JP2018021060A5 - - Google Patents
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- Publication number
- JP2018021060A5 JP2018021060A5 JP2017170727A JP2017170727A JP2018021060A5 JP 2018021060 A5 JP2018021060 A5 JP 2018021060A5 JP 2017170727 A JP2017170727 A JP 2017170727A JP 2017170727 A JP2017170727 A JP 2017170727A JP 2018021060 A5 JP2018021060 A5 JP 2018021060A5
- Authority
- JP
- Japan
- Prior art keywords
- species
- compound
- difluoroethyl
- pyrrolo
- chloro
- 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 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 206010017533 Fungal infection Diseases 0.000 claims 4
- 208000031888 Mycoses Diseases 0.000 claims 4
- 241000228143 Penicillium Species 0.000 claims 4
- 241001225321 Aspergillus fumigatus Species 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 241000235395 Mucor Species 0.000 claims 3
- 229940091771 aspergillus fumigatus Drugs 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 241001019659 Acremonium <Plectosphaerellaceae> Species 0.000 claims 2
- 241000228212 Aspergillus Species 0.000 claims 2
- 201000007336 Cryptococcosis Diseases 0.000 claims 2
- 241000221204 Cryptococcus neoformans Species 0.000 claims 2
- 241001123635 Dipodascus Species 0.000 claims 2
- 241000233866 Fungi Species 0.000 claims 2
- 241000223218 Fusarium Species 0.000 claims 2
- 241001480037 Microsporum Species 0.000 claims 2
- 241000235402 Rhizomucor Species 0.000 claims 2
- 241000122799 Scopulariopsis Species 0.000 claims 2
- 241000223238 Trichophyton Species 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- SZUVGFMDDVSKSI-WIFOCOSTSA-N (1s,2s,3s,5r)-1-(carboxymethyl)-3,5-bis[(4-phenoxyphenyl)methyl-propylcarbamoyl]cyclopentane-1,2-dicarboxylic acid Chemical compound O=C([C@@H]1[C@@H]([C@](CC(O)=O)([C@H](C(=O)N(CCC)CC=2C=CC(OC=3C=CC=CC=3)=CC=2)C1)C(O)=O)C(O)=O)N(CCC)CC(C=C1)=CC=C1OC1=CC=CC=C1 SZUVGFMDDVSKSI-WIFOCOSTSA-N 0.000 claims 1
- GHYOCDFICYLMRF-UTIIJYGPSA-N (2S,3R)-N-[(2S)-3-(cyclopenten-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]propanoyl]amino]propanamide Chemical compound C1(=CCCC1)C[C@@H](C(=O)[C@@]1(OC1)C)NC([C@H]([C@@H](C1=CC=C(C=C1)OC)O)NC([C@H](C)NC(CN1CCOCC1)=O)=O)=O GHYOCDFICYLMRF-UTIIJYGPSA-N 0.000 claims 1
- 125000006002 1,1-difluoroethyl group Chemical group 0.000 claims 1
- ITZKLSPBAIOEBP-UHFFFAOYSA-N 4-[3-(1,1-difluoroethyl)-4-fluorophenyl]-7-fluoro-6h-pyrrolo[1,2-a][1,4]benzodiazepine Chemical compound C1=C(F)C(C(F)(F)C)=CC(C=2C3=CC=CN3C3=CC=CC(F)=C3CN=2)=C1 ITZKLSPBAIOEBP-UHFFFAOYSA-N 0.000 claims 1
- VLVUEAVVOMODPQ-UHFFFAOYSA-N 7-chloro-4-[3-(1,1-difluoroethyl)-4-fluorophenyl]-6h-pyrrolo[1,2-a][1,4]benzodiazepine Chemical compound C1=C(F)C(C(F)(F)C)=CC(C=2C3=CC=CN3C3=CC=CC(Cl)=C3CN=2)=C1 VLVUEAVVOMODPQ-UHFFFAOYSA-N 0.000 claims 1
- MENMBOPAWKKEBV-UHFFFAOYSA-N 7-chloro-4-[3-(1,1-difluoroethyl)phenyl]-5,6-dihydro-4h-pyrrolo[1,2-a][1,4]benzodiazepine Chemical compound CC(F)(F)C1=CC=CC(C2C3=CC=CN3C3=CC=CC(Cl)=C3CN2)=C1 MENMBOPAWKKEBV-UHFFFAOYSA-N 0.000 claims 1
- SHRFDURMQQNBRR-UHFFFAOYSA-N 7-chloro-4-[3-(1,1-difluoroethyl)phenyl]-6h-pyrrolo[1,2-a][1,4]benzodiazepine Chemical compound CC(F)(F)C1=CC=CC(C=2C3=CC=CN3C3=CC=CC(Cl)=C3CN=2)=C1 SHRFDURMQQNBRR-UHFFFAOYSA-N 0.000 claims 1
- XLHURASFFGMRRF-UHFFFAOYSA-N 9-chloro-4-[3-(1,1-difluoroethyl)-4-fluorophenyl]-6h-pyrrolo[1,2-a][1,4]benzodiazepine Chemical compound C1=C(F)C(C(F)(F)C)=CC(C=2C3=CC=CN3C3=CC(Cl)=CC=C3CN=2)=C1 XLHURASFFGMRRF-UHFFFAOYSA-N 0.000 claims 1
- 241000985243 Arthrographis Species 0.000 claims 1
- 241000725132 Arthrographis sp. Species 0.000 claims 1
- 241000222120 Candida <Saccharomycetales> Species 0.000 claims 1
- 241000222173 Candida parapsilosis Species 0.000 claims 1
- 241000893980 Microsporum canis Species 0.000 claims 1
- OPFJDXRVMFKJJO-ZHHKINOHSA-N N-{[3-(2-benzamido-4-methyl-1,3-thiazol-5-yl)-pyrazol-5-yl]carbonyl}-G-dR-G-dD-dD-dD-NH2 Chemical compound S1C(C=2NN=C(C=2)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(=O)N[C@H](CC(O)=O)C(=O)N[C@H](CC(O)=O)C(=O)N[C@H](CC(O)=O)C(N)=O)=C(C)N=C1NC(=O)C1=CC=CC=C1 OPFJDXRVMFKJJO-ZHHKINOHSA-N 0.000 claims 1
- 241001236817 Paecilomyces <Clavicipitaceae> Species 0.000 claims 1
- 206010039509 Scab Diseases 0.000 claims 1
- 241000223259 Trichoderma Species 0.000 claims 1
- 241001045770 Trichophyton mentagrophytes Species 0.000 claims 1
- 241000223229 Trichophyton rubrum Species 0.000 claims 1
- SMNRFWMNPDABKZ-WVALLCKVSA-N [[(2R,3S,4R,5S)-5-(2,6-dioxo-3H-pyridin-3-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [[[(2R,3S,4S,5R,6R)-4-fluoro-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] hydrogen phosphate Chemical compound OC[C@H]1O[C@H](OP(O)(=O)OP(O)(=O)OP(O)(=O)OP(O)(=O)OC[C@H]2O[C@H]([C@H](O)[C@@H]2O)C2C=CC(=O)NC2=O)[C@H](O)[C@@H](F)[C@@H]1O SMNRFWMNPDABKZ-WVALLCKVSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 229940055022 candida parapsilosis Drugs 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 229940125797 compound 12 Drugs 0.000 claims 1
- 229940126543 compound 14 Drugs 0.000 claims 1
- 229940125810 compound 20 Drugs 0.000 claims 1
- 229940126086 compound 21 Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- JAXFJECJQZDFJS-XHEPKHHKSA-N gtpl8555 Chemical compound OC(=O)C[C@H](N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@H](B1O[C@@]2(C)[C@H]3C[C@H](C3(C)C)C[C@H]2O1)CCC1=CC=C(F)C=C1 JAXFJECJQZDFJS-XHEPKHHKSA-N 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 235000013599 spices Nutrition 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10165076 | 2010-06-07 | ||
| EP10165076.0 | 2010-06-07 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016004295A Division JP6208263B2 (ja) | 2010-06-07 | 2016-01-13 | 新規抗真菌５，６−ジヒドロ−４−［（ジフルオロエチル）フェニル］−４Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピンおよび４−（ジフルオロエチル）フェニル−６Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピン誘導体 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019057689A Division JP6653036B2 (ja) | 2010-06-07 | 2019-03-26 | 新規抗真菌５，６−ジヒドロ−４−［（ジフルオロエチル）フェニル］−４Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピンおよび４−（ジフルオロエチル）フェニル−６Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピン誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018021060A JP2018021060A (ja) | 2018-02-08 |
| JP2018021060A5 true JP2018021060A5 (enExample) | 2018-03-22 |
| JP6505176B2 JP6505176B2 (ja) | 2019-04-24 |
Family
ID=42294978
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013513625A Active JP5922107B2 (ja) | 2010-06-07 | 2011-06-01 | 新規抗真菌５，６−ジヒドロ−４−［（ジフルオロエチル）フェニル］−４Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピンおよび４−（ジフルオロエチル）フェニル−６Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピン誘導体 |
| JP2016004295A Active JP6208263B2 (ja) | 2010-06-07 | 2016-01-13 | 新規抗真菌５，６−ジヒドロ−４−［（ジフルオロエチル）フェニル］−４Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピンおよび４−（ジフルオロエチル）フェニル−６Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピン誘導体 |
| JP2017170727A Active JP6505176B2 (ja) | 2010-06-07 | 2017-09-06 | 新規抗真菌５，６−ジヒドロ−４−［（ジフルオロエチル）フェニル］−４Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピンおよび４−（ジフルオロエチル）フェニル−６Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピン誘導体 |
| JP2019057689A Active JP6653036B2 (ja) | 2010-06-07 | 2019-03-26 | 新規抗真菌５，６−ジヒドロ−４−［（ジフルオロエチル）フェニル］−４Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピンおよび４−（ジフルオロエチル）フェニル−６Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピン誘導体 |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013513625A Active JP5922107B2 (ja) | 2010-06-07 | 2011-06-01 | 新規抗真菌５，６−ジヒドロ−４−［（ジフルオロエチル）フェニル］−４Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピンおよび４−（ジフルオロエチル）フェニル−６Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピン誘導体 |
| JP2016004295A Active JP6208263B2 (ja) | 2010-06-07 | 2016-01-13 | 新規抗真菌５，６−ジヒドロ−４−［（ジフルオロエチル）フェニル］−４Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピンおよび４−（ジフルオロエチル）フェニル−６Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピン誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019057689A Active JP6653036B2 (ja) | 2010-06-07 | 2019-03-26 | 新規抗真菌５，６−ジヒドロ−４−［（ジフルオロエチル）フェニル］−４Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピンおよび４−（ジフルオロエチル）フェニル−６Ｈ−ピロロ［１，２−ａ］［１，４］ベンゾジアゼピン誘導体 |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US9637490B2 (enExample) |
| EP (1) | EP2576557B1 (enExample) |
| JP (4) | JP5922107B2 (enExample) |
| KR (1) | KR101886136B1 (enExample) |
| CN (1) | CN102947307B (enExample) |
| AP (1) | AP3285A (enExample) |
| AR (1) | AR081642A1 (enExample) |
| AU (1) | AU2011263946B2 (enExample) |
| BR (1) | BR112012030895A2 (enExample) |
| CA (1) | CA2799634C (enExample) |
| EA (1) | EA021220B1 (enExample) |
| ES (1) | ES2489191T3 (enExample) |
| JO (1) | JO3029B1 (enExample) |
| MX (1) | MX2012014271A (enExample) |
| MY (1) | MY156731A (enExample) |
| NZ (1) | NZ602981A (enExample) |
| PH (1) | PH12012502293A1 (enExample) |
| SG (1) | SG185650A1 (enExample) |
| TW (1) | TWI500619B (enExample) |
| UA (1) | UA107963C2 (enExample) |
| WO (1) | WO2011154298A1 (enExample) |
| ZA (1) | ZA201209246B (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ587490A (en) * | 2010-08-20 | 2013-03-28 | Greentide Ltd | Anti-Microbial Compounds containing compounds with a sugar substituent |
| UA109676C2 (xx) * | 2010-11-24 | 2015-09-25 | ПРОТИГРИБКОВІ 5,6-ДИГІДРО-4H-ПІРОЛО$1,2-а]$1,4]БЕНЗОДІАЗЕПІНИ І 6H-ПІРОЛО$1,2-а]$1,4]БЕНЗОДІАЗЕПІНИ, ЗАМІЩЕНІ ФЕНІЛЬНИМИ ПОХІДНИМИ | |
| AU2013204604B2 (en) * | 2012-05-30 | 2016-05-19 | Biodiem Limited | Method of treating Scedosporium spp. infection |
| JP6197348B2 (ja) * | 2013-04-25 | 2017-09-20 | セントラル硝子株式会社 | α，α−ジフルオロ芳香族化合物の保存安定性の向上方法 |
| RU2771019C1 (ru) * | 2021-06-29 | 2022-04-25 | Федеральное государственное автономное образовательное учреждение высшего образования "Пермский государственный национальный исследовательский университет" (ПГНИУ) | Применение 10-метил-2-(трифторметил)-6,7-дигидро-5Н-бензо[b]пирроло[1,2-d][1,4]диазепина в качестве антибактериального средства в отношении грамположительных микроорганизмов |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE431826T1 (de) * | 2000-10-23 | 2009-06-15 | Janssen Pharmaceutica Nv | In der 4-stellung substituierte 5,6-dihydro-4h- pyrroloä1,2-aü ä1,4ü benzodiazepine als fungizide |
-
2011
- 2011-01-06 UA UAA201211701A patent/UA107963C2/uk unknown
- 2011-05-30 JO JOP/2011/0174A patent/JO3029B1/ar active
- 2011-06-01 SG SG2012084901A patent/SG185650A1/en unknown
- 2011-06-01 NZ NZ602981A patent/NZ602981A/xx not_active IP Right Cessation
- 2011-06-01 AU AU2011263946A patent/AU2011263946B2/en not_active Ceased
- 2011-06-01 PH PH1/2012/502293A patent/PH12012502293A1/en unknown
- 2011-06-01 JP JP2013513625A patent/JP5922107B2/ja active Active
- 2011-06-01 AP AP2012006502A patent/AP3285A/xx active
- 2011-06-01 MY MYPI2012005016A patent/MY156731A/en unknown
- 2011-06-01 US US13/702,361 patent/US9637490B2/en active Active
- 2011-06-01 KR KR1020127030661A patent/KR101886136B1/ko not_active Expired - Fee Related
- 2011-06-01 ES ES11723445.0T patent/ES2489191T3/es active Active
- 2011-06-01 BR BR112012030895A patent/BR112012030895A2/pt not_active Application Discontinuation
- 2011-06-01 CN CN201180028301.XA patent/CN102947307B/zh active Active
- 2011-06-01 CA CA2799634A patent/CA2799634C/en active Active
- 2011-06-01 MX MX2012014271A patent/MX2012014271A/es active IP Right Grant
- 2011-06-01 EA EA201291401A patent/EA021220B1/ru not_active IP Right Cessation
- 2011-06-01 EP EP11723445.0A patent/EP2576557B1/en active Active
- 2011-06-01 WO PCT/EP2011/059058 patent/WO2011154298A1/en not_active Ceased
- 2011-06-03 TW TW100119491A patent/TWI500619B/zh not_active IP Right Cessation
- 2011-06-06 AR ARP110101951A patent/AR081642A1/es unknown
-
2012
- 2012-12-06 ZA ZA2012/09246A patent/ZA201209246B/en unknown
-
2016
- 2016-01-13 JP JP2016004295A patent/JP6208263B2/ja active Active
-
2017
- 2017-09-06 JP JP2017170727A patent/JP6505176B2/ja active Active
-
2019
- 2019-03-26 JP JP2019057689A patent/JP6653036B2/ja active Active
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