AR042886A1 - Derivados de diarilmetilen piperidina, su preparacion y uso de los mismos tanto en composiciones farmaceuticas como en la fabricacion de medicamentos. - Google Patents

Derivados de diarilmetilen piperidina, su preparacion y uso de los mismos tanto en composiciones farmaceuticas como en la fabricacion de medicamentos.

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Publication number
AR042886A1
AR042886A1 ARP040100104A ARP040100104A AR042886A1 AR 042886 A1 AR042886 A1 AR 042886A1 AR P040100104 A ARP040100104 A AR P040100104A AR P040100104 A ARP040100104 A AR P040100104A AR 042886 A1 AR042886 A1 AR 042886A1
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AR
Argentina
Prior art keywords
nrc
alkyl
independently
so2r
so3h
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ARP040100104A
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English (en)
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Astrazeneca Ab
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Publication of AR042886A1 publication Critical patent/AR042886A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/70Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • 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
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P25/14Drugs 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
    • A61P25/20Hypnotics; Sedatives
    • 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
    • A61P25/30Drugs 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
    • 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
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/06Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Anesthesiology (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Nutrition Science (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Se preparan compuestos de fórmula general (1) en los cuales R1, R2, R3, R4 y R5 son los definidos en la memoria descriptiva, como así también sales, enantiómeros de los mismos, composiciones farmacéuticas y medicamentos que los incluyen. Los mismos son de utilidad en terapia, en particular en el tratamiento del dolor. Reivindicación 1: Un compuesto de fórmula (1), una sal del mismo aceptable desde el punto de vista farmacéutico, diastereómeros, enantiómeros o mezclas de los mismos, en los cuales R1 se selecciona entre arilo C6-10 y heteroarilo C2-6, en el cual dichos arilo C6-10 y heteroarilo C2-6 están opcionalmente sustituidos con uno o más grupos seleccionados entre -R, -NO2, -OR, -Cl, -Br, -I, -F, -CF3, -C(=O)OH, -NH2, -SH, -NHR, -NR2, -SR, -SO3H, -SO2R, -S(=O)R, -CN, -OH, -C(=O)OR, -C(=O)NR2, -NRC(=O)R y -NRC(=O)-OR, en los cuales R es, independientemente, un H o alquilo C1-6; y R2, R3, R4 y R5 se seleccionan independientemente entre H, alquilo C1-6 y cicloalquilo C3-6, en los cuales dichos alquilo C1-6 y cicloalquilo C3-6 están opcionalmente sustituidos con uno o más grupos seleccionados entre -R, -NO2, -OR, -Cl, -Br, -I, -F, -CF3, -C(=O)R, -C(=O)OH, -NH2, -SH, -NHR, -NR2, -SR, -SO3H, -SO2R, -S(=O)R, -CN, -OH, -C(=O)OR, -C(=O)NR2, -NRC(=O)R y -NRC(=O)-OR, en los cuales R es, independientemente, un H o alquilo C1-6. Reivindicación 11: Un proceso para la preparación de un compuesto de fórmula (1), que comprende hacer reaccionar un compuesto de la fórmula (2) con X-C(=O)-O-R4; en el cual X es Cl, Br, o I; R1 se selecciona entre arilo C6-10 y heteroarilo C2-6, donde dichos arilo C6-10 y heteroarilo C2-6 están opcionalmente sustituidos con uno o más grupos seleccionados entre: -R, -NO2, -OR, -Cl, -Br, -I, -F, -CF3, -C(=O)R, -C(=O)OH, -NH2, -SH, -NHR, -NR2, -SR, -SO3H, -SO2R, -S(=O)R, -CN, -OH, -C(=O)OR, -C(=O)NR2, -NRC(=O)R y -NRC(=O)-OR, en los cuales R es, independientemente, un H o alquilo C1-6; y R2, R3, R4 y R5 se seleccionan independientemente entre H, alquilo C1-6 y cicloalquilo C3-6, en los cuales dichos alquilo C1-6 y cicloalquilo C3-6 están opcionalmente sustituidos con uno o más grupos seleccionados entre: -R, -NO2, -OR, -Cl, -Br, -I, -F, -CF3, -C(=O)R, -C(=O)OH, -NH2, -SH, -NHR, -NR2, -SR, -SO3H, -SO2R, -S(=O)R, -CN, -OH, -C(=O)OR, -C(=O)NR2, -NRC(=O)R y -NRC(=O)-OR, en los cuales R es, independientemente, un H o alquilo C1-6. Reivindicación 13: Un proceso para preparar un compuesto de fórmula (1), que comprende hacer reaccionar un compuesto de fórmula (4) con R1-CHO o R1CH2-X en la cual X es Cl, Br, o I; R1 se selecciona entre arilo C6-10 y heteroarilo C2-6, donde dichos arilo C6-10 y heteroarilo C2-6 están opcionalmente sustituidos con uno o más grupos seleccionados entre-R, -NO2, -OR, -Cl, -Br, -I, -F, -CF3, -C(=O)R, -C(=O)OH, -NH2, -SH, -NHR, -NR2, -SR, -SO3H, -SO2R, -S(=O)R, -CN, -OH, -C(=O)OR, -C(=O)NR2, -NRC(=O)R y -NRC(=O)-OR, en los cuales R es, independientemente, un H o alquilo C1-6; y R2, R3, R4 y R5 se seleccionan independientemente entre H, alquilo C1-6 y cicloalquilo C3-6, en los cuales dichos alquilo C1-6 y cicloalquilo C3-6 están opcionalmente sustituidos con uno o más grupos seleccionados entre: -R, -NO2, -OR, -Cl, -Br, -I, -F, -CF3, -C(=O)R, -C(=O)OH, -NH2, -SH, -NHR, -NR2, -SR, -SO3H, -SO2R, -S(=O)R, -CN, -OH, -C(=O)OR, -C(=O)NR2, -NRC(=O)R y -NRC(=O)-OR, en los cuales R es, independientemente, un H o alquilo C1-6.
ARP040100104A 2003-01-16 2004-01-15 Derivados de diarilmetilen piperidina, su preparacion y uso de los mismos tanto en composiciones farmaceuticas como en la fabricacion de medicamentos. AR042886A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
SE0300103A SE0300103D0 (sv) 2003-01-16 2003-01-16 Diarylmethylidene piperidine derivatives, preparations thereof and uses thereof

Publications (1)

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AR042886A1 true AR042886A1 (es) 2005-07-06

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ARP040100104A AR042886A1 (es) 2003-01-16 2004-01-15 Derivados de diarilmetilen piperidina, su preparacion y uso de los mismos tanto en composiciones farmaceuticas como en la fabricacion de medicamentos.

Country Status (21)

Country Link
US (1) US20060116399A1 (es)
EP (1) EP1587791A1 (es)
JP (1) JP2006515356A (es)
KR (1) KR20050096138A (es)
CN (1) CN100430379C (es)
AR (1) AR042886A1 (es)
AU (1) AU2004203969B2 (es)
BR (1) BRPI0406594A (es)
CA (1) CA2510400A1 (es)
IL (1) IL169360A0 (es)
IS (1) IS7961A (es)
MX (1) MXPA05007483A (es)
NO (1) NO20053805L (es)
NZ (1) NZ540759A (es)
PL (1) PL378335A1 (es)
RU (1) RU2326865C2 (es)
SE (1) SE0300103D0 (es)
TW (1) TW200427449A (es)
UA (1) UA80310C2 (es)
WO (1) WO2004063157A1 (es)
ZA (1) ZA200505189B (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE0203301D0 (sv) * 2002-11-07 2002-11-07 Astrazeneca Ab Novel Compounds
US20070099957A1 (en) * 2003-05-16 2007-05-03 Astra Zeneca Ab Diarylmethylidene piperidine derivatives, preparations thereof and uses thereof
NZ546834A (en) 2003-10-01 2010-03-26 Adolor Corp Spirocyclic heterocyclic derivatives and methods of their use
US7598261B2 (en) 2005-03-31 2009-10-06 Adolor Corporation Spirocyclic heterocyclic derivatives and methods of their use
US7576207B2 (en) 2006-04-06 2009-08-18 Adolor Corporation Spirocyclic heterocyclic derivatives and methods of their use

Family Cites Families (14)

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Publication number Priority date Publication date Assignee Title
US2898339A (en) * 1957-07-29 1959-08-04 Wm S Merrell Co N-substituted benzhydrol, benzhydryl, and benzhydrylidene piperidine
US4581171A (en) * 1983-07-27 1986-04-08 Janssen Pharmaceutica, N.V. [[Bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones useful for treating psychotropic disorders
US4816586A (en) * 1987-07-29 1989-03-28 Regents Of The University Of Minnesota Delta opioid receptor antagonists
US5140029A (en) * 1989-01-09 1992-08-18 Janssen Pharmaceutica N.V. 2-aminopyrimidinone derivatives
US4939137A (en) * 1989-06-28 1990-07-03 Ortho Pharmaceutical Corporation Ring-fused thienopyrimidinedione derivatives
US5683998A (en) * 1991-04-23 1997-11-04 Toray Industries, Inc. Tricyclic triazolo derivatives, processes for producing the same and the uses of the same
US5574159A (en) * 1992-02-03 1996-11-12 Delta Pharmaceuticals, Inc. Opioid compounds and methods for making therefor
TW548271B (en) * 1996-12-20 2003-08-21 Astra Pharma Inc Novel piperidine derivatives having an exocyclic double bond with analgesic effects
KR20030009376A (ko) * 2000-03-03 2003-01-29 오르토-맥네일 파마슈티칼, 인코퍼레이티드 3-(디아릴메틸렌)-8-아자비사이클로[3.2.1]옥탄 유도체
US6556387B1 (en) * 2000-03-31 2003-04-29 Seagate Technology Llc Controlling mechanical response characteristics of a disc drive actuator by adjusting a fastener engaging the actuator shaft to vary axial force on the bearing assembly
SE0001207D0 (sv) * 2000-04-04 2000-04-04 Astrazeneca Canada Inc Novel compounds
SE0101765D0 (sv) * 2001-05-18 2001-05-18 Astrazeneca Ab Novel compounds
SE0101766D0 (sv) * 2001-05-18 2001-05-18 Astrazeneca Ab Novel compounds
EA015491B1 (ru) * 2003-06-27 2011-08-30 Янссен Фармацевтика Н.В. ТРИЦИКЛИЧЕСКИЕ δ-ОПИОИДНЫЕ МОДУЛЯТОРЫ

Also Published As

Publication number Publication date
NO20053805D0 (no) 2005-08-12
MXPA05007483A (es) 2005-12-05
IS7961A (is) 2005-07-27
AU2004203969A1 (en) 2004-07-29
WO2004063157A1 (en) 2004-07-29
IL169360A0 (en) 2007-07-04
SE0300103D0 (sv) 2003-01-16
EP1587791A1 (en) 2005-10-26
NZ540759A (en) 2008-03-28
CN100430379C (zh) 2008-11-05
JP2006515356A (ja) 2006-05-25
TW200427449A (en) 2004-12-16
PL378335A1 (pl) 2006-03-20
RU2326865C2 (ru) 2008-06-20
UA80310C2 (en) 2007-09-10
KR20050096138A (ko) 2005-10-05
CA2510400A1 (en) 2004-07-29
RU2005121490A (ru) 2006-02-10
ZA200505189B (en) 2006-04-26
US20060116399A1 (en) 2006-06-01
CN1735596A (zh) 2006-02-15
NO20053805L (no) 2005-10-17
BRPI0406594A (pt) 2005-12-20
AU2004203969B2 (en) 2007-09-06

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