1-(2,6-difluorophenyl)piperazine | 255893-56-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 1-(2,6-difluorophenyl)piperazine
• CAS: 255893-56-2
• 化学式: C₁₀H₁₂F₂N₂
• mdl: MFCD09894120
• 分子量: 198.215
• InChiKey: YWTWDUFMPFRGJQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  15.3
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-(2,6-difluorophenyl)piperazine 在 盐酸 、 sodium tetrahydroborate 、 对甲苯磺酸 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 乙醇 为溶剂， 反应 98.67h， 生成 2-[4-[(E)-3-[4-(2,6-difluorophenyl)piperazin-1-yl]prop-1-enyl]-5-methylpyrazol-1-yl]pyrimidine
  参考文献：
  名称：

  Synthesis and Antitumor Activity of Novel Pyrimidinyl Pyrazole Derivatives. II. Optimization of the Phenylpiperazine Moiety of 1-[5-Methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-3-phenylpiperazinyl-1-trans-propenes.

  摘要：

  为提高原型化合物3-[4-(3-氯苯基)-1-哌嗪基]-1-[5-甲基-1-(2-嘧啶基)-4-吡唑基]-1-反式-丙烯（2）的体外和体内活性，合成了一系列新型的3-取代-1-[5-甲基-1-(2-嘧啶基)-4-吡唑基]-1-反式-丙烯，并通过体外对几种肿瘤细胞系的生长抑制试验和体内对某些肿瘤模型的抗肿瘤活性试验（经腹腔和口服给药）进行了评估。化合物7a和7e，分别是2的3,5-二氟苯基和3,5-二氯苯基类似物，其体外细胞毒性显著强于2，并有较强的抗肿瘤活性，且不会因副作用导致体温下降。

  DOI：

  10.1248/cpb.50.453
• 作为产物：
  描述：

  tert-butyl 4-(2,6-difluorophenyl)piperazine-1-carboxylate 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 生成 1-(2,6-difluorophenyl)piperazine
  参考文献：
  名称：

  [EN] COMPOUNDS AND METHODS OF THEIR USE
  [FR] COMPOSÉS ET LEURS PROCÉDÉS D'UTILISATION

  摘要：

  提供了能够结合CBP或MED15的KIX结构域以抑制SREBP1与MED15或CBP的KIX结构域之间结合的试剂。还提供了含有这些试剂的组合物和它们的使用方法。

  公开号：

  WO2020077361A1

文献信息

• Compounds specific for the human alpha1d adrenergic receptor and uses thereof
  申请人：——

  公开号：US20020028760A1

  公开（公告）日：2002-03-07

  This invention is directed towards a method of inhibiting activation of a human &agr; 1d adrenergic receptor which comprises contacting the receptor with a compound so as to inhibit activation of the receptor, wherein the compound binds selectively to a human ald adrenergic receptor. This invention provides for a compound which binds selectively to a human &agr; 1d adrenergic receptor. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier. This invention further provides for a method of treating a subject afflicted with a disease which is susceptible to treatment by antagonism of the human &agr; 1d adrenergic receptor which comprises administering to the subject an amount of the above defined compounds effective to treat the disease.

  这项发明涉及一种抑制人类α1d肾上腺素受体激活的方法，包括将受体与一种化合物接触，以抑制受体的激活，其中该化合物选择性地结合到人类α1d肾上腺素受体。这项发明提供了一种选择性结合到人类α1d肾上腺素受体的化合物。该发明还提供了一种包含上述定义的化合物的治疗有效量和药学上可接受的载体的药物组合物。这项发明还提供了一种治疗患有易受人类α1d肾上腺素受体拮抗治疗的疾病的方法，包括向受试者施用上述定义的化合物的有效量以治疗疾病。
• INHIBITORS OF STEAROYL-COA DESATURASE
  申请人：Gillespie Paul

  公开号：US20090149466A1

  公开（公告）日：2009-06-11

  Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity.

  提供以下式(I)化合物： 以及药用可接受的盐，其中取代基如说明书中所披露。这些化合物以及包含它们的药物组合物可用于治疗诸如肥胖等疾病。
• 신규한 이미다조트리아지논 또는 이미다조피라지논 유도체, 및 이들의 용도
  申请人：ST Pharm Co., Ltd. 에스티팜 주식회사(120100631570) Corp. No ▼ 154511-0039704BRN ▼303-81-52269

  公开号：KR20160007347A

  公开（公告）日：2016-01-20

  본 발명은 신규한 이미다조트리아지논 또는 이미다조피라지논 유도체, 이들의 토토머, 이들의 입체이성질체 및 혼합물, 또는 이들의 약학적으로 허용가능한 염; 및 이를 유효성분으로 포함하는 탄키라제 관련 질환의 예방 또는 치료용 약학적 조성물에 관한 것이다.

  本发明涉及新的伊米达佐替利亚酮或伊米达佩拉酮衍生物，它们的同分异构体，立体异构体和混合物，或它们的药学上可接受的盐；以及包含它们作为有效成分的用于预防或治疗坦基拉症相关疾病的药学组合物。
• [EN] COMPOUNDS SPECIFIC FOR THE HUMAN alpha 1d ADRENERGIC RECEPTOR AND USES THEREOF<br/>[FR] COMPOSES SPECIFIQUES DU RECEPTEUR ADRENERGIQUE alpha 1d HUMAIN ET SES UTILISATIONS
  申请人：SYNAPTIC PHARMA CORP

  公开号：WO2000004012A1

  公开（公告）日：2000-01-27

  This invention is directed towards a method of inhibiting activation of a human α1d adrenergic receptor which comprises contacting the receptor with a compound so as to inhibit activation of the receptor, wherein the compound binds selectively to a human α1d adrenergic receptor. This invention provides for a compound which binds selectively to a human α1d adrenergic receptor. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier. This invention further provides for a method of treating a subject afflicted with a disease which is susceptible to treatment by antagonism of the human α1d adrenergic receptor which comprises administering to the subject an amount of the above defined compound to treat the disease.

  本发明涉及一种抑制人类α1d肾上腺素能受体激活的方法，其中包括将化合物与受体接触以抑制受体的激活，所述化合物选择性地结合于人类α1d肾上腺素能受体。本发明提供了一种选择性结合于人类α1d肾上腺素能受体的化合物。本发明还提供了一种包含上述定义化合物的治疗有效量和药学上可接受的载体的制剂。本发明还提供了一种治疗患有可通过对抗人类α1d肾上腺素能受体治疗的疾病的受试者的方法，其中包括向受试者施用上述定义化合物的量以治疗疾病。
• Compounds specific for the human &agr;1d adrenergic receptor and uses thereof
  申请人：Synaptic Pharmaceutical Corporation

  公开号：US06706716B2

  公开（公告）日：2004-03-16

  This invention is directed towards a method of inhibiting activation of a human &agr;1d adrenergic receptor which comprises contacting the receptor with a compound so as to inhibit activation of the receptor, wherein the compound binds selectively to a human &agr;1d adrenergic receptor. This invention provides for a compound which binds selectively to a human &agr;1d adrenergic receptor. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier. This invention further provides for a method of treating a subject afflicted with a disease which is susceptible to treatment by antagonism of the human &agr;1d adrenergic receptor which comprises administering to the subject an amount of the above defined compounds effective to treat the disease.

  本发明涉及一种抑制人类α1d肾上腺素能受体激活的方法，该方法包括将化合物与受体接触以抑制其激活，其中该化合物选择性地结合于人类α1d肾上腺素能受体。本发明提供了一种选择性结合于人类α1d肾上腺素能受体的化合物。本发明还提供了一种制药组合物，包括上述定义的化合物的治疗有效量和药学可接受载体。本发明还提供了一种治疗易受人类α1d肾上腺素能受体拮抗剂治疗的疾病的方法，该方法包括向患者施用上述定义的化合物的有效治疗量以治疗该疾病。