Patent classifications
C07C2602/50
Process for the preparation of spiro[2.5]octane-5,7-dione and spiro[3.5]nonane-6,8-dione
This invention relates to methods for the synthesis of spiro[2.5]octane-5,7-dione and spiro[3.5]nonane-6,8-dione which are useful as intermediates in the manufacture of pharmaceutically active ingredients.
Unnatural Analogues of Calcitriol and Uses Thereof
Disclosed is a compound of Formula (I)
##STR00001##
in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, and a are defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are a pharmaceutical composition comprising a compound or salt thereof of Formula (I) and a method of treating a disease which benefits from the modulation of the vitamin D receptor, such as a bone disorder, cardiovascular disease, a cardiovascular complication associated with renal disease, endothelial dysfunction, hyperparathyroidism, hypocalcemia, an immune disorder, left ventricular hypertrophy, a proliferative disease, proteinuria, renal disease, and thrombosis.
High density turbine and diesel fuels from tricyclic sesquiterpenes
A method for converting cedarwood oil into high density fuels including, hydrogenating cedarwood oil in the presence of at least one hydrogenation catalyst to generate hydrogenated cedarwood oil, removing the hydrogenation catalyst from the hydrogenated cedarwood oil, purifying the hydrogenated cedarwood oil to produce a first high density fuel, isomerizing the first high density fuel in the presence of at least one acid catalyst to generate a hydrocarbon mixture including adamantanes, and distilling the adamantane mixture to produce a second alkyl-adamantane high density fuel.
Tetracycline compounds
The present invention is directed to a compound represented by Structural Formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
Synthesis and Evaluation of Novel (4-Hydroxyphenyl) Substituted Carbocycles as Potent and Selective Estrogen Receptor Beta Agonists
Disclosed are 4-hydroxylphenyl substituted carbocycles and there use as selective agonists of the estrogen receptor beta isoform (ER). The disclosed compounds may be formulated as pharmaceutical compositions and administered to treat diseases associated with ER activity, such as proliferative diseases and disorders and/or psychiatric diseases or disorders.
Cyclobutane containing carboxylic acid GPR120 modulators
The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments. ##STR00001##
Novel process for the preparation of spiro[2.5]octane-5,7-dione and spiro[3.5]nonane-6,8-dione
This invention relates to methods for the synthesis of spiro[2.5]octane-5,7-dione and spiro[3.5]nonane-6,8-dione which are useful as intermediates in the manufacture of pharmaceutically active ingredients.
CYCLOPROPANATION OF SUBSTITUTED ALKENES
Disclosed is a cyclopropanation process comprising the step of reacting an alkene compound having at least one carbon-carbon double bond with at least one dihaloalkane. The reaction is carried out in the presence of (i) particulate metal Zn, (ii) catalytically effective amount of particulate metal Cu or a salt thereof, (iii) at least one haloalkylsilane, and (iv) at least one solvent.
Alpha-7 nicotinic acetylcholine receptor modulators and uses thereof
Disclosed are compounds of Formula (IVA), or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof: Formula (IVA), wherein R.sup.Ia, R.sup.Ib, R.sup.Ic, R.sup.Id, R.sup.Ie, are defined herein above, which compounds are believed suitable for use in positive modulation of the alpha 7 nicotinic acetylcholine receptor (7 nAChR) receptors, for example, those found in the cerebral cortex and the hippocampus. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Alzheimer's disease (AD), schizophrenia, and Parkinson's disease (PD), or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease. ##STR00001##