公开(公告)号：US09376429B2

公开(公告)日：2016-06-28

申请号：US14435473

申请日：2013-10-15

申请人： Daewoong Pharmaceutical Co., Ltd.

发明人： Ha Young Kim ,  In Woo Kim ,  Sun Ah Jun ,  Yun Soo Na ,  Hyung Geun Lee ,  Min Jae Cho ,  Jun Hee Lee ,  Hyo Shin Kim ,  Yun Soo Yoon ,  Kyung Ha Chung ,  Ji Duck Kim

IPC分类号： C07D417/12 ,  C07D417/14

CPC分类号： C07D417/12 ,  C07D417/14

摘要： The present invention relates to a compound having a blocking effect against sodium ion channels, particularly Nav1.7, a preparation method thereof and the use thereof. A compound represented by formula 1 according to the invention, or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof may be effectively used for the prevention or treatment of pain, for example, acute pain, chronic pain, neuropathic pain, post-surgery pain, migraine, arthralgia, neuropathy, nerve injury, diabetic neuropathy, neuropathic disease, epilepsy, arrhythmia, myotonia, ataxia, multiple sclerosis, irritable bowel syndrome, urinary incontinence, visceral pain, depression, erythromelalgia, or paroxysmal extreme pain disorder (PEPD).

摘要翻译： 本发明涉及对钠离子通道具有阻塞作用的化合物，特别涉及Nav1.7，其制备方法及其应用。 根据本发明的由式1表示的化合物或其药学上可接受的盐，水合物，溶剂合物或异构体可以有效地用于预防或治疗疼痛，例如急性疼痛，慢性疼痛，神经性疼痛，手术后 疼痛，偏头痛，关节痛，神经病变，神经损伤，糖尿病性神经病变，神经病变，癫痫，心律失常，肌强直，共济失调，多发性硬化症，肠易激综合征，尿失禁，内脏痛，抑郁症，红斑性疼痛或阵发性极度疼痛障碍（PEPD） 。

公开(公告)号：US10590078B2

公开(公告)日：2020-03-17

申请号：US15526431

申请日：2016-02-11

申请人： Daewoong Pharmaceutical Co., Ltd.

发明人： Ji Duck Kim ,  Hyung Geun Lee ,  Inwoo Kim ,  Sun Ah Jun ,  Myunggi Jung ,  Hyo Shin Kim

IPC分类号： A61K31/437 ,  A61K31/416 ,  A61K31/4439 ,  C07D209/10 ,  C07D231/56 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/10 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D403/12 ,  C07D209/30 ,  C07D209/42 ,  C07D401/12

摘要： The present invention relates to a compound having a blocking effect against sodium ion channels, particularly Nav1.7, a preparation method thereof and use thereof. The compound represented by the Formula 1 or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof can be effectively used in the prevention or treatment of pains, for example, acute pain, chronic pain, pain from nervous disease, postoperative pain, migraine, arthralgia, neuropathy, nerve injury, diabetic neuropathy, neuropathic disease, epilepsy, arrhythmia, myotonia, ataxia, multiple sclerosis, irritable bowel syndrome, urinary incontinence, visceral pain, depression, erythromelalgia, paroxysmal extreme pain disorder (PEPD).

公开(公告)号：US10227338B2

公开(公告)日：2019-03-12

申请号：US15771775

申请日：2016-11-11

申请人： Daewoong Pharmaceutical Co., Ltd.

发明人： Hyung-Geun Lee ,  Il-Hwan Kim ,  Myunggi Jung ,  Hyo Shin Kim ,  Chun Ho Lee ,  Sun Ah Jun ,  Ji Sung Yoon ,  Sung-Young Kim

IPC分类号： A61K31/18 ,  C07C311/21 ,  C07D417/12 ,  A61K31/427 ,  A61K31/497 ,  C07D417/14 ,  C07D277/52

摘要： The invention relates to a compound represented by Chemical Formula 1, below, a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the compound or salt. The compound of the invention or pharmaceutically acceptable salts thereof can be used for the prevention or treatment of sodium channel blocker-related diseases. in Chemical Formula 1, R1 is hydrogen, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, halogen, or cyano, R2 and R3 are each independently hydrogen, or halogen, R4 is C5-10 heteroaryl containing one or two elements each independently selected from the group consisting of N, S and O, wherein the C5-10 heteroaryl is unsubstituted or substituted with C1-4 alkyl or halogen, R5 is —CH2CH2—N(R7)(R8), or —CH2CH2CH2—N(R7)(R8), R6 is hydrogen, or C1-4 alkyl; or R5 and R6 together form C3-5 alkylene, (C2-4 alkylene)-N(R9)—(C2-4 alkylene), or (C2-4 alkylene)-O—(C2-4 alkylene), wherein the C3-5 alkylene, or C2-4 alkylene is each independently unsubstituted or substituted with one or two R10, R7, R8, and R9 are each independently hydrogen, or C1-4 alkyl, R10 is C1-4 alkyl, C1-4 alkoxy, halogen, amino, NH(C1-4 alkyl), N(C1-4 alkyl)2, NHCO(C1-4 alkyl), or pyrrolidinyl, X1 is C—R′, or N, wherein R′ is hydrogen, or halogen, X2 is CH, or N, and X3 is N—R″, wherein R″ is hydrogen, or C1-4 alkyl.

公开(公告)号：US20150336944A1

公开(公告)日：2015-11-26

申请号：US14435473

申请日：2013-10-15

申请人： DAEWOONG PHARMACEUTICAL CO., LTD.

发明人： Ha Young Kim ,  In Woo Kim ,  Sun Ah Jun ,  Yun Soo Na ,  Hyung Geun Lee ,  Min Jae Cho ,  Jun Hee Lee ,  Hyo Shin Kim ,  Yun Soo Yoon ,  Kyung Ha Chung ,  Ji Duck Kim

IPC分类号： C07D417/12 ,  C07D417/14

CPC分类号： C07D417/12 ,  C07D417/14

摘要： The present invention relates to a compound having a blocking effect against sodium ion channels, particularly Nav1.7, a preparation method thereof and the use thereof. A compound represented by formula 1 according to the invention, or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof may be effectively used for the prevention or treatment of pain, for example, acute pain, chronic pain, neuropathic pain, post-surgery pain, migraine, arthralgia, neuropathy, nerve injury, diabetic neuropathy, neuropathic disease, epilepsy, arrhythmia, myotonia, ataxia, multiple sclerosis, irritable bowel syndrome, urinary incontinence, visceral pain, depression, erythromelalgia, or paroxysmal extreme pain disorder (PEPD).

摘要翻译： 本发明涉及对钠离子通道具有阻塞作用的化合物，特别涉及Nav1.7，其制备方法及其应用。 根据本发明的由式1表示的化合物或其药学上可接受的盐，水合物，溶剂合物或异构体可以有效地用于预防或治疗疼痛，例如急性疼痛，慢性疼痛，神经性疼痛，手术后 疼痛，偏头痛，关节痛，神经病变，神经损伤，糖尿病性神经病变，神经病变，癫痫，心律失常，肌强直，共济失调，多发性硬化症，肠易激综合征，尿失禁，内脏痛，抑郁症，红斑性疼痛或阵发性极度疼痛障碍（PEPD） 。