Claims
- 1. A compound of the formula
- or a physiologically tolerated salt thereof,
- wherein R.sub.1 and R.sub.2, which are the same or different, each represent
- a) alkyl or alkenyl having up to 6 C-atoms,
- b) alkyl or aklenyl having up to 6 C-atoms substituted by
- 1) (C.sub.5 -C.sub.7)-cycloalkyl,
- 2) (C.sub.5 -C.sub.7)-cycloalkenyl,
- 3) fluoro,
- 4) mercapto,
- 5) hydroxy,
- 6) (C.sub.1 -C.sub.3)-alkoxy optionally substituted by N,N-dimethylamino,
- 7) phenoxy,
- 8) phenoxy substituted by
- 8.1 halogen
- 8.2 (C.sub.1 -C.sub.6)-alkyl,
- 8.3 (C.sub.1 -C.sub.6)-alkoxy,
- 8.4 nitro, and/or
- 8.5 carbethoxy,
- 9) naphthyloxy,
- 10) benzyloxy,
- 11) benzyloxy substituted in the aryl part by
- 11.1 methoxy,
- 11.2 carboxamido,
- 11.3 amino,
- 11.4 halogen,
- 11.5 nitro, or
- 11.6 methyl,
- 12) amino,
- 13) monoalkylamino having up to 7 C-atoms,
- 14) monoalkylamino having up to 7 C-atoms substituted in the alkyl part by
- 14.1 hydroxy,
- 14.2 carboxy,
- 14.3 carboxamido,
- 14.4 carbethoxy,
- 14.5 amino,
- 14.6 (C.sub.1 -C.sub.6)-alkylamino,
- 14.7 di-(C.sub.1 -C.sub.6)-alkylamino,
- 14.8 piperidino, or
- 14.9 morpholino,
- 15) dialkylamino having up to 7 C-atoms,
- 16) dialkylamino having up to a total of 7 C-atoms substituted in the alkyl part by
- 16.1 hydroxy,
- 16.2 carboxy,
- 16.3 carboxamido,
- 16.4 carbethoxy,
- 16.5 amino,
- 16. 6 (C.sub.1 -C.sub.6)-alkylamino,
- 16.7 di-(C.sub.1 -C.sub.6)-alkylamino,
- 16.8 piperidino, or
- 16.9 morpholino,
- 17) monocycloalkylamino having up to 7 C-atoms,
- 18) dicycloalkylamino having up to 7 C-atoms,
- 19) (C.sub.1 -C.sub.6)-alkoxycarbonylamino,
- 20) phenoxycarbonylamino,
- 21) phenoxycarbonylamino substituted by
- 21.1 halogen,
- 21.2 (C.sub.1 -C.sub.6)-alkyl,
- 21.3 C.sub.1 -C.sub.6)-alkoxy,
- 21.4 nitro, and/or
- 21.5 carbethoxy,
- 22) naphthyloxycarbonylamino,
- 23) benzyloxycarbonylamino or phenethyloxycarbonylamino,
- 24) benzyloxycarbonylamino or phenethyloxycarbonylamino each substituted in the aryl part by
- 24.1 halogen,
- 24.2 nitro,
- 24.3 (C.sub.1 -C.sub.6)-alkyl, or
- 24.4 (C.sub.1 -C.sub.6)-alkoxy,
- 25) phenylcarbamoyloxy,
- 26) (C.sub.1 -C.sub.6)-alkylureido,
- 27) cyclohexylureido,
- 28) phenylureido,
- 29) phenylureido substituted by
- 29.1 halogen,
- 29. 2 (C.sub.1 -C.sub.6)-alkyl,
- 29.3 (C.sub.1 -C.sub.6)-alkoxy, and/or
- 29.4 nitro,
- 30) naphthylureido,
- 31) benzylureido or phenethylureido,
- 32) benzylureido or phenethylureido each substituted by
- 32.1 halogen,
- 32.2 nitro,
- 32.3 (C.sub.1 -C.sub.6)-alkyl, or
- 32.4 (C.sub.1 -C.sub.6)-alkoxy,
- 33) formyl,
- 34) (C.sub.1 -C.sub.6)-alkanoylamino,
- 35) benzoylamino,
- 36) benzoylamino mono- to tri-substituted by
- 36.1 halogen,
- 36.2 (C.sub.1 -C.sub.6)-alkyl,
- 36.3 (C.sub.1 -C.sub.6)-alkoxy,
- 36.4 hydroxy,
- 36.5 carboxy,
- 36.6 nitro, or
- 36.7 amino,
- 37) naphthoylamino,
- 38) benzylcarbonylamino or phenethylcarbonylamino,
- 39) benzylcarbonylamino or phenethylcarbonylamino each substituted by
- 39.1 halogen,
- 39.2 nitro,
- 39.3 (C.sub.1 -C.sub.6)-alkyl, or
- 39.4 (C.sub.1 -C.sub.6)-alkoxy,
- 40) phenylamino or naphthylamino,
- 41) phenylamino or naphthylamino each mono- or di-substituted by
- 41.1 (C.sub.1 -C.sub.2)-alkyl,
- 41.2 (C.sub.1 -C.sub.2)-alkoxy,
- 41.3 methylenedioxy,
- 41.4 amino,
- 41.5 hydroxy,
- 41.6 acetoxy,
- 41.7 carboxy,
- 41.8 carboxamido,
- 41.9 carbethoxy,
- 41.10 halogen, and/or
- 41.11 nitro,
- 42) 4,6-dimethyl-pyrimidyl-amino,
- 43) benzylamino or phenethylamino,
- 44) benzylamino or phenethylamino each mono- or di-substituted in the aryl part by
- 44.1 (C.sub.1 -C.sub.2)-alkyl,
- 44.2 (C.sub.1 -C.sub.2)-alkoxy,
- 44.3 methylenedioxy,
- 44.4 amino,
- 44.5 hydroxy,
- 44.6 acetoxy,
- 44.7 carboxy,
- 44.8 carboxamido,
- 44.9 carbethoxy,
- 44.10 halogen, and/or
- 44.11 nitro,
- 45) (C.sub.1 -C.sub.6)-alkylmercapto, (C.sub.1 -C.sub.6)-alkylsulfinyl, or (C.sub.1 -C.sub.6)-alkylsulfonyl,
- 46) (C.sub.1 -C.sub.6)-alkylmercapto, (C.sub.1 -C.sub.6)-alkylsulfinyl, or (C.sub.1 -C.sub.6)-alkylsulfonyl each substituted by
- 46.1 methoxy,
- 46.2 ethoxy,
- 46.3 hydroxy,
- 46.4 carboxy,
- 46.5 carboxamido,
- 46.6 carbethoxy,
- 46.7 amino,
- 46.8 (C.sub.1 -C.sub.6)-alkylamino, or
- 46.9 dimethylamino,
- 47) phenylmercapto, naphthylmercapto, phenylsulfinyl, naphthylsulfinyl, phenylsulfonyl, or naphthylsulfonyl,
- 48) phenylmercapto, naphthylmercapto, phenylsulfinyl, naphthylsulfinyl, phenylsulfonyl, or naphthylsulfonyl each substituted by
- 48.1 methoxy,
- 48.2 ethoxy,
- 48.3 hydroxy,
- 48.4 carboxy,
- 48.5 carboxamido,
- 48.6 carbethoxy,
- 48.7 amino,
- 48.8 (C.sub.1 -C.sub.6)-alkylamino,
- 48.9 halogen,
- 48.10 nitro,
- 48. 11 sulfonamido, or
- 48.12 methyl,
- 49) benzylmercapto, benzylsulfinyl, or benzylsulfonyl,
- 50) benzylmercapto, benzylsulfinyl, or benzylsulfonyl each substituted in the alkyl part by
- 50.1 methoxy,
- 50.2 ethoxy,
- 50.3 hydroxy,
- 50.4 carboxy,
- 50.5 carboxamido,
- 50.6 carbethoxy,
- 50.7 amino,
- 50.8 (C.sub.1 -C.sub.6)-alkylamino, or substituted in the aryl part by
- 50.9 methoxy,
- 50.10 ethoxy,
- 50.11 hydroxy, or
- 50.12 carboxy,
- 51) carboxy,
- 52) carboalkoxy with alkyl having up to 3 C-atoms,
- 53) carbobenzyloxy,
- 54) carbamoyl,
- 55) alkylaminocarbonyl having up to 6 C-atoms,
- 56) cycloalkylaminocarbonyl having up to 6 C-atoms,
- 57) cycloalkenylaminocarbonyl having up to 6 C-atoms,
- 58) dialkylaminocarbonyl having up to 6 C-atoms,
- 59) phenylaminocarbonyl,
- 60) phenylaminocarbonyl mono- to tri-substituted by
- 60.1 halogen,
- 60.2 (C.sub.1 -C.sub.6)-alkyl,
- 60.3 (C.sub.1 -C.sub.6)-alkoxy,
- 60.4 carboxy,
- 60.5 carboxamido,
- 60.6 carbethoxy,
- 60.7 hydroxy, and/or
- 60.8 nitro,
- 61) naphthylaminocarbonyl,
- 62) benzylaminocarbonyl or phenethylaminocarbonyl,
- 63) benzylaminocarbonyl or phenethylaminocarbonyl each substituted by
- 63.1 halogen,
- 63.2 nitro,
- 63.3 (C.sub.1 -C.sub.6)-alkyl, or
- 63.4 (C.sub.1 -C.sub.6)-alkoxy,
- 64) guanido,
- 65) phenyl, naphthyl, dihydronaphthyl, or tetrahydronaphthyl,
- 66) phenyl, naphthyl, dihydronaphthyl, or tetrahydronaphthyl, each mono- to tri-substituted by
- 66.1 halogen,
- 66.2 hydroxy,
- 66.3 acetoxy,
- 66.4 carboxy,
- 66. 5 carboxamido,
- 66.6 sulfonamido,
- 66.7 nitro,
- 66.8 methyl,
- 66.9 ethyl,
- 66.10 methoxy,
- 66.11 ethoxy, and/or
- 66.12 amino,
- 67) a 5-membered to 7-membered monocyclic heterocyclic structure, the hetero atoms of which are one or two S- or O-atoms and/or up to four N-atoms,
- 68) a 5-membered to 7-membered monocyclic heterocyclic structure, the hetero atoms of which are one or two S- or O-atoms and up to four N-atoms, which heterocyclic structure is substituted by
- 68.1 halogen,
- 68.2 oxo,
- 68.3 S-oxo,
- 68.4 hydroxy,
- 68.5 carboxy,
- 68.6 carboxamido,
- 68.7 sulfonamido,
- 68.8 nitro,
- 68.9 (C.sub.1 -C.sub.6)-alkyl,
- 68.10 benzyl or phenethyl,
- 68.11 methoxy,
- 68.12 ethoxy, or
- 68.13 amino,
- 69) a 9-membered or 10-membered bicyclic heterocyclic structure, the hetero atoms of which are one or two S- or O-atoms and/or up to four N-atoms per ring, or
- 70) a 9-membered or 10-membered bicyclic heterocyclic structure, the hetero atoms of which are one or two S- or O-atoms per ring, which heterocyclic structure is substituted by
- 70.1 halogen,
- 70.2 oxo,
- 70.3 S-oxo,
- 70.4 hydroxy,
- 70.5 carboxy,
- 70.6 carboxamido,
- 70.7 sulfonamido,
- 70.8 nitro,
- 70.9 (C.sub.1 -C.sub.6)-alkyl,
- 70.10 benzyl or phenethyl,
- 70.11 methoxy, or
- 70.12 ethoxy,
- c) (C.sub.5 -C.sub.7)-cycloalkyl- or cycloalkenyl,
- d) (C.sub.7 -C.sub.12)-cycloalkylalkyl,
- e) phenyl, naphthyl, dihydronaphthyl, or tetrahydronaphthyl,
- f) phenyl, naphthyl, dehydronaphthyl, or tetrahydronaphthyl, each substituted by
- 1) halogen,
- 2) (C.sub.1 -C.sub.6)-alkyl, or
- 3) (C.sub.1 -C.sub.6)-alkoxy,
- g) a 6-membered monocyclic heterocycle, the hetero atoms of which are one or two S-atoms; or
- wherein R.sub.1 is hydrogen and R.sub.2 is defined as above in a)-g); and
- wherein R.sub.3 is hydrogen, alkyl having 1 to 6 carbon atoms, alkenyl having 2 to 10 carbon atoms, or aralkyl having 7 to 14 carbon atoms.
- 2. A compound as in claim 1 in which is N-(1-carboethoxy-3-phenyl-propyl)-L-alanyl-L-decahydroisoquinoline-3-carboxylic acid.
- 3. A compound as in claim 1 which is N-[1-S-carboethoxy-3-(3-indolyl)-propyl]-S-alanyldecahydroisoquinoline-3-S-carboxylic acid.
- 4. A compound as in claim 1 which is N-[1-S-carboethoxy-2-(3-indolyl)-ethyl]-S-alanyldecahydroisoquinoline-3-S-carboxylic acid.
- 5. A pharmaceutical preparation for the treatment of hypertension, said preparation comprising a hypotensively effective amount of a compound or salt as in claim 1 and a pharmaceutically acceptable carrier therefor.
- 6. A method for treating hypertension in a patient suffering therefrom, which method comprises orally, intravenously, or subcutaneously administering to said patient a hypotensively effective amount of a compound as in claim 1.
Priority Claims (2)
Number |
Date |
Country |
Kind |
3032709 |
Aug 1980 |
DEX |
|
3118191 |
May 1981 |
DEX |
|
Parent Case Info
This is a division, of application Ser. No. 297,191, filed Aug. 28, 1981.
US Referenced Citations (5)
Foreign Referenced Citations (3)
Number |
Date |
Country |
0012845 |
Jul 1980 |
EPX |
2448533 |
Sep 1980 |
FRX |
2470767 |
Jun 1981 |
FRX |
Non-Patent Literature Citations (2)
Entry |
Geiger et al., "Chemical Abstracts", vol. 97, 1982, col. 97:92759h. |
Remond, et al., "Chemical Abstracts", vol. 97, 1982, col. 97:216716p. |
Divisions (1)
|
Number |
Date |
Country |
Parent |
297191 |
Aug 1981 |
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