1-Carbamoylmethyl-4-(β-hydroxyaethyl)piperazin | 90228-11-8

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 1-Carbamoylmethyl-4-(β-hydroxyaethyl)piperazin
• 英文别名: 2-[4-(2-Hydroxyethyl)piperazin-1-yl]acetamide
• CAS: 90228-11-8
• 化学式: C₈H₁₇N₃O₂
• mdl: MFCD11505330
• 分子量: 187.242
• InChiKey: OJEUKFXLIICKDY-UHFFFAOYSA-N

物化性质

• 熔点：
  92-93 °C
• 沸点：
  397.0±32.0 °C(Predicted)
• 密度：
  1.155±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.7
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.875
• 拓扑面积：
  69.8
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Polyene macrolide derivatives
  申请人：S P A SOCIETA' PRODOTTI ANTIBIOTICI S.p.a.

  公开号：EP0434943A1

  公开（公告）日：1991-07-03

  There has been prepared a series of secondary and tertiary amide derivatives of the polyene antibiotic partricin as well as of its single components, partricin A and B, having radicals on the amide nitrogen, said radicals being preferab­ly substituted, in turn, with various amine groups. The syn­thesis has been carried out by reacting the C-18 carboxyl of the polyene with suitable amines, in the presence of diphenyl phosphorazidate as activator. From said amines, especially those substituted with basic groups, many salts with a good water solubility have been prepared by reacting them with pharmacologically compatible acids. It has been shown that many amines and related salts are more active than, or as active as, the starting product as antimycotic and antiprotozoan agents, while being less toxic and less hemolytic, and can therefore find a useful applica­tion in the clinical and veterinary therapy. The compounds can also be used in the treatment of hypercholesteremia and hyperlipemia conditions and of some steroid hormones unbalan­ces, as well as in the pharmacological therapy of hyper­trophic prostate, and in the treatment of lipid envelope virus infections.

  现已制备出一系列聚烯类抗生素部分霉素及其单一成分部分霉素 A 和 B 的仲酰胺和叔酰胺衍生物，这些衍生物的酰胺氮上具有基团，所述基团最好依次被各种胺基团取代。合成的方法是：在作为活化剂的磷酸二苯酯存在下，将聚烯的 C-18 羧基与合适的胺反应。 上述胺类，特别是那些被碱性基团取代的胺类，通过与药理学上相容的酸反应，制备出了许多水溶性良好的盐类。 研究表明，许多胺和相关盐类作为抗霉菌剂和抗原虫剂的活性高于或等同于起始产物，同时毒性和溶血性较低，因此可以在临床和兽医治疗中得到有用的应用。这些化合物还可用于治疗高胆固醇血症、高血脂症和某些类固醇激素失衡，以及肥大性前列腺的药物治疗和脂质包膜病毒感染的治疗。
• THIENOPYRIMIDINE COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND APPLICATIONS
  申请人：Hongyun Biotech Co., Ltd.

  公开号：EP3498716A1

  公开（公告）日：2019-06-19

  The present invention relates to thienopyrimidine compound, preparation method thereof, pharmaceutical composition and use thereof, and in particular to a type of compounds having ALK and/or c-Met selective inhibitory activity, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for preventing or treating a disease associated with anaplastic lymphoma kinase in vivo, and in the manufacture of a medicament for preventing or treating a disease associated with angiogenesis or cancer metastasis, in particular in the manufacture of a medicament for preventing or treating tumor growth and metastasis.

  本发明涉及噻吩嘧啶化合物、其制备方法、药物组合物及其用途，特别是涉及一种具有ALK和/或c-Met选择性抑制活性的化合物、其制备方法、包含其的药物组合物、以及这些化合物在制造预防或治疗体内无性淋巴瘤激酶相关疾病的药物中的用途，以及在制造预防或治疗血管生成或癌症转移相关疾病的药物中的用途，特别是在制造预防或治疗肿瘤生长和转移的药物中的用途。
• Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
  申请人：Arvinas, Inc.

  公开号：US10723717B2

  公开（公告）日：2020-07-28

  The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.

  本公开涉及双功能化合物，它们可用作快速加速纤维肉瘤（RAF，如c-RAF、A-RAF和/或B-RAF；靶蛋白）的调节剂。特别是，本公开内容涉及双功能化合物，其一端含有与相应 E3 泛素连接酶结合的 Von Hippel-Lindau、cereblon、抑制细胞凋亡蛋白或小鼠双敏同源物 2 配体，另一端含有与靶蛋白 RAF 结合的分子，从而将靶蛋白置于泛素连接酶附近，以实现对靶蛋白的降解（和抑制）。本公开物具有与降解/抑制靶蛋白相关的广泛药理活性。本公开的化合物和组合物可以治疗或预防由于靶蛋白的聚集或积聚或靶蛋白的组成性激活而导致的疾病或失调。
• Thienopyrimidine compound, preparation method thereof, pharmaceutical composition and application thereof
  申请人：HONGYUN BIOTECH CO., LTD.

  公开号：US11078213B2

  公开（公告）日：2021-08-03

  The present invention relates to thienopyrimidine compound, preparation method thereof, pharmaceutical composition and use thereof, and in particular to a type of compounds having ALK and/or c-Met selective inhibitory activity, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for preventing or treating a disease associated with anaplastic lymphoma kinase in vivo, and in the manufacture of a medicament for preventing or treating a disease associated with angiogenesis or cancer metastasis, in particular in the manufacture of a medicament for preventing or treating tumor growth and metastasis.

  本发明涉及噻吩嘧啶化合物、其制备方法、药物组合物及其用途，特别是涉及一种具有ALK和/或c-Met选择性抑制活性的化合物、其制备方法、包含其的药物组合物、以及这些化合物在制造预防或治疗体内无性淋巴瘤激酶相关疾病的药物中的用途，以及在制造预防或治疗血管生成或癌症转移相关疾病的药物中的用途，特别是在制造预防或治疗肿瘤生长和转移的药物中的用途。
• METHOD OF TREATING MUSCULAR DEGRADATION
  申请人：Rigel Pharmaceuticals, Inc.

  公开号：US20130310340A1

  公开（公告）日：2013-11-21

  A method for treating muscular deterioration is disclosed. Also disclosed are embodiments of a compound, and compositions comprising the compound, for inhibiting muscular deterioriation, including atrophy, dystrophy, and cachexia, such as may result from ventilation.