Patents Issued in July 16, 2020
  • Publication number: 20200223822
    Abstract: The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, U, W1, W2, W3, R1-R6, and R9 are described herein.
    Type: Application
    Filed: December 12, 2019
    Publication date: July 16, 2020
    Inventors: Jian Lin, Anna Ericsson, Ann-Marie Campbell, Gary Gustafson, Zhongguo Wang, R. Bruce Diebold, Susan Ashwell, David R. Lancia, JR., Justin Andrew Caravella, Wei Lu
  • Publication number: 20200223823
    Abstract: A main object of the present invention is to provide new crystals of (S)-N2-[1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2-yl)pyridine-2,6-diamine maleate (hereinafter, referred to as “compound A”). A Form-I crystal of the compound A, showing diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2?: 6.9 degrees, 9.4 degrees, 12.5 degrees, 15.1 degrees, 16.4 degrees, 18.3 degrees, 19.0 degrees, 24.9 degrees, 25.4 degrees, 27.3 degrees, and 27.7 degrees, wherein X-ray powder diffraction spectrum is obtained by using Cu K? radiation (?=1.54 ?). A Form-II crystal of the compound A, showing diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2?: 6.9 degrees, 9.2 degrees, 12.4 degrees, 14.8 degrees, 16.5 degrees, 18.1 degrees, 18.5 degrees, 19.8 degrees, 23.6 degrees, 24.9 degrees, and 27.7 degrees, wherein X-ray powder diffraction spectrum is obtained by using Cu K? radiation (?=1.
    Type: Application
    Filed: September 27, 2018
    Publication date: July 16, 2020
    Applicant: NIPPON SHINYAKU CO., LTD.
    Inventors: Toshio FUJIWARA, Joanna BIS, Senthil Kumar Kusalakumari SUKUMAR
  • Publication number: 20200223824
    Abstract: A composition for promoting longitudinal bone growth, according to the present invention, promotes the proliferation of the chondrocytes and the differentiation of the osteoblasts and has effects of simultaneously increasing longitudinal bone length and thickness (bone density), and thus has an advantage of being widely prescribable to various age groups, thereby being usable as a pharmaceutical composition for promoting the growth of longitudinal bone length and thickness. An indirubin derivative according to the present invention has prevention or treatment effects through oral administration and has an excellent competitive price unlike conventional hormone-based therapeutic agents.
    Type: Application
    Filed: April 10, 2018
    Publication date: July 16, 2020
    Inventors: Kang-Yell Choi, Gyoonhee Han, Jeong-Ha Hwang, Sehee Choi, Changmok Oh
  • Publication number: 20200223825
    Abstract: The invention relates to a compound of formula (I): Formula (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein A is heteraryl selected from 1H-benzimidazolyl and imidazo[1,2-a]pyridine, and R1, R2, R3, R4 and R5 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5) and its isoenzyme glutaminyl-peptide cyclotransferase-like protein (QPCTL). QC and QPCTL catalyze the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
    Type: Application
    Filed: September 20, 2018
    Publication date: July 16, 2020
    Inventors: Ulrich HEISER, Robert SOMMER
  • Publication number: 20200223826
    Abstract: Aspects of the present disclosure include G6PD-modulating agents and methods for modulating a glucose-6-phosphate dehydrogenase (G6PD) in a sample using such agents. A G6PD-modulating agent can be dimeric and include two terminal carbocyclic or heterocyclic groups connected via a linker. In some instances, the agent includes a diamino-containing linker. In certain cases, the agent includes two amino substituents. Also provided are methods for treating a subject for a G6PD deficiency-associated condition, that include administering to a subject an effective amount of a G6PD-modulating agent to selectively activate a mutant G6PD and treat the subject. Kits and compositions for practicing the subject methods are also provided.
    Type: Application
    Filed: July 24, 2018
    Publication date: July 16, 2020
    Inventors: Sunhee Hwang, DARIA MOCHLY-ROSEN, CHE-HONG CHEN, Andrew Goodwin Raub
  • Publication number: 20200223827
    Abstract: The present technology provides 3,3-difluoroallylamines or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The 3,3-difluoroallylamines or their pharmaceutically acceptable salts exhibit potent inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).
    Type: Application
    Filed: December 12, 2019
    Publication date: July 16, 2020
    Inventors: Tae Dong HAN, Hee Jae TAK, Eun Kyung KIM, Eui Chul LEE, Sol PARK, Hyok Jun CHO, Cheol Hee LIM, So Young KIM, Hyun Ho CHOI, Da Na JEONG, Na Yeon YANG, Na Ry HA
  • Publication number: 20200223828
    Abstract: The invention concerns compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 have any of the meanings hereinbefore defined in the description; process for their preparation, pharmaceutical compositions containing them and their use in treating KIT mediated diseases.
    Type: Application
    Filed: April 26, 2018
    Publication date: July 16, 2020
    Inventors: Tudor GRECU, Jason Grant KETTLE, Martin John PACKER, Stuart Eric PEARSON, James Michael SMITH
  • Publication number: 20200223829
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
    Type: Application
    Filed: March 27, 2020
    Publication date: July 16, 2020
    Inventors: Luke Ashcraft, Alessandro Boezio, John Butler, Aroop Chandra, Chihyuan Chuang, Scott E. Collibee, Mikkel V. Debenedetto, Vincent DiMassa, Russell Graceffa, Justin Malinowski, David Moebius, Bradley Paul Morgan, Joshua Payette, Antonio Romero, David St. Jean, JR., Richard Vargas, John Yeoman, Hanmo Zhang, Alan Cheng, Felix Gonzalez Lopez De Turiso, Michael Garrett Johnson
  • Publication number: 20200223830
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
    Type: Application
    Filed: March 27, 2020
    Publication date: July 16, 2020
    Inventors: Luke Ashcraft, Alessandro Boezio, John Butler, Aroop Chandra, Chihyuan Chuang, Scott E. Collibee, Mikkel V. Debenedetto, Vincent DiMassa, Russell Graceffa, Justin Malinowski, David Moebius, Bradley Paul Morgan, Joshua Payette, Antonio Romero, David St. Jean, JR., Richard Vargas, John Yeoman, Hanmo Zhang, Alan Cheng, Felix Gonzalez Lopez De Turiso, Michael Garrett Johnson
  • Publication number: 20200223831
    Abstract: An organic molecule for use in optoelectronic devices having a structure of formula I wherein X1 and X2 are at each occurrence independently selected from the group consisting of CR21 and N; X3 and X4 are at each occurrence independently selected from the group consisting of CR22 and N; X5 and X6 are at each occurrence independently selected from the group consisting of CR23 and N; R21, R22, R23 is at each occurrence independently selected from the group consisting of hydrogen, deuterium, C1-C8-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, C8-C18-aryl, and C3-C17-heteroaryl; and at least one variable of X1 and X2 is N, at least one variable of X3 and X4 is N and at east one variable of X5 and X6 is N.
    Type: Application
    Filed: January 8, 2020
    Publication date: July 16, 2020
    Inventor: Sebastian Dück
  • Publication number: 20200223832
    Abstract: The present invention provides processes for the preparation of Tezacaftor, as well as intermediates useful in the preparation thereof. In particular, processes are provided for the preparation of a compound of Formula (3), and its conversion to Tezacaftor (1).
    Type: Application
    Filed: January 13, 2020
    Publication date: July 16, 2020
    Inventors: Michael R. Emmett, Prabhudas Bodhuri, Yajun Zhao, Eduardo Gustavo Cammisa, Stuart P. Green
  • Publication number: 20200223833
    Abstract: The present invention relates to the compounds according to Formula (1), the racemates, enantiomers, diastereomers thereof or pharmaceutical acceptable salts thereof, or pharmaceutical compositions comprising these, for the treatment or prevention of metabolic disorders. The compounds according to Formula (1) are, as GPR40 agonists, available for oral administration with glucose-dependent insulin secretion mechanism, which exhibit excellent glucose lowering efficacy without the risk of hypoglycemia. Thus, the compounds and/or pharmaceutical compositions comprising the compounds as effective components are useful in treating and/or preventing symptoms of type 2 diabetes through adequate control of blood glucose.
    Type: Application
    Filed: December 14, 2017
    Publication date: July 16, 2020
    Inventors: Jae-Hoon Kang, Hong-Sub Lee, Kyung-Mi An, Chang-Hee Hong, Hyun-Jung Kwak, Shuo-Lin Cui, Hyo-Jung Song
  • Publication number: 20200223834
    Abstract: The present disclosure provides ?-diketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
    Type: Application
    Filed: September 20, 2019
    Publication date: July 16, 2020
    Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
  • Publication number: 20200223835
    Abstract: The present invention provides the compound represented by Formula 1, and an organic electric element comprising a first electrode, a second electrode, and an organic material layer formed between the first electrode and the second electrode, wherein the organic material layer comprises the compound represented by Formula 1. The driving voltage of an organic electronic device can be lowered, and the luminous efficiency, color purity and life time of an organic electronic device can be improved by comprising the compound represented by Formula 1 in the organic material layer.
    Type: Application
    Filed: August 30, 2016
    Publication date: July 16, 2020
    Applicant: DUK SAN NEOLUX CO., LTD.
    Inventors: Jae Wan JANG, Wonsam KIM, Bo Ram PARK, Seung-won CHOI, Jong-jin HA, Junghwan PARK, Sun-Hee LEE, Mun Jae LEE
  • Publication number: 20200223836
    Abstract: The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.
    Type: Application
    Filed: November 15, 2019
    Publication date: July 16, 2020
    Inventors: Jeffrey William Strovel, Makoto Yoshioka, David J. Maloney, Shyh Ming Yang, Ajit Jadhav, Daniel Jason Urban, JR.
  • Publication number: 20200223837
    Abstract: The present invention relates to a pharmaceutical composition comprising a compound of the formula I as described below or a tautomer or a pharmaceutically acceptable salt thereof; to the compound of the formula I as described below or a tautomer or a pharmaceutically acceptable salt thereof for use as a medicament, especially for use in the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularization, and to certain novel compounds of the formula I as described below or a tautomer or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 14, 2018
    Publication date: July 16, 2020
    Inventors: David William Will, George Reid, Iryna Charapitsa, Joe David Lewis
  • Publication number: 20200223838
    Abstract: Disclosed herein are compositions and methods for treating depression using compositions comprising a compound of formula I. Disclosed herein are compositions and methods for treating depression using compositions comprising phenoxypropylamine compounds and derivatives having selective affinity for and antagonistic activity against the 5-HT1A receptor, as well as 5-HT reuptake inhibitory activity. In addition, compositions and methods for treating depression using compositions comprising a compound of formula II are disclosed. Methods of treating or diminishing at least one symptom of depression in a human subject with a composition comprising a compound of the formula (I) or formula (II), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, are also disclosed.
    Type: Application
    Filed: March 25, 2020
    Publication date: July 16, 2020
    Applicant: Minerva Neurosciences, Inc.
    Inventors: Lorenzo PELLEGRINI, Argeris KARABELAS, Remy LUTHRINGER
  • Publication number: 20200223839
    Abstract: The present teachings relate to a fluoro-containing compound, a composition thereof, a method of using the compound or the composition in treating a disease, and a method of preparing the compound. In a particular example, the compound is chosen from Formulae 4, 4f, 7, 8, 9, 10, 11, or 12, or a salt thereof, or a solvate of any of the foregoing.
    Type: Application
    Filed: June 27, 2018
    Publication date: July 16, 2020
    Inventor: Yao MA
  • Publication number: 20200223840
    Abstract: The invention relates to compounds according to general formula (I), which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
    Type: Application
    Filed: January 13, 2020
    Publication date: July 16, 2020
    Applicant: GRUENENTHAL GMBH
    Inventors: Florian JAKOB, Jo ALEN, Sebastian KRÜGER, Daniela FRIEBE, Stephanie HENNEN, Philipp BARBIE
  • Publication number: 20200223841
    Abstract: The disclosure includes compounds of Formula (I) wherein Z1, Z2, Z3, X, R1, R2, R3, R4, R5, R6, and R7 are defined herein. Also disclosed is a method for treating HBV infection.
    Type: Application
    Filed: December 6, 2019
    Publication date: July 16, 2020
    Inventors: Yi Chen, Yan Lou
  • Publication number: 20200223842
    Abstract: The present technology provides compounds according to Formula I expected to be useful in inhibiting an enterovirus, paramyxovirus, respiratory virus, flaviviridae virus, bunyaviridae virus, togaviridae virus, or rabies virus in a cell and/or treating subjects suffering from an enterovirus, paramyxovirus, respiratory virus, flaviviridae virus, bunyaviridae virus, togaviridae virus, or rabies virus.
    Type: Application
    Filed: September 26, 2018
    Publication date: July 16, 2020
    Applicant: The Regents of the University of California
    Inventors: Paul Krogstad, Michael E. Jung, Jun Zuo, Yanpeng Xing
  • Publication number: 20200223843
    Abstract: There are provided compounds of formula I, wherein X, Ak, s, A, R1 and R2 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of the JAK family) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Application
    Filed: December 11, 2019
    Publication date: July 16, 2020
    Inventor: Matthew Colin Thor Fyfe
  • Publication number: 20200223844
    Abstract: The present technology provides triazolopyridin-3-ones or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The triazolopyridin-3-ones or their pharmaceutically acceptable salts exhibit inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).
    Type: Application
    Filed: December 12, 2019
    Publication date: July 16, 2020
    Inventors: Tae Dong HAN, Hee Jae TAK, Eun Kyung KIM, Dong Hoon KIM, Su Bin CHOI, Sol PARK, Hyun Ho CHOI, Tae Wang KIM, Mi Kyeong JU, Na Ry HA
  • Publication number: 20200223845
    Abstract: The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.
    Type: Application
    Filed: February 24, 2020
    Publication date: July 16, 2020
    Applicant: Katholieke Universiteit Leuven
    Inventors: Dorothée Bardiot, Gunter Carlens, Kai Dallmeier, Suzanne Kaptein, Mohamed Koukni, Arnaud Marchand, Johan Neyts, Wim Smets
  • Publication number: 20200223846
    Abstract: The present disclosure relates to 4,6,7-trisubstituted 1,2-dihydropyrrolo[3,4-c]pyridin/pyrimidin-3-one derivatives, and their preparations and medicinal use. Specifically, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof, wherein the definition of each group is as described in the specification and claims.
    Type: Application
    Filed: March 27, 2020
    Publication date: July 16, 2020
    Inventors: Shuchun GUO, Fusheng ZHOU, Xiang CHEN, Jinzhu ZHAO, Dong HUANG, Jing XIE, Changjiang QIAO, Wan HE, Kai ZHANG, Xi CHEN, Jiong LAN
  • Publication number: 20200223847
    Abstract: The invention relates to Substituted-Quinoxaline-Type Bridged-Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound.
    Type: Application
    Filed: December 6, 2019
    Publication date: July 16, 2020
    Inventors: Jiangchao Yao, John W.F. Whitehead, Naoki Tsuno, Kouki Fuchino
  • Publication number: 20200223848
    Abstract: Provided is a degrader for injured mitochondria based on an autophagy mechanism, the degrader including a compound or a salt thereof, the compound containing a ligand capable of binding to or accumulating in mitochondria and a substituent represented by the following general formula (1): where R1, R2, and R3 are identical to or different from each other, and each represent a hydrogen atom or the like.
    Type: Application
    Filed: July 9, 2018
    Publication date: July 16, 2020
    Applicant: TOHOKU UNIVERSITY
    Inventors: Hirokazu ARIMOTO, Kaori ITTO, Daiki TAKAHASHI, Jun MORIYAMA
  • Publication number: 20200223849
    Abstract: Compounds of formula (I): wherein: R1 is butoxy or methylbutoxy; R2 is a group having the structure: where n is an integer having a value of five; Het is a six-membered saturated heterocycle containing five carbon atoms and one nitrogen atom, wherein Het is attached to the —(CH2)n-moiety at the carbon 4 position of the heterocycle; and R3 is hydrogen; or pharmaceutically acceptable salts thereof; and their use as vaccine adjuvants and in the treatment of various disorders.
    Type: Application
    Filed: January 17, 2020
    Publication date: July 16, 2020
    Applicant: GlaxoSmithKline Biologicals SA
    Inventors: Helene G. BAZIN-LEE, Yufeng LI
  • Publication number: 20200223850
    Abstract: The present disclosure relates to various solid state forms of 5-{[(2S,5R)-2,5-dimethyl-4-(tetrahydro-2H-pyran-4-ylmethyl)piperazin-1-yl]carbonyl}-N-(5-fluoro-2-methylpyrimidin-4-yl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-amine and methods of making the same. Such forms of 5-{[(2S,5R)-2,5-dimethyl-4-(tetrahydro-2H-pyran-4-ylmethyl)piperazin-1-yl]carbonyl}-N-(5-fluoro-2-methylpyrimidin-4-yl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-amine are useful in preparation of pharmaceutical compositions and dosage forms for the treatment of cancer, immune disorders and inflammation.
    Type: Application
    Filed: May 25, 2018
    Publication date: July 16, 2020
    Inventors: Kay OLMSTEAD, Julian NORTHEN
  • Publication number: 20200223851
    Abstract: The present disclosure is directed, in part, to compounds, or pharmaceutically acceptable salts thereof, for the treatment and/or prevention of neurodegenerative disease, mitchonodrial disease, fibrosis, and/or cardiomyopathy.
    Type: Application
    Filed: June 21, 2018
    Publication date: July 16, 2020
    Inventors: Daniel de Roulet, Robert Devita
  • Publication number: 20200223852
    Abstract: The invention generally relates to an improved process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolodin-1-yl)cyclohexyl)acetamide, as well as novel intermediates employed in the process, which may be useful for the treatment of cancer.
    Type: Application
    Filed: July 19, 2018
    Publication date: July 16, 2020
    Inventors: Burcu Selin Aytar, Alina Borovika, Collin Chan, Joerg Deerberg, Nathan R. Domagalski, Martin D. Eastgate, Yu Fan, Michael David Bengt Fenster, Robert V. Forest, Francisco Gonzalez-Bobes, Rebecca A. Green, Matthew R. Hickey, Nathaniel David Kopp, Thomas E. La Cruz, Kathleen Lauser, Hong Geun Lee, David K. Leahy, Helen Y. Luo, Thomas M. Razler, Scott A. Savage, Chris Sfouggatakis, Maxime C.D. Soumeillant, Serge Zaretsky, Bin Zheng, Ye Zhu
  • Publication number: 20200223853
    Abstract: Disclosed herein are heterocyclic compounds that inhibit the binding of menin and MLL or MLL fusion proteins. Also described are specific irreversible inhibitors of menin-MLL interaction. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the menin-MLL irreversible inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, leukemia and other diseases or conditions dependent on menin-MLL interaction.
    Type: Application
    Filed: December 31, 2019
    Publication date: July 16, 2020
    Inventors: Thomas Butler, Jim Palmer, Ravi Upasani, Matthew Welsch, Sridhar Vempati, Brendan Kelly, Edward Painter
  • Publication number: 20200223854
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, Y, W, m, n, p and q are as defined herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: March 27, 2020
    Publication date: July 16, 2020
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Patrick DI GIORGIO, Jerome HERT, Daniel HUNZIKER, Patrizio MATTEI, Markus RUDOLPH, Petra SCHMITZ, Christoph ULLMER
  • Publication number: 20200223855
    Abstract: The invention concerns novel substituted pyrazolo- and triazolo-pyrimidine compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment of respiratory syncytial virus infection.
    Type: Application
    Filed: March 30, 2020
    Publication date: July 16, 2020
    Inventors: David Francis Alain LANÇOIS, Jérôme Émile Georges GUILLEMONT, Pierre Jean-Marie Bernard RABOISSON, Dirk André Emmy ROYMANS, Boris ROGOVOY, Vadim BICHKO, Delphine Yvonne Raymonde LARDEAU, Antoine Benjamin MICHAUT, Anil KOUL
  • Publication number: 20200223856
    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: April 1, 2020
    Publication date: July 16, 2020
    Inventors: Norbert Purro, Mark S. Smyth, Erick Goldman, David D. Wirth
  • Publication number: 20200223857
    Abstract: The present invention relates to a nitrogen-containing fused heterocyclic ring compound and application thereof. The compound has the structural formula (I): using the described compound, it is possible to fabricate a device having higher stability and a longer service life.
    Type: Application
    Filed: November 23, 2017
    Publication date: July 16, 2020
    Inventors: Ruifeng HE, Junyou PAN
  • Publication number: 20200223858
    Abstract: The present invention concerns metallated porphyrin derivatives as ligands of G-quadruplex and their novel use as anti-viral agents.
    Type: Application
    Filed: January 14, 2020
    Publication date: July 16, 2020
    Inventors: Samir AMRANE, Marie-Aline Andreola, Geneviève Pratviel, Jean-Louis Mergny
  • Publication number: 20200223859
    Abstract: The disclosure relates to processes for reducing the amount of a compound of formula (I) or a salt or a solvate thereof present in a composition comprising compounds of formulae (I) and (II) or a salt or a solvate thereof.
    Type: Application
    Filed: September 20, 2019
    Publication date: July 16, 2020
    Applicant: Rhodes Technologies
    Inventors: Keith Edward MCCARTHY, Helge Alfred REISCH, Christopher SPROUT
  • Publication number: 20200223860
    Abstract: Glucosepane is a structurally complex protein post-translational modification (PTM) believed to exist in all living organisms. Research in humans suggests that glucosepane plays a critical role in the pathophysiology of both diabetes and human aging; yet comprehensive biological investigations of this metabolite have been greatly hindered by a scarcity of chemically homogeneous material available for study. Glucosepane possesses a unique chemical structure that incorporates a surprising, never-before-prepared non-aromatic tautomer of imidazole (hereafter termed an “iso-imidazole”), rendering it a challenging target for chemical synthesis. In this application, the inventors report the first total synthesis of glucosepane, enabled by the development of a novel one-pot method for preparation of the iso-imidazole core. The synthesis of the present invention is concise (8-steps starting from commercial materials), convergent, high-yielding (12% overall), and enantioselective.
    Type: Application
    Filed: November 15, 2019
    Publication date: July 16, 2020
    Inventors: David Spiegel, Cristian Draghichi
  • Publication number: 20200223861
    Abstract: The present disclosure relates to solid forms of 3-(5-Fluorobenzofuran-3-yl)-4-(5-methyl-5H-[1,3]dioxolo[4,5-f]indol-7-yl)pyrrole-2,5-dione, processes for preparation thereof, pharmaceutical compositions thereof, and uses thereof in treating disease.
    Type: Application
    Filed: August 10, 2018
    Publication date: July 16, 2020
    Inventor: Yamin ZHANG
  • Publication number: 20200223862
    Abstract: Disclosed are a 4?-amino substituted podophyllotoxin derivative and a synthesis method therefor and the use thereof. The present invention respectively introduces the aromatic heterocyclic compounds anthraquinone, quinazoline, quinoline, indole, indazole, pyrimidine as substituent groups to position-4 of the C ring in the podophyllotoxin or 4?-demethylepipodophyllotoxin to obtain the podophyllotoxin derivatives as shown in formula (V). Experiments involving in vitro tumour cell activity inhibition show that the antitumour activity of most of the compounds as shown in formula (V) of the present invention is significantly improved compared to that of the patented medicine of podophyllotoxin-“etoposide”.
    Type: Application
    Filed: June 4, 2018
    Publication date: July 16, 2020
    Inventor: Yajie Tang
  • Publication number: 20200223863
    Abstract: The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.
    Type: Application
    Filed: January 17, 2020
    Publication date: July 16, 2020
    Applicant: President and Fellows of Harvard College
    Inventors: Yoshito Kishi, Atsushi Ueda, Akihiko Yamamoto, Daisuke Kato
  • Publication number: 20200223864
    Abstract: The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
    Type: Application
    Filed: March 30, 2020
    Publication date: July 16, 2020
    Inventors: Francis G. FANG, Dae-Shik KIM, Hyeong-Wook CHOI, Charles E. CHASE, Jaemoon LEE
  • Publication number: 20200223865
    Abstract: The present invention relates to a process for synthesis of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol abbreviated THIP, having the INN name gaboxadol, starting from pyrrolidin-2-one. The process comprises a new direct process to obtain the intermediate dimethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate or the intermediate diethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate.
    Type: Application
    Filed: March 24, 2020
    Publication date: July 16, 2020
    Inventors: Carla De Faveri, Florian Anton Martin Huber
  • Publication number: 20200223866
    Abstract: Methods of making compounds of Formula I are disclosed:
    Type: Application
    Filed: November 18, 2019
    Publication date: July 16, 2020
    Inventors: Anna Chiu, John Enquist, JR., Nolan Griggs, Christopher Hale, Norihiro Ikemoto, Katie Ann Keaton, Matt Kraft, Scott E. Lazerwith, Michel Leeman, Zhihui Peng, Kate Schrier, Jonathan Trinidad, Jochem Van Herpt, Andrew W. Waltman
  • Publication number: 20200223867
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: January 10, 2020
    Publication date: July 16, 2020
    Inventors: Brian C. Shook, In Jong Kim, Thomas P. Blaisdell, Jianming Yu, Joseph Panarese, Yat Sun Or
  • Publication number: 20200223868
    Abstract: To provide novel pesticides, especially insecticides or acaricides. A condensed heterocyclic compound represented by the formula (1) or its salt, or N-oxide thereof: wherein Q is a structure represented by Q1, Q2 or the like, D substituted with —S(O)nR1 is a structure represented by D1 or D2, A1 is N(A1a) or the like, A1a is C1-C6 alkyl or the like, A4 is a nitrogen atom or C(R4), A5 is a nitrogen atom or C(R5), R1 is C1-C6 alkyl or the like, each of R2, R5 and R6 is independently a hydrogen atom or C1-C6 alkyl, each of R3, R4, Y1, Y2, Y3 and Y4 is independently a halogen atom, halo (C1-C6) alkyl or the like, and n is an integer of 0, 1 or 2.
    Type: Application
    Filed: March 27, 2020
    Publication date: July 16, 2020
    Applicant: Nissan Chemical Corporation
    Inventors: Takao KUDO, Keisuke TSUJI, Kenkichi NOTO, Yukihiro MAIZURU, Hiroto MATSUI, Masaki KOBAYASHI, Hotaka IMANAKA
  • Publication number: 20200223869
    Abstract: The present invention relates to luminescent lanthanide complexes comprising a chelating agent, formed of a macrocycle or ligand, complexing a lanthanide ion, as well as corresponding chelating agents and a process for detecting a biomolecule using said lanthanide complex.
    Type: Application
    Filed: July 5, 2018
    Publication date: July 16, 2020
    Inventors: Amandine ROUX, Anh-Thy BUI, Olivier MAURY, Chantal ANDRAUD
  • Publication number: 20200223870
    Abstract: The present technology relates generally cyclobutane boronates, including methods of preparation by exposing a mixture of a compound of Formula I in a solvent and a catalytic amount of a visible light sensitizer to provide a compound of Formula II, stereoisomers thereof, and/or salts of any of the foregoing. The cyclobutane boronate compounds are useful intermediates in the preparation of pharmaceutically active compounds as well as other useful compounds.
    Type: Application
    Filed: March 18, 2020
    Publication date: July 16, 2020
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Tehshik Peter Yoon, Spencer Owen Scholz, Rowan Mark Littlefield, Niecia Elizabeth Flikweert
  • Publication number: 20200223871
    Abstract: The present invention is directed to arginase inhibitor compounds of formula IA or formula IB: or a pharmaceutically acceptable salt thereof, compositions containing these compounds, and methods of their use for the treatment and diagnosis of conditions characterized by upregulation of arginase, abnormally high arginase activity, or by abnormally low nitric oxide synthase activity.
    Type: Application
    Filed: August 22, 2019
    Publication date: July 16, 2020
    Applicants: AstraZeneca AB, The Trustees of the University of Pennsylvania
    Inventors: David W. Christianson, Bruce Edward Tomczuk, Richard Scott Pottorf, Andrew Vargha Colasanti, Gary Lee Olson