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1. 发明申请

US20070265289A1 2-Aminopyrimidine Derivative 审中-公开
标题翻译： 2-氨基嘧啶衍生物
公开(公告)号：US20070265289A1
公开(公告)日：2007-11-15
申请号：US11578608
申请日：2005-04-13
申请人： Yoshinori Okamoto , Hirokazu Kubota , Ippei Sato , Kazuyuki Hattori , Takatoshi Kanayama , Kazuhiro Yokoyama , Yoshiya Terai , Masahiro Takeuchi
发明人： Yoshinori Okamoto , Hirokazu Kubota , Ippei Sato , Kazuyuki Hattori , Takatoshi Kanayama , Kazuhiro Yokoyama , Yoshiya Terai , Masahiro Takeuchi
IPC分类号： A61K31/506 , C07D403/02
CPC分类号： C07D401/04 , A61K31/506 , A61K31/55 , C07D401/12 , C07D403/04 , C07D413/04
摘要： The invention relates to a compound useful as remedies or preventives for IKK2-related inflammatory diseases or autoimmune diseases, or that is, a 2-aminopyrimidine derivative having a 2-hydroxyphenyl group at the 6-position thereof and having a saturated cyclic group that contains one nitrogen atom, such as piperidine, at the 4-position thereof. The pharmaceutical composition of the invention and the compound of the invention have an excellent antiinflammatory effect based on the IKK2-inhibitory effect thereof, and are therefore useful for remedies and preventives for inflammatory diseases and autoimmune diseases, especially for rheumatoid arthritis.
摘要翻译：本发明涉及可用作IKK2相关炎性疾病或自身免疫性疾病的补救措施或预防药物的化合物，或其6-位上具有2-羟基苯基并具有饱和环状基团的2-氨基嘧啶衍生物，其含有一个氮原子，例如哌啶，在其4-位。本发明的药物组合物和本发明化合物基于IKK2抑制作用具有优异的抗炎作用，因此可用于炎性疾病和自身免疫疾病，特别是类风湿性关节炎的治疗和预防药物。

2. 发明申请

US20050096322A1 Nitrogen-containing heterocyclic compound 审中-公开
标题翻译：含氮杂环化合物
公开(公告)号：US20050096322A1
公开(公告)日：2005-05-05
申请号：US10505939
申请日：2003-02-27
申请人： Susumu Igarashi , Ryo Naito , Yoshinori Okamoto , Noriyuki Kawano , Issei Tsukamoto , Ippei Sato , Makoto Takeuchi , Hiroyuki Kanoh , Masato Kobori
发明人： Susumu Igarashi , Ryo Naito , Yoshinori Okamoto , Noriyuki Kawano , Issei Tsukamoto , Ippei Sato , Makoto Takeuchi , Hiroyuki Kanoh , Masato Kobori
IPC分类号： A61P19/00 , A61P19/08 , A61P19/10 , A61P43/00 , C07D487/04 , A61K31/503
CPC分类号： C07D487/04
摘要： As a result of an effort made by us for the purpose of developing a therapeutic agent having a bone formation-stimulating effect by promoting the functions of osteoblasts, the present inventors discovered that a certain nitrogen-containing heterocyclic compound exhibits a potent bone formation-stimulating effect on the osteoblast and thus can serve as an excellent prophylactic or therapeutic agent against a metabolic bone disease, whereby establishing the present invention. Thus, the present invention provides a 3,6-disubstituted 1,2,4-triazolo[4,3-b]pyridazine compound or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition comprising such a compound and a pharmaceutically acceptable carrier, especially a bone-forming agent.
摘要翻译：本发明人为了通过促进成骨细胞的功能开发具有促进骨形成刺激作用的治疗剂而作出努力的结果，发现某些含氮杂环化合物表现出强有力的骨形成刺激对成骨细胞的作用，因此可以作为抗代谢性骨病的优异的预防或治疗剂，由此建立本发明。因此，本发明提供了3,6-二取代的1,2,4-三唑并[4,3-b]哒嗪化合物或其药学上可接受的盐，以及包含这种化合物和药学上可接受的载体的药物组合物，特别是骨形成剂。

3. 发明授权

US07173033B2 Nitrogen-containing heterocyclic compound 失效
标题翻译：含氮杂环化合物
公开(公告)号：US07173033B2
公开(公告)日：2007-02-06
申请号：US11190859
申请日：2005-07-28
申请人： Susumu Igarashi , Ryo Naito , Yoshinori Okamoto , Noriyuki Kawano , Issei Tsukamoto , Ippei Sato , Makoto Takeuchi , Hiroyuki Kanoh , Masato Kobori
发明人： Susumu Igarashi , Ryo Naito , Yoshinori Okamoto , Noriyuki Kawano , Issei Tsukamoto , Ippei Sato , Makoto Takeuchi , Hiroyuki Kanoh , Masato Kobori
IPC分类号： C07D487/04 , A61K31/5025 , A61P19/08
CPC分类号： C07D487/04
摘要： As a result of an effort made by us for the purpose of developing a therapeutic agent having a bone formation-stimulating effect by promoting the functions of osteoblasts, the present inventors discovered that a certain nitrogen-containing heterocyclic compound exhibits a potent bone formation-stimulating effect on the osteoblast and thus can serve as an excellent prophylactic or therapeutic agent against a metabolic bone disease, whereby establishing the present invention.Thus, the present invention provides a 3,6-disubstituted 1,2,4-triazolo[4,3-b]pyridazine compound or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition comprising such a compound and a pharmaceutically acceptable carrier, especially a bone-forming agent.
摘要翻译：本发明人为了通过促进成骨细胞的功能开发具有促进骨形成刺激作用的治疗剂而作出努力的结果，发现某些含氮杂环化合物表现出强有力的骨形成刺激对成骨细胞的作用，因此可以作为抗代谢性骨病的优异的预防或治疗剂，由此建立本发明。因此，本发明提供了3,6-二取代的1,2,4-三唑并[4,3-b]哒嗪化合物或其药学上可接受的盐，以及包含这种化合物和药学上可接受的载体的药物组合物，特别是骨形成剂。

4. 发明申请

US20050261297A1 Nitrogen-containing heterocyclic compound 失效
公开(公告)号：US20050261297A1
公开(公告)日：2005-11-24
申请号：US11190859
申请日：2005-07-28
申请人： Susumu Igarashi , Ryo Naito , Yoshinori Okamoto , Noriyuki Kawano , Issei Tsukamoto , Ippei Sato , Makoto Takeuchi , Hiroyuki Kanoh , Masato Kobori
发明人： Susumu Igarashi , Ryo Naito , Yoshinori Okamoto , Noriyuki Kawano , Issei Tsukamoto , Ippei Sato , Makoto Takeuchi , Hiroyuki Kanoh , Masato Kobori
IPC分类号： A61P19/00 , A61P19/08 , A61P19/10 , A61P43/00 , C07D487/04 , A61K31/503 , A61K31/55
CPC分类号： C07D487/04
摘要： As a result of an effort made by us for the purpose of developing a therapeutic agent having a bone formation-stimulating effect by promoting the functions of osteoblasts, the present inventors discovered that a certain nitrogen-containing heterocyclic compound exhibits a potent bone formation-stimulating effect on the osteoblast and thus can serve as an excellent prophylactic or therapeutic agent against a metabolic bone disease, whereby establishing the present invention. Thus, the present invention provides a 3,6-disubstituted 1,2,4-triazolo[4,3-b]pyridazine compound or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition comprising such a compound and a pharmaceutically acceptable carrier, especially a bone-forming agent.

5. 发明授权

US06348480B1 Pharmaceutical compound comprising a pyrazole derivative and methods of using the same for the treatment of calcium release-activated calcium channel associated diseases 失效
标题翻译：包含吡唑衍生物的药物化合物及其用于治疗钙释放激活的钙通道相关疾病的方法
公开(公告)号：US06348480B1
公开(公告)日：2002-02-19
申请号：US09529131
申请日：2000-04-07
申请人： Hirokazu Kubota , Yasuhiro Yonetoku , Keizou Sugasawa , Masashi Funatsu , Souichirou Kawazoe , Akira Toyoshima , Yoshinori Okamoto , Jun Ishikawa , Makoto Takeuchi
发明人： Hirokazu Kubota , Yasuhiro Yonetoku , Keizou Sugasawa , Masashi Funatsu , Souichirou Kawazoe , Akira Toyoshima , Yoshinori Okamoto , Jun Ishikawa , Makoto Takeuchi
IPC分类号： C07D41710
CPC分类号： C07D231/12 , C07D231/14 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention is directed to drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, wherein each substituent is defined in the specification. The present invention also relates to a pharmaceutical composition containiing an effective amount of the compound of formula (I) and a pharmaceutically effective carrier. The present invention further relates to methods of treatment of diseases associated with calcium release-activated calcium channels, diseases associated with IL-2 production, and methods of treatment of allergic, inflammatory or auto-immune diseases.
摘要翻译：本发明涉及具有钙释放激活的钙通道抑制作用的药物，特别是由以下通式（I）表示的吡唑衍生物，特别是含有上述的钙释放激活的钙通道抑制剂的药物组合物化合物作为活性成分，其中每个取代基在本说明书中定义。本发明还涉及含有有效量的式（I）化合物和药学有效载体的药物组合物。本发明还涉及治疗与钙释放激活的钙通道相关的疾病，与IL-2产生相关的疾病，以及治疗过敏性，炎性或自身免疫性疾病的方法。

6. 发明授权

US07285554B2 Pyrazole derivative 失效
标题翻译：吡唑衍生物
公开(公告)号：US07285554B2
公开(公告)日：2007-10-23
申请号：US11399379
申请日：2006-04-07
申请人： Hirokazu Kubota , Yasuhiro Yonetoku , Keizo Sugasawa , Masashi Funatsu , Souichirou Kawazoe , Akira Toyoshima , Yoshinori Okamoto , Jun Ishikawa , Makoto Takeuchi
发明人： Hirokazu Kubota , Yasuhiro Yonetoku , Keizo Sugasawa , Masashi Funatsu , Souichirou Kawazoe , Akira Toyoshima , Yoshinori Okamoto , Jun Ishikawa , Makoto Takeuchi
IPC分类号： C07D231/12 , A61K31/415
CPC分类号： C07D231/12 , C07D231/14 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要： Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: D: pyrazolyl which may have 1 to 3 substituents selected from the group consisting of -Alk, -lower alkenyl, -lower alkynyl, -halogeno-lower alkyl, -Alk-cycloalkyl, -Alk-O-Alk, -cycloalkyl, —O-Alk, —COOH, —COO-Alk and -Hal, n: 0 or 1, B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4═CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more substituents).
摘要翻译：药物，特别是具有钙释放激活的钙通道抑制作用的以下通式（I）表示的吡唑衍生物和药物组合物，特别是含有上述化合物作为活性成分的钙释放激活的钙通道抑制剂，（式中，每个符号具有以下含义：D：吡唑基，其可以具有1〜3个选自-Alk， - 低级烯基， - 低级炔基， - 卤代 - 低级烷基，-Al-环烷基， -Alk-O-Alk， - 环烷基，-O-Alk，-COOH，-COO-Alk和-Hal，n：0或1，B：亚苯基，含氮二价饱和环基或单环可以被Alk取代的二价杂芳族环基团，X：-NR 1 -CR 2，R 3，...， 2，-NR 3 -NR 1 - ， - NR 1 -SO 2 - ， - SO 2 - ， - SO 2 或者-CR 4 -CR 5 - ，以及可以具有的A：苯环一个o 更多取代基; 可以具有一个或多个取代基的单 - ，二 - 或三环稠合杂芳基; 可以具有一个或多个取代基的环烷基; 可具有一个或多个取代基的含氮饱和环基; 可以具有一个或多个取代基的低级烯基; 可以具有一个或多个取代基的低级炔基; 或Alk，其可以具有一个或多个取代基）。

7. 发明申请

US20050234055A1 Pyrazole derivative 失效
标题翻译：吡唑衍生物
公开(公告)号：US20050234055A1
公开(公告)日：2005-10-20
申请号：US11154591
申请日：2005-06-17
申请人： Hirokazu Kubota , Yasuhiro Yonetoku , Keizo Sugasawa , Masashi Funatsu , Souichirou Kawazoe , Akira Toyoshima , Yoshinori Okamoto , Jun Ishikawa , Makoto Takeuchi
发明人： Hirokazu Kubota , Yasuhiro Yonetoku , Keizo Sugasawa , Masashi Funatsu , Souichirou Kawazoe , Akira Toyoshima , Yoshinori Okamoto , Jun Ishikawa , Makoto Takeuchi
IPC分类号： A61K31/4155 , A61K31/416 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/538 , C07D231/12 , C07D231/14 , C07D401/12 , C07D403/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/02 , C07D417/02 , C07D417/04 , C07D417/12 , C07D417/14 , C07D521/00 , C07D43/02 , C07D49/02
CPC分类号： C07D231/12 , C07D231/14 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要： Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4═CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more substituents).
摘要翻译：药物，特别是具有钙释放依赖性钙通道抑制作用的药物组合物，特别是含有上述化合物作为活性成分的钙释放依赖性钙通道抑制剂的下述通式（I）表示的吡唑衍生物，（在该式中，每个符号具有以下含义：B：亚苯基，含氮，二价饱和环基或可被Alk，X：-NR 1取代的单环，二价杂芳族环基团其中R 1，R 2，R 3，R 3，R 3，R 3， -NR 2 - ， - SO 2 - ， - SO 2 - ， - SO 2 - ， - SO 2 - ， - SO 2 - 可以具有一个或多个取代基的一个 - 二环或三环稠合杂芳基，其可以具有一个或多个取代基;可具有一个或多个取代基的环烷基;可具有一个或多个取代基的含氮饱和环基团 ents 可以具有一个或多个取代基的低级烯基; 可以具有一个或多个取代基的低级炔基; 或Alk，其可以具有一个或多个取代基）。

8. 发明授权

US08524727B2 Pyrimidine compound 有权
标题翻译：嘧啶化合物
公开(公告)号：US08524727B2
公开(公告)日：2013-09-03
申请号：US12933137
申请日：2010-03-29
申请人： Yuji Matsushima , Hirokazu Kubota , Hisao Hamaguchi , Yoshinori Okamoto , Takeshi Hondo , Fusako Nishigaki
发明人： Yuji Matsushima , Hirokazu Kubota , Hisao Hamaguchi , Yoshinori Okamoto , Takeshi Hondo , Fusako Nishigaki
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D239/42 , C07D239/34 , C07D239/38 , C07D239/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/06 , C07D451/04 , C07D453/02 , C07D491/107 , C07D493/08
摘要： A novel and excellent method for preventing and/or treating diseases related to a cannabinoid type 2 receptor, based on an agonistic action on a cannabinoid type 2 receptor. It was found that a hetero ring derivative mainly having two substituents, for example, a pyrimidine-5-carboxamide derivative having a substituent amino group at the 2-position, exhibits a potent agonistic action on a cannabinoid type 2 receptor, and can be an agent for preventing and/or treating diseases related to a cannabinoid type 2 receptor such as inflammatory diseases, pain, and the like.
摘要翻译：基于对大麻素2型受体的激动作用，预防和/或治疗与大麻素2型受体相关的疾病的新颖且优异的方法。发现主要具有两个取代基的杂环衍生物，例如2-位具有取代基氨基的嘧啶-5-甲酰胺衍生物对大麻素2型受体表现出强烈的激动作用，并且可以是用于预防和/或治疗与大麻素2型受体相关的疾病如炎性疾病，疼痛等的药剂。

9. 发明申请

US20110053912A1 PYRIMIDINE COMPOUND 有权
标题翻译：吡嗪化合物
公开(公告)号：US20110053912A1
公开(公告)日：2011-03-03
申请号：US12933137
申请日：2010-03-29
申请人： Yuji Matsushima , Hirokazu Kubota , Hisao Hamaguchi , Yoshinori Okamoto , Takeshi Hondo , Fusako Nishigaki
发明人： Yuji Matsushima , Hirokazu Kubota , Hisao Hamaguchi , Yoshinori Okamoto , Takeshi Hondo , Fusako Nishigaki
IPC分类号： A61K31/55 , C07D405/12 , A61K31/506 , A61P29/00 , C07D413/12 , A61K31/5377 , C07D417/12 , A61K31/541 , C07D491/107 , C07D417/14
CPC分类号： C07D239/42 , C07D239/34 , C07D239/38 , C07D239/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/06 , C07D451/04 , C07D453/02 , C07D491/107 , C07D493/08
摘要： A novel and excellent method for preventing and/or treating diseases related to a cannabinoid type 2 receptor, based on an agonistic action on a cannabinoid type 2 receptor. It was found that a hetero ring derivative mainly having two substituents, for example, a pyrimidine-5-carboxamide derivative having a substituent amino group at the 2-position, exhibits a potent agonistic action on a cannabinoid type 2 receptor, and can be an agent for preventing and/or treating diseases related to a cannabinoid type 2 receptor such as inflammatory diseases, pain, and the like.
摘要翻译：基于对大麻素2型受体的激动作用，预防和/或治疗与大麻素2型受体相关的疾病的新颖且优异的方法。发现主要具有两个取代基的杂环衍生物，例如2-位具有取代基氨基的嘧啶-5-甲酰胺衍生物对大麻素2型受体表现出强烈的激动作用，并且可以是用于预防和/或治疗与大麻素2型受体相关的疾病如炎性疾病，疼痛等的药剂。

10. 发明授权

US07247635B2 Pyrazole derivative 失效
标题翻译：吡唑衍生物
公开(公告)号：US07247635B2
公开(公告)日：2007-07-24
申请号：US11154591
申请日：2005-06-17
申请人： Hirokazu Kubota , Yasuhiro Yonetoku , Keizo Sugasawa , Masashi Funatsu , Souichirou Kawazoe , Akira Toyoshima , Yoshinori Okamoto , Jun Ishikawa , Makoto Takeuchi
发明人： Hirokazu Kubota , Yasuhiro Yonetoku , Keizo Sugasawa , Masashi Funatsu , Souichirou Kawazoe , Akira Toyoshima , Yoshinori Okamoto , Jun Ishikawa , Makoto Takeuchi
IPC分类号： C07D231/12 , A61K31/415
CPC分类号： C07D231/12 , C07D231/14 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要： Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4═CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more substituents).
摘要翻译：药物，特别是具有钙释放依赖性钙通道抑制作用的药物组合物，特别是含有上述化合物作为活性成分的钙释放依赖性钙通道抑制剂的下述通式（I）表示的吡唑衍生物，（在该式中，每个符号具有以下含义：B：亚苯基，含氮，二价饱和环基或可被Alk，X：-NR 1取代的单环，二价杂芳族环基团其中R 1，R 2，R 3，R 3，R 3，R 3， -NR 2 - ， - SO 2 - ， - SO 2 - ， - SO 2 - ， - SO 2 - ， - SO 2 - 可以具有一个或多个取代基的一个 - 二环或三环稠合杂芳基，其可以具有一个或多个取代基;可具有一个或多个取代基的环烷基;可具有一个或多个取代基的含氮饱和环基团 ents 可以具有一个或多个取代基的低级烯基; 可以具有一个或多个取代基的低级炔基; 或Alk，其可以具有一个或多个取代基）。

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