公开(公告)号：US20090131502A1

公开(公告)日：2009-05-21

申请号：US12072414

申请日：2008-02-25

申请人： Martin Quibell ,  John Paul Watts ,  Yikang Wang ,  Lee Patient ,  Jonathan R. Heal

发明人： Martin Quibell ,  John Paul Watts ,  Yikang Wang ,  Lee Patient ,  Jonathan R. Heal

IPC分类号： A61K31/407 ,  A61P19/00 ,  A61P33/06 ,  A61P35/00 ,  G01N33/53 ,  C07D487/04 ,  C07D491/04

CPC分类号： C07D491/048 ,  C07D487/04 ,  C07D498/04

摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease and diseases involving matrix or cartilate degradation.

摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐。 本发明还涉及包含式（I）化合物的药物组合物，以及这些化合物在治疗选自骨质疏松症，佩吉特氏病，恰加斯病，疟疾，牙龈疾病，高钙血症，代谢性骨病和涉及 基质或软骨退化。

公开(公告)号：US20090005575A1

公开(公告)日：2009-01-01

申请号：US12069422

申请日：2008-02-08

申请人： Martin Quibell ,  Yikang Wang ,  James Nally ,  John Paul Watts ,  Virendar Kumar Agrawal ,  Michael Standen

发明人： Martin Quibell ,  Yikang Wang ,  James Nally ,  John Paul Watts ,  Virendar Kumar Agrawal ,  Michael Standen

IPC分类号： C07D487/04

CPC分类号： C07D487/04 ,  Y02P20/55

摘要： The present invention relates to a process for preparing a compound of formula I, wherein R1 is Pg1 or P1′; P1′ is CO-hydrocarbyl; P2 is CH2, O or N-Pg2; and Pg1 and Pg2 are each independently nitrogen protecting groups; (i) reacting a compound of formula II with a dioxirane to form an epoxide of formula III; where X is selected from CN, CH2N3, CH2NH-Pg2, ONH-Pg2, NHNH-Pg2, N(Pg2)NH-Pg2; (ii) converting a compound of formula III to a compound of formula I

摘要翻译： 本发明涉及制备式Ⅰ化合物的方法，其中R1是Pg1或P1'; P1'是CO-烃基; P2是CH2，O或N-Pg2; Pg1和Pg2各自独立地为氮保护基; （i）使式II化合物与二环氧环酮反应以形成式III的环氧化物; 其中X选自CN，CH 2 N 3，CH 2 NH-Pg2，ONH-Pg2，NHNH-Pg2，N（Pg2）NH-Pg2; （ii）将式III化合物转化为式I化合物