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DERIVADOS DE PIRAZINA COMO BLOQUEADORES DE ENaC
专利权人:
NOVARTIS AG
发明人:
BHALAY, GURDIP,EDWARS, LEE,HOWSHAM, CATHERINE,HUNT, PETER,SMITH, NICHOLA
申请号:
PE0005212013
公开号:
PE11632013A1
申请日:
2011.09.16
申请国别(地区):
PE
年份:
2013
代理人:
摘要:
Referring to a pyrazine Derivative of formula (i), wherein R1 is H, halogen, alkyl C8 C1 -, Halo - C1 C8 alkyl R2, R3, R4 and R5 are H or c1-c6 alkyl, R6, R7, R8 and R9 are h, so2r16 R10, among others - (alquileno is 0 to 3 carbon Atoms) - B - X - (cr11ar12a) M - (N - (cr11br12b) cr11cr12c) P - C (o) or R13 is optionally substituted aryl B Z X is (SO2), C (o) or oC (OR), r11a, r11b, among othersR11c, r12a, r12b and R12C is H, alkyl c1-c6 alkyl, among others R13 is C1 - C3 - C (o) or23, among others Z is o, c1-c6 alkyl, Oxo, CN, among others R23 is H, alkyl C8 cycloalkyl - C1 - C3, C8, among others, M, N, and P is an integer from 0 to 3. Preferred compounds are: dipropyl - carbamoyl methyl ester of the acid 3 - (3 - [2 - [(e) - 3.5 - diamino - 6 - Chloro - - 2 - - pirazin imino carbonyl] - - - - 1,3,8 triaza spiro [4.Deccan] - 5 - 8 - carbonyl} - bencen sulfonyl amino) - propionic acid, [(2 - hydroxy - methyl - ethyl) Carbamoyl] - methyl - Ester acid, 3 - [4 - ({2 - [(Z) - 3.5 - diamino - 6 - Chloro - pirazin - 2 - carbonyl - imino] - - - - 1,3,8 triaza spiro [4.5] dec-8-yl} - 3 - oxo - propyl) - phenoxy] - acetic acid, among others. It also relates to a Pharmaceutical composition.These compounds Act by blocking the epithelial sodium channel (ENAC) and are useful in the treatment of allergic or inflammatory diseases, obstructiveREFERIDA A UN DERIVADO PIRAZINA DE FORMULA (I), DONDE R1 ES H, HALOGENO, ALQUILO C1-C8, HALO-ALQUILO C1-C8, ENTRE OTROS R2, R3, R4 Y R5 SON H O ALQUILO C1-C6 R6, R7, R8 Y R9 SON H, SO2R16, ENTRE OTROS R10 ES -(ALQUILENO DE 0 A 3 ATOMOS DE CARBONO)-B-X-(CR11aR12a)m-(CR11bR12b)n-(CR11cR12c)p-C(O)OR13 B ES ARILO OPCIONALMENTE SUSTITUIDO CON Z X ES (SO2), C(O)O, OC(O), ENTRE OTROS R11a, R11b, R11c, R12a, R12b Y R12c SON H, ALQUILO C1-C6, ENTRE OTROS R13 ES ALQUILO C1-C3-C(O)OR23, ENTRE OTROS Z ES OH, ALQUILO C1-C6, OXO, CN, ENTRE OTROS R23 ES H, ALQUILO C1-C8, CICLOALQUILO C3-C8, ENTRE OTROS m, n Y p SON UN ENTERO DE 0 A 3. SON COMPUESTOS PREFERID
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