Patents Issued in February 6, 2020
  • QUINOLINE AMINES USEFUL AS CYTOPROTECTIVE AGENTS
    Publication number: 20200039939
    Abstract: Provided herein are compounds of Formula I, pharmaceutical compositions thereof, and methods of their use for treating, preventing, or ameliorating one or more symptoms of a neurological disease, neurodegenerative disorder, or diabetes.
    Type: Application
    Filed: July 14, 2019
    Publication date: February 6, 2020
    Inventor: Russell Dahl
  • MANUFACTURE OF A CRYSTALLINE PHARMACEUTICAL PRODUCT
    Publication number: 20200039940
    Abstract: The present disclosure relates to crystalline particles of N—((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide (I) having specific surface area (SSA) in the range from about 8 to about 16 m2/g, preferably from about 10 to about 15 m2/g, and to the method for the preparation of such particles. Compound (I) is a potent androgen receptor (AR) modulator which is useful as a medicament for example in the treatment of prostate cancer.
    Type: Application
    Filed: February 27, 2018
    Publication date: February 6, 2020
    Inventors: Merja HARTEVA, Anna STAFFANS
  • CXCR4 CHEMOKINE RECEPTOR MODULATORS
    Publication number: 20200039941
    Abstract: Provided herein are small molecule modulators of CXCR4 activity (e.g., agonists, antagonists, inverse agonists, partial agonists), and methods of use thereof (e.g., for the treatment of disease).
    Type: Application
    Filed: October 8, 2019
    Publication date: February 6, 2020
    Inventors: Gary E. Schiltz, Richard J. Miller, Rama K. Mishra
  • ALKANOLAMINE, FRICTION-REDUCING AGENT, AND LUBRICATING OIL COMPOSITION
    Publication number: 20200039942
    Abstract: To provide a friction-reducing agent containing no sulfur nor phosphorus and being excellent in friction-reducing properties, and a lubricating oil composition using it. An alkanolamine represented by the following formula is used as a friction-reducing agent: wherein A1 and A2 are each independently a hydroxy group or a hydrogen atom, provided that A1 and A2 are not hydrogen atoms at the same time, R1 is a hydrocarbon group having at most 30 carbon atoms, R2 to R6 are each independently a hydrogen atom or a hydrocarbon group having at most 30 carbon atoms, and m and n are each independently an integer of from 0 to 10.
    Type: Application
    Filed: January 18, 2018
    Publication date: February 6, 2020
    Inventors: Arimitsu TAKEMOTO, Hiroshi AWANO, Hisao EGUCHI, Manabu YANASE
  • COMPOUNDS, DEVICES, AND USES THEREOF
    Publication number: 20200039943
    Abstract: The present invention provides compounds, e.g., compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are implantable elements (e.g., devices and materials) comprising the same, as well as methods of use thereof, e.g., for treating or preventing a disease, disorder, or condition.
    Type: Application
    Filed: October 3, 2017
    Publication date: February 6, 2020
    Inventors: Omid Veiseh, Richard Heidebrecht, Paul Kevin Wotton, Matthias Alexander Oberli, Robert James Miller
  • CATHEPSIN-D AND ANGIOGENESIS INHIBITORS AND COMPOSITIONS THEREOF FOR TREATING BREAST CANCER
    Publication number: 20200039944
    Abstract: Cathepsin-D and angiogenesis inhibitors and compositions thereof for treating breast cancer are provided. More particularly, the embodiments relate to the design and synthesis of inhibitors of Cathepsin D, which exhibits antiproliferative activity and also inhibits angiogenesis. Also provided are compositions thereof for treating breast cancer.
    Type: Application
    Filed: March 5, 2018
    Publication date: February 6, 2020
    Inventor: Perumal Yogeeswari
  • Compounds
    Publication number: 20200039945
    Abstract: A compound of formula (I), or a pharmaceutical salt thereof:
    Type: Application
    Filed: June 20, 2019
    Publication date: February 6, 2020
    Applicant: CTxT Pty Limited
    Inventors: Helen Rachel Lagiakos, Benjamin Joseph Morrow, Richard Charles Foitzik, Catherine Fae Hemley, Michelle Ang Camerino, Paul Anthony Stupple, Ylva Elisabet Bergman Bozikis, Scott Raymond Walker
  • 1-PHENYLPROPANONE COMPOUNDS AND USE THEREOF
    Publication number: 20200039946
    Abstract: The present invention relates to a 1-phenylpropanone compound of formula (I), wherein X is CH2 or an atom selected from the group consisting of O, S and Se, n is an integer from 4 to 6, A is a substituent selected from the group consisting of 4-morpholyl, 1-piperidinyl, 4-methyl-1-piperazinyl, A being optionally substituted with a (C1-C3)alkyl or (C1-C3)acyl substituent, with the proviso that when X is CH2, n is equal to 5, for use as an antitumoral agent in the treatment of breast cancer, chronic lymphatic leukemia or neuroblastoma. The invention also concerns new 1-phenylpropanone compounds, and compounds as antitumoral agents.
    Type: Application
    Filed: September 29, 2017
    Publication date: February 6, 2020
    Inventors: Giuseppe ZAGOTTO, Giovanni RIBAUDO, Anna Maria BRUNATI, Mario Angelo Primo PAGANO, Elena TIBALDI, Livio TRENTIN
  • PROCESS TO PRODUCE 5-HYDROXYMETHYLFURFURAL (HMF) FROM CARBOHYDRATES USING A SOLVENT SYSTEM CONTAINING WATER AND A POLAR APROTIC SOLVENT
    Publication number: 20200039947
    Abstract: A method to produce 5-hydroxymethylfurfural (HMF) from C6 carbohydrates. The method includes the steps of reacting a reactant comprising at least one C6 carbohydrate, in a reaction mixture comprising at least about 5% (v/v) water, a polar, aprotic solvent, and an acid, for a time, at a temperature, and at a hydrogen ion concentration wherein at least a portion of the C6 carbohydrate present in the reactant is converted to 5-hydroxymethyl furfural (“HMF”).
    Type: Application
    Filed: July 31, 2018
    Publication date: February 6, 2020
    Inventors: James A. Dumesic, Ali Hussain Motagamwala
  • NOVEL GROUP OF STAT3 PATHWAY INHIBITORS AND CANCER STEM CELL PATHWAY INHIBITORS
    Publication number: 20200039948
    Abstract: The present invention relates to the use of a novel class of cancer stem cell pathway (CSCP) inhibitors; to methods of using such compounds to treat refractory, recurrent, or metastatic cancers; to methods of selective killing cancer cells by using such compounds with specific administration regimen; to methods of targeting cancer stem cells by inhibiting Stat3 pathway; to methods of using novel compounds in the treatment of conditions or disorders in a mammal related to aberrant Stat3 pathway activity; and to processes for preparing such compounds and intermediates thereof, and to the pharmaceutical compositions of relevant compounds, and to the specific methods of administration of these compounds.
    Type: Application
    Filed: December 31, 2018
    Publication date: February 6, 2020
    Inventors: Chiang Jia Li, Harry Rogoff, Youzhi Li, Jifeng Liu, Wei Li
  • PROCESS FOR PREPARING FLUORESCEIN QUINOID FORM
    Publication number: 20200039949
    Abstract: The present invention relates to a process for preparing fluorescein quinoid form of Formula (I): Furthermore, the present invention relates to a new solid fluorescein form and a process for the preparation thereof. The present invention also relates to the use of said new solid fluorescein form in the synthesis of fluorescein quinoid form.
    Type: Application
    Filed: July 31, 2019
    Publication date: February 6, 2020
    Applicant: Delmar Chemicals Inc.
    Inventors: Nicholas Tesson, Eduard Bugan, Nadejda Spassova
  • QUINAZOLINONE DERIVATIVE, PREPARATION METHOD THEREFORE, PHARMACEUTICAL COMPOSITION, AND APPLICATIONS
    Publication number: 20200039950
    Abstract: Disclosed are a quinazolinone derivative, a preparation method therefor, a pharmaceutical composition, and applications. Provided are a compound represented by formula I, a pharmaceutically acceptable salt, a solvate, a crystal form, a eutectic crystal, a stereoisomer, an isotope compound, a metabolite, or a prodrug thereof. Generation or activity of a cell factor can be regulated, and accordingly, cancers and inflammatory diseases can be effectively treated.
    Type: Application
    Filed: January 13, 2017
    Publication date: February 6, 2020
    Inventors: Wen-Cherng LEE, Baisong LIAO
  • N-ARYL AND N-HETEROARYL PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS, COMPOSITIONS, AND THEIR USE
    Publication number: 20200039951
    Abstract: In its many embodiments, the present invention provides certain substituted N-aryl and N-heteroaryl piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R6 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, may be useful as Liver X-? receptor (LXR?) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
    Type: Application
    Filed: October 9, 2017
    Publication date: February 6, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael T. Rudd, Zhaoyang Meng, Jenny Wai, David Jonathan Bennett, Edward J. Brnardic, Nigel J. Liverton, Shawn J. Stachel, Yongxin Han, Paul Tempest, Jiuxiang Zhu, Xuewang Xu
  • 2,6-DISUBSTITUTED PYRIDINE DERIVATIVE
    Publication number: 20200039952
    Abstract: The present invention relates to a pyridine derivative of formula (1) wherein R1 is optionally-substituted C1-6 alkyl, optionally-substituted C3-10 cycloalkyl, or optionally-substituted 5- to 10-membered saturated or partially-unsaturated heterocyclyl; R2 is halogen atom, cyano, C1-6 alkyl which may be optionally substituted with 1 to 3 the same or different halogen atoms, C1-6 alkoxy which may be optionally substituted with 1 to 3 the same or different halogen atoms, or amino which may be optionally substituted with 1 to 2 the same or different C1-6 alkyl; and the bind with broken line is single or double bond, or a pharmaceutically acceptable salt thereof, which is useful as a medicament for treating symptoms in anxiety-related disorder.
    Type: Application
    Filed: March 12, 2018
    Publication date: February 6, 2020
    Applicant: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Hidefumi YOSHINAGA, Hiro UEMACHI, Tomomi OHNO, Jeremy BESNARD
  • BENZIMIDAZOLE DERIVATIVES AS BROMODOMAIN INHIBITORS
    Publication number: 20200039953
    Abstract: Compounds of formula (I) and salts thereof: wherein R1, R2, R3, R4 are defined herein. Compounds of formula (I) and salts thereof have been found to inhibit the binding of the BET family of bromodomain proteins to, for example, acetylated lysine residues and thus may have use in therapy, for example in the treatment of autoimmune and inflammatory diseases, such as rheumatoid arthritis; and cancers.
    Type: Application
    Filed: August 22, 2019
    Publication date: February 6, 2020
    Inventors: Rino Antonio BIT, John Alexander Brown, Philip G. Humphreys, Katherine Louise Jones
  • NICOTINE SALTS, CO-CRYSTALS, AND SALT CO-CRYSTAL COMPLEXES
    Publication number: 20200039954
    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 orotic acid are described. The invention further provides methods of preparation and characterization of such nicotine salts. 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: October 10, 2019
    Publication date: February 6, 2020
    Inventors: Gary M. Dull, Andrew Carr, Emma Sharp
  • ANTIBACTERIAL COMPOUNDS AND USES THEREOF
    Publication number: 20200039955
    Abstract: The present invention relates to compounds of formula (I) including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis.
    Type: Application
    Filed: October 14, 2019
    Publication date: February 6, 2020
    Inventors: Anna Marie Upton, Christopher Blair Cooper, Koenraad Jozef Lodewijk Marcel Andries, Jerome Emile Georges Guillemont, Walter Marcel Mathilde Van den Broeck, Brian Desmond Palmer, Zhenkun Ma
  • PYRIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND HEMOGLOBINOPATHIES
    Publication number: 20200039956
    Abstract: A compound of formula (Ia), (Ib) or (Ic) wherein: n is 1 or 2; RN is H or Me; R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4a is selected from OH, —NH2, —C(?O)NH2, and —CH2OH; R4b is either H or Me; R5 is either H or Me; A is either (i), where R6a is ether; or (ii), where X is selected from CH2, NH and O, one of R7a and R7b is selected from CI and ethoxy and the other of R7a and R7b is H.
    Type: Application
    Filed: March 9, 2017
    Publication date: February 6, 2020
    Inventor: Paul Anthony Stupple
  • AROMATIC COMPOUND
    Publication number: 20200039957
    Abstract: Provided is a novel aromatic ring compound which may have a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof may have a GPR40 agonist activity and a GLP-1 secretagogue action, may be useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and may afford superior efficacy.
    Type: Application
    Filed: March 29, 2018
    Publication date: February 6, 2020
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Seiji MIWATASHI, Yasufumi MIYAMOTO, Koji WATANABE, Yayoi NAKAYAMA, Yuko HITOMI, Jumpei AIDA, Nobuyuki TAKAKURA, Hideki FURUKAWA, Naoyoshi NOGUCHI, Yasuhiro HIRATA, Kazuaki TAKAMI, Norihito TOKUNAGA, Tomohiro OKAWA, Akita SHIBUYA, Shizuo KASAl, Toshitake KOBAYASHI, Tsuyoshi MAEKAWA
  • BENZIMIDAZOLE COMPOUNDS AS C-KIT INHIBITORS
    Publication number: 20200039958
    Abstract: The invention relates to c-Kit inhibitors useful in the treatment of cancers, and other serine-threonine kinase mediated diseases, having the Formula: (I) where A, L, R1, R2, R3, and n are described herein.
    Type: Application
    Filed: December 14, 2017
    Publication date: February 6, 2020
    Inventors: Nicholas E. BENCIVENGA, David C. DALGARNO, Joseph M. GOZGIT, Wei-Sheng HUANG, Anna KOHLMANN, Feng LI, Jiwei QI, William C. SHAKESPEARE, Ranny M. THOMAS, Yihan WANG, Yun ZHANG, Xiaotian ZHU
  • NOVEL BENZIMIDAZOLE DERIVATIVE HAVING JNK INHIBITORY ACTIVITY AND USE THEREOF
    Publication number: 20200039959
    Abstract: The present invention relates to a novel benzimidazole derivative having JNK (C-Jun N-terminal kinase) inhibitory activity and use thereof. The novel benzimidazole derivative or a pharmaceutically acceptable salt thereof according to the present invention exhibits excellent inhibitory activity against c-Jun N-terminal kinase 3(JNK 3), and thus it is expected that target therapy can be attained through a more fundamental approach in the prevention or treatment of degenerative brain-nerve system disease.
    Type: Application
    Filed: August 19, 2019
    Publication date: February 6, 2020
    Applicant: INDUSTRY-UNIVERSITY COOPERATION FOUNDATION HANYANG UNIVERSITY ERICA CAMPUS
    Inventors: Jung Mi HAH, Song I YANG
  • RORC2 INHIBITORS AND METHODS OF USE THEREOF
    Publication number: 20200039960
    Abstract: The present invention provides compounds, pharmaceutical compositions, methods of inhibiting ROR? activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such compounds and pharmaceutical compositions.
    Type: Application
    Filed: October 18, 2019
    Publication date: February 6, 2020
    Applicant: Pfizer Inc.
    Inventors: Mark Edward Schnute, Göran Mattias Wennerstål, James Robert Blinn, Neelu Kaila, James Richard Kiefer, Jr., Scot Richard Mente, Ravi G. Kurumbail, Marvin Jay Meyers, Atli Thorarensen, Li Xing, Christoph Wolfgang Zapf, Edouard Zamaratski, Andrew Christopher Flick, Peter Jones
  • SUBSTITUTED FUSED BI- OR TRI- HETEROCYCLIC COMPOUNDS AS EHMT2 INHIBITORS
    Publication number: 20200039961
    Abstract: The present disclosure relates to substituted fused bi- or tri-heterocyclic compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., sickle cell anemia) via inhibition of a methyltransferase enzyme selected from EHMT1 and EHMT2, by administering a substituted fused bi- or tri-heterocyclic compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: September 29, 2017
    Publication date: February 6, 2020
    Inventors: John Emmerson CAMPBELL, Kenneth William DUNCAN
  • FLAME RETARDANTS
    Publication number: 20200039962
    Abstract: The invention relates to flame retardants comprising atriazine compound according to Formula 1: (1) with R=phosphite substituted with alkyl, functionalized alkyl, aryl, functionalized aryl, except halogen-substituted alkyl or aryl; R?=alkylene, arylene, alkoxy or aryloxy, all unsubstituted or functionalized, except halogen-substituted; X1 and X2=hetero atoms and X1=X2 or X1 not=X2 and to specific triazine compounds as such.
    Type: Application
    Filed: October 9, 2017
    Publication date: February 6, 2020
    Inventors: Khalifah Salmeia, Sabyasachi Gaan, Markus Brühwiler
  • PRC1 INHIBITORS AND METHODS OF TREATMENT THEREWITH
    Publication number: 20200039963
    Abstract: Provided herein are small molecule inhibitors of Polycomb Repressive Complex 1 (PRC1) activity, and methods of use thereof for the treatment of disease, including leukemia and other cancers, as well as other diseases dependent on the activity of PRC1.
    Type: Application
    Filed: June 7, 2019
    Publication date: February 6, 2020
    Inventors: Tomasz Cierpicki, Jolanta Grembecka, Weijiang Ying, Yiwu Yao, Felicia Gray, Qingjie Zhao
  • NOVEL CITRIC ACID DERIVATIVE
    Publication number: 20200039964
    Abstract: Compounds (citric acid derivatives) represented by formulas (1) and (2) below are novel compounds having an inhibitory effect against liver disorder and can be used as liver disorder inhibitors and food additives (wherein R1 represents a C1 to C3 alkyl group optionally having a carboxyl group or a hydroxyl group, and R2 represents a hydrogen atom, or R1 and R2 optionally form a cyclic structure together to represent a C2 to C3 alkylene chain).
    Type: Application
    Filed: October 15, 2019
    Publication date: February 6, 2020
    Applicants: ADABIO CO., LTD., OTSUKA PHARMACEUTICAL FACTORY, INC.
    Inventors: Katsuya HIRAISHI, Fumie JIMMA, Hiroyuki SOMA, Taro ADACHI, Masakazu ADACHI, Ippei YAMAOKA, Tomohiro KAGAWA
  • DEUTERATED N-(5-(2,3-DIHYDROBENZO[B][1,4]DIOXINE-6-CARBOXAMIDO)-2-FLUOROPHENYL)-2-((4-ETHYLPIPERAZIN-1-YL)METHYL)QUINOLINE-6-CARBOXAMIDE
    Publication number: 20200039965
    Abstract: The present invention relates to N-(5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-fluorophenyl)-2-((4-ethylpiperazin-1-yl)methyl)quinoline-6-carboxamide, or a pharmaceutically acceptable salt or solvate thereof, wherein at least one hydrogen atom has been substituted with a deuterium atom. Other aspects include pharmaceutical compositions comprising said compounds and medical uses and methods of treatment using said compounds.
    Type: Application
    Filed: October 6, 2017
    Publication date: February 6, 2020
    Inventors: Keith Jones, Matthew D. Cheeseman, A. Elisa Pasqua, Michael J. Tucker
  • URACIL CONTAINING COMPOUNDS
    Publication number: 20200039966
    Abstract: Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
    Type: Application
    Filed: November 21, 2017
    Publication date: February 6, 2020
    Inventor: Robert D. Ladner
  • NOVEL FORMS OF AFATINIB DIMALEATE
    Publication number: 20200039967
    Abstract: The present disclosure is directed to a crystalline, hydrated form of afatinib dimaleate having about 2 to 3 molecules of water, designated as Form Z, a pharmaceutical composition comprising the form, its method of use for treating a patient, and process for its preparation.
    Type: Application
    Filed: October 4, 2019
    Publication date: February 6, 2020
    Inventor: Ronald MUELLER
  • EZH2 INHIBITORS AND USES THEREOF
    Publication number: 20200039968
    Abstract: The present disclosure provides compounds of any one of Formulae (I), (II), and (III). The compounds described herein are inhibitors of histone methyltransferases (e.g., enhancer of zeste homolog 1 (EZH1) and enhancer of zeste homolog 2 (EZH2)) and are useful in treating and/or preventing a broad range of diseases (e.g., proliferative diseases). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
    Type: Application
    Filed: April 21, 2017
    Publication date: February 6, 2020
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: James E. Bradner, Joshiawa Paulk, Jun Qi
  • MODULATORS OF CHEMOKINE RECEPTORS
    Publication number: 20200039969
    Abstract: Compounds are provided as chemokine inhibitors having the structure:
    Type: Application
    Filed: May 16, 2019
    Publication date: February 6, 2020
    Inventors: Xi CHEN, Dean R. DRAGOLI, Junfa FAN, Jaroslaw KALISIAK, Antoni KRASINSKI, Manmohan Reddy LELETI, Venkat MALI, Jeffrey McMAHON, Rajinder SINGH, Hiroko TANAKA, Ju YANG, Chao YU, Penglie ZHANG
  • HYDANTOIN MODULATORS OF KV3 CHANNELS
    Publication number: 20200039970
    Abstract: The invention provides the compound of formula (I): Said compound bein-ganinhibitor of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
    Type: Application
    Filed: December 15, 2017
    Publication date: February 6, 2020
    Inventors: Giuseppe ALVARO, Agostino MARASCO
  • NOVEL HETEROCYCLIC COMPOUND AND ORGANIC LIGHT EMITTING DEVICE COMPRISING THE SAME
    Publication number: 20200039971
    Abstract: Provided is a heterocyclic compound Chemical Formula 1 or 2: and an organic light emitting device comprising the same.
    Type: Application
    Filed: July 19, 2017
    Publication date: February 6, 2020
    Inventors: Min Young KANG, Tae Yoon PARK, Seongmi CHO, Jeong Wook MUN, Min Woo JUNG, Jung Ha LEE
  • INHIBITORS OF JUN N-TERMINAL KINASE
    Publication number: 20200039972
    Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
    Type: Application
    Filed: October 15, 2019
    Publication date: February 6, 2020
    Applicant: IMAGO PHARMACEUTICALS, INC.
    Inventors: Hing L. SHAM, Roy K. HOM, Andrei W. KONRADI, Gary D. PROBST, Simeon BOWERS, Anh TRUONG, R. Jeffrey NEITZ, Jennifer SEALY, Gergely TOTH
  • NOVEL 5-SUBSTITUTED IMIDAZOLYLMETHYL DERIVATIVES
    Publication number: 20200039973
    Abstract: The present invention relates to novel 5-substituted imidazolylmethyl derivatives, to processes for preparing these compounds, to compositions and mixtures comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.
    Type: Application
    Filed: September 22, 2017
    Publication date: February 6, 2020
    Inventors: Pierre-Yves COQUERON, David BERNIE, Ricarda MILLER, Pierre GENIX, Sebastien NAUD, Sven WITTROCK, Stephane BRUNET, Philippe KENNEL, Ruth MEISSNER, Ulrike WACHENDORFF-NEUMANN
  • PYRIDINE COMPOUND
    Publication number: 20200039974
    Abstract: The present invention relates to a compound having RET kinase inhibiting action or a pharmaceutically acceptable salt thereof, useful in the treatment of diseases such as cancer. In particular a compound represented by the following general formula (I) as defined herein: (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 28, 2017
    Publication date: February 6, 2020
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Hiroaki Inagaki, Yoshihiro Shibata, Hidenori Namiki, Hideaki Kageji, Kiyoshi Nakayama, Yasuyuki Kaneta
  • PROCESSES FOR THE PREPARATION OF A BACE INHIBITOR
    Publication number: 20200039975
    Abstract: This invention provides an improved processes for the preparation of verubecestat (Compound of Formula (I)), a potent inhibitor of BACE-1 and BACE-2.
    Type: Application
    Filed: February 10, 2017
    Publication date: February 6, 2020
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: William J. Morris, David Thaisrivongs, Thomas W. Lyons
  • COMPOUNDS AND METHODS FOR INHIBITING FASCIN
    Publication number: 20200039976
    Abstract: Provided are compounds, compositions and methods for inhibiting fascin activity or treating a condition or disorder mediated by fascin activity in a subject in need thereof.
    Type: Application
    Filed: March 11, 2019
    Publication date: February 6, 2020
    Inventors: Xin-Yun HUANG, Christy Young SHUE
  • CYCLIC SUBSTITUTED IMIDAZO[4,5-C]QUINOLINE DERIVATIVES
    Publication number: 20200039977
    Abstract: The present invention provides novel cyclic substituted imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof, wherein R1, R2, R4, R5, R6, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
    Type: Application
    Filed: March 1, 2018
    Publication date: February 6, 2020
    Inventors: Thomas Allen Chappie, Paul Galatsis, Michelle Renee Garnsey, Christopher John Helal, Jaclyn Louise Henderson, Bethany Lyn Kormos, Ravi G. Kurumbail, Luis Angel Martinez-Alsina, Martin Youngjin Pettersson, Antonia Friederike Stepan, Travis T. Wager
  • SOLID FORM OF AZETIDINE DERIVATIVE AND PREPARATION METHOD THEREFOR AND USE THEREOF
    Publication number: 20200039978
    Abstract: The present invention relates to a solid form of a compound of Formula (I), a method for preparing the solid form, a pharmaceutical composition comprising the solid form, and use of the solid form in the treatment of Janus kinase (JAK) related diseases comprising, for example, inflammatory diseases, autoimmune diseases, and cancers.
    Type: Application
    Filed: May 28, 2018
    Publication date: February 6, 2020
    Applicant: SICHUAN KELUN-BIOTECH BIOPHARMACEUTICAL CO., LTD.
    Inventors: JIANHUA GE, Zengying HAN, Fengchun CHEN, Shihu JIAO, Hong ZHANG, Ping ZHANG, Lichun WANG, Jingyi WANG
  • Substituted-3H-imidazo[4,5-c]pyridine and 1H-pyrrolo[2,3-c]pyridine series of novel Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) and Stimulator for Interferon Genes (STING) modulators as cancer immunotherapeutics
    Publication number: 20200039979
    Abstract: Substituted -3H-imidazo[4,5-c]pyridine and 1H-pyrrolo[2,3-c]pyridine series of novel Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) and related compounds, which are useful as inhibitors of ENPP1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the ENPP1.
    Type: Application
    Filed: August 1, 2019
    Publication date: February 6, 2020
    Inventors: Hariprasad Vankayalapati, Sunil Sharma, Mohan Rao Kaadige, Alexis Weston, Trason Thode
  • RUTAECARPINE ANALOGS AND APPLICATIONS THEREOF
    Publication number: 20200039980
    Abstract: The present invention provides RUT analogs with various biological activities. In particular, the biological activities comprise anti-inflammatory activity, vasodilator effects, migration/invasion-suppressive activities, ability against damage due to remodeling between the epithelium and endothelium, collagen deposition and cardiac fibrosis suppress, Snail protein inhibitory effect, etc., which may improve cardiac, vasodilation, and lung functions. The RUT analogs disclosed herein also exhibit a lower cytotoxicity comparing to RUT.
    Type: Application
    Filed: September 25, 2019
    Publication date: February 6, 2020
    Inventors: Chun-Mao LIN, Chi-Ming LEE, Chi WANG, Sheng-Tung HUANG, Jiun-An GU, Tin-An RAU
  • PROCESSES AND INTERMEDIATES FOR PREPARING A BTK INHIBITOR
    Publication number: 20200039981
    Abstract: Disclosed is a process for the preparation of certain intermediates, e.g. the following compound: which intermediate and processes are useful in the preparation of a BTK inhibitor, such as ibrutinib.
    Type: Application
    Filed: October 5, 2017
    Publication date: February 6, 2020
    Inventors: Ben Haim Cyril, Thomas Joost Martti Michiels, Florian Damien Brussels, Simon Wagschal, Dominique Paul M. Depre
  • CRYSTALLINE BINARY SODIUM SALTS OF 5-METHYL-(6S)-TETRAHYDROFOLIC ACID WITH ORGANIC BASES
    Publication number: 20200039982
    Abstract: The present invention is directed to crystalline salt of 5-methyl-(6S)-tetrahydrofolic acid comprising (i) 5-methyl-(6S)-tetrahydrofolic acid, (ii) sodium and (iii) an organic base having a pKa value from 6 to 11; wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to the sodium is from 1:0.5 to 1:1.5 and the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to the organic base is 1:0.5 to 1:1.5 and/or hydrates and/or solvates thereof, as well as, a processes of obtaining the same.
    Type: Application
    Filed: March 28, 2018
    Publication date: February 6, 2020
    Applicant: MERCK PATENT GMBH
    Inventors: Rudolf MOSER, Viola GROEHN, Fritz BLATTER, Martin SZELAGIEWICZ, Ruth BOEHNI STAMM, Markus RUETTIMANN, Giuseppe LAPADULA
  • PYRIDYLAMINO SUBSTITUTED HETEROTRICYCLIC COMPOUNDS, AND PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
    Publication number: 20200039983
    Abstract: The present disclosure relates to pyridinamine-substituted heterotricyclo compounds, a preparation method thereof, and a use thereof in medicines. Specifically, a compound of formula (I), or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, a preparation method and a use thereof are disclosed, wherein the groups in the formula (I) are as defined in the Description and claims.
    Type: Application
    Filed: November 10, 2017
    Publication date: February 6, 2020
    Inventors: Yang LIU, Jiangwei WANG, Qing ZHANG, Yonggang CHEN, Baoxin XI, Wangbin SUN, Yingtao LIU, Xi CHEN
  • Novel [1,2,4]Triazolo[4,3-a]Quinoxaline Derivative, Method For Preparing Same, And Pharmaceutical Composition For Preventing Or Treating BET Protein-Related Diseases, Containing Same As Active Ingredient
    Publication number: 20200039984
    Abstract: Provided are a novel [1,2,4]triazolo[4,3-a]quinoxaline derivative, a method for preparing the same, and a pharmaceutical composition for preventing or treating bromodomain extra-terminal (BET) protein-related diseases including cancer and autoimmune diseases, containing the same as an active ingredient.
    Type: Application
    Filed: January 25, 2018
    Publication date: February 6, 2020
    Inventors: Kwangho Lee, Gildon Choi, Imran Ali, Joo Yun Lee, Jin Soo Lee, Whui Jung Park, Yong Tae Kim, Seung Hwan Kim, Jung Hwan Kim, Jae-Kyung Lim
  • NOVEL MODULATORS OF THE SIGMA-2 RECEPTOR AND THEIR METHOD OF USE
    Publication number: 20200039985
    Abstract: Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of sigma-2 receptor activity.
    Type: Application
    Filed: March 15, 2018
    Publication date: February 6, 2020
    Inventors: Benjamin E. Blass, Daniel J. Canney, Kevin M. Blattner
  • 2H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS AND METHODS AND USES THEREFOR
    Publication number: 20200039986
    Abstract: Compounds according to formula II are useful as agonists of Toll-like receptor 7 (TLR7). Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.
    Type: Application
    Filed: August 1, 2019
    Publication date: February 6, 2020
    Inventors: Yam B. POUDEL, Sanjeev Gangwar, Liqi He, Prasanna Sivaprakasam
  • HETEROAROMATIC NMDA RECEPTOR MODULATORS AND USES THEREOF
    Publication number: 20200039987
    Abstract: Provided is 5-(3-chloro-4-fluorophenyl)-7-cyclopropyl-3-(2-(3-fluoro-3-methylazetidin-1-yl)-2-oxoethyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one and pharmaceutically acceptable salts thereof, and their uses in the treatment of psychiatric, neurological, and neurodevelopmental disorders, as well as diseases of the nervous system.
    Type: Application
    Filed: August 2, 2019
    Publication date: February 6, 2020
    Inventors: David R. Anderson, Robert A. Volkmann, Gregg F. Keaney, Steven C. Leiser, Sam Malekiani, Timothy Piser
  • TLR7 AGONIST CRYSTALLINE FORM A, PREPARATION METHOD AND USE THEREOF
    Publication number: 20200039988
    Abstract: The present invention relates to crystalline form A of a TLR7 agonist 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)-benzyl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine (formula I), a method for preparing the crystalline form A, and the use thereof.
    Type: Application
    Filed: September 25, 2019
    Publication date: February 6, 2020
    Inventors: Zhaozhong DING, Fei SUN, Yinghu HU, Yilong ZHOU, Zheng WANG, Rui ZHAO, Ling YANG