New 1,3,4-benzotriazepin-5(4H)-one derivs.

摘要

Racemic or optically active 1,3,4-benzotriazepin-5(4H)-one derivs. of formula (I) and their mixts., tautomers and salts, are new. In (I) (A) R1 is H, or 1-4C alkyl (opt. mono substd. by pyridyl or phenyl (itself opt. substd. by halo or alkoxy); R2 is cyanoamino; R3 is H or 1-4C alkyl (opt. mono substd. by halo, R5O,R6R7N or pyridyl phenyl (themselves opt. more substd. by halo or alkoxy); R5 is H, pyridylcarbonyl or phenylcarbonyl (opt. monosubstd. by halo or substd. by one or more alkoxy); R6,R7 is H or 1-4C alkyl; or NR6R7 is a 5-7 membered heterocycle gp. opt. contg. an O atom or an NR8 gp.; R8 is H, 1-4C alkyl, or phenyl (opt. monosubstd. by halo or alkoxy); R4 is 1-4C alkyl. The dotted line is absent; or (B) The dotted line represents a bond; R1 is absent; R2 is NR9R10; R3 is H, pyridyl or 1-4C alkyl (opt. monosubstd. by OR14, NR15R16 or a pyridyl or phenyl gp. (themselves opt. monosubstd. by halo or alkoxy)); R4 is 1-4C alkyl; R9, R10 is H, phenyl or 1-10C alkyl (opt. mono substd. by pyridyl or phenyl (themselves opt. monosubstd. by halo or alkoxy)); or NR9R10 is N=C(NR12R13)NH2, or a 5-7 membered heterocyclic gp. opt. contg. an O atom or NR" gp.; R" is H, 1-4C alkyl, or phenyl (opt. monosubstd. by alkoxy or halo); R12, R13 is H, or 1-10C alkyl (opt. monosubstd. by pyridyl); or NR12R13 is a 5-7 membered heterocyclic gp. opt. contg. an O atom or NR" gp.; R14 is pyridylcarbonyl or phenylcarbonyl opt. substd. by alkoxy; R15,R16 is H or 1-4C alkyl; or NR15R16 is a 5-7 membered heterocyclic gp. opt. contg. an O atom or NR17 gp.; and R17 is H, 1-4C alkyl or phenyl (opt. monosubstd. by halo or alkoxy) provided that R9 and R10 may not both be H.