CN116096720A - 二氢吡咯并[2,3-d]哒嗪-7-酮衍生物，其制备方法和应用 - Google Patents
二氢吡咯并[2,3-d]哒嗪-7-酮衍生物，其制备方法和应用 Download PDFInfo
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- CN116096720A CN116096720A CN202180047630.2A CN202180047630A CN116096720A CN 116096720 A CN116096720 A CN 116096720A CN 202180047630 A CN202180047630 A CN 202180047630A CN 116096720 A CN116096720 A CN 116096720A
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- 125000001624 naphthyl group Chemical group 0.000 description 1
- 239000012299 nitrogen atmosphere Substances 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
- 239000003208 petroleum Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000012071 phase Substances 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- CHUPNGGCNPHUEN-UHFFFAOYSA-M potassium;ethanesulfonate Chemical compound [K+].CCS([O-])(=O)=O CHUPNGGCNPHUEN-UHFFFAOYSA-M 0.000 description 1
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- 229940002612 prodrug Drugs 0.000 description 1
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- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 125000000168 pyrrolyl group Chemical group 0.000 description 1
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- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 239000000779 smoke Substances 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- QDRKDTQENPPHOJ-UHFFFAOYSA-N sodium ethoxide Chemical compound [Na+].CC[O-] QDRKDTQENPPHOJ-UHFFFAOYSA-N 0.000 description 1
- 238000009987 spinning Methods 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 238000000967 suction filtration Methods 0.000 description 1
- 125000004434 sulfur atom Chemical group 0.000 description 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical group C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 description 1
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- IAQRGUVFOMOMEM-ONEGZZNKSA-N trans-but-2-ene Chemical compound C\C=C\C IAQRGUVFOMOMEM-ONEGZZNKSA-N 0.000 description 1
- 125000004784 trichloromethoxy group Chemical group ClC(O*)(Cl)Cl 0.000 description 1
- 125000003866 trichloromethyl group Chemical group ClC(Cl)(Cl)* 0.000 description 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
- JGOIIPRSFZFFHG-UHFFFAOYSA-N trimethyl(2-tributylstannylethynyl)silane Chemical compound CCCC[Sn](CCCC)(CCCC)C#C[Si](C)(C)C JGOIIPRSFZFFHG-UHFFFAOYSA-N 0.000 description 1
- CWMFRHBXRUITQE-UHFFFAOYSA-N trimethylsilylacetylene Chemical group C[Si](C)(C)C#C CWMFRHBXRUITQE-UHFFFAOYSA-N 0.000 description 1
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- 238000010792 warming Methods 0.000 description 1
- 239000003643 water by type Substances 0.000 description 1
- 230000029663 wound healing Effects 0.000 description 1
- 239000008096 xylene Substances 0.000 description 1
Classifications
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (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)
Abstract
一种具有式(I)结构的二氢吡咯并[2,3‑d]哒嗪‑7‑酮衍生物、其制备方法、含有其的药物组合物，以及其作为FGFR及其突变抑制剂的用途和其在制备治疗和/或预防至少部分由FGFR激酶介导的肿瘤或癌症以及FGFR抑制剂具有耐受性的肿瘤患者的药物中的用途，特别是在制备治疗和/或预防FGFR信号通路的V561、V565、N550、N540、V555、E566、K660和/或V550具有突变的肿瘤患者的药物中的用途。其中式(I)的各取代基与说明书中的定义相同。
Description
PCT国内申请，说明书已公开。
Claims (14)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202010878356 | 2020-08-27 | ||
| CN2020108783560 | 2020-08-27 | ||
| PCT/CN2021/114580 WO2022042612A1 (zh) | 2020-08-27 | 2021-08-25 | 二氢吡咯并[2,3-d]哒嗪-7-酮衍生物，其制备方法和应用 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN116096720A true CN116096720A (zh) | 2023-05-09 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN202180047630.2A Pending CN116096720A (zh) | 2020-08-27 | 2021-08-25 | 二氢吡咯并[2,3-d]哒嗪-7-酮衍生物，其制备方法和应用 |
Country Status (2)
| Country | Link |
|---|---|
| CN (1) | CN116096720A (zh) |
| WO (1) | WO2022042612A1 (zh) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN117003710A (zh) * | 2023-07-19 | 2023-11-07 | 镇江先锋植保科技有限公司 | 一种2-巯基-6-氯苯并恶唑的制备方法 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6427599B2 (ja) * | 2014-05-19 | 2018-11-21 | チャンスー ヘンルイ メディシン カンパニー，リミテッド | チロシンキナーゼ阻害剤としての置換エチニルヘテロ二環式化合物 |
| CA2953798C (en) * | 2014-07-07 | 2019-06-11 | Eternity Bioscience Inc. | Aminopyridazinone compounds as protein kinase inhibitors |
| CA3028824C (en) * | 2016-06-22 | 2023-12-12 | Shanghai Fochon Pharmaceutical Co., Ltd. | Substituted pyrrolo[2,3-d]pyridazin-4-ones and pyrazolo[3,4-d]pyridazin-4-ones as protein kinase inhibitors |
-
2021
- 2021-08-25 WO PCT/CN2021/114580 patent/WO2022042612A1/zh active Application Filing
- 2021-08-25 CN CN202180047630.2A patent/CN116096720A/zh active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| WO2022042612A1 (zh) | 2022-03-03 |
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