Additional Hetero Ring Patents (Class 514/397)
-
Publication number: 20140163025Abstract: The present invention relates to compounds of general formula I, wherein the groups (Het)Ar and R1 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds 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: December 2, 2013Publication date: June 12, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Sara FRATTINI, Elke LANGKOPF, Holger WAGNER
-
Publication number: 20140165223Abstract: Described are methods and compositions for inhibiting the trimerization of ligands belonging to the TNF superfamily, in particular, inhibiting RANKL trimerization. Accordingly, the methods and compositions provided herein can be used to treat disorders associated with increased RANK signaling, in particular those related to bone loss. Compounds that inhibit trimerization of ligands belonging to the TNF superfamily are also described.Type: ApplicationFiled: February 12, 2014Publication date: June 12, 2014Applicant: B.S.R.C. "Alexander Fleming"Inventors: Eleni Ntouni, Georgios Kollias
-
Patent number: 8748425Abstract: Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.Type: GrantFiled: August 1, 2013Date of Patent: June 10, 2014Assignee: Allergan Sales, LLCInventors: Chin-Ming Chang, Gary J. Beck, Cynthia C. Pratt, Amy L. Batoosingh
-
Publication number: 20140155447Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: February 5, 2014Publication date: June 5, 2014Applicant: N30 Pharmaceuticals, Inc.Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
-
Publication number: 20140155382Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: November 22, 2013Publication date: June 5, 2014Applicant: ABBVIE INC.Inventors: David A. DEGOEY, Allan C. KRUEGER, Charles W. HUTCHINS, Warren M. KATI, William A. CARROLL
-
Publication number: 20140154319Abstract: Provided is a pharmaceutical composition for the treatment and prevention of cardiac diseases, containing (a) a therapeutically effective amount of a compound represented by Formula 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.Type: ApplicationFiled: June 21, 2013Publication date: June 5, 2014Inventors: Taehwan KWAK, Myung-Gyu Park
-
Publication number: 20140155377Abstract: The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: February 6, 2014Publication date: June 5, 2014Applicant: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Amy Qi Han, Darius J. Robinson, Changsheng Zheng, Anlai Wang, Yingxin Zhang
-
Patent number: 8741943Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.Type: GrantFiled: May 21, 2012Date of Patent: June 3, 2014Assignee: Tobira Therapeutics, Inc.Inventors: Mitsuru Shiraishi, Masanori Baba, Katsuji Aikawa, Naoyuki Kanzaki, Masaki Seto, Yuji Iizawa
-
Patent number: 8741942Abstract: The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis.Type: GrantFiled: February 21, 2012Date of Patent: June 3, 2014Assignees: President and Fellows of Harvard College, The Brigham and Women's Hospital, Inc.Inventors: Gregory D. Cuny, Prakash Jagtap, Junying Yuan, Alexei Degterev
-
Publication number: 20140148491Abstract: The present application discloses chemical compositions and methods for enhancing the transdermal permeation of therapeutic agents through skin. The chemical compositions and methods of the invention can include combinations of a first fatty acid having about 14 or more carbon atoms and a second fatty acid having about 10 or less carbon atoms. These compositions are useful for the delivery of therapeutic agents, in particular hard to deliver drugs such as those that have fused rings, including ondansetron, and large drugs such as peptides. The compositions of the invention can be formulated as transdermal gels, lotions, creams, transdermal patches, sprays or mists.Type: ApplicationFiled: January 30, 2014Publication date: May 29, 2014Applicant: InteguRx Therapeutics, LLCInventors: Kirti H. Valia, Agis Kydonieus
-
Publication number: 20140147517Abstract: Amisulpride is used in the therapy of nausea, vomiting or retches. The therapy may utilize a novel injectable formulation, in unit dosage form, comprising less than 50 mg amisulpride.Type: ApplicationFiled: February 4, 2014Publication date: May 29, 2014Inventors: Julian Clive Gilbert, Robert William Gristwood, Nicola Cooper, Gabriel Fox
-
Publication number: 20140148448Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: January 30, 2014Publication date: May 29, 2014Applicant: Janssen Pharmaceutica NVInventors: Carl R. ILLIG, Shelley K. BALLENTINE, Jinsheng CHEN, Renee Louise DESJARLAIS, Sanath K. MEEGALLA, Mark WALL, Kenneth WILSON
-
Patent number: 8735438Abstract: A compound having selective modulating activity at the alpha 2B and/or alpha 2C adrenergic receptor subtypes is represented by the general Formula 1: wherein n=1-4; X is C or N; R1-R6 can be the same or different and are independently selected from the group consisting of H, C1-6 alkyl, OCH3, OH, F, Cl, Br, CH2OH, CH2N(R7)2, C(O)R8, CH2CN, CF3, wherein R7 is H or C1-6 alkyl; and R8 is C1-6 alkyl or aryl. The compounds of Formula 1 can be incorporated in pharmaceutical compositions and used in methods of treatment of alpha 2 receptor mediated diseases and conditions.Type: GrantFiled: December 13, 2010Date of Patent: May 27, 2014Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Todd M. Heidelbaugh, Smita Bhat, Ken Chow, Michael Garst
-
Patent number: 8735398Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: GrantFiled: November 7, 2012Date of Patent: May 27, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
-
Publication number: 20140142154Abstract: An antifungal agent against a fungus of the genus Scytalidium (Scytalidium—dimidiatum, Scytalidium—hyalinum etc.), preferably an antifungal agent for superficial mycosis caused by a fungus of the genus Scytalidium as a pathogenic fungus, which contains luliconazole or a pharmaceutically acceptable salt thereof and/or lanoconazole or a pharmaceutically acceptable salt thereof as active ingredient(s).Type: ApplicationFiled: September 25, 2012Publication date: May 22, 2014Applicant: NIHON NOHYAKU CO., LTD.Inventors: Hiroyasu Koga, Yasuko Nanjoh, Ryoji Tsuboi
-
Publication number: 20140142116Abstract: A method of treatment, reversal and/or symptomatic relief of inflammatory pain, including hyperalgesia, thermal or mechanical allodynia, in vertebrate animals, particularly in human subjects, comprising administering angiotensin II receptor 2 (AT2 receptor) antagonists is disclosed. The AT2 receptor antagonist may be provided alone or in combination with other compounds such as those that are useful in the control of inflammatory pain.Type: ApplicationFiled: September 3, 2013Publication date: May 22, 2014Applicant: Spinifex Pharmaceuticals Pty LtdInventor: Maree Therese Smith
-
Patent number: 8729077Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.Type: GrantFiled: November 19, 2009Date of Patent: May 20, 2014Assignee: GlaxoSmithKline LLCInventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Don Roberts, Wieslaw Kazmierski, Richard Grimes
-
Patent number: 8729101Abstract: The present invention relates to a group of novel 1H-imidazole derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component. These 1H-imidazole derivatives are potent cannabinoid-CB1 receptor agonists, partial agonists or antagonists, useful for the treatment of psychiatric and neurological disorders, as well as and other diseases involving cannabinoid neurotransmission. The compounds have the general formula (I), wherein R and R1-R4 have the meanings given in the specification.Type: GrantFiled: September 2, 2008Date of Patent: May 20, 2014Assignee: Solvay Pharmaceuticals, B.V.Inventors: Cornelis G. Kruse, Josephus H. M. Lange, Arnoldus H. J. Herremans, Herman H. Van Stuivenberg
-
Patent number: 8722719Abstract: Provided is an ester of 3-[(4-dipropylamino-butyl)(4-{[(1H-imidazole-2-ylmethyl)(1-methyl-1H-imidazole-2-ylmethyl)amino]methyl}benzyl)amino]propionic acid which is easily hydrolyzed in serum. The amine compound of the present invention is an ester compound represented by general formula (1). (In general formula (1), n is 1-4, and R1 and R2 represent an alkyl group having 1-3 carbon atoms.Type: GrantFiled: September 30, 2011Date of Patent: May 13, 2014Assignee: Kureha CorporationInventors: Ryo Matsui, Toru Yamazaki, Shigeyuki Kikumoto
-
Patent number: 8722718Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: GrantFiled: April 18, 2007Date of Patent: May 13, 2014Assignee: Janssen Pharmaceutica NVInventors: Carl R. Illig, Jinsheng Chen, Renee Louise DesJarlais, Kenneth Wilson
-
Publication number: 20140127285Abstract: The present invention includes compound compositions and methods of making compounds that include an oligo-benzamide compound having at least two optionally substituted benzamides.Type: ApplicationFiled: October 28, 2013Publication date: May 8, 2014Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventor: Jung-Mo Ahn
-
Publication number: 20140128429Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3 and R4 n are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: February 13, 2013Publication date: May 8, 2014Applicant: HOFFMANN-LA ROCHE INC.Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Xuefei Tan
-
Publication number: 20140128409Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R6 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.Type: ApplicationFiled: January 13, 2014Publication date: May 8, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: John Edward PARK, Nveed CHAUDHARY, Gerald Juergen ROTH, Armin HECKEL, Thorsten LEHMANN-LINTZ, Joerg KLEY
-
Publication number: 20140128329Abstract: Compositions and methods related to ophthalmic use of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymers and therapeutic uses are described herein.Type: ApplicationFiled: January 10, 2014Publication date: May 8, 2014Applicant: Allergan, Inc.Inventors: Anuradha V. Gore, Chetan P. Pujara, Richard S. Graham, Melissa Gulmezian, Kristin Prinn, Ramakrishnan Srikumar
-
Patent number: 8716492Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.Type: GrantFiled: December 15, 2011Date of Patent: May 6, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
-
Publication number: 20140113946Abstract: The present invention is directed to compositions and methods for treating presbyopia, mild hyperopia, and irregular astigmatism. The compositions include a cholinergic agent, such as a muscarinic acetylcholine receptor M3 agonist, and an alpha agonist having an imidazoline group or a non-steroidal anti-inflammatory agent (NSAID) having COX-2 selectivity. It has been found that an alpha agonist having an imidazoline group or non-steroidal anti-inflammatory agent (NSAID) having COX-2 selectivity in combination with a cholinergic agent, such as pilocarpine, act synergistically to improve the accommodative and focusing ability of the eye while minimizing the side effects from each compound.Type: ApplicationFiled: December 24, 2013Publication date: April 24, 2014Applicant: ALLERGAN, INC.Inventor: Juan Carlos Abad
-
Publication number: 20140113938Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: January 2, 2014Publication date: April 24, 2014Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
-
Publication number: 20140113945Abstract: The present invention is directed to novel pyrrole inhibitors of S-nitrosoglutathione reductase, pharmaceutical compositions comprising such inhibitors, and methods of using the same for liver toxicity.Type: ApplicationFiled: July 3, 2012Publication date: April 24, 2014Applicant: N30 PHARMACEUTICALS, INC.Inventors: Gary J. Rosenthal, Charles H. Scoggin, Dorothy Colagiovanni
-
Patent number: 8703776Abstract: Chemical compounds which act as agonists of, or otherwise modulate the activity of, GPR131 are disclosed. Related compositions, formulations and methods of use are also described.Type: GrantFiled: June 13, 2012Date of Patent: April 22, 2014Assignee: Cymabay Therapeutics, Inc.Inventors: Aaron Robert Novack, Dong-Fang Shi, Jingyuan Ma, Imad Nashashibi, Phuongly Pham, Jiangao Song, David W. G. Wone, Xueyan Wang, Jeffrey D. Johnson, Brian Edward Lavan, Charles A. McWherter, Xin Chen
-
Patent number: 8703803Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: GrantFiled: September 21, 2012Date of Patent: April 22, 2014Inventors: Peter A. Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
-
Publication number: 20140105976Abstract: Disclosed herein are pharmaceutical compositions comprising at least one minitablet, where the minitablet comprises a core, comprising pilocarpine, or a pharmaceutically acceptable salt thereof; and a coating layer comprising a coating polymer.Type: ApplicationFiled: October 11, 2013Publication date: April 17, 2014Applicant: THERAVIDA, INC.Inventors: Mehdi PABORJI, Robert V. TUOHY, Stephen P. LEVINE, Dana E. MOSESON, Nicolas D. KIRKLAND
-
Publication number: 20140107125Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.Type: ApplicationFiled: April 29, 2013Publication date: April 17, 2014Applicant: Dermira (Canada), Inc.Inventor: Dermira (Canada), Inc.
-
Publication number: 20140107111Abstract: The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat type-2 diabetes-associated pain and related symptoms.Type: ApplicationFiled: May 18, 2012Publication date: April 17, 2014Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jose Miguel Vela Hernandez, Maria Isabel Martin Fontelles
-
Publication number: 20140107095Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: ApplicationFiled: December 20, 2013Publication date: April 17, 2014Applicant: SERAGON PHARMACEUTICALS, INC.Inventors: Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Nicholas D. Smith
-
Patent number: 8697704Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: August 11, 2011Date of Patent: April 15, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Xiaowen Peng, Ce Wang, Yat Sun Or
-
Publication number: 20140100223Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:Type: ApplicationFiled: September 26, 2013Publication date: April 10, 2014Applicants: PRESIDENT & FELLOWS OF HARVARD COLLEGE, THE BROAD INSTITUTE, INC.Inventors: Mahmud Hussain, Daisuke Ito, Jason Law, Matthias Leiendecker, Ke Liu, Benito Munoz, Stuart Schreiber, Alykhan Shamji, Andrew Stern
-
Publication number: 20140100183Abstract: The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS.Type: ApplicationFiled: April 12, 2013Publication date: April 10, 2014Applicant: The Regents of the University of Colorado, a body corporateInventors: Daniel J. ABRAMS, Raymond BUNCH, Tom ANCHORDOQUY, Karen E. STEVENS
-
Patent number: 8691816Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: GrantFiled: August 14, 2009Date of Patent: April 8, 2014Assignee: N30 Pharmaceuticals, Inc.Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
-
Publication number: 20140094497Abstract: The present invention provides, among other things, methods and compositions for treating brain conditions. In some embodiments, the methods include administering to a subject suffering from or susceptible to a brain condition an angiotensin (1-7) peptide via either an intravenous or subcutaneous route of administration.Type: ApplicationFiled: May 17, 2013Publication date: April 3, 2014Inventor: Richard Franklin
-
Publication number: 20140094474Abstract: Compounds of formula (I) or (II) wherein Rx, Rz, R9, R10, R14, R14?, R15, R15?, A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.Type: ApplicationFiled: April 20, 2012Publication date: April 3, 2014Applicant: ORION CORPORATIONInventors: Olli Törmakängas, Gerd Wohlfahrt, Harri Salo, Rathna Durga Ramasurbamanian, Pranab Kumar Patra, Arputharaj Ebenezer Martin, Terhi Heikkinen, Anniina Vesalainen, Anu Moilanen, Arja Karjalainen
-
Publication number: 20140094436Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: ApplicationFiled: December 11, 2013Publication date: April 3, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Weiwen Ying, Zhenjian Du, Kevin Foley
-
Patent number: 8685984Abstract: The present invention features interferon- and ribavirin-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents without interferon and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to a subject an effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), and an inhibitor of cytochrome P450 (e.g., ritonavir).Type: GrantFiled: July 5, 2013Date of Patent: April 1, 2014Assignee: AbbVie Inc.Inventors: Barry M. Bernstein, Rajeev M. Menon, Amit Khatri, Sven Mensing, Sandeep Dutta, Daniel E. Cohen, Scott C. Brun, Walid M. Awni, Emily O. Dumas, Cheri E. Klein, Thomas J. Podsadecki
-
Patent number: 8685451Abstract: This invention pertains to a multi-layered tablet for a triple combination release of active agents to an environment of use. More particularly, the invention pertains to a multi-layered tablet (1) comprising two external drug-containing layers (2 and 3) in stacked arrangement with respect to and on opposite sides of an oral dosage form (4) that provides a triple combination release of at least one active agent. In one embodiment of the invention the dosage form is an osmotic device. In another embodiment of the invention the dosage form is a gastro-resistant coated core. In yet another embodiment of the invention the dosage form is a matrix tablet. In a different embodiment the dosage form is a hard capsule.Type: GrantFiled: June 18, 2008Date of Patent: April 1, 2014Assignee: Osmotica Kereskedelmi és Szolgáltató KFTInventors: Fernando G. Toneguzzo, Glenn A. Meyer, Marcelo A. Ricci, Marcelo A. Coppari, Ana C. Pastini, Gustavo A. Fischbein
-
Patent number: 8685978Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.Type: GrantFiled: July 26, 2010Date of Patent: April 1, 2014Assignee: University of Tennessee Research FoundationInventors: Richard E. Lee, Jianjun Qi, Julian G. Hurdle, Bernd Meibohm, Vnr Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
-
Publication number: 20140088002Abstract: The present invention relates to compositions and methods for treatment and/or prevention of diabetes or pre-diabetes. In particular, the invention provides compositions and methods for the treatment and/or prevention of diabetes or pre-diabetes, based on the use of angiotensin-(1-7) peptides, functional equivalents thereof, and/or angiotensin (1-7) agonists.Type: ApplicationFiled: August 29, 2013Publication date: March 27, 2014Applicant: TARIX PHARMACUTICALS LTD.Inventor: Richard Franklin
-
Patent number: 8680106Abstract: The present invention features interferon-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to the subject effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), an inhibitor of cytochrome P450 (e.g., ritonavir), and ribavirin.Type: GrantFiled: July 5, 2013Date of Patent: March 25, 2014Assignee: AbbVic Inc.Inventors: Barry M. Bernstein, Rajeev M. Menon, Amit Khatri, Sven Mensing, Sandeep Dutta, Daniel E. Cohen, Scott C. Brun, Walid M. Awni, Emily O. Dumas, Cheri E. Klein, Thomas J. Podsadecki
-
Publication number: 20140080882Abstract: An object is to provide means for improving the solubility of luliconazole. Disclosed is a crystal consisting of luliconazole and short chain alcohol having a number of carbon atom or atoms of 1 to 4.Type: ApplicationFiled: September 6, 2013Publication date: March 20, 2014Applicants: Nihon Nohyaku Co., Ltd., Pola Pharma Inc.Inventors: Takaaki Masuda, Makoto Gotoh, Yoshiyuki Miyata
-
Patent number: 8673955Abstract: Imidazole derivatives of formula (I): wherein R1, R2a, R2b, A, V and W are as defined in the description, as inhibitors of fructose-1,6-bisphosphatase, their preparation process and their use in the prevention or treatment of diabetes, and other diseases where the inhibition of gluconeogenesis, control of blood glucose levels, reduction in glycogen stores, or reduction in insulin levels is beneficial and diseases related to the insulin resistance syndrome.Type: GrantFiled: July 19, 2006Date of Patent: March 18, 2014Assignee: Merck Patent GmbHInventors: Denis Carniato, Gérard Moinet, Gérard Botton, Annick Arbellot De Vacqueur, Annick Audet
-
Publication number: 20140073574Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.Type: ApplicationFiled: November 13, 2013Publication date: March 13, 2014Inventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
-
Publication number: 20140072576Abstract: The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.Type: ApplicationFiled: November 8, 2013Publication date: March 13, 2014Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Masaya KOKUBO, Motoyuki TANAKA, Hiroshi OCHIAI, Yoshikazu TAKAOKA, Shiro SHIBAYAMA