[(3S,4R)-4-hydroxypiperidin-3-yl]carbamic acid

• 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: [(3S,4R)-4-hydroxypiperidin-3-yl]carbamic acid
• 化学式: C₆H₁₂N₂O₃
• 分子量: 160.17
• InChiKey: YLIYEUGUOLVKHG-CRCLSJGQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.5
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  81.6
• 氢给体数：
  4
• 氢受体数：
  4

文献信息

• [EN] SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS<br/>[FR] COMPOSÉS DE PYRAZOLO[1,5-A]PYRIDINE SUBSTITUÉS EN TANT QU'INHIBITEURS DE LA KINASE RET
  申请人：ANDREWS STEVEN W

  公开号：WO2018071454A1

  公开（公告）日：2018-04-19

  Provided herein are compounds of the Formula I: (I) or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X1, X2, X3, X4, Ring D, E, Ra, Rb, n and m have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

  本文提供了Formula I的化合物：(I)或其药用可接受的盐或溶剂，其中A、B、X1、X2、X3、X4、环D、E、Ra、Rb、n和m的含义如规范中所述，它们是RET激酶的抑制剂，并且在治疗和预防可以用RET激酶抑制剂治疗的疾病中非常有用，包括与RET相关的疾病和紊乱。
• [EN] BENZOIMIDAZOLE DERIVATIVES AS PAD4 INHIBITORS<br/>[FR] DÉRIVÉS DE BENZOIMIDAZOLE EN TANT QU'INHIBITEURS DE PAD4
  申请人：GLAXOSMITHKLINE IP DEV LTD

  公开号：WO2016185279A1

  公开（公告）日：2016-11-24

  Compounds of formula (I): wherein X, Y, R1 and R3-R11 are as herein defined, and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.

  式(I)的化合物：其中X、Y、R1和R3-R11如本文所定义，并其盐为PAD4抑制剂，可能在治疗各种疾病中有用，例如类风湿关节炎、血管炎、系统性红斑狼疮、溃疡性结肠炎、癌症、囊性纤维化、哮喘、皮肤红斑狼疮和牛皮癣。
• [EN] MACROCYCLIC INHIBITORS OF PEPTIDYLARGININE DEIMINASES<br/>[FR] INHIBITEURS MACROCYCLIQUES DE PEPTIDYLARGININE DÉIMINASES
  申请人：GILEAD SCIENCES INC

  公开号：WO2021222353A1

  公开（公告）日：2021-11-04

  The present disclosure relates to novel compounds for use in therapeutic treatement of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.

  本公开涉及用于治疗与肽精氨酸脱亚氨酶（PADs）相关的疾病的新化合物，例如肽精氨酸脱亚氨酶类型4（PAD4）。本公开还涉及用于制备这些化合物的过程和中间体，使用这些化合物的方法以及包含所述化合物的药物组合物。
• [EN] 2 - (AZAINDOL- 2 -YL) BENZ IMIDAZOLES AS PAD4 INHIBITORS<br/>[FR] 2-(AZAINDOL-2-YL)BENZIMIDAZOLES UTILISÉS COMME INHIBITEURS DE PAD4
  申请人：GLAXO GROUP LTD

  公开号：WO2014015905A1

  公开（公告）日：2014-01-30

  Compounds of formula (I) wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O-, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6alkyl; A is C-R5 or N; B is C-R6 or N; D is C-R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.

  式（I）的化合物，其中; R1为氢或C1-6烷基; R2为氢，C1-6烷基，全氟甲基C0-5烷基-O-，或C1-6烷氧基; R3为氢，C1-6烷基，或C1-6烷氧基C1-6烷基; R4为氢，C1-6烷基，全氟甲基C1-6烷基; 或未取代的C3-6环烷基C1-6烷基; A为C-R5或N; B为C-R6或N; D为C-R7或N; 但A、B和D中至少有一个为N; R5为氢或C1-6烷基; R6为氢或C1-6烷基; R7为氢，C1-6烷基，C1-6烷氧基，或羟基; R8为氢或C1-6烷基，但R4和R8中至少有一个为氢; R9为氢或羟基; R10为氢或C1-6烷基; 其盐是PAD4抑制剂，可能对多种疾病的治疗有用，例如类风湿关节炎、血管炎、系统性红斑狼疮、溃疡性结肠炎、癌症、囊性纤维化、哮喘、皮肤性红斑狼疮和银屑病。
• 2-(azaindol-2-yl) benzimidazoles as PAD4 inhibitors
  申请人：Glaxo Group Limited

  公开号：US10039755B2

  公开（公告）日：2018-08-07

  Compounds of formula (I) wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O—, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6alkyl; A is C—R5 or N; B is C—R6 or N; D is C—R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.

  式(I)化合物 其中；R1是氢或C1-6烷基；R2是氢、C1-6烷基、全卤甲基C0-5烷基-O-或C1-6烷氧基；R3是氢、C1-6烷基或C1-6烷氧基C1-6烷基；R4是氢、C1-6烷基、全卤甲基C1-6烷基；或未取代的 C3-6 环烷基 C1-6 烷基；A 是 C-R5 或 N；B 是 C-R6 或 N；D 是 C-R7 或 N；但 A、B 和 D 中至少有一个是 N；R5 是氢或 C1-6 烷基；R6 是氢或 C1-6 烷基；R7是氢、C1-6烷基、C1-6烷氧基或羟基； R8是氢或C1-6烷基，但条件是R4和R8之一是氢； R9是氢或羟基； R10是氢或C1-6烷基；及其盐类是 PAD4 抑制剂，可用于治疗各种疾病，例如类风湿性关节炎、血管炎、系统性红斑狼疮、溃疡性结肠炎、癌症、囊性纤维化、哮喘、皮肤红斑狼疮和银屑病。