Abstract: The present disclosure relates to a pharmaceutical composition comprising ibrutinib as an effective ingredient for preventing or treating neurodegenerative brain disease. Ibrutinib according to the present disclosure inhibits LPS-induced proinflammatory cytokine levels and BV2 microglial cell migration. In addition, ibrutinib treatment significantly reduced LPS-mediated microglial and astroglial activation. Ibrutinib treatment significantly diminished AP plaque numbers, tau hyperphosphorylation, and tau kinase CDK5 phosphorylation. Moreover, ibrutinib treatment enhances memory and thus can be used as a therapeutic agent for prevention or treatment of neurodegenerative brain disease.

Abstract: Provided are crystalline forms of (R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-2-(oxetan-3-yl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-5-yl)-1H-1,2,3-triazole-4-carboxamide, pharmaceutical compositions, methods of use and methods of making thereof.

Abstract: Provided herein are compounds of formula (I?): or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein Y2, Y3, L1, L2, X1, X2, X3, X4, X5, Q1, R1, R2, Rk, Rm, and Rn are as defined elsewhere herein. Also provided herein are methods of preparing compounds of formula (I?). Also provided herein are methods of inhibiting GYS1 and methods of treating a GYS1-mediated disease, disorder, or condition in an individual in need thereof.

Abstract: The present invention relates to fused cyclic urea derivatives which have antagonistic activities against CRHR1 and/or CRHR2, and which are useful in the treatment or prevention of disorders and diseases in which CRHR1 and/or CRHR2 is involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CRHR1 and/or CRHR2 is involved.

Abstract: A method of inhibiting cyclooxygenase includes administering an inhibitory agent to a patient in need thereof. The inhibitory agent is selected from Compound 1 (5-{[(4-fluorobenzyl)(tetrahydrofuran-2-ylmethyl)amino]methyl}-2-methoxyphenyl)methanol), Compound 2 (N-{[3-(3-methoxyphenyl)-1-phenyl-1H-pyrazol-4-yl]methyl}-N-methyl-2-(1H-pyrazol-4-yl)ethanamine), Compound 3 ({4-[3-(2-pyridinyl)benzyl]-3-morpholinyl}acetic acid), and Compound 4 ([4-chloro-2-(7-oxo-5,6,7,8-tetrahydro-1H-pyrazole[4,3-g]quinoline-5-yl)phenoxy]acetic acid). Compounds 1-4 may inhibit both the COX-1 and the COX-2 enzymes.

Abstract: The pyrrolo[3,2-b]quinoline compounds are antibacterial agents. The emergence of drug-resistant bacteria calls for constant development of new antibacterial agents with the aim of generating medicaments that are potent against drug sensitive and resistant bacteria and are well tolerated. The present compounds are not only new, but have very valuable antimicrobial properties. These compounds showed a broad spectrum of activity against gram-positive and gram-negative bacteria, as well tuberculosis mycobacteria. They also showed potent activity against drug-resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.

Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and at least one pharmaceutical excipient selected from the group consisting of fillers, binders, disintegrants, glidants and lubricants, wherein the compound according to formula I is represented by:

Abstract: The 4-arylamino-2-(6-indolylamino)pyrimidine derivative compounds are antibacterial agents having broad spectrum antibacterial activity. The present 4-arylamino-2-(6-indolylamino)pyrimidine compounds have antimicrobial activity against various susceptible and resistant gram-positive and gram-negative bacteria as well as drug resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.

Abstract: The N-(Pyrido[2,3-b]indol-7-yl)acetamide compounds are antibacterial agents. The emergence of drug-resistant bacteria calls for constant development of new antibacterial agents with the aim of generating medicaments that are potent against drug sensitive and resistant bacteria and are well tolerated. The present compounds are not only new, but have very valuable antimicrobial properties. These compounds showed a broad spectrum of activity against gram-positive and gram-negative bacteria, as well tuberculosis mycobacteria. They also showed potent activity against drug-resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.

Abstract: In one aspect, the invention provides compounds and methods that are useful for treating bacterial infections:

Abstract: Disclosed in the present invention are a crystal form of a TrkA inhibitor and a preparation method thereof, and an application thereof in preparation of drugs for treating diseases associated with pain, cancer, inflammation, neurodegenerative diseases, and certain infectious diseases.

Abstract: The invention relates to novel molecules having the general formula (I), and which molecules are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma inflammation and/or vasoconstriction, e.g. hypertension.

Abstract: The present disclosure provides combination therapy comprising a BET inhibitor and a protein phosphatase 2A (PP2A) activator, a B-cell lymphoma-2 (Bcl-2) inhibitor, a B-cell lymphoma-extra large (Bcl-xl) inhibitor, a casein kinase 2 (CK2) inhibitor, and/or a mediator complex subunit 1 (MED1) for cancer. The combination therapy is expected to be synergistic in treating the cancer, compared to the monotherapy. Methods for identifying a subject having a cancer that is resistant to or at risk of developing resistance to bromodomain and extra terminal (BET) inhibitor therapy are also provided.

Abstract: The present disclosure provides for treatments of restless legs syndrome (RLS) or one or more symptoms associated with RLS comprising administering leucine, acetyl-leucine or a pharmaceutically acceptable salt thereof.