Patents Issued in May 4, 2017
  • Publication number: 20170121303
    Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.
    Type: Application
    Filed: October 20, 2016
    Publication date: May 4, 2017
    Inventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller
  • Publication number: 20170121304
    Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.
    Type: Application
    Filed: October 20, 2016
    Publication date: May 4, 2017
    Inventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller
  • Publication number: 20170121305
    Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.
    Type: Application
    Filed: October 20, 2016
    Publication date: May 4, 2017
    Inventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller
  • Publication number: 20170121306
    Abstract: The invention relates to a polymorphic form of [5-fluoro-3-({2-[(4-fluorobenzene)sulfonyl]pyridin-3-yl}methyl)-2-methylindol-1-yl]-acetic acid which has higher solublity than other forms and is therefore useful for preparing stable pharmacetical formulations.
    Type: Application
    Filed: May 1, 2015
    Publication date: May 4, 2017
    Inventors: Rolf HILFIKER, Katja GROSSE-SENDER
  • Publication number: 20170121307
    Abstract: The present invention relates to polymorphic forms of compound 1 or 1a and processes for preparing compound 1 and 1a polymorphs, which are useful as antifungal agents. In particular, the invention seeks to provide a new methodology for preparing polymorphs of compound 1 and substituted derivatives thereof.
    Type: Application
    Filed: March 17, 2016
    Publication date: May 4, 2017
    Inventors: William J. Hoekstra, David Dale Wirth, Tracy Ehiwe, Thierry Bonnaud
  • Publication number: 20170121308
    Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as a medicament such as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies and the like, and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof. wherein each symbol is as described in the attached DESCRIPTION.
    Type: Application
    Filed: June 11, 2015
    Publication date: May 4, 2017
    Inventors: Masaki OGINO, Eiji KIMURA, Shinkichi SUZUKI, Tomoko ASHIZAWA, Toshihiro IMAEDA, Ikuo FUJIMORI, Ryosuke ARAI
  • Publication number: 20170121309
    Abstract: The present invention relates to certain intermediates useful in the preparation of certain benzoimidazol-2-yl pyrimidines and processes for preparing them.
    Type: Application
    Filed: November 2, 2016
    Publication date: May 4, 2017
    Inventors: Diego Broggini, Matteo Conza, Oliver Flögel, Stefan Horns, Susanne Lochner, Guangrong Tang, Zhaobin Wang, Lucie Lovelle
  • Publication number: 20170121310
    Abstract: The present invention relates to salt forms of the Pim kinase inhibitor N-{(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of Pim kinase-related diseases such as cancer.
    Type: Application
    Filed: September 9, 2016
    Publication date: May 4, 2017
    Inventors: Zhongjiang Jia, Ganfeng Cao, Qiyan Lin, Yongchun Pan, Lei Qiao, Vaqar Sharief, Chongsheng Eric Shi, Michael Xia, Changsheng Zheng, Jiacheng Zhou, Qun Li
  • Publication number: 20170121311
    Abstract: The disclosures herein relate to novel compounds of formula wherein Ar1 and R1 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
    Type: Application
    Filed: October 28, 2016
    Publication date: May 4, 2017
    Inventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Bucknell, Francesca Deflorian, Mark Pickworth, Jonathan Stephen Mason
  • Publication number: 20170121312
    Abstract: Described herein are compounds that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
    Type: Application
    Filed: November 1, 2016
    Publication date: May 4, 2017
    Inventors: Jason D. Brubaker, Joseph L. Kim, Kevin J. Wilson, Douglas Wilson, Lucian V. DiPietro
  • Publication number: 20170121313
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: May 26, 2015
    Publication date: May 4, 2017
    Inventors: Jing DENG, Hui LEI, Xin MA, Feng REN, Wei CAI, Xichen LIN
  • Publication number: 20170121314
    Abstract: The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: January 12, 2017
    Publication date: May 4, 2017
    Applicant: GRÜNENTHAL GMBH
    Inventors: STEFAN SCHUNK, Melanie Reich, Florian Jakob, Nils Damann, Michael Haurand, Achim Kless, Marc Rogers, Kathy Sutton
  • Publication number: 20170121315
    Abstract: The present application relates to novel heterobicyclically substituted 4-oxobutanoic acid derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of respiratory, pulmonary and cardiovascular disorders.
    Type: Application
    Filed: June 8, 2015
    Publication date: May 4, 2017
    Inventors: Hartmut BECK, Volkhart Min-Jian LI, Yolanda CANCHO GRANDE, Andreas TIMMERMAN, Dirk BROHM, Hannah JÖRIßEN, Pamela BOGNER, Michael GERISCH, Dieter LANG
  • Publication number: 20170121316
    Abstract: It relates to the use of compounds of formula (I?), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, as anticancer agents and as agents for generating induced pluripotent stem cells. Compounds of formula (I?), wherein R2? is an alcoxy group, a hydrocarbon chain or a ring system, and R1, R3, and R4 are as defined herein, are dual inhibitors of histone methyltransferases and DNA methyltransferases. It also relates to the compounds of formula (I?), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, wherein R2? is phenyl or 5- to 6-membered heteroaromatic ring, both optionally fused to another rings (i.e., compounds of formula (I)). It also relates to pharmaceutical or veterinary compositions containing compounds of formula (I).
    Type: Application
    Filed: March 30, 2015
    Publication date: May 4, 2017
    Inventors: Xabier AGUIRRE ENA, Julen OYARZABAL SANTAMARINA, Felipe PRÓSPER CARDOSO, Maria Obdulia RABAL GRACIA, Juan Roberto RODRÍGUEZ MADOZ, Edurne SAN JOSÉ ENÉRIZ
  • Publication number: 20170121317
    Abstract: A method for producing a composition of glycidyl ethers synthesised from furan derivatives (furan glycidyl ethers), partly characterized by azeotropic distillation performed under reduced pressure and without the addition of a catalyst. Such products are used to produce epoxy resins, with the aim of forming a three-dimensional macromolecular network. With the compositions of the invention the cross-linking density of the network is increased, allowing the production of a material which is more resistant, both chemically and mechanically, and has a higher glass transition temperature (Tg) than the same materials produced with compositions of furan glycidyl ethers synthesized at atmospheric pressure according to prior art.
    Type: Application
    Filed: May 20, 2015
    Publication date: May 4, 2017
    Inventors: Clothilde BUFFE, Mathias IBERT
  • Publication number: 20170121318
    Abstract: The invention relates to compositions and methods for inhibiting Krüppel-like Factor 10 (KLF10) for modulation of T regulatory cells and cancer immunotherapy.
    Type: Application
    Filed: October 28, 2016
    Publication date: May 4, 2017
    Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
    Inventor: Mark Feinberg
  • Publication number: 20170121319
    Abstract: The invention relates to dihydro-hydantoin compounds of the formula (I) wherein X, Rb, Rc, R2 and R3 are as defined in the specification. Furthermore, the present invention relates to processes and intermediates for making compounds of formula (I), to herbicidal compositions comprising these compounds and to methods of using these compounds to control plant growth.
    Type: Application
    Filed: June 12, 2015
    Publication date: May 4, 2017
    Applicant: Syngenta Participations AG
    Inventors: Alan Joseph HENNESSY, James Alan MORRIS, Mangala PHADTE, Timothy Robert DESSON, Jake GOODWIN-TINDALL, Sally Elizabeth RUSSELL, Jutta Elisabeth BOEHMER, Donn Warwick MOSELEY
  • Publication number: 20170121320
    Abstract: The disclosures herein relate to novel compounds of formula wherein W, X and Y1, Y2, Y3 and Y4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.
    Type: Application
    Filed: January 18, 2017
    Publication date: May 4, 2017
    Inventors: Miles Stuart Congreve, John Andrew Christopher, Benjamin Gerald Tehan, Sukhbinder Singh Klair, Sarah Joanne Aves
  • Publication number: 20170121321
    Abstract: The present invention includes novel compounds and methods for preventing or treating diseases associated with and/or caused by overexpression and/or uncontrolled activation of a tyrosine kinase in a subject in need thereof. In certain embodiments, the compounds of the present invention comprise a tyrosine kinase inhibitor, a linker and a ubiquitin ligase binder. The methods of the present invention comprise administering to the subject an pharmaceutically effective amount of at least one compound of the invention.
    Type: Application
    Filed: November 2, 2016
    Publication date: May 4, 2017
    Inventors: Craig CREWS, Momar TOURE, Eunhwa KO, Saul Jaime-Figueroa
  • Publication number: 20170121322
    Abstract: The present invention relates to BET protein-inhibitory, especially BRD4-inhibitory 3,4-dihydropyrido[2,3-b]pyrazinones with a meta-substituted aromatic amino or ether group of the general formula (I) in which A, X, Y, R1, R2, R3, R4, R5, R6 and n are each as defined in the description, to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders, especially in the case of tumour disorders. Furthermore, this invention relates to the use of BET protein inhibitors in viral infections, in neurodegenerative disorders, in inflammatory diseases, in atherosclerotic disorders and in male fertility control.
    Type: Application
    Filed: June 15, 2015
    Publication date: May 4, 2017
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Norbert SCHMEES, Bernard HAENDLER, Detlef STÖCKIGT, Richard Alexander BISSELL, Richard Alexander BOUGLAS, Ian STEFANUTI, Stephan SIEGEL
  • Publication number: 20170121323
    Abstract: The invention provides compounds as CDK small-molecule inhibitors and uses thereof, the compounds can be used for treating inflammation and cell proliferation diseases. The novel compound of the invention is a powerful cyclin-dependent kinase 4 (CDK 4) or cyclin-dependent kinase-6 (CDK 6) inhibitor.
    Type: Application
    Filed: July 23, 2015
    Publication date: May 4, 2017
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Bing Liu, Yingjun ZHANG, Linlin NIE, Shun BAI, Mingyu GUAN, Xuke LI, Changchung CHENG
  • Publication number: 20170121324
    Abstract: A series of pyrazolo[3,4-b]pyridine derivatives that are substituted at the 4-position by a diaza monocyclic, bridged bicyclic or spirocyclic moiety, being selective inhibitors of phosphatidylinositol-4-kinase III? (PI4KIII?) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
    Type: Application
    Filed: June 11, 2015
    Publication date: May 4, 2017
    Inventors: Daniel James Ford, James Thomas Reuberson
  • Publication number: 20170121325
    Abstract: The present application relates to compounds and methods for the modulation (e.g., inhibition) of the enzyme indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase (IDO/TDO), and methods of treating diseases and disorders in which IDO/TDO plays a role.
    Type: Application
    Filed: October 28, 2016
    Publication date: May 4, 2017
    Inventors: Ben C. Askew, Takeru Furuya
  • Publication number: 20170121326
    Abstract: Disclosed are substituted aromatic N-heterocyclic compounds. The disclosed compounds typically exhibit kinase inhibition activity, for example, and inhibit Mnk1 kinase and/or Mnk2 kinase. The disclosed compounds may be used in pharmaceutical compositions and methods for treating diseases or disorders associated with Mnk1 kinase activity and/or Mnk2 kinase activity, such as cancers, diabetes, autism, and fragile X syndrome.
    Type: Application
    Filed: October 28, 2016
    Publication date: May 4, 2017
    Applicant: Northwestern University
    Inventors: Gary E. Schiltz, Rama K. Mishra, Leonidas C. Platanias, Javier Izquierdo-Ferrer
  • Publication number: 20170121327
    Abstract: The invention provides compounds of formula (I): wherein X is and the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: November 2, 2016
    Publication date: May 4, 2017
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, John R. Jacobsen, Anne-Marie Beausoleil, Gary E. Brandt, Melissa Fleury, Lan Jiang, Cameron Smith, Steven D.E. Sullivan, Lori Jean Van Orden, Pierre-Jean Colson, Gene Timothy Fass, Miroslav Rapta, Noah Benjamin, Marta Dabros, Venkat R. Thalladi
  • Publication number: 20170121328
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Application
    Filed: November 9, 2016
    Publication date: May 4, 2017
    Inventors: George D. Hartman, Scott Kuduk
  • Publication number: 20170121329
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Application
    Filed: November 15, 2016
    Publication date: May 4, 2017
    Inventors: George D. Hartman, Scott Kuduk
  • Publication number: 20170121330
    Abstract: The present disclosure relates to a process and new intermediates for the synthesis of (R)-praziquantel, which is obtained through four steps in proper order, that is, condensation reaction, reduction reaction, acylation reaction and ring-closing reaction, using (1R)-2-substituted-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid as starting material. Overall, the present disclosure provides a (R)-praziquantel product with higher optical purity through a process route that is more cost effective and environmentally friendly.
    Type: Application
    Filed: January 11, 2017
    Publication date: May 4, 2017
    Inventor: Mingxin Qian
  • Publication number: 20170121331
    Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2 and R3 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
    Type: Application
    Filed: October 28, 2016
    Publication date: May 4, 2017
    Inventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Bucknell, Francesca Deflorian, Mark Pickworth, Jonathan Stephen Mason
  • Publication number: 20170121332
    Abstract: The present invention relates to a purine compound useful as a kinase inhibitor.
    Type: Application
    Filed: January 9, 2017
    Publication date: May 4, 2017
    Inventors: DiZhong Chen, Meredith Williams
  • Publication number: 20170121333
    Abstract: Described herein are methods for making folic acid derivatives, intermediates, pharmaceutical compositions and uses thereof.
    Type: Application
    Filed: June 3, 2016
    Publication date: May 4, 2017
    Inventors: Gerald S. Jones, JR., Joseph P. St. Laurent, Scott A. Goodrich
  • Publication number: 20170121334
    Abstract: Crystalline forms of pemetrexed diacid are provided (Forms 1 and 2) which are readily produced for either laboratory-scale or industrial scale. Processes for the preparation of Forms 1 and 2 are also provided.
    Type: Application
    Filed: May 10, 2016
    Publication date: May 4, 2017
    Inventors: Ying-Tzu Lin, Kuan-Hsun Wang, Wei-Shuo Lo, Wen-Wei Lin, Wan-Yin Cheng
  • Publication number: 20170121335
    Abstract: The present invention describes new pyrazolo-pyrimidine derivatives which are generally interacting with MALT1 proteolytic and/or autoproteolytic activity, and in particular which may inhibit said activity. The present invention further describes the synthesis of said new pyrazolo-pyrimidine derivatives, their use as a medicament, especially by interacting with MALT1 proteolytic and/or autoproteolytic activity.
    Type: Application
    Filed: May 27, 2015
    Publication date: May 4, 2017
    Applicant: NOVARTIS AG
    Inventors: Carole Pissot Soldermann, Jean Quancard, Achim Schlapbach, Oliver Simic, Marina Tintelnot-Bromley, Thomas Zoller
  • Publication number: 20170121336
    Abstract: The present invention relates to solid state forms of a p-toluenesulfonic acid salt (PTSA) of the selective PI3K delta inhibitor (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one (TGR-1202). The present invention also relates to methods of preparing the same, pharmaceutical compositions containing them, and methods of treating a PI3K kinase mediated disease or disorder, such as cancer, by administering the same.
    Type: Application
    Filed: May 26, 2015
    Publication date: May 4, 2017
    Applicant: Rhizen Pharmaceuticals SA
    Inventor: Swaroop K. VAKKALANKA
  • Publication number: 20170121337
    Abstract: A series of fused bicyclic heteroaromatic derivatives of formula (I), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase III? (PI4KIII?) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
    Type: Application
    Filed: June 11, 2015
    Publication date: May 4, 2017
    Inventors: Helen Tracey Horsley, Qiuya Huang, Judi Charlotte Neuss, James Thomas Reuberson, Bart Vanderhoydonck
  • Publication number: 20170121338
    Abstract: The present disclosure relates to an amino pyran ring derivative and a composition and use thereof, and in particular, to an amino pyran ring derivative represented by general formula (I) or a stereoisomer, a pharmaceutically acceptable salt or a prodrug thereof, a pharmaceutical composition comprising the derivative, and their medical use in the manufacture of a di-peptidyl peptidase IV (DPP-IV) inhibitor, in formula (I) the substituents are defined the same as those in the specification.
    Type: Application
    Filed: May 14, 2015
    Publication date: May 4, 2017
    Inventors: Chen Zhang, Jianmin Wang, Caihu Li, Yonggang Wei
  • Publication number: 20170121339
    Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds A1, A2, A3, A4, A5, A6, A7, W1, R1, R2, R3, R4, R5a, R5b, R6, R7, R7a, R7b, R8, R8a, R8b, R9, R9a, R9b and R10 and subscripts “m” and “n” are as defined in the specification. The inventive Formula I compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
    Type: Application
    Filed: October 28, 2016
    Publication date: May 4, 2017
    Inventors: Paul A. Sprengeler, Siegfried H. Reich, Justin T. Ernst, Stephen E. Webber
  • Publication number: 20170121340
    Abstract: Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth.
    Type: Application
    Filed: June 10, 2015
    Publication date: May 4, 2017
    Inventors: Tao WANG, Zhongxing Zhang, Kyle E. Parcella, Kyle J. Eastman, John F. Kadow
  • Publication number: 20170121341
    Abstract: Optically active 2-hydroxytetrahydrothienopyridine derivatives represented by Formula I and pharmaceutically acceptable salts, preparation method and use in the manufacture of a medicament thereof are disclosed. The pharmacodynamic experiment results show that the present compounds of Formula I are useful for inhibiting platelet aggregation. The pharmacokinetic experiment results show that the present compound of Formula I can be converted in vivo into pharmacologically active metabolites and are therefore useful for inhibiting platelet aggregation. Therefore, the present compounds are useful for the manufacture of a medicament for preventing or treating thrombosis and embolism related diseases.
    Type: Application
    Filed: September 26, 2016
    Publication date: May 4, 2017
    Applicant: Jiangsu Vcare PharmaTech Co., Ltd.
    Inventors: Hong-Bin Sun, Jiaqi Shan, Boyu Zhang, Fang Yuan
  • Publication number: 20170121342
    Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.
    Type: Application
    Filed: October 4, 2016
    Publication date: May 4, 2017
    Inventors: Philip Jones, Maria Emilia Di Francesco, Alessia Petrocchi, Christopher L. Carroll, Joe Marszalek, Barbara Czako, Ryan Johnson, Jay Theroff
  • Publication number: 20170121343
    Abstract: The present invention provides a substituted pyridine compound of the formula I or an agriculturally suitable salt or N-oxide thereof, wherein the variables in the formula I are defined as in the description. Substituted pyridine compounds of formula I are useful as herbicides.
    Type: Application
    Filed: April 7, 2015
    Publication date: May 4, 2017
    Inventors: Gilbert BESONG, Matthias WITSCHEL, Ruediger REINGRUBER, Helmut KRAUS, Thomas SEITZ, Liliana PARRA RAPADO, Trevor William NEWTON, Gerd KRAEMER, Richard Roger EVANS, Michael RACK
  • Publication number: 20170121344
    Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment 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: January 9, 2017
    Publication date: May 4, 2017
    Applicant: Siga Technologies, Inc.
    Inventors: Dongcheng DAI, James R. BURGESON, Shanthankumar R. TYAVANAGIMATT, Chelsea OLSEN, Dennis E. HRUBY
  • Publication number: 20170121345
    Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
    Type: Application
    Filed: March 31, 2015
    Publication date: May 4, 2017
    Inventors: Johnnie Y. Ramphal, Brad Owen Buckman, Kumaraswamy Emayan, John Beamond Nicholas, Scott D. Seiwert
  • Publication number: 20170121346
    Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds A1, A2, A3, A4, A5, W1, Y, R1, R2, R3, R4, R5, R6a, R6b, R7, R8, R8a, R8b, R9, R9a, R9b, and R10 and subscript “n” are as defined in the specification. The inventive Formula I compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
    Type: Application
    Filed: October 28, 2016
    Publication date: May 4, 2017
    Inventors: Paul A. Sprengeler, Siegfried H. Reich, Justin T. Ernst, Stephen E. Webber, Mike Shaghafi, Douglas Murphy, Chinh Tran
  • Publication number: 20170121347
    Abstract: The present invention relates to an amorphous solid form of (4S)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one, and processes for its preparation, which is an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and is useful in the treatment of various diseases such as cancer.
    Type: Application
    Filed: October 28, 2016
    Publication date: May 4, 2017
    Inventors: Shili Chen, William Frietze, Zhongjiang Jia, Pingli Liu, Jiacheng Zhou
  • Publication number: 20170121348
    Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
    Type: Application
    Filed: October 28, 2016
    Publication date: May 4, 2017
    Inventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Bucknell, Francesca Deflorian, Mark Pickworth, Jonathan Stephen Mason
  • Publication number: 20170121349
    Abstract: The present invention relates to small molecule compounds having the general formula (I): wherein A is a moiety selected from the group consisting of formulae (A) to (K) and their use in the treatment of bacterial infections, in particular Tuberculosis.
    Type: Application
    Filed: June 22, 2015
    Publication date: May 4, 2017
    Inventors: Jaeseung KIM, Sunhee KANG, Juhee KANG, Sumi LEE, Jeong Jea SEO, Mooyoung SEO
  • Publication number: 20170121350
    Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. 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 provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Application
    Filed: January 11, 2017
    Publication date: May 4, 2017
    Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Douglas G. Stafford, Jianjun Xu
  • Publication number: 20170121351
    Abstract: The disclosure provides an improved synthesis for a zinc-lysine complex having the formula [Zn(C6H14N2O2)2Cl]+Cl?, in which zinc chloride is reacted with lysine, in aqueous solution. The disclosure also provides oral care and personal care compositions comprising the complex prepared by the synthesis, and methods of using these complexes and compositions.
    Type: Application
    Filed: June 18, 2014
    Publication date: May 4, 2017
    Applicant: Colgate-Palmolive Company
    Inventors: Shiri Nawrocki, Ravi SUBRAMANYAM, Long PAN
  • Publication number: 20170121352
    Abstract: The invention relates to a novel class of compounds that exhibit activity inhibitory activity toward arginase, and pharmaceutical compositions comprising the compounds of the invention. Also provided herein are methods of treating cancer with the arginase inhibitors of the invention.
    Type: Application
    Filed: October 28, 2016
    Publication date: May 4, 2017
    Inventors: Eric B. Sjogren, Jim Li, Michael Van Zandt, Darren Whitehouse