Patents Examined by Mukund J. Shah
  • Patent number: 6780857
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: October 24, 2002
    Date of Patent: August 24, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker, Ui Tae Kim
  • Patent number: 6777426
    Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human &agr;2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the &agr;2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: August 20, 2001
    Date of Patent: August 17, 2004
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Wai C. Wong, Yoon T. Jeon, T. G. Murali Dhar, Charles Gluchowski
  • Patent number: 6777551
    Abstract: The present invention relates to a process for the preparation of sulphonamide-substituted imidazotriazinones of the general formula (I) characterized in that compounds of the formula (II) are reacted with sulphuric acid and the products obtained are then reacted with thionyl chloride and converted in situ in an inert solvent using an amine into the compounds according to the invention and, if appropriate, reacted to give the corresponding salts, hydrates or N-oxides.
    Type: Grant
    Filed: December 17, 2001
    Date of Patent: August 17, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Marc Nowakowski, Reinhold Gehring, Werner Heilmann, Karl-Heinz Wahl
  • Patent number: 6777403
    Abstract: Therefore, it is critical that the roles these enzymes play in biological processes outside of extracellular matrix degradation or remodeling be understood in order to assess their potential as targets for therapeutic intervention, and to design safe, conveniently produced, orally active inhibitors. Elastase inhibitors can differ with respect to their ability to inhibit different elastases. As a result, the spectrum of elastases inhibited by a specific drug candidate as well as the spectrum of activities these enzymes have with respect to proteins other than elastin are properties to consider in evaluating the drug candidates.
    Type: Grant
    Filed: December 23, 2002
    Date of Patent: August 17, 2004
    Assignee: Cortech, Inc.
    Inventor: John C. Cheronis
  • Patent number: 6774129
    Abstract: The present invention concerns the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; Alk is C1-6alkanediyl; n is 1 or 2; p is 0, 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine.
    Type: Grant
    Filed: April 16, 2002
    Date of Patent: August 10, 2004
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ludo Edmond Josephine Kennis, Serge Maria Aloysius Pieters, François Paul Bischoff
  • Patent number: 6774235
    Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0, 1, 2, 3 or 4; R1 and R2 are each independently selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each of the aforementioned C1-12alkyl groups may optionally and each individually be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl; and each R4 independently is hydroxy, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is —X—R5 or —X—Alk—R6; wherein R5 and R6 each independently are indanyl, indolyl or phen
    Type: Grant
    Filed: February 5, 2002
    Date of Patent: August 10, 2004
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frederik Frans Desiré Daeyaert, Bart De Corte, Marc René De Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici
  • Patent number: 6770667
    Abstract: The present invention is a compound and pharmaceutical composition comprising a compound of formula (I): wherein R1 is a 4-(lower) alkyl-imidazol-1-yl or a 4,5-di(lower) alkyl-imidazol-1-yl group, R2 is a hydrogen atom or a lower alkyl group, and R3 is a fluorenyl group. The compound of formula (I) includes pharmaceutically acceptable salts: The compound of formula (I) and salts thereof have 5-HT antagonism activity.
    Type: Grant
    Filed: March 21, 2002
    Date of Patent: August 3, 2004
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kiyotaka Ito, Glen W. Spears, Fumie Takahashi, Akira Yamada, Masaki Tomishima, Hiroshi Miyake
  • Patent number: 6770666
    Abstract: The present invention provides a fused ring compound of the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a therapeutic agent for hepatitis C, which contains this compound. The compound of the present invention shows an anti-hepatitis C virus (HCV) action based on the HCV polymerase inhibitory activity, and is useful as a therapeutic agent or prophylactic agent for hepatitis C.
    Type: Grant
    Filed: August 24, 2001
    Date of Patent: August 3, 2004
    Assignee: Japan Tobacco Inc.
    Inventors: Hiromasa Hashimoto, Kenji Mizutani, Atsuhito Yoshida
  • Patent number: 6770637
    Abstract: Substituted 4-phenyl-pyridine compounds with activity as antagonists of Neurokinin 1 receptors, methods of making these compounds and preparing.
    Type: Grant
    Filed: August 3, 2001
    Date of Patent: August 3, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Thierry Godel, Torsten Hoffmann, Patrick Schnider, Heinz Stadler
  • Patent number: 6770608
    Abstract: The present invention generally relates to a textile softening composition which comprises, as the softening agent, a quaternary ammonium salt which comprises a mixture of mono-, di- and tri-ester components, wherein the amount of diester quaternary is greater than about 50% by weight, and the amount of triester quaternary is less than about 25% by weight based on the total amount of quaternary ammonium salt. The invention also relates to a softening agent which comprises a high diester quaternary ammonium salt mixture comprising mono- and diester components derived for ether dialkanolamines. The invention also relates to processes for preparing said softening agents, and methods of use as a fabric softener and as a hair and skin conditioner.
    Type: Grant
    Filed: April 6, 2001
    Date of Patent: August 3, 2004
    Assignee: Akzo Nobel N.V.
    Inventors: Ralph Franklin, Robert Mendello, Paul Albert Iacobucci, Dale Steichen, Phuong-Nga Trinh
  • Patent number: 6770664
    Abstract: Bicyclic heterocyclic substituted phenyl oxazolidinone compounds of the formula: wherein Y is a radical of Formulae II or III: in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.
    Type: Grant
    Filed: June 9, 2003
    Date of Patent: August 3, 2004
    Inventors: Steven D. Paget, Dennis J. Hlasta
  • Patent number: 6770646
    Abstract: The invention provides certain pyrrolo-, thieno-, furano-and pyrazolo-[3,4-d]-pyridazinones, processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and methods of treatment involving their use.
    Type: Grant
    Filed: December 10, 2001
    Date of Patent: August 3, 2004
    Assignee: AstraZeneca AB
    Inventors: John Bantick, Martin Cooper, Philip Thorne, Matthew Perry
  • Patent number: 6767909
    Abstract: A compound, suitable as an alpha-2B-adrenoceptor antagoist, having a structure of formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4 and R5 are independently of each other H, a straight or branched alkyl or alkoxy group with 1 to 4 carbon atoms, or a halogen; X is H, a straight or branched alkyl chain with 1 to 4 carbon atoms, phenyl, —OH or ═O; Z is H, acetyl, —CH2—Ph—O—CF3 or —CH2—Ph—CF3, Y is a ring structure optionally linked to formula (I) with an alkyl chain having one or two carbon atoms. The compound is suitable for use in a method for treatment or prevention of a disease mediated by the alpha-2B-adrenoceptor in a mammal.
    Type: Grant
    Filed: July 17, 2002
    Date of Patent: July 27, 2004
    Assignee: Oy Juvantia Pharma Ltd.
    Inventors: Topi Joutsamo, Andrei Yurievitch Tauber, Harri Salo, Anna-Maria Hoffrén, Siegfreid Wurster
  • Patent number: 6762171
    Abstract: The invention creates a very high-novelty medicinal drug for the carbohydrate and lipid metabolism-related diseases by finding out an inhibitory substance or antagonist against PPAR &agr; and PPAR &ggr;, and relates to an application of fatty acid CoA thioester that was found out as an active inhibitory substance against peroxisome proliferator-activated receptor &agr; and &ggr; (hereinafter referred to as PPARs) to the assay of medicinal drug, and a use of fatty acid CoA thioester for medicinal drug.
    Type: Grant
    Filed: May 30, 2002
    Date of Patent: July 13, 2004
    Assignee: Kyorin Pharmaceutical Co, Ltd.
    Inventors: Koji Murakami, Tomohiro Ide, Toshiro Mochizuki, Takashi Kadowaki
  • Patent number: 6759407
    Abstract: Novel pesticides of formula (I) wherein the substituents, R, R1, R2, R2′, T, U, X and Y are as defined in claim 1, are described. Also described are compositions suitable for use as parasiticides comprising those compounds as active ingredient and to methods of controlling parasites that are based on the administration of those compounds or compositions, and to the use of the said compounds and compositions in a method of controlling parasites and in the manufacture of pesticides for use against parasites. Also described are intermediates of formula (XX) wherein R1, R2, R2′, T, U, X and Y are as defined in claim 1; and Hal is halogen. The latter also exhibit parasiticidal activity and are suitable for the preparation of the compounds of formula (I).
    Type: Grant
    Filed: January 21, 2003
    Date of Patent: July 6, 2004
    Assignee: Novartis Animal Health US, Inc.
    Inventors: Thomas Goebel, Eliane Humbert-Droz, Maurizio Schwarzenbach
  • Patent number: 6759534
    Abstract: The present invention relates to a process for preparing pyridazinone aldose reductase inhibitors which are useful in the prevention and/or treatment of diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. The invention also relates to novel intermediates useful in preparing those aldose reductase inihibitors.
    Type: Grant
    Filed: January 7, 2003
    Date of Patent: July 6, 2004
    Assignee: Pfizer Inc.
    Inventor: Norma J. Tom
  • Patent number: 6756393
    Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.
    Type: Grant
    Filed: April 7, 2003
    Date of Patent: June 29, 2004
    Assignee: Acadia Pharmaceuticals, Inc.
    Inventors: Carl-Magnus A. Andersson, Glenn Croston, Eva L. Hansen, Allan Kjaersgaard Uldam
  • Patent number: 6756512
    Abstract: The invention relates to a novel process for preparing 2-alkyl-3-chlorophenols.
    Type: Grant
    Filed: October 30, 2002
    Date of Patent: June 29, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Walter Hübsch, Reinhard Lantzsch, Thorsten Müh, Holger Weintritt
  • Patent number: 6756371
    Abstract: The compounds of formula (I) in which R1, R2, A, B and Ar have the meanings as given in the description are novel effective PDe4 inhibitors
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: June 29, 2004
    Assignee: Altana Pharma AG
    Inventor: Geert Jan Sterk
  • Patent number: 6750349
    Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-6alkynyl-oxy; R2 is hydrogen, C1-6alkyl C1-6alkyloxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk-X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or
    Type: Grant
    Filed: June 5, 2002
    Date of Patent: June 15, 2004
    Assignee: Janssen Pharmaceutics, N.V.
    Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn