72791-76-5Relevant academic research and scientific papers
Design and Scalable Synthesis of N-Alkylhydroxylamine Reagents for the Direct Iron-Catalyzed Installation of Medicinally Relevant Amines**
Delcaillau, Tristan,Falk, Eric,Gürtler, Laura,Makai, Szabolcs,Morandi, Bill
supporting information, p. 21064 - 21071 (2020/09/21)
Secondary and tertiary alkylamines are privileged substance classes that are often found in pharmaceuticals and other biologically active small molecules. Herein, we report their direct synthesis from alkenes through an aminative difunctionalization reaction enabled by iron catalysis. A family of ten novel hydroxylamine-derived aminating reagents were designed for the installation of several medicinally relevant amine groups, such as methylamine, morpholine and piperazine, through the aminochlorination of alkenes. The method has excellent functional group tolerance and a broad scope of alkenes was converted to the corresponding products, including several drug-like molecules. Besides aminochlorination, the installation of other functionalities through aminoazidation, aminohydroxylation and even intramolecular carboamination reactions, was demonstrated, further highlighting the broad potential of these new reagents for the discovery of novel amination reactions.
Heterocyclic Compound
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Paragraph 1903; 1904, (2018/06/15)
The present invention provide a compound having an orexin receptor antagonistic activity, which is expected to be useful as medicaments such as agents for the prophylaxis or treatment of sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
Oxadiazole Amine Derivative Compounds as Histone Deacetylase 6 Inhibitor, and the Pharmaceutical Composition Comprising the same
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Paragraph 0693-0696, (2017/07/18)
The present invention relates to a novel compound having an activity of inhibiting histone deacetylase 6 (HDAC6), an optical isomer thereof or a pharmaceutically acceptable salt thereof, a use thereof for preparation of a drug for treatment, a pharmaceutical composition comprising the same, a treatment method using the composition, and a method for preparing the same. The novel compound, an optical isomer thereof or a pharmaceutically acceptable salt thereof according to the present invention has an activity of inhibiting histone deacetylase 6 (HDAC6), and is effective for preventing or treating HDAC6-related diseases, including infectious diseases; neoplasm; endocrine, nutritional and metabolic diseases; mental and behavior disorders; nerve disorders; eye and adnexa diseases; cardiovascular diseases; respiratory diseases; digestive organ diseases; skin and subcutaneous tissue diseases; musculoskeletal and connective tissue diseases; or congenital malformation, deformation and chromosomal abnormality.COPYRIGHT KIPO 2017
INDUCTION OF GATA2 BY HDAC1 AND HDAC2 INHIBITORS
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Page/Page column 63, (2016/05/02)
Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with Gata2 deficiency, particularly diseases or disorders that involve any type of HDAC1 and/or HDAC2 expression. Such diseases include acute myeloid leukemia (AML); familial myelodysplastic syndrome (MDS); leukemia; sickle-cell anemia; beta-thalassemia; monocytopenia and mycobacterial infections; dendritic cell, nonocyte, B, and natural killer lymphoid deficiency; Emberger syndrome; asymptomatic neurocognitive impairment; mild neurocognitive disorder; and HIV- associated dementia.
PYRIMIDINE HYDROXY AMIDE COMPOUNDS AS HISTONE DEACETYLASE INHIBITORS
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Paragraph 0174; 0175, (2015/04/21)
Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1, HDAC2, and/or HDAC6. Also provided herein are methods for inhibiting migration of a neuroblastoma cell, inducing maturation of a neuroblastoma cell, and altering cell cycle progression of a neuroblastoma cell comprising administering to the cell a therapeutically effective amount of a HDAC1, HDAC2, and/or HDAC6 selective inhibitor or a pharmaceutically acceptable salt thereof.
NOVEL BENZENESULFONAMIDE COMPOUNDS, METHOD FOR SYNTHESIZING SAME, AND USE THEREOF IN MEDICINE AS WELL AS IN COSMETICS
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Paragraph 0251, (2014/09/30)
Provided herein are novel benzenesulfonamide compounds having a structure of formula (I) below: as well as to the method for synthesizing same and to the use thereof in pharmaceutical compositions to be used in human or veterinary medicine, as well as to
NOVEL BENZENESULFONAMIDE COMPOUNDS, METHOD FOR SYNTHESIZING SAME, AND USE THEREOF IN MEDICINE AS WELL AS IN COSMETICS
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Page/Page column 17, (2013/02/27)
Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
OXAZOLIDINONE DERIVATIVE HAVING 7-MEMBERED HETERO RING
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Page/Page column 55-57, (2010/08/07)
The present invention provides a novel oxazolidinone derivative of the formula (I): wherein Ring A is (A-1) a 7-membered monocyclic heterocycle containing three N atoms; (A-2) a 7-membered monocyclic heterocycle containing two N atoms and one O atom; or (A-3) a 7-membered monocyclic heterocycle containing two N atoms and one S atom, SO or SO2, wherein said monocyclic heterocycle is optionally substituted, optionally unsaturated and optionally fused with another ring; X1 is a single bond, or a heteroatom-containing group selected from the group consisting of -O-, -S-, -NR2-, -CO-, -CS-, -CONR3-, -NR4CO-, -SO2NR5-, and -NR6SO2-, wherein R2, R3, R4, R5 and R6 are independently hydrogen or lower alkyl, or lower alkylene or lower alkenylene each optionally interrupted by said heteroatom-containing group; Ring B is optionally substituted carbocycle or optionally substituted heterocycle; and R1 is hydrogen, or an organic residue which is able to bind to the 5-position of the oxazolidinone ring in oxazolidinone antimicrobial agents, pharmaceutically acceptable salts and solvates thereof which are useful as an antibacterial agent.
Synthesis and biological evaluation of triazepane derivatives as DPP-IV inhibitors
Park, Woul Seong,Jun, Mi Ae,Shin, Mi Sik,Kwon, Sung Wook,Kang, Seung Kyu,Kim, Ki Young,Dal Rhee, Sang,Bae, Myung Ae,Narsaiah, Banda,Lee, Duck Hyung,Cheon, Hyae Gyeong,Ahn, Jin Hee,Kim, Sung Soo
experimental part, p. 1001 - 1010 (2010/04/24)
A series of triazepane derivatives such as (R)-3-amino-1-(1,2,5-triazepan-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-ones (7, 13a-p) and (R)-3-amino-1-(1,2,5-triazepan-5-yl)-4-(2,4,5-trifluorophenyl)butan-1-ones (17a-e) was synthesized and evaluated for their
Syntheses of new spirocarbocyclic nucleoside analogs using iminonitroso diels-alder reactions
Lin, Weimin,Gupta, Anuradha,Kim, Kyung Hee,Mendel, David,Miller, Marvin J.
supporting information; experimental part, p. 449 - 452 (2009/07/11)
(Chemical Equation Presented) N-Cbz- and Boc-protected spirocyclic dienes were prepared by dialkylation of cyclopentadiene. These dienes coupled efficiently in a series of iminonitroso Diels-Alder reactions to produce a series of new spirocyclic adducts.
