AR072470A1 - Moduladores de los canales de iones de calcio y sus usos - Google Patents

Moduladores de los canales de iones de calcio y sus usos

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Publication number
AR072470A1
AR072470A1 ARP090102503A ARP090102503A AR072470A1 AR 072470 A1 AR072470 A1 AR 072470A1 AR P090102503 A ARP090102503 A AR P090102503A AR P090102503 A ARP090102503 A AR P090102503A AR 072470 A1 AR072470 A1 AR 072470A1
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AR
Argentina
Prior art keywords
group
groups
hydrogen atom
unsubstituted
alkyl
Prior art date
Application number
ARP090102503A
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English (en)
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Lectus Therapeutics Ltd
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Application filed by Lectus Therapeutics Ltd filed Critical Lectus Therapeutics Ltd
Publication of AR072470A1 publication Critical patent/AR072470A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/056Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12Radicals substituted by oxygen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/24Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Electrotherapy Devices (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)

Abstract

Son bloqueadores de los canales Cavx y son utiles en el tratamiento de diversas afecciones incluyendo el dolor. Composiciones farmacéuticas. Reivindicacion 1: Un compuesto representado mediante la formula general (1) o su sal o profármaco aceptable para uso farmacologico, donde R1, R2, R3 y R4 se seleccionan independientemente entre átomos de hidrogeno, grupos alquilo, hidroxialquilo, átomos de halogeno, grupos haloalquilo, alcoxi, haloalcoxi, alcoxicarbonilo, carboxilo, hidroxilo, nitro, amino, monoalquilamino, dialquilamino, acilamino, alcoxicarbonilamino, alquilsulfonilo, arilsulfonilo, alquilsulfonilamino, arilsulfonilamino, aminosulfonilo y grupos ciano, o cualesquiera dos de R1 a R4 que están adyacentes en el anillo pueden en forma conjunta representar la porcion -O-(CH2)n-O- donde n es un numero entero entre 1 y 3; R5 es un átomo de hidrogeno o un grupo alquilo; R6 es un átomo de hidrogeno o un grupo alquilo; y X se selecciona del grupo formado por: (a) grupos de formula OR7 donde R7 es un átomo de hidrogeno o un grupo alquilo el cual está opcionalmente sustituido con un sustituyente seleccionado del grupo formado por grupos alquilsulfonilalquilo, grupos heterocíclicos saturados o parcialmente insaturados, grupos alcoxi, grupos carboxilo, nitro, amino, monoalquilamino, dialquilamino, átomos de halogeno, y grupos alcoxicarbonilo, siempre y cuando R7 es H o etilo, entonces R1, R2, R3 y R4 no pueden seleccionarse entra átomos de hidrogeno, átomos de halogeno y grupos alquilo; y (b) grupos de formula NR8R9 donde R8 y R9 junto con el átomo de nitrogeno al cual están unidos forman un grupo heterocíclico saturado o parcialmente insaturado el cual opcionalmente contiene por lo menos un heteroátomo más seleccionado entre átomos de nitrogeno, oxigeno y azufre, dicho grupo heterocíclico saturado o parcialmente insaturado es además opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo formado por grupos alquilo, átomos de halogeno, grupos haloalquilo, alcoxi, alcoxicarbonilo, carboxilo, nitro, amino, monoalquilamino, dialquilamino y grupo hidroxilo, siempre que: (i) cuando R8 y R9 junto con el átomo de nitrogeno al cual están unidos forman un grupo piperazina, y uno o más de R1 a R4 se seleccionan entre átomos de hidrogeno, grupos hidroxilo, nitro, amino, alquilamino, dialquilamino, alcoxicarbonilamino, átomos de halogeno, grupos alcoxi y grupos alquilo, el átomo de nitrogeno del grupo piperazina en la posicion 4 del anillo no puede ser sustituido con un grupo alquilo, (ii) cuando cada uno de R1, R2, R3, R4, R5 y R6 es un átomo de hidrogeno, entonces X no puede ser un grupo piperazinilo no sustituido o un grupo morfolino no sustituido, (iii) cuando cada uno de R1, R2, R4, R5 y R6 es un átomo de hidrogeno y R3 se selecciona del grupo formado por un átomo de hidrogeno, un átomo de bromo y un grupo hidroxilo, entonces X no puede ser un grupo metoxi, (iv) cuando cada uno de R2 y R3 es un grupo metoxi o representan en forma conjunta la porcion -O-CH2-O- y cada uno de R1, R4, R5 y R6 es un átomo de hidrogeno, entonces X no puede ser un grupo piperidina no sustituido, un grupo morfolino no sustituido, un grupo pirrolidina no sustituido, un grupo azepano no sustituido, un grupo azocano no sustituido, o cuando R2 y R3 en forma conjunta representan la porcion -O-CH2-O- y cada uno de R1, R4, R5 y R6 es un átomo de hidrogeno X no puede representar un grupo 4-metilpiperazina.
ARP090102503A 2008-07-03 2009-07-03 Moduladores de los canales de iones de calcio y sus usos AR072470A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0812192.3A GB0812192D0 (en) 2008-07-03 2008-07-03 Calcium ion channel modulators & uses thereof

Publications (1)

Publication Number Publication Date
AR072470A1 true AR072470A1 (es) 2010-09-01

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ID=39717915

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090102503A AR072470A1 (es) 2008-07-03 2009-07-03 Moduladores de los canales de iones de calcio y sus usos

Country Status (20)

Country Link
US (1) US20110166136A1 (es)
EP (1) EP2303840A2 (es)
JP (1) JP2011526618A (es)
KR (1) KR20110046460A (es)
CN (1) CN102143946A (es)
AR (1) AR072470A1 (es)
AU (1) AU2009265292A1 (es)
BR (1) BRPI0913970A2 (es)
CA (1) CA2729688A1 (es)
CO (1) CO6341611A2 (es)
EA (1) EA201170135A1 (es)
GB (1) GB0812192D0 (es)
IL (1) IL210224A0 (es)
MA (1) MA32429B1 (es)
MX (1) MX2010014455A (es)
PE (1) PE20110406A1 (es)
TW (1) TW201004942A (es)
UY (1) UY31959A (es)
WO (1) WO2010001179A2 (es)
ZA (1) ZA201100068B (es)

Families Citing this family (4)

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Publication number Priority date Publication date Assignee Title
CN105481851A (zh) * 2014-09-19 2016-04-13 龚兆龙 六氢苯并萘啶类光学活性化合物及其药物用途
WO2018100206A1 (en) * 2016-12-02 2018-06-07 Sophion Bioscience A/S Seal enhancer
US11215606B2 (en) 2016-12-02 2022-01-04 Sophion Bioscience A/S Seal enhancer
CN115894330A (zh) * 2022-09-06 2023-04-04 吉林医药学院 一种1-乙酰基-1h-吲哚-3-基乙酸酯衍生物的合成方法和应用

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US2825734A (en) * 1955-04-11 1958-03-04 Upjohn Co Reduction of carbonylic radicals in indolyl-3 compounds
GB944443A (es) * 1959-09-25 1900-01-01
US3217011A (en) * 1965-05-07 1965-11-09 Sterling Drug Inc 1-(indolyglyoxalyl)-piperidines
GB9523999D0 (en) * 1995-11-23 1996-01-24 Lilly Co Eli Indolyl neuropeptide y receptor antagonists
US5756507A (en) * 1995-12-14 1998-05-26 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
DE19946301A1 (de) * 1998-04-02 2001-04-19 Asta Medica Ag Indolyl-3-glyoxylsäure-Derivate mit therapeutisch wertvollen Eigenschaften
JP2006510673A (ja) * 2002-12-10 2006-03-30 ワイス プラスミノゲンアクティベータインヒビター1(pai−1)のインヒビターとしての、アリール、アリールオキシ、および、アルキルオキシ置換1h−インドール−3−イルグリオキシル酸誘導体
UA80453C2 (en) * 2002-12-10 2007-09-25 Derivatives of substituted dyhydropyranoindol-3,4-dion as inhibitors of plasminogen activator inhibitor-1 (pai-1)
ES2325071T3 (es) * 2002-12-10 2009-08-25 Wyeth Derivados del acido indol-oxo-acetilaminoacetico sustituido como inhibidores del inhibidor del activador del plasminogeno-1 (pai-1).
WO2007040166A1 (ja) * 2005-09-30 2007-04-12 Dainippon Sumitomo Pharma Co., Ltd. 新規な縮合ピロール誘導体
RU2008118001A (ru) * 2005-10-06 2009-11-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Модуляторы атф-зависимых транспортеров
AU2007217363A1 (en) * 2006-02-27 2007-08-30 Wyeth Inhibitors of PAI-1 for treatment of muscular conditions
US7504399B2 (en) * 2006-06-08 2009-03-17 Bristol-Meyers Squibb Company Piperazine enamines as antiviral agents

Also Published As

Publication number Publication date
EP2303840A2 (en) 2011-04-06
EA201170135A1 (ru) 2011-10-31
JP2011526618A (ja) 2011-10-13
IL210224A0 (en) 2011-03-31
CO6341611A2 (es) 2011-11-21
AU2009265292A1 (en) 2010-01-07
GB0812192D0 (en) 2008-08-13
CA2729688A1 (en) 2010-01-07
MX2010014455A (es) 2011-04-11
KR20110046460A (ko) 2011-05-04
BRPI0913970A2 (pt) 2018-05-29
CN102143946A (zh) 2011-08-03
US20110166136A1 (en) 2011-07-07
PE20110406A1 (es) 2011-06-19
WO2010001179A2 (en) 2010-01-07
WO2010001179A3 (en) 2010-11-11
MA32429B1 (fr) 2011-06-01
TW201004942A (en) 2010-02-01
UY31959A (es) 2010-01-05
ZA201100068B (en) 2012-06-27

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