Patents Issued in January 9, 2020
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Publication number: 20200010387Abstract: A process for isolating pure 1,3-butadiene from a crude C4 fraction, which produces pure 1,3-butadiene having a prescribed maximum content of at least one low boiler and a prescribed maximum content of 1,2-butadiene, in each case based on 1,3-butadiene, wherein (a) a low boiler fraction and a high boiler fraction are separated off by distillation from the crude C4 fraction, giving a purified C4 fraction whose content of the at least one low boiler, based on 1,3-butadiene, is equal to or lower than the prescribed maximum content of the at least one low boiler and whose content of 1,2-butadiene, based on 1,3-butadiene, is equal to or lower than the prescribed maximum content of 1,2-butadiene; (b) the purified C4 fraction is subjected to at least one extractive distillation using a selective solvent, giving at least a fraction comprising butanes and butenes and a pure 1,3-butadiene fraction, is described. The process makes a pure distillation column dispensable.Type: ApplicationFiled: March 12, 2018Publication date: January 9, 2020Applicant: BASF SEInventors: Bernd HEIDA, Tobias KELLER
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Publication number: 20200010388Abstract: A manufacturing method of 1-chloro-3,3,3-trifluoropropene (1233zd) is provided. This manufacturing method includes a reaction in which a halogenated hydrocarbon compound having a carbon number of 3 and represented by a general formula (1) is heated: CFaCl3-a—CH2—CHFbCl2-b??(1) In the formula, a is an integer from 0 to 2, b is 1 or 2 when a=0, b is 0 or 1 when a=1, and b is 0 when a=2.Type: ApplicationFiled: September 17, 2019Publication date: January 9, 2020Inventors: Masamune OKAMOTO, Kohei SUMIDA, Kei MATSUNAGA, Yoshio NISHIGUCHI, Satoru OKAMOTO
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Publication number: 20200010389Abstract: According to a method for producing a perfluoroalkadiene compound represented by general formula (1): CF2?CF—(CF2)n-4—CF?CF2 (1), wherein n is an integer of 4 or more, the method comprising a reaction step of adding a nitrogen-containing compound to a solution of a compound represented by general formula (2): X1CF2—CFX2—(CF2)n-4—CF2X1 (2), wherein n is the same as above, X1 is the same or different and is a halogen atom other than fluorine, and X2 is a halogen atom, the perfluoroalkadiene compound can be obtained at a high yield.Type: ApplicationFiled: February 2, 2018Publication date: January 9, 2020Applicant: DAIKIN INDUSTRIES, LTD.Inventors: Yuusuke ETOU, Atsushi MARUO, Katsuya NAKAI, Kazuhiro TAKAHASHI
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Publication number: 20200010390Abstract: The present invention provides an improved process for preparation of 2,3,3,3- tetrafluoropropene, wherein recyclization of the reaction by-products result in equilibrium between feed and outlet composition.Type: ApplicationFiled: November 24, 2017Publication date: January 9, 2020Applicant: SRF LimitedInventors: Jose George, Sunil Raj, Ambuj Mishra, Anurag Katiyar, Rajdeep Anand
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Publication number: 20200010391Abstract: The invention relates to a method for the synthesis of 9,10-bis(chloromethyl)anthracene, comprising the mixing of the reagents, anthracene and 1,3,5-trioxane, a phase transfer catalyst selected from the group comprising quarternary ammonium salt and crown ether with hydrochloric acid and acetic acid.Type: ApplicationFiled: September 18, 2019Publication date: January 9, 2020Inventors: Francisco José ORTEGA HIGUERUELO, Fernando LANGA DE LA PUENTE
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Publication number: 20200010392Abstract: Aspects of the invention relate to systems and processes for recovering R1233zd in purified form from compositions additionally comprising hydrogen fluoride. In accordance with one aspect, the invention provides a process that includes separating a feed stream comprised of hydrogen fluoride and R1233zd using azeotropic distillation in a first distillation column to produce a first distillate stream comprised of hydrogen fluoride and R1233zd and a first bottoms stream consisting essentially of hydrogen fluoride. The first distillation column is operated at a first pressure. The process further includes separating the first distillate stream using azeotropic distillation in a second distillation column to produce a second distillate stream comprised of hydrogen fluoride and R1233zd and a second bottoms stream consisting essentially of R1233zd. The second distillation column is operated at a second pressure that may be different than the first pressure of the first distillation column.Type: ApplicationFiled: December 14, 2017Publication date: January 9, 2020Inventors: Jay F. Miller, John A. Wismer (Deceased)
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Publication number: 20200010393Abstract: Process for the preparation of alpha, beta unsaturated aldehydes by oxidation of alcohols in the presence of a liquid phase wherein the liquid phase contains 0.1 to less than 25 weight-% water and wherein the liquid phase contains at least 25 weight-% of alcohol(s) of general formula (II) and alpha, beta unsaturated aldehyde(s) of general formula (I) and wherein the oxidant is oxygen and/or hydrogen peroxide.Type: ApplicationFiled: March 12, 2018Publication date: January 9, 2020Inventors: Nicolas VAUTRAVERS, Joaquim Henrique TELES, Andreas Keller, Kirsten BRAUNSMANN, Andreas Jorg UFER, Stefan BAUER, Vera LUENSE, Marco BOSCH, Joseph John ZAKZESKI, Michaela FENYN
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Publication number: 20200010394Abstract: Method for preparing 1-hydroxy-2-methyl-3-pentanone (I) by reacting formaldehyde with diethyl ketone in a reactor in the presence of water and a basic component at a temperature of 50 to 150° C. and a pressure of 0.2 to 10 MPa abs, in which the basic component used is a trialkylamine from the group comprising trimethylamine, N,N-dimethylethylamine, N,N-diethylmethylamine, triethylamine, N,N-dimethyl-n-propylamine, N-ethyl-N-methyl-n-propylamine, N,N-dimethylisopropylamine, N-ethyl-N-methylisopropylamine, N,N-dimethyl-n-butylamine, N,N-dimethylisobutylamine and N,N-dimethyl-sec-butylamine, and from the reaction mixture obtained, trialkylamine as low boiler and a bottom product comprising 1-hydroxy-2-methyl-3-pentanone (I) as high boiler are separated in a distillation apparatus, wherein the distillation apparatus is operated at a top pressure of 0.2 to 1 MPa abs.Type: ApplicationFiled: July 2, 2019Publication date: January 9, 2020Inventors: Dagmar Pascale KUNSMANN-KEITEL, Georg Heinrich GROSCH, Jan-Dirk ARNDT, Gauthier Luc Maruice AVERLANT, Wolf-Steffen WEISSKER, Marcus Georg SCHREMS, Dan-Tam Daniel TANG
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Publication number: 20200010395Abstract: Method for preparing a ?-hydroxyketone having 4 to 8 carbon atoms by reacting formaldehyde with a branched or unbranched dialkyl ketone having 3 to 7 carbon atoms in the liquid phase in a reactor in the presence of a basic component at a temperature of 50 to 150° C. and a pressure of 0.2 to 10 MPa abs, in which (a) a trialkylamine having 1 to 4 carbon atoms per alkyl group is used as basic component and the reaction (b) is carried out in the presence of 1 to 25% by weight water, based on the liquid phase, and (c) at a molar ratio of trialkylamine to formaldehyde in the liquid phase of from 1 to 5.Type: ApplicationFiled: July 2, 2019Publication date: January 9, 2020Inventors: Dagmar Pascale KUNSMANN-KEITEL, Georg Heinrich GROSCH, Jan-Dirk ARNDT, Gauthier Luc Maruice AVERLANT, Wolf-Steffen WEISSKER, Marcus Georg SCHREMS, Dan-Tam Daniel TANG
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Publication number: 20200010396Abstract: Synthetic kava analog compounds of formula I are disclosed. Specifically, kava analogs of the structural type 3-oxoclclohex-1-en-1-yl benzoates, and corresponding benzamides are disclosed. The compounds of the within invention are useful in the inhibition of cytokine TNF-?, the management of chronic inflammation such as but not limited to Porphyromonas gingivalis induced periodontitis, and in infective arthritis, either as compounds, pharmaceutically acceptable salts (when appropriate), pharmaceutical composition ingredients, whether or not in combination with other anti-inflammatory active pharmaceutical ingredients. Methods of treating chronic inflammation such as periodontitis and infective arthritis are also disclosed.Type: ApplicationFiled: July 3, 2019Publication date: January 9, 2020Inventor: Salomon Amar
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Publication number: 20200010397Abstract: The present invention provides a process for preparation of halo substituted benzoic acid compound of Formula (1) and intermediates thereof.Type: ApplicationFiled: March 7, 2018Publication date: January 9, 2020Inventors: Amardeep Singh, Bhupender Singh, Kapil Kumar, Rajdeep Anand
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Publication number: 20200010398Abstract: The invention describes novel mono-hydroxy, di-hydroxy and tri-hydroxy docosapentaenoic acid (DPA) analogues, their preparation, isolation, identification, purification and uses thereof.Type: ApplicationFiled: August 26, 2019Publication date: January 9, 2020Inventors: Charles N. SERHAN, Jesmond DALLI
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Publication number: 20200010399Abstract: A method for the manufacture of a diester of terephthalic acid includes reacting terephthalic acid and a C6-18 alkyl monohydric alcohol in the presence of a catalyst having the formula MO[CH3COCH?C(0-)CH3]2 wherein M=Ti, Zr, or Hf, under conditions effective to form a reaction mixture comprising the di(C6-18 alkyl) terephthalate.Type: ApplicationFiled: March 15, 2018Publication date: January 9, 2020Inventors: Ritesh Nandy, Vishal Patrick, Edward Joseph Nesakumar
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Publication number: 20200010400Abstract: The invention relates to an integrated process for the production of ethylene and vinyl acetate (VAM), comprising contacting in a first reaction zone a gas stream comprising ethane and optionally ethylene with an oxygen-containing gas stream in the presence of a oxydehydrogenation catalyst under oxidative dehydrogenation conditions to produce a first product stream comprising ethane, ethylene, acetic acid and water, and optionally other compounds, separating said first product stream in a vapor permeation unit into a second stream comprising water and a third stream comprising ethane, ethylene, acetic acid, and optionally other gaseous compounds, contacting in a second reaction zone all or at least a portion of said third stream with a stream comprising concentrated acetic acid and with an oxygen-containing gas stream in the presence of a VAM catalyst, to produce a fourth product stream comprising vinyl acetate, acetic acid, ethane, ethylene, water, carbon dioxide, and optionally other compounds, separating sType: ApplicationFiled: December 18, 2017Publication date: January 9, 2020Inventor: Jean Paul Andre Marie Joseph Ghislain LANGE
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Publication number: 20200010401Abstract: The present invention relates to a method for preparing dialkyl dicarbonates from the corresponding alkyl chloroformates using specific amine oxides as catalysts.Type: ApplicationFiled: June 25, 2019Publication date: January 9, 2020Applicant: LANXESS Deutschland GmbHInventor: Christoph HOFMANN
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Publication number: 20200010402Abstract: A fragrance mixture and its applications, in particular perfume oils, cosmetic agents, application agents or washing and cleaning agents, containing a sensory effective amount of (i) (E)-2-methyl-but-2-endicarboxylic acid diethyl ester, (ii) (Z)-2-methyl-but-2-endicarboxylic acid diethyl ester or (iii) 2-methylenebutanedicarboxylic acid diethyl ester and mixtures thereof and analogous esters derived from these compounds and mixtures.Type: ApplicationFiled: September 27, 2017Publication date: January 9, 2020Inventors: Vijayanand Chandrasekaran, Johannes Panten, Oskar Koch, Edison Diaz Gomez
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Publication number: 20200010403Abstract: Provided are the crystalline form of tefluthrin of formula (I), the crystal preparation process, the analyses of the crystal through various analytical methods and using the crystal to prepare stable agrochemical formulation. Also provided is the use of various solvents towards the crystalline form preparation conditions.Type: ApplicationFiled: November 28, 2017Publication date: January 9, 2020Applicant: JIANGSU ROTAM CHEMISTRY CO., LTDInventor: James Timothy BRISTOW
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Publication number: 20200010404Abstract: A nickel diatomaceous earth catalyst having a weight loss rate measured by hydrogen-TG at 400 to 600° C. of 0.05 to 2.0%.Type: ApplicationFiled: September 18, 2019Publication date: January 9, 2020Applicant: Mitsubishi Gas Chemical Company, Inc.Inventors: Kouji Suzuki, Hajime Yamada
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Publication number: 20200010405Abstract: Methods of preparing a polyaspartic ester composition comprise reacting a primary diamine reactant composition with a diester reactant composition under conditions to prepare a polyaspartic ester composition having a primary amine value of less than 35 mg KOH/g wherein, at the time of the reaction, the combined water content of the primary diamine reactant composition and the diester reactant composition is less than 300 ppm. Compositions and methods of use of the compositions are also described.Type: ApplicationFiled: March 2, 2018Publication date: January 9, 2020Applicant: CARGILL, INCORPORATEDInventors: Andrew M. KARL, Todd L. KURTH
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Publication number: 20200010406Abstract: It is provided a process for the preparation of bimatoprost, which comprises: a) reacting a compound of formula (III) with ethylamine in the presence of a suitable solvent; and b) deprotecting compound obtained in step a) to obtain bimatoprost, wherein R1 is selected from (C1-C16)alkyl, (C1C16)haloalkyl, (C2-C16)alkenyl, (C2-C16)haloalkenyl, (C1-C16)alkoxy(C1-C16)alkyl, aryl, (C1-C16)alkylaryl, allyl, —(CH2—CH2—O)n—CH3 wherein n=1, 2, 3 or 4, and —CH(O—CH2—CH2)2; R2 is selected from H, (C1-C16)alkyl, (C1-C16)haloalkyl, (C2-C16)alkenyl, (C2-C16)haloalkenyl, (C1-C16)alkoxy(CrC16)alkyl, aryl, (C1-C16)alkylaryl, allyl; or, alternatively, R1 and R2 taken together are selected from —CH2—CH2—CH2—, —CH2—CH2—, —O—CH2—CH2—, and —O—CH?CH—. There are also provided intermediates useful in such preparation process.Type: ApplicationFiled: April 18, 2017Publication date: January 9, 2020Inventors: Luis Octavio SILVA GUISASOLA, Joaquín NEBOT TROYANO, Jordi RIPOLL ALTADILL
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Publication number: 20200010407Abstract: The present invention relates to pyrimidine hydroxy amide compounds, the use of such compounds in the inhibition of HDAC6, and the use of such compounds in the treatment of various diseases, disorders, or conditions related to HDAC6.Type: ApplicationFiled: July 19, 2019Publication date: January 9, 2020Inventors: John H. van Duzer, Ralph Mazitschek
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Publication number: 20200010408Abstract: The present invention relates to a process for the synthesis of mono-protected ?,?-diamino alkanes, the use of said process in a process for the synthesis of a linker drug comprising an ?,?-diamino alkane moiety and the use of the process of the present invention in a process for preparing an antibody-drug conjugate comprising an ?,?-diamino alkane moiety.Type: ApplicationFiled: November 3, 2017Publication date: January 9, 2020Inventor: Wiro Michael Petrus Bernardus MENGE
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Publication number: 20200010409Abstract: The present invention relates compounds useful as reagents for the diazomethylation reaction, their preparation and the use thereof as reagents in a method for the diazomethylation reaction of aromatic substrates. It relates in particular to a compound of formula (I) wherein E is an electron withdrawing group.Type: ApplicationFiled: February 8, 2018Publication date: January 9, 2020Inventors: Marcos GARCÍA SUERO, Zhaofeng WANG
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Publication number: 20200010410Abstract: A bis-urea compound of general formula (IV): The compound is useful as a thermo-thickening agent in a non-polar liquid such as engine lubricating oil or thermosetting varnish. Also, a method for preparing the thermo-thickening compound. Further, a composition comprising the thermo-thickening compound and a non-polar liquid.Type: ApplicationFiled: December 12, 2017Publication date: January 9, 2020Applicants: SORBONNE UNIVERSITE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Virgile AYZAC, Laurent BOUTEILLER, Matthieu RAYNAL, Benjamin ISARE
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Publication number: 20200010411Abstract: There are provided, inter alia, compositions and methods for covalently binding peptides to proteins.Type: ApplicationFiled: March 16, 2017Publication date: January 9, 2020Inventors: Lei Wang, Christian Hoppmann
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Publication number: 20200010412Abstract: Provided is a process for preparing polythiols by preparing a sulfhydration reaction medium, simultaneously carrying out radical sulfhydration reaction of at least one polyene and acid-catalyzed sulfhydration reaction of the polyene and recovering a mixture including at least two polythiols. Also provided is a mixture of polythiols obtained from the process described herein.Type: ApplicationFiled: February 6, 2018Publication date: January 9, 2020Applicant: Arkema FranceInventors: Pascal Saint-Louis-Augustin, Georges Fremy, Bernard Monguillon, Louis Corbel
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Publication number: 20200010413Abstract: The present invention benzoquinone derivatives of the formula (I): and to pharmaceutically acceptable salts or solvates thereof. In formula (I) one of X or Y is hydrogen and the other one of X or Y is 3-Trifluoro-methylaniline; 3,4,5-trifluoroaniline; 4-methoxylaniline; 4-fluoroaniline; 3,3?-Dimethyl-1,1?-Biphenyl-4,4?-diamine; 2-(pyrrolidin-1-yl)ethyl)amine; 4-trifluoromethyl-benzylamine; 4-fluorobenzyl-amine; 3,4-dimethoxybenzylamine; or 3,5-ditrifluoromethyl-benzylamine. Compounds of formula (I) have been identified as being useful in the treatment of cancer, in particular lung, breast and pancreatic cancer. The invention relates also to a method of making the benzoquinone derivatives and to methods of treatment.Type: ApplicationFiled: September 24, 2019Publication date: January 9, 2020Inventors: Alaa Eldin Salem, Ibrahim Abdou, Ismail El Haty
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Publication number: 20200010414Abstract: The present invention concerns a compound of following formula (1): where: —R1 is H or OH, —R2 is a (C1-C6)alkyl, COOH, COO—((C1-C6)alkyl) or thiazolyl group, —R3 is H or a (C1-C6)alkyl group, and —R4 is: ?a straight-chain or branched, saturated or unsaturated hydrocarbon group having 1 to 8 carbon atoms substituted by one or more groups chosen from among OH and NR5R6, ?—(CH2CH2X1)(CH2CH2X2)a2(CH2CH2X3)a3(CH2CH2X4)a4(CH2CH2X5)a5R7, ?an aryl-(C1-C8)alkyl group substituted by one N or more groups chosen from among OH and NR9R10 groups, or ?a heterocycle-(C1-C8)alkyl group optionally substituted by one or C more groups chosen from among (C1-C6)alkyl, OH and NR12R13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.Type: ApplicationFiled: May 30, 2019Publication date: January 9, 2020Applicant: PIERRE FABRE MEDICAMENTInventors: Michel PEREZ, Ian RILATT, Marie LAMOTHE
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Publication number: 20200010415Abstract: Provided is a compound having a formyl peptide receptor like 1 (FPRL1) agonist effect. The present invention relates to a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. The present invention also relates to a pharmaceutical composition containing the compound represented by the general formula (I) or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: September 24, 2019Publication date: January 9, 2020Inventors: Hiroyasu Takahashi, Yoshifumi Saito, Kosuke Tsuda, Mitsuhito Shibasaki, Kohei Ohata
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Publication number: 20200010416Abstract: The present disclosure is directed to novel forms of apremilast and pharmaceutical compositions comprising any of the novel forms of apremilast. Also provided are processes for the preparation of novel forms of apremilast.Type: ApplicationFiled: August 29, 2019Publication date: January 9, 2020Applicant: Johnson Matthey Public Limited CompanyInventor: Padmini KAVURU
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Publication number: 20200010417Abstract: Provided are compounds that target the nucleotide-binding oligomerization domain, leucine rich repeat containing X1 (NLRX1) pathway. The compounds can be used to treat multiple conditions, including inflammatory, immune-mediated, and/or chronic inflammatory gastrointestinal diseases; systemic immune-mediated diseases; cancers; and infectious diseases.Type: ApplicationFiled: July 2, 2019Publication date: January 9, 2020Applicant: Landos Biopharma, Inc.Inventors: Josep Bassaganya-Riera, Andrew Leber, Raquel Hontecillas
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Publication number: 20200010418Abstract: The present application relates to compounds comprising an ester, a thioester, or a hydrazide moiety and methods of synthesizing these compounds. The present application also relates to pharmaceutical compositions containing the compounds and methods of treating cell proliferative disorders mediated by the Hh signaling pathway, such as cancer, by administering the compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: September 19, 2019Publication date: January 9, 2020Inventors: James BRADNER, Michael ERB, Jun QI
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NANOHOOP COMPOUND EMBODIMENTS COMPRISING META-SUBSTITUTION AND MOLECULAR SYSTEMS COMPRISING THE SAME
Publication number: 20200010419Abstract: Disclosed herein are embodiments of nanohoop compounds, methods of making, and methods of using the same. The nanohoop compounds disclosed herein have discrete ring system(s) that comprise a unique meta-substituted motif that affords a strained cavity in which myriad reaction chemistries can take place. The unique structures and properties of the nanohoop compounds disclosed herein also lend to their use in a variety of biological applications, and as interlocked structures in molecular machines.Type: ApplicationFiled: July 8, 2019Publication date: January 9, 2020Inventors: Ramesh Jasti, Jeff Van Raden -
Publication number: 20200010420Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.Type: ApplicationFiled: September 18, 2019Publication date: January 9, 2020Applicants: GENENTECH, INC., CURIS, INC.Inventors: Janet L. GUNZNER-TOSTE, Daniel SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
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Publication number: 20200010421Abstract: The invention is directed to compounds of general formula (I) and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.Type: ApplicationFiled: May 15, 2019Publication date: January 9, 2020Applicant: BerGenBio ASAInventors: Jason John Shiers, John Paul Watts, Stuart Thomas Onions, Mohammed Abdul Quddus, Joseph William Wrigglesworth, Colin Peter Sambrook-Smith, Alan Naylor, Derek Londesbrough
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Publication number: 20200010422Abstract: A variety of compounds are provided capable of chelating a metal, in particular a lanthanide such as Eu(III) and Tb(III). Luminescent complexes of the compound and a metal ion are also provided, in particular luminescent metal complexes are provided containing a lanthanide such as Eu(III) or Tb(III) and a compound described herein. In some aspects, the luminescent complexes are capable of exhibiting bright emissions with high quantum yields. Methods of making the compound are provided. Methods of using the compounds and luminescent complexes are also provided, for example for imaging and therapeutic applications.Type: ApplicationFiled: September 6, 2017Publication date: January 9, 2020Inventors: LAWRENCE MILLER, ALI MOHAMADI
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Publication number: 20200010423Abstract: The invention provides a method capable of more simply and efficiently producing halogen-containing pyrazolecarboxylic acids and intermediates thereof, which are useful as pharmaceutical or agrochemical intermediates, in a manner suitable for industrial production. In particular, the invention provides a method of producing a compound represented by the formula (b), which comprises reacting a compound represented by the formula (a) with a halogenating agent selected from the group consisting of a compound represented by X2 (formula (1)), a compound represented by SOX2 (formula (2)), and a compound represented by SO2X2 (formula (3)) to obtain the compound represented by the formula (b): formula (1) X2 formula (2) SOX2 formula (3) SO2X2 wherein each symbol is as described in the description.Type: ApplicationFiled: September 17, 2019Publication date: January 9, 2020Applicant: AGC INC.Inventor: Yuichiro ISHIBASHI
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Publication number: 20200010424Abstract: The invention provides a method capable of more simply and efficiently producing halogen-containing pyrazolecarboxylic acids useful as pharmaceutical or agrochemical intermediates, in a manner suitable for industrial production. In particular, the invention provides a method of producing a compound represented by the formula (b), which comprises reacting a compound represented by the formula (a) with oxygen in the presence of a compound containing a transition metal atom to obtain the compound represented by the formula (b): wherein each symbol is as described in the description.Type: ApplicationFiled: September 17, 2019Publication date: January 9, 2020Applicant: AGC INC.Inventors: Shota SHIMIZU, Masanori SAWAGUCHI
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Publication number: 20200010425Abstract: The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formulae (Ia), (Ib) and (Ic), and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.Type: ApplicationFiled: September 18, 2019Publication date: January 9, 2020Inventors: Lyudmyla Chumakova, Andrew Patron, Chad Priest, Donald Karanewsky, Rachel Kimmich, Brant Clayton Boren, Jeffrey Robert Hammaker, Volodymyr Chumakov, Wen Zhao, Alain Noncovich, Jane Ung
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Publication number: 20200010426Abstract: The present invention describes new amino pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel amino pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.Type: ApplicationFiled: September 16, 2019Publication date: January 9, 2020Inventors: Daniela Angst, Francois Gessier, Anna Vulpetti
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Publication number: 20200010427Abstract: The present teachings relate to hydroxypyridinone and hydroxypyrimidinone derivatives, pharmaceutical compositions thereof, and methods of using such compounds to treat bacterial infections.Type: ApplicationFiled: July 15, 2019Publication date: January 9, 2020Inventors: Min TENG, Baskar NAMMALWAR, Konstantin TAGANOV, David T. PUERTA
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Publication number: 20200010428Abstract: The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.Type: ApplicationFiled: September 18, 2019Publication date: January 9, 2020Inventors: Francis Gosselin, Chong Han, Hans Iding, Reinhard Reents, Scott Savage, Beat Wirz
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Publication number: 20200010429Abstract: The present invention is related to an improved process for the preparation and purification of crystalline Vortioxetine hydrobromide of Formula-I. The process according to present invention is operationally simple and suitable for industrial application which will avoid hazardous chemicals and eliminate column chromatography to get ICH quality of pharmaceutically acceptable active pharmaceutical ingredient having snow white appearance.Type: ApplicationFiled: February 21, 2018Publication date: January 9, 2020Applicant: Unichem Laboratories LtdInventors: Dhananjay G. SATHE, Arijit DAS, Vishal KULKARNI, Tushar PATIL, Yogesh PATIL, Prafulla NAGAWADE
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Publication number: 20200010430Abstract: Disclosed is a novel compound having HSP90 inhibitory activity or a pharmaceutically acceptable salt thereof, and a medicinal use thereof, and composition comprising a dihydroxyphenyl compound or a benzamide compound, which is a novel compound having the HSP90 inhibitory activity of the present invention can effectively inhibit HSP90, and thus can be usefully used as a pharmaceutical composition for preventing or treating HSP90-mediated diseases or a health functional food for preventing or improving HSP90-mediated diseases, which selected from the group consisting of cancer diseases, degenerative neurological diseases and viral infections.Type: ApplicationFiled: September 19, 2019Publication date: January 9, 2020Inventor: Young Ho SEO
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Publication number: 20200010431Abstract: A method for precipitating as particles 2,6-diamino-3,5-dinitropyrazine-1-oxide (or ANPZO) present in an acid medium, which comprises adding the acid medium to an aqueous solution and which is characterized in that the aqueous solution comprises a nitrate salt. Further disclosed is a method for synthesizing ANPZO implementing this precipitation method. The synthesis method comprises converting 2,6-diaminopyrazine-1-oxide (or DAPO) into ANPZO by nitration in an acid medium, and then precipitating as particles the ANPZO by adding the acid medium to an aqueous solution, and is characterized in that the aqueous solution comprises a nitrate salt.Type: ApplicationFiled: February 26, 2018Publication date: January 9, 2020Inventors: Eric Pasquinet, Anne Wuillaume, Nicolas Pin, Arnaud Beaucamp, Christelle Barthet
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Publication number: 20200010432Abstract: The present invention provides novel phenazine derivatives, such as compounds of Formula (I) (e.g., Formulae (II)-(XIX)), and pharmaceutically acceptable salts thereof. The compounds of the invention are expected to be antimicrobial agents and may act by a microbial warfare strategy (e.g., a reactive oxygen species (ROS)-based competition strategy). The present invention also provides pharmaceutical compositions, kits, uses, and methods that involve the compounds of the invention and may be useful in preventing or treating a microbial infection (e.g., a bacterial infection or mycobacterial infection) in a subject, inhibiting the growth and/or reproduction of a microorganism (e.g., a bacterium or mycobacterium), killing a microorganism (e.g., a bacterium or mycobacterium), inhibiting the formation and/or growth of a biofilm, reducing or clearing a biofilm, and/or disinfecting a surface.Type: ApplicationFiled: February 17, 2018Publication date: January 9, 2020Applicant: University of Florida Research Foundation, IncorporatedInventors: Robert William Huigens, III, Aron Garrison, Yasmeen Abouelhassan, Hongfen Yang, Gena Burch
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Publication number: 20200010433Abstract: The present specification relates to a compound of Chemical Formula 1 and an organic electronic device comprising the same.Type: ApplicationFiled: April 11, 2017Publication date: January 9, 2020Applicant: LG Chem, Ltd.Inventors: Min Woo Jung, Dong Hoon Lee, Tae Yoon Park, Jungoh Huh, Boonjae Jang, Seongmi Cho, Minyoung Kang, Dong Uk Heo, Miyeon Han, Jungha Lee
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Publication number: 20200010434Abstract: Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3 ; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem subsituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoType: ApplicationFiled: June 24, 2019Publication date: January 9, 2020Inventors: Lourdes Salvador ODEN, Magnus NILSSON, Pia KAHNBERG, Bertil SAMUELSSON, Urszula GRABOWSKA
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Publication number: 20200010435Abstract: Lanthionine ketimine phosphonate (LK-P), lanthionine ketimine ester phosphonate (LKE-P), other lanthionine ketimine, lanthionine ketimine phosphonate, and lanthionine ketimine ester derivatives, and methods of making and using the same, are described.Type: ApplicationFiled: February 16, 2018Publication date: January 9, 2020Applicants: The University of Toledo, Washington State UniversityInventors: Kenneth Hensley, Travis Denton
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Publication number: 20200010436Abstract: The present invention relates to: a process for preparing 3,7-bis-(dimethylamino)-phenothiazin-5-ium bromide or chloride; a method of converting 3,7-bis-(dimethylamino)-phenothiazin-5-ium bromide to 3,7-bis-(di-methylamino)-phenothiazin-5-ium chloride; and the purification of 7-bis-(di-methylamino)-phenothiazin-5-ium chloride by crystallization from aqueous solution of hydrochloric acid, leading to a pharmaceutically acceptable 3,7-bis-(di-methylamino)-phenothiazin-5-ium chloride (methylthioninium chloride, methylene blue, MTC) of formula I below reported.Type: ApplicationFiled: March 15, 2018Publication date: January 9, 2020Applicant: MIKROCHEM spol. s r.o.Inventors: Daniela BENADIKOVÁ, Juraj CECH, Erik JUHÁS, Vladimír OREMUS, Vendel SMAHOVSKÝ