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1. 发明授权

US08822459B2 Compound containing basic group and use thereof 有权
标题翻译：含有碱性基团的化合物及其用途
公开(公告)号：US08822459B2
公开(公告)日：2014-09-02
申请号：US13027957
申请日：2011-02-15
申请人： Masaya Kokubo , Yoshikazu Takaoka , Shiro Shibayama
发明人： Masaya Kokubo , Yoshikazu Takaoka , Shiro Shibayama
IPC分类号： A61K31/535 , C07D265/28 , C07D471/10 , C07D233/90 , C07D401/14 , C07D487/10 , C07D233/16 , C07D233/84 , C07D403/12 , C07D403/14
CPC分类号： C07D471/10 , C07D233/16 , C07D233/84 , C07D233/90 , C07D401/14 , C07D403/12 , C07D403/14 , C07D487/10
摘要： The present invention relates to a compound represented by formula (I-0): wherein symbols in formula have the same meanings as described in the present specification, a salt thereof, an N-oxide thereof or a solvate thereof or a prodrug thereof, and medical use 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, 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, 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-0）表示的化合物：其中式中的符号与本说明书中所述的相同含义，其盐，其N-氧化物或其溶剂合物或其前药，以及医疗用途。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，代谢疾病和癌性疾病（例如癌症，癌转移等）或再生治疗剂。

2. 发明授权

US08519124B2 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：US08519124B2
公开(公告)日：2013-08-27
申请号：US13415399
申请日：2012-03-08
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： C07D221/20 , C07D265/14 , C07D401/14 , C07D403/12 , C07D403/14
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。

3. 发明申请

US20120328627A1 CHEMOKINE RECEPTOR ANTAGONISTS AND USE THEREOF 失效
标题翻译：化疗受体拮抗剂及其用途
公开(公告)号：US20120328627A1
公开(公告)日：2012-12-27
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： A61K31/438 , A61K31/5377 , A61P35/00 , A61K39/42 , A61K31/713 , A61P37/06 , A61P31/18 , A61P35/04 , A61P29/00 , A61P19/02 , A61P9/10 , C07D471/10 , A61K39/21
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。

4. 发明授权

US08318931B2 Chemokine receptor antagonists and use thereof 有权
标题翻译：趋化因子受体拮抗剂及其用途
公开(公告)号：US08318931B2
公开(公告)日：2012-11-27
申请号：US12091403
申请日：2006-10-27
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： A61P35/00 , 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. 发明授权

US08293896B2 Chemokine receptor antagonists and use thereof 有权
公开(公告)号：US08293896B2
公开(公告)日：2012-10-23
申请号：US12091403
申请日：2006-10-27
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： A61P35/00 , C07D471/10
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.

6. 发明申请

US20090118279A1 COMPOUND CONTAINING BASIC GROUP AND USE THEREOF 有权
标题翻译：包含基本组合的化合物及其用途
公开(公告)号：US20090118279A1
公开(公告)日：2009-05-07
申请号：US12091403
申请日：2006-10-27
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： A61K31/5377 , C07D471/10 , A61P35/00 , A61K31/438
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。

7. 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。

8. 发明申请

US20120207765A1 CHEMOKINE RECEPTOR ANTAGONISTS AND USE THEREOF 失效
标题翻译：化疗受体拮抗剂及其用途
公开(公告)号：US20120207765A1
公开(公告)日：2012-08-16
申请号：US13415399
申请日：2012-03-08
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： A61K31/454 , A61K39/42 , A61K31/7052 , A61K39/21 , C07D403/12 , A61K31/4178 , C07D221/20 , A61K31/438 , C07D403/14 , A61K31/55 , C07D265/14 , A61K31/537 , A61P11/06 , A61P31/18 , A61P37/06 , A61P35/00 , A61P19/02 , A61P11/00 , C07D401/14
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. 发明申请

US20110142856A1 COMPOUND CONTAINING BASIC GROUP AND USE THEREOF 有权
标题翻译：包含基本组合的化合物及其用途
公开(公告)号：US20110142856A1
公开(公告)日：2011-06-16
申请号：US13027957
申请日：2011-02-15
申请人： Masaya KOKUBO , Yoshikazu Takaoka , Shiro Shibayama
发明人： Masaya KOKUBO , Yoshikazu Takaoka , Shiro Shibayama
IPC分类号： A61K31/4178 , C07D403/12 , C07D401/14 , C07D401/12 , C07D413/12 , C07D471/10 , C07D498/10 , C07D487/10 , A61K31/713 , A61K39/42 , A61K39/21 , A61K31/454 , A61K31/4725 , A61K31/4439 , A61K31/4709 , A61K31/5377 , A61K31/4184 , A61K31/438 , A61K31/537 , A61K31/55 , A61P35/00 , A61P31/18 , A61P37/02 , A61P35/04 , A61P29/00 , A61P19/02 , A61P27/02 , A61P11/00 , A61P37/06 , A61P43/00
CPC分类号： C07D471/10 , C07D233/16 , C07D233/84 , C07D233/90 , C07D401/14 , C07D403/12 , C07D403/14 , C07D487/10
摘要： The present invention relates to a compound represented by formula (I-0): wherein symbols in formula have the same meanings as described in the present specification, a salt thereof, an N-oxide thereof or a solvate thereof or a prodrug thereof, and medical use 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, rheumatoidarthritis, arthritis, retinopathy, 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, 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-0）表示的化合物：其中式中的符号与本说明书中所述的相同含义，其盐，其N-氧化物或其溶剂合物或其前药，以及医疗用途。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（例如类风湿关节炎，关节炎，视网膜病，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，代谢性疾病和癌性疾病（例如癌症，癌症转移等）或再生治疗剂。

10. 发明申请

US20100261641A1 SPIRO-PIPERIDINE COMPOUNDS AND MEDICINAL USE THEREOF 审中-公开
标题翻译：螺旋哌啶化合物及其药物用途
公开(公告)号：US20100261641A1
公开(公告)日：2010-10-14
申请号：US12332716
申请日：2008-12-11
申请人： Rena Nishizawa , Yoshikazu Takaoka , Hiromu Habashita , Shiro Shibayama , Masaya Kokubo
发明人： Rena Nishizawa , Yoshikazu Takaoka , Hiromu Habashita , Shiro Shibayama , Masaya Kokubo
IPC分类号： A61K38/17 , C07D487/10 , A61K31/551 , A61K31/69 , C07D498/10 , A61K31/553 , C07D221/20 , A61K31/438 , C07D471/10 , A61K31/499 , C07D285/16 , A61K31/549 , A61P31/18 , A61P13/12 , A61P9/10
CPC分类号： C07D471/10 , A61K31/438
摘要： The present invention relates to a spiro-piperidine compound represented by formula (I): wherein R1 represents hydrogen, an aliphatic hydrocarbon group which may have a substituent(s) or a cyclic group which may have a substituent(s); and ring A represents a 5- to 8-membered cyclic group which may have a substituent(s), a salt thereof, an N-oxide thereof, a quaternary ammonium salt thereof or a solvate thereof, or a prodrug thereof. The compounds represented by formula (I) have chemokine antagonistic action, so that they are useful for prevention and/or treatment of various inflammatory diseases, immune diseases such as autoimmune diseases or allergic diseases, or HIV infection.
摘要翻译：本发明涉及由式（I）表示的螺哌啶化合物：其中R1表示氢，可具有取代基的脂族烃基或可具有取代基的环状基团; 环A表示可具有取代基的5至8元环基，其盐，其N-氧化物，其季铵盐或其溶剂合物或其前药。由式（I）表示的化合物具有趋化因子拮抗作用，因此它们可用于预防和/或治疗各种炎性疾病，免疫疾病如自身免疫性疾病或过敏性疾病或HIV感染。

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