HRP20220459T1 - Inhibitori cd73 - Google Patents
Inhibitori cd73 Download PDFInfo
- Publication number
- HRP20220459T1 HRP20220459T1 HRP20220459TT HRP20220459T HRP20220459T1 HR P20220459 T1 HRP20220459 T1 HR P20220459T1 HR P20220459T T HRP20220459T T HR P20220459TT HR P20220459 T HRP20220459 T HR P20220459T HR P20220459 T1 HRP20220459 T1 HR P20220459T1
- Authority
- HR
- Croatia
- Prior art keywords
- image
- pharmaceutically acceptable
- acceptable salt
- compound according
- cancer
- Prior art date
Links
- 229940127272 CD73 inhibitor Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 15
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- SXVLKJCZFKIBAV-WPRPVWTQSA-N 5-[5-[(1S,2S)-2-ethylcyclopropyl]-6-methylpyridazin-3-yl]-1H-pyrimidine-2,4-dione Chemical compound C(C)[C@@H]1[C@H](C1)C=1C=C(N=NC=1C)C=1C(NC(NC=1)=O)=O SXVLKJCZFKIBAV-WPRPVWTQSA-N 0.000 claims 1
- WHRUIISQCORGKK-KOLCDFICSA-N 5-[6-methyl-5-[(1S,2R)-2-propan-2-ylcyclopropyl]pyridazin-3-yl]-1H-pyrimidine-2,4-dione Chemical compound C(C)(C)[C@@H]1[C@H](C1)C=1C=C(N=NC=1C)C=1C(NC(NC=1)=O)=O WHRUIISQCORGKK-KOLCDFICSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (16)
1. Spoj formule:
[image]
,
naznačen time što
n je 0-3;
R1 je -H, -F, -gem-difluor, -gem-dimetil,
-C1-4 alkil, -CHF2, -CF2CH3 ili -CH2CH2F; i
R2 se bira između -H, -CH3, -F, -Cl, -CN ili -OCH3;
ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je:
[image]
,
ili njegova farmaceutski prihvatljiva sol.
3. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je:
[image]
,
ili njegova farmaceutski prihvatljiva sol.
4. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je:
[image]
,
ili njegova farmaceutski prihvatljiva sol.
5. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što je:
[image]
,
ili njegova farmaceutski prihvatljiva sol.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što n je 0, R1 je -C1-4 alkil, a R2 je -CH3, ili njegova farmaceutski prihvatljiva sol.
7. Spoj u skladu s patentnim zahtjevom 6, naznačen time što je R1 izopropil, ili njegova farmaceutski prihvatljiva sol.
8. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
ili njegova farmaceutski prihvatljiva sol.
9. Spoj u skladu s bilo kojim od patentnih zahtjeva 1, 2, 6 ili 7, naznačen time što je:
[image]
,
ili njegova farmaceutski prihvatljiva sol.
10. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 9, naznačen time što je 5-[5-[(1S,2R)-2-izopropilciklopropil]-6-metilpiridazin-3-il]-1H-pirimidin-2,4-dion, ili njegova farmaceutski prihvatljiva sol.
11. Spoj u skladu s bilo kojim od patentnih zahtjeva 1, 2 ili 6, naznačen time što je:
[image]
,
ili njegova farmaceutski prihvatljiva sol.
12. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 6, 8 ili 11, naznačen time što je 5-[5-[(1S,2S)-2-etilciklopropil]-6-metilpiridazin-3-il]-1H-pirimidin-2,4-dion, ili njegova farmaceutski prihvatljiva sol.
13. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 12, ili njegovu farmaceutski prihvatljivu sol, i jedan ili više farmaceutski prihvatljivih nosača, razrjeđivača ili pomoćnih sredstava.
14. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 12, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u terapiji.
15. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 12, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u liječenju raka.
16. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 15, naznačen time što je rak rak mokraćnog mjehura, rak dojke, kolangiokarcinom, kolorektalni rak, rak debelog crijeva, rak želuca, mokraćnog žučng mjehura, glioblastom, rak glave i vrata, rak jetre, rak pluća, limfom, meduloblastom, melanom, rak jajnika, rak gušterače, rak prostate ili rak bubrega.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862636978P | 2018-03-01 | 2018-03-01 | |
| US201862775553P | 2018-12-05 | 2018-12-05 | |
| PCT/US2019/019074 WO2019168744A1 (en) | 2018-03-01 | 2019-02-22 | Cd73 inhibitors |
| EP19709335.4A EP3759096B1 (en) | 2018-03-01 | 2019-02-22 | Cd73 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20220459T1 true HRP20220459T1 (hr) | 2022-05-27 |
Family
ID=65686120
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20220459TT HRP20220459T1 (hr) | 2018-03-01 | 2019-02-22 | Inhibitori cd73 |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US11028074B2 (hr) |
| EP (1) | EP3759096B1 (hr) |
| JP (1) | JP6794560B2 (hr) |
| KR (1) | KR20200116965A (hr) |
| CN (1) | CN111819173B (hr) |
| AU (1) | AU2019228473B2 (hr) |
| BR (1) | BR112020016066A2 (hr) |
| CA (1) | CA3092661C (hr) |
| CL (1) | CL2020002158A1 (hr) |
| CO (1) | CO2020010191A2 (hr) |
| CR (1) | CR20200376A (hr) |
| CY (1) | CY1125145T1 (hr) |
| DK (1) | DK3759096T3 (hr) |
| DO (1) | DOP2020000148A (hr) |
| EC (1) | ECSP20052897A (hr) |
| ES (1) | ES2909701T3 (hr) |
| HR (1) | HRP20220459T1 (hr) |
| IL (1) | IL277006B2 (hr) |
| JO (1) | JOP20200209A1 (hr) |
| LT (1) | LT3759096T (hr) |
| MA (1) | MA52413A (hr) |
| MX (1) | MX2020009115A (hr) |
| PE (1) | PE20210177A1 (hr) |
| PH (1) | PH12020551464A1 (hr) |
| PL (1) | PL3759096T3 (hr) |
| PT (1) | PT3759096T (hr) |
| RS (1) | RS63073B1 (hr) |
| SG (1) | SG11202008366RA (hr) |
| SI (1) | SI3759096T1 (hr) |
| TW (1) | TWI702954B (hr) |
| UA (1) | UA123890C2 (hr) |
| WO (1) | WO2019168744A1 (hr) |
| ZA (1) | ZA202004805B (hr) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114502548A (zh) * | 2019-08-29 | 2022-05-13 | 伊莱利利公司 | Cd73抑制剂的结晶形式 |
| US20210198239A1 (en) * | 2019-12-06 | 2021-07-01 | Plexxikon Inc. | Compounds and methods for cd73 modulation and indications therefor |
| AU2021261383A1 (en) * | 2020-04-23 | 2022-11-17 | Opna Bio SA | Compounds and methods for CD73 modulation and indications therefor |
| WO2021222522A1 (en) * | 2020-05-01 | 2021-11-04 | Gilead Sciences, Inc. | Cd73 inhibiting 2,4-dioxopyrimidine compounds |
| WO2022007677A1 (zh) * | 2020-07-07 | 2022-01-13 | 贝达药业股份有限公司 | Cd73抑制剂及其在医药上的应用 |
| AU2021341258A1 (en) | 2020-09-08 | 2023-04-13 | Betta Pharmaceuticals Co., Ltd. | CD73 inhibitor and application thereof in medicine |
| WO2022068929A1 (zh) * | 2020-09-30 | 2022-04-07 | 武汉人福创新药物研发中心有限公司 | 嘧啶二酮类化合物及其用途 |
| WO2022090711A1 (en) | 2020-10-26 | 2022-05-05 | AdoRx Therapeutics Limited | Compounds as cd73 inhibitors |
| CA3197340A1 (en) | 2020-11-05 | 2022-05-12 | Xuejun Zhang | Cd73 inhibitor and use thereof |
| CN114437038A (zh) * | 2020-11-05 | 2022-05-06 | 武汉人福创新药物研发中心有限公司 | 哒嗪炔烃类化合物及其用途 |
| CN116134029A (zh) * | 2020-12-10 | 2023-05-16 | 上海翰森生物医药科技有限公司 | 氧代氮环类衍生物调节剂、其制备方法和应用 |
| WO2022195499A1 (en) * | 2021-03-19 | 2022-09-22 | Aurigene Discovery Technologies Limited | Substituted pyridazine compounds as cd73 inhibitors |
| AU2022376954A1 (en) | 2021-10-29 | 2024-05-02 | Gilead Sciences, Inc. | Cd73 compounds |
| WO2023169327A1 (zh) * | 2022-03-07 | 2023-09-14 | 贝达药业股份有限公司 | 一种哒嗪类衍生物的晶型、制备方法及其应用 |
| WO2023201267A1 (en) | 2022-04-13 | 2023-10-19 | Gilead Sciences, Inc. | Combination therapy for treating trop-2 expressing cancers |
| WO2024006929A1 (en) * | 2022-07-01 | 2024-01-04 | Gilead Sciences, Inc. | Cd73 compounds |
| WO2024013206A1 (en) * | 2022-07-14 | 2024-01-18 | F. Hoffmann-La Roche Ag | Heterocycle compounds for the treatment of cancer |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0709660A2 (pt) | 2006-04-03 | 2011-07-19 | Glaxo Group Limided | derivados de azabiciclo [3,1,0] hexila como moduladores dos receptores de dopamina d3 |
| EP1860113A1 (en) | 2006-05-24 | 2007-11-28 | Rheinische Friedrich-Wilhelms-Universität Bonn | Ectonucleotidase inhibitors |
| AR105654A1 (es) | 2015-08-24 | 2017-10-25 | Lilly Co Eli | Anticuerpos pd-l1 (ligando 1 de muerte celular programada) |
| FI3399984T3 (fi) * | 2016-01-08 | 2023-11-10 | Arcus Biosciences Inc | Ekto-5'-nukleotidaasin modulaattoreita ja niiden käyttö |
| WO2017153952A1 (en) | 2016-03-10 | 2017-09-14 | Glaxosmithkline Intellectual Property Development Limited | 5-sulfamoyl-2-hydroxybenzamide derivatives |
-
2019
- 2019-02-15 TW TW108105130A patent/TWI702954B/zh active
- 2019-02-22 CR CR20200376A patent/CR20200376A/es unknown
- 2019-02-22 PE PE2020001302A patent/PE20210177A1/es unknown
- 2019-02-22 WO PCT/US2019/019074 patent/WO2019168744A1/en active Application Filing
- 2019-02-22 AU AU2019228473A patent/AU2019228473B2/en active Active
- 2019-02-22 PL PL19709335T patent/PL3759096T3/pl unknown
- 2019-02-22 JO JOP/2020/0209A patent/JOP20200209A1/ar unknown
- 2019-02-22 CN CN201980016287.8A patent/CN111819173B/zh active Active
- 2019-02-22 SI SI201930184T patent/SI3759096T1/sl unknown
- 2019-02-22 EP EP19709335.4A patent/EP3759096B1/en active Active
- 2019-02-22 SG SG11202008366RA patent/SG11202008366RA/en unknown
- 2019-02-22 ES ES19709335T patent/ES2909701T3/es active Active
- 2019-02-22 RS RS20220310A patent/RS63073B1/sr unknown
- 2019-02-22 LT LTEPPCT/US2019/019074T patent/LT3759096T/lt unknown
- 2019-02-22 PT PT197093354T patent/PT3759096T/pt unknown
- 2019-02-22 MX MX2020009115A patent/MX2020009115A/es unknown
- 2019-02-22 KR KR1020207025071A patent/KR20200116965A/ko active IP Right Grant
- 2019-02-22 CA CA3092661A patent/CA3092661C/en active Active
- 2019-02-22 MA MA052413A patent/MA52413A/fr unknown
- 2019-02-22 UA UAA202005110A patent/UA123890C2/uk unknown
- 2019-02-22 DK DK19709335.4T patent/DK3759096T3/da active
- 2019-02-22 JP JP2019557361A patent/JP6794560B2/ja active Active
- 2019-02-22 BR BR112020016066-0A patent/BR112020016066A2/pt not_active IP Right Cessation
- 2019-02-22 HR HRP20220459TT patent/HRP20220459T1/hr unknown
- 2019-02-22 US US16/481,146 patent/US11028074B2/en active Active
- 2019-02-22 IL IL277006A patent/IL277006B2/en unknown
-
2020
- 2020-07-28 DO DO2020000148A patent/DOP2020000148A/es unknown
- 2020-08-03 ZA ZA2020/04805A patent/ZA202004805B/en unknown
- 2020-08-19 CO CONC2020/0010191A patent/CO2020010191A2/es unknown
- 2020-08-21 CL CL2020002158A patent/CL2020002158A1/es unknown
- 2020-08-31 EC ECSENADI202052897A patent/ECSP20052897A/es unknown
- 2020-09-01 PH PH12020551464A patent/PH12020551464A1/en unknown
-
2022
- 2022-04-12 CY CY20221100276T patent/CY1125145T1/el unknown
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