Patents Issued in June 4, 2020
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Publication number: 20200172466Abstract: The invention relates to a process for the preparation of an alkanediol and a dialkyl carbonate comprising reacting an alkylene carbonate and an alkanol in the presence of a catalyst, wherein the catalyst is aluminum phosphate.Type: ApplicationFiled: July 16, 2018Publication date: June 4, 2020Inventors: Henri PREISING, Frederik Hendrik VAN DER STEEN, Garo Garbis VAPORCIYAN, Wolfgang Dirk LOSE, Silke Eva Sabine LEONHARDT
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Publication number: 20200172467Abstract: Low-viscosity epoxy methacrylate compounds are useful for lowering the viscosity of reactive resins and for reducing the forces for extruding a reactive-resin component containing these compounds. Furthermore, the low-viscosity epoxy methacrylate compounds are useful for chemical fastening.Type: ApplicationFiled: June 19, 2018Publication date: June 4, 2020Applicant: Hilti AktiengesellschaftInventors: Georg Nickerl, Beate Gnass, Jens Bunzen, Gerald Gaefke, Thomas Bürgel
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Publication number: 20200172468Abstract: The present invention relates to a method for preparing substituted 4-aminoindane derivatives of the general formula (I) by rearrangement of compounds of the formula (II) in HF, wherein R1, R2, R3, R4, and R5 have the definitions as specified in the description.Type: ApplicationFiled: June 20, 2018Publication date: June 4, 2020Inventors: Sergii PAZENOK, Christoph SAEMANN, Yuriy SHERMOLOVICH
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Publication number: 20200172469Abstract: Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, attention deficit hyperactivity disorder, fibromyalgia, irritable bowel syndrome, and/or premature ejaculation are described.Type: ApplicationFiled: September 10, 2019Publication date: June 4, 2020Inventors: Thomas G. Gant, Sepehr Sarshar, Soon Hyung Woo
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Publication number: 20200172470Abstract: A (poly)amine compound represented by the following formula (0): wherein RX is a 2nA-valent group having 1 to 70 carbon atoms or a single bond; each R1A is independently any of an alkyl group having 1 to 30 carbon atoms and optionally having a substituent, an aryl group having 6 to 30 carbon atoms and optionally having a substituent, a crosslinking group having 2 to 30 carbon atoms and optionally having a substituent, an alkoxy group having 1 to 30 carbon atoms and optionally having a substituent, a halogen atom, a nitro group, an amino group having 0 to 30 carbon atoms and optionally having a substituent, a carboxyl group, a thiol group and a hydroxy group, wherein when R1A is any of the alkyl group, the aryl group, the crosslinking group and the alkoxy group, R1A optionally contains at least one bond selected from the group consisting of an ether bond, a ketone bond and an ester bond, and at least one R1A is an amino group having 0 to 30 carbon atoms and optionally having a substituent; X is an oxygen atType: ApplicationFiled: July 27, 2018Publication date: June 4, 2020Inventors: Masatoshi ECHIGO, Takashi MAKINOSHIMA, Yutaka MATSUURA, Toru SHISHIMI
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Publication number: 20200172471Abstract: The present invention provides cationic pillar[n]arenes, e.g., positively charged poly-ammonium, poly-phosphonium and poly-imidazolium pillar[5-6]arene derivatives, capable of inhibiting or preventing biofilm formation, and facilitating existing biofilm decomposition; as well as compositions thereof and methods of use.Type: ApplicationFiled: August 3, 2016Publication date: June 4, 2020Inventors: Yoram Cohen, Micha Fridman, Roymon Joseph, Alissa Naugolny, Mark Feldman, Ido M. Herzog, Dana Kaizerman
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Publication number: 20200172472Abstract: Compounds are provided having the following structure (I) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6, R7, R8, L1, L2, G1, G2, G3, a, b, c and d are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.Type: ApplicationFiled: August 17, 2018Publication date: June 4, 2020Inventor: Xinyao DU
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Publication number: 20200172473Abstract: The present invention pertains to novel dual modulators of farnesoid X receptor (FXR) and soluble epoxide hydrolase (sEH). The modulators of the invention were designed to provide compounds which harbor a dual activity as agonists of FXR and inhibitors (antagonists) of sEH. The invention also provides methods for treating subjects suffering from diseases associated with FXR and sEH, such as metabolic disorders, in particular non-alcoholic fatty liver or nonalcoholic steatohepatitis (NASH).Type: ApplicationFiled: May 24, 2018Publication date: June 4, 2020Inventors: Daniel Merk, Jurema Schmidt, Ewgenij Proschak, Manfred Schubert-Zsilavecz, Moritz Helmstaedter
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Publication number: 20200172474Abstract: The present invention provides novel compounds which activate the Kv7 potassium channels. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders responsive to the activation of Kv7 potassium channels.Type: ApplicationFiled: February 4, 2020Publication date: June 4, 2020Inventors: Mario Rottlander, Anette Graven Sams, Xiaofang Wang, Debasis Das, Jian Hong, Shu Hui Chen
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Publication number: 20200172475Abstract: Provided are urea manufacturing method and apparatus, which can increase the conversion ratio into urea and to reduce the consumption of steam. The temperature of the reactor is increased by introducing the entire amount of raw material ammonia and introducing a portion of the decomposed gas from the stripper into the reactor. The raw material ammonia is preferably heated using the steam condensate generated in the purification step, and/or the steam generated by the heat of condensation of the decomposed gas and the unreacted substances in the condensation step. The heating temperature is preferably between 70 and 140° C.Type: ApplicationFiled: February 12, 2020Publication date: June 4, 2020Applicant: Toyo Engineering CorporationInventors: Keishi SATO, Kenji YOSHIMOTO, Haruyuki MORIKAWA
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Publication number: 20200172476Abstract: A sulfuric acid ester containing a plurality of carbonyl groups or a salt thereof, and a surfactant. The sulfuric acid ester is a compound represented by the following formula: R1—C(?O)—R2—C(?O)—R3—OSO3X wherein R1, R2 and R3 are as defined herein; X is H, a metal atom, NR44, imidazolium optionally containing a substituent, pyridinium optionally containing a substituent, or phosphonium optionally containing a substituent, where R4s are each H or an organic group and are the same as or different from each other; and any two of R1, R2, and R3 optionally bind to each other to form a ring.Type: ApplicationFiled: September 29, 2017Publication date: June 4, 2020Applicant: DAIKIN INDUSTRIES, LTD.Inventors: Satoru YONEDA, Manabu FUJISAWA, Kazuya ASANO, Takahiro KITAHARA, Masahiro HIGASHI, Akiyoshi YAMAUCHI, Sumi ISHIHARA, Yosuke KISHIKAWA
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Publication number: 20200172477Abstract: The invention relates to a color developer of formula (I), (Ar1—SO2—NH-)m-Y—(—NH—C(O)—NH—SO2—Ar2)n (I), wherein Ar1 is an unsubstituted or substituted aromatic moiety, Ar2 is an unsubstituted or substituted phenyl moiety, Y is at least an (m+n)-times substituted benzene group or naphthalene group, and Y is substituted in such a way that at least one Ar2—SO2—NH—C(O)—NH group is in ortho-position with respect to at least one Ar1—SO2—NH group. The invention further relates to a heat-sensitive recording material, comprising a carrier substrate and a heat-sensitive color-forming layer, which contains at least one color former and at least one phenol-free color developer, the at least one color developer being the compound of formula (I). The invention further relates to a method for producing said heat-sensitive recording material.Type: ApplicationFiled: May 17, 2018Publication date: June 4, 2020Applicant: Papierfabrik August Koehler SEInventors: Michael Horn, Timo Stalling, Maren Steppat
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Publication number: 20200172478Abstract: An online continuous flow production process for directly preparing organic peroxides by using hydrogen peroxide as a raw material. This production process uses hydrogen peroxide, catalyst, and an oxidation substrate as a raw material. Substrate will be turned to designated peroxides sequentially through oxidation and workup. This process is performed in a plug-and-produce integrated continuous flow reactor, and the raw materials are continuously fed to the reactor. So, specified peroxide can be continuously obtained at the outlet of the plug-and-produce integrated continuous flow reactor.Type: ApplicationFiled: February 11, 2020Publication date: June 4, 2020Inventors: Bing MA, Shuai PAN, Xinlin SHU
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Publication number: 20200172479Abstract: A preparing method for high-purity levetiracetam, comprising: adjusting the pH of an extracted aqueous layer obtained by dissociating (S)-?-ethyl-2-oxo-1-pyrrolidineacetic acid (R)-methylbenzylamine salt to 5-9; removing water; adding an organic solvent to form a solution and then performing an esterification reaction with ethyl chloroformate or methylchlorofonmate; and carrying out an ammonolysis reaction to obtain the levetiracetam. The method simplifies production process, increases yield, reduces or even avoids the use of triethylamine in the esterification process, and reduces the emission of a great amount of three wastes.Type: ApplicationFiled: August 9, 2018Publication date: June 4, 2020Inventors: Xinlei Chen, Zhicheng Hu, Liang Zheng, Peng Dong
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Publication number: 20200172480Abstract: A conjugate of a potent cytotoxic agent with a cell-binding molecule having a structure represented by Formula (I), wherein T, L, m, n, , R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 are as defined herein, can be used for targeted treatment of cancer, autoimmune disease, and infectious disease.Type: ApplicationFiled: February 5, 2020Publication date: June 4, 2020Applicant: HANGZHOU DAC BIOTECH CO., LTD.Inventors: R. Yongxin ZHAO, Yue ZHANG, Yourang MA
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Publication number: 20200172481Abstract: The invention provides novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.Type: ApplicationFiled: November 11, 2019Publication date: June 4, 2020Inventors: Michael Reardon, Richard A. Silva
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Publication number: 20200172482Abstract: Provided is a method for purifying ropinirole hydrochloride (4-2-di-n-propylaminoethyl-1,3-dihydro-2H-indole-2-ketohydrochloride). The method comprises: adding ropinirole hydrochloride containing a monopropyl impurity A into water, adding organic solvent, stirring and dissolving at room temperature, adding alkali, stirring, standing, demixing, and removing an aqueous layer; optionally, drying the organic layer by using anhydrous magnesium sulfate, and filtering; and adding acyl chloride or acid anhydride into the organic layer, stirring, concentrating the organic layer to be dry, adding an organic solvent into the obtained oily matter, adding concentrated hydrochloric acid, and stirring, so as to obtain the ropinirole hydrochloride. By using the method, the impurity A in the ropinirole hydrochloride can be effectively removed, and the ropinirole hydrochloride can be obtained with a high yield and a high purity, so that the impurity A is controlled and the purity of the product reaches a medicinal standard.Type: ApplicationFiled: June 16, 2017Publication date: June 4, 2020Inventors: Guoliang TU, Zhongming XU, Tao ZHOU, Wenfeng HUANG, Shiwen ZHANG
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Publication number: 20200172483Abstract: The present invention relates to compounds of formula (I). The compounds may be used to modulate the Stimulator of Interferon Genes (STING) protein and thereby treat diseases such as cancer and microbial infections.Type: ApplicationFiled: June 21, 2018Publication date: June 4, 2020Inventors: Monali Banerjee, Sandip Middya, Sourav Basu, Dharmendra Yadav, Rajib Ghosh, David Pryde, Ritesh Shrivastava, Arjun Surya
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Publication number: 20200172484Abstract: The present invention relates to a method for the synthesis of compounds useful in the preparation of antibody drug conjugates (ADC), namely, monoprotected dimeric bifunctional prodrugs based on duocarmycin analogs. In a further aspect, compounds obtained by the method according to the present invention are provided. The monoprotected bifunctional prodrug is used for preparing antibody drug conjugates composed of an antibody moiety and the monoprotected bifunctional prodrug. The antibody compound conjugates thus obtained are provided. Further, a method of preparing an antibody drug conjugate composed of two identical or two different antibody moieties is provided as well as the antibody compound conjugate containing two different antibody moieties accordingly. These conjugates can be used in pharmaceutical compositions, in particular, for use in treatment of tumors, e.g. for use in ADC therapy.Type: ApplicationFiled: August 10, 2018Publication date: June 4, 2020Inventor: Lutz F. TIETZE
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Publication number: 20200172485Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: ApplicationFiled: February 5, 2020Publication date: June 4, 2020Applicant: CELGENE QUANTICEL RESEARCH, INC.Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
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Publication number: 20200172486Abstract: Provided are a pyridone compound represented by Formula (1): wherein R1 represents a C1-C6 alkyl group which may be substituted, etc., R2 represents a halogen atom, a cyano group, etc., R3 and R4 are independent to each other, and each represents a hydrogen atom, a C1-C6 alkyl group which may be substituted, etc., or in combination with the nitrogen atom to which they are bonded form a pyrrolidinyl group, a piperidinyl group, etc., which may be substituted, Y represents a phenyl group which may be substituted, etc., X represents an oxygen atom or a sulfur atom, and an agricultural and horticultural fungicide containing the same as an active ingredient.Type: ApplicationFiled: June 7, 2018Publication date: June 4, 2020Applicant: MITSUI CHEMICALS AGRO, INC.Inventors: Hideki UMETANI, Hideaki IKISHIMA, Kouji TAKAGI, Takeshi FUKUMOTO, Ryohei NAITO, Tomomi SHIRAKAWA, Hikaru KOISHIHARA, Hisaki YAMANAKA, Miyuki KAWASHIMA, Akane SAKURADA
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Publication number: 20200172487Abstract: The present invention provides compound of formula (XVII), wherein P is hydroxyl protecting group; R2 and R3 are independently lower alkyl or R2 and R3 can be alkyl and joined to form a 5-, 6- or 7-membered ring; R4 is lower alkyl, and process for its preparation.Type: ApplicationFiled: December 15, 2016Publication date: June 4, 2020Inventors: Girij Pal Singh, Dhananjai Shrivastava, Harishchandra Sambhaji Jadhav, Pramod Sudhakar Utekar, Digambar Yashwant Salunke
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Publication number: 20200172488Abstract: The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as methods for using the (+)-morphinans to treat pain. Also provided are pharmaceutical combination compositions comprising a (+)-morphinan and an opioid agonist/monoamine reuptake inhibitor, as well as methods for using the combination compositions to treat pain.Type: ApplicationFiled: February 3, 2020Publication date: June 4, 2020Inventor: Bobby N. Trawick
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Publication number: 20200172489Abstract: A fluorescent compound or a salt thereof represented by General Formulae (I) or (II) shown below: In the General Formulae (1) and (II) shown above, R1 and R11 represent an alkyl group or an ?-aminoalkyl group, R2 and R12 represent a hydrogen atom or a alkyl group, R3 and R13 represent an atomic group represented by a formula —(CH2)m— (m is a natural number of 10 or less), R4 and R14 represent an atomic group represented by a formula —CH2— or —NR6— (—NR16—) (R6 and R16 represent an alkyl group), R5 and R15 represent an atomic group represented by a formula —(CH2)n— (n is a natural number of or less), R represents an atomic group represented by any one of formulae —NH2, —NHR7—, NR7R8 and —NR7R8R9 (—NHR17, —NR17R18 and —N+R17R18R19) (R7, R8, R9, R17, R18 and R19 independently represents an alkyl group, respectively) and when R2 and R12 are alkyl groups and R4 (R14) is an atomic group represented by the formula —NR6—(—NR16—), R2 and R6 and R12 and R16 may bind with each other to form a ring.Type: ApplicationFiled: May 18, 2018Publication date: June 4, 2020Applicant: DOJINDO LABORATORIESInventors: Hidefumi IWASHITA, Ryo SAKAMOTO, Takatoshi EZOE, Nobuyuki OZEKI, Munetaka ISHIYAMA
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Publication number: 20200172490Abstract: The invention relates to a compound capable of blocking the absorption of heavy metals by plants and a composition containing the same. The compound was extracted from Aegiceras corniculatum. The compound is extracted by enzyme extraction, filtration, concentrating and drying. The compound is derived from natural plants, and no organic solvents are used in the extraction process. The compound and the composition formed by the compound have a certain barrier effect on the absorption of heavy metals by plants.Type: ApplicationFiled: November 29, 2019Publication date: June 4, 2020Inventors: Lezhang CHEN, Junbo YANG
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Publication number: 20200172491Abstract: The invention relates to substituted 5-(Het-)arylpyrazolamides of general formula (I) and to the their use as herbicides, in particular for controlling 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 agents comprising one or more of the compounds of general formula (I).Type: ApplicationFiled: July 12, 2018Publication date: June 4, 2020Inventors: Joerg TIEBES, Joachim TELSER, Guido BOJACK, Michael Charles McLEOD, Ling MA, Hansjoerg DIETRICH, Elmar GATZWEILER, Anu Bheemaiah MACHETTIRA, Christopher Hugh ROSINGER, Dirk SCHMUTZLER
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Publication number: 20200172492Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises formula (I) wherein X1, and X2 may be the same or different and each is independently selected from C, N, O and S; X3, X4, X5, and X6 may be the same or different and each is independently selected from C and N; each bond represented by a dotted line may be present or absent, provided that at least one such bond is present; R1, R2, R3, R4, R5 and R6 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R1, R2, R3, R4, R5 and R6 groups present is such that the respective valencies of X1, X2, X3, X4, X5, and X6 are maintained; and wherein at least one of R5 and R6 comprises a group Y, wherein Y is a group having a formula selected from (II), (III), (IV), (V), (VI), (VII) wherein L may be present or absent, and may be a substituted or unsubType: ApplicationFiled: February 3, 2020Publication date: June 4, 2020Applicant: IOmet Pharma Ltd.Inventors: Phillip M. Cowley, Alan Wise, Susan Davis, Michael Kiczun
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Publication number: 20200172493Abstract: The present disclosure is directed to a cleavable agent for enhanced magnetic resonance generally corresponding to the formula Y-L-R, wherein Y represents a catalyst-binding moiety having at least one isotopically labeled heteroatom, L represents a cleavable bond, and R represents a hyperpolarized payload having at least one isotopically labeled carbon. Also disclosed herein is a method of cleaving the cleavable agent for enhanced magnetic resonance.Type: ApplicationFiled: November 27, 2019Publication date: June 4, 2020Applicants: Board of Trustees of Southern Illinois University, Vanderbilt UniversityInventors: Boyd M. Goodson, Eduard Y. Chekmenev, Bryce E. Kidd, Jamil A. Mashni, Miranda Limbach, Yuqing Hou, Fan Shi
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Publication number: 20200172494Abstract: Cystic fibrosis is developed through mutation of Cystic Fibrosis Transmembrane conductance Regulator (CFTR), which is one type of chloride channel. An object of the present invention is to provide compounds effective in the treatment of cystic fibrosis that open a chloride channel different from CFTR, which is the cause of the disease, and do not depend on CFTR. Compounds of the present invention are compounds or pharmaceutically acceptable salts thereof that open calcium dependent chloride channels (CaCCs) via G-protein coupled receptor 39 (GPR39) agonism to have strong chloride ion-secretory action, and are represented by the following general formula (I): General formula (I): wherein, X represents a carboxyl group or a tetrazolyl group; Q represents a C1-C3 alkylene group, an oxygen atom, a sulfur atom, etc.; G represents a phenyl group where the phenyl group may have 1 to 3 substituents independently selected from the group consisting of a halogen atom, a cyano group, a C1-C6 alkyl group, etc.Type: ApplicationFiled: December 26, 2017Publication date: June 4, 2020Applicant: Daiichi Sankyo Company, LimitedInventors: Yasuyuki Takeda, Yamato Suzuki, Toshiharu Noji, Hidenobu Murafuji, Satoshi Muneoka, Hidekazu Inoue, Bitoku Takahashi, Rie Inaba
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Publication number: 20200172495Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.Type: ApplicationFiled: December 4, 2019Publication date: June 4, 2020Inventors: Xiangping QIAN, Yong-Liang ZHU
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Publication number: 20200172496Abstract: Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.Type: ApplicationFiled: February 7, 2020Publication date: June 4, 2020Inventors: Agostino Marasco, Giuseppe Alvaro, Anne Dècor, Dieter Hamprecht, Paolo Dambruoso, Simona Tommasi
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Publication number: 20200172497Abstract: The present disclosure is directed to asymmetric triazole benzamide compounds of formula (I) and formula (II), pharmaceutical compositions thereof and methods for modulating or activating a Parkin ligase The present disclosure is also directed to methods of treating and/or reducing the incidence of diseases or conditions related to the activation of Parkin ligase. R1, R2, R3, M1, M2, M3, L1, L2, and L3 are as defined herein.Type: ApplicationFiled: December 3, 2018Publication date: June 4, 2020Inventors: Jennifer JOHNSTON, Paul Ross FATHEREE
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Publication number: 20200172498Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially as fungicides.Type: ApplicationFiled: February 10, 2020Publication date: June 4, 2020Applicant: SYNGENTA PARTICIPATIONS AGInventors: Daniel STIERLI, Thomas James HOFFMAN, Renaud BEAUDEGNIES, Martin POULIOT
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Publication number: 20200172499Abstract: The present invention provides novel compounds of Formulae (I?), (I), (II?), and (II), 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 proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.Type: ApplicationFiled: September 9, 2016Publication date: June 4, 2020Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhandg, Nicholas Paul Kwiatkowski, Mingfeng Hao
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Publication number: 20200172500Abstract: Disclosed is a cost-effective process for catalytic conversion of simple C6-based sugars (such as glucose and fructose) and industrial-grade sugar syrups derived from starch (such as different grades of High Fructose Corn Syrup) and cellulosic biomass to 5-HydroxyMethylFurfural (5-HMF) in a continuous-flow tubular reactor in bi-phasic media using inexpensive heterogeneous solid catalysts. Commercial and synthesized heterogeneous solid catalysts were used and their activities in terms of sugar conversion and HMF selectivity and yield were compared. Continuous dehydration of fructose, glucose and industrial-grade sugar syrups derived from corn and wood to HMF was achieved and the stability of selected catalysts and feasibility of catalyst recycling and regeneration were demonstrated.Type: ApplicationFiled: June 29, 2017Publication date: June 4, 2020Inventors: Chunbao XU, Sadra SOUZANCHI, Tirumala Venkateswara Rao KASANNENI, Zhongshun YUAN
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Publication number: 20200172501Abstract: The present disclosure relates to a process for the production of aromatic primary amines, by reacting an aromatic dialdehyde with hydrogen and ammonia or an ammonia-liberating compound, in the presence of a hydrogenation catalyst and an amine, wherein the molar ratio of the amine to the aromatic dialdehyde is no less than 1:4 at the start of the reaction.Type: ApplicationFiled: February 4, 2020Publication date: June 4, 2020Inventors: Peng LI, Floryan DECAMPO
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Publication number: 20200172502Abstract: Disclosed are a 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride polymorph, a preparation method therefor and an application thereof. Specifically, disclosed are three crystalline forms, i.e., crystalline forms A, B, and C, of 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride (formula I), preparation methods for the three crystalline forms, and use of the three crystalline forms in preparation of drugs.Type: ApplicationFiled: May 31, 2018Publication date: June 4, 2020Inventors: Chunhao YANG, Zehong MIAO, Cun TAN, Xiajuan HUAN, Jian DING, Yi CHEN
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Publication number: 20200172503Abstract: Embodiments of a method of purifying tetrahydrocannabinol (THC) from a composition containing THC and at least one impurity, e.g., from pesticides, waxes, lipids, pigments, and other cannabinoids, can use a continuous simulated moving bed process, a batch column chromatography method, or a single column, and a combination of one or more of a sequence of purification steps including: filtration, decolorization, activation or decarboxylation, dewaxing, polishing, and crystallization to separate a cannabinoid from the cannabis plant and to provide various cannabinoid products. The THC products can be used in various pharmaceutical and nutraceutical applications.Type: ApplicationFiled: December 2, 2019Publication date: June 4, 2020Applicant: Orochem Technologies Inc.Inventors: Anil OROSKAR, Kunal GULATI, David HOUSE, Asha OROSKAR, Gautham OROSKAR
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Publication number: 20200172504Abstract: The present invention provides compounds useful as modulators, agonists or antagonists of androgen receptor (AR), compositions thereof, and methods of making and using the same.Type: ApplicationFiled: October 21, 2019Publication date: June 4, 2020Inventors: Minna D. Balbas, Michael J. Evans, Charles L. Sawyers, Yang Shen, David Hosfield, Geoffrey L. Greene
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Publication number: 20200172505Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of inflammation, neurological or psychiatric disorders associated with modulating mGlu5 receptor function.Type: ApplicationFiled: February 3, 2020Publication date: June 4, 2020Inventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Aves, Benjamin Gerald Tehan
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Publication number: 20200172506Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds as exemplified as follows, The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: ApplicationFiled: February 3, 2020Publication date: June 4, 2020Applicant: CELGENE QUANTICEL RESEARCH, INC.Inventors: Young CHEN, Toufike Kanouni, Jeffrey Alan Stafford, James Veal
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Publication number: 20200172507Abstract: Crystals of a compound that exhibits an analgesic action against neuropathic pain and/or fibromyalgia syndrome are useful as pharmaceuticals. The crystals may be of (S)-1-(4-(dimethylamino)piperidin-1-yl)-3-hydroxy-3-(1-methyl-1H-imidazol-2-yl)propan-1-one or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: August 25, 2017Publication date: June 4, 2020Inventors: Hirozumi Takahashi, Yoko Baba, Yasuhiro Morita, Katsuhiko Iseki, Naoki Izumimoto
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Publication number: 20200172508Abstract: The present invention encompasses compounds of the formula I which are suitable for the treatment of diseases related to Vanin, and processes for making these compounds, pharmaceutical preparations containing these compounds, and their methods of use.Type: ApplicationFiled: December 2, 2019Publication date: June 4, 2020Inventors: Martin Thomas FLECK, Cedrickx GODBOUT, Hannes Fiepko KOOLMAN
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Publication number: 20200172509Abstract: The present invention provides a production method of heterocyclic compound having an excellent CH24H inhibitory action, which is suitable for industrial production. In the present invention, a 2-halogenonicotinic acid or a reactive derivative thereof or a salt thereof is reacted with 4-benzyl-4-hydroxypiperidine acid addition salt to give a (4-benzyl-4-hydroxypiperidin-1-yl)(2-halogenopyridin-3-yl)methanone or a salt thereof, and then the obtained compound is reacted with pyridine-4-boronic acid or a reactive derivative thereof or a salt thereof in the presence of a metal catalyst and a base to give (4-benzyl-4-hydroxypiperidin-1-yl) (2,4?-bipyridin-3-yl)methanone or a salt thereof.Type: ApplicationFiled: February 6, 2020Publication date: June 4, 2020Applicant: Takeda Pharmaceutical Company LimitedInventors: Fumiya Komura, Yoshihiro Higuchi
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Publication number: 20200172510Abstract: Provided in the present invention are a substituted amino six-membered nitric heterocyclic ring compound and a preparation and use thereof. In particular, provided in the present invention is a compound as shown by general formula (I) below, wherein the definition of each group is as described in the description. The compound of the present invention has an excellent tyrosine kinase inhibitory activity, and can thus be used to prepare a series of medicines for treating diseases related to tyrosine kinase inhibitory activity.Type: ApplicationFiled: February 17, 2017Publication date: June 4, 2020Inventors: Ao ZHANG, Meiyu GENG, Li XING, Jing AI, Zilan SONG, Xia PENG, Wangting GU, Jian DING
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Publication number: 20200172511Abstract: The present invention relates to a method for preparing substituted imidazolyl carboxyamides of the formula (II) proceeding from compounds of the formula (I) via an intermediate of the formula (IIIa) or (IIIb) in which the structural elements specified in the formulae (I), (II), (IIIa) and (IIIb) have the definitions stated. Furthermore, the invention relates to the compounds of the formulae (IIIa) and (IIIb).Type: ApplicationFiled: May 8, 2018Publication date: June 4, 2020Inventors: Marc MOSRIN, Matthieu WILLOT, Johannes-Rudolf JANSEN
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Publication number: 20200172512Abstract: The invention relates to pyrazole derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to HbS modulators of formula (I) or tautomers thereof, or pharmaceutically acceptable salts of said modulators or tautomers thereof, wherein X, Y, R2 and R3 are as defined in the description. HbS modulators are potentially useful in the treatment of a wide range of disorders, including sickle cell disease (SCD).Type: ApplicationFiled: November 26, 2019Publication date: June 4, 2020Applicant: Pfizer Inc.Inventors: Ariamala Gopalsamy, Arjun Venkat Narayanan, Agustin Casimiro-Garcia, Chulho Choi, David Hepworth, David Walter Piotrowski, Hatice Gizem Yayla, Jayasankar Jasti, Lee Richard Roberts, Lyn Howard Jones, Mihir Dineshkumar Parikh, Ming Zhu Chen, Olugbeminiyi Omezia Fadeyi, Ralph Pelton Robinson, JR., Robert Lee Dow, Shawn Cabral
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Publication number: 20200172513Abstract: This invention relates to new benzazepine carboxamide compounds of the formula wherein X and R1 to R6 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR8 agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer, autoimmune diseases, inflammation, sepsis, allergy, asthma, graft rejection, graft-versus-host disease, immunodeficiencies, and infectious diseases.Type: ApplicationFiled: February 5, 2020Publication date: June 4, 2020Applicant: Hoffmann-La Roche Inc.Inventors: Fabian Dey, Lisha Wang, Hongying Yun, Weixing Zhang, Zhiwei Zhang, Wei Zhu
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Publication number: 20200172514Abstract: The present invention provides processes for the preparation of Veliparib (1), as well as intermediates useful in the preparation thereof. In particular, processes are provided for the production of the compound of Formula (3), or a salt thereof, and cyclization to afford Veliparib (1).Type: ApplicationFiled: February 6, 2020Publication date: June 4, 2020Inventors: Prabhudas Bodhuri, Kaarina K. Milnes, Melanie R. A. Green, Gamini Weeratunga, Boris Gorin
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Publication number: 20200172515Abstract: Benzimidazole derivatives of formula (I): wherein: R1 is —(CH2)m-R4 or R2 is halo, —(CH2)m—NH2 or —(CH2)n—C(?NH)—NH2; R3 is H or F; R4 is —NH—(CH2)2—(NH)r—R5, —NH—(CHR5R6) or a group of the following formula (A): (A) W is —(CH2)m—, —CH2—O—CH2—, —CH2—S—CH2—, —(CH2)r—S(O)2—CH2— or —(CH2)r—NR5—CH2—; m is an integer of 1 to 3; n is 1 or 2; p is 1 and V is CH; or p is O and V is N; q is 0 or 1; r is 0 or 1; R5 is H, —SO2Me, —SO2Et, —SO2CF3, —COMe, —CONMe2, —CONH2 or —CH2CH2SO2Me; R6 is H or C1-C6 alkyl; and R7 is —SO2Me, —SO2Et, —SO2CF3, —COMe, —CONMe2, —CONH2 or —CH2CH2SO2Me; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.Type: ApplicationFiled: July 20, 2018Publication date: June 4, 2020Inventors: Stuart George Cockerill, James Good