JP2016506419A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2016506419A5 JP2016506419A5 JP2015552833A JP2015552833A JP2016506419A5 JP 2016506419 A5 JP2016506419 A5 JP 2016506419A5 JP 2015552833 A JP2015552833 A JP 2015552833A JP 2015552833 A JP2015552833 A JP 2015552833A JP 2016506419 A5 JP2016506419 A5 JP 2016506419A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- heterocyclyl
- heteroaryl
- compound according
- compound
- 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 46
- 125000000623 heterocyclic group Chemical group 0.000 claims 33
- 125000001072 heteroaryl group Chemical group 0.000 claims 20
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- 150000002431 hydrogen Chemical class 0.000 claims 13
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 9
- 125000001153 fluoro group Chemical group F* 0.000 claims 9
- 125000001309 chloro group Chemical group Cl* 0.000 claims 8
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 7
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 6
- 125000001246 bromo group Chemical group Br* 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 239000000651 prodrug Substances 0.000 claims 5
- 229940002612 prodrug Drugs 0.000 claims 5
- -1 pyridin-1-yl Chemical group 0.000 claims 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 4
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 4
- 150000001204 N-oxides Chemical class 0.000 claims 4
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 4
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 4
- 239000003782 beta lactam antibiotic agent Substances 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 4
- XSCHRSMBECNVNS-UHFFFAOYSA-N quinoxaline Chemical compound N1=CC=NC2=CC=CC=C21 XSCHRSMBECNVNS-UHFFFAOYSA-N 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- 239000002132 β-lactam antibiotic Substances 0.000 claims 4
- 229940124586 β-lactam antibiotics Drugs 0.000 claims 4
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- 150000002923 oximes Chemical class 0.000 claims 3
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims 2
- LJMZRBZETLXDSO-UHFFFAOYSA-N 1h-thieno[3,2-c]pyrazole Chemical compound N1N=CC2=C1C=CS2 LJMZRBZETLXDSO-UHFFFAOYSA-N 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 208000035143 Bacterial infection Diseases 0.000 claims 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 2
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-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
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 2
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 2
- 125000002015 acyclic group Chemical group 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004429 atom 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
- IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical compound C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 2
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 2
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000002207 metabolite Substances 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 229930192474 thiophene Natural products 0.000 claims 2
- 150000003852 triazoles Chemical class 0.000 claims 2
- OWQPOVKKUWUEKE-UHFFFAOYSA-N 1,2,3-benzotriazine Chemical compound N1=NN=CC2=CC=CC=C21 OWQPOVKKUWUEKE-UHFFFAOYSA-N 0.000 claims 1
- JYEUMXHLPRZUAT-UHFFFAOYSA-N 1,2,3-triazine Chemical compound C1=CN=NN=C1 JYEUMXHLPRZUAT-UHFFFAOYSA-N 0.000 claims 1
- CSNIZNHTOVFARY-UHFFFAOYSA-N 1,2-benzothiazole Chemical compound C1=CC=C2C=NSC2=C1 CSNIZNHTOVFARY-UHFFFAOYSA-N 0.000 claims 1
- KTZQTRPPVKQPFO-UHFFFAOYSA-N 1,2-benzoxazole Chemical compound C1=CC=C2C=NOC2=C1 KTZQTRPPVKQPFO-UHFFFAOYSA-N 0.000 claims 1
- BCMCBBGGLRIHSE-UHFFFAOYSA-N 1,3-benzoxazole Chemical compound C1=CC=C2OC=NC2=C1 BCMCBBGGLRIHSE-UHFFFAOYSA-N 0.000 claims 1
- FLBAYUMRQUHISI-UHFFFAOYSA-N 1,8-naphthyridine Chemical compound N1=CC=CC2=CC=CN=C21 FLBAYUMRQUHISI-UHFFFAOYSA-N 0.000 claims 1
- AMFYRKOUWBAGHV-UHFFFAOYSA-N 1h-pyrazolo[4,3-b]pyridine Chemical compound C1=CN=C2C=NNC2=C1 AMFYRKOUWBAGHV-UHFFFAOYSA-N 0.000 claims 1
- RSEBUVRVKCANEP-UHFFFAOYSA-N 2-pyrroline Chemical compound C1CC=CN1 RSEBUVRVKCANEP-UHFFFAOYSA-N 0.000 claims 1
- GAMYYCRTACQSBR-UHFFFAOYSA-N 4-azabenzimidazole Chemical compound C1=CC=C2NC=NC2=N1 GAMYYCRTACQSBR-UHFFFAOYSA-N 0.000 claims 1
- KDOPAZIWBAHVJB-UHFFFAOYSA-N 5h-pyrrolo[3,2-d]pyrimidine Chemical compound C1=NC=C2NC=CC2=N1 KDOPAZIWBAHVJB-UHFFFAOYSA-N 0.000 claims 1
- 241000251169 Alopias vulpinus Species 0.000 claims 1
- 229930186147 Cephalosporin Natural products 0.000 claims 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- 229930182555 Penicillin Natural products 0.000 claims 1
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-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
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- WFIHKLWVLPBMIQ-UHFFFAOYSA-N [1,3]thiazolo[5,4-b]pyridine Chemical compound C1=CN=C2SC=NC2=C1 WFIHKLWVLPBMIQ-UHFFFAOYSA-N 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- RFRXIWQYSOIBDI-UHFFFAOYSA-N benzarone Chemical compound CCC=1OC2=CC=CC=C2C=1C(=O)C1=CC=C(O)C=C1 RFRXIWQYSOIBDI-UHFFFAOYSA-N 0.000 claims 1
- QRUDEWIWKLJBPS-UHFFFAOYSA-N benzotriazole Chemical compound C1=CC=C2N[N][N]C2=C1 QRUDEWIWKLJBPS-UHFFFAOYSA-N 0.000 claims 1
- 125000005621 boronate group Chemical group 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- YZBQHRLRFGPBSL-RXMQYKEDSA-N carbapenem Chemical compound C1C=CN2C(=O)C[C@H]21 YZBQHRLRFGPBSL-RXMQYKEDSA-N 0.000 claims 1
- 150000001720 carbohydrates Chemical class 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 229940124587 cephalosporin Drugs 0.000 claims 1
- 150000001780 cephalosporins Chemical class 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- WCZVZNOTHYJIEI-UHFFFAOYSA-N cinnoline Chemical compound N1=NC=CC2=CC=CC=C21 WCZVZNOTHYJIEI-UHFFFAOYSA-N 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 1
- 150000002500 ions Chemical class 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- ZLTPDFXIESTBQG-UHFFFAOYSA-N isothiazole Chemical compound C=1C=NSC=1 ZLTPDFXIESTBQG-UHFFFAOYSA-N 0.000 claims 1
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 229940049954 penicillin Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 1
- YEYHFKBVNARCNE-UHFFFAOYSA-N pyrido[2,3-b]pyrazine Chemical compound N1=CC=NC2=CC=CN=C21 YEYHFKBVNARCNE-UHFFFAOYSA-N 0.000 claims 1
- OHZYAOYVLLHTGW-UHFFFAOYSA-N pyrido[3,2-c]pyridazine Chemical compound C1=CN=NC2=CC=CN=C21 OHZYAOYVLLHTGW-UHFFFAOYSA-N 0.000 claims 1
- BWESROVQGZSBRX-UHFFFAOYSA-N pyrido[3,2-d]pyrimidine Chemical compound C1=NC=NC2=CC=CN=C21 BWESROVQGZSBRX-UHFFFAOYSA-N 0.000 claims 1
- ZVJHJDDKYZXRJI-UHFFFAOYSA-N pyrroline Natural products C1CC=NC1 ZVJHJDDKYZXRJI-UHFFFAOYSA-N 0.000 claims 1
- 125000001422 pyrrolinyl group Chemical group 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
- 125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361751161P | 2013-01-10 | 2013-01-10 | |
| US61/751,161 | 2013-01-10 | ||
| US201361783261P | 2013-03-14 | 2013-03-14 | |
| US61/783,261 | 2013-03-14 | ||
| PCT/US2014/011144 WO2014110442A1 (en) | 2013-01-10 | 2014-01-10 | Beta-lactamase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016506419A JP2016506419A (ja) | 2016-03-03 |
| JP2016506419A5 true JP2016506419A5 (enExample) | 2017-01-05 |
| JP6346904B2 JP6346904B2 (ja) | 2018-06-20 |
Family
ID=51061422
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015552833A Expired - Fee Related JP6346904B2 (ja) | 2013-01-10 | 2014-01-10 | ベータ−ラクタマーゼ阻害剤 |
Country Status (6)
| Country | Link |
|---|---|
| US (6) | US9403850B2 (enExample) |
| EP (1) | EP2943204B1 (enExample) |
| JP (1) | JP6346904B2 (enExample) |
| CN (1) | CN105101970B (enExample) |
| ES (1) | ES2730013T3 (enExample) |
| WO (1) | WO2014110442A1 (enExample) |
Families Citing this family (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL3412676T3 (pl) | 2010-08-10 | 2021-04-06 | Melinta Therapeutics, Inc. | Cykliczne pochodne estrowe kwasu boronowego, sposób otrzymywania oraz ich zastosowania terapeutyczne |
| WO2013033461A1 (en) | 2011-08-31 | 2013-03-07 | Rempex Pharmaceuticals, Inc. | Heterocyclic boronic acid ester 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 |
| PL2928898T3 (pl) | 2012-12-07 | 2021-10-25 | VenatoRx Pharmaceuticals, Inc. | Inhibitory beta-laktamaz |
| US9241947B2 (en) | 2013-01-04 | 2016-01-26 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| EP2941246A4 (en) * | 2013-01-04 | 2016-12-21 | Rempex Pharmaceuticals Inc | BORONIC ACID DERIVATIVES AND THEIR THERAPEUTIC USES |
| KR20150103270A (ko) | 2013-01-04 | 2015-09-09 | 렘펙스 파머수티클스 인코퍼레이티드 | 보론산 유도체 및 그의 치료적 용도 |
| US9101638B2 (en) | 2013-01-04 | 2015-08-11 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| ES2730013T3 (es) * | 2013-01-10 | 2019-11-07 | Venatorx Pharmaceuticals Inc | Inhibidores de betalactamasa |
| US9944658B2 (en) | 2013-03-14 | 2018-04-17 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| EP3527569B1 (en) | 2014-02-03 | 2021-08-25 | Vitae Pharmaceuticals, LLC | Dihydropyrrolopyridine inhibitors of ror-gamma for use in treating drye eye |
| US9687497B1 (en) | 2014-05-05 | 2017-06-27 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
| EP3140310B1 (en) | 2014-05-05 | 2019-08-07 | Rempex Pharmaceuticals, Inc. | Synthesis of boronate salts and uses thereof |
| AU2015264418A1 (en) | 2014-05-19 | 2016-11-10 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| ES2874579T3 (es) | 2014-06-11 | 2021-11-05 | Venatorx Pharmaceuticals Inc | Inhibidores de betalactamasa |
| 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 |
| US10206937B2 (en) | 2014-07-01 | 2019-02-19 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| LT6177B (lt) | 2014-10-10 | 2015-07-27 | Uab "Biocentras" | Fermentų kompleksų išskyrimas iš steptomyces gougerotii 101, daugiafermentinių biopreparatų ruošimas bei taikymas |
| WO2016081297A1 (en) | 2014-11-18 | 2016-05-26 | Rempex Pharmaceuticals, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| US10364257B2 (en) | 2014-12-19 | 2019-07-30 | Rempex Pharmaceuticals, Inc. | Apparatus and continuous flow process for production of boronic acid derivatives |
| WO2016126726A1 (en) | 2015-02-02 | 2016-08-11 | Forma Therapeutics, Inc. | Bicyclic [4,6,0] hydroxamic acids as hdac6 inhibitors |
| WO2016126721A1 (en) | 2015-02-02 | 2016-08-11 | Forma Therapeutics, Inc. | 3-aryl-bicyclic [4,5,0] hydroxamic acids as hdac inhibitors |
| US20180051041A1 (en) | 2015-03-17 | 2018-02-22 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| CN108472284A (zh) | 2015-09-11 | 2018-08-31 | 维纳拓尔斯制药公司 | β-内酰胺酶抑制剂 |
| EP3868750A1 (en) | 2015-11-20 | 2021-08-25 | Vitae Pharmaceuticals, LLC | Modulators of ror-gamma |
| 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 |
| EP3472131B1 (en) | 2016-06-17 | 2020-02-19 | Forma Therapeutics, Inc. | 2-spiro-5- and 6-hydroxamic acid indanes as hdac inhibitors |
| MY196909A (en) | 2016-06-30 | 2023-05-09 | Qpex Biopharma Inc | Boronic acid derivatives and therapeutic uses thereof |
| US10889600B2 (en) | 2016-08-04 | 2021-01-12 | VenatoRx Pharmaceuticals, Inc. | Boron-containing compounds |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| CA3036250C (en) * | 2016-09-14 | 2023-09-26 | Yufeng Jane Tseng | Novel substituted benzimidazole derivatives as d-amino acid oxidase (daao) inhibitors |
| US10201518B2 (en) | 2016-09-28 | 2019-02-12 | The University Of Hong Kong | Bismuth(III) compounds and methods thereof |
| WO2018134127A1 (en) | 2017-01-23 | 2018-07-26 | Basf Se | Fungicidal pyridine compounds |
| PL3592362T3 (pl) | 2017-03-06 | 2025-06-23 | VenatoRx Pharmaceuticals, Inc. | Postacie stałe i kompozycje skojarzone zawierające inhibitor beta-laktamaz i ich zastosowania |
| WO2018199291A1 (ja) * | 2017-04-28 | 2018-11-01 | 大日本住友製薬株式会社 | ヘテロ環誘導体 |
| EP3630782A4 (en) | 2017-05-26 | 2021-03-03 | Venatorx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| US11267826B2 (en) | 2017-05-26 | 2022-03-08 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| WO2019018975A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF ROR GAMMA |
| MA49685A (fr) | 2017-07-24 | 2021-04-14 | Vitae Pharmaceuticals Llc | INHIBITEURS DE ROR gamma |
| CN107607572B (zh) * | 2017-09-15 | 2019-12-03 | 山东大学齐鲁医院 | 一种用于离体细胞水溶性代谢物的二维核磁共振检测方法 |
| EP3694864B1 (en) | 2017-10-11 | 2025-03-05 | Qpex Biopharma, Inc. | Boronic acid derivatives and synthesis thereof |
| WO2019100106A1 (en) * | 2017-11-24 | 2019-05-31 | The University Of Sydney | Antibacterial compounds and methods of use thereof |
| US11613549B2 (en) | 2018-01-23 | 2023-03-28 | Basf Se | Bromination of pyridine derivatives |
| KR102526964B1 (ko) | 2018-02-26 | 2023-04-28 | 길리애드 사이언시즈, 인코포레이티드 | Hbv 복제 억제제로서의 치환된 피롤리진 화합물 |
| AU2019256351B2 (en) | 2018-04-20 | 2024-02-29 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| CN118638140A (zh) | 2018-04-27 | 2024-09-13 | 住友制药株式会社 | 氧代取代化合物 |
| CA3003032A1 (en) * | 2018-04-27 | 2019-10-27 | Nanostics Inc. | Methods of diagnosing disease using microflow cytometry |
| EP3802551A4 (en) | 2018-05-25 | 2022-03-02 | Venatorx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| EP3886798B1 (en) | 2018-11-29 | 2026-01-28 | Venatorx Pharmaceuticals, Inc. | Combination compositions comprising a beta-lactamase inhibitor and 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 |
| WO2021108023A1 (en) * | 2019-11-26 | 2021-06-03 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| CN111254091B (zh) * | 2020-01-20 | 2022-04-19 | 浙江工业大学 | 一种嗜麦芽窄食单胞菌gyh及其在降解氯代烃类污染物中的应用 |
| US12552815B2 (en) | 2020-05-05 | 2026-02-17 | Qpex Biopharma, Inc. | Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof |
| IL298324A (en) | 2020-06-10 | 2023-01-01 | Aligos Therapeutics Inc | Anti-viral compounds for treating coronavirus, picornavirus, and norovirus infections |
| US12606573B2 (en) | 2020-10-07 | 2026-04-21 | VenatoRx Pharmaceuticals, Inc. | Process for boron-containing compounds |
| IL294231A (en) * | 2021-06-23 | 2023-01-01 | Yoda Pharmaceuticals Inc | Benzimidazole derivatives for treatment and/or prevention of diseases and disorders mediated by nlrp3 |
| CA3224494A1 (en) | 2021-07-09 | 2023-01-12 | Koen Vandyck | Anti-viral compounds |
| WO2023043816A1 (en) | 2021-09-17 | 2023-03-23 | Aligos Therapeutics, Inc. | Anti-viral compounds for treating coronavirus, picornavirus, and norovirus infections |
| TW202529745A (zh) | 2023-11-21 | 2025-08-01 | 美商維納拓爾斯製藥公司 | 經口遞送之β-內醯胺酶抑制劑之檸檬酸鹽配位錯合物及其用途 |
| 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 |
| US20250332181A1 (en) * | 2024-04-30 | 2025-10-30 | Ai Bio Discovery Llc | Antibiotic methods and compositions |
Family Cites Families (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IE41109B1 (en) | 1974-04-20 | 1979-10-24 | Beecham Group Ltd | Novel -lactam antibiotic from streptomyces clavuligerus |
| KR20020088406A (ko) | 1999-09-17 | 2002-11-27 | 애보트 게엠베하 운트 콤파니 카게 | 치료제로서의 피라졸로피리미딘 |
| US7271186B1 (en) | 2002-12-09 | 2007-09-18 | Northwestern University | Nanomolar β-lactamase inhibitors |
| WO2005004799A2 (en) | 2003-06-10 | 2005-01-20 | Fulcrum Pharmaceuticals, Inc. | β-LACTAMASE INHIBITORS AND METHODS OF USE THEREOF |
| RS53259B (sr) | 2004-03-30 | 2014-08-29 | Millennium Pharmaceuticals Inc. | Sinteza bortezomiba |
| CN1965838A (zh) | 2005-11-17 | 2007-05-23 | 李海超 | 含头孢匹胺和β－内酰胺酶抑制剂的药物组合物 |
| ATE529111T1 (de) | 2005-12-07 | 2011-11-15 | Basilea Pharmaceutica Ag | Nützliche monobactam-antibiotika |
| US20100120715A1 (en) * | 2007-11-13 | 2010-05-13 | Burns Christopher J | Beta-lactamase inhibitors |
| CN101983203A (zh) | 2007-11-13 | 2011-03-02 | 诺瓦提斯国际药物有限公司 | β-内酰胺酶抑制剂 |
| MY162532A (en) | 2008-01-18 | 2017-06-15 | Merck Sharp & Dohme | Beta-lactamase inhibitors |
| US20100292185A1 (en) | 2009-05-12 | 2010-11-18 | Burns Christopher J | Beta-lactamase inhibitors |
| KR20130031233A (ko) | 2009-07-28 | 2013-03-28 | 아나코르 파마슈티칼스 인코포레이티드 | 삼치환된 붕소 함유 분자 |
| PL3412676T3 (pl) | 2010-08-10 | 2021-04-06 | Melinta Therapeutics, Inc. | Cykliczne pochodne estrowe kwasu boronowego, sposób otrzymywania oraz ich zastosowania terapeutyczne |
| MX362683B (es) | 2011-07-26 | 2019-01-31 | Wockhardt Ltd | Composiciones farmacéuticas que comprenden antibiótico de beta-lactama, sulbactama e inhibidor de beta-lactamasa. |
| WO2013053372A1 (en) | 2011-10-13 | 2013-04-18 | Therabor Pharmaceuticals | Boronic acid inhibitors of beta-lactamases |
| US9688702B2 (en) | 2011-12-22 | 2017-06-27 | Ares Trading | Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors |
| EP2814483A2 (en) | 2012-02-15 | 2014-12-24 | Rempex Pharmaceuticals, Inc. | Methods of treating bacterial infections |
| BR112015012909A2 (pt) | 2012-12-03 | 2017-07-11 | Hoffmann La Roche | compostos de ácido borônico de triazol substituído |
| PL2928898T3 (pl) | 2012-12-07 | 2021-10-25 | VenatoRx Pharmaceuticals, Inc. | Inhibitory beta-laktamaz |
| EP2941246A4 (en) | 2013-01-04 | 2016-12-21 | Rempex Pharmaceuticals Inc | BORONIC ACID DERIVATIVES AND THEIR THERAPEUTIC USES |
| KR20150103270A (ko) | 2013-01-04 | 2015-09-09 | 렘펙스 파머수티클스 인코퍼레이티드 | 보론산 유도체 및 그의 치료적 용도 |
| US9101638B2 (en) * | 2013-01-04 | 2015-08-11 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| ES2730013T3 (es) | 2013-01-10 | 2019-11-07 | Venatorx Pharmaceuticals Inc | Inhibidores de betalactamasa |
| US9944658B2 (en) | 2013-03-14 | 2018-04-17 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| US9938291B2 (en) | 2013-03-14 | 2018-04-10 | The Trustess Of Columbia University In The City Of New York | N-alkyl-2-phenoxyethanamines, their preparation and use |
| WO2015051101A1 (en) | 2013-10-02 | 2015-04-09 | Cubist Pharmaceuticals, Inc. | B-lactamase inhibitor picoline salt |
| WO2015157618A1 (en) | 2014-04-11 | 2015-10-15 | The Texas A&M University System | Novel inhibitors of the new delhi metallo beta lactamase (ndm-1) |
| AU2015264418A1 (en) * | 2014-05-19 | 2016-11-10 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| US9511142B2 (en) | 2014-06-11 | 2016-12-06 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| ES2874579T3 (es) | 2014-06-11 | 2021-11-05 | Venatorx Pharmaceuticals Inc | Inhibidores de betalactamasa |
| US20150361107A1 (en) | 2014-06-11 | 2015-12-17 | VenatoRx Pharmaceuticals, Inc. | Orally bioavailable beta-lactamase inhibitors |
| US20150361108A1 (en) * | 2014-06-11 | 2015-12-17 | VenatoRx Pharmaceuticals, Inc. | Orally bioavailable beta-lactamase inhibitors |
| US10206937B2 (en) * | 2014-07-01 | 2019-02-19 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| US10364257B2 (en) | 2014-12-19 | 2019-07-30 | Rempex Pharmaceuticals, Inc. | Apparatus and continuous flow process for production of boronic acid derivatives |
| CN108472284A (zh) * | 2015-09-11 | 2018-08-31 | 维纳拓尔斯制药公司 | β-内酰胺酶抑制剂 |
| 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 |
| MY196909A (en) | 2016-06-30 | 2023-05-09 | Qpex Biopharma Inc | Boronic acid derivatives and therapeutic uses thereof |
| US10889600B2 (en) | 2016-08-04 | 2021-01-12 | VenatoRx Pharmaceuticals, Inc. | Boron-containing compounds |
| PL3592362T3 (pl) | 2017-03-06 | 2025-06-23 | VenatoRx Pharmaceuticals, Inc. | Postacie stałe i kompozycje skojarzone zawierające inhibitor beta-laktamaz i ich zastosowania |
| EP3630782A4 (en) | 2017-05-26 | 2021-03-03 | Venatorx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| US11267826B2 (en) | 2017-05-26 | 2022-03-08 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| WO2019118358A1 (en) | 2017-12-11 | 2019-06-20 | VenatoRx Pharmaceuticals, Inc. | Hepatitis b capsid assembly modulators |
| EP3802551A4 (en) | 2018-05-25 | 2022-03-02 | Venatorx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| CN112513043A (zh) | 2018-05-30 | 2021-03-16 | 维纳拓尔斯制药公司 | 广谱碳青霉烯 |
| KR20210019489A (ko) | 2018-06-11 | 2021-02-22 | 베나토알엑스 파마슈티컬스, 인크. | B형 간염 캡시드 조립 조절제 |
| WO2020056048A1 (en) | 2018-09-12 | 2020-03-19 | VenatoRx Pharmaceuticals, Inc. | Combination compositions comprising a beta-lactamase inhibitor |
| EP3886798B1 (en) | 2018-11-29 | 2026-01-28 | Venatorx Pharmaceuticals, Inc. | Combination compositions comprising a beta-lactamase inhibitor and uses thereof |
| AU2020256179A1 (en) | 2019-04-02 | 2021-11-18 | VenatoRx Pharmaceuticals, Inc. | Solid forms of an orally-delivered beta-lactamase inhibitor and uses thereof |
-
2014
- 2014-01-10 ES ES14737623T patent/ES2730013T3/es active Active
- 2014-01-10 US US14/759,853 patent/US9403850B2/en not_active Expired - Fee Related
- 2014-01-10 WO PCT/US2014/011144 patent/WO2014110442A1/en not_active Ceased
- 2014-01-10 US US14/152,916 patent/US9040504B2/en not_active Expired - Fee Related
- 2014-01-10 EP EP14737623.0A patent/EP2943204B1/en active Active
- 2014-01-10 JP JP2015552833A patent/JP6346904B2/ja not_active Expired - Fee Related
- 2014-01-10 CN CN201480013394.2A patent/CN105101970B/zh not_active Expired - Fee Related
-
2015
- 2015-04-22 US US14/693,318 patent/US9376454B2/en not_active Expired - Fee Related
-
2016
- 2016-06-27 US US15/194,433 patent/US9771382B2/en not_active Expired - Fee Related
-
2017
- 2017-08-11 US US15/675,262 patent/US10125152B2/en active Active
-
2020
- 2020-05-01 US US16/864,634 patent/US11414435B2/en active Active