公开(公告)号：EP2041103A2

公开(公告)日：2009-04-01

申请号：EP07765216.2

申请日：2007-07-10

申请人： Galapagos SAS ,  Amgen, Inc

发明人： DEPREZ, Pierre ,  LIVELY, Sarah ,  TEMAL-LAIB, Taoues

IPC分类号： C07D277/48 ,  C07D277/82 ,  C07D417/12 ,  A61K31/17 ,  A61K31/426 ,  A61K31/428 ,  C07C275/18 ,  C07C275/28

CPC分类号： C07D277/48 ,  C07C275/42 ,  C07C2601/14 ,  C07C2603/18 ,  C07D277/82 ,  C07D417/12

摘要： Compounds of formula (I): Z is >CH-, >C=CH- or >N-, R1 and R2 are optionally substituted and are the same or different, and each represents an aryl group, a heteroaryl group, or Z, R1 and R2 form a fused ring structure of formula: in which A represents a single bond, or linking group, R3 represents hydrogen, a group selected from: -AIkCOOR, -AIkNR7R8, -AIkCONR7R8, -AIkCOR9, -AIkSO2NR10R10', -AIkOR10, and -AIkS(O)nR10, in which AIk is alkyl, R is hydrogen or alkyl, R7 and R8 each represents H, optionally substituted alkyl, alkylaminoalkyl or dialkylaminoalkyl, or CONR7R8 forms an optionally substituted heterocycle, and R10 and R10 are hydrogen atom, optionally substituted alkyl, an alkylaminoalkyl group, an optionally substituted cycle, optionally spaced by an AIk group as defined, Q represents >C=0 or >C=S, R5 is a hydrogen atom or an alkyl, alkoxy, hydroxyalkyl, alkylthio, or thioalkyl group, p is 1, 2 or 3, q is 0, 1 or 2, R6 represents an optionally substituted aryl or heteroaryl group, and salts and esters thereof, are useful as calcimimetics in therapy.

摘要翻译： 式（I）的化合物：Z是> CH - ，> C = CH-或> N-，R 1和R 2任选地substituiertem并且它们是相同的或不同的，并且每个darstellt芳基，杂芳基，或者 Z，R 1和R 2形成下式的稠环结构：其中A代表单键，或连接基团，R 3 darstellt氢，基团选自：-AlkCOOR，-AlkNR 7 R 8，R 7 -AlkCONR 8，-AlkCOR 9，-AlkSO 2 NR 10 R 10”，-AlkOR1O，和-AlkS（O）N R 10，在其中Alk是烷基，R是氢或烷基，R 7和R 8各自darstellt H，任选 取代的烷基，烷基氨基烷基，或二烷基氨基烷基，或CONR 7 R 8组的形式在任选取代的杂环，且R“°和R 10”是氢原子，任选取代的烷基，在烷基氨基烷基，任选substituiertem循环，任选地被烷基隔开 所定义的，q darstellt> C = O或> C = S，R 5是氢原子或烷基，烷氧基，羟烷基，烷硫基，或硫代烷基，p是1，2或3，q为0，1或2个 中，R 6可选darstellt到 LY substituiertem芳基或杂芳基，和其盐和酯，如在治疗拟钙剂有用。

公开(公告)号：EP1874765B1

公开(公告)日：2012-03-07

申请号：EP06724709.8

申请日：2006-04-24

申请人： Galapagos SAS

发明人： DEPREZ, Pierre ,  JARY, Helène ,  TEMAL, Taoues

IPC分类号： C07D417/12 ,  C07D413/12 ,  C07D417/14

CPC分类号： C07D263/58 ,  C07D277/48 ,  C07D277/82 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

摘要： The present invention provides compounds of formula (I): in which R1, R'1, R2, R'2, R3, Y and G have the meanings given in the description, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.

公开(公告)号：EP1965805B1

公开(公告)日：2009-12-02

申请号：EP06829733.2

申请日：2006-10-31

申请人： Galapagos SAS

发明人： DEPREZ, Pierre ,  JARY, Helène ,  TEMAL, Taoues

IPC分类号： A61K31/5375 ,  A61K31/5377 ,  C07D213/38 ,  C07D213/75 ,  C07D213/80 ,  C07D213/82 ,  C07D217/22 ,  C07D231/52 ,  C07D231/56 ,  C07D235/14 ,  C07D235/30 ,  C07D239/46 ,  C07D257/04 ,  C07D261/08 ,  C07D261/20

CPC分类号： C07D295/13 ,  C07D209/08 ,  C07D209/88 ,  C07D213/40 ,  C07D213/70 ,  C07D213/75 ,  C07D213/80 ,  C07D213/82 ,  C07D217/02 ,  C07D231/22 ,  C07D231/40 ,  C07D231/52 ,  C07D231/56 ,  C07D235/18 ,  C07D235/30 ,  C07D239/47 ,  C07D239/48 ,  C07D241/20 ,  C07D257/04 ,  C07D261/08 ,  C07D261/14 ,  C07D261/18 ,  C07D261/20 ,  C07D263/32 ,  C07D263/48 ,  C07D277/28 ,  C07D277/66 ,  C07D285/08 ,  C07D285/135 ,  C07D295/125 ,  C07D307/52 ,  C07D307/88 ,  C07D317/66 ,  C07D319/08 ,  C07D319/18 ,  C07D333/20 ,  C07D333/28 ,  C07D333/38 ,  C07D333/68 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04

摘要： The present invention provides compounds of formula (I): in which Y is oxygen or sulphur; R1 and R”1 are optionally substituted aryl, heteroaryl or a fused ring structure, R2 and R'2 are each H, or optionally substituted alkyl, alkylaminoalkyl or dialkylaminoalkyl, or R2 and R'2 and their N form a saturated or unsaturated optionally substituted heterocycle, R3 represents a group of formula -(CH2)P-Ar-Rn, wherein p is 0 or 1 and, when p is 1, is optionally substituted, Ar is aryl or heteroaryl, and each R is H, halogen; hydroxyl; trifiuoromethyl; linear and branched alkyl, alkenyl, alkynyl, and alkoxyl groups, all optionally further substituted by one or more of hydroxy groups, halogen atoms, alkoxy groups, amino groups, and alkylthio groups; linear and branched alkoxyl groups; linear and branched thioalkyl groups; aryl groups; aralkyl groups; aralkoxy groups; aryloxy groups; perfluoroalkyl; -CN; -NR4R5, -C(=X)NR4R5,-O-C(=X)NR4R5, -SO2NR4R5, - Alk-NR4R5, -NZC(=X)(NH)qR6, -Alk-NZC(=X)(NH)qR6, -C(=X)R6, -Alk-C(=X)(NH)qR6, -NHSO2R7, -SO2R7, -SOR7, -SR7, or is a saturated or unsaturated heterocyclyl group, and salts and esters thereof, are useful in the treatment of conditions susceptible to modulating ion channels, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.

公开(公告)号：EP2176247A2

公开(公告)日：2010-04-21

申请号：EP08780119.7

申请日：2008-07-10

申请人： Amgen Inc.

发明人： DEPREZ, Pierre ,  FOTSCH, Christopher ,  HARRINGTON, Paul ,  LIVELY, Sarah, E. ,  PATTABIRAMAN, Kanaka ,  ST. JEAN, David ,  TEMAL-LAIB, Taoues ,  WEHN, Paul

IPC分类号： C07D277/46 ,  C07D277/82 ,  C07D417/12 ,  C07D417/14 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61P19/10

CPC分类号： C07D277/82 ,  C07D277/46 ,  C07D417/12 ,  C07D417/14

摘要： The present invention relates generally to compounds represented in Formula (I), pharamaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.