JP2010514829A5 - - Google Patents
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- Publication number
- JP2010514829A5 JP2010514829A5 JP2009544448A JP2009544448A JP2010514829A5 JP 2010514829 A5 JP2010514829 A5 JP 2010514829A5 JP 2009544448 A JP2009544448 A JP 2009544448A JP 2009544448 A JP2009544448 A JP 2009544448A JP 2010514829 A5 JP2010514829 A5 JP 2010514829A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound
- compound according
- table below
- 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
- 150000003839 salts Chemical class 0.000 claims 36
- 150000001875 compounds Chemical class 0.000 claims 35
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- -1 n- propyl Chemical group 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 claims 1
- 101000996752 Homo sapiens Glucose-dependent insulinotropic receptor Proteins 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000036186 satiety Effects 0.000 claims 1
- 235000019627 satiety Nutrition 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0700124A GB0700124D0 (en) | 2007-01-04 | 2007-01-04 | GPCR agonists |
| GB0708740A GB0708740D0 (en) | 2007-05-08 | 2007-05-08 | Gpcr agonists |
| GB0719762A GB0719762D0 (en) | 2007-10-10 | 2007-10-10 | GPCR agonists |
| PCT/GB2008/050011 WO2008081205A1 (en) | 2007-01-04 | 2008-01-04 | Piperidine gpcr agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010514829A JP2010514829A (ja) | 2010-05-06 |
| JP2010514829A5 true JP2010514829A5 (enExample) | 2011-02-24 |
Family
ID=39203222
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009544448A Pending JP2010514829A (ja) | 2007-01-04 | 2008-01-04 | ピペリジンｇｐｃｒアゴニスト |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US20100022591A1 (enExample) |
| EP (2) | EP2383270A1 (enExample) |
| JP (1) | JP2010514829A (enExample) |
| KR (1) | KR20090104092A (enExample) |
| CN (1) | CN101627036A (enExample) |
| AR (1) | AR064736A1 (enExample) |
| AT (1) | ATE531710T1 (enExample) |
| AU (1) | AU2008203673A1 (enExample) |
| BR (1) | BRPI0806468A2 (enExample) |
| CA (1) | CA2674093A1 (enExample) |
| CL (1) | CL2008000017A1 (enExample) |
| DK (1) | DK2114931T3 (enExample) |
| EA (1) | EA015805B9 (enExample) |
| ES (1) | ES2376015T3 (enExample) |
| HR (1) | HRP20110964T1 (enExample) |
| IL (1) | IL199680A0 (enExample) |
| MA (1) | MA31084B1 (enExample) |
| MX (1) | MX2009007180A (enExample) |
| NZ (1) | NZ578144A (enExample) |
| PE (1) | PE20081849A1 (enExample) |
| PL (1) | PL2114931T3 (enExample) |
| PT (1) | PT2114931E (enExample) |
| RS (1) | RS52168B (enExample) |
| SA (1) | SA08280756B1 (enExample) |
| SI (1) | SI2114931T1 (enExample) |
| TW (1) | TWI380818B (enExample) |
| WO (1) | WO2008081205A1 (enExample) |
Families Citing this family (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| US7501426B2 (en) | 2004-02-18 | 2009-03-10 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions |
| DE102004054054A1 (de) | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
| WO2006067531A1 (en) * | 2004-12-24 | 2006-06-29 | Prosidion Ltd | G-protein coupled receptor (gpr116) agonists and use thereof for treating obesity and diabetes |
| NZ564759A (en) * | 2005-06-30 | 2011-08-26 | Prosidion Ltd | GPCR agonists |
| DE102005035891A1 (de) | 2005-07-30 | 2007-02-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| CN102838599A (zh) | 2006-05-04 | 2012-12-26 | 贝林格尔.英格海姆国际有限公司 | 多晶型 |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| CL2008000018A1 (es) * | 2007-01-04 | 2008-08-01 | Prosidion Ltd | Compuestos derivados de heterociclos de nitrogeno y oxigeno, agonistas de gpcr; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de la obesidad, diabetes, sindrome metabolico, hiperlipidemia, toleranci |
| WO2009034388A1 (en) | 2007-09-10 | 2009-03-19 | Prosidion Limited | Compounds for the treatment of metabolic disorders |
| BRPI0817881A2 (pt) | 2007-10-10 | 2015-03-31 | Novartis Ag | Compostos orgânicos e seus usos |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| GB0812648D0 (en) * | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| GB0812642D0 (en) * | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| GB0812649D0 (en) * | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| AU2009268527B2 (en) | 2008-07-11 | 2012-11-01 | Irm Llc | 4-phenoxymethylpiperidines as modulators of GPR119 activity |
| KR20200118243A (ko) | 2008-08-06 | 2020-10-14 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| BRPI0919288A2 (pt) | 2008-09-10 | 2015-12-15 | Boehring Ingelheim Internat Gmbh | teriapia de combinação para tratamento de diabetes e condições relacionadas. |
| US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| EA022310B1 (ru) | 2008-12-23 | 2015-12-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Солевые формы органического соединения |
| AR074990A1 (es) | 2009-01-07 | 2011-03-02 | Boehringer Ingelheim Int | Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina |
| GB0904285D0 (en) | 2009-03-12 | 2009-04-22 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| GB0904287D0 (en) | 2009-03-12 | 2009-04-22 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| GB0904284D0 (en) | 2009-03-12 | 2009-04-22 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| NZ596445A (en) | 2009-06-24 | 2013-04-26 | Boehringer Ingelheim Int | New compounds, pharmaceutical composition and methods relating thereto |
| JP2012530758A (ja) | 2009-06-24 | 2012-12-06 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規化合物、医薬組成物及びそれに関する方法 |
| EP2464228B1 (en) * | 2009-08-13 | 2017-12-06 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment |
| NZ599298A (en) | 2009-11-27 | 2014-11-28 | Boehringer Ingelheim Int | Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| EP2547339A1 (en) | 2010-03-18 | 2013-01-23 | Boehringer Ingelheim International GmbH | Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions |
| GB201006167D0 (en) | 2010-04-14 | 2010-05-26 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| GB201006166D0 (en) | 2010-04-14 | 2010-05-26 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| ITMI20100770A1 (it) | 2010-05-03 | 2011-11-04 | Dipharma Francis Srl | Procedimento per la preparazione di 3-(4-piridinil)-propanolo e suoi intermedi |
| WO2011138421A1 (en) | 2010-05-05 | 2011-11-10 | Boehringer Ingelheim International Gmbh | Combination therapy |
| TW201209054A (en) | 2010-05-28 | 2012-03-01 | Prosidion Ltd | Novel compounds |
| ITMI20100984A1 (it) | 2010-05-31 | 2011-12-01 | Dipharma Francis Srl | Procedimento per la preparazione di ossadiazoli |
| US8933024B2 (en) | 2010-06-18 | 2015-01-13 | Sanofi | Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| NZ603319A (en) | 2010-06-24 | 2015-04-24 | Boehringer Ingelheim Int | Diabetes therapy |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| AR083878A1 (es) | 2010-11-15 | 2013-03-27 | Boehringer Ingelheim Int | Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento |
| WO2012066077A1 (en) | 2010-11-18 | 2012-05-24 | Prosidion Limited | 1,4 di substituted pyrrolidine - 3 - yl -amine derivatives and their use for the treatment of metabolic disorders |
| GB201114389D0 (en) | 2011-08-22 | 2011-10-05 | Prosidion Ltd | Novel compounds |
| EP2693882B1 (en) * | 2011-04-08 | 2017-06-28 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment |
| AU2012267556B9 (en) | 2011-06-09 | 2017-05-11 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of GPR-119 |
| CA2838079A1 (en) | 2011-06-16 | 2012-12-20 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds, and methods of treatment |
| CA2841552C (en) | 2011-07-15 | 2020-06-23 | Boehringer Ingelheim International Gmbh | Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| EP2760855B1 (en) | 2011-09-30 | 2017-03-15 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds as well as their use in treating type-2 diabetes |
| US9018200B2 (en) | 2011-10-24 | 2015-04-28 | Merck Sharp & Dohme Corp. | Substituted piperidinyl compounds useful as GPR119 agonists |
| US9018224B2 (en) | 2011-11-15 | 2015-04-28 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds useful as GPR119 agonists |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| US20130303554A1 (en) | 2012-05-14 | 2013-11-14 | Boehringer Ingelheim International Gmbh | Use of a dpp-4 inhibitor in sirs and/or sepsis |
| EP3685839A1 (en) | 2012-05-14 | 2020-07-29 | Boehringer Ingelheim International GmbH | Linagliptin for use in the treatment of albuminuria and kidney related diseases |
| WO2013174767A1 (en) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference |
| ES2950384T3 (es) | 2014-02-28 | 2023-10-09 | Boehringer Ingelheim Int | Uso médico de un inhibidor de DPP-4 |
| KR101726819B1 (ko) * | 2014-10-27 | 2017-04-13 | 동아에스티 주식회사 | Gpr119 작용 활성을 갖는 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 약제학적 조성물 |
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| EP3421455B1 (en) * | 2017-06-29 | 2019-03-27 | F.I.S.- Fabbrica Italiana Sintetici S.p.A. | Improved process for the preparation of chiral 3-amino-piperidins, useful intermediates for the preparation of tofacitinib |
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| KR20050111588A (ko) | 2003-02-13 | 2005-11-25 | 사노피-아벤티스 도이칠란트 게엠베하 | 치환된 헥사하이드로피라지노[1,2-ａ]피리미딘-4,7-디온유도체, 이의 제조방법 및 약제로서의 이의 용도 |
| RU2005128499A (ru) | 2003-02-13 | 2006-01-27 | Санофи-Авентис Дойчланд Гмбх (De) | Замещенные у азота производные гексагидропиразино (1,2-а) пиримидин-4, 7-диона, способ их получения и их применение в качестве лекарственного средства |
| US7169797B2 (en) * | 2003-02-14 | 2007-01-30 | Abbott Laboratories | Protein-tyrosine phosphatase inhibitors and uses thereof |
| US20040167188A1 (en) * | 2003-02-14 | 2004-08-26 | Zhili Xin | Protein-tyrosine phosphatase inhibitors and uses thereof |
| US20060172019A1 (en) | 2003-03-07 | 2006-08-03 | Ralston Stuart H | Cannabinoid receptor inverse agonists and neutral antagonists as therapeutic agents for the treatment of bone disorders |
| US7232823B2 (en) | 2003-06-09 | 2007-06-19 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
| AR045496A1 (es) * | 2003-08-29 | 2005-11-02 | Schering Corp | Analolgos de benzimidazolpiperidinas 2- substiyuidas como antagonistas de los receptores de la hormona que concentra melanina selectivos para el tratamiento de la obesidad y trastornos relacionados |
| BRPI0418149A (pt) | 2003-12-24 | 2007-04-17 | Prosidion Ltd | derivados heterocìclicos como agonistas do receptor de gprc |
| WO2006067531A1 (en) | 2004-12-24 | 2006-06-29 | Prosidion Ltd | G-protein coupled receptor (gpr116) agonists and use thereof for treating obesity and diabetes |
| EP1838706A1 (en) | 2004-12-24 | 2007-10-03 | Prosidion Limited | G-protein coupled receptor agonists |
| GB0428514D0 (en) | 2004-12-31 | 2005-02-09 | Prosidion Ltd | Compounds |
| DOP2006000008A (es) * | 2005-01-10 | 2006-08-31 | Arena Pharm Inc | Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1 |
| NZ564759A (en) | 2005-06-30 | 2011-08-26 | Prosidion Ltd | GPCR agonists |
| WO2007003960A1 (en) | 2005-06-30 | 2007-01-11 | Prosidion Limited | Gpcr agonists |
| JP2008545008A (ja) | 2005-06-30 | 2008-12-11 | プロシディオン・リミテッド | Ｇｐｃｒアゴニスト |
| US20090203676A1 (en) | 2005-06-30 | 2009-08-13 | Oscar Barba | G-protein Coupled Receptor Agonists |
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| CN101657471B (zh) * | 2006-12-06 | 2013-07-03 | 史密丝克莱恩比彻姆公司 | 二环化合物及其作为抗糖尿病药的用途 |
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| CL2008000018A1 (es) * | 2007-01-04 | 2008-08-01 | Prosidion Ltd | Compuestos derivados de heterociclos de nitrogeno y oxigeno, agonistas de gpcr; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de la obesidad, diabetes, sindrome metabolico, hiperlipidemia, toleranci |
-
2008
- 2008-01-03 AR ARP080100018A patent/AR064736A1/es not_active Application Discontinuation
- 2008-01-03 PE PE2008000085A patent/PE20081849A1/es not_active Application Discontinuation
- 2008-01-03 CL CL200800017A patent/CL2008000017A1/es unknown
- 2008-01-04 AT AT08700184T patent/ATE531710T1/de active
- 2008-01-04 CN CN200880007091A patent/CN101627036A/zh active Pending
- 2008-01-04 HR HR20110964T patent/HRP20110964T1/hr unknown
- 2008-01-04 RS RS20120031A patent/RS52168B/sr unknown
- 2008-01-04 CA CA002674093A patent/CA2674093A1/en not_active Abandoned
- 2008-01-04 US US12/522,018 patent/US20100022591A1/en not_active Abandoned
- 2008-01-04 NZ NZ578144A patent/NZ578144A/en not_active IP Right Cessation
- 2008-01-04 JP JP2009544448A patent/JP2010514829A/ja active Pending
- 2008-01-04 KR KR1020097016214A patent/KR20090104092A/ko not_active Withdrawn
- 2008-01-04 EA EA200900796A patent/EA015805B9/ru not_active IP Right Cessation
- 2008-01-04 SI SI200830517T patent/SI2114931T1/sl unknown
- 2008-01-04 EP EP11172885A patent/EP2383270A1/en not_active Withdrawn
- 2008-01-04 ES ES08700184T patent/ES2376015T3/es active Active
- 2008-01-04 AU AU2008203673A patent/AU2008203673A1/en not_active Abandoned
- 2008-01-04 MX MX2009007180A patent/MX2009007180A/es active IP Right Grant
- 2008-01-04 WO PCT/GB2008/050011 patent/WO2008081205A1/en not_active Ceased
- 2008-01-04 BR BRPI0806468-7A patent/BRPI0806468A2/pt not_active IP Right Cessation
- 2008-01-04 TW TW097100419A patent/TWI380818B/zh not_active IP Right Cessation
- 2008-01-04 DK DK08700184.8T patent/DK2114931T3/da active
- 2008-01-04 EP EP08700184A patent/EP2114931B1/en active Active
- 2008-01-04 PT PT08700184T patent/PT2114931E/pt unknown
- 2008-01-04 PL PL08700184T patent/PL2114931T3/pl unknown
- 2008-01-05 SA SA8280756A patent/SA08280756B1/ar unknown
-
2009
- 2009-07-02 IL IL199680A patent/IL199680A0/en unknown
- 2009-07-03 MA MA32072A patent/MA31084B1/fr unknown
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