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
- 108010016626 Dipeptides Proteins 0.000 title abstract 3
- 102000005600 Cathepsins Human genes 0.000 abstract 7
- 108010084457 Cathepsins Proteins 0.000 abstract 7
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 abstract 3
- 235000018417 cysteine Nutrition 0.000 abstract 3
- 239000003112 inhibitor Substances 0.000 abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000002825 nitriles Chemical class 0.000 abstract 2
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 208000037260 Atherosclerotic Plaque Diseases 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010027476 Metastases Diseases 0.000 abstract 1
- 206010064390 Tumour invasion Diseases 0.000 abstract 1
- 230000009400 cancer invasion Effects 0.000 abstract 1
- 208000029078 coronary artery disease Diseases 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- 230000001687 destabilization Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 230000009401 metastasis Effects 0.000 abstract 1
- 201000008482 osteoarthritis Diseases 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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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