Patents Issued in January 12, 2017
  • Publication number: 20170008859
    Abstract: The invention provides compounds and compositions that are useful for treating conditions including Alzheimer's disease, Parkinson's disease, diabetes, cancer, and psychotic disorders such as schizophrenia.
    Type: Application
    Filed: February 26, 2015
    Publication date: January 12, 2017
    Applicant: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY
    Inventors: Carl WAGNER, Pamela MARSHALL, Peter JURUTKA
  • Publication number: 20170008860
    Abstract: A process for preparing clomazone is provided, the process comprising reacting 4,4-dimethyl-3-isoxazolidinone with 2-chlorobenzyl chloride in an aqueous medium in the presence of a base, in particular an alkali metal hydroxide. A method for preparing clomazone is also disclosed, the method comprising (a) crystallizing clomazone from solution in an organic solvent; and (b) isolating the resulting crystals. N-benzene is a particularly suitable solvent. Further, there is provided Form I crystalline 2-[(2-chlorophenyl)methyl]-4,4-dimethyl-3-isoxazolidinone (clomazone), wherein the polymorph Form I is characterized by at least one of the following properties: (i) an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2?(+/?0.20° ?) at one or more of the following positions: about 10.63, 16.07, 18.08, 19.11, 19.34, 21.20, 24.78 and 28.80; and (ii) an infrared (IR) spectrum having a characteristic peak: at about 2967 and 2870 cm?1.
    Type: Application
    Filed: June 13, 2014
    Publication date: January 12, 2017
    Applicant: ROTAM AGROCHEM INTERNATIONAL COMPANY LIMITED
    Inventor: James Timothy BRISTOW
  • Publication number: 20170008861
    Abstract: An improved process for the preparation of Efavirenz which avoids the distillations of the solvents is provided.
    Type: Application
    Filed: May 7, 2015
    Publication date: January 12, 2017
    Inventors: Francesco FONTANA, Pierluigi PADOVAN, Marco PREBIANCA
  • Publication number: 20170008862
    Abstract: This method for a manufacturing a 1,1-disubstituted hydrazine compound represented by a formula (II) involves reacting a hydrazino compound represented by a formula (I) with a compound represented by a formula: R-Hal in an aprotic polar solvent in the presence of a base selected from an alkali metal hydroxide and alkaline-earth metal hydroxide in an amount of 1.0 to 3.0 equivalents based on the hydrazino compound. In the formulae, X represents an oxygen atom, a sulfur atom, —CH2— or the like, and each of RX represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, a cyano group, a nitro group, a fluoroalkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms or the like. An arbitrary C—RX that forms the ring is optionally substituted with a nitrogen atom. Hal represents a chlorine atom, a bromine atom, or an iodine atom, and R represents a substituted or unsubstituted organic group having 1 to 12 carbon atoms.
    Type: Application
    Filed: February 24, 2015
    Publication date: January 12, 2017
    Applicant: ZEON CORPORATION
    Inventors: Kanako SANUKI, Kumi OKUYAMA
  • Publication number: 20170008863
    Abstract: Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
    Type: Application
    Filed: September 20, 2016
    Publication date: January 12, 2017
    Inventor: Hyun-Soon Chong
  • Publication number: 20170008864
    Abstract: Catalytic conversion of ketoacids is disclosed, including methods for increasing the molecular weight of ketoacids. An exemplary method includes providing in a reactor a feedstock having at least one ketoacid. The feedstock is then subjected to one or more C—C-coupling reaction(s) in the presence of a catalyst system having a first metal oxide and a second metal oxide.
    Type: Application
    Filed: September 26, 2016
    Publication date: January 12, 2017
    Applicant: NESTE OYJ
    Inventors: Marina LINDBLAD, Elias IKONEN, Maaria SELÄNTAUS, Mats KÄLDSTRÖM
  • Publication number: 20170008865
    Abstract: Psicose is converted into 5-hydroxymethylfurfural or an alkyl ether thereof in a process for the catalysed conversion of psicose, including the steps of: a. forming a feed including psicose and water or at least one alkanol or a mixture thereof and b. converting the psicose in the feed at a temperature in the range of 50 to 300 degrees Celsius in the presence of a catalyst.
    Type: Application
    Filed: March 5, 2015
    Publication date: January 12, 2017
    Inventors: Robert-Jan van Putten, Jan Cornelis van der Waal, Edserd de Jong
  • Publication number: 20170008866
    Abstract: The present invention relates to a catalyst system for oxidation of o-xylene and/or naphthalene to phthalic anhydride (PA), comprising a plurality of catalyst zones arranged in succession in the reaction tube, which have been produced using antimony trioxide comprising a noticeable proportion of senarmontite wherein some of the primary crystallites have a size of less than 200 nm. The present invention further relates to a process for gas phase oxidation, in which a gas stream comprising at least one hydrocarbon and molecular oxygen is passed through a catalyst system which comprises a plurality of catalyst zones arranged in succession in the reaction tube and which has been produced using an antimony trioxide comprising a noticeable proportion of senarmontite wherein some of the primary crystallites have a size of less than 200 nm.
    Type: Application
    Filed: February 17, 2015
    Publication date: January 12, 2017
    Inventors: Nico F. FISCHER, Diana C. GALEANO NUNEZ, Michael KRÄMER, Markus SCHUBERT, Jürgen ZÜHLKE, Hans-Martin ALLMANN
  • Publication number: 20170008867
    Abstract: The present invention relates to a catalyst system for oxidation of o-xylene and/or naphthalene to phthalic anhydride (PA), comprising a plurality of catalyst zones arranged in succession in the reaction tube, which has been produced using antimony trioxide consisting predominantly of the senarmontite modification of which all primary crystallites have a size of less than 200 nm. The present invention further relates to a process for gas phase oxidation, in which a gas stream comprising at least one hydrocarbon and molecular oxygen is passed through a catalyst system which comprises a plurality of catalyst zones arranged in succession in the reaction tube and which has been produced using an antimony trioxide consisting predominantly of the senarmontite modification with a median primary crystallite size of less than 200 nm.
    Type: Application
    Filed: February 17, 2015
    Publication date: January 12, 2017
    Inventors: Diana C. GALEANO NUNEZ, Christian WALSDORFF, Jürgen ZÜHLKE, Hans-Martin ALLMANN
  • Publication number: 20170008868
    Abstract: The present disclosure relates to the preparation of a cannabidiol compound or a derivative thereof. The cannabidiol compound or derivatives thereof can be prepared by an acid-catalyzed reaction of a suitably selected and substituted di-halo-olivetol or derivative thereof with a suitably selected and substituted cyclic alkene to produce a dihalo-cannabidiol compound or derivative thereof. The dihalo-cannabidiol compound or derivative thereof can be produced in high yield, high stereospecificity, or both. It can then be converted under reducing conditions to a cannabidiol compound or derivatives thereof.
    Type: Application
    Filed: June 30, 2016
    Publication date: January 12, 2017
    Inventors: Lukas Dialer, Denis Petrovic, Ulrich Weigl
  • Publication number: 20170008869
    Abstract: The present disclosure relates to the preparation of a cannabidiol compound or a derivative thereof. The cannabidiol compound or derivatives thereof can be prepared by an acid-catalyzed reaction of a suitably selected and substituted di-halo-olivetol or derivative thereof with a suitably selected and substituted cyclic alkene to produce a dihalo-cannabidiol compound or derivative thereof. The dihalo-cannabidiol compound or derivative thereof can be produced in high yield, high stereospecificity, or both. It can then be converted under reducing conditions to a cannabidiol compound or derivatives thereof.
    Type: Application
    Filed: June 30, 2016
    Publication date: January 12, 2017
    Inventors: Lukas Dialer, Denis Petrovic, Ulrich Weigl
  • Publication number: 20170008870
    Abstract: The present invention includes a method for obtaining a higher purity cannabinoid solvent extract from a plant which comprises cannabinoids and/or terpenes. A solvent extraction is performed on the optionally dried plant material, followed by a step of removing high molecular weight impurities by a cooling step. Following the cooling step, the precipitate is removed and a higher quality filtrate is obtained which contains higher levels of purity of cannabinoids and/or terpenes than the starting solvent extract. The methods of the invention also include a method for obtaining crystallized THCa, which comprises obtaining a filtrate by the methods disclosed herein, or obtaining a solvent extract, and allowing crystallization of the THCa to occur. The filtrate, crystallized THCa, and residual filtrate remaining after crystallization of THCa can be used as starting materials for products that include cannabinoids and/or terpenes.
    Type: Application
    Filed: July 5, 2016
    Publication date: January 12, 2017
    Inventors: Clare J. Dibble, Isaac B. Cole
  • Publication number: 20170008871
    Abstract: 2-hydroxyethyl 2-oxo-1,3-dioxolane-4-carboxylates of formula (I): wherein one of R1 and R2 can be hydrogen. R1 and R2, if not hydrogen, and in each case independently of one another, are selected from straight-chain, branched or cyclic C1-22-alkyl groups, preferably C1-12-alkyl groups, C6-12-aryl groups, C6-18-aralkyl groups and C6-18-alkaryl groups, wherein R1 and/or R2, in each case independently of one another, may comprise at least one additional functional group, selected from hydroxyl groups, ether groups, ester groups, epoxy groups, and double bonds, and wherein R2 may be substituted with up to 10, preferably with 1 to 5, and in particular with 1 or 2 further 2-hydroxyethyl 2-oxo-1,3-dioxolane-4-carboxylic groups. The 2-hydroxyethyl 2-oxo-1,3-dioxolane-4-carboxylates can be prepared by reacting 2-oxo-1,3-dioxolane-4-carboxylic acid with epoxides and can be used for the preparation of hydroxyurethanes through reaction with amines, such as amine hardeners.
    Type: Application
    Filed: February 20, 2015
    Publication date: January 12, 2017
    Inventors: Sophie PUTZIEN, Burkhard WALTHER, Maximilian KOHLER
  • Publication number: 20170008872
    Abstract: A liquid crystal composition including at least one of the liquid crystal molecules represented by Chemical Formulas 1 to 3:
    Type: Application
    Filed: February 19, 2016
    Publication date: January 12, 2017
    Inventors: Ji Hong BAE, Keun Chan OH
  • Publication number: 20170008873
    Abstract: The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.
    Type: Application
    Filed: June 30, 2016
    Publication date: January 12, 2017
    Inventors: Elizabeth M. Bacon, Gayatri Balan, Chien-Hung Chou, Christopher T. Clark, Jeromy J. Cottell, Musong Kim, Thorsten A. Kirschberg, John O. Link, Gary Phillips, Scott D. Schroeder, Neil H. Squires, Kirk L. Stevens, James G. Taylor, William J. Watkins, Nathan E. Wright, Sheila M. Zipfel
  • Publication number: 20170008874
    Abstract: An object of the present invention is to provide a production method of an intermediate used in the production method of a sulfonylpyrrole compound useful as a pharmaceutical product. The present invention relates to a method of producing sulfonylpyrrole compound (VI) by reacting a pyridine-3-sulfonic acid compound with phosphorus pentachloride in a solvent of chlorobenzene or trifluoromethylbenzene to give a pyridine-3-sulfonyl chloride compound, reacting the compound without isolation with compound (III) to give compound (IV), and subjecting the compound (IV) to a reductive amination reaction. wherein R2 is a hydrocarbon group etc. and R3 and R4 are each a hydrogen atom etc., wherein R1 is an optionally substituted pyridin-3-yl group, and the other symbols are as defined above, wherein R5 is an alkyl group and the other symbols are as defined above.
    Type: Application
    Filed: September 15, 2016
    Publication date: January 12, 2017
    Inventor: Keisuke MAJIMA
  • Publication number: 20170008875
    Abstract: The present invention relates to novel substituted oxindole derivatives of formula (I) wherein the variables are as defined in the claims and description; to pharmaceutical compositions comprising them, and to their use for treatment of vasopressin-related disorders.
    Type: Application
    Filed: December 19, 2014
    Publication date: January 12, 2017
    Inventors: Hervé GENESTE, Wilfried HORNBERGER, Charles W. HUTCHINS, Katja JANTOS, Andreas KLING, Loic LAPLANCHE, Marcel VAN GAALEN
  • Publication number: 20170008876
    Abstract: The present invention is directed to compounds that bind to glycoprotein IIb/IIIa and can be used for diagnostic imaging, in particular magnetic resonance imaging of thrombi. The disclosed compounds enable the binding to glycoprotein IIb/IIIa receptor combined with an adequate imaging sensitivity.
    Type: Application
    Filed: February 6, 2015
    Publication date: January 12, 2017
    Inventors: Markus Berger, Jessica Lohrke, Gregor Jost, Michael Reinhardt
  • Publication number: 20170008877
    Abstract: The invention provides novel compounds having the general formula I: wherein R1, X, Z1, L, n, the A ring, the B ring, and the C ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: July 1, 2016
    Publication date: January 12, 2017
    Applicant: Genentech, Inc.
    Inventors: Snahel PATEL, Gregory HAMILTON, Craig Stivala, Huifen Chen, Guiling Zhao
  • Publication number: 20170008878
    Abstract: Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.
    Type: Application
    Filed: September 21, 2016
    Publication date: January 12, 2017
    Inventors: Deepak BANDYOPADHYAY, Patrick M. EIDAM, Peter J. GOUGH, Philip Anthony HARRIS, Jae U. JEONG, Jianxing KANG, Bryan Wayne KING, Ami LAKDAWALA SHAH, Lara Kathryn LEISTER, Robert W. MARQUIS, JR., Attiq RAHMAN, Joshi M. RAMANJULU, Clark A. SEHON, Robert SINGHAUS, JR., Daohua ZHANG
  • Publication number: 20170008879
    Abstract: The present invention relates to novel Fused Tricyclic Compounds, compositions comprising at least one Fused Tricyclic Compound, and methods of using Fused Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: September 26, 2016
    Publication date: January 12, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kevin X. Chen, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Publication number: 20170008880
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: July 21, 2016
    Publication date: January 12, 2017
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Roland Gendron, Adam D. Hughes
  • Publication number: 20170008881
    Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ? proteins. A compound of the formula (I): wherein X is —C(R3a)(R3b)—, —C(R3a)(R3b)—C(R3c)(R3d)— or —C(R3a)?C(R3c)—, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R3a, R3b, R3c and R3d are each independently hydrogen, halogen or the like, R4 is hydrogen or halogen, Ring B is substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 21, 2016
    Publication date: January 12, 2017
    Inventors: Ken-ichi KUSAKABE, Syuhei YOSHIDA, Kenji Nakahara, Tsuyoshi HASEGAWA, Genta TADANO, Kouki FUCHINO
  • Publication number: 20170008882
    Abstract: The present disclosure provides pyridines and pyrimidines of Formula I and pharmaceutically acceptable salts and solvates thereof: wherein A, G, W1, W2, W3, and R5 are defined as set forth in the specification. The present disclosure also provides uses of the compounds of Formula I and pharmaceutically acceptable salts and solvates thereof. In certain embodiments, Compounds of the present disclosure are useful for treating pain. In another embodiment, Compounds of the present disclosure are useful for treating a disorder responsive to blockade of sodium channels, or alleviating symptoms of the disorder.
    Type: Application
    Filed: January 23, 2015
    Publication date: January 12, 2017
    Inventor: Stephen M. Lynch
  • Publication number: 20170008883
    Abstract: The present invention refers to novel substituted thiazole and oxazole compounds of formula (I) having P2X7 receptor (P2X7) antagonistic properties. The compounds are useful in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.
    Type: Application
    Filed: February 4, 2015
    Publication date: January 12, 2017
    Applicant: Axxam S.P.A.
    Inventors: Paolo Pevarello, Stefan Lohmer, Chiara LIberati, Pierfausto Seneci, Cristina Pesenti, Adolfo Prandi
  • Publication number: 20170008884
    Abstract: The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors.
    Type: Application
    Filed: June 24, 2016
    Publication date: January 12, 2017
    Inventors: Gregory R.J. Thatcher, Isaac Thomas Schiefer, Ottavio Arancio, Mauro Fa
  • Publication number: 20170008885
    Abstract: The present invention provides a heterocyclic compound having a TLR7, TLR9, TLR7/8, TLR7/9 or TLR7/8/9 inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases, inflammatory diseases and the like, in particular, systemic lupus erythematosus, Sjogren's syndrome, rheumatoid arthritis, psoriasis, inflammatory bowel disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.
    Type: Application
    Filed: December 12, 2014
    Publication date: January 12, 2017
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Summon KOUL, Suresh KURHADE, Sandeep BHOSALE, Keshav NAIK, Videsh SALUNKHE, Yogesh MUNOT, Debnath BHUNIYA
  • Publication number: 20170008886
    Abstract: The present invention discloses the novel process for preparation of Apixaban intermediate formula (D), intermediate formula (E) and preparation of Apixaban from theses intermediates.
    Type: Application
    Filed: January 6, 2015
    Publication date: January 12, 2017
    Applicant: Wanbury Ltd.
    Inventors: Nitin Sharadchandra Pradhan, SACHIN ULHAS SONAVANE, DAYAGHAN GHANGADHAR PATIL, UTTAM SAKHARAM PUJARI, RAVINDRA BHAUSAHEB PAGIRE
  • Publication number: 20170008887
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Application
    Filed: February 13, 2015
    Publication date: January 12, 2017
    Inventors: Kyle J. EASTMAN, John F. KADOW, B. Narasimhulu NAIDU, Kyle E. PARCELLA, Kevin PEESE
  • Publication number: 20170008888
    Abstract: Provided herein are compounds of formula I and compositions containing the compounds. The compounds and compositions are useful in the methods of inhibiting the action of ERK5, a BET family protein or both. In certain embodiments, the compounds and compositions are useful in the prevention, amelioration or treatment of a ERK5-mediated disease, a BET protein-mediated disease or both.
    Type: Application
    Filed: February 26, 2015
    Publication date: January 12, 2017
    Inventors: Yi Hu, Emme C. K. Lin, Bei Li, Shyama Sidique, Jonathan S. Rosenblum, Oana M. Cociorva, Kevin R. Shreder, Shigeki Seto
  • Publication number: 20170008889
    Abstract: The present invention provides a class of 2,4-substituted phenylene-1,5-diamine derivatives, having an inhibiting effect on EGFR tyrosine kinases, and pharmaceutically acceptable salt, stereoisomer, solvate or prodrug of said derivatives. See the description for the definition of each group in the formula. In addition, the present invention also discloses pharmaceutical compositions, pharmaceutically acceptable compositions and applications thereof.
    Type: Application
    Filed: February 13, 2015
    Publication date: January 12, 2017
    Applicants: SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO. LTD., YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Jiong LAN, Yunzhou JIN, Fusheng ZHOU, Jing XIE, Sida SHEN, Yi HU, Wei LIU, Qiang LV
  • Publication number: 20170008890
    Abstract: Substituted 4-azaindoles as NR2B receptor ligands. Such compounds may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by NR2B receptor activity.
    Type: Application
    Filed: July 8, 2016
    Publication date: January 12, 2017
    Inventors: Christa C. CHROVIAN, Michael A. LETAVIC, Jason C. RECH, Akinola SOYODE-JOHNSON, Jessica L. WALL
  • Publication number: 20170008891
    Abstract: Disclosed herein are compounds that inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases using the compounds.
    Type: Application
    Filed: September 27, 2016
    Publication date: January 12, 2017
    Inventors: Zhi-Fu Tao, Xilu Wang, Michael Wendt, Andrew Souers, Andrew Judd, Aaron Kunzer, Gerard Sullivan
  • Publication number: 20170008892
    Abstract: A process for preparation of a compound of Formula (I) is disclosed.
    Type: Application
    Filed: March 12, 2015
    Publication date: January 12, 2017
    Applicant: WOCKHARDT LIMITED
    Inventors: Vijay Prakash CHAVAN, Karuna Suresh WANKHEDE, Vikas Vithalrao DESHMUKH, Satish BHAVSAR, Kiran Ramchandra PATIL, Ravindra Dattatraya YEOLE, Prasad Keshav DESHPANDE, Mahesh Vithalbhai PATEL
  • Publication number: 20170008893
    Abstract: This application discloses a process to synthesize 8-({1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy)-methyl]-8-pheny-1,7-diazaspiro[4.5]decan-2-one comprising reacting a compound of the Formula 27a-sulfonate with zinc in the presence of acetic acid.
    Type: Application
    Filed: February 12, 2016
    Publication date: January 12, 2017
    Inventors: Ingrid Mergelsberg, Dominik Hermann Scherer, Monika Erika Huttenloch, Hon-Chung Tsui, Sunil Paliwal, Neng-Yang Shih
  • Publication number: 20170008894
    Abstract: The present invention encompasses compounds of the formula (I) wherein the variables are defined herein which are suitable for the modulation of ROR? and the treatment of diseases related to the modulation of ROR?. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
    Type: Application
    Filed: September 20, 2016
    Publication date: January 12, 2017
    Inventors: Johanna BAKONYI, Steven Richard BRUNETTE, Delphine COLLIN, Robert Owen HUGHES, Xiang LI, Shuang LIANG, Robert SIBLEY, Michael Robert TURNER, Lifen WU, Qiang ZHANG
  • Publication number: 20170008895
    Abstract: The present invention provides compounds of Formula (II) (e.g., compounds of Formula (I)), and pharmaceutically compositions thereof. Compounds of Formula (II) are believed to be binders of bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits using the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception.
    Type: Application
    Filed: February 2, 2015
    Publication date: January 12, 2017
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: James E. Bradner, Nathanael S. Gray, Jun Qi, Michael R. McKeown, Dennis Buckley
  • Publication number: 20170008896
    Abstract: The invention relates to new substituted heteroaryls of formula 1 wherein A is selected from the group consisting of N and CH D is selected from the group consisting of CH, N, NH, E is C, T is selected from the group consisting of C and N, G is selected from the group consisting of C and N, and wherein each of the broken (dotted) double bonds in ring 1 are selected from either a single bond or a double bond under the proviso that all single and double bonds of ring 1 are arranged in such a way that they all form together with ring 2 an aromatic ring system, and wherein R1, M and R3 are defined according to claim 1, and to the above compounds for the treatment of a disease selected from the group consisting of asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.
    Type: Application
    Filed: March 12, 2015
    Publication date: January 12, 2017
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Georg DAHMANN, Matthias HOFFMANN, Jasna KLICIC, David James LAMB, Clive McCARTHY, Spencer NAPIER, Karen PARRISH, John SCOTT, Jennifer L. Swantek FITZGERALD, Edward WALKER
  • Publication number: 20170008897
    Abstract: Provided herein are formulations, methods and substituted tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds.
    Type: Application
    Filed: June 14, 2016
    Publication date: January 12, 2017
    Inventors: Michael O'Neil Hanrahan Clarke, Edward Doerffler, Richard L. Mackman, Dustin Siegel
  • Publication number: 20170008898
    Abstract: The present invention is directed to novel cyclic amines which inhibit the P2X7 receptor.
    Type: Application
    Filed: July 8, 2016
    Publication date: January 12, 2017
    Applicant: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohamed Eldemenky, Bin Chen, Yu Jiang
  • Publication number: 20170008899
    Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
    Type: Application
    Filed: August 30, 2016
    Publication date: January 12, 2017
    Applicants: MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME B.V.
    Inventors: ADRIANUS PETRUS ANTONIUS DE MAN, JAN-GERARD STERRENBURG, HANS C. A. RAAIJMAKERS, ALLARD KAPTEIN, ARTHUR A. OUBRIE, JOHANNES BERNARDUS MARI REWINKEL, CHRISTIAAN GERARDUS JOHANNES MARIA JANS, JACOBUS C.H.M. WIJKMANS, TJEERD A. BARF, ALAN B. COOPER, RONALD M. KIM, SOBHANA BABU BOGA, HUGH Y. ZHU, XIAOLEI GAO, XIN YAO, RAJAN ANAND, HAO WU, SHILAN LIU, CHUNDAO YANG, ABDUL-BASIT ALHASSAN, JAMES WANG, YOUNONG YU, JIAN LIU, HENRY M. VACCARO
  • Publication number: 20170008900
    Abstract: Compounds of formula (I) wherein R1, R2, A, W, m, n, p and q are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.
    Type: Application
    Filed: September 21, 2016
    Publication date: January 12, 2017
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Patrick Di Giorgio, Jerome Hert, Daniel Hunziker, Holger Kuehne, Patrizio Mattei, Markus Rudolph
  • Publication number: 20170008901
    Abstract: The present invention provides spiro-oxazolones, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The present compounds are useful as therapeutics acting peripherally and centrally in the conditions of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.
    Type: Application
    Filed: June 6, 2016
    Publication date: January 12, 2017
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Valerie Runtz-Schmitt, Patrick Schnider, Cosimo Dolente, Bernhard Fasching
  • Publication number: 20170008902
    Abstract: A method for acid-catalyzed acylation of an isohexide is described. The method can enable direct alcohol acylation with carboxylic acids. In particular, the method involves reacting an isohexide and an excess of carboxylic acid, in the presence of a water-tolerant Lewis acid catalyst. Water-tolerant Lewis acid catalysts can furnish relatively high diester yields (e.g., ?55%-60%) at lower catalyst loads. This feature, among others, is highly desirable for cost savings, and can improve process economics.
    Type: Application
    Filed: December 11, 2014
    Publication date: January 12, 2017
    Inventors: Kenneth Stensrud, Erik Hagberg, Erin Rockafellow, Stephen Howard
  • Publication number: 20170008903
    Abstract: Piperidino-dihydrothienopyrimidine sulfoxides of formula I wherein: Ring A is a 6-membered aromatic ring optionally comprising one or two nitrogen atoms and R is Cl and is located in the para-, meta-, or ortho-position of Ring A, S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
    Type: Application
    Filed: August 9, 2013
    Publication date: January 12, 2017
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Pascale A.J. POUZET, Peter NICKOLAUS, Ulrike WERTHMANN, Rogelio P. FRUTOS, Bing-Shiou YANG, Soojin KIM, Jason Alan MULDER, Nitinchandra D. PATEL, Chris Hugh SENANAYAKE, Thomas Gabriel TAMPONE, Xudong WEI
  • Publication number: 20170008904
    Abstract: The description relates to MDM2 binding compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the MDM2 E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
    Type: Application
    Filed: July 11, 2016
    Publication date: January 12, 2017
    Inventors: Andrew P. Crew, Craig M. Crews, Hanqing Dong, Yimin Qian, Jing Wang
  • Publication number: 20170008905
    Abstract: The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.
    Type: Application
    Filed: June 30, 2016
    Publication date: January 12, 2017
    Inventors: Elizabeth M. Bacon, Gayatri Balan, Chien-Hung Chou, Christopher T. Clark, Jeromy J. Cottell, Musong Kim, Thorsten A. Kirschberg, John O. Link, Gary Phillips, Scott D. Schroeder, Neil H. Squires, Kirk L. Stevens, James G. Taylor, William J. Watkins, Nathan E. Wright, Sheila M. Zipfel
  • Publication number: 20170008906
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: September 22, 2016
    Publication date: January 12, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Steven W. Ludmerer, Kun Liu, Hao Wu, Richard Soll, Bin Zhong, Jian Zhu
  • Publication number: 20170008907
    Abstract: The present invention provides oxazine compounds, method of using and method of making oxazine compounds and its pharmaceutical use.
    Type: Application
    Filed: September 23, 2016
    Publication date: January 12, 2017
    Inventors: Edward R. Biehl, Haribabu Ankati, Sukanta Kamila
  • Publication number: 20170008908
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Application
    Filed: February 19, 2015
    Publication date: January 12, 2017
    Inventor: B. Narasimhulu NAIDU