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    • 1. 发明授权
    • Dihydropyridines and new uses thereof
    • 二氢吡啶类及其新用途
    • US06211198B1
    • 2001-04-03
    • US09098699
    • 1998-06-15
    • Charles GluchowskiJohn M. WetzelGeorge ChiuMohammed R. MarzabadiWai C. WongDhanapalan Nagarathnam
    • Charles GluchowskiJohn M. WetzelGeorge ChiuMohammed R. MarzabadiWai C. WongDhanapalan Nagarathnam
    • A61K314545
    • C07D401/12C07D211/90C07D401/14C07D405/14C07D471/04C07D471/10C07F7/0812
    • 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: wherein Y is —(CH2)n—, where n is 1, 2, 3, 4 or 5; —(CH2)h—O—(CH2)k—, where h and k are independently the same or different and are 2, 3 or 4; —(CH2)h—CH═CH—(CH2)k—; or —(CH2)h—C≡C—(CH2)k—, where h and k are independently the same or different and are 1, 2, 3 or 4; wherein Z is O, NH, or CH2; wherein R1 is a linear or branched chain alkyl, alkoxyalkyl or arylalkyl group; wherein R2 and R4 are independently the same or different and are H, or a linear or branched chain alkyl group; wherein R3 is H, a linear or branched chain alkyl, alkoxy, alkoxyalkyl or acyl group; and wherein R5 and R6 are independently the same or different and are H, OH, Cl, Br, F, NO2, CN, CF3, or NH2, 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.
    • 本发明提供一种治疗受试者的良性前列腺增生的方法,其包括向受试者施用治疗有效量的具有以下结构的化合物:其中Y为 - (CH 2)n - ,其中n为1,2,3,4 或5; - (CH 2)h -O-(CH 2)k - ,其中h和k独立地相同或不同,为2,3或4; - (CH 2)h -CH = CH-(CH 2)k - ; 或 - (CH 2)h -C = C-(CH 2)k - ,其中h和k独立地相同或不同,为1,2,3或4; 其中Z是O,NH或CH 2; 其中R1是直链或支链烷基,烷氧基烷基或芳基烷基; 其中R2和R4独立地相同或不同,为H或直链或支链烷基; 其中R3是H,直链或支链烷基,烷氧基,烷氧基烷基或酰基; 并且其中R 5和R 6独立地相同或不同,为H,OH,Cl,Br,F,NO 2,CN,CF 3或NH 2,或直链或支链烷基,烷氧基,烷氧基羰基,酰基,烷基亚砜,烷基砜, 或一或二烷基氨基。 还公开了含有一个,两个或三个环的其它活性化合物以及由其制备的药物组合物以及用于治疗BPH,抑制胆固醇合成和降低眼内压的方法。
    • 3. 发明授权
    • Dihydropyridines and new uses thereof
    • 二氢吡啶类及其新用途
    • US06310076B1
    • 2001-10-30
    • US09588973
    • 2000-06-07
    • Charles GluchowskiJohn M. WetzelGeorge ChiuMohammed R. MarzabadiWai C. WongDhanapalan Nagarathnam
    • Charles GluchowskiJohn M. WetzelGeorge ChiuMohammed R. MarzabadiWai C. WongDhanapalan Nagarathnam
    • C07D40102
    • C07D401/12C07D211/90C07D401/14C07D405/14C07D471/04C07D471/10C07F7/0812
    • 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: wherein Y is —(CH2)n—, where n is 1, 2, 3, 4 or 5; —(CH2)h—O—(CH2)k—, where h and k are independently the same or different and are 2, 3 or 4; —(CH2)h—CH═CH—(CH2)k—; or —(CH2)h—C≡C—(CH2)k—, where h and k are independently the same or different and are 1, 2, 3 or 4; wherein Z is O, NH, or CH2; wherein R1 is a linear or branched chain alkyl, alkoxyalkyl or arylalkyl group; wherein R2 and R4 are independently the same or different and are H, or it linear or branched chain alkyl group; wherein R3 is H, a linear or branched chain alkyl, alkoxy, alkoxyalkyl or acyl group; and wherein R5 and R6 are independently the same or different and are H, OH, Cl, Br, F, NO2, CN, CF3, or NH2, 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.
    • 本发明提供一种治疗受试者的良性前列腺增生的方法,其包括向受试者施用治疗有效量的具有以下结构的化合物:其中Y为 - (CH 2)n - ,其中n为1,2,3,4 或5; - (CH 2)h -O-(CH 2)k - ,其中h和k独立地相同或不同,为2,3或4; - (CH 2)h -CH = CH-(CH 2)k - ; 或 - (CH 2)h -C = C-(CH 2)k - ,其中h和k独立地相同或不同,为1,2,3或4; 其中Z是O,NH或CH 2; 其中R1是直链或支链烷基,烷氧基烷基或芳基烷基; 其中R2和R4独立地相同或不同,为H,或者是直链或支链烷基; 其中R3是H,直链或支链烷基,烷氧基,烷氧基烷基或酰基; 并且其中R 5和R 6独立地相同或不同,为H,OH,Cl,Br,F,NO 2,CN,CF 3或NH 2,或直链或支链烷基,烷氧基,烷氧基羰基,酰基,烷基亚砜,烷基砜, 或一或二烷基氨基。 还公开了含有一个,两个或三个环的其它活性化合物以及由其制备的药物组合物和用于治疗BPH,抑制胆固醇合成和降低眼内压的方法。
    • 4. 发明授权
    • Dihydropyridines and new uses thereof
    • 二氢吡啶类及其新用途
    • US5767131A
    • 1998-06-16
    • US211764
    • 1996-02-23
    • Charles GluchowskiJohn M. WetzelGeorge ChiuMohammed R. MarzabadiWai C. WongDhanapalan Nagarathnam
    • Charles GluchowskiJohn M. WetzelGeorge ChiuMohammed R. MarzabadiWai C. WongDhanapalan Nagarathnam
    • C07D211/90C07D401/12C07D401/14C07D405/14C07D471/04C07D471/10C07F7/08A01N43/40
    • C07D211/90C07D401/12C07D401/14C07D405/14C07D471/04C07D471/10C07F7/0812
    • 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: ##STR1## wherein Y is --(CH.sub.2).sub.n --, where n is 1, 2, 3, 4 or 5; --(CH.sub.2).sub.h --O--(CH.sub.2).sub.k --, where h and k are independently the same or different and are 2, 3 or 4; --(CH.sub.2).sub.h --CH.dbd.CH--(CH.sub.2).sub.k --; or --(CH.sub.2).sub.h --C.tbd.C--(CH.sub.2).sub.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.sub.2 ; wherein R.sup.1 is a linear or branched chain alkyl, alkoxyalkyl or arylalkyl group; wherein R.sup.2 and R.sup.4 are independently the same or different and are H, or a linear or branched chain alkyl group; wherein R.sup.3 is H, a linear or branched chain alkyl, alkoxy, alkoxyalkyl or acyl group; and wherein R.sup.5 and R.sup.6 are independently the same or different and are H, OH, Cl, Br, F, NO.sub.2, CN, CF.sub.3, or NH.sub.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.
    • PCT No.PCT / US94 / 03852 Sec。 371日期1996年2月23日 102(e)日期1996年2月23日PCT 1994年4月5日PCT PCT。 公开号WO94 / 22829 1994年10月13日发明内容本发明提供一种治疗受试者的良性前列腺增生的方法,其包括向受试者施用治疗有效量的具有以下结构的化合物:其中Y为 - (CH 2)n - ,其中n 是1,2,3,4或5; - (CH 2)h -O-(CH 2)k - ,其中h和k独立地相同或不同,为2,3或4; - (CH 2)h -CH = CH-(CH 2)k - ; 或 - (CH 2)h -C 3 CF 3 - (CH 2)k - ,其中h和k独立地相同或不同,并且为1,2,3或4; 其中Z是O,NH或CH 2; 其中R1是直链或支链烷基,烷氧基烷基或芳基烷基; 其中R2和R4独立地相同或不同,为H或直链或支链烷基; 其中R3是H,直链或支链烷基,烷氧基,烷氧基烷基或酰基; 并且其中R 5和R 6独立地相同或不同,为H,OH,Cl,Br,F,NO 2,CN,CF 3或NH 2,或直链或支链烷基,烷氧基,烷氧基羰基,酰基,烷基亚砜,烷基砜, 或一或二烷基氨基。 还公开了含有一个,两个或三个环的其它活性化合物以及由其制备的药物组合物和用于治疗BPH,抑制胆固醇合成和降低眼内压的方法。