2-[2-[4-(4-methoxyphenyl)piperazin-1-yl]-4-phenyl-1,3-thiazol-5-yl]acetic Acid

• 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: 2-[2-[4-(4-methoxyphenyl)piperazin-1-yl]-4-phenyl-1,3-thiazol-5-yl]acetic Acid
• 化学式: C₂₂H₂₃N₃O₃S
• 分子量: 409.5
• InChiKey: ANDDADRRZBTHAI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  94.1
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• Thiazole Compounds and Their Use as PGD2 Antagonists
  申请人：Harris Neil Victor

  公开号：US20090221604A1

  公开（公告）日：2009-09-03

  A compound for use as a PGD2 antagonist is of structural formula [1] in which: A represents a fully saturated or partially unsaturated monocyclic 5-7 membered ring containing one or two nitrogen atoms; B represents a direct bond, an optionally substituted methylene group, an optionally substituted nitrogen atom, oxygen, or S(O) n , where n=0, 1, or 2; L represents a direct bond, or an optionally substituted alkylene or alkenylene group; R 1 represents an optionally substituted aryl or heteroaryl group, or an optionally substituted aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group; R 2 represents an optionally substituted aryl or heteroaryl group, or an optionally substituted aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group; X represents a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, sulfonic acid or a group of formula C(═O)NHSO 2 Y or SO 2 NHC(═O)Y; and Y represents an optionally substituted aryl or heteroaryl group or an optionally substituted alkyl or cycloalkyl group; or a N-oxide, pharmaceutically acceptable salt, solvate or prodrug thereof.

  可用作PGD2拮抗剂的化合物具有结构式[1]，其中：A代表一个完全饱和或部分不饱和的单环5-7成员环，其中包含一个或两个氮原子；B代表直接键，可选择性取代的亚甲基基团，可选择性取代的氮原子、氧或S（O）n，其中n = 0、1或2；L代表直接键或可选择性取代的烷基或烯基基团；R1代表可选择性取代的芳基或杂环芳基基团，或可选择性取代的芳基融合杂环烷基、杂环芳基融合环烷基、杂环芳基融合杂环烷基或芳基融合环烷基基团；R2代表可选择性取代的芳基或杂环芳基基团，或可选择性取代的芳基融合杂环烷基、杂环芳基融合环烷基、杂环芳基融合杂环烷基或芳基融合环烷基基团；X代表羧酸、四唑、3-羟基异噁唑、羟肟酸、磷酸酯、膦酸酯、膦酰胺、磺酸或式C（═O）NHSO2Y或SO2NHC（═O）Y的基团；Y代表可选择性取代的芳基或杂环芳基基团或可选择性取代的烷基或环烷基基团；或其N-氧化物、药学上可接受的盐、溶剂合物或前药。
• THIAZOLE COMPOUNDS AND THEIR USE AS PGD2 ANTAGONISTS
  申请人：Argenta Discovery Limited

  公开号：EP1922312A1

  公开（公告）日：2008-05-21
• METHODS OF TREATING THYROID EYE DISEASE
  申请人：Phipps Richard P.

  公开号：US20120015001A1

  公开（公告）日：2012-01-19

  The present invention relates to a methods and compositions for the treatment of and management of symptoms for thyroid eye disease. The methods include administering to a patient having thyroid eye disease an agent that interferes with hyaluronan synthesis in an amount that is effective to inhibit hyaluronan synthesis in a retro-ocular space. The pharmaceutical compositions hat includes a carrier suitable for ophthalmic delivery and an agent that interferes with hyaluronan synthesis. Combination therapies are also disclosed.
• US9320723B2
  申请人：——

  公开号：US9320723B2

  公开（公告）日：2016-04-26
• US9750749B2
  申请人：——

  公开号：US9750749B2

  公开（公告）日：2017-09-05