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US 11,964,942 B2Granted
SSAO inhibitors and use thereof
AssigneeEccogene (Shanghai) Co., Ltd.
InventorsZaifang Ren, Xuefeng Sun, Qing Xu
Life of this patent
Estimating the term…
Abstract
The application relates to a compound of Formula (I′) or (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of Formula (I′) or (I), and a method of treating or preventing a disease in which SSAO plays a role.
Claims21
A compound of Formula (I)
- or a pharmaceutically acceptable salt, solvate, stereoisomer, or tautomer thereof, wherein:
- each X is independently Cl or F;
- p is 0, 1, 2, or 3;
- L is absent, —O—, (C1-C4) alkylene, substituted (C1-C4) alkylene, —O—(C1-C4) alkylene, substituted —O—(C1-C4) alkylene, (C1-C4) alkylene-O—, or substituted (C1-C4) alkylene-O—, wherein the substituted (C1-C4) alkylene, substituted —O—(C1-C4) alkylene, or substituted (C1-C4) alkylene-O— is substituted with one or more L1;
- each L1 is independently (C1-C4) alkyl, F, or CF3;
- or two L1, together with the atom to which they are attached, form a 3- to 5-membered cycloalkyl ring;
- each R1 is independently H, F, methyl, ethyl, or CF3;
- R2 is (C1-C4) alkyl substituted with one or more (C1-C4) alkoxy, (C1-C4) alkoxy, NR3C(O)R4, or C(O)NR3R4;
- or
- R2 is
- wherein R2 is optionally substituted with one or more R5;
- R3 is H, methyl, or ethyl;
- R4 is (C1-C4) alkyl or (C3-C10) cycloalkyl optionally substituted with one or more R8;
- or
- R3 and R4, together with atom(s) to which they are attached, form a 3- to 6-membered ring optionally comprising one additional heteroatom selected from N and O and optionally substituted with one or more R5;
- each R5 is independently (C1-C4) alkyl, (C1-C4) alkoxy, hydroxy, cyano, oxo, C(O)R7, C(O)NR7R7′, NR3C(O)R7, NR3S(O)2R4, S(O)2R4, (C1-C4) alkyl substituted with one or more hydroxy or R6, (C3-C10) cycloalkyl optionally substituted with one or more hydroxy or R6, or heterocyclyl comprising one or two 3- to 6-membering rings and 1 to 3 heteroatoms selected from N and O and optionally substituted with one or more hydroxy or R6;
- or two R5, together with the atom or atoms to which they are attached, form a 3- to 5-membered saturated or 5- or 6-membered aromatic ring optionally comprising 1 or 2 heteroatoms selected from N and O;
- each R6 is independently NR3C(O)R7 or C(O)NR3R7;
- each R7 is independently
- OH, (C1-C4) alkoxy, (C1-C6) alkyl optionally substituted with one or more (C1-C4) alkoxy, CF3, F, or (C3-C10) cycloalkyl,
- (C3-C10) cycloalkyl optionally substituted with one or more R8, or
- phenyl optionally substituted with one or more R8;
- each R7′ is independently H, methyl, or ethyl;
- or
- R7 and R7′, together with the atom to which they are attached, form a 3- to 6-membered ring optionally comprising one additional heteroatom selected from N and O and optionally substituted with one or more R8;
- or
- R3 and R7, together with atom(s) to which they are attached, form a 3- to 6-membered ring optionally comprising one additional heteroatom selected from N and O and optionally substituted with one or more R8;
- and
- each R8 is independently (C1-C4) alkyl, (C1-C4) alkoxy, CF3, OH, or F.
26 more elements
Dependencies are inferred from the claim text.