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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| JP6926126B2 (ja) | 2016-02-23 | 2021-08-25 | パドロック・セラピューティクス・インコーポレイテッドPadlock Therapeutics, Inc. | Pad4のヘテロアリール阻害剤 |
| KR102398941B1 (ko) | 2016-07-27 | 2022-05-17 | 패들락 테라퓨틱스, 인코포레이티드 | Pad4의 공유결합성 억제제 |
| JP7118951B2 (ja) | 2016-09-12 | 2022-08-16 | パドロック・セラピューティクス・インコーポレイテッド | Pad4のヘテロアリール阻害剤 |
| WO2019059202A1 (ja) * | 2017-09-19 | 2019-03-28 | 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 |
| MX2020003242A (es) | 2017-09-22 | 2020-09-18 | Jubilant Epipad LLC | Compuestos heterociclicos como inhibidores de pad. |
| AU2018352142B2 (en) | 2017-10-18 | 2022-08-25 | Jubilant Epipad LLC | Imidazo-pyridine compounds as PAD inhibitors |
| KR20200085836A (ko) | 2017-11-06 | 2020-07-15 | 주빌런트 프로델 엘엘씨 | Pd1/pd-l1 활성화 억제제로서의 피리미딘 유도체 |
| BR112020010322A2 (pt) | 2017-11-24 | 2020-11-17 | Jubilant Episcribe Llc | composto da fórmula i; composto da fórmula ia; composto da fórmula ib; processo de preparação de compostos da fórmula i; composição farmacêutica; método para o tratamento e/ou prevenção de várias doenças; uso dos compostos; método para o tratamento de câncer; e método para o tratamento e/ou prevenção de uma afecção mediada por prmt5 ou um distúrbio proliferativo ou câncer |
| WO2019122202A1 (en) * | 2017-12-20 | 2019-06-27 | Ecole Polytechnique Federale De Lausanne (Epfl) | Sting inhibitors |
| SG11202008950PA (en) | 2018-03-13 | 2020-10-29 | Jubilant Prodel LLC | Bicyclic compounds as inhibitors of pd1/pd-l1 interaction/activation |
| 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 |
| CN112789087B (zh) * | 2018-08-08 | 2024-08-13 | 百时美施贵宝公司 | Pad酶的苯并咪唑抑制剂 |
| AU2020337720B2 (en) * | 2019-08-30 | 2024-02-15 | Tsd Life Sciences Co., Ltd. | Imidazopyridine derivative and pharmaceutical composition comprising same as active ingredient |
| 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 |
| CA3166630A1 (en) | 2020-01-03 | 2021-07-08 | Berg Llc | Polycyclic amides as ube2k modulators for treating cancer |
| EP4100405A1 (en) | 2020-02-06 | 2022-12-14 | Bristol-Myers Squibb Company | Macrocyclic pad4 inhibitors useful as immunosuppressant |
| 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 |
| EP4143189A1 (en) * | 2020-04-30 | 2023-03-08 | Gilead Sciences, Inc. | Macrocyclic inhibitors of peptidylarginine deiminases |
| 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 |
| 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 |
| KR20220122879A (ko) * | 2021-02-26 | 2022-09-05 | 주식회사 티에스디라이프사이언스 | 이미다조피리딘 유도체 및 이를 유효성분으로 함유하는 약학적 조성물 |
| CN121399122A (zh) | 2023-04-18 | 2026-01-23 | 卡尔优普公司 | Nk3调节剂及其用途 |
| WO2025006962A1 (en) | 2023-06-30 | 2025-01-02 | Bristol-Myers Squibb Company | Kras inhibitors |
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| WO2025080781A1 (en) * | 2023-10-12 | 2025-04-17 | Kallyope, Inc. | Nk3 modulators and uses thereof |
| WO2026020127A2 (en) | 2024-07-19 | 2026-01-22 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad2 modulators |
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| 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 |
| JP6926126B2 (ja) | 2016-02-23 | 2021-08-25 | パドロック・セラピューティクス・インコーポレイテッドPadlock Therapeutics, Inc. | Pad4のヘテロアリール阻害剤 |
| KR102398941B1 (ko) * | 2016-07-27 | 2022-05-17 | 패들락 테라퓨틱스, 인코포레이티드 | Pad4의 공유결합성 억제제 |
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| KR20180110160A (ko) | 2018-10-08 |
| TW201825476A (zh) | 2018-07-16 |
| CA3015482A1 (en) | 2017-08-31 |
| JP6926126B2 (ja) | 2021-08-25 |
| AU2017223416A1 (en) | 2018-10-11 |
| IL261167A (en) | 2018-10-31 |
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