CN116249529A - 喹唑啉衍生物及其在医药上的应用 - Google Patents
喹唑啉衍生物及其在医药上的应用 Download PDFInfo
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- CN116249529A CN116249529A CN202180063168.5A CN202180063168A CN116249529A CN 116249529 A CN116249529 A CN 116249529A CN 202180063168 A CN202180063168 A CN 202180063168A CN 116249529 A CN116249529 A CN 116249529A
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- Prior art keywords
- compound
- quinazolin
- ethyl
- pharmaceutically acceptable
- meso
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- 125000002294 quinazolinyl group Chemical class N1=C(N=CC2=CC=CC=C12)* 0.000 title abstract 2
- 201000010099 disease Diseases 0.000 claims abstract description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 7
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- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 6
- 238000011282 treatment Methods 0.000 claims abstract description 5
- 238000004519 manufacturing process Methods 0.000 claims abstract description 4
- 238000011321 prophylaxis Methods 0.000 claims abstract 2
- 150000001875 compounds Chemical class 0.000 claims description 116
- 239000000203 mixture Substances 0.000 claims description 46
- 239000013078 crystal Substances 0.000 claims description 32
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- 125000000217 alkyl group Chemical group 0.000 claims description 30
- 229940002612 prodrug Drugs 0.000 claims description 30
- 239000000651 prodrug Substances 0.000 claims description 30
- 150000003839 salts Chemical class 0.000 claims description 30
- 239000012453 solvate Substances 0.000 claims description 26
- 239000002207 metabolite Substances 0.000 claims description 25
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 22
- 125000004432 carbon atom Chemical group C* 0.000 claims description 19
- 229910052799 carbon Inorganic materials 0.000 claims description 18
- 210000004027 cell Anatomy 0.000 claims description 15
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 15
- 125000001424 substituent group Chemical group 0.000 claims description 13
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- 125000003545 alkoxy group Chemical group 0.000 claims description 9
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- GQHTUMJGOHRCHB-UHFFFAOYSA-N 2,3,4,6,7,8,9,10-octahydropyrimido[1,2-a]azepine Chemical compound C1CCCCN2CCCN=C21 GQHTUMJGOHRCHB-UHFFFAOYSA-N 0.000 description 10
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- VHYFNPMBLIVWCW-UHFFFAOYSA-N 4-Dimethylaminopyridine Chemical compound CN(C)C1=CC=NC=C1 VHYFNPMBLIVWCW-UHFFFAOYSA-N 0.000 description 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 8
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- VIGYFTAOWACDSE-UHFFFAOYSA-N quinazolin-4-yl 2,4,6-tri(propan-2-yl)benzenesulfonate Chemical compound C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)OC1=NC=NC2=CC=CC=C12 VIGYFTAOWACDSE-UHFFFAOYSA-N 0.000 description 8
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- 235000011152 sodium sulphate Nutrition 0.000 description 7
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 6
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- 230000002018 overexpression Effects 0.000 description 1
- SFJGCXYXEFWEBK-UHFFFAOYSA-N oxazepine Chemical compound O1C=CC=CC=N1 SFJGCXYXEFWEBK-UHFFFAOYSA-N 0.000 description 1
- 125000003585 oxepinyl group Chemical group 0.000 description 1
- NXJCBFBQEVOTOW-UHFFFAOYSA-L palladium(2+);dihydroxide Chemical compound O[Pd]O NXJCBFBQEVOTOW-UHFFFAOYSA-L 0.000 description 1
- 125000002262 penten-4-yl group Chemical group C=CCC(C)* 0.000 description 1
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- MQDVUDAZJMZQMF-UHFFFAOYSA-N pyridin-2-ylurea Chemical compound NC(=O)NC1=CC=CC=N1 MQDVUDAZJMZQMF-UHFFFAOYSA-N 0.000 description 1
- ZDYVRSLAEXCVBX-UHFFFAOYSA-N pyridinium p-toluenesulfonate Chemical compound C1=CC=[NH+]C=C1.CC1=CC=C(S([O-])(=O)=O)C=C1 ZDYVRSLAEXCVBX-UHFFFAOYSA-N 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
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Classifications
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4741—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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| CN2020116002676 | 2020-12-30 | ||
| CN202011600267 | 2020-12-30 | ||
| CN202110150212 | 2021-02-04 | ||
| CN2021101502128 | 2021-02-04 | ||
| CN202110144993X | 2021-02-05 | ||
| CN202110144993 | 2021-02-05 | ||
| CN202110398907 | 2021-04-14 | ||
| CN2021103989078 | 2021-04-14 | ||
| CN2021112386652 | 2021-10-29 | ||
| CN202111238665 | 2021-10-29 | ||
| PCT/CN2021/141677 WO2022143533A1 (fr) | 2020-12-30 | 2021-12-27 | Dérivé de quinazoline et son utilisation en médecine |
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| CN116249529A true CN116249529A (zh) | 2023-06-09 |
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| WO (1) | WO2022143533A1 (fr) |
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| WO2022258057A1 (fr) * | 2021-06-11 | 2022-12-15 | Jingrui Biopharma Co., Ltd. | Composés en tant qu'agents anticancéreux |
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| GB9520822D0 (en) * | 1995-10-11 | 1995-12-13 | Wellcome Found | Therapeutically active compounds |
| US7078409B2 (en) * | 2002-03-28 | 2006-07-18 | Beta Pharma, Inc. | Fused quinazoline derivatives useful as tyrosine kinase inhibitors |
| US10898487B2 (en) * | 2016-12-22 | 2021-01-26 | Boehringer Ingelheim International Gmbh | Benzylamino substituted quinazolines and derivatives as SOS1 inhibitors |
| CN115244058A (zh) * | 2020-04-08 | 2022-10-25 | 江苏恒瑞医药股份有限公司 | 嘧啶并二环类衍生物、其制备方法及其在医药上的应用 |
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- 2021-12-27 CN CN202180063168.5A patent/CN116249529A/zh active Pending
- 2021-12-27 WO PCT/CN2021/141677 patent/WO2022143533A1/fr active Application Filing
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| Publication number | Publication date |
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| WO2022143533A1 (fr) | 2022-07-07 |
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