RU97104165A

RU97104165A - SPYRO-ABABYCLIC COMPOUNDS USEFUL IN THERAPY

Info

Publication number: RU97104165A
Application number: RU97104165/04A
Authority: RU
Inventors: Балестра Майкл; Чарлз Гордон Джон; Конрад Гриффит Роналд; Джон Мюррей Роберт
Original assignee: Астра Актиеболаг
Priority date: 1994-08-24
Filing date: 1995-08-22
Publication date: 1999-03-10

Claims

1. The compound of formula I:

Where
R represents hydrogen or methyl;
n = 1 or 2,
or their pharmaceutically acceptable acid addition salts or enantiomers.

2. The compound according to claim 1, in which R represents hydrogen, or its pharmaceutically acceptable acid addition salt, or enantiomer.

3. The compound according to claim 1, representing spiro [1-azabicyclo [2.2.2] octane-3,5'-oxazolidine] -2'-one, or its pharmaceutically acceptable acid addition salt, or enantiomer.

4. The compound according to claim 1, representing (+) - spiro [1-azabicyclo [2.2.2] octane-3,5-oxazolidine] -2'-one, or its pharmaceutically acceptable acid addition salt, or enantiomer.

5. The compound according to claim 1, representing (-) - spiro [1-azabicyclo [2.2.2] octane-3,5'-oxazolidine] -2'-one, or its pharmaceutically acceptable acid addition salt, or enantiomer .

6. The compound according to claim 1, representing spiro [1-azabicyclo [2.2.2] heptane-3,5'-oxazolidin-2'-one], or its pharmaceutically acceptable acid addition salt, or enantiomer.

7. The compound according to claim 1, representing 3'-methyl-spiro [1-azabicyclo [2.2.2] octane-3,5'-oxazolidin-2'-one], or its pharmaceutically acceptable acid addition salt, or enantiomer.

8. A pharmaceutical composition comprising a compound as defined in any one of claims. 1-7, or its pharmaceutically acceptable acid addition salt or enantiomer in a mixture with a pharmaceutically acceptable diluent or carrier.

9. The compound according to any one of paragraphs. 1-7, or its pharmaceutically acceptable acid addition salt or enantiomer, for use as a pharmaceutical.

10. The use of compounds defined in any of paragraphs. 1-7, or its pharmaceutically acceptable acid addition salt or enantiomer, in the manufacture of medicines for treating or preventing psychotic disorders or disorders with impaired intelligence.

11. The use according to claim 10, wherein the disorder is schizophrenia, Alzheimer's disease, lack of learning ability, lack of cognitive function or disorders associated with hyperactivity and attention deficit.

12. The use of compounds defined in any of paragraphs. 1-7, or its pharmaceutically acceptable acid addition salt or enantiomer, in the manufacture of a medicament for treating or preventing anxiety or fear.

13. A method for preparing a compound of formula I as defined in claim 1 or a pharmaceutically acceptable acid addition salt or enantiomer thereof, which includes: (a) preparing a compound of formula I, in which R is hydrogen, by cyclizing the corresponding compound of formula II

in which n corresponds to the definition in paragraph 1; (b) obtaining the compounds of formula I by reaction of the corresponding compounds of formula III

in which n and R correspond to the definition in p. 1, with a compound that gives carbonyl; (c) obtaining the compounds of formula I, in which R represents methyl, by alkylation of the corresponding compounds of formula I, in which R represents hydrogen; or (d) obtaining a single enantiomer of a compound of formula I by isolating one enantiomer from a mixture of enantiomers; and, if desired or necessary, the conversion of the resulting compound of formula I or its acid addition salt or enantiomer into its pharmaceutically acceptable acid addition salt or enantiomer, or vice versa.

14. The compound of formula IV

in which n corresponds to the definition in p. 1, or its pharmaceutically acceptable acid addition salt or enantiomer.

15. The compound of formula III

in which n corresponds to the definition in p. 1, and R represents methyl, or its pharmaceutically acceptable acid addition salt or enantiomer.