公开(公告)号：US20150080382A1

公开(公告)日：2015-03-19

申请号：US14313672

申请日：2014-06-24

申请人： Celtaxsys, Inc.

发明人： Damian O. Arnaiz ,  Greg Brown ,  Emmanuel Claret ,  Arwed Cleve ,  David Davey ,  William Guilford ,  Seock-Kyu Khim ,  Thomas Kirkland ,  Monica J. Kochanny ,  Amy Liang ,  David Light ,  John Parkinson ,  Guo Ping Wei ,  Bin Ye

IPC分类号： C07D487/08 ,  C07D243/08 ,  C07C229/08 ,  C07D409/12 ,  C07D401/12 ,  C07D263/14 ,  C07D405/12

CPC分类号： C07D487/08 ,  C07B2200/07 ,  C07C217/58 ,  C07C229/08 ,  C07C229/38 ,  C07C233/78 ,  C07C255/57 ,  C07C271/20 ,  C07C2601/14 ,  C07D207/04 ,  C07D207/09 ,  C07D207/16 ,  C07D211/26 ,  C07D211/34 ,  C07D211/58 ,  C07D243/08 ,  C07D263/14 ,  C07D263/32 ,  C07D277/22 ,  C07D277/68 ,  C07D295/04 ,  C07D295/096 ,  C07D295/16 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D451/02 ,  C07D451/04

摘要： This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

摘要翻译： 本发明涉及式（I）化合物：其中r，q，R，R2，R3，R4，R5a，R5b，R5c，R6a，R6b，R6c，R7，R8和R9在本文中描述为单立体异构体 或作为立体异构体或其药学上可接受的盐，溶剂合物，包合物，多晶型物，铵离子，N-氧化物或前药的混合物; 其是白三烯A4水解酶抑制剂，因此可用于治疗炎症性疾病。 还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。

公开(公告)号：US20200308181A1

公开(公告)日：2020-10-01

申请号：US16738190

申请日：2020-01-09

申请人： Celtaxsys, Inc.

发明人： Damian O. Arnaiz ,  Greg Brown ,  Emmanuel Claret ,  Arwed Cleve ,  David Davey ,  William Guilford ,  Seock-Kyu Khim ,  Thomas Kirkland ,  Monica J. Kochanny ,  Amy Liang ,  David Light ,  John Parkinson ,  Guo Ping Wei ,  Bin Ye

IPC分类号： C07D487/08 ,  C07C217/58 ,  C07C229/38 ,  C07C233/78 ,  C07C255/57 ,  C07C271/20 ,  C07D207/04 ,  C07D211/58 ,  C07D243/08 ,  C07D295/04 ,  C07D295/16 ,  C07D451/04 ,  C07D207/09 ,  C07D211/26 ,  C07D263/32 ,  C07D295/096 ,  C07D401/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07C229/08 ,  C07D263/14 ,  C07D401/12 ,  C07D207/16 ,  C07D211/34 ,  C07D277/22 ,  C07D277/68 ,  C07D451/02

摘要： This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

公开(公告)号：US20180230159A1

公开(公告)日：2018-08-16

申请号：US15891585

申请日：2018-02-08

申请人： Celtaxsys, Inc.

发明人： Damian O. Arnaiz ,  Greg Brown ,  Emmanuel Claret ,  Arwed Cleve ,  David Davey ,  William Guilford ,  Seock-Kyu Khim ,  Thomas Kirkland ,  Monica J. Kochanny ,  Amy Liang ,  David Light ,  John Parkinson ,  Guo Ping Wei ,  Bin Ye

IPC分类号： C07D487/08 ,  C07D263/32 ,  C07C271/20 ,  C07D211/58 ,  C07C229/38 ,  C07C229/08 ,  C07D295/096 ,  C07C255/57 ,  C07D211/34 ,  C07D207/04 ,  C07D401/12 ,  C07D243/08 ,  C07D295/16 ,  C07D295/04 ,  C07D451/04 ,  C07D277/68 ,  C07D401/10 ,  C07C217/58 ,  C07D207/09 ,  C07D405/12 ,  C07D403/12 ,  C07D409/12 ,  C07D211/26 ,  C07D413/12 ,  C07D451/02 ,  C07D277/22 ,  C07C233/78 ,  C07D263/14 ,  C07D207/16

CPC分类号： C07D487/08 ,  C07B2200/07 ,  C07C217/58 ,  C07C229/08 ,  C07C229/38 ,  C07C233/78 ,  C07C255/57 ,  C07C271/20 ,  C07C2601/14 ,  C07D207/04 ,  C07D207/09 ,  C07D207/16 ,  C07D211/26 ,  C07D211/34 ,  C07D211/58 ,  C07D243/08 ,  C07D263/14 ,  C07D263/32 ,  C07D277/22 ,  C07D277/68 ,  C07D295/04 ,  C07D295/096 ,  C07D295/16 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D451/02 ,  C07D451/04

摘要： This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

公开(公告)号：US20160272649A1

公开(公告)日：2016-09-22

申请号：US15069484

申请日：2016-03-14

申请人： Celtaxsys, Inc.

发明人： Damian O. Arnaiz ,  Greg Brown ,  Emmanuel Claret ,  Arwed Cleve ,  David Davey ,  William Guilford ,  Seock-Kyu Khim ,  Thomas Kirkland ,  Monica J. Kochanny ,  Amy Liang ,  David Light ,  John Parkinson ,  Guo Ping Wei ,  Bin Ye

IPC分类号： C07D487/08 ,  C07D263/32 ,  C07D211/58 ,  C07D277/22 ,  C07D207/09 ,  C07D207/16 ,  C07D451/02 ,  C07D277/68 ,  C07D295/16 ,  C07D211/34

CPC分类号： C07D487/08 ,  C07B2200/07 ,  C07C217/58 ,  C07C229/08 ,  C07C229/38 ,  C07C233/78 ,  C07C255/57 ,  C07C271/20 ,  C07C2601/14 ,  C07D207/04 ,  C07D207/09 ,  C07D207/16 ,  C07D211/26 ,  C07D211/34 ,  C07D211/58 ,  C07D243/08 ,  C07D263/14 ,  C07D263/32 ,  C07D277/22 ,  C07D277/68 ,  C07D295/04 ,  C07D295/096 ,  C07D295/16 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D451/02 ,  C07D451/04

摘要： This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

摘要翻译： 其中r，q，R，R2，R3，R4，R5a，R5b，R5c，R6a，R6b，R6c，R6a，R6b，R6c，R7，R8和R9在本文中作为单一立体异构体或立体异构体的混合物或其药学上可接受的盐，溶剂合物 ，包合物，多晶型物，铵离子，N-氧化物或前药; 其是白三烯A4水解酶抑制剂，因此可用于治疗炎症性疾病。 还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。

公开(公告)号：US09315509B2

公开(公告)日：2016-04-19

申请号：US14313672

申请日：2014-06-24

申请人： Celtaxsys, Inc.

发明人： Damian O. Arnaiz ,  Greg Brown ,  Emmanuel Claret ,  Arwed Cleve ,  David Davey ,  William Guilford ,  Seock-Kyu Khim ,  Thomas Kirkland ,  Monica J. Kochanny ,  Amy Liang ,  David Light ,  John Parkinson ,  Guo Ping Wei ,  Bin Ye

IPC分类号： A61K31/495 ,  C07D241/36 ,  C07D487/08 ,  C07C217/58 ,  C07C229/38 ,  C07C233/78 ,  C07C255/57 ,  C07C271/20 ,  C07D207/04 ,  C07D211/58 ,  C07D243/08 ,  C07D295/04 ,  C07D295/16 ,  C07D451/04 ,  C07D207/09 ,  C07D211/26 ,  C07D263/32 ,  C07D295/096 ,  C07D401/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07C229/08 ,  C07D263/14 ,  C07D401/12

CPC分类号： C07D487/08 ,  C07B2200/07 ,  C07C217/58 ,  C07C229/08 ,  C07C229/38 ,  C07C233/78 ,  C07C255/57 ,  C07C271/20 ,  C07C2601/14 ,  C07D207/04 ,  C07D207/09 ,  C07D207/16 ,  C07D211/26 ,  C07D211/34 ,  C07D211/58 ,  C07D243/08 ,  C07D263/14 ,  C07D263/32 ,  C07D277/22 ,  C07D277/68 ,  C07D295/04 ,  C07D295/096 ,  C07D295/16 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D451/02 ,  C07D451/04

摘要： This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

公开(公告)号：US20130123243A1

公开(公告)日：2013-05-16

申请号：US13654669

申请日：2012-10-18

申请人： Celtaxsys, Inc.

发明人： Damian O. Arnaiz ,  Greg Brown ,  Emmanuel Claret ,  Arwed Cleve ,  David Davey ,  William Guilford ,  Seok-Kyu Khim ,  Thomas Kirkland ,  Monica J. Kochanny ,  Amy Liang ,  David Light ,  John Parkinson ,  David Vogel ,  Guo Ping Wei ,  Bin Ye

IPC分类号： C07D487/08 ,  C07D263/32 ,  C07D211/58 ,  C07D211/26 ,  C07D207/09 ,  C07D295/096 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D401/10 ,  C07C229/38 ,  C07D243/08 ,  C07D451/04

CPC分类号： C07D487/08 ,  C07B2200/07 ,  C07C217/58 ,  C07C229/08 ,  C07C229/38 ,  C07C233/78 ,  C07C255/57 ,  C07C271/20 ,  C07C2601/14 ,  C07D207/04 ,  C07D207/09 ,  C07D207/16 ,  C07D211/26 ,  C07D211/34 ,  C07D211/58 ,  C07D243/08 ,  C07D263/14 ,  C07D263/32 ,  C07D277/22 ,  C07D277/68 ,  C07D295/04 ,  C07D295/096 ,  C07D295/16 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D451/02 ,  C07D451/04

摘要： This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.