Patents Issued in May 14, 2020
  • Publication number: 20200148646
    Abstract: The application is directed to compounds of Formula I or II: and pharmaceutically acceptable salts and solvates thereof, wherein R?, R?, R?? R1, R2, R3, R4, R4a, and R20 are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I or II and the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the modulation of one or more opioid receptors. Certain compounds of the invention are especially useful for treating pain.
    Type: Application
    Filed: January 10, 2020
    Publication date: May 14, 2020
    Inventors: Jeffrey Lockman, Laykea Tafesse, Jae Hyun Park, Mark A. Youngman
  • Publication number: 20200148647
    Abstract: Methods and intermediates for synthesizing triethylenetetramine and salts thereof, as well as novel triethylenetetramine salts and their crystal structure, and triethylenetetramine salts of high purity.
    Type: Application
    Filed: August 8, 2019
    Publication date: May 14, 2020
    Inventors: Marco Jonas, Irene Vaulont, Antonio Soi, Gunther Schmidt
  • Publication number: 20200148648
    Abstract: In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition.
    Type: Application
    Filed: January 10, 2020
    Publication date: May 14, 2020
    Inventors: Varghese JOHN, Dale E. BREDESEN
  • Publication number: 20200148649
    Abstract: Provided herein are 5-fluoro-4-imino-3-(alkyl/substituted alkyl)-1-(arylsulfonyl)-3,4-dihydropyrimidin-2(1H)-one and processes for their preparation which may include the use of an alkali carbonate and an alkylating agent
    Type: Application
    Filed: January 13, 2020
    Publication date: May 14, 2020
    Applicant: Adama Makhteshim Ltd.
    Inventors: Nakyen Choy, Ronald Ross, JR.
  • Publication number: 20200148650
    Abstract: The present disclosure provides substituted isoxazole carboxamide compounds having Formula (1) and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, A, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2 Compounds of the present disclosure are especially useful for treating cancer.
    Type: Application
    Filed: September 30, 2019
    Publication date: May 14, 2020
    Inventors: Megan Alene Cloonan Foley, Kevin Wayne KUNTZ, James Edward John MILLS, Lorna Helen MITCHELL, Michael John MUNCHHOF, Darren Martin HARVEY
  • Publication number: 20200148651
    Abstract: The present invention relates to novel oxazolidinones (Formula I): or a pharmaceutically acceptable salt having ring A characterized by N-containing monocyclic, bicyclic or spirocyclic substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.
    Type: Application
    Filed: January 13, 2020
    Publication date: May 14, 2020
    Inventors: Christopher B. COOPER, Haihong HUANG, Dongfeng ZHANG, Nader FOTOUHI, Takushi KANEKO
  • Publication number: 20200148652
    Abstract: The invention relates to novel compounds of the Formula (I) to a process for their preparation and to their use as medicaments, in particular as antiviral medicaments.
    Type: Application
    Filed: January 20, 2020
    Publication date: May 14, 2020
    Inventors: Gerald Kleymann, Christian Gege
  • Publication number: 20200148653
    Abstract: Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
    Type: Application
    Filed: January 10, 2020
    Publication date: May 14, 2020
    Inventors: Cheryl A. GRICE, Daniel J. BUZARD, Michael B. SHAGHAFI
  • Publication number: 20200148654
    Abstract: A method for preparing atetrafluoro-1,2-epoxypropane comprising reacting a 2-bromo-tetrafluoropropan-3-ol with an alkaline or alkaline earth metal hydroxide solution, a compound which is 2,3,3,3-tetrafluoro-1,2-epoxypropane, and partially fluorinated polyethers of formula [OCRR1CR2R3]n wherein n is from 5 to 100, R is F or H, R1 is CF3, R2 is F or H and R3 is H.
    Type: Application
    Filed: April 27, 2018
    Publication date: May 14, 2020
    Inventors: James Henry Murray, Andrew Paul Sharratt
  • Publication number: 20200148655
    Abstract: The invention relates to a process for the recovery and recycling of ethylene oxide (EO) after use in a sterilization process. The process involves the steps of introducing a mixed gas stream containing EO, nitrogen, oxygen, CO2, water, and a few other trace elements. The system includes integrated EO concentration sensors to determine the concentration of the EO in the gas stream. The system includes a series of compressors to pressurize the gas stream, and chillers or condensers to cool the gas stream to condense the EO out of the gas stream. The system includes temperature and pressure sensors to determine the conditions in the gas stream, and a control system that evaluates the temperature and pressure data and controls the compressors and chillers to achieve the properties to maximize the condensation of EO out of the gas stream.
    Type: Application
    Filed: January 17, 2020
    Publication date: May 14, 2020
    Inventors: Joseph D. Duff, Joseph E. Paganessi
  • Publication number: 20200148656
    Abstract: A method of treatment of an aqueous effluent stream obtained during production of furfural is disclosed. The aqueous effluent stream containing organic solvents, furfural, and water is subjected to azeotropic distillation to obtain a distillate stream and a treated effluent stream having lower BOD and COD values which can be further reduced by biomethanation.
    Type: Application
    Filed: June 1, 2017
    Publication date: May 14, 2020
    Inventors: Sunil Sadashiv DIVEKAR, Pramod Shankar KUMBHAR, Rahul Vasantrao BAGAL, Shreekant Uttam SATAV
  • Publication number: 20200148657
    Abstract: A process for preparing 5-hydroxymethylfurfural includes the steps of: subjecting a glucose-containing material to a catalytic reaction in the presence of an isomerase enzyme to form an aqueous saccharide solution containing fructose and glucose, converting the fructose into 5-hydroxymethylfurfural via a first dehydration reaction, and converting the glucose into 5-hydroxymethylfurfural via a second dehydration reaction.
    Type: Application
    Filed: May 15, 2019
    Publication date: May 14, 2020
    Applicant: FAR EASTERN NEW CENTURY CORPORATION
    Inventors: Ying-Jen Chen, Yi-Fen Yang, Fa-Chen Chi, Ruey-Fen Liao, Chien-Hung Chou
  • Publication number: 20200148658
    Abstract: An embodiment of the present invention provides a method of preparing 2,5-furandimethylcarboxylate (FDMC), including preparing 2,5-furandimethylcarboxylate (FDMC) by subjecting a reaction mixture including 5-hydroxymethylfurfural (HMF), air, and an alcohol solvent to oxidative esterification in the presence of a gold (Au)-nanoparticle-supported catalyst, in which the gold (Au)-nanoparticle-supported catalyst includes a support and gold (Au) nanoparticles supported on the support.
    Type: Application
    Filed: June 29, 2018
    Publication date: May 14, 2020
    Applicants: KOREA INSTITUTE OF INDUSTRIAL TECHNOLOGY, SK CHEMICALS CO., LTD.
    Inventors: Yong Jin KIM, Dinesh Kumar MISHRA, Jin Ku CHO, Yong Jin YI, Han Seok KIM, Jong Ryang KIM
  • Publication number: 20200148659
    Abstract: The inventive subject matter provides compounds, compositions and methods for lowering serum acid (sUA) for the treatment of gout, and having reduced liver toxicity, associated with CYP2C9 metabolic pathway.
    Type: Application
    Filed: November 14, 2019
    Publication date: May 14, 2020
    Inventors: Shunqi YAN, Li-Tain YEH, Robert ORR
  • Publication number: 20200148660
    Abstract: The present invention relates to a coumarin (keto) oxime ester compound of formula (I), wherein n and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification. The compound has strong ultraviolet absorption in the range of 300 to 450 nm. After absorbing light energy, it can quickly transfer energy and continuously initiate polymerization. It has obvious advantages in terms of photosensitivity and pattern integrity, and is very suitable for radiation curing by UV-LED light source. In addition, the compound of formula (I) also has good thermal stability. The present invention also relates to a method for preparing the compound of formula (I) and use of the compound. The compound is suitable as a photoinitiator in a UV-LED light curing system and is suitable for the radiation wavelength of UV-LED light curing.
    Type: Application
    Filed: May 29, 2018
    Publication date: May 14, 2020
    Applicant: HUBEI GURUN TECHNOLOGY CO. LTD
    Inventors: Yulian PANG, Yingquan ZOU, Shuheng FAN, Ming GAO, Yangyang XIN
  • Publication number: 20200148661
    Abstract: The present disclosure relates to salts of the compound: polymorphic forms thereof, methods for preparation and use thereof, and pharmaceutical compositions thereof.
    Type: Application
    Filed: June 18, 2019
    Publication date: May 14, 2020
    Applicant: Research Development Foundation
    Inventors: Michael O'NEILL, Barbara KIDON, Thomas ADKINS, Hongqiao WU, Emmanuel T. AKPORIAYE
  • Publication number: 20200148662
    Abstract: A stilbene derivative, which is a compound of the following general formula I or general formula II, or an acceptable salt formed by the compound of the general formula I or the general formula II and an inorganic or organic acid; wherein, in the general formula I or the general formula II, the atom represented by X is a hydrogen atom or a halogen atom; the substituent represented by R is C1-C6 alkyl, 1-6-membered heteroalkyl, C2-C4 alkenyl, C2-C4 alkynyl, C3-C6 cycloalkyl, substituted C3-C6 cycloalkyl, 3-6-membered heterocycloalkyl, substituted 3-6-membered heterocycloalkyl, 5-18-membered aryl, substituted 5-18-membered aryl, 5-18-membered heteroaryl, or substituted 5-18-membered heteroaryl.
    Type: Application
    Filed: October 26, 2016
    Publication date: May 14, 2020
    Applicant: BEIJING INSTITUTE OF TECHNOLOGY
    Inventors: Jianhua LIANG, Hong QING, Si WU, Sisi LIU, Nuomin LI, Liang YANG
  • Publication number: 20200148663
    Abstract: Substituted isoindolinones of Formula (I), methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat or ameliorate diseases, disorders, or conditions associated with protein malfunction, such as cancer, are provided.
    Type: Application
    Filed: November 12, 2019
    Publication date: May 14, 2020
    Inventors: Kyle W.H. Chan, Aparajita Hoskote Chourasia, Paul E. Erdman, Leah Fung, Imelda Lam, Frank Mercurio, Robert Sullivan, Eduardo Torres
  • Publication number: 20200148664
    Abstract: The invention provides certain nicotine salts, co-crystals, and salt co-crystals and provides novel polymorphic forms of certain nicotine salts. In particular, nicotine salts with mucic acid, 3,5-dihydroxybenzoic acid, and 2,3-dihydroxybenzoic acid, and crystalline polymorphic forms of nicotine 4-acetamidobenzoate, nicotine gentisate, and nicotine 1-hydroxy-2-naphthoate are described. The invention further provides methods of preparation and characterization of such nicotine salts, co-crystals, and salt co-crystals and polymorphic forms thereof. In addition, tobacco products, including smoking articles, smokeless tobacco products, and electronic smoking articles comprising nicotine salts, co-crystals, and/or salt co-crystals are also provided.
    Type: Application
    Filed: January 10, 2020
    Publication date: May 14, 2020
    Inventors: Gary M. Dull, Andrew Carr, Emma Sharp
  • Publication number: 20200148665
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
    Type: Application
    Filed: January 16, 2020
    Publication date: May 14, 2020
    Inventors: Yan Shi, Peter Tai Wah Cheng, Ying Wang, Jun Shi, Shiwei Tao, Jun Li, Lawrence J. Kennedy, Robert F. Kaltenbach, III, Hao Zhang, James R. Corte
  • Publication number: 20200148666
    Abstract: The present invention relates to novel organic dinitroxide biradical compounds and their use as polarizing agents, in particular, in the techniques of Nuclear Magnetic Resonance (NMR) of solids or liquid samples and medical imaging.
    Type: Application
    Filed: July 3, 2018
    Publication date: May 14, 2020
    Applicants: COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES, University of Iceland
    Inventors: Gaël De Paepe, Frédéric Mentink-Vigier, Snorri Sigurdsson, Anil Jagtap
  • Publication number: 20200148667
    Abstract: This application relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-? which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
    Type: Application
    Filed: November 12, 2019
    Publication date: May 14, 2020
    Inventors: Stacey Shepard, Andrew P. Combs
  • Publication number: 20200148668
    Abstract: Methods described herein enable the production of numerous molecular species through decarboxylative cross-coupling via use of photoredox and transition metal catalysts. For example, methods described herein enable the production of numerous molecular species through decarboxylative cross-coupling via use of photoredox and transition metal catalysts. A method described herein, in some embodiments, comprises providing a reaction mixture including a photoredox catalyst, a transition metal catalyst, a coupling partner and a substrate having a carboxyl group. The reaction mixture is irradiated with a radiation source resulting in cross-coupling of the substrate and coupling partner via a mechanism including decarboxylation, wherein the coupling partner is selected from the group consisting of a substituted aromatic compound and a substituted aliphatic compound.
    Type: Application
    Filed: January 9, 2020
    Publication date: May 14, 2020
    Inventors: DAVID W.C. MACMILLAN, Zhiwei Zuo
  • Publication number: 20200148669
    Abstract: Provided herein are substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
    Type: Application
    Filed: January 16, 2020
    Publication date: May 14, 2020
    Applicant: Pfizer Inc.
    Inventors: Matthew Dowling, Dilinie Fernando, Kentaro Futatsugi, Kim Huard, Thomas Victor Magee, Brian Raymer, Andre Shavnya, Aaron Smith, Benjamin Thuma, Andy Tsai, Meihua Tu
  • Publication number: 20200148670
    Abstract: The invention relates to a process for the preparation of lifitegrast (I) comprising a) reacting benzofuran-6-carboxylic in acid (II) with a non-chlorinated carboxyl activating agent; and b) reacting the activated compound obtained in step a) with compound (III) or a salt thereof to give lifitegrast. It also relates to a process for the purification of lifitegrast (I) by i) reacting lifitegrast with dicyclohexylamine to give the dicyclohexylamine salt of lifitegrast (Ia); ii) isolating the salt from the reaction medium; iii) converting the isolated salt into lifitegrast by treatment with an acid; and iv) isolating lifitegrast from the reaction medium. It also relates to the dicyclohexylamine salt of lifitegrast (Ia) and to a process for its preparation.
    Type: Application
    Filed: July 23, 2018
    Publication date: May 14, 2020
    Applicant: INTERQUIM, S.A.
    Inventors: Xavier BERZOSA RODRÍGUEZ, Francisco MARQUILLAS OLONDRIZ
  • Publication number: 20200148671
    Abstract: This application relates to compounds of the following Formula: or pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-? which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
    Type: Application
    Filed: November 12, 2019
    Publication date: May 14, 2020
    Inventors: Stacey Shepard, Yanran Ai, Andrew P. Combs, Artem Shvartsbart
  • Publication number: 20200148672
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein R1, L and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: April 5, 2018
    Publication date: May 14, 2020
    Inventors: Robert James PASTERIS, Srinivas CHITTABOINA, Travis Chandler MCMAHON, Balreddy KAMIREDDY, Ravisekhara Pochimireddy REDDY
  • Publication number: 20200148673
    Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating non-alcoholic steatohepatitis are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.
    Type: Application
    Filed: January 10, 2020
    Publication date: May 14, 2020
    Inventors: Adnan M.M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
  • Publication number: 20200148674
    Abstract: Disclosed herein are compounds of formula (I), and pharmaceutical compositions comprising the same. The compounds of formula (I) are neutrophilic inflammation inhibitors, thus, they are useful for treatment and/or prophylaxis of inflammatory diseases and/or disorders associated with abnormal activation of neutrophils, such as ARDS, ALI, COPD, lung fibrosis, chronic bronchitis, pulmonary emphysema, ?-1 anti-trypsin deficiency, cystic fibrosis, idiopathic pulmonary fibrosis, liver injury, steatohepatitis, liver fibrosis, damages caused by ischemia and reperfusion, myocardial infarction, shock, stroke, and organ transplantation, ulcerative cholitis, vasculitis, SLE, sepsis, SIRS, arthritis, psoriasis, atopic dermatitis, and inflammatory skin diseases.
    Type: Application
    Filed: November 9, 2018
    Publication date: May 14, 2020
    Applicant: Chang Gung University of Science and Technology
    Inventors: Tsong-Long HWANG, Yeh-Long CHEN, Cherng-Chyi TZENG, Chih-Hua TSENG
  • Publication number: 20200148675
    Abstract: There is described herein imidopiperidine compounds as inhibitors of human polynucleotide kinase phosphatase.
    Type: Application
    Filed: April 5, 2018
    Publication date: May 14, 2020
    Inventors: Dennis HALL, Michael WEINFELD, Sylvain BERNARD, Tristan VERDELET, Timothy MORGAN, Vikie LAMONTAGNE, Zahra SHIRE, Afsaneh LAVASANIFAR
  • Publication number: 20200148676
    Abstract: The present invention relates to novel 11-oxo-11H-pyrido[2,1-b]quinazoline-6-carboxamide derivatives as potent inhibitors of protein kinase, to pharmaceutical compositions containing them and to the use of said compounds for the manufacture of a drug for the treatment of diseases or pathological diseases that can be improved by inhibiting protein kinase.
    Type: Application
    Filed: May 31, 2018
    Publication date: May 14, 2020
    Inventors: Guido KURZ, Juan CAMACHO GÓMEZ
  • Publication number: 20200148677
    Abstract: The present disclosure relates to processes for the production of salts and crystalline forms of a compound having the formula.
    Type: Application
    Filed: July 24, 2018
    Publication date: May 14, 2020
    Inventors: Robert J. Duguid, John A. Grosso, Sergiy Krasutsky
  • Publication number: 20200148678
    Abstract: Provided herein are compounds and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of conditions associated with inhibition of HDAC (e.g., HDAC2).
    Type: Application
    Filed: November 12, 2019
    Publication date: May 14, 2020
    Inventors: Nathan Oliver Fuller, John A. Lowe, III
  • Publication number: 20200148679
    Abstract: The present invention relates to novel compounds that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).
    Type: Application
    Filed: January 9, 2020
    Publication date: May 14, 2020
    Inventors: Sreenivasachary NAMPALLY, Emanuele GABELLIERI, Jerome MOLETTE
  • Publication number: 20200148680
    Abstract: Disclosed herein are processes for preparing 8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one and FGFR inhibitor, as well as polymorphs and/or salt forms thereof.
    Type: Application
    Filed: January 17, 2020
    Publication date: May 14, 2020
    Inventors: Jiang ZHU, Mohammad MASJEDIZADEH
  • Publication number: 20200148681
    Abstract: There is a crystalline compound of (S)-ethyl 8-(2-amino-6-((R)-1-(5-chloro-[1,1?-biphenyl]-2-yl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)-2,8-diazaspiro[4.5]decane-3-carboxylate that exhibits an XRPD pattern having a characteristic peak at 19.05±0.20 (° 2?). There is also a pharmaceutical composition containing the compound. There is also a dosage form containing the crystalline compound and one or more pharmaceutically acceptable excipients. There is also a method for crystallizing/recrystallizing the compound. There is also a method for treating or preventing a disease with the compound.
    Type: Application
    Filed: November 14, 2019
    Publication date: May 14, 2020
    Applicant: Roivant Sciences GmbH
    Inventor: Daniel PATTERSON
  • Publication number: 20200148682
    Abstract: The present invention is directed to a compound of Formula (I) wherein A, X, Y, R1, R2, R3, R4, and n are as described herein. The present invention also relates to: 1) a method of treating cancer using a compound of Formula (I) and 2) a method of inhibiting pan-Akt in a cell or a tissue using a compound of Formula (I).
    Type: Application
    Filed: June 6, 2018
    Publication date: May 14, 2020
    Inventors: Yimon AYE, Xuyu LIU, Marcus J.C. LONG
  • Publication number: 20200148683
    Abstract: The present application relates to solid state forms of Lumateperone p-Tosylate and processes for preparation thereof. The present application provides amorphous Lumateperone p-tosylate and a solid dispersion comprising amorphous Lumateperone p-tosylate and one or more pharmaceutically acceptable polymers, their processes. The amorphous form and amorphous solid dispersions of the present application can be reproduced easily and is amenable for processing into a dosage form.
    Type: Application
    Filed: April 9, 2018
    Publication date: May 14, 2020
    Inventors: Vishweshwar PEDDY, Raja Sekhar VOGURI
  • Publication number: 20200148684
    Abstract: The present invention relates to novel quinazolinone derivatives inhibiting PI3K; a method for preparing the derivatives; and a pharmaceutical composition for treating hematologic neoplasms or liver diseases, containing the quinazolinone derivatives, wherein the novel quinazolinone derivatives according to the present invention have a beneficial effect in the treatment of hematologic neoplasms or liver diseases. Particularly, the quinazolinone derivatives inhibit PI3K? with high selectivity compared to that of a conventional anticancer drug of PI3K? inhibitors, thereby significantly reducing immunotoxicity, or simultaneously inhibit PI3K? and PI3K?, thereby enabling the treatment of autoimmune diseases, and anticancer therapy for blood cancer and the like. These targeted drugs have an advantage of enabling the problem of side effects of a conventional highly toxic anticancer therapy to be resolved.
    Type: Application
    Filed: January 20, 2020
    Publication date: May 14, 2020
    Applicant: BIOWAY., INC
    Inventors: Jongwoo KIM, Chiwoo LEE, Suji HONG
  • Publication number: 20200148685
    Abstract: A chemical entity of Formula (I), wherein V, W, Y, and Z, have any of the values described herein, and compositions comprising such chemical entities, methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques, radioactive treatments; modulating and treating disorders mediated by PDE2 activity; treating neurological disorders, CNS disorders, dementia, cognitive disorders, neurodegenerative diseases, and trauma-dependent losses of function, enhancing the efficiency of cognitive and motor training, including in stroke or TBI rehabilitation; and treating peripheral disorders, including hematological, cardiovascular, gastroenterological, dermatoiogical, inflammatory, and pain disorders.
    Type: Application
    Filed: December 22, 2017
    Publication date: May 14, 2020
    Inventors: Laurent Gomez, William Francois Vernier
  • Publication number: 20200148686
    Abstract: The invention relates to novel compounds of the formula (I) in which R1, Ra, Rb, Rc, R3, R4, A1, A2 and n have the definitions given above, to agrochemical formulations comprising the compounds of formula (I) and to their use as acaricides and/or insecticides for controlling animal pests, particularly arthropods and especially insects and arachnids.
    Type: Application
    Filed: April 25, 2018
    Publication date: May 14, 2020
    Inventors: Marc MOSRIN, Ruediger FISCHER, Dominik HAGER, Laura HOFFMEISTER, Nina KAUSCH-BUSIES, David WILCKE, Matthieu WILLOT, Kerstin ILG, Daniela PORTZ, Ulrich GOERGENS, Sascha EILMUS, Andreas TURBERG
  • Publication number: 20200148687
    Abstract: Compounds of formula: are useful as antitumor agents. In these compounds, R10 is (a) (C1-C10) hydrocarbyl, (C1-C10)halohydrocarbyl, (C1-C6)hydroxyalkyl, or or R10 is (b) in which Q and A are linkers and Ar is optionally substituted monocyclic or bicyclic aryl or heteroaryl.
    Type: Application
    Filed: May 18, 2018
    Publication date: May 14, 2020
    Applicant: The Rockefeller University
    Inventors: Tarun M. KAPOOR, Moriteru ASANO, Kazuyoshi ASO, Michael A. FOLEY, Yoshiyuki FUKASE, Hideki FURUKAWA, Yashuhiro HIRATA, Sachie TAKASHIMA, Tomohiro OKAWA, Yuta TANAKA, Yayoi YOSHITOMI
  • Publication number: 20200148688
    Abstract: The present disclosure relates to compounds that bind to at least one of ACAT1/2 and OXCT1/2 and inhibit mitochondrial ATP production, referred to herein as mitoketoscins. Methods of screening compounds for mitochondrial inhibition and anti-cancer properties are disclosed. Also described are methods of using mitoketoscins to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitoketoscins to provide anti-aging benefits. Specific mitoketoscin compounds are also disclosed.
    Type: Application
    Filed: June 25, 2018
    Publication date: May 14, 2020
    Inventors: Michael P. LISANTI, Federica SOTGIA
  • Publication number: 20200148689
    Abstract: This application relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-? which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
    Type: Application
    Filed: November 12, 2019
    Publication date: May 14, 2020
    Inventors: Stacey Shepard, Yanran Ai, Andrew P. Combs, Nikoo Falahatpisheh, Lixin Shao, Artem Shvartsbart
  • Publication number: 20200148690
    Abstract: The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
    Type: Application
    Filed: January 10, 2020
    Publication date: May 14, 2020
    Inventors: Zhiwei WANG, Yunhang GUO
  • Publication number: 20200148691
    Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Application
    Filed: January 15, 2020
    Publication date: May 14, 2020
    Inventors: Norbert Purro, Mark S. Smyth, Erick Goldman, David D. Wirth
  • Publication number: 20200148692
    Abstract: The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.
    Type: Application
    Filed: January 16, 2020
    Publication date: May 14, 2020
    Inventors: Hong Lin, Juan Luengo, Rupa Shetty, Michael Hawkins
  • Publication number: 20200148693
    Abstract: The present invention describes novel compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the invention have activity as prostaglandin EP4 receptor antagonists, and are useful in the treatment or alleviation of pain and inflammation and other inflammation-associated disorders, such as arthritis, treating or preventing disorders or medical conditions selected from pain, inflammatory diseases and the like. Also described herein are methods of treating pain by administering the compounds of the invention, which are EP4 receptor antagonists.
    Type: Application
    Filed: January 17, 2020
    Publication date: May 14, 2020
    Inventors: Jason D. SPEAKE, Bharathi PANDI, Cyprian O. OGBU, Brent Christopher BECK
  • Publication number: 20200148694
    Abstract: There are provided, prodrugs of opioid and other controlled substance, having enhanced physical and chemical stability to resist tampering and to make long-acting release formulations, and pharmaceutically accepted salts and solvates thereof. There are also provided methods of using the disclosed compounds as abuse deterrent products.
    Type: Application
    Filed: July 19, 2018
    Publication date: May 14, 2020
    Inventors: Hui OUYANG, Yong QIU
  • Publication number: 20200148695
    Abstract: Disclosed are a class of coumarin-like cyclic compounds as MEK inhibitors and pharmaceutical compositions comprising the compounds, and the use of same in the preparation of a drug for treating MEK-related diseases. Particularly disclosed are compounds as shown in formula (I) and pharmaceutically acceptable salts thereof or tautomers thereof.
    Type: Application
    Filed: June 22, 2018
    Publication date: May 14, 2020
    Applicants: CSTONE PHARMACEUTICALS, CSTONE PHARMACEUTICAL (SUZHOU) CO., LTD., CSTONE PHARMACEUTICALS (SHANGHAI) CO., LTD.
    Inventors: Qinghua MAO, Chengde WU, Yong HUANG, Zhen GONG, Jian LI, Shuhui CHEN