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Antagonists of the il-8 receptors gonistas of il-8

机译:il-8的il-8受体促性腺激素拮抗剂

摘要

Compound administered in effective amount to a Mammal for the treatment of a disease mediated by chemokine, selected from the group consisting of malaria, restinosis,Angiogenesis, atherosclerosis, osteoporosis, gingivitis, unwanted release of Haematopoietic stem cells and diseases caused by Respiratory virus, herpes virus, and hepatitis virus,The chemokine that binds to a receptor or beta il-8, The Compound of formula (i) EMI file = "00044292 _ 1" id = "1" = : JPEG MFIs where z is or11, cyano, C (or c) nr15r16, R11 R18 (,, OR)Or s (OR) is 2r17; nitrogenUnder the condition that only one or two of the TRACES are the remaining Carbon and Nitrogen are replaced with Hydrogen or R1, R is any other functional or ionizable Hydrogen and has aN PKA of 10 or less; r1 is selected independentlyBetween Hydrogen, halogen, Nitro, cyano - 10 halosustituido C1; rent; rent alquenilo C1 - C2 - 10; 10; alkoxy C1 C1 - alkoxy - 10; 10 halosustituido; AZIDE; (cr8r8) QS (TR4); hydroxy c1-4 alkyl, HydroxyAryl alkyl; aryl; c1-4, ariloxi; aryl heteroaryl alquiloxi c1-4, heteroarilalquilo; radical; heterocycle; heterociclil c1-4 alkyl; heteroaryl - alquiloxi C1 - C2 - 4; alquenilo aryl heteroaryl - 10;Alquenilo C2 - 10; heterociclil - alquenilo C2 - 10; (cr8r8) qnr4r5; alquenil C2 - 10 - C (o) nr4r5 (cr8r8); (o) nr4r5 QC QC (cr8r8); (o) nr4r10; S (or S) 3h; (o) (cr8r8 QC (3R8); or R11; alquenil C2 - 10 - C (o) R11; alquenil C2 - 10 -(c) or11; (cr8r8) QC (or or12 (QOC); cr8r8 (R11); (o) cr8r8) qnr4c (R11); (cr8r8) QNHS (or 2r19 (QS) or cr8r8) or two (or 2nr4r5); r1 remains together can form or - (CH2) - or a saturated or unsaturated Ring 5 6Members; Q is 0 or an integer number that has a value of 1 to 10; t is 0 or an integer number that has a value of 1 or 2; s is an integer that has a value of 1 to 3 V is 0;Or a whole number that has a value of 1 to 4; R4 and R5 are independently Hydrogen, optionally substituted c1-4 alkyl, optionally substituted aryl,(optionally substituted aryl alkyl C1) - 4 - (heteroaryl heteroaryl, optionally substituted, optionally substituted alkyl) - C1 - 4, Heterocyclic radical or heterociclil c1-4 alkyl,Or R4 and R5 with nitrogen are United to form a Ring of 5 to 7 members that can contain an optional additional heteroatom selected from o / N / s;...
机译:以有效量向哺乳动物给药的化合物,用于治疗由趋化因子介导的疾病,选自疟疾,再狭窄,血管生成,动脉粥样硬化,骨质疏松,齿龈炎,造血干细胞的有害释放以及由呼吸道病毒,疱疹引起的疾病病毒和肝炎病毒,与受体或beta il-8结合的趋化因子,式(i)的化合物:JPEG MFI z为or11,氰基,C(或c)nr15r16,R11 R18(``OR)或s(OR)为2r17;氮在仅一个或两个TRACES残留的碳和氮被氢或R1取代的条件下,R为任何其他功能性或可电离的氢且N PKA为10以下; r1在氢,卤素,硝基,氰基之间独立选择-10 halosustituido C1;出租;出租alquenilo C1-C2-10; 10; C1-烷氧基-10; 10 halosustituido;叠氮化物; (cr8r8)QS(TR4);羟基C 1-4烷基,羟基芳烷基;芳基c1-4,ariloxi;芳基杂芳基alquiloxi c1-4,杂芳基基铝基;激进;杂环杂C1-4烷基;杂芳基-Alquiloxi C1-C2-4; Alquenilo芳基杂芳基-10; Alquenilo C2-10;异氰基-阿奎尼洛C2-10; (cr8r8)qnr4r5; Alquenil C2-10-C(o)nr4r5(cr8r8); (o)nr4r5 QC QC(cr8r8); (o)nr4r10; S(或S)3小时; (o)(cr8r8 QC(3R8);或R11; Alquenil C2-10-C(o)R11; alquenil C2-10-(c)or11;(cr8r8)QC(or or12(QOC); cr8r8(R11); (o)cr8r8)qnr4c(R11);(cr8r8)QNHS(或2r19(QS)或cr8r8)或两个(或2nr4r5); r1可以一起形成-(CH2)-或饱和或不饱和的5-6环成员; Q为0或值为1到10的整数; t为0或值为1或2的整数; s为值为1到3的整数V为0;或者a数值为1-4的整数; R4和R5独立为氢,任选取代的c1-4烷基,任选取代的芳基,(任选取代的芳烷基C1)-4-(杂芳基杂芳基,任选取代的,任选取代的烷基) -C 1-4,杂环基或杂环基的C 1-4烷基,或R 4和R 5与氮结合形成5至7个成员的环,该环可以包含选自o / N的任选的额外杂原子。 。

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