Carboximidamida Derivatives of benzimidazole compounds and imidazopiridina

摘要

1. The substance refers to indolamine inhibitor of 2,3-dioxane-1 (ido1);In addition to the pharmaceutical components including a formula compound (1),or its pharmaceutically acceptable salts, and methods of using them to treat diseases mediated by IDO1. Claim 1: A compound of the formula (1) characterized in that R¹ is mono or bicyclic aryl or heteroaryl, wherein each mono or bicyclic aryl or heteroaryl is optionally substituted with one, two or three substituents independently selected from hydroxyl, halo; -CN, C₁₋₆ haloalkyl,C₁₋₆ haloalkoxy,C₁₋₆ alkoxy,1. Lease land No. c833218331 and 832626;C₂₋₆ alkenyl,1. C 83228331 asphaand C₃₋₆ cycloalkyl,wherein two of the optional substituents can be joined to form an additional partially saturated heterocyclic ring; and where each C₁₋₆ alkoxy,1. Lease land No. c833218331 and 832626;C₂₋₆ alkenyl,1. C 83228331 asphaand C₃₋₆ cycloalkyl is optionally substituted with one, two or three substituents independently selected from hydroxyl, halo, -CN, -N (R²⁰) (R²²) and C₃₋₆ cycloalkyl;X is N or CR²ᶜ;749191,74955,and R²ᶜ each independently are hydrogen, hydroxyl, halo, CN, C₁₋₆ haloalkyl,C₁₋₆ haloalkoxy,C₁₋₆ alkoxy,or C₁₋₆ alkyl;Rs74969 and rs74977 are independent hydrogen, halide c833126;C₁₋₆ haloalkoxy,or C₁₋₆ alkyl;n and m are independently 0, 1, 2, or 3; each Rⁿ and Rᵐ are independently hydrogen, hydroxyl, halo, C₁₋₆ alkoxy,1. Lease land No. c833218331 and 832626;C₃₋₆ cycloalkyl,aryl, heterocyclyl, or heteroaryl; or two Rⁿ or Rᵐ join to form a C₃₋₆ cycloalkyl;and where each C₁₋₆ alkoxy,1. Lease land No. c833218331 and 832626;and C₃₋₆ cycloalkylaryl,1. Non-n-propene or isopropene can be replaced by one, two or three independent substitutes of hydroxyl, halogen-cn-n (r.83204);C₂₋₆ alkenyl,1. C 83228331 asphaC₁₋₆ haloalkyl,C₁₋₆ haloalkoxy,C₁₋₆ alkoxy,1. Lease land No. c833218331 and 832626;and C₃₋₆ cycloalkyl;L is a combination, nr-3,-C (O) -NR --NR -C (O) --NR³SO₂-,-NR SO -NR --1-2-2- that is...- yes.This is life. This is life.where t is 0, 1 or 2; each R³ is independently hydrogen, C₁₋₆ alkyl,C₃₋₆ cycloalkyl,aryl, heterocyclyl, or heteroaryl; and Rᵗ is hydrogen, C₁₋₆ alkyl,C₁₋₆ alkoxy,-C (O) R-C (O) OR-NC (O) OR-N (R) (R)-C (O) N (R) (R)-SO₂R²⁰,-N (R) SO (R)-N (R) SO -N (R) (R)-SO N (R) (R)cicloalquilo Caryl, heteroaryl, or heterocyclyl, provided that when Rᵗ C₁₋₆ alkoxy,-NC (O) OR-N (R) (R)-N (R) SO (R)-N (R) SO -N (R) (R)o - SO N (R) (R)and m is 0, then L is a union; wherein said C alquilo alkyl,C₁₋₆ alkoxy,cicloalquilo Ca. Arilo, isopropene or isopropene can be replaced by one, two or three independent hydroxy, halogen-no832222 substitutes;C₁₋₆ haloalkyl,C₁₋₆ haloalkoxy,-C (O) R-N (R) (R)-SO₂R²⁰,-N (R) SO (R)-N (R) SO -N (R) (R)-SO N (R) (R)C₃₋₆ cycloalkyl,-CN, C₁₋₆ alkoxy,1. Lease land No. c833218331 and 832626;and heterocyclyl; and wherein said heterocyclyl is optionally substituted with one or two oxo; wherein said C₃₋₆ cycloalkyl,C₁₋₆ alkyl or C₁₋₆ alkoxy is optionally substituted with one, two or three substituents independently selected from hydroxyl, halo, -NO₂,C₁₋₆ haloalkyl,C₁₋₆ haloalkoxy,C₁₋₆ alkoxy,-N (R) (R)-SO₂R²⁰,-N (R) SO (R)-N (R) SO -N (R) (R) -a. Y-so83222 (R 8304n) (R2);and said C₁₋₆ alkyl is optionally substituted with aryl; R²⁰,R2,and R²² are independently selected from hydrogen, C₁₋₆ alkyl,C₁₋₆ haloalkyl,C₃₋₆ cycloalkyl,1. Acyclic propene, isopropene and isopropene; among the alternatives of acyclic propene, isopropene or isopropene, one, two or three halogens can be selected; or one of the salts, isomers or the former salt, isomer or mixture acceptable on drugs.