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Dipeptidyl peptidase IV inhibitors based on cyclopropyl condensed pyrrolidine, preparation process and use thereof
专利权人:
BRISTOL-MYERS SQUIBB COMPANY
发明人:
ROBL, JEFFREY A.,SULSKY, RICHARD B.,AUGERI, DAVID J.,MAGNIN, DAVID R.,HAMANN, LAWRENCE G.,BETEBENNER, DAVID A.
申请号:
ES05005368
公开号:
ES2456667T3
申请日:
2001.03.05
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound that has the structure. where x is 0 or 1 and y is 0 or 1, with the proviso that x>; = 1 when y>; = 0 and x>; = 0 when y>; = 1; and in which n is 0 or 1; X is H; R1 R2, R3 and R4 are the same or different and are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, bicycloalkyl, tricycloalkyl, alkylcycloalkyl, hydroxyalkyl, hydroxyalkylcycloalkyl, hydroxycycloalkyl, hydroxyalkylcycloalkyl, cycloalkylcycloalkyl, alkylcycloalkyl, alkylcycloalkyl, alkyl , aryl, aralkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl or cycloheteroalkylalkyl; all optionally substituted through available carbon atoms with 1, 2, 3, 4 or 5 groups selected from hydrogen, halo, alkyl, polyhaloalkyl, alkoxy, haloalkoxy, polyhaloalkoxy, alkoxycarbonyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, polycycloalkyl, heteroarylamino , arylamino, cycloheteroalkyl, cycloheteroalkylalkyl, hydroxy, hydroxyalkyl, nitro, cyano, amino, substituted amino, alkylamino, dialkylamino, thiol, alkylthio, alkylcarbonyl, acyl, alkoxycarbonyl, aminocarbonyl, alkynylaminocarbonyl, alkylaminocarbonyl, alkenylaminocarbonyl, alkylcarbonyloxy, alkylcarbonylamino, arylcarbonylamino, alkylsulfonylamino, alkylaminocarbonylamino, alkoxycarbonylamino, alkylsulfonyl, aminosulfinyl, aminosulfonyl, alkylsulfinyl, sulfonamido or sulfonyl; and R1 and R3 can optionally be taken together to form - (CR5R6) m- in which m is from 2 to 6, and R5 and R6 are the same or different and are independently selected from hydroxy, alkoxy, H, alkyl, alkenyl, alkynyl , cycloalkyl, halo, amino, substituted amino, cycloalkylalkyl, cycloalkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl, alkyloxylamino, arylcarbonylamino, alkoxycarbonylamino, aryloxycarbonylamino alkoxycarbonyl, or may together take R4 or arylamino, or together, may take R4 together (CR7R8) p- in which p is from 2 to 6, and R7 and R8 are the same or different and are independently
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