CPC A61K 31/166 (2013.01) [A61K 31/351 (2013.01); A61K 31/405 (2013.01); A61K 38/45 (2013.01); A61K 47/545 (2017.08); A61K 47/55 (2017.08); A61K 47/555 (2017.08); A61P 35/00 (2018.01); C07D 401/14 (2013.01); C07D 405/12 (2013.01); C07D 405/14 (2013.01); C07D 409/14 (2013.01); C07D 417/14 (2013.01); C07D 471/04 (2013.01); C12N 9/1007 (2013.01); C12Y 201/01043 (2013.01)] | 16 Claims |
1. A compound having the chemical structure:
ULM-L-PTM,
or a pharmaceutically acceptable salt thereof,
wherein:
(a) the ULM is:
wherein:
W is CH2 or C═O;
A is H;
represents a bond that may be stereospecific or non-stereospecific;
n is 1; and
R is a bond to the chemical linking moiety or NHR′ covalently joined to the chemical linking moiety;
R′ is alkyl;
(b) the L is a chemical linking moiety connecting the ULM and the PTM which comprises (1) a chemical structural unit represented by the formula:
—(CH2)m-O(CH2)n-O(CH2)o-O(CH2)p-O(CH2)q-O(CH2)r-O—, —NH—(CH2)m-O(CH2)n-O(CH2)o-O(CH2)p-O(CH2)q-O(CH2)r-O—;
wherein:
each m, o, p, q, and r of the chemical linking moiety are independently 0, 1, 2, 3, 4, 5, 6, with the proviso that when the number is zero, there is no N—O or O—O bond;
n of the chemical linking moiety is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10; or
(2) a polyethylenoxy group comprising 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10 ethylene glycol units; and
(c) the PTM is PTM-I-1, PTM-IVa-1, or PTM-IVb-1:
wherein:
WPTM and XPTM are independently C or N;
YPTM and ZPTM are CH;
XPTM1 is NH or O;
XPTM2 is absent;
RPTM is methyl or methoxy;
RPTM5 is methyl; and
indicates a covalent linkage to the chemical linking moiety.
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