Abstract: The present application provides bicyclic amines that are inhibitors of cyclin-dependent kinase 12 (CDK12), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.

Abstract: The present invention relates to an amide derivative compound, which exhibits the activity of a diacylglycerol acyltransferase (DGAT) 2 inhibitor and is represented by chemical formula (1), a pharmaceutical composition comprising same as an active ingredient, and a use thereof.

Abstract: The present disclosure provides compositions and methods for treating pulmonary hypertension. The compositions and methods are based on administering a NO-releasing compound, such as nitrite, to a subject in need thereof in an amount sufficient to increase the level of circulating nitric oxide (NO), a potent vasodilator, thereby reducing the subject's blood pressure and increasing blood flow.

Abstract: The present invention provides a combination of a 5HT3-antagonist and/or a NK-1 antagonist with 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine and with fluoxetine or a pharmaceutically acceptable salt or solvate thereof, zonisamide or a pharmaceutically acceptable salt or solvate thereof, or a statin or a pharmaceutically acceptable salt or solvate thereof, for use for treating a protein misfolding neurodegenerative disease such as Alzheimer's disease, Lewy body disease, Parkinson's disease, or Huntington's disease.

Abstract: Disclosed herein are heterocyclic compounds that activate GLP-1R pathways. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the GLP-1R agonists are disclosed, alone or in combination with other therapeutic agents, for the treatment of diabetes, obesity, and other diseases or conditions dependent on GLP-1R pathways.

Abstract: The present invention relates to a crystal form of a compound of Formula (I), i.e. (2-((5-chloro-2-((2-methoxy-4-(9-methyl-3,9-diaza-spiro[5.5]undecan-3-yl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide. The present invention further relates to a pharmaceutical composition of the crystal form, and the pharmaceutical use thereof and a preparation method therefor.

Abstract: The present invention relates to process for preparation of Form I polymorph of 1-[(6-chloro-3-pyridyl) methyl]-N-nitroimidazolidin-2-ylideneamine (imidacloprid). In particular the present invention relates to process for preparation of Form I of imidacloprid containing dimer impurity?0.5%.

Abstract: Bifunctional compounds, which find utility as modulators of leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Abstract: The present invention relates to a slow release formulation. It relates also to the use of said repellent formulation, to a method of use thereof, and to a composition comprising said formulation. It further relates to PMD glucovanillin conjugate compound of formula (II), a process for preparing the compound of formula (II), and further to the use of the compound of formula (II) for the controlled release of PMD. It refers also to a process for isolating racemic cis/trans-PMD from an extract containing PMD.

Abstract: A sterile storage stable ready-to-inject epinephrine composition contained within a flexible container and packaged within a secondary container, the composition including an aqueous pharmaceutically acceptable carrier containing epinephrine and a metal ion chelator, the epinephrine being present in a concentration of equal to or less than 0.07 mg/mL, substantially all of the epinephrine being an R-isomer, the composition having a pH of between 3.5-4.7, and the composition having, after storage of at least one month at 25° C., total impurities of equal or less than 0.7% and equal or less than 4% S-isomer content.

Abstract: An orally dissolvable or chewable tableted powder formulation is presented. The formulation includes one or more carrier systems including one or more liquid or solid self-emulsifying systems loaded with cannabinoids in an amount of at least 10% by weight of the tableted powder formulation. The one or more self-emulsifying systems includes: at least one or more surfactants, one or more lipids and one or more isolated or synthetic cannabinoids when self-emulsifying system is a liquid self-emulsifying system, and at least one or more surfactants, one or more waxes and one or more isolated or synthetic cannabinoids when self-emulsifying system is a solid self-emulsifying system. The formulation further includes one or more water-soluble agents in an amount of 20-80% by weight of the tableted powder formulation and one or more flavors. The one or more surfactants includes one or more surfactants having a chemical structure that includes a polyethylene glycol moiety.

Abstract: The invention concerns a compound of formula (Ia) or (Ib) wherein R1 is hydrogen or a methyl group; R2 is an unsubstituted or substituted alkyl group; R3 is an aryl group or a heteroaryl group, optionally substituted by one or more groups selected from halogen, alkyl or alkoxy; and, in Formula (Ia), X is CH or N and Y is NH, S or O, or, in Formula (Ib), X is NH, S or O and Y is CH or N. The invention further concerns a method of synthesizing the inventive compound, a composition comprising the inventive compound or a pharmaceutically acceptable salt thereof and bedaquiline (BDQ), an analogue of bedaquiline (BDQ) or a mixture thereof, and the use of said composition or compound for the treatment of tuberculosis.

Abstract: The invention relates to trazodone for use in the treatment of insomnia in the pediatric population, wherein said pediatric population is affected by an Intellectual Disability or a Neurodevelopmental Disorder. The invention also relates to pediatric formulations at a trazodone concentration comprised of from 0.1 to 4% and pediatrically suitable excipients.

Abstract: A ready-to-administer epinephrine composition having between about 0.005 and about 0.07 mg/mL epinephrine, at least about 0.9 wt % sodium chloride; between about 1 and about 50 ug/mL ethylenediaminetetraacetic acid; 0.005 wt % or less sodium metabisulfite, and water. Also included are systems having the composition contained in a container.

Abstract: The invention provides methods of treatment of heart failure with preserved ejection fraction (HFpEF) using modified forms of trimetazidine, such as CV-8972 and CV-8814.

Abstract: This disclosure provides crystalline forms of trofinetide and trofinetide hydrate, pharmaceutical compositions comprising crystalline forms of trofinetide and trofinetide hydrate, methods of making crystalline forms of trofinetide or trofinetide hydrate, and methods of treating a disease, condition, or disorder in a subject comprising administering a composition comprising crystalline forms of trofinetide or trofinetide hydrate to the subject.

Abstract: Provided herein are GLP-1 receptor modulator compounds, pharmaceutical compositions, methods of their preparation, and methods of their use in treatment, and/or diagnosis.

Abstract: Pharmaceutical compositions with tryptamines having enhanced active stability properties are described.

Abstract: The present invention provides compounds useful for the treatment of narcolepsy or cataplexy in a subject in need thereof. Related pharmaceutical compositions and methods are also provided herein.

Abstract: Disclosed herein are methods of synthesis of a trans isomeric form of a C—C chemokine receptor type 4 (CCR4) modulator, or a salt or ester thereof that comprise making a trans isomeric compound of formula (III) by reacting a compound of formula (I) with a compound of formula (II) in the presence of a carboxylic acid directed reducing agent, wherein the compound of formula (III) is in a predominantly trans isomerically pure form.