Abstract: The present invention provides a class of pyrimidinedione cyclohexenyl compounds and methods of using these compounds as glucocorticoid receptor modulators.

Abstract: Described herein are compounds that are inhibitors of autophagy and their use in the treatment of disorders such as cancers.

Abstract: The instant invention describes compounds having IL-6 modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by IL-6.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; Wherein R1, R3-R6, X2 and X3 are as defined herein, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: Described herein are splice modifying compounds affecting splicing of mRNA, such as pre-mRNA, expressed from the FOXM1 gene, compositions comprising thereof, and methods using the same.

Abstract: The disclosure provides, inter alia, alpha-5 beta-1 inhibitors, pharmaceutical compositions comprising alpha-5 beta-1 inhibitors, methods for treating diseases using alpha-5 beta-1 inhibitors, and processes for making alpha-5 beta-1 inhibitors.

Abstract: The present invention relates to compounds that are modulators of Integrin Linked Kinase (ILK), and methods of treating diseases with such compounds. In certain embodiments, the compounds are within Formulas I-VII (e.g., Csbl-1). In some embodiments, the compounds are used to treat an ILK-mediated disease, such as cancer (e.g., triple negative breast cancer) or an inflammatory disease.

Abstract: A compound with the formula I: (I) and salts and solvates thereof, wherein: R? is a group of formula II: (II) where each of n and m are independently selected from 1, 2 and 3.

Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.

Abstract: The present invention describes compounds of formula (I) Wherein: R1 is selected from H and CH3 R2 is selected from H, C4H9 alkyl, C6H13 alkyl and C3H6-phenyl, said phenyl optionally substituted by OH or OCH3, (1R,2S,5S)-5-methylcyclopent-3-ene-1,2-diol X is O or S Y is C, N or S. These compounds have been identified as novel compounds useful in the treatment of multiple sclerosis and other autoimmune diseases.

Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth:

Abstract: Compounds of formula (I) and related aspects.

Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Abstract: Provided are compounds represented by Formula (I-A) and the pharmaceutically acceptable salts and solvates thereof, wherein R8, R9a, R9b, R9c, R9d, X, Y, Z, Z1, W, and (aa) are as defined as set forth in the specification. Provided are also compounds of Formula (I-A) for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.

Abstract: A phenyleneethynylene macrocycle (PEMC) is constructed that is a cyclic or polycyclic oligo (oligophenyleneethynylene-co-polyamine) where a monodispersed oligophenyleneethynylene is coupled with a polyamine. The PEMC is formed by coupling a monodispersed di-aldehyde end-capped oligophenyleneethynylene with a polyamine to form a macrocyclic imine and reducing the imine to an amine. The PEMC is useful at entering living cells for the fluorescence imaging of the living cells without toxicity to the cells.

Abstract: The present invention is directed to inhibitors of the interaction of menin with MLL and MLL fusion proteins, pharmaceutical compositions containing the same, and their use in the treatment of cancer and other diseases mediated by the menin-MLL interaction.

Abstract: Disclosed are a compound and a pharmaceutically acceptable salt thereof, which can be used, by means of a chemical small molecule which targets both UHFR1 and HDAC1, or a pharmaceutically acceptable salt thereof, as corresponding inhibitors or drugs for treating diseases, and are used for treating myelodysplastic syndrome, psoriasis, scar hyperplasia, prostate or breast hyperplasia, hematologic neoplasms and solid cancers alone or combined with other methods. Same have a good therapeutic effect.

Abstract: This invention provides Degronimers that have E3 Ubiquitin Ligase targeting moieties (Degrons) that can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation. The invention also provides Degrons that can be used to treat disorders mediated by cereblon or an Ikaros family protein, and methods of use and compositions thereof as well as methods for their preparation.

Abstract: The invention relates to substituted bicyclic heterocyclic compounds of formula (I), pharmaceutically acceptable salts thereof and pharmaceutical compositions for treating diseases, disorders or conditions associated with the overexpression of PRMT5 enzyme. The invention also relates to methods of treating diseases, disorders or conditions associated with the overexpression of PRMT5 enzyme.