Divalent Chalcogen Or Acyclic Nitrogen Double Bonded At 2-position, Or Tautomeric Equivalent Patents (Class 514/392)
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Publication number: 20140073574Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.Type: ApplicationFiled: November 13, 2013Publication date: March 13, 2014Inventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
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Publication number: 20140037547Abstract: The present invention relates to cGMP protein kinase (PKG) and regulatory domains and methods of use thereof. The structural determination of PKG domains is also described. cGMP independent PKG activators and uses thereof are also described.Type: ApplicationFiled: March 13, 2013Publication date: February 6, 2014Applicant: The University of Vermont and State Agricultural CollegeInventors: Wolfgang Dostmann, Brent W. Osborne, Thomas M. Moon
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Publication number: 20140011809Abstract: A method and means for delivery of drugs to the chorio-retina and the optic nerve head which comprises contacting the surface of the eye with an effective amount of drug for treatment of chorio-retina and optic nerve head and a physiologically acceptable adrenergic agent for enhancing delivery of the drug to these tissues in an ophtalmologically acceptable carrier, said adrenergic agent being selected from the group consisting of alpha adrenergic agonist agents, derivatives of the alpha adrenergic agonist agents, beta-blocking agents, derivatives of the beta-blocking agents and mixtures thereof.Type: ApplicationFiled: June 7, 2013Publication date: January 9, 2014Inventor: Raouf Rekik
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Patent number: 8618149Abstract: Disclosure is provided for methods of preventing, removing or inhibiting microbial biofilm formation or microbial infection in a plant or plant part thereof, including applying thereto a treatment effective amount of an active compound as described herein, or an agriculturally acceptable salt thereof. Methods of enhancing a microbicide (e.g., including a copper, antibiotic, bacteriophage, etc.) and/or plant defense activator are also provided, including applying an active compound as described herein. Compositions comprising an active compound as described herein in an agriculturally acceptable carrier are also provided, and in some embodiments the compositions further include a microbicide (e.g., including copper, antibiotic, bacteriophage, etc.) and/or plant defense activator.Type: GrantFiled: August 31, 2012Date of Patent: December 31, 2013Assignee: North Carolina State UniversityInventors: Christian Melander, John Cavanagh, David Ritchie, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards, Thomas W. Lindsey, Jonathan S. Lindsey
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Publication number: 20130345275Abstract: Compounds of formula I and a method for their preparation are described: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies -alkyl-aryl or -alkyl-heteroaryl; X signifies CH2, oxygen atom or sulphur atom; n is 2 or 3; including the individual (R)- and (S)-enantiomers or mixtures of enantiomers thereof; and including pharmaceutically acceptable salts and esters thereof. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.Type: ApplicationFiled: June 13, 2013Publication date: December 26, 2013Inventors: Patricio Manuel Vieira Araujo Soares Da Silva, David Alexander Learmonth, Alexander Beliaev
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Patent number: 8609075Abstract: A heparanase activity inhibitor comprising, as an active ingredient, a cyclic carboxamide derivative represented by formula (I): wherein n is an integer of 1 to 3, R1 is hydrogen or a C1-6 hydrocarbon group optionally substituted with hydroxyl, X is —CH2— or a group represented by —N(R2)—, and R2 is hydrogen or a C1-6 hydrocarbon group optionally substituted with hydroxyl, or a salt thereof.Type: GrantFiled: September 29, 2010Date of Patent: December 17, 2013Assignee: Shiseido Company, Ltd.Inventors: Shunsuke Iriyama, Hirotada Fukunishi, Masaru Suetsugu, Satoshi Amano
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Patent number: 8592454Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like.Type: GrantFiled: September 18, 2009Date of Patent: November 26, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Junya Shirai, Hideyuki Sugiyama, Taku Kamei, Hironobu Maezaki
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Publication number: 20130310412Abstract: Disclosed are compositions for treatment of pain comprising a first compound and a second compound, where the first compound is an opioid antagonist that treats pain by blocking Toll-like receptor 4 (TLR4) and the second compound is a direct-acting alpha-2 adrenergic agonist that enhances the pain treatment effect and abates adverse effects of the first compound, synergistic pharmaceutical compositions thereof, and their use in the treatment, prevention, and reversal of pain, particularly neuropathic pain.Type: ApplicationFiled: March 13, 2013Publication date: November 21, 2013Inventor: Annette Channa Toledano
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Publication number: 20130303489Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.Type: ApplicationFiled: March 11, 2013Publication date: November 14, 2013Applicant: Eisai R&D Management Co., Ltd.Inventors: Sergei Agoulnik, Bruce Decosta, Hong Du, Yimin Jiang, Xiang-Yi Li, Kenichi Nomoto, John (Yuan) Wang, Huiming Zhang
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Publication number: 20130281410Abstract: The invention provides methods for the treatment of major depressive disorder in male subjects and methods for the treatment of psychiatric disorders at high altitudes by administering one or more creatine-containing compounds.Type: ApplicationFiled: May 13, 2011Publication date: October 24, 2013Applicants: University of Utah Research Foundation, The McLean Hospital CorporationInventor: Perry F. Renshaw
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Publication number: 20130281451Abstract: A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.Type: ApplicationFiled: April 3, 2013Publication date: October 24, 2013Applicant: ANNJI PHARMACEUTICAL CO., LTD.Inventors: Ji-Wang Chern, Ajit Dhananjay Jagtap, Hsiao-Chun Wang, Grace Shiahuy Chen
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Patent number: 8563714Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.Type: GrantFiled: May 17, 2010Date of Patent: October 22, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Publication number: 20130274303Abstract: The present disclosure relates to methods of treating a stimulant addiction of a patient comprising administering to a patient in need a therapeutically effective dose of a selective dopamine beta-hydroxylase inhibitor thereby decreasing stimulant reward, inducing aversion for the stimulant or preventing relapse in the patient. The disclosure further encompasses methods whereby a therapeutically effective dose of a selective dopamine beta-hydroxylase inhibitor is determined by: characterizing the genetic profile of the patient with respect to the gene encoding dopamine beta-hydroxylase, a polymorphism therein correlating to the level of endogenous dopamine beta-hydroxylase activity in the patient before administering the therapeutic agent.Type: ApplicationFiled: October 2, 2012Publication date: October 17, 2013Applicants: YALE UNIVERSITY, EMORY UNIVERSITYInventors: EMORY UNIVERSITY, YALE UNIVERSITY
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Patent number: 8557855Abstract: The present invention provides a method of providing neuroprotection to a mammal comprising administering to said mammal suffering from or at risk of suffering a noxious action on its nerve cells an effective amount of a ryanodine antagonist, e.g. dantrolene, to inhibit or prevent nerve cell injury or death.Type: GrantFiled: July 3, 2002Date of Patent: October 15, 2013Assignee: Allergan, Inc.Inventors: Cun-Jian Dong, William A. Hare
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Publication number: 20130266631Abstract: Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of clonidine in a matrix at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate matrix formulations are provided within biodegradable polymers, this pain relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.Type: ApplicationFiled: April 5, 2012Publication date: October 10, 2013Applicant: Warsaw Orthopedic, Inc.Inventors: Danielle L. Clay, Nicholas A. Moore
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Patent number: 8518968Abstract: Disclosed herein are novel hydrazone and diacyl hydrazine derivatives that are inhibitors of the endoplasmic reticulum-associated protein degradation (ERAD) pathway. Also disclosed are hydrazone and diacyl hydrazine derivatives as potent and selective inhibitors of the p97 ATPase. These agents provide useful tools for the study of protein degradation and other processes involving p97. Methods of treating diseases or disorders for which p97 inhibition and/or ER stress induction is an effective treatment with certain hydrazone and diacyl hydrazine derivatives are also disclosed.Type: GrantFiled: December 3, 2010Date of Patent: August 27, 2013Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Adrian Wiestner, Yihong Ye, Qiuyan Wang, William C. Trenkle, Bidhan A. Shinkre
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Publication number: 20130217739Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.Type: ApplicationFiled: March 29, 2013Publication date: August 22, 2013Applicant: Allergan, Inc.Inventor: Allergan, Inc.
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Publication number: 20130217732Abstract: This invention provides compounds of formula I, pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds and intermediates useful in the preparation of same.Type: ApplicationFiled: September 27, 2011Publication date: August 22, 2013Inventor: Chris P. Miller
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Publication number: 20130210769Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Applicant: IRM LLCInventors: Hong Liu, Xiaohui He, Dean Paul Phillips, Xuefeng Zhu, Kunyong Yang, Thomas Lau, Baogen Wu, Yongping Xie, Truc Ngoc Nguyen, Xing Wang
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Publication number: 20130210876Abstract: The present invention provides a method of lowering intraocular pressure which comprises administering a therapeutically effective amount of a pharmaceutical composition comprising 4-bromo-5-(2-imidazolin-2-ylamino)benzimidazole, or a salt thereof to the affected eye of a patient, as a single dose, wherein the affected eye maintains an intraocular pressure less than the baseline thereafter.Type: ApplicationFiled: March 14, 2013Publication date: August 15, 2013Applicant: ALLERGAN, INCInventor: ALLERGAN, INC
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Publication number: 20130203827Abstract: Embodiments of the invention are directed to identifying or treating a patient that would benefit from phosphodiesterase inhibitor therapy.Type: ApplicationFiled: September 13, 2010Publication date: August 8, 2013Applicant: The Regents of the University of Colorado. a BodyInventors: Carmen Sucharov, Michael Bristow, Matthew Taylor, Dobromir Slavov
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Publication number: 20130178453Abstract: The present disclosure relates to compounds useful as agonists of the cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders, either alone or in combination therapy. The compounds of the invention have Formula (I).Type: ApplicationFiled: February 9, 2011Publication date: July 11, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Jason Rohde, Bo Peng, Takashi Nakai, Kevin Sprott, Ara Mermerían, Wayne C. Schairer, Galen John Carey
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Patent number: 8481582Abstract: Compounds of formula I and a method for their preparation are described: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies -alkyl-aryl or -alkyl-heteroaryl; X signifies CH2, oxygen atom or sulphur atom; n is 2 or 3; including the individual (R)- and (S)-enantiomers or mixtures of enantiomers thereof; and including pharmaceutically acceptable salts and esters thereof. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.Type: GrantFiled: May 6, 2008Date of Patent: July 9, 2013Assignee: Bial-Portela & CA, S.A.Inventors: Patrício Manuel Vieira Araújo Soares Da Silva, David Alexander Learmonth, Alexander Beliaev
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Publication number: 20130149318Abstract: A PEG based hydrogel and a procedure for its topical application to the surface of the pia mater of the spinal cord that can be used for intrathecal delivery of diverse drug and biomolecular therapies for the treatment of traumatic central nervous system injuries and disorders including spinal cord injury (SCI), multiple sclerosis (MS) and amyotrophic lateral sclerosis (ALS) are provided. This “painting of the pia” with biofunctionalized hydrogel material may be used as a prelude strategy in the therapeutic management of these CNS disorders. The strategy may be designed to create a microenvironment within the damaged regions of the spinal cord that is more conducive to the successful application of subsequent regeneration based treatments such as cell replacement therapies or endogenous regeneration and plasticity stimulation via application of growth factors or gene therapy.Type: ApplicationFiled: December 13, 2012Publication date: June 13, 2013Applicant: INVIVO THERAPEUTICS CORPORATIONInventor: InVivo Therapeutics Corporation
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Publication number: 20130150367Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: September 12, 2012Publication date: June 13, 2013Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20130149363Abstract: The present invention relates to five-layered pigments based on multicoated platelet-shaped substrates which comprise a layer sequence comprising (A) a layer of SnO2 having a layer thickness of 0.1-50 nm, (B) a high-refractive-index coating consisting of TiO2 in the rutile modification having a layer thickness of 10-800 nm, (C) a colorless coating having a refractive index n?1.8 having a layer thickness of 20-800 nm, (D) a high-refractive-index coating consisting of SnO2 having a layer thickness of 0.1-50 nm, (E) a layer of TiO2 in the rutile modification having a layer thickness of 10-800 nm, and optionally (F) an outer protective layer, and to the use thereof in paints, coatings, powder coatings, printing inks, security printing inks, plastics, ceramic materials, glasses, as dopants for the laser marking of papers and plastics, in cosmetic formulations and for the preparation of pigment preparations and dry preparations.Type: ApplicationFiled: February 8, 2013Publication date: June 13, 2013Applicant: MERCK PATENT GMBHInventor: MERCK PATENT GMBH
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Publication number: 20130137725Abstract: Disclosed herein is a method of treating sensorimotor disorders comprising administering to a subject in need of such treatment an alpha-2 receptor agonist lacking significant alpha-2A receptor activity.Type: ApplicationFiled: January 22, 2013Publication date: May 30, 2013Applicant: Allergan, Inc.Inventor: Allergan, Inc.
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Patent number: 8450337Abstract: Embodiments of the invention generally relate to pharmaceutical compositions containing at least one caffeic acid compound and methods for the topical treatment of proliferative and inflammatory skin disorders such as plaque psoriasis, atopic dermatitis, and other disorders. In some embodiments, the topical treatment includes applications of the pharmaceutical composition containing at least one caffeic acid compound or a mixture of caffeic acid compounds such as caffeic acid ester compounds, caffeic acid amide compounds, analogues thereof, derivatives thereof, salts thereof, or mixtures thereof. The pharmaceutical composition or topical dosage may contain the caffeic acid compound at a concentration by weight within a range from about 0.01% to about 20%, preferably, from about 0.1% to about 15%, preferably, from about 1% to about 10%, more preferably, from about 3% to about 7%, and more preferably, from about 4% to about 6%.Type: GrantFiled: September 30, 2009Date of Patent: May 28, 2013Assignee: Moleculin, LLCInventors: Waldemar Priebe, Charles Conrad, Timothy Madden
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Publication number: 20130129795Abstract: Disclosure is provided for imidazole-triazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.Type: ApplicationFiled: January 2, 2013Publication date: May 23, 2013Inventor: North Carolina State University
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Publication number: 20130129615Abstract: The present invention encompasses a therapeutic method which employs treatment of a disease such as cancer with triiodothyronine (T3) together with an anti-thyroid treatment such as treatment with an anti-thyroid agent, treatment with radioiodine and surgical removal of all or part of the thyroid gland. A pharmaceutical composition comprising T3 and an anti-thyroid agent and a kit comprising the same are also encompassed by the invention.Type: ApplicationFiled: April 28, 2011Publication date: May 23, 2013Inventors: Osnat Ashur-Fabian, Aleck Hercbergs
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Publication number: 20130116240Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.Type: ApplicationFiled: September 26, 2012Publication date: May 9, 2013Applicant: JAPAN TOBACCO INC.Inventor: Japan Tobacco Inc.
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Publication number: 20130090307Abstract: The present invention relates to combinations and methods for the treatment of neurological disorders related to glutamate excitotoxicity and Amyloid ? toxicity. More specifically, the present invention relates to novel combinatorial therapies of Multiple Sclerosis, Alzheimer's disease, Alzheimer's disease related disorder, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, neuropathic pain, alcoholic neuropathy, alcoholism or alcohol withdrawal, or spinal cord injury, based on Baclofen and Acamprosate combination.Type: ApplicationFiled: December 6, 2012Publication date: April 11, 2013Applicant: PHARNEXTInventor: PHARNEXT
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Publication number: 20130085132Abstract: The present invention provides a pyrazole compound of the following general Formula [Ib] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use: wherein each symbol is the same as defined in the description.Type: ApplicationFiled: August 30, 2012Publication date: April 4, 2013Applicant: JAPAN TOBACCO INC.Inventors: Tomoya MIURA, Yosuke OGOSHI, Kazuhito UEYAMA, Dai MOTODA, Toshihiko IWAYAMA, Koichi SUZAWA, Hironobu NAGAMORI, Hiroshi UENO, Akihiko TAKAHASHI, Kazuyuki SUGIMOTO
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Publication number: 20130079326Abstract: The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.Type: ApplicationFiled: May 24, 2011Publication date: March 28, 2013Inventors: Hon-Chung Tsui, Sunil Paliwal, Hyunjin M. Kim, Angela D. Kerekes, Mary Ann Caplen, Sara J. Esposite, Brian A. McKittrick, Thierry Olivier Fischmann, Ronald J. Doll, Matthew Paul Rainka
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Patent number: 8383661Abstract: Preparation of new heterocyclic compounds characterized by 1,3-imidazolidine structure useful for stereoselective synthesis of optically pure key intermediates in 1?-methylcarbapenem production.Type: GrantFiled: October 1, 2009Date of Patent: February 26, 2013Assignee: ACS DOBFAR S.p.A.Inventors: Mauro Freccero, Giovanni Fogliato, Antonio Manca, Michele Bassanini
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Publication number: 20130046003Abstract: The present invention relates to a method for treating retinal diseases and a method for retinal neuroprotection, in a patient in need thereof which comprises of administering a therapeutically effective amount of a pharmaceutical composition comprising a therapeutically effective amount of 4-bromo-N-(imidazolidin-2-ylidene)-1H-benzimidazol-5-amine or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: July 20, 2012Publication date: February 21, 2013Inventors: Mohammed I. Dibas, John E. Donello, Daniel W. Gil, James A. Burke
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Patent number: 8377936Abstract: Use of nicotine receptor agonists for treating inflammatory diseases, including a variety of pulmonary diseases. Such agonists have fewer side effects than other anti-inflammatory drugs, such as steroids. Moreover, these agonists can be used alone or in combination with other anti-inflammatory drugs to alleviate pulmonary diseases. For example, a method of treating pulmonary inflammation of an inflammatory disease selected from the group of asthma, interstitial pulmonary fibrosis (IPF), sarcoidosis, hypersensitivity pneumonitis (HP), and bronchiolitis obliterans with organizing pneumonitis (BOOP) in an animal in need thereof having said inflammation, including administering orally or by inhalation to said animal a nicotinic receptor agonist.Type: GrantFiled: June 15, 2011Date of Patent: February 19, 2013Assignee: Universite LavalInventors: Yvon Cormier, Evelyne Israel-Assayag, Marie-Renée Blanchet
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Patent number: 8372848Abstract: This invention relates generally to N-benzylamino cyclic thioureas, pharmaceutical compositions containing them, and their use as antagonists of melanin-concentrating hormone receptor (MCH receptor).Type: GrantFiled: March 23, 2005Date of Patent: February 12, 2013Assignees: Mixture Sciences, Inc., The Regents of the University of CaliforniaInventors: Richard A. Houghten, Colette Dooley, Adel Nefzi, Zhiwei Wang, Oliver Civelli, Hiroshi Nagasaki
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Publication number: 20130035361Abstract: The invention relates to the novel use of ergothioneine and preferably, L ergothioneine, as a nutritional additive and preservative in foods, medicines, and/or beverages. According to the invention, the powerful antioxidant ergothioneine was found to be very stable over time in and to have no deleterious effects on taste or consistency of food and beverages even when stored, over a period of several years. In a preferred embodiment, ergothioneine may be used as a replacement for all or part of the antimicrobial/preservative sulfur dioxide or other sulfites traditionally used in the wine making process.Type: ApplicationFiled: October 4, 2012Publication date: February 7, 2013Inventors: Robert B. Beelman, Marvin S. Hausman
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Patent number: 8367713Abstract: Disclosure is provided for imidazole-triazole derivative compounds such as those given in Formulas (I)-(VI) that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.Type: GrantFiled: January 21, 2011Date of Patent: February 5, 2013Assignee: North Carolina State UniversityInventors: Christian Melander, Steven A. Rogers, Robert W. Huigens, III, Catherine S. Reed
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Publication number: 20130029970Abstract: The present disclosure relates to compounds of formula I useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: July 9, 2010Publication date: January 31, 2013Applicant: IRONWOOD PHARMACEUTICALS, INCInventors: Kevin Sprott, Jason Rohde, Takashi Nakai, Bo Peng, John Jeffrey Talley
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Publication number: 20130029981Abstract: The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients.Type: ApplicationFiled: June 18, 2012Publication date: January 31, 2013Applicant: Katholieke Universiteit LeuvenInventors: Sigrid De Keersmaecker, Dirk De Vos, Denis Ermolatev, Hans Steenackers, Erik Van Der Eycken, Jozef Vanderleyden, Bharat S. Savaliya
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Publication number: 20130023572Abstract: The present invention relates to a method for treating skin diseases in a patient in need thereof which comprises of administering a pharmaceutical composition comprising a therapeutically effective amount of 4-bromo-N-(imidazolidin-2-ylidene)-1H-benzimidazol-5-amine or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable excipients.Type: ApplicationFiled: July 18, 2012Publication date: January 24, 2013Inventors: Mohammed I. Dibas, John E. Donello, Daniel W. Gil
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Publication number: 20130023573Abstract: The present invention relates to a method for treating visual disorders mediated by lateral geniculate nucleus, superior colliculus and the visual cortex by administering to a patient in need of such treatment, compounds acting at the alpha 2 adrenergic receptors.Type: ApplicationFiled: July 18, 2012Publication date: January 24, 2013Inventors: Ursula V. Staubli, Alan C. Foster, Daniel W. Gil, John E. Donello
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Publication number: 20130017254Abstract: The present invention relates to a novel pharmaceutical formulation comprising phenytoin sodium, a high amount of magnesium stearate, and a low level of a hydrophilic polymer such as a methocel, and a method of preparing the same by blending.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicant: Taro Pharmaceuticals North America, Inc.Inventors: Tamar Blumberg, Orit Brodzsky, Nataly Zissman, Avraham Yacobi
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Publication number: 20130011361Abstract: The present invention provides heterocyclic derivatives of formula (I) that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: October 1, 2010Publication date: January 10, 2013Applicants: XENON PHARMACEUTICALS INC., NOVARTIS AGInventors: Natalie Dales, Jianmin Fu, Qi Jia, Natalia Pokrovskaia, Shaoyi Sun, Zaihui Zhang
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Publication number: 20130012558Abstract: Process for the protection of fish and invertebrates and all their stages of development against or for the treatment of mycoses caused by fungi of the genera Saprolegnia, Aphanomyces, Achlyaflagellata and other species important in aquacultures by use of 2-[[[[1-[3-(1-fluoro-2-phenylethyl)oxy]phenyl]ethylidene]amino]oxy]methyl]alpha-(methoxyimino)-N-methyl-alphaE-benzeneacetamide, amisulbrom, cyazofamid, enestrobin, famoxadone, fenamidone, fluoxastrobin, orysastrobin, picoxystrobin and pyribencarb. This use leads to an inhibition or destruction of pathogenic fungi. The composition, comprising at least one fungicide selected from the abovementioned group for use in fish fanning and keeping is suitable for the prophylaxis and therapy of diseases of fish in aquaculture, in breeding ponds, breeding tanks, aquariums, natural stretches of game fish waters, ponds, and marine fish farms. Addition to the water and feed and direct application are the associated use forms.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: Bayer Intellectual Property GmbHInventors: Isolde Häuser-Hahn, Klaus Stenzel, Ulrike Wachendorff-Neumann
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Publication number: 20120328577Abstract: Disclosure is provided for methods of preventing, removing or inhibiting microbial biofilm formation or microbial infection in a plant or plant part thereof, including applying thereto a treatment effective amount of an active compound as described herein, or an agriculturally acceptable salt thereof. Methods of enhancing a microbicide (e.g., including a copper, antibiotic, bacteriophage, etc.) and/or plant defense activator are also provided, including applying an active compound as described herein. Compositions comprising an active compound as described herein in an agriculturally acceptable carrier are also provided, and in some embodiments the compositions further include a microbicide (e.g., including copper, antibiotic, bacteriophage, etc.) and/or plant defense activator.Type: ApplicationFiled: August 31, 2012Publication date: December 27, 2012Inventors: Christian Melander, John Cavanagh, David Ritchie, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards, Thomas W. Lindsey, Jonathan S. Lindsey
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Publication number: 20120322830Abstract: The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: June 11, 2012Publication date: December 20, 2012Applicant: Purdue Pharma L.P.Inventor: Xiaoming ZHOU
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Publication number: 20120322753Abstract: The production method prepares a solid preparation by dissolving water-insoluble and/or water indissolvable alkaline active pharmaceutical ingredient in an acidifier-containing acid solution to obtain medicated acid liquid; homogeneously mixing alkalizer, adjuvants and the medicated acid liquid, and carrying out wet granulation. The alkalizer is a reagent to reduce the acidity of the mixture of the alkalizer and the medicated acid liquid relative to the acidity of the medicated acid liquid. The preparation method avoids the problems in mechanical pulverization, such as environmental pollution, great loss and serious security risks. This method is simply operated, has high safety coefficient and is convenient for industrialized production. Also disclosed is the solid preparation produced by the method. The solid preparation produced by the method has better dissolution performance than that produced by prior art, and has better or at least equivalent stability and content uniformity with prior art.Type: ApplicationFiled: December 28, 2010Publication date: December 20, 2012Applicants: SHANGHAI ZHONGXI SUNVE PHARMACEUTICAL CO., LTD., SHANGHAI ZHONGXI PHARMACEUTICAL COMPANYInventors: Siji Zheng, Bo Tan