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NPRA AGONISTS, COMPOSITIONS, AND USES THEREOF

机译:NPRA激动剂,组合物及其用途

摘要

This disclosure provides a natriuretic peptide derivative of Formula (I), and to compositions including a natriuretic peptide derivative of Formula (I),; (fatty acyl)z-(B)x-(G)y-NP   (I),;wherein: z is 1, x is an integer from 2 to 4 and y is 3; or z is 0, x is an integer from 0 to 4 and y is an integer from 1 to 3; fatty acyl comprises from 12 to 24 (e.g., 12 to 18) carbons atoms; B is lysine or arginine; G is glycine; NP is a natriuretic peptide; if present, (fatty acyl)z- is covalently linked to the N-terminus of (B)x; (fatty acyl)z-(B)x- is covalently linked to the N-terminus of (G)y; and (fatty acyl)z-(B)x-(G)y- is covalently linked to the N-terminus of NP. The natriuretic peptide derivative according to the disclosure, and compositions thereof, are useful in the treatment of diseases such as hypertension, vascular congestion, and heart disease.
机译:本公开提供了式(I)的利钠肽衍生物,以及包含式(I)的利钠肽衍生物的组合物, <?in-line-formulae description =“ In-line Formulae” end =“ lead”?>(脂肪酰基) z -(B) x -(G) y -NP(I),<?in-line-formulae description =“在线表达式” end =“ tail”?>;其中:z为1,x为2到1之间的整数4,y为3;或z为0,x为0至4的整数,y为1至3的整数;脂肪酰基包含12至24个(例如12至18个)碳原子; B是赖氨酸或精氨酸; G是甘氨酸; NP是利钠肽; (脂肪酰基) z -(如果存在的话)共价连接到(B) x 的N端; (脂肪酰基) z -(B) x -共价连接至(G) y 的N端; (脂肪酰基) z -(B) x -(G) y -共价连接到NP的N端。根据本发明的利钠肽衍生物及其组合物可用于治疗疾病,例如高血压,血管充血和心脏病。

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