Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

Vanilloid receptor ligands and their use in treatments

The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

Histone demethylase inhibitors

A compound represented by the formula (1) wherein ring A is a ring optionally having 1 to 3 substituents; ring B is a 1,2-azole ring which may further have 1 to 3 substituents; Xa, Xb and Xc are the same or different and each is a bond, - O -, - S - and the like; Ya is a divalent aliphatic hydrocarbon residue having 1 to 20 carbon atoms; Yb and Yc are the same or different and each is a bond or a divalent aliphatic hydrocarbon residue having 1 to 20 carbon atoms; ring C is a monocyclic aromatic ring which may further have 1 to 3 substituents; and R represents -OR4 (R4 is hydrogen atom or optionally substituted hydrocarbon group) and the like, or a salt thereof or a prodrug thereof is useful as an agent for the prophylaxis or treatment of diabetes and the like.

1,2-azole derivatives with hypoglycemic and hypolipidemic activity

The invention concretely relates to a synthetic technology for pyraclostrobin. The synthetic technology comprises: firstly performing cyclization to obtain 1-(4-chlorophenyl)-pyrazol-3-one, oxidizing the pyrazol ring under the effect of an oxidant to generate 1-(4-chlorophenyl)-3-hydroxypyrazole, then using 2-nitrobenzyl bromide to performing etherification to generate 1-(4-chlorophenyl)-3-[2-(nitrophenyl)methoxy]-1H-pyrazole, then using a reducing agent to perform nitro reducing, so as to generate N-hydroxyl-2-[N'-(4-chlorophenyl)pyrazol-3'-yloxymethyl]aniline, then using ClCO2CH3 to perform N-acylation reaction to generate methyl N-hydroxyl-N-2-{[N'-(4-chlorophenyl)pyrazol-3'-yloxymethyl]phenyl}formate, and finally performing hydroxyl methylation under an alkaline condition to generate pyraclostrobin. The technology enables all operations in the pyraclostrobin preparation process to be relatively controllable, helps to improve the stability of the preparation process and improve the product yield, successfully employs low-cost reagents and substantially reduces production cost, and also the employed reagents are relatively small in toxicity, is relatively beneficial for environment protection, and has no corrosivity on plastic pipes, so that the production safety is improved.

Synthetic technology for pyraclostrobin

The invention aims to provide pyraclostrobin and a method for economically synthesizing the same High purity pyraclostrobin can be synthesized at low cost The method comprises the following steps of: adding N-hydroxy-N-2-[(N-parachlorobenzyl)-3-pyrazoloxymethyl]phenyl carbamate and an acid bonding agent into a polar solvent or non-polar solvent, uniformly mixing, adding dimethyl sulfate, and reacting at the temperature of between 20 and 30DEG C; and after the reaction is monitored to be finished through high performance liquid chromatography (HPLC), adding water to neutralize until the pH=7, removing the solvent, immersing in a recrystallization solvent, performing recrystallization, and removing a recrystallization solution to obtain the pyraclostrobin, wherein a molar ratio of the N-hydroxy-N-2-[(N-parachlorobenzyl)-3-pyrazoloxymethyl]phenyl carbamate to the acid bonding agent to the dimethyl sulfate is 1:(1-18):(1-18) By the invention, the energy consumption is low, the utilization rate of materials is high, the operation is simple, and the yield and purity of the product are high; and compared with the traditional method, the method is more energy-saving, environment-friendly and economic, and has great industrial application value

Pyraclostrobin and method for economically synthesizing same

The invention relates to a method for producing N-acylated (hetero)aromatic hydroxylamine derivatives of formula (I), wherein the substituents, the ring atom and the index have the meanings given in the Description, by hydrogenating a (hetero)aromatic nitro-compound of general formula (II) in the presence of a hydrogenation catalyst.

Method for producing (hetero)aromatic hydroxylamines

Process for preparing (hetero)aromatic hydroxylamine derivatives

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Method for producing (hetero)aromatic hydroxylamines

Process for preparing (hetero)aromatic hydroxylamine derivatives