
  • Publication number: 20030125345
    Abstract: 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: Application
    Filed: October 2, 2002
    Publication date: July 3, 2003
    Inventors: 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
  • Publication number: 20030125331
    Abstract: 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: Application
    Filed: October 22, 2002
    Publication date: July 3, 2003
    Applicant: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Taracad K. Ventatachalam
  • Publication number: 20030119882
    Abstract: The present invention relates to a solid pharmaceutical composition, comprising
    Type: Application
    Filed: October 17, 2002
    Publication date: June 26, 2003
    Inventor: Markus Maegerlein
  • Publication number: 20030119881
    Abstract: Compounds of the formula I: 1
    Type: Application
    Filed: September 12, 2002
    Publication date: June 26, 2003
    Applicant: Medivir AB
    Inventors: Christer Salhberg, Rolf Noreen, Marita Hogberg, Per Engelhardt
  • Publication number: 20030109526
    Abstract: 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: Application
    Filed: December 2, 2002
    Publication date: June 12, 2003
    Inventors: David Lauffer, Michael Mullican
  • Patent number: 6576638
    Abstract: 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: Grant
    Filed: May 13, 2002
    Date of Patent: June 10, 2003
    Assignee: Biopolis S.p.A.
    Inventors: Pierluigi Pompei, Maurizio Massi, Massimo Nabissi, Pier Luigi Sparapani
  • Patent number: 6572848
    Abstract: 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: Grant
    Filed: April 28, 2000
    Date of Patent: June 3, 2003
    Assignee: Societe L'Oreal S.A.
    Inventors: Lionel Breton, Olivier De Lacharriere, Isabelle Nonotte
  • Publication number: 20030100538
    Abstract: 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: Application
    Filed: September 26, 2002
    Publication date: May 29, 2003
    Inventors: Gerard Andrew Potter, Paul Crispin Butler, Elugba Wanogho
  • Publication number: 20030092743
    Abstract: Compounds of the formula I: 1
    Type: Application
    Filed: March 5, 2002
    Publication date: May 15, 2003
    Applicant: Medivir AB
    Inventors: Christer Sahlberg, Dmitry Antonov, Hans Wallberg, Rolf Noreen
  • Patent number: 6555561
    Abstract: 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: Grant
    Filed: March 15, 2002
    Date of Patent: April 29, 2003
    Assignee: Wyeth
    Inventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
  • Patent number: 6552050
    Abstract: 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: Grant
    Filed: January 18, 2001
    Date of Patent: April 22, 2003
    Assignee: University of Kentucky Research Foundation
    Inventors: Elaine L. Jacobson, Myron K. Jacobson
  • Publication number: 20030045581
    Abstract: 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: 1
    Type: Application
    Filed: June 3, 2002
    Publication date: March 6, 2003
    Inventors: Sui Xiong Cai, Bao Ngoc Nguyen, John Drewe, P. Sanjeeva Reddy, Shailaja Kasibhatla, Azra Pervin
  • Publication number: 20030045515
    Abstract: Pharmaceutical compositions comprising, as a first anti-neoplastic drug, cyanoguanidine IKK inhibitors, and in particular compounds of formula I 1
    Type: Application
    Filed: May 21, 2002
    Publication date: March 6, 2003
    Inventors: Lise Binderup, Erik Bramm, Pernille-Julia Vig Hjarnaa, Karin Jexner Hamberg
  • Patent number: 6525077
    Abstract: 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: Grant
    Filed: November 20, 2001
    Date of Patent: February 25, 2003
    Assignee: Leo Pharmaceutical Products Ltd. A/S
    Inventors: Ernst Binderup, Pernille-Julia Vig Hjarnaa
  • Patent number: 6511991
    Abstract: 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: Grant
    Filed: April 3, 2001
    Date of Patent: January 28, 2003
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Joseph A. Hrabie, Larry K. Keefer
  • Patent number: 6503933
    Abstract: 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: Grant
    Filed: September 21, 2000
    Date of Patent: January 7, 2003
    Assignee: Aventis CropScience UK Limited
    Inventors: Brian Anthony Moloney, David Hardy, Elizabeth Anne Saville-Stones
  • Patent number: 6503948
    Abstract: 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: Grant
    Filed: April 17, 2002
    Date of Patent: January 7, 2003
    Assignee: Southern Research Institute
    Inventors: Herbert M. Blatter, Donald R. Kahn, James R. Piper, John A. Secrist, III, Robert F. Struck, Carroll Temple
  • Publication number: 20030004192
    Abstract: A method of modulating the level of activated, NF-&kgr;B in cells by contacting cells with a cyanoguanidine compound of general formula I 1
    Type: Application
    Filed: May 24, 2002
    Publication date: January 2, 2003
    Inventors: Mogens Winkel Madsen, Lone Stengelshoj Olsen
  • Publication number: 20020188011
    Abstract: 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: Application
    Filed: April 18, 2002
    Publication date: December 12, 2002
    Inventors: Ivan C. King, Terrance W. Doyle, Mario Sznol, Alan C. Sartorelli, Yung-Chi Cheng
  • Patent number: 6492332
    Abstract: 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: Grant
    Filed: September 11, 2000
    Date of Patent: December 10, 2002
    Assignee: Omeros Corporation
    Inventors: Gregory A. Demopulos, Pamela Pierce-Palmer, Jeffrey M. Herz, Darrell L. Tanelian
  • Publication number: 20020177627
    Abstract: 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: Application
    Filed: June 28, 2002
    Publication date: November 28, 2002
    Applicant: RhoCraft Research Development, Ltd.
    Inventors: Thomas M. Fyles, Robert D. Rowe
  • Publication number: 20020151568
    Abstract: 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: Application
    Filed: December 6, 2001
    Publication date: October 17, 2002
    Inventors: Fatih M. Uckun, Taracad K. Venkatachalam
  • Publication number: 20020151545
    Abstract: Compounds of formula I and II, 1
    Type: Application
    Filed: November 7, 2001
    Publication date: October 17, 2002
    Inventors: Gregory S. Bisacchi, James C. Sutton, Shung C. Wu
  • Patent number: 6458816
    Abstract: 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: Grant
    Filed: October 15, 2001
    Date of Patent: October 1, 2002
    Assignee: Vion Pharmaceuticals, Inc.
    Inventors: Terrence W. Doyle, Srinivasa Karra, Zujin Li, Xu Lin, John Mao, Qi Qiao, Yang Xu
  • Publication number: 20020137774
    Abstract: 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: Application
    Filed: July 19, 2001
    Publication date: September 26, 2002
    Applicant: BAYER CORPORATION
    Inventors: 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
  • Patent number: 6451792
    Abstract: 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: Grant
    Filed: March 20, 2001
    Date of Patent: September 17, 2002
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
  • Patent number: 6444691
    Abstract: 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: Grant
    Filed: July 10, 2000
    Date of Patent: September 3, 2002
    Assignee: Solvakofarma, a.s.
    Inventors: Vladi{acute over (m)}ir Oremus, Vendelín {haeck over (S)}mahovský, Viera Fáberová, Ivan Kakalík, {haeck over (L)}udmila Schmidtová, Marián Zemánek
  • Patent number: 6436944
    Abstract: 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: Grant
    Filed: August 10, 2000
    Date of Patent: August 20, 2002
    Assignee: Pfizer Inc.
    Inventor: Murray C. Maytom
  • Patent number: 6429317
    Abstract: 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: Grant
    Filed: September 5, 2000
    Date of Patent: August 6, 2002
    Assignee: Eli Lilly and Company
    Inventors: Sean P. Hollinshead, Michael A. Staszak, John S. Ward, Joseph W. Wilson, Bret E. Huff, Philip F. Hughes, Jose S. Mendoza, Charles H. Mitch
  • Patent number: 6403617
    Abstract: 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: Grant
    Filed: September 26, 2000
    Date of Patent: June 11, 2002
    Assignee: American Home Products Corp.
    Inventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
  • Patent number: 6403619
    Abstract: 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: Grant
    Filed: April 14, 2000
    Date of Patent: June 11, 2002
    Assignee: University of Kentucky Research Foundation
    Inventors: Elaine L. Jacobson, Myron K. Jacobson
  • Patent number: 6395736
    Abstract: 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: Grant
    Filed: December 13, 1999
    Date of Patent: May 28, 2002
    Assignee: Cellegy Pharmaceuticals, Inc.
    Inventors: Thomas P. Parks, Vivien Mak, Jung-Chung Lee, Charles Lee
  • Publication number: 20020028837
    Abstract: 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: Application
    Filed: September 7, 2001
    Publication date: March 7, 2002
    Inventors: Fatih M. Uckun, Taracad K. Ventatachalam
  • Publication number: 20020028836
    Abstract: Compounds of formula I: 1
    Type: Application
    Filed: February 5, 2001
    Publication date: March 7, 2002
    Inventors: 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
  • Patent number: 6337065
    Abstract: 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: Grant
    Filed: December 1, 1999
    Date of Patent: January 8, 2002
    Assignee: University of Kentucky Research Foundation
    Inventors: Elaine L. Jacobson, Myron K. Jacobson
  • Patent number: 6329349
    Abstract: 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: Grant
    Filed: April 24, 2000
    Date of Patent: December 11, 2001
    Assignees: Trustees of the University of Pennsylvania, The United States of America as represented by the Department of Health and Human Services
    Inventors: Bruce T. Liang, Kenneth A. Jacobson
  • Patent number: 6313148
    Abstract: 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: Grant
    Filed: April 3, 2000
    Date of Patent: November 6, 2001
    Assignee: Zeneca Limited
    Inventor: Gloria Anne Breault
  • Publication number: 20010034342
    Abstract: 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: Application
    Filed: January 26, 2001
    Publication date: October 25, 2001
    Inventors: Jeffrey Alan Oplinger, Barry George Shearer, Eric Cleveland Bigham, Eric Steven Furfine, Edward Patrick Garvey
  • Publication number: 20010033848
    Abstract: 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: Application
    Filed: January 18, 2001
    Publication date: October 25, 2001
    Inventors: Elaine L. Jacobson, Myron K. Jacobson
  • Patent number: 6300351
    Abstract: 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: Grant
    Filed: October 17, 2000
    Date of Patent: October 9, 2001
    Assignee: Parker Hughes Institute
    Inventors: Rakesh Vig, Chen Mao, Fatih A. Uckun
  • Patent number: 6262090
    Abstract: 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: Grant
    Filed: November 22, 1999
    Date of Patent: July 17, 2001
    Assignee: American Home Products Corporation
    Inventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
  • Patent number: 6255323
    Abstract: 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: Grant
    Filed: April 7, 2000
    Date of Patent: July 3, 2001
    Assignee: Shionogi Bioresearch Corp.
    Inventors: Tai-Nang Huang, Guiqing Liang, Weimin Liu, Teresa Przewloka, Ming Shen, Shijie Zhang
  • Patent number: 6251948
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: June 26, 2001
    Assignee: 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 Oregon
    Inventors: Eckard Weber, John F. W. Keana
  • Patent number: 6225305
    Abstract: 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: Grant
    Filed: February 28, 2000
    Date of Patent: May 1, 2001
    Assignee: Glaxo Wellcome Inc.
    Inventors: Jeffrey Alan Oplinger, Barry George Shearer, Eric Cleveland Bigham, Eric Steven Furfine, Edward Patrick Garvey
  • Patent number: 6225309
    Abstract: 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: Grant
    Filed: August 9, 1999
    Date of Patent: May 1, 2001
    Assignee: Zeneca Limited
    Inventors: Alan Wellington Faull, Andrew Stocker, Colette Marie Mayo, John Preston
  • Patent number: 6218411
    Abstract: 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: Grant
    Filed: February 8, 2000
    Date of Patent: April 17, 2001
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventor: Hiroshi Koga
  • Patent number: 6214881
    Abstract: 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: Grant
    Filed: February 9, 1999
    Date of Patent: April 10, 2001
    Assignee: SmithKline Beecham Corporation
    Inventor: Jia-Ning Xiang
  • Patent number: 6211242
    Abstract: 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: Grant
    Filed: January 30, 1998
    Date of Patent: April 3, 2001
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Keiji Hemmi, Hirokazu Tanaka
  • Patent number: 6197797
    Abstract: 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 p
    Type: Grant
    Filed: November 26, 1999
    Date of Patent: March 6, 2001
    Assignee: Leo Pharmaceutical Products Ltd. A/S (Løvens kemiske Fabrik Produktionsaktieselskab)
    Inventors: Charlotte Schou, Erik Rytter Ottosen