主权项 |
1. A combination comprising (a) a phosphatidylinositol 3-kinase inhibitor selected from the group consisting of the compound of formula (I), wherein R1 is naphthyl or phenyl wherein said phenyl is substituted by one or two substituents independently selected from the group consisting of Halogen; lower alkyl unsubstituted or substituted by halogen, cyano, imidazolyl or triazolyl; cycloalkyl; amino substituted by one or two substituents independently selected from the group consisting of lower alkyl, lower alkyl sulfonyl, lower alkoxy and lower alkoxy lower alkylamino; piperazinyl unsubstituted or substituted by one or two substituents independently selected from the group consisting of lower alkyl and lower alkyl sulfonyl; 2-oxo-pyrrolidinyl; lower alkoxy lower alkyl; imidazolyl; pyrazolyl; and triazolyl; R2 is O or S; R3 is lower alkyl; R4 is pyridyl unsubstituted or substituted by halogen, cyano, lower alkyl, lower alkoxy or piperazinyl unsubstituted or substituted by lower alkyl; pyrimidinyl unsubstituted or substituted by lower alkoxy; quinolinyl unsubstituted or substituted by halogen; quinoxalinyl; or phenyl substituted with alkoxy R5 is hydrogen or halogen; n is 0 or 1; R6 is oxido; with the proviso that if n=1, the N-atom bearing the radical R6 has a positive charge; R7 is hydrogen or amino;or compound of formula (II), wherein W is CRw or N, wherein
Rw is selected from the group consisting of:
(1) hydrogen,(2) cyano,(3) halogen,(4) methyl,5) trifluoromethyl,(6) sulfonamide;R1 is selected from the group consisting of:
(1) hydrogen,(2) cyano,(3) nitro,(4) halogen,(5) substituted and unsubstituted alkyl,(6) substituted and unsubstituted alkenyl,(7) substituted and unsubstituted alkynyl,(8) substituted and unsubstituted aryl,(9) substituted and unsubstituted heteroaryl,(10) substituted and unsubstituted heterocyclyl,(11) substituted and unsubstituted cycloalkyl,(12) —COR1a,(13) —CO2R1a,(14) —CONR1aR1b,(15) —NR1aR1b,(16) —NR1aCOR1b,(17) —NR1aSO2R1b,(18) —OCOR1a,(19) —OR1a,(20) —SR1a,(21) —SOR1a,(23) —SO2NRIaR1b whereinR1a, and R1b are independently selected from the group consisting of:
(a) hydrogen,(b) substituted or unsubstituted alkyl,(c) substituted and unsubstituted aryl,(d) substituted and unsubstituted heteroaryl,(e) substituted and unsubstituted heterocyclyl, and(f) substituted and unsubstituted cycloalkyl;R2 is selected from the group consisting of:
(1) hydrogen,(2) cyano,(3) nitro,(4) halogen,(5) hydroxy,(6) amino,(7) substituted and unsubstituted alkyl,(8) —COR2a, and(9) —NR2aCOR2b, whereinR2a, and R2b are independently selected from the group consisting of:
(a) hydrogen, and(b) substituted or unsubstituted alkyl;R3 is selected from the group consisting of:
(1) hydrogen,(2) cyano,(3) nitro,(4) halogen,(5) substituted and unsubstituted alkyl,(6) substituted and unsubstituted alkenyl,(7) substituted and unsubstituted alkynyl,(8) substituted and unsubstituted aryl,(9) substituted and unsubstituted heteroaryl,(10) substituted and unsubstituted heterocyclyl,(11) substituted and unsubstituted cycloalkyl,(12) —COR3a,(14) —NR3aR3b (13) —NR3aCOR3b,(15) —NR3aSO2R3b,(16) —OR3a,(17) —SR3a,(18) —SOR3a,(19) —SO2R3a, whereinR3a, and R3b are independently selected from the group consisting of:
(a) hydrogen,(b) substituted or unsubstituted alkyl,(c) substituted and unsubstituted aryl,(d) substituted and unsubstituted heteroaryl,(e) substituted and unsubstituted heterocyclyl, and(f) substituted and unsubstituted cycloalkyl; andR4 is selected from the group consisting of
(1) hydrogen, and(2) halogen,or a pharmaceutically acceptable salt thereof, and (b) a 17α-Hydroxylase/C17,20-lyase inhibitor or pharmaceutically acceptable salt thereof. |