Additional Hetero Ring Patents (Class 514/397)
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Patent number: 8598217Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.Type: GrantFiled: April 30, 2010Date of Patent: December 3, 2013Assignees: Astex Therapeutics Ltd., Novartis AGInventors: Steven Howard, Paul Neil Mortenson, Steven Douglas Hiscock, Alison Jo-Anne Woolford, Andrew James Woodhead, Gianni Chessari, Marc O'Reilly, Miles Stuart Congreve, Claudio Dagostin, Young Shin Cho, Fan Yang, Christine Hiu-Tung Chen, Christopher Thomas Brain, Bharat Lagu, Yaping Wang, Sunkyu Kim, John Giraldes, Michael Joseph Luzzio, Lawrence Blas Perez
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Patent number: 8598219Abstract: The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.Type: GrantFiled: May 23, 2013Date of Patent: December 3, 2013Assignees: Helsinn Healthcare SA, Roche Palo Alto LLCInventors: Giorgio Calderari, Daniele Bonadeo, Roberta Cannella, Alberto Macciocchi, Andrew Miksztal, Thomas Malefyt, Kathleen M Lee, Carmine Panuccio
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Patent number: 8598181Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: July 2, 2010Date of Patent: December 3, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
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Publication number: 20130317047Abstract: The present invention relates to use of an inhibitor of the renin-anglotensin system (RAS) or a pharmaceutically acceptable derivative thereof, such as ramipril or ramiprilat, in the prevention of stroke, diabetes and/or congestive heart failure (CHF).Type: ApplicationFiled: November 9, 2012Publication date: November 28, 2013Applicant: Aventis Pharma Deutschland GmbHInventor: Aventis Pharma Deutschland GmbH
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Publication number: 20130315874Abstract: Disclosure is provided for methods of preventing, removing or inhibiting microbial biofilm formation or microbial infection in a plant or plant part thereof, including applying thereto a treatment effective amount of an active compound as described herein, or an agriculturally acceptable salt thereof. Methods of enhancing a microbicide (e.g., including a copper, antibiotic, bacteriophage, etc.) and/or plant defense activator are also provided, including applying an active compound as described herein. Compositions comprising an active compound as described herein in an agriculturally acceptable carrier are also provided, and in some embodiments the compositions further include a microbicide (e.g., including copper, antibiotic, bacteriophage, etc.) and/or plant defense activator.Type: ApplicationFiled: July 19, 2013Publication date: November 28, 2013Applicant: North Carolina State UniversityInventors: Christian Melander, John Cavanagh, David F. Ritchie, Steven A. Rogers, Robert W. Huigens, III, Catherine S. Reed
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Patent number: 8592461Abstract: The present invention provides a plant disease control agent containing at least one of tetrazoyloxime dirivatives and salts thereof, and at least one selected from the group consisting of fosetyl, propamocarb, basic copper chloride, chlorothalonil, manzeb, cymoxanil, folpet, iminoctadine, cyazofamid, metalaxyl, fludioxonil, tebuconazole, prothioconazole, thiamethoxam, azoxystrobin and salts thereof.Type: GrantFiled: March 24, 2009Date of Patent: November 26, 2013Assignee: Nippon Soda Co., Ltd.Inventors: Ichirou Urihara, Atsunori Isshiki, Hiroyasu Hosokawa, Tomoyuki Saiga
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Publication number: 20130310319Abstract: The subject invention is directed to a pharmaceutical composition comprising an open matrix network carrying a pharmaceutically active ingredient, wherein the open matrix network comprises levan.Type: ApplicationFiled: July 26, 2013Publication date: November 21, 2013Applicant: Ferring B.V.Inventors: Varinder Ahuja, Tejas Gunjikar, Kristin Wannerberger, Shweta Gupta
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Publication number: 20130310427Abstract: Antiviral compounds may be used to inhibit or reduce the activity of Hepatitis C virus (HCV), particularly HCV's NS5A protein. In these contexts, inhibition and reduction of activity of the NS5A protein refers to a lower level of the measured activity relative to a control experiment in which the cells or the subjects are not treated with the test compound. The inhibition or reduction in the measured activity is at least a 10% reduction or inhibition. The compounds and their isomeric forms and pharmaceutically acceptable salts thereof are useful in treating and preventing HCV infection alone or when used in combination with other compounds targeting viral or cellular elements or functions involved in the HCV lifecycle.Type: ApplicationFiled: June 9, 2011Publication date: November 21, 2013Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Publication number: 20130309195Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: March 14, 2013Publication date: November 21, 2013Inventors: John O. Link, Jeromy J. Cottell, Teresa Alejandra Trejo Martin
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Patent number: 8586620Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.Type: GrantFiled: May 6, 2011Date of Patent: November 19, 2013Assignee: NeurAxon, Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
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Patent number: 8586624Abstract: The present invention is directed to novel thiophene inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: GrantFiled: December 14, 2010Date of Patent: November 19, 2013Assignee: N30 Pharmaceuticals, Inc.Inventor: Xicheng Sun
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Publication number: 20130302378Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.Type: ApplicationFiled: July 8, 2013Publication date: November 14, 2013Inventors: Viswajanani J. SATTIGERI, Venkata P. PALLE, Manoj Kumar KHERA, Ranadheer REDDY, Manoj Kumar TIWARI, Ajay SONI, Abdul Rehman Abdul RAUF, Sony JOSEPH, Arpita MUSIB, Sunanda G. DASTIDAR, Punit Kumar SRIVASTAVA
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Publication number: 20130302422Abstract: Provided is a pharmaceutical composition for the treatment and prevention of kidney diseases, containing (a) a therapeutically effective amount of a compound represented by Formulae 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: May 22, 2013Publication date: November 14, 2013Applicants: KT & G CORPORATION, MAZENCE INC.Inventors: Taehwan Kwak, Myung-Gyu Park, Kyoung Hoon Jung
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Publication number: 20130303538Abstract: The invention relates to compounds of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them.Type: ApplicationFiled: January 20, 2012Publication date: November 14, 2013Inventors: Joachim Nozulak, Dieter Oser
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Publication number: 20130303505Abstract: TGR5 agonists of structural formula VIII(Q), wherein X, R1, R2, and R5 are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.Type: ApplicationFiled: August 11, 2010Publication date: November 14, 2013Inventors: Venkataiah Bollu, Brant Clayton Boren, Jackaline Dalgard Julien, Brenton T. Flatt, Nadia Haq, Sarah Hudson, Raju Mohan, Michael Morrissey, Benjamin Pratt
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Publication number: 20130303572Abstract: Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: wherein Z is N or CH or the Z(R1) part is replaced with a covalent bond, m and n is 0, 1, 2 or 3; HET is heteroaryl; X is CF3, halogen, CO-heterocyclyl, COOR3 or CONHR3; R1 is H, (CH2)o-aryl, (CH2)p-heteroaryl, (CH2)q-biphenyl; C(O)—R5; S(O)2—R6; R2 is H, aryl, heteroaryl, Y—(CH2)r-aryl, Y—(CH2)s-heteroaryl, where some of the above substituents may be substituted; Y is O or S; with the exclusion of the compound where HET is 1,3-thiazol, X is COOH, R1 is 4-fluorophenyl and R2 is benzyloxy. The invention also relates to the use of a compound of general formula (I), salts or solvates thereof for the use in the prevention or treatment of diseases where the activation of MMPs is involved in the pathomechanism. In this aspect the use of the above excluded compound is also inventive.Type: ApplicationFiled: December 19, 2011Publication date: November 14, 2013Inventors: Péter Ferdinandy, Tamás Bálint Csont, Csaba Csonka, Krisztina Kedvesné Kupai, László Kovács, Attila Kis-Tamás, Ferenc Tamás Takács, Dénes Kónya, Gábor Medgyes, Sándor Cseh, István Hajdú, Zsolt Lõrincz, György Dormán, Anikó Görbe
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Publication number: 20130303489Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.Type: ApplicationFiled: March 11, 2013Publication date: November 14, 2013Applicant: Eisai R&D Management Co., Ltd.Inventors: Sergei Agoulnik, Bruce Decosta, Hong Du, Yimin Jiang, Xiang-Yi Li, Kenichi Nomoto, John (Yuan) Wang, Huiming Zhang
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Publication number: 20130303473Abstract: The invention provides pharmaceutical compositions based on liquid vehicles whose density is substantially higher than that of aqueous physiological fluids. The compositions are useful as medicines in ophthalmology, in particular for the treatment of conditions affecting the posterior segment of an eye. They may be administered topically into the eye or in a minimally invasive manner by periocular injection. Preferred liquid carriers are selected from semifluorinated alkanes.Type: ApplicationFiled: November 10, 2011Publication date: November 14, 2013Applicant: NOVALIQ GmbHInventor: Clive G. Wilson
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Publication number: 20130296311Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: May 26, 2011Publication date: November 7, 2013Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Publication number: 20130296322Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: July 8, 2013Publication date: November 7, 2013Applicant: THERAVANCE, INC.Inventors: Eric L. Stangeland, Lori Jean Van Orden, Daisuke Roland Saito
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Publication number: 20130296392Abstract: Disclosed herein are methods of treating overactive bladder in a patient, the method comprising identifying a patient in need thereof; and administering to the patient a composition comprising tolterodine, or a pharmaceutically acceptable salt thereof, and pilocarpine, or a pharmaceutically acceptable salt thereof, wherein after the administration Cmax for tolterodine is between 1.0-8.0 ng/mL.Type: ApplicationFiled: May 1, 2013Publication date: November 7, 2013Applicant: TheraVida, Inc.Inventors: Mehdi PABORJI, Roger S. FLUGEL, Kenneth L. DUCHIN
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Publication number: 20130296304Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C.Type: ApplicationFiled: September 28, 2011Publication date: November 7, 2013Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Patent number: 8574563Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: September 11, 2012Date of Patent: November 5, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Publication number: 20130289086Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein each of Ring A, Ring B, T, R2, R2?, and RA is as defined and described herein and methods for treating subjects or patients with a disease, disorder, or condition.Type: ApplicationFiled: July 13, 2012Publication date: October 31, 2013Inventor: Mark E. Duggan
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Publication number: 20130289057Abstract: The invention relates to N-arylaminomethylenebenzothiophenones of General Formula (I) for use as a drug for the treatment of cardiovascular diseases: wherein E is S, O, or CH2, D is CH or NH, and Ar is a phenyl or naphtyl moiety substituted by an electron-withdrawing group, an unsubstituted heteroaryl residue, or a heteroaryl residue substituted by alkyl or an electron-withdrawing group.Type: ApplicationFiled: January 12, 2012Publication date: October 31, 2013Applicants: FORSCHUNGSVERBUND BERLIN E.V., MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZINInventors: Enno Klussmann, Walter Rosenthal, Jelena Milic, Martin W. Bergmann
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Publication number: 20130289087Abstract: Disclosed herein are pharmaceutical compositions comprising oxybutynin or tolterodine, or a free base thereof or a pharmaceutically acceptable salt thereof, and pilocarpine, or a free base thereof or a pharmaceutically acceptable salt thereof. Also disclosed are methods of treating a patient suffering from overactive bladder comprising administering to the patient the above pharmaceutical composition.Type: ApplicationFiled: June 24, 2013Publication date: October 31, 2013Inventor: Mehdi Paborji
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Publication number: 20130289072Abstract: The present invention relates to provision of a novel indazole compound which is capable of inhibiting HSP90 and shows a cytostatic effect on cancer cells. The present invention also relates to provision of a drug useful for preventing and/or treating, on the basis of an HSP90 inhibitory effect, a disease in which HSP90 participates, in particular, cancer. A compound represented by the general formula (I) or a salt thereof: wherein X represents CH or N; any one or two of Y1, Y2, Y3, and Y4 represent C—R3 or N, and the others represent CH; A and B are the same or different and represent an optionally substituted monocyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R1 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R2 represents a hydrogen atom, a halogen atom etc.; R3 represents a hydrogen atom, a halogen atom etc.; R4 and R5 are the same or different and represent a hydroxyl group etc.Type: ApplicationFiled: January 6, 2012Publication date: October 31, 2013Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Makoto Kitade, Shuichi Ohkubo, Chihoko Yoshimura
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Publication number: 20130280211Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: June 17, 2013Publication date: October 24, 2013Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. ST. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
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Publication number: 20130281475Abstract: 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: ApplicationFiled: June 13, 2013Publication date: October 24, 2013Inventors: Carl R. Illig, Shelly K. Ballentine, Jinsheng Chen, Renee Louise, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
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Publication number: 20130274304Abstract: Disclosed are compounds of Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.Type: ApplicationFiled: June 12, 2013Publication date: October 17, 2013Inventors: Pingyun Chen, Ricky Couch, Maosheng Duan, Beth Adams Norton
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Publication number: 20130274227Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: March 14, 2013Publication date: October 17, 2013Applicant: Axikin Pharmaceuticals, Inc.Inventors: Erik Dean RAAUM, Garrett Thomas Potter, Tai Wei Ly
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Publication number: 20130274260Abstract: This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic ?-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.Type: ApplicationFiled: December 13, 2011Publication date: October 17, 2013Inventors: Gerard Griffioen, Tom Van Dooren, Verónica Rojas De La Parra, Sara Allasia, Arnaud Marchand, Amuri Kilonda, Patrick Chaltin
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Patent number: 8557850Abstract: The present invention provides a plant disease control agent containing at least one of tetrazoyloxime dirivatives and salts thereof, and at least one selected from the group consisting of fosetyl, propamocarb, basic copper chloride, chlorothalonil, manzeb, cymoxanil, folpet, iminoctadine, cyazofamid, metalaxyl, fludioxonil, tebuconazole, prothioconazole, thiamethoxam, azoxystrobin and salts thereof.Type: GrantFiled: March 24, 2009Date of Patent: October 15, 2013Assignee: Nippon Soda Co., Ltd.Inventors: Ichirou Urihara, Atsunori Isshiki, Hiroyasu Hosokawa, Tomoyuki Saiga
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Publication number: 20130267502Abstract: This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.Type: ApplicationFiled: March 15, 2013Publication date: October 10, 2013Inventors: Gregory A. Demopulos, George A. Gaitanaris, Roberto Ciccocioppo
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Patent number: 8552047Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: January 30, 2012Date of Patent: October 8, 2013Assignee: Bristol-Myers Squibb CompanyInventors: John A. Bender, Omar D. Lopez, Gan Wang, Makonen Belema, John F. Kadow
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Patent number: 8546376Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: GrantFiled: September 17, 2010Date of Patent: October 1, 2013Assignee: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
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Patent number: 8546389Abstract: The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:Type: GrantFiled: October 20, 2011Date of Patent: October 1, 2013Assignee: Biota Scientific Management Pty Ltd.Inventors: Rosliana Halim, Michael Harding, Richard Hufton, Craig James Morton, Saba Jahangiri, Brett Raymond Pool, Tyrone Pieter Jeynes, Alistair George Draffan, Barbara Frey, Michael John Lilly
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Publication number: 20130252937Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m 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: March 14, 2013Publication date: September 26, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
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Publication number: 20130253008Abstract: The present invention relates to novel azoles, novel antiviral active components of the general formulas 1A and 1B, pharmaceutical composition, antiviral medicament, method for prophylaxis and treatment of viral diseases, particularly caused by hepatitis C viruses (HCV). In general formulas 1A and 1B wherein: solid lines with accompanying dotted lines () represent ordinary bond or double bond, provided that one of them is an ordinary bond, the other one is double bond; X and Y accept various meanings, one of them is—nitrogen, the other—oxygen, sulfur or NH group; R1 and R2—optionally the same radicals selected from 2-(R)- and (S)-substituted N-acyl pyrrolidine derivatives; N-methyl-N-[2-(R) and (S)-substituted 2,2-disubstituted acetamides; methyl[2-(R) and (S)-substituted ((methyl)amino)-(1-oxobutan-2-yl)-2-(R)-] and (S)-iso-propyl)-carbamates.Type: ApplicationFiled: November 28, 2011Publication date: September 26, 2013Applicant: Alla Chem LLCInventors: Alexandre Vasilievich Ivachtchenko, Vadim Vasilievich Bichko, Oleg Dmitrievich Mitkin
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Publication number: 20130252984Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: March 12, 2013Publication date: September 26, 2013Applicant: ALLERGAN, INC.Inventors: Haiqing YUAN, Richard L. BEARD, Xiaoxia LIU, John E. DONELLO, Veena VISWANATH, Michael E. GARST
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Patent number: 8541453Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: May 20, 2011Date of Patent: September 24, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
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Publication number: 20130245015Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: May 3, 2013Publication date: September 19, 2013Inventors: YUJIA DAI, STEVEN K. DAVIDSEN, ANNA M. ERICSSON, KRESNA HARTANDI, ZHIQIN JI, MICHAEL R. MICHAELIDES
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Publication number: 20130243886Abstract: The present invention relates to the use of one or more compounds selected from the following classes of biologically active agents: an a-adrenergic antagonist, an anthelmintic agent, an antifungal agent, an antimalarial agent, an antineoplastic agent, an antipsychotic agent, an antioxidant, a vasodilator and/or a vitamin, or a pharmaceutically acceptable derivative thereof, for use in the treatment of a microbial infection and in particular for killing multiplying, non-multiplying and/or clinically latent microorganisms associated with such an infection.Type: ApplicationFiled: September 9, 2011Publication date: September 19, 2013Applicant: HELPERBY THERAPEUTICS LIMITEDInventors: Yanmin Hu, Anthony RM Coates
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Publication number: 20130237557Abstract: The present invention derives from the finding that increased levels of alpha 2a adrenergic receptors (ADRA2a) are associated with chronic liver disease and that by decreasing ADRA2a levels in vivo, a number of symptoms and consequences of chronic liver disease may be reduced. Accordingly, the invention provides ADRA2a antagonists for use in a method of treating an individual suffering from liver disease.Type: ApplicationFiled: August 12, 2011Publication date: September 12, 2013Applicant: UCL BUSINESS PLCInventors: Rajeshwar P. Mookerjee, Vikram Sharma, Rajiv Jalan
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Publication number: 20130237514Abstract: Pyrrolidinone carboxamide compounds are provided that are useful for inhibiting the binding of ligands to the ChemR23 receptor.Type: ApplicationFiled: October 5, 2012Publication date: September 12, 2013Applicant: ChemoCentryx, Inc.Inventors: Trevor T. Charvat, Hiufung Chu, Antoni Krasinski, Christopher W. Lange, Manmohan Reddy Leleti, Jay P. Powers, Sreenivas Punna, Timothy J. Sullivan, Solomon Ungashe
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Publication number: 20130237478Abstract: The present invention relates to compositions and methods for the treatment of peripheral vascular disease (PVD). In particular, the invention provides compositions and methods for treatment of critical limb ischemia, and related diseases, disorders or conditions, based on the use of angiotensin-(1-7) peptides or functional equivalents, analogs or derivatives, angiotensin-(1-7) receptor agonists, ACE2 and/or ACE2 activators.Type: ApplicationFiled: April 2, 2013Publication date: September 12, 2013Applicant: TARIX PHARMACEUTICALS LTD.Inventor: Richard Franklin
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Publication number: 20130237552Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: April 29, 2013Publication date: September 12, 2013Applicant: ALLERGAN, INC.Inventors: HAIQING YUAN, RICHARD L. BEARD, MICHAEL E. GARST, JOHN E. DONELLO, XIAOXIA LIU, VEENA VISWANATH
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Publication number: 20130231379Abstract: The invention provides a method for the treatment of fungal dermatitis. The treatment method involves administering an effective amount of luliconazole or a pharmaceutically acceptable salt thereof to a target in need of a treatment of fungal dermatitis.Type: ApplicationFiled: April 19, 2013Publication date: September 5, 2013Applicant: NIHON NOHYAKU CO., LTD.Inventors: Hiroyasu KOGA, Yasuko NANJOH, Hideo KANEDA
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Publication number: 20130231311Abstract: Systems and methods are described for treating un-met medical needs in migraine and related conditions such as cluster headache. Included are treatments that are both rapid onset and long acting, which include sustained release formulations, and combination products. Also included are treatments for multiple symptoms of migraine, especially headache and nausea and vomiting. Systems that are self contained, portable, prefilled, and simple to self administer at the onset of a migraine attack are disclosed, and preferably include a needle-free injector and a high viscosity formulation, to eliminate such issues as fear of self administration with needles, and needle stick and cross contamination.Type: ApplicationFiled: April 16, 2013Publication date: September 5, 2013Inventors: Stephen J. FARR, John TURANIN, Roger HAWLEY, Jeffrey A. SCHUSTER
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Publication number: 20130230501Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.Type: ApplicationFiled: July 16, 2012Publication date: September 5, 2013Applicant: Daiichi Sankyo Company, LimitedInventors: Tsutomu Nagata, Masahiro Inoue, Yuka Ashida, Kengo Noguchi, Makoto Ono