(R)-2-methyl-propane-2-sulfinic acid [6-nitro-chroman-(4E)-ylidene]-amide | 1415108-57-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: (R)-2-methyl-propane-2-sulfinic acid [6-nitro-chroman-(4E)-ylidene]-amide
• 英文别名: (NE,R)-2-methyl-N-(6-nitro-2,3-dihydrochromen-4-ylidene)propane-2-sulfinamide
• CAS: 1415108-57-4
• 化学式: C₁₃H₁₆N₂O₄S
• 分子量: 296.347
• InChiKey: YJXVRJHUVACOAO-RDPWEWGOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  104
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• SPIRO-[1,3]-OXAZINES AND SPIRO-[1,4]-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS
  申请人：Narquizian Robert

  公开号：US20120302549A1

  公开（公告）日：2012-11-29

  The present invention provides spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

  本发明提供了具有BACE1和/或BACE2抑制活性的式I的螺[1,3]-噁唑和螺[1,4]-噁唑环烯化合物，其制备方法，包含它们的药物组合物以及它们作为治疗活性物质的用途。本发明的活性化合物在治疗和/或预防治疗例如阿尔茨海默病和2型糖尿病等疾病方面非常有用。
• [EN] C5-SPIRO IMINOTHIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE<br/>[FR] DIOXYDES D'IMINOTHIAZINE SPIRO-C5 UTILISÉS COMME INHIBITEURS DE BACE, COMPOSITIONS, ET LEUR UTILISATION
  申请人：MERCK SHARP & DOHME

  公开号：WO2015038446A1

  公开（公告）日：2015-03-19

  In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein RL, X, Y, R1A, R1B, R2, R3, m, and RA are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

  在其多种实施方式中，本发明提供了某些C5-螺环亚噻二唑二氧化物化合物，包括化合物的化学式（I）：或其互变异构体和/或立体异构体，以及该化合物、该互变异构体和该立体异构体的药学上可接受的盐，其中RL、X、Y、R1A、R1B、R2、R3、m和RA的定义如本文所述。本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与之相关的各种病理。包括一种或多种这样的化合物（单独或与一种或多种其他活性剂组合）的药物组合物，以及其制备和使用方法，包括可能用于治疗阿尔茨海默病的方法，也已披露。
• C5-SPIRO IMINOTHIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
  申请人：SCOTT Jack D.

  公开号：US20160222032A1

  公开（公告）日：2016-08-04

  In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein R L , X, Y, R 1A , R 1B , R2, R3, m, and RA are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
• C6-SPIRO IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
  申请人：CUMMING Jared N.

  公开号：US20160264538A1

  公开（公告）日：2016-09-15

  In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds, wherein R1, R2, R3, X, Y, s, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed:
• US9079919B2
  申请人：——

  公开号：US9079919B2

  公开（公告）日：2015-07-14