NO322022B1 - Trombinreseptorantagonister, farmasoytisk preparat og anvendelse av disse for fremstilling av medisin - Google Patents

Trombinreseptorantagonister, farmasoytisk preparat og anvendelse av disse for fremstilling av medisin Download PDF

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Publication number
NO322022B1
NO322022B1 NO20002659A NO20002659A NO322022B1 NO 322022 B1 NO322022 B1 NO 322022B1 NO 20002659 A NO20002659 A NO 20002659A NO 20002659 A NO20002659 A NO 20002659A NO 322022 B1 NO322022 B1 NO 322022B1
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Norway
Prior art keywords
alkyl
group
mixture
mmol
independently selected
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NO20002659A
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English (en)
Norwegian (no)
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NO20002659L (no
NO20002659D0 (no
Inventor
Michael F Czarniecki
Samuel Chackalamannil
Theodros Asberom
Yan Xia
Dario Doller
Martin C Clasby
Original Assignee
Schering Corp
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Publication of NO20002659D0 publication Critical patent/NO20002659D0/no
Publication of NO20002659L publication Critical patent/NO20002659L/no
Publication of NO322022B1 publication Critical patent/NO322022B1/no

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    • 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
    • C07D401/06Heterocyclic 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 only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • 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
    • 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
    • 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
    • C07D405/12Heterocyclic 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
    • 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • 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
    • C07D409/14Heterocyclic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
NO20002659A 1997-11-25 2000-05-24 Trombinreseptorantagonister, farmasoytisk preparat og anvendelse av disse for fremstilling av medisin NO322022B1 (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US97797997A 1997-11-25 1997-11-25
PCT/US1998/024523 WO1999026943A1 (en) 1997-11-25 1998-11-23 Thrombin receptor antagonists

Publications (3)

Publication Number Publication Date
NO20002659D0 NO20002659D0 (no) 2000-05-24
NO20002659L NO20002659L (no) 2000-07-24
NO322022B1 true NO322022B1 (no) 2006-08-07

Family

ID=25525702

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20002659A NO322022B1 (no) 1997-11-25 2000-05-24 Trombinreseptorantagonister, farmasoytisk preparat og anvendelse av disse for fremstilling av medisin

Country Status (30)

Country Link
EP (1) EP1036072B1 (cs)
JP (2) JP3449620B2 (cs)
KR (1) KR100393492B1 (cs)
CN (2) CN101274929A (cs)
AR (1) AR017189A1 (cs)
AT (1) ATE266025T1 (cs)
AU (1) AU747204B2 (cs)
BR (1) BR9812793A (cs)
CA (1) CA2309352C (cs)
CO (1) CO4990946A1 (cs)
CZ (1) CZ298578B6 (cs)
DE (1) DE69823694T2 (cs)
DK (1) DK1036072T3 (cs)
ES (1) ES2219919T3 (cs)
HU (1) HUP0100607A3 (cs)
ID (1) ID24726A (cs)
IL (1) IL135797A (cs)
MY (1) MY140887A (cs)
NO (1) NO322022B1 (cs)
NZ (1) NZ504218A (cs)
PE (1) PE133799A1 (cs)
PL (1) PL195027B1 (cs)
PT (1) PT1036072E (cs)
RU (1) RU2204557C2 (cs)
SA (1) SA99190972B1 (cs)
SK (1) SK285153B6 (cs)
TR (1) TR200001480T2 (cs)
TW (1) TWI236476B (cs)
WO (1) WO1999026943A1 (cs)
ZA (1) ZA9810685B (cs)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000229961A (ja) 1998-12-11 2000-08-22 Sagami Chem Res Center ヒドロナフト[2,3−c]フラン誘導体およびその製造方法
JP4577751B2 (ja) 1999-09-02 2010-11-10 塩野義製薬株式会社 芳香族ヘテロ環誘導体を含有するインテグラーゼ阻害剤
US7235567B2 (en) 2000-06-15 2007-06-26 Schering Corporation Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist
US7488742B2 (en) * 2000-06-15 2009-02-10 Schering Corporation Thrombin receptor antagonists
SI1294714T1 (sl) * 2000-06-15 2007-12-31 Schering Corp Antagonisti trobinskega receptorja
ES2291323T3 (es) * 2000-06-15 2008-03-01 Schering Corporation Antagonistas de receptores de trombina.
JP4220249B2 (ja) 2001-04-19 2009-02-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 サイクリックアミジン誘導体
AR036832A1 (es) * 2001-10-18 2004-10-06 Schering Corp Compuestos derivados de himbacina, agonistas receptores de trombina, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de medicamentos
DK2065384T3 (da) * 2002-04-16 2011-05-02 Schering Corp Tricyklisk thrombinreceptor-antagonist
ES2211315B1 (es) * 2002-11-12 2005-10-16 Almirall Prodesfarma, S.A. Nuevos compuestos triciclicos.
AU2004218187C1 (en) 2003-02-19 2011-04-07 Eisai R&D Management Co., Ltd. Methods for producing cyclic benzamidine derivatives
JPWO2005108370A1 (ja) 2004-04-16 2008-03-21 味の素株式会社 ベンゼン化合物
CA2567981C (en) * 2004-05-28 2010-08-31 Schering Corporation Constrained himbacine analogs as thrombin receptor antagonists
US7488752B2 (en) * 2004-10-08 2009-02-10 Schering Corporation Thrombin receptor antagonists
RS52117B (en) * 2005-01-14 2012-08-31 Schering Corporation DIASTEREO-SELECTIVATE SYNTHESIS OF EGZO ANALOGUE IN HIMBAC
CN101137636A (zh) * 2005-01-14 2008-03-05 先灵公司 Himbacine类似物的外型选择性合成
EP1853592B1 (en) * 2005-01-14 2011-03-02 Schering Corporation Synthesis of himbacine analogs
TWI367112B (en) * 2006-06-30 2012-07-01 Schering Corp Immediate-release tablet formulations of a thrombin receptor antagonist
US8153664B2 (en) * 2006-10-04 2012-04-10 Schering Corporation Bicyclic and tricyclic derivatives as thrombin receptor antagonists
EP2558462B1 (de) 2010-04-16 2014-10-22 Sanofi Pyridyl-vinyl-pyrazolo-chinoline als par1-inhibitoren
EP2558465B1 (de) 2010-04-16 2014-12-17 Sanofi Trizyklische pyridyl-vinyl-pyrrole als par1-inhibitoren
CN108658910B (zh) * 2017-03-29 2020-11-03 北京新领先医药科技发展有限公司 一种沃拉帕沙中间体1-α的制备方法
CN113387947B (zh) * 2021-07-12 2022-07-01 中国科学院成都生物研究所 调节雌激素受体合成活性的吡唑并吡啶衍生物

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773792A (en) 1968-03-08 1973-11-20 Itt Rayonier Inc Acetates of plicatic acid and processes for the preparation thereof
US4486445A (en) 1983-01-12 1984-12-04 E. I. Du Pont De Nemours And Company Justicidin insecticidal and antiviral compounds
CA2008116C (en) * 1989-02-23 2001-11-20 Thomas Weller Glycine derivatives
IL106197A (en) * 1992-07-30 1999-11-30 Cor Therapeutics Inc Agagonists for the rhombin receptors and pharmaceutical preparations containing them

Also Published As

Publication number Publication date
CO4990946A1 (es) 2000-12-26
TR200001480T2 (tr) 2000-09-21
SA99190972B1 (ar) 2006-07-30
ES2219919T3 (es) 2004-12-01
RU2204557C2 (ru) 2003-05-20
HK1031726A1 (en) 2001-06-22
NZ504218A (en) 2002-04-26
CZ20001856A3 (cs) 2000-10-11
DK1036072T3 (da) 2004-09-06
NO20002659L (no) 2000-07-24
ATE266025T1 (de) 2004-05-15
ID24726A (id) 2000-08-03
KR20010032439A (ko) 2001-04-25
IL135797A (en) 2003-09-17
KR100393492B1 (ko) 2003-08-02
DE69823694D1 (de) 2004-06-09
JP2003128670A (ja) 2003-05-08
HUP0100607A2 (hu) 2002-05-29
PE133799A1 (es) 2000-01-10
AU1415899A (en) 1999-06-15
AR017189A1 (es) 2001-08-22
DE69823694T2 (de) 2005-04-21
ZA9810685B (en) 1999-12-23
CA2309352C (en) 2005-01-25
JP2001524479A (ja) 2001-12-04
AU747204B2 (en) 2002-05-09
JP3449620B2 (ja) 2003-09-22
PL195027B1 (pl) 2007-08-31
EP1036072A1 (en) 2000-09-20
SK7592000A3 (en) 2001-02-12
WO1999026943A1 (en) 1999-06-03
PL341114A1 (en) 2001-03-26
SK285153B6 (sk) 2006-07-07
CA2309352A1 (en) 1999-06-03
PT1036072E (pt) 2004-08-31
EP1036072B1 (en) 2004-05-06
HUP0100607A3 (en) 2002-06-28
TWI236476B (en) 2005-07-21
BR9812793A (pt) 2000-10-17
CN1290265A (zh) 2001-04-04
CZ298578B6 (cs) 2007-11-14
IL135797A0 (en) 2001-05-20
NO20002659D0 (no) 2000-05-24
MY140887A (en) 2010-01-29
CN101274929A (zh) 2008-10-01

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