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33 条记录 (耗时 0.046 秒)

    Dihydropyrimidines and uses thereof
    2.
    发明授权
    Dihydropyrimidines and uses thereof 失效
    二氢嘧啶及其用途

    公开(公告)号：US06172066B2

    公开(公告)日：2001-01-09

    申请号：US08858061

    申请日：1997-05-16

    申请人： Dhanapalan Nagarathnam ,  Wai C. Wong ,  Shou Wu Miao ,  Michael A. Patane ,  Charles Gluchowski

    发明人： Dhanapalan Nagarathnam ,  Wai C. Wong ,  Shou Wu Miao ,  Michael A. Patane ,  Charles Gluchowski

    IPC分类号： A61K31497

    CPC分类号： C07D239/22

    摘要： This invention is directed to dihydropyrimidine compounds which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

    摘要翻译： 本发明涉及作为人α1A受体的选择性拮抗剂的二氢嘧啶化合物。 本发明还涉及这些化合物降低眼内压，抑制胆固醇合成，松弛下尿路组织，治疗良性前列腺增生，阳ency，心律失常以及治疗任何α1A受体拮抗作用的疾病的用途 可能是有用的 本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

    Dihydropyridines and new uses thereof
    7.
    发明授权
    Dihydropyridines and new uses thereof 失效
    二氢吡啶类及其新用途

    公开(公告)号：US06211198B1

    公开(公告)日：2001-04-03

    申请号：US09098699

    申请日：1998-06-15

    申请人： Charles Gluchowski ,  John M. Wetzel ,  George Chiu ,  Mohammed R. Marzabadi ,  Wai C. Wong ,  Dhanapalan Nagarathnam

    发明人： Charles Gluchowski ,  John M. Wetzel ,  George Chiu ,  Mohammed R. Marzabadi ,  Wai C. Wong ,  Dhanapalan Nagarathnam

    IPC分类号： A61K314545

    CPC分类号： C07D401/12 ,  C07D211/90 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D471/10 ,  C07F7/0812

    摘要： 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.

    摘要翻译： 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。

    Dihydropyridines and new uses thereof
    9.
    发明授权
    Dihydropyridines and new uses thereof 失效
    二氢吡啶类及其新用途

    公开(公告)号：US06310076B1

    公开(公告)日：2001-10-30

    申请号：US09588973

    申请日：2000-06-07

    申请人： Charles Gluchowski ,  John M. Wetzel ,  George Chiu ,  Mohammed R. Marzabadi ,  Wai C. Wong ,  Dhanapalan Nagarathnam

    发明人： Charles Gluchowski ,  John M. Wetzel ,  George Chiu ,  Mohammed R. Marzabadi ,  Wai C. Wong ,  Dhanapalan Nagarathnam

    IPC分类号： C07D40102

    CPC分类号： C07D401/12 ,  C07D211/90 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D471/10 ,  C07F7/0812

    摘要： 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.

    摘要翻译： 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。