A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/343 (2006.01) A61P 7/02 (2006.01) C07C 251/60 (2006.01) C07D 307/81 (2006.01)
Patent
CA 2538574
The present invention relates to benzofuryl-oximes of formula (I) or a pharmaceutically acceptable salt or ester form thereof wherein R1 is a direct bond to A, C1-C4 alkylene, or -O-C1-C4 alkylene; R2 and R3 are, independently hydrogen, halogen, C1-C4 alkyl, C1-C3 perfluoroalkyl, -O-C1-C3 perfluoroalkyl, C1-C3 alkoxy, -OH, -NH2, -NO2, -O(CH2)p-aryl, -O(CH2)P-heteroaryl, aryl, heteroaryl, -NH(CH2)P-aryl, -NH(CH2)P-heteroaryl, -NH(CO)-aryl, NH(CO)- heteroaryl, -O(CO)-aryl, O(CO)-heteroaryl, -NH(CO)-CH=CH-aryl, or -NH(CO)- CH=CH-heteroaryl; p is an integer from 0-6; R4 is hydrogen, C1-C8 alkyl, or C3- C6 cycloalkyl; A is -COOH or an acid mimic; X is C1-C8 alkylène, C3-C6 cycloalkylene, -(CH2)mO-, or -(CH2)mNH-; m is an integer from 1-6; and R5 is hydrogen, C1-C8 alkyl, C3-C6 alkyl, C3-C6 cycloalkyl, -CH2-C3-C6 cycloalkyl, heteroaryl, -CH2-heteroaryl, aryl or benzyl; R6 and R7 are independently, hydrogen, halogen, C1-C6 alkyl, C1-C6 perfluoroalkyl, -O-C1-C6 perfluoroalkyl, C1-C6 alkoxy, _OH, -NH2, -NO2, -O(CH2)n-aryl, -O(CH2)n-heteroaryl, aryl, or heteroaryl; and n is an integer from 0-6, wherein the alkyl, cycloalkyl, aryl and heteroaryl groups are each optionally substituted by one or more substituents. The present compounds are PAI-1 inhibitors for the treatment e.g of impairment of the fibrinolytic system, thrombosis or cardiovascular diseases.
La présente invention concerne des benzofuryl-oximes de formule (I) ou un sel pharmaceutiquement acceptable ou une forme estérique desdits composés. Dans ladite formule, R¿1? est directement lié à A, alkylène C¿1?-C¿4? ou alkylène -O-C¿1?-C¿4?; R¿2? et R¿3? sont, indépendamment, hydrogène, halogène, alkyle C¿1?-C¿4?, perfluoroalkyle C¿1?-C¿3? perfluoroalkyle, perfluoroalkyle -O-C¿1?-C¿3?, alcoxy C¿1?-C¿3?, OH, -NH¿2?, -NO¿2?, -O(CH¿2?)¿p?-aryle, -O(CH¿2?)<SB>P</SB>-hétéroaryle, aryle, hétéroaryle, -NH(CH¿2?)<SB>P</SB>-aryle, -NH(CH¿2?)<SB>P</SB>-hétéroaryle, -NH(CO)-aryle, NH(CO)-hétéroaryle, -O(CO)-aryle, O(CO)-hétéroaryle, -NH(CO)-CH=CH-aryle ou -NH(CO)-CH=CH-hétéroaryle; p est un entier compris entre 0 et 6; R¿4? est hydrogène, alkyle C¿1?-C¿8? ou cycloalkyle C¿3?-C¿6?; A est -COOH ou un analogue de l'acide; X est alkylène C¿1?-C¿8?, cycloalkylène C¿3?-C¿6?, -(CH¿2?)¿m?O- ou -CH¿2?)¿m?NH-; m est un entier compris entre 0 et 6; et R¿5? est hydrogène, alkyle C¿1?-C¿8?, alkyle C¿3?-C¿6?, cycloalkyle C¿3?-C¿6?, cycloalkyle -CH¿2?-C¿3?-C¿6?, hétéroaryle, -CH¿2?-hétéroaryle, aryle ou benzyle; R¿6? et R¿7? sont, indépendamment, hydrogène, halogène, alkyle C¿1?-C¿6?, perfluoroalkyle C¿1?-C¿6?, perfluoroalkyle -O-C¿1?-C¿6?, alcoxy C¿1?-C¿6?, -OH, -NH¿2?, -NO?2¿, -O(CH¿2?)¿n?-aryle, -O(CH¿2?)¿n?-hétéroaryle, aryle ou hétéroaryle; et n est un entier compris entre 0 et 6; les groupes alkyle, cycloalkyle, aryle et hétéroaryle étant chacun éventuellement susbstitués par un ou plusieurs susbstituants. Les composés de l'invention sont des inhibiteurs de PAI-1 destinés au traitement, par exemple, d'une déficience du système fibrinolytique, de la thrombose ou de maladies cardiovasculaire.
Butera John Anthony
Elokdah Hassan Mahmoud
Gundersen Eric Gould
Havran Lisa Marie
Jenkins Douglas John
Torys Llp
Wyeth
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