2-Propenamide, N-((2R)-2,3-dihydro-2-hydroxy-1H-inden-4-yl)-3-(2-(1-piperidinyl)-4-(trifluoromethyl)phenyl)-, (2E)- | 1041478-78-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 2-Propenamide, N-((2R)-2,3-dihydro-2-hydroxy-1H-inden-4-yl)-3-(2-(1-piperidinyl)-4-(trifluoromethyl)phenyl)-, (2E)-
• 英文别名: (E)-N-[(2R)-2-hydroxy-2,3-dihydro-1H-inden-4-yl]-3-[2-piperidin-1-yl-4-(trifluoromethyl)phenyl]prop-2-enamide
• CAS: 1041478-78-7
• 化学式: C₂₄H₂₅F₃N₂O₂
• 分子量: 430.5
• InChiKey: HAZYXDWNLMGLIS-LHUXKHBRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  31
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  52.6
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• NOVEL BENZAMIDE DERIVATIVE AND USE THEREOF
  申请人：VIVOZON, INC.

  公开号：US20140336378A1

  公开（公告）日：2014-11-13

  Disclosed are a novel benzamide derivative and pharmaceutical use thereof, and more particularly, a novel benzamide derivative having a structure of Formula 1 or pharmaceutically acceptable salts thereof, and a composition for prevention or treatment of pain or itching including the above material. The novel benzamide derivative and pharmaceutically acceptable salt thereof according to the present invention exhibit excellent pain-suppressive effect and, in particular, pain-suppressive effect in not only a neuropathic animal model but also other models such as a formalin model, and therefore, may be used in suppression of different pains such as nociceptive pain, chronic pain, etc. Further, since it was demonstrated that the present invention displays anti-pruritic efficacy even in an itching model, to which a mechanism and treatment concept established with respect to pain is applied, the present invention may also be effectively used in radical treatment of atopic dermatitis by applying the inventive product to an anti-pruritic composition in order to suppress an initial itching stage and treat symptoms thereof, thus preventing skin damage or inflammation after the scratching stage.

  揭示了一种新的苯甲酰胺衍生物及其药用，更具体地说，一种具有化学式1结构或其药用盐的新苯甲酰胺衍生物，以及包括上述材料的用于预防或治疗疼痛或瘙痒的组合物。根据本发明，所述新的苯甲酰胺衍生物及其药用盐表现出优异的镇痛效果，特别是在不仅神经病理动物模型中而且其他模型如福尔马林模型中表现出的镇痛效果，因此，可用于抑制不同类型的疼痛，如伤害性疼痛、慢性疼痛等。此外，由于证明了本发明在瘙痒模型中显示出抗瘙痒功效，应用于疼痛方面建立的机制和治疗概念，因此，本发明还可通过将创新产品应用于抗瘙痒组合物中，以抑制初始瘙痒阶段并治疗其症状，从而预防刮痒阶段后的皮肤损伤或炎症。
• MODULATORS AND METHODS FOR THE TREATMENT OF ROSACEA
  申请人：Aubert Jerome

  公开号：US20140031341A1

  公开（公告）日：2014-01-30

  An in vitro method of screening candidate compounds for the preventive or curative treatment of rosacea is described. The method can include determining the capacity of a compound to modulate the expression or activity of the Transient Receptor Potential (TRPs), as well as the use of modulators of the expression or activity of this transcription factor for the treatment of rosacea. The method can also include in vitro diagnosis or prognosis of this pathology.
• Method to Abate Acute Airway Hypersensitivity and Asthma Attacks
  申请人：UTI Limited Partnership

  公开号：US20200215085A1

  公开（公告）日：2020-07-09

  Methods for prevention and treatment of asthma attacks involve the administration of one or more TRPV1 antagonists, one or more LPAr antagonists or preferably a combination of one or more TRPV1 antagonists and one or more LPAr antagonists. TRPV1 antagonists and/or LPAr antagonists or a combination of both inhibit or prevent carotid body activation during an acute asthma attack. TRPV1 antagonists, LPAr antagonists or a combination thereof are useful for preventing or ameliorating the symptoms of asthma attacks. Pharmaceutical compositions for use in treating asthma and more specifically for preventing or treating asthma attacks comprise a combination of a TRPV1 antagonist and an LPAr antagonist. Methods for making medicaments for such treatment are provided. Also provided are kits for treating asthma and for preventing or treating asthma attacks in which a TRPV1 antagonist and an LPAr antagonist are separately formulated for administration at the same time.
• CAPSAICIN AND TRPV1 MODULATOR COMBINATIONS AND METHODS OF USE THEREOF
  申请人：Pano Therapeutics, Inc.

  公开号：US20220098143A1

  公开（公告）日：2022-03-31

  Provided herein are combinations of capsaicin and TrpV1 modulators that are useful for treating capsaicin-responsive diseases or disorders.
• US9359346B2
  申请人：——

  公开号：US9359346B2

  公开（公告）日：2016-06-07