JP2017508746A5 - - Google Patents
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- Publication number
- JP2017508746A5 JP2017508746A5 JP2016555488A JP2016555488A JP2017508746A5 JP 2017508746 A5 JP2017508746 A5 JP 2017508746A5 JP 2016555488 A JP2016555488 A JP 2016555488A JP 2016555488 A JP2016555488 A JP 2016555488A JP 2017508746 A5 JP2017508746 A5 JP 2017508746A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- hydroxy
- oxo
- pyrrolo
- methylsulfonyl
- 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
- -1 1,2-dihydroxyethyl Chemical group 0.000 claims description 237
- 150000001875 compounds Chemical class 0.000 claims description 32
- 150000003839 salts Chemical class 0.000 claims description 16
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims description 6
- GTCAXTIRRLKXRU-UHFFFAOYSA-N carbamic acid methyl ester Natural products COC(N)=O GTCAXTIRRLKXRU-UHFFFAOYSA-N 0.000 claims description 4
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 2
- 125000005504 styryl group Chemical group 0.000 claims description 2
- 125000003545 alkoxy group Chemical group 0.000 claims 10
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 4
- TZGPACAKMCUCKX-UHFFFAOYSA-N 2-hydroxyacetamide Chemical compound NC(=O)CO TZGPACAKMCUCKX-UHFFFAOYSA-N 0.000 claims 3
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-M Aminoacetate Chemical compound NCC([O-])=O DHMQDGOQFOQNFH-UHFFFAOYSA-M 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- DXASQZJWWGZNSF-UHFFFAOYSA-N n,n-dimethylmethanamine;sulfur trioxide Chemical group CN(C)C.O=S(=O)=O DXASQZJWWGZNSF-UHFFFAOYSA-N 0.000 claims 2
- FBTNXKPMTVSCRR-UHFFFAOYSA-N n-methylsulfonylbutanamide Chemical compound CCCC(=O)NS(C)(=O)=O FBTNXKPMTVSCRR-UHFFFAOYSA-N 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000005309 thioalkoxy group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 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
- 239000004480 active ingredient Substances 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical compound OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 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
- 239000003814 drug Substances 0.000 claims 1
- 208000027096 gram-negative bacterial infections Diseases 0.000 claims 1
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 238000000034 method Methods 0.000 description 2
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N DMSO Substances CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 1
- YECIFGHRMFEPJK-UHFFFAOYSA-N lidocaine hydrochloride monohydrate Chemical compound O.[Cl-].CC[NH+](CC)CC(=O)NC1=C(C)C=CC=C1C YECIFGHRMFEPJK-UHFFFAOYSA-N 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 238000002953 preparative HPLC Methods 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14157636 | 2014-03-04 | ||
| EP14157636.3 | 2014-03-04 | ||
| PCT/EP2015/054358 WO2015132228A1 (en) | 2014-03-04 | 2015-03-03 | 1,2-dihydro-3h-pyrrolo[1,2-c]imidazol-3-one derivatives and their use as antibacterial agents |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017508746A JP2017508746A (ja) | 2017-03-30 |
| JP2017508746A5 true JP2017508746A5 (https=) | 2018-04-12 |
| JP6516370B2 JP6516370B2 (ja) | 2019-05-22 |
Family
ID=50189621
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016555488A Expired - Fee Related JP6516370B2 (ja) | 2014-03-04 | 2015-03-03 | １，２−ジヒドロ−３Ｈ−ピロロ［１，２−ｃ］イミダゾール−３−オン誘導体及び抗菌剤としてのそれらの使用 |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US10106544B2 (https=) |
| EP (1) | EP3114126B1 (https=) |
| JP (1) | JP6516370B2 (https=) |
| KR (1) | KR20160127127A (https=) |
| CN (1) | CN106061977B (https=) |
| AR (1) | AR099612A1 (https=) |
| AU (1) | AU2015226250B2 (https=) |
| BR (1) | BR112016020278A8 (https=) |
| CA (1) | CA2938383A1 (https=) |
| CL (1) | CL2016002207A1 (https=) |
| CY (1) | CY1121362T1 (https=) |
| DK (1) | DK3114126T3 (https=) |
| EA (1) | EA030708B1 (https=) |
| ES (1) | ES2709382T3 (https=) |
| HR (1) | HRP20190013T1 (https=) |
| HU (1) | HUE042371T2 (https=) |
| IL (1) | IL247544A0 (https=) |
| LT (1) | LT3114126T (https=) |
| MA (1) | MA39707B1 (https=) |
| MX (1) | MX2016011380A (https=) |
| PH (1) | PH12016501699A1 (https=) |
| PL (1) | PL3114126T3 (https=) |
| PT (1) | PT3114126T (https=) |
| SA (1) | SA516371717B1 (https=) |
| SG (1) | SG11201607304WA (https=) |
| SI (1) | SI3114126T1 (https=) |
| TR (1) | TR201900393T4 (https=) |
| TW (1) | TW201542556A (https=) |
| UA (1) | UA118868C2 (https=) |
| WO (1) | WO2015132228A1 (https=) |
| ZA (1) | ZA201606794B (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR097617A1 (es) | 2013-09-13 | 2016-04-06 | Actelion Pharmaceuticals Ltd | Derivados antibacterianos del 2h-indazol |
| EA030730B1 (ru) | 2013-12-19 | 2018-09-28 | Идорсиа Фармасьютиклз Лтд | Антибактериальные производные 1h-индазола и 1h-индола |
| CA2948077A1 (en) | 2014-05-16 | 2015-11-19 | Actelion Pharmaceuticals Ltd | Antibacterial quinazoline-4(3h)-one derivatives |
| 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 |
| CA2991281A1 (en) * | 2015-08-28 | 2017-03-09 | Idorsia Pharmaceuticals Ltd | Antibacterial annulated pyrrolidin-2-one derivatives |
| AR105848A1 (es) * | 2015-08-31 | 2017-11-15 | Actelion Pharmaceuticals Ltd | Derivados heterocíclicos antibacterianos |
| AR105889A1 (es) * | 2015-09-03 | 2017-11-22 | Actelion Pharmaceuticals Ltd | Compuestos antibacterianos 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituidos |
| 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 |
| 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 |
| WO2023011574A1 (zh) * | 2021-08-05 | 2023-02-09 | 浙江海正药业股份有限公司 | 芳香乙炔类衍生物及其制备方法和用途 |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100984595B1 (ko) | 2002-03-13 | 2010-09-30 | 어레이 바이오파마 인크. | Ｍｅｋ 억제제로서의 ｎ3 알킬화 벤즈이미다졸 유도체 |
| US7781591B2 (en) | 2006-06-13 | 2010-08-24 | Wyeth Llc | Substituted 3-cyanopyridines as protein kinase inhibitors |
| DE102004017930A1 (de) | 2004-04-14 | 2005-11-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
| MX2007006961A (es) | 2004-12-10 | 2007-10-04 | Univ Emory | Analogos nucleosidos de ciclobutilo 2' y 3'-sustituidos para el tratamiento de infeccciones virales y proliferacion celular anormal. |
| JP2008001635A (ja) | 2006-06-22 | 2008-01-10 | Toray Ind Inc | グリシン誘導体及びその用途 |
| DE102008044132A1 (de) | 2008-11-27 | 2010-06-02 | BSH Bosch und Siemens Hausgeräte GmbH | Kältegerät mit zweiseitig anschlagbarer Tür |
| KR20120006016A (ko) | 2009-04-06 | 2012-01-17 | 다이이찌 산쿄 가부시키가이샤 | 치환 페닐기를 갖는 고리형 화합물 |
| EP2432468A2 (en) | 2009-05-20 | 2012-03-28 | Ardea Biosciences, Inc. | Methods of modulating uric acid levels |
| WO2011021209A1 (en) | 2009-07-07 | 2011-02-24 | Portsmouth Technologies Llc | Histone deacetylase inhibitors |
| WO2011045703A2 (en) * | 2009-10-13 | 2011-04-21 | Pfizer Inc. | C-linked hydroxamic acid derivatives useful as antibacterial agents |
| WO2011073845A1 (en) | 2009-12-16 | 2011-06-23 | Pfizer Inc. | N-linked hydroxamic acid derivatives useful as antibacterial agents |
| MX2013005200A (es) | 2010-11-10 | 2013-06-28 | Achaogen Inc | Derivados de acido hidroxamico y su so en el tratamiento de infecciones bacterianas. |
| CN103328482A (zh) | 2011-01-03 | 2013-09-25 | 韩美药品株式会社 | 用于调节g蛋白-偶联受体的新双环化合物 |
| ES2626457T3 (es) * | 2011-03-07 | 2017-07-25 | Pfizer Inc. | Derivados de fluoro-piridinona útiles como agentes antibacterianos |
| CA2830866A1 (en) * | 2011-04-08 | 2012-10-11 | Pfizer Inc. | Imidazole, pyrazole, and triazole derivatives useful as antibacterial agents |
| ES2526687T3 (es) | 2011-04-08 | 2015-01-14 | Pfizer Inc. | Derivados de isoxazol útiles como agentes antibacterianos |
| US8859559B2 (en) | 2011-12-20 | 2014-10-14 | Boehringer Ingelheim International Gmbh | Substituted pyrazines and their use in the treatment of disease |
| EP2847162A1 (en) | 2012-05-09 | 2015-03-18 | Achaogen, Inc. | Antibacterial agents |
| EP2847168A1 (en) * | 2012-05-10 | 2015-03-18 | Achaogen, Inc. | Antibacterial agents |
| 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 |
| EA030730B1 (ru) | 2013-12-19 | 2018-09-28 | Идорсиа Фармасьютиклз Лтд | Антибактериальные производные 1h-индазола и 1h-индола |
| CA2948077A1 (en) | 2014-05-16 | 2015-11-19 | Actelion Pharmaceuticals Ltd | Antibacterial quinazoline-4(3h)-one derivatives |
| 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 |
| CA2991281A1 (en) | 2015-08-28 | 2017-03-09 | Idorsia Pharmaceuticals Ltd | Antibacterial annulated pyrrolidin-2-one derivatives |
| AR105848A1 (es) | 2015-08-31 | 2017-11-15 | Actelion Pharmaceuticals Ltd | Derivados heterocíclicos antibacterianos |
| AR105889A1 (es) | 2015-09-03 | 2017-11-22 | Actelion Pharmaceuticals Ltd | Compuestos antibacterianos 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituidos |
| EP3386950A1 (en) | 2015-12-08 | 2018-10-17 | GlaxoSmithKline Intellectual Property Development Limited | Substituted benzazinones as antibacterial compounds |
-
2015
- 2015-03-02 AR ARP150100626A patent/AR099612A1/es unknown
- 2015-03-03 DK DK15707154.9T patent/DK3114126T3/en active
- 2015-03-03 PL PL15707154T patent/PL3114126T3/pl unknown
- 2015-03-03 SG SG11201607304WA patent/SG11201607304WA/en unknown
- 2015-03-03 TR TR2019/00393T patent/TR201900393T4/tr unknown
- 2015-03-03 HU HUE15707154A patent/HUE042371T2/hu unknown
- 2015-03-03 WO PCT/EP2015/054358 patent/WO2015132228A1/en not_active Ceased
- 2015-03-03 KR KR1020167027128A patent/KR20160127127A/ko not_active Ceased
- 2015-03-03 EP EP15707154.9A patent/EP3114126B1/en not_active Not-in-force
- 2015-03-03 LT LTEP15707154.9T patent/LT3114126T/lt unknown
- 2015-03-03 CN CN201580011865.0A patent/CN106061977B/zh not_active Expired - Fee Related
- 2015-03-03 PT PT15707154T patent/PT3114126T/pt unknown
- 2015-03-03 TW TW104106737A patent/TW201542556A/zh unknown
- 2015-03-03 ES ES15707154T patent/ES2709382T3/es active Active
- 2015-03-03 EA EA201691775A patent/EA030708B1/ru not_active IP Right Cessation
- 2015-03-03 MX MX2016011380A patent/MX2016011380A/es unknown
- 2015-03-03 BR BR112016020278A patent/BR112016020278A8/pt not_active Application Discontinuation
- 2015-03-03 US US15/123,184 patent/US10106544B2/en not_active Expired - Fee Related
- 2015-03-03 SI SI201530520T patent/SI3114126T1/sl unknown
- 2015-03-03 AU AU2015226250A patent/AU2015226250B2/en not_active Ceased
- 2015-03-03 CA CA2938383A patent/CA2938383A1/en not_active Abandoned
- 2015-03-03 MA MA39707A patent/MA39707B1/fr unknown
- 2015-03-03 UA UAA201609996A patent/UA118868C2/uk unknown
- 2015-03-03 HR HRP20190013TT patent/HRP20190013T1/hr unknown
- 2015-03-03 JP JP2016555488A patent/JP6516370B2/ja not_active Expired - Fee Related
-
2016
- 2016-08-23 SA SA516371717A patent/SA516371717B1/ar unknown
- 2016-08-26 PH PH12016501699A patent/PH12016501699A1/en unknown
- 2016-08-30 IL IL247544A patent/IL247544A0/en unknown
- 2016-09-01 CL CL2016002207A patent/CL2016002207A1/es unknown
- 2016-10-03 ZA ZA2016/06794A patent/ZA201606794B/en unknown
-
2019
- 2019-01-30 CY CY20191100131T patent/CY1121362T1/el unknown
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