Use of an efficacy marker for optimizing therapeutic efficacy of an anti-human PD-1 antibody on cancers
    11.
    发明授权
    Use of an efficacy marker for optimizing therapeutic efficacy of an anti-human PD-1 antibody on cancers 有权
    使用功效标记来优化抗人PD-1抗体对癌症的治疗功效

    公开(公告)号:US08460886B2

    公开(公告)日:2013-06-11

    申请号:US13001875

    申请日:2009-07-03

    IPC分类号: G01N33/53 A61K39/395

    摘要: A purpose of the present invention is to provide a method capable of more effectively prescribing an anti-human PD-1 antibody for anti-cancer therapy, a method for estimating or optimizing therapeutic efficacy thereof, and further an efficacy marker that can be used in methods thereof. The present invention enables selection of the cancer patient in whom the therapeutic efficacy of the anti-human PD-1 antibody can be expected in future, by measuring the change which is more than a certain level of several kinds of efficacy markers in blood, after administering the initial dose or doses of the anti-human PD-1 antibody compared to that prior to administering the initial dose, and provides a new prescription of the anti-human PD-1 antibody for anti-cancer therapy.

    摘要翻译: 本发明的目的是提供一种能够更有效地制备用于抗癌治疗的抗人PD-1抗体的方法,用于估计或优化其治疗功效的方法,以及可用于 方法。 本发明能够通过在血液中测定超过一定水平的几种功效标志物的变化,能够选择将来能够预期抗人PD-1抗体的治疗功效的癌症患者 与施用初始剂量之前相比,施用抗人PD-1抗体的初始剂量或剂量,并且提供了用于抗癌治疗的抗人PD-1抗体的新处方。

    Chemokine receptor antagonists and use thereof
    13.
    发明授权
    Chemokine receptor antagonists and use thereof 有权
    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

    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.

    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。

    Chemokine receptor antagonists and use thereof

    公开(公告)号:US08293896B2

    公开(公告)日:2012-10-23

    申请号:US12091403

    申请日:2006-10-27

    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.

    Nitrogen-containing heterocyclic compounds and medicinal use thereof
    15.
    发明授权
    Nitrogen-containing heterocyclic compounds and medicinal use thereof 失效
    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

    IPC分类号: A61K31/55 C07D403/00

    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。

    SPIROPIPERIDINE COMPOUND AND MEDICINAL USE THEREOF
    17.
    发明申请
    SPIROPIPERIDINE COMPOUND AND MEDICINAL USE THEREOF 审中-公开
    螺吡啶化合物及其药物用途

    公开(公告)号:US20110052612A1

    公开(公告)日:2011-03-03

    申请号:US11916040

    申请日:2006-05-30

    摘要: The present invention relates to a CXCR3 antagonist comprising a compound represented by formula (I) (wherein all the symbols have the same meaning as defined in the description),a salt thereof, a quaternary ammonium salt thereof, an N-oxide form thereof or a solvate thereof, or a prodrug thereof.This antagonist is useful as a preventive, therapeutic and/or progression-suppressing agent for a CXCR3-mediated disease such as an immune or an allergic disease [e.g., an atopic disease, an autoimmune disease (e.g., multiple sclerosis, rheumatoid arthritis, systemic lupus erythematosus, type I diabetes, glomerulonephritis, Sjogren's syndrome and the like), systemic inflammatory response syndrome (SIRS), a rejection response to transplanted organ, tissue and/or cell or the like], a gastrointestinal disease [e.g., an inflammatory bowel disease or the like], or a respiratory disease [e.g., asthma, a chronic obstructive pulmonary disease or the like].

    摘要翻译: 本发明涉及包含由式(I)表示的化合物(其中所有符号具有与说明书中定义相同的含义)的CXCR3拮抗剂,其盐,其季铵盐,其N-氧化物形式或 其溶剂合物或其前药。 该拮抗剂可用作CXCR3介导的疾病如免疫或过敏性疾病[例如特应性疾病,自身免疫疾病(例如多发性硬化症,类风湿性关节炎,系统性的)的预防,治疗和/或进展抑制剂 红斑狼疮,I型糖尿病,肾小球肾炎,干燥综合征等),全身炎症反应综合征(SIRS),移植器官,组织和/或细胞等的排斥反应],胃肠疾病[例如炎性肠 疾病等]或呼吸系统疾病[例如哮喘,慢性阻塞性肺病等]。

    COMPOUND CONTAINING BASIC GROUP AND USE THEREOF
    18.
    发明申请
    COMPOUND CONTAINING BASIC GROUP AND USE THEREOF 有权
    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

    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。

    Nitrogen-containing heterocyclic compounds and medicinal use thereof
    19.
    发明申请
    Nitrogen-containing heterocyclic compounds and medicinal use thereof 失效
    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

    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。)

    Multimer of extracellular domain of cell surface functional molecule
    20.
    发明授权
    Multimer of extracellular domain of cell surface functional molecule 有权
    细胞表面功能分子细胞外结构域的多聚体

    公开(公告)号:US08574872B2

    公开(公告)日:2013-11-05

    申请号:US13486189

    申请日:2012-06-01

    IPC分类号: C12P21/04 C07K14/00

    摘要: As a substance which pharmacologically regulates the function of a cell surface functional molecule, a substance which has specificity and an activity or efficacy equal or superior to an antibody and does not require an advanced production technique and facility for application thereof to a pharmaceutical product has been demanded. The invention relates to a multimer of an extracellular domain of a cell surface functional molecule, particularly a tetramer of an extracellular domain of PD-1 or PD-L1. Further, the invention relates to an application of such a tetramer as a preventive and/or therapeutic agent for cancer, cancer metastasis, immunodeficiency, an infectious disease or the like and an application of PD-1 or PD-L1 as a testing or diagnostic agent or a research agent for such a disease.

    摘要翻译: 作为药理学上调节细胞表面功能分子的功能的物质,具有特异性,活性或功效等同于或优于抗体且不需要先进的生产技术的物质及其应用于药物的设备已经被 要求 本发明涉及细胞表面功能分子的细胞外结构域的多聚体,特别是PD-1或PD-L1细胞外结构域的四聚体。 此外,本发明涉及这样的四聚体作为癌症,癌症转移,免疫缺陷,感染性疾病等的预防和/或治疗剂的应用,以及应用PD-1或PD-L1作为检测或诊断 代理人或这种疾病的研究代理人。