Patents Examined by John Kight
  • Patent number: 6506777
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R7, R8, X, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: January 14, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Jennifer L. Loebach, Malcolm Maccoss, Sander G. Mills
  • Patent number: 6420392
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.
    Type: Grant
    Filed: October 9, 1996
    Date of Patent: July 16, 2002
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Tesfaye Biftu, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, T Y Shen
  • Patent number: 6335455
    Abstract: This invention pertains to a process for the preparation of 2,5-dihydrofurans by the isomerization of &ggr;,&dgr;-epoxyalkenes in the presence of a catalyst system comprising an organotin compound and an alkali metal iodide.
    Type: Grant
    Filed: August 28, 1998
    Date of Patent: January 1, 2002
    Assignee: Eastman Chemical Company
    Inventors: Shaowo Liang, Yao-Ching Liu
  • Patent number: 6329390
    Abstract: Disclosed herein are compounds selective for a 5-HT1D receptor, the compounds having the general formula (I): Also disclosed is the use of these compounds as pharmaceuticals to treat indications where stimulation of a 5-HT1D receptor is indicated such as migrane.
    Type: Grant
    Filed: July 17, 1998
    Date of Patent: December 11, 2001
    Assignee: NPS Allelix Corp.
    Inventors: Abdelmalik Slassi, Jalaj Arora, Ashok Tehim
  • Patent number: 6296856
    Abstract: Cosmetic/pharmaceutical/dermatological compositions suited for promoting desquamation of the skin of a mammalian organism in need of such treatment and/or to stimulate epidermal renewal and thus to combat intrinsic and/or extrinsic aging thereof, via topically applying same to the skin of such organism, comprise a cutaneous aging-combating effective amount of at least one polyholoside, preferably a heterogeneous polyholoside, in a topically applicable, cosmetically/pharmaceutically/dermatologically acceptable vehicle, carrier or diluent therefor.
    Type: Grant
    Filed: July 10, 1997
    Date of Patent: October 2, 2001
    Assignee: Societe l'Oreal S.A.
    Inventors: Nathalie Pineau, Lionel Breton
  • Patent number: 6294537
    Abstract: A method for treating diseases which involve interaction of neurokinin B with NK3 receptors in humans. The method comprises administering a therapeutically effective amount of a NK3 antagonist compound having the formula: in which: R1 and R11 together represent a —(CH2)3-group.
    Type: Grant
    Filed: May 7, 1999
    Date of Patent: September 25, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Daniel Bichon, Patrick Gueule, Didier Van Broeck, Xavier Emonds-Alt, Vincenzo Proietto
  • Patent number: 6294574
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 25, 2001
    Assignee: Cytomed, Inc.
    Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
  • Patent number: 6281211
    Abstract: This invention is related to substituted semicarbazides represented by Formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1 and R2 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R3, R4, R5 and R6 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R3 and R4 is defined as above, and R5 and R6 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one of O, S, NR7, CH2, C(O), NR7C(O), C(O)NR7, SO, SO2 or a covalent bond; where R7 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; n is
    Type: Grant
    Filed: September 21, 2000
    Date of Patent: August 28, 2001
    Assignee: Euro-Celtique S.A.
    Inventors: Sui Xiong Cai, Nancy C. Lan, Soo Hong-Bae
  • Patent number: 6268361
    Abstract: The present invention is related to methods for treating pathological conditions resulting from an estrogen deficiency, such as cardiovascular disease and osteoporosis, and is further related to methods for treating estrogen-dependent cancer, such as breast and uterine cancer, employing compounds of formula I
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 31, 2001
    Inventor: Alan D. Palkowitz
  • Patent number: 6265420
    Abstract: Nitric oxide scavengers, such as dithiocarbamate-containing compounds, are used to reduce side effects caused by therapeutic administration of nitric oxide sources by administering the nitric oxide scavenger(s) to the subject after the therapeutic effect of the nitric oxide source has been achieved. For example, the nitric oxide source can be coadministered with the nitric oxide scavenger, with the latter formulated in a time release vehicle selected to delay release of the scavenger for a period of time sufficient to ensure that the therapeutic goal of the nitric oxide source has been achieved before release of the scavenger. Formulations and kits, including a bubble pack with pairwise arrangement of unit doses of a desired nitric oxide source and nitric oxide scavenger, are also provided.
    Type: Grant
    Filed: June 23, 1998
    Date of Patent: July 24, 2001
    Assignee: Medinox, Inc.
    Inventor: Ching-San Lai
  • Patent number: 6265433
    Abstract: The present invention provides compounds having the structure: and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.
    Type: Grant
    Filed: May 14, 1999
    Date of Patent: July 24, 2001
    Assignee: G. D. Searle & Company
    Inventors: Barbara Baosheng Chen, Helen Chen, Mark Andrew Russell, Julie Marion Miyashiro, James Malecha, Thomas Dale Penning
  • Patent number: 6255490
    Abstract: 7-Aza-bicyclo[2.2.1]-heptane and -heptene derivatives are disclosed that can be administered to a mammal, including a human, to treat disorders associated with a decrease or increase in cholinergic activity.
    Type: Grant
    Filed: February 13, 1998
    Date of Patent: July 3, 2001
    Assignee: University of Virginia
    Inventors: T. Y. Shen, W. Dean Harman, Dao Fei Huang, Javier Gonzalez
  • Patent number: 6251898
    Abstract: Newly-created fluorenone drugs can be used to prevent, treat, or otherwise reduce damage to a brain or spinal cord following a medical crisis. These new drugs are markedly improved analogs of previously-known fluorenone compounds that were never commercialized or developed into medically useful treatments. The new analogs have the following structure: where X is a lower alkyl, substituted alkyl, or cycloalkyl group, R is selected from certain types of ether, ester, or amide groups, and Y1 and Y2 are halogen, hydrogen, or methyl. These new compounds can penetrate a blood-brain barrier and potently inhibit the unwanted release of excitotoxic neurotransmitters by astrocyte cells following an injury or insult to the brain or spinal cord. As an illustration, some of these new analogs were more than 30 times more potent than the previously known best compound in reducing aspartate release by stressed astrocytes.
    Type: Grant
    Filed: August 24, 1999
    Date of Patent: June 26, 2001
    Assignee: Questcor Pharmaceuticals, Inc.
    Inventors: Edward J. Cragoe, Jr., Paul J. Marangos, Torsten R. Weimann
  • Patent number: 6248694
    Abstract: The invention provides novel mepiquat plant growth regulator compositions which have improved hygroscopicity and corrosion characteristics. The novel mepiquat plant growth regulator compositions of the invention can be readily prepared from technical mepiquat chlorid inter alia by electrochemical ion exchange processes or by quaternization of N-methylpiperidine with dimethylcarbonate as starting material.
    Type: Grant
    Filed: September 22, 1999
    Date of Patent: June 19, 2001
    Assignees: BASF Aktiengesellschaft, BASF Corporation
    Inventors: Reiner Kober, David G. Hobbs, Scott W. Gibson, Kenneth Eugene Fersch, Wilhelm Rademacher, Jörg Botzem, Markus Frede, Matthias Dernbach, Reimer Göttsche, Reinhard Dötzer
  • Patent number: 6242467
    Abstract: Compounds of formula (I) wherein R is hydroxy, hydrogen, alkenyl, alkynyl or aryl, and R1 is aryl or heteroaryl, are useful in the treatment and prophylaxis of conditions mediated by CD23 or TNF.
    Type: Grant
    Filed: September 17, 1999
    Date of Patent: June 5, 2001
    Assignee: SmithKline Beecham p.l.c.
    Inventor: Andrew Faller
  • Patent number: 6239145
    Abstract: Nitroxyl compounds represented by general formula (I) which are usable in acquiring information about active oxygen or in vivo free radicals as biological images such as magnetic resonance images or magnetoencephalograms, wherein A represents hydrogen or —L—(CH2)n—OCOR (wherein L represents —COO— or -alkylene-COO—; and R represents C1-4 alkyl); R1, R2, R3, and R4 represent each C1-4 alkyl; and n is a number of from 1 to 4. Drugs and reagents containing the above compounds are usable in preventing, treating or diagnosing ischemic diseases, digestive diseases, cancer, cranial nervous diseases accompanied by nerve degeneration, inflammation, cataracts, or drug-induced organopathy.
    Type: Grant
    Filed: December 27, 1999
    Date of Patent: May 29, 2001
    Assignee: Daiitchi Radioisotope Laboratories, Ltd.
    Inventors: Hideo Utsumi, Hiroaki Sano, Masaichi Naruse, Takashi Igarashi, Tetsuo Oi
  • Patent number: 6239121
    Abstract: A subject of the invention is the compounds of formula (I): in which X is a halogen atom, D represents the remainder of an optionally substituted pentagonal or hexagonal ring and optionally carrying an unsaturation, R1, R2, R3, R4, Y and n are as defined in the description, their preparation process and intermediates, their use as medicaments and the compositions containing them.
    Type: Grant
    Filed: November 29, 1999
    Date of Patent: May 29, 2001
    Assignee: Hoechst Marion Roussel
    Inventors: Yamina Bouali, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
  • Patent number: 6239280
    Abstract: The present invention is directed to a process for synthesizing 1,5 disubstituted imidazoles with biaryl components of the formula (I): which are usefull as Farnesyl-Protein Transferase inhibitors.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: May 29, 2001
    Assignee: Merck & Co., Inc.
    Inventors: David Askin, Jennifer A. Cowen, Peter E. Maligres, J. Christopher McWilliams, Marjorie S. Waters
  • Patent number: 6235258
    Abstract: A non-crystalline silica solid is obtainable by a process comprising the step of contacting in a liquid medium at least one silica precursor with at least one template comprising a polyethyleneimine or a mixture of two or more thereof.
    Type: Grant
    Filed: July 27, 1998
    Date of Patent: May 22, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulrich Müller, Ulrich Steuerle
  • Patent number: 6235951
    Abstract: The present invention relates to a method for producing 1,1,1,3,3-pentafluoropropane. This method includes the steps of (a) adding hydrogen fluoride to 1-chloro-3,3,3-trifluoropropene in the presence of an addition catalyst to obtain 1,1,1,3-tetrafluoro-3-chloropropane; and (b) disproportionating the 1,1,1,3-tetrafluoro-3-chloropropane into the 1,1,1,3,3-pentafluoropropane and 1,1,1-trifluoro-3,3-dichloropropane, in the presence of a disproportionation catalyst. This method is a useful method for producing 1,1,1,3,3-pentafluoropropane in an industrial scale, because its steps (a) and (b) are respectively superior in selectivity and yield. According to the invention, 1-chloro-3,3,3-trifluoropropene may be produced by a method including a step of reacting 1,1,1,3,3-pentachloropropane with hydrogen fluoride in a gas phase in the presence of a fluorination catalyst. This method is useful, because yield of 1-chloro-3,3,3-trifluoropropene is high.
    Type: Grant
    Filed: November 20, 1996
    Date of Patent: May 22, 2001
    Assignee: Central Glass Company, Limited
    Inventors: Fuyuhiko Sakyu, Satoshi Yoshikawa, Yasuo Hibino, Yoshihiko Gotoh, Ryouichi Tamai