二氟甲基鸟氨酸 | 66640-93-5

• 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
• 中文名称: 二氟甲基鸟氨酸
• 中文别名: 2,5-二氨基-2-（二氟甲基）戊酸
• 英文名称: L-Eflornithine
• 英文别名: (2S)-2,5-diamino-2-(difluoromethyl)pentanoic acid
• CAS: 66640-93-5
• 化学式: C₆H₁₂F₂N₂O₂
• 分子量: 182.17
• InChiKey: VLCYCQAOQCDTCN-ZCFIWIBFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.9
• 重原子数：
  12
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  89.3
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  L-依氟鸟氨酸盐酸盐 以 甲醇 为溶剂， 生成 二氟甲基鸟氨酸
  参考文献：
  名称：

  Process for the preparation of (-)-&agr;-(difluoromethyl)ornithine-monohydrochloride monohydrate

  摘要：

  (±)-α-(二氟甲基)-鸟氨酸可使用(−)-O,O′-二对甲苯基-L-酒石酸分离其异构体。(−)-α-(二氟甲基)-鸟氨酸单盐酸盐一水合物，特别是(−)-异构体，是鸟氨酸脱羧酶的抑制剂，因此具有许多药理作用。

  公开号：

  US06462229B1

文献信息

• Eflornithine Prodrugs, Conjugates and Salts, and Methods of Use Thereof
  申请人：Xu Feng

  公开号：US20100120727A1

  公开（公告）日：2010-05-13

  In one aspect, the present invention provides a composition of a covalent conjugate of an eflornithine analog with an anti-inflammatory drug. In another aspect, the present invention provides a composition of an eflornithine prodrug. In another aspect, the present invention provides a composition of an eflornithine or its derivatives aspirin salt. In another aspect, the present invention provides methods for treating or preventing cancer using the conjugates or salts of eflornithine analogs or eflornithine prodrugs.

  在一个方面，本发明提供了一种氟硝西汀类似物与抗炎药物的共价结合物的组合物。在另一个方面，本发明提供了一种氟硝西汀前药的组合物。在另一个方面，本发明提供了一种氟硝西汀或其衍生物水杨酸盐的组合物。在另一个方面，本发明提供了使用氟硝西汀类似物或氟硝西汀前药的共轭物或盐来治疗或预防癌症的方法。
• Substituted 1-benzoyl-3-cyano-pyrrolo [1,2-a] quinolines and analogs as activators of caspases and inducers of apoptosis
  申请人：Cai Xiong Sui

  公开号：US20050014759A1

  公开（公告）日：2005-01-20

  The present invention is directed to substituted 1-benzoyl-3-cyano-pyrrolo[1,2-a]quinolines and analogs thereof, represented by the general Formula I: wherein R 1 —R 8 , L, Q, dash line and Ar are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

  本发明涉及取代的1-苯甲酰基-3-氰基-吡咯并[1,2-a]喹啉及其类似物，由通用式I表示： 其中R1-R8，L，Q，虚线和Ar在此定义。本发明还涉及发现具有式I的化合物是caspase的激活剂和凋亡诱导剂。因此，本发明的caspase激活剂和凋亡诱导剂可用于诱导在各种临床病况中发生未受控制的异常细胞生长和扩散的细胞死亡。
• Spirocyclic compounds
  申请人：Berk C. Scott

  公开号：US20070117824A1

  公开（公告）日：2007-05-24

  The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.

  本发明涉及一类新型的取代螺环化合物。这些化合物可以抑制组蛋白去乙酰化酶，并适用于在选择性诱导终末分化、阻止肿瘤细胞生长和/或凋亡的过程中使用，从而抑制这些细胞的增殖。因此，本发明的化合物在治疗具有肿瘤特征的患者方面是有用的，这些肿瘤具有肿瘤细胞的增殖。本发明的化合物还可能在预防和治疗TRX介导的疾病方面有用，例如自身免疫、过敏和炎症性疾病，以及预防和/或治疗中枢神经系统（CNS）疾病，如神经退行性疾病。本发明还提供了包括本发明化合物的药物组合物和这些药物组合物的安全用药方案，这些方案易于遵循，并在体内产生这些化合物的治疗有效量。
• Active salt forms with tyrosine kinase activity
  申请人：——

  公开号：US20040023978A1

  公开（公告）日：2004-02-05

  The present invention relates to orally active salt forms of the mesylate salt of 4-[2-(5-cyano-thiazol-2-ylamino)-pyridin-4-ylmethyl]-piperazine-1-carboxylic acid methylamide which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, retinal ischemia, macular edema, inflammatory diseases, and the like in mammals.

  本发明涉及口服活性盐形式的甲磺酸盐，其抑制、调节和/或调控酪氨酸激酶信号传导的4-[2-(5-氰基噻唑-2-基氨基)-吡啶-4-基甲基]-哌嗪-1-羧酸甲酰胺，含有这些化合物的组合物，以及使用它们治疗酪氨酸激酶依赖性疾病和症状的方法，如血管生成、癌症、肿瘤生长、动脉粥样硬化、老年性黄斑变性、糖尿病视网膜病变、视网膜缺血、黄斑水肿、炎症性疾病等哺乳动物。
• Polymorphs with tyrosine kinase activity
  申请人：——

  公开号：US20040023980A1

  公开（公告）日：2004-02-05

  The present invention relates to active polymorphs of 4-[2-(5-cyano-thiazol-2-ylamino)-pyridin-4-ylmethyl]-piperazine-1-carboxylic acid methylamide which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angio-genesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, retinal ischemia, macular edema, inflammatory diseases, and the like in mammals.

  本发明涉及活性多型体4-[2-(5-氰基噻唑-2-基氨基)-吡啶-4-基甲基]-哌嗪-1-羧酸甲酰胺，其抑制、调节和/或调控酪氨酸激酶信号传导，含有这些化合物的组合物，以及使用它们治疗酪氨酸激酶依赖性疾病和症状的方法，如血管生成、癌症、肿瘤生长、动脉粥样硬化、老年性黄斑变性、糖尿病视网膜病变、视网膜缺血、黄斑水肿、炎症性疾病等在哺乳动物中。