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    • 1. 发明申请
      US20110166135A1 AROMATIC NITROGEN-CONTAINING 6-MEMBERED RING COMPOUNDS AND THEIR USE 审中-公开
    • AROMATIC NITROGEN-CONTAINING 6-MEMBERED RING COMPOUNDS AND THEIR USE
    • 含有硝酸的六元环化合物及其用途
    • US20110166135A1
    • 2011-07-07
    • US13062841
    • 2009-09-09
    • Hiroshi Morimoto , Toshiaki Sakamoto , Toshiyuki Himiyama , Eiji Kawanishi , Takehiko Matsumura
    • Hiroshi Morimoto , Toshiaki Sakamoto , Toshiyuki Himiyama , Eiji Kawanishi , Takehiko Matsumura
    • A61K31/5377 , C07D401/14 , C07D487/04 , C07D413/14 , A61K31/517 , A61K31/506 , A61K31/497 , A61K31/519 , A61P25/18 , A61P25/24 , A61P25/22 , A61P25/16 , A61P25/28
    • C07D401/14 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12
    • The present invention provides aromatic nitrogen-containing 6-membered ring compounds having excellent PDE10 inhibitory activity. The present invention relates to an aromatic nitrogen-containing 6-membered ring compound represented by the following formula [I0] or a pharmaceutically acceptable salt thereof, a method for preparing the same, and use of said compounds for PDE10 inhibitors, and a pharmaceutical composition comprising said compounds as an active ingredient: Formula [I0] wherein: X1, X2 and X3 each independently are N or CH, and at least two of X1, X2 and X3 are N; A is *—CH═CH—, *—C(Alk)=CH—, *—CH2—CH2— or *—O—CH2— (* is a bond with R1); Alk is a lower alkyl group; Ring B is an optionally substituted nitrogen-containing aliphatic heterocyclic group; R1 is an optionally substituted nitrogen-containing heterocyclic group, a nitrogen-containing heterocyclic moiety of which is a moiety selected from the group consisting of quinoxalinyl, quinolyl, isoquinolyl, quinazolinyl, pyrazinyl, pyrimidinyl and a moiety thereof fused with a 5 to 6-membered aliphatic ring thereto; Y0 is a group selected from the group consisting of the following (1) to (5): (1) an optionally substituted phenyl or an optionally substituted aromatic monocyclic 5 to 6-membered heterocyclic group; (2) an optionally substituted aminocarbonyl; (3) an optionally substituted amino lower alkyl; (4) —O—R2 wherein R2 is hydrogen, an optionally substituted lower alkyl, lower cycloalkyl, aliphatic monocyclic 5 to 6-membered heterocyclic group, or Formula [AA]; (5) mono- or di-substituted amino; provided that, when Y0 is mono- or di-substituted amino, the nitrogen-containing heterocyclic moiety of R1 is not quinoxalinyl or quinolyl.
    • 本发明提供具有优异的PDE10抑制活性的芳香族含氮6元环化合物。 本发明涉及由下式[I0]表示的含芳族含氮的6元环化合物或其药学上可接受的盐，其制备方法以及所述化合物用于PDE10抑制剂的用途和药物组合物 包括所述化合物作为活性成分：式[I0]其中：X1，X2和X3各自独立地为N或CH，X1，X2和X3中的至少两个为N; A是* -CH = CH-，* -C（Alk）= CH-，* -CH2-CH2-或* -O-CH2-（*是与R1的键）; Alk是低级烷基; 环B是任选取代的含氮脂族杂环基; R1是任选取代的含氮杂环基团，其含氮杂环部分是选自喹喔啉基，喹啉基，异喹啉基，喹唑啉基，吡嗪基，嘧啶基及其部分与5至6位稠合的部分， 元环脂族环; Y0是选自下列（1）至（5）的基团：（1）任选取代的苯基或任选取代的芳族单环5至6元杂环基; （2）任选取代的氨基羰基; （3）任选取代的氨基低级烷基; （4）-O-R2，其中R2是氢，任选取代的低级烷基，低级环烷基，脂族单环5至6元杂环基或式[AA]; （5）单取代或二取代氨基; 条件是当Y 0是单取代或二取代的氨基时，R 1的含氮杂环部分不是喹喔啉基或喹啉基。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 5. 发明授权
      US5367787A Drying machine 失效
    • Drying machine
    • 烘干机
    • US5367787A
    • 1994-11-29
    • US102307
    • 1993-08-05
    • Tomohiko Ikeda , Toshiaki Sakamoto
    • Tomohiko Ikeda , Toshiaki Sakamoto
    • D06F43/08 , F26B11/18 , F26B21/10 , F26B25/00 , F26B19/00
    • F26B21/10 , D06F43/086 , F26B11/181 , F26B25/006 , F26B25/009
    • A drying machine has a drying chamber for drying an article cleaned with an inflammable solvent as a detergent. A hot air supply channel communicates with the drying chamber and a heater is mounted in the hot air supply channel. A hot air evacuation channel communicates with the drying chamber and a hot air transfer device is mounted at a voluntary portion of the hot air supply channel and the hot air evacuation channel. A control device is provided for driving control of the heater. A first temperature sensor is mounted on the downstream side of the heater in the hot air supply channel and a second temperature sensor is mounted at a position shifted to the drying chamber in the hot air evacuation channel. The control device controls the heater so that the difference in the temperature detected by the first temperature sensor and the temperature detected by the second temperature sensor is kept within a safe temperature range.
    • 干燥机具有干燥室，用于干燥用易燃溶剂清洗的物品作为洗涤剂。 热风供应通道与干燥室连通，并且加热器安装在热空气供应通道中。 热空气排出通道与干燥室连通，热空气传送装置安装在热空气供应通道和热空气排出通道的自愿部分。 提供控制装置用于驱动加热器的控制。 第一温度传感器安装在热空气供应通道中的加热器的下游侧，并且第二温度传感器安装在位于热空气排出通道中的干燥室的位置。 控制装置控制加热器，使得由第一温度传感器检测到的温度差和由第二温度传感器检测到的温度保持在安全的温度范围内。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 6. 发明授权
      US07521430B2 N-glucoside compounds having an inhibitory activity against sodium-dependent glucose transporter 失效
    • N-glucoside compounds having an inhibitory activity against sodium-dependent glucose transporter
    • 对钠依赖性葡萄糖转运蛋白具有抑制活性的N-葡萄糖苷化合物
    • US07521430B2
    • 2009-04-21
    • US10566585
    • 2004-07-30
    • Sumihiro Nomura , Toshiaki Sakamoto , Kiichiro Ueta
    • Sumihiro Nomura , Toshiaki Sakamoto , Kiichiro Ueta
    • A01N43/04 , A61K31/70 , C07H5/06 , C07H19/00
    • C07H15/203 , C07H5/04 , C07H17/02
    • A compound of the formula: wherein Ring A and Ring B are (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, wherein —NR— group and —CH2— group are both on the same ring of the unsaturated fused heterobicyclic ring, and Ring B is an optionally substituted monocyclic unsaturated heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; and R is a hydrogen atom, a lower alkyl group, a lower alkanoyl group or a lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof, or a prodrug thereof.
    • 下式的化合物：其中环A和环B是（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选地 取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环，或（3）环A是 任选取代的不饱和稠合杂双环，其中-NR-基和-CH2-基都在不饱和稠合杂双环的相同环上，环B是任选取代的单环不饱和杂环，任选取代的不饱和稠合杂双环 ，或任选取代的苯环; 或其前体药物，R为氢原子，低级烷基，低级烷酰基或低级烷氧基羰基，或其药学上可接受的盐。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 9. 发明申请
      US20070060545A1 Novel compounds 失效
    • Novel compounds
    • 新型化合物
    • US20070060545A1
    • 2007-03-15
    • US10566585
    • 2004-07-30
    • Sumihiro Nomura , Toshiaki Sakamoto , Kiichiro Ueta
    • Sumihiro Nomura , Toshiaki Sakamoto , Kiichiro Ueta
    • A61K31/7008 , C07H5/04
    • C07H15/203 , C07H5/04 , C07H17/02
    • A compound of the formula: wherein Ring A and Ring B are (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, wherein —NR— group and —CH2— group are both on the same ring of the unsaturated fused heterobicyclic ring, and Ring B is an optionally substituted monocyclic unsaturated heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; and R is a hydrogen atom, a lower alkyl group, a lower alkanoyl group or a lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof, or a prodrug thereof.
    • 下式的化合物：其中环A和环B是（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的不饱和单环杂环 取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环，或（3）环A是 任选取代的不饱和稠合杂双环，其中-NR-基团和-CH 2 - 基团都在不饱和稠合杂双环环的相同环上，环B是任选取代的单环不饱和杂环 ，任选取代的不饱和稠合杂双环，或任选取代的苯环; 或其前体药物，R为氢原子，低级烷基，低级烷酰基或低级烷氧基羰基，或其药学上可接受的盐。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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