利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

29 条记录 (耗时 0.027 秒)

    Methods for oxime conjugation to ketone-modified polypeptides
    1.
    发明授权
    Methods for oxime conjugation to ketone-modified polypeptides 有权

    公开(公告)号：US10172948B2

    公开(公告)日：2019-01-08

    申请号：US14551187

    申请日：2014-11-24

    申请人： Qi-Ying Hu ,  Hidetomo Imase

    发明人： Qi-Ying Hu ,  Hidetomo Imase

    IPC分类号： A61K38/00 ,  A61K47/48 ,  C07K1/113 ,  C07K7/64 ,  A61K47/54 ,  A61K47/62 ,  A61K47/64 ,  A61K47/68

    摘要： The invention provides improved methods to prepare protein conjugates from a ketone-modified protein. In one embodiment, the protein is prepared by linking two free cysteines by reaction with a 1,3-dihaloacetone or similar ketone-containing reactant, linking the sulfur atoms of the two cysteines together. The ketone inserted between the sulfur atoms is then used to form an oxime, thus conjugating the protein to a payload. In another embodiment, two cysteine residues are tied together by reaction with a 1,3-dihaloacetone or similar reactant, and the new ketone is used to form an oxime with a suitable payload molecule, thus conjugating the protein to a payload. The method provides improved reaction conditions for the oxime formation, whereby higher yields and improved product homogeneity are achieved.

    METHODS FOR OXIME CONJUGATION TO KETONE-MODIFIED POLYPEPTIDES
    2.
    发明申请
    METHODS FOR OXIME CONJUGATION TO KETONE-MODIFIED POLYPEPTIDES 审中-公开
    用于与酮改性聚合物结合的方法

    公开(公告)号：US20150150998A1

    公开(公告)日：2015-06-04

    申请号：US14551187

    申请日：2014-11-24

    申请人： Qi-Ying Hu ,  Hidetomo Imase

    发明人： Qi-Ying Hu ,  Hidetomo Imase

    IPC分类号： A61K47/48 ,  C07K7/64 ,  C07K1/113

    CPC分类号： C07K7/64 ,  A61K47/542 ,  A61K47/62 ,  A61K47/646 ,  A61K47/68 ,  A61K47/6803 ,  A61K47/6849 ,  C07K1/1133 ,  C07K2317/40

    摘要： The invention provides improved methods to prepare protein conjugates from a ketone-modified protein. In one embodiment, the protein is prepared by linking two free cysteines by reaction with a 1,3-dihaloacetone or similar ketone-containing reactant, linking the sulfur atoms of the two cysteines together. The ketone inserted between the sulfur atoms is then used to form an oxime, thus conjugating the protein to a payload. In another embodiment, two cysteine residues are tied together by reaction with a 1,3-dihaloacetone or similar reactant, and the new ketone is used to form an oxime with a suitable payload molecule, thus conjugating the protein to a payload. The method provides improved reaction conditions for the oxime formation, whereby higher yields and improved product homogeneity are achieved.

    摘要翻译： 本发明提供了从酮修饰的蛋白质制备蛋白质缀合物的改进方法。 在一个实施方案中，通过与1,3-二卤代丙酮或类似的含酮反应物反应连接两个游离半胱氨酸来制备蛋白质，其将两个半胱氨酸的硫原子连接在一起。 然后将插入硫原子之间的酮用于形成肟，从而使蛋白质与有效载荷共轭。 在另一个实施方案中，通过与1,3-二卤代丙酮或类似反应物反应将两个半胱氨酸残基连接在一起，并且新的酮用于形成具有合适有效载荷分子的肟，从而​​将蛋白质与有效载荷共轭。 该方法为肟形成提供改进的反应条件，从而获得更高的产率和改善的产物均匀性。

    SYNTHETIC APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE
    3.
    发明申请
    SYNTHETIC APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE 有权
    用于治疗心脏衰竭的合成APELINMIMT

    公开(公告)号：US20130196899A1

    公开(公告)日：2013-08-01

    申请号：US13747621

    申请日：2013-01-23

    申请人： Frédéric ZECRI ,  Andrei GOLOSOV ,  Philipp GROSCHE ,  Kayo YASOSHIMA ,  Hongjuan ZHAO ,  Qi-Ying HU ,  Hidetomo IMASE ,  David Thomas PARKER

    发明人： Frédéric ZECRI ,  Andrei GOLOSOV ,  Philipp GROSCHE ,  Kayo YASOSHIMA ,  Hongjuan ZHAO ,  Qi-Ying HU ,  Hidetomo IMASE ,  David Thomas PARKER

    IPC分类号： C07K7/08 ,  C07K7/60 ,  C07K7/56

    CPC分类号： A61M16/0816 ,  A61K38/00 ,  A61K38/10 ,  A61M16/0066 ,  A61M16/201 ,  A61M2016/0027 ,  A61M2016/003 ,  A61M2205/35 ,  A61M2205/502 ,  C07K7/08 ,  C07K7/56 ,  C07K7/60

    摘要： The invention provides a synthetic polypeptide of Formula I′: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

    摘要翻译： 本发明提供式I'的合成多肽：或其酰胺，酯或其盐，其中X1，X2，X3，X4，X5，X6，X7，X8，X9，X10，X11，X12和X13被定义 这里。 多肽是APJ受体的激动剂。 本发明还涉及制备本发明多肽的方法及其治疗用途，例如治疗或预防急性失代偿性心力衰竭（ADHF），慢性心力衰竭，肺动脉高压，心房颤动，Brugada综合征，室性心动过速，动脉粥样硬化 ，高血压，再狭窄，缺血性心血管疾病，心肌病，心脏纤维化，心律失常，保水，糖尿病（包括妊娠糖尿病），肥胖，外周动脉疾病，脑血管意外，短暂性脑缺血发作，创伤性脑损伤，肌萎缩性侧索硬化，烧伤（ 包括晒伤）和先兆子痫。 本发明还提供药理活性剂和药物组合物的组合。

    SYNTHETIC APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE
    6.
    发明申请
    SYNTHETIC APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE 有权
    用于治疗心脏衰竭的合成APELINMIMT

    公开(公告)号：US20150252076A1

    公开(公告)日：2015-09-10

    申请号：US14714914

    申请日：2015-05-18

    申请人： Frederic ZECRI ,  Andrei GOLOSOV ,  Philipp GROSCHE ,  Hongjuan ZHAO ,  Qi-Ying HU ,  Hidetomo IMASE

    发明人： Frederic ZECRI ,  Andrei GOLOSOV ,  Philipp GROSCHE ,  Hongjuan ZHAO ,  Qi-Ying HU ,  Hidetomo IMASE

    IPC分类号： C07K7/08 ,  A61K38/10

    CPC分类号： A61M16/0816 ,  A61K38/00 ,  A61K38/10 ,  A61M16/0066 ,  A61M16/201 ,  A61M2016/0027 ,  A61M2016/003 ,  A61M2205/35 ,  A61M2205/502 ,  C07K7/08 ,  C07K7/56 ,  C07K7/60

    摘要： The invention provides a synthetic polypeptide of Formula I′: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

    摘要翻译： 本发明提供式I'的合成多肽：或其酰胺，酯或其盐，其中X1，X2，X3，X4，X5，X6，X7，X8，X9，X10，X11，X12和X13被定义 这里。 多肽是APJ受体的激动剂。 本发明还涉及制备本发明多肽的方法及其治疗用途，例如治疗或预防急性失代偿性心力衰竭（ADHF），慢性心力衰竭，肺动脉高压，心房颤动，Brugada综合征，室性心动过速，动脉粥样硬化 ，高血压，再狭窄，缺血性心血管疾病，心肌病，心脏纤维化，心律失常，保水，糖尿病（包括妊娠糖尿病），肥胖，外周动脉疾病，脑血管意外，短暂性脑缺血发作，创伤性脑损伤，肌萎缩性侧索硬化，烧伤（ 包括晒伤）和先兆子痫。 本发明还提供药理活性剂和药物组合物的组合。

    SYNTHETIC APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE
    8.
    发明申请
    SYNTHETIC APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE 审中-公开
    用于治疗心脏衰竭的合成APELINMIMT

    公开(公告)号：US20140142022A1

    公开(公告)日：2014-05-22

    申请号：US14165680

    申请日：2014-01-28

    申请人： Frederic ZECRI ,  Andrei GOLOSOV ,  Philipp GROSCHE ,  Kayo YASOSHIMA ,  Hongjuan ZHAO ,  Qi-Ying HU ,  Hidetomo IMASE ,  David Thomas PARKER

    发明人： Frederic ZECRI ,  Andrei GOLOSOV ,  Philipp GROSCHE ,  Kayo YASOSHIMA ,  Hongjuan ZHAO ,  Qi-Ying HU ,  Hidetomo IMASE ,  David Thomas PARKER

    IPC分类号： C07K7/08

    CPC分类号： A61M16/0816 ,  A61K38/00 ,  A61K38/10 ,  A61M16/0066 ,  A61M16/201 ,  A61M2016/0027 ,  A61M2016/003 ,  A61M2205/35 ,  A61M2205/502 ,  C07K7/08 ,  C07K7/56 ,  C07K7/60

    摘要： The invention provides a synthetic polypeptide of Formula I′: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

    摘要翻译： 本发明提供式I'的合成多肽：或其酰胺，酯或其盐，其中X1，X2，X3，X4，X5，X6，X7，X8，X9，X10，X11，X12和X13被定义 这里。 多肽是APJ受体的激动剂。 本发明还涉及制备本发明多肽的方法及其治疗用途，例如治疗或预防急性失代偿性心力衰竭（ADHF），慢性心力衰竭，肺动脉高压，心房颤动，Brugada综合征，室性心动过速，动脉粥样硬化 ，高血压，再狭窄，缺血性心血管疾病，心肌病，心脏纤维化，心律失常，保水，糖尿病（包括妊娠糖尿病），肥胖，外周动脉疾病，脑血管意外，短暂性脑缺血发作，创伤性脑损伤，肌萎缩性侧索硬化，烧伤（ 包括晒伤）和先兆子痫。 本发明还提供药理活性剂和药物组合物的组合。