CN115215808B - 用于治疗癌症的组合物和方法 - Google Patents

用于治疗癌症的组合物和方法 Download PDF

Info

Publication number
CN115215808B
CN115215808B CN202210268803.XA CN202210268803A CN115215808B CN 115215808 B CN115215808 B CN 115215808B CN 202210268803 A CN202210268803 A CN 202210268803A CN 115215808 B CN115215808 B CN 115215808B
Authority
CN
China
Prior art keywords
compound
depicts
nmr
cancer
erlotinib
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.)
Active
Application number
CN202210268803.XA
Other languages
English (en)
Chinese (zh)
Other versions
CN115215808A (zh
Inventor
D·A·内桑森
M·E·荣格
J·曾
L·乌纳
P·M·克拉克
T·F·克劳希
G·金姆
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of California San Diego UCSD
Original Assignee
University of California San Diego UCSD
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by University of California San Diego UCSD filed Critical University of California San Diego UCSD
Publication of CN115215808A publication Critical patent/CN115215808A/zh
Application granted granted Critical
Publication of CN115215808B publication Critical patent/CN115215808B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/056Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN202210268803.XA 2019-03-15 2020-03-13 用于治疗癌症的组合物和方法 Active CN115215808B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201962819322P 2019-03-15 2019-03-15
US62/819,322 2019-03-15
US201962904241P 2019-09-23 2019-09-23
US62/904,241 2019-09-23
PCT/US2020/022743 WO2020190765A2 (en) 2019-03-15 2020-03-13 Compositions and methods for treating cancer
CN202080034742.XA CN113811528A (zh) 2019-03-15 2020-03-13 用于治疗癌症的组合物和方法

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN202080034742.XA Division CN113811528A (zh) 2019-03-15 2020-03-13 用于治疗癌症的组合物和方法

Publications (2)

Publication Number Publication Date
CN115215808A CN115215808A (zh) 2022-10-21
CN115215808B true CN115215808B (zh) 2025-04-18

Family

ID=72521289

Family Applications (2)

Application Number Title Priority Date Filing Date
CN202210268803.XA Active CN115215808B (zh) 2019-03-15 2020-03-13 用于治疗癌症的组合物和方法
CN202080034742.XA Pending CN113811528A (zh) 2019-03-15 2020-03-13 用于治疗癌症的组合物和方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN202080034742.XA Pending CN113811528A (zh) 2019-03-15 2020-03-13 用于治疗癌症的组合物和方法

Country Status (17)

Country Link
US (3) US11377451B2 (https=)
EP (1) EP3938354A4 (https=)
JP (2) JP7474269B2 (https=)
KR (1) KR102809395B1 (https=)
CN (2) CN115215808B (https=)
AU (1) AU2020241703B2 (https=)
BR (1) BR112021018295A2 (https=)
CA (1) CA3133688A1 (https=)
CL (1) CL2021002409A1 (https=)
CO (1) CO2021013496A2 (https=)
CR (1) CR20210498A (https=)
IL (1) IL286350A (https=)
MX (1) MX2021011272A (https=)
PH (1) PH12021552208A1 (https=)
SA (1) SA521430328B1 (https=)
SG (1) SG11202109662YA (https=)
WO (1) WO2020190765A2 (https=)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111868039A (zh) * 2017-09-26 2020-10-30 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
KR102809395B1 (ko) 2019-03-15 2025-05-16 더 리전트 오브 더 유니버시티 오브 캘리포니아 암을 치료하기 위한 조성물 및 방법
US20240058340A1 (en) * 2020-09-21 2024-02-22 The Regents Of The University Of California Compositions and methods for treating cancer
WO2022061299A1 (en) * 2020-09-21 2022-03-24 The Regents Of The University Of California Non-invasive functional companion assays for oncogene targeted therapy for brain cancer
WO2022061201A1 (en) * 2020-09-21 2022-03-24 The Regents Of The University Of California Compositions and methods for treating cancer
WO2022155311A1 (en) * 2021-01-14 2022-07-21 The Regents Of The University Of California Methods and systems for analysis of drug target engagement and treatment of cancer
TW202309022A (zh) 2021-04-13 2023-03-01 美商努法倫特公司 用於治療具egfr突變之癌症之胺基取代雜環
US20240165132A1 (en) * 2021-05-12 2024-05-23 Mayo Foundation For Medical Education And Research Methods and materials for treating cancer
CN113307799B (zh) * 2021-05-21 2022-07-19 大连医科大学 一种检测葡萄糖醛酸转移酶1a1荧光探针及其应用
EP4405360A4 (en) * 2021-09-23 2025-08-20 Erasca Inc POLYMORPHIC FORMS OF EGFR INHIBITOR
WO2023244639A1 (en) * 2022-06-14 2023-12-21 The Regents Of The University Of California Methods of predicting cns cancer response to treatment with egfr inhibitors
WO2024081447A1 (en) * 2022-10-14 2024-04-18 The Regents Of The University Of California Egfr inhibitors for treating lung cancer
WO2024102177A1 (en) * 2022-11-08 2024-05-16 The Regents Of The University Of California Combination therapies for the treatment of brain cancer
WO2025117739A1 (en) * 2023-11-27 2025-06-05 Erasca, Inc. Compositions and methods for treating cancer

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5538325A (en) * 1978-09-11 1980-03-17 Sankyo Co Ltd 4-anilinoquinazoline derivative and its preparation
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US6706721B1 (en) 1998-04-29 2004-03-16 Osi Pharmaceuticals, Inc. N-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate anhydrate and monohydrate
KR100397792B1 (ko) * 2001-06-28 2003-09-13 한국과학기술연구원 4-(페닐아미노)-[1,4]디옥사노[2,3-g]퀴나졸린 유도체 및그의 제조방법
CN1854130B (zh) 2005-04-15 2011-04-20 中国医学科学院药物研究所 喹唑啉衍生物、及其制法和药物组合物与用途
WO2008046242A1 (fr) 2006-10-16 2008-04-24 Institute Of Mataria Medica, Chinese Academy Of Medical Sciences Nouveaux dérivés quinazolines, leurs procédés de préparation et leurs utilisations
WO2011035540A1 (zh) 2009-09-28 2011-03-31 齐鲁制药有限公司 作为酪氨酸激酶抑制剂的4-(取代苯胺基)喹唑啉衍生物
ITPD20110091A1 (it) 2011-03-24 2012-09-25 Univ Padova Inibitori multitirosinchinasi utili per le patologie correlate: modelli farmacoforici, composti identificati tramite questi modelli, metodi per la loro preparazione, la loro formulazione e il loro impiego terapeutico.
NZ732511A (en) * 2014-12-15 2018-11-30 Univ Michigan Regents Small molecule inhibitors of egfr and pi3k
CA2974442A1 (en) * 2015-02-03 2016-08-11 Trillium Therapeutics Inc. Novel fluorinated derivatives as egfr inhibitors useful for treating cancers
CN105017163A (zh) 2015-08-25 2015-11-04 佛山市赛维斯医药科技有限公司 双乙氧基苯并喹唑啉类酪氨酸激酶抑制剂、制备方法及其用途
US10473255B2 (en) 2015-12-29 2019-11-12 Ge-Hitachi Nuclear Energy Americas Llc Reactor pressure vessel including pipe restraint device, and/or a pipe restraint device
AU2017204973A1 (en) 2016-01-06 2018-07-12 Trillium Therapeutics Inc. Novel fluorinated quinazoline derivatives as EGFR inhibitors
CN106432202B (zh) 2016-09-22 2019-04-02 郑州大学第一附属医院 喹唑啉类衍生物及其应用
CN111868039A (zh) * 2017-09-26 2020-10-30 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
KR102809395B1 (ko) 2019-03-15 2025-05-16 더 리전트 오브 더 유니버시티 오브 캘리포니아 암을 치료하기 위한 조성물 및 방법
WO2022061201A1 (en) 2020-09-21 2022-03-24 The Regents Of The University Of California Compositions and methods for treating cancer
US20240058340A1 (en) 2020-09-21 2024-02-22 The Regents Of The University Of California Compositions and methods for treating cancer
WO2022061299A1 (en) 2020-09-21 2022-03-24 The Regents Of The University Of California Non-invasive functional companion assays for oncogene targeted therapy for brain cancer
EP4405360A4 (en) * 2021-09-23 2025-08-20 Erasca Inc POLYMORPHIC FORMS OF EGFR INHIBITOR
WO2023244639A1 (en) * 2022-06-14 2023-12-21 The Regents Of The University Of California Methods of predicting cns cancer response to treatment with egfr inhibitors

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
"7-Substituted-[1, 4]dioxano[2, 3-g]quinazolines as Inhibitors of Epidermal Growth Factor Receptor Kinase";Jae Yeol Lee等;《Arch. Pharm. Pharm. Med. Chem.,》;第35卷(第10期);第487–494页 *
"Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors";Tsang, Jonathan E.等;《ACS Medicinal Chemistry Letters》;第11卷(第10期);第1799-1809页 *
Jae Du Ha等."Design and Synthesis of Novel Epidermal Growth Factor Receptor Kinase Inhibitors".《Bull. Korean Chem. Soc.,》.2005,第26卷(第6期),第959-965页. *

Also Published As

Publication number Publication date
CA3133688A1 (en) 2020-09-24
CL2021002409A1 (es) 2022-06-17
CN115215808A (zh) 2022-10-21
EP3938354A2 (en) 2022-01-19
SG11202109662YA (en) 2021-10-28
AU2020241703A1 (en) 2021-10-14
US20220064177A1 (en) 2022-03-03
CO2021013496A2 (es) 2022-01-17
SA521430328B1 (ar) 2024-03-28
PH12021552208A1 (en) 2022-05-30
WO2020190765A3 (en) 2020-11-26
JP7789832B2 (ja) 2025-12-22
JP2024102094A (ja) 2024-07-30
AU2020241703B2 (en) 2026-02-05
US11377451B2 (en) 2022-07-05
IL286350A (en) 2021-10-31
KR20210151820A (ko) 2021-12-14
JP2022526266A (ja) 2022-05-24
WO2020190765A2 (en) 2020-09-24
KR102809395B1 (ko) 2025-05-16
CR20210498A (es) 2022-01-11
US20250145634A1 (en) 2025-05-08
US20230115366A1 (en) 2023-04-13
EP3938354A4 (en) 2022-12-28
JP7474269B2 (ja) 2024-04-24
CN113811528A (zh) 2021-12-17
BR112021018295A2 (pt) 2021-11-23
MX2021011272A (es) 2021-10-01

Similar Documents

Publication Publication Date Title
CN115215808B (zh) 用于治疗癌症的组合物和方法
AU2023282187B2 (en) Compositions and methods for treating cancer
JP6193268B2 (ja) Cdk8/cdk19選択的阻害剤、ならびに癌のための抗転移および化学防御の方法におけるそれらの使用
US9073916B2 (en) Prodrug forms of kinase inhibitors and their use in therapy
TW202140485A (zh) 化合物及其用途
US20240058340A1 (en) Compositions and methods for treating cancer
WO2022061201A1 (en) Compositions and methods for treating cancer
HK40083017A (en) Compositions and methods for treating cancer
HK40062377A (en) Compositions and methods for treating cancer
WO2013144632A1 (en) Treatment of proliferative diseases with pyrimidodiazepinones
EA044668B1 (ru) Композиции и способы для лечения рака
WO2014106763A1 (en) Pyridopyrazines as anticancer agents
HK40037064A (en) Compositions and methods for treating cancer
US20180303797A1 (en) Chalcone Compounds
Goerguen et al. MLN-8237

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40083017

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant