Abstract: The present invention relates to a process for the preparation of 2H-benzotriazole compounds and congeners, novel 2H-benzotriazole compounds and congeners and their use as UV absorbers in coatings and bulk plastics.

Abstract: The invention relates to compounds of formula (I): or a salt or solvate thereof, wherein the variables are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are antagonists of toll-like receptors such as TLR7, TLR8 and/or TLR9 that are useful for inhibiting immune response and treating diseases associated with undesirable immune response.

Abstract: The invention provides novel compounds having the general formula I: wherein R1, RB1, RB2, n, p, q, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.

Abstract: The present invention relates to a process for the synthesis of 5-(4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)piperidin-1-yl)-1H-1,2,4-triazol-3-amine in two hydrated crystalline forms and in one anhydrous crystalline form. The present invention further relates to methyl (Z)-4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)-N-cyanopiperidine-1-carbimidothioate which is an intermediate in this process.

Abstract: Provided are embodiments of para-substituted 1,1-dialkyl-4-phenylpiperazin-1-ium iodides advantageous for modulating inflammation that have been synthesized and their electrophysiology activities for ?9, ?9?10, and ?7 nAChRs compared. The para position contained alkyl or aryl amides, or heterocyclic isosteres for the amide, and the alkyl groups were varied at the ammonium piperazine nitrogen to see if compensatory changes in size at this position of the molecule impacted function. The compounds were characterized with two-electrode voltage-clamp measurements on Xenopus oocytes expressing nAChRs. General, the compounds were more potent for ?9-containing receptors than for ?7, and the majority were either full or strong partial agonists for ?9-containing nAChR.

Abstract: Disclosed herein are compounds which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer.

Abstract: The invention provides a method comprising hydrogenating a ketone in the presence of (i) a base, (ii) hydrogen gas and (iii) a catalyst comprising a charged or neutral complex of formula (I): wherein: Mn is a manganese atom or a manganese ion in oxidation state (I) to (VII); R1 and R2 are each independently optionally substituted C4-8monocyclic aryl or C3-7monocyclic heteroaryl moieties; -Fc- denotes a ferrocene (bis(?5-cyclopentadienyl)iron) moiety covalently bonded via adjacent carbon atoms of one of the two cyclopentadienyl moieties, and which may be optionally further substituted, in either cyclopentadienyl ring; —Z— is an alkylene linker of the formula —(CH2)1-6— in which one or more of the hydrogen atoms of the alkylene may be independently substituted; —Nx is an optionally substituted nitrogen-containing heteroaryl moiety, with the proviso that at least one of R1, R2 and —Nx is substituted one or more times with an electron donating group; and L1-L3 constitute one, two or three ligands, wherein,

Abstract: A combination therapy including one or more compounds of formula (I): wherein R represents hydrogen, halo, cyano, C1-4 haloalkyl, C1-4 haloalkoxy, or SO2NR5R6, R1a and R1b independently represent hydrogen or halo; R2 represents hydrogen, halo, cyano, C1-4 alkyl, C1-4 alkoxy, or C1-4 haloalkoxy; R3 represents halo, cyano, C1-4 alkyl, or C1-4 hydroxyalkyl; R4 represents hydrogen or C1-4 alkyl; X represents CH or N; Y represents N or CH which carbon atom may optionally be substituted by R, R1a or R1b; R5 and R6 independently represent hydrogen or C1-4 alkyl; or a pharmaceutically acceptable salt thereof; and a second or further active ingredient.

Abstract: Compounds belonging to the group of N-benzyl-2-(4-(4-substituted-1H-1,2,3-triazol-1-yl)phenylacetamides have cytotoxic activities against MCF7 breast cancer cells, and are useful in therapeutic regimes for breast cancer. The N-benzyl-2-(4-(4-substituted-1H-1,2,3-triazol-1-yl)phenylacetamides also have beneficial effects on BAX, BCL-2, MCL-1 and MAPK pathways within MCF& breast cancer cells.

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.

Abstract: The present disclosure relates to crystalline forms of N-{3-[1-(2-nitrophenyl)-1H-pyrrol-2-yl]-allylidene}-aminoguanidinium salts having high solubility. The disclosure also relates to use of said crystalline forms in medicine.

Abstract: Provided is an imidazotriazine thiobenzamide derivative of formula (I), A preparation method for the imidazotriazine thiobenzamide derivative, and a use of the imidazotriazine thiobenzamide derivative or an isomer, a pharmaceutically-acceptable salt, or a prodrug thereof in the preparation of drugs for the treatment of cancer are also provided.

Abstract: The present invention relates to peptide conjugates of microtubule-targeting agents such as maytansinoid derivatives which are useful for the treatment of diseases such as cancer.

Abstract: The present invention relates to sulfonamides and related compounds which are inhibitors of PARG and are useful in the treatment of cancer.

Abstract: The present disclosure relates to derivatives of bicyclic compounds and their uses in therapy. In particular, the present disclosure relates to derivatives of bicyclic compounds for use in modulating kinase enzymatic activity and accordingly modulating kinase-dependent diseases and conditions such as cancer and in specific embodiments, hepatocellular carcinoma (HCC). The present disclosure also relates to methods of synthesizing these compounds.

Abstract: Compounds that are inhibitors of at least one of ARG1 and ARG2, and compositions containing the compounds and methods for synthesizing the compounds, are described herein. The use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by ARG1 and ARG2 are also described herein.

Abstract: A compound of Formula I includes a stereoisomer thereof and/or a salt thereof; wherein R1 is a substituted alkane group, a heterocylic group, or a pyridine group; X is hydrogen, a halogen, an amino acid residue, a substituted amino acid residue, an alkyl group, or an ester.

Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof and their use in methods for the alleviation and/or treatment of visceral pain, for example abdominal pain; pelvic pain; male pelvic pain; pain from an internal organ; bladder pain; painful bladder syndrome; post-surgical abdominal pain (e.g., GI resection, hysterectomy, oophorectomy, C-section, and the like); or pain arising from or related to: pancreatitis (e.g., chronic pancreatitis), prostatitis (e.g., chronic prostatitis), inflammatory bowel disease (e.g., Crohn's disease), endometriosis, interstitial cystitis, prostatitis (e.g., chronic prostatitis), epididymitis (e.g., chronic epididymitis), or post-surgical abdominal lesions. In some embodiments, the visceral pain is consequent to inflammatory bowel disease, for example Crohn's disease.

Abstract: The present application discloses a method for identifying an agent for the treatment or prevention of cancer or metastatic cancer comprising the steps of contacting stem cell with a potential agent, and identifying an agent that induces differentiation, or inhibits stem cell pluripotency or growth of the stem cell, wherein such agent is determined to be an anti-cancer agent.

Abstract: Provided are systems and methods for continuously administering to a subject in need of treatment a formulation comprising an immunomodulatory imide compound. In some embodiments, the method are for use in treating multiple myeloma, transfusion-dependent anemia due to low- or intermediate-1-risk myelodysplastic syndromes, mantle cell lymphoma, hematologic cancers, or solid tumor cancers.