CN114430741A - Egfr抑制剂、组合物及其制备方法 - Google Patents
Egfr抑制剂、组合物及其制备方法 Download PDFInfo
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- CN114430741A CN114430741A CN202080066249.6A CN202080066249A CN114430741A CN 114430741 A CN114430741 A CN 114430741A CN 202080066249 A CN202080066249 A CN 202080066249A CN 114430741 A CN114430741 A CN 114430741A
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- Prior art keywords
- compound
- amino
- cancer
- phenyl
- egfr
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- 150000003839 salts Chemical class 0.000 claims description 34
- -1 -C1-6Alkyl Inorganic materials 0.000 claims description 25
- WQAWEUZTDVWTDB-UHFFFAOYSA-N dimethyl(oxo)phosphanium Chemical compound C[P+](C)=O WQAWEUZTDVWTDB-UHFFFAOYSA-N 0.000 claims description 13
- 239000003814 drug Substances 0.000 claims description 12
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 12
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- 229940002612 prodrug Drugs 0.000 claims description 8
- 239000012453 solvate Substances 0.000 claims description 8
- 229910052794 bromium Inorganic materials 0.000 claims description 7
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- 239000003937 drug carrier Substances 0.000 claims description 7
- 125000005842 heteroatom Chemical group 0.000 claims description 7
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- 229910052736 halogen Inorganic materials 0.000 claims description 6
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- 125000001072 heteroaryl group Chemical group 0.000 claims description 5
- 125000000623 heterocyclic group Chemical group 0.000 claims description 5
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- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 8
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- 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
- C07D403/10—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 linked by a carbon chain containing aromatic rings
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- 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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
涉及式I化合物,使用这些化合物作为EGFR抑制剂的方法,以及包含这些化合物的药物组合物。该化合物可用于治疗、预防或改善诸如癌症或感染的疾病或病症。
Description
PCT国内申请,说明书已公开。
Claims (21)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CNPCT/CN2019/111636 | 2019-10-17 | ||
CN2019111636 | 2019-10-17 | ||
PCT/CN2020/120611 WO2021073498A1 (zh) | 2019-10-17 | 2020-10-13 | Egfr抑制剂、组合物及其制备方法 |
Publications (1)
Publication Number | Publication Date |
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CN114430741A true CN114430741A (zh) | 2022-05-03 |
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CN202080066249.6A Pending CN114430741A (zh) | 2019-10-17 | 2020-10-13 | Egfr抑制剂、组合物及其制备方法 |
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Country | Link |
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US (1) | US20230133169A1 (zh) |
CN (1) | CN114430741A (zh) |
WO (1) | WO2021073498A1 (zh) |
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EP4393930A1 (en) | 2021-08-27 | 2024-07-03 | Chengdu Di'Ao Jiuhong Pharmaceutical Factory | Crystal forms, preparation method and application of aryl phosphine oxide compound |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2009126515A1 (en) * | 2008-04-07 | 2009-10-15 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
WO2009143389A1 (en) * | 2008-05-21 | 2009-11-26 | Ariad Pharmaceuticals, Inc. | Phosphorous derivatives as kinase inhibitors |
WO2012151561A1 (en) * | 2011-05-04 | 2012-11-08 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
CN103153064A (zh) * | 2010-10-14 | 2013-06-12 | 阿里亚德医药股份有限公司 | 抑制egfr导致的癌症中细胞增殖的方法 |
WO2018108064A1 (zh) * | 2016-12-13 | 2018-06-21 | 南京明德新药研发股份有限公司 | 作为第四代egfr激酶抑制剂的螺环芳基磷氧化合物 |
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WO2009126515A1 (en) * | 2008-04-07 | 2009-10-15 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
WO2009143389A1 (en) * | 2008-05-21 | 2009-11-26 | Ariad Pharmaceuticals, Inc. | Phosphorous derivatives as kinase inhibitors |
CN103153064A (zh) * | 2010-10-14 | 2013-06-12 | 阿里亚德医药股份有限公司 | 抑制egfr导致的癌症中细胞增殖的方法 |
WO2012151561A1 (en) * | 2011-05-04 | 2012-11-08 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
WO2018108064A1 (zh) * | 2016-12-13 | 2018-06-21 | 南京明德新药研发股份有限公司 | 作为第四代egfr激酶抑制剂的螺环芳基磷氧化合物 |
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