2,6-二氯-3-甲基异烟酸2,6-二氯-3-甲基-4-吡啶甲酸 | 1256835-40-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 2,6-二氯-3-甲基异烟酸2,6-二氯-3-甲基-4-吡啶甲酸
• 英文名称: 2,6-Dichloro-3-methylisonicotinic acid
• 英文别名: 2,6-dichloro-3-methylpyridine-4-carboxylic acid
• CAS: 1256835-40-1
• 化学式: C₇H₅Cl₂NO₂
• 分子量: 206.02
• InChiKey: TWYNDQHXDSFICB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  50.2
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H315,H319,H335

文献信息

• MODULATORS FOR AMYLOID BETA
  申请人：Baumann Karlheinz

  公开号：US20090215759A1

  公开（公告）日：2009-08-27

  The invention relates to compounds of formula wherein the substituents are as described in claim 1 . Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

  该发明涉及以下式的化合物 其中取代基如权利要求中所述 。式I的化合物是淀粉样蛋白β的调节剂，因此它们可能对治疗或预防与大脑中β-淀粉样蛋白沉积相关的疾病有用，特别是阿尔茨海默病，以及其他疾病，如脑淀粉样血管病变，遗传性脑出血伴淀粉样变性，荷兰型（HCHWA-D），多梗死性痴呆，拳击性痴呆和唐氏综合征。
• [EN] PYRROLIDINE-FUSED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE<br/>[FR] COMPOSÉS DE DIOXYDE DE THIADIAZINE FUSIONNÉE À LA PYRROLIDINE EN TANT QU'INHIBITEURS DE BACE, COMPOSITIONS ET LEUR UTILISATION
  申请人：MERCK SHARP & DOHME

  公开号：WO2012138590A1

  公开（公告）日：2012-10-11

  In its many embodiments, the present invention provides provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of W, Z, R1H, R2, R3, R4, ring A, ring B, m, n, p, and- L1- is as defined herein. The novel compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous 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 Alzheimer's disease, are also disclosed.

  在其众多实施方式中，本发明提供了特定的咪唑噻二唑二氧化物化合物，包括化合物式（I）中的化合物及其互变异构体和立体异构体，以及所述化合物的药用可接受盐，所述互变异构体和所述立体异构体，其中W、Z、R1H、R2、R3、R4、环A、环B、m、n、p和-L1-的每一个在此处定义。本发明的新化合物被发现具有出乎意料的性质，预计将使它们在作为BACE抑制剂和/或用于治疗和预防与之相关的各种病理方面具有优势。还公开了包括一种或多种此类化合物（单独或与一种或多种其他活性剂的组合）的制备和使用方法，包括治疗阿尔茨海默病的药物组合。
• MODULATORS OF AMYLOID BETA
  申请人：Hoffman-La Roche Inc.

  公开号：US20130190302A1

  公开（公告）日：2013-07-25

  The invention relates to compounds of formula wherein the substituents are as described in claim 1 . Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

  本发明涉及公式I的化合物，其中取代基如权利要求书1所述。公式I的化合物是淀粉样β调节剂，因此它们可能对与β-淀粉样沉积在大脑中有关的疾病，特别是阿尔茨海默病和其他疾病，如脑淀粉样血管病、遗传性淀粉样出血性脑病，荷兰型（HCHWA-D）、多发性梗塞性痴呆、拳击性痴呆和唐氏综合症的治疗或预防可能有用。
• PYRROLIDINE-FUSED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP2694521B1

  公开（公告）日：2015-11-25
• US4474602A
  申请人：——

  公开号：US4474602A

  公开（公告）日：1984-10-02