NO950533D0 - Hydroksyetylaminosulfonamider som er nyttige som retrovirale proteasehemmere - Google Patents

Hydroksyetylaminosulfonamider som er nyttige som retrovirale proteasehemmere

Info

Publication number
NO950533D0
NO950533D0 NO950533A NO950533A NO950533D0 NO 950533 D0 NO950533 D0 NO 950533D0 NO 950533 A NO950533 A NO 950533A NO 950533 A NO950533 A NO 950533A NO 950533 D0 NO950533 D0 NO 950533D0
Authority
NO
Norway
Prior art keywords
hydroxyethylaminosulfonamides
useful
protease inhibitors
retroviral protease
retroviral
Prior art date
Application number
NO950533A
Other languages
English (en)
Other versions
NO950533L (no
NO305478B1 (no
Inventor
Michael L Vazques
Richard A Mueller
John J Talley
Daniel Getman
Gary A Decrescenzo
John N Freskos
Original Assignee
Searle & Co
Monsanto Co
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=25466397&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NO950533(D0) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Searle & Co, Monsanto Co filed Critical Searle & Co
Publication of NO950533L publication Critical patent/NO950533L/no
Publication of NO950533D0 publication Critical patent/NO950533D0/no
Publication of NO305478B1 publication Critical patent/NO305478B1/no

Links

Classifications

    • 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
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C311/05—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • 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
    • 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
    • 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
    • C07C311/11—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic unsaturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—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
    • C07C311/14—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of rings other than 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
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/20—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than 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
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/23—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms
    • C07C311/24—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22—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
    • C07C311/31—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 atoms of the sulfonamide groups bound to acyclic carbon atoms
    • C07C311/32—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 atoms of the sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—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
    • C07C311/41—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 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
    • C07C311/30—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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/02—Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to acyclic carbon atoms
    • C07C317/04—Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/02—Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to acyclic carbon atoms
    • C07C317/10—Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/14—Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/28—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/46—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having at least one of the nitrogen atoms, not being part of nitro or nitroso groups, further bound to other hetero atoms
    • C07C323/49—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having at least one of the nitrogen atoms, not being part of nitro or nitroso groups, further bound to other hetero atoms to sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/64—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton
    • C07C323/67—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfonamide groups, bound to the carbon skeleton
    • 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • 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
    • C07D213/81—Amides; Imides
    • 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
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • C07D213/89—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 with hetero atoms directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—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
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • C07D277/22—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/24—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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 in position 2
    • C07D277/82—Nitrogen 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
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/40—Radicals substituted by oxygen atoms
    • C07D307/42—Singly bound 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
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/62—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring 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 atoms of the carbocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/34—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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
    • C07C2601/04—Systems containing only non-condensed rings with a four-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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/18—Systems containing only non-condensed rings with a ring being at least seven-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline

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)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
NO950533A 1992-08-25 1995-02-13 Hydroksyetylaminosulfonamider som retrovirale proteasehemmere NO305478B1 (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US93498492A 1992-08-25 1992-08-25
PCT/US1993/007814 WO1994004492A1 (en) 1992-08-25 1993-08-24 Hydroxyethylamino sulfonamides useful as retroviral protease inhibitors

Publications (3)

Publication Number Publication Date
NO950533L NO950533L (no) 1995-02-13
NO950533D0 true NO950533D0 (no) 1995-02-13
NO305478B1 NO305478B1 (no) 1999-06-07

Family

ID=25466397

Family Applications (2)

Application Number Title Priority Date Filing Date
NO950533A NO305478B1 (no) 1992-08-25 1995-02-13 Hydroksyetylaminosulfonamider som retrovirale proteasehemmere
NO983099A NO307047B1 (no) 1992-08-25 1998-07-03 Nye hydroksyetylaminosulfonamider som er nyttige som retrovirale proteasehemmere, farmasøytisk preparat inneholdende slike, og anvendelse derav

Family Applications After (1)

Application Number Title Priority Date Filing Date
NO983099A NO307047B1 (no) 1992-08-25 1998-07-03 Nye hydroksyetylaminosulfonamider som er nyttige som retrovirale proteasehemmere, farmasøytisk preparat inneholdende slike, og anvendelse derav

Country Status (17)

Country Link
US (16) US5843946A (no)
EP (2) EP0810209B1 (no)
JP (1) JP3657002B2 (no)
KR (2) KR100336699B1 (no)
AT (2) ATE172717T1 (no)
AU (1) AU680635C (no)
CA (1) CA2140929C (no)
DE (3) DE122007000045I2 (no)
DK (2) DK0656887T3 (no)
ES (2) ES2177868T3 (no)
FI (2) FI112471B (no)
FR (1) FR07C0034I2 (no)
LU (1) LU91339I2 (no)
NL (1) NL300283I1 (no)
NO (2) NO305478B1 (no)
PT (1) PT810209E (no)
WO (1) WO1994004492A1 (no)

Families Citing this family (110)

* 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
ATE161828T1 (de) * 1992-08-25 1998-01-15 Searle & Co Sulfonylalkanoylaminohydroxyethylaminosulfonami e verwendbar als retrovirale protease-inhibitoren
US6046190A (en) * 1992-08-25 2000-04-04 G.D. Searle & Co. Hydroxyethylamino sulphonamides 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
US7141609B2 (en) 1992-08-25 2006-11-28 G.D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
CA2142998C (en) * 1992-08-25 2008-01-29 Michael L. Vazquez N-(alkanoylamino-2-hydroxypropyl)-sulfonamides useful as retroviral protease inhibitors
DE122007000045I2 (de) * 1992-08-25 2011-07-21 Gd Searle Llc Gd Searle Llc Darunavir oder pharmazeutisch vertragliche Salze, Hydroxyethylaminosulfonamide verwendbar als InhibiEster oder Prodrugs davon. toren retroviraler Proteasen.
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
US5484926A (en) * 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US5846993A (en) * 1992-12-22 1998-12-08 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
ES2127938T3 (es) * 1993-08-24 1999-05-01 Searle & Co Hidroxietilamino sulfonamidas utiles como inhibidores de proteasas retroviricas.
MX9603909A (es) * 1994-03-07 1997-03-29 Vertex Pharma Derivados de sulfonamida como inhibidores de proteasa aspartilo.
US5527829A (en) * 1994-05-23 1996-06-18 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
DE69637380T2 (de) 1995-01-20 2009-09-17 G.D. Searle Llc, Chicago Bis-sulfonamid-hydroxyethylamino-derivate als inhibitoren retroviraler proteasen
US5831117A (en) 1995-01-20 1998-11-03 G. D. Searle & Co. Method of preparing retroviral protease inhibitor intermediates
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
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
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
CN1149223C (zh) * 1995-03-10 2004-05-12 G·D·瑟尔公司 杂环羰基氨基酸羟乙氨基磺酰胺逆转录病毒蛋白酶抑制剂
US5776971A (en) * 1995-03-10 1998-07-07 G.D. Searle & Co. Heterocyclecarbonyl 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
US6861539B1 (en) 1995-03-10 2005-03-01 G. D. Searle & 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
US6004957A (en) * 1995-06-07 1999-12-21 Vertex Pharmaceuticals, Incorporated Sulfonamide inhibitors of aspartyl protease
JP3974656B2 (ja) * 1995-11-16 2007-09-12 ジー．ディー．サール アンド カンパニー Ｎ−保護／ｎ−置換−ベータ−アミノヒドロキシスルホネート
US6730679B1 (en) 1996-03-22 2004-05-04 Smithkline Beecham Corporation Pharmaceutical formulations
KR20000022226A (ko) 1996-06-25 2000-04-25 그레이엄 브레레톤;레슬리 에드워즈 Hiv 치료에 사용하기 위한 vx478, 지도부딘, ftc 및(또는) 3tc를 포함하는 배합물
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
US5705647A (en) * 1996-09-05 1998-01-06 Agouron Pharmaceuticals, Inc. Intermediates for making HIV-protease inhibitors
US6001851A (en) * 1997-03-13 1999-12-14 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US6084107A (en) * 1997-09-05 2000-07-04 Agouron Pharmaceuticals, Inc. Intermediates for making HIV-protease inhibitors
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
BR9912169A (pt) * 1998-06-19 2001-04-10 Vertex Pharma Inibidores de sulfonamida de protease de aspartil
PT2336134T (pt) 1998-06-23 2016-10-19 The Board Of Trustees Of The Univ Of Illionis Ensaio de aptidão e métodos para reduzir a resistência do hiv à terapia
EP1095022A1 (en) 1998-07-08 2001-05-02 G.D. Searle & Co. Retroviral protease inhibitors
JP2002536298A (ja) * 1999-01-13 2002-10-29 デュポン ファーマシューティカルズ カンパニー Ｈｉｖプロテアーゼ阻害剤としてｎ末端置換ベンジル基を含むビス−アミノ酸スルホンアミド
EP1159278B1 (en) * 1999-02-12 2005-11-30 Vertex Pharmaceuticals Incorporated Inhibitors of aspartyl protease
US6319946B1 (en) * 1999-02-12 2001-11-20 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
CA2386850C (en) * 1999-10-06 2010-03-30 Piet Tom Bert Paul Wigerinck 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
US6391919B1 (en) 2000-01-12 2002-05-21 Bristol-Myers Squibb Pharma Company Bis-amino acid sulfonamides containing substituted benzyl amines HIV protease inhibitors
US6992081B2 (en) 2000-03-23 2006-01-31 Elan Pharmaceuticals, Inc. Compounds to treat Alzheimer's disease
AU2001252958A1 (en) 2000-03-23 2001-10-03 Elan Pharmaceuticals, Inc. Compounds and methods to treat alzheimer's disease
EP1666452A2 (en) 2000-06-30 2006-06-07 Elan Pharmaceuticals, Inc. Compounds to treat Alzheimer's disease
US6846813B2 (en) * 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
US20030096864A1 (en) * 2000-06-30 2003-05-22 Fang Lawrence Y. Compounds to treat alzheimer's disease
CA2410680A1 (en) 2000-06-30 2002-01-10 Elan Pharmaceuticals, Inc. Compounds to treat alzheimer's disease
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
EP1370543B1 (en) * 2001-02-14 2006-10-25 Tibotec Pharmaceuticals Ltd. Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors
CA2452039A1 (en) 2001-06-27 2003-01-09 Elan Pharmaceuticals, Inc. Beta-hydroxyamine derivatives useful in treatment of alzheimer's disease
US20070213407A1 (en) * 2001-06-29 2007-09-13 Elan Pharmaceuticals And Pharmacia & Upjohn Company Llc Compounds to treat Alzheimer's disease
WO2003024932A1 (en) * 2001-09-18 2003-03-27 Bristol-Myers Squibb Company Bis-amino acid sulfonamides as hiv protease inhibitors
CA2462851A1 (en) 2001-10-04 2003-04-10 Elan Pharmaceuticals, Inc. Hydroxypropylamines
US7320878B2 (en) * 2001-11-08 2008-01-22 Tibotec Pharmaceuticals, Ltd. Protease assay for therapeutic drug monitoring
BR0214295A (pt) * 2001-11-19 2004-11-09 Elan Pharm Inc Composto, método para tratar um paciente que tem ou prevenir um paciente de adquirir uma doença ou condição, e, método para produzir um composto
CA2470111A1 (en) * 2001-12-11 2003-06-19 Wyeth Production of chirally pure .alpha.-amino acids and n-sulfonyl .alpha.-amino acids
US7109230B2 (en) * 2002-01-07 2006-09-19 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
MY142238A (en) * 2002-03-12 2010-11-15 Tibotec Pharm Ltd Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors
US7157489B2 (en) 2002-03-12 2007-01-02 The Board Of Trustees Of The University Of Illinois HIV protease inhibitors
US7262208B2 (en) * 2002-04-30 2007-08-28 Elan Pharmaceuticals, Inc. Hydroxypropyl amides for the treatment of Alzheimer's disease
CA2485903C (en) * 2002-05-17 2011-08-16 Tibotec Pharmaceuticals Ltd. Broadspectrum substituted benzisoxazole sulfonamide hiv protease inhibitors
RU2357962C2 (ru) * 2002-09-06 2009-06-10 Элан Фармасьютикалз, Инк. Пролекарственные производные 1,3-диамино-2-гидроксипропана
GB0228410D0 (en) 2002-12-05 2003-01-08 Glaxo Group Ltd Novel Compounds
GB0310593D0 (en) * 2003-05-08 2003-06-11 Leuven K U Res & Dev Peptidic prodrugs
GB0314476D0 (en) * 2003-06-20 2003-07-23 Glaxo Group Ltd Compounds
US7273533B2 (en) * 2003-11-19 2007-09-25 Tokyo Electron Limited Plasma processing system with locally-efficient inductive plasma coupling
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
JP4818124B2 (ja) 2003-12-23 2011-11-16 テイボテク・フアーマシユーチカルズ・リミテツド （３Ｒ，３ａＳ，６ａＲ）−ヘキサヒドロフロ〔２，３−ｂ〕フラン−３−イル（１Ｓ，１Ｒ）−３−〔〔（４−アミノフェニル）スルホニル〕（イソブチル）アミノ〕−１−ベンジル−２−ヒドロキシプロピルカルバマートの製造方法
WO2005087728A1 (en) 2004-03-11 2005-09-22 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
AU2005244121B2 (en) * 2004-05-07 2012-01-19 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
JP2008533017A (ja) * 2005-03-11 2008-08-21 スミスクライン ビーチャム コーポレーション Ｈｉｖプロテアーゼ阻害薬
US20110178092A1 (en) * 2005-06-22 2011-07-21 Akbar Ali HIV-1 Protease Inhibitors
ES2426345T3 (es) * 2005-07-20 2013-10-22 Eli Lilly And Company Compuesto unidos en posición 1-amino
ES2628730T3 (es) * 2006-09-21 2017-08-03 Taimed Biologics, Inc. Inhibidores de proteasa
WO2008132154A1 (en) 2007-04-27 2008-11-06 Tibotec Pharmaceuticals Ltd. Methods for the preparation of n-isobutyl-n-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide derivatives
CN103479604B (zh) * 2007-07-30 2016-08-10 阿迪生物科学公司 作为mek抑制剂的包括多晶型物的n-(芳氨基)磺酰胺衍生物和组合物、其使用方法和制备方法
WO2009055006A1 (en) * 2007-10-26 2009-04-30 Concert Pharmaceuticals, Inc. Deuterated darunavir
US8592487B2 (en) 2007-10-26 2013-11-26 Concert Pharmaceuticals, Inc. Deuterated darunavir
PT2231628E (pt) * 2008-01-04 2015-12-29 Gilead Sciences Inc Inibidores de citocromo p450
US8921415B2 (en) 2009-01-29 2014-12-30 Mapi Pharma Ltd. Polymorphs of darunavir
WO2010127272A2 (en) * 2009-04-30 2010-11-04 Concert Pharmaceuticals, Inc. Hydroxyethylamino sulfonamide derivatives
BR112012009956A2 (pt) 2009-10-30 2015-09-29 Lupin Ltd um novo processo para a preparação de darunavir e etanolato darunavir de tamanho de partícula.
WO2011061590A1 (en) 2009-11-17 2011-05-26 Hetero Research Foundation Novel carboxamide derivatives as hiv inhibitors
PL2528923T3 (pl) 2010-01-28 2015-01-30 Mapi Pharma Ltd Sposób wytwarzania darunawiru i pochodnych darunawiru
GB201118182D0 (en) 2011-10-21 2011-12-07 Jagotec Ag Improvements in or relating to organic compounds
WO2013108105A2 (en) 2012-01-18 2013-07-25 Aurobindo Pharma Limited Novel solvates of darunavir
EP3795572B1 (en) 2012-07-24 2023-11-15 Laurus Labs Limited Darunavir propionate solvate
HK1220390A1 (zh) 2013-08-29 2017-05-05 Teva Pharmaceutical Industries Ltd. 包括恩曲他滨，替诺福韦，达芦那韦和利托那韦的单位剂型以及包含达芦那韦和利托那韦的单体片剂
EP3129009A1 (en) 2014-04-08 2017-02-15 Teva Pharmaceutical Industries Ltd Unit dosage form comprising emtricitabine, tenofovir, darunavir and ritonavir
US20160075643A1 (en) 2014-09-16 2016-03-17 Zcl Chemicals Limited Novel process to prepare intermediates of hiv-protease inhibitors thereof
US9738664B2 (en) 2014-10-29 2017-08-22 Wisconsin Alumni Research Foundation Boronic acid inhibitors of HIV protease
WO2016193481A1 (en) 2015-06-05 2016-12-08 Amneal Pharmaceuticals Company Gmbh Process for the preparation of darunavir
US11045423B2 (en) 2016-08-08 2021-06-29 Hetero Labs Limited Anti-retroviral compositions
WO2018029565A1 (en) 2016-08-08 2018-02-15 Hetero Labs Limited A multi-class anti-retroviral composition
EP3532478B1 (en) 2016-10-27 2021-05-26 Gilead Sciences, Inc. Crystalline form of darunavir free base
CN108558808B (zh) * 2018-05-22 2020-05-05 中国医学科学院医药生物技术研究所 一种酰胺类衍生物或其药学上可接受的盐及其制备方法和应用
CN111205206B (zh) * 2020-02-13 2021-10-22 中国医学科学院医药生物技术研究所 一种包含氨基酸连接链的羰基化合物或其药学上可接受的盐及其制备方法和应用
US12083099B2 (en) 2020-10-28 2024-09-10 Accencio LLC Methods of treating symptoms of coronavirus infection with viral protease inhibitors
CN113277991B (zh) * 2021-02-03 2022-07-12 中国医学科学院医药生物技术研究所 一种含氮杂环氨基衍生物及其制备方法和一种抗hiv-1的药物
CN116693595B (zh) * 2023-06-07 2025-09-02 中国医学科学院医药生物技术研究所 一种雷公藤甲素衍生物及其制备方法和应用

Family Cites Families (110)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US725A (en) 1838-05-04 Cabbiage-spbing
DE264795C (no) *
GB1435386A (en) 1973-07-26 1976-05-12 Made Labor Sa Cyanoglutaric acid derivatives
DE2352452A1 (de) 1973-10-19 1975-04-30 Made Labor Sa 2-cyan-3-dialcoximethyl-alkylglutarate sowie verfahren zur herstellung dieser verbindungen und ihrer derivate
JPS5041814Y1 (no) 1975-03-06 1975-11-27
US5142056A (en) 1989-05-23 1992-08-25 Abbott Laboratories Retroviral protease inhibiting compounds
EP0068378B1 (en) 1981-06-26 1986-03-05 Schering Corporation Novel imidazo(1,2-a)pyridines and pyrazines, processes for their preparation and pharmaceutical compositions containing them
EP0104041B1 (en) 1982-09-15 1988-07-27 Aktiebolaget Hässle Enzyme inhibitors
EP0114993B1 (en) 1982-12-27 1990-05-16 Merck & Co. Inc. Renin inhibitory tripeptides
US4668770A (en) 1982-12-27 1987-05-26 Merck & Co., Inc. Renin inhibitory tripeptides
EP0118223A1 (en) 1983-02-07 1984-09-12 Aktiebolaget Hässle Enzyme inhibitors
JPS59227851A (ja) * 1983-06-09 1984-12-21 Sankyo Co Ltd レニン阻害作用を有するペプチド類
US4514391A (en) 1983-07-21 1985-04-30 E. R. Squibb & Sons, Inc. Hydroxy substituted peptide compounds
US4477441A (en) 1983-09-14 1984-10-16 Merck & Co., Inc. Renin inhibitors containing a C-terminal disulfide cycle
US4645759A (en) 1984-06-22 1987-02-24 Abbott Laboratories Renin inhibiting compounds
US4616088A (en) 1984-10-29 1986-10-07 E. R. Squibb & Sons, Inc. Amino acid ester and amide renin inhibitor
DE3689223T2 (de) 1985-05-15 1994-03-03 Amoco Corp Cytidinanaloga.
US4826815A (en) 1985-05-17 1989-05-02 Abbott Laboratories Renin inhibiting compounds
US4668769A (en) 1985-08-02 1987-05-26 Hoover Dennis J Oxa- and azahomocyclostatine polypeptides
US4599198A (en) 1985-08-02 1986-07-08 Pfizer Inc. Intermediates in polypeptide synthesis
CA1282549C (en) 1985-11-12 1991-04-02 Eric M. Gordon Aminocarbonyl renin inhibitors
CA1297631C (en) 1985-12-23 1992-03-17 Sesha I. Natarajan Ureido renin inhibitors
US4757050A (en) * 1985-12-23 1988-07-12 E. R. Squibb Sons, Inc. Ureido renin inhibitors
US4757060A (en) * 1986-03-04 1988-07-12 Bristol-Myers Company Non-steroidal anti-inflammatory compositions protected against gastrointestinal injury with a combination of certain H1 and H2, receptor blockers
US4880938A (en) 1986-06-16 1989-11-14 Merck & Co., Inc. Amino acid analogs
DE3635109A1 (de) 1986-10-15 1988-04-21 Patent Treuhand Ges Fuer Elektrische Gluehlampen Mbh Schaltungsanordnung zum betrieb von niedervolt-halogengluehlampen
DE3635907A1 (de) * 1986-10-22 1988-04-28 Merck Patent Gmbh Hydroxy-aminosaeurederivate
CH676988A5 (no) 1987-01-21 1991-03-28 Sandoz Ag
USH725H (en) 1987-02-26 1990-01-02 E. R. Squibb & Sons, Inc. Ureido amino and imino acids, compositions and methods for use
GB8707412D0 (en) 1987-03-27 1987-04-29 Fujisawa Pharmaceutical Co Peptide compounds
USH1649H (en) 1987-07-31 1997-05-06 Barrish; Joel C. HIV protease inhibitor combinations
DE3830825A1 (de) 1987-09-15 1989-03-23 Sandoz Ag Hydrophile reninhemmer, ihre herstellung und verwendung
CA1328333C (en) * 1988-03-04 1994-04-05 Quirico Branca Amino acid derivatives
IL89900A0 (en) 1988-04-12 1989-12-15 Merck & Co Inc Hiv protease inhibitors useful for the treatment of aids and pharmaceutical compositions containing them
US4977277A (en) 1988-05-09 1990-12-11 Abbott Laboratories Functionalized peptidyl aminodiols and -triols 4-amino-5-cyclohexyl-3-hydroxy-1,2-oxopentane and derivatives thereof
IL90218A0 (en) 1988-05-13 1989-12-15 Abbott Lab Retroviral protease inhibitors
DE3816890A1 (de) * 1988-05-18 1989-11-30 Schaeffler Waelzlager Kg Ausruecklagereinrichtung fuer eine gedrueckte kraftfahrzeugkupplung
CA1340588C (en) 1988-06-13 1999-06-08 Balraj Krishan Handa Amino acid derivatives
IL91307A0 (en) 1988-08-24 1990-03-19 Merck & Co Inc Hiv protease inhibitors and pharmaceutical compositions for the treatment of aids containing them
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
US5268374A (en) * 1988-10-04 1993-12-07 Abbott Laboratories Non-peptide renin inhibitors
DE3840289A1 (de) * 1988-11-30 1990-05-31 Merck Patent Gmbh Aminosaeurederivate
US4969530A (en) * 1989-03-03 1990-11-13 Kopczynski John F All-terrain vehicle
CA2012306A1 (en) 1989-03-28 1990-09-28 Werner Neidhart Amino acid derivatives
CA2012901A1 (en) * 1989-04-05 1990-10-05 Quirico Branca Amino acid derivatives
JP2701932B2 (ja) 1989-04-10 1998-01-21 サントリー株式会社 タンパク質分解酵素阻害剤
DE3912829A1 (de) 1989-04-19 1990-10-25 Bayer Ag Verwendung von renininhibitorischen peptiden als mittel gegen retroviren
US5696270A (en) 1989-05-23 1997-12-09 Abbott Laboratories Intermediate for making retroviral protease inhibiting compounds
EP0428849A3 (en) 1989-09-28 1991-07-31 Hoechst Aktiengesellschaft Retroviral protease inhibitors
GB8927913D0 (en) 1989-12-11 1990-02-14 Hoffmann La Roche Amino acid derivatives
CA2032259A1 (en) 1989-12-18 1991-06-19 Wayne J. Thompson Hiv protease inhibitors useful for the treatment of aids
US5122514A (en) * 1990-04-23 1992-06-16 Abbott Laboratories Psoriasis treatment
TW225540B (no) * 1990-06-28 1994-06-21 Shionogi & Co
US5223615A (en) * 1990-06-28 1993-06-29 Shionogi & Co., Ltd. Dipeptide derivatives
US5272268A (en) * 1990-06-28 1993-12-21 Shionogi & Co., Ltd. Dipeptide derivatives
WO1992000750A1 (en) 1990-07-06 1992-01-23 Smithkline Beecham Corporation Retroviral protease inhibitors
GB9024938D0 (en) 1990-11-16 1991-01-02 Process Dev Ltd Filtering
ES2243959T3 (es) 1990-11-19 2005-12-01 Monsanto Company Inhibidores de proteasas retrovirales.
WO1993023388A1 (en) 1992-05-20 1993-11-25 G.D. Searle & Co. Method for making intermediates useful in synthesis of retroviral protease inhibitors
WO1992008699A1 (en) * 1990-11-19 1992-05-29 Monsanto Company Retroviral protease inhibitors
US5475013A (en) 1990-11-19 1995-12-12 Monsanto Company Retroviral protease inhibitors
KR100268694B1 (ko) 1991-10-11 2000-10-16 미리암 디. 메코너헤이, 블레어큐. 퍼거슨 레트로바이러스 프로테아제 억제제로 유용한 시클릭 우레아 및 유사체
WO1993008184A1 (en) 1991-10-23 1993-04-29 Merck & Co., Inc. Hiv protease inhibitors
DK0541168T3 (da) 1991-11-08 1998-05-11 Merck & Co Inc HIV-proteaseinhibitorer, som er egnede til behandling af AIDS
US5413999A (en) 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
ATE116640T1 (de) 1992-03-13 1995-01-15 Bio Mega Boehringer Ingelheim Substituierte pipecoline-säurederivate als hiv- protease-hemmer.
US5559256A (en) 1992-07-20 1996-09-24 E. R. Squibb & Sons, Inc. Aminediol 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
US7141609B2 (en) 1992-08-25 2006-11-28 G.D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
CA2142998C (en) 1992-08-25 2008-01-29 Michael L. Vazquez N-(alkanoylamino-2-hydroxypropyl)-sulfonamides useful as retroviral protease inhibitors
ATE161828T1 (de) 1992-08-25 1998-01-15 Searle & Co Sulfonylalkanoylaminohydroxyethylaminosulfonami e verwendbar als retrovirale protease-inhibitoren
US6046190A (en) 1992-08-25 2000-04-04 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
US6022994A (en) 1992-08-25 2000-02-08 G. D. Searle &. Co. Succinoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
DE122007000045I2 (de) 1992-08-25 2011-07-21 Gd Searle Llc Gd Searle Llc Darunavir oder pharmazeutisch vertragliche Salze, Hydroxyethylaminosulfonamide verwendbar als InhibiEster oder Prodrugs davon. toren retroviraler Proteasen.
US5830897A (en) 1992-08-27 1998-11-03 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
AU4812393A (en) 1992-09-03 1994-03-29 Biochem Pharma Inc. Use of rapamycin in the treatment of aids
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
US6869925B1 (en) 1992-09-09 2005-03-22 Amgen Inc. Inhibition of retrovirus infection
US5376633A (en) 1992-09-30 1994-12-27 Lezdey; John Method for deactivating viruses in blood component containers
US5578606A (en) 1992-10-30 1996-11-26 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
US5484926A (en) 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US5514801A (en) 1992-12-29 1996-05-07 Monsanto Company Cyclic sulfone containing retroviral protease inhibitors
WO1994026749A1 (en) 1993-05-14 1994-11-24 Merck & Co., Inc. Hiv protease inhibitors
ES2127938T3 (es) 1993-08-24 1999-05-01 Searle & Co Hidroxietilamino sulfonamidas utiles como inhibidores de proteasas retroviricas.
US5567592A (en) 1994-02-02 1996-10-22 Regents Of The University Of California Screening method for the identification of bioenhancers through the inhibition of P-glycoprotein transport in the gut of a mammal
UA49803C2 (uk) 1994-06-03 2002-10-15 Дж.Д. Сьорль Енд Ко Спосіб лікування ретровірусних інфекцій
US5691372A (en) 1995-04-19 1997-11-25 Vertex Pharmaceuticals Incorporated Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease
GB9509321D0 (en) 1995-05-09 1995-06-28 Zylepsis Ltd Methods of and substances for inhibiting oxidative enzymes
US6037157A (en) 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
KR980009238A (ko) 1995-07-28 1998-04-30 우에노 도시오 설포닐아미노산 유도체
HU226203B1 (en) 1996-01-26 2008-06-30 Virco B V B A Method for determining of the chemotherapy of patients who are hiv positive based on the phenotypic drug sensitivity of human hiv strains
ES2175355T3 (es) 1996-01-29 2002-11-16 Virologic Inc Composiciones y metodos para determinar la susceptibilidad y la resistencia a farmacos antivirales y rastreo de farmacos antivirales.
US5837464A (en) 1996-01-29 1998-11-17 Virologic, Inc. Compositions and methods for determining anti-viral drug susceptibility and resistance and anti-viral drug screening
US6191165B1 (en) 1996-05-31 2001-02-20 Allelix Neuroscience Inc. Pharmaceutical for treatment of neurological and neuropsychiatric disorders
US6210875B1 (en) 1996-08-22 2001-04-03 Northwestern University Process of determining the efficacy of drug treatment in HIV infected subjects
US6245809B1 (en) 1996-12-09 2001-06-12 Cor Therapeutics Inc. Integrin antagonists
ZA984514B (en) 1997-05-29 1998-11-30 Merck & Co Inc Hiv protease inhibitor
GB9712253D0 (en) 1997-06-13 1997-08-13 Glaxo Group Ltd Antiviral compound
AU2010299A (en) 1997-12-24 1999-07-19 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
US6251874B1 (en) 1998-03-26 2001-06-26 Research Institute For Genetic And Human Therapy (R.I.G.H.T.) Method of inhibiting human immunodeficiency virus using hydroxurea and a reverse transcriptase inhibitor in vivo
PT2336134T (pt) 1998-06-23 2016-10-19 The Board Of Trustees Of The Univ Of Illionis Ensaio de aptidão e métodos para reduzir a resistência do hiv à terapia
EP1095022A1 (en) 1998-07-08 2001-05-02 G.D. Searle & Co. Retroviral protease inhibitors
MXPA01012270A (es) 1999-05-28 2003-06-24 Virco Nv Nuevos perfiles mutacionales en la transcriptasa reversa de vih-1 correlacionadas con resistencia fenotipica a farmacos.
GB9913079D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
US6869759B1 (en) 1999-06-22 2005-03-22 Virologic, Inc. Means and methods for monitoring protease inhibitor antiretroviral therapy and guiding therapeutic decisions in the treatment of HIV/AIDS
US6943170B2 (en) 2002-11-14 2005-09-13 Bristol-Myers Squibb Company N-cycloalkylglycines as HIV protease inhibitors
US6890942B2 (en) 2003-05-16 2005-05-10 Bristol-Myers Squibb Company Acyl sulfonamides as inhibitors of HIV integrase

Also Published As

Publication number Publication date
RU95106624A (ru) 1996-12-10
KR100296463B1 (ko) 2001-10-24
US6500832B1 (en) 2002-12-31
US6335460B1 (en) 2002-01-01
ES2177868T3 (es) 2002-12-16
FR07C0034I1 (no) 2007-06-07
US6172082B1 (en) 2001-01-09
LU91339I2 (fr) 2007-07-23
AU680635C (en) 2007-05-17
US20040229922A1 (en) 2004-11-18
NO950533L (no) 1995-02-13
KR950702960A (ko) 1995-08-23
KR100336699B1 (ko) 2002-05-13
WO1994004492A1 (en) 1994-03-03
EP0656887B1 (en) 1998-10-28
FI119427B (fi) 2008-11-14
JPH08501288A (ja) 1996-02-13
FR07C0034I2 (fr) 2008-05-09
EP0810209A3 (en) 1998-12-02
DK0810209T3 (da) 2002-08-12
US20040044047A1 (en) 2004-03-04
EP0656887A1 (en) 1995-06-14
FI112471B (fi) 2003-12-15
US7115618B2 (en) 2006-10-03
CA2140929C (en) 2006-09-12
DK0656887T3 (da) 1999-07-05
US5786483A (en) 1998-07-28
NO307047B1 (no) 2000-01-31
NO983099D0 (no) 1998-07-03
DE69332002T2 (de) 2002-12-19
US5744481A (en) 1998-04-28
US20070078173A1 (en) 2007-04-05
US20090023664A1 (en) 2009-01-22
US6455581B1 (en) 2002-09-24
DE122007000045I2 (de) 2011-07-21
US5843946A (en) 1998-12-01
US6846954B2 (en) 2005-01-25
FI950650A0 (fi) 1995-02-14
NO305478B1 (no) 1999-06-07
USRE43596E1 (en) 2012-08-21
DE69332002D1 (de) 2002-07-11
FI20012317L (fi) 2001-11-27
DE69321845D1 (en) 1998-12-03
NL300283I1 (nl) 2007-09-03
DE122007000045I1 (de) 2007-08-16
AU680635B2 (en) 1997-08-07
EP0810209A2 (en) 1997-12-03
FI950650L (fi) 1995-02-14
AU5347494A (en) 1994-03-15
US6472407B1 (en) 2002-10-29
US7320983B2 (en) 2008-01-22
US6534493B1 (en) 2003-03-18
ATE218541T1 (de) 2002-06-15
PT810209E (pt) 2002-09-30
NO983099L (no) 1995-02-13
ES2123065T3 (es) 1999-01-01
DE69321845T2 (de) 1999-04-29
ATE172717T1 (de) 1998-11-15
EP0810209B1 (en) 2002-06-05
US6060476A (en) 2000-05-09
CA2140929A1 (en) 1994-02-26
JP3657002B2 (ja) 2005-06-08
US7829564B2 (en) 2010-11-09
USRE43802E1 (en) 2012-11-13

Similar Documents

Publication Publication Date Title
NO950533L (no) Hydroksyetylaminosulfonamider som er nyttige som retrovirale proteasehemmere
ATE136888T1 (de) Retrovirale proteaseinhibitoren
DK0727419T3 (da) Mellemprodukter til fremstilling af forbindelser, som inhiberer retroviral protease
BR9206623A (pt) Uréias cíclicas e análogas úteis como inibidoras da protease retroviral
DE69126987D1 (de) Retrovirale protease-inhibitoren
AU667593B2 (en) Inhibitors of HIV protease useful for the treatment of AIDS
DE69131317D1 (de) HIV-Proteaseinhibitoren
DK0604186T3 (da) HIV-proteaseinhibitorer, som er egnede til behandling af AIDS
FI960206A0 (fi) Menetelmä HIV-proteaasi-inhibiittoreiden valmistamiseksi

Legal Events

Date Code Title Description
MK1K Patent expired