AR107694A1 - Heteroarilos inhibidores de pad4 - Google Patents
Heteroarilos inhibidores de pad4Info
- Publication number
- AR107694A1 AR107694A1 ARP170100442A ARP170100442A AR107694A1 AR 107694 A1 AR107694 A1 AR 107694A1 AR P170100442 A ARP170100442 A AR P170100442A AR P170100442 A ARP170100442 A AR P170100442A AR 107694 A1 AR107694 A1 AR 107694A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- fluorine
- ring
- aliphatic
- groups
- Prior art date
Links
- 101100406797 Arabidopsis thaliana PAD4 gene Proteins 0.000 title abstract 2
- 101150094373 Padi4 gene Proteins 0.000 title abstract 2
- 102100035731 Protein-arginine deiminase type-4 Human genes 0.000 title abstract 2
- 230000002401 inhibitory effect Effects 0.000 title 1
- 125000001931 aliphatic group Chemical group 0.000 abstract 5
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 4
- 229910052731 fluorine Inorganic materials 0.000 abstract 4
- 239000011737 fluorine Substances 0.000 abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000001153 fluoro group Chemical group F* 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 239000001301 oxygen Chemical group 0.000 abstract 3
- 229910052717 sulfur Chemical group 0.000 abstract 3
- 239000011593 sulfur Chemical group 0.000 abstract 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 229940122298 Peptidyl arginine deiminase IV inhibitor Drugs 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229930195734 saturated hydrocarbon Natural products 0.000 abstract 1
- 229930195735 unsaturated hydrocarbon Natural products 0.000 abstract 1
Classifications
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- 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
- C07D401/14—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 three or more hetero rings
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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| US10703741B2 (en) | 2016-07-27 | 2020-07-07 | Padlock Therapeutics, Inc. | Covalent inhibitors of PAD4 |
| KR102502992B1 (ko) | 2016-09-12 | 2023-02-24 | 패들락 테라퓨틱스, 인코포레이티드 | Pad4의 헤테로아릴 억제제 |
| JP7504349B2 (ja) * | 2017-09-19 | 2024-06-24 | 三菱瓦斯化学株式会社 | 半導体リソグラフィー膜形成組成物、並びにレジストパターン形成方法及びデバイス |
| RU2764243C2 (ru) | 2017-09-22 | 2022-01-14 | ДЖУБИЛАНТ ЭПИПЭД ЭлЭлСи | Гетероциклические соединения в качестве ингибиторов PAD |
| CN111225915B (zh) | 2017-10-18 | 2023-03-07 | 朱比兰特埃皮帕德有限公司 | 作为pad抑制剂的咪唑并吡啶化合物 |
| US11629135B2 (en) | 2017-11-06 | 2023-04-18 | Jubilant Prodell Llc | Pyrimidine derivatives as inhibitors of PD1/PD-L1 activation |
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| ES2929200T3 (es) * | 2018-08-08 | 2022-11-25 | Bristol Myers Squibb Co | Tienopirroles sustituidos como inhibidores de PAD4 |
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| EP3833440A1 (en) | 2018-08-08 | 2021-06-16 | Bristol-Myers Squibb Company | Indole and azaindole inhibitors of pad enzymes |
| JP7345220B2 (ja) * | 2019-08-30 | 2023-09-15 | ティーエスディー ライフ サイエンス カンパニー リミテッド | イミダゾピリジン誘導体及びこれを有効成分として含有する薬学的組成物 |
| TW202115083A (zh) * | 2019-09-27 | 2021-04-16 | 大陸商南京藥捷安康生物科技有限公司 | 肽醯精胺酸脫亞胺酶抑制劑及其用途 |
| WO2021138540A1 (en) | 2020-01-03 | 2021-07-08 | Berg Llc | Polycyclic amides as ube2k modulators for treating cancer |
| CN115298175B (zh) | 2020-02-06 | 2024-05-07 | 百时美施贵宝公司 | 可用作免疫抑制剂的大环pad4抑制剂 |
| CN113248507A (zh) * | 2020-02-09 | 2021-08-13 | 上海茂晟康慧科技有限公司 | 瑞德西韦关键中间体7-卤代吡咯并[1,2-f][1,2,4]三嗪-4-胺的合成方法 |
| 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 |
| MX2022013615A (es) | 2020-04-30 | 2022-11-16 | Gilead Sciences Inc | Inhibidores de macrociclo de peptidilarginina deiminasas. |
| CN112618546B (zh) * | 2020-12-22 | 2022-03-01 | 陈昊 | Pad4抑制剂在制备放射治疗增敏药物方面的应用 |
| EP4267562A1 (en) | 2020-12-22 | 2023-11-01 | Gilead Sciences, Inc. | Inhibitors of peptidylarginine deiminases |
| TW202233174A (zh) | 2020-12-22 | 2022-09-01 | 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 |
| KR20220122879A (ko) * | 2021-02-26 | 2022-09-05 | 주식회사 티에스디라이프사이언스 | 이미다조피리딘 유도체 및 이를 유효성분으로 함유하는 약학적 조성물 |
| KR20260011143A (ko) | 2023-04-18 | 2026-01-22 | 칼리오페, 인크. | Nk3 조정제 및 이의 용도 |
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