NEP inhibitor, 6p

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: NEP inhibitor, 6p
• 英文别名: 2-[(2-benzyl-3-sulfanylpropanoyl)amino]-1,3-thiazole-4-carboxylic acid
• 化学式: C₁₄H₁₄N₂O₃S₂
• 分子量: 322.4
• InChiKey: TZESSPPAPLHFEQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  21
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  109
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• [EN] ORGANIC COMPOUNDS<br/>[FR] COMPOSÉS ORGANIQUES
  申请人：INTRA CELLULAR THERAPIES INC

  公开号：WO2016022893A1

  公开（公告）日：2016-02-11

  The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.

  该发明涉及新型磷酸二酯酶1（PDE1）抑制剂，用于治疗由于某些cGMP/PKG介导的途径受到破坏或损害而表现出的疾病或紊乱（例如在心脏组织中）。该发明还涉及包含该抑制剂的药物组合物以及治疗心血管疾病和相关疾病的方法，例如充血性心力衰竭、动脉粥样硬化、心肌梗死和中风。
• ORGANIC COMPOUNDS
  申请人：Intra-Cellular Therapies, Inc.

  公开号：US20160039829A1

  公开（公告）日：2016-02-11

  The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.

  本发明涉及新型磷酸二酯酶1（PDE1）抑制剂，用于治疗由于某些cGMP/PKG介导的通路（例如在心脏组织中）受到破坏或损伤而表现出的疾病或障碍。本发明还涉及包含该抑制剂的制药组合物以及用于治疗心血管疾病和相关疾病的方法，例如充血性心脏病，动脉粥样硬化，心肌梗死和中风。
• COMPOUNDS CONTAINING S-N-VALERYL-N--VALINE AND (2R,4S)-5-BIPHENYL-4-YL-4-(3-CARBOXY-PROPIONYLAMINO)-2-METHYL-PENTANOIC ACID ETHYL ESTER MOIETIES AND CATIONS
  申请人：Feng Lili

  公开号：US20160324821A1

  公开（公告）日：2016-11-10

  A method for treatment of a cardiovascular or renal condition or disease with a specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi.

  一种治疗心血管或肾脏疾病的方法，使用特定组合、联接型前药或血管紧张素受体拮抗剂和NEPi化合物。
• Pharmaceutical combinations of an angiotensin receptor antagonist and an nep inhibitor
  申请人：Novartis AG

  公开号：EP2340828A1

  公开（公告）日：2011-07-06

  The invention relates to a dual-acting compound having the sum formula [((S)-N-valeryl-N-[2'-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine) ((2R,4S)-5-biphenyl4-yl-5-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester)]Na1-3 x H2O, wherein x is 0 to 3, and related invention embodiments. The dual-acting compound is an angiotensin receptor blocker and a neutral endopeptidase inhibitor.

  本发明涉及一种具有和式[((S)-N-缬氨酰-N-[2'-(1H-四唑-5-基)-联苯-4-基]-甲基}-缬氨酸)((2R,4S)-5-联苯-4-基-5-(3-羧基丙酰氨基)-2-甲基戊酸乙酯)]Na1-3 x H2O，其中x为0至3的双效化合物及相关的发明实施例。 双效化合物是血管紧张素受体阻滞剂和中性内肽酶抑制剂。
• PHARMACEUTICAL COMPOSITION
  申请人：Wuhan LL Science And Technology Development Co., Ltd.

  公开号：EP3524250A1

  公开（公告）日：2019-08-14

  The present invention relates to a pharmaceutical composition comprising: (a) at least one neutral endopeptidase inhibitor or a pharmaceutically acceptable salt or ester thereof, (b) at least one compound represented by formula (I) or a pharmaceutically acceptable salt or ester thereof, and a pharmaceutically acceptable carrier. Combined administration showed better medicinal effects than separate administration.

  本发明涉及一种药物组合物，它包含：(a) 至少一种中性内肽酶抑制剂或其药学上可接受的盐或酯；(b) 至少一种由式（I）代表的化合物或其药学上可接受的盐或酯；以及一种药学上可接受的载体。联合用药比单独用药显示出更好的药效。