EP1017393A4 - Pyrazinone thrombin inhibitors - Google Patents

Pyrazinone thrombin inhibitors

Info

Publication number
EP1017393A4
EP1017393A4 EP98946835A EP98946835A EP1017393A4 EP 1017393 A4 EP1017393 A4 EP 1017393A4 EP 98946835 A EP98946835 A EP 98946835A EP 98946835 A EP98946835 A EP 98946835A EP 1017393 A4 EP1017393 A4 EP 1017393A4
Authority
EP
European Patent Office
Prior art keywords
thrombin inhibitors
pyrazinone
pyrazinone thrombin
inhibitors
thrombin
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP98946835A
Other languages
German (de)
French (fr)
Other versions
EP1017393A1 (en
Inventor
Philip E Sanderson
Terry A Lyle
Bruce D Dorsey
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
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
Priority claimed from GBGB9801005.1A external-priority patent/GB9801005D0/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of EP1017393A1 publication Critical patent/EP1017393A1/en
Publication of EP1017393A4 publication Critical patent/EP1017393A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
EP98946835A 1997-09-05 1998-09-03 Pyrazinone thrombin inhibitors Withdrawn EP1017393A4 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US5805897P 1997-09-05 1997-09-05
US58058P 1997-09-05
GB9801005 1998-01-16
GBGB9801005.1A GB9801005D0 (en) 1998-01-16 1998-01-16 Pyrazinone thrombin inhibitors
PCT/US1998/018417 WO1999011267A1 (en) 1997-09-05 1998-09-03 Pyrazinone thrombin inhibitors

Publications (2)

Publication Number Publication Date
EP1017393A1 EP1017393A1 (en) 2000-07-12
EP1017393A4 true EP1017393A4 (en) 2002-01-23

Family

ID=26312966

Family Applications (1)

Application Number Title Priority Date Filing Date
EP98946835A Withdrawn EP1017393A4 (en) 1997-09-05 1998-09-03 Pyrazinone thrombin inhibitors

Country Status (4)

Country Link
EP (1) EP1017393A4 (en)
JP (1) JP2001514227A (en)
CA (1) CA2301520A1 (en)
WO (1) WO1999011267A1 (en)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9710809D0 (en) 1997-05-23 1997-07-23 Medical Res Council Nucleic acid binding proteins
US6147078A (en) * 1998-05-19 2000-11-14 Merck & Co., Inc. Pyrazinone thrombin inhibitors
DE69926884T2 (en) 1998-06-11 2006-06-14 Johnson & Johnson Pharm Res PYRAZINE PROTEASE INHIBITORS
ES2209337T3 (en) 1998-08-14 2004-06-16 Pfizer Inc. ANTITROMBOTIC AGENTS.
AU752186B2 (en) 1998-10-30 2002-09-12 Merck & Co., Inc. Thrombin inhibitors
EP1124822A4 (en) 1998-10-30 2002-04-03 Merck & Co Inc Thrombin inhibitors
PL352403A1 (en) * 1999-05-19 2003-08-25 Pharmacia Corp Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of coagulation cascade
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6664255B1 (en) * 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
EP1586565A1 (en) * 1999-05-19 2005-10-19 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6750342B1 (en) 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
PL352368A1 (en) * 1999-05-19 2003-08-25 Pharmacia Corp Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
UA58636C2 (en) * 1999-06-04 2003-08-15 Мерк Енд Ко., Інк. Pyrazinone thrombin inhibitors, pharmaceutical composition, method for treatment conditions caused by thrombus formation
EP1202976B1 (en) 1999-07-19 2006-11-02 Merck Frosst Canada Ltd. Pyrazinones, compositions containing such compounds
AU2044401A (en) 1999-11-23 2001-06-04 Merck & Co., Inc. Pyrazinone thrombin inhibitors
AU2001243598A1 (en) 2000-03-13 2001-09-24 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
EP1267876A1 (en) 2000-03-23 2003-01-02 Merck & Co., Inc. Thrombin inhibitors
CA2405561A1 (en) 2000-04-05 2001-10-18 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade
AU2001251315A1 (en) * 2000-04-05 2001-10-23 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
AU2001255399A1 (en) * 2000-04-14 2001-10-30 Corvas International, Inc. Pyridine and pyrazine derivatives as thrombin inhibitors
US6506754B1 (en) 2000-04-14 2003-01-14 Corvas International, Inc. Non-covalent thrombin inhibitors
US20040171616A9 (en) 2000-04-17 2004-09-02 South Michael S. Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade
AU2001265094A1 (en) * 2000-06-01 2001-12-11 Merck And Co., Inc. Pyrazinone thrombin inhibitors
AU2001278927A1 (en) * 2000-07-17 2002-01-30 3-Dimensional Pharmaceuticals, Inc. Cyclic oxyguanidine pyrazinones as protease inhibitors
WO2002009711A1 (en) * 2000-07-28 2002-02-07 Merck & Co., Inc. Thrombin inhibitors
US7119094B1 (en) 2000-11-20 2006-10-10 Warner-Lambert Company Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade
WO2002042272A2 (en) 2000-11-20 2002-05-30 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
US7015223B1 (en) 2000-11-20 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade
JP2004518643A (en) * 2000-12-06 2004-06-24 メルク エンド カムパニー インコーポレーテッド Method for producing thrombin inhibitor
JP2004520399A (en) * 2001-02-09 2004-07-08 メルク エンド カムパニー インコーポレーテッド Thrombin inhibitor
CA2462305A1 (en) 2001-10-03 2003-04-10 Michael S. South 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade
CA2462645A1 (en) 2001-10-03 2003-11-13 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997001338A1 (en) * 1995-06-27 1997-01-16 Merck & Co., Inc. Pyridinone-thrombin inhibitors

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5668289A (en) * 1996-06-24 1997-09-16 Merck & Co., Inc. Pyridinone thrombin inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997001338A1 (en) * 1995-06-27 1997-01-16 Merck & Co., Inc. Pyridinone-thrombin inhibitors

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
SANDERSON et al. "Small, Noncovalent Serine Protease Inhibitors" MEDICINAL RESEARCH REVIEWS, 1999, VOL 19, NR 2, 179-197 *
See also references of WO9911267A1 *

Also Published As

Publication number Publication date
CA2301520A1 (en) 1999-03-11
EP1017393A1 (en) 2000-07-12
WO1999011267A1 (en) 1999-03-11
JP2001514227A (en) 2001-09-11

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