ECSP961987A - MATRIX METALOPROTEASE INHIBITORS (CASE RAN 4070/106) - Google Patents
MATRIX METALOPROTEASE INHIBITORS (CASE RAN 4070/106)Info
- Publication number
- ECSP961987A ECSP961987A ECSP961987A ECSP961987A EC SP961987 A ECSP961987 A EC SP961987A EC SP961987 A ECSP961987 A EC SP961987A EC SP961987 A ECSP961987 A EC SP961987A
- Authority
- EC
- Ecuador
- Prior art keywords
- cycloalkyl
- lower alkyl
- hydrogen
- heteroaralkyl
- heteroaryl
- Prior art date
Links
- 239000011159 matrix material Substances 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 12
- 125000000217 alkyl group Chemical group 0.000 abstract 11
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 8
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 7
- 125000004475 heteroaralkyl group Chemical group 0.000 abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 5
- -1 arylheteroalkyl Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 108030004510 Interstitial collagenases Proteins 0.000 abstract 1
- 102000000380 Matrix Metalloproteinase 1 Human genes 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000003475 metalloproteinase inhibitor Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Compuestos de la fórmula: (gráfico) en donde: n es 0, 1 o 2 Y es hidroxilo o XONH-donde X es hidrógeno o alquilo inferior, R1 es hidrógeno o alquilo inferior, R2 es hidrógeno, alquilo inferior, heteroalquilo, arilo, aralquilo, arilheteroalquilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroaralquilo, heteroarilheteroalquilo, heterociclo, heterociclo-alquilo inferior, heterociclo-heteroalquilo inferior o -NR5R7, donde: R6 es hidrógeno, alquilo inferior, cicloalquilo o cicloalquil alquilo, arilo, heteroarilo y heteroaralquilo; R7 es hidrógeno alquilo inferior, cicloalquilo o cicloalquil alquilo, arilo aralquilo, heteroarilo, heteroaralquilo, C(O)R8 -C(O)NR8R9, -SO2NR8R9 -SO2NR8R9, -SO2R10, ariloxicarbonilo, o alcoxicarbonilo; o R6 y R7 junto con el átomo de nitrógeno al que están unidos representan un grupo heterociclo; donde R8 y R9 son independientemente hidrógeno, alquilo inferior, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo o heteroalquilo; y R10 es alquilo inferior, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, heteroalquilo o heterociclo; o R1 y R2 junto con el tomo de carbono al que están unidos representan un grupo cicloalquilo o heterociclo; R3 es hidrógeno, alquilo inferior, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, heteroalquilo o alcoxilo inferior. R4 es hidrógeno, alquilo inferior, cicloalquilo, o cicloalquil-alquilo; o R2 y R3 junto a los carbonos a los que están unidos representan un grupo cicloalquilo, o heterociclo; o R3 y R4 junto con el carbono al que están unidos representan un grupo cicloalquilo, o y heterociclo; y R5 es alquilo inferior, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heteroarilo o heteroaralquilo; o sus sales farmacéuticamente aceptables o ésteres respectivos exhiben propiedades farmacológicas útiles, en particularpara empleo como inhibidores de metaloproteasa de matriz, partcularmente para colagenasas intersticiales.Compounds of the formula: (graph) where: n is 0, 1 or 2 Y is hydroxyl or XONH-where X is hydrogen or lower alkyl, R1 is hydrogen or lower alkyl, R2 is hydrogen, lower alkyl, heteroalkyl, aryl, aralkyl, arylheteroalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroaralkyl, heteroarylheteroalkyl, heterocycle, heterocyclo-lower alkyl, heterocyclo-lower heteroalkyl or -NR5R7, where: R6 is hydrogen, lower alkyl, cycloalkyl or cycloalkyl, hetero; R7 is hydrogen lower alkyl, cycloalkyl or cycloalkyl alkyl, aryl aralkyl, heteroaryl, heteroaralkyl, C (O) R8 -C (O) NR8R9, -SO2NR8R9 -SO2NR8R9, -SO2R10, aryloxycarbonyl, or alkoxycarbonyl; or R6 and R7 together with the nitrogen atom to which they are attached represent a heterocycle group; where R8 and R9 are independently hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl or heteroalkyl; and R10 is lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heteroalkyl, or heterocycle; or R1 and R2 together with the carbon atom to which they are attached represent a cycloalkyl or heterocycle group; R3 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heteroalkyl, or lower alkoxy. R4 is hydrogen, lower alkyl, cycloalkyl, or cycloalkyl-alkyl; or R2 and R3 together with the carbons to which they are attached represent a cycloalkyl group, or heterocycle; or R3 and R4 together with the carbon to which they are attached represent a cycloalkyl group, or and heterocycle; and R5 is lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; or their respective pharmaceutically acceptable salts or esters exhibit useful pharmacological properties, in particular for use as matrix metalloprotease inhibitors, particularly for interstitial collagenases.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP961987 ECSP961987A (en) | 1996-12-20 | 1996-12-20 | MATRIX METALOPROTEASE INHIBITORS (CASE RAN 4070/106) |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP961987 ECSP961987A (en) | 1996-12-20 | 1996-12-20 | MATRIX METALOPROTEASE INHIBITORS (CASE RAN 4070/106) |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP961987A true ECSP961987A (en) | 1998-07-23 |
Family
ID=42042714
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP961987 ECSP961987A (en) | 1996-12-20 | 1996-12-20 | MATRIX METALOPROTEASE INHIBITORS (CASE RAN 4070/106) |
Country Status (1)
| Country | Link |
|---|---|
| EC (1) | ECSP961987A (en) |
-
1996
- 1996-12-20 EC ECSP961987 patent/ECSP961987A/en unknown
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