摘要:
The invention concerns compounds of formula (I),in which R is (i), (ii) or (iii); n is 0, 1 or 2; X means O or S; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have different meanings, or a cyclized tautomeric shape. The invention also concerns the (E) isomers and salts of these compounds which display endothelin receptor antagonistic properties. ##STR1##
摘要:
Novel compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, --A.dbd.B--C.dbd.D--, Ar and X have the meaning indicated in claim 1, and their salts show endothelin receptor-antagonistic properties.
摘要:
New diamino acid derivatives of the formula IX--Z--NH--CH(CH.sub.2 R.sup.1)--CH(NH.sub.2)--CH.sub.2 --CO--E--G--Y IwhereinX is H, R.sup.2 --O--C.sub.n H.sub.2n --CO--, R.sup.2 --C.sub.n H.sub.2n --O--CO--, R.sup.2 --C.sub.2n --CO--, R.sup.2 --SO.sub.2, (R.sup.2 --C.sub.n H.sub.2n)--L(R.sup.2 --C.sub.r H.sub.2r)--C.sub.t H.sub.2t --CO--, H--(NHCH.sub.2 CH.sub.2).sub.n --NH--CH.sub.2 CO-- or 9-fluorenyl--C.sub.n H.sub.2n --O--CO--,Z is 0 to 4 amino acid radicals, bonded to one another in a peptide-like manner, selected from the group consisting of Abu, Ada, Ala, Arg, Dab, Gly, His, Ile, Leu, tert.-Leu, Lys, Met, Nbg, Nle, N--Me--His, N--Me--Phe, Orn, Phe, Pro, Ser, Thr, Tic, Trp, Tyr and Val,R.sup.1 is H, A, cycloalkyl with 3-7 C atoms, Ar or C.sub.p H.sub.2p --W,E is absent or is Ala, Gly, Ile, Leu, tert.-Leu, Met, Ser, Thr or Val,G is absent or is His, Phe, Trp, Tyr or --NH--CH(CH.sub.2 R.sup.1)--CH(NH.sub.2)--CH.sub.2 CO--,Y is --O--C.sub.m H.sub.2m --R.sup.3, --NH--C.sub.m H.sub.2m --R.sup.3, --NH--C.sub.m H.sub.2m-1 (R.sup.3).sub.2 or NA.sub.2,R.sup.2 is A, cycloalkyl with 3-7 C atoms, benzyl or Ar,L is CH or N,R.sup.3 is H, A, cycloalkyl with 3-7 C atoms, Ar, pyridyl, imidazolyl, piperidyl, N-benzyl-piperidyl or piperazinyl,W is OH, NH.sub.2, OA, NHA or NA.sub.2,A is alkyl with 1-6 C atoms,Ar is unsubstituted phenyl, phenyl which is mono- or poly-substituted by A, AO, F, Cl, Br, I, CF.sub.3 and/or NH.sub.2, or unsubstituted naphthyl andm, n, p, r and t are each 0, 1, 2, 3, 4 or 5, and salts thereof,inhibit the activity of human plasma renin.
摘要翻译:式I XZ-NH-CH(CH 2 R 1)-CH(NH 2)-CH 2 -CO-EGY I的新二氨基酸衍生物其中X是H,R 2 -O-C n H 2n-CO-,R 2 -C n H 2n-O-CO- ,R2-C2n-CO-,R2-SO2,(R2-CnH2n)-L(R2-CrH2r)-CtH2t-CO-,H-(NHCH2CH2)n-NH-CH2CO-或9-芴基-CnH2n- CO-,Z为0至4个氨基酸基团,以肽样方式彼此键合,选自Abu,Ada,Ala,Arg,Dab,Gly,His,Ile,Leu, Leu,Lys,Met,Nbg,Nle,N-Me-His,N-Me-Phe,Orn,Phe,Pro,Ser,Thr,Tic,Trp,Tyr和Val,R1是H,A, 7个C原子,Ar或CpH2p-W,E不存在或不是Ala,Gly,Ile,Leu,叔Leu,Met,Ser,Thr或Val,G不存在或者是His,Phe,Trp,Tyr或 - NH-CH(CH2R1)-CH(NH2)-CH2CO-,Y是-O-CmH2m-R3,-NH-CmH2m-R3,-NH-CmH2m-1(R3)2或NA2,R2是A, 3-7个C原子,苄基或Ar,L是CH或N,R3是H,A,具有3-7个C原子的环烷基,Ar,吡啶基,咪唑基,哌啶基,N-苄基 - 哌啶基或哌嗪基,W是OH, NH 2,OA,NHA或NA 2,A为具有1-6个C原子的烷基,Ar为 未取代的苯基,被A,AO,F,Cl,Br,I,CF 3和/或NH 2或未取代的萘基单取代或多取代的苯基,m,n,p,r和t分别为0,1,2, 2,3,4或5及其盐抑制人血浆肾素的活性。
摘要:
New diamino acid derivatives of the formula IX--Z--NH--CH(CH.sub.2 R.sup.1)--CH(NH.sub.2)--CH.sub.2 --CO--E--G--Y IwhereinX is H, R.sup.2 --O--C.sub.n H.sub.2n --CO--, R.sup.2 --C.sub.n H.sub.2n --O--CO--, R.sup.2 --C.sub.n H.sub.2n --CO--, R.sup.2 --SO.sub.2, (R.sup.2 --C.sub.n H.sub.2n)--L(R.sup.2 --C.sub.r H.sub.2r)--C.sub.t H.sub.2t --CO--, H--(NHCH.sub.2 CH.sub.2).sub.n --NH--CH.sub.2 CO-- or 9-fluorenyl--C.sub.n H.sub.2n --O--CO--,Z is 0 to 4 amino acid radicals, bonded to one another in a peptide-like manner, selected from the group consisting of Abu, Ada, Ala, Arg, Dab, Gly, His, Ile, Leu, tert.-Leu, Lys, Met, Nbg, Nle, N-Me-His, N-Me-Phe, Orn, Phe, Pro, Ser, Thr, Tic, Trp, Tyr and Val,R.sup.1 is H, A, cycloalkyl with 3-7 C atoms, Ar or C.sub.p H.sub.2p --W,E is absent or is Ala, Gly, Ile, Leu, tert.-Leu, Met, Ser, Thr or Val,G is absent or is His, Phe, Trp, Tyr or --NH--CH(CH.sub.2 R.sup.1)--CH(NH.sub.2)--CH.sub.2 CO--,Y is --O--C.sub.m H.sub.2m --R.sup.3, --NH--C.sub.m H.sub.2m --R.sup.3, --NH--C.sub.m H.sub.2m-1 (R.sup.3).sub.2 or NA.sub.2,R.sup.2 is A, cycloalkyl with 3-7 C atoms, benzyl or Ar,L is CH or N,R.sup.3 is H, A, cycloalkyl with 3-7 C atoms, Ar, pyridyl, imidazolyl, piperidyl, N-benzyl-piperidyl or piperazinyl,W is OH, NH.sub.2, OA, NHA or NA.sub.2,A is alkyl with 1-6 C atoms,Ar is unsubstituted phenyl, phenyl which is mono- or polysubstituted by A, AO, F, Cl, Br, I, CF.sub.3 and/or NH.sub.2, or unsubstituted naphthyl andm, n, p, r and t are each 0, 1, 2, 3, 4 or 5, and salts thereof,inhibit the activity of human plasma renin.
摘要翻译:式I XZ-NH-CH(CH 2 R 1)-CH(NH 2)-CH 2 -CO-EGY I的新二氨基酸衍生物其中X是H,R 2 -O-C n H 2n-CO-,R 2 -C n H 2n-O-CO- ,R2-CnH2n-CO-,R2-SO2,(R2-CnH2n)-L(R2-CrH2r)-CtH2t-CO-,H-(NHCH2CH2)n-NH-CH2CO-或9-芴基-CnH2n- CO-,Z为0至4个氨基酸基团,以肽样方式彼此键合,选自Abu,Ada,Ala,Arg,Dab,Gly,His,Ile,Leu, Leu,Lys,Met,Nbg,Nle,N-Me-His,N-Me-Phe,Orn,Phe,Pro,Ser,Thr,Tic,Trp,Tyr和Val,R1是H,A, 7个C原子,Ar或CpH2p-W,E不存在或不是Ala,Gly,Ile,Leu,叔Leu,Met,Ser,Thr或Val,G不存在或者是His,Phe,Trp,Tyr或 - NH-CH(CH2R1)-CH(NH2)-CH2CO-,Y是-O-CmH2m-R3,-NH-CmH2m-R3,-NH-CmH2m-1(R3)2或NA2,R2是A, 3-7个C原子,苄基或Ar,L是CH或N,R3是H,A,具有3-7个C原子的环烷基,Ar,吡啶基,咪唑基,哌啶基,N-苄基 - 哌啶基或哌嗪基,W是OH, NH 2,OA,NHA或NA 2,A是具有1-6个C原子的烷基,Ar i 未取代的苯基,被A,AO,F,Cl,Br,I,CF 3和/或NH 2或未取代的萘基单取代或多取代的苯基,m,n,p,r和t分别为0,1,2 ,3,4或5及其盐抑制人血浆肾素的活性。