Abstract: The invention relates to 17&agr;-alkyl-17&bgr;-oxy-estra-1,3,5(10)-trienes that have an antiestrogenic action with general formula I. In addition, the invention also relates to 17-oxo-estra-1,3,5(10)-trienes as well as 17&bgr;-hydroxy-estra-1,3,5(10)-trienes as intermediate products in the production of the estratrienes according to the invention. The invention also relates to the use of 17&agr;-alkyl-17&bgr;-oxy-estratrienes for the production of pharmaceutical agents as well as pharmaceutical preparations that contain at least one 17&agr;-alkyl-17&bgr;-oxy-estratriene as well as at least one pharmaceutically compatible vehicle.

Abstract: A composition and method of preventing or inhibiting tumor growth and, more particularly, of treating a malignant tumor, using prodrugs of plant-derived compounds and derivatives is disclosed. In the method, a composition containing betulinic acid or a betulinic acid derivative is administered in a prodrug form to release betulinic acid or a betulinic acid derivative in vivo at the tumor site.

Abstract: A substituted 3-phenyl-5-alkoxy-3H-(1,3,4)-oxadiazol-2-one, compound of formula 1, 1

Abstract: The present invention provides hybrid molecules and methods of synthesizing such hybrid molecules from a cholinergic agent and a bile acid. The hybrid molecules function as cholinergic agents and may be either cholinergic agonists or cholinergic antagonists. Further disclosed herein are compositions comprising hybrid cholinergic agents and methods of making such compositions. Methods of treating a patient having a cholinergic disorder are also disclosed.

Abstract: The present invention provides hybrid molecules and methods of synthesizing such hybrid molecules from a cholinergic agent and a bile acid. The hybrid molecules function as cholinergic agents and may be either cholinergic agonists or cholinergic antagonists. Further disclosed herein are compositions comprising hybrid cholinergic agents and methods of making such compositions. Methods of treating a patient having a cholinergic disorder are also disclosed.

Abstract: This invention describes the new 8&bgr;-substituted estratrienes of general formula I in which R2, R3, R6, R6′, R7, R7′, R9, R11, R11′, R12, R14, R15, R15′, R16, R16′, R17 and R17′ have the meanings that are indicated in the description, and R8 means a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.

Abstract: The present invention is directed to a compound, method and composition of treating or preventing viral infections, in particular, human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infections, in human patients or other animal hosts, comprising the administration of N4-acylcytosine-1,3-dioxolane and pharmaceutically acceptable salts, prodrugs, and other derivatives thereof.

Abstract: A method and composition for the treatment, prevention and/or prophylaxis of a host, and in particular, a human, infected with Epstein-Barr virus (EBV), is provided that includes administering an effective amount of a 5-substituted uracil nucleoside or its pharmaceutically acceptable salt or prodrug, optionally in a pharmaceutically acceptable diluent or excipient.

Abstract: This invention relates to 11&bgr;-(para-substituted)phenyl-estra-1,3,5(10)-trienes with a straight-chin or branched-chain, optionally partially or completely halogenated alkyl radical or alkenyl radical in each case with up to 5 carbon atoms, an ethinyl radical or prop-1-inyl radical in 8&bgr;-position.

Abstract: Cardiovascular disease, including preeclampsia in pregnant women and hypertension in both women and men, are prevented or treated by administering thereto prostacyclin or a prostacyclin analog in combination with one or both of an estrogen and a progestin, which combination is also useful for HRT in peri- and post-menopausal women.

Abstract: A method of enhancing hair growth or treating alopecia in a subject uses topically administered estrogen receptor antagonists. Pharmaceutical formulations comprising estrogen receptor antagonists are described.

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: Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.

Abstract: The invention concerns new vitamin D derivatives of general formula (I) a process for their production, their use for production of medicaments, and intermediate products used in the process.

Abstract: New steroids and amides of formula I are described, in which the variables are defined by the description. Relative to the basic hydroxy compounds (“initial compounds”), the new compounds are distinguished by a considerably improved solubility and partially also by increased biological action and selectivity. The new compounds are suitable for the production of pharmaceutical agents.

Abstract: This invention describes the new 17&agr;-fluoroalkyl steroids of general formula I 1

Abstract: The invention is drawn to particles for oral drug delivery produced by spray-drying a dilute solution of a poorly soluble agent. The particles comprise regions of poorly soluble agent wherein the dissolution rate enhancement is between about 2-fold and about 25-fold compared to the agent in bulk form.

Abstract: Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across the intestinal wall after oral administration to provide for enhanced therapeutic, and optionally prolonged therapeutic, systemic blood concentrations of the drugs upon oral administration of the drug-compound conjugate. Also disclosed are pharmaceutical compositions containing and methods of using such compounds.

Abstract: Described is a deliverable composition with low toxicity comprising an amphipathic compound, a polycation, and a siRNA. The composition may be used in the process of delivering a siRNA to an animal cell or more particularly, a mammal cell.

Abstract: The invention relates to new C13-substituted estra-1,3,5(10)-trien-3-yl sulfamates of general formula I, wherein R1 represents an acyl residue, oxycarbonyl residue, aminocarbonyl residue, sulfonyl residue, or aminosulfonyl residue, and R15 represents ethyl, methods of preparing same, and pharmaceutical compositions containing these compounds. The compounds of the invention of general formula I inhibit the activity of steroid sulfatase (EC 3.1.6.2) and do not exhibit any estrogenic effect.

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: The invention provides steroidal alkaloids for inhibiting or reversing multidrug resistance in cancer or in bacterial, fungal or parasitic infections. The steroidal alkaloid may be administered to the patient alone or in combination with an anticancer, antibacterial, antifungal or antiparasitic agent. Examples of steroidal alkaloids include members of the solanidane or spirosolane e.g. tomatidine, families, and C-nor-D-homo steroid such as of the jervane or veratramine families.

Abstract: The invention concerns pharmaceutical preparations containing estra-1,3,5(10)-triene derivatives as active ingredients which carry a group of the general formula R—SO2—O— at their C3 position wherein R is a R1R2N group wherein R1 and R2 are independent of each other and represent a hydrogen atom, a C1-C5 alkyl radical or, together with the N atom, a polymethylene imino radical containing 4 to 6 C atoms, or a morpholino radical. The preparations according to the invention can be used for hormonal contraception and for hormon replacement therapy (HRT). They exhibit a low hepatic estrogenity.

Abstract: The application discloses novel 2-alkoxyestradiol analogs which exhibit anti-proliferative properties, and methods of making and using such compounds to inhibit undesired cell proliferation and tumor growth. Additionally, methods are disclosed of treating diseases associated with undesired angiogenesis and undesired proliferation, and methods of treating infectious disease wherein the infectious agent is particularly susceptible to inhibition by agents that disrupt microtubule organization and function.

Abstract: There is provided according to the invention a pharmaceutical formulation comprising an aqueous carrier liquid having dissolved therein (a) an ester of fluticasone or a solvate thereof as medicament and (b) a solubilising agent for assisting the solubilisation of the medicament in the aqueous carrier liquid.

Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.

Abstract: Compounds of the formula Where the substituents are defined in the application.

Abstract: 7-Oxo-DHEA derivatives, various of which are themselves novel compounds, are well suited for cosmetically/therapeutically treating adverse conditions/afflictions of a keratinous substrate/material, notably of human skin, hair, eyelashes and nails, to improve the appearance thereof, in particular to prevent or treat signs of aging of the skin and/or a dull complexion and/or skin or hair pigmentation disorders and/or dryness of the skin and/or hyperseborrhoea and/or hyperseborrhoea-related imperfections and/or sensitive skin and/or dandruff and/or natural hair loss and/or baldness.

Abstract: The present invention provides a novel pharmaceutical composition based on the use of a particular oil phase which comprises a lipophilic, pharmaceutically active agent, a mixture of diglyceride and monoglyceride in a ratio of from about 9:1 to about 6:4 by weight (diglyceride:monoglyceride) wherein the diglyceride and monoglyceride are mono- or di-unsaturated fatty acid esters of glycerol having sixteen to twenty-two carbon chain length, one or more pharmaceutically acceptable solvents, and one or more pharmaceutically acceptable surfactants. The composition is in a form of self-emulsifying formulation which provides high concentration and high oral bioavailability for lipophilic compounds.

Abstract: The present invention discloses dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds of the present invention may contain either a mixture of Type 1 and Type 2 agents or a single entity that integrates both units in the same molecules. The compounds are designed to produce both Type 1 and Type 2 phototherapeutic effect at once using dual wavelength light source that will produce singlet oxygen and free radicals at the lesion of interest.

Abstract: A process for the preparation of a compound of the formula 1

Abstract: A pharmaceutically active inventive compound comprises two independently active analgesic moieties covalently conjoined through a physiologically labile linker. A preferred embodiment comprises an opioid, such as morphine, covalently linked to at least one analgesic compound selected from the group consisting of an opioid or a non-opioid compound through a physiologically labile linker. Suitable covalent linkers are covalently bonded to the two independently active analgesic compounds through one or more lactone, lactam, or sulfonamido linkages. Suitable linkers include endogenous carboxylate, amido, and sulfonamido moieties, and exogenous moieties that form the aforementioned lactone, lactam or sulfonamido linkages.

Abstract: The present invention provides a highly sensitive immunoassay system for estrogens, which utilizes as a labeled compound a biotinylated estradiol derivative of the formula (1) wherein one of R1 and R2 is hydrogen and the other is a group represented by wherein R3s are the same or different and represent an arginine residue or a lysine residue, x is 0 or 1, y is an integer from 1 to 5, and z is an integer from 1 to 3.

Abstract: The invention concerns compounds of formula (I) wherein: X, Y, R1, R2, Z, G are as defined in the description, the methods for preparing them and the intermediates in said method, their use as medicine and the pharmaceutical compositions containing them.

Abstract: The present invention provides hybrid molecules and methods of synthesizing such hybrid molecules from a cholinergic agent and a bile acid. The hybrid molecules function as cholinergic agents and may be either cholinergic agonists or cholinergic antagonists. Further disclosed herein are compositions comprising hybrid cholinergic agents and methods of making such compositions. Methods of treating a patient having a cholinergic disorder are also disclosed.

Abstract: The present invention provides hybrid molecules and methods of synthesizing such hybrid molecules from a cholinergic agent and a bile acid. The hybrid molecules function as cholinergic agents and may be either cholinergic agonists or cholinergic antagonists. Further disclosed herein are compositions comprising hybrid cholinergic agents and methods of making such compositions. Methods of treating a patient having a cholinergic disorder are also disclosed.

Abstract: Compounds of formula for treating osteoporosis with minimal estrogenic activity are disclosed.

Abstract: A compound selected from the group consisting of the compounds of the formula wherein the substituents are defined as in the specification and their addition salts with non-toxic, pharmaceutically acceptable acids and bases having estrogenic activity at the bone level but little or no endometrial hyperplasia activity nor any activity for proliferation of mammary tumors.

Abstract: A subject of the invention is the compounds of formula (I): in which X is a halogen atom, D represents the remainder of an optionally substituted pentagonal or hexagonal ring and optionally carrying an unsaturation, R1, R2, R3, R4, Y and n are as defined in the description, their preparation process and intermediates, their use as medicaments and the compositions containing them.

Abstract: An anti-cancer substance has a porphyrin-like molecule conjugated to an anti-cancer drug. In one embodiment, the porphyrin-like molecule is conjugated directly to an anti-cancer drug. In a second embodiment, the porphyrin-like molecule is conjugated to a first end of a peptide chain, while a second end of the peptide chain is conjugated to the anti-cancer drug. The peptide chain is designed to be cleaved under physiological conditions surrounding the tumor. In the preferred embodiment, the peptide chain functions as a protease inhibitor once it has been cleaved.

Abstract: Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.

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: Treatment of androgen deficiency using a pharmaceutically effective dose of ethisterone or an ethisterone derivative such as danazol. In particular, androgen deficiency in the aging male, also known as the male climateric andropause or the male menopause, can be treated by ethisterone or ethisterone derivatives. Treatment of hypogonadism using ethisterone or ethisterone derivative in combination with testosterone is also effective.

Abstract: Compositions and methods for enhancing paracellular permeability at an absorption site in a subject are disclosed. The method includes: (a) administering an effective amount of a phospholipase C inhibitor to a subject at a time in which enhanced paracellular permeability is desired; and (b) enhancing paracellular permeability in the subject at the absorption site through the administering of the effective amount of the phospholipase C inhibitor. The disclosed compositions and methods provide enhanced absorption of a hydrophilic drug in a subject.

Abstract: New non-estrogenic derivative compounds of estradiol, which have no estrogenic activity and comparatively high anti-oxidative activity, are disclosed. These new non-estrogenic derivative compounds are potentially useful as non-estrogenic antioxidants, especially for administration in post-menopausal women and in men. The compounds of the invention can also inhibit aromatase and sulfatase.

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: Corticoid 17,21-dicarboxylic esters and corticosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compounds

Abstract: An androgenic steroid compound of the formula: 1

Abstract: A compound of the formula wherein the substituents are as defined in the application and its non-toxic, pharmaceutically acceptable acid and base salts useful for hormone replacement for treating menopause or perimenopause without activity at the uterine level treating osteoporosis and strengthening cardiovascular protection in warm-blooded animals.

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 saturated fatty acid radicals and X is either a direct bond or a bonding member between bile acid or bile salt and the fatty acid(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. The fatty acids are preferably saturated fatty acids having 6-26 carbon atoms.