JP2015502387A5 - - Google Patents
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- Publication number
- JP2015502387A5 JP2015502387A5 JP2014548061A JP2014548061A JP2015502387A5 JP 2015502387 A5 JP2015502387 A5 JP 2015502387A5 JP 2014548061 A JP2014548061 A JP 2014548061A JP 2014548061 A JP2014548061 A JP 2014548061A JP 2015502387 A5 JP2015502387 A5 JP 2015502387A5
- Authority
- JP
- Japan
- Prior art keywords
- hal
- formula
- alkyl
- independently
- ring
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161579076P | 2011-12-22 | 2011-12-22 | |
| EP11195107.5 | 2011-12-22 | ||
| EP11195107 | 2011-12-22 | ||
| US61/579,076 | 2011-12-22 | ||
| PCT/EP2012/076595 WO2013092979A1 (en) | 2011-12-22 | 2012-12-21 | Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015502387A JP2015502387A (ja) | 2015-01-22 |
| JP2015502387A5 true JP2015502387A5 (enExample) | 2016-02-18 |
| JP6129203B2 JP6129203B2 (ja) | 2017-05-17 |
Family
ID=48667763
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014548061A Expired - Fee Related JP6129203B2 (ja) | 2011-12-22 | 2012-12-21 | α−アミノボロン酸誘導体、選択性免疫プロテアソーム阻害剤 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US9688702B2 (enExample) |
| EP (1) | EP2793900B1 (enExample) |
| JP (1) | JP6129203B2 (enExample) |
| KR (1) | KR20140114391A (enExample) |
| CN (1) | CN104321060B (enExample) |
| AU (1) | AU2012356890B2 (enExample) |
| BR (1) | BR112014015363A2 (enExample) |
| CA (1) | CA2860142C (enExample) |
| EA (1) | EA201400735A1 (enExample) |
| ES (1) | ES2699267T3 (enExample) |
| HK (1) | HK1206261A1 (enExample) |
| IL (1) | IL233200A (enExample) |
| MX (1) | MX352652B (enExample) |
| SG (2) | SG10201605152SA (enExample) |
| WO (1) | WO2013092979A1 (enExample) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102205755B1 (ko) | 2010-08-10 | 2021-01-22 | 렘펙스 파머수티클스 인코퍼레이티드 | 고리형 보론산 에스터 유도체의 결정 형태 |
| WO2013033461A1 (en) | 2011-08-31 | 2013-03-07 | Rempex Pharmaceuticals, Inc. | Heterocyclic boronic acid ester derivatives and therapeutic uses thereof |
| US9156858B2 (en) | 2012-05-23 | 2015-10-13 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| US10561675B2 (en) | 2012-06-06 | 2020-02-18 | Rempex Pharmaceuticals, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| WO2014086664A1 (en) | 2012-12-03 | 2014-06-12 | F. Hoffmann-La Roche Ag | Substituted triazole boronic acid compounds |
| PT2928898T (pt) | 2012-12-07 | 2021-07-05 | Venatorx Pharmaceuticals Inc | Inibidores de beta-lactamase |
| US9241947B2 (en) | 2013-01-04 | 2016-01-26 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| US9101638B2 (en) | 2013-01-04 | 2015-08-11 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| JP6324409B2 (ja) * | 2013-01-04 | 2018-05-16 | レンペックス・ファーマシューティカルズ・インコーポレイテッド | ボロン酸誘導体及びその治療的使用 |
| JP2016509594A (ja) * | 2013-01-04 | 2016-03-31 | レンペックス・ファーマシューティカルズ・インコーポレイテッド | ボロン酸誘導体及びその治療的使用 |
| JP6346904B2 (ja) | 2013-01-10 | 2018-06-20 | ベナトルクス ファーマシューティカルズ,インク. | ベータ−ラクタマーゼ阻害剤 |
| WO2014151958A1 (en) | 2013-03-14 | 2014-09-25 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| US9988421B2 (en) | 2014-01-10 | 2018-06-05 | Cornell University | Dipeptides as inhibitors of human immunoproteasomes |
| FI3604316T3 (fi) | 2014-05-05 | 2024-02-29 | Melinta Therapeutics Inc | Boronaattisuolojen synteesi |
| US9687497B1 (en) | 2014-05-05 | 2017-06-27 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
| AU2015264418A1 (en) | 2014-05-19 | 2016-11-10 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| RU2686740C2 (ru) * | 2014-06-11 | 2019-04-30 | Венаторкс Фармасьютикалс, Инк. | Ингибиторы бета-лактамазы |
| EA201692301A1 (ru) * | 2014-07-01 | 2017-06-30 | Ремпекс Фармасьютикалз, Инк. | Производные бороновой кислоты и их терапевтическое применение |
| EP3193904B1 (en) | 2014-08-18 | 2025-10-01 | Cornell University | Dipeptidomimetics as inhibitors of human immunoproteasomes |
| ES2873000T3 (es) * | 2014-10-01 | 2021-11-03 | Merck Patent Gmbh | Derivados del ácido borónico. |
| JP6662865B2 (ja) | 2014-10-01 | 2020-03-11 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung | ボロン酸誘導体 |
| KR20170062518A (ko) | 2014-10-01 | 2017-06-07 | 메르크 파텐트 게엠베하 | 보론산 유도체 |
| CN107108660B (zh) * | 2014-10-01 | 2020-09-15 | 默克专利股份公司 | 硼酸衍生物 |
| WO2016081297A1 (en) | 2014-11-18 | 2016-05-26 | Rempex Pharmaceuticals, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| US20180051041A1 (en) | 2015-03-17 | 2018-02-22 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| CN108472284A (zh) | 2015-09-11 | 2018-08-31 | 维纳拓尔斯制药公司 | β-内酰胺酶抑制剂 |
| EP3362754B1 (en) | 2015-10-15 | 2021-12-22 | Cornell University | Proteasome inhibitors and uses thereof |
| WO2017100537A1 (en) | 2015-12-10 | 2017-06-15 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| CN107151255A (zh) * | 2016-03-06 | 2017-09-12 | 复旦大学 | 硼酸类化合物及其制备方法和用途 |
| UA124464C2 (uk) | 2016-06-30 | 2021-09-22 | Кьюпекс Біофарма, Інк. | Похідні боронової кислоти та їх терапевтичні застосування |
| EP3630783A4 (en) | 2017-05-26 | 2021-03-03 | Venatorx Pharmaceuticals, Inc. | PENICILLIN-BINDING PROTEIN INHIBITORS |
| WO2018218190A1 (en) | 2017-05-26 | 2018-11-29 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| IL272806B2 (en) | 2017-08-24 | 2023-09-01 | Merck Patent Gmbh | The history of boronic acid, its preparation and pharmaceutical preparations containing it |
| EP3694864B1 (en) | 2017-10-11 | 2025-03-05 | Qpex Biopharma, Inc. | Boronic acid derivatives and synthesis thereof |
| EP3694605A4 (en) | 2017-10-11 | 2021-10-27 | Cornell University | PEPTIDOMIMETIC PROTEASOME INHIBITORS |
| CN107556336A (zh) * | 2017-10-16 | 2018-01-09 | 康化(上海)新药研发有限公司 | 一种呋喃‑2‑甲烷基硼酸频哪醇酯的合成方法 |
| EP3710457B1 (en) | 2017-11-16 | 2022-08-03 | Principia Biopharma Inc. | Immunoproteasome inhibitors |
| WO2019099582A1 (en) | 2017-11-16 | 2019-05-23 | Principia Biopharma Inc. | Immunoproteasome inhibitors |
| CN108130370B (zh) * | 2018-01-05 | 2020-11-17 | 武汉惠康达科技有限公司 | Psmb8及其抑制剂在制备治疗脂肪肝及其相关疾病药物中的应用 |
| WO2019204419A1 (en) | 2018-04-20 | 2019-10-24 | The Medicines Company (San Diego), Llc | Boronic acid derivatives and therapeutic uses thereof |
| WO2019226931A1 (en) | 2018-05-25 | 2019-11-28 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| CN112469480A (zh) | 2018-07-26 | 2021-03-09 | 默克专利股份公司 | 硼酸衍生物 |
| WO2020112542A1 (en) | 2018-11-29 | 2020-06-04 | VenatoRx Pharmaceuticals, Inc. | Combination compositions comprising a beta-lactamase inhibitor and uses thereof |
| CN113135944A (zh) * | 2020-01-19 | 2021-07-20 | 首药控股(北京)有限公司 | 硼酸衍生物 |
| AU2021266715A1 (en) | 2020-05-05 | 2022-11-17 | Qpex Biopharma, Inc. | Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof |
| CN114075227B (zh) * | 2020-08-19 | 2023-07-04 | 北京嵩润医药科技有限责任公司 | 吡唑硼酸类化合物、包含其的药物组合物及它们的用途 |
| WO2022187362A1 (en) * | 2021-03-02 | 2022-09-09 | Case Western Reserve University | Β-lactamase inhibitors and uses thereof |
| JP7758028B2 (ja) * | 2021-03-05 | 2025-10-22 | Agc株式会社 | 化合物、化合物の製造方法及び表面処理剤の製造方法 |
| CA3227452A1 (en) | 2021-07-29 | 2023-02-02 | Merck Patent Gmbh | Novel crystalline forms of [(1r)-2-(1-benzofuran-3-yl)-1-{[(1s,2r,4r)-7- oxabicyclo[2.2.1]heptan-2-yl]formamido}ethyl]boronic acid, adducts thereof, and processes to obtain |
| WO2023061445A1 (zh) * | 2021-10-14 | 2023-04-20 | 首药控股(北京)股份有限公司 | 硼酸衍生物 |
| WO2023232830A1 (en) | 2022-06-02 | 2023-12-07 | Merck Patent Gmbh | Boronic acid adducts |
| TW202529745A (zh) | 2023-11-21 | 2025-08-01 | 美商維納拓爾斯製藥公司 | 經口遞送之β-內醯胺酶抑制劑之檸檬酸鹽配位錯合物及其用途 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL111175A0 (en) | 1993-10-07 | 1994-12-29 | Du Pont Merck Pharma | Electrophilic peptide analogs as inhibitors of trypsin-like serine proteases and pharmaceutical compositions containing them |
| US7271186B1 (en) | 2002-12-09 | 2007-09-18 | Northwestern University | Nanomolar β-lactamase inhibitors |
| US7332343B2 (en) * | 2004-01-16 | 2008-02-19 | Board Of Regents, The University Of Texas System | Determining enantiomeric excess using indicator-displacement assays |
| NZ598172A (en) * | 2004-03-30 | 2013-08-30 | Millennium Pharm Inc | Synthesis of boronic ester and acid compounds |
| CA2668662A1 (en) | 2006-11-14 | 2008-05-22 | Merck & Co., Inc. | Tricyclic heteroaromatic compounds as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes |
| MY161991A (en) * | 2007-08-06 | 2017-05-31 | Millennium Pharm Inc | Proteasome inhibitors |
| JP5600595B2 (ja) * | 2007-10-16 | 2014-10-01 | ミレニアム ファーマシューティカルズ, インコーポレイテッド | プロテアソーム阻害剤 |
| TW200936143A (en) * | 2007-11-13 | 2009-09-01 | Protez Pharmaceuticals Inc | Beta-lactamase inhibitors |
| AR075090A1 (es) | 2008-09-29 | 2011-03-09 | Millennium Pharm Inc | Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden. |
| AU2011235227B2 (en) * | 2010-03-31 | 2016-09-08 | Millennium Pharmaceuticals, Inc. | Derivatives of 1-amino-2-cyclopropylethylboronic acid |
| EP2563126B1 (en) | 2010-04-30 | 2016-05-11 | Merck Sharp & Dohme Corp. | Heterocyclic quinolizine derived m1 receptor positive allosteric modulators |
-
2012
- 2012-12-21 JP JP2014548061A patent/JP6129203B2/ja not_active Expired - Fee Related
- 2012-12-21 MX MX2014007362A patent/MX352652B/es active IP Right Grant
- 2012-12-21 AU AU2012356890A patent/AU2012356890B2/en not_active Ceased
- 2012-12-21 KR KR1020147020413A patent/KR20140114391A/ko not_active Ceased
- 2012-12-21 US US14/366,949 patent/US9688702B2/en not_active Expired - Fee Related
- 2012-12-21 ES ES12806491T patent/ES2699267T3/es active Active
- 2012-12-21 EP EP12806491.2A patent/EP2793900B1/en active Active
- 2012-12-21 CN CN201280063440.0A patent/CN104321060B/zh not_active Expired - Fee Related
- 2012-12-21 HK HK15106906.3A patent/HK1206261A1/xx unknown
- 2012-12-21 SG SG10201605152SA patent/SG10201605152SA/en unknown
- 2012-12-21 CA CA2860142A patent/CA2860142C/en active Active
- 2012-12-21 SG SG11201403254QA patent/SG11201403254QA/en unknown
- 2012-12-21 WO PCT/EP2012/076595 patent/WO2013092979A1/en not_active Ceased
- 2012-12-21 EA EA201400735A patent/EA201400735A1/ru unknown
- 2012-12-21 BR BR112014015363A patent/BR112014015363A2/pt not_active Application Discontinuation
-
2014
- 2014-06-17 IL IL233200A patent/IL233200A/en active IP Right Grant
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