Abstract: The present invention provides salts and crystalline forms of Linsitinib (OSI-906; cis-3-[8-amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutanol). These forms of Linsitinib provide increased solubility and improved pharmacokinetic profiles for orally administered pharmaceutical formulations. Accordingly, the invention enables improved methods for treating human insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) mediated conditions.

Abstract: A compound N?-[(2-chlorobenzoyl)oxy]-1,3-benzothiazole-2-carboximidamide, its synthesis, and its use as an anticancer and/or antimicrobial agent.

Abstract: This invention relates to novel salts and crystal forms of 2-[3-({1-[2-(dimethylamino)ethyl]-2-(2,2-dimethylpropyl)-1H-1,3-benzodiazol-5-yl}sulfonyl)azetidin-1-yl]ethan-1-ol, simply abbreviated as Compound A, which is a selective CB2 receptor agonist. The present invention provides a salt of Compound A, a crystal form thereof, a method for preparing the said salt and a pharmaceutical composition thereof and its use. The salts of Compound A of the present invention show good pharmaceutical formulation properties such as high aqueous solubility, good crystallinity, high melting point, good chemical and physical stability, or non-deliquescent.

Abstract: The invention discloses compositions and methods comprising enriched Bisdemethoxycurcumin (BDMC) present not less than 20% w/w for use in inhibiting Receptor for Advanced Glycation End-Products (RAGE) expression in a subject with chronic-inflammatory condition. The composition further comprises ?-amyrin palmitate (BAP). The invention also includes disclose the use of the above composition in the management of chronic inflammatory condition in a subject.

Abstract: RAS modulating compounds and methods of using the same are provided. The compounds find use in modulating the activity of a target RAS in a sample. The target RAS can be a mutant RAS that is implicated in a disease of interest. In some cases, the subject compounds can inhibit the growth of cancer cells whose progression is driven by kRAS or a mutated kRAS. Methods of treating a subject for a RAS driven disease including administering a therapeutically effective amount of the subject compound are provided. Also provided are pharmaceutical compositions and kits which include the subject compounds.

Abstract: The invention relates to a pharmaceutical composition comprising a protein phosphatase 2A (PP2A) inhibitor and monosodium glutamate.

Abstract: Disclosed herein are pyrazole pyrimidine compounds that modulate and/or inhibit hematopoietic progenitor kinase 1, as well as methods of making such compounds and therapeutic methods of using same.

Abstract: The application relates to N-(4-fluoro-3-(6-(3-methylpyridin-2-yl)-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)phenyl)-2,4-dimethyloxazole-5-carboxamide (Compound I) fumaric acid co-crystals and X-ray amorphous complexes of Compound (I) and fumaric acid. The application also provides methods of making the same; pharmaceutical compositions comprising them; and their use in treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a kinetoplastid parasite, such as leishmaniasis, human African trypanosomiasis and Chagas disease.

Abstract: The present invention relates to a compound according to general formula (I), which acts as an inhibitor of PqsR (the currently only known receptor for the Pseudomonas Quinolone Signal (PQS)); to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament, e.g. the use in the treatment or prophylaxis of a bacterial infection, especially a Pseudomonas aeruginosa or Burkholderia infection.

Abstract: This disclosure pertains to compounds, the preparation thereof, and the use of these compounds in the treatment of prostate cancer, including metastatic and/or castrate-resistant prostate cancer, in subjects in need thereof.

Abstract: The present disclosure relates to novel compounds for use in therapeutic treatment of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.

Abstract: The present disclosure relates to the discovery that certain ocular diseases may be treated using Edonentan crystalline forms. Specific Edonentan crystalline form can be used alone or in combination with an intra-ocular pressure (TOP) reducing agent, a neuroprotective agent, or an anti-VEGF agent. Using Edonentan crystalline forms, alone or in combination with an additional agent, provides increased perfusion to the retina or reduced IOP in certain ocular diseases and reduces damage to retinal cells.

Abstract: The present invention is related to the inhibition of the formation of Streptococci biofilms through the inhibition of glucosyl transferase (Gtf). Compounds, compositions and methods for inhibiting Streptococcus biofilm formation, as well as for preventing, inhibiting and/or treating the formation of dental caries, and methods of identifying compounds that prevent, inhibit and/or treat the formation of dental caries are provided.

Abstract: The disclosure provides methods, treatments and materials for enhancing the effect of an adenosine A2 receptor agonist in the treatment, mitigation or prophylaxis of a disease or condition characterized by inotropic and/or lusitropic dysfunction, and/or enhancing adenosine A2 receptor function in the treatment, mitigation or prophylaxis of a disease or condition characterized by impaired adenosine A2 receptor function, comprising administration of an effective amount of a PDE1 inhibitor to a patient in need thereof, for example a patient suffering from heart failure.

Abstract: The present invention relates to novel compounds of formula I: which have the properties of CDK8/19 inhibitors, to a pharmaceutical composition comprising said compounds, and to use thereof as a medicine for treating diseases and disorders.

Abstract: There is provided a compound of formula (I), wherein R1, R2, R3, Q1, Q2, Q3, X, A and n are as defined herein, which compounds are useful in the treatment of diseases characterised by impaired signalling of neurotrophins and/or other trophic factors, such as Alzheimer's disease and the like.

Abstract: Disclosed herein are methods for treating or limiting development of cardiovascular disease-related neurological disorders by administering a compound of general formula (I), as defined herein.

Abstract: The present disclosure relates to a pharmaceutical composition comprising ibrutinib as an effective ingredient for preventing or treating neurodegenerative brain disease. Ibrutinib according to the present disclosure inhibits LPS-induced proinflammatory cytokine levels and BV2 microglial cell migration. In addition, ibrutinib treatment significantly reduced LPS-mediated microglial and astroglial activation. Ibrutinib treatment significantly diminished AP plaque numbers, tau hyperphosphorylation, and tau kinase CDK5 phosphorylation. Moreover, ibrutinib treatment enhances memory and thus can be used as a therapeutic agent for prevention or treatment of neurodegenerative brain disease.

Abstract: Provided are crystalline forms of (R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-2-(oxetan-3-yl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-5-yl)-1H-1,2,3-triazole-4-carboxamide, pharmaceutical compositions, methods of use and methods of making thereof.

Abstract: Provided herein are compounds of formula (I?): or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein Y2, Y3, L1, L2, X1, X2, X3, X4, X5, Q1, R1, R2, Rk, Rm, and Rn are as defined elsewhere herein. Also provided herein are methods of preparing compounds of formula (I?). Also provided herein are methods of inhibiting GYS1 and methods of treating a GYS1-mediated disease, disorder, or condition in an individual in need thereof.