ATE217321T1 - Aromatische heterocyclische derivate als enzyminhibitoren - Google Patents

Aromatische heterocyclische derivate als enzyminhibitoren

Info

Publication number
ATE217321T1
ATE217321T1 AT95943130T AT95943130T ATE217321T1 AT E217321 T1 ATE217321 T1 AT E217321T1 AT 95943130 T AT95943130 T AT 95943130T AT 95943130 T AT95943130 T AT 95943130T AT E217321 T1 ATE217321 T1 AT E217321T1
Authority
AT
Austria
Prior art keywords
enzymin
hibitors
aromatic heterocyclic
heterocyclic derivatives
pharmaceutically acceptable
Prior art date
Application number
AT95943130T
Other languages
English (en)
Inventor
Susan Yoshiko Tamura
Joseph Edward Semple
William Charles Ripka
Robert John Ardecky
Yu Ge
Stephen H Carpenter
Terence Kevin Brunck
Marguerita S Lim-Wilby
Ruth F Nutt
Matthew Mark Abelman
Original Assignee
Corvas Int 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 US08/356,833 external-priority patent/US6608204B1/en
Priority claimed from US08/481,660 external-priority patent/US5658930A/en
Priority claimed from US08/484,506 external-priority patent/US5656645A/en
Application filed by Corvas Int Inc filed Critical Corvas Int Inc
Application granted granted Critical
Publication of ATE217321T1 publication Critical patent/ATE217321T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • C07D211/76—Oxygen atoms attached in position 2 or 6
    • 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
    • C07D213/60—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AT95943130T 1994-12-13 1995-12-13 Aromatische heterocyclische derivate als enzyminhibitoren ATE217321T1 (de)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US08/356,833 US6608204B1 (en) 1994-12-13 1994-12-13 Aromatic heterocyclic derivatives as enzyme inhibitors
US08/481,660 US5658930A (en) 1994-12-13 1995-06-07 Aromatic heterocyclic derivatives as enzyme inhibitors
US08/484,506 US5656645A (en) 1994-12-13 1995-06-07 Aromatic heterocyclic derivatives as enzyme inhibitors
PCT/US1995/016410 WO1996018644A1 (en) 1994-12-13 1995-12-13 Aromatic heterocyclic derivatives as enzyme inhibitors

Publications (1)

Publication Number Publication Date
ATE217321T1 true ATE217321T1 (de) 2002-05-15

Family

ID=27408281

Family Applications (1)

Application Number Title Priority Date Filing Date
AT95943130T ATE217321T1 (de) 1994-12-13 1995-12-13 Aromatische heterocyclische derivate als enzyminhibitoren

Country Status (12)

Country Link
US (1) US6008351A (de)
EP (1) EP0804464B1 (de)
JP (1) JPH10510539A (de)
AT (1) ATE217321T1 (de)
AU (1) AU693636B2 (de)
BR (1) BR9509994A (de)
CA (1) CA2206400A1 (de)
DE (1) DE69526677T2 (de)
HU (1) HUT77888A (de)
MX (1) MX9704439A (de)
NZ (1) NZ298699A (de)
WO (1) WO1996018644A1 (de)

Families Citing this family (54)

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US6011158A (en) * 1994-12-13 2000-01-04 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
US6342504B1 (en) 1994-12-13 2002-01-29 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
WO1998009987A1 (en) * 1996-09-06 1998-03-12 Biochem Pharma, Inc. Lactam inhibitors of thrombin
CA2268381A1 (en) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. Selective factor xa inhibitors
JP2001502674A (ja) * 1996-10-11 2001-02-27 シーオーアール・セラピューティックス・インコーポレーテッド 選択的Ｘａ因子阻害物質
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
WO1998016524A1 (en) * 1996-10-11 1998-04-23 Cor Therapeutics, Inc. HETEROCYCLIC DERIVATIVES AS 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
CA2277929A1 (en) * 1997-01-22 1998-07-23 Merck & Co., Inc. Thrombin inhibitors
US6369063B1 (en) 1997-04-14 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
AU747531B2 (en) 1997-04-14 2002-05-16 Millennium Pharmaceuticals, Inc. Selective factor Xa inhibitors
US6133256A (en) * 1997-04-14 2000-10-17 Cor Therapeutics Inc Selective factor Xa inhibitors
EP0977772A1 (de) 1997-04-14 2000-02-09 Cor Therapeutics, Inc. Selektive faktor xa-inhibitoren
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6037356A (en) 1997-11-26 2000-03-14 3-Dimensional Pharmaceuticals, Inc. Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
WO1999026920A1 (en) * 1997-11-26 1999-06-03 Corvas International, Inc. Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors (ii)
US6204384B1 (en) 1997-11-26 2001-03-20 Corvas International, Inc. Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors (II)
CA2325471C (en) * 1998-03-23 2010-08-17 Aventis Pharmaceuticals Products Inc. Piperididinyl and n-amidinopiperidinyl derivatives
NZ508669A (en) 1998-06-11 2003-06-30 Dimensional Pharm Inc Pyrazinone protease inhibitors
DE69912379T2 (de) 1998-08-14 2004-05-06 Pfizer Inc. Antithrombosemittel
US7015230B1 (en) 1999-05-19 2006-03-21 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
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
JP2002544263A (ja) * 1999-05-19 2002-12-24 ファルマシア・コーポレイション 抗凝血剤としての置換多環式アリールおよびヘテロアリールウラシル
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones 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
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
WO2000073302A1 (en) * 1999-05-27 2000-12-07 3-Dimensional Pharmaceuticals, Inc. Oxazaheterocycles as protease inhibitors
DE60005351D1 (de) 1999-07-09 2003-10-23 Dimensional Pharm Inc Heteroaryl protease inhibitoren und diagnostische bilderzeugungsmittel
WO2001036351A2 (en) 1999-11-19 2001-05-25 Corvas International, Inc. Plasminogen activator inhibitor antagonists related applications
WO2001068605A1 (en) 2000-03-13 2001-09-20 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
ATE289299T1 (de) 2000-04-05 2005-03-15 Pharmacia Corp Polyzyclisch aryl und heteroaryl substituierte 4- pyronen verwendbar als selektive hemmung von dem koagulationsprozess
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EP1274676A2 (de) 2000-04-17 2003-01-15 Pharmacia Corporation Polycyclische aryl- und heteroaryl- substuierte 1,4-chinone zur selektiven hemmung des blutgerinnungsprozesses
WO2001087842A1 (en) * 2000-05-18 2001-11-22 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
WO2001087851A1 (en) * 2000-05-18 2001-11-22 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
MXPA03000512A (es) 2000-07-17 2003-10-06 Dimensional Pharm Inc Oxiguanidina-pirazinonas ciclicas como inhibidores de proteasas.
JP2004505956A (ja) 2000-08-04 2004-02-26 ３−ディメンショナル　ファーマシューティカルズ，　インコーポレイテッド 環式オキシグアニジンプロテアーゼインヒビター
CA2430037A1 (en) 2000-11-20 2002-05-30 Michael S. South 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
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
HUP0303631A2 (hu) * 2000-12-26 2004-03-01 Ono Pharmaceutical Co., Ltd. Pirimidinszármazékok és eljárás előállításukra
BR0213092A (pt) 2001-10-03 2004-10-19 Pharmacia Corp Compostos heterocìclicos de 6 elementos úteis para a inibição seletiva da cascata de coagulação
MXPA04003170A (es) 2001-10-03 2004-07-08 Pharmacia Corp Compuestos policiclicos, sustituidos, provisto de 5 miembros, utiles para la inhibicion selectiva de la cascada de coagulacion.
CN100513398C (zh) 2002-12-03 2009-07-15 Axys药物公司 作为因子viia抑制剂的2-(2-羟基联苯-3-基)-1h-苯并咪唑-5-甲脒衍生物
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EP1529778A1 (de) * 2003-11-04 2005-05-11 Ajinomoto Co., Inc. Verfahren zu Herstellung von Pyrimidin- Derivat, Zwischenprodukt dafür
EP1533306A1 (de) 2003-11-04 2005-05-25 Ajinomoto Co., Inc. Azlactone und Verfahren zu deren Herstellung
EP2001875A2 (de) * 2006-03-08 2008-12-17 Takeda San Diego, Inc. Glucokinase-aktivatoren
SG176628A1 (en) 2009-06-05 2012-01-30 Link Medicine Corp Aminopyrrolidinone derivatives and uses thereof

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Publication number Priority date Publication date Assignee Title
US5371072A (en) * 1992-10-16 1994-12-06 Corvas International, Inc. Asp-Pro-Arg α-keto-amide enzyme inhibitors
DE69419141D1 (de) * 1993-02-12 1999-07-22 Corvas Int Inc Inhibitoren gegen thrombose
CN1118458C (zh) * 1994-03-31 2003-08-20 弗特克斯药品有限公司 作为白细胞介素抑制剂的嘧啶基衍生物
US5658930A (en) * 1994-12-13 1997-08-19 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
US5656645A (en) * 1994-12-13 1997-08-12 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors

Also Published As

Publication number Publication date
NZ298699A (en) 2001-03-30
CA2206400A1 (en) 1996-06-20
BR9509994A (pt) 1997-12-30
EP0804464A1 (de) 1997-11-05
HUT77888A (hu) 1998-09-28
DE69526677T2 (de) 2002-12-05
JPH10510539A (ja) 1998-10-13
AU693636B2 (en) 1998-07-02
EP0804464B1 (de) 2002-05-08
AU4424896A (en) 1996-07-03
MX9704439A (es) 1997-10-31
WO1996018644A1 (en) 1996-06-20
DE69526677D1 (de) 2002-06-13
US6008351A (en) 1999-12-28

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