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    • 46. 发明申请
    • CYCLIC PEPTIDE COMPOUND OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF AND METHOD FOR PRODUCING SAME
    • 循环肽化合物或其药学上可接受的盐及其生产方法
    • US20130109833A1
    • 2013-05-02
    • US13808772
    • 2011-07-06
    • Yohei HiraiYoji Okugawa
    • Yohei HiraiYoji Okugawa
    • C07K7/64
    • C07K7/64A61K38/00C07K7/06C07K7/56
    • Provided are a cyclic peptide compound or a pharmacologically acceptable salt thereof capable of inhibiting parakeratosis of skin, and a method for producing the same. This method comprises subjecting a cyclic peptide compound of Formula (I): or a pharmacologically acceptable salt thereof, wherein Xaa1 and Xaa5 are each optionally substituted Ser, optionally substituted Thr, or optionally substituted Tyr; Xaa2 is optionally substituted Ile, optionally substituted Val, or optionally substituted Leu; Xaa3 and Xaa4 are each optionally substituted Asn, optionally substituted Gln, optionally substituted Asp, or optionally substituted Glu; and R1 is a group of Formula (II): —CO—(CH2)n—NH—  (II), or Formula (III): —NH—(CH2)n—CO—  (III), wherein n is the same as defined above, and in Formula (I), the linkage between Cys and Cys is a peptide bond or a disulfide bond, and the other linkages are peptide bonds, to cyclization with a compound of Formula (IV): Cys-R1-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Cys  (IV), wherein, Xaa1, Xaa2, Xaa3, Xaa4, Xaa5, and R1 are the same as defined above.
    • 提供能够抑制皮肤角化不全的环状肽化合物或其药学上可接受的盐及其制造方法。 该方法包括使式(I)的环状肽化合物或其药理学上可接受的盐,其中Xaa1和Xaa5各自任选被取代为Ser,任选取代的Thr或任选取代的Tyr; Xaa2是任选取代的Ile,任选取代的Val或任选取代的Leu; Xaa3和Xaa4各自为任选取代的Asn,任选取代的Gln,任选取代的Asp或任选取代的Glu; 并且R 1是式(II)的基团:-CO-(CH 2)n -NH-(II)或式(III):-NH-(CH 2)n -CO-(III),其中n相同 和式(I)中,Cys和Cys之间的连接是肽键或二硫键,其它键是肽键,以与式(IV)化合物环化:Cys-R1-Xaa1 -Xaa2-Xaa3-Xaa4-Xaa5-Cys(IV),其中,Xaa1,Xaa2,Xaa3,Xaa4,Xaa5和R1与上述定义相同。