TW201713630A - Substituted quinazoline compounds and methods of use thereof - Google Patents
Substituted quinazoline compounds and methods of use thereofInfo
- Publication number
- TW201713630A TW201713630A TW105123325A TW105123325A TW201713630A TW 201713630 A TW201713630 A TW 201713630A TW 105123325 A TW105123325 A TW 105123325A TW 105123325 A TW105123325 A TW 105123325A TW 201713630 A TW201713630 A TW 201713630A
- Authority
- TW
- Taiwan
- Prior art keywords
- methods
- compounds
- quinazoline compounds
- substituted quinazoline
- activity
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- 125000002294 quinazolinyl group Chemical class N1=C(N=CC2=CC=CC=C12)* 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 102100030708 GTPase KRas Human genes 0.000 abstract 2
- 101000584612 Homo sapiens GTPase KRas Proteins 0.000 abstract 2
- 102200006538 rs121913530 Human genes 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R, R1, R<SP>2a</SP>, R<SP>2b</SP>, R<SP>2c</SP>, A, B, L1 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562195636P | 2015-07-22 | 2015-07-22 | |
| US201662342078P | 2016-05-26 | 2016-05-26 | |
| JOP/2016/0150A JOP20160150B1 (en) | 2015-07-22 | 2016-07-21 | Substituted quinazoline compounds and methods of use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW201713630A true TW201713630A (en) | 2017-04-16 |
Family
ID=59298009
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW105123325A TW201713630A (en) | 2015-07-22 | 2016-07-22 | Substituted quinazoline compounds and methods of use thereof |
Country Status (1)
| Country | Link |
|---|---|
| TW (1) | TW201713630A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112225734A (en) * | 2019-10-25 | 2021-01-15 | 南京瑞捷医药科技有限公司 | KRAS G12C inhibitors and their uses |
| CN113015724A (en) * | 2018-11-16 | 2021-06-22 | 美国安进公司 | Improved synthesis of key intermediates of KRAS G12C inhibitor compounds |
-
2016
- 2016-07-22 TW TW105123325A patent/TW201713630A/en unknown
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113015724A (en) * | 2018-11-16 | 2021-06-22 | 美国安进公司 | Improved synthesis of key intermediates of KRAS G12C inhibitor compounds |
| CN112225734A (en) * | 2019-10-25 | 2021-01-15 | 南京瑞捷医药科技有限公司 | KRAS G12C inhibitors and their uses |
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