Patents Issued in March 1, 2018
  • Publication number: 20180057448
    Abstract: A compound having formula I for histone deacetylase inhibition is provided: or a pharmaceutically acceptable salt or hydrate thereof wherein R is alkyl, C6-18 aryl, C5-18 heteroaryl, C8-22 alkylaryl, C8-22 alkylheteroaryl, or halo.
    Type: Application
    Filed: August 25, 2017
    Publication date: March 1, 2018
    Inventor: MARY KAY PFLUM
  • Publication number: 20180057449
    Abstract: The present invention relates to a pharmaceutical composition for treating or preventing CNS disorders containing a carbamate derivative compound and/or pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or prevention CNS disorders comprising administering a carbamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or prevention of CNS disorders.
    Type: Application
    Filed: February 28, 2017
    Publication date: March 1, 2018
    Inventor: Yong Moon CHOI
  • Publication number: 20180057450
    Abstract: The present invention provides a compound of the formula (I): wherein, A is R6(R7)s, N, O, S, or —NR5—; R6 is an s-valent organic group; R7 is each independently, —O—, —S—, —NR5— or —O—P(?O)OR4?—; R2 and R3 are each independently a hydrogen atom or a hydrocarbon group; R4? is each independently, a hydrocarbon group; R5 is each independently, a hydrogen atom or a hydrocarbon group; and s is an integer of 1-10.
    Type: Application
    Filed: March 10, 2016
    Publication date: March 1, 2018
    Applicants: DAIKIN INDUSTRIES, LTD., TOKYO INSTITUTE OF TECHNOLOGY
    Inventors: Tadashi KANBARA, Tsuyoshi NOGUCHI, Toshikazu TAKATA, Hiromitsu SOGAWA, Toyokazu TSUTSUBA
  • Publication number: 20180057451
    Abstract: Provided herein are various methods for forming alkylaromatic sulfonate compositions and blended alkylaromatic sulfonate compositions, and such compositions themselves. The methods of various embodiments include obtaining a C8-C30 hydrocarbon mixture, optionally treating the mixture to concentrate the mixture in sulfonatable aromatics, and sulfonating the mixture to form the alkylaromatic sulfonates. The mixture or treated mixture may be blended with linear alkyl benzene (LAB) compositions and sulfonated, and/or the alkylaryl sulfonates may be blended with linear alkylbenzene sulfonate (LAS) compositions, to form the blended alkylaromatic sulfonates of some embodiments. These compositions and processes for making them may be tailored to serve a variety of end uses, such as detergents in cleaning solutions or for enhanced oil recovery operations, and/or as low foaming and/or hydrotropic additives in detergent formulations, and the like.
    Type: Application
    Filed: August 9, 2017
    Publication date: March 1, 2018
    Inventors: Tracie L. Owens, Virginia M. Reiner, Mosha H. Zhao, Jingwen Zhang, Beatrice M. Gooding, James R. Bielenberg
  • Publication number: 20180057452
    Abstract: Provided herein are various methods for forming alkylaromatic sulfonate compositions and blended alkylaromatic sulfonate compositions, and such compositions themselves. The methods of various embodiments include obtaining a C8-C30 hydrocarbon mixture, optionally treating the mixture to concentrate the mixture in sulfonatable aromatics, and sulfonating the mixture to form the alkylaromatic sulfonates. The mixture or treated mixture may be blended with linear alkyl benzene (LAB) compositions and sulfonated, and/or the alkylaryl sulfonates may be blended with linear alkylbenzene sulfonate (LAS) compositions, to form the blended alkylaromatic sulfonates of some embodiments. These compositions and processes for making them may be tailored to serve a variety of end uses, such as detergents in cleaning solutions or for enhanced oil recovery operations, and/or as low foaming and/or hydrotropic additives in detergent formulations, and the like.
    Type: Application
    Filed: August 9, 2017
    Publication date: March 1, 2018
    Inventors: Mosha H. Zhao, Virginia M. Reiner, Jingwen Zhang, Tracie L. Owens
  • Publication number: 20180057453
    Abstract: Provided herein are various methods for forming alkylaromatic sulfonate compositions and blended alkylaromatic sulfonate compositions, and such compositions themselves. The methods of various embodiments include obtaining a C8-C30 hydrocarbon mixture, optionally treating the mixture to concentrate the mixture in sulfonatable aromatics, and sulfonating the mixture to form the alkylaromatic sulfonates. The mixture or treated mixture may be blended with linear alkyl benzene (LAB) compositions and sulfonated, and/or the alkylaryl sulfonates may be blended with linear alkylbenzene sulfonate (LAS) compositions, to form the blended alkylaromatic sulfonates of some embodiments. These compositions and processes for making them may be tailored to serve a variety of end uses, such as detergents in cleaning solutions or for enhanced oil recovery operations, and/or as low foaming and/or hydrotropic additives in detergent formulations, and the like.
    Type: Application
    Filed: August 9, 2017
    Publication date: March 1, 2018
    Inventors: Virginia M. Reiner, Jingwen Zhang, Tracie L. Owens, Mosha H. Zhao
  • Publication number: 20180057454
    Abstract: Isosulfan blue and processes for the preparation thereof are provided. A process is also provided for preparation of the intermediate, 2-chlorobenzaldehyde-5-sulfonic acid, sodium salt of formula (2), used in the preparation thereof and a procedure for the isolation of benzaldehyde-2,5-disulfonic acid, di-sodium salt of the formula (3). Also provided is a process for the preparation of an isoleuco acid of formula (4), which upon oxidation gives rise to isosulfan blue of pharmaceutical grade which can be used for preparation of pharmaceutical formulations. The isolation and purification procedures provided in the process provide substantially pure isosulfan blue with HPLC purity 99.5% or greater.
    Type: Application
    Filed: November 2, 2017
    Publication date: March 1, 2018
    Applicant: Apicore US LLC
    Inventors: Ravishanker Kovi, Satyam Nampalli, Peter Xavier Tharial
  • Publication number: 20180057455
    Abstract: The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.
    Type: Application
    Filed: August 29, 2017
    Publication date: March 1, 2018
    Inventors: KAP-SUN YEUNG, Katharine A. Grant-Young, Juliang Zhu, Mark G. Saulnier, David B. Frennesson, David R. Langley, Piyasena Hewawasam, Tao Wang, Zhongxing Zhang, Zhaoxing Meng, Li-Qiang Sun, Eric Mull, Paul Michael Scola
  • Publication number: 20180057456
    Abstract: Dual function compounds are provided that may be inhibitors of histone deacetylase (HDAC) and activators of ataxia telangiectasia mutated (ATM). Pharmaceutical compositions and methods of use are also provided that utilize such compounds.
    Type: Application
    Filed: November 6, 2017
    Publication date: March 1, 2018
    Inventors: Scott GRINDROD, Mira JUNG, Milton BROWN, Anatoly DRITSCHILO
  • Publication number: 20180057457
    Abstract: The present disclosure relates to a method of synthesizing 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine (ceritinib) and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing ceritinib.
    Type: Application
    Filed: March 4, 2015
    Publication date: March 1, 2018
    Applicant: Novartis AG
    Inventors: Mark Clinton Davis, Baoqing Gong, Denis Har, Tobias Kapferer, Xuchun Zheng
  • Publication number: 20180057458
    Abstract: Described herein are compounds that are LOXL2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.
    Type: Application
    Filed: March 3, 2016
    Publication date: March 1, 2018
    Inventors: Martin W. ROWBOTTOM, John Howard HUTCHINSON, David LONERGAN
  • Publication number: 20180057459
    Abstract: The present invention relates to a novel process for producing of 2,3-dichloro-5-(trichloromethyl)pyridine by using PCl5 as chlorinating agent at elevated temperature and pressure.
    Type: Application
    Filed: November 3, 2017
    Publication date: March 1, 2018
    Applicant: Cheminova A/S
    Inventor: Casper Stoubeak ANDERSEN
  • Publication number: 20180057460
    Abstract: This disclosure relates to picolinamides of Formula I and their use as fungicides.
    Type: Application
    Filed: August 30, 2017
    Publication date: March 1, 2018
    Applicant: Dow AgroSciences LLC
    Inventors: Zachary A. Buchan, Yu Lu, David M. Jones, Kevin G. Meyer, Chenglin Yao
  • Publication number: 20180057461
    Abstract: This disclosure relates to picolinamides of Formula I and their use as fungicides.
    Type: Application
    Filed: August 30, 2017
    Publication date: March 1, 2018
    Applicant: Dow AgroSciences LLC
    Inventors: Zachary A. Buchan, Yu Lu, David M. Jones, Kevin G. Meyer, Chenglin Yao
  • Publication number: 20180057462
    Abstract: The present invention relates to novel substituted 2-difluoromethyl-nicotin(thio)carboxanilides derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
    Type: Application
    Filed: February 15, 2016
    Publication date: March 1, 2018
    Inventors: CHRISTOPHE DUBOST, SIMON MAECHLING, II, PHILIPP WINTER, ULRIKE WACHENDORFF-NEUMANN, CYRIL MONTAGNE, JEAN-PIERRE VORS, STEPHANE BRUNET
  • Publication number: 20180057463
    Abstract: This disclosure relates to picolinamide N-oxides of Formula I and their use as fungicides.
    Type: Application
    Filed: August 30, 2017
    Publication date: March 1, 2018
    Applicant: Dow AgroSciences LLC
    Inventors: Jared W. Rigoli, Kevin G. Meyer, Chenglin Yao, Brian A. Loy, Brannon Sam
  • Publication number: 20180057464
    Abstract: Provided herein are novel processes and methods for making 4-[(3-[(4-cyclopropylcarbonyl)piperazin-1-yl]carbonyl)-4-fluorophenyl]methyl(2H)phthalazin-1-one (Olaparib) and intermediates thereof. Olaparib is a poly ADP ribose polymerase (PARP) inhibitor useful in the treatment of cancers. Benefits of the present disclosure include the use of less toxic compounds and improved yields.
    Type: Application
    Filed: August 23, 2017
    Publication date: March 1, 2018
    Inventors: Tsung-Yu HSIAO, Yung-Hung CHANG
  • Publication number: 20180057465
    Abstract: The invention relates to novel heterocyclic compounds of Formula (I) which inhibit necroptosis and methods for their use. The compounds may be useful in the treatment of conditions associated with deregulated necroptosis.
    Type: Application
    Filed: February 10, 2016
    Publication date: March 1, 2018
    Inventors: Guillaume Laurent Lessene, Jean-Marc Garnier, Anthony Nicholas Cuzzupe, John Thomas Feutrill, Peter Edward Czabotar, Pooja Sharma
  • Publication number: 20180057466
    Abstract: Compounds of Formula (I), which are activators of long form cyclic nucleotide phosphodiesterase-4 (PDE4) enzymes, are provided. Methods and uses of these compounds for the treatment or prevention of disorders requiring a reduction of second messenger responses mediated by cyclic 3?,5?-adenosine monophosphate (cAMP) are also described.
    Type: Application
    Filed: March 18, 2016
    Publication date: March 1, 2018
    Applicant: MIRONID LIMITED
    Inventor: Julia Adam
  • Publication number: 20180057467
    Abstract: The present invention relates to novel triazole derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.
    Type: Application
    Filed: March 29, 2016
    Publication date: March 1, 2018
    Inventors: GORKA PERIS, JUERGEN BENTING, II, PETER DAHMEN, ULRIKE WACHENDORFF-NEUMANN, PIERRE-YVES COQUERON, PIERRE GENIX, STEPHANE BRUNET, RICARDA MILLER, DAVID BERNIER, JEAN-PIERE VORS, SVEN WITTROCK, PHILIPPE KENNEL, SEBASTIEN NAUD, RUTH MEISSNER
  • Publication number: 20180057468
    Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.
    Type: Application
    Filed: October 30, 2017
    Publication date: March 1, 2018
    Inventor: Gary David Annis
  • Publication number: 20180057469
    Abstract: The invention relates to various polymorphic forms and amorphous form of sodium 4-((3-(4-cyclo-hexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzate, including the polymorphic form A, mixtures of the polymorphs, process for the preparation thereof and the use thereof in a pharmaceutical composition containing thereof.
    Type: Application
    Filed: July 13, 2017
    Publication date: March 1, 2018
    Applicant: Purdue Pharma L.P.
    Inventors: Jay Jie-Qiang WU, Ling Wang
  • Publication number: 20180057470
    Abstract: Chemical entities of Formula (I): Including enantiomers thereof, wherein R1 has any of the values described herein, and compositions comprising such chemical entities; their preparation; and their use in various methods, including the treatment of depression, pain, cognitive disorders, neurodegenerative disorders, and other neurological and peripheral disorders.
    Type: Application
    Filed: August 31, 2016
    Publication date: March 1, 2018
    Inventors: Laurent Gomez, Mark Eben Massari
  • Publication number: 20180057471
    Abstract: Compounds for use as electrolyte in a non-aqueous redox battery are provided, including an N-substituted phenothiazine compound according to the formula: R? is alkyl and R is selected from alkyl, aryl, alkylaryl, alkoxyaryl, alkylcarboxyl, arylcarbonyl, haloalkyl, perfluoroalkyl, glycol, polyether, haloaryl, a negative electrolyte, a polymerizable unit, and a polymer.
    Type: Application
    Filed: August 22, 2017
    Publication date: March 1, 2018
    Inventors: Susan A. Odom, Aman Preet Kaur, Matthew D. Casselman, N. Harsha Attanayake
  • Publication number: 20180057472
    Abstract: Ester derivatives of sobetirome with enhanced CNS distribution are disclosed.
    Type: Application
    Filed: June 6, 2017
    Publication date: March 1, 2018
    Applicant: OREGON HEALTH & SCIENCE UNIVERSITY
    Inventors: Thomas S. Scanlan, Andrew Placzek, Tapasree Banerji, Sky Ferrara, James Matthew Meinig
  • Publication number: 20180057473
    Abstract: The method for the epoxidation of propene comprises continuously reacting propene with hydrogen peroxide in the presence of a homogeneous epoxidation catalyst in a reaction mixture comprising an aqueous liquid phase and an organic liquid phase using a loop reactor with mixing of the liquid phases, withdrawing aqueous phase from the loop reactor and extracting it by liquid-liquid-extraction using propene as extractant to provide an extract comprising propene and propene oxide.
    Type: Application
    Filed: February 3, 2016
    Publication date: March 1, 2018
    Applicant: Evonik Degussa GmbH
    Inventors: Juergen Stock, Daniel REIN, Jörg SCHALLENBERG, Georg Friedrich THIELE
  • Publication number: 20180057474
    Abstract: Compounds having a structure of Formula I and compositions comprising these compounds are provided. Uses of such compounds and compositions are provided for treatment or prophylaxis of viral infection. In particular, compounds and compositions may be for use in the treatment or prophylaxis of viral influenza.
    Type: Application
    Filed: February 16, 2017
    Publication date: March 1, 2018
    Inventors: Stephen Withers, Andrew Graham Watts, Jin Hyo Kim, Tom Wennekes
  • Publication number: 20180057475
    Abstract: The present invention is directed to a class of anti-inflammatory, antioxidant nitroalkene compounds used in biological or biochemical applications to reduce oxidative stress or damage. The nitroalkene compounds described herein further avoid disadvantageous metabolism currently present in this field.
    Type: Application
    Filed: August 23, 2016
    Publication date: March 1, 2018
    Applicant: Institut Pasteur de Montevideo
    Inventors: Carlos Batthyány, Gloria Virginia López, Rosina Dapueto, Carlos Escande, Jorge Rodriguez Duarte
  • Publication number: 20180057476
    Abstract: Process for increasingly producing D-Lactide and meso lactide by depolymerizing by back biting polylactide (PLA) said process which comprises: (i) Depolymerizing polylactide into its corresponding dimeric cyclic esters by heating the polylactide in the presence of a catalyst system comprising a catalyst and a co-catalyst in a reaction zone at temperature and pressure at which the polylactide is molten; (ii) Forming a vapor product stream from the reaction zone; (iii) Removing the vapor product stream and optionally condense it; (iv) Recovering, either together or separately meso-lactide, D-lactide and L-lactide.
    Type: Application
    Filed: November 6, 2017
    Publication date: March 1, 2018
    Inventors: Christian Penu, Benjamine Belloncle
  • Publication number: 20180057477
    Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to compounds of formula (I), as described herein, compositions containing them and their CM use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
    Type: Application
    Filed: March 9, 2016
    Publication date: March 1, 2018
    Applicant: NOVARTIS AG
    Inventors: Jane BROWN, Thomas David MCCARTHY, Alan NAYLOR, John Paul WATTS
  • Publication number: 20180057478
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: May 23, 2017
    Publication date: March 1, 2018
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Publication number: 20180057479
    Abstract: Inhibitor compounds of Bcr-Abl and Bcr-Abl mutants including Bcr-Abl T315I mutant protein are disclosed. Compositions comprising the inhibitor compounds and methods of using the compounds in the treatment of leukemia such as chronic myelogenous leukemia are also disclosed.
    Type: Application
    Filed: August 24, 2017
    Publication date: March 1, 2018
    Inventors: Matthew B. Soellner, Sameer Phadke
  • Publication number: 20180057480
    Abstract: The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: March 21, 2016
    Publication date: March 1, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, Jonathan E. Wilson, Meng Yang, Dann Parker, Zack Zhiqiang Guo, Alejandro Crespo, Deping Wang, Troy McCracken
  • Publication number: 20180057481
    Abstract: The invention relates to solid forms of cenicriviroc mesylate, methods of their preparation, pharmaceutical compositions thereof and methods of their use.
    Type: Application
    Filed: August 30, 2017
    Publication date: March 1, 2018
    Inventors: Pasit PHIASIVONGSA, Martin Ian COOPER, Emma Kay SHARP
  • Publication number: 20180057482
    Abstract: The invention provides methods of synthesizing a viral protease inhibitor in high yield, without using expensive catalysts or challenging reaction conditions.
    Type: Application
    Filed: November 6, 2017
    Publication date: March 1, 2018
    Inventors: Russell D. Cink, Kirill A. Lukin, Marvin R. Leanna, Matthew J. Pelc, Timothy B. Towne, Dennie S. Welch, Kenneth M. Engstrom, Matthew M. Ravn, Richard D. Bishop, Gang Zhao, Jianzhang Mei, Jeff M. Kallemeyn, David R. Hill, Michael J. Abrahamson, Westin H. Morrill
  • Publication number: 20180057483
    Abstract: The present invention includes novel RAD51 inhibitors. The compounds of the invention may be useful in preventing or treating cancer in a subject in need thereof. The present invention also includes methods of preventing or treating cancer in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of the invention.
    Type: Application
    Filed: March 1, 2016
    Publication date: March 1, 2018
    Applicant: The Regents of the University of California
    Inventors: Jiewen ZHU, Wen-Hwa LEE, Hongyuan CHEN, Xuning GUO, Xia-Long QUI
  • Publication number: 20180057484
    Abstract: The present invention is directed to an improved process for the preparation of compounds of Formula (II) and Formula (III), which are useful in the inhibition of PDE10. In particular, the present invention is directed to an improved process for the preparation of 1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, which is useful in the inhibition of PDE10.
    Type: Application
    Filed: April 7, 2017
    Publication date: March 1, 2018
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas L. Little, Wayne Douglas Luke, Elisabeth C. A. Brot, Marco Jonas, Michael James McDermott, Karl E. Reineke
  • Publication number: 20180057485
    Abstract: The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Application
    Filed: March 16, 2016
    Publication date: March 1, 2018
    Inventors: Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Ulrike Obst Sander, Jens-Uwe Peters, Thomas Woltering
  • Publication number: 20180057486
    Abstract: Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
    Type: Application
    Filed: August 28, 2017
    Publication date: March 1, 2018
    Inventors: Liangxing Wu, Fenglei Zhang, Song Mei, Wenqing Yao
  • Publication number: 20180057487
    Abstract: The present disclosure provides compounds of formula (I) to (III) as glutaminase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders involving glutamine.
    Type: Application
    Filed: August 31, 2017
    Publication date: March 1, 2018
    Inventors: Prashant K Bhavar, Swaroop K. Vakkalanka, Srikant Viswanadha, Gayatri Swaroop Merikapudi, Govindarajulu Babu
  • Publication number: 20180057488
    Abstract: The present invention provides compounds for the prevention or treatment of cancer or a bacterial or viral infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the prevention or treatment of cancer or a bacterial or viral infection in a subject.
    Type: Application
    Filed: November 7, 2017
    Publication date: March 1, 2018
    Inventors: Milton H. Werner, Terence A. Kelly
  • Publication number: 20180057489
    Abstract: Provided herein is a compound, 1-(4-(3-amino-[1,2,3]triazolo[1,5-a]pyridin-4-yl)phenyl)-3-(3-chlorophenyl)urea, pharmaceutical compositions thereof and crystal forms thereof. Also provided are particles (e.g., nanoparticles) comprising the compound, and pharmaceutical compositions thereof that are mucus penetrating. Also provided herein are methods and kits for using the compound, and pharmaceutical compositions thereof for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Application
    Filed: December 10, 2015
    Publication date: March 1, 2018
    Inventors: Pawel Wojciech Nowak, Minh Ngoc Nguyen, Elizabeth Enlow, Winston Zapanta Ong
  • Publication number: 20180057490
    Abstract: Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
    Type: Application
    Filed: September 1, 2017
    Publication date: March 1, 2018
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Andrew Felts
  • Publication number: 20180057491
    Abstract: Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
    Type: Application
    Filed: September 1, 2017
    Publication date: March 1, 2018
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Andrew Felts, Aaron M. Bender
  • Publication number: 20180057492
    Abstract: The field of the DISCLOSURE lies in active materials for organic image sensors. The present disclosure relates to naphtalene diimide-based molecules and naphtalene diimide dimer-based molecules. The present disclosure relates to transparent N materials and/or to transparent P materials including the molecule(s) according to the present disclosure and their use in absorption layer(s), photoelectric conversion layer(s) and/or an organic image sensor and methods for their synthesis. The present disclosure also relates to photoelectric conversion layer(s) including an active material according to the present disclosure, to a device, including active material(s) according to the present disclosure or photoelectric conversion layer(s) according to the present disclosure. Moreover, the present disclosure relates to an organic image sensor including photoelectric conversion layer(s) according to the present disclosure.
    Type: Application
    Filed: March 31, 2016
    Publication date: March 1, 2018
    Applicant: Sony CORPORATION
    Inventors: Silvia ROSSELLI, Nikolaus KNORR, Tzenka MITEVA, Gabriele NELLES, Vitor DEICHMANN, David DANNER, William E. FORD, Dennis CHERCKA, Vladimir YAKUTKIN, Lars-Peter SCHELLER
  • Publication number: 20180057493
    Abstract: A morphinan derivative represented by the following general formula (I): (wherein R1 represents hydrogen, C1-10 alkyl, cycloalkylalkyl where the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms, etc., R2 represents heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S and at least one carbon atom as ring-constituting atoms, containing at least one set of adjacent ring-constituting atoms bound by a double bond, and further substituted with at least one oxo group, Y binds to a carbon atom as a ring-constituting atom of R2, R3, R4, and R5 represent hydrogen; hydroxy, etc., R6a and R6b represent hydrogen, etc., R7 and R8 represent hydrogen, etc., R9 and R10, which are the same or different, represent hydrogen, etc., X represents O or CH2, and Y represents C(?O)), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an anxiolytic drug, antidepressant, etc.
    Type: Application
    Filed: March 17, 2016
    Publication date: March 1, 2018
    Applicants: UNIVERSITY OF TSUKUBA, SCHOOL JURIDICAL PERSON KITASATO INSTITUTE, NATIONAL CENTER OF NEUROLOGY AND PSYCHIATRY, NIPPON CHEMIPHAR CO., LTD.
    Inventors: Hiroshi NAGASE, Hideaki FUJII, Akiyoshi SAITOH, Eriko NAKATA, Masaaki HIROSE, Isao OOI, Kohei HAYASHIDA
  • Publication number: 20180057494
    Abstract: The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, for use as a human PDE1 inhibitor.
    Type: Application
    Filed: August 18, 2017
    Publication date: March 1, 2018
    Inventors: Mark David Rekhter, Qing Shi
  • Publication number: 20180057495
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: November 2, 2017
    Publication date: March 1, 2018
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER
  • Publication number: 20180057496
    Abstract: The present invention relates to heterocyclyl linked imidazopyridazine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PI3K? inhibitors. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: December 18, 2015
    Publication date: March 1, 2018
    Inventors: Laurence Anne Mevellec, Lieven Meerpoel, Sophie Coupa, Virginie Sophie Poncelet, Isabelle Noelle Constance Pilatte, Elisabeth Therese Jeanne Pasquier, Didier Jean-Claude Berthelot, Olivier Alexis Georges Querolle, Christophe Meyer, Patrick Rene Angibaud, Christophe Gabriel Marcel Demestre, Guillaume Jean Maurice Mercey
  • Publication number: 20180057497
    Abstract: The present invention provides substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors wherein X, ring A, ring B, L1, L2, R1, R2, R3, R4, R6, m, n and p have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.
    Type: Application
    Filed: March 8, 2016
    Publication date: March 1, 2018
    Applicant: Aurigene Discovery Technologies Limited
    Inventors: Susanta Samajdar, Ramulu Poddutoori, Subhendu Mukherjee, Rajeev Goswami