The Hetero Ring Is Six-membered And Includes At Least Two Nitrogens And No Other Hetero Atoms Patents (Class 514/157)
  • Patent number: 10669235
    Abstract: The present invention relates inter alia to a compound of formula (I) wherein R1, R2 and R3, are as defined in the specification and to compositions comprising the same and to the use of the compounds and to compositions of the compounds in treatment, for example in the treatment of fibrotic diseases or interstitial lung diseases, in particular idiopathic pulmonary fibrosis.
    Type: Grant
    Filed: March 8, 2017
    Date of Patent: June 2, 2020
    Assignee: RESPIVERT LIMITED
    Inventors: Iain Walters, Louise Birch, Stephen Paul Collingwood, Christopher Scott Stevenson
  • Patent number: 10479793
    Abstract: Compounds of formula I or a stereoisomer or pharmaceutically-acceptable salt thereof, are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition.
    Type: Grant
    Filed: November 17, 2016
    Date of Patent: November 19, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: David S. Weinstein, Ryan M. Moslin, Yanlei Zhang, Daniel S. Gardner, Joseph B. Santella, Charles M. Langevine, Sylwia Stachura
  • Patent number: 10383876
    Abstract: The present invention relates:—to 2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo-[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide dihydrochloride salt of formula (II): or a tautomer, solvate or hydrate thereof;—to methods of preparing said dihydrochloride salt;—to said dihydrochloride salt for the treatment and/or prophylaxis of a disease;—to the use of said dihydrochloride salt for the preparation of a medicament for the treatment and/or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, more particularly for the treatment or prophylaxis of a cancer, particularly lung cancer, in particular non-small cell lung carcinoma, colorectal cancer, melanoma, pancreatic cancer, hepatocyte carcinoma, pancreatic cancer, hepatocyte carcinoma or breast cancer;—to a pharmaceutical composition comprising said dihydrochloride salt; and—to a pharmaceutical combination comprising said dihydrochloride salt in combination with one or more further pharmaceutical agent
    Type: Grant
    Filed: March 29, 2012
    Date of Patent: August 20, 2019
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jan-Georg Peters, Hans-Christian Militzer, Hartwig Müller
  • Patent number: 10335408
    Abstract: Compositions and methods of using nintedanib for improving the success rate of glaucoma filtration surgery are disclosed herein. Nintedanib can be used alone or in combination with an anti-metabolite drug in a topical or implant eye formulation.
    Type: Grant
    Filed: September 14, 2018
    Date of Patent: July 2, 2019
    Assignee: Cloudbreak Therapeutics, LLC
    Inventors: Jinsong Ni, Rong Yang
  • Patent number: 10221174
    Abstract: The present disclosure provides compounds having Formula I-A: and the pharmaceutically acceptable salts and solvates thereof, wherein A, X1, X2, X3 R1a, R1b, E, and are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a disease, disorder, or condition responsive to Bcl-2 protein inhibition such as cancer.
    Type: Grant
    Filed: August 1, 2018
    Date of Patent: March 5, 2019
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Jianyong Chen
  • Patent number: 9993485
    Abstract: An aqueous cyclodextrin-free solution of meloxicam suitable is provided for administration by needleless injection, containing a pharmacologically acceptable meloxicam salt of an organic or inorganic base and one or more suitable excipients.
    Type: Grant
    Filed: October 29, 2014
    Date of Patent: June 12, 2018
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Martin A. Folger, Stefan Henke, Bernhard Hassel, Bernd Zierenberg
  • Patent number: 9737559
    Abstract: The present invention is concerned with improved synergistic compositions effective in the treatment of diabetes and/or hyperglycemia. In particular, the present invention is concerned with synergistic compositions comprising inulin preparations having a defined degree of polymerisation (DP) of below about 25 and sulfonylureas and/or a sulfonamide and/or derivatives and/or metabolites thereof used in the treatment of Type-2 Diabetes Meliitus (T2DM). Said compositions are also used for preventing the development of, or ameliorating, side-effects or conditions in a subject treated with sulfonylurea and/or a sulfonamide compounds (and/or derivatives and/or metabolites thereof, or combinations thereof), said side-effects including hypoglycemia, gastrointestinal disturbances, fatigue, weight gain, and satiety.
    Type: Grant
    Filed: November 23, 2012
    Date of Patent: August 22, 2017
    Assignee: Ozstar Therapeutics Pty Ltd
    Inventor: Nick Naser Gorgani
  • Patent number: 9676708
    Abstract: Protected HNO donors designed to undergo non-enzymatic release at neutral pH via an intramolecular cyclization-elimination are disclosed. The rate of cyclization, and therefore HNO release, can be controlled by substituents and chain length. Thus, biologically useful HNO donors having tunable HNO release rates are provided.
    Type: Grant
    Filed: October 30, 2013
    Date of Patent: June 13, 2017
    Assignee: The Johns Hopkins University
    Inventors: John P. Toscano, Art D. Sutton
  • Patent number: 9439423
    Abstract: An antiparasitic agent for fish includes an inhibitor of folate synthesis and/or an inhibitor of folate activation as the active substance(s). A combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is disclosed. Sulfonamide is disclosed as suitable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist are disclosed as suitable inhibitors of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is effective against fish parasites belonging to the ciliate group.
    Type: Grant
    Filed: October 29, 2008
    Date of Patent: September 13, 2016
    Assignee: NIPPON SUISAN KAISHA, LTD.
    Inventors: Fumi Kawano, Noritaka Hirazawa
  • Patent number: 9315459
    Abstract: Crystalline forms of 4-[2-(4-methylphenylsulfanyl)-phenyl]piperidine and salts thereof are provided, e.g., for the treatment of neuropathic pain.
    Type: Grant
    Filed: November 14, 2014
    Date of Patent: April 19, 2016
    Assignee: H. Lundbeck A/S
    Inventors: Benny Bang-Andersen, Andre Faldt, Tine Bryan Stensbol, Silke Miller, Heidi Lopez De Diego
  • Patent number: 9265777
    Abstract: A method of controlling proliferation of fish parasites comprising the administration of 1 to 50 mg/kg fish body weight/day of an inhibitor of folate synthesis and/or an inhibitor of folate activation to fish continuously for 1 to 2 weeks. Using a combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is preferable, and a sulfonamide is preferable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist, etc., can be used as the inhibitor of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is particularly effective against parasites belonging to the ciliate group among fish parasites.
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: February 23, 2016
    Assignee: NIPPON SUISAN KAISHA, LTD.
    Inventors: Fumi Kawano, Noritaka Hirazawa
  • Patent number: 9125833
    Abstract: The present invention is in the field of oral, abuse resistant pharmaceutical compositions of opioid agonists, extended release pharmaceutical compositions of opioid agonists and extended release abuse resistant pharmaceutical compositions of opioid agonists and the use thereof. The present invention is also directed to extended release pharmaceutical compositions and the use thereof for preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering. The present invention is further directed at a method of preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering.
    Type: Grant
    Filed: April 26, 2008
    Date of Patent: September 8, 2015
    Assignee: Relmada Therapeutics, Inc.
    Inventor: Najib Babul
  • Patent number: 9060952
    Abstract: The present invention is a preservative formulation which includes a combination of at least two (2) compounds having bactericidal and/or fungicidal properties wherein the at least two (2) compounds is selected from the group consisting of methylisothiazolinone/piroctone olamine; caprylyl glycol/dehydroacetic acid; undecanol/dehydroacetic acid and lauryl alcohol/sorbic acid. The invention also includes preparations including such combination as well as a method of using the combination to reduce bacterial and fungal load of preparations.
    Type: Grant
    Filed: May 20, 2009
    Date of Patent: June 23, 2015
    Assignee: LONZA LTD.
    Inventors: Rosita Nunez, Larry Kent Hall, Crystal Maira, Joseph Kimler, Craig Carter
  • Publication number: 20150111857
    Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
  • Publication number: 20150094283
    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 2, 2015
    Inventor: Rakesh KUMAR
  • Patent number: 8946197
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: February 3, 2015
    Assignee: CHDI Foundation, Inc.
    Inventors: Celia Dominguez, John Wityak, Michael Prime, Stephen Martin Courtney, Christopher Yarnold, Frederick Brookfield, Richard Marston, Douglas Macdonald
  • Publication number: 20150031652
    Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
    Type: Application
    Filed: August 1, 2014
    Publication date: January 29, 2015
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
  • Publication number: 20150005265
    Abstract: The present invention provides methods and compositions for treating cancers using a combination of a CYP 1 7 inhibitor and an additional therapeutic agent which modulates the PBK/Akt/mTOR pathway. In one aspect, the invention provides methods for the treatment of a disorder in a human subject. In some embodiments, the disorder is a neoplastic disorder. In some embodiments, the neoplastic disorder is a cancer. In some embodiments, the method comprises administering to said subject a 17a-hydroxylase/C17,20-lyase inhibitor (CYP17 inhibitor) and an additional agent, wherein the additional agent is a PBK inhibitor and/or mTOR inhibitor.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 1, 2015
    Inventor: Susan Stewart
  • Patent number: 8921521
    Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: December 30, 2014
    Assignee: Ocera Therapeutics, Inc.
    Inventors: Eric Marsault, Carl St-Louis
  • Patent number: 8883766
    Abstract: In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: November 11, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Esther Martinborough, Tim Neubert, Tara Whitney, Danielle Lehsten, Tara Hampton, Nicole Zimmermann, Andreas P. Termin
  • Patent number: 8871248
    Abstract: Compositions containing a surface active agent and a sub-lethal amount of an antimicrobial agent and methods for using such compositions are provided herein.
    Type: Grant
    Filed: November 26, 2012
    Date of Patent: October 28, 2014
    Assignee: PluroGen Therapeutics, Inc.
    Inventors: George Rodeheaver, Adam Katz
  • Publication number: 20140243295
    Abstract: The present invention relates to: —use of a 2,3-dihydroimidazo[1,2-c]quinazoline compound, or of a pharmaceutical composition containing same, as a sole active agent, or of a combination of a) said compound or a pharmaceutical composition containing said compound and b) one or more further active agents, for the preparation of a medicament for the treatment or prophylaxis of cancer; —combinations of a) said compound and b) one or more further active agents; —a pharmaceutical composition comprising said compound as a sole active agent for the treatment of breast cancer; —a pharmaceutical composition comprising a combination of a) said compound and b) one or more further active agents; —use of biomarkers involved in the modification of Bel expression, HER family expression and/or activation, PIK3CA signaling and/or loss of PTEN for predicting the sensitivity and/or resistance of a cancer patient to said compound and providing a rationale-based synergistic combination as defined herein to increase sensitivity an
    Type: Application
    Filed: March 29, 2012
    Publication date: August 28, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ningshu Liu, Claudia Schneider
  • Patent number: 8796001
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: August 5, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger
  • Patent number: 8691573
    Abstract: The present invention relates compounds for stabilizing cells and methods of their use.
    Type: Grant
    Filed: December 3, 2009
    Date of Patent: April 8, 2014
    Assignee: The Scripps Research Institute
    Inventors: Yue Xu, Sheng Ding
  • Publication number: 20140018326
    Abstract: Compounds of Formula I are disclosed: wherein L, A, R1, R2, R3A, R3B, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 27, 2011
    Publication date: January 16, 2014
    Inventors: Oscar M. Moradei, Sheldon Crane, Daniel J. Mckay, Marie-Eve Lebrun, Vouy Linh Truong
  • Patent number: 8628751
    Abstract: The invention provides compounds, including compositions, preparations and formulations, and methods of using and making such compounds. Compounds of the present invention include pyrazine derivatives having a pyrazine core and a plurality of substituents. In some embodiments, pyrazine derivatives of the invention are pyrazine core compounds having one or more electron donating groups and one or more electron withdrawing groups optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.
    Type: Grant
    Filed: April 15, 2010
    Date of Patent: January 14, 2014
    Assignee: Medi Beacon Development, LLC
    Inventors: William L. Neumann, John N. Freskos
  • Publication number: 20140011770
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: September 10, 2013
    Publication date: January 9, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
  • Publication number: 20130345180
    Abstract: There are provided compounds of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as indicated in claim 1, useful in disorders where ZAP-70 and/or Syk inhibition plays a role or caused by a malfunction of signal cascades connected with FAK.
    Type: Application
    Filed: March 15, 2013
    Publication date: December 26, 2013
    Applicant: NOVARTIS AG
    Inventor: Novartis AG
  • Publication number: 20130310348
    Abstract: 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: Application
    Filed: July 25, 2013
    Publication date: November 21, 2013
    Applicants: State University
    Inventors: David H. Peyton, Steven Burgess
  • Publication number: 20130310344
    Abstract: The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
    Type: Application
    Filed: August 5, 2011
    Publication date: November 21, 2013
    Applicant: ASTRAZENECA AB
    Inventors: Robert Bruce Diebold, Thomas Gero, Paul Grover, Shan Huang, Stephanos Ioannidis, Claude Afona Ogoe, Jamal Carlos Saeh, Jeffrey Gilbert Varnes
  • Publication number: 20130303491
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.
    Type: Application
    Filed: July 22, 2013
    Publication date: November 14, 2013
    Applicant: Siga Technologies Inc.
    Inventors: Chelsea M. Byrd, Robert Jordan, Dongcheng Dai, Tove Bolken, Dennis E. Hruby
  • Publication number: 20130281403
    Abstract: The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.
    Type: Application
    Filed: June 7, 2013
    Publication date: October 24, 2013
    Inventors: Arnab K. Chatterjee, Advait S. Nagle, Tao Wu, David C. Tully, Kelli L. Kuhen
  • Publication number: 20130190258
    Abstract: Methods and small molecule compounds for inhibition of cancer cell proliferation are provided. One example of a class of compounds that may be used is represented by the compound of Formula I or a pharmaceutically acceptable salt, N-oxide or solvate thereof, wherein A, B, D, E, F, G, I, J, R, R1, R2, R2?, R3, R4, R5, R6, R7, R8, R9 are as described herein.
    Type: Application
    Filed: January 24, 2013
    Publication date: July 25, 2013
    Inventors: John CASHMAN, Mark MERCOLA, Dennis SCHADE, Masanao TSUDA
  • Patent number: 8481001
    Abstract: The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: July 9, 2013
    Assignee: Exelixis, Inc.
    Inventors: Peter Lamb, David Matthews
  • Publication number: 20130150334
    Abstract: Embodiments of topical formulations for administering compound I or a pharmaceutically acceptable salt or solvate thereof are disclosed. Embodiments of methods for using the topical formulations in the treatment of dermatological disorders such as cutaneous collagen vascular diseases, e.g., cutaneous lupus, also are disclosed.
    Type: Application
    Filed: December 6, 2012
    Publication date: June 13, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventor: Rigel Pharmaceuticals, Inc.
  • Patent number: 8454984
    Abstract: Methods for making antimicrobial resins and for forming coatings comprising antimicrobial resins on substrate surfaces are disclosed. The methods involve providing a mixture comprising about 15 weight % to about 80 weight % of a hydrophilic acrylic oligomer, about 10 weight % to about 80 weight % of a multifunctional acrylic monomer, about 5 weight % to about 40 weight % of an adhesion-promoting acrylic or vinyl monomer, and about 0.1 weight % to about 15 weight % of a metal salt; and exposing the mixture to a radiation source to cure at least a portion of the mixture, thereby forming an antimicrobial resin.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: June 4, 2013
    Assignees: Baxter International Inc., Baxter Healthcare SA
    Inventors: Vadim V. Krongauz, Dustin C. Cawthon, Michael Tung-Kiung Ling
  • Publication number: 20130116216
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Application
    Filed: November 12, 2010
    Publication date: May 9, 2013
    Inventors: Celia Dominguez, John Wityak, Michael Prime, Stephen Martin Courtney, Christopher Yarnold, Frederick Brookfield, Richard Marston, Douglas Macdonald
  • Publication number: 20130101661
    Abstract: Compositions containing a surface active agent and a sub-lethal amount of an antimicrobial agent and methods for using such compositions are provided herein.
    Type: Application
    Filed: November 26, 2012
    Publication date: April 25, 2013
    Applicant: PLUROGEN THERAPEUTICS, INC.
    Inventor: PLUROGEN THERAPEUTICS, INC.
  • Publication number: 20130053333
    Abstract: This invention relates to novel aminoquinoline derivatives of Formula (I) or Ia, or pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an aminoquinoline derivative, such as a derivative of primaquine.
    Type: Application
    Filed: January 19, 2011
    Publication date: February 28, 2013
    Inventor: Roger D. Tung
  • Publication number: 20130035310
    Abstract: The present invention relates to piperidine and piperazine phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.
    Type: Application
    Filed: October 2, 2012
    Publication date: February 7, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Esther Ann Martinborough, Lev Tyler Dewey Fanning, Urvi Jagdishbhai Sheth, Dean Mitchell Wilson, Andreas P. Termin, Timothy Donald Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
  • Publication number: 20130029944
    Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
    Type: Application
    Filed: June 20, 2012
    Publication date: January 31, 2013
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Yonghong Song, Qing Xu, Shawn M. Bauer, Zhaozhong J. Jia, Mukund Mehrotra, Anjali Pandey
  • Publication number: 20130023497
    Abstract: The present invention comprises inter alia triazine compounds as shown in formula (I) and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: June 7, 2010
    Publication date: January 24, 2013
    Inventors: Chunlin Tao, Qinwei Wang, Tulay Polat, Laxman Nallan, Neil Desai
  • Publication number: 20130023499
    Abstract: Certain chemical entities chosen from compounds represented by Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer (e.g., B-cell lymphoma and leukemia), autoimmune diseases, inflammatory diseases, acute inflammatory reactions, and allergic disorders. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Application
    Filed: January 4, 2012
    Publication date: January 24, 2013
    Applicant: Gilead Connecticut, Inc.
    Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, David M. ARMISTEAD, Joseph RAKER
  • Publication number: 20130004557
    Abstract: Methods for making antimicrobial resins and for forming coatings comprising antimicrobial resins on substrate surfaces are disclosed. The methods involve providing a mixture comprising about 15 weight % to about 80 weight % of a hydrophilic acrylic oligomer, about 10 weight % to about 80 weight % of a multifunctional acrylic monomer, about 5 weight % to about 40 weight % of an adhesion-promoting acrylic or vinyl monomer, and about 0.1 weight % to about 15 weight % of a metal salt; and exposing the mixture to a radiation source to cure at least a portion of the mixture, thereby forming an antimicrobial resin.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicants: BAXTER INTERNATIONAL INC.
    Inventors: Vadim V. Krongauz, Dustin C. Cawthon, Michael Tung-Kiung Ling
  • Publication number: 20120208790
    Abstract: In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.
    Type: Application
    Filed: April 27, 2012
    Publication date: August 16, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Esther Martinborough, Tim Neubert, Tara Whitney, Danielle Lehsten, Tara Hampton, Nicole Zimmermann, Andreas P. Termin
  • Patent number: 8242096
    Abstract: Ascorbic acid compositions in the form of a powder and/or granules contain as principle components L-ascorbic acid and/or a pharmaceutically acceptable salt thereof, and a high molecular (300 kDalton or higher) pectin. The compositions are compressible into tablets with improved mechanical strength and hardness.
    Type: Grant
    Filed: February 13, 2009
    Date of Patent: August 14, 2012
    Assignee: DSM IP Assets B.V.
    Inventors: Chyi-Cheng Chen, Bruno Leuenberger
  • Publication number: 20120190654
    Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: July 28, 2010
    Publication date: July 26, 2012
    Applicant: MERCK PATENT GMBH
    Inventors: Xiaoling Chen, Srinivasa R. Karra, Bayard R. Huck, Ruoxi Lan, Amanda E. Sutton, Andreas Goutopoulos, Brian L. Hodous, Reinaldo Jones
  • Publication number: 20120165298
    Abstract: The present invention includes novel compound and methods of treating a disease or disorder by antagonizing Bcl-2 family proteins, particularly compounds of formula (I): or pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Bcl-2 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: September 8, 2010
    Publication date: June 28, 2012
    Applicant: NOVARTIS AG
    Inventors: Karen Miller-Moslin, Bakary-Barry Toure, Michael Scott Visser, Naeem Yusuff
  • Publication number: 20120101072
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: December 21, 2011
    Publication date: April 26, 2012
    Inventors: Joseph A. Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Patent number: 8163720
    Abstract: The present invention relates to phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: April 24, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Esther Martinborough, Lev T. D. Fanning, Urvi Sheth, Dean Wilson, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson