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)
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Publication number: 20120238609Abstract: Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for treating COPD.Type: ApplicationFiled: December 23, 2011Publication date: September 20, 2012Applicant: The Board of Regents of The University of Texas SystemInventors: Satish K. Srivastava, Kota V. Ramana, Umesh Yadav
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Publication number: 20120219609Abstract: 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: ApplicationFiled: May 10, 2012Publication date: August 30, 2012Applicant: WARWICK MILLS, INC.Inventor: Charles A. Howland
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Publication number: 20120196864Abstract: 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: ApplicationFiled: August 4, 2010Publication date: August 2, 2012Inventors: Atsushi Hasuoka, Koji Ono, Masanori Kawasaki
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Publication number: 20120190717Abstract: 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: ApplicationFiled: January 23, 2012Publication date: July 26, 2012Applicant: Natural Alternatives Internatioal, Inc.Inventors: Roger Harris, Mark Dunnett
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Patent number: 8227473Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.Type: GrantFiled: July 17, 2009Date of Patent: July 24, 2012Assignee: Lixte Biotechnology, Inc.Inventors: John S. Kovach, Francis Johnson
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Publication number: 20120183494Abstract: 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: ApplicationFiled: October 11, 2011Publication date: July 19, 2012Applicant: AUBURN UNIVERSITYInventors: Shelby D. Worley, Royall M. Broughton, Hasan B. Kocer, Idris Cerkez
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Publication number: 20120177745Abstract: 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: ApplicationFiled: September 27, 2010Publication date: July 12, 2012Inventors: Freddie L. Singleton, Bei Yin, Janardhanan S. Rajan
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Publication number: 20120177725Abstract: 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: ApplicationFiled: March 9, 2012Publication date: July 12, 2012Inventors: Dieter Ruckert, Hermann Gumbel, Wolfgang Fleischer, Karen Reimer, Horst Winkler
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Patent number: 8217068Abstract: 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: GrantFiled: May 5, 2008Date of Patent: July 10, 2012Assignees: Universidade Federal de Pernambuco—UFPE, Universidade Federal do Rio de Janeiro—UFRJInventors: Ivan Da Rocha Pitta, Maria Do Carmo Alves De Lima, Teresinha Gonçalves da Silva, Gisele Zapata Sudo, Suely Lins Galdino, Roberto Takashi Sudo
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Publication number: 20120171127Abstract: 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: ApplicationFiled: March 12, 2012Publication date: July 5, 2012Applicant: S.C. JOHNSON & SON, INC.Inventors: Richard S. VALPEY, III, Paul A. CLARK, Jessica A. HEISER
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Publication number: 20120148651Abstract: 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: ApplicationFiled: December 10, 2010Publication date: June 14, 2012Applicant: MEDLINE INDUSTRIES INC.Inventors: Samuel T. Amdur, Min Yao
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Publication number: 20120149702Abstract: 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: ApplicationFiled: February 21, 2012Publication date: June 14, 2012Applicants: The Brigham and Women's Hospital, Inc., President and Fellows of Harvard CollegeInventors: Gregory D. Cuny, Prakash Jagtap, Junying Yuan, Alexei Degterev
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Patent number: 8193227Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: December 10, 2004Date of Patent: June 5, 2012Assignee: Abbott LaboratoriesInventors: 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
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Publication number: 20120136034Abstract: 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: ApplicationFiled: August 2, 2010Publication date: May 31, 2012Applicant: University of Pittsburgh -Of the Commonwealth SystInventors: Bruce A. Freeman, Francisco J. Schopfer
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Patent number: 8188130Abstract: 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: GrantFiled: May 15, 2008Date of Patent: May 29, 2012Assignee: University of Louisiana at MonroeInventors: Girish Shah, Khalid El Sayed
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Publication number: 20120121728Abstract: 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: ApplicationFiled: June 7, 2010Publication date: May 17, 2012Applicant: BROMINE COMPOUNDS LTD.Inventors: Shlomo Antebi, Chen Zolkov, David Feldman
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Publication number: 20120115849Abstract: 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: ApplicationFiled: November 7, 2011Publication date: May 10, 2012Inventors: Gregory A. Demopulos, George A. Gaitanaris
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Publication number: 20120115895Abstract: 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: ApplicationFiled: July 14, 2010Publication date: May 10, 2012Applicant: Merck Serono S.A.Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Tania Grippi-Vallotton
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Patent number: 8168666Abstract: 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: GrantFiled: November 29, 2007Date of Patent: May 1, 2012Assignee: Kowa Company, Ltd.Inventors: Takayuki Matsuda, Ayumu Okuda, Minoru Koura, Yuki Yamaguchi, Sayaka Kurobuchi, Yuuichirou Watanabe, Kimiyuki Shibuya
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Patent number: 8168667Abstract: 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, orType: GrantFiled: March 31, 2010Date of Patent: May 1, 2012Assignee: Galapagos NVInventors: Francois Nique, Catherine Jagerschmidt, Philippe Clement-Lacroix
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Patent number: 8153634Abstract: [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: GrantFiled: May 29, 2009Date of Patent: April 10, 2012Assignee: Kowa Company, Ltd.Inventors: Yuki Yamaguchi, Minoru Koura, Sayaka Kurobuchi, Takayuki Matsuda, Ayumu Okuda, Hisashi Sumida, Yuichiro Watanabe, Takashi Enomoto, Kimiyuki Shibuya
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Patent number: 8153673Abstract: 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: GrantFiled: January 26, 2010Date of Patent: April 10, 2012Assignee: AstraZeneca ABInventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
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Patent number: 8148390Abstract: 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: GrantFiled: March 7, 2008Date of Patent: April 3, 2012Assignee: Merck, Sharp & Dohme, Corp.Inventors: Craig A. Stump, Ian M. Bell, Harold G. Selnick
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Publication number: 20120064129Abstract: 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: ApplicationFiled: November 21, 2011Publication date: March 15, 2012Applicant: DEPOMED, INC.Inventors: Bret Berner, Sui Yuen Eddie Hou, Gloria M. Gusler
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Publication number: 20120065195Abstract: 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: ApplicationFiled: March 31, 2011Publication date: March 15, 2012Inventors: Christopher T. Clark, Adam Cook, Indrani W. Gunawardana, Kevin W. Hunt, Nicholas C. Kallan, Michael Siu, Allen A. Thomas, Matthew Volgraf
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Publication number: 20120045500Abstract: Compounds of general formula (I): and cosmetic and pharmaceutical compositions including such a compound are described.Type: ApplicationFiled: February 26, 2010Publication date: February 23, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Cédric Poinsard, Thibaud Portal, Jean-Claude Pascal
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Patent number: 8110225Abstract: 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: GrantFiled: March 4, 2010Date of Patent: February 7, 2012Assignee: Lyotropic Therapeutics, Inc.Inventors: David Anderson, Benjamin G. Cameransi, Jr., Vincent M. Conklin
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Publication number: 20120021017Abstract: Compounds of general Formula (I), and cosmetic and pharmaceutical compositions including such a compound are described.Type: ApplicationFiled: February 26, 2010Publication date: January 26, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Cédric Poinsard, Thibaud Portal
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Publication number: 20120021016Abstract: Compounds of general Formula (I), and cosmetic and pharmaceutical compositions containing such a compound are described.Type: ApplicationFiled: February 26, 2010Publication date: January 26, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventor: Cédric Poinsard
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Publication number: 20120015926Abstract: 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: ApplicationFiled: November 9, 2009Publication date: January 19, 2012Inventors: 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
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Publication number: 20120015994Abstract: 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: ApplicationFiled: August 31, 2011Publication date: January 19, 2012Applicant: Medivir ABInventors: Hans WALLBERG, Ming-Hua Xu, Guo-Qiang Lin, Xin-Sheng Lei, Piaoyang Sun, Kevin Parkes, Tony Johnson, Bertil Samuelsson
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Patent number: 8097640Abstract: 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: GrantFiled: July 23, 2010Date of Patent: January 17, 2012Assignee: Sanwa Kagaku Kenkyusho Co., Ltd.Inventors: Noriaki Kato, Hiroshi Nagano, Kaori Taniko, Takahito Jomori
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Publication number: 20120010181Abstract: 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: ApplicationFiled: November 9, 2009Publication date: January 12, 2012Inventors: 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
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Publication number: 20110318308Abstract: 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: ApplicationFiled: June 24, 2011Publication date: December 29, 2011Applicant: WINTHROP-UNIVERSITY HOSPITALInventor: Louis RAGOLIA
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Publication number: 20110306601Abstract: 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: ApplicationFiled: August 19, 2011Publication date: December 15, 2011Applicant: The Regents of the University of CaliforniaInventors: Julie C. Lauterborn, Christine M. Gall, Gary Lynch
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Publication number: 20110288054Abstract: 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: ApplicationFiled: September 22, 2009Publication date: November 24, 2011Applicant: Schering CorporationInventors: 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
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Publication number: 20110288077Abstract: 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: ApplicationFiled: September 22, 2009Publication date: November 24, 2011Applicant: SCHERING CORPORATIONInventors: 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
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Publication number: 20110288083Abstract: 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: ApplicationFiled: May 19, 2011Publication date: November 24, 2011Applicant: NEW YORK UNIVERSITYInventors: Timothy CARDOZO, Hong WANG, David Ron
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Patent number: 8063085Abstract: 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: GrantFiled: December 10, 2008Date of Patent: November 22, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Shaoqing Chen, Nicholas J. S. Huby, Norman Kong, John Anthony Moliterni, Omar Jose Morales
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Publication number: 20110269763Abstract: 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: ApplicationFiled: June 2, 2011Publication date: November 3, 2011Applicant: 7TM Pharma A/SInventors: Trond Ulven, Thomas Frimurer, Øystein Rist, Evi Kostenis, Thomas Högberg, Jean-Marie Receveur, Marie Grimstrup
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Publication number: 20110262510Abstract: 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: ApplicationFiled: July 6, 2011Publication date: October 27, 2011Applicant: Albemarle CorporationInventor: Hassan Y. Elnagar
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Patent number: 8044082Abstract: 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: GrantFiled: March 5, 2010Date of Patent: October 25, 2011Assignee: Galderma Research & DevelopmentInventors: Thibaud Portal, Laurence Dumais, Jérôme Aubert, Laurent Lamy
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Patent number: 8039499Abstract: 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: GrantFiled: August 24, 2007Date of Patent: October 18, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Jun Ohshita, Toru Uekawa
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Patent number: 8022092Abstract: 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: GrantFiled: December 13, 2006Date of Patent: September 20, 2011Assignee: Medivir ABInventors: Hans Wallberg, Ming-Hua Xu, Guo-Qiang Lin, Xin-Sheng Lei, Piaoyang Sun, Kevin Parkes, Tony Johnson, Bertil Samuelsson
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Publication number: 20110212994Abstract: 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: ApplicationFiled: June 28, 2010Publication date: September 1, 2011Inventors: BRIAN CLEM, SUCHETA TELANG, JOHN TRENT, JASON CHESNEY, POORAN CHAND, GILLES TAPOLSKY
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Publication number: 20110190329Abstract: 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: ApplicationFiled: August 11, 2009Publication date: August 4, 2011Inventors: Michael R. Wood, June J. Kim, Harold G. Selnick, Shawn J. Stachel
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Patent number: 7985413Abstract: 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: GrantFiled: March 5, 2009Date of Patent: July 26, 2011Assignee: Albemarle CorporationInventors: Jonathan N. Howarth, Christopher J. Nalepa, Michael J. Sanders, David L. Shelton
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Publication number: 20110165118Abstract: 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: ApplicationFiled: November 13, 2008Publication date: July 7, 2011Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
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Patent number: 7973067Abstract: 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: GrantFiled: December 10, 2008Date of Patent: July 5, 2011Assignee: Schering CorporationInventors: 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
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Publication number: 20110144173Abstract: 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: ApplicationFiled: February 10, 2011Publication date: June 16, 2011Applicant: BAYER CROPSCIENCE INC.Inventor: Edwin VANDENBERG