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Pharmaceutical composition of 2-aminopyrimidine compound

A composition and compound technology, which can be used in drug combinations, medical preparations containing active ingredients, organic chemistry, etc., and can solve problems such as weak inhibitory activity of wild-type EGFR

Active Publication Date: 2020-03-03
JIANGSU AOSAIKANG PHARMA CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The compound of formula I is an EGFR inhibitor that selectively inhibits the mutation of EGFRT790M, can overcome the drug resistance induced by existing drugs such as gefitinib and erlotinib, and has weak inhibitory activity on wild-type EGFR
However, there is still a lack in the art of adapting N-((5-((5-chloro-4-((naphthalene-2-yl)amino))pyrimidin-2-yl)amino)-2-((N-methyl- Pharmaceutical composition for N-dimethylaminoethyl) amino)-4-methoxyphenyl) acrylamide administration

Method used

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  • Pharmaceutical composition of 2-aminopyrimidine compound
  • Pharmaceutical composition of 2-aminopyrimidine compound
  • Pharmaceutical composition of 2-aminopyrimidine compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0132] components Proportion / % Content of 1 tablet / mg Compound of formula I 25 80 lactose 16.75 53.60 microcrystalline cellulose 50.25 160.80 Crospovidone 3.5 11.20 Sodium stearyl fumarate 3 9.60 colloidal silica 1.5 4.80

[0133] Weighing: Accurately weigh the compound of formula I, lactose, microcrystalline cellulose (PH302), crospovidone, sodium stearyl fumarate (S96), and colloidal silicon dioxide according to the scale of 500 tablets.

[0134] Mixing: Premix other materials except sodium stearyl fumarate first, then sieve through a 40-mesh stainless steel sieve for 3 times, add sodium stearyl fumarate to the sieved material and mix well, take 9 samples at different positions , to measure content uniformity.

[0135] Tablet compression: Calculate the standard tablet weight according to the measurement results of the intermediate content, control the tablet weight ± 3%, hardness 90-120N, and compress the tablet.

...

Embodiment 2

[0138] components Proportion / % Content of 1 tablet / mg Compound of formula I 25 80 Mannitol 50.25 160.80 microcrystalline cellulose 16.75 53.60 Crospovidone 3.5 11.20 Sodium stearyl fumarate 3 9.60 colloidal silica 1.5 4.80

[0139] Weighing: Accurately weigh the compound of formula I, mannitol, microcrystalline cellulose (PH302), crospovidone, sodium stearyl fumarate (S96), and colloidal silicon dioxide according to the scale of 500 tablets.

[0140] Mixing: Premix other materials except sodium stearyl fumarate, and then pass through a 40-mesh stainless steel sieve for 3 times, add sodium stearyl fumarate to the sieved materials and mix evenly, and measure the content of intermediates.

[0141] Tablet compression: Calculate the standard tablet weight according to the measurement results of the intermediate content, control the tablet weight ± 3%, hardness 90-120N, and compress the tablet.

[0142] Coating: The concent...

Embodiment 3～ Embodiment 6

[0144]

[0145] Weighing: Accurately weigh the compound of formula I, lactose, microcrystalline cellulose (PH302), crospovidone, and sodium stearyl fumarate (S96) according to the scale of 1100 tablets.

[0146] Mixing: Premix other materials except sodium stearyl fumarate, and then pass through a 40-mesh stainless steel sieve for 3 times, add sodium stearyl fumarate to the sieved materials and mix evenly, and measure the content of intermediates.

[0147] Tablet compression: Calculate the standard tablet weight according to the measurement results of the intermediate content, control the tablet weight ± 3%, hardness 90-120N, and compress the tablet.

[0148] Coating: The concentration of the coating solution is prepared to be 12%, and the weight gain of the coating is 3-4%.

[0149] Take 15 tablets from the tablets prepared in each example and divide them into 3 parts for dissolution investigation (dissolution medium pH=3.8). Samples were taken and measured at 5 minutes, ...

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Abstract

The invention provides a pharmaceutical composition of a 2-aminopyrimidine compound or a pharmaceutically acceptable salt thereof. In particular, the invention provides a pharmaceutical composition containing N-((5-((5-chloro-4-((naphthalene-2-yl)amino))pyrimidine-2-yl)amino)-2-((N-methyl-N-dimethylaminoethyl)amino)-4-methoxyphenyl) acrylamide or a pharmaceutically acceptable salt thereof, and a method for preparing the above pharmaceutical composition.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular, the invention relates to compound N-((5-((5-chloro-4-((naphthalene-2-yl)amino))pyrimidin-2-yl)amino)-2 -((N-methyl-N-dimethylaminoethyl)amino)-4-methoxyphenyl)acrylamide or its pharmaceutically acceptable salt pharmaceutical composition, and preparation of the pharmaceutical composition method. Background technique [0002] Epidermal growth factor receptor (EGFR), a receptor tyrosine protein kinase, regulates cell proliferation, survival, adhesion, migration and differentiation. EGFR is overactivated or continuously activated in a variety of tumor cells, such as lung cancer, breast cancer, and prostate cancer. Blocking the activation of EGFR and Erb-B2 has been clinically validated as the leading approach to target therapy of tumor cells. Two small-molecule inhibitors targeting EGFR, gefitinib and erlotinib, received fast-track approval from the U.S. Food and Drug Admi...

Claims

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Application Information

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IPC IPC(8): A61K31/505A61P35/00
CPCA61K31/505A61P35/00A61K31/506A61K31/5377C07D239/47C07D239/48C07D401/02C07D403/12
Inventor 陈庆财宋婷婷孙敏仇海镇田帅华
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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