Chalcogen Bonded Directly To Pyrimidine At 2-position Patents (Class 514/274)
  • Publication number: 20140314882
    Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 23, 2014
    Inventors: Frederick P. ROTH, Murat COKOL, Hon Nian CHUA
  • Publication number: 20140308336
    Abstract: Drug-eluting devices and methods for the treatment of tumors of the pancreas, biliary system, gallbladder, liver, small bowel, or colon, are provided. Methods include deploying a drug-eluting device having a film which includes a mixture of a degradable polymer and a chemotherapeutic drug, wherein the film has a thickness from about 2 ?m to about 1000 ?m, into a tissue site and releasing a therapeutically effective amount of the chemotherapeutic drug from the film to treat the tumor, wherein the release of the therapeutically effective amount of the drug from the film is controlled by in vivo degradation of the polymer at the tissue site.
    Type: Application
    Filed: April 10, 2014
    Publication date: October 16, 2014
    Applicants: THE GENERAL HOSPITAL CORPORATION, MASSACHUSETTS INSTITUTE OF TECHNOLOGY
    Inventors: Laura Indolfi, Elazer R. Edelman, Robert S. Langer, Jeffrey W. Clark, David T. Ting, Cristina Rosa Annamaria Ferrone, Matteo Ligorio
  • Publication number: 20140309234
    Abstract: The present invention provides methods for treating fibrotic diseases by administering a compound having the general structural formula (I)
    Type: Application
    Filed: March 10, 2014
    Publication date: October 16, 2014
    Applicant: ANGION BIOMEDICA CORP
    Inventors: Lambertus J.W.M Oehlen, Bijoy Panicker, Latha Paka
  • Publication number: 20140309226
    Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, in which X1, X2, R3, R4, R5, Rx, R7, R9, R10 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.
    Type: Application
    Filed: November 14, 2012
    Publication date: October 16, 2014
    Inventors: Jay Bradford Fell, John P. Fischer, Ronald J. Hinklin
  • Publication number: 20140309237
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: June 26, 2014
    Publication date: October 16, 2014
    Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
  • Publication number: 20140308342
    Abstract: The present invention relates to chimeric (preferably, bifunctional) compounds, compositions comprising those compounds and methods of treating cancer in a patient or subject, especially including metastatic cancer where cancer cells exhibit overexpression (heightened expression) of cell surface urokinase-type plasminogen activator receptor (urokinase receptor) compared to normal (non-cancerous) cells. The compounds preferably covalently bind to the urokinase receptor and recruit native antibodies of the patient or subject where the antibodies can selectively degrade and/or deactivate targeted cancer cells through antibody-dependent cellular phagocytosis and/or antibody-dependent cellular cytotoxicity (ADCC) against a large number and variety of cancers, thus providing cancer cell death and/or an inhibition of growth, elaboration and/or metastasis of the cancer, including remission and cure of the patient's cancer.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 16, 2014
    Inventors: David A. Spiegel, Charles E. Jakobsche
  • Patent number: 8859529
    Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: October 14, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K. C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • Patent number: 8859573
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Grant
    Filed: December 5, 2011
    Date of Patent: October 14, 2014
    Assignee: Glaxo Group Limited
    Inventors: Zehong Wan, Xiaomin Zhang, Jian Wang, Cheng Peng, Yun Jin, Yimin Hu
  • Patent number: 8859589
    Abstract: Compound represented by the formulae: wherein each R individually is H or aliphatic acyl or aromatic acyl group; X is selected from the group consisting of hydrogen, fluoro, chloro, bromo, iodo, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano, aryl and nitro; pharmaceutically acceptable salts thereof, prodrugs thereof and mixtures thereof are used as inhibitors of orthopoxviruses and for treating patients suffering from an orthopoxvirus infection such as, but not limited to, smallpox, cowpox, monkeypox and camelpox.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: October 14, 2014
    Assignee: Southern Research Institute
    Inventors: John A. Secrist, III, Kamal N. Tiwari, Joseph A. Maddry
  • Publication number: 20140303139
    Abstract: The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A1, X, A2, W1, W2, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Application
    Filed: August 31, 2012
    Publication date: October 9, 2014
    Inventors: Chiyou Ni, Laykea Tafesse, Jiangcho Yao, Mark Youngman, Minnie Park, Bin Shao
  • Publication number: 20140303112
    Abstract: The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.
    Type: Application
    Filed: April 9, 2013
    Publication date: October 9, 2014
    Inventors: Han-Min CHEN, Cheng-Yi KUO, Chun-Fang HUANG, Jiun-Tsai LIN
  • Publication number: 20140303137
    Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
    Type: Application
    Filed: April 5, 2013
    Publication date: October 9, 2014
    Inventors: Michael Mortimore, Julian Golec, Daniel Robinson, John Studley
  • Publication number: 20140303162
    Abstract: It is intended to provide a novel azabicyclo compound which exhibits both HSP90 inhibitory activity and cell proliferation inhibitory effect. Specifically disclosed is a compound represented by the following general formula (I) or a salt thereof: wherein X1 represents CH or N; any one of X2, X3 and X4 represents N, and the others represent CH; any one or two of Y1, Y2, Y3 and Y4 represent C—R4, and the others are the same or different and represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S and O; R2 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R3 and R4 represent —CO—R5 or the like.
    Type: Application
    Filed: April 1, 2014
    Publication date: October 9, 2014
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Makoto KITADE, Shuichi Ohkubo, Chihoko Yoshimura, Satoshi Yamashita, Hiromi Oshiumi, Takao Uno, Yuichi Kawai
  • Publication number: 20140301976
    Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
    Type: Application
    Filed: June 20, 2014
    Publication date: October 9, 2014
    Inventors: Erik J. VERNER, Martin SENDZIK, Chitra BASKARAN, Joseph J. BUGGY, James ROBINSON
  • Publication number: 20140303109
    Abstract: Water-soluble fluorinated analogs of natural curcumin, and particularly difluoro Knoevenagel condensates and Schiff bases, along with their corresponding copper (H) complexes have improved bioavailablity over curcumin. The fluorine-substituted analogs of curcumin are useful as chemopreventive and/or therapeutic agents against cancers and/or against the development of drug-resistant cancer. A preferred compound is (IE,6E)-1,7-bis(4-hydroxy-3-methoxyphenyl)hepta-1,6-diene{4(3,4 difluorobenzaldehyde)}-3,5-dione.
    Type: Application
    Filed: March 25, 2011
    Publication date: October 9, 2014
    Inventors: Fazlul H. Sarkar, Subhash Padhye
  • Publication number: 20140302173
    Abstract: A method for treating side effects of anticancer agent includes administering to a subject in need thereof a prophylactic and/or therapeutic agent containing a therapeutically effective amount of a compound shown by the following Formula (1): R1—NHCH2COCH2CH2COOR2 ??(I) wherein R1 represents a hydrogen atom or an acyl group, and R2 represents a hydrogen atom, a linear or branched alkyl group, a cycloalkyl group, an aryl group, or an aralkyl group, or a salt thereof.
    Type: Application
    Filed: October 5, 2012
    Publication date: October 9, 2014
    Applicants: NATIONAL UNIVERSITY CORPORATION KOCHI UNIVERSITY, SBI PHARMACEUTICALS CO., LTD.
    Inventors: Tohru Tanaka, Kyoko Tsuchiya, Masahiro Ishizuka, Motowo Nakajima, Hitoshi Nakagawa, Taro Shuin, Keiji Inoue, Hideo Fukuhara, Masayuki Tsuda, Mutsuo Furihata
  • Publication number: 20140296065
    Abstract: The present disclosure is related to the field agrochemicals including 5-fluorocytosine and its derivatives and their use as fungicides.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Zoltan L. Benko, Kristy Bryan, George E. Davis, Jeffrey B. Epp, Beth Lorsbach, Kevin G. Meyer, W. John Owen, Michael T. Sullenberger, Jeffery D. Webster, David H. Young, Chenglin Yao
  • Publication number: 20140296219
    Abstract: The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-?B activation to treat viral infections and inflammatory conditions.
    Type: Application
    Filed: November 14, 2013
    Publication date: October 2, 2014
    Applicant: UNIVERSITY OF MASSACHUSETTS
    Inventors: Robert W. Finberg, Evelyn A. Kurt-Jones, Shenghua Zhou
  • Publication number: 20140294806
    Abstract: This invention provides methods and compositions useful for treating early and late stage metastatic cancer to prevent or treat acquired resistance due to gene amplification or mutation in response to chemotherapeutic and/or targeted drugs. In particular, the methods and compositions include carboxiamidotriazole orotate (CTO) alone or in combination with specific regimens of chemotherapeutic and/or targeted drugs designed to overcome the genomic resistance raised to prior therapy.
    Type: Application
    Filed: April 1, 2013
    Publication date: October 2, 2014
    Inventor: Rashida A. Karmali
  • Publication number: 20140296176
    Abstract: The invention provides a method of treating a subject with cancer, particularly leukemia, lymphoma, solid cancer such as colorectal cancer, gastric cancer, bladder cancer, non-small cell lung cancer, and breast cancer, comprising administering to the subject a compound of formulae (I) 40 or (Ia) in combination with an antimetabolite such as methotrexate, pemetrexed, cytarabine or nelarabine, or 5-fluorouracil, or capecitabine or their derivatives.
    Type: Application
    Filed: August 17, 2012
    Publication date: October 2, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: David Proia, Julie Friedland
  • Publication number: 20140296268
    Abstract: The present invention is directed to methods and compositions for suppressing lymphangiogenesis, angiogenesis and/or tumor growth. The methods comprise contacting the tumor with a compound that (i) stabilizes a protein kinase in the inactive state and (ii) is not an ATP competitive inhibitor of the protein kinase in the active state.
    Type: Application
    Filed: February 7, 2011
    Publication date: October 2, 2014
    Inventors: Eric A. Murphy, David A. Cheresh, Lee Daniel Arnold
  • Publication number: 20140296244
    Abstract: A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.
    Type: Application
    Filed: February 17, 2014
    Publication date: October 2, 2014
    Inventors: Michael J. Gerber, Christopher Dufton
  • Publication number: 20140294766
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 2, 2014
    Inventor: AbbVie Inc.
  • Publication number: 20140296240
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Gary Mark COPPOLA, Yuki IWAKI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Gary Michael KSANDER, Muneto MOGI, Robert SUN
  • Publication number: 20140296232
    Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Applicants: Massachusetts General Hospital, The Broad Institute, Inc.
    Inventors: Deborah Hung, Sarah Stanley, Tomohiko Kawate, Noriakie Iwase, Motohisa Shimizu
  • Publication number: 20140296203
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
    Type: Application
    Filed: October 25, 2012
    Publication date: October 2, 2014
    Inventors: Jongwon Lim, Elizabeth Helen Kelley, Joey L. Methot, Hua Zhou, Alessia Petrocchi, Faruk Mansoor, Christian Fischer, Brendan O'Boyle, David Joseph Guerin, Corey E. Bienstock, Christopher W. Boyce, Matthew H. Daniels, Danielle Falcone, Ronald D. Ferguson, Salem Fevrier, Xianhai Huang, Kathryn Ann Lipford, David L. Sloman, Kevin Wilson, Wei Zhou, David Witter, Milana M. Maletic, Phieng Siliphaivanh
  • Publication number: 20140296066
    Abstract: A compound of formula (I) (I), wherein R1 to R4 are, for example, each hydrogen, R5 is pyridyl, which has one or more substituents at least one of which is, for example, a 5 membered heterocycle; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 are, independently selected, from, for example, N, and C—H; and its use as a pesticidal agent.
    Type: Application
    Filed: October 31, 2012
    Publication date: October 2, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Thomas Pitterna, Olivier Loiseleur, Anthony Cornelius O'Sullivan, Torsten Luksch
  • Patent number: 8846746
    Abstract: The present invention provides a pyrazole compound of the following general Formula [Ib] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use: wherein each symbol is the same as defined in the description.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: September 30, 2014
    Assignee: Japan Tobacco Inc.
    Inventors: Tomoya Miura, Yosuke Ogoshi, Kazuhito Ueyama, Dai Motoda, Toshihiko Iwayama, Koichi Suzawa, Hironobu Nagamori, Hiroshi Ueno, Akihiko Takahashi, Kazuyuki Sugimoto
  • Patent number: 8846653
    Abstract: Methods are disclosed for treating neoplastic disorders, such as pancreatic cancer, using tocotrienols; namely, gamma-tocotrienol and delta tocotrienol. The antitumorogenic effects of these compounds are shown both in vitro and in vivo using several human pancreatic cancer cell lines and MIA-PACA2 human pancreatic cancer cells xenografted in nude mice. Also disclosed are methods of testing the efficacy of potential chemotherapeutic agents by measuring their effect on surrogate endpoint biomarkers, such as Ki-67 and p27. Associated compounds are also disclosed.
    Type: Grant
    Filed: October 16, 2012
    Date of Patent: September 30, 2014
    Assignee: University of South Florida
    Inventors: Mokenge P. Malafa, Said M. Sebti
  • Patent number: 8846023
    Abstract: 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: Grant
    Filed: September 9, 2013
    Date of Patent: September 30, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: 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
  • Publication number: 20140288108
    Abstract: An extrusion process for preparation of solid dispersion of lopinavir and ritonavir carried out in twin screw extruder.
    Type: Application
    Filed: November 28, 2012
    Publication date: September 25, 2014
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Ravindra Tiwari, Ravindra Agarwa, Janaki Raman Kailya, Ravi Kochhar
  • Publication number: 20140288105
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: EPIZYME, INC.
    Inventors: RICHARD CHESWORTH, LORNA HELEN MITCHELL, GIDEON SHAPIRO, OSCAR MIGUEL MORADEI
  • Publication number: 20140288049
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Application
    Filed: June 9, 2014
    Publication date: September 25, 2014
    Inventors: Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
  • Publication number: 20140286902
    Abstract: A pharmaceutical combination comprising a platinum-containing anticancer agent, and an Hsp90 inhibitor according to the following formulae (I) & (Ia), a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein. Also provided is a method of treating a proliferative disorder such as cancer in a subject in need thereof, using the pharmaceutical combination described herein.
    Type: Application
    Filed: November 1, 2012
    Publication date: September 25, 2014
    Inventor: David Proia
  • Publication number: 20140288106
    Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Applicant: Sanofi
    Inventors: Imre BATA, Peter BUZDER-LANTOS, Attila VASAS, Veronika BARTANE BODOR, Gyorgy FERENCZY, Zsuzsanna TOMOSKOZI, Gabor SZELECZKY, Sandor BATORI, Martin SMRCINA, Marcel PATEK, Aleksandra WEICHSEL, David Squire Thorpe
  • Publication number: 20140288107
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger, Gary D. Gustafson
  • Publication number: 20140286938
    Abstract: The present invention relates to spiroketal compounds that are useful in methods of treating or preventing protozoal infections, parasitic infections, bacterial infections, cell proliferative disorders and anti inflammatory disorders. The spiroketal compounds are also useful as immunosuppressive agents, and also in methods of controlling pests.
    Type: Application
    Filed: March 21, 2014
    Publication date: September 25, 2014
    Applicant: EcoBiotics Ltd
    Inventors: Paul Warren Reddell, Victoria Anne Gordon
  • Publication number: 20140288017
    Abstract: The present invention is directed to novel catechol diether compounds, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV 1 and 2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 25, 2014
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Publication number: 20140288048
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
  • Patent number: 8841314
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Grant
    Filed: May 2, 2013
    Date of Patent: September 23, 2014
    Assignee: Pfizer Inc.
    Inventors: David Hepworth, Roger B. Ruggeri
  • Patent number: 8841310
    Abstract: The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and/or nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: September 23, 2014
    Assignee: Janssen R & D Ireland
    Inventor: Paul Stoffels
  • Patent number: 8841447
    Abstract: The present invention is based on the discovery of a process for preparing pyrimidin-dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV).
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: September 23, 2014
    Assignee: Mapi Pharma Ltd.
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
  • Publication number: 20140274939
    Abstract: Kits and methods for treating disordered tissue caused by a virus in a mammal involve co-administration of a systemic anti-virus drug and topically administering an anti-infective composition. The systemic anti-virus drug is internally administered and disrupts or inhibits virus replication systemically within the mammal. Examples include nucleoside analogues, nucleoside analogue precursors, and nucleotide analogues. The topically administered anti-infective composition includes at least one anti-infective agent, such as an organohalide (e.g., benzalkonium chloride), and is formulated to penetrate below the disordered tissue surface and allow the anti-infective agent to kill viruses at the disordered tissue site. The anti-infective composition reduces the time and/or number of dosages required for the systemic anti-virus drug to treat the disordered tissue in the absence of topically administering the anti-infective composition. It also reduces or eliminates incidences of post-treatment neuralgia.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 18, 2014
    Applicant: QUADEX PHARMACEUTICALS, LLC
    Inventor: B. RON JOHNSON
  • Publication number: 20140275077
    Abstract: The present application provides compounds of Formula I or salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c, Y, R3, X, E and G are as defined herein, compositions, methods of treatment and uses thereof.
    Type: Application
    Filed: May 13, 2014
    Publication date: September 18, 2014
    Applicant: Cephalon, Inc.
    Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
  • Publication number: 20140275065
    Abstract: The present invention is directed to compounds of Formula I: wherein ring A is phenyl, naphthalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyl, thiazolyl, isoxazolyl, pyrazolyl, imidazothiazolyl, benzimidazolyl, or indazolyl; R1 is H, alkyl, alkoxy, hydroxyalkylene, OH, halo, phenyl, triazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, pyrazolyl, oxadiazolyl, pyrrolidinyl, thiophenyl, morpholinyl, or dialkylamino; R2 is H, alkyl, alkoxy, hydroxyalkylene, or halo; Z is NH, N-alkyl, or O; R5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl, optionally substituted with a one or two substituents independently selected from the group consisting of alkyl, alkoxy, or halo; and n is 0 or 1. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Inventors: Heather R. Coate, Curt A. Dvorak, Terry P. Lebold, Cathy Preville, Brock T. Shireman
  • Publication number: 20140283218
    Abstract: Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as insecticides and can be prepared in a manner known per se.
    Type: Application
    Filed: June 27, 2012
    Publication date: September 18, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Roger Graham Hall, Andrew Edmunds, Andre Jeanguenat, Thomas Pitterna, Sebastian Rendler
  • Publication number: 20140275094
    Abstract: There is provided a method of treating pulmonary hypertension in a patient in need thereof, said method comprising: administering a therapeutically effective amount of ambrisentan to the patient with pulmonary arterial hypertension, wherein the patient has been determined not to have idiopathic pulmonary fibrosis.
    Type: Application
    Filed: December 17, 2013
    Publication date: September 18, 2014
    Inventors: Hunter Campbell Gillies, Tobias Peschel, David J. Pizzuti
  • Publication number: 20140275029
    Abstract: The present invention relates to compounds of Formula (I), and solvates, hydrates, and pharmaceutically acceptable salts thereof, wherein X1, X1?, X1?, R1, R2 and R3 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Wenying Chai, Curt A. Dvorak, Wendy Eccles, James P. Edwards, Steven D. Goldberg, Paul J. Krawczuk, Alec D. Lebsack, Jing Liu, Daniel J. Pippel, Zachary S. Sales, Virginia M. Tanis, Mark S. Tichenor, John J. M. Wiener
  • Publication number: 20140275103
    Abstract: Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed. Combination therapy with antibodies and PK/PD data are also disclosed.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Aerpio Therapeutics Inc.
    Inventors: Kevin Peters, Robert Shalwitz, John Janusz, Alexander Smith
  • Patent number: 8835376
    Abstract: A process for making particles for delivery of drug nanoparticles is disclosed herein. The process comprises the steps of (a) forming a suspension of drug nanoparticles by mixing a precipitant solution with an anti-solvent solution under micro-mixing environment, where the formed nanoparticles have a narrow particle size distribution; (b) providing an excipient to at least one of the precipitant solution, the anti-solvent solution and the suspension of drug nanoparticles, the excipient being selected to maintain said drug nanoparticles in a dispersed state when in liquid form; and (c) drying the suspension of drug nanoparticles containing the excipient therein to remove solvent therefrom, wherein removal of the solvent causes the excipient to solidify and thereby form micro-sized matrix particles, each micro-sized particle being comprised of drug nanoparticles dispersed in a solid matrix of the excipient.
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: September 16, 2014
    Assignee: Nanomaterials Technology Pte Ltd
    Inventors: Zhigang Shen, Jimmy Sung Lai Yun, Jun Hu, Nital Arvind Jugade, Jiyao Zhang, Wenhao Chen, Zhe Wang, Lingyan Gao, William Glover, Jian Feng Chen