CN107835812A - 靶向突变体k‑ras 的组合物和方法 - Google Patents
靶向突变体k‑ras 的组合物和方法 Download PDFInfo
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- CN107835812A CN107835812A CN201680032351.8A CN201680032351A CN107835812A CN 107835812 A CN107835812 A CN 107835812A CN 201680032351 A CN201680032351 A CN 201680032351A CN 107835812 A CN107835812 A CN 107835812A
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- compound
- dmso
- kras
- alkyl
- bases
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/44—Acylated amino or imino radicals
- C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/06—Peri-condensed systems
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- C07—ORGANIC CHEMISTRY
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
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- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Description
化合物 | G-LISA(野生型) | G-LISA(G12D) | G-LISA(G12V) |
A0837/4562 | 0.5 | 7-13 | 38 |
4639 | n/a | >25 | n/a |
4662 | n/a | >25 | n/a |
4663 | 7 | >25 | 32 |
4664 | n/a | >25 | n/a |
4665 | n/a | >25 | n/a |
4666 | n/a | >25 | n/a |
4683 | n/a | 11.89 | n/a |
4684 | n/a | >25 | n/a |
4685 | n/a | >25 | n/a |
4686 | n/a | 11 | n/a |
4687 | n/a | 19 | n/a |
4734 | n/a | >25 | n/a |
4735 | n/a | >25 | n/a |
4747 | n/a | >25 | n/a |
4748 | n/a | 21 | n/a |
4749 | n/a | 36 | n/a |
4800 | n/a | >25 | n/a |
4801 | 25.7 | 8.2 | 10.7 |
4802 | n/a | 27 | 17 |
4803 | n/a | 71 | n/a |
4805 | 7 | 187 | n/a |
4824 | n/a | >25 | n/a |
4825 | n/a | >25 | n/a |
4826 | n/a | >25 | n/a |
2827 | >25 | 36.6 | n/a |
4828 | n/a | >25 | n/a |
4829 | n/a | >25 | n/a |
4874 | n/a | 16 | n/a |
4875 | n/a | 17 | n/a |
4877 | 16 | 6 | 9 |
4878 | n/a | 19 | >25 |
4888 | 11.3 | 6 | 14.5 |
Claims (36)
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US201562142974P | 2015-04-03 | 2015-04-03 | |
US62/142,974 | 2015-04-03 | ||
PCT/US2016/025697 WO2016161361A1 (en) | 2015-04-03 | 2016-04-01 | Compositions and methods of targeting mutant k-ras |
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CN107835812A true CN107835812A (zh) | 2018-03-23 |
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CN201680032351.8A Pending CN107835812A (zh) | 2015-04-03 | 2016-04-01 | 靶向突变体k‑ras 的组合物和方法 |
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US (1) | US10487078B2 (zh) |
EP (1) | EP3277678B1 (zh) |
JP (1) | JP2018511614A (zh) |
KR (1) | KR20170132332A (zh) |
CN (1) | CN107835812A (zh) |
AU (1) | AU2016244017B2 (zh) |
CA (1) | CA2981677A1 (zh) |
IL (1) | IL254811A0 (zh) |
WO (1) | WO2016161361A1 (zh) |
Cited By (2)
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WO2022198905A1 (zh) * | 2021-03-26 | 2022-09-29 | 浙江海正药业股份有限公司 | 三环类衍生物及其制备方法和用途 |
CN115702025A (zh) * | 2020-04-16 | 2023-02-14 | 因赛特公司 | 稠合三环kras抑制剂 |
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CA2983927A1 (en) | 2015-05-06 | 2016-11-10 | The Regents Of The University Of California | K-ras modulators |
SG11201804901WA (en) | 2015-12-22 | 2018-07-30 | SHY Therapeutics LLC | Compounds for the treatment of cancer and inflammatory disease |
IL262794B2 (en) | 2016-05-10 | 2023-10-01 | Univ Nat Corp Tokyo Medical & Dental | An inhibitor of the expression of a pro-inflammatory factor, a masking method for its active component, a useful expression cassette for said method, a diagnostic factor and a diagnosis method |
US10344026B2 (en) * | 2017-01-18 | 2019-07-09 | Nantbio, Inc. | Compositions and methods of targeting mutant K-ras |
EP3573964A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Benzothiophene and benzothiazole compounds and methods of use thereof |
JP2020505395A (ja) * | 2017-01-26 | 2020-02-20 | アラクセス ファーマ エルエルシー | 縮合n−複素環式化合物およびその使用方法 |
JP2020512981A (ja) * | 2017-03-31 | 2020-04-30 | カーザ グローバル,リミティド ライアビリティ カンパニー | 置換2−アミノイミダゾールを含む組成物と方法 |
MX2019012532A (es) | 2017-04-20 | 2019-12-02 | Univ California | Moduladores de k-ras. |
JOP20190272A1 (ar) * | 2017-05-22 | 2019-11-21 | Amgen Inc | مثبطات kras g12c وطرق لاستخدامها |
WO2018218069A1 (en) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant kras, hras or nras |
CN111032662A (zh) | 2017-06-21 | 2020-04-17 | 尚医治疗有限责任公司 | 与ras超家族相互作用的用于治疗癌症、炎性疾病、ras蛋白病和纤维化疾病的化合物 |
IL274456B2 (en) * | 2017-11-09 | 2024-08-01 | National Univ Corporation Tokyo Medical And Dental Univ | Inhibitor of expression of pro-carcinogenic factors, screening method for an active ingredient thereof, expression cassette used in this method, diagnostic drug and diagnostic method |
WO2020033413A2 (en) * | 2018-08-07 | 2020-02-13 | Tosk, Inc. | Modulators of ras gtpase |
WO2020159942A1 (en) | 2019-01-29 | 2020-08-06 | Tosk, Inc. | Pyrazolopyrimidine modulators of ras gtpase |
KR102222693B1 (ko) * | 2019-04-04 | 2021-03-04 | 금정제약 주식회사 | H-rev107 유래 펩타이드의 신규한 용도 |
WO2021231526A1 (en) | 2020-05-13 | 2021-11-18 | Incyte Corporation | Fused pyrimidine compounds as kras inhibitors |
KR102488353B1 (ko) * | 2020-10-08 | 2023-01-12 | 부산대학교 산학협력단 | 돌연변이 kras를 표적하는 펩타이드 및 이의 용도 |
KR20230016158A (ko) * | 2021-07-22 | 2023-02-01 | 국립암센터 | Kras 돌연변이 특이적 저해제 및 이를 포함하는 암 예방 또는 치료용 조성물 |
WO2023049697A1 (en) | 2021-09-21 | 2023-03-30 | Incyte Corporation | Hetero-tricyclic compounds as inhibitors of kras |
EP4408536A1 (en) | 2021-10-01 | 2024-08-07 | Incyte Corporation | Pyrazoloquinoline kras inhibitors |
US11939328B2 (en) | 2021-10-14 | 2024-03-26 | Incyte Corporation | Quinoline compounds as inhibitors of KRAS |
WO2024040131A1 (en) | 2022-08-17 | 2024-02-22 | Treeline Biosciences, Inc. | Pyridopyrimidine kras inhibitors |
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US10344026B2 (en) | 2017-01-18 | 2019-07-09 | Nantbio, Inc. | Compositions and methods of targeting mutant K-ras |
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2016
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- 2016-04-01 EP EP16774366.5A patent/EP3277678B1/en active Active
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- 2016-04-01 JP JP2017552081A patent/JP2018511614A/ja not_active Ceased
- 2016-04-01 CA CA2981677A patent/CA2981677A1/en not_active Abandoned
- 2016-04-01 CN CN201680032351.8A patent/CN107835812A/zh active Pending
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
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CN115702025A (zh) * | 2020-04-16 | 2023-02-14 | 因赛特公司 | 稠合三环kras抑制剂 |
WO2022198905A1 (zh) * | 2021-03-26 | 2022-09-29 | 浙江海正药业股份有限公司 | 三环类衍生物及其制备方法和用途 |
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EP3277678A4 (en) | 2018-08-15 |
WO2016161361A1 (en) | 2016-10-06 |
CA2981677A1 (en) | 2016-10-06 |
KR20170132332A (ko) | 2017-12-01 |
US10487078B2 (en) | 2019-11-26 |
IL254811A0 (en) | 2017-12-31 |
EP3277678B1 (en) | 2020-03-18 |
EP3277678A1 (en) | 2018-02-07 |
WO2016161361A4 (en) | 2016-12-22 |
JP2018511614A (ja) | 2018-04-26 |
AU2016244017B2 (en) | 2020-07-23 |
AU2016244017A1 (en) | 2017-10-26 |
US20180086752A1 (en) | 2018-03-29 |
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