O-Benzoyl-L-malic acid | 22138-51-8

• 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: O-Benzoyl-L-malic acid
• 英文别名: (2S)-2-benzoyloxybutanedioic acid
• CAS: 22138-51-8
• 化学式: C₁₁H₁₀O₆
• 分子量: 238.19
• InChiKey: NVPJTXMOQCANSN-QMMMGPOBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  17
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  101
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• [EN] CRYSTALLINE FORMS OF A LYSYL OXIDASE-LIKE 2 INHIBITOR AND METHODS OF MAKING<br/>[FR] FORMES CRISTALLINES D'UN INHIBITEUR DE LYSYL OXYDASE DE TYPE 2 ET LEURS PROCÉDÉS DE FABRICATION
  申请人：PHARMAKEA INC

  公开号：WO2018048943A1

  公开（公告）日：2018-03-15

  Described herein are crystalline forms of pharmaceutically acceptable salts of the lysyl oxidase-like 2 (LOXL2) inhibitor (3-(4-(aminomethyl)-6-(trifluoromethyl)pyridin-2-yloxy)phenyl)((3R,4R)-3-fluoro-4-hydroxypyrrolidin-1-yl)methanone. Also described are methods of making the LOXL2 inhibitor, pharmaceutical compositions and medicaments comprising the LOXL2 inhibitor, and methods of using the LOXL2 inhibitor in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.

  本文描述了赖氨酸氧化酶样2（LOXL2）抑制剂（3-（4-（氨甲基）-6-三氟甲基吡啶-2-氧基）苯基）（（3R,4R）-3-氟-4-羟基吡咯烷-1-基）的药用盐的晶体形式。还描述了制备LOXL2抑制剂的方法，包含LOXL2抑制剂的药物组合物和药物，以及在治疗与LOXL2活性相关的状况、疾病或障碍中使用LOXL2抑制剂的方法。
• [EN] PROCESS FOR THE SYNTHESIS OF 2-[(2S)-1-AZABICYCLO[2.2.2]OCT-2-YL]-6- (3-METHYL-1 H-PYRAZOL-4-YL)THIENO[3,2-D]PYRIMIDIN-4(3H)-ONE<br/>[FR] PROCÉDÉS DE SYNTHÈSE DE 2-[(2S)-1-AZABICYCLO[2.2.2]OCT-2-YL]-6- (3-MÉTHYL-1 H-PYRAZOL-4-YL)THIÉNO[3,2-D]PYRIMIDIN-4(3H)-ONE
  申请人：TAKEDA PHARMACEUTICALS CO

  公开号：WO2019194319A1

  公开（公告）日：2019-10-10

  The present invention provides processes and synthetic intermediates for the synthesis of 2-[(2S)-l- azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-lH-pyrazol-4- yl)thieno[3,2-d]pyrimidin-4 3H) -one or a salt, hydrate, or tautomer thereof, or any combination thereof, which are Cdc7 kinase inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with Cdc7 activity.

  本发明提供了合成2-[(2S)-1-氮杂双环[2.2.2]辛-2-基]-6-(3-甲基-1H-吡唑-4-基)噻唑并[3,2-d]嘧啶-4(3H)-酮或其盐、水合物或互变异构体的过程和合成中间体，这些化合物是Cdc7激酶抑制剂，可用于治疗细胞增殖紊乱，特别是癌症，以及与Cdc7活性相关的其他疾病。
• POLYCYCLIC COMPOUND
  申请人：Eisai R&D Management Co., Ltd.

  公开号：EP2181992A1

  公开（公告）日：2010-05-05

  Disclosed is a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, which is effective as a therapeutic or prophylactic agent for a disease induced by Aβ, wherein Ar1 represents an imidazolyl group which may be substituted with a C1-6 alkyl group, or the like; Ar2 represents a phenyl group which may be substituted with a C1-6 alkoxy group, or the like; X1 represents a double bond, or the like; and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, or the like.

  本发明公开了一种由式 (I) 表示的化合物： 或其药理上可接受的盐，可有效治疗或预防由 Aβ 诱导的疾病，其中 Ar1 代表咪唑基团，可被 C1-6 烷基或类似基团取代；Ar2 代表苯基，可被 C1-6 烷氧基或类似基团取代；X1 代表双键或类似基团；Het 代表三唑基团或类似基团，可被 C1-6 烷基或类似基团取代。
• PYRIDOPYRIMIDINONE COMPOUND AND APPLICATION THEREOF
  申请人：Bebetter Med Inc.

  公开号：EP4101852A1

  公开（公告）日：2022-12-14

  The present disclosure provides the Pyridopyrimidinone compounds having the structure represented by the general Formula (II) and applications thereof. Studies have shown that the compounds provided by the present disclosure can effectively inhibit the KRAS G12C mutation. KRAS mutation accounts for a large proportion of tumors, and currently there is no approved drug for its treatment. The compounds provided by the present disclosure have the potential to become a therapeutic medicine for malignant tumors (especially non-small cell lung cancer (NSCLC) and colorectal cancer) haboring KRAS G12C mutation, and have great application value.

  本公开提供了具有通式（II）所代表结构的吡啶嘧啶酮化合物及其应用。研究表明，本公开提供的化合物可以有效抑制 KRAS G12C 突变。KRAS突变在肿瘤中占很大比例，目前还没有获批的治疗药物。本发明提供的化合物有望成为携带KRAS G12C突变的恶性肿瘤（尤其是非小细胞肺癌（NSCLC）和结直肠癌）的治疗药物，具有很大的应用价值。
• Crystalline forms of a lysyl oxidase-like 2 inhibitor and methods of making
  申请人：PHARMAKEA, INC.

  公开号：US10774069B2

  公开（公告）日：2020-09-15

  Described herein are crystalline forms of pharmaceutically acceptable salts of the lysyl oxidase-like 2 (LOXL2) inhibitor (3-(4-(aminomethyl)-6-(trifluoromethyl)pyridin-2-yloxy)phenyl)((3R,4R)-3-fluoro-4-hydroxypyrrolidin-1-yl)methanone. Also described are methods of making the LOXL2 inhibitor, pharmaceutical compositions and medicaments comprising the LOXL2 inhibitor, and methods of using the LOXL2 inhibitor in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.

  本文描述了赖氨酰氧化酶样2（LOXL2）抑制剂（3-(4-(氨基甲基)-6-(三氟甲基)吡啶-2-基氧基)苯基)((3R,4R)-3-氟-4-羟基吡咯烷-1-基)甲酮的药学上可接受的盐的结晶形式。还描述了制造LOXL2抑制剂的方法，包含LOXL2抑制剂的药物组合物和药物，以及使用LOXL2抑制剂治疗与LOXL2活性相关的病症、疾病或紊乱的方法。