JPWO2019152911A5 - - Google Patents
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- Publication number
- JPWO2019152911A5 JPWO2019152911A5 JP2020564033A JP2020564033A JPWO2019152911A5 JP WO2019152911 A5 JPWO2019152911 A5 JP WO2019152911A5 JP 2020564033 A JP2020564033 A JP 2020564033A JP 2020564033 A JP2020564033 A JP 2020564033A JP WO2019152911 A5 JPWO2019152911 A5 JP WO2019152911A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- alkoxy
- pharmaceutically acceptable
- amide
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 62
- 125000005843 halogen group Chemical group 0.000 claims description 50
- 150000001875 compounds Chemical class 0.000 claims description 46
- 125000003545 alkoxy group Chemical group 0.000 claims description 44
- 150000003839 salts Chemical class 0.000 claims description 44
- 150000001408 amides Chemical class 0.000 claims description 42
- 150000002148 esters Chemical class 0.000 claims description 40
- 239000012453 solvate Substances 0.000 claims description 38
- 125000003118 aryl group Chemical group 0.000 claims description 30
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 24
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 22
- 239000012636 effector Substances 0.000 claims description 20
- -1 amino, hydroxy, thio Chemical group 0.000 claims description 19
- 125000000304 alkynyl group Chemical group 0.000 claims description 16
- 229960005277 gemcitabine Drugs 0.000 claims description 16
- 125000001072 heteroaryl group Chemical group 0.000 claims description 14
- 229910052757 nitrogen Inorganic materials 0.000 claims description 14
- 125000003342 alkenyl group Chemical group 0.000 claims description 12
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 10
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 229910052739 hydrogen Inorganic materials 0.000 claims description 8
- 239000001257 hydrogen Substances 0.000 claims description 8
- 150000002431 hydrogen Chemical class 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 8
- 150000008298 phosphoramidates Chemical class 0.000 claims description 8
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 6
- 230000002062 proliferating effect Effects 0.000 claims description 6
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims description 4
- 125000003302 alkenyloxy group Chemical group 0.000 claims description 4
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 4
- 125000004171 alkoxy aryl group Chemical group 0.000 claims description 4
- 125000006350 alkyl thio alkyl group Chemical group 0.000 claims description 4
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims description 4
- 125000004104 aryloxy group Chemical group 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 239000001301 oxygen Substances 0.000 claims description 4
- 150000003013 phosphoric acid derivatives Chemical class 0.000 claims description 4
- 150000008299 phosphorodiamidates Chemical class 0.000 claims description 4
- 229940124530 sulfonamide Drugs 0.000 claims description 4
- 150000003456 sulfonamides Chemical class 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 125000004434 sulfur atom Chemical group 0.000 claims description 4
- 210000004881 tumor cell Anatomy 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 3
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 2
- 101000725164 Homo sapiens Cytochrome P450 1B1 Proteins 0.000 claims description 2
- 229910019142 PO4 Inorganic materials 0.000 claims description 2
- 125000004423 acyloxy group Chemical group 0.000 claims description 2
- 125000005041 acyloxyalkyl group Chemical group 0.000 claims description 2
- 125000003282 alkyl amino group Chemical group 0.000 claims description 2
- 125000005133 alkynyloxy group Chemical group 0.000 claims description 2
- 210000004556 brain Anatomy 0.000 claims description 2
- 210000000481 breast Anatomy 0.000 claims description 2
- 125000001246 bromo group Chemical group Br* 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 150000001721 carbon Chemical group 0.000 claims description 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 210000001072 colon Anatomy 0.000 claims description 2
- 125000004122 cyclic group Chemical group 0.000 claims description 2
- 229910052805 deuterium Inorganic materials 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 210000003128 head Anatomy 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 210000003734 kidney Anatomy 0.000 claims description 2
- 210000004185 liver Anatomy 0.000 claims description 2
- 210000004072 lung Anatomy 0.000 claims description 2
- 239000002207 metabolite Substances 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims description 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 2
- 210000003739 neck Anatomy 0.000 claims description 2
- 210000001672 ovary Anatomy 0.000 claims description 2
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims description 2
- 210000000496 pancreas Anatomy 0.000 claims description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 2
- 239000010452 phosphate Substances 0.000 claims description 2
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 210000002307 prostate Anatomy 0.000 claims description 2
- 210000003491 skin Anatomy 0.000 claims description 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 2
- LURSQGOJGVDZFI-UHFFFAOYSA-N sulfino hydrogen sulfate Chemical compound OS(=O)OS(O)(=O)=O LURSQGOJGVDZFI-UHFFFAOYSA-N 0.000 claims description 2
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 claims description 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 2
- 150000003536 tetrazoles Chemical class 0.000 claims description 2
- 150000003568 thioethers Chemical class 0.000 claims description 2
- 150000003573 thiols Chemical class 0.000 claims description 2
- 210000003932 urinary bladder Anatomy 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 239000003814 drug Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024019158A JP2024073414A (ja) | 2018-02-02 | 2024-02-13 | ゲムシタビン誘導体の新規小分子薬物コンジュゲート |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862625779P | 2018-02-02 | 2018-02-02 | |
| US62/625,779 | 2018-02-02 | ||
| PCT/US2019/016477 WO2019152911A1 (en) | 2018-02-02 | 2019-02-04 | Novel small molecule drug conjugates of gemcitabine derivatives |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024019158A Division JP2024073414A (ja) | 2018-02-02 | 2024-02-13 | ゲムシタビン誘導体の新規小分子薬物コンジュゲート |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021512951A JP2021512951A (ja) | 2021-05-20 |
| JP2021512951A5 JP2021512951A5 (https=) | 2022-02-14 |
| JPWO2019152911A5 true JPWO2019152911A5 (https=) | 2022-02-14 |
Family
ID=65494546
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020564033A Pending JP2021512951A (ja) | 2018-02-02 | 2019-02-04 | ゲムシタビン誘導体の新規小分子薬物コンジュゲート |
| JP2024019158A Pending JP2024073414A (ja) | 2018-02-02 | 2024-02-13 | ゲムシタビン誘導体の新規小分子薬物コンジュゲート |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024019158A Pending JP2024073414A (ja) | 2018-02-02 | 2024-02-13 | ゲムシタビン誘導体の新規小分子薬物コンジュゲート |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20210380626A1 (https=) |
| EP (1) | EP3746133A1 (https=) |
| JP (2) | JP2021512951A (https=) |
| KR (1) | KR20200118828A (https=) |
| CN (1) | CN112135635A (https=) |
| AU (1) | AU2019216514A1 (https=) |
| BR (1) | BR112020015747A2 (https=) |
| CA (1) | CA3090272A1 (https=) |
| EA (1) | EA202091857A1 (https=) |
| IL (1) | IL276442A (https=) |
| PH (1) | PH12020551178A1 (https=) |
| SG (1) | SG11202007381YA (https=) |
| WO (1) | WO2019152911A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20210367A1 (es) * | 2018-02-02 | 2021-02-26 | Maverix Oncology Inc | Conjugados de farmacos de molecula pequena de monofosfato de gemcitabina |
| CN114349816B (zh) * | 2021-11-30 | 2024-08-30 | 潍坊博创国际生物医药研究院 | 一种基于氨肽酶n/cd13的小分子偶联分子及其制备方法和应用 |
| WO2026009986A1 (ja) * | 2024-07-05 | 2026-01-08 | 学校法人東京理科大学 | 化合物の製造方法及び化合物 |
| WO2026009987A1 (ja) * | 2024-07-05 | 2026-01-08 | 学校法人東京理科大学 | 化合物の製造方法、化合物、及びヌクレオチドプロドラッグ前駆体 |
| CN119708099B (zh) * | 2024-12-23 | 2025-10-24 | 中国药科大学 | 吉西他滨前药及其医药用途 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2531599A (en) | 1998-02-12 | 1999-08-30 | De Montfort University | Hydroxylation activated drug release |
| US7148226B2 (en) | 2003-02-21 | 2006-12-12 | Agouron Pharmaceuticals, Inc. | Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same |
| GB0317009D0 (en) * | 2003-07-21 | 2003-08-27 | Univ Cardiff | Chemical compounds |
| GB0907551D0 (en) * | 2009-05-01 | 2009-06-10 | Univ Dundee | Treatment or prophylaxis of proliferative conditions |
| JP6212831B2 (ja) * | 2013-12-04 | 2017-10-18 | 杭州源昶医薬科技有限公司 | ゲムシタビン誘導体、該誘導体を含む組成物及び該誘導体の製薬用途 |
| WO2015134334A1 (en) * | 2014-03-03 | 2015-09-11 | Suo Zucai | Gemcitabine analogs |
| CN105001291B (zh) * | 2014-04-15 | 2018-12-04 | 上海知萌生物医药科技有限公司 | 吉西他滨化学传递前药及其制备方法和应用 |
| US20180044368A1 (en) * | 2015-02-25 | 2018-02-15 | Ligand Pharmaceuticals, Inc. | Gemcitabine derivatives |
-
2019
- 2019-02-04 US US16/967,086 patent/US20210380626A1/en not_active Abandoned
- 2019-02-04 KR KR1020207025177A patent/KR20200118828A/ko not_active Ceased
- 2019-02-04 SG SG11202007381YA patent/SG11202007381YA/en unknown
- 2019-02-04 EA EA202091857A patent/EA202091857A1/ru unknown
- 2019-02-04 EP EP19706106.2A patent/EP3746133A1/en not_active Withdrawn
- 2019-02-04 CN CN201980024089.6A patent/CN112135635A/zh active Pending
- 2019-02-04 AU AU2019216514A patent/AU2019216514A1/en not_active Abandoned
- 2019-02-04 WO PCT/US2019/016477 patent/WO2019152911A1/en not_active Ceased
- 2019-02-04 BR BR112020015747-3A patent/BR112020015747A2/pt not_active IP Right Cessation
- 2019-02-04 CA CA3090272A patent/CA3090272A1/en active Pending
- 2019-02-04 JP JP2020564033A patent/JP2021512951A/ja active Pending
-
2020
- 2020-08-02 IL IL276442A patent/IL276442A/en unknown
- 2020-08-03 PH PH12020551178A patent/PH12020551178A1/en unknown
-
2024
- 2024-02-13 JP JP2024019158A patent/JP2024073414A/ja active Pending
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