5,6,7,8-四氢-6-(2-丙基)-4H-噻唑并[4,5-d]氮杂-2-胺二盐酸盐

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吖庚因类
• 中文名称: 5,6,7,8-四氢-6-(2-丙基)-4H-噻唑并[4,5-d]氮杂-2-胺二盐酸盐
• 中文别名: 他利克索；盐酸他利克索
• 英文名称: hydron;6-prop-2-enyl-4,5,7,8-tetrahydro-[1,3]thiazolo[4,5-d]azepin-2-amine;dichloride
• 化学式: C10H17Cl2N3S
• 分子量: 282.2
• InChiKey: DPQAXNSOFFYKDS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.16
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  70.4
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• Kinase antagonists
  申请人：Knight A. Zachary

  公开号：US20070293516A1

  公开（公告）日：2007-12-20

  The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tryosine kinase, PI3Kinase and mTOR, or PI3Kinase, mTOR and tryosine kinase.

  本发明提供了一种新型化合物，它们是 PI3 激酶、PI3 激酶和酪氨酸激酶、PI3 激酶和 mTOR，或者 PI3 激酶、mTOR 和酪氨酸激酶的拮抗剂。
• METAL COMPLEX PHOSPHATIDYL-INOSITOL-3-KINASE INHIBITORS
  申请人：Meggers Eric

  公开号：US20090275547A1

  公开（公告）日：2009-11-05

  Provided are novel organometallic compounds that inhibit PI3K lipid kinase and phospho-AKT in human melanoma cells, and also inhibit the migration of melanoma cells. The present invention is also directed to methods for inhibiting cancer cell proliferation, migration or both comprising contacting a cancer cell with a disclosed organometallic kinase inhibitor. Also disclosed are methods for treating a kinase-affected disease or condition comprising administering to a subject in need thereof a therapeutically effective amount of a disclosed organometallic kinase inhibitor.

  提供的是新型有机金属化合物，它们能抑制人黑色素瘤细胞中的PI3K脂质激酶和磷酸化AKT，并且还能抑制黑色素瘤细胞的迁移。本发明还涉及抑制癌细胞增殖、迁移或两者的方法，包括将癌细胞与公开的有机金属激酶抑制剂接触。还公开了治疗激酶相关疾病或状况的方法，包括向有需要的受试者施用治疗有效量的公开的有机金属激酶抑制剂。
• SUBSTITUTED 8-SULFONYL-2,3,4,5-TETRAHYDRO-1H-GAMMA-CARBOLINES, LIGANDS AND PHARMACEUTICAL COMPOSITION; METHOD FOR THE PRODUCTION AND USE OF SAME
  申请人：Ivashchenko Andrey Alexandrovich

  公开号：US20120071493A1

  公开（公告）日：2012-03-22

  The invention relates to novel substituted 8-sulfonyl-2,3,4,5-tetrahydro-1H-γ-carbolines of the general formula 1 and their pharmaceutically acceptable salt—ligands exhibiting biological activity simultaneously towards alpha-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors, sigma receptors, norepinefrine receptors, serotonin receptors, to active components, pharmaceutical compositions, comprising as an active component novel ligands, to novel medicaments intended for treatment of conditions and diseases of central nervous system. In the general formula 1 R 1 represents a substituent selected from hydrogen, optionally substituted C 1 -C 3 alkyl or C 1 -C 4 alkyloxycarbonyl; R 2 represents a cyclic system substituent selected from hydrogen, optionally substituted C 1 -C 3 alkyl, optionally substituted C 2 -C 3 alkenyl or substituted sulfonyl; R 3 represents optionally substituted aryl or substituted amino group.

  该发明涉及一种新型的取代的8-磺酰基-2,3,4,5-四氢-1H-γ-咔啉的化合物，其一般式为1，以及它们的药用盐——配体，同时对α-肾上腺素受体、多巴胺受体、组胺受体、咪唑啉受体、西格玛受体、去甲肾上腺素受体、5-羟色胺受体表现出生物活性的配体，以及作为活性成分的新型配体组成的药物组合物，用于治疗中枢神经系统疾病和病症的新型药物。在一般式1中，R1代表从氢、可选取代的C1-C3烷基或C1-C4烷氧羰基中选择的取代基；R2代表从氢、可选取代的C1-C3烷基、可选取代的C2-C3烯基或取代的磺酰基中选择的环系统取代基；R3代表可选取代的芳基或取代的氨基团。
• [EN] POLYMERIC HYPERBRANCHED CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À DES EXCIPIENTS POLYMÉRIQUES HYPERBRANCHÉS
  申请人：ASCENDIS PHARMA AS

  公开号：WO2013024048A1

  公开（公告）日：2013-02-21

  The present invention relates to water-soluble carrier-linked prodrugs of formula (I),wherein POL is a polymeric moiety,each Hyp is independently a hyperbranched moiety,each moiety SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, m is 0 or 1, each n is independently an integer from 2 to 200 and each x is independently 0 or 1. It further relates to pharmaceutical compositions comprising said water- soluble carrier-linked prodrugs and methods of treatment.

  本发明涉及水溶性载体连接的前药，其化学式为（I），其中POL是聚合物基团，每个Hyp是独立的超支化基团，每个基团SP是独立的间隔基团，每个L是独立的可逆前药连接基团，m为0或1，每个n是独立的整数，范围从2到200，每个x是独立的0或1。此外，还涉及包含所述水溶性载体连接的前药的药物组合物和治疗方法。
• [EN] HIGH-LOADING WATER-SOLUBLE CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À DES EXCIPIENTS HYDROSOLUBLES DE FORTE CHARGE
  申请人：ASCENDIS PHARMA AS

  公开号：WO2013024047A1

  公开（公告）日：2013-02-21

  The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein B, A and Hyp form the carrier, B is a branching core, each A is independently a poly(ethylene glycol)-based polymeric chain, each Hyp is independently a branched moiety, each SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, each D is independendly a biologically active moiety, each x is independently 0 or 1, each m is independently an integer of from 2 to 64, n is an integer from 3 to 32; or the pharmaceutically acceptable salt thereof. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs, their use asmedicament or diagnostic, and methods of treatment.

  本发明涉及水溶性载体连接的前药，其化学式为(I)，其中B、A和Hyp形成载体，B是一个分支核心，每个A独立地是一条聚乙二醇基聚合链，每个Hyp独立地是一个分支基团，每个SP独立地是一个间隔基团，每个L独立地是一个可逆前药连接基团，每个D独立地是一个生物活性基团，每个x独立地为0或1，每个m独立地是从2到64的整数，n是从3到32的整数；或其药学上可接受的盐。进一步涉及包括所述水溶性载体连接的前药的药物组合物，其用作药物或诊断，以及治疗方法。