公开(公告)号：US07750155B2

公开(公告)日：2010-07-06

申请号：US12278580

申请日：2007-02-06

申请人： Fumiyuki Shirai ,  Hideo Tsutsumi ,  Hiromichi Itani ,  Yoshihiro Kozuki ,  Yoshiteru Eikyu ,  Taro Masunaga

发明人： Fumiyuki Shirai ,  Hideo Tsutsumi ,  Hiromichi Itani ,  Yoshihiro Kozuki ,  Yoshiteru Eikyu ,  Taro Masunaga

IPC分类号： C07D241/02

CPC分类号： C07D409/14 ,  C07D401/12 ,  C07D403/12

摘要： This invention relates to novel N-hydroxyacrylamide compounds of formula (I) and pharmaceutically acceptable salts thereof. More particularly, it relates to novel N-hydroxyacrylamide compounds and pharmaceutically acceptable salts thereof which act as a HDAC inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of HDAC-related disease.

摘要翻译： 本发明涉及式（I）的新型N-羟基丙烯酰胺化合物及其药学上可接受的盐。 更具体地说，本发明涉及作为HDAC抑制剂的新型N-羟基丙烯酰胺化合物及其药学上可接受的盐，涉及含有该N-羟基丙烯酰胺的HDAC抑制剂的药物组合物及其在治疗和/或预防HDAC相关性中的用途 疾病。

公开(公告)号：US20090054465A1

公开(公告)日：2009-02-26

申请号：US12278580

申请日：2007-02-06

申请人： Fumiyuki Shirai ,  Hideo Tsutsumi ,  Hiromichi Itani ,  Yoshihiro Kozuki ,  Yoshiteru Eikyu ,  Taro Masunaga

发明人： Fumiyuki Shirai ,  Hideo Tsutsumi ,  Hiromichi Itani ,  Yoshihiro Kozuki ,  Yoshiteru Eikyu ,  Taro Masunaga

IPC分类号： A61K31/497 ,  C07D403/12 ,  C07D401/12 ,  A61P29/00 ,  A61P3/00 ,  A61P37/00

CPC分类号： C07D409/14 ,  C07D401/12 ,  C07D403/12

摘要： This invention relates to novel N-hydroxyacrylamide compounds of formula (I) and pharmaceutically acceptable salts thereof. More particularly, it relates to novel N-hydroxyacrylamide compounds and pharmaceutically acceptable salts thereof which act as a HDAC inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of HDAC-related disease.

摘要翻译： 本发明涉及式（I）的新型N-羟基丙烯酰胺化合物及其药学上可接受的盐。 更具体地说，本发明涉及作为HDAC抑制剂的新型N-羟基丙烯酰胺化合物及其药学上可接受的盐，涉及含有该N-羟基丙烯酰胺的HDAC抑制剂的药物组合物及其在治疗和/或预防HDAC相关性中的用途 疾病。

公开(公告)号：US07465731B2

公开(公告)日：2008-12-16

申请号：US11199453

申请日：2005-08-09

申请人： Naoki Ishibashi ,  Yuki Sawada ,  Yasuharu Urano ,  Shigeki Satoh ,  Yoshikazu Inoue ,  Yoshiteru Eikyu ,  Koichiro Mukoyoshi ,  Kazunori Kamijo ,  Fumiyuki Shirai ,  Hisashi Takasugi

发明人： Naoki Ishibashi ,  Yuki Sawada ,  Yasuharu Urano ,  Shigeki Satoh ,  Yoshikazu Inoue ,  Yoshiteru Eikyu ,  Koichiro Mukoyoshi ,  Kazunori Kamijo ,  Fumiyuki Shirai ,  Hisashi Takasugi

IPC分类号： C07D401/12 ,  C07D403/12 ,  A61K31/497 ,  A61K31/506 ,  A61K31/501

CPC分类号： C07D213/74 ,  C07C259/06 ,  C07D207/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14

摘要： A compound having the formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower)alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is arylene, heterorarylene, cycloalkylene, heterocycloalkylene or aryl-fused cycloalkene, Y is arylene, heteroarylene, which may be substituted with one or more suitable substituent(s), Z lower alenylene, which may be substituted with lower alkyl or halogen, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.

摘要翻译： 具有式（I）的化合物：其中R1是氢，低级烷基，低级烯基，低级或高级炔基，环（低级）烷基，环（高级）烷基，环（低级）烷基（低级）烷基，环 ）（低级）烷基，低级（低级）烷基，芳基稠合环（低级）烷基，低级烷氧基，酰基，芳基，芳（低级）烷氧基， ，氨基，杂芳基，杂环基或杂环基（低级）烷基，其可以被一个或多个合适的取代基取代，R 2是氢或低级烷基，X是亚芳基，杂亚芳基，亚环烷基，亚杂环基或芳基稠合的环烯，Y 是亚芳基，可以被一个或多个合适的取代基取代的亚杂芳基，Z可以被低级烷基或卤素取代的低级亚烯基或其盐。 该化合物可用作组蛋白脱乙酰酶抑制剂。

公开(公告)号：US20060052599A1

公开(公告)日：2006-03-09

申请号：US11199453

申请日：2005-08-09

申请人： Naoki Ishibashi ,  Yuki Sawada ,  Yasuharu Urano ,  Shigeki Satoh ,  Yoshikazu Inoue ,  Yoshiteru Eikyu ,  Koichiro Mukoyoshi ,  Kazunori Kamijo ,  Fumiyuki Shirai ,  Hisashi Takasugi

发明人： Naoki Ishibashi ,  Yuki Sawada ,  Yasuharu Urano ,  Shigeki Satoh ,  Yoshikazu Inoue ,  Yoshiteru Eikyu ,  Koichiro Mukoyoshi ,  Kazunori Kamijo ,  Fumiyuki Shirai ,  Hisashi Takasugi

IPC分类号： C07D237/02 ,  C07C259/04

CPC分类号： C07D213/74 ,  C07C259/06 ,  C07D207/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14

摘要： A compound having the following formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower) alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is arylene, heteroarylene, cycloalkylene, heterocycloalkylene or aryl-fused cycloalkylene, Y is arylene or heteroarylene, which may be substituted with one or more suitable substituent(s), Z is lower alkenylene, which may be substituted with lower alkyl or halogen, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.

摘要翻译： 具有下式（I）的化合物：

公开(公告)号：US07557127B2

公开(公告)日：2009-07-07

申请号：US12264363

申请日：2008-11-04

申请人： Naoki Ishibashi ,  Yuki Sawada ,  Yasuharu Urano ,  Shigeki Satoh ,  Yoshikazu Inoue ,  Yoshiteru Eikyu ,  Koichiro Mukoyoshi ,  Kazunori Kamijo ,  Fumiyuki Shirai ,  Hisashi Takasugi

发明人： Naoki Ishibashi ,  Yuki Sawada ,  Yasuharu Urano ,  Shigeki Satoh ,  Yoshikazu Inoue ,  Yoshiteru Eikyu ,  Koichiro Mukoyoshi ,  Kazunori Kamijo ,  Fumiyuki Shirai ,  Hisashi Takasugi

IPC分类号： C07D401/12 ,  C07D403/12 ,  A61K31/497 ,  A61K31/506 ,  A61K31/501

CPC分类号： C07D213/74 ,  C07C259/06 ,  C07D207/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14

摘要： Compounds having the formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower)alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is pyrrolidinylene or piperidinylene, Y is pyridylene, which may be substituted with one or more suitable substituent(s), Z is lower alkenylene, which may be substituted with lower alkyl or halogen, and salts thereof are useful as a histone deacetylase inhibitors.

摘要翻译： 具有式（I）的化合物：其中R1是氢，低级烷基，低级烯基，低级或高级炔基，环（低级）烷基，环（高级）烷基，环（低级）烷基（低级）烷基， 烷基，低级烷基，低级烷基，低级烷基，低级烷基，低级烷基，低级烷基，低级烷基， 氨基，杂芳基，杂环基或杂环基（低级）烷基，其可以被一个或多个合适的取代基取代，R 2是氢或低级烷基，X是吡咯烷基或哌啶子基，Y是亚吡啶基，其可以被一个或多个 更合适的取代基，Z是低级亚烯基，其可以被低级烷基或卤素取代，其盐可用作组蛋白脱乙酰酶抑制剂。

公开(公告)号：US20100069388A1

公开(公告)日：2010-03-18

申请号：US12517290

申请日：2007-12-14

申请人： Yoshikazu Inoue ,  Yoshiteru Eikyu ,  Fumiyuki Shirai

发明人： Yoshikazu Inoue ,  Yoshiteru Eikyu ,  Fumiyuki Shirai

IPC分类号： A61K31/5377 ,  C07D211/72 ,  C07D241/02 ,  C07D413/12 ,  A61K31/44 ,  A61K31/4965 ,  A61P3/10

CPC分类号： C07D213/74 ,  C07D241/20 ,  C07D405/12

摘要： A compound having the following formula (I): wherein —R1 is hydrogen, optionally substituted lower alkyl, cyclo(lower)alkyl, cyclo(higher)alkyl, optionally substituted aryl, optionally substituted heterocyclyl, or aryl-fused cyclo(lower)alkyl, R2 is hydrogen or halogen, Z is CH or N, X is formula (II) R3 is lower alkyl which may be substituted with —OH or optionally substituted aryl, or lower alkanoyl, R4 is hydrogen or lower alkyl, Y is optionally substituted lower alkylene, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.

摘要翻译： 具有下式（I）的化合物：其中-R 1是氢，任选取代的低级烷基，环（低级）烷基，环（高级）烷基，任选取代的芳基，任选取代的杂环基或芳基稠合的环（低级）烷基 R 2为氢或卤素，Z为CH或N，X为式（II）R 3为可被-OH或任选取代的芳基或低级烷酰基取代的低级烷基，R 4为氢或低级烷基，Y为任选取代的 低级亚烷基或其盐。 该化合物可用作组蛋白脱乙酰酶抑制剂。

公开(公告)号：US07166598B2

公开(公告)日：2007-01-23

申请号：US10968473

申请日：2004-10-20

申请人： Kazuhiko Take ,  Nobukiyo Konishi ,  Shinji Shigenaga ,  Natsuko Kayakiri ,  Hidenori Azami ,  Yoshiteru Eikyu ,  Kazuo Nakai ,  Junya Ishida ,  Masataka Morita

发明人： Kazuhiko Take ,  Nobukiyo Konishi ,  Shinji Shigenaga ,  Natsuko Kayakiri ,  Hidenori Azami ,  Yoshiteru Eikyu ,  Kazuo Nakai ,  Junya Ishida ,  Masataka Morita

IPC分类号： A61K31/5355 ,  C07D413/06 ,  A61K31/496 ,  C07D401/06

CPC分类号： C07D401/06 ,  C07D241/04 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D491/08 ,  C07D495/04 ,  C07D498/04 ,  C07D498/08 ,  C07F7/1804

摘要： This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.

摘要翻译： 本发明涉及下式的哌嗪衍生物：其中每个符号如说明书中所定义，及其药学上可接受的盐，其制备方法，包含其的药物组合物及其用于治疗或预防的用途 速激肽介导的人类或动物疾病。

公开(公告)号：US6159961A

公开(公告)日：2000-12-12

申请号：US356684

申请日：1999-07-19

申请人： Kohji Kawabata ,  Hirofumi Yamamoto ,  Yoshiteru Eikyu ,  Shinya Okuda ,  Hisashi Takasugi

发明人： Kohji Kawabata ,  Hirofumi Yamamoto ,  Yoshiteru Eikyu ,  Shinya Okuda ,  Hisashi Takasugi

IPC分类号： C07D501/04 ,  A61K31/00 ,  A61K31/545 ,  A61K31/546 ,  A61P31/00 ,  A61P31/04 ,  C07D501/00 ,  C07D501/06 ,  C07D501/22 ,  C07D501/24 ,  C07D501/36 ,  C07D501/56 ,  C07D501/59 ,  A61L31/546

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： A compound of the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is hydrogen or hydroxy protective group,R.sup.3 is carboxy or protected carboxy,R.sup.4 is hydrogen, lower alkenyl, acyloxy(lower)alkenyl, optionally substituted heterocyclic(lower)alkenyl, optionally substituted heterocyclic(lower)alkenylthio, optionally substituted heterocyclic(lower)alkylthio, or optionally substituted heterocyclic-thio(lower)alkylthio andR5 is halogen or lower alkyland pharmaceutically acceptable salts thereof, which is useful as a medicament for prophylactic and therapeutic treatment of infectious diseases.

摘要翻译： 下式的化合物：其中R1是氨基或被保护的氨基，R2是氢或羟基保护基，R3是羧基或保护的羧基，R4是氢，低级烯基，酰氧基（低级）烯基，任选取代的杂环（低级）烯基， 任选取代的杂环（低级）烯硫基，任选取代的杂环（低级）烷硫基，或任选取代的杂环硫代（低级）烷硫基，R 5为卤素或低级烷基及其可药用盐，其可用作预防和治疗性治疗药物 的传染病。

公开(公告)号：US20070123532A1

公开(公告)日：2007-05-31

申请号：US11562149

申请日：2006-11-21

申请人： Kazuhiko Take ,  Nobukiyo Konishi ,  Shinji Shigenaga ,  Natsuko Kayakiri ,  Hidenori Azami ,  Yoshiteru Eikyu ,  Kazuo Nakai ,  Junya Ishida ,  Masataka Morita

发明人： Kazuhiko Take ,  Nobukiyo Konishi ,  Shinji Shigenaga ,  Natsuko Kayakiri ,  Hidenori Azami ,  Yoshiteru Eikyu ,  Kazuo Nakai ,  Junya Ishida ,  Masataka Morita

IPC分类号： A61K31/5377 ,  A61K31/496

CPC分类号： C07D401/06 ,  C07D241/04 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D491/08 ,  C07D495/04 ,  C07D498/04 ,  C07D498/08 ,  C07F7/1804

摘要： This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.

摘要翻译： 本发明涉及下式的哌嗪衍生物：其中每个符号如说明书中所定义，及其药学上可接受的盐，其制备方法，包含其的药物组合物及其用于治疗或预防的用途 速激肽介导的人类或动物疾病。

公开(公告)号：US20060014948A1

公开(公告)日：2006-01-19

申请号：US10968473

申请日：2004-10-20

申请人： Kazuhiko Take ,  Nobukiyo Konishi ,  Shinji Shigenaga ,  Natsuko Kayakiri ,  Hidenori Azami ,  Yoshiteru Eikyu ,  Kazuo Nakai ,  Junya Ishida ,  Masataka Morita

发明人： Kazuhiko Take ,  Nobukiyo Konishi ,  Shinji Shigenaga ,  Natsuko Kayakiri ,  Hidenori Azami ,  Yoshiteru Eikyu ,  Kazuo Nakai ,  Junya Ishida ,  Masataka Morita

IPC分类号： A61K31/5377 ,  C07D413/02 ,  C07D43/02

CPC分类号： C07D401/06 ,  C07D241/04 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D491/08 ,  C07D495/04 ,  C07D498/04 ,  C07D498/08 ,  C07F7/1804

摘要： This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.

摘要翻译： 本发明涉及下式的哌嗪衍生物：其中每个符号如说明书中所定义，及其药学上可接受的盐，其制备方法，包含其的药物组合物及其用于治疗或预防的用途 速激肽介导的人类或动物疾病。