Monomeric and dimeric heterocycles, and therapeutic uses thereof

A compound of formula (I):

• X—L—X1 (I)
• wherein X and X1 are each independently a compound of formula II
• wherein:
• Y is NR6, —C(R4)(R5)—, or —O—;
• R1 is —C(═O)ORa, —C(═O)N(Ra)2, cyano, (C1-C6)alkyl, (C1-C6)alkanoyl, (C2-C6)alkenyl, (C2-C6)alkynyl, or 1,2,4-oxadiazol-5-yl unsubstituted or substituted at the 3-position by W, wherein any (C1-C6)alkyl, (C1-C6)alkanoyl, (C2-C6)alkenyl, or (C2-C6)alkynyl is unsubstituted or substituted with 1, 2 or 3 substituents independently selected from the group consisting of halo, nitro, cyano, hydroxy, (C1-C6)alkoxy, (C2-C6)acyloxy, trifluoromethyl, C(═O)ORb, C(═O)NRcRd, NReRf, and S(═O)nRg;
• and R3 is (C6-C10)aryl, 5-10 membered heteroaryl, (C6-C10)aryl(C1-C6)alkyl, 5-10 membered heteroaryl(C1-C6)alkyl, (C6-C10)arylcarbonyl, biphenyl, or 5-10 membered heteroarylcarbonyl, wherein any aryl, biphenyl, or heteroaryl substituent is unsubstituted or substituted on carbon with 1, 2 or 3 substituents independently selected from the group consisting of halo, nitro, cyano, hydroxy, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkoxy, (C2-C6)acyloxy, trifluoromethyl, C(═O)ORb, C(═O)NRcRd, NReRf, and S(═O)nRg;
• or
• R1 is —CH2—, or —CH2CH2—, wherein R1 is attached to a carbon at the ortho position of R3;
• and R3 is (C6-C10)aryl, or 5-10 membered heteroaryl;
• R2 is hydrogen or (C1-C6)alkyl;
• R4 and R5 are independently hydrogen or (C1-C6)alkyl;
• R6 is hydrogen, (C1-C6)alkyl, (C1-C6)alkanoyl, (C2-C6)alkenyl, (C2-C6)alkynyl, trifluoromethyl, aryl, heteroaryl, aryl(C1-C4)alkyl, heteroaryl(C1-C4)alkyl, aryl(C1-C4)alkanoyl, or heteroaryl(C1-C4)alkanoyl;
• wherein any (C2-C6)alkyl, (C2-C6)alkanoyl, (C2-C6)alkenyl, or (C2-C6)alkynyl is unsubstituted or substituted on a carbon other than the carbon attached to the piperidine nitrogen with 1, 2 or 3 substituents independently selected from the group consisting of nitro, cyano, hydroxy, (C1-C6)alkoxy, (C2-C6)acyloxy, trifluoromethyl, C(═O)ORb, C(═O)NRcRd, and S(═O)nRg;
• each n is independently 0, 1 or 2;
• W is (C1-C6)alkyl, or aryl, unsubstituted or substituted with 1, 2, or 3 substituents independently selected from the group consisting of halo, nitro, cyano, hydroxy, (C1-C6)alkoxy, (C2-C6)acyloxy, trifluoromethyl, C(═O)ORb, C(═O)NRcRd, NReRf and S(═O)nRg;
• Ra is L2 hydrogen, (C1-C4)alkyl, aryl, heteroaryl, aryl(C1-C4)alkyl, or heteroaryl(C1-C4)alkyl;
• each Rb is independently hydrogen, (C1-C4)alkyl, aryl, heteroaryl, aryl(C1-C4)alkyl, or heteroaryl(C1-C4)alkyl;
• each Rc and Rd is independently hydrogen, (C1-C4)alkyl, aryl, heteroaryl, aryl(C1-C4)alkyl, or heteroaryl(C1-C4)alkyl;
• or, independently, each NRcRd together is piperidino, pyrrolidino, or morpholino;
• each Re and Rf is independently hydrogen, (C1-C4)alkyl, (C1-C4)alkanoyl, (C1-C4)alkoxycarbonyl, aryl, heteroaryl, aryl(C1-C4)alkyl, heteroaryl(C1-C4)alkyl, aryl(C1-C4)alkanoyl, or heteroaryl(C1-C4)alkanoyl;
• or, independently, each NReRf together is piperidino, pyrrolidino, or morpholino;
• each Rg is independently hydrogen, (C1-C4)alkyl, aryl, heteroaryl, aryl(C1-C4)alkyl, or heteroaryl(C1-C4)alkyl;
• and
• L is an unbranched (C2-C12)alkylene chain, unsubstituted or substituted with one, two, or three substituents selected from the group consisting of (C1-C4)alkyl, (C1-C4)alkoxy, hydroxy, oxo, and halo;
• or L is an unbranched (C2-C10)alkylene chain including, within the chain, at least one divalent radical selected from the group consisting of non peroxide oxy (—O—), thio (—S—), sulfinyl, sulfonyl, —OC(═O)—, and —N(Rm)C(═O)—;
• or L is Ri—(C2-C10alkylene)—Rk wherein Ri and Rk are each independently —N(Rm)—, —O—, or —S—;
• each Rm is independently hydrogen or (C1-C4)alkyl;
• or a pharmaceutically acceptable salt thereof.