1-Tert-butyl-3-pyrrolidinamine | 1096325-48-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 1-Tert-butyl-3-pyrrolidinamine
• 英文别名: 1-tert-butylpyrrolidin-3-amine
• CAS: 1096325-48-2
• 化学式: C₈H₁₈N₂
• 分子量: 142.24
• InChiKey: UTEZMBDWXGWOQJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  29.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 4 POLYPEPTIDES
  申请人：Arvinas, Inc.

  公开号：US20190151295A1

  公开（公告）日：2019-05-23

  The present disclosure relates to bifunctional compounds, which find utility as modulators of Interleukin-1 Receptor-Associated Kinase 4 (IRAK-4); the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hppel-Lindau, cereblon, ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds the target protein, 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 are treated or prevented with compounds and compositions of the present disclosure.

  本公开涉及双功能化合物，其作为白细胞介素-1受体相关激酶4（IRAK-4；目标蛋白）的调节剂具有实用性。具体而言，本公开涉及包含一端结合E3泛素连接酶的Von Hppel-Lindau、cereblon配体的双功能化合物，另一端结合目标蛋白的部分，使得目标蛋白靠近泛素连接酶以实现目标蛋白的降解（和抑制）。本公开展示了与目标蛋白的降解/抑制相关的广泛药理活性。本公开的化合物和组合物用于治疗或预防由目标蛋白聚集或积累导致的疾病或紊乱。
• Derivatives of Amphotericin B
  申请人：Revolution Medicines, Inc.

  公开号：US20160304548A1

  公开（公告）日：2016-10-20

  Disclosed are derivatives of amphotericin B (AmB) characterized by improved therapeutic index compared to AmB. The AmB derivatives include C16 ureas, carbamates, and amides according to Formula (I); C3′-substituted C16 ureas, carbamates, and amides according to Formula (II); C16 acyls according to Formula (III); C2′epi-C16 ureas, carbamates, and amides according to Formula (IV); and C16 oxazolidinone derivatives according to Formula (V). Also disclosed are pharmaceutical compositions comprising the AmB derivatives, and therapeutic methods of using the AmB derivatives.

  披露了与AmB相比具有改善的治疗指数的Amphotericin B（AmB）衍生物。这些AmB衍生物包括根据公式（I）的C16脲、碳酸酯和酰胺；根据公式（II）的C3′-取代的C16脲、碳酸酯和酰胺；根据公式（III）的C16酰基；根据公式（IV）的C2′epi-C16脲、碳酸酯和酰胺；以及根据公式（V）的C16噁唑烷酮衍生物。还披露了包括这些AmB衍生物的药物组合物，以及使用这些AmB衍生物的治疗方法。
• FURO- AND THIENO-PYRIDINE CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS
  申请人：Incyte Corporation

  公开号：US20150057265A1

  公开（公告）日：2015-02-26

  The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

  本公开描述了呋喃和噻吩吡啶羧酰胺化合物，以及它们的组合物和使用方法。这些化合物抑制Pim激酶的活性，并且在治疗与Pim激酶活性相关的疾病方面具有用处，例如癌症和其他疾病。
• [EN] INHIBITORS OF BRUTON'S TYROSINE KINASE<br/>[FR] INHIBITEURS DE LA TYROSINE KINASE DE BRUTON
  申请人：PHARMACYCLICS LLC

  公开号：WO2016004272A1

  公开（公告）日：2016-01-07

  Disclosed herein are compounds that inhibit Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

  本文披露了抑制布鲁顿酪氨酸激酶（Btk）的化合物。还描述了Btk的不可逆抑制剂。此外，还描述了Btk的可逆抑制剂。还披露了包括这些化合物的药物组合物。披露了使用Btk抑制剂的方法，单独或与其他治疗剂联合治疗自身免疫疾病或症状、异源免疫疾病或症状、癌症（包括淋巴瘤）和炎症性疾病或症状。
• CCR2 INHIBITORS AND METHODS OF USE THEREOF
  申请人：Basak Arindrajit

  公开号：US20100234364A1

  公开（公告）日：2010-09-16

  Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists, and as controls in assays for the identification of CCR9 antagonists.

  提供了作为CCR2或CCR9受体强效拮抗剂的化合物。动物实验表明，这些化合物对于治疗炎症非常有效，而炎症是CCR2和CCR9的典型疾病。这些化合物通常是芳基磺酰胺衍生物，在制药组合物、治疗CCR2介导疾病的方法、治疗CCR9介导疾病的方法、作为CCR2拮抗剂鉴定的检测中的对照物，以及作为CCR9拮抗剂鉴定的检测中的对照物中非常有用。