Abstract: The present invention relates to co-crystals comprising levothyroxine and a dicarboxylic acid, preferably L-tartaric acid or oxalic acid, and processes for the preparation thereof. Furthermore, the invention relates to a pharmaceutical composition comprising a co-crystal of the present invention, preferably the co-crystal comprising levothyroxine and L-tartaric acid or oxalic acid, and at least one pharmaceutically acceptable excipient. The pharmaceutical composition of the present invention can be used as a medicament, in particular for the treatment of hypothyroidism.

Abstract: The present invention relates to the discovery of novel N-(substituted)-1H-1,2,4-triazole-3-carboxamide compounds capable of inhibiting DksA activity in a bacteria cell. In certain embodiments, the compounds are capable of killing or weakening bacteria. In another aspect, the invention relates to methods of treating bacterial infection in a subject in need thereof, the method comprising administering to the subject a compound of the invention.

Abstract: Provided herein are compounds that can inhibit the replication of influenza viruses, reduce the amount of influenza viruses, and/or treat influenza.

Abstract: The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I) In the formula Q is O, R1 is the side chain of Ser, R2 is —CO-Thr, R3 is the side chain of Asn or Glu, and R4, R5 and R6 are each H.

Abstract: Disclosed are compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.

Abstract: Provided is a pharmaceutical composition for treating malignant peripheral nerve sheath (MPNST), including a benzenesulfonamide derivative and a pharmaceutically acceptable carrier. Also provided is a method for treating canine MPNST by administering the pharmaceutical composition to a subject in need thereof.

Abstract: A complex salt formed from a compound of formula (I) and an alkaloid, a preparation method therefor and use thereof are provided. In particular, a complex salt formed from rupestonic acid and matrine, oxymatrine, sophocarpine and sophoridine, or a composition thereof, has potential efficacy in treating a tumor/cancer or preparing related medicaments.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, ester, stereoisomer, tautomer, solvate, hydrate, or combination thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcohol steatohepatitis disease (NASH).

Abstract: The present disclosure relates to compounds of Formula (I): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.

Abstract: The present invention relates to a combination treatment which comprises (a) at least one ERK inhibitor preferably Compound B as described herein, and (b) a c-RAF inhibitor or a pharmaceutically acceptable salt thereof, preferably Compound A, which may be combined into a single pharmaceutical composition or prepared for separate or sequential administration. It includes a c-RAF inhibitor and an ERK inhibitor prepared for simultaneous, separate or sequential administration for the treatment of a proliferative disease, particularly an advanced solid tumor that harbors a Mitogen-activated protein kinase (MAPK) alteration, and includes methods of using these compounds in combination as well as a commercial package comprising such combination.

Abstract: The present invention provides an intermediate for synthesizing a TGF-? inhibitor represented by Chemical Formula 1 and an improved method for preparing the TGF-? inhibitor represented by Chemical Formula 1 using the same. The preparation method according to the present invention can not only allow inexpensive and safe reagents to be used, but also simplify the synthesis steps and purification methods to improve the reaction yield, thereby maximizing the production efficiency of the TGF-? inhibitor represented by Chemical Formula 1 to be used usefully for mass production.

Abstract: The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, such as a compound of Formula I: or a tautomer, stereoisomer, mixture of stereoisomers, hydrate, solvate, isotopically enriched analog, or pharmaceutically acceptable salt thereof, to products containing the same, as well as to methods of their use and preparation.

Abstract: The present invention relates to a novel process for preparing substituted cyclohexane amino acid esters and spiroketal-substituted cyclic keto-enols, and to novel intermediates or starting compounds that are passed through or used in the process according to the invention.

Abstract: The disclosure provides crystalline and amorphous forms of aticaprant. Also provided by the disclosure are pharmaceutical compositions comprising the amorphous or crystalline forms, methods of treating major depressive disorder using the amorphous or crystalline forms of aticaprant, amorphous or crystalline forms of aticaprant for use in the treatment of major depressive disorder in a human patient having anhedonia, uses of the amorphous or crystalline forms of aticaprant in the manufacture of a medicament for the treatment of major depressive disorder, and packages or pharmaceutical products comprising (i) amorphous or crystalline forms of aticaprant and (ii) instructions for treating major depressive disorder. In some aspects, the human patient treated as described herein has anhedonia.

Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, R5 and are as defined in the description.

Abstract: The present invention relates to a ubiquitin-specific peptidase 24 inhibitor, a medicinal composition and a method of delaying or reversing multidrug resistance in cancers using the same. The USP24 inhibitor, which includes a shUSP24 RNA and/or a carbonyl substituted phenyl compound, can serve as a chemosensitizing agent for inhibiting the drug pump out, cancer stemness and genomic instability of cancer cells, thereby being applied to a medicinal composition and a method for delaying or reversing multidrug resistance in cancers.

Abstract: Disclosed herein are compounds of formula (I): and salts thereof. Also disclosed are compositions comprising compounds of formula I and compounds of formula I for use in treating or preventing bacterial infections.

Abstract: The present invention provides novel compounds having the general formula (I) wherein R1 to R6, and m are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The present invention provides a compound of Formula (I) Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.

Abstract: The present invention provides a novel compound for effectively preventing nerve damage and protecting nerves, and a preparation method thereof. Besides, the present invention also provides a pharmaceutical composition comprising the novel compound, and a use of the novel compound for preventing nerve damage and protecting nerves.