Abstract: The present disclosure provides crystalline solid forms, spray-dried dispersions and pharmaceutical compositions, including solid oral dosage forms, of (S)-1-(5-[2H,3H-[1,4]dioxino[2,3-b]pyridine-7-sulfonyl]-1H,2H,3H,4H,5H,6H-pyrrolo[3,4-c]pyrrol-2-yl)-3-hydroxy-2-phenylpropan-1-one (“Compound 1”), and preparation methods thereof.

Abstract: An object of the present invention is to provide an agent for enhancing fertilization function of a mammal sperm, which comprises a low molecular compound which can be produced relatively easily and inexpensively as an active ingredient, and a method for enhancing fertilization function of a mammal sperm and a method for preparing a mammal fertilized egg, which use a low molecular compound which can be produced relatively easily and inexpensively. An agent comprising one or more compounds selected from the group consisting of compounds of the following formula (I0), formula (II), and formula (III), and physiologically acceptable salts thereof when R3 is OH is used as an agent for enhancing fertilization function of a mammal sperm.

Abstract: Disclosed in certain embodiments is a method of treating respiratory depression modulated by a non-opioid agent comprising administering, to a patient in need thereof, an effective amount of a compound selected from Formula (I) as disclosed herein.

Abstract: Sustained-release abiraterone prodrug formulations, methods, and kits for parenteral administration to a subject having a sex hormone-dependent benign or malignant disorder such as prostate cancer, a syndrome due to androgen excess, and/or a syndrome due to glucocorticoid excess such as hypercortisolemia.

Abstract: The invention relates to a kinase inhibitor, in particular an inhibitor of protein kinases including the protein-tyrosine kinases LCK, ABL, SRC, KIT, SIK-family and/or their mutants. Although structurally similar to dasatinib, the kinase inhibitor of the invention displays, eg functional and ADMET properties distinct to dasatinib. Also, the invention relates to pharmaceutical compositions that comprise the kinase inhibitor, including those formulated for oral administration, such as in unit dose form that comprise particular ranges or amounts of the kinase inhibitor. The kinase inhibitor or pharmaceutical composition may be used in the treatment of a proliferative disorder, such as a leukaemia or solid tumour.

Abstract: A N-heterocyclic five-membered ring-containing capsid protein assembly inhibitor, and a pharmaceutical composition and use thereof, specifically relating to a compound as represented by formula I, a stereoisomer, a tautomer, a geometrical isomer, a solvate, an active metabolite, a hydrate, a prodrug or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and a medical use thereof. The medical use comprises the use in treating diseases benefiting from the capsid protein assembly inhibitor, and in particular, diseases caused by hepatitis B virus infection.

Abstract: The present application relates to a linker containing arylnitro, an antibody-drug conjugate the linker and use of the linker, as well as a pharmaceutical composition comprising the antibody-drug conjugate and use of the antibody-drug conjugate for treatment and/or prevention of a disease

Abstract: The present disclosure relates to a manufacturing method for 4-methoxypyrrole derivatives. The embodiment of the present disclosure is useful for industrial mass production of 4-methoxypyrrole derivatives, because the process efficiency and yield are improved, and the use of hazardous reagents and environmental polluting reagents is avoided.

Abstract: Provided are a salt form of an estrogen receptor down-regulator, a crystalline form thereof, and a preparation method therefor

Abstract: The present document describes methods of using compositions for inhibiting biofilm formation, or disrupting existing or developing biofilms in a subject, which composition comprises at least one chromophore and a pharmacologically acceptable carrier.

Abstract: The present invention provides methods of efficiently producing various optically active aromatic amino acid derivatives by reacting, using an additive, a specific ester compound with an aromatic halide and zinc in the presence of a catalyst. The present invention also provides amino acid derivatives that can be produced by the methods.

Abstract: The present disclosure relates generally to Cyclin-dependent kinase 2 (CDK2) inhibiting chemical compounds and uses thereof in the inhibition of the activity of CDK2. The disclosure also provides pharmaceutically acceptable compositions comprising compounds disclosed herein and methods of using said compounds and compositions in the treatment of various disorders related to CDK2 activity.

Abstract: One embodiment of the disclosure is a compound represented by Formula I or a pharmaceutically acceptable salt thereof. The variables in Formula I are defined herein. Compounds of Formula I are selective MAP4K1 inhibitors, which can be used to treat a diseases or disorders in a subject that benefits from control of MAP4K1 activity.

Abstract: There is herein provided a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein the ring containing Q1 to Q5, and the groups R1, R2 and R3, have meanings as provided in the description.

Abstract: The invention provides a method for producing a dichloro addition product of an aliphatic olefin by photocatalysis under visible light. The method includes reacting an aliphatic olefin as a substrate with hydrochloric acid as a chlorine source in an organic solvent under visible light irradiation in the presence of copper chloride with visible light absorption ability as a catalyst, to obtain the dichloro addition product of the aliphatic olefin, wherein the reaction is carried out under an oxygen-containing atmosphere, the aliphatic olefin comprises a carbon-carbon double bond and a C9-C15 aliphatic chain connected to the carbon-carbon double bond by a covalent bond. In the invention, visible light is used to provide the energy and a transition metal chloride with visible light absorption ability is used to undergo light-induced electron transfer from chloride with a reaction substrate, thereby initiating an addition reaction to obtain a dichloro addition product.

Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5, R23, R24, L, A and B are as defined in claim 1, or pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as cytochrome P450 monooxygenase 11A1 (CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as prostate cancer.

Abstract: Improving the solubility of an organic compound. A cocrystal of (1) 6-ethyl-N-[1-(hydroxyacetyl)piperidin-4-yl]-1-methyl-4-oxo-5-(2-oxo-2-phenylethyl)-3-(2,2,2-trifluoroethoxy)-4,5-dihydro-1H-pyrrolo[3,2-c]pyridine-2-carboxamide and (2) L-malic acid or L-tartaric acid.

Abstract: Disclosed herein are compounds, 3,4,6,8-substituted-2-([1,1?-biphenyl]-4-yl)quinoline analogs, that are inhibitors of dihydroorotate dehydrogenase (DHODH) with improved pharmacokinetic properties. The disclosed compounds can be used in the treatment of a variety of disorders and diseases in which inhibition of DHODH can be clinically useful, including cancer, such as a hematological cancer, including acute myeloid leukemia (AML); graft-versus-host-diseases; autoimmune disorders; and disorders associated with T-cell proliferation. The disclosed compounds can demonstrate flip-flop kinetics when administered orally, i.e., pharmacokinetics in which the rate of absorption, rather than the rate of elimination, dominates the pharmacokinetics. The disclosed compounds can demonstrate a sustained pharmacokinetic profile instead of an immediate release profile. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

Abstract: Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X1, X2, X3, X4, Y, A, L1, L2, R1, R2, R5, m and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

Abstract: The present application discloses a synthesis method of chiral nicotine from nicotinate and ?-butyrolactone, including the following steps: Step S1: performing condensation under an alkaline condition, and performing ring opening reaction with hydrochloric acid; Step S2: reacting with (+)—B-diisopinocampheyl chloroborane to produce a chiral hydroxyl group; Step S3: performing a chlorination reaction; and Step S4: performing cyclization under an alkaline condition to obtain the chiral nicotine. In the present application, nicotinate and ?-butyrolactone, both cheap and readily available, are used as raw materials, so as to reduce the production cost of (S)-nicotine. (+)—B-diisopinocampheyl chloroborane is used to reduce a carbonyl group of an intermediate to obtain a target chiral center.