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    Cyclic amine compounds as CCR5 antagonists
    1.
    发明授权
    Cyclic amine compounds as CCR5 antagonists 有权
    环胺化合物作为CCR5拮抗剂

    公开(公告)号：US07348324B2

    公开(公告)日：2008-03-25

    申请号：US10273111

    申请日：2002-10-18

    申请人： Shinichi Imamura ,  Shohei Hashiguchi ,  Taeko Hattori ,  Osamu Nishimura ,  Naoyuki Kanzaki ,  Masanori Baba ,  Yoshihiro Sugihara

    发明人： Shinichi Imamura ,  Shohei Hashiguchi ,  Taeko Hattori ,  Osamu Nishimura ,  Naoyuki Kanzaki ,  Masanori Baba ,  Yoshihiro Sugihara

    IPC分类号： A61P31/18 ,  A61K31/535 ,  A61K31/4965 ,  A61K31/44 ,  A61K31/47 ,  C07D413/00 ,  C07D241/00 ,  C07D211/00

    CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D211/62 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/14

    摘要： A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Y− (R5 is a hydrocarbon group; Y− is a counter anion); R3 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; R4 is a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; G1 is a bond, CO or SO2; G2 is CO, SO2, NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent C1-3 aliphatic hydrocarbon which may be substituted; provided that J is methine when G2 is OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when G1 is a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).

    摘要翻译： 式（I）化合物（其中R 1为氢原子，可被取代的烃基，可被取代的非芳香族杂环基，R 2 O 2 >可以被取代的烃基，可以被取代的非芳族杂环基，或者R 1和R 2可以彼此结合形成A至 形成可以被取代的杂环基; A是N或N + - - - - - - - （R 5） SUP>为烃基; Y为 - 抗衡阴离子）; R 3为可被取代的环状烃基或可被取代的杂环基; n 为0或1; R 4为氢原子，可被取代的烃基，可被取代的杂环基，可被取代的烷氧基，可被取代的芳氧基 ，或可以被取代的氨基，E是可以是二价脂族烃基 被除氧基以外的基团取代; G 1是一个键，CO或SO 2; G 2是CO，SO 2，NHCO，CONH或OCO; J为次甲基或氮原子; 并且Q和R中的每一个是可被取代的键或二价C 1-3烷基脂族烃; 条件是当G 2 O是OCO时J为次甲基，当另一个为键并且Q和R各自不被氧代基取代时，Q和R中的一个不为键， 当G 1是一个键时）或其盐具有强的CCR5拮抗活性，并且可以有利地用于治疗或预防人类各种HIV感染性疾病（如艾滋病）。

    Cyclic amine compounds as CCR5 antagonists
    2.
    发明授权
    Cyclic amine compounds as CCR5 antagonists 有权
    环胺化合物作为CCR5拮抗剂

    公开(公告)号：US06562978B1

    公开(公告)日：2003-05-13

    申请号：US10089374

    申请日：2002-03-29

    申请人： Shinichi Imamura ,  Shohei Hashiguchi ,  Taeko Hattori ,  Osamu Nishimura ,  Naoyuki Kanzaki ,  Masanori Baba ,  Yoshihiro Sugihara

    发明人： Shinichi Imamura ,  Shohei Hashiguchi ,  Taeko Hattori ,  Osamu Nishimura ,  Naoyuki Kanzaki ,  Masanori Baba ,  Yoshihiro Sugihara

    IPC分类号： C07D21128

    CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D211/62 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/14

    摘要： A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Y−(R5 is a hydrocarbon group; Y− is a counter anion); R3 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; R4 is a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; G1 is a bond, CO or SO2; G2 is CO, SO2, NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent C1-3 aliphatic hydrocarbon which may be substituted; provided that J is methine when G2 is OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when G1 is a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).

    摘要翻译： 式（I）的化合物（其中R 1为氢原子，可被取代的烃基，可被取代的非芳族杂环基，R 2为可被取代的烃基，非芳香族杂环基 或者R 1和R 2可以与A相互结合形成可被取代的杂环基; A是N或-N + -R 5 .Y-（R 5是烃基; Y-是抗衡阴离子 ）; R3是可以被取代的环状烃基或可以被取代的杂环基; n是0或1; R4是氢原子，可以被取代的烃基，可以被取代的杂环基， 可被取代的烷氧基，可被取代的芳氧基或可被取代的氨基，E是可被除氧以外的基团取代的二价脂族烃基; G 1是键，CO 或SO 2; G2是CO，SO 2，NHCO，CONH或OCO; J是次甲基或硝基 原子 Q和R分别为可以被取代的键或二价C 1-3脂族烃; 条件是当G2是OCO时J是次甲基，当另一个是键时Q和R中的一个不是键，并且当G 1是键时，Q和R各自不被氧代基取代）或 其盐具有有效的CCR5拮抗活性，可有利地用于治疗或预防人类各种HIV感染性疾病（如艾滋病）。

    Urea compounds, process for producing the same and use thereof
    3.
    发明授权
    Urea compounds, process for producing the same and use thereof 失效
    尿素化合物，其制造方法及其用途

    公开(公告)号：US06787650B1

    公开(公告)日：2004-09-07

    申请号：US10089961

    申请日：2002-04-05

    申请人： Osamu Kurasawa ,  Shinichi Imamura ,  Shohei Hashiguchi ,  Osamu Nishimura ,  Naoyuki Kanzaki ,  Masanori Baba

    发明人： Osamu Kurasawa ,  Shinichi Imamura ,  Shohei Hashiguchi ,  Osamu Nishimura ,  Naoyuki Kanzaki ,  Masanori Baba

    IPC分类号： C07D41700

    CPC分类号： C07D211/14

    摘要： A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.

    摘要翻译： 下式的化合物：其中R 1为可被取代的烃基; R 2为可被取代的环状烃基或可被取代的杂环基; R 3为卤素原子 ，可以被取代的氨基甲酰基，可以被取代的氨磺酰基，可以被取代的酰基，可以被取代的C1-4烷基，可被取代的C1-4烷氧基，氨基 其可以被取代，硝基或氰基; R 4是氢原子或羟基; n是0或1; 和p为0或1至4];或其盐具有有效的CCR5拮抗活性，并且可有利地用作抑制人外周血单核细胞的HIV感染的药物，特别是用于治疗或预防AIDS。

    Imidazopyridazine derivative having kinase inhibitory activity and pharmaceutical agent thereof
    5.
    发明授权
    Imidazopyridazine derivative having kinase inhibitory activity and pharmaceutical agent thereof 有权
    具有激酶抑制活性的咪唑并哒嗪衍生物及其药剂

    公开(公告)号：US08034812B2

    公开(公告)日：2011-10-11

    申请号：US12263884

    申请日：2008-11-03

    申请人： Nozomu Sakai ,  Shinichi Imamura ,  Naoki Miyamoto ,  Takaharu Hirayama

    发明人： Nozomu Sakai ,  Shinichi Imamura ,  Naoki Miyamoto ,  Takaharu Hirayama

    IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61P35/00

    CPC分类号： C07D487/04

    摘要： The present invention provides an imidazopyridazine derivative compound having a potent kinase inhibitory activity and a pharmaceutical agent thereof useful for treatment or prevention of cancer and the like. One such compound is represented by the formula: or a salt thereof or a prodrug thereof. The pharmaceutical agent contains the imidazopyridazine derivative compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor, or a cancer metastasis suppressor.

    摘要翻译： 本发明提供了可用于治疗或预防癌症等的具有强激酶抑制活性的咪唑并哒嗪衍生化合物及其药剂。 一种这样的化合物由下式表示：或其盐或其前药。 药剂含有作为激酶（VEGFR，VEGFR2，PDGFR，Raf）抑制剂，血管发生抑制剂，癌症预防或治疗剂，癌症生长抑制剂或癌症的咪唑并哒嗪衍生物化合物或其前药 转移抑制因子

    Fused heterocyclic derivative and use thereof
    6.
    发明授权
    Fused heterocyclic derivative and use thereof 有权
    熔融杂环衍生物及其用途

    公开(公告)号：US08044049B2

    公开(公告)日：2011-10-25

    申请号：US12064903

    申请日：2007-08-03

    申请人： Nozomu Sakai ,  Shinichi Imamura ,  Naoki Miyamoto ,  Takaharu Hirayama

    发明人： Nozomu Sakai ,  Shinichi Imamura ,  Naoki Miyamoto ,  Takaharu Hirayama

    IPC分类号： C07D487/04 ,  A61K31/5025 ,  A61P35/00

    CPC分类号： C07D487/04

    摘要： The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof.A compound represented by the formula (I): wherein each symbol is as defined in the specification, except a particular compound, or a salt thereof, and a pharmaceutical agent containing the compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor or a cancer metastasis suppressor.

    摘要翻译： 本发明提供具有强激酶抑制活性的稠合杂环衍生物及其应用。 由式（I）表示的化合物：其中每个符号如说明书中所定义，除了特定化合物或其盐，以及含有作为激酶的化合物或其前药的药物（VEGFR，VEGFR2 ，PDGFR，Raf）抑制剂，血管发生抑制剂，用于预防或治疗癌症的药物，癌症生长抑制剂或癌症转移抑制剂。

    Carbapenem compound, their production and use
    8.
    发明授权
    Carbapenem compound, their production and use 失效
    碳青霉烯化合物，其生产和使用

    公开(公告)号：US06174877B1

    公开(公告)日：2001-01-16

    申请号：US09101470

    申请日：1998-07-10

    申请人： Yukio Ishibashi ,  Shinichi Imamura ,  Tetsuo Miwa

    发明人： Yukio Ishibashi ,  Shinichi Imamura ,  Tetsuo Miwa

    IPC分类号： A61K3140

    CPC分类号： C07D477/20

    摘要： A cephem compound of the formula: wherein R1 stands for an optionally substituted lower alkyl group, R2 stands for H or a lower alkyl group, R3 stands for H, an optionally substituted hydrocarbon group, cyano group, a lower alkyloxy group or a lower alkylthio group, and the ring A stands for an optionally substituted non-quaternarized nitrogen-containing heterocyclic ring, provided that, when A is unsubstituted 2-pyridyl group, R3 stands for a group other than hydrogen, or their esters or salts, has excellent antibacterial activities, oral absorbability and stability, and is useful as an antibacterial agent.

    摘要翻译： 下式的头孢烯化合物：其中R1代表任意取代的低级烷基，R2代表H或低级烷基，R3代表H，任意取代的烃基，氰基，低级烷氧基或低级烷硫基 并且环A代表任选取代的非季铵化含氮杂环，条件是当A是未取代的2-吡啶基时，R 3代表氢以外的基团或其酯或盐，具有优异的抗菌性 活性，口服吸收性和稳定性，可用作抗菌剂。

    Fused heterocycle derivatives and use thereof
    10.
    发明授权
    Fused heterocycle derivatives and use thereof 有权
    稠合杂环衍生物及其用途

    公开(公告)号：US08304557B2

    公开(公告)日：2012-11-06

    申请号：US12133063

    申请日：2008-06-04

    申请人： Yuya Oguro ,  Shinichi Imamura

    发明人： Yuya Oguro ,  Shinichi Imamura

    IPC分类号： C07D277/62 ,  A61K31/428

    CPC分类号： C07D471/04 ,  C07D417/12 ,  C07D471/14 ,  C07D513/04

    摘要： A compound represented by the formula (I): wherein Z1, Z2, Z3 and Z4 are the following combination, (Z1,Z2,Z3,Z4)=(CR4,N,CR5,C), (N,N,CR5,C), (N,C,CR5,N), (S,C,CR5,C) or (S,C,N,C); R1 and R2 are the same or different and each is (1) a hydrogen atom, (2) a halogen atom, (3) a group bonded via a carbon atom, (4) a group bonded via a nitrogen atom, (5) a group bonded via an oxygen atom or (6) a group bonded via a sulfur atom; R3 is an amino optionally having substituent(s); R4 and R5 are the same or different and each is (1) a hydrogen atom, (2) a halogen atom, (3) a group bonded via a carbon atom, (4) a group bonded via a nitrogen atom, (5) a group bonded via an oxygen atom or (6) a group bonded via a sulfur atom; R3 and R4 optionally form a ring optionally having substituent(s); and a group represented by the formula is a cyclic group optionally having substituent(s), or a salt thereof.

    摘要翻译： 由式（I）表示的化合物：其中Z 1，Z 2，Z 3和Z 4是以下组合：（Z 1，Z 2，Z 3，Z 4）=（CR 4，N，CR 5，C），（N，N， C），（N，C，CR5，N），（S，C，CR5，C）或（S，C，N，C） R1和R2相同或不同，分别为（1）氢原子，（2）卤素原子，（3）通过碳原子键合的基团，（4）通过氮原子键合的基团，（5） 通过氧原子键合的基团或（6）通过硫原子键合的基团; R3是任选具有取代基的氨基; R4和R5相同或不同，分别为（1）氢原子，（2）卤素原子，（3）通过碳原子键合的基团，（4）通过氮原子键合的基团，（5） 通过氧原子键合的基团或（6）通过硫原子键合的基团; R3和R4任选地形成任选具有取代基的环; 并且由下式表示的基团是任选具有取代基的环状基团或其盐。