Patent classifications
C07D231/44
POLYMORPHS AND AMORPHOUS FORMS OF 5-AMINO-1-[2,6-DICHLORO-4-(TRIFLUOROMETHYL)PHENYL]-4-[(TRIFLUOROMETHYL)SULFINYL]-1H-PYRAZOLE-3-CARBONITRILE
The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.
FIPRONIL PRODUCTION PROCESS
An improved oxidation process for preparing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylsulphinyl-pyrazole, of formula (I) is described. The process includes admixing 5-amino-3-cyano-1-(2, 6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylthiopyrazole of formula (II) with dichloroacetic acid and hydrogen peroxide in the presence of a strong acid.
FIPRONIL PRODUCTION PROCESS
An improved oxidation process for preparing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylsulphinyl-pyrazole, of formula (I) is described. The process includes admixing 5-amino-3-cyano-1-(2, 6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylthiopyrazole of formula (II) with dichloroacetic acid and hydrogen peroxide in the presence of a strong acid.
COMPLEXES
A palladium(II) complex of formula (1) or a palladium(II) complex of formula (3).
##STR00001##
Also, processes for the preparation of the complexes, and their use in carbon-carbon and carbon-heteroatom coupling reactions.
COMPLEXES
A palladium(II) complex of formula (1) or a palladium(II) complex of formula (3).
##STR00001##
Also, processes for the preparation of the complexes, and their use in carbon-carbon and carbon-heteroatom coupling reactions.
SREBP-1 INHIBITOR AND PHARMACEUTICAL COMPOSITION FOR TREATING HYPERTRIGLYCERIDEMIA
There is provided an SREBP-1 inhibitor that has inhibitory activity against SREBP-1 and no inhibitory activity against SREBP-2, the SREBP-1 inhibitor containing, as an active ingredient, any one or more compounds among compounds represented by Formulae (1) to (23). There is also provided a pharmaceutical composition for treating hypertriglyceridemia, which contains the SREBP-1 inhibitor and a pharmaceutically acceptable carrier.
MASP-2 INHIBITORS AND METHODS OF USE
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.
MASP-2 INHIBITORS AND METHODS OF USE
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.
N-bicyclic aryl,N'-pyrazolyl urea, thiourea, guanidine cyanoguanidine compounds as TrkA kinase inhibitors
Compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome. ##STR00001##
MASP-2 INHIBITORS AND METHODS OF USE
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.