AR070534A1 - Agonistas de receptores muscarinicos - Google Patents

Agonistas de receptores muscarinicos

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Publication number
AR070534A1
AR070534A1 ARP090100687A ARP090100687A AR070534A1 AR 070534 A1 AR070534 A1 AR 070534A1 AR P090100687 A ARP090100687 A AR P090100687A AR P090100687 A ARP090100687 A AR P090100687A AR 070534 A1 AR070534 A1 AR 070534A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocycloalkyl
heteroaryl
cycloalkyl
independently
Prior art date
Application number
ARP090100687A
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English (en)
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Astrazeneca Ab
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Publication of AR070534A1 publication Critical patent/AR070534A1/es

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    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • 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
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory 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
    • A61P23/00Anaesthetics
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • 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
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • A61P9/10Drugs 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Pulmonology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Composiciones farmacéuticas que incluyen los compuestos proceso e intermediario. Son utiles en terapia, en particular en el tratamiento del dolor, alzheimer y esquizofrenia. Reivindicacion 1: Un compuesto de Formula 1: o una sal farmacéuticamente aceptable del mismo; en la que: Y es -CR3R4-, -NR5-, -O-, o -S-; X es -CR6R7-, -NR8-, -O-, o -S-; con la condicion de que Y sea -CR3R4- o X sea -CR6R7-; cada A es, independientemente, alquilo de C1-3, o dos A están enlazados juntos para formar un puente de alquileno de C1-3; R1 es hidrogeno, alquilo de C1-6, o haloalquilo de C1-6; R2 es -C(O)ORa, -C(O)Rb, -C(O)NRcRd, alquilo de C1-6, haloalquilo de C1-6, cicloalquilo de C3-7, cicloalquil C3-7-alquilo de C1-3, heterocicloalquilo de C3-7, heterocicloalquil C3-7-alquilo de C1-3, aril C6-10-alquilo de C1-3, heteroarilo de C3-9, o heteroaril C3-9alquilo de C1-3 en el que los anillos de dichos arilo C6-10 aril de C6-10-alquilo de C1-3, heteroarilo de C3-9, y heteroaril C3-9-alquilo de C1-3 están cada uno opcionalmente sustituidos con 1, 2, 3 o 4 grupos seleccionados independientemente; en el que los anillos de dichos cicloalquilo de C3-7, cicloalquil C3-7-alquilo de C1-3, heterocicloalquilo de C3-7, y heterocicloalquil C3-7-alquilo de C1-3 están cada uno opcionalmente sustituidos con 1, 2, 3 o 4 grupos R10 seleccionados independientemente; y en el que dichos alquilo de C1-6, alquenilo de C2-6, alquinilo de C2-6, haloalquilo de C1-6, alcoxi de C1-6, y haloalcoxi de C1-6 están cada uno opcionalmente sustituidos con 1, 2 o 3 grupos R11 seleccionados independientemente: R3, R4, R6, y R7 son cada uno, independientemente, hidrogeno, fluoro, alquilo de C1-4, alcoxi de C1-4-metilo, ciano-alquilo de C1-4 o haloalquilo de C1-4; R5 y R8 son cada uno, independientemente, hidrogeno, alquilo de C1-4, o haloalquilo de C1-4: cada R9 y R10 es, independientemente, fenilo, cicloalquilo de C3-6, heterocicloalquilo de C2-5 , heteroarilo de C3-5, -CN, -SRe, -ORe, O(CH2)r-ORe, Re, -C(O)-Re, -CO2Re, -SO2Re, -SO2NReRf, halogeno, -NO2, NReRf, -(CH2)rNReRf, o -C(O)NReRf: cada R11 es, independientemente, -CN, -NO2, ORe, o NReRf; Ra, Rb, Rc, y Rd son cada uno, independientemente, hidrogeno, alquilo de C1-7, alquenilo de C2-6, alquinilo de C2-6, haloalquilo de C1-6, cicloalquilo de C3-7, cicloalquil C3-7 alquilo de C1-3, heterocicloalquilo de C3-7, heterocicloalquil C3-7-alquilo de C1-3, arilo de C6-10, aril C6-10-alquilo de C1-3, heteroarilo de C3-9, o heteroaril C3-9-alquilo de C1-3: en los que los anillos de dichos arilo de C6-10, aril C6-10-alquilo de C1-3, heteroarilo de C3-9, y heteroaril C3-9-alquilo de C1-3 están cada uno opcionalmente sustituidos con 1, 2, 3 o 4 grupos R12 seleccionados independientemente; en los que los anillos de dichos cicloalquilo de C3-7, cicloalquil C3-7-alquilo de C1-3, heterocicloalquilo de C3-7, y heterocicloalquil C3-7-alquilo de C1-3, están cada uno opcionalmente sustituidos con 1, 2, 3 o 4 grupos R13 seleccionados independientemente: y en los que dicho alquilo de C1-7, alquenilo de C2-6, alquinilo de C2-6, haloalquilo de C1-6, alcoxi de C1-7, y haloalcoxi de C1-6 están cada uno opcionalmente sustituidos con 1, 2 o 3 grupos R14 seleccionados independientemente: cada R12, R13, y R14 es, independientemente, fenilo, cicloalquilo de C3-6, heterocicloalquilo de C2-5, heteroarilo de C3-5, -CN, -SRg, -ORg, -O(CH2)r-ORg, Rg, -C(O)-Rg, -CO2Rg, -SO2Rg, -SO2NRgRh, halogeno, -NO2, -NRgRh, -(CH2)NRgRh, o -C(O)-NRgRh: cada Re, Rf, Rg y Rh es, independientemente, hidrogeno, alquilo de C1-6, alquenilo de C2-6 o haloalquilo de C1-6, m es 1, 2 o 3: p es 0, 1 o 2: q es un numero entero de 0 a [6+(px2)]; y r es 1, 2, 3 o 4; con la condicion de que el compuesto no sea 4'-metil-4-((4aS,8aS)-2-oxooctahidroquinoxalin-1(2H)-il)-1,4'-bipiperidin-1'-carboxilato de isopropilo, 4-[4-[(4aS,8aS)2-oxo-3,4,4a,5,6,7,8,8a-octahidroquinoxalin-1-il]-1-piperidil]-4-metil-piperidin-1-carboxilato de isopropilo, (3S)-3-[4-[(4aS,8aS)-3-oxo-4a,5,6,7,8,8a-hexahidrobenzo[b][1,4]oxazin-4-iI]-1-piperidil]pirrolidin-1-carboxilato de isopropilo, 4-[4-[(4aR,8aR)-2-oxo-4a,5,6,7,8,8a-hexahidro-4H-benzo[d][1,3]oxazin-1-il]-1-piperidil]piperidin-1-carboxilato de terc-butilo, 4-[4-[(4aS,8aS)-3-oxo-4a,5,6,7,8,8a-hexahidrobenzo[b][1,4]oxazin-4-il]-1-piperidil]-4-metil-piperidin-1-carboxilato de isopropilo, (4aS,8aS)-1-[1-[1-(2-metilbenzoil)-4-piperidil]-4-piperidil]-4a,5,6,7,8,8a-hexahidro-4H-benzo[d][1,3]oxazin-2-ona, 4-[4-[(4aS,8aS)-3-oxo-4a,5,6,7,8,8a-hexahidrobenzo[b][1,4]oxazin-4-il]-1-piperidil]piperidin-1-carboxilato de terc-butilo, 4-[4-[(4aS,8aS)-2-oxo-4a,5,6,7,8,8a-hexahidro-4H-benzo[d][1,3]oxazin-1-il]-1-piperidil]piperidin-1-carboxilato de metilo, o una sal farmacéuticamente aceptable de los mismos.
ARP090100687A 2008-02-28 2009-02-27 Agonistas de receptores muscarinicos AR070534A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US3213808P 2008-02-28 2008-02-28

Publications (1)

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AR070534A1 true AR070534A1 (es) 2010-04-14

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ARP090100687A AR070534A1 (es) 2008-02-28 2009-02-27 Agonistas de receptores muscarinicos

Country Status (16)

Country Link
US (1) US20090221567A1 (es)
EP (1) EP2257543A4 (es)
JP (1) JP2011513302A (es)
KR (1) KR20100131463A (es)
CN (1) CN102015687A (es)
AR (1) AR070534A1 (es)
AU (1) AU2009217823A1 (es)
BR (1) BRPI0907992A2 (es)
CA (1) CA2716855A1 (es)
CL (1) CL2009000445A1 (es)
MX (1) MX2010009395A (es)
PE (1) PE20091433A1 (es)
RU (1) RU2010135253A (es)
TW (1) TW200940522A (es)
UY (1) UY31672A1 (es)
WO (1) WO2009108117A1 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200815405A (en) * 2006-06-09 2008-04-01 Astrazeneca Ab Novel compounds
TW200813018A (en) * 2006-06-09 2008-03-16 Astrazeneca Ab Novel compounds
US9187451B2 (en) 2011-11-18 2015-11-17 Heptares Therapeutics Limited Muscarinic M1 receptor agonists
WO2014045031A1 (en) * 2012-09-18 2014-03-27 Heptares Therapeutics Limited Bicyclic aza compounds as muscarinic m1 receptor agonists
US9593106B2 (en) 2013-02-07 2017-03-14 Heptares Therapeutics Limited Piperidin-1-yl and azepin-1-yl carboxylates as muscarinic M4 receptor agonists
GB201513743D0 (en) 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonists
GB201513742D0 (en) 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonists
GB201617454D0 (en) 2016-10-14 2016-11-30 Heptares Therapeutics Limited Pharmaceutical compounds
GB201819960D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
WO2024088408A1 (zh) * 2022-10-28 2024-05-02 纽欧申医药(上海)有限公司 一种含氮杂环化合物、其药学上可接受的盐及其制备方法与应用

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2307999A (en) * 1997-12-23 1999-07-12 Alcon Laboratories, Inc. Muscarinic agents and use thereof to treat glaucoma, myopia and various other conditions
WO2003105781A2 (en) * 2002-06-17 2003-12-24 Merck & Co., Inc. Ophthalmic compositions for treating ocular hypertension
US8288412B2 (en) * 2005-09-30 2012-10-16 Glaxo Group Limited Compounds which have activity at M1 receptor and their uses in medicine
TW200815405A (en) * 2006-06-09 2008-04-01 Astrazeneca Ab Novel compounds
TW200813018A (en) * 2006-06-09 2008-03-16 Astrazeneca Ab Novel compounds

Also Published As

Publication number Publication date
TW200940522A (en) 2009-10-01
JP2011513302A (ja) 2011-04-28
BRPI0907992A2 (pt) 2017-06-13
US20090221567A1 (en) 2009-09-03
KR20100131463A (ko) 2010-12-15
RU2010135253A (ru) 2012-04-10
PE20091433A1 (es) 2009-10-24
EP2257543A4 (en) 2012-03-21
CA2716855A1 (en) 2009-09-03
EP2257543A1 (en) 2010-12-08
CL2009000445A1 (es) 2011-05-06
CN102015687A (zh) 2011-04-13
AU2009217823A1 (en) 2009-09-03
WO2009108117A1 (en) 2009-09-03
MX2010009395A (es) 2010-09-24
UY31672A1 (es) 2009-09-30

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