4-甲基-5,6,7,8-四氢喹唑啉 | 103796-40-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 4-甲基-5,6,7,8-四氢喹唑啉
• 英文名称: 4-methyl-5,6,7,8-tetrahydroquinazoline
• 英文别名: 4-Methyl-5,6,7,8-tetrahydro-chinazolin；4-Methyl-5,6,7,8-tetrahydroquinazoline
• CAS: 103796-40-3
• 化学式: C₉H₁₂N₂
• mdl: MFCD27957843
• 分子量: 148.208
• InChiKey: BEMZWSZJDPWKBU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.555
• 拓扑面积：
  25.8
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  2-乙酰基环己酮 、 formamide 在 palladium diacetate 碘苯 、 三苯基膦 作用下， 反应 8.0h， 以58%的产率得到4-甲基-5,6,7,8-四氢喹唑啉
  参考文献：
  名称：

  Palladium-catalysed Synthesis of Pyrimidines

  摘要：

  DOI：

  10.3987/com-05-10469

文献信息

• SILICON BASED DRUG CONJUGATES AND METHODS OF USING SAME
  申请人：BlinkBio, Inc.

  公开号：US20170202970A1

  公开（公告）日：2017-07-20

  Described herein are silicon based conjugates capable of delivering one or more payload moieties to a target cell or tissue. Contemplated conjugates may include a silicon-heteroatom core, one or more optional catalytic moieties, a targeting moiety that permits accumulation of the conjugate within a target cell or tissue, one or more payload moieties (e.g., a therapeutic agent or imaging agent), and two or more non-interfering moieties covalently bound to the silicon-heteroatom core.

  本文描述了基于硅的共轭物，能够将一个或多个有效载荷基团传递到靶细胞或组织。考虑到的共轭物可能包括一个硅-杂原子核心，一个或多个可选的催化基团，一个定位基团，允许共轭物在靶细胞或组织内积累，一个或多个有效载荷基团（例如，治疗剂或成像剂），以及与硅-杂原子核心共价结合的两个或更多个不干扰基团。
• HALOGENATED-HETEROARYL AND OTHER HETEROCYCLIC KINASE INHIBITORS, AND USES THEREOF
  申请人：iOmx Therapeutics AG

  公开号：EP3901151A1

  公开（公告）日：2021-10-27

  The invention relates to kinase inhibitors, in particular inhibitors of protein kinases including the SIK-family CSF1R, ABL/BCR-ABL, SRC, HCK, PDGFR, KIT and/or their mutants. Although structurally similar to dasatinib, the kinase inhibitors of the invention are distinctive; possessing a particular class of halogenated heteroaryls. Such kinase inhibitors can display one or more certain properties distinct to dasatinib and other structurally similar kinase inhibitors. The kinase inhibitors of the invention or pharmaceutical compositions comprising them may be used in the treatment of a disorder or condition, such as a proliferative disorder, for example, a leukaemia or solid tumour. In particular, these and other structurally similar kinase inhibitors may be used in the treatment of a proliferative disorder - such as a mixed phenotype acute leukaemia (MPAL) - characterised by (inter-alia) the presence of MEF2C protein, a human chromosomal translocation at 11q23, and/or a KMT2A fusion oncoprotein. The kinase inhibitors or pharmaceutical compositions disclosed herein may be used topically to modulate skin pigmentation in a subject, for example to impart UV protection and reduce skin cancer risk.

  该发明涉及激酶抑制剂，特别是蛋白激酶的抑制剂，包括SIK家族CSF1R，ABL/BCR-ABL，SRC，HCK，PDGFR，KIT和/或它们的突变体。尽管在结构上类似于达沙替尼，但该发明的激酶抑制剂具有独特之处；具有一类特殊的卤代杂环芳基。这种激酶抑制剂可能表现出与达沙替尼和其他在结构上相似的激酶抑制剂不同的某些性质。该发明的激酶抑制剂或包含它们的药物组合物可用于治疗某种疾病或病况，例如增生性疾病，例如白血病或实体肿瘤。特别是，这些和其他在结构上相似的激酶抑制剂可用于治疗增生性疾病 - 例如混合表型急性白血病（MPAL）- 其特征包括MEF2C蛋白的存在，11q23处的人类染色体易位，和/或KMT2A融合致癌蛋白。本文披露的激酶抑制剂或药物组合物可用于局部调节受试者的皮肤色素沉着，例如赋予UV保护并降低皮肤癌风险。
• [EN] PROTEIN KINASE C INHIBITORS AND METHODS OF THEIR USE<br/>[FR] INHIBITEURS DE PROTÉINE KINASE C ET LEURS PROCÉDÉS D'UTILISATION
  申请人：NOVARTIS AG

  公开号：WO2016020864A1

  公开（公告）日：2016-02-11

  PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.

  PKC抑制剂已被披露。这些PKC抑制剂对治疗与PKC相关的疾病，包括某些癌症，非常有用。这些PKC抑制剂在更低剂量下具有改善的疗效，可实现肿瘤的退化，提高了效力、PK特性、吸收、胃肠耐受性和激酶选择性。
• HETEROCYCLIC KINASE INHIBITORS AND USES THEREOF
  申请人：iOmx Therapeutics AG

  公开号：EP3643713A1

  公开（公告）日：2020-04-29

  The invention relates to kinase inhibitors, in particular inhibitors of protein kinases including the protein-tyrosine kinases LCK, ABL, SRC, KIT, SIK-family and/or their mutants. Although structurally similar to dasatinib, the kinase inhibitors of the invention can display one or more certain properties distinct to dasatinib. Also, the invention relates to pharmaceutical compositions that comprise one or more of the kinase inhibitors. The kinase inhibitors or pharmaceutical compositions of the invention may be used in the treatment of a disorder or condition, such as a proliferative disorder, for example, a leukaemia or solid tumour. The kinase inhibitors or pharmaceutical compositions may be used in a treatment regimen that corresponds to, is similar to or is distinct from that used with dasatinib for a corresponding disorder, and in particular may be used in a combination treatment regimen together with one or more additional therapeutic agents, such as immune-checkpoint inhibitors.

  本发明涉及激酶抑制剂，特别是蛋白激酶的抑制剂，包括LCK、ABL、SRC、KIT、SIK家族和/或它们的突变体。虽然在结构上类似于达沙替尼，但本发明的激酶抑制剂可以表现出与达沙替尼不同的一种或多种特定性质。此外，本发明涉及包含一种或多种激酶抑制剂的制药组合物。本发明的激酶抑制剂或制药组合物可用于治疗疾病或病况，例如增生性疾病，例如白血病或实体肿瘤。本发明的激酶抑制剂或制药组合物可用于与达沙替尼用于相应疾病的治疗方案相对应、类似或不同的治疗方案中，并且特别可用于与一种或多种额外的治疗药物，例如免疫检查点抑制剂一起使用的联合治疗方案中。
• Boron-Containing Diacylhydrazines
  申请人：Intrexon Corporation

  公开号：US20150322092A1

  公开（公告）日：2015-11-12

  The present disclosure provides boron-containing diacylhydrazines having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R 1 , R 2 , R 3 , R 4 , and R 5 are defined as set forth in the specification. The present disclosure also provides the use of boron-containing diacylhydrazines is ecdysone receptor-based inducible gene expression systems. Thus, the present disclosure is useful for applications such as gene therapy, treatment of disease, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable.

  本公开提供具有I式的含硼二酰肼化合物及其药学上可接受的盐和溶剂化物，其中R1、R2、R3、R4和R5的定义如规范中所述。本公开还提供了使用含硼二酰肼化合物的ecdysone受体基础的诱导基因表达系统。因此，本公开适用于基因治疗、疾病治疗、大规模生产蛋白质和抗体、基于细胞的筛选测定、功能基因组学、蛋白质组学、代谢组学和调控转基因生物的特征等应用，其中需要控制基因表达水平。