CN115279762A - 作为乙肝表面抗原抑制剂的氮杂双环化合物 - Google Patents
作为乙肝表面抗原抑制剂的氮杂双环化合物 Download PDFInfo
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- CN115279762A CN115279762A CN202180020994.1A CN202180020994A CN115279762A CN 115279762 A CN115279762 A CN 115279762A CN 202180020994 A CN202180020994 A CN 202180020994A CN 115279762 A CN115279762 A CN 115279762A
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- Prior art keywords
- alkyl
- cycloalkyl
- compound
- pharmaceutically acceptable
- radical
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- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 48
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- 238000006467 substitution reaction Methods 0.000 claims description 38
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- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 4
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- 125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000000623 heterocyclic group Chemical group 0.000 description 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
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- 125000003548 sec-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
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- 230000008685 targeting Effects 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- 125000005958 tetrahydrothienyl group Chemical group 0.000 description 1
- 125000004632 tetrahydrothiopyranyl group Chemical group S1C(CCCC1)* 0.000 description 1
- 125000001984 thiazolidinyl group Chemical group 0.000 description 1
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- 238000012546 transfer Methods 0.000 description 1
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- 238000005533 tritiation Methods 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
- A61K31/495—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
- 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
- A61K31/529—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/18—Bridged systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Oncology (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
提供作为乙肝表面抗原抑制剂的氮杂双环化合物，具体涉及式I'化合物、其立体异构体、其药学上可接受的盐，其制备方法，含有该化合物的药物组合物，及其作为治疗乙型肝炎病毒感染的药物的用途。
Description
PCT国内申请，说明书已公开。
Claims (23)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2020102738805 | 2020-04-09 | ||
| CN202010273880 | 2020-04-09 | ||
| CN202011455840 | 2020-12-10 | ||
| CN2020114557904 | 2020-12-10 | ||
| CN2020114558409 | 2020-12-10 | ||
| CN202011455790 | 2020-12-10 | ||
| PCT/CN2021/086205 WO2021204258A1 (zh) | 2020-04-09 | 2021-04-09 | 作为乙肝表面抗原抑制剂的氮杂双环化合物 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN115279762A true CN115279762A (zh) | 2022-11-01 |
Family
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202180020994.1A Pending CN115279762A (zh) | 2020-04-09 | 2021-04-09 | 作为乙肝表面抗原抑制剂的氮杂双环化合物 |
Country Status (2)
| Country | Link |
|---|---|
| CN (1) | CN115279762A (zh) |
| WO (1) | WO2021204258A1 (zh) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107108610A (zh) * | 2014-12-30 | 2017-08-29 | 豪夫迈·罗氏有限公司 | 用于治疗和预防肝炎b病毒感染的新的四氢吡啶并嘧啶和四氢吡啶并吡啶化合物 |
| CN107624113A (zh) * | 2015-05-04 | 2018-01-23 | 豪夫迈·罗氏有限公司 | 作为HBsAg(HBV表面抗原)和HBV DNA生成的抑制剂用于治疗乙型肝炎病毒感染的四氢吡啶并嘧啶和四氢吡啶并吡啶类化合物 |
| CN110088103A (zh) * | 2016-11-03 | 2019-08-02 | 豪夫迈·罗氏有限公司 | 用于治疗和预防乙型肝炎病毒感染的新的四氢吡啶并嘧啶化合物 |
-
2021
- 2021-04-09 WO PCT/CN2021/086205 patent/WO2021204258A1/zh active Application Filing
- 2021-04-09 CN CN202180020994.1A patent/CN115279762A/zh active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107108610A (zh) * | 2014-12-30 | 2017-08-29 | 豪夫迈·罗氏有限公司 | 用于治疗和预防肝炎b病毒感染的新的四氢吡啶并嘧啶和四氢吡啶并吡啶化合物 |
| CN107624113A (zh) * | 2015-05-04 | 2018-01-23 | 豪夫迈·罗氏有限公司 | 作为HBsAg(HBV表面抗原)和HBV DNA生成的抑制剂用于治疗乙型肝炎病毒感染的四氢吡啶并嘧啶和四氢吡啶并吡啶类化合物 |
| CN110088103A (zh) * | 2016-11-03 | 2019-08-02 | 豪夫迈·罗氏有限公司 | 用于治疗和预防乙型肝炎病毒感染的新的四氢吡啶并嘧啶化合物 |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2021204258A1 (zh) | 2021-10-14 |
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