2-oxo-2-(2-phenyl-5,6,7,8-tetrahydro-indolizin-3-yl)-acetamide derivatives and related compounds as antifungal agents
AssigneeF2G Limited British Body Corporate
InventorsLloyd James Payne, Robert Downham, Graham Edward Morris Sibley, Philip Edwards, Gareth Morse Davies
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Abstract
The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof: wherein: R1, R2, R3, R4, R5, R6, R7, R8, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
Claims16
A tetrahydroindolizine derivative of formula (I), or a pharmaceutically or agriculturally acceptable salt thereof:
- wherein:
- R1 represents hydrogen, unsubstituted or substituted C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, —COR′ or —SO2(C1-C4 alkyl), or a group -A2, -L2-A2, -L3-A2 or -A2-L3-A3;
- A1, A2 and A3 are the same or different and represent C3-C6 cycloalkyl or an unsubstituted or substituted C6-C10 aryl or 5- to 12-membered heterocyclyl group;
- L1 represents a bond, a C1-C6 alkylene group in which none, one, two or three —CH2— groups are independently replaced by —O—, —S— or —NR′—, or a 5- to 12-membered heterocyclyl group;
- L2 represents —NR′—, —O—, —CO—, —OCO—, —OCONR′R″—, —CONR′R″— or —SO2—;
- L3 represents a bond or a C1-C4 alkylene group in which none, one or two —CH2— groups are independently replaced by —O—, —S— or —NR′—;
- n represents 0 or 1;
- R8 represents hydrogen or C1-C4 alkyl;
- R2 represents an unsubstituted or substituted group selected from C6-C10 aryl, a 5- to 12-membered heterocyclyl group, C1-C8 alkyl and C3-C6 cycloalkyl, halogen or a group of formula —B1—B2;
- B1 represents an unsubstituted or substituted C6-C10 aryl group;
- B2 represents an unsubstituted or substituted C6-C10 aryl or 5- to 12-membered heterocyclyl group;
- R3, R4, R5 and R6 independently represent C6-C10 aryl, a 5- to 12-membered heterocyclyl group, —(C1-C4 alkylene)-(C6-C10 aryl), —(C1-C4 alkylene)-(5- to 12-membered heterocyclyl), hydrogen, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, halogen, C3-C6 cycloalkyl, —OR′, —SR′, —SOR′, —SO2R′, —SO2NR′R″, —SO3H, —NR′R″, —NR′COR′, —CO2R′, —CONR′R″, —COR′, —OCOR′, —CF3, —NSO2R′ or —OCONR′R″;
- R7 represents hydrogen, halogen, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, —OR′, —CO2R′, —CONR′R″, —COR′, —CN, —NO2, —NR′R″, CF3, —Y—Z, C6-C10 aryl or a group of formula -Alk6-L5-A12, where Alk6 is a C1-C4 alkylene group, L5 is a group of formula —O—C(═O)—, —C(═O)— or —NR13-C(═O)— and R13 is hydrogen or C1-C4 alkyl, and A12 is an unsubstituted or substituted C6-C10 aryl or 5- to 12-membered heterocyclyl group;
- Y represents C1-C8 alkylene, C2-C8 alkenylene or C2-C8 alkynylene;
- Z represents halogen, C3-C6 cycloalkyl, —OR′, —SR′, —SOR′, —SO2R′, —SO2NR′R″, —SO3H, —NR′R″, —NR′COR′, —NO2, —CO2R′, —CONR′R″, —COR′, —OCOR′, —CN, —CF3, —NSO2R′, —OCONR′R″ or —CR′═NOR″;
- and
- R′ and R″ independently represent hydrogen, C1-C8 alkyl, C2-C8 alkenyl or C2-C8 alkynyl.
Dependencies are inferred from the claim text.