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1. 发明申请

US20090270376A1 HETEROCYCLIC JANUS KINASE 3 INHIBITORS 有权
标题翻译：杂交种JANUS KINASE 3抑制剂
公开(公告)号：US20090270376A1
公开(公告)日：2009-10-29
申请号：US12065234
申请日：2006-12-25
申请人： Takayuki Inoue , Akira Tanaka , Kazuo Nakai , Hiroshi Sasaki , Fumie Takahashi , Shohei Shirakami , Keiko Hatanaka , Yutaka Nakajima , Koichiro Mukoyoshi , Hisao Hamaguchi , Shigeki Kunikawa , Yasuyuki Higashi
发明人： Takayuki Inoue , Akira Tanaka , Kazuo Nakai , Hiroshi Sasaki , Fumie Takahashi , Shohei Shirakami , Keiko Hatanaka , Yutaka Nakajima , Koichiro Mukoyoshi , Hisao Hamaguchi , Shigeki Kunikawa , Yasuyuki Higashi
IPC分类号： A61K31/437 , C07D471/04 , C07D471/14 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P37/00 , A61P25/28 , A61P35/00
CPC分类号： C07D451/04 , C07D471/04 , C07D471/14 , C07D519/00
摘要： The present invention provides a compound of formula (I) having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. The compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).
摘要翻译：本发明提供了具有优异的JAK3抑制活性的式（I）化合物，并且可用作治疗和/或预防各种免疫疾病，包括自身免疫性疾病炎性疾病和过敏性疾病的药剂的活性成分。根据本发明的化合物对JAK3具有抑制活性，因此可用作治疗或预防由不良细胞因子信号传导引起的疾病（例如器官/组织移植期间的排斥，自身免疫性疾病，多发性硬化症）的活性成分，类风湿性关节炎，牛皮癣，哮喘，特应性皮炎，阿尔茨海默病和动脉粥样硬化疾病）或由异常细胞因子信号传导引起的疾病（例如癌症和白血病）。

2. 发明授权

US07879844B2 Heterocyclic janus kinase 3 inhibitors 有权
标题翻译：杂环janus激酶3抑制剂
公开(公告)号：US07879844B2
公开(公告)日：2011-02-01
申请号：US12065234
申请日：2006-12-25
申请人： Takayuki Inoue , Akira Tanaka , Kazuo Nakai , Hiroshi Sasaki , Fumie Takahashi , Shohei Shirakami , Keiko Hatanaka , Yutaka Nakajima , Koichiro Mukoyoshi , Hisao Hamaguchi , Shigeki Kunikawa , Yasuyuki Higashi
发明人： Takayuki Inoue , Akira Tanaka , Kazuo Nakai , Hiroshi Sasaki , Fumie Takahashi , Shohei Shirakami , Keiko Hatanaka , Yutaka Nakajima , Koichiro Mukoyoshi , Hisao Hamaguchi , Shigeki Kunikawa , Yasuyuki Higashi
IPC分类号： A61K31/437 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D471/04 , C07D471/14 , A61P37/00 , A61P25/28 , A61P35/00
CPC分类号： C07D451/04 , C07D471/04 , C07D471/14 , C07D519/00
摘要： The present invention provides a compound of formula (I) having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. The compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).
摘要翻译：本发明提供了具有优异的JAK3抑制活性的式（I）化合物，并且可用作治疗和/或预防各种免疫疾病，包括自身免疫性疾病炎性疾病和过敏性疾病的药剂的活性成分。根据本发明的化合物对JAK3具有抑制活性，因此可用作治疗或预防由不良细胞因子信号传导引起的疾病（例如器官/组织移植期间的排斥，自身免疫性疾病，多发性硬化症）的活性成分，类风湿性关节炎，牛皮癣，哮喘，特应性皮炎，阿尔茨海默病和动脉粥样硬化疾病）或由异常细胞因子信号传导引起的疾病（例如癌症和白血病）。

3. 发明申请

US20110039822A1 HETEROCYCLIC JANUS KINASE 3 INHIBITORS 审中-公开
标题翻译：杂交种JANUS KINASE 3抑制剂
公开(公告)号：US20110039822A1
公开(公告)日：2011-02-17
申请号：US12914475
申请日：2010-10-28
申请人： Takayuki INOUE , Akira Tanaka , Kazuo Nakai , Hiroshi Sasaki , Fumie Takahashi , Shohei Shirakami , Keiko Hatanaka , Yutaka Nakajima , Koichiro Mukoyoshi , Hisao Hamaguchi , Shigeki Kunikawa , Yasuyuki Higashi
发明人： Takayuki INOUE , Akira Tanaka , Kazuo Nakai , Hiroshi Sasaki , Fumie Takahashi , Shohei Shirakami , Keiko Hatanaka , Yutaka Nakajima , Koichiro Mukoyoshi , Hisao Hamaguchi , Shigeki Kunikawa , Yasuyuki Higashi
IPC分类号： A61K31/437 , C07D471/04 , C07D471/14 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61P17/06 , A61P19/02 , A61P37/00 , A61P37/06
CPC分类号： C07D451/04 , C07D471/04 , C07D471/14 , C07D519/00
摘要： The present invention provides a compound having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases.As a result of studies on a novel condensed heterocyclic derivative, the inventors have found that a compound having a cross-linked structure has an excellent JAK3 inhibition activity, and have completed the present invention.In other words, it is verified that the compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).
摘要翻译：本发明提供具有优异的JAK3抑制活性的化合物，可用作治疗和/或预防各种免疫疾病，包括自身免疫性疾病，炎症性疾病和过敏性疾病的药剂的活性成分。作为研究新型稠合杂环衍生物的结果，本发明人发现具有交联结构的化合物具有优异的JAK3抑制活性，并且完成了本发明。换句话说，证实了本发明的化合物对JAK3具有抑制活性，因此可用作治疗或预防由不期望的细胞因子信号传导引起的疾病的药剂的活性成分（例如器官/ 组织移植，自身免疫性疾病，多发性硬化，类风湿性关节炎，牛皮癣，哮喘，特应性皮炎，阿尔茨海默病和动脉粥样硬化疾病）或由异常细胞因子信号传导引起的疾病（例如癌症和白血病）。

4. 发明申请

US20100105661A1 CONDENSED PYRIDINE COMPOUND 审中-公开
标题翻译：浓缩的吡啶化合物
公开(公告)号：US20100105661A1
公开(公告)日：2010-04-29
申请号：US12522987
申请日：2008-01-11
申请人： Shohei Shirakami , Takayuki Inoue , Koichiro Mukoyoshi , Yutaka Nakajima , Hiroyuki Usuda , Hisao Hamaguchi , Yasuyuki Higashi , Keiko Hatanaka
发明人： Shohei Shirakami , Takayuki Inoue , Koichiro Mukoyoshi , Yutaka Nakajima , Hiroyuki Usuda , Hisao Hamaguchi , Yasuyuki Higashi , Keiko Hatanaka
IPC分类号： A61K31/55 , A61K31/501 , A61K31/4965 , A61K31/506 , A61K31/437 , C07D471/04
CPC分类号： C07D471/04 , C07D471/14
摘要： The present invention provides a compound having excellent JAK3 inhibitory activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases.As a result of investigations with respect to novel condensed heterocyclic derivatives, the inventors have verified that a condensed pyridine compound has excellent JAK3 inhibitory activity, thereby completing the present invention.More specifically, it has been verified that since the compound according to the present invention has inhibitory activity against JAK3, the compound is useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transduction (e.g., rejection during live organ/tissue transplantation, autoimmune diseases, asthma, atopic dermatitis, rheumatism, psoriasis and atherosclerotic disease), or diseases caused by abnormal cytokine signal transduction (e.g., cancer and leukemia).
摘要翻译：本发明提供了具有优异的JAK3抑制活性的化合物，可用作治疗和/或预防各种免疫疾病，包括自身免疫性疾病，炎症性疾病和过敏性疾病的药剂的活性成分。作为关于新的稠合杂环衍生物的研究结果，本发明人证实了缩合的吡啶化合物具有优异的JAK3抑制活性，从而完成了本发明。更具体地说，由于本发明的化合物对JAK3具有抑制活性，所以该化合物可用作治疗或预防由不良细胞因子信号转导引起的疾病（例如活体排斥）的药剂的有效成分器官/组织移植，自身免疫疾病，哮喘，特应性皮炎，风湿病，牛皮癣和动脉粥样硬化疾病）或由细胞因子信号转导异常引起的疾病（例如癌症和白血病）。

5. 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。

6. 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。

7. 发明申请

US20100105658A1 AZA-BRIDGED-RING COMPOUND 有权
标题翻译： AZA-BRIDGED-RING化合物
公开(公告)号：US20100105658A1
公开(公告)日：2010-04-29
申请号：US12524758
申请日：2008-02-07
申请人： Shinya Nagashima , Toru Kontani , Hiroshi Nagata , Yuji Matsushima , Hisao Hamaguchi , Tadatsura Koshika
发明人： Shinya Nagashima , Toru Kontani , Hiroshi Nagata , Yuji Matsushima , Hisao Hamaguchi , Tadatsura Koshika
IPC分类号： A61K31/439 , C07D453/02 , C07D223/14 , A61K31/55 , A61P29/00
CPC分类号： C07D453/02 , C07D471/18
摘要： [Problems] Provided is a compound which has an antagonistic action on a muscarinic M3 receptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.[Means for Solving Problems] The present inventors have made studies on a compound having an antagonistic action on the binding of a muscarinic M3 receptor, and they have found that an aza-bridged-ring compound or a salt thereof has an antagonistic action on the binding of a muscarinic M3 receptor, thereby completing the present invention. The aza-bridged-ring compound of the present invention has an antagonistic action on the binding of a muscarinic M3 receptor, and can be used as a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.
摘要翻译： [问题]提供对毒蕈碱M3受体具有拮抗作用的化合物，并且可用作炎性疾病如慢性阻塞性肺病（COPD），哮喘的预防和/或治疗剂的活性成分喜欢。解决问题的手段本发明人研究了对毒蕈碱性M3受体的结合具有拮抗作用的化合物，并且已经发现，氮杂桥环化合物或其盐对其有拮抗作用结合毒蕈碱M3受体，从而完成本发明。本发明的氮杂桥环化合物对毒蕈碱性M3受体的结合具有拮抗作用，可用作炎性疾病如慢性阻塞性肺疾病（COPD）的预防和/或治疗剂，，哮喘等。

8. 发明授权

US08367696B2 Aza-bridged-ring compound 有权
标题翻译：氮杂桥环化合物
公开(公告)号：US08367696B2
公开(公告)日：2013-02-05
申请号：US12524758
申请日：2008-02-08
申请人： Shinya Nagashima , Toru Kontani , Hiroshi Nagata , Yuji Matsushima , Hisao Hamaguchi , Tadatsura Koshika
发明人： Shinya Nagashima , Toru Kontani , Hiroshi Nagata , Yuji Matsushima , Hisao Hamaguchi , Tadatsura Koshika
IPC分类号： A61K31/439 , C07D221/00 , C07D221/02
CPC分类号： C07D453/02 , C07D471/18
摘要： [PROBLEMS] Provided is a compound which has an antagonistic action on a muscarinic M3 receptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.[MEANS For SOLVING PROBLEMS] The present inventors have made studies on a compound having an antagonistic action on the binding of a muscarinic M3 receptor, and they have found that an aza-bridged-ring compound or a salt thereof has an antagonistic action on the binding of a muscarinic M3 receptor, thereby completing the present invention. The aza-bridged-ring compound of the present invention has an antagonistic action on the binding of a muscarinic M3 receptor, and can be used as a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.
摘要翻译： [问题]提供对毒蕈碱M3受体具有拮抗作用并可用作炎性疾病如慢性阻塞性肺疾病（COPD），哮喘的预防和/或治疗剂的活性成分的化合物喜欢。解决问题的手段本发明人研究了对毒蕈碱性M3受体的结合具有拮抗作用的化合物，并且已经发现氮杂桥环化合物或其盐对其具有拮抗作用结合毒蕈碱M3受体，从而完成本发明。本发明的氮杂桥环化合物对毒蕈碱性M3受体的结合具有拮抗作用，可用作炎性疾病如慢性阻塞性肺疾病（COPD）的预防和/或治疗剂，，哮喘等。

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