Patents Issued in February 1, 2018
  • Publication number: 20180030023
    Abstract: Methods for recovering monomers from polymers, such as polyurethanes (including thermoset polyurethanes) include heating the polymer to depolymerize the polymer and release the monomer. The monomer may be directly recovered. The polymer may include a poly(?-methyl-?-valerolactone) (PMVL) block and the monomer recovered may be ?-methyl-?-valerolactone (MVL).
    Type: Application
    Filed: October 10, 2017
    Publication date: February 1, 2018
    Inventors: Marc Andrew Hillmyer, Tessie Rose Panthani, Marie Elizabeth Vanderlaan, Deborah Kay Schneiderman, Alexander Michael Rauch Mannion, Derek Charles Batiste, Christopher Ward Macosko, Jay Z. Wang, Frank S. Bates
  • Publication number: 20180030024
    Abstract: A process for recovering tocotrienols/tocopherols from vegetable oil distillate comprising the steps of esterifying the vegetable oil distillate with an alcohol in the presence of an acid catalyst to convert the fatty acids contained therein to produce an esterified mixture comprising fatty acid esters, thereby reducing fatty acid content in the oil to less than 3% by weight; distilling the esterified mixture for separating and removing the fatty acid esters therefrom; transesterifying the distilled mixture with an alcohol in the presence of a basic catalyst for converting glycerides present therein to fatty acid esters and glycerine, forming a transesterified mixture comprising glycerine and fatty acid esters; purifying the transesterified mixture to substantially remove glycerine therefrom; and distilling the purified mixture to substantially remove fatty acid esters, producing a composition comprising a predetermined concentration of tocotrienols/tocopherols.
    Type: Application
    Filed: February 4, 2016
    Publication date: February 1, 2018
    Inventor: DAVID SUE SAN HO
  • Publication number: 20180030025
    Abstract: A method for producing lactide including the steps of: providing a solution of lactic acid in a volatile organic solvent, subjecting the solution to an evaporation step to remove volatile organic solvent and water, resulting in the formation of a composition including lactic acid oligomer, adding catalyst to the composition including lactic acid oligomer, and bringing the mixture to reaction conditions, to form lactide. It has been found that the process results in the efficient production of lactide with a high production rate and a good product quality.
    Type: Application
    Filed: February 11, 2016
    Publication date: February 1, 2018
    Applicant: PURAC BIOCHEM B.V.
    Inventors: Wim Jacob GROOT, Jan VAN KRIEKEN, Tanja DEKIC ZIVKOVIC, Andre Banier DE HAAN
  • Publication number: 20180030026
    Abstract: The present application provides novel inhibitors of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase, metabolites thereof, and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. A therapeutically effective amount of one or more of the compounds of formula (I) is useful in treating diseases resulting from dysregulation of the kynurenine pathway. Compounds of formula (I) act by inhibiting the enzymatic activity or expression of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxy-genase.
    Type: Application
    Filed: October 4, 2017
    Publication date: February 1, 2018
    Inventors: Monali Banerjee, Sandip Middya, Ritesh Shrivastava, Sushil Raina, Arjun Surya, Dharmendra B. Yadav, Veejendra K. Yadav, Kamal Kishore Kapoor, Aranapakam Venkatesan, Roger A. Smith, Scott K. Thompson
  • Publication number: 20180030027
    Abstract: Disclosed herein are reversible and irreversible inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are describeded, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Application
    Filed: April 12, 2017
    Publication date: February 1, 2018
    Inventors: Wei Chen, Zhaozhong J. Jia, William D. Thomas
  • Publication number: 20180030028
    Abstract: The present disclosure generally relates to methods of preparing nicotine and resolving R,S nicotine to enrich the (S)(?) enantiomer. The method may comprise combining N-methyl-2-pyrrolidone or a salt thereof with a nicotinate compound in the presence of a solvent and a strong base to form 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof; and reducing the 1-methyl-3-nicotinoyl-2-pyrrolidone or salt thereof in solution with Na2S2O4 to produce racemic nicotine or salt thereof. Resolving the racemic nicotine (or other enantiomeric mixture) may comprise combining the nicotine with (?)-O,O?-di-p-toluoyl-L-tartaric acid (L-PTTA).
    Type: Application
    Filed: October 6, 2017
    Publication date: February 1, 2018
    Applicant: NJOY, LLC
    Inventors: Bert WILLIS, Mohammed Moinuddin AHMED, Wesley FREUND, Douglas SAWYER
  • Publication number: 20180030029
    Abstract: 3-(3-Chloro-1H-pyrazol-1-yl)pyridine is prepared by cyclizing 3-hydrazinopyridine.dihydrochloride with commercially available 3-ethoxyacrylonitrile to provide 3-(3-amino-1H-pyrazol-1-yl)pyridine, and by converting the amino group to a chloro group by a Sandmeyer reaction.
    Type: Application
    Filed: October 9, 2017
    Publication date: February 1, 2018
    Inventors: Xiaoyong LI, Qiang YANG, Gary ROTH, Beth LORSBACH
  • Publication number: 20180030030
    Abstract: [Problem] A compound which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy is provided. [Means for Solution] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and have found that an amide compound or a salt thereof exhibits an EP4 receptor antagonistic action, thereby completing the present invention. The amide compound or a salt thereof has an EP4 receptor antagonistic action, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy.
    Type: Application
    Filed: March 25, 2015
    Publication date: February 1, 2018
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Takao OKUDA, Eisuke NOZAWA, Tohru UGAWA, Ryo MIZOGUCHI
  • Publication number: 20180030031
    Abstract: The present invention relates to compound of Formula (I) containing carbon-carbon linker, a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, a prodrug, a polymorph, N-oxide, S-oxide, or a carboxylic acid isostere thereof; processes for their preparation; pharmaceutical compositions comprising said compounds; and their use for the treatment of the diseases or disorders mediated by GPR120 receptor.
    Type: Application
    Filed: February 2, 2016
    Publication date: February 1, 2018
    Inventors: Rajiv SHARMA, Sanjay KUMAR, Vishal MAHAJAN, Komal BAJAJ, Pallavi GODSE
  • Publication number: 20180030032
    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: July 26, 2017
    Publication date: February 1, 2018
    Inventors: Jason D. BRUBAKER, LUCIAN V. DIPIETRO
  • Publication number: 20180030033
    Abstract: The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Application
    Filed: October 4, 2017
    Publication date: February 1, 2018
    Inventors: Hervé GENESTE, Sean Colm TURNER, Michael OCHSE, Karla DRESCHER, Lawrence A. BLACK, Katja JANTOS
  • Publication number: 20180030034
    Abstract: A compound of formula I wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Application
    Filed: October 4, 2017
    Publication date: February 1, 2018
    Inventors: John Lloyd, Heather Finlay, Prashantha Gunaga, Abhisek Banerjee, Ashokkumar Adisechan
  • Publication number: 20180030035
    Abstract: A compound having the structure according to formula III wherein: X is NH or S; R1 is H or (1C-4C)alkyl; R2 is (1C-4C)alkyl, phenyl or a monocyclic aromatic ring having one or more N—, O— or S— atoms in the ring, which alkyl, phenyl or aromatic ring is optionally substituted with one or more groups selected from (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, phenyloxy, phenylthio, halogen, or nitro; R3 and R4 are each independently H, (1C-6C)alkyl, (2C-6C) alkenyl, (2C-6C)alkynyl, cyano, (3C-6C)cycloalkyl, phenyl, a monocyclic aromatic ring having one or more N—, O— or S— atoms in the ring, a monocyclic non-aromatic ring having one or more N—, O— or S— atoms in the ring, each optionally substituted with hydroxyl, (1C-4C)alkoxy, phenyl, cycloalkyl, piperidyl, piperazinyl, furyl, thienyl, pirazinyl, pyrrolyl, 2H-pyrrolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyrrolidonyl, pyrrolinyl, imidazolinyl, imidazolyl, a monocyclic aromatic ring having one or more N—, O— or S— atoms in the r
    Type: Application
    Filed: October 10, 2017
    Publication date: February 1, 2018
    Applicants: Compound Handling B.V., Stichting Katholieke Universiteit
    Inventors: Onno Van Hooij, Jacobus Antonius Schalken, Hendrik Engelbertus Vietor, Dennis Patrick Piet, Petrus Emmanuel Marie Maas, Johann Heinrich Tijhuis, Sirik Deerenberg, Nanda Elisabeth Sprenkels, Siu Ha Tang
  • Publication number: 20180030036
    Abstract: The present invention provides a compound of Formula I, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.
    Type: Application
    Filed: December 7, 2015
    Publication date: February 1, 2018
    Applicants: MERCK SHARP & DOHME CORP., MOCHIDA PHARMACEUTICAL CO., LTD
    Inventors: Ting Zhang, Yi-Heng Chen, Liangqin Guo, Alan Hruza, Tianying Jian, Bing Li, Dongfang Meng, Dann L. Parker, Edward C. Sherer, Harold B. Wood, Isao Sakurada
  • Publication number: 20180030037
    Abstract: The present invention encompasses compounds of the formula (I) wherein the groups R1, Cy and Y are defined herein, which are suitable for the treatment of diseases related to BTK, and processes for making these compounds, pharmaceutical preparations containing these compounds, and their methods of use.
    Type: Application
    Filed: October 12, 2017
    Publication date: February 1, 2018
    Inventors: Todd BOSANAC, Joerg BENTZIEN, Michael Jason BURKE, Ryan Michael FRYER, Eric Thomas LARSON, Wang MAO, Bryan Patrick MCKIBBEN, Yue SHEN, Fariba SOLEYMANZADEH, Matt Aaron TSCHANTZ
  • Publication number: 20180030038
    Abstract: The present disclosure relates to amorphous and crystalline forms of 2-butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethyl amino)-,(2E)-, (2Z)-2-butenedioate (1:2) (afatinib dimaleate). The present disclosure also relates to process for the preparation of amorphous and crystalline forms of afatinib dimaleate. Further, the present disclosure relates to solid dispersion of amorphous afatinib dimaleate and the crystalline form of afatinib.
    Type: Application
    Filed: August 1, 2016
    Publication date: February 1, 2018
    Inventors: Ramakoteswara Rao Jetti, Anjaneyaraju Indukuri, Satish Beeravelly, Asharani Gorantla, B.A. Ramireddy, Ruchira M. Sarbajna, Sivalakshmidevi Arikatla
  • Publication number: 20180030039
    Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Application
    Filed: April 13, 2017
    Publication date: February 1, 2018
    Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
  • Publication number: 20180030040
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.
    Type: Application
    Filed: August 15, 2017
    Publication date: February 1, 2018
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Publication number: 20180030041
    Abstract: Disclosed is a storage-stable condensation product prepared from 1-amino-2-propanol and formaldehyde in a molar ratio in the range from 1:2.0 to 1:3.1. The condensation product contains less than 10% by weight of water. Also, disclosed is the preparation of the condensation product and the use thereof for reducing the amount of hydrogen sulphide in liquids and gases.
    Type: Application
    Filed: July 24, 2017
    Publication date: February 1, 2018
    Inventors: Wolfgang BEILFUSS, Ralf GRADTKE, Jennifer KNOPF, Klaus WEBER
  • Publication number: 20180030042
    Abstract: Disclosed are small molecule non-peptidic compounds, as well as methods and compositions for the treatment of angiotensin-related diseases and disorders, including cardiovascular diseases, metabolic diseases, gastrointestinal diseases, renal diseases, inflammatory/autoimmune diseases, neurological diseases, bone marrow diseases and cancer. In particular, the invention provides compounds, methods and compositions for the treatment of metabolic diseases and disorders, such as diabetes mellitus, diabetes-related cardiovascular disorders, diabetes-related dermal ulcerations, diabetes related hypertension, and diabetes-related ophthalmic diseases.
    Type: Application
    Filed: July 12, 2017
    Publication date: February 1, 2018
    Inventors: Nicos A. Petasis, Kathleen E. Rodgers, Stan G. Louie, Gere S. DiZerega, Kevin J. Gaffney
  • Publication number: 20180030043
    Abstract: The present invention relates to novel processes for the preparation 1,3-Thiazol-5-ylmethyl[(2R,5R)-5-{[(2S)-2-[(methyl{[2-(propan-2-yl)-1,3-thiazol-4-yl]methyl} carbamoyl)amino]-4-(morpholin-4-yl)butanoyl]amino}-1,6-diphenylhexan-2-yl] carbamate having the following structural formula-1 and it's intermediates thereof.
    Type: Application
    Filed: February 17, 2016
    Publication date: February 1, 2018
    Inventors: Srinivasan THIRUMALAI RAJAN, Sajja ESWARAIAH, Gutta MADHUSUDHAN, Komati SATYANA RAYAMA, Jakku MALLESWARA REDDY
  • Publication number: 20180030044
    Abstract: The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 11, 2016
    Publication date: February 1, 2018
    Applicant: Eli Lilly and Compny
    Inventor: Adam Jan Sanderson
  • Publication number: 20180030045
    Abstract: Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
    Type: Application
    Filed: August 7, 2017
    Publication date: February 1, 2018
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: J. Eric CARLSON, Hans HANSEN, Lynn HAWKINS, Sally ISHIZAKA, Matthew MACKEY, Shawn SCHILLER, Chikako OGAWA, Heather DAVIS, Atsushi ENDO
  • Publication number: 20180030046
    Abstract: The present invention provides compounds useful for treating or preventing an IL-1R-mediated disease or disorder. In certain embodiments, the disease or disorder comprises scleroderma.
    Type: Application
    Filed: October 6, 2017
    Publication date: February 1, 2018
    Inventors: Sandhya KORTAGERE, Carol M. ARTLETT
  • Publication number: 20180030047
    Abstract: Disclosed are compounds of the following formula I: wherein: m represents an integer being equal to 0, 1, 2, 3, 4, 5 or 6, X represents a simple bond or a radical —CHR1— wherein R1 represents: a hydrogen atom, or a linear or branched, possibly interrupted by up to 3 heteroatoms selected from O, S or N and/or possibly substituted, (C1-C12)-alkyl, R2, R3 and R4 represent independently from each other: a hydrogen atom, or a linear or branched (C1-C12)-alkyl or (C1-C12)-acyl R5 represents: a hydrogen atom, or a linear or branched, possibly substituted, (C1-C13)-alkyl possibly interrupted by up to 3 heteroatoms selected from O, S or N, R6 represents: a hydrogen atom, or a linear or branched possibly substituted (C1-C12)-alkyl, possibly substituted and possibly interrupted by up to 3 heteroatoms selected from O, S or N, for their use as antibacterial drugs.
    Type: Application
    Filed: August 26, 2015
    Publication date: February 1, 2018
    Inventors: Olivier MARTIN, Estelle GALLIENNE-BOIVINEAU, Cyril NICOLAS, Piotr B. HECZKO, Grazyna STOCHEL, Magdalena STRUS, Agnieszka KYZIOL, Diana MIKOLAJCZYK, Agnieszka MACHUL
  • Publication number: 20180030048
    Abstract: A composition and method for treating autoimmune disease includes administering an effective amount of an aryl hydrocarbon receptor (AhR) ligand. The AhR ligand includes 11-Cl-BBQ, 10-Cl-BBQ, an analog of 11-Cl-BBQ, or combination thereof. The AhR ligand is administered topically, orally, transdermally, intravenously, subcutaneously, or with a nanoparticle. The AhR ligand induces regulatory T cells (AhR-Tregs). AhR-Treg cells block the differentiation of cytotoxic T-lymphocytes (CTL). The AhR ligand activates AhR in CD4+ T cells to induce CD4+ AhR-Tregs that suppress the development of effector CTL, thereby suppressing the development of CTL that attack host cells in graft versus host disease (GVHD) or ?-cells in the pancreas in diabetes mellitus type 1 (T1DM). The AhR ligand can also suppress development of CTL independently of Foxp3+ regulatory T cell induction. The AhR ligand can therefore be used to treat autoimmune diseases characterized by an absence of functional Foxp3+ regulatory T cell.
    Type: Application
    Filed: October 28, 2015
    Publication date: February 1, 2018
    Applicant: Oregon State University
    Inventors: Nancy I. Kerkvliet, Siva Kumar Kolluri
  • Publication number: 20180030049
    Abstract: Disclosed is a preparation method for praziquantel and intermediates thereof. The method includes: obtaining a target product praziquantel by using ?-phenethylamine as an initial raw material through a condensation reaction with chloroacetyl chloride, a substitution reaction with ethanolamine, and an acylation reaction with cyclohexanecarbonyl chloride, followed by an oxidation reaction and cyclization reaction. Also disclosed are two key intermediates, namely, a compound of formula IV and a compound of formula V for preparing praziquantel. The preparation method is reasonable and simple in its technological design, uses moderate reaction conditions, and is economical and environmentally friendly. Additionally, the raw materials are inexpensive and easy to obtain, the key intermediates are easy to prepare, and the total reaction yield and purity of the obtained target compound praziquantel is high, so that industrialized mass production is easy to achieve.
    Type: Application
    Filed: February 12, 2015
    Publication date: February 1, 2018
    Applicants: Zhejiang Hisun Pharmaceutical Co., Ltd., Shanghai Institute of Pharmaceutical Industry
    Inventors: Fuli ZHANG, Zhezhou YANG, Rusheng BAO, Weiwei XU, Hua BAI
  • Publication number: 20180030050
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: May 5, 2017
    Publication date: February 1, 2018
    Inventors: Rajinder Singh, Matthew Duncton, Jing Zhang, Salvador Alvarez, Kin Tso, Sacha Holland, Rose Yen, Rao Kolluri, Thilo Heckrodt, Yan Chen, Esteban Masuda, Hui Li, Donald G. Payan, Ryan Kelley
  • Publication number: 20180030051
    Abstract: Solid forms of the compound, [5-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-pyridin-2-yl]-(6-trifluoromethyl-pyridin-3-ylmethyl)-amine HCl salt (Compound I) and its free base, active on the receptor protein kinases c-Kit and/or c-Fms and/or Flt3, were prepared and characterized: Also provided are methods of using the solid forms.
    Type: Application
    Filed: October 4, 2017
    Publication date: February 1, 2018
    Inventors: Prabha N. Ibrahim, Gary Conard Visor
  • Publication number: 20180030052
    Abstract: Use of a tetramic acid compound according to formula (I) or (I?) with a second nematicide as a treatment for crop plants to combat and control nematodes in the soil of said crop plants.
    Type: Application
    Filed: October 11, 2017
    Publication date: February 1, 2018
    Applicant: Syngenta Participations AG
    Inventors: Fabienne HATT, Anke BUCHHOLZ
  • Publication number: 20180030053
    Abstract: The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by hepatitis B virus, and reducing the occurrence of serious conditions associated with HBV.
    Type: Application
    Filed: October 12, 2017
    Publication date: February 1, 2018
    Inventors: Jiping FU, Xianming JIN, Patrick LEE, Peichao LU, Joseph Michael YOUNG
  • Publication number: 20180030054
    Abstract: Provided in the present invention is a novel inhibitor of FLT3 kinase, comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, ester, acid, metabolite or prodrug thereof. Also provided in the present invention are a pharmaceutical composition comprising a compound of formula (I) and a use and method for preventing or treating cell proliferative conditions and/or FLT3-related conditions, in particular for conditions responding to the inhibition of FLT3 kinase (especially FLT3/ITD mutant kinases).
    Type: Application
    Filed: August 7, 2015
    Publication date: February 1, 2018
    Applicants: HEFEI INSTITUTES OF PHYSICAL SCIENCE, CHINESE ACADEMY OF SCIENCES, HEFEI COSOURCE PHARMACEUTICAL CO., LTD.
    Inventors: Jing LIU, Qingsong LIU, Xixiang LI, Aoli WANG, Hong WU, Cheng CHEN, Wenchao WANG, Chen HU, Zheng ZHAO, Jiaxin WU, Juan LIU, Kailin YU, Wei WANG, Li WANG, Beilei WANG
  • Publication number: 20180030055
    Abstract: Disclosed are chemical entities of Formula (I): wherein X, Y, Z, R1, R3, R4 and R5 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
    Type: Application
    Filed: February 3, 2016
    Publication date: February 1, 2018
    Inventor: Gideon Shapiro
  • Publication number: 20180030056
    Abstract: Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth.
    Type: Application
    Filed: February 17, 2016
    Publication date: February 1, 2018
    Inventors: Tao Wang, Zhiwei Yin, John F. Kadow
  • Publication number: 20180030057
    Abstract: The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which arc CGRP-receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).
    Type: Application
    Filed: September 21, 2017
    Publication date: February 1, 2018
    Applicant: Bristol-Myers Squibb Company
    Inventor: Andrew P. Degnan
  • Publication number: 20180030058
    Abstract: The present invention provides a new crystal form of 5-((2-(6-amino)-9H-purin-9-yl)ethyl)amino)pentan-1-ol, which has a relatively better effect in selectively inhibiting adenylate cyclase 1 and is capable of preparing a medicament for treating neuropathic pain and/or inflammatory pain.
    Type: Application
    Filed: July 17, 2017
    Publication date: February 1, 2018
    Inventor: Min ZHUO
  • Publication number: 20180030059
    Abstract: Described are coelenterazine analogues, methods for making the analogues, kits comprising the analogues, and methods of using the compounds for the detection of luminescence in luciferase-based assays.
    Type: Application
    Filed: July 27, 2017
    Publication date: February 1, 2018
    Inventors: Mary Hall, Thomas Kirkland, Thomas Machleidt, Anton Shakhmin, Joel R. Walker
  • Publication number: 20180030060
    Abstract: The present invention provides a compound having the structure: wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 2, 2017
    Publication date: February 1, 2018
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Konstantin Petrukhin, Christopher Cioffi, Graham Johnson, Rando Allikmets, Emily Freeman, Ping Chen, Michael Conlon, Lei Zhu
  • Publication number: 20180030061
    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: October 11, 2017
    Publication date: February 1, 2018
    Inventors: Carole Pissot Soldermann, Jean Quancard, Achim Schlapbach, Oliver Simic, Marina Tintelnot-Blomley, Thomas Zoller
  • Publication number: 20180030062
    Abstract: The invention provides a method of treating drug and alcohol abuse, depression, anxiety, or a compulsive disorder in a subject comprising administering to the subject a compound having the formula: or a pharmaceutically acceptable salt or solvate thereof, wherein R, R1, R2, R3, R4, R5, and X are as defined in the specification.
    Type: Application
    Filed: October 3, 2017
    Publication date: February 1, 2018
    Applicant: The University of Bath
    Inventors: John Lewis, Stephen Husbands
  • Publication number: 20180030063
    Abstract: The present invention provides compounds of formula (I), wherein: R1 is unsubstituted C1-C6 alkyl; La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10 aryl; or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.
    Type: Application
    Filed: August 22, 2017
    Publication date: February 1, 2018
    Inventors: Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
  • Publication number: 20180030064
    Abstract: Disclosed are compounds of formula (I): and pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disease and disorders in a subject in need are also disclosed.
    Type: Application
    Filed: July 28, 2017
    Publication date: February 1, 2018
    Inventors: Linghong XIE, Michele L.R. HEFFERNAN, Philip Glyn JONES, Taleen G. HANANIA
  • Publication number: 20180030065
    Abstract: This technology relates to fluorescein conjugates including fluorescein conjugates of polymers.
    Type: Application
    Filed: January 27, 2016
    Publication date: February 1, 2018
    Applicant: ISI Life Sciences, Inc.
    Inventors: Gerald F. Swiss, Richard Willency, Craig Keshishian, Richard Pariza, Robert M. Moriarty
  • Publication number: 20180030066
    Abstract: The present invention relates to crystal form A of a compound. The present invention also discloses a preparation method and a pharmaceutical composition of the crystal form A. The crystal form A has strong hypoglycemic activity in vivo and is expected to be a novel pharmaceutically active ingredient for treating or preventing type II diabetes and/or complications of type II diabetes.
    Type: Application
    Filed: February 3, 2016
    Publication date: February 1, 2018
    Inventors: Hong LIU, Jian WANG, Jian LI, Jia LI, Jingya LI, Shengbin ZHOU, Mingbo SU, Hualiang JIANG, Xiaomin LUO, Kaixian CHEN
  • Publication number: 20180030067
    Abstract: An object of the present invention is to provide a crystal of trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol having excellent stability and favorable characteristics in terms of its production and formulation into drugs. The present invention provides a crystal of trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol having characteristic peaks of diffraction angle (2?±0.1°) at 7.7°, 9.5°, 10.3°, 12.3°, 14.5°, 15.6°, 16.3°, 17.8°, 18.3°, 19.3°, 20.9°, 22.8°, 24.2°, 25.7°, 26.8°, 27.7°, 29.0° and 30.1° in a powder X-ray diffraction spectrum.
    Type: Application
    Filed: February 26, 2016
    Publication date: February 1, 2018
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Masaya HASHIMOTO
  • Publication number: 20180030068
    Abstract: Provided are an organic electroluminescent device (organic EL device) that is improved in luminous efficiency, sufficiently secures driving stability, and has a simple construction, and a material for an organic EL device to be used in the device. The material for an organic EL device includes a carborane compound represented by the general formula (1), and the carborane compound has a structure in which a six-membered ring group containing at least two nitrogen atoms is bonded to a carborane ring. The material for an organic EL device is suitable as a host material for a light-emitting layer containing a phosphorescent light-emitting dopant and the host material, or as a material for a hole-blocking layer. In the formula, rings A's each represent a divalent carborane group represented by the formula (1a) or the formula (1b), and two or more of X's each represent N.
    Type: Application
    Filed: March 8, 2016
    Publication date: February 1, 2018
    Applicant: NIPPON STEEL & SUMIKIN CHEMICAL CO., LTD.
    Inventors: Tokiko UEDA, Junya OGAWA, Takahiro KAI, Masashi TADA
  • Publication number: 20180030069
    Abstract: The present invention discloses new molecules having defined structures of a series of thienothiophene (TT) and boron derivatives, light emitting devices of which are expected to be applied to organic light emitting diodes (OLED)
    Type: Application
    Filed: February 20, 2015
    Publication date: February 1, 2018
    Inventors: Turan OZTURK, Emine TEKIN, Selin PIRAVIDILI MUCUR, Ahmet Ceylan GOREN, Gulsen TURKOGLU, Mehmet Emin CINAR, Ali BUYRUK
  • Publication number: 20180030070
    Abstract: Novel polymerizable multivinylaminosilanes which are useful as branching agents for synthetic and natural rubber are described. The compounds can be used in the polymerization of conjugated diene monomers, optionally together with aromatic vinyl monomers, thus producing polymers, which can favorably be used in rubber articles such as tires.
    Type: Application
    Filed: January 20, 2016
    Publication date: February 1, 2018
    Applicant: Trinseo Europe GMBH
    Inventors: Michael Rossle, Christian Doring, Sven Thiele, Dominique Thielemann
  • Publication number: 20180030071
    Abstract: Hydridosilapyrroles and hydridosilaazapyrrole are a new class of heterocyclic compounds having a silicon bound to carbon and nitrogen atoms within the ring system and one or two hydrogen atoms on the silicon atom. The compounds have formula (I): in which R is a substituted or unsubstituted organic group and R? is an alkyl group. These compounds react with a variety of organic and inorganic hydroxyl groups by a ring-opening reaction and may be used to produce silicon nitride or silicon carbonitride films.
    Type: Application
    Filed: October 10, 2017
    Publication date: February 1, 2018
    Inventors: Barry C. ARKLES, Youlin PAN, Fernando JOVE
  • Publication number: 20180030072
    Abstract: Hydridosilapyrroles and hydridosilaazapyrrole are a new class of heterocyclic compounds having a silicon bound to carbon and nitrogen atoms within the ring system and one or two hydrogen atoms on the silicon atom. The compounds have formula (I): in which R is a substituted or unsubstituted organic group and R? is an alkyl group. These compounds react with a variety of organic and inorganic hydroxyl groups by a ring-opening reaction and may be used to produce silicon nitride or silicon carbonitride films.
    Type: Application
    Filed: October 10, 2017
    Publication date: February 1, 2018
    Inventors: Barry C. ARKLES, Youlin PAN, Fernando JOVE