Abstract: The present invention provides a medicament comprising a compound represented by general formula (1) which has Axl inhibitory activity, and an EGFR tyrosine kinase inhibitor in combination, and a method for treating cancer using this combination. The present invention provides an excellent medicament and method for treating cancer which is highly effective for inhibiting resistance to an EGFR tyrosine kinase inhibitor in cancer treatment, and causes less adverse reactions such as weight loss.

Abstract: A method of treating a subject suffering from a condition characterized by over-expression of Ten-eleven translocation 1 (TET1) is provided, the method including administering to the subject an effective amount of a compound, or a pharmaceutically acceptable salt thereof, having the Formula I: wherein: R1, R2, R3, R4, and R5 are each independently selected from the group consisting of H, hydroxyl, alkyl, alkoxy, amine, halo, and trifluoromethyl, and wherein any two adjacent moieties of R1, R2, R3, R4, and R5 may come together to form a heterocyclic ring; R6 is H or hydroxyl; and R7 is selected from H, wherein R8 is C or O. Also provided are methods for selectively suppressing transcription of TET1 and/or reducing a level of 5-hydroxymethylcytosine in a subject by administering an effective amount of a Formula I compound and pharmaceutical compositions comprising Formula I compounds.

Abstract: The present invention provides a compound of general formulae I useful as GSK3? inhibitors and their anticancer potential and process for preparation of these spirooxindoles. wherein Z is hydrogen, halogen, hydroxy, alkoxy, cyano, nitro; Ring A is a five membered or six membered or seven membered optionally containing additional hetero atom in the ring X is optionally CH2 Ring B is triazole or cyclic amine alone or with one or more hetero atoms part of the ring and optionally substituted with one or more substituents Y is hydrogen, alkoxy, aryloxy, hydroxy, ester, amide, amino, alkyl or aryl, heteroaryl, wherein these substituents are optionally substituted with one or more halogen, hydroxy, alkoxy, alkyl, aryl, heteroaryl, aryloxy, nitro, cyano, ester, aldehyde, wherein these substituents are further substituted with one or more halogen, hydroxy, alkoxy, alkyl, aryl, heteroaryl, aryloxy, nitro, cyano, ester, aldehyde.

Abstract: The present invention provides novel compounds of Formulae (I?) and (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.

Abstract: The invention relates to medical chemistry, in particular to the use of 7-bromo-5-(o-chlorophenyl)-3-propoxy-1,2-di-hydro-3H-1,4-benzodiazepin-2-one as a drug which inhibits neuropathic pain without the formation of defects in the gastric mucosa (ulcerogenic effect), and possesses an anticonvulsant property.

Abstract: The disclosure relates to pharmaceutical combinations comprising an HDAC6 selective inhibitor and a BET inhibitor for the treatment of cancer in a subject in need thereof. Also provided herein are methods for treating cancer in a subject in need thereof, comprising administering to the subject an effective amount of an HDAC6 selective inhibitor and a BET inhibitor.

Abstract: Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to macrocyclic ?-keto amide derivatives and their use as therapeutic agents.

Abstract: The present invention discloses in situ generated catalyst bound alpha radical compound represented by formula (I) or (II) and a single pot process for the preparation of oxo compounds by using in situ generated catalyst bound alpha radical compound of formula (I) or (II).

Abstract: The present disclosure relates to certain macrocyclic compounds that inhibit SRC and MET, and/or CSF1R, pharmaceutical compositions containing such compounds, and methods of using such compounds to treat cancer.

Abstract: There is provided novel anticancer and antibacterial compounds, pharmaceutically acceptable salts thereof, and processes for their preparation. The compounds have anticancer activity, which results in the reduction of tumour cell proliferation, enhances cancers cells apoptosis and regulation of iron signalling. The compounds are also particularly active against various Gram-negative and Gram-positive multidrug-resistant bacteria, such as extended-spectrum beta-lactamase (ESBL) producing and colistin-resistant Escherichia coli, carbapenem-resistant E. coli, carbapenem-resistant Acinetobacter baumannii, and methicillin-resistant Staphylococcus aureus (MRSA) including those with reduced susceptibility to many control antibiotics.

Abstract: Disclosed herein are p38? mitogen-activated protein kinase inhibitors, pharmaceutical compositions thereof, and therapeutic methods of using the p38? mitogen-activated protein kinase inhibitors.

Abstract: The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers or pharmaceutically acceptable salt (s) thereof as muscarinic M1 receptor positive allosteric modulators (M1 PAMs). The present invention describes the preparation, pharmaceutical composition and the use of compound formula (I).

Abstract: The present invention relates to the field of anti-viral active agents, particularly to salts, more particularly to a maleate salt of the free base of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide, to pharmaceutical formulations thereof as well as to methods for the production of these salts. The present invention also relates to the use of theses salts and of respective pharmaceutical formulations thereof in methods of treatment and/or prevention of human herpes simplex virus infections, particularly infections caused by HSV-1 and HSV-2.

Abstract: A process is provided for preparing ethyleneamines of the formula NH2—(C2H4—NH—)pH wherein p is at least 3, or derivatives thereof wherein one or more units —NH—C2H4—NH— may be present as a cyclic ethylene urea unit or piperazine unit or between two units —NH—C2H4—NH— a carbonyl moiety is present. The process includes reacting an ethanolamine-functional compound OH—(C2H4—NH—)qH wherein q is at least 2, an amine-functional compound NH2—(C2H4—NH—)rH wherein r is at least 1, in the presence of a carbon oxide delivering agent, wherein the molar ratio of ethanolamine-functional compound to amine-functional compound is from about 0.05:1 to about 0.7:1 and the molar ratio of carbon oxide delivering agent to amine-functional compound is higher than the molar ratio of ethanolamine-functional compound to amine-functional compound, provided that the process does not comprise reacting 3 moles of ethylenediamine (EDA) and 1 mole of AEEA (aminoethylethanolamine) in the presence of 1.65 moles of urea at 280 deg C.

Abstract: The invention provided here creates a new paradigm for the treatment of a variety of conditions where modulation of a BAF complex is desired. The disclosure that follows outlines a strategy for modulating a BAF complex in a cell, and provides effective compounds, pharmaceutical compositions, development strategies, and treatment protocols, and describes many of the ensuing benefits. A new family of BAF complex modulating compounds has been developed based on a new chemical scaffold including a 12-membered macrolactam core structures. Contacting target cells in vitro or in vivo with the compounds and compositions of this invention can selectively inhibit the activity of BAF complexes in such cells. Some of the BAF complex modulating compounds in this family are particularly effective agents for treating cancer in conjunction with a ATR inhibitor.

Abstract: To provide a method that can efficiently produce 2,5-bis(aminomethyl)tetrahydrofuran. The method for producing 2,5-bis(aminomethyl)tetrahydrofuran, the method including subjecting 2,5-bis(aminomethyl)furan to a reaction with hydrogen source by using a hydrogenation catalyst to obtain 2,5-bis(aminomethyl)tetrahydrofuran.

Abstract: The present invention relates to a fluorene derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition comprising the same as an effective ingredient for preventing or treating HCV-related disease. A fluorene derivative according to the present invention is identified to exhibit an antiviral performance against not only HCV, but also highly against HCV mutants, particularly double mutants and thus can be used in a pharmaceutical composition for prevention or treatment of HCV-caused liver disease, such as acute hepatitis C, chronic hepatitis C, liver cirrhosis, hepatocellular cancer, etc., particularly, liver disease caused by mutants of HCV. The derivative can be useful in a pharmaceutical composition for prevention or treatment of HCV-related liver disease by which the problem of resistant mutation against conventional therapeutic agents is solved.

Abstract: There are provided methods of making an N-demethylated derivative of morphine namely, normorphine. The normorphine can be substituted at the N—H position with various ligands that may result in new useful morphine derivatives. These derivatives may have increased analgesic efficacy, have less addictive properties, and/or have effective anti-opiate properties capable of rescuing overdosed persons or lead to recovery from conditions caused by opiate drug abuse.

Abstract: The present invention discloses a compound, which comprises the structure shown in FIG. 1; and further discloses a preparation method thereof, a precursor material used in the preparation method, explosives comprising the compound, and the application thereof in the field of explosives, in particular in the application of green environmentally-friendly primers. The compound disclosed by the invention may provide green environmental protection type primer, and meets the problem of requiring green environmental protection primers in many fields such as military industry, firework and civil explosion engineering.

Abstract: The invention relates to compounds of formula (I), and pharmaceutical uses thereof. Particular aspects of the invention relate to methods of synthesising the compounds and the use of those compounds in treating, ameliorating, or preventing a microbial infection.