JP2017517508A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017517508A5 JP2017517508A5 JP2016568679A JP2016568679A JP2017517508A5 JP 2017517508 A5 JP2017517508 A5 JP 2017517508A5 JP 2016568679 A JP2016568679 A JP 2016568679A JP 2016568679 A JP2016568679 A JP 2016568679A JP 2017517508 A5 JP2017517508 A5 JP 2017517508A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- alkyl
- group
- hydroxy
- halogen
- 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
- 229910052736 halogen Chemical group 0.000 claims 70
- 150000002367 halogens Chemical group 0.000 claims 70
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 69
- 125000001424 substituent group Chemical group 0.000 claims 68
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 57
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 45
- KWEDUNSJJZVRKR-UHFFFAOYSA-N carbononitridic azide Chemical group [N-]=[N+]=NC#N KWEDUNSJJZVRKR-UHFFFAOYSA-N 0.000 claims 36
- -1 hydroxy Chemical group 0.000 claims 31
- 125000000217 alkyl group Chemical group 0.000 claims 30
- 150000001875 compounds Chemical class 0.000 claims 30
- 125000004093 cyano group Chemical group *C#N 0.000 claims 30
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 18
- 150000001540 azides Chemical group 0.000 claims 17
- 125000000623 heterocyclic group Chemical group 0.000 claims 16
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 14
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 13
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 11
- 125000004452 carbocyclyl group Chemical group 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 125000005865 C2-C10alkynyl group Chemical group 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- MZAGXDHQGXUDDX-JSRXJHBZSA-N (e,2z)-4-ethyl-2-hydroxyimino-5-nitrohex-3-enamide Chemical compound [O-][N+](=O)C(C)C(/CC)=C/C(=N/O)/C(N)=O MZAGXDHQGXUDDX-JSRXJHBZSA-N 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 150000001732 carboxylic acid derivatives Chemical group 0.000 claims 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical group [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 3
- UUGRTBCTVUNWTN-DLRIENLKSA-N (2s,3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[(1,5-dihydroxy-4-oxopyridin-2-yl)methoxyimino]acetyl]amino]-2-methyl-4-oxoazetidine-1-sulfonic acid Chemical compound O=C1N(S(O)(=O)=O)[C@@H](C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCC1=CC(=O)C(O)=CN1O UUGRTBCTVUNWTN-DLRIENLKSA-N 0.000 claims 2
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 2
- 125000006545 (C1-C9) alkyl group Chemical group 0.000 claims 2
- WZPBZJONDBGPKJ-UHFFFAOYSA-N Antibiotic SQ 26917 Natural products O=C1N(S(O)(=O)=O)C(C)C1NC(=O)C(=NOC(C)(C)C(O)=O)C1=CSC(N)=N1 WZPBZJONDBGPKJ-UHFFFAOYSA-N 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- JUZNIMUFDBIJCM-ANEDZVCMSA-N Invanz Chemical compound O=C([C@H]1NC[C@H](C1)SC=1[C@H](C)[C@@H]2[C@H](C(N2C=1C(O)=O)=O)[C@H](O)C)NC1=CC=CC(C(O)=O)=C1 JUZNIMUFDBIJCM-ANEDZVCMSA-N 0.000 claims 2
- TYMABNNERDVXID-DLYFRVTGSA-N Panipenem Chemical compound C([C@@H]1[C@H](C(N1C=1C(O)=O)=O)[C@H](O)C)C=1S[C@H]1CCN(C(C)=N)C1 TYMABNNERDVXID-DLYFRVTGSA-N 0.000 claims 2
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- WKDDRNSBRWANNC-UHFFFAOYSA-N Thienamycin Natural products C1C(SCCN)=C(C(O)=O)N2C(=O)C(C(O)C)C21 WKDDRNSBRWANNC-UHFFFAOYSA-N 0.000 claims 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 2
- KLFSEZJCLYBFKQ-WXYNYTDUSA-N [(3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[(1,5-dihydroxy-4-oxopyridin-2-yl)methoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCC1=CC(=O)C(O)=CN1O KLFSEZJCLYBFKQ-WXYNYTDUSA-N 0.000 claims 2
- 239000003242 anti bacterial agent Substances 0.000 claims 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 2
- 239000000043 antiallergic agent Substances 0.000 claims 2
- 239000003429 antifungal agent Substances 0.000 claims 2
- 229940121375 antifungal agent Drugs 0.000 claims 2
- 239000003443 antiviral agent Substances 0.000 claims 2
- WZPBZJONDBGPKJ-VEHQQRBSSA-N aztreonam Chemical compound O=C1N(S([O-])(=O)=O)[C@@H](C)[C@@H]1NC(=O)C(=N/OC(C)(C)C(O)=O)\C1=CSC([NH3+])=N1 WZPBZJONDBGPKJ-VEHQQRBSSA-N 0.000 claims 2
- 229960003644 aztreonam Drugs 0.000 claims 2
- 239000003782 beta lactam antibiotic agent Substances 0.000 claims 2
- MRMBZHPJVKCOMA-YJFSRANCSA-N biapenem Chemical compound C1N2C=NC=[N+]2CC1SC([C@@H]1C)=C(C([O-])=O)N2[C@H]1[C@@H]([C@H](O)C)C2=O MRMBZHPJVKCOMA-YJFSRANCSA-N 0.000 claims 2
- 229960003169 biapenem Drugs 0.000 claims 2
- UIMOJFJSJSIGLV-JNHMLNOCSA-N carumonam Chemical compound O=C1N(S(O)(=O)=O)[C@H](COC(=O)N)[C@@H]1NC(=O)C(=N/OCC(O)=O)\C1=CSC(N)=N1 UIMOJFJSJSIGLV-JNHMLNOCSA-N 0.000 claims 2
- 229960000662 carumonam Drugs 0.000 claims 2
- ORFOPKXBNMVMKC-DWVKKRMSSA-N ceftazidime Chemical compound S([C@@H]1[C@@H](C(N1C=1C([O-])=O)=O)NC(=O)\C(=N/OC(C)(C)C(O)=O)C=2N=C(N)SC=2)CC=1C[N+]1=CC=CC=C1 ORFOPKXBNMVMKC-DWVKKRMSSA-N 0.000 claims 2
- 229960000484 ceftazidime Drugs 0.000 claims 2
- UNJFKXSSGBWRBZ-BJCIPQKHSA-N ceftibuten Chemical compound S1C(N)=NC(C(=C\CC(O)=O)\C(=O)N[C@@H]2C(N3C(=CCS[C@@H]32)C(O)=O)=O)=C1 UNJFKXSSGBWRBZ-BJCIPQKHSA-N 0.000 claims 2
- 229960004086 ceftibuten Drugs 0.000 claims 2
- AVAACINZEOAHHE-VFZPANTDSA-N doripenem Chemical compound C=1([C@H](C)[C@@H]2[C@H](C(N2C=1C(O)=O)=O)[C@H](O)C)S[C@@H]1CN[C@H](CNS(N)(=O)=O)C1 AVAACINZEOAHHE-VFZPANTDSA-N 0.000 claims 2
- 229960000895 doripenem Drugs 0.000 claims 2
- 229960002770 ertapenem Drugs 0.000 claims 2
- ZSKVGTPCRGIANV-ZXFLCMHBSA-N imipenem Chemical compound C1C(SCC\N=C\N)=C(C(O)=O)N2C(=O)[C@H]([C@H](O)C)[C@H]21 ZSKVGTPCRGIANV-ZXFLCMHBSA-N 0.000 claims 2
- 229960002182 imipenem Drugs 0.000 claims 2
- DMJNNHOOLUXYBV-PQTSNVLCSA-N meropenem Chemical compound C=1([C@H](C)[C@@H]2[C@H](C(N2C=1C(O)=O)=O)[C@H](O)C)S[C@@H]1CN[C@H](C(=O)N(C)C)C1 DMJNNHOOLUXYBV-PQTSNVLCSA-N 0.000 claims 2
- 229960002260 meropenem Drugs 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229950011346 panipenem Drugs 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- VAMSVIZLXJOLHZ-QWFSEIHXSA-N tigemonam Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(=N/OCC(O)=O)\C1=CSC(N)=N1 VAMSVIZLXJOLHZ-QWFSEIHXSA-N 0.000 claims 2
- 229950010206 tigemonam Drugs 0.000 claims 2
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims 1
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- QUKGLNCXGVWCJX-UHFFFAOYSA-N 1,3,4-thiadiazol-2-amine Chemical compound NC1=NN=CS1 QUKGLNCXGVWCJX-UHFFFAOYSA-N 0.000 claims 1
- RAIPHJJURHTUIC-UHFFFAOYSA-N 1,3-thiazol-2-amine Chemical compound NC1=NC=CS1 RAIPHJJURHTUIC-UHFFFAOYSA-N 0.000 claims 1
- MCTWTZJPVLRJOU-UHFFFAOYSA-N 1-methyl-1H-imidazole Chemical compound CN1C=CN=C1 MCTWTZJPVLRJOU-UHFFFAOYSA-N 0.000 claims 1
- OMAFFHIGWTVZOH-UHFFFAOYSA-N 1-methyltetrazole Chemical compound CN1C=NN=N1 OMAFFHIGWTVZOH-UHFFFAOYSA-N 0.000 claims 1
- JWAWEQBUZOGIBZ-UHFFFAOYSA-N 1-methyltriazole Chemical compound CN1C=CN=N1 JWAWEQBUZOGIBZ-UHFFFAOYSA-N 0.000 claims 1
- XJLITJHUQRBWPN-UHFFFAOYSA-N 2-acetamidoacetic acid;4-[2-(4-carbamimidoylphenyl)iminohydrazinyl]benzenecarboximidamide Chemical compound CC(=O)NCC(O)=O.C1=CC(C(=N)N)=CC=C1NN=NC1=CC=C(C(N)=N)C=C1 XJLITJHUQRBWPN-UHFFFAOYSA-N 0.000 claims 1
- ULRPISSMEBPJLN-UHFFFAOYSA-N 2h-tetrazol-5-amine Chemical compound NC1=NN=NN1 ULRPISSMEBPJLN-UHFFFAOYSA-N 0.000 claims 1
- QRZMXADUXZADTF-UHFFFAOYSA-N 4-aminoimidazole Chemical compound NC1=CNC=N1 QRZMXADUXZADTF-UHFFFAOYSA-N 0.000 claims 1
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims 1
- KLSJWNVTNUYHDU-UHFFFAOYSA-N Amitrole Chemical compound NC1=NC=NN1 KLSJWNVTNUYHDU-UHFFFAOYSA-N 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- 241001024304 Mino Species 0.000 claims 1
- MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical group CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 1
- 102000013566 Plasminogen Human genes 0.000 claims 1
- 108010051456 Plasminogen Proteins 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
- 235000018936 Vitellaria paradoxa Nutrition 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 229950003476 aminothiazole Drugs 0.000 claims 1
- 230000001548 androgenic effect Effects 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 230000003796 beauty Effects 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 229960003194 meglumine Drugs 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical compound C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical class [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 claims 1
- 150000003536 tetrazoles Chemical class 0.000 claims 1
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 claims 1
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 1
- 229930192474 thiophene Natural products 0.000 claims 1
- 150000003852 triazoles Chemical class 0.000 claims 1
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical group [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462000400P | 2014-05-19 | 2014-05-19 | |
| US62/000,400 | 2014-05-19 | ||
| PCT/US2015/031400 WO2015179308A1 (en) | 2014-05-19 | 2015-05-18 | Boronic acid derivatives and therapeutic uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017517508A JP2017517508A (ja) | 2017-06-29 |
| JP2017517508A5 true JP2017517508A5 (enExample) | 2018-07-05 |
| JP6672176B2 JP6672176B2 (ja) | 2020-03-25 |
Family
ID=54554593
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016568679A Active JP6672176B2 (ja) | 2014-05-19 | 2015-05-18 | ボロン酸誘導体およびその治療的使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9963467B2 (enExample) |
| EP (1) | EP3145936B1 (enExample) |
| JP (1) | JP6672176B2 (enExample) |
| KR (1) | KR20170007448A (enExample) |
| CN (1) | CN106459096B (enExample) |
| AU (1) | AU2015264418A1 (enExample) |
| BR (1) | BR112016026291A2 (enExample) |
| CA (1) | CA2947041A1 (enExample) |
| EA (1) | EA201691988A1 (enExample) |
| MX (1) | MX2016015093A (enExample) |
| WO (1) | WO2015179308A1 (enExample) |
Families Citing this family (34)
| 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 |
| CA2893943C (en) | 2012-12-07 | 2021-03-02 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| AU2014204045B2 (en) | 2013-01-04 | 2018-10-18 | 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 |
| RS59488B1 (sr) | 2014-05-05 | 2019-12-31 | Rempex Pharmaceuticals Inc | Sinteza boronatnih soli i njihove upotrebe |
| WO2015171398A1 (en) | 2014-05-05 | 2015-11-12 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
| US9511142B2 (en) | 2014-06-11 | 2016-12-06 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| US20150361108A1 (en) * | 2014-06-11 | 2015-12-17 | VenatoRx Pharmaceuticals, Inc. | Orally bioavailable beta-lactamase inhibitors |
| 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 |
| 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 |
| TWI759267B (zh) | 2015-07-02 | 2022-04-01 | 美商地平線罕見醫學製藥有限責任公司 | Ａｄｏ抗性半胱胺類似物及其用途 |
| WO2017044828A1 (en) | 2015-09-11 | 2017-03-16 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| WO2017100537A1 (en) | 2015-12-10 | 2017-06-15 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| 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 |
| EP3494121B1 (en) | 2016-08-04 | 2021-10-06 | Venatorx Pharmaceuticals, Inc. | Boron-containing compounds |
| JOP20190188A1 (ar) | 2017-02-01 | 2019-08-01 | Rempex Pharmaceuticals Inc | جهاز وعملية تدفق مستمرة لإنتاج مشتق حمض بورونيك |
| TW201841642A (zh) * | 2017-04-28 | 2018-12-01 | 日商大日本住友製藥股份有限公司 | 雜環衍生物 |
| EP3630783A4 (en) | 2017-05-26 | 2021-03-03 | Venatorx Pharmaceuticals, Inc. | PENICILLIN-BINDING PROTEIN INHIBITORS |
| US11332485B2 (en) | 2017-05-26 | 2022-05-17 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| WO2019009369A1 (ja) * | 2017-07-06 | 2019-01-10 | 大日本住友製薬株式会社 | イミン誘導体 |
| TW201906616A (zh) * | 2017-07-06 | 2019-02-16 | 日商大日本住友製藥股份有限公司 | 醯胺衍生物 |
| CA3078627A1 (en) | 2017-10-11 | 2019-04-18 | Qpex Biopharma, Inc. | Boronic acid derivatives and synthesis thereof |
| EP3781576B1 (en) | 2018-04-20 | 2024-06-12 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| KR102679411B1 (ko) * | 2018-04-27 | 2024-07-01 | 스미토모 파마 가부시키가이샤 | 옥소 치환 화합물 |
| WO2019226931A1 (en) | 2018-05-25 | 2019-11-28 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| AU2019386849B2 (en) * | 2018-11-29 | 2025-07-24 | VenatoRx Pharmaceuticals, Inc. | Combination compositions comprising a beta-lactamase inhibitor and uses thereof |
| TW202038941A (zh) * | 2018-12-28 | 2020-11-01 | 日商大日本住友製藥股份有限公司 | 烷基取代化合物 |
| US20230144152A1 (en) | 2019-06-19 | 2023-05-11 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| JP7550421B2 (ja) * | 2019-10-25 | 2024-09-13 | 住友ファーマ株式会社 | オキソ置換化合物からなる医薬 |
| WO2021079984A1 (ja) * | 2019-10-25 | 2021-04-29 | 大日本住友製薬株式会社 | 新規置換縮環型化合物 |
| KR20220156047A (ko) * | 2020-03-18 | 2022-11-24 | 큐펙스 바이오파마 인코포레이티드 | 보론산 유도체 및 이의 치료적 용도 |
Family Cites Families (89)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4194047A (en) | 1975-11-21 | 1980-03-18 | Merck & Co., Inc. | Substituted N-methylene derivatives of thienamycin |
| US4260543A (en) | 1978-07-03 | 1981-04-07 | Merck & Co., Inc. | Crystalline N-formimidoyl thienamycin |
| US4409214A (en) | 1979-11-19 | 1983-10-11 | Fujisawa Pharmaceutical, Co., Ltd. | 7-Acylamino-3-vinylcephalosporanic acid derivatives and processes for the preparation thereof |
| FR2573070B1 (fr) | 1984-11-13 | 1987-01-30 | Rhone Poulenc Sante | Procede de preparation de composes carbonyles |
| US4783443A (en) | 1986-03-03 | 1988-11-08 | The University Of Chicago | Amino acyl cephalosporin derivatives |
| US4822786A (en) | 1986-07-01 | 1989-04-18 | Kaken Pharmaceutical Co., Ltd. | Cephalosporin compounds, and antibacterial agents |
| ZA893284B (en) | 1988-05-04 | 1990-03-28 | Igen Inc | Peptide analogs and their use as haptens to elicit catalytic antibodies |
| US5442100A (en) | 1992-08-14 | 1995-08-15 | The Procter & Gamble Company | β-aminoalkyl and β-N-peptidylaminoalkyl boronic acids |
| US5888998A (en) | 1997-04-24 | 1999-03-30 | Synphar Laboratories, Inc. | 2-oxo-1-azetidine sulfonic acid derivatives as potent β-lactamase inhibitors |
| AU8140898A (en) | 1997-06-13 | 1998-12-30 | Northwestern University | Inhibitors of beta-lactamases and uses therefor |
| US6184363B1 (en) | 1997-06-13 | 2001-02-06 | Northwestern University | Inhibitors of β-lactamases and uses therefor |
| AU3124300A (en) | 1998-12-16 | 2000-07-03 | Northwestern University | Inhibitors of beta-lactamases and uses therefor |
| AU2190400A (en) | 1998-12-16 | 2000-07-03 | Northwestern University | Inhibitors of beta-lactamases and uses therefor |
| US6747030B1 (en) | 1999-09-25 | 2004-06-08 | Smithkline Beecham P.L.C. | Piperazine derivatives as 5-HT1B antagonists |
| CA2388077A1 (en) | 1999-10-28 | 2001-05-03 | James M. Balkovec | Novel succinic acid metallo-beta-lactamase inhibitors and their use in treating bacterial infections |
| WO2002022137A1 (en) | 2000-09-12 | 2002-03-21 | Shoichet Brian K | β-LACTAM ANALOGS AND USES THEREFOR |
| EP1322648B1 (en) | 2000-09-14 | 2005-06-29 | Pantherix Limited | 3-(heteroaryl acetamido)-2-oxo-azetidine-1-sulfonic acids derivatives as antibacterial agents |
| AU2002243508A1 (en) | 2001-01-10 | 2002-07-24 | Bristol-Myers Squibb Company Patent Department | Alpha-aminoboronic acids prepared by novel synthetic methods |
| DE10118698A1 (de) | 2001-04-17 | 2002-11-07 | Jerini Ag | Verfahren zur Immobilisierung und damit hergestellte Anordnungen von Verbindungen auf einer planaren Oberfläche |
| FR2835186B1 (fr) | 2002-01-28 | 2006-10-20 | Aventis Pharma Sa | Nouveaux composes heterocycliques, actifs comme inhibiteurs de beta-lactamases |
| JP2003229277A (ja) | 2002-02-04 | 2003-08-15 | Matsushita Electric Ind Co Ltd | 発光素子材料およびそれを用いた発光素子並びに装置 |
| AUPS065102A0 (en) | 2002-02-20 | 2002-03-14 | Unisearch Limited | Fluorous acetalation |
| CA2488785C (en) | 2002-09-11 | 2012-07-03 | Kureha Chemical Industry Company, Limited | Amine compound and use thereof |
| EP2325226A1 (en) | 2002-10-30 | 2011-05-25 | Sumitomo Chemical Company, Limited | Complex aryl copolymer compounds and polymer light emitting devices made by using the same |
| US7439253B2 (en) | 2002-12-06 | 2008-10-21 | Novexel | Heterocyclic compounds, their preparation and their use as medicaments, in particular as antibacterials and beta-lactamase inhibitors |
| US7271186B1 (en) | 2002-12-09 | 2007-09-18 | Northwestern University | Nanomolar β-lactamase inhibitors |
| AU2003300358A1 (en) | 2002-12-20 | 2004-07-22 | Migenix Corp. | Ligands of adenine nucleotide translocase (ant) and compositions and methods related thereto |
| TW200418791A (en) | 2003-01-23 | 2004-10-01 | Bristol Myers Squibb Co | Pharmaceutical compositions for inhibiting proteasome |
| JP4233365B2 (ja) | 2003-03-25 | 2009-03-04 | 三井化学株式会社 | アザジオール錯体化合物、及び該化合物を用いる光記録媒体 |
| US7842941B2 (en) | 2003-10-06 | 2010-11-30 | Sumitomo Chemical Company, Limited | Aromatic compound |
| BRPI0415185A (pt) | 2003-10-10 | 2006-11-28 | Pfizer Prod Inc | 2h-[1,2,4]triazol[4,3-a]pirazinas substituìdas como inibidores da gsk-3 |
| TW200600494A (en) | 2004-03-08 | 2006-01-01 | Chugai Pharmaceutical Co Ltd | Bisphenyl compounds useful as vitamin d3 receptor agonists |
| US20060019116A1 (en) | 2004-07-22 | 2006-01-26 | Eastman Kodak Company | White electroluminescent device with anthracene derivative host |
| TW200618820A (en) | 2004-11-05 | 2006-06-16 | Alza Corp | Liposome formulations of boronic acid compounds |
| US20060178357A1 (en) | 2005-02-10 | 2006-08-10 | Buynak John D | Chphalosporin-derived mercaptans as inhibitors of serine and metallo-beta-lactamases |
| AU2006214247C1 (en) | 2005-02-16 | 2012-11-08 | Anacor Pharmaceuticals, Llc | Boron-containing small molecules |
| CA2680693A1 (en) | 2005-02-22 | 2006-08-31 | Teva Pharmaceutical Industries Ltd. | Preparation of rosuvastatin |
| US9184428B2 (en) | 2005-03-15 | 2015-11-10 | Uchicago Argonne Llc | Non-aqueous electrolytes for lithium ion batteries |
| TW200734311A (en) | 2005-11-21 | 2007-09-16 | Astrazeneca Ab | New compounds |
| EP2484680B1 (en) | 2005-12-07 | 2013-06-26 | Basilea Pharmaceutica AG | Useful Combinations of Monobactam Antibiotics with beta-Lac-tamase Inhibitors |
| CA2642583C (en) | 2006-02-16 | 2016-08-23 | Anacor Pharmaceuticals, Inc. | Boron-containing small molecules as anti-inflammatory agents |
| AU2007300531A1 (en) | 2006-09-27 | 2008-04-03 | Merck Sharp & Dohme Corp. | Novel inhibitors of beta-lactamase |
| MX2009009918A (es) | 2007-03-23 | 2009-10-19 | Basilea Pharmaceutica Ag | Medicamentos combinados para el tratamiento de infecciones bacterianas. |
| GB0719366D0 (en) | 2007-10-03 | 2007-11-14 | Smithkline Beecham Corp | Compounds |
| BRPI0820532A2 (pt) * | 2007-11-13 | 2012-07-10 | Protez Pharmaceuticals Inc | inibidores de beta-lactamase |
| US20100120715A1 (en) | 2007-11-13 | 2010-05-13 | Burns Christopher J | Beta-lactamase inhibitors |
| JP5038509B2 (ja) | 2008-01-18 | 2012-10-03 | メルク・シャープ・エンド・ドーム・コーポレイション | β−ラクタマーゼ阻害剤 |
| US8129398B2 (en) | 2008-03-19 | 2012-03-06 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| EP2285384A4 (en) | 2008-05-12 | 2012-04-25 | Anacor Pharmaceuticals Inc | BORN SMALL MOLECULES |
| WO2009139834A1 (en) | 2008-05-13 | 2009-11-19 | Poniard Pharmaceuticals, Inc. | Bioactive compounds for treatment of cancer and neurodegenerative diseases |
| US20120046242A1 (en) | 2008-12-24 | 2012-02-23 | Massachusetts Institute Of Technology | Molecular activators of the wnt/beta-catenin pathway |
| WO2010097675A1 (en) | 2009-02-27 | 2010-09-02 | Dhanuka Laboratories Ltd. | An improved preparation process for cefpodoxime proxetil |
| US20100292185A1 (en) | 2009-05-12 | 2010-11-18 | Burns Christopher J | Beta-lactamase inhibitors |
| WO2010144338A1 (en) | 2009-06-08 | 2010-12-16 | Abraxis Bioscience, Llc | Triazine derivatives and their therapeutical applications |
| JP2013500974A (ja) | 2009-07-28 | 2013-01-10 | アナコール ファーマシューティカルズ，インコーポレイテッド | 三置換ホウ素含有分子 |
| WO2011103686A1 (en) | 2010-02-26 | 2011-09-01 | Viswanatha , Sundaramma | CEPHALOSPORIN DERIVATIVES USEFUL AS β-LACTAMASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF |
| EA029521B1 (ru) | 2010-03-31 | 2018-04-30 | Милленниум Фармасьютикалз, Инк. | Производные 1-амино-2-циклопропилэтилбороновой кислоты |
| US20110288063A1 (en) | 2010-05-19 | 2011-11-24 | Naeja Pharmaceutical Inc. | Novel fused bridged bicyclic heteroaryl substituted 6-alkylidene penems as potent beta-lactamase inhibitors |
| US8822516B2 (en) | 2010-06-10 | 2014-09-02 | Technion Research & Development Foundation Limited | Process for the preparation of iodides |
| RU2599791C2 (ru) | 2010-08-10 | 2016-10-20 | Ремпекс Фармасьютикэлз, Инч. | Циклические бороновые кислотно-эфирные производные и их использование в терапии |
| HUE027317T2 (en) | 2010-10-26 | 2016-10-28 | Mars Inc | Boronates as arginase inhibitors |
| TW201221518A (en) | 2010-11-18 | 2012-06-01 | Glaxo Group Ltd | Compounds |
| EP2487159A1 (en) | 2011-02-11 | 2012-08-15 | MSD Oss B.V. | RorgammaT inhibitors |
| EP2508506A1 (en) | 2011-04-08 | 2012-10-10 | LEK Pharmaceuticals d.d. | Preparation of sitagliptin intermediates |
| WO2013033461A1 (en) | 2011-08-31 | 2013-03-07 | Rempex Pharmaceuticals, Inc. | Heterocyclic boronic acid ester derivatives and therapeutic uses thereof |
| WO2013053372A1 (en) | 2011-10-13 | 2013-04-18 | Therabor Pharmaceuticals | Boronic acid inhibitors of beta-lactamases |
| WO2013056163A1 (en) | 2011-10-14 | 2013-04-18 | The Regents Of The University Of California | Beta-lactamase inhibitors |
| JP6129203B2 (ja) | 2011-12-22 | 2017-05-17 | アレス トレーディング ソシエテ アノニム | 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 |
| CA2862710A1 (en) | 2012-01-09 | 2013-07-18 | University Of Tromso | Therapeutic boron-containing compounds |
| EP2615080A1 (en) | 2012-01-12 | 2013-07-17 | LEK Pharmaceuticals d.d. | Preparation of Optically Pure ß-Amino Acid Type Active Pharmaceutical Ingredients and Intermediates thereof |
| EP2814483A2 (en) | 2012-02-15 | 2014-12-24 | Rempex Pharmaceuticals, Inc. | Methods of treating bacterial infections |
| 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 |
| 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 |
| 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 |
| US8999885B2 (en) | 2013-01-09 | 2015-04-07 | General Electric Company | Methods of activating charcoal resulting from biomass gasification |
| 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 |
| US9127024B2 (en) | 2013-03-15 | 2015-09-08 | Intrexon Corporation | Boron-containing diacylhydrazines |
| RS59488B1 (sr) | 2014-05-05 | 2019-12-31 | Rempex Pharmaceuticals Inc | Sinteza boronatnih soli i njihove upotrebe |
| WO2015171398A1 (en) | 2014-05-05 | 2015-11-12 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
| US9511142B2 (en) | 2014-06-11 | 2016-12-06 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| 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 |
| WO2016065282A1 (en) | 2014-10-24 | 2016-04-28 | The Regents Of The University Of Michigan | Nasal formulation, nasal kit, and method for enhancing nasal nitric oxide (no) levels |
| US20160339045A1 (en) | 2015-04-24 | 2016-11-24 | Rempex Pharmaceuticals, Inc. | Methods of treating bacterial infections |
-
2015
- 2015-05-18 JP JP2016568679A patent/JP6672176B2/ja active Active
- 2015-05-18 CN CN201580026757.0A patent/CN106459096B/zh active Active
- 2015-05-18 EP EP15796968.4A patent/EP3145936B1/en active Active
- 2015-05-18 AU AU2015264418A patent/AU2015264418A1/en not_active Abandoned
- 2015-05-18 WO PCT/US2015/031400 patent/WO2015179308A1/en not_active Ceased
- 2015-05-18 BR BR112016026291A patent/BR112016026291A2/pt not_active Application Discontinuation
- 2015-05-18 CA CA2947041A patent/CA2947041A1/en not_active Abandoned
- 2015-05-18 EA EA201691988A patent/EA201691988A1/ru unknown
- 2015-05-18 US US15/312,173 patent/US9963467B2/en active Active
- 2015-05-18 KR KR1020167035427A patent/KR20170007448A/ko not_active Withdrawn
- 2015-05-18 MX MX2016015093A patent/MX2016015093A/es unknown