Patents Issued in May 28, 2020
  • PROCESS TO EXTRACT AND PURIFY DELTA-9-TETRAHYDROCANNABINOL
    Publication number: 20200165219
    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: January 28, 2020
    Publication date: May 28, 2020
    Inventors: Lekhram CHANGOER, Cornelis Herman Michel VAN DER LOO, Erik KELLER
  • OXIME COMPOUNDS AS AGONISTS OF THE MUSCARINIC M1 AND/OR M4 RECEPTOR
    Publication number: 20200165220
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula (I) where p; q; X1; X2; Y; R1; R2; R3; R4; R5 and R6 are as defined herein.
    Type: Application
    Filed: November 2, 2016
    Publication date: May 28, 2020
    Inventors: Giles Albert Brown, Benjamin Gerald Tehan
  • CRYSTALLINE FORM OF N-[1-(5-CYANO-PYRIDIN-2-YLMETHYL)-1 H-PYRAZOL-3-YL]-2-[4-(1-TRIFLUO-ROMETHYL-CYCLOPROPYL)-PHENYL]-ACETAMIDE
    Publication number: 20200165221
    Abstract: The present invention relates to crystalline forms of N-[1-(5-cyano-pyridin-2-ylmethyl)-1H-pyrazol-3-yl]-2-[4-(1-trifluoromethyl-cyclopropyl)-phenyl]-acetamide, pharmaceutical compositions comprising said crystalline forms and their use as T-type calcium channel blockers in the treatment or prevention of diseases or disorders where T-type calcium channels are involved.
    Type: Application
    Filed: July 4, 2018
    Publication date: May 28, 2020
    Inventors: Bibia HEIDMANN, Markus VON RAUMER
  • INDOLE CARBOXAMIDE COMPOUNDS
    Publication number: 20200165222
    Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR4 or N; R1, R2, R3, R4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Application
    Filed: January 28, 2020
    Publication date: May 28, 2020
    Inventors: Qingjie LIU, Scott Hunter Watterson, John E. Macor, Khehyong Ngu, Saleem Ahmad
  • Diamide Compounds Having Muscarinic Receptor Antagonist and Beta2 Adrenergic Receptor Agonist Activity
    Publication number: 20200165223
    Abstract: The invention relates to a pharmaceutical composition comprising an isotonic aqueous solution comprising a compound of formula I: or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 28, 2020
    Publication date: May 28, 2020
    Inventors: Adam D. HUGHES, Daniel BYUN, Yan CHEN, Melissa FLEURY, John R. JACOBSEN, Eric STANGELAND, Richard D. WILSON, Rose YEN
  • METHODS AND COMPOSITIONS FOR INHIBITING THE INTERACTION OF MENIN WITH MLL PROTEINS
    Publication number: 20200165224
    Abstract: The present disclosure provides compositions and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The compositions and methods of use are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.
    Type: Application
    Filed: June 7, 2018
    Publication date: May 28, 2020
    Inventors: Liansheng LI, Tao WU, Jun FENG, Pingda REN, Yi LIU, Jolanta GREMBECKA, Tomasz CIERPICKI, Dmitry BORKIN, Jonathan POLLOCK
  • BACE1 INHIBITORS FOR TREATMENT OF ALZHEIMER'S DISEASE
    Publication number: 20200165225
    Abstract: Compounds, pharmaceutical compositions containing the same useful in the treatment of Alzheimer's disease are disclosed. Methods of preparing the compounds and compositions and use thereof are also disclosed.
    Type: Application
    Filed: May 8, 2018
    Publication date: May 28, 2020
    Applicant: NantBio, Inc.
    Inventors: Chunlin TAO, Tulay POLAT, Chengzhi YU
  • HINDERED AMINE LIGHT STABILIZERS
    Publication number: 20200165226
    Abstract: A compound of formula (I) wherein R1 and R2 independently of one another are hydrogen, C1-C22alkyl, —O—, —OH, —CH2CN, C1-C18alkoxy, C2-C18alkoxy substituted by —OH; C5-C12cycloalkoxy, C3-C6alkenyl, C3-C6alkenyloxy, C7-C9phenylalkyl unsubstituted or substituted on the phenyl by 1, 2 or 3 C1-C4alkyl; or C1-C8acyl; and R3 and R4 independently of one another are C1-C22alkyl or a group of the formula (Ia) wherein R0 has one of the meanings of R1 and R2.
    Type: Application
    Filed: January 30, 2020
    Publication date: May 28, 2020
    Applicant: BASF SE
    Inventors: Cornelia Schleth, Liane Schulz, Bruno Rotzinger, Bjoern Ludolph, Manuele Vitali
  • 2,4-BIS(NITROGEN-CONTAINING GROUP)-SUBSTITUTED PYRIMIDINE COMPOUND, PREPARATION METHOD AND USE THEREOF
    Publication number: 20200165227
    Abstract: Provided are a 2, 4-di-(nitrogen containing group) substituted pyrimidine compound represented by a general formula (I), a pharmaceutically acceptable salt and a stereoisomer thereof, a preparation method thereof, and a use thereof in preparation of anti-tumor drugs. The compound having a structural feature shown in the general formula (I) can selectively suppress activity of mutant epidermal growth factor receptors (EGFR), including single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. The compound has a weak suppression effect on wild-type EFGR and a very high selectivity, and thus it has a potential to be used in preparation of drugs for treating EGFR mutant tumors, especially non-small cell lung cancer (NSCLC) comprising a T790M EGFR mutation.
    Type: Application
    Filed: July 26, 2016
    Publication date: May 28, 2020
    Applicant: GUANGZHOU BEBETTER MEDICINE TECHNOLOGY CO., LTD.
    Inventors: Xiong CAI, Changgeng QIAN, Yunwo WENG, Bin LIU, Yanyan WANG, Mingsheng LIN, Junqi LI, Yuanhui QING, Huajin YOU, Shiqing ZHOU, Weicai XUE
  • A METHOD FOR PRODUCING POTASSIUM 1,1 -DINITRAMINO-5,5-BISTETRAZOLATE AND EXPLOSIVE COMPOSITIONS COMPRISING SAID SALT
    Publication number: 20200165228
    Abstract: A method of producing K2DNABT wherein a biztetrazole intermediate is nitrated using a nitrating agent selected from the following: dinitronium disulphate; a mixture of nitric acid and sulfuric acid; a mixture of nitric acid and phosphorous pentoxide; and nitric acid with acetic anhydride.
    Type: Application
    Filed: May 10, 2018
    Publication date: May 28, 2020
    Applicant: DETNET SOUTH AFRICA (PTY) LTD
    Inventors: Elmar Lennox Muller, Thomas M. Klapotke, Jorg Stierstorfer, Marc F. Bolter, Maurus Volkl
  • POLYFLUORO-SUBSTITUTED AROMATIC HETEROCYCLIC DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND APPLICATIONS THEREOF
    Publication number: 20200165229
    Abstract: A polyfluoro-substituted aromatic heterocyclic derivative having the structure as represented by formula I or formula I?, wherein at least one of Ri and R2 is a fluorine atom, and at least two substituents of Rc, Rd, Re, and Rf are fluorine atoms; and an optical isomer of the derivative, or a pharmaceutically acceptable salt or solvate of the same, or a pharmaceutically acceptable salt or solvate of the optical isomer of the same. A composition containing the polyfluoro-substituted aromatic heterocyclic derivative and an application of the composition in preparing an anti-tumour medicament. The compound provides significant inhibitory effects with respect to Aktl and demonstrates strong proliferation inhibitory activity with respect to tumour cell lines such as an ovarian cancer cell line, a colon cancer cell line, and a prostate cancer cell line.
    Type: Application
    Filed: January 19, 2018
    Publication date: May 28, 2020
    Inventors: Xiaowu DONG, Bo YANG, Yongzhou HU, Qiaojun HE, Qinjie WENG, Wenhu ZHAN, Tao LIU
  • 3,4,5-Trisubstituted-1,2,4-Triazoles and 3,4,5-Trisubstituted-3-Thio-1,2,4-Triazoles and Uses Thereof
    Publication number: 20200165230
    Abstract: The present disclosure describes novel compounds that are somatostatin receptor type 4 agonists.
    Type: Application
    Filed: May 11, 2018
    Publication date: May 28, 2020
    Inventors: Kenneth A. Witt, Albert M. Crider, William Neumann, Audrey Hospital, Karin Sandoval, Maria Kontoyianni
  • KRAS G12C INHIBITORS AND METHODS OF USING THE SAME
    Publication number: 20200165231
    Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
    Type: Application
    Filed: November 18, 2019
    Publication date: May 28, 2020
    Inventors: Youngsook SHIN, Victor J. CEE, Christopher M. TEGLEY, Brian Alan LANMAN, Ryan Paul WURZ, Kevin C. YANG, Vu Van MA, Daniel ERLANSON, Joon Won JEONG, Raymond V. FUCINI, Jeffrey IWIG
  • PYRIDINE QUINOLINE COMPOUNDS AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION
    Publication number: 20200165232
    Abstract: Pyridine quinoline compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease states associated with glutamate dysfunction.
    Type: Application
    Filed: June 28, 2018
    Publication date: May 28, 2020
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Andrew S. Felts, Colleen M. Niswender, Rory A. Capstick, Paul K. Spearing, Sean R. Bollinger
  • LDHA ACTIVITY INHIBITORS
    Publication number: 20200165233
    Abstract: The invention provides compounds of formula (I), stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof: (I) wherein A1 to A6 and R1 to R4 are as defined herein. Such compounds are suitable for use in the treatment or prevention of diseases or conditions which are mediated by the activation of lactate dehydrogenase A (LDHA), for example cancer.
    Type: Application
    Filed: May 16, 2018
    Publication date: May 28, 2020
    Inventors: Jo KLAVENESS, Bora SIENG, Steffi LUNDVALL, Claudia Alejandra BØEN, Kathrin HNIDA
  • COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE COMPRISING SAME
    Publication number: 20200165234
    Abstract: Provided is a compound of Formula 1: and an organic light emitting device including the same.
    Type: Application
    Filed: November 19, 2018
    Publication date: May 28, 2020
    Inventors: Minjun KIM, Kongkyeom KIM, Hyoung Seok KIM, Min Woo LEE
  • NADPH OXIDASE 4 INHIBITORS
    Publication number: 20200165235
    Abstract: The invention relates to 2,5-disubstituted benzoxazole and benzothiazole derivatives of Formula (I) wherein L, X, Y, and ring (A) are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds may be useful for the prevention or treatment of diseases or disorders associated with impaired reactive oxygen species (ROS) production, and/or for the prevention or treatment of various fibrotic diseases.
    Type: Application
    Filed: January 30, 2020
    Publication date: May 28, 2020
    Applicant: ACTELION PHARMACEUTICALS LTD
    Inventors: Hamed Aissaoui, Martin Bolli, Christoph Boss, Sylvia Richard-Bildstein, Patrick Sieber
  • IMPROVED PROCESS FOR PREPARING AMINOPYRIMIDINE DERIVATIVES
    Publication number: 20200165236
    Abstract: The present invention provides an improved process for preparing an aminopyrimidine derivative or pharmaceutically acceptable salt thereof having a selective inhibitory activity against protein kinases, especially against the protein kinases for mutant epidermal growth factor receptors. And also, the present invention provides novel intermediates useful for said process and processes for preparing the same.
    Type: Application
    Filed: July 25, 2018
    Publication date: May 28, 2020
    Inventors: Sang-Ho OH, Ja-Heouk KHOO, Jong-Chul LIM, Seong-Ran LEE, Hyun JU, Woo-Seob SHIN, Dae-Gyu PARK, Su-Min PARK, Yoon-Ah HWANG
  • FIVE MEMBERED-AMINOHETEROCYCLE AND 5,6-or 6,6-MEMBERED BICYCLIC AMINOHETEROCYCLIC INHIBITORS OF ROCK FOR THE TREATMENT OF HEART FAILURE
    Publication number: 20200165237
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
    Type: Application
    Filed: July 11, 2018
    Publication date: May 28, 2020
    Inventors: Donald J. P. Pinto, Tarun Kumar Maishal
  • Heterocyclic Inhibitors of Glutaminase
    Publication number: 20200165238
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Application
    Filed: December 6, 2019
    Publication date: May 28, 2020
    Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric B. Sjogren
  • PROTEIN KINASE INHIBITORS, PREPARATION METHOD AND MEDICAL USE THEREOF
    Publication number: 20200165239
    Abstract: The embodiments disclosed herein provide compounds as shown in formula I or a tautomer, a mesomer, a racemate, an enantiomer, a diastereomer, a deuterated compound, a prodrug or a mixture thereof, or a pharmaceutically acceptable salt or solvate of the compounds as shown in formula I or a tautomer, a mesomer, a racemate, an enantiomer, a diastereomer, a deuterated compound, a prodrug or a mixture thereof, wherein R1 to R7 are as defined in the description. This application also provides a preparation method and a medical use of the compounds. The compounds of this disclosure have an activity superior or equivalent to the candidate drug LY2835219 currently under phase III clinical trial, and some of the compounds exhibit better selectivity. Moreover, the preferred compounds exhibit good absorption and good blood-brain distribution when administered orally.
    Type: Application
    Filed: November 28, 2016
    Publication date: May 28, 2020
    Inventors: Lei Yin, Wenjian Liu, Heng Li, Dianxi Zhu
  • BENZOQUINOLONE INHIBITORS OF VMAT2
    Publication number: 20200165240
    Abstract: The present invention relates to new benzoquinolone inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: June 27, 2019
    Publication date: May 28, 2020
    Inventors: Andreas Sommer, Chengzhi Zhang
  • INHIBITOR COMPOUNDS
    Publication number: 20200165241
    Abstract: The present invention relates to compounds of formula I wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
    Type: Application
    Filed: October 10, 2019
    Publication date: May 28, 2020
    Inventors: Swen Hoelder, Julian Blagg, Savade Solanki, Hannah Woodward, Sebastien Gaston Andre Naud, Vassilios Bavetsias, Peter Sheldrake, Paolo Innocenti, Kwai-Ming J. Cheung, Butrus Atrash
  • INDOLIZINE DERIVATIVES AND THEIR APPLICATION IN MEDICINE
    Publication number: 20200165242
    Abstract: This invention relates to indolizine derivatives and their use in medicine. In particular, the present invention discloses novel substituted indolizine derivatives of formula I, or an isotopically labeled compound thereof, or an optical isomer thereof, a geometric isomer thereof, a tautomer thereof or a mixture of various isomers, or a pharmaceutically acceptable salt thereof, or a prodrug thereof. The invention also relates to the use of these compounds in medicine.
    Type: Application
    Filed: May 8, 2018
    Publication date: May 28, 2020
    Inventors: Dong LIU, Dongdong CHEN, Biao DENG, Xiangyun TU, Zinan FANG, Haohao WU, Danyan GU
  • PYRROLOPYRIDINE-ANILINE COMPOUNDS FOR TREATMENT OF DERMAL DISORDERS
    Publication number: 20200165243
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions in treating diseases or disorders in a subject where the subject is in need of an inhibitor of MEK where the Compound is according to Formula (I), where X1, R1, R2, R2a, R3, R3a and R3b are as described herein.
    Type: Application
    Filed: May 18, 2018
    Publication date: May 28, 2020
    Inventors: John Kincaid, Matthew Duncton
  • HETEROCYCLIC COMPOUND AND HARMFUL-ARTHROPOD CONTROL AGENT CONTAINING SAME
    Publication number: 20200165244
    Abstract: A compound represented by formula (I), which is highly effective in controlling harmful arthropods, an intermediate thereof and a production method thereof are described. In formula (I), A1 represents CH or a nitrogen atom; R1 represents a C1-C6 alkyl group optionally having one or more halogen atoms; R5 represents CF3, C2F5, or S(O)mCF3; Q represents NR2C(O)OR3 or N?CR4R6; R2 represents a hydrogen atom or the like; R3 represents a C1-C6 alkyl group optionally having one or more halogen atoms or the like; R4 represents a hydrogen atom or the like; R6 represents a phenyl group optionally having one or more substituents selected from group D, or the like; and n and m each independently are 0, 1, or 2. Group D: a group consisting of C1-C6 alkyl groups optionally having one or more halogen atoms and C1-C6 alkoxy groups optionally having one or more halogen atoms or the like.
    Type: Application
    Filed: July 12, 2018
    Publication date: May 28, 2020
    Inventors: Takayuki SHIODA, Daisuke OOHIRA, Kaori IKARI, Natsuru HIRAGURI
  • INHIBITORS OF ROR GAMMA
    Publication number: 20200165245
    Abstract: The present disclosure relates to salts and crystalline forms of a compound having the formula (I): Also described are processes for the production of the salts and crystalline forms described herein.
    Type: Application
    Filed: July 24, 2018
    Publication date: May 28, 2020
    Inventors: Chaoyi Deng, Jun He, Bo Xu
  • SUBSTITUTED PENTA-FUSED HEXA-HETEROCYCLIC COMPOUNDS, PREPARATION METHOD THEREFOR, DRUG COMBINATION AND USE THEREOF
    Publication number: 20200165246
    Abstract: A type of substituted penta-fused hexa-heterocyclic compounds having selective inhibition for PIKfyve kinase, a pharmaceutically acceptable salt and pharmaceutically acceptable solvate thereof, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for preventing or treating a disease associated with PIKfyve in vivo, in particular in the manufacture of a medicament for preventing or treating tumor growth and metastasis.
    Type: Application
    Filed: August 3, 2018
    Publication date: May 28, 2020
    Applicant: Xiamen University
    Inventors: Xianming Deng, Wei Huang, Xihuan Sun, Ting Zhang, Zhixiang He, Yan Liu, Xinrui Wu, Baoding Zhang, Xiaoyang Li, Jingfang Zhang, Yun Chen, Li Li, Qingyan Xu, Zhiyu Hu
  • TETRAHYDROPYRAN (THP)-SUBSTITUTED BICYCLIC-PYRIMIDINEDIONE COMPOUNDS
    Publication number: 20200165247
    Abstract: The present disclosure provides novel tetrahydropyran (THP)-substituted bicyclic pyrimidinedione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM), conditions associated with left ventricular hypertrophy, conditions associated with diastolic dysfunction, and/or symptoms associated thereof. The synthesis and characterization of the compounds is described, as well as methods for treating HCM and other forms of heart disease.
    Type: Application
    Filed: October 28, 2019
    Publication date: May 28, 2020
    Inventors: Mark Grillo, Brian Kane, Johan Oslob, Min Zhong, Fabienne Thompson
  • IMIDAZOPYRIDINE DERIVATIVES
    Publication number: 20200165248
    Abstract: The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.
    Type: Application
    Filed: October 29, 2019
    Publication date: May 28, 2020
    Inventors: Peter A. Blomgren, Taryn Campbell, Jayaraman Chandrasekhar, Christopher T. Clark, Julian A. Codelli, Kevin S. Currie, Jeffrey E. Kropf, Yasamin Moazami, Nicole Nava, Leena Patel, Stephane Perreault, Jason K. Perry, Kassandra F. Sedillo, Natalie Seeger, Kirk L. Stevens, Jennifer Anne Treiberg, Suet C. Yeung, Zhongdong Zhao
  • FUNCTIONALIZED HETEROCYCLES AS ANTIVIRAL AGENTS
    Publication number: 20200165249
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: November 20, 2019
    Publication date: May 28, 2020
    Inventors: Joseph Panarese, Dexter Davis, Samuel Bartlet, Katherine Chong, Nathaniel Kenton, Yat Sun Or
  • Small Molecule Inhibitors of the JAK Family of Kinases
    Publication number: 20200165250
    Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK.
    Type: Application
    Filed: January 29, 2020
    Publication date: May 28, 2020
    Inventors: Philippe Fernandes, Paul J. Krawczuk, Mark S. Tichenor
  • COMPOUNDS AND METHODS FOR TREATING BACTERIAL INFECTIONS
    Publication number: 20200165251
    Abstract: Provided herein are antibacterial compounds represented by Formula I, or a pharmaceutically acceptable salt thereof, wherein X, Y, R4, R5, and R6 are as defined herein. Also provided are pharmaceutical compositions comprising the compounds of Formula I.
    Type: Application
    Filed: May 8, 2018
    Publication date: May 28, 2020
    Inventors: Janelle Comita-Prevoir, Thomas Francois Durand-Reville, Satenig Guler, Jan Romero, Mark Sylvester, Ruben Tommasi, Camilo Velez-Vega, Xiaoyun Wu, Jing Zhang
  • HEXACYCLIC HETEROAROMATIC COMPOUNDS FOR ELECTRONIC DEVICES
    Publication number: 20200165252
    Abstract: The invention relates to heteroaromatic compounds, particularly for use in electronic devices. The invention further relates to a method for producing the compounds according to the invention and to electronic devices containing same.
    Type: Application
    Filed: May 18, 2018
    Publication date: May 28, 2020
    Inventors: Amir PARHAM, Jonas KROEBER, Dominik JOOSTEN, Aurélie LUDEMANN, Tobias GROSSMANN
  • Phthalazine Derivatives, Preparation Method, Pharmaceutical Composition and Usage Thereof
    Publication number: 20200165253
    Abstract: The present invention provides a compound of formula I, a cis-trans isomer, an enantiomer, a diastereoisomer, a racemate, a solvate, a hydrate, or a pharmaceutical acceptable salt and ester thereof, a preparation method for preparing the same, a pharmaceutical composition comprising the same and a use of the compound as an ?5-GABAA receptor regulator, wherein T, Z, A and Y are as defined in the description.
    Type: Application
    Filed: December 8, 2016
    Publication date: May 28, 2020
    Inventors: Shuai LI, Yong SUN
  • AZAARYL DERIVATIVE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF FOR USE IN PHARMACY
    Publication number: 20200165254
    Abstract: An azaaryl derivative with the structure of formula (I), a preparation method therefor and a pharmaceutical use thereof are disclosed in this application. The series of compounds of the this application can be widely applied in the preparation of drugs for treating cancer, tumor, autoimmune disease, metabolic disease or metastatic disease, particularly for treating ovarian cancer, pancreatic cancer, prostate cancer, breast cancer, cervical cancer, glioblastoma, multiple myeloma, metabolic disease, neurodegenerative disease, primary site tumor metastasis or osseous metastasis cancer, and are expected to be developed into a new generation of CSF-1R inhibitor drugs.
    Type: Application
    Filed: May 22, 2018
    Publication date: May 28, 2020
    Inventors: Baowei ZHAO, Mingming ZHANG, Hongping YU, Zhui CHEN, Yaochang XU
  • Bicyclic Pesticidal Compounds
    Publication number: 20200165255
    Abstract: The present invention relates to compounds of formula I, wherein the variables are defined as given in the description and claims. The invention further relates to uses, processes and composition for compounds I.
    Type: Application
    Filed: May 7, 2018
    Publication date: May 28, 2020
    Inventors: Martin John MCLAUGHLIN, Arun NARINE, Wolfgang VON DEYN, Birgit GOCKEL
  • COMPOUNDS FOR TREATING HUNTINGTON'S DISEASE
    Publication number: 20200165256
    Abstract: The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted bicyclic heteroaryl compounds of Formula (I), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.
    Type: Application
    Filed: June 5, 2018
    Publication date: May 28, 2020
    Inventors: Matthew G. Woll, Lukiana Amedzo, Suresh Babu, Scott J. Barraza, Anuradha Bhattacharyya, Gary Mitchell Karp, Anthony R. Mazzotti, Jana Narasimhan, Jigar Patel, Anthony Turpoff, Zhenrong Xu
  • INHIBITORS OF PHOSPHOINOSITIDE 3-KINASE AND HISTONE DEACETYLASE FOR TREATMENT OF CANCER
    Publication number: 20200165257
    Abstract: The present invention is directed to a dual inhibitor of phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC), including a core containing a quinazoline moiety or a quinazolin-4(3H)-one moiety, a kinase hinge binding moiety, and a histone deacetylase pharmacophore, a pharmaceutically acceptable salt thereof, a prodrug thereof, or solvate thereof. The present invention is also directed to a histone deacetylase inhibitor, including a core containing a quinazolin-4(3H)-one moiety and a histone deacetylase pharmacophore.
    Type: Application
    Filed: June 20, 2018
    Publication date: May 28, 2020
    Inventors: Gurmit Grewal, Ashish Thakur, Gregory James Tawa, Marc Ferrer, Anton M. Simeonov
  • ATROPISOMERISM FOR ENHANCED KINASE INHIBITOR SELECTIVITY
    Publication number: 20200165258
    Abstract: The invention provides a series of conformationally stable and selective kinase inhibitors, and methods of using the kinase inhibitors. The effect of atropisomerism on kinase selectivity was assessed, finding improved selectivity compared to rapidly interconverting parent compounds. The compounds herein are atropisomers having increased kinase selectivity, and are for use in treating conditions that benefit from selective kinase inhibition.
    Type: Application
    Filed: June 21, 2018
    Publication date: May 28, 2020
    Applicant: San Diego State University Research Foundation
    Inventors: Jeffrey L. GUSTAFSON, Sean T. TOENJES, Sean M. MADDOX
  • PYRROLOPYRIMIDINE AND PYRROLOPYRIDINE DERIVATIVES
    Publication number: 20200165259
    Abstract: The present invention relates to pyrrolopyrimidine compounds according to Formula I and their use in the prophylaxis and/or treatment of pain, inflammatory conditions, cardiovascular diseases, neurodegenerative diseases, neurological diseases, complications of type I diabetes, cancer and/or fibrotic diseases. In a particular aspect, the present compounds are ASK inhibitors, particularly ASK1 inhibitors. The present invention also provides methods for the production of a compound of the invention, pharmaceutical compositions comprising a compound of the invention, the use of the compounds in the prophylaxis and/or treatment of pain, inflammatory conditions, cardiovascular diseases, neurodegenerative diseases, neurological diseases, complications of type I diabetes, cancer and/or fibrotic diseases.
    Type: Application
    Filed: July 12, 2018
    Publication date: May 28, 2020
    Inventors: David AMANTINI, Milan MESIC, Gordon SAXTY, Tanja POLJAK, Ines VUJASINOVIC, Dinko ZIHER, David WITTY, Karl Richard GIBSON
  • INHALED POWDER FORMULATIONS
    Publication number: 20200165260
    Abstract: Compounds of Formula (00A) and salts thereof, wherein R1, R2 R3, R4 and n are defined herein, are useful as inhibitors of one or more Janus kinases. Also provided are pharmaceutical compositions that include a compound of Formula (00A) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.
    Type: Application
    Filed: January 30, 2020
    Publication date: May 28, 2020
    Applicant: Genentech, Inc.
    Inventors: Yun-Xing Cheng, Paul Gibbons, Terry Kellar, Wei Li, Rohan Mendonca, Po-wai Yuen, Mark Edward Zak, Lei Zhang
  • CRYSTALLINE OF CAMPHORSULFONIC ACID SALT OF RUCAPARIB AND METHOD OF PREPARING OF TRICYCLIC COMPOUNDS, RUCAPARIB AND CRYSTALLINE OF CAMPHORSULFONIC ACID SALT OF RUCAPARIB
    Publication number: 20200165261
    Abstract: A method of preparing a tricyclic compound of formula (I), comprising the step of converting a compound of formula (II) into a compound of formula (III); and hydrogenating the compound of formula (III) in the presence of hydrogenation catalyst and hydrogen to form the tricyclic compound of formula (I); wherein R1 is H or a C1-3 alkyl group; and R2 is H, a halogen element or a C1-3 alkyl group.
    Type: Application
    Filed: August 1, 2019
    Publication date: May 28, 2020
    Inventors: Wen-Chieh Yang, Mei-Jing Lee, Hsueh-Chen Lee, Lung-Hsiang Li
  • Quinazoline and Indole Compounds to Treat Medical Disorders
    Publication number: 20200165262
    Abstract: Compounds, methods of use, and processes for making inhibitors of Complement Factor B are provided.
    Type: Application
    Filed: January 28, 2020
    Publication date: May 28, 2020
    Applicant: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Avinash Phadke
  • FURO[2,3-b]PYRAN-2-ONE COMPOUNDS AND PROCESS FOR PREPARATION THEREOF
    Publication number: 20200165263
    Abstract: The present invention discloses a novel furo[2,3-b]pyran-2-one compound of formula (I) and a single step process for the preparation of furo[2,3-b]pyran-2-ones using Lewis acid-promoted cascade annulation of alkynols and ?-ketoesters.
    Type: Application
    Filed: May 30, 2018
    Publication date: May 28, 2020
    Inventors: Ravindar Kontham, Sagar Sudam Thorat
  • MACROCYCLIC HIV-1 PROTEASE INHIBITORS AND USES THEREOF
    Publication number: 20200165264
    Abstract: Described herein are compounds of the formulae (I), (Ia), (Ib), and (II) and pharmaceutically acceptable salts, isomers, mixture of isomers, crystalline forms, non-crystalline forms, hydrates, or solvates thereof, as well as methods of making and using compounds of the formulae (I), (Ia), (Ib), and (II) to, among other things, treat HIV/AIDS.
    Type: Application
    Filed: June 29, 2018
    Publication date: May 28, 2020
    Inventors: Arun K. Ghosh, Hiroaki Mitsuya, Sean Fyvie, Margherita Brindisi
  • COMPOUND AS ACC INHIBITOR AND USE THEREOF
    Publication number: 20200165265
    Abstract: Disclosed are a class of compounds which are inhibitors of acetyl-CoA carboxylase (ACC) and the use thereof. In particular, provided are compounds as shown in formula I or isomers, pharmaceutically acceptable salts, solvates, crystals or prodrugs thereof, and methods for preparing the same, and pharmaceutical compositions comprising the compounds and the use of the compounds or compositions for treating and/or preventing diseases associated with ACC expression, such as fibrotic diseases, metabolic diseases, cancers or tissue hyperplasia diseases. The compound has a good inhibitory activity against ACC and shows good promise to be a therapeutic drug for fibrotic diseases, metabolic diseases, cancers or tissue hyperplasia diseases.
    Type: Application
    Filed: July 25, 2018
    Publication date: May 28, 2020
    Applicant: NANJING SANHOME PHARMACEUTICAL CO., LTD.
    Inventors: Yong WANG, Liwen ZHAO, Yazhou WANG, Xu QUAN, Chunhuan JIANG, Hongyan CHEN, Menghua CHEN, Chao LI, Yexin LIAO, Qi LIU, Chen WANG, Hai WANG, Shengwei YANG, Guochuang ZHENG
  • RING CLOSURE REACTION
    Publication number: 20200165266
    Abstract: The present invention relates to a ring closure reaction useful in synthesizing fused aromatic or heteroaromatic ring systems, which may, for example, be used as organic semiconductor materials.
    Type: Application
    Filed: July 9, 2018
    Publication date: May 28, 2020
    Applicant: FLEXENABLE LIMITED
    Inventors: Changsheng WANG, William MITCHELL
  • THIAZOLYL-CONTAINING COMPOUNDS FOR TREATING PROLIFERATIVE DISEASES
    Publication number: 20200165267
    Abstract: The present disclosure provides thiazolyl-containing compounds of Formula (I), (II), or (III). The compounds described herein may be able to inhibit protein kinases (e.g. Src family kinases (e.g. hemopoietic cell kinase (HCK)), Bruton's tyrosine kinase (BTK)) and may be useful in treating and/or preventing proliferative diseases (e.g. myelodysplasia, leukemia, lymphoma, (e.g. Waldenström's macroglobulinemia)) and in inducing apoptosis in a cell (e.g. malignant blood cell). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
    Type: Application
    Filed: November 1, 2019
    Publication date: May 28, 2020
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Sara Jean Buhrlage, Steven P. Treon, Hwan Geun Choi, Yuan Xiong, Guang Yang
  • COMPOUND AND THIN FILM TRANSISTOR AND ELECTRONIC DEVICE
    Publication number: 20200165268
    Abstract: Disclosed are a compound represented by Chemical Formula 1A or 1B, an organic thin film, a thin film transistor, and an electronic device. In Chemical Formulae 1A and 1B, X1, Ar13 , R1 to R4, and n1 are the same as described in the detailed description.
    Type: Application
    Filed: November 25, 2019
    Publication date: May 28, 2020
    Applicant: Samsung Electronics Co., Ltd.
    Inventors: Don-Wook Lee, Jeong II Park, Eun Kyung Lee