Patents Examined by Mukund J. Shah
  • Patent number: 6747045
    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, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6—Alk2— (b-1), or -Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6a
    Type: Grant
    Filed: April 3, 2002
    Date of Patent: June 8, 2004
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn
  • Patent number: 6743821
    Abstract: A method and lactate compound for four unique purposes: (1) the provision of a fuel energy source to skeletal muscles, hearts and other tissues and organs of humans and other mammals during exercise and recovery; (2) cardiac energy supplementation following ischemia; (3) the maintenance of blood glucose and restoration of liver glycogen; and (4) the provision of fluid and electrolytes to humans and other mammals before, during and after exercise. The lactate compound is preferably a glycerol-lactate ester or a glycerol-acetate ester.
    Type: Grant
    Filed: May 30, 2002
    Date of Patent: June 1, 2004
    Inventor: George A. Brooks
  • Patent number: 6743914
    Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.
    Type: Grant
    Filed: November 20, 2002
    Date of Patent: June 1, 2004
    Assignee: Brandeis University
    Inventors: Li Deng, Jianfeng Hang, Liang Tang
  • Patent number: 6740656
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, R1, R2, R3a, R3b, R4, R5, R6, and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Grant
    Filed: August 2, 2002
    Date of Patent: May 25, 2004
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Joseph Pontillo, Chen Chen
  • Patent number: 6740647
    Abstract: Novel five-membered heterocyclic amidines, their preparation and use as competitive inhibitors of trypsin-like serine proteases, especially thrombin and kininogenases such as kallikrein. Pharmaceutical compositions which contain the compounds as active ingredients, and use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory agents.
    Type: Grant
    Filed: June 21, 2000
    Date of Patent: May 25, 2004
    Assignee: Abbott GmbH & Co., KG
    Inventors: Dorit Baucke, Udo Lange, Helmut Mack, Werner Seitz, Hans Wolfgang Höffken, Wilfried Hornberger
  • Patent number: 6740654
    Abstract: Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —S—, —C(O)—, —C(S)—, —S(O)—, —S(O)2, —N(R8)— or —C(R8)(R8a)—; Ar2 is an optionally substituted aromatic or heteroaromatic group; Alk is a chain  in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group other than a 2,6-naphthyridin-1-yl, isoquinolin-1-yl, 2,7-naphthyridin-1-yl or quinazolin-4-yl group; and the salt
    Type: Grant
    Filed: July 5, 2001
    Date of Patent: May 25, 2004
    Assignee: Celltech R & D Limited
    Inventors: Barry John Langham, Rikki Peter Alexander, John Clifford Head, Janeen Marsha Linsley, John Robert Porter, Sarah Catherine Archibald, Graham John Warrellow
  • Patent number: 6737418
    Abstract: This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R13 are set in the specification. The invention also is directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    Type: Grant
    Filed: April 30, 2002
    Date of Patent: May 18, 2004
    Assignee: Euro-Celtique S.A.
    Inventors: Derk Hogenkamp, Ravindra Upasani, Phong Nguyen
  • Patent number: 6730670
    Abstract: A compound of the formula Compounds of formula I have a good affinity to the A2A receptor and are useful for the treatment of diseases mediated by this receptor.
    Type: Grant
    Filed: December 10, 2002
    Date of Patent: May 4, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Alexander Flohr
  • Patent number: 6730672
    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 (1-4C)alkyl; M1 is a group of the formula: NR2—L1—T1R3 in which R2 and R3 together form a (1-4C)alkylene 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)r—L2—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: March 8, 2001
    Date of Patent: May 4, 2004
    Assignee: Zeneca Limited
    Inventors: Alan Wellington Faull, Andrew Stocker, Colette Marie Mayo, John Preston
  • Patent number: 6730668
    Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; each R2 unit is independently selected from the group consisting of: a) hydrogen; b) —(CH2)jO(CH2)nR8; c) —(CH2)jNR9aR9b; d) —(CH2)jCO2R10; e) —(CH2)jOCO2R10 f) —(CH2)jCON(R10)2; g) —(CH2)jOCON(R10)2; h) two R2 units can be taken together to form a carbonyl unit; i) and mixtures thereof; R8, R9a, R9b, and R10 are each independently hydrogen, C1-C4 alkyl, and mixtures thereof; R9a and R9b can be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10 units can be take together to form a carbocyclic or heterocyclic ring
    Type: Grant
    Filed: September 18, 2002
    Date of Patent: May 4, 2004
    Assignee: The Procter & Gamble Company
    Inventors: Michael Philip Clark, Matthew John Laufersweiler, Jane Far-Jine Djung, Michael George Natchus, Biswanath De
  • Patent number: 6730683
    Abstract: Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.
    Type: Grant
    Filed: June 10, 2002
    Date of Patent: May 4, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: Timothy Francis Gallagher, Jeffrey Charles Boehm, Jerry Leroy Adams
  • Patent number: 6730674
    Abstract: This invention relates to novel sulfonyl pyridazinone compounds of the formula: wherein R1, R2, X, and Y are defined herein, which are useful as aldose reductase inhibitors in the treatment or prevention of certain complications arising from diabetes mellitus, pharmaceutical compositions comprising the sulfonyl pyridazinone, pharmaceutical compositions comprising a combination of the sulfonyl pyridazinone together with a second pharmaceutical agent, therapeutic methods comprising the administration of the sulfonyl pyridazinone compounds, therapeutic methods comprising the administration of the sulfonyl pyridazinone compounds in combination with a second pharmaceutical agent and compounds useful as intermediates for preparing the sulfonyl pyridazinone compounds of this invention.
    Type: Grant
    Filed: February 26, 2002
    Date of Patent: May 4, 2004
    Assignee: Pfizer Inc
    Inventors: William H. Martin, Banavara L. Mylari
  • Patent number: 6727380
    Abstract: A process for the oxidation of a C2 to C4 alkane to produce the corresponding alkene and carboxylic acid which process comprises contacting in an oxidation reaction zone, said alkane, molecular oxygen-containing gas, and optionally, at least one of the corresponding alkene and water, in the presence of at least two catalysts each active, with different selectivities, for the oxidation of the alkane to the corresponding alkene and carboxylic acid, to produce a product stream comprising said alkene, carboxylic acid and water, and in which process the molar ratio of alkene to carboxylic acid produced in said oxidation reaction zone is adjusted or maintained at a pre-determined value by controlling the relative proportions of the at least two catalysts in said oxidation reaction zone. Such an oxidation process may be used in an integrated process, such as for the manufacture of ethyl acetate or vinyl acetate.
    Type: Grant
    Filed: February 21, 2003
    Date of Patent: April 27, 2004
    Assignee: BP Chemicals Limited
    Inventors: Brian Ellis, Mark Stephen Roberts
  • Patent number: 6727237
    Abstract: The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme.
    Type: Grant
    Filed: October 25, 2002
    Date of Patent: April 27, 2004
    Inventors: Wayne J. Brouillette, Donald Muccio, Mark J. Jedrzejas, Christie G. Brouillette, Yancho Devedjiev, Walter Cristofoli, Lawrence J. DeLucas, Jose Gabriel Garcia, Laurent Schmitt, Sadanadan E. Velu
  • Patent number: 6727254
    Abstract: Novel compounds of the formula wherein R is optionally substituted heteroaryl or R1 is H or C1-C6 alkyl; and R2 and R3 are —CH3, —OCH3 or halo; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions therefore, and the use of said compounds in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.
    Type: Grant
    Filed: November 6, 2002
    Date of Patent: April 27, 2004
    Assignee: Schering Corporation
    Inventors: Deen Tulshian, Ginny D. Ho, Fay W. Ng
  • Patent number: 6727257
    Abstract: This invention is directed to dihydropyrimidine compounds of the following formula: wherein A is which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: December 5, 2000
    Date of Patent: April 27, 2004
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Dhanapalan Nagarathnam, George Chiu, T. G. Murali Dhar, Wai C. Wong, Mohammad R. Marzabadi, Charles Gluchowski, Bharat Lagu, Shou Wu Miao
  • Patent number: 6723719
    Abstract: Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein R1 is C1 to C3 alkyl substituted with C3 to C6 cycloalkyl, CONR5R6 or a N-linked heterocyclic group; (CH2)nHet or (CH2)nAr; R2 is C1 to C6 alkyl; R3 is C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy; R4 is SO2NR7R8; R5 and R6 are each independently selected from H and C1 to C4 alkyl optionally substituted with C1 to C4 alkoxy, or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic group; R7 and R8, together with the nitrogen atom to which they are attached, form a 4-R10-piperazinyl group; R10 is H or C1 to C4 alkyl optionally substituted with OH, C1 to C4 alkoxy or CONH2; H is an optionally substituted C-linked 5- or 6-membered heterocyclic group; Ar is optionally substituted phenyl; and n is 0 or 1; are potent and selective cGMP PDE5 inhibitors useful in the treatment of, in
    Type: Grant
    Filed: September 29, 1999
    Date of Patent: April 20, 2004
    Assignee: Pfizer Inc
    Inventors: Mark Edward Bunnage, John Paul Mathias, Stephen Derek Albert Street, Anthony Wood
  • Patent number: 6723728
    Abstract: Solid phases of (−)-cis-FTC, which are designated herein as amorphous (−)-FTC and Forms II and III (−)-cis-FTC) are provided that can be distinguished from Form I (−)-cis-FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. A hydrated crystalline form of (±)-cis-FTC (i.e. racemic cis-FTC), and a dehydrated form of the hydrate, are also provided, and can similarly be distinguished from other forms of FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These FTC forms can be used in the manufacture of other forms of FTC, or in pharmaceutical compositions. Particularly preferred uses of these forms are in the treatment of HIV or hepatitis B.
    Type: Grant
    Filed: March 1, 2002
    Date of Patent: April 20, 2004
    Assignees: Gilead Sciences, Inc., Abbott Laboratories
    Inventors: Yuerong Hu, Devalina Law, Kenneth R. Phares
  • Patent number: 6723711
    Abstract: A compound of the structure A method for the inhibition of the binding of &agr;4&bgr;1 integrin to its receptors, for example VCAM-1(vascular cell adhesion molecule-1) and fibronectin; pharmaceutically active compositions comprising these compounds; and the use of these compounds for the control or prevention of diseases states in which &agr;4&bgr;1 is involved are also disclosed.
    Type: Grant
    Filed: October 9, 2001
    Date of Patent: April 20, 2004
    Assignee: Texas Biotechnology Corporation
    Inventors: Ronald J. Biediger, Brian Dupre, Linda K. Hamaker, George W. Holland, Jamal M. Kassir, Wen Li, Robert V. Market, Noel Nguyen, Ian L. Scott, Chengde Wu, E. Radford Decker
  • Patent number: 6720421
    Abstract: Phenylurethane compounds of the following general formula (1); asymmetric urea compounds of the following general formula (10) obtained from the phenylurethane compounds; barbituric acid derivatives of general formula (18) produced from the asymmetric urea compounds, which have specific substituents and are useful in diazo thermal recording materials; and diazo thermal recording materials containing the barbituric acid derivative.
    Type: Grant
    Filed: February 19, 2002
    Date of Patent: April 13, 2004
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Akinori Fujita, Naoto Yanagihara, Yohsuke Takeuchi, Daisuke Arioka, Kimi Ikeda, Sachiko Arai