Rec 15/3079 | 220382-87-6

• 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: Rec 15/3079
• 英文别名: 1-[N-(2-nitrophenyl)-N-cyclohexylcarbonyl-2-aminoethyl]-4-(2-methoxyphenyl) piperazine；N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-(2-nitrophenyl)cyclohexanecarboxamide
• CAS: 220382-87-6
• 化学式: C₂₆H₃₄N₄O₄
• 分子量: 466.58
• InChiKey: HVMKWKIPLGPYAR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  34
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  81.8
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  Rec 15/3079 在 magnesium monoperoxyphthalate 作用下， 以43%的产率得到1-[N-(2-nitrophenyl)-N-cyclohexylcarbonyl-2-aminoethyl]-4-(2-methoxyphenyl)-piperazine N1,N4-dioxide
  参考文献：
  名称：

  1-(N-PHENYLAMINOALKYL)-PIPERAZINE DERIVATIVES SUBSTITUTED AT POSITION 2 OF THE PHENYL RING

  摘要：

  公开号：

  EP1000047B1
• 作为产物：
  描述：

  环己甲酰氯 、 1-[N-(2-nitrophenyl)-2-aminoethyl]-4-(2-methoxyphenyl)-piperazine 在 三乙胺 作用下， 以 1,2-二氯乙烷 为溶剂， 反应 16.0h， 以65%的产率得到Rec 15/3079
  参考文献：
  名称：

  1-(N-PHENYLAMINOALKYL)-PIPERAZINE DERIVATIVES SUBSTITUTED AT POSITION 2 OF THE PHENYL RING

  摘要：

  公开号：

  EP1000047B1

文献信息

• 1-(N-phenylalkylaminoalkyl)piperazine derivatives substituted at position 2 of the phenyl ring
  申请人：Recordati S.A., Chemical and Pharmaceutical Comoany

  公开号：US20020193383A1

  公开（公告）日：2002-12-19

  The present invention is directed to novel 1-(N-phenylaminoalkyl)piperazine derivatives substituted at the position 2 of the phenyl ring. Pharmaceutical compositions comprising the compounds of the invention also are contemplated. The compounds of the present invention also are contemplated for use in treating neuromuscular dysfunction of the lower urinary tract in a mammal.

  本发明涉及在苯环的位置2被取代的新型1-(N-苯基氨基烷基)哌嗪衍生物。还考虑包括本发明化合物的药物组合物。本发明化合物还被考虑用于治疗哺乳动物下尿路神经肌肉功能障碍。
• [EN] 1-(N-PHENYLAMINOALKYL)-PIPERAZINE DERIVATIVES SUBSTITUTED AT POSITION 2 OF THE PHENYL RING<br/>[FR] DERIVES DE 1-(N-PHENYLAMINOALKYL)-PIPERAZINE SUBSTITUES A LA POSITION 2 DU CYCLE PHENYLE
  申请人：RECORDATI S.A., CHEMICAL AND PHARMACEUTICAL COMPANY

  公开号：WO1999006384A1

  公开（公告）日：1999-02-11

  (EN) 1-(N-phenylaminoalkyl)-piperazine derivatives of formula (I), (R = H, alkyl-CO, cycloalkyl-CO, substituted cycloalkyl-CO or monocyclic heteroaryl-CO; R1 = H or lower alkyl; R2 = halogen, alkoxy, phenoxy, NO2, CN, acyl, NH2, NH(acyl), alkyl-SO2NH, alkoxycarbonyl, NH2CO, (alkyl)NHCO, (alkyl)2NCO, (acyl)NHCO, CF3 or polyfluoroalkoxy; B = benzyl or mono- or bicyclic aryl or heteroaryl, all optionally substituted) bind to 5HT1A receptors and are useful for the treatment of neuromuscular dysfunctions of the lower urinary tract. The use of these compounds for the preparation of a medicament for this treatment is claimed, and some of the compounds (with restricted B values) are claimed per se.(FR) L'invention concerne des dérivés de 1-(N-phénylaminoalkyl)-pipérazine qui correspondent à la formule (I) (R=H, alkyl-CO, cycloalkyl-CO, cycloalkyl-CO substitué ou hétéroaryl-CO monocyclique; R1=H ou alkyle inférieur; R2=halogène, alcoxy, phénoxy, NO2, CN, acyle, NH2, NH(acyle), alkyl-SO2NH, alcoxycarbonyle, NH2CO, (alkyl)NHCO, (alkyl)2NCO, (acyl)NHCO, CF3 ou polyfluoroalcoxy; B = benzyle ou hétéroaryle ou aryle mono- ou bicyclique, tous éventuellement substitués). Ces dérivés se lient aux récepteurs 5HT1A, et sont utiles lors du traitement de dysfonctionnements neuro-musculaires des voies urinaires inférieures. Cette invention concerne également l'utilisation de ces composés dans la préparation d'un médicament utilisé pour ce traitement, ainsi que certains de ces composés dont la valeur B est réduite.

  1-(N-苯基氨基烷基)-哌嗪衍生物的化学式为(I)，其中(R = H，烷基-CO，环烷基-CO，取代环烷基-CO或单环杂环基-CO; R1 = H或低烷基; R2 = 卤素，烷氧基，苯氧基，NO2，CN，酰基，NH2，NH(酰基)，烷基-SO2NH，烷氧羰基，NH2CO，(烷基)NHCO，(烷基)2NCO，(酰基)NHCO，CF3或多氟烷氧基; B = 苄基或单环或双环芳基或杂芳基，均可选配取代基)，可与5HT1A受体结合，并用于治疗下泌尿道神经肌肉功能障碍。本发明声明了这些化合物用于制备此类治疗药物，并声明了一些化合物（具有限定的B值）本身。
• 1-(N-phenylaminoalkyl)piperazine derivatives substituted at position 2 of the phenyl ring
  申请人：Recordati S.A. Chemical and Pharmaceutical Company

  公开号：US06399614B1

  公开（公告）日：2002-06-04

  The present invention is directed to novel 1-(N-phenylaminoalkyl)piperazine derivatives substituted at the position 2 of the phenyl ring. Pharmaceutical compositions comprising the compounds of the invention also are contemplated. The compounds of the present invention also are contemplated for use in treating neuromuscular dysfunction of the lower urinary tract in a mammal.

  本发明涉及一种新型1-(N-苯基氨基烷基)哌嗪衍生物，其在苯环的2号位上被取代。本发明还考虑了包含该化合物的药物组合物。本发明的化合物还可用于治疗哺乳动物下泌尿道神经肌肉功能障碍。
• Combination therapy with 5HT 1A and 5HT 1B-receptor antagonists
  申请人：Leonardi Amedeo

  公开号：US20050165025A1

  公开（公告）日：2005-07-28

  Described is the novel use of combinations of molecules endowed with antagonistic activity toward the serotonin 5-HT 1A or 5-HT 1B receptor, and of molecules simultaneously endowed with antagonistic activity at both said receptors. These compounds and their enantiomers, diastereoisomers, N-oxides, polymorphs, solvates, prodrugs, and pharmaceutically acceptable salts are useful in the treatment of patients with neuromuscular dysfunction of the lower urinary tract. Also described are the pharmaceutical compositions containing them. There is also provided a method of therapeutic treatment of urinary disorders in a mammal, including man, comprising administering to said mammal, including man, in need of such treatment, a therapeutically effective amount of a composition according to the invention.

  描述了具有拮抗血清素 5-HT 1A 或 5-HT 1B 受体具有拮抗活性的分子组合，以及同时对上述两种受体具有拮抗活性的分子组合。这些化合物及其对映体、非对映异构体、N-氧化物、多晶型物、溶解物、原药和药学上可接受的盐可用于治疗下尿路神经肌肉功能障碍患者。还描述了含有它们的药物组合物。还提供了一种治疗哺乳动物（包括人）泌尿系统疾病的方法，包括给需要这种治疗的哺乳动物（包括人）施用治疗有效量的根据本发明的组合物。
• LEISHMANIA ANTIGENS FOR USE IN THE THERAPY AND DIAGNOSIS OF LEISHMANIASIS
  申请人：CORIXA CORPORATION

  公开号：EP1287026B1

  公开（公告）日：2005-11-23