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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

US08748485B2 Compound and medical use thereof 有权
标题翻译：其复合和医疗用途
公开(公告)号：US08748485B2
公开(公告)日：2014-06-10
申请号：US13991025
申请日：2011-12-01
申请人： Masaya Kokubo , Koji Yano
发明人： Masaya Kokubo , Koji Yano
IPC分类号： A01N37/34 , A61K31/275 , A01N37/12 , A01N37/44 , A61K31/195 , C07C229/00 , A61K31/198 , C07C229/36
CPC分类号： C07C229/26 , A61K31/12 , A61K31/122 , A61K31/165 , A61K31/198 , A61K31/216 , A61K31/235 , A61K31/24 , A61K31/277 , A61K31/4412 , A61K45/06 , C07B2200/13 , C07C229/36 , A61K2300/00
摘要： Provided is a levodopa prodrug that overcomes the problems attributed to the blood kinetics of levodopa such as large number of doses and the incidence of side effects due to frequent dosing. (2S)-2-Amino-3-(3,4-bis((2-(benzoyloxy)-2-methylpropanoyl)oxy)phenyl)propanoic acid, a salt thereof, or a solvate thereof is a levodopa prodrug, and provides a flat blood concentration-time profile of levodopa through oral administration, and therefore is useful as a preventive and/or therapeutic agent for Parkinson's disease and/or Parkinson's syndrome that overcomes the problems associated with pharmaceutical preparations of levodopa.
摘要翻译：提供了左旋多巴前药，其克服了左旋多巴的血液动力学所引起的问题，例如大量的剂量以及由于频繁给药引起的副作用的发生率。（2S）-2-氨基-3-（3,4-双（（2-（苯甲酰氧基）-2-甲基丙酰基）氧基）苯基）丙酸，其盐或其溶剂合物是左旋多巴前药，并提供通过口服给药左旋多巴的平坦血液浓度 - 时间曲线，因此可用作克服与左旋多巴药物制剂相关的问题的帕金森病和/或帕金森综合征的预防和/或治疗剂。

3. 发明授权

US08618122B2 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基团的化合物及其用途
公开(公告)号：US08618122B2
公开(公告)日：2013-12-31
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： A61K31/44 , A61K31/415 , C07D215/00 , C07D233/00
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。

4. 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。

5. 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。

6. 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。

7. 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.

8. 发明授权

US08153625B2 Nitrogen-containing heterocyclic compounds and medicinal use thereof 失效
标题翻译：含氮杂环化合物及其医药用途
公开(公告)号：US08153625B2
公开(公告)日：2012-04-10
申请号：US12776989
申请日：2010-05-10
申请人： Hiromu Habashita , Masaya Kokubo , Shiro Shibayama , Hideaki Tada , Tatsuya Tanihiro
发明人： Hiromu Habashita , Masaya Kokubo , Shiro Shibayama , Hideaki Tada , Tatsuya Tanihiro
IPC分类号： A61K31/55 , C07D403/00
CPC分类号： C07D221/22 , C07D239/48 , C07D239/95 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D493/10
摘要： The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.).
摘要翻译：由式（I）和（II）表示的化合物，其盐，其N-氧化物或其溶剂合物或其前药及其药物组合物具有CXCR4调节作用，并且它们在治疗中有效预防各种炎症性疾病，各种过敏性疾病，人类免疫缺陷病毒的获得性免疫缺陷综合征感染或再生治疗药物。（其中环A表示可以具有取代基的含氮杂环基;环B表示可以具有取代基的杂环基或可以具有取代基的杂环基; Y表示可以具有取代基的烃基，可以具有取代基的杂环基，可被保护的氨基，可被保护的羟基或可被保护的巯基; T代表环A或可被保护的氨基。

9. 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。

10. 发明申请

US20070167459A1 Nitrogen-containing heterocyclic compounds and medicinal use thereof 失效
标题翻译：含氮杂环化合物及其医药用途
公开(公告)号：US20070167459A1
公开(公告)日：2007-07-19
申请号：US10538758
申请日：2003-12-09
申请人： Hiromu Habashita , Masaya Kokubo , Shiro Shibayama , Hideaki Tada , Tatsuya Tanihiro
发明人： Hiromu Habashita , Masaya Kokubo , Shiro Shibayama , Hideaki Tada , Tatsuya Tanihiro
IPC分类号： A61K31/519 , A61K31/517 , C07D403/02
CPC分类号： C07D221/22 , C07D239/48 , C07D239/95 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D493/10
摘要： The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.)
摘要翻译：由式（I）和（II）表示的化合物，其盐，其N-氧化物或其溶剂合物或其前药及其药物组合物具有CXCR4调节作用，并且它们在治疗中有效预防各种炎症性疾病，各种过敏性疾病，人类免疫缺陷病毒的获得性免疫缺陷综合征感染或再生治疗药物。（其中环A表示可以具有取代基的含氮杂环基;环B表示可以具有取代基的杂环基或可以具有取代基的杂环基; Y表示可以具有取代基的烃基，可以具有取代基的杂环基，可被保护的氨基，可被保护的羟基或可被保护的巯基; T代表环A或可被保护的氨基。）

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