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DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF AS HIF ACTIVATORS
专利权人:
SANOFI
发明人:
ILLIANO, STEPHANE,MANETTE, GERALDINE,ALTENBURGER, JEAN-MICHEL,FOSSEY, VALERIE
申请号:
NZ59375109
公开号:
NZ593751A
申请日:
2009.12.24
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
Abstract 593751 The disclosure relates to compounds according to the formula (I) that are 2-pyridin-2-yl-pyrazol-3(2H)-one derivatives their preparation and their therapeutic uses and activity as HIF activators Disclosed are compounds according to the formula (I): R is a -SO2-NR3R4 group, a hydrogen atom, a halogen atom, a -halogeno(C1-C5)alkyl group, a -CO2R5 group or a -SO2-R4 group; R1 is a heterocycloalkyl group containing no nitrogen atoms, a -W-(C3-C6)cycloalkyl group, a -W-aryl group, a -W-heteroaryl group, a -W-heterocycloalkyl group, a -W-COOR5 group, a -W-CONR5R6 group; R2 is a hydrogen atom, a -(C1-C5)alkyl group, a -(C1-C5)alkylene-0-(C1-C5)alkyl group, a -halogeno(C1-C5)alkyl group, a -W-COOR5 group, a -W-C(O)NHR5 group or a -W-C(O)-NR5R6 group; n is 0, 1 or 2; W is a -(C1-C5)alkylene- group- or a -(C3-C6)cycloalkylene- group; R3 and R4, identical or different, are, independently from one another, a hydrogen atom, a -(C1-C5)alkyl group, a -(C3-C6)cycloalkyl group, a -(C1-C5)alkylene-O-(C1-C5)alkyl group, an aryl, a -CH2-aryl group, a heteroaryl, a heterocycloalkyl, a -W-OH group, a -W-CHOH-CH2OH group, a -W-CO2R5 group, a -W-NR5R6 group or a -W-O-(CH2)n-aryl group; or else R3 and R4 jointly form a heterocycloalkyl group with the nitrogen atom that supports them; R5 and R6, identical or different, are, independently from one another, a hydrogen atom, a -(C1-C5)alkyl group or a (C1-C5)halogenoalkyl group, as well as to a method for preparing same and their use in treatment of cardiac conditions. Compounds disclosed include: N-cyclopentyl-N-ethyl-6-[5-oxo-4-(pyridin-3-ylmethyl)-2,5-dihydro-1H-pyrazol-1-yl]pyridine-3-sulfonamide; N-(2,2-dimethylpropyl)-N-methyl-6-[5-oxo-4-(pyridin-3-ylmethyl)-2,5-dihydro-1H-pyrazol-1-yl]pyridine-3-sulfonamide; 6-(4-benzyl-5-oxo-2,5-dihydro-1H-pyrazol-1-yl)-N-cyclopentyl-N-[3-(dimethylamino)propyl]-pyridine-3-sulfonamide hydrochloride; And 4-(2-chlorobenzyl)-5-methyl-2-[5-(trifluoromethyl)pyridin-2-yl]-1,2-dihydro-3H-pyrazol
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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