HRP20231037T1 - Deuterirani spojevi za upotrebu u liječenju raka - Google Patents
Deuterirani spojevi za upotrebu u liječenju raka Download PDFInfo
- Publication number
- HRP20231037T1 HRP20231037T1 HRP20231037TT HRP20231037T HRP20231037T1 HR P20231037 T1 HRP20231037 T1 HR P20231037T1 HR P20231037T T HRP20231037T T HR P20231037TT HR P20231037 T HRP20231037 T HR P20231037T HR P20231037 T1 HRP20231037 T1 HR P20231037T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- formula
- image
- derivative
- deuterated derivative
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims 19
- 206010028980 Neoplasm Diseases 0.000 title claims 2
- 201000011510 cancer Diseases 0.000 title claims 2
- 238000011282 treatment Methods 0.000 title claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- XDGNFDFXUBJGRV-YQCADYNBSA-N ClC=1C(=CC(=C(C=1)N(C(=O)[C@H]1N(C([C@H]([C@H]1O)O)=O)C1=NC(=CC(=C1)C(F)(F)F)C)C([2H])([2H])[2H])F)F Chemical compound ClC=1C(=CC(=C(C=1)N(C(=O)[C@H]1N(C([C@H]([C@H]1O)O)=O)C1=NC(=CC(=C1)C(F)(F)F)C)C([2H])([2H])[2H])F)F XDGNFDFXUBJGRV-YQCADYNBSA-N 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (10)
1. Deuterirani derivat spoja formule (I):
[image]
ili njegov tautomerni ili stereokemijski izomerni oblik, ili njegov farmaceutski prihvatljiv solvat.
2. Spoj prema tvrdnji 1 u kojem deuterirani derivat sadrži deuteraciju jednog ili više (kao što su sva 3) atoma vodika N-metilne skupine.
3. Spoj prema tvrdnji 2 u kojem je deuterirani derivat spoj formule (II):
[image]
ili njegov tautomerni ili stereokemijski izomerni oblik, ili njegov farmaceutski prihvatljiv solvat.
4. Spoj prema tvrdnji 3 koji je slobodna baza spoja formule (II) i (2S,3S,4S)-N-(5-kloro-2,4-difluorofenil)-3,4- dihidroksi-N-(metil-d3)-1-(6-metil-4-(trifluormetil)piridin-2-il)-5-oksopirolidin-2-karboksamid (E1).
5. Farmaceutski pripravak koji sadrži spoj formule (I) prema bilo kojoj od tvrdnji 1 do 4.
6. Farmaceutski pripravak koji sadrži spoj formule (I) prema bilo kojoj od tvrdnji 1 do 4, u kombinaciji s jednim ili više terapijskih aktivnih tvari.
7. Spoj prema bilo kojoj od tvrdnji 1 do 4 koji se koristi u terapiji.
8. Spoj prema bilo prema bilo kojoj od tvrdnji 1 do 4 koji se koristi u profilaksi ili liječenju raka.
9. Postupak za pripremu deuteriranog derivata spoja formule (I) prema tvrdnji 1 koji sadrži sljedeće:
(a) reakcija deuteriranog derivata spoja formule (III):
[image]
sa spojem formule (IV):
[image]
(b) uklanjanje zaštite sa zaštićenog derivata spoja formule (I): i
(c) međukonverzija spoja formule (I) ili njegovog zaštićenog derivata u daljnji spoj formule (I) ili njegov zaštićeni derivat.
10. Postupak prema zahtjevu 9, naznačen time što je spoj formule (III) spoj formule (III)a:
[image]
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/GB2019/052240 WO2021028643A1 (en) | 2019-08-09 | 2019-08-09 | Heterocyclic compounds for use in the treatment of cancer |
| GBGB1917863.1A GB201917863D0 (en) | 2019-12-06 | 2019-12-06 | Novel compounds |
| EP20754011.3A EP4010329B9 (en) | 2019-08-09 | 2020-08-10 | Deuterated compounds for use in the treatment of cancer |
| PCT/GB2020/051901 WO2021028670A1 (en) | 2019-08-09 | 2020-08-10 | Deuterated compounds for use in the treatment of cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20231037T1 true HRP20231037T1 (hr) | 2023-12-08 |
Family
ID=72039615
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20231037TT HRP20231037T1 (hr) | 2019-08-09 | 2020-08-10 | Deuterirani spojevi za upotrebu u liječenju raka |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US20220259174A1 (hr) |
| EP (1) | EP4010329B9 (hr) |
| JP (1) | JP2022544211A (hr) |
| KR (1) | KR20220050148A (hr) |
| CN (1) | CN114846003A (hr) |
| AU (1) | AU2020327661A1 (hr) |
| BR (1) | BR112022002496A2 (hr) |
| CA (1) | CA3149119A1 (hr) |
| DK (1) | DK4010329T3 (hr) |
| ES (1) | ES2952281T3 (hr) |
| FI (1) | FI4010329T3 (hr) |
| HR (1) | HRP20231037T1 (hr) |
| HU (1) | HUE063145T2 (hr) |
| IL (1) | IL290415A (hr) |
| LT (1) | LT4010329T (hr) |
| MX (1) | MX2022001690A (hr) |
| PL (1) | PL4010329T3 (hr) |
| PT (1) | PT4010329T (hr) |
| RS (1) | RS64486B1 (hr) |
| SI (1) | SI4010329T1 (hr) |
| TW (1) | TW202120486A (hr) |
| WO (1) | WO2021028670A1 (hr) |
| ZA (1) | ZA202201364B (hr) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2022216878A1 (en) * | 2021-02-07 | 2023-08-17 | Artios Pharma Limited | Novel process |
| WO2023125841A1 (zh) * | 2021-12-29 | 2023-07-06 | 武汉人福创新药物研发中心有限公司 | 作为Polθ抑制剂的杂环化合物及其制备方法和用途 |
| WO2023125918A1 (zh) * | 2021-12-30 | 2023-07-06 | 上海湃隆生物科技有限公司 | 一种DNA聚合酶theta抑制剂及其应用 |
| TW202341998A (zh) * | 2022-03-10 | 2023-11-01 | 大陸商四川海思科製藥有限公司 | DNA聚合酶θ抑制劑及其用途 |
| WO2023169573A1 (zh) * | 2022-03-11 | 2023-09-14 | 武汉人福创新药物研发中心有限公司 | 一种Polθ抑制剂 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9474779B2 (en) * | 2012-01-19 | 2016-10-25 | Agios Pharmaceuticals, Inc. | Therapeutically active compositions and their methods of use |
| CA2860858A1 (en) * | 2012-01-19 | 2013-07-25 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and their methods of use |
| WO2015010297A1 (en) * | 2013-07-25 | 2015-01-29 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and their methods of use |
| WO2017062754A1 (en) | 2015-10-07 | 2017-04-13 | New York University | Compositions and methods for enhancing crispr activity by polq inhibition |
| CN107556366A (zh) * | 2016-06-30 | 2018-01-09 | 上海海和药物研究开发有限公司 | 具有突变型异柠檬酸脱氢酶抑制活性的化合物、其制备方法及用途 |
-
2020
- 2020-08-07 TW TW109126865A patent/TW202120486A/zh unknown
- 2020-08-10 ES ES20754011T patent/ES2952281T3/es active Active
- 2020-08-10 LT LTEPPCT/GB2020/051901T patent/LT4010329T/lt unknown
- 2020-08-10 AU AU2020327661A patent/AU2020327661A1/en active Pending
- 2020-08-10 CA CA3149119A patent/CA3149119A1/en active Pending
- 2020-08-10 BR BR112022002496A patent/BR112022002496A2/pt unknown
- 2020-08-10 HU HUE20754011A patent/HUE063145T2/hu unknown
- 2020-08-10 PL PL20754011.3T patent/PL4010329T3/pl unknown
- 2020-08-10 CN CN202080070533.0A patent/CN114846003A/zh active Pending
- 2020-08-10 RS RS20230694A patent/RS64486B1/sr unknown
- 2020-08-10 FI FIEP20754011.3T patent/FI4010329T3/fi active
- 2020-08-10 JP JP2022507895A patent/JP2022544211A/ja active Pending
- 2020-08-10 HR HRP20231037TT patent/HRP20231037T1/hr unknown
- 2020-08-10 DK DK20754011.3T patent/DK4010329T3/da active
- 2020-08-10 PT PT207540113T patent/PT4010329T/pt unknown
- 2020-08-10 MX MX2022001690A patent/MX2022001690A/es unknown
- 2020-08-10 SI SI202030260T patent/SI4010329T1/sl unknown
- 2020-08-10 EP EP20754011.3A patent/EP4010329B9/en active Active
- 2020-08-10 US US17/597,957 patent/US20220259174A1/en active Pending
- 2020-08-10 KR KR1020227007755A patent/KR20220050148A/ko unknown
- 2020-08-10 WO PCT/GB2020/051901 patent/WO2021028670A1/en active Application Filing
-
2022
- 2022-01-28 ZA ZA2022/01364A patent/ZA202201364B/en unknown
- 2022-02-07 IL IL290415A patent/IL290415A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP4010329A1 (en) | 2022-06-15 |
| EP4010329B9 (en) | 2023-10-04 |
| BR112022002496A2 (pt) | 2022-04-26 |
| AU2020327661A1 (en) | 2022-02-24 |
| RS64486B1 (sr) | 2023-09-29 |
| MX2022001690A (es) | 2022-05-10 |
| US20220259174A1 (en) | 2022-08-18 |
| TW202120486A (zh) | 2021-06-01 |
| CA3149119A1 (en) | 2021-02-18 |
| LT4010329T (lt) | 2023-09-11 |
| ZA202201364B (en) | 2023-11-29 |
| IL290415A (en) | 2022-04-01 |
| EP4010329B1 (en) | 2023-06-07 |
| PL4010329T3 (pl) | 2023-10-16 |
| ES2952281T3 (es) | 2023-10-30 |
| PT4010329T (pt) | 2023-08-18 |
| CN114846003A (zh) | 2022-08-02 |
| WO2021028670A1 (en) | 2021-02-18 |
| JP2022544211A (ja) | 2022-10-17 |
| FI4010329T3 (fi) | 2023-08-30 |
| KR20220050148A (ko) | 2022-04-22 |
| DK4010329T3 (da) | 2023-09-04 |
| HUE063145T2 (hu) | 2023-12-28 |
| SI4010329T1 (sl) | 2023-10-30 |
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