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Novel cyclic compound having cycloalkylene chain, process for producing the same, and pharmaceutical composition containing the same

机译:具有亚环烷基链的新型环状化合物,其制备方法以及含有该化合物的药物组合物

摘要

Cycloalkene substituted cyclic derivatives (I) are new. Cycloalkene substituted cyclic derivatives of formula (I), their enantiomers, diastereoisomers and their acid or base addition salts are new. A = a group of formula (i) or (ii) (optionally substituted by Ra, ORa, OH, CORa, formyl, COORa, COOH or OCORa; Ra = 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 1-6C polyhaloalkyl, 3-8C cycloalkyl, 3-8C cycloalkyl-(1-6C) alkyl, 3-8C cycloalkenyl, 3-8C cycloalkenyl-(1-6C) alkyl (all optionally substituted with at least one OH, 1-6C alkoxy, 1-6C alkyl, 1-6C polyhaloalkyl, amino or halo), aryl, aryl-(1-6C) alkyl, heteroaryl or heteroaryl-(1-6C) alkyl; X, Y' = O, S or CH2; D' = benzene or naphthalene; a-d = single or double bond; Z = O, S, CH2 or NR1; R1 = H, 1-6C alkyl, aryl or aryl-(1-6C) alkyl; D'' = benzene or pyridine; R = H, halo, OH, SH, Ra, ORa, S(O)nRa or a (un)saturated 5- to 7-membered ring of formula (iii) (optionally substituted with at least one 1-6C alkyl, 1-6C alkoxy, carboxy, 1-6C alkoxycarbonyl, OH or =O); n = 0-2; E = O or -S(O)n-; G1, G2 = single bond, -(CH2)t- (optionally substituted with at least one OH, COOH, formyl, Ra, ORa, COORa, CORa or halo; p, q = 0-4; p + q = 1-4; B' = -NR1aC(Q)R2a, -NR1aC(Q)NR2aR3a or -C(Q)NR1aR2a; R1a-R3a = H or Ra; Q = O or S; aryl = phenyl, naphthyl, biphenyl (all optionally substituted with at least one OH, 1-6C alkoxy, 1-6C alkyl, 1-6C polyhaloalkyl, CN, COOH, 1-6C alkoxycarbonyl, NO2, amino or halo); heteroaryl = 5- to 10-membered mono- or polycyclic aromatic ring containing 1-3 N, O or S (optionally substituted with at least one OH, 1-6C alkoxy, 1-6C alkyl, 1-6C polyhaloalkyl, CN, COOH, 1-6C alkoxycarbonyl, NO2, amino or halo); and provided that q = 0 and p = 4, or q = 4 and p = 0 do not apply, when A is naphthyl (optionally substituted with methoxy or methyl), G1 and G2 are single bonds and B' is a group of formula (iv) or NHCOCH3; that A is other than halo substituted naphthyl, when G1 is a single bond and p + q is 1; B' is other than urea, when A is indolyl substituted on position 2 with a group of formula (v); and that B' is other than CONH-aryl, when A is indolyl substituted on position 2 with carboxyl or alkoxycarbonyl, p is 1, q is 0 (p is 0 and q is 1) and G1 is single bond. A Independent claim is also included for the preparation of (I).
机译:环烯烃取代的环状衍生物(I)是新的。式(I)的环烯烃取代的环状衍生物,其对映异构体,非对映异构体及其酸或碱加成盐是新的。 A =式(i)或(ii)的基团(可选地被Ra,ORa,OH,CORa,甲酰基,COORa,COOH或OCORa取代; Ra = 1-6C烷基,2-6C烯基,2-6C炔基, 1-6C聚卤代烷基,3-8C环烷基,3-8C环烷基-(1-6C)烷基,3-8C环烯基,3-8C环烯基-(1-6C)烷基(均可选地被至少一个OH,1- 6C烷氧基,1-6C烷基,1-6C多卤代烷基,氨基或卤素),芳基,芳基-(1-6C)烷基,杂芳基或杂芳基-(1-6C)烷基; X,Y'= O,S或CH2 ; D'=苯或萘; ad =单键或双键; Z = O,S,CH 2或NR 1; R 1 = H,1-6C烷基,芳基或芳基-(1-6C)烷基; D” =苯或吡啶; R = H,卤素,OH,SH,Ra,ORa,S(O)n Ra或式(iii)的(不饱和)5至7元环(任选地被取代为:至少一个1-6C烷基,1-6C烷氧基,羧基,1-6C烷氧基羰基,OH或= O); n = 0-2; E = O或-S(O)n-; G1,G2 =单键,-(CH2)t-(可选地被至少一个OH,COOH,甲酰基,Ra,ORa,COORa,CORa或卤素取代; p,q = 0-4; p + q = 1 -4; B'= -NR 1 aC(Q)R 2 a,-NR 1aC(Q)NR 2 aR 3a或-C(Q)NR 1 aR 2一种; R 1 a -R 3 a = H或Ra; Q = O或S;芳基=苯基,萘基,联苯(全部任选地被至少一个OH,1-6C烷氧基,1-6C烷基,1-6C多卤代烷基,CN,COOH,1-6C烷氧基羰基,NO 2,氨基或卤素取代);杂芳基=含有1-3个N,O或S的5至10元单环或多环芳香环(可选地被至少一个OH,1-6C烷氧基,1-6C烷基,1-6C多卤代烷基,CN,COOH取代,1-6C烷氧羰基,NO2,氨基或卤素);并假设q = 0和p = 4或q = 4和p = 0不适用,则当A为萘基(可选被甲氧基或甲基取代)时,G1和G2为单键,B'为下式的基团(iv)或NHCOCH3;当G1为单键且p + q为1时,A不是卤素取代的萘基;当A是在位置2上被式(v)基团取代的吲哚基时,B′不是脲。并且B′不是CONH-芳基,当A为在2位上被羧基或烷氧羰基取代的吲哚基时,p为1,q为0(p为0,q为1),G1为单键。准备(I)也包括独立权利要求。

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