Benzoxazina and benzotiazina derivatives as inhibitors of nitric oxide synthase

摘要

Refers to benzoxazina and benzotiazina Derivatives of formula I, where X is s or, som(chr9); r1 is - - - - nr7 nr8 B; R2 is H or R1 and R2 together form a monociclico bicyclic or 5 to 8 members replaced with - (R nr7 ch2r9) - - - - nr8 B; R3 is H, NO2, CN, CF3, NR9 - C (= NR10) - nhcsnr12r13, R11,Among others; R4 is H or acyl; R5 and R6 are h, cycloalkyl C3 - C7, phenyl, among others; R7 and R8 is H, alkyl of C1 - C6; is alquileno C1 - C6 - (CH2) P - Q - Q - (CH2); b is H (CH2) - U P; Q is cycloalkyl C3 - C7C6 C10 aryl, heteroaryl or C6 C10; C1 - C6 is H, alkyl, cycloalkyl indanilo bicicloalquilo C3 - C7, C7, C10,Among others, R8 and B with N form a Five Member heterocycle - 7; R7 and together with N form a Five Member heterocycle - 7; M is 0 - 2, N, r, P and q are 0 - 6; R9 and R10 are h,C1 - C6 alkyl; R11 is C1 - C6 alkyl CH3, NH2, NH - NH -, CN -, aryl C6 C10, among others; R12 and R13 C1 - C6 is H, alkyl, phenyl, among others.When X is o, R6 is Methyl, R2, R3, R4 and R5 are h; r1 is not 6 - ((4 - aminobencil) aminometilo), among others.A Preferred Compound is triclorhidrato 6 - ((3 - (aminomethyl) - benzyl aminomethyl) - 2 - amino - 2 - methyl - 1.4 - benzoxacina, among others. It also relates to a process for Preparation.Compound I is an inhibitor of nitric oxide synthase and may be useful for the treatment of Neurodegenerative Diseases