Claims
- 1. A hetrazepine of formula Ia, ##STR121## wherein R.sub.1 is hydrogen or methyl;
- R.sub.2 is hydrogen or methyl;
- R.sub.3 is hydrogen or methyl;
- R.sub.4 is phenyl optionally substituted in the 2-position by halogen;
- R.sub.5 is C.sub.1-4 -alkyl or
- R.sub.5 is a group ##STR122## wherein R.sub.7 is hydrogen, halogen, nitro, trifluoromethyl, branched or unbranched C.sub.1-8 -alkyl optionally substituted by halogen or hydroxy, C.sub.3-6 -cycloalkyl optionally substituted by halogen or hydroxy, branched or unbranched C.sub.1-4 -alkoxy, C.sub.1-4 -alkyl--S--, HS--, amino, C.sub.1-6 -alkylamino, or C.sub.1-6 -dialkylamino,
- k is 1, 2 or 3, whilst if
- k is greater than 1, R.sub.7 may be identical or different; or
- R.sub.5 is pentafluorophenyl, or a group: ##STR123## wherein R.sub.8 is hydrogen, halogen or C.sub.1-4 -alkyl.
- 2. The hetrazepine as recited in claim 1 wherein
- R.sub.1 is CH.sub.3 ;
- R.sub.2 is hydrogen;
- R.sub.3 is hydrogen or methyl;
- R.sub.4 is ortho-chlorophenyl;
- R.sub.5 is a group ##STR124## wherein R.sub.7 is hydrogen, halogen, trifluoromethyl, branched or unbranched C.sub.1-4 -alkyl, branched or unbranched C.sub.1-4 -alkoxy, k is 1, 2 or 3, whilst if k is greater than 1, R.sub.7 may be identical or different; or
- R.sub.5 is pentafluorophenyl; or
- R.sub.5 is a group: ##STR125## wherein R.sub.8 is hydrogen.
- 3. The heterazepine as recited in claim 1 wherein
- R.sub.4 is a phenyl ring substituted in the 2- position by chlorine and
- R.sub.5 is a group ##STR126## wherein R7 is C.sub.1-4 -alkyl.
- 4. The heterazepine as recited in claim 1 wherein
- R.sub.1 is CH.sub.3 ;
- R.sub.2 is hydrogen;
- R.sub.3 is hydrogen or methyl;
- R.sub.4 is ortho-chlorophenyl;
- R.sub.5 is a group ##STR127## wherein R.sub.7 is hydrogen, methyl, tert.-butyl, iso-butyl, sec.-butyl, methoxy, trifluormethyl, ethyl, or chloro.
- 5. The heterazepine as recited in claim 2, wherein
- R.sub.5 is 2-thiophene or 2-furan.
- 6. 3-(4-Chlorobenzoyl)-6-(2-chlorophenyl)-8-11-dimethyl-2,3,4,5-tetrahydro-4H-pyrido-�4,3:4',5'!thieno-�3,2-f!�1,2,4!triazolo�4,3-a!-1,4-diazepine.
- 7. A pharmaceutical composition of matter comprising a therapeutically effective amount of a hetrazepine as recited in claim 1 and a pharmaceutically acceptable inert carrier.
- 8. A pharmaceutical composition of matter comprising a therapeutically effective amount of a hetrazepine as recited in claim 6 and a pharmaceutically acceptable inert carrier.
- 9. A method of treating disease in a warm-blooded animal induced by endogenously formed PAF which comprises administering to said animal a therapeutically effective amount of a hetrazepine as recited in claim 1.
- 10. A method of treating disease in a warm-blooded animal induced by endogenously formed PAF which comprises administering to said animal a therapeutically effective amount of a hetrazepine as recited in claim 6.
Priority Claims (1)
Number |
Date |
Country |
Kind |
41 075 21.8 |
Mar 1991 |
DEX |
|
Parent Case Info
This is a continuation of application Ser. No. 08/152,045, filed Nov. 12, 1993, now abandoned, which is a continuation of application Ser. No. 07/848,575, filed Mar. 9, 1992, now abandoned.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
5304553 |
Okano et al. |
Apr 1994 |
|
Foreign Referenced Citations (5)
Number |
Date |
Country |
0230942 |
Aug 1987 |
EPX |
254245 |
Jan 1988 |
EPX |
0328924 |
Aug 1989 |
EPX |
0368175 |
May 1990 |
EPX |
367110 |
May 1990 |
EPX |
Non-Patent Literature Citations (1)
Entry |
Miyazawa et al, Chem. Pharm. Bull 39(12), pp. 3215-3220 (1991). |
Continuations (2)
|
Number |
Date |
Country |
Parent |
152045 |
Nov 1993 |
|
Parent |
848575 |
Mar 1992 |
|