JP6926126B2 - Pad4のヘテロアリール阻害剤 - Google Patents
Pad4のヘテロアリール阻害剤 Download PDFInfo
- Publication number
- JP6926126B2 JP6926126B2 JP2018563393A JP2018563393A JP6926126B2 JP 6926126 B2 JP6926126 B2 JP 6926126B2 JP 2018563393 A JP2018563393 A JP 2018563393A JP 2018563393 A JP2018563393 A JP 2018563393A JP 6926126 B2 JP6926126 B2 JP 6926126B2
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- Prior art keywords
- methyl
- disease
- mmol
- ring
- pharmaceutically acceptable
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- 0 CCCC(C)(CCCC(CCC1)C(*(**)C2=C)=*C2=CC(C(C2CCCCCCC2)=O)=C**)CCC1(C)C(C)(C)* Chemical compound CCCC(C)(CCCC(CCC1)C(*(**)C2=C)=*C2=CC(C(C2CCCCCCC2)=O)=C**)CCC1(C)C(C)(C)* 0.000 description 22
- BPXLYRFJPLNLSI-UHFFFAOYSA-N CN(C1)CC11OCCNC1 Chemical compound CN(C1)CC11OCCNC1 BPXLYRFJPLNLSI-UHFFFAOYSA-N 0.000 description 2
- IGONQKDBVGZQKD-UHFFFAOYSA-N CN(CC1CC2)C2C1N Chemical compound CN(CC1CC2)C2C1N IGONQKDBVGZQKD-UHFFFAOYSA-N 0.000 description 2
- YRXAYAXARURDCO-UHFFFAOYSA-N CN(CC1CC2)C2C1NCc1ccccc1 Chemical compound CN(CC1CC2)C2C1NCc1ccccc1 YRXAYAXARURDCO-UHFFFAOYSA-N 0.000 description 2
- YYCQWPUGLXCXGU-UHFFFAOYSA-N CN1CC2NCCOC2CC1 Chemical compound CN1CC2NCCOC2CC1 YYCQWPUGLXCXGU-UHFFFAOYSA-N 0.000 description 2
- SLPIUOQCDAFBAG-UHFFFAOYSA-N NC1C(CC2)NCC2C1 Chemical compound NC1C(CC2)NCC2C1 SLPIUOQCDAFBAG-UHFFFAOYSA-N 0.000 description 2
- IUTWKWRTLRWYRA-UHFFFAOYSA-N CC(C)N1CC2NCCC2CC1 Chemical compound CC(C)N1CC2NCCC2CC1 IUTWKWRTLRWYRA-UHFFFAOYSA-N 0.000 description 1
- UCWAUSRHBDLEGE-UHFFFAOYSA-N CN(C1)CC11CNCCC1 Chemical compound CN(C1)CC11CNCCC1 UCWAUSRHBDLEGE-UHFFFAOYSA-N 0.000 description 1
- YSHLVNOVNXNSQS-UHFFFAOYSA-N CN(CC(C1)N)CC1F Chemical compound CN(CC(C1)N)CC1F YSHLVNOVNXNSQS-UHFFFAOYSA-N 0.000 description 1
- QZSACHHNFDNCNB-UHFFFAOYSA-N CN(CCC1)CC1N Chemical compound CN(CCC1)CC1N QZSACHHNFDNCNB-UHFFFAOYSA-N 0.000 description 1
- HLQIJIWWHUNNMY-UHFFFAOYSA-N CN(CCC1F)CC1N Chemical compound CN(CCC1F)CC1N HLQIJIWWHUNNMY-UHFFFAOYSA-N 0.000 description 1
- HPBHVEBWKQHAAJ-JXMHAVLCSA-N CN([C@@H](C1)C11CC2)[C@H]2[C@@H]1N Chemical compound CN([C@@H](C1)C11CC2)[C@H]2[C@@H]1N HPBHVEBWKQHAAJ-JXMHAVLCSA-N 0.000 description 1
- ATGFVZVPFZBMDU-YCASGBEESA-N C[n]1c(-c(cc2)c(CC3CC3)nc2C#N)nc2cc(C(N(C[C@H]3CC4)[C@H]4[C@@H]3N)=O)cc(OC)c12 Chemical compound C[n]1c(-c(cc2)c(CC3CC3)nc2C#N)nc2cc(C(N(C[C@H]3CC4)[C@H]4[C@@H]3N)=O)cc(OC)c12 ATGFVZVPFZBMDU-YCASGBEESA-N 0.000 description 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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- A61K31/395—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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- A61K31/4353—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 |
| RS65576B1 (sr) | 2017-11-24 | 2024-06-28 | Jubilant Episcribe Llc | Heterociklična jedinjenja kao inhibitori prmt5 |
| WO2019122202A1 (en) * | 2017-12-20 | 2019-06-27 | Ecole Polytechnique Federale De Lausanne (Epfl) | Sting inhibitors |
| CN112105610B (zh) | 2018-03-13 | 2024-01-26 | 朱比连特普罗德尔有限责任公司 | 作为pd1/pd-l1相互作用/活化的抑制剂的双环化合物 |
| 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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| 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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| RU2611010C2 (ru) | 2012-07-26 | 2017-02-17 | Глаксо Груп Лимитед | 2-(Азаиндол-2-ил)бензимидазолы в качестве ингибиторов PAD4 |
| WO2016185279A1 (en) * | 2015-05-21 | 2016-11-24 | Glaxosmithkline Intellectual Property Development Limited | Benzoimidazole derivatives as pad4 inhibitors |
| AR107030A1 (es) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores aza-bencimidazol de pad4 |
| AR107032A1 (es) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores bicíclicos de pad4 |
| SG11201807021UA (en) | 2016-02-23 | 2018-09-27 | Padlock Therapeutics Inc | Heteroaryl inhibitors of pad4 |
| 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 |
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| EP3419969A1 (en) | 2019-01-02 |
| BR112018016433A2 (pt) | 2018-12-26 |
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