Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/469)
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Publication number: 20130115294Abstract: The present invention relates to a stable liquid oily ready-to-use formulation comprising an active pharmaceutical ingredient, which has hydrophobic and/or lipophilic properties and/or which exhibits stability problems in aqueous environments. The present invention further relates to a method for preparing said formulation, and said formulation for use in the medical treatment of particular patient groups.Type: ApplicationFiled: October 11, 2012Publication date: May 9, 2013Applicant: CTS CHEMICAL INDUSTRIES LTD.Inventor: CTS Chemical Industries Ltd.
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Publication number: 20130116308Abstract: The disclosure relates to the therapeutic utility of CD36 antagonists to reduce body weight, inhibit fat accumulation and especially visceral fat accumulation, improve insulin sensitivity, lower blood glucose levels, and treat and prevent metabolic syndrome, pre-diabetes and diabetes, and lower plasma cholesterol levels and decrease fat deposit in the liver. CD36 antagonists, including SAB or its metabolites, such as RA and DSS, are useful for these purposes.Type: ApplicationFiled: June 1, 2011Publication date: May 9, 2013Applicant: CORNELL UNIVERSITYInventors: Sunghee Cho, Yi Bao, Eunhee Kim
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Patent number: 8436043Abstract: Provision of a prophylactic or therapeutic agent for diabetes, which has superior efficacy. A compound represented by the formula: wherein each symbol is as described in the specification, or a salt thereof.Type: GrantFiled: March 4, 2009Date of Patent: May 7, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Yoshihiro Banno, Ryoma Hara, Ryosuke Tokunoh
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Patent number: 8436208Abstract: A process for the preparation of a substituted 2,2?-dithiophene is described, which process comprises the steps (a), (c) and optional steps (b) and (d): a reaction of a compound of the formula: with a suitable lithium organic compound, preferably Li-alkyl or Li-alkylamide; b) optional exchange of lithium against another metal selected from Mg1 Zn and Cu; c) reaction of the metallated intermediate obtained in step (a) or (b) with a suitable electrophil, which is CO2 or an aldehyde (addition reaction), or a compound Y?—R17 or Y?—R18-Z (substitution reaction), where R17 and R18 are as defined in claim 1; and optionally d) modification of the product obtained in step (c), e.g. by introducing one or more conjugating moieties Y ring closure between suitable monovalent residues R17, exchange or extension of functional groups or substituents such as addition to carbonyl or substitution of carbonyl in R17 or R18.Type: GrantFiled: March 6, 2009Date of Patent: May 7, 2013Assignee: BASF SEInventors: Hans Jürg Kirner, Frank Bienewald, Jean-Charles Flores, Olivier Frédéric Aebischer
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Publication number: 20130101650Abstract: This invention relates to cosmetic and pharmaceutical preparations comprising (i) a diastereomer or a mixture of two or more diastereomers of the compound of formula (I) or (ii) a salt of a diastereomer or of a mixture of two or more diastereomers of the compound of formula (I) or (iii) a mixture of two or more salts of a diastereomer or of a mixture of two or more diastereomers of the compound of formula (I), a diastereomer, salt or a mixture as defined above as a drug for topical application and/or for the treatment of lipoatrophy; the non-therapeutic use of a diastereomer, salt or a mixture as defined above for the prevention, treatment or reduction of skin aging, especially skin wrinkles; the use of a diastereomer, salt or a mixture as defined above for the production of an orally administered non-pharmaceutical preparation.Type: ApplicationFiled: April 8, 2010Publication date: April 25, 2013Inventors: Imke Meyer, Oskar Koch, Jean Krutmann
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Patent number: 8410167Abstract: Methods of using dronedarone or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for use in the prevention of cardiovascular hospitalization or of mortality, articles of manufacture and packages related thereto.Type: GrantFiled: April 16, 2009Date of Patent: April 2, 2013Assignee: SANOFIInventors: Davide Radzik, Martin Van Eickels, Nacéra Hamdani, Christophe Gaudin
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Publication number: 20130079293Abstract: Isolated compounds from adelostemma gracillimum refined fractions and compositions containing the compounds are provided by the present invention. Adelostemma gracillimum refined fractions and the extraction process thereof are also provided by the present invention. The uses of the compounds and the adelostemma gracillimum refined fractions for inhibiting the activities of NMDA receptor or amyloid-beta peptide, for improving memory, and for treating neurodegenerative diseases, neuropathological conditions or epilepsy are further provided by the present invention.Type: ApplicationFiled: March 18, 2011Publication date: March 28, 2013Applicant: BIOTECHNOLOGY RESEARCH CORPORATION LIMITEDInventors: Nancy Yuk-yu Ip, Fanny Chui-Fun Ip, Shengjun Guo
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Patent number: 8399507Abstract: Tricyclic compounds containing a cyclopropanecarboxylic acid fused to a bicyclic ring, including pharmaceutically acceptable salts, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.Type: GrantFiled: October 27, 2008Date of Patent: March 19, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Gui-Bai Liang, Xibin Liao, Weiguo Liu, Paul E. Finke, Dooseop Kim, Lihu Yang, Songnian Lin
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Publication number: 20130064880Abstract: N-hydroxy-4-{2-[3-(N,N-dimethylaminomethyl)benzofuran-2-ylcarbonylamino]ethoxy}-benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, alone or in association with surgery, chemotherapy or hormone therapy treatment or radiotherapy, for use in the treatment of cancer, characterised in that it is administered for 4 consecutive days, that period being followed by 3 consecutive days without any administration of compound of formula (I), with the proviso that the chemotherapy is not FOLFOX.Type: ApplicationFiled: September 6, 2012Publication date: March 14, 2013Applicants: LES LABORATOIRES SERVIERInventors: Ioana Kloos, Renata Robert, Anne Jacquet-Bescond, Stéphane Depil, Marylore Chenel, Sylvain Fouliard, Sriram Balasubramanian
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Publication number: 20130064820Abstract: The present disclosure relates to, inter alia, compositions containing an inhibitor of human complement and/or an inhibitor of interferon alpha, and the use of the compositions in methods for treating or preventing Degos' disease in a subject. In some embodiments, the inhibitor is an antibody, or antigen-binding fragment thereof, that binds to a human complement component C5 protein or to a biologically-active fragment of C5 such as C5a or C5b. In some embodiments, the inhibitor is an antibody, or an antigen-binding fragment thereof, that binds to interferon alpha or to an interferon alpha receptor.Type: ApplicationFiled: March 1, 2011Publication date: March 14, 2013Applicant: ALEXION PHARMACEUTICALS, INCInventor: Cynthia Magro
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Publication number: 20130064897Abstract: The invention relates to life's necessities and in particular those relating to health, more particularly a method for dissolving and improving the intestinal absorption of active ingredients which are poorly-water-soluble or water-insoluble or which cannot be turned into salts in gastric juice, containing one or more active ingredients dispersed in a polyoxyethylene 32 fatty acid ester then hot spraying said dispersion onto a granular excipient in a fluid bed. The powder mixture thus formed is distributed in pharmaceutical compositions after optional dilution in a pharmaceutically-acceptable non-toxic inert excipient. The above is of use in the production of pharmaceutical compositions containing one or more pharmaceutically-acceptable non-toxic inert excipients.Type: ApplicationFiled: July 7, 2008Publication date: March 14, 2013Inventor: Patrice Binay
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Patent number: 8394844Abstract: Provided is a compound represented by the formula (1): wherein R1 and R2 are each independently a hydrogen atom or a straight chain alkyl group having a carbon number of 1-3, R3 is a hydrogen atom, an alkyl group having a carbon number of 1 -4, an alkoxyalkyl group, an aryl group, a halogen atom or a haloalkyl group, or a pharmaceutically acceptable salt thereof, which has, unlike known PGI2 analogs, a selective EP4 agonist action, and a medicament containing the compound, which is useful for the prophylaxis and/or treatment of immune diseases, diseases of the digestive tract, cardiovascular diseases, cardiac diseases, respiratory diseases, neurological diseases, ophthalmic diseases, renal diseases, hepatic diseases, bone diseases, skin diseases and the like.Type: GrantFiled: November 2, 2010Date of Patent: March 12, 2013Assignees: Asahi Glass Company, Limited, Kaken Pharmaceutical Co., Ltd.Inventors: Takahiko Murata, Masahiro Amakawa, Shin Teradaira, Yasushi Matsumura, Katsuhiko Konishi
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Patent number: 8389570Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: GrantFiled: August 12, 2011Date of Patent: March 5, 2013Assignee: Pharmacyclics, Inc.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Patent number: 8389542Abstract: A dosage unit for treating constipation in a human patient is described. The dosage unit of the invention includes a halogenated prostaglandin analog and a pharmaceutically suitable excipient. The dosage unit relieves constipation without substantial side effects.Type: GrantFiled: December 20, 2011Date of Patent: March 5, 2013Assignee: Sucampo AGInventors: Ryuji Ueno, Myra L. Patchen
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Patent number: 8389571Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.Type: GrantFiled: July 19, 2011Date of Patent: March 5, 2013Assignee: Sequoia Pharmaceuticals, Inc.Inventor: Michael Eissenstat
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Patent number: 8389548Abstract: Novel methods for the medical treatment and/or inhibition of the development of osteoporosis, breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure: and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3?,17?-diol and compounds converted in vivo to one of the foregoing presursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursor is disclosed for the medical treatment and/or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.Type: GrantFiled: February 18, 2005Date of Patent: March 5, 2013Assignee: Endorecherche, Inc.Inventor: Fernand Labrie
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Publication number: 20130053392Abstract: A carbonic anhydrase IX (CA IX) inhibitor which comprises a compound of general formula: R—NH—CX—NH—(CH2)n—Ar-Q-SO2—NH2 or a pharmaceutically-acceptable salt, derivative or prodrug thereof; wherein n=0, 1 or 2; Q is O or NH; X is O or S; and R comprises an organic substituent group.Type: ApplicationFiled: February 14, 2011Publication date: February 28, 2013Inventors: Peter Ebbesen, Claudlu T. Supuran, Andrea Scozzafava, Erik Olai Pettersen, Kaye Williams, Ludwig Dubois, Philippe Lambin
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Publication number: 20130053351Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.Type: ApplicationFiled: October 22, 2012Publication date: February 28, 2013Applicant: BIONOMICS LIMITEDInventor: BIONOMICS LIMITED
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Publication number: 20130041025Abstract: Described herein are compositions including prostaglandin analogs including prostamides and methods for using these compositions for increasing eyelash and eyebrow growth and hair growth on the scalp.Type: ApplicationFiled: March 23, 2011Publication date: February 14, 2013Applicant: ALLERGAN, INC.Inventors: John G. Walt, David F. Woodward, Amanda M. Vandenburgh
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Publication number: 20130041023Abstract: The present invention relates to a composition for preventing or treating rotavirus infection, comprising a licorice extract, fractions thereof or compounds separated therefrom. The licorice extract, fractions thereof or compounds separated therefrom have anti-rotavirus effects and exhibit not only virucidal effects against various rotaviruses, but also the effect of inhibiting the cytopathic effect of rotaviruses. Thus, the composition can be effectively used for the prevention or treatment of rotavirus infection.Type: ApplicationFiled: February 11, 2011Publication date: February 14, 2013Inventors: Woo Song Lee, Mun Chual Rho, Young Bae Ryu, Su Jin Park, Jong Sun Chang, Hyung Jun Kwon, Ha Hyun Kim, Hyung Jae Jeong
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Patent number: 8367719Abstract: Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A4 hydrolase (LTA4H or LTA4H) modulation and for the treatment of disease states, disorders, and conditions mediated by LTA4H activity, such as allergy, asthma, autoimmune diseases, pruritis, inflammatory bowel disease, ulcerative colitis, and cardiovascular disease, including atherosclerosis and prevention of myocardial infarction.Type: GrantFiled: April 21, 2011Date of Patent: February 5, 2013Assignee: Janssen Pharmaceutica NVInventors: Genesis M. Bacani, Scott D. Bembenek, Wendy Eccles, James P. Edwards, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Kelly J. McClure, Taraneh Mirzadegan, Alejandro Santillán, Jr.
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Publication number: 20130029846Abstract: The present invention relates to the use of bicyclic amidine compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to novel bicyclic amidines and processes and intermediates for preparing these compounds.Type: ApplicationFiled: March 28, 2011Publication date: January 31, 2013Applicant: BASF SEInventors: Joachim Rheinheimer, Christian Pilger, Stefan Redlich, Doris Kremzow, Claudia Rosenbaum, Burghard Liebmann, Wassilios Grammenos
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Publication number: 20130018093Abstract: This invention relates to a stable epoprostenol composition that can be combined with commercially available IV fluids and can be administered in its reconstituted and/or diluted form under ambient conditions of about 15-30° C. for greater than 24 hours. The composition preferably contains (a) epoprostenol or a salt thereof; (b) a alkalinization agent; and (c) a base, such that when reconstituted or in solution, the solution has a pH>11. Methods for making the lyophilized composition are also disclosed.Type: ApplicationFiled: September 17, 2012Publication date: January 17, 2013Inventor: Nagesh PALEPU
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Patent number: 8354410Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: March 9, 2011Date of Patent: January 15, 2013Assignee: Bristol-Meyers Squibb CompanyInventors: Kap-Sun Yeung, Katharine A. Grant-Young, John F. Kadow
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Publication number: 20130012536Abstract: The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, or a pharmaceutically acceptable salt thereof, wherein RB, n, B, RC, RD, RE, A, and Z are described generally and in classes and subclasses below. The present invention also provides pharmaceutical compositions, methods and kits associated with Formula I, useful for as modulators, and for the treatments of disease and disease conditions associated with ABC transporter proteins.Type: ApplicationFiled: June 27, 2012Publication date: January 10, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Mark Miller, Ashvani Singh, Matthew Hamilton, Peter D.J. Grootenhuis
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Publication number: 20130005767Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.Type: ApplicationFiled: September 14, 2012Publication date: January 3, 2013Applicant: Allergan, Inc.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20130005800Abstract: The invention provides a composition for transdermal or transmucosal administration useful as an anti-Alzheimer's drug, an antiparkinson drug, an antidepressant, a psychoactive drug, or to treat drug dependence. The composition has an effective dose of a racemate or an optically acceptable substance of 1-(benzofuran-2-yl)-2-propylaminopentane or a pharmacologically acceptable salt thereof and a vehicle, which can be administered without an invasion of skin or mucous membrane. The composition enables its active ingredient to stably arrive in a sufficient effective amount through the skin and mucous membrane to the body or brain. The composition is free of disadvantages such as a reduction in an active component caused by a first pass effect in the liver, as well as pain, damage or infection.Type: ApplicationFiled: August 13, 2012Publication date: January 3, 2013Inventors: Fumio Yoneda, Hironori Ohde, Mayumi Watanabe, Mikiyo Sugimoto, Takahiro Kamada, Mizue Hukumoto, Azusa Takase, Naoya Hoshino
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Patent number: 8344181Abstract: the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, S, NR6, SO or SO2; R1 represents hydrogen, cyano, hydroxy, or C1-4alkyl optionally substituted with halo, R2 represents hydrogen, C1-4alkyl, or C1-4alkyloxy-; R3 represents hydrogen, C1-4alkyl, C1-4alkyloxy- or R3 combined with R2 form together a divalent radical selected from the group consisting of —O—CH2— (a), —NR7—CH2— (b), —(CR8R9)m- (c) and —CR10? (d) wherein m represents 1 or 2 and R7, R8, R9 and R10 are each independently selected from hydrogen or C1-4alkyl; R4 represents hydrogen, halo, hydroxy, cyano, amino, NR11R12, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy and halo or R4 represents C1-4alkyl optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R5 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxType: GrantFiled: August 26, 2005Date of Patent: January 1, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Louis Jozef Elisabeth Van Der Veken, Gustaaf Henri Maria Willemsens, François Paul Bischoff
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Publication number: 20120328569Abstract: Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: March 2, 2011Publication date: December 27, 2012Inventors: Casey Cameron McComas, Nigel J. Liverton, Richard Soll, Peng Li, Xuanjia Peng, Hao Wu, Frank Narjes, Joerg Habermann, Uwe Koch, Shilan Liu
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Publication number: 20120329781Abstract: The instant invention relates to a combination, particularly a synergistic combination, of an alpha-2-delta ligand and a dual serotonin-noradrenaline re-uptake inhibitor (DSNRI) or one or both of a selective serotonin re-uptake inhibitor (SSRI) and a selective noradrenaline re-uptake inhibitor (SNRI), and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly neuropathic pain.Type: ApplicationFiled: August 29, 2012Publication date: December 27, 2012Inventors: David James Dooley, Mark John Field, Richard Griffith Williams
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Publication number: 20120329867Abstract: The present invention concerns the use of dronedarone or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for use in the prevention and/or treatment of patients with atrial fibrillation (AF) or atrial Flutter (AFL), shortly after discontinuation of a previous treatment with amiodarone.Type: ApplicationFiled: September 6, 2012Publication date: December 27, 2012Applicant: SANOFIInventors: Christophe GAUDIN, Ihsen Merioua, Davide RADZIK
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Patent number: 8334316Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: GrantFiled: February 9, 2009Date of Patent: December 18, 2012Assignee: ACEA Biosciences, Inc.Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
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Patent number: 8334317Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula I.Type: GrantFiled: October 15, 2008Date of Patent: December 18, 2012Assignee: Amgen Inc.Inventors: Thomas S. Coulter, Christopher H. Fotsch, Chiara Ghiron, Paul E. Harrington, Michael G. Kelly, Philip Miller, Gilbert M. Rishton, David J. St. Jean, Jr., David J. Semin
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Publication number: 20120316230Abstract: The present invention relates to compounds of formula (I), where R1 and R2, which may be identical or different, are selected from the group comprising H, CnH2n-1, a linear or branched alkyl group having 1 to 6 carbons, or together form an aromatic or aliphatic ring with 5 or 6 atoms; R3 is —CO—CH3, —NHOH, —OH, or —OR6 where R6 is a linear or branched alkyl group having 1 to 6 carbon atoms; R4 is H, linear or branched alkyl group having from 1 to 6 atoms, phenyl, benzyl, —CF3 or CF2CF3, vinyl or allyl; R5, R7, R8 are hydrogen atoms; or R3 and R4, R4 and R5, or R7 and R8 together form a ring, fused to the benzene, aromatic or aliphatic ring with 5 or 6 atoms comprising from 1 to 2 heteroatoms selected independently from the group comprising N, O, and use thereof in the medical field.Type: ApplicationFiled: February 15, 2012Publication date: December 13, 2012Inventors: Giancarlo Naccari, Sergio Baroni
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Publication number: 20120316149Abstract: The present invention relates to compounds: and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases like cancer and inflammation.Type: ApplicationFiled: June 7, 2012Publication date: December 13, 2012Inventors: Ramulu PODDUTOORI, Can WANG, Xianglin ZHAO
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Publication number: 20120309770Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: ApplicationFiled: December 5, 2011Publication date: December 6, 2012Inventors: Kap-Sun Yeung, John F. Kadow, Rajesh Onkardas Bora, Kumaravel Selvakumar
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Publication number: 20120309739Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: November 3, 2010Publication date: December 6, 2012Applicant: ALMAC DISCOVERY LIMITEDInventors: Mark Peter Bell, Colin Roderick O'Dowd, James Samuel Shane Rountree, Graham Peter Trevitt, Timothy Harrison, Mary Melissa McFarland
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Publication number: 20120309768Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.Type: ApplicationFiled: August 13, 2012Publication date: December 6, 2012Applicant: BIONOMICS LIMITEDInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
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Publication number: 20120301552Abstract: A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.Type: ApplicationFiled: December 23, 2011Publication date: November 29, 2012Applicant: JAPAN TOBACCO INC.Inventors: Yuko Shinagawa, Teruhiko Inoue, Toshihiro Kiguchi, Taku Ikenogami, Naoki Ogawa, Kenji Fukuda, Takashi Nakagawa, Masanori Shindo, Yuki Soejima
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Publication number: 20120302566Abstract: The present invention relates to compounds defined by formula (I) wherein the variables R1, R2, R3, m, and n are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are activators of the receptor GPR40 and thus are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: November 30, 2011Publication date: November 29, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank Himmelsbach, Remko Bakker, Matthias Eckhardt, Dieter Hamprecht, Elke Langkopf, Holger Wagner
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Patent number: 8318802Abstract: This invention relates to a stable epoprostenol composition that can be combined with commercially available IV fluids and can be administered in its reconstituted and/or diluted form under ambient conditions of about 15-30° C. for greater than 24 hours. The composition preferably contains (a) epoprostenol or a salt thereof; (b) a alkalinization agent; and (c) a base, such that when reconstituted or in solution, the solution has a pH>11. Methods for making the lyophilized composition are also disclosed.Type: GrantFiled: February 2, 2007Date of Patent: November 27, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventor: Naglesh R. Palepu
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Patent number: 8318799Abstract: The present invention provides a therapeutic agent for substance dependence, which prevents relapse/recurrence of compulsive substance-taking behavior based on craving for addictive substances such as stimulant substances, opioids, barbiturate type anesthetics, hallucinogens, cocaine, hemp, cannabis, alcohol, or volatile organic solvents. (?)-1-(Benzofuran-2-yl)-2-propylaminopentane or a pharmacologically acceptable acid addition salt thereof is useful as a therapeutic agent for substance dependence, which prevents relapse/recurrence of compulsive substance-taking behavior associated with craving for addictive substances.Type: GrantFiled: August 5, 2010Date of Patent: November 27, 2012Assignees: National University Corporation Kyushu University, Fujimoto Co., Ltd.Inventors: Tsuneyuki Yamamoto, Fumio Yoneda, Kazuhiko Morimoto
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Patent number: 8318800Abstract: The present invention relates to a solid pharmaceutical composition for oral administration characterized in that it comprises a benzofuran derivative with antiarrhythmic activity, or one of the pharmaceutically acceptable salts thereof, as an active principle, and a pharmaceutically acceptable nonionic hydrophilic surfactant optionally in combination with one or more pharmaceutical excipients.Type: GrantFiled: December 13, 2007Date of Patent: November 27, 2012Assignee: SanofiInventors: Bernard Abramovici, Jean-Claude Gautier, Jean-Claude Gromenil, Jean-Marie Marrier
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Patent number: 8318801Abstract: The invention relates to a compound represented by the following formula (I): and pharmaceutically acceptable salts, stereoisomers, enantiomers, prodrugs and solvates thereof. The compounds are useful as an agent for enhancing the neurite outgrowth and preventing or treating of diseases associated with HDAC in particular, tumor or cell proliferative diseases. In particular, the compounds of the invention can be used as an agent for anti-cancer, anti-diabetic, and anti-neurodegenerative diseases such as Alzheimer's disease, Huntington's disease, Spinocerebellar Ataxias (SCA), and human spinal muscular atrophy (SMA).Type: GrantFiled: May 24, 2011Date of Patent: November 27, 2012Assignee: Naturewise Biotech & Medicals CorporationInventors: Chung-Yang Huang, Chia-Nan Chen, Wei-Jan Huang, Chia-Wei Lin, Jing-Shi Huang, Li-Ling Chi, Ai-Ling Chen, Chi-Yun Lee, Yu-Chen Huang
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Patent number: 8309545Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.Type: GrantFiled: October 4, 2007Date of Patent: November 13, 2012Assignee: Bionomics LimitedInventors: Bernard Luke Flynn, Jonathan B. Baell, Andrew J. Harvey, Jason Hugh Chaplin, Dharam Paul, Jorgen Alvar Mould
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Publication number: 20120283205Abstract: The present invention relates to a pharmaceutical composition comprising a pharmaceutical agent and a pharmaceutically acceptable carrier, which carrier comprises a protein, for example, human serum albumin and/or deferoxamine. He human serum albumin is present in an amount effective to reduce one or more side effects associated with administration of the pharmaceutical composition. The inventor also provides methods for reducing on or more side effects of administration of the pharmaceutical composition, and methods for enhancing transport and binding of a pharmaceutical agent to a cell.Type: ApplicationFiled: February 7, 2012Publication date: November 8, 2012Inventors: Neil P. DESAI, Patrick Soon-Shiong, Vuong Trieu
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Publication number: 20120283095Abstract: The present invention relates to synergistic mixtures comprising, as active components, one insecticidal compound I selected from the group consisting of carbamates; and one fungicidal compound II selected from the group of strobilurines in synergistic effective amounts.Type: ApplicationFiled: November 29, 2010Publication date: November 8, 2012Applicant: BASF SEInventors: Markus Gewehr, Egon Haden, Lutz Brahm
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Patent number: 8304431Abstract: The present invention relates to the use of compounds and compositions of compounds having D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic activity for the treatment of the underlying dysregulation of the emotional functionality of mental disorders (i.e. affect instability-hypersensitivity-hyperaesthesia-dissociative phenomena-etc). The invention also relates to methods comprising administering to a patient diagnosed as having a neuropsychiatric disorder a pharmaceutical composition containing (i) compounds having D4 antagonistic, partial agonistic or inverse agonistic activity and (ii) compounds having 5-HT2A antagonistic, partial agonistic or inverse agonistic, and (iii) any known medicinal compound and compositions of said compounds. The combined D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic effects may reside within the same chemical or biological compound or in two different chemical and/or biological compounds.Type: GrantFiled: December 2, 2004Date of Patent: November 6, 2012Assignee: PharmaNeuroBoost N.V.Inventor: Erik Buntinx
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Publication number: 20120276051Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.Type: ApplicationFiled: July 9, 2012Publication date: November 1, 2012Applicant: Presidio Pharmaceuticals, Inc.Inventors: Min Zhong, Leping Li
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Publication number: 20120270899Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a cardiovascular disease in an individual using such pharmaceutical compositions.Type: ApplicationFiled: February 3, 2012Publication date: October 25, 2012Inventors: Robin Mark Bannister, John Brew, Suzanne Jane Dilly, Gregory Alan Stoloff, Wilson Caparros-Wanderley