Patents Examined by Mukund J. Shah
  • Patent number: 6716833
    Abstract: Compounds of the formula: are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
    Type: Grant
    Filed: February 27, 2003
    Date of Patent: April 6, 2004
    Assignee: Wyeth Holdings Corporation
    Inventors: Jeremy I. Levin, James M. Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
  • Patent number: 6716836
    Abstract: A compound of formula I: wherein A is a connecting chain of (C1-3) alkyl; B is O or S; R1 is H, (C1-6) alkyl, halo, CF3, or OR1a wherein R1a is H or (C1-6)alkyl; R2 is H or Me; R3 is H or Me; R4 is H, (C1-4) alkyl, (C3-4) cycloalkyl and (C1-4)alkyl(C3-7)cycloalkyl; W is selected from  wherein, a) one of Y is SO2 and the other Y is NR5, provided that both are not the same, wherein R5 is H, (C1-6)alkyl,(C3-6) cycloalkyl, the alkyl being substituted, COR5o, COOR5p or CONR5pPR5q; and each R8 is H, (C1-4) alkyl, (C3-6) cycloalkyl, or (C1-4) alkyl-(C3-6) cycloalkyl; or b) E is CR8aR8b wherein R8a and R8b is H, or alkyl and J is CH2; or J is CR8aR8b and E is CH2, and the dotted line represents a single bond; or c) E is C(O) and J is CR8aR8b or J is C(O) and E is CR8aR8b and the dotted line represents a single bond; or d) E and J are CR8aR8b and the dotted line represents a double bond. Compounds of formula I have activity against HIV WT and double mutant strains.
    Type: Grant
    Filed: March 13, 2002
    Date of Patent: April 6, 2004
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: William W. Ogilvie, Robert Déziel, Julie Naud, Jeffrey O'Meara, Dale R. Cameron
  • Patent number: 6716828
    Abstract: This invention relates to compounds, pharmaceutical compositions, and methods for the treatment or prevention of neural or cardiovascular tissue damage related to cerebral ischemia and reperfusion injury in an animal by administering Poly(ADP-ribose) polymerase (“PARP”) inhibitors.
    Type: Grant
    Filed: February 13, 2001
    Date of Patent: April 6, 2004
    Assignee: Guilford Pharmaceuticals, Inc.
    Inventors: Jia-He Li, Jie Zhang
  • Patent number: 6716851
    Abstract: The present invention is directed to substituted 2-aryl-4-arylaminopyrimidine and analogs thereof, represented by the general Formula I: wherein A, Ar1, Ar2, R1 and R3 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. The compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: April 6, 2004
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, John A. Drewe, Bao Nguyen, Azra Pervin
  • Patent number: 6716837
    Abstract: Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with the proviso that at least one of B and D is CH and with the further proviso that one of B and D can represent N only when W and Z are both other than N; A is a group of Formula II, III or IV, such that group A contains at least 1 N atom; NR7 is either —NH— or —N═; is a single or double bond; X is a N atom, a CH group or a C(OH) group when is a single bond; or, when is a double bond, a C atom; Y is an NH, N-alkyl, N-benzyl or CH2 group; U and V each represent a N atom or a CH group, with the proviso that both cannot be N; a and b are, independently, 0 or 1; c is an integer from 0 to 3; d is an integer from 1 to 3; e is an integer from 1 to 2; f is an integer from 0 to 3; g is an integer from 3 to 6 and h is an integer from 2 to 3; such that the sum of c a
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: April 6, 2004
    Assignee: NPS Allelix Biopharmaceuticals, Inc.
    Inventors: Louise Edwards, Methvin Isaac, Shawn Maddaford, Abdelmalik Slassi, Tao Xin
  • Patent number: 6713467
    Abstract: Compounds of formula I and II, or pharmaceutically-acceptable salts thereof, are useful as inhibitors of Factor VIIa, Factor IXa, Factor Xa, Factor FXIa, tryptase, and urokinase, wherein ring B is phenyl or pyridyl, L is a linker, and R1-R27, W, Z1, and Z2 are as defined in the specification.
    Type: Grant
    Filed: November 7, 2001
    Date of Patent: March 30, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory S. Bisacchi, James C. Sutton, Shung C. Wu
  • Patent number: 6713474
    Abstract: Chemical compounds having structural formula I and physiologically acceptable salts and metabolites thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the kinases, whose activity is inhibited by these chemical compounds, are involved in immunologic, hyperproliferative, or angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyper proliferative disorders, rheumatiod arthritis, disorders of the immune system, trasplant rejections and imflammatory disorders.
    Type: Grant
    Filed: March 29, 2000
    Date of Patent: March 30, 2004
    Assignee: Abbott GmbH & Co. KG
    Inventors: Gavin C. Hirst, David Calderwood, Rainer Munschauer, Lee D. Arnold, David N. Johnston, Paul Rafferty
  • Patent number: 6710047
    Abstract: The invention relates to compounds of formula I, wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* or (iii) together form a bridge in subformula I** wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa, thia, or imino; Q is methyl; R is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstited amino, halogen, alkyl, substituted alkyl, hydroxy, etheritied or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, p
    Type: Grant
    Filed: January 7, 2003
    Date of Patent: March 23, 2004
    Assignee: Novartis AG
    Inventors: Guido Bold, Jörg Frei, Peter Traxler, Karl-Heinz Altmann, Helmut Mett, David Raymond Stover, Jeanette Marjorie Wood
  • Patent number: 6706698
    Abstract: The present invention relates to novel &agr;-substituted-&bgr;-aminoethylphosphonate and &agr;-substituted-&bgr;-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.
    Type: Grant
    Filed: September 26, 2001
    Date of Patent: March 16, 2004
    Assignee: Ilex Products, Inc.
    Inventors: Hieu Trung Phan, Lan Mong Nguyen, Vinh Van Diep, Raymond Azoulay, Harald Eschenhof, Eric Joseph Niesor, Craig Leigh Bentzen, Robert John Ife
  • Patent number: 6706703
    Abstract: A bis(5-aryl-2-pyridyl) compound represented by formula (1) or a salt thereof: wherein A is a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted aromatic heterocyclic group, and X is a group selected from the group consisting of moieties having formulas (2) to (5): wherein, in formula (2), m is an integer of 1 or 2; in formula (3), n is an integer of 1 to 6; and in formula (4), R is hydrogen or a lower alkyl group and p is an integer of 1 to 6.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: March 16, 2004
    Assignee: Kowa Co., Ltd.
    Inventors: Hiroyuki Ishiwata, Seiichi Sato, Mototsugu Kabeya, Soichi Oda, Makoto Suda, Manabu Shibasaki
  • Patent number: 6706740
    Abstract: Heterocyclic aromatic amides (HAA) according to Formula I: wherein X1-X4, M, Z, and A are herein defined. The invention also encompasses hydrates, salts and complexes thereof. These compounds are useful as antifungal agents.
    Type: Grant
    Filed: December 13, 2001
    Date of Patent: March 16, 2004
    Assignee: Dow AgroSciences LLC
    Inventors: Michael J. Ricks, William H. Dent, III, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesel, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Matthew J. Henry, Jenifer L. Adamski Butz, Robert P. Gajewski
  • Patent number: 6706724
    Abstract: The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pyl
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: March 16, 2004
    Assignee: NitroMed, Inc.
    Inventors: Subhash P. Khanapure, David S. Garvey, Richard A. Earl, Maiko Ezawa, Xinqin Fang, Ricky D. Gaston
  • Patent number: 6706663
    Abstract: There are provided 3-heterocyclic substituted benzisothiazole and benzisoxazole compounds having the structural formula I where Q, X, X1 and Z are defined as in claim 1. Further provided are compositions and methods comprising those compounds for the control of undesirable plant species.
    Type: Grant
    Filed: April 17, 2001
    Date of Patent: March 16, 2004
    Assignee: Wyeth
    Inventors: Peter John Wepplo, Richard Anthony Rampulla, Gavin David Heffernan, Michael Vernie Cossette, Charles Malcolm Langevine, Venkataraman Kameswaran, Robert Eugene Diehl, James Joseph Fiordeliso, Gregory Jay Haley, Michael Anthony Guaciaro
  • Patent number: 6703387
    Abstract: The invention is concerned with novel benzodiazepine derivatives, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds are inhibitors of the human papillomavirus E1 helicase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HPV mediated diseases.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: March 9, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David N. Hurst, Philip Stephen Jones, Kevin Edward Burdon Parkes, Martin John Parratt, Francis Xavier Wilson
  • Patent number: 6699853
    Abstract: The present invention relates to 4-Haloalkyl-3-heterocyclylpyridines, 4-haloalkyl-5-heterocyclyl-pyrimidines and 4-trifluoromethyl-3-oxadiazolylpyridines, Processes for Their Preparation, Compositions Comprising Them, and Their Use as Pesticides More particularly, the present invention relates to 4-trifluoromethyl-3-oxadiazolylpyridines of the formula (I′), to processes for their preparation, to compositions comprising them and to the use of these compounds for controlling animal pests, in particular insects, spider mites, ectoparasites and helminths: wherein X, Y are as defined in the description.
    Type: Grant
    Filed: January 24, 2002
    Date of Patent: March 2, 2004
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Sven Harmsen, Henricus Maria Martinus Bastiaans, Wolfgang Schaper, Jörg Tiebes, Uwe Döller, Daniela Jans, Ulrich Sanft, Waltraud Hempel, Maria-Theresia Thönessen, Thomas Taapken, Burkhard Rook, Manfred Kern
  • Patent number: 6699862
    Abstract: Novel indolyl-2-phenyl bisamidines are described which are DNA methyltransferase inhibiting agents, and pharmaceutical compositions containing them are used as antiproliferative agents for treating a disease, especially a neoplastic disease, characterized by abnormally rapid proliferation of tissue involved in said disease; said indolyl-2-phenyl bisamidines comprising a and a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen or (C1-C3)alkyl; R3, R4, R5, R8, R9, and R10 are hydrogen or (C1-C3)alkyl, or R3 and R4 may be taken together, or R8 and R9 may be taken together with the nitrogen atoms to which they are attached, to form an imidazolinyl group; R14 is —H; —NHC(═O)(CH2)mR20; —(CH2)mR20; —CH(CH3)R20; —(CH2)m(C6H3)—R17; —(CH2)m(C6H3)—R20; —(CH2)m(heterocyclyl)—R17; —(CH2)m(heterocyclyl)—R20; —CH2CH═CHR20; —(CH2)mC(═O)NH—CHR20R21; or —(CH2)mC(═O)NH—CH2&m
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: March 2, 2004
    Assignee: Pfizer Inc.
    Inventors: Steven W. Goldstein, Banauara L. Mylari, Jose R. Perez, Edward A. Glazer
  • Patent number: 6699855
    Abstract: The present invention relates to compounds of Formula (I): wherein A1 is methylene, ethylene or propylene group and A2 is N or CR5, or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HCV NS3 protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: March 2, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Xiaojun Zhang, Wei Han
  • Patent number: 6700016
    Abstract: Acrylic acid or methacrylic acid is purified be crystallization to obtain crystals and a mother liquor, by a process in which the crystals are washed with a was liquid containing the acid and having a temperature from 15 to 40° C. Furthermore, a process for the preparation of acrylic acid or methacrylic acid comprises the abovementioned purification process.
    Type: Grant
    Filed: December 6, 2001
    Date of Patent: March 2, 2004
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Eck, Jörg Heilek, Dieter Baumann, Volker Schliephake
  • Patent number: 6699854
    Abstract: The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukaemia, psoriasis and the like.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: March 2, 2004
    Assignee: Cyclacel Limited
    Inventors: Shudong Wang, Peter M. Fischer
  • Patent number: 6696463
    Abstract: The invention relates to 3-heteroarylidenyl-2-azaindolinone compounds of the formula: wherein, A is selected from the group consisting of nitrogen, oxygen and sulfur; only one of B, D, E, F or G is nitrogen; Z is selected from the group consisting of oxygen, sulfur and NR11; or physiologically acceptable salts thereof; and wherein the groups R1-R7 are defined herein. The 3-heteroarylidenyl-2-azaindolinone compounds of the preferred embodiments of the present invention have improved hydrosolubility and are expected to modulate the activity of protein tyrosine kinases. The 3-heteroarylidenyl-2-azaindolinone compounds of the preferred embodiments of the present invention should be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.
    Type: Grant
    Filed: September 7, 2001
    Date of Patent: February 24, 2004
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon