Polycyclo Ring System Having The Additional Oxygen Hetero Ring As One Of The Cyclos Patents (Class 514/254.11)
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Publication number: 20120232094Abstract: The present invention describes phenylpiperazinyl alpha adrenergic antagonists that corresponds to the formula (I) which selectively act on the alpha 1A/alpha 1D subtypes, where its selectivity index in comparison to alpha 1B subtype is, at minimum, 1700 for the alpha 1A subtype and 10000 for the alpha 1D subtype, being therefore useful for the treatment of the lower urinary tract symptoms, including the benign prostatic hyperplasia treatment in mammals, preferentially humans. Also described are pharmaceutical compositions containing said compounds and methods for its preparation.Type: ApplicationFiled: May 15, 2012Publication date: September 13, 2012Inventors: Luiz Antonio Soares Romeiro, Carlos Alberto Manssour Fraga, Eliezer de Jesus De Lacerda Barreiro, Cláudia Lúcia Martins da Silva, Ana Luisa Palhares Miranda, Eduardo Vera Tibiriçá, Fernanda Carla Ferreira de Brito, Helena Carla Castro Cardoso de Almeida, François Germain Noël
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Publication number: 20120220518Abstract: A therapeutic agent delivery system includes a therapeutic agent delivery platform and a therapeutic guest agent. The therapeutic agent delivery platform is capable of being implanted in a tissue being treated. The platform includes a substrate and at least one host molecule coupled to the substrate. The therapeutic guest agent is capable of reversibly coupling with the host molecule when administered to the tissue being treated. The reversible coupling is defined by the binding affinity between the host molecule and the therapeutic guest agent. The therapeutic guest agent is delivered at a rate determined by the affinity release rate between the host molecule and the therapeutic guest agent. The degradation rate of the therapeutic guest agent may be slower than the affinity release rate between the host molecule and the therapeutic guest agent.Type: ApplicationFiled: June 3, 2010Publication date: August 30, 2012Applicant: CASE WESTERN RESERVE UNIVERSITYInventors: Horst A. von Recum, ThimmaReddy Thatiparti, Julius N. Korley, Travis Sill, Iryna Makovey
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Publication number: 20120220457Abstract: Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to imidazopyridine compounds, synthesis thereof, and methods of using same. Disclosed herein are various imidazo[1,2-a]pyhdine compounds and methods of using the novel compounds to treat or prevent tuberculosis in a subject or to inhibit fungal growth on plant species. Other embodiments include methods of synthesizing imidazo [1,2- a]pyridine compounds, such as the disclosed imidazo[1,2-a]pyridine compounds.Type: ApplicationFiled: November 5, 2010Publication date: August 30, 2012Applicants: Dow AgroSciences LLC, University of Notre Dame du LacInventors: Marvin J. Miller, Garrett C. Moraski, Lowell D. Markley, George E. Davis
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Publication number: 20120214770Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.Type: ApplicationFiled: May 1, 2012Publication date: August 23, 2012Applicant: BIONOMICS LIMITEDInventors: JASON HUGH CHAPLIN, GURMIT SINGH GILL, DAMIAN WOJCIECH GROBELNY, BERNARD LUKE FLYNN, GABRIEL KREMMIDIOTIS
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Publication number: 20120190690Abstract: The present invention relates to the treatment of an individual afflicted with a weight disorder, particularly obesity, the instant treatment comprising administering to the individual an effective amount of eltoprazine or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 30, 2010Publication date: July 26, 2012Applicant: MERZ PHARMA GmbH & CO. KGaAInventors: Barbara Valastro, Lutz Franke
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Patent number: 8227468Abstract: The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof. Also, the present invention provides a pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable diluent or carrier. The present invention further provides methods for treating abdominal aortic aneurysm, plaque instability, atherosclerosis, or autoimmune disorders such as rheumatoid arthritis, psoriasis, and lupus comprising administering a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable diluent or carrier.Type: GrantFiled: October 14, 2011Date of Patent: July 24, 2012Assignee: Eli Lilly and CompanyInventors: Gary G. Deng, Konstantinos Gavardinas, Prabhakar Kondaji Jadhav, Euibong Jemes Kim, Matthew Allen Schiffler
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Patent number: 8227473Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.Type: GrantFiled: July 17, 2009Date of Patent: July 24, 2012Assignee: Lixte Biotechnology, Inc.Inventors: John S. Kovach, Francis Johnson
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Patent number: 8222255Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.Type: GrantFiled: September 25, 2008Date of Patent: July 17, 2012Assignees: Merck Sharp & Dohme Corp., Scynexis, Inc.Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, legal representative, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
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Publication number: 20120178735Abstract: Provided is a 2H-chromene compound or a derivative thereof which has an excellent S1P1 agonist action. The 2H-chromene compound or derivative is particularly useful for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells.Type: ApplicationFiled: February 15, 2012Publication date: July 12, 2012Applicant: ASTELLAS PHARMA INC.Inventors: Hironori Harada, Kazuyuki Hattori, Kazuya Fujita, Sunao Imada, Tatsuaki Morokata
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Publication number: 20120165308Abstract: The present invention provides compounds of the formula (I) or a pharmaceutically acceptable salt, ester or prodrug thereof.Type: ApplicationFiled: February 13, 2012Publication date: June 28, 2012Applicant: UNIVERSITY OF KENTUCKYInventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
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Publication number: 20120157463Abstract: The present invention relates to chromone derivatives, their preparation, their pharmaceutical compositions and their application as D3 dopaminergic ligands as a medicament for disorders of the central nervous system.Type: ApplicationFiled: August 31, 2010Publication date: June 21, 2012Applicant: PIERRE FABRE MEDICAMENTInventors: Pierre Sokoloff, Thierry Imbert, Jean-François Patoiseau, Jean-Pierre Rieu
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Publication number: 20120157373Abstract: Antimicrobial compounds, such as silanol or alcohol, include a protecting or leaving group that can protect the compound from degradation during the process of preparing a medical device containing the compound or reduce the volatility of the compound relative to its counterpart without the leaving group. Nearly any hydrolysable leaving group may be employed. The leaving group may be an agent that may serve a therapeutic function in addition to protecting or retaining the antimicrobial agents.Type: ApplicationFiled: February 29, 2012Publication date: June 21, 2012Applicant: MEDTRONIC, INC.Inventors: Paul Hsien-Fu Wu, Catherine E. Taylor, Linnus Cheruiyot, Jianwei Li, Terese A. Bartlett, Matt Bergan
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Publication number: 20120149665Abstract: A pharmaceutical composition of a tubulin polymerisation inhibitor and an mTOR inhibitor and a method of treating proliferative disease with a combination of a tubulin polymerisation inhibitor and an mTOR inhibitor.Type: ApplicationFiled: August 25, 2010Publication date: June 14, 2012Applicant: Bionomics LimitedInventors: Gabriel Kremmidiotis, David Bibby, Annabell Leske
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Publication number: 20120149716Abstract: Methods of treating, preventing, and managing tuberculosis and other related disorders are disclosed. The methods comprise the administration of a PDE4 modulator, or a pharmaceutically acceptable salt, solvate, hydrate, clathrate, stereoisomer, or prodrug thereof, optionally in combination with a second active agent and/or other conventional therapies. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in such methods are also disclosed.Type: ApplicationFiled: February 9, 2010Publication date: June 14, 2012Inventor: Jerome B. Zeldis
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Patent number: 8198280Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: December 16, 2010Date of Patent: June 12, 2012Assignee: Merck Serono SAInventors: Dominique Swinnen, Jerome Gonzalez
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Publication number: 20120142682Abstract: Compounds that inhibit bacterial virulence factors from the mono-ADP-ribosyltransferase (mART) family of toxins have been identified that are not toxic to cells or the producing bacterial pathogen. These compounds have great potential as antivirulence agents for treating many bacterial infections and disease states.Type: ApplicationFiled: December 2, 2011Publication date: June 7, 2012Applicant: UNIVERSITY OF GUELPHInventor: Allen Rod Merrill
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Patent number: 8193196Abstract: Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin ? and rifaximin ? useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.Type: GrantFiled: February 27, 2006Date of Patent: June 5, 2012Assignee: Alfa Wassermann, S.p.A.Inventors: Giuseppe Claudio Viscomi, Manuela Campana, Donatella Confortini, Maria Miriam Barbanti, Dario Braga
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Publication number: 20120136005Abstract: The present invention relates to the treatment of an individual afflicted with certain forms of anxiety, the instant treatment comprising administering to the individual an effective amount of eltoprazine or a pharmaceutically acceptable salt thereofType: ApplicationFiled: June 30, 2010Publication date: May 31, 2012Applicant: MERZ PHARMA GmbH & CO. KGaAInventors: Barbara Valastro, Lutz Franke, Andreas Gravius
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Patent number: 8188089Abstract: Compounds of Formula I are described: preferably subject to the proviso that either (a) R2 and R3 together form —O—CH(R10)—O—, or (b) R5 and R6 together form —O—CH(R10)—O—, wherein R10 is H, halo, or loweralkyl. Pharmaceutical salts, formulations, and methods of using the same in the treatment of cancer are also described.Type: GrantFiled: December 20, 2006Date of Patent: May 29, 2012Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Linyi Wei, Kenneth F. Bastow, Arnold Brossi, Tian-Shung Wu
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Publication number: 20120129816Abstract: The present invention relates to novel aryl sulfonamide amine compounds of the formula (I), their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates described herein and pharmaceutically acceptable compositions containing them.Type: ApplicationFiled: March 3, 2009Publication date: May 24, 2012Applicant: Suven Life Sciences LimitedInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Rama Sastri Kambhampati, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Venkateswarlu Jasti
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Patent number: 8183234Abstract: Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidinocarbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.Type: GrantFiled: June 30, 2010Date of Patent: May 22, 2012Assignee: Piramal Life Sciences LimitedInventors: Bansi Lal, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More, Anil Ghate, Jacqueline Trivedi, Sapna Parikh
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Patent number: 8183239Abstract: The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; sleep/wake disorders; cardiovascular disease; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.Type: GrantFiled: October 27, 2006Date of Patent: May 22, 2012Assignee: Janssen Pharmaceutica NVInventors: Pascal Bonaventure, Nicholas I. Carruthers, Wenying Chai, Curt A. Dvorak, Jill A. Jablonowski, Dale A. Rudolph, Mark Seierstad, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong
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Publication number: 20120115850Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.Type: ApplicationFiled: May 10, 2011Publication date: May 10, 2012Inventors: Oren Becker, Rosa Melendez, Yael Marantz, Anurag Sharadendu, Merav Fichman, Mercedes Lobera, Hanoch Senderowitz, Srinivasa Rao Cheruku, Sharon Shacham, Laurence Wu, Ashis Saha, Pini Orbach, Dale S. Dhanoa
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Publication number: 20120115778Abstract: Methods for treating eating disorders associated with excessive weight gain, suppressing appetite, reducing body weight, or treating obesity in an animal by administering one or more antagonists of the serotonin Htr1a or Htr2b receptor, or a Tph2 inhibitor are provided, or combinations thereof.Type: ApplicationFiled: July 15, 2010Publication date: May 10, 2012Applicant: The Trustees of Columbia University in the City of New YorkInventors: Gerard Karsenty, Vijay Yadav, Franck Oury
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Patent number: 8173660Abstract: The invention relates to a novel process for the preparation of 3-amino-8-(1-piperazinyl)-2H-1-benzopyran-2-one, a broad spectrum 5-HT receptor binding ligand having potent 5-HT1A-agonistic as well as 5-HT1D-antagonistic activity. The invention also relates to novel salts and solvates, in particular hydrates of salts of said compound, as well as to their use as medicaments.Type: GrantFiled: July 2, 2010Date of Patent: May 8, 2012Assignee: Solvay Pharmaceuticals B.V.Inventor: Cornelis Bakker
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Publication number: 20120095020Abstract: The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof. Also, the present invention provides a pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable diluent or carrier. The present invention further provides methods for treating abdominal aortic aneurysm, plaque instability, atherosclerosis, or autoimmune disorders such as rheumatoid arthritis, psoriasis, and lupus comprising administering a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable diluent or carrier.Type: ApplicationFiled: October 14, 2011Publication date: April 19, 2012Applicant: Eli Lilly and CompanyInventors: Gary G. DENG, Konstantinos GAVARDINAS, Prabhakar Kondaji JADHAV, Euibong Jemes KIM, Matthew Allen SCHIFFLER
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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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Patent number: 8158623Abstract: The invention discloses a new use of a class of heptacyclic compounds in the preparation of formulations for the prevention and treatment of diabetes and metabolic syndromes; the present invention also discloses a new class of heptacyclic compounds; the present invention also discloses a process for preparing the heptacyclic compounds and a composition containing the same. The heptacyclic compounds of the present invention can be used to effectively preventing or treating diseases such as diabetes and metabolic syndromes.Type: GrantFiled: May 29, 2007Date of Patent: April 17, 2012Assignee: Shanghai Institute of Materia Medica Chinese Academy of SciencesInventors: Jianhua Shen, Ying Leng, Hualiang Jiang, Junhua Chen
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Publication number: 20120088671Abstract: The present invention provides polyphenolic compositions derived from a plant that inhibit the formation of a biofilm. Also provided are combinations that comprise at least one phenolic phytochemical and at least one antimicrobial agent that inhibit the growth of an established biofilm. Further, the present invention provides methods for inhibiting the formation and growth of biofilms.Type: ApplicationFiled: October 6, 2011Publication date: April 12, 2012Applicant: BOARD OF TRUSTEES UNIVERSITY OF ARKANSASInventors: Cassandra L. Quave, Mark S. Smeltzer, Cesar M. Compadre, Howard Hendrickson
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Publication number: 20120083488Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).Type: ApplicationFiled: June 9, 2010Publication date: April 5, 2012Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
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Publication number: 20120078165Abstract: A therapeutic agent eluting element includes an elongate body member and one or more therapeutic agents elutable from the body member. The elongate body member is configured to be implanted subcutaneously along side of a therapy delivery element. The elongate body member may be formed from a polymeric material, and the agent eluting element may consist essentially of the body member and the one or more therapeutic agents. The therapeutic agent eluting element may be a part of a system or kit that includes a therapy delivery element and a tunneling tool, such as a dilator, sheath, catheter passer, or the like.Type: ApplicationFiled: December 5, 2011Publication date: March 29, 2012Applicant: MEDTRONIC, INC.Inventor: Thomas C. Bischoff
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Publication number: 20120077775Abstract: Disclosed are macrocyclic compounds of formulae I-V, which are analogs of the pochonin resorcylic acid lactones, and processes for the preparation of the compounds. The compounds disclosed are useful as inhibitors of kinases and Heat Shock Protein 90 (HSP 90). Also disclosed are pharmaceutical compositions comprising an effective kinase-inhibiting amount or an effective HSP90-inhibiting amount of the compounds and methods for the treatment of disorders that are mediated by kinases and HSP90.Type: ApplicationFiled: September 23, 2011Publication date: March 29, 2012Applicants: LE CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE STRASBOURGInventors: Nicolas WINSSINGER, Sofia BARLUENGA, Martin KARPLUS
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Publication number: 20120077818Abstract: Provided herein are methods of and compositions for, treating, preventing and managing various neurological disorders. The methods comprise administering a transnorsertraline in combination with a serotonin receptor IA agonist, antagonist or modulator.Type: ApplicationFiled: May 12, 2010Publication date: March 29, 2012Applicant: Sunovion Pharmaceuticals Inc.Inventors: Una Campbell, Judith Dunn
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Publication number: 20120071495Abstract: Methods for treating neurological or mental disorders in humans and the symptoms associated therewith are provided by administering eltoprazine and/or related compounds. In some embodiments, specific symptoms are treated by administering eltoprazine and/or a related compound in an effective amount to ameliorate the symptoms. Of particular significance are symptoms that are associated with cognitive dysfunction where eltoprazine will improve the symptoms and the disorder associated with that symptom. Of particular interest are non-ADHD-associated inattention, hyperactivity and impulsiveness. The methods provided herein are especially useful for improving functional recovery after CNS injury such as stroke where improved cognitive function will facilitate the acquisition of learning and memory of rehabilitative tasks.Type: ApplicationFiled: November 23, 2011Publication date: March 22, 2012Applicant: Psychogenics, Inc.Inventors: Emer Leahy, Mark Day
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Publication number: 20120071487Abstract: Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof.Type: ApplicationFiled: May 26, 2010Publication date: March 22, 2012Inventors: Vladimir Kogan, Lev Tabachnik
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Publication number: 20120070494Abstract: A method for treating Attention Deficit/Hyperactivity Disorder (ADHD) in humans and the symptoms associated therewith, inattentiveness, and hyperactivity with impulsivity, using eltoprazine and related compounds is provided.Type: ApplicationFiled: August 16, 2011Publication date: March 22, 2012Applicant: Psychogenics, Inc.Inventors: Daniela Brunner, Daniel W. Goodman
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Publication number: 20120052292Abstract: The present invention relates to coatings comprising polyethylene glycol and at least one polyphenolic polymer. In particular, the polyphenolic polymer could be selected from the group consisting of tyrosine-derived polyarylates, linear polyesteramides, dihydroxybenzoate polymers, and resorcinol-derived polymers. The coating of the present invention may also include a drug, such as an antibiotic. The coatings of the present invention are suitable for use as coatings for medical devices, such as orthopedic pins or stents.Type: ApplicationFiled: August 25, 2011Publication date: March 1, 2012Applicant: TYRX PHARMA, INC.Inventors: Satish Pulapura, Qing Ge
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Publication number: 20120046238Abstract: A method for treating an infection with a virus. The method includes administering to a subject in need thereof an effective amount of one or more coumarin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, and X are defined herein. Also disclosed is a pharmaceutical composition including a coumarin compound.Type: ApplicationFiled: November 10, 2011Publication date: February 23, 2012Applicant: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Tsu-An Hsu, Jiann-Yih Yeh, Jim-Tong Horng, Shin-Ru Shih, Sui-yuan Chang, Yu-Sheng Chao
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Publication number: 20120046277Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted bromopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R3 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloakyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, wherein R2 and R3 do not exist when carbon atoms respectively adjacent to R2: and R3 form a double bond, and there is noType: ApplicationFiled: March 9, 2010Publication date: February 23, 2012Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Taiichi Ohra
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Publication number: 20120035149Abstract: Contemplated compounds, compositions, and methods of prokineticin antagonists are presented where a prokineticin antagonist is used in the treatment and prevention of various conditions and disorders, and especially type II diabetes.Type: ApplicationFiled: December 16, 2009Publication date: February 9, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Qun-Yong Zhou, Jia-Da Li, Qi Huang
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Publication number: 20120035170Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.Type: ApplicationFiled: August 22, 2011Publication date: February 9, 2012Inventors: José Maria Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
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Publication number: 20120027853Abstract: This invention relates to a process for preparing a pharmaceutical composition comprising four antitubercular drugs: rifampin or a pharmaceutically acceptable salt thereof, isoniazid or a pharmaceutically acceptable salt thereof, pyrazinamide or a pharmaceutically acceptable salt thereof and ethambutol or a pharmaceutically acceptable salt thereof, wherein rifampin and isoniazid are in separate layers. The invention also provides a pharmaceutical composition prepared therefrom having advantageous stability and bioavailability.Type: ApplicationFiled: July 29, 2010Publication date: February 2, 2012Applicants: Taiwan Biotech Co., Ltd.Inventors: Li-Heng Pao, Nion-Heng Shiao, Kuo-Hua Yang, Jui-Ming Chou
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Publication number: 20120022062Abstract: The present invention relates to flavanoid compounds of general formula (X1) wherein: R1 is selected from a group consisting of morpholinyl, N-methyl piperizinyl, piperidinyl and N,N?-dimethylamino groups, and n ranges from 3 to 6, and process for preparation thereof. The present invention relates to the demonstration of anti Helicobacter pylori activity and gastric antisecretory activity of semisynthetically designed flavonoid compounds, to be used for the prevention and treatment of gastroduodenal disorders in general and peptic ulcer diseases in particular. The present invention also relates to a hetero-dimeric bi-functional molecule that can be used as monotherapy substituting/replacing/overcoming currently used triple/quadruple therapy, thereby implicating/anticipating/envisaging its commercial applicability.Type: ApplicationFiled: February 26, 2010Publication date: January 26, 2012Inventors: Pratap Kumar Dab, Suchandra Goswami, Annalaskhmi Chinniah, Janaswamy Madusudana Rao, Suresh Babu Katragadda
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Patent number: 8101605Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.Type: GrantFiled: December 3, 2010Date of Patent: January 24, 2012Assignee: Aquinox Pharmaceuticals Inc.Inventors: Lloyd Mackenzie, Tom MacRury, Curtis Harwig, Jeremy Pettigrew, Noor Aini Bhatti, Sam Place, Paul Bird, Vladimir Khlebnikov, Rudong Shan
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Publication number: 20110311624Abstract: Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.Type: ApplicationFiled: April 16, 2010Publication date: December 22, 2011Applicant: PHARMACYCLICS, INC.Inventors: David J. LOURY, Joseph J. BUGGY, Tarak D. MODY, Erik J. VERNER, Norbert PURRO, Sriram BALASUBRAMANIAN
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Patent number: 8076326Abstract: The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein X is a bond or a group N—R4; R1 is hydrogen or methyl; R2 is hydrogen or methyl; R3 is hydrogen, C1-C3 alkyl, fluorine, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl, C3-C4 cycloalkyl, or C3-C4 cycloalkyl-CH2—; R5 is hydrogen, fluorine, chlorine, C1-C2 alkyl, fluorinated C1-C2 alkyl, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R6 is hydrogen, fluorine or chlorine; and n is 1 or 2.Type: GrantFiled: April 30, 2010Date of Patent: December 13, 2011Assignees: Abbott GmbH & Co. KG, Abbott LaboratoriesInventors: Andreas Haupt, Frauke Pohlki, Karla Drescher, Karsten Wicke, Liliane Unger, Ana-Lucia Relo, Anton Bespalov, Barbara Vogg, Gisela Backfisch, Juergen Delzer, Min Zhang, Yanbin Lao
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Patent number: 8076332Abstract: The present invention relates to a study on the synthesis of a novel N-(2-aminophenyl)benzamide derivative having an urea structure and represented by the general formula (1); and the utilization of a pharmacological effect of the derivative. A compound represented by the general formula (1) or a salt thereof has an effect of cellular morphological change on trabecular meshwork cells and is effective in the prevention and/or treatment of a disease considered to be related to intraocular pressure. In the formula, R1 and R2 represent a hydrogen atom, a lower alkyl group, or the like; R3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, or the like; R4 and R5 represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, or the like; X represents a lower alkylene group or the like; Y represents a single bond, a lower alkylene group, or the like; l and m represent 0, 1, 2, or the like.Type: GrantFiled: December 26, 2007Date of Patent: December 13, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Publication number: 20110293640Abstract: A method of treating a subject with a cytokine-mediated inflammatory disorder comprising administering to the subject an effective amount of a pharmaceutically acceptable cholinesterase inhibitor, provided that the inhibitor is not galantamine.Type: ApplicationFiled: May 27, 2011Publication date: December 1, 2011Inventors: Kevin J. Tracey, Valentin A. Pavlov
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Publication number: 20110294760Abstract: The invention generally relates to compositions and methods for preventing sternal wound infections, such as mediastinitis. In certain embodiments, the invention provides an antimicrobial composition including at least one bioresorbable polymer, such as a tyrosine-derived polyesteramide, and at least one antimicrobial agent, in which the composition is adapted to be topically applied to an esophageal perforation in a subject or a median sternotomy incision site in the subject, and in which the at least one antimicrobial agent is present in an amount effective to inhibit development of mediastinitis in the subject.Type: ApplicationFiled: June 1, 2010Publication date: December 1, 2011Applicant: TyRx Pharma, Inc.Inventors: Raman Bahulekar, Arikha Moses, Satish Pulapura, William C. McJames, II, Fatima Buevich
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Publication number: 20110288105Abstract: The present invention relates to the treatment of an individual afflicted with L-DOPA-induced dyskinesia, which condition may arise as a consequence of long-term treatment with L-DOPA therapy in Parkinson's patients, the instant treatment comprising administering to the individual an effective amount of eltoprazine or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 4, 2009Publication date: November 24, 2011Applicant: Merz Pharma GmbH & Co. KGaAInventors: Barbara Valastro, Andrzej Dekundy, Frank Tennigkeit, Hermann Russ, Lutz Franke