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 | ||
| JOP/2016/0150A JOP20160150B1 (ar) | 2015-07-22 | 2016-07-21 | مركبات كينازولين مستبدلة وطرق استعمالها |
| GCGC-2016-31750 | 2016-07-21 | ||
| GC201631750 | 2016-07-21 | ||
| JO150/2016 | 2016-07-21 | ||
| 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 (cg-RX-API-DMAC7.html) | 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 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6869947B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2993013A1 (cg-RX-API-DMAC7.html) |
| MX (1) | MX388781B (cg-RX-API-DMAC7.html) |
| WO (1) | WO2017015562A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (105)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY35464A (es) | 2013-03-15 | 2014-10-31 | Araxes Pharma Llc | Inhibidores covalentes de 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 |
| ES2826443T3 (es) | 2014-09-25 | 2021-05-18 | Araxes Pharma Llc | Inhibidores de proteínas mutantes KRAS G12C |
| US10011600B2 (en) | 2014-09-25 | 2018-07-03 | Araxes Pharma Llc | Methods and compositions for inhibition of Ras |
| MX382355B (es) | 2015-04-10 | 2025-03-13 | Araxes Pharma Llc | Compuestos de quinazolina sustituidos y métodos de uso de los mismos. |
| CA2982360A1 (en) | 2015-04-15 | 2016-10-20 | Liansheng Li | 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 |
| WO2017058807A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017058902A1 (en) | 2015-09-28 | 2017-04-06 | 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 |
| US10858343B2 (en) | 2015-09-28 | 2020-12-08 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058768A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356354A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| US10975071B2 (en) | 2015-09-28 | 2021-04-13 | 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 |
| MX2018005967A (es) | 2015-11-16 | 2018-08-29 | Araxes Pharma Llc | Compuestos de quinazolina 2-sustituida que comprenden un grupo heterociclico sustituido y metodos de uso de los mismos. |
| WO2017100546A1 (en) | 2015-12-09 | 2017-06-15 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| CA3008171A1 (en) | 2015-12-22 | 2017-06-29 | 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 |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| CN110036010A (zh) | 2016-09-29 | 2019-07-19 | 亚瑞克西斯制药公司 | Kras g12c突变蛋白的抑制剂 |
| WO2018068017A1 (en) | 2016-10-07 | 2018-04-12 | Araxes Pharma Llc | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
| KR20250152110A (ko) | 2016-12-22 | 2025-10-22 | 암젠 인크 | 폐암, 췌장암 또는 대장암을 치료하기 위한 kras g12c 억제제로서의 벤즈이소티아졸, 이소티아졸로[3,4-b]피리딘, 퀴나졸린, 프탈라진, 피리도[2,3-d]피리다진 및 피리도[2,3-d]피리미딘 유도체 |
| JOP20190272A1 (ar) | 2017-05-22 | 2019-11-21 | Amgen Inc | مثبطات kras g12c وطرق لاستخدامها |
| MX2019013954A (es) | 2017-05-25 | 2020-08-31 | Araxes Pharma Llc | Inhibidores covalentes de kras. |
| CN110869357A (zh) * | 2017-05-25 | 2020-03-06 | 亚瑞克西斯制药公司 | 化合物及其用于治疗癌症的使用方法 |
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| EP3679040B1 (en) | 2017-09-08 | 2022-08-03 | Amgen Inc. | Inhibitors of kras g12c and methods of using the same |
| BR112020005469A2 (pt) | 2017-09-20 | 2020-09-29 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | receptores de células t restritivas a hla classe ii contra ras mutado |
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| TW201942115A (zh) * | 2018-02-01 | 2019-11-01 | 美商輝瑞股份有限公司 | 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物 |
| CA3099118A1 (en) | 2018-05-04 | 2019-11-07 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| US11090304B2 (en) | 2018-05-04 | 2021-08-17 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| EP3790551A4 (en) * | 2018-05-07 | 2022-03-09 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| TW202012415A (zh) | 2018-05-08 | 2020-04-01 | 瑞典商阿斯特捷利康公司 | 化學化合物 |
| EP3790886B1 (en) | 2018-05-10 | 2024-06-26 | Amgen Inc. | Kras g12c inhibitors for the treatment of cancer |
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| EP3807276B1 (en) | 2018-06-12 | 2025-12-10 | Amgen Inc. | Kras g12c inhibitors encompassing a piperazine ring and use thereof in the treatment of cancer |
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| JP7516029B2 (ja) | 2018-11-16 | 2024-07-16 | アムジエン・インコーポレーテツド | Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法 |
| JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法 |
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| JP7407461B2 (ja) | 2018-12-19 | 2024-01-04 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ｒａｓ病、及び線維性疾患の処置のためのｒａｓスーパーファミリーと相互作用する化合物 |
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2016
- 2016-07-22 MX MX2018000777A patent/MX388781B/es unknown
- 2016-07-22 JP JP2018502355A patent/JP6869947B2/ja active Active
- 2016-07-22 EP EP16747678.7A patent/EP3325447A1/en not_active Withdrawn
- 2016-07-22 CA CA2993013A patent/CA2993013A1/en not_active Abandoned
- 2016-07-22 WO PCT/US2016/043568 patent/WO2017015562A1/en not_active Ceased