专利号:US-9422326-B2 优先权日:2012-09-04 标 题:Process for preparing 11-methylene-18-methyl-estr-4-en-3, 17-dione, useful as intermediate compound for the synthesis of molecules having pharmacological activity 发明人:LENNA ROBERTO; MARIANI EDOARDO; VANOSSI ANDREA 权利人:IND CHIMICA SRL 摘要:There is described a process for the industrial synthesis of 11-methylene-18-methyl-estr-4-en-3,17-dione, a compound having the structure formula (I) depicted below: (Formula I) (I) useful as intermediate compound in the synthesis of the progestin compounds Desogestrel and Etonogestrel.
专利号:US-4913852-A 优先权日:1986-06-24 标题 :Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with pregnane derivatives 发明人:MILIONI CATHERINE; EFTHYIMIOPOULOS CONSTANTIN; KOCH BERNARD; JUNG LOUIS; JUNG JEAN 权利人:MILIONI CATHERINE; EFTHYIMIOPOULOS CONSTANTIN; KOCH BERNARD; JUNG LOUIS; JUNG JEAN 摘要:Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with derivatives of Δ-4-pregnene-3,20-dione or with derivatives of Δ-1,4-pregnadiene-3,20-dione of the general formulas (I), (II) and (III), having glucocorticoidal and anti-inflammatory properties have been prepared and tested. Pharmaceutical compositions, medicaments containing them as well as their applications are claimed, particularly in the cutaneous and ophthalmic fields. ##STR1##
专利号:US-2025235415-A1 优先权日:2022-02-23 标 题:Modulation of human breast milk composition 发明人:ROSS MICHAEL G; DESAI MINA 权利人:LUNDQUIST INST FOR BIOMEDICAL INNOVATION AT HARBOR UCLA MEDICAL CENTER 摘要:Compositions and methods for improving a child, such as an infant's health, are provided. The methods entail improving the quality of breast milk in a female human individual that provides breast milk, or expects to provide breast milk, to the child, by administering to the individual an agent that increases the individual's sensitivity to insulin, and/or an agent that reduces the substrate uptake, synthesis or secretion of long chain fatty acids, reduces the substrate uptake, synthesis or secretion of short chain fatty acids, increases the amino acid uptake, protein synthesis or protein secretion of proteins, or reduces the uptake or synthesis of lactose.
专利号:EP-1474119-B1 优先权日:2002-02-15 标题:Use of extracts containing phytoestrogen selectively modulating estrogen-receptor-beta 发明人:WUTTKE WOLFGANG; JARRY HUBERTUS; CHRISTOFFEL VOLKER; SPENGLER BARBARA; POPP MICHAEL 权利人:BIONORICA AG 摘要:The present invention relates to the use of phytoestrogen-containing extracts that selectively modulate estrogen receptor beta (ER-beta) without producing any uterotropic effect, for the treatment of clinical situations and pathophysiological conditions that are selected from the group consisting of: Obesity and thereby to possibly influence the metabolic syndrome, particularly hypertension, asterosclerosis, cardiac infarct, hyperandrogenemia; Menopausal continence disorders; Menopausal heat surges associated with hyperstimulation of the hypothalamic gonadotropin releasing hormone pulse generator; steroid hormonal synthesis disorder, particularly that of progesterone synthesis of the human corpus luteum, resulting in luteal insuffeciency; Alzheimer's disease associated with elevated expression of estrogen receptor beta in hippocampal neurons.
专利号:WO-2006052263-A1 优先权日:2004-11-10 标题:Synthesis and separation of optically active isomers and cyclopropyl derivatives of spironolactone and their biological action 发明人:RANADE VASANT V; SOMBERG JOHN CHARIN 权利人:RANADE VASANT V 摘要:Methods for separation and synthesis of the optically active 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone are provided. Preferred stereoisomerically purified 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone have fewer effects mediated by gonadal steroid receptors relative to effects mediated by minteralocorticoid progesterone receptors, compared to the stereoisomerically unpurified form of the compound. These optically active compounds can be useful for obtaining reduction in moderate essential hypertension and in the treatment of congestive heart failure in humans with minimized undesirable side effects such as gynecomastia, tender breast enlargement and menstrual irregularities in women, and loss of libido in
专利号:WO-2013001322-A1 优先权日:2011-06-30 标 题:PROCESS FOR THE SYNTHESIS OF (5α,17β)-N-[(2,5-BIS(TRIFLUOROMETHYL)-PHENYL]-3-OXO-4-AZA-5-ANDROST-1-ENE-17-CARBOXAMIDE 发明人:SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; MAHO SANDOR; BALOGH LASZLO; VINCZE PETER; HORVATH JANOS; KOVACS ANDRAS; BENI ZOLTAN; VARGA FRIGYES 权利人:RICHTER GEDEON NYRT; SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; MAHO SANDOR; BALOGH LASZLO; VINCZE PETER; HORVATH JANOS; KOVACS ANDRAS; BENI ZOLTAN; VARGA FRIGYES 摘要:The synthesis consists of reaction steps as follows: oxidizing the α,β-unsaturated ketone system of ring 'A' of pregn-4-ene-3,20-dion- of formula (II) with sodium metaperiodate in tert-butanol in the presence of potassium permanganate and alkali metal carbonate, reacting the obtained 3,5-seco acid with an ester of chloroformic acid in the presence of tertier organic base below 0°C, reacting the obtained new compound after isolation or without isolation with ammonia or ammonium acetate, cyclization of the resulting carboxamides with an acid, cathalytic hydrogenating the obtained ene lactame, and oxidizing the side chain at position 17 of the obtained pregnane compound with an alkali metal hypobromide in aqueous dioxane below 10°C. Thereafter on one hand the obtained (5α,17β)-3-oxo-4-aza-5-androstane-17-carboxylic acid is reacted with chloroformic acid ester, the obtained new compound is reacted with 2,5-bis(trifluoromethyl)-aniline in the presence of a Lewis acid, the obtained amide is reacted with trimethyl chlorosilane in inert atmosphere in the presence of Î ,Î ,Î ',Î '-tetramethyl-ethylendiamine, then en excess iodine is added to the reaction mixture and the product of the iodination reaction is crystallized from acetonitrile, then the obtained 2-iodo-3-oxo-4-aza-17β-carboxamide is reacted with potassium tert-butylate to furnish final product. On the other hand, (5α,17β)-3-oxo-4-aza-5-androstane-17-carboxylic acid is transformed into methylester by known method, this latter is transformed into methyl (2α,5α,17β)-2-iodo-3-oxo-4-aza-5-androstane-17-carboxylate according to known method, the obtained compound is reacted with potassium-tert-butylate, the obtained (5α,17β)-3-oxo-4-aza-5-androst-1-ene-17-carboxylic acid is reacted with an ester of chloroformic acid, then the obtained new compound is coupled with 2,5-bis(trifluoromethyl)-aniline in the presence of a Lewis acidcatalyst to gain final product.
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