Carbamic acid, (5-methoxypentyl)-, 1,1-dimethylethyl ester | 174699-44-6

• 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: Carbamic acid, (5-methoxypentyl)-, 1,1-dimethylethyl ester
• 英文别名: tert-butyl N-(5-methoxypentyl)carbamate
• CAS: 174699-44-6
• 化学式: C₁₁H₂₃NO₃
• 分子量: 217.31
• InChiKey: MQMIMXPPNOPRTC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  15
• 可旋转键数：
  8
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.91
• 拓扑面积：
  47.6
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
  申请人：Arvinas Operations, Inc.

  公开号：EP3660004A1

  公开（公告）日：2020-06-03

  The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.

  本公开涉及双功能化合物，它们可用于降解和（抑制）雄激素受体。特别是，本公开涉及的化合物一端含有与 E3 泛素连接酶结合的脑龙配体，另一端含有与雄激素受体结合的分子，这样雄激素受体就被置于泛素连接酶附近，从而实现对雄激素受体的降解（和抑制）。本公开的化合物具有广泛的药理活性，与雄激素受体的降解/抑制作用相一致。
• Compounds and methods for the targeted degradation of androgen receptor
  申请人：Arvinas, Inc.

  公开号：US11352351B2

  公开（公告）日：2022-06-07

  The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.

  本发明涉及双功能化合物，可用于降解和（抑制）雄激素受体。特别是，本发明涉及的化合物一端含有与泛素连接酶结合的 VHL 配体，另一端含有与雄激素受体结合的分子，从而使雄激素受体靠近泛素连接酶，以实现对雄激素受体的降解（和抑制）。本发明显示了与根据本发明的化合物相关的广泛药理活性，与雄激素受体的降解/抑制一致。
• EPOXYSUCCINIC ACID DERIVATIVES, THEIR PRODUCTION AND USE
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP0763029A1

  公开（公告）日：1997-03-19
• US5679708A
  申请人：——

  公开号：US5679708A

  公开（公告）日：1997-10-21
• [EN] EPOXYSUCCINIC ACID DERIVATIVES, THEIR PRODUCTION AND USE<br/>[FR] DERIVES D'ACIDE EPOXYSUCCINIQUE, LEUR PRODUCTION ET LEUR UTILISATION
  申请人：TAKEDA CHEMICAL INDUSTRIES, LTD.

  公开号：WO1995032954A1

  公开（公告）日：1995-12-07

  (EN) The present invention relates to a compound of formula (I), wherein R1 stands for an optionally esterified or amidated carboxyl group, X stands for an optionally substituted divalent hydrocarbon residue, R2 stands for hydrogen or an optionally substituted hydrocabon residue, R3 stands for an alkyl group which is substituted with a group bonded through O or S(O)n wherein n is 0, 1 or 2, with a proviso that when the partial structural formula: -NH-X-CO- is leucine residue, R3 is not 3-hydroxy-3-methylbutyl group nor 4-hydroxy-3-methylbutyl group, or a salt thereof, which is useful as prophylactic and therapeutic agents of bone diseases and as inhibitory agents of thiol protease.(FR) La présente invention concerne un composé représenté par la formule générale (I). Dans cette formule, R1 correspond à un groupe carboxyle éventuellement estérifié ou amidé, X correspond à un hydrocarbure résiduel bivalent éventuellement substitué, R2 représente un hydrogène ou un hydrocarbure résiduel éventuellement substitué, R3 représente un groupe alkyle qui est substitué par un groupe à liaison O ou S(O)n où 'n' vaut 0, 1 ou 2, sous réserve que lorsque la structure partielle '-NH-X-CO-' de la formule générale est une leucine résiduelle, R3 n'est ni un groupe 3-hydroxy-3-méthylbutyle, ni un groupe 4-hydroxy-3-méthylbutyle, ni l'un de leurs sels. Ce composé est utile en tant qu'agent prophylactique et thérapeutique dans les affections osseuses et en tant qu'agent inhibiteur de la protéase thiol.