Patent classifications
C07D513/16
CHIMERIC COMPOUNDS TARGETING PROTEINS, COMPOSITIONS, METHODS, AND USES THEREOF
The present invention provides chimeric compounds that modulate protein function, to restore protein homeostasis, including cytokine, aiolos, and/or ikaros activity, TNF-alpha activity, CK1-alpha activity and cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions, including in combination with other cytokine and inflammatory mediators, are provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions, such as cytokine-mediated diseases, disorders, and conditions, including inflammation, fibromyalgia, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, inflammatory bowel diseases, Crohn's disease, ulcerative colitis, uveitis, inflammatory lung diseases, chronic obstructive pulmonary disease, Alzheimer's disease, organ transplant rejection, and cancer, are provided.
Macrocyclic compounds as protein kinase inhibitors
There is provided compounds of formula I, wherein R1, R.sup.2a, R.sup.2b, R.sup.2c, X, Y, Z, R.sup.3 and ring A/B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K, PIM family kinase and/or mTOR) is desired and/or required, and particularly in the treatment of cancer. The invention also relates to combinations containing such compounds. ##STR00001##
Macrocyclic compounds as protein kinase inhibitors
There is provided compounds of formula I, wherein R1, R.sup.2a, R.sup.2b, R.sup.2c, X, Y, Z, R.sup.3 and ring A/B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K, PIM family kinase and/or mTOR) is desired and/or required, and particularly in the treatment of cancer. The invention also relates to combinations containing such compounds. ##STR00001##
Sulfur-containing polycyclic-hydroxypyridone carboxamide analog against HIV
The disclosure discloses a sulfur-containing polycyclic-hydroxypyridone carboxamide analog against HIV and an application thereof. The sulfur-containing polycyclic-hydroxypyridone carboxamide analog has a compound represented by the following formula (I) or a stereoisomer thereof or a pharmaceutically acceptable salt thereof. The sulfur-containing polycyclic-hydroxypyridone carboxamide analogs provided by the disclosure have good anti-HIV activity, and in particularly, compound 2, compound 18, compound 34 and compound 66 have strong inhibitory effects on HIV-1 replication in vitro, and the therapeutic index thereof against HIV is hundreds of times greater than that of the existing drugs TDF and Dolutegravir. The development of such the compounds is of great significance for the development of AIDS drugs and will bright good news to AIDS patients.
PRC1 inhibitors and methods of treatment therewith
Provided herein are small molecule inhibitors of Polycomb Repressive Complex 1 (PRC1) activity, and methods of use thereof for the treatment of disease, including leukemia and other cancers, as well as other diseases dependent on the activity of PRC1.
PRC1 inhibitors and methods of treatment therewith
Provided herein are small molecule inhibitors of Polycomb Repressive Complex 1 (PRC1) activity, and methods of use thereof for the treatment of disease, including leukemia and other cancers, as well as other diseases dependent on the activity of PRC1.
MATERIALS FOR ORGANIC ELECTROLUMINESCENT DEVICES
Abstract: The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices, and to electronic device.
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MATERIALS FOR ORGANIC ELECTROLUMINESCENT DEVICES
Abstract: The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices, and to electronic device.
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MATERIALS FOR ORGANIC ELECTROLUMINESCENT DEVICES
The present invention relates to compounds suitable for use in electronic devices, and to electronic devices, especially organic electroluminescent devices, comprising these compounds.
MATERIALS FOR ORGANIC ELECTROLUMINESCENT DEVICES
The present invention relates to compounds suitable for use in electronic devices, and to electronic devices, especially organic electroluminescent devices, comprising these compounds.