申请人:Synaptic Pharmaceutical Corporation
公开号:US20020193599A1
公开(公告)日:2002-12-19
The invention provides a method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound having the structure:
1
wherein Y is —(CH
2
)
n
—, where n is 1, 2, 3, 4 or 5; —(CH
2
)
b
—O—(CH
2
)
k
—, where h and k are independently the same or different and are 2, 3 or 4; —(CH
2
)
b
—CH═CH—(CH
2
)
k
—; or —(CH
2
)
h
—C═C—(CH
2
)
k
—, where h and k are independently the same or different and are 1, 2, 3 or 4; wherein Z is O, NH, or CH
2
; wherein R
1
is a linear or branched chain alkyl, alkoxyalkyl or arylalkyl group; wherein R
2
and R
4
are independently the same or different and are H, or a linear or branched chain alkyl group; wherein R
3
is H, a linear or branched chain alkyl, alkoxy, alkoxyalkyl or acyl group; and wherein R
5
and R
6
are independently the same or different and are H, OH, Cl, Br, F, NO
2
, CN, CF
3
, or NH
2
, or a linear or branched chain alkyl, alkoxy, alkoxycarbonyl, acyl, alkylsulfoxide, alkylsulfone, or mono- or dialkylamino group. Other active compounds containing one, two or three rings are also disclosed as well as pharmaceutical compositions prepared therefrom and methods of use in the treatment of BPH, inhibition of cholesterol synthesis, and reduction of intraocular pressure.
本发明提供了一种治疗良性前列腺增生症的方法,该方法包括向受试者施用具有以下结构的化合物的治疗有效量:1其中,Y为—(CH2)n—,其中n为1、2、3、4或5;—(CH2)b—O—(CH2)k—,其中h和k独立且相同或不同,为2、3或4;—(CH2)b—CH═CH—(CH2)k—;或—(CH2)h—C═C—(CH2)k—,其中h和k独立且相同或不同,为1、2、3或4;其中,Z为O、NH或CH2;R1为线性或支链烷基、烷氧基烷基或芳基烷基;R2和R4独立且相同或不同,为H或线性或支链烷基;R3为H、线性或支链烷基、烷氧基、烷氧基烷基或酰基;R5和R6独立且相同或不同,为H、OH、Cl、Br、F、NO2、CN、CF3或NH2,或线性或支链烷基、烷氧基、烷氧基羰基、酰基、烷基亚砜、烷基磺酸、或单烷基或双烷基氨基。还公开了其他含有一个、两个或三个环的活性化合物,以及由此制备的药物组成物和用于治疗BPH、抑制胆固醇合成和降低眼压的使用方法。