ECSP982497A - PROTEASE INHIBITORS V - Google Patents
PROTEASE INHIBITORS VInfo
- Publication number
- ECSP982497A ECSP982497A ECSP982497A ECSP982497A EC SP982497 A ECSP982497 A EC SP982497A EC SP982497 A ECSP982497 A EC SP982497A EC SP982497 A ECSP982497 A EC SP982497A
- Authority
- EC
- Ecuador
- Prior art keywords
- alkyl
- het
- alkenyl
- alkynyl
- co2nr
- Prior art date
Links
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 11
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000006529 (C3-C6) alkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 206010065687 Bone loss Diseases 0.000 abstract 1
- 102000004171 Cathepsin K Human genes 0.000 abstract 1
- 108090000625 Cathepsin K Proteins 0.000 abstract 1
- 102000005927 Cysteine Proteases Human genes 0.000 abstract 1
- 108010005843 Cysteine Proteases Proteins 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Esta invención se refiere a los compuestos según la fórmula (I) (gráfico), en la que: Y es Ar o NR1R2; R1 es R¿¿RC(O), R¿¿C(S), R¿¿SO2, R¿¿ OC(O), R¿¿R¿NC(O),ÓR¿¿R¿Nc(S); R2 e H, alquilo (C1-C6), alquinilo (C2--C6),Ar, alquilo (C0-C6)ó Het-alquilo C0-C6); R3 es H, alquenilo (C2-C6), alquinilo C2-C6), Het, Ar, o alquilo (C1-C6)opcionalmente sustituido con OR¿, SR¿, NR¿¿2, N(R¿)C(O)oR¿¿, CO2r¿, CO2NR¿2, N(C=NH)NH2, Het o Ar; R4 es H, alquilo (C1-C6), alquenilo (C2-C6), Ar-alquilo (C0-C6), o Het-alquilo (C0-C6), (gráfico), Ar-alquilo (C0-C6), Het-alquilo (C0-C6), adamntil-C(0)-, Ar-C(O)-, ó Het-C(0)-; R6 es R¿¿, R¿¿, R¿¿C(0), R¿¿c(S), R¿¿SO2, R¿¿OC(0), R¿¿OC(0), R¿¿OC(O), R¿¿R¿NC(0), R¿¿R¿¿NC(S), ó R¿¿OC(0)NR¿CH(R*)C(0); R7 es cicloalquil (C3-C6)-alquilo (C0-C6), Ar-alquilo (C0-C6), Het-alquilo (C0-C6), Ar-alcoxi (C0-C6), Het-alcoxi(C0-C6) o alquilo (C1-C6) opcionalmente sustituido con OR{, SR{, NR¿2, N(R¿), C(=)OR¿¿, CO2R¿, CO2NR¿2, N(N0NH)NH2, Het o Ar; R*e H, alquilo (C1-C6), alquenilo (C2-C6), cicloalquil (C3-C6)-alquilo (C0-C6), Ar-alquilo (C0-C6), Het-alquilo (C0-C6), cada R¿independientemente es H, alquilo (C1-C6), alquenilo (C2-C6), Ar-alquilo (C0-C6) o Het-alquilo (C0-C6), cicloalquil (C3-C6)-alquilo (C0-C6), Ar alquinilo (C0-C6), o Het-alquilo (C0-C6); R¿¿es H alquilo (C1-C6); Z es C(0) ó CH2; y n es 1,2 ó 3; o una sal aceptable farmacéuticamente de los mismos, que son inhibidores de proteasas de cisteína, en particular de la catepsina K, y los útiles en el tratamiento de enfermedades en las que la inhibición de la perdida ósea es un factor.This invention relates to compounds according to formula (I) (graph), wherein: Y is Ar or NR1R2; R1 is R¿¿RC (O), R¿¿ (S), R¿¿SO2, R¿¿ OC (O), R¿¿R¿NC (O), ÓR¿¿R¿Nc (S) ; R2 and H, (C1-C6) alkyl, (C2-C6) alkynyl, Ar, (C0-C6) alkyl or Het-C0-C6 alkyl); R3 is H, (C2-C6) alkenyl, C2-C6 alkynyl), Het, Ar, or (C1-C6) alkyl optionally substituted with OR¿, SR¿, NR¿¿2, N (R¿) C (O ) oR¿¿, CO2r¿, CO2NR¿2, N (C = NH) NH2, Het or Ar; R4 is H, (C1-C6) alkyl, (C2-C6) alkenyl, Ar (C0-C6) alkyl, or Het (C0-C6) alkyl, (graph), Ar (C0-C6) alkyl, Het-C0-C6-alkyl, Adamntyl-C (0) -, Ar-C (O) -, or Het-C (0) -; R6 is R¿¿, R¿¿, R¿¿ (0), R¿¿c (S), R¿¿SO2, R¿¿OC (0), R¿¿OC (0), R¿¿ OC (O), R¿¿R¿NC (0), R¿¿R¿¿NC (S), or R¿¿OC (0) NR¿CH (R *) C (0); R7 is (C3-C6) cycloalkyl-(C0-C6) alkyl, Ar-C0-C6 alkyl, Het-C0-C6 alkyl, Ar-C0-C6 alkoxy, Het-C0-C6 alkoxy ) or (C1-C6) alkyl optionally substituted with OR {, SR {, NR¿2, N (R¿), C (=) OR¿¿, CO2R¿, CO2NR¿2, N (N0NH) NH2, Het or Ar; R * and H, (C1-C6) alkyl, (C2-C6) alkenyl, (C3-C6) cycloalkyl (C0-C6) alkyl, Ar (C0-C6) alkyl, Het-(C0-C6) alkyl , each R¿independently is H, (C1-C6) alkyl, (C2-C6) alkenyl, Ar-(C0-C6) alkyl or Het-(C0-C6) alkyl, cyclo (C3-C6) -alkyl (C0) -C6), Ar (C0-C6) alkynyl, or Het-(C0-C6) alkyl; R¿¿ is H (C1-C6) alkyl; Z is C (0) or CH2; and n is 1,2 or 3; or a pharmaceutically acceptable salt thereof, which are inhibitors of cysteine proteases, particularly cathepsin K, and useful in the treatment of diseases in which inhibition of bone loss is a factor.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP982497 ECSP982497A (en) | 1998-05-06 | 1998-05-06 | PROTEASE INHIBITORS V |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP982497 ECSP982497A (en) | 1998-05-06 | 1998-05-06 | PROTEASE INHIBITORS V |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP982497A true ECSP982497A (en) | 1999-04-13 |
Family
ID=42043418
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP982497 ECSP982497A (en) | 1998-05-06 | 1998-05-06 | PROTEASE INHIBITORS V |
Country Status (1)
| Country | Link |
|---|---|
| EC (1) | ECSP982497A (en) |
-
1998
- 1998-05-06 EC ECSP982497 patent/ECSP982497A/en unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| MY116947A (en) | Protease inhibitors | |
| PL373299A1 (en) | Compounds containing lactam and their derivatives as factor Xa inhibitors | |
| NO995433L (en) | Protease inhibitors | |
| CY1111130T1 (en) | CATEGORY PROTECTION CATALOG Suspensions | |
| ECSP055696A (en) | 2-HYDROXI-1, 3-DIAMINOALCAN OIL | |
| ATE244227T1 (en) | 4,4'-DIAMINOSTILBENE-2,2'-DISULFONIC ACID DERIVATIVES | |
| PL361404A1 (en) | Synergistic combinations comprising a renin inhibitor for cardiovascular diseases | |
| DK0810209T3 (en) | Alpha and beta amino acid hydroxyethylaminosulfonamides for use as inhibitors of retroviral proteases | |
| ES2118710T3 (en) | NEW PEPTIDASE INHIBITORS. | |
| TR199901191T2 (en) | Use of benzamidoaldehydes as cysteine protease inhibitors. | |
| SG128491A1 (en) | Heterocyclic sulfonamide inhibitors of beta amyloid production | |
| NO973657L (en) | Thrombin inhibitors | |
| MXPA04002785A (en) | Substituted amines for the treatment of alzheimer's disease. | |
| BRPI0417345A (en) | azole-based kinase inhibiting compounds, compositions and their uses | |
| UY25143A1 (en) | PROCEDURE FOR THE PREPARATION OF PROTEASE INHIBITORS. | |
| CO5700776A2 (en) | USEFUL COMPOUNDS FOR THE TREATMENT OF DISEASES | |
| DE60224535D1 (en) | UNSYMMETRIC CYCLIC DIAMOND COMPOUND | |
| ATE326964T1 (en) | AMINO ACID DERIVATIVES FOR THE TREATMENT OF ALZHEIMER'S DISEASE | |
| AR021241A1 (en) | PROTEASE INHIBITORS | |
| MX9303587A (en) | PRODUCT FOR THE CARE OF CONTACT LENSES, FOR HARD OR SOFT CONTACT LENSES. | |
| ECSP982497A (en) | PROTEASE INHIBITORS V | |
| SE0102921D0 (en) | Pharmaceutically useful compounds | |
| UY26416A1 (en) | COMPOUNDS | |
| ECSP982495A (en) | PROTEASE INHIBITORS IV | |
| CR7720A (en) | 2-HYDROXI-1,3- DIAMINOALCANE OIL |