7-amino-3-benzyl-1,2,3,4-tetrahydro-1-phenylpyrido[2,3-d]pyrimidine-2,4-dione

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶并嘧啶类
• 英文名称: 7-amino-3-benzyl-1,2,3,4-tetrahydro-1-phenylpyrido[2,3-d]pyrimidine-2,4-dione
• 英文别名: 7-Amino-3-benzyl-1-phenylpyrido[2,3-d]pyrimidine-2,4-dione
• 化学式: C₂₀H₁₆N₄O₂
• 分子量: 344.373
• InChiKey: SBYBOXFTOPFTFZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  79.5
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Therapeutic agent for dermatitis
  申请人：——

  公开号：US20010056097A1

  公开（公告）日：2001-12-27

  The present invention provides a therapeutic agent for dermatitis, particularly a therapeutic agent for atopic dermatitis, which is very safe and which shows few adverse side-effects in comparison to, for example, steroidal agents. The present invention relates to a therapeutic agent containing a compound represented by the following formula (I) or a pharmaceutically acceptable salt or hydrate thereof as an effective ingredient: 1 wherein R is hydrogen or a halogen. The therapeutic agent for dermatitis according to the present invention effectively and in a dose-dependent manner suppresses antigen-induced swelling in a mouse ear, a recognized animal model for atopic dermatitis, and suppresses the antigen-induced flare-up reaction in mice which occurred with the swelling reaction. In addition, no adverse reaction in the skin are observed.

  本发明提供了一种治疗皮炎，特别是治疗特应性皮炎的治疗剂，与例如类固醇类药物相比，该治疗剂非常安全，并且显示出很少的不良副作用。本发明涉及一种治疗剂，其包含以下式(I)所代表的化合物或其药学上可接受的盐或水合物作为有效成分：1其中R是氢或卤素。根据本发明的皮炎治疗剂能够有效地、剂量依赖地抑制小鼠耳朵抗原诱导的肿胀，这是一种被公认为特应性皮炎的动物模型，并且抑制了伴随肿胀反应发生的小鼠抗原诱导的红斑反应。此外，没有观察到皮肤的不良反应。
• 7-Aminopyrido(2,3-d)-pyrimidine derivatives for treatment of bronchial asthma
  申请人：NIPPON ZOKI PHARMACEUTICAL CO., LTD.

  公开号：EP0994113A2

  公开（公告）日：2000-04-19

  The invention provides 7-amino-1-phenylpyrido[2,3-d]pyrimidine-2,4-dione derivatives of the formula (I) or a pharmaceutically acceptable salt or hydrate thereof; wherein R1 is hydrogen, lower alkenyl, phenyl or optionally substituted lower alkyl which is optionally substituted with a substituent selected from oxo; lower alkoxy; phenyl which is optionally substituted with one or more lower alkyl, lower alkoxy, carboxyl, lower alkoxycarbonyl, mercapto, halogen, trifluoromethyl and/or nitro; naphthyl; furyl; isoxazolyl which is optionally substituted with one or more lower alkyl; pyridyl which is optionally substituted with one or more lower alkyl and/or halogen; thienyl which is optionally substituted with halogen; and 1,3-dioxolanyl; and R2, R3 and R4 each independently is hydrogen, halogen, lower alkoxy, benzyloxy, carboxyl or lower alkoxycarbonyl, which is useful for a therapeutic agent for bronchial asthma by exhibiting excellent bronchial dilating action as well as high safety and a favorable behavior in vivo.

  本发明提供了式 (I) 的 7-氨基-1-苯基吡啶并[2,3-d]嘧啶-2,4-二酮衍生物或其药学上可接受的盐或水合物； 其中 R1 是氢、低级烯基、苯基或任选被选自以下取代基取代的低级烷基：氧代；低级烷氧基；任选被一个或多个低级烷基、低级烷氧基、羧基、低级烷氧羰基、巯基、卤素、三氟甲基和/或硝基取代的苯基；萘基；呋喃基；任选被一个或多个低级烷基取代的异噁唑基；任选被一个或多个低级烷基和/或卤素取代的吡啶基；任选被卤素取代的噻吩基；以及 1,3-二氧戊环基；以及 R2、R3 和 R4 各自独立地为氢、卤素、低级烷氧基、苄氧基、羧基或低级烷氧羰基、 该化合物具有优异的支气管扩张作用，安全性高，在体内表现良好，可作为支气管哮喘的治疗剂。
• Therapeutic agent for the treatment of dermatitis
  申请人：NIPPON ZOKI PHARMACEUTICAL CO., LTD.

  公开号：EP1145716A2

  公开（公告）日：2001-10-17

  The present invention provide a therapeutic agent for dermatitis, particularly a therapeutic agent for atopic dermatitis, having high safety and showing little adverse reaction such as steroidal agent. The present invention relates to a therapeutic agent for dermatitis, particularly a therapeutic agent for atopic dermatitis, containing a compound represented by the following formula (I) or a pharmaceutically acceptable salt or hydrate thereof as an effective ingredient. (In the formula, R is hydrogen or halogen.) The therapeutic agent for dermatitis according to the present invention significantly and dose-dependently suppressed the antigen-induced swelling reaction in ear of mouse recognized as an animal model for atopic dermatitis. Also, the agent suppressed the antigen-induced flare reaction of mice occurred with the swelling reaction. In addition, the adverse reaction to the skin was not observed. The therapeutic agent for dermatitis of this invention is, therefore, is very useful as a drug for atopic dermatitis with high safety.

  本发明提供了一种皮炎治疗剂，特别是特应性皮炎治疗剂，其安全性高，不良反应小，如类固醇制剂。 本发明涉及一种皮炎治疗剂，特别是特应性皮炎治疗剂，其有效成分含有下式（I）代表的化合物或其药学上可接受的盐或水合物。 (式中，R 为氢或卤素）。 根据本发明的皮炎治疗剂可显著抑制作为特应性皮炎动物模型的小鼠耳部的抗原诱导肿胀反应，且其抑制作用与剂量有关。此外，本发明的药剂还能抑制小鼠在发生肿胀反应时由抗原诱发的发炎反应。此外，也没有观察到对皮肤的不良反应。因此，本发明的皮炎治疗剂作为治疗特应性皮炎的药物非常有用，而且安全性高。
• US6242452B1
  申请人：——

  公开号：US6242452B1

  公开（公告）日：2001-06-05
• US6440978B2
  申请人：——

  公开号：US6440978B2

  公开（公告）日：2002-08-27