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Heterocyclic compounds as bcr-abl inhibitors
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A compound, the technology of heterocyclyl, applied in the field of heterocyclic compounds as BCR-ABL inhibitors
Active Publication Date: 2021-09-14
ASCENTAGE PHARMA SUZHOU CO LTD +1
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Potentially, allosteric inhibitors that bind the myristoyl binding site could be used to prevent the emergence of resistance to ATP inhibitors
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preparation example Construction
[0481] The present disclosure covers the preparation and use of salts of the compounds of the present disclosure. As used herein, a pharmaceutical "pharmaceutically acceptable salt" refers to a salt or zwitterionic form of the compounds of the present disclosure. Salts of the compounds of the present disclosure can be prepared during the final isolation and purification of the compounds, or separately by reacting the compounds with a suitable acid. The pharmaceutically acceptable salts of the compounds of the present disclosure may be acid addition salts formed with pharmaceutically acceptable acids. Examples of acids that can be used to form pharmaceutically acceptable salts include inorganic acids such as nitric, boric, hydrochloric, hydrobromic, sulfuric and phosphoric, and organic acids such as oxalic, maleic, succinic and citric. Non-limiting examples of salts of compounds of the present disclosure include, but are not limited to, hydrochloride, hydrobromide, hydroiodide...
Embodiment approach I
[0534] Embodiment I. A method of treating an individual comprising administering to the individual a therapeutically effective amount of a compound of the present disclosure, wherein the individual has cancer, neurodegenerative disease, muscular dystrophy, autoimmune disease, inflammatory disease, Viral infection or prion disease.
[0535] Embodiment II. The method of Embodiment I, wherein the individual has cancer.
[0536] Embodiment III. The method of Embodiment II, wherein the cancer is any one or more of the cancers of Table 3.
[0537] Embodiment IV. The method of Embodiment II, wherein the cancer is selected from the group consisting of acute monocytic leukemia, acute myeloid leukemia, chronic myeloid leukemia, chronic lymphocytic leukemia, mixed lineage leukemia, NUT midline carcinoma, multiple myeloma , small cell lung cancer, non-small cell lung cancer, neuroblastoma, Burkitt lymphoma, cervical cancer, esophageal cancer, ovarian cancer, colorectal cancer, prostate can...
Embodiment approach VII
[0540] Embodiment VII. The method of any one of Embodiments I-VI, wherein the compound of the present disclosure is a compound of any one of Formulas I-X, or a pharmaceutically acceptable salt or solvate thereof.
[0541] Embodiment VIII. The method of Embodiment VII, wherein the compound of the present disclosure is a compound of Formula V, or a pharmaceutically acceptable salt or solvate thereof.
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Abstract
The present disclosure provides heterocyclic compounds that are BCR-ABL inhibitors. The present disclosure provides compounds represented by formula I, wherein R 1 , R 2a , R 2b , R 2c , R 2d , R 3 , R 4a , R 4b , A, L, X, Y, Z and as defined in the instructions, and pharmaceutically acceptable salts and solvates thereof. Compounds of formula I are BCR-ABL inhibitors. BCR‑ABL inhibitors are useful in the treatment of cancer and other diseases.
Description
[0001] Field of Invention [0002] The present disclosure provides heterocyclic compounds that inhibit the enzymatic activity of Abelson protein (ABL1), Abelson-related protein (ABL2), and related chimeric proteins, particularly BCR-ABL1. The present disclosure also provides methods of making these compounds, pharmaceutical compositions comprising these compounds, and methods of using these compounds to treat diseases, disorders or conditions responsive to inhibition of BCR-ABL1. [0003] Background of the Invention [0004] Abelson murine leukemia virus oncogene homolog 1, also known as ABL1, is a protein encoded in humans by the ABL1 gene located on chromosome 9. The ABL1 proto-oncogene encodes cytoplasmic and nuclear protein tyrosine kinases involved in the processes of cell differentiation, cell division, cell adhesion and stress response. The activity of the ABL1 protein is self-inhibited by its SH3 domain, and loss of the SH3 domain turns ABL1 into an oncogene. The hall...
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