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: 8211897Abstract: The present invention is directed to a method of using compounds of Formula (I) to inhibit Cathepsin B. Specifically the compounds of the present invention are useful as therapeutic agents for the treatment of tumor invasion, metastasis, Alzheimer's Disease, arthritis, inflammatory diseases such as chronic and acute pancreatitis, inflammatory airway disease, and bone and joint disorders, including osteoporosis, osteoarthritis, rheumatoid arthritis, psoriasis, and other autoimmune disorders, liver fibrosis, including liver fibrosis associated with HCV, all types of steatosis (including non-alcoholic steatohepatitis) and alcohol-associated steatohepatitis, non-alcoholic fatty liver disease, forms of pulmonary fibrosis including idiopathic pulmonary fibrosis, pathological diagnosis of interstitial pneumonia following lung biopsy, renal fibrosis, cardiac fibrosis, retinal angiogenesis and fibrosis/gliosis in the eye, schleroderma, and systemic sclerosis.Type: GrantFiled: February 5, 2009Date of Patent: July 3, 2012Assignee: ViroBay, Inc.Inventor: Leslie Holsinger
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Patent number: 8211882Abstract: The present invention discloses methods of modulating the activity of Group I mGluRs using a defined class of benzamide compounds. In one embodiment, methods of modulating the activity of mGluR1 are provided. In another embodiment, methods of modulating the activity of mGluR5 are provided. In still another embodiment, methods of simultaneously modulating the activities of both mGluR1 and mGluR5 are provided. The present invention also provides methods of treating diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of benzamide compounds. The present invention further provides methods of preventing diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of compounds.Type: GrantFiled: March 6, 2009Date of Patent: July 3, 2012Inventors: Richard Delarey Wood, William J Welsh, Sean Ekins, Ni Ai
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Publication number: 20120165386Abstract: The present invention relates to a stable oral pharmaceutical composition comprising atorvastatin or a pharmaceutically acceptable salt thereof and an alkalizing agent, wherein the buffering capacity of the composition is between 2 to 5.Type: ApplicationFiled: December 22, 2011Publication date: June 28, 2012Applicant: RANBAXY LABORATORIES LIMITEDInventors: Ravindra AGARWAL, Parikshit Rameshrao KULKARNI, Ravi KOCHHAR
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Patent number: 8206751Abstract: The subject invention relates to novel compositions containing a diffusion enhancing compound and their use in treating a variety of disorders.Type: GrantFiled: October 31, 2008Date of Patent: June 26, 2012Assignee: Diffusion Pharmaceuticals LLCInventor: John L. Gainer
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Publication number: 20120157420Abstract: A method of administering one or multiple medications to human patients with CNS injury through oral or parenteral (including transdermal, intravenous, subcutaneous, intramuscular) routes. Inflammatory and immunological processes have been shown to cause secondary damage to CNS tissues in individuals with acute CNS injury. The present invention administers one or more of the following medications, which have properties that mitigate the inflammatory and immunological processes that lead to secondary CNS damage, via trans-dermal absorption: a statin compound (e.g., a HMG-CoA reductase inhibitor), a progesterone compound, or a cholinesterase inhibiting compound, among others, either alone or in combination with other compounds.Type: ApplicationFiled: August 31, 2010Publication date: June 21, 2012Inventor: Eric B Schneider
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Publication number: 20120156255Abstract: A polymeric matrix for delivery of an HMG CoA reductase inhibitor such as a statin to tissue such as cardiac tissue in need thereof for the treatment or prevention of a disease or defect such as atrial fibrillation has been developed. In the preferred embodiment, a statin is delivered by means of a patch sutured to cardiac tissue at the time of cardiothoracic surgery. In the most preferred embodiment, the patch is a biodegradable material providing controlled or sustained release over a prolonged period of time, such as a week. Suitable materials include extracellular matrix, or other biodegradable hydrogels or polymeric materials providing sustained or controlled release of statin at the site of application.Type: ApplicationFiled: December 16, 2011Publication date: June 21, 2012Inventors: Jaipal Singh, Nicolas Chronos
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Publication number: 20120157459Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (I): (where n is 0 to 2; p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is an aryl group which is optionally substituted with L or a heterocyclic group which is optionally substituted with L; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is O, S, —NR7—; and R1 to R7 are specific groups), a salt of the compound, or a solvate of the salt or the compound.Type: ApplicationFiled: December 24, 2010Publication date: June 21, 2012Inventors: Akihiro Okano, Naoto Kosuga, Munetaka Ohkouchi, Daido Hotta, Muneyoshi Makabe
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Patent number: 8203003Abstract: Novel 4-fluoropyrrolidine-2-carbonyl fluoride compounds as useful fluorinated intermediates are disclosed. Their preparative methods are also disclosed. Useful applications of the 4-fluoropyrrolidine-2-carbonyl fluorides are shown.Type: GrantFiled: January 8, 2010Date of Patent: June 19, 2012Assignee: UBE Industries, Ltd.Inventors: Teruo Umemoto, Rajendra P. Singh
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Publication number: 20120148689Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of active drugs through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.Type: ApplicationFiled: February 17, 2012Publication date: June 14, 2012Inventor: Todd Maibach
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Publication number: 20120149678Abstract: The invention provides organonitro compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat non-Hodgkin's lymphoma and certain leukemias in a patient. The compounds, compositions, kits, and methods are contemplated to provide a therapeutic benefit in treating non-Hodgkin's lymphoma, chronic lymphocytic leukemia, acute myelogenous leukemia, chronic myelogenous leukemia, and acute lymphoblastic leukemia. Exemplary organonitro compounds described herein include alkyl-substituted and acyl-substituted di-nitroheterocycles.Type: ApplicationFiled: December 9, 2011Publication date: June 14, 2012Inventors: Bryan T. Oronsky, Susan Knox, Jan Scicinski, Shoucheng Ning
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Publication number: 20120141391Abstract: The present invention relates to the use of creatine compounds such as, for example, creatine, creatine phosphate or analogs of creatine, such as creatine-pyruvate, creatine-ascorbate, cyclocreatine, 3 guanidinopropionic acid, guanidinoacetate, homocyclocreatine, guanidino benzoates as energy generating systems and antioxidants for preservation of skin against adverse aging effects and damage secondary to insults such as harmful sun radiations, stress and fatigue. The creatine compounds which can be used in the present method include (1) creatine, creatine phosphate and analogs of these compounds which can act as substrates or substrate analogs for creatine kinase; (2) molecules that mimic the biological activity of creatine (3) molecules that modulate the creatine kinase system.Type: ApplicationFiled: June 29, 2011Publication date: June 7, 2012Applicant: AVICENA GROUP, INC.Inventor: Rima Kaddurah-Daouk
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Publication number: 20120142698Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or X—N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.Type: ApplicationFiled: August 6, 2010Publication date: June 7, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Laura Quaranta, Mathias Stephan Respondek
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Publication number: 20120136006Abstract: 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: ApplicationFiled: February 6, 2012Publication date: May 31, 2012Inventors: 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: 20120129818Abstract: Ortho methoxy phenolic compounds are provided that include methylenedioxyphenyl ferulate and ferulylproline and derivatives thereof. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating cardiovascular diseases, including hypertension, atherosclerosis, coronary heart disease, angina, stroke, and myocardial infarction, are further provided. The compounds are also useful in reducing low-density lipoprotein oxidation, improving or increasing vasodilation, and reducing plaque destabilization in a subject.Type: ApplicationFiled: April 23, 2010Publication date: May 24, 2012Inventor: Desikan Rajagopal
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Publication number: 20120129827Abstract: The present invention relates to novel derivatives of 1-alkyl-6-oxo-piperidine-3-carboxylic acids and 1-alkyl-5-oxo-pyrrolidine-3-carboxylic acids represented by Formula I: wherein n is an integer of 1 or 2; R1, R2, R3, and R4 are each independently selected from the group consisting of hydrogen and methyl; X is selected from the group consisting of oxygen and nitrogen; and R5 is hydrogen or a C1-C7 linear or branched acyclic hydrocarbon group, or R5 together with X form a 3- to 8-membered heterocyclic hydrocarbon group, and their uses as cooling compounds.Type: ApplicationFiled: November 22, 2010Publication date: May 24, 2012Inventor: Arkadiusz Kazimierski
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Publication number: 20120128660Abstract: The present invention relates to compounds, compositions, methods and/or kits for determining and/or predicting and/or diagnosing and/or treating restenosis in a patient.Type: ApplicationFiled: June 2, 2010Publication date: May 24, 2012Applicant: UNIVERSITY OF SASKATCHEWANInventor: Kailash Prasad
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Patent number: 8183280Abstract: The present invention concerns compounds, according to general formula (I), which find utility preferably for the treatment of cancer.Type: GrantFiled: August 31, 2006Date of Patent: May 22, 2012Assignee: Vantia LimitedInventors: David Michael Evans, John Horton, Julie Elizabeth Trim
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Publication number: 20120121711Abstract: A nanosphere or microsphere drug carrier, formulations comprising the drug carrier and the preparation method of the formulations and the use of the carrier are disclosed. The carrier comprises a biodegradable methoxy end-capped polyethylene glycol-polylactide block copolymersor a derivative thereof represented by formula (I) as the main carrier material: CH3O—[CH2—CH2—O]m—[C(O)—CH(CH3)—O]n—R (I).Type: ApplicationFiled: July 30, 2010Publication date: May 17, 2012Applicant: XI'AN LIBANG MEDICAL TECHNOLOGY CO., LTD.Inventors: Renle Hu, Jiucheng Wang, Tao Chen, Hua Liang, Duohao Ding, Yaqi Jiao
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Publication number: 20120121724Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of nitroglycerin, as well as other therapeutic agents either with or without nitroglycerin, through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.Type: ApplicationFiled: January 20, 2012Publication date: May 17, 2012Inventor: Todd Maibach
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Publication number: 20120122950Abstract: New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to 1-(sulfonyl)-N-phenyl-pyrrolidine 2-carboxamides which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.Type: ApplicationFiled: December 22, 2011Publication date: May 17, 2012Inventors: JOSEP CASTELLS BOLIART, David Enrique Miguel Centeno, Marta Pascual Gilabert
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Publication number: 20120122839Abstract: 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: ApplicationFiled: January 17, 2012Publication date: May 17, 2012Applicant: Priaxon AGInventors: Christoph BURDACK, Cedric Kalinski, Vladimir Khazak, Gunther Ross, Lutz Weber
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Publication number: 20120121698Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising EPA and one or more cardiovascular agents, and to therapeutic methods for treating various diseases and disorders using the same.Type: ApplicationFiled: April 29, 2010Publication date: May 17, 2012Applicant: AMARIN PHARMA, INC.Inventors: Mehar Manku, Jonathan Rowe
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Patent number: 8178125Abstract: Oral formulations of G-2MePE including microemulsions, coarse emulsions, liquid crystals, tablets and encapsulated forms of G-2MePE have improved bioavailability than conventional aqueous formulations. In particular, microparticles, nanoparticles and microemulsions can exhibit great neuroprotective effects after oral administration. In a microemulsion formulation, G-2MePE can nearly completely inhibit cerebral infarction in an animal model of stroke even after the stroke had been initiated. Thus, improved oral formulations can be desirably used to treat a variety of neurodegenerative conditions with improved convenience and improved efficacy.Type: GrantFiled: February 14, 2011Date of Patent: May 15, 2012Assignee: Neuron Pharmaceuticals LimitedInventors: Jingyuan Wen, Gregory Brian Thomas, Mike John Bickerdike
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Publication number: 20120114696Abstract: This disclosure relates to materials and methods for inhibiting Botulinum neurotoxin, and more particularly to materials and methods for inhibiting the zinc endopeptidase of Botulinum neurotoxin serotypes A, D and/or E (BoNTA, BoNTD and/or BoNTE).Type: ApplicationFiled: July 29, 2010Publication date: May 10, 2012Inventors: Yuan-Ping Pang, Jewn Giew Park, Shaohua Wang, Anuradha Vummenthala, Rajesh K. Mishra, Jon Davis, Charles B. Millard, James J. Schmidt
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Publication number: 20120114740Abstract: Disclosed are formulations comprising multivesicular liposomes and one or more non-steroidal anti-inflammatory drugs which minimize the side effects of unencapsulated non-steroidal anti-inflammatory drugs while maintaining or improving efficacy. Methods of making and administering the formulations comprising multivesicular liposomes and one or more non-steroidal anti-inflammatory drugs and their use as medicaments are also provided.Type: ApplicationFiled: October 27, 2011Publication date: May 10, 2012Applicant: PACIRA PHARMACEUTICALS, INCInventors: Louie Daniel Garcia, Liangjin Zhu, William Joseph Lambert, Gary Patou
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Patent number: 8173694Abstract: Provided are agents and methods for use in depleting serum amyloid P component (SAP) from a patient in need thereof.Type: GrantFiled: March 16, 2009Date of Patent: May 8, 2012Assignee: Pentraxin Therapeutics LimitedInventor: Mark B. Pepys
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Publication number: 20120107400Abstract: A pH dependent drug delivery system comprising a pH sensitive graft copolymer, a therapeutically active agent and other pharmaceutically acceptable ingredients. More specifically, a composition which is capable of suppressing the drug release in the acidic pH prevalent in the stomach and releasing the drug over an extended period of time at pH prevalent in the intestinal region.Type: ApplicationFiled: March 5, 2010Publication date: May 3, 2012Inventors: Ramesh Muthusamy, Mohan Gopalkrishna Kulkarni
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Publication number: 20120107401Abstract: Osteoconductive matrices and methods are provided that have one or more statins disposed therein. The matrices may be injected into a fracture site. The osteoconductive matrices provided allow for sustain release of the statin and facilitate bone formation and repair of the fracture site.Type: ApplicationFiled: October 27, 2010Publication date: May 3, 2012Applicant: WARSAW ORTHOPEDIC, INC.Inventor: William F. McKay
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Publication number: 20120108639Abstract: The present invention provides a compound having excellent regulating action on blood lipid level that is represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein, in one embodiment, A represents a 5-membered nitrogen-containing aromatic heterocyclyl group; R1 represents COOH; each R2 represents an alkyl; each R3 represents an optionally substituted phenyl, an optionally substituted phenylalkyl; m represents 0, 1, 2, or 3; n represents 0 or 1; each of R4, R5, R6, and R7 represents H, an alkyl; and B represents an optionally substituted naphthyl, an optionally substituted aromatic heterocyclyl, or a group represented by the following formula (II) wherein each of B1 and B2 represents an optionally substituted phenyl or an optionally substituted aromatic heterocyclyl.Type: ApplicationFiled: July 7, 2009Publication date: May 3, 2012Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Keiko Suzuki, Takahiro Yamaguchi, Akihiro Tamura, Tomohiro Nishizawa, Mitsuhiro Yamaguchi
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Publication number: 20120107383Abstract: Osteoconductive matrices and methods are provided that have one or more statins disposed in calcium phosphate particles. The matrices may be injected into a fracture site. The osteoconductive matrices provided allow for sustained release of the statin and facilitate bone formation and repair of the fracture site.Type: ApplicationFiled: October 27, 2010Publication date: May 3, 2012Applicant: WARSAW ORTHOPEDIC, INC.Inventor: William F. McKay
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Publication number: 20120108517Abstract: Various agents are described to denerve, modulate, or otherwise affect the renal nerves and other neural tissue. Also, various delivery devices are described to deliver an agent locally to the renal nerves. The delivery devices are positioned in the renal artery and penetrate into the wall of the renal artery to deliver the agent to the renal nerves. The delivery devices may be used to deliver the agent according to longitudinal position, radial position, and depth of the renal nerves relative to the renal artery. In addition, various methods are described to denervate, modulate, or otherwise affect the renal nerves and other neural tissue.Type: ApplicationFiled: April 28, 2011Publication date: May 3, 2012Inventors: Michael A. EVANS, Kondapavulur T. VENKATESWARA-RAO, Emily A. STEIN
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Patent number: 8168631Abstract: Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: February 3, 2009Date of Patent: May 1, 2012Assignee: Allergan, Inc.Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Rong Yang, Cédric Chauvignac
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Publication number: 20120100234Abstract: Compositions are provided that provide improved nasal moisture, clarity, and lubrication. Compositions are oil-in-glycerin emulsions that include a surfactant promoting emulsification of a hydrophobic or otherwise water insoluble bioactive agent. The compositions are used in methods of promoting improved nasal moisture and reduction in nasal congestion.Type: ApplicationFiled: October 20, 2011Publication date: April 26, 2012Inventors: John E. Kulesza, Jeffrey Katz
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Publication number: 20120101080Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C?CH, C?N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.Type: ApplicationFiled: June 25, 2010Publication date: April 26, 2012Applicant: BioVersys AGInventors: Ronald Schoenmakers, Wilfried Weber, Marc Gitzinger, Martin Fussenegger, Marcel Tigges, Peter Schneider
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Patent number: 8163727Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: GrantFiled: December 18, 2009Date of Patent: April 24, 2012Assignee: AstraZeneca ABInventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Patent number: 8163793Abstract: The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: April 16, 2010Date of Patent: April 24, 2012Assignee: Hoffman-La Roche Inc.Inventors: Rubén Alvarez Sánchez, David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Peter Hartman, Guido Hartmann, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher
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Patent number: 8163796Abstract: A novel treatment regimen is described for the control and elimination of cancer cell populations including cancer stem cells. The disclosed protocol consists of a pretreatment step followed by a treatment step. The pretreatment step sensitizes cancer cells to apoptosis by altering their intracellular oxidation-reduction state via reduced glutathione depletion. The treatment step involves the sequential administration of a cancerostatic dicarbonyl compound to induce apoptosis. The use of nanoparticle delivery systems further enhances both the pharmacokinetic and pharmacodynamic properties of the pretreatment compounds and the cancerostatic dicarbonyls. Since the pretreatment and treatment compounds are carefully selected and delivered, normal cells are not affected and side effects are kept to a minimum.Type: GrantFiled: July 20, 2010Date of Patent: April 24, 2012Assignee: BioChemical Solutions, LLCInventors: Morris A. Johnson, Michael M. Smits
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Publication number: 20120095072Abstract: Crystalline sodium atorvastatin, compositions containing the same and methods for the production thereof.Type: ApplicationFiled: December 13, 2011Publication date: April 19, 2012Applicants: ZHEJIANG NEO-DANKONG PHARMACEUTICAL CO. LTD., ARROW INTERNATIONAL LIMITEDInventors: Kailan ZHOU, Hong LIU, Zhirong CHEN, Huabin HONG, Yang SUN, Yunde WANG, Jiangchun PAN
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Publication number: 20120093922Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising EPA and one or more cardiovascular agents, and to therapeutic methods for treating various diseases and disorders using the same.Type: ApplicationFiled: April 29, 2010Publication date: April 19, 2012Applicant: AMARIN CORPORATION PLCInventors: Mehar Manku, Jonathan Rowe
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Publication number: 20120095003Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.Type: ApplicationFiled: October 14, 2011Publication date: April 19, 2012Applicant: XenoPort, Inc.Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
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Publication number: 20120093923Abstract: A method and apparatus for delivering a plurality of medicaments in a single delivery vehicle for the management of co-morbid diseases, illnesses and conditions. The present invention provides a novel delivery process for many medicaments. Medicaments may be encapsulated and stored separately within a larger capsule until the time of ingestion, consumption, or the like. Benefits of the present invention include maintaining separation of distinct ingredients within a single capsule and the capability to control the time release of multiple ingredients within the capsule.Type: ApplicationFiled: September 19, 2011Publication date: April 19, 2012Applicant: INNERCAP Technologies, Inc.Inventors: Frederick H. MILLER, James H. Ruble, Gary D.E. Pierce
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Publication number: 20120094973Abstract: The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetes and ischemia, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier.Type: ApplicationFiled: December 21, 2011Publication date: April 19, 2012Applicant: NATIONAL TAIWAN UNIVERSITYInventors: Yueh-Hsiung Kuo, Ming-Jai Su
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Publication number: 20120087928Abstract: The invention provides compositions and methods of predicting a subject's risk of developing age-related macular degeneration (AMD) and methods of treating, delaying, or preventing the development and progression of AMD.Type: ApplicationFiled: October 28, 2011Publication date: April 12, 2012Inventor: Kameran Lashkari
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Publication number: 20120087953Abstract: The present invention provides a pharmaceutical composition comprising at least one active pharmaceutical ingredient comprising sulphonylurea moiety, wherein the at least one active pharmaceutical ingredient comprising sulphonylurea moiety is intimately mixed with a basic agent. The weight ratio of the basic agent and the at least one active pharmaceutical ingredient comprising sulphonylurea moiety is from 2.5:1 to 50:1, preferably from 2.5:1 to 25:1, more preferably from 3.5:1 to 15:1, yet more preferably from 3.5:1 to 10:1. The pharmaceutical composition can be obtained by simply mixing active pharmaceutical ingredient comprising sulphonylurea moiety and the basic agent in the aforementioned weight ratio, optionally in the presence of the granulation liquid. Alternatively, the pharmaceutical composition can be obtained by at least partially or fully dissolving the compounds in the granulation liquid or solvent, and at least partly precipitating them.Type: ApplicationFiled: March 3, 2010Publication date: April 12, 2012Applicant: LEK PHARMACEUTICALS D.D.Inventors: Sebastjan Reven, Miha T. Jaklic
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Patent number: 8153623Abstract: Compounds of formula (I), pharmaceutical compositions thereof, and methods for treatment using the same.Type: GrantFiled: August 4, 2010Date of Patent: April 10, 2012Assignee: Convergence Pharmaceuticals LimitedInventors: Giuseppe Alvaro, David Amantini, Markus Bergauer, Francesca Bonetti, Roberto Profeta
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Patent number: 8153821Abstract: The present invention related to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to novel salts thereof, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).Type: GrantFiled: November 30, 2009Date of Patent: April 10, 2012Assignee: Targacept, Inc.Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Timothy J. Cuthbertson, Craig Harrison Miller, Joseph Pike Mitchener, Jr.
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Publication number: 20120083500Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: December 8, 2011Publication date: April 5, 2012Inventors: Li CHEN, Michael Patrick DILLON, Lichun FENG, Minmin YANG
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Publication number: 20120082640Abstract: The invention provides small molecule mimics of the Smac peptide that are dimer- or dimer-like compounds having two amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.Type: ApplicationFiled: October 4, 2010Publication date: April 5, 2012Inventors: Gunnar J. Hanson, David Thomas, Nizal Chandrakumar, Susan Harran
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Patent number: 8148419Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: November 21, 2006Date of Patent: April 3, 2012Assignee: Bayer Cropscience AGInventors: Pierre-Yves Coqueron, Darren James Mansfield, Philippe Desbordes, Heiko Rieck, Pierre Genix, Alain Villier, Marie-Claire Grosjean-Cournoyer
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Publication number: 20120077779Abstract: Disclosed are peptide-based compounds that include boronic acid or cyano functionality, which efficiently and selectively inhibit fibroblast activation protein alpha. Among other therapeutic utilities, the peptide-based compounds may be useful for the treatment of cancer.Type: ApplicationFiled: July 6, 2011Publication date: March 29, 2012Applicant: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-Sen Lai