Patents Issued in August 18, 2016
-
Publication number: 20160237040Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is a divalent linking moiety; and R1-R10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R3 or R8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.Type: ApplicationFiled: April 25, 2016Publication date: August 18, 2016Applicants: University of Pittsburgh - Of the Commonwealth System of Higher Education, The United States Government as represented by the Department of Veterans AffairsInventors: Beibei Chen, Rama K. Mallampalli
-
Publication number: 20160237041Abstract: Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.Type: ApplicationFiled: February 16, 2015Publication date: August 18, 2016Inventor: Mark Quang Nguyen
-
Publication number: 20160237042Abstract: Piperazinyl derivatives of formula (I) and their use as a drug, particularly for the treatment of cancer, are disclosed. Also disclosed are pharmaceutical compositions comprising the piperazinyl derivatives, and methods for synthesizing the piperazinyl derivatives.Type: ApplicationFiled: April 22, 2016Publication date: August 18, 2016Inventors: Denis CARNIATO, Jean-Francois BRIAND, Mathieu GUTMANN, Olivier BUSNEL, Cécile BOUGERET, Benoit DEPREZ, Karine JAILLARDON
-
Publication number: 20160237043Abstract: Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.Type: ApplicationFiled: February 12, 2016Publication date: August 18, 2016Inventors: Hugh Y. Rienhoff, JR., John M. McCall, Michael Clare, Cassandra Celatka, Amy E. Tapper
-
Publication number: 20160237044Abstract: The invention relates to substituted phenylalanine derivatives and to processes for preparation thereof, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and/or severe perioperative blood loss.Type: ApplicationFiled: September 24, 2014Publication date: August 18, 2016Applicant: Bayer Pharma AktiengesellschaftInventors: Ulrike RÖHN, Manuel ELLERMANN, Julia STRASSBURGER, Astrid WENDT, Susanne RÖHRIG, Robert Alan WEBSTER, Martina Victoria SCHMIDT, Adrian TERSTEEGEN, Kristin BEYER, Martina SCHÄFER, Anja BUCHMÜLLER, Christoph GERDES, Michael SPERZEL, Steffen SANDMANN, Stefan HEITMEIER, Alexander HILLISCH, Jens ACKERSTAFF, Carsten TERJUNG
-
Publication number: 20160237045Abstract: The invention relates to substituted phenylalanine derivatives and to processes for preparation thereof, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and/or severe perioperative blood loss.Type: ApplicationFiled: September 24, 2014Publication date: August 18, 2016Applicant: Bayer Pharma AktiengesellschaftInventors: Ulrike RÖHN, Manuel ELLERMANN, Julia STRASSBURGER, Astrid WENDT, Susanne RÖHRIG, Robert Alan WEBSTER, Martina Victoria SCHMIDT, Adrian TERSTEEGEN, Kristin BEYER, Martina SCHÄFER, Anja BUCHMÜLLER, Christoph GERDES, Michael SPERZEL, Steffen SANDMANN, Stefan HEITMEIER, Alexander HILLISCH, Jens ACKERSTAFF, Carsten TERJUNG
-
Publication number: 20160237046Abstract: The present invention provides biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds, isomers thereof, or pharmaceutically acceptable salts. The compounds of the invention show a CETP inhibitory effect that increases HDL-cholesterol levels and reduces LDL-cholesterol levels. Pharmaceutical compositions comprising the compounds are useful for the prevention or treatment of dyslipidemia or dyslipidemia-related diseases.Type: ApplicationFiled: January 29, 2014Publication date: August 18, 2016Inventors: Jae Kwang LEE, Jung Taek OH, Jae Won LEE, Seo Hee LEE, Il-Hyang KIM, Jae Young LEE, Su Yeal BAE, Se Ra LEE, Yun Tae KIM
-
Publication number: 20160237047Abstract: The disclosure includes a process for preparing fluoxostrobin which includes: (i) reacting benzofuran-3(2H)-one O-methyl oxime (10) with an alkyl nitrite in the presence of an acid to form (3E)-2,3-benzofuran-dione O3-methyl dioxime (11A) as a predominant isomer; (ii) reacting (3E)-2,3-benzofuran-dione O3-methyl dioxime (11A) with 2-haloethanol to form (3E)-benzofuran-2,3-dione O2-(2-hydroxyethyl) O3-methyl dioxime (12A); and (iii) reacting (3E)-benzofuran-2,3-dione O2-(2-hydroxyethyl) O3-methyl dioxime (12A) with a base to form (E)-(5,6-dihydro-1,4,2-dioxazin-3-yl)(2-hydroxyphenyl)methanone O-methyl oxime (13) (iv) reacting a 4,6-di-halo-5-fluoro-pyrimidine (5), wherein X1 is halogen, with (E)-(5,6-dihydro-1,4,2-dioxazin-3-yl)(2-hydroxyphenyl)methanone O-methyl oxime (13), in the presence of a solvent and optionally in the presence of a base, to form an (E)-(2-((6-halo-5-fluoropyrimidin-4-yl)oxy)phenyl)(5,6-dihydro-1,4,2-dioxazin-3-yl)methanone O-methyl oxime (14):Type: ApplicationFiled: October 23, 2015Publication date: August 18, 2016Inventors: Rama Mohan Hindupur, Avinash Sheshrao Mane, Sankar Balakrishnan, Jivan Dhanraj Pawar, Mahagundappa Rachappa Maddani, Sandeep Wadhwa, Vic Prasad
-
Publication number: 20160237048Abstract: Disclosed are compounds of general formula (I): and pharmaceutically acceptable salts thereof, formulations, methods and uses in, for example, the treatment of disease.Type: ApplicationFiled: February 29, 2016Publication date: August 18, 2016Applicant: WisTa Laboratories Ltd.Inventors: COLIN MARSHALL, Scott Clunas, John Mervyn David Storey, James Peter Sinclair, Thomas Craven Baddeley, Ahtsham Ishaq, Michael Simpson, Craig Williamson, Barry Alan Wood, Claude Michel Wischik, Charles Robert Harrington, Janet Elizabeth Rickard, David Horsley, Yin Sze Loh, Karrar Ahmad Khan, Christopher Paul Larch
-
Publication number: 20160237049Abstract: The present invention relates to crystal modifications of N-{(2R)-2-[({[3,3-dibutyl-7-(methyl-thio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl]oxy}acetyl)amino]-2-phenylethanolyl}glycine (elobixibat), more specifically crystal modifications I, IV, MeOH-1, EtOH-1, 1-PrOH-1 and 2-PrOH-1. The invention also relates to a process for the preparation of these crystal modifications and to a pharmaceutical composition comprising crystal modification IV.Type: ApplicationFiled: April 21, 2016Publication date: August 18, 2016Inventors: Martin Bohlin, Erica Tjerneld, Andreas Vestermark, Ingvar Ymen
-
Publication number: 20160237050Abstract: The present invention relates to a process for the synthesis of diacetyl epoxy glyceryl oleate, comprising the steps of: a). esterification of glycerol and oleic acid at 115-190° C. for 1.5-4.5 hours in the presence of an esterification catalyst to obtain glyceryl monooleate; b). acetylation of glyceryl monooleate and an acetylating reagent at 90-160° C. for 2-10 hours in the presence of an acetylation catalyst to obtain diacetyl glyceryl oleate; c). epoxidation of diacetyl glyceryl oleate and hydrogen peroxide at 60-80° C. for 2-4 hours in the presence of an epoxidation catalyst and a weak acid to obtain diacetyl epoxy glyceryl oleate. The prepared diacetyl epoxy glyceryl oleate can be used as plasticizer in plastics, with the advantages of improved stability, good flowability, and high compatibility with plastics.Type: ApplicationFiled: January 23, 2014Publication date: August 18, 2016Applicant: GUANGZHOU HAIRMA CHEMICAL (GZ) LTD.Inventors: DAOBIN LI, QIHONG CAI, CHAOJIE LIN
-
Publication number: 20160237051Abstract: The present disclosure generally relates to a silica-titanium catalyst prepared by first reacting a solid support with a metal alkoxide and then depositing titanium onto the solid support for the epoxidation of alkenes and aralkenes and a method of preparing the catalyst thereof. In some embodiments, the present disclosure relates to methods of using the catalyst described herein for the production of epoxides.Type: ApplicationFiled: February 16, 2016Publication date: August 18, 2016Applicant: Lyondell Chemical Technology, L.P.Inventors: Sandor Nagy, Vu A. Dang, Roger A. Grey
-
Publication number: 20160237052Abstract: The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I; and a method of treatment of a disorder or condition selected from the list consisting of acute myocardial infarction; memory processes disorders; dementia; cognition disorders such as Alzheimer's disease; attention deficit disorder (ADD); attention-deficit hyperactivity disorder (ADHD); cancers such as cutaneous carcinoma, medullary thyroid carcinoma and melanoma; Meniere's disease; gastrointestinal disorders; inflammation; migraine; motion sickness; obesity; pain; septic shock; respiratory disorders (including allergic rhinitis, nasal congestion and allergic congestion) in a mammal, including a human, that may be effected by administering to said mammal a pharmacologically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.Type: ApplicationFiled: February 18, 2015Publication date: August 18, 2016Applicant: MediSynergics, LLCInventors: Dennis Michael Godek, Harry Ralph Howard
-
Publication number: 20160237053Abstract: A compound derived from the culture product of an actinomycete and having an antitumor activity is provided. Provided is a compound represented by any one of formulas (I), (II) and (III) or an optical isomer thereof or a pharmaceutically acceptable salt thereof which can be isolated from the culture fluid of an actinomycete which belongs to the genus Streptomyces, wherein R1, R2, R5 and R6 each independently represent a hydrogen atom, a methyl group, a hydroxymethyl group, a hydroxyl group, or a double bond by which R1 and R2 or R5 and R6 are bonded; R3, R4, R7 and R8 each independently represent a methyl group or a hydroxymethyl group; and R9 represents a hydrogen atom or a hydroxyl group.Type: ApplicationFiled: March 10, 2016Publication date: August 18, 2016Inventors: Seizo SATO, Fumie IWATA, Shoichi YAMADA, Jiro TAKEO, Akihisa ABE, Hiroyuki KAWAHARA
-
Publication number: 20160237054Abstract: The present invention provides a process for the preparation of (1C)-2,3,4,6-tetra-O-acetyl-1,5-anhydro-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-D-glucitol of Formula III. The invention also provides a process for the purification of dapagliflozin using (1C)-2,3,4,6-tetra-O-acetyl-1,5-anhydro-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-D-glucitol of Formula III.Type: ApplicationFiled: September 19, 2014Publication date: August 18, 2016Applicant: SUN PHARMACEUTICAL INDUSTRIES LIMITEDInventors: Suresh Babu JAYACHANDRA, Devendra Prakash NAGDA, Tarun Kumar SINGH
-
Publication number: 20160237055Abstract: The present invention relates to compounds of formula (I), and salts thereof and the pharmaceutical composition containing them in treatment of various diseases, as allergic rhinitis where R1 and R2 are, independently, hydrogen, halogen, C1_3 alkyl or C1-3alkoxy; R3 is phenyl optionally substituted by R4 and R5 which are, independently hydrogen, halogen, C1-3 alkyl, C1-3-alkoxy, fluoro-, difluoro- and trifluoromethyl, nitrile group, N,N-diC1-3alkyl-amide, carboC1-3 alkoxy or C1-3alkylsulphone groups; R3 is pyridyl group containing nitrogen at various positions in the benzene ring, n is one of the integers 1 or 2.Type: ApplicationFiled: September 30, 2013Publication date: August 18, 2016Inventors: Piotr Kopczacki, Mieczyslaw Wosko, Jaroslaw Walczak, Krzysztof Walczynski
-
Publication number: 20160237056Abstract: Methods of synthesizing prostaglandins, prostaglandin analogs and their synthetic intermediates are described. The methods can comprise metal-catalyzed metathesis reactions. Also provided are synthetic intermediates that can be used in the synthesis of the prostaglandins and prostaglandin analogs.Type: ApplicationFiled: September 30, 2014Publication date: August 18, 2016Inventors: George Petros Yiannikouros, Panos Kalaritis, Chaminda Priyapushpa Gamage, Denis Viktorovich Arefyev
-
Publication number: 20160237057Abstract: The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof: It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses as anti-proliferative and pro-apoptotic agents for cancer therapy.Type: ApplicationFiled: October 9, 2014Publication date: August 18, 2016Inventors: Benedetto Grimaldi, Esther Torrente, Rita Scarpelli, Giovanni Bottegoni, Tiziano Bandiera, Marina Veronesi
-
Publication number: 20160237058Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. The glucuronidase inhibitors include phenoxy thiophene sulfonamides, and other compounds such as pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls. These compounds include nialamide, isocarboxazid, phenelzine, amoxapine, loxapine and mefloquine. Also compositions including one or more of such compounds for use in inhibiting glucuronidase and methods of using one or more of such compounds for selective inhibition of bacterial ?-glucoronidase. These compounds may be used as a co-drug in combination with the anticancer drug CPT-11. Also a method for screening compounds to determine their usefulness in reducing diarrhea associated with irinotecan chemotherapy.Type: ApplicationFiled: March 3, 2016Publication date: August 18, 2016Applicants: NORTH CAROLINA CENTRAL UNIVERSITY, THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILLInventors: ALFRED L. WILLIAMS, JOHN E. SCOTT, LI-AN YEH, MATTHEW R. REDINBO
-
Publication number: 20160237059Abstract: The present application relates to novel heterocyclically substituted 6-(trifluoromethyl)pyrimidin-4(3H)-one derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of cardiovascular, renal, inflammatory and fibrotic diseases.Type: ApplicationFiled: September 12, 2014Publication date: August 18, 2016Applicant: Bayer Pharma AktiengesellschaftInventors: Alexander STRAUB, Marie-Pierre COLLIN, Michael KOCH, Jutta MEYER, Karl-Heinz SCHLEMMER, Carl Friedrich NISING, Nicole BIBER, Sonja ANLAUF, Alexey GROMOV, Matthias Beat WITTWER
-
Publication number: 20160237060Abstract: The present invention relates to compounds of the formula I, wherein Ht, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: April 27, 2016Publication date: August 18, 2016Inventors: Sven RUF, Josef PERNERSTORFER, Thorsten SADOWSKI, Georg HORSTICK, Herman SCHREUDER, Christian BUNING, Klaus WIRTH
-
Publication number: 20160237061Abstract: The invention relates to compounds and methods of treatment relating to nicotinic receptor antagonists. For example, the compounds and methods of treatment function block the activity of certain acetylcholine receptors and subtypes therein, and are useful treating diseases and conditions mediated by nicotinic receptor stimulation, e.g., small cell lung cancer.Type: ApplicationFiled: January 11, 2016Publication date: August 18, 2016Applicant: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng LI, Youyi PENG, John TOMESCH, Lawrence P. WENNOGLE, Qiang ZHANG
-
Publication number: 20160237062Abstract: Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds.Type: ApplicationFiled: December 23, 2015Publication date: August 18, 2016Inventors: Yunfeng Eric Hu, Petr JANSA, Eric LANSDON, Richard L. MACKMAN
-
Publication number: 20160237063Abstract: A compound of the formula (I), wherein R1 and R2 independently of one another are hydrogen, C1-C22alkyl, —O., —OH, —CH2CN, C1-C18alkoxy, C2-C18alkoxy substituted by —OH; C5-C12cycloalkoxy, C3-C6alkenyl, C3-C6alkenyloxy, C7-C9phenylalkyl unsubstituted or substituted on the phenyl by 1, 2 or 3 C1-C4alkyl; or C1-C8acyl; and R3 and R4 independently of one another are C1-C22alkyl or a group of the formula (1a), wherein R0 has one of the meanings of R1 and R2.Type: ApplicationFiled: October 13, 2014Publication date: August 18, 2016Applicant: BASF SEInventors: Cornelia SCHLETH, Liane SCHULZ, Bruno ROTZINGER, Bjoern LUDOLPH, Manuele VITALI
-
Publication number: 20160237064Abstract: The present invention is directed to methods and compositions for suppressing lymphangiogenesis, angiogenesis and/or tumor growth. The methods comprise contacting the tumor with a compound that (i) stabilizes a protein kinase in the inactive state and (ii) is not an ATP competitive inhibitor of the protein kinase in the active state.Type: ApplicationFiled: February 12, 2016Publication date: August 18, 2016Inventors: Eric A. MURPHY, David A. CHERESH, Lee Daniel ARNOLD
-
Publication number: 20160237065Abstract: Compounds that are agonists of the MCIR receptor and that exhibit reduced toxicity relative to other compounds of the same class are described. These compounds can have the general formula (I) wherein: R1 represents a cyclopropylmethyl or a 4-hydroxybutyl group; R2 represents a hydrogen atom or a methyl group; and also the salts and enantiomers of the corresponding compounds of general formula (I). Also described, are methods for treating hypopigmentary pathologies and photosensitive dermatoses.Type: ApplicationFiled: April 26, 2016Publication date: August 18, 2016Inventor: Claire BOUIX-PETER
-
Publication number: 20160237066Abstract: The present invention relates to process for the preperation of (3S,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl-4-methylbenzene sulfonate compound of formula-1 through novel intermediates. Further the said compound of formula-1 is useful as a key intermediate for the preparation of Posaconazole.Type: ApplicationFiled: October 21, 2014Publication date: August 18, 2016Applicant: MSN LABORATORIES PRIVATE LIMITEDInventors: Srinivasan Thirumalai Rajan, Sajja Eswaraiah, Maramreddy Sahadeva Reddy
-
Publication number: 20160237067Abstract: The invention relates to substituted phenylalanine derivatives and to processes for preparation thereof, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and/or severe perioperative blood loss.Type: ApplicationFiled: September 24, 2014Publication date: August 18, 2016Applicant: Bayer Pharma AktiengesellschaftInventors: Ulrike RÖHN, Manuel ELLERMANN, Julia STRASSBURGER, Astrid WENDT, Susanne RÖHRIG, Robert Alan WEBSTER, Martina Victoria SCHMIDT, Adrian TERSTEEGEN, Kristin BEYER, Martina SCHÄFER, Anja BUCHMÜLLER, Christoph GERDES, Michael SPERZEL, Steffen SANDMANN, Stefan HEITMEIER, Alexander HILLISCH, Jens ACKERSTAFF, Carsten TERJUNG
-
Publication number: 20160237068Abstract: Provided herein are novel solid forms of N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4?-(morpholinomethyl)-[1,1?-biphenyl]-3-carboxamide hydrochloride, and related compositions and methods.Type: ApplicationFiled: October 15, 2014Publication date: August 18, 2016Inventors: Kevin W. KUNTZ, Hyeong-wook CHOI, Steven MATHIEU, Kristen SANDERS, Arani CHANDA
-
Publication number: 20160237069Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of Olig2. Also described herein are methods of using such Olig2 inhibitors, alone and in combination with other compounds, for treating cancer and other diseases. In particular the Olig2 inhibitors may be used to treat glioblastoma.Type: ApplicationFiled: February 10, 2016Publication date: August 18, 2016Inventors: Graham BEATON, Fabio TUCCI, Satheesh B. RAVULA, Hua-Yu WANG
-
Publication number: 20160237070Abstract: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones represented by the Formula (I): wherein Ar, R1-R6 are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.Type: ApplicationFiled: February 12, 2016Publication date: August 18, 2016Inventors: Sui Xiong CAI, Ye TIAN, Haijun DONG, Qingbing XU, Lizhen WU, Lijun LIU, Yangzhen JIANG, Qingli BAO, Guoxiang WANG, Feng YIN, Chengyun GU, Xiuhua HU, Xiaozhu WANG, Sishun KANG, Shengzhi CHEN
-
Publication number: 20160237071Abstract: A novel compound that has an excellent T-type calcium channel inhibitory activity and is specifically useful for prevention or treatment of pain, chronic kidney disease and atrial fibrillation. The novel triazinone compound of Formula (I): where each substituent in the formula is defined in detail in the description, and R1 could be a hydrogen atom, or a C1-6 alkyl group, etc., E could be a 7 to 14-membered non-aromatic fused heterocyclic group, L3 could be a C1-6 alkylene group, etc., D could be a C6-14 aryl group or a 5 to 10-membered heteroaryl group each of which is optionally substituted, etc., a tautomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof.Type: ApplicationFiled: October 2, 2014Publication date: August 18, 2016Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Masatoshi NIWA, Yusuke INABA, Toshimasa IWAMOTO, Yusuke SHINTANI, Hiroshi NAGAI, Jun EGI, Michiaki ADACHI, Yuichi HIRAI
-
Publication number: 20160237072Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.Type: ApplicationFiled: October 6, 2014Publication date: August 18, 2016Inventors: Andrew P. Degnan, Darrell Maxwell, Matthew D. Hill, Haiquan Fang, Michael F. Parker, Fukang Yang, Joanne J. Bronson, John E. Macor
-
Publication number: 20160237073Abstract: The present invention is directed to novel polymorphs and salts of a compound which is an inhibitor of kinase activity.Type: ApplicationFiled: April 26, 2016Publication date: August 18, 2016Inventors: Julie Nicole HAMBLIN, Paul Spencer JONES, Suzanne Elaine KEELING, Joelle LE, Charlotte Jane MITCHELL, Nigel James PARR, Robert David WILLACY
-
Publication number: 20160237074Abstract: Disclosed are compounds or pharmaceutically acceptable salts thereof, having the structure of formula I. Also disclosed are methods of preventing and/or treating degenerative disease in a subject, comprising administering to said subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions for preventing and/or treating degenerative disease in a subject comprising a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: January 15, 2016Publication date: August 18, 2016Inventors: Craig C. BEESON, Baerbel ROHRER, Nathan Perron
-
Publication number: 20160237075Abstract: Compounds of Formula I, as shown below and defined herein: and pharmaceutically acceptable salts, syntheses, intermediates, formulations, and methods of treating diseases including cancer, inflammation, and autoimmune disease mediated at least in part by Bruton's Tyrosine Kinase (BTK).Type: ApplicationFiled: September 29, 2014Publication date: August 18, 2016Inventors: Xiangyang CHEN, Yingxiang GAO, Chong LIU, Haihong NI, Mark MULVIHILL
-
Publication number: 20160237076Abstract: Provided herein are compounds that bind to dCK and methods for treating cancer.Type: ApplicationFiled: January 11, 2016Publication date: August 18, 2016Inventors: Caius G. Radu, Zheng Li, Raymond M. Gipson, Jue Wang, Nagichettiar Satyamurthy, Arnon Lavie, Jennifer M. Murphy, David A. Nathanson, Michael E. Jung
-
Publication number: 20160237077Abstract: Disclosed is a process for the industrial synthesis of Lurasidone from (1R,2R)-cyclohexane-1,2-diyldimethanol (1), 3-(piperazin-1-yl)benzo[d]isothiazole (3) and (3aR,4R,7R,7aS)-3a,4,7,7a-tetrahydro-4,7-methanoisobenzofuran-1,3-dione (6).). Said process is optimised to obtain Lurasidone with high yields and high purities by preparing highly pure synthesis intermediates, using critical raw materials and reagents in amounts close to the stoichiometric amounts, increasing productivity and reducing the costs and environmental impact of the process.Type: ApplicationFiled: October 16, 2014Publication date: August 18, 2016Applicant: PROCOS S.P.A.Inventors: Tommaso Angelini, Piergiorgio Bettoni, Jacopo Roletto, Paolo Paissoni
-
Publication number: 20160237078Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4 and A are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: September 10, 2013Publication date: August 18, 2016Applicant: HOFFMANN-LA ROCHE INC.Inventors: Lei Guo, Taishan Hu, Yimin Hu, Buelent Kocer, Xianfeng Lin, Haixia Liu, Alexander V Mayweg, Zongxing Qiu, Hong Shen, Guozhi Tang, Lisha Wang, Guolong Wu, Shixiang Yan, Weixing Zhang, Mingwei Zhou, Wei Zhu
-
Publication number: 20160237079Abstract: The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators.Type: ApplicationFiled: April 22, 2016Publication date: August 18, 2016Inventors: Sara Hadida-Ruah, Fredrick Van Goor, Mark Miller, Jason McCartney, Jinglan Zhou, Vijayalaksmi Arumugam
-
Publication number: 20160237080Abstract: A process of synthesizing 2-bromo-LSD or a salt or hydrate thereof comprising the steps of reacting methylergometrine with a brominating agent to produce [(15)-1-(Hydroxymethyl)propylamino][(6aR, 9R)-5 -bromo-7-methyl-4,7-diaza-4,6,6a,7,8,9-hexahydroacephenanthrylen-9-yl]formaldehyde as a first intermediate, and then hydrolyzing [(15)-1-(Hydroxymethyl)propylamino][(6aR,9R)-5-bromo-7-methyl-4,7-diaza-4,6,6a,7,8,9-hexahydroacephenanthrylen-9-yl]formaldehyde to yield bromo-lysergic acid as a second intermediate, wherein bromo-lysergic acid is then amidated to yield 2-bromo-LSD or a salt or hydrate thereof.Type: ApplicationFiled: January 7, 2016Publication date: August 18, 2016Inventor: Justin Kirkland
-
Publication number: 20160237081Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system.Type: ApplicationFiled: September 18, 2014Publication date: August 18, 2016Inventors: Lawrence R. Marcin, Mendi A. Higgins, Joanne J. Bronson, F. Christopher Zusi, John E. Macor, Min Ding
-
Publication number: 20160237082Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB) by contact with a compound of formula (I)Type: ApplicationFiled: October 10, 2014Publication date: August 18, 2016Inventors: Nicholas J. Donato, Moshe Talpaz, Luke Peterson, Matthew Young, Hollis D. Showalter, Christiane Wobus, Mary Xuan Dziem O'Riordan, Monika Ermann
-
Publication number: 20160237083Abstract: Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: ApplicationFiled: April 22, 2016Publication date: August 18, 2016Inventors: Ludwig Paul COOYMANS, Samuël Dominique DEMIN, Lili HU, Tim Hugo Maria JONCKERS, Pierre Jean-Marie Bernard RABOISSON, Abdellah TAHRI, Sandrine Marie Helene VENDEVILLE
-
Publication number: 20160237084Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, and R5 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: ApplicationFiled: April 25, 2016Publication date: August 18, 2016Inventors: Le Wang, John Pratt, Lisa A. Hasvold, Dachun Liu, Yujia Dai, Steven D. Fidanze, James H. Holms, Robert A. Mantei, Keith F. McDaniel, George S. Sheppard, William J. McClellan
-
Publication number: 20160237085Abstract: N-[4-(2,4-difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethanesulfonamide and crystalline forms thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.Type: ApplicationFiled: April 25, 2016Publication date: August 18, 2016Inventor: Yuchuan Gong
-
Publication number: 20160237086Abstract: Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.Type: ApplicationFiled: April 26, 2016Publication date: August 18, 2016Applicant: Genentech, Inc.Inventors: Mark Edward ZAK, Nicholas Charles RAY, Simon Charles GOODACRE, Rohan MENDONCA, Terry KELLAR, Yun-Xing CHENG, Wei LI, Po-Wei YUEN
-
Publication number: 20160237087Abstract: A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: wherein each symbol is as defined herein, or a salt thereof, a medicament comprising the compound or a salt thereof, and use of the compound or a salt thereof as an agent for the prophylaxis or treatment of diabetes mellitus are provided.Type: ApplicationFiled: April 27, 2016Publication date: August 18, 2016Applicant: Takeda Pharmaceutical Company LimitedInventors: Shizuo Kasai, Hideki Hirose, Takeshi Yamasaki, Tohru Yamashita, Asato Kina, Yoichi Nishikawa
-
Publication number: 20160237088Abstract: The invention relates to compounds of formula I wherein “” is a bond or is absent, V is CH, CR6 or N; R0 is H or, if “” is a bond, may also be alkoxy; R1 is H or halogen; U is CH or N when “” is a bond, or, if “” is absent, U is CH2, NH or NRg; R2 is H, alkylcarbonyl or —CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2 wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to saltType: ApplicationFiled: April 21, 2016Publication date: August 18, 2016Inventors: Christian HUBSCHWERLEN, Daniel RITZ, Georg RUEEDI, Jean-Philippe SURIVET, Cornelia ZUMBRUNN-ACKLIN
-
Publication number: 20160237089Abstract: Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.Type: ApplicationFiled: April 25, 2016Publication date: August 18, 2016Inventors: Bertrand L. Chenard, Randall J. Gallaschun