CN107250145A - 被取代的核苷、核苷酸及其类似物 - Google Patents
被取代的核苷、核苷酸及其类似物 Download PDFInfo
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- CN107250145A CN107250145A CN201580076647.5A CN201580076647A CN107250145A CN 107250145 A CN107250145 A CN 107250145A CN 201580076647 A CN201580076647 A CN 201580076647A CN 107250145 A CN107250145 A CN 107250145A
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- 208000008494 pericarditis Diseases 0.000 description 1
- 230000000737 periodic effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 description 1
- PMOIAJVKYNVHQE-UHFFFAOYSA-N phosphanium;bromide Chemical compound [PH4+].[Br-] PMOIAJVKYNVHQE-UHFFFAOYSA-N 0.000 description 1
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 description 1
- 125000004437 phosphorous atom Chemical group 0.000 description 1
- 230000026731 phosphorylation Effects 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
- LFSXCDWNBUNEEM-UHFFFAOYSA-N phthalazine Chemical class C1=NN=CC2=CC=CC=C21 LFSXCDWNBUNEEM-UHFFFAOYSA-N 0.000 description 1
- JTHRRMFZHSDGNJ-UHFFFAOYSA-N piperazine-2,3-dione Chemical compound O=C1NCCNC1=O JTHRRMFZHSDGNJ-UHFFFAOYSA-N 0.000 description 1
- 150000003053 piperidines Chemical class 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 230000008488 polyadenylation Effects 0.000 description 1
- 239000001103 potassium chloride Substances 0.000 description 1
- 235000011164 potassium chloride Nutrition 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 description 1
- 230000004224 protection Effects 0.000 description 1
- CPNGPNLZQNNVQM-UHFFFAOYSA-N pteridine Chemical compound N1=CN=CC2=NC=CN=C21 CPNGPNLZQNNVQM-UHFFFAOYSA-N 0.000 description 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 description 1
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical class O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 description 1
- QFYXSLAAXZTRLG-UHFFFAOYSA-N pyrrolidine-2,3-dione Chemical class O=C1CCNC1=O QFYXSLAAXZTRLG-UHFFFAOYSA-N 0.000 description 1
- 150000003235 pyrrolidines Chemical class 0.000 description 1
- 150000004040 pyrrolidinones Chemical class 0.000 description 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 description 1
- 230000002285 radioactive effect Effects 0.000 description 1
- 229940038850 rebif Drugs 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 238000004007 reversed phase HPLC Methods 0.000 description 1
- 239000002336 ribonucleotide Substances 0.000 description 1
- 125000002652 ribonucleotide group Chemical group 0.000 description 1
- 210000003705 ribosome Anatomy 0.000 description 1
- 238000007363 ring formation reaction Methods 0.000 description 1
- 125000006413 ring segment Chemical group 0.000 description 1
- 229910052701 rubidium Inorganic materials 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
- 230000035807 sensation Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 238000013207 serial dilution Methods 0.000 description 1
- 230000000405 serological effect Effects 0.000 description 1
- 235000015170 shellfish Nutrition 0.000 description 1
- 229910000077 silane Inorganic materials 0.000 description 1
- 239000001632 sodium acetate Substances 0.000 description 1
- 235000017281 sodium acetate Nutrition 0.000 description 1
- 235000017550 sodium carbonate Nutrition 0.000 description 1
- KIEOKOFEPABQKJ-UHFFFAOYSA-N sodium dichromate Chemical compound [Na+].[Na+].[O-][Cr](=O)(=O)O[Cr]([O-])(=O)=O KIEOKOFEPABQKJ-UHFFFAOYSA-N 0.000 description 1
- JQWHASGSAFIOCM-UHFFFAOYSA-M sodium periodate Chemical compound [Na+].[O-]I(=O)(=O)=O JQWHASGSAFIOCM-UHFFFAOYSA-M 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 210000000278 spinal cord Anatomy 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid Chemical compound OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 230000003319 supportive effect Effects 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 230000002194 synthesizing effect Effects 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229960001367 tartaric acid Drugs 0.000 description 1
- 238000003419 tautomerization reaction Methods 0.000 description 1
- MHYGQXWCZAYSLJ-UHFFFAOYSA-N tert-butyl-chloro-diphenylsilane Chemical compound C=1C=CC=CC=1[Si](Cl)(C(C)(C)C)C1=CC=CC=C1 MHYGQXWCZAYSLJ-UHFFFAOYSA-N 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- DZLFLBLQUQXARW-UHFFFAOYSA-N tetrabutylammonium Chemical compound CCCC[N+](CCCC)(CCCC)CCCC DZLFLBLQUQXARW-UHFFFAOYSA-N 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 229960004559 theobromine Drugs 0.000 description 1
- 150000004867 thiadiazoles Chemical class 0.000 description 1
- CBDKQYKMCICBOF-UHFFFAOYSA-N thiazoline Chemical compound C1CN=CS1 CBDKQYKMCICBOF-UHFFFAOYSA-N 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 description 1
- 229930192474 thiophene Natural products 0.000 description 1
- 229940104230 thymidine Drugs 0.000 description 1
- 210000001541 thymus gland Anatomy 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
- ZGYICYBLPGRURT-UHFFFAOYSA-N tri(propan-2-yl)silicon Chemical compound CC(C)[Si](C(C)C)C(C)C ZGYICYBLPGRURT-UHFFFAOYSA-N 0.000 description 1
- 125000005270 trialkylamine group Chemical group 0.000 description 1
- 150000003852 triazoles Chemical class 0.000 description 1
- FAQYAMRNWDIXMY-UHFFFAOYSA-N trichloroborane Chemical compound ClB(Cl)Cl FAQYAMRNWDIXMY-UHFFFAOYSA-N 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical compound [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 description 1
- GRGCWBWNLSTIEN-UHFFFAOYSA-N trifluoromethanesulfonyl chloride Chemical compound FC(F)(F)S(Cl)(=O)=O GRGCWBWNLSTIEN-UHFFFAOYSA-N 0.000 description 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 description 1
- 125000004385 trihaloalkyl group Chemical group 0.000 description 1
- PQDJYEQOELDLCP-UHFFFAOYSA-N trimethylsilane Chemical compound C[SiH](C)C PQDJYEQOELDLCP-UHFFFAOYSA-N 0.000 description 1
- 229940094989 trimethylsilane Drugs 0.000 description 1
- FTVLMFQEYACZNP-UHFFFAOYSA-N trimethylsilyl trifluoromethanesulfonate Chemical compound C[Si](C)(C)OS(=O)(=O)C(F)(F)F FTVLMFQEYACZNP-UHFFFAOYSA-N 0.000 description 1
- BPLKQGGAXWRFOE-UHFFFAOYSA-M trimethylsulfoxonium iodide Chemical compound [I-].C[S+](C)(C)=O BPLKQGGAXWRFOE-UHFFFAOYSA-M 0.000 description 1
- 150000004901 trioxanes Chemical class 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 229940116269 uric acid Drugs 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
-
- 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
- A61P31/14—Antivirals for RNA viruses
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- General Health & Medical Sciences (AREA)
- Virology (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Oncology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Communicable Diseases (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (3)
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|---|---|---|---|
| US201462094418P | 2014-12-19 | 2014-12-19 | |
| US62/094418 | 2014-12-19 | ||
| PCT/US2015/066193 WO2016100569A1 (en) | 2014-12-19 | 2015-12-16 | Substituted nucleosides, nucleotides and analogs thereof |
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| CN107250145A true CN107250145A (zh) | 2017-10-13 |
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| CN201580076647.5A Pending CN107250145A (zh) | 2014-12-19 | 2015-12-16 | 被取代的核苷、核苷酸及其类似物 |
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| US (2) | US9890188B2 (enExample) |
| EP (1) | EP3233879A4 (enExample) |
| JP (1) | JP2017538722A (enExample) |
| CN (1) | CN107250145A (enExample) |
| AU (1) | AU2015364630A1 (enExample) |
| CA (1) | CA2970936A1 (enExample) |
| HK (1) | HK1245800A1 (enExample) |
| MA (1) | MA41213A (enExample) |
| MX (1) | MX2017008184A (enExample) |
| TW (1) | TW201625658A (enExample) |
| WO (1) | WO2016100569A1 (enExample) |
| ZA (1) | ZA201704876B (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114288313A (zh) * | 2022-02-18 | 2022-04-08 | 常晓宇 | 嘧啶核苷类药物在制备预防或治疗冠状病毒感染性疾病药物中的用途 |
| WO2023142803A1 (zh) * | 2022-01-28 | 2023-08-03 | 北京恩泰伟医药科技有限公司 | 抗病毒化合物及其用途 |
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| MX356509B (es) | 2011-12-22 | 2018-05-30 | Alios Biopharma Inc | Nucleósidos sustituidos, nucleótidos y análogos de los mismos. |
| US9441007B2 (en) | 2012-03-21 | 2016-09-13 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| CN104321333A (zh) | 2012-03-21 | 2015-01-28 | 沃泰克斯药物股份有限公司 | 硫代氨基磷酸酯核苷酸前药的固体形式 |
| USRE48171E1 (en) | 2012-03-21 | 2020-08-25 | Janssen Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| PE20151433A1 (es) | 2012-12-21 | 2015-10-16 | Alios Biopharma Inc | Nucleosidos sustituidos, nucleotidos y analogos de los mismos |
| US9598457B2 (en) | 2012-12-21 | 2017-03-21 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| AR099632A1 (es) | 2013-04-05 | 2016-08-10 | Alios Biopharma Inc | Tratamiento de una infección viral de hepatitis c, que usa una combinación de compuestos |
| GEP201706793B (en) | 2013-06-26 | 2017-12-11 | Alios Biopharma Inc | Substituted nucleosides, nucleotides and analogs thereof |
| CA2913206C (en) * | 2013-06-26 | 2022-08-02 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| WO2015054465A1 (en) | 2013-10-11 | 2015-04-16 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| WO2015200219A1 (en) | 2014-06-24 | 2015-12-30 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| EP3160475B1 (en) | 2014-06-24 | 2024-01-03 | Janssen Pharmaceuticals, Inc. | Substituted nucleosides and nucleotides to treat filoviridae infections |
| WO2016069489A1 (en) | 2014-10-28 | 2016-05-06 | Alios Biopharma, Inc. | Methods of preparing substituted nucleoside analogs |
| MA41441A (fr) | 2014-12-19 | 2017-12-12 | Alios Biopharma Inc | Nucléosides substitués, nucléotides et analogues de ceux-ci |
| WO2016144918A1 (en) | 2015-03-06 | 2016-09-15 | Atea Pharmaceuticals, Inc. | β-D-2'-DEOXY-2'α-FLUORO-2'-β-C-SUBSTITUTED-2-MODIFIED-N6-SUBSTITUTED PURINE NUCLEOTIDES FOR HCV TREATMENT |
| EP3268368A4 (en) | 2015-03-11 | 2018-11-14 | Alios Biopharma, Inc. | Aza-pyridone compounds and uses thereof |
| TW201718618A (zh) * | 2015-09-18 | 2017-06-01 | 田邊三菱製藥股份有限公司 | 架橋型核酸ＧｕＮＡ，其製造方法，及中間體化合物 |
| US10202412B2 (en) | 2016-07-08 | 2019-02-12 | Atea Pharmaceuticals, Inc. | β-D-2′-deoxy-2′-substituted-4′-substituted-2-substituted-N6-substituted-6-aminopurinenucleotides for the treatment of paramyxovirus and orthomyxovirus infections |
| SG11201901457TA (en) | 2016-09-07 | 2019-03-28 | Atea Pharmaceuticals Inc | 2'-substituted-n6-substituted purine nucleotides for rna virus treatment |
| JP7125714B2 (ja) * | 2016-12-13 | 2022-08-25 | ヤマサ醤油株式会社 | 抗ウイルス活性を有する２’－デオキシ－７－デアザプリンヌクレオシド誘導体 |
| IL295609B2 (en) | 2017-02-01 | 2023-11-01 | Atea Pharmaceuticals Inc | Nucleotide hemisulfate salt for the treatment of hepatitis C virus |
| KR102696517B1 (ko) * | 2017-09-18 | 2024-08-21 | 얀센 바이오파마, 인크. | 치환된 뉴클레오시드, 뉴클레오티드 및 이들의 유사체 |
| CN112351799A (zh) | 2018-04-10 | 2021-02-09 | 阿堤亚制药公司 | 具有硬化的hcv感染患者的治疗 |
| MA55200A (fr) | 2019-03-06 | 2022-01-12 | Glaxosmithkline Ip No 2 Ltd | Composés utiles dans la thérapie du vih |
| TWI874791B (zh) | 2020-02-18 | 2025-03-01 | 美商基利科學股份有限公司 | 抗病毒化合物 |
| AR121356A1 (es) * | 2020-02-18 | 2022-05-11 | Gilead Sciences Inc | Compuestos antivirales |
| TWI883391B (zh) | 2020-02-18 | 2025-05-11 | 美商基利科學股份有限公司 | 抗病毒化合物 |
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| TWI845826B (zh) | 2020-03-20 | 2024-06-21 | 美商基利科學股份有限公司 | 4'-c-經取代-2-鹵基-2'-去氧腺苷核苷之前藥及其製造與使用方法 |
| US12274700B1 (en) | 2020-10-30 | 2025-04-15 | Accencio LLC | Methods of treating symptoms of coronavirus infection with RNA polymerase inhibitors |
| EP4323362B1 (en) | 2021-04-16 | 2025-05-07 | Gilead Sciences, Inc. | Methods of preparing carbanucleosides using amides |
| JP2024525164A (ja) | 2021-06-17 | 2024-07-10 | アテア ファーマシューティカルズ， インコーポレイテッド | 有利な抗ｈｃｖ併用療法 |
| CA3228162A1 (en) | 2021-08-18 | 2023-02-23 | Gilead Sciences, Inc. | Phospholipid compounds and methods of making and using the same |
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2015
- 2015-12-15 MA MA041213A patent/MA41213A/fr unknown
- 2015-12-16 HK HK18105072.0A patent/HK1245800A1/zh unknown
- 2015-12-16 WO PCT/US2015/066193 patent/WO2016100569A1/en not_active Ceased
- 2015-12-16 JP JP2017532656A patent/JP2017538722A/ja not_active Withdrawn
- 2015-12-16 MX MX2017008184A patent/MX2017008184A/es unknown
- 2015-12-16 CN CN201580076647.5A patent/CN107250145A/zh active Pending
- 2015-12-16 EP EP15871022.8A patent/EP3233879A4/en not_active Withdrawn
- 2015-12-16 AU AU2015364630A patent/AU2015364630A1/en not_active Abandoned
- 2015-12-16 US US14/971,926 patent/US9890188B2/en not_active Expired - Fee Related
- 2015-12-16 CA CA2970936A patent/CA2970936A1/en not_active Abandoned
- 2015-12-18 TW TW104142822A patent/TW201625658A/zh unknown
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2017
- 2017-07-18 ZA ZA2017/04876A patent/ZA201704876B/en unknown
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2018
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| WO2023142803A1 (zh) * | 2022-01-28 | 2023-08-03 | 北京恩泰伟医药科技有限公司 | 抗病毒化合物及其用途 |
| CN114288313A (zh) * | 2022-02-18 | 2022-04-08 | 常晓宇 | 嘧啶核苷类药物在制备预防或治疗冠状病毒感染性疾病药物中的用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| US9890188B2 (en) | 2018-02-13 |
| JP2017538722A (ja) | 2017-12-28 |
| US20160176910A1 (en) | 2016-06-23 |
| HK1245800A1 (zh) | 2018-08-31 |
| EP3233879A1 (en) | 2017-10-25 |
| CA2970936A1 (en) | 2016-06-23 |
| TW201625658A (zh) | 2016-07-16 |
| ZA201704876B (en) | 2020-01-29 |
| MX2017008184A (es) | 2018-03-06 |
| MA41213A (fr) | 2017-10-24 |
| WO2016100569A1 (en) | 2016-06-23 |
| US20180155384A1 (en) | 2018-06-07 |
| EP3233879A4 (en) | 2018-09-19 |
| AU2015364630A1 (en) | 2017-07-06 |
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