| 摘要 |
The present invention relates to a novel class of 1,3-benzoxazol-2(3H)-ones and their use as a medicament, preferably as a dermatologic agent, and as a cosmetic. These novel compounds are particularly useful in treating and/or preventing inflammation, irritation, itching, pruritus, pain, oedema and/or pro-allergic or allergic conditions in a patient. Usually they are topically applied to the skin or mucosa in the form of a pharmaceutical or cosmetic composition comprising the compound and a pharmaceutically and/or cosmetically acceptable carrier. |
| 主权项 |
1. A compound of formula (1) and the enantiomers, diastereomers, tautonmers, solvates and pharmaceutically acceptable salts thereof, wherein R1 is selected from the group consisting of
—(CH2)nN(R4)C(O)R5 and—C(O)NR4R6; R2 is selected from the group consisting of
hydrogen,—C1-6alkyl,—C3-7cycloalkyl, and—(C3-7cycloalkyl)-C1-6-alkyl, R3 is hydrogen, halogen, hydroxy, methoxy or —CN; R4 is hydrogen or C1-6-alkyl; R5 is selected from C8-15alkyl, C8-15alkenyl, C8-15alkinyl, (C6-10aryl)-C6-10alkyl, (C6-10aryl)-C6-10alkenyl, and (C6-10aryl)-C6-10alkinyl; R6 is selected from C9-16alkyl, C9-16alkenyl, C9-16alkinyl, (C6-10aryl)-C7-11alkyl, (C6-10aryl)-C7-11alkenyl, and (C6-10aryl)-C7-11alkinyl; and, n is 0, 1, or 2. |
