GW2433 | 227941-61-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: GW2433
• 英文别名: GW-2433；2-[4-[3-[2-(2-Chloro-6-fluorophenyl)ethyl-[(2,3-dichlorophenyl)carbamoyl]amino]propyl]phenoxy]-2-methylpropanoic acid
• CAS: 227941-61-9
• 化学式: C₂₈H₂₈Cl₃FN₂O₄
• 分子量: 581.899
• InChiKey: YMWJDWJXIXITMD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.5
• 重原子数：
  38
• 可旋转键数：
  11
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  78.9
• 氢给体数：
  2
• 氢受体数：
  5

制备方法与用途

GW2433是一种激活PPAR受体的化合物。

反应信息

• 作为反应物：
  描述：

  硫辛酸氨基丁三醇盐 、 法格立他扎 、 FK614 、 5-[(2,4-二氧代噻唑啉-5-基)甲基]-2-甲氧基-N-[[4-(三氟甲基)苯基]甲基]苯甲酰胺 、 巴格列酮 、 4-[2-(2-9H-Fluoren-9-yl-acetylamino)-ethyl]-benzoic acid 2-[2-methoxy-2-(3-trifluoromethyl-phenyl)-ethylamino]-ethyl ester 、 KB-R7785 、 苯(甲)醛,2-(4-羟基-1-哌啶基)- 、 ragaglitazar 、 、 GW2433 、 、 hinnuliquinone 、 去甲基阿斯吲醒 B1 生成 利格列酮
  参考文献：
  名称：

  Drug comprising combination

  摘要：

  一种包含胰岛素增敏剂和HMG-CoA还原酶抑制剂的TNF-α抑制剂，可用作预防或治疗炎症性疾病等的药物。

  公开号：

  US20030060488A1

文献信息

• Compositions and methods for treating obesity, obesity related disorders and for inhibiting the infectivity of human immunodeficiency virus
  申请人：Lee-Huang Sylvia

  公开号：US20090061031A1

  公开（公告）日：2009-03-05

  The present invention relates to methods and pharmaceutical compositions for treating obesity or obesity-related disorders in a subject suffering from or predisposed to developing obesity or an obesity-related disorder, or for inhibiting the infectivity of HIV, by administering oleuropein, an analogue or derivative thereof, or the major metabolites of oleuropein including oleuropein aglycone, hydroxytyrosol, and elenolic acid or their analogues, or derivatives thereof, an iridoid glycoside, or a secoiridoid glycoside or analogues or derivatives thereof, or any combination of the foregoing including olive leave extract. The invention also relates to methods for screening/diagnosing a subject having, or predisposed to having obesity or a related disorder by measuring the expression profiles of an adipogenic gene selected from PPARγ2, LPL and αP2 gene and gene product, or other adipogenic, lipogenic, or lipolytic genes and gene products in an individual. The invention further provides for screening for novel oleuropein analogues.

  本发明涉及一种治疗肥胖或肥胖相关疾病的方法和制药组合物，该方法适用于患有或易于发展肥胖或肥胖相关疾病的个体，或用于抑制HIV的感染，通过给予欧洲橄榄苦苷、其类似物或衍生物，或欧洲橄榄苦苷的主要代谢产物，包括欧洲橄榄苦苷去糖基体、羟基酪醇和环醇酸或其类似物、衍生物、一种虫草苷苷苷或一种secoiridoid苷苷苷或其类似物或衍生物，或上述任何组合，包括橄榄叶提取物。本发明还涉及通过测量从PPARγ2、LPL和αP2基因和基因产物选择的脂肪生成基因或其他脂肪生成、脂肪合成或脂解基因和基因产物的表达谱来筛选/诊断患有或易于患有肥胖或相关疾病的个体的方法。本发明还提供了筛选新欧洲橄榄苦苷类似物的方法。
• Activator of peroxisome proliferator-activated receptor delta
  申请人：Sakuma Shogo

  公开号：US20070027196A1

  公开（公告）日：2007-02-01

  A compound represented by the formula (I) or a salt of the compound, and a PPAR-δ activator which contains the compound or salt as the active ingredient: (wherein A represents O or S; B 1 represents N, etc.; B 2 represents O, etc.; each of X 1 and X 2 represents O, S, a bond, etc.; Y represents C 1-8 alkylene chain; z represents O or S; R 1 represents aryl, etc. which can have substituents; R 2 represents C 1-8 alkyl, etc.; R 3 represents C 1-8 alkyl, C 2-8 alkenyl, etc.; each of R 4 and R 5 represents hydrogen, C 1-8 alkyl, etc.; and R 6 represents hydrogen, etc.; provided that each of Z and R 3 is attached to the benzene ring, and X 2 is not attached to the benzene ring).

  化合物的化学式为(I)或该化合物的盐，以及含有该化合物或盐为活性成分的PPAR-δ激动剂：（其中A代表O或S；B1代表N等；B2代表O等；X1和X2分别代表O、S、键等；Y代表C1-8烷基链；z代表O或S；R1代表苯基等，可以有取代基；R2代表C1-8烷基等；R3代表C1-8烷基、C2-8烯基等；R4和R5分别代表氢、C1-8烷基等；R6代表氢等；但要求Z和R3均连接到苯环上，且X2未连接到苯环上）。
• Activator for peroxisome proliferator-activated receptor delta
  申请人：Sakuma Shogo

  公开号：US20080009631A1

  公开（公告）日：2008-01-10

  A compound represented by the following general formula (I): (wherein R 1 represents phenyl, etc. which can have substituents selected from the group consisting of C 1-8 alkyl, C 1-8 alkyl having halogen, halogen, hydroxyl, etc.; R 2 represents C 1-8 alkyl, etc.; A represents oxygen, sulfur, etc.; X represents C 1-8 alkylene chain, etc.; Y represents C(═O), CH═CH, etc.; R 3 , R 4 , and R 5 each represents hydrogen, C 1-8 alkyl, etc.; B represents CH or nitrogen; Z represents oxygen or sulfur; R 6 and R 7 each represents hydrogen, C 1-8 alkyl, etc.; and R 8 represents hydrogen or C 1-8 alkyl; provided that at least one of R 3 , R 4 , and R 5 is not hydrogen) or a salt of the compound; and a PPAR-δ activator which contains the compound or salt as the active ingredient.

  以下是一种由下列通式（I）表示的化合物：（其中，R1代表苯基等，可以具有选自C1-8烷基，具有卤素的C1-8烷基，卤素，羟基等的取代基; R2代表C1-8烷基等; A代表氧，硫等; X代表C1-8烷基链等; Y代表C(═O)，CH═CH等; R3、R4和R5各代表氢，C1-8烷基等; B代表CH或氮; Z代表氧或硫; R6和R7各代表氢，C1-8烷基等; R8代表氢或C1-8烷基; 前提是R3、R4和R5中至少有一个不是氢）或该化合物的盐;以及包含该化合物或盐作为活性成分的PPAR-δ激动剂。
• Compositions and Methods for Treating Obesity, Obesity Related Disorders and for Inhibiting the Infectivity of Human Immunodeficiency Virus
  申请人：The General Hospital Corporation

  公开号：US20140296141A1

  公开（公告）日：2014-10-02

  The present invention relates to methods and pharmaceutical compositions for treating obesity or obesity-related disorders in a subject suffering from or predisposed to developing obesity or an obesity-related disorder, or for inhibiting the infectivity of HIV, by administering oleuropein, an analogue or derivative thereof, or the major metabolites of oleuropein including oleuropein aglycone, hydroxytyrosol, and elenolic acid or their analogues, or derivatives thereof, an iridoid glycoside, or a secoiridoid glycoside or analogues or derivatives thereof, or any combination of the foregoing including olive leave extract. The invention also relates to methods for screening/diagnosing a subject having, or predisposed to having obesity or a related disorder by measuring the expression profiles of an adipogenic gene selected from PPARγ2, LPL and αP2 gene and gene product, or other adipogenic, lipogenic, or lipolytic genes and gene products in an individual. The invention further provides for screening for novel oleuropein analogues.

  本发明涉及使用欧洲橄榄苷、其类似物或衍生物，或欧洲橄榄苷的主要代谢产物，包括欧洲橄榄苷苷元、羟基酪醇和羟基酪醛酸或其类似物或衍生物、半萜苷苷元或半萜苷苷元类似物或衍生物，或上述任何组合物，包括橄榄叶提取物，用于治疗患有或易于发展肥胖症或肥胖相关疾病的受体，或用于抑制HIV的感染。本发明还涉及通过测量个体中PPARγ2、LPL和αP2基因和基因产物或其他脂肪生成、脂肪生成或脂肪分解基因和基因产物的表达谱来筛选/诊断患有或易于患有肥胖症或相关疾病的受体的方法。本发明还提供筛选新的欧洲橄榄苷类似物的方法。
• PHARMACEUTICAL COMPRISING PPAR AGONIST
  申请人：Senju Pharmaceutical Co., Ltd.

  公开号：EP1964575A1

  公开（公告）日：2008-09-03

  An object of the present invention is to provide an agent for promoting proliferation of a meibomian gland epithelial cell and a corneal epithelial cell, as well as provide an agent for treating an ocular disease such as meibomian gland dysfunction or evaporative dry eye. There are provided an agent for promoting proliferation of a meibomian gland epithelial cell or a corneal epithelial cell, containing a PPARα or δ agonist as an active ingredient, as well as an agent for treating an ocular disease such as meibomian gland dysfunction or evaporative dry eye, containing a PPARα or δ agonist as an active ingredient.

  本发明的目的是提供一种促进睑板腺上皮细胞和角膜上皮细胞增殖的制剂，以及提供一种治疗睑板腺功能障碍或蒸发性干眼症等眼部疾病的制剂。 提供了一种促进睑板腺上皮细胞或角膜上皮细胞增殖的制剂，其中含有 PPARα 或 δ 激动剂作为活性成分，还提供了一种治疗眼部疾病如睑板腺功能障碍或蒸发性干眼症的制剂，其中含有 PPARα 或 δ 激动剂作为活性成分。