13054-02-9Relevant articles and documents
A new and efficient synthesis of 6-[(5 S,9 R)-9-(4-Cyanophenyl)-3-(3,5- dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl]nicotinic acid, a potent LFA-1/ICAM inhibitor
Zhang, Huiping,Watterson, Scott H.,Xiao, Zili,Dhar, T. G. Murali,Balasubramanian, Balu,Barrish, Joel C.,Chen, Bang-Chi
body text, p. 936 - 938 (2011/03/20)
An efficient synthesis of 6-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5- dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl]nicotinic acid 1 is described. This new process involves an in situ protection of 6-chloronicotinic acid as trimethylsilyl est
N-ALKYL PYRROLES AS HMG-COA REDUCTASE INHIBITORS
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Page/Page column 135, (2010/02/12)
HMGCo-A reductase inhibitor compounds useful as hypocholesterolemic and hypolipidemic compounds are provided. Also provided are pharmaceutical compositions of the compounds. Methods of making and methods of using the compounds are also provided. Formula (I).
Disubstituted acetylenes bearing heterobicyclic groups and heteroaromatic or phenyl groups having retinoid like activity
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Page column 17-18, (2010/01/30)
Compounds of the formula where R1and R2, independently are alkyl groups having 2 to 8 carbons; R3is hydrogen or lower alkyl; X is S, O or N—R4where R4is hydrogen or lower alkyl; Y is phenyl or pyridyl
Method for inhibiting gene expression promoted by AP1 protein with RAR beta selective retinoids and method for treatment of diseases and conditions with such retinoids
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, (2008/06/13)
Retinoid compounds which repress expression of the gene promoted by AP1 protein but which do not significantly activate expression of the genes having RA-responsive elements in their promoter region through RAR alpha and RAR GAMMA receptor subtypes, are u
Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
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, (2008/06/13)
Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.
SYNTHESIS AND USE OF RETINOID COMPOUNDS HAVING NEGATIVE HORMONE AND/OR ANTAGONIST ACTIVITIES
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, (2008/06/13)
2,2-Dialkyl-4-aryl-substituted benzopyran and benzothiopyran derivatives of the formula STR1 where the symbols have the meaning described in the specification, have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists.
[(3""-thioxacyclohex-1""-enyl)]-but-3'-ene-1'-ynyl]aryl and [(3""-thioxacyclohex-1""-enyl)]-but-3'-ene-1'-ynyl]heteroaryl carboxylic acids and esters having retinoid-like biological activity
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, (2008/06/13)
Compounds of the formula STR1 where R 1, R 2, R 3, and R 4 independently are H or lower alkyl of 1 to 10 carbons; R 5 is lower alkyl of 1 to 10 carbons, fluoro, chloro, bromo, iodo, nitro, or fluoroalkyl having 1 to 10 carbons; m is an integer having the
Sulfides, sulfoxides and sulfones disubstituted with a tetrahydronaphthalenyl, chromanyl, thiochromanyl or tetrahydroquinolinyl and substituted phenyl or heteroaryl group, having retinoid-like biological activity
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, (2008/06/13)
STR1 wherein the symbols have the meaning described in the specification, are selective agonists of RXR retinoid receptors.
Acetylenes disubstituted with a 5-amino or substituted 5-amino substituted tetrahydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity
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, (2008/06/13)
Compounds of the formula STR1 having retinoid like biological activity.
Acetylenes disubstituted with 2-tetrahydropyranoxyaryl and aryl or heteroaryl groups having retinoid-like biological activity
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, (2008/06/13)
Compounds of the formula STR1 wherein R1 -R5, X, Y, A, B are as defined in the specification have retinoid-like biological activity.