Abstract: Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders.

Abstract: A plurality of hip, ridge or rake shingles, and the shingles produced thereby and stacks and packages of such shingles are provided. An adhesive impregnated mat is moved longitudinally, and granules are provided onto adhesive, in predetermined bands. An overlay band of adhesive, continuous or discontinuous is provided, with granules thereon, increasing the thickness of the shingle material being made, in predetermined bands, relative to the remainder of the shingle material. The shingle material is slit longitudinally, and one portion can be laminated to another portion, preferably creating a multiple-ply laminated shingle material with thickened overlay portions and optionally with shadow line portions. The material is then slit longitudinally, and cut transversely into a plurality of hip, ridge or rake shingles, which may be individually separated from each other, or which may comprise a plurality of connected together shingles. The shingles are then stacked and wrapped.

Abstract: The invention relates to an antagonist of CB1 receptor for use in the treatment of a pathologic condition or disorder selected from the group consisting of bladder and gastrointestinal disorders; inflammatory diseases; cardiovascular diseases; nephropathies; glaucoma; spasticity; cancer; osteoporosis; metabolic disorders; obesity; addiction, dependence, abuse and relapse related disorders; psychiatric and neurological disorders; neurodegenerative disorders; autoimmune hepatitis and encephalitis; pain; reproductive disorders and skin inflammatory and fibrotic diseases.

Abstract: The invention provides skin protecting and penetrating, easy-to-administer base and active agent-containing compositions, such as those including hydrocortisone, for treating the skin of mammals for different dermatologic disorders. This is effected by topically administering effective amounts of the compositions thereto in forms that address the skin and mucosa of the mouth and lips, and the rest of the body. Additionally, an optional flavoring addition to these products affords significantly better tasting, and less bitter, compositions, allowing a more pleasant experience and better compliance by patients. The compositions include a unique formulation of FANCOL VB, Natunola Castor 1023, Finsolv TN, bees wax and, optionally, one or a plurality of plant or plant seed oils, fatty alcohols, fats and flavorings, in desirable weight percents thereof, in various forms, and preferably in a form of a solid roll-on stick in a variety of sizes and of a jar or pot.

Abstract: Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders.

Abstract: Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders.

Abstract: The invention relates to methods to manipulate stem cells in vivo and in vitro to treat, e.g., a condition where cell or tissue repair is needed.

Abstract: Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders.

Abstract: A compound with general formula I for treatment of various diseases of the central nervous system, in treatment of neuropsychiatric disorders related to imbalance of glutamatergic neurotransmitter system, ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, PTSD and other diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addictions, multiple sclerosis, epilepsy and gliomas.

Abstract: Polymers may include a plurality of tetradecahydroanthracene moieties. Such polymers may be used to make food or beverage containers or medical devices. Food or beverage containers or medical devices may be coated with polymers including a plurality of tetradecahydroanthracene moieties.

Abstract: Polymers may include a plurality of tetradecahydroanthracene moieties. Such polymers may be used to make food or beverage containers or medical devices. Food or beverage containers or medical devices may be coated with polymers including a plurality of tetradecahydroanthracene moieties.

Abstract: There is provided a process for preparing 21-acetyloxy-6-alpha-fluoro-pregna-1,4,9(11),16-tetraene-3,20-dione compound of Formula I, which comprises reacting 21-acetyloxy-pregna-1,3,5,9(11),16-pentaene-3-oxo acetate with a fluorinating agent.

Abstract: Steroidal compounds or their salts having general formulas (I) and (II) wherein: s is an integer equal to 1 or 2, preferably s=2; b0=0 or 1; A=R—, wherein R is the steroidal drug radical, C and C1 are two bivalent radicals. The precursors of the radicals B and B1 are such as to meet the pharmacological tests reported in the description.

Abstract: This invention is directed to methods for providing sustained systemic concentrations of therapeutic or prophylactic agents such as GABA analogs following oral administration to animals. This invention is also directed to compounds and pharmaceutical compositions that are used in such methods.

Abstract: The invention relates to 17&agr; fluoroalkyl steroids of the general formula (I). STEROID (I), wherein R3 represents a group of the formula CnFmHo, wherein n=1, 2, 3, 4, 5 or 6, m>1 and m+o=2n+1. The invention further relates to methods for producing the same and to compositions that contain said compounds. The inventive composition of the general formula (I) possess androgenic activity.

Abstract: The present invention concerns with steroid compounds of formula (I) wherein R1 is cyclohexyl or cycloheptyl, R2 is hydrogen or C1-C6 alkyl, R3 is hydrogen, C1-C6 alkyl or methylol, R4 is hydrogen or hydroxymethylene and a pharmaceutically acceptable salt thereof. The invention also concerns with a method for preparation of the compounds, pharmaceutical compositions containing the compounds as its active component and use of the compounds and the pharmaceutical compositions in preparing medicines for treating diseases, e.g. those associated with progestin dependence.

Abstract: Certain novel sterol derivatives can be used for regulating the meiosis in oocytes and in male germ cells.

Abstract: A water soluble delivery system for nucleic acids to cells having androgen receptors, preferably prostate cells, is provided comprising a steroid moiety capable of binding to said receptors, said steroid moiety being covalently linked to a polycationic material. This molecule may be complexed with therapeutic or diagnostic nucleic acids. Methods of diagnosis and therapy using these compositions are also provided, including gene therapy treatments for prostate cancer.

Abstract: Bile-acid conjugates useful for sustained release of L-DOPA, inhibitors of catechol O-methyl transferase and/or inhibitors of L-aromatic amino acid decarboxylase are provided.

Abstract: A series of novel steroid derivatives are described. The steroid derivatives are antibacterial agents. The steroid derivatives also act to sensitize bacteria to other antibiotics including erythromycin and novobiocin.

Abstract: This invention provides a method of providing progestational therapy to a mammal in need thereof which comprises administering a progestationally effective amount of a pharmaceutically acceptable salt of 5&agr;-pregnan-3&bgr;-ol-20-one 3-sulfate ester to said mammal.

Abstract: Newly isolated aminosterol compounds and pharmaceutical compositions based on the aminosterol compounds are described. Methods for the treatment of various disorders, for example, a microbial infection, are also described.

Abstract: The subject of the invention is the products of formula (I): 1

Abstract: The invention relates to 17&bgr;-aryl(arylmethyl)oxy(thio)alkyl-androstane derivatives having general formula (I), wherein R1 is (H,OR), (H,OSO3H) or NOR; with R being H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 is independently hydrogen or (C1-6)alyl; n is 0, 1, or 2; X is O, S, S(O) or S(O)2; m is 0 or 1; each of R4, R5 and R6 is independently hydrogen, hydroxy, (C1-4)alkoxy, halogen, NR7R8 or (C1-4)alkyl, optionally substituted by hydroxy, alkoxy, halogen or oxo; each of R7 and R8 is independently hydrogen or (C1-4)alkyl, and wherein the dotted lines indicate a &Dgr;7 or a &Dgr;8 double bond, or a pair of conjugated double bonds selected from &Dgr;7,14, &Dgr;8,14 and &Dgr;6,8(14); or a pharmaceutically acceptable salt thereof. The compounds of the invention have meiosis regulating activity and can be used for the control of fertility.

Abstract: Certain novel sterol derivatives can be used for regulating the meiosis in oocytes and in male germ cells.

Abstract: Disclosed are (i) compounds of a steroid, a &bgr;-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, &bgr;-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.

Abstract: The invention relates to compounds of the formula: in which R1, R2, R3, R4, R5, R6, n and X are as defined in the specification, and to pharmaceutical compositions containing them. These compounds are excellent progestogens which are devoid of residual androgenic activity.

Abstract: The invention relates to 20-aralkyl-5&agr;-pregnane derivative having general formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 is (H,OR), (H,OSO3H) or NOR; R is H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 is independently hydrogen or (C1-6)alkyl; X is a straight chain divalent C1-8 hydrocarbon radical, optionally comprising a double or a triple bond; or X is —(CH2)m—CR7R8—; m=0-4; at least one of R7 and R8 is (C1-4)alkyl, hydroxy, (C1-4)alkoxy or halogen; the other, if present, being hydrogen; or R7 and R8 together represent O or NOR′; R′ is H, (C1-6)alkyl or (C1-6)acyl; each of R4, R5 and R6 is independently hydrogen, hydroxy, (C1-4)alkoxy, halogen, NR9, R10 or (C1-4)alkyl, optionally substituted by hydroxy, alkoxy, halogen or oxo; each of R9 and R10 is independently hydrogen or (C1-4)alkyl; and the dotted lines indicate a &Dgr;7 or a &Dgr;8 double bond, or a pair of conjugated double bonds selected from &Dgr;7,14, &Dgr;8,14 and

Abstract: Novel potentiating steroid carbamates having the general formula (I)ST-OCONR.sub.1 R.sub.2 (I)wherein ST is a steroid or steroid derivative, of the structure (II) ##STR1## optionally containing double bonds and additional oxygen substituents; the carbamate moiety OCONR.sub.1 R.sub.

Abstract: 16.alpha., 17.alpha.-dialkylated steroids are prepared by reacting a 16.alpha.-alkyl-17(20)-enyl-20-silyl ether with an alkylating agent and an enol silyl ether cleaving agent in a suitable solvent.

Abstract: Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R.sup.1 through R.sup.10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat androgen-related clinical conditions are provided, as are methods and compositions for using the compounds as contraceptive agents.

Abstract: Invented are 17.alpha. and 17.beta.-substituted acyl-3-carboxy-3,5-diene analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates and processes used in preparing these compounds.

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: 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: The present invention relates to an oligonucleotide or analog thereof conjugated to a molecule comprising a structure, which structure (a) is of substantially fixed conformation; (b) contains, is directly attached to, or is attached to a carbon atom that is directly attached to, an first amine; and (c) contains, is directly attached to, or is attached to an atom that is directly attached to a phosphate, a second amine, or a cationic sulfur. In a preferred embodiment, the structure consists of at least a nonaromatic cyclic portion or substituted derivative thereof. In a specific embodiment, the structure is a nonaromatic cyclic compound. In another embodiment, the molecule is a steroid. In yet another particular aspect, the structure is an aromatic compound. In another embodiment, the structure can bind to a nucleic acid sequence in a nonintercalative manner.

Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted by halogen or a nitrogen or oxygen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A, B, C and D rings are optionally substituted by at least one member of the group consisting of optionally protected --OH or .dbd.0, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 and the A, B, C and D rings are defined as above with an oxidizing agent in the presence of water and an at least partially water-miscible solvent to obtain a compound of the formula ##STR3## wherein R.sub.1 and R.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: 14.beta.-hydroxy-3.beta.-(.alpha.-L-rhamnopyranosyl) and-tridigitoxide-oxy-20-nitro-21-nor-5.beta.,14.beta.-pregnanes exhibit unexpectedly high cardiac potency with tolerance to high dosage levels.

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: Invented are 3-acetic acid-steroidal compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase including using these compounds to reduce prostate size and to treat prostatic adenocarcinoma. Also invented are intermediates used in preparing these compounds.

Abstract: This invention relates to a stereoisomerically pure .DELTA..sup.2 compound of the formula (I): ##STR1## wherein: R.sup.1 is hydrogen or --(C.dbd.O)--R.sup.2, wherein:R.sup.2 is an organic substituent selected from the group consisting of alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkylalkylenes, haloalkyls, aryls, haloaryls and arylalkylenes, and their product by the process of:(a) reacting the 17.beta.-hydroxy group of 17.beta.-hydroxy-5.alpha.-estr-1-en-3-one with dihydropyran to produce the 3-keto-17.beta.-ether;(b) reducing the 3-keto-17.beta.-ether product of step (a) with lithium in ammonia;(c) reacting the product of step (b) with dialkyl chlorophosphate to produce the 3-substituted phosphate;(d) reducing the product of step (c) with lithium and ammonia to produce the .DELTA..sup.2 -protected-17.beta.-ether product;(e) hydrolysis of the produce of step (d) to product the .DELTA..sup.2 -17.beta.-hydroxy compound;(f) oxidizing the 17.beta.

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.