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Pharmaceuticals Containing Other Organic And Inorganic Compounds
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Claims (20)
85 PATENTNI ZAHTEVKI 1. Spojine s splošno formulo ,4 1 1 I R—N C O CH R (°) R7T>R •CH2—Nv R 19 8 v kateri n predstavlja število 0 ali 1; Rl predstavlja alkoksikarbonil, aralkoksikarbonil, alkanoil, cikloalkilkarbonil, aralkanoil, aroil, heterociklil-karbonil, alkilsulfonil, arilsulfonil, monoaralkilkarbamoil, cinamoil ali a-aralkoksikarbonil-aminoalkanoil in predstavlja vodik, ali R^ in R7 skupaj z atomom dušika na katerega sta vezana, predstavljata ciklično imidno skupino s formulo OA compound of the general formula, 4 1 1 I R — N C O CH R (°) R7T > R • CH2 — Nv R 19 8 in which n represents the number 0 or 1; R1 represents alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, cycloalkylcarbonyl, aralkanoyl, aroyl, heterocyclylcarbonyl, alkylsulfonyl, arylsulfonyl, monoaralkylcarbamoyl, cinamoyl or α-aralkoxycarbonyl-aminoalkanoyl, together with R and represents a hydrogen and R a cyclic imide group of formula OP^ N— / (a) O v kateri P in Q skupaj predstavljata aromatski sistem; R^ predstavlja alkil, cikloalkil, aril, aralkil, heterociklilalkil, cianoalkil, alkilsulfinilalkil, karbamoilalkil ali alkoksikarbonilalkil, ali kadar n predstavlja število 0, lahko R-* predstavlja alkiltioalkil, ali kadar n označuje število 1, lahko R^ prav tako predstavlja alkilsulfonilalkil; R^ predstavlja alkil, cikloalkil, cikloalkilalkil, aril ali aralkil; R^ predstavlja vodik in R6 predstavlja hidroksi, ali R-^ in R^ skupaj predstavljata okso; R7 in R8 skupaj predstavljata trimetilensko ali tetrametilensko skupino, katera je lahko substituirana s hidroksi, alkoksikarbonilamino ali acilamino, ali v kateri je ena od skupin -CH2- zamenjana z -NH-, -N(alkoksikarbonil)-, -N(acil)- ali -S-, ali katera nosi kondenziran cikloalkan, aromatski ali heteroaromatski obroč; in R^ predstavlja alkoksikarbonil, monoalkilkarbamoil, monoaralkilkarbamoil, monoarilkarbamoil ali skupino s formulo 86P ^ N— / (a) O in which P and Q together represent an aromatic system; R 1 represents alkyl, cycloalkyl, aryl, aralkyl, heterocyclylalkyl, cyanoalkyl, alkylsulfinylalkyl, carbamoylalkyl or alkoxycarbonylalkyl, or when n represents the number 0, R 1 represents alkylthioalkyl, or when n represents the number 1, R 1 may also represent alkyl; R 1 represents alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; R 1 represents hydrogen and R 6 represents hydroxy, or R 1 and R 6 together represent oxo; R7 and R8 together represent a trimethylene or tetramethylene group which may be substituted by hydroxy, alkoxycarbonylamino or acylamino, or in which one of the groups -CH2- is replaced by -NH-, -N (alkoxycarbonyl) -, -N (acyl) - or -S-, or which carries a fused cycloalkane, aromatic or heteroaromatic ring; and R 1 represents alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of formula 86v kateri R.10 in vsak posebej predstavlja alkil; in njihove farmacevtsko sprejemljive kislinske adicijske soli.wherein R 10 and each independently represents alkyl; and pharmaceutically acceptable acid addition salts thereof.2. Spojine po zahtevku 1, v katerih n označuje 0 (nič), predstavlja alkil, cikloalkil, aril, aralkil, heterociklilalkil, cianoalkil, alkiltioalkil, karbamoilalkil ali alkoksikarbonilalkil in in R^ skupaj predstavljata trimetilensko ali tetrametilensko skupino, v kateri je ena od skupin -CH2- zamenjana z -NH-, ali -S-, ali katera lahko nosi kondenzirani cikloalkanski, aromatski ali heteroaromatski obroč.Compounds according to claim 1, wherein n denotes 0 (zero), represents alkyl, cycloalkyl, aryl, aralkyl, heterocyclylalkyl, cyanoalkyl, alkylthioalkyl, carbamoylalkyl or alkoxycarbonylalkyl, and and R 1 together represent a trimethylene or tetramethylene group in which is one; groups -CH2- replaced by -NH-, or -S-, or which may carry a fused cycloalkane, aromatic or heteroaromatic ring.3. Spojine po zahtevku 1 ali 2, v katerih R^ predstavlja alkoksikarbonil, aralkoksikarbonil, alkanoil, cikloalkilkarbonil, aralkanoil, aroil, heterociklil-karbonil ali α-aralkoksikarbonilaminoalkanoil, prednostno benziloksikarbonil, 2-naftoil, 1-hidroksi-2-naftoil, 3-hidroksi-2-naftoil, 3-benziloksi-2-naftoil, 2-kinolilkarbonil ali 3-kinolilkarbonil in R^ predstavlja vodik.Compounds according to claim 1 or 2, wherein R 1 represents alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, cycloalkylcarbonyl, aralkanoyl, aroyl, heterocyclylcarbonyl or α-aralkoxycarbonylaminoalkanoyl, preferably benzyloxycarbonyl, 2-naphthoyl -hydroxy-2-naphthoyl, 3-benzyloxy-2-naphthoyl, 2-quinolylcarbonyl or 3-quinolylcarbonyl and R 1 represents hydrogen.4. Spojine po kateremkoli od zahtevkov od 1 do 3, v katerih R^ predstavlja alkil, cianolakil, alikiltioalkil ali karbamoilalkil, prednostno cianometil, metiltiometil ali karbamoilmetil.Compounds according to any one of claims 1 to 3, wherein R 1 represents alkyl, cyanolakyl, alkylthioalkyl or carbamoylalkyl, preferably cyanomethyl, methylthiomethyl or carbamoylmethyl.5. Spojine po kateremkoli od zahtevkov 1 do 4, v katerih R^ predstavlja aralkil, prednostno benzil.Compounds according to any one of claims 1 to 4, in which R 1 represents aralkyl, preferably benzyl.6. Spojine po kateremkoli izmed zahtevkov 1 do 5, v katerih R^ predstavlja vodik in predstavlja hidroksi.Compounds according to any one of claims 1 to 5, wherein R 1 represents hydrogen and represents hydroxy.7. Spojine po kateremkoli od zahtevkov 1 do 6, v katerih -N(R7)-CH(R8)(r9) predstavlja eno od naslednjih skupin 12 87 RCompounds according to any one of claims 1 to 6, wherein -N (R 7) -CH (R 8) (r 9) represents one of the following groups 12 87 RR 9 /' N \ / 9 \ N—R 13 / (c) (d) I9 N. (e)R 9 / 'N \ / 9 \ N — R 13 / (c) (d) I9 N. (e)/ \ ,// \, /N. R (h) 9N. R (h) 9II( i) 88 kjer ima pomen, ki je naveden v zahtevku 1, R.12 predstavlja vodik, hidroksi, alkoksikarbonilamino ali acilamino, R.13 predstavlja vodik, alkoksikarbonil ali acil, m označuje 1 ali 2 in p označuje 1 ali 2, prednostno skupino s formulo (c), v kateri R.12 predstavlja vodik in m označuje 2, ali predstavlja terc.-butoksikarbonilamino in m označuje 1, skupino s formulo (d), v kateri R^ predstavlja terc.-butoksikarbonil, skupino s formulo (e), v kateri m označuje 1, skupino s formulo (f), v kateri m in p oba označujeta 1, ali skupino s formulo (g), (i) ali (j).(i) 88 wherein the meaning given in claim 1, R.12 represents hydrogen, hydroxy, alkoxycarbonylamino or acylamino, R.13 represents hydrogen, alkoxycarbonyl or acyl, m denotes 1 or 2 and p denotes 1 or 2, preferably a group of formula (c) in which R 12 represents hydrogen and m represents 2, or represents tert-butoxycarbonylamino and m represents 1, a group of formula (d) in which R 1 represents tert-butoxycarbonyl, a group of formula (e) wherein m denotes 1, a group of formula (f) wherein m and p both denote 1, or a group of formula (g), (i) or (j).8. Spojine po kateremkoli izmed zahtevkov od 1 do 7, v katerih R^ predstavlja alkoksikarbonil, monoalkilkarbamoil ali skupino s formulo (b), navedeno v zahtevku 1, prednostno terc.-butoksikarbonil, izobutilkarbamoil, terc.-butilkarbamoil ali skupino s formulo (b), navedeno v zahtevku 1, kjer RlO predstavlja sek.-butil in Ril predstavlja izobutil.Compounds according to any one of claims 1 to 7, wherein R 1 represents alkoxycarbonyl, monoalkylcarbamoyl or a group of formula (b), as claimed in claim 1, preferably tert-butoxycarbonyl, isobutylcarbamoyl, tert-butylcarbamoyl or a group of formula ( b), claimed in claim 1, wherein R 10 represents sec-butyl and R 1 represents isobutyl.9. Spojine po kateremkoli izmed zahtevkov od 1 do 8, v katerih Rl predstavlja benziloksikarbonil, 2-naftoil, l-hidroksi-2-naftoil, 3-hidroksi-2-naftoil, 3-benziloksi-2-naftoil, 2-kinolilkarboni! ali 3-kinolilkarbonil in R^ predstavlja vodik, R^ predstavlja cianometil, metiltiometil ali karbamoilmetil, R^ predstavlja benzil, R^ predstavlja vodik in R^ predstavlja hidroksi, in -N(R7)-CH(R8)(R9) predstavlja skupino s formulo (c) navedeno v zahtevku 7, kjer Rl2 predstavlja vodik in m označuje 2, ali Rl2 predstavlja terc.-butoksikarbonilamino in m označuje 1, skupino s formulo (d), navedeno v zahtevku 7, kjer Rl3 predstavlja terc.-butoksikarbonil, skupino s formulo (e), dano v zahtevku 7, v kateri m označuje 1, skupino s formulo (f), prikazano v zahtevku 7, v kateri m in p označujeta 1, ali skupino s formulami (g), (i) ali (j), navedenmi v zahtevku 7, in R^ predstavlja terc.-butoksikarbonil, izobutilkarbamoil, terc.-butilkarbamoil, ali skupino s formulo (b), navedeno v zahtevku 1, v kateri RlO predstavlja sek.-butil in R^ predstavlja izobutil.Compounds according to any one of claims 1 to 8, wherein R 1 represents benzyloxycarbonyl, 2-naphthoyl, 1-hydroxy-2-naphthoyl, 3-hydroxy-2-naphthoyl, 3-benzyloxy-2-naphthoyl, 2-quinolylcarbonyl! or 3-quinolylcarbonyl and R 1 represents hydrogen, R 1 represents cyanomethyl, methylthiomethyl or carbamoylmethyl, R 1 represents benzyl, R 1 represents hydrogen and R 1 represents hydroxy, and -N (R 7) -CH (R 8) (R 9) represents a group of formula (c) according to claim 7, wherein R 12 represents hydrogen and m represents 2, or R 12 represents tert-butoxycarbonylamino and m represents 1, a group of formula (d), as claimed in claim 7, wherein R 13 represents tert-butoxycarbonyl , a group of formula (e) given in claim 7, in which m represents 1, a group of formula (f) shown in claim 7, in which m and p represent 1, or a group of formulas (g), (i) or (j) mentioned in claim 7, and R 1 represents tert-butoxycarbonyl, isobutylcarbamoyl, tert-butylcarbamoyl, or a group of formula (b), as claimed in claim 1, in which R 10 represents sec-butyl and R 1. represents isobutyl.10. N2-[3(S)-[[N-(benziloksikarbonil)-L-asparaginil]amino]-2(R ali S)-hidroksi-4-fenilbutil]-Nl-terc.-butiI-L-prolinamid ali N^-[3(S)-[[N-(benziloksikarbonil)-L-asparaginil]amino]-2(R ali S)-hidroksi-4-fenilbutil]-Nl-izobutil-L-prolinamid.10. N2- [3 (S) - [[N- (benzyloxycarbonyl) -L-asparaginyl] amino] -2 (R or S) -hydroxy-4-phenylbutyl] -N1-tert-butyl-L-prolinamide or N 1 - [3 (S) - [[N- (benzyloxycarbonyl) -L-asparaginyl] amino] -2 (R or S) -hydroxy-4-phenylbutyl] -N1-isobutyl-L-prolinamide.11. Spojine po zahtevku 1, izbrane iz skupine, ki jo sestavljajo: N^-[3(S)-[[N-(benziloksikarbonil)-L-asparaginil]amino]-2(R )-hidroksi-4-fenilbutil]-Nl-terc.-butil-4(R)-tiazolidin-karboksamid, N-terc.-butil-l-[2(R)-hidroksi-3(S)-[[N-(2-naftoil)-L-asparaginil]amino]-4-fenilbutil]- 2(S)-piperidinkarboksamid, 89 l-[3(S)-[[N-(benziloksikarbonil)-L-asparaginil]amino]-2-(R)-hidroksi-4-fenilbutil]-N- terc.-butil-oktahidro-(3aS,6aS)-ciklopenta[b]pirol-2(S)-karboksamid, 1- [3(S)-[[N-(benziloksikarbonil)-L-asparaginil]amino]-2-(R)-hidroksi-4-fenilbutil]-N-terc.-butil-2(S)-piperidin-karboksamid, 2- [3(S)-[[N-(benziloksikarbonil)-L-asparaginil]amino]-2-(R)-hidroksi-4-fenilbutil]-N-terc.-butil-l,2,3,4-tetrahidropirido[3,4-b]indol-l-karboksamid, N-terc.-butil-3-[2(R)-hidroksi-3(S)-[[N-(2-naftoil)-L-asparaginil]amino]-4-fenilbutil]- 4(R)-tiazolidinkarboksamid, Nl-terc.-butil-N2-[2(R)-hidroksi-4-fenil-3(S)-[[N-(2-kinolilkarbonil)-L-asparaginil]amino]-L-proIinamid N^-oksid, l-[3(S)-[[N-(benziloksikarbonil)-3-ciano-L-alanil]amino]-2-(R)-hidroksi-4-fenilbutil- N-terc.-butil-2(S)-piperidinkarboksamid, l-[3(S)-[[N-(benziloksikarbonil)-L-asparaginil]amino]-2(R)-hidroksi-4-fenilbutil]-4-(terc.-butoksikarbonil)-N-terc.-butiI-2-(R ali S)-piperazinkarboksamid, l-[3(S)-[[N-(benziloksikarbonil)-3-ciano-L-alanil]amino]-2-(R)-hidroksi-4-fenilbutil]-4-(terc.-butoksikarbonil)-N-terc.-butil-2(R ali S)-piperazinkarboksamid, N^-[3(S)-[[N-(benziloksikarbonil)-L-asparaginil]amino]-2-(R)-hidroksi-4-fenilbutil]-4(R)-(terc.-butoksiformamido)-Nl-terc.-butil-L-prolinamid, l-[3(S)-[[N-(3-benziloksi-2-naftoil)-L-asparaginil]amino]-2-(R)-hidroksi-4-fenilbutil]- N-(terc.-butil-2(S)-piperidin-karboksamid, N-terc.-butil-l-[2(R)-hidroksi-4-fenil-3(S)-[[N-(2-kinolilkarbonil)-L-asparaginil]amino]butil]-2-piperidinkarboksamid 1-oksid, N-terc.-butil-l-[3(S)-[[N-(3-hidroksi-2-naftoil)-L-asparaginil]amino]-2(R)-hidroksi-4- fenilbutil]-2(S)-piperidinkarboksamid, trans-2-[3(S)-[[N-benziloksikarbonil)-L-asparaginil]amino]-2-(R)-hidroksi-4- fenilbutil]-N-terc.-butil-dekahidro-(4aR,8aS)-izokinolin-3(S)-karboksamid, 4-(terc.-butoksikarbonil)-N-terc.-butil-l-[2(R)-hidroksi-4-fenil-3(S)-[[N-(2- kinolilkarbonil)-L-asparaginil]amino]butil]'2(R ali S)piperazinkarboksamid, N-terc.-butil-l-[2(R)-hidroksi-3(S)-[[N-(l-hidroksi-2-naftoil)-L-asparaginil]amino]-4- fenilbutil]-2(S)-piperidinkarboksamid, trans-N-terc.-butil-dekahidro-2-[2(R)-hidroksi-4-fenil-3(S)-[[N-(2-kinolilkarbonil)-L-asparaginil]amino]butil]-(4aR,8aS)-izokinolin-3(S)-karboksamid in N-terc.-butil-l-[2(R)-hidroksi-4-fenil-3(S)-[[N-(2-kinolilkarbonil)-L-cisteinil]amino]butil]-2(S)-piperidinkarboksamid. 90Compounds according to claim 1, selected from the group consisting of: N 2 - [3 (S) - [[N- (benzyloxycarbonyl) -L-asparaginyl] amino] -2 (R) -hydroxy-4-phenylbutyl] -N1-tert-butyl-4 (R) -thiazolidinecarboxamide, N-tert-butyl-1- [2 (R) -hydroxy-3 (S) - [[N- (2-naphthoyl) -L -asparaginyl] amino] -4-phenylbutyl] -2 (S) -piperidinecarboxamide, 89 1- [3 (S) - [[N- (benzyloxycarbonyl) -L-asparaginyl] amino] -2- (R) -hydroxy- 4-Phenylbutyl] -N-tert-butyl-octahydro- (3aS, 6aS) -cyclopenta [b] pyrrole-2 (S) -carboxamide, 1- [3 (S) - [[N- (benzyloxycarbonyl) -L -asparaginyl] amino] -2- (R) -hydroxy-4-phenylbutyl] -N-tert-butyl-2 (S) -piperidinecarboxamide, 2- [3 (S) - [[N- (benzyloxycarbonyl) -L-asparaginyl] amino] -2- (R) -hydroxy-4-phenylbutyl] -N-tert-butyl-1,2,3,4-tetrahydropyrido [3,4-b] indole-1-carboxamide, N-tert-butyl-3- [2 (R) -hydroxy-3 (S) - [[N- (2-naphthoyl) -L-asparaginyl] amino] -4-phenylbutyl] -4 (R) -thiazolidinecarboxamide , N1-tert-butyl-N2- [2 (R) -hydroxy-4-phenyl-3 (S) - [[N- (2-quinolylcarbonyl) -L-asparaginyl] amino] -L-pronynamide N 2 - oxide, 1- [3 (S) - [[N- (ben zyloxycarbonyl) -3-cyano-L-alanyl] amino] -2- (R) -hydroxy-4-phenylbutyl-N-tert-butyl-2 (S) -piperidinecarboxamide, 1- [3 (S) - [[ N- (benzyloxycarbonyl) -L-asparaginyl] amino] -2 (R) -hydroxy-4-phenylbutyl] -4- (tert-butoxycarbonyl) -N-tert-butyl-2- (R or S) -piperazinecarboxamide , 1- [3 (S) - [[N- (benzyloxycarbonyl) -3-cyano-L-alanyl] amino] -2- (R) -hydroxy-4-phenylbutyl] -4- (tert-butoxycarbonyl) - N-tert-butyl-2 (R or S) -piperazinecarboxamide, N, N- [3 (S) - [[N- (benzyloxycarbonyl) -L-asparaginyl] amino] -2- (R) -hydroxy-4- phenylbutyl] -4 (R) - (tert-butoxyformamido) -N1-tert-butyl-L-prolinamide, 1- [3 (S) - [[N- (3-benzyloxy-2-naphthoyl) -L- asparaginyl] amino] -2- (R) -hydroxy-4-phenylbutyl] -N- (tert-butyl-2 (S) -piperidinecarboxamide, N-tert-butyl-1- [2 (R) - hydroxy-4-phenyl-3 (S) - [[N- (2-quinolylcarbonyl) -L-asparaginyl] amino] butyl] -2-piperidinecarboxamide 1-oxide, N-tert-butyl-1- [3 ) - [[N- (3-hydroxy-2-naphthoyl) -L-asparaginyl] amino] -2 (R) -hydroxy-4-phenylbutyl] -2 (S) -piperidinecarboxamide, trans-2- [3 ) - [[N-benzyloxycarbonyl) -L -asparaginyl] amino] -2- (R) -hydroxy-4-phenylbutyl] -N-tert-butyl-decahydro- (4aR, 8aS) -isoquinoline-3 (S) -carboxamide, 4- (tert-butoxycarbonyl) ) -N-tert-butyl-1- [2 (R) -hydroxy-4-phenyl-3 (S) - [[N- (2-quinolylcarbonyl) -L-asparaginyl] amino] butyl] '2 (R or S) piperazinecarboxamide, N-tert-butyl-1- [2 (R) -hydroxy-3 (S) - [[N- (1-hydroxy-2-naphthoyl) -L-asparaginyl] amino] -4- phenylbutyl] -2 (S) -piperidinecarboxamide, trans-N-tert-butyl-decahydro-2- [2 (R) -hydroxy-4-phenyl-3 (S) - [[N- (2-quinolylcarbonyl) - L-asparaginyl] amino] butyl] - (4aR, 8aS) -isoquinoline-3 (S) -carboxamide and N-tert-butyl-1- [2 (R) -hydroxy-4-phenyl-3 (S) - [N- (2-quinolylcarbonyl) -L-cysteinyl] amino] butyl] -2 (S) -piperidinecarboxamide. 9012. N-terc.-butil-l-[2(R)-hidroksi-4-fenil-3(S)-[[N-(2-kinolilkarbonil)-L-asparaginil]amino]butil]-2(S)-piperidinkarboksamid.12. N-tert-butyl-1- [2 (R) -hydroxy-4-phenyl-3 (S) - [[N- (2-quinolylcarbonyl) -L-asparaginyl] amino] butyl] -2 (S ) -piperidinecarboxamide.13. N-terc.-butil-oktahidro-l-[2(R)-hidroksi-4-fenil-3(S)-[[N-(2-kinolilkarbonil)-L-asparaginil]amino]butil]-(3aS,6aS)-ciklopenta[b]pirol-2(S)-karboksamid.13. N-tert-butyl-octahydro-1- [2 (R) -hydroxy-4-phenyl-3 (S) - [[N- (2-quinolylcarbonyl) -L-asparaginyl] amino] butyl] - ( 3aS, 6aS) -cyclopenta [b] pyrrole-2 (S) -carboxamide.14. N-terc.-butil-l,2,3,4-tetrahidro-2-[2(R)-hidroksi-4-fenil-3(S)-[[N-(2-kinolil-karbonil)-L-asparaginil]amino]butil]pirido[3,4-b]indol-l(R ali S)-karboksamid.14. N-tert-butyl-1,2,3,4-tetrahydro-2- [2 (R) -hydroxy-4-phenyl-3 (S) - [[N- (2-quinolyl-carbonyl) - L-asparaginyl] amino] butyl] pyrido [3,4-b] indole-1 (R or S) -carboxamide.15. Spojine s splošno formulo R15. Compounds of general formula RR A R CH 5R A R CH 5R 8 v kateri R predstavlja vodik ali skupino CO CH .2 \ R^ predstavlja alkil, cikloalkil, aril, aralkil, heterociklilalkil, cianoalkil, alkiltioalkil, alkilsulfinilalkil, karbamoilalkil ali alkoksikarbonilalkil; R^ predstavlja alkil, cikloalkil, cikloalkilalkil, aril ali aralkil; R^ predstavlja vodik in R^ predstavlja hidroksi, ali R^ in R^ skupaj predstavljata okso; R^ in R^ skupaj predstavljata trimetilensko ali tetrametilensko skupino, katera je lahko substituirana s hidroksi, alkoksikarbonilamino ali acilamino, ali v kateri je ena od skupin -CH2- lahko zamenjana z -NH-, -N(alkoksikarbonil)-, N(acil)- ali -S-, ali katera nosi kondenziran cikloalkanski, aromatski ali heteroaromatski obroč; in R^ predstavlja alkoksikarbonil, monoalkilkarbamoil, mono-aralkilkarbamoil, monoarilkarbamoil ali skupino s formulo NH / —CO . /C°\ CH NH· ,11 (b) ; R 10 VI 91 v kateri vsak izmed R.10 in predstavlja alkil.R 8 in which R represents hydrogen or a CO group CH 2 R 2 represents alkyl, cycloalkyl, aryl, aralkyl, heterocyclylalkyl, cyanoalkyl, alkylthioalkyl, alkylsulfinylalkyl, carbamoylalkyl or alkoxycarbonylalkyl; R 1 represents alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; R 1 represents hydrogen and R 1 represents hydroxy, or R 1 and R 2 together represent oxo; R 1 and R 2 together represent a trimethylene or tetramethylene group which may be substituted by hydroxy, alkoxycarbonylamino or acylamino, or in which one of the groups -CH 2 - may be replaced by -NH-, -N (alkoxycarbonyl) -, N ) - or -S-, or which carries a fused cycloalkane, aromatic or heteroaromatic ring; and R 1 represents alkoxycarbonyl, monoalkylcarbamoyl, mono-aralkylcarbamoyl, monoarylcarbamoyl or a group of formula NH / -CO. Δ C 1 CH NH 3, 11 (b); R 10 VI 91 wherein each of R 10 and represents alkyl.16. Spojine s splošno formulo VI 91 R Rl“-N\ /C°\ /CH\ . XCH NH .C ψη R7' ,CH_-N R2 \ca/19 8 R v kateri n predstavlja število 0 ali 1; R.1 predstavlja alkoksikarbonil, aralkoksikarbonil, alkanoil, cikloalkilkarbonil, aralkanoil, aroil, heterociklil-karbonil, alkilsulfonil, arilsulfonil, monoaralkilkarbamoil, cinamoil ali a-aralkoksikarbonil-aminoalkanoil in R^ predstavlja vodik, ali in R^ skupaj z atomom dušika na katerega sta vezana, predstavljata ciklično imidno skupino s formulo O (a) N— P I Q O v kateri P in Q skupaj predstavljata aromatski sistem; R^ predstavlja alkil, cikloalkil, aril, aralkil, heterociklilalkil, cianoalkil, alkilsulfinilalkil, karbamoilalkil ali alkoksi-karbonilalkil, ali kadar n predstavlja število 0, R^ lahko tudi predstavlja alkiltioalkil, ali kadar n označuje število 1, R^ prav tako lahko tudi predstavlja alkilsulfonilalkil; R^ predstavlja alkil, cikloalkil, cikloalkilalkil, aril ali aralkil; R^ predstavlja vodik in r6 predstavlja hidroksi ali R^ in R^ skupaj predstavljata okso; R^ in R^ skupaj predstavljata trimetilensko ali tetrametilensko skupino, katera je lahko substituirana z amino; in R^ predstavlja alkoksi-karbonil, monoalkilkarbamoil, monoaralkilkarbamoil, monoarilkarbamoil ali skupino s formulo —coCompounds of general formula VI. XCH NH .C ψη R7 ', CH_-N R2 \ ca / 19 8 R in which n represents the number 0 or 1; R 1 represents alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, cycloalkylcarbonyl, aralkanoyl, aroyl, heterocyclylcarbonyl, alkylsulfonyl, arylsulfonyl, monoaralkylcarbamoyl, cinnamoyl or α-aralkoxycarbonyl-aminoalkanoyl, and R 1 represents an atom and R 1 represents bound, represent a cyclic imide group of formula O (a) N-PIQO in which P and Q together represent an aromatic system; R 1 represents alkyl, cycloalkyl, aryl, aralkyl, heterocyclylalkyl, cyanoalkyl, alkylsulfinylalkyl, carbamoylalkyl or alkoxycarbonylalkyl, or when n represents the number 0, R 1 may also represent alkylthioalkyl, or when n represents the number 1, R 1 may also represent represents alkylsulfonylalkyl; R 1 represents alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; R 1 represents hydrogen and R 6 represents hydroxy or R 1 and R 6 together represent oxo; R 1 and R 2 together represent a trimethylene or tetramethylene group which may be substituted by amino; and R 1 represents alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of formula -co/“N CH R10 NH-R 11 (b) 92 v kateri vsak izmed RlO in Ril predstavlja alkil./ N N R R 10 NH-R 11 (b) 92 wherein each of R 10 and R 1 represents alkyl.17. Derivati aminokislin po kateremkoli izmed zahtevkov 1 do 14 za uporabo kot terapevtsko aktivne snovi.Amino acid derivatives according to any one of claims 1 to 14 for use as therapeutically active substances.18. Derivati aminokislin po kateremkoli izmed zahtevkov 1 do 14 za uporabo pri zdravljenju ali profilaksi virusnih infekcij.Amino acid derivatives according to any one of claims 1 to 14 for use in the treatment or prophylaxis of viral infections.19. Postopek za proizvodnjo spojine po kateremkoli izmed zahtevkov 1 do 14, označen s tem, da obsega (a) za pripravo spojin s formulo I, v kateri n označuje 0, spojina s splošno formulo H2NProcess for the production of a compound according to any one of claims 1 to 14, characterized in that it comprises (a) for the preparation of compounds of formula I in which n represents 0, a compound of general formula H2NI I v kateri imajo R^, r5? r6; r7? r8 jn r9 v zahtevku 1 navedeni pomen, reagira s kislino s splošno formulo R' R I -N CH-,3 COOH III v kateri imajo Rl, R^ in R^ v zahtevku 1 navedeni pomen, ali z njenim reaktivnim derivatom, ali 93 (b) za pripravo spojine s formulo I, v kateri n označuje 0, predstavlja vodik in predstavlja hidroksi, reduciramo spojino s formulo I, v kateri n označuje 0, in R3 in R^ skupaj predstavljata okso, ali (c) za pripravo spojine s formulo I, v kateri n označuje 0 in R* predstavlja alkanoil, cikloalkilkarbonil, aralkanoil, aroil, heterociklilkarbonil, alkilsulfonil, arilsulfonil, cinamoil ali a-aralkoksikarbonilaminoalkanoil, in R2 predstavlja vodik, ali Rl in R2 skupaj z atomom dušika s katerim sta vezana, predstavljata ciklično imidno skupino s formulo (a), navedeno v zahtevku 1, spojina s splošno formuloI I in which they have R ^, r5? r6; r7? r8 and r9 as claimed in claim 1 react with an acid of the general formula R 1 R 1 -N CH-, 3 COOH III in which R 1, R 2 and R 2 have the meaning stated in claim 1, or with a reactive derivative thereof, or 93 (b) for the preparation of a compound of formula I in which n represents 0, represents hydrogen and represents hydroxy, reduce a compound of formula I in which n represents 0, and R 3 and R 2 together represent oxo, or (c) for the preparation of a compound of formula I wherein n denotes 0 and R * represents alkanoyl, cycloalkylcarbonyl, aralkanoyl, aroyl, heterocyclylcarbonyl, alkylsulfonyl, arylsulfonyl, cinamoyl or α-aralkoxycarbonylaminoalkanoyl, and R2 represents hydrogen, or R1 and R2 together with the atom , representing a cyclic imide group of formula (a) as claimed in claim 1, a compound of general formulav kateri imajo R3, R4, R5, R6, R7, R8 in R^ v zahtevku 1 prikazani pomen, reagira s sredstvom, ki da skupino alkanoil, cikloalkilkarbonil, aralkanoil, aroil, heterociklilkarbonil, alkilsulfonil, arilsulfonil, cinamoil ali a-aralkoksikarbonil-aminoalkanoil, ali s sredstvom, ki tvori skupino cikličnega imida s formulo (a), ki je prikazana v zahtevku 1, ali (d) za pripravo spojine s formulo I, v kateri n označuje 0 in R3 predstavlja monoaralkilkarbamoil in R2 predstavlja vodik, spojina s prej prikazano formulo IV reagira s spojino s splošno formulo Rl’ -N=C=0 V v kateri R^ predstavlja aralkil, ali (e) za pripravo spojine s formulo I, v kateri R3 predstavlja alikilsulfinilalkil in n označuje 0, oksidiramo spojino s formulo I, v kateri R3 predstavlja alkiltioalkil in n označuje 0, ali 94 (f) za pripravo spojine s formulo I, v kateri n označuje 1, oksidiramo spojino s formulo I, v kateri n označuje 0, ali (g) za pripravo spojine s formulo I, v kateri n označuje 1 in predstavlja aromatsko N-heterociklilkarbonil N-oksidno skupino, in predstavlja vodik, oksidiramo spojino s formulo I, v kateri n označuje 1 in Rl predstavlja aromatsko N-hetero-ciklilkarbonilno skupino in R^ predstavlja vodik, ali (h) za pripravo spojine s formulo I, v kateri n označuje 1 in R^ predstavlja alkilsulfonilalkil, oksidiramo spojino s formulo I, v kateri n označuje 1 in R^ predstavlja alkilsulfinilalkil, ali (i) za pripravo spojine s formulo I, v kateri Rl predstavlja karboksi-substituirani aroil, hidroksi-substituirani aroil ali hidrocinamoil, in R^ predstavlja vodik, katalitsko hidrogeniramo spojino s formulo I, v kateri Rl predstavlja benziloksikarbonil-substituiran aroil, benziloksi-substituiran aroil ali cinamoil in R^ predstavlja vodik, ali (j) za pripravo spojine s formulo I, v kateri R^ predstavlja imidazol-4-il in/ali R^ predstavlja hidroksi-substituirani aril ali hidroksi-substituirani aralkil in/ali R^ in R8 skupaj predstavljata skupino trimetilen ali tetrametilen, v kateri je ena skupina -CH2- zamenjana z -NH-, obdelamo spojino s formulo I, v kateri R^ predstavlja 1-(benziloksikarbonil)-imidazol-4-il in/ali R^ predstavlja terc.-butoksi-substituiran aril ali terc.-butoksi-substituiran aralkil in/ali R^ in R8 skupaj predstavljata skupino trimetilen ali tetrametilen, v kateri je ena skupina -CH2- zamenjana z -N(terc.-butoksikarbonil)- skupino, z močno kislino, ali (k) za pripravo spojine s formulo I, v kateri R^ in R8 skupaj predstavljata skupino trimetilen ali tetrametilen, ki je substituirana z acilamino, ali v kateri je ena skupina -CH2- zamenjana z -N(acil)-, aciliramo spojino s splošno formulo H 2 R 4 CH NH /C» /Ch2 C '°»n R7-l' 'CH' R9 R 8' VI 95 v kateri imajo n, R1, R2, R3, R4, R5, R6 in R9 v zahtevku 1 navedeni pomen in R2 in R^ skupaj predstavljata skupino trimetilen ali tetrametilen, ki je substituirana z amino ali v kateri je ena skupina -CH2- zamenjana z -NH-, in/ali (l) če želimo, ločimo zmes diastereoizomernih racematov na diastereoizomerne racemate ali optično čiste diastereoizomere in/ali (m) če želimo, ločimo zmes diastereoizomerov na optično čiste diastereoizomere in/ali (n) če želimo, dobljene spojine s formulo I prevedemo v farmacevtsko sprejemljive kislinske adicijske soli.in which R 3, R 4, R 5, R 6, R 7, R 8 and R 6 have the meaning shown in claim 1, react with an agent which gives the group alkanoyl, cycloalkylcarbonyl, aralkanoyl, aroyl, heterocyclylcarbonyl, alkylsulfonyl, arylsulfonyl, cinamoyl or α-aralkoxycarbonyl aminoalkanoyl, or with an agent forming a cyclic imide group of formula (a) as claimed in claim 1, or (d) for the preparation of a compound of formula I in which n represents 0 and R 3 represents monoaralkylcarbamoyl and R 2 represents hydrogen, a compound with the above formula IV is reacted with a compound of general formula R 1 '-N = C = 0 V in which R 1 represents aralkyl, or (e) to prepare a compound of formula I in which R 3 represents alkylsulfinylalkyl and n represents 0, oxidize the compound of formula I in which R3 represents alkylthioalkyl and n represents 0, or 94 (f) for the preparation of a compound of formula I in which n represents 1 is oxidized to a compound of formula I in which n represents 0, or (g) for the preparation compounds of formula I in which n denotes 1 and represents a flavor N-heterocyclylcarbonyl N-oxide group, and represents hydrogen, oxidize a compound of formula I in which n represents 1 and R1 represents an aromatic N-heterocyclylcarbonyl group and R1 represents hydrogen, or (h) to prepare a compound of formula I , wherein n represents 1 and R 1 represents alkylsulfonylalkyl, oxidizing a compound of formula I in which n represents 1 and R 1 represents alkylsulfinylalkyl, or (i) to prepare a compound of formula I in which R 1 represents carboxy-substituted aroyl, hydroxy -substituted aroyl or hydrocinnamoyl, and R 1 represents hydrogen, catalytically hydrogenated a compound of formula I in which R 1 represents benzyloxycarbonyl-substituted aroyl, benzyloxy-substituted aroyl or cinamoyl and R 1 represents hydrogen, or (j) for the preparation of a compound of formula I , wherein R 1 represents imidazol-4-yl and / or R 1 represents hydroxy-substituted aryl or hydroxy-substituted aralkyl and / or R 1 and R 8 together represent a trimethylene or tetramethylene group in which one group -CH2- replaced by -NH-, is treated with a compound of formula I in which R 1 represents 1- (benzyloxycarbonyl) -imidazol-4-yl and / or R 1 represents tert-butoxy-substituted aryl or tert- butoxy-substituted aralkyl and / or R 1 and R 8 together represent a trimethylene or tetramethylene group in which one -CH 2 - group is replaced by an -N (tert-butoxycarbonyl) - group, with a strong acid, or (k) for the preparation of a compound of formula I, in which R 1 and R 8 together represent an acylamino-substituted trimethylene or tetramethylene group, or in which one -CH 2 - group is replaced by -N (acyl) -, a compound of general formula H 2 R 4 is acylated CH NH / C »/ Ch2 C '°» n R7-1' 'CH' R9 R 8 'VI 95 in which n, R1, R2, R3, R4, R5, R6 and R9 have the meaning given in claim 1 and R2 and R 1 together represent a group of trimethylene or tetramethylene substituted with amino or in which one group -CH 2 - is replaced by -NH-, and / or (l) if desired, separate the mixture of diastereoisomeric racemates to diast ereoisomeric racemates or optically pure diastereoisomers and / or (m) if desired, separating the mixture of diastereoisomers into optically pure diastereoisomers and / or (n) if desired, converting the obtained compounds of formula I into pharmaceutically acceptable acid addition salts.20. Postopek po zahtevku 19, označen s tem, da spojine s formulo I, v kateri n označuje 0, R3 predstavlja alkil, cikloalkil, aril, aralkil, heterociklilalkil, cianoalkil, alkiltioalkil, karbamoilalkil ali alkoksikarbonilalkil in R2 in R^ skupaj predstavljata skupino trimetilen ali tetrametilen, v kateri je ena skupina -CH2- lahko zamenjana z -NH- ali -S-, ali katera lahko nosi kondenzirani cikloalkanski, aromatski ali heteroaromatski obroč, in njihove farmacevtsko sprejemljive kislinske adicijske soli pripravimo na osnovi izvedb (a), (b), (c), (d) in/ali (n) postopka. Za: F.HOFFMANN-LA ROCHE AG 4 VRELI J A G 4.Process according to Claim 19, characterized in that the compounds of the formula I in which n represents 0, R 3 represents alkyl, cycloalkyl, aryl, aralkyl, heterocyclylalkyl, cyanoalkyl, alkylthioalkyl, carbamoylalkyl or alkoxycarbonylalkyl and R 2 and R 2 together represent a group trimethylene or tetramethylene, in which one group -CH2- may be replaced by -NH- or -S-, or which may bear a fused cycloalkane, aromatic or heteroaromatic ring, and their pharmaceutically acceptable acid addition salts are prepared on the basis of embodiments (a), (b), (c), (d) and / or (n) of the procedure. For: F.HOFFMANN-LA ROCHE AG 4 VRELI J A G 4.
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