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：US08314240B2

公开(公告)日：2012-11-20

申请号：US13000677

申请日：2009-06-22

申请人： Hideki Kubota ,  Issei Tsukamoto ,  Kazunori Kamijo ,  Koji Kato ,  Yuta Fukuda ,  Hidenori Azami

发明人： Hideki Kubota ,  Issei Tsukamoto ,  Kazunori Kamijo ,  Koji Kato ,  Yuta Fukuda ,  Hidenori Azami

IPC分类号： A61K31/44 ,  C07D213/62

CPC分类号： C07C311/21 ,  A61K31/341 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  C07C2602/08 ,  C07D213/71 ,  C07D213/80 ,  C07D277/20 ,  C07D277/36 ,  C07D277/56 ,  C07D307/64 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12

摘要： [Object] A compound which is useful as an EP1 receptor antagonist is provided.[Means for Solution] The present inventors investigated EP1 receptor antagonists, and confirmed that a compound having a sulfonamide structure, in which the nitrogen atom of the sulfonamide structure is substituted with 2-fluoropropyl group, 3-fluoro-2-methylpropyl group or the like, has a potent EP1 receptor antagonistic action, thereby completing the present invention. The sulfonamide compound of the present invention has a potent EP1 receptor antagonistic action and can be used as an agent for preventing and/or treating a lower urinary tract symptom or the like.

摘要翻译： 提供了可用作EP1受体拮抗剂的化合物。 [解决方案]本发明人研究了EP1受体拮抗剂，并证实了具有磺酰胺结构的化合物，其中磺酰胺结构的氮原子被2-氟丙基取代，3-氟-2-甲基丙基或 具有有效的EP1受体拮抗作用，从而完成本发明。 本发明的磺酰胺化合物具有有效的EP1受体拮抗作用，可用作预防和/或治疗下尿路症状等的药剂。

公开(公告)号：US20110319385A1

公开(公告)日：2011-12-29

申请号：US13254368

申请日：2010-03-04

申请人： Hiroyuki Kaizawa ,  Mari Sugita ,  Hidenori Azami ,  Ryushi Seo ,  Takaho Nomura ,  Satoshi Yamamoto ,  Hirofumi Yamamoto ,  Kazuyuki Tsuchiya ,  Hideki Kubota ,  Kazunori Kamijo

发明人： Hiroyuki Kaizawa ,  Mari Sugita ,  Hidenori Azami ,  Ryushi Seo ,  Takaho Nomura ,  Satoshi Yamamoto ,  Hirofumi Yamamoto ,  Kazuyuki Tsuchiya ,  Hideki Kubota ,  Kazunori Kamijo

IPC分类号： A61K31/4985 ,  C07D413/14 ,  A61P13/00 ,  A61K31/5377 ,  A61K31/55 ,  C07D487/04 ,  C07D403/14

CPC分类号： C07D498/04 ,  C07D487/04 ,  C07D491/107 ,  C07D519/00

摘要： [Problem]Provided is a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.[Means for Solution]The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like, and thus, have found that an imidazoquinoxaline compound or a triazoloquinoxaline compound has a PDE9-inhibiting action, thereby completing the present invention. The imidazoquinoxaline compound or the triazoloquinoxaline compound of the present invention has a PDE9-inhibiting action and can be used as an agent for preventing and/or treating storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.

摘要翻译： [问题]提供具有PDE9抑制作用并可用作治疗和/或预防储存功能障碍，排尿功能障碍和膀胱/尿道疾病的药剂的活性成分的化合物等。 [解决方案]本发明人已经研究了具有PDE9抑制作用并可用作治疗和/或预防储存功能障碍，排尿功能障碍和膀胱/尿道疾病等的活性成分的化合物 ，因此已经发现咪唑并喹喔啉化合物或三唑并喹喔啉化合物具有抑制PDE9的作用，从而完成了本发明。 本发明的咪唑并喹喔啉化合物或三唑并喹喔啉化合物具有PDE9抑制作用，可用作预防和/或治疗储存功能障碍，排尿功能障碍和膀胱/尿道疾病等的药剂。

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：US07135493B2

公开(公告)日：2006-11-14

申请号：US10754541

申请日：2004-01-12

申请人： Yasuharu Urano ,  Shigeki Satoh ,  Naoki Ishibashi ,  Kazunori Kamijo

发明人： Yasuharu Urano ,  Shigeki Satoh ,  Naoki Ishibashi ,  Kazunori Kamijo

IPC分类号： A61K31/4188 ,  A61K31/484 ,  A61K31/4164 ,  C07D233/61 ,  C07D491/113 ,  C07D487/04 ,  C07D235/08

CPC分类号： C07D213/75 ,  C07C57/58 ,  C07C61/40 ,  C07C211/50 ,  C07C211/52 ,  C07C233/22 ,  C07C233/31 ,  C07C233/43 ,  C07C233/44 ,  C07C233/51 ,  C07C271/28 ,  C07D233/56 ,  C07D233/64 ,  C07D233/68 ,  C07D233/70 ,  C07D233/90 ,  C07D235/12 ,  C07D235/16 ,  C07D239/47 ,  C07D317/66 ,  C07D401/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D471/04 ,  C07D473/08 ,  C07D491/04

摘要： A compound having the following formula (I): wherein R1 is N-containing heterocyclic ring optionally substituted with one or more suitable substituent(s), R2 is hydroxyamino, R3 is hydrogen or a suitable substituent, L1 is —(CH2)n— (wherein n is an integer of 0 to 6) optionally substituted with one or more suitable substituent(s), wherein one or more methylene(s) may be replaced with suitable heteroatom(s), and L2 is lower alkenylene, 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是任选被一个或多个合适的取代基取代的含N的杂环，R 2是羟基氨基， R 3是氢或合适的取代基，L 1是 - （CH 2 CH 2）n - （其中n 是0至6的整数），其任选地被一个或多个合适的取代基取代，其中一个或多个亚甲基可被适当的杂原子替代，并且L 2低 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：US20090054464A1

公开(公告)日：2009-02-26

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： A61K31/4439 ,  C07D401/02 ,  C07D401/14 ,  C07D417/02 ,  C07D405/14 ,  C07D409/14 ,  A61P33/02 ,  A61P35/02 ,  A61K31/497 ,  A61K31/506 ,  A61K31/4545 ,  A61K31/454

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：US08357688B2

公开(公告)日：2013-01-22

申请号：US13254368

申请日：2010-03-04

申请人： Hiroyuki Kaizawa ,  Mari Sugita ,  Hidenori Azami ,  Ryushi Seo ,  Takaho Nomura ,  Satoshi Yamamoto ,  Hirofumi Yamamoto ,  Kazuyuki Tsuchiya ,  Hideki Kubota ,  Kazunori Kamijo

发明人： Hiroyuki Kaizawa ,  Mari Sugita ,  Hidenori Azami ,  Ryushi Seo ,  Takaho Nomura ,  Satoshi Yamamoto ,  Hirofumi Yamamoto ,  Kazuyuki Tsuchiya ,  Hideki Kubota ,  Kazunori Kamijo

IPC分类号： A61K31/495

CPC分类号： C07D498/04 ,  C07D487/04 ,  C07D491/107 ,  C07D519/00

摘要： Substituted imidazo[1,5-a]quinoxalin-4(5H)-ones are useful as PDE9 inhibitors.

摘要翻译： 取代的咪唑并[1,5-a]喹喔啉-4（5H） - 酮可用作PDE9抑制剂。

公开(公告)号：US20110201616A1

公开(公告)日：2011-08-18

申请号：US13000677

申请日：2009-06-22

申请人： Hideki Kubota ,  Issei Tsukamoto ,  Kazunori Kamijo ,  Koji Kato ,  Yuta Fukuda ,  Hidenori Azami

发明人： Hideki Kubota ,  Issei Tsukamoto ,  Kazunori Kamijo ,  Koji Kato ,  Yuta Fukuda ,  Hidenori Azami

IPC分类号： A61K31/501 ,  C07D213/71 ,  A61K31/4402 ,  C07D277/36 ,  A61K31/426 ,  C07D403/12 ,  A61K31/506 ,  C07D417/12 ,  A61K31/427 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/444 ,  C07D307/64 ,  A61K31/341 ,  A61K31/497 ,  A61P13/00

CPC分类号： C07C311/21 ,  A61K31/341 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  C07C2602/08 ,  C07D213/71 ,  C07D213/80 ,  C07D277/20 ,  C07D277/36 ,  C07D277/56 ,  C07D307/64 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12

摘要： [Object] A compound which is useful as an EP1 receptor antagonist is provided.[Means for Solution] The present inventors investigated EP1 receptor antagonists, and confirmed that a compound having a sulfonamide structure, in which the nitrogen atom of the sulfonamide structure is substituted with 2-fluoropropyl group, 3-fluoro-2-methylpropyl group or the like, has a potent EP1 receptor antagonistic action, thereby completing the present invention. The sulfonamide compound of the present invention has a potent EP1 receptor antagonistic action and can be used as an agent for preventing and/or treating a lower urinary tract symptom or the like.

摘要翻译： 提供了可用作EP1受体拮抗剂的化合物。 [解决方案]本发明人研究了EP1受体拮抗剂，并证实了具有磺酰胺结构的化合物，其中磺酰胺结构的氮原子被2-氟丙基取代，3-氟-2-甲基丙基或 具有有效的EP1受体拮抗作用，从而完成本发明。 本发明的磺酰胺化合物具有有效的EP1受体拮抗作用，可用作预防和/或治疗下尿路症状等的药剂。

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。