N-(4-bromobenzyl)-N-methylethanamine | 60760-02-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-(4-bromobenzyl)-N-methylethanamine
• 英文别名: N-[(4-bromophenyl)methyl]-N-methylethanamine
• CAS: 60760-02-3
• 化学式: C₁₀H₁₄BrN
• mdl: MFCD14646601
• 分子量: 228.132
• InChiKey: ZJDKIYOCCQTFJZ-UHFFFAOYSA-N

物化性质

• 沸点：
  246.3±15.0 °C(Predicted)
• 密度：
  1.276±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• 3-SUBSTITUTED-6-ARYL PYRIDINES
  申请人：Hutchinson Alan J.

  公开号：US20110281837A1

  公开（公告）日：2011-11-17

  3-substituted-6-aryl pyridines of Formula I are provided: wherein R 1 , R 2 , R 3 , R 8 , R 9 , A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.

  本发明提供了式I的3-取代-6-芳基吡啶化合物：其中R1、R2、R3、R8、R9、A和Ar的定义在此处。这些化合物是C5a受体的配体。式I的优选化合物具有高亲和力结合到C5a受体，并在C5a受体上表现出中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的制药组合物，以及将这些化合物用于治疗各种炎症、心血管和免疫系统疾病的用途。此外，本发明提供了标记的3-取代-6-芳基吡啶，可用作C5a受体定位的探针。
• LINCOMYCIN DERIVATIVES AND ANTIMICROBIAL AGENTS COMPRISING THE SAME AS ACTIVE INGREDIENT
  申请人：Wakiyama Yoshinari

  公开号：US20100210570A1

  公开（公告）日：2010-08-19

  An objective of the present invention is to provide compounds of formula (1) or their pharmacologically acceptable salts or solvates wherein A represents aryl; R 1 represents N-optionally substituted C 1-6 alkyl-N-optionally substituted C 1-6 alkylamino-C 1-6 alkyl; R 2 represents a hydrogen atom or optionally substituted C 1-6 alkyl; R 3 represents optionally substituted C 1-6 alkyl or C 3-6 cycloalkyl-C 1-4 alkyl; m is 1 to 3; n is 0; and p is 0 to 2. The compounds are novel lincomycin derivatives that have a potent activity against resistant Streptococcus pneumoniae, which have recently posed problems, in the treatment of infectious diseases. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.

  本发明的目标是提供以下化合物(1)或其药理学上可接受的盐或溶剂，其中A代表芳基；R1代表N-可选取代的C1-6烷基-N-可选取代的C1-6烷基氨基-C1-6烷基；R2代表氢原子或可选取代的C1-6烷基；R3代表可选取代的C1-6烷基或C3-6环烷基-C1-4烷基；m为1至3；n为0；p为0至2。这些化合物是新颖的林可霉素衍生物，对最近在感染性疾病治疗中引起问题的耐药性肺炎链球菌具有强效活性。此外，这些化合物可用作抗微生物药物，有助于预防或治疗细菌感染性疾病。
• SUBSTITUTED 1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES FOR THE TREATMENT OF HORMONE-DEPENDENT DISEASES
  申请人：UNIVERSITÉ LAVAL

  公开号：US20160200685A1

  公开（公告）日：2016-07-14

  Provided are compounds of general formula A and A′, wherein X 1 and X 2 are each C, CH or N; R 3 and R 4 are each H, optionally substituted C 1 -C 30 saturated or unsaturated chemical group, or together form an optionally substituted C 5 -C 8 cycle; Z 1 ; Z 2 and Z 3 are each N or CH; V is C═O, C═S or CH 2 ; n is from 1 to 12; W 1 and W 2 are each H, CH 2 , O or S; and R 1 and R 2 are each H, Cr 1 C 6 alkyl, C 1 C 6 aryl, C 1 C 12 alkylaryl, optionally substituted phenyl, C 1 C 6 alkoxy, C 1 C 6 thioalkoxy, F, Cl, Br or I. These compounds inhibit steroid sulfatase (STS), act as selective estrogen receptor modulators (SERMs), increase alkaline phosphatase (ALP) activity, and are useful in the treatment of medical conditions involving hormones such as breast cancer, prostate cancer, endometriosis, osteoporosis, benign prostatic hyperplasia and endometrial cancer.

  提供了一般式为A和A'的化合物，其中X1和X2分别为C、CH或N；R3和R4分别为H、可选取代的C1-C30饱和或不饱和化学基团，或共同形成可选取代的C5-C8环；Z1、Z2和Z3分别为N或CH；V为C═O、C═S或CH2；n为1至12；W1和W2分别为H、 、O或S；R1和R2分别为H、Cr1C6烷基、C1C6芳基、C1C12烷基芳基、可选取代的苯基、C1C6烷氧基、C1C6硫代烷氧基、F、Cl、Br或I。这些化合物抑制类固醇磺酸酯酶（STS），作为选择性雌激素受体调节剂（SERMs），增加碱性磷酸酶（ALP）活性，并可用于治疗涉及激素的医疗条件，如乳腺癌、前列腺癌、子宫内膜异位症、骨质疏松症、良性前列腺增生和子宫内膜癌。
• 3-Substituted-6-Aryl Pyridines
  申请人：Hutchison Alan J.

  公开号：US20090176980A1

  公开（公告）日：2009-07-09

  3-substituted-6-aryl pyridines of Formula I are provided: wherein R 1 , R 2 , R 3 , R 8 , R 9 , A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.

  本发明提供了式I中的3-取代-6-芳基吡啶化合物： 其中R1、R2、R3、R8、R9、A和Ar在此定义。这些化合物是C5a受体的配体。式I的优选化合物具有高亲和力结合C5a受体，并在C5a受体上表现出中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物，以及在治疗各种炎症，心血管和免疫系统疾病中使用这些化合物的用途。此外，本发明提供了标记的3-取代-6-芳基吡啶，可用作C5a受体的定位探针。
• LINCOMYCIN DERIVATIVES AND ANTIBACTERIAL AGENTS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
  申请人：Meiji Seika Kaisha Ltd.

  公开号：EP2151447A1

  公开（公告）日：2010-02-10

  An objective of the present invention is to provide compounds of formula (1) or their pharmacologically acceptable salts or solvates wherein A represents aryl; R1 represents N-optionally substituted C1-6 alkyl-N-optionally substituted C1-6 alkylamino-C1-6 alkyl; R2 represents a hydrogen atom or optionally substituted C1-6 alkyl; R3 represents optionally substituted C1-6alkyl or C3-6 cycloalkyl-C1-4 alkyl; m is 1 to 3; n is 0; and p is 0 to 2. The compounds are novel lincomycin derivatives that have a potent activity against resistant Streptococcus pneumoniae, which have recently posed problems, in the treatment of infectious diseases. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.

  本发明的目的是提供式（1）化合物或其药理学上可接受的盐或溶液，其中 A 代表芳基；R1 代表 N-任选取代的 C1-6 烷基-N-任选取代的 C1-6 烷基氨基-C1-6 烷基；R2 代表氢原子或任选取代的 C1-6 烷基；R3 代表任选取代的 C1-6 烷基或 C3-6 环烷基-C1-4 烷基；m 为 1 至 3；n 为 0；p 为 0 至 2。这些化合物是新型的林可霉素衍生物，在治疗传染性疾病方面对耐药性肺炎链球菌有很强的活性，而耐药性肺炎链球菌近来已造成了一些问题。此外，这些化合物还可用作抗菌剂，用于预防或治疗细菌性传染病。