FLUOROPIRROLIDINS AS INHIBITORS OF DIPEPTIDIL PEPTIDASA.

摘要

A compound of formula (I): including its salts and solvates, wherein X is F or H; R1 and R2 are the same and are each optionally substituted aryl or heteroaryl; and R3 is H or alkyl; where the term "alkyl" refers to a saturated straight or branched chain aliphatic hydrocarbon that may be optionally substituted, allowing multiple degrees of substitution. The term "aryl" refers to an aromatic ring system, which includes condensed systems in which the ring (s) may be optionally substituted, allowing multiple degrees of substitution, and also includes an optional alkylene linker, such as C1-C6 alkylene , through which the aryl group may be attached; The term "heteroaryl" refers to a monocyclic aromatic ring system or a fused bicyclic aromatic ring system comprising two aromatic rings, wherein the heteroaryl rings contain one or more nitrogen, sulfur and / or oxygen atoms, wherein the N-oxides, sulfur oxides and dioxides are substitutions of allowable heteroatoms, and the rings can be optionally substituted, allowing multiple degrees of substitution, and also includes an optional alkylene linker, such as C1-C6 alkylene, through which it can be attached the heteroaryl group; "optionally substituted" denotes an optional substitution, one or more times, with acyl; I rent; alkenyl; alkynyl; alkylsulfonyl; alkoxy; cyano; halogen; haloalkyl; hydroxy; nitro; aryl, which may also be substituted with acyl, alkoxy, alkyl, alkenyl, alkynyl, alkylsulfonyl, cyano, halogen, haloalkyl, hydroxy or nitro; heteroaryl, which may also be substituted with acyl, alkoxy, alkyl, alkenyl, alkynyl, alkylsulfonyl, cyano, halogen, haloalkyl, hydroxy or nitro; arylsulfonyl, which may also be substituted with acyl, alkoxy, alkyl, alkenyl, alkynyl, alkylsulfonyl, cyano, halogen, haloalkyl, hydroxy or nitro; heteroarylsulfonyl, which may also be substituted with acyl, alkoxy, alkyl, alkenyl, alkynyl, alkylsulfonyl, cyano, halogen, haloalkyl, hydroxy or nitro; aryloxy, which may also be substituted with acyl, alkoxy, alkyl, alkenyl, alkynyl, alkylsulfonyl, cyano, halogen, haloalkyl, hydroxy or nitro; heteroaryloxy, which may also be substituted with acyl, alkoxy, alkyl, alkenyl, alkynyl, alkylsulfonyl, cyano, halogen, haloalkyl, hydroxy or nitro; -R''OR''R4; or -NR4R5; where for each case R '' is alkylene, alkenylene or alkynylene, and R4 and R5 are each independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, alkylsulfonyl, arylsulfonyl or heteroarylsulfonyl, where each occurrence of said aryl or heteroaryl may be substituted with one or more acyl, alkoxy, alkyl, alkenyl, alkylsulfonyl, cyano, halogen, haloalkyl, hydroxy or nitro, or R4 and R5 may be combined to form a ring, which optionally has additional heteroatoms, which optionally It has one or more degrees of unsaturation and can optionally be further substituted with acyl, alkoxy, alkyl, alkenyl, alkynyl, alkylsulfonyl, cyano, halogen, haloalkyl, hydroxy or nitro.