HUP0100607A2 - Trombin receptor antagonisták és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Trombin receptor antagonisták és ezeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP0100607A2
HUP0100607A2 HU0100607A HUP0100607A HUP0100607A2 HU P0100607 A2 HUP0100607 A2 HU P0100607A2 HU 0100607 A HU0100607 A HU 0100607A HU P0100607 A HUP0100607 A HU P0100607A HU P0100607 A2 HUP0100607 A2 HU P0100607A2
Authority
HU
Hungary
Prior art keywords
group
hydrogen atom
bond
optionally substituted
present
Prior art date
Application number
HU0100607A
Other languages
English (en)
Inventor
Theodros Asberom
Samuel Chackalamannil
Martin C. Clasby
Michael F. Czarnieczki
Dario Doller
Yan Xia
Original Assignee
Schering Corp.
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 Schering Corp. filed Critical Schering Corp.
Publication of HUP0100607A2 publication Critical patent/HUP0100607A2/hu
Publication of HUP0100607A3 publication Critical patent/HUP0100607A3/hu

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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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pyridine Compounds (AREA)

Abstract

A találmány tárgyát általános képletű vegyületek - ahol <-adottesetben kettős kötés; == adott esetben egyes kötés; n = 0, 1 vagy 2; Qadott esetben szubsztituált cikloalkán, heterocikloalkán, aromás vagyheteroaromás gyűrű; Het adott esetben szubsztituált mono-, bi- vagytriciklusos heteroaromás csoport; B -(CH2)n3-, -CH2-O-, -CH2S- képletűcsoport, -CH2-NR6-, -C(O)NR6-, -NR6C(O)- általános képletű csoport,<><> képletű csoport, adott esetben szubsztituált alkeniléncsoportvagy adott esetben szubsztituált alkiniléncsoport, ahol n3 = 0, 1, 2,3, 4 vagy 5; X oxicsoport vagy NR6 általános képletű csoport, ha ==egyes kötés, vagy X hidroxicsoport vagy adott esetben szubsztituáltaminocsoport, ha a kötés nincs jelen; Y oxo-, tioxocsoport, kéthidrogénatom, egy hidrogénatom és egy hidroxicsoport, vagy egyhidrogénatom és egy alkoxicsoport, ha == egyes kötés, vagy Yoxocsoport, két hidrogénatom, egy hidrogénatom és egy hidroxicsoport,egy hidrogénatom és egy merkaptocsoport, vagy egy hidrogénatom és egyalkoxicsoport, ha a kötés nincs jelen; R15 nincs jelen, ha == egyeskötés, vagy hidrogénatom, alkilcsoport, adott esetben szubsztituáltaminocsoport vagy alkoxicsoport, ha a kötés nincs jelen; vagy Y vagyáltalános képletű csoport, és R15 hidrogénatom vagy alkilcsoport - ésgyógyszerészetileg elfogadható sóik, valamint ezeket tartalmazógyógyszerkészítmények képezik, továbbá a vegyületek alkalmazásagyógyszerkészítmények előállítására. Ó
HU0100607A 1997-11-25 1998-11-23 Thrombin receptor antagonists and pharmaceutical compositions containing them HUP0100607A3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US97797997A 1997-11-25 1997-11-25

Publications (2)

Publication Number Publication Date
HUP0100607A2 true HUP0100607A2 (hu) 2002-05-29
HUP0100607A3 HUP0100607A3 (en) 2002-06-28

Family

ID=25525702

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0100607A HUP0100607A3 (en) 1997-11-25 1998-11-23 Thrombin receptor antagonists and pharmaceutical compositions containing them

Country Status (31)

Country Link
EP (1) EP1036072B1 (hu)
JP (2) JP3449620B2 (hu)
KR (1) KR100393492B1 (hu)
CN (2) CN101274929A (hu)
AR (1) AR017189A1 (hu)
AT (1) ATE266025T1 (hu)
AU (1) AU747204B2 (hu)
BR (1) BR9812793A (hu)
CA (1) CA2309352C (hu)
CO (1) CO4990946A1 (hu)
CZ (1) CZ298578B6 (hu)
DE (1) DE69823694T2 (hu)
DK (1) DK1036072T3 (hu)
ES (1) ES2219919T3 (hu)
HK (1) HK1031726A1 (hu)
HU (1) HUP0100607A3 (hu)
ID (1) ID24726A (hu)
IL (1) IL135797A (hu)
MY (1) MY140887A (hu)
NO (1) NO322022B1 (hu)
NZ (1) NZ504218A (hu)
PE (1) PE133799A1 (hu)
PL (1) PL195027B1 (hu)
PT (1) PT1036072E (hu)
RU (1) RU2204557C2 (hu)
SA (1) SA99190972B1 (hu)
SK (1) SK285153B6 (hu)
TR (1) TR200001480T2 (hu)
TW (1) TWI236476B (hu)
WO (1) WO1999026943A1 (hu)
ZA (1) ZA9810685B (hu)

Families Citing this family (20)

* 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
EP1219607B1 (en) * 1999-09-02 2011-04-06 Shionogi & Co., Ltd. Integrase inhibitors containing aromatic heterocycle derivatives
US7304078B2 (en) * 2002-04-16 2007-12-04 Schering Corporation Thrombin receptor antagonists
SI1294714T1 (sl) * 2000-06-15 2007-12-31 Schering Corp Antagonisti trobinskega receptorja
US7235567B2 (en) 2000-06-15 2007-06-26 Schering Corporation Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist
JP4642318B2 (ja) * 2000-06-15 2011-03-02 シェーリング コーポレイション トロンビンレセプターアンタゴニスト
EP1391456B1 (en) 2001-04-19 2009-07-22 Eisai R&D Management Co., Ltd. 2-iminoimidazole derivatives
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
MY143987A (en) * 2004-05-28 2011-07-29 Schering Corp Constrained himbacine analogs as thrombin receptor antagonists
JP2008515899A (ja) * 2004-10-08 2008-05-15 シェーリング コーポレイション トロンビンレセプターアンタゴニスト
JP4775971B2 (ja) * 2005-01-14 2011-09-21 シェーリング コーポレイション ヒンバシンアナログのエキソ−選択的合成
ATE500249T1 (de) * 2005-01-14 2011-03-15 Schering Corp Synthese von himbacinanaloga
ATE530516T1 (de) * 2005-01-14 2011-11-15 Schering Corp Exo- und diastereoselektive synthese von himbacin-analoga
TWI367112B (en) * 2006-06-30 2012-07-01 Schering Corp Immediate-release tablet formulations of a thrombin receptor antagonist
EP2069326B1 (en) * 2006-10-04 2015-03-18 Merck Sharp & Dohme Corp. Bicyclic and tricyclic derivatives as thrombin receptor antagonists
EP2558465B1 (de) 2010-04-16 2014-12-17 Sanofi Trizyklische pyridyl-vinyl-pyrrole als par1-inhibitoren
EP2558462B1 (de) 2010-04-16 2014-10-22 Sanofi Pyridyl-vinyl-pyrazolo-chinoline 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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
TWI236476B (en) 2005-07-21
AU1415899A (en) 1999-06-15
EP1036072A1 (en) 2000-09-20
AU747204B2 (en) 2002-05-09
WO1999026943A1 (en) 1999-06-03
SA99190972B1 (ar) 2006-07-30
PE133799A1 (es) 2000-01-10
DE69823694T2 (de) 2005-04-21
JP2003128670A (ja) 2003-05-08
TR200001480T2 (tr) 2000-09-21
SK7592000A3 (en) 2001-02-12
ZA9810685B (en) 1999-12-23
NO322022B1 (no) 2006-08-07
AR017189A1 (es) 2001-08-22
PL195027B1 (pl) 2007-08-31
BR9812793A (pt) 2000-10-17
HUP0100607A3 (en) 2002-06-28
IL135797A0 (en) 2001-05-20
CZ298578B6 (cs) 2007-11-14
PL341114A1 (en) 2001-03-26
ES2219919T3 (es) 2004-12-01
CZ20001856A3 (cs) 2000-10-11
PT1036072E (pt) 2004-08-31
JP3449620B2 (ja) 2003-09-22
IL135797A (en) 2003-09-17
MY140887A (en) 2010-01-29
KR20010032439A (ko) 2001-04-25
EP1036072B1 (en) 2004-05-06
CN101274929A (zh) 2008-10-01
NO20002659D0 (no) 2000-05-24
KR100393492B1 (ko) 2003-08-02
DK1036072T3 (da) 2004-09-06
HK1031726A1 (en) 2001-06-22
JP2001524479A (ja) 2001-12-04
NZ504218A (en) 2002-04-26
DE69823694D1 (de) 2004-06-09
CO4990946A1 (es) 2000-12-26
CN1290265A (zh) 2001-04-04
CA2309352C (en) 2005-01-25
CA2309352A1 (en) 1999-06-03
ID24726A (id) 2000-08-03
SK285153B6 (sk) 2006-07-07
RU2204557C2 (ru) 2003-05-20
ATE266025T1 (de) 2004-05-15
NO20002659L (no) 2000-07-24

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