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US 10,376,531 B2Granted
Substituted-6,8-dioxabicyclo[3.2.1]octane-2,3-diol compounds as targeting agents of ASGPR
AssigneePfizer Inc.
InventorsSpiros Liras, Vincent Mascitti, Benjamin Thuma
Life of this patent
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Abstract
Compounds of Formula (A) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by pharmaceutical compositions and the uses thereof as asialoglycoprotein receptor (ASGPR) targeting agents.
Claims7
A compound of Formula (A)
- wherein
- R1 is —Z—X—Y wherein X is a linker of any of structures L1or L2
- each Q is independently absent or is C(O), C(O)—NR4, NR4—C(O),O—C(O)—NR4, NR4—C(O)—O, —CH2—, or —O—, wherein at least two carbon atoms separate the —O— from any other heteroatom group;
- each T is independently absent or is alkylene, wherein one or more —CH2— groups of the alkylene, may each independently be replaced with a —O—, wherein the —O— are separated by at least 2 carbon atoms;
- Y is an amino acid sequence, a nucleic acid sequence, or an oligomer, and
- Z is absent;
- each n is independently 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, or 40, wherein if n is greater than 1, each T and each Q of each (T-Q-T-Q) is independently selected;
- R2 is —N(R3)—C(O)—R3 or —N(R3)—C(O)—OR3;
- and
- each R3 is independently H, —(C1-C5)alkyl, halo-substituted (C1-C5)alkyl, or (C3-C6)cycloalkyl,
- each R4 is independently —H, —(C1-C20)alkyl, or (C3-C6)cycloalkyl wherein one to six —CH2— groups of the alkyl or cycloalkyl separated by at least two carbon atoms may be replaced with —O—, —S—, or —N(H)—, and wherein the alkyl and cycloalkyl may be substituted with one to six halo atoms;
- and
- or a pharmaceutically acceptable salt thereof.
10 more elements
A compound of Formula (A)
- wherein
- R1 is —Z—X—Y, —Z—Y, or —X—Y wherein X is a linker of any of structures L1, L2, L9 or L10
- each Q is independently absent or is C(O), C(O)—NR4, NR4—C(O),O—C(O)—NR4, NR4—C(O)—O, —CH2—, or —O—, wherein at least two carbon atoms separate the —O— from any other heteroatom group;
- each T is independently absent or is alkylene, wherein one or more —CH2— groups of the alkylene, may each independently be replaced with a —O—, wherein the —O— are separated by at least 2 carbon atoms;
- Y is an amino acid sequence, a nucleic acid sequence, or an oligomer, and
- Z is absent;
- each n is independently 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10,11,12,13,14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, or 40, wherein if n is greater than 1, each T and each Q of each (T-Q-T-Q) is independently selected;
- R2 is —N(R3)—C(O)—R3 or —N(R3)—C(O)—OR3, and
- each R3 is independently —H, —(C1-C5)alkyl, halo-substituted (C1-C5)alkyl, or (C3-C6)cycloalkyl,
- each R4 is independently-H, —(C1-C20)alkyl, or (C3-C6)cycloalkyl wherein one to six —CH2— groups of the alkyl or cycloalkyl separated by at least two carbon atoms may be replaced with —O—, —S—, or —N(H)—, and wherein the alkyl and cycloalkyl may be substituted with one to six halo atoms;
- and
- or a pharmaceutically acceptable salt thereof.
9 more elements
Dependencies are inferred from the claim text.