Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Six Membered Hetero Ring By Nonionic Bonding Patents (Class 514/313)
-
Publication number: 20140011837Abstract: The invention provides compositions and methods for the treatment, as well as the inhibition and prevention, of an infection of the human papillomavirus and the epithelial lesions, namely, the warts of the skin and mucosal surfaces, associated therewith. The compositions comprise a therapeutically effective amount of an active ingredient comprising a compound selected from the group consisting of chloroquine, hydroxychloroquine, chloroquine combined with amodiaquine, and hydroxychloroquine combined with amodiaquine, or in each case, a pharmaceutically acceptable salt thereof. The methods comprise topically administering a therapeutically and/or antivirally effective amount of such a compound to a human being in need of such treatment, although in certain of the compounds may alternatively be administered subcutaneously or transdermally. The compositions may optionally also comprise one or more pharmaceutically acceptable non-active ingredients.Type: ApplicationFiled: July 3, 2012Publication date: January 9, 2014Inventor: Justice E. OBI
-
Publication number: 20140011838Abstract: The invention provides compositions and methods for the treatment, as well as the inhibition and prevention, of an infection of the human papillomavirus and the epithelial lesions, namely, the warts of the skin and mucosal surfaces, associated therewith. The compositions comprise a therapeutically effective amount of an active ingredient comprising at least one compound selected from the group consisting of chloroquine, hydroxychloroquine, amodiaquine, or in each case, a pharmaceutically acceptable salt thereof. The methods comprise topically administering a therapeutically and/or antivirally effective amount of such a compound to a human being in need of such treatment, although in certain of the compounds may alternatively be administered subcutaneously or transdermally. The compositions may optionally also comprise one or more pharmaceutically acceptable non-active ingredients.Type: ApplicationFiled: November 28, 2012Publication date: January 9, 2014Inventor: Justice E. OBI
-
Publication number: 20140004184Abstract: The present invention provides coated tablet formulations comprising neratinib maleate, and improved methods for making such coated tablets.Type: ApplicationFiled: August 21, 2013Publication date: January 2, 2014Applicant: Wyeth LLCInventors: Muhammad Ashraf, Mainuddin Mahmud, Chimanlall Goolcharran, Krishnendu Ghosh, Arwinder Singh Nagi
-
Publication number: 20140005222Abstract: The present invention provides a compound of the Formula II: wherein A is: R1 is CH3, CF3, or F; R2 is H, CH3, or F; R3 is CH3, OCH3, OH, F; R4 is OH or CH2OH; and X is CH or N; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 20, 2013Publication date: January 2, 2014Inventors: Maria-Jesus BLANCO-PILLADO, Matthew Joseph FISHER, Steven Lee KUKLISH, Tatiana Natali VETMAN
-
Publication number: 20140005178Abstract: The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).Type: ApplicationFiled: August 12, 2013Publication date: January 2, 2014Applicant: Almirall, S.A.Inventors: Julio Cesar CASTRO PALOMINO LARIA, Emma Terricabras Belart, Montserrat Erra Sola, Eloisa Navarro Romero, Siliva Fonquerna Pou, Aranzazu Cardus Figueras, Maria Estrella Lozoya Toribio
-
Publication number: 20140005250Abstract: A method of (a) treating a lymphoproliferative disease in a subject in need thereof; (b) slowing the progression of lymphoproliferative disease in a subject who has been diagnosed with a lymphoproliferative disease; or (c) preventing or delaying development of a lymphoproliferative disease in a subject who is at risk of developing a lymphoproliferative disease. The method generally comprises administering to the individual an effective amount of a combination therapy comprising: i) at least one autophagy modulating agent, or a derivative, pharmaceutically acceptable salt thereof, or prodrug thereof; and ii) at least one CDK inhibitor agent, or a derivative, pharmaceutically acceptable salt thereof, or prodrug thereof, wherein the i) agent and the ii) agents are administered in amounts sufficient to enhance the cytotoxicity of the combination relative to the CDK inhibitor agent treatment alone.Type: ApplicationFiled: November 7, 2011Publication date: January 2, 2014Applicant: THE OHIO STATE UNIVERSITYInventors: John C. Byrd, Amy J. Johnson, Emilia Mahoney, David M. Lucas, Michael R. Grever
-
Publication number: 20130345258Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.Type: ApplicationFiled: March 2, 2012Publication date: December 26, 2013Applicant: Glaxosmithline LLCInventors: Michael Jonathan Bury, Linda N. Casillas, Adam Kenneth Charnley, Pamela A. Haile, Robert W. Marquis, JR., John F. Mehlmann, Joseph J. Romano, Robert R. Singhaus, JR., Gren Z. Wang
-
Publication number: 20130344061Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating lupus, a fibrotic condition, or inflammatory myopathies and other conditions (e.g., skin conditions).Type: ApplicationFiled: March 15, 2013Publication date: December 26, 2013Applicant: INFINITY PHARMACEUTICALS, INC.Inventors: Vito J. PALOMBELLA, David G. WINKLER
-
Publication number: 20130344165Abstract: This disclosure relates to compounds and compositions for forming bone and methods related thereto. In certain embodiments, the disclosure relates to methods of forming bone comprising implanting a bone graft composition comprising a growth factor such as BMP in a subject at a site of desired bone growth or enhancement in combination with a JAB1 blocker.Type: ApplicationFiled: February 23, 2012Publication date: December 26, 2013Applicant: EMORY UNIVERSITYInventors: Scott D. Boden, Sreedhara Sangadala
-
Publication number: 20130338190Abstract: Provided as represented by formula (I) is a pharmaceutically acceptable salt of (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide, a preparation method thereof, and a use thereof as a therapeutic agent, and especially as a protein kinase inhibitor.Type: ApplicationFiled: February 10, 2012Publication date: December 19, 2013Applicants: JIANGSU HENGRUI MEDICINE CO., LTD., SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD.Inventors: Xin Li, Bin Wang
-
Patent number: 8604030Abstract: The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R7, a sulfur atom or an oxygen atom, R1, R2, R2?, R3 and R3? independently represent a hydrogen atom, C1-6 alkyl group or C3-6 cycloalkyl group, and R4, R5 and R6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.Type: GrantFiled: March 25, 2010Date of Patent: December 10, 2013Assignee: Kowa Company, Ltd.Inventors: Masanori Ashikawa, Toshiharu Morimoto, Hajime Yamada, Shunji Takemura, Tatsuaki Nishiyama, Takeshi Doi, Hiroyuki Ishiwata
-
Patent number: 8604055Abstract: The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.Type: GrantFiled: June 28, 2006Date of Patent: December 10, 2013Assignee: Dr. Reddy's Laboratories Ltd.Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dagar, Shanavas Alikunju
-
Publication number: 20130315940Abstract: The present invention derives from the finding that increased levels of Toll related receptor 9 (TLR9) and Toll related receptor 7 (TLR7) are associated with liver cancer and in particular hepatocellular carcinoma. Accordingly, the invention provides TLR9 and TLR7 antagonists for use in a method of treating liver cancer. The invention provides other strategies such as modulation of endosomal signalling by using compounds such as chloroquine to prevent or treat such liver cancer. The invention also provides agents capable of inducing an immune response against TLR9 and TLR7 for use in a method of treating liver cancer. The presence of TLR9 and TLR7 expression may be indicative of the presence of liver cancer and the amount of TLR9 and TLR7 expression may be indicative of the rate of growth or spreading of the cancer.Type: ApplicationFiled: August 19, 2011Publication date: November 28, 2013Inventors: Rajiv Jalan, Fatma El-zahraa Ammar Saleh Mohamed
-
Publication number: 20130310348Abstract: This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).Type: ApplicationFiled: July 25, 2013Publication date: November 21, 2013Applicants: State UniversityInventors: David H. Peyton, Steven Burgess
-
Publication number: 20130310393Abstract: Disclosed are heteroaryl compounds of Formula (I), (I), or pharmaceutically acceptable salts thereof, wherein Z is CH or N; W is CR3 or N; and R1, R2, and R3 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: September 23, 2011Publication date: November 21, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Audris Huang
-
Patent number: 8586608Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetra-hydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetra-hydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transductionType: GrantFiled: September 21, 2009Date of Patent: November 19, 2013Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Stefan Blech, Birgit Jung, Anke Baum, Flavio Solca
-
Patent number: 8586570Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.Type: GrantFiled: April 27, 2011Date of Patent: November 19, 2013Assignee: Massachusetts Institute of TechnologyInventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
-
Publication number: 20130302329Abstract: The present invention provides for methods and compositions for identifying and detecting autoantigens. Candidate autoantigens are identified by obtaining a subject sample from which HLA-DR-presented peptides are collected and identified using mass spectometry, then synthesized and reacted with the same subject peripheral blood or effected tissue. In particular, the present invention provides for endothelial cell growth factor as a novel autoantigen biomarker for Lyme disease-associated arthritis.Type: ApplicationFiled: September 21, 2011Publication date: November 14, 2013Applicants: TRUSTEES OF BOSTON UNIVERSITY, THE GENERAL HOSPITAL CORPORATIONInventors: Allen C. Steere, Elise Drouin, Catherine Costello, Robert Seward
-
Publication number: 20130296361Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity, wherein these compounds selected from the group consisting of wherein A, B, C, D, X, Y, Z and R3 are defined in the specification. Said compounds are useful for treating a disease or condition of a mammal selected from the group consisting of ocular diseases; systemic vascular barrier related diseases; allergies and other inflammatory diseases; cardiac diseases or conditions; fibrosis; pain and wounds.Type: ApplicationFiled: June 27, 2013Publication date: November 7, 2013Inventors: Wenkui K. Fang, Evelyn G. Corpuz, Wha-Bin Im, Ken Chow, Liming Wang
-
Publication number: 20130296363Abstract: Provided herein are compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 31, 2011Publication date: November 7, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventors: Raffaella Faraoni, Michael J. Hadd, Mark W. Holladay, Martin W. Rowbottom, Eduardo Setti
-
Publication number: 20130296237Abstract: The present invention provides methods and compositions for modulating certain metabolic processes and for treating a variety of disorders associated with metabolic syndrome, including insulin related disorders, ischemia, oxidative stress, atherosclerosis, hypertension, obesity, abnormal lipid metabolism, and stroke by administering an effective dose of a chloroquine compound. The invention also provides methods and compositions relating to administering an effective dose of a chloroquine compound in combination with at least a second pharmaceutically active ingredient or compound including an antihyperglycemic diabetes treatment, an antihypertensive agent, an antithrombotic agent, and/or an inhibitor of cholesterol synthesis or absorption.Type: ApplicationFiled: March 14, 2013Publication date: November 7, 2013Inventors: Michael B. Kastan, Clay F. Semenkovich, Jochen Schneider
-
Patent number: 8575195Abstract: Methods of treating a hepatitis C virus (HCV) related disease, such as HCV infections in subjects non-responsive to anti-HCV therapy, are described herein, comprising administering to the subject a therapeutically effective amount of hydroxychloroquine. An antiviral agent may be co-administered with the hydroxychloroquine. Methods utilizing synergistic combinations of hydroxychloroquine and an antiviral agent are disclosed. Further disclosed are compositions comprising hydroxychloroquine and an antiviral agent, as well as hydroxychloroquine and uses thereof for the treatment of a hepatitis C virus (HCV) related disease.Type: GrantFiled: March 15, 2013Date of Patent: November 5, 2013Assignees: Panmed Ltd., Genoscience Pharma SASInventor: Philippe Halfon
-
Publication number: 20130281488Abstract: The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.Type: ApplicationFiled: February 12, 2013Publication date: October 24, 2013Inventor: Wyeth LLC
-
Publication number: 20130281433Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
-
Publication number: 20130274278Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: ApplicationFiled: June 6, 2013Publication date: October 17, 2013Inventors: Stephen M. CONDON, Yijun DENG, Matthew D. ALEXANDER, Matthew G. LAPORTE
-
Patent number: 8557843Abstract: A compound of formula (I) as well as pharmaceutically acceptable salts thereof. A pharmaceutical composition having a therapeutically effective amount of the compound. The compound is useful for the treatment of cancer, diabetic retinopathy, age-related macular degeneration, inflammation, stroke, ischemic myocardium, atherosclerosis, macular edema or psoriasis.Type: GrantFiled: November 14, 2008Date of Patent: October 15, 2013Assignee: ClanoTech ABInventors: Jacob Westman, Natalia Nekhotiaeva, Johan Wannberg, Ulrika Backman, Johan Malm
-
Publication number: 20130266588Abstract: This invention relates generally to a therapeutic use of TLR3 and TLR7 inhibitors to treat or reduce pruritus in a subject.Type: ApplicationFiled: October 21, 2011Publication date: October 10, 2013Applicant: BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Ru-Rong Ji, Temugin Berta, Zhen-Zhong Xu, Tong Liu, Chul-Kyu Park
-
Patent number: 8551992Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.Type: GrantFiled: May 23, 2012Date of Patent: October 8, 2013Assignee: Neosome Life Sciences, LLCInventors: Laxman S. Desai, Srinivas Chittaboina
-
Patent number: 8552067Abstract: Provided herein are bioactive agents comprising a compound that inhibits the ion transport activity of a cystic fibrosis transmembrane conductance regulator (CFTR) and that is linked to a macromolecule that interacts with a cell that expresses CFTR. The bioactive agents described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea.Type: GrantFiled: December 19, 2007Date of Patent: October 8, 2013Assignee: The Regents of the University of CaliforniaInventors: Alan S. Verkman, Nitin D. Sonawane
-
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
-
Publication number: 20130243794Abstract: The invention provides methods for determining the propensity to develop, or the presence of, one or more infection-induced illness(es). The invention further provides methods of treating an infection (e.g., bacterial infection), methods of diagnosing an infection-induced illness in a subject, and methods of predicting the future severity of one or more infection-induced illness(es). Also provided are kits for determining the likelihood or propensity of a subject to develop one or more infection-induced illness(es) and kits for diagnosing one or more infection-induced illness(es) in a subject and identifying a subject as having an increased risk of later developing one or more severe infection-induced illness(es).Type: ApplicationFiled: December 5, 2011Publication date: September 19, 2013Applicant: Beth Israel Deaconess Medical Center, Inc.Inventor: Carl J. Hauser
-
Publication number: 20130237531Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: April 19, 2013Publication date: September 12, 2013Inventors: Guoxian Wu, Jiazhong Zhang, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, James Tsai
-
Patent number: 8530496Abstract: The present invention is bis-acridine or bis-quinoline intercalators having a modified bis(4-aminophenyl)ether tether to improve activity, selectivity, solubility and bioavailability of the antitumor compound.Type: GrantFiled: September 20, 2011Date of Patent: September 10, 2013Assignee: Trustees of Dartmouth CollegeInventors: Gordon W. Gribble, Justin M. Lopchuk
-
Patent number: 8524739Abstract: This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).Type: GrantFiled: April 25, 2011Date of Patent: September 3, 2013Assignee: State of Oregon acting by and through the State Board of Higher Education on behalf of Portland State UniversityInventors: David H. Peyton, Steven Burgess
-
Patent number: 8524740Abstract: A compound of Formula I is disclosed as follows: or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein R is hydrogen, P(?O)(OH)2, P(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, P(?O)(OH)(OM), P(?O)(OM)2, P?O(O2M), S(?O)(OH)2, S(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, S(?O)(OH)(OM), S(?O)(OM)2; M is a monovalent or divalent metal ion, or alkylammonium ion; W is (C6-C20)aryl, (C6-C20)heteroaryl, (C1-C18)alkyl(C6-C20)aryl, (C1-C18)alkyl(C6-C20)heteroaryl, hydroxy(C6-C20)aryl, hydroxy(C6-C20)heteroaryl, (C1-C18)alkoxy(C6-C20)aryl, (C1-C18)alkoxy(C6-C20)heteroaryl, (C1-C18)alkylenedioxy(C6-C20)aryl, (C1-C18)alkylenedioxy(C6-C20)heteroaryl, halo(C6-C20)aryl, halo(C6-C20)heteroaryl, (C1-C18)alkylamino(C6-C20)aryl, (C1-C18)alkylamino(C6-C20)heteroaryl, (C1-C18)cycloalkylamino(C6-C20)aryl, or (C1-C18)cycloalkylamino(C6-C20)heteroaryl, and their OR8 substutes; R5 is (C1-C18alkoxy, hydrogen, hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or OR8, or R5 and R6 are (C1-C18)dioxy provided that R7 iType: GrantFiled: July 13, 2011Date of Patent: September 3, 2013Assignee: Tairx, Inc.Inventors: Sheng-Chu Kuo, Kuo-Hsiung Lee, Li-Jiau Huang, Li-Chen Chou, Tian-Shung Wu, Tzong-Der Way, Jing-Gung Chung, Jai-Sing Yang, Chi-Hung Huang, Meng-Tung Tsai
-
Patent number: 8524281Abstract: The present invention provides an oral pharmaceutical formulation comprising coated spheroids of a kinase inhibitor such as neratinib, which formulation is designed to reduce or eliminate side effects associated with existing oral formulations of kinase inhibitors.Type: GrantFiled: November 5, 2010Date of Patent: September 3, 2013Assignee: Wyeth LLCInventors: Sripriya Venkata Ramana Rao, Syed Muzafar Shah, Christopher Richard Diorio, Maja Vencl-Joncic, Eugene James Murphy
-
Publication number: 20130225524Abstract: The invention is directed to substituted quinoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, R4, and R5 are defined herein. The compounds of the invention are inhibitors of lactate dehydrogenase A and can be useful in the treatment of cancer and diseases associated with tumor cell metabolism, such as cancer, and more specifically cancers of the breast, colon, prostate and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting lactate dehydrogenase A activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: November 3, 2011Publication date: August 29, 2013Inventors: Deping Chai, Mariela Colon, Christopher Dodson, Kevin J. Duffy, Antony Nicholas Shaw
-
Publication number: 20130225579Abstract: Disclosed is a compound of formula I, a stereoisomer thereof, a cis-trans-isomer thereof, a tautomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof, wherein R1, R2, R3 and R4 are each as defined in the present application.Type: ApplicationFiled: June 8, 2011Publication date: August 29, 2013Applicant: Tianjin Hemay Bio-Tech Co., Ltd.Inventors: Hesheng Zhang, Yingwei Chen, Qingchao He
-
Publication number: 20130225580Abstract: Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.Type: ApplicationFiled: February 28, 2013Publication date: August 29, 2013Applicant: CHEMOCENTRYX, INC.Inventor: ChemoCentryx, Inc.
-
Patent number: 8518965Abstract: The present invention embraces bis-acridine and bis-quinoline intercalators having a bis(4-aminophenyl)ether tether, and diglycolate salts thereof, for selectively decreasing colon cancer and glial cell proliferation and preventing or treating colon cancers and gliomas.Type: GrantFiled: July 13, 2010Date of Patent: August 27, 2013Assignee: Trustees of Dartmouth CollegeInventors: Gordon W. Gribble, Dmitry A. Androsov
-
Publication number: 20130217671Abstract: The present invention directs a compound represented by formula (I).Type: ApplicationFiled: July 28, 2011Publication date: August 22, 2013Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Raymond Huntley, Joel R. Walker, Helene Decomez
-
Publication number: 20130217709Abstract: The invention provides novel cyclic amine azaheterocyclic carboxamide according to Formula (I), Formula (II) and Formula (III) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: July 28, 2011Publication date: August 22, 2013Applicant: MERCK PATENT GMBHInventors: Bayard R. Huck, Xiaoling Chen, Constantin Neagu, Reinaldo Jones, Yufang Xiao, Igor Mochalkin
-
Patent number: 8513284Abstract: A series of amino-substituted fused pyridine and pyrazine derivatives, in particular amino-substituted quinoline and quinoxaline derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: GrantFiled: February 11, 2010Date of Patent: August 20, 2013Assignee: UCB Pharma, S.A.Inventors: Daniel Rees Allen, Julien Alistair Brown, Roland Burli, Alan Findlay Haughan, Jonathan David MacDonald, Elizabeth Anne Saville-Stones, Andrew Sharpe
-
Publication number: 20130210861Abstract: Methods of treating cardiovascular disease in patients predisposed to or afflicted with kidney disease, particularly chronic kidney disease, are described. In such methods, therapeutically effective amounts of chloroquine-based compounds, for example, hydroxychloroquine, are administered to prevent or otherwise ameliorate arthrosclerosis and other cardiovascular diseases.Type: ApplicationFiled: December 9, 2012Publication date: August 15, 2013Inventors: Ashutosh M. SHUKLA, Sudhir V. SHAH
-
Publication number: 20130202556Abstract: Methods of treating a hepatitis C virus (HCV) related disease, such as HCV infections in subjects non-responsive to anti-HCV therapy, are described herein, comprising administering to the subject a therapeutically effective amount of hydroxychloroquine. An antiviral agent may be co-administered with the hydroxychloroquine. Methods utilizing synergistic combinations of hydroxychloroquine and an antiviral agent are disclosed. Further disclosed are compositions comprising hydroxychloroquine and an antiviral agent, as well as hydroxychloroquine and uses thereof for the treatment of a hepatitis C virus (HCV) related disease.Type: ApplicationFiled: March 15, 2013Publication date: August 8, 2013Applicants: Genoscience Pharma SAS, Panmed Ltd.Inventor: Philippe Halfon
-
Publication number: 20130203768Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: September 28, 2011Publication date: August 8, 2013Inventors: Michael Berger, Christopher Kern, Marko Eck, Jörg Schröder
-
Publication number: 20130189274Abstract: Methods for treating breast cancer, specifically cancers resistant to treatment with one or more known breast cancer treatment drugs, and related patient selection strategies for predicting patient response to drug therapy, such strategies including detecting the presence or absence in a patient of one or more of PIK3CA gene amplification, a mutation in PIK3CA, and a decrease in PTEN protein expression, and treating a patient positive for the presence of one or more of same by administering to the subject a pan-ErbB tyrosine kinase inhibitor.Type: ApplicationFiled: December 6, 2010Publication date: July 25, 2013Inventors: Anna Berkenblit, Christina Marie Coughlin, Jay Marshall Feingold, Daniel Stephen Johnston, Andrew Louis Strahs, Charles Michael Zacharchuk
-
Patent number: 8492404Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including autoimmune disease and inflammation. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, L, R1, R2 and R3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of the present invention, methods of use such as treatment of Lck and/or c-Kit kinase mediated diseases by administering the compounds of the invention, or compositions including one or more compounds of the invention, and intermediates and processes useful for the preparation of compounds of the present invention.Type: GrantFiled: May 26, 2010Date of Patent: July 23, 2013Assignee: Amgen Inc.Inventors: Matthew W. Martin, David C. McGowan
-
Publication number: 20130178499Abstract: The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: October 7, 2011Publication date: July 11, 2013Applicant: N30 PHARMACEUTICALS, INC.Inventors: Xicheng Sun, Jian Qiu, Adam Stout
-
Publication number: 20130178494Abstract: The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy.Type: ApplicationFiled: June 29, 2012Publication date: July 11, 2013Applicant: Academia SinicaInventors: Tsann-Long SU, Ting-Chao Chou, Te-Chuang Lee