CN113382986A - 酪氨酸激酶抑制剂组合物、其制备方法和使用方法 - Google Patents
酪氨酸激酶抑制剂组合物、其制备方法和使用方法 Download PDFInfo
- Publication number
- CN113382986A CN113382986A CN201980077292.XA CN201980077292A CN113382986A CN 113382986 A CN113382986 A CN 113382986A CN 201980077292 A CN201980077292 A CN 201980077292A CN 113382986 A CN113382986 A CN 113382986A
- Authority
- CN
- China
- Prior art keywords
- compound
- seq
- hal
- composition
- alkyl
- 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.)
- Pending
Links
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K31/535—Heterocyclic 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/535—Heterocyclic 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
-
- 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
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/74—Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
- C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
-
- 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
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D403/06—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 only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/14—Heterocyclic 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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
- C07D417/14—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
- 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
- C07D471/08—Bridged systems
-
- 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
- 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
- C07D487/08—Bridged systems
-
- 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
- C07D487/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D491/02—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 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D491/02—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 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D491/02—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 in which the condensed system contains two hetero rings
- C07D491/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D491/02—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 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D491/02—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 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (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)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862736293P | 2018-09-25 | 2018-09-25 | |
| US62/736293 | 2018-09-25 | ||
| US201962903592P | 2019-09-20 | 2019-09-20 | |
| US62/903592 | 2019-09-20 | ||
| PCT/US2019/052784 WO2020068867A1 (en) | 2018-09-25 | 2019-09-24 | Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN113382986A true CN113382986A (zh) | 2021-09-10 |
Family
ID=68165800
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980077292.XA Pending CN113382986A (zh) | 2018-09-25 | 2019-09-24 | 酪氨酸激酶抑制剂组合物、其制备方法和使用方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US11034672B1 (enExample) |
| EP (1) | EP3856726A1 (enExample) |
| JP (1) | JP2022502495A (enExample) |
| KR (1) | KR20210137422A (enExample) |
| CN (1) | CN113382986A (enExample) |
| AU (1) | AU2019346550A1 (enExample) |
| BR (1) | BR112021005513A2 (enExample) |
| CA (1) | CA3113241A1 (enExample) |
| IL (1) | IL281805A (enExample) |
| MX (1) | MX2021003517A (enExample) |
| SG (1) | SG11202102981SA (enExample) |
| WO (1) | WO2020068867A1 (enExample) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114787150A (zh) * | 2019-08-15 | 2022-07-22 | 黑钻治疗公司 | 炔基喹唑啉化合物 |
| CN116655599A (zh) * | 2023-05-17 | 2023-08-29 | 江南大学 | 一类egfr别构抑制剂的合成及其用途 |
| CN118084767A (zh) * | 2024-04-02 | 2024-05-28 | 康龙化成手性医药技术(宁波)有限公司 | 一种外型-6-氟甲基-3-氮杂双环[3,1,0]己烷盐酸盐及其衍生物的合成方法 |
| CN118652239A (zh) * | 2024-05-29 | 2024-09-17 | 江南大学 | 一类egfr别构抑制剂的合成及其用途 |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20210137422A (ko) | 2018-09-25 | 2021-11-17 | 블랙 다이아몬드 테라퓨틱스, 인코포레이티드 | 티로신 키나아제 억제제로서의 퀴나졸린 유도체, 조성물, 이들의 제조 방법 및 이들의 용도 |
| WO2021195206A1 (en) * | 2020-03-24 | 2021-09-30 | Black Diamond Therapeutics, Inc. | Polymorphic forms and related uses |
| TWI782504B (zh) * | 2020-05-08 | 2022-11-01 | 美商美國禮來大藥廠 | (三氟甲基)嘧啶-2-胺化合物 |
| WO2022006386A1 (en) * | 2020-07-02 | 2022-01-06 | Enliven Therapeutics, Inc. | Alkyne quinazoline derivatives as inhibitors of erbb2 |
| CA3188077A1 (en) * | 2020-08-10 | 2022-02-17 | Fei Yang | Egfr inhibitor, preparation method therefor and application thereof |
| WO2022040377A1 (en) | 2020-08-20 | 2022-02-24 | Black Diamond Therapeutics, Inc. | Methods for preparing quinazoline derivatives |
| MX2023003338A (es) | 2020-09-23 | 2023-06-14 | Erasca Inc | Piridonas y pirimidonas tricíclicas. |
| WO2022076671A1 (en) * | 2020-10-08 | 2022-04-14 | Black Diamond Therapeutics, Inc. | Method of treating cancers using quinazoline derivatives |
| CN116710096A (zh) * | 2020-11-02 | 2023-09-05 | 黑钻治疗公司 | 用炔取代的喹唑啉衍生物治疗癌症的方法 |
| TWI910256B (zh) * | 2020-11-02 | 2026-01-01 | 美商黑鑽醫療公司 | 使用經炔取代之喹唑啉衍生物類以治療癌症之方法 |
| US20230107642A1 (en) | 2020-12-18 | 2023-04-06 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| CA3213079A1 (en) | 2021-04-13 | 2022-10-20 | Kristin Lynne ANDREWS | Amino-substituted heterocycles for treating cancers with egfr mutations |
| EP4724436A1 (en) * | 2023-06-12 | 2026-04-15 | Remix Therapeutics Inc. | Compounds and methods for modulating splicing |
| WO2025096300A1 (en) * | 2023-10-30 | 2025-05-08 | Eli Lilly And Company | Novel methods for the preparation of 3-azabicylco[3.1,0]hexane-6-carboxamide derivatives |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6127374A (en) * | 1997-07-29 | 2000-10-03 | Warner-Lambert Company | Irreversible inhibitors of tyrosine kinases |
| WO2012136099A1 (zh) * | 2011-04-02 | 2012-10-11 | 齐鲁制药有限公司 | 4-(取代苯氨基)喹唑啉衍生物及其制备方法、药物组合物和用途 |
| US20130035350A1 (en) * | 2009-12-21 | 2013-02-07 | Qiang Zhang | Novel Quinazoline Derivatives |
| CN103965120A (zh) * | 2013-01-25 | 2014-08-06 | 上海医药集团股份有限公司 | 喹啉及喹唑啉衍生物、制备方法、中间体、组合物及应用 |
| US20150126537A1 (en) * | 2012-05-14 | 2015-05-07 | Hangzhouderenyucheng Biotechnology Ltd | Bicyclic compounds as kinases inhibitors |
| US20160039838A1 (en) * | 2013-04-28 | 2016-02-11 | Sunshine Lake Pharma Co., Ltd. | Aminoquinazoline derivatives and their salts and methods of use thereof |
| WO2016055982A1 (en) * | 2014-10-10 | 2016-04-14 | Acerta Pharma B.V. | Quinoline and quinazoline compounds |
Family Cites Families (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6041077B2 (ja) | 1976-09-06 | 1985-09-13 | 喜徳 喜谷 | 1,2‐ジアミノシクロヘキサン異性体のシス白金(2)錯体 |
| US4261989A (en) | 1979-02-19 | 1981-04-14 | Kaken Chemical Co. Ltd. | Geldanamycin derivatives and antitumor drug |
| US5266573A (en) | 1989-08-07 | 1993-11-30 | Elf Sanofi | Trifluoromethylphenyltetrahydropyridines for the treatment and/or prophylaxis of intestinal motility disorders |
| EP0647450A1 (en) | 1993-09-09 | 1995-04-12 | BEHRINGWERKE Aktiengesellschaft | Improved prodrugs for enzyme mediated activation |
| DE69536015D1 (de) | 1995-03-30 | 2009-12-10 | Pfizer Prod Inc | Chinazolinone Derivate |
| US5763263A (en) | 1995-11-27 | 1998-06-09 | Dehlinger; Peter J. | Method and apparatus for producing position addressable combinatorial libraries |
| JP3370340B2 (ja) | 1996-04-12 | 2003-01-27 | ワーナー―ランバート・コンパニー | チロシンキナーゼの不可逆的阻害剤 |
| TW436485B (en) | 1997-08-01 | 2001-05-28 | American Cyanamid Co | Substituted quinazoline derivatives |
| UA71945C2 (en) | 1999-01-27 | 2005-01-17 | Pfizer Prod Inc | Substituted bicyclic derivatives being used as anticancer agents |
| JP3270834B2 (ja) | 1999-01-27 | 2002-04-02 | ファイザー・プロダクツ・インク | 抗がん剤として有用なヘテロ芳香族二環式誘導体 |
| BRPI0017548B8 (pt) | 1999-02-10 | 2023-05-02 | Astrazeneca Ab | Composto |
| YU90901A (sh) | 1999-06-21 | 2004-07-15 | Boehringer Ingelheim Pharma Gmbh. & Co.Kg. | Biciklični heterocikli, lekovi koji sadrže ta jedinjenja, njihova primena i postupci za njihovo pripremanje |
| PE20010306A1 (es) | 1999-07-02 | 2001-03-29 | Agouron Pharma | Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa |
| GB0018891D0 (en) | 2000-08-01 | 2000-09-20 | Novartis Ag | Organic compounds |
| CA2403152C (en) | 2000-04-08 | 2008-10-28 | Boehringer Ingelheim Pharma Kg | Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them |
| DE10042061A1 (de) | 2000-08-26 | 2002-03-07 | Boehringer Ingelheim Pharma | Bicyclische Heterocyclen,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| EP1415987B1 (en) | 2000-10-20 | 2007-02-28 | Eisai R&D Management Co., Ltd. | Nitrogenous aromatic ring compounds as anti cancer agents |
| DE10063435A1 (de) | 2000-12-20 | 2002-07-04 | Boehringer Ingelheim Pharma | Chinazolinderviate,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| US6995162B2 (en) | 2001-01-12 | 2006-02-07 | Amgen Inc. | Substituted alkylamine derivatives and methods of use |
| BR0214606A (pt) | 2001-11-30 | 2004-09-14 | Pfizer Prod Inc | Processos para a preparação de derivados bicìclicos substituìdos para o tratamento de crescimento de célula anormal |
| BR0307544A (pt) | 2002-02-01 | 2004-12-07 | Ariad Gene Therapeutics Inc | Compostos contendo fósforos, componentes e composição bem como, sua utilização através de métodos de tratamentos |
| JP4201716B2 (ja) | 2002-03-05 | 2008-12-24 | メルク フロスト カナダ リミテツド | カテプシンシステインプロテアーゼ阻害剤 |
| DE10217689A1 (de) | 2002-04-19 | 2003-11-13 | Boehringer Ingelheim Pharma | Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, ihre Verwendung und Verfahren zu ihrer Herstellung |
| TWI275390B (en) | 2002-04-30 | 2007-03-11 | Wyeth Corp | Process for the preparation of 7-substituted-3- quinolinecarbonitriles |
| PE20040945A1 (es) | 2003-02-05 | 2004-12-14 | Warner Lambert Co | Preparacion de quinazolinas substituidas |
| US7399865B2 (en) | 2003-09-15 | 2008-07-15 | Wyeth | Protein tyrosine kinase enzyme inhibitors |
| US20070032513A1 (en) | 2003-09-16 | 2007-02-08 | Hennequin Laurent F A | Quinazoline derivatives |
| AP2204A (en) | 2004-05-06 | 2011-02-07 | Warner Lambert Co | 4-phenylamino-quinazolin-6-yl-amides. |
| KR20200019263A (ko) | 2004-09-02 | 2020-02-21 | 제넨테크, 인크. | 헤지호그 신호전달에 대한 피리딜 억제제 |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| PE20070207A1 (es) | 2005-07-22 | 2007-03-09 | Genentech Inc | Tratamiento combinado de los tumores que expresan el her |
| WO2007055513A1 (en) | 2005-11-08 | 2007-05-18 | Hanmi Pharm. Co., Ltd. | Quinazoline derivatives as a signal transduction inhibitor and method for the preparation thereof |
| US8604044B2 (en) | 2006-09-11 | 2013-12-10 | Curis, Inc. | Quinazoline based EGFR inhibitors containing a zinc binding moiety |
| TWI377944B (en) | 2007-06-05 | 2012-12-01 | Hanmi Holdings Co Ltd | Novel amide derivative for inhibiting the growth of cancer cells |
| AU2008298948B2 (en) | 2007-09-12 | 2014-09-04 | F. Hoffmann-La Roche Ag | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| EP2214675B1 (en) | 2007-10-25 | 2013-11-20 | Genentech, Inc. | Process for making thienopyrimidine compounds |
| US8168784B2 (en) | 2008-06-20 | 2012-05-01 | Abbott Laboratories | Processes to make apoptosis promoters |
| EP2331530B8 (en) | 2008-09-26 | 2013-12-25 | National Health Research Institutes | Fused multicyclic compounds as protein kinase inhibitors |
| CN102382106A (zh) | 2010-08-30 | 2012-03-21 | 黄振华 | 苯胺取代的喹唑啉衍生物 |
| CN102382065B (zh) | 2010-08-30 | 2014-05-28 | 山东轩竹医药科技有限公司 | 苯胺取代的喹唑啉衍生物 |
| CN102452989B (zh) | 2010-10-19 | 2014-10-22 | 山东轩竹医药科技有限公司 | 苯胺取代的喹唑啉衍生物 |
| KR102061743B1 (ko) | 2011-03-04 | 2020-01-03 | 뉴젠 세러퓨틱스 인코포레이티드 | 알킨 치환된 퀴나졸린 화합물 및 그것의 사용 방법 |
| CN102898386B (zh) | 2011-07-27 | 2015-07-29 | 上海医药集团股份有限公司 | 喹唑啉衍生物、其制备方法、中间体、组合物及其应用 |
| CN103987700B (zh) | 2012-03-09 | 2016-08-31 | 江苏豪森药业集团有限公司 | 4-喹唑啉胺类衍生物及其用途 |
| CN104513229A (zh) | 2013-09-28 | 2015-04-15 | 正大天晴药业集团股份有限公司 | 喹唑啉衍生物及其制备方法 |
| JP6559123B2 (ja) | 2013-10-10 | 2019-08-14 | アラクセス ファーマ エルエルシー | Krasg12cの阻害剤 |
| US10196365B2 (en) | 2014-08-15 | 2019-02-05 | Arromax Pharmatech Co., Ltd. | Quinazoline derivative, preparation method therefor, and pharmaceutical composition and application thereof |
| KR20210137422A (ko) | 2018-09-25 | 2021-11-17 | 블랙 다이아몬드 테라퓨틱스, 인코포레이티드 | 티로신 키나아제 억제제로서의 퀴나졸린 유도체, 조성물, 이들의 제조 방법 및 이들의 용도 |
-
2019
- 2019-09-24 KR KR1020217011604A patent/KR20210137422A/ko not_active Ceased
- 2019-09-24 CA CA3113241A patent/CA3113241A1/en active Pending
- 2019-09-24 CN CN201980077292.XA patent/CN113382986A/zh active Pending
- 2019-09-24 JP JP2021540390A patent/JP2022502495A/ja active Pending
- 2019-09-24 BR BR112021005513-4A patent/BR112021005513A2/pt not_active IP Right Cessation
- 2019-09-24 WO PCT/US2019/052784 patent/WO2020068867A1/en not_active Ceased
- 2019-09-24 SG SG11202102981SA patent/SG11202102981SA/en unknown
- 2019-09-24 EP EP19783859.2A patent/EP3856726A1/en not_active Withdrawn
- 2019-09-24 AU AU2019346550A patent/AU2019346550A1/en not_active Abandoned
- 2019-09-24 MX MX2021003517A patent/MX2021003517A/es unknown
-
2020
- 2020-04-17 US US16/851,767 patent/US11034672B1/en active Active
-
2021
- 2021-03-12 US US17/200,743 patent/US20220363666A1/en not_active Abandoned
- 2021-03-25 IL IL281805A patent/IL281805A/en unknown
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6127374A (en) * | 1997-07-29 | 2000-10-03 | Warner-Lambert Company | Irreversible inhibitors of tyrosine kinases |
| US20130035350A1 (en) * | 2009-12-21 | 2013-02-07 | Qiang Zhang | Novel Quinazoline Derivatives |
| WO2012136099A1 (zh) * | 2011-04-02 | 2012-10-11 | 齐鲁制药有限公司 | 4-(取代苯氨基)喹唑啉衍生物及其制备方法、药物组合物和用途 |
| US20150126537A1 (en) * | 2012-05-14 | 2015-05-07 | Hangzhouderenyucheng Biotechnology Ltd | Bicyclic compounds as kinases inhibitors |
| CN103965120A (zh) * | 2013-01-25 | 2014-08-06 | 上海医药集团股份有限公司 | 喹啉及喹唑啉衍生物、制备方法、中间体、组合物及应用 |
| US20160039838A1 (en) * | 2013-04-28 | 2016-02-11 | Sunshine Lake Pharma Co., Ltd. | Aminoquinazoline derivatives and their salts and methods of use thereof |
| WO2016055982A1 (en) * | 2014-10-10 | 2016-04-14 | Acerta Pharma B.V. | Quinoline and quinazoline compounds |
Non-Patent Citations (1)
| Title |
|---|
| M. ASADOLLAHI-BABOLI: "In silico evaluation, molecular docking and QSAR analisis of quinazoline-based EGFR-T790M inhibitors", MOL. DIVERS, vol. 20, pages 729 - 739, XP035999887, DOI: 10.1007/s11030-016-9672-0 * |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114787150A (zh) * | 2019-08-15 | 2022-07-22 | 黑钻治疗公司 | 炔基喹唑啉化合物 |
| US12435046B2 (en) | 2019-08-15 | 2025-10-07 | Black Diamond Therapeutics, Inc. | Alkynyl quinazoline compounds |
| CN116655599A (zh) * | 2023-05-17 | 2023-08-29 | 江南大学 | 一类egfr别构抑制剂的合成及其用途 |
| CN116655599B (zh) * | 2023-05-17 | 2025-07-29 | 江南大学 | 一类egfr别构抑制剂的合成及其用途 |
| CN118084767A (zh) * | 2024-04-02 | 2024-05-28 | 康龙化成手性医药技术(宁波)有限公司 | 一种外型-6-氟甲基-3-氮杂双环[3,1,0]己烷盐酸盐及其衍生物的合成方法 |
| CN118652239A (zh) * | 2024-05-29 | 2024-09-17 | 江南大学 | 一类egfr别构抑制剂的合成及其用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| BR112021005513A2 (pt) | 2021-06-22 |
| CA3113241A1 (en) | 2020-04-02 |
| US20220363666A1 (en) | 2022-11-17 |
| MX2021003517A (es) | 2021-08-16 |
| AU2019346550A1 (en) | 2021-04-22 |
| IL281805A (en) | 2021-05-31 |
| WO2020068867A1 (en) | 2020-04-02 |
| SG11202102981SA (en) | 2021-04-29 |
| KR20210137422A (ko) | 2021-11-17 |
| US11034672B1 (en) | 2021-06-15 |
| JP2022502495A (ja) | 2022-01-11 |
| US20210163447A1 (en) | 2021-06-03 |
| EP3856726A1 (en) | 2021-08-04 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US11034672B1 (en) | Tyrosine kinase inhibitor compositions, methods of making and methods of use | |
| US12435046B2 (en) | Alkynyl quinazoline compounds | |
| TWI848901B (zh) | Shp2磷酸酶抑制劑及其使用方法 | |
| CN107787323B (zh) | 用于抑制shp2活性的化合物和组合物 | |
| CN104144926B (zh) | 噁唑烷-2-酮化合物及其作为磷脂酰肌醇-3-激酶抑制剂的用途 | |
| IL324078A (en) | Fused ring compounds | |
| TW201629065A (zh) | 三唑并嘧啶化合物及其用途 | |
| TW201408658A (zh) | 絲胺酸/酥胺酸激酶抑制劑 | |
| CN110003178A (zh) | 二杂芳基化合物及其用途 | |
| EP3373934B1 (en) | Crystalline form of a substituted quinoline compound and pharmaceutical compositions thereof | |
| CN113348170A (zh) | 联苯类衍生物抑制剂、其制备方法和应用 | |
| CA3222549A1 (en) | Combination therapy for cancer treatment | |
| JP2025529821A (ja) | Kif18a阻害剤及びその使用 | |
| CN113164776A (zh) | 酪氨酸激酶抑制剂组合物、其制备方法和使用方法 | |
| KR20260023023A (ko) | Wrn 억제제 | |
| HK40121649A (zh) | 炔基喹唑啉化合物 | |
| HK40116977A (zh) | 氮杂-四环氧氮杂䓬化合物及其用途 | |
| HK40102590A (zh) | 用於癌症治疗的组合疗法 | |
| HK40049641A (en) | Biphenyl derivative inhibitor, preparation method therefor and use | |
| EA048940B1 (ru) | Соединения алкинилхиназолина |
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 | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20210910 |