JP6129203B2 - 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 - Google Patents
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 Download PDFInfo
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- JP6129203B2 JP6129203B2 JP2014548061A JP2014548061A JP6129203B2 JP 6129203 B2 JP6129203 B2 JP 6129203B2 JP 2014548061 A JP2014548061 A JP 2014548061A JP 2014548061 A JP2014548061 A JP 2014548061A JP 6129203 B2 JP6129203 B2 JP 6129203B2
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- boronic acid
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Classifications
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
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| EP11195107.5 | 2011-12-22 | ||
| PCT/EP2012/076595 WO2013092979A1 (en) | 2011-12-22 | 2012-12-21 | Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors |
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| RU2599791C2 (ru) | 2010-08-10 | 2016-10-20 | Ремпекс Фармасьютикэлз, Инч. | Циклические бороновые кислотно-эфирные производные и их использование в терапии |
| 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 |
| MX2015006715A (es) | 2012-12-03 | 2015-08-14 | Hoffmann La Roche | Compuestos de acido triazolboronico sustituido. |
| JP6403219B2 (ja) | 2012-12-07 | 2018-10-10 | 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 |
| 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 |
| AU2014204045B2 (en) * | 2013-01-04 | 2018-10-18 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| KR20150103270A (ko) | 2013-01-04 | 2015-09-09 | 렘펙스 파머수티클스 인코퍼레이티드 | 보론산 유도체 및 그의 치료적 용도 |
| CN105101970B (zh) | 2013-01-10 | 2018-11-20 | 维纳拓尔斯制药公司 | β-内酰胺酶抑制剂 |
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| ES2748434T3 (es) | 2014-01-10 | 2020-03-16 | Univ Cornell | Dipéptidos como inhibidores de inmunoproteasomas humanos |
| WO2015171398A1 (en) | 2014-05-05 | 2015-11-12 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
| US10385074B2 (en) | 2014-05-05 | 2019-08-20 | Rempex Pharmaceuticals, Inc. | Synthesis of boronate salts and uses thereof |
| AU2015264418A1 (en) | 2014-05-19 | 2016-11-10 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| KR102396753B1 (ko) | 2014-06-11 | 2022-05-12 | 베나토알엑스 파마슈티컬스, 인크. | 베타-락타마제 억제제 |
| AU2015284307A1 (en) * | 2014-07-01 | 2017-02-02 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| US11202817B2 (en) | 2014-08-18 | 2021-12-21 | Cornell University | Dipeptidomimetics as inhibitors of human immunoproteasomes |
| EP3201207B1 (en) * | 2014-10-01 | 2021-02-24 | Merck Patent GmbH | Boronic acid derivatives |
| EP3201208B1 (en) * | 2014-10-01 | 2021-03-24 | Merck Patent GmbH | Boronic acid derivatives |
| US10640520B2 (en) * | 2014-10-01 | 2020-05-05 | Merck Patent Gmbh | Boronic acid derivatives |
| AU2015327345B9 (en) | 2014-10-01 | 2020-06-18 | Merck Patent Gmbh | Boronic acid derivatives |
| WO2016081297A1 (en) | 2014-11-18 | 2016-05-26 | Rempex Pharmaceuticals, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| WO2016149393A1 (en) | 2015-03-17 | 2016-09-22 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| EP3347008B1 (en) | 2015-09-11 | 2022-03-09 | Venatorx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| EP4006012A1 (en) | 2015-10-15 | 2022-06-01 | 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 |
| AU2017290060B2 (en) | 2016-06-30 | 2021-07-22 | Qpex Biopharma, Inc | Boronic acid derivatives and therapeutic uses thereof |
| US11267826B2 (en) | 2017-05-26 | 2022-03-08 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| EP3630782A4 (en) | 2017-05-26 | 2021-03-03 | 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 |
| WO2019075252A1 (en) | 2017-10-11 | 2019-04-18 | Cornell University | PEPTIDOMIMETIC INHIBITORS OF PROTEASOME |
| BR112020007138B1 (pt) | 2017-10-11 | 2023-03-21 | Qpex Biopharma, Inc | Derivados de ácido borônico, métodos de síntese, composição farmacêutica e uso dos mesmos |
| 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 |
| WO2019099582A1 (en) | 2017-11-16 | 2019-05-23 | Principia Biopharma Inc. | Immunoproteasome inhibitors |
| PL3710457T3 (pl) | 2017-11-16 | 2023-02-20 | Principia Biopharma Inc. | Inhibitory immunoproteasomu |
| 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 |
| CN112424209A (zh) | 2018-04-20 | 2021-02-26 | Qpex生物制药有限公司 | 硼酸衍生物及其治疗用途 |
| US12173018B2 (en) | 2018-05-25 | 2024-12-24 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| MX2021000214A (es) | 2018-07-26 | 2021-03-31 | Merck Patent Gmbh | Derivados de acido boronico. |
| DK3886798T3 (da) | 2018-11-29 | 2026-04-20 | Basilea Pharmaceutica Int Ag Allschwil | Kombinationssammensætninger, som omfatter en beta-lactamase-hæmmer, og anvendelser deraf |
| US12636297B2 (en) | 2019-06-19 | 2026-05-26 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic 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 |
| US12637481B2 (en) | 2020-03-18 | 2026-05-26 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| IL297458A (en) | 2020-05-05 | 2022-12-01 | Qpex Biopharma Inc | Boronic acid derivatives and their synthesis, polymorphic forms and medicinal uses |
| 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 |
| US20250340577A1 (en) * | 2021-03-02 | 2025-11-06 | Case Western Reserve University | Beta-lactomase inhibitors and uses thereof |
| CN116940580A (zh) * | 2021-03-05 | 2023-10-24 | Ａｇｃ株式会社 | 化合物、化合物的制造方法及表面处理剂的制造方法 |
| US20240287102A1 (en) | 2021-07-29 | 2024-08-29 | 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 |
| JP7734276B2 (ja) * | 2021-10-14 | 2025-09-04 | ショウヤオ ホールディングス（ベイジン） カンパニー， リミテッド | ボロン酸誘導体 |
| CN117003776A (zh) * | 2022-04-29 | 2023-11-07 | 科辉智药生物科技(深圳)有限公司 | 一种硼酸类蛋白酶体抑制剂及其用途 |
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| CN122374318A (zh) | 2023-11-21 | 2026-07-10 | 巴斯利尔药物阿尔施维尔国际股份公司 | 口服递送的β-内酰胺酶抑制剂的柠檬酸盐配位复合物及其用途 |
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| 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 |
| ES2899606T3 (es) * | 2004-03-30 | 2022-03-14 | Millennium Pharm Inc | Síntesis de compuestos de ésteres y ácidos borónicos |
| WO2008060488A1 (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 |
| KR20140042933A (ko) * | 2007-08-06 | 2014-04-07 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 프로테아좀 억제제 |
| EP2212334B1 (en) * | 2007-10-16 | 2012-08-15 | Millennium Pharmaceuticals, Inc. | Proteasome inhibitors |
| EA201000774A1 (ru) * | 2007-11-13 | 2010-12-30 | Новартис Интернэшнл Фармасьютикл Лтд. | Ингибиторы бета-лактамазы |
| 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 |
| US8507494B2 (en) | 2010-04-30 | 2013-08-13 | Merck Sharp & Dohme Corp. | Heterocyclic quinolizine derived M1 receptor positive allosteric modulators |
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| CA2860142C (en) | 2020-10-27 |
| BR112014015363A2 (pt) | 2017-06-13 |
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| HK1206261A1 (en) | 2016-01-08 |
| BR112014015363A8 (pt) | 2017-06-13 |
| EP2793900B1 (en) | 2018-08-22 |
| IL233200A0 (en) | 2014-07-31 |
| KR20140114391A (ko) | 2014-09-26 |
| MX352652B (es) | 2017-12-04 |
| CN104321060B (zh) | 2018-08-07 |
| CN104321060A (zh) | 2015-01-28 |
| AU2012356890B2 (en) | 2017-06-08 |
| ES2699267T3 (es) | 2019-02-08 |
| US9688702B2 (en) | 2017-06-27 |
| WO2013092979A1 (en) | 2013-06-27 |
| JP2015502387A (ja) | 2015-01-22 |
| CA2860142A1 (en) | 2013-06-27 |
| AU2012356890A1 (en) | 2014-08-07 |
| US20140364396A1 (en) | 2014-12-11 |
| IL233200A (en) | 2017-08-31 |
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