JP2018524403A5 - - Google Patents
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- JP2018524403A5 JP2018524403A5 JP2018520047A JP2018520047A JP2018524403A5 JP 2018524403 A5 JP2018524403 A5 JP 2018524403A5 JP 2018520047 A JP2018520047 A JP 2018520047A JP 2018520047 A JP2018520047 A JP 2018520047A JP 2018524403 A5 JP2018524403 A5 JP 2018524403A5
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- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- membered
- substituted
- compound according
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims description 51
- 150000001875 compounds Chemical class 0.000 claims description 45
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 29
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 25
- 125000005843 halogen group Chemical group 0.000 claims description 25
- 125000000623 heterocyclic group Chemical group 0.000 claims description 24
- 125000004429 atom Chemical group 0.000 claims description 23
- 229910052739 hydrogen Inorganic materials 0.000 claims description 22
- 125000001153 fluoro group Chemical group F* 0.000 claims description 21
- 210000004027 cell Anatomy 0.000 claims description 20
- 125000003545 alkoxy group Chemical group 0.000 claims description 16
- 239000001257 hydrogen Substances 0.000 claims description 14
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 13
- 229910052717 sulfur Inorganic materials 0.000 claims description 13
- 102100023933 Deoxyuridine 5'-triphosphate nucleotidohydrolase, mitochondrial Human genes 0.000 claims description 12
- 108010011219 dUTP pyrophosphatase Proteins 0.000 claims description 12
- 229910052799 carbon Inorganic materials 0.000 claims description 11
- 125000001424 substituent group Chemical group 0.000 claims description 11
- 201000010099 disease Diseases 0.000 claims description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 239000000203 mixture Substances 0.000 claims description 10
- 125000001072 heteroaryl group Chemical group 0.000 claims description 9
- 206010009944 Colon cancer Diseases 0.000 claims description 8
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 8
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 8
- 229910052805 deuterium Inorganic materials 0.000 claims description 8
- 150000002431 hydrogen Chemical class 0.000 claims description 8
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 206010017758 gastric cancer Diseases 0.000 claims description 6
- 230000014509 gene expression Effects 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 230000002018 overexpression Effects 0.000 claims description 6
- 201000011549 stomach cancer Diseases 0.000 claims description 6
- 239000011593 sulfur Substances 0.000 claims description 6
- 238000002560 therapeutic procedure Methods 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 5
- 230000002401 inhibitory effect Effects 0.000 claims description 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 5
- 229910052760 oxygen Inorganic materials 0.000 claims description 5
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 125000003342 alkenyl group Chemical group 0.000 claims description 4
- 125000002947 alkylene group Chemical group 0.000 claims description 4
- 208000029742 colonic neoplasm Diseases 0.000 claims description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
- 201000010536 head and neck cancer Diseases 0.000 claims description 4
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 3
- 125000000304 alkynyl group Chemical group 0.000 claims description 3
- 229910052731 fluorine Inorganic materials 0.000 claims description 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 3
- 150000003839 salts Chemical class 0.000 claims description 3
- 239000012453 solvate Substances 0.000 claims description 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 210000000601 blood cell Anatomy 0.000 claims description 2
- 230000005907 cancer growth Effects 0.000 claims description 2
- 229910052801 chlorine Inorganic materials 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000002708 enhancing effect Effects 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims description 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 238000012216 screening Methods 0.000 claims description 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 2
- KEQGZUUPPQEDPF-UHFFFAOYSA-N 1,3-dichloro-5,5-dimethylimidazolidine-2,4-dione Chemical compound CC1(C)N(Cl)C(=O)N(Cl)C1=O KEQGZUUPPQEDPF-UHFFFAOYSA-N 0.000 claims 1
- 230000003796 beauty Effects 0.000 claims 1
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 238000000034 method Methods 0.000 description 10
- 125000005647 linker group Chemical group 0.000 description 5
- 125000004450 alkenylene group Chemical group 0.000 description 3
- 125000004474 heteroalkylene group Chemical group 0.000 description 3
- 238000002405 diagnostic procedure Methods 0.000 description 2
- 239000000651 prodrug Substances 0.000 description 2
- 229940002612 prodrug Drugs 0.000 description 2
- -1 substituted Chemical class 0.000 description 2
- 125000006833 (C1-C5) alkylene group Chemical group 0.000 description 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 description 1
- 208000022072 Gallbladder Neoplasms Diseases 0.000 description 1
- 125000004419 alkynylene group Chemical group 0.000 description 1
- 125000000732 arylene group Chemical group 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 201000010175 gallbladder cancer Diseases 0.000 description 1
- 125000004404 heteroalkyl group Chemical group 0.000 description 1
- 125000005549 heteroarylene group Chemical group 0.000 description 1
- WJRBRSLFGCUECM-UHFFFAOYSA-N hydantoin Chemical group O=C1CNC(=O)N1 WJRBRSLFGCUECM-UHFFFAOYSA-N 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN740KO2015 | 2015-07-08 | ||
| IN740/KOL/2015 | 2015-07-08 | ||
| PCT/IB2016/054091 WO2017006282A1 (en) | 2015-07-08 | 2016-07-07 | Hydantoin containing deoxyuridine triphosphatase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020170594A Division JP7071044B2 (ja) | 2015-07-08 | 2020-10-08 | ヒダントインを含むデオキシウリジントリホスファターゼ阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018524403A JP2018524403A (ja) | 2018-08-30 |
| JP2018524403A5 true JP2018524403A5 (enExample) | 2019-08-22 |
| JP6836589B2 JP6836589B2 (ja) | 2021-03-03 |
Family
ID=56740270
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018520047A Active JP6836589B2 (ja) | 2015-07-08 | 2016-07-07 | ヒダントインを含むデオキシウリジントリホスファターゼ阻害剤 |
| JP2020170594A Active JP7071044B2 (ja) | 2015-07-08 | 2020-10-08 | ヒダントインを含むデオキシウリジントリホスファターゼ阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020170594A Active JP7071044B2 (ja) | 2015-07-08 | 2020-10-08 | ヒダントインを含むデオキシウリジントリホスファターゼ阻害剤 |
Country Status (16)
| Country | Link |
|---|---|
| US (6) | US10570098B2 (enExample) |
| EP (1) | EP3319939B1 (enExample) |
| JP (2) | JP6836589B2 (enExample) |
| CN (1) | CN107922330A (enExample) |
| AU (1) | AU2016290987C1 (enExample) |
| CA (1) | CA2991468C (enExample) |
| DK (1) | DK3319939T3 (enExample) |
| EA (1) | EA037990B1 (enExample) |
| ES (1) | ES3016670T3 (enExample) |
| FI (1) | FI3319939T3 (enExample) |
| HU (1) | HUE070225T2 (enExample) |
| IL (1) | IL256221B (enExample) |
| PL (1) | PL3319939T3 (enExample) |
| PT (1) | PT3319939T (enExample) |
| SI (1) | SI3319939T1 (enExample) |
| WO (1) | WO2017006282A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6450323B2 (ja) | 2013-01-07 | 2019-01-09 | ユニバーシティ オブ サザン カリフォルニア | デオキシウリジントリホスファターゼ阻害剤 |
| CA2935717C (en) | 2014-01-03 | 2022-06-21 | University Of Southern California | Uracil isostere and pharmaceutical compositions thereof useful as deoxyuridine triphosphatase inhibitors |
| WO2017006270A1 (en) | 2015-07-08 | 2017-01-12 | University Of Southern California | Deoxyuridine triphosphatase inhibitors |
| US10570100B2 (en) | 2015-07-08 | 2020-02-25 | University Of Southern California | Deoxyuridine triphosphatase inhibitors containing amino sulfonyl linkage |
| EP3319939B1 (en) | 2015-07-08 | 2024-11-27 | CV6 Therapeutics (NI) Limited | Hydantoin containing deoxyuridine triphosphatase inhibitors |
| WO2017006283A1 (en) | 2015-07-08 | 2017-01-12 | Cv6 Therapeutics (Ni) Limited | Deoxyuridine triphosphatase inhibitors containing cyclopropano linkage |
| CN109153648B (zh) | 2016-05-23 | 2022-07-22 | 豪夫迈·罗氏有限公司 | 具有叔酰胺官能团的苯并氮杂卓二甲酰胺化合物 |
| CN109311854B (zh) | 2016-05-23 | 2021-08-10 | 豪夫迈·罗氏有限公司 | 具有仲酰胺官能团的苯并氮杂卓二甲酰胺化合物 |
| CN109311851B (zh) | 2016-06-12 | 2021-08-10 | 豪夫迈·罗氏有限公司 | 二氢嘧啶基苯并氮杂䓬甲酰胺化合物 |
| WO2018098207A1 (en) * | 2016-11-23 | 2018-05-31 | Cv6 Therapeutics (Ni) Limited | Hydantoin containing deoxyuridine triphosphatase inhibitors |
| US10829457B2 (en) | 2016-11-23 | 2020-11-10 | Cv6 Therapeutics (Ni) Limited | Nitrogen ring linked deoxyuridine triphosphatase inhibitors |
| WO2018098206A1 (en) * | 2016-11-23 | 2018-05-31 | Cv6 Therapeutics (Ni) Limited | Hydantoin containing deoxyuridine triphosphatase inhibitors |
| US11168059B2 (en) | 2016-11-23 | 2021-11-09 | Cv6 Therapeutics (Ni) Limited | Amino sulfonyl compounds |
| WO2018098204A1 (en) | 2016-11-23 | 2018-05-31 | Cv6 Therapeutics (Ni) Limited | 6-membered uracil isosteres |
| WO2018128720A1 (en) | 2017-01-05 | 2018-07-12 | Cv6 Therapeutics (Ni) Limited | Uracil containing compounds |
| CA3185648A1 (en) * | 2020-06-26 | 2021-12-30 | Cv6 Therapeutics (Ni) Limited | Combination therapy with deoxyuridine triphosphatase inhibitors |
| CA3195519A1 (en) | 2020-09-18 | 2022-03-24 | Bayer Aktiengesellschaft | Pyrido[2,3-d]pyrimidin-4-amines as sos1 inhibitors |
| EP4074317A1 (en) | 2021-04-14 | 2022-10-19 | Bayer AG | Phosphorus derivatives as novel sos1 inhibitors |
| US12404242B2 (en) | 2021-12-17 | 2025-09-02 | Reglagene, Inc. | Compositions and methods for making and using small molecules in the treatment of cancer |
| EP4673130A1 (en) | 2023-02-28 | 2026-01-07 | Reglagene, Inc. | Compositions and methods for making and using small molecules for the treatment of health conditions |
| WO2025202022A1 (en) | 2024-03-27 | 2025-10-02 | Bayer Aktiengesellschaft | Anticancer macrocyclic quinazoline-based inhibitors of the ineraction between ras and sos1 |
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| JP6479970B2 (ja) | 2015-05-01 | 2019-03-06 | 大鵬薬品工業株式会社 | ウラシル化合物の新規結晶 |
| WO2017006270A1 (en) | 2015-07-08 | 2017-01-12 | University Of Southern California | Deoxyuridine triphosphatase inhibitors |
| EP3319939B1 (en) | 2015-07-08 | 2024-11-27 | CV6 Therapeutics (NI) Limited | Hydantoin containing deoxyuridine triphosphatase inhibitors |
| WO2017006283A1 (en) | 2015-07-08 | 2017-01-12 | Cv6 Therapeutics (Ni) Limited | Deoxyuridine triphosphatase inhibitors containing cyclopropano linkage |
| US10570100B2 (en) | 2015-07-08 | 2020-02-25 | University Of Southern California | Deoxyuridine triphosphatase inhibitors containing amino sulfonyl linkage |
| JP6871868B2 (ja) | 2016-01-08 | 2021-05-19 | 大鵬薬品工業株式会社 | 免疫調節剤を含有する抗腫瘍剤及び抗腫瘍効果増強剤 |
| WO2018098207A1 (en) | 2016-11-23 | 2018-05-31 | Cv6 Therapeutics (Ni) Limited | Hydantoin containing deoxyuridine triphosphatase inhibitors |
| US11168059B2 (en) | 2016-11-23 | 2021-11-09 | Cv6 Therapeutics (Ni) Limited | Amino sulfonyl compounds |
| WO2018098204A1 (en) | 2016-11-23 | 2018-05-31 | Cv6 Therapeutics (Ni) Limited | 6-membered uracil isosteres |
| WO2018098206A1 (en) | 2016-11-23 | 2018-05-31 | Cv6 Therapeutics (Ni) Limited | Hydantoin containing deoxyuridine triphosphatase inhibitors |
| US10829457B2 (en) | 2016-11-23 | 2020-11-10 | Cv6 Therapeutics (Ni) Limited | Nitrogen ring linked deoxyuridine triphosphatase inhibitors |
| WO2018128720A1 (en) | 2017-01-05 | 2018-07-12 | Cv6 Therapeutics (Ni) Limited | Uracil containing compounds |
-
2016
- 2016-07-07 EP EP16753974.1A patent/EP3319939B1/en active Active
- 2016-07-07 WO PCT/IB2016/054091 patent/WO2017006282A1/en not_active Ceased
- 2016-07-07 CN CN201680051434.1A patent/CN107922330A/zh active Pending
- 2016-07-07 JP JP2018520047A patent/JP6836589B2/ja active Active
- 2016-07-07 CA CA2991468A patent/CA2991468C/en active Active
- 2016-07-07 FI FIEP16753974.1T patent/FI3319939T3/fi active
- 2016-07-07 PT PT167539741T patent/PT3319939T/pt unknown
- 2016-07-07 SI SI201631891T patent/SI3319939T1/sl unknown
- 2016-07-07 DK DK16753974.1T patent/DK3319939T3/da active
- 2016-07-07 EA EA201890247A patent/EA037990B1/ru not_active IP Right Cessation
- 2016-07-07 US US15/741,202 patent/US10570098B2/en active Active
- 2016-07-07 AU AU2016290987A patent/AU2016290987C1/en active Active
- 2016-07-07 ES ES16753974T patent/ES3016670T3/es active Active
- 2016-07-07 PL PL16753974.1T patent/PL3319939T3/pl unknown
- 2016-07-07 HU HUE16753974A patent/HUE070225T2/hu unknown
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2017
- 2017-12-10 IL IL256221A patent/IL256221B/en active IP Right Grant
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2018
- 2018-03-07 US US15/914,958 patent/US10562860B2/en not_active Expired - Fee Related
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2020
- 2020-05-04 US US16/789,687 patent/US11104649B2/en active Active
- 2020-10-08 JP JP2020170594A patent/JP7071044B2/ja active Active
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2021
- 2021-05-14 US US17/320,650 patent/US11584723B2/en active Active
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2022
- 2022-12-05 US US18/075,316 patent/US12098133B2/en active Active
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2024
- 2024-08-16 US US18/807,770 patent/US20250188039A1/en active Pending
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