Abstract: Disclosed are aqueous pharmaceutical compositions which provide sustained released delivery of corticosteroid compounds. The pharmaceutical composition comprises a soluble corticosteroid and at least one viscosity enhancing agent. Also provided are methods for using the pharmaceutical compositions in an epidural injection, intra-articular injection, or an intra-lesional injection.

Abstract: The invention discloses an improved process for production of vitamin D3 from 7-dehydrocholesterol (7-DHC) and to a simple process for recovery unreacted 7-DHC for further reuse. The invention further describes a process for isolation and purification of Vitamin D3.

Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.

Abstract: Provided herein is a transdermal liquid formulation that includes a propionic acid-based non-steroidal anti-inflammatory agent, such as ketoprofen, and a dermal penetration enhancer containing an alcohol, an emollient and an essential oil. Methods of using and making the aforementioned transdermal liquid formulation are also provided herein.

Abstract: A small molecule compound IODVA1 has been found to have cellular inhibitory activity against several transformed cell lines including Ras-driven cells. IODVA1 decreases cell-cell and cell-extra cellular matrix interactions and reduces growth of Ras-driven tumors. Applicants also synthesized compound NIRA2 and showed in vitro and in vivo efficacy and potency against models of Ph+(BCR-ABL1) B-ALL and of colon adenocarcinoma xenografts.

Abstract: Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R19, R5, R3a, R1a, R1b, R2a, R2b, R4a, R4b, R6a, R6b, R7a, R7b, R11a, R11b, R12a, R12b, R18, RD, and q are defined herein. L is selected from the group consisting of: wherein A indicates the point of attachment at C17 and wherein X is selected from the group consisting of —C(O)N(R55a)(R55b), —N(R55a)(R55b), —N(R55b)C(O)(R55a), and R55C wherein R55c is carbon-bound substituted or unsubstituted heteroaryl or substituted or unsubstituted aryl. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

Abstract: The present disclosure encompasses solid state forms of Mavacamten, in embodiments crystalline polymorphs of Mavacamten, processes for preparation thereof, and pharmaceutical compositions thereof.

Abstract: Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R19, R5, R3a, R1a, R1b, R2a, R2b, R4a, R4b, R6a, R6b, R7a, R7b, R11a, R11b, R12a, R12b, R18, RD, and q are defined herein. L is selected from the group consisting of: wherein A indicates the point of attachment at C17 and wherein X is selected from the group consisting of —C(O)N(R55a)(R55b), —N(R55a)(R55b), —N(R55b)C(O)(R55a), and R55C wherein R55c is carbon-bound substituted or unsubstituted heteroaryl or substituted or unsubstituted aryl. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

Abstract: The present invention is directed to a process for the preparation of cortexolone 17?-propionate, comprising a hydrolysis reaction of an ortho-ester of formula (III) in which R is a hydrogen atom or a methyl group, in the presence of a dilute solution of acetic acid. The present invention is also directed to a hydrated crystalline form of cortexolone 17?-propionate obtained by such process.

Abstract: The present invention provides methods of treating or suppressing Adenoid Cystic Carcinoma (ACC) or inhibiting ACC tumor growth in subjects by administering compositions comprising bisfluoroalkyl-1,4-benzodiazepinone compounds, including compounds of Formula (III) or prodrugs thereof.

Abstract: Compounds having the formula or solvates of the compounds can be used as intermediates in the preparation of the synthetic steroids, Etonogestrel and Desogestrel, as well as other pharmaceutically active agents.

Abstract: A composition having the following structure: wherein: R1 is OH, ester group, ether group, amine, thiol, thioether, halide, or a group containing an alkynyl or azido functionality; R2 is H, OH, ester group, ether group, amine, thiol, thioether, halide, or a group containing an alkynyl or azido functionality; R3 is a group containing a reactive functionality capable of covalent binding to a thiol or amine; and R4 is H, OH, ester group, ether group, amine, thiol, thioether, halide, or a group containing an alkynyl or azido functionality; wherein one of R1, R2 and R4 is a group containing an alkynyl or azido functionality. Also disclosed is a method for profiling changes in BSH enzyme activity by attaching active BSH enzymes in a sample to the probe shown above, attaching a tag to the probe, and detecting the active BSH enzymes to obtain an activity profile.

Abstract: A method of treating Alcohol Use Disorder (AUD), Substance Use Disorder (SUD), tobacco use, pain, or proinflammatory disorders comprising: providing a subject with an effective amount of a modified tetracycline or derivative thereof to ameliorate or eliminate the AUD, SUD, tobacco use, pain, or proinflammatory disorder, and wherein the modified tetracycline or derivative thereof has reduced binding to a microbial ribosome and has the formula: wherein R1 is acetyl, R2 is OH or acetyl, R3 is acetyl, R4 is H or acetyl, and R5 is acetyl.

Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein, R1, R2a, R2b, R3 and A are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.

Abstract: The present invention includes DNP derivatives that are useful for preventing or treating a metabolic disease or disorder in a subject in need thereof. In certain embodiments, the subject is further administered at least one additional therapeutic agent.

Abstract: Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function where the compounds are 11,13-modified saxitoxins according to Formula (I): (Formula (I)); where R1, and R2 are as described herein.

Abstract: Provided are compositions comprising unequal mixtures of (R)-amisulpride and (S)-amisulpride, or pharmaceutically acceptable salts thereof, where the amount of (R)-amisulpride is greater than the amount of (S)-amisulpride, compositions and medicaments comprising the same used for the treatment of various diseases and disorders, and methods of using same for the treatment of various diseases and disorders, including, but not limited to, dosage regimens. In addition, provided are various formulations thereof, including, but not limited to, formulations employing polymorphs of enantiomeric amisulpride.

Abstract: The present invention provides a compound of Formula I: wherein R1 is H, halogen, C1-C3 alkyl, or C1-C3 alkoxy; R2 is H or halogen; and X is O, OCH2, or CH2, or a pharmaceutically acceptable salt thereof, wherein the compound of Formula I, or pharmaceutically acceptable salt thereof is useful for treating autoimmune and inflammatory diseases, such as atopic dermatitis, rheumatoid arthritis, and lupus nephritis.

Abstract: The invention generally relates to conducting reactions in Leidenfrost-levitated droplets.

Abstract: Methods of treating a liver disease or condition, or a symptom thereof, in a subject in need of treatment, are disclosed and described. One method comprises orally administering to a subject, a pharmaceutical composition having an amount of a testosterone, or an ester thereof, sufficient to treat the liver disease or condition, or symptom thereof.