JP2017509684A5 - - Google Patents
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- Publication number
- JP2017509684A5 JP2017509684A5 JP2016560802A JP2016560802A JP2017509684A5 JP 2017509684 A5 JP2017509684 A5 JP 2017509684A5 JP 2016560802 A JP2016560802 A JP 2016560802A JP 2016560802 A JP2016560802 A JP 2016560802A JP 2017509684 A5 JP2017509684 A5 JP 2017509684A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- rapamycin
- amount
- micrograms
- microns
- 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
- 239000000203 mixture Substances 0.000 claims description 50
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims description 40
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims description 39
- 229960002930 sirolimus Drugs 0.000 claims description 39
- 239000002245 particle Substances 0.000 claims description 20
- 210000004072 lung Anatomy 0.000 claims description 13
- 239000008280 blood Substances 0.000 claims description 10
- 210000004369 blood Anatomy 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 9
- 239000000443 aerosol Substances 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
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- 208000035475 disorder Diseases 0.000 claims description 4
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- 238000001694 spray drying Methods 0.000 claims description 3
- 239000007900 aqueous suspension Substances 0.000 claims description 2
- 238000011282 treatment Methods 0.000 claims description 2
- 239000002775 capsule Substances 0.000 claims 4
- 239000011859 microparticle Substances 0.000 claims 4
- 239000011888 foil Substances 0.000 claims 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 2
- GKIRPKYJQBWNGO-OCEACIFDSA-N clomifene Chemical compound C1=CC(OCCN(CC)CC)=CC=C1C(\C=1C=CC=CC=1)=C(\Cl)C1=CC=CC=C1 GKIRPKYJQBWNGO-OCEACIFDSA-N 0.000 claims 2
- 229940112141 dry powder inhaler Drugs 0.000 claims 2
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- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
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- HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 claims 1
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 claims 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-QTVWNMPRSA-N D-mannopyranose Chemical compound OC[C@H]1OC(O)[C@@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-QTVWNMPRSA-N 0.000 claims 1
- HMFHBZSHGGEWLO-SOOFDHNKSA-N D-ribofuranose Chemical compound OC[C@H]1OC(O)[C@H](O)[C@@H]1O HMFHBZSHGGEWLO-SOOFDHNKSA-N 0.000 claims 1
- 229920002307 Dextran Polymers 0.000 claims 1
- 229930091371 Fructose Natural products 0.000 claims 1
- 239000005715 Fructose Substances 0.000 claims 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 claims 1
- 108010010803 Gelatin Proteins 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- PYMYPHUHKUWMLA-LMVFSUKVSA-N Ribose Natural products OC[C@@H](O)[C@@H](O)[C@@H](O)C=O PYMYPHUHKUWMLA-LMVFSUKVSA-N 0.000 claims 1
- 229920002472 Starch Polymers 0.000 claims 1
- 229930006000 Sucrose Natural products 0.000 claims 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 1
- HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 claims 1
- HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 claims 1
- HMFHBZSHGGEWLO-UHFFFAOYSA-N alpha-D-Furanose-Ribose Natural products OCC1OC(O)C(O)C1O HMFHBZSHGGEWLO-UHFFFAOYSA-N 0.000 claims 1
- PYMYPHUHKUWMLA-WDCZJNDASA-N arabinose Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)C=O PYMYPHUHKUWMLA-WDCZJNDASA-N 0.000 claims 1
- PYMYPHUHKUWMLA-UHFFFAOYSA-N arabinose Natural products OCC(O)C(O)C(O)C=O PYMYPHUHKUWMLA-UHFFFAOYSA-N 0.000 claims 1
- SRBFZHDQGSBBOR-UHFFFAOYSA-N beta-D-Pyranose-Lyxose Natural products OC1COC(O)C(O)C1O SRBFZHDQGSBBOR-UHFFFAOYSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 229920000159 gelatin Polymers 0.000 claims 1
- 239000008273 gelatin Substances 0.000 claims 1
- 235000019322 gelatine Nutrition 0.000 claims 1
- 235000011852 gelatine desserts Nutrition 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 239000008249 pharmaceutical aerosol Substances 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 235000019698 starch Nutrition 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 description 12
- 239000003814 drug Substances 0.000 description 9
- 229940079593 drug Drugs 0.000 description 8
- 239000000243 solution Substances 0.000 description 6
- 239000013011 aqueous formulation Substances 0.000 description 5
- 238000001238 wet grinding Methods 0.000 description 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 4
- 239000004094 surface-active agent Substances 0.000 description 4
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 238000005259 measurement Methods 0.000 description 3
- 239000002736 nonionic surfactant Substances 0.000 description 3
- 150000003904 phospholipids Chemical class 0.000 description 3
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- 229920005862 polyol Polymers 0.000 description 2
- 150000003077 polyols Chemical class 0.000 description 2
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 2
- 238000001179 sorption measurement Methods 0.000 description 2
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- 241000124008 Mammalia Species 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 241000282579 Pan Species 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
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- 238000011374 additional therapy Methods 0.000 description 1
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461975127P | 2014-04-04 | 2014-04-04 | |
| US61/975,127 | 2014-04-04 | ||
| PCT/US2015/024551 WO2015154084A1 (en) | 2014-04-04 | 2015-04-06 | An inhalable rapamycin formulation for treating age-related conditions |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019083679A Division JP2019142934A (ja) | 2014-04-04 | 2019-04-25 | 加齢関連状態を処置するための吸入可能なラパマイシン配合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017509684A JP2017509684A (ja) | 2017-04-06 |
| JP2017509684A5 true JP2017509684A5 (enExample) | 2018-05-17 |
| JP6525285B2 JP6525285B2 (ja) | 2019-06-05 |
Family
ID=53005668
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016560802A Active JP6525285B2 (ja) | 2014-04-04 | 2015-04-06 | 加齢関連状態を処置するための吸入可能なラパマイシン配合物 |
| JP2019083679A Pending JP2019142934A (ja) | 2014-04-04 | 2019-04-25 | 加齢関連状態を処置するための吸入可能なラパマイシン配合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019083679A Pending JP2019142934A (ja) | 2014-04-04 | 2019-04-25 | 加齢関連状態を処置するための吸入可能なラパマイシン配合物 |
Country Status (21)
| Country | Link |
|---|---|
| US (5) | US20170014341A1 (enExample) |
| EP (2) | EP3125875B1 (enExample) |
| JP (2) | JP6525285B2 (enExample) |
| KR (1) | KR102352249B1 (enExample) |
| CN (1) | CN106659686A (enExample) |
| AU (1) | AU2015240485B2 (enExample) |
| BR (1) | BR112016022598A8 (enExample) |
| CA (1) | CA2944075C (enExample) |
| DK (1) | DK3125875T3 (enExample) |
| ES (1) | ES2952025T3 (enExample) |
| FI (1) | FI3125875T3 (enExample) |
| HR (1) | HRP20230863T1 (enExample) |
| HU (1) | HUE062742T2 (enExample) |
| IL (1) | IL248048A0 (enExample) |
| MX (2) | MX394266B (enExample) |
| NZ (1) | NZ724756A (enExample) |
| PL (1) | PL3125875T3 (enExample) |
| PT (1) | PT3125875T (enExample) |
| RS (1) | RS64482B1 (enExample) |
| RU (1) | RU2718583C2 (enExample) |
| WO (1) | WO2015154084A1 (enExample) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11951139B2 (en) | 2015-11-30 | 2024-04-09 | Seed Health, Inc. | Method and system for reducing the likelihood of osteoporosis |
| US11951140B2 (en) | 2011-02-04 | 2024-04-09 | Seed Health, Inc. | Modulation of an individual's gut microbiome to address osteoporosis and bone disease |
| US12279989B2 (en) | 2011-02-04 | 2025-04-22 | Seed Health, Inc. | Method and system for increasing beneficial bacteria and decreasing pathogenic bacteria in the oral cavity |
| US11844720B2 (en) | 2011-02-04 | 2023-12-19 | Seed Health, Inc. | Method and system to reduce the likelihood of dental caries and halitosis |
| US12533312B2 (en) | 2011-02-04 | 2026-01-27 | Seed Health, Inc. | Method and system for preventing sore throat in humans |
| US11998479B2 (en) | 2011-02-04 | 2024-06-04 | Seed Health, Inc. | Method and system for addressing adverse effects on the oral microbiome and restoring gingival health caused by sodium lauryl sulphate exposure |
| US12257272B2 (en) | 2015-12-24 | 2025-03-25 | Seed Health, Inc. | Method and system for reducing the likelihood of developing depression in an individual |
| US11419903B2 (en) | 2015-11-30 | 2022-08-23 | Seed Health, Inc. | Method and system for reducing the likelihood of osteoporosis |
| DK2948134T3 (da) | 2013-01-24 | 2020-06-02 | Palvella Therapeutics Inc | Sammensætninger til transdermal indgivelse af mtor-inhibitorer |
| KR102256576B1 (ko) | 2013-10-08 | 2021-05-27 | 에이아이 테라퓨틱스, 인코포레이티드 | 림프관평활근종증의 치료를 위한 라파마이신 |
| US11980643B2 (en) | 2013-12-20 | 2024-05-14 | Seed Health, Inc. | Method and system to modify an individual's gut-brain axis to provide neurocognitive protection |
| US11642382B2 (en) | 2013-12-20 | 2023-05-09 | Seed Health, Inc. | Method for treating an individual suffering from bladder cancer |
| US11213552B2 (en) | 2015-11-30 | 2022-01-04 | Joseph E. Kovarik | Method for treating an individual suffering from a chronic infectious disease and cancer |
| US12005085B2 (en) | 2013-12-20 | 2024-06-11 | Seed Health, Inc. | Probiotic method and composition for maintaining a healthy vaginal microbiome |
| US11672835B2 (en) | 2013-12-20 | 2023-06-13 | Seed Health, Inc. | Method for treating individuals having cancer and who are receiving cancer immunotherapy |
| US12329783B2 (en) | 2013-12-20 | 2025-06-17 | Seed Health, Inc. | Method and system to improve the health of a person's skin microbiome |
| US11998574B2 (en) | 2013-12-20 | 2024-06-04 | Seed Health, Inc. | Method and system for modulating an individual's skin microbiome |
| US11826388B2 (en) | 2013-12-20 | 2023-11-28 | Seed Health, Inc. | Topical application of Lactobacillus crispatus to ameliorate barrier damage and inflammation |
| US11833177B2 (en) | 2013-12-20 | 2023-12-05 | Seed Health, Inc. | Probiotic to enhance an individual's skin microbiome |
| US11529379B2 (en) | 2013-12-20 | 2022-12-20 | Seed Health, Inc. | Method and system for reducing the likelihood of developing colorectal cancer in an individual human being |
| US11026982B2 (en) | 2015-11-30 | 2021-06-08 | Joseph E. Kovarik | Method for reducing the likelihood of developing bladder or colorectal cancer in an individual human being |
| US11969445B2 (en) | 2013-12-20 | 2024-04-30 | Seed Health, Inc. | Probiotic composition and method for controlling excess weight, obesity, NAFLD and NASH |
| US12246043B2 (en) | 2013-12-20 | 2025-03-11 | Seed Health, Inc. | Topical application to treat acne vulgaris |
| US11839632B2 (en) | 2013-12-20 | 2023-12-12 | Seed Health, Inc. | Topical application of CRISPR-modified bacteria to treat acne vulgaris |
| US10307371B2 (en) | 2014-02-11 | 2019-06-04 | AI Therapeutics, Inc. | Rapamycin for the treatment of lymphangioleiomyomatosis |
| PL3125875T3 (pl) * | 2014-04-04 | 2023-11-20 | AI Therapeutics, Inc. | Nadający się do inhalacji preparat rapamycyny do leczenia stanów związanych z wiekiem |
| AU2015330905B2 (en) | 2014-10-07 | 2021-02-25 | AI Therapeutics, Inc. | An inhalable rapamycin formulation for the treatment of pulmonary hypertension |
| MA40910A (fr) * | 2014-11-07 | 2017-09-12 | Civitas Therapeutics Inc | Poudres de rapamycine pour administration pulmonaire |
| PT109030B (pt) * | 2015-12-15 | 2019-09-25 | Hovione Farmaciência, S.A. | Preparação de partículas inaláveis de zafirlucaste |
| PT109117B (pt) * | 2016-01-28 | 2019-02-01 | Hovione Farm Sa | Complexação de ingredientes ativos farmacêuticos |
| CN110520097B (zh) | 2017-01-06 | 2023-10-27 | 帕尔维拉治疗股份有限公司 | Mtor抑制剂的无水组合物及其使用方法 |
| CN108926533B (zh) * | 2017-05-24 | 2022-03-25 | 江苏天士力帝益药业有限公司 | 一种替西罗莫司脂质体及其制备方法 |
| JP2021530463A (ja) | 2018-07-02 | 2021-11-11 | パルヴェラ セラピューティクス、インク． | ｍＴＯＲ阻害剤の無水組成物および使用方法 |
| EP3962455B1 (en) | 2020-05-18 | 2022-08-31 | Orexo AB | New pharmaceutical composition for drug delivery |
| AU2020277132B1 (en) * | 2020-11-24 | 2021-11-04 | Aft Pharmaceuticals Limited | A Rapamycin Composition |
| CN113444730A (zh) * | 2021-03-17 | 2021-09-28 | 昆明市延安医院 | 一种原发性肝细胞klotho基因转导干细胞筛选构建方法 |
| WO2023094826A1 (en) | 2021-11-25 | 2023-06-01 | Orexo Ab | Pharmaceutical composition comprising adrenaline |
| GB202117016D0 (en) | 2021-11-25 | 2022-01-12 | Orexo Ab | New pharmaceutical device |
| CN114796208B (zh) * | 2022-05-27 | 2024-01-23 | 上海海洋大学 | 雷帕霉素在制备预防或治疗鲫造血器官坏死病药物中的应用 |
Family Cites Families (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2517482A (en) | 1949-04-09 | 1950-08-01 | Sharp & Dohme Inc | Inhaler |
| GB1242211A (en) | 1967-08-08 | 1971-08-11 | Fisons Pharmaceuticals Ltd | Pharmaceutical composition |
| ZA737247B (en) | 1972-09-29 | 1975-04-30 | Ayerst Mckenna & Harrison | Rapamycin and process of preparation |
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- 2015-04-06 BR BR112016022598A patent/BR112016022598A8/pt not_active Application Discontinuation
- 2015-04-06 HR HRP20230863TT patent/HRP20230863T1/hr unknown
- 2015-04-06 RS RS20230673A patent/RS64482B1/sr unknown
- 2015-04-06 CN CN201580029505.3A patent/CN106659686A/zh active Pending
- 2015-04-06 NZ NZ724756A patent/NZ724756A/en unknown
- 2015-04-06 HU HUE15718687A patent/HUE062742T2/hu unknown
- 2015-04-06 WO PCT/US2015/024551 patent/WO2015154084A1/en not_active Ceased
- 2015-04-06 CA CA2944075A patent/CA2944075C/en active Active
- 2015-04-06 JP JP2016560802A patent/JP6525285B2/ja active Active
- 2015-04-06 FI FIEP15718687.5T patent/FI3125875T3/fi active
- 2015-04-06 EP EP15718687.5A patent/EP3125875B1/en active Active
- 2015-04-06 DK DK15718687.5T patent/DK3125875T3/da active
- 2015-04-06 AU AU2015240485A patent/AU2015240485B2/en active Active
- 2015-04-06 RU RU2016143365A patent/RU2718583C2/ru active
- 2015-04-06 PT PT157186875T patent/PT3125875T/pt unknown
- 2015-04-06 KR KR1020167029824A patent/KR102352249B1/ko active Active
- 2015-04-06 US US15/301,252 patent/US20170014341A1/en not_active Abandoned
- 2015-04-06 MX MX2016012712A patent/MX394266B/es unknown
- 2015-04-06 EP EP23162835.5A patent/EP4218742A1/en not_active Withdrawn
- 2015-04-06 ES ES15718687T patent/ES2952025T3/es active Active
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