ECSP961987A - MATRIX METALOPROTEASE INHIBITORS (CASE RAN 4070/106) - Google Patents

MATRIX METALOPROTEASE INHIBITORS (CASE RAN 4070/106)

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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
Application number
Other languages
Spanish (es)
Inventor
Chris Allen Broka
Steven Lee Bender
Jeffrey Allen Campbell
Arlindo Lucas Castelhano
Lawrence Emerson Fisher
Robert Than Hendricks
Keshab Sarma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed filed Critical
Priority to ECSP961987 priority Critical patent/ECSP961987A/en
Publication of ECSP961987A publication Critical patent/ECSP961987A/en

Links

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.

ECSP961987 1996-12-20 1996-12-20 MATRIX METALOPROTEASE INHIBITORS (CASE RAN 4070/106) ECSP961987A (en)

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)

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