IP Library Granted Patent US 8,153,841
Granted Patent B2
US 8,153,841 · App. 11/989,090 · Granted Apr 10, 2012

Compounds and their salts specific to the PPAR receptors and the EGF receptors and their use in the medical field

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Quick Facts
Patent No.
US 8,153,841
App. No.
11/989,090
Granted
Apr 10, 2012
Kind
B2
Abstract

The present invention relates to compounds comprising the general formula (I), in which R 1 and R 2 , which may be identical or different, are selected from the group comprising —H or a linear or branched alkyl group having from 1 to 6 carbon atoms or together form an aromatic or aliphatic ring with 5 or 6 atoms; Y and Z, which may be identical or different, are selected from the group comprising —H, —OH, —COOH, —OR 3 , —CH(OR 3 )COOH, in which R 3 is selected from H, phenyl, benzyl, —CF 3 or —CF 2 CF 3 , vinyl, allyl and a linear or branched alkyl group having from 1 to 6 carbon atoms.

Claims (29)

1. A compound of the general formula (I)

in which

R 1 and R 2 , which may be identical or different, are selected from the group consisting of —H or a linear or branched alkyl group having from 1 to 6 carbon atoms or together form an aromatic or aliphatic ring with 5 or 6 atoms;

Y is selected from the group consisting of —H, —OH, —COOH, —OR 3 , —CH(OR 3 )COOH, in which R 3 is selected from phenyl, benzyl, —CF 3 or —CF 2 CF 3 , vinyl, allyl and a linear or branched alkyl group having from 1 to 6 carbon atoms;

Z is selected from the group consisting of, —CH(OR 3 )COOH, in which R 3 is selected from phenyl, benzyl, —CF 3 or —CF 2 CF 3 , vinyl, allyl and a linear or branched alkyl group having from 1 to 6 carbon atoms; wherein —NR 1 R 2 is bonded at the 4-position;

and salts thereof.

2. A compound of claim 1 of the general formula (Ia)

in which

R 1 and R 2 , which may be identical or different, are selected from the group consisting of —H or a linear or branched alkyl group having from 1 to 6 carbon atoms;

Y is selected from the group consisting of —H, —OH, —OR 3 , —CH(OR 3 )COOH, in which R 3 is selected from a linear or branched alkyl group having from 1 to 6 carbon atoms; and

Z is —CH(OR 3 )COOH, in which R 3 is selected from phenyl, benzyl, —CF 3 or —CF 2 CF 3 , vinyl, allyl and a linear or branched alkyl group having from 1 to 6 carbon atoms.

3. A compound as claimed in claim 1 wherein the linear or branched alkyl group having from 1 to 6 carbon atoms is selected from —CH 3 , —CH 2 CH 3 , —CH(CH 3 ) 2 , and —CH 2 CH 2 CH 3 .

4. A compound as claimed in claim 1 wherein Y is H.

5. A compound as claimed in claim 1 wherein Z is —CH(OR 3 )COOH.

6. A compound as claimed in claim 1 wherein R 3 is —CH 3 .

7. A compound as claimed in claim 1 according to the following formula:

8. A compound according to the following formula:

9. A compound as claimed in claim 1 wherein R 3 is —CH 2 CH 3 .

10. A compound as claimed in claim 1 according to the following formula

11. A compound according to the following formula

12. A compound according to the following formula

13. A compound according to the following formula

14. A compound according to the following formula

15. A compound according to claim 1 in enantiomerically pure R or S form.

16. A pharmaceutical composition comprising one or more compounds as defined in claim 1 as active principles in combination with one or more pharmaceutically acceptable excipients or adjuvants.

17. A compound represented by:

or salts thereof.

18. A pharmaceutical composition comprising a compound of claim 17 and a pharmaceutically acceptable excipient.

19. The compound of claim 17 in an enantiomerically pure R or S form.

Assignments (1)
CHANGE OF NAME Recorded Nov 14, 2012
From: GIULIANI INTERNATIONAL LIMITED
To: NOGRA PHARMA LIMITED
Reel/Frame 029295/0861 →