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US 10,590,125 B2Granted
Compounds
AssigneeProximagen Limited
InventorsMax Espensen, Lee Patient, David Evans, Edward Savory, Iain Simpson
Life of this patent
Estimating the term…
Abstract
The present invention relates to compounds which are inhibitors of SSAO activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.
Claims9
A compound of formula (I) or a pharmaceutically acceptable salt, or N-oxide thereof:
- wherein:
- Y is selected from hydrogen, hydroxyl, —NH2, —NH—C1-4-alkyl, —NH-halo-C1-4-alkyl, and —C1-4-alkoxy;
- Z is selected from hydrogen, halogen, hydroxyl, cyano, C1-4-alkyl, halo-C1-4-alkyl, C1-4-alkoxy, halo-C1-4-alkoxy, —CONH2, —SO2NH2, —NH2, —NHC1-4-alkyl, and —NHhalo-C1-4-alkyl;
- R1 is a phenyl ring being optionally substituted with one or more substituents selected from halogen, cyano, C1-4-alkyl, halo-C1-4-alkyl, cyano-C1-4-alkyl, —OR5, —NR4AR4B, —NR6C(O)OR5, —NR6C(O)R5, —NR6C(O)NR4AR4B, —C(O)NR4AR4B, —C(O)R5, —C(O)OR5, and —NR6S(O)2R5;
- R4A, R4B, R5 and R6 are each independently selected from hydrogen, C1-4-alkyl and halo-C1-4-alkyl;
- W is a pyridyl ring being optionally substituted with one or more substituents selected from halogen, cyano, C1-4-alkyl, halo-C1-4-alkyl, cyano-C1-4-alkyl, —OR5, —NR7AR7B, —NR6C(O)OR5, —NR6C(O)R5, —NR6C(O)NR7AR7B, —C(O)NR7AR7B, —C(O)R5, —C(O)OR5, —SO2R5, —SO2R7AR7B and —NR6S(O)2R5;
- R7A and R7B are independently hydrogen, C1-4-alkyl, or halo-C1-4-alkyl;
- V is selected from a bond, —O—, —N(R6)—, —(C═O)—, —CONR6—, —NR6C(O)—, and —C1-4-alkylene-, wherein the C1-4-alkylene group is optionally substituted by halogen, and wherein any one of the carbon atoms of the C1-4-alkylene group may be replaced by —O— or —N(R6)—;
- and
- R3 is a cyclobutyl ring optionally substituted with one or more substituents selected from halogen, oxo, hydroxyl, cyano, C1-4-alkyl, halo-C1-4-alkyl, cyano-C1-4-alkyl, —OR5, —NR4AR4B, —NR6C(O)OR5, —NR6C(O)R5, —NR6C(O)NR4AR4B, —C(O)NR4AR4B, —C(O)R5, —C(O)OR5, —SO2R5,—SO2NR4AR4B and —NR6S(O)2R5.
7 more elements
A pharmaceutical composition comprising:
- a pharmaceutically acceptable carrier and/or excipient;
- and
- a compound of formula (I) or a pharmaceutically acceptable salt, or N-oxide thereof:
- wherein:
- Y is selected from hydrogen, hydroxyl, —NH2, —NH—C1-4-alkyl, —NH-halo-C1-4-alkyl, and —C1-4-alkoxy;
- Z is selected from hydrogen, halogen, hydroxyl, cyano, C1-4-alkyl, halo-C1-4-alkyl, C1-4-alkoxy, halo-C1-4-alkoxy, —CONH2, —SO2NH2, —NH2, —NHC1-4-alkyl, and —NHhalo-C1-4-alkyl;
- R1 is a phenyl ring being optionally substituted with one or more substituents selected from halogen, cyano, C1-4-alkyl, halo-C1-4-alkyl, cyano-C1-4-alkyl, —OR5, —NR4AR4B, —NR6C(O)OR5, —NR6C(O)R5, —NR6C(O)NR4AR4B, —C(O)NR4AR4B, —C(O)R5, —C(O)OR5, and —NR6S(O)2R5,
- R4A, R4B, R5, and R6 are each independently selected from hydrogen, C1-4-alkyl and halo-C1-4-alkyl;
- W is a pyridyl ring being optionally substituted with one or more substituents selected from halogen, cyano, C1-4-alkyl, halo-C1-4-alkyl, cyano-C1-4-alkyl, —OR5, —NR7AR7B, —NR6C(O)OR5, —NR6C(O)R5, —NR6C(O)NR7AR7B, —C(O)NR7AR7B, —C(O)R5, —C(O)OR5, —SO2R5, —SO2R7AR7B and —NR6S(O)2R5;
- R7A and R7B are independently hydrogen, C1-4-alkyl, or halo-C1-4-alkyl;
- V is selected from a bond, —O—, —N(R6)—, —(C═O)—, —CONR6—, —NR6C(O)—, and —C1-4-alkylene-, wherein the C1-4-alkylene group is optionally substituted by halogen, and wherein any one of the carbon atoms of the C1-4-alkylene group may be replaced by —O— or —N(R6)—;
- and
- R3 is a cyclobutyl ring optionally substituted with one or more substituents selected from halogen, oxo, hydroxyl, cyano, C1-4-alkyl, halo-C1-4-alkyl, cyano-C1-4-alkyl, —OR5, —NR4AR4B, —NR6C(O)OR5, —NR6C(O)R5, —NR6C(O)NR4AR4B, —C(O)NR4AR4B, —C(O)R5, —C(O)OR5, —SO2R5, —SO2R4AR4B and —NR6S(O)2R5.
10 more elements
Dependencies are inferred from the claim text.