Patents Issued in September 12, 2019
  • Publication number: 20190276390
    Abstract: The present invention relates to the formation of a stable dianionic ?-dimer-[TCNE]22? (TCNE-tetracyanoethylene) at ambient conditions that exhibits unusually intense white emission over the entire visible spectral range (400-800 nm) and has application in designing white light emitting devices. Particularly, the present invention relates to a process for the preparation of stable dimer in an organic solvent upon aging at room temperature, in the presence of anions such as Br?, Cl?, SCN?, which reduces the TCNE to a TCNE anion radical (TCNE.?) which subsequently dimerizes to form the stable dianionic dimer upon aging. More particularly, the dimer formed in this invention opens a new class of materials to design white light emitting devices having high intensity over the entire visible spectral range. The dimer also forms electron transfer salts used to develop new molecule-based metals, superconductors, and magnets.
    Type: Application
    Filed: March 11, 2019
    Publication date: September 12, 2019
    Inventors: Yatendra Singh Chaudhary, Biswajit Mishra, Surjendu Bhattacharyya
  • Publication number: 20190276391
    Abstract: The current invention offers a process for the production of N-Boc-2-amino-3,3-dimethylbutyric acid by a reaction of tert-Leucine with di-tert-butyl-dicarbonate, the process comprising (i) contacting the tert-Leucine with di-tert-butyl-dicarbonate in an aqueous medium, optionally comprising a first organic solvent, in the presence of an inorganic base, (ii) optionally removing the first organic solvent, (iii) optionally extracting the resulting N-Boc-2-amino-3,3-dimethylbutyric acid into a second organic solvent, (iv) isolating the product by precipitation from the reaction mixture at acidic pH, and (v) optionally reuse the first and/or second organic solvents recovered from step (ii) and/or step (iv) for the next production cycle. The process is sufficiently short, uses preferably environmental friendly solvents, avoids waste and leads to good yields.
    Type: Application
    Filed: November 23, 2017
    Publication date: September 12, 2019
    Applicant: Siegfried (Nantong) Pharmaceuticals Co. Ltd.
    Inventors: Jiang Chen, Christian Lothschuetz, Beat Theodor Weber
  • Publication number: 20190276392
    Abstract: The invention relates to a process for the production of urea ammonium nitrate, a system and a method of modifying a plant. The process comprises subjecting ammonia-containing off-gas resulting from the production of ammonium nitrate (AN off-gas) to condensation under acidic conditions so as to form an acidic condensate, and using at least part of the acidic condensate as an acidic scrubbing liquid in a finishing treatment section having a gas inlet in fluid communication with a gas outlet of a finishing section of a urea production unit, wherein the finishing section is adapted to solidify urea liquid, and wherein said finishing treatment section is adapted to subject ammonia-containing off-gas of the finishing section to treatment with an acidic scrubbing liquid.
    Type: Application
    Filed: May 28, 2019
    Publication date: September 12, 2019
    Applicant: Stamicarbon B.V.
    Inventors: Giusy Elisa PUCI, Joey DOBREE
  • Publication number: 20190276393
    Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapetitic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition, Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
    Type: Application
    Filed: October 10, 2018
    Publication date: September 12, 2019
    Applicant: Molecular Insight Pharmaceuticals, Inc.
    Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
  • Publication number: 20190276394
    Abstract: The present invention concerns a process for the continuous industrial preparation of an alkanesulphonic acid, from the corresponding alkane and sulphur trioxide, said process being carried out in a solvent which is the said alkane sulphonic acid.
    Type: Application
    Filed: February 28, 2019
    Publication date: September 12, 2019
    Applicant: Arkema France
    Inventor: Jean-Luc DUBOIS
  • Publication number: 20190276395
    Abstract: Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells.
    Type: Application
    Filed: March 1, 2019
    Publication date: September 12, 2019
    Inventors: David J. MALONEY, Diane K. LUCI, Ajit JADHAV, Theodore HOLMAN, Jerry L. NADLER, Michael HOLINSTAT, David TAYLOR-FISHWICK, Anton SIMEONOV, Adam YASGAR, Steven MCKENZIE
  • Publication number: 20190276396
    Abstract: The present invention relates to a multi-step process for the production of dihydrolipoic acid, which can particularly be carried out as a one-pot reaction and without isolation of intermediates.
    Type: Application
    Filed: December 22, 2017
    Publication date: September 12, 2019
    Applicant: ALZCHEM TROSTBERG GMBH
    Inventors: Ingo SCHNAPPERELLE, Stephan WINKLER, Jürgen SANS, Franz THALHAMMER
  • Publication number: 20190276397
    Abstract: The present invention relates to novel compounds containing fluorinated end groups, to the use thereof as surface-active substances, and to compositions comprising these compounds.
    Type: Application
    Filed: November 1, 2017
    Publication date: September 12, 2019
    Applicant: MERCK PATENT GMBH
    Inventors: Reiner FRIEDRICH, Fabian KOCH
  • Publication number: 20190276398
    Abstract: Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
    Type: Application
    Filed: February 12, 2019
    Publication date: September 12, 2019
    Inventor: Bing Wang
  • Publication number: 20190276399
    Abstract: Disclosed is a partly crystalline form of nintedanib ethanesulphonate and its preparation process.
    Type: Application
    Filed: June 6, 2017
    Publication date: September 12, 2019
    Applicant: Olon S.P.A.
    Inventors: Barbara Novo, Jacopo Bonanomi, Stella De Fiore, Francesco Calogero
  • Publication number: 20190276400
    Abstract: The invention particularly relates to crystalline (solid) forms of N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]acetamide), i.e. Form N, Form M, Form O and Form P. It also refers to a pharmaceutical composition or dosage form comprising said crystalline forms. The invention also concerns said pharmaceutical composition or dosage form for use in a method of treating a disease or disorder defined in the claims. Finally, the invention pertains to the use of said novel crystalline forms for the preparation of a pharmaceutical composition or dosage form.
    Type: Application
    Filed: November 21, 2016
    Publication date: September 12, 2019
    Applicant: ZAKLADY FARMACEUTYCZNE POLPHARMA SA
    Inventors: Monika ORACZ, Piotr GARCZAREK, Przemyslaw SKOCZEN, Dominika PODWYSOCKA, Marcin SZULC, Arkadiusz MAJEWSKI
  • Publication number: 20190276401
    Abstract: The present disclosure relates to novel, safe and efficient processes for the synthesis of Pimavanserin and salts thereof, as well as novel intermediates that can be used in these processes.
    Type: Application
    Filed: May 28, 2019
    Publication date: September 12, 2019
    Inventors: Tomislav BILJAN, Jasna DOGAN, Leonid METSGER, Sara Morasi PIPERCIC, Marina RATKAJ, Maja Matanovic SKUGOR, Yi WANG
  • Publication number: 20190276402
    Abstract: Intermediates and methods are provided for the preparation of selected C5aR antagonist compounds.
    Type: Application
    Filed: March 21, 2019
    Publication date: September 12, 2019
    Inventors: Pingchen FAN, Jaroslaw KALISIAK, Antoni KRASINSKI, Rebecca M. LUI, Jay POWERS, Sreenivas PUNNA, Hiroko TANAKA, Penglie ZHANG
  • Publication number: 20190276403
    Abstract: Provided herein is a process for the preparation of i-butyl 2-carbamothioyl-2-(3-(5-(4-cyanophenoxy)pyridin-2-yl)-2-(2,4-difluorophenyl)-3,3-difluoro-2-hydroxypropyl)hydrazine-1-carboxylate.
    Type: Application
    Filed: November 17, 2017
    Publication date: September 12, 2019
    Inventors: Kaitlyn Gray, Qiang Yang, Nicholas R. Babij, Yan Hao, Jim Renga
  • Publication number: 20190276404
    Abstract: This disclosure relates to picolinamides of Formula I and their use as fungicides.
    Type: Application
    Filed: March 8, 2019
    Publication date: September 12, 2019
    Applicant: Dow AgroSciences LLC
    Inventors: Brian A. Loy, Nicolaas Vermeulen, Brannon Sam, Kevin G. Meyer, Chenglin Yao, Nicholas R. Babij, Jeff Petkus
  • Publication number: 20190276405
    Abstract: Crystals of [8-chloro-3-(4-chlorobenzyl)-4-difluoromethoxy-2-ethylquinolin-5-yloxy]acetic acid L-lysine salt, i.e., a crystal A which has peaks at diffraction angles 2?=6.0°, 10.0°, 10.7°, 12.1°, 18.4°, 19.2° and 20.1° in powder X-ray diffraction spectra and a crystal B which has peaks at diffraction angles 2?=6.0°, 11.7°, 12.4°, 15.2°, 16.4°, 20.3° and 22.6° in powder X-ray diffraction spectra. These crystals are chemically stable and have excellent thermal stability and physical properties, and are therefore suitable as medicinal substances.
    Type: Application
    Filed: May 15, 2017
    Publication date: September 12, 2019
    Inventors: Donald John Daley, John Gary Montana, George Hynd, Mitsuru Teramoto, Takahiro Ito, Taro Tameyama
  • Publication number: 20190276406
    Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.
    Type: Application
    Filed: May 29, 2019
    Publication date: September 12, 2019
    Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
  • Publication number: 20190276407
    Abstract: A pyridonecarboxylic acid derivative or a salt thereof is represented by Formula (1), where R1 is hydrogen, a halogen atom, a lower alkyl group, or an amino group; R2 is —NH—R6, where R6 is hydrogen, a lower alkyl group, an amino lower alkyl group, or the like; —O—R7, where R7 is hydrogen, a lower alkyl group, or the like; —(CH2)m—R8, where R8 is an amino group or the like, m is 1, 2, 3 or 4; or a cyclic amino group of Formula (2), where Y represents NH or C—R9aR9b, where R9a and R9b are each independently hydrogen, a lower alkyl group, an amino group, a lower alkyl amino group, or the like; n and p are 1 or 2; R3 is hydrogen, a halogen atom, a lower alkyl group, or the like; R4 is hydrogen or a carboxyl group-protecting group; and R5 is hydrogen or a hydroxyl group-protecting group.
    Type: Application
    Filed: June 14, 2017
    Publication date: September 12, 2019
    Applicant: WAKUNAGA PHARMACEUTICAL CO., LTD.
    Inventors: Tomohiko KINOSHITA, Yasuhiro KURAMOTO, Satoshi INOUE, Kouji NISHIMURA, Tatsuya HIRANO, Mai ARAI, Asuka SAKURAI, Daichi KAZAMORI, Ayuka SASAKI
  • Publication number: 20190276408
    Abstract: The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof.
    Type: Application
    Filed: October 11, 2018
    Publication date: September 12, 2019
    Inventors: Claudia Witschi, Jung Min Park, Michael D. Thompson, Michael John Martinelli, David A. Yeowell, Michael P. Arend
  • Publication number: 20190276409
    Abstract: This invention concerns a process for the manufacture of carboxylic acids or carboxylic acid derivatives and a process for the manufacture of agrochemically and pharmaceutically active compounds comprising the process for the manufacture of carboxylic acids or their derivatives. The process for the manufacture of carboxylic acids or carboxylic acid derivatives comprises the steps of: a) halogenating a compound of formula (I): R1—C(O)—CHX2, to obtain a compound of formula (II): R1—C(O)—CX2X?, b) transforming the compound of formula (II) in the presence of a compound A into a compound of formula (III): R?C(O)Z, wherein Z is a residue selected from the group consisting of —OH, —O?, —NR?R?. The process can optionally comprise additional steps.
    Type: Application
    Filed: November 6, 2017
    Publication date: September 12, 2019
    Inventor: Janis JAUNZEMS
  • Publication number: 20190276410
    Abstract: Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
    Type: Application
    Filed: November 21, 2017
    Publication date: September 12, 2019
    Inventors: Mark Spyvee, Robert D. Ladner
  • Publication number: 20190276411
    Abstract: A simple method for producing a clinically applicable radiopharmaceutical composition containing 1-(2,2-dihydroxymethyl-3-[18F]fluoropropyl)-2-nitroimidazole ([18F]DiFA) or a salt thereof as an active ingredient, is provided which includes a synthesis step of obtaining a crude product of [18F]DiFA from a labeling precursor compound for [18F]DiFA; and a purification step of purifying the crude product, in which the purification step includes purifying [18F]DiFA using two or more different types of reverse phase solid phase extraction cartridges.
    Type: Application
    Filed: February 28, 2019
    Publication date: September 12, 2019
    Applicants: Nihon Medi-Physics Co., Ltd., National University Corporation Hokkaido University
    Inventors: Masato Kiriu, Soichi Nakamura, Yuji Kuge, Norifumi Abo
  • Publication number: 20190276412
    Abstract: An amidine containing at least one structural unit of the formula (I) and the use thereof as catalyst for the crosslinking of a functional compound, especially of a polymer having silane groups. The amidine is preparable in a simple process from readily available starting materials, is largely odorless at room temperature and is of low toxicity. It accelerates the crosslinking of functional compounds surprisingly efficiently and can be adjusted for optimal compatibility with different compositions via the radical to which the structural units of the formula (I) is bonded, which means that such compositions do not have a tendency to migration-related defects such as separation, exudation or substrate soiling.
    Type: Application
    Filed: December 12, 2017
    Publication date: September 12, 2019
    Applicant: SIKA TECHNOLOGY AG
    Inventors: Rita CANNAS, Urs BURCKHARDT
  • Publication number: 20190276413
    Abstract: The present invention relates to a pyrazine derivative, and preparation method and medical use thereof. The pyrazine derivative can remove free radicals and suppress calcium overload and has cytoprotective effects, and can be used for the prevention and treatment of cardiovascular and cerebrovascular diseases, neurodegenerative diseases and other related diseases.
    Type: Application
    Filed: July 4, 2016
    Publication date: September 12, 2019
    Applicant: GUANGZHOU MAGPIE PHARMACEUTICALS CO., LTD.
    Inventors: Yuqiang WANG, Pei YU, Yewei SUN, Luchen SHAN, Gaoxiao ZHANG, Zaijun ZHANG, Peng YI
  • Publication number: 20190276414
    Abstract: Relating to processes for preparing suvorexant or its pharmaceutically acceptable salts through the formation of a cocrystal of (R)-benzyl 5-methyl-1,4-diazepane-1-carboxylate hydrochloride with (R)-(+)-1,1,2-triphenyl-1,2-ethanediol ((R)-TED). This cocrystal provides the resolution of an intermediate of suvorexant, in particular, of (rac)-benzyl5-methyl-1,4-diazepane-1-carboxy-lateor a hydrochloride salt thereof. It also relates to a new cocrystal useful in such preparation processes.
    Type: Application
    Filed: June 2, 2017
    Publication date: September 12, 2019
    Inventors: Alexander Christian COMELY, Nicolas TESSON
  • Publication number: 20190276415
    Abstract: The present invention relates to compounds having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opiod receptor and more particularly to piperazine compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Application
    Filed: May 30, 2019
    Publication date: September 12, 2019
    Inventors: Félix CUEVAS-CORDOBÉS, Carmen ALMANSA-ROSALES, Monica GARCIA-LOPEZ
  • Publication number: 20190276416
    Abstract: A method for preparing a NOTA derivative is revealed. The method includes a plurality of steps. First take 4-toluenesulfonyl chloride and diethylenetriamine to carry out tosylation reaction and obtain a first product. Then the first substitution reaction takes place upon addition of the first product with sodium methoxide to get the second product. Next take 4-toluenesulfonyl chloride to react with ethylene glycol for preparing a third product by tosylation reaction therebewteen. Then a coupling reaction between the third product and the second product is carried out to produce a fourth product. The second substitution reaction occurs involving the fourth product in the presence of sulfuric acid. Lastly take the reaction product and hydrochloric acid to have bonding reaction and obtain a final product. The method solves the water-absorption problem of the cyclic organic compound TACN, a NOTA derivative.
    Type: Application
    Filed: March 6, 2018
    Publication date: September 12, 2019
    Inventors: YU CHANG, CHENG-FANG HSU
  • Publication number: 20190276417
    Abstract: Prodrugs of tizoxanide, an analogue or salt thereof are disclosed. The prodrugs have an ester moiety comprising an amino acid moiety, and increase the bioavailability of the tizoxanide, an analogue or salt thereof. Compositions and methods of treating an intracellular protozoan infection, a viral infection or a cancer are also disclosed.
    Type: Application
    Filed: May 23, 2019
    Publication date: September 12, 2019
    Applicant: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, Andrew Stachulski
  • Publication number: 20190276418
    Abstract: New classes of thiadiazole and oxadiazole compounds for use in LC mixtures are disclosed. In an embodiment, the new classes of thiadiazoles and oxadiazoles comprise at least one phenyl ring attached to the heterocyclic ring, where no alkyl, alkenyl or alkynyl tails are attached to the phenyl ring, but one alkyl, alkenyl or alkynyl tail is attached to the other end of the molecule, and a fluoro or cyano group appears in the para position of the phenyl ring. These compounds are disclosed as being effective at inducing smectic A phases in liquid crystal mixtures, particularly in liquid crystal mixtures also possessing a smectic C phase, more particularly in materials possessing a chiral smectic C (ferroelectric) phase.
    Type: Application
    Filed: March 7, 2018
    Publication date: September 12, 2019
    Inventors: William Thurmes, Christopher Gabriel
  • Publication number: 20190276419
    Abstract: The integrated process comprises a step a) of dehydrogenating propane providing a stream S1 comprising propane and propene; a step b) of separating stream S1 in at least one rectification column, providing an overhead product stream S2 comprising more than 99% by weight propene, a side stream S3 comprising from 90 to 98% by weight propene and a bottoms product stream S4 enriched in propane; a step c) of reacting propene with hydrogen peroxide in the presence of an epoxidation catalyst using propene in molar excess; and a step d) of separating non-reacted propene and propene oxide from the reaction mixture of step c) providing a propene oxide product and a stream S5 comprising propene and propane; wherein stream S3 is passed to step c), stream S5 is recycled to step b) and stream S4 is recycled to step a).
    Type: Application
    Filed: May 11, 2017
    Publication date: September 12, 2019
    Applicants: EVONIK DEGUSSA GMBH, thyssenkrupp Industrial Solutions AG
    Inventors: Holger WIEDERHOLD, David BOLZ, Georg Friedrich THIELE
  • Publication number: 20190276420
    Abstract: In alternative embodiments, provided are processes comprising the continuous isolation and purification of cannabinoids and further isomerization of the purified cannabidiol to ?8tetrahydrocannabinol (?8THC) and ?9tetrahydrocannabinol (?9THC). In alternative embodiments, provided are processes for converting ?8-THC into ?9-THC. In alternative embodiments, provided are processes for the industrial scale continuous isolation and purification of cannabinoids and further isomerization of the purified cannabidiol to ?9-THC.
    Type: Application
    Filed: April 18, 2019
    Publication date: September 12, 2019
    Inventors: Mark G. TEGEN, Joon CHO
  • Publication number: 20190276421
    Abstract: A compound useful as a release agent, and a release agent, a curable composition, and a nanoimprint lithography resin material each containing the compound are provided. More specifically, a calixarene compound with a molecular structure represented by the following structural formula (1) and a composition containing the calixarene compound are provided. wherein R1 denotes a structural moiety with a perfluoroalkyl group, R2 denotes a hydrogen atom, a polar group, a polymerizable group, or a structural moiety with a polar group or a polymerizable group, R3 denotes a hydrogen atom, an aliphatic hydrocarbon group that may have a substituent, or an aryl group that may have a substituent, n denotes an integer in the range of 2 to 10, and * denotes a bonding point with an aromatic ring.
    Type: Application
    Filed: November 16, 2017
    Publication date: September 12, 2019
    Inventors: Shinya Yamamoto, Masanori Miyamoto, Tomoyuki Imada
  • Publication number: 20190276422
    Abstract: Disclosed is a process for the extraction of furfural including: (a) subjecting a composition comprising furfural, water, at least one inorganic acid, at least one organic acid and a solvent mixture comprising an aromatic solvent and an oxygenate solvent, to a first separation step providing: (i) a first organic phase; (b) subjecting the first organic phase to a first distillation step providing: (i) a first top stream comprising furfural and a portion of the at least one organic acid; (c) subjecting the first top stream from step (b) to a second separation step providing: (i) a second top stream enriched with furfural; (d) subjecting the second top stream from step (c) to a second distillation step providing: (i) a third top stream comprising a furfural-water azeotrope, and (ii) a third bottom stream comprising furfural.
    Type: Application
    Filed: October 30, 2017
    Publication date: September 12, 2019
    Inventors: Juben Nemchand CHHEDA, Jean Paul Andre Marie Joseph Ghislain LANGE
  • Publication number: 20190276423
    Abstract: Disclosed are tricyclic heterocyclic compounds having kinase inhibitory activity, pharmaceutical compositions and kits comprising the compounds, and use of the compounds in the treatment of or in medicaments for the treatment of various diseases and conditions. In particular, disclosed are tricyclic heterocyclic compounds of the formula (I) having CSF-1R (c-FMS kinase) inhibitory activity and their use in the treatment of various diseases and conditions, such as those mediated by CSF-1R, including proliferative or neoplastic diseases and conditions, including cancers, and bone, inflammatory, and autoimmune diseases and conditions.
    Type: Application
    Filed: November 3, 2017
    Publication date: September 12, 2019
    Applicant: AUCKLAND UNISERVICES LIMITED
    Inventors: Swarnalatha Akuratiya GAMAGE, Peter Robin SHEPHERD, Jack Urquhart FLANAGAN, Gordon William REWCASTLE, Andrew James MARSHALL, Christina Maree BUCHANAN, Guo-Liang LU, Muriel BONNET, Stephen Michael Frazer JAMIESON, William Alexander DENNY
  • Publication number: 20190276424
    Abstract: The present invention provides processes for the preparation of Apalutamide (1), as well as intermediates useful in the preparation thereof. In particular, the process of the invention utilizes the intermediate compound of Formula (2), wherein G is OH or a leaving group, which provides improvements over the known processes for the preparation of Apalutamide (1).
    Type: Application
    Filed: March 6, 2019
    Publication date: September 12, 2019
    Inventors: Prabhudas Bodhuri, Alfredo Paul Ceccarelli, Michael R. Emmett, Avedis Karadeolian, Fabio E. S. Souza, Gamini Weeratunga, Boris Gorin
  • Publication number: 20190276425
    Abstract: The present disclosure describes biaryl triazole compounds, as well as their compositions and methods of use. The compounds inhibit the activity of macrophage migration inhibitory factor and are useful for the treatment of diseases, e.g., inflammatory diseases and cancer.
    Type: Application
    Filed: May 22, 2019
    Publication date: September 12, 2019
    Inventors: William L. Jorgensen, Pawel Dziedzic, Jose Cisneros
  • Publication number: 20190276426
    Abstract: The present invention provides novel compounds of Formula (I?), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, lymphoma)), 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 an interleukin-1 receptor-associated kinase (IRAK) (e.g., IRAKI and/or IRAK4) in the subject.
    Type: Application
    Filed: November 22, 2017
    Publication date: September 12, 2019
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Tinghu Zhang, John Hatcher, Sara Jean Buhrlage
  • Publication number: 20190276427
    Abstract: The present invention provides a process for preparing a compound of the formula (I): wherein each occurrence of R1 is a C1-C4 alkyl; and R2 is C1-C4 alkyl.
    Type: Application
    Filed: November 14, 2017
    Publication date: September 12, 2019
    Applicant: Adama Agan Ltd.
    Inventors: Tzurit Kusneic, Omer Tzor, Avihai Yacovan
  • Publication number: 20190276428
    Abstract: A method for producing (R)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione, the method comprising, (a) a step for isolating an isomer represented by formula (2) from a mixture of isomers represented by formula (1), and (b) a step for obtaining (R)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione by removing the menthyloxycarbonyl group from the compound represented by formula (2), which was isolated in step (a).
    Type: Application
    Filed: September 21, 2017
    Publication date: September 12, 2019
    Applicant: KAKEN PHARMACEUTICAL CO., LTD.
    Inventors: Yoshitake SUMIKAWA, Noriyuki KAMEI, Shingo TODO
  • Publication number: 20190276429
    Abstract: Provided herein is a process for the preparation of 4-(6-(2-(2,4-difluorophenyl)-1.1-difluoro-2-hydroxy-3-(5-mercapto-1H-1,2,4-triazol-1-yl)propyl)pyridin-3-yl)oxy)benzonitrile.
    Type: Application
    Filed: November 17, 2017
    Publication date: September 12, 2019
    Inventors: Qiang Yang, Nicholas R. Babij, Xiaoyong Li, Sarah Ryan, Yan Han
  • Publication number: 20190276430
    Abstract: Provided herein is a process for the preparation of 4-((6-(2-(2,4-difluorophenyl)-1, 1-difluoro-2-hydroxy-3-(5-mercapto-1H-1,2,4-triazol-1-yl)propyl)pyridin-3-yl)oxy)benzonitrile from 4-((6-(2-(2,4-difluorophenyl)-1,1-difluoro-3-hydrazinyl-2-hydroxypropyl)pyridin-3-yl)oxy)benzonitrile.
    Type: Application
    Filed: November 17, 2017
    Publication date: September 12, 2019
    Inventors: Kaitlyn Gray, Qiang Yang, Nicholas R. Babij
  • Publication number: 20190276431
    Abstract: Provided herein is a process for the preparation of 4-((6-(2-(2,4-difluorophenyl)-1,1-difluoro-2-hydroxy-3-(5-mercapto-1H-1,2,4-triazol-1-yl)propyl)pyridin-3-yl)oxy)benzonitrile.
    Type: Application
    Filed: November 17, 2017
    Publication date: September 12, 2019
    Inventors: Nicholas R. Babij, Qiang Yang, Sarah Ryan, Yan Hao, Gary Roth, Kaitlyn Gray
  • Publication number: 20190276432
    Abstract: The present invention provides compounds of formula I useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
    Type: Application
    Filed: July 27, 2017
    Publication date: September 12, 2019
    Inventors: Edward Jean Beaumont, Rajesh Devraj, Philip Stephen Kerry, Gnanasambandam Kumaravel, Pui Leng Loke, Mirco Meniconi, Jordan John Palfrey, Carl North, Cristine Lecci, Heather Tye
  • Publication number: 20190276433
    Abstract: The present invention provides novel compounds having the general formula (I): wherein R1, R2, R3, U, V, W, X and Y are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: November 2, 2017
    Publication date: September 12, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Zhanling CHENG, Jianhua WANG, Min WANG, Song YANG
  • Publication number: 20190276434
    Abstract: Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
    Type: Application
    Filed: December 1, 2017
    Publication date: September 12, 2019
    Applicant: Quentis Therapeutics, Inc.
    Inventors: Joseph P. Vacca, Dansu Li, Sarah Bettigole
  • Publication number: 20190276435
    Abstract: This application relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-? which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
    Type: Application
    Filed: March 7, 2019
    Publication date: September 12, 2019
    Inventors: Stacey Shepard, Andrew P. Combs, Nikoo Falahatpisheh, Lixin Shao
  • Publication number: 20190276436
    Abstract: The present invention provides compounds of the Formula (I), or a pharmaceutically acceptable salt thereof, where n and RI are defined herein, methods of treating patients for liver disease, and processes for preparing the compounds.
    Type: Application
    Filed: March 18, 2019
    Publication date: September 12, 2019
    Applicant: Eli Lilly and Company
    Inventors: David Andrew COATES, Luo Heng QIN, Yi WEI, Jingye ZHOU
  • Publication number: 20190276437
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula (1) wherein X1; X2; R1 and R4 are as defined herein.
    Type: Application
    Filed: May 14, 2019
    Publication date: September 12, 2019
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Benjamin Gerald Tehan, Barry John Teobald
  • Publication number: 20190276438
    Abstract: The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
    Type: Application
    Filed: March 18, 2019
    Publication date: September 12, 2019
    Inventors: Blair T. Lapointe, Peter H. Fuller, Hakan Gunaydin, Kun Liu, Mark E. Scott, B. Wesley Trotter, Hongjun Zhang
  • Publication number: 20190276439
    Abstract: Disclosed are methods for treating a solid tumor, such as a neuroendocrine tumor, in a patient comprising administration to the patient in need thereof a therapeutically effective amount of a compound that is an inhibitor of VEGFR 1, 2, and 3, FGFR 1, and CSF1R, such as N-(2-(dimethylamino)ethyl)-1-(3-((4-((2-methyl-1H-indol-5-yl)oxy)pyrimidin-2-yl)amino)phenyl)-methanesulfonamide.
    Type: Application
    Filed: November 18, 2016
    Publication date: September 12, 2019
    Inventors: Chuan QI, Jianming XU