JP2016509594A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2016509594A5 JP2016509594A5 JP2015551761A JP2015551761A JP2016509594A5 JP 2016509594 A5 JP2016509594 A5 JP 2016509594A5 JP 2015551761 A JP2015551761 A JP 2015551761A JP 2015551761 A JP2015551761 A JP 2015551761A JP 2016509594 A5 JP2016509594 A5 JP 2016509594A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- compound according
- pharmaceutically acceptable
- formula
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 21
- 125000000217 alkyl group Chemical group 0.000 claims 17
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000003795 chemical substances by application Substances 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- -1 amino, hydroxy Chemical group 0.000 claims 6
- 239000003242 anti bacterial agent Substances 0.000 claims 6
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 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
- QUKGLNCXGVWCJX-UHFFFAOYSA-N 1,3,4-thiadiazol-2-amine Chemical compound NC1=NN=CS1 QUKGLNCXGVWCJX-UHFFFAOYSA-N 0.000 claims 2
- OMAFFHIGWTVZOH-UHFFFAOYSA-N 1-methyltetrazole Chemical compound CN1C=NN=N1 OMAFFHIGWTVZOH-UHFFFAOYSA-N 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
- 208000035143 Bacterial infection Diseases 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
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-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
- 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
- 239000000654 additive Substances 0.000 claims 2
- 230000000996 additive effect Effects 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
- 239000003443 antiviral agent Substances 0.000 claims 2
- 125000003118 aryl group Chemical group 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
- 208000022362 bacterial infectious disease Diseases 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
- 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
- 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
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 229960002182 imipenem 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
- 229960002260 meropenem 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
- 229950011346 panipenem Drugs 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 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
- 229940124586 β-lactam antibiotics Drugs 0.000 claims 2
- 125000006545 (C1-C9) alkyl group Chemical group 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
- 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
- KLSJWNVTNUYHDU-UHFFFAOYSA-N Amitrole Chemical compound NC1=NC=NN1 KLSJWNVTNUYHDU-UHFFFAOYSA-N 0.000 claims 1
- 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 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
- 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
- 229950003476 aminothiazole Drugs 0.000 claims 1
- 239000003429 antifungal agent Substances 0.000 claims 1
- 229940121375 antifungal agent Drugs 0.000 claims 1
- 150000001540 azides Chemical class 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 229960002770 ertapenem Drugs 0.000 claims 1
- 230000002538 fungal effect Effects 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 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
- 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
- 150000003536 tetrazoles Chemical class 0.000 claims 1
- 150000003852 triazoles Chemical class 0.000 claims 1
- 0 CCOC(OC(C)OC(c1c2OB3*=C(CSC)N[C@]3Cc2ccc1)=O)=O Chemical compound CCOC(OC(C)OC(c1c2OB3*=C(CSC)N[C@]3Cc2ccc1)=O)=O 0.000 description 2
- VELHQRMGDOGMPM-UHFFFAOYSA-N CC(C)(C)C(OCOC(c(cccc1CC2NC(CSC)=O)c1OB2O)=O)=O Chemical compound CC(C)(C)C(OCOC(c(cccc1CC2NC(CSC)=O)c1OB2O)=O)=O VELHQRMGDOGMPM-UHFFFAOYSA-N 0.000 description 1
- WUQGISQYFIRBLU-ZDUSSCGKSA-N CC(C)OC(OCOC(c(cccc1C[C@@H]2NC(CSC)=O)c1OB2O)=O)=O Chemical compound CC(C)OC(OCOC(c(cccc1C[C@@H]2NC(CSC)=O)c1OB2O)=O)=O WUQGISQYFIRBLU-ZDUSSCGKSA-N 0.000 description 1
- IEYYFPPOBKZHPG-HNNXBMFYSA-N CCC(CC)C(OCOC(c(cccc1C[C@@H]2NC(CSC)=O)c1OB2O)=O)=O Chemical compound CCC(CC)C(OCOC(c(cccc1C[C@@H]2NC(CSC)=O)c1OB2O)=O)=O IEYYFPPOBKZHPG-HNNXBMFYSA-N 0.000 description 1
- JLXAZUMNJODWBO-ZDUSSCGKSA-N CCCC(OCOC(c(cccc1C[C@@H]2NC(CSC)=O)c1OB2O)=O)=O Chemical compound CCCC(OCOC(c(cccc1C[C@@H]2NC(CSC)=O)c1OB2O)=O)=O JLXAZUMNJODWBO-ZDUSSCGKSA-N 0.000 description 1
- GNWXQXUVACQZAY-VIFPVBQESA-N COB([C@H](Cc1ccc2)N/C(/c3nnc(N)[o]3)=[O]\C)Oc1c2C(O)=O Chemical compound COB([C@H](Cc1ccc2)N/C(/c3nnc(N)[o]3)=[O]\C)Oc1c2C(O)=O GNWXQXUVACQZAY-VIFPVBQESA-N 0.000 description 1
- QTNJTYOSJMJPKB-ZETCQYMHSA-N Nc1nnc(C(N[C@H]2Cc3cccc(C(O)=O)c3OB2O)=O)[s]1 Chemical compound Nc1nnc(C(N[C@H]2Cc3cccc(C(O)=O)c3OB2O)=O)[s]1 QTNJTYOSJMJPKB-ZETCQYMHSA-N 0.000 description 1
- ZZZBWSAVQFPOLP-LBPRGKRZSA-N OB([C@H](Cc1ccc2)NC(c3cc(F)cnc3)=O)Oc1c2C(O)=O Chemical compound OB([C@H](Cc1ccc2)NC(c3cc(F)cnc3)=O)Oc1c2C(O)=O ZZZBWSAVQFPOLP-LBPRGKRZSA-N 0.000 description 1
- OMCMDOYTIDGOJK-LBPRGKRZSA-N OB([C@H](Cc1ccc2)NC(c3cccnc3)=O)Oc1c2C(O)=O Chemical compound OB([C@H](Cc1ccc2)NC(c3cccnc3)=O)Oc1c2C(O)=O OMCMDOYTIDGOJK-LBPRGKRZSA-N 0.000 description 1
- OQGUPXPWULVSPM-NSHDSACASA-N OB([C@H](Cc1ccc2)NC(c3cncnc3)=O)Oc1c2C(O)=O Chemical compound OB([C@H](Cc1ccc2)NC(c3cncnc3)=O)Oc1c2C(O)=O OQGUPXPWULVSPM-NSHDSACASA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361749210P | 2013-01-04 | 2013-01-04 | |
| US61/749,210 | 2013-01-04 | ||
| US201361780828P | 2013-03-13 | 2013-03-13 | |
| US61/780,828 | 2013-03-13 | ||
| PCT/US2014/010106 WO2014107535A1 (en) | 2013-01-04 | 2014-01-02 | Boronic acid derivatives and therapeutic uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016509594A JP2016509594A (ja) | 2016-03-31 |
| JP2016509594A5 true JP2016509594A5 (cg-RX-API-DMAC7.html) | 2017-02-09 |
Family
ID=51061421
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015551761A Pending JP2016509594A (ja) | 2013-01-04 | 2014-01-02 | ボロン酸誘導体及びその治療的使用 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US9642869B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2941246A4 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2016509594A (cg-RX-API-DMAC7.html) |
| KR (1) | KR20150103269A (cg-RX-API-DMAC7.html) |
| CN (1) | CN104994844A (cg-RX-API-DMAC7.html) |
| AU (1) | AU2014204045B2 (cg-RX-API-DMAC7.html) |
| BR (1) | BR112015016001A2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2894891A1 (cg-RX-API-DMAC7.html) |
| EA (1) | EA201591003A1 (cg-RX-API-DMAC7.html) |
| MX (1) | MX2015008628A (cg-RX-API-DMAC7.html) |
| TW (1) | TW201431866A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2014107535A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE048859T2 (hu) | 2010-08-10 | 2020-08-28 | Rempex Pharmaceuticals Inc | Gyûrûs bórsavészter származékok, eljárás elõállításukra, és terápiás alkalmazásuk |
| WO2013033461A1 (en) | 2011-08-31 | 2013-03-07 | Rempex Pharmaceuticals, Inc. | Heterocyclic boronic acid ester derivatives and therapeutic uses thereof |
| WO2013074615A1 (en) | 2011-11-14 | 2013-05-23 | Yale University | Compositions and methods for modulating coagulation |
| US10561675B2 (en) | 2012-06-06 | 2020-02-18 | Rempex Pharmaceuticals, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| RU2654692C2 (ru) | 2012-12-07 | 2018-05-22 | Венаторкс Фармасьютикалс, Инк. | Ингибиторы бета-лактамаз |
| US9241947B2 (en) | 2013-01-04 | 2016-01-26 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| EA201591003A1 (ru) | 2013-01-04 | 2015-12-30 | Ремпекс Фармасьютикалз, Инк. | Производные бороновой кислоты и их терапевтическое применение |
| AU2014204046B2 (en) | 2013-01-04 | 2017-02-23 | 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 |
| PT3140310T (pt) | 2014-05-05 | 2019-11-18 | Rempex Pharmaceuticals Inc | Síntese de sais de boronato e utilizações dos mesmos |
| WO2015171398A1 (en) | 2014-05-05 | 2015-11-12 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
| BR112016026291A2 (pt) * | 2014-05-19 | 2017-08-15 | Rempex Pharmaceuticals Inc | Derivados do ácido borônico e usos terapêuticos dos mesmos |
| US9511142B2 (en) | 2014-06-11 | 2016-12-06 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| CA2950917C (en) | 2014-06-11 | 2022-08-23 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| MX2016016666A (es) * | 2014-07-01 | 2017-08-08 | Rempex Pharmaceuticals Inc | Derivados de acido boronico y usos terapeuticos de los mismos. |
| US10662205B2 (en) | 2014-11-18 | 2020-05-26 | Qpex Biopharma, 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 |
| EP3283492B1 (en) | 2015-04-14 | 2021-01-06 | B-organic Films Corp. | Antiviral and antibacteria agents based on quaternary ammonium compound complexed with boric acid and its derivatives |
| US10399996B2 (en) * | 2015-09-11 | 2019-09-03 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| WO2017100537A1 (en) | 2015-12-10 | 2017-06-15 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| CN105801610B (zh) * | 2016-04-19 | 2018-05-18 | 武汉维舜医药科技有限公司 | 新型广谱β-内酰胺酶抑制剂 |
| WO2017190043A1 (en) * | 2016-04-29 | 2017-11-02 | University Of Kansas | Cephalosporin-type compounds |
| SG11201811549UA (en) | 2016-06-30 | 2019-01-30 | Qpex Biopharma Inc | Boronic acid derivatives and therapeutic uses thereof |
| WO2018027062A1 (en) | 2016-08-04 | 2018-02-08 | 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 |
| CN110678186A (zh) | 2017-03-06 | 2020-01-10 | 维纳拓尔斯制药公司 | 包含β-内酰胺酶抑制剂的固体形式和组合式组合物及其用途 |
| CN110959008A (zh) * | 2017-05-26 | 2020-04-03 | 维纳拓尔斯制药公司 | 青霉素结合蛋白抑制剂 |
| WO2018218154A1 (en) * | 2017-05-26 | 2018-11-29 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| JP7511469B2 (ja) | 2017-09-27 | 2024-07-05 | イノザイム ファーマ， インコーポレイテッド | 組換えエクトヌクレオチドピロホスファターゼ／ホスホジエステラーゼ（ｎｐｐ１）を使用して心血管機能を改善し、心血管疾患を処置するための方法。 |
| CN111212843B (zh) | 2017-10-11 | 2025-05-16 | Qpex生物制药有限公司 | 硼酸衍生物及其合成 |
| JP7329260B2 (ja) | 2018-04-20 | 2023-08-18 | 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 |
| WO2019208797A1 (ja) | 2018-04-27 | 2019-10-31 | 大日本住友製薬株式会社 | オキソ置換化合物 |
| US12173018B2 (en) | 2018-05-25 | 2024-12-24 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| SG11202105505TA (en) * | 2018-11-29 | 2021-06-29 | Venatorx Pharmaceuticals Inc | Combination compositions comprising a beta-lactamase inhibitor and uses thereof |
| WO2020205932A1 (en) * | 2019-04-02 | 2020-10-08 | VenatoRx Pharmaceuticals, Inc. | Solid forms of an orally-delivered beta-lactamase inhibitor and uses thereof |
| JP7654554B2 (ja) | 2019-10-25 | 2025-04-01 | 住友ファーマ株式会社 | 新規置換縮環型化合物 |
| US20250340577A1 (en) * | 2021-03-02 | 2025-11-06 | Case Western Reserve University | Beta-lactomase inhibitors and uses thereof |
| CN113150022B (zh) * | 2021-04-23 | 2022-12-06 | 四川大学 | 3-取代五元环状硼酸酯衍生物及其药物组合物和制药用途 |
| WO2025119216A1 (zh) * | 2023-12-04 | 2025-06-12 | 珠海联邦制药股份有限公司 | 硼酸类β-内酰胺酶抑制剂及其制备方法和应用 |
Family Cites Families (85)
| 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 |
| FR2574070B1 (fr) | 1984-11-30 | 1987-02-27 | Stam | Catalyseur de prise de mortiers d'anhydrite projetes a la lance, a resistance amelioree a un stockage a temperature et humidite elevees, et utilisation d'un tel catalyseur |
| US4783443A (en) | 1986-03-03 | 1988-11-08 | The University Of Chicago | Amino acyl cephalosporin derivatives |
| CA1283404C (en) | 1986-07-01 | 1991-04-23 | Shigeru Sanai | Cephalosporin compounds, processes for their preparation 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 |
| US6184363B1 (en) | 1997-06-13 | 2001-02-06 | Northwestern University | Inhibitors of β-lactamases and uses therefor |
| WO1998056392A1 (en) | 1997-06-13 | 1998-12-17 | 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 |
| WO2000035905A1 (en) | 1998-12-16 | 2000-06-22 | Northwestern University | INHIBITORS OF β-LACTAMASES AND USES THEREFOR |
| ATE259363T1 (de) | 1999-09-25 | 2004-02-15 | Smithkline Beecham Plc | Piperazinderivate als 5-ht1b antagonisten |
| 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 |
| JP2004509122A (ja) | 2000-09-14 | 2004-03-25 | パンセリックス・リミテッド | 抗菌剤としての、３−（ヘテロアリールアセトアミド）−２−オキソ−アゼチジン−１−スルホン酸誘導体 |
| 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 |
| KR100863667B1 (ko) | 2002-09-11 | 2008-10-15 | 가부시끼가이샤 구레하 | 아민 화합물 및 그 용도 |
| AU2003268752A1 (en) | 2002-10-30 | 2004-05-25 | Sumitomo Chemical Company, Limited | High-molecular compounds and polymerer 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 |
| MXPA05006798A (es) | 2002-12-20 | 2006-03-09 | Migenix Corp | Ligandos de adenina nucleotido translocasa (ant) y composiciones y metodos relacionados a estos. |
| 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 |
| JP5038912B2 (ja) | 2005-02-16 | 2012-10-03 | 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 | ホウ素含有小分子 |
| PL1851206T3 (pl) | 2005-02-22 | 2013-01-31 | Teva Pharma | Rozuwastatyna i jej wolne od alkilenowych eterów sole oraz sposób ich wytwarzania |
| 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 |
| CN103724330B (zh) | 2005-12-07 | 2015-08-19 | 巴斯利尔药物股份公司 | 单环-内酰胺类抗生素与β-内酰胺酶抑制剂的有效的联合应用 |
| DK1988779T5 (en) | 2006-02-16 | 2016-10-10 | Anacor Pharmaceuticals Inc | SMALL boron MOLECULES AS ANTI-INFLAMMATORY AGENTS |
| US20100009957A1 (en) | 2006-09-27 | 2010-01-14 | Blizzard Timothy A | Novel inhibitors of beta-lactamase |
| US8486929B2 (en) | 2007-03-23 | 2013-07-16 | Basilea Pharmaceutica Ag | Combination medicaments for treating bacterial infections |
| GB0719366D0 (en) | 2007-10-03 | 2007-11-14 | Smithkline Beecham Corp | Compounds |
| US20100120715A1 (en) | 2007-11-13 | 2010-05-13 | Burns Christopher J | Beta-lactamase inhibitors |
| MX2010005252A (es) * | 2007-11-13 | 2011-04-11 | Novartis Int Pharm Ltd | Inhibidores de beta-lactamasa. |
| ES2533826T3 (es) | 2008-01-18 | 2015-04-15 | Merck Sharp & Dohme Corp. | Inhibidores de beta-lactamasa |
| US8129398B2 (en) | 2008-03-19 | 2012-03-06 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US20100256092A1 (en) | 2008-05-12 | 2010-10-07 | Anacor Pharmaceuticals, Inc. | Boron-containing small molecules |
| WO2009139834A1 (en) | 2008-05-13 | 2009-11-19 | Poniard Pharmaceuticals, Inc. | Bioactive compounds for treatment of cancer and neurodegenerative diseases |
| WO2010075286A1 (en) | 2008-12-24 | 2010-07-01 | University Of Washington | MOLECULAR ACTIVATORS OF THE Wnt/β-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 |
| CN102573485B (zh) | 2009-06-08 | 2014-11-26 | 加利福尼亚资本权益有限责任公司 | 三嗪衍生物及其治疗应用 |
| EP2458995A1 (en) | 2009-07-28 | 2012-06-06 | Anacor Pharmaceuticals, Inc. | Trisubstituted boron-containing molecules |
| 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 |
| HUE048859T2 (hu) | 2010-08-10 | 2020-08-28 | Rempex Pharmaceuticals Inc | Gyûrûs bórsavészter származékok, eljárás elõállításukra, és terápiás alkalmazásuk |
| AU2011320732B2 (en) | 2010-10-26 | 2018-07-05 | Mars Incorporated | Boronates as arginase inhibitors |
| AU2011329486A1 (en) | 2010-11-18 | 2013-04-18 | Glaxo Group Limited | 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 |
| EP2802593A1 (en) | 2012-01-09 | 2014-11-19 | The University of Tromsoe | 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 |
| US20150119363A1 (en) | 2012-02-15 | 2015-04-30 | 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 |
| RU2654692C2 (ru) * | 2012-12-07 | 2018-05-22 | Венаторкс Фармасьютикалс, Инк. | Ингибиторы бета-лактамаз |
| 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 |
| EA201591003A1 (ru) | 2013-01-04 | 2015-12-30 | Ремпекс Фармасьютикалз, Инк. | Производные бороновой кислоты и их терапевтическое применение |
| AU2014204046B2 (en) | 2013-01-04 | 2017-02-23 | 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 |
| WO2015171398A1 (en) | 2014-05-05 | 2015-11-12 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
| PT3140310T (pt) | 2014-05-05 | 2019-11-18 | Rempex Pharmaceuticals Inc | Síntese de sais de boronato e utilizações dos mesmos |
| BR112016026291A2 (pt) | 2014-05-19 | 2017-08-15 | Rempex Pharmaceuticals Inc | Derivados do ácido borônico e usos terapêuticos dos mesmos |
| MX2016016666A (es) | 2014-07-01 | 2017-08-08 | Rempex Pharmaceuticals Inc | Derivados de acido boronico y usos terapeuticos de los mismos. |
| 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 |
| CA2982911C (en) | 2015-04-24 | 2023-10-03 | Rempex Pharmaceuticals, Inc. | Methods of treating bacterial infections |
-
2014
- 2014-01-02 EA EA201591003A patent/EA201591003A1/ru unknown
- 2014-01-02 AU AU2014204045A patent/AU2014204045B2/en not_active Expired - Fee Related
- 2014-01-02 KR KR1020157021053A patent/KR20150103269A/ko not_active Withdrawn
- 2014-01-02 CA CA2894891A patent/CA2894891A1/en not_active Abandoned
- 2014-01-02 EP EP14735173.8A patent/EP2941246A4/en not_active Withdrawn
- 2014-01-02 US US14/146,671 patent/US9642869B2/en not_active Expired - Fee Related
- 2014-01-02 JP JP2015551761A patent/JP2016509594A/ja active Pending
- 2014-01-02 MX MX2015008628A patent/MX2015008628A/es unknown
- 2014-01-02 BR BR112015016001A patent/BR112015016001A2/pt not_active IP Right Cessation
- 2014-01-02 CN CN201480003981.3A patent/CN104994844A/zh active Pending
- 2014-01-02 WO PCT/US2014/010106 patent/WO2014107535A1/en not_active Ceased
- 2014-01-03 TW TW103100234A patent/TW201431866A/zh unknown