CN115298174A - 嘧啶并杂环类化合物及其应用 - Google Patents
嘧啶并杂环类化合物及其应用 Download PDFInfo
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- CN115298174A CN115298174A CN202180021254.XA CN202180021254A CN115298174A CN 115298174 A CN115298174 A CN 115298174A CN 202180021254 A CN202180021254 A CN 202180021254A CN 115298174 A CN115298174 A CN 115298174A
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 24
- 125000001624 naphthyl group Chemical group 0.000 claims description 22
- 239000000126 substance Substances 0.000 claims description 18
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- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 9
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- 238000011580 nude mouse model Methods 0.000 description 1
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- 238000011533 pre-incubation Methods 0.000 description 1
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- JWHAUXFOSRPERK-UHFFFAOYSA-N propafenone Chemical compound CCCNCC(O)COC1=CC=CC=C1C(=O)CCC1=CC=CC=C1 JWHAUXFOSRPERK-UHFFFAOYSA-N 0.000 description 1
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- ZDYVRSLAEXCVBX-UHFFFAOYSA-N pyridinium p-toluenesulfonate Chemical compound C1=CC=[NH+]C=C1.CC1=CC=C(S([O-])(=O)=O)C=C1 ZDYVRSLAEXCVBX-UHFFFAOYSA-N 0.000 description 1
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- 108700042226 ras Genes Proteins 0.000 description 1
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- 230000021014 regulation of cell growth Effects 0.000 description 1
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- 102200006532 rs112445441 Human genes 0.000 description 1
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- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
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- WRIKHQLVHPKCJU-UHFFFAOYSA-N sodium bis(trimethylsilyl)amide Chemical compound C[Si](C)(C)N([Na])[Si](C)(C)C WRIKHQLVHPKCJU-UHFFFAOYSA-N 0.000 description 1
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- BEOOHQFXGBMRKU-UHFFFAOYSA-N sodium cyanoborohydride Chemical compound [Na+].[B-]C#N BEOOHQFXGBMRKU-UHFFFAOYSA-N 0.000 description 1
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- ISIJQEHRDSCQIU-UHFFFAOYSA-N tert-butyl 2,7-diazaspiro[4.5]decane-7-carboxylate Chemical compound C1N(C(=O)OC(C)(C)C)CCCC11CNCC1 ISIJQEHRDSCQIU-UHFFFAOYSA-N 0.000 description 1
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- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
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- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
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- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- PJVWKTKQMONHTI-UHFFFAOYSA-N warfarin Chemical compound OC=1C2=CC=CC=C2OC(=O)C=1C(CC(=O)C)C1=CC=CC=C1 PJVWKTKQMONHTI-UHFFFAOYSA-N 0.000 description 1
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- 230000003442 weekly effect Effects 0.000 description 1
- LQUPKVMEAATBSL-UHFFFAOYSA-L zinc;2,3,4-trichlorophenolate Chemical compound [Zn+2].[O-]C1=CC=C(Cl)C(Cl)=C1Cl.[O-]C1=CC=C(Cl)C(Cl)=C1Cl LQUPKVMEAATBSL-UHFFFAOYSA-L 0.000 description 1
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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- C—CHEMISTRY; METALLURGY
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- 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
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
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- C07D—HETEROCYCLIC COMPOUNDS
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- C—CHEMISTRY; METALLURGY
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- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
Abstract
一类嘧啶并杂环类化合物,具体公开了式(III)所示化合物或其药学上可接受的盐。
Description
PCT国内申请,说明书已公开。
Claims (22)
- PCT国内申请,权利要求书已公开。
Priority Applications (2)
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CN202311017911.0A CN117050079A (zh) | 2020-03-12 | 2021-03-11 | 嘧啶并杂环类化合物及其应用 |
CN202311335558.0A CN117510492A (zh) | 2020-03-12 | 2021-03-11 | 嘧啶并杂环类化合物及其应用 |
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CN202010953203 | 2020-09-11 | ||
CN202011593642 | 2020-12-29 | ||
CN2020115936429 | 2020-12-29 | ||
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EP (1) | EP4105211A4 (zh) |
JP (2) | JP2023517995A (zh) |
KR (1) | KR20220152295A (zh) |
CN (3) | CN115298174B (zh) |
AU (2) | AU2021233058A1 (zh) |
BR (2) | BR112022018140B1 (zh) |
CA (2) | CA3171365A1 (zh) |
IL (1) | IL296357A (zh) |
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WO (1) | WO2021180181A1 (zh) |
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WO2019217307A1 (en) | 2018-05-07 | 2019-11-14 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
EP3908283A4 (en) | 2019-01-10 | 2022-10-12 | Mirati Therapeutics, Inc. | KRAS G12C INHIBITORS |
JP2022546043A (ja) | 2019-08-29 | 2022-11-02 | ミラティ セラピューティクス, インコーポレイテッド | Kras g12d阻害剤 |
KR20220091480A (ko) | 2019-09-24 | 2022-06-30 | 미라티 테라퓨틱스, 인크. | 병용 요법 |
CA3163218A1 (en) * | 2019-12-02 | 2021-06-10 | Shanghai Yingli Pharmaceutical Co., Ltd | Oxygen-containing heterocyclic compound, preparation method therefor and use thereof |
IL294048A (en) | 2019-12-20 | 2022-08-01 | Mirati Therapeutics Inc | sos1 inhibitors |
US20220112204A1 (en) * | 2020-10-14 | 2022-04-14 | Accutar Biotechnology Inc. | Substituted dihydropyranopyrimidine compounds as kras inhibitors |
US20230107642A1 (en) | 2020-12-18 | 2023-04-06 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
WO2022235870A1 (en) | 2021-05-05 | 2022-11-10 | Revolution Medicines, Inc. | Ras inhibitors for the treatment of cancer |
CR20230570A (es) | 2021-05-05 | 2024-01-22 | Revolution Medicines Inc | Inhibidores de ras |
TWI820901B (zh) * | 2021-09-10 | 2023-11-01 | 大陸商德昇濟醫藥(無錫)有限公司 | 嘧啶並雜環類化合物的晶型及其製備方法 |
AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
TW202340214A (zh) | 2021-12-17 | 2023-10-16 | 美商健臻公司 | 做為shp2抑制劑之吡唑并吡𠯤化合物 |
CN114539246A (zh) * | 2021-12-30 | 2022-05-27 | 苏州闻天医药科技有限公司 | 一种哌啶并嘧啶类化合物及其用途 |
EP4227307A1 (en) | 2022-02-11 | 2023-08-16 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
WO2023172940A1 (en) | 2022-03-08 | 2023-09-14 | Revolution Medicines, Inc. | Methods for treating immune refractory lung cancer |
WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
WO2023246914A1 (zh) * | 2022-06-24 | 2023-12-28 | 南京明德新药研发有限公司 | 杂环取代的嘧啶并吡喃类化合物及其应用 |
WO2024081674A1 (en) | 2022-10-11 | 2024-04-18 | Aadi Bioscience, Inc. | Combination therapies for the treatment of cancer |
Citations (3)
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WO2020035031A1 (en) * | 2018-08-16 | 2020-02-20 | Genentech, Inc. | Fused ring compounds |
WO2020239123A1 (zh) * | 2019-05-31 | 2020-12-03 | 上海翰森生物医药科技有限公司 | 芳香杂环类衍生物调节剂、其制备方法和应用 |
CN112390788A (zh) * | 2019-08-13 | 2021-02-23 | 苏州闻天医药科技有限公司 | 一种用于抑制krasg12c突变蛋白的化合物及其制备方法和用途 |
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ES2863873T3 (es) * | 2016-05-18 | 2021-10-11 | Mirati Therapeutics Inc | Inhibidores de KRAS G12C |
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WO2020035031A1 (en) * | 2018-08-16 | 2020-02-20 | Genentech, Inc. | Fused ring compounds |
WO2020239123A1 (zh) * | 2019-05-31 | 2020-12-03 | 上海翰森生物医药科技有限公司 | 芳香杂环类衍生物调节剂、其制备方法和应用 |
CN112390788A (zh) * | 2019-08-13 | 2021-02-23 | 苏州闻天医药科技有限公司 | 一种用于抑制krasg12c突变蛋白的化合物及其制备方法和用途 |
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JP2024045251A (ja) | 2024-04-02 |
CN117510492A (zh) | 2024-02-06 |
US20240116934A1 (en) | 2024-04-11 |
EP4105211A4 (en) | 2023-09-06 |
BR112022018140B1 (pt) | 2024-02-15 |
JP2023517995A (ja) | 2023-04-27 |
US20230151004A1 (en) | 2023-05-18 |
CN115298174B (zh) | 2023-11-03 |
IL296357A (en) | 2022-11-01 |
CA3171365A1 (en) | 2021-09-16 |
MX2022011283A (es) | 2022-11-16 |
CN117050079A (zh) | 2023-11-14 |
AU2021233058A1 (en) | 2022-10-13 |
BR122023026304A2 (pt) | 2024-01-16 |
EP4105211A1 (en) | 2022-12-21 |
BR112022018140A2 (pt) | 2022-11-22 |
AU2024201366A1 (en) | 2024-03-21 |
KR20220152295A (ko) | 2022-11-15 |
WO2021180181A1 (zh) | 2021-09-16 |
CA3232127A1 (en) | 2021-09-16 |
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