JPWO2020033488A5 - - Google Patents
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- Publication number
- JPWO2020033488A5 JPWO2020033488A5 JP2021506621A JP2021506621A JPWO2020033488A5 JP WO2020033488 A5 JPWO2020033488 A5 JP WO2020033488A5 JP 2021506621 A JP2021506621 A JP 2021506621A JP 2021506621 A JP2021506621 A JP 2021506621A JP WO2020033488 A5 JPWO2020033488 A5 JP WO2020033488A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- independently selected
- heterocyclyl
- alkynyl
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 133
- 229910052739 hydrogen Inorganic materials 0.000 claims 66
- 229910052799 carbon Inorganic materials 0.000 claims 54
- 125000000623 heterocyclic group Chemical group 0.000 claims 52
- 229910052731 fluorine Inorganic materials 0.000 claims 44
- 229910052801 chlorine Inorganic materials 0.000 claims 42
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 35
- 229910052794 bromium Inorganic materials 0.000 claims 35
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 34
- 150000003839 salts Chemical class 0.000 claims 21
- 125000004452 carbocyclyl group Chemical group 0.000 claims 20
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 17
- 229910052757 nitrogen Inorganic materials 0.000 claims 17
- -1 NR 6 Inorganic materials 0.000 claims 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 13
- 125000003118 aryl group Chemical group 0.000 claims 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 12
- 125000000304 alkynyl group Chemical group 0.000 claims 9
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 101100406797 Arabidopsis thaliana PAD4 gene Proteins 0.000 claims 3
- 101150094373 Padi4 gene Proteins 0.000 claims 3
- 102100035731 Protein-arginine deiminase type-4 Human genes 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 208000004921 cutaneous lupus erythematosus Diseases 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862715858P | 2018-08-08 | 2018-08-08 | |
| US62/715,858 | 2018-08-08 | ||
| PCT/US2019/045424 WO2020033488A1 (en) | 2018-08-08 | 2019-08-07 | Substituted benzimidazoles as pad4 inhibitors |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021534097A JP2021534097A (ja) | 2021-12-09 |
| JP2021534097A5 JP2021534097A5 (https=) | 2022-08-08 |
| JPWO2020033488A5 true JPWO2020033488A5 (https=) | 2022-08-08 |
| JP7483678B2 JP7483678B2 (ja) | 2024-05-15 |
Family
ID=67766299
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021506621A Active JP7483678B2 (ja) | 2018-08-08 | 2019-08-07 | Ｐａｄ４阻害剤としての置換ベンズイミダゾール |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US20220402950A1 (https=) |
| EP (1) | EP3833438B1 (https=) |
| JP (1) | JP7483678B2 (https=) |
| KR (1) | KR102825194B1 (https=) |
| CN (1) | CN112805066A (https=) |
| AU (1) | AU2019318415A1 (https=) |
| BR (1) | BR112021002089A2 (https=) |
| CA (1) | CA3108871A1 (https=) |
| CL (1) | CL2021000292A1 (https=) |
| CO (1) | CO2021001219A2 (https=) |
| EA (1) | EA202190464A1 (https=) |
| ES (1) | ES2973714T3 (https=) |
| IL (1) | IL280641A (https=) |
| MX (1) | MX2021001471A (https=) |
| PE (1) | PE20211067A1 (https=) |
| SG (1) | SG11202101176YA (https=) |
| TW (1) | TW202019411A (https=) |
| WO (1) | WO2020033488A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3833671B1 (en) * | 2018-08-08 | 2022-08-24 | Bristol-Myers Squibb Company | Substituted thienopyrroles as pad4 inhibitors |
| AU2019319835A1 (en) | 2018-08-08 | 2021-03-25 | Bristol-Myers Squibb Company | Indole and azaindole inhibitors of PAD enzymes |
| EP4100405A1 (en) | 2020-02-06 | 2022-12-14 | Bristol-Myers Squibb Company | Macrocyclic pad4 inhibitors useful as immunosuppressant |
| TW202140477A (zh) | 2020-02-12 | 2021-11-01 | 美商必治妥美雅史谷比公司 | 雜環ｐａｄ４抑制劑 |
| EP4143189A1 (en) | 2020-04-30 | 2023-03-08 | Gilead Sciences, Inc. | Macrocyclic inhibitors of peptidylarginine deiminases |
| TW202241884A (zh) | 2020-12-22 | 2022-11-01 | 美商基利科學股份有限公司 | 肽基精胺酸去亞胺酶之抑制劑 |
| WO2022140428A2 (en) | 2020-12-22 | 2022-06-30 | Gilead Sciences, Inc. | Inhibitors of peptidylarginine deiminases |
| CN116492462B (zh) * | 2023-02-03 | 2023-09-22 | 山东第一医科大学附属眼科医院(山东省眼科医院) | Pad4抑制剂在防治角膜移植术后免疫排斥反应中的应用 |
| WO2025024265A1 (en) | 2023-07-21 | 2025-01-30 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad4 modulators |
| WO2026020127A2 (en) | 2024-07-19 | 2026-01-22 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad2 modulators |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS55684B1 (sr) * | 2012-07-26 | 2017-07-31 | Glaxo Group Ltd | 2-(azaindol-2-il)benzimidazoli kao pad4 inhibitori |
| US10407407B2 (en) * | 2015-05-21 | 2019-09-10 | Glaxosmithkline Intellectual Property Development Limited | Benzoimidazole derivatives as PAD4 inhibitors |
| AR107032A1 (es) | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores bicíclicos de pad4 |
| AR107030A1 (es) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores aza-bencimidazol de pad4 |
| KR102398941B1 (ko) * | 2016-07-27 | 2022-05-17 | 패들락 테라퓨틱스, 인코포레이티드 | Pad4의 공유결합성 억제제 |
-
2019
- 2019-08-07 WO PCT/US2019/045424 patent/WO2020033488A1/en not_active Ceased
- 2019-08-07 JP JP2021506621A patent/JP7483678B2/ja active Active
- 2019-08-07 EP EP19759133.2A patent/EP3833438B1/en active Active
- 2019-08-07 TW TW108128157A patent/TW202019411A/zh unknown
- 2019-08-07 PE PE2021000170A patent/PE20211067A1/es unknown
- 2019-08-07 BR BR112021002089-6A patent/BR112021002089A2/pt not_active Application Discontinuation
- 2019-08-07 KR KR1020217006450A patent/KR102825194B1/ko active Active
- 2019-08-07 CN CN201980064958.8A patent/CN112805066A/zh active Pending
- 2019-08-07 EA EA202190464A patent/EA202190464A1/ru unknown
- 2019-08-07 US US17/265,844 patent/US20220402950A1/en active Pending
- 2019-08-07 CA CA3108871A patent/CA3108871A1/en active Pending
- 2019-08-07 SG SG11202101176YA patent/SG11202101176YA/en unknown
- 2019-08-07 MX MX2021001471A patent/MX2021001471A/es unknown
- 2019-08-07 AU AU2019318415A patent/AU2019318415A1/en not_active Abandoned
- 2019-08-07 ES ES19759133T patent/ES2973714T3/es active Active
-
2021
- 2021-02-03 CL CL2021000292A patent/CL2021000292A1/es unknown
- 2021-02-03 CO CONC2021/0001219A patent/CO2021001219A2/es unknown
- 2021-02-04 IL IL280641A patent/IL280641A/en unknown