氯(3-氯苄基)镁 | 29874-01-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 氯(3-氯苄基)镁
• 英文名称: magnesium,1-chloro-3-methanidylbenzene,chloride
• 英文别名: 3-chlorobenzylmagnesium chloride；chloro(3-chlorobenzyl)magnesium；m-ClC6H4CH2MgCl；meta-chlorobenzylmagnesium chloride；m-Chlorbenzylmagnesiumchlorid；m-chlorobenzylmagnesium chloride
• CAS: 29874-01-9
• 化学式: C₇H₆Cl₂Mg
• 分子量: 185.336
• InChiKey: FXQFOXTUJOAWNN-UHFFFAOYSA-M

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  10.0
• 可旋转键数：
  2.0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  0.0
• 氢给体数：
  0.0
• 氢受体数：
  0.0

安全信息

• 危险等级：
  3

反应信息

• 作为反应物：
  描述：

  氯(3-氯苄基)镁 在 lithium hydroxide 、 sodium hydride 作用下， 以 四氢呋喃 、 甲醇 、 乙醚 、 水 为溶剂， 反应 2.0h， 生成
  参考文献：
  名称：

  Studies Leading to Potent, Dual Inhibitors of Bcl-2 and Bcl-xL

  摘要：

  Overexpression of the antiapototic proteins Bcl-2 and Bcl-xL provides a common mechanism through which cancer cells gain a survival advantage and become resistant to conventional chemotherapy. Inhibition of these prosurvival proteins is an attractive strategy for cancer therapy. We recently described the discovery of a selective Bcl-xL antagonist that potentiates the antitumor activity of chemotherapy and radiation. Here we describe the use of structure-guided design to exploit a deep hydrophobic binding pocket on the surface of these proteins to develop the first dual, subnanomolar inhibitors of Bcl-xL and Bcl-2. This study culminated in the identification of 2, which exhibited EC50 values of 8 nM and 30 nM in Bcl-2 and Bcl-xL dependent cells, respectively. Compound 2 demonstrated single agent efficacy against human follicular lymphoma cell lines that overexpress Bcl-2, and efficacy in a murine xenograft model of lymphoma when given both as a single agent and in combination with etoposide.

  DOI：

  10.1021/jm061152t
• 作为产物：
  描述：

  间氯氯苄 生成 氯(3-氯苄基)镁
  参考文献：
  名称：

  ITOH, OSAMU;NUMATA, TATSUO;YOSHIMURA, TOSHIAKI;OAE, SHIGERU, BULL. CHEM. SOC. JAP., 1983, 56, N 1, 266-269

  摘要：

  DOI：

文献信息

• [EN] NEW BICYCLIC DIHYDROISOQUINOLINE-1-ONE DERIVATIVES<br/>[FR] NOUVEAUX DÉRIVÉS BICYCLIQUES DE LA DIHYDROISOQUINOLINE-1-ONE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2013079452A1

  公开（公告）日：2013-06-06

  The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4¸ R5, R6, A1, A2, A3, A4, A5 and n are as described herein,compositions including the compounds and methods of using the compounds as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrom.

  该发明提供了具有一般式(I)的新化合物，其中R1、R2、R3、R4、R5、R6、A1、A2、A3、A4、A5和n如本文所述，包括这些化合物的组合物以及将这些化合物用作醛固酮合成酶（CYP11B2或CYP11B1）抑制剂治疗或预防慢性肾病、充血性心力衰竭、高血压、原发性醛固酮增多症和库欣综合征的方法。
• Substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives
  申请人：Knust Henner

  公开号：US20060079507A1

  公开（公告）日：2006-04-13

  The present invention is concerned with a method of treating a disease selected from the group consisting of cognitive disorders, anxiety, Alzheimer's disease, and schizophrenia comprising administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the following formula wherein R 1 is halogen, lower alkyl, lower alkynyl, cycloalkyl, lower alkoxy, OCF 3 , —NHR, —NHC(O)R or —NHSO 2 R; R 2 is hydrogen, methyl or aryl which is unsubstituted or substituted by one or two substituents selected from the group consisting of halogen and lower alkoxy; R 3 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, lower alkoxy, —O(CH 2 ) n+1 —O-lower alkyl, —(CH 2 ) n -aryl which is optionally substituted by lower alkyl or halogen, heteroaryl, —NHR, —N(R) 2 , wherein each R can be the same or different, —NHCH 2 C≡CH, or pyrrolidin-1-one; R is hydrogen, lower alkyl, lower alkyl substituted by halogen, heteroaryl, —(CH 2 ) n O-lower alkyl, —NH-lower alkyl, cycloalkyl or aryl, and n is 0, 1, 2 or 3; and with their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them. The most preferred indication is Alzheimer's disease.

  本发明涉及一种治疗从认知障碍、焦虑、阿尔茨海默病和精神分裂症中选择的疾病的方法，包括给予下列公式的取代咪唑[1,5-a][1,2,4]三唑[1,5-d][1,4]苯二氮䓬啉衍生物的治疗有效量：其中R1是卤素、较低烷基、较低炔基、环烷基、较低烷氧基、OCF3、—NHR、—NHC(O)R或—NHSO2R；R2是氢、甲基或芳基，未取代或由卤素和较低烷氧基中选择的一种或两种取代基取代；R3是氢、较低烷基、较低烯基、环烷基、较低烷氧基、—O(CH2)n+1—O-较低烷基、—( )n-芳基，可由较低烷基或卤素取代，杂芳基、—NHR、—N(R)2，其中每个R可以相同也可以不同，—NH C≡CH，或吡咯烷酮；R是氢、较低烷基、由卤素取代的较低烷基、杂芳基、—( )nO-较低烷基、—NH-较低烷基、环烷基或芳基，n为0、1、2或3；以及其药学上可接受的酸盐。该发明还提供了公式I-A的新化合物和含有它们的药物组合物。最受欢迎的适应症是阿尔茨海默病。
• SUBSTITUTED PYRIDO(3,2-D) PYRIMIDINES AND PHARMACEUTICAL COMPOSITIONS FOR TREATING VIRAL INFECTIONS
  申请人：Herdewijn Piet Andre' Maurits Maria

  公开号：US20090253696A1

  公开（公告）日：2009-10-08

  This invention provides di-, tri- and tetra-substituted pyrido(3,2-d)pyrimidine derivatives with specific substituting patterns, their pharmaceutically acceptable salts, N-oxides, solvates, pro-drugs and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular being highly active antiviral agents. The invention also provides use of such derivatives in the treatment of viral infections and pathologic conditions associated therewith, including hepatitis C.

  这项发明提供了具有特定取代模式的二、三和四取代吡啶并[3,2-d]嘧啶衍生物，其药学上可接受的盐、N-氧化物、溶剂合物、前药和对映体，具有意外地理想的药理特性，特别是作为高活性抗病毒剂。该发明还提供了利用这些衍生物治疗病毒感染及相关病理状况，包括丙型肝炎的用途。
• Substituted (.omega.-aminoalkoxy)stilbene derivatives as a new class of anticonvulsants
  作者：Ryoji Kikumoto、Akihiro Tobe、Harukazu Fukami、Kunihiro Ninomiya、Mitsuo Egawa

  DOI：10.1021/jm00371a015

  日期：1984.5

  (omega- aminoalkoxy )stilbene derivatives has been synthesized and screened for anticonvulsant activity. The effect of structural modification of these molecules on the activities has been systematically examined. Potent anticonvulsant activity was displayed by 2-[4-(4-methyl-1 piperazinyl)butoxy]stilbene (20) and some 2-[4-(3-alkoxy-1-piperidino)butoxy]stilbene derivatives (21, 37, 38, and 40), as determined

  已合成了一系列取代的（ω-氨基烷氧基）二苯乙烯衍生物，并筛选了其抗惊厥活性。已经系统地检查了这些分子的结构修饰对活性的影响。2- [4-（4-甲基-1哌嗪基）丁氧基] sti烯（20）和某些2- [4-（3-烷氧基-1-哌啶基）丁氧基] sti烯衍生物（21，37， 38和40），通过最大电击惊厥（MES）和戊四氮诱发的小鼠惊厥试验确定。在大鼠的进一步药理试验中，化合物21的抗MES活性比二苯乙内酰脲和卡马西平更强，其治疗指数优于两种抗癫痫药。
• 3-Amino-2-benzyl-1-phenylpropane derivatives
  申请人：——

  公开号：US20020161262A1

  公开（公告）日：2002-10-31

  Substituted 3-amino-2-benzyl-1-phenlypropane derivatives, methods for preparing them, pharmaceutical compositions containing them, and methods of using them to treat various medical conditions.

  替代3-氨基-2-苄基-1-苯丙烷衍生物，制备它们的方法，含有它们的药用组合物，以及使用它们治疗各种医疗状况的方法。