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3,4-Dihydropyrazine 2,3-b pyrazin-2 (1H) -one compounds as mTOR kinase inhibitors for oncological indications and diseases associated with the mTOR / PI3K / Akt pathway

机译:3,4-二氢吡嗪[2,3-b]吡嗪2(1H)-一种作为mTOR激酶抑制剂的化合物,用于与mTOR / PI3K / Akt途径相关的肿瘤适应症和疾病

摘要

A compound having the formula (II): ** Formula ** or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, wherein: R1 is pyridyl substituted with one or more substituents independently selected from the group consisting of C1- alkyl 8 substituted or unsubstituted, substituted or unsubstituted heterocyclyl, halogen, aminocarbonyl, cyano, hydroxyalkyl, -OR and -NR2, where each R is independently H, or a substituted or unsubstituted C1-4 alkyl; R2 is substituted or unsubstituted cycloalkyl, and R3 is H, or a substituted or unsubstituted C1-8 alkyl; wherein the term "substituted" denotes a substitution with any of the substituents recited in the subsequent claims or with halogen; I rent; hydroxyl; alkoxy; alkoxyalkyl; Not me; alkylamino; carboxy; nitro; cyano; thiol; thioether; imine; imide; amidine; guanidine; enamine; aminocarbonyl; acylamino; phosphonate; phosphine; thiocarbonyl; sulfonyl; sulfone; sulfonamide; ketone; aldehyde; ester; urea; urethane; oxime; hydroxyl amine; alkoxyamine; aralkoxyamine; N-oxide; hydrazine; hydrazide; hydrazone; azide; isocyanate; isothiocyanate; cyanate; thiocyanate; oxygen ( = O); B (OH) 2, O (alkyl) aminocarbonyl; cocloalkyl, which may be monocyclic or polycyclic condensed or non-condensed; heterocyclyl; which can be monocyclic or polycyclic condensed or non-condensed; condensed or non-condensed monocyclic or polycyclic aryl or heteroaryl; aryloxy; aralkyloxy; heterocyclyloxy or heterocyclyl alkoxy.
机译:具有式(II):** **的化合物或其药学上可接受的盐,立体异构体或互变异构体,其中:R1是被一个或多个独立选自C1-烷基8取代或未取代的取代基取代的吡啶基,取代或未取代的杂环基,卤素,氨基羰基,氰基,羟烷基,-OR和-NR 2,其中每个R独立地为H,或取代或未取代的C 1-4烷基; R2为取代或未取代的环烷基,R3为H或取代或未取代的C1-8烷基;其中术语“取代的”表示被随后的权利要求中所述的任何取代基或卤素取代;我租羟;烷氧基烷氧基烷基;不是我;烷基氨基;羧基硝基氰基;硫醇硫醚亚胺酰亚胺idine胍;胺氨基羰基酰基氨基膦酸酯膦;硫代羰基;磺酰基砜磺酰胺;酮;醛;酯;尿素氨基甲酸酯肟羟胺烷氧基胺芳烷氧基胺氮氧化物肼酰肼hydr叠氮化物异氰酸酯异硫氰酸酯氰酸盐硫氰酸盐氧气(> = O); B(OH)2,O(烷基)氨基羰基;共氯烷基,其可以是单环或多环稠合或非稠合的;杂环基它们可以是单环或多环稠合或非稠合的;稠合或非稠合的单环或多环芳基或杂芳基;芳氧基;芳烷氧基;杂环基氧基或杂环基烷氧基。

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