JP2015502387A5 - - Google Patents
Download PDFInfo
- 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
- 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 | |
| EP11195107 | 2011-12-22 | ||
| EP11195107.5 | 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 (OSRAM) | 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 (OSRAM) |
| EP (1) | EP2793900B1 (OSRAM) |
| JP (1) | JP6129203B2 (OSRAM) |
| KR (1) | KR20140114391A (OSRAM) |
| CN (1) | CN104321060B (OSRAM) |
| AU (1) | AU2012356890B2 (OSRAM) |
| BR (1) | BR112014015363A2 (OSRAM) |
| CA (1) | CA2860142C (OSRAM) |
| EA (1) | EA201400735A1 (OSRAM) |
| ES (1) | ES2699267T3 (OSRAM) |
| HK (1) | HK1206261A1 (OSRAM) |
| IL (1) | IL233200A (OSRAM) |
| MX (1) | MX352652B (OSRAM) |
| SG (2) | SG10201605152SA (OSRAM) |
| WO (1) | WO2013092979A1 (OSRAM) |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2603514B1 (en) | 2010-08-10 | 2018-07-18 | Rempex Pharmaceuticals, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| US9012491B2 (en) | 2011-08-31 | 2015-04-21 | 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 |
| JP6018319B2 (ja) * | 2012-12-03 | 2016-11-02 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 置換トリアゾールボロン酸化合物 |
| 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 |
| AU2014204046B2 (en) | 2013-01-04 | 2017-02-23 | 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 |
| 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 |
| US9241947B2 (en) | 2013-01-04 | 2016-01-26 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| EP2943204B1 (en) | 2013-01-10 | 2019-03-13 | Venatorx Pharmaceuticals Inc | Beta-lactamase inhibitors |
| US9944658B2 (en) | 2013-03-14 | 2018-04-17 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| ES2748434T3 (es) | 2014-01-10 | 2020-03-16 | Univ Cornell | Dipéptidos como inhibidores de inmunoproteasomas humanos |
| RS59488B1 (sr) | 2014-05-05 | 2019-12-31 | Rempex Pharmaceuticals Inc | Sinteza boronatnih soli i njihove upotrebe |
| US9687497B1 (en) | 2014-05-05 | 2017-06-27 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
| MX2016015093A (es) | 2014-05-19 | 2017-03-27 | Rempex Pharmaceuticals Inc | Derivados de acido boronico y sus usos terapeuticos. |
| KR20220065084A (ko) * | 2014-06-11 | 2022-05-19 | 베나토알엑스 파마슈티컬스, 인크. | 베타-락타마제 억제제 |
| 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 |
| SG11201702623TA (en) * | 2014-10-01 | 2017-04-27 | Merck Patent Gmbh | Boronic acid derivatives |
| AU2015327411B2 (en) * | 2014-10-01 | 2020-01-02 | Merck Patent Gmbh | Boronic acid derivatives |
| CA2963198A1 (en) * | 2014-10-01 | 2016-04-07 | Merck Patent Gmbh | Boronic acid derivatives |
| 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 |
| 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 |
| JP6970085B2 (ja) | 2015-10-15 | 2021-11-24 | コーネル・ユニバーシティーCornell University | プロテアソーム阻害剤およびその用途 |
| 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 |
| EP3478693B1 (en) | 2016-06-30 | 2021-07-21 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| WO2018218190A1 (en) | 2017-05-26 | 2018-11-29 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| WO2018218154A1 (en) | 2017-05-26 | 2018-11-29 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| WO2019038250A1 (en) | 2017-08-24 | 2019-02-28 | Merck Patent Gmbh | Boronic acid derivatives |
| US11203613B2 (en) | 2017-10-11 | 2021-12-21 | Cornell University | Peptidomimetic proteasome inhibitors |
| JP7377545B2 (ja) | 2017-10-11 | 2023-11-10 | 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合成 |
| 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 |
| EA202090900A1 (ru) | 2017-11-16 | 2020-10-02 | Принсипиа Биофарма Инк. | Ингибиторы иммунопротеасом |
| LT3710457T (lt) | 2017-11-16 | 2022-11-10 | Principia Biopharma Inc. | Imunoproteasomos inhibitoriai |
| 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 |
| CA3097127A1 (en) | 2018-04-20 | 2019-10-24 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| US12173018B2 (en) | 2018-05-25 | 2024-12-24 | 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 |
| 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 |
| WO2022186265A1 (ja) * | 2021-03-05 | 2022-09-09 | 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 |
| IL310390A (en) | 2021-07-29 | 2024-03-01 | Merck Patent Gmbh | 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 |
| KR20240090392A (ko) * | 2021-10-14 | 2024-06-21 | 쇼우야오 홀딩스 (베이징) 코., 엘티디. | 보론산 유도체 |
| 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 |
| PL4008721T3 (pl) | 2004-03-30 | 2024-05-13 | Millennium Pharmaceuticals, Inc. | Synteza związków estrów i kwasów boronowych |
| 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 |
| GEP20125599B (en) * | 2007-08-06 | 2012-08-10 | Millennium Pharm Inc | Proteasome inhibitors |
| WO2009051581A1 (en) * | 2007-10-16 | 2009-04-23 | 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. |
| CN106008570A (zh) * | 2010-03-31 | 2016-10-12 | 米伦纽姆医药公司 | 1-氨基-2-环丙基乙硼酸衍生物 |
| WO2011137049A1 (en) | 2010-04-30 | 2011-11-03 | Merck Sharp & Dohme Corp. | Heterocyclic quinolizine derived m1 receptor positive allosteric modulators |
-
2012
- 2012-12-21 SG SG10201605152SA patent/SG10201605152SA/en unknown
- 2012-12-21 ES ES12806491T patent/ES2699267T3/es active Active
- 2012-12-21 EP EP12806491.2A patent/EP2793900B1/en active Active
- 2012-12-21 US US14/366,949 patent/US9688702B2/en not_active Expired - Fee Related
- 2012-12-21 AU AU2012356890A patent/AU2012356890B2/en not_active Ceased
- 2012-12-21 HK HK15106906.3A patent/HK1206261A1/xx unknown
- 2012-12-21 JP JP2014548061A patent/JP6129203B2/ja 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 BR BR112014015363A patent/BR112014015363A2/pt not_active Application Discontinuation
- 2012-12-21 KR KR1020147020413A patent/KR20140114391A/ko not_active Ceased
- 2012-12-21 CN CN201280063440.0A patent/CN104321060B/zh not_active Expired - Fee Related
- 2012-12-21 MX MX2014007362A patent/MX352652B/es active IP Right Grant
- 2012-12-21 EA EA201400735A patent/EA201400735A1/ru unknown
- 2012-12-21 WO PCT/EP2012/076595 patent/WO2013092979A1/en not_active Ceased
-
2014
- 2014-06-17 IL IL233200A patent/IL233200A/en active IP Right Grant
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2015502387A5 (OSRAM) | ||
| AU2020262221B2 (en) | 4H-pyrrolo(3,2-c)pyridin-4-one compounds | |
| JP2018537483A (ja) | ビアリールモノバクタム化合物および細菌感染治療のためのそれの使用方法 | |
| EA023826B1 (ru) | Дигидропиримидинизохинолиноны и содержащие их фармацевтические композиции для лечения воспалительных нарушений | |
| JP2016534146A5 (OSRAM) | ||
| JP2008503591A5 (OSRAM) | ||
| JP2015163632A5 (OSRAM) | ||
| JP2016500661A5 (OSRAM) | ||
| BR112015023142B1 (pt) | Moduladores do p2x7, seu uso, processo de preparação e composição farmacêutica que os compreende | |
| JP2011523945A5 (OSRAM) | ||
| JP2016530338A5 (OSRAM) | ||
| JP2015501327A5 (OSRAM) | ||
| JP2013536259A5 (OSRAM) | ||
| WO2007113289A1 (en) | Benzofuran compounds as ep1 receptor antagonists | |
| JP2017509689A5 (OSRAM) | ||
| JP2019501927A5 (OSRAM) | ||
| KR20210005668A (ko) | Hpk1 억제제, 그의 제조 방법 및 응용 | |
| JP2016532669A5 (OSRAM) | ||
| JP2017508733A5 (OSRAM) | ||
| JP2014505033A5 (OSRAM) | ||
| JP2010518146A (ja) | ベンゾフラン化合物 | |
| JP2009513718A5 (OSRAM) | ||
| JP2015502371A5 (OSRAM) | ||
| JP2018510131A5 (OSRAM) | ||
| JP2018534267A5 (OSRAM) |