JP2019529484A5 - - Google Patents
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- JP2019529484A5 JP2019529484A5 JP2019516992A JP2019516992A JP2019529484A5 JP 2019529484 A5 JP2019529484 A5 JP 2019529484A5 JP 2019516992 A JP2019516992 A JP 2019516992A JP 2019516992 A JP2019516992 A JP 2019516992A JP 2019529484 A5 JP2019529484 A5 JP 2019529484A5
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- 150000001875 compounds Chemical class 0.000 claims description 113
- 238000000034 method Methods 0.000 claims description 27
- 125000005843 halogen group Chemical group 0.000 claims description 26
- 125000000217 alkyl group Chemical group 0.000 claims description 25
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 25
- 239000008194 pharmaceutical composition Substances 0.000 claims description 24
- -1 C 1 -C 6 alkyl Chemical group 0.000 claims description 22
- 230000035772 mutation Effects 0.000 claims description 21
- 206010028980 Neoplasm Diseases 0.000 claims description 20
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 20
- 201000011510 cancer Diseases 0.000 claims description 18
- 102200006538 rs121913530 Human genes 0.000 claims description 16
- 125000001424 substituent group Chemical group 0.000 claims description 16
- 102100030708 GTPase KRas Human genes 0.000 claims description 15
- 101000584612 Homo sapiens GTPase KRas Proteins 0.000 claims description 15
- 125000002837 carbocyclic group Chemical group 0.000 claims description 14
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 14
- 102100029974 GTPase HRas Human genes 0.000 claims description 13
- 101000584633 Homo sapiens GTPase HRas Proteins 0.000 claims description 13
- 125000004181 carboxyalkyl group Chemical group 0.000 claims description 12
- 125000004966 cyanoalkyl group Chemical group 0.000 claims description 12
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 12
- 125000001153 fluoro group Chemical group F* 0.000 claims description 12
- 125000001072 heteroaryl group Chemical group 0.000 claims description 12
- 102200124918 rs121913250 Human genes 0.000 claims description 11
- 125000003118 aryl group Chemical group 0.000 claims description 10
- 125000000623 heterocyclic group Chemical group 0.000 claims description 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 10
- 102100039788 GTPase NRas Human genes 0.000 claims description 8
- 101000744505 Homo sapiens GTPase NRas Proteins 0.000 claims description 8
- 125000005097 aminocarbonylalkyl group Chemical group 0.000 claims description 8
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 102000008300 Mutant Proteins Human genes 0.000 claims description 7
- 108010021466 Mutant Proteins Proteins 0.000 claims description 7
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims description 6
- 206010009944 Colon cancer Diseases 0.000 claims description 6
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 6
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 6
- 125000000304 alkynyl group Chemical group 0.000 claims description 6
- 208000029742 colonic neoplasm Diseases 0.000 claims description 6
- 201000005787 hematologic cancer Diseases 0.000 claims description 6
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims description 6
- 201000005202 lung cancer Diseases 0.000 claims description 6
- 208000020816 lung neoplasm Diseases 0.000 claims description 6
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 6
- 201000002528 pancreatic cancer Diseases 0.000 claims description 6
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 6
- 208000015768 polyposis Diseases 0.000 claims description 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 6
- 102200006614 rs104894229 Human genes 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 208000035475 disorder Diseases 0.000 claims description 5
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 239000000651 prodrug Substances 0.000 claims description 4
- 229940002612 prodrug Drugs 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 3
- 230000005764 inhibitory process Effects 0.000 claims description 3
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims description 2
- 206010027476 Metastases Diseases 0.000 claims description 2
- 229910019142 PO4 Inorganic materials 0.000 claims description 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims description 2
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical group [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 claims description 2
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical group OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims description 2
- 125000005620 boronic acid group Chemical group 0.000 claims description 2
- 230000003833 cell viability Effects 0.000 claims description 2
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims description 2
- 125000002433 cyclopentenyl group Chemical group C1(=CCCC1)* 0.000 claims description 2
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 150000002148 esters Chemical class 0.000 claims description 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 2
- 238000002347 injection Methods 0.000 claims description 2
- 239000007924 injection Substances 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 230000009401 metastasis Effects 0.000 claims description 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims description 2
- 125000004043 oxo group Chemical group O=* 0.000 claims description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 2
- 239000010452 phosphate Substances 0.000 claims description 2
- 230000035755 proliferation Effects 0.000 claims description 2
- 230000001105 regulatory effect Effects 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 7
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 description 2
- 125000001188 haloalkyl group Chemical group 0.000 description 2
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 1
- 125000004103 aminoalkyl group Chemical group 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 235000018102 proteins Nutrition 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662401345P | 2016-09-29 | 2016-09-29 | |
| US62/401,345 | 2016-09-29 | ||
| PCT/US2017/054363 WO2018064510A1 (en) | 2016-09-29 | 2017-09-29 | Inhibitors of kras g12c mutant proteins |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019529484A JP2019529484A (ja) | 2019-10-17 |
| JP2019529484A5 true JP2019529484A5 (show.php) | 2020-11-12 |
Family
ID=60043402
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019516992A Pending JP2019529484A (ja) | 2016-09-29 | 2017-09-29 | Ｋｒａｓ ｇ１２ｃ変異体タンパク質の阻害剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US10280172B2 (show.php) |
| EP (1) | EP3519402A1 (show.php) |
| JP (1) | JP2019529484A (show.php) |
| CN (1) | CN110036010A (show.php) |
| WO (1) | WO2018064510A1 (show.php) |
Families Citing this family (159)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Ｋｒａｓ ｇ１２ｃ之抑制劑 |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| AU2016245864C1 (en) | 2015-04-10 | 2021-09-09 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| WO2016168540A1 (en) | 2015-04-15 | 2016-10-20 | Araxes Pharma Llc | Fused-tricyclic inhibitors of kras and methods of use thereof |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| EP3356353A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356339A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| US10882847B2 (en) | 2015-09-28 | 2021-01-05 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| EP3356351A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356349A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058805A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356347A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| KR20240113606A (ko) | 2015-11-16 | 2024-07-22 | 아락세스 파마 엘엘씨 | 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법 |
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| US10377743B2 (en) | 2016-10-07 | 2019-08-13 | Araxes Pharma Llc | Inhibitors of RAS and methods of use thereof |
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2017
- 2017-09-29 WO PCT/US2017/054363 patent/WO2018064510A1/en not_active Ceased
- 2017-09-29 EP EP17781353.2A patent/EP3519402A1/en not_active Withdrawn
- 2017-09-29 CN CN201780073660.4A patent/CN110036010A/zh active Pending
- 2017-09-29 US US15/721,021 patent/US10280172B2/en active Active
- 2017-09-29 JP JP2019516992A patent/JP2019529484A/ja active Pending
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2019
- 2019-04-03 US US16/374,356 patent/US10723738B2/en active Active