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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. 发明授权

US07875745B2 Compounds having lysophosphatidic acid receptor antagonism and uses thereof 有权
标题翻译：具有溶血磷脂酸受体拮抗作用的化合物及其用途
公开(公告)号：US07875745B2
公开(公告)日：2011-01-25
申请号：US10583469
申请日：2004-12-17
申请人： Motoyuki Tanaka , Shinji Nakade , Yoshikazu Takaoka
发明人： Motoyuki Tanaka , Shinji Nakade , Yoshikazu Takaoka
IPC分类号： C07C53/134 , A61K31/19
CPC分类号： C07D231/12 , C07C59/66 , C07C69/734 , C07C69/92 , C07D207/337 , C07D261/08 , C07D403/06 , C07D409/06 , C07D417/12
摘要： The present invention relates to a compound represented by formula (I): (wherein the symbols in formula were described in the description), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention binds to and is antagonistic to an LPA receptor (particularly, EDG-2), it is useful for prevention and/or treatment of urinary system disease (prostatic hypertrophy or neurogenic bladder dysfunction disease, spinal cord neoplasm, nucleous hernia, spinal canal stenosis, diseases caused by diabetes, occlusion disease of lower urinary tract, inflammatory disease of lower urinary tract, and polyuria), carcinoma-associated disease, proliferative disease, inflammation system disease, immune system disease, disease by secretory dysfunction, brain-related disease and/or chronic disease.
摘要翻译：本发明涉及由式（I）表示的化合物：其中式中的符号在描述中描述），其盐，其溶剂化物或其前药。由于本发明的化合物与LPA受体（特别是EDG-2）结合并拮抗，因此可用于预防和/或治疗泌尿系统疾病（前列腺肥大或神经源性膀胱功能障碍性疾病，脊髓肿瘤，核疝，椎管狭窄，糖尿病引起的疾病，下尿路闭塞性疾病，下尿路炎症和多尿症），癌相关疾病，增殖性疾病，炎症系统疾病，免疫系统疾病，分泌功能障碍脑相关疾病和/或慢性疾病。

7. 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。

8. 发明申请

US20060148830A1 Lpa receptor antagonist 有权
标题翻译： Lpa受体拮抗剂
公开(公告)号：US20060148830A1
公开(公告)日：2006-07-06
申请号：US10530249
申请日：2003-05-28
申请人： Masahiko Terakado , Shinji Nakade , Takuya Seko , Yoshikazu Takaoka
发明人： Masahiko Terakado , Shinji Nakade , Takuya Seko , Yoshikazu Takaoka
IPC分类号： A61K31/519 , A61K31/517 , C07D487/02 , C07D403/02
CPC分类号： C07D211/96 , C07C217/58 , C07C233/22 , C07C233/51 , C07C233/63 , C07C233/73 , C07C233/87 , C07C235/34 , C07C235/48 , C07C235/52 , C07C2601/08 , C07D207/12 , C07D207/327 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/46 , C07D213/65 , C07D213/89 , C07D217/06 , C07D231/12 , C07D231/14 , C07D235/12 , C07D239/91 , C07D257/04 , C07D277/36 , C07D277/56 , C07D279/08 , C07D307/68 , C07D317/68 , C07D333/70
摘要： A compound of the general formula (I): (wherein the symbols are as defined in the description), or a non-toxic salt thereof. This compound engages in LPA receptor bonding and antagonism and hence is useful in the prevention and/or treatment of urinary system disease (symptom with prostatic hypertrophy or neurogenic bladder dysfunction disease, symptom to be caused by spinal cord neoplasm, nucleous hernia, spinal canal stenosis or diabetes, occlusion disease of lower urinary tract, inflammatory disease of lower urinary tract, polyuria), carcinoma-associated disease (solid tumor, solid tumor metastasis, angiofibroma, myeloma, multiple myeloma, Kaposi's sarcoma, leucemia and carcinomatous infiltration transition), proliferative disease (disorder with aberrant angiogenesis, artery obstruction and pulmonary fibrosis), inflammation/immune system disease (psoriasis, nephropathy, hepatitis and pneumonitis symptom), disease caused by secretory dysfunction (Sjogren syndrome), brain-related disease (brain infarction, cerebral apoplexy and brain or peripheral neuropathy) or chronic disease (chronic asthma, glomerulonephritis, obesity, prostate hyperplasia, diseases caused by arteriosclerosis process, rheumatism or atopic dermatitis).
摘要翻译：通式（I）的化合物或其无毒盐，其中符号如说明书中所定义。该化合物参与LPA受体结合和拮抗作用，因此可用于预防和/或治疗泌尿系统疾病（前列腺肥大或神经源性膀胱功能障碍症状，由脊髓肿瘤引起的症状，核疝，椎管狭窄或糖尿病，下尿路闭塞性疾病，下尿路炎症，多尿症），癌相关疾病（实体瘤，实体瘤转移，血管纤维瘤，骨髓瘤，多发性骨髓瘤，卡波西肉瘤，乳腺癌和癌性浸润转换），增殖性疾病（异常血管生成障碍，动脉阻塞和肺纤维化），炎症/免疫系统疾病（牛皮癣，肾病，肝炎和肺炎症状），由分泌功能障碍（干燥综合征）引起的疾病，脑相关疾病（脑梗塞，脑中风和脑或周围神经病）或慢性疾病（慢性哮喘，肾小球肾炎）腹泻，肥胖，前列腺增生，由动脉硬化过程引起的疾病，风湿病或特应性皮炎）。

9. 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。

10. 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。

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