Claims
- 1. A compound of the formula ##STR31## wherein A is selected from the group consisting of ##STR32## R.sup.1 is selected from the group consisting of hydrogen, chlorine, bromine, lower alkyl, the group NR.sub.4 R.sub.5, the group --CH.sub.2 --CO-- R.sub.7, the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, hydroxy, lower alkoxy, mercapto and lower alkyl mercapto; R.sub.2 is hydrogen; R.sub.3 is selected from the group consisting of hydrogen, the radical of the formula ##STR33## wherein R is lower alkyl or hydrogen and hydroxy; X is selected from the group consisting of hydrogen, halogen, trifluoromethyl, ethyl, .alpha.-hydroxy ethyl and acetyl; Y is hydrogen or halogen; R.sub.4 and R.sub.5 are hydrogen or lower alkyl or together with their co-bonded nitrogen atom form a five to seven membered heterocyclic group selected from the group consisting of morpholino, piperidino, 3-pyrrolino, piperazino, azetidino, aziridino, pyrrolidino and hexamethyleneimino; R.sub.7 is selected from the group consisting of hydroxy, lower alkoxy and NR.sub.8 R.sub.9 ; R.sub.8 and R.sub.9 are hydrogen or lower alkyl; n is 0 or 1 and m is 1 to 7 with the limitation that (1) when R.sub.3 is the radical ##STR34## or hydroxy, A is the group (a), X is hydrogen, halogen, trifluoromethyl, ethyl or acetyl and R.sub.1 is the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, then R.sub.8 and R.sub.9 are lower alkyl, (2) when A is group (d) and R.sub.1 is the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, then R.sub.8 and R.sub.9 are lower alkyl and (3) when n is 1, R.sub.1 is hydrogen, lower alkyl, lower alkoxy, chlorine, bromine or the group --CH.sub.2 --CO--R.sub.7 with R.sub.7 as above, then A is the group (a) or (b) and the pharmaceutically acceptable salts thereof.
- 2. The compound of claim 1 wherein A is group (b), R.sub.1 is amino, n is 0, X is selected from the group consisting of hydrogen, halogen and trifluoromethyl and Y is hydrogen or halogen.
- 3. The compound of claim 1 wherein R.sub.1 is selected from the group consisting of hydrogen, chlorine, bromine, lower alkyl, the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9 wherein m is 1 to 7 and R.sub.8, R.sub.9 are hydrogen or lower alkyl, the group --CH.sub.2 --CO--R.sub.7, hydroxy lower alkoxy, mercapto and lower alkyl mercapto; R.sub.7 is lower alkoxy or dialkylaminoalkylamino; and R.sub.2 is hydrogen.
- 4. The compound of claim 1 wherein A is group (a) and n is 0.
- 5. The compound of claim 4 wherein R.sub.2 and R.sub.3 are hydrogen; R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, the group NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are hydrogen or lower alkyl, hydroxy, chlorine, bromine, the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are lower alkyl and the group --CH.sub.2 --CO--R.sub.7.
- 6. The compound of claim 5 wherein R.sub.1 is selected from the group consisting of hydrogen, amino and lower alkyl.
- 7. The compound of claim 4 wherein R.sub.2 is hydrogen; R.sub.3 is hydroxy and R.sub.1 is selected from the group consisting of hydrogen, lower alkyl and the group NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are hydrogen or lower alkyl.
- 8. The compound of claim 4 wherein R.sub.1 and R.sub.3 are hydrogen and R.sub.2 is amino or di-lower alkylmino.
- 9. The compound of claim 8 wherein R.sub.2 is dimethylamino.
- 10. The compound of claim 1 wherein X is halogen.
- 11. The compound of claim 10 wherein X is chlorine.
- 12. The compound of claim 11 wherein Y is selected from the group consisting of hydrogen, chlorine and fluorine.
- 13. The compound: 9-chloro-7-(2chlorophenyl)-5H-pyrimido[5,4-d][2]benzazepine.
- 14. The compound: b 9-chloro-7-(2-fluorophenyl)-5H-pyrimido[5,4-d][2]benzazepine.
- 15. The compound: 9-chloro-7-(2-chlorophenyl)-2-methyl-5H-pyrimido[5,4-d][2]benzazepine.
- 16. The compound: 9-chloro-7-(2-fluorophenyl)-N,N-dimethyl-5H-pyrimido[5,4-d][2]benzazepine-4-amine.
- 17. The compound: 9-chloro-7-(2fluorophenyl)-5H-pyrimido[5,4-d][2]benzazepin-2ol.
- 18. The compound: 9-chloro-N,N-dimethyl-7-(2-fluorophenyl)-5H-pyrimido[5,4-d][2benzazepin-2amine.
RELATED APPLICATIONS
This is a continuation, of application Ser. No. 151,025 filed May 19, 1980 (abandoned), which is a continuation-in-part of Ser. No. 16,709, filed Mar. 1, 1979 (abandoned).
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
3599300 |
Finizio |
May 1976 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
833249 |
Sep 1975 |
BEX |
Continuations (1)
|
Number |
Date |
Country |
Parent |
151025 |
May 1980 |
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Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
16709 |
Mar 1979 |
|