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1.发明授权Aryl substituted carboxamide derivatives as calcium or sodium channel blockers 有权芳基取代的甲酰胺衍生物作为钙或钠通道阻断剂公开(公告)号：US09101616B2
公开(公告)日：2015-08-11
申请号：US13375117
申请日：2010-05-31
申请人： Tadashi Inoue , Shuzo Watanabe , Tatsuya Yamagishi , Yoshimasa Arano , Mikio Morita , Kaoru Shimada
发明人： Tadashi Inoue , Shuzo Watanabe , Tatsuya Yamagishi , Yoshimasa Arano , Mikio Morita , Kaoru Shimada
IPC分类号： A61K31/498 , C07D401/12 , C07D213/65 , C07D241/18 , A61K31/497 , A61K31/444 , A61K31/44 , A61K31/4965 , A61K31/4439 , A61K31/4709 , C07D413/12 , A61K31/4725 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4706 , A61K31/506 , C07D215/40 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4706 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/506 , C07D213/65 , C07D215/40 , C07D241/18 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as NaV1.3 and NaV1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.
摘要翻译： 本发明涉及式（I）的芳基取代的甲酰胺衍生物或其药学上可接受的盐，其具有作为河豚毒素敏感型（TTX-S）阻滞剂如NaV1的T型钙通道或电压门控钠通道的阻断活性 3和NaV1.7，其可用于治疗或预防其中涉及T型钙通道或电压门控钠通道的疾病和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及T型钙通道或电压门控钠通道的疾病中的用途。
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公开(公告)号：US20120232052A1
公开(公告)日：2012-09-13
申请号：US13509442
申请日：2010-11-16
IPC分类号： A61K31/4545 , A61K31/5377 , A61K31/502 , A61K31/498 , A61K31/506 , A61K31/519 , A61K31/4375 , A61K31/437 , A61K31/4725 , A61K31/4709 , C07D405/06 , A61K31/454 , C07D498/04 , C07D413/14 , C07D487/04 , C07D471/04 , C07D401/06 , C07D401/10 , C07D417/10 , C07D413/06 , C07D401/14 , A61P25/00 , A61P29/00 , A61P25/28 , A61P1/00 , A61P19/02 , A61P25/06 , A61P25/08 , A61P25/24 , A61P25/18 , A61P25/22 , A61P35/00 , A61K31/5383
CPC分类号： C07D401/06 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/4745 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/5383 , C07D211/46 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D413/06 , C07D417/06 , C07D417/10 , C07D455/04 , C07D471/04 , C07D471/06 , C07D487/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to aryl carboxamide derivatives of formula (I), wherein Ar1 is phenyl; Ar2 is aryl; n is 1-4; X is —O—, —S—, —SO— or —SO2—, a prodrug thereof or a pharmaceutically acceptable salt thereof, which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of such disorders and diseases as pain in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases as pain in which voltage gated sodium channels are involved.
摘要翻译： 本发明涉及式（I）的芳基甲酰胺衍生物，其中Ar 1是苯基; Ar2是芳基; n为1-4; X是-O - ， - S-，-SO-或-SO 2 - ，其前药或其药学上可接受的盐，其具有作为TTX-S通道的电压门控钠通道的阻断活性，并且其可用于 治疗或预防这种疾病和疾病，如涉及电压门控钠通道的疼痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗诸如涉及电压门控钠通道的疼痛的疾病中的用途。
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3.发明申请ARYL SUBSTITUTED CARBOXAMIDE DERIVATIVES AS CALCIUM OR SODIUM CHANNEL BLOCKERS 有权ARYL替代羧酰胺衍生物作为钙或钠通道阻断剂公开(公告)号：US20120101105A1
公开(公告)日：2012-04-26
申请号：US13375117
申请日：2010-05-31
申请人： Tadashi Inoue , Shuzo Watanabe , Tatsuya Yamagishi , Yoshimasa Arano , Mikio Morita , Kaoru Shimada
发明人： Tadashi Inoue , Shuzo Watanabe , Tatsuya Yamagishi , Yoshimasa Arano , Mikio Morita , Kaoru Shimada
IPC分类号： A61K31/498 , C07D401/12 , C07D213/65 , C07D241/18 , A61K31/497 , A61K31/444 , A61K31/44 , A61K31/4965 , A61K31/4439 , A61P29/00 , A61P25/16 , A61P25/18 , A61P25/00 , A61P1/00 , A61P35/00 , A61P25/28 , A61P25/02 , A61P25/24 , A61P25/08 , A61P25/06 , A61P5/00 , A61P19/00 , A61P25/22 , C07D413/12 , A61K31/4709 , A61K31/4725 , A61K31/506 , A61P25/14 , A61P25/20 , A61P19/02 , A61P9/06 , A61P1/18 , C07D403/12
CPC分类号： A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4706 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/506 , C07D213/65 , C07D215/40 , C07D241/18 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Nav1.3 and Nav1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.
摘要翻译： 本发明涉及式（I）的芳基取代的甲酰胺衍生物或其药学上可接受的盐，其具有T型钙通道或电压门控钠通道的阻断活性，作为河豚毒素敏感型（TTX-S）阻断剂如Nav1 3和Nav1.7，其可用于治疗或预防其中涉及T型钙通道或电压门控钠通道的疾病和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及T型钙通道或电压门控钠通道的疾病中的用途。
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公开(公告)号：US09051296B2
公开(公告)日：2015-06-09
申请号：US13509442
申请日：2010-11-16
IPC分类号： A61K31/435 , A01N43/40 , C07D221/04 , C07D401/06 , A61K31/44 , A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/4745 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/5383 , C07D211/46 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D413/06 , C07D417/06 , C07D417/10 , C07D455/04 , C07D471/04 , C07D471/06 , C07D487/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04
CPC分类号： C07D401/06 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/4745 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/5383 , C07D211/46 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D413/06 , C07D417/06 , C07D417/10 , C07D455/04 , C07D471/04 , C07D471/06 , C07D487/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to aryl carboxamide derivatives of formula (I), wherein Ar1 is phenyl; Ar2 is aryl; n is 1-4; X is —O—, —S—, —SO— or —SO2—, a prodrug thereof or a pharmaceutically acceptable salt thereof, which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of such disorders and diseases as pain in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases as pain in which voltage gated sodium channels are involved.
摘要翻译： 本发明涉及式（I）的芳基甲酰胺衍生物，其中Ar 1是苯基; Ar2是芳基; n为1-4; X是-O - ， - S-，-SO-或-SO 2 - ，其前药或其药学上可接受的盐，其具有作为TTX-S通道的电压门控钠通道的阻断活性，并且其可用于 治疗或预防这种疾病和疾病，如涉及电压门控钠通道的疼痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗诸如涉及电压门控钠通道的疼痛的疾病中的用途。
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公开(公告)号：US20140336377A1
公开(公告)日：2014-11-13
申请号：US13879673
申请日：2011-10-18
IPC分类号： C07D213/64 , C07D213/75 , C07D239/42 , C07D471/04 , C07D413/12 , C07D413/14 , C07D401/12 , C07D401/14
CPC分类号： C07D213/64 , A61K31/44 , A61K31/4427 , A61K31/444 , A61K31/506 , C07D213/75 , C07D213/81 , C07D239/42 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention relates to arylamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
摘要翻译： 本发明涉及具有电压门控钠通道作为TTX-S通道的阻断活性的芳基酰胺衍生物，其可用于治疗或预防涉及电压门控钠通道的疾病和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及电压门控钠通道的疾病中的用途。
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公开(公告)号：US09302991B2
公开(公告)日：2016-04-05
申请号：US13879673
申请日：2011-10-18
IPC分类号： C07D213/64 , A61K31/44 , A61K31/4427 , A61K31/444 , A61K31/506 , C07D213/75 , C07D213/81 , C07D239/42 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
CPC分类号： C07D213/64 , A61K31/44 , A61K31/4427 , A61K31/444 , A61K31/506 , C07D213/75 , C07D213/81 , C07D239/42 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention relates to arylamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
摘要翻译： 本发明涉及具有电压门控钠通道作为TTX-S通道的阻断活性的芳基酰胺衍生物，其可用于治疗或预防涉及电压门控钠通道的疾病和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及电压门控钠通道的疾病中的用途。
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公开(公告)号：US20120142691A1
公开(公告)日：2012-06-07
申请号：US13388740
申请日：2010-08-04
申请人： Hirohide Noguchi , Tadashi Inoue , Mikio Morita , Yoshimasa Arano
发明人： Hirohide Noguchi , Tadashi Inoue , Mikio Morita , Yoshimasa Arano
IPC分类号： A61K31/5377 , C07D401/14 , C07D413/14 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61P1/00 , A61P25/00 , A61P19/08 , A61P19/02 , A61P1/18 , A61P25/08 , A61P9/06 , A61P25/22 , A61P25/24 , A61P5/00 , A61P29/00 , C07D401/12
CPC分类号： C07D401/12 , A61K31/4433 , A61K31/4439 , A61K31/497 , A61K31/5377 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
摘要翻译： 本发明涉及具有电压门控钠通道作为TTX-S通道的阻断活性的吡啶酰胺衍生物，其可用于治疗或预防涉及电压门控钠通道的疾病和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及电压门控钠通道的疾病中的用途。
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公开(公告)号：US08809380B2
公开(公告)日：2014-08-19
申请号：US13388740
申请日：2010-08-04
申请人： Hirohide Noguchi , Tadashi Inoue , Mikio Morita , Yoshimasa Arano
发明人： Hirohide Noguchi , Tadashi Inoue , Mikio Morita , Yoshimasa Arano
IPC分类号： A61K31/4439
CPC分类号： C07D401/12 , A61K31/4433 , A61K31/4439 , A61K31/497 , A61K31/5377 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
摘要翻译： 本发明涉及具有电压门控钠通道作为TTX-S通道的阻断活性的吡啶酰胺衍生物，其可用于治疗或预防涉及电压门控钠通道的疾病和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及电压门控钠通道的疾病中的用途。
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公开(公告)号：US08697877B2
公开(公告)日：2014-04-15
申请号：US13203301
申请日：2010-03-01
申请人： Masaki Sudo , Yasuhiro Iwata , Yoshimasa Arano , Madoka Jinno , Masashi Ohmi , Hirohide Noguchi
发明人： Masaki Sudo , Yasuhiro Iwata , Yoshimasa Arano , Madoka Jinno , Masashi Ohmi , Hirohide Noguchi
IPC分类号： C07D401/04 , A61K31/454
CPC分类号： C07D401/04 , C07D401/14
摘要： The present invention relates to novel oxyindole derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the motilin receptor (GPR38).
摘要翻译： 本发明涉及式（I）的新型氧吲哚衍生物或其药学上可接受的盐，其制备方法，含有它们的药物组合物及其用于治疗通过胃动素受体（GPR38）介导的各种病症的用途。
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公开(公告)号：US20110312933A1
公开(公告)日：2011-12-22
申请号：US13203301
申请日：2010-03-01
申请人： Masaki Sudo , Yasuhiro Iwata , Yoshimasa Arano , Madoka Jinno , Masashi Ohmi , Hirohide Noguchi
发明人： Masaki Sudo , Yasuhiro Iwata , Yoshimasa Arano , Madoka Jinno , Masashi Ohmi , Hirohide Noguchi
IPC分类号： A61K31/454 , C07D401/04 , A61P1/04 , A61K31/496 , A61P1/00 , C07D401/14 , A61K31/4545
CPC分类号： C07D401/04 , C07D401/14
摘要： The present invention relates to novel oxyindole derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the motilin receptor (GPR38).
摘要翻译： 本发明涉及式（I）的新型氧吲哚衍生物或其药学上可接受的盐，其制备方法，含有它们的药物组合物及其用于治疗通过胃动素受体（GPR38）介导的各种病症的用途。
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