TWI741268B - 干擾素基因刺激劑（ｓｔｉｎｇ）的環戊烷為主體之調節劑 - Google Patents
干擾素基因刺激劑（ｓｔｉｎｇ）的環戊烷為主體之調節劑 Download PDFInfo
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- TWI741268B TWI741268B TW108108048A TW108108048A TWI741268B TW I741268 B TWI741268 B TW I741268B TW 108108048 A TW108108048 A TW 108108048A TW 108108048 A TW108108048 A TW 108108048A TW I741268 B TWI741268 B TW I741268B
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- acceptable salt
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- BEGKMFFZJBOVOW-PQONOLLKSA-N CN(C=Nc1c2nc[n]1[C@H](C[C@@H]([C@H]1O)OP(O)(O[C@H]([C@@H](CO3)O[C@H]4[n]5c(ncnc6N)c6nc5)[C@H]4F)=O)[C@@H]1OP3(O)=O)C2=O Chemical compound CN(C=Nc1c2nc[n]1[C@H](C[C@@H]([C@H]1O)OP(O)(O[C@H]([C@@H](CO3)O[C@H]4[n]5c(ncnc6N)c6nc5)[C@H]4F)=O)[C@@H]1OP3(O)=O)C2=O BEGKMFFZJBOVOW-PQONOLLKSA-N 0.000 description 1
- BTCUYIDXTLYAGE-GZQJALTCSA-N CN(C=Nc1c2nc[n]1[C@H](C[C@@H]([C@H]1O)OP(O)(O[C@H]([C@@H](CO3)O[C@H]4[n]5c(ncnc6N)c6nc5)[C@H]4F)=O)[C@@H]1OP3(S)=O)C2=O Chemical compound CN(C=Nc1c2nc[n]1[C@H](C[C@@H]([C@H]1O)OP(O)(O[C@H]([C@@H](CO3)O[C@H]4[n]5c(ncnc6N)c6nc5)[C@H]4F)=O)[C@@H]1OP3(S)=O)C2=O BTCUYIDXTLYAGE-GZQJALTCSA-N 0.000 description 1
- ONXGWHMOJWHEBW-GZQJALTCSA-N CN(C=Nc1c2nc[n]1[C@H](C[C@@H]([C@H]1O)OP(O[C@H]([C@@H](CO3)O[C@H]4[n]5c(ncnc6N)c6nc5)[C@H]4F)(S)=O)[C@@H]1OP3(O)=O)C2=O Chemical compound CN(C=Nc1c2nc[n]1[C@H](C[C@@H]([C@H]1O)OP(O[C@H]([C@@H](CO3)O[C@H]4[n]5c(ncnc6N)c6nc5)[C@H]4F)(S)=O)[C@@H]1OP3(O)=O)C2=O ONXGWHMOJWHEBW-GZQJALTCSA-N 0.000 description 1
- CQZPNWQHPYNXRU-VULZSUNMSA-N CN(C=Nc1c2nc[n]1[C@H](C[C@@H]([C@H]1O)OP(O[C@H]([C@@H](CO3)O[C@H]4[n]5c(ncnc6N)c6nc5)[C@H]4F)(S)=S)[C@@H]1OP3(S)=O)C2=O Chemical compound CN(C=Nc1c2nc[n]1[C@H](C[C@@H]([C@H]1O)OP(O[C@H]([C@@H](CO3)O[C@H]4[n]5c(ncnc6N)c6nc5)[C@H]4F)(S)=S)[C@@H]1OP3(S)=O)C2=O CQZPNWQHPYNXRU-VULZSUNMSA-N 0.000 description 1
- UIFNZLJEUSSYFS-PQONOLLKSA-N CN(C=Nc1c2nc[n]1[C@H](C[C@@H]([C@H]1O)OP(O[C@H]([C@@H](CO3)O[C@H]4[n]5c(ncnc6N)c6nc5)[C@H]4F)(S)=S)[C@@H]1OP3(S)=S)C2=O Chemical compound CN(C=Nc1c2nc[n]1[C@H](C[C@@H]([C@H]1O)OP(O[C@H]([C@@H](CO3)O[C@H]4[n]5c(ncnc6N)c6nc5)[C@H]4F)(S)=S)[C@@H]1OP3(S)=S)C2=O UIFNZLJEUSSYFS-PQONOLLKSA-N 0.000 description 1
- ZBULTWRPOHNBKI-UHFFFAOYSA-N CN[n]1c(ncnc2N)c2nc1 Chemical compound CN[n]1c(ncnc2N)c2nc1 ZBULTWRPOHNBKI-UHFFFAOYSA-N 0.000 description 1
- MPUQZZVXUAVLFX-MWWRQMINSA-N COc1n[n]([C@H](C[C@@H]([C@H]2O)OP(O[C@H]([C@@H](CO3)O[C@H]4[n]5c(ncnc6N)c6nc5)[C@H]4F)(S)=O)[C@@H]2OP3(S)=O)c2c1c(N)ncn2 Chemical compound COc1n[n]([C@H](C[C@@H]([C@H]2O)OP(O[C@H]([C@@H](CO3)O[C@H]4[n]5c(ncnc6N)c6nc5)[C@H]4F)(S)=O)[C@@H]2OP3(S)=O)c2c1c(N)ncn2 MPUQZZVXUAVLFX-MWWRQMINSA-N 0.000 description 1
- WRXCXOUDSPTXNX-UHFFFAOYSA-N C[n]1c(ncnc2N)c2nc1 Chemical compound C[n]1c(ncnc2N)c2nc1 WRXCXOUDSPTXNX-UHFFFAOYSA-N 0.000 description 1
- KYLNRLGTUGNTDS-KFMYDLODSA-N NC(c1c(N[C@H](C[C@@H]([C@H]2O)OP(O[C@H]([C@@H](CO3)O[C@H]4[n]5c(ncnc6N)c6nc5)[C@H]4F)(S)=O)[C@@H]2OP3(S)=O)ncnc1N)=O Chemical compound NC(c1c(N[C@H](C[C@@H]([C@H]2O)OP(O[C@H]([C@@H](CO3)O[C@H]4[n]5c(ncnc6N)c6nc5)[C@H]4F)(S)=O)[C@@H]2OP3(S)=O)ncnc1N)=O KYLNRLGTUGNTDS-KFMYDLODSA-N 0.000 description 1
- QHWRPYQNSZKXDH-KHSDFGGFSA-N Nc1ncnc2c1nc[n]2[C@H](C[C@@H]([C@H]1O)OP(O[C@H]([C@@H](CS2)O[C@H]3N4[I]=Nc5c4ncnc5N)[C@H]3F)(S)=O)[C@@H]1OP2(O)=O Chemical compound Nc1ncnc2c1nc[n]2[C@H](C[C@@H]([C@H]1O)OP(O[C@H]([C@@H](CS2)O[C@H]3N4[I]=Nc5c4ncnc5N)[C@H]3F)(S)=O)[C@@H]1OP2(O)=O QHWRPYQNSZKXDH-KHSDFGGFSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
- C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
- C07F9/6574—Esters of oxyacids of phosphorus
- C07F9/65744—Esters of oxyacids of phosphorus condensed with carbocyclic or heterocyclic rings or ring systems
-
- 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
- C07H19/23—Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups C07H19/14 - C07H19/22
-
- 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
- C07H19/16—Purine radicals
- C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
- C07H19/213—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
-
- 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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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (8)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862643467P | 2018-03-15 | 2018-03-15 | |
| US62/643,467 | 2018-03-15 | ||
| US201862666204P | 2018-05-03 | 2018-05-03 | |
| US62/666,204 | 2018-05-03 | ||
| US201862742532P | 2018-10-08 | 2018-10-08 | |
| US62/742,532 | 2018-10-08 | ||
| US201962809990P | 2019-02-25 | 2019-02-25 | |
| US62/809,990 | 2019-02-25 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW201945036A TW201945036A (zh) | 2019-12-01 |
| TWI741268B true TWI741268B (zh) | 2021-10-01 |
Family
ID=66103038
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW108108048A TWI741268B (zh) | 2018-03-15 | 2019-03-11 | 干擾素基因刺激劑（ｓｔｉｎｇ）的環戊烷為主體之調節劑 |
Country Status (25)
| Country | Link |
|---|---|
| US (4) | US10538542B2 (https=) |
| EP (1) | EP3765474B1 (https=) |
| JP (1) | JP7266942B2 (https=) |
| KR (1) | KR20200131878A (https=) |
| CN (1) | CN111918871A (https=) |
| AU (1) | AU2019234043A1 (https=) |
| BR (1) | BR112020018593A2 (https=) |
| CA (1) | CA3093631C (https=) |
| CL (1) | CL2020002352A1 (https=) |
| CR (1) | CR20200382A (https=) |
| DO (1) | DOP2020000160A (https=) |
| EC (1) | ECSP20057847A (https=) |
| ES (1) | ES2923298T3 (https=) |
| IL (1) | IL277278A (https=) |
| MA (1) | MA52012A (https=) |
| MX (1) | MX2020009587A (https=) |
| NI (1) | NI202000058A (https=) |
| PE (1) | PE20210412A1 (https=) |
| PH (1) | PH12020551486A1 (https=) |
| PY (1) | PY1919127A (https=) |
| RU (1) | RU2020130048A (https=) |
| SG (1) | SG11202008102VA (https=) |
| TW (1) | TWI741268B (https=) |
| UY (1) | UY38145A (https=) |
| WO (1) | WO2019175776A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10966999B2 (en) | 2017-12-20 | 2021-04-06 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3′3′ cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| CN111511754B (zh) | 2017-12-20 | 2023-09-12 | 捷克共和国有机化学与生物化学研究所 | 活化sting转接蛋白的具有膦酸酯键的2’3’环状二核苷酸 |
| US10538542B2 (en) * | 2018-03-15 | 2020-01-21 | Pfizer Inc. | Cyclopentane-based modulators of STING (stimulator of interferon genes) |
| TWI833744B (zh) | 2018-04-06 | 2024-03-01 | 捷克科學院有機化學與生物化學研究所 | 3'3'-環二核苷酸 |
| TW202028179A (zh) | 2018-10-08 | 2020-08-01 | 美商普萊恩醫療公司 | 胺基酸化合物及使用方法 |
| JP2022550297A (ja) * | 2019-09-25 | 2022-12-01 | ファイザー・インク | Ｓｔｉｎｇ（インターフェロン遺伝子刺激因子）のヘテロ多環式モジュレーター |
| WO2021206158A1 (ja) | 2020-04-10 | 2021-10-14 | 小野薬品工業株式会社 | がん治療方法 |
| JP2023553069A (ja) * | 2020-12-08 | 2023-12-20 | エフ． ホフマン－ラ ロシュ アーゲー | ホスホロジチオエートオリゴヌクレオチドの新規合成 |
| US11964978B2 (en) * | 2021-03-18 | 2024-04-23 | Pfizer Inc. | Modulators of STING (stimulator of interferon genes) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015185565A1 (en) * | 2014-06-04 | 2015-12-10 | Glaxosmithkline Intellectual Property Development Limited | Cyclic di-nucleotides as modulators of sting |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
| GB201501462D0 (en) * | 2015-01-29 | 2015-03-18 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| US10538542B2 (en) * | 2018-03-15 | 2020-01-21 | Pfizer Inc. | Cyclopentane-based modulators of STING (stimulator of interferon genes) |
-
2019
- 2019-03-11 US US16/297,910 patent/US10538542B2/en active Active
- 2019-03-11 TW TW108108048A patent/TWI741268B/zh not_active IP Right Cessation
- 2019-03-12 MX MX2020009587A patent/MX2020009587A/es unknown
- 2019-03-12 SG SG11202008102VA patent/SG11202008102VA/en unknown
- 2019-03-12 CR CR20200382A patent/CR20200382A/es unknown
- 2019-03-12 AU AU2019234043A patent/AU2019234043A1/en not_active Abandoned
- 2019-03-12 CA CA3093631A patent/CA3093631C/en active Active
- 2019-03-12 ES ES19717149T patent/ES2923298T3/es active Active
- 2019-03-12 KR KR1020207029472A patent/KR20200131878A/ko not_active Withdrawn
- 2019-03-12 EP EP19717149.9A patent/EP3765474B1/en active Active
- 2019-03-12 WO PCT/IB2019/052009 patent/WO2019175776A1/en not_active Ceased
- 2019-03-12 JP JP2020548916A patent/JP7266942B2/ja active Active
- 2019-03-12 CN CN201980019494.9A patent/CN111918871A/zh active Pending
- 2019-03-12 PE PE2020001412A patent/PE20210412A1/es unknown
- 2019-03-12 RU RU2020130048A patent/RU2020130048A/ru unknown
- 2019-03-12 BR BR112020018593-0A patent/BR112020018593A2/pt not_active IP Right Cessation
- 2019-03-12 MA MA052012A patent/MA52012A/fr unknown
- 2019-03-13 PY PY201901919127A patent/PY1919127A/es unknown
- 2019-03-13 UY UY38145A patent/UY38145A/es not_active Application Discontinuation
- 2019-12-04 US US16/702,738 patent/US10968242B2/en active Active
-
2020
- 2020-08-25 DO DO2020000160A patent/DOP2020000160A/es unknown
- 2020-08-28 NI NI202000058A patent/NI202000058A/es unknown
- 2020-09-10 IL IL277278A patent/IL277278A/en unknown
- 2020-09-11 CL CL2020002352A patent/CL2020002352A1/es unknown
- 2020-09-12 PH PH12020551486A patent/PH12020551486A1/en unknown
- 2020-09-15 EC ECSENADI202057847A patent/ECSP20057847A/es unknown
-
2021
- 2021-03-03 US US17/190,924 patent/US20210230196A1/en not_active Abandoned
-
2023
- 2023-07-24 US US18/225,589 patent/US20230382932A1/en not_active Abandoned
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015185565A1 (en) * | 2014-06-04 | 2015-12-10 | Glaxosmithkline Intellectual Property Development Limited | Cyclic di-nucleotides as modulators of sting |
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| MM4A | Annulment or lapse of patent due to non-payment of fees |