CN100537546C - 作为内皮素拮抗剂的新型烷基磺酰胺 - Google Patents

作为内皮素拮抗剂的新型烷基磺酰胺 Download PDF

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Publication number
CN100537546C
CN100537546C CNB028266447A CN02826644A CN100537546C CN 100537546 C CN100537546 C CN 100537546C CN B028266447 A CNB028266447 A CN B028266447A CN 02826644 A CN02826644 A CN 02826644A CN 100537546 C CN100537546 C CN 100537546C
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Prior art keywords
pyrimidin
bromo
ethoxy
amide
yloxy
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Expired - Fee Related
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CNB028266447A
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Chinese (zh)
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CN1612864A (zh
Inventor
马丁·博利
克里斯托夫·博斯
马丁内·克洛泽尔
瓦尔特·菲施利
托马斯·韦勒
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Actelion Pharmaceuticals Ltd
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Actelion Pharmaceuticals Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
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    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A—HUMAN NECESSITIES
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/56—One oxygen atom and one sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CNB028266447A 2002-01-02 2002-12-10 作为内皮素拮抗剂的新型烷基磺酰胺 Expired - Fee Related CN100537546C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP0200002 2002-01-02
EPPCT/EP02/00002 2002-01-02

Publications (2)

Publication Number Publication Date
CN1612864A CN1612864A (zh) 2005-05-04
CN100537546C true CN100537546C (zh) 2009-09-09

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CNB028266447A Expired - Fee Related CN100537546C (zh) 2002-01-02 2002-12-10 作为内皮素拮抗剂的新型烷基磺酰胺

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US (1) US7323465B2 (enExample)
JP (1) JP4769418B2 (enExample)
KR (1) KR100940432B1 (enExample)
CN (1) CN100537546C (enExample)
AR (1) AR037943A1 (enExample)
AT (1) ATE381545T1 (enExample)
AU (1) AU2002361033B8 (enExample)
BR (1) BR0215424A (enExample)
CA (1) CA2471220C (enExample)
DE (1) DE60224223T2 (enExample)
ES (1) ES2297040T3 (enExample)
HU (1) HUP0500082A2 (enExample)
IL (2) IL162534A0 (enExample)
MX (1) MXPA04006457A (enExample)
MY (1) MY138502A (enExample)
NO (1) NO327220B1 (enExample)
NZ (1) NZ533693A (enExample)
TW (1) TWI248436B (enExample)
WO (1) WO2003055863A1 (enExample)
ZA (1) ZA200404927B (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010523540A (ja) * 2007-04-03 2010-07-15 ファイザー・インク スルホンアミドおよびその医薬組成物
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
AR077999A1 (es) * 2009-09-02 2011-10-05 Vifor Int Ag Antagonistas de pirimidin y triazin-hepcidina
EP2907811A1 (en) * 2014-02-14 2015-08-19 Actelion Pharmaceuticals Ltd. Process for manufacturing pyrimidine sulfamide derivatives

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5739333A (en) 1995-05-16 1998-04-14 Tanabe Seiyaku Co., Ltd. Sulfonamide derivative and process for preparing the same
JP3013752B2 (ja) * 1995-05-16 2000-02-28 田辺製薬株式会社 スルホンアミド誘導体
AU703386B2 (en) * 1995-12-20 1999-03-25 Astellas Pharma Inc. Arylethenesulfonamide derivatives and drug composition containing the same
WO1998003488A1 (en) * 1996-07-23 1998-01-29 Shionogi & Co., Ltd. Novel pyrimidine compounds and drug compositions
JP3116347B2 (ja) * 1996-11-13 2000-12-11 田辺製薬株式会社 医薬組成物
WO1998057938A1 (en) * 1997-06-19 1998-12-23 Yamanouchi Pharmaceutical Co., Ltd. Substituted lower alkanesulfonamide derivatives and pharmaceutical composition containing the same
AU775194B2 (en) * 1999-09-03 2004-07-22 Actelion Pharmaceuticals Ltd Bis-sulfonamides
GB0023074D0 (en) * 2000-09-20 2000-11-01 Pfizer Ltd Pyridazines

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Ethenesulfonamide and ethanesulfonamide derivatives,anovel class of orally active endothelin-A receptorantagonists. HARADA, HIRONORI ET AL.BIOORGANIC & MEDICINAL CHEMISTRY,Vol.9 No.11. 2001 *

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Publication number Publication date
HUP0500082A2 (hu) 2005-04-28
WO2003055863A1 (en) 2003-07-10
KR20040073525A (ko) 2004-08-19
DE60224223D1 (de) 2008-01-31
CA2471220A1 (en) 2003-07-10
ATE381545T1 (de) 2008-01-15
JP2005513155A (ja) 2005-05-12
AU2002361033B8 (en) 2009-01-29
NO20043215L (no) 2004-07-29
CA2471220C (en) 2010-11-16
US7323465B2 (en) 2008-01-29
BR0215424A (pt) 2004-12-14
DE60224223T2 (de) 2008-12-04
ZA200404927B (en) 2005-11-30
ES2297040T3 (es) 2008-05-01
CN1612864A (zh) 2005-05-04
KR100940432B1 (ko) 2010-02-10
AU2002361033A1 (en) 2003-07-15
IL162534A0 (en) 2005-11-20
TW200404063A (en) 2004-03-16
JP4769418B2 (ja) 2011-09-07
AR037943A1 (es) 2004-12-22
TWI248436B (en) 2006-02-01
MY138502A (en) 2009-06-30
US20050085639A1 (en) 2005-04-21
NO327220B1 (no) 2009-05-18
MXPA04006457A (es) 2004-10-04
AU2002361033B2 (en) 2008-11-20
IL162534A (en) 2011-07-31
NZ533693A (en) 2007-02-23

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