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    Glycopeptide Antibiotic Monomer Derivatives
    2.
    发明申请
    Glycopeptide Antibiotic Monomer Derivatives 失效
    糖肽抗生素单体衍生物

    公开(公告)号：US20080097078A1

    公开(公告)日：2008-04-24

    申请号：US11791446

    申请日：2005-11-24

    申请人： Hirokazu Arimoto ,  Jun Lu ,  Yoshinori Yamano ,  Tatsuro Yasukata ,  Osamu Yoshida ,  Tsutomu Iwaki ,  Yutaka Yoshida ,  Issei Kato ,  Kenji Morimoto ,  Kayo Yasoshima

    发明人： Hirokazu Arimoto ,  Jun Lu ,  Yoshinori Yamano ,  Tatsuro Yasukata ,  Osamu Yoshida ,  Tsutomu Iwaki ,  Yutaka Yoshida ,  Issei Kato ,  Kenji Morimoto ,  Kayo Yasoshima

    IPC分类号： C07K7/64 ,  C07K5/12

    CPC分类号： C07K9/008 ,  A61K38/00 ,  A61K38/04

    摘要： Novel glycopeptide antibiotic derivatives. These derivatives are represented by the formula (aglycon part of glycopeptide antibiotic derivative)-(Sac-NH)—RA [wherein (aglycon part of glycopeptide antibiotic derivative) is the part formed by removing the sugar part from a known glycopeptide antibiotic derivative; (Sac-NH) part is an amino sugar part or a sugar chain part containing an amino sugar; and RA represents, e.g., the formula —X1—Ar1—X2—Y—X3—Ar2 (wherein X1, X2, and X3 each represents 1) a single bond or 2) a heteroatom or heteroatom-containing group selected from the group consisting of —N═, ═N—, —NR1—, —O—, etc.; Y represents —NR2CO— or —CONR2— (wherein R2 represents hydrogen or lower alkyl), etc.)]. These derivatives have antibacterial activity against vancomycin-resistant bacteria.

    摘要翻译： 新型糖肽抗生素衍生物。 这些衍生物由式（糖肽抗生素衍生物的糖苷配基部分） - （Sac-NH）-R A表示[其中（糖肽抗生素衍生物的糖苷配基部分）是通过除去糖部分而形成的部分 从已知的糖肽抗生素衍生物; （Sac-NH）部分是含有氨基糖的氨基糖部分或糖链部分; 并且R A表示例如式-X 1 -Ar 1 -x 2 -YX SUP >其中X 1，X 2和X 3各自表示 1）单键或2）选自-N-，-N-，-NR 1 - ， - O - 等的杂原子或含杂原子的基团; Y表示-NR 2 CO-或-CONR 2 - （其中R 2表示氢或低级烷基）等）。 这些衍生物对万古霉素抗性细菌具有抗菌活性。

    Fused azole-pyrimidine derivatives
    3.
    发明授权
    Fused azole-pyrimidine derivatives 有权
    熔融唑 - 嘧啶衍生物

    公开(公告)号：US07511041B2

    公开(公告)日：2009-03-31

    申请号：US10527376

    申请日：2003-09-18

    申请人： Mitsuyuki Shimada ,  Toshiki Murata ,  Kinji Fuchikami ,  Hideki Tsujishita ,  Naoki Omori ,  Issei Kato ,  Mami Miura ,  Klaus Urbahns ,  Florian Gantner ,  Kevin Bacon

    发明人： Mitsuyuki Shimada ,  Toshiki Murata ,  Kinji Fuchikami ,  Hideki Tsujishita ,  Naoki Omori ,  Issei Kato ,  Mami Miura ,  Klaus Urbahns ,  Florian Gantner ,  Kevin Bacon

    IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D237/26 ,  C07D237/36 ,  C07D241/36 ,  C07D239/00 ,  C07D471/00 ,  C07D471/04 ,  C07D401/04 ,  C07D401/22 ,  C07D487/00 ,  C07D487/04 ,  C07D491/00 ,  C07D495/00 ,  C07D497/00

    CPC分类号： C07D471/14 ,  C07D487/04

    摘要： The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoixnmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis. The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.

    摘要翻译： 本发明涉及霍夫唑唑吡啶衍生物，其制备方法和含有它们的药物制剂。 本发明的稠合吡唑嘧啶衍生物对于磷脂酰肌醇-3-激酶（PI3K）抑制的效力显着增强，特别是对于PI3K-γ抑制，可用于预防和治疗与PI3K相关的疾病，特别是PI3K-γ活性。 更具体地说，本发明的唑类衍生物可用于治疗和预防以下疾病：炎性和免疫调节性疾病，如哮喘，特应性皮炎，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），脓毒性休克，关节 疾病，自身免疫性疾病如类风湿性关节炎，格雷夫斯病，癌症，心肌收缩性疾病，心力衰竭，血栓栓塞，缺血和动脉粥样硬化。 本发明的化合物还可用于肺动脉高压，肾衰竭，心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病，糖尿病和局灶性缺血，因为这些疾病还涉及人或动物中的PI3K活性 学科。

    Glycopeptide antibiotic monomer derivatives
    5.
    发明授权
    Glycopeptide antibiotic monomer derivatives 失效
    糖肽抗生素单体衍生物

    公开(公告)号：US08778874B2

    公开(公告)日：2014-07-15

    申请号：US11791446

    申请日：2005-11-24

    申请人： Hirokazu Arimoto ,  Jun Lu ,  Yoshinori Yamano ,  Tatsuro Yasukata ,  Osamu Yoshida ,  Tsutomu Iwaki ,  Yutaka Yoshida ,  Issei Kato ,  Kenji Morimoto ,  Kayo Yasoshima

    发明人： Hirokazu Arimoto ,  Jun Lu ,  Yoshinori Yamano ,  Tatsuro Yasukata ,  Osamu Yoshida ,  Tsutomu Iwaki ,  Yutaka Yoshida ,  Issei Kato ,  Kenji Morimoto ,  Kayo Yasoshima

    IPC分类号： A61K38/00 ,  A61P31/04 ,  A61K38/14 ,  C07K9/00 ,  A61K38/04

    CPC分类号： C07K9/008 ,  A61K38/00 ,  A61K38/04

    摘要： Novel glycopeptide antibiotic derivatives. These derivatives are represented by the formula (aglycon part of glycopeptide antibiotic derivative)-(Sac-NH)—RA [wherein (aglycon part of glycopeptide antibiotic derivative) is the part formed by removing the sugar part from a known glycopeptide antibiotic derivative; (Sac-NH) part is an amino sugar part or a sugar chain part containing an amino sugar; and RA represents, e.g., the formula —X1—Ar1—X2—Y—X3—Ar2 (wherein X1, X2, and X3 each represents 1) a single bond or 2) a heteroatom or heteroatom-containing group selected from the group consisting of —N═, ═N—, —NR1—, —O—, etc.; Y represents —NR2CO— or —CONR2— (wherein R2 represents hydrogen or lower alkyl), etc.)]. These derivatives have antibacterial activity against vancomycin-resistant bacteria.

    摘要翻译： 新型糖肽抗生素衍生物。 这些衍生物由式（糖肽抗生素衍生物的糖苷配基） - （Sac-NH）-RA [其中（糖肽抗生素衍生物的糖苷配基部分）是通过从已知的糖肽抗生素衍生物中除去糖部分而形成的部分） （Sac-NH）部分是含有氨基糖的氨基糖部分或糖链部分; RA表示例如式-X1-Ar1-X2-Y-X3-Ar2（其中X1，X2和X3各自表示1）单键或2）选自以下的杂原子或含杂原子的基团： 的-N =，-N =，-NR1-，-O-等; Y表示-NR2CO-或-CONR2-（其中R2表示氢或低级烷基）等）。 这些衍生物对万古霉素抗性细菌具有抗菌活性。

    Glycopeptide antibiotic derivative
    6.
    发明授权
    Glycopeptide antibiotic derivative 有权
    糖肽抗生素衍生物

    公开(公告)号：US08933012B2

    公开(公告)日：2015-01-13

    申请号：US12224443

    申请日：2007-05-25

    申请人： Yasuhiro Nishitani ,  Osamu Yoshida ,  Tsutomu Iwaki ,  Issei Kato

    发明人： Yasuhiro Nishitani ,  Osamu Yoshida ,  Tsutomu Iwaki ,  Issei Kato

    IPC分类号： A61K38/00 ,  A61P31/04 ,  A01N43/40 ,  A61K31/445 ,  C07K9/00 ,  A61K38/04

    CPC分类号： C07K9/008 ,  A61K38/00 ,  A61K38/04

    摘要： The present invention provides a novel glycopeptide antibiotic derivative.These derivatives are represented by the formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein RA is —X1—Ar1—X2—Y—X3—Ar2 wherein X1, X2 and X3 are single bond; heteroatom-containing group selected from the group consisting of —N═, ═N—, —NR1— (R1 is hydrogen or lower alkyl), —O—, —S—, —SO— and —SO2—, or a linkage thereof; or alkylene or alkenylene optionally substituted and optionally interrupted by one or more of said heteroatom-containing group; Y is —NR2CO—, —CONR2— (R2 is hydrogen or lower alkyl), or a group of the formula (II) wherein R3 is alkylene; Ar1 and Ar2 are a carbocycle or a heterocycle which is optionally substituted and may have an unsaturated bond; RB is —NHNRXRY or —NRZORW wherein RX is hydrogen or lower alkyl; RY is hydrogen, optionally substituted lower alkyl, C(═NH)NH2, CSNH2, COCONH2, CN, optionally substituted heterocyclic group, and optionally substituted carbamoyl; RZ is hydrogen or lower alkyl; RW is hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted heterocyclic group, optionally substituted heterocyclic carbonyl or optionally substituted carbamoyl; RC is hydrogen or optionally substituted alkyl, wherein said alkyl may be interrupted by a heteroatom-containing group selected from N═, ═N—, —NR1— (R1 is hydrogen or lower alkyl), —O—, —S—, —SO— and —SO2—; and R is optionally substituted alkyl.

    摘要翻译： 本发明提供了一种新型糖肽抗生素衍生物。 这些衍生物由式（I）表示或其药学上可接受的盐或溶剂化物，其中RA为-X1-Ar1-X2-Y-X3-Ar2，其中X1，X2和X3为单键; 选自-N =，N-，-NR1-（R 1为氢或低级烷基）， - O - ， - S - ， - SO-和-SO 2 - 的杂原子的基团，或其连接基 ; 或任选被取代并任选被一个或多个所述含杂原子基团中断的亚烷基或亚烯基; Y是-NR 2 CO-，-CONR 2 - （R 2是氢或低级烷基）或式（II）的基团，其中R 3是亚烷基; Ar1和Ar2是任选被取代并可具有不饱和键的碳环或杂环; RB是-NHNRXRY或-NRZORW，其中RX是氢或低级烷基; RY是氢，任选取代的低级烷基，C（= NH）NH 2，CSNH 2，COCONH 2，CN，任选取代的杂环基和任选取代的氨基甲酰基; RZ是氢或低级烷基; RW是氢，任选取代的低级烷基，任选取代的低级烯基，任选取代的杂环基，任选取代的杂环羰基或任选取代的氨基甲酰基; RC是氢或任选取代的烷基，其中所述烷基可以被选自N =，N-，-NR1-（R 1是氢或低级烷基），-O - ， - S - ， - SO-和-SO 2 - ; R是任选取代的烷基。

    Fused azole-pyrimidine derivatives
    8.
    发明授权
    Fused azole-pyrimidine derivatives 有权
    熔融唑 - 嘧啶衍生物

    公开(公告)号：US08129386B2

    公开(公告)日：2012-03-06

    申请号：US12414257

    申请日：2009-03-30

    申请人： Mitsuyuki Shimada ,  Toshiki Murata ,  Kinji Fuchikami ,  Hideki Jishita ,  Naoki Omori ,  Issei Kato ,  Mami Miura ,  Klaus Urbahns ,  Florian Gantner ,  Kevin Bacon

    发明人： Mitsuyuki Shimada ,  Toshiki Murata ,  Kinji Fuchikami ,  Hideki Jishita ,  Naoki Omori ,  Issei Kato ,  Mami Miura ,  Klaus Urbahns ,  Florian Gantner ,  Kevin Bacon

    IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495

    CPC分类号： C07D471/14 ,  C07D487/04

    摘要： The present invention relates to novel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity.More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis.The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.

    摘要翻译： 本发明涉及新型稠合吡唑嘧啶衍生物，其制备方法和含有它们的药物制剂。 本发明的稠合唑类嘧啶衍生物对磷脂酰肌醇-3-激酶（PI3K）抑制的效力显着增强，特别是PI3K-γ抑制作用，可用于预防和治疗与PI3K相关的疾病，特别是PI3K-γ活性。 更具体地说，本发明的唑类衍生物可用于治疗和预防以下疾病：炎性和免疫调节性疾病，如哮喘，特应性皮炎，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），脓毒性休克，关节 疾病，自身免疫疾病如类风湿性关节炎，格雷夫斯病，癌症，心肌收缩性疾病，心力衰竭，血栓栓塞，缺血和动脉粥样硬化。 本发明的化合物还可用于肺动脉高压，肾衰竭，心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病，糖尿病和局灶性缺血，因为这些疾病还涉及人或动物中的PI3K活性 学科。

    Glycopeptide Antibiotic Derivative
    9.
    发明申请
    Glycopeptide Antibiotic Derivative 有权
    糖肽抗生素衍生物

    公开(公告)号：US20090286717A1

    公开(公告)日：2009-11-19

    申请号：US12224443

    申请日：2007-05-25

    申请人： Yasuhiro Nishitani ,  Osamu Yoshida ,  Tsutomu Iwaki ,  Issei Kato

    发明人： Yasuhiro Nishitani ,  Osamu Yoshida ,  Tsutomu Iwaki ,  Issei Kato

    IPC分类号： A61K38/00 ,  C07K9/00 ,  A61P43/00

    CPC分类号： C07K9/008 ,  A61K38/00 ,  A61K38/04

    摘要： The present invention provides a novel glycopeptide antibiotic derivative.These derivatives are represented by the formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein RA is —X1—Ar1—X2—Y—X3—Ar2 wherein X1, X2 and X3 are single bond; heteroatom-containing group selected from the group consisting of —N═, ═N—, —NR1— (R1 is hydrogen or lower alkyl), —O—, —S—, —SO— and —SO2—, or a linkage thereof; or alkylene or alkenylene optionally substituted and optionally interrupted by one or more of said heteroatom-containing group; Y is —NR2CO—, —CONR2— (R2 is hydrogen or lower alkyl), or a group of the formula (II) wherein R3 is alkylene; Ar1 and Ar2 are a carbocycle or a heterocycle which is optionally substituted and may have an unsaturated bond; RB is —NHNRXRY or —NRZORW wherein RX is hydrogen or lower alkyl; RY is hydrogen, optionally substituted lower alkyl, C(═NH)NH2, CSNH2, COCONH2, CN, optionally substituted heterocyclic group, and optionally substituted carbamoyl; RZ is hydrogen or lower alkyl; RW is hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted heterocyclic group, optionally substituted heterocyclic carbonyl or optionally substituted carbamoyl; RC is hydrogen or optionally substituted alkyl, wherein said alkyl may be interrupted by a heteroatom-containing group selected from N═, ═N—, —NR1— (R1 is hydrogen or lower alkyl), —O—, —S—, —SO— and —SO2—; and R is optionally substituted alkyl.

    摘要翻译： 本发明提供了一种新型糖肽抗生素衍生物。 这些衍生物由式（I）表示或其药学上可接受的盐或溶剂化物，其中RA为-X1-Ar1-X2-Y-X3-Ar2，其中X1，X2和X3为单键; 选自-N-，-N-，-NR1-（R 1为氢或低级烷基）， - ， - - ， - S - ， - SO - 和-SO 2 - 或其连接基团 ; 或任选被取代并任选被一个或多个所述含杂原子基团中断的亚烷基或亚烯基; Y是-NR 2 CO-，-CONR 2 - （R 2是氢或低级烷基）或式（II）的基团，其中R 3是亚烷基; Ar1和Ar2是任选被取代并可具有不饱和键的碳环或杂环; RB是-NHNRXRY或-NRZORW，其中RX是氢或低级烷基; RY是氢，任选取代的低级烷基，C（-NH）NH 2，CSNH 2，COCONH 2，CN，任选取代的杂环基和任选取代的氨基甲酰基; RZ是氢或低级烷基; RW是氢，任选取代的低级烷基，任选取代的低级烯基，任选取代的杂环基，任选取代的杂环羰基或任选取代的氨基甲酰基; RC是氢或任选取代的烷基，其中所述烷基可以被选自N-，-N-，-NR1-（R 1是氢或低级烷基），-O - ， - S - ， - SO-和-SO 2 - ; R是任选取代的烷基。

    FUSED AZOLE-PYRIMIDINE DERIVATIVES
    10.
    发明申请
    FUSED AZOLE-PYRIMIDINE DERIVATIVES 有权
    熔融的偶氮吡啶衍生物

    公开(公告)号：US20090270388A1

    公开(公告)日：2009-10-29

    申请号：US12414257

    申请日：2009-03-30

    申请人： Mitsuyuki Shimada ,  Toshiki Murata ,  Kinji Fuchikami ,  Hideki Tsujishita ,  Naoki Omori ,  Issei Kato ,  Mami Miura ,  Klaus Urbahns ,  Florian Gantner ,  Kevin Bacon

    发明人： Mitsuyuki Shimada ,  Toshiki Murata ,  Kinji Fuchikami ,  Hideki Tsujishita ,  Naoki Omori ,  Issei Kato ,  Mami Miura ,  Klaus Urbahns ,  Florian Gantner ,  Kevin Bacon

    IPC分类号： A61K31/519 ,  C07D487/04 ,  A61K31/5377 ,  A61P29/00 ,  A61P37/00 ,  A61P3/10 ,  A61P35/00

    CPC分类号： C07D471/14 ,  C07D487/04

    摘要： The present invention relates to novel fused azolepyriimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity.More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis.The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.

    摘要翻译： 本发明涉及新的稠合唑吡喃衍生物，其制备方法和含有它们的药物制剂。 本发明的稠合吡唑嘧啶衍生物对于磷脂酰肌醇-3-激酶（PI3K）抑制的效力显着增强，特别是对于PI3K-γ抑制，可用于预防和治疗与PI3K相关的疾病，特别是PI3K-γ活性。 更具体地说，本发明的唑类衍生物可用于治疗和预防以下疾病：炎性和免疫调节性疾病，如哮喘，特应性皮炎，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），脓毒性休克，关节 疾病，自身免疫疾病如类风湿性关节炎，格雷夫斯病，癌症，心肌收缩性疾病，心力衰竭，血栓栓塞，缺血和动脉粥样硬化。 本发明的化合物还可用于肺动脉高压，肾衰竭，心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病，糖尿病和局灶性缺血，因为这些疾病还涉及人或动物中的PI3K活性 学科。