Patents Issued in September 29, 2016
  • Publication number: 20160280673
    Abstract: The present invention relates to a method for prevention of premature polymerization during the preparation, purification, transportation and storage of a polymerizable compound with at least one conjugated unsaturated group in the presence of an azine dye-based compound as inhibitor. Further the present invention relates to methods of preparing such inhibitors as well as to the inhibitors itself, as well as to methods of improving solubility and stability of dissolved inhibitors.
    Type: Application
    Filed: March 24, 2016
    Publication date: September 29, 2016
    Applicant: Nitto Europe N.V.
    Inventors: Greet BOSSAERT, Monica GOMES, Bart FORIER
  • Publication number: 20160280674
    Abstract: Direct epoxidation of propene is carried out on electrochemically tuned mixed oxide catalyst surfaces in a single chamber reactor with mixed reaction gas of hydrocarbon and oxygen. Yield and selectivity improvement compared to platinum- or silver-based noble metal catalysts have been demonstrated for the same reactor set up. Increase in propylene oxide yield has been demonstrated when a cell voltage is applied.
    Type: Application
    Filed: November 4, 2014
    Publication date: September 29, 2016
    Inventor: Monika Backhaus-Ricoult
  • Publication number: 20160280675
    Abstract: The actinic ray-sensitive or radiation-sensitive resin composition includes a crosslinking agent having a polarity converting group and an alkali-soluble resin, in which the polarity converting group is a group capable of decomposing by the action of an alkaline aqueous solution to generate a carboxylic acid or sulfonic acid on the side having a crosslinking group.
    Type: Application
    Filed: June 8, 2016
    Publication date: September 29, 2016
    Applicant: FUJIFILM Corporation
    Inventors: Shuhei YAMAGUCHI, Koutarou TAKAHASHI, Tomotaka TSUCHIMURA, Natsumi YOKOKAWA, Hidehiro MOCHIZUKI
  • Publication number: 20160280676
    Abstract: Sulfated and unsulfated flavonoid oligomers as inhibitors of cancer stem cells (CSCs) are provided. In particular, sulfated flavonoid dimers are shown to selectively inhibit CSCs growth and self-renewal both in vitro and in vivo.
    Type: Application
    Filed: November 7, 2014
    Publication date: September 29, 2016
    Inventors: Umesh R. Desai, Rajesh Karuturi, Bhaumik B. Patel, Nirmita J. Patel
  • Publication number: 20160280677
    Abstract: The present invention provides a process for the synthesis of olopatadine. Further, the invention discloses a process that results in improved yield of the desired Z isomer.
    Type: Application
    Filed: March 19, 2014
    Publication date: September 29, 2016
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Subhash Prataprao Chavan, Pradeep Bhaskarrao Laonkar
  • Publication number: 20160280678
    Abstract: Disclosed herein are a novel crown ether with bulky and rigid groups and a method for preparing the same. Also provided are a lithium adsorbent comprising the novel crown ether immobilized onto a nanofiber, and a method for preparing the same. The lithium-selective crown ether is synthesized through intermolecular cyclization between a bulky epoxide and a rigid aromatic compound such as 1,2-dihydroxybenzene, and can effectively recover lithium ions. For use as a lithium adsorbent, the novel crown ether with both bulky and rigid subunits is immobilized onto a polymer nanofiber. The crown ether-immobilized polymer nanofibers may be formed into a recyclable membrane.
    Type: Application
    Filed: April 30, 2015
    Publication date: September 29, 2016
    Applicant: MYONGJI UNIVERSITY INDUSTRY AND ACADEMIA COOPERATION FOUNDATION
    Inventors: Wook-Jin CHUNG, Lawrence A. LIMJUCO, Grace M. NISOLA, Rey Eliseo C. TORREJOS, Eleazer L. VIVAS, Hern KIM, Myoung Jun PARK, Jeong Gil SEO, Seong-Poong LEE
  • Publication number: 20160280679
    Abstract: A resist composition which generates acid upon exposure and exhibits changed solubility in a developing solution under action of acid, and which includes a base component which exhibits changed solubility in a developing solution under action of acid and an acid-generator component including a compound (B0-1) represented by general formula (b0) shown below in which Ra1 represents an aromatic ring; Ra01 represents an alkyl group of 5 or more carbon atoms optionally having a substituent; Ra02 and Ra03 each independently represents an alkyl group of 1 to 10 carbon atoms optionally having a substituent; n1 represents an integer of 1 to 5; n2 represents an integer of 0 to 2; n3 represents an integer of 0 to 4; and X? represents a counteranion.
    Type: Application
    Filed: March 22, 2016
    Publication date: September 29, 2016
    Inventors: Takashi NAGAMINE, Kotaro ENDO, Miki SHINOMIYA
  • Publication number: 20160280680
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
    Type: Application
    Filed: November 15, 2013
    Publication date: September 29, 2016
    Inventors: Bruce A. Ellsworth, Elizabeth A. Jurica, Jun Shi, William R. Ewing, Xiang-Yang Ye, Ximao Wu, Zhu Yeheng, Sun Chongqing
  • Publication number: 20160280681
    Abstract: Compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
    Type: Application
    Filed: November 12, 2013
    Publication date: September 29, 2016
    Applicant: Array BioPharma Inc.
    Inventors: Shelley Allen, James F. Blake, Barbara J. Brandhuber, Yutong Jiang, Gabrielle R. Kolakowski, Rui Xu, Shannon L. Winski
  • Publication number: 20160280682
    Abstract: Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Ring B, and Ring C are as defined herein, and wherein Ring B and the NH—C(?X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
    Type: Application
    Filed: November 12, 2013
    Publication date: September 29, 2016
    Applicant: Array BioPharma Inc.
    Inventors: Shelley Allen, Barbara J. Brandhuber, Timothy Kercher, Gabrielle R. Kolakowski, Shannon L. Winski
  • Publication number: 20160280683
    Abstract: Crystalline forms of 5-(4-cyclopropyl-1H-imidazol-1-yl)-N-(6-(4-isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-2-fluoro-4-methylbenzamide (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.
    Type: Application
    Filed: December 22, 2015
    Publication date: September 29, 2016
    Applicant: Gilead Sciences, Inc.
    Inventors: Mark Andres, Brenda J. Burke Chan, Ernest A. Carra, Anna Chiu, Olga Viktorovna Lapina, Stephen P. Lathrop, Valeriya Smolenskaya, Lok Him Yu
  • Publication number: 20160280684
    Abstract: The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.
    Type: Application
    Filed: June 3, 2016
    Publication date: September 29, 2016
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Jun TAKEUCHI, Satoshi ITADANI, Kazuya HASHIMURA, Masahiro IKURA, Masato HIGASHINO, Tetsuya YASUHIRO, Takeshi NAGAURA
  • Publication number: 20160280685
    Abstract: Amine substituted pyridine and pyrazine compounds and forms thereof that inhibit the function and reduce the level of B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.
    Type: Application
    Filed: November 21, 2013
    Publication date: September 29, 2016
    Inventors: Ramil Baiazitov, Soongyu Choi, Wu Du, Seongwoo Hwang, Chang-Sun Lee, Ronggang Liu, Young-Choon Moon, Steven D. Paget, Hongyu Ren, Nadiya Sydorenko, Richard Gerald Wilde
  • Publication number: 20160280686
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.
    Type: Application
    Filed: June 10, 2016
    Publication date: September 29, 2016
    Inventors: Shenlin Huang, Xianming Jin, Zuosheng Liu, Daniel Poon, John Tellew, Yongqin Wan, Xing Wang, Yongping Xie
  • Publication number: 20160280687
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.
    Type: Application
    Filed: June 10, 2016
    Publication date: September 29, 2016
    Inventors: Shenlin Huang, Xianming Jin, Zuosheng Liu, Daniel Poon, John Tellew, Yongqin Wan, Xing Wang, Yongping Xie
  • Publication number: 20160280688
    Abstract: 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: Application
    Filed: September 24, 2014
    Publication date: September 29, 2016
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: 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: 20160280689
    Abstract: The present invention is relates to an improved process for the preparation of pazopanib or a pharmaceutically acceptable salts thereof. The present invention also relates to novel polymorphic Forms of pazopanib hydrochloride, and its intermediates thereof.
    Type: Application
    Filed: November 5, 2014
    Publication date: September 29, 2016
    Inventors: Satyanarayana CHAVA, Seeta Rama Anjaneyulu GORANTLA, Venkata Sunil Kumar INDUKURI, Sanjay Kumar DEHURY, Nagaraju MEKALA, Jahangeer Baba SHAIK, Durga Prasad KUCHIPUDI
  • Publication number: 20160280690
    Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
    Type: Application
    Filed: November 13, 2013
    Publication date: September 29, 2016
    Applicant: Array BioPharma Inc.
    Inventors: Barbara J. Brandhuber, Yutong Jiang, Gabrielle R. Kolakowski, Shannon L. Winski
  • Publication number: 20160280691
    Abstract: Described herein are compounds and methods of making such compounds useful in the synthesis of protected N-alkyl-triazolecarbaldehydes.
    Type: Application
    Filed: November 6, 2014
    Publication date: September 29, 2016
    Inventor: Mark HENDERSON
  • Publication number: 20160280692
    Abstract: Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
    Type: Application
    Filed: November 12, 2013
    Publication date: September 29, 2016
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Steven Wade Andrews, James F. Blake, Barbara J. Brandhuber, Timothy Kercher, Shannon L. Winski
  • Publication number: 20160280693
    Abstract: The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS (amyotrophic lateral sclerosis), traumatic brain injury, ischemic brain injury, stroke, frontal temporal dementia, Pick's disease, corticobasal degeneration, supra cerebral palsy, prion diseases (e.g., Creutzfeldt-Jakob disease, Gerstmann-Straussler-Scheinker syndrome, Fatal Familial Insomnia, and Kuru), Nieman Pick type C, spinal cerebellar ataxia, spinal muscular dystrophy, ataxia telangiectasia, hippocampal sclerosis, Cockayne syndrome, Werner syndrome, xeroderma pigmentosaum, and Bloom syndrome.
    Type: Application
    Filed: August 25, 2015
    Publication date: September 29, 2016
    Applicants: Massachusetts Institute of Technology, The General Hospital Corporation d/b/a Massachusetts General Hospital
    Inventors: Li-Huei Tsai, Ling Pan, Stephen J. Haggarty, Debasis Patnaik
  • Publication number: 20160280694
    Abstract: The present invention relates to novel quinoline compounds of formula (I), and their pharmaceutically acceptable salts and process for their preparation. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptor agonists.
    Type: Application
    Filed: October 18, 2013
    Publication date: September 29, 2016
    Applicant: SUVEN LIFE SCIENCES LIMITED
    Inventors: Ramakrishna NIROGI, Anil Karbhari SHINDE, Venkateswarlu JASTI
  • Publication number: 20160280695
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
    Type: Application
    Filed: November 4, 2015
    Publication date: September 29, 2016
    Applicant: AMGEN INC.
    Inventors: Ana Elena MINATTI, Jonathan D. LOW, Jennifer R. ALLEN, Albert AMEGADZIE, James BROWN, Michael J. FROHN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Patricia LOPEZ, Vu Van MA, Nobuko NISHIMURA, Wenyuan QIAN, Shannon RUMFELT, Robert M. RZASA, Kelvin SHAM, Adrian L. SMITH, Ryan WHITE, Qiufen XUE
  • Publication number: 20160280696
    Abstract: The present invention relates to a compound of formula I, wherein the variables are defined as in the specification. The invention further refers to a composition comprising such compound and to the use thereof for controlling unwanted vegetation.
    Type: Application
    Filed: October 7, 2014
    Publication date: September 29, 2016
    Inventors: Frederick CALO, Markus KORDES, Helmut KRAUS, Thomas SEITZ, Trevor William NEWTON, Klaus KREUZ, Maciej PASTERNAK, Dario MASSA
  • Publication number: 20160280697
    Abstract: Compounds and compositions comprising compounds that activate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that activate PKM2 in the treatment of cancer.
    Type: Application
    Filed: March 24, 2016
    Publication date: September 29, 2016
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders
  • Publication number: 20160280698
    Abstract: This application relates to various salts and solid state forms of Compound (I). This application also relates to pharmaceutical compositions and therapeutic uses of these materials and compositions.
    Type: Application
    Filed: April 25, 2016
    Publication date: September 29, 2016
    Inventors: Stephen J. Bierlmaier, Ralph C. Heltiwanger, Martin J. Jacobs
  • Publication number: 20160280699
    Abstract: 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: Application
    Filed: September 24, 2014
    Publication date: September 29, 2016
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: 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: 20160280700
    Abstract: The invention relates to 1,2,4-thiadiazole derivatives and their use to treat parasites.
    Type: Application
    Filed: November 14, 2014
    Publication date: September 29, 2016
    Inventors: Hao LIU, Jessica Marie SLIGAR, Jason Daniel SPEAKE, Joseph A. MOORE, III, Brent Christopher BECK
  • Publication number: 20160280701
    Abstract: Biheteroaryl dicarboxylates and esters, and salts thereof which are useful as modulators of CP4H activity and more particularly as inhibitors of CP4H. Compounds of formula: and salts thereof where: X is S, O, NH, or NR, where R is an alkyl group having 1-3 carbon atoms; R1 and R2 independently are —OR7, or —NHSO2R8, where R7 is selected from: hydrogen, alkyl, alkenyl, alkoxyalkyl, —R?—CO—R?, —R?—CO—O—R?, —CO—R?, —R?—O—CO—R?, —R?—CO—NR?, —CO—NR?, or —R?—O—CO—NR?, and R8 is selected from hydrogen, alkyl, aryl, arylalkyl; R3, R4 and R6 independently are hydrogen, alkyl, alkoxy, alkenyl, alkenoxy, halo alkyl, haloalkenyl, halogen, hydroxyl, hydroxyalkyl, hydroxyalkenyl, aryl, aryloxy, arylalkyl or arylalkyloxy; R5 is hydrogen, halogen, alkyl having 1-3 carbon atoms, or alkoxy having 1-3 carbon atoms; —R?— is a divalent straight chain or branched alkylene, and —R? is an alkyl, alkenyl, arylalkyl, or aryl group. Methods for inhibition of CP4H in vivo and in vitro.
    Type: Application
    Filed: March 28, 2016
    Publication date: September 29, 2016
    Inventors: Ronald T. RAINES, James Vasta
  • Publication number: 20160280702
    Abstract: Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
    Type: Application
    Filed: November 12, 2013
    Publication date: September 29, 2016
    Applicant: Array BioPharma Inc.
    Inventors: Barbara J. Brandhuber, Yutong Jiang, Gabrielle R. Kolakowski, Shannon L. Winski
  • Publication number: 20160280703
    Abstract: Heteroaryloxycarbocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Application
    Filed: December 22, 2014
    Publication date: September 29, 2016
    Inventors: Jennifer R. Allen, Michael J. Frohn, Paul E. Harrington, Essa Hu Harrington, Alexander J. Pickrell
  • Publication number: 20160280704
    Abstract: Compounds of formula I are provided, which are JAK inhibitors and are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: March 19, 2014
    Publication date: September 29, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Matthew Lloyd Childers, Christopher Dinsmore, Peter Fuller, David Guerin, Jason David Katz, Qinglin Pu, Mark E. Scott, Christopher F. Thompson, Hongjun Zhang, Danielle Falcone, Luis Torres, Jason Brubaker, Hongbo Zeng, Jiaqiang Cai, Xiaoxing Du, Chonggang Wang, Yunfeng Bai, Norman Kong, Yumei Liu, Zhixiang Zheng
  • Publication number: 20160280705
    Abstract: A compound of formula (I) or a salt thereof wherein R1 represents a hydrogen atom, a methyl group or a ethyl group R2 represents a hydrogen atom or a fluorine atom R3 represents a hydrogen atom, a methyl group or an ethyl group.
    Type: Application
    Filed: March 26, 2014
    Publication date: September 29, 2016
    Inventors: Niall Andrew Anderson, Brendan John Fallon, John Martin Pritchard
  • Publication number: 20160280706
    Abstract: This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
    Type: Application
    Filed: March 31, 2014
    Publication date: September 29, 2016
    Inventors: Elbert Chin, Robert James Weikert, Weiya Yun, Jing Zhang
  • Publication number: 20160280707
    Abstract: Imidazoquinoline compounds with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
    Type: Application
    Filed: June 13, 2016
    Publication date: September 29, 2016
    Inventors: Kyle J. Lindstrom, Bryon A. Merrill, Chad A. Haraldson, Michael J. Rice, Tushar A. Kshirsagar, Philip D. Heppner, Joshua R. Wurst, Shri Niwas, Sarah J. Slania
  • Publication number: 20160280708
    Abstract: The present invention relates to certain spirocyclic compounds that are inhibitors of 11-? hydroxyl steroid dehydrogenase type 1 (11?HSD1), compositions containing the same, and methods of using the same for the treatment of diabetes, obesity and other diseases.
    Type: Application
    Filed: June 10, 2016
    Publication date: September 29, 2016
    Inventors: Wenqing Yao, Jincong Zhuo, Colin Zhang
  • Publication number: 20160280709
    Abstract: The invention relates to new and improved processes for the preparation of Alcaftadine and pharmaceutically acceptable salts thereof as well as an intermediate for the preparation of Alcaftadine. The new process saves a number of steps compared to the known process and results in a higher yield.
    Type: Application
    Filed: March 24, 2014
    Publication date: September 29, 2016
    Inventors: Antonio Lorente Bonde-Larsen, Jesús Miguel Iglesias Retuerto, Franciso Javiér Gallo Nieto, Juan José Ferreiro Gil
  • Publication number: 20160280710
    Abstract: The present invention provides process for preparing crystalline Pemetrexed dipotassium (I) Form-SP9 characterized by X-ray powder diffraction pattern comprising at least 5 characteristic 2?° peaks selected from the XRPD peak set of 5.0, 12.5, 17.2, 20.8, 22.4, 25.7, 26.9 and 27.9±0.2 2?°. The invention also provides process for preparing its pharmaceutical composition thereof, which may be useful for anti-cancer treatment.
    Type: Application
    Filed: November 11, 2014
    Publication date: September 29, 2016
    Applicant: SHILPA MEDICARE LIMITED
    Inventors: BHAGAT RAJ PIPAL, VENKATA REDDY GAYAM, AKSHAY KANT CHATURVEDI
  • Publication number: 20160280711
    Abstract: The present invention relates to a novel family of protein kinase inhibitors, more specifically the present invention is directed to inhibitors of the Tec or Src protein kinase families. The present invention also relates to the processes of preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative, inflammatory, autoimmune or infectious diseases, disorders, or conditions in which protein kinase activity is implicated.
    Type: Application
    Filed: November 20, 2014
    Publication date: September 29, 2016
    Applicant: Pharmascience Inc.
    Inventors: Alain Laurent, Yannick Rose
  • Publication number: 20160280712
    Abstract: The present invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.
    Type: Application
    Filed: June 3, 2016
    Publication date: September 29, 2016
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Benno Rothenhaeusler, Rene Trussardi, Fabienne Hoffmann-Emery, Urs Schwitter, Jean-Michel Adam, Olaf Grassmann, Thomas Hartung, Frederic Ran, Ralph Diodone, Christophe Pfleger, Bjorn Bartels
  • Publication number: 20160280713
    Abstract: The present invention relates to pyrazine derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
    Type: Application
    Filed: June 14, 2016
    Publication date: September 29, 2016
    Inventors: Liang Lu, Chunhong He, Wenqing Yao
  • Publication number: 20160280714
    Abstract: Embodiments of the present disclosure provide compositions including metal-organic polyhedrons, metalloporphyrin framework structures, methods of making these, methods of using these, and the like.
    Type: Application
    Filed: April 22, 2016
    Publication date: September 29, 2016
    Applicant: University of South Florida
    Inventors: Shengqian Ma, Peter X. Zhang, Xisen Wang, Le Meng, Qigan Cheng
  • Publication number: 20160280715
    Abstract: The invention provides methods of inhibiting the growth or metastasis of a cancer in a mammal by inhibiting a Ral GTPase in the mammal. The invention also provides small molecule inhibitors of Ral GTPases useful in the methods of the invention and pharmaceutical compositions containing the therapeutically effective compounds of the invention, and methods of using the same.
    Type: Application
    Filed: April 29, 2016
    Publication date: September 29, 2016
    Inventors: Dan THEODORESCU, Michael Fitzpatrick WEMPE, David ROSS, Samy MEROUEH, Martin A. SCHWARTZ, Phillip REIGAN
  • Publication number: 20160280716
    Abstract: The present disclosure relates to the preparation of pharmaceutically acceptable salt forms of the medicinal alkaloids Cepharanthine and Tetrandrine with improved solubility and physicochemical properties compared with the free base form of these alkaloids.
    Type: Application
    Filed: March 23, 2016
    Publication date: September 29, 2016
    Inventors: William E. BAUTA, Joseph A. McDonough, Mathew P.D. MAHINDARATNE, Robert A. DAVEY
  • Publication number: 20160280717
    Abstract: The compound “2-((4-nitrophenyl)amino)-6,7,8,9-tetrahydro-3H-cyclohepta[4,5]thieno-[2,3-d]pyrimidin-4(5H)-one” and method of synthesizing it, wherein the compound is effective to inhibit the growth and proliferation of human liver cancer cells HepG2. The compound has an inhibitory concentration value (IC50) of 0.7 ?g, compared to reference medication Doxorubicin that has an (IC50) value of 1.2 ?g. It further surpasses that reference medication Doxorubicin at all tested concentraions. The method includes the steps of: preparing a first compound of cycloheptanone, ethylcyanoacetate, sulfur, ethanol and diethyl amine; preparing a second compound by heating of the first compound with excess of hydrazine hydrate in absolute ethanol as solvent; and preparing the effective compound of the invention by reaction of the second chemical compound with 4-nitrophenylisothiocyanate in dry dimethylformamide as solvent.
    Type: Application
    Filed: March 25, 2015
    Publication date: September 29, 2016
    Inventor: Zainab Saeed Alghamdi
  • Publication number: 20160280718
    Abstract: This invention relates to novel macrolides, to the preparation of novel macrolides, to the use of such novel macrolides preventing, treating, or ameliorating various conditions, and to the use of such novel macrolides as antibacterial agents.
    Type: Application
    Filed: November 4, 2015
    Publication date: September 29, 2016
    Inventors: Chang-Hsing Liang, Jonathan Duffield, Alex Romero, Yu-Hung Chiu, Steve Sucheck, Kenneth Marby, Youe-Kong Shue, Yoshitaka Ichikawa, Chan-Kou Hwang, David Rabuka, Sulan Yao
  • Publication number: 20160280719
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: November 20, 2014
    Publication date: September 29, 2016
    Applicant: NOVARTIS AG
    Inventors: Jutta BLANK, Guido BOLD, Vincent BORDAS, Simona COTESTA, Vito GUAGNANO, Heinrich RUEGER, Andrea VAUPEL
  • Publication number: 20160280720
    Abstract: A reagent includes an element, formally in oxidation state zero, in complex with a hydride molecule and an incorporated ligand. The incorporated ligand typically has surface active properties. The reagent, termed a Ligated Anionic Element Reagent Complex, can be useful in synthesis of elemental nanoparticles. A method for synthesizing the aforementioned reagent includes a step of ball-milling a mixture containing an elemental powder, bulk hydride molecule, and bulk ligand. The components of the reagent, once complexed, have altered electronic structure and vibrational modes.
    Type: Application
    Filed: June 8, 2016
    Publication date: September 29, 2016
    Inventors: Michael Paul Rowe, Elizabeth Marie Skoropata, Johan Alexander van Lierop
  • Publication number: 20160280721
    Abstract: Provided are methods for site- and stereo-retentive cross-couplings with unactivated secondary boronic acids, which methods are particularly useful in building block-based approach for small molecule synthesis. Also provided is a method of forming an air-stable chiral secondary boronic acid.
    Type: Application
    Filed: November 3, 2014
    Publication date: September 29, 2016
    Inventors: Martin D. Burke, Pulin Wang, Ian Crouch
  • Publication number: 20160280722
    Abstract: Bis phenolate transition metal complexes are disclosed for use in alkene polymerization, with optional chain transfer agent, to produce polyolefins.
    Type: Application
    Filed: February 23, 2016
    Publication date: September 29, 2016
    Inventors: Crisita Carmen H. Atienza, David A. Cano, John R. Hagadorn, Rhutesh K. Shah