JP2012508734A5 - - Google Patents
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- Publication number
- JP2012508734A5 JP2012508734A5 JP2011536289A JP2011536289A JP2012508734A5 JP 2012508734 A5 JP2012508734 A5 JP 2012508734A5 JP 2011536289 A JP2011536289 A JP 2011536289A JP 2011536289 A JP2011536289 A JP 2011536289A JP 2012508734 A5 JP2012508734 A5 JP 2012508734A5
- Authority
- JP
- Japan
- Prior art keywords
- disease
- dementia
- pharmaceutically acceptable
- alzheimer
- acceptable salt
- 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
- 208000024827 Alzheimer disease Diseases 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 9
- 206010012289 Dementia Diseases 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 208000010877 cognitive disease Diseases 0.000 claims 4
- 230000001575 pathological effect Effects 0.000 claims 4
- 230000002792 vascular Effects 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- -1 2- (difluoromethyl) pyridin-4-yl Chemical group 0.000 claims 2
- 208000000044 Amnesia Diseases 0.000 claims 2
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 2
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 2
- 206010059245 Angiopathy Diseases 0.000 claims 2
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 2
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 2
- 208000028698 Cognitive impairment Diseases 0.000 claims 2
- 201000010374 Down Syndrome Diseases 0.000 claims 2
- 208000026139 Memory disease Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 206010036631 Presenile dementia Diseases 0.000 claims 2
- 206010039966 Senile dementia Diseases 0.000 claims 2
- 210000004227 basal ganglia Anatomy 0.000 claims 2
- 230000006735 deficit Effects 0.000 claims 2
- 230000007850 degeneration Effects 0.000 claims 2
- 230000003412 degenerative effect Effects 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000006984 memory degeneration Effects 0.000 claims 2
- 208000023060 memory loss Diseases 0.000 claims 2
- 208000027061 mild cognitive impairment Diseases 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 230000000750 progressive effect Effects 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- MRXBCEQZNKUUIP-UHFFFAOYSA-N 3-[2-(difluoromethyl)pyridin-4-yl]-7-fluoro-3-(3-pyrimidin-5-ylphenyl)isoindol-1-amine Chemical compound C12=CC=CC(F)=C2C(N)=NC1(C=1C=C(N=CC=1)C(F)F)C(C=1)=CC=CC=1C1=CN=CN=C1 MRXBCEQZNKUUIP-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11463408P | 2008-11-14 | 2008-11-14 | |
| US61/114,634 | 2008-11-14 | ||
| US13976708P | 2008-12-22 | 2008-12-22 | |
| US61/139,767 | 2008-12-22 | ||
| US22165309P | 2009-06-30 | 2009-06-30 | |
| US61/221,653 | 2009-06-30 | ||
| PCT/SE2009/051295 WO2010056196A1 (en) | 2008-11-14 | 2009-11-13 | New compounds 578 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012508734A JP2012508734A (ja) | 2012-04-12 |
| JP2012508734A5 true JP2012508734A5 (show.php) | 2012-12-20 |
Family
ID=42170158
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011536289A Pending JP2012508734A (ja) | 2008-11-14 | 2009-11-13 | Ｂａｃｅ阻害剤としての置換イソインドール類及びそれらの使用 |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US8030500B2 (show.php) |
| EP (1) | EP2367814A4 (show.php) |
| JP (1) | JP2012508734A (show.php) |
| KR (1) | KR20110091540A (show.php) |
| CN (1) | CN102282140A (show.php) |
| AR (1) | AR074341A1 (show.php) |
| AU (1) | AU2009314664A1 (show.php) |
| BR (1) | BRPI0921879A2 (show.php) |
| CA (1) | CA2743938A1 (show.php) |
| CL (1) | CL2011001098A1 (show.php) |
| CO (1) | CO6362004A2 (show.php) |
| CR (1) | CR20110255A (show.php) |
| CU (1) | CU20110106A7 (show.php) |
| DO (1) | DOP2011000138A (show.php) |
| EA (1) | EA201190020A1 (show.php) |
| EC (1) | ECSP11011051A (show.php) |
| IL (1) | IL212590A0 (show.php) |
| MX (1) | MX2011004918A (show.php) |
| NI (1) | NI201100099A (show.php) |
| PE (1) | PE20110875A1 (show.php) |
| TW (1) | TW201020244A (show.php) |
| UY (1) | UY32241A (show.php) |
| WO (1) | WO2010056196A1 (show.php) |
| ZA (1) | ZA201104396B (show.php) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007049532A1 (ja) | 2005-10-25 | 2007-05-03 | Shionogi & Co., Ltd. | アミノジヒドロチアジン誘導体 |
| TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| RU2476430C2 (ru) | 2007-04-24 | 2013-02-27 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина, замещенные циклической группой |
| BRPI0915500A2 (pt) | 2008-06-13 | 2019-08-27 | Shionogi & Co | derivado heterocíclico contendo enxofre tendo atividade inibitória de beta secretase |
| EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| EP2485591B1 (en) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| BR112012013854A2 (pt) | 2009-12-11 | 2019-09-24 | Shionogi & Co | derivados de oxazina. |
| UY33376A (es) * | 2010-05-12 | 2011-12-30 | Astrazeneca Ab | Sal de tipo hemifumarato |
| EP2601197B1 (en) | 2010-08-05 | 2014-06-25 | Amgen Inc. | Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use |
| WO2012057247A1 (ja) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
| CA2816285A1 (en) | 2010-10-29 | 2012-05-03 | Shionogi & Co., Ltd. | Naphthyridine derivative |
| US20120165346A1 (en) * | 2010-12-22 | 2012-06-28 | Astrazeneca Ab | Compounds and their use as BACE inhibitors |
| EP2703399A4 (en) | 2011-04-26 | 2014-10-15 | Shionogi & Co | OXAZINE DERIVATIVE AND BACE-1 HEMMER THEREOF |
| US9540359B2 (en) | 2012-10-24 | 2017-01-10 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity |
| EP3353844B1 (en) | 2015-03-27 | 2022-05-11 | Mason K. Harrup | All-inorganic solvents for electrolytes |
| CN105272884B (zh) * | 2015-11-02 | 2017-05-24 | 浙江大学 | 一种邻氰基二苯甲酮衍生物的制备方法 |
| US10707531B1 (en) | 2016-09-27 | 2020-07-07 | New Dominion Enterprises Inc. | All-inorganic solvents for electrolytes |
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| US4605642A (en) * | 1984-02-23 | 1986-08-12 | The Salk Institute For Biological Studies | CRF antagonists |
| US5063245A (en) * | 1990-03-28 | 1991-11-05 | Nova Pharmaceutical Corporation | Corticotropin-releasing factor antagonism compounds |
| ATE198622T1 (de) * | 1993-10-27 | 2001-01-15 | Elan Pharm Inc | Transgene tiere, die app allele mit der schwedischen mutation beherbergen |
| US5877399A (en) * | 1994-01-27 | 1999-03-02 | Johns Hopkins University | Transgenic mice expressing APP-Swedish mutation develop progressive neurologic disease |
| DE4419849A1 (de) * | 1994-06-07 | 1995-12-14 | Hoechst Ag | Isoindolinpigmente |
| DK0765327T3 (da) | 1994-06-16 | 1999-11-29 | Pfizer | Pyrazolo- og pyrrolopyridiner |
| DE19516804A1 (de) | 1995-05-08 | 1996-11-14 | Hoechst Ag | Isoindolinpigmente auf Basis von Aminochinoxalindionen |
| AU6383396A (en) * | 1995-06-07 | 1996-12-30 | Athena Neurosciences, Inc. | Beta-secretase, antibodies to beta-secretase, and assays for detecting beta-secretase inhibition |
| US6211235B1 (en) * | 1996-11-22 | 2001-04-03 | Elan Pharmaceuticals, Inc. | Compounds for inhibiting β-amyloid peptide release and/or its synthesis |
| GB9701684D0 (en) | 1997-01-28 | 1997-03-19 | Smithkline Beecham Plc | Novel compounds |
| CN1278819A (zh) | 1997-09-02 | 2001-01-03 | 杜邦药品公司 | 作为促肾上腺皮质素释放激素拮抗剂、可用于治疗cns障碍和紧张相关性疾病的杂环基取代的环稠合吡啶和嘧啶 |
| US5981168A (en) * | 1998-05-15 | 1999-11-09 | The University Of British Columbia | Method and composition for modulating amyloidosis |
| CN1502696A (zh) | 1998-09-24 | 2004-06-09 | �������Ŷ���Լ��������˾ | 阿尔茨海默氏疾病分泌酶 |
| US6245884B1 (en) * | 1998-10-16 | 2001-06-12 | Vivian Y. H. Hook | Secretases related to alzheimer's dementia |
| HK1044543B (zh) | 1999-02-10 | 2004-12-03 | Elan Pharmaceuticals Inc | 贝他分泌酶组合物及其方法 |
| AU3770800A (en) | 1999-03-26 | 2000-10-16 | Amgen, Inc. | Beta secretase genes and polypeptides |
| CA2376420A1 (en) | 1999-06-15 | 2000-12-21 | Elan Pharmaceuticals, Inc. | Statine-derived tetrapeptide inhibitors of beta-secretase |
| WO2001000665A2 (en) | 1999-06-28 | 2001-01-04 | Oklahoma Medical Research Foundation | Inhibitors of memapsin 2 and use thereof |
| ATE431419T1 (de) | 1999-09-23 | 2009-05-15 | Pharmacia & Upjohn Co Llc | Alzheimer krankheit sekretase, app (amyloid vorlaüfer-protein) substrate dafür und verwendungen |
| GB9924957D0 (en) | 1999-10-21 | 1999-12-22 | Smithkline Beecham Plc | Novel treatment |
| PE20020276A1 (es) | 2000-06-30 | 2002-04-06 | Elan Pharm Inc | COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER |
| US6846813B2 (en) | 2000-06-30 | 2005-01-25 | Pharmacia & Upjohn Company | Compounds to treat alzheimer's disease |
| WO2002002506A2 (en) | 2000-06-30 | 2002-01-10 | Elan Pharmaceuticals, Inc. | Compounds to treat alzheimer's disease |
| AU2001281250A1 (en) | 2000-08-11 | 2002-02-25 | The Brigham And Women's Hospital, Inc. | (hydroxyethyl)ureas as inhibitors of alzheimer's beta-amyloid production |
| US7630838B2 (en) | 2000-09-22 | 2009-12-08 | American Home Products Corporation | Method for identifying agents that interact with beta-site APP cleaving enzyme (BACE) |
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| EP1773807A2 (en) | 2004-06-14 | 2007-04-18 | Takeda San Diego, Inc. | Kinase inhibitors |
| BRPI0512213A (pt) * | 2004-06-16 | 2008-02-19 | Wyeth Corp | método para tratamento, prevenção ou melhora de uma doença ou distúrbio; composição farmacêutica; processo para a preparação de um composto; e uso de um composto |
| EP1758907B1 (en) * | 2004-06-16 | 2009-02-18 | Wyeth | Diphenylimidazopyrimidine and -imidazole amines as inhibitors of b-secretase |
| TW200613272A (en) * | 2004-08-13 | 2006-05-01 | Astrazeneca Ab | Isoindolone compounds and their use as metabotropic glutamate receptor potentiators |
| EA200700712A1 (ru) | 2004-09-21 | 2008-02-28 | Эсерсис, Инк. | Производные индолуксусной кислоты, способ получения таких производных (варианты), фармацевтическая композиция, набор на их основе, способ ингибирования связывания эндогенных лигандов и способ лечения заболеваний и расстройств, восприимчивых к ингибированию связывания эндогенных лигандов с рецептором crth-2 |
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| JP2008523139A (ja) | 2004-12-14 | 2008-07-03 | アストラゼネカ・アクチエボラーグ | 置換アミノピリジン類及びその使用 |
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| US20060223849A1 (en) | 2005-03-14 | 2006-10-05 | Mjalli Adnan M | Benzazole derivatives, compositions, and methods of use as beta-secretase inhibitors |
| MX2007016182A (es) | 2005-06-14 | 2008-03-07 | Schering Corp | Inhibidores de aspartil proteasas. |
| MX2007016186A (es) | 2005-06-14 | 2008-03-07 | Schering Corp | Preparacion y uso de inhibidores de proteasas. |
| EP1902057B1 (en) * | 2005-06-14 | 2013-10-23 | Merck Sharp & Dohme Corp. | Macrocyclic heterocyclic aspartyl protease inhibitors |
| CA2609582A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Aspartyl protease inhibitors |
| KR20080028881A (ko) | 2005-06-14 | 2008-04-02 | 쉐링 코포레이션 | 헤테로사이클릭 아스파르틸 프로테아제 억제제, 이의제조방법 및 용도 |
| DE602006018456D1 (de) | 2005-06-14 | 2011-01-05 | Schering Corp | Herstellung und verwendung von verbindungen als aspartylproteasehemmer |
| EP1896448A1 (en) * | 2005-06-30 | 2008-03-12 | Wyeth | AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION |
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| AU2006270084B2 (en) | 2005-07-18 | 2011-08-25 | Merck Sharp & Dohme Corp. | Spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's disease |
| US7601751B2 (en) * | 2005-09-01 | 2009-10-13 | Bristol-Myers Squibb Company | Indole acetic acid acyl guanidines as β-secretase inhibitors |
| WO2007049532A1 (ja) | 2005-10-25 | 2007-05-03 | Shionogi & Co., Ltd. | アミノジヒドロチアジン誘導体 |
| JP2009513656A (ja) * | 2005-10-27 | 2009-04-02 | シェーリング コーポレイション | 複素環式アスパルチルプロテアーゼインヒビター |
| PE20070798A1 (es) * | 2005-10-31 | 2007-08-24 | Schering Corp | Compuestos heterociclicos como inhibidores de aspartil proteasas |
| EP1951682A4 (en) | 2005-11-15 | 2011-06-15 | Astrazeneca Ab | NEW 2-AMINOPYRIMIDONE OR 2-AMINOPYRIDINONE DERIVATIVES AND THEIR USE |
| JP2009515950A (ja) | 2005-11-15 | 2009-04-16 | アストラゼネカ・アクチエボラーグ | 新規な２−アミノピリミジン誘導体およびその使用 |
| US20090215801A9 (en) | 2005-11-15 | 2009-08-27 | Astrazeneca Ab, Sodertaije, Swedenastex Thereapeutics Ltd | Novel 2-Aminopyrimidinone Derivatives And Their Use |
| TW200804290A (en) | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
| TW200734311A (en) | 2005-11-21 | 2007-09-16 | Astrazeneca Ab | New compounds |
| WO2007058601A1 (en) | 2005-11-21 | 2007-05-24 | Astrazeneca Ab | Novel 2-amino-imidazole-4-one compounds and their use in the manufacture of a medicament to be used in the treatment of cognitive impairment, alzheimer’s disease, neurodegeneration and dementia |
| AR058381A1 (es) | 2005-12-19 | 2008-01-30 | Astrazeneca Ab | Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica |
| CN101460480A (zh) | 2006-04-05 | 2009-06-17 | 阿斯利康(瑞典)有限公司 | 2-氨基嘧啶-4-酮类化合物及其用于治疗或预防Aβ相关病理的用途 |
| TW200808751A (en) | 2006-04-13 | 2008-02-16 | Astrazeneca Ab | New compounds |
| AU2007258435A1 (en) | 2006-06-12 | 2007-12-21 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| TW200815443A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds I |
| TW200815447A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds IV |
| TW200808796A (en) | 2006-06-14 | 2008-02-16 | Astrazeneca Ab | New compounds III |
| TW200815449A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds II |
| TW200815349A (en) * | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
| WO2008063114A1 (en) | 2006-11-20 | 2008-05-29 | Astrazeneca Ab | Amino- imidazolones and their use as medicament for treating cognitive impairment alzheimer disease, neurodegeneration and dementia |
| WO2008076044A1 (en) | 2006-12-20 | 2008-06-26 | Astrazeneca Ab | Novel 2-amino-5, 5-diaryl-imidazol-4-ones |
| TW200831091A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| TW200831484A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| TW200902499A (en) * | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| TW200902503A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| WO2009005470A1 (en) * | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
| WO2009005471A1 (en) | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
| WO2010056194A1 (en) | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | 5h-pyrrolo [ 3, 4-b] pyridin derivatives and their use |
| US20100125087A1 (en) * | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 575 |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| EP2485590B1 (en) | 2009-10-08 | 2015-01-07 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| EP2485591B1 (en) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US8569310B2 (en) | 2009-10-08 | 2013-10-29 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use |
-
2009
- 2009-11-12 TW TW098138485A patent/TW201020244A/zh unknown
- 2009-11-13 US US12/618,212 patent/US8030500B2/en not_active Expired - Fee Related
- 2009-11-13 CN CN2009801545281A patent/CN102282140A/zh active Pending
- 2009-11-13 EA EA201190020A patent/EA201190020A1/ru unknown
- 2009-11-13 AU AU2009314664A patent/AU2009314664A1/en not_active Abandoned
- 2009-11-13 PE PE2011001034A patent/PE20110875A1/es not_active Application Discontinuation
- 2009-11-13 KR KR1020117013516A patent/KR20110091540A/ko not_active Withdrawn
- 2009-11-13 WO PCT/SE2009/051295 patent/WO2010056196A1/en not_active Ceased
- 2009-11-13 BR BRPI0921879A patent/BRPI0921879A2/pt not_active Application Discontinuation
- 2009-11-13 CA CA2743938A patent/CA2743938A1/en not_active Abandoned
- 2009-11-13 AR ARP090104400A patent/AR074341A1/es unknown
- 2009-11-13 MX MX2011004918A patent/MX2011004918A/es not_active Application Discontinuation
- 2009-11-13 EP EP09826375A patent/EP2367814A4/en not_active Withdrawn
- 2009-11-13 JP JP2011536289A patent/JP2012508734A/ja active Pending
- 2009-11-13 UY UY0001032241A patent/UY32241A/es not_active Application Discontinuation
-
2011
- 2011-04-28 CO CO11052264A patent/CO6362004A2/es not_active Application Discontinuation
- 2011-04-28 IL IL212590A patent/IL212590A0/en unknown
- 2011-05-13 EC EC2011011051A patent/ECSP11011051A/es unknown
- 2011-05-13 CL CL2011001098A patent/CL2011001098A1/es unknown
- 2011-05-13 NI NI201100099A patent/NI201100099A/es unknown
- 2011-05-13 CU CU20110106A patent/CU20110106A7/es unknown
- 2011-05-13 DO DO2011000138A patent/DOP2011000138A/es unknown
- 2011-05-13 CR CR20110255A patent/CR20110255A/es unknown
- 2011-06-13 ZA ZA2011/04396A patent/ZA201104396B/en unknown
- 2011-09-06 US US13/225,707 patent/US20110319426A1/en not_active Abandoned
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