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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • A61P9/04—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
    • A61P9/06—Antiarrhythmics
    • 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
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (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 (ja)
EP (1) EP1436298B1 (ja)
JP (2) JP4307260B2 (ja)
KR (1) KR100960170B1 (ja)
CN (1) CN100369917C (ja)
AR (1) AR036832A1 (ja)
AT (1) ATE525378T1 (ja)
AU (1) AU2002335031C1 (ja)
BR (1) BR0213967A (ja)
CA (1) CA2463628A1 (ja)
CO (1) CO5570668A2 (ja)
EC (1) ECSP045064A (ja)
HU (1) HUP0500443A3 (ja)
IL (1) IL160918A0 (ja)
MX (1) MXPA04003610A (ja)
MY (1) MY139335A (ja)
NO (1) NO329349B1 (ja)
NZ (1) NZ531869A (ja)
PE (1) PE20030808A1 (ja)
PL (1) PL371948A1 (ja)
RU (1) RU2319704C9 (ja)
WO (1) WO2003033501A1 (ja)
ZA (1) ZA200402849B (ja)

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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
SG164279A1 (en) * 2002-04-16 2010-09-29 Schering Corp Tricyclic thrombin receptor antagonists
ATE536889T1 (de) * 2003-07-08 2011-12-15 Accumetrics Inc Kontrollierte thrombozyten-aktivierung zur überwachung der behandlung von adp-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
DE602005009355D1 (de) * 2004-05-28 2008-10-09 Schering Corp Gehinderte himbacinanaloga als thrombinrezeptorantagonisten
US20060063930A1 (en) * 2004-08-20 2006-03-23 Agoston Gregory E Compositions and methods comprising proteinase activated receptor antagonists
US8563511B2 (en) * 2004-10-06 2013-10-22 University Of Rochester Treatment of pulmonary hypertension using an agent that inhibits a tissue factor pathway
EP2075250B1 (en) * 2004-10-08 2015-03-04 Merck Sharp & Dohme Corp. Thrombin receptor antagonists
SI1848705T1 (sl) * 2005-01-14 2010-06-30 Schering Corp Eksoselektivne in diastereoselektivne sinteze himbacinskih analogov
WO2006076564A1 (en) * 2005-01-14 2006-07-20 Schering Corporation Synthesis of himbacine analogs
EP2399912B1 (en) * 2005-01-14 2015-02-25 Merck Sharp & Dohme Corp. An exo-selective synthesis of himbacine analogs
TWI316937B (en) * 2005-03-31 2009-11-11 Schering Corp 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
CN101384590A (zh) * 2005-12-22 2009-03-11 先灵公司 作为凝血酶受体拮抗剂的唑并异喹啉
US20070202140A1 (en) * 2005-12-22 2007-08-30 Veltri Enrico P Thrombin receptor antagonists as prophylaxis to complications from cardiopulmonary surgery
US7888377B2 (en) * 2006-03-29 2011-02-15 Schering Corporation Monocyclic and bicyclic himbacine derivatives useful as thrombin receptor antagonists
US8003803B2 (en) * 2006-04-13 2011-08-23 Schering Corporation Fused ring thrombin receptor antagonists
CN101506198A (zh) 2006-06-29 2009-08-12 先灵公司 取代的双环和三环凝血酶受体拮抗剂
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
CA2667082A1 (en) * 2006-10-04 2008-04-10 Schering Corporation Bicyclic and tricyclic derivatives as thrombin receptor antagonists
WO2008060372A2 (en) * 2006-10-04 2008-05-22 Schering Corporation Thrombin receptor antagonists based on the modified tricyclic unit of himbacine
US20080194560A1 (en) * 2006-12-22 2008-08-14 Zhi Yun Wang Disintegration promoters in solid dose wet granulation formulations
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
EP2153235B1 (en) * 2007-05-03 2012-05-16 Accumetrics, Inc. Methods of measuring inhibition of platelet aggregation by thrombin receptor antagonists
JP5526040B2 (ja) 2008-02-05 2014-06-18 サノフイ Ｐａｒ１阻害剤としてのトリアゾロピリダジン類、その製造法および薬剤としての使用
AR071823A1 (es) 2008-05-19 2010-07-14 Schering Corp Derivados heterociclicos de imidazol y pirazol, inhibidores del factor ixa de coagulacion, composiciones farmaceuticas que los contienen y uso de los mismos para tratar diversos trastornos tromboembolicos.
DK2438060T3 (da) 2009-06-04 2014-01-13 Merck Sharp & Dohme Aktiv metabolit af en trombin-receptor-antagonist
MX2011013091A (es) 2009-06-08 2012-01-12 Schering Corp Un antagonista del receptor de trombina y tableta con dosificacion fija de clopidogrel.
EP2462123B1 (en) 2009-08-04 2013-10-02 Merck Sharp & Dohme Corp. 4,5,6-trisubstituted pyrimidine derivatives as factor ixa inhibitors
US9340530B2 (en) 2012-03-06 2016-05-17 Merck Sharp & Dohme Corp. Preparation and use of bicyclic himbacine derivatives as PAR-1 receptor antagonists
EP3035928B1 (en) 2013-08-22 2023-10-18 Merck Sharp & Dohme LLC 3'-pyridyl substituted- 6,6-difluoro bicyclic himbacine derivatives
WO2015026685A1 (en) 2013-08-22 2015-02-26 Merck Sharp & Dohme Corp. 7a-heterocycle substituted- 6, 6-difluoro bicyclic himbacine derivatives
WO2015026693A1 (en) 2013-08-22 2015-02-26 Merck Sharp & Dohme Corp. 7a-amide substituted-6,6-difluoro bicyclic himbacine derivatives
WO2015160636A1 (en) 2014-04-16 2015-10-22 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
US20230312560A1 (en) 2020-07-22 2023-10-05 Janssen Pharmaceutica Nv Compounds 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
US11814364B2 (en) 2021-03-18 2023-11-14 Janssen Pharmaceutica Nv Pyridine N-oxide derivatives useful as factor XIa inhibitors
US11919881B2 (en) 2021-03-18 2024-03-05 Janssen Pharmaceutica Nv Substituted 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

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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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Also Published As

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

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