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: 20120238609
    Abstract: Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for treating COPD.
    Type: Application
    Filed: December 23, 2011
    Publication date: September 20, 2012
    Applicant: The Board of Regents of The University of Texas System
    Inventors: Satish K. Srivastava, Kota V. Ramana, Umesh Yadav
  • Publication number: 20120219609
    Abstract: A moisture-permeable glove or other garment protects against user contamination and cross-contamination by providing both rapid and persistent sterilization. Exposure to halogen of inherent NH groups and/or attached hydantoin can form a persistent outer halamine sterilization layer. A second inner halamine layer intercepts any pathogens that penetrate the outer surface. The garment can be single layer, or can include a detachable inner liner. Embodiments are compatible with rapid decontamination using an alcohol-based agent. Some embodiments provide a 180 second 3-log kill rate for at least S. aureus ATCC and E. coli. Embodiments include a moistening agent to activate the halamine. An anti-cut/puncture layer and/or a pathogen barrier layer can also be included. The protective layer can include contiguous layers of soft and hard metal flexed to improve flexibility and Moisture Vapor Transport Rate (MVTR). The pathogen barrier can include urethane and/or CNT fibers. The garment MVTR can be greater than 0.
    Type: Application
    Filed: May 10, 2012
    Publication date: August 30, 2012
    Applicant: WARWICK MILLS, INC.
    Inventor: Charles A. Howland
  • Publication number: 20120196864
    Abstract: A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has a superior activity as an estrogen-related receptor-? modulator, and is useful as a prophylactic or therapeutic agent for cancer.
    Type: Application
    Filed: August 4, 2010
    Publication date: August 2, 2012
    Inventors: Atsushi Hasuoka, Koji Ono, Masanori Kawasaki
  • Publication number: 20120190717
    Abstract: Provided are compositions comprising beta-alanylhistidine peptides and/or beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.
    Type: Application
    Filed: January 23, 2012
    Publication date: July 26, 2012
    Applicant: Natural Alternatives Internatioal, Inc.
    Inventors: Roger Harris, Mark Dunnett
  • Patent number: 8227473
    Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: July 24, 2012
    Assignee: Lixte Biotechnology, Inc.
    Inventors: John S. Kovach, Francis Johnson
  • Publication number: 20120183494
    Abstract: Novel acrylamide and methacrylamide hydantoin monomers which can be reacted with other acrylamide, methacrylamide, acrylate, and methacrylate monomers to form copolymers, which upon halogenation, provide oxidative coatings which are biocidal for use with various materials including, but not limited to, textiles, filters, and latex paints.
    Type: Application
    Filed: October 11, 2011
    Publication date: July 19, 2012
    Applicant: AUBURN UNIVERSITY
    Inventors: Shelby D. Worley, Royall M. Broughton, Hasan B. Kocer, Idris Cerkez
  • Publication number: 20120177745
    Abstract: The application describes synergistic microbicidal compositions comprising: 2,2-dibromomalonamide and an oxidizing biocide selected from the group consisting of: monochloramine, bromochlorodimethylhydantoin, hypobromite ion or hypobromous acid, hydrogen peroxide, dichloroisocyanurate, trichloroisocyanurate and chlorine dioxide and a method for controlling microorganism growth in an aqueous or water-containing system.
    Type: Application
    Filed: September 27, 2010
    Publication date: July 12, 2012
    Inventors: Freddie L. Singleton, Bei Yin, Janardhanan S. Rajan
  • Publication number: 20120177725
    Abstract: The present invention relates to liposomal pharmaceutical preparations which include active agents such as antiseptic agents, wound-healing agents, or combinations thereof, useful in the treatment of external wounds. The active agents are encapsulated in liposomes, and the liposomes are incorporated in pharmaceutical preparations such as liquids, ointments, gels, lotions, or creams capable of delivering the active agents to external wound sites. The invention further relates to methods of preparation of the liposomes and the pharmaceutical preparations, and to methods of treatment of external wounds and ophthalmic infections.
    Type: Application
    Filed: March 9, 2012
    Publication date: July 12, 2012
    Inventors: Dieter Ruckert, Hermann Gumbel, Wolfgang Fleischer, Karen Reimer, Horst Winkler
  • Patent number: 8217068
    Abstract: The present invention is related to a new series of chemical compounds, namely 3-benzyl-imidazolidine-2,4-dione substituted in the position 2 and/or 6 of benzyl ring by halogens as presented to the molecule named LPSF-PT-31, GIRSUPAN and its therapeutic use as drug with analgesic, sedative and adjuvant of anesthetics activities. The invention is also related to a process for production of said compounds as well as pharmaceutical compositions comprising them.
    Type: Grant
    Filed: May 5, 2008
    Date of Patent: July 10, 2012
    Assignees: Universidade Federal de Pernambuco—UFPE, Universidade Federal do Rio de Janeiro—UFRJ
    Inventors: Ivan Da Rocha Pitta, Maria Do Carmo Alves De Lima, Teresinha Gonçalves da Silva, Gisele Zapata Sudo, Suely Lins Galdino, Roberto Takashi Sudo
  • Publication number: 20120171127
    Abstract: Certain surfactants suitable for use alone to dissolve a water-insoluble component in compositions is described for providing VOC-free compressed gas aerosol compositions. The compositions include water-insoluble component(s), a surfactant and water. The water-insoluble component(s) can be active agent(s), such as fragrance(s) and/or an insecticide(s). The surfactant is present as a single surfactant which, in the absence of a solvent, dissolves or disperses the water-insoluble component(s) and provides a homogenous blend in water which provides a stable compressed gas emulsion.
    Type: Application
    Filed: March 12, 2012
    Publication date: July 5, 2012
    Applicant: S.C. JOHNSON & SON, INC.
    Inventors: Richard S. VALPEY, III, Paul A. CLARK, Jessica A. HEISER
  • Publication number: 20120148651
    Abstract: According to one embodiment, a coagulant comprising calcium nitrate and an antimicrobial agent is disclosed. The coagulant may be used in the molding process to releasably bond the substrate material to the mold and to bond to the antimicrobial to the substrate material.
    Type: Application
    Filed: December 10, 2010
    Publication date: June 14, 2012
    Applicant: MEDLINE INDUSTRIES INC.
    Inventors: Samuel T. Amdur, Min Yao
  • Publication number: 20120149702
    Abstract: The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis.
    Type: Application
    Filed: February 21, 2012
    Publication date: June 14, 2012
    Applicants: The Brigham and Women's Hospital, Inc., President and Fellows of Harvard College
    Inventors: Gregory D. Cuny, Prakash Jagtap, Junying Yuan, Alexei Degterev
  • Patent number: 8193227
    Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Grant
    Filed: December 10, 2004
    Date of Patent: June 5, 2012
    Assignee: Abbott Laboratories
    Inventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
  • Publication number: 20120136034
    Abstract: Compounds of formula I and their metabolites are potent mediators of an inflammatory response: (I) where a, b, c, d, e, f, V, W, X, Y, Ra, Ra?, Rb, Rb?, Rc, and Rc? are defined herein. In particular, the compounds of the invention are candidate therapeutics for treating inflammatory conditions.
    Type: Application
    Filed: August 2, 2010
    Publication date: May 31, 2012
    Applicant: University of Pittsburgh -Of the Commonwealth Syst
    Inventors: Bruce A. Freeman, Francisco J. Schopfer
  • Patent number: 8188130
    Abstract: The present invention relates to methods of either treating or preventing cancer and novel compositions relevant to that treatment and prevention. More particularly, this invention relates to compounds which share features with (Z)-5-(4-hydroxybenzylidene)imidazolidine-2,4-dione and (Z)-5-(4-S-ethylbenzylidene)imidazolidine-2,4-dione and anti-cancer uses for those compounds. Embodiments of the present invention include methods that have anti-cancer effects including anti-metastatic, anti-growth, and anti-invasive activities.
    Type: Grant
    Filed: May 15, 2008
    Date of Patent: May 29, 2012
    Assignee: University of Louisiana at Monroe
    Inventors: Girish Shah, Khalid El Sayed
  • Publication number: 20120121728
    Abstract: The invention provides a process of removing or preventing biofouling, particularly on surfaces of industrial and agricultural equipment in contact with aqueous liquids. The process employs an antifouling composition of stabilized active halogen having a low pH.
    Type: Application
    Filed: June 7, 2010
    Publication date: May 17, 2012
    Applicant: BROMINE COMPOUNDS LTD.
    Inventors: Shlomo Antebi, Chen Zolkov, David Feldman
  • Publication number: 20120115849
    Abstract: This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.
    Type: Application
    Filed: November 7, 2011
    Publication date: May 10, 2012
    Inventors: Gregory A. Demopulos, George A. Gaitanaris
  • Publication number: 20120115895
    Abstract: The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases. The compounds according to Formula (I) are suitable as modulators of CRTH2. The invention provides Spiro derivatives according to Formula (I) and related formulae that are useful in the treatment and/or prevention of diseases selected from allergic diseases such as allergic asthma, allergic rhinitis, allergic conjunctivitis, and inflammatory dermatoses such as atopic dermatitis, contact hypersensitivity, allergic contact dermatitis, chronic urticaria/chronic idiopathic/autoimmune urticaria, drag-induced exanthems (e.g., toxic epidermal necrolysis or Lyell's syndrome/Stevens-Johnson syndrome/drug hypersensitivity syndrome), photodermatosis or polymorphous light emption (e.g.
    Type: Application
    Filed: July 14, 2010
    Publication date: May 10, 2012
    Applicant: Merck Serono S.A.
    Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Tania Grippi-Vallotton
  • Patent number: 8168666
    Abstract: There is provided a novel LXR? agonist useful as a preventative and/or therapeutic agent for arteriosclerosis; arteriosclerosis such as those resulting from diabetes; hyperlipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases caused by inflammatory cytokines, skin diseases such as allergic skin diseases, diabetes or Alzheimer's disease. The agonist is a carbinol derivative represented by the following general formula (1) or salt thereof, or their solvate.
    Type: Grant
    Filed: November 29, 2007
    Date of Patent: May 1, 2012
    Assignee: Kowa Company, Ltd.
    Inventors: Takayuki Matsuda, Ayumu Okuda, Minoru Koura, Yuki Yamaguchi, Sayaka Kurobuchi, Yuuichirou Watanabe, Kimiyuki Shibuya
  • Patent number: 8168667
    Abstract: Compounds of formula (I): wherein X is O or S, R1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R2 is H, alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R3 and R4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R3 and R4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R5 is H, halogen, trifluoromethyl, —CN, or —NO2; not all of R3, R4, and R5 being H, R6 and R9 are H, halogen, OH; alkyl, hydroxyalkyl, alkoxyl, thioalkyl, haloalkyl, alkenyl, or alkynyl; R7 and R8 are H, halogen, OH, SH; alkoxyl or alkylthio optionally substituted by OH and/or halogen; one of R7 and R8 not being H or halogen; or one of R7 and R8 is a pharmaceutically acceptable ester or thioester grouping, or R6 is C1-3-alkyl or, together with either R1 or R2, represents C1-3 alkylene or alkenylene linking group, optionally substituted by methyl, trifluoromethyl, OH, or
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: May 1, 2012
    Assignee: Galapagos NV
    Inventors: Francois Nique, Catherine Jagerschmidt, Philippe Clement-Lacroix
  • Patent number: 8153634
    Abstract: [Object] To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: April 10, 2012
    Assignee: Kowa Company, Ltd.
    Inventors: Yuki Yamaguchi, Minoru Koura, Sayaka Kurobuchi, Takayuki Matsuda, Ayumu Okuda, Hisashi Sumida, Yuichiro Watanabe, Takashi Enomoto, Kimiyuki Shibuya
  • Patent number: 8153673
    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: January 26, 2010
    Date of Patent: April 10, 2012
    Assignee: AstraZeneca AB
    Inventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
  • Patent number: 8148390
    Abstract: The present invention is directed to compounds of Formula I: (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and 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 7, 2008
    Date of Patent: April 3, 2012
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Craig A. Stump, Ian M. Bell, Harold G. Selnick
  • Publication number: 20120064129
    Abstract: A method of treatment for epilepsy and other disease states is described, which comprises the delivery of gabapentin in a gastric retained dosage form.
    Type: Application
    Filed: November 21, 2011
    Publication date: March 15, 2012
    Applicant: DEPOMED, INC.
    Inventors: Bret Berner, Sui Yuen Eddie Hou, Gloria M. Gusler
  • Publication number: 20120065195
    Abstract: The invention provides novel spirotetrahydronaphthalene compounds of Formula ? that inhibit ?-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.
    Type: Application
    Filed: March 31, 2011
    Publication date: March 15, 2012
    Inventors: Christopher T. Clark, Adam Cook, Indrani W. Gunawardana, Kevin W. Hunt, Nicholas C. Kallan, Michael Siu, Allen A. Thomas, Matthew Volgraf
  • Publication number: 20120045500
    Abstract: Compounds of general formula (I): and cosmetic and pharmaceutical compositions including such a compound are described.
    Type: Application
    Filed: February 26, 2010
    Publication date: February 23, 2012
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Cédric Poinsard, Thibaud Portal, Jean-Claude Pascal
  • Patent number: 8110225
    Abstract: Provided are low-volume, safe for injection formulations of dantrolene yielding significant advantages over the currently approved and marketed dantrolene for malignant hyperthermia (MH) threatening anesthetic crisis. Once dantrolene can be made immediately available to patients triggered of MH, the anesthesiologist will be able to focus exclusively on the management of the patient's physiologic status in this complex and evolving crisis, not on the laborious and time consuming reconstitution process of the rescue agent. The low volume, safe for injection formulations of dantrolene have significant advantages over currently used approaches to the prevention and treatment of pumphead, and other neurological, cognitive and motor dysfunction incident to iatrogenically or trauma induced situations of altered blood flow, including those incurred during surgical procedures involving CPB or related procedures, as well as those incurred during non-normothermic episodes caused iatrogenically or by disease.
    Type: Grant
    Filed: March 4, 2010
    Date of Patent: February 7, 2012
    Assignee: Lyotropic Therapeutics, Inc.
    Inventors: David Anderson, Benjamin G. Cameransi, Jr., Vincent M. Conklin
  • Publication number: 20120021017
    Abstract: Compounds of general Formula (I), and cosmetic and pharmaceutical compositions including such a compound are described.
    Type: Application
    Filed: February 26, 2010
    Publication date: January 26, 2012
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Cédric Poinsard, Thibaud Portal
  • Publication number: 20120021016
    Abstract: Compounds of general Formula (I), and cosmetic and pharmaceutical compositions containing such a compound are described.
    Type: Application
    Filed: February 26, 2010
    Publication date: January 26, 2012
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventor: Cédric Poinsard
  • Publication number: 20120015926
    Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt 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: November 9, 2009
    Publication date: January 19, 2012
    Inventors: Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Michael K.C. Wong, Lei Chen, Guowei Zhou, Razia K. Rizvi, Robert Feltz, Aneta Maria Kosinski, De-Yi Yang, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristen E. Rosner, M. Arshad Siddiqui, Liping Yang
  • Publication number: 20120015994
    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: August 31, 2011
    Publication date: January 19, 2012
    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: 8097640
    Abstract: A prophylactic or therapeutic agent for diabetic maculopathy, which can be administered for a long time and exhibits efficacy in a mechanism different from that of existing medicines. The invention relates to a prophylactic or therapeutic agent for diabetic maculopathy, comprising, as an active ingredient, a compound represented by the general formula: wherein X represents a halogen or a hydrogen atom, R1 and R2 concurrently or differently represent a hydrogen atom or an optionally substituted C1 to C6 alkyl group, or R1 and R2, together with a nitrogen atom bound thereto and optionally another nitrogen atom or an oxygen atom, are combined to form a 5- to 6-membered heterocycle. Preferably, the compound is (2S,4S)-6-fluoro -2?,5?-dioxospiro chroman-4,4?-imidazolidine]-2-carboxamide. The invention also provides a model animal with diabetic maculopathy produced by subjecting a diabetic animal to intraocular ischemia/reperfusion to express edema in a retinal visual cell layer or in a macula lutea.
    Type: Grant
    Filed: July 23, 2010
    Date of Patent: January 17, 2012
    Assignee: Sanwa Kagaku Kenkyusho Co., Ltd.
    Inventors: Noriaki Kato, Hiroshi Nagano, Kaori Taniko, Takahito Jomori
  • Publication number: 20120010181
    Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (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: November 9, 2009
    Publication date: January 12, 2012
    Inventors: Joseph A. Kozlowski, Wensheng Yu, Michael K.C. Wong, Seong Heon Kim, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, De-Yi Yang, Robert Feltz, Aneta Maria Kosinski, Guowei Zhou, Razia K. Rizvi, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristen E. Rosner, M. Arshad Siddiqui, Liping Yang
  • Publication number: 20110318308
    Abstract: A PGD(2) receptor (DP) deficiency enhances tumor progression accompanied by abnormal vascular expansion. In tumors, angiogenic endothelial cells highly express DP receptor, and its deficiency accelerates vascular leakage and angiogenesis. Administration of a synthetic DP agonist, BW245C, markedly suppresses tumor growth as well as tumor hyperpermeability in WT mice, but not in DP-deficient mice. In a corneal angiogenesis assay and a modified Miles assay, host DP deficiency potentiates angiogenesis and vascular hyperpermeability under COX-2-active situation, whereas exogenous administration of BW245C strongly inhibits both angiogenic properties in WT mice. In an in vitro assay, BW245C does not affect endothelial migration and tube formation, processes that are necessary for angiogenesis; however, it strongly improves endothelial barrier function via an increase in intracellular cAMP production.
    Type: Application
    Filed: June 24, 2011
    Publication date: December 29, 2011
    Applicant: WINTHROP-UNIVERSITY HOSPITAL
    Inventor: Louis RAGOLIA
  • Publication number: 20110306601
    Abstract: Antagonists of group 1 metabotropic glutamate receptors (mGluR) potentiate the effect of positive AMPA receptor modulators on neurotrophin expression, such as brain-derived neurotrophic factor (BDNF). The findings described herein suggest a combinatorial approach for drug therapies, using both positive AMPA receptor modulators and mGluR antagonists, to enhance brain neurotrophism.
    Type: Application
    Filed: August 19, 2011
    Publication date: December 15, 2011
    Applicant: The Regents of the University of California
    Inventors: Julie C. Lauterborn, Christine M. Gall, Gary Lynch
  • Publication number: 20110288054
    Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester 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: September 22, 2009
    Publication date: November 24, 2011
    Applicant: Schering Corporation
    Inventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K.C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • Publication number: 20110288077
    Abstract: This invention relates to compounds of the Formula (I)-(IX):, as defined herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? combinations thereof.
    Type: Application
    Filed: September 22, 2009
    Publication date: November 24, 2011
    Applicant: SCHERING CORPORATION
    Inventors: Michael K.C. Wong, Wensheng Yu, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Joseph A. Kozlowski, Seong Heon Kim, Guowei Zhou, De-Yi Yang, Razia K. Rizvi, Lei Chen, Aneta Maria Kosinski, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • Publication number: 20110288083
    Abstract: The present invention relates to a method of identifying compounds useful in inhibiting protein kinase-like endoplasmic reticulum protein kinase (PERK). The method comprises providing a first model comprising PERK active domains, where the said active domains are selected from the group consisting of the peptide spanning from amino acid residue Asp144 to amino acid residue Ser191 of SEQ ID NO: 1 and a peptide comprising the amino acid residue at position 7 of SEQ ID NO: 1, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying the compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for inhibiting PERK.
    Type: Application
    Filed: May 19, 2011
    Publication date: November 24, 2011
    Applicant: NEW YORK UNIVERSITY
    Inventors: Timothy CARDOZO, Hong WANG, David Ron
  • Patent number: 8063085
    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: December 10, 2008
    Date of Patent: November 22, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Shaoqing Chen, Nicholas J. S. Huby, Norman Kong, John Anthony Moliterni, Omar Jose Morales
  • Publication number: 20110269763
    Abstract: Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis: wherein A represents a carboxyl group —COOH, or a carboxyl bioisostere; A1 is hydrogen or methyl; ring Ar1 is an optionally substituted phenyl ring or 5- or 6-membered monocyclic heteroaryl ring, in which AA1CHO— and L2 are linked to adjacent ring atoms; rings Ar2, Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; t is 0 or 1; L2 and L3 are linker radicals as defined in the description.
    Type: Application
    Filed: June 2, 2011
    Publication date: November 3, 2011
    Applicant: 7TM Pharma A/S
    Inventors: Trond Ulven, Thomas Frimurer, Øystein Rist, Evi Kostenis, Thomas Högberg, Jean-Marie Receveur, Marie Grimstrup
  • Publication number: 20110262510
    Abstract: This invention provides a process for the N-halogenation of at least one 5-hydrocarbyl hydantoin and/or at least one 5,5-dihydrocarbyl hydantoin. The process comprises concurrently feeding into a reaction zone (i) water, inorganic base, and 5,5-dimethylhydantoin, these being fed separately and/or in any combination(s), (ii) a separate feed of a brominating agent, and (iii) a separate feed of a chlorinating agent, in proportions such that during all or substantially all of the time the concurrent feeding is occurring halogenation of the 5-hydrocarbyl hydantoin and/or 5,5-dihydrocarbyl hydantoin occurs and resultant halogenated product precipitates in the liquid phase of an aqueous reaction mixture, and in which the pH of the liquid phase is continuously or substantially continuously maintained in the range of about 2.0 to about 8.0 during all or substantially all of the time the concurrent feeding is occurring.
    Type: Application
    Filed: July 6, 2011
    Publication date: October 27, 2011
    Applicant: Albemarle Corporation
    Inventor: Hassan Y. Elnagar
  • Patent number: 8044082
    Abstract: Novel N-phenylacetamide compounds of formula (I): and cosmetic and pharmaceutical compositions containing same are useful for treating disorders of the sebaceous gland, e.g., acne, or have cosmetic applications.
    Type: Grant
    Filed: March 5, 2010
    Date of Patent: October 25, 2011
    Assignee: Galderma Research & Development
    Inventors: Thibaud Portal, Laurence Dumais, Jérôme Aubert, Laurent Lamy
  • Patent number: 8039499
    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: Grant
    Filed: August 24, 2007
    Date of Patent: October 18, 2011
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Jun Ohshita, Toru Uekawa
  • Patent number: 8022092
    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: Grant
    Filed: December 13, 2006
    Date of Patent: September 20, 2011
    Assignee: Medivir AB
    Inventors: Hans Wallberg, Ming-Hua Xu, Guo-Qiang Lin, Xin-Sheng Lei, Piaoyang Sun, Kevin Parkes, Tony Johnson, Bertil Samuelsson
  • Publication number: 20110212994
    Abstract: Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided.
    Type: Application
    Filed: June 28, 2010
    Publication date: September 1, 2011
    Inventors: BRIAN CLEM, SUCHETA TELANG, JOHN TRENT, JASON CHESNEY, POORAN CHAND, GILLES TAPOLSKY
  • Publication number: 20110190329
    Abstract: The present invention is directed to novel non-amidic linkers with branched termini derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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: Application
    Filed: August 11, 2009
    Publication date: August 4, 2011
    Inventors: Michael R. Wood, June J. Kim, Harold G. Selnick, Shawn J. Stachel
  • Patent number: 7985413
    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: March 5, 2009
    Date of Patent: July 26, 2011
    Assignee: Albemarle Corporation
    Inventors: Jonathan N. Howarth, Christopher J. Nalepa, Michael J. Sanders, David L. Shelton
  • Publication number: 20110165118
    Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: November 13, 2008
    Publication date: July 7, 2011
    Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
  • Patent number: 7973067
    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: Grant
    Filed: December 10, 2008
    Date of Patent: July 5, 2011
    Assignee: Schering Corporation
    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 D. Mazzola, Jr., John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X. H. Le, Kurt W. Saionz, Suresh D. Babu, Rachel C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
  • Publication number: 20110144173
    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 iprodione 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: February 10, 2011
    Publication date: June 16, 2011
    Applicant: BAYER CROPSCIENCE INC.
    Inventor: Edwin VANDENBERG