AU6391796A - Pyridinone-thrombin inhibitors - Google Patents

Pyridinone-thrombin inhibitors

Info

Publication number
AU6391796A
AU6391796A AU63917/96A AU6391796A AU6391796A AU 6391796 A AU6391796 A AU 6391796A AU 63917/96 A AU63917/96 A AU 63917/96A AU 6391796 A AU6391796 A AU 6391796A AU 6391796 A AU6391796 A AU 6391796A
Authority
AU
Australia
Prior art keywords
pyridinone
thrombin inhibitors
thrombin
inhibitors
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.)
Granted
Application number
AU63917/96A
Other versions
AU703744B2 (en
Inventor
Bruce D Dorsey
Dona L. Dyer
Mark E. Fraley
Richard C. A. Isaacs
Adel M. Naylor-Olsen
Philip E. Sanderson
Joseph P. Vacca
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 to US56095P priority Critical
Priority to US60/000560 priority
Priority to US381895P priority
Priority to US60/003818 priority
Priority to GB9603450 priority
Priority to GBGB9603450.9A priority patent/GB9603450D0/en
Priority to PCT/US1996/010778 priority patent/WO1997001338A1/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of AU6391796A publication Critical patent/AU6391796A/en
Application granted granted Critical
Publication of AU703744B2 publication Critical patent/AU703744B2/en
Anticipated expiration legal-status Critical
Application status is Ceased legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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 heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/64One oxygen atom attached in position 2 or 6
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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 heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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 heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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 heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/76Nitrogen atoms to which a second hetero atom is attached
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
AU63917/96A 1995-06-27 1996-06-24 Pyridinone-thrombin inhibitors Ceased AU703744B2 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
US56095P true 1995-06-27 1995-06-27
US60/000560 1995-06-27
US381895P true 1995-09-15 1995-09-15
US60/003818 1995-09-15
GBGB9603450.9A GB9603450D0 (en) 1996-02-19 1996-02-19 Pyridinone thrombin inhibitors
GB9603450 1996-02-19
PCT/US1996/010778 WO1997001338A1 (en) 1995-06-27 1996-06-24 Pyridinone-thrombin inhibitors

Publications (2)

Publication Number Publication Date
AU6391796A true AU6391796A (en) 1997-01-30
AU703744B2 AU703744B2 (en) 1999-04-01

Family

ID=27268133

Family Applications (1)

Application Number Title Priority Date Filing Date
AU63917/96A Ceased AU703744B2 (en) 1995-06-27 1996-06-24 Pyridinone-thrombin inhibitors

Country Status (5)

Country Link
EP (1) EP0835109A4 (en)
JP (1) JPH11508558A (en)
AU (1) AU703744B2 (en)
CA (1) CA2224437A1 (en)
WO (1) WO1997001338A1 (en)

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US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6063794A (en) 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
AT234091T (en) * 1996-10-24 2003-03-15 Merck & Co Inc Thrombin inhibitors
US5869487A (en) * 1996-10-24 1999-02-09 Merck & Co., Inc. Pyrido 3,4-B!pyrazines for use as thrombin inhibitors
US6017934A (en) * 1997-01-22 2000-01-25 Merck & Co., Inc. Thrombin inhibitors
AU722429B2 (en) * 1997-01-22 2000-08-03 Merck & Co., Inc. Thrombin inhibitors
US5792779A (en) * 1997-02-19 1998-08-11 Merck & Co., Inc. Pyridinone thrombin inhibitors
AU728006B2 (en) * 1997-03-24 2001-01-04 Merck & Co., Inc. Thrombin inhibitors
US5932606A (en) * 1997-03-24 1999-08-03 Merck & Co., Inc. Pyrazinone, pyridinone, piperidine and pyrrolidine thrombin inhibitors
EP0975625A1 (en) 1997-04-14 2000-02-02 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
NZ500352A (en) 1997-04-14 2001-10-26 Cor Therapeutics Inc Cyclic diaza selective factor Xa inhibitors
NZ500353A (en) 1997-04-14 2002-02-01 Cor Therapeutics Inc Cyclic diaza compounds that are selective inhibitors of factor Xa
EP0975659A1 (en) * 1997-04-14 2000-02-02 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
US6011038A (en) * 1997-09-05 2000-01-04 Merck & Co., Inc. Pyrazinone thrombin inhibitors
EP1017393A4 (en) * 1997-09-05 2002-01-23 Merck & Co Inc Pyrazinone thrombin inhibitors
US6087373A (en) * 1997-09-23 2000-07-11 Merck & Co., Inc. Thrombin inhibitors
US6133297A (en) * 1997-09-30 2000-10-17 Merck & Co., Inc. Thrombin inhibitors
CA2311969A1 (en) 1997-11-26 1999-06-03 3-Dimensional Pharmaceuticals, Inc. Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
JP2001524522A (en) * 1997-12-01 2001-12-04 メルク エンド カムパニー インコーポレーテッド Thrombin inhibitor
CN1209368C (en) * 1998-02-17 2005-07-06 日本化药株式会社 Novel acetamide derivative and use thereof
US6147078A (en) * 1998-05-19 2000-11-14 Merck & Co., Inc. Pyrazinone thrombin inhibitors
JP2002516326A (en) * 1998-05-26 2002-06-04 メルク エンド カムパニー インコーポレーテッド Imidazopyridine thrombin inhibitors
AU759427B2 (en) * 1998-06-11 2003-04-17 3-Dimensional Pharmaceuticals, Inc. Pyrazinone protease inhibitors
PT997474E (en) 1998-08-14 2004-01-30 Pfizer Antitrombotic agents
EP1117660A4 (en) * 1998-09-28 2002-01-09 Merck & Co Inc Thrombin inhibitors
JP2002528543A (en) 1998-10-30 2002-09-03 メルク エンド カムパニー インコーポレーテッド Thrombin inhibitor
WO2000026210A1 (en) 1998-10-30 2000-05-11 Merck & Co., Inc. Thrombin inhibitors
FR2786482B1 (en) * 1998-11-27 2002-08-09 Synthelabo Novel 2-pyridone derivatives, their preparation and their therapeutic application
AR023510A1 (en) 1999-04-21 2002-09-04 Astrazeneca Ab A kit of parts, pharmaceutical formulation and use of a thrombin inhibitor.
US6239132B1 (en) 1999-04-23 2001-05-29 Merck & Co., Inc. Thrombin inhibitors
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
WO2000069834A1 (en) * 1999-05-19 2000-11-23 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones 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
PL352403A1 (en) * 1999-05-19 2003-08-25 Pharmacia Corp Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of 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
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US6750342B1 (en) 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
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JP4495377B2 (en) * 1999-06-04 2010-07-07 メルク・シャープ・エンド・ドーム・コーポレイション Pyrazinone thrombin inhibitor
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US6777431B2 (en) * 2001-07-13 2004-08-17 Corvas International, Inc. Non-convalent thrombin inhibitors
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TW223629B (en) * 1992-03-06 1994-05-11 Hoffmann La Roche

Also Published As

Publication number Publication date
CA2224437A1 (en) 1997-01-16
JPH11508558A (en) 1999-07-27
EP0835109A1 (en) 1998-04-15
EP0835109A4 (en) 1999-02-03
WO1997001338A1 (en) 1997-01-16
AU703744B2 (en) 1999-04-01

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