60638-81-5Relevant academic research and scientific papers
Discovery of Chromane-6-Sulfonamide Derivative as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist
Chen, Lei,Su, Mei,Jin, Qiu,Wang, Wei,Wang, Chun-Gu,Assani, Israa,Wang, Mu-Xuan,Zhao, Shi-Feng,Lv, Shen-Min,Wang, Jia-Wei,Sun, Bo,Li, Yan,Liao, Zhi-Xin
, p. 16106 - 16131 (2021/11/18)
Interleukin-17 (IL-17) is a proinflammatory cytokine that plays a dominant role in inflammation, autoimmunity, and host defense. RORγt is a key transcription factor mediating T helper 17 (Th17) cell differentiation and IL-17 production, which is able to activate CD8+ T cells and elicit antitumor efficacy. A series of sulfonamide derivatives as novel RORγt inverse agonists were designed and synthesized. Using GSK2981278 (phase II) as a starting point, we engineered structural modifications that significantly improved the activity and pharmacokinetic profile. In animal studies, oral administration of compound d3 showed a robust and dose-dependent inhibition of the IL-17A cytokine expression in a mouse imiquimod-induced skin inflammation model. Docking analysis of the binding mode revealed that the compound d3 occupied the active pocket suitably. Thus, compound d3 was selected as a clinical compound for the treatment of Th17-driven autoimmune diseases.
SULFONYL-SUBSTITUTED BICYCLIC COMPOUND WHICH ACTS AS ROR INHIBITOR
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Paragraph 0195; 0199; 0205; 0209, (2020/08/16)
Provided is a sulfonyl-substituted bicyclic compound (A) which acts as a RORγ inhibitor, said compound has good RORγ inhibitory activity and is expected to be used for treating diseases mediated by a RORγ receptor in mammals.
SULPHAMOYLARYL DERIVATIVES AND USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF LIVER FIBROSIS
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, (2018/09/08)
Potent 5-HT2B antagonist of Formula (A), including stereochemically isomeric forms, and salts, hydrates, solvates thereof and their use wherein R1 to R4 and Ar have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them, alone or in combination with other drugs, in fibrosis and/or cirrhosis prevention or therapy.
INHIBITORS OF N-LINKED GLYCOSYLATION AND METHODS USING SAME
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Page/Page column 62, (2017/02/24)
The present invention includes novel compounds and methods for preventing or treating diseases associated with N-linked glycosylation in a subject in need thereof. The methods comprise administering to the subject an effective amount of at least one compo
Method for preparing 2-ethyoxyl-5-(4-methyl piperazine-1-sulfonyl) benzoic acid from methyl salicylate
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Paragraph 0017;, (2016/11/14)
The invention relates to a method for preparing 2-ethyoxyl-5-(methyl piperazine-1-sulfonyl) benzoic acid from methyl salicylate. The method comprises the following steps: taking the methyl salicylate as a raw material, sulfonating with chlorosulfonic acid
CLASS II HMG-COA REDUCTASE INHIBITORS AND METHODS OF USE
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Paragraph 0048, (2014/01/08)
Disclosed are compositions and methods for treating bacterial infections.
NOVEL COMPOUNDS
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Page/Page column 66, (2011/04/25)
The present invention discloses novel compounds inhibiting LRRK2 kinase activity, the preparation processes thereof, the compositions containing them, as well as the use in treating diseases characterized by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.
Pyrrolopyrimidinone derivatives, process for preparation thereof, and method of using and composition comprising them
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Page/Page column 6, (2008/06/13)
The invention relates to a series of pyrrolopyrimidinone derivatives, processes for their preparation, intermediates in their preparation, their use as therapeutic agents, and pharmaceutical compositions containing them.
Aminoalcohol derivatives
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Page/Page column 21, (2010/02/07)
The present invention relates to a compound formula [I]: wherein R1 is hydrogen or halogen, R2 is hydrogen or an amino protective group, R3 is hydrogen or lower alkyl, X is bond, —CH2— or —O—, and Y is ?in which R4 is lower alkoxycarbonyl, ?in which R5 is carboxy(lower)alkyl, etc., ?in which R6 is hydroxy, etc., and so on, or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.
AMINOALCOHOL DERIVATIVES AND THEIR USE AS BETA-3 ADRENERGIC RECEPTOR AGONISTS
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Page/Page column 65, (2010/02/07)
The present invention relates to a compound formula [I] or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.
