50712-64-6Relevant articles and documents
Immunomodulator
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, (2021/02/10)
The invention provides an immunomodulator, and belongs to the field of medical chemistry. The immunomodulator is a compound represented by formula I, or a stereoisomer, or a salt, or a solvate, or a prodrug, or a metabolite thereof. The compound disclosed by the invention shows good IL-17A inhibitory activity, can be used for preparing an IL-17A inhibitor, is used for treating diseases with abnormal IL-17A activity, and the invention provides a new medicinal possibility for clinically treating diseases related to abnormal IL-17A activity.
Immunomodulator
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, (2021/05/22)
The invention discloses an immunomodulator, and particularly relates to a compound for inhibiting IL-17A and application of the compound serving as the immunomodulator in preparation of drugs. The invention discloses application of a compound shown in a formula I or a stereoisomer thereof in preparation of medicines for inhibiting IL-17A, and provides a new choice for clinically screening and/or preparing medicines for treating diseases related to IL-17A activity.
Immunomodulator
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Paragraph 0276; 0277; 0278-0280, (2021/02/10)
The invention discloses an immunomodulator, and particularly relates to a compound shown as a formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. Experiments prove that the compound has good IL-17A inhibitory activity, can be used for preparing an IL-17A inhibitor and drugs for preventing and/or treating IL-17A mediated diseases (such as inflammation, autoimmune diseases, infectious diseases, cancers and precancerous syndromes), and provides a new medical possibility for clinical treatment of diseases related to abnormal IL-17A activity.
Immunomodulator
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Paragraph 0241-0245; 0294-0298, (2021/02/10)
The invention discloses an immunomodulator, and particularly relates to a compound shown as a formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. Experiments prove that the compound has good IL-17A inhibitory activity, can be used for preparing an IL-17A inhibitor and drugs for preventing and/or treating IL-17A mediated diseases (such as inflammation, autoimmune diseases, infectious diseases, cancers and precancerous syndromes), and provides a new medical possibility for clinical treatment of diseases related to abnormal IL-17A activity.
Discovery of 2-(3,5-difluoro-4-methylsulfonaminophenyl)propanamides as potent TRPV1 antagonists
Kim, Changhoon,Ann, Jihyae,Lee, Sunho,Sun, Wei,Blumberg, Peter M.,Frank-Foltyn, Robert,Bahrenberg, Gregor,Stockhausen, Hannelore,Christoph, Thomas,Lee, Jeewoo
, p. 2539 - 2542 (2018/06/07)
A series of A-region analogues of 2-(3-fluoro-4-methylsufonamidophenyl) propanamide 1 were investigated as TRPV1 antagonists. The analysis of structure-activity relationship indicated that a fluoro group at the 3- (or/and) 5-position and a methylsulfonamido group at the 4-position were optimal for antagonism of TRPV1 activation by capsaicin. The most potent antagonist 6 not only exhibited potent antagonism of activation of hTRPV1 by capsaicin, low pH and elevated temperature but also displayed highly potent antagonism of activation of rTRPV1 by capsaicin. Further studies demonstrated that antagonist 6 blocked the hypothermic effect of capsaicin in vivo, consistent with its in vitro mechanism, and it showed promising analgesic activity in the formalin animal model.
Application of the mild-condition phthalimidine synthesis with use of 1,2,3-1h-benzotriazole and 2-mercaptoethanol as dual synthetic auxiliaries. Effective synthesis of phthalimidines possessing a variety of substituents at 2-position
Takahashi, Ichiro,Kawakami, Teruki,Hirano, Etsushi,Kimino, Mako,Kamimura, Shigeki,Miwa, Takayuki,Tamura, Takanori,Tazaki, Ryo,Kitajima, Hidehiko,Hatanaka, Minoru,Isa, Kimio,Hosoi, Shinzo
, p. 557 - 571 (2017/04/10)
The mild-condition phthalimidine synthesis based on Mannich type 1:1 condensation reaction between o-phthalaldehyde with a variety of primary amines in the presence of excess 2-mercaptoethanol and 1,2,3-1H-benzotriazole as "dual synthetic auxiliaries" in MeCN for 13 h at room temperature afford 2-substituted phthalimidines (2,3-dihydroisoindol-1-one) in fair to good isolated yields.
TYK2 INHIBITORS AND USES THEREOF
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Paragraph 0625; 0626; 0627, (2016/09/26)
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.
TYK2 INHIBITORS AND USES THEREOF
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Paragraph 00856; 00857, (2015/09/28)
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.
QUINAZOLINE DERIVATIVES
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Page/Page column 52-53, (2012/09/25)
Novel quinazolinamide derivatives of the formula (I), in which R1-R4 and X have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
Vanilloid Receptor Ligands, Pharmaceutical Compositions Containing Them, Process for Making Them, and Use Thereof for Treating Pain and Other Conditions
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Page/Page column 62; 64; 65-66, (2009/07/03)
Vanilloid receptor ligand compounds corresponding to formula I: pharmaceutical compositions containing such compounds, a process for producing such compounds, and methods of using such compounds for treating or inhibiting pain and various other disorders or conditions.