INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
发明人:
DMARCHI RICHARD D.
申请号：
ARP110102185
公开号：
AR081984A1
申请日:
2011.06.23
申请国别(地区):
AR
年份:
2012
代理人:
摘要：
It provides an element of dipeptide car non Enzymatic breakage can be linked to known medicinal agents through an amide Bond. The dipeptide breaks spontaneously from the medicinal Agent in physiological conditions through a reaction driven by chemical instability.Therefore, the element of dipeptide provides a Union of various compounds known to medicinal agents, where the compounds are released later from the medicinal Agent after a default exposure time to Physiological conditions.For example, the dipeptide can bind to the active site of a drug to form a prodrug and / or dipeptide can comprise a Polymer injection Depot to hijack a composition comprising the complex at the site of Administration.Claim 1, characterized in that it comprises: a prodrug Structure: A - B - Q where q is a bioactive Peptide (For example, a Peptide of insulin), where a - B includes the structure of formula (1) wherein R1 and R2 are independently selected from the group consisting of H, alkyl C1 - C2 - alquenilo 18, 18, (C1 - 18 alkyl (alkyl) Oh, SH 18 (C1, C2) alkyl - (3) Sch3 c1-4 alkyl, CONH2),(c1-4 alkyl (alkyl) COOH, NH2 (c1-4), c1-4 alkyl) NHC (NH2 + NH2 (C0), alkyl - (4 - 6), C3 (cycloalkyl) alkyl (C0, C2 Heterocyclic - 4) - (5), alkyl aryl C0 - 4 (C6) (10) R7, c1-4 alkyl (heteroaryl) C3 and C1 alkyl) - 9, - 12 (W1) alkyl C1 - 12, where W1 is a heteroatom selected from the group consisting of By N, s and o,Or R1 and R2 together with Atoms which are United to form a cycloalkyl C3 - 12； R3 is C1 - 18 alkyl； R4 and R5 R8 are each h； is nhr6 or R2, R5 and together with the Atoms which are United to form a Heterocyclic Ring 4,5 or 6 members； R6 H or c1-4 alkyl； and R7 is selected from the group consisting of H and Oh； where a - B Q is joined via a link between a-b and amide aliphatic amino Group of Q, where the half-life (T1 / 2) Chemical cleavage of a - B since q is at least 1 week and 1 hour N PBS under Physiological conditions, with the condition that when both R1 and R2 are h,R3 is C
