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    Heart muscular cell apoptosis inhibitors and remedies/preventives for heart diseases
    1.
    发明授权
    Heart muscular cell apoptosis inhibitors and remedies/preventives for heart diseases 失效
    心脏肌细胞凋亡抑制剂和心脏病的治疗/预防药物

    公开(公告)号：US06794383B2

    公开(公告)日：2004-09-21

    申请号：US10363290

    申请日：2003-02-27

    申请人： Haruhide Kimura ,  Seiichi Tanida ,  Tatsuhiko Kaneko

    发明人： Haruhide Kimura ,  Seiichi Tanida ,  Tatsuhiko Kaneko

    IPC分类号： A61K315415

    CPC分类号： C07D417/04 ,  A61K31/5415 ,  C07D279/08 ,  C07D279/16

    摘要： The present invention is intended to provide excellent preventives and/or remedies for heart diseases. Specifically, the present invention provides heart muscle cell apoptosis inhibitors, preventives and/or remedies for heart diseases, comprising a compound represented by the following formula: wherein R represents an optionally substituted hydrocarbon group, an optionally substituted aromatic heterocyclic group, or an optionally substituted amino group; or a salt thereof.

    摘要翻译： 本发明旨在为心脏病提供优异的预防措施和/或补救措施。 具体而言，本发明提供心肌细胞凋亡抑制剂，心脏病的预防剂和/或治疗药物，其包含由下式表示的化合物：其中R表示任选取代的烃基，任选取代的芳族杂环基或任选取代的 氨基; 或其盐。

    Method of preparing heart muscle cells and method of searching for remedy for heart diseases
    2.
    发明申请
    Method of preparing heart muscle cells and method of searching for remedy for heart diseases 审中-公开
    心肌细胞的制备方法及心脏病的治疗方法

    公开(公告)号：US20080160553A1

    公开(公告)日：2008-07-03

    申请号：US12069074

    申请日：2008-02-07

    申请人： Haruhide Kimura ,  Nobuyuki Koyama ,  Seiichi Tanida ,  Tadamitsu Kishimoto ,  Keiko Takihara ,  Hisao Hirota

    发明人： Haruhide Kimura ,  Nobuyuki Koyama ,  Seiichi Tanida ,  Tadamitsu Kishimoto ,  Keiko Takihara ,  Hisao Hirota

    IPC分类号： C12Q1/02 ,  C12Q1/48

    CPC分类号： G01N33/5061 ,  C12N5/0657 ,  C12N2503/02 ,  C12N2509/00 ,  G01N2510/00 ,  G01N2800/324

    摘要： The present invention relates to a method of preparing primary heart muscle cells, characterized by washing a fine fragmented heart tissue with a phosphate-buffered physiological saline to thereby eliminate non-heart muscle cells and then hemolyzing the heart tissue digested with a protease to thereby eliminate erythrocytes. According to this method, highly pure primary heart muscle cells can be conveniently obtained in a large amount from the heart of an animal embryo or newborn. By using the heart muscle thus prepared, apoptosis of heart muscle cells can be efficiently and highly sensitively detected. Thus, it is possible to efficiently screen candidate compounds for heart muscle cell apoptosis inhibitors, gp 130-mediated receptor agonists, heart muscle cell-protective signal enhancers, preventives and remedies for heart diseases. A method of detecting apoptosis comprises inducing apoptosis of heart muscle cells by incubating the cells in a serum-free medium, adding serum to the liquid culture medium thereof, then incubating the cells and counting viable heart muscle cells.

    摘要翻译： 本发明涉及一种制备主要心肌细胞的方法，其特征在于用磷酸盐缓冲生理盐水洗涤细碎的心脏组织，从而消除非心脏肌肉细胞，然后溶解用蛋白酶消化的心脏组织，从而消除 红细胞。 根据该方法，可以从动物胚胎或新生儿的心脏中大量获得高纯度的原代心肌细胞。 通过使用如此制备的心肌，可以高效且高度敏感地检测心肌细胞的凋亡。 因此，可以有效地筛选用于心肌细胞凋亡抑制剂，gp130介导的受体激动剂，心肌细胞保护性信号增强剂，预防药物和心脏病的药物的候选化合物。 检测凋亡的方法包括通过在无血清培养基中孵育细胞来诱导心肌细胞凋亡，向其液体培养基中加入血清，然后孵育细胞并计数活的心肌细胞。

    15-hydroxy 6,9-hemiacetal erythromycin compounds
    4.
    发明授权
    15-hydroxy 6,9-hemiacetal erythromycin compounds 失效
    15-羟基6,9-半缩醛红霉素化合物

    公开(公告)号：US5854407A

    公开(公告)日：1998-12-29

    申请号：US475557

    申请日：1995-06-07

    申请人： Setsuo Harada ,  Yasunori Funabashi ,  Nobuhiro Inatomi ,  Shigeharu Tanayama ,  Seiichi Tanida

    发明人： Setsuo Harada ,  Yasunori Funabashi ,  Nobuhiro Inatomi ,  Shigeharu Tanayama ,  Seiichi Tanida

    IPC分类号： C07H17/08 ,  C12P19/62

    CPC分类号： C12P19/62 ,  C07H17/08

    摘要： Disclosed are (1) a structurally novel 6,9-hemiacetal- erythromycin derivative having a hydroxyl group at at least one of the 14- and 15-positions br a salt thereof, which has an excellent gastrointestinal function promoting effect and is low in toxicity; (2) a process for preparing a 6,9-hemiacetal-erythromycin derivative having a hydroxyl group at at least one of the 14- and 15-positions or a salt thereof, which comprises reacting a 6,9-hemiacetal-erythromycin derivative or a salt thereof with an organism-derived oxidase; and (3) a gastrointestinal function promoting agent containing a 6,9-hemiacetal-erythromycin derivative having a hydroxyl group at at least one of the 14- and 15-positions or a salt thereof.

    摘要翻译： 公开了（1）结构上新的6,9-半缩醛红霉素衍生物，其在14位和15位的至少一个位上具有羟基，其盐具有优异的胃肠功能促进作用，毒性低 ; （2）制备在14位和15位的至少一个位置具有羟基的6,9-半缩醛红霉素衍生物或其盐的方法，该方法包括使6,9-半缩醛红霉素衍生物或 其与生物体衍生的氧化酶的盐; 和（3）包含在14位和15位中的至少一个具有羟基的6,9-半缩醛红霉素衍生物或其盐的胃肠功能促进剂。

    14 and/or 15-hydroxy 6,9 hemiacetal erythromycin derivatives
    5.
    发明授权
    14 and/or 15-hydroxy 6,9 hemiacetal erythromycin derivatives 失效
    14和/或15-羟基6,9半缩醛红霉素衍生物

    公开(公告)号：US5470961A

    公开(公告)日：1995-11-28

    申请号：US33777

    申请日：1993-03-19

    申请人： Setsuo Harada ,  Yasunori Funabashi ,  Nobuhiro Inatomi ,  Shigeharu Tanayama ,  Seiichi Tanida

    发明人： Setsuo Harada ,  Yasunori Funabashi ,  Nobuhiro Inatomi ,  Shigeharu Tanayama ,  Seiichi Tanida

    IPC分类号： C07H17/08 ,  C12P19/62 ,  A61K31/70

    CPC分类号： C12P19/62 ,  C07H17/08

    摘要： Disclosed are (1) a structurally novel 6,9-hemiacetal-erythromycin derivative having a hydroxyl group at at least one of the 14- and 15-positions or a salt thereof, which has an excellent gastrointestinal function promoting effect and is low in toxicity; (2) a process for preparing a 6,9-hemiacetal-erythromycin derivative having a hydroxyl group at at least one of the 14- and 15-positions or a salt thereof, which comprises reacting a 6,9-hemiacetal-erythromycin derivative or a salt thereof with an organism-derived oxidase; and (3) a gastrointestinal function promoting agent containing a 6,9-hemiacetal-erythromycin derivative having a hydroxyl group at at least one of the 14- and 15-positions or a salt thereof.

    摘要翻译： 公开了（1）在14位和15位中的至少一个上具有羟基的结构新颖的6,9-半缩醛红霉素衍生物或其盐，其具有优异的胃肠功能促进作用并且毒性低 ; （2）制备在14位和15位的至少一个位置具有羟基的6,9-半缩醛红霉素衍生物或其盐的方法，该方法包括使6,9-半缩醛红霉素衍生物或 其与生物体衍生的氧化酶的盐; 和（3）包含在14位和15位中的至少一个具有羟基的6,9-半缩醛红霉素衍生物或其盐的胃肠功能促进剂。

    Method for producing maytansinol and its derivatives
    6.
    发明授权
    Method for producing maytansinol and its derivatives 失效
    生产美登素及其衍生物的方法

    公开(公告)号：US4151042A

    公开(公告)日：1979-04-24

    申请号：US811442

    申请日：1977-06-29

    申请人： Eiji Higashide ,  Mitsuko Asai ,  Seiichi Tanida

    发明人： Eiji Higashide ,  Mitsuko Asai ,  Seiichi Tanida

    IPC分类号： C12P17/18 ,  C12D9/20

    CPC分类号： C12P17/188 ,  Y10S435/872

    摘要： Maytansinol, maytanacine or maytansinol propionate is (are) produced by cultivating a microorganism belonging to the genus Nocardia and being capable of producing maytansinol, maytanacine or maytansinol propionate, causing the microorganism to accumulate maytansinol, maytanacine or maytansinol propionate and recovering the same.Those compounds are useful for anti-tumor agents.

    摘要翻译： 通过培养属于诺卡氏菌属的微生物并且能够产生美登素，可以在马来西亚或丙酸美他曲诺醇中产生美登那诺，依托那康或丙酸美他坦诺，使微生物积累美登醇，美沙酮或丙酸美他曲诺醇并回收它们。

    Thioglycerol derivatives
    7.
    发明授权
    Thioglycerol derivatives 失效
    硫代甘油衍生物

    公开(公告)号：US5506267A

    公开(公告)日：1996-04-09

    申请号：US302337

    申请日：1994-09-08

    申请人： Tetsuya Aono ,  Koichi Yukishige ,  Seiichi Tanida

    发明人： Tetsuya Aono ,  Koichi Yukishige ,  Seiichi Tanida

    IPC分类号： A61K38/00 ,  C07C317/44 ,  C07C323/60 ,  C07D209/46 ,  C07D209/48 ,  C07K5/06 ,  C07K5/072 ,  C07K5/083 ,  C07K5/103 ,  C07K5/11 ,  A61K31/16

    CPC分类号： C07D209/48 ,  C07C317/44 ,  C07C323/60 ,  C07D209/46 ,  C07K5/06026 ,  C07K5/06104 ,  C07K5/0806 ,  C07K5/1008 ,  C07K5/1019 ,  A61K38/00

    摘要： A compound of the invention is represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different, an acyl group; R.sup.3, R.sup.4, R.sup.6 and R.sup.7 are the same or different, hydrogen or an alkyl group; R.sup.5 is hydrogen, an alkyl group or a hydroxyl group which may optionally be protected, or R.sup.4 and R.sup.5 are combined to form a chemical bond; X is a carbonyl group or a sulfonyl group; Y is an amino acid sequence consisting of 1 to 7 amino acid residues which may optionally be protected and having optionally an intervening --SO.sub.2 NH--; n is an integer of 0 to 2, or a salt thereof.The compound or salt thereof of the present invention possesses immunoenhancing activity and platelet reduction recovery activity, and can be used as a prophylactic/therapeutic agent for leukocytopenia in cancer chemotherapy or radiotherapy, as an immunoenhancing agent in bone marrow transplantation therapy and the treatment of osteomyelodysplasia and aplastic anemia, and as a prophylactic/therapeutic agent for thrombocytopenia.

    摘要翻译： 本发明的化合物由下式表示：其中R1和R2相同或不同，酰基; R3，R4，R6和R7相同或不同，为氢或烷基; R5是氢，烷基或可任意被保护的羟基，或R4和R5组合形成化学键; X是羰基或磺酰基; Y是由1至7个氨基酸残基组成的氨基酸序列，其可任选被保护并且任选地具有中间的-SO 2 NH-; n为0〜2的整数，或其盐。 本发明的化合物或其盐具有免疫增强活性和血小板减少恢复活性，可用作癌症化学疗法或放射治疗中的白细胞减少症的预防/治疗剂，作为骨髓移植治疗中的免疫增强剂和骨髓移植治疗 和再生障碍性贫血，以及作为血小板减少症的预防/治疗剂。