Abstract: Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R1A to R4A are defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating cough, itch, acute pain and neuropathic pain disorders using the same.
Type:
Application
Filed:
November 13, 2017
Publication date:
April 30, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Thomas J. Greshock, James Mulhearn, Anthony J. Roecker, Tianying Jian, Gang Zhou, Liangqin Guo, Walter Won, Ting Zhang, Rajan Anand, John E. Stelmach, Deping Wang, Ronald M. Kim, Mark E. Layton, Christopher S. Burgey, Philippe G. Nantermet
Abstract: The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
Type:
Application
Filed:
May 30, 2019
Publication date:
April 30, 2020
Inventors:
William W. Turner, JR., Lee D. Arnold, Hans Maag, Leping Li, Mark G. Bures, Simon Nicolas Haydar, Samson Francis
Abstract: The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.
Type:
Application
Filed:
October 1, 2019
Publication date:
April 30, 2020
Applicant:
Bayer Aktiengesellschaft
Inventors:
Adam James DAVENPORT, Nico BRÄUER, Oliver Martin FISCHER, Andrea ROTGERI, Antje ROTTMANN, Ioana NEAGOE, Jens NAGEL, Anne-Marie GODINHO-COELHO, Jürgen KLAR
Abstract: The invention relates to compounds of formula (I), compositions containing the same, and methods for treating and/or diminishing pain in a subject. The compounds of formula (I) are effective for treating opioid-induced tachyphylaxis and opioid-induced hyperalgesia.
Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
Type:
Application
Filed:
December 30, 2019
Publication date:
April 30, 2020
Inventors:
Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
Abstract: This application is directed to inhibitors of dynamin-1-like protein (Drp1) represented by the following structural formula (I): and methods for their use, such as to treat one or more DRP1-related diseases.
Type:
Application
Filed:
April 25, 2018
Publication date:
April 30, 2020
Inventors:
Nan Ji, Jeyaprakash Narayanan Seenisamy
Abstract: Provided is a compound selected from compounds of Formula (I) and pharmaceutically acceptable salts, solvates, and hydrates thereof: (I) wherein R1, R2, R3 and R4 are as defined herein. Such compounds are inhibitors of the vesicular monoamine transporter 2 (VMAT2) and have utility for treating, for example, neurological and psychiatric diseases and disorders. Also disclosed are compositions containing such compounds in combination with a pharmaceutically acceptable carrier, as well as methods relating to their use in subjects in need thereof.
Type:
Application
Filed:
April 17, 2018
Publication date:
April 30, 2020
Inventors:
Nicole Harriott, Donald Hettinger, Shawn Branum, Jeffrey C. Culhane
Abstract: The present invention provides a compound or a salt thereof having a calcium-sensing receptor antagonistic activity, and being expected to be useful as an agent for preventing or treating heart failure, pulmonary hypertension, or the like. The compounds represented by formula (I) or a salt thereof has a calcium-sensing receptor antagonistic activity, and is expected to be useful as an agent for preventing or treating heart failure, pulmonary hypertension, or the like, wherein each symbol is as described in the specification.
Type:
Application
Filed:
April 26, 2018
Publication date:
April 30, 2020
Inventors:
Shuji KITAMURA, Zenichi IKEDA, Sachie MORIMOTO, Minoru IKOMA, Koji WATANABE, Hideki HIROSE, Takafumi YUKAWA, Kenjiro SATO
Abstract: The present invention covers azaquinoline compounds of general formula (I), with A being (A1) or (A2), and in which T, R1, R2, R3, R4, R5, R6 and Q are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.
Type:
Application
Filed:
June 22, 2018
Publication date:
April 30, 2020
Applicant:
BAYER ANIMAL HEALTH GMBH
Inventors:
Nils GRIEBENOW, Wei ZHUANG, Adeline KÖHLER, Daniel KULKE, Claudia BÖHM, Kirsten BÖRNGEN, Thomas ILG, Hans-Georg SCHWARZ, Werner HALLENBACH, Ulrich GÖRGENS, Walter HÜBSCH, Bernd ALIG, Iring HEISLER, Isa Jana Irina JANSSEN
Abstract: The present invention provides compounds of Formula (I) or a subgeneric structure or species thereof, or a pharmaceutically acceptable salt, ester, solvate, and/or prodrug thereof, and methods and compositions for treating or ameliorating abnormal cell proliferative disorders, such as cancer, wherein A, R2, R3, R10, E1, E2, E3, Y, and Z are as defined herein.
Type:
Application
Filed:
July 5, 2018
Publication date:
April 30, 2020
Inventors:
Yuntao SONG, Alexander James BRIDGES, Xiaoqi CHEN
Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
Type:
Application
Filed:
July 5, 2018
Publication date:
April 30, 2020
Applicant:
SYNGENTA PARTICIPATIONS AG
Inventors:
Sebastian RENDLER, Andrew EDMUNDS, Michel MUEHLEBACH, Daniel EMERY, Girish RAWAL, Indira SEN, Vikas SIKERVAR
Abstract: The invention provides a compound of formula 1 or a pharmaceutically-acceptable salt thereof, that is useful as a JAK inhibitor. The invention also provides pharmaceutical compositions comprising the compound, methods of using the compound to treat diseases amenable to a JAK inhibitor, and processes useful for preparing the compound.
Abstract: The present invention provides crystalline solids of 6?-((6-aminopyrimidin-4-yl)amino)-8?-methyl-2?H-spiro[cyclohexane-1,3?-imidazo[1,5-a]pyridine]-1?,5?-dione: The crystalline compounds of the present application are inhibitors of Mnk and finds utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
Type:
Application
Filed:
October 23, 2019
Publication date:
April 30, 2020
Inventors:
Siegfried H. Reich, Paul A. Sprengeler, Stephen E. Webber, Alan X. Xiang, Justin T. Emst, Bennett C. Borer, Samuel Sperry, Jo Ann Z. Wilson
Abstract: Described are positive allosteric modulators of muscarinic acetylcholine receptor M1 (mAChR M1), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating neurological disorders, psychiatric disorders, or a combination thereof.
Type:
Application
Filed:
October 24, 2019
Publication date:
April 30, 2020
Inventors:
Craig W. Lindsley, P. Jeffrey Conn, Darren W. Engers, Julie L. Engers, Madeline Long, Aaron M. Bender
Abstract: The present invention relates to solid forms of the insecticide of formula I: I, compositions comprising the solid forms and methods of their use as insecticides.
Type:
Application
Filed:
December 15, 2017
Publication date:
April 30, 2020
Applicant:
SYNGENTA PARTICIPATIONS AG
Inventors:
Ian Kevin JONES, John HONE, Neil GEORGE
Abstract: The present invention relates to solid forms of the insecticide of formula (I): (I) compositions comprising the solid forms and methods of their use as insecticides.
Type:
Application
Filed:
December 15, 2017
Publication date:
April 30, 2020
Applicant:
SYNGENTA PARTICIPATIONS AG
Inventors:
Ian Kevin JONES, John HONE, Neil GEORGE
Abstract: Disclosed is a composition and method for a therapeutic treatment that is able to combat certain conditions such as alcohol dependence, opioid abuse treatment, neurological disorders, neuropathic pain, and fibromyalgia. The novel gliotoxin analog compound acts by acting as an antagonist to one or more opioid receptors, which, when present leads to the inhibition of conditions, providing increased performance over known treatments. The disclosed compounds also shows the ability to cross the blood-brain-barrier in a highly efficient manner.
Abstract: Provided are a compound represented by formula (I), an isomer or a pharmaceutically acceptable salt thereof, and an application of the same in preparing a drug for treating a disease related to A2A receptor. The R1, R2, R3, ring A, ring B, n, and m are as defined in the specification.
Type:
Application
Filed:
April 6, 2018
Publication date:
April 30, 2020
Applicant:
MEDSHINE DISCOVERY INC.
Inventors:
KEVIN X CHEN, Yanxin YU, Xinde CHEN, Li ZHANG, Zhaoguo CHEN, Cheng XIE, Xiaofei WANG, Linghui WU, Guoping HU, Jian LI, Shuhui CHEN
Abstract: This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.
Type:
Application
Filed:
September 4, 2019
Publication date:
April 30, 2020
Inventors:
Yun-Long Li, Xiaozhao Wang, Chunhong He
Abstract: The present disclosure relates to an improved process for the synthesis of piperazine ring, particularly for the preparation of heterocyclic compounds useful as intermediates in the synthesis of pyrazinocarbazoles such as the antidepressant Pirlindole. The process described is useful to prepare Pirlindole enantiomers, or a pharmaceutically accepted salt thereof.
Type:
Application
Filed:
April 20, 2018
Publication date:
April 30, 2020
Inventors:
Carla Patrícia DA COSTA PEREIRA ROSA, João Carlos RAMOS DAMIL, Ana Vanessa CORDEIRO SIMÕES, João Pedro SILVA SERRA
Abstract: A heteroaryl-pyrazole derivative, and a preparation method therefor and a medical application thereof are described. Specifically, a new heteroaryl-pyrazole derivative as shown in formula (I), a preparation method for the derivative, a pharmaceutical composition containing the derivative, and a use of the derivative as a therapeutic agent, in particular as a TLR7 agonist, are described. The substituents in formula (I) have the same definitions as in the description.
Abstract: The present invention relates to substituted pyrazolo-quinazoline derivatives which modulate the activity of Choline Kinase (ChoK). The compounds of this invention are therefore useful in treating diseases caused by an altered choline metabolism, such as cancer, cell proliferative disorders, infectious diseases of different origin, immune-related disorders and neurodegenerative disorders. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
Type:
Application
Filed:
July 3, 2018
Publication date:
April 30, 2020
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Alessandra BADARI, Elena CASALE, Marcella NESI, Francesca QUARTIERI
Abstract: Provided is 5-(3-chloro-4-fluorophenyl)-7-cyclopropyl-3-(2-(3-fluoro-3-methylazetidin-1-yl)-2-oxoethyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one and pharmaceutically acceptable salts thereof, and their uses in the treatment of psychiatric, neurological, and neurodevelopmental disorders, as well as diseases of the nervous system.
Type:
Application
Filed:
November 8, 2019
Publication date:
April 30, 2020
Inventors:
David R. Anderson, Robert A. Volkmann, Gregg F. Keaney, Steven C. Leiser, Sam Malekiani, Timothy Piser
Abstract: The invention provides a series of conformationally stable kinase inhibitors, and methods of using the kinase inhibitors. The effect of atropisomerism on kinase selectivity was assessed, finding improved selectivity compared to rapidly interconverting parent compounds.
Type:
Application
Filed:
December 18, 2019
Publication date:
April 30, 2020
Applicant:
SAN DIEGO STATE UNIVERSITY RESEARCH FOUNDATION
Inventors:
Jeffrey L. GUSTAFSON, Davis E. SMITH, David HECHT, Isaac MARQUEZ, Sean TOENJES
Abstract: Disclosed are imidazo[1,2-b]pyrimido[4,5-d]pyridazin-5(6H)-one compounds, specifically represented by the Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A and R1-R5 are defined herein. Compounds having Formula I are Wee1 kinase inhibitors. Therefore, compounds of the disclosure may be used to treat diseases caused by abnormal Wee1 activity.
Type:
Application
Filed:
July 10, 2018
Publication date:
April 30, 2020
Applicant:
IMPACT THERAPEUTICS, INC.
Inventors:
Suixiong CAI, Ye Edward TIAN, Zhiqiang DONG, Xiaozhu WANG
Abstract: [Problem] A problem is presented in that conventional photochromic compounds cannot be considered adequate in terms of the colorizing/decolorizing rate and durability, and the production process therefore has many steps. The present invention provides an industrially applicable photochromic compound that has both a rapid colorizing/decolorizing reaction and high durability and can also be synthesized at a low cost. [Solution] This compound is characterized in that etheric oxygen atoms are bonded to the carbon atoms at position 1 of a pyranoquinazoline (8H-pyrano[3,2-f]quinazoline) skeleton and position 10 of a naphthopyran (3H-naphtho[2,1-b]pyran) skeleton, said compound having photochromic properties and being a photochromic compound that has both a rapid colorizing/decolorizing reaction and high durability. Also provided is an industrially applicable photochromic compound that can be synthesized at a low cost.
Abstract: The present invention relates to Fms-like tyrosine kinase (FLT3) inhibitors. The present invention provides novel 4-quinolinone derivatives used as FLT3 inhibitors and for treatment and/or prevention of tumors.
Abstract: The present invention relates to tricyclic heterocycles of Formula (I): which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
Type:
Application
Filed:
September 27, 2019
Publication date:
April 30, 2020
Inventors:
Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, JR., James D. Rodgers
Abstract: The present invention relates to a novel rapamycin analogue (e.g., of Formula I or Formula II), mixtures, methods for its production, and its use in cancer therapy (e.g., prevention and/or treatment).
Type:
Application
Filed:
February 9, 2018
Publication date:
April 30, 2020
Applicant:
Mount Tam Therapeutics, Inc.
Inventors:
Timothy S. Powers, Bryan F. Cox, Richard B. Marshak
Abstract: The present invention relates to a crystal of cephalosporin intermediate 7?-methoxy cephalothin (I) and a method for preparing same. The crystal of 7?-methoxy cephalothin (I) undergoes Cu-Ka radiation and X-ray powder diffraction expressed in terms of angle 2?; the crystal of 7?-methoxy cephalothin (I) has characteristic absorption peaks at positions of 7.34°±0.20°, 12.71°±0.20°, 14.25°±0.20°, 14.68°±0.20°, 16.52°±0.20°, 17.99°±0.20°, 19.98°±0.20°, and 22.69°±0.20°. The crystal of 7?-methoxy cephalothin provided by the present invention is easy to prepare. Related test data shows that the crystal of 7?-methoxy cephalothin has high purity, low impurity content, and good stability. The preparation cost is low, the preparation method is simple to operate, conditions are mild and easy to control, and crystals of 7?-methoxy cephalothin can be obtained stably. The invention is applicable to industrial production.
Abstract: The present invention relates to substituted pyrimidinium compounds of formula (I), to the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these substituted pyrimidinium compounds and of compositions thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such substituted pyrimidinium compounds. The substituted pyrimidinium compounds of the present invention are defined by the following general formula (I) wherein X, Y, Z, R1, R2, A and R3 are defined as in the description.
Type:
Application
Filed:
June 18, 2018
Publication date:
April 30, 2020
Inventors:
Joachim Dickhaut, Ashokkumar Adisechan, Gopal Krishna Datta, Olesya Kuzmina
Abstract: Provided is a pharmaceutical composition for preventing and treating tumors, the pharmaceutical composition including an imidazooxazole derivative compound, a solvate, a stereoisomer, or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition is administered to an entity which has developed a tumor or is in danger of developing a tumor, and thus tumors can be prevented or treated.
Type:
Application
Filed:
December 31, 2019
Publication date:
April 30, 2020
Applicant:
KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
Inventors:
Gamal El-din MAHMOUD, Hong Seok CHOI, Kyung Ho YOO, Dong Keun HAN, Chang Hyun OH, Abdel-Maksoud MOHAMMED, I. El-Gamal MOHAMMED, Usama M. AMMAR
Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
Type:
Application
Filed:
January 10, 2020
Publication date:
April 30, 2020
Inventors:
Leon M. Smith, II, Vladimir Ladziata, Indawati De Lucca, Donald J.P. Pinto, Michael J. Orwat, Andrew K. Dilger, Kumar Balashnmuga Pabbisetty, Wu Yang, Scott A. Shaw, Peter W. Glunz, Manoranjan Panda
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
Type:
Application
Filed:
October 15, 2019
Publication date:
April 30, 2020
Inventors:
Craig E. Masse, Jeremy Robert Greenwood, Sayan Mondal
Abstract: An organic compound, an organic photoelectric device, an image sensor, and an electronic device, the organic compound being represented by Chemical Formula 1: wherein, in Chemical Formula 1, R1, R2, R3, R4, R5, and R6 are each independently a hydrogen atom, a substituted or unsubstituted C1-C4 alkyl group, a substituted or unsubstituted C1-C4 alkoxy group, or a substituted or unsubstituted C1-C4 alkylthio group, and A is a functional group including a heteroaryl group that includes at least one sulfur atom.
Abstract: The present invention relates to boronic acid and boronate ester compounds that are inhibitors of aldose reductase, and to compositions that contain the compounds and methods of using the compounds.
Abstract: A silicon-containing electron transporting material and its application are disclosed. The silicon-containing electron transporting material employs a silicon-containing compound with a novel structure containing one or more silicon atoms and a specific group. The compound can be used as an electron transporting layer of an electroluminescent device, which can effectively improve the lifetime of the device and improve device performance. An electroluminescent device and compound formulation are also disclosed.
Type:
Application
Filed:
October 24, 2019
Publication date:
April 30, 2020
Inventors:
Xiao Chen, Chuanjun Xia, Chi Yuen Raymond Kwong
Abstract: Provided are a novel disilylamine compound, a method for preparing same, and a composition for depositing a silicon-containing thin film including the same. A disilylamine compound of the present invention has excellent reactivity, is thermally stable, and has high volatility, and thus, is used as a silicon-containing precursor, thereby manufacturing a high-quality silicon-containing thin film.
Type:
Application
Filed:
April 19, 2018
Publication date:
April 30, 2020
Inventors:
Sung Gi KIM, Se Jin JANG, Byeong-il YANG, Joong Jin PARK, Sang-Do LEE, Jeong Joo PARK, Sam Dong LEE, Gun-Joo PARK, Sang Ick LEE, Myong Woon KIM
Abstract: The present invention provides a phosphorus-containing compound characterized by being a compound represented by the following structure: the compound is a novel immune cell migration inhibitor. The compound has good hydrophilicity and can be developed into eye drops. The compound has a strong inhibitory ability to immune cell migration and can relieve the symptoms of most dry-eye patients.
Type:
Application
Filed:
May 21, 2018
Publication date:
April 30, 2020
Applicant:
VivaVisionShanghaiLtd
Inventors:
Wang SHEN, Yue DING, Hao JIANG, Fu li CHEN, Jiangfeng WANG, Xinglong WU, Cunfei LI, Liguo YANG, Biao HU, Qiyang JIANG, Zhixing AN, Kuifeng DANG
Abstract: A novel compound has pharmacological activities comparable to those of Nahlsgen and is storable excellently stably. The compound can be produced by a method according to the present invention for producing an optically active 2-amino-phosphonoalkanoic acid salt. In the method, a starting material DL-2-amino-phosphonoalkanoic acid represented by Formula (1) or a hydrate thereof is reacted with an optically active basic compound other than an optically active lysine, to give a diastereomeric salt mixture including a first salt (including a hydrate salt) between a D-2-amino-phosphonoalkanoic acid represented by Formula (1-1) and the optically active basic compound, and a second salt (including a hydrate salt) between an L-2-amino-phosphonoalkanoic acid represented by Formula (1-2) and the optically active basic compound. The diastereomeric salt mixture is fractionally crystallized to isolate one of the first and second diastereomeric salts.
Type:
Application
Filed:
April 13, 2018
Publication date:
April 30, 2020
Applicants:
NAHLS CORPORATION CO., LTD., KYOTO UNIVERSITY
Abstract: This invention relates to compounds that are useful as cancer therapies. The compounds comprise derivatives of tetracycline antibiotics, e.g. doxycycline, having a phosphonium cation tethered to the tetracycline tetracycle. The invention also relates to methods of using said compounds and to pharmaceutical formulations comprising said compounds.
Type:
Application
Filed:
April 20, 2018
Publication date:
April 30, 2020
Inventors:
Tim Sparey, Andrew Ratcliffe, David Hallett, Edward Cochrane, Gilbert Lassalle, Alexandre Froidbise, Brett Stevenson
Abstract: The present invention provides compounds of Formula I?: wherein , W, X, Y, Z, Z1, Z2, R1, R2, R3, R4 and R5 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the STING protein and thus can be used as medicaments for treating or preventing disorders affected by the agonism of STING.
Type:
Application
Filed:
October 24, 2019
Publication date:
April 30, 2020
Inventors:
David J. Diller, Axel Metzger, David E. Kaelin, JR., Steven Paget, Chia-Yu Huang, Brian F. Mcguinness, Audrey Julie Hospital, William Ronald Solvibile, JR.
Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein one of R1, R2 or R3 is —P(?O)(OH)2, and the other two of R1, R2 and R3 are each H, are provided. Pharmaceutical compositions comprising the compounds, and methods for use of the compounds for treating diseases associated with overexpression of a cyclin-dependent kinase (CDK) are also provided.
Abstract: The present invention relates to certain acid salts of (((1-(6-amino-9H-purin-9-yl)propan-2-yloxy)methyl)(phenoxy) phosphoryloxy)methyl pivalate of Formula (I), to processes for their preparation; to pharmaceutical compositions comprising such compounds, and methods of treating a disease which responds to inhibition of nucleotide reverse transcriptase activity.
Abstract: Provided are a compound for treating metabolic diseases having the structure as shown in formula (I) or formula (II), or a racemate, stereoisomer, geometric isomer, tautomer, solvate, hydrate, metabolite, pharmaceutically acceptable salt or prodrug thereof. The compound is an activator of FXR and/or a TGR5 receptor, and thus has the activity of activating FXR and/or a TGR5 receptor, and can be used in the preparation of drugs for treating chronic liver diseases, metabolic diseases or portal hypertension.
Type:
Application
Filed:
August 15, 2018
Publication date:
April 30, 2020
Inventors:
Guoqin Fu, Wei Ding, Bo Yin, Chao Yang, Cuiqin Wang, Yong Dou, Ruiling Wang
Abstract: We report the design of a catalytic, bifunctional template that binds heterocyclic substrate via reversible coordination instead of covalent linkage, allowing remote site-selective C—H olefination of heterocycles. The two metal centers coordinated to this template play different roles; anchoring substrates to the proximity of catalyst and cleaving the remote C—H bonds respectively. Using this strategy, we demonstrate remote site-selective C—H olefination of heterocyclic substrates which do not have functional group handles for covalently attaching templates. For instance the olefination can be an alkenylation of a 3-phenylpyridine with an acrylate alkyl ester selective for the meta position of the phenyl group with respect to the pyridine, or can be an alkenylation of a quinoline with an acrylate alkyl ester selective for the 5-position of the quinoline.
Abstract: The present invention relates to nanoparticles including a crystal structure-controlled zeolitic imidazolate framework (ZIF) and a method of producing the same. Nanoparticles according to the present invention comprise: metal ions; and an organic ligand coupled to the metal ions, wherein the organic ligand includes an imidazolate-based organic ligand and an alkylamine-based organic ligand.
Type:
Application
Filed:
October 22, 2019
Publication date:
April 30, 2020
Inventors:
Jong Suk Lee, Kie Yong Cho, Jin Won Lee, Byung Keun Oh, Jeong Geol Na, He Seong An, Ju Ho Shin
Abstract: The present invention relates to a crystalline form of a co-crystal of an inhibitor against sodium-glucose cotransporter 2 with L-proline, a method for preparing the same, a pharmaceutical composition comprising the same, and use thereof. Specifically, the present invention relates to a crystalline form of a co-crystal of an inhibitor against sodium-glucose cotransporter 2 represented by formula (1), i.e., (2S,3R,4R,5S,6R)-2-(3-(4-(((1R,3s,5S)-bicyclo[3.1.0]hexan-3-yl)oxy)benzyl)-4-chlorophenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol, with L-proline, a method for preparing the same, a pharmaceutical composition comprising the same, and use thereof.