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    Sulphonyl compounds for use as linkers in solid phase and combinatorial synthesis
    1.
    发明授权
    Sulphonyl compounds for use as linkers in solid phase and combinatorial synthesis 失效
    用作固相和组合合成中的接头的磺酰基化合物

    公开(公告)号：US06225480B1

    公开(公告)日：2001-05-01

    申请号：US09331580

    申请日：1999-06-30

    申请人： Akito Tanaka ,  Hideo Tsutsumi

    发明人： Akito Tanaka ,  Hideo Tsutsumi

    IPC分类号： C07D31104

    CPC分类号： C40B80/00 ,  C07C309/87 ,  C07D311/70 ,  C07D311/92 ,  C40B40/04 ,  C40B50/14 ,  Y02P20/55

    摘要： The present invention relates to a linker shown by the following formula (I): X—SO2—R1—(A)m—R2  (I) wherein R1 is a group of the formula (A): [wherein R3, R4 and R5 are the same or different hydrogen, etc], etc, R2 is a group which can form a chemical bond to a resin which may be protected by a conventional protective group, A is lower alkylene, etc, X is a leaving group, and m is an integer of 0 or 1, with proviso that A is (C2-C6)alkylene, and m is an integer of 1, when R1 is a group of the formula (A).

    摘要翻译： 本发明涉及由下式（I）表示的接头：其中R1是式（A）的基团：[其中R3，R4和R5是相同或不同的氢等]等，R2是 可以与常规保护基保护的树脂形成化学键的基团，A为低级亚烷基等，X为离去基团，m为0或1的整数，条件是A为（C2- C6）亚烷基，当R1是式（A）的基团时，m是1的整数。

    HETERO COMPOUND
    2.
    发明申请
    HETERO COMPOUND 有权
    HETERO化合物

    公开(公告)号：US20090076070A1

    公开(公告)日：2009-03-19

    申请号：US12244102

    申请日：2008-10-02

    申请人： Hironori HARADA ,  Kazuyuki Hattori ,  Kazuya Fujita ,  Masataka Morita ,  Sunao Imada ,  Yoshito Abe ,  Hiromichi Itani ,  Tatsuaki Morokata ,  Hideo Tsutsumi

    发明人： Hironori HARADA ,  Kazuyuki Hattori ,  Kazuya Fujita ,  Masataka Morita ,  Sunao Imada ,  Yoshito Abe ,  Hiromichi Itani ,  Tatsuaki Morokata ,  Hideo Tsutsumi

    IPC分类号： A61K31/4245 ,  C07D413/14 ,  A61K31/437 ,  A61P35/02 ,  A61P19/02 ,  A61P1/00 ,  A61P9/10 ,  A61P37/06 ,  A61P35/00 ,  A61K31/4709

    CPC分类号： C07D413/04 ,  C07D417/04 ,  C07D471/04

    摘要： [Problems] To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.[Means for Solving] Since the compound of the invention has an S1P1 agonist activity, it is useful as an active ingredient for a treating or preventing agent for a disease caused by unfavorable lymphocytic infiltration, for example, an autoimmune disease such as graft rejection in the transplantation of an organ, bone marrow, or a tissue, a graft-versus-host disease, rheumatic arthritis, multiple sclerosis, systemic lupus erythematosus, a nephrotic syndrome, encephalomeningitis, myasthenia gravis, pancreatitis, hepatitis, nephritis, diabetes, pulmonary disorder, asthma, atopic dermatitis, inflammatory bowel disease, atherosclerosis, ischemia-reperfusion injury, or an inflammatory disease, and further, a disease caused by the abnormal growth or accumulation of cells such as cancer and leukemia.

    摘要翻译： [问题]提供一种有用的化合物作为活性成分，用于预防和/或治疗移植器官，骨髓或组织，自身免疫疾病等中的排斥反应，其具有优异的S1P1激动剂 活动。 [解决手段]由于本发明的化合物具有S1P1激动剂活性，因此可用作由不利的淋巴细胞浸润引起的疾病的治疗或预防剂的活性成分，例如自身免疫性疾病例如移植排斥反应 器官移植，骨髓或组织，移植物抗宿主病，风湿性关节炎，多发性硬化，系统性红斑狼疮，肾病综合征，脑炎，重症肌无力，胰腺炎，肝炎，肾炎，糖尿病，肺功能障碍 哮喘，特应性皮炎，炎症性肠病，动脉粥样硬化，局部缺血再灌注损伤，炎症性疾病等疾病，以及癌症，白血病等细胞异常生长或积累引起的疾病。

    Kasugamycin derivatives, pharmaceutical compositions and method of use
    4.
    发明授权
    Kasugamycin derivatives, pharmaceutical compositions and method of use 失效
    春日霉素衍生物，药物组合物和使用方法

    公开(公告)号：US4554269A

    公开(公告)日：1985-11-19

    申请号：US573377

    申请日：1984-01-24

    申请人： Takao Takaya ,  Nobuyoshi Yasuda ,  Hideo Tsutsumi ,  Keiji Matsuda

    发明人： Takao Takaya ,  Nobuyoshi Yasuda ,  Hideo Tsutsumi ,  Keiji Matsuda

    IPC分类号： C07H15/207 ,  A61K31/71 ,  C07H15/20

    CPC分类号： C07H15/207

    摘要： This invention relates to new aminoglycoside derivatives and pharmaceutically acceptable salts thereof. More particularly it relates to new aminoglycoside derivatives and pharmaceutically acceptable salts thereof which have anti-viral activity, and immuno-stimulating activity and pharmaceutical compositions comprising the same. In addition, this invention also relates to methods of preparing the aminoglycoside derivatives and salts thereof.

    摘要翻译： 本发明涉及新的氨基糖苷衍生物及其药学上可接受的盐。 更具体地说，本发明涉及具有抗病毒活性的新的氨基糖苷衍生物及其药学上可接受的盐以及免疫刺激活性以及包含其的药物组合物。 此外，本发明还涉及制备氨基糖苷衍生物及其盐的方法。

    HETERO COMPOUND
    5.
    发明申请
    HETERO COMPOUND 有权
    HETERO化合物

    公开(公告)号：US20100168159A1

    公开(公告)日：2010-07-01

    申请号：US12696327

    申请日：2010-01-29

    申请人： Hironori Harada ,  Kazuyuki Hattori ,  Kazuya Fujita ,  Masataka Morita ,  Sunao Imada ,  Yoshito Abe ,  Hiromichi Itani ,  Tatsuaki Morokata ,  Hideo Tsutsumi

    发明人： Hironori Harada ,  Kazuyuki Hattori ,  Kazuya Fujita ,  Masataka Morita ,  Sunao Imada ,  Yoshito Abe ,  Hiromichi Itani ,  Tatsuaki Morokata ,  Hideo Tsutsumi

    IPC分类号： A61K31/4439 ,  A61K31/4709 ,  C07D471/04 ,  C07D413/14 ,  A61P35/02 ,  A61P37/06 ,  A61P29/00 ,  A61P9/10 ,  A61P35/00

    CPC分类号： C07D413/04 ,  C07D417/04 ,  C07D471/04

    摘要： [Problems]To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.[Means for solving]Since the compound of the invention has an S1P1 agonist activity, it is useful as an active ingredient for a treating or preventing agent for a disease caused by unfavorable lymphocytic infiltration, for example, an autoimmune disease such as graft rejection in the transplantation of an organ, bone marrow, or a tissue, a graft-versus-host disease, rheumatic arthritis, multiple sclerosis, systemic lupus erythematosus, a nephrotic syndrome, encephalomeningitis, myasthenia gravis, pancreatitis, hepatitis, nephritis, diabetes, pulmonary disorder, asthma, atopic dermatitis, inflammatory bowel disease, atherosclerosis, ischemia-reperfusion injury, or an inflammatory disease, and further, a disease caused by the abnormal growth or accumulation of cells such as cancer and leukemia.

    摘要翻译： [问题]提供一种有用的化合物作为活性成分，用于预防和/或治疗移植器官，骨髓或组织，自身免疫疾病等中的排斥反应，其具有优异的S1P1激动剂 活动。 [解决方法]由于本发明的化合物具有S1P1激动剂活性，因此可用作由不利的淋巴细胞浸润引起的疾病的治疗或预防剂的活性成分，例如自身免疫性疾病如移植排斥反应 器官移植，骨髓或组织，移植物抗宿主病，风湿性关节炎，多发性硬化，系统性红斑狼疮，肾病综合征，脑炎，重症肌无力，胰腺炎，肝炎，肾炎，糖尿病，肺功能障碍 哮喘，特应性皮炎，炎症性肠病，动脉粥样硬化，局部缺血再灌注损伤，炎症性疾病等疾病，以及癌症，白血病等细胞异常生长或积累引起的疾病。

    Certain tricyclic pyrido[3,2,1-ij]cinnoline-8-carboxylates, useful as antimicrobial agents
    6.
    发明授权
    Certain tricyclic pyrido[3,2,1-ij]cinnoline-8-carboxylates, useful as antimicrobial agents 失效
    某些三环吡啶并[3,2,1-ij]噌啉-8-羧酸盐，可用作抗微生物剂

    公开(公告)号：US5359066A

    公开(公告)日：1994-10-25

    申请号：US938249

    申请日：1993-06-15

    申请人： Hideo Tsutsumi ,  Takeshi Terasawa ,  David Barrett ,  Masayoshi Murata ,  Kazuo Sakane ,  Akira Yazaki ,  Satoshi Inoue

    发明人： Hideo Tsutsumi ,  Takeshi Terasawa ,  David Barrett ,  Masayoshi Murata ,  Kazuo Sakane ,  Akira Yazaki ,  Satoshi Inoue

    IPC分类号： C07D471/06 ,  C07D519/00 ,  A61K31/50 ,  C07D487/06

    CPC分类号： C07D471/06 ,  Y02P20/55

    摘要： A compound represented by the following general formula: ##STR1## which is useful as an intermediate for production of a clinically excellent synthetic antibacterial, a salt thereof, and a process for producing the same.In said formula,R.sup.1 is a hydrogen atom or a carboxyl-protecting group;R.sup.2 is a hydrogen atom or a lower alkyl group;X.sup.1 is a hydrogen atom or a halogen atom;X.sup.2 is a halogen atom;X.sub.a.sup.5 is a hydrogen atom or a halogen atom;A is a methylene group; a group of >CH--COOR.sup.4, etc.,in which R.sup.4, R.sup.5 and R.sup.6 each are a hydrogen atom or a carboxyl-protecting group;B is a methylene group or a carbonyl group;provided that both A and B must not be methylene groups at the same time.

    摘要翻译： PCT No.PCT / JP92 / 00215 Sec。 371日期：1993年6月15日 102（e）日期1993年6月15日PCT提交1992年2月27日PCT公布。 第WO92 / 15584号公报 日期：1992年9月17日，由以下通式表示的化合物：作为制备临床上优异的合成抗菌剂的中间体及其制备方法可以使用的化合物（A）。 在所述式中，R 1为氢原子或羧基保护基; R2是氢原子或低级烷基; X1是氢原子或卤素原子; X2是卤原子; Xa5是氢原子或卤素原子; A是亚甲基; 一组> CH-COOR4等，其中R4，R5和R6各自为氢原子或羧基保护基; B是亚甲基或羰基; 条件是A和B不能同时为亚甲基。

    Aminopyrimidine compounds, processes for their preparation and pharmaceutical compositions containing them
    10.
    发明申请
    Aminopyrimidine compounds, processes for their preparation and pharmaceutical compositions containing them 审中-公开
    氨基嘧啶化合物，其制备方法和含有它们的药物组合物

    公开(公告)号：US20050043315A1

    公开(公告)日：2005-02-24

    申请号：US10498016

    申请日：2002-12-27

    申请人： Hideo Tsutsumi ,  Satoshi Yonishi ,  Atsushi Akahane

    发明人： Hideo Tsutsumi ,  Satoshi Yonishi ,  Atsushi Akahane

    IPC分类号： C07D401/14 ,  C07D403/04 ,  C07D409/14 ,  C07D43/02 ,  A61K31/501

    CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D409/14

    摘要： An aminopyrimidine compound of the following formula (I) wherein Q is (a) or (b) in which R and R′ are each optionally substituted aryl or heterocyclic group,R5 is hydrogen, halogen, lower alkyl,optionally substituted hydroxy, optionally substituted amino which may form N-containing heterocyclic group, optionally substituted mercapto, lower alkylsulfinyl or lower alkylsulfonyl, and X is oxygen or sulfur; R1 is hydrogen, optionally substituted lower alkyl or cyclo(lower) alkyl which may be interrupted by an oxygen atom; R2 and R3 are each independently hydrogen, lower alkyl, acyl, aryl or heterocyclic(lower)alkyl, R2 and R3 may be combined together with N atom to which they are attached to form N-containing heterocyclic group; or a salt thereof. The aminopyrimidine compound (I) and salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.

    摘要翻译： 其中Q为（a）或（b）的下式（I）的氨基嘧啶化合物，其中R和R'各自为任选取代的芳基或杂环基，R 5为氢，卤素，低级烷基，任选取代的羟基 ，可以形成含氮杂环基的任选取代的氨基，任选取代的巯基，低级烷基亚磺酰基或低级烷基磺酰基，X是氧或硫; R 1是氢，任选取代的可被氧原子间隔的低级烷基或环（低级）烷基; R 2和R 3各自独立地为氢，低级烷基，酰基，芳基或杂环（低级）烷基，R 2和R 3可以与它们所连接的N原子一起形成 含氮杂环基; 或其盐。 本发明的氨基嘧啶化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁症，痴呆（例如阿尔茨海默氏病，脑血管性痴呆，伴有帕金森病的痴呆等），帕金森病， 焦虑，疼痛，脑血管疾病（例如中风等），心力衰竭等。