Abstract: Provided herein are acyclic oxazepinyl compounds useful in the treatment on cancers.

Abstract: Provided are an ROR?t modulator, and a preparation method therefor and an application thereof. The ROR?t modulator is selected from a compound represented by formula I, and a pharmaceutically acceptable salt, solvate, solvate of pharmaceutically acceptable salt, metabolite or prodrug thereof. The compound has inhibitory activity on ROR?t, and can effectively inhibit an ROR?t protein receptor, thereby regulating the differentiation of Th17 cells, inhibiting generation of IL-17, and then treating ROR?t-mediated relevant autoimmune diseases.

Abstract: Provided herein are inhibitors of ubiquitin-specific-processing Protease 1 (USP1), their pharmaceutical compositions, and methods of use for treating diseases or disorders, such as cancers described herein.

Abstract: The disclosure discloses a fatty acid synthase inhibitor and application thereof and belongs to the technical field of medical biology. The fatty acid synthase inhibitor of the disclosure can significantly inhibit the activity of fatty acid synthase without affecting normal expression, and adjust the ratio of fatty acids in cells. The fatty acid synthase inhibitor of the disclosure has a good tumor proliferation inhibitory effect, can arrest the growth cycle of tumor cells in the interphase, prevent tumor cell division, inhibit tumor cell proliferation, promote tumor cell apoptosis and exert a tumor treatment effect, can be used to treat tumors and metabolism related diseases, and has an important clinical application prospect.

Abstract: Provided are a class of compounds, represented by formula (I??), as selective EGFR inhibitors, a pharmaceutical composition containing the compounds, useful intermediates for preparing the compounds, and a method for using the compounds of the present invention to treat cell proliferative diseases, such as cancers.

Abstract: The present invention provides a novel aminopyrimidine compound as a fourth-generation EGFR (T790M/C797S mutation) selective inhibitor, a pharmaceutical composition comprising the compound, an intermediate useful for preparing the compound, and a method for treating a cell proliferative disease, such as a cancer, by using the compound of the present invention.

Abstract: Provided are a class of compounds, represented by formula (I??), as selective EGFR inhibitors, a pharmaceutical composition containing the compounds, useful intermediates for preparing the compounds, and a method for using the compounds of the present invention to treat cell proliferative diseases, such as cancers.

Abstract: 1,5-dihydro-2,4-benzodiazepine-3-one derivatives, such as a compound represented by formula I, acts on 5-HT2A and 5-HT2C receptors. The selectivity for 5-HT2A is superior or similar to pimavanserin. The derivative is used for treating schizophrenia or Parkinson’s disease, dementia-related behavioral disorders, and psychosis. The antipsychotic activity of the compound is equivalent to that of pimavanserin, the side effects of sedation and and worsening of exercise are less than those of pimavanserin, and cardiotoxicity is less than that of pimavanserin.

Abstract: Presently provided are inhibitors of cellularly expressed TD02 and IDO1, and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2,3 dioxygenase and indoleamine 2,3-dioxygenase 1; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.

Abstract: Described herein are pyrido-pyrimidinone and pteridinone compounds or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods treating cancer, alone and in combination with other therapeutic agents.

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of lipoprotein signal peptidase II (LspA), a key protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

Abstract: Provided herein are compounds of the Formula (I), (II), and (III): as well as pharmaceutically acceptable salts thereof, wherein the substituents are those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of oncologic diseases.

Abstract: Presently provided are inhibitors of cellularly expressed TD02 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.

Abstract: Provided herein are compounds and pharmaceutically acceptable salts thereof useful in the treatment of IRE1-related diseases and disorders described herein.

Abstract: Provided herein are compounds and pharmaceutically acceptable salts thereof useful in the treatment of IRE1-related diseases and disorders described herein.

Abstract: Provided herein are compounds of formula (I): and pharmaceutically acceptable salts thereof, where the substituents are as described herein. These compounds and their pharmaceutical compositions may be useful in the treatment of oncologic diseases.

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of lipoprotein signal peptidase II (LspA), a key protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

Abstract: The present invention relates to a spiro compound and medical uses thereof. Specifically, the present invention relates to a spiro compound represented by the general formula (I), a preparation method thereof, a pharmaceutical composition containing the same, and is used as an acetyl-Coenzyme A carboxylase (ACC) inhibitor and is used for treating diseases associated with ACC activity. Each substituent in the general formula (I) is as defined in description.

Abstract: The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

Abstract: A programmable operation and control chip, comprising: at least one controller with a control flow operation mode; at least one bus; at least one programmable operation structure with data stream flow operation mode which communicates with the controller via the bus and the data buffering structure to control and schedule the programmable operation structure and/or the data buffering structure, and allocate and process serial and parallel operation of data and/or dynamically reconfigure internal structure of the chip.