| 主权项 |
1. A compound of the Formula (I) or a pharmaceutically acceptable salt thereof, wherein: X1 is C(R2) or N; X2 is O, S, S(O), S(O)2, CH2, or C(O); R1 is H, C1-C3 alkyl, or C1-C3 alkyl substituted by hydroxy; R2 is H, halo, or C1-C3 alkyl; R3 is selected from the group consisting of:
(a.) H;(b.) C1-C6 alkyl;(c.) —(C(Ra)2)n1OH;(d.) —(C(Ra)2)n1N(Rb)2;(e.) —(C(Ra)2)n1N(H)C(O)N(Rb)2;(f.) —(C(Ra)2)n1N(H)C(O)Rd;(g.) —(C(Ra)2)n1N(H)S(O)2N(Rb)2;(h.) —(C(Ra)2)n1N(H)S(O)2Rd;(i.) —(C(Ra)2)n2CO2Rc;(j.) —(C(Ra)2)n2C(O)N(Rb)2;(k.) —(C(Ra)2)n1S(O)2N(Rb)2;(l.) —(C(Ra)2)n2N(H)C(O)ORd;(m.) —(C(Ra)2)n2C(O)N(H)S(O)2Rd;(n.) —(C(Ra)2)n1N(H)S(O)2ORd;(o.) —(C(Ra)2)n1S(O)n3Rd;(p.) —(C(Ra)2)n2C(O)N(H)ORd;(q.) —(C(Ra)2)n1CN;(r.) —CH or —(C(Ra)2)n1—CH;(s.) —C(Ra)2O—CC;(t.) —C(O)CF3;(u.) —OH, with the proviso that R3 is —OH only when X2 is CH2; and(v.) —N(Rb)2, with the proviso that R3 is —N(Rb)2 only when X2 is CH2;
each Ra is independently H, C1-C3 alkyl, C1-C3 fluoroalkyl, or C3-C6 cycloalkyl, or alternatively two Ra when bonded to a common carbon atom may together with the common carbon atom form a cyclopropyl ring;each Rb is independently:
(ii.) H;(ii.) C1-C6 alkyl, wherein said C1-C6 alkyl is unsubstituted or independently substituted by 1 to 3 fluoro, or hydroxyl;(iii.) —(CH2)n3CO2Re; or(iv.) —CC or —CH2—CC; oralternatively, two Rb together with the N atom to which they are attached form a 5- to 9-membered heterocyclyl, wherein said heterocyclyl is a saturated, partially saturated, or aromatic ring system containing 0, 1, or 2 additional heteroatoms independently selected from the group consisting of N, O, S, and S(O)2; wherein said heterocyclyl is unsubstituted or substituted by 1 to 4 moieties independently selected from the group consisting of C1-C6 alkyl, C1-C3 alkoxy, fluoro, hydroxyl, oxo, cyano, amino, C1-C3 alkylamino, and C1-C3 dialkylamino;Rc is
(i.) H;(ii.) C1-C6 alkyl, wherein said C1-C6 alkyl is unsubstituted or independently substituted by 1 to 3 fluoro or hydroxy; or(iii.) —CC or CH2—CC;Rd is
(i.) C1-C6 alkyl, wherein said C1-C6 alkyl is unsubstituted or independently substituted by 1 to 3 fluoro or hydroxy;(ii). —C(O)N(Rf)2; or(iii.) —CC or CH2—CC;Re is H or C1-C3 alkyl;Rf is H or C1-C3 alkyl;ring CH is
(i.) C3-C6 cycloalkyl;(ii.) phenyl; or(iii.) a 4- to 9-membered mono- or bicyclic heterocyclyl, wherein said heterocyclyl is a saturated, partially saturated, or aromatic ring system containing 1 to 4 heteroatoms independently selected from the group consisting of N, O, S, and S(O)2;wherein ring CH is unsubstituted or independently substituted by 1 to 4 C1-C6 alkyl, C1-C3 alkoxy, halo, hydroxyl, oxo, cyano, amino, C1-C3 alkylamino, or C1-C3 dialkylamino;ring CC is
(i.) C3-C6 cycloalkyl;(ii.) phenyl; or(iii.) a heterocyclyl of the formula wherein said heterocyclyl is a 5- to 9-membered heterocyclyl, wherein said heterocyclyl is a saturated, partially saturated, or aromatic ring system that contains 1, 2, or 3 heteroatoms independently selected from the group consisting of N, O, S, and S(O)2;wherein ring CC is unsubstituted or independently substituted by 1 to 4 C1-C6 alkyl, C1-C3 alkoxy, halo, hydroxyl, oxo, cyano, amino, C1-C3 alkylamino, or C1-C3 dialkylamino;the subscript n1 is 1, 2, or 3;the subscript n2 is 0, 1, 2, or 3;the subscript n3 is 1 or 2; R4 is
(a.) C1-C8 alkyl, wherein said C1-C8 alkyl of R4 is unsubstituted or independently substituted by 1 to 6 halo, C1-C3 alkoxy, hydroxy, cyano, trimethylsilyl, or methylsulfonyl;(b.) C2-C8 alkenyl, wherein said C2-C8 alkenyl of R4 is unsubstituted or independently substituted by 1 to 6 fluoro or cyano; or(c.) a group of the formula -M-RCH;
M is
(i.) a bond; or(ii.) C1-C6 alkylene, wherein said C1-C6 alkylene of M is unsubstituted or substituted by 1 to 6 fluoro;RCH is a ring selected from the group consisting of
(i.) C3-C9 mono- or bicycloalkyl;(ii.) phenyl; and(iii.) a 3- to 6-membered heterocyclyl, wherein said heterocyclyl of RCH is a saturated, partially saturated or aromatic ring system containing 1 to 2 heteroatoms independently selected from the group consisting of N, O, and S;wherein RCH is unsubstituted or independently substituted by 1 to 4 halo, C1-C3 alkyl, C1-C3 trifluoroalkyl, cyano, C1-C4 alkylcarbonylamino, or oxo; Cy is
(a.) phenyl;(b.) C3-C6 cycloalkyl;(c.) a 5- to 9-membered mono- or bicyclic heterocyclyl, wherein said heterocyclyl of Cy is a saturated, partially saturated, or aromatic ring system containing 1 to 3 heteroatoms independently selected from the group consisting of N, O, S and S(O)2; orwherein Cy is unsubstituted or independently substituted by 1 to 4 Rk moieties selected from the group consisting of:
(i.) C1-C6 alkyl, wherein said C1-C6 alkyl is unsubstituted or independently substituted by 1 to 3 hydroxy or fluoro;(ii.) C1-C6 alkoxy, wherein said C1-C6 alkoxy is unsubstituted or independently substituted by 1 to 3 fluoro, hydroxy, amino, (C1-C3 alkyl)amino,
di(C1-C3 alkyl)amino, methoxy, or phenyl;(iii.) —N(Re1)2;(iv.) —O(CH2)n4C(O)N(Re1)2;(v.) —O(CH2)n5CO2Re1;(vi.) hydroxyl;(vii.) oxo;(viii.) halo;(ix.) C1-C3 alkylsulfonyl;(x.) cyano;(xi.) oxetanyl; and(xii.) cyclopropyl;or alternatively, two Rk moieties, when substituted on adjacent ring atoms of Cy, form a second ring, wherein said second ring is a 5- to 7-membered saturated, partially saturated, or aromatic ring system that contains 0, 1, or 2 heteroatoms independently selected from the group consisting of N, O, and S; wherein said second ring is unsubstituted or substituted by 1 to 3 Rk moieties independently selected from (i)-(xi);
each Re1 is independently H or C1-C3 alkyl;the subscript n4 is 1, 2, or 3; andthe subscript n5 is 1, 2, or 3. |
