PE20010989A1 - 8-arilquinolinas sustituidas inhibidoras de 4-fosfodiesterasa - Google Patents

8-arilquinolinas sustituidas inhibidoras de 4-fosfodiesterasa

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Publication number
PE20010989A1
PE20010989A1 PE2000001396A PE0013962000A PE20010989A1 PE 20010989 A1 PE20010989 A1 PE 20010989A1 PE 2000001396 A PE2000001396 A PE 2000001396A PE 0013962000 A PE0013962000 A PE 0013962000A PE 20010989 A1 PE20010989 A1 PE 20010989A1
Authority
PE
Peru
Prior art keywords
inhibitor
halogen
alkyl
arylquinolines
heteroaryl
Prior art date
Application number
PE2000001396A
Other languages
English (en)
Inventor
Denis Deschenes
Daniel Dube
Michel Gallant
Helene Perrier
Patrick Lacombe
Dwight Macdonald
Anthony Mastracchio
Yves Girard
Original Assignee
Merck Frosst Canada Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Merck Frosst Canada Inc filed Critical Merck Frosst Canada Inc
Publication of PE20010989A1 publication Critical patent/PE20010989A1/es

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    • 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
    • C07D401/10Heterocyclic 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 aromatic 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
    • A61P11/00Drugs for disorders of the respiratory system
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P11/16Central respiratory analeptics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00Drugs for dermatological disorders
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D215/14Radicals substituted by oxygen atoms
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    • 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
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    • C07ORGANIC CHEMISTRY
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    • 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
    • C07D405/12Heterocyclic 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 chain containing hetero atoms as chain links
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    • 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
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    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
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    • 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
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    • 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
    • C07D417/10Heterocyclic 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 aromatic rings
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    • 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
    • C07D417/12Heterocyclic 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 chain containing hetero atoms as chain links
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Quinoline Compounds (AREA)

Abstract

SE REFIERE A 8-ARILQUINOLINAS SUSTITUIDAS DE FORMULA I DONDE S1, S2, S3 SON H, CN, ALCOXI C1-C6, OH, HALOGENO, ENTRE OTROS; R1 ES H, OH, HALOGENO, CARBONILO, ALQUILO C1-C6, CICLOALQUILO C3-C6, ENTRE OTROS; A ES CH, C-ESTER, CR4; R2 Y R3 SON ARILO, HETEROARILO, H, HALOGENO, CN, ALQUILO C1-C6, ENTRE OTROS; R4 ES ARILO, ALQUILO C1-C6, HETEROARILO, CN, CARBONILO, ENTRE OTROS; R2 O R3 OPCIONALMENTE UNIDO A R4 POR UN ENLACE FORMAN UN ANILLO. SON COMPUESTOS PREFERIDOS 6-ISOPROPIL-8-(3-{(Z/E)-2-[4-(METILSULFONIL)FENIL]-2-FENILETENIL}FENILQUINOLINA, ENTRE OTROS; TAMBIEN SE REFIERE A UNA COMPOSICION QUE COMPRENDE ADEMAS ANTAGONISTA DE RECEPTORES DE LEUCOTRIENO, INHIBIDOR DE LA BIOSINTESIS DE LEUCOTRIENO, ANTAGONISTA M2/M3, CORTICOSTEROIDE, UN ANTAGONISTA DE RECEPTORES H1, AGONISTA DE ADRENORECEPTORES ß2. EL COMPUESTO I ES UN INHIBIDOR DE FOSFODIESTERASA 4 PDE4 Y PUEDE SER UTIL PARA EL TRATAMIENTO DEL ASMA, BRONQUITIS CRONICA, ENFERMEDAD PULMONAR OBSTRUCTIVA CRONICA, PSORIASIS
PE2000001396A 1999-12-22 2000-12-22 8-arilquinolinas sustituidas inhibidoras de 4-fosfodiesterasa PE20010989A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US17152299P 1999-12-22 1999-12-22

Publications (1)

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PE20010989A1 true PE20010989A1 (es) 2001-10-01

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ID=22624050

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000001396A PE20010989A1 (es) 1999-12-22 2000-12-22 8-arilquinolinas sustituidas inhibidoras de 4-fosfodiesterasa

Country Status (32)

Country Link
EP (1) EP1244628A1 (es)
JP (1) JP3782011B2 (es)
KR (1) KR20020082839A (es)
CN (1) CN1221534C (es)
AR (1) AR029214A1 (es)
AU (1) AU778531B2 (es)
BG (1) BG65403B1 (es)
BR (1) BR0016651A (es)
CA (1) CA2393749C (es)
CO (1) CO5261613A1 (es)
CZ (1) CZ20022171A3 (es)
DZ (1) DZ3244A1 (es)
EA (1) EA004747B1 (es)
EE (1) EE200200342A (es)
GE (1) GEP20053626B (es)
HK (1) HK1057560A1 (es)
HR (1) HRP20020545A2 (es)
HU (1) HUP0203896A3 (es)
IL (1) IL150114A0 (es)
IS (1) IS6413A (es)
MX (1) MXPA02006329A (es)
MY (1) MY134008A (es)
NO (1) NO20023013L (es)
NZ (1) NZ520258A (es)
PE (1) PE20010989A1 (es)
PL (1) PL355752A1 (es)
SK (1) SK8972002A3 (es)
TW (1) TWI280240B (es)
UA (1) UA74815C2 (es)
WO (1) WO2001046151A1 (es)
YU (1) YU47102A (es)
ZA (1) ZA200204862B (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10110772A1 (de) * 2001-03-07 2002-09-12 Boehringer Ingelheim Pharma Neue Arzneimittelkompositionen auf der Basis von Anticholinergika und PDE-IV-Inhibitoren
US7776315B2 (en) 2000-10-31 2010-08-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions based on anticholinergics and additional active ingredients
US6740666B2 (en) * 2000-12-20 2004-05-25 Merck & Co., Inc. Substituted 8-arylquinoline phosphodiesterase-4 inhibitors
CA2431559A1 (en) * 2000-12-20 2002-08-08 Merck & Co., Inc. Process for making substituted 8-arylquinolinium benzenesulfonate
JP2005501822A (ja) * 2001-06-27 2005-01-20 メルク フロスト カナダ アンド カンパニー 置換8−アリールキノリン系pde4阻害薬
WO2003010137A1 (en) * 2001-07-24 2003-02-06 Merck & Co., Inc. Preparation of sulfonyl quinoline
WO2003024488A2 (en) * 2001-09-19 2003-03-27 Altana Pharma Ag Combination of a pde inhibitor and a leukotriene receptor antagonist
EP1487797B1 (en) 2002-03-18 2009-05-27 Merck Frosst Canada Ltd. Hetero-bridge substituted 8-arylquinoline pde4 inhibitors
CN1780811A (zh) * 2003-03-05 2006-05-31 细胞基因公司 二苯基乙烯化合物及其用途
CA2560895A1 (en) * 2004-03-25 2005-10-06 Synta Pharmaceuticals Corp. Acrylonitrile derivatives for inflammation and immune-related uses
EP1888776A4 (en) * 2005-05-19 2009-07-29 Synergenz Bioscience Ltd METHODS AND COMPOSITIONS FOR ASSESSING FUNCTION AND PULMONARY DISORDERS
ME01648B (me) 2006-07-05 2014-09-20 Nycomed Gmbh Kombinacija inhibitora hmg-coa reduktaze rosuvastatina sa inhibitorom fosfodiesteraze 4,kao što je roflumilast, roflumilast-n-oksid za liječenje inflamatornih plućnih oboljenja
KR20150004441A (ko) * 2006-07-07 2015-01-12 칼립시스, 인코포레이티드 Pde4의 바이사이클릭 헤테로아릴 억제제
AU2007299726A1 (en) * 2006-09-22 2008-03-27 Braincells, Inc. Combination comprising an HMG-COA reductase inhibitor and a second neurogenic agent for treating a nervous system disorder and increasing neurogenesis
JP2010518064A (ja) 2007-02-12 2010-05-27 メルク・シャープ・エンド・ドーム・コーポレイション Adおよび関連状態の治療のためのピペラジン誘導体
US8461389B2 (en) 2008-04-18 2013-06-11 University College Dublin, National University Of Ireland, Dublin Psycho-pharmaceuticals
BR112012020060B8 (pt) 2010-02-12 2021-05-25 Askat Inc uso de n-((1-((4-hidroxitetrahidro-2h-piran-4-il)metil)piperidin-4-il)metil)-3-isopropil-2-oxo-2,3-dihidro-1h-benzo[d]imidazol-1-carboxamida para tratar doença de alzheimer e demência
US20140271680A1 (en) 2011-08-12 2014-09-18 Universite Paris-Est Creteil Val De Marne Methods and pharmaceutical compositions for treatment of pulmonary hypertension
WO2013054153A1 (en) 2011-10-11 2013-04-18 INSERM (Institut National de la Santé et de la Recherche Médicale) Nutlin compounds for use in he treatment of pulmonary hypertension
CA3073956A1 (en) 2017-09-03 2019-03-07 Angion Biomedica Corp. Vinylheterocycles as rho-associated coiled-coil kinase (rock) inhibitors

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GB9226830D0 (en) * 1992-12-23 1993-02-17 Celltech Ltd Chemical compounds
US5455252A (en) * 1993-03-31 1995-10-03 Syntex (U.S.A.) Inc. Optionally substituted 6,8-quinolines
US6245774B1 (en) * 1994-06-21 2001-06-12 Celltech Therapeutics Limited Tri-substituted phenyl or pyridine derivatives
JPH11209350A (ja) * 1998-01-26 1999-08-03 Eisai Co Ltd 含窒素複素環誘導体およびその医薬

Also Published As

Publication number Publication date
NO20023013D0 (no) 2002-06-21
JP3782011B2 (ja) 2006-06-07
HRP20020545A2 (en) 2005-10-31
JP2003531112A (ja) 2003-10-21
HK1057560A1 (en) 2004-04-08
WO2001046151A1 (en) 2001-06-28
CO5261613A1 (es) 2003-03-31
HUP0203896A3 (en) 2003-05-28
GEP20053626B (en) 2005-10-10
KR20020082839A (ko) 2002-10-31
EP1244628A1 (en) 2002-10-02
MXPA02006329A (es) 2004-05-14
CN1221534C (zh) 2005-10-05
CN1434801A (zh) 2003-08-06
AR029214A1 (es) 2003-06-18
BG106840A (en) 2003-01-31
BG65403B1 (bg) 2008-06-30
NZ520258A (en) 2004-05-28
EE200200342A (et) 2003-06-16
CA2393749C (en) 2008-06-17
CA2393749A1 (en) 2001-06-28
YU47102A (sh) 2005-06-10
HUP0203896A2 (hu) 2003-04-28
BR0016651A (pt) 2002-09-10
MY134008A (en) 2007-11-30
AU2336201A (en) 2001-07-03
CZ20022171A3 (cs) 2002-11-13
IS6413A (is) 2002-06-11
DZ3244A1 (fr) 2001-06-28
PL355752A1 (en) 2004-05-17
TWI280240B (en) 2007-05-01
NO20023013L (no) 2002-08-22
EA200200702A1 (ru) 2003-02-27
UA74815C2 (en) 2006-02-15
ZA200204862B (en) 2003-03-17
AU778531B2 (en) 2004-12-09
IL150114A0 (en) 2002-12-01
SK8972002A3 (en) 2002-11-06
EA004747B1 (ru) 2004-08-26

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