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    • 3. 发明授权
    • Allene polyamines
    • 艾伦聚氨酯
    • US3712896A
    • 1973-01-23
    • US3712896D
    • 1971-02-25
    • RICHARDSON MERRELL INC
    • TILFORD CBLOHM TMCKENZIE R
    • C07C47/21C07D203/12C07D233/06C07D29/28
    • C07D233/06C07C47/21C07D203/12
    • NOVEL COMPOUNDS WHICH HAVE ACTIVITY IN INHIBITING THE CLOTTING OF BLOOD ARE SELECTED FROM BASES OF THE FORMULA

      R3-(R4-)C=C=C(-R5)-C(-R6)(-R7)-CH2-NH-A

      WHEREIN: (A) R3 IS HYDROGEN, (LOWER)ALKYL OR (LOWER)ALKENYL; (B) R4 IS (LOWER)ALKYL OR (LOWER)ALKENYL; (C) R3 AND R4 TAKEN TOGETHER WITH THE CARBON ATOM TO WHICH THEY ARE ATTACHED IS CYCLOALKYL OF 5 TO 7 RING CARBON ATOMS; (D) R5 IS HYDROGEN OR (LOWER)ALKYL; (E) EACH OF R6 AND R7 IS (LOWER)ALKYL, (LOWER)ALLKENYL, OR R6 AND R7 TOGETHER WITH CARBON ATOMS TO WHICH THEY ARE ATTACHED IS (I) CYCLOALKYL OF 5 TO 7 RING CARBON ATOMS; (II) CYCLOALKENYL OF 5 TO 7 RING CARBON ATOMS; OR (III) BICYCLOALKYL SELECTED FROM BORNYL, NORBORNYL OR NORBORNENYL; (F) A IS THE GROUP (I)

      -X-N(-R1)-R2

      WHEREIN X IS ALKYLENE OF 2 TO ABOUT 8 CARBON ATOMS AND SEPARATES THE ADJACENT NITROGEN ATOMS BY AN ALKYLENE CHAIN OF AT LEAST 2 CARBON ATOMS, MONOHYDROXY ALKYLENE OF 3 TO ABOUT 8 CARBON ATOMS, AND SEPARATES THE ADJACENT NITROGEN ATOMS BY AN ALKYLENE CHAIN OF AT LEAST 3 CARBON ATOMS, OR A CYCLOALKYLSUBSTITUTED ALKYLENE GROUP OF THE FORMULA

      (-CH2)V-C(-(CH2)U-)-(CH2)V''-

      WHEREIN EACH OF V AND V'' IS AN INTEGER OF 0 TO 4, U WHEREIN EACH OF V AND V'' IS AN INTEGER OF 0 TO 4, U IS AN INTEGER OF 3 TO 5 PROVIDED THAT AT LEAST ONE OF V AND V'' IS 1, AND THE TOTAL OF V, V7 AND U IS NOT GREATER THAN 8, R1 IS HYDROGEN, (LOWER)ALKYL, PHENYL, HYDROXY(LOWER)ALKYL, CYCLOALKYL OF 4 TO 6 RING CARBON ATOMS, DI(LOWER)ALKYLAMINO(LOWER)ALKYL, PYRIDYL(LOWER)ALKYL, PIPERIDYL(LOWER)ALKYLAMINO(LOWER) ALKYL, OR PIPERIDYL(LOWER)ALKYL, R2 IS HYDROGEN, (LOWER)ALKYL OR HYDROXY(LOWER)ALKYL, OR R1 AND R2 TAKEN TOGETHER WITH THE NITROGEN TO WHICH THEY ARE ATTACHED IS PIPERAZINO, N-(LOWER)ALKYLPIPERAZINO, MORPHOLINO, PYRROLIDINO, AZIRIDINO, PIPERIDINO, (LOWER)ALKYLPIPERIDINO, (LOWER)ALKYLIMIDAZOLIDINO, OR (II) A IS

      -(CH2)N-CH
      WHEREIN N'' IS AN INTEGER OF 0 TO 3, M IS AN INTEGER OF 1 OR 2, R8 IS HYDROGEN, (LOWER)ALKYL, (LOWER) ALKENYL, HYDROXY(LOWER)ALKYL, PHENYL(LOWER)ALKYL, CYANO(LOWER)ALKYL, PIPERIDINO(LOWER)ALKYL, R9 IS (LOWER)ALKYL; AND N IS IN INTEGER OF 0 TO 4; OR PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALTS OF SAID BASES.