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1. 发明授权

US07732456B2 Pyridone derivative 失效
标题翻译：吡啶酮衍生物
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]。

2. 发明申请

US20070208046A1 Pyridone derivative 失效
标题翻译：吡啶酮衍生物
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]。

3. 发明申请

US20060111380A1 Novel azole derivatives 失效
标题翻译：新型唑衍生物
公开(公告)号：US20060111380A1
公开(公告)日：2006-05-25
申请号：US10536360
申请日：2003-11-25
申请人： Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
发明人： Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
IPC分类号： A61K31/4747 , C07D471/10
CPC分类号： C07D491/10
摘要： The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
摘要翻译：本发明涉及式（I）化合物：其中Az是包含相同或不同稠合唑的单环唑或双环芳环的基团; T，U，V和W独立为次甲基或氮，所述次甲基任选被取代基取代，T，U，V和W中的至少两个为所述次甲基; X是氮或次甲基。本发明的化合物可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，神经系统疾病，基因疾病，代谢疾病，生殖器或生殖障碍，胃肠道疾病，呼吸系统疾病，炎症性疾病疾病或青光眼等。

4. 发明授权

US07589096B2 Azole derivatives 失效
标题翻译：唑衍生物
公开(公告)号：US07589096B2
公开(公告)日：2009-09-15
申请号：US12071808
申请日：2008-02-26
申请人： Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
发明人： Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
IPC分类号： A61K31/438 , A61K31/506 , A61K31/4545 , C07D233/96 , C07D401/14 , C07D401/02
CPC分类号： C07D491/10
摘要： The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, wherein a methine may be optionally substituted by a substituent, and at least two of T, U, V and W are methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastro-intestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
摘要翻译：本发明涉及式（I）化合物：其中Az是包含相同或不同稠合唑的单环唑或双环芳环的基团; T，U，V和W独立地是次甲基或氮，其中次甲基可以任选地被取代基取代，并且T，U，V和W中的至少两个是次甲基; X是氮或次甲基。本发明的化合物可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，神经系统疾病，基因疾病，代谢疾病，生殖器或生殖障碍，胃肠道疾病，呼吸障碍，炎症性疾病或青光眼等。

5. 发明申请

US20080188507A1 Novel azole derivatives 失效
标题翻译：新型唑衍生物
公开(公告)号：US20080188507A1
公开(公告)日：2008-08-07
申请号：US12071808
申请日：2008-02-26
申请人： Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
发明人： Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
IPC分类号： A61K31/4747 , C07D491/14
CPC分类号： C07D491/10
摘要： The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine.The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastro-intestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
摘要翻译：本发明涉及式（I）化合物：其中Az是包含相同或不同稠合唑的单环唑或双环芳环的基团; T，U，V和W独立为次甲基或氮，所述次甲基任选被取代基取代，T，U，V和W中的至少两个为所述次甲基; X是氮或次甲基。本发明的化合物可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，神经系统疾病，基因疾病，代谢疾病，生殖器或生殖障碍，胃肠道疾病，呼吸障碍，炎症性疾病或青光眼等。

6. 发明授权

US07365079B2 Azole derivatives 失效
标题翻译：唑衍生物
公开(公告)号：US07365079B2
公开(公告)日：2008-04-29
申请号：US10536360
申请日：2003-11-25
申请人： Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
发明人： Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
IPC分类号： A61K31/4355 , C07D471/04
CPC分类号： C07D491/10
摘要： The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
摘要翻译：本发明涉及式（I）化合物：其中Az是包含相同或不同稠合唑的单环唑或双环芳环的基团; T，U，V和W独立为次甲基或氮，所述次甲基任选被取代基取代，T，U，V和W中的至少两个为所述次甲基; X是氮或次甲基。本发明的化合物可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，神经系统疾病，基因疾病，代谢疾病，生殖器或生殖障碍，胃肠道疾病，呼吸系统疾病，炎症性疾病疾病或青光眼等。

7. 发明授权

US07875633B2 Phenylpyridone derivative 失效
标题翻译：苯基吡啶酮衍生物
公开(公告)号：US07875633B2
公开(公告)日：2011-01-25
申请号：US11990889
申请日：2006-08-23
申请人： Akira Naya , Toshihiro Sakamoto , Yuji Haga , Norikazu Otake
发明人： Akira Naya , Toshihiro Sakamoto , Yuji Haga , Norikazu Otake
IPC分类号： A61K31/444 , A61K31/4439 , A61K31/5377 , A61K31/4545 , A61P9/00 , A61P25/00 , A61P3/00 , C07D213/64 , C07D401/02 , C07D413/02 , C07D401/14
CPC分类号： C07D213/69 , C07D213/64 , C07D401/10 , C07D413/10
摘要： A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents —CH2—O—, —CH═CH— or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.
摘要翻译：作为活性成分，含有式（I）所示的化合物：其中，R 1和R 2分别独立地表示氢原子，低级烷基等，或者与连接有L，Z 2和R 1的氮原子一起形成可以形成脂族氮杂环基，并且R 1和R 2与它们所连接的氮原子一起形成脂族氮杂环基; X表示次甲基或氮原子; Y表示-CH 2 -O-，-CH = CH-等; Z1表示单键，C1-4亚烷基等; Z2表示单键或C1-4亚烷基; L表示亚甲基，C3-8亚环烷基等; Ar表示芳族碳环基等。该化合物可用作中枢神经系统疾病，心血管疾病或代谢疾病的药物。

8. 发明申请

US20090137587A1 Phenylpyridone Derivative 失效
标题翻译：苯基吡啶酮衍生物
公开(公告)号：US20090137587A1
公开(公告)日：2009-05-28
申请号：US11990889
申请日：2006-08-23
申请人： Akira Naya , Toshihiro Sakamoto , Yuji Haga , Norikazu Otake
发明人： Akira Naya , Toshihiro Sakamoto , Yuji Haga , Norikazu Otake
IPC分类号： A61K31/444 , C07D213/64 , C07D401/02 , C07D413/02 , A61K31/4439 , A61P9/00 , A61P25/00 , A61P3/00 , C07D401/14 , A61K31/5377 , A61K31/4545
CPC分类号： C07D213/69 , C07D213/64 , C07D401/10 , C07D413/10
摘要： A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents —CH2—O—, —CH═CH— or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.
摘要翻译：作为活性成分，含有式（I）所示的化合物：其中，R 1和R 2分别独立地表示氢原子，低级烷基等，或者与连接有L，Z 2和R 1的氮原子一起形成可以形成脂族氮杂环基，并且R 1和R 2与它们所连接的氮原子一起形成脂族氮杂环基; X表示次甲基或氮原子; Y表示-CH 2 -O - ， - CH-CH-等; Z1表示单键，C1-4亚烷基等; Z2表示单键或C1-4亚烷基; L表示亚甲基，C3-8亚环烷基等; Ar表示芳族碳环基等。该化合物可用作中枢神经系统疾病，心血管疾病或代谢疾病的药物。

9. 发明授权

US08044070B2 Heteroaryloxy nitrogenous saturated heterocyclic derivative 有权
标题翻译：杂环氧基含氮饱和杂环衍生物
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

10. 发明申请

US20060178375A1 Heteroaryloxy nitrogenous saturated heterocyclic derivative 有权
标题翻译：杂环氧基含氮饱和杂环衍生物
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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