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    • 3. 发明授权
    • Selective NPY (Y5) antagonists
    • 选择性NPY(Y5)拮抗剂
    • US07273880B2
    • 2007-09-25
    • US11040328
    • 2005-01-20
    • Mohammad R. MarzabadiWai C. WongStewart A. NobleYasuchika Yamaguchi
    • Mohammad R. MarzabadiWai C. WongStewart A. NobleYasuchika Yamaguchi
    • A61K31/426
    • C07D277/60C07D277/42C07D417/12C07D513/04
    • This invention is directed to bicyclic and tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. The invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.
    • 本发明涉及作为NPY(Y5)受体的选择性拮抗剂的双环和三环化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明提供通过将治疗有效量的本发明化合物和药学上可接受的载体组合而制备的药物组合物。 本发明提供了制备药物组合物的方法,其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。 本发明还提供了本发明化合物用于制备用于治疗异常的药物组合物的用途,其中所述异常通过降低人Y5受体的活性而减轻。
    • 6. 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。