JP2006527773A5 - - Google Patents
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- JP2006527773A5 JP2006527773A5 JP2006517152A JP2006517152A JP2006527773A5 JP 2006527773 A5 JP2006527773 A5 JP 2006527773A5 JP 2006517152 A JP2006517152 A JP 2006517152A JP 2006517152 A JP2006517152 A JP 2006517152A JP 2006527773 A5 JP2006527773 A5 JP 2006527773A5
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- JP
- Japan
- Prior art keywords
- arg
- tyr
- ser
- pro
- compound
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 13
- 208000008589 Obesity Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 description 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 7
- 108090000765 processed proteins & peptides Proteins 0.000 description 6
- 239000000556 agonist Substances 0.000 description 4
- 150000001413 amino acids Chemical class 0.000 description 4
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 3
- 108700034262 4-Nle-7-Phe-alpha- MSH Proteins 0.000 description 3
- QMXOFBXZEKTJIK-UHFFFAOYSA-N Glycinol Natural products C1=C(O)C=C2OCC3(O)C4=CC=C(O)C=C4OC3C2=C1 QMXOFBXZEKTJIK-UHFFFAOYSA-N 0.000 description 3
- 108090000950 Melanocortin Receptors Proteins 0.000 description 3
- 102000004378 Melanocortin Receptors Human genes 0.000 description 3
- 102000008314 Type 1 Melanocortin Receptor Human genes 0.000 description 3
- 108010021428 Type 1 Melanocortin Receptor Proteins 0.000 description 3
- UAHFGYDRQSXQEB-LEBBXHLNSA-N afamelanotide Chemical compound C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(N)=O)NC(=O)[C@H](CO)NC(C)=O)C1=CC=C(O)C=C1 UAHFGYDRQSXQEB-LEBBXHLNSA-N 0.000 description 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 3
- 150000003839 salts Chemical class 0.000 description 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 description 2
- 102000030612 Melanocortin 5 receptor Human genes 0.000 description 2
- 108010088565 Melanocortin 5 receptor Proteins 0.000 description 2
- 102400000740 Melanocyte-stimulating hormone alpha Human genes 0.000 description 2
- 101710200814 Melanotropin alpha Proteins 0.000 description 2
- 108010021433 Type 3 Melanocortin Receptor Proteins 0.000 description 2
- 102000008318 Type 3 Melanocortin Receptor Human genes 0.000 description 2
- 102000008316 Type 4 Melanocortin Receptor Human genes 0.000 description 2
- 108010021436 Type 4 Melanocortin Receptor Proteins 0.000 description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 2
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 description 2
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 description 2
- 102000004196 processed proteins & peptides Human genes 0.000 description 2
- 108010026333 seryl-proline Proteins 0.000 description 2
- WHNFPRLDDSXQCL-UAZQEYIDSA-N α-msh Chemical compound C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(N)=O)NC(=O)[C@H](CO)NC(C)=O)C1=CC=C(O)C=C1 WHNFPRLDDSXQCL-UAZQEYIDSA-N 0.000 description 2
- ORTUTLYEGOSCRP-ATNXLWBUSA-N (2s)-2-acetamido-n-[(3s,6s,13e)-14-[[(2s)-2-[[(2s)-2-[[(2r)-2-amino-3-naphthalen-2-ylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-(2,3-dihydro-1h-indol-3-yl)propanoyl]amino]-3-(4h-imidazol-4-ylmethyl)-2,5,8,15-tetraoxo-1,4,9-triazacyclop Chemical compound C([C@H]1C(=O)NC(=O)\C(NC(=O)[C@H](CC2C3=CC=CC=C3NC2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)CC=2C=C3C=CC=CC3=CC=2)=C/CCCNC(=O)C[C@@H](C(N1)=O)NC(=O)[C@@H](NC(C)=O)CCCC)C1C=NC=N1 ORTUTLYEGOSCRP-ATNXLWBUSA-N 0.000 description 1
- 0 C*CNCCCNC(N)=N Chemical compound C*CNCCCNC(N)=N 0.000 description 1
- RMIVMBYMDISYFZ-UHFFFAOYSA-N CNCCCCN Chemical compound CNCCCCN RMIVMBYMDISYFZ-UHFFFAOYSA-N 0.000 description 1
- COLNVLDHVKWLRT-MRVPVSSYSA-N D-phenylalanine Chemical compound OC(=O)[C@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-MRVPVSSYSA-N 0.000 description 1
- AVXURJPOCDRRFD-UHFFFAOYSA-N Hydroxylamine Chemical compound ON AVXURJPOCDRRFD-UHFFFAOYSA-N 0.000 description 1
- 229940124757 MC-4 agonist Drugs 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 239000004365 Protease Substances 0.000 description 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 description 1
- 108010021820 SHU 9119 Proteins 0.000 description 1
- 150000001414 amino alcohols Chemical class 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 125000002619 bicyclic group Chemical group 0.000 description 1
- 210000004899 c-terminal region Anatomy 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000012634 fragment Substances 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 108010053037 kyotorphin Proteins 0.000 description 1
- 150000003951 lactams Chemical class 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 description 1
- 239000004031 partial agonist Substances 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 229940044601 receptor agonist Drugs 0.000 description 1
- 239000000018 receptor agonist Substances 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US47974003P | 2003-06-19 | 2003-06-19 | |
| US55734704P | 2004-03-29 | 2004-03-29 | |
| US57073704P | 2004-05-13 | 2004-05-13 | |
| US57067604P | 2004-05-13 | 2004-05-13 | |
| PCT/US2004/016625 WO2005000339A2 (en) | 2003-06-19 | 2004-06-17 | Melanocortin receptor 4(mc4) agonists and their uses |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006527773A JP2006527773A (ja) | 2006-12-07 |
| JP2006527773A5 true JP2006527773A5 (https=) | 2007-07-12 |
Family
ID=33556652
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006517152A Withdrawn JP2006527773A (ja) | 2003-06-19 | 2004-06-17 | メラノコルチン受容体４（ｍｃ４）作用薬とその用途 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US20070105759A1 (https=) |
| EP (1) | EP1644023A2 (https=) |
| JP (1) | JP2006527773A (https=) |
| KR (1) | KR20060014444A (https=) |
| AR (1) | AR044824A1 (https=) |
| AU (1) | AU2004251616A1 (https=) |
| BR (1) | BRPI0410731A (https=) |
| CA (1) | CA2530024A1 (https=) |
| CR (1) | CR8159A (https=) |
| EA (1) | EA200600055A1 (https=) |
| EC (1) | ECSP056236A (https=) |
| IL (1) | IL171931A0 (https=) |
| MX (1) | MXPA05013951A (https=) |
| NO (1) | NO20060259L (https=) |
| PE (1) | PE20050284A1 (https=) |
| TW (1) | TW200514791A (https=) |
| WO (1) | WO2005000339A2 (https=) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1658285B1 (en) | 2003-08-20 | 2007-05-02 | Eli Lilly And Company | Compounds, methods and formulations for the oral delivery of a glucagon like peptide (glp)-1 compound or an melanocortin 4 receptor (mc4) agonist peptide |
| ATE350369T1 (de) | 2003-08-20 | 2007-01-15 | Lilly Co Eli | Verbindungen, verfahren und formulierungen zur oralen verabreichung einer glucagon like peptide (glp)-1-verbindung oder eines am melanocortin-4- rezeptor (mc4) als agonist wirkenden peptids |
| WO2006073772A1 (en) * | 2005-01-05 | 2006-07-13 | Eli Lilly And Company | Polyethylene glycol linked mc4r or mc3r agonist peptides |
| NZ565217A (en) * | 2005-07-08 | 2010-03-26 | Ipsen Pharma Sas | Melanocortin receptor ligands |
| JP2009500426A (ja) * | 2005-07-08 | 2009-01-08 | ソシエテ・ドゥ・コンセイユ・ドゥ・ルシェルシュ・エ・ダプリカーション・シャンティフィック・エス・ア・エス | メラノコルチン受容体のリガンド |
| EP2061767B1 (de) | 2006-08-08 | 2014-12-17 | Sanofi | Arylaminoaryl-alkyl-substituierte Imidazolidin-2,4-dione, Verfahren zu ihrer Herstellung, diese Verbindungen enthaltende Arzneimittel und ihre Verwendung |
| TWI364290B (en) * | 2007-05-25 | 2012-05-21 | Ipsen Pharma Sas | Melanocortin receptor ligands modifled with hydantoin |
| EP2167112A4 (en) * | 2007-06-15 | 2012-01-25 | Ipsen Pharma Sas | CYCLIC PEPTIDE MELANOCORTIN RECEPTOR LIGANDS |
| EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| BRPI0819188B1 (pt) | 2007-11-05 | 2021-06-22 | Ipsen Pharma S.A.S. | Uso de melanocortinas para a preparação de um medicamento para tratar resistência à insulina |
| CN101918545A (zh) | 2008-01-02 | 2010-12-15 | 丹尼斯科美国公司 | 应用嗜糖假单胞菌g4-淀粉酶和其变体获得乙醇的无葡糖淀粉酶的方法 |
| KR101687037B1 (ko) * | 2008-06-09 | 2016-12-15 | 팔라틴 테크놀로지스 인코포레이티드 | 성기능 장애 치료용 멜라노코르틴 수용체-특이적 펩티드 |
| WO2009151383A1 (en) * | 2008-06-09 | 2009-12-17 | Palatin Technologies, Inc. | Melanocortin receptor-specific peptides for the treatment of obesity and other diseases associated with melanocortin receptor function |
| UY31968A (es) | 2008-07-09 | 2010-01-29 | Sanofi Aventis | Nuevos derivados heterocíclicos, sus procesos para su preparación, y sus usos terapéuticos |
| EP2348857B1 (en) | 2008-10-22 | 2016-02-24 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| US8329914B2 (en) | 2008-10-31 | 2012-12-11 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| WO2010068601A1 (en) | 2008-12-08 | 2010-06-17 | Sanofi-Aventis | A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof |
| CA2761607C (en) * | 2009-06-08 | 2018-09-04 | Yi-Qun Shi | Melanocortin receptor-specific peptides |
| UY32690A (es) | 2009-06-08 | 2011-01-31 | Astrazeneca Ab | Péptidos específicos para receptores de melanocortina |
| EP2440572B1 (en) | 2009-06-08 | 2017-04-05 | Palatin Technologies, Inc. | Lactam-bridged melanocortin receptor-specific peptides |
| KR20120060207A (ko) | 2009-08-26 | 2012-06-11 | 사노피 | 신규한 결정성 헤테로방향족 플루오로글리코시드 수화물, 이들 화합물을 포함하는 약제 및 이들의 용도 |
| BR112012011780A2 (pt) | 2009-11-23 | 2019-09-24 | Palatin Technologies, Inc | peptídeo linear,composição farmacêutica,métodopara tratamento de umadoença,indicação,condição ou sídrome mediadsa por receptor de melanocortina emum mamífero humano ou não humano e método para tratamento de uma condição responsiva ás alterações em função de receptor de melanocortina em um mamifero humano ou não humano |
| JP5999702B2 (ja) | 2009-11-23 | 2016-09-28 | パラティン テクノロジーズ, インコーポレイテッドPalatin Technologies, Inc. | メラノコルチン−１受容体特異的環状ペプチド |
| JP2013520502A (ja) | 2010-02-25 | 2013-06-06 | メルク・シャープ・エンド・ドーム・コーポレイション | 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体 |
| SG192941A1 (en) | 2011-02-25 | 2013-09-30 | Merck Sharp & Dohme | Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents |
| WO2012120056A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| US8895547B2 (en) | 2011-03-08 | 2014-11-25 | Sanofi | Substituted phenyl-oxathiazine derivatives, method for producing them, drugs containing said compounds and the use thereof |
| WO2012120058A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Mit benzyl- oder heteromethylengruppen substituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| EP2683699B1 (de) | 2011-03-08 | 2015-06-24 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| EP2683702B1 (de) | 2011-03-08 | 2014-12-24 | Sanofi | Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| EP2683704B1 (de) | 2011-03-08 | 2014-12-17 | Sanofi | Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| EP2766349B1 (de) | 2011-03-08 | 2016-06-01 | Sanofi | Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| US8828994B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| WO2012120051A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Mit adamantan- oder noradamantan substituierte benzyl-oxathiazinderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| LT3539551T (lt) | 2011-12-29 | 2022-01-10 | Rhythm Pharmaceuticals, Inc. | Su melanokortino-4 receptoriumi susijusių sutrikimų gydymo būdas heterozigotiniuose nešiotojuose |
| RU2015106909A (ru) | 2012-08-02 | 2016-09-27 | Мерк Шарп И Доум Корп. | Антидиабетические трициклические соединения |
| KR20150118158A (ko) | 2013-02-22 | 2015-10-21 | 머크 샤프 앤드 돔 코포레이션 | 항당뇨병 비시클릭 화합물 |
| WO2014139388A1 (en) | 2013-03-14 | 2014-09-18 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
| CN115957297A (zh) * | 2013-03-15 | 2023-04-14 | 节奏制药公司 | 药物组合物 |
| EP2970388B1 (en) * | 2013-03-15 | 2018-07-25 | Rhythm Pharmaceuticals, Inc. | Peptide compositions |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| PL3356386T3 (pl) | 2015-09-30 | 2024-08-05 | Rhythm Pharmaceuticals, Inc. | Sposób leczenia zaburzeń związanych ze szlakiem receptora melanokortyny 4 |
| US11072602B2 (en) | 2016-12-06 | 2021-07-27 | Merck Sharp & Dohme Corp. | Antidiabetic heterocyclic compounds |
| EP3558298B1 (en) | 2016-12-20 | 2026-03-11 | Merck Sharp & Dohme LLC | Antidiabetic spirochroman compounds |
| KR101917854B1 (ko) * | 2017-08-24 | 2018-11-12 | 한국콜마주식회사 | 세포 수용체 결합능이 있는 펩티드를 포함하는 마이크로 캡슐 및 이를 포함하는 화장료 조성물 |
| CN115010793A (zh) * | 2022-06-17 | 2022-09-06 | 中国农业大学 | 玫瑰叶畸形病毒外壳蛋白多克隆抗体的制备方法及应用 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4485039A (en) * | 1982-06-11 | 1984-11-27 | University Patents, Inc. | Synthetic analogues of α-melanotropin |
| US5674839A (en) * | 1987-05-22 | 1997-10-07 | Competitive Technologies, Inc. | Cyclic analogs of alpha-MSH fragments |
| GB9808229D0 (en) * | 1998-04-17 | 1998-06-17 | Quadrant Holdings Cambridge | Melanocortin receptor ligands |
| EP1137340A4 (en) * | 1998-12-09 | 2005-12-21 | Eleanor Roosevelt Inst | COMPOSITION AND METHODS FOR REGULATION OF BODY WEIGHT AND ASSOCIATED PATHOLOGIES |
| US6716810B1 (en) * | 1998-12-09 | 2004-04-06 | Eleanor Roosevelt Institute | Composition and method for regulation of body weight and associated conditions |
| GB9827500D0 (en) * | 1998-12-14 | 1999-02-10 | Wapharm Ab | Compounds for control of eating, growth and body weight |
| CA2368431C (en) * | 1999-03-29 | 2006-01-24 | The Procter & Gamble Company | Melanocortin receptor ligands |
| US6579968B1 (en) * | 1999-06-29 | 2003-06-17 | Palatin Technologies, Inc. | Compositions and methods for treatment of sexual dysfunction |
| US6659982B2 (en) * | 2000-05-08 | 2003-12-09 | Sterling Medivations, Inc. | Micro infusion drug delivery device |
| SI1315750T1 (sl) * | 2000-08-30 | 2007-06-30 | Hoffmann La Roche | Cikliäśni peptidi kot agonisti za receptorje melanokortina-4 |
| US6960646B2 (en) * | 2001-07-12 | 2005-11-01 | Merck & Co., Inc. | Cyclic peptides as potent and selective melanocortin-4 receptors agonists |
-
2004
- 2004-06-17 EP EP04753454A patent/EP1644023A2/en not_active Withdrawn
- 2004-06-17 WO PCT/US2004/016625 patent/WO2005000339A2/en not_active Ceased
- 2004-06-17 BR BRPI0410731-4A patent/BRPI0410731A/pt not_active Application Discontinuation
- 2004-06-17 MX MXPA05013951A patent/MXPA05013951A/es unknown
- 2004-06-17 JP JP2006517152A patent/JP2006527773A/ja not_active Withdrawn
- 2004-06-17 AU AU2004251616A patent/AU2004251616A1/en not_active Abandoned
- 2004-06-17 US US10/556,689 patent/US20070105759A1/en not_active Abandoned
- 2004-06-17 CA CA002530024A patent/CA2530024A1/en not_active Abandoned
- 2004-06-17 KR KR1020057024261A patent/KR20060014444A/ko not_active Ceased
- 2004-06-17 EA EA200600055A patent/EA200600055A1/ru unknown
- 2004-06-18 PE PE2004000599A patent/PE20050284A1/es not_active Application Discontinuation
- 2004-06-18 TW TW093117823A patent/TW200514791A/zh unknown
- 2004-06-18 AR ARP040102134A patent/AR044824A1/es unknown
-
2005
- 2005-11-13 IL IL171931A patent/IL171931A0/en unknown
- 2005-12-16 EC EC2005006236A patent/ECSP056236A/es unknown
- 2005-12-16 CR CR8159A patent/CR8159A/es unknown
-
2006
- 2006-01-18 NO NO20060259A patent/NO20060259L/no not_active Application Discontinuation
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