发明名称 BORON-CONTAINING SMALL MOLECULES
摘要 This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.
申请公布号 US2015065459(A1) 申请公布日期 2015.03.05
申请号 US201414537694 申请日期 2014.11.10
申请人 Anacor Pharmaceuticals, Inc. 发明人 BAKER Stephen J.;Akama Tsutomu;BELLINGER-KAWAHARA Carolyn;Hernandez Vincent S.;Hold Karin M.;Leyden James J.;Maples Kirk R.;Plattner Jacob J.;Sanders Virginia;Zhang Yong-Kang
分类号 C07F5/02 主分类号 C07F5/02
代理机构 代理人
主权项 1. A compound having a structure according to Formula I:wherein B is boron; R1a is a member selected from a negative charge, a salt counterion, H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; M1 is a member selected from oxygen, sulfur and NR2a; wherein R2a is a member selected from H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; J1 is a member selected from (CR3aR4a)n1 and CR5a wherein R3a, R4a, and R5a are members independently selected from H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; andn1 is an integer selected from 0 to 2; W1 is a member selected from C═O (carbonyl), (CR6aR7a)m1 and CR8a; R6a, R7a, and R8a are members independently selected from H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl;m1 is an integer selected from 0 and 1; A1 is a member selected from CR9a and N; D1 is a member selected from CR10a and N; E1 is a member selected from CR11a and N; G1 is a member selected from CR12a and N; wherein R9a, R10a, R11a and R12a are members independently selected from H, OH, NH2, SH, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl;the combination of nitrogens (A1+D1+E1+G1) is an integer selected from 0 to 3; wherein a member selected from R3a, R4a and R5a and a member selected from R6a, R7a and R8a, together with the atoms to which they are attached, are optionally joined to form a 4 to 7 membered ring;R3a and R4a, together with the atoms to which they are attached, are optionally joined to form a 4 to 7 membered ring;R6a and R7a, together with the atoms to which they are attached, are optionally joined to form a 4 to 7 membered ring;R9a and R10a, together with the atoms to which they are attached, are optionally joined to form a 4 to 7 membered ring;R10a and R11a, together with the atoms to which they are attached, are optionally joined to form a 4 to 7 membered ring;R11a and R12a, together with the atoms to which they are attached, are optionally joined to form a 4 to 7 membered ring; with the proviso that when M1 is oxygen, W1 is a member selected from (CR3aR4a)n1, wherein n1 is 0, J1 is a member selected from (CR6aR7a)m1, wherein m1 is 1, A1 is CR9a, D1 is CR10a, E1 is CR11a, G1 is CR12a, then R9a is not halogen, methyl, ethyl, or optionally joined with R10a to a form phenyl ring; R10a is not unsubstituted phenoxy, C(CH3)3, halogen, CF3, methoxy, ethoxy, or optionally joined with R9a to form a phenyl ring; R11a is not halogen or optionally joined with R10a to form a phenyl ring; and R12a is not halogen; with the further proviso that when M1 is oxygen, W1 is a member selected from (CR3aR4a)n1, wherein n1 is 0, J1 is a member selected from (CR6aR7a)m1, wherein m1 is 1, A1 is CR9a, D1 is CR10a, E1 is CR11a, G1 is CR12a, then neither R6a nor R7a are halophenyl; with the further proviso that when M1 is oxygen, W1 is a member selected from (CR3aR4a)n1, wherein n1 is 0, J1 is a member selected from (CR6aR7a)m1, wherein m1 is 1, A1 is CR9a, D1 is CR10a, E1 is CR11a, G1 is CR12a, and R9a, R10a and R11a are H, then R6a, R7a and R12a are not H; with the further proviso that when M1 is oxygen n1 is 1, J1 is a member selected from (CR6aR7a)m1, wherein m1 is 0, A1 is CR9a, D1 is CR10a, E1 is CR11a, G1 is CR12a, R9a is H, R10a is H, R11a is H, R6a is H, R7a is H, R12a is H, then W1 is not C═O (carbonyl); with the further proviso that when M1 is oxygen, W1 is CR5a, n1 is 1, J1 is CR8a, m1 is 1, A1 is CR9a, D1 is CR10a, E1 is CR11a, G1 is CR12a, R6a, R7a, R9a, R10a, R11a and R12a are H, then R5a and R8a, together with the atoms to which they are attached, do not form a phenyl ring.
地址 Palo Alto CA US