83430-98-2

Upstream product

• 83430-93-7 2,4-Di-tert-butyl-6-(3-methyl-pyrazol-1-yl)-phenol 
• 1453-58-3 3-Methylpyrazole 
• 533-58-4 2-Iodophenol 

Relevant academic research and scientific papers

NITROGENOUS HETEROCYCLIC AROMATIC COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION THEREOF, AND APPLICATION THEREOF

Provided are a nitrogenous heterocyclic aromatic compound, a preparation method therefor, a pharmaceutical composition thereof, and an application thereof. The nitrogenous heterocyclic aromatic compound can be used for treating and/or preventing various diseases mediated by ALK5.

ANTI-TRICHOPHYTIC ADHESIVE PATCH

According to the present invention, a patch for nail and/or skin having antifungal activity against dermatophytes, and having higher nail permeability can be provided. The patch for nail and/or skin for prevention or treatment of dermatophytosis comprises in a pressure sensitive adhesive layer a compound represented by the formula: wherein R1 represents a hydrogen atom, C1-6 alkyl, or trifluoromethyl; R2 represents a hydrogen atom, C1-6 alkyl, halogen, -COO(C1-6 alkyl), or (CH2)1-3COOR (R represents a hydrogen atom or C1-6 alkyl); R3 represents a hydrogen atom, C1-6 alkyl, amino, trifluoromethyl, or OR (R represents a hydrogen atom or C1-6 alkyl); R4 represents a hydroxyl group; R5 represents a hydrogen atom, C1-6 alkyl, a hydroxyl group, or halogen; R6 represents a hydrogen atom, C1-6 alkyl, trifluoromethyl, halogen, amino, -NRaRb, nitro, hydroxy-C1-6 alkyl, -CONRaRb, -COO(C1-6 alkyl), -COOH, -(CH2)1-3COOR, or ORa (R represents a hydrogen atom or C1-6 alkyl, Ra and Rb may be the same or different from each other, and each represent a hydrogen atom, C1-6 alkyl, or C1-6 acyl); R7 represents a hydrogen atom, C1-6 alkyl, -OR (R represents a hydrogen atom or C1-6 alkyl), or halogen; and R8 represents a hydrogen atom, C1-6 alkyl, a hydroxyl group, amino, or nitro, or a salt thereof.

ANTITRICHOPHYTOSIS SOLUTION FOR EXTERNAL USE

According to the present invention, a topical liquid agent having antifungal activity against dermatophytes, and further high nail permeability can be provided. The topical liquid agent for nail and/or skin for prevention or treatment of dermatophytosis comprises a film-forming agent and a compound represented by the formula: wherein R1 represents a hydrogen atom, C1-6 alkyl, or trifluoromethyl, R2 represents a hydrogen atom, C1-6 alkyl, halogen, -COO(C1-6 alkyl), or (CH2)1-3COOR where R represents a hydrogen atom or C1-6 alkyl, R3 represents a hydrogen atom, C1-6 alkyl, amino, trifluoromethyl, or OR where R represents a hydrogen atom or C1-6 alkyl, R4 represents a hydroxyl group, R5 represents a hydrogen atom, C1-6 alkyl, a hydroxyl group, or halogen, R6 represents a hydrogen atom, C1-6 alkyl, trifluoromethyl, halogen, amino, -NRaRb, nitro, hydroxy-C1-6 alkyl, -CONRaRb, -COO(C1-6 alkyl), -COOH, -(CH2)1-3COOR, or ORa where R represents a hydrogen atom or C1-6 alkyl, Ra and Rb may be the same or different from each other, and each represent a hydrogen atom, C1-6 alkyl, or C1-6 acyl, R7 represents a hydrogen atom, C1-6 alkyl, -OR where R represents a hydrogen atom or C1-6 alkyl, or halogen, R8 represents a hydrogen atom, C1-6 alkyl, a hydroxyl group, amino, or nitro, or a salt thereof.

PATCH FOR ANTI-DERMATOPHYTOSIS

A patch for nails or skin for prevention or treatment of dermatophytosis, containing a layer including a pressure sensitive adhesive layer and a compound represented by the formula: wherein R1 represents hydrogen, C1-16 alkyl, or trifluoromethyl; R2 represents hydrogen, C1-6 alkyl, halogen, —COO(C1-6 alkyl), or (CH2)1-3COOR; R3 represents hydrogen, C1-6 alkyl, amino, trifluoromethyl, or OR; R4 represents hydroxyl; R5 represents hydrogen, C1-6 alkyl, hydroxyl, or halogen; R6 represents hydrogen, C1-6 alkyl, trifluoromethyl, halogen, amino, —NRaRb, nitro, hydroxy-C1-6 alkyl, —CONRaRb, —COO(C1-6 alkyl), —COOH, —(CH2)1-3COOR, or ORa (Ra and Rb each represents hydrogen, C1-6 alkyl, or C1-6 acyl); R7 represents hydrogen, C1-6 alkyl, —OR, or halogen; R8 represents hydrogen, C1-6 alkyl, hydroxyl, amino, or nitro; and R represents hydrogen or C1-6 alkyl; or a salt thereof.

TOPICAL LIQUID AGENT FOR THE TREATMENT OF DERMATOPHYTOSIS

A topical liquid agent for a nail and/or skin for prevention or treatment of dermatophytosis comprises a film-forming agent and a compound represented by the formula: wherein R1 represents hydrogen, C1-6 alkyl, or trifluoromethyl, R2 represents hydrogen, C1-6 alkyl, halogen, —COO(C1-6 alkyl), or (CH2)1-3COOR where R represents hydrogen or C1-6 alkyl, R3 represents hydrogen, C1-6 alkyl, amino, trifluoromethyl, or OR where R represents hydrogen or C1-6 alkyl, R4 represents hydroxyl, R5 represents hydrogen, C1-6 alkyl, hydroxyl, or halogen, R6 represents hydrogen, C1-6 alkyl, trifluoromethyl, halogen, amino, —NRaRb, nitro, hydroxy-C1-6 alkyl, —CONRaRb, —COO(C1-6 alkyl), —COOH, —(CH2)1-3COOR, or ORa where R represents hydrogen or C1-6 alkyl, Ra and Rb each represent hydrogen, C1-6 alkyl, or C1-6 acyl, R7 represents hydrogen, C1-6 alkyl, —OR where R represents hydrogen or C1-6 alkyl, or halogen, R8 represents hydrogen, C1-6 alkyl, hydroxyl, amino, or nitro, or a salt thereof.

TOPICAL ANTIFUNGAL AGENT

An anti-fungal agent for tinea comprising as active ingredient a compound having the skeleton of 2-(1H-pyrazol-1-yl)phenol represented by the following formula (I) or (II) or a salt thereof is provided

CYCLODIENONES. 9. REACTION 4-HALO-2,4,6-TRI-TERT-BUTYL-2,5-CYCLOHEXADIEN-1-ONES WITH PYRAZOLES AND PREPARATION OF 1-(2-HYDROXYPHENYL)- AND 1-(4-HYDROXYPHENYL)PYRAZOLES

Reaction of 4-halo-2,4,6-tri-tert-butyl-2,5-cyclohexadien-1-one (1) with pyrazoles (8) afforded 4-(pyrazol-1-yl)-2,4,6-tri-tert-butyl-2,5-cyclohexadien-1-ones (9), 1-(4-hydroxy-3,5-di-tert-butylphenyl)- and 1-(2-hydroxy-3,5-di-tert-butylphenyl)pyrazoles (10 and 11) together with by-products.De-tert-butylation of 9, 10 and 11 was carried out in boiling 85percent H3PO4 to give the corresponding 1-(4-hydroxyphenyl)- and 1-(2-hydroxyphenyl)pyrazoles (17 and 18) in good yields, respectively.