Aromatic and heterocyclic carboxamide derivatives as...

C - Chemistry – Metallurgy – 07 – D

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167/208, 260/309

C07D 277/82 (2006.01) A61K 31/425 (2006.01) C07D 417/12 (2006.01)

Patent

CA 1328871

ABSTRACT OF THE DISCLOSURE Acyl derivatives of 2-aminobenzothiazole and alkylated analogs of the formula: Image ---I ---II ---III or Image ---IV (wherein X is alkyl, hydrogen, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, nitro, trifluoromethyl, carbamyl, N,N-dialkylcarbamyl, phenyl, fluorophenyl, methoxy- phenyl, hydroxyphenyl, cyano, cyclohexyl or hydroxy- alkyl; Y is hydrogen, alkyl, alkoxy, F or C1; W is hydrogen, alkoxy, cyano, F, C1 or Br; X and Y together may form a benzo or tetrahydro- benzo ring; Z is hydrogen, F, C1, Br or alkyl; R is a substituent of the formula: Image -(Q)-(CH2)pNR4R5 [where n is an integer of 0 to 2; m is an integer of 0 to 1; R3, R4 and R5 are each hydrgoen alkyl; Q is CH2, O, NR4 or S; p is an integer of 2 to 3; R4 and R5 together with the nitrogen may form a saturated heterocyclic] R1 is hydrogen or methyl; R2 is hydrogen, alkyl, nitro, cyano, trifluoromethyl, F, C1 or Br; and R6 is alkyl, alkoxycarbonylmethyl, with the proviso that in formula I, R is at the m- or p-position to the carbonyl and p is 2 or 3 when Q is O, NR4 or S) are use- ful as antitumor agents and anti-plasmin agents.

600370

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