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1. 发明授权

US07732442B2 Chemokine receptor antagonist and medical use thereof 失效
标题翻译：趋化因子受体拮抗剂及其医疗用途
公开(公告)号：US07732442B2
公开(公告)日：2010-06-08
申请号：US10570813
申请日：2004-09-03
申请人： Hiromu Habashita , Hiroshi Ochiai , Natsuko Tokuda , Shiro Shibayama , Noriki Watanabe , Takaki Komiya , Kazuhiko Takeda
发明人： Hiromu Habashita , Hiroshi Ochiai , Natsuko Tokuda , Shiro Shibayama , Noriki Watanabe , Takaki Komiya , Kazuhiko Takeda
IPC分类号： A61K31/538
CPC分类号： C07D213/82 , C07D213/76 , C07D241/22 , C07D241/44 , C07D401/12 , C07D403/12 , C07D417/12
摘要： The present invention relates to a compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound represented by formula (I) has chemokine receptor (especially in CCR4 and/or CCR5) antagonistic activity. Therefore it is useful for prevention and/or treatment of a chemokine receptor-mediated disease such as inflammatory and/or allergic diseases [systemic inflammatory response syndrome (SIRS), anaphylaxis, anaphylactoid reaction, allergic angiitis, transplant rejection reaction, hepatitis, nephritis, nephropathy, pancreatitis, rhinitis, arthritis, inflammatory ocular disease, inflammatory bowel disease, disease in cerebro and/or circulatory system, respiratory disease, dermatosis, autoimmune disease, and the like], infection [viral disease (human immunodeficiency virus infection, acquired immunodeficiency syndrome, SARS, etc.), and the like], and the like.
摘要翻译：本发明涉及由式（I）表示的化合物，其盐，其N-氧化物，其溶剂合物或前体药物及其医疗用途（式中的符号如说明书中所述）。由式（I）表示的化合物具有趋化因子受体（特别是CCR4和/或CCR5）拮抗活性。因此，可用于预防和/或治疗趋化因子受体介导的疾病如炎性和/或过敏性疾病[全身炎症反应综合征（SIRS），过敏反应，过敏反应，过敏性血管炎，移植排斥反应，肝炎，肾炎，肾病，胰腺炎，鼻炎，关节炎，炎症性眼病，炎性肠病，脑脊液和/或循环系统疾病，呼吸系统疾病，皮肤病，自身免疫性疾病等），感染[病毒性疾病（人类免疫缺陷病毒感染，获得性免疫缺陷综合征，SARS等）等]等。

2. 发明申请

US20070254886A1 Chemokine Receptor Antagonist and Medical Use Thereof 失效
标题翻译：趋化因子受体拮抗剂及其用途
公开(公告)号：US20070254886A1
公开(公告)日：2007-11-01
申请号：US10570813
申请日：2004-09-03
申请人： Hiromu Habashita , Hiroshi Ochiai , Natsuko Tokuda , Shiro Shibayama , Noriki Watanabe , Takaki Komiya , Kazuhiko Takeda
发明人： Hiromu Habashita , Hiroshi Ochiai , Natsuko Tokuda , Shiro Shibayama , Noriki Watanabe , Takaki Komiya , Kazuhiko Takeda
IPC分类号： A61K31/4412 , A61K31/444 , A61K31/4965 , A61K31/498 , A61P11/06 , A61P17/00 , A61P31/00 , A61P9/00 , C07D213/72 , C07D241/22 , C07D241/44
CPC分类号： C07D213/82 , C07D213/76 , C07D241/22 , C07D241/44 , C07D401/12 , C07D403/12 , C07D417/12
摘要： The present invention relates to a compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound represented by formula (I) has chemokine receptor (especially in CCR4 and/or CCR5) antagonistic activity. Therefore it is useful for prevention and/or treatment of a chemokine receptor-mediated disease such as inflammatory and/or allergic diseases [systemic inflammatory response syndrome (SIRS), anaphylaxis, anaphylactoid reaction, allergic angiitis, transplant rejection reaction, hepatitis, nephritis, nephropathy, pancreatitis, rhinitis, arthritis, inflammatory ocular disease, inflammatory bowel disease, disease in cerebro and/or circulatory system, respiratory disease, dermatosis, autoimmune disease, and the like], infection [viral disease (human immunodeficiency virus infection, acquired immunodeficiency syndrome, SARS, etc.), and the like], and the like.
摘要翻译：本发明涉及由式（I）表示的化合物，其盐，其N-氧化物，其溶剂合物或前体药物及其医疗用途（式中的符号如说明书中所述）。由式（I）表示的化合物具有趋化因子受体（特别是CCR4和/或CCR5）拮抗活性。因此，可用于预防和/或治疗趋化因子受体介导的疾病如炎性和/或过敏性疾病[全身炎症反应综合征（SIRS），过敏反应，过敏反应，过敏性血管炎，移植排斥反应，肝炎，肾炎，肾病，胰腺炎，鼻炎，关节炎，炎症性眼病，炎性肠病，脑脊液和/或循环系统疾病，呼吸系统疾病，皮肤病，自身免疫性疾病等），感染[病毒性疾病（人类免疫缺陷病毒感染，获得性免疫缺陷综合征，SARS等）等]等。

3. 发明申请

US20100266539A1 CHEMOKINE RECEPTOR ANTAGONIST AND MEDICAL USE THEREOF 审中-公开
标题翻译：化疗受体拮抗剂及其医疗用途
公开(公告)号：US20100266539A1
公开(公告)日：2010-10-21
申请号：US12731390
申请日：2010-03-25
申请人： Hiromu HABASHITA , Hiroshi Ochiai , Natsuko Tokuda , Shiro Shibayama , Noriki Watanabe , Takaki Komiya , Kazuhiko Takeda
发明人： Hiromu HABASHITA , Hiroshi Ochiai , Natsuko Tokuda , Shiro Shibayama , Noriki Watanabe , Takaki Komiya , Kazuhiko Takeda
IPC分类号： A61K38/21 , C07D213/76 , A61K31/44 , C07D401/12 , A61K31/444 , C07D241/22 , A61K31/4965 , A61K31/497 , C07D241/44 , A61K31/498 , C07D403/12 , C07D417/12 , A61K31/56 , A61K38/22 , A61P37/06 , A61P37/08 , A61P29/00 , A61P17/00 , A61P11/06 , A61K31/557
CPC分类号： C07D213/82 , C07D213/76 , C07D241/22 , C07D241/44 , C07D401/12 , C07D403/12 , C07D417/12
摘要： The present invention relates to a compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound represented by formula (I) has chemokine receptor (especially in CCR4 and/or CCR5) antagonistic activity. Therefore it is useful for prevention and/or treatment of a chemokine receptor-mediated disease such as inflammatory and/or allergic diseases [systemic inflammatory response syndrome (SIRS), anaphylaxis, anaphylactoid reaction, allergic angiitis, transplant rejection reaction, hepatitis, nephritis, nephropathy, pancreatitis, rhinitis, arthritis, inflammatory ocular disease, inflammatory bowel disease, disease in cerebro and/or circulatory system, respiratory disease, dermatosis, autoimmune disease, and the like], infection [viral disease (human immunodeficiency virus infection, acquired immunodeficiency syndrome, SARS, etc.), and the like], and the like.
摘要翻译：本发明涉及由式（I）表示的化合物，其盐，其N-氧化物，其溶剂合物或前体药物及其医疗用途（式中的符号如说明书中所述）。由式（I）表示的化合物具有趋化因子受体（特别是CCR4和/或CCR5）拮抗活性。因此，可用于预防和/或治疗趋化因子受体介导的疾病如炎性和/或过敏性疾病[全身炎症反应综合征（SIRS），过敏反应，过敏反应，过敏性血管炎，移植排斥反应，肝炎，肾炎，肾病，胰腺炎，鼻炎，关节炎，炎症性眼病，炎性肠病，脑脊液和/或循环系统疾病，呼吸系统疾病，皮肤病，自身免疫性疾病等），感染[病毒性疾病（人类免疫缺陷病毒感染，获得性免疫缺陷综合征，SARS等）等]等。

4. 发明授权

US08614323B2 Chemokine receptor antagonists and use thereof 失效
标题翻译：趋化因子受体拮抗剂及其用途
公开(公告)号：US08614323B2
公开(公告)日：2013-12-24
申请号：US13596780
申请日：2012-08-28
申请人： Masaya Kokubo , Motoyuki Tanaka , Hiroshi Ochiai , Yoshikazu Takaoka , Shiro Shibayama
发明人： Masaya Kokubo , Motoyuki Tanaka , Hiroshi Ochiai , Yoshikazu Takaoka , Shiro Shibayama
IPC分类号： C07D471/10
CPC分类号： A61K31/695 , A61K31/4178 , A61K31/435 , A61K31/5377 , A61K45/06 , C07D233/64 , C07D471/10 , C07F7/1804
摘要： The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.
摘要翻译：本发明涉及由式（I）表示的化合物：其中所有符号如本文所定义，其盐，其溶剂化物或其前药。本发明的化合物对CXCR4具有拮抗作用，因此可用作CXCR4介导的疾病的预防和/或治疗剂，例如炎性和免疫疾病（例如类风湿性关节炎，关节炎，视网膜病变，肺纤维化，移植器官的排斥等），过敏性疾病，感染（例如，人类免疫缺陷病毒感染，获得性免疫缺陷综合征等），精神神经病，脑疾病，心血管疾病，代谢疾病和癌性疾病（例如，癌症，癌症转移等）或再生治疗剂。

5. 发明申请

US20120101280A1 COMPOUND HAVING SPIRO-BONDED CYCLIC GROUP AND USE THEREOF 失效
标题翻译：具有螺旋结合循环组的化合物及其用途
公开(公告)号：US20120101280A1
公开(公告)日：2012-04-26
申请号：US13378799
申请日：2010-06-15
申请人： Koji Yoshida , Hiroshi Ochiai , Kousuke Tani , Shiro Shibayama , Miki Kasano
发明人： Koji Yoshida , Hiroshi Ochiai , Kousuke Tani , Shiro Shibayama , Miki Kasano
IPC分类号： C07D471/10
CPC分类号： C07D471/10
摘要： The invention relates to a compound represented by formula (I): a salt thereof, an N-oxide thereof, or a solvate thereof (symbols in the formula are as described in the specification).The compound of the present invention exhibits very low risk of side effects and also has persistent and strong antagonistic activity against CXCR4, and is therefore useful as pharmaceuticals, for example, preventive and/or therapeutic agent for inflammatory and immune diseases, infections (for example, HIV infection), diseases associated with HIV infection (for example, acquired immunodeficiency syndrome (AIDS)), cancer, cancer metastasis, psychoneurotic diseases and cardiovascular diseases (for example, retinopathy), metabolic diseases, cancerous diseases, or an agent for regeneration therapy.
摘要翻译：本发明涉及由式（I）表示的化合物：其盐，其N-氧化物或其溶剂化物（式中的符号如说明书中所述）。本发明的化合物显示出非常低的副作用风险，并且对CXCR4具有持久和强烈的拮抗活性，因此可用作药物，例如用于炎症和免疫疾病，感染的预防和/或治疗剂（例如，艾滋病毒感染），与艾滋病毒感染有关的疾病（例如，获得性免疫缺陷综合征（AIDS）），癌症，癌症转移，精神神经病和心血管疾病（例如视网膜病变），代谢疾病，癌性疾病或再生药剂治疗。

6. 发明申请

US20090325992A1 COMPOUND HAVING CYCLIC GROUP BOUND THERETO THROUGH SPIRO BINDING AND USE THEREOF 审中-公开
标题翻译：具有通过螺旋结合的循环组合物的化合物及其用途
公开(公告)号：US20090325992A1
公开(公告)日：2009-12-31
申请号：US12375841
申请日：2007-07-30
申请人： Keisuke Hanada , Masaya Kokubo , Hiroshi Ochiai , Kousuke Tani , Shiro Shibayama
发明人： Keisuke Hanada , Masaya Kokubo , Hiroshi Ochiai , Kousuke Tani , Shiro Shibayama
IPC分类号： A61K31/438 , C07D471/10
CPC分类号： C07D471/04 , A61K45/06 , C07D401/12 , C07D471/10 , C07D487/10
摘要： A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, cancerous diseases (for example, cancer, cancer metastasis, etc.), a preventive and/or therapeutic agent for cancerous diseases or infections, or an agent for regeneration therapy.
摘要翻译：由通式（I）表示的化合物：其盐，其溶剂化物或前药，其中所有符号如本说明书中所定义，具有对CXCR4的拮抗活性，因此可用作预防和/或治疗剂 CXCR4介导的疾病，例如炎症和免疫疾病（例如类风湿性关节炎，关节炎，视网膜病变，黄斑变性，肺纤维化，移植器官排斥反应等），过敏性疾病，感染（例如，人类免疫缺陷病毒感染，获得性免疫缺陷综合征等），精神神经性疾病，脑疾病，心血管疾病，代谢疾病，癌性疾病（例如癌症，癌症转移等），癌性疾病或感染的预防和/或治疗剂，或再生治疗剂。

7. 发明申请

US20090192182A1 COMPOUND HAVING ACIDIC GROUP WHICH MAY BE PROTECTED, AND USE THEREOF 失效
标题翻译：具有可被保护的酸性化合物的化合物及其用途
公开(公告)号：US20090192182A1
公开(公告)日：2009-07-30
申请号：US12301194
申请日：2007-05-15
申请人： Kensuke Kusumi , Masaya Kokubo , Hiroshi Ochiai , Shiro Shibayama
发明人： Kensuke Kusumi , Masaya Kokubo , Hiroshi Ochiai , Shiro Shibayama
IPC分类号： A61K31/438 , C07D471/10 , A61P35/00
CPC分类号： C07D471/10
摘要： A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification. The compound of the present invention has antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.
摘要翻译：由通式（I）表示的化合物：其盐，其溶剂合物或其前药，其中所有符号如说明书中所定义。本发明的化合物对CXCR4具有拮抗作用，因此可用作CXCR4介导的疾病的预防和/或治疗剂，例如炎性和免疫疾病（例如类风湿性关节炎，关节炎，全身性红斑狼疮，视网膜病变，黄斑变性，肺纤维化，移植器官排斥反应等），过敏性疾病，感染（例如人类免疫缺陷病毒感染，获得性免疫缺陷综合征等），精神神经病，脑疾病，心血管疾病，代谢疾病，癌性疾病例如癌症，癌症转移等）或再生治疗剂。

8. 发明申请

US20090169567A1 BASIC GROUP-CONTAINING COMPOUND AND USE THEREOF 失效
标题翻译：含基本组合物及其用途
公开(公告)号：US20090169567A1
公开(公告)日：2009-07-02
申请号：US12094100
申请日：2006-11-17
申请人： Masaya Kokubo , Hiroshi Ochiai , Yoshikazu Takaoka , Shiro Shibayama
发明人： Masaya Kokubo , Hiroshi Ochiai , Yoshikazu Takaoka , Shiro Shibayama
IPC分类号： C07D471/10 , A61K31/438 , A61K31/537 , C07D498/10 , A61K39/42 , A61K31/7105 , A61K39/21 , A61P31/18
CPC分类号： C07D403/12 , C07D233/64 , C07D401/12 , C07D403/14 , C07D471/10 , C07D498/10
摘要： A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiac /vascular disease (for example, arteriosclerosis, myocardial infarction, stenocardia, cerebral infarction, chronic arterial occlusive disease, etc.), metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), a preventive and/or therapeutic agent for cancerous diseases or infections, or an agent for regeneration therapy.
摘要翻译：由通式（I）表示的化合物：其盐，其溶剂化物或前药，其中所有符号如本说明书中所定义，具有对CXCR4的拮抗活性，因此可用作预防和/或治疗剂 CXCR4介导的疾病，例如炎症和免疫疾病（例如类风湿性关节炎，关节炎，全身性红斑狼疮，视网膜病变，黄斑变性，肺纤维化，移植器官排斥反应等），过敏性疾病，感染（例如人类免疫缺陷病毒感染，获得性免疫缺陷综合征等），精神神经病，脑疾病，心脏/血管疾病（例如动脉硬化，心肌梗塞，心动过速，脑梗死，慢性动脉闭塞性疾病等），代谢疾病和癌性疾病（例如，癌症，癌症转移等），癌性疾病或感染的预防和/或治疗剂，或再生治疗剂。

9. 发明授权

US08168783B2 Chemokine receptor antagonists and use thereof 失效
标题翻译：趋化因子受体拮抗剂及其用途
公开(公告)号：US08168783B2
公开(公告)日：2012-05-01
申请号：US12094100
申请日：2006-11-17
申请人： Masaya Kokubo , Hiroshi Ochiai , Yoshikazu Takaoka , Shiro Shibayama
发明人： Masaya Kokubo , Hiroshi Ochiai , Yoshikazu Takaoka , Shiro Shibayama
IPC分类号： C07D471/10
CPC分类号： C07D403/12 , C07D233/64 , C07D401/12 , C07D403/14 , C07D471/10 , C07D498/10
摘要： A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease (for example, arteriosclerosis, myocardial infarction, stenocardia, cerebral infarction, chronic arterial occlusive disease, etc.), metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), a preventive and/or therapeutic agent for cancerous diseases or infections, or an agent for regeneration therapy.
摘要翻译：由通式（I）表示的化合物：其盐，其溶剂化物或前药，其中所有符号如本说明书中所定义，具有对CXCR4的拮抗活性，因此可用作预防和/或治疗剂 CXCR4介导的疾病，例如炎症和免疫疾病（例如类风湿性关节炎，关节炎，全身性红斑狼疮，视网膜病变，黄斑变性，肺纤维化，移植器官排斥反应等），过敏性疾病，感染（例如人类免疫缺陷病毒感染，获得性免疫缺陷综合征等），精神神经病，脑疾病，心脏/血管疾病（例如动脉硬化，心肌梗塞，心动过速，脑梗死，慢性动脉闭塞性疾病等），代谢疾病和癌性疾病（例如，癌症，癌症转移等），癌性疾病或感染的预防和/或治疗剂，或再生治疗剂。

10. 发明授权

US08680092B2 Nitrogenous heterocyclic compound and medicinal use thereof 失效
标题翻译：氮杂环化合物及其医药用途
公开(公告)号：US08680092B2
公开(公告)日：2014-03-25
申请号：US11816940
申请日：2006-02-24
申请人： Hiroshi Ochiai , Akira Ohhata , Yoshikazu Takaoka , Shiro Shibayama
发明人： Hiroshi Ochiai , Akira Ohhata , Yoshikazu Takaoka , Shiro Shibayama
IPC分类号： A61P11/00 , A61P19/02 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/06 , A61P43/00 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , A61K31/506 , A61K31/5377 , A61K39/21 , A61K39/395 , A61K45/00
CPC分类号： A61K45/06 , A61K31/506 , A61K31/5377 , A61K31/55 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14
摘要： A compound represented by formula (I): (wherein the symbols are the same as defined in the description), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medicinal use thereof. The compound represented by formula (I) has CXCR4 antagonistic activity. It is hence useful as, e.g., a preventive and/or therapeutic agent for CXCR4-mediated diseases such as inflammatory/immunologic diseases (e.g., rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, and rejection reactions of transplanted organs), allergic diseases, infections diseases (e.g., human immunodeficiency virus infection and acquired immunologic deficiency syndrome), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease, metabolic diseases, cancer diseases (e.g., cancer, cancer metastasis) or as an agent for regeneration therapy.
摘要翻译：由式（I）表示的化合物：其中符号与说明书中定义相同，其盐，其N-氧化物，其溶剂合物或其前药，及其药物用途。由式（I）表示的化合物具有CXCR4拮抗活性。因此，其可用作例如CXCR4介导的疾病如炎症/免疫疾病（例如类风湿性关节炎，关节炎，视网膜病变，肺纤维化和移植器官的排斥反应）的预防和/或治疗剂，过敏性疾病，感染疾病（例如人类免疫缺陷病毒感染和获得性免疫缺陷综合征），精神神经病，脑疾病，心脏/血管疾病，代谢疾病，癌症疾病（例如癌症，癌症转移）或再生治疗剂。

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