3-aminopyrazole-substituted tricyclic n as PDGF receptor inhibitors.
2003
A compound of Formula (I): ** ** see formula wherein n is an integer of 1 to 4; R1 is selected from the group consisting of hydrogen, lower alkyl, -OH, alkoxy, -oxo, -NH2, -NH (alkyl) and -N (alkyl) 2; ** ** see formula is selected from the group consisting of an aryl, a monocyclic heteroaryl five to six members, a benzofused heteroaryl nine to ten membered benzo-fused heterocycloalkyl one group of nine to ten membered benzo-fused cycloalkyl group and of nine to ten members; wherein the heteroaryl group benzofused benzofused heterocycloalkyl, benzofused cycloalkyl or is attached to the molecule such that the phenyl ring is bound directly to the portion ** ** see formula of the molecule; p is an integer from 0 to 2; R2 is selected from the group consisting ** ** see formula and -X-A1-Y-A2; wherein X and Y are each independently absent or selected from the group consisting of -O-, -NH-, -N (alkyl) -, -S-, -SO-, -SO2-, -OC (= O ), -C (= O) O-, -NH (= O) -, -N (alkyl) C (= O) -, -C (= O) NH-, -C (= O) N (alkyl) -, -OC (= O) O-, -NHC (= O) O-, -OC (= O) NH-, -N (alkyl) C (= O) O-, -OC (= O) N ( alkyl) -, -NHC (= O) NH-, -NHC (= O) N (alkyl) -, -N (alkyl) C (= O) NH-, -N (alkyl) C (= O) N ( alkyl) -, -NHSO2-, -SO2NH-, -N (alkyl) SO2- and -SO2N (alkyl) -; A1 is absent or selected from alkyl or alkenyl; A2 is selected from alkyl, alkenyl, or H; wherein, when A1 or A2 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from halogen, cyano, hydroxy, alkoxy, thio, halogenated alkoxy, -OC (= O) alkyl, - OC (= O) Oalkyl, amino, alkylamino, -NHC (= O) alkyl, -N (alkyl) C (= O) alkyl, dialkylamino, -NHC (= O) NH2, -NHC (= O) NHalkyl, - N (alkyl) C (= O) NHalkyl, -N (alkyl) C (= O) NH2, -OC (= O) NHalkyl, -NHC (= O) O-, -N (alkyl) C (= O) OC , -NHSO2alquilo, -N (alkyl) SO 2 alkyl, thioalkyl, halogenated thioalkyl, -SO 2, -SO 2 halogen, -NHC (= O) N (alkyl) 2, -N (alkyl) C (= O) N (alkyl) 2 or -OC (= O) N (alkyl) 2; ** ** see formula is selected from the group consisting of an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a cycloalkyl benzofused nine to ten membered benzo-fused heterocycloalkyl and nine to ten members; wherein the aryl, cycloalkyl, carbocyclic partially unsaturated, heteroaryl, heterocycloalkyl, cycloalkyl benzofused or benzofused heterocycloalkyl, is optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC (= O) alkyl, -N (alkyl) C (= O) alkyl, or dialkylamino, -NHC (= O) NH2, -NHC (= O) NHalkyl, -N (alkyl ) C (= O) NHalkyl, -OC (= O) NHalkyl, -NHC (= O) O-, -N (alkyl) C (= O) O, -NHSO2alquilo, -N (alkyl) SO 2 alkyl, thioalkyl, halogenated thioalkyl , -SO2, -SO2 halogenated, -NHC (= O) N (alkyl) 2, -N (alkyl) C (= O) N (alkyl) 2 or -OC (= O) N (alkyl) 2; q is an integer of 0 to 4; R3 is selected from the group consisting of halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkyloxy, alkylamino, -NHC (= O) alkyl, -N (alkyl) C (= O) alkyl, or dialkylamino, -NHC (= O) NH2, -NHC (= O) NHalkyl, -N (alkyl) C (= O) NHalkyl, -OC (= O) NHalkyl, -NHC (= O) O-, - N (alkyl) C (= O) O, -NHSO2alquilo, -N (alkyl) SO 2 alkyl, thioalkyl, halogenated thioalkyl, -SO 2, -SO 2 halogen, -NHC (= O) N (alkyl) 2, -N (alkyl) C (= O) N (alkyl) 2 and -OC (= O) N (alkyl) 2; provided that the sum of p and q is an integer of 0 to 4; L1 is absent or selected from the group consisting of alkyl; ** ** see formula is selected from the group consisting of an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a cycloalkyl benzofused nine to ten membered benzo-fused heterocycloalkyl and nine to ten members; or one of their optical isomers, enantiomers, diastereomers, racemates, or pharmaceutically acceptable salts; where "alkyl" means an alkyl group of straight or branched chain having 1 to 10 carbon atoms; "Alkoxy" and "alkyloxy" mean a radical ether oxygen of said alkyl group; "Lower alkyl" means an alkyl group of straight or branched chain alkyl having 1 to 4 carbon atoms; "Lower alkoxy" and "lower alkyloxy" mean a radical ether oxygen of said lower alkyl group; "Aryl" means phenyl, naphthyl or fluorenyl; "Heteroaryl" means an aromatic ring structure of monocyclic or bicyclic five to ten membered containing carbon atoms and at least one heteroatom selected from the group consisting of O, N and S; "Cycloalkyl" means a saturated ring system, three to ten members; "Heterocycloalkyl" means a ring structure saturated or partially unsaturated, monocyclic or bicyclic five- to ten-membered ring containing carbon atoms and at least one heteroatom selected from the group consisting of O, N and S; and "partially unsaturated carbocycle" means a partially unsaturated ring system, five to ten membered ring containing at least one unsaturated bond.
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