JP2015502387A5 - - Google Patents
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- 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
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- 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
- 150000001875 compounds Chemical class 0.000 claims 13
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 5
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 4
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- ABFPKTQEQNICFT-UHFFFAOYSA-M 2-chloro-1-methylpyridin-1-ium;iodide Chemical compound [I-].C[N+]1=CC=CC=C1Cl ABFPKTQEQNICFT-UHFFFAOYSA-M 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 206010018364 Glomerulonephritis Diseases 0.000 claims 2
- 101001136986 Homo sapiens Proteasome subunit beta type-8 Proteins 0.000 claims 2
- 208000010159 IgA glomerulonephritis Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 208000005777 Lupus Nephritis Diseases 0.000 claims 2
- 102100035760 Proteasome subunit beta type-8 Human genes 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 230000005856 abnormality Effects 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 229910002091 carbon monoxide Inorganic materials 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000004957 immunoregulator effect Effects 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 206010028417 myasthenia gravis Diseases 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 239000007821 HATU Substances 0.000 claims 1
- 206010066476 Haematological malignancy Diseases 0.000 claims 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 208000019802 Sexually transmitted disease Diseases 0.000 claims 1
- 206010050207 Skin fibrosis Diseases 0.000 claims 1
- 239000012317 TBTU Substances 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- CLZISMQKJZCZDN-UHFFFAOYSA-N [benzotriazol-1-yloxy(dimethylamino)methylidene]-dimethylazanium Chemical compound C1=CC=C2N(OC(N(C)C)=[N+](C)C)N=NC2=C1 CLZISMQKJZCZDN-UHFFFAOYSA-N 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 210000004204 blood vessel Anatomy 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 150000001718 carbodiimides Chemical class 0.000 claims 1
- 230000009787 cardiac fibrosis Effects 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 239000003153 chemical reaction reagent Substances 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 239000007822 coupling agent Substances 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 230000009610 hypersensitivity Effects 0.000 claims 1
- 230000028993 immune response Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 230000002194 synthesizing effect Effects 0.000 claims 1
- 125000001984 thiazolidinyl group Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161579076P | 2011-12-22 | 2011-12-22 | |
| US61/579,076 | 2011-12-22 | ||
| EP11195107 | 2011-12-22 | ||
| EP11195107.5 | 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) | SG11201403254QA (enExample) |
| WO (1) | WO2013092979A1 (enExample) |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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. |
| CA2893943C (en) | 2012-12-07 | 2021-03-02 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| 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 |
| AU2014204045B2 (en) * | 2013-01-04 | 2018-10-18 | 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 |
| US9241947B2 (en) | 2013-01-04 | 2016-01-26 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| 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 |
| WO2015171398A1 (en) | 2014-05-05 | 2015-11-12 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
| RS59488B1 (sr) | 2014-05-05 | 2019-12-31 | Rempex Pharmaceuticals Inc | Sinteza boronatnih soli i njihove upotrebe |
| JP6672176B2 (ja) | 2014-05-19 | 2020-03-25 | 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 | ボロン酸誘導体およびその治療的使用 |
| EP3882252B1 (en) | 2014-06-11 | 2025-11-19 | Venatorx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| 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 |
| BR112017006349A2 (pt) | 2014-10-01 | 2017-12-12 | Merck Patent Gmbh | derivados de ácido borônico |
| ES2873000T3 (es) * | 2014-10-01 | 2021-11-03 | Merck Patent Gmbh | Derivados del ácido borónico. |
| CN107001391B (zh) * | 2014-10-01 | 2020-11-27 | 默克专利股份公司 | 硼酸衍生物 |
| ES2811273T3 (es) * | 2014-10-01 | 2021-03-11 | Merck Patent Gmbh | Derivados del ácido borónico |
| US10662205B2 (en) | 2014-11-18 | 2020-05-26 | Qpex Biopharma, 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 |
| WO2017044828A1 (en) | 2015-09-11 | 2017-03-16 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| KR102764027B1 (ko) | 2015-10-15 | 2025-02-07 | 코넬 유니버시티 | 프로테아좀 억제제 및 이의 용도 |
| 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 |
| JP7060245B2 (ja) | 2016-06-30 | 2022-04-26 | キューペックス バイオファーマ， インコーポレイテッド | ボロン酸誘導体およびその治療的使用 |
| US11332485B2 (en) | 2017-05-26 | 2022-05-17 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| EP3630783A4 (en) | 2017-05-26 | 2021-03-03 | Venatorx Pharmaceuticals, Inc. | PENICILLIN-BINDING PROTEIN INHIBITORS |
| ES2927283T3 (es) | 2017-08-24 | 2022-11-03 | Merck Patent Gmbh | Derivados del ácido borónico |
| US11203613B2 (en) | 2017-10-11 | 2021-12-21 | Cornell University | Peptidomimetic proteasome inhibitors |
| CA3078627A1 (en) | 2017-10-11 | 2019-04-18 | Qpex Biopharma, Inc. | Boronic acid derivatives and synthesis thereof |
| 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 |
| CN111491938B (zh) | 2017-11-16 | 2024-05-24 | 普林斯匹亚生物制药公司 | 免疫蛋白酶体抑制剂 |
| 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 |
| EP3781576B1 (en) | 2018-04-20 | 2024-06-12 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| WO2019226931A1 (en) | 2018-05-25 | 2019-11-28 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| KR20210038590A (ko) | 2018-07-26 | 2021-04-07 | 메르크 파텐트 게엠베하 | 보론산 유도체 |
| CN113135944A (zh) * | 2020-01-19 | 2021-07-20 | 首药控股(北京)有限公司 | 硼酸衍生物 |
| 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 |
| 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 |
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 |
| NZ550522A (en) * | 2004-03-30 | 2010-08-27 | Millennium Pharm Inc | Synthesis of boronic ester and acid compounds |
| JP5232160B2 (ja) | 2006-11-14 | 2013-07-10 | メルク・シャープ・アンド・ドーム・コーポレーション | 糖尿病の治療又は予防のためのジペプチジルペプチダーゼｉｖインヒビターとしての三環式芳香族複素環化合物 |
| ES2390606T3 (es) * | 2007-08-06 | 2012-11-14 | Millennium Pharmaceuticals, Inc. | Inhibidores de proteasomas |
| WO2009051581A1 (en) * | 2007-10-16 | 2009-04-23 | Millennium Pharmaceuticals, Inc. | Proteasome inhibitors |
| BRPI0820532A2 (pt) * | 2007-11-13 | 2012-07-10 | Protez Pharmaceuticals Inc | inibidores de beta-lactamase |
| 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. |
| EA029521B1 (ru) * | 2010-03-31 | 2018-04-30 | Милленниум Фармасьютикалз, Инк. | Производные 1-амино-2-циклопропилэтилбороновой кислоты |
| WO2011137049A1 (en) | 2010-04-30 | 2011-11-03 | 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 BR BR112014015363A patent/BR112014015363A2/pt not_active Application Discontinuation
- 2012-12-21 ES ES12806491T patent/ES2699267T3/es active Active
- 2012-12-21 US US14/366,949 patent/US9688702B2/en not_active Expired - Fee Related
- 2012-12-21 MX MX2014007362A patent/MX352652B/es active IP Right Grant
- 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 CN CN201280063440.0A patent/CN104321060B/zh not_active Expired - Fee Related
- 2012-12-21 SG SG11201403254QA patent/SG11201403254QA/en unknown
- 2012-12-21 CA CA2860142A patent/CA2860142C/en active Active
- 2012-12-21 SG SG10201605152SA patent/SG10201605152SA/en unknown
- 2012-12-21 AU AU2012356890A patent/AU2012356890B2/en not_active Ceased
- 2012-12-21 EP EP12806491.2A patent/EP2793900B1/en active Active
- 2012-12-21 KR KR1020147020413A patent/KR20140114391A/ko not_active Ceased
- 2012-12-21 HK HK15106906.3A patent/HK1206261A1/xx unknown
-
2014
- 2014-06-17 IL IL233200A patent/IL233200A/en active IP Right Grant
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