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公开(公告)号:US08044070B2
公开(公告)日:2011-10-25
申请号:US12540534
申请日:2009-08-13
申请人: Norikazu Ohtake , Akira Naya , Yuji Haga , Makoto Jitsuoka , Takuya Suga , Ryo Yoshimoto , Shigeru Tokita , Akio Kanatani
发明人: Norikazu Ohtake , Akira Naya , Yuji Haga , Makoto Jitsuoka , Takuya Suga , Ryo Yoshimoto , Shigeru Tokita , Akio Kanatani
IPC分类号: A61K31/445 , C07D211/00
CPC分类号: C07D401/12 , A61K31/4545 , A61K31/501 , A61K31/506 , C07D401/14 , C07D403/12 , C07D413/14 , C07D471/04
摘要: Provided are compounds of a formula (I) and their pharmaceutically-acceptable salts: wherein X1, X2 and X3 each independently represent N or CH; W represents the following formula (II): or the following formula (III): Y represents a group of a formula (IV): The compounds have a histamine-H3 receptor antagonistic or inverse-agonistic activity and are useful for remedy and/or prevention of obesity, diabetes, hormone secretion disorders, sleep disorders, etc.
摘要翻译: 提供式(I)化合物及其药学上可接受的盐:其中X1,X2和X3各自独立地表示N或CH; W表示下式(II):或下式(III):Y表示式(IV)的基团:所述化合物具有组胺H3受体拮抗或反向激动活性,可用于治疗和/或 预防肥胖,糖尿病,激素分泌障碍,睡眠障碍等
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公开(公告)号:US07732456B2
公开(公告)日:2010-06-08
申请号:US10591373
申请日:2005-03-04
申请人: Norikazu Otake , Yuji Haga , Akira Naya , Sayaka Mizutani , Akio Kanatani
发明人: Norikazu Otake , Yuji Haga , Akira Naya , Sayaka Mizutani , Akio Kanatani
IPC分类号: A61K31/444 , C07D401/02
CPC分类号: C07D213/69 , C07D237/16 , C07D239/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D451/02 , C07D471/04
摘要: The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R1 and R2 may be same or different and stands for H, etc., or R1 and R2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X1-X3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X4-X7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y1 and Y3 may be same or different and stand for single bond, —O—, —NR—, —S—, etc; Y2 stands for lower lkylene, etc.; R stands for H, etc., L stands for methylene; Z1 and Z2 may be same or different and stand for single bond or lower alkylene; or R1, L and Z2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R1 binds; and Ar stands for aromatic carbocyclic group, etc.].
摘要翻译: 本发明提供由通式(I)表示的吡啶酮衍生物[在该式中,R 1和R 2可以相同或不同,代表H等,或者R 1和R 2可以与脂族含氮杂环基一起形成 他们绑定的N X1-X3可以相同或不同,代替次甲基或N,但不是全部同时代表氮; X4-X7可以相同或不同,代表次甲基或N,条件是它们中的三个或更多不同时代表N; Y1和Y3可以相同或不同,代表单键,-O-,-NR-,-S-等; Y2代表低级亚烷基等; R代表H等,L代表亚甲基; Z 1和Z 2可以相同或不同,代表单键或低级亚烷基; 或R1,L和Z2可以与R1结合的N形成脂族含氮杂环基; 和Ar代表芳族碳环基团等]。
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公开(公告)号:US20070208046A1
公开(公告)日:2007-09-06
申请号:US10591373
申请日:2005-03-04
申请人: Norikazu Otake , Yuji Haga , Akira Naya , Sayaka Mizutani , Akio Kanatani
发明人: Norikazu Otake , Yuji Haga , Akira Naya , Sayaka Mizutani , Akio Kanatani
IPC分类号: A61K31/513 , A61K31/444 , A61K31/4412 , C07D403/02 , C07D401/02
CPC分类号: C07D213/69 , C07D237/16 , C07D239/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D451/02 , C07D471/04
摘要: The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R1 and R2 may be same or different and stands for H, etc., or R1 and R2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X1-X3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X4-X7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y1 and Y3 may be same or different and stand for single bond, —O—, —NR—, —S—, etc; Y2 stands for lower alkylene, etc.; R stands for H, etc., L stands for methylene; Z1 and Z2 may be same or different and stand for single bond or lower alkylene; or R1, L and Z2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R1 binds; and Ar stands for aromatic carbocyclic group, etc.].
摘要翻译: 本发明提供由通式(I)表示的吡啶酮衍生物[在式中,R 1和R 2可以相同或不同,代表H等, 或R 1和R 2可以与它们所键合的N一起形成脂族含氮杂环基; X 1 -X 3可以相同或不同,代表次甲基或N,但并不全部同时代表氮; X 4 -X 7可以相同或不同,代表次甲基或N,条件是它们中的三个或更多个不同时代表N; Y 1和Y 3可以相同或不同,代表单键,-O-,-NR-,-S-等; Y 2代表低级亚烷基等; R代表H等,L代表亚甲基; Z 1和Z 2可以相同或不同,代表单键或低级亚烷基; 或R 1,L和Z 2可以与R 1结合的N形成脂族含氮杂环基; 和Ar代表芳族碳环基团等]。
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公开(公告)号:US20060178375A1
公开(公告)日:2006-08-10
申请号:US10561115
申请日:2004-06-24
申请人: Norikazu Ohtake , Akira Naya , Yuji Haga , Makoto Jitsuoka , Takuya Suga , Ryo Yoshimoto , Shigeru Tokita , Akio Kanatani
发明人: Norikazu Ohtake , Akira Naya , Yuji Haga , Makoto Jitsuoka , Takuya Suga , Ryo Yoshimoto , Shigeru Tokita , Akio Kanatani
IPC分类号: A61K31/506 , C07D413/14 , C07D403/14
CPC分类号: C07D401/12 , A61K31/4545 , A61K31/501 , A61K31/506 , C07D401/14 , C07D403/12 , C07D413/14 , C07D471/04
摘要: Compound of the formula: (I) [wherein each of X1, X2, and X3 independently represents N or CH, W represents the formula (II):(II) or the formula (III):(III) and Y represents a group of the formula (IV):(IV)], or a pharmacologically acceptable salt thereof. This compound exhibits histamine receptor H3 antagonist or inverse agonist activity and is useful of the treatment and/or prevention of obesity, diabetes, hormonal secretion abnormality, sleep, disorder, etc.
摘要翻译: 式(I)的化合物[其中X 1,X 2和X 3各自独立地表示N或CH,W表示 式(II):(II)或式(III):III),Y表示式(IV):(IV)]的基团,或其药理学上可接受的盐。 该化合物显示组胺受体H3拮抗剂或反向激动剂活性,并且可用于治疗和/或预防肥胖症,糖尿病,激素分泌异常,睡眠,障碍等。
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