benzhydrylproline

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: benzhydrylproline
• 英文别名: N-diphenylmethylproline；1-Benzhydrylpyrrolidine-2-carboxylic acid
• 化学式: C₁₈H₁₉NO₂
• 分子量: 281.354
• InChiKey: OFPWENIUCJQNPC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  benzhydrylproline 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 以900 mg的产率得到(1-benzhydrylpyrrolidin-2-yl)methanol
  参考文献：
  名称：

  [EN] PRODRUGS FOR SUSTAINED RELEASING THERAPEUTIC AGENTS AND USES THEREOF
  [FR] PROMÉDICAMENTS POUR AGENTS THÉRAPEUTIQUES À LIBÉRATION PROLONGÉE ET LEURS UTILISATIONS

  摘要：

  提供了用于缓释治疗剂的前药，以及使用这种前药治疗疾病的方法。

  公开号：

  WO2022083679A1
• 作为产物：
  描述：

  methyl benzhydrylprolinate 在 sodium hydroxide 作用下， 以 甲醇 为溶剂， 反应 17.0h， 以7.8 g的产率得到benzhydrylproline
  参考文献：
  名称：

  [EN] PRODRUGS FOR SUSTAINED RELEASING THERAPEUTIC AGENTS AND USES THEREOF
  [FR] PROMÉDICAMENTS POUR AGENTS THÉRAPEUTIQUES À LIBÉRATION PROLONGÉE ET LEURS UTILISATIONS

  摘要：

  提供了用于缓释治疗剂的前药，以及使用这种前药治疗疾病的方法。

  公开号：

  WO2022083679A1

文献信息

• Collection of traceable compounds and uses thereof
  申请人：Centre National de la Recherche Scientifique (CNRS)

  公开号：US07745413B2

  公开（公告）日：2010-06-29

  The use of a collection of compounds of general formula (I), wherein: n is 0 or 1; p represents an integer between 1 and 6; r represents an integer between 1 and 12; R1 and R′1 represent in particular a hydrogen atom; R2 represents an amino acid side chain or an amino acid derivative; R3 represents a group derived from a carboxylic acid, bearing a basic entity; R4 represents in particular an alkyl group containing 1 to 10 carbon atoms; and A represents a hydrogen atom, a protecting group or a tracing group, in particular a fluorophor, a coloring agent or a quencher, for determining, through binding studies, ligands of receptors whose ligand is unknown or whose ligand useful for carrying out specific affinity binding assays is unknown.

  使用一系列通式（I）的化合物，其中：n为0或1；p表示1到6之间的整数；r表示1到12之间的整数；R1和R′1特别表示氢原子；R2表示氨基酸侧链或氨基酸衍生物；R3表示从羧酸衍生的带有碱性实体的基团；R4特别表示含有1到10个碳原子的烷基基团；A表示氢原子、保护基或示踪基，特别是荧光染料、着色剂或猝灭剂，用于通过结合研究确定受体配体的配体是未知的或用于进行特定亲和结合测定的配体是未知的。
• Collection of Traceable Compounds and Uses Thereof
  申请人：Hibert Marcel Francois Louis

  公开号：US20080176763A1

  公开（公告）日：2008-07-24

  The invention concerns the use of a collection of compounds of general formula (I), wherein: n is 0 or 1; p represents an integer between 1 and 6; r represents an integer between 1 and 12; R 1 and R′ 1 represent in particular a hydrogen atom; R 2 represents an amino acid side chain or an amino acid derivative; R 3 represents a group derived from a carboxylic acid, bearing a basic entity; R 4 represents in particular an alkyl group containing 1 to 10 carbon atoms; and A represents a hydrogen atom, a protecting group or a tracing group, in particular a fluorophor, a colouring agent or a quencher, for determining, through binding studies, ligands of receptors whose ligand is unknown or whose ligand useful for carrying out specific affinity binding assays is unknown.

  本发明涉及使用一系列化合物的方法，其通式为（I），其中：n为0或1；p表示1到6之间的整数；r表示1到12之间的整数；R1和R′1特别表示氢原子；R2表示氨基酸侧链或氨基酸衍生物；R3表示从羧酸衍生的带有碱性基团的基团；R4特别表示含有1到10个碳原子的烷基基团；A表示氢原子、保护基或示踪基，特别是荧光团、着色剂或淬灭剂，用于通过结合研究确定受体的配体，其配体未知或用于进行特定亲和结合测定的配体未知。
• Substrates and inhibitors of prolyl oligopeptidase and methods of use thereof
  申请人：The Board of Regents of the University of Oklahoma

  公开号：US10155789B2

  公开（公告）日：2018-12-18

  Inhibitors of fibroblast activation protein alpha (FAP) and Prolyl Oligopeptidase (POP) are disclosed, along with their use in various therapies related to conditions, diseases, and disorders involving abnormal cell proliferation such as malignancies and angiogenesis, and in neural disorders such as Alzheimer's disease. Stalk portions of the inhibitor molecules, and substrates of FAP and POP, are also disclosed and may be used, for example, in screening methods for identifying such inhibitors.

  本研究公开了成纤维细胞活化蛋白α（FAP）和脯氨酰寡肽酶（POP）的抑制剂，以及它们在涉及异常细胞增殖（如恶性肿瘤和血管生成）的条件、疾病和紊乱以及神经紊乱（如阿尔茨海默病）的各种疗法中的用途。此外，还公开了抑制剂分子的柄部分以及 FAP 和 POP 的底物，例如，可用于识别此类抑制剂的筛选方法。
• Method of inhibiting activity of cell surface fibroblast activation protein alpha
  申请人：The Board of Regents of the University of Oklahoma

  公开号：US10174077B2

  公开（公告）日：2019-01-08

  The presently disclosed inventive concept(s) include inhibitors of antiplasmin cleaving enzyme (APCE) and fibroblast activation protein alpha (FAP) which can be used in various therapies related to disorders of fibrin and α2-antiplasmin and abnormal cell proliferation. The presently disclosed inventive concept(s) also include substrates of APCE and FAP, which may be used, for example, in screening methods for identifying such inhibitors. The presently disclosed inventive concept(s) further include, but are not limited to, methods of treating or inhibiting atherosclerosis and thrombus disorders by altering the ratios of types of plasma α2-antiplasmin and to methods of treating conditions involving abnormal cell proliferation such as cancers.

  本发明公开的发明概念包括抗蛋白溶解酶（APCE）和成纤维细胞活化蛋白α（FAP）的抑制剂，这些抑制剂可用于与纤维蛋白和α2-抗蛋白溶解酶紊乱以及异常细胞增殖有关的各种治疗中。本发明公开的发明构思还包括 APCE 和 FAP 的底物，例如，可用于鉴定此类抑制剂的筛选方法中。目前公开的发明概念还包括但不限于通过改变血浆α2-抗蛋白酶类型的比例来治疗或抑制动脉粥样硬化和血栓疾病的方法，以及治疗涉及异常细胞增殖（如癌症）的病症的方法。
• Acceleration of Mycobacterium growth
  申请人：ST GEORGE'S HOSPITAL MEDICAL SCHOOL

  公开号：US10633630B2

  公开（公告）日：2020-04-28

  The invention is in the field of growth of Mycobacteria. In particular, agents have been identified which enhance the growth of Mycobacterial species, which are naturally slow-growing. Such agents can therefore be used in the identification of Mycobacteria and in the diagnosis of Mycobacterial infections.

  本发明属于分枝杆菌生长领域。特别是，已经发现了能促进自然生长缓慢的分枝杆菌生长的制剂。因此，这些制剂可用于分枝杆菌的鉴定和分枝杆菌感染的诊断。