Abstract: A compound of compound according to formula (I): wherein X is selected from the group consisting of CH, CCl and N, Z is selected from the group consisting of CH2COOH, CH(CH3)COOH, C(CH3)2COOH and CH2F, D is a single bond connecting A and Ar or selected from the group consisting of CO, NHCO and N(C0-6)alkyl-CO, A is selected from the group consisting of a (C1-6)alkanediyl and a (C3-6)cycloalkanediyl or, if D is N(C0)alkyl-CO, A forms a 4- to 7-membered aliphatic heterocyclic ring with the nitrogen atom of N(C0)alkyl-CO in D, and Ar is a 6-membered aromatic ring with a first hydroxyl group in para-position to D, a second hydroxyl group in meta-position to D, and with at least one electron-withdrawing element and uses thereof.

Abstract: The present invention relates to methods, compositions, and combinations for inhibiting the NLRP3 inflammasome and/or LON protease as well as methods, compositions, and combinations for treating cancer, particularly blood cancer or brain cancer. In certain aspects, the compositions and combinations include a synthetic triterpenoid, such as 1-[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]-4(-pyridin-2-yl)-1H-imidazole (“CDDO-2P-Im”) and 1-[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]-4(-pyridin-3-yl)-1H-imidazole (“CDDO-3P-Im”).

Abstract: Disclosed are bioavailable solid state (17-?)-3-Oxoandrost-4-en-17-yl dodecanoate compositions and methods of use in administration to mammals in need of thereof. The (17-?)-3-Oxoandrost-4-en-17-yl dodecanoate is preferably provided in a solid state crystalline form having a plurality of peaks corresponding to the peaks shown in FIG. 2, a plurality of crystallites ranging in size from about 40 nm to about 60 nm based as identified via powder x-ray diffraction spectra, and a melting point in the range of about 51° C. to about 63° C. The compositions may be provided in oral or injectable administration form for the treatment of conditions such as in need of testosterone therapy.

Abstract: The application relates to a compound of formula (I) containing a thiazole ring, an indazol ring and a 6,7-dihydro-5H-pyrrolo[1,2-c]imidazole ring system, to pharmaceutical compositions containing it and its medical use. The compounds are described as selective allosteric inhibitors of T790M/L858R, T790M/L858R/C797S, L858R, L858R/C797S containing EGFR mutants and thus useful for the treatment of cancer, in particular non-small cell lung cancer.

Abstract: The present invention relates to compounds, and methods of use thereof, capable of entering macrophages. The invention further relates to compounds capable of modulating (for example inhibiting) the activity of the mammalian target of rapamycin (mTor), treating mTor-associated diseases, in particular, but not limited to, related to mTor in macrophages. The invention also relates to compounds capable of imaging mTor in a subject, in particular, but not limited to, mTor in macrophages.

Abstract: A refining method of a midbody of latamoxef sodium includes: dissolving 7?-amino-7?-methoxy-3-(5-tetrazolyl)thiomethyl-1-oxa-3-cephem-4-carboxylic acid in dichloromethane, and then dividing into a dichloromethane layer and a water layer; extracting the dichloromethane layer, adding a NaHCO3 solution to stir, and remaining an organic layer after stratification; stirring, crystallizing and filtering the organic layer in turn, to obtain a filtrate, preparing a second powder by stirring the filtrate under conditions of a catalyst and a normal temperature; preparing a first powder by extracting the water layer, dropping the hydrochloric acid to adjust a pH value thereof, performing crystal cultivation and suction filtration after performing cooling, and then performing vacuum drying; combining the first powder and the second powder to prepare the midbody of latamoxef sodium: 7?3-amino-7?-methoxy-3-(5-tetrazolyl)thiomethyl-1-oxa-3-cephem-4-carboxylic acid, which has a yield of 95.6-96.8% and a purity of 99.2-99.5%.

Abstract: The present invention is directed to compounds of Formula (I), which includes enantiomer and diasteromers thereof: The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.

Abstract: LSD derivative compounds and polymorphs thereof, methods for their synthesis, compositions and treatment of diseases and disorders are described herein, the compounds having the structure of Formula I: including pharmaceutically acceptable salts, hydrates, solvates, tautomers, enantiomers, diastereomers, racemates, polymorphs or combinations thereof; wherein: R1 to R14 are each independently selected from H, or a substituted or unsubstituted hydrocarbon group and X is selected from a halo group.

Abstract: The present invention relates to Compounds of Formula (I): Formula (I) and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, R3, Ra, Rb, A and B are as defined herein. The present invention also relates to compositions comprising at least one compound of Formula (I), and methods of using the compounds of Formula (I) for treating or preventing HIV infection in a subject.

Abstract: The present application provides compounds of Formula (Ia), or an enantiomer, diastereomer, stereoisomer, or pharmaceutically acceptable salt thereof, which act as protein degradation inducing moieties for one or more of cyclin-dependent kinase 8 (CDK8) and cyclin-dependent kinase 19 (CDK19). The present application also relates to methods for the targeted degradation of CDK8 and/or CDK19 through the use of the compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK8 and/or CDK19 which can be utilized in the treatment of disorders modulated by CDK8 and/or CDK19.

Abstract: Disclosed are a Crystal Form (I) of a pyrimidine sulfonamide compound and a preparation method therefor. The present disclosure relates to an application thereof in the preparation of a medicament for treating diseases related to ETA receptor antagonists.

Abstract: Macrocyclic Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, and Formula VIII or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

Abstract: Disclosed are a glycerol derivative that is useful for improving, preventing or treating inflammation-related diseases by inhibiting overexpression of various inflammatory cytokines such as IL-4, IL-6 and so on, or chemokine CXCL8 and reducing migration of HL-60 cell lines, preparation method therefor, and an immunomodulator containing the same as active ingredient. It includes a glycerol derivative represented by Chemical formula 2 or 3 in the specification.

Abstract: The present invention relates to a compound of formula I or a pharmaceutically acceptable salt, a solvate, an active metabolite, a polymorph, an ester, an optical isomer or a prodrug thereof, a pharmaceutical composition comprising the compound of formula I, and use of the compound, as a Bruton's tyrosine kinase inhibitor with high selectivity for BTK(C481S) mutant, in the manufacture of a medicament for preventing or treating a heteroimmune disease, an autoimmune disease or a cancer.

Abstract: Disclosed are stable dosage forms for oral administration of active pharmaceutical ingredients in which any unpleasant taste sensation, caused by release of the active pharmaceutical ingredient and/or of the excipients in the oral and pharyngeal cavity of the patient, is masked by the use of theobromine-free cocoa.

Abstract: An object of the present invention is to provide a compound and a pharmaceutical composition which exhibit strong antibacterial activity against Gram-negative bacteria and drug-resistant Gram-negative bacteria. A compound represented by General Formula [1](the reference signs in Formula have the same definitions as those described in the present specification) or a salt thereof has strong antibacterial activity against Gram-negative bacteria such as Pseudomonas aeruginosa and drug-resistant Gram-negative bacteria including multidrug-resistant Pseudomonas aeruginosa, and the pharmaceutical composition containing the compound or a salt thereof is useful as an antibacterial agent.

Abstract: The present invention is directed to 5-oxo-1,2,3,5,8,8a-hexahydroindolizine-3-carboxamide derivatives, stereoisomers, isotopologues, and pharmaceutically acceptable salts thereof The present invention is also directed to pharmaceutical compositions containing such compounds and the use of such compounds in the treatment and/or prophylaxis of thromboembolic disorders, inflammatory disorders and diseases or conditions in which plasma kallikrein activity is implicated.

Abstract: Provided is a substituted piperidine compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as a prophylactic or therapeutic agent for narcolepsy.

Abstract: Disclosed herein are heterocyclic compounds that inhibit the binding of menin and MLL or MLL fusion proteins. Also described are specific inhibitors of menin-MLL interaction. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the menin-MLL inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, leukemia and other diseases or conditions dependent on menin-MLL interaction.

Abstract: Described herein are compounds represented by formulas (IA) or (IB) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables R1, R3, R4, Y1, Y2, Ar, Z and n are as defined herein.