- N-(AZAARYL)CYCLOLACTAM-1-CARBOXAMIDE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
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An N-(azaaryl)cyclolactam-1-carboxamide derivative having a structure of formula (I), a preparation method therefor, and a use thereof are disclosed in the application. Each substituent are defined in the specification and claims. The series of compounds of the application can be widely applied in the preparation of drugs for treating cancer, tumor, autoimmune disease, metabolic disease or metastatic disease, particularly for treating ovarian cancer, pancreatic cancer, prostate cancer, breast cancer, cervical cancer, glioblastoma, multiple myeloma, metabolic disease, neurodegenerative disease, primary tumor site metastasis or osseous metastasis cancer, and are expected to be developed into a new generation of CSF-1R inhibitor drugs.
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Paragraph 0143; 0304; 0305; 0306
(2020/03/23)
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- HIGHLY ACTIVE CSF1R INHIBITOR COMPOUND
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ABSTRACT The present invention relates to a CSF1R inhibitor, and in particular to a highly active CSF1R inhibitor compound having the structure of formula (I). Said compound of the present invention has high inhibitory activity on CSF1R.
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Paragraph 0127; 0129-0130
(2020/12/10)
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- Reaktionen mit Aziridinen, XXII. Einstufensynthese von Pyrrolidonen durch Amidoethylierung einfacher Ester mit N-Acylaziridinen
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Sodium enolates of simple esters (2) react smoothly with N-acylaziridines (3) in THF forming 3-substituted 2-pyrrolidones 8.If the α-position of the ester carries more than one H-atom amidoethylated pyrrolidones can result.Whilst a simple butyrolactone behaves analogously amidoethylation of coumaranone furnished mono and bis amidoethyl derivatives of coumaranone besides a pyrrolidone. - In tert-butyl alcohol only extremly acidic esters like 1e and 1j could be amidoethylated.
- Stamm, Helmut,Woderer, Anton,Wiesert, Wolfgang
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