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GRP119 RECEPTOR AGONISTS COUPLED TO PROTEIN G. PIRIDONA.
专利权人:
BRISTOL-MYERS SQUIBB COMPANY
发明人:
WACKER, DEAN A.,ROSSI, KAREN A.,WANG, YING
申请号:
ES08781867
公开号:
ES2371515T3
申请日:
2008.07.16
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound selected from the compounds of Formula I and Formula IA: and pharmaceutically acceptable enantiomers, diastereomers, solvates and salts thereof having a ring A and a ring B, in which: ring A is optionally substituted with one or more of R shown as R20 and R21; G is CH or N; Q is C or N; X is CH or N, with the proviso that Q and X are not both N; Y is CH2, N (R3), C (= O), O, OCR9R9, S, S (= O) or S (O) 2; n1 is 0-2; n2 is 0-2; n3 is 1-2; R1 is a 6-membered monocyclic aryl, a 5-membered monocyclic heteroaryl or a 6-membered monocyclic heteroaryl, each of which may be optionally substituted with one or more members selected from R1a, R1b, R1c, R1d and R1e; each of R1a, R1b, R1c, R1d and R1e is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, halo, - NH2, -CN, -NO2, -C (= O) OH, -C (= O) OR10, -OCF3, -OR11, -OH, -SH, -SR11r S (O) 3H, -P (O) 3H2, -C (= O) NR9R9, -NR12R12, -S (O) 2NR9R9, -NR9S (O) 2CF3, - C (= O) NR9S (O) 2R9, -S (O) 2NR9C (= O) OR9, -S (O) 2NR9C (= O) NR9R9, -C (= O) NR9S (O) 2CF3, -C (= O) R11, -NR9C (= O) H, - NR9C (= O) R10, -OC (= O) R10, -OC (= O) NR9R9, -C (= NR14) NR9R9, -NHC (= NR14) NR14R14, -S (= O) R11, -S (O) 2R11, - NR9C (= O) OR8 and -NR9S (O2) R8, in that: (a) each of the alkenyl, alkynyl, cycloalkyl, aryl and heterocyclyl may be optionally substituted with one or more of R6; and (b) the alkyl may be optionally substituted with one or more of R7; R2 is cycloalkyl, aryl, heteroaryl, heterocyclyl, -S (O) 2R5, -C (= O) NR3R5, -C (= O) R5 or -C (= O) OR5, in which each of the cycloalkyl, aryl, heteroaryl and heterocyclyl may be optionally substituted with one or more of R6; R3 is hydrogen, alkyl, alkoxy, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl; R5 is alkyl, alkenyl, aryl, cycloalkyl, heteroaryl or heterocyclyl, each of which may be optionally substituted with one or more of R6; R6, in each case, is independently
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