JP2015500294A5 - - Google Patents
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- JP2015500294A5 JP2015500294A5 JP2014546115A JP2014546115A JP2015500294A5 JP 2015500294 A5 JP2015500294 A5 JP 2015500294A5 JP 2014546115 A JP2014546115 A JP 2014546115A JP 2014546115 A JP2014546115 A JP 2014546115A JP 2015500294 A5 JP2015500294 A5 JP 2015500294A5
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- 150000001875 compounds Chemical class 0.000 claims description 80
- 239000000203 mixture Substances 0.000 claims description 48
- 239000007909 solid dosage form Substances 0.000 claims description 37
- 230000037396 body weight Effects 0.000 claims description 26
- 206010065973 Iron Overload Diseases 0.000 claims description 12
- 208000002903 Thalassemia Diseases 0.000 claims description 9
- MVAWDZLMOYASSX-JPKZNVRTSA-L magnesium (4S)-2-[2-hydroxy-3-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]phenyl]-4-methyl-5H-1,3-thiazole-4-carboxylate hydroxide Chemical compound [OH-].[Mg+2].COCCOCCOCCOC1=CC=CC(C=2SC[C@@](C)(N=2)C([O-])=O)=C1O MVAWDZLMOYASSX-JPKZNVRTSA-L 0.000 claims description 6
- 239000002775 capsule Substances 0.000 claims description 4
- 206010058314 Dysplasia Diseases 0.000 claims description 3
- 208000007056 sickle cell anemia Diseases 0.000 claims description 3
- 208000032467 Aplastic anaemia Diseases 0.000 claims description 2
- 208000033932 Blackfan-Diamond anemia Diseases 0.000 claims description 2
- 201000004449 Diamond-Blackfan anemia Diseases 0.000 claims description 2
- 208000033981 Hereditary haemochromatosis Diseases 0.000 claims description 2
- 208000000733 Paroxysmal Hemoglobinuria Diseases 0.000 claims description 2
- 102100036050 Phosphatidylinositol N-acetylglucosaminyltransferase subunit A Human genes 0.000 claims description 2
- 230000001684 chronic effect Effects 0.000 claims description 2
- 201000008230 cutaneous porphyria Diseases 0.000 claims description 2
- 230000001419 dependent effect Effects 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 206010028537 myelofibrosis Diseases 0.000 claims description 2
- 201000003045 paroxysmal nocturnal hemoglobinuria Diseases 0.000 claims description 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 2
- 208000022806 beta-thalassemia major Diseases 0.000 claims 1
- 208000031162 sideroblastic anemia Diseases 0.000 claims 1
- 238000009472 formulation Methods 0.000 description 31
- 229910052751 metal Inorganic materials 0.000 description 23
- 239000002184 metal Substances 0.000 description 23
- 150000003839 salts Chemical class 0.000 description 19
- 238000002360 preparation method Methods 0.000 description 16
- 238000004090 dissolution Methods 0.000 description 15
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 description 12
- 210000002966 serum Anatomy 0.000 description 10
- 238000003556 assay Methods 0.000 description 8
- 239000004721 Polyphenylene oxide Substances 0.000 description 7
- 125000003545 alkoxy group Chemical group 0.000 description 7
- 229920000570 polyether Polymers 0.000 description 7
- 125000000217 alkyl group Chemical group 0.000 description 6
- 229910052739 hydrogen Inorganic materials 0.000 description 6
- 239000001257 hydrogen Substances 0.000 description 6
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 6
- 229910052742 iron Inorganic materials 0.000 description 6
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 6
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 description 4
- 230000000747 cardiac effect Effects 0.000 description 4
- 239000000546 pharmaceutical excipient Substances 0.000 description 4
- 239000011591 potassium Substances 0.000 description 4
- 229910052700 potassium Inorganic materials 0.000 description 4
- 239000011734 sodium Substances 0.000 description 4
- 229910052708 sodium Inorganic materials 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- 229920002785 Croscarmellose sodium Polymers 0.000 description 3
- 102000008857 Ferritin Human genes 0.000 description 3
- 238000008416 Ferritin Methods 0.000 description 3
- 108050000784 Ferritin Proteins 0.000 description 3
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical group [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 3
- 125000003710 aryl alkyl group Chemical group 0.000 description 3
- 229960001681 croscarmellose sodium Drugs 0.000 description 3
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 229910052736 halogen Inorganic materials 0.000 description 3
- 150000002367 halogens Chemical class 0.000 description 3
- 235000019359 magnesium stearate Nutrition 0.000 description 3
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 2
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 2
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 description 2
- 239000011575 calcium Substances 0.000 description 2
- 229910052791 calcium Inorganic materials 0.000 description 2
- 239000002738 chelating agent Substances 0.000 description 2
- DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 0.000 description 2
- 230000009089 cytolysis Effects 0.000 description 2
- 210000004185 liver Anatomy 0.000 description 2
- 239000000314 lubricant Substances 0.000 description 2
- 239000011777 magnesium Substances 0.000 description 2
- 229910052749 magnesium Inorganic materials 0.000 description 2
- 159000000003 magnesium salts Chemical class 0.000 description 2
- 239000008055 phosphate buffer solution Substances 0.000 description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 2
- 229920000053 polysorbate 80 Polymers 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 229910052725 zinc Inorganic materials 0.000 description 2
- 239000011701 zinc Substances 0.000 description 2
- BVKZGUZCCUSVTD-UHFFFAOYSA-M Bicarbonate Chemical class OC([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-M 0.000 description 1
- 206010020880 Hypertrophy Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 229910052770 Uranium Inorganic materials 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 208000007502 anemia Diseases 0.000 description 1
- 150000001450 anions Chemical class 0.000 description 1
- 125000005228 aryl sulfonate group Chemical group 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-M bisulphate group Chemical group S([O-])(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-M 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000007963 capsule composition Substances 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 150000004649 carbonic acid derivatives Chemical class 0.000 description 1
- 150000007942 carboxylates Chemical class 0.000 description 1
- 150000001768 cations Chemical class 0.000 description 1
- 230000009920 chelation Effects 0.000 description 1
- AWHIMFSHNAAMBM-GOSISDBHSA-N chembl487465 Chemical compound COCCOCCOCCOC1=CC=CC(C=2SC[C@@](C)(N=2)C(O)=O)=C1O AWHIMFSHNAAMBM-GOSISDBHSA-N 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 229940109239 creatinine Drugs 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 230000010437 erythropoiesis Effects 0.000 description 1
- 150000004820 halides Chemical class 0.000 description 1
- 150000004679 hydroxides Chemical class 0.000 description 1
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 1
- 239000007951 isotonicity adjuster Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 description 1
- 239000000347 magnesium hydroxide Substances 0.000 description 1
- 229910001862 magnesium hydroxide Inorganic materials 0.000 description 1
- 150000002823 nitrates Chemical class 0.000 description 1
- 235000021317 phosphate Nutrition 0.000 description 1
- 150000003013 phosphoric acid derivatives Chemical class 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 125000001273 sulfonato group Chemical class [O-]S(*)(=O)=O 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- JFALSRSLKYAFGM-UHFFFAOYSA-N uranium(0) Chemical compound [U] JFALSRSLKYAFGM-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161568914P | 2011-12-09 | 2011-12-09 | |
| US201161568890P | 2011-12-09 | 2011-12-09 | |
| US61/568,890 | 2011-12-09 | ||
| US61/568,914 | 2011-12-09 | ||
| PCT/US2012/068432 WO2013086312A1 (en) | 2011-12-09 | 2012-12-07 | Oral formulations for treating metal overload |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015500294A JP2015500294A (ja) | 2015-01-05 |
| JP2015500294A5 true JP2015500294A5 (enExample) | 2016-01-28 |
Family
ID=48574916
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014546115A Pending JP2015500294A (ja) | 2011-12-09 | 2012-12-07 | 金属過剰症を治療する経口製剤 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US8993606B2 (enExample) |
| EP (1) | EP2787994A4 (enExample) |
| JP (1) | JP2015500294A (enExample) |
| AR (1) | AR089122A1 (enExample) |
| AU (1) | AU2012347595A1 (enExample) |
| BR (1) | BR112014013985A2 (enExample) |
| CA (1) | CA2857990A1 (enExample) |
| TW (1) | TW201338777A (enExample) |
| WO (1) | WO2013086312A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140343110A1 (en) | 2011-12-16 | 2014-11-20 | University Of Florida Research Foundation, Inc. | Uses of 4'-desferrithiocin analogs |
| EP2970162A1 (en) | 2013-03-15 | 2016-01-20 | Ferrokin Biosciences, Inc. | Polymorph forms of desazadesferrithiocin analogs |
| AU2014352780A1 (en) * | 2013-11-22 | 2016-06-09 | University Of Florida Research Foundation, Inc. | Desferrithiocin analogs and uses thereof |
| WO2016176343A1 (en) | 2015-04-27 | 2016-11-03 | University Of Florida Research Foundation, Incorporated | Metabolically programmed metal chelators and uses thereof |
| WO2018104130A1 (en) | 2016-12-07 | 2018-06-14 | Lumileds Holding B.V. | Flash light emitter with remote communication function |
| CN114302882A (zh) * | 2019-07-19 | 2022-04-08 | 威佛（国际）股份公司 | 用于治疗输血依赖型β-地中海贫血（tdt）的膜铁转运蛋白抑制剂 |
| WO2022157185A1 (en) | 2021-01-20 | 2022-07-28 | Vifor (International) Ag | Ferroportin-inhibitors for the use in the treatment of myelodysplastic syndromes (mds) |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL1866296T3 (pl) | 2005-04-04 | 2017-05-31 | University Of Florida Research Foundation, Inc. | Polieterowe analogi desferritiocyny |
| US8067451B2 (en) | 2006-07-18 | 2011-11-29 | Horizon Pharma Usa, Inc. | Methods and medicaments for administration of ibuprofen |
| US8324397B2 (en) | 2007-03-15 | 2012-12-04 | University Of Florida Research Foundation, Inc. | Desferrithiocin polyether analogues |
| NZ605452A (en) * | 2008-07-14 | 2014-05-30 | Ferrokin Biosciences Inc | Novel salts and polymorphs of desazadesferrithiocin polyether analogues as metal chelation agents |
| BR112012001761A2 (pt) | 2009-07-27 | 2017-05-09 | Ferrokin Bioscience Inc | composto de formula i, composto farmacêutica e método de tratamento de uma condição mediada por metal em um indivduo |
| WO2011028255A2 (en) | 2009-08-25 | 2011-03-10 | University Of Florida Research Foundation, Inc. | Desferrithiocin polyether analogues and uses thereof |
| US9045440B2 (en) | 2010-05-04 | 2015-06-02 | Ferrokin Biosciences, Inc. | Desazadesferrothiocin and desazadesferrothiocin polyether analogues as metal chelation agents |
-
2012
- 2012-12-07 CA CA2857990A patent/CA2857990A1/en not_active Abandoned
- 2012-12-07 TW TW101146269A patent/TW201338777A/zh unknown
- 2012-12-07 WO PCT/US2012/068432 patent/WO2013086312A1/en not_active Ceased
- 2012-12-07 BR BR112014013985A patent/BR112014013985A2/pt not_active IP Right Cessation
- 2012-12-07 EP EP12856135.4A patent/EP2787994A4/en not_active Withdrawn
- 2012-12-07 AR ARP120104611A patent/AR089122A1/es not_active Application Discontinuation
- 2012-12-07 JP JP2014546115A patent/JP2015500294A/ja active Pending
- 2012-12-07 AU AU2012347595A patent/AU2012347595A1/en not_active Abandoned
- 2012-12-07 US US13/708,087 patent/US8993606B2/en not_active Expired - Fee Related
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