主权项 |
1. A pharmaceutical composition comprising at least one pyrazolo piperidine derivative according to Formula (I) and a pharmaceutically acceptable carrier, diluent or excipient thereof: wherein R1 is selected from H; optionally substituted alkoxycarbonyl; optionally substituted C1-C6 alkyl; optionally substituted C2-C6 alkenyl; optionally substituted C2-C6 alkynyl; optionally substituted alkoxy; optionally substituted alkoxy C1-C6 alkyl; optionally substituted aminoalkyl; optionally substituted acyl; optionally substituted aryl; optionally substituted C1-C6 alkyl aryl; optionally substituted aryl C1-C6 alkyl; optionally substituted heteroaryl; optionally substituted C1-C6 alkyl heteroaryl; optionally substituted heteroaryl C1-C6 alkyl; optionally substituted C2-C6 alkenyl aryl; optionally substituted aryl C2-C6 alkenyl; optionally substituted C2-C6 alkenyl heteroaryl; optionally substituted heteroaryl C2-C6 alkenyl; optionally substituted C3-C8-cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted C1-C6 alkyl C3-C8-cycloalkyl; optionally substituted C3-C8-cycloalkyl C1-C6 alkyl; optionally substituted C1-C6 alkyl heterocycloalkyl or optionally substituted heterocycloalkyl C1-C6 alkyl; R2 is selected from H; optionally substituted C1-C6 alkyl; optionally substituted C2-C6 alkenyl; optionally substituted C2-C6 alkynyl; optionally substituted aryl; optionally substituted heteroaryl; optionally substituted C3-C8-cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted C3-C8-cycloalkyl C1-C6 alkyl; optionally substituted heterocycloalkyl C1-C6 alkyl; optionally substituted aryl C1-C6 alkyl or optionally substituted heteroaryl C1-C6 alkyl; R3 is selected from H, —S(O)—R4, —S(O)2—R4, optionally substituted C3-C8-cycloalkyl, optionally substituted heterocycloalkyl and —CR5R6R7; R4 is selected from H; optionally substituted amino; optionally substituted C1-C6 alkyl; optionally substituted C2-C6 alkenyl; optionally substituted C2-C6 alkynyl; optionally substituted alkoxy; optionally substituted alkoxy C1-C6 alkyl; optionally substituted aminoalkyl; optionally substituted acyl; optionally substituted aryl; optionally substituted C1-C6 alkyl aryl; optionally substituted aryl C1-C6 alkyl; optionally substituted heteroaryl; optionally substituted C1-C6 alkyl heteroaryl; optionally substituted heteroaryl C1-C6 alkyl; optionally substituted C2-C6 alkenyl aryl; optionally substituted aryl C2-C6 alkenyl; optionally substituted C2-C6 alkenyl heteroaryl; optionally substituted heteroaryl C2-C6 alkenyl; optionally substituted C3-C8-cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted C1-C6 alkyl C3-C8-cycloalkyl; optionally substituted C3-C8-cycloalkyl C1-C6 alkyl; optionally substituted C1-C6 alkyl heterocycloalkyl or optionally substituted heterocycloalkyl C1-C6 alkyl; R5 is selected from H and —CR8R9R10; R6 is selected from H and —CR11R12R13; R7 is selected from H and —CR14R15R16 and —C(O)—R17; R8, R9, R10, R11, R12, R13, R14, R15, R16 and R17 are independently selected from H; halogen; optionally substituted amino; optionally substituted acyl; optionally substituted C1-C6 alkyl; optionally substituted C2-C6 alkenyl; optionally substituted C2-C6 alkynyl; optionally substituted aryl; optionally substituted C1-C6 alkyl aryl; optionally substituted aryl C1-C6 alkyl; optionally substituted heteroaryl; optionally substituted C1-C6 alkyl heteroaryl; optionally substituted heteroaryl C1-C6 alkyl; optionally substituted C2-C6 alkenyl aryl; optionally substituted aryl C2-C6 alkenyl; optionally substituted C2-C6 alkenyl heteroaryl; optionally substituted heteroaryl C2-C6 alkenyl; optionally substituted C3-C8-cycloalkyl; optionally substituted heterocycloalkyl; optionally substituted C1-C6 alkyl C3-C8-cycloalkyl; optionally substituted C3-C8-cycloalkyl C1-C6 alkyl; optionally substituted C1-C6 alkyl heterocycloalkyl or optionally substituted heterocycloalkyl C1-C6 alkyl; —CR8R9R10, —CR11R12R13 or —CR14R15R16 can independently form an optionally substituted ring selected from an optionally substituted aryl; an optionally substituted heteroaryl; an optionally substituted C3-C8-cycloalkyl or an optionally substituted heterocycloalkyl; or tautomers, geometrical isomers, optically active forms, and pharmaceutically acceptable salts and thereof. |