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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| 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 |
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| 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 |
| WO2025024265A1 (en) | 2023-07-21 | 2025-01-30 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad4 modulators |
| 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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| 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 |
| 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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| CN109071497B (zh) | 2021-10-22 |
| KR20180110160A (ko) | 2018-10-08 |
| TW201825476A (zh) | 2018-07-16 |
| CA3015482A1 (en) | 2017-08-31 |
| AU2017223416A1 (en) | 2018-10-11 |
| IL261167A (en) | 2018-10-31 |
| EA201891910A1 (ru) | 2019-02-28 |
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