Patents Issued in July 1, 2021
  • Publication number: 20210198171
    Abstract: Disclosed are methods of selective hydrodeoxygenation of aromatic compounds by using catalyst systems comprising N-heterocyclic carbene (NHC) and 4-pyridinol-derived pincer ligands and metal complexes containing these ligands.
    Type: Application
    Filed: October 1, 2020
    Publication date: July 1, 2021
    Inventors: Elizabeth Papish, Aaron Vannucci
  • Publication number: 20210198172
    Abstract: The present invention provides a process for preparing an alkoxymethyl alkynyl ether compound having a terminal triple bond of the following formula (4): H—C?C(CH2)aOCH2OCH2R (4), wherein R represents a hydrogen atom, an n-alkyl group having 1 to 9 carbon atoms, or a phenyl group, and “a” represents an integer of 1 to 10, the method comprising subjecting an alkynol compound having a terminal triple bond of the following formula (1): H—C?C(CH2)aOH (1), wherein “a” is as defined above, to an alkoxymethylation with a halomethyl alkyl ether compound of the following formula (3): RCH2OCH2X (3), wherein X represents a halogen atom, and R is as defined above, in the presence of a dialkylaniline compound of the following formula (2): [CH3(CH2)b][CH3(CH2)c]NC6H5 (2), wherein b and c represent, independently of each other, an integer of 0 to 9, to form the alkoxymethyl alkynyl ether compound (4) having a terminal triple bond.
    Type: Application
    Filed: December 21, 2020
    Publication date: July 1, 2021
    Inventors: Yuki Miyake, Miyoshi Yamashita, Takeshi Kinsho, Akihiro Baba
  • Publication number: 20210198173
    Abstract: A process for oxidizing methyl-substituted biphenyl compounds comprises contacting a mixture comprising isomers of at least one methyl-substituted biphenyl compound with a source of oxygen, wherein the mixture comprises at least 20 wt % of isomer(s) having a methyl group at a 2-position or a 3-position on at least one benzene ring and at least 50 wt % of isomer(s) having a methyl group at a 4-position on at least one benzene ring, wherein said percentages are based on the total weight of the at least one methylbiphenyl compound in the mixture.
    Type: Application
    Filed: February 19, 2021
    Publication date: July 1, 2021
    Inventors: Jihad M. Dakka, Bryan A. Patel, Michael Salciccioli, Stephen Zushma
  • Publication number: 20210198174
    Abstract: A process for making a high purity salt comprises the steps of providing an organic compound, providing a metal salt, adding the metal salt and organic compound to an aqueous medium, heating the reaction mixture to react the organic compound and the metal salt to form an organic salt, collecting the organic salt, and directly contacting the collected organic salt with a heated gas stream while agitating the collected organic salt to reduce the moisture content of the dried organic salt to about 7% or less.
    Type: Application
    Filed: December 11, 2020
    Publication date: July 1, 2021
    Inventor: Darin L. Dotson
  • Publication number: 20210198175
    Abstract: Compounds derived from biomass, e.g., cellulose and lignins, methods of forming such compounds and polymers and products formed using such compounds.
    Type: Application
    Filed: December 20, 2019
    Publication date: July 1, 2021
    Applicant: NDSU RESEARCH FOUNDATION
    Inventors: Mukund P. Sibi, Selvakumar Sermadurai, Nicolas Zimmermann, Eric Serum, Gaoyuan Ma, Ramkumar Moorthy, Krystal Kalliokoski
  • Publication number: 20210198176
    Abstract: Disclosed are a reduction method and reduction product of an alkenyl active methylene compound. The reduction reaction comprises the following steps: taking an alkenyl active methylene compound as a substrate, a metal hydride as a reducing agent, and a palladium compound as a catalyst, performing a reduction reaction to obtain a reduction product, and then reducing the alkenyl active methylene compound. The reduction system is a simple method for reducing the alkenyl active methylene compound, and the used hydride and palladium compound catalyst are both reagents that could easily be obtained in a laboratory. Compared with conventional hydrogen hydrogenation methods and reduction methods of reducing agents, the method is easier to operate, higher in safety, mild in conditions, and high in reaction yield, a reaction in a one-pot two-step manner can be achieved, and high atom economy and step economy can be obtained.
    Type: Application
    Filed: March 12, 2021
    Publication date: July 1, 2021
    Inventors: Shilei ZHANG, Yujian MAO
  • Publication number: 20210198177
    Abstract: Methods and compositions comprising an emulsion or a microemulsion for use treating an oil and/or gas well are provided. In some embodiments, the emulsion or the microemulsion comprises an aqueous phase, a solvent, a surfactant comprising alkyl polyglycoside, an alcohol, and, optionally, one or more additives.
    Type: Application
    Filed: March 8, 2021
    Publication date: July 1, 2021
    Applicant: Flotek Chemistry, LLC
    Inventors: Siwar Trabelsi, Randal M. Hill
  • Publication number: 20210198178
    Abstract: A calixarene compound represented by formula (1) below is provided. The calixarene compound contains, per molecule, at least one —CH2OH group or phenolic hydroxy group and at least one carbon-carbon unsaturated bond. R1's are a structural moiety (A), which has a —CH2OH group; a structural moiety (B), which has a carbon-carbon unsaturated bond; a structural moiety (C), which has a —CH2OH group and a carbon-carbon unsaturated bond; a monovalent organic group (D), which is different from (A), (B), and (C); or a hydrogen atom (E). R2's are (A), (B), (C), (D), or (E) provided that not all R2's are (E). R3's are one of a hydrogen atom, an aliphatic hydrocarbon group, and an aryl group. n is 2 to 10. * is a point of attachment to an aromatic ring. A curable composition including the calixarene compound is provided. A cured product of the curable composition is provided.
    Type: Application
    Filed: July 19, 2018
    Publication date: July 1, 2021
    Inventors: Shinya Yamamoto, Yutaka Kadomoto, Masanori Miyamoto, Tomoyuki Imada, Hidetomo Kai
  • Publication number: 20210198179
    Abstract: A compound serving as coalescing agent and a coating composition employing the compound are provided. The compound has a structure represented by Formula (I) wherein n is 0, 1, 2, or 3; m is 0, 1, 2, or 3; R1 is R2 is R3, R4, R5, and R6 are independently C1-12 alkyl group; and, R1 is distinct from R2 when n is equal to m.
    Type: Application
    Filed: December 30, 2019
    Publication date: July 1, 2021
    Applicant: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTE
    Inventors: Ya-I HSU, Yuan-Chang HUANG, Yi-Che SU, Wei-Cheng TANG
  • Publication number: 20210198180
    Abstract: The present invention relates to a method for preparing substituted 4-aminoindane derivatives from 2-(hydroxyalkyl)-anilines by cyclization, in which the substituents R1, R2, R3 and R4 have the definitions as specified in the description.
    Type: Application
    Filed: May 21, 2019
    Publication date: July 1, 2021
    Inventors: Florian ERVER, Frank MEMMEL, Sergii PAZENOK
  • Publication number: 20210198181
    Abstract: Provided are: a method for producing a compound that excels in storage stability and handleability; the compound; and an epoxy curing agent containing the compound. The method for producing a compound represented by Formula (1-1) includes subjecting the compound represented by Formula (5-1) to an addition reaction to add ethylene and/or propylene in the presence of a base. In Formula (5-1), RX to RZ each independently represent a hydrogen atom, an ethyl group, an n-propyl group, or an isopropyl group, and n is an integer of from 1 to 3. In Formula (1-1), RA to RD each independently represent a hydrogen atom, an ethyl group, an n-propyl group, or an isopropyl group, and n is an integer of from 1 to 3.
    Type: Application
    Filed: May 28, 2019
    Publication date: July 1, 2021
    Applicant: MITSUBISHI GAS CHEMICAL COMPANY, INC.
    Inventors: Yoichi TAKANO, Kazuyoshi UERA
  • Publication number: 20210198182
    Abstract: A process to prepare an amine-functional ester of an amino carboxylic acid includes the step of reacting a polyol of the formula (I) HO-A-OH??(I) where A is a carbon chain with about 2 to about 36 carbon atoms that is aliphatic linear or branched, saturated or unsaturated, or aromatic, or CH2CH(OH)CH2, CH2C(CH2OH)2CH2, CH2C(CH2OH)(CH3)CH2, CH2C(CH2OH)(CH2CH3)CH2, p-tetrahydrofuran, erythritol or an ester of di- or tricarboxylic acids with ethylene or propylene glycol, and wherein A can optionally be alkoxylated or reacted with hydroxy carboxylic acids, with an aminocarboxylic acid of formula II or its cyclic amide of the formula III, where m is an integer of about 1 to about 8 in formula II and about 3 to about 8 in formula III, each R independently is hydrogen or a C1-C4 alkyl group, or CH2CH2COOH, or CH2COOH, or (CH2)4NH2, in the presence of a Brønsted-Lowry acid.
    Type: Application
    Filed: December 22, 2020
    Publication date: July 1, 2021
    Applicant: NOURYON CHEMICALS INTERNATIONAL B.V.
    Inventors: Natalija SMOLKO SCHWARZMAYR, Ruifei WANG, Alexander Michael WETZEL, Louis Eckhard SCHWARZMAYR, Göran Thomas LJUNGDAHL, Krzysztof Piotr KOLMAN
  • Publication number: 20210198183
    Abstract: Disclosed are a glycerol derivative that is useful for improving, preventing or treating inflammation-related diseases by inhibiting overexpression of various inflammatory cytokines such as IL-4, IL-6 and so on, or chemokine CXCL8 and reducing migration of HL-60 cell lines, preparation method therefor, and an immunomodulator containing the same as active ingredient. It includes a glycerol derivative represented by Chemical formula 2 or 3 in the specification.
    Type: Application
    Filed: April 19, 2019
    Publication date: July 1, 2021
    Applicant: Enzychem Lifesciences Corporation
    Inventors: Ki Young SOHN, Jae Wha KIM, Sun Young YOON, Chang Hyun YOO, Jin Seon JEONG
  • Publication number: 20210198184
    Abstract: The invention relates to a composition excellent in stability during storage and stability during utilization, and relates to a method of producing the composition. The composition includes a compound (A) represented by general formula (1) and a compound (B) represented by general formula (2), and includes 0.00002 to 0.2 parts by mass of the compound (B) with respect to 100 parts by mass of the compound (A), (R1—COO)n—R2—(NCO)m??(1) (R1—COO)n—R2—(R3—R1)m??(2) wherein in general formulae (1) and (2), R1 is an ethylenically unsaturated group having 2 to 7 carbon atoms; R2 is a (m+n)-valent hydrocarbon group having 1 to 7 carbon atoms and optionally contains an ether group; R1 and R2 in the general formula (1) are the same as R1 and R2 in the general formula (2); in general formula (2), R3 is —NHC(?O)—; and n and m each represent an integer of one or two.
    Type: Application
    Filed: August 16, 2019
    Publication date: July 1, 2021
    Applicant: SHOWA DENKO K.K.
    Inventors: Norihito NISHIMURA, Katsutoshi OHNO
  • Publication number: 20210198185
    Abstract: A process for producing an intermediate adiponitrile stream, the process comprising separating an adiponitrile process stream comprising less than 50 wt % adiponitrile, and optionally TCH, to form the intermediate adiponitrile stream comprising at least 5 wt % adiponitrile and a heavies stream comprising high-boiling components and optionally solid impurities; and optionally utilizing at least a portion of the intermediate adiponitrile stream outside of the process.
    Type: Application
    Filed: December 30, 2020
    Publication date: July 1, 2021
    Inventors: Sanjay Dube, Benjamin Haseltine, Jefferson Thomas Ebert, Darrick Elmore
  • Publication number: 20210198186
    Abstract: The present disclosure relates generally to processes for recovering tricyanohexane (TCH) via purification of by-product or co-product streams of adiponitrile production. In particular, the present disclosure relates to a process for purifying tricyanohexane (TCH), the process having the steps of (a) separating an adiponitrile process stream comprising adiponitrile and TCH to form a first overhead lights stream comprising low-boiling components and high-boiling components and a first bottoms heavies stream comprising high-boiling components and solid impurities; and (b) separating the first overhead lights stream in a distillation column to form a second overhead lights stream comprising low-boiling components, a second bottoms heavies stream comprising high-boiling components, and a TCH stream comprising TCH and less than 10 wt. % impurities; wherein the distillation column is a low pressure distillation column.
    Type: Application
    Filed: December 30, 2020
    Publication date: July 1, 2021
    Applicant: Ascend Performance Materials Operations LLC
    Inventors: Sanjay Dube, Benjamin Haseltine, Jefferson Thomas Ebert, Darrick Elmore
  • Publication number: 20210198187
    Abstract: A process for producing a TCH stream, the process comprising: separating, in a first column, an adiponitrile process stream comprising TCH and optionally adiponitrile, to form an adiponitrile stream comprising greater than 5 wt. % adiponitrile and a first TCH stream comprising TCH, and optionally a heavies stream comprising high-boiling components and solid impurities; and optionally purifying the first TCH stream, via one or more columns, to form a purified TCH stream comprising greater than 50 wt. % TCH; wherein the first column is operated at a pressure drop less than 25 mmHg.
    Type: Application
    Filed: December 30, 2020
    Publication date: July 1, 2021
    Applicant: Ascend Performance Materials Operations LLC
    Inventors: Sanjay Dube, Benjamin Haseltine, Jefferson Thomas Ebert, Darrick Elmore
  • Publication number: 20210198188
    Abstract: The present invention relates to a novel cathode buffer layer material, and an organic or organic/inorganic hybrid photoelectric device comprising same, and, if a novel compound of the present invention is applied to a cathode buffer layer of an organic photoelectric device such as organic solar cells, organic photodiode, colloidal quantum dot solar cell, and perovskite solar cell, a surface property of an electron transfer layer is improved via a high dipole moment of the novel compound, an electron can be easily extracted from a photoactive layer to a cathode electrode, and series resistance and leakage current can be reduced, thereby having a useful industrial effect, as performance of the organic or organic/inorganic hybrid photoelectric device being manufactured, such as an organic solar cell, organic photodiode, colloidal quantum dot solar cell, and perovskite solar cell, can be significantly improved.
    Type: Application
    Filed: April 22, 2019
    Publication date: July 1, 2021
    Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Sung Cheol Yoon, Chang Jin Lee, Jaemin Lee, Seung Hun Eom, Seung Hoon Lee, Ju Hyoung Jung
  • Publication number: 20210198189
    Abstract: The present invention relates to novel hydroxamic acid derivatives as inhibitors of meprin ? and/or ?, pharmaceutical compositions comprising such compounds, methods for treatment or prophylaxis of diseases or conditions, especially such that are related to meprin ? and/or ?, and compounds and pharmaceutical compositions for use in such methods.
    Type: Application
    Filed: March 8, 2021
    Publication date: July 1, 2021
    Applicant: Vivoryon Therapeutics AG
    Inventors: Michael Wermann, Mirko Buchholz, Hans-Ulrich Demuth, Daniel Ramsbeck, Dagmar Schlenzig, Stephen Schilling
  • Publication number: 20210198190
    Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Application
    Filed: May 28, 2019
    Publication date: July 1, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shuwen He, Dane Clausen, Liangqin Guo, Yongxin Han, Xianhai Huang, Alexander Pasternak, Qinglin Pu, Dong Xiao, Li Xiao, Feng Ye, Hongjun Zhang
  • Publication number: 20210198191
    Abstract: This invention provides illudin derivatives, intermediates, preparation methods, pharmaceutical compositions and uses thereof. Specific examples include novel synthetic routes to prepare illudin derivatives and an illudin derivative having a positive optical rotation, which has therapeutic value.
    Type: Application
    Filed: March 4, 2021
    Publication date: July 1, 2021
    Inventors: Gregory J. Tobin, Shawn T. Blumberg, Andrey D. Malakhov, Varsin A. Archer
  • Publication number: 20210198192
    Abstract: The present invention discloses a method for preparing florfenicol and its intermediate (V), comprising an addition reaction, a ring closure reaction, a hydrolysis reaction, a ring opening reaction, a reduction reaction, a ring reaction, a fluorination reaction and a ring opening reaction. In the present method for preparing florfenicol, respective reaction steps can be continuously operated, therefore the methods of the present invention features simplified process and shorter synthetic route, and obtained florfenicol has high chiral purity and is of high yield. The method of the present invention for preparing florfenicol (TM) using the intermediate (V) avoids waste water pollution and reduces the cost for treating wastewater and alleviates environmental pollution. At the same time, the methods of the present invention eliminates a chiral resolution procedure, thus increasing the utilization rate of atoms in the reaction. As a result, cost is reduced and process is simplified.
    Type: Application
    Filed: August 20, 2018
    Publication date: July 1, 2021
    Inventors: Wensen LI, Wenqi ZHANG
  • Publication number: 20210198193
    Abstract: Involved are a diketone oxime ester compound shown in formula I and a manufacturing method therefor, and a photo-curable composition using the compound of formula I as a photoinitiator. The composition has extremely high light sensitivity and relatively low yellowing resistance when applied to prepare a color filter for a light resistance device such as a display screen.
    Type: Application
    Filed: August 30, 2018
    Publication date: July 1, 2021
    Inventors: Wenchao ZHAO, Jiaqi LI, Chenlong WANG
  • Publication number: 20210198194
    Abstract: The present invention provides a route for synthesizing monofunctional thiuram compounds that is safe, environmentally friendly, and cost effective. This method specifically involves synthesizing a monofunctional thiuram by (1) reacting a tetraorganylthiuram disulfide with an organyl mercaptan to produce the monofunctional thiuram and a dithiocarbamate metal salt or a dithiocarbamate metalloid salt under basic conditions, (2) separating the monofunctional thiuram in an organic phase from the dithiocarbamate metal salt or the dithiocarbamate metalloid salt in an aqueous phase, and (3) recovering the monofunctional thiuram from the aqueous phase. The monofunctional thiuram compounds made in accordance with this invention are of particular value as accelerators for use in the vulcanization of rubber. The use of these monofunctional thiuram compounds as accelerators provides good cure rates and as well as good scorch safety.
    Type: Application
    Filed: December 10, 2020
    Publication date: July 1, 2021
    Inventors: Thomas Franklin Spilker, Ji Yang Jin, Frank J. Feher
  • Publication number: 20210198195
    Abstract: Topical formulations comprising soft glycopyrrolates are useful for treating excessive sweating conditions in subjects, such as humans suffering from hyperhidrosis. Preferably, at least one soft anticholinergic agent is provided in an effective amount or concentration in an anhydrous formulation that can inhibit excessive perspiration resulting from a condition such as hyperhidrosis.
    Type: Application
    Filed: March 15, 2021
    Publication date: July 1, 2021
    Inventors: NICHOLAS S. BODOR, JOHN J. KOLENG, DAVID ANGULO
  • Publication number: 20210198196
    Abstract: Heptamethine cyanine fluorophore conjugates and conjugate precursors are disclosed. Methods of using the conjugates and conjugate precursors are also disclosed. The disclosed conjugates are neutral zwitterionic molecules and exhibit little or no aggregation.
    Type: Application
    Filed: February 18, 2021
    Publication date: July 1, 2021
    Applicant: The USA, as represented by the Secretary, Department of Health and Human Services
    Inventors: Martin John Schnermann, Michael Philip Luciano, Roger Rauhauser Nani
  • Publication number: 20210198197
    Abstract: The present disclosure belongs to the technical field of indomethacin synthesis, and discloses a method for synthesizing an indomethacin and an analogue thereof. The method for synthesizing an indomethacin and an analogue thereof includes steps of: introducing an alkyl group, an aromatic ring or a heteroaromatic ring directly at the C2 position of indole, a carboxylic acid fragment at the C3 position of the indole, and an aroyl group at the N1 position of the indole through palladium-catalyzed reactions. The present disclosure solves a problem: most of the existing indomethacin synthesis methods are achieved by construction of an indole ring and modification; simple structural changes of an indomethacin molecule based on this synthetic strategy often require de novo synthesis; the late modification and structure-activity relationship study of the indomethacin molecule have lengthy synthetic steps.
    Type: Application
    Filed: December 3, 2020
    Publication date: July 1, 2021
    Inventors: Zhilong CHEN, Helin LU
  • Publication number: 20210198198
    Abstract: The present invention relates to crystalline forms of (1R,5S)-1-(naphthalen-2-yl)-3-azabicyclo[3.1.0]hexane hydrochloride and compositions comprising the same and methods of making and using the same.
    Type: Application
    Filed: August 14, 2020
    Publication date: July 1, 2021
    Inventors: Anthony Alexander MCKINNEY, Franklin BYMASTER, Walter PISKORSKI, Fred J. FLEITZ, Yonglai YANG, David A. ENGERS, Valeriya SMOLENSKAYA, Venkat KUSUKUNTLA
  • Publication number: 20210198199
    Abstract: To provide a novel therapeutic agent for fibrosis that induces selective cell death of lung fibroblasts and suppresses lung fibrosis without injuring alvocar epithelial cells. A pharmaceutical composition for treating fibrosis, the pharmaceutical composition comprising a compound of formula (I) or formula (II): wherein in formula (I), R1 represents a C1-4 alkyl group optionally substituted with a halogen atom, and l represents an integer of 3 to 6; and in formula (II), n represents an integer of 8 to 12, or a pharmaceutically acceptable salt thereof or a solvate of the compound or the salt thereof.
    Type: Application
    Filed: September 26, 2019
    Publication date: July 1, 2021
    Applicants: LTT BIO-PHARMA CO., LTD., MUSASHINO UNIVERSITY
    Inventors: Tohru MIZUSHIMA, Ken-ichiro TANAKA
  • Publication number: 20210198200
    Abstract: The disclosure features amino lipids and compositions involving the same. Nanoparticle compositions include an amino lipid as well as additional lipids such as phospholipids, structural lipids, PEG lipids, or a combination thereof. Nanoparticle compositions further including therapeutic and/or prophylactic agents such as RNA are useful in the delivery of therapeutic and/or prophylactic agents to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
    Type: Application
    Filed: June 14, 2018
    Publication date: July 1, 2021
    Inventors: Kerry E. BENENATO, William BUTCHER
  • Publication number: 20210198201
    Abstract: A compound of the formula where R1, R2, R3, R4, R5, R6a, and R6b are as defined in the specification and claims, or an enantiomer, stereoisomer or diastereoisomer thereof, or a pharmaceutically acceptable salt thereof, and the use thereof in the treatment of diseases, disorders, syndromes and conditions responsive to modulation of a melanocortin receptor.
    Type: Application
    Filed: March 17, 2021
    Publication date: July 1, 2021
    Inventors: James Bullington, Axel Metzger, John Harold Dodd
  • Publication number: 20210198202
    Abstract: The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl) pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morphohnoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
    Type: Application
    Filed: March 17, 2021
    Publication date: July 1, 2021
    Inventors: David G. HANGAUER, JR., Debasis PATRA, Jeremy A. CODY, Grant J. PALMER, Paul K. ISBESTER, Jonathon SALSBURY
  • Publication number: 20210198203
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Application
    Filed: March 12, 2021
    Publication date: July 1, 2021
    Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, JR.
  • Publication number: 20210198204
    Abstract: Disclosed are compounds of formula I, II, and III, and pharmaceutically acceptable salts thereof, which are inhibitors of kallikrein. Also provided are pharmaceutical compositions comprising such a compound, and methods involving use of the compounds and compositions in the treatment and prevention of acquired or hereditary angioedema, or other diseases and conditions characterized by aberrant kallikrein activity.
    Type: Application
    Filed: August 7, 2020
    Publication date: July 1, 2021
    Inventors: Pravin L. Kotian, Yarlagadda S. Babu, V. Satish Kumar, Venkat R. Chintareddy, Weihe Zhang, Lakshminarayana Vogeti
  • Publication number: 20210198205
    Abstract: The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N?-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.
    Type: Application
    Filed: October 29, 2020
    Publication date: July 1, 2021
    Inventors: Dana T. Aftab, Nathan Guz, Stephen Lau, Noel Hamill, Tracy Walker, Jana Galbraith, Simon Yau, Khalid Shah
  • Publication number: 20210198206
    Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Application
    Filed: March 8, 2021
    Publication date: July 1, 2021
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders, Shunqi Yan
  • Publication number: 20210198207
    Abstract: A novel quinolone derivative and methods of its preparation are described in which the novel derivative comprises a diphenyl ether substituent on the nitrogen atom at the 1-position of the main quinolone ring. The novel derivative is shown to have antibacterial and anti-tumor cell activity.
    Type: Application
    Filed: March 24, 2020
    Publication date: July 1, 2021
    Inventors: Pengfei ZHANG, Wanmei LI, Weiming XU, Haifeng WU
  • Publication number: 20210198208
    Abstract: This invention relates to 4-substituted isoquinoline compounds and their derivatives and uses thereof for treatment of cancer, for example, acute myeloid leukemia.
    Type: Application
    Filed: March 1, 2021
    Publication date: July 1, 2021
    Inventor: Herman O. SINTIM
  • Publication number: 20210198209
    Abstract: The present invention relates to a process for preparing compounds of the formula (I) by halogenating compounds of the formula (II), where in R1, R2, R3 and X are defined according to the invention.
    Type: Application
    Filed: May 20, 2019
    Publication date: July 1, 2021
    Applicant: Bayer Aktiengesellschaft
    Inventors: Andreas REMBIAK, Eike Kevin HEILMANN
  • Publication number: 20210198210
    Abstract: A process for the sigmatropic rearrangement of the compound of formula in which R3 is an NO2 group and R4 is either a hydrogen or an NO2 group, includes heat treating the compound by microwave.
    Type: Application
    Filed: August 30, 2019
    Publication date: July 1, 2021
    Inventors: Sébastien COMTE, Elsa DELMAS
  • Publication number: 20210198211
    Abstract: Object of the present invention is a better crystalline form of Eltrombopag (ETP) monoethanolamine salt, named Form D, stable, suitable for pharmaceutical purposes, and with the highest solubility in water and excellent non-hygroscopicity, then the related process and intermediates thereof.
    Type: Application
    Filed: July 25, 2019
    Publication date: July 1, 2021
    Applicant: F.I.S. - FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Nicolas TESSON, Jordi DE MIER VINUE, Paolo STABILE, Pierluigi PADOVAN, Matteo DE POLI, Angelo RESTELLI
  • Publication number: 20210198212
    Abstract: The present disclosure relates to an organic compound and an organic light emitting display device using the same wherein the organic compound is represented by Chemical Formula 1 and a display device using the organic compound. The organic compound represented by Chemical Formula 1 has excellent electron transport properties and durability and is used for an electron transport layer of an organic light emitting element, thereby lowering a driving voltage and improving the luminous efficiency and lifetime. (In the above Chemical Formula 1, at least two of X1, X2 and X3 are N, Y1 and Y2 are each independently a substituted or unsubstituted phenylene group or a single bond, at least one of Ar1 and Ar2 is selected from a substituted or unsubstituted triazine group, a functional group represented by Chemical Formula 2 and a functional group represented by Chemical Formula 3.
    Type: Application
    Filed: December 22, 2020
    Publication date: July 1, 2021
    Applicants: LG DISPLAY CO., LTD., Lapto Co., Ltd.
    Inventors: DaeWon RYU, DoHan KIM, KyouSic KIM, ChulSoo LIM, MunSoo KIM
  • Publication number: 20210198213
    Abstract: Compounds having a structure of formula (I), (I-A), (Ia)-(Ie), (A)-(E), and (II) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of disorders including prostate cancer are also provided.
    Type: Application
    Filed: May 24, 2019
    Publication date: July 1, 2021
    Inventors: Han-Jie Zhou, Peter Virsik, Raymond John Andersen, Marianne Dorothy Sadar, Kunzhong Jian, Daniel Andrew Golec
  • Publication number: 20210198214
    Abstract: The present invention provides the compound represented by Formula 1, 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, and electronic device thereof, and by comprising the compound represented by Formula 1 in the organic material layer, the driving voltage of the organic electronic device can be lowered, and the luminous efficiency and life time of the organic electronic device can be improved.
    Type: Application
    Filed: December 30, 2016
    Publication date: July 1, 2021
    Applicant: DUK SAN NEOLUX CO., LTD.
    Inventors: Soung Yun MUN, Sun-Hee LEE, Bumsung LEE, Junghwan PARK, Gyu min LEE
  • Publication number: 20210198215
    Abstract: The present invention relates to an organic material and to an electronic device comprising the organic material, particularly to an electroluminescent device, particularly to an organic light emitting diode (OLED), wherein the semiconducting material comprises a tetrasubstituted pyrazine.
    Type: Application
    Filed: June 13, 2019
    Publication date: July 1, 2021
    Inventors: Elena Galan, Benjamin Schulze
  • Publication number: 20210198216
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: August 12, 2020
    Publication date: July 1, 2021
    Inventors: John M. MCCALL, Donna L. ROMERO, John MCKEARN, Michael CLARE
  • Publication number: 20210198217
    Abstract: The present invention relates to reagents which are suitable to be used in mass spectrometry as well as methods of mass spectrometric determination of analyte molecules using said reagents.
    Type: Application
    Filed: January 21, 2021
    Publication date: July 1, 2021
    Inventors: Dieter Heindl, Hans-Peter Josel, Uwe Kobold, Christoph Seidel, Martin Rempt, Andreas Leinenbach, Giuseppe Prencipe, Silvia Baecher, Simon Ferdinand Loibl, Anna-Skrollan Geiermann, Jelena Milic, Nicole Pirkl
  • Publication number: 20210198218
    Abstract: Chemical entities of Formula (I): Including enantiomers thereof, wherein R1 has any of the values described herein, and compositions comprising such chemical entities; their preparation; and their use in various methods, including the treatment of depression, pain, cognitive disorders, neurodegenerative disorders, and other neurological and peripheral disorders.
    Type: Application
    Filed: August 10, 2020
    Publication date: July 1, 2021
    Inventors: Laurent Gomez, Mark Eben Massari
  • Publication number: 20210198219
    Abstract: The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I) In the formula Q is O, R1 is the side chain of Ser, R2 is —CO-Thr, R3 is the side chain of Asn or Glu, and R4, R5 and R6 are each H.
    Type: Application
    Filed: March 4, 2021
    Publication date: July 1, 2021
    Applicant: Aurigene Discovery Technologies Limited
    Inventors: Pottayil Govindan Nair Sasikumar, Muralidhara Ramachandra, Seetharamaiah Setty Sudarshan Naremaddepalli
  • Publication number: 20210198220
    Abstract: The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 3, 2021
    Publication date: July 1, 2021
    Inventors: Zhi LUO, Xiaolin LI, Yaxun YANG, Lele YANG, Peng LI, Haiying HE, Jian LI, Shuhui CHEN