3-(difluoromethoxy)-3-methyl-2H-pyridine-2-carboxamide

• 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: 3-(difluoromethoxy)-3-methyl-2H-pyridine-2-carboxamide
• 化学式: C₈H₁₀F₂N₂O₂
• 分子量: 204.17
• InChiKey: XLELYZIMRFQTGZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  64.7
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• BACE1 inhibitors
  申请人：Hoffmann-La Roche Inc.

  公开号：US10246468B2

  公开（公告）日：2019-04-02

  The present invention provides a compound of formula I, having BACE1 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.

  本发明提供了具有 BACE1 抑制活性的式 I 化合物、含有它们的药物组合物的制造方法以及它们作为治疗活性物质的用途。本发明的活性化合物可用于阿尔茨海默病等疾病的治疗和/或预防。
• BACE1 INHIBITORS
  申请人：Hoffmann-La Roche Inc.

  公开号：US20190002476A1

  公开（公告）日：2019-01-03

  The present invention provides a compound of formula I, having BACE1 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.
• [EN] AMINO - DIHYDROTHIAZINE AND AMINO - DIOXIDO DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE ANTAGONISTS AND METHODS OF USE<br/>[FR] COMPOSÉS AMINO-DIHYDROTHIAZINE ET AMINO-DIOXYDO DIHYDROTHIAZINE EN TANT QU'ANTAGONISTES DE BÊTA-SÉCRÉTASE ET PROCÉDÉS D'UTILISATION
  申请人：AMGEN INC

  公开号：WO2014059185A1

  公开（公告）日：2014-04-17

  The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.
• [EN] FUSED MULTICYCLIC 3-AMINO-5,6-DIHYDRO-2H-1,4-THIAZINE DERIVATIVES AND THEIR USE AS BETA-SECRETASE INHIBITORS<br/>[FR] DÉRIVÉS DE 3-AMINO-5,6-DIHYDRO-2H-1,4-THIAZINE MULTICYCLIQUES CONDENSÉS ET LEUR UTILISATION À TITRE D'INHIBITEURS DE BÊTA-SÉCRÉTASE
  申请人：AMGEN INC

  公开号：WO2014120658A1

  公开（公告）日：2014-08-07

  The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A5, A6, A8, R1, R2, R3, R7, X, Y, n and o of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
• [EN] BRIDGED BICYCLIC AMINO THIAZINE DIOXIDE COMPOUNDS AS INHIBITORS OF BETA- SECRETASE<br/>[FR] COMPOSÉS DE DIOXYDE D'AMINO-THIAZINE BICYCLIQUES PONTÉS EN TANT QU'INHIBITEURS DE BÊTA-SÉCRÉTASE
  申请人：AMGEN INC

  公开号：WO2015017407A1

  公开（公告）日：2015-02-05

  The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I, wherein variables A4, A5, A6, A8, R1, R2, R3, R7and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds and the compounds and compositions for treatment of disorders and/ or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions.