Patents Issued in November 29, 2018
  • Publication number: 20180339955
    Abstract: The present invention relates to a method for preparing mannitol which includes performing the hydrogenation of fructose in the presence of a Cu-based nanocomposite catalyst, for example, a nanocomposite catalyst of CuO(x)/SiO2(100-x) (wherein x is a real number from 20 to 90), using butanol as a solvent.
    Type: Application
    Filed: May 29, 2018
    Publication date: November 29, 2018
    Inventors: Dong Won HWANG, Pravin Pandharinath UPARE, Young Kyu HWANG, Do Young HONG, Jong San CHANG, U Hwang LEE, Su Kyung LEE, Kyung Ho CHO
  • Publication number: 20180339956
    Abstract: The present invention relates to a new process for the synthesis of 17?-hydroxy-des-A-androst-9,10-en-5-one, the compound of the following formula (1), which can be used as an intermediate in the synthesis of retroprogesterones.
    Type: Application
    Filed: October 28, 2016
    Publication date: November 29, 2018
    Applicant: INDUSTRIALE CHIMICA S.R.L.
    Inventors: Roberto LENNA, Roberto DI BRISCO
  • Publication number: 20180339957
    Abstract: A method of recycling a polyester includes the steps of providing the polyester, preparing a solution containing water and an alcohol, submerging the polyester in the solution, and hydrolytically depolymerizing the polyester while the polyester is submerged in the solution.
    Type: Application
    Filed: May 23, 2018
    Publication date: November 29, 2018
    Inventors: Rafael Auras, Fabiola Maria Iñiguez-Franco, Maria Rubino, Daniel Holmes, Susan E. Selke, Xiaoyi Fang
  • Publication number: 20180339958
    Abstract: Methods for preparing isotopically modified 1,4-diene systems from non-isotopically modified 1,4-dienes involve selective oxidation of one or more bis-allylic position(s), or the preparation of isotopically modified 1,4-diene systems via trapping pi-allylic complexes with a source of deuterium or tritium. Such methods are useful for preparing isotopically modified polyunsaturated lipid including polyunsaturated fatty acids and polyunsaturated fatty acid derivatives.
    Type: Application
    Filed: September 9, 2016
    Publication date: November 29, 2018
    Inventors: Dragoslav Vidovic, Mikhail Sergeevich Shchpinov
  • Publication number: 20180339959
    Abstract: The present invention relates to a process for hydrogenating nitrile compounds to amino compounds, in which the cross-sectional loading of the reactor during the hydrogenation is less than or equal to 4.0 kg/m2*s, based on the liquid phase.
    Type: Application
    Filed: May 17, 2018
    Publication date: November 29, 2018
    Inventors: Anne Rittsteiger, Stephan Kohlstruk, Dirk Hoppe, Alexander Martin Rüfer, Sabrina Sowka, Sven Schneider, Norbert Schlüter, Axel Hengstermann, Markus Galle, Stefan Röder, Monika Berweiler
  • Publication number: 20180339960
    Abstract: Described herein, inter alia, are compositions of PCNA modulators and methods for treating or preventing cancer.
    Type: Application
    Filed: September 16, 2016
    Publication date: November 29, 2018
    Inventors: Linda H. Malkas, David Horne, Robert J. Hickey, Long Gu
  • Publication number: 20180339961
    Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a dimethyl-nonatetraenyl-trimethyl-cyclohexyl structure useful as therapeutics for the treatment of subjects suffering from disorders characterized by abnormal proliferation and/or abnormal differentiation of cells, in particular of cells of which the growth and differentiation is sensitive to the actions of retinoids.
    Type: Application
    Filed: May 23, 2018
    Publication date: November 29, 2018
    Inventors: James Varani, Hollis Showalter, Andy White, Kent J. Johnson
  • Publication number: 20180339962
    Abstract: Described are new forms of crystalline minocycline base. In particular, two new crystalline polymorphic forms, designated Form IV and Form V of minocycline base are provided. These are characterized by XRD, FTIR and TGA. Processes for preparing the new polymorphic forms and their use in pharmaceutical compositions are also provided. Form IV and Form V are prepared by dissolving and/or suspending minocycline base in an organic solvent followed by crystallization.
    Type: Application
    Filed: July 23, 2018
    Publication date: November 29, 2018
    Applicant: Hovione Scientia Limited
    Inventors: Zita Mendes, Constanca Cacela, Gloria Ten Figas, Ana Fernandez Casares
  • Publication number: 20180339963
    Abstract: The invention contemplates novel materials as anticonvulsant agents.
    Type: Application
    Filed: May 22, 2018
    Publication date: November 29, 2018
    Applicant: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
    Inventors: Meir BIALER, David BIBI, Hafiz MAWASI
  • Publication number: 20180339964
    Abstract: The present invention provides an industrial method for production of silodosin, which is useful for a therapeutic agent for dysuria associated with benign prostatic hyperplasia. The production of silodosin is characterized by mixing (R)-1-(3-hydroxypropyl)-5-(2-(2-(2-(2, 2, 2-trifluoroethoxy) phenoxy) ethyl amino) propyl) indoline-7-carbonitrile (V) and N-acetyl-L-glutamic acid to yield the N-acetyl-L-glutamate salt, subsequently neutralising the N-acetyl-L-glutamate salt and hydrolyzing the same, and manufacturing intermediates used therefore. The invention also provides an industrial production method of silodosin alpha, beta and gamma crystalline forms.
    Type: Application
    Filed: September 21, 2016
    Publication date: November 29, 2018
    Inventors: Chandrashekar ASWATHANARAYANAPPA, Thilak Gregory SOUNDARARAJAN, Nooka Appa Rao GORLI V, Surendra Babu JAGABATHUNI, Palle Venkata Raghavendra CHARYULU
  • Publication number: 20180339965
    Abstract: The present invention relates to a novel oxindole derivative having anticancer activity, a preparation method thereof, and a method for treating cancer using the same. More specifically, the present invention relates to an oxindole derivative produced as a result of CH alkylation and subsequent intramolecular cyclization reaction using a rhodium (III) catalyst, a preparation method of the same, and a method for treating cancer containing the same as an active ingredient. The novel oxindole derivatives according to the present invention have excellent anticancer activity against various human cancer cell lines and are expected to be useful for the treatment of cancer. In addition, the preparation method of an oxindole derivative using the rhodium (III) catalyst of the present invention can be applied and introduced into a wide range of functional groups, and is a reaction having positional selectivity and chemical selectivity.
    Type: Application
    Filed: May 24, 2018
    Publication date: November 29, 2018
    Applicant: RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIVERSITY
    Inventors: In Su KIM, Hyung Sik KIM
  • Publication number: 20180339966
    Abstract: The invention provides a compound of formula I: or a salt thereof, wherein R1, R2, R3, R4 and ring A have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as anti-cancer agents.
    Type: Application
    Filed: April 20, 2018
    Publication date: November 29, 2018
    Inventors: Zigang Dong, Ann M. Bode, Kanamata Reddy
  • Publication number: 20180339967
    Abstract: The present invention relates to a compound for an organic optoelectronic device represented by chemical formula 1, an organic optoelectronic device employing the same and a display device apparatus. The details of chemical formula 1 are as defined in the specification.
    Type: Application
    Filed: April 18, 2016
    Publication date: November 29, 2018
    Inventors: Byungku KIM, Hyung Sun KIM, Eun Sun YU, Sangshin LEE, Yuna JANG, Chunkeun JANG, Sung-Hyun JUNG, Ho-Kuk JUNG
  • Publication number: 20180339968
    Abstract: The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): comprising treating a compound of Formula (I): with a transition metal catalyst and under alkylation conditions as valence and stability permit.
    Type: Application
    Filed: July 30, 2018
    Publication date: November 29, 2018
    Inventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
  • Publication number: 20180339969
    Abstract: A compound having a SF4 group on a pyridine ring is provided. Specifically, the compound is represented by the general formula (c): wherein k is 1 or 2; X is a hydrogen atom or a halogen atom; R1 is a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl group having 1 to 18 carbon atoms, a substituted or unsubstituted aryl group having 6 to 30 carbon atoms, or a nitro group; and R2 is a substituted or unsubstituted alkyl group having 1 to 18 carbon atoms or a substituted or unsubstituted aryl group having 6 to 30 carbon atoms.
    Type: Application
    Filed: September 23, 2016
    Publication date: November 29, 2018
    Inventors: Norio SHIBATA, Kohei MATSUZAKI, Norimichi SAITO
  • Publication number: 20180339970
    Abstract: Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of monoacylglycerol lipase (MAGL). Furthermore, the subject compounds and compositions are useful for the treatment of pain.
    Type: Application
    Filed: May 22, 2018
    Publication date: November 29, 2018
    Inventors: Cheryl A. GRICE, John J. M. WIENER, Olivia D. WEBER, Katharine K. DUNCAN
  • Publication number: 20180339971
    Abstract: The invention relates to morpholine and 1,4-oxazepane amide derivatives of general formula (I), which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture of the compounds according to the invention.
    Type: Application
    Filed: July 30, 2018
    Publication date: November 29, 2018
    Inventors: Rocco MAZZAFERRO, Marco FERRARA, Riccardo GIOVANNINI, Iain LINGARD, Klaus RUDOLF
  • Publication number: 20180339972
    Abstract: The invention provides a compound of formula I: or a salt thereof, wherein R1, R2, R3, R4, L1, L2 and Y have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful for labeling penicillin-binding proteins (PBPs).
    Type: Application
    Filed: May 24, 2018
    Publication date: November 29, 2018
    Applicants: REGENTS OF THE UNIVERSITY OF MINNESOTA, Indiana University Research and Technology Corporation
    Inventors: Erin Elizabeth Carlson, Shabnam Sharifzadeh, Alireza Shokri, Ozden Kocaoglu, Clayton Brown
  • Publication number: 20180339973
    Abstract: ?9-THC carboxylic acid is extracted from cannabis flowers using a first organic solvent, then separated using a second aqueous solvent. ?9-THC carboxylic acid is converted to ?9-THC carboxylic salt before being extracted by a third organic solvent and converted back to ?9-THC carboxylic acid. Using a solvent swap, ?9-THC carboxylic acid is decarboxylated and extracted again with an organic solvent prior to purification to give ?9-THC.
    Type: Application
    Filed: August 1, 2018
    Publication date: November 29, 2018
    Inventors: Lekhram CHANGOER, Cornelis Herman Michel VAN DER LOO, Erik KELLER
  • Publication number: 20180339974
    Abstract: The present disclosure belongs to the technical field of organic synthesis and particularly relates to a preparation method for 2-((4R,6S)-6-bromomethyl-2-oxo-1,3-dioxane-4-yl)acetate. The 2-((4R,6S)-6-bromomethyl-2-oxo-1,3-dioxane-4-yl)acetate is a key chiral intermediate for preparation of statin antilipemic agents. In the present disclosure, the 2-((4R,6S)-6-bromomethyl-2-oxo-1,3-dioxane-4-yl)acetate is obtained by bromination and cyclization of 3-((substituted oxycarbonyl)oxy)-5-hexenoate as raw material with hypochlorite and bromide in an organic solvent in the presence of CO2. The method of the present disclosure has the advantages of readily available raw material, mild reaction conditions, easy operation, low cost, excellent atomic economy and less by-products, and is applicable to industrial production.
    Type: Application
    Filed: January 14, 2018
    Publication date: November 29, 2018
    Inventors: Fener CHEN, Guanxin HUANG, Ge MENG, Minjie LIU, Yan WU, Dang CHENG, Zedu HUANG, Haihui PENG, Fangjun XIONG
  • Publication number: 20180339975
    Abstract: The present invention relates to compounds of formula I wherein R1? is CH3; R1 is CH3, ethyl, CF3, CH2OH, cyclopropyl or cyano, or R1? and R1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R2 is hydrogen, CH3, ethyl, isopropyl, tert-butyl, cyclopropyl, cyclopropyl-methyl or hydroxy-methyl; R3 is hydrogen, Cl, F, CF3, CH3, isopropyl, methoxy, cyano or cyclopropyl; R4 is hydrogen, CH3, F or Cl; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.
    Type: Application
    Filed: July 30, 2018
    Publication date: November 29, 2018
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Marius HOENER, Juergen WICHMANN
  • Publication number: 20180339976
    Abstract: The present invention relates to novel triazole derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.
    Type: Application
    Filed: March 29, 2016
    Publication date: November 29, 2018
    Inventors: ALEXANDER SUDAU, SEBASTIAN HOFFMANN, PETER DAHMEN, ULRIKE WACHENDORFF-NEUMANN, DAVID BERNIER, RICARDA MILLER, PIERRE-YVES COQUERON, PIERRE GENIX, SVEN WITTROCK, JEAN-PIERRE VORS, PHILIPPE KENNEL, STEPHANE BRUNET, SEBASTIEN NAUD, RUTH MEISSNER
  • Publication number: 20180339977
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma Kallikrein.
    Type: Application
    Filed: October 24, 2016
    Publication date: November 29, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Jiayi Xu, Amjad Ali, Wei Zhou, Ying-Duo Gao, Scott D. Edmondson, Eric Mertz, Santhosh F. Neelamkavil, Weiguo Liu, Wanying Sun, Dong-Ming Shen, Bart Harper, Cheng Zhu, Thomas Bara, Yeon-Hee Lim, Meng Yang
  • Publication number: 20180339978
    Abstract: The present invention relates to substituted pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: August 6, 2018
    Publication date: November 29, 2018
    Applicant: NERVIANO MEDICAL SCIENCES S.r.l.
    Inventors: Maria Gabriella Brasca, Simona Bindi, Marina Caldarelli, Marcella Nesi, Sten Christian Orrenius, Achille Panzeri
  • Publication number: 20180339979
    Abstract: Disclosed are aryl pyrimidine compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure (I) and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein A, Z, R and R? are as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-? superfamily, and can be used to treat disease by blocking such activity.
    Type: Application
    Filed: March 29, 2016
    Publication date: November 29, 2018
    Inventors: Marina Gelman, Pingyu Ding, Todd Kinsella, Rajinder Singh, Somasekhar Bhamidipati, Jeffrey Clough
  • Publication number: 20180339980
    Abstract: The invention relates to thiocarbamate prodrug compounds of the Janus kinase (JAK) inhibitor tofacitinib having formula I: wherein R1, R2, R3, R4 and n are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: May 22, 2018
    Publication date: November 29, 2018
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventor: DANIEL D. LONG
  • Publication number: 20180339981
    Abstract: The manufacture and use of compounds of formula (Ia) or a pharmaceutically acceptable salt thereof for preventing, inhibiting or treating cancer, AIDS and/or premature aging. The compounds of formula (Ia) being: where: R independently represents a hydrogen atom, a halogen atom, a (C1-C3)alkyl group, a —CN group, a hydroxyl group, a —COOR1 group, a (C1-C3)fluoroalkyl group, a —NO2 group, a —NR1R2 group, or a (C1-C3)alkoxy group; R? is a hydrogen atom, a halogen atom, a (C1-C3)alkyl group, a —NO2 group, a (C1-C3)alkoxy group, or a —NR1R2 group; and R1 and R2 are a hydrogen atom or a (C1-C3) alkyl group.
    Type: Application
    Filed: July 31, 2018
    Publication date: November 29, 2018
    Applicants: ABIVAX, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, UNIVERSITE DE MONTPELLIER
    Inventors: Jamal TAZI, Florence MAHUTEAU, Romain NAJMAN, Didier SCHERRER, Julien SANTO
  • Publication number: 20180339982
    Abstract: The present disclosure provides bicyclic heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as bromodomain inhibitors; (I), in which R1, R2, R3, R4, L1, L2, Cy1, Cy2, X, n, and dotted line have the same meaning given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in diseases or disorders associated as bromodomain inhibitors. The present disclosure also provides preparation of compounds and pharmaceutical formulations comprising at least one of bicyclic heterocyclic derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent, or excipient.
    Type: Application
    Filed: August 1, 2018
    Publication date: November 29, 2018
    Inventors: Susanta SAMAJDAR, Chandrasekhar Abbineni, Sanjita Sasmal, Subramanya Hosahalli
  • Publication number: 20180339983
    Abstract: The present invention relates to biaryl monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A1, Q, M, W, RX and Rz are as defined herein. The present invention also relates to compositions which comprise a biaryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.
    Type: Application
    Filed: December 12, 2016
    Publication date: November 29, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Weiguo Liu, Fa-Xiang Ding, Wanying Sun, Yi Zang, Weidong Pan, Anthony Ogawa, Linda Brockunier, Xianhai Huang, Hongwu Wang, Rudrajit Mal, Tesfaye Biftu, Min Park, Yan Guo, Jinlong Jiang, Helen Y. Chen, Christopher W. Plummer
  • Publication number: 20180339984
    Abstract: The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula I for treatment of neurodegenerative diseases and disorders, such as Alzheimer's disease.
    Type: Application
    Filed: May 18, 2018
    Publication date: November 29, 2018
    Inventors: Nicolas Jacques Francois Dreyfus, Peter James Lindsay-Scott, Richard Edmund Rathmell
  • Publication number: 20180339985
    Abstract: The invention relates to pyrridinobenzodiazepines (PDDs) comprising three fused 6-7-6-membered rings linked to aromatic groups, and pharmaceutically acceptable salts thereof, which are useful as medicaments, such as anti-proliferative agents.
    Type: Application
    Filed: April 14, 2018
    Publication date: November 29, 2018
    Inventors: Paul Joseph Mark JACKSON, David Edwin THURSTON, Khondaker Mirazur RAHMAN
  • Publication number: 20180339986
    Abstract: The application relates to inhibitors of USP1 useful in the treatment of cancers, and other USP1 associated diseases and disorders, having the Formula: where R1, R2, R3, R3?, R4, R5, X1, X2, X3, X4, and n are described herein.
    Type: Application
    Filed: August 1, 2018
    Publication date: November 29, 2018
    Inventors: Alexandre Joseph Buckmelter, Stephanos Ioannidis, Bruce Follows, Gary Gustafson, Minghua Wang, Justin A. Caravella, Zhongguo Wang, Edward L. Fritzen, Jian Lin
  • Publication number: 20180339987
    Abstract: Compound I and a compound II as well as preparation methods therefor and use thereof are disclosed. A newly synthesized compound of formula I is capable of stimulating congenital immunity and cellular immunity for tumor resistance while greatly improving the antitumor effect of ethacrynic acid (EA), and thus an integrated synergistic anti-tumor dual-immunity drug design is explored. The immune response mechanism for resisting melanoma of the compound as shown in the formula I is demonstrated. A compound that is as shown in a formula II and is prepared from the compound of formula I and ROR1 by means of covalency markedly slows down the growth of subcutaneously transplanted mammary cancer tumor, such that the immune response mechanism, for treating the mammary cancer, of the compound as shown in the formula II is demonstrated.
    Type: Application
    Filed: November 8, 2016
    Publication date: November 29, 2018
    Applicants: SHENZHEN UNIVERSITY, SHENZHEN KANGJUZHENG PHARMACEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Guangyi JIN, Zhulin WANG
  • Publication number: 20180339988
    Abstract: The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where m, n, X1, X2, R1-R5, R5 and R6 are described herein.
    Type: Application
    Filed: January 18, 2018
    Publication date: November 29, 2018
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell, Darby Rye Schmidt, David Joseph Guerin, Justin Andrew Caravella, R. Bruce Diebold, Anna Ericsson, David R. Lancia, JR.
  • Publication number: 20180339989
    Abstract: The invention provides novel methods for preparing indolinobenzodiazepine monomer compounds and their synthetic precursors.
    Type: Application
    Filed: April 19, 2018
    Publication date: November 29, 2018
    Inventors: Baudouin Gérard, Richard A. Silva, Michael Louis Miller, Manami Shizuka
  • Publication number: 20180339990
    Abstract: The invention relates to glucuronide prodrug compounds of Janus kinase (JAK) inhibitors having formula I: where W1, R1 and A1 are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: May 22, 2018
    Publication date: November 29, 2018
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: DANIEL D. LONG, DONNA A.A. WILTON, MANDY M. LOO, RYAN HUDSON, PATRICK J. BRASSIL
  • Publication number: 20180339991
    Abstract: The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R5, R5?, R6, X1, X2, m, and n are described herein.
    Type: Application
    Filed: May 24, 2018
    Publication date: November 29, 2018
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell
  • Publication number: 20180339992
    Abstract: The present disclosure is concerned with certain pyrrolopyrimidine compounds that are capable of inhibiting certain protein kinases, and especially the leucine-rich repeat kinase 2 (LRRK2) protein. Compounds of the present disclosure can be used to treat a number of disorders caused by or associated with abnormal LRRK2 kinase activity. Compounds of the present disclosure can be used to treat disorders including neurodegenerative diseases such as Parkinson's disease; precancerous conditions and cancer; autoimmune disorders such as Crohn's disease, rheumatoid arthritis and psoriasis; and leprosy (Hansen's disease). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: July 11, 2018
    Publication date: November 29, 2018
    Inventors: Corinne E. Augelli-Szafran, Mark Suto, Robert Galemmo, Omar Moukha-Chafiq, Vandana Gupta, Subramaniam Ananthan
  • Publication number: 20180339993
    Abstract: The present invention relates to azaspiro derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor,
    Type: Application
    Filed: July 31, 2018
    Publication date: November 29, 2018
    Applicant: RaQualia Pharma Inc.
    Inventors: Yuji SHISHIDO, Masashi OHMI, Kazuo ANDO
  • Publication number: 20180339994
    Abstract: A compound represented by the following formula (1):
    Type: Application
    Filed: August 26, 2016
    Publication date: November 29, 2018
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Yu KUDO, Yumiko MIZUKI, Masahiro KAWAMURA, Tomoki KATO, Hirokatsu ITO, Tasuku HAKETA, Yuichi NISHIMAE, Annemarie WOLLEB
  • Publication number: 20180339995
    Abstract: A compound according to Formula IA and IB, reversibly convertible under photochromic and electrochromic conditions between a ring-open isomer A and a ring-closed isomer B is provided. For substitutent groups, Z is N, O or S; each R1 is independently selected from the group consisting of H, or halo; each R2 is independently selected from the group consisting of H, halo, a polymer backbone, alkyl or aryl; or, when both R2 together form —CH?CH— and form part of a polymer backbone; each R3 is independently selected from the group consisting of H, halo, alkyl, alkoxy, thioalkyl or aryl; each R4 is aryl; and each R5 is independently selected from the group consisting of H, halo, alkyl, alkoxy, thioalkyl or aryl.
    Type: Application
    Filed: July 25, 2018
    Publication date: November 29, 2018
    Applicant: SWITCH MATERIALS, INC.
    Inventors: Neil Robin BRANDA, Jeremy Graham FINDEN, Simon James GAUTHIER, Ali HAYEK, Kyle Andrew HOPE-ROSS, James Daniel SENIOR, Andreea SPANTULESCU, Serguei SVIRIDOV
  • Publication number: 20180339996
    Abstract: The present invention relates to compound of formula (I) (I) wherein the variables are as defined in the claims and the description. The invention further relates to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, to their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to methods for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
    Type: Application
    Filed: November 24, 2016
    Publication date: November 29, 2018
    Inventors: Gisela BACKFISCH, Margaretha Henrica Maria BAKKER, Günter BLAICH, Wilfried BRAJE, Karla DRESCHER, Thomas ERHARD, Andreas HAUPT, Carolin HOFT, Viktor LAKICS, Helmut MACK, Frank OELLIEN, Raimund PETER, Ana Lucia RELO
  • Publication number: 20180339997
    Abstract: The present invention relates to crystalline polymorph forms of (S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide (GDC-0077), having the structure, Formula I: or stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, and processes of preparing the polymorph forms.
    Type: Application
    Filed: April 26, 2018
    Publication date: November 29, 2018
    Applicant: Genentech, Inc.
    Inventors: Paroma Chakravarty, Chong Han, Sean M. Kelly, Karthik Nagapudi, Scott Savage
  • Publication number: 20180339998
    Abstract: Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 26, 2018
    Publication date: November 29, 2018
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Peter Dragovich, Xiongcai Liu, Snahel Patel, Po-Wai Yuen, Mark Zak, Guiling Zhao, Yamin Zhang, Xiaozhang Zheng
  • Publication number: 20180339999
    Abstract: The present invention relates to chiral phosphoramidimidates, their salts and metal complexes as well as derivatives thereof and their use as catalysts.
    Type: Application
    Filed: August 31, 2016
    Publication date: November 29, 2018
    Applicant: STUDIENGESELLSCHAFT KOHLE MBH
    Inventors: Benjamin LIST, Philip Stephan Joseph KAIB, Lucas SCHREYER, Sunggi LEE, Roberta PROPERZI, Luping LIU
  • Publication number: 20180340000
    Abstract: An electrolyte for Li-ion and other secondary electrochemical cells includes an FSI anion and at least one of methyltriethylphosphonium; trimethylisobutylphosphonium; methyltributylphosphonium; and trihexyltetradecylphosphonium. The electrolyte uniquely enables stable cell cycling even when water is present in the electrolyte at levels as high as 5000 ppm. Methyltriethylphosphonium and trimethylisobutylphosphonium-containing electrolytes are particularly effective in this water-stabilizing capacity.
    Type: Application
    Filed: May 26, 2017
    Publication date: November 29, 2018
    Inventors: Nikhilendra Singh, Timothy S. Arthur, Kensuke Takechi, Patrick Howlett, Maria Forsyth, Robert Kerr, Fuminori Mizuno
  • Publication number: 20180340001
    Abstract: The present invention contemplates a method for synthesizing [18F] fluoride complexes suitable for performing radio-labeling reactions to generate [18F] fluorinated species for use as imaging agents. The present invention further contemplates kits for making [18F] fluoride complexes suitable for performing radio-labeling reactions to generate [18F] fluorinated species. The present invention further contemplates a method of using [18F] fluoride prosthetic group for targeted tissue and disease imaging.
    Type: Application
    Filed: April 19, 2018
    Publication date: November 29, 2018
    Inventors: Francois P. Gabbai, Boris Vabre, Kantapat Chansaenpak, Zibo Li, Mengzhe Wang, Hui Wang
  • Publication number: 20180340002
    Abstract: An organometallic compound represented by Formula 1: wherein in Formula 1, A1 to A4, M, and T1 to T3 are the same as described in the specification.
    Type: Application
    Filed: May 17, 2018
    Publication date: November 29, 2018
    Inventors: Bumwoo PARK, Sangdong KIM, Soyeon KIM, Sukekazu ARATANI, Jungin LEE, Kyuyoung HWANG, Yoonhyun KWAK, Ohyun KWON
  • Publication number: 20180340003
    Abstract: A method of enhancing the growth of an animal, as well as treating or preventing antimicrobial infections is provided. The method includes causing the animal to ingest or absorb an effective amount of one or more Fe III complex compounds, including but not limited to Fe III complexes comprising ligands bound to the iron center such as amino acids or ?-hydroxy acids. The compounds are also useful for inhibiting, reducing, or preventing biofilm formation or buildup on a surface; the treatment of, inhibition of growth of, and inhibition of colonization by, bacteria, both in biological and non-biological environments; disinfecting surfaces, potentiating the effects of antibiotics and other anti-microbial agents, and increasing the sensitivity of bacteria and other microorganisms, to anti-microbial agents are also provided.
    Type: Application
    Filed: August 3, 2018
    Publication date: November 29, 2018
    Inventors: Dlawer Ala'Aldeen, Jafar Mahdavi, Panos Soultanas
  • Publication number: 20180340004
    Abstract: Provided herein are formulations, methods and substituted 2?-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2?-chloro aminopyrimidinone and pyrimidine dione compounds.
    Type: Application
    Filed: April 11, 2018
    Publication date: November 29, 2018
    Inventors: Michael O' Neil Hanrahan Clarke, Richard L. Mackman, Dustin Siegel