AR060403A1 - Compuestos de amino- pirimidina 2,6- sustituidos -4- monosustituidos como antagonistas del receptor de prostaglandina d2 - Google Patents

Compuestos de amino- pirimidina 2,6- sustituidos -4- monosustituidos como antagonistas del receptor de prostaglandina d2

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Publication number
AR060403A1
AR060403A1 ARP070101501A ARP070101501A AR060403A1 AR 060403 A1 AR060403 A1 AR 060403A1 AR P070101501 A ARP070101501 A AR P070101501A AR P070101501 A ARP070101501 A AR P070101501A AR 060403 A1 AR060403 A1 AR 060403A1
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AR
Argentina
Prior art keywords
piperidin
phenyl
methyl
ethyl
carboxy
Prior art date
Application number
ARP070101501A
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English (en)
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Sanofi Aventis
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Publication date
Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR060403A1 publication Critical patent/AR060403A1/es

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    • CCHEMISTRY; METALLURGY
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/12Ophthalmic agents for cataracts
    • 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
    • A61P27/14Decongestants or antiallergics
    • 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
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    • A61P3/04Anorexiants; Antiobesity agents
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P37/00Drugs for immunological or allergic disorders
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    • 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
    • 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
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Vascular Medicine (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)

Abstract

Estos compuestos son utiles para tratar enfermedades alérgicas tales como rinitis alérgica, conjuntivitis alérgica, dermatitis atopica, asma bronquial y alergia alimentaria), mastocitosis sistémica, trastornos acompanados por la activacion sistémica de mastocitos, choque anafiláctico, broncoconstriccion, bronquitis, urticaria, eccema, enfermedades acompanadas por picor (tales como dermatitis atopica y urticaria), enfermedades (tales como cataratas, desprendimiento de retina, inflamacion, infeccion y trastornos del sueno) que se generan secundariamente como resultado del comportamiento que acompana al picor (tal como rascarse y golpearse), inflamacion, enfermedad pulmonar obstructiva cronica, lesion por isquemia-reperfusion, accidente cerebrovascular, artritis reumatoide cronica, pleuritis, colitis ulcerosa y similares, por medio de la administracion a dicho paciente de una cantidad farmacéuticamente eficaz de un compuesto de la presente. Reivindicacion 1: Un compuesto de formula (1):en la que: R1 es 2,4-dicloro-fenilo o 4-trifluorometoxi-fenilo, y cuando R1 es 2,4-dicloro-fenilo, entonces R2 es 3-carboxi-pirrolidinilo, 3,5-di-(1-hidroxi-1-metil-etil)-fenilo, 3-amino-piperidin-1-ilo, 4-amino-piperidin-1- ilo, 4-acetamida-piperidin-1-ilo, 1-metil-2-carboxi-2,3-dihidro-1 H-indol-5-ilo, 3-(1-terc-butilsulfonilaminocarbonil-1-metil-etil)-fenilo, 3-(1-dimetilaminosulfonilaminocarbonil-1 -metil-etil)-fenilo, 3-(1-tiomorfolin-4- ilcarbonil-1-metil-etil)- fenilo, 3-(1-aminocarbonil-1-metil-etil)-fenilo, 3-(1- dimetilaminocarbonil-1-metil-etil)-enilo, 3-carboximetil-piperidin-1-ilo, 3-metilsulfonilaminocarbonil-piperidin-1-ilo, 3-etilsulfonilaminocarbonil-piperidin-1-ilo, 3-terc- butilsulfonilaminocarbonil-piperidin-1-ilo, 3- trifluorometilsulfonilaminocarbonil-piperidin-1-ilo, 3[(1H-tetrazol-5-il)-aminocarbonil]-piperidin-1-ilo, 3-aminocarbonil-piperidin-1-ilo, 3-dimetilaminocarbonil-piperidin-1-ilo, 3- dimetilaminosulfonilaminocarbonil- piperidin-1-ilo o 2-carboxi-2,3-dihidro-benzofuran-5-ilo, y cuando R1 es 4-trifluorometoxi-fenilo, entonces R2 es 3-(1-metil-1-carboxi-etil)-piperidinilo, 3-carboxi-piperidinilo, 3-metilsulfonilaminocarbonil- piperidin-1-ilo, 5-carboxi-tiofen-2-ilo, o una sal farmacéuticamente aceptable, hidrato o solvato del mismo, un profármaco farmacéuticamente aceptable del mismo, o una sal farmacéuticamente aceptable, hidrato o solvato del profármaco.
ARP070101501A 2006-04-12 2007-04-10 Compuestos de amino- pirimidina 2,6- sustituidos -4- monosustituidos como antagonistas del receptor de prostaglandina d2 AR060403A1 (es)

Applications Claiming Priority (1)

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US74467606P 2006-04-12 2006-04-12

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AR060403A1 true AR060403A1 (es) 2008-06-11

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ARP070101501A AR060403A1 (es) 2006-04-12 2007-04-10 Compuestos de amino- pirimidina 2,6- sustituidos -4- monosustituidos como antagonistas del receptor de prostaglandina d2

Country Status (25)

Country Link
US (1) US20090036469A1 (es)
EP (1) EP2010503A1 (es)
JP (1) JP2009533473A (es)
KR (1) KR20080108287A (es)
CN (1) CN101421252B (es)
AR (1) AR060403A1 (es)
AU (1) AU2007238052B2 (es)
BR (1) BRPI0710710A2 (es)
CA (1) CA2649083C (es)
CR (1) CR10249A (es)
DO (1) DOP2007000068A (es)
EC (1) ECSP088813A (es)
HN (1) HN2008001530A (es)
MA (1) MA30409B1 (es)
MX (1) MX2008011369A (es)
NO (1) NO20084291L (es)
NZ (1) NZ571793A (es)
PE (1) PE20080186A1 (es)
RU (1) RU2431631C2 (es)
TN (1) TNSN08339A1 (es)
TW (1) TW200815395A (es)
UA (1) UA95950C2 (es)
UY (1) UY30283A1 (es)
WO (1) WO2007121280A1 (es)
ZA (1) ZA200807380B (es)

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JP5039594B2 (ja) * 2008-02-08 2012-10-03 株式会社日立ハイテクノロジーズ レビュー装置,検査領域設定支援システム、および、欠陥の画像得方法
TW201034675A (en) * 2008-12-18 2010-10-01 Sanofi Aventis Method for treating macular degeneration
RU2012143978A (ru) * 2010-03-16 2014-04-27 Авентис Фармасьютикалз Инк. Замещенный пиримидин в качестве антагониста рецептора простагландина d2
MX2012010035A (es) * 2010-03-16 2012-10-01 Aventis Pharma Inc Pirimidinas sustituidas como antagonistas del receptor de la prostaglandina d2.
EP2590944B1 (en) 2010-07-05 2015-09-30 Actelion Pharmaceuticals Ltd. 1-phenyl-substituted heterocyclyl derivatives and their use as prostaglandin d2 receptor modulators
WO2012044561A2 (en) * 2010-09-30 2012-04-05 Merck Sharp & Dohme Corp. 2-alkoxy pyrimidine pde10 inhibitors
JP6097765B2 (ja) 2011-12-21 2017-03-15 アクテリオン ファーマシューティカルズ リミテッドActelion Pharmaceuticals Ltd ヘテロシクリル誘導体及びプロスタグランジンd2受容体調節剤としてのそれらの使用
WO2014006585A1 (en) 2012-07-05 2014-01-09 Actelion Pharmaceuticals Ltd 1-phenyl-substituted heterocyclyl derivatives and their use as prostaglandin d2 receptor modulators
ES2690782T3 (es) 2012-10-24 2018-11-22 Nyu Winthrop Hospital Biomarcador no invasivo para identificar sujetos en riesgo de parto prematuro
RU2673084C2 (ru) * 2013-11-08 2018-11-22 Киссеи Фармасьютикал Ко., Лтд. Производное карбоксиметилпиперидина
HRP20220522T1 (hr) 2014-08-04 2022-06-10 Nuevolution A/S Proizvoljno kondenzirani heterociklil-supstituirani derivati pirimidina koji su korisni za liječenje upalnih, metaboličkih, onkoloških i autoimunih bolesti
CR20180323A (es) 2015-11-20 2018-08-06 Idorsia Pharmaceuticals Ltd Derivados de indol n-sustituídos como moduladores de los receptores de pge2
EA201992676A1 (ru) 2017-05-18 2020-05-06 Идорсия Фармасьютиклз Лтд Фенильные производные в качестве модуляторов pge2 рецепторов
CN110621667A (zh) 2017-05-18 2019-12-27 爱杜西亚药品有限公司 嘧啶衍生物
PL3625228T3 (pl) 2017-05-18 2021-12-20 Idorsia Pharmaceuticals Ltd Pochodne pirymidyny jako modulatory receptora pge2
CN110621671A (zh) 2017-05-18 2019-12-27 爱杜西亚药品有限公司 作为pge2受体调节剂的苯并呋喃及苯并噻吩衍生物
US20200264188A1 (en) 2017-09-13 2020-08-20 Progenity, Inc. Preeclampsia biomarkers and related systems and methods
EP4029380B1 (en) * 2019-09-13 2026-01-28 Meiji Co., Ltd Solid milk
EP4070113A4 (en) 2019-12-04 2023-12-20 Biora Therapeutics, Inc. ASSESSMENT OF PREECLAMPSIA USING FREE AND DISSOCIATE PLACENTAL GROWTH FACTOR TESTS
US11685727B2 (en) 2019-12-20 2023-06-27 Nuevolution A/S Compounds active towards nuclear receptors
MX2022007265A (es) 2019-12-20 2022-09-09 Nuevolution As Compuestos activos frente a receptores nucleares.
CA3174176A1 (en) 2020-03-31 2021-10-07 Sanne Schroder Glad Compounds active towards nuclear receptors
EP4126874A1 (en) 2020-03-31 2023-02-08 Nuevolution A/S Compounds active towards nuclear receptors

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DE3644799A1 (de) * 1986-06-04 1987-12-10 Hoechst Ag Neue pyrimidin-derivate, deren herstellung und verwendung
US5047554A (en) * 1989-04-18 1991-09-10 Pfizer Inc. 3-substituted-2-oxindole derivatives
SE0200411D0 (sv) * 2002-02-05 2002-02-05 Astrazeneca Ab Novel use
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BRPI0710710A2 (pt) 2011-08-16
MX2008011369A (es) 2008-09-18
ECSP088813A (es) 2008-11-27
CN101421252A (zh) 2009-04-29
MA30409B1 (fr) 2009-05-04
AU2007238052A1 (en) 2007-10-25
US20090036469A1 (en) 2009-02-05
NZ571793A (en) 2011-08-26
NO20084291L (no) 2008-11-11
UY30283A1 (es) 2007-11-30
DOP2007000068A (es) 2007-10-31
UA95950C2 (en) 2011-09-26
ZA200807380B (en) 2009-05-27
PE20080186A1 (es) 2008-04-15
EP2010503A1 (en) 2009-01-07
RU2008144578A (ru) 2010-05-20
HN2008001530A (es) 2012-01-17
TNSN08339A1 (en) 2009-12-29
RU2431631C2 (ru) 2011-10-20
CA2649083C (en) 2011-06-28
HK1131975A1 (en) 2010-02-12
CN101421252B (zh) 2011-10-12
TW200815395A (en) 2008-04-01
CA2649083A1 (en) 2007-10-25
JP2009533473A (ja) 2009-09-17
KR20080108287A (ko) 2008-12-12
WO2007121280A1 (en) 2007-10-25
CR10249A (es) 2008-11-26
AU2007238052B2 (en) 2011-12-22

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