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)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (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)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (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)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6346510B1 (en) 1995-10-23 2002-02-12 The Children's Medical Center Corporation Therapeutic antiangiogenic endostatin compositions
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
ATE378330T1 (de) 2002-04-16 2007-11-15 Schering Corp Trizyklische thrombin rezeptor antagonisten
WO2005007868A2 (en) * 2003-07-08 2005-01-27 Accumetrics, Inc. Controlled platelet activation to monitor therapy of adp antagonists
US20070243632A1 (en) * 2003-07-08 2007-10-18 Coller Barry S Methods for measuring platelet reactivity of patients that have received drug eluting stents
ATE406366T1 (de) * 2004-05-28 2008-09-15 Schering Corp Gehinderte himbacinanaloga als thrombinrezeptorantagonisten
EP1778652A2 (en) * 2004-08-20 2007-05-02 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
WO2006041872A2 (en) * 2004-10-08 2006-04-20 Schering Corporation Thrombin receptor antagonists
PL2206697T3 (pl) 2005-01-14 2012-03-30 Merck Sharp & Dohme Egzo- oraz diastereoselektywna synteza analogów himbacyny
US7772276B2 (en) * 2005-01-14 2010-08-10 Schering Corporation Exo-selective synthesis of himbacine analogs
WO2006076564A1 (en) * 2005-01-14 2006-07-20 Schering Corporation Synthesis of himbacine analogs
KR20070116066A (ko) * 2005-03-31 2007-12-06 쉐링 코포레이션 스피로사이클릭 트롬빈 수용체 길항제
US7595169B2 (en) * 2005-04-27 2009-09-29 Accumetrics, Inc. Method for determining percent platelet aggregation
WO2007075808A2 (en) * 2005-12-20 2007-07-05 Schering Corporation 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
EP1971336A2 (en) * 2005-12-22 2008-09-24 Shering Corporation Thrombin receptor antagonists as phophylaxis to complications from cardiopulmonary surgery
KR20080104352A (ko) * 2006-03-29 2008-12-02 쉐링 코포레이션 트롬빈 수용체 길항제로서 유용한 모노사이클릭 및 비사이클릭 힘바신 유도체
EP2266976B1 (en) 2006-04-13 2013-07-31 Merck Sharp & Dohme Corp. Fused ring thrombin receptor antagonists
AR061664A1 (es) * 2006-06-29 2008-09-10 Schering Corp Derivados de himbacina como antagonistas del receptor de trombina biciclicos y triciclicos sustituidos. composiciones farmaceuticas.
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
WO2008060372A2 (en) * 2006-10-04 2008-05-22 Schering Corporation Thrombin receptor antagonists based on the modified tricyclic unit of himbacine
US8153664B2 (en) * 2006-10-04 2012-04-10 Schering Corporation Bicyclic and tricyclic derivatives as thrombin receptor antagonists
WO2008079260A2 (en) * 2006-12-22 2008-07-03 Schering Corporation Disintegration promoters in solid dose wet granulation formulations
JP2010522169A (ja) * 2007-03-23 2010-07-01 シェーリング コーポレイション トロンビン受容体アンタゴニストの使用による、経皮的インターベンション後の有害事象の低減
KR20100017576A (ko) * 2007-05-03 2010-02-16 아큐메트릭스, 인크. 트롬빈 수용체 길항제에 의한 혈소판 응집 억제의 측정 방법
MY152040A (en) 2008-02-05 2014-08-15 Sanofi Aventis Triazolopyridazines as par1 inhibitors, production thereof, and use as medicaments
EP2300435A2 (en) 2008-05-19 2011-03-30 Schering Corporation Heterocyclic compounds as factor ixa inhibitors
WO2010141525A1 (en) 2009-06-04 2010-12-09 Schering Corporation Active metabolite of a thrombin receptor antagonist
EP2440191A2 (en) 2009-06-08 2012-04-18 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
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
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
JP2023534704A (ja) 2020-07-22 2023-08-10 ヤンセン ファーマシューティカ エヌ．ベー． 第ｘｉａ因子阻害剤として有用な化合物
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
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

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5716952A (en) 1992-03-18 1998-02-10 Allergan Method for reducing intraocular pressure in the mammalian eye by administration of muscarinic antagonists
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
US6063847A (en) * 1997-11-25 2000-05-16 Schering Corporation Thrombin receptor antagonists
DE19801636A1 (de) * 1998-01-17 1999-07-22 Bayer Ag Substituierte bicyclische Lactone
CA2410177C (en) 2000-06-15 2010-05-11 Schering Corporation Thrombin receptor antagonists

Also Published As

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

Similar Documents

Publication Publication Date Title
ZA200402849B (en) Himbacine analogues as thrombin receptor antagonists.
IL153308A0 (en) Thrombin receptor antagonists
IL174538A0 (en) Thrombin receptor antagonists
MXPA03001143A (es) Derivados de 4-fenil-piridina como antagonistas del receptor de neuroquinina-1.
IL165841A0 (en) Mchir antagonists
AU2002367424A1 (en) Androgen receptor antagonists
AU2003261392A8 (en) M3muscarinic acetylcholine receptor antagonists
MXPA03005854A (es) Derivados de quinazolona como antagonistas del receptor adrenergico alfa 1a/b.
EP1351933A4 (en) ANTAGONISTS OF IL-8 RECEPTORS
AUPR833401A0 (en) G protein-coupled receptor antagonists
HK1058360A1 (en) 4-Phenyl-pyridine derivatives as neurokinin-1 receptor antagonists.
GB0130261D0 (en) Lactams as tachykinin antagonists
HK1063791A1 (en) Nk1 antagonists
EP1359915A4 (en) UROTENSIN-II RECEPTOR ANTAGONISTS
HK1042699A1 (en) N-triazolylmethyl-piperazine derivatives as neurokinin receptor antagonists.
PL362838A1 (en) Somatostatin antagonists
GB0203412D0 (en) 5-HT 2B receptor antagonists
PL370821A1 (en) N-ureido-piperidines as antagonists viii for ccr-3 receptor
MXPA03006408A (es) Antagonistas de receptores de histamina.
GB0026327D0 (en) Thrombin receptor antagonists
IL158063A0 (en) Crf receptor antagonists
AU2002240149A1 (en) Aminomethyl-pyrroloquinazoline compounds as thrombin receptor antagonists
SI1294714T1 (sl) Antagonisti trobinskega receptorja
SI1406888T1 (sl) Substituirane gama-laktonske spojine kot NMDA antagonisti
AU2002248361A1 (en) Il-8 receptor antagonists