1-(2,4-dimethoxyphenyl)piperazine hydrochloride | 16015-74-0

• 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-(2,4-dimethoxyphenyl)piperazine hydrochloride
• 英文别名: 1-(2,4-dimethoxyphenyl) piperazine hydrochloride；1-(2,4-dimethoxyphenyl)piperazine;hydrochloride
• CAS: 16015-74-0
• 化学式: C₁₂H₁₈N₂O₂*ClH
• 分子量: 258.748
• InChiKey: HJBXDGLSLSGHRV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.54
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  33.7
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-(2,4-dimethoxyphenyl)piperazine hydrochloride 在 氢溴酸 作用下， 以78%的产率得到1-(2-methoxy-4-hydroxyphenyl)piperazine dihydrobromide
  参考文献：
  名称：

  Evidence of an effective antiarrhythmic compound by study of in vivo metabolisation

  摘要：

  DOI：

  10.1016/0223-5234(90)90214-n
• 作为产物：
  描述：

  二(2-氯乙基)胺盐酸盐 、 2,4-二甲氧基苯胺 在 sodium hydroxide 、 potassium carbonate 作用下， 以 ethereal HCl 、 乙醇 为溶剂， 生成 1-(2,4-dimethoxyphenyl)piperazine hydrochloride
  参考文献：
  名称：

  Series of 5-[-(4-aryl-1-piperazinyl)alkyl]-2-oxazolidinone derivatives

  摘要：

  揭示了一种治疗过敏性疾病的方法和药物组合物，用于一系列Formula I的5-[(4-芳基-1-哌嗪基)烷基]-2-噁唑烷酮衍生物。这些化合物在抑制活体动物中的I型过敏##STR1##反应方面很有用，因此可用于治疗哮喘、鼻炎、特应性皮炎、慢性荨麻疹、过敏性结膜炎等过敏现象。

  公开号：

  US05086055A1

文献信息

• [EN] PYRAZOLOTRIAZOLOPYRIMIDINE DERIVATIVES AS A2A RECEPTOR ANTAGONIST<br/>[FR] DÉRIVÉS DE PYRAZOLOTRIAZOLOPYRIMIDINE EN TANT QU'ANTAGONISTE DU RÉCEPTEUR A2A
  申请人：BEIGENE LTD

  公开号：WO2020020097A1

  公开（公告）日：2020-01-30

  Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as A2A receptor antagonist.

  本文揭示了一种吡唑三唑吡嘧啶衍生物或其立体异构体，或其药学上可接受的盐，可用作A2A受体拮抗剂，以及包含该物质的药物组合物。本文还揭示了一种使用该吡唑三唑吡嘧啶衍生物或其立体异构体，或其药学上可接受的盐作为A2A受体拮抗剂治疗癌症的方法。
• HYDROQUINONE DERIVATIVES
  申请人：——

  公开号：US20010008893A1

  公开（公告）日：2001-07-19

  A hydroquinone derivative useful as an intraocular pressure lowering, anti-hypertensive and radical scavenging agent represented by the following formula 1 wherein B 1 and B 2 in formula (I) are the same or different and at any position on the benzene ring (when W is nitrogen, however, at any other position on the benzene ring) and each denotes a substituent selected from the group consisting of hydrogen, halogen, hydroxyl, lower alkoxyl and carboxyl, and the substituent CH 3 is at position 2 or 3, and W are the same or different and each denotes a nitrogen or carbon atom. R 1 , R 2 , R 3 and R 4 in formula (II) are the same or different and each denotes a substituent selected from the group consisting of hydrogen, lower alkyl and lower alkoxyl, and B 1 and B 2 are as hereinbefore defined, or a pharmacologically acceptable salt thereof.

  一种具有降低眼内压、抗高血压和自由基清除作用的有用氢醌衍生物，由以下式1表示，其中式（I）中的B1和B2相同或不同，并且在苯环上的任何位置（当W为氮时，在苯环上的任何其他位置），每个表示从氢、卤素、羟基、低级烷氧基和羧基组成的组中选择的取代基，并且取代基CH3位于位置2或3，并且W相同或不同，每个表示氮或碳原子。式（II）中的R1、R2、R3和R4相同或不同，每个表示从氢、低级烷基和低级烷氧基组成的组中选择的取代基，并且B1和B2如前所述，或其药理学上可接受的盐。
• \x9b3-(4-phenylpiperazin-1-yl)propyl-amino, thio and oxy!-pyridine,
  申请人：Syntex (U.S.A.) Inc.

  公开号：US05688795A1

  公开（公告）日：1997-11-18

  The present invention relates to novel .alpha..sub.1 -adrenoceptor antagonists of Formula I: ##STR1## in which: p is 0 or 1; t is 0, 1 or 2; X is O, S or NR.sup.6 (in which R.sup.6 is hydro or (C.sub.1-6)alkyl); Y and Z are independently CH or N; R.sup.1 is hydro, hydroxy, halo, nitro, amino, cyano, (C.sub.1-4)alkylthio, acetylamino, trifluoroacetylamino, methylsulfonylamino, (C.sub.1-6)alkyl, (C.sub.3-6)cycloalkyl, (C.sub.3-6)cycloalkyl (C.sub.1-4)alkyl, oxazol-2-yl, aryl, heteroaryl, aryl (C.sub.1-4)alkyl, heteroaryl (C.sub.1-4)alkyl, (C.sub.1-6)alkyloxy, (C.sub.3-6)cycloalkyloxy, (C.sub.3-6)cycloalkyl (C.sub.1-4)alkyloxy, 2-propynyloxy, aryloxy, heteroaryloxy, aryl (C.sub.1-4)alkyloxy or heteroaryl (C.sub.1-4)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms and aryl or heteroaryl is optionally substituted with one to two substituents independently selected from halo and cyano); R.sup.2 is hydro, hydroxy, halo, cyano, (C.sub.1-6)alkyl or (C.sub.1-6)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms); R.sup.3 is -C (O)R.sup.7 (wherein R.sup.7 is (C.sub.1-6)alkyl, (C.sub.3-6)cycloalkyl, di(C.sub.1-4)alkylamino, N-(C.sub.1-4)alkyl-N-(C.sub.1-4)alkyloxyamino, (C.sub.1-4)alkyl((C.sub.1-4)alkyloxy)amino, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or piperazin-1-yl); R.sup.4 is halo, hydroxy, cyano, (C.sub.1-6)alkyl or (C.sub.1-6)alkyloxy; and R.sup.5 is (C.sub.1-6)alkyl; and the pharmaceutically acceptable salts and N-oxides thereof.

  本发明涉及一种新型的α1-肾上腺素受体拮抗剂，其化学式为I：##STR1## 其中：p为0或1；t为0、1或2；X为O、S或NR6（其中R6为氢或（C1-6）烷基）；Y和Z独立地为CH或N；R1为氢、羟基、卤素、硝基、氨基、氰基、（C1-4）烷基硫醇、乙酰氨基、三氟乙酰氨基、甲基磺酰氨基、（C1-6）烷基、（C3-6）环烷基、（C3-6）环烷基（C1-4）烷基、噁唑-2-基、芳基、杂环芳基、芳基（C1-4）烷基、杂环芳基（C1-4）烷基、（C1-6）烷氧基、（C3-6）环烷氧基、（C3-6）环烷基（C1-4）烷氧基、2-丙炔氧基、芳基氧基、杂环芳基氧基、芳基（C1-4）烷氧基或杂环芳基（C1-4）烷氧基（其中烷基可选地被1-3个卤素原子取代，芳基或杂环芳基可选地被1-2个独立选择自卤素和氰基的取代基取代）；R2为氢、羟基、卤素、氰基、（C1-6）烷基或（C1-6）烷氧基（其中烷基可选地被1-3个卤素原子取代）；R3为-C（O）R7（其中R7为（C1-6）烷基、（C3-6）环烷基、二（C1-4）烷基氨基、N-（C1-4）烷基-N-（C1-4）烷氧基氨基、（C1-4）烷基（（C1-4）烷氧基）氨基、吡咯烷-1-基、哌啶-1-基、吗啉-4-基或哌嗪-1-基）；R4为卤素、羟基、氰基、（C1-6）烷基或（C1-6）烷氧基；R5为（C1-6）烷基；以及其药学上可接受的盐和N-氧化物。
• Modulators or Alpha7 Nicotinic Acetylcholine Receptors and Therapeutic Uses Thereof
  申请人：Gaviraghi Giovanni

  公开号：US20080275028A1

  公开（公告）日：2008-11-06

  The present invention relates to compounds with α7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory disorders.

  本发明涉及具有α7 nAChR激动活性的化合物，其制备方法，含有该化合物的制药组合物以及用于治疗神经、精神、认知、免疫和炎症性疾病的用途。
• 3-(4-phenylpiperazin-1-yl)propyl-amino, thio and oxy -pyridine, pyrimidine and benzene derivatives as alpha1-adrenoceptor antagonists
  申请人：F. Hoffmann-La Roche AG

  公开号：EP0711757A1

  公开（公告）日：1996-05-15

  The present invention relates to novel α₁-adrenoceptor antagonists of Formula I: in which: p is 0 or 1; t is 0, 1 or 2; X is O, S or NR⁶ (in which R⁶ is hydro or (C₁₋₆)alkyl); Y and Z are independently CH or N; R¹ is hydro, hydroxy, halo, nitro, amino, cyano, (C₁₋₄)alkylthio, acetylamino, trifluoroacetylamino, methylsulfonylamino, (C₁₋₆)alkyl, (C₃₋₆)cycloalkyl, (C₃₋₆)cycloalkyl(C₁₋₄)alkyl, oxazol-2-yl, aryl, heteroaryl, aryl(C₁₋₄)alkyl, heteroaryl(C₁₋₄)alkyl, (C₁₋₆)alkyloxy, (C₃₋₆)cycloalkyloxy, (C₃₋₆)cycloalkyl(C₁₋₄)alkyloxy, 2-propynyloxy, aryloxy, heteroaryloxy, aryl(C₁₋₄)alkyloxy or heteroaryl(C₁₋₄)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms and aryl or heteroaryl is optionally substituted with one to two substituents independently selected from halo and cyano); R² is hydro, hydroxy, halo, cyano, (C₁₋₆)alkyl or (C₁₋₆)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms); R³ is -C(O)R⁷ (wherein R⁷ is (C₁₋₆)alkyl, (C₃₋₆)cycloalkyl, di(C₁₋₄)alkylamino, N-(C₁₋₄)alkyl-N-(C₁₋₄)alkyloxyamino, (C₁₋₄)alkyl((C₁₋₄)alkyloxy)amino, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or piperazin-1-yl); R⁴ is halo, hydroxy, cyano, (C₁₋₆)alkyl or (C₁₋₆)alkyloxy; and R⁵ is (C₁₋₆)alkyl; and the pharmaceutically acceptable salts and N-oxides thereof.

  本发明涉及式 I 的新型 α₁-肾上腺素受体拮抗剂： 其中 p 是 0 或 1； t 是 0、1 或 2 X 是 O、S 或 NR⁶（其中 R⁶ 是氢或 (C₁₋₆)烷基）； Y 和 Z 独立地为 CH 或 N； R¹是氢、羟基、卤代、硝基、氨基、氰基、(C₁₋₄)烷硫基、乙酰氨基、三氟乙酰氨基、甲磺酰氨基、(C₁₋₆)烷基、(C₃₋₆)环烷基、(C₃₋₆)环烷基(C₁₋₄)烷基、噁唑-2-基、芳基、杂芳基、芳基(C₁₋₄)烷基、杂芳基(C₁₋₄)烷基、(C₁₋₆)烷氧基、(C₃₋₆)环烷氧基、(C₃₋₆)环烷基(C₁₋₄)烷氧基，2-丙炔氧基，芳基氧基，杂芳基氧基、芳基（C₁₋₄）烷氧基或杂芳基（C₁₋₄）烷氧基（其中烷基任选被一至三个卤原子取代，芳基或杂芳基任选被一至两个独立选自卤素和氰基的取代基取代）； R² 是氢、羟基、卤代、氰基、(C₁₋₆)烷基或(C₁₋₆)烷氧基（其中烷基任选被一至三个卤原子取代）； R³ 是 -C(O)R⁷（其中 R⁷ 是 (C₁₋₆)烷基、(C₃₋₆)环烷基、二(C₁₋₄)烷基氨基、N-(C₁₋₄)烷基-N-(C₁₋₄)烷氧基氨基、(C₁₋₄)烷基((C₁₋₄烷氧基)氨基、吡咯烷-1-基、哌啶-1-基、吗啉-4-基或哌嗪-1-基)； R⁴ 是卤素、羟基、氰基、(C₁₋₆)烷基或 (C₁₋₆)烷氧基；和 R⁵ 是 (C₁₋₆)烷基；及其药学上可接受的盐和 N-氧化物。