Abstract: The present invention relates to a thienopyrimidine derivative and use thereof in medicine, and also to a pharmaceutical composition containing the compound. The compound or pharmaceutical composition is used for inhibiting acetyl-CoA carboxylase (ACC). The present invention also relates to a method of preparing such compound and pharmaceutical composition, as well as their use in the treatment or prevention of diseases regulated by acetyl-CoA carboxylase in mammals, especially in humans.

Abstract: Described herein are quinoline compounds useful for, among other things, inhibition of the proteasome and for treatment of cancer and inflammation.

Abstract: Indazole sulfonamide derivatives of formula (I), the pharmaceutically acceptable addition salts thereof, the hydrates and/or solvates thereof, and the use of same as inverse agonists of retinoid-related orphan receptor gamma ROR?t are described. Pharmaceutical compositions including such compounds, as well as the use thereof for the topical and/or oral treatment of ROR?t receptor-mediated inflammatory diseases, in particular acne, psoriasis and/or atopic dermatitis are also described.

Abstract: The present application relates to novel binder drug conjugates (ADCs), to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for the treatment and/or prophylaxis of diseases and to the use of these ADCs for preparing medicaments for treatment and/or prophylaxis of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.

Abstract: The present invention relates to various compounds capable of temporarily hardening soft tissue for surgical suturing of the soft tissue. The compounds according to the present invention can temporarily increase the hardness or tension of soft tissue, thereby improving the suturing efficiency during suturing of the soft tissue, thereby preventing aftereffects or the like from occurring due to insufficient anastomosis. In addition, the compounds according to the present invention can temporarily increase the hardness or tension of soft tissue, particularly pancreas, thereby increasing the suturing efficiency during pancreaticoduodenectomy and effectively preventing pancreatic leakage.

Abstract: A novel method for forming a metal-carbene bond is disclosed.

Abstract: The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.

Abstract: Provided are compounds useful for treating of cancer and methods for treating of cancer, comprising administering to a subject in need thereof a compound described therein.

Abstract: Processes for the preparation of dolutegravir and pharmaceutically acceptable salts utilizing alkenylamine are disclosed. Intermediates in those synthetic schemes are also disclosed.

Abstract: Calprotectin inhibitors and derivatives thereof, and methods of using them for inhibiting or reducing metastatis and treating cancer are provided. The pharmaceutical formulations prepared from the compounds can be used in the treatment of cancer either as a single agent or in combination with at least one other cancer therapeutic, chemotherapeutic or anti-cancer agent.

Abstract: The present disclosure relates to an organic electroluminescent compound and an organic electroluminescent device comprising the same. The organic electroluminescent compound of the present disclosure provides an organic electroluminescent device having high efficiency and/or long lifespan.

Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

Abstract: The present application provides solid forms of (R)-6-(2-fluorophenyl)-N-(3-(2-(2-methoxyethylamino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride, and methods of preparing and using same.

Abstract: The invention relates to a combination of a first compound selected from N-(3,5-dimethoxyphenyl)-N?-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof; and a second compound which is a cMet inhibitor. The combination is for use in the treatment of a proliferative disorder, in particular for use in the treatment of cancer.

Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R4, R7, A, D, E, F, V, W, X, Y, n, r and q are defined in claim 1, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases, and synthetic intermediates.

Abstract: The invention is directed to functionalized aluminum reagents of formula 1 where R is a linear or branched alkane group containing 1 to 8 carbon atoms, and R1 is phenylene, or a linear or branched alkane diyl group containing 2 to 10 carbon atoms, or a combination of one or more phenylene groups and one or more linear or branched alkane diyl groups containing 1 to 10 carbon atoms; Q is of formula 2 where R3 and R4 are independently phenyl or a linear or branched alkyl group containing 1 to 10 carbon atoms, or R3 and R4 taken together with the nitrogen atom represent a nitrogen containing heterocyclic group containing from 4 to 12 carbon atoms.

Abstract: The present invention is to provide a method of producing a glyceric acid ester which is easy for production and high in yield, and in which a pyridine to be used for the reaction is easily reused. Provided is a method of producing a compound represented by the following formula (II), including a step of oxidatively esterifying Compound A represented by the following formula (I) with Compound B selected from an organic nitroxyl radical, an N-hydroxy form thereof, and a salt containing an oxo ammonium cation of them, and an oxidizing agent in the presence of a pyridine having an alkyl substituent, wherein the use amount of Compound B is 0.0001 or more and 0.1 or less in terms of a molar ratio relative to Compound A: wherein, in the formulae (I) and (II), R1 and R2 each independently represent a hydrogen atom or a monovalent hydrocarbon group, or R1 and R2 are bonded to each other to form a divalent hydrocarbon group for constituting a ring structure.

Abstract: Disclosed herein are methods of treating pulmonary hypertension, including pulmonary arterial hypertension, by administering to a patient in need thereof an effective amount of temozolomide, optionally in conjunction with one or more additional therapeutic agents. Compositions and kits including temozolomide for use in treating pulmonary hypertension, including pulmonary arterial hypertension, are also disclosed.

Abstract: The present invention provides an EGFR kinase inhibitor and a preparation method and use thereof. Specifically, the present invention provides a compound as shown in formula (I), the definition of each group therein being as described in the description. Said compound is an efficient EGFR inhibitor.

Abstract: Compound I and a compound II as well as preparation methods therefor and use thereof are disclosed. A newly synthesized compound of formula I is capable of stimulating congenital immunity and cellular immunity for tumor resistance while greatly improving the antitumor effect of ethacrynic acid (EA), and thus an integrated synergistic anti-tumor dual-immunity drug design is explored. The immune response mechanism for resisting melanoma of the compound as shown in the formula I is demonstrated. A compound that is as shown in a formula II and is prepared from the compound of formula I and ROR1 by means of covalency markedly slows down the growth of subcutaneously transplanted mammary cancer tumor, such that the immune response mechanism, for treating the mammary cancer, of the compound as shown in the formula II is demonstrated.