Poly:prenyl-carboxamide derivs. and analogues

摘要

Cpds. (I) and their salts are new. In A,B,Y and Z are all H or (1) A and B and/or (2) Y and Z together form a double bond(s); W is COR or a gp. X; n is 0-4 when W is COR or 1-3 when W is gp.X; R is NR1-(CH2)mOH, N((CH2)kOH)(CH2)lOH , NHCH2-COOR2, NH(CH2)p-NR3R4, NH(CH2)q-NR5R6R7(+)Hal(-), or N'-(1-6C)alkyl-N-piperazino or -homopiperazino (and corresp. N'-quat.salts with a (1-6C) alkyl halide), D-substd.-N-piperidino, NR16(CH2)wSH, NH(CH2)x-N-R17-3-piperidinyl or NH(CH2)y-N-R18-2-pyrrolidinyl; D is (CH2)tOH, (CH2)u-NR11R12 or (CH2)v-NR13R14R15(+) Hal(-); R1, R3-R7, R11, R12, R16-R18 are H or 1-6C alkyl; R2 is H, 1-6C alkyl or aryl; R13-R15 are 1-6C alkyl; m, k, l, q, w and y are 1-5; p, t, u, v and x are 0-5; X is R21-substd. p-COR22-phenyl, a gp. of formula (II), 4- or 5-COR22-1-naphthyl, 4-COR22-5,6,7,8-tetrahydro-1-naphthyl, N-R30-2-piperidinyl-(CH2)a-CONH, N-R31-2-pyrrolidinyl-(CH2)b-CONH, N-morpholinyl-(CH2)c-CONH, R32R33N-(CH2)d-CONH, 3-pyridinylaminocarbonyl, R34C(CH2OH)2-CONH, 1-imidazolylcarbonyl, CONH-CH2CH(OH)CH2OH, a gp. of formula (III), CH2NHCO(CH2)gNR39R40 or CH2NH(CH2)hNR41R32; K and L are both H or together form a bond; R22 is NR23-(CH2)mOH, N((CH2)lOH)(CH2)lOH)), NH(CH2)pNR24R25 or a gp. of formula (IV); a-d are 0-5; e-j are 1-5; R23-25 and R35-42 are H or 1-6C alkyl; R26-34 are 1-6C alkyl; and R21 is H, 1-6C alkyl or halogen. (0/0) EPAB- EP-110397 B Cpds (I) and their salts are new. In A, B, Y and Z are all H or (1) A and B and/or (2) Y and Z together form a double bond(s); W is COR or a gp. X; n is 0-4 when W is COR or 1-3 when W is gp. X; R is - NR1-(CH2)mOH, N((CH2)kOH)(CH2)lOH, NHCH2-COOR2, NH(CH2)p-NR3R4, NH(CH2)q-NR5R6R7 (+) Hal(-), or N'-(1-6C)alkyl-N-piperazino or -homopiperazino (and correp N'-qat. salts with a (1-6C) alkyl halide), D-susbtd.-N-piperidino, NR16(CH2)wSH, NH(CH2)x-N-R17-3-piperidinyl or NH(CH2)y-N-R18-2-pyrrolidinyl; D is (CH2)tOH, (CH2)u-NR11R12 or (CH2v-NR13R14R15(+) Hal(-); R1, R3-R7, R11, R12, R16-R18 are H or 1-6C alkyl; R2 is H, 1-6C alkyl or aryl; R13-R15 are 1-6C alkyl; m, k, l, q, w and y are 1-5; p, t, u, v and x are 0-5; X is R21-substd. p-COR22-phenyl, a gp. of formula (II), 4- or 5-COR22-1-naphthyl, 4-COR22-5,6,7,8-tetrahydro-1-naphthyl, N-R30-2-piperidinyl-(CH2)a-CO NH, N-R31-2-pyrrolidinyl-(CH2)b-CONH, N-morpholinyl-(CH2)c-CONH, R32R33N-(CH2)d-CONH, 3-pyridinylaminocarbonyl, R34C(CH2OH)2-CONH, 1-imidazolylcarbonyl, CONH-CH2CH(OH)CH2OH, a gp of formula (III), CH2NHCO(CH2)gNR39R40 or CH2NH(CH2)hNR41R43; K and L are both H or together form a bond; R22 is NR23-(CH2)mOH, N((CH2)1OH)(CH2)1OH)), NH(CH2)pNR24R25 or a gp of formula (IV); a-d are 0-5; e-j are 1-5; R23-R25 and R35-42 are H or 1-6C alkyl; R26-34 are1-6C alkyl; and R21 is H, 1-6C alkyl or halogen. (50pp) USAB- US4742058 A Polyprenyl carboxylic acid amide of formula (I) and salts are new. In (I), A, B, Y and Z are each H or pairs A and B and/ or Y and Z form double bonds; n is 1-3; X is (Ia) where R22 is (Ib) and R23 is H, or 1-6C lakyl; m is 1-5; or more complex gps; R21 is H, 1-6C alkyl, halo: or (Ia) is other substd mono- or bi-cyclic aryl. - (I) may be prod e.g. by reacting polyprenyl carboxylic acid (II) or its reactive deriv. with amine R22H.