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1.
公开(公告)号:US07214712B2
公开(公告)日:2007-05-08
申请号:US11238502
申请日:2005-09-29
申请人: Nicole Chantel Barvian , David Thomas Connor , Richard Dennis Dyer , Adam Richard Johnson , William Chester Patt
发明人: Nicole Chantel Barvian , David Thomas Connor , Richard Dennis Dyer , Adam Richard Johnson , William Chester Patt
IPC分类号: C07C229/00 , A61K31/195 , A61K31/19
CPC分类号: C07D213/30 , C07C69/80 , C07C69/90 , C07C69/92 , C07C229/60 , C07C233/66 , C07C233/69 , C07C233/73 , C07C233/75 , C07C233/78 , C07C235/60 , C07D285/14 , C07D317/54 , C40B50/14
摘要: Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula wherein: R1, R2, and R3 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; each R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.
摘要翻译: 选择性MMP-13抑制剂是下式的间苯二甲酸衍生物,其中:R 1,R 2和R 3独立地是氢,卤素, 羟基,C 1 -C 6烷基,C 1 -C 6烷氧基,C 2 -C 6烷基,C 1 -C 6烷基,C 1 -C 6烷基, C 1 -C 6亚烷基,C 2 -C 6炔基,NO 2,NR 2, 4,R 5,CN或CF 3; E独立地为O或S; A和B独立地为OR 4或NR 4 R 5; 每个R 4和R 5独立地是H,C 1 -C 6烷基,C 2 C 1 -C 6亚烷基,C 2 -C 6炔基,(CH 2 2) (CH 2)2芳基,(CH 2)2芳基,(CH 2 CH 2)n个杂芳基, 或R 4和R 5与它们所连接的氮原子一起形成3至8元环,任选含有选自O,S的杂原子 ,或NH,并且任选取代或未取代; n为0〜6; 或其药学上可接受的盐。 该化合物可用于治疗由MMP酶介导的哺乳动物中的疾病。
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2.
公开(公告)号:US06995151B2
公开(公告)日:2006-02-07
申请号:US10075918
申请日:2002-02-13
申请人: Nicole Chantel Barvian , David Thomas Connor , Richard Dennis Dyer , Adam Richard Johnson , William Chester Patt
发明人: Nicole Chantel Barvian , David Thomas Connor , Richard Dennis Dyer , Adam Richard Johnson , William Chester Patt
IPC分类号: A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4545 , A61K31/4025
CPC分类号: C07D213/30 , C07C69/80 , C07C69/90 , C07C69/92 , C07C229/60 , C07C233/66 , C07C233/69 , C07C233/73 , C07C233/75 , C07C233/78 , C07C235/60 , C07D285/14 , C07D317/54 , C40B50/14
摘要: Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula wherein: R1, R2, and R3 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; each R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.
摘要翻译: 选择性MMP-13抑制剂是下式的间苯二甲酸衍生物:化学式id =“CHEM-US-00001”num =“000
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