- IMINO ETHER DERIVATIVE COMPOUNDS AND DRUGS CONTAINING THE COMPOUNDS AS THE ACTIVE INGREDIENT
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The compound represented by formula (I) (wherein R1 and R2 are cyclic group which may have a substituent(s) and so on.; W is a spacer of which main chain has an atom number of 1-6.; X is -O- and so on.; ringA is cyclic group which may have a substituent(s).; Y is a spacer of which main chain has an atom number of 1-6 and so on.; Z is acidic group.) a salt thereof, a solvent thereof or an N-oxide thereof or a prodrug thereof Since the compounds in the present invention have a regulatory activity for peroxisome proliferator activated receptor, the compounds in the present invention are useful as a preventive and/or therapeutic agent for diseases associating metabolic disorders (e.g., hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipidemia, atherosclerosis, hypertension, circulatory diseases, overeating, ischemic heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or a VLDL cholesterol-lowering agent and a drug for relief from risk factors of diabetes or metabolic syndrom.
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Page/Page column 28
(2010/02/14)
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- Triphenylalkene derivatives and their use as selective estrogen receptor modulators
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The invention provides novel selective estrogen receptor modulator compounds of the general formula: wherein R1 and R2, which are the same or different are a) H, halogen, OCH3, OH; or ?where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, —CH2C≡CH or —CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or c) —Y—(CH2)nCH2—O—R6 where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, —CH2CH2OH, or —CH2CH2Cl; or d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and R3 is H, halogen, OH or —OCH3; stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.
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- Multivariate analysis by the minimum spanning tree method of the structural determinants of diphenylethylenes and triphenylacrylonitriles implicated in estrogen receptor binding, protein kinase C activity, and MCF7 cell proliferation
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The response profiles of 36 para-substituted diphenylethylenes (DPEs) and triphenylacrylonitriles (TPEs) have been compared by multivariate analysis. The responses measured were (a) relative binding affinity (RBA) for the cytosol estrogen receptor (ER), (
- Dore,Gilbert,Bignon,De Paulet,Ojasoo,Pons,Raynaud,Miquel
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p. 573 - 583
(2007/10/02)
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