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公开(公告)号：US20110212919A1
公开(公告)日：2011-09-01
申请号：US13058647
申请日：2009-08-11
申请人： Katsuhiko Mikoshiba , Nobuyuki Nukina , Shoichiro Ozaki , Kouzo Hamada , Jun-Ichi Goto , Akinobu Suzuki , Etsuko Ebisui , Akiko Terauchi
发明人： Katsuhiko Mikoshiba , Nobuyuki Nukina , Shoichiro Ozaki , Kouzo Hamada , Jun-Ichi Goto , Akinobu Suzuki , Etsuko Ebisui , Akiko Terauchi
IPC分类号： A61K31/69 , C07F5/02 , C07F5/04 , A61P25/00 , A61P25/16 , A61P25/28 , A61P27/12 , A61P3/00 , A61P17/00 , A61P7/00
摘要： The present invention provides a protein cross-linking inhibitor containing a compound represented by any of the following formulas (1)-(13), or a pharmaceutically acceptable salt thereof: R3—[—X—B(ZR1)—Y—B(ZR2)—W—]n—R4, (1) R3—[—X—B(ZR1)—Y—]n—R4, (2) R3—[—B(ZR1)—Y—B(ZR2)—W—]n—R4, (3) R3—[—X—B(ZR1)—]n—R4, (4) R3—[—B(ZR2)—W—]n—R4, (5) R3—X—B(ZR1)-T[B(ZR2)—W—R4]2, (6) R3—B(OH)2, (7) R3—B(ZR1)—X—B(ZR2)—R4, (8) R3—B(R1)—O—B(R2)—R4, (9) R3—[—X—B(ZR1)—Y—B(ZR2)—]n—R4, (10) R3—[—X—B(ZR1)—Y—B(ZR2)—W-Q-]n—R4, (11) R3—[—P—X—B(ZR1)—Y—B(ZR2)—W—]n—R4, (12) [R3—X—B(ZR1)—Y]2B(ZR2), (13) wherein each symbol is as defined in the DESCRIPTION.
摘要翻译： 本发明提供一种蛋白质交联抑制剂，其含有下述式（1） - （13）中任一项所示的化合物或其药学上可接受的盐：R3 - [ - X-B（ZR1）-Y-B ZR2）-W-] n-R4，（1）R3 - [ - X-B（ZR1）-Y-] n-R4，（2）R3 - [ - B（ZR1）-Y-B（ZR2） - W - ] n-R4，（3）R3 - [ - X-B（ZR1） - ] n-R4，（4）R3 - [ - B（ZR2）-W-] n-R4，（5） X-B（ZR1）-T [B（ZR2）-W-R4] 2，（6）R3-B（OH）2，（7）R3-B（ZR1）-X-B（ZR2）-R4， （8）R3-B（R1）-O-B（R2）-R4，（9）R3 - [ - X-B（ZR1）-Y-B（ZR2） - ] n-R4，（10） [-X-B（ZR1）-Y-B（ZR2）-WQ-] n-R4，（11）R3 - [ - P-X-B（ZR1）-Y-B（ZR2）-W-] n -R4，（12）[R3-X-B（ZR1）-Y] 2B（ZR2），（13）其中每个符号如说明书中所定义。
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公开(公告)号：US08853424B2
公开(公告)日：2014-10-07
申请号：US13058647
申请日：2009-08-11
申请人： Katsuhiko Mikoshiba , Nobuyuki Nukina , Shoichiro Ozaki , Kouzo Hamada , Jun-Ichi Goto , Akinobu Suzuki , Etsuko Ebisui , Akiko Terauchi
发明人： Katsuhiko Mikoshiba , Nobuyuki Nukina , Shoichiro Ozaki , Kouzo Hamada , Jun-Ichi Goto , Akinobu Suzuki , Etsuko Ebisui , Akiko Terauchi
IPC分类号： C07D333/00 , A61K31/67 , C07F5/02 , A61K31/69
摘要： The present invention provides a protein cross-linking inhibitor containing a compound represented by any of the following formulas (1)-(13), or a pharmaceutically acceptable salt thereof: R3—[—X—B(ZR1)—Y—B(ZR2)—W—]n—R4, (1) R3—[—X—B(ZR1)—Y—]n—R4, (2) R3—[—B(ZR1)—Y—B(ZR2)—W—]n—R4, (3) R3—[—X—B(ZR1)—]n—R4, (4) R3—[—B(ZR2)—W—]n—R4, (5) R3—X—B(ZR1)-T[B(ZR2)—W—R4]2, (6) R3—B(OH)2, (7) R3—B(ZR1)—X—B(ZR2)—R4, (8) R3—B(R1)—O—B(R2)—R4, (9) R3—[—X—B(ZR1)—Y—B(ZR2)—]n—R4, (10) R3—[—X—B(ZR1)—Y—B(ZR2)—W-Q-]n—R4, (11) R3—[—P—X—B(ZR1)—Y—B(ZR2)—W—]n—R4, (12) [R3—X—B(ZR1)—Y]2B(ZR2), (13) wherein each symbol is as defined in the DESCRIPTION.
摘要翻译： 本发明提供一种蛋白质交联抑制剂，其含有下述式（1） - （13）中任一项所示的化合物或其药学上可接受的盐：R3 - [ - X-B（ZR1）-Y-B ZR2）-W-] n-R4，（1）R3 - [ - X-B（ZR1）-Y-] n-R4，（2）R3 - [ - B（ZR1）-Y-B（ZR2） - W - ] n-R4，（3）R3 - [ - X-B（ZR1） - ] n-R4，（4）R3 - [ - B（ZR2）-W-] n-R4，（5） X-B（ZR1）-T [B（ZR2）-W-R4] 2，（6）R3-B（OH）2，（7）R3-B（ZR1）-X-B（ZR2）-R4， （8）R3-B（R1）-O-B（R2）-R4，（9）R3 - [ - X-B（ZR1）-Y-B（ZR2） - ] n-R4，（10） [-X-B（ZR1）-Y-B（ZR2）-WQ-] n-R4，（11）R3 - [ - P-X-B（ZR1）-Y-B（ZR2）-W-] n -R4，（12）[R3-X-B（ZR1）-Y] 2B（ZR2），（13）其中每个符号如说明书中所定义。
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公开(公告)号：US08937091B2
公开(公告)日：2015-01-20
申请号：US13508247
申请日：2010-05-19
申请人： Katsuhiko Mikoshiba , Kozo Hamada , Akiko Terauchi , Shouichirou Ozaki , Jun-ichi Goto , Etsuko Ebisui , Akinobu Suzuki
发明人： Katsuhiko Mikoshiba , Kozo Hamada , Akiko Terauchi , Shouichirou Ozaki , Jun-ichi Goto , Etsuko Ebisui , Akinobu Suzuki
IPC分类号： A61K31/45 , C07D295/10 , A61K31/045 , A61K31/085 , A61K31/12 , A61K31/136 , A61K31/137 , A61K31/216 , A61K31/341 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/417 , A61K31/426 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/444 , A61K31/4453 , A61K31/4545 , A61K31/496 , A61K31/4965 , A61K31/5375 , A61K31/55
CPC分类号： A61K31/045 , A61K31/085 , A61K31/12 , A61K31/136 , A61K31/137 , A61K31/216 , A61K31/341 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/417 , A61K31/426 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/444 , A61K31/4453 , A61K31/4545 , A61K31/496 , A61K31/4965 , A61K31/5375 , A61K31/55
摘要： The present invention relates to: a ketone compound having transglutaminase-inhibiting activity, which is represented by the following Formula 1, 2, or 3: wherein R1 is a substituted or unsubstituted aryl or heterocyclyl group, R2, R3, and R4 are hydrogen atoms, n is 2, X is halogen, R5 and R6 independently represent a hydrogen atom or a substituted or unsubstituted C1-C10 alkyl, aryl, or aralkyl group, wherein R5 and R6 are not hydrogen atoms at the same time, or R5 and R6 may be taken together to form a saturated or unsaturated and substituted or unsubstituted heterocyclyl group containing a nitrogen atom (N); an inhibitor of protein crosslinking comprising the compound; and a composition for preventing or treating a protein-crosslinking causative disease, which comprises the compound or the protein crosslinking inhibitor.
摘要翻译： 本发明涉及：具有转谷氨酰胺酶抑制活性的酮化合物，其由下式1,2或3表示：其中R 1为取代或未取代的芳基或杂环基，R 2，R 3和R 4为氢原子 ，n为2，X为卤素，R5和R6独立地表示氢原子或取代或未取代的C1-C10烷基，芳基或芳烷基，其中R5和R6不同时为氢原子，或R5和R6 可以一起形成含有氮原子（N）的饱和或不饱和和取代或未取代的杂环基。 包含该化合物的蛋白质交联抑制剂; 和用于预防或治疗蛋白质交联致病性疾病的组合物，其包含该化合物或蛋白质交联抑制剂。
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公开(公告)号：US20120277423A1
公开(公告)日：2012-11-01
申请号：US13508247
申请日：2010-05-19
申请人： Katsuhiko Mikoshiba , Kozo Hamada , Akiko Terauchi , Shouichirou Ozaki , Jun-ichi Goto , Etsuko Ebisui , Akinobu Suzuki
发明人： Katsuhiko Mikoshiba , Kozo Hamada , Akiko Terauchi , Shouichirou Ozaki , Jun-ichi Goto , Etsuko Ebisui , Akinobu Suzuki
IPC分类号： C07D213/50 , C07D223/10 , C07D409/06 , C07D333/22 , C07D295/16
CPC分类号： A61K31/045 , A61K31/085 , A61K31/12 , A61K31/136 , A61K31/137 , A61K31/216 , A61K31/341 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/417 , A61K31/426 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/444 , A61K31/4453 , A61K31/4545 , A61K31/496 , A61K31/4965 , A61K31/5375 , A61K31/55
摘要： The present invention relates to: a ketone compound having transglutaminase-inhibiting activity, which is represented by the following Formula 1, 2, or 3: wherein R1 is a substituted or unsubstituted aryl or heterocyclyl group, R2, R3, and R4 are hydrogen atoms, n is 2, X is halogen, R5 and R6 independently represent a hydrogen atom or a substituted or unsubstituted C1-C10 alkyl, aryl, or aralkyl group, wherein R5 and R6 are not hydrogen atoms at the same time, or R5 and R6 may be taken together to form a saturated or unsaturated and substituted or unsubstituted heterocyclyl group containing a nitrogen atom (N); an inhibitor of protein crosslinking comprising the compound; and a composition for preventing or treating a protein-crosslinking causative disease, which comprises the compound or the protein crosslinking inhibitor.
摘要翻译： 本发明涉及：具有转谷氨酰胺酶抑制活性的酮化合物，其由下式1,2或3表示：其中R 1为取代或未取代的芳基或杂环基，R 2，R 3和R 4为氢原子 ，n为2，X为卤素，R5和R6独立地表示氢原子或取代或未取代的C1-C10烷基，芳基或芳烷基，其中R5和R6不同时为氢原子，或R5和R6 可以一起形成含有氮原子（N）的饱和或不饱和和取代或未取代的杂环基。 包含该化合物的蛋白质交联抑制剂; 和用于预防或治疗蛋白质交联致病性疾病的组合物，其包含该化合物或蛋白质交联抑制剂。
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