Patents Examined by Floyd D. Higel
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Patent number: 6448260Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: July 10, 2001Date of Patent: September 10, 2002Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 6444829Abstract: The present invention relates to a pyrrolidine compound and pharmaceutically acceptable esters and/or salts thereof. The compounds are useful as inhibitors of metalloproteases, e.g. zinc proteases, particularly zinc hydrolases, and which are effective in treating disease states are associated with vasoconstriction of increasing occurrences.Type: GrantFiled: July 6, 2001Date of Patent: September 3, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Henrietta Dehmlow, Eric Argirios Kitas
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Patent number: 6441230Abstract: Material and process of preparing such material, of the formula where R1 is a linker and C(R2P(R3)2)3 group is a triphos moiety; and wherein R1 is selected from branched and linear alkyl group and alkyl carbonyl group optionally substituted with functional groups comprising carbonyl, alkoxy, hydroxy, amino, nitro, carboxylic or sulfonic acid and esters or amides thereof; R2 are methylene (CH2) or substituted methylene groups; R3 are linear or branched alkyl or phenyl or substituted phenyl groups; polymer is any polymer containing aromatic groups, comprising polystyrene, poly-vinyl pyridine, poly pyrrole, poly pyrrolidone or derivatives thereof. The material impregnated with a transition metal has catalytic properties. The preparation of the material involves the use of an acylating agent having the formula CF3SO3C(O)C(H2X)3 or an anhydride thereof, where X is a halogen.Type: GrantFiled: February 12, 2001Date of Patent: August 27, 2002Assignee: Haldor Topsoe A/SInventors: Niels Christian Schiødt, Finn Joensen
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Patent number: 6440749Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins, and which additionally reverse pre-formed crosslinks in the advanced glycosylation endproducts by cleaving alpha-dicarbonyl-based protein crosslinks present in the advanced glycosylation endproducts. Certain agents useful are thiazolium salts. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.Type: GrantFiled: December 22, 1999Date of Patent: August 27, 2002Assignees: Alteon. Inc., The Picower Institute for Medical ResearchInventors: Anthony Cerami, Peter C. Ulrich, Dilip R. Wagle, San-Bao Hwang, Sara Vasan, John J. Egan
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Patent number: 6437167Abstract: The present invention describes new chiral stationary phases and optically active compounds therein contained. The optically active compounds contained in the stationary phases are represented by the formula of structure (I), containing at least one asymmetric carbon atom, and a substituent acting as a spacer. The stationary phases of the present invention are useful in the preparation of chromatographic columns useful for the separation of enantiomers.Type: GrantFiled: December 8, 2000Date of Patent: August 20, 2002Assignee: Societa' Cooperative Centro Ricerche Polytech A Responsabilitia' LimitataInventors: Vitomir Sunjic, Darko Kontrec, Vladimir Vinkovic
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Patent number: 6436967Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to prodrugs of compounds which selectively inhibit cyclooxygenase-2. The use of non-steroidal antiinflammatory drugs (NSAIDs) in treating pain and the swelling associated with inflammation also produce severe side effects, including life threatening ulcers. The recent discovery of an inducible enzyme associated with inflammation (“prostaglandin G/H synthase II” or “cyclooxygenase-2 (COX-2)”) provides a viable target of inhibition which more effectively reduces inflammation and produces fewer and less drastic side effects.Type: GrantFiled: September 14, 2000Date of Patent: August 20, 2002Assignee: Pharmacia CorporationInventors: John J Talley, James W Malecha, Stephen Bertenshaw, Matthew J Graneto, Jeffery Carter, Jinglin Li, Srinivasan Nagarajan, David L Brown, Donald J Rogier, Jr., Thomas D Penning, Ish K Khanna, Xiangdong Xu, Richard M Weier
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Patent number: 6437165Abstract: Immunoregulatory compounds are disclosed of the formula: as well as the pharmaceutically acceptable salts and hydrates thereof, are disclosed. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.Type: GrantFiled: August 30, 2001Date of Patent: August 20, 2002Assignee: Merck & Co., Inc.Inventors: Suzanne Mandala, James Bergstrom, Richard Hajdu, Hugh Rosen, William Parsons, Deborah J. Card, Malcolm Maccoss, Rupprecht Kathleen
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Patent number: 6437147Abstract: A novel class of imidazo heterocyclic compounds, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.Type: GrantFiled: March 16, 2001Date of Patent: August 20, 2002Assignees: Novo Nordisk, Boehringer Ingelheim International GmbHInventors: Knud Erik Andersen, Florencio Zaragoza Dorwald, Bernd Peschke, Ulla Grove Sidelmann, Klaus Rudolf, Dirk Stenkamp, Rudolf Hurnaus, Stephan Georg Muller, Bernd Krist, Birgitte Eriksen
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Patent number: 6437146Abstract: Oxazole compounds of formula (I), wherein R1 is aryl which may be substituted with halogen(s), R2 is aryl which may be substituted with halogen(s), X is single bond, (a) or SO2, R3 and R4 are independently hydrogen or suitable substituent, (wherein X is (a), neither R3 nor R4 is hydrogen), R3 and R4 may be linked together to form (b), (b) is N-containing heterocyclic group which may be substituted with one or more suitable substituent(s), R5 is hydrogen, etc., A1 is lower alkylene or single bond, (c) is cyclo(C3-C9)alkane or cyclo(C5-C9)alkene, or a pro-drug thereof, or a pharmaceutically acceptable salt thereof, which are useful as medicament.Type: GrantFiled: April 20, 2001Date of Patent: August 20, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kouji Hattori, Akira Tanaka, Yutaka Kono, Shoko Nakazato
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Patent number: 6433184Abstract: The present invention relates to polyamide-imides having head-to-tail backbone and more particularly, to polyamide-imimdes having head-to-tail ragularity to provide excellent heat and chemical resistance, physical and mechanical properties, processability, and gas permeability and selectivity.Type: GrantFiled: June 28, 2000Date of Patent: August 13, 2002Assignee: Korea Research Institute of Chemical TechnologyInventors: Kil-Yeong Choi, Jae Heung Lee, Young-Taik Hong, Moon Young Jin, Kyoung-Su Choi, Ho-Jin Park
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Patent number: 6433175Abstract: A chemical compound of formula (I), wherein n is 1, 2 or 3; R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, or R5 and R6 together form a carbocyclic or heterocyclic ring, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders, diabetes insipidus, and sleep apnea, and particularly for the treatment of obesityType: GrantFiled: February 28, 2001Date of Patent: August 13, 2002Assignee: Vernalis Research LimitedInventors: David Reginald Adams, Jonathan Mark Bentley, Jonathan Richard Anthony Roffey, Richard John Hamlyn, Suneel Gaur, Matthew Alexander James Duncton, James Edward Paul Davidson, Michael John Bickerdike, Ian Anthony Cliffe, Howard Langham Mansell
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Patent number: 6429223Abstract: In accordance with the present invention, there are provided modified forms of nonsteroidal anti-inflammatory drugs (NSAIDs). Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.Type: GrantFiled: November 17, 2000Date of Patent: August 6, 2002Assignee: Medinox, Inc.Inventors: Ching-San Lai, Tingmin Wang
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Patent number: 6429328Abstract: The invention relates to new compounds of general formula I or the pharmaceutically acceptable salts thereof, wherein X=N-R3 or CH-R4, Y=CH2 or (CH2)2, Z=O or H2; and R1, R2, R3, R4 and Ar have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: July 2, 2001Date of Patent: August 6, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Sven Luettke, Andreas Mathes
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Patent number: 6426357Abstract: The present invention provides a compound of the formula: and methods for using the same, wherein R1, R2, R3, R4 and X are those defined herein.Type: GrantFiled: July 31, 2000Date of Patent: July 30, 2002Assignee: Affymax, Inc.Inventors: Randall A. Scheuerman, Stephen D. Yanofsky, Christopher P. Holmes, Derek MacLean, Beatrice Ruhland, Ronald W. Barrett, Jay E. Wrobel, Ariamala Gopalsamy
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Patent number: 6426360Abstract: A class of compounds is described for treating inflammation and inflammation-related disorders.Type: GrantFiled: May 15, 2000Date of Patent: July 30, 2002Assignee: G D Searle & Co.Inventors: Richard M Weier, Paul W Collins, Michael A Stealey, Thomas E Barta, Renee M Huff
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Patent number: 6423712Abstract: The present invention relates to imidazolidine compounds of the formula I, The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy and prophylaxis of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of the formula I are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy or prophylaxis of illnesses which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or are associated therewith, or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part.Type: GrantFiled: September 18, 1998Date of Patent: July 23, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Volkmar Wehner, Hans Ulrich Stilz, Wolfgang Schmidt, Dirk Seiffge
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Patent number: 6423709Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.Type: GrantFiled: November 28, 2001Date of Patent: July 23, 2002Assignee: Eli Lilly and CompanyInventors: Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, III, David Lee Varie
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Patent number: 6423710Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.Type: GrantFiled: November 21, 2000Date of Patent: July 23, 2002Assignee: ICOS CorporationInventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward A. Kesicki, Amy Oliver, Laurence E. Burgess, John J. Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlachter
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Patent number: 6420364Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.Type: GrantFiled: September 8, 2000Date of Patent: July 16, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Michel Jose Emmanuel, Leah L. Frye, Eugene R. Hickey, Weimin Liu, Tina Marie Morwick, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey David Ward, Erick Richard Roush Young
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Patent number: 6420567Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides, formulations of pharmaceutically-acceptable salts thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit the activity of endothelin are also provided.Type: GrantFiled: September 26, 1997Date of Patent: July 16, 2002Assignee: Texas Biotechnology CorporationInventors: Chengde Wu, Bore Gowda Raju, Timothy Kogan, Natalie Blok