Patents Examined by Robert Gerstl
  • Patent number: 6495525
    Abstract: OMePUPA-V, (R)-N-[[4-[[(2-methylphenylamino)carbonyl]amino]phenyl]acetyl]-L-prolyl-3-methyl)-&bgr;-Alanine, a cell adhesion inhibitor, pharmaceutical compositions, and methods of treatment of cell-adhesion mediated pathologies.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: December 17, 2002
    Assignee: Biogen, Inc.
    Inventors: Wen-Cherng Lee, Alan Gill
  • Patent number: 6495580
    Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infections.
    Type: Grant
    Filed: October 18, 1999
    Date of Patent: December 17, 2002
    Assignee: ViroPharma Incorporated
    Inventors: Theodore J. Nitz, Daniel C. Pevear
  • Patent number: 6492404
    Abstract: Compounds represented by the general formula (1); and pest controlling agents containing one or more of the compounds as the active ingredients, wherein A is substituted phenyl, C1-C6 alkly or the like; B is hydrogen, optionally substituted phenyl or the like; R is C1-C6 alkly, a group represented by the general formula: COR1 (wherein R1 is C1-C12 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl or the like) or the like; X is halogeno, C1-C6 alkyl, C1-C6 haloalkyl or the like; and n is an integer of 1 to 5.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: December 10, 2002
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Yasushi Shibata, Koichiro Aoyagi, Hidemitsu Takahashi, Takao Iwasa, Tomohiro Take
  • Patent number: 6492403
    Abstract: Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4, X, Y and Z are defined in the specification.
    Type: Grant
    Filed: February 9, 2000
    Date of Patent: December 10, 2002
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Carl R. Illig, Nalin L. Subasinghe, James B. Hoffman, Kenneth J. Wilson, M. Jonathan Rudolph, Roger F. Bone, Scott L. Klein, Troy L. Randle
  • Patent number: 6489484
    Abstract: Thiadiazole-poly(ether)glycol reaction products and adducts useful as extreme pressure additives. Lubricating compositions (e.g., greases) containing the reaction products and adducts exhibit improved Timken Load properties.
    Type: Grant
    Filed: October 20, 2000
    Date of Patent: December 3, 2002
    Assignee: R. T. Vanderbilt Company, Inc.
    Inventors: Thomas J. Karol, Ronald J. Tepper
  • Patent number: 6486142
    Abstract: The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and conditions related to diabetes.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: November 26, 2002
    Assignee: Merck Frosst Canada & Co.
    Inventors: Yves Leblanc, Claude Dufresne, Jacques Yves Gauthier, Cheuk Kun Lau, Chun Sing Li, Patrick Roy, Michel Therien, John Scheigetz, Zhaoyin Wang
  • Patent number: 6486324
    Abstract: Methods for performing ring-opening cross-metathesis reactions on solid support are disclosed. Substituted cyclic compounds, libraries of the compounds, and methods of using the compounds to treat bacterial infections are also disclosed.
    Type: Grant
    Filed: January 23, 2001
    Date of Patent: November 26, 2002
    Assignee: Sepracor Inc.
    Inventors: Gregory D. Cuny, Jingrong Cao, James R. Hauske
  • Patent number: 6486141
    Abstract: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related conditions.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: November 26, 2002
    Assignee: Merck Frosst Canada & Co.
    Inventors: Cheuk Kun Lau, Christopher Bayly, Jacques Yves Gauthier, Yves Leblanc, Chun Sing Li, Patrick Roy, Michel Therien, Zhaoyin Wang
  • Patent number: 6486328
    Abstract: A novel route has been developed for substituted 2-[-6-benzyl-5-oxo-3-phenyl-(3s,7s,7aR)-perhydroimidazol[1,5-c][1,3]thiazol] compounds; crucial intermediates for D(+)-biotin of formula (7) which involves simple, efficient, practical and cost effective protocol. These are crucial intermediates for commercially important D(+)-biotin preparation. These compounds are more stable and are produced by non-hazardous methods.
    Type: Grant
    Filed: October 12, 2000
    Date of Patent: November 26, 2002
    Assignee: Council of Scientific and Industrial Research
    Inventors: Subhash Prataprao Chavan, Amar Gopal Chittiboyina, Subhash Krishnaji Kamat, Uttam Ramrao Kalkote, Thotapallil Ravindranathan
  • Patent number: 6482990
    Abstract: A prostaglandin analog represented by Formula (I): [wherein A is an ethylene group, a vinylene group or an ethynylene group, Y1 and Y2 are the same or different, and each a hydrogen atom, a halogen atom, a cyano group, —CONR3R4 (wherein R3 and R4 are the same or different, and each a hydrogen atom or a C1-6 alkyl group, or R3 and R4 together with the nitrogen atom to which they are attached form a C4-8 cyclic amine), a C1-3 aminoalkyl group, a C1-6 hydroxyalkyl group, NR5R6 (wherein R5 and R6 are the same or different, and each a hydrogen atom or a C1-6 alkyl group), a hydroxyl group, a C1-6 alkoxy group, a C1-9 alkyl group, a C1-6 alkyl group substituted with halogen(s), a C1-5 acyl group or COOR7 (wherein R7 is a hydrogen atom, a C1-6 alkyl group or a phenyl group), R1 and R2 are the same or different, and each a hydrogen atom, a halogen atom, a C1-9 alkyl group or a C1-6 alkyl group substituted with halogen(s), m is an integer of 0 to 6, and n is an integer of 0 to 3], a p
    Type: Grant
    Filed: March 4, 2002
    Date of Patent: November 19, 2002
    Assignees: Taisho Pharmaceutical Co., Ltd.
    Inventors: Fumie Sato, Tohru Tanami, Hideo Tanaka, Naoya Ono, Makoto Yagi
  • Patent number: 6479667
    Abstract: Crystalline 2S-cis-3-[[(4-mercapto-2-pyrrolidinyl)carbonyl]-amino]benzoic acid and salts and solvates thereof are disclosed. A crystalline type is described.
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: November 12, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Karel J. M. Brands, Karen M. Conrad, John M. Williams
  • Patent number: 6479507
    Abstract: The present invention relates to compounds of Formula (I) that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
    Type: Grant
    Filed: April 19, 2001
    Date of Patent: November 12, 2002
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Soan Cheng, David Michael Goldstein, Teresa Alejandra Trejo Martin, Eric Brian Sjogren
  • Patent number: 6476282
    Abstract: A superalkalinized alkylaryl sulfonate of alkaline earth metal is disclosed. The aryl radical is either a tolyl, xylyl, o xylyl, ethyl phenyl, or cumenyl radical. The alkyl chain is a linear chain that contains between 14 and 40 carbon atoms, and the aryl sulfonate radical of alkaline earth metal is fixed, in a molar proportion comprised between 0 and 13% in positions 1 or 2 of the linear alkyl chain.
    Type: Grant
    Filed: April 15, 1999
    Date of Patent: November 5, 2002
    Assignee: Chevron Chemical S.A.
    Inventor: Jean-Louis Marie Le Coent
  • Patent number: 6472405
    Abstract: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
    Type: Grant
    Filed: April 26, 1999
    Date of Patent: October 29, 2002
    Assignee: Eli Lilly and Company
    Inventors: Matthew J. Fisher, Anne Marie Happ, Joseph A. Jakubowski, Michael Dean Kinnick, Allen D. Kline, John Michael Morin, Jr., Daniel J. Sall, Marshall A. Skelton, Robert Theodore Vasileff
  • Patent number: 6472414
    Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) —O—; or (3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X,  are as defined herein.
    Type: Grant
    Filed: May 18, 1999
    Date of Patent: October 29, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
  • Patent number: 6472564
    Abstract: Toluylene diisocyanate is produced by nitration of toluene toy yield dinitrotoluene, hydrogenation of the dinitrotoluene, optionally in the presence of a solvent or diluent, to yield a crude solution of toluylene diamine and reaction water, processing the crude solution of toluylene diamine and water to yield an intermediate mixture of toluylene diamine and water wherein the processing is interrupted to result in a water content of about 1-40% by weight, preferably about 2-10% by weight of the intermediate mixture, transporting this intermediate mixture from a first production facility to a second production facility, whereat the intermediate mixture of TDA and water is completed to yield dry toluylene diamine of commercial quality, and followed by phosgenation of the toluylene diamine to give toluylene diisocyanate. It is optional to additionally process the dry toluylene diamine prior to phosgenation.
    Type: Grant
    Filed: September 8, 1998
    Date of Patent: October 29, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Biskup, Berthold Keggenhoff
  • Patent number: 6469207
    Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: June 20, 2001
    Date of Patent: October 22, 2002
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 6468977
    Abstract: Novel 1,2,4-thiadiazole compounds are provided, which are effective as inhibitors of cysteine activity-dependent enzymes and in particular of cysteine proteases. The compounds are useful in treating acne by inhibition of transglutaminase, common cold by inhibition of human rhinovirus 3C protease and inflammatory joint disease by inhibition of cathepsins. The compounds of the present invention are 3,5-disubstituted 1,2,4-thiadazole of the general formula (I): where Z is a nitrogen containing group with recognition sequence for the enzyme and Y is a substituent that tunes the reactivity of the inhibitor towards the thiol group of the cysteine activity-dependent enzyme. The Y group may also serve in recognition.
    Type: Grant
    Filed: May 23, 2000
    Date of Patent: October 22, 2002
    Assignee: Apotex Inc.
    Inventors: Khashayar Karimian, Tim Fat Tam, Regis C. S. H. Leung-Toung, Wanren Li, Steve Patrick Bryson, Jolanta Maria Wodzinska
  • Patent number: 6469004
    Abstract: The invention provides compounds having formula (I), wherein W is OH, or derivatives of the carboxylic acid, and Q is a heterocyclo-condensed ortho-phenylene residue. These compounds are useful as MEK inhibitors, particularly in the treatment of proliferative diseases such as cancer.
    Type: Grant
    Filed: July 11, 2001
    Date of Patent: October 22, 2002
    Assignee: Warner-Lambert Company
    Inventors: Stephen Barrett, Haile Tecle, Alexander J. Bridges
  • Patent number: 6465500
    Abstract: Compounds of the formula where W is n is 0, 1, or 2; m is 0, 1, 2, or 3: Y and G are each independently oxygen or sulfur; Z is —O—, —S—, —NH, or —CH2; R1 is hydrogen, C1 to C8 alkyl, substituted C1 to C8 alkyl substituted with one hydroxy, C3 to C8 alkenyl, C3 to C8 alkynyl, aryl, C1 to C3 alkylaryl, C1 to C3 alkylheteroaryl, or —Q—R4; R2 and R3 are each independently hydrogen, C1 to C6 alkyl, aryl, C1 to C3 alkylaryl, or C1 to C3 alkylheteroaryl; R4 is cyano, trifluoromethyl, —COR3, —CO2R8, —CONR9R10, —OR3, —SO2NR9R10, or —S(O)4R9; R9 and R10 are each independently hydrogen, C1 to C8 alkyl, C1 to C3 alkylaryl, aryl, or R9 and R10 may together be taken to form a three- to seven-membered alkyl ring or a three- to seven-membered heteroalkyl ring having 1 heteroatom of O; Q is C1 to C3 alkyl; R11 is hydrogen, —OR12, or —NHCOR12; R12 is hydrogen, C1 to C6 alkyl, aryl, or C1 to C3 alk
    Type: Grant
    Filed: October 23, 2000
    Date of Patent: October 15, 2002
    Assignee: Pfizer Inc.
    Inventors: John Eugene Macor, Martin James Wythes