CO4870779A1 - Nuevas sulfonamidas que inhiben la proteasa aspartilo - Google Patents

Nuevas sulfonamidas que inhiben la proteasa aspartilo

Info

Publication number
CO4870779A1
CO4870779A1 CO93406779A CO93406779A CO4870779A1 CO 4870779 A1 CO4870779 A1 CO 4870779A1 CO 93406779 A CO93406779 A CO 93406779A CO 93406779 A CO93406779 A CO 93406779A CO 4870779 A1 CO4870779 A1 CO 4870779A1
Authority
CO
Colombia
Prior art keywords
compound
group
het
hiv aspartyl
aspartyl protease
Prior art date
Application number
CO93406779A
Other languages
English (en)
Spanish (es)
Inventor
Roger D Tung
Murcko Max A
Rao Bhisetti Govinda
Original Assignee
Vertex Pharma
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 Pharma filed Critical Vertex Pharma
Publication of CO4870779A1 publication Critical patent/CO4870779A1/es

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)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Virology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Quinoline Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Furan Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Pyrrole Compounds (AREA)
  • Indole Compounds (AREA)
  • Peptides Or Proteins (AREA)
CO93406779A 1992-09-08 1993-09-07 Nuevas sulfonamidas que inhiben la proteasa aspartilo CO4870779A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
CO4870779A1 true CO4870779A1 (es) 1999-12-27

Family

ID=25477403

Family Applications (1)

Application Number Title Priority Date Filing Date
CO93406779A CO4870779A1 (es) 1992-09-08 1993-09-07 Nuevas sulfonamidas que inhiben la proteasa aspartilo

Country Status (40)

Country Link
US (7) US5585397A (en, 2012)
EP (2) EP0885887B1 (en, 2012)
JP (1) JP3012002B2 (en, 2012)
KR (1) KR100262056B1 (en, 2012)
CN (1) CN1061339C (en, 2012)
AP (1) AP390A (en, 2012)
AT (2) ATE241602T1 (en, 2012)
AU (1) AU691160B2 (en, 2012)
BG (1) BG62488B1 (en, 2012)
BR (1) BR1100824A (en, 2012)
CA (1) CA2143208C (en, 2012)
CO (1) CO4870779A1 (en, 2012)
CY (1) CY2164B1 (en, 2012)
CZ (1) CZ289475B6 (en, 2012)
DE (3) DE69333012T2 (en, 2012)
DK (2) DK0659181T3 (en, 2012)
ES (2) ES2200243T3 (en, 2012)
FI (1) FI120685B (en, 2012)
GE (1) GEP20012579B (en, 2012)
GR (1) GR3030719T3 (en, 2012)
HU (1) HU228198B1 (en, 2012)
IL (1) IL106927A (en, 2012)
IS (1) IS2334B (en, 2012)
LT (1) LT3302B (en, 2012)
LU (1) LU90736I2 (en, 2012)
MX (1) MXPA03010538A (en, 2012)
MY (1) MY142901A (en, 2012)
NL (1) NL300039I2 (en, 2012)
NO (2) NO303444B1 (en, 2012)
NZ (2) NZ314376A (en, 2012)
PH (1) PH31251A (en, 2012)
PL (1) PL185635B1 (en, 2012)
PT (1) PT885887E (en, 2012)
RO (1) RO118747B1 (en, 2012)
RU (1) RU2135496C1 (en, 2012)
SG (1) SG43862A1 (en, 2012)
SK (1) SK281360B6 (en, 2012)
TW (1) TW254927B (en, 2012)
UA (1) UA44694C2 (en, 2012)
WO (1) WO1994005639A1 (en, 2012)

Families Citing this family (305)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6878728B1 (en) 1999-06-11 2005-04-12 Vertex Pharmaceutical Incorporated Inhibitors of aspartyl protease
US20040122000A1 (en) * 1981-01-07 2004-06-24 Vertex Pharmaceuticals 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
DE69329920T2 (de) * 1992-03-27 2001-09-27 Akiko Itai Verfahren zur analyse der struktur von stabilen zusammengesetzten biopolymerligandmolekuelen
US6743929B1 (en) 1992-08-25 2004-06-01 G. D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
KR100336699B1 (ko) * 1992-08-25 2002-05-13 윌리암스 로저 에이 레트로바이러스 프로테아제 저해제로서 유용한히드록시에틸아미노 술폰아미드
US5968942A (en) 1992-08-25 1999-10-19 G. D. Searle & Co. α- and β-amino acid 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
US6046190A (en) * 1992-08-25 2000-04-04 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
US5783701A (en) * 1992-09-08 1998-07-21 Vertex Pharmaceuticals, Incorporated 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
DK0666842T3 (da) 1992-10-30 1998-11-02 Searle & Co Hydroxyethylaminosulfaminsyrederivater til anvendelse som inhibitorer af retrovirale proteaser
WO1994010136A1 (en) * 1992-10-30 1994-05-11 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfamic acids 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
US6376523B1 (en) 1994-05-20 2002-04-23 Texas Biotechnology Corporation Benzenesulfonamides and the use thereof to modulate the activity of endothelin
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
US6541498B2 (en) 1993-05-20 2003-04-01 Texas Biotechnology 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
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
CA2210889C (en) 1995-01-20 2007-08-28 G.D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
US5831117A (en) 1995-01-20 1998-11-03 G. D. Searle & Co. Method of preparing retroviral protease inhibitor intermediates
US6140505A (en) 1995-03-10 2000-10-31 G. D. Searle & Co. Synthesis of benzo fused heterocyclic sulfonyl chlorides
US5756533A (en) * 1995-03-10 1998-05-26 G.D. Searle & Co. Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6407134B1 (en) 1995-03-10 2002-06-18 G. D. Searle & Co. Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
CA2215022A1 (en) * 1995-03-10 1996-09-19 G.D. Searle & Co. Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6861539B1 (en) * 1995-03-10 2005-03-01 G. D. Searle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
EP1188766A1 (en) 1995-03-10 2002-03-20 G.D. Searle & Co. Bis-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
US5776971A (en) * 1995-03-10 1998-07-07 G.D. Searle & Co. Heterocyclecarbonyl 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
US7339078B2 (en) 1995-03-10 2008-03-04 G.D. Searle Llc 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
US5696135A (en) * 1995-06-07 1997-12-09 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity effective at stimulating neuronal growth
US5859031A (en) 1995-06-07 1999-01-12 Gpi Nil Holdings, Inc. Small molecule inhibitors of rotamase enzyme activity
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
EP0906107B1 (en) * 1996-03-22 2003-01-08 Glaxo Group Limited Compositions comprising vx 478 and a water soluble vitamin e compound such as vitamin 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
IL127350A0 (en) * 1996-06-25 1999-10-28 Glaxo Group Ltd Combinations comprising VX478 zidovudine and/or 1592U89 for use in the treatment of HIV
DE69727240T2 (de) * 1996-06-25 2004-11-25 Glaxo Group Ltd., Greenford Kombinationen, enthaltend VX478, Zidovudin und 3TC zur Behandlung von HIV
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
US5962725A (en) * 1996-09-05 1999-10-05 Agouron Pharmaceuticals, Inc. Intermediate compounds useful for making HIV protease inhibitors such as nelfinavir
US5801187A (en) 1996-09-25 1998-09-01 Gpi-Nil Holdings, Inc. Heterocyclic esters and amides
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
IN183408B (en, 2012) * 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
US5935989A (en) 1996-12-31 1999-08-10 Gpi Nil Holdings Inc. N-linked ureas and carbamates of heterocyclic thioesters
JP2002515050A (ja) 1996-12-31 2002-05-21 ジーピーアイ エヌアイエル ホールディングス インコーポレイテッド ヘテロ環式チオエステルのｎ−結合尿素およびカルバメート
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
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
TR200101905T2 (tr) 1997-04-28 2002-06-21 Texas Biotechnology Corporation Endotelin ile ilgili hastalıkların tedavisinde kullanılan sülfanoamidler.
US5783705A (en) * 1997-04-28 1998-07-21 Texas Biotechnology Corporation Process of preparing alkali metal salys of hydrophobic sulfonamides
AU734302B2 (en) * 1997-05-08 2001-06-07 Smithkline Beecham Corporation Protease inhibitors
US20010049381A1 (en) 1997-06-04 2001-12-06 Gpl Nil Holdings, Inc., Pyrrolidine derivative hair growth compositions and uses
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
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
WO1999033795A1 (en) * 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
AU2010299A (en) * 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs os aspartyl protease inhibitors
HUP0101598A3 (en) * 1997-12-24 2002-08-28 Vertex Pharmaceuticals Inc Cam Prodrugs of aspartyl protease inhibitors and medicaments containing them
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of 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
AU1708099A (en) 1998-06-03 1999-12-20 Amgen, Inc. N-linked sulfonamides of n-heterocyclic carboxylic acids or carboxylic acid isosteres
CA2334204A1 (en) 1998-06-03 1999-12-09 Gpi Nil Holdings, Inc. Heterocyclic ester and amide hair growth compositions and uses
US6331537B1 (en) 1998-06-03 2001-12-18 Gpi Nil Holdings, Inc. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic 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
CA2335477C (en) 1998-06-19 2010-11-30 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of aspartyl protease
ES2604662T3 (es) 1998-06-23 2017-03-08 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Ensayo de acondicionamiento físico y métodos para reducir la resistencia del VIH a la terapia
AU4862799A (en) 1998-07-08 2000-02-01 G.D. Searle & Co. 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
WO2000005400A1 (en) * 1998-07-24 2000-02-03 Samsung Fine Chemicals Co., Ltd. Process for preparing optically pure (s)-3,4-dihydroxybutyric acid derivatives
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
US7338976B1 (en) 1998-08-14 2008-03-04 Gpi Nil Holdings, Inc. Heterocyclic esters or amides 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
US6384056B1 (en) 1998-08-14 2002-05-07 Gpi Nil Holdings, Inc. Heterocyclic thioesters or ketones 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
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
US6376517B1 (en) 1998-08-14 2002-04-23 Gpi Nil Holdings, Inc. Pipecolic acid derivatives 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
US6333340B1 (en) 1998-08-14 2001-12-25 Gpi Nil Holdings, Inc. Small molecule sulfonamides for vision and memory disorders
US6462072B1 (en) 1998-09-21 2002-10-08 Gpi Nil Holdings, Inc. Cyclic ester or amide derivatives
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
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
CO5261510A1 (es) 1999-02-12 2003-03-31 Vertex Pharma Inhibidores de aspartil proteasa
WO2000047551A2 (en) * 1999-02-12 2000-08-17 Vertex Pharmaceuticals Incorporated Inhibitors of aspartyl protease
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
NZ518580A (en) * 1999-10-06 2004-01-30 Us Gov Health & Human Serv Hexahydrofuro[2,3-B]furan-3-YL-N- {3-[1,3-benzodioxol-5-ylsulfonyl) (isobutyl) amino]-1-benzyl-2-hydroxypropyl} carbamate as retroviral protease inhibitor
EP2314564A3 (en) 1999-12-23 2012-04-04 Ampac 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
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
US6391919B1 (en) 2000-01-12 2002-05-21 Bristol-Myers Squibb Pharma Company Bis-amino acid sulfonamides containing substituted benzyl amines HIV protease inhibitors
SI2269591T1 (en) 2000-01-19 2018-08-31 Abbvie Inc. Improved pharmaceutical formulations
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
KR100870184B1 (ko) * 2001-02-14 2008-11-24 티보텍 파마슈티칼즈 리미티드 광범위 2-(치환된-아미노)-벤조티아졸 설폰아미드 ｈｉｖ프로티아제 억제제
US6756063B2 (en) 2001-03-29 2004-06-29 Zoltan Laboratories, Llc Methods and compositions for the treatment of human and animal cancers
BR0208796A (pt) * 2001-04-09 2004-03-09 Tibotec Pharm Ltd Inibidores 2-(amino substituìdo)-benzoxazol sulfonamida hiv protease de amplo espectro
US6696494B2 (en) 2001-10-22 2004-02-24 Enanta Pharmaceuticals, Inc. α-hydroxyarylbutanamine inhibitors of aspartyl protease
CA2473231A1 (en) * 2002-01-07 2003-08-07 Sequoia Pharmaceuticals Resistance-repellent retroviral protease inhibitors
JP4625637B2 (ja) 2002-02-22 2011-02-02 シャイア エルエルシー 活性物質送達系及び活性物質を保護し投与する方法
US7157489B2 (en) * 2002-03-12 2007-01-02 The Board Of Trustees Of The University Of Illinois HIV protease inhibitors
DE60315023T2 (de) 2002-04-26 2008-04-03 Gilead Sciences, Inc., Foster City Anreicherung in der zelle an phosphonat analoga von hiv protease inhibitor verbindungen und die verbindungen selbst
NZ536496A (en) * 2002-05-17 2006-06-30 Tibotec Pharm Ltd Broadspectrum substituted benzisoxazole sulfonamide HIV protease inhibitors
AU2003276047A1 (en) * 2002-06-17 2003-12-31 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
US7115652B2 (en) * 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
HRP20050606B1 (hr) * 2002-08-14 2014-04-25 Tibotec Pharmaceuticals Ltd. Supstituirani oksindol sulfonamid hiv proteazni inhibitori širokog spektra
UY27967A1 (es) * 2002-09-10 2004-05-31 Pfizer Acetil 2-hindroxi-1,3-diaminoalcanos
EP1546088B1 (en) * 2002-10-03 2014-12-17 Novaremed Ltd. Compounds for use in the treatment of autoimmune diseases, immuno-allergical diseases and organ or tissue transplantation rejection
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
EP1565428A1 (en) * 2002-11-27 2005-08-24 Elan Pharmaceuticals, Inc. Substituted ureas and carbamates
US20050261237A1 (en) * 2003-04-25 2005-11-24 Boojamra Constantine G Nucleoside phosphonate analogs
US7452901B2 (en) 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
WO2005002626A2 (en) * 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
US7427636B2 (en) * 2003-04-25 2008-09-23 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
CN101410120A (zh) * 2003-04-25 2009-04-15 吉里德科学公司 抗炎的膦酸酯化合物
ATE490788T1 (de) 2003-04-25 2010-12-15 Gilead Sciences Inc Antivirale phosphonate analoge
US7432261B2 (en) * 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
WO2004096285A2 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Anti-infective phosphonate conjugates
US7470724B2 (en) * 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
JP2006524710A (ja) * 2003-04-25 2006-11-02 ギリアード サイエンシーズ， インコーポレイテッド キナーゼインヒビターホスホネート抱合体
US20090247488A1 (en) * 2003-04-25 2009-10-01 Carina Cannizzaro Anti-inflammatory phosphonate compounds
US7407965B2 (en) * 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
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
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
EP1671937A4 (en) * 2003-09-19 2007-08-08 Ube Industries METHOD FOR PRODUCING A NITRILE COMPOUND, CARBOXYLIC COMPOUND OR CARBOXYLATE COMPOUND
US7432273B2 (en) * 2003-10-24 2008-10-07 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
US7427624B2 (en) * 2003-10-24 2008-09-23 Gilead Sciences, Inc. Purine nucleoside phosphorylase inhibitory phosphonate compounds
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
BRPI0418031A (pt) * 2003-12-22 2007-04-17 Gilead Sciences Inc inibidores de quinase fosfonato-substituìdos
CA2548753A1 (en) * 2003-12-22 2005-07-14 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
ME01059B (me) 2003-12-23 2012-10-20 Janssen Sciences Ireland Uc Proces za pripremanje (3r,3as,6ar)-heksahidrofuro [2,3-b] furan-3-il (1s,2r)-3-[[(4-aminofenil) sulfonil] (izobutil) amino]-1-benzil-2- hidroksipropilkarbamata
US7200207B2 (en) * 2004-03-13 2007-04-03 Intrado Inc. Communication network for providing emergency services
CA2560922C (en) * 2004-03-26 2014-01-07 New Era Biotech, Ltd. Improvements in or relating to compounds for use in the treatment of aids and other viral diseases and hiv-related infections and compositions containing such compounds, methods of treating such diseases and infections and methods of making such compounds and compositions
LT2258376T (lt) 2004-07-27 2019-05-10 Gilead Sciences, Inc. Živ inhibuojančių junginių fosfonato analogai
US20060116397A1 (en) * 2004-10-13 2006-06-01 The Trustees Of The University Of Pennsylvania Use of saquinavir as a radiation sensitizer
US20060135510A1 (en) * 2004-10-13 2006-06-22 The Trustees Of The University Of Pennsylvania Use of amprenavir as a radiation sensitizer
CN101098698A (zh) 2004-12-01 2008-01-02 德福根有限公司 与离子通道尤其是Kv家族离子通道相互作用的5-羧酰胺基取代的噻唑衍生物
MX2007006534A (es) 2004-12-17 2007-07-25 Devgen Nv Composiciones nematicidas.
WO2006104646A1 (en) * 2005-03-11 2006-10-05 Smithkline Beecham Corporation 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
AU2007246779B2 (en) * 2006-05-09 2013-11-28 Novaremed Ltd Compounds for the treatment of cell proliferative disorders
CA2679482C (en) 2007-03-12 2015-04-21 Nektar Therapeutics Oligomer-protease inhibitor conjugates
MX2009011574A (es) 2007-04-27 2009-11-09 Tibotec Pharm Ltd Metodos para la preparacion de derivados de n-isobutil-n-(2-hidrox i-3-amino-4-fenilbutil)-p-nitrobencensulfonilamida.
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
AU2008305678A1 (en) * 2007-09-25 2009-04-02 Merck Sharp & Dohme Corp. 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
KR101479371B1 (ko) * 2008-06-05 2015-01-05 아사히 가세이 파마 가부시키가이샤 술폰아미드 화합물 및 그 용도
EP2307345A4 (en) * 2008-07-01 2012-05-02 Purdue Research Foundation NON-PEPTIDINHIBITORS OF HIV-1 PROTEASE
ES2393962T3 (es) * 2008-07-08 2013-01-03 Gilead Sciences, Inc. Sales de compuestos inhibidores del VIH.
AU2010254415B2 (en) 2009-05-27 2013-07-04 Merck Sharp & Dohme Corp. HIV protease inhibitors
EP2440249A2 (en) 2009-06-12 2012-04-18 Nektar Therapeutics Covalent conjugates comprising a protease inhibitor, a water-soluble, non-peptidic oligomer and a lipophilic moiety
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
EP2533793B1 (en) 2010-02-12 2015-12-09 Emory University GAL-4 for use in the treatment of infectious diseases
AU2011222900B2 (en) 2010-03-02 2016-09-29 Ph Pharma Co., Ltd. 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
US20130115237A1 (en) 2010-06-09 2013-05-09 Vaccine Technologies, Incorporated Therapeutic immunization in hiv infected subjects to augment antiretroviral treatment
EP2585463A1 (en) 2010-06-25 2013-05-01 Facultés Universitaires Notre-Dame de la Paix Beta carboline derivatives useful in the treatment of proliferative disorders
US8785648B1 (en) 2010-08-10 2014-07-22 The Regents Of The University Of California PKC-epsilon inhibitors
US9511071B2 (en) 2010-08-18 2016-12-06 Emory University Compounds and compositions for ossification and methods related thereto
WO2012022780A1 (en) 2010-08-19 2012-02-23 Université Libre de Bruxelles 18-beta-glycyrrhetinic acid derivatives with anti-tumor activity
WO2012032389A2 (en) 2010-09-10 2012-03-15 Lupin Limited Process for preparation of substantially pure fosamprenavir calcium and its intermediates
WO2012055031A1 (en) 2010-10-28 2012-05-03 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
US8969381B2 (en) 2010-12-03 2015-03-03 Emory University Chemokine CXCR4 receptor modulators and used 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
EP2678052B1 (en) 2011-02-24 2018-09-26 Emory University Jab1 blocking compositions for ossification and methods related thereto
EP2691095B1 (en) 2011-03-31 2017-07-05 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
AU2012252433A1 (en) 2011-05-09 2013-11-07 Universiteit Antwerpen Activity-based probes for the urokinase plasminogen activator
GB201108225D0 (en) 2011-05-17 2011-06-29 Amakem Nv Novel KBC inhibitors
WO2012177618A1 (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
EP2744775B1 (en) 2011-08-19 2018-03-07 Emory University Bax agonist, compositions, and methods related thereto
GB201114854D0 (en) 2011-08-29 2011-10-12 Amakem Nv Novel rock inhibitors
JP2014525427A (ja) 2011-08-31 2014-09-29 アマケン エンヴェー Ｒｏｃｋキナーゼ阻害剤としてのビフェニルカルボキサミド
EA025881B1 (ru) 2011-09-30 2017-02-28 Онкодизайн С.А. Макроциклические ингибиторы flt3-киназы
ES2583477T3 (es) 2011-09-30 2016-09-21 Ipsen Pharma S.A.S. Inhibidores macrocíclicos de cinasa de LRRK2
WO2013059928A1 (en) 2011-10-26 2013-05-02 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
EP2810198B1 (en) 2012-01-30 2023-07-12 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
WO2013181135A1 (en) 2012-05-31 2013-12-05 Emory University Quinazoline derivatives, compositions, and uses related thereto
WO2014018741A1 (en) 2012-07-27 2014-01-30 Emory University Heterocyclic flavone derivatives, compositions, and methods related thereto
WO2014043019A1 (en) 2012-09-11 2014-03-20 Merck Sharp & Dohme Corp. Hiv protease inhibitors
US9877981B2 (en) 2012-10-09 2018-01-30 President And Fellows Of Harvard College NAD biosynthesis and precursors for the treatment and prevention of cancer and proliferation
EP2912047B1 (en) 2012-10-29 2016-08-24 Cipla Limited Antiviral phosphonate analogues and process for preparation thereof
CN104812744B (zh) 2012-11-05 2017-12-01 爱默蕾大学 7,8‑二羟黄酮和7,8‑取代的黄酮衍生物、组合物及其相关方法
WO2014072419A1 (en) 2012-11-08 2014-05-15 Universiteit Antwerpen Novel anti-hiv compounds
SMT201700317T1 (it) 2013-01-29 2017-09-07 Redx Pharma Plc Derivati piridinici in qualità di inibitori rock teneri
KR20150133767A (ko) 2013-03-15 2015-11-30 온코디자인 에스.에이. 거대고리 염-유도성 키나아제 억제제
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
EP3057619A1 (en) 2013-10-16 2016-08-24 Université Libre de Bruxelles Formulations useful in the treatment of proliferative diseases affecting the respiratory tract
ES2666380T3 (es) 2013-11-12 2018-05-04 Vrije Universiteit Brussel Vector de transcripción de ARN y sus usos
US9834526B2 (en) 2013-12-19 2017-12-05 Merck Sharp & Dohme Corp. HIV protease inhibitors
EP3113780B1 (en) 2014-03-06 2019-08-14 Merck Sharp & Dohme Corp. Hiv protease inhibitors
US20170165240A1 (en) 2014-04-01 2017-06-15 Université Libre de Bruxelles New strategies for treating melanoma
WO2015150337A1 (en) 2014-04-01 2015-10-08 Amakem Nv Lim kinase inhibitors
AU2015256266B2 (en) 2014-05-05 2019-01-17 Emory University BH4 antagonists and methods related thereto
US10450293B2 (en) 2014-05-16 2019-10-22 Emory University Chemokine CXCR4 and CCR5 receptor modulators and uses 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
AU2015316801B2 (en) 2014-09-17 2019-03-07 Oncodesign S.A. Macrocyclic LRRK2 kinase inhibitors
JP6736545B2 (ja) 2014-09-17 2020-08-05 オンコデザイン エス．ア． 大環状ｒｉｐ２キナーゼ阻害剤
US9738664B2 (en) 2014-10-29 2017-08-22 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
JP6735751B2 (ja) 2014-12-15 2020-08-05 エモリー ユニバーシティー Ｂ型肝炎ウイルスの治療のためのホスホルアミデート
SG11201705069YA (en) 2014-12-26 2017-07-28 Univ Emory N4-hydroxycytidine and derivatives and anti-viral uses related thereto
WO2016146651A1 (en) 2015-03-16 2016-09-22 Oncodesign Sa Macrocyclic activin-like receptor kinase inhibitors
CN108025187A (zh) 2015-04-28 2018-05-11 新南创新私人有限公司 靶向nad+以治疗化学疗法和放射疗法引发的认知损害、神经病变和不活动
EP4272820A3 (en) 2015-05-29 2024-01-03 Emory University 2-amino-n'-benzylideneacetohydrazides and derivatives for the management of cftr protein mediated diseases
US10716869B2 (en) 2016-02-29 2020-07-21 Oncodesign Sa Radiolabeled macrocyclic EGFR inhibitor
WO2017157882A1 (en) 2016-03-14 2017-09-21 Université Catholique de Louvain Serine biosynthetic pathway inhibitors
US11192914B2 (en) 2016-04-28 2021-12-07 Emory University Alkyne containing nucleotide and nucleoside therapeutic compositions and uses related thereto
EP3458072B1 (en) 2016-05-19 2020-09-30 Universiteit Antwerpen Bis(acetamidophenyl) guanidinophenylethylphosphonates for use in the prevention and/or treatment of par-related diseases
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
EP3532488A4 (en) 2016-10-14 2020-04-29 Emory University NANOPARTICLES HAVING MOLECULES THAT BIND OR BLOCK PD-L1 AND THEIR USES IN THE TREATMENT OF CANCER
WO2018081442A1 (en) 2016-10-26 2018-05-03 Emory University Polyoxometalate complexes and uses in managing cancer
US10738002B2 (en) 2016-11-24 2020-08-11 Universitair Ziekenhuis Antwerpen Halogenated benzotropolones as ATG4B inhibitors
EP3554533B1 (en) 2016-12-13 2021-06-09 Emory University Polypeptides for managing viral infections
EP3573608A1 (en) 2017-01-30 2019-12-04 Université de Liège Perk and ire-1a inhibitors against neurodevelopmental disorders
CN110545814A (zh) 2017-02-21 2019-12-06 爱默蕾大学 趋化因子cxcr4受体调节剂及其相关用途
EP3621963B1 (en) 2017-05-11 2024-01-24 Remynd N.V. Compounds for the treatment of epilepsy, neurodegenerative disorders and other cns disorders
US12178805B2 (en) 2017-05-11 2024-12-31 Remynd N.V. Inhibitors of PDE6Delta for use in the prevention and/or treatment of epilepsy and/or neurodegenerative disorders
EP3960740B1 (en) 2017-08-01 2023-11-15 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) vanillate for treating viral infections
EP3651747A4 (en) 2017-11-17 2020-07-22 Cellix Bio Private Limited COMPOSITIONS AND METHODS OF TREATMENT OF EYE DISORDERS
JP6804790B1 (ja) 2017-12-07 2020-12-23 エモリー ユニバーシティー Ｎ４−ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途
CA3135420A1 (en) 2018-04-05 2019-10-10 Universiteit Hasselt Selective pde4d inhibitors against demyelinating diseases
ES2965834T3 (es) 2018-06-29 2024-04-17 Rejuvenate Biomed Combinación farmacéutica que comprende una biguanida y un inhibidor de la acetilcolinesterasa para usar en enfermedades relacionadas con la edad y/o degenerativas
WO2020033604A1 (en) 2018-08-07 2020-02-13 Emory University Heterocyclic flavone derivatives, compositions, and methods related thereto
US12281308B2 (en) 2018-08-29 2025-04-22 University Of Massachusetts Inhibition of protein kinases to treat Friedreich ataxia
US12240829B2 (en) 2019-03-20 2025-03-04 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
BR112022016733A2 (pt) 2020-02-24 2022-10-11 Univ Leuven Kath Compostos antivirais de pirrolpiridina e imidazopiridina
GB202003240D0 (en) 2020-03-05 2020-04-22 Ecosynth Nv Antiviral treatment
WO2021188592A1 (en) 2020-03-16 2021-09-23 Emory University Radionuclide tracers of 1-amino-3,4-difluorocyclopentane-1-carboxylic acid, derivatives, and uses thereof
US20230218644A1 (en) 2020-04-16 2023-07-13 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
WO2023006893A1 (en) 2021-07-30 2023-02-02 Confo Therapeutics N.V. Compounds for the treatment of pain, in particular neuropathic pain, and/or other diseases or disorders that are associated with at2r and/or at2r mediated signaling
US20250144125A1 (en) 2021-08-18 2025-05-08 Katholieke Universiteit Leuven 6-substituted- and 6,7-disubstituted-7-deazapurine ribonucleoside analogues
US20250066365A1 (en) 2021-09-23 2025-02-27 Katholieke Universiteit Leuven 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
WO2023111683A1 (en) 2021-12-16 2023-06-22 Ascletis Bioscience Co., Ltd. N4-hydroxycytidine derivatives and use thereof as antiviral agent
US11541071B1 (en) 2021-12-16 2023-01-03 Ascletis BioScience Co., Ltd Nucleoside derivatives 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
WO2023139402A1 (en) 2022-01-18 2023-07-27 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
CN116514783A (zh) 2022-11-21 2023-08-01 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
GB2200115B (en) * 1987-01-21 1990-11-14 Sandoz Ltd Novel peptide derivatives, their production and use
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
EP0532693A1 (en) * 1990-06-01 1993-03-24 The Du Pont Merck Pharmaceutical Company 1,4-diamino-2,3-dihydroxybutanes
TW225540B (en, 2012) * 1990-06-28 1994-06-21 Shionogi & Co
WO1992008698A1 (en) * 1990-11-19 1992-05-29 Monsanto Company Retroviral protease inhibitors
DK0558673T3 (da) 1990-11-19 1996-07-29 Monsanto Co Retrovirale proteaseinhibitorer
ES2059295T3 (es) * 1990-11-19 1998-06-01 Monsanto Co Inhibidores de las proteasas retrovirales.
DK0731088T3 (da) 1990-11-19 2000-10-16 Monsanto Co Retrovirale proteaseinhibitorer
IE913840A1 (en) * 1990-11-20 1992-05-20 Abbott Lab Retroviral protease inhibiting compounds
CA2195027C (en) * 1991-11-08 2000-01-11 Joseph P. Vacca Hiv protease inhibitors useful for the treatment of aids
KR100290516B1 (ko) * 1992-05-20 2001-09-17 죤 에이치. 뷰센 레트로바이러스프로테아제억제인자의합성에유용한중간생성물의제조방법
WO1993023379A1 (en) * 1992-05-21 1993-11-25 Monsanto Company Retroviral protease inhibitors
DK0656886T3 (da) * 1992-08-25 1998-02-02 Searle & Co N-(Alkanoylamino-2-hydroxypropyl)-sulfonamider til anvendelse som inhibitorer af retrovirale proteaser
KR100336699B1 (ko) * 1992-08-25 2002-05-13 윌리암스 로저 에이 레트로바이러스 프로테아제 저해제로서 유용한히드록시에틸아미노 술폰아미드
ATE161828T1 (de) * 1992-08-25 1998-01-15 Searle & Co Sulfonylalkanoylaminohydroxyethylaminosulfonami e verwendbar als retrovirale protease-inhibitoren
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
DK0666842T3 (da) * 1992-10-30 1998-11-02 Searle & Co Hydroxyethylaminosulfaminsyrederivater til anvendelse som inhibitorer af retrovirale proteaser
WO1994010136A1 (en) * 1992-10-30 1994-05-11 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfamic acids useful as retroviral protease inhibitors
WO1994018192A1 (en) * 1993-02-12 1994-08-18 Merck & Co., Inc. Piperazine derivatives as hiv protease inhibitors
JP3419539B2 (ja) * 1993-02-17 2003-06-23 中外製薬株式会社 インドリン−２−オン誘導体

Also Published As

Publication number Publication date
US20100210603A1 (en) 2010-08-19
CZ58795A3 (en) 1995-12-13
ATE241602T1 (de) 2003-06-15
PT885887E (pt) 2003-10-31
BG99540A (bg) 1995-11-30
NO2001012I1 (no) 2001-07-23
US7608632B2 (en) 2009-10-27
LTIP917A (en) 1994-11-25
NZ256238A (en) 1997-04-24
SK29395A3 (en) 1995-09-13
TW254927B (en, 2012) 1995-08-21
IL106927A0 (en) 1993-12-28
GR3030719T3 (en) 1999-11-30
HK1023561A1 (en) 2000-09-15
SK281360B6 (sk) 2001-02-12
PH31251A (en) 1998-05-05
EP0659181B1 (en) 1999-04-07
CZ289475B6 (cs) 2002-01-16
DE69324369T2 (de) 1999-08-26
DK0885887T3 (da) 2003-09-22
HK1012631A1 (en) 1999-08-06
KR100262056B1 (ko) 2000-07-15
NO303444B1 (no) 1998-07-13
DE10199024I1 (de) 2001-07-12
DE69333012D1 (de) 2003-07-03
CA2143208A1 (en) 1994-03-17
BG62488B1 (bg) 1999-12-30
CY2164B1 (en) 2002-08-23
JPH08501299A (ja) 1996-02-13
AU4852093A (en) 1994-03-29
AU691160B2 (en) 1998-05-14
US20080293727A1 (en) 2008-11-27
PL307858A1 (en) 1995-06-26
DE10199024I2 (de) 2006-04-06
EP0885887B1 (en) 2003-05-28
MY142901A (en) 2011-01-31
DE69333012T2 (de) 2004-04-01
US5856353A (en) 1999-01-05
RO118747B1 (ro) 2003-10-30
EP0659181A1 (en) 1995-06-28
DK0659181T3 (da) 1999-10-18
WO1994005639A1 (en) 1994-03-17
IS2334B (is) 2008-02-15
HU228198B1 (en) 2013-01-28
NL300039I2 (nl) 2001-09-03
LU90736I2 (fr) 2001-05-07
HU9500685D0 (en) 1995-04-28
AP9300572A0 (en) 1993-10-31
CA2143208C (en) 2003-01-07
US20030069222A1 (en) 2003-04-10
ES2131589T3 (es) 1999-08-01
JP3012002B2 (ja) 2000-02-21
MXPA03010538A (es) 2011-12-16
AP390A (en) 1995-08-02
DE69324369D1 (de) 1999-05-12
FI120685B (fi) 2010-01-29
ES2200243T3 (es) 2004-03-01
RU95109928A (ru) 1997-03-20
GEP20012579B (en) 2001-11-26
US5585397A (en) 1996-12-17
IL106927A (en) 2001-01-11
EP0885887A3 (en) 1999-02-03
US20060189810A1 (en) 2006-08-24
ATE178598T1 (de) 1999-04-15
NZ314376A (en) 1998-10-28
BR1100824A (pt) 1999-08-31
HUT71892A (en) 1996-02-28
SG43862A1 (en) 1997-11-14
LT3302B (en) 1995-06-26
PL185635B1 (pl) 2003-06-30
FI951059L (fi) 1995-04-18
UA44694C2 (uk) 2002-03-15
CN1061339C (zh) 2001-01-31
FI951059A0 (fi) 1995-03-07
US6372778B1 (en) 2002-04-16
NO950876D0 (no) 1995-03-07
NO950876L (no) 1995-05-08
IS4068A (is) 1994-03-09
CN1087347A (zh) 1994-06-01
RU2135496C1 (ru) 1999-08-27
EP0885887A2 (en) 1998-12-23

Similar Documents

Publication Publication Date Title
CO4870779A1 (es) Nuevas sulfonamidas que inhiben la proteasa aspartilo
PE20221277A1 (es) Inhibidores de ras
CO5690593A2 (es) Nuevos derivados de pirimidin 2-amina
AR045938A1 (es) Peptidos macrociclicos activos contra el virus de la hepatitis c
KR960014126A (ko) 시클로알카노-인돌 및 -아자인돌 유도체
CO6251241A2 (es) Compuestos de prolina modificados con actividad anti-vhc
BR9810555A (pt) Derivados epotilona
BR0114657A (pt) Compostos de benzamida e seu uso
AR070193A1 (es) Terapia combinada que comprende inhibidores de sglt e inhibidores de dpp4, composicion farmaceutica y uso
CO6150164A2 (es) Derivados de 2-metilmorfolina pirido-,pirazo-ypirimido-pirimidina como inhibidores de mtor
CO5570660A2 (es) Indazolilpirrolotriazinas c-6 modificadas
ES2087097T3 (es) Derivados de acidos fenilcarboxilicos que contienen un heterociclo.
AR057626A1 (es) Derivados de pirido pirazo y pirimido- pirimidina y su uso como inhibidores de mtor
AR063458A1 (es) Derivados de piridina inhibidores de 11beta hsd1
KR940021063A (ko) 퀴놀론카르복실산 유도체, 이의 제조방법 및 용도
RU2420291C3 (ru) Состав в мягкой желатиновой капсуле
AR058198A1 (es) Derivados de morfolina y composiciones farmaceuticas
PE20211053A1 (es) Inhibicion de la proteasa 30 especifica de la ubiquitina (usp30)
AR042827A1 (es) Compuestos de furano condensados
ES2476422T3 (es) Compuestos de piperidina 3,5-sustituida como inhibidores de renina
AR039190A1 (es) Derivados de benzofurano, composicion farmaceutica y medicamento que comprende el compuesto
CO4940477A1 (es) Inhibidores de proteasa
AR121275A1 (es) Compuesto de sulfonamida o sulfinamida que tiene acción inhibidora de la proteína brd4 y su uso como medicamento
AR081064A1 (es) Compuestos de tetraciclina policiclica
AR119594A1 (es) Derivados de tienopirimidina como inhibidores acc y usos de los mismos