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HETEROCYCLIC NITRIED COMPOUNDS AS ANTOTHELINE RECEPTOR ANTAGONISTS

机译:杂环硝化化合物作为对位受体拮抗剂

摘要

1. The compound of General formula (I), or its pharmaceutically acceptable salt, or its stereoisomer! ! where m, m 'and m' 'are 0 or 1; ! n, n 'and n' 'are 0 or 1; ! s, s' and s' 'are 0 or 1; ! And selected from the group consisting of:! ! ! ! ! !! ! ! ! ! ! ! ! ! ! ! ! ! ! ! ! where N1 is —O—, —OH; ! N2 is —N—, —NH—; ! N3 is —C (O) O—, —C (O) NH—; ! B, B 'and B' 'are —CO—, —C (O) O—, —C (O) NH—; ! C, C 'and C' 'are! ,,; ! provided that ! 1) if A is selected from the group consisting of:! (Ia), (Ib), (Ic), (Ie), (If), (Ig), (Ih), (Ii), (Ij), (Ik), (Il) and (Im), then, at least one of m, m ′, m ″, n, n ′ or n ″ is 1; ! 2) if A is selected from the group consisting of:! (In), (Io), (Ip), (Iq), (Ir), (Is) and (Iu), then s', s' 'and m are 0; whereas n is 0 or 1; ! 3) if A is (It), then m, m 'and s'' are 0; whereas n and n 'are 0 or 1; ! 4) at least one of N1 or N2 is a group -O- or -N- capable of linking at least one of the groups - [(B) m- (C) n- (Y-ONO2)], - [(B ') m' - (C ') n' - (Y'-ONO2)] or - [(B '') m '' - (C '') n '' - (Y '' - ONO2) ]; ! Y, Y 'and Y' 'are a bivalent radical having the following properties:! a)! linear or branched C1-C20 alkylene, optionally substituted with one or more substituents selected from the group consisting of: halogen atoms, hydroxy, -ONO2 or Ta, where Ta is! -OC (O) (C1-C10 alkyl) -ONO2 or -O (C1-C10 alkyl) -ONO2; ! cycloalkene from 5 to 7 carbon atoms in the cycloalkene ring, the ring being possibly substituted with a side chain T, where T is a linear or branched alkyl of 1 to 10 carbon atoms; ! b)! ! c)! ! where n0 is an integer from 0 to 20, and n1 is an integer from 1 to 20; ! d)! ! where n1 is as defined above, and n2 is an integer from 0 to 2; X1 = —OCO— or —COO— and R2 is H or CH3; ! e)! ! where n1, n2, R2 and X1 are such as op
机译:1.通式(I)的化合物或其药学上可接受的盐或立体异构体! !其中m,m和m为0或1; ! n,n'和n''为0或1; ! s,s'和s''为0或1; !并从以下组中选择: ! ! ! ! !! ! ! ! ! ! ! ! ! ! ! ! ! ! ! !其中N1为-O-,-OH; ! N 2为-N-,-NH-; ! N3为-C(O)O-,-C(O)NH-; ! B,B'和B''为-CO-,-C(O)O-,-C(O)NH-; ! C,C'和C''是! ,,; !提供那个! 1)如果从包括以下项的组中选择A: (Ia),(Ib),(Ic),(Ie),(If),(Ig),(Ih),(Ii),(Ij),(Ik),(Il)和(Im),然后, m,m',m'',n,n'或n''中的至少一个是1; ! 2)如果从包括以下项的组中选择A: (In),(Io),(Ip),(Iq),(Ir),(Is)和(Iu),则s',s'和m为0而n为0或1; ! 3)如果A是(It),则m,m'和s''为0;而n和n'为0或1; ! 4)N1或N2中的至少一个是-O-或-N-基团,能够连接基团-[[(B)m-(C)n-(Y-ONO2)],-[[ B')m'-(C')n'-(Y'-ONO2)]或-[[B)m''-(C))n''-(Y''-ONO2)]; ! Y,Y'和Y''是具有以下特性的二价基团:一种)!直链或支链的C 1 -C 20亚烷基,其任选地被一个或多个选自以下的取代基取代:卤素原子,羟基,-ONO 2或Ta,其中Ta为! -OC(O)(C1-C10烷基)-ONO2或-O(C1-C10烷基)-ONO2; !环烯烃环中具有5至7个碳原子的环烯烃,该环可能被侧链T取代,其中T是具有1至10个碳原子的直链或支链烷基; ! b)! ! C)! !其中n0是0至20的整数,n1是1至20的整数; ! d)! !其中n1如上定义,n2为0到2的整数; X1 = -OCO-或-COO-,R2为H或CH3; ! e)! !其中n1,n2,R2和X1如op

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