首页> 外国专利> Tienopirimidinas containing heterocicloalquilo inhibiting Mnk1 Kinases and / or Mnk2, Pharmaceutical compositions containing them and Use thereof for the treatment of Metabolic Disorders such as Diabetes and obesity, and hiperproliferativos disorders, among others.

Tienopirimidinas containing heterocicloalquilo inhibiting Mnk1 Kinases and / or Mnk2, Pharmaceutical compositions containing them and Use thereof for the treatment of Metabolic Disorders such as Diabetes and obesity, and hiperproliferativos disorders, among others.

机译:包含异环氯喹啉抑制Mnk1激酶和/或Mnk2的梯虫(Tienopirimidinas),含有它们的药物组合物及其在治疗代谢性疾病例如糖尿病和肥胖症以及髋关节增殖性疾病中的用途。

摘要

1: A compound characterized by a general formula (1), wherein X is ch or N, R1 is h, halogeno, CN, CH3 or CF3, and R2 is a selected (2) group in which (3) - SO2 - (c1-3 tar) can be used instead.-Co - (c1-3 tar)-Co - (CH2) N-O - (c1-3 tar),-CO- (CH2) nN (C1-3 alkyl) 2, C1-4 alkyl, - (CH2) n-CF3, - (CH2) n-CHF2, - (CH2) n-OH, - (CH2) nO- (C1-3 alkyl),- (CH2) n-CN, (4) and where it can be substituted on a carbon atom with a group -CH2OH, where n is 1 or 2, and where the group can be substituted on the nitrogen atom with alkyl (3 ) C1-4 linear or branched, - (CH2) n-CF3, - (CH2) n-CHF2, - (CH2) n-OH, - (CH2) nO- (C1-3 alkyl),-(CH2) n-cn, - (CH2) n-co-n (c1-3 tar) 2, - SO2 - (aiquilo c1-3),-Co - (c1-3 tar)-CO2 (C1-4 tar),-CO2 - (CH2) n-cf3 - (CH2) N-O - (c1-3 tar),-CO2 - (CH2) n-co-n (c1-3 tar) 2, (4) n is 1 or 2, R3 is a group of C1-2 tar, R4 is CO2 (c1-3 tar),-CO2- (CH2) nN (C1-3 alkyl) 2, -CONH2, -CO-NHR5, -CO-NH- (CH2) p-R6, -CO-NH- (CH2) m-R7, -CO- N (CH3) - (CH2) m-R7, CO-N (CH3) - (CH2) -cyclohexyl, (5),R5 is - CN - Oh, C1-6 linear tar or tree branch, or (c1-3 tar),1. Cycloquilo C3-6, SO2 - (c1-3 tar);Methyl can be used instead of pyridine formate, or methyl can be used instead of pyridine glycol. In methyl, NH2, - oh u-och3, - R6 es-c (CH3) 2Cl, - C (CH3) 2OH, - chc3-6 cyclopentadiene, oh can be used instead, methylene can be used instead, pindienediol, 1. C1-3 tar or oxo; tetrahydrofuran; tetrahydropyridine; phenyl, one or two kinds of - F, - Ci, - CN, - Oh, c1-3 U-O tar (c1-3 tar) can be used instead;Naftio; pyridine; furan; thiophosphor; oxazolilo; thiazole; pyrazole; morphine, optionally methyl substituted; benzothion; co-phenyl; o-so2-n (c1-3 tar) 2; R7 is f-oh-ocf3-o - (c1-3 tar)-O-phenyl-o (CH2) m-oh-n (c1-3 tar) 2, - nh-phenyl, pyridyl, pyridyl, Azerbaijani atom or aziridini, in which the hydrogen atom in the NH group can be replaced by c1-3 tar, in which p is 1, 2 or 3, M is 2 or 3, or a sea bream, enantiomero, diastereomero or salt thereof.
机译:1:以通式(1)为特征的化合物,其中X为ch或N,R 1为h,卤代,CN,CH 3或CF 3,R 2为选择的(2)基团,其中(3)-SO 2-( -Co-(c1-3 tar)-Co-(CH2)NO-(c1-3 tar),-CO-(CH2)nN(C1-3烷基)2,C1 -4烷基,-(CH2)n-CF3,-(CH2)n-CHF2,-(CH2)n-OH,-(CH2)nO-(C1-3烷基),-(CH2)n-CN,( 4)并且其中它可以在碳原子上被-CH2OH基团取代,其中n为1或2,并且其中该基团可以在氮原子上被烷基(3)C1-4直链或支链取代,-( CH2)n-CF3,-(CH2)n-CHF2,-(CH2)n-OH,-(CH2)nO-(C1-3烷基),-(CH2)n-cn,-(CH2)n-co -n(c1-3焦油)2,-SO2--(aiquilo c1-3),-Co-(c1-3焦油)-CO2(C1-4焦油),-CO2-(CH2)n-cf3-(CH2 )NO-(c1-3焦油),-CO2-(CH2)n-co-n(c1-3焦油)2,(4)n为1或2,R3为C1-2焦油基团,R4为CO2(c1-3焦油),-CO2-(CH2)nN(C1-3烷基)2,-CONH2,-CO-NHR5,-CO-NH-(CH2)p-R6,-CO-NH-(CH2 )m-R7,-CO- N(CH3)-(CH2)m-R7,CO-N(CH3)-(C H2)-环己基,(5),R5是-CN-哦,C1-6线性焦油或树枝,或(c1-3焦油),1。环基C3-6,SO2-(c1-3焦油);可用甲基代替甲酸吡啶,或用甲基代替吡啶二醇。在甲基NH2中,-OH-Och3,-R6 es-c(CH3)2Cl,-C(CH3)2OH,-chc3-6环戊二烯,可替代使用OH,可替代使用亚甲基,methylene二烯二醇1。 C1-3焦油或氧代;四氢呋喃四氢吡啶;苯基,可以使用-F,-Ci,-CN,-哦中的一种或两种,或者使用c1-3 U-O焦油(c1-3焦油)代替;吡啶呋喃硫代磷恶唑利洛噻唑吡唑吗啡,可选地被甲基取代;苯并硫磷;共苯基o-so2-n(c1-3焦油)2; R 7是f-oh-ocf3-o-(c1-3 tar)-O-苯基-o(CH2)m-oh-n(c1-3 tar)2-nh-苯基,吡啶基,吡啶基,阿塞拜疆原子或其中的NH基团中的氢原子可以被p1-3,p为1、2或3,M为2或3的c1-3焦油或其鲷,对映异构体,非对映异构体或其盐取代。

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