Divalent Chalcogen Or Acyclic Nitrogen Double Bonded Directly At Both 2- And 4- Positions, Or Tautomeric Equivalent (e.g., Hydantoin, Etc.) Patents (Class 514/389)
  • Publication number: 20090306162
    Abstract: A composition for treating fungus infection of turfgrass, such as snow mould infection, comprises a mixture of fungicidally effective amounts of formulae 1 and 2: And in particular mixtures of oprodione and trifloxystrobin. A method for treating snow moulds comprises applying the mixture before the onset of continuous snow cover, in at least one application.
    Type: Application
    Filed: October 19, 2005
    Publication date: December 10, 2009
    Applicant: Bayer CropScience Inc.
    Inventor: Edwin Vandenberg
  • Publication number: 20090306047
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: June 8, 2009
    Publication date: December 10, 2009
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
  • Publication number: 20090298900
    Abstract: Compounds represented by Formula I and II, or pharmaceutically acceptable salts thereof: inhibit bacterial 2-epimerase and are useful anti-infective agents.
    Type: Application
    Filed: May 11, 2009
    Publication date: December 3, 2009
    Inventors: David J. Bearss, Hariprasad Vankayalapati, Yong Xu, Charles Erec Stabbins, Vincent A. Fischetti
  • Patent number: 7612212
    Abstract: The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
    Type: Grant
    Filed: January 25, 2007
    Date of Patent: November 3, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Shaoqing Chen, Nicholas J. S. Huby, Norman Kong, Steven Gregory Mischke, John Anthony Moliterni, Hong Wang, Zhuming Zhang
  • Publication number: 20090257968
    Abstract: The present invention provides an enhanced gelling agent composition comprising a mixture of an anionic surfactant and a coupling agent. The invention also describes compositions in gel form comprising: (a) a solvent selected from the group consisting of polar solvents, non-polar solvents and combinations thereof; and (b) a gelling agent in an amount sufficient to impart gelation to the composition, the gelling agent being a mixture comprising an anionic surfactant and a coupling agent. The gels of the invention may be substantially anhydrous or may optionally contain water as part of the formulation.
    Type: Application
    Filed: May 6, 2009
    Publication date: October 15, 2009
    Inventors: Richard Walton, Edward T. Borish
  • Publication number: 20090258868
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: December 10, 2008
    Publication date: October 15, 2009
    Inventors: Zhaoning Zhu, Brian A. McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
  • Publication number: 20090253763
    Abstract: An ester compound represented by the formula (I): (wherein, R1 represents a C1-C3 alkyl group, a 2-propenyl group or a 2-propynyl group.) has excellent pest controlling activity and is useful as an active ingredient for a pest controlling agent.
    Type: Application
    Filed: August 24, 2007
    Publication date: October 8, 2009
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Jun Ohshita, Toru Uekawa
  • Publication number: 20090239888
    Abstract: Compositions and uses of mGluR5 antagonists for the treatment and inhibition of amyloid precursor protein (APP), A? protein, and APP proteolytic products in Alzheimer's disease, Fragile X Syndrome, autism, and Down's Syndrome are provided. The invention provides methods for diagnosing Fragile X Syndrome via the assessment of A?1-42 levels in blood plasma.
    Type: Application
    Filed: February 12, 2009
    Publication date: September 24, 2009
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: James Malter, Cara Westmark
  • Patent number: 7589057
    Abstract: Biocompatible microparticles include an ophthalmically active alpha-2 adrenergic receptor agonist and a biodegradable polymer. The microparticles include oil-in-water emulsified microparticles which can be used to treat an ocular condition, such as glaucoma.
    Type: Grant
    Filed: March 31, 2006
    Date of Patent: September 15, 2009
    Assignee: Allergan, Inc.
    Inventors: James Chang, Patrick Hughes
  • Publication number: 20090220559
    Abstract: Solid formulations for use in water conditioning of circulating reservoirs, processes of preparing same and methods for water conditioning utilizing same are disclosed. The solid formulations combine a sanitizer with a bath salt and/or an odoriferous substance.
    Type: Application
    Filed: April 25, 2007
    Publication date: September 3, 2009
    Applicant: Bromine Compounds Ltd.
    Inventors: David Feldman, Theodore M. Fishler, Amiram Groweiss, Aharon Weissman, Gideon Shikolsky, Moshe Link
  • Publication number: 20090215846
    Abstract: The invention provides compounds of the formula (I) wherein the variables are as defined in the specification. The compounds of the invention are inhibitors of metalloproteinase MMP-12 and are among other things useful for the treatment of obstructive airway diseases, such as chronic obstructive pulmonary disease (COPD).
    Type: Application
    Filed: December 13, 2006
    Publication date: August 27, 2009
    Applicant: Medivir AB
    Inventors: Hans Wallberg, Ming-Hua Xu, Guo-Qiang Lin, Xin-Sheng Lei, Piaoyang Sun, Kevin Parkes, Tony Johnson, Bertil Samuelsson
  • Patent number: 7579018
    Abstract: Microbiological control is achieved by continuously and inexpensively dosing water in contact with biofilm, or that comes into contact with biofilm, using a highly effective biocide that provides very effective microbiocidal control of planktonic microorganisms and of biofilm species, even where the biofilm infestations have been in existence for long periods of time and thus have encased themselves in a substantial quantity of slimy defensive polysaccharide layers or films. In addition, the biocide used makes possible significant reduction in copper and/or iron surfaces in contact with the water as compared to N,N?-bromochloro- 5,5-dimethyl hydantoin. Still other advantages are made possible by the described technology.
    Type: Grant
    Filed: October 17, 2003
    Date of Patent: August 25, 2009
    Assignee: Albemarle Corporation
    Inventors: Jonathan N. Howarth, Christopher J. Nalepa, Michael J. Sanders, David L. Shelton
  • Publication number: 20090186882
    Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.
    Type: Application
    Filed: January 21, 2009
    Publication date: July 23, 2009
    Inventors: Corey Don Anderson, Andreas P. Termin, Pramod Joshi, Sara S. Hadida Ruah, Daniele Bergeron, Sanghee Yoo
  • Publication number: 20090156586
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.
    Type: Application
    Filed: February 3, 2009
    Publication date: June 18, 2009
    Inventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Bandarpalle B. Shankar, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Razia Rizvi, Lei Chen, De-Yi Yang, Robert Feltz, Seong Heon Kim
  • Publication number: 20090155385
    Abstract: A method for reducing or eliminating Salmonella in reptiles and/or reptile eggs through the use of at least one N,N-dihalo-5,5-dialkylhydantoin in which each of the alkyl groups is independently selected from those containing in the range of from 1 to about 6 carbon atoms.
    Type: Application
    Filed: June 15, 2007
    Publication date: June 18, 2009
    Inventors: Joe D. Sauer, George W. Cook, Jr., Christopher J. Nalepa
  • Publication number: 20090149417
    Abstract: The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions.
    Type: Application
    Filed: October 17, 2008
    Publication date: June 11, 2009
    Inventors: Valeria Ossovskaya, Barry M. Sherman
  • Publication number: 20090149522
    Abstract: The invention concerns a process for producing a preserved customised consumer composition, preferably from a Vending machine, wherein a plurality of ingredient streams are mixed together in predefined relative amounts, characterised in that At least two streams consist of water and preservative only, at least two of which having different concentrations of preservative. The Invention permits the final preservative mix to be independently variable to the formation.
    Type: Application
    Filed: July 28, 2006
    Publication date: June 11, 2009
    Inventors: Geetha Basappa, Maria Teresa Belmar, Ana Martin-Herranz, Iain Sunil Young
  • Publication number: 20090117202
    Abstract: Novel formulations containing a non-oxidative biocide, such as DBNPA, and a source of an in situ produced active biocide, such as a concentrated aqueous solution of an inorganic halide salt, are disclosed. These novel formulations are particularly effective in the treatment of water, and are characterized by high stability, desirable rheological properties and an excellent biocidal activity.
    Type: Application
    Filed: February 25, 2007
    Publication date: May 7, 2009
    Applicant: BROMINE COMPOUNDS LTD.
    Inventors: David Feldman, Michel Adda, Raymond J. Roccon
  • Publication number: 20090111803
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF—or combinations thereof.
    Type: Application
    Filed: December 18, 2008
    Publication date: April 30, 2009
    Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K.C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankat
  • Publication number: 20090105323
    Abstract: In the growing of crops for consumption, a method for the removal of pathogens includes the addition to irrigation water for the crops of an anti-pathogen composition and supplying the anti-pathogen composition to the crops prior to harvest while normal irrigation is effected. The anti-pathogen composition is based on halogens, such as chlorine, bromine and iodine, or mixtures of halogens or halogens combined with other organic radicals including cyanurate, hydantoin, peroxide and chlorine dioxide. BCDMH and TICA are preferred anti-pathogen components of the anti-pathogen composition and may be added to a carrier concentrate and measured and dosed into the irrigation water.
    Type: Application
    Filed: May 18, 2006
    Publication date: April 23, 2009
    Inventor: William Bliss
  • Patent number: 7521465
    Abstract: Novel diphenyl ether derivatives are provided that exhibit activity useful for reducing glucose, cholesterol, and/or triglyceride levels in plasma, and for treatment of obesity, inflammation, immunological diseases, autoimmune diseases, diabetes and disorders associated with insulin resistance.
    Type: Grant
    Filed: March 31, 2005
    Date of Patent: April 21, 2009
    Assignee: Bexel Pharmaceuticals, Inc.
    Inventors: Bishwajit Nag, Abhijeet Nag, Debendranath Dey, Shiv Kumar Agarwal, Partha Neogi, Gaddam Om Reddy, Sangamesh Badiger, Gajendra Singh, Surendra Kumar Pandey, Santhanagopalan Chithra
  • Patent number: 7514462
    Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the following formula I: wherein the hatched segment represents an ? bonds, the solid triangle represents a ? bond, the wavy segments represent ? or ? bond, dashed lines represent a double bond or a single bond, X is selected from the group consisting of hydrogen and halogen radicals, R3 is heteroaryl or a substituted heteroaryl radical, R1 and R2 are independently selected from the group consisting of hydrogen or a lower alkyl radical having up to six carbon atoms, or a lower acyl radical having up to six carbon atoms, R is selected from the group consisting of CO2R4, CONR42, CH2OR4, CONR4SO2R4, P(O)(OR4) and wherein R4 is selected from the group consisting of H, phenyl and lower alkyl having from one to six carbon atoms and n is 0 or an integer of from 1 to 4.
    Type: Grant
    Filed: June 6, 2007
    Date of Patent: April 7, 2009
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
  • Publication number: 20090076045
    Abstract: Compounds of formula I, wherein R1, X1, X2 and A, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
    Type: Application
    Filed: May 30, 2008
    Publication date: March 19, 2009
    Inventors: Joshua Kennedy-Smith, Zachary Kevin Sweeney, Jeffrey Wu
  • Publication number: 20090075986
    Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.
    Type: Application
    Filed: June 9, 2006
    Publication date: March 19, 2009
    Inventors: Daniel L. Flynn, Peter A. Petillo
  • Publication number: 20090012066
    Abstract: The present invention provides methods of treating and/or preventing pathologic cardiac hypertrophy and heart failure comprising administering hydroxamate compounds which are deacetylase inhibitors.
    Type: Application
    Filed: August 9, 2006
    Publication date: January 8, 2009
    Inventors: Seigo Izumo, Suraj Shivappa Shetty
  • Publication number: 20080318987
    Abstract: Methods and compositions for modulating bone formation and mineralization are described.
    Type: Application
    Filed: February 15, 2008
    Publication date: December 25, 2008
    Inventor: Laurie H. GLIMCHER
  • Publication number: 20080306065
    Abstract: Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.
    Type: Application
    Filed: May 6, 2008
    Publication date: December 11, 2008
    Inventors: Anders Eriksson, Matti Lepisto, Michael Lundkvist, Magnus Munck Af Rosenschold, Pavol Zlatoidsky
  • Publication number: 20080262045
    Abstract: Compounds of the formula (I) wherein Z is SO2(N6) or N(R7)SO2 or N(R7)SO2N(R6) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.
    Type: Application
    Filed: May 5, 2008
    Publication date: October 23, 2008
    Inventors: Anders Eriksson, Matti Lepisto, Michael Lundkvist, Magnus Munck Af Rosenschold, Pavol Zlatoidsky
  • Publication number: 20080234204
    Abstract: Provide is a method for evaluating test agents as candidates for treating prostatic diseases, including benign prostatic hyperplasia (BPH) and androgen dependent and androgen independent prostate cancer. The method comprises providing a mouse comprising a human prostate primary xenograft, where the xenograft contains blood vessels that include human endothelial cells, initiating androgen deprivation in the mouse, administering to the mouse a test agent within a period of 1-7 days after initiating the androgen deprivation, and determining a reduction in human epithelial cells in the xenografts and/or a reduction in number of the endothelial cells or blood vessels in the xenograft. Also provided is a method for treating an individual for human prostate cancer or benign prostatic hyperplasia.
    Type: Application
    Filed: January 30, 2008
    Publication date: September 25, 2008
    Inventors: Gary J. Smith, Howard M. Reisner, Danny R. Gray, Wendy Huss
  • Publication number: 20080226618
    Abstract: This invention relates to compounds of the Formula (I), or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.
    Type: Application
    Filed: August 29, 2007
    Publication date: September 18, 2008
    Inventors: Umar Faruk Mansoor, Panduranga Adulla P. Reddy, M. Arshad Siddiqui
  • Publication number: 20080221181
    Abstract: The invention provides compounds of formula (I): wherein E, A, B?, R6, R7, R8, and R9 are defined in the specification which compounds exhibit anticancer activity and are useful for treating cancer.
    Type: Application
    Filed: April 17, 2008
    Publication date: September 11, 2008
    Applicant: Wyeth Holdings Corporation
    Inventors: Arie Zask, Joshua Kaplan, Ayako Yamashita, Chuan S. Niu, Gary Harold Birnberg, Emily Norton, Kinwang Cheung, Ronald Suayan, Vincent Sandanayaka, Philip Ross Hamann, Semiramis Ayral-Kaloustian
  • Patent number: 7381737
    Abstract: A process is provided for preparing spiro-hydantoin compounds of the formula II wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A2 is a linker, G? is a linker; Q is a linker; and R2, R4a, R4c, and Rh are defined in the specification. The process optionally includes the enantiomeric separation of intermediates to allow preparation of enantiomers of the spiro-hydantoin compounds of formula II. Substituted spiro-hydantoin compounds may be prepared from the spiro-hydantoin compounds of formula II. The spiro-hydantoin compound of formula II and the substituted spiro-hydantoin compounds are useful in the treatment of immune or inflammatory diseases. Also, provided are products made by the instant inventive process and crystalline forms (prepared by any process) of the substituted spiro-hydantoin compound, 5-[(5S,9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.
    Type: Grant
    Filed: September 29, 2005
    Date of Patent: June 3, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Albert J. DelMonte, T. G. Murali Dhar, Yu Fan, Jack Z. Gougoutas, Mary F. Malley, Douglas D. McLeod, Robert E. Waltermire, Chenkou Wei
  • Publication number: 20080118553
    Abstract: The subject invention provides a composition comprising a mixture of polypeptides in the form of a tannate salt wherein each polypeptide is a copolymer of the amino acids L-glutamic acid, L-alanine, L-tyrosine and L-Lysine, methods of preparation and uses thereof.
    Type: Application
    Filed: June 12, 2007
    Publication date: May 22, 2008
    Inventors: Anton Frenkel, Arthur A. Komlosh
  • Patent number: 7371397
    Abstract: Microbiological control in aqueous media and/or eradication or reduction of biofilm on a surface in contact with such media is achieved by introducing into the aqueous medium a microbiocidally effective quantity of one or more 1,3-dibromo-5,5-dialkylhydantoins where one of the alkyls is methyl and the other is a C1-4 alkyl, wherein (i) the molar quantity of 1,3-dibromo-5,5-dialkylhydantoin introduced is less than the molar quantity of N,N?-bromochloro-5,5-dimethylhydantoin that would be required to effect the same degree of microbiological control in that medium, (ii) the molar quantity of the 1,3-dibromo-5,5-dialkylhydantoin introduced releases an amount of “free chlorine” that is greater than the amount of “free chlorine” that would be released in that medium by an equimolar quantity of N,N?-bromochloro-5,5-dimethylhydantoin, and (iii) the amount of “free chlorine” released by the quantity of the 1,3-dibromo-5,5-dialkylhydantoin introduced is greater than the amount of “free chlorine” that could be predicte
    Type: Grant
    Filed: October 17, 2003
    Date of Patent: May 13, 2008
    Assignee: Albemarle Corporation
    Inventors: Jonathan N. Howarth, Christopher J. Nalepa, Michael J. Sanders
  • Patent number: 7368465
    Abstract: Compounds of the formula (I) wherein Z is SO2(N6) or N(R7)SO2 or N(R7)SO2N(R6) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.
    Type: Grant
    Filed: March 13, 2002
    Date of Patent: May 6, 2008
    Assignee: AstraZeneca AB
    Inventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
  • Publication number: 20080096923
    Abstract: The present invention relates to a method for treating one or more diabetic microvascular complications in a patient in need of said treatment comprising: (a) diagnosing the severity of at least three different microvascular complications in said patient by calculating a diabetes microvascular complications score with a diabetes microvascular complications scoring tool; and (b) administering to said patient in need thereof a therapeutic amount of a compound selected from the group consisting of ruboxistaurin, enzastaurin, PKC 412, candesartan cilexetil, fidarestat, lidorestat, pyridoxamine and pegaptanib, or a pharmaceutically acceptable salt thereof, and ranibizumab; in an amount that is effective in treating one or more diabetic microvascular complications in said diabetic patient.
    Type: Application
    Filed: July 13, 2005
    Publication date: April 24, 2008
    Inventor: Aniz Girach
  • Patent number: 7358239
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -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 of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; 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, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: April 15, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 7354940
    Abstract: The invention provides compounds of formula (I) in which L, X, Y, Z1, Z2, R1, R2, R3 and G2 have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy. The compounds of the invention are inhibitors of metalloproteinase MMP12 and are among other things useful for the treatment of obstructive airways diseases, such as asthma and chronic obstructive pulmonary disease (COPD).
    Type: Grant
    Filed: August 26, 2003
    Date of Patent: April 8, 2008
    Assignee: AstraZeneca AB
    Inventors: Krister Henriksson, Magnus Munck Af Rosenschöld
  • Patent number: 7354933
    Abstract: The present invention relates to a cyclic urea compound of formula I: as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use, as an inhibitor on a protein kinase. Thus, it is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.
    Type: Grant
    Filed: February 2, 2004
    Date of Patent: April 8, 2008
    Assignee: Aventis Pharma SA
    Inventors: Marcel Patek, Anil Nair, Augustin Hittinger, Conception Nemecek, Daniel Bond, Greg Harlow, Herve Bouchard, Jacques Mauger, Jean-Luc Malleron, Mark Palermo, Fahad Al-Obeidi, Thomas Faitg, Hartmut Strobel, Sven Ruf, Kurt Ritter, Youssef El-Ahmad, Dominique Lesuisse, Didier Bénard
  • Publication number: 20080081052
    Abstract: A method for enhancing solubility of allantoin in an aqueous vehicle using a solubilization enhancer is described. Aqueous compositions containing the solubilized allantoin at a level of 0.5% by weight or higher are able to be obtained by using urea or urea derivatives as the solubilization enhancer. The aqueous topical compositions are suitable for cosmetic, dermatological, and pharmaceutical use.
    Type: Application
    Filed: October 2, 2006
    Publication date: April 3, 2008
    Inventor: Jerry Zhang
  • Publication number: 20080069791
    Abstract: The present invention relates to the use of IL-15 polynucleotides, polypeptides or compounds which bind to an antibody which specifically recognizes the IL-15 polypeptide or which specifically bind to an IL-15 receptor alpha chain for the preparation of a composition for stimulating hair growth or for treating, preventing and/or ameliorating hair loss. Moreover the present invention encompasses a transgenic non-human animal comprising an IL-15 polynucleotide. The present invention also relates to a method for stimulating hair growth in a non-human animal and to methods for manufacturing animal hair. Finally, the present invention relates to a method of treating, preventing and/or ameliorating a subject which suffers from hair loss.
    Type: Application
    Filed: December 7, 2004
    Publication date: March 20, 2008
    Applicant: Universitaetsklinikum Muenster
    Inventor: Stefan Beissert
  • Publication number: 20070197617
    Abstract: The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
    Type: Application
    Filed: January 25, 2007
    Publication date: August 23, 2007
    Inventors: Shaoqing Chen, Nicholas J. S. Huby, Norman Kong, Steven Gregory Mischke, John Anthony Moliterni, Hong Wang, Zhuming Zhang
  • Patent number: 7226940
    Abstract: The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease
    Type: Grant
    Filed: August 24, 2005
    Date of Patent: June 5, 2007
    Assignees: Incyte San Diego, Inc., Ortho McNeil Pharmaceutical Inc.
    Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul, David P. M. Pleynet, Lyle W. Spruce
  • Patent number: 7202251
    Abstract: The present invention is directed to compounds of the formula: that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: March 10, 2004
    Date of Patent: April 10, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Ian M. Bell, Steven N. Gallicchio, Cory R. Theberge, Xu-Fang Zhang, Craig Stump, C. Blair Zartman
  • Patent number: 7202366
    Abstract: Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidinedione compounds, known to lower leptin levels, the present compounds increase leptin levels and have no known liver toxicity. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.
    Type: Grant
    Filed: March 25, 2004
    Date of Patent: April 10, 2007
    Assignee: Theracos, Inc.
    Inventors: Bishwajit Nag, Debendranath Dey, Satyanarayana Medicherla, Partha Neogi
  • Patent number: 7189722
    Abstract: The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: March 10, 2004
    Date of Patent: March 13, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Ian M. Bell, Cory R. Theberge, Xu-Fang Zhang, C. Blair Zartman
  • Patent number: 7179831
    Abstract: 5-[3-(4-benzyloxyphenylthio)-fur-2-yl]-imidazolidin-2,4-dione and analogues useful as inhibitors of macrophage elastase are disclosed.
    Type: Grant
    Filed: August 17, 2005
    Date of Patent: February 20, 2007
    Assignee: Quest Pharmaceutical Services
    Inventor: Fude Yang
  • Patent number: 7176223
    Abstract: Process for the synthesis of 5-(3-pyridylmethyl)imidazolidine-2,4-dione, according to which 5-(3-pyridylmethylene)imidazolidine-2,4-dione is subjected to a hydrogenation reaction.
    Type: Grant
    Filed: October 24, 2005
    Date of Patent: February 13, 2007
    Assignee: Solvay S.A.
    Inventor: Roland Callens
  • Patent number: 7173057
    Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
    Type: Grant
    Filed: February 24, 2005
    Date of Patent: February 6, 2007
    Assignee: Schering Corporation
    Inventors: Kevin X. Chen, F. George Njoroge, Mousumi Sannigrahi, Latha G. Nair, Weiying Yang, Bancha Vibulbhan, Srikanth Venkatraman, Ashok Arasappan, Stephane L. Bogen, Frank Bennett, Viyyoor M. Girijavallabhan
  • Patent number: 7144583
    Abstract: A pesticidal composition comprising an oxadiazine compound given by formula (A): and an ester compound given by formula (B): as active ingredients, wherein the weight ratio of the oxadiazine compound given by formula (A) to the ester compound given by formula (B) is within the range of 50:1 to 1:10, has an excellent efficacy for controlling pests.
    Type: Grant
    Filed: February 3, 2004
    Date of Patent: December 5, 2006
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Satoshi Sembo