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Thieno-pyrimidine derivatives and uses thereof

一种药物、化合物的技术，应用在表皮生长因子受体的组合物领域，能够解决活性突变患者用途限制、剂量限制性毒性等问题，达到降低副作用的效果

Active Publication Date: 2018-07-17
ZHEJIANG JIANFENG YIEN BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of afatinib in patients with active mutations is limited by dose-limiting toxicities that cause inhibition of wild-type EGFR

Method used

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  • Thieno-pyrimidine derivatives and uses thereof
  • Thieno-pyrimidine derivatives and uses thereof
  • Thieno-pyrimidine derivatives and uses thereof

Examples

Experimental program
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preparation example Construction

[0067] The preparation of pharmaceutical compositions comprising active ingredients is well known in the art, for example by mixing, granulating or tabletting procedures. The active therapeutic ingredient is usually mixed with excipients which are pharmaceutically acceptable and compatible with the active ingredient. For oral administration, the active agent is mixed with additives customary for this purpose, such as carriers, stabilizers or inert diluents, and converted by usual methods into a suitable administration form, such as tablets, coated tablets, hard or Soft gel capsules, water, alcohol or oil solutions, etc., as described above.

[0068] The amount of compound administered to a patient is less than that which would cause toxicity to the patient. In certain embodiments, the amount of compound administered to a patient is less than the amount that would cause the patient's blood levels to equal or exceed the toxic level of the compound. In the practice of this inve...

Embodiment 1

[0140] Example 1: N-[2-[2-(dimethylamino)ethyl-methyl-amino]-5-[-[[4-(1H-indol-3-yl)thiophene Synthesis of [3,2-d]pyrimidin-2-yl]amino]-4-methoxy-phenyl]prop-2-enamide (compound 1):

[0141]

[0142] Synthesis of Thieno[3,2-d]pyrimidine-2,4(1H,3H)-dione (Compound 102)

[0143] A mixture of methyl 3-amino-2-thiophenecarboxylate (13.48 g, 85.85 mmol) and urea (29.75 g, 0.43 mol) was heated at 190°C for 2 hours. The hot reaction mixture was then poured into sodium hydroxide solution and insoluble material was removed by filtration. The mixture was then acidified with 2N HCl solution, collected by filtration and air dried to afford the compound (9.62 g, 67%) as a white precipitate.

[0144] Synthesis of 2,4-Dichlorothieno[3,2-d]pyrimidine (Compound 103)

[0145] Compound 102 (8.5 g) was suspended with phosphorus oxychloride (130 mL). The mixture was heated at 100°C for 10 hours. POCl was removed under reduced pressure 3 . The mixture was dissolved in dichlorometha...

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Abstract

Compounds having the general formula I or III,and pharmaceutical compositions comprising the same. The compounds of the present invention are useful as selective mutant epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitor, and for the treatment of EGFR related diseases and disorders such as cancer.

Description

technical field [0001] The invention relates to cancer treatment, in particular to a composition and method for inhibiting epidermal growth factor receptor of cancer cells. Background technique [0002] Epidermal growth factor receptor (EGFR, Erbb1) is involved in the proliferation of normal cells and malignant tumor cells. Overexpression of EGFR has been found to be associated with cancers such as lung, breast, head and neck, and bladder cancers. [0003] There are four receptor tyrosine kinases in the EGFR family: EGFR (ErbB1), human epidermal growth factor receptor 2 (HER2, ErbB2), HER3 (ErbB3) and HER4 (ErbB4). Tyrosine kinases function in signal transduction. The ligand binds to the ligand-binding domain of the receptor outside the cell to form active homodimers or heterodimers, causing autophosphorylation of EGFR and activation of docking proteins (Greulich H.Chen, PLoS Med, 2005, 2, e313; Olayioye MA, EMBO J, 2000, 19, 3159-3167). These signals promote cellular pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5377A61K31/5355A61P37/02
CPCA61P37/02C07D495/04A61P35/00
Inventor 翟海啸吴凡
Owner ZHEJIANG JIANFENG YIEN BIOTECH CO LTD
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