Abstract: A process for preparing a bioabsorbable sheet preparation holding thrombin is provided. A process for preparing a bioabsorbable sheet preparation holding thrombin which comprises immersing a bioabsorbable sheet consisting of polyglycolic acid in a thrombin solution containing thrombin as an active ingredient, glycerol as a softening agent, Tween 80 as a permeating agent, and optionally histidine and trehalose as a stabilizing agent followed by drying to hold thrombin on said bioabsorbable sheet, and a bioabsorbable sheet preparation holding thrombin prepared by said process.

Abstract: The present invention provides compositions comprising the ligand binding domain (LBD) of a farnesoid X receptor (FXR) in crystalline form. In alternative embodiments, the LBD of FXR is complexed with a ligand therefor. There are provided high resolution structures of FXR complexed with a novel high affinity agonist fexaramine. The discovered structure of a FXR LBD provides the first three-dimensional view of the structural basis for FXR ligand binding. The present invention further provides a computer for producing a time-dimensional representation of FXR or a complex thereof, and a computer for determining at least a portion of the structure coordinates of FXR or a complex thereof. The present invention further provides methods of using this structural information to predict molecules capable of binding to FXR; to identify compounds with agonist, antagonist or partial agonist activity for FXR; and to determine whether a test compound is capable of binding to the LBD of FXR.

Abstract: The present invention relates to the use of nor-bile acids and their pharmaceutically acceptable salts, esters and/or derivatives in the treatment arteriosclerosis.

Abstract: An object of the present invention is to provide a liquid composition wherein minoxidil can be dissolved at a relatively high concentration (the saturating amount or above), stimulation of skin and stickiness is suppressed without containing an organic solvent, and excellent effects of percutaneous absorption is achieved. The present invention provides a liquid composition comprising (i) minoxidil, (ii) bile acid or a salt thereof, and (iii) an aqueous medium in an amount of 30% by weight or more of the weight of the composition.

Abstract: Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.

Abstract: The invention relates to compounds of Formula A: or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, liver disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.

Abstract: Synthetic methods for preparing deoxycholic acid and intermediates thereof are provided.

Abstract: It is an object of the present invention to provide a novel method for producing a steroid compound. The present invention provides a method for producing 5?-3,7-dioxocholanic acid or an ester derivative thereof, using, as a raw material, a sterol having double bonds at position 5 and at position 24, such as cholesta-5,7,24-trien-3?-ol, ergosta-5,7,24(28)-trien-3?-ol, desmosterol, fucosterol, or ergosta-5,24(28)-dien-3?-ol, via the following 4 steps: (I) a step involving oxidation of a hydroxyl group at position 3 and isomerization of a double bond at position 5 to position 4; (II) a step involving the oxidative cleavage of a side chain to convert position 24 to a carboxyl group or an ester derivative thereof; (III) a step of introducing an oxygen functional group into position 7; and (IV) a step of constructing a 5? configuration by reductive saturation of a double bond at position 4.

Abstract: The invention relates to 17?-(5-hydroxy-C5-hydrocarbyl)-1,3,5(10)-estratrien-3,17?-diol derivatives having cicatrising activity, preferably for topical use on wounds, without significant systemic effects, and to pharmaceutical compositions containing them. In particular, the invention relates to estradiol 17?-(5-hydroxypentyn-1-yl)derivatives and 3-esters, 5?-esters and 3,5?-diesters thereof and to a process for the preparation thereof by reaction of 3-OR-protected estrone with an alkali metal derivative of OR-protected 5-pentynol, followed by 3-, 5-? or 3,5?-esterification.

Abstract: The use of mesoprogestins as pharmaceutical components for the manufacture of a medicament for hormone replacement therapy (HRT) and as components for the combined use together with an estrogen for the manufacture of a medicament for HRT as well as in respective HRT-methods and methods of treating hormone deficiency and hormone irregularity symptoms. Mesoprogestins are defined as compounds possessing both agonistic and antagonistic activities at the progesterone receptor (PR) in vivo. They stabilize the function of PR at an intermediate level of agonistic and antagonistic. Corresponding functional states cannot be achieved with progestins or antiprogestins. J867, J912, J956 and J1042 are the mesoprogestins preferred herein.

Abstract: Synthetic methods for preparing deoxycholic acid and intermediates thereof are provided.

Abstract: The present invention refers to new organic molecules, derived from the class of polycarbocycle derivatives, and their application as components of photoresists, and in particular as components of photoresist compositions where no polymer is comprised as one of the photoresists components. In these photoresist formulations the new molecule(s) is/are the main component(s) (i.e. percentage higher than 50% w/w).

Abstract: The present invention relates to the use of nor-ursodeoxycholic acid for the manufacture of a drug for the treatment and/or the prevention of liver diseases, preferably chronic liver diseases.

Abstract: In the formation of a fine pattern using a photolithography process, a dissolution promoter which can increase the difference of solubility between exposed region and unexposed region, and a photoresist composition including the same are disclosed. The dissolution promoter has the structure of the following formula (wherein, R is a hydrocarbon group of 1 to 40 carbon atoms, A is an alkyl group of 1 to 10 carbon atoms, p is 0 or 1, and q is an integer of 1 to 20). Moreover, the photoresist composition comprises 3 to 30 wt % (weight %) of the photosensitive compound; 1 to 30 weight parts of a dissolution promoter represented by the formula, with respect to 100 weight parts of the photosensitive compound; 0.05 to weight parts of a photo-acid generator with respect to 100 weight parts of the photosensitive compound; and a remaining organic solvent.

Abstract: A novel, improved method of synthesizing alkylated bile acid derivatives is provided. Such derivatives include, but are not limited to the active, potent, and selective FXR receptor agonist such as 6-ECDCA and other CA, DCA and CDCA derivatives. The first step of the synthesis selectively oxidates CDCA, CD, or DCA related starting material. An efficient combined deprotonation, trapping, ethylation, deprotection and reduction system is used to produce the desired alkylated bile acid derivatives. This practical synthesis offers a simple and economical pathway suitable for a large-scale manufacturing of alkylated bile acid derivatives including, but not limited to, 6-ECDCA.

Abstract: The present invention relates to a process for the preparation of 17?-(3-hydroxypropyl)-17?-hydroxysteroids of the formula I starting from 17-ketosteroids of the formula III via the intermediates of the formula V wherein the radicals R3, R5, R6, R7, R10, R13, R15, R16, R40, R41 and R42 have the meaning indicated in the description.

Abstract: Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.

Abstract: Process for preparing 3?-7?(?)-di-hydroxy-6?(?)-alkyl-5?-cholanic acid (I) in which R is a linear or branched C1-C5 alkyl and the relative intermediates 3?-hydroxy-6?-alkyl-7-keto-5?-cholanic (VIII) and 3?-hydroxy-6?-alkyl-7-keto-5?-cholanic (IX).

Abstract: The present invention involves intermediates, including a 7?-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent.

Abstract: The present invention involves intermediates, including a 7?-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent.

Abstract: The present invention relates to compounds of formula (I): wherein R is hydrogen or alpha-hydroxy, the hydroxyl group in position 7 is in the alpha or beta position; and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof.

Abstract: The present invention comprises the design, synthesis and development of a new class of chemotherapeutic agents for prophylactic and therapeutic treatments in a mammal, particularly a human, believed to be at risk of suffering from a hormone-responsive disorder. In an aspect of the invention, such treatments include therapeutic compositions comprising novel steroidal antiestrogen and antiandrogen compounds. In a preferred aspect, such a novel compound of the present invention has an address and a message component, which are made into a single composite entity for more aggressive intervention and effective treatment of hormone-responsive disorders, thereby prolonging the disease-free interval for the patient and reducing a number of side effects.

Abstract: 7?-Hydroxy-pregn-4-en-3-one-20-carbaldehyde, a production method thereof and a method for producing 7?,21 -dihydroxy-20-methyl-pregn-4-en-3-one, which is useful as a synthetic intermediate for pharmaceuticals such as squalamine and the like, efficiently at high purity from the carbaldehyde.

Abstract: The invention describes new compounds as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action on bone rather than the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The new compounds are 16?- and 16?-hydroxy-estra-1,3,5(10)-estratrienes, which carry additional substituents on the steroid skeleton and can have one or more additional double bonds in the B-, C- and/or D-rings.

Abstract: This invention relates to methods for treating asthma or allergy in a mammal by administering a 3-aminosteroid compound to a mammal in need thereof. The 3-aminosteroid compound being capable of down regulating the IL-9 pathway and alleviating asthmatic responses to allergen. Exemplary 3-aminosteroid compounds used in the methods of the invention include compounds having the chemical formula (I), wherein X, R1, R2, R3, and R4 groups are as defined herein. The invention also relates to certain novel compounds of formula (I). Moreover, the invention also provides methods for identifying an immunomodulatory 3-aminosteroid compound.

Abstract: A conjugated prodrug of an estradiol compound conjugated to a biological activity modifying agent.

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: Compounds of formula (I) in which: R1 represents a hydrogen atom or an O-protecting group; R2 represents a hydroxyl, lower alkoxy, carboxaldehyde, lower alk-1-enyl or hydroxy- or lower alkoxy-substituted lower alkyl group; R3 represents a methyl group having ?- or ?-configuration; X represents a C1-3 alkylene group or a valence bond; Y represents a carboxaldehyde group or a group of formula —C(R4)(R5)OR1 where R1 is as defined above and R4 and R5, which may be the same or different, are each selected from hydrogen atoms, alkyl, alkenyl and alkynyl groups such that the total carbon content of R4 and R5 does not exceed three atoms, with the proviso that X is a valence bond when both R4 and R5 are other than hydrogen; and the dotted line signifies that a double bond may optionally be present at the 16(17)-position exhibit potent cell modulating activity, including antiproliferative and antiangiogenic effects.

Abstract: The present invention provides a novel (meth)acrylic acid ester compound useful as a resin material for photosensitive compositions, which enables control of the molecular weight of a resin to be prepared. The novel (meth)acrylic acid ester compound is one represented by the following formula (I): wherein R1 and R2 each independently represent a hydrogen atom or a hydroxyl group; and R3 represents a hydrogen atom or a methyl group.

Abstract: A linear actuator monitors and distinguishes between the open and closed states of a valve. The states of the actuator are monitored electrically by two switches and visually via a mechanical indicator. The electrical switches are initialized by an adjustable system, according to the random position of the valve stem when it is opened or closed. The visual indicator is also adjusted to an initial position corresponding to the valve stem position. The adjustment of the system allows for flexibility and use on a wide range of valve stems with various stroke lengths. The visual indicator is visible from the top and the sides of the unit. It is visible on the circumference of the unit so that it is visible at an angle as well. The visual indicator matches three possible states of the valve as follows: when the valve is closed, the indicator is not visible, when the valve is either opening or closing, only one indication area is visible, and when the valve is fully open, two indication areas are visible.

Abstract: Disclosed is a photographic element comprising a light-sensitive silver halide emulsion layer having associated therewith a phenolic “NB magenta coupler” having the formula: wherein: the term “NB magenta coupler” represents a coupler of formula (I) that forms a magenta dye with the developer 4-amino-3-methyl-N-ethyl-N-(2-methanesulfonamidoethyl) aniline sesquisulfate hydrate for which the maximum absorption of the dye upon spin coating is in the range of from 520 to 590 nm and the left bandwidth (LBW) or the right bandwidth (RBW) using spin-coating, is at least 5 nm less than that of the same dye in solution form; R1 is a heterocyclic, carbocyclic, or alkenyl group with substituents of sufficient electron withdrawing capacity to obtain a spin-coated dye as described in the preceding subparagraph that exhibits a maximum absorption in the range of 520-590 nm; Y is H or a coupling-off group; each Z* is an independently selected substituent group where p is independen

Abstract: The present invention comprises the design, synthesis and development of a new class of chemotherapeutic agents for prophylactic and therapeutic treatments in a mammal, particularly a human, believed to be at risk of suffering from a hormone-responsive disorde. In an embodiment of the invention, such treatments include therapeutic compositions comprising novel steroidal antiestrogen and antiandrogen compounds. In a preferred embodiment, such a novel compound of the present invention has an address and a message component, which are made into a single composite entity for more aggressive intervention and effective treatment of hormone-responsive disorders, thereby prolonging the disease-free interval for the patient and reducing a number of side effects.

Abstract: Steroid derivatives of this invention interact with nuclear liver X receptor (LXR) and ubiquitous receptor (UR) and can be used to treat a variety of LXR- or UR-mediated disorders.

Abstract: Novel 9&agr;-hydroxy steroid compounds, including compounds of Formula IX wherein —A—A—, —B—B—, R1, R3, R8 and R9 are as defined in the specification.

Abstract: Compounds of formula (I) in which: R1 represents a hydrogen atom or an O-protecting group; R2 represents a hydroxyl, lower alkoxy, carboxaldehyde, lower alk-1-enyl or hydroxy- or lower alkoxy-substituted lower alkyl group; R3 represents a methyl group having &agr;- or &bgr;-configuration; X represents a C1-3 alkylene group or a valence bond; Y represents a carboxaldehyde group or a group of formula —C(R4)(R5)OR1 where R1 is as defined above and R4 and R5, which may be the same or different, are each selected from hydrogen atoms, alkyl, alkenyl and alkynyl groups such that the total carbon content of R4 and R5 does not exceed three atoms, with the proviso that X is a valence bond when both R4 and R5 are other than hydrogen; and the dotted line signifies that a double bond may optionally be present at the 16(17)-position exhibit potent cell modulating activity, including antiproliferative and antiangiogenic effects.

Abstract: Analysis of full-blood glucose, serum insulin, serum triglycerides and total serum cholesterol were performed. Glucose levels in blood samples from the oral glucose tolerance test were used for calculation of the incremental Area Under the Curve (AUC0-120 min−baseline). All data are expressed as percentage change of vehicle treated animals (cf. FIGS. 1 and 2).

Abstract: A fuel pellet is produced by the combination of organic waste material with a binder obtained by direct liquefaction and/or fast pyrolysis of biomass material. Direct liquefaction and fast pyrolysis are carried out according to known liquefaction processes. The liquefied bio-binder base is mixed with additives, if desired, such as petroleum asphalt and cross-linking agents, in order to modify its characteristics to meet specific needs of particular applications, and the resulting mixture is mixed with organic-waste material preheated to 100° C. or more and allowed to react at about 150-200° C. Combustible extenders and fillers, reinforcing fibers, and cross-linking agents may be mixed with the organic material or the bio-binder base to provide additional specific properties to the mixture. The resulting well mixed mass is then pelletized or otherwise molded in conventional equipment.

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

Abstract: Substituted acylguanidines and their pharmaceutically tolerable salts and physiologically functional derivatives. Compounds of the formula I in which the radicals have the meanings indicated, and their physiologically tolerable salts, physiologically functional derivatives and a process for their preparation are described. The compounds are suitable, for example, as medicaments for the prophylaxis or treatment of gallstones.

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 19-nor 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 relates to bile acid or bile salt fatty acid conjugates (hereinafter called “BAFAC), to their use in dissolving cholesterol gallstones in bile, preventing their occurrence or recurrence, to their use in reducing or preventing arteriosclerosis and to methods for the treatment of said diseases. The conjugates are of the formula W—X—G in which G is a bile acid or bile salt radical, W stands for one or two fatty acid radical(s) having 18-22 carbon atoms and X stands for a NH bond between said bile acid or bile salt radical and the fatty acid radical(s). The conjugation is advantageously performed at a position selected among the 3, 6, 7, 12 and 24 positions of the bile acid or bile salt nucleus.

Abstract: Thiol esters of S-substituted 11&bgr;-benzaldoxime-estra-4,9-dien-carboxylic acids of the formula I their pharmaceutically acceptable salts, a method for their synthesis and pharmaceutical preparations containing these compounds are described. These compounds bind to progesterone receptors and have distinctly reduced anti-glucocorticoid action.

Abstract: A compound having the general formula: 1

Abstract: The present invention provides an additive for a photoresist composition for a resist flow process. A compound of following Formula 1 having low glass transition temperature is added to a photoresist composition containing a polymer which is not suitable for the resist flow process due to its high glass transition temperature, thus improving a flow property of the photoresist composition. As a result, the photoresist composition comprising an additive of Formula 1 can be used for the resist flow process.

Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: 1

Abstract: This invention relates to novel carboxylic acid derivatives represented by the following formula I and their synthesis: wherein, R1 is an hydrogen atom, an alkyl group or an alkoxy group of 1 to 20 carbon atoms in a linear, branched or cyclic form; R2 is a carboxy group of 1 to 40 carbon atoms in a linear, branched or cyclic form which is unsubstituted, or substituted into a hydroxy group, an ester group and an ether group. The novel carboxylic acid derivatives are more easily decomposed by acid than t-butyl ester compounds but are not dissolved in basic aqueous solution. According to this invention, carboxylic acid is under condensation with halogen compounds designed to prepare a larger monomolecular compound compared to the conventional method. Further, the condensed site is easily decomposed by acid but is extremely insoluble by basic aqueous solution.

Abstract: Multiple reaction schemes, process steps and intermediates are provided for the synthesis of epoxymexrenone, useful as a diuretic, and other compounds of Formula I wherein the variables are as defined by the specification.

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: 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: Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) wherein r1 is an optional double bond, R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen and lower alky, or together form a cyclic substituent (II) ##STR1## wherein Q is NH, O or CH.sub.2, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.