The ester compound of the present invention is represented by the following formula (1), wherein R.sup.1 to R.sup.24 are each independently a hydrogen atom, a halogen atom, a hydrocarbon group, or a hetero atom-containing hydrocarbon group; R.sup.1 to R.sup.10, R.sup.23, and R.sup.24 may be bonded to one another to form a ring or may form a multiple bond at which adjacent substituents are directly bonded; R.sup.11 to R.sup.24 may be bonded to one another to form a ring, or adjacent substituents may be bonded to one another to form a multiple bond; at least one set in R.sup.1 to R.sup.24 is bonded to one another to form a ring structure; n2 to n5 each independently represent an integer of 0 to 2; n1 and n6 each independently represent an integer of 0 or 1; and L.sup.1 and L.sup.2 are each independently a hydrocarbon group or a hetero atom-containing hydrocarbon group.

##STR00001##

The present invention relates to compounds of formula (I) having insecticidal activity to processes and interediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests ##STR00001## claim 1: or salts thereof.

The present invention relates to compounds of formula (I) having insecticidal activity to processes and interediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests ##STR00001## claim 1: or salts thereof.

A method for preparing 2-hydroxy-5-[2-(4-(trifluoromethylphenyl)ethylamino)]benzoic acid is proposed. The method may include protection, condensation, and hydrolysis. By means of the screening of a hydroxyl protecting reagent for a starting material, for example, 2-(4-trifluoromethyl)phenethylalcohol and the optimization of other process parameters, the contents of meta-isomer impurities and disubstituted impurities in a target product are effectively controlled. Accordingly, the quality of the product is significantly improved, the reaction yield is also greatly improved, and the improved product quality can satisfy related requirements of preparation research.

A method for preparing 2-hydroxy-5-[2-(4-(trifluoromethylphenyl)ethylamino)]benzoic acid is proposed. The method may include protection, condensation, and hydrolysis. By means of the screening of a hydroxyl protecting reagent for a starting material, for example, 2-(4-trifluoromethyl)phenethylalcohol and the optimization of other process parameters, the contents of meta-isomer impurities and disubstituted impurities in a target product are effectively controlled. Accordingly, the quality of the product is significantly improved, the reaction yield is also greatly improved, and the improved product quality can satisfy related requirements of preparation research.

The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII, formula VIII, formula IX, formula X, formula XI, formula XII, formula XIII, formula XIV and formula XV and the methods for the treatment of chronic pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of chronic pain.

2-hydroxy-5-[2-(4-(trifluoromethylphenyl)ethylamino)]benzoic acid crystal forms and a preparation method therefor are proposed. Crystal form I is a monoclinic crystal system, which has a Pc space group and can be obtained by slow cooling, evaporating the solvent at a constant temperature, evaporating the solvent at an increased temperature, or adding an anti-solvent. Crystal form II is a triclinic crystal system, which has a P1 space group and can be obtained by rapid cooling or freeze-drying. According to the method, the process is simple, costs are low, and the yield exceeds 90%; and the crystal forms of the crystal forms I and II have high purity, the crystal shapes thereof are intact, and have excellent fluidity, facilitating preparation, particularly the preparation of a pharmaceutical preparation for preventing and/or treating degenerative diseases of the central nervous system. Furthermore, the two crystal forms have a better apparent solubility than that of raw materials.

2-hydroxy-5-[2-(4-(trifluoromethylphenyl)ethylamino)]benzoic acid crystal forms and a preparation method therefor are proposed. Crystal form I is a monoclinic crystal system, which has a Pc space group and can be obtained by slow cooling, evaporating the solvent at a constant temperature, evaporating the solvent at an increased temperature, or adding an anti-solvent. Crystal form II is a triclinic crystal system, which has a P1 space group and can be obtained by rapid cooling or freeze-drying. According to the method, the process is simple, costs are low, and the yield exceeds 90%; and the crystal forms of the crystal forms I and II have high purity, the crystal shapes thereof are intact, and have excellent fluidity, facilitating preparation, particularly the preparation of a pharmaceutical preparation for preventing and/or treating degenerative diseases of the central nervous system. Furthermore, the two crystal forms have a better apparent solubility than that of raw materials.

Disclosed are an aromatic acetylene or aromatic ethylene compound, an intermediate, a preparation method, a pharmaceutical composition and a use thereof. The aromatic acetylene or aromatic ethylene compound has a significant inhibitory effect on PD-1 and PD-L1, and can effectively relieve or treat cancers and other related diseases.

##STR00001##

Disclosed are an aromatic acetylene or aromatic ethylene compound, an intermediate, a preparation method, a pharmaceutical composition and a use thereof. The aromatic acetylene or aromatic ethylene compound has a significant inhibitory effect on PD-1 and PD-L1, and can effectively relieve or treat cancers and other related diseases.

##STR00001##