IP Library › Granted Patent US 7,858,603
Granted Patent B2
US 7,858,603 · App. 10/548,473 · Granted Dec 28, 2010

Use of derivatives of cholest-4-en-3-one as medicaments, pharmaceutical compositions containing same, novel derivatives and preparation method thereof

Assignee: TROPHOS
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Quick Facts
Patent No.
US 7,858,603
App. No.
10/548,473
Granted
Dec 28, 2010
Kind
B2
Abstract

Compound of formula I where X=O or ═N—OH group, R represents a group chosen from A=hydrogen or together with B a carbon-carbon bond, B=hydrogen, hydroxy or together with A a carbon-carbon bond, C, D, E, F=hydrogen or together with D a carbon-carbon bond, or the one of its addition salts with pharmaceutically acceptable acids, with the exception of a few compounds, as a medicament, use in particular as neuroprotectors, novel compounds of formula I and pharmaceutical compositions.

Claims (26)

1. A pharmaceutical compound corresponding to the formula I

in which X represents an ═N—OH group,

R represents a group chosen from

A represents a hydrogen atom or together with B a carbon-carbon bond,

B represents a hydrogen atom, a hydroxy group or together with A a carbon-carbon bond,

C represents a hydrogen atom or together with D a carbon-carbon bond,

D represents a hydrogen atom or together with C a carbon-carbon bond,

E represents a hydrogen atom or together with F a carbon-carbon bond,

F represents a hydrogen atom or together with E a carbon-carbon bond,

or one of its addition salts with pharmaceutically acceptable acids,

with the exception of, cholest-4-en-3-one oxime, stigmast 4-en-3-one oxime, cholest-1-en-3-one oxime, cholestan-3-one-oxime, cholesta-4,6-dien-3-one oxime, 5α-stigmastan-3-one oxime and 5α-stigmast-22-en-3-one oxime.

2. A pharmaceutical compound according to claim 1 characterized in that in formula I, A represents together with B a carbon-carbon bond, C, D, represent a hydrogen atom, E, F represent a hydrogen atom or together a carbon-carbon bond and R has the meaning R1, or one of its addition salts with pharmaceutically acceptable acids, with the exception of cholest-4-en-3-one oxime.

3. A pharmaceutical compound according to claim 1 characterized in that in formula I, A represents together with B a carbon-carbon bond, C, D represent a hydrogen atom, E, F represent a hydrogen atom and R has the meaning R2, R3 or R4, or one of its addition salts with pharmaceutically acceptable acids.

4. A pharmaceutical compound according to claim 1 characterized in that in formula I, A represents together with B a double bond, C represents together with D a carbon-carbon bond, E, F represent a hydrogen atom and R has the meaning R1 or R6, or one of its addition salts with pharmaceutically acceptable acids.

5. A pharmaceutical compound according to claim 1 characterized in that in formula I, A represents together with B a carbon-carbon bond, C represents together with D a carbon-carbon bond, E represents together with F a carbon-carbon bond and R has the meaning R1, or one of its addition salts with pharmaceutically acceptable acids.

6. A pharmaceutical composition comprising, as active ingredient, at least one of the compounds defined in claim 1 in a pharmaceutically effective amount, as well as a pharmaceutically acceptable excipient.

7. A pharmaceutical composition comprising, as active ingredient, at least one of the compounds defined in claim 2 in a pharmaceutically effective amount, as well as a pharmaceutically acceptable excipient.

8. A pharmaceutical composition comprising, as active ingredient, at least one of the compounds defined in claim 3 in a pharmaceutically effective amount, as well as a pharmaceutically acceptable excipient.

9. A pharmaceutical composition comprising, as active ingredient, at least one of the compounds defined in claim 4 in a pharmaceutically effective amount, as well as a pharmaceutically acceptable excipient.

10. A pharmaceutical composition comprising, as active ingredient, at least one of the compounds defined in claim 5 in a pharmaceutically effective amount, as well as a pharmaceutically acceptable excipient.

11. A pharmaceutical composition comprising, as active ingredient, at least one of the compounds defined in claim 6 in a pharmaceutically effective amount, as well as a pharmaceutically acceptable excipient.

12. A medicament comprising at least one compound according to claim 1 characterized in that in formula I A represents together with B a carbon-carbon bond, C, D, represent a hydrogen atom, E, F represent a hydrogen atom or together a carbon-carbon bond and R has the meaning R1, or one of its addition salts with pharmaceutically acceptable acids.

13. A medicament comprising at least one compound according to claim 1 characterized in that in formula I, A represents together with B a carbon-carbon bond, C, D represent a hydrogen atom, E, F represent a hydrogen atom and R has the meaning R2 or R3 or R4, or one of its addition salts with pharmaceutically acceptable acids.

14. A medicament comprising at least one compound according to claim 1 characterized in that in formula I, A represents together with B a double bond, C represents together with D a carbon-carbon bond, E, F represent a hydrogen atom and R has the meaning R1 or R6, or one of its addition salts with pharmaceutically acceptable acids.

15. A medicament comprising at least one compound according to claim 1 characterized in that in formula I, A represents together with B a carbon-carbon bond, C represents together with D a carbon-carbon bond, E represents together with F a carbon-carbon bond represent a hydrogen atom and R has the meaning R1, or one of its addition salts with pharmaceutically acceptable acids.

16. A medicament comprising at least one compound according to claim 1 characterized in that in formula I, E represents together with F a carbon-carbon bond, C, D, A, B, represent a hydrogen atom and R has the meaning R1, or one of its addition salts with pharmaceutically acceptable acids.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 24, 2009
From: BORDET, THIERRY; DROUOT, CYRILLE; BUISSON, BRUNO
To: TROPHOS
Reel/Frame 022867/0635 →
Priority Claims (2)
FR 03 02992 · Mar 11, 2003 · national
FR 03 11324 · Sep 26, 2003 · national
Continuity (1)
Related Publication 20060217358A1 · Sep 28, 2006