Abstract: The invention relates to substituted 4-benzylaminoquinolines and their hetero analogs, and to the pharmaceutically acceptable salts and physiologically functional derivatives thereof. Compounds of formula I in which the radicals are defined in the specification, and their physiologically tolerated salts, physiologically functional derivatives and processes for their preparation are described. The compounds are suitable, for example, as medicines for the prophylaxis or treatment of gallstones.

Abstract: A subject of the invention is the compounds of formula (I): 1

Abstract: A process for producing a compound of formula (I): wherein the dotted lines - - - independently represent a single or double bond and R, R1, R2 and R3 are each hydrogen or an organic radical, comprises treating the corresponding 17&bgr;-carbonylimidazole intermediates with anhydrous acids in the presence of an amine and, optionally, hydrogenating the resulting compound.

Abstract: This invention describes new, substituted 7&agr;-(&egr;-aminoalkyl)-estratrienes of general formula I in which side chain SK is a radical of partial formula The new compounds represent compounds with very strong antiestrogenic action. The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.

Abstract: A subject of the invention is the compounds of formula (I): 1

Abstract: The present invention discloses compounds which are cationic cholesteryl derivatives having a nitrogen-containing ring structure as their polar head group. These compounds are useful for delivering biologically active substances to cells and for transfecting nucleic acids into cells.

Abstract: A subject of the invention is the compounds of formula (I): 1

Abstract: The invention concerns steroid compounds of general formula (I) in which n=2, 3, either R1 and R2═H, (C1-C4) alkyl, or R1 and R2 form with nitrogen a heterocyclic compound, X═OH optionally esterified, Y═(C1-C4)alkyl, and their additive salts, the method for preparing them, their application as medicine and the pharmaceutical compositions containing them.

Abstract: Compounds of formula (I) in which the radicals are as defined in the specification and claims, and physiologically tolerated and physiologically functional derivatives thereof and processes for their preparation are described. The compounds are suitable, for example, as hypolipidemic agents.

Abstract: Methods, compositions, and compounds for modulating the GABA.sub.A receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia.

Abstract: The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.

Abstract: The invention is directed to 20-keto-11.beta.-arylsteroids of formula I: ##STR1## wherein R.sup.1, R.sup.6, R.sup.7, R.sup.9, R.sup.12 and X are as defined by the specification. The compounds exhibit progestational and antiprogestational activities.

Abstract: Compounds represented by the following formula I: ##STR1## in which: R.sup.1 to R.sup.5 can have various meanings of which alkyl, substituted or non-substituted aryl, and m is equal to 0 or 1, X is selected from (CR.sup.6 R.sup.7).sub.n in which n=0 or 1, and CO are disclosed. These compounds are useful as anti-tumor drugs, especially with pro-oxidizing activity.

Abstract: Methods, compositions, and compounds for modulating the GABA.sub.A receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia.

Abstract: Compounds of the general formula I ##STR1## are described, in which x represents an oxygen atom or the hydroxyimino grouping >N.about.OH,R.sup.1 represents a hydrogen atom or a methyl group,G represents a hydrogen atom, a halogen atom or a C.sub.1 -C.sub.4 -alkyl radical, when M and Q are hydrogen atoms or together are an additional bond,Q represents a C.sub.1 -C.sub.4 -alkyl radical when M and G are hydrogen atoms, orG and M together represent a methylene or ethylene group when Q is a hydrogen atom,and R.sup.2, R.sup.3 and R.sup.4 have the meanings given in the description.The novel compounds have pronounced antigestagenic and also antiglucocorticoid, antimineralocorticoid and antiandrogenic properties and are suitable for the preparation of medicaments.

Abstract: Compounds of formula I ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings indicated in the description, are described, as well as processes for their production, pharmaceutical preparations containing these compounds as well as their use for treatment of diseases. The compounds have antigestagenic, antiglucocorticoid, antimineralocorticoid and antiandrogenic properties.

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: A compound represented by the following formula (I):X--Y--Z (I)?where Y is represented by the following formula (III): ##STR1## X is a monovalent group of a tetracycline type compound, and Z is a monovalent group of a steroid type compound such as estrogen!. The compound can concentrate on the bone tissue and has a bone resorption inhibition/ossification promotion functions.

Abstract: Compounds of formula (I): ##STR1## ?wherein: R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is: aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl!; and pharmaceutically acceptable salts and esters thereof have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydrotestosterone.

Abstract: A 19-nor-steroid having a formula selected from the group consisting of ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2##

Abstract: Bile acid derivatives of the formula IW--X--Gin which G is a bile acid radical, W is an active compound moiety of a medicament and X is a bonding member between a bile acid radical and active compound moiety, are outstandingly suitable for introducing active compounds into the enterohepatic circulation. The compounds I are absorbed and pass into the bloodstream. It is possible in this way, using the natural reabsorption of the bile acids, to achieve improved absorption of non-absorbable or poorly absorbable pharmaceuticals.W may be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a hepatoprotective agent, an antihyperlipidemic, a diuretic, a hypotensive, a renin inhibitor, a substance for the treatment of cirrhosis of the liver or a substance for the treatment of diabetes.G is a bile acid radical in the form of the free natural or chemically modified acids, the esters and amides, the salt forms and forms derivatized on alcohol groups.

Abstract: Bile acid derivatives of the formula IW--X--Gin which G is a bile acid radical, W is an active compound moiety of a medicament and X is a bonding member between a bile acid radical and active compound moiety, are outstandingly suitable for introducing active compounds into the entercepatic circulation. The compounds I are absorbed and pass into the bloodstream. It is possible in this way, using the natural reabsorption of the bile acids, to achieve improved absorption of non-absorbable or poorly absorbable pharmaceuticals.W may be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a hepatoprotective agent, an antihyperlipidemic, a diuretic, a hypotensive, a renin inhibitor, a substance for the treatment of cirrhosis of the liver or a substance for the treatment of diabetes.G is a bile acid radical in the form of the free natural or chemically modified acids, the esters and amides, the salt forms and forms derivatized on alcohol groups.

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: The invention relates to a 11,21-bisphenyl-19-norpregnane derivative of formula I ##STR1## wherein R.sub.1 is selected from H, halogen, (1-6C)alkoxy, and NR.sub.5 R.sub.6, R.sub.5 and R.sub.6 being independently hydrogen or (1-6C)alkyl or R.sub.5 and R.sub.6 together are (3-6C)alkylene; R.sub.2 is hydrogen; or R.sub.1 and R.sub.2 together are a (1-3C)alkylenedioxy group, optionally substituted by one or more halogen atoms; R.sub.3 is methyl or ethyl; R.sub.4 is selected from C(O)-NR.sub.5 R.sub.6, SO.sub.n -(1-6C)alkyl optionally substituted by one or more halogen atoms, SO.sub.n -(3-6C)cycloalkyl, n being 1 or 2, SO.sub.2 -NR.sub.5 R.sub.6, 2-oxypyrrolidinyl, and NR.sub.5 R.sub.6 ; R.sub.7 is H or (1-6C)alkyl; R.sub.8 is H or carboxy-1-oxo(1-6C)alkyl; and X is selected from (H,OH), O, and NOH; 11 or a pharmaceutically acceptable salt thereof.The compounds of the invention have anti-glucocorticoid activity and can be used in treating or preventing glucocorticoid-dependent diseases.

Abstract: Corticoid 17-alkyl carbonate 21-carboxylic and carbonic esters of the formula I ##STR1## are described in which A is CHOH and CHCl, CH.sub.2, C.dbd.O or 9(11) double bond; Y is H, F or Cl; Z is H, F or CH.sub.3 ; R(1) is aryl or hetaryl; n and m are zero or 1; R(2) is alkyl or --(CH.sub.2).sub.2 --OCH.sub.3 ; R(3) is H or methyl. They are obtained by reacting a compound of the formula II, ##STR2## in which R(5) is OH, with an activated carboxylic acid of the formula III,R(6)--CO--(O).sub.n --(X)--R(1) III.The compounds I have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects, which ratio is often markedly superior to that of analogous corticoid 17-alkyl carbonate 21-esters which do not carry any aryl or heteraryl group in the 21-ester radical.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.

Abstract: Described is a new process for producing 7.beta.-substituted-4-aza-5.alpha.-androstan-3-ones and related compounds which are 5.alpha.-reductase inhibitors, consisting of reducing the corresponding androsteneone with lithium and liquid ammonia, contacting the product with an isomerizing agent, oxidizing the product to a seco acid and reacting that seco acid with an amine to cyclize to form 4-aza-5.alpha.-androstan-3-ones.

Abstract: New 9-alpha-hydroxy steroids are prepared by the introduction of substituents on the D-ring of 9-alpha-hydroxy-androst-4-ene-3,17-dione.The resulting compounds are useful intermediates in the synthesis of corticosteroids.

Abstract: Novel, therapeutically active 21-aminosteroids of formula (I) ##STR1## with pregnane skeleton, are disclosed wherein two of X, Y and Z are a nitrogen atom each and the third one is a methine group; R.sup.1 and R.sup.2 are independently from each other, a primary amino group bearing as substituent a branched-chain C.sub.4-8 alkyl -alkenyl or -alkynyl group, or a C.sub.4-10 cycloalkyl group comprising 1 to 3 ring(s) and being optionally substituted by at least one C.sub.1-3 alkyl group; or R.sup.1 and R.sup.2 are each a spiro-heterocyclic secondary amino group containing at most 10 carbon atoms and optionally at least one oxygen atom as additional heteroatom; or one of R.sup.1 and R.sup.2 is an unsubstituted heterocyclic secondary amino group containing 4 to 7 carbon atoms and the other one is an above-identified primary amino group, an above-identified spiro-heterocyclic secondary amino group, or a heterocyclic secondary amino group containing 4 to 7 carbon atoms and substituted by at least one C.sub.

Abstract: 14-Deoxy-14.alpha.-cardenolides 3.beta.-thioderivatives and pharmaceutical compositions comprising same for treating cardiovascular disorders, such as heart failure and hypertension, are disclosed.

Abstract: Bile acid derivatives, processes for their preparation and use as pharmaceuticals Bile acid derivatives of the formula IW--X--Gin which G is a bile acid radical, W is an active compound moiety of a medicament and X is a bonding member between a bile acid radical and active compound moiety, are outstandingly suitable for introducing active compounds into the enterohepatic circulation. The compounds I are absorbed and pass into the bloodstream. It is possible in this way, using the natural reabsorption of the bile acids, to achieve improved absorption of non-absorbable or poorly absorbable pharmaceuticals.W may be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a hepatoprotective agent, an antihyperlipidemic, a diuretic, a hypotensive, a renin inhibitor, a substance for the treatment of cirrhosis of the liver or a substance for the treatment of diabetes.

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: Disclosed are amino substituted steroids (XI) which contain a pyridinylpiperazinyl group group attached to the terminal carbon atom of the C.sub.17 -side chain of the steroid which are useful as pharmaceutical agents for treating a number of conditions.

Abstract: Disclosed are amino substituted steroids (XI) which contain a phenylpiperazinyl group attached to the terminal carbon atoms of the C.sub.17 -side chain, which are useful as pharmaceutical agents for treating a number of conditions.

Abstract: The invention includes compounds of the following formula ##STR1## where A and B either A and B form an additional double bond and D is a hydrogen atom or B and D form an additional double bond and A is a hydrogen atom and the other variables are as defined in the specification. Also disclosed is a process of making the compounds and a process of using the compounds to make compounds of the following formula ##STR2## where the variables are defined in the specification. These compounds are useful as antigestigens.

Abstract: The novel compounds of the invention are 19 nor-steroids of the formula: ##STR1## Where A, B, C, D, X, Y, Z, R.sub.17, and R.sup.1 are as defined in the specification, having hormonal properties and their preparation and intermediates.

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: New 11.beta.-phenyl-14.beta.H-steroids of general formula (I), where Z is an oxygen atom or the hydroxyimino-grouping N.about.OH, and M and N are either jointly a second compound or L is a hydrogen atom and M is an .alpha.-permanent hydroxy group and either A and B together are a second compound and D is a hydrogen atom, where R.sup.1 is a five or six-part heteroalkyl residue or a cycloalkyl, cycloalkenyl or aryl residue or A is a hydrogen atom and B and D together are a methylene bridge, where R.sup.1 besides the aforementioned residues may be a possibly substituted hydrocarbon residue with up to 10 C atoms, a possibly substituted amino group, a hydroxy or C.sub.1-8 alkoxy, mercapto or thioalkyl group, R.sup.2 is a methyl or ethyl residue, and R.sup.3 /R.sup.4 represents the usual combination of substituents on the C17 atom in steroid chemistry, having antigestagenic and other properties.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionophore (GBR) complex.

Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.A, R'.sub.A, R.sub.B and R'.sub.B are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms or R.sub.A and R'.sub.A or R.sub.B and R'.sub.B together with the nitrogen atom to which they are attached form a 5- to 6-member heterocycle optionally substituted with alkyl of 1 to 3 carbon atoms and Y is hydrogen or ##STR2## wherein R.sub.6 is selected from the group consisting of hydrogen, --CH.sub.3, --F and --Cl, R.sub.9 and R.sub.11 form a second bond at 9(11) or R.sub.9 is hydrogen or --F is hydrogen, --OH or .dbd.O, R.sub.16 is --CH.sub.3 or hydrogen, R.sub.17 is hydrogen, --OH or acyloxy, the dotted lines indicate the possible presence of a second bond at 1(2) and 6(7)-positions and the wavy line indicates the .alpha.- and .beta.-position and their non-toxic, pharmaceutically acceptable acid addition salts having anti-inflammatory and antioxidant activity.

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: 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: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.

Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.2 and R'.sub.2 are individually hydrogen or methyl, R.sub.11 is an organo of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom adjacent to the 11-carbon atom being a carbon, the wavy lines at the 13 and 17-positions indicate that when the 13-methyl is .alpha., R'.sub.17 group is .beta. and R.sub.17 is .alpha. and when the 13-methyl is .sub..beta., R.sub.17 is .sub..beta. and R'.sub.17 is .alpha., R.sub.17 is --OH or acyloxy of 1 to 18 carbon atoms and R'.sub.

Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.

Abstract: The invention relates to new 11-arylsteroid compounds, having a strong antiprogestin and a weak or nonexistent antiglucocorticoid activity, to processes for preparing said compounds and also to pharmaceutical preparations which contain these derivatives as active constituent, characterized in that said steroids have the following formula: ##STR1## in which R.sub.1 is an aryl group with a ##STR2## group as substituent, X and Y each being separately H or a (1-4 C) hydrocarbyl group or together a (2-C) hydrocarbyl group which forms a 3- to 7-membered ring together with the nitrogen atom;R.sub.2 is hydrogen, hydroxyl, an acyloxy or an alkoxy group or a saturated or unsaturated hydrocarbyl group containing 1-8 carbon atoms, which hydrocarbyl group is provided with at least one hydroxyl, oxo, azido, cyano and/or halogen group;R.sub.3 is a hydroxyl, an acyloxy or an alkoxy group or an acyl group optionally substituted by a hydroxyl, alkoxy, acyloxy or halogen group; or R.sub.2 and R.sub.

Abstract: Steroids of the formula: ##STR1## which are characterized by a 17.alpha.-cyanomethyl, azidomethyl, methoxymethyl, phenylmethyl, or ethynylmethyl substituent and a 17.beta.-hydroxy/esterified hydroxy substituent. The steroids of this invention have glucocorticoid, anti-glucocorticoid, progestational, or anti-progestational activity, depending on the particular structure.

Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.