| 摘要 |
The compositions and methods of described herein comprise novel ingredients effective to reduce unwanted pigmentation, such as skin discoloration, freckles, age spots, liver spots, sun damage, tans, pigmented acne marks, scars, pigmented birthmarks, hyperpigmentation, post-inflammatory hyperpigmentation, post-injury hyperpigmentation, melasma, cholasma, after-burn scar, nail stain, yellowing of skin, dark circles under eyes, and the like. The composition may include additional ingredients accordingly for a colored cosmetic, moisturizer, cleanser, toner, and the like. |
| 主权项 |
1. A method for improving the aesthetic appearance of human skin comprising topically applying to an area of the skin in need thereof, for a time sufficient to improve the aesthetic appearance of said human skin, a composition comprising a cosmetically acceptable vehicle, and an effective amount of a compound according to formula I(a): wherein, R1 is hydrogen, lower alkyl, or a group R, ε1 is C, N, C—O—, C—S—, C—NR*—, C—CH2—, C—CH═CH—, C—CH═N—, or C—N═CH—; ε2-ε6 are independently selected from a bond (i.e., it is absent), —N—, —NH—, —NR*—, —O—, —S—, —CH—, —CR—, —CR*—, so as to form a five or six-membered ring, and in the case where ring “B” is a five membered ring, ε4 is a bond (i.e., it is absent), and where the dashed circle in ring “B” indicates that the ring is aromatic, partially unsaturated, or saturated; and wherein ε2 or ε6 may be a group -CL1- or -NL1-, wherein L1 is a linking moiety that forms an additional linkage between thiazole ring “A” and ring “B” through R1 (in which case R1 is absent) to form a five or six membered fused ring, where L1 is group —Xa—(CH2)n—(CH═CH)m—Xb—(CH2)n—(CH═CH)m—Xc—, where Xa, Xb, and Xc are independently a bond (i.e., absent), —O—, —S—, —NH—, —NR*— and “n” and “m” are independently at each occurrence integers from 0-2, with the proviso that L1 comprises no more than three atoms in the direct chain between rings “A” and “B”; and wherein any two adjacent groups R* may together form a five or six membered fused ring with ring “B”; Ra and Rb are independently hydrogen, aliphatic C1-C12 hydrocarbon radicals; C1-C12 aromatic hydrocarbon radicals; aliphatic C1-C12 heterocycles, aromatic C1-C12 heterocycles, or combinations thereof; each of the foregoing optionally containing from 1-8 heteroatoms selected from halogen, O, N, and S and being optionally substituted with one or more groups R, and wherein Ra and Rb may together form a three- to six-membered optionally aromatic heterocycle; R is selected, independently at each occurrence, from hydrogen, —F; —Cl; —Br; —I; ═O, —OH, —OR*; —NH2; —NHR*; —N(R*)2; —N(R*)3+; —N(R*)—OH; —N(—O)(R*)2; —O—N(R*)2; —N(R*)—O—R*; —N(R*)—N(R*)2; —C═N—R*; —N═C(R*)2; —C═N—N(R*)2; —C(═NR*)—N(R*)2; —SH; —SR*; —CN; —NC; —(C═O)—R*; —CHO; —CO2H; —CO2−; —CO2R*; —(C═O)—S—R*; —O—(C═O)—H; —O—(C═O)—R*; —S—(C═O)—R*; —(C═O)—NH2; —(C═O)—N(R*)2; —(C═O)—NHNH2; —O—(C═O)—NHNH2; —(C═S)—NH2; —(C═S)—N(R*)2; —N(R*)—CHO; —N(R*)—(C═O)—R*; —(C═NR)—O—R*; —O—(C═NR*)—R*, —SCN; —NCS; —NSO; —SSR*; —N(R*)—C(═O)—N(R*)2; —N(R*)—C(═S)—N(R*)2; —SO2—R*; —O—S(═O)2—R*; —S(═O)2—OR*; —N(R*)—SO2—R*; —SO2—N(R*)2; —O—SO3−; —O—S(═O)2—OR*; —O—S(═O)—OR*; —O—S(═O)—R*; —S(═O)—OR*; —S(═O)—R*; —NO; —NO2; —NO3; —O—NO; —O—NO2; —N3; —N2—R*; —N(C2H4); —Si(R*)3; —CF3; —O—CF3; —PR*2; —O—P(═O)(OR*)2; —P(═O)(OR*)2; C1-C8 perfluoroalkyl; an aliphatic C1-C8 hydrocarbon radical; a C1-C8 aromatic hydrocarbon radical; or a C1-C8 heteroaryl radical; where R* is independently at each occurrence hydrogen or a straight chained, branched, or cyclic C1-C20 hydrocarbon radical, which may be saturated, partially saturated, or aromatic, each of which may be optionally substituted with one or more groups R, or optionally substituted with 1-6 heteroatoms selected from nitrogen, oxygen, sulfur, or halogen; and cosmetically acceptable salts thereof. |
