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）。

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）。

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）。

公开(公告)号：US08163767B2

公开(公告)日：2012-04-24

申请号：US11995445

申请日：2006-07-13

申请人： Takayuki Inoue ,  Takashi Tojo ,  Masataka Morita ,  Yutaka Nakajima ,  Keiko Hatanaka ,  Shohei Shirakami ,  Hiroshi Sasaki ,  Akira Tanaka ,  Fumie Takahashi ,  Koichiro Mukoyoshi ,  Yasuyuki Higashi ,  Akira Okimoto ,  Takeshi Hondo ,  Hitoshi Sawada

发明人： Takayuki Inoue ,  Takashi Tojo ,  Masataka Morita ,  Yutaka Nakajima ,  Keiko Hatanaka ,  Shohei Shirakami ,  Hiroshi Sasaki ,  Akira Tanaka ,  Fumie Takahashi ,  Koichiro Mukoyoshi ,  Yasuyuki Higashi ,  Akira Okimoto ,  Takeshi Hondo ,  Hitoshi Sawada

IPC分类号： A61K31/44 ,  C07D471/14

CPC分类号： C07D471/14 ,  C07D519/00

摘要： The invention relates to compound of the formula (I) or its salt, wherein —R1, —R2, —R3, —R4, —R5, -M-, —X— and —Y═ are as defined in the description, their use of as, medicament, the process for their preparation and use for the treatment of JAK3 mediated diseases.

摘要翻译： 本发明涉及式（I）化合物或其盐，其中-R1，-R2，-R3，-R4，-R5，-M-，-X-和-Y =如说明书中所定义，它们 使用as，药物，其制备方法和用于治疗JAK3介导的疾病。

公开(公告)号：US20090264399A1

公开(公告)日：2009-10-22

申请号：US11995445

申请日：2006-07-13

申请人： Takayuki Inoue ,  Takashi Tojo ,  Masataka Morita ,  Yutaka Nakajima ,  Keiko Hatanaka ,  Shohei Shirakami ,  Hiroshi Sasaki ,  Akira Tanaka ,  Fumie Takahashi ,  Koichiro Mukoyoshi ,  Yasuyuki Higashi ,  Akira Okimoto ,  Takeshi Hondo ,  Hitoshi Sawada

发明人： Takayuki Inoue ,  Takashi Tojo ,  Masataka Morita ,  Yutaka Nakajima ,  Keiko Hatanaka ,  Shohei Shirakami ,  Hiroshi Sasaki ,  Akira Tanaka ,  Fumie Takahashi ,  Koichiro Mukoyoshi ,  Yasuyuki Higashi ,  Akira Okimoto ,  Takeshi Hondo ,  Hitoshi Sawada

IPC分类号： A61K31/437 ,  C07D471/04 ,  C07D413/14 ,  C07D471/14 ,  A61K31/5377 ,  A61K31/397 ,  A61P25/00 ,  A61P37/06 ,  A61P35/00 ,  A61P35/02 ,  A61P11/06

CPC分类号： C07D471/14 ,  C07D519/00

摘要： The invention relates to compound of the formula (I) or its salt, wherein —R1, —R2, —R3, —R4, —R5, -M-, —X— and —Y═ are as defined in the description, their use of as, medicament, the process for their preparation and use for the treatment of JAK3 mediated diseases.

摘要翻译： 本发明涉及式（I）或其盐的化合物，其中-R1，-R2，-R3，-R4，-R5，-M-，-X-和-Y-如说明书中所定义，它们 使用as，药物，其制备方法和用于治疗JAK3介导的疾病。

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）。

公开(公告)号：US20050014812A1

公开(公告)日：2005-01-20

申请号：US10860139

申请日：2004-06-04

申请人： Hisashi Hayashida ,  Keiko Hatanaka ,  Takeshi Kato ,  Yoshiyuki Kido ,  Masaki Tomishima ,  Hiroshi Kayakiri ,  Ichiro Takase ,  Takahiro Hiramura

发明人： Hisashi Hayashida ,  Keiko Hatanaka ,  Takeshi Kato ,  Yoshiyuki Kido ,  Masaki Tomishima ,  Hiroshi Kayakiri ,  Ichiro Takase ,  Takahiro Hiramura

IPC分类号： C07D235/08 ,  C07D235/10 ,  C07D235/26 ,  C07D235/28 ,  C07D401/06 ,  C07D401/12 ,  C07D413/06 ,  C07D417/06 ,  A61K31/4184 ,  C07D235/20 ,  C07

CPC分类号： C07D401/06 ,  C07D235/08 ,  C07D235/10 ,  C07D235/26 ,  C07D235/28 ,  C07D401/12 ,  C07D413/06 ,  C07D417/06

摘要： The present invention provides novel benzimidazole compounds of the formula (I): wherein each symbol is as defined in the specification, salts thereof and prodrugs thereof, which are useful in treating, for example, the diseases curable through decrease in blood sugar level.

摘要翻译： 本发明提供新的式（I）的苯并咪唑化合物：其中每个符号如本说明书中所定义，其盐和前药，其可用于治疗例如通过降低血糖水平可治愈的疾病。