FI3929190T3 - Yhdisteitä ja koostumuksia EGFR-mutanttikinaasin aktiivisuuksien moduloimiseksi - Google Patents
Yhdisteitä ja koostumuksia EGFR-mutanttikinaasin aktiivisuuksien moduloimiseksi Download PDFInfo
- Publication number
- FI3929190T3 FI3929190T3 FIEP21171619.6T FI21171619T FI3929190T3 FI 3929190 T3 FI3929190 T3 FI 3929190T3 FI 21171619 T FI21171619 T FI 21171619T FI 3929190 T3 FI3929190 T3 FI 3929190T3
- Authority
- FI
- Finland
- Prior art keywords
- formula
- compound
- alkyl
- membered
- organic solvent
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims 16
- 108091000080 Phosphotransferase Proteins 0.000 title 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 title 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 title 1
- 102000020233 phosphotransferase Human genes 0.000 title 1
- 238000000034 method Methods 0.000 claims 15
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 11
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims 9
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 claims 9
- 239000003960 organic solvent Substances 0.000 claims 9
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 8
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 125000002950 monocyclic group Chemical group 0.000 claims 7
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 6
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- FXHOOIRPVKKKFG-UHFFFAOYSA-N N,N-Dimethylacetamide Chemical compound CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- 239000002904 solvent Substances 0.000 claims 4
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- SJRJJKPEHAURKC-UHFFFAOYSA-N N-Methylmorpholine Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 claims 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- SCYULBFZEHDVBN-UHFFFAOYSA-N 1,1-Dichloroethane Chemical compound CC(Cl)Cl SCYULBFZEHDVBN-UHFFFAOYSA-N 0.000 claims 2
- PAYRUJLWNCNPSJ-UHFFFAOYSA-N Aniline Chemical compound NC1=CC=CC=C1 PAYRUJLWNCNPSJ-UHFFFAOYSA-N 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 101100516572 Caenorhabditis elegans nhr-8 gene Proteins 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- -1 Cs 2 CO 3 Chemical compound 0.000 claims 2
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 claims 2
- DKGAVHZHDRPRBM-UHFFFAOYSA-N Tert-Butanol Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 claims 2
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Natural products CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 239000003638 chemical reducing agent Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- LPNYRYFBWFDTMA-UHFFFAOYSA-N potassium tert-butoxide Chemical compound [K+].CC(C)(C)[O-] LPNYRYFBWFDTMA-UHFFFAOYSA-N 0.000 claims 2
- MFRIHAYPQRLWNB-UHFFFAOYSA-N sodium tert-butoxide Chemical compound [Na+].CC(C)(C)[O-] MFRIHAYPQRLWNB-UHFFFAOYSA-N 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- HFBMWMNUJJDEQZ-UHFFFAOYSA-N acryloyl chloride Chemical compound ClC(=O)C=C HFBMWMNUJJDEQZ-UHFFFAOYSA-N 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 239000003054 catalyst Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 239000003446 ligand Substances 0.000 claims 1
- DLEDOFVPSDKWEF-UHFFFAOYSA-N lithium butane Chemical compound [Li+].CCC[CH2-] DLEDOFVPSDKWEF-UHFFFAOYSA-N 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- MZRVEZGGRBJDDB-UHFFFAOYSA-N n-Butyllithium Substances [Li]CCCC MZRVEZGGRBJDDB-UHFFFAOYSA-N 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 229910052763 palladium Inorganic materials 0.000 claims 1
- 238000006268 reductive amination reaction Methods 0.000 claims 1
- 150000003457 sulfones Chemical class 0.000 claims 1
- 150000003462 sulfoxides Chemical class 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 125000003944 tolyl group Chemical group 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/14—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 three or more hetero 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Quick-Acting Or Multi-Walled Pipe Joints (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462063394P | 2014-10-13 | 2014-10-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| FI3929190T3 true FI3929190T3 (fi) | 2025-02-28 |
Family
ID=55654993
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FIEP21171619.6T FI3929190T3 (fi) | 2014-10-13 | 2015-10-13 | Yhdisteitä ja koostumuksia EGFR-mutanttikinaasin aktiivisuuksien moduloimiseksi |
| FIC20250023C FIC20250023I1 (fi) | 2014-10-13 | 2025-06-06 | Latsertinibi kaikissa peruspatentin suojaamissa muodoissa |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FIC20250023C FIC20250023I1 (fi) | 2014-10-13 | 2025-06-06 | Latsertinibi kaikissa peruspatentin suojaamissa muodoissa |
Country Status (30)
| Country | Link |
|---|---|
| US (2) | US9593098B2 (OSRAM) |
| EP (4) | EP3207035B1 (OSRAM) |
| JP (3) | JP6524221B2 (OSRAM) |
| KR (5) | KR20240074820A (OSRAM) |
| CN (2) | CN111686110B (OSRAM) |
| AU (1) | AU2015331166B2 (OSRAM) |
| BR (1) | BR112017007769B1 (OSRAM) |
| CA (1) | CA2962914C (OSRAM) |
| CY (2) | CY1122737T1 (OSRAM) |
| DK (3) | DK3207035T3 (OSRAM) |
| ES (3) | ES2879474T3 (OSRAM) |
| FI (2) | FI3929190T3 (OSRAM) |
| FR (1) | FR25C1021I1 (OSRAM) |
| HR (3) | HRP20250213T1 (OSRAM) |
| HU (4) | HUE054848T2 (OSRAM) |
| LT (4) | LT3207035T (OSRAM) |
| MX (3) | MX2017003181A (OSRAM) |
| NL (1) | NL301329I2 (OSRAM) |
| NO (1) | NO2025025I1 (OSRAM) |
| NZ (1) | NZ730012A (OSRAM) |
| PH (1) | PH12017500488A1 (OSRAM) |
| PL (3) | PL3604294T3 (OSRAM) |
| PT (3) | PT3207035T (OSRAM) |
| RS (3) | RS61865B1 (OSRAM) |
| RU (1) | RU2727700C2 (OSRAM) |
| SG (1) | SG11201701960XA (OSRAM) |
| SI (3) | SI3207035T1 (OSRAM) |
| SM (3) | SMT202100266T1 (OSRAM) |
| TW (2) | TWI730331B (OSRAM) |
| WO (1) | WO2016060443A2 (OSRAM) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20250213T1 (hr) | 2014-10-13 | 2025-04-25 | Yuhan Corporation | Spojevi i pripravci za modulaciju aktivnosti egfr mutantne kinaze |
| US9938257B2 (en) | 2015-09-11 | 2018-04-10 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| JP2019501222A (ja) | 2016-01-07 | 2019-01-17 | シーエス ファーマテック リミテッド | Egfrチロシンキナーゼの臨床的に重要な変異体の選択的阻害薬 |
| EP3464275B1 (en) | 2016-05-26 | 2024-05-08 | Recurium IP Holdings, LLC | Egfr inhibitor compounds |
| KR102030886B1 (ko) * | 2016-09-23 | 2019-10-10 | 재단법인 대구경북첨단의료산업진흥재단 | 신규한 이미다졸일 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
| AR111469A1 (es) * | 2017-04-21 | 2019-07-17 | Yuhan Corp | Sal de un compuesto del derivado de aminopiridina, una forma cristalina de la misma, y un proceso para preparar la misma |
| KR102388312B1 (ko) * | 2017-06-13 | 2022-04-19 | 베이징 아다메이들 바이오테크놀로지 리미티드 라이어빌리티 컴퍼니 | 아미노피리미딘 화합물, 이의 제조방법 및 용도 |
| DK3658552T3 (da) | 2017-07-28 | 2023-11-20 | Yuhan Corp | Fremgangsmåde til fremstilling af n-(5-((4-(4-((dimethylamino)methyl)-3-phenyl-1h-pyrazol-1-yl)pyrimidin-2-yl)amino)-4-methoxy-2-morpholinophenyl)acrylamid ved reaktion af den tilsvarende amin med et 3-halogen-propionylchlorid |
| HUE059501T2 (hu) * | 2017-07-28 | 2022-11-28 | Yuhan Corp | Aminopirimidin származékok elõállításához alkalmas intermedierek, eljárás elõállításukra, és eljárás aminopirimidin származékok elõállítására azok alkalmazásával |
| PT3658547T (pt) * | 2017-07-28 | 2023-10-20 | Yuhan Corp | Processo de preparação de n -(5 -(4 -(4 -formil -3- fenil- 1h -pirazol- 1 -il)pirimidin -2- ilamino) -4 -metoxi 2- morfolinofenil) acrilamida |
| WO2019042187A1 (zh) | 2017-08-30 | 2019-03-07 | 深圳市塔吉瑞生物医药有限公司 | 一种氨基嘧啶类化合物及包含该化合物的组合物及其用途 |
| CN108047207A (zh) * | 2018-01-30 | 2018-05-18 | 天津大学 | N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-2-氟代丙烯酰胺氘代物及应用 |
| CN108017633A (zh) * | 2018-01-30 | 2018-05-11 | 天津大学 | N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-2-氟代丙烯酰胺衍生物及应用 |
| EP3849538A4 (en) | 2018-09-10 | 2022-06-29 | Mirati Therapeutics, Inc. | Combination therapies |
| KR20200043618A (ko) * | 2018-10-18 | 2020-04-28 | 주식회사유한양행 | 아미노피리미딘 유도체 또는 이의 염을 포함하는 경구투여용 약학 조성물 |
| CN111349084B (zh) * | 2018-12-21 | 2022-11-25 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制蛋白激酶活性的氨基嘧啶类化合物 |
| AU2020229467A1 (en) | 2019-02-26 | 2021-08-12 | Janssen Biotech, Inc. | Combination therapies and patient stratification with bispecific anti-EGFR/c-met antibodies |
| PL3943491T3 (pl) * | 2019-03-19 | 2025-11-17 | Voronoi Inc. | Pochodna heteroarylowa, sposób jej wytwarzania i kompozycja farmaceutyczna zawierająca ją jako skuteczny składnik |
| US12157730B2 (en) | 2019-03-19 | 2024-12-03 | Voronoi Inc. | Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component |
| CN111747950B (zh) | 2019-03-29 | 2024-01-23 | 深圳福沃药业有限公司 | 用于治疗癌症的嘧啶衍生物 |
| MX2021011810A (es) | 2019-03-29 | 2021-10-26 | Astrazeneca Ab | Osimertinib para su uso en el tratamiento de cancer de pulmon de celulas no peque?as. |
| PH12021552798A1 (en) | 2019-05-14 | 2022-09-19 | Janssen Biotech Inc | Combination therapies with bispecific anti-egfr/c-met antibodies and 3rd generation egfr tyrosine kinase inhibitors |
| US11850248B2 (en) * | 2019-05-14 | 2023-12-26 | Yuhan Corporation | Therapies with 3rd generation EGFR tyrosine kinase inhibitors |
| CA3140360A1 (en) * | 2019-05-14 | 2020-11-19 | Janssen Biotech, Inc. | Combination therapies with bispecific anti-egfr/c-met antibodies and 3rd generation egfr tyrosine kinase inhibitors |
| CN110128354A (zh) * | 2019-06-20 | 2019-08-16 | 大连大学 | 一种5-氟-2-甲磺酰基-4-氨基嘧啶的制备方法 |
| KR20210032093A (ko) | 2019-09-16 | 2021-03-24 | 제이투에이치바이오텍 (주) | Egfr 돌연변이 키나제 성장 억제 효과를 나타내는 피리미딘 유도체 및 이의 의약 용도 |
| WO2021094379A1 (en) | 2019-11-12 | 2021-05-20 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| AU2021211871A1 (en) | 2020-01-20 | 2022-09-08 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| JOP20220184A1 (ar) | 2020-02-12 | 2023-01-30 | Janssen Biotech Inc | علاج مصابي السرطان ممن لديهم طفرات تخطي c-Met إكسون14 |
| TW202207940A (zh) | 2020-04-14 | 2022-03-01 | 美商健生生物科技公司 | 包含胺基嘧啶衍生物或其醫藥上可接受之鹽、水合物、或溶劑化物之用於經口投予之醫藥組成物 |
| US20210369709A1 (en) | 2020-05-27 | 2021-12-02 | Astrazeneca Ab | EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER |
| KR20210152312A (ko) * | 2020-06-08 | 2021-12-15 | 주식회사 종근당 | 카나비노이드 수용체 (cb1 수용체) 길항제로서의 4-(4,5-디하이드로-1h-피라졸-1-닐)피리미딘 화합물 및 이를 포함하는 약제학적 조성물 |
| KR20230069958A (ko) | 2020-09-14 | 2023-05-19 | 얀센 파마슈티카 엔.브이. | Fgfr 억제제 조합 요법 |
| TWI867047B (zh) * | 2020-09-18 | 2024-12-21 | 南韓商沃若諾伊公司 | 雜芳基衍生物、其製備方法、及含彼作為活性成份之藥學組成物 |
| TW202227425A (zh) * | 2020-09-18 | 2022-07-16 | 南韓商沃若諾伊生物公司 | 雜芳基衍生物、彼之製法、及包含彼作為活性成份之藥學組成物 |
| WO2022131741A1 (ko) * | 2020-12-14 | 2022-06-23 | 보로노이바이오 주식회사 | 아이소옥사졸리딘 유도체 화합물 및 이의 용도 |
| EP4335847A1 (en) * | 2021-05-07 | 2024-03-13 | Voronoi Inc. | Heteroaryl derivative, method for preparing same, and pharmaceutical composition comprising same as active ingredient |
| CA3180295A1 (en) | 2021-05-17 | 2022-11-24 | Youn Ho Lee | Heteroaryl derivative compounds, and uses thereof |
| CN117425651A (zh) | 2021-06-01 | 2024-01-19 | 杭州领业医药科技有限公司 | Lazertinib甲磺酸盐的水合物晶型及其制备方法和用途 |
| KR102685187B1 (ko) | 2021-10-15 | 2024-07-16 | 제이투에이치바이오텍 (주) | Alk 및/또는 egfr 돌연변이 키나제 억제 효과를 나타내는 화합물 및 이의 의약 용도 |
| TW202342057A (zh) | 2022-02-07 | 2023-11-01 | 美商健生生物科技公司 | 用於減少用egfr/met雙特異性抗體治療之患者的輸注相關反應之方法 |
| CA3255389A1 (en) | 2022-03-31 | 2023-10-05 | Astrazeneca Ab | Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors in Combination with an AKT Inhibitor for the Treatment of Cancer |
| WO2023209088A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | Bicyclic heteroaromatic compounds and their use in the treatment of cancer |
| WO2023209086A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | Bicyclic heteroaromatic compounds for treating cancer |
| WO2023209084A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | Condensed bicyclic heteroaromatic compounds and their use in the treatment of cancer |
| WO2023209090A1 (en) | 2022-04-28 | 2023-11-02 | Astrazeneca Ab | Bicyclic heteroaromatic compounds and their application in the treatment of cancer |
| MA71241A (fr) | 2022-06-27 | 2025-04-30 | Astrazeneca Ab | Combinaisons impliquant des inhibiteurs de tyrosine kinase du récepteur du facteur de croissance épidermique pour traiter le cancer |
| WO2024008929A1 (en) | 2022-07-08 | 2024-01-11 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors in combination with hgf-receptor inhibitors for the treatment of cancer |
| AU2023371904A1 (en) * | 2022-11-03 | 2025-04-17 | Voronoi Inc. | Fumarate, tartrate, malate, and citrate salts of an egfr inhibitor |
| CA3228195A1 (en) | 2023-05-23 | 2025-06-30 | Janssen Biotech, Inc. | Methods for treatment of non-small cell lung cancer (nsclc) |
| CN116655600B (zh) * | 2023-05-23 | 2025-08-22 | 江南大学 | 一种取代的2-芳氨基嘧啶类化合物、药物组合物及其用途 |
| WO2025017409A1 (en) | 2023-07-14 | 2025-01-23 | Janssen Biotech, Inc. | Dosing regimen for therapies comprising bispecific antiegfr/c-met antibodies |
| WO2025052273A1 (en) | 2023-09-05 | 2025-03-13 | Janssen Biotech, Inc. | Methods of treating non-small cell lung cancer |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2280515A1 (en) | 1997-03-11 | 1998-09-17 | E.I. Du Pont De Nemours And Company | Heteroaryl azole herbicides |
| US20030004174A9 (en) | 2000-02-17 | 2003-01-02 | Armistead David M. | Kinase inhibitors |
| GB0016877D0 (en) | 2000-07-11 | 2000-08-30 | Astrazeneca Ab | Chemical compounds |
| ATE354573T1 (de) | 2000-12-21 | 2007-03-15 | Vertex Pharma | ßPYRAZOLVERBINDUNGEN, DIE SICH ALS PROTEINKINASEINHIBITOREN EIGNENß |
| WO2003030909A1 (en) | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
| EA007298B1 (ru) | 2001-11-01 | 2006-08-25 | Янссен Фармацевтика Н.В. | Гетероариламины в качестве ингибиторов гликогенсинтаза-киназы 3-бета (ингибиторов gsk3) |
| EP1565446A1 (en) | 2002-11-28 | 2005-08-24 | Schering Aktiengesellschaft | Chk-, pdk- and akt-inhibitory pyrimidines, their production and use as pharmaceutical agents |
| TW200528101A (en) | 2004-02-03 | 2005-09-01 | Astrazeneca Ab | Chemical compounds |
| JP4428565B2 (ja) | 2004-10-05 | 2010-03-10 | 東京エレクトロン株式会社 | 処理液塗布装置 |
| AU2005295788A1 (en) | 2004-10-13 | 2006-04-27 | Wyeth | N-benzenesulfonyl substituted anilino-pyrimidine analogs |
| EP1841760B1 (en) | 2004-12-30 | 2011-08-10 | Exelixis, Inc. | Pyrimidine derivatives as kinase modulators and method of use |
| US20070072894A1 (en) | 2005-03-24 | 2007-03-29 | Kempf J V | Synthesis of pyrroloquinoline quinone (PQQ) |
| JP5007029B2 (ja) | 2005-07-13 | 2012-08-22 | Ntn株式会社 | グリース組成物および該グリース封入転がり軸受 |
| EP1919470A1 (en) | 2005-08-25 | 2008-05-14 | F.Hoffmann-La Roche Ag | FUSED PYRAZOLE AS p38 MAP KINASE INHIBITORS |
| JP2007117465A (ja) | 2005-10-28 | 2007-05-17 | Sharp Corp | 集塵器およびそれを備えた電気掃除機 |
| WO2007111471A1 (en) | 2006-03-29 | 2007-10-04 | Ktfreetel Co., Ltd. | Digital device and method for providing additional service by using the same |
| MX2008012482A (es) | 2006-03-31 | 2008-10-10 | Abbott Lab | Compuestos de indazol. |
| CN101460491A (zh) | 2006-04-12 | 2009-06-17 | 惠氏公司 | 苯胺基嘧啶苯基和苯并噻吩类似物 |
| EP2125781A2 (en) | 2006-12-20 | 2009-12-02 | Amgen Inc. | Substituted heterocycles and methods of use |
| TWI458721B (zh) | 2008-06-27 | 2014-11-01 | Celgene Avilomics Res Inc | 雜芳基化合物及其用途 |
| KR101705158B1 (ko) * | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Egfr 억제제 및 질환 치료방법 |
| NZ599041A (en) * | 2009-11-13 | 2014-05-30 | Genosco | Kinase inhibitors |
| PL2678332T3 (pl) * | 2011-02-25 | 2016-12-30 | Pochodne diaminopirymidyny i sposoby ich wytwarzania | |
| ES2654177T3 (es) | 2011-07-27 | 2018-02-12 | Astrazeneca Ab | Derivados de 2-(2,4,5-anilino sustituido)pirimidina como moduladores de EGFR útiles para tratar el cáncer |
| CN104203943B (zh) | 2012-01-20 | 2017-12-29 | 盖诺斯克公司 | 取代的嘧啶化合物及其作为syk抑制剂的用途 |
| CN104583195B (zh) * | 2012-09-12 | 2018-08-17 | 山东亨利医药科技有限责任公司 | 作为酪氨酸激酶抑制剂的含氮杂芳环衍生物 |
| US8957080B2 (en) * | 2013-04-09 | 2015-02-17 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| US10273224B2 (en) * | 2013-08-22 | 2019-04-30 | Jubilant Biosys Limited | Substituted pyrimidine compounds, compositions and medicinal applications thereof |
| WO2015094803A1 (en) | 2013-12-16 | 2015-06-25 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| CN104860941B (zh) | 2014-02-25 | 2017-03-22 | 上海海雁医药科技有限公司 | 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物 |
| CN111892579B (zh) | 2014-06-12 | 2023-07-25 | 上海艾力斯医药科技股份有限公司 | 一类激酶抑制剂 |
| BR112016029662B1 (pt) | 2014-06-19 | 2023-10-24 | Takeda Pharmaceutical Company Limited | COMPOSTO DE FÓRMULA Bf OU UMA FORMA FARMACEUTICAMENTE ACEITÁVEL DO MESMO, COMPOSIÇÃO FARMACÊUTICA COMPREENDENDO O MESMO E SEU USO |
| HRP20250213T1 (hr) * | 2014-10-13 | 2025-04-25 | Yuhan Corporation | Spojevi i pripravci za modulaciju aktivnosti egfr mutantne kinaze |
| CN104788427B (zh) * | 2015-02-05 | 2017-05-31 | 上海泓博智源医药股份有限公司 | 3‑(2‑嘧啶氨基)苯基丙烯酰胺类化合物及其应用 |
-
2015
- 2015-10-13 HR HRP20250213TT patent/HRP20250213T1/hr unknown
- 2015-10-13 SI SI201531055T patent/SI3207035T1/sl unknown
- 2015-10-13 SM SM20210266T patent/SMT202100266T1/it unknown
- 2015-10-13 WO PCT/KR2015/010784 patent/WO2016060443A2/en not_active Ceased
- 2015-10-13 RS RS20210608A patent/RS61865B1/sr unknown
- 2015-10-13 SG SG11201701960XA patent/SG11201701960XA/en unknown
- 2015-10-13 SI SI201531611T patent/SI3604294T1/sl unknown
- 2015-10-13 NZ NZ730012A patent/NZ730012A/en unknown
- 2015-10-13 TW TW108118264A patent/TWI730331B/zh active
- 2015-10-13 AU AU2015331166A patent/AU2015331166B2/en active Active
- 2015-10-13 CN CN202010422259.0A patent/CN111686110B/zh active Active
- 2015-10-13 TW TW104133539A patent/TWI664173B/zh active
- 2015-10-13 MX MX2017003181A patent/MX2017003181A/es active IP Right Grant
- 2015-10-13 SM SM20200059T patent/SMT202000059T1/it unknown
- 2015-10-13 HU HUE19196713A patent/HUE054848T2/hu unknown
- 2015-10-13 LT LTEP15850314.4T patent/LT3207035T/lt unknown
- 2015-10-13 PL PL19196713T patent/PL3604294T3/pl unknown
- 2015-10-13 ES ES19196713T patent/ES2879474T3/es active Active
- 2015-10-13 DK DK15850314.4T patent/DK3207035T3/da active
- 2015-10-13 PL PL15850314T patent/PL3207035T3/pl unknown
- 2015-10-13 BR BR112017007769-8A patent/BR112017007769B1/pt active IP Right Grant
- 2015-10-13 KR KR1020247013986A patent/KR20240074820A/ko active Pending
- 2015-10-13 DK DK21171619.6T patent/DK3929190T3/da active
- 2015-10-13 ES ES21171619T patent/ES3009926T3/es active Active
- 2015-10-13 DK DK19196713.2T patent/DK3604294T3/da active
- 2015-10-13 EP EP15850314.4A patent/EP3207035B1/en active Active
- 2015-10-13 JP JP2017519685A patent/JP6524221B2/ja active Active
- 2015-10-13 KR KR1020237000623A patent/KR102662358B1/ko active Active
- 2015-10-13 PT PT158503144T patent/PT3207035T/pt unknown
- 2015-10-13 KR KR1020177012969A patent/KR102073854B1/ko active Active
- 2015-10-13 EP EP19196713.2A patent/EP3604294B1/en active Active
- 2015-10-13 EP EP24166947.2A patent/EP4421069B1/en active Active
- 2015-10-13 EP EP21171619.6A patent/EP3929190B1/en active Active
- 2015-10-13 PT PT191967132T patent/PT3604294T/pt unknown
- 2015-10-13 US US14/881,930 patent/US9593098B2/en not_active Ceased
- 2015-10-13 ES ES15850314T patent/ES2770058T3/es active Active
- 2015-10-13 CA CA2962914A patent/CA2962914C/en active Active
- 2015-10-13 HR HRP20200201TT patent/HRP20200201T1/hr unknown
- 2015-10-13 CN CN201580055717.9A patent/CN106795144B/zh active Active
- 2015-10-13 HU HUE21171619A patent/HUE070874T2/hu unknown
- 2015-10-13 LT LTEP19196713.2T patent/LT3604294T/lt unknown
- 2015-10-13 RS RS20200101A patent/RS59900B1/sr unknown
- 2015-10-13 HU HUE15850314A patent/HUE048006T2/hu unknown
- 2015-10-13 PT PT211716196T patent/PT3929190T/pt unknown
- 2015-10-13 SI SI201532056T patent/SI3929190T1/sl unknown
- 2015-10-13 KR KR1020207002949A patent/KR102208775B1/ko active Active
- 2015-10-13 PL PL21171619.6T patent/PL3929190T3/pl unknown
- 2015-10-13 SM SM20250069T patent/SMT202500069T1/it unknown
- 2015-10-13 KR KR1020217002019A patent/KR102487451B1/ko active Active
- 2015-10-13 LT LTEP21171619.6T patent/LT3929190T/lt unknown
- 2015-10-13 RS RS20250168A patent/RS66529B1/sr unknown
- 2015-10-13 FI FIEP21171619.6T patent/FI3929190T3/fi active
- 2015-10-13 MX MX2020002168A patent/MX385942B/es unknown
- 2015-10-13 RU RU2017116598A patent/RU2727700C2/ru active
-
2017
- 2017-03-10 MX MX2021010761A patent/MX2021010761A/es unknown
- 2017-03-14 PH PH12017500488A patent/PH12017500488A1/en unknown
-
2019
- 2019-04-26 JP JP2019085608A patent/JP6754864B2/ja active Active
-
2020
- 2020-02-17 CY CY20201100143T patent/CY1122737T1/el unknown
- 2020-08-24 JP JP2020141205A patent/JP2020196740A/ja not_active Withdrawn
-
2021
- 2021-06-14 HR HRP20210949TT patent/HRP20210949T1/hr unknown
- 2021-07-26 CY CY20211100670T patent/CY1124359T1/el unknown
-
2022
- 2022-11-18 US US18/057,062 patent/USRE50528E1/en active Active
-
2025
- 2025-05-28 NL NL301329C patent/NL301329I2/nl unknown
- 2025-06-02 HU HUS2500023C patent/HUS2500023I1/hu unknown
- 2025-06-03 LT LTPA2025522C patent/LTPA2025522I1/lt unknown
- 2025-06-03 FR FR25C1021C patent/FR25C1021I1/fr active Active
- 2025-06-05 NO NO2025025C patent/NO2025025I1/no unknown
- 2025-06-06 FI FIC20250023C patent/FIC20250023I1/fi unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| FI3929190T3 (fi) | Yhdisteitä ja koostumuksia EGFR-mutanttikinaasin aktiivisuuksien moduloimiseksi | |
| PH12012501773A1 (en) | Arylethynyl derivatives | |
| CY1120188T1 (el) | ΠΑΡΑΓΩΓΑ ΝΑΦΘΥΡΙΔΙΝΗΣ ΧΡΗΣΙΜΑ ΩΣ ΑΝΤΑΓΩΝΙΣΤΕΣ ΙΝΤΕΓΚΡΙΝΗΣ αvβ6 | |
| MX2017010230A (es) | Derivados de mono- y poliazanaftaleno sustituidos y su uso. | |
| PH12013501197B1 (en) | Indeno-fused ring compounds | |
| AR087418A1 (es) | Inhibidores de replica de virus de influenza | |
| CO2018009876A2 (es) | Nuevos compuestos y sus composiciones farmacéuticas para el tratamiento de fibrosis | |
| MX374409B (es) | Derivados de etinilo como moduladores del receptor de glutamato metabotrópico. | |
| SA515360504B1 (ar) | عملية لامتصاص ثاني اكسيد الكربون من خليط غاز باستخدام محلول مائي من داي أمين | |
| PH12013501196B1 (en) | Indeno- fused ring compounds having photochromic properties | |
| MX352470B (es) | Disales de acido malonico y metodo para preparar dihaluros de malonilo. | |
| AR052580A1 (es) | Antagonistas del receptor de pgd2 para el tratamiento de enfermedades inflamatorias | |
| MX2016017276A (es) | Formulaciones, produccion y uso de las mismas y componentes adecuados. | |
| EA201301315A1 (ru) | Способ получения промежуточных соединений эстетрола | |
| MY170822A (en) | Ethynyl derivatives as mglur5 allosteric modulators | |
| MX337443B (es) | Derivados de etinilo como moduladores alostericos positivos del receptor de glutamato metabotropico del subtipo 5 (mglur5). | |
| GB2544905A (en) | Synthesis and use of amino lipids | |
| CL2020001049A1 (es) | Proceso para producir compuestos de piridazinona herbicida. | |
| CY1125355T1 (el) | Πεντακυκλικη ενωση | |
| EA201891769A1 (ru) | СПОСОБ ПОЛУЧЕНИЯ СОЕДИНЕНИЯ ПИРРОЛО[3,2-d]ПИРИМИДИНА И ПРОМЕЖУТОЧНЫХ СОЕДИНЕНИЙ | |
| MX369974B (es) | Compuestos farmaceuticos. | |
| DK3486324T3 (da) | Fremgangsmåde til fremstilling af aminer fra carbonylforbindelser ved transaminasereaktion under saltudfældning | |
| CY1117087T1 (el) | Διαδικασια για την παρασκευη εστερων (5-φθορο-2-μεθυλο-3-κινολιν-2-υλμεθυλ-ινδoλ-1-υλ)- οξικου οξεος | |
| PH12016500152A1 (en) | Novel triazine derivative | |
| AR072051A1 (es) | Compuestos que comprenden un grupo ciclobutoxi |