Claims
- 1. A compound of the formula ##STR71## an acid addition salt thereof with an inorganic or organic acid, or a quaternary ammonium salt thereof formed by reaction with an alkyl halide,
- wherein
- R.sup.1, R.sup.4, and R.sup.5, taken alone, are the same or different and are hydrogen, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.6 alkanoyloxy, or halogen, or
- any two of R.sup.1, R.sup.4 and R.sup.5, in adjacent positions and taken together, are methylenedioxy or ethylenedioxy;
- R.sup.2 and R.sup.3, taken alone, are the same or different and are hydrogen, hydroxy, amino, C.sub.1 -C.sub.6 alkyl substituted by furyl or tetra-hydrofuryl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, di(C.sub.1 -C.sub.3 alkoxy) C.sub.1 -C.sub.6 alkyl, halo-C.sub.1 -C.sub.6 alkyl, di(C.sub.1 -C.sub.4 alkyl)amino C.sub.1 -C.sub.6 alkyl, phenyl-C.sub.1 -C.sub.2 alkyl, or phenyl-C.sub.1 -C.sub.2 alkyl wherein the phenyl is mono-, di-, or tri-substituted with C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.6 alkanoyl, unsubstituted phenyl or by phenyl mono- or poly-substituted with C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkyl, halogen, or trifluoromethyl, or
- R.sup.2 and R.sup.3, taken together with the nitrogen atom to which they are attached, are morpholino or piperizino or morpholino or piperizino substituted with C.sub.1 -C.sub.6 alkyl, piperidino, phenyl, or phenyl substituted with C.sub.1 -C.sub.3 alkoxy or by tri-fluoromethyl; and
- R.sup.6 is hydrogen, C.sub.1 -C.sub.6 alkyl, di-(C.sub.1 -C.sub.4 alkyl) amino-C.sub.1 -C.sub.6 alkyl, or di-(C.sub.1 -C.sub.6 alkyl)-phosphinyl-C.sub.1 -C.sub.3 alkyl; but
- if R.sup.6 is defined as above, then R.sup.2 represents an electron pair and if R.sup.2 is defined as above, then R.sup.6 represents an electron pair.
- 2. 9,10-Dimethoxy-2-tert.-butylamino-6,7-dihydro-4H-pyrimido(6,1-a)isoquinoline-4-one hydrochloride.
- 3. 9,10-Dimethoxy-2-(2,4,6-trimethylanilino)-6,7-dihydro-4H-pyrimido(6,1-a)isoquinolin-4-one hydrochloride dihydrate.
- 4. 9,10-Dimethoxy-3-methyl-2-mesitylimino-2,3,6,7-tetrahydro-4H-pyrimido(6,1-a)isoquinolin-4-one hydrochloride.
- 5. 9,10-Dimethoxy-2-(N-methyl-2,4,6-trimethylanilino)-6,7-dihydro-4H-pyrimido(6,1-a)isoquinolin-4-one hydrochloride.
- 6. 9,10-Dimethoxy-3-isopropyl-2-mesitylimino-2,3,6,7-tetrahydro-4H-pyrimido(6,1-a)isoquinolin-4-one hydrochloride.
- 7. 9,10-Dimethoxy-2-(N-isopropyl-2,4,6-trimethylanilino)-6,7-dihydro-4H-pyrimido(6,1-a)isoquinolin-4-one hydrochloride.
- 8. 9,10-Dimethoxy-3-ethyl-2-mesitylimino-2,3,6,7-tetrahydro-4H-pyrimido(6,1-a)isoquinolin-4-one hydrochloride.
- 9. 9,10-Dimethoxy-2-(N-ethyl-2,4,6-trimethylanilino)-6,7-dihydro-4H-pyrimido(6,1-a)isoquinolin-4-one hydrochloride.
- 10. 9,10-Dimethoxy-3-acetyl-2-mesitylimino-2,3,6,7-tetrahydro-4H-pyrimido(6,1-a)isoquinolin-4-one.
- 11. 9,10-Dimethoxy-2-(N-acetyl-2,4,6-trimethylanilino)-6,7-dihydro-4H-pyrimido(6,1-a)isoquinolin-4-one.
- 12. A pharmaceutical composition for the treatment of hypertonia, bronchospasms, or allergies, which composition comprises a pharmaceutically effective amount of a compound as in claim 1 and a pharmaceutically acceptable excipient.
- 13. A method for the treatment of hypertonia, bronchospasms, or allergies in a mammal suffering therefrom, which method comprises orally, parenterally, rectally, or topically administering to said mammal a pharmaceutically effective amount of a compound as in claim 1.
Priority Claims (1)
Number |
Date |
Country |
Kind |
2720085 |
May 1977 |
DEX |
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Parent Case Info
This application is a continuation-in-part application of application Ser. No. 848,289 filed Nov. 3, 1977 and now abandoned.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
3021331 |
Lombardino et al. |
Feb 1962 |
|
3081306 |
Lombardino et al. |
Mar 1963 |
|
Non-Patent Literature Citations (3)
Entry |
Lal et al., "Chemical Abstracts", vol. 90, 1979, col. 90:54969z. |
Lal et al., "Chemical Abstracts", vol. 90, 1979, col. 90:54974y. |
Lal et al., "Chemical Abstracts", vol. 91, 1979, col. 91:39527f. |
Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
848289 |
Nov 1977 |
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