IS2334B - Aspartyl próteasi hemjari af nýjum flokki súlfonamíða - Google Patents

Aspartyl próteasi hemjari af nýjum flokki súlfonamíða

Info

Publication number
IS2334B
IS2334B IS4068A IS4068A IS2334B IS 2334 B IS2334 B IS 2334B IS 4068 A IS4068 A IS 4068A IS 4068 A IS4068 A IS 4068A IS 2334 B IS2334 B IS 2334B
Authority
IS
Iceland
Prior art keywords
sulfonamides
protease inhibitor
new class
aspartyl protease
aspartyl
Prior art date
Application number
IS4068A
Other languages
English (en)
Icelandic (is)
Other versions
IS4068A (is
Inventor
D. Tung Rogert
A. Murcko Mark
Rao Bhisetti Govinda
Original Assignee
Vertex Pharmaceuticals Inc., (A Massachusetts Corporation)
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 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) filed Critical Vertex Pharmaceuticals Inc., (A Massachusetts Corporation)
Publication of IS4068A publication Critical patent/IS4068A/is
Publication of IS2334B publication Critical patent/IS2334B/is

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C307/00—Amides of sulfuric acids, i.e. compounds having singly-bound oxygen atoms of sulfate groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C307/04—Diamides of sulfuric acids
    • C07C307/06—Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon 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
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
    • C07C311/13—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
    • 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
    • C07C311/22—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
    • 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
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C07C311/38—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
    • C07C311/39—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton 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
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/46—Y being a hydrogen or a carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • 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
    • 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
    • C07D213/78—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
    • 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
    • C07D215/38—Nitrogen atoms
    • 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
    • C07D215/48—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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole 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
    • 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
    • C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/24—Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other 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
    • C07D271/08—1,2,5-Oxadiazoles; Hydrogenated 1,2,5-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
    • C07D277/36—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
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/10—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/12—Radicals substituted by oxygen 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
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/20—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • 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
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • 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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Genetics & Genomics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Oncology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Communicable Diseases (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Quinoline Compounds (AREA)
  • Furan Compounds (AREA)
  • Indole Compounds (AREA)
  • Peptides Or Proteins (AREA)
IS4068A 1992-09-08 1993-08-31 Aspartyl próteasi hemjari af nýjum flokki súlfonamíða IS2334B (is)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US94198292A 1992-09-08 1992-09-08

Publications (2)

Publication Number Publication Date
IS4068A IS4068A (is) 1994-03-09
IS2334B true IS2334B (is) 2008-02-15

Family

ID=25477403

Family Applications (1)

Application Number Title Priority Date Filing Date
IS4068A IS2334B (is) 1992-09-08 1993-08-31 Aspartyl próteasi hemjari af nýjum flokki súlfonamíða

Country Status (40)

Country Link
US (7) US5585397A (forum.php)
EP (2) EP0885887B1 (forum.php)
JP (1) JP3012002B2 (forum.php)
KR (1) KR100262056B1 (forum.php)
CN (1) CN1061339C (forum.php)
AP (1) AP390A (forum.php)
AT (2) ATE241602T1 (forum.php)
AU (1) AU691160B2 (forum.php)
BG (1) BG62488B1 (forum.php)
BR (1) BR1100824A (forum.php)
CA (1) CA2143208C (forum.php)
CO (1) CO4870779A1 (forum.php)
CY (1) CY2164B1 (forum.php)
CZ (1) CZ289475B6 (forum.php)
DE (3) DE69324369T2 (forum.php)
DK (2) DK0659181T3 (forum.php)
ES (2) ES2200243T3 (forum.php)
FI (1) FI120685B (forum.php)
GE (1) GEP20012579B (forum.php)
GR (1) GR3030719T3 (forum.php)
HU (1) HU228198B1 (forum.php)
IL (1) IL106927A (forum.php)
IS (1) IS2334B (forum.php)
LT (1) LT3302B (forum.php)
LU (1) LU90736I2 (forum.php)
MX (1) MXPA03010538A (forum.php)
MY (1) MY142901A (forum.php)
NL (1) NL300039I2 (forum.php)
NO (2) NO303444B1 (forum.php)
NZ (2) NZ314376A (forum.php)
PH (1) PH31251A (forum.php)
PL (1) PL185635B1 (forum.php)
PT (1) PT885887E (forum.php)
RO (1) RO118747B1 (forum.php)
RU (1) RU2135496C1 (forum.php)
SG (1) SG43862A1 (forum.php)
SK (1) SK281360B6 (forum.php)
TW (1) TW254927B (forum.php)
UA (1) UA44694C2 (forum.php)
WO (1) WO1994005639A1 (forum.php)

Families Citing this family (305)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040122000A1 (en) 1981-01-07 2004-06-24 Vertex Pharmaceuticals Incorporated. Inhibitors of aspartyl protease
US6878728B1 (en) 1999-06-11 2005-04-12 Vertex Pharmaceutical Incorporated Inhibitors of aspartyl protease
US5962490A (en) 1987-09-25 1999-10-05 Texas Biotechnology Corporation Thienyl-, furyl- and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin
US5736509A (en) * 1990-12-14 1998-04-07 Texas Biotechnology Corporation Cyclic peptide surface feature mimics of endothelin
US5642292A (en) * 1992-03-27 1997-06-24 Akiko Itai Methods for searching stable docking models of biopolymer-ligand molecule complex
US6743929B1 (en) * 1992-08-25 2004-06-01 G. D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US7141609B2 (en) * 1992-08-25 2006-11-28 G.D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US5968942A (en) 1992-08-25 1999-10-19 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US6046190A (en) * 1992-08-25 2000-04-04 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
CA2140929C (en) * 1992-08-25 2006-09-12 Michael L. Vazquez Hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
US5783701A (en) * 1992-09-08 1998-07-21 Vertex Pharmaceuticals, Incorporated Sulfonamide inhibitors of aspartyl protease
EP0885880A3 (en) * 1992-10-30 1999-10-06 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfamic acids useful as retroviral protease inhibitors
EP0666842B1 (en) 1992-10-30 1998-06-24 G.D. Searle & Co. Hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors
US5846993A (en) * 1992-12-22 1998-12-08 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US5484926A (en) * 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US6342610B2 (en) 1993-05-20 2002-01-29 Texas Biotechnology Corp. N-aryl thienyl-, furyl-, and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin
US6030991A (en) * 1993-05-20 2000-02-29 Texas Biotechnology Corp. Benzenesulfonamides and the use thereof to modulate the activity of endothelin
US6376523B1 (en) 1994-05-20 2002-04-23 Texas Biotechnology Corporation Benzenesulfonamides and the use thereof to modulate the activity of endothelin
US6613804B2 (en) 1993-05-20 2003-09-02 Encysive Pharmaceuticals, Inc. Biphenylsulfonamides and derivatives thereof that modulate the activity of endothelin
US6541498B2 (en) 1993-05-20 2003-04-01 Texas Biotechnology Benzenesulfonamides and the use thereof to modulate the activity of endothelin
US5798355A (en) * 1995-06-07 1998-08-25 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity
US5846981A (en) * 1993-05-28 1998-12-08 Gpi Nil Holdings Inc. Inhibitors of rotamase enzyme activity
US7831470B1 (en) * 1996-09-04 2010-11-09 Walker Digital, Llc Method and apparatus for facilitating electronic commerce through providing cross-benefits during a transaction
US5750648A (en) * 1993-08-20 1998-05-12 G.D. Searle & Co. Retroviral protease inhibitors and combinations thereof
IL110752A (en) * 1993-09-13 2000-07-26 Abbott Lab Liquid semi-solid or solid pharmaceutical composition for an HIV protease inhibitor
US5559158A (en) * 1993-10-01 1996-09-24 Abbott Laboratories Pharmaceutical composition
US5602119A (en) * 1993-10-29 1997-02-11 Vazquez; Michael L. Succinoylamino hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors
US5527829A (en) * 1994-05-23 1996-06-18 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US20030207813A1 (en) * 1996-12-09 2003-11-06 G.D. Searle Retroviral protease inhibitor combinations
UA49803C2 (uk) * 1994-06-03 2002-10-15 Дж.Д. Сьорль Енд Ко Спосіб лікування ретровірусних інфекцій
US5831117A (en) 1995-01-20 1998-11-03 G. D. Searle & Co. Method of preparing retroviral protease inhibitor intermediates
WO1996022287A1 (en) * 1995-01-20 1996-07-25 G.D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
US5756533A (en) * 1995-03-10 1998-05-26 G.D. Searle & Co. Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6140505A (en) 1995-03-10 2000-10-31 G. D. Searle & Co. Synthesis of benzo fused heterocyclic sulfonyl chlorides
US6407134B1 (en) 1995-03-10 2002-06-18 G. D. Searle & Co. Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US7339078B2 (en) * 1995-03-10 2008-03-04 G.D. Searle Llc Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US5776971A (en) 1995-03-10 1998-07-07 G.D. Searle & Co. Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6143788A (en) * 1995-03-10 2000-11-07 G.D. Searle & Co. Bis-amino acid hydroxyethlamino sulfonamide retroviral protease inhibitors
EP1188766A1 (en) 1995-03-10 2002-03-20 G.D. Searle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
DE69625183T2 (de) * 1995-03-10 2003-10-09 G.D. Searle & Co., Chicago Heterocyclocarbonyl-aminosäure-hydroxyethylamino-sulfonamid inhibitoren retroviraler proteasen
US6861539B1 (en) * 1995-03-10 2005-03-01 G. D. Searle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6150556A (en) * 1995-03-10 2000-11-21 G. D. Dearle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US5691372A (en) * 1995-04-19 1997-11-25 Vertex Pharmaceuticals Incorporated Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease
US5859031A (en) * 1995-06-07 1999-01-12 Gpi Nil Holdings, Inc. Small molecule inhibitors of rotamase enzyme activity
US5696135A (en) * 1995-06-07 1997-12-09 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity effective at stimulating neuronal growth
US6037157A (en) 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
US5942253A (en) 1995-10-12 1999-08-24 Immunex Corporation Prolonged release of GM-CSF
US5801197A (en) * 1995-10-31 1998-09-01 Gpi Nil Holdings, Inc. Rotamase enzyme activity inhibitors
DE69619067T2 (de) 1995-11-17 2002-10-02 Ajinomoto Co., Inc. Verfahren zur Herstellung von 3-Amino-2-oxo-1-Halogenpropan-Derivaten
US5646180A (en) * 1995-12-05 1997-07-08 Vertex Pharmaceuticals Incorporated Treatment of the CNS effects of HIV
US5914332A (en) 1995-12-13 1999-06-22 Abbott Laboratories Retroviral protease inhibiting compounds
US5977117A (en) * 1996-01-05 1999-11-02 Texas Biotechnology Corporation Substituted phenyl compounds and derivatives thereof that modulate the activity of endothelin
US6730679B1 (en) 1996-03-22 2004-05-04 Smithkline Beecham Corporation Pharmaceutical formulations
MY126358A (en) * 1996-03-22 2006-09-29 Glaxo Group Ltd Compositions comprising vx478 and a water soluble tocopherol derivative such as vitamin e-tpgs
EA001484B1 (ru) * 1996-03-22 2001-04-23 Глаксо Груп Лимитед Композиции, содержащие ингибитор вич протеазы, а именно as vx 478, и водорастворимое соединение витамина e, а именно витамин e-tpgs
US5958905A (en) * 1996-03-26 1999-09-28 Texas Biotechnology Corporation Phosphoramidates, phosphinic amides and related compounds and the use thereof to modulate the activity of endothelin
US5804585A (en) 1996-04-15 1998-09-08 Texas Biotechnology Corporation Thieno-pyridine sulfonamides derivatives thereof and related compounds that modulate the activity of endothelin
ZA975565B (en) * 1996-06-25 1998-12-23 Glaxo Group Ltd Antiviral combinations
DE69727240T2 (de) * 1996-06-25 2004-11-25 Glaxo Group Ltd., Greenford Kombinationen, enthaltend VX478, Zidovudin und 3TC zur Behandlung von HIV
US5962725A (en) 1996-09-05 1999-10-05 Agouron Pharmaceuticals, Inc. Intermediate compounds useful for making HIV protease inhibitors such as nelfinavir
US5705647A (en) * 1996-09-05 1998-01-06 Agouron Pharmaceuticals, Inc. Intermediates for making HIV-protease inhibitors
US5925759A (en) * 1996-09-05 1999-07-20 Agouron Pharmaceuticals, Inc. Methods of making HIV-protease inhibitors and intermediates for making HIV-protease inhibitors
US6218424B1 (en) 1996-09-25 2001-04-17 Gpi Nil Holdings, Inc. Heterocyclic ketone and thioester compounds and uses
US5786378A (en) * 1996-09-25 1998-07-28 Gpi Nil Holdings, Inc. Heterocyclic thioesters
US5801187A (en) 1996-09-25 1998-09-01 Gpi-Nil Holdings, Inc. Heterocyclic esters and amides
IN183408B (forum.php) * 1996-11-20 1999-12-25 Kuraray Co
ZA9710071B (en) * 1996-11-21 1998-05-25 Abbott Lab Pharmaceutical composition.
US6232333B1 (en) 1996-11-21 2001-05-15 Abbott Laboratories Pharmaceutical composition
US5874449A (en) * 1996-12-31 1999-02-23 Gpi Nil Holdings, Inc. N-linked sulfonamides of heterocyclic thioesters
US6121273A (en) * 1996-12-31 2000-09-19 Gpi Nil Holdings, Inc N-linked sulfonamides of heterocyclic thioesters
US5958949A (en) * 1996-12-31 1999-09-28 Gpi Nil Holdings Inc. N-linked ureas and carbamates of piperidyl thioesters
US5935989A (en) * 1996-12-31 1999-08-10 Gpi Nil Holdings Inc. N-linked ureas and carbamates of heterocyclic thioesters
US5721256A (en) 1997-02-12 1998-02-24 Gpi Nil Holdings, Inc. Method of using neurotrophic sulfonamide compounds
US5846979A (en) 1997-02-28 1998-12-08 Gpi Nil Holdings, Inc. N-oxides of heterocyclic esters, amides, thioesters, and ketones
US6001851A (en) * 1997-03-13 1999-12-14 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US5783705A (en) * 1997-04-28 1998-07-21 Texas Biotechnology Corporation Process of preparing alkali metal salys of hydrophobic sulfonamides
JP3455233B2 (ja) 1997-04-28 2003-10-14 テキサス・バイオテクノロジー・コーポレイシヨン エンドテリン介在障害治療用のスルホンアミド類
JP2002512621A (ja) * 1997-05-08 2002-04-23 スミスクライン・ビーチャム・コーポレイション プロテアーゼ阻害剤
US5945441A (en) 1997-06-04 1999-08-31 Gpi Nil Holdings, Inc. Pyrrolidine carboxylate hair revitalizing agents
US6271244B1 (en) 1998-06-03 2001-08-07 Gpi Nil Holdings, Inc. N-linked urea or carbamate of heterocyclic thioester hair growth compositions and uses
US6187796B1 (en) 1998-06-03 2001-02-13 Gpi Nil Holdings, Inc. Sulfone hair growth compositions and uses
US6187784B1 (en) 1998-06-03 2001-02-13 Gpi Nil Holdings, Inc. Pipecolic acid derivative hair growth compositions and uses
US6274602B1 (en) 1998-06-03 2001-08-14 Gpi Nil Holdings, Inc. Heterocyclic thioester and ketone hair growth compositions and uses
US20010049381A1 (en) 1997-06-04 2001-12-06 Gpl Nil Holdings, Inc., Pyrrolidine derivative hair growth compositions and uses
GB9712253D0 (en) * 1997-06-13 1997-08-13 Glaxo Group Ltd Antiviral compound
AU745081B2 (en) 1997-06-27 2002-03-14 Fujisawa Pharmaceutical Co., Ltd. Sulfonamide compounds and medicinal use thereof
US6084107A (en) * 1997-09-05 2000-07-04 Agouron Pharmaceuticals, Inc. Intermediates for making HIV-protease inhibitors
US6576231B2 (en) * 1997-09-12 2003-06-10 Schering Ag Methods for treating HIV-Infected Patients by the Administration of GM-CSF and a protease inhibitor
US6180634B1 (en) * 1997-11-13 2001-01-30 Merck & Co., Inc. Combination therapy for the treatment of AIDS
AP2000001856A0 (en) * 1997-12-24 2000-09-30 Vertex Pharma Prodrugs of aspartyl protease inhibitors.
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
AU2012199A (en) * 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
WO1999033792A2 (en) * 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs os aspartyl protease inhibitors
GB9805898D0 (en) * 1998-03-20 1998-05-13 Glaxo Group Ltd Process for the sythesis of hiv protease inhibitors
US6251906B1 (en) 1998-05-15 2001-06-26 Abbott Laboratories Retroviral protease inhibiting compounds
US6172087B1 (en) 1998-06-03 2001-01-09 Gpi Nil Holding, Inc. N-oxide of heterocyclic ester, amide, thioester, or ketone hair growth compositions and uses
BR9815882A (pt) 1998-06-03 2002-09-17 Gpi Nil Holding Inc Sulfonamidas ligadas por n de ácido carboxìlicos n-heterocìclicos ouou de isósteros de ácidos carboxìlicos
US6331537B1 (en) 1998-06-03 2001-12-18 Gpi Nil Holdings, Inc. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds
EP1085853A1 (en) 1998-06-03 2001-03-28 GPI NIL Holdings, Inc. Heterocyclic ester and amide hair growth compositions and uses
WO1999065870A2 (en) 1998-06-19 1999-12-23 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of aspartyl protease
CA2872424C (en) 1998-06-23 2017-03-07 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Bisfuran derivatives useful in preventing the emergence of multidrug resistant hiv strains and treatment of hiv
US6538006B1 (en) 1998-07-08 2003-03-25 Pharmacia Corporation Retroviral protease inhibitors
US6713290B2 (en) 1998-07-24 2004-03-30 Samsung Fine Chemicals Co., Ltd. Process for preparing optically pure (S)-3-hydroxy-γ-butyrolactone
AU5067899A (en) 1998-07-24 2000-02-14 Samsung Fine Chemicals Co., Ltd. Process for preparing alpha-(1,4) linked oligosaccharide
US6384056B1 (en) 1998-08-14 2002-05-07 Gpi Nil Holdings, Inc. Heterocyclic thioesters or ketones for vision and memory disorders
US6376517B1 (en) 1998-08-14 2002-04-23 Gpi Nil Holdings, Inc. Pipecolic acid derivatives for vision and memory disorders
US7338976B1 (en) 1998-08-14 2008-03-04 Gpi Nil Holdings, Inc. Heterocyclic esters or amides for vision and memory disorders
US6506788B1 (en) 1998-08-14 2003-01-14 Gpi Nil Holdings, Inc. N-linked urea or carbamate of heterocyclic thioesters for vision and memory disorders
US6399648B1 (en) 1998-08-14 2002-06-04 Gpi Nil Holdings, Inc. N-oxides of heterocyclic ester, amide, thioester, or ketone for vision and memory disorders
US6333340B1 (en) 1998-08-14 2001-12-25 Gpi Nil Holdings, Inc. Small molecule sulfonamides for vision and memory disorders
US6337340B1 (en) 1998-08-14 2002-01-08 Gpi Nil Holdings, Inc. Carboxylic acids and isosteres of heterocyclic ring compounds having multiple heteroatoms for vision and memory disorders
US6335348B1 (en) 1998-08-14 2002-01-01 Gpi Nil Holdings, Inc. Nitrogen-containing linear and azepinyl/ compositions and uses for vision and memory disorders
US6218423B1 (en) 1998-08-14 2001-04-17 Gpi Nil Holdings, Inc. Pyrrolidine derivatives for vision and memory disorders
US6395758B1 (en) 1998-08-14 2002-05-28 Gpi Nil Holdings, Inc. Small molecule carbamates or ureas for vision and memory disorders
US6339101B1 (en) 1998-08-14 2002-01-15 Gpi Nil Holdings, Inc. N-linked sulfonamides of N-heterocyclic carboxylic acids or isosteres for vision and memory disorders
US6462072B1 (en) 1998-09-21 2002-10-08 Gpi Nil Holdings, Inc. Cyclic ester or amide derivatives
US7635690B2 (en) * 1999-01-22 2009-12-22 Emory University HIV-1 mutations selected for by β-2′,3′-didehydro-2′,3′-dideoxy-5-fluorocytidine
US7115584B2 (en) * 1999-01-22 2006-10-03 Emory University HIV-1 mutations selected for by β-2′,3′-didehydro-2′,3′-dideoxy-5-fluorocytidine
CO5261510A1 (es) 1999-02-12 2003-03-31 Vertex Pharma Inhibidores de aspartil proteasa
ES2254156T3 (es) * 1999-02-12 2006-06-16 Vertex Pharmaceuticals Incorporated Inhibidores de aspartil-proteasa.
AR031520A1 (es) * 1999-06-11 2003-09-24 Vertex Pharma Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion
GB9914821D0 (en) * 1999-06-24 1999-08-25 Glaxo Group Ltd Compounds
CZ300031B6 (cs) * 1999-10-06 2009-01-14 Tibotec Pharmaceuticals Ltd. Hexahydrofuro[2,3-b]furan-3-yl-N-{3-[(1,3-benzodioxol-5-ylsulfonyl) (isobutyl)amino]-1-benzyl-2-hydroxypropyl}karbamát a farmaceutický prípravek s jeho obsahem
US6548706B2 (en) 1999-12-23 2003-04-15 Aerojet Fine Chemicals Llc Preparation of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl) -p-nitrobenzenesulfonylamide hydrochloride and other derivatives of 2-hydroxy-1,3-diamines
WO2001046120A1 (en) 1999-12-23 2001-06-28 Aerojet Fine Chemicals Llc Improved preparation of 2s,3s-n-isobutyl-n-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride and other derivatives of 2-hydroxy-1,3-diamines
US6391919B1 (en) 2000-01-12 2002-05-21 Bristol-Myers Squibb Pharma Company Bis-amino acid sulfonamides containing substituted benzyl amines HIV protease inhibitors
KR100861885B1 (ko) 2000-01-19 2008-10-09 아보트 러보러터리즈 개선된 약제학적 조성물
PE20020276A1 (es) * 2000-06-30 2002-04-06 Elan Pharm Inc COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER
US6617310B2 (en) 2000-07-19 2003-09-09 Bristol-Myers Squibb Pharma Company Phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines
WO2003079972A2 (en) 2002-02-22 2003-10-02 New River Parmaceuticals Inc. Active agent delivery systems and methods for protecting and administering active agents
HRP20030735B1 (en) 2001-02-14 2012-02-29 Tibotec Pharmaceuticals Ltd. Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors
US6756063B2 (en) 2001-03-29 2004-06-29 Zoltan Laboratories, Llc Methods and compositions for the treatment of human and animal cancers
HRP20030905B1 (en) * 2001-04-09 2012-03-31 Tibotec Pharmaceuticals Ltd. Broadspectrum 2-(substituted-amino)-benzoxazole sulfonamide hiv protease inhibitors
US6696494B2 (en) 2001-10-22 2004-02-24 Enanta Pharmaceuticals, Inc. α-hydroxyarylbutanamine inhibitors of aspartyl protease
US7109230B2 (en) * 2002-01-07 2006-09-19 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
US7157489B2 (en) * 2002-03-12 2007-01-02 The Board Of Trustees Of The University Of Illinois HIV protease inhibitors
JP2006508634A (ja) 2002-04-26 2006-03-16 ギリアード サイエンシーズ， インコーポレイテッド 抗ｈｉｖ治療化合物を同定するための方法および組成物
TWI356700B (en) * 2002-05-17 2012-01-21 Tibotec Pharm Ltd Broadspectrum substituted benzisoxazole sulfonamid
CA2489095A1 (en) * 2002-06-17 2003-12-24 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
US7115652B2 (en) * 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
NZ538714A (en) * 2002-08-14 2007-03-30 Tibotec Pharm Ltd Broadspectrum substituted oxindole sulfonamide HIV protease inhibitors
UY27967A1 (es) * 2002-09-10 2004-05-31 Pfizer Acetil 2-hindroxi-1,3-diaminoalcanos
SI1546088T1 (sl) * 2002-10-03 2015-04-30 Novaremed Ltd. Spojine za uporabo v zdravljenju avtoimunskih bolezni, imunoalergijskih bolezni in zavrnitve transpalantata organa ali tkiva
US6713639B1 (en) 2002-10-28 2004-03-30 Council Of Scientific And Industrial Research Process for preparing enantiomerically pure (S)-3-hydroxy-gamma-butyrolactone
AU2003291308B2 (en) 2002-11-12 2009-06-18 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
US7351738B2 (en) * 2002-11-27 2008-04-01 Elan Pharmaceuticals, Inc. Substituted ureas and carbamates
US20090247488A1 (en) * 2003-04-25 2009-10-01 Carina Cannizzaro Anti-inflammatory phosphonate compounds
EA200501676A1 (ru) 2003-04-25 2006-04-28 Джилид Сайэнс, Инк. Фосфонатсодержащие ингибиторы киназы (варианты), способ их получения, фармацевтическая композиция, лекарственная форма на их основе и способ ингибирования киназы у млекопитающего (варианты)
WO2005002626A2 (en) * 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
US7407965B2 (en) * 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
CN101410120A (zh) * 2003-04-25 2009-04-15 吉里德科学公司 抗炎的膦酸酯化合物
US7452901B2 (en) 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
US7300924B2 (en) * 2003-04-25 2007-11-27 Gilead Sciences, Inc. Anti-infective phosphonate analogs
WO2004096287A2 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
US20050261237A1 (en) * 2003-04-25 2005-11-24 Boojamra Constantine G Nucleoside phosphonate analogs
US7432261B2 (en) * 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
CA2523083C (en) 2003-04-25 2014-07-08 Gilead Sciences, Inc. Antiviral phosphonate analogs
US7470724B2 (en) * 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
US8025899B2 (en) 2003-08-28 2011-09-27 Abbott Laboratories Solid pharmaceutical dosage form
US8377952B2 (en) 2003-08-28 2013-02-19 Abbott Laboratories Solid pharmaceutical dosage formulation
US7300953B2 (en) 2003-09-19 2007-11-27 Ube Industries, Ltd Process for preparing nitrile compound, carboxylic acid compound or carboxylic acid ester compound
CN100432038C (zh) * 2003-09-19 2008-11-12 宇部兴产株式会社 腈化合物、羧酸化合物或羧酸酯化合物的制备方法
WO2005044308A1 (en) * 2003-10-24 2005-05-19 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
WO2005044279A1 (en) * 2003-10-24 2005-05-19 Gilead Sciences, Inc. Purine nucleoside phosphonate conjugates
US20050131042A1 (en) * 2003-12-11 2005-06-16 Flentge Charles A. HIV protease inhibiting compounds
US8193227B2 (en) 2003-12-11 2012-06-05 Abbott Laboratories HIV protease inhibiting compounds
US20070281907A1 (en) * 2003-12-22 2007-12-06 Watkins William J Kinase Inhibitor Phosphonate Conjugates
EP1706405B1 (en) * 2003-12-22 2009-03-04 Gilead Sciences, Inc. 4'-substituted carbovir- and abacavir-derivatives as well as related compounds with hiv and hcv antiviral activity
US20050153990A1 (en) * 2003-12-22 2005-07-14 Watkins William J. Phosphonate substituted kinase inhibitors
UA85567C2 (en) 2003-12-23 2009-02-10 Тиботек Фармасьютикелз Лтд. Process for the preparation of (3r,3as,6ar)-hexahydrofuro [2,3-b] furan-3-yl (1s,2r)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate
US7200207B2 (en) * 2004-03-13 2007-04-03 Intrado Inc. Communication network for providing emergency services
EP1750691B1 (en) * 2004-03-26 2016-08-10 Novaremed Ltd. Compounds for treatment of aids and other diseases
EP2258376B1 (en) 2004-07-27 2019-02-27 Gilead Sciences, Inc. Phosphonate analogs of HIV inhibitor compounds
US20060135510A1 (en) * 2004-10-13 2006-06-22 The Trustees Of The University Of Pennsylvania Use of amprenavir as a radiation sensitizer
US20060116397A1 (en) * 2004-10-13 2006-06-01 The Trustees Of The University Of Pennsylvania Use of saquinavir as a radiation sensitizer
CA2588517A1 (en) 2004-12-01 2006-06-08 Devgen N.V. 5-carboxamido substituted thiazole derivatives that interact with ion channels, in particular with ion channels from the kv family
EP1938691A3 (en) 2004-12-17 2009-07-22 Devgen NV Nematicidal compositions
US20080194554A1 (en) * 2005-03-11 2008-08-14 Mclean Ed W Hiv Protease Inhibitors
US20080009517A1 (en) * 2005-10-13 2008-01-10 The Trustees Of The University Of Pennsylvania Use of nelfinavir as a radiation sensitizer
ES2542344T3 (es) * 2006-05-09 2015-08-04 Novaremed Ltd. Uso de inhibidores de tirosina cinasa Syk para el tratamiento de trastornos proliferativos celulares
KR101518079B1 (ko) 2007-03-12 2015-05-06 넥타르 테라퓨틱스 올리고머-프로테아제 억제제 컨주게이트
PL2152667T3 (pl) 2007-04-27 2011-06-30 Tibotec Pharm Ltd Sposoby wytwarzania pochodnych N-izobutylo-N-(2-hydroksy-3-amino-4-fenylo-butylo)-p-nitrobenzenosulfonyloamidu
US20090075942A1 (en) * 2007-09-13 2009-03-19 Protia, Llc Deuterium-enriched fosamprenavir
GB2452952A (en) * 2007-09-20 2009-03-25 Npil Pharmaceuticals N-[2-Hydroxy-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-sulphonamide derivatives via N-[2-oxo-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-imine skeleton
US20100093811A1 (en) * 2007-09-25 2010-04-15 Coburn Craig A Hiv protease inhibitors
GB0804213D0 (en) * 2008-03-06 2008-04-16 New Era Biotech Ltd A method of printing or preventing pain
EP2262538B1 (en) * 2008-03-12 2014-12-10 Nektar Therapeutics Oligomer-amino acid conjugate
EP2116236A1 (en) 2008-04-21 2009-11-11 Université de Mons-Hainaut Bisbenzamidine derivatives for use as antioxidant
WO2009148052A1 (ja) * 2008-06-05 2009-12-10 旭化成ファーマ株式会社 スルホンアミド化合物及びその用途
EP2307345A4 (en) * 2008-07-01 2012-05-02 Purdue Research Foundation NON-PEPTIDINHIBITORS OF HIV-1 PROTEASE
PE20110219A1 (es) * 2008-07-08 2011-03-31 Gilead Sciences Inc Sales del compuesto n-[(s)({[(2r,5r)-5-(6-amino-9h-purin-9-il)-4-fluoro-2,5-dihidrofuran-2-il]oxi}metil)fenoxifosfinoil]-l-alaninato de etilo como inhibidores de vih
US8497383B2 (en) 2009-05-27 2013-07-30 Merck Sharp & Dohme Corp. HIV protease inhibitors
US20120108501A1 (en) 2009-06-12 2012-05-03 Nektar Therapeutics Protease Inhibitors
US8802734B2 (en) * 2009-09-09 2014-08-12 Novaremed Limited Method of treating or preventing pain
WO2011061590A1 (en) 2009-11-17 2011-05-26 Hetero Research Foundation Novel carboxamide derivatives as hiv inhibitors
DE102010004957A1 (de) 2010-01-14 2011-07-21 Universitätsklinikum Jena, 07743 Biologisch wirksame Moleküle zur Beeinflussung von Virus-, Bakterien-, Parasiten-infizierten Zellen und/oder Tumorzellen und Verfahren zu deren Anwendung
US20120328568A1 (en) 2010-02-12 2012-12-27 Emory University Compositions and uses of lectins
NZ602191A (en) 2010-03-02 2014-07-25 Amakem Nv Heterocyclic amides as rock inhibitors
CN102190638A (zh) * 2010-03-16 2011-09-21 中国科学院上海药物研究所 联芳基醇二胺类化合物、其药物组合物、制备方法及应用
WO2011156594A2 (en) 2010-06-09 2011-12-15 Vaccine Technologies, Incorporated Therapeutic immunization in hiv infected subjects receiving stable antiretroviral treatment
JP2013533239A (ja) 2010-06-25 2013-08-22 ファキュルテ ユニヴェルシテール ノートル−ダム ド ラ ペ 増殖性疾患の治療に有用なβカルボリン誘導体
US8785648B1 (en) 2010-08-10 2014-07-22 The Regents Of The University Of California PKC-epsilon inhibitors
CN103153352B (zh) 2010-08-18 2015-07-15 爱默蕾大学 用于骨化的化合物和组合物以及其相关的方法
WO2012022780A1 (en) 2010-08-19 2012-02-23 Université Libre de Bruxelles 18-beta-glycyrrhetinic acid derivatives with anti-tumor activity
EP2614055A2 (en) 2010-09-10 2013-07-17 Lupin Limited Process for preparation of substantially pure fosamprenavir calcium and its intermediates
US9079834B2 (en) 2010-10-28 2015-07-14 Merck Canada Inc. HIV protease inhibitors
CA2816022C (en) 2010-10-29 2019-09-10 Emory University Quinazoline derivatives, compositions, and uses related thereto
GB201019043D0 (en) 2010-11-10 2010-12-22 Protea Biopharma N V Use of 2',5'-oligoadenylate derivative compounds
EP3153510B1 (en) 2010-12-03 2020-05-06 Emory University Fused azines as chemokine cxcr4 receptor modulators and uses related thereto
CN102584748B (zh) * 2011-01-13 2015-02-11 浙江九洲药业股份有限公司 夫沙那韦中间体的制备方法
US8691777B2 (en) 2011-01-27 2014-04-08 Emory University Combination therapy
WO2012116135A2 (en) 2011-02-24 2012-08-30 Emory University Noggin blocking compositions for ossification and methods related thereto
US11179500B2 (en) 2011-02-24 2021-11-23 Emory University JAB1 inhibitory compositions for ossification and methods related thereto
US9365523B2 (en) 2011-03-31 2016-06-14 Emory University Imidazolyl amide compounds and uses related thereto
US20140045936A1 (en) 2011-04-21 2014-02-13 Wake Forest University Health Sciences Cyclopropyl derivatives and methods of use
GB201107223D0 (en) 2011-04-29 2011-06-15 Amakem Nv Novel rock inhibitors
EP2707034A1 (en) 2011-05-09 2014-03-19 Universiteit Antwerpen Activity-based probes for the urokinase plasminogen activator
GB201108225D0 (en) 2011-05-17 2011-06-29 Amakem Nv Novel KBC inhibitors
CA2839956A1 (en) 2011-06-20 2012-12-27 Emory University Prostaglandin receptor ep2 antagonists, derivatives, compositions, and uses related thereto
WO2013011485A1 (en) 2011-07-20 2013-01-24 Ranbaxy Laboratories Limited Process for the preparation of sulfonamides useful as retroviral protease inhibitors
GB201113689D0 (en) 2011-08-09 2011-09-21 Amakem Nv Novel PDE4 inhibitors
WO2013028543A1 (en) 2011-08-19 2013-02-28 Emory University Bax agonist, compositions, and methods related thereto
GB201114854D0 (en) 2011-08-29 2011-10-12 Amakem Nv Novel rock inhibitors
BR112014004545A2 (pt) 2011-08-31 2017-04-04 Amakem Nv inibidores leves de rock
CN104023728B (zh) 2011-09-30 2016-11-02 益普生制药股份有限公司 大环lrrk2激酶抑制剂
MX347765B (es) 2011-09-30 2017-05-12 Oncodesign Sa Inhibidores macrociclicos de la quinasa flt3.
US9133157B2 (en) 2011-10-26 2015-09-15 Merck Canada Inc. HIV protease inhibitors
GB201119358D0 (en) 2011-11-10 2011-12-21 Lewi Paulus J Disubstituted triazine dimers for treatment and/or prevention of infectious diseases
WO2013113722A1 (en) 2012-01-30 2013-08-08 Universiteit Gent Anti-invasive compounds
GB201204756D0 (en) 2012-03-19 2012-05-02 Lewi Paulus J Triazines with suitable spacers for treatment and/or prevention of HIV infections
US20150110723A1 (en) 2012-05-31 2015-04-23 Emory University Quinazoline derivatives, compositions, and uses related thereto
EP2877461B1 (en) 2012-07-27 2018-05-09 Emory University Heterocyclic flavone derivatives, compositions, and methods related thereto
EP2895482B1 (en) 2012-09-11 2016-10-19 Merck Sharp & Dohme Corp. Hiv protease inhibitors
WO2014059034A2 (en) 2012-10-09 2014-04-17 President And Fellows Of Harvard College Nad biosynthesis and precursors for the treatment and prevention of cancer and proliferation
US9227990B2 (en) 2012-10-29 2016-01-05 Cipla Limited Antiviral phosphonate analogues and process for preparation thereof
EP2914585B1 (en) 2012-11-05 2018-03-07 Emory University 7,8-dihydroxyflavone and 7,8-substituted flavone derivatives, compositions, and methods related thereto
WO2014072419A1 (en) 2012-11-08 2014-05-15 Universiteit Antwerpen Novel anti-hiv compounds
DK2951172T3 (en) 2013-01-29 2017-07-17 Redx Pharma Plc PYRIDINE DERIVATIVES LIKE SOFT ROCK INHIBITORS
BR112015022650A8 (pt) 2013-03-15 2018-01-23 Oncodesign Sa inibidores de quinase induzível por sal macrocíclico.
WO2015013835A1 (en) 2013-07-31 2015-02-05 Merck Sharp & Dohme Corp. Piperazine derivatives as hiv protease inhibitors
JP6762873B2 (ja) 2013-09-11 2020-09-30 エモリー・ユニバーシテイ ヌクレオチドおよびヌクレオシド組成物ならびにこれらに関連する使用
WO2015055796A1 (en) 2013-10-16 2015-04-23 Université Libre de Bruxelles Formulations useful in the treatment of proliferative diseases affecting the respiratory tract
CA2929203C (en) 2013-11-12 2023-04-18 Vrije Universiteit Brussel Rna transcription vector and uses thereof
WO2015095276A1 (en) 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Hiv protease inhibitors
EP3113780B1 (en) 2014-03-06 2019-08-14 Merck Sharp & Dohme Corp. Hiv protease inhibitors
EP3125940A2 (en) 2014-04-01 2017-02-08 Université Libre de Bruxelles New strategies for treating melanoma
WO2015150337A1 (en) 2014-04-01 2015-10-08 Amakem Nv Lim kinase inhibitors
WO2015171589A1 (en) 2014-05-05 2015-11-12 Emory University Bh4 antagonists and methods related thereto
WO2015175855A1 (en) 2014-05-16 2015-11-19 Emory University Chemokine cxcr4 and ccr5 receptor modulators and used related thereto
EP3180003B1 (en) 2014-07-01 2022-01-12 The Regents of the University of California Pkc-epsilon inhibitors
WO2016005340A1 (en) 2014-07-08 2016-01-14 Universiteit Gent Hamamelitannin analogues and uses thereof
HUE048518T2 (hu) 2014-09-17 2020-07-28 Oncodesign Sa Makrociklusos RIP2 kináz inhibitorok
TR201904514T4 (tr) 2014-09-17 2019-04-22 Oncodesign Sa Makrosiklik LRRK2 kinaz inhibitörleri.
WO2016069955A1 (en) 2014-10-29 2016-05-06 Wisconsin Alumni Research Foundation Boronic acid inhibitors of hiv protease
WO2016083490A1 (en) 2014-11-27 2016-06-02 Remynd Nv Compounds for the treatment of amyloid-associated diseases
EP3233878B1 (en) 2014-12-15 2025-09-03 Emory University Phosphoramidates for the treatment of hepatitis b virus
HUE056470T2 (hu) 2014-12-26 2022-02-28 Univ Emory Vírusellenes N4-Hidroxicitidin származékok
WO2016146651A1 (en) 2015-03-16 2016-09-22 Oncodesign Sa Macrocyclic activin-like receptor kinase inhibitors
WO2016176437A1 (en) 2015-04-28 2016-11-03 Newsouth Innovations Pty Limited Targeting nad+ to treat chemotherapy and radiotherapy induced cognitive impairment, neuropathies and inactivity
EP3804706B1 (en) 2015-05-29 2023-08-23 Emory University 2-amino-n'-benzylideneacetohydrazides and derivatives for the management of cftr protein mediated diseases
CA3015430A1 (en) 2016-02-29 2017-09-08 Oncodesign S.A. Radiolabeled macrocyclic egfr inhibitor
WO2017157882A1 (en) 2016-03-14 2017-09-21 Université Catholique de Louvain Serine biosynthetic pathway inhibitors
WO2017189978A1 (en) 2016-04-28 2017-11-02 Emory University Alkyne containing nucleotide and nucleoside therapeutic compositions and uses related thereto
JP2019516715A (ja) 2016-05-19 2019-06-20 ユニバーシタット アントウェルペン Ｐａｒ関連疾患の予防および／または治療における使用のためのビス（アセトアミドフェニル）グアニジノフェニルエチルホスホネート
BE1023757B1 (nl) 2016-06-30 2017-07-12 Yun NV Bewaring van micro-organismen
WO2018065387A1 (en) 2016-10-04 2018-04-12 Universiteit Gent Novel hamamelitannin analogues and uses thereof
CN109923123B (zh) 2016-10-14 2024-01-23 爱默蕾大学 具有结合或阻断pd-l1的分子的纳米颗粒及其在治疗癌症中的用途
US11331297B2 (en) 2016-10-26 2022-05-17 Emory University Polyoxometalate complexes and uses in managing cancer
WO2018096088A1 (en) 2016-11-24 2018-05-31 Universiteit Antwerpen Halogenated benzotropolones as atg4b inhibitors
CN110325206A (zh) 2016-12-13 2019-10-11 埃默里大学 用于管理病毒感染的多肽
WO2018138358A1 (en) 2017-01-30 2018-08-02 Université de Liège Perk and ire-1a inhibitors against neurodevelopmental disorders
EP3585387A4 (en) 2017-02-21 2020-08-12 Emory University CHEMIOKIN CXCR4 RECEIVER MODULATORS AND THEIR USES
EP3634407A1 (en) 2017-05-11 2020-04-15 Remynd N.V. Inhibitors of pde6delta for use in the prevention and/or treatment of epilepsy and/or neurodegenerative disorders
US11548881B2 (en) 2017-05-11 2023-01-10 Remynd N.V. Compounds for the treatment of epilepsy, neurodegenerative disorders and other CNS disorders
EP3661937B1 (en) 2017-08-01 2021-07-28 Gilead Sciences, Inc. Crystalline forms of ethyl ((s)-((((2r,5r)-5-(6-amino-9h-purin-9-yl)-4-fluoro-2,5-dihydrofuran-2-yl)oxy)methyl)(phenoxy)phosphoryl)-l-alaninate (gs-9131) for treating viral infections
EP3651747A4 (en) 2017-11-17 2020-07-22 Cellix Bio Private Limited COMPOSITIONS AND METHODS OF TREATMENT OF EYE DISORDERS
PH12022550371A1 (en) 2017-12-07 2023-05-03 Univ Emory N4-hydroxycytidine and derivatives and anti-viral uses related thereto
WO2019193091A1 (en) 2018-04-05 2019-10-10 Universiteit Hasselt Selective pde4d inhibitors against demyelinating diseases
SG11202012731WA (en) 2018-06-29 2021-01-28 Rejuvenate Biomed Pharmaceutical combination for use in age-related and/or degenerative diseases
ES2974972T3 (es) 2018-08-07 2024-07-02 Univ Emory Derivados heterocíclicos de flavona, composiciones y métodos relacionados con los mismos
US12281308B2 (en) 2018-08-29 2025-04-22 University Of Massachusetts Inhibition of protein kinases to treat Friedreich ataxia
CA3133797A1 (en) 2019-03-20 2020-09-24 Emory University Prostaglandin receptor ep2 antagonists, derivatives, and uses related thereto
US20220227757A1 (en) 2019-05-14 2022-07-21 Suzhou Four Health Pharmaceuticals Co., Ltd. Quinazoline-2,4-dione derivatives as parp inhibitors
AR121403A1 (es) 2020-02-24 2022-06-01 Univ Leuven Kath Compuestos derivados de pirrolopiridina e imidazopiridina con actividad antiviral
GB202003240D0 (en) 2020-03-05 2020-04-22 Ecosynth Nv Antiviral treatment
EP4121121A4 (en) 2020-03-16 2024-09-25 Emory University RADIONUCLIDE TRACERS OF 1-AMINO-3,4-DIFLUOROCYCLOPENTAN-1-CARBOXYLIC ACID, DERIVATIVES AND USES THEREOF
WO2021209563A1 (en) 2020-04-16 2021-10-21 Som Innovation Biotech, S.A. Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus
US12083099B2 (en) 2020-10-28 2024-09-10 Accencio LLC Methods of treating symptoms of coronavirus infection with viral protease inhibitors
WO2022157381A1 (en) 2021-01-25 2022-07-28 Universiteit Hasselt Phloretin for use in the treatment of neurodegenerative and demyelinating diseases
JP7637827B2 (ja) 2021-07-30 2025-02-28 コンフォ セラピューティクス エヌ．ベー． 疼痛、特に神経障害性疼痛、並びに／又は、ａｔ２ｒ及び／若しくはａｔ２ｒ媒介性シグナル伝達に関連する他の疾患若しくは障害の治療のための化合物
EP4387629A1 (en) 2021-08-18 2024-06-26 Katholieke Universiteit Leuven KU Leuven Research & Development 6-substituted- and 6,7-disubstituted-7-deazapurine ribonucleoside analogues
EP4405357A1 (en) 2021-09-23 2024-07-31 Katholieke Universiteit Leuven KU Leuven Research & Development Ribonucleoside analogues against -sars-cov-2
WO2023105283A1 (en) 2021-12-08 2023-06-15 Fundacio Privada Institut De Recerca De La Sida - Caixa Nucleoside reverse transcriptase inhibitors for use in down syndrome and alzheimer`s disease therapy
US11541071B1 (en) 2021-12-16 2023-01-03 Ascletis BioScience Co., Ltd Nucleoside derivatives and methods of use thereof
WO2023111683A1 (en) 2021-12-16 2023-06-22 Ascletis Bioscience Co., Ltd. N4-hydroxycytidine derivatives and use thereof as antiviral agent
WO2023139402A1 (en) 2022-01-18 2023-07-27 Ascletis Bioscience Co., Ltd. Inhibitors of cysteine proteases and methods of use thereof
US11760722B2 (en) 2022-01-18 2023-09-19 Ascletis Bioscience Co., Ltd. Inhibitors of cysteine proteases and methods of use thereof
WO2023180567A1 (en) 2022-03-24 2023-09-28 Fundacion Privada Institut De Recerca De La Sida-Caixa Cyclodextrins for use in coronavirus infection therapy
WO2023241799A1 (en) 2022-06-15 2023-12-21 Université Libre de Bruxelles Flavanols for use in the treatment of retroviral infections
US20240025885A1 (en) 2022-07-08 2024-01-25 Ascletis BioScience Co., Ltd Triazine derivatives and methods of use thereof
CN115504968B (zh) 2022-11-21 2023-04-18 歌礼生物科技（杭州）有限公司 三嗪衍生物
WO2024193451A1 (en) 2023-03-17 2024-09-26 Ascletis BioScience Co., Ltd Triazine derivatives, method of making and method of using thereof
WO2025104221A1 (en) 2023-11-15 2025-05-22 Université Libre de Bruxelles Uses of protein tyrosine phosphatase receptor kappa inhibitors

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3743722A (en) * 1971-07-14 1973-07-03 Abbott Lab Anti-coagulant isolation
FR2459235A1 (fr) * 1979-06-14 1981-01-09 Sanofi Sa Nouveaux derives de sulfonyl-aniline, leur procede de preparation et leur application therapeutique
JPS5946252A (ja) * 1982-09-09 1984-03-15 Dainippon Ink & Chem Inc 含フツ素アミノカルボキシレ−トおよびその製法
JPS5948449A (ja) * 1982-09-13 1984-03-19 Dainippon Ink & Chem Inc 直鎖状含フツ素アニオン化合物およびその製造方法
JPS6171830A (ja) * 1984-09-17 1986-04-12 Dainippon Ink & Chem Inc 界面活性剤組成物
US4616088A (en) * 1984-10-29 1986-10-07 E. R. Squibb & Sons, Inc. Amino acid ester and amide renin inhibitor
US4629724A (en) * 1984-12-03 1986-12-16 E. R. Squibb & Sons, Inc. Amino acid ester and amide renin inhibitors
DE3635907A1 (de) * 1986-10-22 1988-04-28 Merck Patent Gmbh Hydroxy-aminosaeurederivate
NL8800100A (nl) * 1987-01-21 1988-08-16 Sandoz Ag Nieuwe peptidederivaten en werkwijzen voor het bereiden en toepassen van deze derivaten.
CA1340588C (en) 1988-06-13 1999-06-08 Balraj Krishan Handa Amino acid derivatives
IL91780A (en) * 1988-10-04 1995-08-31 Abbott Lab History of the amine of the xenon-preventing xanine acid, the process for their preparation and the pharmaceutical preparations containing them
WO1990007329A1 (en) 1989-01-06 1990-07-12 The Regents Of The University Of California Selection method for pharmacologically active compounds
US5354866A (en) * 1989-05-23 1994-10-11 Abbott Laboratories Retroviral protease inhibiting compounds
US5151438A (en) * 1989-05-23 1992-09-29 Abbott Laboratories Retroviral protease inhibiting compounds
IE902295A1 (en) * 1989-07-07 1991-01-16 Abbott Lab Amino acid analog cck antagonists
GB8927913D0 (en) * 1989-12-11 1990-02-14 Hoffmann La Roche Amino acid derivatives
CA2084087A1 (en) * 1990-06-01 1991-12-02 Prabhakar Kondaji Jadhav 1,4-diamino 2,3-dihydroxy butanes
TW225540B (forum.php) * 1990-06-28 1994-06-21 Shionogi & Co
HU9301447D0 (en) * 1990-11-19 1993-11-29 Monsanto Co Inhibitors of retrovirus protease
DK0558673T3 (da) 1990-11-19 1996-07-29 Monsanto Co Retrovirale proteaseinhibitorer
DK0554400T3 (da) * 1990-11-19 1998-02-16 Monsanto Co Retrovirale proteaseinhibitorer
ES2151618T3 (es) 1990-11-19 2001-01-01 Monsanto Co Inhibidores de proteasas retrovirales.
IE20010533A1 (en) * 1990-11-20 2003-03-05 Abbott Lab Intermediates for preparing retroviral protease inhibiting compounds
SG52731A1 (en) 1991-11-08 1998-09-28 Merck & Co Inc Hiv protease inhibitors useful for the treatment of aids
ES2091000T3 (es) * 1992-05-20 1996-10-16 Searle & Co Metodo para elaborar intermedios utiles en la sintesis de inhibidores de proteasas retroviricas.
CA2136312A1 (en) * 1992-05-21 1993-11-25 Michael Clare Retroviral protease inhibitors
ES2103488T3 (es) * 1992-08-25 1997-09-16 Searle & Co N-(alcanoilamino-2-hidroxipropil)sulfonamidas utiles como inhibidores de proteasas retrovirales.
CA2140929C (en) * 1992-08-25 2006-09-12 Michael L. Vazquez Hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
ATE161828T1 (de) * 1992-08-25 1998-01-15 Searle & Co Sulfonylalkanoylaminohydroxyethylaminosulfonami e verwendbar als retrovirale protease-inhibitoren
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
EP0885880A3 (en) * 1992-10-30 1999-10-06 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfamic acids useful as retroviral protease inhibitors
EP0666842B1 (en) * 1992-10-30 1998-06-24 G.D. Searle & Co. Hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors
AU6135294A (en) * 1993-02-12 1994-08-29 Merck & Co., Inc. Piperazine derivatives as hiv protease inhibitors
TW281669B (forum.php) * 1993-02-17 1996-07-21 Chugai Pharmaceutical Co Ltd

Also Published As

Publication number Publication date
WO1994005639A1 (en) 1994-03-17
MXPA03010538A (es) 2011-12-16
DE69324369D1 (de) 1999-05-12
CZ58795A3 (en) 1995-12-13
LT3302B (en) 1995-06-26
TW254927B (forum.php) 1995-08-21
FI951059A0 (fi) 1995-03-07
DE69333012T2 (de) 2004-04-01
BG99540A (bg) 1995-11-30
DE10199024I2 (de) 2006-04-06
DE10199024I1 (de) 2001-07-12
DE69333012D1 (de) 2003-07-03
CO4870779A1 (es) 1999-12-27
US5856353A (en) 1999-01-05
AU691160B2 (en) 1998-05-14
NO303444B1 (no) 1998-07-13
NZ256238A (en) 1997-04-24
GEP20012579B (en) 2001-11-26
HUT71892A (en) 1996-02-28
EP0659181A1 (en) 1995-06-28
AP9300572A0 (en) 1993-10-31
SK281360B6 (sk) 2001-02-12
NO950876L (no) 1995-05-08
HU228198B1 (en) 2013-01-28
CA2143208A1 (en) 1994-03-17
CZ289475B6 (cs) 2002-01-16
ATE178598T1 (de) 1999-04-15
EP0659181B1 (en) 1999-04-07
BR1100824A (pt) 1999-08-31
MY142901A (en) 2011-01-31
IS4068A (is) 1994-03-09
DK0659181T3 (da) 1999-10-18
US6372778B1 (en) 2002-04-16
ES2200243T3 (es) 2004-03-01
ATE241602T1 (de) 2003-06-15
EP0885887A3 (en) 1999-02-03
AP390A (en) 1995-08-02
CN1087347A (zh) 1994-06-01
PL185635B1 (pl) 2003-06-30
LU90736I2 (fr) 2001-05-07
NO950876D0 (no) 1995-03-07
PT885887E (pt) 2003-10-31
FI951059L (fi) 1995-04-18
NL300039I2 (nl) 2001-09-03
NO2001012I1 (no) 2001-07-23
AU4852093A (en) 1994-03-29
GR3030719T3 (en) 1999-11-30
RU2135496C1 (ru) 1999-08-27
DK0885887T3 (da) 2003-09-22
US7608632B2 (en) 2009-10-27
CA2143208C (en) 2003-01-07
KR100262056B1 (ko) 2000-07-15
PL307858A1 (en) 1995-06-26
RU95109928A (ru) 1997-03-20
JPH08501299A (ja) 1996-02-13
BG62488B1 (bg) 1999-12-30
IL106927A (en) 2001-01-11
JP3012002B2 (ja) 2000-02-21
CN1061339C (zh) 2001-01-31
US20080293727A1 (en) 2008-11-27
FI120685B (fi) 2010-01-29
NZ314376A (en) 1998-10-28
SK29395A3 (en) 1995-09-13
HU9500685D0 (en) 1995-04-28
US20060189810A1 (en) 2006-08-24
EP0885887B1 (en) 2003-05-28
ES2131589T3 (es) 1999-08-01
US20030069222A1 (en) 2003-04-10
UA44694C2 (uk) 2002-03-15
HK1012631A1 (en) 1999-08-06
LTIP917A (en) 1994-11-25
US20100210603A1 (en) 2010-08-19
EP0885887A2 (en) 1998-12-23
RO118747B1 (ro) 2003-10-30
US5585397A (en) 1996-12-17
PH31251A (en) 1998-05-05
HK1023561A1 (en) 2000-09-15
IL106927A0 (en) 1993-12-28
CY2164B1 (en) 2002-08-23
SG43862A1 (en) 1997-11-14
DE69324369T2 (de) 1999-08-26

Similar Documents

Publication Publication Date Title
IS2334B (is) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
DK0846110T3 (da) THF-holdige sulfonamidinhibitorer af aspartylprotease
EE200000386A (et) Aspartüülproteaasi inhibiitorite eelravimid
DK1086076T3 (da) Sulfonamidinhibitorer af aspartylprotease
DK0889036T3 (da) HIV-proteaseinhibitorer
NO932620D0 (no) Amindiol-proteaseinhibitorer
DK633189A (da) Anvendelse af peptidisostere som retrovirale proteasehaemmere
NO934628D0 (no) Retrovirus-protease-inhibitorer
FI962073A0 (fi) HIV-proteaasin estäjän prodrug-muotoja
ZA938470B (en) Sulfonamide inhibitors of aspartyl protease
SI0846110T1 (en) Thf-containing sulfonamide inhibitors of aspartyl protease
FI935707A0 (fi) Anvaendning av hirudinderivat som trombininhibitorer
NO920023L (no) Hiv-proteaseinhibitorer