Abstract: Substituted phenylalkenoylguanidines, processes for their preparation, uses as medicaments or diagnostics, and medicaments containing them are described.The invention relates to substituted phenylalkenoylguanidines and their pharmaceutically tolerable salts and physiologically functional derivatives of the formula ##STR1## in which the radicals have the meanings indicated, and their physiologically tolerable salts and processes for their preparation. The compounds are suitable as medicaments for the prophylaxis or treatment of gallstones.

Abstract: The present invention provides a method for the direct esterification of stanols and sterols with fatty acids to form stanol/sterol-esters. The method provides a synthetic route that is amenable to large scale production of the esters in high yields. A preferred embodiment employs a food grade process free ot organic solvents or mineral acids.

Abstract: The invention concerns a process for the preparation of stanol fatty acid esters mixtures by interesterification of stanol fatty acid esters starting material, of which at least 50% of the fatty acid groups are saturated, with fatty acid mixtures containing at least 35%, and preferably at least 45%, of poly unsaturated fatty acid (PUFA) groups, and wherein preferably the hardening of sterol fatty acid esters. The sterol fatty acid esters are preferably prepared by the esterification of phytosterols with a fatty acid ester mixture comprising at least 70% of C18 fatty acids, all steps can be carried out in the absence of a solvent. Also claimed are food products comprising the stanol fatty acid esters obtained by the process.

Abstract: This invention is relating to new estra-1,3,5(10)-trien-sulfamates carrying at the 3-position an R--SO.sub.2 --O--group, with R being an R.sup.1 R.sup.2 N--group in which R.sup.1 and R.sup.2, independently of each other, represent a hydrogen atom, an alkyl residue with 1-5 C atoms or, together with the N atom, a polymethylene-imino residue with 4-6 C atoms or a morpholino residue.The compounds, according to this invention, are suitable for hormonal contraception and climacteric hormone replacement therapy (HRT) as well as for treatment of gynecological and andrological diseases. Hence, only low hepatic estrogenicity is exhibited by the compounds according to this invention.Also described are processes for preparation of the compounds according to this invention and for preparation of pharmaceutical compositions.

Abstract: The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human vomeropherin, e.g. a pregnane or cholane steroid, or a pharmaceutical composition containing a vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.

Abstract: The present invention provides a method for the direct esterification of stanols and sterols with fatty acids to form stanol/sterol-esters. The method provides a synthetic route that is amenable to large scale production of the esters in high yields. A preferred embodiment employs a food grade process free of organic solvents or mineral acids.

Abstract: 21-norvitamin D.sub.3 analogs in which the methyl group normally attached to the side chain at carbon 20 has been replaced by a hydrogen atom. The compounds are characterized by a marked intestinal calcium transport activity while exhibiting much lower activity than 1.alpha.,25-dihydroxyvitamin D.sub.3 in their ability to mobilize calcium from bone. Because of their preferential calemic activity, these compounds would be useful for the treatment of diseases where bone formation is desired, such as osteodystrophy. Novel intermediates formed during the synthesis of the end products are also disclosed.

Abstract: Novel 17-hydroxyiminoalkyl and 17-hydroxyiminomethylalkenyl steroids of the general formula (I) ##STR1## where A, R.sup.1 and R.sup.2 are defined in the specification are disclosed. The compounds have cardiovascular activity. Pharmaceutical compositions containing compounds of formula (I) are also disclosed for the treatment of heart failure and hypertension.

Abstract: The present invention relates to a bile acid derivative, which comprises a bile acid derivatized at the carboxyl group with a hydroxamic acid or hydroxamate ester. The carboxyl group in the bile acid compound can also be derivatized with an amino acid or oligopeptide, whose C-terminus is derivatized with a hydroxamic acid or a hydroxamate ester. The present invention also relates to a method of use of a bile acid or a bile acid derivative to inhibit a metalloproteinase enzyme, comprising contacting a metalloproteinase with an effective amount of a bile acid or bile acid derivative. In another embodiment, the present invention further relates to a method of use of a bile acid or bile acid derivative to therapeutically treat a disease, which is ameliorated by inhibiting a metalloproteinase enzyme. In this method, a therapeutically effective amount of a bile acid, a bile acid derivative or physiologically acceptable salts thereof, is administered to a human or other mammal.

Abstract: Compounds having a broad range of antimicrobial activity generally have a structure including asteroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compounds of the Formula III: ##STR1## preferably where the steroid ring nucleus is saturated; the steroid ring substituent Z.sub.5 is .alpha.-H; one Z.sub.7 is .beta.-H and the other is .alpha.-H or .alpha.-OH; both substituents Z.sub.12 are hydrogen; X' is a polyamine side chain of the formula --NH--(CH.sub.2).sub.p --NH--(CH.sub.2).sub.q --N(R.sup.II)(R.sup.III) where p and q are each independently 3 or 4, and R.sup.II and R.sup.III are each independently hydrogen or methyl; R' is methyl; and Y' is (C.sub.1 -C.sub.10)-alkyl substituted with a group such as --CO.sub.2 H or --SO.sub.3 H.

Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.

Abstract: Invented are 17.alpha. and 17.beta.-substituted acyl-3-carboxy aromatic A ring analogues of steroidal synthetic compounds. Representative of such compounds include the following ##STR1## wherein Z is .alpha. or .beta. ##STR2## in which A is absent or present as a linear or branched, saturated or unsaturated hydrocarbon chain containing from 1-6 carbon atoms and R isa) a linear or branched, saturated or unsaturated hydrocarbon chain containing 1-12 carbon atoms substituted with one or more substituents selected from the group consisting of: --OC.sub.6 -C.sub.12 aryl, --OC.sub.1 -C.sub.4 alkyl, halogen, carboxy and --S(O).sub.n .sup.R.sup.7, where n is 0-2 and R.sup.7 is hydrogen or C.sub.1-4 alkyl;b) C.sub.3 -C.sub.8 nonaromatic, unsaturated or saturated, cycloalkyl, optionally substituted with one or more substituents selected from the group consisting of:--OC.sub.6 -C.sub.12 aryl, --(CH.sub.2).sub.m OH, --OC.sub.1 -C.sub.4 alkyl, C.sub.6 -C.sub.12 aryl, C.sub.1 -C.sub.

Abstract: A process for the preparation of glycine-conjugated bile acids as general formula (I):Y--NH--CH.sub.2 --COOH (I)wherein Y is the acyl radical of a bile acid selected from the group consisting of ursodeoxycholic, chenodeoxycholic, lithocholic, 3.alpha.-7.beta.-12.alpha.-tri-hydroxycholanic, 3.alpha.-7.beta.-dihydroxy-12-ketocholanic, deoxycholic, dehydrocholic, iodeoxycholic, iocholic acids and relative compositions for hepatic insufficiency treatment, containing the abovesaid acids as active ingredients, in continuation with suitable excipients and/or diluents.

Abstract: The invention describes hydrazino and hydroxyamino-14.beta.-hydroxyandrostane derivatives having general formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration and A, B, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 have the meanings given in the description and their use in the treatment of cardiovascular disorders such as heart failure and hypertension.

Abstract: Disclosed are 17-iminomethylalkenyl and 17-iminoalkyl-14.beta.-hydroxy-5.beta.-androstane derivatives of the formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration or a Z or E configuration; A represents (CH.sub.2).sub.m or --(CH.dbd.CH).sub.n --; m represents an integer number from 1 to 6; n represents an integer number from 1 to 3; R.sup.2 represents hydrogen or hydroxy; R.sup.1 represents hydrogen, C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5, which may be the same or different, represent hydrogen, C.sub.1 -C.sub.4 alkyl or R.sup.4 and R.sup.5 may form, when taken together with the nitrogen atom, a five- or six- membered heterocyclic ring optionally containing one or more heteroatoms selected from oxygen and nitrogen; R.sup.3 represents NHC(.dbd.X)NR.sup.6 R.sup.7 or OR.sup.8 wherein R.sup.6 and R.sup.7, which may be the same or different, represent hydrogen, methyl, or C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.

Abstract: The invention discloses steroid conjugates having the following structure: ##STR1## where Y is NHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, NH(CH.sub.2).sub.3 NH(CH.sub.2).sub.4 NH(CH.sub.2).sub.3 NH.sub.2, or NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2, and each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is individually H, OH and OSO.sub.3 H. These conjugates posses antimicrobial properties and are, therefore, useful as antibiotics.

Abstract: A process is described for the preparation of taurocholanic acids of formula (I): ##STR1## in which A completes the 5.beta.-cyclopentaneperhydrophenanthrene structure of a cholanic acid and E is hydrogen or a methyl group, by reacting the corresponding cholanic acid with the chloride of an acid having a tertiary carbon in the alpha-position, and treating the resulting mixed anhydride with taurine.

Abstract: The invention relates to substituted 17.alpha.-acyl steroidal 5.alpha.-reductase inhibiting compounds. The invention also relates to pharmaceutical compositions containing these compounds and their use for reducing prostate size and treating prostate adenocarcinoma. Further, the invention describes a process for making these compounds by heating the corresponding substituted 17.beta.-acyl steroid in a solvent, such as ethylene glycol or dimethyl sulfoxide (DMSO), in a base, such as sodium or potassium hydroxide.

Abstract: Novel bile acids according to the general formula ##STR1## wherein R.sub.1 represents a hydroxyl group, R.sub.2 and R.sub.3 both represent a hydrogen or a hydroxyl group, or R.sub.2 represents a hydroxyl group or a .beta. hydroxyl group and R.sub.3 represents a hydrogen or R.sub.3 represents a hydroxyl group and R.sub.2 represents a hydrogen, and R.sub.4 represents a (CH.sub.2).sub.n R.sub.5 wherein n is from 1 to 6, and R.sub.5 represents --0--PO(OH).sub.2, --CH(OH)COOH, a nitrogen containing saturated heterocyclic ring group, NR.sub.6 R.sub.7, wherein R.sub.6 and R.sub.7 are the same or different and each represent hydrogen or a C.sub.1 -C.sub.10 alkyl group or CO--R.sub.8 wherein R.sub.8 represents an amino acid moiety, R-phenylglycine, 12-aminododecanoic acid or 4-aminohippuric acid are synthesized from cholic, deoxycholic, chenodeoxycholic, ursodeoxycholic and lithocholic acids and iodo-derivatives thereof by known processes and/or by novel processes according to the present invention.

Abstract: The present invention relates to intermediates for use in the preparation of taurocholanic acids. The intermediates have the following formula (IV): ##STR1## in which A completes the 5.beta.-cyclopentaneperhydrophenanthrene structure of a cholanic acid; E is hydrogen or a methyl; and R is a hydrocarbon residue bonded to the carbonyl group by a tertiary carbon.

Abstract: The invention discloses N-alkyl-tauroursodeoxycholic acids and their pharmaceutically acceptable salts of the formula ##STR1## wherein R is a C.sub.2 -C.sub.4 alkyl group and R.sub.1 is hydrogen, an alkali metal, an alkaline earth metal or a radical of a basic amino acid.The compounds are prepared by reacting a mixed anhydride of ursodeoxycholic acid and alkyltaurine followed by percolation through two columns respectively containing a strong cationic resin in H.sup.+ form and a weakly anionic resin OH.sup.- form. The compounds are useful for the treatment of hepatic diseases.

Abstract: Vitamin D.sub.2 analogs in which a cyclopentane ring is introduced into the side chain of 1.alpha.,25-dihydroxyvitamin D.sub.2. The compounds are characterized by a marked intestinal calcium transport activity while exhibiting much lower activity than 1.alpha.,25-dihydroxyvitamin D.sub.3 in their ability to mobilize calcium from bone. Because of their preferential calcemic activity, these compounds would be useful for the treatment of diseases where bone formation is desired, such as osteoporosis.

Abstract: There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH;R.sup.2 is alpha- or beta-position methyl or ethyl;R.sup.1 is selected from heteroaryl radicals, cycloalkyl radicals, cycloalkenyl radicals, aryl radicals, alkenyl radicals, and alkyl radicals where R.sup.2 is in the alpha-position and an ethyl radical where R.sup.2 is in the beta-position; andR.sup.3 and R.sup.4 are selected from one of two different groups of substituent pairs, the group from which the selection is made being determined by the position of R.sup.2.

Abstract: Anti-inflammatory compounds, a method of treating inflamed ocular tissue and compositions of these compounds are described. The compounds are derivatives and analogues of known steroid compounds (e.g., dexamethasone) and are advantageously characterized in that they do not cause any significant increase in intraocular pressure during chronic use.

Abstract: Novel compounds of the general formula I ##STR1## and the pharmacologically tolerable addition salts thereof with acids are described, in which eitherIa) R.sup.11 represents a hydrogen atom in the .beta.-configuration and each of R.sup.12 and R.sup.13 represents a hydrogen atom, orIb) R.sup.11 represents a hydrogen atom in the .beta.-configuration and R.sup.12 and R.sup.13 together represent a second bond, orIc) R.sup.11 and R.sup.12 together represent a second bond and R.sup.13 represents a hydrogen atom, orId) R.sup.11 represents a hydrogen atom in the .alpha.-configuration and R.sup.12 and R.sup.13 together represent a second bond,and in Ia), Ib), Ic) or Id)X represents an oxygen atom, the hydroxyimino grouping >N.about.OH or two hydrogen atoms,R.sup.1 represents a hydrogen atom or a methyl group,R.sup.2 represents a hydroxy group, a C.sub.1 -C.sub.10 -alkoxy group or a C.sub.1 -C.sub.10 -acyloxy group, andR.sup.3 and R.sup.

Abstract: Process for the preparation of taurine-conjugated biliary acids of general formula (I):(Y--NH--CH.sub.2 --CH.sub.2 --SO.sub.3).sub.1 M (I)where Y is the acyl of a biliary acid selected from the group consisting of ursodeoxycholic, chenodeoxycholic, lithocholic, 3.alpha.-7.beta.-12.alpha.-tri-hydroxycholanic, 3.alpha.-7.beta.-dihydroxy-12-ketocholanic, deoxycholic, dehydrocholic, iodeoxycholic, iocholic acids; M is H, Na, K, Mg, Ca; 1 is 1 or 2, being 2 when M=Mg or Ca.

Abstract: Disclosed are compositions containing bile acid-aminosalicylate conjugates having the formula, or a pharmaceutically acceptable salt thereof ##STR1## wherein R.sub.1 is OH either the .alpha. or the .beta. position;R.sub.2 is OH;R.sub.3 is H or OH; andR.sub.4 is H or acetyl,the process for their preparation and method of treating/preventing gastrointestinal disorders, impaired liver function, autoimmune diseases of the liver and biliary tract, colon cancer, inflammatory bowel diseases, Crohn's disease, cystic fibrosis, dissolving gallstones, and regulating dietary cholesterol absorption by administering said compositions to a mammal in need of such treatment.

Abstract: A compound of the formula ##STR1## wherein R.sub.1 is an aliphatic hydrocarbon of 1 to 8 carbon atoms, R.sub.2 and R.sub.3 are individually hydrogen or alkyl of 1 to 4 carbon atoms, G is a hydrocarbon of 1 to 18 carbon atoms optionally containing at least one heteroatom and linked to the steroid nucleus by a carbon atom, X is X.sub.A or X.sub.B, X.sub.A is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, aralkyl of 7 to 15 carbon atoms, acyl of an organic carboxylic acid of 1 to 8 carbon atoms and Y is -B-O--CO--A-Z, B is a saturated or unsaturated, linear or branched alkylene of 1 to 8 carbon atoms, A is a saturated or unsaturated, linear or branched alkylene of 1 to 6 carbon atoms and optionally interrupted or ended by a bivalent aromatic or is a bivalent aromatic and Z is --COOH or --SO.sub.3 H which may be salified with an alkali metal, alkaline earth metal, an organic amine or --NH.sub.4 or X.sub.

Abstract: There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH;R.sup.2 is alpha- or beta-position methyl or ethyl;R.sup.1 is selected from heteroaryl radicals, cycloalkyl radicals, cycloalkenyl radicals, aryl radicals, alkenyl radicals, and alkyl radicals where R.sup.2 is in the alpha-position and an ethyl radical where R.sup.2 is in the beta-position; andR.sup.3 and R.sup.4 are selected from one of two different groups of substituent pairs, the group from which the selection is made being determined by the position of R.sup.2.

Abstract: The invention relates to 11-aryl steroid derivatives, having the structure ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as described in the specificationand to processes for their preparation and to pharmaceuticals comprising these compounds.These compounds exhibit a strong anti-progestinic activity and a weak or non-existent anti-glucocorticoid activity.

Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain.

Abstract: Compounds of general formula I ##STR1## wherein R.sub.1 is hydrogen or hydroxy, and the hydroxy group at the 7-position can be either in .alpha. or .beta. configuration, are valuable in human therapy. Compounds I can be prepared by fluorination of the suitably protected 6.alpha.-hydroxy-7-keto-derivatives.

Abstract: Novel 19-nor-steroids of the formula ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2## having hormonal properties and their preparation and intermediates.

Abstract: A process for the production of 3-deoxy-4-ene steroids of the general formula I ##STR1## is described, in which R.sub.1, R.sub.2 and R.sub.3 mean a hydrogen atom or a methyl group,R.sub.4 represents a lower alkyl group, a phenyl group or a free, esterified or etherified hydroxy group,R.sub.5 symbolizes a hydrogen atom, a vinyl group or the grouping --C.tbd.CR.sub.6 with R.sub.6 meaning a hydrogen atom, an alkyl group with a maximum of 4 carbon atoms or a halogen atom,X represents a methylene group, a fluoromethylene group, an ethylidene group or a vinylidene group,Y and U represent a methylene group or an ethylidene group andZ symbolizes a methylene group, an ethylidene group, a vinylidene group, a chloromethylene group or a hydroxymethylene group and in which the bonds represent three single bonds or one double bond and two single bonds or a conjugated double bond.

Abstract: Acid addition salt of taurine or glycine, their amino group being amidated with a carboxylic acid residue which contains the structure of a 3.alpha., 7.alpha., 12.alpha.-trihydroxysteroid, their acid group being neutralized with the amino group of an aliphatic amine or neutralized with the amino group of a basic .alpha.-amino carboxylic acid which group is connected over an alkylene bridge with the .alpha.-amino acid group, may be used e.g. as transmucuous resorption promoter of drug compounds.

Abstract: Aldosterone biosynthesis inhibitors having substantially no intrinsic antiandrogenic activity are disclosed as well as pharmaceutical compositions containing such compounds and methods of treatment utilizing these compositions.

Abstract: A compound of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl, R.sub.2 is methyl or ethyl, the A,B,C and D rings optionally containing at least one double bond and optionally substituted with at least one member of the group consisting of optionally protected --OH, .dbd.O, alkyl and alkoxy of 1 to 4 carbon atoms, halogen and alkenyl and alkynyl of 2 to 4 carbon atoms, R is selected from the group consisting of halogen, --OH, alkylthio and alkoxy of 1 to 6 carbon atoms, aralkoxy, arylthio and aralkylthio of 7 to 15 carbon atoms and ##STR2## R.sub.3 and R.sub.4 are individually hydrogen, or alkyl of 1 to 6 carbon atoms or aralkyl of 7 to 15 carbon atoms or taken together with the nitrogen form a heterocycle optionally containing another nitrogen or oxygen atom, excepting the product in which R is methoxy, R.sub.1 and R.sub.2 each represent methyl, A ring carries a 3.beta.-acetoxy function and B ring contains a double bond in 5(6) useful as intermediates for the preparation of 20-keto-pregnanes.

Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl, alkylthio and haloalkyl of 1 to 6 carbon atoms, alkenyl and alkynyl of 2 to 6 carbon atoms, optionally substituted arylthio of 6 to 10 carbon atoms, aryl of 6 to 12 carbon atoms, acyl of an organic carboxylic acid of 1 to 12 carbon atoms, --CN, cycloalkyl of 3 to 6 carbon atoms and --(CH.sub.2).sub.m --Re, m is an integer from 1 to 3, Re is --OH or --SH or --Salk, Alk is alkyl of 1 to 6 carbon atoms, X is selected from the group consisting of oxygen, N--O--R.sub.1, ##STR2## or =X is H.sub.2 or ##STR3## R.sub.A and R.sub.B are individually selected from the group consisting of hydrogen, halogen and alkyl of 1 to 6 carbon atoms, R.sub.1 is hydrogen or alkyl of 1 to 6 carbon, R' is hydrogen or acyl, the wavy lines indicate --or -position, Y is selected from the group consisting of oxygen, NOR, ##STR4## or =Y is ##STR5## H.sub.

Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of naphthyl, phenylphenyl, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms optionally containing additional unsaturations, phenoxy, furyl, cycloalkyl of 3 to 6 carbon atoms, thienyl optionally substituted with at least one member of the group consisting of halogen and alkyl and haloalkyl of 1 to 6 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of --OH, halogen, --CF.sub.3, alkyl and alkoxy of 1 to 6 carbon atoms, alkenyloxy of 2 to 6 carbon atoms, phenoxy and alkylthio of 1 to 6 carbon atoms optionally oxidized to the sulfoxide or sulfone, R.sub.2 is selected from the group consisting of methyl and ethyl, R.sub.

Abstract: Novel esters of 9.alpha.-fluoro- and chloro-corticosteroids of the formula ##STR1## wherein Y is chlorine or OR.sub.1, R.sub.1 and R.sub.2 represent an acyl group of 2-6 carbon atoms or a benzoyl group and where R.sub.1 and R.sub.2 can be the same or different in the same molecule, R.sub.3 is methyl or fluorine in either the .alpha.- or .beta.- orientation, X is chlorine or fluorine, and the C.sub.1 C.sub.2 bond can be saturated or not, especially those compounds of the formula ##STR2## wherein Y and R.sub.2 have the significance given above, are prepared by reacting the respective 9.beta.,11.beta.-epoxy compounds with hydrogen fluoride or chloride.

Abstract: Novel 19-nor steroids of the formula ##STR1## wherein R' is selected from the group consisting of propyl, propenyl, iodoethenyl, iodoethynyl or --C.tbd.C--CH.sub.2 --Hal.sub.1, Hal.sub.1 is selected from the group consisting of fluorine, chlorine and bromine and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antiglucocorticoid and antiprogestomimetic activity.

Abstract: Disclosed herein is a novel steroids represented by the formula (1): ##STR1## wherein Z represents ##STR2## n is integer of 1 to 3, R represents hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy or --CO.sub.2 R', wherein R' represents hydrogen, alkali metal or lower alkyl, andR.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent hydrogen or acyl, respectively.The compound of the formula (1) of the present invention exhibits high durability as well as excellent plant growth regulation.

Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutial compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase including using these compounds to reduce prostate size. Also invented are intermediates used in preparing these compounds.

Abstract: A compound of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl, R.sub.2 is methyl or ethyl, and A,B,C and D rings optionally containing at least one double bond and optionally substituted with at least one member of the group consisting of optionally protected --OH, .dbd.O, alkyl and alkoxy of 1 to 4 carbon atoms, halogen and alkenyl and alkynyl of 2 to 4 carbon atoms, R is selected from the group consisting of halogen, --OH, alkylthio and alkoxy of 1 to 6 carbon atoms, aralkoxy, arylthio and aralkylthio of 7 to 15 carbon atoms and ##STR2## R.sub.3 and R.sub.4 are individually hydrogen, or alkyl of 1 to 6 carbon atoms or aralkyl of 7 to 15 carbon atoms or taken together with the nitrogen form a heterocycle optionally containing another nitrogen or oxygen atom, excepting the product in which R is methoxy, R.sub.1 and R.sub.2 each represent methyl, A ring carries a 3.beta.-acetoxy function and B ring contains a double bond in 5(6) useful as intermediates for the preparation of 20-keto-pregnanes.