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Pyrazin-carboxamides of the amiloride type as ENaC blockers
专利权人:
NOVARTIS AG
发明人:
BHALAY, Gurdip,BUDD, Emma,BLOOMFIELD, Graham Charles,COLLINGWOOD, Stephen Paul,DUNSTAN, Andrew,EDWARDS, Lee,GEDECK, Peter,HOWSHAM, Catherine,HUNT, Peter,HUNT, Thomas Anthony,OAKLEY, Paul,SMITH, Nichol
申请号:
ES08860731
公开号:
ES2602331T3
申请日:
2008.12.09
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
Compound according to the formula the ** Formula ** in which R6 and R11 are both H; R7, R8, R9, and R10 are each independently selected from H; SO2R16; aryl optionally substituted with one or more Z groups; a C3-C10 carbocyclic group optionally substituted with one or more Z groups; C3-C14 heterocyclic group optionally substituted with one or more Z groups; C1-C8 alkyl substituted with an aryl group optionally substituted with one or more Z groups, a C3-C10 carbocyclic group optionally substituted with one or more Z groups or a C3-C14 heterocyclic group optionally substituted with one or more Z groups; R16 is selected from C1-C8 alkyl, aryl and a 3- to 14-membered heterocyclic group; Z is independently selected from OH, aryl, O-aryl, C7-C14 aralkyl, C7-C14 O-aralkyl, C1-C6 alkyl, C1-C6 alkoxy, NR19 (SO2) R21, (SO2) NR19R21, (SO2) R20 , NR19C (O) R20, C (O) NR19R20, NR19C (O) NR20R18, NR19C (O) OR20, NR19R21, C (O) OR19, C (O) R19, SR19, OR19, oxo, CN, NO2 and halogen , wherein the alkyl, alkoxy, aralkyl and aryl groups are each optionally substituted with one or more substituents selected from OH, halogen, C1-C4 haloalkyl and C1-C4 alkoxy; R18, R19 and R20 are each independently selected from H and C1-C6 alkyl; R21 is selected from C1-C8 alkyl, aryl and a 3- to 14-membered heterocyclic group; n is 0 or 2; with the proviso that when n is 0, at least one of R6, R7, R8, R9, R10 and R11 is different from H.Compuesto según la fórmula la**Fórmula** en la que R6 y R11 son ambos H; R7, R8, R9, y R10 se seleccionan cada uno independientemente de H; SO2R16; arilo opcionalmente sustituido con uno o más grupos Z; un grupo carbocíclico C3-C10 opcionalmente sustituido con uno o más grupos Z; grupo heterocíclico C3-C14 opcionalmente sustituido con uno o más grupos Z; alquilo C1-C8 sustituido con un grupo arilo opcionalmente sustituido con uno o más grupos Z, un grupo carbocíclico C3-C10 opcionalmente sustituido con uno o más grupos Z o un grupo heterocíclico C3-C14 opcionalmente s
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