NZ554720A - Compositions and uses of fingolimod (2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol) - Google Patents
Compositions and uses of fingolimod (2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol)Info
- Publication number
- NZ554720A NZ554720A NZ554720A NZ55472005A NZ554720A NZ 554720 A NZ554720 A NZ 554720A NZ 554720 A NZ554720 A NZ 554720A NZ 55472005 A NZ55472005 A NZ 55472005A NZ 554720 A NZ554720 A NZ 554720A
- Authority
- NZ
- New Zealand
- Prior art keywords
- agonist
- receptor modulator
- daily dosage
- day
- ethyl
- Prior art date
Links
- KKGQTZUTZRNORY-UHFFFAOYSA-N fingolimod Chemical compound CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 KKGQTZUTZRNORY-UHFFFAOYSA-N 0.000 title claims abstract description 53
- 229960000556 fingolimod Drugs 0.000 title claims abstract description 48
- 239000000203 mixture Substances 0.000 title description 2
- 102000011011 Sphingosine 1-phosphate receptors Human genes 0.000 claims abstract description 110
- 108050001083 Sphingosine 1-phosphate receptors Proteins 0.000 claims abstract description 107
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- 239000000556 agonist Substances 0.000 claims abstract description 85
- 229940075993 receptor modulator Drugs 0.000 claims abstract description 84
- 238000011282 treatment Methods 0.000 claims abstract description 46
- 229940079593 drug Drugs 0.000 claims abstract description 38
- 239000003814 drug Substances 0.000 claims abstract description 38
- 150000003839 salts Chemical group 0.000 claims abstract description 28
- 230000036765 blood level Effects 0.000 claims abstract description 16
- 208000023275 Autoimmune disease Diseases 0.000 claims abstract description 11
- KIHYPELVXPAIDH-UHFFFAOYSA-N 1-[[4-[n-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-c-methylcarbonimidoyl]-2-ethylphenyl]methyl]azetidine-3-carboxylic acid Chemical compound CCC1=CC(C(C)=NOCC=2C=C(C(C3CCCCC3)=CC=2)C(F)(F)F)=CC=C1CN1CC(C(O)=O)C1 KIHYPELVXPAIDH-UHFFFAOYSA-N 0.000 claims abstract description 5
- 206010052779 Transplant rejections Diseases 0.000 claims abstract description 5
- UKNPZNCFUIYBMA-UHFFFAOYSA-N 5-amino-5-[2-chloro-4-(2-phenylmethoxyphenyl)sulfanylphenyl]pentane-1,3-diol Chemical compound NC(CC(CCO)O)C1=C(C=C(C=C1)SC1=C(C=CC=C1)OCC1=CC=CC=C1)Cl UKNPZNCFUIYBMA-UHFFFAOYSA-N 0.000 claims abstract description 3
- MIYSLZPNGDBEIR-UHFFFAOYSA-N 5-amino-5-[2-chloro-4-(3-phenylmethoxyphenoxy)phenyl]pentane-1,3-diol Chemical compound C1=C(Cl)C(C(CC(O)CCO)N)=CC=C1OC1=CC=CC(OCC=2C=CC=CC=2)=C1 MIYSLZPNGDBEIR-UHFFFAOYSA-N 0.000 claims abstract description 3
- 230000005764 inhibitory process Effects 0.000 claims abstract 2
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- 238000000034 method Methods 0.000 claims description 9
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- 238000004458 analytical method Methods 0.000 claims 1
- 238000001294 liquid chromatography-tandem mass spectrometry Methods 0.000 claims 1
- 238000012216 screening Methods 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 description 49
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- 125000005843 halogen group Chemical group 0.000 description 32
- 125000000217 alkyl group Chemical group 0.000 description 29
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 27
- 150000002367 halogens Chemical class 0.000 description 25
- -1 2-substituted 2-amino- propane-1,3-diol Chemical class 0.000 description 24
- 229910052739 hydrogen Inorganic materials 0.000 description 17
- 125000002252 acyl group Chemical group 0.000 description 16
- 239000000018 receptor agonist Substances 0.000 description 14
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 12
- 125000001424 substituent group Chemical group 0.000 description 11
- 238000004519 manufacturing process Methods 0.000 description 10
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 8
- 125000003118 aryl group Chemical group 0.000 description 8
- 125000000623 heterocyclic group Chemical group 0.000 description 8
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- 125000004423 acyloxy group Chemical group 0.000 description 7
- 125000004442 acylamino group Chemical group 0.000 description 6
- 238000003556 assay Methods 0.000 description 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 6
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- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 description 2
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
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- 125000003072 pyrazolidinyl group Chemical group 0.000 description 2
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- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 description 2
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
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- GWGANHYLDPKJLO-HSZRJFAPSA-N (2r)-2-amino-4-[3-(4-cyclohexyloxybutyl)-1-benzothiophen-6-yl]-2-methylbutan-1-ol Chemical compound C=1SC2=CC(CC[C@@](N)(CO)C)=CC=C2C=1CCCCOC1CCCCC1 GWGANHYLDPKJLO-HSZRJFAPSA-N 0.000 description 1
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- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 description 1
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- YPFDHNVEDLHUCE-UHFFFAOYSA-N 1,3-propanediol Substances OCCCO YPFDHNVEDLHUCE-UHFFFAOYSA-N 0.000 description 1
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- FLBPTSOAFRMSPF-UHFFFAOYSA-N 1-[4-[3-amino-4-hydroxy-3-(hydroxymethyl)butyl]phenyl]-5-phenylpentan-1-one Chemical compound C1=CC(CCC(CO)(CO)N)=CC=C1C(=O)CCCCC1=CC=CC=C1 FLBPTSOAFRMSPF-UHFFFAOYSA-N 0.000 description 1
- JKMHFZQWWAIEOD-UHFFFAOYSA-N 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid Chemical compound OCC[NH+]1CCN(CCS([O-])(=O)=O)CC1 JKMHFZQWWAIEOD-UHFFFAOYSA-N 0.000 description 1
- BXIWYZLGTUWLCD-UHFFFAOYSA-N 2-amino-2-tetradecylpropane-1,3-diol Chemical compound CCCCCCCCCCCCCCC(N)(CO)CO BXIWYZLGTUWLCD-UHFFFAOYSA-N 0.000 description 1
- ITJCKQTXCLGXHE-UHFFFAOYSA-N 2-amino-4-(4-heptoxyphenyl)-2-methylbutan-1-ol Chemical compound CCCCCCCOC1=CC=C(CCC(C)(N)CO)C=C1 ITJCKQTXCLGXHE-UHFFFAOYSA-N 0.000 description 1
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- NESAWTWENPISNE-UHFFFAOYSA-N 5-amino-5-[2-chloro-4-(3-phenylmethoxyphenoxy)phenyl]hexane-1,3-diol Chemical compound C1=C(Cl)C(C(N)(CC(O)CCO)C)=CC=C1OC1=CC=CC(OCC=2C=CC=CC=2)=C1 NESAWTWENPISNE-UHFFFAOYSA-N 0.000 description 1
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- 125000004115 pentoxy group Chemical group [*]OC([H])([H])C([H])([H])C([H])([H])C(C([H])([H])[H])([H])[H] 0.000 description 1
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- 230000000144 pharmacologic effect Effects 0.000 description 1
- 230000026731 phosphorylation Effects 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
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- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
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- LVTJOONKWUXEFR-FZRMHRINSA-N protoneodioscin Natural products O(C[C@@H](CC[C@]1(O)[C@H](C)[C@@H]2[C@]3(C)[C@H]([C@H]4[C@@H]([C@]5(C)C(=CC4)C[C@@H](O[C@@H]4[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@@H](O)[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@H](CO)O4)CC5)CC3)C[C@@H]2O1)C)[C@H]1[C@H](O)[C@H](O)[C@H](O)[C@@H](CO)O1 LVTJOONKWUXEFR-FZRMHRINSA-N 0.000 description 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
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- DUYSYHSSBDVJSM-KRWOKUGFSA-N sphingosine 1-phosphate Chemical compound CCCCCCCCCCCCC\C=C\[C@@H](O)[C@@H](N)COP(O)(O)=O DUYSYHSSBDVJSM-KRWOKUGFSA-N 0.000 description 1
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Classifications
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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Landscapes
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
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| BRPI0514316A (pt) | 2004-08-13 | 2008-06-10 | Praecis Pharm Inc | métodos e composições para modulação de atividade de receptor de esfingosina-1-fosfato (s1p) |
| CN102600472A (zh) * | 2004-11-29 | 2012-07-25 | 诺瓦提斯公司 | S1p受体激动剂的剂量方案 |
| SG165364A1 (en) * | 2005-09-09 | 2010-10-28 | Novartis Ag | Treatment of autoimmune diseases |
| GB0612721D0 (en) * | 2006-06-27 | 2006-08-09 | Novartis Ag | Organic compounds |
| CN101674819A (zh) | 2007-05-04 | 2010-03-17 | 诺瓦提斯公司 | S1p受体调节剂的用途 |
| HRP20170246T4 (hr) * | 2008-03-17 | 2020-02-07 | Actelion Pharmaceuticals Ltd. | Režim doziranja za selektivni agonist s1p1-receptora |
| JPWO2009142195A1 (ja) * | 2008-05-20 | 2011-09-29 | 杏林製薬株式会社 | 寛解導入維持剤 |
| DK2307007T3 (da) * | 2008-07-23 | 2014-11-10 | Novartis Ag | Sphingosin-1-phosphat-receptormodulatorer samt deres anvendelse til behandling af muskelinflammation |
| PT2326325E (pt) | 2008-08-18 | 2015-02-05 | Novartis Ag | Derivado de azetidina para o tratamento de neuropatias periféricas |
| CA2747558A1 (en) * | 2008-12-18 | 2010-07-15 | Novartis Ag | New salts |
| KR20110112352A (ko) * | 2008-12-18 | 2011-10-12 | 노파르티스 아게 | 1-（4-｛ｌ-［（ｅ）-4-시클로헥실-3-트리플루오로메틸-벤질옥시이미노］-에틸｝-2-에틸-벤질）-아제티딘-3-카르복실산의 신규한 다형체 형태 |
| KR20160064245A (ko) * | 2008-12-18 | 2016-06-07 | 노파르티스 아게 | 1-［4-［1-(4-시클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸］-2-에틸-벤질］-아제티딘-3-카르복실산의 헤미푸마레이트 염 |
| LT3453387T (lt) * | 2008-12-22 | 2020-08-25 | Novartis Ag | S1p receptoriaus antagonisto dozavimo režimas |
| DK2379069T3 (en) * | 2008-12-22 | 2015-06-08 | Novartis Ag | Dosage Plan for an S1P receptor agonist |
| AU2015275246B2 (en) * | 2008-12-22 | 2018-02-01 | Novartis Ag | Dosage regimen for a S1P receptor agonist |
| SG178987A1 (en) * | 2009-09-29 | 2012-04-27 | Novartis Ag | Dosage regimen of an s1p receptor modulator |
| US20110124605A1 (en) * | 2009-11-20 | 2011-05-26 | Shreeram Aradhye | Use of an S1P Receptor Agonist |
| US8791100B2 (en) | 2010-02-02 | 2014-07-29 | Novartis Ag | Aryl benzylamine compounds |
| CN102917698A (zh) * | 2010-05-06 | 2013-02-06 | 诺瓦提斯公司 | 二芳基硫醚衍生物的给药方案 |
| HRP20191842T1 (hr) | 2011-01-07 | 2019-12-27 | Novartis Ag | Formulacije imunosupresiva |
| CN103889408A (zh) * | 2011-10-21 | 2014-06-25 | 诺华股份有限公司 | S1p受体调节剂或激动剂的剂量方案 |
| EP2885266B1 (en) | 2012-08-17 | 2020-03-18 | Actelion Pharmaceuticals Ltd | Process for the preparation of (2z,5z)-5-(3-chloro-4-((r)-2,3-dihydroxypropoxy)benzylidene)-2-(propylimino)-3-(o-tolyl)thiazolidin-4-one and intermediate used in said process |
| CN102887829B (zh) * | 2012-09-05 | 2014-07-02 | 中国科学院上海药物研究所 | 芬戈莫德粘酸盐及其晶体的制备方法和用途 |
| US10675254B2 (en) | 2013-10-11 | 2020-06-09 | Teikoku Seiyaku Co., Ltd. | Sphingosine-1-phosphate receptor agonist iontophoretic devices and methods of using the same |
| EP3054933A4 (en) | 2013-10-11 | 2017-03-15 | Teikoku Pharma USA, Inc. | Topical sphingosine-1-phosphate receptor agonist formulations and methods of using the same |
| KR102590068B1 (ko) | 2014-12-11 | 2023-10-16 | 액테리온 파마슈티칼 리미티드 | 선택적 s1p1 수용체 효능제에 대한 투약 섭생 |
| MA41139A (fr) | 2014-12-11 | 2017-10-17 | Actelion Pharmaceuticals Ltd | Combinaison pharmaceutique comportant un agoniste sélectif du récepteur sip1 |
| CA2973540A1 (en) | 2015-02-26 | 2016-09-01 | Novartis Ag | Treatment of autoimmune disease in a patient receiving additionally a beta-blocker |
| US10250466B2 (en) * | 2016-03-29 | 2019-04-02 | Juniper Networks, Inc. | Application signature generation and distribution |
| US11629124B2 (en) | 2017-03-09 | 2023-04-18 | Novartis Ag | Solid forms comprising an oxime ether compound, compositions and methods of use thereof |
| MX2022005014A (es) | 2019-10-31 | 2022-05-16 | Idorsia Pharmaceuticals Ltd | Combinacion de un antagonista de cxcr7 con un modulador del receptor s1p1. |
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| JP2579602B2 (ja) * | 1992-10-21 | 1997-02-05 | 吉富製薬株式会社 | ２−アミノ−１，３−プロパンジオール化合物および免疫抑制剤 |
| DE69524962D1 (de) | 1994-08-22 | 2002-02-14 | Welfide Corp | Benzolderivate und deren medizinische verwendung |
| SK282225B6 (sk) * | 1995-12-28 | 2001-12-03 | Welfide Corporation | Použitie 2-amino-2[2-(4-oktylfenyl)etyl]-propán-1,3-diolu alebo jeho farmaceuticky prijateľnej adičnej soli s kyselinou na výrobu farmaceutického prostriedku |
| US6476004B1 (en) * | 1996-07-18 | 2002-11-05 | Mitsubishi Pharma Corporation | Pharmaceutical composition |
| DK0990440T3 (da) * | 1997-02-27 | 2009-02-23 | Novartis Ag | Farmaceutisk sammensætning indeholdende 2-amino-2[2-(4-octylphenyl)-ethyl]-propan-1,3-diol, en lecithin og et saccharid |
| IL155065A (en) | 1997-04-04 | 2004-01-04 | Mitsubishi Pharma Corp | History - 2 Aminopropene - 1, 3 - Diol and Pharmaceutical Preparations Containing Them |
| JPH1180026A (ja) * | 1997-09-02 | 1999-03-23 | Yoshitomi Pharmaceut Ind Ltd | 新規免疫抑制剤、その使用方法およびその同定方法 |
| JPH11116479A (ja) * | 1997-10-10 | 1999-04-27 | Sugen Inc | 脳癌のための組み合わせ化学療法処置 |
| PL359411A1 (en) | 2000-07-13 | 2004-08-23 | Sankyo Company, Limited | Amino alcohol derivatives |
| AU2001285331B2 (en) | 2000-08-31 | 2006-04-06 | Merck & Co., Inc. | Phosphate derivatives as immunoregulatory agents |
| ATE314383T1 (de) | 2001-03-26 | 2006-01-15 | Novartis Pharma Gmbh | 2-amino-propanol derivate |
| ES2261655T3 (es) * | 2001-04-02 | 2006-11-16 | Astrazeneca Ab | Composicion farmaceutica solida que comprende 4'-ciano-trifluoro-3-(4-fluorofenilsulfonil)-2-hidroxi-2-metilpropiono-m-toluiduro y pvp. |
| JP4679035B2 (ja) * | 2001-04-02 | 2011-04-27 | ジェネンテック， インコーポレイテッド | 併用療法 |
| JP2002316985A (ja) | 2001-04-20 | 2002-10-31 | Sankyo Co Ltd | ベンゾチオフェン誘導体 |
| RU2003136730A (ru) * | 2001-06-08 | 2005-05-20 | Новартис АГ (CH) | Лечение или профилактика отторжения инсулин-продуцирующего клеточного трансплантата |
| US6963012B2 (en) * | 2001-09-27 | 2005-11-08 | Kyorin Pharmaceutical Co., Ltd. | Diaryl ether derivative, addition salt thereof, and immunosuppressant |
| PT1431284E (pt) | 2001-09-27 | 2008-01-21 | Kyorin Seiyaku Kk | Derivado de sulfureto de diarilo, um seu sal de adição e imunossupressor |
| ATE441654T1 (de) | 2002-01-18 | 2009-09-15 | Merck & Co Inc | Edg-rezeptoragonisten |
| ATE448193T1 (de) | 2002-01-18 | 2009-11-15 | Merck & Co Inc | ßN-(BENZYL)AMINOALKYL CARBOXYLATE, PHOSPHINATE, PHOSPHONATE UND TETRAZOLE ALS EDG REZEPTORAGONISTENß |
| CA2472680A1 (en) | 2002-01-18 | 2003-07-31 | Merck & Co., Inc. | Selective s1p1/edg1 receptor agonists |
| EP2251007A3 (en) * | 2002-09-24 | 2011-03-23 | Novartis AG | Sphingosine-1-phosphate (S1P) receptor agonists for use in the treatment of demyelinating diseases |
| BRPI0410439A (pt) | 2003-05-19 | 2006-06-06 | Irm Llc | compostos e composições imunossupressoras |
| MY150088A (en) * | 2003-05-19 | 2013-11-29 | Irm Llc | Immunosuppressant compounds and compositions |
| UA74941C2 (en) | 2004-04-26 | 2006-02-15 | Fos Internat S A | A metal-thermal process for producing magnesium and vacuum induction furnace for realizing the same |
| WO2005113330A1 (en) | 2004-05-05 | 2005-12-01 | Adler, Richard, S. | Systems and methods for protecting ship from attack on the surface or under water |
| JPWO2006041015A1 (ja) * | 2004-10-12 | 2008-05-15 | 杏林製薬株式会社 | アミノアルコール誘導体とその付加塩及び免疫抑制剤 |
| CN102600472A (zh) * | 2004-11-29 | 2012-07-25 | 诺瓦提斯公司 | S1p受体激动剂的剂量方案 |
| GT200600350A (es) * | 2005-08-09 | 2007-03-28 | Formulaciones líquidas |
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- 2005-11-28 KR KR1020147018084A patent/KR20140095109A/ko not_active Withdrawn
- 2005-11-28 SG SG200907947-6A patent/SG158096A1/en unknown
- 2005-11-28 MX MX2007006373A patent/MX2007006373A/es active IP Right Grant
- 2005-11-28 US US11/720,205 patent/US20090275553A1/en not_active Abandoned
- 2005-11-28 PL PL05826219T patent/PL1819326T3/pl unknown
- 2005-11-28 EP EP10179083A patent/EP2384749A1/en not_active Withdrawn
- 2005-11-28 BR BRPI0518674-9A patent/BRPI0518674A2/pt not_active Application Discontinuation
- 2005-11-28 ES ES05826219.7T patent/ES2495690T3/es not_active Expired - Lifetime
- 2005-11-28 KR KR1020077011969A patent/KR20070085465A/ko not_active Ceased
- 2005-11-28 RU RU2007124327/15A patent/RU2478384C2/ru not_active IP Right Cessation
- 2005-11-28 KR KR20157005416A patent/KR20150028858A/ko not_active Ceased
- 2005-11-28 EP EP10179081A patent/EP2359821A1/en not_active Withdrawn
- 2005-11-28 EP EP05826219.7A patent/EP1819326B1/en not_active Revoked
- 2005-11-28 PT PT58262197T patent/PT1819326E/pt unknown
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2007
- 2007-04-24 ZA ZA200703328A patent/ZA200703328B/xx unknown
- 2007-05-10 IL IL183134A patent/IL183134A0/en unknown
- 2007-05-10 NO NO20072401A patent/NO20072401L/no not_active Application Discontinuation
- 2007-05-22 MA MA29926A patent/MA29034B1/fr unknown
- 2007-05-28 TN TNP2007000209A patent/TNSN07209A1/fr unknown
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2011
- 2011-11-22 US US13/302,881 patent/US20120071446A1/en not_active Abandoned
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2012
- 2012-02-27 JP JP2012040574A patent/JP2012107059A/ja not_active Withdrawn
- 2012-10-02 RU RU2012141951/15A patent/RU2012141951A/ru unknown
- 2012-11-06 NO NO20121305A patent/NO20121305L/no not_active Application Discontinuation
- 2012-12-06 IL IL223502A patent/IL223502A0/en unknown
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2013
- 2013-03-05 JP JP2013043351A patent/JP2013129664A/ja not_active Withdrawn
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2014
- 2014-10-16 US US14/516,153 patent/US20150087720A1/en not_active Abandoned
- 2014-12-26 JP JP2014266267A patent/JP2015061883A/ja active Pending
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| RENW | Renewal (renewal fees accepted) | ||
| PSEA | Patent sealed | ||
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| LAPS | Patent lapsed |