1-[6-(5-methyl-2-{[2-(tetrahydro-2H-pyran-4-yl)-1,2,3,4-tetrahydroisoquinolin-6-yl]methoxy}phenyl)pyridin-2-yl]-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid | 1398411-37-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 1-[6-(5-methyl-2-{[2-(tetrahydro-2H-pyran-4-yl)-1,2,3,4-tetrahydroisoquinolin-6-yl]methoxy}phenyl)pyridin-2-yl]-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid
• 英文别名: 1-[6-[5-methyl-2-[[2-(oxan-4-yl)-3,4-dihydro-1H-isoquinolin-6-yl]methoxy]phenyl]pyridin-2-yl]-5-(trifluoromethyl)pyrazole-4-carboxylic acid
• CAS: 1398411-37-4
• 化学式: C₃₂H₃₁F₃N₄O₄
• 分子量: 592.618
• InChiKey: LMECIGJXULIQBI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  43
• 可旋转键数：
  7
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.34
• 拓扑面积：
  89.7
• 氢给体数：
  1
• 氢受体数：
  10

文献信息

• SOLUBLE GUANYLATE CYCLASE ACTIVATORS
  申请人：Brenneman Jehrod Burnett

  公开号：US20130065918A1

  公开（公告）日：2013-03-14

  The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A and B are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

  本发明涉及式(I)的化合物及其药学上可接受的盐，其中R1，R2，R3，R4，R5，R6，A和B的定义如本文所述。本发明还涉及包含这些化合物的制药组合物，使用这些化合物治疗各种疾病和障碍的方法，制备这些化合物的过程以及这些过程中有用的中间体。
• THE USE OF SGC STIMULATORS AND SGC ACTIVATORS ALONE OR IN COMBINATION WITH PDE5 INHIBITORS FOR THE TREATMENT OF BONE DISORDERS INCLUDING OSTEOGENESIS IMPERFECTA (OI)
  申请人：Bayer AG

  公开号：EP3498298A1

  公开（公告）日：2019-06-19

  The present invention relates to sGC stimulators and sGC activators alone or in combination with PDE5 inhibitors or other combination partners for use in the treatment and/or prophylaxis of bone disorders, including osteogenesis imperfecta (OI).

  本发明涉及sGC刺激剂和sGC激活剂，可单独使用，也可与PDE5抑制剂或其他组合伙伴结合使用，用于治疗和/或预防骨质紊乱，包括成骨不全症（OI）。
• THE USE OF NON-STEROIDAL MINERALOCORTICOID RECEPTOR ANTAGONISTS ALONE OR IN COMBINATION FOR THE TREATMENT OF MUSCULAR OR NEUROMUSCULAR DISEASES
  申请人：Bayer Aktiengesellschaft

  公开号：EP3566704A1

  公开（公告）日：2019-11-13

  The present disclosure relates to non-steriodal mineralocorticoid receptor (MR) and the pharmacology of mineralocorticoid receptor antagonists (MR Antagonists, MRAs). In particular, the invention relates to MRAs alone (preferably finerenone), or preferably in combination with sGC stimulators and/or sGC activators (preferably BAY 41-2272), for use in the prevention and/or treatment of muscular or neuromuscular diseases, especially for the treatment of Duchenne Muscular Dystrophy (DMD).

  本公开涉及非甾体类矿物皮质激素受体（MR）和矿物皮质激素受体拮抗剂（MR 拮抗剂，MRAs）的药理学。特别是，本发明涉及单独使用（优选非格列酮）或优选与sGC刺激剂和/或sGC激活剂（优选BAY 41-2272）联合使用的MRAs，用于预防和/或治疗肌肉或神经肌肉疾病，特别是治疗杜氏肌肉萎缩症（DMD）。
• METHOD OF IDENTIFYING A SUBGROUP OF PATIENTS SUFFERING FROM DCSSC WHICH BENEFITS FROM A TREATMENT WITH SGC STIMULATORS AND SGC ACTIVATORS IN A HIGHER DEGREE THAN A CONTROL GROUP
  申请人：Adverio Pharma GmbH

  公开号：EP3574905A1

  公开（公告）日：2019-12-04

  The present invention relates to a method of identifying a subgroup of patients suffering from diffuse cutaneous systemic sclerosis (dcSSc) which subgroup of patients benefits from a treatment with at least one sGC stimulator and/or sGC activator in a higher degree than patients not belonging to this subgroup.

  本发明涉及一种确定弥漫性皮肤系统性硬化症（dcSSc）患者亚群的方法，该亚群患者从至少一种sGC刺激剂和/或sGC激活剂的治疗中获益的程度高于不属于该亚群的患者。
• THE USE OF SGC ACTIVATORS AND SGC STIMULATORS FOR THE TREATMENT OF COGNITIVE IMPAIRMENT
  申请人：Bayer Aktiengesellschaft

  公开号：EP3787610A1

  公开（公告）日：2021-03-10