Abstract: The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular bleeding disorders and endometriosis.

Abstract: The invention provides amphiphilic compounds with hydrophobic and hydrophilic faces. The compounds can be readily prepared from steroids such as cholic acid or deoxycholic acid, which provide hydrophobic skeletons with structures similar to that of the lipid cholesterol. The compounds of the invention can be used to aid the solubilization, isolation, purification, stabilization, crystallization, and/or structural determination of membrane proteins, and to prepare micelles for delivery of a bioactive agent, such as a drug or a gene, to a subject.

Abstract: In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.

Abstract: Disclosed herein are methods of preparing a phosphorothioate nucleotide analog, which are useful in treating diseases and/or conditions such as viral infections.

Abstract: A method for treating or preventing spontaneous preterm birth in pregnant women and improving neonatal morbidity and mortality. The method includes administering to a pregnant woman in need thereof an effective amount of progesterone sufficient to prolong gestation by minimizing the shortening or effacing of her cervix. Treatment and prophylaxis with progesterone in pregnant women having symptoms of short cervix has been clinically shown to increase neonatal health.

Abstract: The invention provides 11?-hydroxyandrosta-4-ene-3-one compounds of Formula I, or physiologically acceptable salts or solvates thereof: wherein R4 represents a moiety selected from a group consisting of (A), (B) and (C), with a proviso that when R4 represents moiety (C), Z is S:

Abstract: The present invention relates to methods and compositions for increasing telomerase activity in cells. Such compositions include pharmaceutical formulations. The methods and compositions are useful for treating diseases subject to treatment by an increase in telomerase activity in cells or tissue of a patient. They are also useful for enhancing replicative capacity of cells in culture, as in ex vivo cell therapy and for enhancing proliferation of stem and progenitor cells.

Abstract: The present invention provides glycoside compounds, methods of preparing such compounds, pharmaceutical compositions comprising such compounds, and a method for the treatment of hyperproliferative diseases using the same.

Abstract: In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.

Abstract: In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.

Abstract: A method for treating or preventing spontaneous preterm birth in pregnant women and improving neonatal morbidity and mortality. The method includes administering to a pregnant woman in need thereof an effective amount of progesterone sufficient to prolong gestation by minimizing the shortening or effacing of her cervix. Treatment and prophylaxis with progesterone in pregnant women having symptoms of short cervix has been clinically shown to increase neonatal health.

Abstract: Polymorphic crystal forms of 3-methylthiophene-2-carboxylic acid (6S,9R,10S,11S,13S,16R, 17R)-9-chloro-6-fluoro-11-hydroxy-17-methoxycarbonyl-10,13,16-trimethyl-3-oxo-6,7,8,9,10, 11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl ester. The crystal forms possess anti-inflammatory activity and have very good stability. Methods for preparing the crystal forms are also described.

Abstract: The invention provides a diagnostics assay for measuring the responsiveness to a drug by comparing the protein levels of a gene that responds to the drug, such as a steroid, to the protein levels of a gene that does not respond to the drug. Methods according to the invention are useful for predicting the ability of a patient (or a tissue, body fluid or cell sample in vitro) to respond to a drug or steroid at any stage of their treatment (i.e., before, during or after), and to monitor the patient (or a tissue, body fluid or cell) over time to assess continued responsiveness to the drug or steroid.

Abstract: Disclosed herein is rocuronium bromide having a potentiometrical assay of from 99% to 101% in acetic acid and perchloric acid, having less than about 0.2% area by HPLC of 2?-(4-morpholinyl)-16?-(1-pyrrolidinyl)-5?-androstan-3?-ol-17?-acetate, and having at least one of the solvents ethyl ether and dichioromethane in an amount equal to or less than about 850 ppm, and 600 ppm, respectively.

Abstract: Acridinium-functionalized solid-phase supports and methods for making acridinium-functionalized solid-phase supports are disclosed. The acridinium-functionalized solid-phase supports comprise a solid phase support linked to a chemiluminescent substituted acridinium compound through a linker group covalently attached to the nitrogen atom of the acridinium nucleus and the solid phase support as exemplified in FIG. 1.

Abstract: The present invention provides compounds, compositions and methods that enhance the transfer of an agent into a cell. The agents can include polypeptides, polynucleotides such as genes and antisense nucleic acids, and other molecules. In some embodiments, the agents are modulating agents that can modulate a cellular activity or function when introduced into the cell. The compounds, compositions and methods are useful for introducing agents such as genes into individual cells, as well as cells that are present as a tissue or organ.

Abstract: Provided herein are assays for detecting enzyme activity using Raman Spectroscopy.

Abstract: There are provided compounds of formula (I) wherein R1 represents O, S or NH; R2 represents —C(?O)-aryl or —C(?O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the ? or ? configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and represents a single or a double bond; and salts and solvates thereof; process for preparing them, compositions containing them and their use in therapy.

Abstract: This invention relates to a sealed container containing a powder formulation comprising a dehydroepiandrosterone, its analogue(s) or salt(s) by itself or with a pharmaceutically or veterinarily acceptable carrier or diluent, and having a particle size of about 0.1 ?m to about 100 ?m. The formulation can be used to treat or prevent asthma, chronic obstructive pulmonary disease, lung inflammation, and other respiratory diseases or conditions. The formulation may be prepared by jet milling, and may be delivered through the respiratory tract or other routes using a nebulizer. The sealed container is provided in a device and/or a therapeutic kit.

Abstract: The present invention relates to a method for preparation of organofluoro compounds containing radioactive isotope fluorine-18. More particularly, the present invention relates to a method for preparation of organofluoro compound by reacting fluorine salt containing radioactive isotope fluorine-18 with alkyl halide or alkyl sulfonate in the presence of alcohol of Chemistry (FIG. 1) as a solvent to obtain high yield of organofluoro compound. Synthesis reaction according to the present invention may be carried out under mild condition to give high yield of the organofluoro compounds and the reaction time is decreased, and thereby is suitable for the mass production of the organofluoro compounds.

Abstract: A method for preparing organic nanotubules in an aqueous medium including preparing a basic solution with a pH from 10 to 14, adding an organic compound of the formula: wherein R1 is a C17-C20 polycyclic radical with fused rings optionally including alkyl substituents, R2 is a C3-C20 linear or branched alkylene group, and R3 represents a hydrogen atom, a C1-C20 alkyl or C6-C30 aromatic group, and submitting the solution to stirring for sufficient time in order to form stable tubules of the organic compound in the solution; and nanotubules prepared by the method.

Abstract: A compound of formula wherein R has various meanings and its use as a pharmaceutical.

Abstract: The present invention relates to useful diterpenes and pharmaceutical compositions containing them of the formula: for use in the treatment of cardiovascular and inflammatory diseases and for cancers susceptible to an NF-?B inhibitor and an endothelin receptor inhibitor. The present invention also relates to compounds and methods useful to inhibit cell proliferation and for the induction of apoptosis.

Abstract: Disclosed herein is a paroxetine cholate or cholic acid derivative salt and a composition comprising paroxetine and cholic acid or a derivative thereof. Further disclosed is a pharmaceutical composition comprising the paroxetine salt or the composition. The pharmaceutical composition can be formulated into an oral preparation for swallowing without water as an orally disintegrating tablet for paroxetine.

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: Compounds of formula (I), where R is a monovalent cyclic organic group having from 3 to 15 atoms in the ring system, useful as pharmaceuticals

Abstract: Compounds having an ansamycin anitibiotic, or other moiety which binds to hsp90, coupled to a targeting moiety which binds specifically to a protein, receptor or marker can provide effective targeted delivery of the ansamycin antibiotic leading to the degradation of proteins and death of the targeted cells. These compositions may have different specificity than the ansamycin alone, allowing for a more specific targeting of the therapy, and can be effective in instances where the ansamycin alone has no effect. Thus, these compounds provide an entirely new class of targeted chemotherapy agents with application, depending on the nature of the targeting moiety, to treatment of a variety of different forms of cancer. Such agents can further be used to promote selective degradation of proteins associated with the pathogenesis of others diseases, including antigens associated with autoimmune disorders and pathogenic proteins associated with Alzheimer's disease.

Abstract: Methods for modulating amyloid deposition in a subject are described. An effective amount of at least one ATP binding cassette (ABC) transporter blocker is administered to a subject, such that modulation of amyloid deposition occurs. Methods also include administering and effective amount of at least one ABC transporter blocker, or a pharmaceutically acceptable salt thereof, to a subject such that a disease state associated with amyloidosis is treated. Packaged pharmaceutical compositions for treating amyloidosis are described. The package includes a container for holding an effective amount of a pharmaceutical composition and instructions for using the pharmaceutical composition for treatment of amyloidosis. The pharmaceutical composition includes at least one ABC blocker for modulating amyloid deposition in a subject. Methods for identifying agents which modulate amyloid deposition in a subject are also described.

Abstract: Novel compounds having a formula selected from the group consisting of wherein the substituents are defined as in the specification which are intermediates for the production of vinyl compounds having a remarkable anti-estrogenic and anti-proliferative activity.

Abstract: Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I 1

Abstract: A method of decreasing atherosclerosis and its complications involving administering to a human or animal various combinations of medications with Finasteride, Bicalutamide, Flutamide and Nilutamide.

Abstract: In a process for recovering medicinal substances or active substances from preparations, their initial products or waste, a flat-shaped starting material in the form of a film with adhesive and an active substance-containing material is provided with one edge length of from 0.1 to 5 cm and a second edge length of 50 cm. A starting material having an active substance is placed in an aqueous extraction liquor. The extraction liquor then takes effect until the active substance is dissolved in the aqueous extraction liquor forming an active substance-containing solution. The active substance is isolated from the active substance-containing solution be means of precipitation.

Abstract: A novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone is provided having relatively high physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form L eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form L eplerenone and for preparing compositions comprising Form L eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.

Abstract: Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I 1

Abstract: The instant invention involves a process for oxidizing compounds containing an allylic group, i.e. those containing an allylic hydrogen or allylic alcohol group, to the corresponding enones, using a ruthenium-based catalyst in the presence of a hydroperoxide. Particularly, &Dgr;-5-steroidal alkenes can be oxidized to the corresponding &Dgr;-5-7-keto alkenes.

Abstract: A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.

Abstract: The protective group having the following formula (I): Ar—L—  (I) wherein Ar represents a substantially planar, fused ring system containing at least 4 aromatic rings, and L represents a group containing at least one carbon atom which is capable of bonding to a group to be protected.

Abstract: Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of 1

Abstract: Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I 1

Abstract: Androgen synthesis inhibitors, as well as methods for the use of the same to reduce plasma levels of testosterone and/or dyhydrotestosterone, and to treat prostate cancer and benign prostatic hypertrophy, are disclosed.

Abstract: This invention provides a method of increasing the level of estrogen receptors in the neural tissue of a subject which comprises administering to the subject estrogen in an amount effective to increase the level of neurotrophin receptors and a neurotrophin in an amount effective to increase the level of estrogen receptors, so as to thereby increase the level of estrogen receptors. This invention also provides a method of increasing the level of estrogen receptors in a sample of neural tissue from a subject which comprises contacting the sample with estrogen in an amount effective to increase the level of neurotrophin receptors and neurotrophin in an amount effective to increase the level of estrogen receptors, so as to thereby increase the level of estrogen receptors. Lastly, this invention provides a method of preventing the onset of Alzheimer's disease.

Abstract: Estradiol facilitates non-viral gene delivery to breast tumor cells. The effect is dose dependent, and is independent of the gene construct, temperature, and tumor cell line. Thus, compositions and treatment regimens that use estradiol, or other estrogen pharmacologic agents, in combination with genes of interest can be used to provide targeted delivery and expression of genetic products in target cells and tissues of estrogen, such as breast cells. The compositions and treatment regimens have particular application to the enhanced delivery of genetic constructs useful in killing breast tumor cells and preventing tumor recurrence.

Abstract: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.

Abstract: In a process for reprocessing devices for the transdermal application of active substances or their process waste, active substance-containing components are brought into solution and the active substances are recovered therefrom.

Abstract: The protective group having the following formula (I):Ar--L-- (I)whereinAr represents a substantially planar, fused ring system containing at least 4 aromatic rings, andL represents a group containing at least one carbon atom which is capable of bonding to a group to be protected.

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: As a novel digoxigenin derivative which makes the labeling procedure simple, can be used to label a naturally-occurring nucleic acid, and enables highly sensitive assay, carbodiimide group-containing digoxigenin derivative represented by the following formula is used as the label in a nucleic acid detection method or immunoassay.

Abstract: 17-Deoxycorticoid-21-carboxylic 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 and R(2) is H or methyl. They are obtained by reacting a compound of the formula II, ##STR2## in which R(4) is OH, with an activated carboxylic acid of the formula III,R(5)-CO--X-R(1) III.The compounds I possess very strong local and topical antiinflammatory activity and exhibit a very good ratio of local to systemic antiinflammatory effect, which ratio is often clearly superior to that of structurally related corticoid 21-esters which do not carry any aryl or hetaryl group in the 21-ester residue or to that of analogous 17-deoxycorticoids having an unesterified, that is a free, 21-hydroxyl group.

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: The preparation of a novel crystalline cefaclor and the conversion of such a product to cefaclor monohydrate are described. The new intermediate cefaclor is a particular crystalline form and possesses the same antibiotic properties as cefaclor monohydrate.