JP2001506606A - プロテアーゼインヒビターとしてのアミノグアニジンおよびアルコキシグアニジン - Google Patents

プロテアーゼインヒビターとしてのアミノグアニジンおよびアルコキシグアニジン

Info

Publication number
JP2001506606A
JP2001506606A JP52482998A JP52482998A JP2001506606A JP 2001506606 A JP2001506606 A JP 2001506606A JP 52482998 A JP52482998 A JP 52482998A JP 52482998 A JP52482998 A JP 52482998A JP 2001506606 A JP2001506606 A JP 2001506606A
Authority
JP
Japan
Prior art keywords
alkyl
methyl
phenoxy
hydrogen
aryl
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.)
Ceased
Application number
JP52482998A
Other languages
English (en)
Japanese (ja)
Other versions
JP2001506606A5 (enExample
Inventor
イー. トムシュック,ブルース
エム. ソル,リチャード
ル,ティアンバオ
エル. フェデ,シンシア
アール. イリグ,カール
ピー. マーコタン,トーマス
ピー. スタグナロ,トーマス
Original Assignee
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
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 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 filed Critical 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
Publication of JP2001506606A publication Critical patent/JP2001506606A/ja
Publication of JP2001506606A5 publication Critical patent/JP2001506606A5/ja
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/72—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/73—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/72—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/75—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing singly-bound oxygen atoms bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/72—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/76—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/72—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/77—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing carboxyl groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/17—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/18—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/19—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/21—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/14—Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/64—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton
    • C07C323/66—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfo, esterified sulfo or halosulfonyl groups, bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96—Sulfur atom
    • 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
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/42—Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
    • 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
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/36—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three 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
    • C07D307/66—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Materials For Medical Uses (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Furan Compounds (AREA)
  • Pyridine Compounds (AREA)
JP52482998A 1996-11-26 1997-11-26 プロテアーゼインヒビターとしてのアミノグアニジンおよびアルコキシグアニジン Ceased JP2001506606A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US3182296P 1996-11-26 1996-11-26
US60/031,822 1996-11-26
PCT/US1997/021649 WO1998023565A2 (en) 1996-11-26 1997-11-26 Aminoguanidines and alkoxyguanidines as protease inhibitors

Publications (2)

Publication Number Publication Date
JP2001506606A true JP2001506606A (ja) 2001-05-22
JP2001506606A5 JP2001506606A5 (enExample) 2005-08-11

Family

ID=21861593

Family Applications (1)

Application Number Title Priority Date Filing Date
JP52482998A Ceased JP2001506606A (ja) 1996-11-26 1997-11-26 プロテアーゼインヒビターとしてのアミノグアニジンおよびアルコキシグアニジン

Country Status (24)

Country Link
US (5) US6235778B1 (enExample)
EP (1) EP0944590B1 (enExample)
JP (1) JP2001506606A (enExample)
KR (1) KR100587546B1 (enExample)
CN (1) CN1237961A (enExample)
AR (1) AR008327A1 (enExample)
AT (1) ATE214693T1 (enExample)
AU (1) AU725058B2 (enExample)
BR (1) BR9713328A (enExample)
CA (1) CA2273023C (enExample)
DE (1) DE69711222T2 (enExample)
DK (1) DK0944590T3 (enExample)
EA (1) EA002740B1 (enExample)
ES (1) ES2174309T3 (enExample)
HU (1) HUP0000733A3 (enExample)
IL (1) IL130102A (enExample)
IN (1) IN190530B (enExample)
NO (1) NO314140B1 (enExample)
NZ (1) NZ336093A (enExample)
PL (1) PL333434A1 (enExample)
PT (1) PT944590E (enExample)
TW (1) TW499412B (enExample)
WO (1) WO1998023565A2 (enExample)
ZA (1) ZA9710646B (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004510759A (ja) * 2000-10-06 2004-04-08 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 プロテアーゼ阻害剤としての、アミノピリジニル、アミノグアニジニル、およびアルコキシグアニジニルで置換されたフェニルアセトアミド
JP2015042652A (ja) * 2009-05-20 2015-03-05 積水メディカル株式会社 血液凝固時間延長剤
JP2019006787A (ja) * 2012-04-12 2019-01-17 ザ トラスティーズ オブ ザ ユニバーシティ オブ ペンシルバニア フィロウイルスコンセンサス抗原、核酸構築物、およびそれから作製されるワクチン、ならびにその使用方法

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6037356A (en) 1997-11-26 2000-03-14 3-Dimensional Pharmaceuticals, Inc. Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
US6344486B1 (en) 1998-04-03 2002-02-05 3-Dimensional Pharmaceuticals, Inc. Benzamide and sulfonamide substituted aminoguanidines and alkoxyguanidines as protease inhibitors
AU750561B2 (en) 1998-04-24 2002-07-25 3-Dimensional Pharmaceuticals, Inc. Amino acid amidinohydrazones, alkoxyguanidines and aminoguanidines as protease inhibitors
NZ508669A (en) 1998-06-11 2003-06-30 Dimensional Pharm Inc Pyrazinone protease inhibitors
AU3731400A (en) 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Methods and compositions useful in inhibiting apoptosis
US6544541B1 (en) * 1999-06-02 2003-04-08 Cardiovascular Solutions, Inc. Devices and compounds for treating arterial restenosis
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
KR100371008B1 (ko) * 2000-08-05 2003-02-06 조동련 혈소판 응집 억제제 부착 스텐트의 그 제조 방법
US20060264608A1 (en) * 2001-08-03 2006-11-23 Wender Paul A Bi-directional synthesis of oligoguanidine transport agents
US7067698B2 (en) * 2001-08-03 2006-06-27 The Board Of Trustees Of The Leland Stanford Junior University Bi-directional synthesis of oligoguanidine transport agents
CN102353569A (zh) * 2002-05-13 2012-02-15 贝克顿·迪金森公司 蛋白酶抑制剂样品采集系统
DK2520654T3 (en) 2003-08-26 2017-05-01 Univ Colorado Regents Inhibitors of serine protease activity and their use in methods and compositions for the treatment of bacterial infections
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
JP2008544987A (ja) * 2005-06-30 2008-12-11 バイエル・クロツプサイエンス・アクチエンゲゼルシヤフト 殺虫性の(二置換プロペニル)フェニルアルキル置換複素環式環を調製するための改善された方法
WO2007075964A2 (en) * 2005-12-22 2007-07-05 Schering Corporation Thrombin receptor antagonists as prophylaxis to complications from cardiopulmonary surgery
DK2474523T3 (da) 2006-12-26 2020-07-13 Lantheus Medical Imaging Inc Ligander til billeddannelse af hjerte-innervation
CN106977429B (zh) 2010-05-11 2021-08-24 蓝瑟斯医学影像公司 用于合成和使用造影剂的组合物、方法和系统
RU2019121905A (ru) 2010-12-31 2019-09-03 Астразенека Юкей Лимитед Ингибиторы аргиназы и способы их применения
US9788539B2 (en) 2011-05-17 2017-10-17 Velico Medical, Inc. Platelet protection solution having beta-galactosidase and sialidase inhibitors
WO2012158983A2 (en) 2011-05-17 2012-11-22 Qiyong Peter Liu Improved platelet storage using a sialidase inhibitor
CN102850451B (zh) * 2011-06-29 2014-05-07 辽宁诺康生物制药有限责任公司 具有抑制纤溶酶活性的重组textilinin-1及其制备方法和应用
EP2903430A1 (en) 2012-10-05 2015-08-12 Velico Medical, Inc. Platelet additive solution having a beta-galactosidase inhibitor
WO2014120886A1 (en) 2013-01-30 2014-08-07 Velico Medical, Inc. Platelet additive solution having a self-assembling hydrogel-forming peptide
US9555016B2 (en) 2013-06-10 2017-01-31 Covidien Lp Lytic agents for use in treating intravascular clots
CN107382869A (zh) * 2017-08-01 2017-11-24 李凯 一种治疗中风后遗症的化合物及制备方法和应用
GB2568550B (en) * 2017-11-21 2021-06-30 Univ Cape Town Method of synthesising 6-deoxy-6-amino-ß-d-glucopyranoside-containing polymers
EP4183777A4 (en) * 2020-07-20 2023-11-29 Shenzhen Mindray Bio-Medical Electronics Co., Ltd USE OF A PLATELET DISAGGREGATION COMPOSITION, DISAGGREGATION REAGENT AND DISAGGREGATION METHOD
GB202108544D0 (en) * 2021-06-15 2021-07-28 Z Factor Ltd Compounds and their use for the treatment of alpha1-antitrypsin deficiency
CN115772196A (zh) * 2021-09-08 2023-03-10 赛诺哈勃药业(成都)有限公司 一种纤溶酶抑制活性的化合物、其制备方法及应用

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3131218A (en) * 1961-02-15 1964-04-28 Smith Kline French Lab N-amino guanidine derivatives
US3271448A (en) 1961-11-21 1966-09-06 Pfizer & Co C Phenoxyalkyl aminoguanidines
BE663481A (enExample) 1964-05-05
US3413303A (en) * 1965-09-27 1968-11-26 Ciba Geigy Corp Aralkenyloxyguanidines
JPS57178739A (en) 1981-04-27 1982-11-04 Mitsubishi Heavy Ind Ltd Bead supplying device for tire molding machine
US4429146A (en) * 1982-04-15 1984-01-31 Gaf Corporation Substituted diphenyl ether herbicides and process for use
JPS6229566A (ja) 1985-07-30 1987-02-07 Taiyo Yakuhin Kogyo Kk 新規グアニジノメチル安息香酸誘導体
DE3929582A1 (de) 1989-09-06 1991-03-07 Hoechst Ag Benzoylguanidine, verfahren zu ihrer herstellung, ihre verwendung als medikament sowie sie enthaltendes medikament
EP0604022A1 (en) 1992-12-22 1994-06-29 Advanced Cardiovascular Systems, Inc. Multilayered biodegradable stent and method for its manufacture
TW257757B (enExample) 1993-03-03 1995-09-21 Boehringer Mannheim Gmbh
GB9318637D0 (en) 1993-09-08 1993-10-27 Ferring Res Ltd Enzyme inhibitors
US6087479A (en) 1993-09-17 2000-07-11 Nitromed, Inc. Localized use of nitric oxide-adducts to prevent internal tissue damage
US5466811A (en) 1994-07-18 1995-11-14 Merck & Co., Inc. Dioxolenylmethyl carbamates pro moieties for amine drugs
AU699821B2 (en) 1994-10-17 1998-12-17 Kabushikikaisha Igaki Iryo Sekkei Stent for liberating drug
US5643580A (en) 1994-10-17 1997-07-01 Surface Genesis, Inc. Biocompatible coating, medical device using the same and methods
US5637113A (en) 1994-12-13 1997-06-10 Advanced Cardiovascular Systems, Inc. Polymer film for wrapping a stent structure
DE19514104C2 (de) * 1995-04-13 1997-05-28 Behringwerke Ag Beschichtung für in den Blutstrom oder in das Gewebe des menschlichen Körpers einbringbares Biomaterial
HU211262A9 (hu) 1995-05-12 1995-11-28 Hoechst Ag Benzoil-guanidinek
HUP9802764A3 (en) 1995-09-29 2000-03-28 Dimensional Pharm Inc Guanidino protease inhibitors
US5792769A (en) 1995-09-29 1998-08-11 3-Dimensional Pharmaceuticals, Inc. Guanidino protease inhibitors
GB9525620D0 (en) 1995-12-15 1996-02-14 Glaxo Group Ltd Chemical compounds
CA2256309C (en) 1995-12-29 2006-08-15 3-Dimensional Pharmaceuticals, Inc. Amidino protease inhibitors
ES2273365T3 (es) 1996-03-29 2007-05-01 Ortho-Mcneil Pharmaceutical, Inc. Amidinohidrazonas utiles como inhibidores de proteasa.
SE9602646D0 (sv) 1996-07-04 1996-07-04 Astra Ab Pharmaceutically-useful compounds

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004510759A (ja) * 2000-10-06 2004-04-08 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 プロテアーゼ阻害剤としての、アミノピリジニル、アミノグアニジニル、およびアルコキシグアニジニルで置換されたフェニルアセトアミド
JP2015042652A (ja) * 2009-05-20 2015-03-05 積水メディカル株式会社 血液凝固時間延長剤
JP2019006787A (ja) * 2012-04-12 2019-01-17 ザ トラスティーズ オブ ザ ユニバーシティ オブ ペンシルバニア フィロウイルスコンセンサス抗原、核酸構築物、およびそれから作製されるワクチン、ならびにその使用方法
US10765733B2 (en) 2012-04-12 2020-09-08 The Trustees Of The University Of Pennsylvania Filovirus consensus antigens, nucleic acid constructs and vaccines made therefrom, and methods of using same
US11723969B2 (en) 2012-04-12 2023-08-15 The Trustees Of The University Of Pennsylvania Filovirus consensus antigens, nucleic acid constructs and vaccines made therefrom, and methods of using same

Also Published As

Publication number Publication date
US20030158252A1 (en) 2003-08-21
US6518310B2 (en) 2003-02-11
EA199900544A1 (ru) 2000-02-28
WO1998023565A2 (en) 1998-06-04
US20010037039A1 (en) 2001-11-01
US6706765B2 (en) 2004-03-16
ES2174309T3 (es) 2002-11-01
ATE214693T1 (de) 2002-04-15
DE69711222D1 (de) 2002-04-25
HUP0000733A2 (hu) 2000-09-28
KR20000069139A (ko) 2000-11-25
EA002740B1 (ru) 2002-08-29
NZ336093A (en) 2000-11-24
PL333434A1 (en) 1999-12-06
US6730783B2 (en) 2004-05-04
IN190530B (enExample) 2003-08-09
HUP0000733A3 (en) 2001-02-28
AU5458498A (en) 1998-06-22
US6638931B1 (en) 2003-10-28
IL130102A0 (en) 2000-06-01
US20040002539A1 (en) 2004-01-01
BR9713328A (pt) 2000-05-09
AU725058B2 (en) 2000-10-05
AR008327A1 (es) 1999-12-29
NO314140B1 (no) 2003-02-03
EP0944590B1 (en) 2002-03-20
DK0944590T3 (da) 2002-07-15
NO992512L (no) 1999-07-26
DE69711222T2 (de) 2002-11-14
CA2273023C (en) 2008-09-02
EP0944590A2 (en) 1999-09-29
NO992512D0 (no) 1999-05-25
TW499412B (en) 2002-08-21
ZA9710646B (en) 1998-09-15
WO1998023565A3 (en) 1998-07-30
CA2273023A1 (en) 1998-06-04
PT944590E (pt) 2002-09-30
US6235778B1 (en) 2001-05-22
CN1237961A (zh) 1999-12-08
IL130102A (en) 2005-09-25
KR100587546B1 (ko) 2006-06-08

Similar Documents

Publication Publication Date Title
DE69711222T2 (de) Aminoguanidine und alkoxyguanidine als protease-hemmer
AU755805B2 (en) Benzamide and sulfonamide substituted aminoguanidines and alkoxyguanidines as protease inhibitors
JP2000507588A (ja) プロテアーゼインヒビターとしてのアミジノヒドラゾン
AU1799199A (en) Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
DE69631692T2 (de) Amidino proteaseinhibitoren
HK1058032A1 (en) Aminopyridinyl-, aminoguanidinyl- and alkoxyguanidinyl- substituted phenyl acetamides as protease inhibitors
JPH08301833A (ja) 選択的トロンビン抑制剤
KR19990063800A (ko) 구아니디노 프로테아제 억제제
JPH11512722A (ja) グアニジノプロテアーゼインヒビター
EP1613319B1 (en) Substituted phenyl acetamides and their use as protease inhibitors
NZ517603A (en) Azacycloalkanone serine protease inhibitors
US6635637B2 (en) Cyclic oxyguanidine protease inhibitors
WO1999055355A1 (en) Amino acid amidinohydrazones, alkoxyguanidines and aminoguanidines as protease inhibitors
UA63887C2 (en) Selective thrombin inhibitors and a pharmaceutical composition based thereon
HK1058032B (en) Aminopyridinyl-, aminoguanidinyl- and alkoxyguanidinyl- substituted phenyl acetamides as protease inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20041126

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20041126

A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A712

Effective date: 20070316

A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20070511

RD02 Notification of acceptance of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7422

Effective date: 20080424

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20081118

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20090218

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20090330

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20090317

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20090526

A313 Final decision of rejection without a dissenting response from the applicant

Free format text: JAPANESE INTERMEDIATE CODE: A313

Effective date: 20090914

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20091020