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Purinone compounds and their use in treating cancer

A compound, purine technology, applied in the crystal form and its pharmaceutically acceptable salt, to treat DNA-PK-mediated diseases, to treat or prevent DNA-PK-mediated diseases, and to solve problems such as poor selectivity

Pending Publication Date: 2021-01-15
ASTRAZENECA AB +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

DNA-PK is a member of the phosphatidylinositol 3-kinase-related kinase (PIKK) family of protein kinases, and older generation DNA-PK inhibitors such as NU7026, NU7441, KU-0060648, and CC-115 are the choice for other PIKK family members poor sex

Method used

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  • Purinone compounds and their use in treating cancer
  • Purinone compounds and their use in treating cancer
  • Purinone compounds and their use in treating cancer

Examples

Experimental program
Comparison scheme
Effect test

example 44

[0164] Thus, in another aspect, Compound A Form A (Example 44, 7-methyl-9-(1-methylpiperidin-4-yl)-2-((7-methylquinoline-6 -yl)amino)-7,9-dihydro-8H-purin-8-one).

[0165] According to the present disclosure, there is provided Form A of Compound A having an XRPD pattern with at least one specific peak at about 2-theta = 7.1° measured using CuKα radiation.

[0166] According to the present disclosure, there is provided Form A of Compound A having an XRPD pattern with at least one specific peak at about 2-theta = 8.5° measured using CuKα radiation.

[0167] According to the present disclosure, there is provided Form A of Compound A having an XRPD pattern with at least two specific peaks at about 2-theta = 7.1° and 8.5° measured using CuKα radiation.

[0168] According to the present disclosure, there is provided crystalline Form A of Compound A having a crystallographic value at about 2-theta = 7.1°, 8.5°, 12.7°, 14.2°, 15.4°, 16.3°, 18.8°, 19.8° measured using CuKα radiation. ...

example 21

[0175] According to another aspect, Compound B Form A (Example 21, (S)-7-methyl-2-((7-methylcinnolin-6-yl)amino)-9-(tetrahydrofuran-3-yl )-7,9-dihydro-8H-purin-8-one).

[0176] According to the present disclosure, there is provided Form A of Compound B having an XRPD pattern with at least one specific peak at about 2-theta = 9.7° measured using CuKα radiation.

[0177] According to the present disclosure, there is provided Form A of Compound B having an XRPD pattern with at least one specific peak at about 2-theta = 12.9°.

[0178] According to the present disclosure, there is provided Form A of Compound B having an XRPD pattern with at least two specific peaks at about 2-theta = 9.7° and 12.9° measured using CuKα radiation.

[0179] According to the present disclosure, there is provided crystalline Form A of Compound B, which has a temperature range of about 2-theta = 9.7°, 12.5°, 12.9°, 15.8°, 17.6°, 17.9°, 19.4°, 21.0° measured using CuKα radiation. , 26.0°, 26.4° have th...

example 52

[0186] In another aspect, Compound C Form A (Example 52, 9-((3R,4R)-4-fluoropyrrolidin-3-yl)-7-methyl-2-((7-methylquin (olin-6-yl)amino)-7,9-dihydro-8H-purin-8-one).

[0187] According to the present disclosure, there is provided Form A of Compound C having an XRPD pattern with at least one specific peak at about 2-theta = 7.3° measured using CuKα radiation.

[0188] According to the present disclosure, there is provided Form A of Compound C having an XRPD pattern with at least one specific peak at about 2-theta = 15.0°.

[0189] According to the present disclosure, there is provided Form A of Compound C having an XRPD pattern with at least two specific peaks at about 2-theta = 7.3° and 15.0° measured using CuKα radiation.

[0190] According to the present disclosure, there is provided crystalline Form A of Compound C, which has a temperature range of about 2-theta = 7.3°, 15.0°, 14.6°, 26.5°, 12.2°, 26.0°, 17.0°, 15.9° measured using CuKα radiation. , 27.3°, and 10.8° have ...

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PUM

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Abstract

The specification generally relates to compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, where R1, A1, A2 and A3 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.

Description

technical field [0001] This specification generally relates to substituted purinone compounds and pharmaceutically acceptable salts thereof. These compounds and their pharmaceutically acceptable salts selectively modulate DNA-dependent protein kinase ("DNA-PK"), and thus this description also relates to these compounds and their salts for the treatment or prevention of DNA-PK mediated diseases (including cancer) use. The description further relates to crystalline forms of purinone compounds and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of making such compounds and salts; Intermediates for the manufacture of such compounds and salts; and methods involving the use of such compounds and salts for the treatment of DNA-PK mediated diseases, including cancer. Background technique [0002] DNA-PK is a nuclear serine / threonine protein kinase complex composed of the c...

Claims

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Application Information

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IPC IPC(8): C07D473/32A61K31/522A61P35/00
CPCC07D473/32A61P35/00A61K31/502A61K31/704C07B2200/13A61K31/437A61K31/5377A61K9/127A61K31/519A61K31/522A61N5/10
Inventor M·R·V·芬莱F·W·戈德伯格M·R·霍华德A·K·T·廷
Owner ASTRAZENECA AB
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