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    • 4. 发明授权
    • Indolocarbazoles from saccharothrix aerocolonigenes copiosa subsp. nov
SCC 1951 ATCC 53856
    • 来自糖酵母(Aerobolithrix aerocolonigenes copiosa subsp。)的Indolocarbazoles nov SCC 1951 ATCC 53856
    • US5618809A
    • 1997-04-08
    • US394937
    • 1995-02-27
    • Ellen B. BarrabeeAnn C. HoranFrank A. GentileMahesh G. Patel
    • Ellen B. BarrabeeAnn C. HoranFrank A. GentileMahesh G. Patel
    • C12P17/18C07D498/22A61K31/55
    • C12P17/18
    • N-alkanoyl derivatives of staurospodne represented by the formula I ##STR1## wherein R.sub.a and R.sub.b are each H or ##STR2## wherein R.sub.1 and R.sub.2 are independently H or --OH or --OCH.sub.3 and R.sub.3 is OH, NHCH.sub.3, NCH COCH.sub.3 or NHCOCH.sub.3 and R.sub.4 is OH or H and, stereochemical isomers thereof with the provisos that (1) when R.sub.a and R.sub.b .dbd.A, and R.sub.1.dbd.H.sub.2 or OH R.sub.3 is not NHCH.sub.3 ; (2) when R.sub.a and R.sub.b.dbd. B, then R.sub.1 .dbd.R.sub.4 .dbd.OH or R.sub.1 .dbd.R.sub.4 .dbd.H; (3) when R.sub.a .dbd.R.sub.b .dbd.H R.sub.1 .dbd.--OCH.sub.3, and (4) when R.sub.a and R.sub.b .dbd.A, and R.sub.1 .dbd.H and R.sub.2 .dbd.OCH.sub.3, then R3 is not and ##STR3## pharmaceutical compositions thereof useful for inhibiting myosin light chain kinase, protein kinase C or tumor cell proliferation as well as producing an antihypertensive effect and an anti-inflammatory effect in warm-blood animals such as man are disclosed.
    • 其中R a和R b各自为H或A,其中R 1和R 2独立地为H或-OH或-OCH 3且R 3为OH,NHCH 3, NCH COCH 3或NHCOCH 3和R 4是OH或H及其立体化学异构体,条件是(1)当R a和R b = A时,R 1 = H 2或OH R 3不是NHCH 3; (2)当Ra和Rb = B时,R1 = R4 = OH或R1 = R4 = H; (3)当Ra = Rb = H R1 = -OCH3时,和(4)当Ra和Rb = A,R1 = H和R2 = OCH3时,R3不是和其中用于抑制肌球蛋白光的药物组合物 链激酶,蛋白激酶C或肿瘤细胞增殖,以及在温血动物如人中产生抗高血压作用和抗炎作用。