Abstract: The present invention relates to compounds of general Formula (I), and/or tautomers, enantiomers, solvates, hydrates, and pharmaceutically acceptable salts thereof. The present invention also relates to compounds of Formula (I) for use in therapy, methods of treating isoprenylcysteine carboxyl methyltransferase (ICMT) related disorders or uses of compounds of Formula (I) in the manufacture of a medicament for the treatment of ICMT-related disorders, wherein the disorder is cancer and/or progeria. The present invention further relates to processes for synthesizing compounds of Formula (I).

Abstract: The present application relates to compounds of Formula I comprising an antibody binding domain (ABD) comprising a hapten that binds to an antibody in a subject, the antibody comprising a hapten binding site, an antibody labelling domain (ALD) comprising a functional group that forms a covalent bond with an amino acid in the antibody that is proximal to the hapten binding site and the formation of the covalent bond results in elimination of the ABD and either a target binding domain (TBD) or a detection moiety domain (DMD), each domain being optionally connected with independently selected linkers. The present application also includes methods and uses of the compounds, for example, for immune recognition of target cells by recruited labelled antibodies.

Abstract: Improved methods and intermediates thereof for preparing substituted 4-amino-1H-imidazo[4,5-c]quinoline compounds are described. These compounds are useful as NLRP3 modulators.

Abstract: The present invention relates to an improved process for the preparation of 4-amino-N-tert-butyl-4,5-dihydro-3-isopropyl-5-oxo-1H-1,2,4-triazole-1-carboxamide (Amicarbazone). The present invention more particularly relates to an improved process for the preparation of 4-amino-N-tert-butyl-4,5-dihydro-3-isopropyl-5-oxo-1H-1,2,4-triazole-1-carboxamide (Amicarbazone) by coupling of 4-Amino-2,4-dihydro-5-(1-methylethyl)-3H-1,2,4-triazol-3-one (TAZ) and poor quality tert-Butyl isocyanate (TBIC) with purity less than or equal to 98%, preferably less than or equal to 85%.

Abstract: DCAF15 is a substrate recognition (adaptor) protein of E3 ubiquitin ligase. Disclosed herein are compounds that recruit ubiquitin ligase CRL4DCAF15, to a target RNA recognition motif (RRM), causing its degradation. Also disclosed herein are compositions and methods of use in treating associated disorders and diseases.

Abstract: The aim is to provide a novel compound that can luminesce with high brightness and be used as a luminescent substrate in a firefly bioluminescence system. Provided is a heterocyclic compound, or salt thereof, represented by the following general formula (1): [R1, R2, and R3 are independently hydrogen or an alkyl group having a carbon number of 1-4, with provisos that R1 and R2 are optionally bonded to form a ring and that one of R1 and R2 is optionally bonded to Y1 to form a ring; X is S, O, NR4, or CH2, and Y1 and Y2 are independently N or CR4, where each R4 is independently hydrogen, an alkyl group having a carbon number of 1-4, an alkenyl group having a carbon number of 2-4, or an acyl group having a carbon number of 2-4; n is an integer of 0-4].

Abstract: The present invention relates to preparation of pyrazoles. This invention further relates to a continuous flow micro-total process system for preparation of celecoxib, a COX-2 selective non-steroidal anti-inflammatory drug, and analogs thereof.

Abstract: The present invention provides substituted pyrazole compounds, compositions containing same, and use thereof. The substituted pyrazole compounds comprise a compound represented by formula (I) or a tautomer, stereoisomer, prodrug, crystalline form, pharmaceutically acceptable salt, hydrate, or solvate thereof. The compound represented by formula (I) can serve as a tissue selective androgen receptor modulator (SARM), particularly serving as a drug for treating prostate cancer and other AR-dependent conditions and diseases in which AR antagonism is desired.

Abstract: The present invention concerns substituted indoline derivatives, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.

Abstract: Compounds, compositions and methods are provided for modulating the activity of EP2 and EP4 receptors, and for the treatment, prevention and amelioration of one or more symptoms of diseases or disorders related to the activity of EP2 and EP4 receptors. In certain embodiments, the compounds are antagonists of both the EP2 and EP4 receptors.

Abstract: The present disclosure relates to novel crystalline forms of tafamidis (hereinafter referred to as compound I) and processes for preparation thereof. The present disclosure also relates to pharmaceutical composition containing the novel crystalline forms, use of the novel crystalline forms for preparing drugs treating disease caused by transthyretin-mediated amyloidosis. The crystalline forms of tafamidis of the present disclosure have one or more improved properties compared with crystalline forms of prior art and have significant value for future drug optimization and development.

Abstract: The invention generally relates to methods of coupling a carbon containing moiety to an amine containing moiety.

Abstract: The present invention relates to carbamoyl phenylalaninol compounds and methods of using the same to treat disorders.

Abstract: The present invention is directed to novel aminobenzimidazole derivatives. The present invention is also directed to methods of treating a histone deacetylase (HDAC)-associated disease or inhibiting the histone deacetylating activity of a HDAC isoform in a cell or with one or more of the aminobenzimidazole derivatives.

Abstract: The disclosure relates to crystalline forms of bis(4-hydroxy-N-methyl-N-isopropyltryptammonium) fumarate (“crystalline bis-miprocin fumarate”), compositions containing that crystalline form, and their methods of treatment using them.

Abstract: Disclosed herein are compositions and methods for modulating cereblon neosubstrates. A small molecule modulator of Formula (I*), or a pharmaceutically acceptable salt or solvate thereof can be used to modulate cereblon neosubstrates.

Abstract: Described herein are compounds of formula (I) as defined herein, which comprise a greater proportion of deuterium to protium than naturally found in hydrogen; and compositions, including pharmaceutical compositions, comprising these compounds and optionally analogous compounds of formula (I), which are not deuterium-enriched. These compounds and compositions are of use in therapy, in particular in the treatment of psychiatric or neurological disorders. Varying the amounts of the different compounds within the compositions of the invention allows tailoring of the compositions' therapeutic effects. A particularly efficient synthetic method which enables compounds of formula (I) and related compounds of formula (I?) is also provided.

Abstract: The present invention relates to a novel near-infrared fluorescent probe having specificity for mitochondria due to a hydrophobic group attached to a silicon-rhodamine core, and the use thereof for mitochondrial detection and cancer diagnosis. The fluorescent probe of the present invention has improved mitochondrial targeting efficiency compared to conventional probes due to a hydrophobic group attached to a silicon-rhodamine core, can detect mitochondria in living tissue with high sensitivity and specificity in a near-infrared (NIR) region (700 to 1,700 nm), and can acquire three-dimensional high-resolution biological images without harming the human body. Due to these advantages, the fluorescent probe can be used not only for mitochondrial detection in cells in the laboratory, but also as a contrast agent or a drug delivery carrier in cancer diagnosis and surgery.

Abstract: The present invention relates to N-aromatic amide compounds with formula (I) and/or (II) and preparation methods therefor, pharmaceutical compositions and pharmaceutical formulations containing the compounds with formula (I) and/or (II), and use of the compounds with formula (I) and/or (II) in preparing a medicament for the treatment of diseases related to androgens. The definitions of R1, R2, R3, R4, R5, R6, W1, W2, W3, W4 and W5 in the formula are the same as those in the description. The compounds with the formula (I) and/or (II) are capable of binding to the androgen receptors and have activity for anti-androgen and degrading androgen receptor. The compounds can be used alone or as compositions for the treatment of various androgen-related diseases such as prostate cancer, prostate hyperplasia, breast cancer, bladder cancer, ovarian cancer and the like, and also for the treatment of acne, hirsutism, psilosis and other diseases.

Abstract: Mcl-1 selective inhibitors, Bcl-2 selective inhibitors, and Mcl-1/Bcl-2 dual inhibitors and methods of using the same for the treatment of disease are disclosed.