3-(Cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide 3-(环丙甲氧基)-N-(3,5-二氯-4-吡啶基)-4-(二氟甲氧基)苯甲酰胺

CAS 162401-32-3 MFCD00938270

化学结构图

162401-32-3
SMILES: O=C(Nc1c(Cl)cncc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1

化学属性

Mol. FormulaC17H14Cl2F2N2O3
Mol. Weight403.21
Melting Point157.0 to 161.0 deg-C
Appearance solid powder
SolubilitySoluble in DMSO.

别名和识别编码

Chemical Name3-(Cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
CAS Number162401-32-3
Synonym 3-(Cyclopropylmethoxy)-N-(3,5-dichloro-4-pyridinyl)-4-(difluoromethoxy)benzamide B 9302-107 BY 217 BY217; BY-217; BY 217; B 9302-107; B9302-107; B-9302-107; BYK 20869; BYK-20869; BYK20869; Daxas; Daliresp BYK 20869
MDL NumberMFCD00938270
Chemical Name Translation3-(环丙甲氧基)-N-(3,5-二氯-4-吡啶基)-4-(二氟甲氧基)苯甲酰胺
Reaxys-RN9802592
Merck Number8249
PubChem Substance ID354334855
FormulaC17H14Cl2F2N2O3
IUPAC Name3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
InChIKeyMNDBXUUTURYVHR-UHFFFAOYSA-N
InChIInChI=1S/C17H14Cl2F2N2O3/c18-11-6-22-7-12(19)15(11)23-16(24)10-3-4-13(26-17(20)21)14(5-10)25-8-9-1-2-9/h3-7,9,17H,1-2,8H2,(H,22,23,24)
Canonical SMILESO=C(NC1=C(Cl)C=NC=C1Cl)C2=CC=C(OC(F)F)C(OCC3CC3)=C2
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分类

  • Inhibitors
  • Pharmaceuticals
  • Intermediates & Fine Chemicals,

产品应用

  • Roflumilast is a drug which acts as a selective, long-acting inhibitor of the enzyme PDE-4. It has anti-inflammatory effects and is under development as an orally administered drug for the treatment of inflammatory conditions of the lungs such as asthma, and chronic obstructive pulmonary disease (COPD). In June 2010, Daxas was approved in the EU for severe COPD associated with chronic bronchitis.[9] In March 2011, Daliresp gained FDA approval in the US for reducing COPD exacerbations.

相关文献及参考

  • [2]. Rabe KF. Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. Br J Pharmacol. 2011 May;163(1):53-67.
  • [3]. Hatzelmann A, et al. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J Pharmacol Exp Ther. 2001 Apr;297(1):267-79.
  • [4]. Richmond BW, et al. Airway bacteria drive a progressive COPD-like phenotype in mice with polymeric immunoglobulin receptor deficiency. Nat Commun. 2016 Apr 5;7:11240.
  • [5]. Ding H, et al. Treatment of obesity-associated overactive bladder by the phosphodiesterase type-4 inhibitor roflumilast. Int Urol Nephrol. 2017 Jul 29.
  • Hatzelmann, A., et al.: J. Pharmacol. Exp. Ther., 297, 267 (2001),
  • Schmidt, B.M.W., et al.: J. Allergy Clin. Immunol., 108, 530 (2001),
  • Timmer, W., et al.: J. Clin. Pharmacol., 42, 297 (2002),
  • [1]. Hatzelmann A, et al. The preclinical pharmacology of roflumilast--a

安全信息

Hazard statements
  • H315 Causes skin irritation 会刺激皮肤
RTECSCV3325600
GHS Symbol
Signal word
Precautionary statements
  • P264 Wash hands thoroughly after handling. 处理后要彻底洗净双手。
  • P280 Wear protective gloves/protective clothing/eye protection/face protection. 戴防护手套/防护服/眼睛的保护物/面部保护物。
  • P302+P352+P332+P313+P362+P364
  • P305+P351+P338+P337+P313
Storage condition -20°C Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

系列性分类

  1. Medical Research Areas
  2. Metabolism
  3. PDE
  1. Medical Research Areas
  2. Metabolism
  3. Phosphodiesterase (PDE)  (磷酸二酯酶)

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