26088-66-4Relevant articles and documents
Tricyclic compound and application thereof
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Paragraph 0292; 0294-0295, (2021/07/17)
The invention discloses a tricyclic compound and application thereof. The invention specifically discloses a compound as shown in a formula I or pharmaceutically acceptable salt thereof. The tricyclic compound disclosed by the invention has a very good inhibition effect on HDAC (histone deacetylase), especially HDAC6, has relatively good selectivity and can be used for inhibiting proliferation of various tumor cells.
METHODS AND MATERIALS FOR INCREASING OR MAINTAINING NICOTINAMIDE MONONUCLEOTIDE ADENYLYL TRANSFERASE-2 (NMNAT2) POLYPEPTIDE LEVELS
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, (2020/09/08)
This document provides methods and materials for increasing or maintaining NMNAT2 polypeptide levels within cells. For example, compounds (e.g., organic compounds) having the ability to increase or maintain NMNAT2 polypeptide levels within cells, formulations containing compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for making compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for making formulations containing compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for increasing or maintain NMNAT2 polypeptide levels within cells, and methods for treating mammals (e.g., humans) having a condition responsive to an increase in NMNAT2 polypeptide levels are provided (or for preventing said condition).
2,3,4,9- TETRAHYDRO-1H-CARBAZOLE DERIVATIVES AS CRTH2 RECEPTOR ANTAGONISTS
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Page/Page column 16, (2009/10/31)
The invention relates to novel tetrahydro-1H-carbazole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to patients.
2,3,4,9-TETRAHYDRO-1H-CARBAZOLE DERIVATIVES AS CRTH2 RECEPTOR ANTAGONISTS
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Page/Page column 44, (2008/06/13)
The invention relates to novel tetrahydro-lH-carbazole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to patients.
CYCLOALKYLFUSED INDOLE, BENZOTHIOPHENE, BENZOFURAN AND INDENE DERIVATIVES
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Page/Page column 71, (2008/06/13)
The present invention provides cycloalkylfused indole, benzothiophene, benzofuran, and indene derivatives, and methods for using them to, for example, treat, prevent and/or ameliorate central nervous system diseases by antagonizing 5-HT1A receptors and mo
A Novel Synthesis Towards Ellipticine and Its Derivatives. Synthesis of a New Precursor Compound
Erguen,Patir,Okay
, p. 435 - 442 (2007/10/03)
The synthesis of a new precursor comppund 3, which may be important for the synthesis of ellipticine and its derivatives, was described. Many new intermediates 5-10 have also been synthesized.
Tetrahydrocarbazol derivatives as ligands for G-protein-coupled receptors (GPCR)
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Page 14, (2010/11/30)
This invention provides new tetrahydrocarbazole derivatives that act as ligands for G-protein-coupled receptors (GPCR), especially as antagonists of the gonadotropin-releasing hormone (GnRH). A pharmaceutical composition that contains these new tetrahydro
Heterocyclic compounds, their preparation and their therapeutic use
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, (2008/06/13)
A compound of formula (I): STR1 wherein Y1, Y2, Y3 and Y4 are each hydrogen, halogen, nitro, cyano, hydroxyl, thiol, amino, alkyl, haloalkyl, alkylthio, a protected or unprotected carboxyl, a protected or unprotected sulfonamide, or tetrazol; one of R1 and R2 is hydrogen, alkyl, aryl, aralkyl, oxazolyl, or a protected or unprotected carboxyl and the other of R1 and R2 is hydrogen, alkyl, aryl or aralkyl; and R3 is hydrogen or an amino protecting group, and pharmaceutically acceptable salts or esters thereof. The compounds are effective for treating dementia, Alzheimer's disease and delirium and are effective as sedatives.
Conformer interconversion in the excited state of constrained tryptophan derivatives
McMahon, Lloyd P.,Yu, Hong-Tao,Vela, Marco A.,Morales, Guillermo A.,Shui, Li,Fronczek, Frank R.,McLaughlin, Mark L.,Berkley, Mary D.
, p. 3269 - 3280 (2007/10/03)
The conformer model of tryptophan photophysics ascribes the multiple fluorescence lifetimes to ground-state heterogeneity. It is usually assumed that the different conformers do not interconvert in the excited state. Previous studies of two constrained tryptophan derivatives supported this assumption (Colucci, W. J.; Tilstra, L.; Sattler, M. C.; Fronczek, F. R.; Barkley, M. D. J. Am. Chem. Soc. 1990, 112, 9182-9190; Yu, H.-T.; Vela, M. A.; Fronczek, F. R.; McLaughlin, M. L.; Barkley, M. D. J. Am. Chem. Soc. 1995, 117, 348-357). Five constrained derivatives have been synthesized and shown to undergo conformer inversion during the lifetime of the excited state. All derivatives have two ground-state conformations as determined by X-ray crystallography, molecular mechanics calculations, and 1H-NMR. Fluorescence lifetime data were fit to single-and double-exponential models and to a reversible two-state excited-state reaction model. 2-Ammo-1,2-dihydrocyclopenta[b]indole-2-carboxylic acid has a single-exponential decay consistent with conformer inversion much faster than fluorescence decay. 1,2,3,4-Tetrahydrocarbazole-3-carboxylic acid, ethyl 1,2,3,4-tetrahydrocarbazole-3-carboxylate, and their 9-methyl derivatives have double-exponential decays with a minor second component of small positive or negative amplitude. Conformer inversion rates of ～107 s-1 were determined by analyzing the fluorescence decay data using the excited-state reaction model. Temperature dependence of the fluorescence lifetimes was measured in H2O and D2O, and solvent quenching rates were calculated from the Arrhenius parameters. The carboxylate and carbonyl functional groups appear to have little effect on solvent quenching of indole fluorescence. Model calculations examining the effect of conformer inversion rate on the decay parameters of a biexponential model indicate that the presence of a small amplitude, short lifetime component may be a good predictor of excited-state conformer interconversion of tryptophans in peptides and proteins.
