JP6987843B2 - Pad4の共有結合性阻害剤 - Google Patents
Pad4の共有結合性阻害剤 Download PDFInfo
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- JP6987843B2 JP6987843B2 JP2019504110A JP2019504110A JP6987843B2 JP 6987843 B2 JP6987843 B2 JP 6987843B2 JP 2019504110 A JP2019504110 A JP 2019504110A JP 2019504110 A JP2019504110 A JP 2019504110A JP 6987843 B2 JP6987843 B2 JP 6987843B2
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- Prior art keywords
- disease
- methyl
- pharmaceutically acceptable
- cyclopropylmethyl
- pyrrolo
- Prior art date
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- 0 ***(C(C1=CC(C=CC*2)=C2*1*)=*1)c(c(*)c2)c1cc2C(N)=O Chemical compound ***(C(C1=CC(C=CC*2)=C2*1*)=*1)c(c(*)c2)c1cc2C(N)=O 0.000 description 7
- RHRTXOZMOPKTHO-CVYTVXJSSA-N CCC(C)CC(CC)[C@H](C)CC(/C=C\CNC)=C Chemical compound CCC(C)CC(CC)[C@H](C)CC(/C=C\CNC)=C RHRTXOZMOPKTHO-CVYTVXJSSA-N 0.000 description 1
- AUMOTOMONTWPED-FNQBFKTISA-N CCCC[C@@H](CCC)C[IH]C(C(C)CC(C)C)C1=N[C@@H](C)C(CCCOCN(C[C@@H]23)CC2C3NC)N1C Chemical compound CCCC[C@@H](CCC)C[IH]C(C(C)CC(C)C)C1=N[C@@H](C)C(CCCOCN(C[C@@H]23)CC2C3NC)N1C AUMOTOMONTWPED-FNQBFKTISA-N 0.000 description 1
- ZGLMYLGLRULPPR-PWNYCUMCSA-N I[C@H]1[C@@H](N2)[I]2NC1 Chemical compound I[C@H]1[C@@H](N2)[I]2NC1 ZGLMYLGLRULPPR-PWNYCUMCSA-N 0.000 description 1
- OVASYMCRZHEQMU-IKNVJDIESA-N O[C@@H]1[C@H]2NC[C@@H]3[C@H]2C1C3 Chemical compound O[C@@H]1[C@H]2NC[C@@H]3[C@H]2C1C3 OVASYMCRZHEQMU-IKNVJDIESA-N 0.000 description 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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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- A61K31/437—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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- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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| PCT/US2017/044194 WO2018022897A1 (en) | 2016-07-27 | 2017-07-27 | Covalent inhibitors of pad4 |
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| EP3419969B1 (en) | 2016-02-23 | 2019-12-18 | Padlock Therapeutics, Inc. | Heteroaryl inhibitors of pad4 |
| CN110248934B (zh) | 2016-09-12 | 2022-05-24 | 帕德罗科治疗公司 | 杂芳基pad4抑制剂 |
| KR20210042933A (ko) * | 2018-08-08 | 2021-04-20 | 브리스톨-마이어스 스큅 컴퍼니 | Pad 효소의 벤즈이미다졸 억제제 |
| CN112566916B (zh) | 2018-08-08 | 2023-10-20 | 百时美施贵宝公司 | 作为pad4抑制剂的经取代的噻吩并吡咯 |
| EP3833440A1 (en) | 2018-08-08 | 2021-06-16 | Bristol-Myers Squibb Company | Indole and azaindole inhibitors of pad enzymes |
| MX2021001471A (es) * | 2018-08-08 | 2021-04-28 | Bristol Myers Squibb Co | Benzimidazoles sustituidos como inhibidores de peptidil arginina deiminasa 4 (pad4). |
| WO2020085493A1 (ja) | 2018-10-26 | 2020-04-30 | 大鵬薬品工業株式会社 | 新規なインダゾール化合物又はその塩 |
| UA129778C2 (uk) | 2019-10-28 | 2025-07-30 | Мерк Шарп Енд Доум Елелсі | Низькомолекулярні інгібітори g12c-мутантного kras |
| WO2021084765A1 (en) * | 2019-10-31 | 2021-05-06 | Taiho Pharmaceutical Co., Ltd | 4-aminobut-2-enamide derivatives and salts thereof |
| WO2021102361A1 (en) * | 2019-11-22 | 2021-05-27 | The Regents Of The University Of California | Caspase 6 inhibitors and uses thereof |
| US12479834B2 (en) | 2019-11-29 | 2025-11-25 | Taiho Pharmaceutical Co., Ltd. | Phenol compound or salt thereof |
| WO2021158840A1 (en) * | 2020-02-06 | 2021-08-12 | 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 |
| PE20230488A1 (es) | 2020-04-30 | 2023-03-21 | Gilead Sciences Inc | Inhibidores macrociclicos de las peptidilarginina deiminasas |
| US12240862B2 (en) | 2020-12-22 | 2025-03-04 | Gilead Sciences, Inc. | Inhibitors of peptidylarginine deiminases |
| EP4267562A1 (en) | 2020-12-22 | 2023-11-01 | Gilead Sciences, Inc. | Inhibitors of peptidylarginine deiminases |
| EP4329750A4 (en) * | 2021-04-27 | 2025-06-18 | Merck Sharp & Dohme LLC | Small-molecule inhibitors of the KRAS G12C mutant |
| CN119604287A (zh) * | 2022-05-26 | 2025-03-11 | 细胞基因公司 | 杂环pad4抑制剂 |
| WO2025024265A1 (en) | 2023-07-21 | 2025-01-30 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad4 modulators |
| TW202535891A (zh) | 2023-10-20 | 2025-09-16 | 美商默沙東有限責任公司 | Kras蛋白之小分子抑制劑 |
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| AU778689B2 (en) | 2000-02-09 | 2004-12-16 | Akzo Nobel N.V. | Pulping process |
| CA2555199A1 (en) * | 2004-02-04 | 2005-08-18 | Yokohama City University | Peptidylarginine deiminase 4 inhibitor |
| RU2424233C2 (ru) * | 2006-06-29 | 2011-07-20 | Ф.Хоффманн-Ля Рош Аг | Производные бензимидазола, методы их получения, применение их в качестве агонистов фарнезоид-х-рецептора (fxr) и содержащие их фармацевтические препараты |
| KR20090029827A (ko) * | 2006-07-20 | 2009-03-23 | 제네랩스 테크놀로지스, 인코포레이티드 | 폴리사이클릭 바이러스 억제제 |
| WO2014015905A1 (en) * | 2012-07-26 | 2014-01-30 | Glaxo Group Limited | 2 - (azaindol- 2 -yl) benz imidazoles as pad4 inhibitors |
| KR20150133172A (ko) * | 2013-03-15 | 2015-11-27 | 셀진 아빌로믹스 리서치, 인코포레이티드 | Mk2 억제제 및 이의 용도 |
| CA3199601A1 (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 |
| EP3419969B1 (en) | 2016-02-23 | 2019-12-18 | Padlock Therapeutics, Inc. | Heteroaryl inhibitors of pad4 |
| CN110248934B (zh) | 2016-09-12 | 2022-05-24 | 帕德罗科治疗公司 | 杂芳基pad4抑制剂 |
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- 2017-07-27 KR KR1020197005300A patent/KR102398941B1/ko active Active
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| CN109790162A (zh) | 2019-05-21 |
| US20190276432A1 (en) | 2019-09-12 |
| US10703741B2 (en) | 2020-07-07 |
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| ES2828623T3 (es) | 2021-05-27 |
| CN109790162B (zh) | 2022-06-28 |
| EP3490989B1 (en) | 2020-09-09 |
| EP3490989A1 (en) | 2019-06-05 |
| KR102398941B1 (ko) | 2022-05-17 |
| WO2018022897A1 (en) | 2018-02-01 |
| KR20190035773A (ko) | 2019-04-03 |
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