HUP0300965A2 - Új aril-etén-szulfonamidok pirimidinszármazékai, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

Új aril-etén-szulfonamidok pirimidinszármazékai, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk

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Publication number
HUP0300965A2
HUP0300965A2 HU0300965A HUP0300965A HUP0300965A2 HU P0300965 A2 HUP0300965 A2 HU P0300965A2 HU 0300965 A HU0300965 A HU 0300965A HU P0300965 A HUP0300965 A HU P0300965A HU P0300965 A2 HUP0300965 A2 HU P0300965A2
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HU
Hungary
Prior art keywords
alkyl
heterocyclyl
amino
group
aryl
Prior art date
Application number
HU0300965A
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English (en)
Inventor
Martin Bolli
Christoph Boss
Martine Clozel
Walter Fischli
Thomas Weller
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Actelion Pharmaceuticals Ltd.
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Publication date
Application filed by Actelion Pharmaceuticals Ltd. filed Critical Actelion Pharmaceuticals Ltd.
Publication of HUP0300965A2 publication Critical patent/HUP0300965A2/hu
Publication of HUP0300965A3 publication Critical patent/HUP0300965A3/hu

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    • 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
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    • C07ORGANIC CHEMISTRY
    • 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • 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
    • 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
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • 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
    • A61P35/00Antineoplastic agents
    • 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
    • A61P9/10Drugs 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
    • 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
    • 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
    • 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
    • C07D239/52Two oxygen atoms
    • 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
    • C07D239/56One oxygen atom and one sulfur atom
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
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    • 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
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    • C07ORGANIC CHEMISTRY
    • 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
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    • C07ORGANIC CHEMISTRY
    • 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
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    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
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    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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    • 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
    • C07D413/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

A találmány (I) általános képletű aril-etén-szulfonamidokra és azokgyógyászatilag alkalmazható sóira vonatkozik - a képletben R1 és R2egymástól függetlenül aril- vagy heteroaril-csoportot jelent; R3jelentése fenilcsoport, mono-, di- vagy triszubsztituált fenilcsoport,arilcsoport vagy heteroaril-csoport; R4 jelentése hidrogénatom,halogénatom vagy trifluor-metil-alkil-, alkil-amino-, alkoxi-, alkil-szulfono-, alkil-szulfinil-, alkil-tio-, alkil-tio-alkil-, hidroxi-alkil-, alkoxi-alkil-, hidroxi-alkoxi-alkil-, hidroxi-alkil-amino-,alkil-amino-alkil-, amino-, di-alkil-amino-,[N-(hidroxi-alkil)-N-alkil]-amino-, aril-, aril-amino-, aril-alkil-amino-, aril-tio-, aril-alkil-tio-, aril-oxi-, aril-alkil-oxi-, aril-alkil-, aril-szulfinil-,heteroaril-, heteroaril-oxi-, heteroaril-alkil-oxi-, heteroaril-amino-, heteroaril-alkil-amino-, heteroaril-tio-, heteroaril-alkil-tio-, heteroaril-alkil-, heteroaril-szulfinil-, heterociklil-,heterociklil-alkil-oxi-, heterociklil-oxi-, heterociklil-amino-,heterociklil-alkil-amino-, heterociklil-tio-, heterociklil-alkil-tio-,heterociklil-alkil-, heterociklil-szulfinil-, cikloalkil-, cikloalkil-oxi-, cikloalkil-alkil-oxi-, cikloalkil-amino-, cikloalkil-alkil-amino-, cikloalkil-tio-, cikloalkil-alkil-tio-, cikloalkil-alkil- vagycikloalkil-szulfinil-csoport; R5 és R6 egymástól függetlenülhidrogénatomot vagy alkilcsoportot jelent; X vegyértékkötést vagy -O-,-S-, -NH- vagy -CH2- csoportot jelent; Y -O-, -S- vagy -NH- csoportotjelent; Z vegyértékkötést vagy -O-, -S- vagy -NH- csoportot jelent; ésQ jelentése -(CH2)n-, -CH2-ciklopropilén-CH2- vagy -(CH2)m-C<C-(CH2)p- csoport. A találmány kiterjed a vegyületeket tartalmazógyógyszerkészítményekre és a vegyületek alkalmazásáragyógyszerkészítmények előállítására. Ó
HU0300965A 2000-07-21 2001-07-10 Novel pyrimidin derivatives of arylethene sulfonamides, pharmaceutical compositions containing them and their use HUP0300965A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP0007006 2000-07-21
PCT/EP2001/007922 WO2002008200A2 (en) 2000-07-21 2001-07-10 Arylethene-sulfonamides, their preparation and their use as endothelin antagonists

Publications (2)

Publication Number Publication Date
HUP0300965A2 true HUP0300965A2 (hu) 2003-10-28
HUP0300965A3 HUP0300965A3 (en) 2004-01-28

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ID=8164031

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HU0300965A HUP0300965A3 (en) 2000-07-21 2001-07-10 Novel pyrimidin derivatives of arylethene sulfonamides, pharmaceutical compositions containing them and their use

Country Status (21)

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US (1) US6951856B2 (hu)
EP (1) EP1309564B1 (hu)
JP (1) JP4832706B2 (hu)
KR (1) KR100826332B1 (hu)
CN (1) CN100562518C (hu)
AR (1) AR030247A1 (hu)
AT (1) ATE329908T1 (hu)
AU (2) AU2001281970B2 (hu)
BR (1) BR0112614A (hu)
CA (1) CA2416785C (hu)
DE (1) DE60120711T2 (hu)
ES (1) ES2266233T3 (hu)
HU (1) HUP0300965A3 (hu)
IL (2) IL153471A0 (hu)
MX (1) MXPA03000430A (hu)
MY (1) MY140724A (hu)
NO (1) NO324771B1 (hu)
NZ (1) NZ523304A (hu)
TW (1) TWI289553B (hu)
WO (1) WO2002008200A2 (hu)
ZA (1) ZA200300137B (hu)

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BRPI0508461B8 (pt) 2004-03-05 2021-05-25 Hoffmann La Roche diaminopirimidinas, seus usos, e composição farmacêutica
EP1924564B1 (en) 2005-09-01 2016-11-09 F.Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
EP1924566B1 (en) 2005-09-01 2016-01-13 F.Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
KR101025381B1 (ko) 2005-09-01 2011-03-28 에프. 호프만-라 로슈 아게 P2x3 및 p2x2/3 조정자로서의 다이아미노피리미딘
TWI331523B (en) * 2005-12-08 2010-10-11 Nat Health Research Institutes Vinylsulfonate compounds
WO2009020579A1 (en) * 2007-08-07 2009-02-12 Schering Corporation Gamma secretase modulators
WO2009104152A1 (en) * 2008-02-20 2009-08-27 Actelion Pharmaceuticals Ltd Combination treatment for ovarian cancer
IT1393136B1 (it) * 2009-03-11 2012-04-11 Sifa Vitor S R L Procedimento per la preparazione del bosentan
US20100256371A1 (en) * 2009-04-02 2010-10-07 Glenmark Processes for the preparation of bosentan and its intermediates thereof
AU2018332634A1 (en) * 2017-09-12 2020-04-30 Agency For Science, Technology And Research Compounds useful as inhibitors of isoprenylcysteine carboxyl methyltransferase
CN110885328B (zh) * 2018-09-10 2022-08-12 成都康弘药业集团股份有限公司 作为钠通道阻滞剂的磺酰胺类化合物及其用途
TWI833430B (zh) 2021-11-08 2024-02-21 大陸商正大天晴藥業集團股份有限公司 氮雜聯苯類化合物及其應用

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RU2086544C1 (ru) * 1991-06-13 1997-08-10 Хоффманн-Ля Рош АГ Бензолсульфонамидные производные пиримидина или их соли, фармацевтическая композиция для лечения заболеваний, связанных с активностью эндотелина
TW287160B (hu) * 1992-12-10 1996-10-01 Hoffmann La Roche
TW394761B (en) 1993-06-28 2000-06-21 Hoffmann La Roche Novel Sulfonylamino Pyrimidines
JP2790065B2 (ja) * 1993-12-17 1998-08-27 田辺製薬株式会社 ベンゼンスルホンアミド誘導体及びその製法
IL111959A (en) * 1993-12-17 2000-07-16 Tanabe Seiyaku Co N-(polysubstituted pyrimidin-4-yl) benzenesulfonamide derivatives their preparation and pharmaceutical compositions containing them
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Publication number Publication date
US20030220359A1 (en) 2003-11-27
US6951856B2 (en) 2005-10-04
KR100826332B1 (ko) 2008-05-02
DE60120711T2 (de) 2007-06-06
IL153471A0 (en) 2003-07-06
NO20030274D0 (no) 2003-01-20
HUP0300965A3 (en) 2004-01-28
AU2001281970B2 (en) 2006-03-16
CA2416785A1 (en) 2002-01-31
CN1441788A (zh) 2003-09-10
TWI289553B (en) 2007-11-11
CA2416785C (en) 2009-11-10
IL153471A (en) 2007-09-20
ZA200300137B (en) 2004-04-06
ES2266233T3 (es) 2007-03-01
KR20030016382A (ko) 2003-02-26
BR0112614A (pt) 2003-06-10
WO2002008200A3 (en) 2002-05-10
ATE329908T1 (de) 2006-07-15
EP1309564B1 (en) 2006-06-14
EP1309564A2 (en) 2003-05-14
AU8197001A (en) 2002-02-05
AR030247A1 (es) 2003-08-13
JP4832706B2 (ja) 2011-12-07
JP2004504385A (ja) 2004-02-12
MY140724A (en) 2010-01-15
WO2002008200A2 (en) 2002-01-31
MXPA03000430A (es) 2003-06-24
NO20030274L (no) 2003-01-20
DE60120711D1 (de) 2006-07-27
NZ523304A (en) 2005-02-25
CN100562518C (zh) 2009-11-25
NO324771B1 (no) 2007-12-10

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