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1, 2-DIHYDROCYCLOBUTANEDIONE DERIVATIVES AS NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE INHIBITORS
专利权人:
TOPOTARGET A/S
发明人:
KRISTENSEN Mette Knak (DK),КРИСТЕНСЕН Метте Кнак (DK),B'ERKLING Fredrik (SE),БЬЕРКЛИНГ Фредрик (SE),KRISTENSEN METTE KNAK,КРИСТЕНСЕН Метте Кнак,BERKLING FREDRIK,БЬЕРКЛИНГ Фредрик
申请号:
RU2011102444/04
公开号:
RU0002529468C2
申请日:
2009.06.24
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to compound of formula (I) , where A is selected from -C(=O)-, -S(=O)2-, and -P(=O)(R5)-, where R5 is selected from C1-6-alkyl, C1-6-alkoxy and hydroxy; B is selected from single bond, -O-, and -C(=O)-NR6-, where R6 is selected from hydrogen; D is selected from single bond, -O-, and -NR9, where R7, R8 and R9 are independently selected from hydrogen; m equals integer number 0-12 and n equals integer number 0-12, where the sum m+n equals 1-20; p equals integer number 0-2; R1 is selected from optionally substituted heteroaryl, where heteroaryl represents aromatic carbocyclic ring, where one carbon atom is substituted with heteroatom; R2 is selected from hydrogen, optionally substituted C1-12-alkyl, and substituents are selected from phenyl, morpholine, halogen and pyridine; C3-12-cycloalkyl, -[CH2CH2O]1-10-C1-6-alkyl); and R3 is selected from optionally substituted C1-12-alkyl, and substituents are selected from morpholine, phenyl, dialkylamine and C3-12-cycloalkyl, optionally substituted with halogen aryl; or R2 and R3 together with adjacent atoms form optionally substituted with alkylcarbonyl or alkyl N-containing heterocyclic or heteroaromatic ring; each of R4 and R4* independently represents hydrogen; and their pharmaceutically acceptable salts, as well as to application of said compounds for treatment of diseases/states, induced by increased level of nicotinamide phosphoribosyltransferase (NAmPRTase).EFFECT: obtaining novel compounds.21 cl, 1 dwg, 2 tbl, 83 exИзобретение относится к соединению формулы (I)где A выбирают из -C(=O)-, -S(=O)2-, и -P(=O)(R5)-, где R5 выбирают из C1-6-алкила, C1-6-алкокси и гидрокси; B выбирают из одинарной связи, -O-, и -C(=O)-NR6-, где R6 выбирают из водорода; D выбирают из одинарной связи, -O- и -NR9, где R7, R8 и R9 независимо выбирают из водорода; m равно целому числу 0-12 и n равно целому числу 0-12, где сумма m+n равна 1-20; p равно целому числу 0-2; R1 выбирают из нео
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