Patents Issued in June 2, 2022
  • Publication number: 20220169592
    Abstract: The invention relates to a continuously operating process for producing nitrobenzene, comprising the following steps: a) nitriding benzene in adiabatic conditions with sulfuric acid and nitric acid, using a stoichiometric excess of benzene in relation to the nitric acid; b) first separating a gaseous phase containing benzene and gaseous secondary components from the raw process product of the nitridation in a gas separator provided specifically for this purpose, then separating, in a downstream phase-separating apparatus, the resulting liquid phase, which is depleted in gaseous components and contains nitrobenzene and sulfuric acid, into a sulfuric acid phase and a nitrobenzene phase; and c) processing the nitrobenzene phase, obtaining nitrobenzene. The invention also relates to a production plant suitable for carrying out the claimed process.
    Type: Application
    Filed: April 14, 2020
    Publication date: June 2, 2022
    Inventors: Thomas Knauf, Murat Kalem, Christian Drumm, Alexandre Racoes
  • Publication number: 20220169593
    Abstract: The present disclosure provides for alkyl-aryl amine-rich small molecules that are prepared by nucleophilic substitution from tri- and hexa-bromine-substituted aromatic cores with various aliphatic diamines. The resulting products can be subsequently subjected by solution impregnation into solid mesoporous supports.
    Type: Application
    Filed: June 3, 2021
    Publication date: June 2, 2022
    Inventors: Christopher W. Jones, Dharam Raj Kumar, Eric W. Ping, Cornelia Rosu, Miles A. Sakwa-Novak, Achintya Sujan
  • Publication number: 20220169594
    Abstract: The present invention describes a new crystalline form of triethylenetetramine tetrachloride which has improved room temperature stability over known forms and over the dichloride salt. The new crystalline form is characterised by having peaks in an XRPD spectrum at 22.9, 25.4, 25.8, 26.6, 34.6 and 35.3±0.1° 2? and Raman shifts 943, 1173, 1527 and 1612±5 cm?1. The crystalline form of triethylenetetramine tetrachloride is useful in the treatment of Wilson's disease.
    Type: Application
    Filed: August 10, 2021
    Publication date: June 2, 2022
    Applicant: Orphalan S.A.
    Inventors: Timothy James Morley, Ronnie Maxwell Lawrence, Naseem Amin
  • Publication number: 20220169595
    Abstract: Disclosed are methods for preparing deuterated analogs of D-serine and compounds useful for preparing deuterated analogs of D-serine.
    Type: Application
    Filed: April 3, 2020
    Publication date: June 2, 2022
    Inventors: Adam Morgan, Robert S. Lewis
  • Publication number: 20220169596
    Abstract: The present invention relates to derivatives of 10-methylene lipids, their preparation and their use.
    Type: Application
    Filed: March 26, 2020
    Publication date: June 2, 2022
    Inventors: Jean-Christophe RABOIN, Henri STRUB
  • Publication number: 20220169597
    Abstract: The invention comprises a process for preparing mixtures of DEFI and amide taurate (ATA) having excellent yields of ATA and substantial absence of browning of final ATA and DEFI mixtures. The process permits much greater flexibility in ratios of DEFI to ATA. The invention further relates to mixtures prepared by processes of the invention.
    Type: Application
    Filed: February 16, 2022
    Publication date: June 2, 2022
    Applicant: Conopco, Inc., d/b/a UNILEVER
    Inventors: Van AU, Bijan HARICHIAN
  • Publication number: 20220169598
    Abstract: The present application relates to fluorinated benzylsulfonamide hydroxamic acid compounds of Formula I and/or pharmaceutically acceptable salt, solvate and/or prodrug thereof: (I) for use as a inhibitor of HDAC6. The application also relates to methods of treating a disease, disorder or condition using the compounds and compositions of the application.
    Type: Application
    Filed: March 27, 2020
    Publication date: June 2, 2022
    Inventors: Patrick T. Gunning, Olasunkanmi Olaoye, Krimo Toutah, Andrew E. Shouksmith, Justyna M. Shouksmith, Nabanita Nawar, Yasir S. Raouf
  • Publication number: 20220169599
    Abstract: The present invention provides new arylsulfonamide compounds having the general formula (I) wherein L, R1, R2, R3 and R4 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
    Type: Application
    Filed: February 15, 2022
    Publication date: June 2, 2022
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Barbara BIEMANS, Luca GOBBI, Georg JAESCHKE, Henner KNUST, Lothar LINDEMANN, Fionn O'HARA, Jean-Marc PLANCHER
  • Publication number: 20220169600
    Abstract: The present invention provides a method for producing a compound represented by Formula (1a), (1b), or (1c), comprising a step of reducing a compound represented by Formula (3) in the presence of a metal complex represented by Formula (5), an inorganic base, and a solvent under a hydrogen atmosphere to obtain a compound represented by Formula (4). In the formula, Ar1 is an aryl group, each Are is independently a phenyl group or the like, W is a biphenyl group or the like, Z is an ethylene group that is substituted with a phenyl group or the like, and L is a chlorine atom or if Z has a phenyl group or a C1-3 alkoxyphenyl group, L is one of carbon atoms constituting the phenyl group or the C1-3 alkoxyphenyl group.
    Type: Application
    Filed: February 21, 2020
    Publication date: June 2, 2022
    Applicant: KYOWA PHARMA CHEMICAL CO., LTD.
    Inventors: Tatsuhiro ASANO, Ryota MAENISHI, Junpei TAKENAKA, Takayuki ATAGO, Chihiro NARUMI
  • Publication number: 20220169601
    Abstract: The present invention relates to a process for synthesizing hydroperoxy alcohols by perhydrolysis of epoxides, using an aqueous solution of hydrogen peroxide, in the presence of a catalyst consisting of phosphotungstic acid.
    Type: Application
    Filed: February 20, 2020
    Publication date: June 2, 2022
    Inventors: CORENTIN BORDIER, VINCENT ESCANDE, FRÉDÉRIC CAIJO, CHRISTOPHE DARCEL
  • Publication number: 20220169602
    Abstract: The present invention relates to novel compounds, pharmaceutical compositions comprising such compounds and their use for treating, alleviating or preventing diseases or disorders relating to the activity of potassium channels.
    Type: Application
    Filed: March 20, 2020
    Publication date: June 2, 2022
    Inventors: David Tristram BROWN, Palle CHRISTOPHERSEN, Thomas Amos JACOBSEN, Janus S. LARSEN, Pernille Hartveit Poulsen, Dorte STRØBAEK
  • Publication number: 20220169603
    Abstract: Present invention relates to novel salts of saroglitazar and certain polymorphic forms of saroglitazar salts. Invention provides process for the preparation of novel salts and polymorphic forms of saroglitazar. Invention also provides novel co-precipitants or premixes of saroglitazar with pharmaceutically acceptable excipients/secondary therapeutic agent and process for the preparing same.
    Type: Application
    Filed: March 11, 2020
    Publication date: June 2, 2022
    Inventors: Rajiv Sharma, Sanjay Kumar, Brijesh Kumar Srivastava, Harikishore Pingali, Ranjeet Nair, Kalpesh Shah, Pandurang Zaware, Manoj Patel, Kamal Dave
  • Publication number: 20220169604
    Abstract: The present invention in general relates to the field of bioconjugation. More in particular, the invention relates to novel bioconjugation reactants based on an ?,? unsaturated ?-hydroxylactam structure, amongst others allowing a higher degree of functionalization compared to classical bioconjugation reactants such as maleimide. The present invention also provides methods of preparing the novel bioconjugation reactants, as well as uses thereof in human and/or veterinary medicine; and conjugation processes.
    Type: Application
    Filed: February 28, 2020
    Publication date: June 2, 2022
    Applicant: Universiteit Gent
    Inventors: Annemieke Madder, Ewout De Geyter, Eirini Antonatou, Sabina Smolen, Dimitris Kalaitzakis, Georgios Vassilikogiannakis
  • Publication number: 20220169605
    Abstract: The present invention relates to novel heterocyclic compounds of the general formula (I) their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers and polymorphs. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds and their use as the compounds of the invention belong to the family of NOD-like receptor family (NLR) protein NLRP3 modulators. The present invention thus relates to novel NLRP3 modulators as well as to the use of the novel inhibitor compounds in the treatment of diseases or conditions in which interleukin 1? activity is implicated.
    Type: Application
    Filed: January 13, 2020
    Publication date: June 2, 2022
    Inventors: Rajiv Sharma, Sameer Agarwal
  • Publication number: 20220169606
    Abstract: The present invention relates to compositions comprising compounds of formula I and II. These compositions have uses in the treatment of psychiatric or neurological disorders. Varying the relative amounts of the compounds of formula I and II within the compositions is expected to modulate the therapeutic effect. Related compounds of formula Ill comprise d3-monomethylamino or d6-dimethylamino groups and are useful internal standards for quantifying the amount of a target compound, such as an analogous compound comprising protio-monomethylamino or protio-dimethylamino groups. Thus, the present invention also relates to compounds of formula Ill and their uses as internal standards in assays for quantifying the amount of a target compound in a sample. A method of quantifying the amount of a target compound in a sample by adding a known amount of a compound of formula Ill to the sample is also included.
    Type: Application
    Filed: December 1, 2020
    Publication date: June 2, 2022
    Applicant: Small Pharma Ltd.
    Inventors: Peter Rands, Ellen James, Tiffanie Benway
  • Publication number: 20220169607
    Abstract: The present invention provides photocatalysts, methods for their preparation, and methods for preparing linear polymers with high propagation rate.
    Type: Application
    Filed: March 30, 2020
    Publication date: June 2, 2022
    Applicant: Colorado State University Research Foundation
    Inventors: Bonnie L. Buss, Garret Miyake, Chern-Hooi Lim, Max Kudisch
  • Publication number: 20220169608
    Abstract: A compound of the formula (1) exhibits high photoluminescence quantum yields, high radiative decay constant and low ASE thresholds from solution-processed neat and blend films. Ar1 and Ar2 are aryl groups, L is a divalent group having a group of the formula (2), and R is H or a diarylamino group. At least one alkyl group having at least five carbon atoms which are bonded is present in the formula (1).
    Type: Application
    Filed: June 5, 2020
    Publication date: June 2, 2022
    Inventors: Sangarange Don Atula SANDANAYAKA, Adikari Mudiyanselage Chathuranganie SENEVIRATHNE, Toshinori MATSUSHIMA, Chihaya ADACHI, Ebinazar Benjamin NAMDAS, Shih-Chun LO, Van T. N. MAI, Atul SHUKLA, Ilene ALLISON, Sarah K. MCGREGOR
  • Publication number: 20220169609
    Abstract: The present invention relates to carbazoles of general formula (I), and process for the preparation thereof: wherein ‘R1’ is H, C1-C6 alkyl, benzyl, or allyl; R2 is H, C1-C6 alkyl, cyclopropyl, phenyl, aryl, heteroaryl, or NO2; R3 is H, C1-C6 alkyl, cyclopropyl, phenyl aryl, heteroaryl, 4-methoxy phenyl, 4-ethyl phenyl, 2-methyl phenyl, or 2-Fluoro phenyl; R4 is H, benzoyl, —CO2Et, —CHO, Br, or —OMe; R5 is OH, OMOM, OMe, CN, or OTf; R6 is H, or O-alkyl; and R3-R4 is —CHNCH2CH2-. This invention also relates to the process for the preparation of carbazomycin A of Formula (1), calothrixin B of Formula (2) and staurosporinone of Formula (3) involving carbazoles of general formula (I) as an intermediate.
    Type: Application
    Filed: March 24, 2020
    Publication date: June 2, 2022
    Inventors: Srihari PABBARAJA, Goverdhan MEHTA, Ramesh SAMINENI, Shweta SINGH
  • Publication number: 20220169610
    Abstract: The disclosure is directed to, in part, compounds, or pharmaceutically acceptable salts or solvates thereof, for modulating the activity of aldehyde dehydrogenase such as ALDH2 and/or methods for treating and/or preventing an alcohol related disorder such as alcohol use disorder, alcohol induced disorder, alcohol abuse, alcohol dependence, alcohol intoxication, alcohol withdrawal, and the like and/or methods for reducing the amount of alcohol consumed, reducing alcoholic cravings, or increasing the percentage of no heavy drinking days for a subject with alcohol use disorder.
    Type: Application
    Filed: November 30, 2021
    Publication date: June 2, 2022
    Inventors: Lewis Feldberg, Akram Sabouni, Thomas R. Bailey, Vincent Wing-Fai Tai
  • Publication number: 20220169611
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: February 15, 2022
    Publication date: June 2, 2022
    Inventors: Michael D. Bartberger, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason A. Dequette, I, John Eksterowicz, Benjamin Fisher, Brian M. Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael W. Gribble, Darin J. Gustin, Julie A. Heath, Xin Huang, XianYun Jiao, Michael G. Johnson, Frank Kayser, David John Kopecky, SuJen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan D. Low, Brian S. Lucas, Zhihua Ma, Lawrence R. McGee, Josel McIntosh, Dustin L. McMinn, Julio C. Medina, Jeffrey Thomas Mihalic, Steven H. Olson, Yossup Rew, Philip M. Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
  • Publication number: 20220169612
    Abstract: The present disclosure is directed to chemical compounds and to the use of such compounds in the treatment of diseases associated with an adrenergic receptor. In certain embodiments of the methods disclosed herein, the methods include administering to the subject a compound as disclosed herein and a peripherally acting P-blocker (PABRA).
    Type: Application
    Filed: March 26, 2020
    Publication date: June 2, 2022
    Inventors: Anthony P. Ford, Wei Chen, David Scott Carter, Jiaxin Yu
  • Publication number: 20220169613
    Abstract: Compounds represented by formula (I) below and pharmacologically acceptable salts thereof and solvates of them; pharmaceutical compositions and dynamin-related protein 1 (Drp1)-filamin complex formation inhibitors containing them; and uses of the compounds, salts, solvates, pharmaceutical compositions, and (Drp1)-filamin complex formation inhibitors for use as a prophylactic or therapeutic agent.
    Type: Application
    Filed: May 26, 2020
    Publication date: June 2, 2022
    Inventors: Akio OJIDA, Naoya SHINDO, Akiyuki NISHIMURA, Motohiro NISHIDA
  • Publication number: 20220169614
    Abstract: The present invention is directed to new crystalline forms of Pitavastatin hemicalcium salt, referred to hereinafter as polymorphic Forms A, B, C, D, E and F, as well as the amorphous form. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and the amorphous form and pharmaceutical compositions comprising these crystalline forms or the amorphous forms.
    Type: Application
    Filed: February 18, 2022
    Publication date: June 2, 2022
    Applicant: NISSAN CHEMICAL CORPORATION
    Inventors: Paul Adriaan VAN DER SCHAAF, Fritz BLATTER, Martin SZELAGIEWICZ, Kai-Uwe SCHOENING
  • Publication number: 20220169615
    Abstract: The present disclosure relates to amorphous and crystalline forms of (R)-N-(4-chlorophenyl)-2-(1S,4S)-4-(6-fluoroquinolin-4-yl)cyclohexyl)propanamide and its salts and hydrates, processes for their production, pharmaceutical compositions comprising them, and methods of treatment using them.
    Type: Application
    Filed: December 16, 2021
    Publication date: June 2, 2022
    Inventors: Jay Patrick POWERS, Hilary Plake BECK, Maksim OSIPOV, Maureen Kay REILLY, Hunter Paul SHUNATONA, James Ross WALKER, Mikhail ZIBINSKY, Tamar ROSENBAUM, Ian Scott YOUNG, Jennifer NELSON, Petinka VLAHOVA
  • Publication number: 20220169616
    Abstract: The present invention relates to compounds of the general formula (I): (I), wherein V, W, M, R, R and Y have the designations cited below, or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof, and to processes for the preparation of compounds of the general formula (I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof. The invention also relates to compounds of the general formula (I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof for use as a medicament. Further, the invention relates to compounds of the general formula (I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof for use in the treatment of cancer. Moreover, the invention relates to compounds of the general formula (I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof for treating cancer in simultaneous, alternating or subsequent combination with another cancer therapy.
    Type: Application
    Filed: March 19, 2020
    Publication date: June 2, 2022
    Inventors: Raffaella Di Lucrezia, Tim Bergbrede, Peter Nussbaumer, Peter Schröder
  • Publication number: 20220169617
    Abstract: Disclosed are continuous processes for producing benzimidazole derivative Compound I comprising reduction of Compound 2 and reaction with valeraldehyde and conditions and apparatuses for the same.
    Type: Application
    Filed: March 12, 2020
    Publication date: June 2, 2022
    Applicant: HELSINN HEALTHCARE SA
    Inventors: Loïc JOST, Christophe ALLEMANN, Luca FADINI, Christophe VIGLIOTTA
  • Publication number: 20220169618
    Abstract: Described are substituted 2-heteroarylaminobenzenes of the general formula (I) and their use as herbicides, in particular for controlling broad-leaved weeds and/or weed grasses in crops of useful plants and/or as plant growth regulators for influencing the growth of crops of useful plants. The present invention further relates to herbicidal and/or plant growth-regulating compositions comprising one or more compounds of the general formula (I).
    Type: Application
    Filed: March 23, 2020
    Publication date: June 2, 2022
    Applicant: Bayer Aktiengesellschaft
    Inventors: Ralf BRAUN, Michael Charles MCLEOD, Alexandra MANOS-TURVEY, David Michael BARBER, Harald JAKOBI, Dirk SCHMUTZLER, Anu Bheemaiah MACHETTIRA, Elisabeth ASMUS
  • Publication number: 20220169619
    Abstract: Disclosed is crystal form M of the proline hydroxylase inhibitor daprodustat, wherein the X-ray powder diffraction thereof, expressed in 2? angles and using Cu-Ka radiation, has characteristic peaks at 4.7±0.2°, 6.5±0.2°, and 6.8±0.2°. Disclosed are the preparation method for and the use of crystal form M. The crystal form M has good light stability, high temperature stability and high humidity stability, good solubility, and high purity.
    Type: Application
    Filed: February 18, 2022
    Publication date: June 2, 2022
    Inventors: Guobin Ren, Weijie Ji, Dongxu Yi, Jiajun Huang
  • Publication number: 20220169620
    Abstract: The present invention is directed to spiro-cyclic amine derivatives which are modulators of S1P receptors and are useful in the treatment of CNS disorders.
    Type: Application
    Filed: November 30, 2021
    Publication date: June 2, 2022
    Inventors: Willie Amberg, Gisela Backfisch, Karen Bodié, Katja Hempel, Loic Laplanche, Mario Mezler, Michael Ochse, Sean Turner, Jeroen van Bergeijk, Elizabeth van der Kam
  • Publication number: 20220169621
    Abstract: The present invention relates to novel oxadiazoles of Formula I. wherein, R1, L1, A, L2 and R10 are as defined in the detailed description.
    Type: Application
    Filed: February 17, 2022
    Publication date: June 2, 2022
    Applicant: PI INDUSTRIES LTD.
    Inventors: Paras Raybhan Bhujade, Rajesh Pawar, Maruti N. Naik, Rajender Kumar Potlapally, Nitin Ramesh Tembhare, Santosh Shridhar Autkar, Ruchi Garg, Hagalavadi M. Venkatesha, Alexander G.M. Klausener, Visannagari Ramakrishna, Nilesh Bharat Adhav, Pooja Trivedi
  • Publication number: 20220169622
    Abstract: Provided herein is technology relating to amplification of nucleic acids and particularly, but not exclusively, to compositions and methods for doing improving the polymerase chain reaction and providing reagents for polymerase chain reaction with improved stability.
    Type: Application
    Filed: February 15, 2022
    Publication date: June 2, 2022
    Inventors: Tomasz Krupinski, Jeffrey D. Wuitschick, Shihai Huang
  • Publication number: 20220169623
    Abstract: A reaction of azacyclopropane derivative with elemental selenium and TMSCN to construct a selenium-containing heterocycle under metal-free and additive-free conditions is provided. The new strategy features no metal participation, no additive promotion, a wide substrate selection range and a good functional group compatibility, and provides an efficient and green approach to constructing a variety of selenium-containing heterocyclic compounds in a highly concise way.
    Type: Application
    Filed: November 16, 2021
    Publication date: June 2, 2022
    Inventors: Miaochang Liu, Liguo Lu, Chuanli Chen, Yunbing Zhou, Huayue Wu
  • Publication number: 20220169624
    Abstract: Processes and systems for producing olefin epoxides with three or more carbon atoms by oxidation of the corresponding branched hydrocarbons using oxygen are disclosed. An example process for producing olefin epoxides may include oxidizing a branched alkane to produce at least an organic hydroperoxide. The example process may further include epoxidizing a branched alkene by a catalytic reaction with least a portion of the organic hydroperoxide to produce at least an olefin epoxide and an alcohol. The example process may further include converting at least a portion of the alcohol to either additional branched alkane and/or additional branched alkene.
    Type: Application
    Filed: June 30, 2020
    Publication date: June 2, 2022
    Inventors: Kun Wang, Timothy D. Shaffer
  • Publication number: 20220169625
    Abstract: A method may include: oxidizing iso-butane with oxygen to produce t-butyl hydroperoxide and t-butyl alcohol; dehydrating at least a portion of the t-butyl alcohol to produce di-tert-butyl ether and isobutylene; epoxidizing at least a portion of the isobutylene with the t-butyl hydroperoxide to produce isobutylene oxide and t-butyl alcohol; and carbonylating at least a portion of the isobutylene oxide with carbon monoxide to produce pivalolactone.
    Type: Application
    Filed: July 2, 2020
    Publication date: June 2, 2022
    Inventors: Kun Wang, Timothy D. Shaffer
  • Publication number: 20220169626
    Abstract: A cannabichromene derivative, cannabichromene-o-acetate, synthesis, compositions comprising the same, and methods of use.
    Type: Application
    Filed: November 29, 2021
    Publication date: June 2, 2022
    Applicant: Marquette Analytica
    Inventor: Robert Opperman
  • Publication number: 20220169627
    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: June 18, 2021
    Publication date: June 2, 2022
    Inventors: Thomas Butler, Jim Palmer, Ravi Upasani, Matthew Welsch, Sridhar Vempati, Brendan Kelly, Edward Painter
  • Publication number: 20220169628
    Abstract: The invention is directed towards compounds (e.g., Formula (I)), their mechanism of action, and methods of modulating proliferation activity, and methods of treating diseases and disorders using the compounds described herein (e.g., Formula (I)).
    Type: Application
    Filed: February 7, 2020
    Publication date: June 2, 2022
    Applicant: University of Florida Research Foundation, Incorporated
    Inventors: Guangrong Zheng, Daohong Zhou, Pratik Pal, Xingui Liu, Dinesh Thummuri, Wanyi HU, Peiyi Zhang, Dongwen Lyu, Yaxia Yuan, Xuan Zhang
  • Publication number: 20220169629
    Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides.
    Type: Application
    Filed: April 7, 2020
    Publication date: June 2, 2022
    Applicant: SYNGENTA CROP PROTECTION AG
    Inventors: Jurgen Harry SCHAETZER, Andrew EDMUNDS, Julien Daniel Henri GAGNEPAIN, Roger Graham HALL, Andre JEANGUENAT, Amandine KOLLETH KRIEGER, Camille LE CHAPELAIN, Shrikant PALWE, Mangala PHADTE, Thomas PITTERNA, Sebastian RENDLER, Christopher Charles SCARBOROUGH
  • Publication number: 20220169630
    Abstract: The present invention relates to a method of synthesizing a compound of formula (I) also referred to as 4-(((2S,4S)-(4-ethoxy-1-(((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl))benzoic acid, or a pharmaceutically acceptable salt thereof, and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 9, 2021
    Publication date: June 2, 2022
    Inventors: Peng FU, Yu GAI, Feng GAO, Weiyong KONG, Yadong LU, Zhongcheng MIN, Shaofeng RONG, Chutian SHU, Can WANG, Ruidong WANG, Jibin ZHAO, Xianglin ZHAO, Yi ZHAO, Jianguang ZHOU, Benjamin MARTIN
  • Publication number: 20220169631
    Abstract: Provided herein are compounds of Formula (I?) or (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing diseases (e.g., proliferative diseases (e.g., cancers (e.g., carcinoma); lung cancer, breast cancer, liver cancer, pancreatic cancer, gastric cancer, ovarian cancer, colon cancer, colorectal cancer)), metabolic disorders (e.g., diabetes), autoimmune diseases, and neurological diseases (e.g., Alzheimer's disease, gliosis, spinal cord injury)) in a subject, as well as for male contraception (e.g., reducing or inhibiting spermatogenesis, or reducing the rate of male fertility in a healthy fertile male subject). Provided are methods of inhibiting a CDK (e.g., CDK14, CDK15, CDK16, CDK17, CDK18) in a subject.
    Type: Application
    Filed: June 24, 2019
    Publication date: June 2, 2022
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Fleur M. Ferguson, Zainab M. Doctor
  • Publication number: 20220169632
    Abstract: This document provides methods and materials for increasing or maintaining NMNAT2 polypeptide levels within cells. For example, compounds (e.g., organic compounds) having the ability to increase or maintain NMNAT2 polypeptide levels within cells, formulations containing compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for making compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for making formulations containing compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for increasing or maintain NMNAT2 polypeptide levels within cells, and methods for treating mammals (e.g., humans) having a condition responsive to an increase in NMNAT2 polypeptide levels are provided (or for preventing said condition).
    Type: Application
    Filed: February 21, 2020
    Publication date: June 2, 2022
    Inventors: Beibei Chen, Toren Finkel, Yuan Liu
  • Publication number: 20220169633
    Abstract: A squarylium compound has high transmittance in a visible wavelength spectrum of light and is configured to selectively absorb light in an infrared/near infrared wavelength spectrum of light.
    Type: Application
    Filed: February 17, 2022
    Publication date: June 2, 2022
    Applicant: Samsung Electronics Co., Ltd.
    Inventors: Moon Gyu HAN, Kyung Bae PARK, Dongseon LEE, Yong Wan JIN, Chul Joon HEO
  • Publication number: 20220169634
    Abstract: The present disclosure relates generally to aromatic derivatives that are inhibitors of FGFR4 and are useful in treating FGFR4-associated diseases or conditions. Compositions containing the compounds of the present disclosure are also provided.
    Type: Application
    Filed: February 19, 2020
    Publication date: June 2, 2022
    Inventors: Ding WANG, Ning SHAO, Hongbin YUAN, Frank KAYSER
  • Publication number: 20220169635
    Abstract: Disclosed herein are plinabulin polymorphs, compositions, their use and preparation as therapeutic agents. In particular, some embodiments relate to plinabulin monohydrate in a crystalline form.
    Type: Application
    Filed: February 18, 2022
    Publication date: June 2, 2022
    Inventors: Lan Huang, Aniruddh Singh
  • Publication number: 20220169636
    Abstract: The present invention provides compounds of the Formula or a pharmaceutically acceptable salt thereof, and compounds processes for preparing the compounds and their salts, and a pharmaceutical composition.
    Type: Application
    Filed: February 15, 2022
    Publication date: June 2, 2022
    Inventors: Celia Lafuente BLANCO, Nuria Diaz BUEZO, Jose Antonio Martinez PEREZ, Gema Consuelo SANZ GIL, Julian Priego SOLER
  • Publication number: 20220169637
    Abstract: Aspects of the present application relate to solid forms of Encequidar, its mesylate salt and pharmaceutical compositions thereof. Specific aspects relate to the crystalline Form E1 of Encequidar, crystalline Form EM1, crystalline Form EM2 and crystalline Form EM3 of Encequidar mesylate. Further aspects relate to processes for the preparation of solid forms of Encequidar and its mesylate salt.
    Type: Application
    Filed: March 24, 2020
    Publication date: June 2, 2022
    Inventors: Srinivas ORUGANTI, Vishnu Vardhana Vema Reddy EDA, Saikat SEN, Arijit MUKHERJEE, Satyanarayana THIRUNAHARI
  • Publication number: 20220169638
    Abstract: This invention relates to the compound (2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide, and in particular to novel physical forms of the compound, a process for preparing the compound and synthetic intermediates for use in the process, and novel formulations containing the compound, as well as therapeutic uses of the compound.
    Type: Application
    Filed: September 1, 2021
    Publication date: June 2, 2022
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Michael READER, Nicola Elizabeth WILSHER, Mark Henry SAUNDERS, Paul Anthony BAGULEY, Colin Thomas LINDLEY, Robert Craig MELLING, Bozena Ewa ADAMCZYK, Mirka SCARATI
  • Publication number: 20220169639
    Abstract: The present invention provides the compounds having the general formula: (I) wherein R1 to R8, and X are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: December 11, 2019
    Publication date: June 2, 2022
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Song FENG, Jiamin ZHENG, Yongfu LIU, Dongdong CHEN, Hong SHEN, Xuefei TAN
  • Publication number: 20220169640
    Abstract: Provided is a method for industrially advantageously synthesizing a production intermediate of a quinolinecarboxamide derivative or a salt thereof. The present invention provides a method for producing a quinolinecarboxylic acid derivative of formula (4) or a salt thereof, including reacting an aniline of the following formula (1), in the presence of boron trifluoride-tetrahydrofuran complex or boron trifluoride-diethyl ether complex, with an aldehyde of formula (2) and subsequently reacting the resulting compound with an ?-keto acid of formula (3), wherein R1, R2, R3 and R4 are the same or different and each represent a hydrogen atom, a halogen atom, a lower alkyl group, or the like, R5 represents a hydrogen atom, a lower alkyl group, or the like, and R6 represents a hydrogen atom, a lower alkyl group, or the like.
    Type: Application
    Filed: March 19, 2020
    Publication date: June 2, 2022
    Applicant: KABUSHIKI KAISHA YAKULT HONSHA
    Inventors: Takahide SHIGEYAMA, Takuya SUGIMOTO, Hideyuki KOMATSU, Hiroyuki NISHIYAMA
  • Publication number: 20220169641
    Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating renal diseases are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.
    Type: Application
    Filed: August 11, 2021
    Publication date: June 2, 2022
    Inventors: Adnan M.M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta