4-(pyridin-4-ylamino)-2-(4-chlorophenyl)quinazoline

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 4-(pyridin-4-ylamino)-2-(4-chlorophenyl)quinazoline
• 英文别名: 4-(4-pyridylamino)-2-(4-chlorophenyl)quinazoline；2-(4-chlorophenyl)-N-pyridin-4-ylquinazolin-4-amine
• 化学式: C₁₉H₁₃ClN₄
• 分子量: 332.792
• InChiKey: OTDSITCZDVDCNP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  50.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  4-氨基吡啶 、 4-氯-2-(4-氯苯基)-喹唑啉 在 potassium carbonate 作用下， 以 N-甲基乙酰胺 为溶剂， 生成 4-(pyridin-4-ylamino)-2-(4-chlorophenyl)quinazoline
  参考文献：
  名称：

  Quinazoline derivatives as medicaments

  摘要：

  该发明涉及使用下述公式的化合物或其药用盐来抑制TGF-β和/或p38-α激酶的方法，其中R3是非干扰取代基；每个Z是CR2或N，环A中不超过两个Z位置是N，并且环A中相邻的两个Z位置不能同时是N；每个R2是独立的非干扰取代基；L是连接基；n为0或1；Ar′是环状脂肪族、环状杂脂肪族、芳香族或杂芳香族残基，可选地取代1-3个非干扰取代基的残基。

  公开号：

  US06476031B1

文献信息

• Hyperglycosylated variants of interferon alfacon-1
  申请人：Alios Biopharma Inc.

  公开号：EP2093235A1

  公开（公告）日：2009-08-26

  The present invention provides synthetic Type I interferon receptor polypeptide agonists comprising consensus or hybrid Type I interferon receptor polypeptide agonists, containing one or more native or non-native glycosylation sites. The present invention provides synthetic Type I interferon receptor polypeptide agonists comprising consensus or hybrid Type I interferon receptor polypeptide agonists, containing one or more native or nonnative glycosylation sites, as well as erythropoietin and darbepoetin alfa, each of which are linked to a penetrating peptide that facilitates translocation of a substance across a biological barrier as well as pharmaceutical compositions, including oral formulations, of the same. The present invention further provides oral formulations of hyperglycosylated or protease-resistant, hyperglycosylated polypeptide variants, which polypeptide variants lack at least one protease cleavage site found in a parent polypeptide, and thus exhibit increased protease resistance compared to the parent polypeptide, which polypeptide variants further include (1) a carbohydrate moiety covalently linked to at least one non-native glycosylation site not found in the parent protein therapeutic or (2) a carbohydrate moiety covalently linked to at least one native glycosylation site found but not glycosylated in the parent protein therapeutic. The present invention further provides compositions, including oral pharmaceutical compositions, comprising the synthetic Type I interferon receptor polypeptide agonist, the hyperglycosylated polypeptide variant, or the hyperglycosylated, protease-resistant polypeptide variant. The present invention further provides containers, devices, and kits comprising the synthetic Type I interferon receptor polypeptide agonist, the hyperglycosylated polypeptide variant, or the hyperglycosylated, protease-resistant polypeptide variant. The present invention further provides therapeutic methods involving administering an effective amount of an oral pharmaceutical composition comprising a synthetic Type I interferon receptor polypeptide agonist, a hyperglycosylated polypeptide variant, or a hyperglycosylated, protease-resistant polypeptide variant to an individual in need thereof.

  本发明提供合成的I型干扰素受体多肽激动剂，包括共识或混合I型干扰素受体多肽激动剂，含有一个或多个原生或非原生糖基化位点。本发明提供合成的 I 型干扰素受体多肽激动剂，包括共识或混合 I 型干扰素受体多肽激动剂，含有一个或多个原生或非原生糖基化位点，以及促红细胞生成素和达贝胎素α，其中每一种都与促进物质通过生物屏障转运的穿透肽相连，以及药物组合物，包括其口服制剂。本发明进一步提供了高糖基化或抗蛋白酶的高糖基化多肽变体的口服制剂，这些多肽变体缺乏母体多肽中的至少一个蛋白酶裂解位点，因此与母体多肽相比表现出更强的抗蛋白酶能力、多肽变体进一步包括(1)与至少一个非原生糖基化位点共价连接的碳水化合物分子，该糖基化位点在母体蛋白治疗剂中未发现；或(2)与至少一个原生糖基化位点共价连接的碳水化合物分子，该糖基化位点在母体蛋白治疗剂中发现但未糖基化。本发明进一步提供了包含合成的 I 型干扰素受体多肽激动剂、高糖基化多肽变体或高糖基化、抗蛋白酶多肽变体的组合物，包括口服药物组合物。本发明进一步提供了包含合成 I 型干扰素受体多肽激动剂、高糖基化多肽变体或高糖基化、抗蛋白酶多肽变体的容器、装置和试剂盒。本发明进一步提供了治疗方法，包括向有需要的个体施用有效量的口服药物组合物，该组合物包含合成的I型干扰素受体多肽激动剂、高糖基化多肽变体或高糖基化、抗蛋白酶多肽变体。
• Synthetic hyperglycosylated, protease-resistant polypeptide variants, oral formulations and methods of using the same
  申请人：Hong Jin

  公开号：US20060182716A1

  公开（公告）日：2006-08-17

  The present invention provides synthetic Type I interferon receptor polypeptide agonists comprising consensus or hybrid Type I interferon receptor polypeptide agonists, containing one or more native or non-native glycosylation sites. The present invention further provides oral formulations of protease-resistant or protease-resistant, hyperglycosylated polypeptide variants, which polypeptide variants lack at least one protease cleavage site found in a parent polypeptide, and thus exhibit increased protease resistance compared to the parent polypeptide, which polypeptide variants further include (1) a carbohydrate moiety covalently linked to at least one non-native glycosylation site not found in the parent protein therapeutic or (2) a carbohydrate moiety covalently linked to at least one native glycosylation site found but not glycosylated in the parent protein therapeutic. The present invention further provides compositions, including oral pharmaceutical compositions, comprising the synthetic Type I interferon receptor polypeptide agonist, the hyperglycosylated polypeptide variant, the protease-resistant polypeptide variant, or the hyperglycosylated, protease-resistant polypeptide variant. The present invention further provides containers, devices, and kits comprising the synthetic Type I interferon receptor polypeptide agonist, the hyperglycosylated polypeptide variant, the protease-resistant polypeptide variant, or the hyperglycosylated, protease-resistant polypeptide variant. The present invention further provides therapeutic methods involving administering an effective amount of an oral pharmaceutical composition comprising a synthetic Type I interferon receptor polypeptide agonist, a hyperglycosylated polypeptide variant, a protease-resistant polypeptide variant, or a hyperglycosylated, protease-resistant polypeptide variant to an individual in need thereof.

  本发明提供合成的I型干扰素受体多肽激动剂，包括共识或混合I型干扰素受体多肽激动剂，含有一个或多个原生或非原生糖基化位点。本发明进一步提供了抗蛋白酶或抗蛋白酶、高糖基化多肽变体的口服制剂，这些多肽变体缺乏母体多肽中的至少一个蛋白酶裂解位点，因此与母体多肽相比，表现出更强的抗蛋白酶能力、多肽变体进一步包括(1)与至少一个非原生糖基化位点共价连接的碳水化合物分子，该糖基化位点在母体蛋白治疗剂中未发现；或(2)与至少一个原生糖基化位点共价连接的碳水化合物分子，该糖基化位点在母体蛋白治疗剂中发现但未糖基化。本发明进一步提供了包含合成的 I 型干扰素受体多肽激动剂、高糖基化多肽变体、抗蛋白酶多肽变体或高糖基化、抗蛋白酶多肽变体的组合物，包括口服药物组合物。本发明进一步提供了包含合成 I 型干扰素受体多肽激动剂、高糖基化多肽变体、抗蛋白酶多肽变体或高糖基化、抗蛋白酶多肽变体的容器、装置和试剂盒。本发明进一步提供了治疗方法，包括向有需要的个体施用有效量的口服药物组合物，该组合物包含合成的Ⅰ型干扰素受体多肽激动剂、高糖基化多肽变体、抗蛋白酶多肽变体或高糖基化、抗蛋白酶多肽变体。
• Synthetic hyperglycosylated, and hyperglycosylated protease-resistant polypeptide variants, oral formulations and methods of using the same
  申请人：Blatt M. Lawrence

  公开号：US20060204473A1

  公开（公告）日：2006-09-14

  The present invention provides synthetic Type I interferon receptor polypeptide agonists comprising consensus or hybrid Type I interferon receptor polypeptide agonists, containing one or more native or non-native glycosylation sites. The present invention provides synthetic Type I interferon receptor polypeptide agonists comprising consensus or hybrid Type I interferon receptor polypeptide agonists, containing one or more native or non-native glycosylation sites, as well as erythropoietin and darbepoetin alfa, each of which are linked to a penetrating peptide that facilitates translocation of a substance across a biological barrier as well as pharmaceutical compositions, including oral formulations, of the same. The present invention further provides oral formulations of hyperglycosylated or protease-resistant, hyperglycosylated polypeptide variants, which polypeptide variants lack at least one protease cleavage site found in a parent polypeptide, and thus exhibit increased protease resistance compared to the parent polypeptide, which polypeptide variants further include (1) a carbohydrate moiety covalently linked to at least one non-native glycosylation site not found in the parent protein therapeutic or (2) a carbohydrate moiety covalently linked to at least one native glycosylation site found but not glycosylated in the parent protein therapeutic. The present invention further provides compositions, including oral pharmaceutical compositions, comprising the synthetic Type I interferon receptor polypeptide agonist, the hyperglycosylated polypeptide variant, or the hyperglycosylated, protease-resistant polypeptide variant. The present invention further provides containers, devices, and kits comprising the synthetic Type I interferon receptor polypeptide agonist, the hyperglycosylated polypeptide variant, or the hyperglycosylated, protease-resistant polypeptide variant. The present invention further provides therapeutic methods involving administering an effective amount of an oral pharmaceutical composition comprising a synthetic Type I interferon receptor polypeptide agonist, a hyperglycosylated polypeptide variant, or a hyperglycosylated, protease-resistant polypeptide variant to an individual in need thereof.

  本发明提供合成的I型干扰素受体多肽激动剂，包括共识的或混合的I型干扰素受体多肽激动剂，含有一个或多个原生或非原生糖基化位点。本发明提供合成的 I 型干扰素受体多肽激动剂，包括共识或混合 I 型干扰素受体多肽激动剂，含有一个或多个原生或非原生糖基化位点，以及促红细胞生成素和达贝胎素α，其中每一种都与促进物质通过生物屏障转运的穿透肽相连，以及药物组合物，包括其口服制剂。本发明进一步提供了高糖基化或抗蛋白酶的高糖基化多肽变体的口服制剂，这些多肽变体缺乏母体多肽中的至少一个蛋白酶裂解位点，因此与母体多肽相比表现出更强的抗蛋白酶能力、多肽变体进一步包括(1)与至少一个非原生糖基化位点共价连接的碳水化合物分子，该糖基化位点在母体蛋白治疗剂中未发现；或(2)与至少一个原生糖基化位点共价连接的碳水化合物分子，该糖基化位点在母体蛋白治疗剂中发现但未糖基化。本发明进一步提供了包含合成的 I 型干扰素受体多肽激动剂、高糖基化多肽变体或高糖基化、抗蛋白酶多肽变体的组合物，包括口服药物组合物。本发明进一步提供了包含合成 I 型干扰素受体多肽激动剂、高糖基化多肽变体或高糖基化、抗蛋白酶多肽变体的容器、装置和试剂盒。本发明进一步提供了治疗方法，包括向有需要的个体施用有效量的口服药物组合物，该组合物包含合成的I型干扰素受体多肽激动剂、高糖基化多肽变体或高糖基化、抗蛋白酶多肽变体。
• US6184226
  申请人：——

  公开号：——

  公开（公告）日：——
• QUINAZOLINE DERIVATIVES AS MEDICAMENTS
  申请人：SCIOS INC.

  公开号：EP1107959A2

  公开（公告）日：2001-06-20