8-Hydroxy-7-methyl-9H-pyrido[1,2-b]isoquinolin-9-one--hydrogen bromide (1/1) | 21852-25-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 英文名称: 8-Hydroxy-7-methyl-9H-pyrido[1,2-b]isoquinolin-9-one--hydrogen bromide (1/1)
• 英文别名: 8-hydroxy-7-methylbenzo[b]quinolizin-9-one;hydrobromide
• CAS: 21852-25-5
• 化学式: C14H12BrNO2
• 分子量: 306.15
• InChiKey: DWNIXHARVTYMBF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  18
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  44.6
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• RHAMNOSE SUBSTITUENTS OF SL0101 AND THERAPEUTIC USES THEREOF
  申请人：Smith Jeffrey A.

  公开号：US20100016245A1

  公开（公告）日：2010-01-21

  The present invention provides compositions and methods useful for preparing and using analogs, derivatives, and modifications of kaempferols that have anti-neoplastic activity. More specifically, the compounds are analogs, derivatives, and modifications of SLO1O1. The invention further provides compounds that are inhibitors of rsk activity. The invention further provides compounds that selectively inhibit excessive rsk activity in cancers. The present invention further provides methods for treating cancer using compounds of the invention.

  本发明提供了用于制备和使用具有抗肿瘤活性的山柰酚的类似物、衍生物和修饰物的组合物和方法。更具体地说，这些化合物是SLO1O1的类似物、衍生物和修饰物。本发明还提供了抑制rsk活性的化合物。本发明还提供了在癌症中选择性抑制过度rsk活性的化合物。本发明还提供了使用本发明中的化合物治疗癌症的方法。
• Combination therapy with antibodies and anti-VEGF agents for the treatment of cancer
  申请人：Tracon Pharmaceuticals, Inc.

  公开号：EP2722055A1

  公开（公告）日：2014-04-23

  The present application relates to compositions of chimeric anti-endoglin antibodies and anti-VEGF agents. Another aspect relates to the use of the compositions to inhibit VEGF induced sprouting. Another aspect relates to the use of the compositions to inhibit angiogenesis.

  本申请涉及嵌合抗内皮素抗体和抗血管内皮生长因子制剂的组合物。另一个方面涉及组合物用于抑制血管内皮生长因子诱导的发芽。另一个方面涉及组合物抑制血管生成的用途。
• Antibody formulations and uses thereof
  申请人：Tracon Pharmaceuticals, Inc.

  公开号：US10195281B2

  公开（公告）日：2019-02-05

  The present application relates to formulations of anti-CD105 antibodies, antigen-binding fragments thereof, and uses thereof. Another aspect relates to pre-filled syringes of the formulations of anti-CD105 antibodies or antigen-binding fragments thereof. Another aspect relates to the use of the formulations to reduce one or more signs or symptoms of an angiogenesis-related disorder such as cancers and ophthalmologic diseases.

  本申请涉及抗 CD105 抗体制剂、其抗原结合片段及其用途。另一方面涉及抗 CD105 抗体或其抗原结合片段制剂的预灌封注射器。另一个方面涉及制剂在减少血管生成相关疾病（如癌症和眼科疾病）的一种或多种体征或症状方面的用途。
• T type calcium channel inhibitors
  申请人：University of Virginia Patent Foundation

  公开号：US10369120B2

  公开（公告）日：2019-08-06

  The present invention provides novel T type calcium channel inhibitors of formula (I), the use thereof in the treatment of a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels, wherein R1 is C1-C4 alkyl, hydroxy, or C1-C4 alkoxy; Z is NH, NCH3, O, S, or CH2; Y is NH, O, or CH2 with the proviso that Y and Z are not the same; R2 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy; m and n are independently selected from integers ranging from 1-5 with the proviso that m+n=an integer ranging from 2-9; and R3 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy.

  本发明提供了式(I)的新型T型钙通道抑制剂，其用途是治疗哺乳动物体内与细胞外钙通过T型钙通道流入有关的疾病或病症，其中R1是C1-C4烷基、羟基或C1-C4烷氧基；Z是NH、NCH3、O、S或CH2；Y是NH、O或CH2，但Y和Z不相同；R2是H、卤素、NH2、C1-C4烷基、羟基或C1-C4烷氧基；m和n独立地选自1-5的整数，但m+n=2-9的整数；以及R3是H、卤素、NH2、C1-C4烷基、羟基或C1-C4烷氧基。
• Rsk inhibitors and therapeutic uses thereof
  申请人：Smith A Jeffrey

  公开号：US20050233985A1

  公开（公告）日：2005-10-20

  The present invention is directed to novel compounds and compositions that have Rsk specific inhibitory activity. In addition, inhibition of Rsk by the present compounds has been discovered to halt the proliferation of cancer cell lines while having little effect on the proliferation rate of normal cells. Therefore, the present invention identifies Rsk as a target for therapeutic intervention in diseased states in which the disease or the symptoms can be ameliorated by inhibition of Rsk catalytic activity.

  本发明涉及具有 Rsk 特异性抑制活性的新型化合物和组合物。此外，已发现本发明化合物对 Rsk 的抑制可阻止癌细胞株的增殖，而对正常细胞的增殖率影响甚微。因此，本发明将 Rsk 确定为疾病状态下的治疗干预靶点，通过抑制 Rsk 的催化活性可以改善疾病或症状。