PAUL MICHAEL SCOLA,ERIC P. GILLIS,ERIC MULL,QIAN ZHAO,LI SUN,KENNETH M. QIANG - BOY
申请号:
ARP160100725
公开号:
AR103969A1
申请日:
2016.03.17
申请国别(地区):
AR
年份:
2017
代理人:
摘要:
Claim 1: A compound characterized by the formula (1) or a pharmaceutically acceptable salt thereof, wherein: A is selected from the compounds of the group of formulas (2) wherein: the wavy line * indicates the point of attachment to the carbonyl group and the wavy line indicates the point of attachment to the nitrogen atom; n is 0 or 1; m is 1 or 2; w is 0, 1 or 2; R¹⁴ and R¹⁵ are independently selected from hydrogen and methyl; R¹⁶ᵃ is selected from hydrogen and C₁₋₆ alkyl; R¹⁶ is selected from - (C (R¹⁷ᵃ) ₂) -C (O) -NR⁵⁰R⁵¹;wherein: each R¹⁷ᵃ is independently selected from hydrogen and C₁₋₆ alkyl; one of R⁵⁰ and R⁵¹ is selected from hydrogen and C₁₋₆ alkyl, and the other is selected from - (CH₂) ₙX, C₁₋₆ alkyl, C₃₋₇ cycloalkyl, heterocyclyl and phenyl, wherein the cycloalkyl is optionally substituted with 1 , 2 or 3 groups independently selected from C₁₋₃ alkoxy, C₁₋₃ alkyl, amino, cyano and hydroxy, or; R⁵⁰ and R⁵¹,together with the nitrogen atom to which they are attached, they form a saturated, unsaturated ring of four, five, six or seven members that optionally contain one or two additional heteroatoms independently selected from nitrogen, oxygen and sulfur; wherein the ring is optionally substituted with one, two or three groups selected from C₁₋₆ alkoxy, C₁₋₃ alkyl, cyano, halo, halo-C₁₋₃ alkyl, hydroxy, hydroxy (C₁₋₃ alkyl),-8311; 8304; 8311;oxo and phenyl; wherein phenyl is optionally substituted with one, two or three groups independently selected from C₁₋₃ alkoxy, cyano and halo; n is 1-5; X is selected from a remainder of formula (3),Formula (4),C₂₋₆ alkoxymethyl, C₁₋₆ alkoxycarbonylmethyl, C₁₋₆ alkylsulfanylmethyl, C₁₋₆ alkylsulfonylmethyl, azidomethyl, tert-butoxymethyl, C₃₋₇ cycloalkyl, haloalkoxymethyl, halomethyl, heterocyclyl, hydroxymethyl, isopropoxymethyl, (NR⁷⁰R⁷¹) methyl, phenyl, phenyl, methyl Phenylsulfanylmethyl, one of R⁷⁰ and R⁷¹ is selected from hydrogen, C₁₋₆ alkyl and hydroxy-C₂₋₆ alkyl, and the other is selected from C₁₋₆ alkoxycarbo