JP2018520195A5 - - Google Patents
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- JP2018520195A5 JP2018520195A5 JP2018502355A JP2018502355A JP2018520195A5 JP 2018520195 A5 JP2018520195 A5 JP 2018520195A5 JP 2018502355 A JP2018502355 A JP 2018502355A JP 2018502355 A JP2018502355 A JP 2018502355A JP 2018520195 A5 JP2018520195 A5 JP 2018520195A5
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- 150000001875 compounds Chemical class 0.000 claims description 144
- -1 cyano, amino Chemical group 0.000 claims description 51
- 125000005843 halogen group Chemical group 0.000 claims description 38
- 125000000623 heterocyclic group Chemical group 0.000 claims description 38
- 125000000217 alkyl group Chemical group 0.000 claims description 35
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 32
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 30
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 28
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 28
- 125000004181 carboxyalkyl group Chemical group 0.000 claims description 28
- 125000004966 cyanoalkyl group Chemical group 0.000 claims description 28
- 125000002837 carbocyclic group Chemical group 0.000 claims description 26
- 125000001072 heteroaryl group Chemical group 0.000 claims description 22
- 239000008194 pharmaceutical composition Substances 0.000 claims description 22
- 238000000034 method Methods 0.000 claims description 17
- 230000035772 mutation Effects 0.000 claims description 16
- 102200124918 rs121913250 Human genes 0.000 claims description 16
- 102100029974 GTPase HRas Human genes 0.000 claims description 14
- 102100030708 GTPase KRas Human genes 0.000 claims description 14
- 101000584633 Homo sapiens GTPase HRas Proteins 0.000 claims description 14
- 101000584612 Homo sapiens GTPase KRas Proteins 0.000 claims description 14
- 206010028980 Neoplasm Diseases 0.000 claims description 14
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 14
- 125000003118 aryl group Chemical group 0.000 claims description 14
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 14
- 125000004043 oxo group Chemical group O=* 0.000 claims description 14
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 12
- 201000011510 cancer Diseases 0.000 claims description 12
- 125000002947 alkylene group Chemical group 0.000 claims description 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 9
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims description 8
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 8
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 8
- 235000018102 proteins Nutrition 0.000 claims description 8
- 102000004169 proteins and genes Human genes 0.000 claims description 8
- 108090000623 proteins and genes Proteins 0.000 claims description 8
- 102200006538 rs121913530 Human genes 0.000 claims description 8
- 125000003545 alkoxy group Chemical group 0.000 claims description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 6
- 125000001188 haloalkyl group Chemical group 0.000 claims description 6
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 claims description 6
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 6
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 4
- 206010009944 Colon cancer Diseases 0.000 claims description 4
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 4
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 4
- 230000001404 mediated effect Effects 0.000 claims description 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
- 201000002528 pancreatic cancer Diseases 0.000 claims description 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 4
- 208000015768 polyposis Diseases 0.000 claims description 4
- 102200006614 rs104894229 Human genes 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- 230000005764 inhibitory process Effects 0.000 claims description 3
- 230000035755 proliferation Effects 0.000 claims description 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- 206010027476 Metastases Diseases 0.000 claims description 2
- 229910019142 PO4 Inorganic materials 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 2
- 125000003282 alkyl amino group Chemical group 0.000 claims description 2
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 2
- 125000001769 aryl amino group Chemical group 0.000 claims description 2
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims description 2
- 230000003833 cell viability Effects 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 2
- 125000002993 cycloalkylene group Chemical group 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 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
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000005241 heteroarylamino group Chemical group 0.000 claims description 2
- 125000004468 heterocyclylthio group Chemical group 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
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 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
- 239000000651 prodrug Substances 0.000 claims description 2
- 229940002612 prodrug Drugs 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 125000001424 substituent group Chemical group 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 6
- 102100039788 GTPase NRas Human genes 0.000 claims 2
- 101000744505 Homo sapiens GTPase NRas Proteins 0.000 claims 2
- 230000002489 hematologic effect Effects 0.000 claims 2
- 0 CC(C(C)=*)C(C(*)=N[C@@]1C=C(C)*)=C(**)[C@]1C=IC=CC Chemical compound CC(C(C)=*)C(C(*)=N[C@@]1C=C(C)*)=C(**)[C@]1C=IC=CC 0.000 description 6
- 201000005787 hematologic cancer Diseases 0.000 description 2
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 description 2
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical group [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562195636P | 2015-07-22 | 2015-07-22 | |
| US62/195,636 | 2015-07-22 | ||
| US201662342078P | 2016-05-26 | 2016-05-26 | |
| US62/342,078 | 2016-05-26 | ||
| JO150/2016 | 2016-07-21 | ||
| GCGC-2016-31750 | 2016-07-21 | ||
| GC201631750 | 2016-07-21 | ||
| JOP/2016/0150A JOP20160150B1 (ar) | 2015-07-22 | 2016-07-21 | مركبات كينازولين مستبدلة وطرق استعمالها |
| PCT/US2016/043568 WO2017015562A1 (en) | 2015-07-22 | 2016-07-22 | Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018520195A JP2018520195A (ja) | 2018-07-26 |
| JP2018520195A5 true JP2018520195A5 (OSRAM) | 2019-08-15 |
| JP6869947B2 JP6869947B2 (ja) | 2021-05-12 |
Family
ID=57821530
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018502355A Active JP6869947B2 (ja) | 2015-07-22 | 2016-07-22 | 置換キナゾリン化合物ならびにそのｇ１２ｃ変異ｋｒａｓ、ｈｒａｓおよび／またはｎｒａｓタンパク質の阻害剤としての使用 |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP3325447A1 (OSRAM) |
| JP (1) | JP6869947B2 (OSRAM) |
| CA (1) | CA2993013A1 (OSRAM) |
| MX (1) | MX388781B (OSRAM) |
| WO (1) | WO2017015562A1 (OSRAM) |
Families Citing this family (104)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| WO2016049524A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2016049568A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Methods and compositions for inhibition of ras |
| EA201792214A1 (ru) | 2015-04-10 | 2018-01-31 | Араксис Фарма Ллк | Соединения замещенного хиназолина |
| EP3283462B1 (en) | 2015-04-15 | 2020-12-02 | 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 |
| WO2017058915A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| US10875842B2 (en) | 2015-09-28 | 2020-12-29 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10858343B2 (en) | 2015-09-28 | 2020-12-08 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058792A1 (en) | 2015-09-28 | 2017-04-06 | 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 |
| US10647703B2 (en) | 2015-09-28 | 2020-05-12 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10730867B2 (en) | 2015-09-28 | 2020-08-04 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| JP2018533939A (ja) | 2015-10-19 | 2018-11-22 | アラクセス ファーマ エルエルシー | Ｒａｓの阻害剤をスクリーニングするための方法 |
| TW201726656A (zh) | 2015-11-16 | 2017-08-01 | 亞瑞克西斯製藥公司 | 包含經取代雜環基團之２－經取代喹唑啉化合物及其使用方法 |
| WO2017100546A1 (en) | 2015-12-09 | 2017-06-15 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| AU2016378723B2 (en) | 2015-12-22 | 2021-09-30 | SHY Therapeutics LLC | Compounds for the treatment of cancer and inflammatory disease |
| US10822312B2 (en) | 2016-03-30 | 2020-11-03 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
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| JP2019529484A (ja) | 2016-09-29 | 2019-10-17 | アラクセス ファーマ エルエルシー | Ｋｒａｓ ｇ１２ｃ変異体タンパク質の阻害剤 |
| US10377743B2 (en) | 2016-10-07 | 2019-08-13 | Araxes Pharma Llc | Inhibitors of RAS and methods of use thereof |
| EP3558955B1 (en) | 2016-12-22 | 2021-08-11 | Amgen Inc. | Benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer |
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| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| WO2025016899A1 (en) | 2023-07-19 | 2025-01-23 | Bayer Aktiengesellschaft | Spirocyclic compounds for the treatment of cancer |
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| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025072462A1 (en) | 2023-09-27 | 2025-04-03 | Nikang Therapeutics, Inc. | Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202535891A (zh) | 2023-10-20 | 2025-09-16 | 美商默沙東有限責任公司 | Ｋｒａｓ蛋白之小分子抑制劑 |
| TW202527955A (zh) | 2023-11-27 | 2025-07-16 | 美商尼坎醫療公司 | 用於經由泛素蛋白酶體途徑降解週期蛋白依賴性激酶２和週期蛋白依賴性激酶４的含有２，５－取代的嘧啶衍生物的雙功能化合物 |
| WO2025117881A1 (en) * | 2023-12-01 | 2025-06-05 | Casma Therapeutics, Inc. | Compounds and methods for inhibiting autophagy |
| WO2025117981A1 (en) | 2023-12-02 | 2025-06-05 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025212828A1 (en) | 2024-04-03 | 2025-10-09 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and cyclin-dependent kinase 4 via ubiquitin proteasome pathway |
| WO2025240536A1 (en) | 2024-05-15 | 2025-11-20 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and/or cyclin-dependent kinase 4 via ubiquitin proteasome pathway |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI271406B (en) * | 1999-12-13 | 2007-01-21 | Eisai Co Ltd | Tricyclic condensed heterocyclic compounds, preparation method of the same and pharmaceuticals comprising the same |
| JP2002371078A (ja) * | 2001-06-12 | 2002-12-26 | Sankyo Co Ltd | キノリン誘導体及びキノロン誘導体 |
| AU2002352444A1 (en) * | 2001-12-20 | 2003-07-09 | Celltech R And D Limited | Quinazolinedione derivatives |
| EP1723146A1 (en) * | 2004-03-01 | 2006-11-22 | Eli Lilly And Company | Fused pyrazole derivatives as tgf-beta signal transduction inhibitors for the treatment of fibrosis and neoplasms |
| TW200643015A (en) * | 2005-03-11 | 2006-12-16 | Akzo Nobel Nv | 2-(4-oxo-4H-quinazolin-3-yl)acetamide derivatives |
| BR112013002182B8 (pt) * | 2010-07-30 | 2023-02-28 | Oncotherapy Science Inc | Compostos derivados de quinolina, composição farmacêutica, inibidor de melk, agente modulador de expressão de melk, agente antitumor, agente terapêutico e/ou preventivo para uma doença que envolve a superexpressão de melk contendo os mesmos e uso dos referidos compostos |
| BR112015022417A2 (pt) * | 2013-03-14 | 2017-07-18 | Convergene Llc | métodos e composições para inibição de proteínas contendo bromodomínio |
| WO2015054572A1 (en) * | 2013-10-10 | 2015-04-16 | Araxes Pharma Llc | Inhibitors of kras g12c |
| NZ724691A (en) * | 2014-03-24 | 2018-02-23 | Guangdong Zhongsheng Pharmaceutical Co Ltd | Quinoline derivatives as smo inhibitors |
-
2016
- 2016-07-22 WO PCT/US2016/043568 patent/WO2017015562A1/en not_active Ceased
- 2016-07-22 JP JP2018502355A patent/JP6869947B2/ja active Active
- 2016-07-22 MX MX2018000777A patent/MX388781B/es unknown
- 2016-07-22 CA CA2993013A patent/CA2993013A1/en not_active Abandoned
- 2016-07-22 EP EP16747678.7A patent/EP3325447A1/en not_active Withdrawn
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