CN112513027A - 吲唑胺类衍生物及其制备方法和其在医药上的用途 - Google Patents
吲唑胺类衍生物及其制备方法和其在医药上的用途 Download PDFInfo
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- CN112513027A CN112513027A CN201980050268.7A CN201980050268A CN112513027A CN 112513027 A CN112513027 A CN 112513027A CN 201980050268 A CN201980050268 A CN 201980050268A CN 112513027 A CN112513027 A CN 112513027A
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- 125000003678 cyclohexadienyl group Chemical group C1(=CC=CCC1)* 0.000 description 1
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 description 1
- 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 description 1
- 125000002433 cyclopentenyl group Chemical group C1(=CCCC1)* 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
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- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 description 1
- 230000007783 downstream signaling Effects 0.000 description 1
- 238000009509 drug development Methods 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- OGPBJKLSAFTDLK-UHFFFAOYSA-N europium atom Chemical compound [Eu] OGPBJKLSAFTDLK-UHFFFAOYSA-N 0.000 description 1
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- 125000002541 furyl group Chemical group 0.000 description 1
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- 125000000592 heterocycloalkyl group Chemical group 0.000 description 1
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- 125000004491 isohexyl group Chemical group C(CCC(C)C)* 0.000 description 1
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- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
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- 238000003674 kinase activity assay Methods 0.000 description 1
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- LMEIFDLPUOSPCQ-UHFFFAOYSA-N methyl 5-amino-1h-indazole-6-carboxylate Chemical compound C1=C(N)C(C(=O)OC)=CC2=C1C=NN2 LMEIFDLPUOSPCQ-UHFFFAOYSA-N 0.000 description 1
- DEZHKDZFGIGNPH-UHFFFAOYSA-N methyl 5-nitro-1h-indazole-6-carboxylate Chemical compound C1=C([N+]([O-])=O)C(C(=O)OC)=CC2=C1C=NN2 DEZHKDZFGIGNPH-UHFFFAOYSA-N 0.000 description 1
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- 239000006186 oral dosage form Substances 0.000 description 1
- 239000012074 organic phase Substances 0.000 description 1
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- 125000006340 pentafluoro ethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 description 1
- 125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 description 1
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- 230000000171 quenching effect Effects 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
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- 230000004044 response Effects 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 239000012679 serum free medium Substances 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
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- 238000010998 test method Methods 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 125000003554 tetrahydropyrrolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
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- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 230000001960 triggered effect Effects 0.000 description 1
- 238000001291 vacuum drying Methods 0.000 description 1
- 239000011534 wash buffer Substances 0.000 description 1
- DGVVWUTYPXICAM-UHFFFAOYSA-N β‐Mercaptoethanol Chemical compound OCCS DGVVWUTYPXICAM-UHFFFAOYSA-N 0.000 description 1
Classifications
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- 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
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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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
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- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
本发明涉及具有通式(I)所示的吲唑类衍生物或其药学上可接受的盐、及其制备方法,以及它们作为治疗剂,特别是作为IRAK4激酶抑制剂的用途。其中通式(I)中的R1,R2,R3,W的定义与说明书中的定义相同
Description
PCT国内申请,说明书已公开。
Claims (8)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (3)
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CN201810937427 | 2018-08-17 | ||
CN2018109374272 | 2018-08-17 | ||
PCT/CN2019/100760 WO2020035019A1 (zh) | 2018-08-17 | 2019-08-15 | 吲唑胺类衍生物及其制备方法和其在医药上的用途 |
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CN112513027A true CN112513027A (zh) | 2021-03-16 |
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CN113278017B (zh) * | 2021-05-27 | 2023-03-28 | 上海应用技术大学 | 取代吲唑类化合物、制备方法、应用和包含其的组合物 |
CN113402499B (zh) * | 2021-06-21 | 2022-05-13 | 上海勋和医药科技有限公司 | 一种亚磺酰亚胺取代的吲唑类irak4激酶抑制剂、制备方法及用途 |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN106458982A (zh) * | 2014-01-10 | 2017-02-22 | 奥列基因发现技术有限公司 | 作为irak4抑制剂的吲唑化合物 |
WO2017108744A1 (de) * | 2015-12-22 | 2017-06-29 | Bayer Pharma Aktiengesellschaft | Neue substituierte indazole, verfahren zu ihrer herstellung, pharmazeutische präparate die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln |
WO2017148902A1 (de) * | 2016-03-03 | 2017-09-08 | Bayer Pharma Aktiengesellschaft | Neue 2-substituierte indazole, verfahren zu ihrer herstellung, pharmazeutische präparate die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln |
CN107406416A (zh) * | 2014-11-26 | 2017-11-28 | 拜耳医药股份有限公司 | 新型取代的吲唑、其制备方法、包含其的药物制剂及其用于制备药物的用途 |
Family Cites Families (3)
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---|---|---|---|---|
MX2008012598A (es) | 2006-03-31 | 2008-10-10 | Novartis Ag | Tiadiazolidinonas inhibidoras de ptpasa. |
CN106456609A (zh) | 2014-06-20 | 2017-02-22 | 奥瑞基尼探索技术有限公司 | 作为irak4抑制剂的取代的吲唑化合物 |
CU20180006A7 (es) | 2015-07-15 | 2018-06-05 | Aurigene Discovery Tech Ltd | Compuestos de indazaol y azaindazol como inhibidores de irak-4 |
-
2019
- 2019-08-15 WO PCT/CN2019/100760 patent/WO2020035019A1/zh active Application Filing
- 2019-08-15 CN CN201980050268.7A patent/CN112513027B/zh active Active
- 2019-08-15 US US17/267,771 patent/US11897863B2/en active Active
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN106458982A (zh) * | 2014-01-10 | 2017-02-22 | 奥列基因发现技术有限公司 | 作为irak4抑制剂的吲唑化合物 |
CN107406416A (zh) * | 2014-11-26 | 2017-11-28 | 拜耳医药股份有限公司 | 新型取代的吲唑、其制备方法、包含其的药物制剂及其用于制备药物的用途 |
WO2017108744A1 (de) * | 2015-12-22 | 2017-06-29 | Bayer Pharma Aktiengesellschaft | Neue substituierte indazole, verfahren zu ihrer herstellung, pharmazeutische präparate die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln |
WO2017148902A1 (de) * | 2016-03-03 | 2017-09-08 | Bayer Pharma Aktiengesellschaft | Neue 2-substituierte indazole, verfahren zu ihrer herstellung, pharmazeutische präparate die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln |
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US11897863B2 (en) | 2024-02-13 |
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WO2020035019A1 (zh) | 2020-02-20 |
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