JPWO2020002714A5 - - Google Patents
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- Publication number
- JPWO2020002714A5 JPWO2020002714A5 JP2020572859A JP2020572859A JPWO2020002714A5 JP WO2020002714 A5 JPWO2020002714 A5 JP WO2020002714A5 JP 2020572859 A JP2020572859 A JP 2020572859A JP 2020572859 A JP2020572859 A JP 2020572859A JP WO2020002714 A5 JPWO2020002714 A5 JP WO2020002714A5
- Authority
- JP
- Japan
- Prior art keywords
- folate
- formulation
- skin
- tetrahydrofolic acid
- salt
- 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.)
- Pending
Links
- 229940014144 Folate Drugs 0.000 claims 37
- 235000019152 folic acid Nutrition 0.000 claims 37
- 239000011724 folic acid Substances 0.000 claims 37
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical group C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 claims 36
- 238000009472 formulation Methods 0.000 claims 36
- 239000000203 mixture Substances 0.000 claims 36
- 150000002224 folic acids Chemical class 0.000 claims 11
- 208000006641 Skin Disease Diseases 0.000 claims 10
- 238000002360 preparation method Methods 0.000 claims 9
- 201000004624 dermatitis Diseases 0.000 claims 6
- MSWZFWKMSRAUBD-IVMDWMLBSA-N 2-amino-2-deoxy-D-glucopyranose Chemical compound N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O MSWZFWKMSRAUBD-IVMDWMLBSA-N 0.000 claims 4
- 229960004373 Acetylcholine Drugs 0.000 claims 4
- 239000004475 Arginine Substances 0.000 claims 4
- 229960001231 Choline Drugs 0.000 claims 4
- 229960002442 Glucosamine Drugs 0.000 claims 4
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 claims 4
- 229960003121 arginine Drugs 0.000 claims 4
- CRBHXDCYXIISFC-UHFFFAOYSA-N choline Chemical compound C[N+](C)(C)CC[O-] CRBHXDCYXIISFC-UHFFFAOYSA-N 0.000 claims 4
- RGHNJXZEOKUKBD-SQOUGZDYSA-M D-gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O RGHNJXZEOKUKBD-SQOUGZDYSA-M 0.000 claims 3
- 229960002887 Deanol Drugs 0.000 claims 3
- 210000000981 Epithelium Anatomy 0.000 claims 3
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims 3
- UEEJHVSXFDXPFK-UHFFFAOYSA-N N-dimethylaminoethanol Chemical compound CN(C)CCO UEEJHVSXFDXPFK-UHFFFAOYSA-N 0.000 claims 3
- BPXPDKIAGXMZSD-UHFFFAOYSA-N NC(=N)NNC(=N)NCCC1=CC=CC=C1 Chemical compound NC(=N)NNC(=N)NCCC1=CC=CC=C1 BPXPDKIAGXMZSD-UHFFFAOYSA-N 0.000 claims 3
- MSTNYGQPCMXVAQ-KIYNQFGBSA-N Tetrahydrofolic acid Chemical compound N1C=2C(=O)NC(N)=NC=2NCC1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 MSTNYGQPCMXVAQ-KIYNQFGBSA-N 0.000 claims 3
- 235000014113 dietary fatty acids Nutrition 0.000 claims 3
- 239000003995 emulsifying agent Substances 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 3
- 235000019441 ethanol Nutrition 0.000 claims 3
- 239000000194 fatty acid Substances 0.000 claims 3
- -1 folate compound Chemical class 0.000 claims 3
- 229940050410 gluconate Drugs 0.000 claims 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- QYNUQALWYRSVHF-OLZOCXBDSA-N (6R)-5,10-methylenetetrahydrofolic acid Chemical compound C([C@H]1CNC=2N=C(NC(=O)C=2N1C1)N)N1C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 QYNUQALWYRSVHF-OLZOCXBDSA-N 0.000 claims 2
- VVIAGPKUTFNRDU-STQMWFEESA-N (6S)-5-formyltetrahydrofolic acid Chemical group C([C@H]1CNC=2N=C(NC(=O)C=2N1C=O)N)NC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-STQMWFEESA-N 0.000 claims 2
- AUFGTPPARQZWDO-YPMHNXCESA-N 10-formyltetrahydrofolic acid Chemical compound C([C@H]1CNC=2N=C(NC(=O)C=2N1)N)N(C=O)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 AUFGTPPARQZWDO-YPMHNXCESA-N 0.000 claims 2
- AGNTUZCMJBTHOG-UHFFFAOYSA-N 3-[3-(2,3-dihydroxypropoxy)-2-hydroxypropoxy]propane-1,2-diol Chemical compound OCC(O)COCC(O)COCC(O)CO AGNTUZCMJBTHOG-UHFFFAOYSA-N 0.000 claims 2
- ZNOVTXRBGFNYRX-STQMWFEESA-N 5-methyltetrahydrofolic acid Chemical compound C([C@@H]1N(C=2C(=O)N=C(N)NC=2NC1)C)NC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 ZNOVTXRBGFNYRX-STQMWFEESA-N 0.000 claims 2
- NQACWOLNMUVBMP-KBPBESRZSA-N C(=O)N1C=2C(NC(=NC=2NC[C@H]1CN(C1=CC=C(C(N[C@@H](CCC(=O)O)C(=O)O)=O)C=C1)C=O)N)=O Chemical compound C(=O)N1C=2C(NC(=NC=2NC[C@H]1CN(C1=CC=C(C(N[C@@H](CCC(=O)O)C(=O)O)=O)C=C1)C=O)N)=O NQACWOLNMUVBMP-KBPBESRZSA-N 0.000 claims 2
- AWUCVROLDVIAJX-UHFFFAOYSA-N Glycerol 3-phosphate Chemical compound OCC(O)COP(O)(O)=O AWUCVROLDVIAJX-UHFFFAOYSA-N 0.000 claims 2
- 208000006359 Hepatoblastoma Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 210000003491 Skin Anatomy 0.000 claims 2
- CZMRCDWAGMRECN-GDQSFJPYSA-N Sucrose Natural products O([C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1)[C@@]1(CO)[C@H](O)[C@@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-GDQSFJPYSA-N 0.000 claims 2
- 150000001450 anions Chemical class 0.000 claims 2
- 150000001768 cations Chemical class 0.000 claims 2
- 239000002131 composite material Substances 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- VVIAGPKUTFNRDU-ABLWVSNPSA-N folinic acid Chemical compound C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-ABLWVSNPSA-N 0.000 claims 2
- 150000002315 glycerophosphates Chemical class 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N iso-propanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- 239000011159 matrix material Substances 0.000 claims 2
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 2
- LRHPLDYGYMQRHN-UHFFFAOYSA-N n-butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims 2
- 239000005720 sucrose Substances 0.000 claims 2
- VSUYBDAYEVGQLA-KBPBESRZSA-N CN1C=2C(NC(=NC=2NC[C@H]1CN(C1=CC=C(C(N[C@@H](CCC(=O)O)C(=O)O)=O)C=C1)C=O)N)=O Chemical compound CN1C=2C(NC(=NC=2NC[C@H]1CN(C1=CC=C(C(N[C@@H](CCC(=O)O)C(=O)O)=O)C=C1)C=O)N)=O VSUYBDAYEVGQLA-KBPBESRZSA-N 0.000 claims 1
- HLCFGWHYROZGBI-JJKGCWMISA-M Potassium gluconate Chemical compound [K+].OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O HLCFGWHYROZGBI-JJKGCWMISA-M 0.000 claims 1
- UPMFZISCCZSDND-JJKGCWMISA-M Sodium gluconate Chemical compound [Na+].OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O UPMFZISCCZSDND-JJKGCWMISA-M 0.000 claims 1
- 229940005574 Sodium gluconate Drugs 0.000 claims 1
- 229940046008 Vitamin D Drugs 0.000 claims 1
- 229930003316 Vitamin D Natural products 0.000 claims 1
- SZYSLWCAWVWFLT-UTGHZIEOSA-N [(2S,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-2-[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxolan-2-yl]methyl octadecanoate Chemical group O([C@@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@]1(COC(=O)CCCCCCCCCCCCCCCCC)O[C@H](CO)[C@@H](O)[C@@H]1O SZYSLWCAWVWFLT-UTGHZIEOSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000000511 arginine group Chemical class N[C@@H](CCCNC(N)=N)C(=O)* 0.000 claims 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 1
- 239000011575 calcium Substances 0.000 claims 1
- 229910052791 calcium Inorganic materials 0.000 claims 1
- GHVNFZFCNZKVNT-UHFFFAOYSA-M caprate Chemical compound CCCCCCCCCC([O-])=O GHVNFZFCNZKVNT-UHFFFAOYSA-M 0.000 claims 1
- 230000001684 chronic Effects 0.000 claims 1
- 231100000406 dermatitis Toxicity 0.000 claims 1
- 150000001991 dicarboxylic acids Chemical class 0.000 claims 1
- CHFUHGDBYUITQJ-UHFFFAOYSA-L dipotassium;2,3-dihydroxypropyl phosphate Chemical compound [K+].[K+].OCC(O)COP([O-])([O-])=O CHFUHGDBYUITQJ-UHFFFAOYSA-L 0.000 claims 1
- QXNVGIXVLWOKEQ-UHFFFAOYSA-N disodium Chemical compound [Na][Na] QXNVGIXVLWOKEQ-UHFFFAOYSA-N 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 230000002757 inflammatory Effects 0.000 claims 1
- ZNOVTXRBGFNYRX-ABLWVSNPSA-N levomefolic acid Chemical compound C1NC=2NC(N)=NC(=O)C=2N(C)C1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 ZNOVTXRBGFNYRX-ABLWVSNPSA-N 0.000 claims 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims 1
- 239000011777 magnesium Substances 0.000 claims 1
- 229910052749 magnesium Inorganic materials 0.000 claims 1
- 239000006224 matting agent Substances 0.000 claims 1
- 239000004530 micro-emulsion Substances 0.000 claims 1
- AMQJEAYHLZJPGS-UHFFFAOYSA-N n-pentanol Chemical compound CCCCCO AMQJEAYHLZJPGS-UHFFFAOYSA-N 0.000 claims 1
- 239000002105 nanoparticle Substances 0.000 claims 1
- 201000009053 neurodermatitis Diseases 0.000 claims 1
- 239000007764 o/w emulsion Substances 0.000 claims 1
- IZVQHEYRKDCICI-UHFFFAOYSA-N octanoic acid;propane-1,2,3-triol Chemical compound OCC(O)CO.OCC(O)CO.OCC(O)CO.CCCCCCCC(O)=O IZVQHEYRKDCICI-UHFFFAOYSA-N 0.000 claims 1
- 239000003961 penetration enhancing agent Substances 0.000 claims 1
- 239000004224 potassium gluconate Substances 0.000 claims 1
- 235000013926 potassium gluconate Nutrition 0.000 claims 1
- 229960003189 potassium gluconate Drugs 0.000 claims 1
- BDERNNFJNOPAEC-UHFFFAOYSA-N propanol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims 1
- 201000004681 psoriasis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 150000004671 saturated fatty acids Chemical class 0.000 claims 1
- 235000003441 saturated fatty acids Nutrition 0.000 claims 1
- KEAYESYHFKHZAL-UHFFFAOYSA-N sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000000176 sodium gluconate Substances 0.000 claims 1
- 235000012207 sodium gluconate Nutrition 0.000 claims 1
- 239000007921 spray Substances 0.000 claims 1
- DKGAVHZHDRPRBM-UHFFFAOYSA-N t-BuOH Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 claims 1
- 210000001519 tissues Anatomy 0.000 claims 1
- 239000003860 topical agent Substances 0.000 claims 1
- 235000019156 vitamin B Nutrition 0.000 claims 1
- 239000011720 vitamin B Substances 0.000 claims 1
- 239000011710 vitamin D Substances 0.000 claims 1
- 235000019166 vitamin D Nutrition 0.000 claims 1
- 150000003710 vitamin D derivatives Chemical class 0.000 claims 1
- 239000007762 w/o emulsion Substances 0.000 claims 1
- 200000000019 wound Diseases 0.000 claims 1
- 150000003751 zinc Chemical class 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18181019.3A EP3586849A1 (de) | 2018-06-29 | 2018-06-29 | Folatpräparate |
| EP18181019.3 | 2018-06-29 | ||
| PCT/EP2019/067644 WO2020002714A1 (en) | 2018-06-29 | 2019-07-01 | Folate preparations |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2021529198A JP2021529198A (ja) | 2021-10-28 |
| JPWO2020002714A5 true JPWO2020002714A5 (de) | 2022-09-15 |
Family
ID=62837834
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020572859A Pending JP2021529198A (ja) | 2018-06-29 | 2019-07-01 | 葉酸塩製剤 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20210267982A1 (de) |
| EP (2) | EP3586849A1 (de) |
| JP (1) | JP2021529198A (de) |
| CN (1) | CN112334136A (de) |
| AU (1) | AU2019294572B2 (de) |
| CA (1) | CA3104396A1 (de) |
| WO (1) | WO2020002714A1 (de) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3461826A1 (de) * | 2017-09-29 | 2019-04-03 | Aprofol AG | Multifunktionelle folatsalze |
| US20240316053A1 (en) * | 2021-06-24 | 2024-09-26 | Lianyungang Jinkang Hexin Pharmaceutical Co., Ltd. | Use of folate derivative in preparation of drug for treating contact lens discomfort and dry eye |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1988004927A1 (en) * | 1986-12-31 | 1988-07-14 | Davirand, Inc. | Compositions and formulations containing folic acid, method of treating tissue with folic acid and method for preparing compositions and formulations of folic acid |
| DE4341001A1 (de) * | 1993-12-02 | 1995-06-08 | Beiersdorf Ag | Topische Zubereitungen mit einem Gehalt an L-Arginin |
| DE10062401A1 (de) * | 2000-12-14 | 2002-06-20 | Beiersdorf Ag | Verwendung von Folsäure und/oder deren Derivaten zur Herstellung kosmetischer oder dermatologischer Zubereitungen zur Prophylaxe von Schäden an der hauteigenen DNA und/oder zur Reparatur bereits eingetretener Schäden an der hauteigenen DNA |
| FI121915B (fi) * | 2004-02-06 | 2011-06-15 | Neurofood Ab Oy | Koostumus psoriasiksen hoitoon |
| AU2008351242B2 (en) * | 2008-02-20 | 2012-12-20 | Gnosis S.P.A. | Folates, compositions and uses thereof |
| WO2010102214A2 (en) * | 2009-03-05 | 2010-09-10 | University Of South Florida | Method and composition for modulating canonical wnt pathway using folate and inositol |
| EP2799060A1 (de) * | 2013-04-30 | 2014-11-05 | Aprofol AG | Stabile hochdosierte pharmazeutische Zusammensetzung enthaltend Levoleucovorin |
| US20160207925A1 (en) * | 2013-12-31 | 2016-07-21 | Gianni Fracchia | L-methylfolate salt preparations, medicaments, and nutritional supplements comprising such salts thereof |
| SG11201607440YA (en) * | 2014-03-07 | 2016-10-28 | Mark Tuffley | Composition and method for enhancing wound healing |
-
2018
- 2018-06-29 EP EP18181019.3A patent/EP3586849A1/de not_active Withdrawn
-
2019
- 2019-07-01 AU AU2019294572A patent/AU2019294572B2/en active Active
- 2019-07-01 CA CA3104396A patent/CA3104396A1/en active Pending
- 2019-07-01 JP JP2020572859A patent/JP2021529198A/ja active Pending
- 2019-07-01 EP EP19734400.5A patent/EP3813838A1/de active Pending
- 2019-07-01 US US17/256,456 patent/US20210267982A1/en active Pending
- 2019-07-01 WO PCT/EP2019/067644 patent/WO2020002714A1/en active Application Filing
- 2019-07-01 CN CN201980043916.6A patent/CN112334136A/zh active Pending
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