R¹ is H, C_1-12alkyl, C_2-12alkenyl, C_2-12alkynyl, C_1-12haloalkyl, C_1-12haloalkoxy, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, heterocycloalkyl, heterocycloalkylalkyl, heterocycloalkylalkenyl, heterocycloalkylalkynyl, aryl, arylalkyl, arylalkenyl, heteroarylalkynyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, heteroarylalkynyl, —OR², —SR², or —NR³R⁴; wherein said C_1-12alkyl, C_2-12alkenyl, C_2-12alkynyl, C_1-12haloalkyl, C_1-12haloalkoxy, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, heterocycloalkyl, heterocycloalkylalkyl, heterocycloalkylalkenyl, heterocycloalkylalkynyl, aryl, arylalkyl, arylalkenyl, heteroarylalkynyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, and heteroarylalkynyl are each optionally substituted with 1, 2, 3, or 4 independently selected R⁵ groups;

L1 is an unsubstituted alkylene bridge

each R², R³, and R⁴ is, independently, H, C_1-6alkyl, C_1-6alkenyl, C_1-6alkynyl, C_1-6haloalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; wherein said C_1-6alkyl, C_1-6alkenyl, C_1-6alkynyl, C_1-6haloalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, arylalkyl, heteroaryl, and heteroarylalkyl are each optionally substituted with 1, 2, 3, or 4 independently selected R⁷ groups;

each R⁵ and R⁷ is, independently, OR^a, SR^a, C(O)R^b, C(O)NR^eR^f, C(O)OR^b, OC(O)R^b, OC(O)NR^eR^f, NR^eR^f, NR^cC(O)R^d, NR^cC(O)OR^d, NR^cC(O)NR^d, S(O)R^b, S(O)NR^eR^f, S(O)₂R^b, NR^cS(O)₂R^d, NR^bS(O)₂NR^eR^f, C(═NR^a)R^b, C(═NR^a)NR^b, C(═NR^a)OR^b, OC(═NR^a)R^b, OC(═NR^a)NR^b, NR^cC(═NR^a)R^d NR^cC(═NR^a)OR^d, NR^cC(═NR^a)NR^d, halogen, cyano, nitro, C_1-6alkyl, C_1-6alkenyl, C_1-6alkynyl, C_1-6haloalkyl, C_1-6haloalkoxy, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; wherein said C_1-6alkyl, C_1-6alkenyl, C_1-6alkynyl, C_1-6haloalkyl, C_1-6alkoxy, C_1-6haloalkoxy, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, arylalkyl, heteroaryl, and heteroarylalkyl are each optionally substituted with 1, 2, 3, or 4 independently selected R⁸ groups;

each R⁸ is, independently, OR^a′, SR^a′, C(O)R^b′, C(O)NR^e′R^f′, C(O)OR^b′, OC(O)R^b′, OC(O)NR^e′R^f′, NR^e′R^f′, NR^c′C(O)R^d′, NR^c′C(O)OR^d′, NR^c′C(O)NR^d′, S(O)R^b′, S(O)NR^e′R^f′, S(O)₂R^b′, NR^c′S(O)₂R^d′, NR^bS(O)₂NR^e′R^f′, halogen, cyano, nitro, hydroxyl, carboxy, C_1-6alkyl, C_1-6alkenyl, C_1-6alkynyl, C_1-6haloalkyl, C_1-6alkoxy, C_1-6haloalkoxy, cycloalkyl, cycloalkylalkyl, cycloalkyloxy, cycloalkylalkyloxy, heterocycloalkyl, heterocycloalkylalkyl, heterocycloalkyloxy, heterocycloalkylalkyloxy, aryl, arylalkyl, aryloxy, arylalkyloxy, heteroaryl, heteroarylalkyl, heteroaryloxy, heteroarylalkyloxy, amino, alkylamino, dialkylamino, acyl, formyl, carbamyl, alkylcarbamyl, dialkylcarbamyl, alkylcarbamyloxy, dialkylcarbamyloxy, acyloxy, alkyloxycarbonyl, carboxy, alkylsulfonyl, alkylsulfinyl, or alkylthio;

each R^a, R^b, R^c, R^d, R^e, and R^f is, independently, H, C_1-6alkyl, C_1-6haloalkyl, C_2-6alkenyl, C_2-6alkynyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; wherein said C_1-6alkyl, C_1-6haloalkyl, C_2-6alkenyl, C_2-6alkynyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, arylalkyl, heteroaryl, and heteroarylalkyl are each optionally substituted with 1, 2, or 3 independently selected R^g groups;

or any R^cand R^d, together with the moiety to which they are attached, can form a 3-, 4-, 5-, 6-7- or 8-membered heterocycloalkyl ring, wherein said heterocycloalkyl ring is optionally substituted with 1, 2, or 3 independently selected R^g′ groups;

or any R^e and R^f, together with the nitrogen atom to which they are attached, can form a 3-, 4-, 5-, 6-7- or 8-membered heterocycloalkyl ring or 5-, 6-, 7- or 8-membered heteroaryl ring, wherein said heterocycloalkyl or heteroaryl ring is optionally substituted with 1, 2, or 3 independently selected R^g″ groups;

each R^g is, independently, OR^u, SR^u, C(O)R^v, C(O)NR^yR^z, C(O)OR^v, OC(O)R^v, OC(O)NR^yR^z, NR^yR^z, NR^wC(O)R^x, NR^wC(O)OR^x, NR^wC(O)NR^x, halogen, cyano, nitro, C_1-6alkyl, C_1-6haloalkyl, C_1-6haloalkoxy, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl;

each R^g′ and R^g″ is, independently, halogen, cyano, nitro, hydroxyl, C_1-6alkyl, C_1-6haloalkyl, C_1-6alkoxy, C_1-6haloalkoxy, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, amino, alkylamino, dialkylamino, acyl, formyl, carbamyl, alkylcarbamyl, dialkylcarbamyl, alkylcarbamyloxy, dialkylcarbamyloxy, acyloxy, carboxy, alkylsulfonyl, or alkylsulfinyl;

each R^a′, R^b′, R^c′, R^d′, R^e′, and R^f′ is, independently, H, C_1-6alkyl, C_1-6haloalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl;

or any R^c′ and R^d′, together with the moiety to which they are attached, can form a 3-, 4-, 5-, 6- 7- or 8-membered heterocycloalkyl ring;

or any R^e′ and R^f′, together with the nitrogen atom to which they are attached, can form a 3-, 4-, 5-, 6- 7- or 8-membered heterocycloalkyl ring or 5-, 6-, 7- or 8-membered heteroaryl ring; and

each R^u, R^v, R^w, R^x, R^y, and R^zis, independently, H, C_1-6alkyl, C_1-6haloalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl;

N-(6,7,8,9-tetrahydrodibenzofuran-2-yl)-9H-xanthene-9-acetamide;

2-[(phenylmethylthio)]-N-(6,7,8,9-tetrahydrodibenzofuran-2-yl)-acetamide;

4-oxo-4-[(6,7,8,9-tetrahydro-2-dibenzofuranyl)amino]-butanoic acid methyl ester;

2,2-dimethyl-N,N′-bis(6,7,8,9-tetrahydro-2-dibenzofuranyl)-propanediamide;

3-chloro-N-(6,7,8,9-tetrahydro-2-dibenzofuranyl)benzo[b]thiophene-carboxamide;

2-methoxy-4-(methylthio)-N-(6,7,8,9-tetrahydro-2-dibenzofuranyl)-benzamide;

N-(6,7,8,9-tetrahydro-2-dibenzofuranyl)-cyclohexanecarboxamide;

N-(6,7,8,9-tetrahydro-2-dibenzofuranyl)-cyclopentanecarboxamide;

N-(6,7,8,9-tetrahydro-2-dibenzofuranyl)-3-(trifluoromethyl)-benzamide;

N-(6,7,8,9-tetrahydro-2-dibenzofuranyl)-4-(trifluoromethyl)-benzamide;

1-adamantan-1-yl-3-(6,7,8,9-tetrahydro-dibenzofuran-2-yl)-urea;

N-(3-chlorophenyl)-N′-(6,7,8,9-tetrahydro-2-dibenzofuranyl)-urea;

N-(6,7,8,9-tetrahydro-2-dibenzofuranyl)-1,3-benzodioxole-5-carboxamide;

4-(4-morpholinylsulfonyl)-N-(6,7,8,9-tetrahydro-2-dibenzofuranyl)-benzamide;

8-acetamido-□-methyl-1,2,3,4-tetrahydro-3-dibenzofuranacetic acid methyl ester;

4-(dimethylaminosulfonylamino)-(7,8,9,10-tetrahydro-6H-benzo[b]cyclohepta[d]furan-2-yl)cyclohexanecarboxamide; and

4-(1-pyrrolidinylsulfonyl)-N-(6,7,8,9-tetrahydro-2-dibenzofuranyl)-benzamide;

or pharmaceutically acceptable salt thereof.