ECSP982724A - DIPEPTIDE NITRILS - Google Patents
DIPEPTIDE NITRILSInfo
- Publication number
- ECSP982724A ECSP982724A ECSP982724A ECSP982724A EC SP982724 A ECSP982724 A EC SP982724A EC SP982724 A ECSP982724 A EC SP982724A EC SP982724 A ECSP982724 A EC SP982724A
- Authority
- EC
- Ecuador
- Prior art keywords
- cathepsins
- inhibitors
- cathepsin
- cysteine
- compounds
- Prior art date
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Los nitrilos de dipéptido N-terminal-sustituidos como se definen, son útiles como inhibidores de catepsinas de cisteína, poe ejemplo, catepsinasB, K, L, YS, Y se pueden utilizar para el tratamiento de enfermedades y condiciones dependientes de catepsinas de cisteína, incluyendo inflamación, artritis reumatoide, osteoartritis, esteoporosis, tumores (especialmente invación tumoral y metástasis tumoral), enfermedad coronaria, ateroesclerosis (incluyendo ruptura y desestabilización de la placa ateroesclerótica). Los nitrilos de dipéptido particulares son compuestos de la fórmula I, o ésteres fisiológicamente aceptables y disociables o sales de los mismos, (gráfico), en donde: los simbolos son como se definen. En particular, se ha descubierto que mediante la elección apropiada de los grupos R, R2, R3, R4, R5, X1 Y y L, se puede alterar la selectividad relativa de los compuestos como inhibidores de los diferentes tipos de catepsinas de cisteína, por ejemplo, las catepsinas B, K, L y S por ejemplo, para obtener inhibidores que inhiban selectivamente un tipo de catepsinas particular, o una combinación de tipos de catepsinas.N-terminal-substituted dipeptide nitriles as defined are useful as inhibitors of cysteine cathepsins, eg cathepsins B, K, L, YS, Y can be used for the treatment of cysteine cathepsin-dependent diseases and conditions, including inflammation, rheumatoid arthritis, osteoarthritis, steoporosis, tumors (especially tumor invasion and tumor metastasis), coronary heart disease, atherosclerosis (including atherosclerotic plaque rupture and destabilization). Particular dipeptide nitriles are compounds of formula I, or dissociable physiologically acceptable esters or salts thereof, (graph), wherein: the symbols are as defined. In particular, it has been discovered that by appropriately choosing the groups R, R2, R3, R4, R5, X1 Y and L, the relative selectivity of the compounds as inhibitors of the different types of cysteine cathepsins can be altered, by For example, cathepsins B, K, L and S for example, to obtain inhibitors that selectively inhibit a particular cathepsin type, or a combination of cathepsin types.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP982724 ECSP982724A (en) | 1998-11-04 | 1998-11-04 | DIPEPTIDE NITRILS |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP982724 ECSP982724A (en) | 1998-11-04 | 1998-11-04 | DIPEPTIDE NITRILS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP982724A true ECSP982724A (en) | 1999-04-21 |
Family
ID=42043642
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP982724 ECSP982724A (en) | 1998-11-04 | 1998-11-04 | DIPEPTIDE NITRILS |
Country Status (1)
| Country | Link |
|---|---|
| EC (1) | ECSP982724A (en) |
-
1998
- 1998-11-04 EC ECSP982724 patent/ECSP982724A/en unknown
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