Claims
- 1. A compound of formula (I): ##STR14## wherein R is a hydrogen atom or a group selected from C.sub.1-6 alkyl unsubstituted or substituted by C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, C.sub.3-7 cycloalkyl, phenalkyl in which the alkyl moiety contains 1-5 carbon atoms, and --CHO; R.sup.1 is a group selected from halogen, C.sub.1-4 alkyl, or hydroxyl; and
- R.sup.2 is a hydrogen atom or a substituent as defined above for R.sup.1 ;
- and the physiologically acceptable salts thereof.
- 2. A compound according to claim 1, wherein, in the general formula (I), R is a hydrogen atom.
- 3. A compound according to claim 1, wherein, in the general formula (I), R is a C.sub.1-3 alkyl group.
- 4. A compound according to claim 1, wherein, in the general formula (I), R.sup.1 is a halogen atom or a C.sub.1-4 alkyl group.
- 5. A compound according to claim 1, wherein, in the general formula (I), R.sup.2 is a hydrogen or fluorine atom.
- 6. A compound according to claim 1, wherein, in the general formula (I), R is a hydrogen atom or a methyl or ethyl group; R.sup.1 is a chlorine or fluorine atom or a methyl group; and R.sup.2 is a hydrogen or fluorine atom.
- 7. A compound selected from (.+-.)-trans-2,3,3a,9a-tetrahydro-5-methyl-1H-[1,4]benzodioxino[2,3-c]pyrrole, and its 3aS- and 3aR-isomers; (.+-.)-trans-5-chloro-2,3,3a,9a-tetrahydro-1H-[1,4]benzodioxino[2,3-c]-pyrrole, and its 3aS- and 3aR-isomers; (.+-.)-trans-5,8-difluoro-2,3,3a,9a-tetrahydro-1H-[1,4]benzodioxino[2,3-c]pyrrole and its 3aS- and 3aR-isomers; and their physiologically acceptable salts.
- 8. A compound selected from (.+-.)-trans-5-fluoro-2,3,3a,9a-tetrahydro-1H-[1,4]benzodioxino[2,3-c]pyrrole and its 3aS- and 3aR-isomers and their physiologically acceptable salts.
- 9. (.+-.)-trans-5-Fluoro-2,3,3a,9a-tetrahydro-1H-[1,4]benzodioxino[2,3-c]pyrrole hydrochloride and its 3aS- and 3aR-isomers.
- 10. An alpha.sub.2 -adrenoreceptor antagonist composition comprising a pharmaceutically effective amount of an alpha.sub.2 -adrenoreceptor antagonist compound selected from the group consisting of compounds of formula (I), claim 1, physiologically acceptable salts thereof and their mixtures, together with a physiologically acceptable carrier or excipient.
- 11. An alpha.sub.2 -adrenoreceptor composition according to claim 10 which also comprises an effective amount of an established antidepressant selected from the group consisting of desmethylimipramine, imipramine or amitriptyline.
- 12. A method of treating or preventing depression susceptible to amelioration by an alpha.sub.2 -adrenoreceptor antagonist comprising administering an effective amount of a compound selected from the group consisting of compounds of formula (I), claim 1, physiologically acceptable salts thereof and mixtures thereof.
- 13. A method of treating or preventing migraine and senile dementia susceptible to amelioration by an alpha.sub.2 -adrenoreceptor antagonist comprising administering an effective amount of a compound selected from the group consisting of compounds of formula (I), claim 1, physiologically acceptable salts thereof and mixtures thereof.
- 14. A method of treating or preventing thrombosis, diabetes and hypertension susceptible to amelioration by an alpha.sub.2 -adrenoreceptor antagonist comprising administering an effective amount of a compound selected from the group consisting of compounds of formula (I), claim 1, physiologically acceptable salts thereof and mixtures thereof.
- 15. A method of treating or preventing obesity, constipation and paralytic ileus susceptible to amelioration by an alpha.sub.2 -adrenoreceptor antagonist comprising administering an effective amount of a compound selected from the group consisting of compounds of formula (I), claim 1, physiologically acceptable salts thereof and mixtures thereof.
Priority Claims (2)
Number |
Date |
Country |
Kind |
8410456 |
Apr 1984 |
GBX |
|
8503975 |
Feb 1985 |
GBX |
|
Parent Case Info
This is a continuation of co-pending application Ser. No. 930,891 filed Nov. 17, 1986, now abandoned which is a continuation of application Ser. No. 726,604 filed Apr. 24, 1985, now abandoned.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
4496579 |
Crame et al. |
Jan 1985 |
|
4680411 |
Picart |
Jul 1987 |
|
Non-Patent Literature Citations (4)
Entry |
A. Burger, Medicinal Chemistry (Second Edition), pp. 42-43 (1960), Interscience Publishers, Inc. N.Y. RS403B8. |
A. Funke et al., Chem. Abstr. vol. 56, No. 14257i (1962). |
G. Marini-Bettolo, Chem. Abstr. vol. 52, No. 16356h (1958). |
R. Berthold et al., Helvetica Chimica Acta, 55:2461-2467, (1977). |
Continuations (2)
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Number |
Date |
Country |
Parent |
930891 |
Nov 1986 |
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Parent |
726604 |
Apr 1985 |
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