JP2018526391A5 - - Google Patents
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- Publication number
- JP2018526391A5 JP2018526391A5 JP2018511713A JP2018511713A JP2018526391A5 JP 2018526391 A5 JP2018526391 A5 JP 2018526391A5 JP 2018511713 A JP2018511713 A JP 2018511713A JP 2018511713 A JP2018511713 A JP 2018511713A JP 2018526391 A5 JP2018526391 A5 JP 2018526391A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- hydroxy
- methylsulfonyl
- oxo
- pyrrolo
- 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.)
- Ceased
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- -1 3-fluoroazetidin-3-yl Chemical group 0.000 claims 232
- 150000001875 compounds Chemical class 0.000 claims 32
- 150000003839 salts Chemical class 0.000 claims 18
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 15
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 7
- 229910052731 fluorine Chemical group 0.000 claims 7
- 239000011737 fluorine Chemical group 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- DNSISZSEWVHGLH-UHFFFAOYSA-N butanamide Chemical compound CCCC(N)=O DNSISZSEWVHGLH-UHFFFAOYSA-N 0.000 claims 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 3
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 3
- GMWFCJXSQQHBPI-UHFFFAOYSA-N azetidin-3-ol Chemical compound OC1CNC1 GMWFCJXSQQHBPI-UHFFFAOYSA-N 0.000 claims 3
- 125000004567 azetidin-3-yl group Chemical group N1CC(C1)* 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000006299 oxetan-3-yl group Chemical group [H]C1([H])OC([H])([H])C1([H])* 0.000 claims 3
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 2
- PWPJWHXPIKDVAY-UHFFFAOYSA-N methyl 4-methylpiperazine-1-carboxylate Chemical compound COC(=O)N1CCN(C)CC1 PWPJWHXPIKDVAY-UHFFFAOYSA-N 0.000 claims 2
- 238000011282 treatment Methods 0.000 claims 2
- 125000004484 1-methylpiperidin-4-yl group Chemical group CN1CCC(CC1)* 0.000 claims 1
- SNBYDHCSBZIOQL-UHFFFAOYSA-N 3-hydroxyazetidine-1-carboxylic acid Chemical compound OC1CN(C(O)=O)C1 SNBYDHCSBZIOQL-UHFFFAOYSA-N 0.000 claims 1
- OHZUEFKOZYWUFF-UHFFFAOYSA-N 4-hydroxypiperidine-1-carboxylic acid Chemical compound OC1CCN(C(O)=O)CC1 OHZUEFKOZYWUFF-UHFFFAOYSA-N 0.000 claims 1
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- KNWWGBNAUNTSRV-UHFFFAOYSA-N 4-methylpiperazine-1-carboxylic acid Chemical compound CN1CCN(C(O)=O)CC1 KNWWGBNAUNTSRV-UHFFFAOYSA-N 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-M dihydrogenphosphate Chemical compound OP(O)([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-M 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 1
- 208000027096 gram-negative bacterial infections Diseases 0.000 claims 1
- PDCPSVRSNHMDJH-UHFFFAOYSA-N methyl 3-hydroxyazetidine-1-carboxylate Chemical compound COC(=O)N1CC(O)C1 PDCPSVRSNHMDJH-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 125000006300 thietan-3-yl group Chemical group [H]C1([H])SC([H])([H])C1([H])* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP2015070144 | 2015-09-03 | ||
| EPPCT/EP2015/070144 | 2015-09-03 | ||
| PCT/EP2016/070695 WO2017037221A1 (en) | 2015-09-03 | 2016-09-02 | Substituted 1,2-dihydro-3h-pyrrolo[1,2-c]imidazol-3-one antibacterial compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018526391A JP2018526391A (ja) | 2018-09-13 |
| JP2018526391A5 true JP2018526391A5 (cg-RX-API-DMAC10.html) | 2019-10-10 |
Family
ID=56852279
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018511713A Ceased JP2018526391A (ja) | 2015-09-03 | 2016-09-02 | 置換１，２−ジヒドロ−３Ｈ−ピロロ［１，２−ｃ］イミダゾール−３−オン抗菌性化合物 |
Country Status (17)
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR099612A1 (es) | 2014-03-04 | 2016-08-03 | Actelion Pharmaceuticals Ltd | Derivados antibacterianos de 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona |
| AR105646A1 (es) | 2015-08-11 | 2017-10-25 | Actelion Pharmaceuticals Ltd | Agentes antibacterianos de 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituida |
| TW201840569A (zh) * | 2017-03-01 | 2018-11-16 | 瑞士商愛杜西亞製藥有限公司 | (2r)-n-羥基-4-(6-((1-(2-羥基乙基)氮雜環丁烷-3-基)丁-1,3-二炔-1-基)-3-氧基-1h-吡咯并[1,2-c]咪唑-2(3h)-基)-2-甲基-2-(甲磺醯基)丁醯胺之結晶形式 |
| WO2018224455A1 (en) | 2017-06-07 | 2018-12-13 | Basf Se | Substituted cyclopropyl derivatives |
| WO2019038362A1 (en) | 2017-08-24 | 2019-02-28 | Idorsia Pharmaceuticals Ltd | ANTIBACTERIAL PYRROLOIMIDAZOLONES |
| WO2019086452A1 (en) | 2017-10-31 | 2019-05-09 | Idorsia Pharmaceuticals Ltd | Antibacterial heteroaromatic compounds |
| WO2019121143A1 (en) | 2017-12-20 | 2019-06-27 | Basf Se | Substituted cyclopropyl derivatives |
| JP7156199B2 (ja) * | 2018-08-09 | 2022-10-19 | 信越化学工業株式会社 | レジスト材料及びパターン形成方法 |
| US11458149B1 (en) | 2019-05-31 | 2022-10-04 | Ikena Oncology, Inc. | TEAD inhibitors and uses thereof |
| BR112021024108A2 (pt) | 2019-05-31 | 2022-03-22 | Ikena Oncology Inc | Inibidores de tead e usos dos mesmos |
| US12703680B2 (en) | 2019-11-21 | 2026-08-11 | University Of Utah Research Foundation | TRPV4 receptor ligands |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG2013013339A (en) | 2002-03-13 | 2014-12-30 | Array Biopharma Inc | N3 alkylated benzimidazole derivatives as mek inhibitors |
| UA80500C2 (en) | 2003-10-17 | 2007-09-25 | Basf Ag | Fungicidal mixture and agent for controlling rice pathogens, containing triazolopyrimidine derivative and metalaxyl-m, method for controlling rice pathogens and sowing material |
| DE102008044132A1 (de) | 2008-11-27 | 2010-06-02 | BSH Bosch und Siemens Hausgeräte GmbH | Kältegerät mit zweiseitig anschlagbarer Tür |
| CA2774250C (en) | 2009-10-13 | 2013-12-17 | Pfizer Inc. | C-linked hydroxamic acid derivatives useful as antibacterial agents |
| JP5793766B2 (ja) | 2009-12-16 | 2015-10-14 | ファイザー・インク | 抗菌剤として有用なｎ−結合型ヒドロキサム酸誘導体 |
| KR20120079015A (ko) | 2011-01-03 | 2012-07-11 | 한미약품 주식회사 | Ｇ 단백질-커플링된 수용체의 조절을 위한 신규한 비사이클릭 화합물 |
| AP3336A (en) | 2011-03-07 | 2015-07-31 | Pfizer | Fluoro-pyridinone derivatives useful as antibacterial agents |
| WO2012137099A1 (en) | 2011-04-08 | 2012-10-11 | Pfizer Inc. | Imidazole, pyrazole, and triazole derivatives useful as antibacterial agents |
| WO2012137094A1 (en) | 2011-04-08 | 2012-10-11 | Pfizer Inc. | Isoxazole derivatives useful as antibacterial agents |
| WO2013170165A1 (en) | 2012-05-10 | 2013-11-14 | Achaogen, Inc. | Antibacterial agents |
| EA201590953A1 (ru) | 2012-11-16 | 2015-08-31 | Бристол-Майерс Сквибб Компани | Пирролидиновые модуляторы gpr40 |
| WO2014165075A1 (en) | 2013-03-12 | 2014-10-09 | Achaogen, Inc. | Antibacterial agents |
| AR097617A1 (es) * | 2013-09-13 | 2016-04-06 | Actelion Pharmaceuticals Ltd | Derivados antibacterianos del 2h-indazol |
| WO2015066413A1 (en) | 2013-11-01 | 2015-05-07 | Novartis Ag | Oxazolidinone hydroxamic acid compounds for the treatment of bacterial infections |
| KR20160098503A (ko) | 2013-12-19 | 2016-08-18 | 액테리온 파마슈티칼 리미티드 | 항균성 1h-인다졸 및 1h-인돌 유도체 |
| AR099612A1 (es) * | 2014-03-04 | 2016-08-03 | Actelion Pharmaceuticals Ltd | Derivados antibacterianos de 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona |
| WO2015173329A1 (en) | 2014-05-16 | 2015-11-19 | Actelion Pharmaceuticals Ltd | Antibacterial quinazoline-4(3h)-one derivatives |
| BR112017010474A2 (pt) | 2014-11-19 | 2017-12-26 | Actelion Pharmaceuticals Ltd | derivados antibacterianos de benzotiazol |
| AR105646A1 (es) | 2015-08-11 | 2017-10-25 | Actelion Pharmaceuticals Ltd | Agentes antibacterianos de 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituida |
| AR105839A1 (es) | 2015-08-28 | 2017-11-15 | Actelion Pharmaceuticals Ltd | Derivados antibacterianos pirrolidin-2-ona anulares |
| AR105848A1 (es) | 2015-08-31 | 2017-11-15 | Actelion Pharmaceuticals Ltd | Derivados heterocíclicos antibacterianos |
| WO2017098440A1 (en) | 2015-12-08 | 2017-06-15 | Glaxosmithkline Intellectual Property Development Limited | Substituted benzazinones as antibacterial compounds |
| AU2017267194A1 (en) | 2016-05-17 | 2019-01-17 | Idorsia Pharmaceuticals Ltd | 6-(BUTA-1,3-DIYN-1-YL)benzo[D]thiazole derivatives |
-
2016
- 2016-09-01 AR ARP160102671A patent/AR105889A1/es unknown
- 2016-09-02 CA CA2994996A patent/CA2994996A1/en not_active Abandoned
- 2016-09-02 AU AU2016313794A patent/AU2016313794B2/en not_active Expired - Fee Related
- 2016-09-02 MX MX2018002644A patent/MX2018002644A/es unknown
- 2016-09-02 KR KR1020187009472A patent/KR20180049017A/ko not_active Withdrawn
- 2016-09-02 EP EP16759792.1A patent/EP3344630B1/en not_active Not-in-force
- 2016-09-02 WO PCT/EP2016/070695 patent/WO2017037221A1/en not_active Ceased
- 2016-09-02 US US15/756,366 patent/US10314823B2/en not_active Expired - Fee Related
- 2016-09-02 CN CN201680049395.1A patent/CN108137596A/zh active Pending
- 2016-09-02 TW TW105128540A patent/TW201714885A/zh unknown
- 2016-09-02 JP JP2018511713A patent/JP2018526391A/ja not_active Ceased
- 2016-09-02 HK HK18115746.5A patent/HK1256614A1/zh unknown
- 2016-09-02 EA EA201890626A patent/EA201890626A1/ru unknown
- 2016-09-02 BR BR112018004343-5A patent/BR112018004343A2/pt not_active Application Discontinuation
-
2018
- 2018-02-13 PH PH12018500323A patent/PH12018500323A1/en unknown
- 2018-02-27 IL IL257757A patent/IL257757A/en unknown
- 2018-02-28 CL CL2018000533A patent/CL2018000533A1/es unknown
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