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PROTEIN INFOSPHATASE-1 INHIBITORS AND THEIR APPLICATION
专利权人:
Говард Юнивесити (US)
发明人:
НЕХАЙ Сергей (US),КОВАЛЬСКИЙ Дмитро Б. (UA)
申请号:
RU2010146147/13
公开号:
RU2010146147A
申请日:
2009.04.14
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
1. The compound of formula (I):! ! where n is 1 or 2; ! Ar is phenyl or thienyl and is optionally substituted; ! R1 independently in each case is R6, C (O) R6, C (O) -OR6 or C (O) N (R6) 2; ! R2 is H or an optionally substituted C1-C6 alkyl or a group of the formula -C (O) NH-R1; ! R3 is independently selected at each occurrence from halogen, NO2, CN, R, OR, NR2; S (O) qR, COOR and CONR2, where each R is independently H, C1-C4 alkyl or C1-C4 haloalkyl; ! m is 0-4; ! R4 is R6, halogen, = O, COOR6, CON (R6) 2, S (O) qR6, N (R6) 2 or OR6; ! p is 0-2; ! each q independently represents 0-2; ! Z is O or NR5; ! R5 is R6 or C (O) R6; and! R6 is independently selected at each occurrence from H, C1-C6 alkyl, C5-C6 aryl, and (C5-C6-aryl) -C1-C6 alkyl, where each alkyl and aryl is optionally substituted; ! provided that n is 2 when Z is O and Ar is para-halogenophenyl; ! or a pharmaceutically acceptable salt thereof. ! 2. The compound according to claim 1, which is a pharmaceutically acceptable salt of the compounds of formula I.! 3. The compound according to claim 1, in which Z is O.! 4. The compound according to claim 1, in which n is 1.! 5. The compound according to claim 1, in which n is 2.! 6. The compound according to claim 1, in which R2 is H or C1-C4 alkyl. ! 7. The compound of claim 1, wherein Ar is optionally substituted phenyl. ! 8. The compound according to claim 1, in which Ar is optionally substituted 2-thienyl. ! 9. The compound of claim 1, wherein Ar is optionally substituted 3-thienyl. ! 10. A pharmaceutical composition comprising a compound of formula (I) in a mixture with at least one pharmaceutically acceptable excipient or diluent. ! 11. A method of treating a subject infected with HIV-1 or with an increased risk of infection1. Соединение формулы (I): ! ! где n обозначает 1 или 2; ! Ar обозначает фенил или тиенил и является необязательно замещенным; ! R1 независимо в каждом случае обозначает R6, C(O)R6, C(O)-OR6 или C(O)N(R6)2; ! R2 обозначает Н или нео
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