发明名称 Cyclopropane compounds and pharmaceutical use thereof
摘要 The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
申请公布号 US2010105894(A1) 申请公布日期 2010.04.29
申请号 US20090457391 申请日期 2009.06.09
申请人 JAPAN TOBACCO INC. 发明人 INABA TAKASHI;HAAS JULIA;SHIOZAKI MAKOTO;LITTMANN NICOLE M.;YASUE KATSUTAKA;ANDREWS STEVEN W.;SAKAI ATUSHI;FRYER ANDREW M.;MATSUO TAKAFUML;LAIRD ELLEN R.;SUMA AKIRA;SHINOZAKI YUICHI;HORI YOSHIKAZU;IMAI HIROTO;NEGORO TAMOTSU
分类号 C07D243/08;A61K31/18;A61K31/381;A61K31/496;C07C229/02;C07C307/00;C07C311/13;C07C311/20;C07C311/22;C07C311/29;C07C311/36;C07C311/46;C07D205/04;C07D207/08;C07D207/48;C07D209/44;C07D211/14;C07D211/58;C07D211/96;C07D213/18;C07D213/30;C07D213/65;C07D213/71;C07D213/74;C07D213/81;C07D213/82;C07D215/14;C07D217/08;C07D217/16;C07D223/14;C07D231/10;C07D231/12;C07D233/54;C07D237/12;C07D239/22;C07D241/04;C07D241/36;C07D241/38;C07D257/04;C07D261/06;C07D261/08;C07D265/30;C07D271/06;C07D271/10;C07D271/107;C07D277/20;C07D277/26;C07D277/36;C07D277/82;C07D295/00;C07D295/26;C07D307/79;C07D307/81;C07D307/91;C07D333/06;C07D333/18;C07D333/34;C07D333/36;C07D333/38;C07D333/62;C07D401/02;C07D401/04;C07D403/04;C07D409/02;C07D409/04;C07D409/12;C07D409/14;C07D413/02;C07D413/04;C07D413/14;C07D417/04;C07D417/12;C07D419/04;C07D419/14;C07D471/04;C07D487/04;C07D513/04;C07D513/06 主分类号 C07D243/08
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