CAS: 1970972-74-7; (R)-4-(1-((3-(Difluoromethyl)-1-Methyl-1H-Pyrazol-4-yl)Sulfonyl)-1-Fluoroethyl)-N-(Isoxazol-3-yl)Piperidine-1-Carboxamide

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    专利号:US-2022289709-A1
    优先权日:2019-07-16
    标题:Polymorphic forms of (r)-4-(1-((3-(difluoromethyl)-1-methyl-1h-pyrazol-4-yl)sulfonyl)-1-fluoroethyl)-n-(isoxazol-3-yl)piperidine-1-carboxamide
    发明人:ZHONG MIN; MONNIER OLIVIER; JELIN JEAN-PHILIPPE; DUVOUX RICHARD; ALIE JEAN; OCHSENBEIN PHILIPPE
    权利人:MYOKARDIA INC
    摘要:The present invention provides novel polymorphs of (R)-4-(1-((3-(difluoromethyl)-1-methyl-1H-pyrazol-4-yl)sulfonyl)-1-fluoroethyl)-N-(isoxazol-3-yl)piperidine-1-carboxamide (I-491) that are useful for the treatment of cardiac disorders including systolic dysfunction, dilated cardiomyopathy (DCM), heart failure with reserved ejection fraction (HFrEF), and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the polymorphs is described, as well as methods for treating systolic dysfunction, DCM, HFrEF, and other forms of heart disease.

    专利号:US-9925177-B2
    优先权日:2015-01-22
    标题:4-methylsulfonyl-substituted piperidine urea compounds
    发明人:OSLOB JOHAN; AUBELE DANIELLE; KIM JAE; MCDOWELL ROBERT; SONG YONGHONG; SRAN ARVINDER; ZHONG MIN
    权利人:MYOKARDIA INC
    摘要:The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.

    专利号:US-11123337-B2
    优先权日:2015-01-22
    标题 :4-methylsulfonyl-substituted piperidine urea compounds
    发明人:OSLOB JOHAN; AUBELE DANIELLE; KIM JAE; MCDOWELL ROBERT; SONG YONGHONG; SRAN ARVINDER; ZHONG MIN
    权利人:MYOKARDIA INC
    摘要:The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.

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    主要参考文献


    1: Landim-Vieira M, Knollmann BC. Danicamtiv Recruits Myosin Motors to Aid the Failing Heart. Circ Res. 2023 Aug 18;133(5):444-446. doi: 10.1161/CIRCRESAHA.123.323366. Epub 2023 Aug 17. 19(6):353-363. doi: 10.1038/s41569-022-00682-0. Epub 2022 Mar 18.
    3: Kooiker KB, Mohran S, Turner KL, Ma W, Martinson A, Flint G, Qi L, Gao C, Zheng Y, McMillen TS, Mandrycky C, Mahoney-Schaefer M, Freeman JC, Costales Arenas EG, Tu AY, Irving TC, Geeves MA, Tanner BCW, Regnier M, Davis J, Moussavi-Harami F. Danicamtiv Increases Myosin Recruitment and Alters Cross- Bridge Cycling in Cardiac Muscle. Circ Res. 2023 Aug 18;133(5):430-443. doi: 10.1161/CIRCRESAHA.123.322629. Epub 2023 Jul 20.
    4: Kooiker KB, Mohran S, Turner KL, Ma W, Flint G, Qi L, Gao C, Zheng Y, McMillen TS, Mandrycky C, Martinson A, Mahoney-Schaefer M, Freeman JC, Costales Arenas EG, Tu AY, Irving TC, Geeves MA, Tanner BCW, Regnier M, Davis J, Moussavi-Harami F. Danicamtiv increases myosin recruitment and alters the chemomechanical cross bridge cycle in cardiac muscle. bioRxiv [Preprint]. 2023 Feb

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    参考文献:10.1007/s12181-025-00732-0
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