摘要:
The present invention provides, inter alia, triphenylethylene derivatives, such as, 3-null4-null6-(3-Methoxy-phenyl)-8,9-dihydro-7H-benzocyclohepten-5-ylnull-phenylnull-acrylic acid, as selective estrogen receptor modulators. Also provided are methods for the treatment and/or prevention of estrogen stimulated diseases in mammals including breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as pharmaceutical compositions of the compounds of the present invention.
摘要:
A process to prepare an ester which reacts an acid and a base in a solvent which contains 1-methyl-2-pyrrolidinone. The use of 1-methyl-2-pyrrolidinone can replace pyridine solvent. The pyridine solvent is a challenge for disposal and safe handling.
摘要:
Amidomethyl esters, carbonylmercaptomethyl esters, keto-containing esters, amidomethyl thioesters, amidomethyl amides, and methylene dithioesters are disclosed. The novel compounds have two carbonyl groups connected by a linking moiety having an oxygen, sulfur or nitrogen attached to a methylene group, to which is further attached a sulfur, nitrogen or CH2 group. Methods of treating illnesses and conditions, such as cancer, hemological disorders, inherited metabolic disorders and others, using these compounds are also disclosed.
摘要:
3,3null-Substituted chiral biaryl phosphine and phosphinite ligands and metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The metal complexes are useful as catalysts in asymmetric reactions, such as, hydrogenation, hydride transfer, allylic alkylation, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, olefin metathesis, hydrocarboxylation, isomerization, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition, epoxidation, kinetic resolution and nullmnullnnull cycloaddition. The metal complexes are particularly effective in Ru-catalyzed asymmetric hydrogenation of beta-ketoesters to beta-hydroxyesters and Ru-catalyzed asymmetric hydrogenation of enamides to beta amino acids.
摘要:
The invention relates to novel biaromatic compounds having general formula I and their use in pharmaceutical compositions for use in human and veterinary medicine, in particular for treating dermatological, rheumatic, respiratory, cardiovascular, and ophthalmological disorders, and for use in cosmetic compositions.
摘要:
6-tert-Butyl-1,1-dimethylindane derivatives which are unsaturated in the 4-position of formula: X represents: (i) either a radical of formula: and Y represents a radical of formula: (ii) or a radical of formula: and Y represents either a radical of formula (b) or a radical of formula: Z being —O—, —S— or R1 represents —CH3, —(CH2)p—OR4, —(CH2)p—COR5 or —S(O)t—R6, p being 0, 1, 2 or 3, t being 0, 1 or 2, R2 represents H or lower alkyl, R3 represents H, lower alkyl or —COR7, R4 represents H, lower alkyl, —COR7, aryl, aralkyl, mono- or polyhydroxyalkyl, or a polyether radical, R5 represents H, lower alkyl, —OR8 or —N(r′)(r″), R6 represents H or lower alkyl, R7 represents lower alkyl, R8 represents H, alkyl, alkenyl, alkynyl, aryl, aralkyl, mono- or polyhydroxyalkyl, a sugar residue or an amino acid residue, r′ and r″ represent H, lower alkyl, —COR7, aryl, a sugar residue or an amino acid residue or r′ and r″ form a heterocycle, and the salts of the compounds of formula (I). Use in the topical and systemic treatment of dermatological conditions, as well as in cosmetics.
摘要:
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.
摘要:
Novel trienoic retinoid compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use.
摘要:
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.
摘要:
Compounds of general formula (I) ##STR1## characterised in that R.sup.1 and R.sup.2 are independently selected from the group consisting of COOR, CN, aryl, substituted aryl, COOH, halogen, C(O)NHR.sup.4, C(O)NR.sup.5 R.sup.6 ; X and Y are independently selected from the group consisting of H, COOH, COOR, CN, R.sup.3 CO--, C(O)NHR.sup.4, C(O)NR.sup.5 R.sup.6, P(O)(OR.sup.7).sub.2 and SO.sub.2 R.sup.8 ; with the proviso that X and Y are not both H; or X and Y together with the carbon atom to which they are attached form a carbocyclic or heterocyclic ring system which can contain oxygen, sulfur or nitrogen atoms; and R, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are various groups; and polymers and copolymers derived from such compounds.