Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, Ra, Rb, Q1, and Q2 are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-?-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

Abstract: The present disclosure provides methods and formulations for reducing ammonia and carbon dioxide emissions from a bovine using lubabegron, or a physiologically acceptable salt thereof. The present disclosure also provides bovine feed additives and bovine feed compositions.

Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

Abstract: Methods for inhibiting cell growth, inhibiting DNA polymerase activity, and inhibiting DNA replication and repair are provided. In a method of inhibiting cell growth, a cell, such as a cancer cell, is contacted with zelpolib or a derivative or pharmaceutically acceptable salt thereof. The cell growth can be inhibited in vivo, and in certain embodiments, the cell growth is inhibited in vitro. In a method for inhibiting DNA polymerase activity, a DNA polymerase is contacted with zelpolib or a derivative or pharmaceutically acceptable salt thereof. In certain embodiments, the DNA polymerase is Pol ?. In a method for inhibiting DNA replication and repair, a cell, such as a cancer cell, is contacted with zelpolib or a derivative or pharmaceutically acceptable salt thereof. The DNA replication and repair can be inhibited in vivo, and in certain embodiments, the DNA replication and repair is inhibited in vitro.

Abstract: The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.

Abstract: Use of imeglimin for the prevention and/or treatment of hepatocellular carcinoma.

Abstract: The present invention describes the combination of a 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine or of a pharmaceutically acceptable salt or solvate thereof with fluoxetine or a pharmaceutically acceptable salt or solvate thereof, for use for treating a synucleinopathy such as Parkinson's disease, Lewy body disease, mutations in the glucocerebrosidase gene, or multiple system atrophy.

Abstract: The present invention is directed to heteroarylpiperidine ether compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

Abstract: A 7H-azulene [1,2,3-i,j] isoquinolin-7-one compound, a single crystal and a use thereof are provided. The compound has a structure as shown in a formula (I). The present invention obtains a crude extract of Acorus calamus L., then extracts with different polar solvents in sequence and separates column chromatography to obtain a novel alkaloid compound, which is expected to be developed into a novel class of drug exerting neuroprotective effects, so as to prevent and treat senile dementia, stroke and epilepsy diseases.

Abstract: Provided herein are arylcyclopropyl amino-isoquinoline amide compounds. In particular, the disclosure provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the disclosure are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, diseases characterized by abnormal growth, such as cancers, and inflammatory diseases. The disclosure further provides compositions containing isoquinoline amide compounds.

Abstract: Methods for treating Shiga toxicosis, caused by infection with Shiga toxin bacteria, are provided. The methods include administering to a subject in need thereof an effective amount of one or more active agents selected from tamoxifen, 4-hydroxytamoxifen, endoxifen, toremifene, raloxifene, bazedoxifene, and pharmaceutically acceptable salts thereof. In some embodiments, the methods further include the administration of an antibiotic or a manganese compound to the subject. Pharmaceutical compositions for the treatment of Shiga toxicosis are also described.

Abstract: Provided herein are methods of using KRAS G12C inhibitors. These methods of using the inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof. wherein R1 is —C(?O)O-alkyl, carbonate ester, or —C(?O)-alkyl, ester, or —C(?O)N-alkyl, carbamate ester and wherein R2 is —CH3 or —CD3. The alkyl ester can contain saturated or unsaturated C12 to C26 alkyl carbon. The alkyl carbon chain can have either a straight, branched, noncyclic, cyclic, unsubstituted or substituted structure.

Abstract: The present invention relates to the technical field of chiral synthesis, and specifically provides a new type of oxa-spirodiphosphine ligands. The bisphosphine ligand is prepared with oxa-spirobisphenol as a starting material after triflation, palladium catalyzed coupling with diaryl phosphine oxide, reduction of trichlorosilane, further palladium catalyzed coupling with diaryl phosphine oxide, and further reduction of trichlorosilane. The oxa-spiro compound has central chirality, and thus includes L-oxa-spirodiphosphine ligand and R-oxa-spirodiphosphine ligand. The racemic spirodiphosphine ligand is capable of being synthesized from racemic oxa-spirobisphenol as a raw material. The present invention can be used as a chiral ligand in the asymmetric hydrogenation of unsaturated carboxylic acids. The complex of the ligand with ruthenium can achieve an enantioselectivity of greater than 99% in the asymmetric hydrogenation of methyl-cinnamic acid.

Abstract: Disclosed are new polycyclic carbogenic molecules and their methods of synthesis. The new polycyclic carbogenic molecules may be utilized in anti-cancer therapies. In particular, the polycyclic carbogenic molecules may be formulated as pharmaceutical compositions that comprise the small molecules, which compositions may be administered in methods of treating and/or preventing cell proliferative diseases and disorders such as cancer. The new polycyclic carbogenic molecules may be prepared from vinyl- or allyl-substituted cyclohexenone precursors via preparation of a silyl bis-enol ether intermediate.

Abstract: Disclosed are a compound as a selective JAK inhibitor, and an isomer, a solvate or a pharmaceutically acceptable salt thereof, wherein: the definitions of (A), R, R1 and n are described in detail in the specification. In addition, also disclosed are a medicament including the compound and salts thereof as an active ingredient, and the use thereof in the preparation of a medicament for treating JAK-related target diseases, such as immune system diseases, rheumatoid arthritis and tumors.

Abstract: Provided, in part, are compounds of Formula I: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of conditions associated with the activity of sodium channels. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein.

Abstract: The invention relates to novel compounds of the formula (I) in which the R1, R2a, R2b, R3, A1, A2, A3, A4, A5 and n radicals are each as defined above, to the use thereof as acaricides and/or insecticides for controlling animal pests and to processes and intermediates for preparation thereof.

Abstract: The present invention provides a compound having an MAGL inhibitory action, and expected to be useful as an agent for the prophylaxis or treatment of neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, traumatic brain injury, glaucoma, multiple sclerosis etc.), anxiety disorder, pains (e.g., inflammatory pain, cancerous pain, neurogenic pain etc.), epilepsy, depression and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof.

Abstract: The present disclosure relates to choline salts, and crystalline forms thereof, of a compound which is N—((S-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bS,4aR)-5,5-difluoro-3- (trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment and prevention of a Retroviridae viral infection including an infection caused by the HIV virus.