JP2018536714A5 - - Google Patents
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- Publication number
- JP2018536714A5 JP2018536714A5 JP2018546763A JP2018546763A JP2018536714A5 JP 2018536714 A5 JP2018536714 A5 JP 2018536714A5 JP 2018546763 A JP2018546763 A JP 2018546763A JP 2018546763 A JP2018546763 A JP 2018546763A JP 2018536714 A5 JP2018536714 A5 JP 2018536714A5
- Authority
- JP
- Japan
- Prior art keywords
- ethyl
- group
- pharmaceutical composition
- phosphinoyl
- propionylamino
- 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
- 239000008194 pharmaceutical composition Substances 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 12
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- -1 acryloxy Chemical group 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 229930195734 saturated hydrocarbon Natural products 0.000 claims 3
- 239000011593 sulfur Chemical group 0.000 claims 3
- 229910052717 sulfur Chemical group 0.000 claims 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- KXDHJXZQYSOELW-UHFFFAOYSA-N Carbamic acid Chemical group NC(O)=O KXDHJXZQYSOELW-UHFFFAOYSA-N 0.000 claims 2
- 229920000858 Cyclodextrin Polymers 0.000 claims 2
- 206010015958 Eye pain Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 229930195735 unsaturated hydrocarbon Natural products 0.000 claims 2
- KEZOVSDHSZHSOM-UHFFFAOYSA-N 1-[1-(2-methylpropanoyloxy)ethoxycarbonylamino]ethyl-[3-oxo-3-[(1-oxo-1-phenylmethoxypropan-2-yl)amino]-2-[(4-phenylphenyl)methyl]propyl]phosphinic acid Chemical compound C=1C=CC=CC=1COC(=O)C(C)NC(=O)C(CP(O)(=O)C(C)NC(=O)OC(C)OC(=O)C(C)C)CC(C=C1)=CC=C1C1=CC=CC=C1 KEZOVSDHSZHSOM-UHFFFAOYSA-N 0.000 claims 1
- DBHIEVDTXYZXEG-UHFFFAOYSA-N 1-aminoethyl-[2-[(4-bromophenyl)methyl]-3-oxo-3-[(1-oxo-1-phenylmethoxypropan-2-yl)amino]propyl]phosphinic acid Chemical compound C(C1=CC=CC=C1)OC(C(C)NC(C(CP(=O)(C(C)N)O)CC1=CC=C(C=C1)Br)=O)=O DBHIEVDTXYZXEG-UHFFFAOYSA-N 0.000 claims 1
- NHFOJXYRWFXHHZ-UHFFFAOYSA-N 1-aminoethyl-[3-oxo-3-[(1-oxo-1-phenylmethoxypropan-2-yl)amino]-2-[(4-phenylphenyl)methyl]propyl]phosphinic acid Chemical compound C=1C=CC=CC=1COC(=O)C(C)NC(=O)C(CP(O)(=O)C(N)C)CC(C=C1)=CC=C1C1=CC=CC=C1 NHFOJXYRWFXHHZ-UHFFFAOYSA-N 0.000 claims 1
- IFTBAMQPMPLZOL-UHFFFAOYSA-N 2-[[2-[(4-bromophenyl)methyl]-3-[hydroxy-[1-[1-(2-methylpropanoyloxy)ethoxycarbonylamino]ethyl]phosphoryl]propanoyl]amino]propanoic acid Chemical compound CC(C)C(=O)OC(C)OC(=O)NC(C)P(O)(=O)CC(C(=O)NC(C)C(O)=O)CC1=CC=C(Br)C=C1 IFTBAMQPMPLZOL-UHFFFAOYSA-N 0.000 claims 1
- WRVVJFLQCNNQSS-UHFFFAOYSA-N 2-[[2-[[1-azaniumylethyl(hydroxy)phosphoryl]methyl]-3-(4-bromophenyl)propanoyl]amino]propanoate Chemical compound OC(=O)C(C)NC(=O)C(CP(O)(=O)C(N)C)CC1=CC=C(Br)C=C1 WRVVJFLQCNNQSS-UHFFFAOYSA-N 0.000 claims 1
- CWJPVKSBGVPXRD-UHFFFAOYSA-N 2-[[2-[[1-azaniumylethyl(hydroxy)phosphoryl]methyl]-3-(4-phenylphenyl)propanoyl]amino]propanoate Chemical compound C1=CC(CC(CP(O)(=O)C(N)C)C(=O)NC(C)C(O)=O)=CC=C1C1=CC=CC=C1 CWJPVKSBGVPXRD-UHFFFAOYSA-N 0.000 claims 1
- ODSBYECYRZQRIK-UHFFFAOYSA-N 2-[[2-[[hydroxy-[1-[1-(2-methylpropanoyloxy)ethoxycarbonylamino]ethyl]phosphoryl]methyl]-3-(4-phenylphenyl)propanoyl]amino]propanoic acid Chemical compound C1=CC(CC(CP(O)(=O)C(C)NC(=O)OC(C)OC(=O)C(C)C)C(=O)NC(C)C(O)=O)=CC=C1C1=CC=CC=C1 ODSBYECYRZQRIK-UHFFFAOYSA-N 0.000 claims 1
- BDXDIOMYACZVMS-UHFFFAOYSA-N C(C)OC(=O)OOC(C(C)NC(C(CP(=O)(C(C)N)O)CC1=CC=C(C=C1)C1=CC=CC=C1)=O)=O Chemical compound C(C)OC(=O)OOC(C(C)NC(C(CP(=O)(C(C)N)O)CC1=CC=C(C=C1)C1=CC=CC=C1)=O)=O BDXDIOMYACZVMS-UHFFFAOYSA-N 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013774 Dry eye Diseases 0.000 claims 1
- 239000001116 FEMA 4028 Substances 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 208000004454 Hyperalgesia Diseases 0.000 claims 1
- 208000035154 Hyperesthesia Diseases 0.000 claims 1
- 125000000815 N-oxide group Chemical group 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- HQHQUKKBWTVSRU-UHFFFAOYSA-N [2-[(4-bromophenyl)methyl]-3-oxo-3-[(1-oxo-1-phenylmethoxypropan-2-yl)amino]propyl]-[1-[1-(2-methylpropanoyloxy)ethoxycarbonylamino]ethyl]phosphinic acid Chemical compound C=1C=CC=CC=1COC(=O)C(C)NC(=O)C(CP(O)(=O)C(C)NC(=O)OC(C)OC(=O)C(C)C)CC1=CC=C(Br)C=C1 HQHQUKKBWTVSRU-UHFFFAOYSA-N 0.000 claims 1
- UOYXBIFDUUCEHF-UHFFFAOYSA-N [3-[(1-ethoxy-1-oxopropan-2-yl)amino]-3-oxo-2-[(4-phenylphenyl)methyl]propyl]-[1-[1-(2-methylpropanoyloxy)ethoxycarbonylamino]ethyl]phosphinic acid Chemical compound C1=CC(CC(C(=O)NC(C)C(=O)OCC)CP(O)(=O)C(C)NC(=O)OC(C)OC(=O)C(C)C)=CC=C1C1=CC=CC=C1 UOYXBIFDUUCEHF-UHFFFAOYSA-N 0.000 claims 1
- WIQWUFMEEZUBRR-UHFFFAOYSA-N [3-[(1-ethoxycarbonylperoxy-1-oxopropan-2-yl)amino]-3-oxo-2-[(4-phenylphenyl)methyl]propyl]-[1-[1-(2-methylpropanoyloxy)ethoxycarbonylamino]ethyl]phosphinic acid Chemical compound C(C)OC(=O)OOC(C(C)NC(C(CP(=O)(C(C)NC(=O)OC(C)OC(C(C)C)=O)O)CC1=CC=C(C=C1)C1=CC=CC=C1)=O)=O WIQWUFMEEZUBRR-UHFFFAOYSA-N 0.000 claims 1
- 125000001931 aliphatic group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 239000007864 aqueous solution Substances 0.000 claims 1
- 235000011175 beta-cyclodextrine Nutrition 0.000 claims 1
- 229960004853 betadex Drugs 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003889 eye drop Substances 0.000 claims 1
- 229940012356 eye drops Drugs 0.000 claims 1
- 239000003885 eye ointment Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 239000000499 gel Substances 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- RCCPEORTSYDPMB-UHFFFAOYSA-N hydroxy benzenecarboximidothioate Chemical compound OSC(=N)C1=CC=CC=C1 RCCPEORTSYDPMB-UHFFFAOYSA-N 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 230000002981 neuropathic effect Effects 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 229920001467 poly(styrenesulfonates) Polymers 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims 1
- 229940006186 sodium polystyrene sulfonate Drugs 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 229940097346 sulfobutylether-beta-cyclodextrin Drugs 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR1561598 | 2015-11-30 | ||
| FR1561598A FR3044227B1 (fr) | 2015-11-30 | 2015-11-30 | Derives aminophosphiniques pour la prevention et le traitement des douleurs oculaires |
| PCT/EP2016/079285 WO2017093322A1 (fr) | 2015-11-30 | 2016-11-30 | Dérivés aminophosphiniques pour la prévention et le traitement des douleurs oculaires |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018536714A JP2018536714A (ja) | 2018-12-13 |
| JP2018536714A5 true JP2018536714A5 (https=) | 2020-01-16 |
| JP6889176B2 JP6889176B2 (ja) | 2021-06-18 |
Family
ID=55346018
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018546763A Active JP6889176B2 (ja) | 2015-11-30 | 2016-11-30 | 眼痛を予防及び治療するためのアミノホスフィン酸誘導体 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US20180344753A1 (https=) |
| EP (1) | EP3383403B1 (https=) |
| JP (1) | JP6889176B2 (https=) |
| KR (1) | KR102657652B1 (https=) |
| CN (2) | CN108289901B (https=) |
| BR (1) | BR112018010007A2 (https=) |
| CA (1) | CA3006365A1 (https=) |
| DK (1) | DK3383403T3 (https=) |
| ES (1) | ES2773148T3 (https=) |
| FR (1) | FR3044227B1 (https=) |
| IL (1) | IL259562B (https=) |
| MX (1) | MX382921B (https=) |
| TW (1) | TWI729039B (https=) |
| WO (1) | WO2017093322A1 (https=) |
| ZA (1) | ZA201804037B (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9993427B2 (en) * | 2013-03-14 | 2018-06-12 | Biorest Ltd. | Liposome formulation and manufacture |
| FR3063635B1 (fr) * | 2017-03-09 | 2019-06-07 | Pharmaleads | Derives aminophosphiniques pour la prevention et le traitement de l'inflammation oculaire |
| TWI771386B (zh) * | 2017-03-09 | 2022-07-21 | 法商領先藥物公司 | 用於預防及治療眼發炎的氨基膦衍生物 |
| FR3104581B1 (fr) * | 2019-12-11 | 2021-11-26 | Pharmaleads | Procédé de préparation industrielle du sel disodique de ((2S)-3-([1,1'-biphenyl]-4-yl)-2-((hydroxy((1R)-1-(((1-(isobutyryloxy)ethoxy)carbonyl)amino)ethyl)phosphoryl) methyl)propanoyl)-L-alanine |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0987291A (ja) * | 1995-09-26 | 1997-03-31 | Wakamoto Pharmaceut Co Ltd | 新規なアラニン誘導体 |
| FR2755135B1 (fr) | 1996-10-25 | 2002-12-27 | Inst Nat Sante Rech Med | Nouveaux derives d'(alpha-aminophosphino)peptides, leur procede de preparation et les compositions qui les contiennent |
| ES2174337T3 (es) * | 1996-12-16 | 2002-11-01 | Alcon Lab Inc | Uso topico de los agonistas opioides kappa para el tratamiento del dolor ocular. |
| FR2777780B1 (fr) * | 1998-04-22 | 2001-05-04 | Inst Nat Sante Rech Med | Derives d'(alpha-aminophosphino) peptides, leur procede de preparation et les compositions qui les contiennent |
| FR2934267B1 (fr) | 2008-07-23 | 2010-08-13 | Pharmaleads | Derives aminophosphiniques utiles dans le traitement de la douleur |
| FR2934627B1 (fr) | 2008-07-29 | 2010-08-13 | Paul Marie Bernard | Dispositif de positionnement et de calage d'un garde corps escamotable sur plateforme support de banches |
| JP2016511246A (ja) * | 2013-02-13 | 2016-04-14 | ノバルティス アーゲー | 局所眼用鎮痛薬 |
-
2015
- 2015-11-30 FR FR1561598A patent/FR3044227B1/fr not_active Expired - Fee Related
-
2016
- 2016-11-30 WO PCT/EP2016/079285 patent/WO2017093322A1/fr not_active Ceased
- 2016-11-30 JP JP2018546763A patent/JP6889176B2/ja active Active
- 2016-11-30 EP EP16809676.6A patent/EP3383403B1/fr active Active
- 2016-11-30 CN CN201680070092.8A patent/CN108289901B/zh active Active
- 2016-11-30 CA CA3006365A patent/CA3006365A1/fr active Pending
- 2016-11-30 BR BR112018010007-2A patent/BR112018010007A2/pt not_active Application Discontinuation
- 2016-11-30 KR KR1020187018504A patent/KR102657652B1/ko active Active
- 2016-11-30 TW TW105139517A patent/TWI729039B/zh active
- 2016-11-30 MX MX2018006580A patent/MX382921B/es unknown
- 2016-11-30 US US15/779,220 patent/US20180344753A1/en not_active Abandoned
- 2016-11-30 DK DK16809676.6T patent/DK3383403T3/da active
- 2016-11-30 CN CN202010893476.8A patent/CN112121008A/zh active Pending
- 2016-11-30 ES ES16809676T patent/ES2773148T3/es active Active
-
2018
- 2018-05-23 IL IL259562A patent/IL259562B/en active IP Right Grant
- 2018-06-15 ZA ZA2018/04037A patent/ZA201804037B/en unknown
-
2019
- 2019-02-11 US US16/272,573 patent/US10688113B2/en active Active
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