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DERIVADOS DE DIAZAHETEROCICLOS N, N-DISUSTITUIDOS COMO INHIBIDORES DEL CANAL DE POTASIO MEDULAR EXTERNO RENAL (ROMK)
专利权人:
MERCK SHARP AND DOHME CORP.
发明人:
PASTERNAK, ALEXANDER,SHAHRIPOUR, AURASH,TEUMELSAN, NARDOS H.,YANG, LIHU,ZHU, YUPING,WALSH, SHAWN P.,TANG, HAIFENG
申请号:
PE0019122011
公开号:
PE03462012A1
申请日:
2010.04.29
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
Relates to Heterocyclic compounds of formula (i) where the Ring with 2 n is a compound of formula (i), (ii), among others Z1 is a compound of formula (Z1 - (R) - (Z1, Z2), among others, is a compound of formula (Z2 - i) (Z2 - II), among others, where X and y are each h, Oh, oalquilo (C1 - C3 - (f), among others x1 and Y1 are each H or CH3, R3A, r3b, R4A r4b are each cn and NO2.Among others, ra and RB are each h, Halo (C1 - C6) alkyl, optionally substituted with 1 to 3 - F, among others R5 and R6 are each h, alkyl, cycloalkyl (C1 - C6) (C3 and C6), NF3, among others.Preferred compounds are: 6 - [(1S) - 1 - hydroxy - 2 - (4 - [(2R) - 2 - hydroxy - 2 - (4 - methyl - 1 - 2 - oxo - 1,3 dihydro - benzofuran - 5 - il) ethyl] piperazin-1-yl] pyridin - ethyl} 3 - carbonitrilo {5,5 - Piperazine - 1.4 - diilbis [(1R) - 1 - hidroxietano - 2.1 - diyl]} bis (4 - methyl - 2 - benzofuran - 1 (3H) - One) 6 - [(1R) - 1 - hydroxy - 2 - (4 - [(2R) - 2 - hydroxy - 2 - (4 - methyl - 2 - oxo - 13 - dihydro - 2-benzofuran - 5 - il) ethyl] piperazin-1-yl] ethyl] - 4 - metoxipiridin - 3 - carbonitrilo among others. It also relates to a Pharmaceutical composition. These compounds are inhibitors of the renal Outer medullary Potassium Channel (romk) being useful in the treatment of hypertensionSE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA (I) DONDE EL ANILLO CON 2 N ES UN COMPUESTO DE FORMULA (i), (ii), ENTRE OTROS Z1 ES UN COMPUESTO DE FORMULA (z1-i), (z1-ii), ENTRE OTROS Z2 ES UN COMPUESTO DE FORMULA (z2-i), (z2-ii), ENTRE OTROS, EN DONDE X E Y SON CADA UNO H, OH, -OALQUILO(C1-C3), F, ENTRE OTROS X1 E Y1 SON CADA UNO H O CH3 R3a, R3b, R4a Y R4b SON CADA UNO CN, NO2, ENTRE OTROS Ra Y Rb SON CADA UNO H, HALO, ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO CON 1 A 3 DE -F, ENTRE OTROS R5 Y R6 SON CADA UNO H, ALQUILO(C1-C6), CICLOALQUILO(C3-C6), CF3, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 6-[(1S)-1-HIDROXI-2-{4-[(2R)-2-HIDROXI-2-(4-METIL-1-OXO-1,3-DIHIDRO-2-BENZOFURAN-5-IL)ETIL]PIPERAZIN-1-IL}ETIL]
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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