Patent classifications
C07D231/44
PROCESS FOR SYNTHESIS OF FIPRONIL
A process for the synthesis of fipronil, which is a broad spectrum insecticide of the following chemical structure, is provided.
##STR00001##
The process provides fipronil with a yield in the range of 75% to 90% and purity in the range of 95% to 97%. By the process, the observed amount of sulfone impurity i.e., 5-amino-1-(2,6-dichloro-4-trifluoromethylphenyl)-3-cyano-4-trifluoro methylsulfonyl pyrazole in fipronil is in the range of 0% to 0.5%.
PYRAZOLONE FORMYL PEPTIDE 2 RECEPTOR AGONISTS
The disclosure relates to compounds of formula I, which are formyl peptide 2 (FPR2) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.
##STR00001##
Inhibitors of receptor interacting protein kinase I for the treatment of disease
Disclosed herein are compounds which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer.
Inhibitors of receptor interacting protein kinase I for the treatment of disease
Disclosed herein are compounds which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer.
Pyrazole compound
The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT.sub.2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT.sub.2C inverse agonistic action comprising Compound (1): ##STR00001## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen or C.sub.1-6 alkyl etc.; R.sup.5 is C.sub.4-7 alkyl or —(CR.sup.8R.sup.9).sub.r-E; R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are independently hydrogen, fluorine or C.sub.1-6 alkyl; A is C.sub.6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C.sub.3-8 cycloalkyl or C.sub.6-10 aryl etc.; L is oxygen, sulfur or —NR.sup.10—; n is 1, 2 or 3; R.sup.10 is hydrogen or C.sub.1-6 alkyl etc.; and X is hydrogen or halogen etc.
Pyrazole compound
The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT.sub.2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT.sub.2C inverse agonistic action comprising Compound (1): ##STR00001## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen or C.sub.1-6 alkyl etc.; R.sup.5 is C.sub.4-7 alkyl or —(CR.sup.8R.sup.9).sub.r-E; R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are independently hydrogen, fluorine or C.sub.1-6 alkyl; A is C.sub.6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C.sub.3-8 cycloalkyl or C.sub.6-10 aryl etc.; L is oxygen, sulfur or —NR.sup.10—; n is 1, 2 or 3; R.sup.10 is hydrogen or C.sub.1-6 alkyl etc.; and X is hydrogen or halogen etc.
PYRAZOLE DERIVATIVES USEFUL AS 5-LIPOXYGENASE ACTIVATING PROTEIN (FLAP) INHIBITORS
The present application relates to novel compounds of formula (I)
##STR00001##
to their utility in treating and/or preventing clinical conditions including cardiovascular diseases (CVD), to methods for their therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds.
PYRAZOLE DERIVATIVES USEFUL AS 5-LIPOXYGENASE ACTIVATING PROTEIN (FLAP) INHIBITORS
The present application relates to novel compounds of formula (I)
##STR00001##
to their utility in treating and/or preventing clinical conditions including cardiovascular diseases (CVD), to methods for their therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds.
SUBSTITUTED HALOALKYL SULFONANILIDE HERBICIDES
Disclosed are compounds of Formula 1, all stereoisomers, N-oxides, and salts thereof,
##STR00001##
wherein G is CONR.sup.5R.sup.6 or selected from
##STR00002## and R.sup.1 through R.sup.18, R.sup.f and G are as defined in the Disclosure.
Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
SUBSTITUTED HALOALKYL SULFONANILIDE HERBICIDES
Disclosed are compounds of Formula 1, all stereoisomers, N-oxides, and salts thereof,
##STR00001##
wherein G is CONR.sup.5R.sup.6 or selected from
##STR00002## and R.sup.1 through R.sup.18, R.sup.f and G are as defined in the Disclosure.
Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.