公开(公告)号：US20130303572A1

公开(公告)日：2013-11-14

申请号：US13990684

申请日：2011-12-19

申请人： Péter Ferdinandy ,  Tamás Bálint Csont ,  Csaba Csonka ,  Krisztina Kedvesné Kupai ,  László Kovács ,  Attila Kis-Tamás ,  Ferenc Tamás Takács ,  Dénes Kónya ,  Gábor Medgyes ,  Sándor Cseh ,  István Hajdú ,  Zsolt Lõrincz ,  György Dormán ,  Anikó Görbe

发明人： Péter Ferdinandy ,  Tamás Bálint Csont ,  Csaba Csonka ,  Krisztina Kedvesné Kupai ,  László Kovács ,  Attila Kis-Tamás ,  Ferenc Tamás Takács ,  Dénes Kónya ,  Gábor Medgyes ,  Sándor Cseh ,  István Hajdú ,  Zsolt Lõrincz ,  György Dormán ,  Anikó Görbe

IPC分类号： C07D417/14 ,  C07D213/38 ,  C07D213/30 ,  C07C47/575 ,  C07D295/16 ,  C07D233/90 ,  C07D233/64 ,  C07D417/12 ,  C07D277/30

CPC分类号： C07C47/575 ,  C07D213/30 ,  C07D213/38 ,  C07D233/64 ,  C07D233/90 ,  C07D277/28 ,  C07D277/30 ,  C07D277/56 ,  C07D295/16 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14

摘要： Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: wherein Z is N or CH or the Z(R1) part is replaced with a covalent bond, m and n is 0, 1, 2 or 3; HET is heteroaryl; X is CF3, halogen, CO-heterocyclyl, COOR3 or CONHR3; R1 is H, (CH2)o-aryl, (CH2)p-heteroaryl, (CH2)q-biphenyl; C(O)—R5; S(O)2—R6; R2 is H, aryl, heteroaryl, Y—(CH2)r-aryl, Y—(CH2)s-heteroaryl, where some of the above substituents may be substituted; Y is O or S; with the exclusion of the compound where HET is 1,3-thiazol, X is COOH, R1 is 4-fluorophenyl and R2 is benzyloxy. The invention also relates to the use of a compound of general formula (I), salts or solvates thereof for the use in the prevention or treatment of diseases where the activation of MMPs is involved in the pathomechanism. In this aspect the use of the above excluded compound is also inventive.

摘要翻译： 通式（I）的化合物，其盐或溶剂化物和含有它们的药物组合物：其中Z是N或CH或Z（R1）部分被共价键取代，m和n是0,1,2或3; HET是杂芳基; X是CF 3，卤素，CO-杂环基，COOR 3或CONHR 3; R1是H，（CH2）O-芳基，（CH2）p-杂芳基，（CH2）q-联苯基; C（O）-R 5; S（O）2 -R 6; R2是H，芳基，杂芳基，Y-（CH2）r-芳基，Y-（CH2）s-杂芳基，其中一些上述取代基可以被取代; Y为O或S; 除去HET是1,3-噻唑的化合物，X是COOH，R 1是4-氟苯基，R 2是苄氧基。 本发明还涉及通式（I）的化合物，其盐或溶剂合物用于预防或治疗MMPs的活化参与病理机制的疾病的用途。 在这方面，使用上述排除的化合物也是有创造性的。

公开(公告)号：US09487462B2

公开(公告)日：2016-11-08

申请号：US13990684

申请日：2011-12-19

申请人： Péter Ferdinandy ,  Tamás Bálint Csont ,  Csaba Csonka ,  Krisztina Kedvesné Kupai ,  László Kovács ,  Attila Kis-Tamás ,  Ferenc Tamás Takács ,  Dénes Kónya ,  Gábor Medgyes ,  Sándor Cseh ,  István Hajdú ,  Zsolt Lörincz ,  György Dormán ,  Anikó Görbe

发明人： Péter Ferdinandy ,  Tamás Bálint Csont ,  Csaba Csonka ,  Krisztina Kedvesné Kupai ,  László Kovács ,  Attila Kis-Tamás ,  Ferenc Tamás Takács ,  Dénes Kónya ,  Gábor Medgyes ,  Sándor Cseh ,  István Hajdú ,  Zsolt Lörincz ,  György Dormán ,  Anikó Görbe

IPC分类号： A61K31/4025 ,  A61K31/417 ,  C07C47/575 ,  C07D213/30 ,  C07D233/64 ,  C07D233/90 ,  C07D277/28 ,  C07D277/56 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14 ,  C07D213/38 ,  C07D277/30 ,  C07D295/16

CPC分类号： C07C47/575 ,  C07D213/30 ,  C07D213/38 ,  C07D233/64 ,  C07D233/90 ,  C07D277/28 ,  C07D277/30 ,  C07D277/56 ,  C07D295/16 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14

摘要： Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: wherein Z is N or CH or the Z(R1) part is replaced with a covalent bond, m and n is 0, 1, 2 or 3; HET is heteroaryl; X is CF3, halogen, CO-heterocyclyl, COOR3 or CONHR3; R1 is H, (CH2)o-aryl, (CH2)p-heteroaryl, (CH2)q-biphenyl; C(O)—R5; S(O)2—R6; R2 is H, aryl, heteroaryl, Y—(CH2)r-aryl, Y—(CH2)s-heteroaryl, where some of the above substituents may be substituted; Y is O or S; with the exclusion of the compound where HET is 1,3-thiazol, X is COOH, R1 is 4-fluorophenyl and R2 is benzyloxy. The invention also relates to the use of a compound of general formula (I), salts or solvates thereof for the use in the prevention or treatment of diseases where the activation of MMPs is involved in the pathomechanism. In this aspect the use of the above excluded compound is also inventive.