Patents Issued in August 1, 2019
  • Publication number: 20190233388
    Abstract: An electrolyte, electrochemical device, battery, capacitor, and/or the like include a salt; and a fluorinated organosulfate compound represented by Formula I: wherein, R1 is H, OR3, alkyl, alkenyl, alkynyl, aralkyl, or silyl; R2 is H, OR3, alkyl, alkenyl, alkynyl, aralkyl, or silyl; and R3 is H, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, or siloxy; or where R1 and R2 join together to form a cyclic compound incorporating the —O—S(O)2—O— group; wherein at least one R1 and R2 is fluorinated.
    Type: Application
    Filed: January 31, 2018
    Publication date: August 1, 2019
    Inventors: Khalil Amine, Chi Cheung Su, Meinan He, Tianyuan Ma
  • Publication number: 20190233389
    Abstract: The present invention is related to an improved process for the preparation of Pomalidomide with higher yields and high purity. Particularly the present invention relates to form A preparation of Pomalidomide and its purification, wherein the present process doesn't involve use of dioxane solvent and avoids higher temperatures.
    Type: Application
    Filed: August 22, 2016
    Publication date: August 1, 2019
    Inventors: Durga Prasad Konakanchi, Buchappa Gongalla, Dharmendher Ragidi, Uma Naresh Babu Kotra, Kali Satya Bhujanga Rao Adibhatla, Venkaiah Chowdary Nannapaneni
  • Publication number: 20190233390
    Abstract: The present invention provides a compound of a general formula I, a stereomeride, pharmaceutically acceptable salt or a solvate thereof, a preparation method thereof, and usages in preparing medicines for preventing and/or treating diseases or symptoms caused by drug-resistant tumors or drug-resistant bacteria and in preparing medicines for preventing and/or treating diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and infection. Preferably, the diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and infection are diseases or symptoms caused by a heat shock protein 70 (Hsp70). The compound in the present invention is used for overcoming a difficult problem of drug resistance of tumors, improves the effect of tumor treatment, and provides a new medical strategy for clinical tumor treatment.
    Type: Application
    Filed: April 9, 2019
    Publication date: August 1, 2019
    Applicant: Institute of Pharmacology and Toxicology Academy of Millitary Medical Sciences P.L.A. China
    Inventors: Wu ZHONG, Song Li, Yanqun Zeng, Junhai Xiao, Xinbo Zhou, Zhibing Zheng, Xingzhou Li, Xiaokui Wang
  • Publication number: 20190233391
    Abstract: The invention relates to benzodiazepine derivatives of formula (A) useful as CCK2/gastrin receptor antagonists, their preparation and their use in the treatment or prevention of disorders associated with CCK2/gastrin receptors, disorders caused by or associated with hypergastrinaemia, and gastric acid-related disorders.
    Type: Application
    Filed: April 12, 2019
    Publication date: August 1, 2019
    Inventors: Malcolm James Boyce, Liv Thomsen, Donald Alan Gilbert, David Wood
  • Publication number: 20190233392
    Abstract: This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases.
    Type: Application
    Filed: January 29, 2019
    Publication date: August 1, 2019
    Inventors: Dengjin Wang, Pingli Liu, Yongzhong Wu, Jiacheng Zhou
  • Publication number: 20190233393
    Abstract: The present invention relates to the crystalline forms of a 5-HT1F receptor agonist 2,4,6-trifluoro-N-[6-[(1-methyl-piperidine-4-yl)carbonyl]pyridin-2-yl]-benzene formamide (lasmiditan) and its hydrochloride. The crystalline forms of the present invention have advantages in crystallinity, hygroscopicity, morphology, crystal form stability, and chemical stability as compared with the known forms of lasmiditan and lasmiditan hydrochloride. The present invention also relates to processes for the preparation of the crystalline forms of lasmiditan and lasmiditan hydrochloride, pharmaceutical compositions thereof and their use in treating and/or preventing a patient's migraine and other diseases or conditions associated with 5-HT1F receptor dysfunction.
    Type: Application
    Filed: November 11, 2016
    Publication date: August 1, 2019
    Applicant: Solipharma LLC
    Inventors: Xiaohong SHENG, Xiaoxia SHENG, Xiawei JIANG
  • Publication number: 20190233394
    Abstract: The present invention relates to compounds of Formula (I) that are useful as inhibitors of the activity of the ubiquitin specific protease USP19. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in therapy.
    Type: Application
    Filed: July 26, 2017
    Publication date: August 1, 2019
    Applicant: Almac Discovery Limited
    Inventors: Peter HEWITT, Mary Melissa MCFARLAND, James Samuel Shane ROUNTREE, Frank BURKAMP, Christina BELL, Lauren PROCTOR, Matthew Duncan HELM, Colin O'DOWD, Timothy HARRISON
  • Publication number: 20190233395
    Abstract: The present application relates to novel substituted indazoles, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of endometriosis and endometriosis-associated pain and other endometriosis-associated symptoms such as dysmenorrhoea, dyspareunia, dysuria and dyschezia, of lymphoma, rheumatoid arthritis, spondyloarthritis (especially psoriatic spondyloarthritis and Bekhterev's disease), lupus erythematosus, multiple sclerosis, macular degeneration, COPD, gout, fatty liver disorders, insulin resistance, neoplastic disorders and psoriasis.
    Type: Application
    Filed: April 5, 2019
    Publication date: August 1, 2019
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Ulrich BOTHE, Holger SIEBENEICHER, Nicole SCHMIDT, Reinhard NUBBEMEYER, Ulf BÖMER, Judith GÜNTHER, Holger STEUBER, Martin LANGE, Christian STEGMANN, Andreas SUTTER, Alexandra RAUSCH, Christian FRIEDRICH, Peter HAUFF
  • Publication number: 20190233396
    Abstract: Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Application
    Filed: September 13, 2018
    Publication date: August 1, 2019
    Inventors: Sunil Kumar KC, Chi Ching Mak, Brian Walter Eastman, Jianguo Cao, Venkataiah Bollu, Gopi Kumar Mittapalli, Chandramouli Chiruta
  • Publication number: 20190233397
    Abstract: Disclosed herein, inter alia, are compounds and methods of use thereof for the modulation of certain chemokine receptor activity.
    Type: Application
    Filed: January 24, 2019
    Publication date: August 1, 2019
    Inventors: Jeffrey J. Jackson, John Michael Ketcham, Akinori Okano, Maureen Kay Reilly, Omar Robles-Resendiz, Jacob Bradley Schwarz, Parcharee Tivitmahaisoon, David Juergen Wustrow, Ashkaan Younai, Mikhail Zibinsky
  • Publication number: 20190233398
    Abstract: The present application provides a hetero-cyclic compound capable of significantly enhancing lifespan, efficiency, electrochemical stability and thermal stability of an organic light emitting device, and an organic light emitting device containing the hetero-cyclic compound in an organic compound layer.
    Type: Application
    Filed: July 6, 2017
    Publication date: August 1, 2019
    Applicant: HEESUNG MATERIAL LTD.
    Inventors: Han-Kook OH, Jun-Tae MO, Yong-Geun JUNG, Won-Jang JEONG, Jin-Seok CHOI, Dae-Hyuk CHOI, Joo-Dong LEE
  • Publication number: 20190233399
    Abstract: Crystalline forms of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide (1) and its pharmaceutically acceptable salts and compositions thereof useful for the treatment or prevention of diseases or medical conditions mediated through mutated forms of epidermal growth factor receptor (EGFR), such as various cancers, are disclosed.
    Type: Application
    Filed: June 16, 2017
    Publication date: August 1, 2019
    Applicant: Beta Pharma, Inc.
    Inventors: Michael N. Greco, Michael J. Costanzo, Michael A. Green, Jirong Peng, Victoria Lynn Wilde, Don Zhang
  • Publication number: 20190233400
    Abstract: The present invention provides a novel crystalline form of Olaparib comprising Olaparib and benzyl alcohol, compositions thereof, and the use of this crystalline form in the treatment of cancers, such as germline BRCA-mutated (gBRCAm) advanced ovarian cancer.
    Type: Application
    Filed: January 30, 2019
    Publication date: August 1, 2019
    Inventors: Allan W. Rey, Fabio E. S. Souza, Annyt Bhattacharyya, Bahareh Khalili
  • Publication number: 20190233401
    Abstract: Methods for increasing biocidal activity of a substrate are provided. The methods can include attaching one or more ionic compounds to the substrate. The ionic compound can include a cationic moiety and at least one of an N-halamine precursor group or an N-halamine moiety.
    Type: Application
    Filed: February 1, 2019
    Publication date: August 1, 2019
    Inventor: Song Liu
  • Publication number: 20190233402
    Abstract: The invention relates to compounds of general formula (I): wherein R1, R2, R3, R10 and X? are as defined herein. The compounds are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions.
    Type: Application
    Filed: June 21, 2017
    Publication date: August 1, 2019
    Applicant: ENTERPRISE THERAPEUTICS LIMITED
    Inventors: Clive MCCARTHY, Jonathan David HARGRAVE, Duncan Alexander HAY, Thomas Beauregard SCHOFIELD, Naomi WENT
  • Publication number: 20190233403
    Abstract: The invention discloses polymorphic forms of a compound of formula I, pharmaceutical compositions containing same, preparation method therefor and use thereof. The compound of formula I of the present invention is as shown in formula I, of which the crystalline form can be crystalline form 1, crystalline form 2, crystalline form 3, crystalline form 5, crystalline form 6 or crystalline form 7. All the crystalline forms of the compound of formula I in the present invention have good crystalline stability and chemical stability and a decrease in purity of their main ingredient less than 2%. The preparation method of the present invention may be used to produce the various crystalline forms of the compound of formula I with high purity, and suitable for large scale production.
    Type: Application
    Filed: September 29, 2017
    Publication date: August 1, 2019
    Inventors: Congxin LIANG, Lihua XIE
  • Publication number: 20190233404
    Abstract: Provided herein are compounds having the structure of Formulas A-D and compositions thereof for use in the detection and quantification of viral neuraminidase. In particular, the compounds may be useful for the evaluation of viral strains and for vaccine evaluation.
    Type: Application
    Filed: January 25, 2019
    Publication date: August 1, 2019
    Inventors: Stephen G. Withers, Zhizeng Gao
  • Publication number: 20190233405
    Abstract: The present invention discloses a phenylate derivative, a preparation method therefor, and a pharmaceutical composition and uses thereof. Specifically, the invention relates to phenylate derivatives represented by formula (I), a pharmaceutically-acceptable salt thereof, a stereoisomer thereof, a preparation method therefor, a pharmaceutical composition containing the one or more compounds, and uses of the compounds in treating diseases related to PD-1/PD-L1 signal channels, such as cancers, infectious diseases and autoimmune diseases.
    Type: Application
    Filed: May 23, 2017
    Publication date: August 1, 2019
    Inventors: Zhiqiang Feng, Xiaoguang Chen, Yang Yang, Chuan Zhou, Fangfang Lai, Ming Ji, Xiaofeng Jin, Nina Xue, Yi Zheng, Hao Chen, Ling Li
  • Publication number: 20190233406
    Abstract: Disclosed are compounds of Formula A, or a salt thereof: wherein R1, R2, and E are defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same.
    Type: Application
    Filed: January 11, 2019
    Publication date: August 1, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Thomas J. Greshock, James Mulhearn, Junying Zheng, Ronald M. Kim, Ting Zhang, Anthony J. Roecker, Walter Won, Philippe Nantermet, Rajan Anand, Gang Zhou, Deping Wang, Liangqin Guo
  • Publication number: 20190233407
    Abstract: The present disclosure relates to the field of pharmaceutical synthesis, and more particularly, relates to a monocyclic ?-lactam-siderophore conjugate as well as a method for synthesizing same and its use in the treatment of bacterial infectious diseases. Provided are a monocyclic ?-lactam-siderophore conjugate represented by formula (I) as described herein, an optical isomer thereof or a pharmaceutically acceptable salt thereof, and a method for synthesizing same, and a use thereof in treating bacterial infectious diseases.
    Type: Application
    Filed: January 18, 2019
    Publication date: August 1, 2019
    Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Yushe Yang, Liang Tan, Qunhuan Kou
  • Publication number: 20190233408
    Abstract: The present disclosure relates to compounds and a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing the compounds, and processes for their preparation. The disclosure also relates to the use of the compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.
    Type: Application
    Filed: April 5, 2019
    Publication date: August 1, 2019
    Inventors: Andrew P. Crew, Yimin Qian, Hanqing Dong, Jing Wang, Craig M. Crews
  • Publication number: 20190233409
    Abstract: The present invention relates to compound of the formula 1.2, or a pharmaceutically acceptable salt, or hydrate thereof wherein R1 is C1-C5 alkyl; R2, is independently hydrogen, halogen, C1-C3 alkyl, CF3, OCF3 or OCH3; i is 1, 2,3, or 4; Ar is unsubstituted phenyl or substituted phenyl substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, a substituted amino group or trifluoromethyl; or Ar is a substituted or unsubstituted 6-membered aromatic heterocycle one or, with two nitrogen atoms in the heterocycle; excluding the compounds of the formulas A1-A4 The invention relates to the novel chemical compounds, methods for their preparation and use as antagonists of 5-HT6 receptors, simultaneously regulating homeostasis of calcium ions in cells.
    Type: Application
    Filed: April 12, 2017
    Publication date: August 1, 2019
    Inventors: Alexandre Vasilievich Ivachtchenko, Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk
  • Publication number: 20190233410
    Abstract: The invention relates to: a compound derived from 7,7?-diazaisoindigo; an organogel, formed by these compounds, having an aggregation-induced emission (AIE) in the red region of the visible spectrum (600-800 nm); and a xerogel produced by drying said organogel. Due to these properties, said organogel or xerogel can be applied to optoelectronic devices or fluorescent sensors.
    Type: Application
    Filed: July 6, 2016
    Publication date: August 1, 2019
    Inventor: Eva Maria Garcia Frutos
  • Publication number: 20190233411
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: January 28, 2019
    Publication date: August 1, 2019
    Inventors: Matthew Bleich, Jean-Damien Charrier, Huijun Dong, Steven Durrant, Meredith Suzanne Eno, Gorka Etxebarria I Jardi, Simon Everitt, Damien Fraysse, Ronald Knegtel, Igor Mochalkin, Kiri North, Filippos Porichis, Hui Qiu, Robert Pullin, Pierre-Henri Storck, Heather Clare Twin, Yufang Xiao
  • Publication number: 20190233412
    Abstract: The present disclosure relates to compounds capable of emitting delayed fluorescence and uses of these compounds in organic light-emitting diodes.
    Type: Application
    Filed: January 30, 2019
    Publication date: August 1, 2019
    Inventors: Shuo-Hsien Cheng, Yu Seok Yang, Yoshitake Suzuki, Hayato Kakizoe, Ayataka Endo, Jorge Aguilera-lparraguirre, Timothy D. Hirzel
  • Publication number: 20190233413
    Abstract: The specification relates to compounds of Formula (I): and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cell proliferative disorders.
    Type: Application
    Filed: January 31, 2019
    Publication date: August 1, 2019
    Inventors: Johannes Wilhelmus Maria Nissink, James Stewart Scott, Thomas Andrew Moss, Samantha Jayne Hughes, Bernard Christophe Barlaam, Bin Yang
  • Publication number: 20190233414
    Abstract: The invention provides novel chemical compounds useful for treating cancer, or a related disease or disorder thereof, and pharmaceutical composition and methods of preparation and use thereof.
    Type: Application
    Filed: October 10, 2017
    Publication date: August 1, 2019
    Inventors: Tinghu Zhang, Jianwei Che
  • Publication number: 20190233415
    Abstract: Novel MEK1, MEK2 and MEK1/2 inhibitors which have lower toxicity in long-term dosage, including the novel compound N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6, 8-dimethyl-2,4,7-trioxo-3,4,6, 7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]-phenyl}-cyclopropanecarboxamide dimethyl sulfoxide solvate according to formula 1:
    Type: Application
    Filed: December 12, 2016
    Publication date: August 1, 2019
    Inventors: Alexandre Vasilievich IVACHTCHENKO, Alexey Evgenievich REPIK, Vasily Gennadievich IGNATIEV, Mikhail Airatovich CHAFEEV
  • Publication number: 20190233416
    Abstract: The present disclosure relates to crystalline forms of venetoclax and process for their preparation. The present disclosure also relates to process for preparation of amorphous venetoclax.
    Type: Application
    Filed: October 13, 2017
    Publication date: August 1, 2019
    Applicant: Mylan Laboratories Limited
    Inventors: Ramakoteswara Rao Jetti, Hemant Malhari Mande, Anjaneyaraju Indukuri, Narasimha Murthy Pilli, Rajesh Joshi, Anil Kumar Tripathi, Chandrakant Chaudhri, Kiran Pokharkar, Nagaraju Gottumukkala
  • Publication number: 20190233417
    Abstract: Imidazo pyridine compounds, and pharmaceutically acceptable compositions thereof are useful as BTK inhibitors.
    Type: Application
    Filed: April 8, 2019
    Publication date: August 1, 2019
    Inventors: Pascale Gaillard, Jeyaprakashnarayanan Seenisamy, Lesley Liu-Bujalski, Richard D. Caldwell, Justin Potnick, Hui Qiu, Constantin Neagu, Reinaldo Jones, Annie Cho Won, Andreas Goutopoulos, Brian A. Sherer, Theresa L. Johnson, Anna Gardberg
  • Publication number: 20190233418
    Abstract: Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Application
    Filed: April 12, 2019
    Publication date: August 1, 2019
    Inventors: Erik VERNER, Kenneth Albert BRAMELD
  • Publication number: 20190233419
    Abstract: The present invention provides novel neuromodulatory compounds and compositions thereof The invention also relates to methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; as well as intermediates for the preparation compounds.
    Type: Application
    Filed: April 10, 2019
    Publication date: August 1, 2019
    Applicant: XOC Pharmaceuticals, Inc.
    Inventors: Thomas Armer, Scott Borland, Miguel Guzman
  • Publication number: 20190233420
    Abstract: The invention relates to activators of FXR useful in the treatment of autoimmune disorders, liver disease, intestinal disease, kidney disease, cancer, and other diseases in which FXR plays a role, having the Formula (I): (I), wherein L1, A, X1, X2, R1, R2, and R3 are described herein.
    Type: Application
    Filed: August 23, 2017
    Publication date: August 1, 2019
    Inventors: Jianhua Chao, Rakesh Jain, Lily Hu, Jason Gustaf Lewis, Helene Baribault, Jeremy Caldwell
  • Publication number: 20190233421
    Abstract: The present invention relates to processes for the preparation of N-protected (2S,5R)-6-hydroxy-7-oxo-N-piperidin-4-yl-1,6-diazabicyclo[3.2.1]octane-2-carboxamide intermediates. Such compounds have application in the preparation of beta-lactamase inhibitors such as 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamides and esters, in particular, the beta lactamase inhibitor, (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also encompasses intermediates useful in the disclosed processes and methods for their preparation.
    Type: Application
    Filed: September 14, 2017
    Publication date: August 1, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jianguo Yin, Zhijian Liu, Nobuyoshi Yasuda, Mark Weisel
  • Publication number: 20190233422
    Abstract: Generally, the present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.
    Type: Application
    Filed: March 2, 2016
    Publication date: August 1, 2019
    Inventor: Mustapha Haddach
  • Publication number: 20190233423
    Abstract: The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.
    Type: Application
    Filed: April 3, 2019
    Publication date: August 1, 2019
    Inventors: Peter SIEGER, Dirk KEMMER, Peter KOHLBAUER, Thomas NICOLA, Martin RENZ
  • Publication number: 20190233424
    Abstract: The present disclosure provides MAT2A inhibitor compounds that are useful as therapeutic agents for treating malignancies, and wherein the compounds conform to general formula (IA): wherein RA, RB, RC, RD, and RE are defined herein.
    Type: Application
    Filed: December 13, 2018
    Publication date: August 1, 2019
    Inventors: Zenon D. Konteatis, Zhihua Sui, Jeremy M. Travins, Zhixiong Ye
  • Publication number: 20190233425
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: January 28, 2019
    Publication date: August 1, 2019
    Inventors: Andrew Bayly, Matthew Bleich, Jean-Damien Charrier, James Dodd, Steven Durrant, Meredith Suzanne Eno, Gorka Etxebarria I Jardi, Simon Everitt, Damien Fraysse, Shazia Kelly, Ronald Knegtel, Igor Mochalkin, Michael Mortimore, Kiri North, Filippos Porichis, Robert Pullin, Alistair Rutherford, Pierre-Henri Storck, Heather Clare Twin, Yufang Xiao
  • Publication number: 20190233426
    Abstract: A compound of Formula (IA), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein A, R3, R4, R6, and R7 are as defined herein.
    Type: Application
    Filed: June 9, 2017
    Publication date: August 1, 2019
    Inventors: Ho Man CHAN, Xingnian Fu, Xiang-Ju Justin Gu, Ying HUANG, Ling LI, Yuan MI, Wei QI, Martin SENDZIK, Yongfeng SUN, Long WANG, Zhengtian YU, Hailong ZHANG, Ji Yue ZHANG, Man ZHANG, Qiong ZHANG, Kehao ZHAO
  • Publication number: 20190233427
    Abstract: The present invention relates to a compound of formula (I), wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy or lower alkoxy substituted by halogen; and R1 may be different if n is 2 or 3; R2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, CN, lower alkoxy or lower alkoxy substituted by halogen; X is CH or N; m is 1, 2 or 3; -( )m is —(CH2)m—; n is 1, 2 or 3; Ar is a five membered heteroaryl group, selected from formula (A), (B), (C), (D), (E) or (F), wherein R3 is hydrogen, methyl or chloro; R4 is hydrogen or methyl; R5 is F, Cl, CHF2 or CF3; or to pharmaceutically active acid addition salts thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
    Type: Application
    Filed: October 2, 2017
    Publication date: August 1, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Bjoern BARTELS, Roland JAKOB-ROETNE, Anja LIMBERG, Werner NEIDHART, Hasane RATNI, Michael REUTLINGER, Greta VASTAKAITE
  • Publication number: 20190233428
    Abstract: Novel polymorphs of rucaparib camsylate include Form alpha having XRPD peaks at diffraction angles (2?) of 6.14±0.2, 12.41±0.2, 15.34±0.2, 15.95±0.2, 16.36±0.2, 16.51±0.2 and 19.67±0.2, Form beta having XRPD peaks at diffraction angles (2?) of 6.86±0.2, 9.58±0.2, 12.75±0.2, 14.56±0.2, 15.05±0.2, 20.76±0.2 and 22.45±0.2, and Form gamma having XRPD peaks at diffraction angles (2?) of 9.5±0.2, 12.73±0.2, 14.77±0.2, 15.16±0.2, 20.62±0.2, 22.33±0.2, 22.63±0.2 and 27.29±0.2. Methods are disclosed for the preparation of such polymorphic forms and pharmaceutical compositions containing such polymorphic forms. A method is disclosed for preparing a highly pure Form B of rucaparib camsylate. Pharmaceutical compositions containing highly pure Form B prepared by the method are disclosed.
    Type: Application
    Filed: January 29, 2019
    Publication date: August 1, 2019
    Applicant: RK Pharma Solutions LLC
    Inventors: Ravishanker Kovi, Jayaraman Kannapan, Ananda Babu Thirunavakarasu, Hemant Mande
  • Publication number: 20190233429
    Abstract: A method of treating a disease condition in a mammal comprising administering a pharmacologically effective amount of a therapeutic, wherein the therapeutic includes a bioisosteres of caffeic acid. A pharmaceutical composition for treating a disease condition in a mammal comprising a first therapeutic that includes a bioisosteres of caffeic acid, wherein the condition may be breast cancer, and the pharmaceutical composition may include a second therapeutic for the disease condition that is not a bioisosteres of caffeic acid.
    Type: Application
    Filed: January 28, 2019
    Publication date: August 1, 2019
    Applicant: Board of Supervisors of Louisiana State University and Agricultural and Mechanical College
    Inventor: Brian Salvatore
  • Publication number: 20190233430
    Abstract: The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins in antibody-drug conjugates (ADCs). The present invention further relates to compositions including these cytotoxic compounds and ADCs, and methods for using these toxins and ADCs to treat pathological conditions including cancer.
    Type: Application
    Filed: April 5, 2019
    Publication date: August 1, 2019
    Applicant: pH Pharma Co., Ltd.
    Inventors: Vasu Jammalamadaka, Kimberly Ann Tipton, Sanjeev Satyal, Hoyoung Huh
  • Publication number: 20190233431
    Abstract: Compounds having the general formula I or III, and pharmaceutical compositions comprising the same. The compounds of the present invention are useful as selective mutant epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitor, and for the treatment of EGFR related diseases and disorders such as cancer.
    Type: Application
    Filed: December 1, 2016
    Publication date: August 1, 2019
    Inventors: Haixiao ZHAI, Fan WU
  • Publication number: 20190233432
    Abstract: The present invention discloses a compound comprising the formula: wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, or a compound of the formula wherein the S is replaced by CH2 or O, and optionally comprising a pharmaceutically acceptable salt or hydrate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt or hydrate thereof.
    Type: Application
    Filed: January 22, 2019
    Publication date: August 1, 2019
    Inventor: Aleem Gangjee
  • Publication number: 20190233433
    Abstract: The description relates to imide-based compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
    Type: Application
    Filed: January 26, 2019
    Publication date: August 1, 2019
    Inventors: Craig M. CREWS, George BURSLEM, Philipp M. CROMM, Saul JAIME-FIGUEROA, Momar TOURE
  • Publication number: 20190233434
    Abstract: Provided is a dihydropyrazole azepine compound serving as an Akt inhibitor; specifically disclosed is a compound as represented by formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 13, 2017
    Publication date: August 1, 2019
    Inventors: Lun LU, Zhibo ZHANG, Gang LI, Lihong HU, Charles Z. DING, Shuhui CHEN
  • Publication number: 20190233435
    Abstract: The present disclosure relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
    Type: Application
    Filed: February 1, 2019
    Publication date: August 1, 2019
    Inventors: Andrew P. Combs, Richard B. Sparks
  • Publication number: 20190233436
    Abstract: The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: April 11, 2019
    Publication date: August 1, 2019
    Inventors: Tatsuki KOIKE, Masato YOSHIKAWA, Haruhi ANDO, William John FARNABY
  • Publication number: 20190233437
    Abstract: This disclosure relates to polymorphs of (7S,13R)-11-fluoro-7,13-dimethyl-6,7,13,14-tetrahydro-1,15-ethenopyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one that are useful in the treatment of disease, such as cancer, in mammals. This disclosure also relates to compositions including such polymorphs, and to methods of using such compositions in the treatment of diseases, such as cancer, in mammals, especially in humans.
    Type: Application
    Filed: April 8, 2019
    Publication date: August 1, 2019
    Inventors: Jingrong J. Cui, Evan W. Rogers