14213-07-1

Usage

Uses

Used in Pharmaceutical Industry:
Roflumilast is used as an anti-inflammatory agent for the treatment of chronic obstructive pulmonary disease (COPD). It is particularly effective in reducing lung inflammation, which aids in alleviating breathing difficulties associated with the condition. As a PDE-4 inhibitor, roflumilast helps to decrease the frequency of COPD exacerbations, improving the quality of life for patients.
Additionally, roflumilast is prescribed in the form of a once-daily tablet, which simplifies the treatment regimen for patients. However, it is important to note that common side effects of the medication include diarrhea, nausea, and headache. Roflumilast should not be used as a rescue medication for sudden breathing problems and is available by prescription only, requiring the guidance of a healthcare professional for proper use.

Upstream product

• 1195-45-5 para-fluorophenyl isocyanate 

Downstream Products

• 155431-57-5 1-<(1R,2S)-2-(2,4-difluorophenyl)-2,3-epoxy-1-methylpropyl>-4-(4-fluorophenyl)-5(1H,4H)-tetrazolone 

Relevant academic research and scientific papers

GPR139 RECEPTOR MODULATORS

Compounds are provided that modulate the GPR139 receptor, compositions containing the same, and to methods of their preparation and use for treatment of a malcondition wherein modulation of the GPR139 receptor is medically indicated or beneficial. Such compounds have the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein R1, R4, R5, R9, R10, Q6, Q7, and Q12 are as defined herein.

TETRAZOLONE SUBSTITUTED STEROIDS AND USE THEREOF

The present disclosure relates to compounds of formula (AI), (I), (AII), and (II), or a pharmaceutically acceptable salt, solvate, stereoisomer, or tautomer thereof, a pharmaceutical composition comprising a compound of formula (AI), (I), (AII), and (II), and use thereof, wherein R2, R3, R4, R5, R6, R7, R10, R11a, R11b, R12, R16, R19a, R19b, and R20 are described herein. Such compounds are envisioned useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, movement disorders, convulsive disorders, schizophrenin spectrum disorders, disorders of memory and/or cognition, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, or tinnitus etc.

Optically active antifungal azoles. VI. Synthesis and antifungal activity of N-[(1R,2R)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl) propyl]-N′-(4-substituted phenyl)-3(2H,4H)-1,2,4-triazolones and 5(1H,4H)-tetrazolones

A new series of optically active antifungal azoles, N-[(1R,2R)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl) propyl]-N′-(4-substituted phenyl)-3(2H,4H)-1,2,4-triazolones (1,2) and 5(1H,4H)-tetrazolones (3), were prepared from the triflate derivative of (1S)-1-[(2R)-2-(2,4-difluorophenyl)-2-oxiranyl]ethanol (13) by an SN2 displacement reaction with the union of an azolone (17-19) and subsequent ring-opening reaction with 1H-1,2,4-triazole. The optically active oxiranylethanol 13 was synthesized from methyl (R)-lactate in a stereocontrolled manner. The azolones 1-3 prepared showed potent antifungal activities in vitro and in vivo.