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ZA200402849B - Himbacine analogues as thrombin receptor antagonists. - Google Patents

Himbacine analogues as thrombin receptor antagonists.

Info

Publication number
ZA200402849B
ZA200402849B ZA200402849A ZA200402849A ZA200402849B ZA 200402849 B ZA200402849 B ZA 200402849B ZA 200402849 A ZA200402849 A ZA 200402849A ZA 200402849 A ZA200402849 A ZA 200402849A ZA 200402849 B ZA200402849 B ZA 200402849B
Authority
ZA
South Africa
Prior art keywords
himbacine
analogues
receptor antagonists
thrombin receptor
thrombin
Prior art date
Application number
ZA200402849A
Other languages
English (en)
Inventor
Samuel Chackalamannil
Martin C Clasby
Mariappan V Chelliah
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 ZA200402849B publication Critical patent/ZA200402849B/xx

Links

Classifications

    • 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
    • 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
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • 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
    • 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
    • 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
    • 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
    • C07D493/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
ZA200402849A 2001-10-18 2004-04-15 Himbacine analogues as thrombin receptor antagonists. ZA200402849B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US33035901P 2001-10-18 2001-10-18

Publications (1)

Publication Number Publication Date
ZA200402849B true ZA200402849B (en) 2005-01-14

Family

ID=23289411

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200402849A ZA200402849B (en) 2001-10-18 2004-04-15 Himbacine analogues as thrombin receptor antagonists.

Country Status (23)

Country Link
US (2) US7037920B2 (xx)
EP (1) EP1436298B1 (xx)
JP (2) JP4307260B2 (xx)
KR (1) KR100960170B1 (xx)
CN (1) CN100369917C (xx)
AR (1) AR036832A1 (xx)
AT (1) ATE525378T1 (xx)
AU (1) AU2002335031C1 (xx)
BR (1) BR0213967A (xx)
CA (1) CA2463628A1 (xx)
CO (1) CO5570668A2 (xx)
EC (1) ECSP045064A (xx)
HU (1) HUP0500443A3 (xx)
IL (1) IL160918A0 (xx)
MX (1) MXPA04003610A (xx)
MY (1) MY139335A (xx)
NO (1) NO329349B1 (xx)
NZ (1) NZ531869A (xx)
PE (1) PE20030808A1 (xx)
PL (1) PL371948A1 (xx)
RU (1) RU2319704C9 (xx)
WO (1) WO2003033501A1 (xx)
ZA (1) ZA200402849B (xx)

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US7488742B2 (en) * 2000-06-15 2009-02-10 Schering Corporation Thrombin receptor antagonists
US7235567B2 (en) * 2000-06-15 2007-06-26 Schering Corporation Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist
ATE378330T1 (de) 2002-04-16 2007-11-15 Schering Corp Trizyklische thrombin rezeptor antagonisten
US20070243632A1 (en) * 2003-07-08 2007-10-18 Coller Barry S Methods for measuring platelet reactivity of patients that have received drug eluting stents
EP1641492B1 (en) 2003-07-08 2011-12-14 Accumetrics, Inc. Controlled platelet activation to monitor therapy of adp antagonists
DE602005009355D1 (de) * 2004-05-28 2008-10-09 Schering Corp Gehinderte himbacinanaloga als thrombinrezeptorantagonisten
CA2576971A1 (en) * 2004-08-20 2006-03-02 Entremed, Inc. Compositions and methods comprising proteinase activated receptor antagonists
CA2582353A1 (en) * 2004-10-06 2006-04-20 University Of Rochester Treatment of pulmonary hypertension using an agent that inhibits a tissue factor pathway
US7488752B2 (en) * 2004-10-08 2009-02-10 Schering Corporation Thrombin receptor antagonists
US7772276B2 (en) * 2005-01-14 2010-08-10 Schering Corporation Exo-selective synthesis of himbacine analogs
EP1848705B1 (en) * 2005-01-14 2010-02-24 Schering Corporation Exo- and diastereo- selective syntheses of himbacine analogs
PT1853592E (pt) * 2005-01-14 2011-05-10 Schering Corp S?ntese de an?logos da himbacina
AU2006230292A1 (en) * 2005-03-31 2006-10-05 Schering Corporation Spirocyclic thrombin receptor antagonists
US7595169B2 (en) * 2005-04-27 2009-09-29 Accumetrics, Inc. Method for determining percent platelet aggregation
US20070219154A1 (en) * 2005-12-20 2007-09-20 Suxing Liu Methods for preventing and/or treating a cell proliferative disorder
EP1966203B1 (en) * 2005-12-22 2013-11-13 Merck Sharp & Dohme Corp. Oxazoloisoquinoline derivatives as thrombin receptor antagonists
AU2006331583A1 (en) * 2005-12-22 2007-07-05 Schering Corporation Thrombin receptor antagonists as prophylaxis to complications from cardiopulmonary surgery
MX2008012574A (es) * 2006-03-29 2008-10-10 Schering Corp Derivados de himbacina monociclitos y biciclicos utiles como antagonistas del receptor de trombina.
CA2650404A1 (en) * 2006-04-13 2007-10-25 Schering Corporation Fused ring thrombin receptor antagonists
EP2032560B1 (en) 2006-06-29 2013-05-01 Merck Sharp & Dohme Corp. Substituted bicyclic and tricyclic thrombin receptor antagonists
AR061727A1 (es) 2006-06-30 2008-09-17 Schering Corp Sintesis de dietil [[ 5- ( 3-fluorofenil) -piridin -2il] metil] fosfonato
TWI367112B (en) 2006-06-30 2012-07-01 Schering Corp Immediate-release tablet formulations of a thrombin receptor antagonist
TWI343262B (en) * 2006-09-26 2011-06-11 Schering Corp Rapidly disintegrating lyophilized oral formulations of a thrombin receptor antagonist
AU2007320029A1 (en) * 2006-10-04 2008-05-22 Schering Corporation Thrombin receptor antagonists based on the modified tricyclic unit of himbacine
WO2008042422A2 (en) * 2006-10-04 2008-04-10 Schering Corporation Bicyclic and tricyclic derivatives as thrombin receptor antagonists
MX2009006873A (es) * 2006-12-22 2009-07-03 Schering Corp Promotores de desintegracion en formulaciones de granulacion humeda de dosis solida.
BRPI0809095A2 (pt) * 2007-03-23 2014-09-09 Schering Corp Redução de eventos adversos após intervenção percutânea através de uso de um antagonista de receptor de trombina
ES2387700T3 (es) * 2007-05-03 2012-09-28 Accumetrics, Inc. Métodos para medir la inhibición de la agregación de plaquetas mediante antagonistas del receptor de trombina
WO2009097970A1 (de) 2008-02-05 2009-08-13 Sanofi-Aventis Triazolopyridazine als par1-inhibitoren, ihre herstellung und verwendung als arzneimittel
WO2009143039A2 (en) 2008-05-19 2009-11-26 Schering Corporation Heterocyclic compounds as factor ixa inhibitors
MX2011012861A (es) 2009-06-04 2012-01-25 Schering Corp Metabolito activo de un antagonista de receptor de trombina.
WO2010144339A2 (en) 2009-06-08 2010-12-16 Schering Corporation A thrombin receptor antagonist and clopidogrel fixed dose tablet
WO2011017296A1 (en) 2009-08-04 2011-02-10 Schering Corporation 4, 5, 6-trisubstituted pyrimidine derivatives as factor ixa inhibitors
EP2822557B1 (en) 2012-03-06 2017-08-23 Merck Sharp & Dohme Corp. Preparation and use of bicyclic himbacine derivatives as par-receptor antagonists
US9808473B2 (en) 2013-08-22 2017-11-07 Merck Sharp & Dohme Corp. Preparation and use of 3-pyridyl substituted-6,6-difluoro bicyclic himbacine derivatives as par-1 receptor antagonists
WO2015026693A1 (en) 2013-08-22 2015-02-26 Merck Sharp & Dohme Corp. 7a-amide substituted-6,6-difluoro bicyclic himbacine derivatives
EP3035930A4 (en) 2013-08-22 2017-03-08 Merck Sharp & Dohme Corp. 7a-heterocycle substituted- 6, 6-difluoro bicyclic himbacine derivatives
US9969724B2 (en) 2014-04-16 2018-05-15 Merck Sharp & Dohme Corp. Factor IXa inhibitors
CN104610330A (zh) * 2015-02-25 2015-05-13 成都安斯利生物医药有限公司 一种制备(e)-3-丙烯酸乙酯频呐硼酸酯的方法
CN116133660B (zh) 2020-07-22 2025-05-02 詹森药业有限公司 可用作因子XIa抑制剂的化合物
US11919881B2 (en) 2021-03-18 2024-03-05 Janssen Pharmaceutica Nv Substituted pyridine N-oxide derivatives useful as a factor XIa inhibitors
US11814364B2 (en) 2021-03-18 2023-11-14 Janssen Pharmaceutica Nv Pyridine N-oxide derivatives useful as factor XIa inhibitors
US11845748B2 (en) 2021-03-18 2023-12-19 Janssen Pharmaceutica Nv Bicyclic pyridine N-oxide derivatives useful as a factor XIa inhibitors
US11897880B2 (en) 2021-04-30 2024-02-13 Janssen Pharmaceutica Nv 7,8-dihydrobenzo[e]pyrido[3,4-c]azocine-2,5(3H,6H)-dione derivatives useful as a factor XIa inhibitors
US11958856B2 (en) 2021-07-22 2024-04-16 Janssen Pharmaceutica Nv Substituted 1,2,3,8,9,9a-hexahydro-5H-pyrrolo[1,2-a]azepin-5-ones as factor XIa inhibitors
US12286429B2 (en) 2021-07-22 2025-04-29 Janssen Pharmaceutica Nv 5-oxo-1,2,3,5,8,8a-hexahydroindolizine-3-carboxamide derivatives useful as a factor XIa inhibitors

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IL106197A (en) 1992-07-30 1999-11-30 Cor Therapeutics Inc Agagonists for the rhombin receptors and pharmaceutical preparations containing them
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
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MY130642A (en) 2000-06-15 2007-07-31 Schering Corp Nor-seco himbacine derivatives useful as thrombin receptor antagonists

Also Published As

Publication number Publication date
JP2005529841A (ja) 2005-10-06
KR20050036845A (ko) 2005-04-20
CA2463628A1 (en) 2003-04-24
ECSP045064A (es) 2004-05-28
RU2319704C9 (ru) 2008-08-20
KR100960170B1 (ko) 2010-05-26
US20060106050A1 (en) 2006-05-18
RU2004115114A (ru) 2005-10-27
RU2319704C2 (ru) 2008-03-20
BR0213967A (pt) 2005-08-30
NO20042021L (no) 2004-05-14
US7037920B2 (en) 2006-05-02
JP2009029820A (ja) 2009-02-12
US20030203927A1 (en) 2003-10-30
HUP0500443A2 (hu) 2005-08-29
JP4307260B2 (ja) 2009-08-05
NZ531869A (en) 2006-11-30
EP1436298B1 (en) 2011-09-21
AU2002335031C1 (en) 2006-11-16
EP1436298A1 (en) 2004-07-14
PE20030808A1 (es) 2003-09-22
IL160918A0 (en) 2004-08-31
HUP0500443A3 (en) 2009-12-28
PL371948A1 (en) 2005-07-11
AR036832A1 (es) 2004-10-06
ATE525378T1 (de) 2011-10-15
CO5570668A2 (es) 2005-10-31
CN1571789A (zh) 2005-01-26
CN100369917C (zh) 2008-02-20
NO329349B1 (no) 2010-10-04
MY139335A (en) 2009-09-30
AU2002335031B2 (en) 2005-06-30
MXPA04003610A (es) 2004-07-27
WO2003033501A1 (en) 2003-04-24

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