申请人:Takeda Chemical Industries, Ltd.
公开号:US06479536B1
公开(公告)日:2002-11-12
Compounds represented by the formula:
wherein R1 and R2 are hydrogen atom, a hydrocarbon group or a heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3- to 8-membered homocyclic or heterocyclic ring,
W indicates
(i) a group represented by the formula:
wherein ring B indicates a 5- to 7-membered ring, or
(ii) a group represented by the formula:
wherein R4 indicates (1) an aliphatic hydrocarbon group, which may be substituted with an aromatic group, or (2) an acyl group containing an aromatic group, R5 is hydrogen atom, a C1-6 alkyl, or an acyl group, provided that, when W is Wa, R3 is hydrogen atom, a hydrocarbon group or a heterocyclic group, when W is Wb, R3 indicates a C6-14 aryl group, or salts thereof or prodrugs thereof have an excellent action to inhibit neurodegeneration and the like as well as an excellent brain penetrability and are low in the toxicity, thereby being useful as prophylactic or therapeutic drugs for nerve degenerative diseases and the like.
该化合物的式子为:其中R1和R2是氢原子、烃基或杂环基,或者R1和R2可以与相邻的碳原子一起形成3-至8-成员的同环或异环环;W表示(i)由公式表示的基团:其中环B表示5-至7-成员环,或(ii)由公式表示的基团:其中R4表示(1)烷基烃基,可以用芳香基取代,或(2)含有芳香基的酰基基团,R5是氢原子、C1-6烷基或酰基基团,但当W为Wa时,R3为氢原子、烃基或杂环基,当W为Wb时,R3表示C6-14芳基,或其盐或前药具有出色的抑制神经退行性等作用,以及出色的脑穿透性,毒性低,因此可用作神经退行性疾病的预防或治疗药物等。