Title:
USE OF BIPHENYL-DERIVED THIAMIDES AS CALPAIN INHIBITORS
Document Type and Number:
WIPO Patent Application WO/2005/108354
Kind Code:
A1
Abstract:
The invention relates to biphenyl-derived compounds having a calpain inhibitor activity. One of the inventive compounds is a 2,2'-disubstituted biphenyl, with the substituents at positions 2 and 2' of the biphenyl skeleton being chains containing structures that are associated with amino acids, including fragments of aminocarbonyl compounds, whereby at least one of the substituents at positions 2 or 2' is attached to the biphenyl skeleton by a thiocarbonyl group, said compounds having a thioamide functionality. The invention also relates to all of the conformational isomers (atropisomers) of the aforementioned compound having formula (I). Compounds having formula (I) can be used for the preventive or therapeutic treatment of a degenerative disease.
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Inventors:
HERRADON GARCIA BERNARDO (ES)
ALONSO GINER MERCEDES (ES)
BENITO CANO ESPERANZA (ES)
CHANA LOPEZ ANTONIO (ES)
MONTERO AGUADO ANA (ES)
ALONSO GINER MERCEDES (ES)
BENITO CANO ESPERANZA (ES)
CHANA LOPEZ ANTONIO (ES)
MONTERO AGUADO ANA (ES)
Application Number:
PCT/ES2005/070058
Publication Date:
November 17, 2005
Filing Date:
May 06, 2005
Export Citation:
Assignee:
CONSEJO SUPERIOR INVESTIGACION (ES)
HERRADON GARCIA BERNARDO (ES)
ALONSO GINER MERCEDES (ES)
BENITO CANO ESPERANZA (ES)
CHANA LOPEZ ANTONIO (ES)
MONTERO AGUADO ANA (ES)
HERRADON GARCIA BERNARDO (ES)
ALONSO GINER MERCEDES (ES)
BENITO CANO ESPERANZA (ES)
CHANA LOPEZ ANTONIO (ES)
MONTERO AGUADO ANA (ES)
International Classes:
A61K31/145; A61K31/165; A61K38/04; C07C233/64; C07C327/38; C07C327/48; C07K5/02; (IPC1-7): C07C327/38; A61K31/145; A61K31/165; A61K38/04; C07C233/64; C07C327/48; C07K5/02
Domestic Patent References:
| WO2004101494A1 | 2004-11-25 | |||
| WO2003014088A1 | 2003-02-20 |
Foreign References:
| US5554767A | 1996-09-10 |
Other References:
MONTERO A ET AL: "Studies on aromatic compounds: inhibition of calpain I by biphenyl derivatives and peptide-biphenyl hybrids.", BIOORGANIC & MEDICINAL CHEM., vol. 14, no. 11, June 2004 (2004-06-01), pages 2735 - 2757, XP004841282
MONTERO A ET AL: "Peptide-biphenyl hybrids as calpain inhibitors.", CHEM & BIODIV., vol. 1, no. 3, March 2004 (2004-03-01), pages 442 - 457, XP008073096
MANN E ET AL: "Synthesis and Crystal Structure of Peptide-2, 2'-Biphenyl Hybrids.", HELV CHIM ACTA., vol. 85, no. 11, 2002, pages 3624 - 3638, XP008073094
MONTERO A ET AL: "Peptide-biphenyl hybrids as calpain inhibitors.", CHEM & BIODIV., vol. 1, no. 3, March 2004 (2004-03-01), pages 442 - 457, XP008073096
MANN E ET AL: "Synthesis and Crystal Structure of Peptide-2, 2'-Biphenyl Hybrids.", HELV CHIM ACTA., vol. 85, no. 11, 2002, pages 3624 - 3638, XP008073094
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