| 主权项 |
1. A compound of formula I:wherein:
B is selected from the group consisting of phenyl, thienyl, pyridinyl, isoquinolinyl, tetrahydroisoquinolinyl, naphthyl, isoxazolyl, indolyl, piperidinyl, tetrahydrofuranyl, piperazinyl, pyrazolyl and pyrrolidinyl (which is optionally substituted with oxo), wherein B is unsubstituted or substituted with 1-5 substituents each independently selected from R1, R2, R3a and R3b;
R1, R2, R3a and R3b are independently selected from:(1) —C1-6alkyl, which is unsubstituted or substituted with 1-7 substituents each independently selected from:
(a) halo,(b) hydroxy,(c) —O—C1-6alkyl,(d) —C3-6cycloalkyl,(e) phenyl or heterocycle, wherein the heterocycle is selected from pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperidinyl, piperazinyl, pyrrolidinyl, thienyl and morpholinyl, and wherein said phenyl or heterocycle is unsubstituted or substituted with 1-5 substituents each independently selected from
(i) —C1-6alkyl,(ii) —O—C1-6alkyl,(iii) halo,(iv) hydroxy,(v) trifluoromethyl, and(vi) —OCF3,(f) —CO2R9, wherein R9 is selected from
(i) hydrogen,(ii) —C1-6alkyl which is unsubstituted or substituted with 1-6 fluoro,(iii) —C5-6cycloalkyl,(iv) benzyl and(v) phenyl,(g) —NR10R11, wherein R10 and R11 are each independently selected from:
(i) hydrogen,(ii) —C1-6alkyl which is unsubstituted or substituted with 1-6 fluoro,(iii) —C5-6cycloalkyl,(iv) benzyl,(v) phenyl,(vi) —CO2R9 and(vii) —SO2R12, wherein R12 is: (I) —C1-6alkyl which is unsubstituted or substituted with 1-6 fluoro; (II) —C5-6cycloalkyl; (III) benzyl; or (IV) phenyl;(h) —SO2R12,(i) —CONR10aR11a, wherein: R10a and R11a are each independently:
(i) hydrogen;(ii) —C1-6alkyl which is unsubstituted or substituted with 1-6 fluoro;(iii) —C5-6cycloalkyl;(iv) benzyl; or(v) phenyl; orR10a and R11a are joined to form a ring selected from azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl and morpholinyl, which ring is unsubstituted or substituted with 1-5 substituents each independently selected from
(i) —C1-6 alkyl;(ii) —O—C1-6 alkyl;(iii) halo;(iv) hydroxyl;(v) phenyl; or(vi) benzyl;(j) trifluoromethyl,(k) —OCO2R9,(l) —(NR10a)CO2R9,(m) —O(CO)NR10aR11a; or(n) —(NR9)(CO)NR10aR11a;(2) —C3-6cycloalkyl, which is unsubstituted or substituted with 1-7 substituents each independently selected from
(a) halo,(b) hydroxy,(c) —O—C1-6 alkyl,(d) trifluoromethyl and(e) phenyl, wherein the phenyl is unsubstituted or substituted with 1-5 substituents each independently selected from
(i) —C1-6 alkyl,(ii) —O—C1-6 alkyl,(iii) halo,(iv) hydroxy and(v) trifluoromethyl,(3) phenyl or heterocycle, wherein the heterocycle is selected from pyridinyl, pyrimidinyl, pyrazinyl, thienyl, pyridazinyl, pyrrolidinyl, azetidinyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, imidazolyl, triazolyl, tetrazolyl, azepanyl, benzimidazolyl, benzopyranyl, benzofuryl, benzothiazolyl, benzoxazolyl, chromanyl, furyl, imidazolidinyl, imidazolinyl, indolinyl, indolyl, quinolinyl, isoquinolinyl, tetrahydroquinolinyl, isoindolinyl, tetrahydroisoquinolinyl, 2-oxopiperazinyl, 2-oxopiperidinyl, 2-oxopyrrolidinyl, pyrazolidinyl, pyrazolyl, pyrrolyl, quinazolinyl, tetrahydrofuryl, thiazolinyl, purinyl, naphthyridinyl, quinoxalinyl, quinazolinyl, 1,3-dioxolanyl, oxadiazolyl, piperidinyl and morpholinyl, and wherein the phenyl or heterocycle is unsubstituted or substituted with 1-5 substituents each independently selected from:
(a) —C1-6alkyl which is unsubstituted or substituted with 1-6 fluoro,(b) halo,(c) hydroxy,(d) —O—C1-6alkyl, which is unsubstituted or substituted with 1-6 fluoro,(e) —C3-6cycloalkyl,(f) phenyl or heterocycle, wherein the heterocycle is selected from pyridinyl, pyrimidinyl, pyrazinyl, thienyl and morpholinyl, and wherein the phenyl or heterocycle is unsubstituted or substituted with 1-5 substituents each independently selected from
(i) —C1-6 alkyl,(ii) —O—C1-6 alkyl,(iii) halo,(iv) hydroxy and(v) trifluoromethyl,(g) —CO2R9,(h) —NR10R11,(i) —CONR10R11,(j) —SO2R12, and(k) oxo,(4) halo,(5) oxo,(6) hydroxy,(7) —O—C1-6alkyl, which is unsubstituted or substituted with 1-5 halo,(8) —CN,(9) —CO2R9,(10) —NR10R11,(11) —SO2R12,(12) —CONR10aR11a,(13) —OCO2R9,(14) —(NR10a)CO2R9,(15) —O(CO)NR10aR11a,(16) —(NR9)(CO)NR10aR11a,(17) —SO2NR10aR11a,(18) —SR12,(19) —S(O)R12,(20) —(NR9)(CO)NR10aR11a,(21) —(CO)—(CO)NR10aR11a, and(22) —(CO)—(CO)OR9;or R3a and R3b and the atom(s) to which they are attached are joined to form a ring selected from azetidinyl, azepanyl, azepinyl, cyclobutyl, cyclopentenyl, cyclopentyl, cyclohexenyl, cyclohexyl, phenyl, naphthyl, thienyl, thiazolyl, thiazolinyl, oxazolyl, oxazolinyl, imidazolyl, imidazolinyl, imidazolidinyl, thiadiazolyl, oxadiazolyl, isoxazolyl, pyrazolyl, triazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazinyl, pyrrolyl, pyrrolinyl, morpholinyl, azetidinyl, pyrrolidinyl, piperidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydropyridinyl, furanyl, dihydrofuranyl, dihydropyranyl, dihydrothienyl, tetrahydrothienyl, dihydrothiopyranyl, tetrahydrothiopyranyl, pyrrolidinyl, piperidinyl, and piperazinyl, which ring is unsubstituted or substituted with 1-5 substituents each independently selected from:
(a) —C1-6alkyl, which is unsubstituted or substituted with 1-3 substituents each independently selected from:
(i) halo,(ii) hydroxy,(iii) —O—C1-6alkyl, which is unsubstituted or substituted with 1-5 substituents each independently selected from (I) —O—C1-6alkyl, (II) halo, and (III) hydroxy,(iv) —C3-6cycloalkyl, which is unsubstituted or substituted with 1-5 substituents each independently selected from (I) —C1-6alkyl, (II) —O—C1-6alkyl, (III) halo, (IV) hydroxy, (V) trifluoromethyl and (VI) —OCF3,(v) phenyl or heterocycle, wherein the heterocycle is selected from pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperidinyl, piperazinyl, pyrrolidinyl, thienyl and morpholinyl, which phenyl or heterocycle is unsubstituted or substituted with 1-5 substituents each independently selected from (I) —C1-6alkyl, (II) —O—C1-6alkyl, (III) halo, (IV) hydroxy, (V) trifluoromethyl and (VI) —OCF3,(vi) —CO2R9,(vii) —NR10R11,(viii) —SO2R12,(ix) —CONR10aR11a, and(x) —(NR10a)CO2R9,(b) —C3-6cycloalkyl, which is unsubstituted or substituted with 1-5 substituents each independently selected from
(i) halo,(ii) hydroxy,(iii) —O—C1-6alkyl,(iv) trifluoromethyl and(v) phenyl,(c) phenyl or heterocycle, wherein the heterocycle is selected from pyridinyl, pyrimidinyl, pyrazinyl, thienyl, pyridazinyl, pyrrolidinyl, azetidinyl, piperidinyl and morpholinyl, which phenyl or heterocycle is unsubstituted or substituted with 1-3 substituents each independently selected from
(i) halo,(ii) hydroxy,(iii) —C3-6cycloalkyl,(iv) —O—C1-6alkyl which is unsubstituted or substituted with 1-6 fluoro, and(v) —C1-6alkyl which is unsubstituted or substituted with 1-6 fluoro,(d) halo,(e) —SO2R12,(f) hydroxy,(g) —O—C1-6alkyl which is unsubstituted or substituted with 1-5 halo,(h) —CN,(i) —COR12,(j) —NR10R11,(k) —CONR10aR11a,(l) —CO2R9,(m) —(NR10a)CO2R9,(n) —O(CO)NR10aR11a,(o) —(NR9)(CO)NR10aR11a, and(p) oxo; A1 and A2 are each independently selected from:
(1) a bond,(2) —CR13R14—, wherein R13 and R14 are independently selected from
(a) hydrogen,(b) C1-6 alkyl, which is unsubstituted or substituted with 1-5 substituents each independently selected from
(i) halo,(ii) hydroxy,(iii) —NR10R11,(iv) —CONR10aR11a and(v) —CO2R9,(c) phenyl, which is unsubstituted or substituted with 1-3 substituents each independently selected from
(i) C1-4alkyl,(ii) hydroxyl and(iii) halo,(d) —CONR10—(C1-6alkyl)-NR15aR16a, wherein R15a and R16a are each independently selected from
(i) hydrogen,(ii) —C1-6 alkyl,(iii) —COR9 and(iv) —CO2R9,(e) —CO2R9,(f) —CONR10aR11a, and(g) hydroxy, or(3) —CH2CR13R14—, and(4) —C(═O)—; G1-and G3 are each —C(R5)=, G2is —N═ or-(N+—O−)═; J is independently selected from:
(1) ═C(R6a)—,(2) —CR13R14—,(3) —C(═O)—, and(4) —N(R15)—; Y is independently selected from:
(1) ═C(R6b)—,(2) —CR13R14—,(3) —C(═O)—,(4) —SO2—,(5) ═N—, and(6) —N(R6b)—; R4 is selected from
(1) hydrogen,(2) C1-6 alkyl which is unsubstituted or substituted with 1-6 fluoro,(3) C5-6 cycloalkyl,(4) benzyl and(5) phenyl, or R4 is joined to B to form a ring selected from piperidinyl, pyrrolidinyl, piperazinyl, azetidinyl, azepinyl and morpholinyl, which ring is unsubstituted or substituted with 1-5 substituents each independently selected from
(1) —C1-6 alkyl,(2) —O—C1-6alkyl,(3) halo,(4) hydroxy,(5) phenyl and(6) benzyl; R5 is independently selected from:
(1) hydrogen,(2) C1-6 alkyl,(3) —O—C1-6alkyl,(4) —OCF3,(5) trifluoromethyl,(6) halo,(7) hydroxy, and(8) —CN; R6a and R6b are each independently selected from:
(1) hydrogen;(2) —C1-4alkyl, which is unsubstituted or substituted with 1-5 substituents each independently selected from:
(a) halo,(b) —O—C1-6alkyl,(c) —C3-6cycloalkyl,(d) phenyl or heterocycle, wherein the heterocycle is selected from imidazolyl, oxazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperidinyl, piperazinyl, pyrrolidinyl, thiazolyl, thienyl, triazolyl, or morpholinyl, which phenyl or heterocycle is unsubstituted or substituted with 1-3 substituents each independently selected from
(i) —C1-6alkyl,(ii) —O—C1-6 alkyl,(iii) halo,(iv) hydroxy,(v) trifluoromethyl and(vi) —OCF3,(3) phenyl or heterocycle, wherein the heterocycle is selected from pyridinyl, pyrimidinyl, pyrazinyl, thienyl, pyrrolidinyl, azetidinyl, thiazolyl, oxazolyl, imidazolyl, triazolyl, tetrahydrofuryl, piperidinyl, and morpholinyl, which phenyl or heterocycle is unsubstituted or substituted with 1-3 substituents each independently selected from
(a) —C1-4alkyl which is unsubstituted or substituted with 1-5 fluoro,(b) halo,(c) hydroxy,(d) —O—C1-4alkyl which is unsubstituted or substituted with 1-5 fluoro,(e) —C3-6cycloalkyl and(f) phenyl,(4) halo,(5) hydroxy,(6) —O—C1-6alkyl, which is unsubstituted or substituted with 1-5 halo,(7) —CN,(8) —CO2R9,(9) —NR10R11, and(10) —CONR10aR11a,or R6a and R6b and the atom(s) to which they are attached are joined to form a ring selected from cyclopentenyl, cyclohexenyl, phenyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, furanyl, dihydrofuranyl, dihydropyranyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, imidazolyl, triazolyl, thienyl, dihydrothienyl and dihydrothiopyranyl, which ring is unsubstituted or substituted with 1-5 substituents each independently selected from:
(a) —C1-6alkyl, which is unsubstituted or substituted with 1-3 substituents each independently selected from:
(i) halo,(ii) hydroxy,(iii) —O—C1-6 alkyl,(iv) —C3-6cycloalkyl,(v) phenyl or heterocycle, wherein the heterocycle is selected from: pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperidinyl, piperazinyl, pyrrolidinyl, thienyl, or morpholinyl, which is unsubstituted or substituted with 1-5 substituents where the substituents are each independently selected from (I) —C1-6alkyl, (II) —O—C1-6alkyl, (III) halo, (IV) hydroxy, (V) trifluoromethyl and (VI) —OCF3,(vi) —CO2R9,(vii) —NR10R11,(viii) —SO2R12,(ix) —CONR10aR11a, and(x) —(NR10a)CO2R9,(b) phenyl or heterocycle, wherein the heterocycle is selected from pyridinyl, pyrimidinyl, pyrazinyl, thienyl, pyridazinyl, pyrrolidinyl, azetidinyl, piperidinyl and morpholinyl, which phenyl or heterocycle is unsubstituted or substituted with 1-3 substituents each independently selected from
(i) —C1-6alkyl, which is unsubstituted or substituted with 1-6 fluoro,(ii) —O—C1-6alkyl, which is unsubstituted or substituted with 1-6 fluoro,(iii) halo,(iv) hydroxy, and(v) —C3-6cycloalkyl,(c) halo,(d) —SO2R12,(e) hydroxy,(f) —O—C1-6alkyl, which is unsubstituted or substituted with 1-5 halo,(g) —CN,(h) —COR12,(i) —NR10R11,(j) —CONR10aR11a,(k) —CO2R9,(l) —(NR10a)CO2R9,(m) —O(CO)NR10aR11a,(n) —(NR9)(CO)NR10aR11a, and(o) oxo; R15 is independently for each occurrence:
(1) hydrogen, or(2) —C1-4alkyl which is unsubstituted or substituted with 1-3 substituents which are independently halo or phenyl; m is 1 ; n is 1 ;or a pharmaceutically acceptable salt thereof, individual enantiomer, or diastereomer thereof. |
