STPHANE DE LOMBEART,DANIEL R. GOLDBERG,KENNETH BRAMELD,ERIC BRIAN SJOGREN,ANDREW SCRIBNER
申请号:
ARP140103327
公开号:
AR097571A1
申请日:
2014.09.05
申请国别(地区):
AR
年份:
2016
代理人:
摘要:
Treatment of peripheral serotonin related diseases or diseases, such as gastroenteropathy, cardiovascular disease, lung disease, inflammation, metabolic disease or bone decay related diseases, as well as serotonin and cancer. 1. Requirement 1: a compound (1) with formula characteristics,a. Non cyclopentadiene with 4 to 10 members, or non cyclopentadiene with 5 to 10 members, or non cyclopentadiene with 5 to 10 members;W is n / cr83099;X is n or cr8310a;This is n or cr8311;There is only one in x E and N; R1 is h, c8321;- (CR R) NR Ro - (CR R) C (O) NR Rwherein said C₁₋₁₀ alkyl, C₃₋₁₀ cycloalkyl, and phenyl is optionally substituted in each case with 1, 2, 3, 4, or 5 substituents independently selected from F, Cl, Br, CN, C₁₋₄ alkyl, and C₁₋₄ haloalkyl; R² and R³ are independently selected from H, C₁₋₄ alkyl, and C₁₋₄ haloalkyl; R⁴ is H or C₁₋₄ alkyl; R⁵ and R⁶ are independently selected from H, halo, and C₁₋₄ alkyl; R⁷ is H, C₁₋₄ alkyl, C₂₋₆ alkenyl, C₆₋₁₀ cycloalkyl, C₆₋₁₀ cycloalkyl-C₁₋₄ alkyl, C₆₋₁₀ aryl, C₆₋₁₀ aryl-C₁₋₄ alkyl,4-10 membered heterocycloalkyl, (4-10 membered heterocycloalkyl) -C₁₋₄ alkyl, 5-10 membered heteroaryl, (5-10 membered heteroaryl) -C₁₋₄ alkyl, NR¹³R¹⁴,Or 830909,C (O) RS (O) qRwhere said C₁₋₄ alkyl, C₂₋₆ alkenyl, C₆₋₁₀ cycloalkyl, C₆₋₁₀ cycloalkyl-C₁₋₄ alkyl, C₆₋₁₀ aryl, C₆₋₁₀ aryl-C₁₋₄ alkyl, heterocycloalkyl of between 4 and 10 members, (4-10 membered heterocycloalkyl) -C₁₋₄ alkyl, 5-10 membered heteroaryl, and (5-10 membered heteroaryl) -C₁₋₄ alkyl is optionally substituted in each occurrence with 1, 2, or 3 substituents selected from halo, C₁₋₄ alkyl, C₂₋₆ alkenyl, amino, C₁₋₄ alkylamino, C₂₋₆ dialkylamino, hydroxy, and C₁₋₄ alkoxy;R⁸ and R⁹ are independently selected from H and C₁₋₄ alkyl; R¹⁰ is C₁₋₆ alkyl optionally substituted with 1, 2 or 3 substituents independently selected from C₁₋₆ haloalkyl, C₆₋₁₀ cycloalkyl, ORᵃ,7580 and r74966;Members of heterosexual; (4-10 member heterosexuals) - c83132248aquilo, 5-10 member heterosexuals,