JP2018519357A5 - - Google Patents
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- Publication number
- JP2018519357A5 JP2018519357A5 JP2018510695A JP2018510695A JP2018519357A5 JP 2018519357 A5 JP2018519357 A5 JP 2018519357A5 JP 2018510695 A JP2018510695 A JP 2018510695A JP 2018510695 A JP2018510695 A JP 2018510695A JP 2018519357 A5 JP2018519357 A5 JP 2018519357A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- nhc
- heterocycloalkyl
- independently
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 87
- 125000001072 heteroaryl group Chemical group 0.000 claims 69
- 125000000753 cycloalkyl group Chemical group 0.000 claims 56
- 125000003118 aryl group Chemical group 0.000 claims 50
- 229910052736 halogen Inorganic materials 0.000 claims 50
- 150000002367 halogens Chemical class 0.000 claims 50
- 125000000217 alkyl group Chemical group 0.000 claims 49
- 150000003839 salts Chemical class 0.000 claims 45
- 150000001875 compounds Chemical class 0.000 claims 44
- 125000004404 heteroalkyl group Chemical group 0.000 claims 40
- 229910052739 hydrogen Inorganic materials 0.000 claims 36
- 239000001257 hydrogen Substances 0.000 claims 36
- 150000002431 hydrogen Chemical class 0.000 claims 34
- 125000001424 substituent group Chemical group 0.000 claims 32
- 125000004474 heteroalkylene group Chemical group 0.000 claims 25
- 229910052757 nitrogen Inorganic materials 0.000 claims 22
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 22
- 125000000732 arylene group Chemical group 0.000 claims 20
- 125000002993 cycloalkylene group Chemical group 0.000 claims 20
- 125000005549 heteroarylene group Chemical group 0.000 claims 20
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 20
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 19
- 125000002947 alkylene group Chemical group 0.000 claims 17
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 8
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 5
- 101710113436 GTPase KRas Proteins 0.000 claims 4
- 238000006243 chemical reaction Methods 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- SLWPRWSXSCAQDF-NSHDSACASA-N COc(ccc(Cl)c1)c1C(N(CC1)C[C@H]1C(NCC(COc(c(F)c(cc1F)F)c1F)=O)=O)=O Chemical compound COc(ccc(Cl)c1)c1C(N(CC1)C[C@H]1C(NCC(COc(c(F)c(cc1F)F)c1F)=O)=O)=O SLWPRWSXSCAQDF-NSHDSACASA-N 0.000 description 1
- SOCJXAGHTRHRHK-ZDUSSCGKSA-N COc(ccc(Cl)c1)c1C(N(CC1)C[C@H]1C(NCC(COc(c(F)ccc1)c1F)=O)=O)=O Chemical compound COc(ccc(Cl)c1)c1C(N(CC1)C[C@H]1C(NCC(COc(c(F)ccc1)c1F)=O)=O)=O SOCJXAGHTRHRHK-ZDUSSCGKSA-N 0.000 description 1
- RJCMMQRYZAOCME-UHFFFAOYSA-N COc(ccc(Cl)c1)c1C(N(CCC1)CC1C(NCC(COc(c(F)c(cc1F)F)c1F)=O)=O)=O Chemical compound COc(ccc(Cl)c1)c1C(N(CCC1)CC1C(NCC(COc(c(F)c(cc1F)F)c1F)=O)=O)=O RJCMMQRYZAOCME-UHFFFAOYSA-N 0.000 description 1
- RBXMNNZBZKBQNF-AWEZNQCLSA-N COc(ccc(Cl)c1)c1C(N(CCC1)C[C@H]1C(NCC(COc(c(F)ccc1)c1F)=O)=O)=O Chemical compound COc(ccc(Cl)c1)c1C(N(CCC1)C[C@H]1C(NCC(COc(c(F)ccc1)c1F)=O)=O)=O RBXMNNZBZKBQNF-AWEZNQCLSA-N 0.000 description 1
- XMKNRZMUYSQMLN-KRWDZBQOSA-N Cc1cccc(C)c1OCC(CNC([C@@H](CC1)CN1C(c(cc(cc1)Cl)c1OC)=O)=O)=O Chemical compound Cc1cccc(C)c1OCC(CNC([C@@H](CC1)CN1C(c(cc(cc1)Cl)c1OC)=O)=O)=O XMKNRZMUYSQMLN-KRWDZBQOSA-N 0.000 description 1
- GXLLQDDBHNKPTM-SFHVURJKSA-N Cc1cccc(C)c1OCC(CNC([C@@H](CCC1)CN1C(c(cc(cc1)Cl)c1OC)=O)=O)=O Chemical compound Cc1cccc(C)c1OCC(CNC([C@@H](CCC1)CN1C(c(cc(cc1)Cl)c1OC)=O)=O)=O GXLLQDDBHNKPTM-SFHVURJKSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562157915P | 2015-05-06 | 2015-05-06 | |
| US62/157,915 | 2015-05-06 | ||
| US201562158356P | 2015-05-07 | 2015-05-07 | |
| US62/158,356 | 2015-05-07 | ||
| PCT/US2016/031344 WO2016179558A1 (en) | 2015-05-06 | 2016-05-06 | K-ras modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018519357A JP2018519357A (ja) | 2018-07-19 |
| JP2018519357A5 true JP2018519357A5 (OSRAM) | 2019-06-13 |
| JP6771023B2 JP6771023B2 (ja) | 2020-10-21 |
Family
ID=57218009
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018510695A Expired - Fee Related JP6771023B2 (ja) | 2015-05-06 | 2016-05-06 | Ｋ−ｒａｓ調節物質 |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US10857140B2 (OSRAM) |
| EP (1) | EP3291813A4 (OSRAM) |
| JP (1) | JP6771023B2 (OSRAM) |
| KR (1) | KR20180017013A (OSRAM) |
| CN (1) | CN107847495A (OSRAM) |
| AU (1) | AU2016258192B2 (OSRAM) |
| BR (1) | BR112017023821A2 (OSRAM) |
| CA (1) | CA2983927A1 (OSRAM) |
| CL (2) | CL2017002786A1 (OSRAM) |
| EA (1) | EA201792443A1 (OSRAM) |
| EC (1) | ECSP17073743A (OSRAM) |
| HK (2) | HK1251485A1 (OSRAM) |
| IL (1) | IL255417A (OSRAM) |
| MA (1) | MA42061A (OSRAM) |
| MX (1) | MX2017014163A (OSRAM) |
| PH (1) | PH12017501999A1 (OSRAM) |
| WO (1) | WO2016179558A1 (OSRAM) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150087628A1 (en) | 2012-04-10 | 2015-03-26 | The Regents Of The University Of California | Compositions and methods for treating cancer |
| US10857140B2 (en) | 2015-05-06 | 2020-12-08 | The Regents Of The University Of California | K-Ras modulators |
| KR102444509B1 (ko) | 2016-05-18 | 2022-09-19 | 미라티 테라퓨틱스, 인크. | Kras g12c 억제제 |
| EP3612526A2 (en) | 2017-04-20 | 2020-02-26 | The Regents of the University of California | K-ras modulators |
| US10647715B2 (en) | 2017-11-15 | 2020-05-12 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| EA202091186A1 (ru) | 2017-11-15 | 2020-10-01 | Мирати Терапьютикс, Инк. | ИНГИБИТОРЫ KRas G12C |
| TW202012396A (zh) * | 2018-04-18 | 2020-04-01 | 美商德洛斯股份有限公司 | 具乙烯磺醯胺部分之k-ras調節劑 |
| US11932633B2 (en) | 2018-05-07 | 2024-03-19 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| CA3112043A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| JP2022500385A (ja) | 2018-09-10 | 2022-01-04 | ミラティ セラピューティクス， インコーポレイテッド | 組み合わせ療法 |
| PT3849537T (pt) | 2018-09-10 | 2025-01-22 | Mirati Therapeutics Inc | Terapêuticas de combinação |
| CA3112129A1 (en) | 2018-12-05 | 2020-06-11 | Mirati Therapeutics, Inc. | Combination therapies |
| EP3908283A4 (en) | 2019-01-10 | 2022-10-12 | Mirati Therapeutics, Inc. | KRAS G12C INHIBITORS |
| EP3946629A4 (en) * | 2019-03-26 | 2023-04-05 | University Of Massachusetts | THERAPEUTIC TARGETS FOR ONCOGENIC KRAS-DEPENDENT CANCERS |
| KR20220071193A (ko) | 2019-08-29 | 2022-05-31 | 미라티 테라퓨틱스, 인크. | Kras g12d 억제제 |
| US11890285B2 (en) | 2019-09-24 | 2024-02-06 | Mirati Therapeutics, Inc. | Combination therapies |
| CN110981943B (zh) * | 2019-12-02 | 2021-08-03 | 清华大学 | 多肽及其在制备药物中的用途和药物 |
| CN115135315B (zh) | 2019-12-20 | 2024-11-26 | 米拉蒂治疗股份有限公司 | Sos1抑制剂 |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| CA3175481A1 (en) * | 2020-04-27 | 2021-11-04 | Verastem, Inc. | Methods of treating abnormal cell growth |
| TW202210633A (zh) | 2020-06-05 | 2022-03-16 | 法商昂席歐公司 | 用於治療癌症之dbait分子與kras抑制劑的組合 |
| TW202214253A (zh) | 2020-06-18 | 2022-04-16 | 美商銳新醫藥公司 | 延遲、預防及治療對ｒａｓ抑制劑之後天抗性之方法 |
| CA3187757A1 (en) | 2020-09-03 | 2022-03-24 | Ethan AHLER | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| MX2023002942A (es) | 2020-09-11 | 2023-05-22 | Mirati Therapeutics Inc | Formas cristalinas de un inhibidor de kras g12c. |
| CA3198885A1 (en) | 2020-12-15 | 2022-06-23 | Xiaolun Wang | Azaquinazoline pan-kras inhibitors |
| US11999753B2 (en) | 2020-12-16 | 2024-06-04 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-KRas inhibitors |
| US20240336563A1 (en) * | 2021-04-26 | 2024-10-10 | The Regents Of The University Of California | G-alpha-s inhibitors and uses thereof |
| EP4389751A1 (en) | 2021-09-03 | 2024-06-26 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| US11873296B2 (en) | 2022-06-07 | 2024-01-16 | Verastem, Inc. | Solid forms of a dual RAF/MEK inhibitor |
| WO2024155770A2 (en) * | 2023-01-18 | 2024-07-25 | Molecular Axiom, Llc | Compositions for modulating kras expression and uses thereof |
| TW202444727A (zh) | 2023-01-26 | 2024-11-16 | 美商艾維納斯手術有限公司 | 基於cereblon之kras降解protac及其相關用途 |
| WO2024243441A1 (en) | 2023-05-24 | 2024-11-28 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| WO2025007000A1 (en) | 2023-06-30 | 2025-01-02 | Kumquat Biosciences Inc. | Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors |
| WO2025171055A1 (en) | 2024-02-06 | 2025-08-14 | Kumquat Biosciences Inc. | Heterocyclic conjugates and uses thereof |
| WO2025230971A1 (en) | 2024-04-30 | 2025-11-06 | Kumquat Biosciences Inc. | Macrocyclic heterocycles as anticancer agents |
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| DE3131527A1 (de) | 1981-08-08 | 1983-02-24 | Kali-Chemie Pharma Gmbh, 3000 Hannover | 1-phenyl-2-aminocarbonylindol-verbindungen sowie verfahren und zwischenprodukte zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
| JPS61227567A (ja) | 1985-04-01 | 1986-10-09 | Eisai Co Ltd | １，４−ジヒドロピリジン誘導体 |
| DK626889A (da) | 1988-12-16 | 1990-06-17 | Roussel Uclaf | Indanderivater, deres fremstilling samt laegemidler med indhold deraf |
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| US9227978B2 (en) * | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| AU2014239542A1 (en) * | 2013-03-15 | 2015-10-01 | Araxes Pharma Llc | Covalent inhibitors of KRas G12C |
| US10196369B2 (en) * | 2013-09-26 | 2019-02-05 | Sanford Burnham Prebys Medical Discovery Institute | Spirocyclic EBI2 modulators |
| CN107835812A (zh) * | 2015-04-03 | 2018-03-23 | 南特生物科学股份有限公司 | 靶向突变体k‑ras 的组合物和方法 |
| US10857140B2 (en) | 2015-05-06 | 2020-12-08 | The Regents Of The University Of California | K-Ras modulators |
| KR20230130747A (ko) | 2016-04-15 | 2023-09-12 | 에피자임, 인코포레이티드 | Ehmt1 및 ehmt2 저해제로서의 아민-치환된 아릴 또는 헤테로아릴 화합물 |
| EP3612526A2 (en) | 2017-04-20 | 2020-02-26 | The Regents of the University of California | K-ras modulators |
-
2016
- 2016-05-06 US US15/571,475 patent/US10857140B2/en not_active Expired - Fee Related
- 2016-05-06 AU AU2016258192A patent/AU2016258192B2/en not_active Ceased
- 2016-05-06 MX MX2017014163A patent/MX2017014163A/es unknown
- 2016-05-06 CA CA2983927A patent/CA2983927A1/en not_active Abandoned
- 2016-05-06 HK HK18111150.3A patent/HK1251485A1/zh unknown
- 2016-05-06 KR KR1020177035079A patent/KR20180017013A/ko not_active Withdrawn
- 2016-05-06 HK HK18111290.4A patent/HK1251972A1/zh unknown
- 2016-05-06 EA EA201792443A patent/EA201792443A1/ru unknown
- 2016-05-06 CN CN201680037365.9A patent/CN107847495A/zh active Pending
- 2016-05-06 WO PCT/US2016/031344 patent/WO2016179558A1/en not_active Ceased
- 2016-05-06 EP EP16790206.3A patent/EP3291813A4/en not_active Withdrawn
- 2016-05-06 BR BR112017023821A patent/BR112017023821A2/pt not_active Application Discontinuation
- 2016-05-06 MA MA042061A patent/MA42061A/fr unknown
- 2016-05-06 JP JP2018510695A patent/JP6771023B2/ja not_active Expired - Fee Related
-
2017
- 2017-11-02 PH PH12017501999A patent/PH12017501999A1/en unknown
- 2017-11-03 IL IL255417A patent/IL255417A/en unknown
- 2017-11-03 CL CL2017002786A patent/CL2017002786A1/es unknown
- 2017-11-06 EC ECIEPI201773743A patent/ECSP17073743A/es unknown
-
2018
- 2018-11-21 CL CL2018003316A patent/CL2018003316A1/es unknown
-
2020
- 2020-10-28 US US17/082,125 patent/US11541044B2/en active Active