TETRAHYDROISOQUINOLIN-1-ONE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, USEFUL AS BB2 ANTAGONIST

FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry and specifically to novel tetrahydroisoquinolin-1-one derivatives of general formulaor pharmaceutically acceptable salts thereof, where Ris: lower alkylene-OH, lower alkylene-N(R)(R), lower alkylene-COR, Ccycloalkyl, Ccycloalkenyl, a...

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Hauptverfasser: KHISAMITI KHIROJUKI, SIMADA ITSURO, TAKUVA TOMOFUMI, ISIKHARA TSUKASA, ISIKAVA NORIKO, MAENO KIOITI, SIMIZU TAKAFUMI, SEKI NORIO
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry and specifically to novel tetrahydroisoquinolin-1-one derivatives of general formulaor pharmaceutically acceptable salts thereof, where Ris: lower alkylene-OH, lower alkylene-N(R)(R), lower alkylene-COR, Ccycloalkyl, Ccycloalkenyl, aryl, heterocyclic group, -(lower alkylen, substituted OR)-aryl or lower alkylene-heterocyclic group, where the lower alkylene in Rcan be substituted with 1-2 groups G; cycloalkyl, cycloalkenyl and heterocyclic group in Rcan be substituted with 1-2 groups G; aryl can be substituted with 1-2 groups G; R: identical or different from each other, each denotes H or a lower alkyl; R: R, or -S(O)-lower alkyl, Ris: lower alkyl, lower alkylene-OR, lower alkylene-aryl, lower alkylene-O-lower alkylene-aryl, -COR, -C(O)N(R), -C(O)N(R)-aryl, -C(O)N(R)-lower alkylene-aryl, aryl or heterocyclic group, where the aryl in Rcan be substituted with 1-3 groups G; Ris: H or lower alkyl, or Rand Rcan be combined to form C-alkylene; Ris: -N(R)(R), -N(R)-OR, -N(R)-N(R)(R), -N(R)-S(O)-aryl or -N(R)-S(O)-R, Ris: lower alkyl, halogen-lower alkyl, lower alkylene-CN, lower alkylene-OR, lower alkylene-COR, lower alkylene-C(O)N(R), lower alkylene-C(O)N(R)N(R), lower alkylene-C(=NOH)NH, heteroaryl, lower alkylene-X-aryl or lower alkylene-X-heterocyclic group, where the lower alkylene in Rcan be substituted with 1-2 groups G; aryl, heteroaryl and heterocyclic group in Rcan be substituted with 1-2 groups G; X is: a single bond, -O-, -C(O)-, -N(R)-, -S(O)- or *-C(O)N(R)-, where * in X has a value ranging from a bond to a lower alkylene, m is: an integer from 0 to 1, p is: is 2, Ris: H, or Rand Rcan be combined to form a lower alkylene-N(R)-lower alkylene group, Ris: aryl, Ris: H, Ris: lower alkyl, halogen, nitro, -OR, -N(R), or -O-lower alkylene-aryl, where the group Gis: -OR, N(R)(R) and aryl; group Gis: lower alkyl, lower alkylene-OR, -OR, -N(R), -N(R)-lower alkylene-OR, -N(R)C(O)OR, -N(R)C(O)-lower alkylene-OR, -N(R)C(O)N(R), -N(R)C(=NR)-lower alkyl, -N(R)S(O)-lower alkyl, -N(lower alkylene-COR)-S(O)-lower alkyl, -N(R)S(O)-aryl, -N(R)S(O)N(R), -S(O)-lower alkyl, -COR, -CO-lower alkylene-Si(lower alkyl), -C(O)N(R), -C(O)N(R)-lower alkylene-OR, -C(O)N(R)-lower alkylene-N(R), -C(O)N(R)-lower alkylene-COR, -C(O)N(R)-O-lower alkylene-heterocyclic group, -C(O)R, -C(O)-lower alkylene-OR, C(O)-heterocyclic group and oxo; under the condition that "aryl" in group Gcan be substituted with one lower alkyl;