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公开(公告)号：US20050119499A1
公开(公告)日：2005-06-02
申请号：US10507831
申请日：2003-03-14
申请人： Masayuki Nakamura , Jun Inoue
发明人： Masayuki Nakamura , Jun Inoue
IPC分类号： A61P9/00 , A61P9/10 , A61P19/02 , A61P21/04 , A61P25/28 , A61P27/12 , A61P43/00 , C07D307/22 , C07F9/02
CPC分类号： C07D307/22
摘要： A compound represented by the following formula (I) wherein R1 is a lower alkyl group, R2 is a hydrogen, a halogen, a cyano group, a lower alkyl group or a lower alkoxy group, and n is 0 or 1, which has a calpain inhibitory activity, is provided.
摘要翻译： 由下式（I）表示的化合物，其中R 1为低级烷基，R 2为氢，卤素，氰基，低级烷基 或低级烷氧基，并且n为0或1，其具有钙蛋白酶抑制活性。
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公开(公告)号：US06551999B1
公开(公告)日：2003-04-22
申请号：US09243822
申请日：1999-02-03
申请人： Chiho Fukiage , Mitsuyoshi Azuma , Jun Inoue , Masayuki Nakamura , Yuka Yoshida
发明人： Chiho Fukiage , Mitsuyoshi Azuma , Jun Inoue , Masayuki Nakamura , Yuka Yoshida
IPC分类号： C07K506
CPC分类号： A61K38/55 , C07C311/19 , C07D303/48
摘要： An angiogenesis inhibitor comprising a cysteine protease inhibitory compound. As the preferable cysteine protease inhibitory compound, epoxysuccinic acid compounds, peptide halohydrazide compounds, calpain inhibitory compounds, compounds of the formula (I) and compounds of the formula (VI) can be used. The angiogenesis inhibitor of the present invention suppresses new formation of blood vessels in the living tissues, so that it can be used as a superior therapeutic or prophylactic agent of angiogenesis associated with wound healing, inflammation, growth of tumor and the like; and angiogenesis as seen in diabetic retinopathy, prematurity retinopathy, retinal venous occlusion, senile discoid macular degeneration and the like, as well as for prevention of metastasis of tumors.
摘要翻译： 一种包含半胱氨酸蛋白酶抑制化合物的血管生成抑制剂。 作为优选的半胱氨酸蛋白酶抑制化合物，可以使用环氧琥珀酸化合物，肽卤代酰肼化合物，钙蛋白酶抑制化合物，式（I）的化合物和式（VI）的化合物。 本发明的血管发生抑制剂抑制活组织中血管的新形成，可以用作与伤口愈合，炎症，肿瘤生长等有关的血管生成的优异治疗或预防剂。 和血管生成，如糖尿病视网膜病变，早产儿视网膜病变，视网膜静脉闭塞，老年性盘状黄斑变性等，以及用于预防肿瘤转移。
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公开(公告)号：US07022738B2
公开(公告)日：2006-04-04
申请号：US10521764
申请日：2003-07-11
申请人： Masayuki Nakamura , Jun Inoue
发明人： Masayuki Nakamura , Jun Inoue
IPC分类号： A61K31/18 , A61K38/05 , C07C311/18
CPC分类号： C07C311/19
摘要： The present invention provides a compound represented by the formula (I): wherein R1, R2 and R3 each represents a lower alkyl group.
摘要翻译： 本发明提供由式（I）表示的化合物：其中R 1，R 2和R 3各自表示低级烷基 。
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公开(公告)号：US20050176704A1
公开(公告)日：2005-08-11
申请号：US10509253
申请日：2003-03-27
申请人： Masayuki Nakamura , Jun Inoue
发明人： Masayuki Nakamura , Jun Inoue
IPC分类号： A61K31/5375 , A61P9/00 , A61P9/10 , A61P19/10 , A61P25/00 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/12 , A61P37/02 , A61P43/00 , C07D265/32 , A61K31/537
CPC分类号： A61K31/5375 , C07D265/32
摘要： A compound represented by the following formula (I) wherein R1 and R2 are each a lower alkyl group optionally having substituents, which has a calpain inhibitory activity, or a salt thereof is provided.
摘要翻译： 由下式（I）表示的化合物，其中R 1和R 2各自为任选具有钙蛋白酶抑制活性的取代基的低级烷基或盐 提供。
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公开(公告)号：US20070004643A1
公开(公告)日：2007-01-04
申请号：US10582015
申请日：2004-12-08
CPC分类号： C07D213/30 , C07C271/22 , C07C2601/02 , C07C2601/04 , C07C2602/08 , C07D295/215 , C07D307/20 , C07D309/12
摘要： The present invention provides a compound represented by the formula (I): (wherein R1 is a lower alkyl substituted by a lower alkoxy or a heterocyclic group, or a heterocyclic group; R2 is a lower alkyl optionally substituted by a phenyl; and R3 is a lower alkyl optionally substituted by a halogen, a lower alkoxy or a phenyl, or a fused polycyclic hydrocarbon group), which is well absorbed orally, exhibits durability of good blood level and has potent calpain inhibitory activity.
摘要翻译： 本发明提供由式（I）表示的化合物：其中R 1是被低级烷氧基或杂环基或杂环基取代的低级烷基; R 2， / SUP>是任选被苯基取代的低级烷基; R 3是任选被卤素，低级烷氧基或苯基或稠合多环烃基取代的低级烷基，其是 良好的口腔吸收，具有良好的血液水平的耐久性，并具有强大的钙蛋白酶抑制活性。
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公开(公告)号：US6057290A
公开(公告)日：2000-05-02
申请号：US740069
申请日：1996-10-24
申请人： Chiho Fukiage , Mitsuyoshi Azuma , Jun Inoue , Masayuki Nakamura , Yuka Yoshida
发明人： Chiho Fukiage , Mitsuyoshi Azuma , Jun Inoue , Masayuki Nakamura , Yuka Yoshida
IPC分类号： A61K38/55 , C07C311/19 , C07D303/48 , A61K38/00 , C07K5/00 , C07K7/00
CPC分类号： A61K38/55 , C07C311/19 , C07D303/48
摘要： An angiogenesis inhibitor comprising a cysteine protease inhibitory compound. As the preferable cysteine protease inhibitory compound, epoxysuccinic acid compounds, peptide halohydrazide compounds, calpain inhibitory compounds, compounds of the formula (I) ##STR1## and compounds of the formula (VI) ##STR2## can be used. The angiogenesis inhibitor of the present invention suppresses new formation of blood vessels in the living tissues, so that it can be used as a superior therapeutic or prophylactic agent of angiogenesis associated with wound healing, inflammation, growth of tumor and the like; and angiogenesis as seen in diabetic retinopathy, prematurity retinopathy, retinal venous occlusion, senile discoid macular degeneration and the like, as well as for prevention of metastasis of tumors.
摘要翻译： 一种包含半胱氨酸蛋白酶抑制化合物的血管生成抑制剂。 作为优选的半胱氨酸蛋白酶抑制化合物，可以使用环氧琥珀酸化合物，肽卤代酰肼化合物，钙蛋白酶抑制化合物，式（I）的化合物和式（VI）的化合物。 本发明的血管发生抑制剂抑制活组织中血管的新形成，可以用作与伤口愈合，炎症，肿瘤生长等有关的血管生成的优异治疗或预防剂。 和血管生成，如糖尿病视网膜病变，早产儿视网膜病变，视网膜静脉闭塞，老年性盘状黄斑变性等，以及用于预防肿瘤转移。
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公开(公告)号：US07202274B2
公开(公告)日：2007-04-10
申请号：US10507831
申请日：2003-03-14
申请人： Masayuki Nakamura , Jun Inoue
发明人： Masayuki Nakamura , Jun Inoue
IPC分类号： A61K31/341 , C07D307/20 , C07D307/22
CPC分类号： C07D307/22
摘要： A compound represented by the following formula (I) wherein R1 is a lower alkyl group, R2 is a hydrogen, a halogen, a cyano group, a lower alkyl group or a lower alkoxy group, and n is 0 or 1, which has a calpain inhibitory activity, is provided.
摘要翻译： 由下式（I）表示的化合物
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公开(公告)号：US06214800B1
公开(公告)日：2001-04-10
申请号：US09282501
申请日：1999-04-09
申请人： Chiho Fukiage , Mitsuyoshi Azuma , Jun Inoue , Masayuki Nakamura , Yuka Yoshida
发明人： Chiho Fukiage , Mitsuyoshi Azuma , Jun Inoue , Masayuki Nakamura , Yuka Yoshida
IPC分类号： A61K3800
CPC分类号： A61K38/55 , C07C311/19 , C07D303/48
摘要： An angiogenesis inhibitor comprising a cysteine protease inhibitory compound. As the preferable cysteine protease inhibitory compound, epoxysuccinic acid compounds, peptide halohydrazide compounds, calpain inhibitory compounds, compounds of the formula (I) and compounds of the formula (VI) can be used. The angiogenesis inhibitor of the present invention suppresses new formation of blood vessels in the living tissues, so that it can be used as a superior therapeutic or prophylactic agent of angiogenesis associated with wound healing, inflammation, growth of tumor and the like; and angiogenesis as seen in diabetic retinopathy, prematurity retinopathy, retinal venous occlusion, senile discoid macular degeneration and the like, as well as for prevention of metastasis of tumors.
摘要翻译： 一种包含半胱氨酸蛋白酶抑制化合物的血管生成抑制剂。 作为优选的半胱氨酸蛋白酶抑制化合物，可以使用环氧琥珀酸化合物，肽卤代酰肼化合物，钙蛋白酶抑制化合物，式（I）的化合物和式（VI）的化合物。 本发明的血管发生抑制剂抑制活组织中血管的新形成，可以用作与伤口愈合，炎症，肿瘤生长等有关的血管生成的优异治疗或预防剂。 和血管生成，如糖尿病视网膜病变，早产儿视网膜病变，视网膜静脉闭塞，老年性盘状黄斑变性等，以及用于预防肿瘤转移。
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公开(公告)号：US07491705B2
公开(公告)日：2009-02-17
申请号：US10582015
申请日：2004-12-08
IPC分类号： A61K38/05
CPC分类号： C07D213/30 , C07C271/22 , C07C2601/02 , C07C2601/04 , C07C2602/08 , C07D295/215 , C07D307/20 , C07D309/12
摘要： The present invention provides a compound represented by the formula (I): (wherein R1 is a lower alkyl substituted by a lower alkoxy or a heterocyclic group, or a heterocyclic group; R2 is a lower alkyl optionally substituted by a phenyl; and R3 is a lower alkyl optionally substituted by a halogen, a lower alkoxy or a phenyl, or a fused polycyclic hydrocarbon group), which is well absorbed orally, exhibits durability of good blood level and has potent calpain inhibitory activity.
摘要翻译： 本发明提供由式（I）表示的化合物：其中R1是被低级烷氧基或杂环基取代的低级烷基或杂环基; R2是任意被苯基取代的低级烷基，R3是 被卤素，低级烷氧基或苯基或稠合多环烃基任选取代的低级烷基），其口服良好吸收，具有良好的血液水平的耐久性，并具有有效的钙蛋白酶抑制活性。
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公开(公告)号：US07223755B2
公开(公告)日：2007-05-29
申请号：US10509253
申请日：2003-03-27
申请人： Masayuki Nakamura , Jun Inoue
发明人： Masayuki Nakamura , Jun Inoue
IPC分类号： A61K31/5375 , C07D265/33
CPC分类号： A61K31/5375 , C07D265/32
摘要： A compound represented by the following formula (I) wherein R1 and R2 are each a lower alkyl group optionally having substituents, which has a calpain inhibitory activity, or a salt thereof is provided.
摘要翻译： 由下式（I）表示的化合物，其中R 1和R 2各自为任选具有钙蛋白酶抑制活性的取代基的低级烷基或盐 提供。
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