Patents Issued in June 21, 2018
  • Publication number: 20180170842
    Abstract: This present disclosure relates to processes and apparatuses for toluene methylation in an aromatics complex for producing paraxylene. More specifically, the present disclosure relates to processes and apparatuses for toluene methylation within an aromatics complex for producing paraxylene wherein an embodiment uses a riser reactor, another embodiment uses a pre-reactor producing dimethyl ether, and another embodiment uses partial regeneration of the catalyst.
    Type: Application
    Filed: December 20, 2017
    Publication date: June 21, 2018
    Inventors: Robert J. Schmidt, Feng Xu, Joseph A. Montalbano, Ling Zhou, Edwin P. Boldingh, Linda S. Cheng, John J. Senetar
  • Publication number: 20180170843
    Abstract: The present invention relates to the field of catalytic hydrogenation and, more particularly, to the use of Fe complexes with tridentate ligands, having one amino or imino coordinating group and two phosphino coordinating groups, in hydrogenation processes for the reduction of ketones or aldehydes, into the corresponding alcohol or diol, respectively.
    Type: Application
    Filed: June 16, 2016
    Publication date: June 21, 2018
    Applicant: Firmenich SA
    Inventors: Lionel SAUDAN, Jézabel PRAZ
  • Publication number: 20180170844
    Abstract: Processes are disclosed for the conversion of a carbohydrate source to hexamethylenediamine (HMDA) and to intermediates useful for the production of hexamethylenediamine and other industrial chemicals. HMDA is produced by direct reduction of a furfural substrate to 1,6-hexanediol in the presence of hydrogen and a heterogeneous reduction catalyst comprising Pt or by indirect reduction of a furfural substrate to 1,6-hexanediol wherein 1,2,6-hexanetriol is produced by reduction of the furfural substrate in the presence of hydrogen and a catalyst comprising Pt and 1,2,6-hexanediol is then converted by hydrogenation in the presence of a catalyst comprising Pt to 1,6 hexanediol, each process then proceding to the production of HMDA by known routes, such as amination of the 1,6 hexanediol. Catalysts useful for the direct and indirect production of 1,6-hexanediol are also disclosed.
    Type: Application
    Filed: August 22, 2017
    Publication date: June 21, 2018
    Inventors: Eric L. DIAS, James A.W. SHOEMAKER, Thomas R. BOUSSIE, Vincent J. MURPHY
  • Publication number: 20180170845
    Abstract: A method for preparation of polyols from an unsaturated TAG oil that involves first epoxidizing the unsaturated TAG oil; then subjecting the epoxidized TAG oil to transesterification using a diol and/or triol in the presence of a catalyst to produce hydroxyalkyl esters of fatty acid epoxides; and finally hydroxylating the transesterification product using a diol and/or triol and a solid acid catalyst to obtain a polyol with relatively high hydroxyl value and low viscosity.
    Type: Application
    Filed: June 27, 2016
    Publication date: June 21, 2018
    Inventors: Jonathan M. CURTIS, Tolibjon S. OMONOV, Ereddad KHARRAZ, Xiaohua KONG, Hossein M. TAVASSOLI-KAFRANI
  • Publication number: 20180170846
    Abstract: The disclosure relates to cannabinoid derivative compounds, pharmaceutical compositions made thereof, and methods for treating various diseases and disorders including cancer.
    Type: Application
    Filed: November 1, 2017
    Publication date: June 21, 2018
    Inventors: Sean D. McAllister, Pierre-Yves Desprez, Anuradha Mahadevan
  • Publication number: 20180170847
    Abstract: Described herein are methods of acylating an aryl substrate comprising combining a substituted aryl substrate with an acylating agent in the presence of a catalyzing medium, thereby acylating the substituted aryl substrate in the para position, wherein the catalyzing medium is an ionic liquid comprising at least one cation and at least one metal halide anion.
    Type: Application
    Filed: December 19, 2017
    Publication date: June 21, 2018
    Inventors: Robin D. Rogers, Rajkumar Kore, Parasu Veera Uppara
  • Publication number: 20180170848
    Abstract: The present invention relates to a process for providing substituted phenyl ketones. Furthermore, the invention relates to the use of substituted phenoxyphenyl ketones obtained by the inventive process for the preparation of triazoles.
    Type: Application
    Filed: June 14, 2016
    Publication date: June 21, 2018
    Inventors: Joachim GEBHARDT, Daniel SAELINGER, Manfred EHRESMANN, Roland GOETZ
  • Publication number: 20180170849
    Abstract: A method for producing photo-cleavable fragrance pre-cursors is described, which includes potential stereoselective method steps, agents containing the fragrance pre-cursors and the use of the fragrance pre-cursors for prolonging the scent impression in the agent and on surfaces treated with said agent.
    Type: Application
    Filed: June 2, 2016
    Publication date: June 21, 2018
    Inventors: Thomas GERKE, Christian KROPF, Ursula HUCHEL, Axel GRIESBECK, Björn PORSCHEN
  • Publication number: 20180170850
    Abstract: A process for preparing 2,6-dimethyl-5-heptenal, comprising oxidizing citral of which more than 50% are present as geranial with hydrogen peroxide in the presence of a catalyst comprising a Baeyer-Villiger oxidation catalyst, preferably a tin-containing molecular sieve.
    Type: Application
    Filed: May 4, 2016
    Publication date: June 21, 2018
    Applicant: BASF SE
    Inventors: Nicolas VAUTRAVERS, Joaquim TELES, Ralf PELZER, Daniel SCHNEIDER, Florian GARLICHS, Andreas KELLER, Andrei-Nicolae PARVULESCU, Ulrich MÜLLER
  • Publication number: 20180170851
    Abstract: The present invention relates to a method of extracting 3-hydroxypropionaldehyde (3-HPA) and/or derivatives thereof from an aqueous solution comprising 3-HPA, the method comprising: (a) contacting the aqueous solution with chitosan and/or chitosan comprising polymers; (b) separating the 3-HPA bound chitosan and/or chitosan comprising polymers; and (c) washing the 3-HPA bound chitosan and/or chitosan comprising polymers at least once with a washing medium; wherein 3-HPA and/or derivatives thereof is in the washing medium.
    Type: Application
    Filed: November 30, 2017
    Publication date: June 21, 2018
    Applicant: EVONIK DEGUSSA GMBH
    Inventors: Tarek DISHISHA, Rajni Hatti KAUL, Roya R. R. SARDARI, Bastian GRUND, Oliver THUM
  • Publication number: 20180170852
    Abstract: The present invention is directed to a process for catalytic hydrodechlorination of dichloroacetic acid, wherein hydrogen gas is contacted with a liquid feed comprising dichloroacetic acid and monochloroacetic acid to form a product stream comprising monochloroacetic acid and an off gas stream comprising hydrogen chloride and hydrogen, and wherein the product stream is contacted with nitrogen gas so as to remove hydrogen gas present in the product stream.
    Type: Application
    Filed: June 9, 2016
    Publication date: June 21, 2018
    Applicant: Akzo Nobel Chemicals International B.V.
    Inventors: Lars Magnus Tollin, Cornelis Kooijman
  • Publication number: 20180170853
    Abstract: The present invention relates to a method for hydrogenolysis of alpha-hydroxy esters or acids, comprising reacting the alpha-hydroxy ester or acid in the presence of a heterogeneous catalyst. The present invention also relates to a method for producing propionic acid ester, and the use of any of the methods for the production of propionic acid esters, such as alkyl propionate.
    Type: Application
    Filed: June 23, 2016
    Publication date: June 21, 2018
    Inventors: Shunmugavel SARAVANAMURUGAN, Santosh Govind KHOKARALE, Anders RIISAGER
  • Publication number: 20180170854
    Abstract: The invention provides a HYA derivative having superior physiological functions intrinsic to HYA and permitting easy ingestion and easy handling, and use thereof. In particular, the invention relates to a triglyceride in which at least one fatty acid forming an ester bond with a hydroxy group of glycerol is 10-hydroxy-cis-12-octadecenoic acid, or an optical isomer thereof, and a composition (edible fat or oil, food, medicament, cosmetic etc.) containing same.
    Type: Application
    Filed: June 2, 2016
    Publication date: June 21, 2018
    Applicants: NITTO PHARMACEUTICAL INDUSTRIES, LTD., KYOTO UNIVERSITY
    Inventors: Yasunori YONEJIMA, Jun OGAWA, Shigenobu KISHINO
  • Publication number: 20180170855
    Abstract: The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.
    Type: Application
    Filed: June 14, 2016
    Publication date: June 21, 2018
    Inventors: Xiaoming ZHANG, Meenakshi S. VENKATRAMAN, Cyrus K. BECKER
  • Publication number: 20180170856
    Abstract: The present invention relates to a process to prepare N,N?-di(2-hydroxybenzyl) ethylenediamine-N,N?-diacetic acid and salts thereof comprising a reaction between formaldehyde, ethylenediamine diacetic acid or a salt thereof and phenol at a pH of between 3 and 7 and a temperature below 60° C. wherein the reaction mixture contains 0.2 to 1.1 molar equivalents of alkali metalions on the molar amount of EDDA.
    Type: Application
    Filed: June 23, 2016
    Publication date: June 21, 2018
    Inventors: Adrianus Maria REICHWEIN, Hubertus Johannes JONGEN, Marjolein GROOTE
  • Publication number: 20180170857
    Abstract: Provided herein are compounds and compositions useful in increasing PPAR? activity. The compounds and compositions provided herein are useful for the treatment of PPAR? related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
    Type: Application
    Filed: February 15, 2018
    Publication date: June 21, 2018
    Applicants: Salk Institute for Biological Studies, Mitobridge, Inc.
    Inventors: Ronald M. Evans, Michael Downes, Thomas J. Baiga, Joseph P. Noel, Emi Kanakubo Embler, Weiwei Fan, John F.W. Keana, Mark G. Bock, Authur F. Kluge, Mike A. Patane
  • Publication number: 20180170858
    Abstract: Described herein are compounds that are EP4 agonists and antagonists which are useful for treating a variety of pathological conditions associated with activity of EP4 receptors.
    Type: Application
    Filed: February 20, 2018
    Publication date: June 21, 2018
    Inventors: David W. Old, Christopher D. Hein
  • Publication number: 20180170859
    Abstract: The present invention provides a process for the preparation of Teriflunomide (Formula-I). The present invention describes the synthesis of Teriflunomide without isolating the intermediate Leflunomide. Teriflunomide is prepared from 5-Methyl isoxazole-4-carboxylic acid by converting to its acid chloride and coupling with 4-trifluoromethyl aniline to obtain Leflunomide (which is not isolated) followed by ring opening reaction using aq. Sodium Hydroxide to form Teriflunomide. In other words, the process is telescoped from 5-methylisoxazole-4-carbonyl chloride.
    Type: Application
    Filed: June 16, 2016
    Publication date: June 21, 2018
    Inventors: Venkata Raghavendracharyulu Palle, Ramakrishna Parameshwar Bhat, Mariappan Kaliappan, Jithendra R. Babu, Rajmahendra Shanmughasamy
  • Publication number: 20180170860
    Abstract: The present invention relates to ureaurethanes of the following formula (I) in which at least one of the R1 or R2 radicals is a mono- or polyunsaturated, branched or unbranched alkenyl or alkynyl radical having 12 to 24 carbon atoms, n is an integer ?1, where the upper limit for n arises from the maximum number average molecular weight Mn of the ureaurethanes of the general formula (I), which is 65 000 g/mol, and which is determined by means of gel permeation chromatography to DIN 55672-2 using a polymethyl methacrylate standard, R3 is a xylylene radical or a hydrogenated xylylene radical and R4 is a tolylene radical or various other radicals. The invention also relates to ureaurethane compositions comprising the ureaurethanes of the invention and to the preparation of both. The invention further relates to the use of the ureaurethanes or ureaurethane compositions as rheology control agent and anti-settling agent.
    Type: Application
    Filed: July 22, 2016
    Publication date: June 21, 2018
    Inventors: Marc EBERHARDT, René NAGELSDIEK, Sylvia BÜHNE, Jürgen OMEIS, Agnetha SCHMITT
  • Publication number: 20180170861
    Abstract: Small molecule compounds derived from ?-sulfophenylacetic amide (SPAA) are provided as novel sulfonic acid based pTyr mimetics. These compounds effectively inhibit a variety of protein tyrosine phosphatases (PTPs), such as mPTPA, mPTPB, LMWPTP, and Laforin. Use of these compounds as pharmaceutical agents for treating diseases associated with abnormal protein tyrosine phosphatase activity is also provided.
    Type: Application
    Filed: June 1, 2016
    Publication date: June 21, 2018
    Inventors: Zhong-Yin Zhang, Rongjun He
  • Publication number: 20180170862
    Abstract: Small molecule compounds derived from ?-sulfophenylacetic amide (SPAA) are provided as novel sulfonic acid based pTyr mimetics. These compounds effectively inhibit a variety of protein tyrosine phosphatases (PTPs), such as mPTPA, mPTPB, LMWPTP, and Laforin. Use of these compounds as pharmaceutical agents for treating diseases associated with abnormal protein tyrosine phosphatase activity is also provided.
    Type: Application
    Filed: June 1, 2016
    Publication date: June 21, 2018
    Inventors: Zhong-Yin Zhang, Rongjun He
  • Publication number: 20180170863
    Abstract: Compounds according to Formula I: or a pharmaceutically acceptable salt thereof wherein: A1 is NR1 or CR1, with R1 being H or methyl, with methyl, if present, optionally being substituted with one or more F; the cyclopropyl moiety can be optionally substituted with one or more methyl and one or more F; A2-A5 are N or CR2-CR5, respectively, with the proviso that no more than two of the four positions A in A2-A5 can be simultaneously N; R2-R5 are independently H, halogen, amino, C(1-3)alkoxy, (di)C(1-3)alkylamino or C(1-6)alkyl; R6 and R7 are independently H, F, methyl, ethyl, hydroxyl or methoxy or R2 and R3 together is carbonyl, all alkyl groups, if present, optionally being substituted with one or more F; R8 is H or C(1-6)alkyl; R9 is selected from the group consisting of Formula II, III, IV and V The compounds can be used as inhibitors of ROR? and are useful for the treatment of ROR? mediated diseases.
    Type: Application
    Filed: June 3, 2016
    Publication date: June 21, 2018
    Applicants: LEAD PHARMA HOLDING B.V., SANOFI
    Inventors: Joseph Maria Gerardus Barbara CALS, Vera DE KIMPE, Sander Bernardus NABUURS, Cosimo Damiano CADICAMO, Jaap Gerardus Henricus LEMMERS
  • Publication number: 20180170864
    Abstract: One exemplary embodiment can be a process for oxidizing one or more thiol compounds from an alkaline stream. The process may include passing a mixed stream having the alkaline stream to a vessel having an oxidation section, a separation section and a vent gas section. Often, the oxidation section includes a body containing one or more packing elements. The process can further include passing an oxidized alkaline stream to the separation section containing a first chamber and a second chamber. Usually, the first chamber contains a coated mesh and packing. The two sections further form a neck contains a packing, a distributor, and a mesh.
    Type: Application
    Filed: November 9, 2017
    Publication date: June 21, 2018
    Inventors: Jonathan A. Tertel, Susanna K. Wong
  • Publication number: 20180170865
    Abstract: What is described is a compound of formula I wherein R1 is a linear alkyl, alkenyl, or alkynyl of 2 to 12 carbons, or a branched alkyl with 25, 24, 23, 22, 21, 20, 19, 18, 17, 16, 15, 14, 13, 12, 11, 10, 9, 8, or 7 carbons, R2 is a branched alkyl with 25, 24, 23, 22, 21, 20, 19, 18, 17, 16, 15, 14, 13, 12, 11, 10, 9, 8, or 7 carbons, L1 and L2 are independently a linear alkylene with 1-18 carbons or alkenylene with 2-18 carbons, X is S or O, L3 is a bond or an alkylene with 1 to 6 carbons, R3 is an alkylene with 1 to 6 carbons, and R4 and R5 are the same or different, each a linear or branched alkyl with 1 to 6 carbons; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 19, 2018
    Publication date: June 21, 2018
    Inventors: Joseph E. Payne, Padmanabh Chivukula
  • Publication number: 20180170866
    Abstract: What is described is a compound of formula I consisting of a compound in which R1 is a branched chain alkyl consisting of 10 to 31 carbons; R2 is a linear alkyl, alkenyl, or alkynyl consisting of 2 to 20 carbons, or a branched chain alkyl consisting of 10 to 31 carbons; L1 and L2 are the same or different, each a linear alkane of 1 to 20 carbons or a linear alkene of 2 to 20 carbons; X1 is S or O; R3 is a linear or branched alkylene consisting of 1 to 6 carbons; and R4 and R5 are the same or different, each a hydrogen or a linear or branched alkyl consisting of 1 to 6 carbons; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 20, 2017
    Publication date: June 21, 2018
    Inventors: Joseph E. Payne, Padmanabh Chivukula, Priya Karmali, Steven P. Tanis
  • Publication number: 20180170867
    Abstract: The retinoid X receptors (RXRs) are ligand-activated transcription factors heterodimerize with a number of nuclear hormone receptors, thereby controlling a variety of physiological processes. The invention relates to novel enantiomer compounds which are derivatives of dihydroretinoic acid, their stereoselective synthesis, to pharmaceutical compositions containing the same and to the use of same in the treatment of diseases.
    Type: Application
    Filed: May 9, 2016
    Publication date: June 21, 2018
    Applicant: University of Debrecen
    Inventors: Wojciech KREZEL, Ralph RÜHL, Angel R. DE LERA
  • Publication number: 20180170868
    Abstract: Novel amisulpride derivatives and pharmaceutical compositions thereof are disclosed. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may have better membrane permeability compared to amisulpride. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for antagonizing dopamine and/or serotonin (e.g., 5-HT2a) and/or ?2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more conditions responsive to modulation of dopamine and/or serotonin (e.g., 5-HT2a) and/or ?2 receptor in a subject, either individually or in combination with other CNS active agents.
    Type: Application
    Filed: February 14, 2018
    Publication date: June 21, 2018
    Inventors: Andrew R. VAINO, Vincent T. GRATTAN, Zachary PRENSKY
  • Publication number: 20180170869
    Abstract: Benzenesulfonamide derivatives of formula (I), the pharmaceutically acceptable addition salts thereof, the hydrates and/or solvates thereof, and the use of same as inverse agonist of retinoid-related orphan receptor gamma (ROR?t) are described. A pharmaceutical composition including such compounds, as well as the use thereof for the topical and/or oral treatment of ROR?t receptor-medicated inflammatory diseases, in particular acne, psoriasis and/or atopic dermatitis are also described.
    Type: Application
    Filed: December 18, 2015
    Publication date: June 21, 2018
    Inventors: Branislav MUSICKI, Claire BOUIX-PETER, Gilles OUVRY, Etienne THOREAU
  • Publication number: 20180170870
    Abstract: Disclosed herein are compositions and methods for treating cancer, FLT3-AML, and CML.
    Type: Application
    Filed: February 9, 2018
    Publication date: June 21, 2018
    Inventors: Sangkil Nam, David Horne, Jun Xie
  • Publication number: 20180170871
    Abstract: This invention relates to crystalline forms of (R)-1-(1-(methylsulfonyl)propan-2-yl)-4-(trifluoromethyl)indoline-5-carbonitrile, a modulator of the androgen receptor, and methods for the use in treatment.
    Type: Application
    Filed: February 12, 2018
    Publication date: June 21, 2018
    Inventors: Istvan KALDOR, Dalin TANG
  • Publication number: 20180170872
    Abstract: Novel alkynyl-substituted 3-phenylpyrrolidine-2,4-diones and use thereof as herbicides The present invention relates to novel effective alkynyl-substituted 3-phenylpyrrolidine-2,4-diones according to the general formula (I) or agrochemically acceptable salts thereof, where X?C1-C4-alkyl, C1-C4-haloalkyl or C3-C6-cycloalkyl; Y?C1-C4-alkyl or C3-C6-cycloalkyl; n=1, 2 or 3; m=1 or 2; R1=C1-C6-alkyl, or C3-C6-cycloalkyl; R2=hydrogen or methyl; R3?C1-C3-alkoxy-C1-C3-alkyl, or a saturated five- or six-membered heterocycle with an oxygen or sulphur atom; G=hydrogen, a cleavable group L or a cation E. The invention also relates to the use of the compounds according to the invention for controlling weeds and weed grasses in crops of useful plants.
    Type: Application
    Filed: June 20, 2016
    Publication date: June 21, 2018
    Inventors: ALFRED ANGERMANN, STEFAN LEHR, HENDRIK HELMKE, REINER FISCHER, GUIDO BOJACK, CHRISTOPHER HUGH ROSINGER, ELMAR GATZWEILER, HANSJÖRG DIETRICH
  • Publication number: 20180170873
    Abstract: The present disclosure is directed to resins and to polymers, copolymers, and blends formed therefrom.
    Type: Application
    Filed: January 3, 2018
    Publication date: June 21, 2018
    Inventors: Sajal Das, Paul Boothe, Patrick Shipman
  • Publication number: 20180170874
    Abstract: The present invention relates to a compound which can be useful for the treatment or prevention of SPT-related diseases including cancer and congenital diseases associated with sphingolipid accumulation (including Niemann-Pick disease).
    Type: Application
    Filed: April 19, 2016
    Publication date: June 21, 2018
    Inventors: Yasutomi ASANO, Takuto KOJIMA, Osamu KURASAWA, Tzu-Tshin WONG, Yasuhiro HIRATA, Naoki IWAMURA, Bunnai SAITO, Yuta TANAKA, Ryosuke ARAI, Shinichi IMAMURA, Kazuko YONEMORI, Yasufumi MIYAMOTO, Shuji KITAMURA, Osamu SANO
  • Publication number: 20180170875
    Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention also relates to substantially pure compound 1 and substantially pure compound 1 salt (e.g., compound 1 hydrochloride salt and compound 1 benzenesulfonate salt). The invention further relates to methods of preparing substantially pure compound 1 and compound 1 salts.
    Type: Application
    Filed: February 13, 2018
    Publication date: June 21, 2018
    Inventor: David G. HANGAUER, JR.
  • Publication number: 20180170876
    Abstract: The present invention is a compound of the formula or a pharmaceutically acceptable salt thereof. The compounds are useful as HDAC inhibitors.
    Type: Application
    Filed: August 2, 2017
    Publication date: June 21, 2018
    Inventors: Stephen J. Shuttleworth, Cyrille D. Tomassi, Alexander R. L. Cecil, Somhairle MacCormick, William J. Nodes, Franck A. Silva
  • Publication number: 20180170877
    Abstract: Compounds according to Formula I: or a pharmaceutically acceptable salt wherein: A1 is NR1 or CR1, with R1 herein; the cyclopropyl moiety with one or more methyl and one or more F; A2-A5 are N or CR2-CR5, with no more than two of the four positions A in A2-A5 can be simultaneously N; R2-R5 are described; R6 and R7 are independently H, F, methyl, ethyl, hydroxyl or methoxy or R6 and R7 together is carbonyl, all alkyl groups, if substituted with one or more F; R8 is H or C(1-6)alkyl; A9-A12 are N or CR9-CR12, with no more than two of the four positions A in A9-A12 can be simultaneously N; R9-R12 herein; R13 and R14 herein; or R13 and R14 fused forming a ring having 5 to 7 atoms by joining R13 being C(1-6)alkyl or C(2-6)alkenyl. The ROR? compounds can treat ROR? mediated diseases.
    Type: Application
    Filed: June 3, 2016
    Publication date: June 21, 2018
    Applicants: LEAD PHARMA HOLDING B.V., SANOFI
    Inventors: Joseph Maria Gerardus Barbara CALS, Vera DE KIMPE, Sander Bernardus NABUURS
  • Publication number: 20180170878
    Abstract: Provided herein are photocrosslinking reagents, crosslinkable proteins displaying photocrosslinking groups, crosslinked protein-protein complexes, and methods of use thereof.
    Type: Application
    Filed: June 9, 2016
    Publication date: June 21, 2018
    Inventors: Alexander V. Statsyuk, David T. Krist, Neil L. Kelleher, Luis Henrique Ferreira do Vale, Heeseon An
  • Publication number: 20180170879
    Abstract: [Problem] The present invention is to provide a novel pyrazole derivative, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and a pharmaceutical use thereof. [Solution] The present invention provides a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof, which has TRPM8 inhibitory effects: wherein ring A is C6-10 aryl or the like; X is CR4a or the like; R1 and R2 are a hydrogen atom or the like; R3 is a hydrogen atom or the like; R4 is a hydrogen atom or the like; ring B is C6-10 aryl or the like; R5 is a hydrogen atom or the like; R6a is a hydrogen atom or the like; R7a is a hydrogen atom or the like; R7b is a hydrogen atom or the like; R6b is a hydrogen atom or the like; R8 is a hydrogen atom or the like; n is 0, 1 or 2.
    Type: Application
    Filed: June 22, 2016
    Publication date: June 21, 2018
    Applicant: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Hideaki HIRASAWA, Fumiya TANADA, Yousuke MUTAI, Nobuhiko FUSHIMI, Junichi KOBAYASHI, Yoshiro KIJIMA
  • Publication number: 20180170880
    Abstract: A method for producing a 1-(acyloxy)alkyl carbamate derivative (III), using a fluorous alkyl carbonate derivative (I), and a fluorous alkyl carbonate derivative (I) and a method for producing the same. In the formula, R1 represents C1-C4 alkyl group or a C3-C6 cycloalkyl group, R2 represents a C1-C4 alkyl group or a hydrogen atom, and A represents a fluorous alkyl group (wherein the fluorous alkyl group represents a C2-C11 alkyl group in which 40% or more of the hydrogen atoms are replaced by fluorine atoms).
    Type: Application
    Filed: June 24, 2016
    Publication date: June 21, 2018
    Inventors: Tsuyoshi UEDA, Yuzo ABE
  • Publication number: 20180170881
    Abstract: The present invention provides a medicament for treating a disease involving Nav 1.7 such as neuropathic pain, nociceptive pain, inflammatory pain, small-fiber neuropathy, erythromelalgia, paroxysmal extreme pain disorder, dysuria, and multiple sclerosis, which comprises a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c and R1d are hydrogen, halogen, cyano, C1-4 alkyl, C1-4 alkoxy, or the like, provided that at least one of R1a, R1b, R1c and R1d is C6-10 aryl, C6-10 aryloxy, or the like, R2 and R3 are hydrogen, C1-6 alkyl, C3-10 cycloalkyl, or the like, R4 is hydrogen, C1-6 alkyl, C3-7 cycloalkyl, or the like, m is 1, 2 or 3, L is CR7R8, and R7 and R8 are hydrogen, hydroxyl, C1-4 alkyl, C1-4 alkoxy, or the like.
    Type: Application
    Filed: September 9, 2016
    Publication date: June 21, 2018
    Inventors: Masafumi Komiya, Kohei Iwamoto, Toshio Kanai, Shingo Mizushima, Keiji Adachi, Kuniko Urashima
  • Publication number: 20180170882
    Abstract: The present invention relates to benzimidazol-2-amines of general formula (I), in which R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: June 3, 2016
    Publication date: June 21, 2018
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Sven RING, Olaf PANKNIN, Katja ZIMMERMANN, Judith GÜNTHER, Lars BÄRFACKER
  • Publication number: 20180170883
    Abstract: The present invention, among other things, provides compounds and compositions thereof for use in the modulation of Hsp70. In some embodiments, the present invention provides a method for inhibiting Hsp70 activity. In some embodiments, the present invention provides a method of treating a subject suffering from or susceptible to a disease, disorder, or condition responsive to Hsp70 inhibition comprising administering to the subject a therapeutically effective amount of a provided compound. In some embodiments, the present invention provides a method for treating or preventing cancer in a subject suffering therefrom, comprising administering to a patient in need thereof a therapeutically effective amount of a provided compound.
    Type: Application
    Filed: December 14, 2017
    Publication date: June 21, 2018
    Inventors: Gabriela Chiosis, Yanlong Kang, Hardik J. Patel, Maulik Patel, Stefan Ochiana, Anna Rodina, Tony Taldone, Liza Shrestha
  • Publication number: 20180170884
    Abstract: This document relates to compounds useful as agents for preventing or treating human cytomegalovirus (HCMV) infections.
    Type: Application
    Filed: November 9, 2015
    Publication date: June 21, 2018
    Inventors: Stacy Remiszewski, Emre Koyuncu, Qun Sun, Lillian Chiang
  • Publication number: 20180170885
    Abstract: The invention relates to an improved process for the manufacture of bis-resorcinyl triazines of formula (I), wherein R1 is hydrogen, a C1-C18alkyl group or a C2-C18alkenyl group and R2 is a C1-C18alkyl group or a C2-C18alkenyl group.
    Type: Application
    Filed: May 12, 2016
    Publication date: June 21, 2018
    Applicant: DMS IP ASSETS B.V.
    Inventors: Nadine GREINER, Sandro SCHMID, René Tobias STEMMLER
  • Publication number: 20180170886
    Abstract: The invention relates to an improved process for the manufacture of bis-resorcinyl triazines of formula (I) wherein R1 is a C1C18alkyl group or C2-C18alkenyl group as well as the respective alkyl substituted bis-resorcinyl derivatives of formula (II) wherein R1 is a C1-C18alkyl group or C2-C18alkenyl group and R2 and R3 are independently of each other a C1-C18alkyl group or a C2-C18alkenyl group.
    Type: Application
    Filed: May 12, 2016
    Publication date: June 21, 2018
    Inventors: Nadine GREINER, Sandro SCHMID, René Tobias STEMMLER
  • Publication number: 20180170887
    Abstract: The present invention describes novel heteroaryl butanoic acid derivatives that are good drug candidates especially with regard to leukotriene A4 hydrolase (LTA4H). The present invention also relates to pharmaceutical compositions comprising said novel heteroaryl butanoic acid derivatives, methods of using said compounds in the treatment of various diseases and disorders, and processes for preparing the said novel compounds.
    Type: Application
    Filed: February 13, 2018
    Publication date: June 21, 2018
    Inventors: Birgit BOLLBUCK, Christian MARKERT, Wolfgang MILTZ, Till ROEHN
  • Publication number: 20180170888
    Abstract: The present invention relates to bicyclic tetrahydrothiazepine of formula (I), wherein R1 to R3, X1, X2 and R18 have the meaning as indicated in the description and claims. The invention further relates to pharmaceutical compositions comprising such compounds as well as their use as medicaments, especially in methods for the treatment or prevention of a neoplastic and/or infectious disease and in vitro methods.
    Type: Application
    Filed: February 29, 2016
    Publication date: June 21, 2018
    Inventors: Monika ERMANN, Guenther LAMETSCHWANDTNER, Patricia Leonie AMOUZEGH, Russell Stuart CRAFT, Thomas HANKE, Timothy Robin JAMES, Severine Danielle JONES, Hans LOIBNER, Pui Leng LOKE, Ina STERNBERGER, Anton STUETZ, Roland WEHR, Mark WHITTAKER
  • Publication number: 20180170889
    Abstract: Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds are described in formulas I, II, III, IV, V and VI herein. One or more compounds herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria and in particular in Staphylococcus aureus. Compounds herein and pharmaceutical compositions containing one or more of these compounds are useful, for example, in treating infections of Staphylococcus bacteria and in particular of Staphylococcus aureus. Methods for treating such bacterial infections are provided.
    Type: Application
    Filed: December 21, 2017
    Publication date: June 21, 2018
    Inventors: Helen BLACKWELL, Joseph VASQUEZ, Yftah TAL-GAN
  • Publication number: 20180170890
    Abstract: A furfural derivative having the chemical formula (1) wherein R represents hydrogen, an alkyl group or an acyl group, is prepared in a process, which process includes reacting a fructose- and/or glucose-containing starting material with a liquid hydroxyl group-containing compound of formula R—OH in the presence of an acid catalyst at a reaction temperature in the range of 150 to 300° C. to produce an acid reaction mixture including the furfural derivative of chemical formula (1), which acid reaction mixture has a pH-value of smaller than 3; neutralizing the acid reaction mixture to a pH-value in the range of 3 to 6.5 to provide a partially neutralized reaction mixture; and purifying the partially neutralized reaction mixture to recover the furfural derivative of chemical formula (1).
    Type: Application
    Filed: July 1, 2016
    Publication date: June 21, 2018
    Inventors: Johannes Maria Franciscus Sijben, Etienne Mazoyer, Ana Sofia Vagueiro De Sousa Dias, Gerardus Johannes Maria Gruter
  • Publication number: 20180170891
    Abstract: The present disclosure relates generally, but not exclusively, to compounds and their use in therapy, to compositions and agents comprising said compounds, to methods of treatment using said compounds, and their use in the manufacture of medicaments. The disclosure further relates to inhibitors of IRAP and their use in the treatment or prevention of Alzheimer's disease and the treatment and prevention of memory and cognitive disorders.
    Type: Application
    Filed: May 6, 2016
    Publication date: June 21, 2018
    Applicants: Monash University, The Florey Institute of Neuroscience and Mental Health, St. Vincent's Institute of Medical Research
    Inventors: Siew Yeen CHAI, Philip THOMPSON, Simon MOUNTFORD, Michael W. PARKER