Abstract: A 1H-pyrazolo[4,3-H]quinazoline compound represented by formula (I) can be used for treating cell proliferation dysfunction, and is an broad-spectrum and strongly-active inhibitor for a cell cyclin-dependent kinase (CDK).

Abstract: The present invention relates to novel fused imidazo pyrazole derivatives of formula (I), and formula (II), and methods for preparation thereof, in the presence of a chitosan-Al2O3 nanocomposite film. The invention also relates to pharmaceutical compositions comprising compounds of the invention as active ingredients as well as the use of compounds of the invention for antimicrobial action.

Abstract: A drug is provided, which containing, as an active ingredient, a compound having ABHD6 inhibitory activity in prevention and/or treatment of a disease associated with ABHD6. A compound of formula (I-A) or a pharmaceutically acceptable salt thereof has ABHD6 inhibitory activity and therefore is useful as a pharmaceutical ingredient having potent ABHD6 inhibitory activity in the prevention and/or treatment of a disease associated with ABHD6: in which all symbols represent the same meaning as the symbols described in the specification.

Abstract: Disclosed are compounds that bind to embryonic ectoderm development (EED) protein and proteolysis-targeting chimeric (PROTAC) derivatives thereof that induce degradation of EED. The disclosed compounds may be characterized as substituted [1,2,4]triazolo[4,3-c]pyrimidin-5-amine compounds. The disclosed PROTAC derivatives thereof typically include a first targeting moiety that binds to EED (MEED) which may be derived from the disclosed [1,2,4]triazolo[4,3-c]pyrimidin-5-amine compounds that bind to EED. The first targeting moiety typically is linked via a bond or a linker (L) to a second targeting moiety that binds to an E3 ubiquitin ligase (ME3). As such, the disclosed PROTACS may be described as having a formula MEED-L-ME3 or ME3-L-MEED, wherein MEED has a formula of where R2, n, and x are as described herein.

Abstract: The invention provides various novel compositions of berberine in combination with pharmacologically active organic acids, and related methods of their use in treating various diseases or disorders. The invention further provides various novel compounds prepared from berberine and pharmacologically active organic acids and prepared from ursodeoxycholic acid and pharmacologically active organic bases, and pharmaceutical compositions thereof, and methods of their preparation and therapeutic use in treating and/or preventing various diseases or disorders.

Abstract: Novel 5-substituted aminopyrimido[6?,1?:2,3]imidazo[4,5-c][1,6]naphthyridine compounds having the formula I below with all substituents as defined in the instant specification, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The 5-substituted aminopyrimido[6?,1?:2,3]imidazo[4,5-c][1,6]naphthyridine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: The present disclosure provides bifunctional compounds of Formula (I), and pharmaceutically acceptable salts, isotopic forms, isolated stereoisomers, or mixtures of stereoisomers thereof, as IRAK4 degraders via ubiquitin proteasome pathway, and method for treating diseases modulated by IRAK4.

Abstract: Compounds for treating tuberculosis and, particularly, to anti-tubercular compounds that are 5-(1H-indol-3-yl)-1,3-substituted-7-thioxo-7,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives and their use as anti-tubercular agents. Each compound may have the formula I: or a pharmaceutically acceptable salt or tautomer thereof, wherein: R1 is H or CH3; R2 is H or CH3; and X is O or S.

Abstract: Pyrimido[4,5-b]indole compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrimido[4,5-b]indole compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: Novel pyrido[3?,4?:4,5]pyrrolo[3,2-c][1,6]naphthyridine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrido[3?,4?:4,5]pyrrolo[3,2-c][1,6]naphthyridine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: Calcium reacting photoproteins are a class of self-illuminating proteins that emit light upon contact with calcium. Fluorescent Proteins are small proteins that change the color of light when excited. Fluorescent Proteins and Calcium Activated Photoproteins can be used to enhance, dazzle, amaze, startle, and otherwise entertain an audience by their direct application on to the audience, surroundings, the actors, or sprayed on settings as in the newer 4D movies. The disclosure comprises novel Coelenterazine compounds and methods of use, including a simple delivery device for the photoprotein to create unique and novel cinematic, theatrical, stage, movie and musical concert optical effects by their luminous reaction upon contact with surfaces that contain calcium. Calcium is ubiquitous in and on most surfaces and in the environment; it is this unique property of calcium that makes this a novel use of the photoproteins for entertainment. A generic formula of Coelenterazine as shown.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or stereoisomer thereof: Pharmaceutical compositions containing said compounds, and the use of said compounds in the treatment and/or prophylaxis of thromboembolic disorders, inflammatory disorders and diseases or conditions in which plasma kallikrein activity is implicated.

Abstract: A combination product comprising a carbapenem and a compound of formula (I?), or a pharmaceutically acceptable salt thereof: a pharmaceutical composition comprising the combination product; and methods of treating bacterial or fungal infections using the combination product and pharmaceutical composition.

Abstract: The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof: It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses, in particular in the treatment of diseases or disorders associated to increased relative to physiological or desired RhoJ/Cdc42 levels of expression or function.

Abstract: The invention relates to compounds of formula (I): or a salt thereof, wherein R1, G, L1, L2, L3, and Y are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are inhibitors of one, or both of, ?v?1 integrin and ?v?6 integrin that are useful for treating fibrosis such as in nonalcoholic steatohepatitis (NASH), idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).

Abstract: Inhibitor compounds and agents of Cathepsin C, CELA1, CELA3A and/or structurally related molecules thereto, compositions comprising the same, and uses thereof in the inhibition and/or prevention of cell and/or tissue necrosis are described. The compounds include imidazoles of Formula VI: wherein G1 is pyrrolidine, pyrazolidine, imidazolidine piperidine, or piperazine and G2 is alkyl, cycloalkyl, heterocycle, or aryl. The pyrrolidine, pyrazolidine, imidazolidine, piperidine, or piperazine of G1 and the alkyl, cycloalkyl, heterocycle, or aryl of G2 are optionally substituted with one or more substituents independently selected from the group consisting of halogen, NO2, CN, C1-C6 alkyl, C1-C6 haloalkyl, NH2, OH, OC1-C6 alkyl, C(O)H, C(O)C1-C6 alkyl, C(O)NH2, C(O)OH, and C(O)OC1-C6 alkyl. Variations applications for the described compounds, and combination therapies are further described as well.

Abstract: Novel dimethyl 7-bromo-1-(4-substituted benzoyl)pyrrolo[1,2-?]quinoline-2,3-dicarboxylates compounds, having the structure: A method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The dimethyl 7-bromo-1-(4-substituted benzoyl)pyrrolo[1,2-?]quinoline-2,3-dicarboxylates compounds, identified as anti-inflammatory agents, are useful for treating inflammation, pain, and swelling in a patient.

Abstract: Pyrrolo[2,3-d]pyrimidine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrrolo[2,3-d]pyrimidine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: The present disclosure relates to a novel PLK1 degradation inducing compound having a structure according to Formula I, a method for preparing the same, and the use thereof. The compounds of the present disclosure exhibit an effect of inducing PLK1 degradation. Therefore, the compounds of the present disclosure may be effectively utilized for preventing or treating PLK1-related diseases.

Abstract: Provided herein are inhibitors of PARG, pharmaceutical compositions comprising the inhibitory compounds, and methods for using the PARG inhibitory compounds for the treatment of disease.