1,2-thiazoles (including Hydrogenated) Patents (Class 548/206)
  • Patent number: 7674810
    Abstract: Compounds having the formula i wherein m, R1, R2, R4 and X1 are herein defined are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis replication, processes for making the compounds and synthetic intermediates used in the process.
    Type: Grant
    Filed: April 28, 2006
    Date of Patent: March 9, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: James F. Blake, Jay Bradford Fell, John P. Fischer, Robert Than Hendricks, Stacey Renee Spencer, Peter J. Stengel
  • Patent number: 7671212
    Abstract: Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.
    Type: Grant
    Filed: December 20, 2004
    Date of Patent: March 2, 2010
    Assignee: Schering Corporation
    Inventors: Arthur G. Taveras, J. Robert Merritt, John J. Baldwin, Junying Zheng, Purakkattle J. Biju, Younong Yu, Jianhua Chao, Gaifa Lai, Minglang Wu
  • Patent number: 7651538
    Abstract: A hair dye composition containing an azo dye (1) or a salt thereof, (wherein R1 to R4 represents H, aliphatic hydrocarbon group, aryl group, halogen atom, acyl group, cyano group, acylamino group, or the like, wherein R1 and R2, and/or R3 and R4 may be coupled to form a 5- or 6-membered ring; X represents C or N, with the proviso that when X represents C, n stands for 1, and when X represents N, n stands for 0; A1, A2, A3 and A4 each represents N or represents C substituted by Y or having H, with the proviso that at least one of A1, A2, A3 and A4 is a nitrogen atom; and Y represents a substituent with the proviso that m stands for an integer from 0 to 3).
    Type: Grant
    Filed: February 10, 2006
    Date of Patent: January 26, 2010
    Assignees: Kao Corporation, Fujifilm Corporation
    Inventors: Masakazu Yamaguchi, Dominic Pratt, Yasuhiro Ishiwata
  • Publication number: 20100016389
    Abstract: The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.
    Type: Application
    Filed: September 24, 2009
    Publication date: January 21, 2010
    Applicant: Wyeth
    Inventors: Youssef L. Bennani, Lawrence Nathan Tumey, Elizabeth Ann Gleason, Michael Joseph Robarge
  • Patent number: 7638648
    Abstract: Compounds of formulas 1 through 17 provided in the specification specifically or selectively inhibit either the cytochrome P450RAI-1 enzyme or the cytochrome P450RAI-2 enzyme.
    Type: Grant
    Filed: March 23, 2007
    Date of Patent: December 29, 2009
    Assignee: Allergan Inc.
    Inventors: Jayasree Vasudevan, Liming Wang, Xiaoxia Liu, Kwok Yin Tsang, Ling Li, Janet A. Takeuchi, Thong Vu, Richard Beard, Smita Bhat, Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 7615570
    Abstract: Compounds having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein L, A, G, R1, R2 and R3 are as defined herein. These compounds are particularly useful in the treatment of pain, inflammatory hyperalgesia, and urinary dysfunctions, such as bladder overactivity and urinary incontinence.
    Type: Grant
    Filed: December 5, 2005
    Date of Patent: November 10, 2009
    Assignee: Abbott Laboratories
    Inventors: Brian S. Brown, Tammie K. Jinkerson, Ryan G. Keddy, Chih-Hung Lee
  • Patent number: 7598423
    Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.
    Type: Grant
    Filed: November 15, 2005
    Date of Patent: October 6, 2009
    Assignee: Eli Lilly and Company
    Inventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
  • Publication number: 20090208449
    Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5 and X are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Application
    Filed: February 12, 2009
    Publication date: August 20, 2009
    Inventors: Sharada Shenvi Labadie, Clara Jeou Jen Lin, Francisco Xavier Talamas, Robert James Weikert
  • Patent number: 7557095
    Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt thereof, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: May 7, 2007
    Date of Patent: July 7, 2009
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, David W. Old, Todd Gac
  • Patent number: 7553964
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: June 1, 2006
    Date of Patent: June 30, 2009
    Assignee: Abbott Laboratories
    Inventors: Huaqing Liu, Kathryn J. Hancock, legal representative, Marlon D. Cowart, Arthur A. Hancock
  • Patent number: 7524870
    Abstract: The present invention relates to compounds of formula (I) wherein Ar, Ar2, R2, R3, R4, m, p and s are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases that are associated with the activation of the glycogen synthase enzyme, such as diabetes.
    Type: Grant
    Filed: November 21, 2005
    Date of Patent: April 28, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paul Gillespie, Robert Alan Goodnow, Jr., Jefferson Wright Tilley
  • Patent number: 7517902
    Abstract: Disclosed are novel substituted indazole compounds, pharmaceutical compositions comprising such compounds, and methods of treatment comprising such compounds.
    Type: Grant
    Filed: December 4, 2006
    Date of Patent: April 14, 2009
    Assignee: Aventis Pharma S.A.
    Inventors: Frank Halley, Michel Tabart, Hervé Bouchard, Catherine Souaille, Alain Le Brun, Fabrice Viviani, Laurence Gauzy-Lazo, Pascal Desmazeau, Odile Angouillant-Boniface, Bruno Filoche-Romme
  • Patent number: 7511149
    Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.
    Type: Grant
    Filed: February 9, 2007
    Date of Patent: March 31, 2009
    Assignee: Dow AgroSciences LLC
    Inventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
  • Patent number: 7498349
    Abstract: Aromatic compounds exemplified by exhibit antimicrobial activity.
    Type: Grant
    Filed: August 1, 2003
    Date of Patent: March 3, 2009
    Assignee: Genesoft Pharmaceuticals, Inc.
    Inventors: Roland W. Burli, Eldon E. Baird, Jacob A. Kaizerman, Dustin L. McMinn
  • Publication number: 20090023789
    Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Application
    Filed: April 10, 2008
    Publication date: January 22, 2009
    Applicant: Abbott Laboratories
    Inventors: William A. Carroll, Michael J. Dart, Teodozyj Kolasa, Tongmei Li, Derek W. Nelson, Meena V. Patel, Sridhar Peddi, Arturo Perez-Medrano, Xueqing Wang
  • Publication number: 20090022689
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.
    Type: Application
    Filed: July 9, 2008
    Publication date: January 22, 2009
    Inventors: Yat Sun Or, Lu Ying, Ce Wang, Yao-Ling Qiu
  • Publication number: 20080255095
    Abstract: A compound of the formula (I): wherein R1 is C1-C6 alkyl, amino, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are hydrogen or C1-C6 alkyl; Arom is phenyl, idenyl, napthyl, phenanthrenyl, furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; A is C1-C6 alkylene; Ra is hydrogen, C1-C6 alkyl or C2-C6 alkenyl; E is a single bond, oxygen, sulfur or —NR4—, wherein R4 is hydrogen or C1-C7 alkanoyl; X1 and X2 are oxygen or sulfur; or a pharmacologically acceptable salt or ester thereof.
    Type: Application
    Filed: June 18, 2007
    Publication date: October 16, 2008
    Applicant: BTG INTERNATIONAL LIMITED
    Inventors: Kazuo Koyama, Shinji Marumoto, Narihiro Toda, Hiroshi Kogen, Keiko Suzuki
  • Patent number: 7335775
    Abstract: Conjugates of epothilones and epothilone derivatives (as effectors) with suitable biomolecules (as recognition units) are described. Their production is carried out by the effectors being reacted with suitable linkers, and the compounds that are produced are conjugated to the recognition units. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.
    Type: Grant
    Filed: August 25, 2006
    Date of Patent: February 26, 2008
    Assignee: Schering Aktiengesellschaft
    Inventors: Markus Berger, Gerhard Siemeister, Ulrich Klar, Jorg Willuda, Andreas Menrad, Klaus Bosslet
  • Patent number: 7316851
    Abstract: An electroluminescent element is disclosed, comprising an electroluminescent material and a fluorescent substance emitting light having an emission maximum at the wavelength different from that of light emitted from the electroluminescent material upon absorption of the light emitted from the electroluminescent material. A color conversion filter is also disclosed, comprising a fluorescent substance emitting light having an emission maximum at the wavelengths of 400 to 700 nm upon absorption of the light emitted from the electroluminescent material.
    Type: Grant
    Filed: September 4, 2003
    Date of Patent: January 8, 2008
    Assignee: Konica Corporation
    Inventors: Hiroshi Kita, Yoshiyuki Suzuri, Taketoshi Yamada, Kazuaki Nakamura, Noriko Ueda, Yasushi Okubo
  • Patent number: 7307173
    Abstract: Electron acceptor compounds, nonlinear optical chromophores, methods for making the compounds and chromophores, and materials and electro-optic devices that include the chromophores.
    Type: Grant
    Filed: February 22, 2005
    Date of Patent: December 11, 2007
    Assignee: University of Washington
    Inventors: Kwan-Yue Jen, Sei-Hum Jang, Bart Kahr
  • Patent number: 7301028
    Abstract: The present invention relates to dihydropyrazole 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 12, 2003
    Date of Patent: November 27, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Arrington, Mark E. Fraley
  • Patent number: 7297797
    Abstract: The invention relates to novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, R4, A1, A2, R5, R6, R7, R8, R9 and Q are as defined in the disclosure, to a process for preparing these compounds and to their use for controlling pests.
    Type: Grant
    Filed: September 8, 2003
    Date of Patent: November 20, 2007
    Assignee: Bayer CropScience AG
    Inventors: Johannes Rudolf Jansen, Udo Kraatz, Hubertus Stakemeier, Thomas Seitz, Fritz Maurer, Martin Füsslein, Bernd Alig, Christian Funke, Werner Hallenbach, Jörg Konze, Udo Beckmann, Ulrich Görgens
  • Patent number: 7273882
    Abstract: There is provided a series of substituted acyl guanidines of Formula (Ik) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R2, R3, R4, R5, R25, R26 and R27 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: June 20, 2006
    Date of Patent: September 25, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Samuel Gerritz, Shuhao Shi, Shirong Zhu
  • Patent number: 7271184
    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: February 17, 2004
    Date of Patent: September 18, 2007
    Assignee: Novartis Animal Health US, Inc.
    Inventors: Thomas Goebel, Eliane Humbert-Droz, Maurizio Schwarzenbach
  • Patent number: 7247720
    Abstract: A process for the phosphitylation of an alcohol or thiol with a phosphitylation agent in the presence of an activator is provided. The activator has the formula: wherein p is 0 or an integer from 1 to 4 and R for each occurrence is a substituent. Preferably X7 is O and p is 0. The activator is commonly employed as a salt complex with an organic base. Preferred alcohols or thiols include nucleosides and oligonucleotides. The process is particularly suited for the synthesis of phosphoramidites.
    Type: Grant
    Filed: October 8, 2003
    Date of Patent: July 24, 2007
    Assignee: Avecia Biotechnology Inc.
    Inventor: Nanda Dulal Sinha
  • Patent number: 7244851
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.
    Type: Grant
    Filed: July 5, 2005
    Date of Patent: July 17, 2007
    Assignee: Genentech, Inc.
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Patent number: 7208169
    Abstract: The invention relates to novel biphenylcarboxamides of the formula (I) in which R1, R2, m, n, R3, Y and A are as defined in the disclosure, to a plurality of processes for preparing these substances and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: April 24, 2007
    Assignee: Bayer CropScience LP
    Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Robert Markert, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck, Martin Kugler, Thomas Jaetsch
  • Patent number: 7199133
    Abstract: Novel compounds of formula (I), wherein D, W, X, Y, T and R1 have the meanings cited in claim 1, are inhibitors of coagulation factor Xa and can be used for the prophylaxis and/or therapy of thromboembolic diseases and in the treatment of tumors
    Type: Grant
    Filed: October 10, 2002
    Date of Patent: April 3, 2007
    Assignee: Merck Patent Gesellschaft
    Inventors: Dieter Dorsch, Bertram Cezanne, Christos Tsaklakidis, Werner Mederski, Johannes Gleitz, Christopher Barnes
  • Patent number: 7186843
    Abstract: This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both.
    Type: Grant
    Filed: April 29, 2004
    Date of Patent: March 6, 2007
    Assignee: Daiichi Pharmaceutical Co. Ltd.
    Inventors: Makoto Takemura, Hisashi Takahashi, Katsuhiro Kawakami, Toshiyuki Takeda, Rie Miyauchi
  • Patent number: 7186738
    Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereo Formula (I): wherein N-HeT is for example triazolyl; Q is for example phenyl or pyridyl, substituted with: T is for example selected from (TAa1 to TAa12) such as (TAa1) and (TAa5): R4h, R5h, R6h are for example selected from hydrogen, (1–4C)alkyl, (1–4C)alkoxy-carbonyl, (1–4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.
    Type: Grant
    Filed: March 16, 2004
    Date of Patent: March 6, 2007
    Assignee: AstraZeneca AB
    Inventors: Michael Barry Gravestock, Neil James Hale, Sheila Irene Hauck
  • Patent number: 7169797
    Abstract: The present invention is directed to compounds of formula (I), or a pharmaceutically suitable salt or prodrug thereof, which are useful for the selective inhibition of protein tyrosine phosphatase-1B (PTP1B), and are useful for the treatment of disorders caused by overexpressed or altered protein tyrosine phosphatase 1B.
    Type: Grant
    Filed: February 4, 2004
    Date of Patent: January 30, 2007
    Assignee: Abbott Laboratories
    Inventors: Zhili Xin, Gang Liu, Zhonghua Pei, Bruce G. Szczepankiewicz, Michael D. Serby, Hongyu Zhao
  • Patent number: 7157482
    Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereof, wherein: N—HET is for example triazolyl substituted with R1; R1 is for example optionally substituted (1-4C)alkyl; Q is for example phenyl or pyridyl, substituted with T; T is for example selected from (TAa1 to TAa12) such as (TAa1 and TAa5); formula (II): R4h, R5h, R6h are for example selected from hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl, (1-4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.
    Type: Grant
    Filed: March 16, 2004
    Date of Patent: January 2, 2007
    Assignee: AstraZeneca AB
    Inventors: Michael Barry Gravestock, Neil James Hale, Sheila Irene Hauck
  • Patent number: 7129254
    Abstract: Conjugates of epothilones and epothilone derivatives (as effectors) with suitable biomolecules (as recognition units) are described. Their production is carried out by the effectors being reacted with suitable linkers, and the compounds that are produced are conjugated to the recognition units. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.
    Type: Grant
    Filed: July 31, 2003
    Date of Patent: October 31, 2006
    Assignee: Schering Aktiengesellschaft
    Inventors: Markus Berger, Gerhard Siemeister, Ulrich Klar, Jorg Willuda, Andreas Menrad, Klaus Bosslet
  • Patent number: 7119104
    Abstract: A compound represented by the formula (I) or a salt of the compound, and a PPAR-? activator which contains the compound or salt as the active ingredient: (wherein A represents O or S; B1 represents N, etc.; B2 represents O, etc.; each of X1 and X2 represents O, S, a bond, etc.; Y represents C1-8 alkylene chain; Z represents O or S; R1 represents aryl, etc. which can have substituents; R2 represents C1-8 alkyl, etc.; R3 represents C1-8 alkyl, C2-8 alkenyl, etc.; each of R4 and R5 represents hydrogen, C1-8 alkyl, etc.; and R6 represents hydrogen, etc.; provided that each of Z and R3 is attached to the benzene ring, and X2 is not attached to the benzene ring).
    Type: Grant
    Filed: October 9, 2002
    Date of Patent: October 10, 2006
    Assignee: Nippon Chemiphar, Co., Ltd.
    Inventors: Shogo Sakuma, Tomio Yamakawa, Takashi Kanda, Seiichiro Masui
  • Patent number: 7105556
    Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
    Type: Grant
    Filed: May 22, 2002
    Date of Patent: September 12, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. Cheng, Yoon Jeon, Wei Wang
  • Patent number: 7091229
    Abstract: A compound of formula (I) wherein A and B are optionally substituted cyclohexenyl or phenyl groups, X is carbonyl or sulfonyl, and Y is 5–7 atoms-linker, is useful as histone deacetylase inhibitors, particularly for inhibiting cell proliferation.
    Type: Grant
    Filed: January 24, 2002
    Date of Patent: August 15, 2006
    Assignee: Hoffman-La Roche Inc.
    Inventors: Guy Georges, Adelbert Grossmann, Olaf Mundigl, Wolfgang von der Saal, Tim Sattelkau
  • Patent number: 7087599
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
    Type: Grant
    Filed: February 14, 2001
    Date of Patent: August 8, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Dann LeRoy Parker, Jr., Ronald W. Ratcliffe, Robert R. Wilkening, Kenneth J. Wildonger
  • Patent number: 7078403
    Abstract: Disclosed herein are compounds of formula II: wherein Alk, Z, X1, X2, R1, —R10 and R11 are defined herein, and their salts and pharmaceutically acceptable derivatives thereof, as well as other compounds of the general formula Het-A-Alk-W-Ar-C(X2)?NO-X2 where Het, A, W and Ar are also defined herein. These compounds are useful in treating picornavirus infections in mammals. Novel intermediates of these compounds, as well as pharmaceutical compositions and methods of use, are also disclosed herein.
    Type: Grant
    Filed: June 16, 2000
    Date of Patent: July 18, 2006
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Wen-Yang Wu, Keith Watson, Darryl McConnell, Betty Jin, Guy Krippner
  • Patent number: 7074870
    Abstract: Metal-ligand complexes that are useful as precursors to catalysts for the polymerization of olefins are provided. Certain of the catalysts are particularly effective at polymerizing ethylene and styrene into copolymers having novel properties, including a low molecular weight and close comparison between vinyl and methyl end groups.
    Type: Grant
    Filed: September 23, 2005
    Date of Patent: July 11, 2006
    Assignee: Symyx Technologies, Inc.
    Inventors: Oliver Brümmer, Gary M. Diamond, Christopher Goh, Anne M. LaPointe, Margarete K. Leclerc, James Longmire, James A. W. Shoemaker
  • Patent number: 7064214
    Abstract: This invention encompasses novel methods of preparing sulfinamides and sulfoxides, particularly stereomerically pure sulfinamides and sulfoxides. The invention further encompasses novel compounds from which sulfinamides and sulfoxides can be prepared.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: June 20, 2006
    Assignee: Apsinterm LLC
    Inventors: Chris Hugh Senanayake, Zhengxu Han, Dhileepkumar Krishnamurthy, Derek Pflum, Harold Scott Wilkinson
  • Patent number: 7045660
    Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.
    Type: Grant
    Filed: March 3, 2004
    Date of Patent: May 16, 2006
    Assignee: Aventis Pharma Limited
    Inventors: Garry Fenton, Tahir Nadeem Majid, Malcolm Norman Palfreyman
  • Patent number: 7041670
    Abstract: The present invention relates to novel florfenicol compounds having the chemical structure: wherein the compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.
    Type: Grant
    Filed: April 8, 2003
    Date of Patent: May 9, 2006
    Assignee: Schering-Plough Animal Health Corporation
    Inventors: Constantine G. Boojamra, Lee S. Chong, Scott J. Hecker, Tomasz W. Glinka, Dale E. Shuster
  • Patent number: 7015225
    Abstract: Derivatives of retinamide are potent and selective apoptosis-inducing agents. These compounds exhibit antitumor properties and as such can be used in the treatment of cancer and other hyperproliferative disorders.
    Type: Grant
    Filed: June 26, 2003
    Date of Patent: March 21, 2006
    Inventor: Larry Chen
  • Patent number: 6989451
    Abstract: Substituted isothiazole compounds and compositions are provided, wherein particularly preferred compositions and methods are directed towards inhibition of various protein kinases (especially MEK and/or ERK). Consequently, particularly preferred methods include treatment of diseases associated with abnormality in MEK and/or ERK function.
    Type: Grant
    Filed: June 4, 2003
    Date of Patent: January 24, 2006
    Assignee: Valeant Research & Development
    Inventors: Weijian Zhang, William Ricketts, Haoyun An, Zhi Hong
  • Patent number: 6987104
    Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: January 17, 2006
    Assignee: Vicuron Pharmaceuticals Inc.
    Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
  • Patent number: 6982264
    Abstract: The invention relates to substituted alcohol compounds of the formula (I): wherein X, R1, R2, R3, RN, R20 and RC are defined herein. The compounds are useful in the treatment or prevention of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers.
    Type: Grant
    Filed: June 27, 2002
    Date of Patent: January 3, 2006
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Varghese John, Roy Hom, John Tucker
  • Patent number: 6965004
    Abstract: Metal-ligand complexes that are useful as precursors to catalysts for the polymerization of olefins are provided. Certain of the catalysts are particularly effective at polymerizing ethylene and styrene into copolymers having novel properties, including a low molecular weight and close comparison between vinyl and methyl end groups.
    Type: Grant
    Filed: May 20, 2004
    Date of Patent: November 15, 2005
    Assignee: Symyx Technologies, Inc.
    Inventors: Oliver Brümmer, Gary M. Diamond, Christopher Goh, Anne M. LaPointe, Margarete K. Leclerc, James Longmire, James A. W. Shoemaker
  • Patent number: 6958348
    Abstract: Disclosed is an anti-cancer compound represented by Structural Formula (I): The variables in Structural Formula (I) are described hereinbelow. Also disclosed is a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound represented by Structural Formula (I) (preferably an effective amount). Also disclosed is a method of treating a subject with cancer by administering to the subject an effective amount of a compound represented by Structural Formula (I).
    Type: Grant
    Filed: August 29, 2002
    Date of Patent: October 25, 2005
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Keizo Koya, Lijun Sun, Mitsunori Ono, Guiqing Liang, David James, Hao Li, Zhi-Qiang Xia
  • Patent number: 6936630
    Abstract: Antiatherosclerotic agents are provided which are represented by Formulas I or II: wherein R is wherein R9, R10, R11, R12, R13, and R14 are each, independently, hydrogen or a lower alkyl of 1-6 carbon atoms; R6, and R7 are each, independently, hydrogen, lower alkyl of 1-6 carbon atoms, or CH2COOR8, where R8 is a lower alkyl of 1-6 carbon atoms; and X is O or S; R1 is hydrogen or a lower alkyl of 1-6 carbon atoms; R2, R3, and R4 are each, independently, hydrogen or halogen; and R5 is a lower alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 10, 2003
    Date of Patent: August 30, 2005
    Assignee: Wyeth
    Inventors: Robert J. Steffan, Amedeo A. Failli
  • Patent number: RE40558
    Abstract: The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: October 28, 2008
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Zaid Jayyosi, Gerard M. McGeehan, Michael F. Kelley, Richard F. Labaudiniere, Litao Zhang, Robert D. Groneberg, Daniel G. McGarry, Thomas J. Caulfield, Anne Minnich, Mark Bobko