4-{(S)-2-[(S)-2-(methoxycarbonylamino)-3-phenylpropanamido]-2-(5-phenylthiazol-2-yl)ethyl}phenylsulfamic acid | 1235331-05-1

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 4-{(S)-2-[(S)-2-(methoxycarbonylamino)-3-phenylpropanamido]-2-(5-phenylthiazol-2-yl)ethyl}phenylsulfamic acid
• 英文别名: [4-[(2S)-2-[[(2S)-2-(methoxycarbonylamino)-3-phenylpropanoyl]amino]-2-(5-phenyl-1,3-thiazol-2-yl)ethyl]phenyl]sulfamic acid
• CAS: 1235331-05-1
• 化学式: C₂₈H₂₈N₄O₆S₂
• 分子量: 580.686
• InChiKey: FILDUXUCFHCOQA-ZEQRLZLVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  40
• 可旋转键数：
  12
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  183
• 氢给体数：
  4
• 氢受体数：
  9

文献信息

• HUMAN PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE
  申请人：Gray Jeffrey Lyle

  公开号：US20100016336A1

  公开（公告）日：2010-01-21

  The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis.

  本公开涉及有效作为人类蛋白酪氨酸磷酸酶β（HPTP-β）抑制剂的化合物，从而调节血管生成。本公开还涉及包含所述人类蛋白酪氨酸磷酸酶β（HPTP-β）抑制剂的组合物，以及调节血管生成的方法。
• COMPOSITIONS AND METHODS FOR TREATING OCULAR EDEMA, NEOVASCULARIZATION AND RELATED DISEASES
  申请人：Peters Kevin Gene

  公开号：US20120129847A1

  公开（公告）日：2012-05-24

  Disclosed are methods for the treatment of diseases or conditions of the eye, especially retinopathies, ocular edema and ocular neovascularization. Non-limiting examples of these diseases or conditions include diabetic macular edema, age-related macular degeneration (wet form), choroidal neovascularization, diabetic retinopathy, retinal vein occlusion (central or branch), ocular trauma, surgery induced edema, surgery induced neovascularization, cystoid macular edema, ocular ischemia, uveitis, and the like.

  本发明公开了治疗眼部疾病或病症的方法，特别是视网膜病变、眼部水肿和眼部新生血管形成。这些疾病或病症的非限制性示例包括糖尿病性黄斑水肿、老年性黄斑变性（湿性）、脉络膜新生血管形成、糖尿病性视网膜病变、视网膜静脉阻塞（中央或分支）、眼部创伤、手术引起的水肿、手术引起的新生血管形成、囊样黄斑水肿、眼部缺血、葡萄膜炎等。
• COMPOSITIONS AND METHODS FOR TREATING OCULAR DISEASES
  申请人：Aerpio Therapeutics Inc.

  公开号：US20150050277A1

  公开（公告）日：2015-02-19

  Disclosed herein are compositions and methods for treating ocular diseases, inter alia, diabetic macular edema, age-related macular degeneration (wet form), choroidal neovascularization, diabetic retinopathy, retinal vein occlusion (central or branch), ocular trauma, surgery induced edema, surgery induced neovascularization, cystoid macular edema, ocular ischemia, uveitis, and the like. These diseases or conditions are characterized by changes in the ocular vasculature whether progressive or non-progressive, whether a result of an acute disease or condition, or a chronic disease or condition.

  本文揭示了治疗眼部疾病的组合物和方法，包括糖尿病性黄斑水肿、老年性黄斑变性（湿型）、脉络膜新生血管、糖尿病视网膜病变、视网膜静脉阻塞（中心或分支）、眼部创伤、手术引起的水肿、手术引起的新生血管、囊样黄斑水肿、眼部缺血、葡萄膜炎等等。这些疾病或症状的特点是眼部血管的变化，无论是进行性还是非进行性，无论是急性疾病或症状的结果，还是慢性疾病或症状。
• COMPOSITIONS, FORMULATIONS AND METHODS FOR TREATING OCULAR DISEASES
  申请人：Aerpio Therapeutics, Inc.

  公开号：US20160220540A1

  公开（公告）日：2016-08-04

  Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed. Combination therapy with antibodies and PK/PD data are also disclosed.

  本文披露了一些有效激活Tie-2并抑制HPTP-beta的化合物。这些化合物可以为与血管生成有关的疾病，例如眼部疾病提供有效的治疗。本文还披露了增加溶解度的配方。同时，本文还披露了抗体的联合疗法和PK/PD数据。
• Compositions and methods for treating ocular diseases
  申请人：Aerpio Therapeutics, Inc.

  公开号：US10220048B2

  公开（公告）日：2019-03-05

  Disclosed herein are compositions and methods for treating ocular diseases, inter alia, diabetic macular edema, age-related macular degeneration (wet form), choroidal neovascularization, diabetic retinopathy, retinal vein occlusion (central or branch), ocular trauma, surgery induced edema, surgery induced neovascularization, cystoid macular edema, ocular ischemia, uveitis, and the like. These diseases or conditions are characterized by changes in the ocular vasculature whether progressive or non-progressive, whether a result of an acute disease or condition, or a chronic disease or condition.

  本文公开了用于治疗眼部疾病的组合物和方法，其中包括糖尿病性黄斑水肿、老年性黄斑变性（湿性）、脉络膜新生血管、糖尿病性视网膜病变、视网膜静脉闭塞（中心静脉或分支静脉）、眼外伤、手术诱发水肿、手术诱发新生血管、囊样黄斑水肿、眼部缺血、葡萄膜炎等。这些疾病或病症的特征是眼部血管发生变化，无论是进行性或非进行性的，无论是急性疾病或病症的结果，还是慢性疾病或病症的结果。