JP2022502495A - チロシンキナーゼ阻害剤としてのキナゾリン誘導体、組成物、それらの作製方法、およびそれらの使用 - Google Patents
チロシンキナーゼ阻害剤としてのキナゾリン誘導体、組成物、それらの作製方法、およびそれらの使用 Download PDFInfo
- Publication number
- JP2022502495A JP2022502495A JP2021540390A JP2021540390A JP2022502495A JP 2022502495 A JP2022502495 A JP 2022502495A JP 2021540390 A JP2021540390 A JP 2021540390A JP 2021540390 A JP2021540390 A JP 2021540390A JP 2022502495 A JP2022502495 A JP 2022502495A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- seq
- alkyl
- composition
- amino acid
- 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
- 0 Cc(c(*)c1)cc(*)c1N Chemical compound Cc(c(*)c1)cc(*)c1N 0.000 description 80
- KYCAEEFYFFBAAP-UHFFFAOYSA-N C(C1)C2NCCN1C2 Chemical compound C(C1)C2NCCN1C2 KYCAEEFYFFBAAP-UHFFFAOYSA-N 0.000 description 1
- POOPWPIOIMBTOH-UHFFFAOYSA-N C(C1)C2OC1CNC2 Chemical compound C(C1)C2OC1CNC2 POOPWPIOIMBTOH-UHFFFAOYSA-N 0.000 description 1
- QXTGVGUYRRGVCU-UHFFFAOYSA-N CC(C)N1C(CC2)CN2CC1 Chemical compound CC(C)N1C(CC2)CN2CC1 QXTGVGUYRRGVCU-UHFFFAOYSA-N 0.000 description 1
- HDYGHGLRQXVEGN-UHFFFAOYSA-N CCCCCNC1=C=CC1 Chemical compound CCCCCNC1=C=CC1 HDYGHGLRQXVEGN-UHFFFAOYSA-N 0.000 description 1
- VIBNQGORIPGYGN-UHFFFAOYSA-N Cc(cc1)ccc1OCc1cccc(F)c1 Chemical compound Cc(cc1)ccc1OCc1cccc(F)c1 VIBNQGORIPGYGN-UHFFFAOYSA-N 0.000 description 1
- FIKPOAQRJVKWBX-UHFFFAOYSA-N Cc(cc1)ccc1OCc1ccccn1 Chemical compound Cc(cc1)ccc1OCc1ccccn1 FIKPOAQRJVKWBX-UHFFFAOYSA-N 0.000 description 1
- SSTNIXFHCIOCJI-UHFFFAOYSA-N Cc(cc1)ccc1Oc1ccccc1 Chemical compound Cc(cc1)ccc1Oc1ccccc1 SSTNIXFHCIOCJI-UHFFFAOYSA-N 0.000 description 1
- NDOWDGXOFCPVQR-UHFFFAOYSA-N IN1C2COCC1CC2 Chemical compound IN1C2COCC1CC2 NDOWDGXOFCPVQR-UHFFFAOYSA-N 0.000 description 1
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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862736293P | 2018-09-25 | 2018-09-25 | |
| US62/736,293 | 2018-09-25 | ||
| US201962903592P | 2019-09-20 | 2019-09-20 | |
| US62/903,592 | 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 (2)
| Publication Number | Publication Date |
|---|---|
| JP2022502495A true JP2022502495A (ja) | 2022-01-11 |
| JP2022502495A5 JP2022502495A5 (https=) | 2022-10-03 |
Family
ID=68165800
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021540390A Pending JP2022502495A (ja) | 2018-09-25 | 2019-09-24 | チロシンキナーゼ阻害剤としてのキナゾリン誘導体、組成物、それらの作製方法、およびそれらの使用 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US11034672B1 (https=) |
| EP (1) | EP3856726A1 (https=) |
| JP (1) | JP2022502495A (https=) |
| KR (1) | KR20210137422A (https=) |
| CN (1) | CN113382986A (https=) |
| AU (1) | AU2019346550A1 (https=) |
| BR (1) | BR112021005513A2 (https=) |
| CA (1) | CA3113241A1 (https=) |
| IL (1) | IL281805A (https=) |
| MX (1) | MX2021003517A (https=) |
| SG (1) | SG11202102981SA (https=) |
| WO (1) | WO2020068867A1 (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2022502495A (ja) * | 2018-09-25 | 2022-01-11 | ブラック ダイアモンド セラピューティクス,インコーポレイティド | チロシンキナーゼ阻害剤としてのキナゾリン誘導体、組成物、それらの作製方法、およびそれらの使用 |
| AU2020328598A1 (en) * | 2019-08-15 | 2022-03-03 | Black Diamond Therapeutics, Inc. | Alkynyl quinazoline compounds |
| 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 |
| EP4194443A4 (en) * | 2020-08-10 | 2024-10-09 | Abbisko Therapeutics Co., Ltd. | Efgr inhibitor, preparation method therefor, and application thereof |
| WO2022040377A1 (en) | 2020-08-20 | 2022-02-24 | Black Diamond Therapeutics, Inc. | Methods for preparing quinazoline derivatives |
| JP2023544450A (ja) | 2020-09-23 | 2023-10-23 | エラスカ・インコーポレイテッド | 三環式ピリドン及びピリミドン |
| 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 |
| US20240075042A1 (en) * | 2020-11-02 | 2024-03-07 | Black Diamond Therapeutics, Inc. | Method of treating cancers with alkyne substituted quinazoline derivatives |
| WO2022133345A1 (en) | 2020-12-18 | 2022-06-23 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| 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 |
| 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 |
| 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 |
| CN118084767B (zh) * | 2024-04-02 | 2025-06-17 | 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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999006378A1 (en) * | 1997-07-29 | 1999-02-11 | Warner-Lambert Company | Irreversible inhibitors of tyrosine kinases |
| 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 |
Family Cites Families (53)
| 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 |
| EA001595B1 (ru) | 1996-04-12 | 2001-06-25 | Варнер-Ламберт Компани | Необратимые ингибиторы тирозинкиназ |
| TW436485B (en) | 1997-08-01 | 2001-05-28 | American Cyanamid Co | Substituted quinazoline derivatives |
| 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 |
| UA71945C2 (en) | 1999-01-27 | 2005-01-17 | Pfizer Prod Inc | Substituted bicyclic derivatives being used as anticancer agents |
| PT1154774E (pt) | 1999-02-10 | 2005-10-31 | Astrazeneca Ab | Derivados de quinazolina como inibidores de angiogenese |
| HK1044769B (zh) | 1999-06-21 | 2005-02-25 | 贝林格尔英格海姆法玛两合公司 | 雙環雜環化合物,含有該化合物的藥物組合物,該化合物的用途及其製備方法 |
| 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 |
| WO2001077104A1 (de) | 2000-04-08 | 2001-10-18 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Bicyclische heterocyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung |
| DE10042061A1 (de) | 2000-08-26 | 2002-03-07 | Boehringer Ingelheim Pharma | Bicyclische Heterocyclen,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| AU9598601A (en) | 2000-10-20 | 2002-04-29 | Eisai Co Ltd | Nitrogenous aromatic ring compounds |
| 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 |
| IL160971A0 (en) | 2001-11-30 | 2004-08-31 | Pfizer Prod Inc | Processes for the preparation of substituted bicyclic derivatives for the treatment of abnormal cell growth |
| PT1478648E (pt) | 2002-02-01 | 2014-07-15 | Ariad Pharma Inc | Compostos contendo fósforo e suas utilizações |
| CN100430052C (zh) | 2002-03-05 | 2008-11-05 | 默克弗罗斯特加拿大有限公司 | 组织蛋白酶半胱氨酸蛋白酶抑制剂 |
| 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 |
| AU2004272346A1 (en) | 2003-09-16 | 2005-03-24 | Astrazeneca Ab | Quinazoline derivatives |
| KR20080095915A (ko) | 2004-05-06 | 2008-10-29 | 워너-램버트 캄파니 엘엘씨 | 4-페닐아미노-퀴나졸린-6-일-아미드 |
| ES2377430T3 (es) | 2004-09-02 | 2012-03-27 | Genentech, Inc. | Inhibidores piridílicos de la señalización de hedgehog |
| 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 |
| AU2007296746B2 (en) | 2006-09-11 | 2012-07-05 | 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 |
| EP2205242B1 (en) | 2007-09-12 | 2015-04-15 | Genentech, Inc. | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| JP5348725B2 (ja) | 2007-10-25 | 2013-11-20 | ジェネンテック, インコーポレイテッド | チエノピリミジン化合物の製造方法 |
| US8168784B2 (en) | 2008-06-20 | 2012-05-01 | Abbott Laboratories | Processes to make apoptosis promoters |
| US9006252B2 (en) | 2008-09-26 | 2015-04-14 | National Health Research Institutes | Fused multicyclic compounds as protein kinase inhibitors |
| CN105037333A (zh) * | 2009-12-21 | 2015-11-11 | 张强 | 新的喹唑啉衍生物 |
| 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 |
| CN102382106A (zh) | 2010-08-30 | 2012-03-21 | 黄振华 | 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 |
| WO2012122058A2 (en) | 2011-03-04 | 2012-09-13 | Newgen Therapeutics, Inc. | Alkyne substituted quinazoline compound and methods of use |
| CN102731485B (zh) * | 2011-04-02 | 2016-06-15 | 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 |
| JP6437820B2 (ja) | 2011-07-27 | 2018-12-12 | シャンハイ ファーマシューティカルズ ホールディング カンパニー,リミティド | キナゾリン誘導体、その製造方法、中間体、組成物及びその適用 |
| WO2013131424A1 (zh) | 2012-03-09 | 2013-09-12 | 上海恒瑞医药有限公司 | 4-喹唑啉胺类衍生物及其用途 |
| US9550738B2 (en) * | 2012-05-14 | 2017-01-24 | Hangzhouderenyucheng Biotechnology Ltd | Bicyclic compounds as kinases inhibitors |
| TWI609012B (zh) * | 2013-04-28 | 2017-12-21 | 廣東東陽光藥業有限公司 | 氨基喹唑啉類衍生物及其鹽和使用方法 |
| 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 |
| EP3055290B1 (en) | 2013-10-10 | 2019-10-02 | Araxes Pharma LLC | Inhibitors of kras g12c |
| EP3181553B1 (en) | 2014-08-15 | 2019-12-11 | Arromax Pharmatech Co., Ltd. | Quinazoline derivative, preparation method therefor, and pharmaceutical composition and application thereof |
| WO2016055982A1 (en) * | 2014-10-10 | 2016-04-14 | Acerta Pharma B.V. | Quinoline and quinazoline compounds |
| JP2022502495A (ja) | 2018-09-25 | 2022-01-11 | ブラック ダイアモンド セラピューティクス,インコーポレイティド | チロシンキナーゼ阻害剤としてのキナゾリン誘導体、組成物、それらの作製方法、およびそれらの使用 |
-
2019
- 2019-09-24 JP JP2021540390A patent/JP2022502495A/ja active Pending
- 2019-09-24 WO PCT/US2019/052784 patent/WO2020068867A1/en not_active Ceased
- 2019-09-24 AU AU2019346550A patent/AU2019346550A1/en not_active Abandoned
- 2019-09-24 KR KR1020217011604A patent/KR20210137422A/ko not_active Ceased
- 2019-09-24 SG SG11202102981SA patent/SG11202102981SA/en unknown
- 2019-09-24 CN CN201980077292.XA patent/CN113382986A/zh active Pending
- 2019-09-24 EP EP19783859.2A patent/EP3856726A1/en not_active Withdrawn
- 2019-09-24 MX MX2021003517A patent/MX2021003517A/es unknown
- 2019-09-24 BR BR112021005513-4A patent/BR112021005513A2/pt not_active IP Right Cessation
- 2019-09-24 CA CA3113241A patent/CA3113241A1/en active Pending
-
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 (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999006378A1 (en) * | 1997-07-29 | 1999-02-11 | Warner-Lambert Company | Irreversible inhibitors of tyrosine kinases |
| 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 |
Also Published As
| Publication number | Publication date |
|---|---|
| MX2021003517A (es) | 2021-08-16 |
| AU2019346550A1 (en) | 2021-04-22 |
| CA3113241A1 (en) | 2020-04-02 |
| IL281805A (en) | 2021-05-31 |
| CN113382986A (zh) | 2021-09-10 |
| KR20210137422A (ko) | 2021-11-17 |
| US11034672B1 (en) | 2021-06-15 |
| EP3856726A1 (en) | 2021-08-04 |
| SG11202102981SA (en) | 2021-04-29 |
| US20220363666A1 (en) | 2022-11-17 |
| BR112021005513A2 (pt) | 2021-06-22 |
| US20210163447A1 (en) | 2021-06-03 |
| WO2020068867A1 (en) | 2020-04-02 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2022502495A (ja) | チロシンキナーゼ阻害剤としてのキナゾリン誘導体、組成物、それらの作製方法、およびそれらの使用 | |
| JP7807589B2 (ja) | アルキニルキナゾリン化合物 | |
| WO2024091409A1 (en) | Tricyclic derivatives as kras inhibitors | |
| US20240287100A1 (en) | Alkylidene derivatives as kras inhibitors | |
| KR20230121756A (ko) | Fgfr 억제제 및 이의 제조 및 사용 방법 | |
| JP2017101055A (ja) | テトラヒドロピラニルメチル基を有するピリドン誘導体 | |
| JP2022502496A (ja) | チロシンキナーゼ阻害剤組成物、作製方法、および使用方法 | |
| CA3222549A1 (en) | Combination therapy for cancer treatment | |
| EP4237423B1 (en) | Substituted 1h-pyrazolo[4,3-c]pyridines and derivatives as egfr inhibitors | |
| KR20220070229A (ko) | 아자-퀴놀린 화합물 및 그의 용도 | |
| KR102779693B1 (ko) | Mll1 억제제 및 항암제 | |
| EA048940B1 (ru) | Соединения алкинилхиназолина |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20220922 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20220922 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20230915 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20230926 |
|
| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20240416 |