WO2011162562A3 - Bicycles fusionnés [6+5] en tant qu'antagonistes de la thrombine, procédé de préparation de ceux-ci et compositions pharmaceutiques contenant les bicycles - Google Patents

Bicycles fusionnés [6+5] en tant qu'antagonistes de la thrombine, procédé de préparation de ceux-ci et compositions pharmaceutiques contenant les bicycles Download PDF

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Publication number
WO2011162562A3
WO2011162562A3 PCT/KR2011/004607 KR2011004607W WO2011162562A3 WO 2011162562 A3 WO2011162562 A3 WO 2011162562A3 KR 2011004607 W KR2011004607 W KR 2011004607W WO 2011162562 A3 WO2011162562 A3 WO 2011162562A3
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WO
WIPO (PCT)
Prior art keywords
bicycles
pharmaceutical compositions
fused
preparation
compositions containing
Prior art date
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PCT/KR2011/004607
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English (en)
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WO2011162562A2 (fr
Inventor
Sun Kyung Lee
Jong Whan Song
Dong Chul Lim
Woo Young Cho
Chul Min Park
Original Assignee
Korea Research Institute Of Chemical Technology
Lg Life Sciences Ltd.
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Application filed by Korea Research Institute Of Chemical Technology, Lg Life Sciences Ltd. filed Critical Korea Research Institute Of Chemical Technology
Publication of WO2011162562A2 publication Critical patent/WO2011162562A2/fr
Publication of WO2011162562A3 publication Critical patent/WO2011162562A3/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/72—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 spiro-condensed with carbocyclic rings
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/06—Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La présente invention porte sur les nouveaux dérivés bicycles fusionnés [6+5], sur des sels ou isomères pharmaceutiquement acceptables de ceux-ci, sur des procédés de préparation de ceux-ci, et sur des compositions pharmaceutiques comprenant ceux-ci. Les dérivés bicycles fusionnés [6+5] peuvent antagoniser le récepteur de la thrombine et peuvent être ainsi utilisés efficacement pour le traitement et la prévention du thrombus, de l'agrégation plaquettaire, de l'athérosclérose, de la resténose, de la coagulation sanguine, de l'hypertension, de l'arythmie, de l'angine de poitrine, de l'insuffisance cardiaque, de l'inflammation et du cancer lorsqu'ils sont utilisés seuls ou avec d'autres agents cardiovasculaires.
PCT/KR2011/004607 2010-06-25 2011-06-24 Bicycles fusionnés [6+5] en tant qu'antagonistes de la thrombine, procédé de préparation de ceux-ci et compositions pharmaceutiques contenant les bicycles WO2011162562A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR20100060863 2010-06-25
KR10-2010-0060863 2010-06-25

Publications (2)

Publication Number Publication Date
WO2011162562A2 WO2011162562A2 (fr) 2011-12-29
WO2011162562A3 true WO2011162562A3 (fr) 2012-05-31

Family

ID=45371970

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2011/004607 WO2011162562A2 (fr) 2010-06-25 2011-06-24 Bicycles fusionnés [6+5] en tant qu'antagonistes de la thrombine, procédé de préparation de ceux-ci et compositions pharmaceutiques contenant les bicycles

Country Status (2)

Country Link
KR (1) KR101303348B1 (fr)
WO (1) WO2011162562A2 (fr)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2822557B1 (fr) 2012-03-06 2017-08-23 Merck Sharp & Dohme Corp. Préparation et utilisation de dérivés bicycliques d'himbacine en tant qu'antagonistes du récepteur de par
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
EP3035929B1 (fr) 2013-08-22 2024-07-03 Merck Sharp & Dohme LLC Dérivés bicycliques de 7a-amide substitué-6,6-difluoro himbacine
WO2015026685A1 (fr) 2013-08-22 2015-02-26 Merck Sharp & Dohme Corp. Dérivés bicycliques de 7a-hétérocycle substitué-6,6-difluoro himbacine
TW201540711A (zh) * 2014-02-27 2015-11-01 Ono Pharmaceutical Co 具有選擇性ｅｐ２促效劑活性的化合物
US20170240539A1 (en) * 2014-10-15 2017-08-24 Merck Sharp & Dohme Corp. Preparation and Use of Cyclic Sulfonamide Derivatives as PAR-1 Receptor Antagonists
US10385045B2 (en) 2015-07-23 2019-08-20 Ono Pharmaceutical Co., Ltd. Compound having EP2 agonist activity

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6063847A (en) * 1997-11-25 2000-05-16 Schering Corporation Thrombin receptor antagonists
WO2005118576A1 (fr) * 2004-05-28 2005-12-15 Schering Corporation Analogues d'himbacine contraints utilises comme antagonistes du recepteur de thrombine

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2065384T1 (sl) 2002-04-16 2011-05-31 Schering Corp Tricikliäśni trombin receptor antagonist

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6063847A (en) * 1997-11-25 2000-05-16 Schering Corporation Thrombin receptor antagonists
WO2005118576A1 (fr) * 2004-05-28 2005-12-15 Schering Corporation Analogues d'himbacine contraints utilises comme antagonistes du recepteur de thrombine

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
CHACKALAMANNIL, SAMUEL.: "Discovery of a Novel, Orally Active Himbacine-Based hrombin Receptor Antagonist (SCH 530348) with Potent Antiplatelet Activity.", J. MED. CHEM., vol. 51, 2008, pages 3061 - 3064 *
STOCKLAND JR. ET AL.: "Remarkable tolerance of ethynyl steroids to air and water in microwave-assisted hydrophosphinylation: Reaction scope and limita tions.", JOURNAL OF ORGANOMETALLIC CHEMISTRY, vol. 69, 2006, pages 4042 - 4053 *

Also Published As

Publication number Publication date
KR101303348B1 (ko) 2013-09-03
WO2011162562A2 (fr) 2011-12-29
KR20120000528A (ko) 2012-01-02

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