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US 2012/0237475 A1Published application
Novel Inhibitors
AssigneeProbiodrug AG
InventorsUlrich Heiser, Daniel Ramsbeck
Life of this patent
Estimating the term…
Abstract
Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).
Claims15
A compound of formula (I):
- or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein:
- R1 represents hydrogen, halogen, —C1-6alkyl, C2-6alkenyl, C2-6alkynyl, -aryl, —C1-6alkylaryl, -cycloalkyl, —C1-6alkylcycloalkyl, -heteroaryl, —C1-6alkylheteroaryl, -heterocyclyl, —C1-6alkylheterocyclyl, -cycloalkyl substituted by phenyl, -cycloalkyl substituted by phenoxy, -phenyl substituted by cycloalkyl, -phenyl substituted by phenoxy, -phenyl substituted by phenyl, heterocyclyl substituted by phenyl, heteroaryl substituted by phenyl, phenyl substituted by heterocyclyl, phenyl substituted by heteroaryl, phenyl substituted by —O-cycloalkyl, phenyl substituted by -heterocyclyl-phenyl or phenyl substituted by -cycloalkyl-heterocyclyl;
- and in which any of aforesaid aryl, cycloalkyl, heterocyclyl, heteroaryl, phenyl or phenoxy groups may optionally be substituted by one or more Rb groups selected from C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, —C1-6thioalkyl, —SOC1-4alkyl, —SO2C1-4alkyl, C1-6alkoxy-, C1-6haloalkoxy, —O—C3-8cycloalkyl, C3-8cycloalkyl, —SO2C3-8cycloalkyl, —SOC3-6cycloalkyl, C3-6alkenyloxy-, C3-6alkynyloxy-, —C(O)C1-6alkyl, —C(O)OC1-6alkyl, C1-6alkoxy-C1-6alkyl-, nitro, halogen, cyano, hydroxyl, ═O, —C(O)OH, —NH2, —NHC1-4alkyl, —N(C1-4alkyl)(C1-4alkyl), —C(O)N(C1-4alkyl)(C1-4alkyl), —C(O)NH2, —C(O)NH(C1-4alkyl) and —C(O)NH(C3-10cycloalkyl);
- R2 represents ═O, —O—C1-6alkyl, —NR3R4 or —O—C1-6haloalkyl;
- R3 and R4 independently represent hydrogen, C1-6alkyl or C3-8cycloalkyl;
- or R3 and R4 together with the nitrogen atom to which they are attached may form a heterocyclyl group optionally substituted by one or more Rb groups;
- n represents an integer selected from 0 to 3;
- and
- Ra represents C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, —C1-6thioalkyl, —SOC1-4alkyl, —SO2C1-4alkyl, C1-6alkoxy-, —O—C3-8cycloalkyl, C3-8cycloalkyl, —SO2C3-8cycloalkyl, —SOC3-6cycloalkyl, C3-6alkenyloxy-, C3-6alkynyloxy-, —C(O)C1-6alkyl, —C(O)OC1-6alkyl, C1-6alkoxy-C1-6alkyl-, nitro, halogen, cyano, hydroxyl, —C(O)OH, —NH2, —NHC1-4alkyl, —N(C1-4alkyl)(C1-4alkyl), —C(O)N(C1-4alkyl)(C1-4alkyl), —C(O)NH2, —C(O)NH(C1-4alkyl) and —C(O)NH(C3-10cycloalkyl).
6 more elements
Dependencies are inferred from the claim text.