Abstract: The present disclosure provides, in part, a solvent compound for use as a substitute for a glycol ether, an alkyl ether of diethylene glycol, ethylene glycol or propylene glycol.
Type:
Application
Filed:
October 1, 2018
Publication date:
August 20, 2020
Inventors:
David A. PASIN, Joseph Mitchell CLARKSON, Laurel L. SCHAFER
Abstract: The invention discloses a method for the preparation of substituted 4-(heptafluoro-2-propyl) anilines by reaction of 2-bromoheptafluoropropane with anilines in the presence of sodium dithionite, in a solvent and in the presence of a catalyst.
Type:
Application
Filed:
August 7, 2018
Publication date:
August 20, 2020
Inventors:
Florencio Zaragoza Doerwald, Daniel Zollinger
Abstract: [Problems to be solved] The present invention provides a novel diamine compound which allows for the synthesis of a polyimide compound having a high solubility in an organic solvent and a high melt moldability. [Solution] The diamine compound according to the present invention is characterized by being represented by the following general formula (1): (wherein R1 to R8 are each independently selected from the group consisting of a hydrogen atom, a fluorine atom, a substituted or unsubstituted alkyl group, and a substituted or unsubstituted aromatic group; and at least one of R1 to R8 is a substituted or unsubstituted aromatic group).
Abstract: [Problems to be Solved] The present invention provides a novel diamine compound which allows for the synthesis of a polyimide compound having a high solubility in an organic solvent and a high melt moldability. [Solution] The diamine compound according to the present invention is characterized by being represented by the following general formula (1): (wherein R1 to R8 are each independently selected from the group consisting of a hydrogen atom, a fluorine atom, a substituted or unsubstituted alkyl group, and a substituted or unsubstituted aromatic group; and at least one of R1 to R8 is a substituted or unsubstituted aromatic group).
Abstract: The present invention provides a process of producing a trifluoromcthoxylated aryl or trifluoromothoxylated heteroaryl having the structure: wherein A is an aryl or heteroaryl, each with or without substitution; and R1 is —H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), —NH-(alkyl), —N(alkyl)2, —NH-(alkenyl), —NH-(alkynyl) —NH-(aryl), —NH-(heteroaryl), —O-(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), —O-(heteroaryl), —S-(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), or —S-(heteroaryl), comprising: (a) reacting a compound having the structure: with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure: and (b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure:
Type:
Application
Filed:
May 6, 2020
Publication date:
August 20, 2020
Applicant:
The Research Foundation for the State University of New York
Abstract: The present invention relates to new enolate structures with utility as active pharmaceutical intermediates for the preparation of efficacious drugs such as those derived from 5-fluorocytosine (5-FC).
Abstract: The present invention relates to a method of manufacturing norbixin or bixin ethyl ester, which is a carotenoid-based compound, from a novel intermediate compound. When the novel intermediate compound is used, it is possible to manufacture norbixin or bixin ethyl ester in high yield through a simple process.
Type:
Application
Filed:
July 12, 2019
Publication date:
August 20, 2020
Applicant:
MYONGI UNIVERSITY INDUSTRY AND ACADEMIA COOPERATION FOUNDATION
Inventors:
Sangho KOO, Dahye Kim, Mohammad Shariful Alam
Abstract: The present invention provides an optical component forming composition comprising a tellurium-containing compound or a tellurium-containing resin.
Type:
Application
Filed:
April 28, 2017
Publication date:
August 20, 2020
Inventors:
Masatoshi ECHIGO, Tomoaki TAKIGAWA, Takumi TOIDA, Takashi SATO
Abstract: The present invention provides process for preparation of molindone (I) comprising: a) reacting compound with cyclohexane-1,3-dione to form 2-(2-oxopentan-3-yl)cyclohexane-1,3-dione wherein X is Cl, Br or I, b) cyclizing 2-(2-oxopentan-3-yl)cyclohexane-1,3-dione to 2-methyl-3-ethyl-4-oxo-4,5,6,7-tetrahydroindole, c) reacting 2-methyl-3-ethyl-4-oxo-4,5,6,7-tetrahydroindole with morpholine and formaldehyde to give molindone (I), and d) optionally converting molindone (I) to its salt. The present invention further provides process for preparation of compound comprising: a) reacting compound with ethyl halide and another halide source to form compound wherein R is alkyl and X is Cl, Br or I; b)converting compound to compound.
Type:
Application
Filed:
February 14, 2020
Publication date:
August 20, 2020
Applicant:
LUPIN LIMITED
Inventors:
Amit Madanrao AGARKAR, Tejas Vilas PURANIK, Rajesh Bharat GAPAT, Umesh Babanrao RANANAWARE, Radhakrishna Bhikaji SHIVDAVKAR, Girij Pal SINGH
Abstract: The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction.
Type:
Application
Filed:
April 30, 2020
Publication date:
August 20, 2020
Applicant:
Supernus Pharmaceuticals, Inc.
Inventors:
Martin Hanbauer, Zarghun Nazir, Peter Hildebrand, Attilia Figini, Likan Liang, Tiziano Fumagalli
Abstract: Pharmaceutical and chemical intermediates and relevant chemicals, and relates to a novel preparation method of N-substituted dibenzo[a,c]carbazole compound. O-alkynylaniline and derivatives thereof as raw materials conduct a cascade cyclization reaction in an anhydrous organic solvent in the presence of catalysts, oxidants and additives, and are converted into the N-substituted dibenzo[a,c]carbazole compound. The preparation method of the N-substituted dibenzo[a,c]carbazole compound has fewer reaction steps, low cost of raw material, mild reaction conditions and convenient operation. Moreover, the obtained product has high yield and high purity, fully meets the quality requirements for drug intermediates, and provides favorable conditions for the industrial production.
Type:
Application
Filed:
June 7, 2018
Publication date:
August 20, 2020
Inventors:
Sheng ZHANG, Hengmin MA, Tienan JIN, Ming BAO
Abstract: A quinoline derivative compound shown in formula (II), a pharmaceutically acceptable salt thereof, and an application of the same in preparing a drug for treating a disease related to a tyrosine kinase inhibitor.
Abstract: The present invention relates to a co-crystal of roxadustat with L-proline and to a process for its preparation. Furthermore, the invention relates to a pharmaceutical composition comprising said roxadustat L-proline co-crystal, at least one pharmaceutically acceptable excipient and optionally at least one photostabilizing agent. The pharmaceutical composition of the present invention can be used as a medicament, in particular for the treatment and/or prevention of anemia in patients with end-stage renal disease (ESRD) and/or chronic kidney disease (CKD).
Type:
Application
Filed:
July 11, 2018
Publication date:
August 20, 2020
Applicant:
Sandoz AG
Inventors:
Hannes Lengauer, Arthur Pichler, Renate Margreiter, Thomas Gelbrich
Abstract: The present invention provides substituted heterocyclylderivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors. These compounds are useful in the treatment and prevention of diseases and/or disorders associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted heterocyclyl derivatives of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.
Abstract: Provided herein are compounds of Formula I and Formula II, and compositions comprising the same, as well as methods of use thereof for treating kidney stones (e.g., inhibiting the formation of oxalate kidney stones; treating primary hyperoxaluria), inhibiting the production of glyoxylate and/or oxalate, and/or inhibiting glycolate oxidase (GO).
Type:
Application
Filed:
December 7, 2016
Publication date:
August 20, 2020
Inventors:
W. Todd Lowther, Ross P. Holmes, Daniel Yohannes
Abstract: The present invention relates to compounds of formula M in which RM has the meaning indicated in claim 1, to liquid crystal mixture comprising the same, to the use of these liquid-crystal media, in particular in components for high-frequency technology, and to components of this type which contain media according to the invention, and to the production and use of these components. The components according to the invention are suitable, in particular, as phase shifters in the microwave and millimetre wave region, for microwave and millimetre wave array antennae and very particularly for so-called tunable “reflectarrays”.
Abstract: A compound represented by Formula (I): Chemical Formula 1 wherein Chemical Formula 2 or the like Y1 is O or the like; Z1 is C(R4) or N; Z2a is C(R5a) or the like; Z3a is C(R6) or the like; R4, R5a and R6 are each independently a hydrogen atom or the like; R1 is substituted or unsubstituted aromatic carbocyclyl or the like; R2a, R2b, R2c and R2d are each independently a hydrogen atom or the like; X is N(R7a) or the like; R7a is a hydrogen atom or the like; R3 is Chemical Formula 3 or the like Ring B is a 6-membered aromatic carbocycle or the like; R9a and R10a are each independently halogen or the like; n is an integer from 1 to 5; m is an integer from 0 to 4; and p is an integer from 0 to 3, or a pharmaceutically acceptable salt thereof.
Abstract: The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1-propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others.
Type:
Application
Filed:
May 4, 2020
Publication date:
August 20, 2020
Inventors:
John J. Freeman, Adrienne Stamper, Melissa Heitmann
Abstract: The present invention relates to a compound represented by any one of the following formula A to formula C, and a photosensitive composition comprising the same, wherein the structure of the compound represented by any one of formula A to formula C is as described in the detailed description of the invention.
Type:
Application
Filed:
September 10, 2018
Publication date:
August 20, 2020
Inventors:
Gyu Sung LEE, Bong Seok MOON, Sung Min CHIN, Ji Soung KANG, Min Su HA, No Gill PARK, Hyun Woo LEE, Ugun BYUN
Abstract: Novel hydrogen isotope-enriched 1,2,4-oxadiazole benzoic acid compounds, methods of their use and pharmaceutical compositions thereof are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination.
Abstract: Disclosed is a polymerizable compound useful in the preparation of a polymer which is capable of producing, for example, an optical film having excellent in-plane thickness uniformity and improved in-plane uniformity in optical properties.
Type:
Application
Filed:
March 16, 2018
Publication date:
August 20, 2020
Applicant:
ZEON CORPORATION
Inventors:
Kei SAKAMOTO, Kumi OKUYAMA, Takanori MIMA
Abstract: This invention provides preparations, compositions, products, and applications of photo-crosslinked hydrogels. Component A—a photosensitive polymer derivative, component B—the photoinitiator, and auxiliary component C—other biocompatible polymer derivative each are respectively dissolved in a biocompatible medium to obtain solution A, solution B, and solution C. The solution A, the solution B, and the optional solution C are mixed homogenously to obtain a hydrogel precursor solution. The hydrogel precursor solution is subject to irradiation of the UV light for photocoupled crosslinking to form a photo-crosslinked hydrogel. The photo-crosslinked hydrogel exhibit rapid speed of photo-curing, strong tissue adhesion, excellent mechanical properties, good biocompatibility, and excellent clinical operability.
Abstract: The invention relates to a process for separating furanic compounds from a feedstock additionally containing dimethoxysulfoxide (DMSO). These furanic compounds are in particular 5-hydroxymethylfurfural (5-HMF), 2,5-diformylfuran (DFF), 2,5-furanedicarboxylic acid (FDCA) or dimethyl 2,5-furandicarboxylate (DMFDCA). The process successively comprises a) bringing the feedstock into contact with water originating from step c), then b) a liquid-liquid extraction with an organic solvent followed by a back extraction c) by the water added in order to obtain an organic extract rich in furanic compounds. The extract may then be subjected to a crystallization step d) and then a filtration in order to obtain the solid furanic compound. The water-rich or solvent-rich effluents are advantageously recycled respectively to the back extraction and the extraction.
Abstract: Isotopically-stabilized tetronimide compounds comprising one or more deuterium atoms, derivatives, and intermediates, thereof, including methods for their synthesis, pharmaceutical compositions thereof, and methods of using these compounds to interact with target molecules in cell-free samples, cell- and tissue-based assays, animal models, and in a subject are disclosed. One aspect relates to molecules that modulate the expression or catalytic activity of aspartyl (asparaginyl) ?-hydroxylase (ASPH) within or on the surface of a cell. Other aspects of the invention relate to use of the molecules disclosed herein to diagnose, ameliorate, or treat cell proliferation disorders and related diseases. Related aspects include uses of the compounds to modulate the activity of viruses, as anti-hyperlipidemia agents, and as agents to ameliorate or treat thrombosis and related cardiovascular and metabolic disorders.
Abstract: The present invention relates to novel compounds, particularly to hydrophilic compounds, comprising a photoactive unit, said novel compounds being particularly suitable for ophthalmic devices. The present application also relates to ophthalmic devices comprising such compounds.
Type:
Application
Filed:
May 7, 2020
Publication date:
August 20, 2020
Applicant:
Merck Patent GmbH
Inventors:
Lars DOBELMANN-MARA, Stefan RIEDMUELLER, Martin SCHRAUB
Abstract: The present invention provides methods of extraction of at least one cannabinoid from an initial cannabis biomass in “one-pot” step using toluene to form a toluene extract and using the toluene extract for producing high concentrations of ?-9-tetrahydrocannabinol (?9THC) and/or cannabinol (CBN) of a purity of at least 75% and at a yield of at least 75% by weight of the at least one cannabinoid from the initial cannabis biomass in the toluene extract.
Type:
Application
Filed:
February 13, 2020
Publication date:
August 20, 2020
Inventors:
Dylan James WEBB, Paul George HAYES, Igor KOVALCHUK
Abstract: The present specification provides a compound represented by Chemical Formula 1, a colorant composition, a resin composition, a photosensitive material, a color filter and a display device comprising the same.
Type:
Application
Filed:
February 26, 2020
Publication date:
August 20, 2020
Applicant:
LG CHEM, LTD.
Inventors:
Jongho PARK, Dami LEE, Seung Jin YANG, Jihye JUNG
Abstract: The present invention generally relates to various dibenzothiophene compounds, processes for preparing these compounds, and uses of these compounds. The present invention also relates to cell imaging agents comprising one or more of the dibenzothiophene compounds and processes for imaging a cell using the compounds. The present invention further relates to methods of producing ground state atomic oxygen.
Abstract: Disclosed is a compound of formula I or a pharmaceutically acceptable hydrate, solvate, crystal, co-crystal, enantiomer, stereoisomer, polymorph or prodrug thereof, which is useful for treatment of eye disorders, skin diseases and/or complications associated therewith. Also disclosed is a pharmaceutical composition comprising as an active ingredient at least one compound of formula I and a pharmaceutically acceptable excipient. Also disclosed is a method of treating an eye disorder, skin disease and/or a complication thereof in a subject in need thereof by administering at least one compound of formula I or a pharmaceutically acceptable hydrate, solvate, crystal, co-crystal, enantiomer, stereoisomer, polymorph or prodrug thereof.
Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione monohydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione monohydrate are also disclosed.
Abstract: The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3 (wherein R3 is piperidin-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3 (wherein R3 is as defined hereinbefore); 3) C2-5alkynylR3 (wherein R3 is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
Type:
Application
Filed:
September 25, 2019
Publication date:
August 20, 2020
Applicant:
Genzyme Corporation
Inventors:
Andrew Peter Thomas, Elaine Sophie Elizabeth Stokes, Laurent Francois Andre Hennequin
Abstract: Provided are 4,5,6-tri-substituted indazoles derivatives, a preparation method therefor, and a use thereof in medicines. Specifically, provided are compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates, or prodrugs thereof, a preparation method therefor, and a use thereof.
Type:
Application
Filed:
November 10, 2017
Publication date:
August 20, 2020
Inventors:
Jianbiao PENG, Yang LIU, Lixiao WANG, Zhihua FANG, Zonglei FEI, Xi CHEN, Jiong LAN
Abstract: The present disclosure relates to 1,5,7-trisubstituted isoquinoline derivatives, their preparation and pharmaceutical use. In particular, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. The definitions of the groups in the formula can be found in the specification and claims.
Abstract: PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
Type:
Application
Filed:
October 28, 2019
Publication date:
August 20, 2020
Inventors:
Michael Joseph Luzzio, Julien Papillon, Michael Scott Visser
Abstract: The present disclosure relates to a compound of formula (Ia), (Ib), (IIa), and (IIb): which are useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.
Type:
Application
Filed:
November 25, 2019
Publication date:
August 20, 2020
Inventors:
Michael Graupe, Steven J. Henry, John O. Link, Charles William Rowe, Roland D. Saito, Scott D. Schroeder, Dimitrios Stefanidis, Winston C. Tse, Jennifer R. Zhang
Abstract: Compound of formula (I): wherein Het, R3, R4, R5, R7, R8, R9, t, p, p?, q, and q? are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring pro-apoptotic agent.
Type:
Application
Filed:
May 4, 2020
Publication date:
August 20, 2020
Inventors:
James Edward Paul DAVIDSON, James Brooke MURRAY, I-Jen CHEN, Claire WALMSLEY, Mark DODSWORTH, Johannes W.G. MEISSNER, Paul BROUGH, lmre FEJES, János TATAI, Miklós NYERGES, András KOTSCHY, Zoltán SZLÁVIK, Olivier GENESTE, Arnaud LE TIRAN, Thierry LE DIGUARHER, Jean-Michel HENLIN, Jérôme-Benoît STARCK, Anne-Françoise GUILLOUZIC, Guillaume DE NANTEUIL
Abstract: The present invention provides compounds of the Formula (I), or a pharmaceutically acceptable salt thereof, where n and R1 are defined herein, methods of treating patients for liver disease, and processes for preparing the compounds,
Type:
Application
Filed:
September 26, 2019
Publication date:
August 20, 2020
Applicant:
Eli Lilly and Company
Inventors:
David Andrew COATES, Luo Heng QIN, Yi WEI, Jingye ZHOU
Abstract: Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I? and I?? or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.
Type:
Application
Filed:
May 5, 2020
Publication date:
August 20, 2020
Applicant:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, William Greenlee
Abstract: Described are benzoimidazole indolyl methane compounds, pharmaceutical compositions containing them, and use of the compounds to inhibit PCSK9-mediated ailments.
Type:
Application
Filed:
February 13, 2020
Publication date:
August 20, 2020
Inventors:
Weiping Tang, Gabrielle N. Winston McPherson, Haibo Xie, Alan D. Attie, Mark Patrick Keller, Ka Yang
Abstract: The present invention is relates to an improved process for the preparation of pazopanib or a pharmaceutically acceptable salts thereof. The present invention also relates to novel polymorphic Forms of pazopanib hydrochloride, and its intermediates thereof.
Abstract: Disclosed are compounds that modulate the physiological action of the proprotein convertase subtilisin kexin type 9 (PCSK9), as well as therapeutic methods for use of such compounds to reduce LDL-cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease (CVD), including treatment of hypercholesterolemia.
Type:
Application
Filed:
May 6, 2020
Publication date:
August 20, 2020
Inventors:
Sherin Salaheldin Abdel-Meguid, Nabil A. Elshourbagy, Harold V. Meyers, Shaker A. Mousa
Abstract: The present invention relates to methods of treating cancer by administering the EZH2 inhibitor compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
Type:
Application
Filed:
January 22, 2020
Publication date:
August 20, 2020
Inventors:
Sarah K. KNUTSON, Natalie WARHOLIC, Heike KEILHACK
Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1. Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi.
Type:
Application
Filed:
September 11, 2018
Publication date:
August 20, 2020
Applicant:
SYNGENTA PARTICIPATIONS AG
Inventors:
Farhan BOU HAMDAN, Matthias WEISS, Laura QUARANTA
Abstract: The present disclosure relates to compounds of formula I that are useful as modulators of 7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation (I).
Type:
Application
Filed:
September 14, 2018
Publication date:
August 20, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Ian M. Bell, Brendan M. Crowley, Peter J. Manley, William D. Shipe
Abstract: An aromatic derivative as represented by formula (I), a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising same, a preparation method therefor, and uses of the aromatic derivative and the pharmaceutically acceptable salt thereof or the pharmaceutical composition comprising same in preparing a therapeutic agent, specifically an FGFR4 tyrosine kinase inhibitor, and in preparing a medicament for treating and/or preventing neoplastic and inflammatory diseases. The substituents of formula (I) are same as defined in the description.
Type:
Application
Filed:
September 4, 2018
Publication date:
August 20, 2020
Applicant:
BIOARDIS LLC
Inventors:
Ning SHAO, Ding WANG, Hongbin YUAN, Frank KAYSER
Abstract: The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
Type:
Application
Filed:
October 24, 2018
Publication date:
August 20, 2020
Inventors:
Matthew LUCAS, Bertrand LE BOURDONNEC, Iwona WRONA, Bhaumik PANDYA, Parcharee TIVITMAHAISOON, Kerem OZBOYA, Benjamin VINCENT, Daniel TARDIFF, Jeff PIOTROWSKI, Eric SOLIS, Robert SCANNEVIN, Chee-Yeun CHUNG, Rebecca ARON, Kenneth RHODES
Abstract: The present invention provides a compound represented by the following formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof. wherein: R1 and R2 are each separately selected from the group consisting of hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl; R3 is hydrogen or halogen; ring A is a benzene ring or a pyridine ring; ring B is selected from the group consisting of the following formulas (i), (ii), (iii), and (iv): in the formula (ii), Ra is alkyl; R4 and R5 are each separately selected from the group consisting of hydrogen, hydroxy, alkoxy, haloalkoxy, halohydroxyalkoxy, and aminoalkyl; and [Formula 3] represents a double bond or a triple bond. The above compound can be used as a molecular probe for imaging tau proteins that accumulate in the brain.