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    Chemokine receptor antagonist and medical use thereof
    1.
    发明授权
    Chemokine receptor antagonist and medical use thereof 失效
    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。

    Chemokine Receptor Antagonist and Medical Use Thereof
    2.
    发明申请
    Chemokine Receptor Antagonist and Medical Use Thereof 失效
    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。

    Spiroheterocyclic derivative compounds and drugs comprising the compound as the active ingredient
    3.
    发明申请
    Spiroheterocyclic derivative compounds and drugs comprising the compound as the active ingredient 审中-公开
    螺杂环衍生物化合物和包含该化合物作为活性成分的药物

    公开(公告)号：US20060019977A1

    公开(公告)日：2006-01-26

    申请号：US10531661

    申请日：2002-10-18

    申请人： Hiromu Habashita ,  Yoshikazu Takaoka ,  Shiro Shibayama

    发明人： Hiromu Habashita ,  Yoshikazu Takaoka ,  Shiro Shibayama

    IPC分类号： A61K31/4747 ,  C07D471/12

    CPC分类号： C07D471/20 ,  A61K31/527 ,  C07D495/20

    摘要： Spiroheterocyclic ring derivatives of the formula (I) (wherein R1 is H, alkyl, alkenyl, etc.; R2 is keto, thioketo, alkyl, etc.; R3 is alkyl, alkenyl, etc.; AB ring is fused bi-cyclic ring or spiro ring), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as an active ingredient. The compounds of the formula (I) regulate the effect of chemokine/chemokine receptor, they are used for prevention and treatment of various inflammatory diseases, allergic diseases, immunosuppression, cancer metastasis and acquired immune deficiency syndrome etc.

    摘要翻译： 式（I）（其中R 1是H，烷基，烯基等）的螺杂环衍生物; R 2是酮，硫代酮，烷基等; R 三环是烷基，烯基等; AB环是稠合的双环环或螺环），其季铵盐，其N-氧化物，其无毒盐或包含它们的药物组合物 ，作为活性成分。 式（I）化合物调节趋化因子/趋化因子受体的作用，用于预防和治疗各种炎性疾病，过敏性疾病，免疫抑制，癌症转移和获得性免疫缺陷综合征等。

    Nitrogen-containing heterocyclic compounds and medicinal use thereof
    7.
    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

    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。

    SPIROPIPERIDINE COMPOUND AND MEDICINAL USE THEREOF
    8.
    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

    申请人： Hiromu Habashita ,  Shiro Shibayama

    发明人： Hiromu Habashita ,  Shiro Shibayama

    IPC分类号： A61K31/499 ,  C07D471/10 ,  C07D221/20 ,  A61K31/438 ,  A61K31/527 ,  A61K31/56 ,  A61K39/00 ,  A61K38/43 ,  A61P37/06 ,  A61P37/00 ,  A61P37/08 ,  A61P1/00 ,  A61P11/00 ,  A61P19/02 ,  A61P25/00 ,  A61P17/06 ,  A61P3/10

    CPC分类号： A61K31/499 ,  A61K31/438 ,  A61K31/527 ,  C07D471/10

    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]。

    Nitrogen-containing heterocyclic compounds and medicinal use thereof
    9.
    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

    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。）

    Ccr4 antagonist and medical use thereof
    10.
    发明申请
    Ccr4 antagonist and medical use thereof 审中-公开
    Ccr4拮抗剂及其医疗用途

    公开(公告)号：US20060004010A1

    公开(公告)日：2006-01-05

    申请号：US10520660

    申请日：2003-07-08

    申请人： Hiromu Habashita ,  Masaya Kokubo ,  Shiro Shibayama ,  Hideaki Tada ,  Kenji Sagawa

    发明人： Hiromu Habashita ,  Masaya Kokubo ,  Shiro Shibayama ,  Hideaki Tada ,  Kenji Sagawa

    IPC分类号： A61K31/498 ,  C07D43/14

    CPC分类号： C07D409/12 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/498 ,  A61K31/506 ,  A61K31/55 ,  C07D241/22 ,  C07D241/26 ,  C07D241/44 ,  C07D401/12

    摘要： A compound of formula (I) or a salt thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound of formula (I) has CCR4 antagonistic activity, and therefore is useful as a preventive and/or therapeutic agent for diseases associated with CCR4, i.e., CCR4-mediated diseases such as inflammatory and/or allergic diseases [e.g., systemic inflammatory response syndrome (SIRS), anaphylaxis or anaphylaxis-like reaction, allergic vasculitis, reject reaction for graft organ, hepatitis, nephritis, nephrosis, pancreatitis, rhinitis, arthritis, inflammatory ocular diseases, inflammatory bowel diseases, diseases in cerebro and/or circulatory system, respiratory diseases, dermatic diseases, autoimmune diseases, etc.], and the like.

    摘要翻译： 式（I）化合物或其盐及其医疗用途（式中的符号如说明书中所述）。 式（I）化合物具有CCR4拮抗活性，因此可用作与CCR4相关的疾病的预防和/或治疗剂，即CCR4介导的疾病如炎性和/或过敏性疾病[例如全身炎症反应 综合征（SIRS），过敏反应或过敏反应，过敏性血管炎，移植器官排斥反应，肝炎，肾炎，肾病，胰腺炎，鼻炎，关节炎，炎性眼部疾病，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]等。