C=x Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding (x Is Chalcogen) Patents (Class 514/423)
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Patent number: 8143306Abstract: The invention provides a compound of formula (I), a solvate, a salt or prodrug thereof, useful in the treatment of diseases and conditions mediated by modulation of use-dependent voltage-gated sodium channels. Methods of treating and moderating one or more bipolar disorders in a mammal are also provided.Type: GrantFiled: January 4, 2011Date of Patent: March 27, 2012Assignee: Convergence Pharmaceuticals LimitedInventors: Giuseppe Alvaro, Markus Bergauer, Roberto Profeta, Riccardo Giovannini
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Patent number: 8143259Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, L, Q, R1, R2, and R3 are defined herein.Type: GrantFiled: August 11, 2009Date of Patent: March 27, 2012Assignee: Janssen Pharmaceutica, NVInventors: Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Donald W. Ludovici, Jay M. Matthews, Mingde Xia, Xiaoqing Xu, Mark A. Youngman, Bin Zhu
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Publication number: 20120071538Abstract: Good bioavailability of desmopressin can be obtained by means of an orodispersible pharmaceutical dosage form. Preferred dosage forms comprise desmopressin and an open matrix network which is an inert water-soluble or water-dispersible carrier material. Desmopressin formulated in this way is useful for voiding postponement, or the treatment or prevention of incontinence, primary noctural enuresis (PNE), nocturia or central diabetes insipidus. Peptides other than desmopressin can also be formulated in this way.Type: ApplicationFiled: May 18, 2011Publication date: March 22, 2012Inventors: Anders Nilsson, Hans Lindner, JØRGEN Wittendorff
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Patent number: 8138200Abstract: The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell.Type: GrantFiled: December 2, 2009Date of Patent: March 20, 2012Assignees: Wake Forest University, University of North Carolina-Chapel HillInventors: Louis S. Kucera, Ronald A. Fleming, Khalid S. Ishaq, Gregory L. Kucera, Susan L. Morris-Natschke
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Publication number: 20120065206Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.Type: ApplicationFiled: December 1, 2009Publication date: March 15, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
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Publication number: 20120065162Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.Type: ApplicationFiled: November 17, 2011Publication date: March 15, 2012Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
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Publication number: 20120064160Abstract: This invention discloses an orally administered pharmaceutical composition for the treatment of elevated levels of cholesterol and related conditions comprising a statin and fenofibrate in the form of microparticles of solid fenofibrate that are stabilized by phospholipid as a surface active substance, wherein a therapeutically effective amount of the composition provides the statin and a quantity of fenofibrate to a fasted human patient that is greater than 80% of the quantity of fenofibrate provided by the same amount of the composition when administered to the same patient who has been fed a high fat meal.Type: ApplicationFiled: November 14, 2011Publication date: March 15, 2012Applicant: Jagotec AGInventors: Pol-Henri Guivarc'h, Indu Parikh, Robert A. Snow
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Publication number: 20120065225Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, Ar, R1, R2, Ra and Rb are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: ApplicationFiled: November 21, 2011Publication date: March 15, 2012Inventors: Pravin Iyer, Clara Jeou Jen Lin, Stephen M. Lynch, Matthew C. Lucas, Ann Marie Madera, Kerem Erol Ozboya, Robert James Weikert, Ryan Craig Schoenfeld
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Publication number: 20120065241Abstract: Pyrrole derivatives are disclosed as agents for the treatment and prevention of neuropathies and neurodegenerative diseases characterized by the presence of axonal blockages, impaired axonal transport or impaired trafficking of vesicles in neurons.Type: ApplicationFiled: November 15, 2011Publication date: March 15, 2012Applicant: Myrexis, Inc.Inventors: Christine Klein, Andrew Gassman, Leena Bhoite, John Manfredi
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Publication number: 20120059040Abstract: Novel forms of atorvastatin magnesium salt designated Form A, Form B, Form C, Form D, Form E, and Form F, pharmaceutical compositions containing such compounds, methods for their preparation and methods utilizing the compounds for treatment of hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease are described.Type: ApplicationFiled: November 14, 2011Publication date: March 8, 2012Inventors: Jason A. Leonard, Janathan M. Miller
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Publication number: 20120053196Abstract: The present disclosure provides products including an endocrine treatment product and a statin as a combined preparation for simultaneous, separate or sequential use in therapy. Further, there is provided a method of treatment of a mammalian breast cancer subject, comprising simultaneous, separate or sequential administration of therapeutically effective amounts of a statin and an endocrine treatment product.Type: ApplicationFiled: January 29, 2010Publication date: March 1, 2012Inventors: Karin Jirström, Donal J. Brennan
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Publication number: 20120053200Abstract: The present invention relates to N-1-Benzyl-2-hydroxy-3-(hetero)arylamino-propyl)-isophthalamides of formula I having BACE2 inhibitory activity and their use as therapeutically active substances, their manufacture and pharmaceutical compositions. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. type 2 diabetes.Type: ApplicationFiled: August 23, 2011Publication date: March 1, 2012Inventors: Harald Mauser, Matthias Nettekoven, Sébastien Schmitt
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Publication number: 20120053192Abstract: This present invention discloses a heterocyclic substituted acardite derivate and application thereof, namely compounds in the general formula (1) or the general formula (2) or pharmaceutically acceptable salts thereof, wherein A is monosubstituted or polysubstituted quinoline, isoquinoline, quinazoline, pyrrole or pyrimidine, and the substituent is halogen, C1-5alkyl, C1-5haloalkyl, C1-5alkoxy, C1-5haloalkoxy, C1-5alkylamino, C1-5haloalkylamino, amino or nitryl; R1 is C1-5alkyl; R2 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy; and R3 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy. The compound of the present invention and the pharmaceutically acceptable salt thereof can be used for treating tumor or leukemia.Type: ApplicationFiled: May 4, 2010Publication date: March 1, 2012Applicants: Nanjing Luyesike Pharmaceutical Co., Ltd., Jiangsu Provincial Institute of Materia Medica Co. Ltd.Inventors: Aihua Zhang, Shengtao Yuan, Guang Cheng, Yipeng Shen, Ancheng Ji
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Publication number: 20120052118Abstract: The present invention provides an apparatus and process for making softgel capsules having incorporated therein other solid dosage forms selected from the group consisting of pellets, smaller capsules, smaller tablets, sustained release solid dosage forms, immediate release solid dosage forms, extended release solid dosage forms and zero order release solid dosage forms, said apparatus comprising: (a) two spreader boxes; (b) two casting drums; (c) a pair of rotary dies having means for suction; (d) a liquid fill system; (e) a wedge for heating gelatine ribbons and feeding said fill; and (f) two lateral dispensing devices said lateral dispensing devices including hoppers having said solid dosage forms, channelguides for transporting said solid dosage forms and a grasping claw for dispensing said solid dosage form into the softgel pocket formed in the rotary dies.Type: ApplicationFiled: July 18, 2011Publication date: March 1, 2012Inventors: Carlos Salazar Altamar, Gustavo Anaya, Braulio Teran, Newman Aguas Navarro, Willmer Herrera
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Patent number: 8124790Abstract: The present invention relates to a preparation process useful in synthesis of atorvastatin, more particularly a process for preparing atorvastatin is effective in treating hyperlipemia, comprising protecting the dihydroxy group at C3 and C5 positions of the starting material cis-t-butyl-6-substituted-3,5-dihydroxy-hexanoate with trialkyl orthoformate, reducing the terminal nitro or cyano group to amine group, performing JV-alkylation by sequentially reacting with ethyl 4-fluorobenzene-2-haloacetate and isobutyryl chloride, cyclizing with JV,3-diphenylpropynamide, and performing deprotection and hydrolysis.Type: GrantFiled: April 4, 2008Date of Patent: February 28, 2012Assignee: Medichem Korea Co., Ltd.Inventors: Dong-Ock Cho, Younja Kwon, Kyeong-Hoi Cha, Yeongsook Kim, Hyun-Seop Tae
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Publication number: 20120045509Abstract: The present invention refers to pharmaceutical composition comprising a DPP-IV inhibitor.Type: ApplicationFiled: October 27, 2011Publication date: February 23, 2012Inventors: Bernd Michael Loeffler, Alexander MacDonald, Cynthia Rocha, Eric Worth
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Publication number: 20120046276Abstract: A method of preventing or treating diseases caused by Mycobacterium, comprising administering to a subject in need of such treatment an effective amount of a pleuromutilin.Type: ApplicationFiled: October 25, 2011Publication date: February 23, 2012Applicant: Nabriva Therapeutics AGInventors: Gerd Ascher, Heinz Berner, Rosemarie Mang
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Publication number: 20120046335Abstract: Atorvastatin potassium crystalline Forms A, B, E, F, and G are provided. Also provided are methods of preparing atorvastatin potassium crystalline Forms A, B, E, F, and G. Atorvastatin potassium crystalline Forms A, B, E, F, and G may be used to prepare pharmaceutical compositions useful for the treatment of hypercholesterolemia or hyperlipidemia.Type: ApplicationFiled: October 31, 2011Publication date: February 23, 2012Inventors: Yoav KOWALSKI, Ariel Mittelman, Sigalit Levi
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Publication number: 20120045483Abstract: The current invention provides new methods and means for the prevention and treatment of ageing-related symptoms and diseases. The invention discloses Mannitol 5 and/or proline containing compositions that are particularly useful for the treatment of premature ageing related symptoms in mammalian subjects suffering from genetic defects in DNA damage response and genome maintenance pathways. Humans suffering from Cockayne syndrome (CS), Xerodema pigmentosum (XP), combined XPCS, trichothiodystrophy (TTD), COFS (cerebro-oculo-facio-skeletal syndrome), 10 XFE disorder (Xpf-Erccl syndrome), Bloom Syndrome (BS), Werner Syndrome (WS), Ataxia telangiectasia (AT), Fanconi Anemia (FA), Hutchinson Guilford Progeria (HGP) may be treated with pharmaceutical compositions comprising mannitol and/or proline according to this invention.Type: ApplicationFiled: September 6, 2011Publication date: February 23, 2012Applicant: ERASMUS MCInventors: Gijsbertus van der Horst, Jan Hoeijmakers, Ingrid van der Pluijm
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Patent number: 8119623Abstract: The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (I) or (Ia) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (I) or (Ia) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.Type: GrantFiled: September 15, 2009Date of Patent: February 21, 2012Assignee: Priaxon AGInventors: Christoph Burdack, Cedric Kalinski, Vladimir Khazak, Gunther Ross, Lutz Weber
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Process for separating the diastereomers of RSS-and SSS-N- ? [1-carboxy-3-phenylpropyl] lysylproline
Patent number: 8119817Abstract: A process for separating the diastereomers of RSS— and SSS—N-?[1-carboxy-3-phenylpropyl]lysylproline is described. Previous chromatographic processes for separating the diastereomers of this peptide active substance, such as for example adsorption chromatography, exhibited disadvantages with regard to the solvents used and throughput. These disadvantages do not occur if basic ion exchangers are used in the chromatographic separation of the diastereomers. In particular, purely aqueous solutions may be used as the eluent.Type: GrantFiled: August 3, 1999Date of Patent: February 21, 2012Assignee: Degussa-Huels AGInventors: Frédéric Boisivon, Jean Debas, Gérard Richet -
Patent number: 8119684Abstract: Compounds of formula (I), compositions, methods and kits are provided. The compounds and compositions may be particularly useful for modulating immunological responses. Formula (I) wherein, R1 is alkyl, aryl, or heterocyclyl; R2 is H, alkyl, aryl, heterocyclyl, OR3 or N(R3)2, R3 is H, alkyl, aryl, or heterocyclyl; R4 is H, CN, halogen, CF3, CO2R3, or C(O)N(R3)2; X is S, SO2, O, or NR3; and Y is S, O, or NR3.Type: GrantFiled: December 29, 2004Date of Patent: February 21, 2012Assignees: Dana-Farber Cancer Institute, Inc., The Brigham and Women's Hospital, Inc.Inventors: Li-An Yeh, Gregory D. Cuny, Melissa Call, Kai Wucherpfennig, Ross L. Stein
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Publication number: 20120041025Abstract: Compounds are provided that comprise dinitroso-derivatives of dihydrolipoic acid. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating various diseases and disorders, including angina, hypertension, diabetes, dyslipidemia, renal insufficiency, myocardial infarction, stroke, atherosclerosis, and the target organ damage that accompanies these various diseases and disorders, are further provided. The compounds are useful in improving vasodilation, reducing low-density lipoprotein oxidation, and reducing inflammation in a subject.Type: ApplicationFiled: February 19, 2010Publication date: February 16, 2012Inventor: Sampath Parthasarathy
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Publication number: 20120040006Abstract: The present invention relates to a pharmaceutical composition comprising brivaracetam as active ingredient, the invention relates specifically to a prolonged release formulation.Type: ApplicationFiled: February 5, 2010Publication date: February 16, 2012Applicant: UCB PHARMA, S.A.Inventors: Frédéric Eeckman, Domenico Fanara, Monique Berwaer
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Publication number: 20120040898Abstract: A pharmaceutical composition comprising a combination of (A) a 1-thio-D-glucitol compound represented by the general formula (I) and (B) at least one member of the group consisting of biguanides, insulin secretagogues, insulin sensitizers, insulins, dipeptidyl peptidase IV inhibitors, ?-glucosidase inhibitors, and GLP-1 mimetics, has superior efficacy in preventing or treating diabetes mellitus, diseases associated with diabetes mellitus, or complications of diabetes mellitus and yet it causes no appreciable side effects.Type: ApplicationFiled: April 16, 2010Publication date: February 16, 2012Applicant: TAISHO PHARMACEUTICAL CO., LTDInventors: Teisuke Takahashi, Saeko Uchida
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Publication number: 20120035197Abstract: The present invention, which is applicable in the pharmaceutical industry, relates to the use of fibrates, in particular fenofibrate, especially in the form of a solid oral composition, for the manufacture of a drug for the treatment of sleep apnea, sleep apnea syndrome, in particular obstructive sleep apnea or obstructive sleep apnea syndrome.Type: ApplicationFiled: December 31, 2009Publication date: February 9, 2012Applicant: Fournier Laboratories Ireland LimitedInventor: Eric Bruckert
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Publication number: 20120035234Abstract: A composition is described that can be used in prevention or treatment of patients having impaired gastro-intestinal tract function. The composition comprises free amino acids including about 9.0% to about 17.0% glutamic acid. Methods of treatment of impaired gastro-intestinal tract function are described.Type: ApplicationFiled: October 18, 2011Publication date: February 9, 2012Applicant: Nestec S.A.Inventors: Constance Whippie, Olivier Ballevre, Julio Boza, Paul-André Finot
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Publication number: 20120035238Abstract: The present application relates to the use of one or more compounds of Formula (I) or pharmaceutically acceptable solvates or prodrugs thereof, for treating cancer or for treating or preventing a viral infection.Type: ApplicationFiled: March 2, 2010Publication date: February 9, 2012Applicant: GOFF HILL LIMITEDInventor: William G. Tucker
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Patent number: 8110598Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. This invention also relates to the process for preparing such compounds, a composition containing such a compound and the use of such a compound and composition in medicine.Type: GrantFiled: January 23, 2008Date of Patent: February 7, 2012Assignee: Cadila Healthcare LimitedInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Gajubhai Barot
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Publication number: 20120029001Abstract: Nephrogenic diabetes insipidus is treated with statins.Type: ApplicationFiled: July 30, 2010Publication date: February 2, 2012Applicant: UNIVERSITA' DEGLI STUDI DI BAR (Italian Nationality)Inventors: Giuseppe Procino, Maria Svelto, Giovanna Valenti, Monica Carmosino
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Publication number: 20120029032Abstract: Disclosed is a matrix-type sustained release preparation containing a basic drug unstable against an acid as an active pharmaceutical ingredient, wherein the decomposition of the basic drug unstable against the acid can be prevented and therefore the pH-dependent release can be reduced. A hardly water-soluble basic normal salt is added to a matrix-type sustained release preparation containing a basic drug that is unstable against an acid.Type: ApplicationFiled: March 26, 2010Publication date: February 2, 2012Applicant: KYORIN PHARMACEUTICAL CO., LTD.Inventors: Mamoru Fukuda, Mayuko Takahashi, Takahiro Goto
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Publication number: 20120029030Abstract: Generally the method involves identifying the concentration of each of two or more active therapeutics tailored to treat a particular patient's unique metabolism and one or more diseases, communicating that information to a producer who has multiple fixed or variable concentrations of each active available, where the producer then combines the individual concentrations of each active into single units such as a tablets or pills, and distributes those indirectly or directly to the patient.Type: ApplicationFiled: August 3, 2011Publication date: February 2, 2012Inventors: Richard L. Kirsh, Steven D. Finkelmeier, Robert Glinecke, Luigi Martini
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Publication number: 20120028937Abstract: Provided is a compound useful as a therapeutic drug for pain and inflammation caused by various pathological conditions such as neuropathic pain and rheumatoid arthritis. The compound of the formula (I) or a salt thereof [wherein R1 is a methyl group or a hydrogen atom, R2 represents a hydrogen atom, an alkyl group, an alkylcarbonyl group or an aryl carbonyl group, A represents a cycloalkyl group, a cycloalkenyl group, an aryl group or a heteroaryl group (each group may be substituted with a substituent selected from the group consisting of alkyl, alkenyl, cycloalkyl and halogen), n and m each represent an integer of 1, 2 or 3, and p represents an integer of 0, 1, 2 or 3].Type: ApplicationFiled: May 7, 2009Publication date: February 2, 2012Inventors: Yasunori Tsuzuki, Toshiya Morie, Takanori Nakamura, Isao Shimizu, Masanori Miyauchi
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Publication number: 20120029003Abstract: Described herein are materials and methods for predicting and monitoring a heart failure patient's physiological response to treatment with a statin. More specifically, the present invention relates to the endogenous protein galectin-3 and its use as a predictor of response to treatment with 3-hydroxy-3-methylglutaryl coenzyme-A reductase inhibitors, or statins.Type: ApplicationFiled: July 1, 2011Publication date: February 2, 2012Applicant: BG Medicine, Inc.Inventor: Pieter Muntendam
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Publication number: 20120027706Abstract: This invention relates to methods and compositions for bringing about changes in skin pigmentation. More particularly, this invention relates to compounds which affect melanogenesis and can be used as depigmenting agents or as agents for darkening skin utilizing the PAR-2 pathway.Type: ApplicationFiled: July 15, 2011Publication date: February 2, 2012Inventors: Stanley S. Shapiro, Miri Seiberg, Susan Niemiec, John Kung
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Patent number: 8106089Abstract: The invention relates to a compound represented by general formula (I) wherein Z represents N, O or S, and A represents a CH group, a nitrogen atom or an NL+ group wherein L represents a straight-chained or branched C1-C12 alkyl group. The invention also relates to a method for the preparation thereof and the use thereof as an antimitotic.Type: GrantFiled: May 13, 2005Date of Patent: January 31, 2012Assignees: Centre National de la Recherche, Universite de Rennes 1Inventors: Yannick Arlot, Bénédicte Martin, Jean-Guy Delcros, Gilles Alcaraz, Olivier Paulus
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Publication number: 20120021049Abstract: The present invention is in the fields of medicine, pharmaceuticals, nutraceuticals, endocrinology and cardiology. The invention provides compositions comprising a statin, an inhibitor of the angiotensin converting enzyme, an antiplatelet compound and an anti-hyperglycemic compound for use in the treatment and/or prevention of cardiometabolic risk factors of Metabolic Syndrome and treatment and/or prevention of Metabolic Syndrome. The present invention provides for the use of such compositions in the manufacture of products for treatment and/or prevention of Metabolic Syndrome. The biguanide metformin of the composition could be present in extended release form allowing its use together with the other drugs in a single dosage form at low dose. This combination of drugs in a single daily dosage greatly improves compliance and adherence to treatment which is a critical factor for treating patients with Metabolic Syndrome.Type: ApplicationFiled: July 21, 2011Publication date: January 26, 2012Applicant: Nucitec S.A. de C.V.Inventors: Miguel Angel Duarte-Vázquez, Sandra Garcia Padilla, Jorge Luis Rosado
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Publication number: 20120022075Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group ? or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group ? consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hydType: ApplicationFiled: August 5, 2011Publication date: January 26, 2012Inventors: Akihiro FURUKAWA, Takehiro FUKUZAKI, Yukari ONISHI, Hideki KOBAYASHI, Takeshi HONDA, Yumi MATSUI, Masahiro KONISHI, Kenjiro UEDA, Tetsuyoshi MATSUFUJI
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Publication number: 20120021048Abstract: The present invention is in the fields of medicine, pharmaceuticals, nutraceuticals and cardiology. The invention provides compositions comprising a statin, an inhibitor of the angiotensin converting enzyme, an antiplatelet compound and an antioxidant compound for the treatment and/or prevention of cardiovascular disease.Type: ApplicationFiled: July 21, 2011Publication date: January 26, 2012Applicant: Nucitec S.A. de C.V.Inventors: Miguel Angel Duarte-Vazquez, Sandra Garcia Padilla, Jorge L. Rosado
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Patent number: 8101650Abstract: A method for treating an immunology-related disease. The method involves administering to a mammal in need thereof a pharmaceutically effective amount of an amino acid compound, a pharmacologically acceptable salt thereof or a pharmacologically acceptable ester thereof. The compound has the following formula: wherein R1 and R2 are each hydrogen; R3 is hydrogen; R4 is C1-C2 alkyl; n is 2; X is ?N-D, wherein D is hydrogen, C1-C4 alkyl or phenyl; Y is ethylene, ethynylene, —CO—CH2 or phenylene; Z is ethylene or trimethylene; R5 is unsubstituted C3-C10 cycloalkyl, unsubstituted C3-C10 aryl, or C3-C10 cycloalkyl or C6-C10 aryl substituted with 1 to 3 substituents selected from the group consisting of halogen, lower alkyl, halogeno lower alkyl and lower alkoxy; and R6 and R7 are each hydrogen.Type: GrantFiled: August 12, 2009Date of Patent: January 24, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Takahide Nishi, Takaichi Shimozato, Futoshi Nara, Shojiro Miyazaki
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Patent number: 8101626Abstract: The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual.Type: GrantFiled: April 1, 2010Date of Patent: January 24, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Zhi-Liang Chu, James N. Leonard, Juerg Lehmann, Robert M. Jones
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Publication number: 20120015928Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
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Publication number: 20120015029Abstract: This invention relates to tablets especially tablets formed by direct compression of a dipeptidylpeptidase IV (DPP-IV) inhibitor compound, a process for the preparation thereof, to new pharmaceutical formulations, and new tableting powders comprising DPP-IV inhibitor formulations capable of being directly compressed into tablets. The invention relates further to a process for preparing the tablets by blending the active ingredient and specific excipients into the new formulations and then directly compressing the formulations into the direct compression tablets. The invention also relates to vildagliptin particle size distribution and a new crystal form of vildagliptin particularly adapted for the preparation of improved tablets and other pharmaceutical compositions.Type: ApplicationFiled: July 19, 2011Publication date: January 19, 2012Inventors: Sabine Pfeffer, Frank Schaefer, Ricardo Schneeberger, Paul Allen Sutton, Martin Friedrich Trueby, Wolfgang Wirth
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Publication number: 20120014889Abstract: A method comprising reacting glycerol with acetaldehyde or 1,1-diethoxyethane to produce 1,3-dihydroxyacetone (DHA), without using fermentation or direct oxidation of the glycerol is provided. DHA is useful in various products, including as a sunless tanning agent.Type: ApplicationFiled: July 14, 2011Publication date: January 19, 2012Inventors: Dennis Miller, Xi Hong, Carl Lira, Omar McGiveron
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Publication number: 20120014907Abstract: Disclosed are methods and compositions for the treatment of hyperlipidemia and conditions associated therewith, such as CHD, ischemic stroke, restenosis after angioplasty, peripheral vascular disease, intermittent claudication, myocardial infarction (e.g. necrosis and apoptosis), dyslipidemia and post-prandial lipemia. The methods include administration of a therapeutically effective amount of a compound of formula (I), wherein R is substituted adamantly; and N is 0 to 3; in free form or in acid addition salt form, and a pharmaceutically acceptable carrier.Type: ApplicationFiled: September 26, 2011Publication date: January 19, 2012Inventors: David Grenville Holmes, Thomas E. Hughes
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Publication number: 20120015011Abstract: Disclosed is a cosmetic composition having a double-shell type nano-structure. More particularly, the nano-structure of the cosmetic composition includes: a water-soluble bioactive ingredient core; a core shell containing poly(ethyleneglycol)-poly(caprolactone)-poly(ethyleneglycol) (PE-PCL-PEG) triblock copolymer in order to include the bioactive ingredient core therein; and an outer shell containing phospholipids or derivatives thereof in order to enclose the core shell therein. Such a cosmetic composition improves stability of active components which are prone to oxidation, light degradation, heat degradation, etc., is formed in a nanoparticle size which in turn shows high transdermal absorption and is very useful to prepare a cosmetic composition stably encapsulating various bioactive ingredients with anti-wrinkle effects, whitening effects, and so forth.Type: ApplicationFiled: February 9, 2011Publication date: January 19, 2012Applicant: WOONGJIN COWAY CO., LTD.Inventors: Sung-Bo SHIM, Byoung-Young JEON, Joo-Hyuck LIM, Jong-Keun CHOI, Yong-Joon JOO, Jin-Hun CHO
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Publication number: 20120015911Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: ApplicationFiled: September 20, 2011Publication date: January 19, 2012Applicant: Bellus Health Inc.Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
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Publication number: 20120015942Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: July 18, 2011Publication date: January 19, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
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Publication number: 20120015943Abstract: This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: July 18, 2011Publication date: January 19, 2012Applicant: Millennium Pharmacuticals, Inc.Inventors: Christopher Blackburn, Emily F. Calderwood, Kenneth M. Gigstad, Alexandra E. Gould, Sean J. Harrison, He Xu
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Publication number: 20120015925Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.Type: ApplicationFiled: May 16, 2011Publication date: January 19, 2012Applicant: ASAHI KASEI PHARMA CORPORATIONInventors: Takehiko SASAHARA, Mitsunobu MOHRI, Ken-ichi KASAHARA