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 (enExample) | 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 (enExample) |
| EP (1) | EP3291813A4 (enExample) |
| JP (1) | JP6771023B2 (enExample) |
| KR (1) | KR20180017013A (enExample) |
| CN (1) | CN107847495A (enExample) |
| AU (1) | AU2016258192B2 (enExample) |
| BR (1) | BR112017023821A2 (enExample) |
| CA (1) | CA2983927A1 (enExample) |
| CL (2) | CL2017002786A1 (enExample) |
| EA (1) | EA201792443A1 (enExample) |
| EC (1) | ECSP17073743A (enExample) |
| HK (2) | HK1251485A1 (enExample) |
| IL (1) | IL255417A (enExample) |
| MA (1) | MA42061A (enExample) |
| MX (1) | MX2017014163A (enExample) |
| PH (1) | PH12017501999A1 (enExample) |
| WO (1) | WO2016179558A1 (enExample) |
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 |
| MX2017014163A (es) | 2015-05-06 | 2018-08-15 | Univ California | Moduladores de k-ras. |
| CN109843856B (zh) | 2016-05-18 | 2023-05-02 | 米拉蒂治疗股份有限公司 | Kras g12c抑制剂 |
| JP2020517600A (ja) * | 2017-04-20 | 2020-06-18 | ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア | Ｋ−Ｒａｓモジュレーター |
| LT3710439T (lt) | 2017-11-15 | 2023-05-10 | Mirati Therapeutics, Inc. | Kras g12c inhibitoriai |
| US10647715B2 (en) | 2017-11-15 | 2020-05-12 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| WO2019204505A2 (en) * | 2018-04-18 | 2019-10-24 | Theras, Inc. | K-ras modulators with a vinyl sulfonamide moiety |
| WO2019217307A1 (en) | 2018-05-07 | 2019-11-14 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| US12208099B2 (en) | 2018-09-10 | 2025-01-28 | Mirati Therapeutics, Inc. | Combination therapies |
| AU2019340436B2 (en) | 2018-09-10 | 2025-04-17 | Mirati Therapeutics, Inc. | Combination therapies |
| CN112955137B (zh) | 2018-09-10 | 2025-05-13 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| JP2022509724A (ja) | 2018-12-05 | 2022-01-24 | 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 |
| JP7592601B2 (ja) | 2019-01-10 | 2024-12-02 | ミラティ セラピューティクス， インコーポレイテッド | Ｋｒａｓ ｇ１２ｃ阻害剤 |
| WO2020198488A1 (en) * | 2019-03-26 | 2020-10-01 | University Of Massachusetts | Therapeutic targets for oncogenic kras-dependent cancers |
| PH12022550469A1 (en) | 2019-08-29 | 2023-02-27 | Array Biopharma Inc | Kras g12d inhibitors |
| JP2022548791A (ja) | 2019-09-24 | 2022-11-21 | 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 |
| 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 |
| JP2023523323A (ja) * | 2020-04-27 | 2023-06-02 | ベラステム・インコーポレーテッド | 異常な細胞成長を処置する方法 |
| 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 |
| BR112022025550A2 (pt) | 2020-06-18 | 2023-03-07 | Revolution Medicines Inc | Métodos para retardar, prevenir e tratar resistência adquirida aos inibidores de ras |
| KR20230081726A (ko) | 2020-09-03 | 2023-06-07 | 레볼루션 메디슨즈, 인크. | Shp2 돌연변이가 있는 악성 종양을 치료하기 위한 sos1 억제제의 용도 |
| JP2023540809A (ja) | 2020-09-11 | 2023-09-26 | ミラティ セラピューティクス， インコーポレイテッド | Ｋｒａｓ ｇ１２ｃ阻害剤の結晶形態 |
| IL303446A (en) | 2020-12-15 | 2023-08-01 | Mirati Therapeutics Inc | Azaquinazoline compounds as PAN-KRas inhibitors |
| EP4262803A4 (en) | 2020-12-16 | 2025-03-12 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| EP4330228A4 (en) * | 2021-04-26 | 2025-03-26 | 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 |
| KR20250136379A (ko) * | 2023-01-18 | 2025-09-16 | 몰레큘라 악시옴, 엘엘씨 | Kras 발현을 조절하기 위한 조성물 및 이의 용도 |
| 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 |
| AU2024276994A1 (en) | 2023-05-24 | 2025-10-23 | 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 |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| IL111730A (en) * | 1993-11-29 | 1998-12-06 | Fujisawa Pharmaceutical Co | Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same |
| WO1996006078A1 (en) | 1994-08-24 | 1996-02-29 | Pfizer Pharmaceuticals Inc. | N-(2-(pyrrolidinyl-1)-1-phenylethyl)acetamides as kappa receptor antagonists |
| US5475109A (en) | 1994-10-17 | 1995-12-12 | Merck & Co., Inc. | Dioxobutanoic acid derivatives as inhibitors of influenza endonuclease |
| US5631251A (en) | 1995-06-07 | 1997-05-20 | Merck & Co., Inc. | 5-cyclopropyl-1,4 benzodiazepine-2-ones |
| US6953855B2 (en) | 1998-12-11 | 2005-10-11 | Targacept, Inc. | 3-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof |
| IL146543A0 (en) | 1999-06-04 | 2002-07-25 | Astrazeneca Ab | Inhibitors of metalloproteinases |
| EP1202733B1 (en) | 1999-08-12 | 2005-10-05 | Pharmacia Italia S.p.A. | 3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents |
| US20030207910A1 (en) | 2001-02-02 | 2003-11-06 | Tao Wang | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives |
| WO2003004474A1 (en) | 2001-07-06 | 2003-01-16 | Syngenta Participations Ag | Pesticidally active aminoacetonitriles |
| EP1556349A1 (en) * | 2002-10-11 | 2005-07-27 | Astrazeneca AB | 1,4-disubstituted piperidine derivatives and their use as 11-betahsd1 inhibitors |
| KR101146806B1 (ko) * | 2003-03-12 | 2012-05-22 | 메이브릿지 리미티드 | 프탈라지논 유도체 |
| US20050119266A1 (en) * | 2003-10-01 | 2005-06-02 | Yan Shi | Pyrrolidine and piperidine derivatives as factor Xa inhibitors |
| GB0326029D0 (en) * | 2003-11-07 | 2003-12-10 | Astrazeneca Ab | Chemical compounds |
| WO2005047286A1 (ja) | 2003-11-13 | 2005-05-26 | Ono Pharmaceutical Co., Ltd. | スピロ複素環化合物 |
| UA83101C2 (en) | 2003-12-15 | 2008-06-10 | Алмирал Аг | 2,6-bisheteroaryl-4-aminopyrimidines as adenosine receptor antagonists |
| US7399778B2 (en) | 2004-01-16 | 2008-07-15 | Wyeth | Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole |
| WO2007093540A1 (en) | 2006-02-17 | 2007-08-23 | F. Hoffmann-La Roche Ag | Benzoyl-piperidine derivatives as 5ht2/d3 modulators |
| WO2007109154A2 (en) | 2006-03-16 | 2007-09-27 | Renovis, Inc. | Bicycloheteroaryl compounds as p2x7 modulators and uses thereof |
| WO2009015237A1 (en) | 2007-07-23 | 2009-01-29 | Syndax Pharmaceuticals, Inc. | Novel compounds and methods of using them |
| SA08290475B1 (ar) | 2007-08-02 | 2013-06-22 | Targacept Inc | (2s، 3r)-n-(2-((3-بيردينيل)ميثيل)-1-آزا بيسيكلو[2، 2، 2]أوكت-3-يل)بنزو فيوران-2-كربوكساميد، وصور أملاحه الجديدة وطرق استخدامه |
| ES2395704T3 (es) | 2008-12-19 | 2013-02-14 | Novartis Ag | Derivados de isoxazolina y su uso como pesticida |
| PL2434891T3 (pl) | 2009-05-27 | 2020-12-28 | Ptc Therapeutics, Inc. | Sposoby leczenia nowotworu złośliwego i stanów nienowotworowych |
| AR082453A1 (es) | 2010-04-21 | 2012-12-12 | Novartis Ag | Compuestos de furopiridina, composiciones farmaceuticas que los contienen y usos de los mismos |
| US20150087628A1 (en) | 2012-04-10 | 2015-03-26 | The Regents Of The University Of California | Compositions and methods for treating cancer |
| EP2698367A1 (en) | 2012-08-14 | 2014-02-19 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Benzimidazoles for the treatment of cancer |
| WO2014093230A2 (en) | 2012-12-10 | 2014-06-19 | Merck Patent Gmbh | Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity |
| EP2970121B1 (en) * | 2013-03-15 | 2017-12-13 | Araxes Pharma LLC | Covalent inhibitors of kras g12c |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | 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 |
| WO2016161361A1 (en) * | 2015-04-03 | 2016-10-06 | Nantbioscience, Inc. | Compositions and methods of targeting mutant k-ras |
| MX2017014163A (es) | 2015-05-06 | 2018-08-15 | Univ California | Moduladores de k-ras. |
| WO2017181177A1 (en) | 2016-04-15 | 2017-10-19 | Epizyme, Inc. | Amine-substituted aryl or heteroaryl compounds as ehmt1 and ehmt2 inhibitors |
| JP2020517600A (ja) | 2017-04-20 | 2020-06-18 | ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア | Ｋ−Ｒａｓモジュレーター |
-
2016
- 2016-05-06 MX MX2017014163A patent/MX2017014163A/es unknown
- 2016-05-06 HK HK18111150.3A patent/HK1251485A1/zh unknown
- 2016-05-06 HK HK18111290.4A patent/HK1251972A1/zh unknown
- 2016-05-06 EA EA201792443A patent/EA201792443A1/ru unknown
- 2016-05-06 EP EP16790206.3A patent/EP3291813A4/en not_active Withdrawn
- 2016-05-06 KR KR1020177035079A patent/KR20180017013A/ko not_active Withdrawn
- 2016-05-06 AU AU2016258192A patent/AU2016258192B2/en not_active Ceased
- 2016-05-06 BR BR112017023821A patent/BR112017023821A2/pt not_active Application Discontinuation
- 2016-05-06 CA CA2983927A patent/CA2983927A1/en not_active Abandoned
- 2016-05-06 WO PCT/US2016/031344 patent/WO2016179558A1/en not_active Ceased
- 2016-05-06 US US15/571,475 patent/US10857140B2/en not_active Expired - Fee Related
- 2016-05-06 MA MA042061A patent/MA42061A/fr unknown
- 2016-05-06 JP JP2018510695A patent/JP6771023B2/ja not_active Expired - Fee Related
- 2016-05-06 CN CN201680037365.9A patent/CN107847495A/zh active Pending
-
2017
- 2017-11-02 PH PH12017501999A patent/PH12017501999A1/en unknown
- 2017-11-03 CL CL2017002786A patent/CL2017002786A1/es unknown
- 2017-11-03 IL IL255417A patent/IL255417A/en 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