ES2174309T3 - Aminoguanidinas y alcoxiguanidinas como inhibidores de proteasa. - Google Patents

Aminoguanidinas y alcoxiguanidinas como inhibidores de proteasa.

Info

Publication number
ES2174309T3
ES2174309T3 ES97948537T ES97948537T ES2174309T3 ES 2174309 T3 ES2174309 T3 ES 2174309T3 ES 97948537 T ES97948537 T ES 97948537T ES 97948537 T ES97948537 T ES 97948537T ES 2174309 T3 ES2174309 T3 ES 2174309T3
Authority
ES
Spain
Prior art keywords
inhibit
compounds
blood
formation
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.)
Expired - Lifetime
Application number
ES97948537T
Other languages
English (en)
Spanish (es)
Inventor
Bruce E Tomczuk
Richard M Soll
Tianbao Lu
Cynthia L Fedde
Carl R Illig
Thomas P Markotan
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.)
3 Dimensional Pharmaceuticals Inc
Original Assignee
3 Dimensional Pharmaceuticals 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
Application filed by 3 Dimensional Pharmaceuticals Inc filed Critical 3 Dimensional Pharmaceuticals Inc
Application granted granted Critical
Publication of ES2174309T3 publication Critical patent/ES2174309T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime 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)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Quinoline Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Furan Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Materials For Medical Uses (AREA)
  • Plural Heterocyclic Compounds (AREA)
ES97948537T 1996-11-26 1997-11-26 Aminoguanidinas y alcoxiguanidinas como inhibidores de proteasa. Expired - Lifetime ES2174309T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US3182296P 1996-11-26 1996-11-26

Publications (1)

Publication Number Publication Date
ES2174309T3 true ES2174309T3 (es) 2002-11-01

Family

ID=21861593

Family Applications (1)

Application Number Title Priority Date Filing Date
ES97948537T Expired - Lifetime ES2174309T3 (es) 1996-11-26 1997-11-26 Aminoguanidinas y alcoxiguanidinas como inhibidores de proteasa.

Country Status (24)

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

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI222441B (en) 1997-11-26 2004-10-21 Dimensional Pharm 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
WO1999064446A1 (en) * 1998-06-11 1999-12-16 3-Dimensional Pharmaceuticals, 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
KR20030015393A (ko) 2000-07-17 2003-02-20 3-디멘져널 파마슈티칼즈 인코오포레이티드 프로테아제 억제제 기능이 있는 시클릭 옥시구아니딘피라지논
MXPA03000963A (es) 2000-08-04 2004-04-05 Dimensional Pharm Inc Inhibidores de oxiguanidina ciclica proteasa.
KR100371008B1 (ko) * 2000-08-05 2003-02-06 조동련 혈소판 응집 억제제 부착 스텐트의 그 제조 방법
UA75093C2 (en) 2000-10-06 2006-03-15 Dimensional Pharm Inc Aminopyridinyl-,aminoguanidinyl-, and alkoxyguanidinesubstituted phenylsubstituted phenylacetamides as protease inhibitors
US20060264608A1 (en) * 2001-08-03 2006-11-23 Wender Paul A Bi-directional synthesis of oligoguanidine transport agents
WO2003014076A2 (en) * 2001-08-03 2003-02-20 The Board Of Trustees Of The Leland Stanford Junior University Bi-directional synthesis of oligoguanidine transport agents
MXPA04011129A (es) * 2002-05-13 2005-02-17 Becton Dickinson Co Sistema de recoleccion de muestra de inhibidor de proteasa.
CA2536918A1 (en) 2003-08-26 2005-03-03 Leland Shapiro Compositions of, and methods for, alpha-1 antitrypsin fc fusion molecules
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
EP1902023A4 (en) * 2005-06-30 2009-08-12 Bayer Cropscience Ag IMPROVED PROCESS FOR PREPARING PHENYLALKYL SUBSTITUTED INSECTICIDE HETEROCYCLES (DISUBSTITUTED PROPENYL)
CN101384259A (zh) * 2005-12-22 2009-03-11 先灵公司 作为预防来自心肺外科手术的并发症的凝血酶受体拮抗剂
RU2506256C2 (ru) 2006-12-26 2014-02-10 Лантеус Медикал Имэджинг, Инк. Лиганды для визуализации иннервации сердца
JPWO2010134345A1 (ja) * 2009-05-20 2012-11-08 積水メディカル株式会社 血液凝固時間延長剤
CA3041113C (en) * 2010-05-11 2022-01-18 Lantheus Medical Imaging, Inc. Compositions, methods, and systems for the synthesis and use of imaging agents
RU2019121905A (ru) 2010-12-31 2019-09-03 Астразенека Юкей Лимитед Ингибиторы аргиназы и способы их применения
JP2014515352A (ja) 2011-05-17 2014-06-30 ベリコ メディカル インコーポレイティッド シアリダーゼ阻害剤を用いた血小板の保存の改善法
US9788539B2 (en) 2011-05-17 2017-10-17 Velico Medical, Inc. Platelet protection solution having beta-galactosidase and sialidase inhibitors
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
EP2836230B1 (en) * 2012-04-12 2022-09-07 The Trustees Of The University Of Pennsylvania Filovirus consensus antigens, nucleic acid constructs and vaccines made therefrom, and methods of using same
CA2887083A1 (en) 2012-10-05 2014-04-10 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 (show.php) * 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 (show.php) 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
ATE434423T1 (de) 1994-10-17 2009-07-15 Igaki Iryo Sekkei Kk Medikamentenfreisetzender stent
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
US5792769A (en) 1995-09-29 1998-08-11 3-Dimensional Pharmaceuticals, Inc. Guanidino protease inhibitors
WO1997011693A1 (en) 1995-09-29 1997-04-03 3-Dimensional Pharmaceuticals, Inc. Guanidino protease inhibitors
GB9525620D0 (en) 1995-12-15 1996-02-14 Glaxo Group Ltd Chemical compounds
JP2000503010A (ja) 1995-12-29 2000-03-14 スリー―ダイメンショナル・ファーマスーティカルス・インコーポレーテッド アミジノプロテアーゼ阻害剤
EP0906091B1 (en) 1996-03-29 2006-10-04 Ortho-McNeil Pharmaceuticals, Inc. Amidinohydrazones as protease inhibitors
SE9602646D0 (sv) 1996-07-04 1996-07-04 Astra Ab Pharmaceutically-useful compounds

Also Published As

Publication number Publication date
BR9713328A (pt) 2000-05-09
AU725058B2 (en) 2000-10-05
EA199900544A1 (ru) 2000-02-28
US6235778B1 (en) 2001-05-22
JP2001506606A (ja) 2001-05-22
IL130102A (en) 2005-09-25
US6730783B2 (en) 2004-05-04
AR008327A1 (es) 1999-12-29
TW499412B (en) 2002-08-21
PL333434A1 (en) 1999-12-06
HUP0000733A3 (en) 2001-02-28
HUP0000733A2 (hu) 2000-09-28
KR100587546B1 (ko) 2006-06-08
DE69711222D1 (de) 2002-04-25
US6706765B2 (en) 2004-03-16
US20040002539A1 (en) 2004-01-01
US6638931B1 (en) 2003-10-28
NO992512L (no) 1999-07-26
EP0944590A2 (en) 1999-09-29
DK0944590T3 (da) 2002-07-15
AU5458498A (en) 1998-06-22
ATE214693T1 (de) 2002-04-15
NO992512D0 (no) 1999-05-25
CN1237961A (zh) 1999-12-08
IN190530B (show.php) 2003-08-09
NZ336093A (en) 2000-11-24
US20010037039A1 (en) 2001-11-01
IL130102A0 (en) 2000-06-01
PT944590E (pt) 2002-09-30
CA2273023C (en) 2008-09-02
WO1998023565A3 (en) 1998-07-30
NO314140B1 (no) 2003-02-03
KR20000069139A (ko) 2000-11-25
DE69711222T2 (de) 2002-11-14
CA2273023A1 (en) 1998-06-04
WO1998023565A2 (en) 1998-06-04
EA002740B1 (ru) 2002-08-29
EP0944590B1 (en) 2002-03-20
US20030158252A1 (en) 2003-08-21
US6518310B2 (en) 2003-02-11
ZA9710646B (en) 1998-09-15

Similar Documents

Publication Publication Date Title
ES2174309T3 (es) Aminoguanidinas y alcoxiguanidinas como inhibidores de proteasa.
BR9815325A (pt) Heteroaril, aminoguanidinas e alcóxiguanidinas eseu uso como inibidores da protease
AR008377A1 (es) Un compuesto derivado de la 3-aroilbencilpiridazinona, una composicion farmaceutica particularmente para el tratamiento de enfermedades inflamatorias o autoinmunes que contiene dicho compuesto
AR029216A1 (es) Compuestos inhibidores no peptidicos de la union celular dependiente de vla-4 utiles en el tratamiento de enfermedades inflamatorias, autoinmunes y respiratorias; composicion farmaceutica y procedimiento de tratamiento
ES2183331T3 (es) Inhibidores de sulfamida-metaloproteasa.
MX9307779A (es) Compuestos benzoicos fundidos.
ES2185711T3 (es) 1,4-benzotiazepina-1,1-dioxidoshipolipimemicos.
ES8600305A1 (es) Procedimiento de preparar compuestos beta-lactamicos
ES2081178T3 (es) Compuestos anti-tumorales que contienen anillos quinazolina y tetrazol.
AR070473A2 (es) Compuestos inhibidores de la renina, un procedimiento de preparacion del compuesto, una composicion farmaceutica, uso del compuesto para preparar un medicamento y compuesto intermediario
ES2122916B1 (es) Esteres de acidos oximsulfonicos y su empleo como acidos sulfonicos latentes.
AR007077A1 (es) Derivados tetrahidroisoquinolina, un procedimiento para su preparacion, una composicion farmaceutica que los contiene, el uso de los mismos parala fabricacion de un medicamento
ES2160640T3 (es) Nuevos (r)-5-carbamoil-8-fluoro-3-amino disustituido en n,n-3,4-dihidro-2h-1-benzopiranos.
ES2031876T3 (es) Un procedimiento para la preparacion de 5,6-dihidro-2-(fenil sustituido)-1,2,4,-triazin-3,5(2h,4h)-dionas.
ES2169248T3 (es) Compuestos aromaticos y composiciones farmaceuticas que los contienen.
ES2032381T3 (es) Un compuesto quimico. (reserva del art. 167.2 cpe).
DK1324981T3 (da) Aminopyridinyl-, aminoguanidinyl- og alkoxyguanidinylsubstituerede phenylacetamider som proteaseinhibitorer
AR008291A1 (es) Derivados de tetrahidroisoquinolina, procedimiento para su preparacion, composiciones farmaceuticas que los contienen y su uso para la preparacionde un medicamento.
ES2142030T3 (es) Nuevos compuestos espiro-heterociclicos, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen.
ATE193012T1 (de) Prodrogen von stickstoff-senfen mit neuen lipophilischen schutzgruppen; und verfahren zu ihrer herstellung
TR200200263T2 (tr) Yeni seçiçi retinoid agonistleri
DK39286A (da) Imidazolderivater, fremgangsmaade til fremstilling heraf og farmaceutiske praeparater indeholdende disse derivater
MX9304399A (es) Proceso novedoso para preparar [[2-bromoetil)-amino]metil]-2-nitro-1h-imidazol-1-etanol quiral y compuestos relacionados.
ES452200A1 (es) Un procedimiento para la preparacion de nuevos derivados de pipendina.
EA200100882A1 (ru) Гетероарильные производные амидина, метиламидина и гуанидина (варианты), способ их получения, фармацевтическая композиция (варианты), способ ингибирования протеазы (варианты) и способ лечения различных заболеваний (варианты)

Legal Events

Date Code Title Description
FG2A Definitive protection

Ref document number: 944590

Country of ref document: ES