- USE OF QUINAZOLINE-BASED TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCERS WITH NRG1 FUSIONS
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Provided herein are methods of selecting cancer patients for treatment with quinazoline-based tyrosine kinase inhibitors, either alone or in combination with anti- HER2/HER3 antibodies, as well as methods of treating cancer patients so selected. Cancer patients are selected for treatment if their cancer has an NRG1 fusion. Selected patients are then treated with quinazoline-based tyrosine kinase inhibitors alone or in combination with anti -HER2/HER3 antibodies.
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Paragraph 0049; 0055
(2021/08/06)
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- HETEROCYCLIC INHIBITORS OF TYROSINE KINASE
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The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of HER2 or EGFR for the treatment or prevention of disease, including cancer.
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Paragraph 0295
(2020/11/03)
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- A pyrido [3,4-d] pyrimidine -4 (3H)-one derivatives method for the preparation of
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Belonging to the field of chemical synthesis, the invention discloses a preparation method for a pyridine[3, 4-d]pyrimidine-4(3H)-one derivative. The method includes: taking a 3-aminopyridine-4-carboxylic acid compound and an amidine compound as raw materials, adopting sodium acetate as a nucleophilic catalyst, subjecting the reaction system to reflux reaction for 4-10h in an organic solvent, and carrying out TLC detection, washing, extraction, concentration, beating and filtering so as to obtain the product pyridine[3, 4-d]pyrimidine-4(3H)-one derivative. The 3-aminopyridine-4-carboxylic acid compound, the amidine compound and sodium acetate are in a mole ratio of 1:3-5:2-4. The method provided by the invention has the advantages of easily available raw materials, mild reaction condition, well operable after-treatment, higher yield, and easy realization of large scale production.
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Paragraph 0030; 0037; 0038
(2016/10/10)
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- Process for preparing 4,6-disubstituted pyrido[3,4-d]pyrimidines
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An improved process for the preparation of 4,6-disubstituted pyrido[3,4-d]pyrimidines is described where 5-amino-2-fluoropyridine is converted in seven operations to the desired products, as well as other valuable intermediates used in the process.
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- Synthesis of 6-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones via directed lithiation of 2-substituted 5-aminopyridine derivatives
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Directed lithiation of Boc or pivaloyl derivatives of 2-substituted 5-aminopyridines with BuLi-TMEDA in diethyl ether at -10°C gave 4-lithio derivatives which were quenched with CO2 to give the analogous C-4 carboxylic acids. Hydrolysis of the protecting groups with either TFA or aqueous KOH gave 2-substituted 5-aminopyridine-4-carboxylic acids which were converted to 6-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones by reaction with formamide or, more optimally, formamidine acetate. Boc protected aminopyridines provided the best overall results, with synthesis of these derivatives best achieved by direct reaction of the aminopyridine with di-tert-butyl dicarbonate in the absence of added base.
- Rewcastle, Gordon W.,Denny, William A.,Winters, R. Thomas,Colbry, Norman L.,Showalter, H. D. Hollis
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p. 2221 - 2226
(2007/10/03)
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