CN113784718A - 对携带酪氨酸激酶抑制剂抗性egfr突变的癌细胞具有抗肿瘤活性的化合物 - Google Patents

对携带酪氨酸激酶抑制剂抗性egfr突变的癌细胞具有抗肿瘤活性的化合物 Download PDF

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CN113784718A
CN113784718A CN202080032255.XA CN202080032255A CN113784718A CN 113784718 A CN113784718 A CN 113784718A CN 202080032255 A CN202080032255 A CN 202080032255A CN 113784718 A CN113784718 A CN 113784718A
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cancer
tki
egfr
mutations
mutation
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J·罗比丘
M·尼尔森
J·V·海马赫
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University of Texas System
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CN202080032255.XA 2019-04-17 2020-04-16 对携带酪氨酸激酶抑制剂抗性egfr突变的癌细胞具有抗肿瘤活性的化合物 Pending CN113784718A (zh)

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US201962835354P 2019-04-17 2019-04-17
US62/835,354 2019-04-17
PCT/US2020/028547 WO2020214831A1 (en) 2019-04-17 2020-04-16 Compounds with anti-tumor activity against cancer cells bearing tyrosine kinase inhibitor resistant egfr mutations

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US (1) US20220193074A1 (https=)
EP (1) EP3955928A4 (https=)
JP (1) JP7822597B2 (https=)
KR (1) KR20220003546A (https=)
CN (1) CN113784718A (https=)
CA (1) CA3132816A1 (https=)
WO (1) WO2020214831A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115998743A (zh) * 2023-01-16 2023-04-25 威尚（上海）生物医药有限公司 喹唑啉类化合物在克服奥希替尼耐药中的用途

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112021016149A2 (pt) 2019-02-26 2021-10-13 Janssen Biotech, Inc. Terapias de combinação e estratificação de pacientes com anticorpos biespecíficos anti-egfr/c-met
US11850248B2 (en) 2019-05-14 2023-12-26 Yuhan Corporation Therapies with 3rd generation EGFR tyrosine kinase inhibitors
US11879013B2 (en) 2019-05-14 2024-01-23 Janssen Biotech, Inc. Combination therapies with bispecific anti-EGFR/c-Met antibodies and third generation EGFR tyrosine kinase inhibitors
JP7783182B2 (ja) 2020-02-12 2025-12-09 ヤンセン バイオテツク，インコーポレーテツド ｃ－ＭＥＴエクソン１４スキッピング変異を有する患者の治療
MX2024008057A (es) 2021-12-30 2024-08-28 Biomea Fusion Inc Compuestos de pirazina como inhibidores de flt3.
WO2024097994A1 (en) * 2022-11-03 2024-05-10 Board Of Regents, The University Of Texas System Methods for the detection and treatment of non-small-cell lung cancer

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018094225A1 (en) * 2016-11-17 2018-05-24 Board Of Regents, The University Of Texas System Compounds with anti-tumor activity against cancer cells bearing egfr or her2 exon 20 mutations
WO2018156812A1 (en) * 2017-02-22 2018-08-30 G1 Therapeutics, Inc. Treatment of egfr-driven cancer with fewer side effects

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2017136709A (ru) * 2015-04-23 2019-05-23 Медиммьюн Лимитед Комбинированное лечение немелкоклеточного рака легкого с выявленной мутацией в egfr

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018094225A1 (en) * 2016-11-17 2018-05-24 Board Of Regents, The University Of Texas System Compounds with anti-tumor activity against cancer cells bearing egfr or her2 exon 20 mutations
WO2018156812A1 (en) * 2017-02-22 2018-08-30 G1 Therapeutics, Inc. Treatment of egfr-driven cancer with fewer side effects

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
YOSHIHISA KOBAYASHI，ET AL.: "EGFR Exon 18 Mutations in Lung Cancer: Molecular Predictors of Augmented Sensitivity to Afatinib or Neratinib as Compared with First- or Third- Generation TKIs", CLINICAL CANCER RESEARCH, vol. 21, no. 23, pages 5305 - 5313, XP093040178, DOI: 10.1158/1078-0432.CCR-15-1046 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115998743A (zh) * 2023-01-16 2023-04-25 威尚（上海）生物医药有限公司 喹唑啉类化合物在克服奥希替尼耐药中的用途
CN115998743B (zh) * 2023-01-16 2024-05-28 威尚（上海）生物医药有限公司 喹唑啉类化合物在克服奥希替尼耐药中的用途
WO2024153256A1 (zh) * 2023-01-16 2024-07-25 威尚（上海）生物医药有限公司 喹唑啉类化合物在克服奥希替尼耐药中的用途
GB2641652A (en) * 2023-01-16 2025-12-10 Weishang Shanghai Bio Pharmaceutical Co Ltd Use of quinazoline compound in overcoming Osimertinib drug resistance

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JP2022529016A (ja) 2022-06-16
WO2020214831A1 (en) 2020-10-22
KR20220003546A (ko) 2022-01-10
EP3955928A4 (en) 2023-05-31
JP7822597B2 (ja) 2026-03-03
US20220193074A1 (en) 2022-06-23
CA3132816A1 (en) 2020-10-22
EP3955928A1 (en) 2022-02-23

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