US2017320826A1PendingUtilityA1
Bivalent linkers and conjugates thereof
Est. expiryJul 23, 2024(expired)· nominal 20-yr term from priority
A61P 43/00A61K 49/0002C07D 401/12A61K 47/551C07D 475/04C07D 213/71A61K 47/6803
63
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Claims
Abstract
Bivalent linkers to be included in or for preparing vitamin, drug, diagnostic agent, and/or imaging agent conjugates are described.
Claims
exact text as granted — not AI-modified1 - 6 . (canceled)
7 . A compound of a formula selected from the group consisting of
wherein
D is a drug;
X 1 and X 2 are each independently a leaving group displaceable by a nucleophile;
R a and R b are each independently hydrogen or alkyl; or R a and R b are taken together with the attached carbon atom to form a carbocyclic ring;
L 1 and L 2 are each independently selected bivalent linkers; and
n is an integer from 1 to about 4.
8 . The compound of claim 7 , wherein X 1 is optionally substituted heteroarylthio.
9 . The compound of claim 7 , wherein X 1 is optionally substituted 2-pyridinylthio or optionally substituted 4-pyridinylthio.
10 . The compound of claim 7 , wherein X 1 is substituted by at least one electron withdrawing substituent selected from the group consisting of cyano, nitro, alkylsulfonyl, arylsulfonyl, halo, haloalkyl, acyl, and carboxyl.
11 . The compound of claim 7 , wherein X 1 is substituted by a nitro group.
12 . The compound of claim 7 , wherein X 1 is selected from the group consisting of
where * represents the point of attachment.
13 . The compound of claim 7 , wherein X 1 is
where * represents the point of attachment.
14 . The compound of claim 7 , wherein n is 1.
15 . The compound of claim 7 , wherein R a and R b are each independently hydrogen or lower alkyl.
16 . The compound of claim 7 , wherein R a and R b are each hydrogen.
17 . The compound of claim 7 , wherein R a and R b are taken together with the attached carbon atom to form a carbocyclic ring.
18 . The compound of claim 7 , wherein R a and R b are taken together with the attached carbon atom to form cyclopropyl.
19 . The compound of claim 7 , wherein the compound is of the formula
20 . The compound of claim 7 , wherein the compound is of the formulaJoin the waitlist — get patent alerts
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