Abstract: The disclosure relates to anti-cancer compounds derived from a payload which binds to poly(ADP-ribose) polymerase (PARP) and a nuclear steroid-targeting epitope (B of Formula I), which components are covalently linked via a linker, to products containing the same, as well as to methods of their use and preparation.

Abstract: Disclosed in the present disclosure are a novel injection polyaminopolycarboxylic acid-modified abiraterone derivative for treatment of prostate tumor, a pharmaceutical preparation containing the polyaminopolycarboxylic acid-modified abiraterone derivative, a preparation method, and an application. The polyaminopolycarboxylic acid-modified abiraterone derivative has the following structure (I). The polyaminopolycarboxylic acid-modified abiraterone derivative in the present disclosure has good water solubility, can be completely dissolved in an aqueous solution of sodium bicarbonate, is simple and convenient to prepare, high in yield, and suitable for large-scale production, has a remarkable effect in resisting tumors, can be used for treating prostate cancer tumor, and has the characteristics of high efficiency and low toxicity.

Abstract: High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (1): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, and status epilepticus.

Abstract: The present invention concerns novel pharmaceutically active triterpene amine derivatives, pharmaceutical compositions containing the same, their use as medicaments, and the use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the triterpene amine compounds. Specifically, the compounds are derivatives of betulinic acid having substitutions at one or more of the C-3, C-28 and C-19 positions as further described herein. The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus-1 (HIV-1).

Abstract: The present application relates to amine salt of obeticholic acid. Specifically, the present application relates to (S)-?-methylbenzylamine and diethylamine salt of obeticholic acid. The present application also relates to a process for preparation of amorphous form of obeticholic acid comprising converting amine salt of obeticholic acid to amorphous form of obeticholic acid.

Abstract: This invention relates the use of cortisol blockers (glucocorticoid receptor [GR] antagonists) for the treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.

Abstract: Provided is a rocuronium preparation designed to reduce vascular pain to be induced. The rocuronium preparation contains rocuronium and a buffer solution, and has titratable acidity of 100 mEg or less. The buffer solution may be an acetate buffer solution, a citrate buffer solution, a formate buffer solution, a tartrate buffer solution, a phosphate buffer solution, a glycine-hydrochloric acid buffer solution, or a citric acid-phosphate buffer solution.

Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, status epilepticus.

Abstract: The invention relates to a composition and method for increasing blood pressure, including a low pain or analgesic state or hypotensive anaesthesia in a subject that has suffered a life threatening hypotension or shock or reducing hypofusion in the whole body of a subject. The composition comprises (i) a compound selected from at least one of a potassium channel opener, a potassium channel agonist and an adenosine receptor agonist; and (ii) an antiarrhythmic agent or a local anaesthetic.

Abstract: Methods and compositions for treating cancer are described herein. More particularly, the methods for treating cancer comprise administering a 17?-hydroxylase/C17, 20-lyase inhibitor, such as abiraterone acetate (i.e., 3?-acetoxy-17-(3-pyridyl) androsta-5, 16-diene), in combination with at least one additional therapeutic agent such as an anti-cancer agent or a steroid. Furthermore, disclosed are compositions comprising a 17?-hydroxylase/C17, 20-lyase inhibitor, and at least one additional therapeutic agent, such as an anti-cancer agent or a steroid.

Abstract: This invention relates the use of cortisol blockers (glucocorticoid receptor [GR] antagonists) for the treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.

Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, and status epilepticus.

Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.

Abstract: Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3?-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3?-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.

Abstract: The invention relates to a composition for preventing bearing loss in subject or for at least partially restoring bearing in a subject having a reduced auditory function. The composition comprises at least one sterol compound inducing neuron differentiation. Said composition is placed in contact with at least part of the cochlea.

Abstract: The invention relates to the use of an anabolic amino acid derivative stimulus acting in combination with vitamin D for the manufacture of a medicament or nutritional composition for the prevention and/or treatment of a loss of any one of muscle mass, muscle strength, muscle function, and physical function, or any combination thereof, in a mammal.

Abstract: Combinations of (3?)-17-(pyridin-3-yl)androsta-5,16-dien-3-yl acetate (Abiraterone acetate) with acidic substances such as citric acid, ascorbic acid, methyl-4-hydroxy benzoate, saccharin, vanillic acid, adipic acid, maleic acid, malic acid, tartaric acid are useful as pharmaceutical preparations and show improved properties such as aqueous solubility and dissolution kinetics, especially in the form of cocrystals or their combination with a suitable acid.

Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, status epilepticus.

Abstract: The present invention discloses a novel bile acid derivatives having substituted nitrogen functionality at C-11 and process for synthesis thereof. These C-11 substituted bile acid derivatives shows anticancer and antimycobacterial activity.

Abstract: The invention provides a method of inhibiting vascular hyperpermeability in an animal in need thereof. The method comprises administering a vascular-hyperpermeability-inhibiting amount of a danazol compound to the animal. The invention also provides a method of modulating the cytoskeleton of an endothelial cell in an animal. The method comprises administering an effective amount of a danazol compound to the animal.

Abstract: The present disclosure provides the design and synthesis of novel steroidal compounds that cause down-regulation of the androgen receptor (AR), both full length and splice variant. The compounds are potential agents for the treatment of all forms of prostate cancer and other diseases that depend on functional AR.

Abstract: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R2, R3, R4, R7 and R8 are as defined in the claims. The invention further relates to their use as inhibitors of 17?-HSD1 and in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17?-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof.

Abstract: Anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, according to formula (I) according to formula (I) defined herein are useful for treating diseases of the respiratory tract characterized by airway obstruction.

Abstract: Compositions and methods for modulating innate and adaptive immunity and for use in immunotherapy are disclosed. In particular, the invention relates to novel ganciclovir derivatives and methods of using them for the treatment of immune-related disorders, including inflammation, autoimmunity, and infections, and neurological disorders, and cancer.

Abstract: The invention relates to AKR1C3 inhibitors of formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of bleeding disorders and endometriosis.

Abstract: Novel solanidine-derived compounds, the synthesis method thereof and the uses of same in the fields of phytosanitary protection and health. In particular, the novel compounds have toxic and/or repellent properties in relation to aphids, as well as other properties.

Abstract: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R2 to R7 are as defined in the claims. The invention further relates to their use as inhibitors of 17?-HSD and in treatment or prevention of steroid hormone de-pendent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17?-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the afore-mentioned compounds or pharmaceutically acceptable salts thereof.

Abstract: The present disclosure relates to pharmaceutically acceptable complex formulae comprising complexes of Abiraterone acetate and pharmaceutically acceptable excipients, process for the preparation thereof and pharmaceutical compositions containing them. The complex formulae of the present disclosure have improved physicochemical properties which results in reduced food effect which allows significant dose reduction and the abandoning of the requirement of taking the drug on an empty stomach.

Abstract: The present invention provides methods and compositions for the treatment of fluid accumulation in and/or under the retina.

Abstract: Disclosed herein are compositions comprising an amide related to a prostaglandin and a biogenic amine. Other aspects relate to certain chemical compounds, pharmaceutical compositions, and methods of treating glaucoma.

Abstract: Described herein are methods and compositions for the treatment of prostate cancer in a subject in need thereof. The prostate cancer may be a castration resistant and an androgen receptor antagonist-resistant prostate cancer. The methods may comprise administering to the subject a CYP17-lyase inhibitor of Formula II.

Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, and status epilepticus.

Abstract: The invention provides a method of inhibiting vascular hyperpermeability in an animal in need thereof. The method comprises administering a vascular-hyperpermeability-inhibiting amount of a danazol compound to the animal. The method comprises administering an effective amount of a danazol compound to the animal accounting for the body fat content of the animal. The invention also provides a method of modulating the cytoskeleton of an endothelial cell in an animal.

Abstract: The present disclosure relates to a novel vascular leakage inhibitor. The novel vascular leakage inhibitor of the present invention inhibits the apoptosis of vascular endothelial cells, inhibits the formation of actin stress fibers induced by VEGF, and enhances the cortical actin ring structure, thereby inhibiting vascular leakage. Accordingly, the vascular leakage inhibitor of the present invention can prevent or treat various diseases caused by vascular leakage. Since the vascular leakage inhibitor of the present invention is synthesized from commercially available or easily synthesizable pregnenolones, it has remarkably superior feasibility of commercial synthesis.

Abstract: Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.

Abstract: Prodrugs of steroidal C-17 benzoazoles, pyrimidinoazoles (az-abenzoazoles) and diazines. Methods of synthesis are also described, whereby a prodrug group is substituted for a functional group at A ring portion of the ABC ring structure of the steroid. Suitable pro-drug groups include amino acid groups, succinate groups, phosphate groups, or sulfamate groups. The prodrugs of the disclosed compounds allow for improved oral bioavailability of the compounds that are inhibitors of human CYP 17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds and the corresponding prodrugs are useful for the treatment of conditions such as human prostate cancer, breast cancer, and prostate hyperplasia.

Abstract: Bivalent multifunctional A? oligomerization inhibitors (BMAOIs) that target multiple risk factors involved in Alzheimer's disease are provided. The BMAOIs are useful for the treatment and/or prevention of Alzheimer's disease, as well as for diagnostic imaging of A? plaques in brain tissue. The BMAOIs comprise i) an A? oligomer (ApO)-inhibitor moiety which may have antioxidant activity (e.g. curcumin, curcumin derivatives, curcumin hybrids, resveratrol, etc.); ii) a cell membrane/lipid raft (CM/LR) anchoring moiety (e.g. cholesterol, cholesterylamine, a steroid, etc.); and iii) a spacer or linker moiety that stably links i) and ii) together.

Abstract: Photosensitive compounds for use in a method of treating a disease or condition are described. The photosensitive compounds have the formula R—Y, wherein R is a ruthenium complex and Y is at least one sulphur-containing photoreleasable group, and the compounds comprise at least one ruthenium-sulphur bond; or a pharmaceutically acceptable salt, solvate, ester or amide, such that upon influence of visible or near infra-red light (400-1400 nm) in vivo, said at least one ruthenium-sulphur bond is broken, thereby generating a pharmacologically active compound.

Abstract: The invention relates to 17-hydroxy-13-methyl-17-pentafluoroethyl-11-acyloxyalkylenephenyldodecahydrocyclopenta[a]phenanthren-3-one derivatives of the formula I with progesterone-antagonizing action and to processes for preparation thereof, to use thereof for treatment and/or prophylaxis of disorders and to the use thereof for production of medicaments for treatment and/or prophylaxis of disorders, especially of fibroids of the uterus (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause, or for fertility control and emergency contraception.

Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.

Abstract: Provided are methods and compositions for reducing superoxide anions such that a prophylactic or therapeutic effect against conditions associated with excess oxidative stress achieved. The compositions and methods provide for reducing inflammation and for enhancing lifespan of eukaryotic organisms. A screen for identifying compounds that can be used in these methods is also provided.

Abstract: Pharmaceutical composition comprising abiraterone acetate, which exhibits a reduced food effect and improved bioavailability.

Abstract: Compositions, and methods of using such compositions, useful for placement, for example injection, into the interior of human or animal eyes are provided. Such compositions include a therapeutic component, such as one or more corticosteroids, a biocompatible polymeric component, and a solvent component. The composition is in a fluid form before placement in the interior of an eye, and becomes less fluid after the composition is placed in the eye to form an extended or delayed release drug delivery element or system. The drug delivery element is formed by the dissipation of the solvent from the composition when the composition is placed in the interior of an eye. One example of a composition includes triamcinolone acetonide as a therapeutic agent. A method of treating an ophthalmic condition, or otherwise improving or enhancing vision of a patient, comprises placing the fluid composition in the interior of the eye. The method may be practiced by injecting the fluid composition into the interior of the eye.

Abstract: This document provides methods and materials related to genetic variations associated with endometriosis. For example, this document provides methods for using such genetic variations to assess risk of, or susceptibility of developing or diagnosing endometriosis.

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: The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.

Abstract: Prodrugs of steroidal C-17 benzoazoles, pyrimidinoazoles (az-abenzoazoles) and diazines. Methods of synthesis are also described, whereby a prodrug group is substituted for a functional group at A ring portion of the ABC ring structure of the steroid. Suitable pro-drug groups include amino acid groups, succinate groups, phosphate groups, or sulfamate groups. The prodrugs of the disclosed compounds allow for improved oral bioavailability of the compounds that are inhibitors of human CYP 17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds and the corresponding prodrugs are useful for the treatment of conditions such as human prostate cancer, breast cancer, and prostate hyperplasia.

Abstract: This application is directed to the use of aminosteroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.

Abstract: The present invention relates to a process for the synthesis of (3beta)17-(3-pyridinyl)androsta-5,16-dien-3-yl acetate (Abiraterone acetate) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates in such processes.