Patents Examined by Zachary C. Tucker
  • Patent number: 7534794
    Abstract: The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are as
    Type: Grant
    Filed: October 11, 2002
    Date of Patent: May 19, 2009
    Assignee: Biovitrum AB
    Inventors: Björn Nilsson, Jan Tejbrant, Benjamin Pelcman, Erik Ringberg, Markus Thor, Jonas Nilsson, Mattias Jönsson
  • Patent number: 7476673
    Abstract: Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RAR? agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: January 13, 2009
    Assignee: Allergan, Inc.
    Inventors: Kwok Yin Tsang, Santosh Sinha, Xiaoxia Liu, Smita Bhat, Roshantha A. Chandraratna
  • Patent number: 7468367
    Abstract: This invention relates to heterocyclic substituted ethylene diamine derivatives and their use as pharmaceuticals.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: December 23, 2008
    Assignee: Smithkline Beecham p.l.c.
    Inventors: Steven Coulton, Amanda Johns, Roderick Alan Porter
  • Patent number: 7459554
    Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein Q1 and R1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases.
    Type: Grant
    Filed: October 14, 2004
    Date of Patent: December 2, 2008
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Han-Qing Dong, Kenneth Foreman, Mark Joseph Mulvihill, Anthony Innocenzo Nigro, Arno G. Steinig, Douglas Werner, Robin Wilkes
  • Patent number: 7456180
    Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where G, J, L, M, x, y, W, V, R2, R3, R4, R5, R6, R7, R8, R8a, R9, R9a, R10, R10a, R11 and R11a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
    Type: Grant
    Filed: July 29, 2004
    Date of Patent: November 25, 2008
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Serguei Sviridov, Vishnumurthy Kodumuru, Shifeng Liu, Melwyn Abreo, Michael D. Winther, Heinz W. Gschwend, Rajender Kamboj, Shaoyi Sun, Mark W. Holladay, Wenbao Li, Chi Tu
  • Patent number: 7449463
    Abstract: The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle Q is R7, pyrrolidinyl substituted with R7, piperidinyl substituted with R7 or homopiperidinyl substituted with R7; one of R2a and R3a is selected from halo, optionally mono- or polysubstituted C1-6alkyl, optionally mono- or polysubstituted C2-6alkenyl, nitro, hydroxy, Ar2, N(R4aR4b), N(R4aR4b)sulfonyl, N(R4aR4b)carbonyl, C1-6alkyloxy, Ar2oxy, Ar2C1-6alkyloxy, carboxyl, C1-6alkyloxycarbonyl, or —C(=Z)Ar2; and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen, C1-6alkyl or halogen and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen,
    Type: Grant
    Filed: December 20, 2004
    Date of Patent: November 11, 2008
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Jean-François Bonfanti, Koenraad Jozef Lodewijk Andries, Jérôme Michel Claude Fortin, Philippe Muller, Frédéric Marc Maurice Doublet, Christophe Meyer, Rudy Edmond Willebrords, Tom Valerius Josepha Gevers, Philip Maria Martha Bern Timmerman
  • Patent number: 7435735
    Abstract: Hydroxy-substituted pyridopyrrolopyrazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I): (I) wherein a, b, A, B, R1, R2, R3, R4, R5, R6, R7 and R8 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: October 18, 2004
    Date of Patent: October 14, 2008
    Assignee: Merck & Co., Inc.
    Inventors: John S. Wai, Thorsten E. Fisher, Linghang Zhuang, Donnette D. Staas, Terry A. Lyle, Boyoung Kim, Mark W. Embrey, Catherine M. Wiscount, Lekhanh O. Tran, Melissa Egbertson, Kelly L. Savage
  • Patent number: 7435728
    Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereofs, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
    Type: Grant
    Filed: June 20, 2005
    Date of Patent: October 14, 2008
    Assignee: Pfizer Inc
    Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
  • Patent number: 7432268
    Abstract: There are disclosed compounds of the formula (I): prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3 17?-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.
    Type: Grant
    Filed: November 14, 2005
    Date of Patent: October 7, 2008
    Assignee: Schering Corporation
    Inventors: Timothy Guzi, Kamil Paruch, Alan Mallams, Jocelyn D. Rivera, Ronald J. Doll, Viyyoor M. Girijavallabhan, Jonathan A. Pachter, Yi-Tsung Liu, Anil K. Saksena
  • Patent number: 7429593
    Abstract: Compounds having an activity to enhance the expression of apoAI are provided, which are used as medicaments. Compounds of formula (I): in which ring A and Ar1 are independently a monocyclic or bicyclic aromatic carbocyclic group or aromatic heterocyclic group, each of which may be optionally substituted, or the like; R is a hydrogen or the like; Z is oxygen or the like; Y1 and Y2 are a hydrogen, a lower alkyl, or the like; n is an integer of 0 to 2; the broken line is the presence or absence of a bond; and the wavy line represents a cis- or trans-geometrical isomerism with respect to the double bond; are disclosed.
    Type: Grant
    Filed: September 14, 2001
    Date of Patent: September 30, 2008
    Assignee: Shionogi & Co., Ltd.
    Inventors: Teruo Yamamori, Kiyoshi Nagata, Natsuki Ishizuka, Katsunori Sakai
  • Patent number: 7427637
    Abstract: The present invention relates to bicyclic dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: June 8, 2004
    Date of Patent: September 23, 2008
    Assignee: Merck & Co. Inc.
    Inventors: Paul J. Coleman, Lou Anne Neilson
  • Patent number: 7425557
    Abstract: New pyridine-based compounds of Formula I, compositions, and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3-mediated disorders in vivo are provided. The methods, compounds, and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
    Type: Grant
    Filed: September 6, 2005
    Date of Patent: September 16, 2008
    Assignee: Novartis Vaccines and Diagnostics, Inc.
    Inventors: John M Nuss, Stephen D Harrison, David B Ring, Rustum S Boyce, Kirk Johnson, Keith B Pfister, Savithri Ramurthy, Lynn Seely, Allan S Wagman, Manoj C Desai, Barry H Levine
  • Patent number: 7423154
    Abstract: An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention includes an asymmetric addition of organometallic compounds to chiral sulfinimine to give adducts in predominantly one diastereomer can subsequently be transferred into pure enantiomers of by cleavage of the chiral auxilliary which is followed by synthesis of the piperazine ring by alkylation procedures.
    Type: Grant
    Filed: November 22, 2005
    Date of Patent: September 9, 2008
    Assignee: AstraZeneca AB
    Inventors: William Brown, Niklas Plobeck
  • Patent number: 7420051
    Abstract: Processes are provided for preparing compounds with a fused ring structure of formula (XIV). Such products include ecteinascidins and have a spiroamine-1,4-bridge. The process involving forming a 1,4 bridge using a 1-labile, 10-hydroxy, 18-protected hydroxyl, di-6,8-en-5-one fused ring compound. After formation of the 1,4 brige, C-18 protection is removed before spiroamine introduction.
    Type: Grant
    Filed: October 11, 2005
    Date of Patent: September 2, 2008
    Assignee: Pharma Mar, S.A.
    Inventors: Andrés Francesch, Carolina Fernández, José Luis Chicharro, Pilar Gallego, Maria Zarzuelo, Ignacio Manzanares, Marta Perez, Carmen Cuevas, María Jes{dot over (u)}s Martin, Simon Munt
  • Patent number: 7417044
    Abstract: The present invention provides particulate tadalafil having a particle size of about 200 to about 600 microns and a process for controlling the particle size of tadalafil.
    Type: Grant
    Filed: February 27, 2006
    Date of Patent: August 26, 2008
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Inbal Ornan, Ehud Amir, Guy Samburski, Yhoshoa Ovadya
  • Patent number: 7410968
    Abstract: The present invention relates to compounds represented by formula (I): where the structural variables are as defined herein. The compounds are useful for promoting hydration of mucosal surfaces.
    Type: Grant
    Filed: August 26, 2005
    Date of Patent: August 12, 2008
    Assignee: PARION SCIENCES, Inc.
    Inventors: Michael R. Johnson, Bruce F. Molino, Jianzhong Zhang, Bruce Sargent
  • Patent number: 7410960
    Abstract: A compound of formula I or a salt thereof [ML1L2]2+??(I) where M is selected from the group consisting of platinum(II), palladium (II) and copper(II); L1 is an intercalator moiety; and L2 is a bidentate ligand, provided that when L2 is other than a bidentate ligand containing an aryl or phenyl group, L2 is a chiral bidentate ligand.
    Type: Grant
    Filed: February 22, 2002
    Date of Patent: August 12, 2008
    Assignees: The University of Western Sydney, The University of Sydney
    Inventors: Ronald Ralph Fenton, Janice Aldrich-Wright
  • Patent number: 7410972
    Abstract: The invention provides N-pyrazinyl-thienylsulphonamides of formula (I) for use in the treatment of chemokine mediated diseases.
    Type: Grant
    Filed: December 17, 2002
    Date of Patent: August 12, 2008
    Assignee: AstraZeneca AB
    Inventors: Andrew Baxter, Timothy Johnson, Nicholas Kindon, Bryan Roberts, John Steele, Michael Stocks, Nicholas Tomkinson
  • Patent number: 7407958
    Abstract: Compounds of the formula: wherein R1, R2, R3, A1 and A2 are as defined herein, which are used advantageously in inhibiting the TGF-? and/or activin signaling pathway in mammals.
    Type: Grant
    Filed: November 8, 2004
    Date of Patent: August 5, 2008
    Assignees: SK Chemicals Co., Ltd., EWHA University Industry Collaboration Foundation
    Inventors: Dae-Kee Kim, Yung-Jue Bang, Hun-Taek Kim, Il-Sang Cho, Myoung-Soon Park, Young Jae An, Joon Hun Choi
  • Patent number: 7407961
    Abstract: A pyrazine derivative of the following formula (I): or a salt thereof. The pyrazine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.
    Type: Grant
    Filed: October 26, 2004
    Date of Patent: August 5, 2008
    Assignee: Astellas Pharma Inc.
    Inventors: Satoshi Yonishi, Satoshi Aoki, Yuji Matsushima, Atsushi Akahane