JP2000500742A - プロテアーゼ阻害剤 - Google Patents

プロテアーゼ阻害剤

Info

Publication number
JP2000500742A
JP2000500742A JP9517638A JP51763897A JP2000500742A JP 2000500742 A JP2000500742 A JP 2000500742A JP 9517638 A JP9517638 A JP 9517638A JP 51763897 A JP51763897 A JP 51763897A JP 2000500742 A JP2000500742 A JP 2000500742A
Authority
JP
Japan
Prior art keywords
leucinyl
alkyl
benzyloxycarbonyl
amino
cbz
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
JP9517638A
Other languages
English (en)
Japanese (ja)
Inventor
カー，トーマス・ジョゼフ
デスジャーレイス，レネー・ルイーズ
ギャラガー，ティモシー・フランシス
ハルバート，ステイシー・マリー
オー，ヒエ−ジャ
トンプソン，スコット・ケビン
ベバー，ダニエル・フランク
ヤマシタ，デニス・シンジ
イェン，ジャック・ウェクオ
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.)
SmithKline Beecham Corp
Original Assignee
SmithKline Beecham Corp
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 SmithKline Beecham Corp filed Critical SmithKline Beecham Corp
Publication of JP2000500742A publication Critical patent/JP2000500742A/ja
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C243/00—Compounds containing chains of nitrogen atoms singly-bound to each other, e.g. hydrazines, triazanes
    • C07C243/24—Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids
    • C07C243/26—Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C243/34—Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of a carbon skeleton further substituted by nitrogen 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
    • 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
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur 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
    • 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
    • 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
    • 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
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D295/14—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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • C07D295/16—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 acylated on ring nitrogen atoms
    • C07D295/20—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 acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/215—Radicals derived from nitrogen analogues of carbonic acid
    • 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
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/91—Dibenzofurans; Hydrogenated dibenzofurans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/34—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/76—Dibenzothiophenes
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6472—Cysteine endopeptidases (3.4.22)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/37—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/573—Immunoassay; Biospecific binding assay; Materials therefor for enzymes or isoenzymes

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Microbiology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • General Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Food Science & Technology (AREA)
  • Cell Biology (AREA)
  • Biophysics (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP9517638A 1995-10-30 1996-10-30 プロテアーゼ阻害剤 Ceased JP2000500742A (ja)

Applications Claiming Priority (21)

Application Number Priority Date Filing Date Title
US810895P 1995-10-30 1995-10-30
US60/008,108 1995-10-30
US747395P 1995-11-22 1995-11-22
US60/007,473 1995-11-22
US899295P 1995-12-21 1995-12-21
US60/008,992 1995-12-21
US1374796P 1996-03-20 1996-03-20
US1374896P 1996-03-20 1996-03-20
US1376496P 1996-03-20 1996-03-20
US60/013,764 1996-03-20
US60/013,747 1996-03-20
US60/013,748 1996-03-20
US1789296P 1996-05-17 1996-05-17
US1745596P 1996-05-17 1996-05-17
US60/017,455 1996-05-17
US60/017,892 1996-05-17
US2204796P 1996-07-22 1996-07-22
US60/022,047 1996-07-22
US2349496P 1996-08-07 1996-08-07
US60/023,494 1996-08-07
PCT/US1996/018000 WO1997016433A1 (en) 1995-10-30 1996-10-30 Protease inhibitors

Publications (1)

Publication Number Publication Date
JP2000500742A true JP2000500742A (ja) 2000-01-25

Family

ID=27580625

Family Applications (1)

Application Number Title Priority Date Filing Date
JP9517638A Ceased JP2000500742A (ja) 1995-10-30 1996-10-30 プロテアーゼ阻害剤

Country Status (17)

Country Link
US (5) US5998470A (2)
EP (1) EP0934291A1 (2)
JP (1) JP2000500742A (2)
KR (1) KR19990067184A (2)
CN (3) CN1341590A (2)
AP (1) AP9801222A0 (2)
AU (1) AU1118097A (2)
BG (1) BG102475A (2)
CZ (1) CZ132798A3 (2)
EA (1) EA199800353A1 (2)
HU (1) HUP9900964A3 (2)
NO (4) NO981938L (2)
OA (1) OA10764A (2)
PL (1) PL326508A1 (2)
SK (1) SK56798A3 (2)
TR (1) TR199800767T2 (2)
WO (1) WO1997016433A1 (2)

Families Citing this family (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5741818A (en) 1995-06-07 1998-04-21 University Of Saskatchewan Semicarbazones having CNS activity and pharmaceutical preparations containing same
US6586466B2 (en) 1995-10-30 2003-07-01 Smithkline Beecham Corporation Carbohydrazide-protease inhibitors
US20020128476A1 (en) * 1996-08-08 2002-09-12 Smithkline Beecham Corporation Inhibitors of cysteine protease
DZ2285A1 (fr) * 1996-08-08 2002-12-25 Smithkline Beecham Corp Inhibiteurs de protéase de la cystéine.
EP0923535A4 (en) * 1996-08-28 2001-01-10 Smithkline Beecham Corp CYSTEINE PROTEASE INHIBITORS
ATE289295T1 (de) * 1997-04-22 2005-03-15 Euro Celtique Sa Die verwendung von durch carbozyklische und heterozyklische reste substituierte semicarbazonen und thiosemicarbazonen als natriumkanalblocker
MA26487A1 (fr) * 1997-04-29 2004-12-20 Smithkline Beecham Corp Heterocyclecetohydrazides inhibiteurs de proteases, procede pour leur preparation et compositions pharmaceutiques les contenant .
EP0983228A4 (en) * 1997-05-08 2002-08-07 Smithkline Beecham Corp PROTEASE INHIBITORS
MA26618A1 (fr) * 1998-04-09 2004-12-20 Smithkline Beecham Corp Composes et compositions pharmaceutiques pour le traitement du paludisme
EP1079821A4 (en) * 1998-05-21 2001-08-29 Smithkline Beecham Corp PROTEASE INHIBITORS
DZ2796A1 (fr) * 1998-05-21 2003-12-01 Smithkline Beecham Corp Composés à fonction bis-aminométhyl-carbonyle nouveaux, procédé pour leur préparation et compositions pharmaceutiques les contenant.
AR018915A1 (es) * 1998-06-24 2001-12-12 Smithkline Beecham Corp Inhibidores de proteasas diacilhidrazinicos, composicion farmaceutica que la comprenden, usos de los mismos para la manufactura de un medicamento, unprocedimiento de fabricacion de dichos compuestos
CA2301201A1 (en) * 1998-08-14 2000-02-24 Smithkline Beecham Corporation Method of inhibiting cathepsin k
BR9913405A (pt) 1998-09-03 2001-10-02 Kyowa Hakko Kogyo Kk Composto heterocìclico que contenha oxigênio, e, inibidor de fosfodiesterase (pde) iv.
EP1126833A4 (en) * 1998-10-29 2004-09-08 Trega Biosciences Inc OXADIAZOLE, THIADIAZOLE AND TRIAZOLE DERIVATIVES AND COMBINATORIAL LIBRARIES CONTAINING THESE DERIVATIVES
US6117870A (en) * 1998-11-12 2000-09-12 Fujirebio Kabushiki Kaisha Cyclic amide derivatives
ES2161594B1 (es) * 1998-12-17 2003-04-01 Servier Lab Nuevos derivados de la hidrazida, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen.
US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
US6562782B1 (en) 1999-05-10 2003-05-13 University Of Rochester Oligocycloalkanoid compounds and methods of use
JP2003513924A (ja) 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション プロテア−ゼ阻害剤
WO2001034600A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
AU1588901A (en) 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
OA12323A (en) 2000-03-21 2006-05-15 Smithkline Beecham Corp Protease inhibitors.
WO2002080920A1 (en) * 2001-04-06 2002-10-17 Axys Pharmaceuticals, Inc. Arylacetamido-ketobenzoxazole as cysteine protease inhibitors
US20040204368A1 (en) * 2001-05-31 2004-10-14 Kazuyuki Ohmoto Oxadiazole derivative compounds and drugs containing these compounds as the active ingredient
US7282512B2 (en) 2002-01-17 2007-10-16 Smithkline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin K inhibitors
WO2003095623A2 (en) * 2002-05-10 2003-11-20 The Trustees Of Columbia University In The City Of New York Genetically engineered cell lines and systems for propagating varicella zoster virus and methods of use thereof
US7101880B2 (en) * 2002-06-24 2006-09-05 Schering Aktiengesellschaft Peptidic compounds as cysteine protease inhibitors
US7056947B2 (en) * 2002-07-05 2006-06-06 Georgia Tech Research Corp. Aza-peptide epoxides
US8013014B2 (en) 2002-07-05 2011-09-06 Georgia Tech Research Corporation Aza-peptide epoxides
AU2003297363A1 (en) * 2002-12-23 2004-07-22 Alcon, Inc. Use of cathepsin k inhibitors for the treatment of glaucoma
US7109243B2 (en) * 2003-03-24 2006-09-19 Irm Llc Inhibitors of cathepsin S
US7384970B2 (en) * 2003-03-24 2008-06-10 Irm Llc Inhibitors of cathepsin S
WO2004106289A1 (en) * 2003-05-30 2004-12-09 Prozymex A/S Protease inhibitors
US7173051B2 (en) * 2003-06-13 2007-02-06 Irm, Llc Inhibitors of cathepsin S
JP2007502831A (ja) * 2003-08-20 2007-02-15 ニトロメッド インコーポレーティッド ニトロソ化およびニトロシル化心血管化合物、組成物、ならびに使用方法
US7256207B2 (en) * 2003-08-20 2007-08-14 Irm Llc Inhibitors of cathepsin S
AU2004270161A1 (en) * 2003-08-28 2005-03-17 Nicox S.A. Nitrosated and nitrosylated cardiovascular compounds, compositions and methods of use
US20090131342A1 (en) * 2004-01-22 2009-05-21 Nitromed, Inc. Nitrosated and/or nitrosylated compounds, compositions and methods of use
GB0412553D0 (en) * 2004-06-04 2004-07-07 Univ Aberdeen Therapeutic agents for the treatment of bone conditions
US8067464B2 (en) 2004-10-04 2011-11-29 Nitromed, Inc. Compositions and methods using apocynin compounds and nitric oxide donors
MX2007007195A (es) 2004-12-20 2007-10-08 Genentech Inc Inhibidores de pirrolidina de iap.
AU2006206249A1 (en) * 2005-01-21 2006-07-27 Nicox S.A. Cardiovascular compounds comprising heterocyclic nitric oxide donor group compositions and methods of use
CA2597422A1 (en) * 2005-02-16 2007-08-02 Nitromed, Inc. Organic nitric oxide donor salts of antimicrobial compounds, compositions and methods of use
WO2006093864A1 (en) * 2005-02-28 2006-09-08 Nitromed, Inc. Cardiovascular compounds comprising nitric oxide enhancing groups, compositions and methods of use
US20090215838A1 (en) * 2005-03-09 2009-08-27 Nitromed, Inc. Organic nitric oxide enhancing salts of angiotensin ii antagonists, compositions and methods of use
EP1883614A4 (en) * 2005-05-23 2010-04-14 Nicox Sa ORGANIC NITRIC OXIDES IMPROVING SALTS FROM NON-SUBSTITUTE INFLAMMATORY COMPOUNDS AND COMPOSITIONS AND USES THEREOF
US20090018091A1 (en) * 2005-08-02 2009-01-15 Nitromed, Inc. Nitric Oxide Enhancing Antimicrobial Compounds, Compositions and Methods of Use
AU2006299383A1 (en) * 2005-10-04 2007-04-12 Nitromed, Inc. Methods for treating respiratory disorders
WO2007059311A2 (en) * 2005-11-16 2007-05-24 Nitromed, Inc. Furoxan compounds, compositions and methods of use
TW201018662A (en) * 2005-12-12 2010-05-16 Astrazeneca Ab Alkylsulphonamide quinolines
WO2007075541A2 (en) * 2005-12-20 2007-07-05 Nitromed, Inc. Nitric oxide enhancing glutamic acid compounds, compositions and methods of use
WO2007075542A2 (en) * 2005-12-22 2007-07-05 Nitromed, Inc. Nitric oxide enhancing pyruvate compounds, compositions and methods of use
CA2647859C (en) 2006-03-29 2016-01-05 Nitromed, Inc. Nitric oxide enhancing prostaglandin compounds, compositions and methods of use
GB0705400D0 (en) 2007-03-21 2007-05-02 Univ Aberdeen Therapeutic compounds andm their use
NZ598890A (en) * 2007-04-30 2013-10-25 Genentech Inc Inhibitors of iap
DK2240506T3 (da) * 2008-01-11 2013-04-08 Genentech Inc IAP inhibitorer
US8835393B2 (en) 2008-08-02 2014-09-16 Genentech, Inc. Inhibitors of IAP
GB0817207D0 (en) 2008-09-19 2008-10-29 Pimco 2664 Ltd therapeutic apsac compounds and their use
GB0817208D0 (en) 2008-09-19 2008-10-29 Pimco 2664 Ltd Therapeutic apsap compounds and their use
BR112015026519A2 (pt) 2013-04-19 2017-07-25 Astrazeneca Ab composto antagonista do receptor nk3 (nk3ra) para uso em um método destinado ao tratamento de síndrome do ovário policístico (sop)
GB201311361D0 (en) 2013-06-26 2013-08-14 Pimco 2664 Ltd Compounds and their therapeutic use
HUE057569T2 (hu) 2014-12-17 2022-05-28 Pimco 2664 Ltd N-(4-hidroxi-4-metil-ciklohexil)-4-fenil-benzolszulfonamid és N-(4-hidroxi-4-metil-ciklohexil)-4-(2-piridil)-benzolszulfonamid vegyületek és terápiás alkalmazásuk
CN105424646B (zh) * 2015-11-05 2018-09-14 湖北瑞昊安科医药科技发展有限公司 一种监控γ-氨基丁酸生物转化过程的系统和方法

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1051084A (2) * 1964-06-25
US4038247A (en) * 1970-05-19 1977-07-26 Ciba-Geigy Corporation Stabilizing polyolefins with diacyl dihydrazides
US5142056A (en) * 1989-05-23 1992-08-25 Abbott Laboratories Retroviral protease inhibiting compounds
US5057525A (en) * 1981-10-01 1991-10-15 Janssen Pharmaceutica N.V. Novel N-(3-hydroxy-4-piperidinyl) benzamide derivatives
IT1195287B (it) * 1981-11-05 1988-10-12 Ausonia Farma Srl Derivato tiazolico,procedimento per la sua preparazione e relative composizioni farmaceutiche
US4518528A (en) * 1983-05-19 1985-05-21 Rasnick David W α Amino fluoro ketones
US4749792A (en) * 1984-09-26 1988-06-07 E. R. Squibb & Sons, Inc. Diamino ketones and alcohols as analgesic agents
US4638010A (en) * 1985-02-28 1987-01-20 E. R. Squibb & Sons, Inc. Ester substituted aminoalkanoylureido amino and imino acid and ester compounds
ZA871860B (en) * 1986-03-14 1988-10-26 Syntex Inc Transglutaminase inhibitors
US5374637A (en) * 1989-03-22 1994-12-20 Janssen Pharmaceutica N.V. N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives
US4994471A (en) * 1989-05-12 1991-02-19 Boc, Inc. N-aryl-N-(1-substituted-3-alkoxy-4-piperidinyl)amides and pharmaceutical compositions and methods employing such compounds
GB9019558D0 (en) * 1990-09-07 1990-10-24 Szelke Michael Enzyme inhibitors
EP0504938A3 (en) * 1991-03-22 1993-04-14 Suntory Limited Prophylactic and therapeutic agent for bone diseases comprising di- or tripeptide derivative as active ingredient
JP3190431B2 (ja) * 1991-07-01 2001-07-23 三菱化学株式会社 ケトン誘導体
JPH05140063A (ja) * 1991-11-19 1993-06-08 Suntory Ltd ジペプチド誘導体及びそれを有効成分とする骨疾患の予防及び治療剤
US5206251A (en) * 1992-04-01 1993-04-27 G. D. Searle & Co. 2- and 3- amino and azido derivatives of 1,5-iminosugars
US5216168A (en) * 1992-04-01 1993-06-01 G. D. Searle & Co. 2- and 3- amino and azido derivatives of 1,5-iminosugars
AU4544993A (en) * 1992-06-24 1994-01-24 Cortex Pharmaceuticals, Inc. Use of calpain inhibitors in the inhibition and treatment of medical conditions associated with increased calpain activity
US5374623A (en) * 1992-08-20 1994-12-20 Prototek, Inc. Cysteine protease inhibitors effective for in vivo use
DK0603769T3 (da) * 1992-12-25 1999-06-14 Mitsubishi Chem Corp Alfa-aminoketonderivater
CA2111930A1 (en) * 1992-12-25 1994-06-26 Ryoichi Ando Aminoketone derivatives
JPH06199850A (ja) * 1992-12-28 1994-07-19 Tanabe Seiyaku Co Ltd インドール含有ペプチド及びその製法
JP2848232B2 (ja) * 1993-02-19 1999-01-20 武田薬品工業株式会社 アルデヒド誘導体
EP0693124A1 (en) * 1993-04-06 1996-01-24 Forsyth Dental Infirmary For Children Human osteoclast-specific and -related genes
CA2120648C (en) * 1993-04-22 2004-06-22 Neil H. Nodelman Novel catalyst package for use in rim systems containing acidic additives
CA2122227A1 (en) * 1993-04-29 1994-10-30 Roland E. Dolle Peptide analogs as irreversible interleukin-1.beta. protease inhibitors
WO1995005192A1 (en) 1993-08-13 1995-02-23 Merck & Co., Inc. SUBSTITUTED KETONE DERIVATIVES AS INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME
US5501969A (en) * 1994-03-08 1996-03-26 Human Genome Sciences, Inc. Human osteoclast-derived cathepsin
CA2187451A1 (en) * 1994-04-13 1995-10-26 Shigetoshi Tsubotani Aziridine derivatives, their production and use
US5585387A (en) * 1994-10-07 1996-12-17 Torcan Chemical Ltd. Prepration of cisapride
US6544767B1 (en) * 1994-10-27 2003-04-08 Axys Pharmaceuticals, Inc. Cathespin O2 protease
TW438591B (en) * 1995-06-07 2001-06-07 Arris Pharm Corp Reversible cysteine protease inhibitors
WO1997049668A1 (en) * 1996-06-13 1997-12-31 Smithkline Beecham Corporation Inhibitiors of cysteine protease
AU6333296A (en) * 1996-06-14 1998-01-07 Human Genome Sciences, Inc. Cathepsin k gene
US5861298A (en) * 1996-06-17 1999-01-19 Smithkline Beecham Corporation Cathepsin K gene
DZ2285A1 (fr) * 1996-08-08 2002-12-25 Smithkline Beecham Corp Inhibiteurs de protéase de la cystéine.
EP0923535A4 (en) * 1996-08-28 2001-01-10 Smithkline Beecham Corp CYSTEINE PROTEASE INHIBITORS
US5830850A (en) * 1996-08-28 1998-11-03 Mount Sinai School Of Medicine Of The City Of New York Methods for the treatment of bone resorption disorders, including osteoporosis

Also Published As

Publication number Publication date
PL326508A1 (en) 1998-09-28
NO20006717D0 (no) 2000-12-29
HUP9900964A2 (hu) 1999-07-28
NO20006718D0 (no) 2000-12-29
BG102475A (en) 1999-04-30
NO20006716D0 (no) 2000-12-29
SK56798A3 (en) 1998-12-02
US6331542B1 (en) 2001-12-18
MX9803548A (es) 1998-09-30
US6284777B1 (en) 2001-09-04
CN1341590A (zh) 2002-03-27
NO20006716L (no) 1998-06-29
WO1997016433A1 (en) 1997-05-09
TR199800767T2 (xx) 1998-07-21
CN1341593A (zh) 2002-03-27
OA10764A (en) 2002-12-11
AU1118097A (en) 1997-05-22
NO981938D0 (no) 1998-04-29
NO20006717L (no) 1998-06-29
US6232342B1 (en) 2001-05-15
AP9801222A0 (en) 1998-06-30
CN1341592A (zh) 2002-03-27
EP0934291A1 (en) 1999-08-11
KR19990067184A (ko) 1999-08-16
EP0934291A4 (2) 1999-08-11
US5998470A (en) 1999-12-07
EA199800353A1 (ru) 1998-12-24
US6057362A (en) 2000-05-02
CZ132798A3 (cs) 1999-02-17
NO20006718L (no) 1998-06-29
NO981938L (no) 1998-06-29
HUP9900964A3 (en) 2001-02-28

Similar Documents

Publication Publication Date Title
US6232342B1 (en) Protease inhibitors
JPH08500825A (ja) レトロウイルスプロテアーゼ阻害剤として有用なスルホニルアルカノイルアミノヒドロキシエチルアミノスルホンアミド
US5583132A (en) Sulfonylalkanoylamino hydroxyethylamino sulfamic acids useful as retroviral protease inhibitors
CA2327282A1 (en) Treatment of parasitic diseases by inhibition of cysteine proteases of the papain superfamily
JP2002513408A (ja) チオールスルホンアミドヒドロキサム酸化合物
KR20010020391A (ko) 프로테아제 억제제
HUT75059A (en) Metalloproteinase inhibitors, pharmaceutical compns. contg. them and process for preparing the said compds.
US5747535A (en) Selective thrombin inhibitors
JPH08504815A (ja) 環状スルホン含有レトロウイルスプロテアーゼ阻害物質
JPH08500824A (ja) レトロウイルスプロテアーゼ阻害剤として有用なｎ−（アルカノイルアミノ−２−ヒドロキシプロピル）スルホンアミド
KR20010012325A (ko) 프로테아제 억제제
JP2000053664A (ja) チアゾ―ル誘導体
JP2002515428A (ja) プロテアーゼ阻害剤
US20020049316A1 (en) Protease inhibitors
US6562842B2 (en) Protease inhibitors
CN101128433A (zh) 作为钙蛋白酶抑制剂的异喹啉衍生物
RU2136657C1 (ru) Производные гидроксамовой или карбоновой кислоты и фармацевтическая или ветеринарная композиция на их основе
WO1998046582A1 (en) Protease inhibitors
JP2004143053A (ja) β−アミノヒドロキサム酸誘導体およびその用途
US5756498A (en) Sulfonylalkanoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
AU2259100A (en) Protease inhibitors - I
AU2260500A (en) Protease inhibitors - III
CA2236111A1 (en) Protease inhibitors
MXPA98003548A (en) Prote inhibitors
KR100472914B1 (ko) 혈관형성억제제

Legal Events

Date Code Title Description
A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20070724

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

Free format text: JAPANESE INTERMEDIATE CODE: A313

Effective date: 20071219

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20080129