KR100296463B1 - 레트로바이러스프로테아제저해제로서유용한히드록시에틸아미노술폰아미드 - Google Patents

레트로바이러스프로테아제저해제로서유용한히드록시에틸아미노술폰아미드 Download PDF

Info

Publication number
KR100296463B1
KR100296463B1 KR1019950700563A KR19950700563A KR100296463B1 KR 100296463 B1 KR100296463 B1 KR 100296463B1 KR 1019950700563 A KR1019950700563 A KR 1019950700563A KR 19950700563 A KR19950700563 A KR 19950700563A KR 100296463 B1 KR100296463 B1 KR 100296463B1
Authority
KR
South Korea
Prior art keywords
amino
phenylmethyl
compound
hydroxy
propyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
KR1019950700563A
Other languages
English (en)
Korean (ko)
Other versions
KR950702960A (ko
Inventor
마이클엘.바즈케즈
리챠드에이.뮤엘러
존제이.탈리
다니엘케트만
가리에이.데크레센조
존엔.프레스코스
Original Assignee
죤 에이치. 뷰센
몬산토컴퍼니
윌리암스 로저 에이
지.디. 썰 앤드 컴파니
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=KR100296463(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 죤 에이치. 뷰센, 몬산토컴퍼니, 윌리암스 로저 에이, 지.디. 썰 앤드 컴파니 filed Critical 죤 에이치. 뷰센
Publication of KR950702960A publication Critical patent/KR950702960A/ko
Application granted granted Critical
Publication of KR100296463B1 publication Critical patent/KR100296463B1/ko
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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
    • 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
    • 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
    • C07C311/30—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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Virology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
KR1019950700563A 1992-08-25 1993-08-24 레트로바이러스프로테아제저해제로서유용한히드록시에틸아미노술폰아미드 Expired - Lifetime KR100296463B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US93498492A 1992-08-25 1992-08-25
US07/934984 1992-08-25
PCT/US1993/007814 WO1994004492A1 (en) 1992-08-25 1993-08-24 Hydroxyethylamino sulfonamides useful as retroviral protease inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020007012894A Division KR100336699B1 (ko) 1992-08-25 1993-08-24 레트로바이러스 프로테아제 저해제로서 유용한히드록시에틸아미노 술폰아미드

Publications (2)

Publication Number Publication Date
KR950702960A KR950702960A (ko) 1995-08-23
KR100296463B1 true KR100296463B1 (ko) 2001-10-24

Family

ID=25466397

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1019950700563A Expired - Lifetime KR100296463B1 (ko) 1992-08-25 1993-08-24 레트로바이러스프로테아제저해제로서유용한히드록시에틸아미노술폰아미드
KR1020007012894A Expired - Lifetime KR100336699B1 (ko) 1992-08-25 1993-08-24 레트로바이러스 프로테아제 저해제로서 유용한히드록시에틸아미노 술폰아미드

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020007012894A Expired - Lifetime KR100336699B1 (ko) 1992-08-25 1993-08-24 레트로바이러스 프로테아제 저해제로서 유용한히드록시에틸아미노 술폰아미드

Country Status (17)

Country Link
US (16) US5843946A (enExample)
EP (2) EP0810209B1 (enExample)
JP (1) JP3657002B2 (enExample)
KR (2) KR100296463B1 (enExample)
AT (2) ATE172717T1 (enExample)
AU (1) AU680635C (enExample)
CA (1) CA2140929C (enExample)
DE (3) DE122007000045I2 (enExample)
DK (2) DK0810209T3 (enExample)
ES (2) ES2123065T3 (enExample)
FI (2) FI112471B (enExample)
FR (1) FR07C0034I2 (enExample)
LU (1) LU91339I2 (enExample)
NL (1) NL300283I1 (enExample)
NO (2) NO305478B1 (enExample)
PT (1) PT810209E (enExample)
WO (1) WO1994004492A1 (enExample)

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
WO1994004491A1 (en) * 1992-08-25 1994-03-03 G.D. Searle & Co. N-(alkanoylamino-2-hydroxypropyl)-sulfonamides useful as retroviral protease inhibitors
US5968942A (en) 1992-08-25 1999-10-19 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US6046190A (en) * 1992-08-25 2000-04-04 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
ES2123065T3 (es) 1992-08-25 1999-01-01 Searle & Co Hidroxietilamino-sulfonamidas utiles como inhibidores de proteasas retroviricas.
US7141609B2 (en) * 1992-08-25 2006-11-28 G.D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
RU2146668C1 (ru) * 1992-08-25 2000-03-20 Джи Ди Сирл энд Компани Сульфонилалканоиламино-гидроксиэтиламино-сульфонамидное соединение, фармацевтические композиции и способы лечения и ингибирования ретровирусных протеаз
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
EP0715618B1 (en) * 1993-08-24 1998-12-16 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
ATE184594T1 (de) * 1994-03-07 1999-10-15 Vertex Pharma Sulfonamidderivate als aspartylprotease- inhibitoren
US5527829A (en) * 1994-05-23 1996-06-18 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US6143747A (en) 1995-01-20 2000-11-07 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
US6861539B1 (en) 1995-03-10 2005-03-01 G. D. Searle & Co. Bis-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
DE69625183T2 (de) * 1995-03-10 2003-10-09 G.D. Searle & Co., Chicago Heterocyclocarbonyl-aminosäure-hydroxyethylamino-sulfonamid inhibitoren retroviraler proteasen
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
US7339078B2 (en) 1995-03-10 2008-03-04 G.D. Searle Llc 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
US5776971A (en) * 1995-03-10 1998-07-07 G.D. Searle & Co. Heterocyclecarbonyl 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
ATE192432T1 (de) 1995-11-16 2000-05-15 Searle & Co N-geschützte/n-substituierte beta- aminohydroxysulfonate
US6730679B1 (en) 1996-03-22 2004-05-04 Smithkline Beecham Corporation Pharmaceutical formulations
JP2000515852A (ja) 1996-06-25 2000-11-28 グラクソ、グループ、リミテッド Ｈｉｖの治療に使用するためのｖｘ４７８、ジドブジン、ｆｔｃおよび／または３ｔｃを含んでなる組合わせ
US5925759A (en) 1996-09-05 1999-07-20 Agouron Pharmaceuticals, Inc. Methods of making HIV-protease inhibitors and intermediates for making HIV-protease inhibitors
US5705647A (en) * 1996-09-05 1998-01-06 Agouron Pharmaceuticals, Inc. 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
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
ATE500823T1 (de) 1998-06-23 2011-03-15 Us Of America Represented By The Secretary Dept Of Health And Human Services Arzneimittel zur behandlung von hiv-infizierten säugetieren
US6538006B1 (en) * 1998-07-08 2003-03-25 Pharmacia Corporation Retroviral protease inhibitors
BR0007854A (pt) * 1999-01-13 2002-01-15 Du Pont Pharm Co Compostos sulfonamidas bis-aminoácidos inibidores de protease de hiv, composição farmacêutica e método de tratamento de infecções por hiv
ES2254156T3 (es) * 1999-02-12 2006-06-16 Vertex Pharmaceuticals Incorporated Inhibidores de aspartil-proteasa.
TNSN00027A1 (fr) 1999-02-12 2005-11-10 Vertex Pharma Inhibiteurs de l'aspartyle 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
BR0014602A (pt) * 1999-10-06 2002-06-11 Tibotec Pharm Ltd Hexaidrofluoro'2,3-bifuran-3-il-n-{3'(1,3-benzodioxol- 5ilsulfonil)(isobutil)amino-1 -benzil-2-hidroxipropil}carbamato como inibidor da protease retroviral
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
ES2275675T3 (es) 2000-03-23 2007-06-16 Elan Pharmaceuticals, Inc. Compuestos y metodos para tratar la enfermedad de alzheimer.
EP1666452A2 (en) 2000-06-30 2006-06-07 Elan Pharmaceuticals, Inc. Compounds to treat Alzheimer's disease
US20030096864A1 (en) * 2000-06-30 2003-05-22 Fang Lawrence Y. Compounds to treat alzheimer's disease
ES2252257T3 (es) 2000-06-30 2006-05-16 Elan Pharmaceuticals, Inc. Compuestos para tratar la enfermedad de alzheimer.
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
US6846813B2 (en) 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
US6617310B2 (en) 2000-07-19 2003-09-09 Bristol-Myers Squibb Pharma Company Phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines
DK1370543T3 (da) 2001-02-14 2007-02-19 Tibotec Pharm Ltd Bredspektrede 2-(substitueret amino) benzothiazol- sulfonamid-HIV-proteaseinhibitorer
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
US6562848B1 (en) * 2001-09-18 2003-05-13 Bristol-Myers Squibb Company Bis-amino acid sulfonamides as HIV protease inhibitors
CA2462851A1 (en) 2001-10-04 2003-04-10 Elan Pharmaceuticals, Inc. Hydroxypropylamines
ATE389029T1 (de) * 2001-11-08 2008-03-15 Tibotec Pharm Ltd Protease assay zur kontrolle medikamentöser therapie
MXPA04004772A (es) * 2001-11-19 2005-06-06 Elan Pharm Inc Piperidinas y piperazinas 3,4-disustituidas, 3,5-disustituidas y 3,4,5-sustituidas.
MXPA04005366A (es) * 2001-12-11 2004-09-27 Wyeth Corp Produccion de alfa-aminoacidos de n-sulfonilo y alfa-aminoacidos quiralmente puros.
EP1483254A4 (en) * 2002-01-07 2005-06-08 Sequoia Pharmaceuticals INHIBITORS OF ANTI-RESISTANCE RETROVIRAL PROTEASE
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
WO2004058686A1 (en) * 2002-04-30 2004-07-15 Elan Pharmaceuticals, Inc. Hydroxypropyl amides for the treatment of alzheimer’s disease
EP1517899B1 (en) * 2002-05-17 2007-08-29 Tibotec Pharmaceuticals Ltd. Broadspectrum substituted benzisoxazole sulfonamide hiv protease inhibitors
BR0314071A (pt) * 2002-09-06 2005-07-05 Pharmacia & Upjohn Co Llc Derivados de pró-droga de 1,3-diamino-2-hidroxipropano
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
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
CA2559328A1 (en) 2004-03-11 2005-09-22 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
EP1750696B1 (en) 2004-05-07 2013-06-26 Sequoia Pharmaceuticals Inc RETROVIRAL PROTEASE INHIBITORS RESISTING THEIR RESISTANCE
WO2006104646A1 (en) * 2005-03-11 2006-10-05 Smithkline Beecham Corporation Hiv protease inhibitors
US20110178092A1 (en) * 2005-06-22 2011-07-21 Akbar Ali HIV-1 Protease Inhibitors
WO2007015805A1 (en) * 2005-07-20 2007-02-08 Eli Lilly And Company 1-amino linked compounds
CA2664118A1 (en) * 2006-09-21 2008-07-03 Ambrilia Biopharma Inc. Protease inhibitors
SI2152667T1 (sl) 2007-04-27 2011-06-30 Tibotec Pharm Ltd Postopki za pripravo N-izobutil-N(2-hidroksi-3-amino-4-fenilbutil)-p- nitrobenzensulfonilamidnih derivatov
KR20100092424A (ko) * 2007-07-30 2010-08-20 아디아 바이오사이언스즈 인크. 다형체를 포함하는, ｍｅｋ의 억제제로서의 ｎ-(아릴아미노) 술폰아미드의 유도체 및 조성물, 사용 방법 및 이의 제조 방법
US8592487B2 (en) 2007-10-26 2013-11-26 Concert Pharmaceuticals, Inc. Deuterated darunavir
US20090131363A1 (en) * 2007-10-26 2009-05-21 Harbeson Scott L Deuterated darunavir
CA2710679A1 (en) * 2008-01-04 2009-07-16 Gilead Sciences, Inc. Inhibitors of cytochrome 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
EP2493891A2 (en) 2009-10-30 2012-09-05 Lupin Limited A novel process for preparation of darunavir and darunavir ethanolate of fine particle size
WO2011061590A1 (en) 2009-11-17 2011-05-26 Hetero Research Foundation Novel carboxamide derivatives as hiv inhibitors
BR112012018862A2 (pt) 2010-01-28 2015-10-13 Mapi Pharma Ltd processo para a preparação de darunavir e intermediários de darunavir
GB201118182D0 (en) 2011-10-21 2011-12-07 Jagotec Ag Improvements in or relating to organic compounds
EP2804869B1 (en) 2012-01-18 2019-06-12 Aurobindo Pharma Limited Novel solvates of darunavir
EP3795572B1 (en) 2012-07-24 2023-11-15 Laurus Labs Limited Darunavir propionate solvate
WO2015028875A2 (en) 2013-08-29 2015-03-05 Teva Pharmaceuticals Industries Ltd. Unit dosage form comprising emtricitabine, tenofovir, darunavir and ritonavir and a monolithic tablet comprising darunavir and ritonavir
TW201622731A (zh) 2014-04-08 2016-07-01 泰瓦藥品工業有限公司 包含恩曲他濱（Ｅｍｔｒｉｃｉｔａｂｉｎｅ）、替諾福韋（Ｔｅｎｏｆｏｖｉｒ）、地瑞那韋（Ｄａｒｕｎａｖｉｒ）及利托那韋（Ｒｉｔｏｎａｖｉｒ）之單位劑型以及包含地瑞那韋及利托那韋之單層錠劑
US20160075643A1 (en) 2014-09-16 2016-03-17 Zcl Chemicals Limited Novel process to prepare intermediates of hiv-protease inhibitors thereof
EP3212196A4 (en) 2014-10-29 2018-07-11 Wisconsin Alumni Research Foundation Boronic acid inhibitors of hiv protease
EP3303343A1 (en) 2015-06-05 2018-04-11 Amneal Pharmaceuticals Company GmbH Process for the preparation of darunavir
US20190175511A1 (en) 2016-08-08 2019-06-13 Hetero Labs Limited A Multi-Class Anti-Retroviral Composition
EP3496718A4 (en) 2016-08-08 2020-01-22 Hetero Labs Limited ANTIRETROVIRAL COMPOSITIONS
US10407438B2 (en) 2016-10-27 2019-09-10 Gilead Sciences, Inc. Crystalline forms of darunavir
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0264795A2 (de) * 1986-10-22 1988-04-27 MERCK PATENT GmbH Aminosäurederivate

Family Cites Families (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US725A (en) 1838-05-04 Cabbiage-spbing
DE264795C (enExample) *
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 (enExample) 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
DE3377497D1 (en) 1982-09-15 1988-09-01 Haessle Ab Enzyme inhibitors
US4668770A (en) 1982-12-27 1987-05-26 Merck & Co., Inc. Renin inhibitory tripeptides
DE3381565D1 (de) 1982-12-27 1990-06-21 Merck & Co Inc Reninhemmende tripeptide.
AU573735B2 (en) 1983-02-07 1988-06-23 Aktiebolaget Hassle Peptide analogue 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
JPH0723393B2 (ja) 1985-05-15 1995-03-15 アモコ・コーポレーション シチジン同族体
US4826815A (en) 1985-05-17 1989-05-02 Abbott Laboratories Renin inhibiting compounds
US4599198A (en) 1985-08-02 1986-07-08 Pfizer Inc. Intermediates in polypeptide synthesis
US4668769A (en) 1985-08-02 1987-05-26 Hoover Dennis J Oxa- and azahomocyclostatine polypeptides
CA1282549C (en) 1985-11-12 1991-04-02 Eric M. Gordon Aminocarbonyl renin inhibitors
US4757050A (en) * 1985-12-23 1988-07-12 E. R. Squibb Sons, Inc. Ureido renin inhibitors
CA1297631C (en) 1985-12-23 1992-03-17 Sesha I. Natarajan 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
CH676988A5 (enExample) 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 (enExample) * 1990-06-28 1994-06-21 Shionogi & Co
US5272268A (en) * 1990-06-28 1993-12-21 Shionogi & Co., Ltd. Dipeptide derivatives
US5223615A (en) * 1990-06-28 1993-06-29 Shionogi & Co., Ltd. Dipeptide derivatives
CA2086414A1 (en) 1990-07-06 1992-01-07 Geoffrey B. Dreyer Retroviral protease inhibitors
GB9024938D0 (en) 1990-11-16 1991-01-02 Process Dev Ltd Filtering
US5475013A (en) 1990-11-19 1995-12-12 Monsanto Company Retroviral protease inhibitors
ATE136888T1 (de) * 1990-11-19 1996-05-15 Monsanto Co Retrovirale proteaseinhibitoren
DE69133464T2 (de) 1990-11-19 2006-05-18 Pharmacia Corp.(N.D.Ges.D.Staates Delaware) Retrovirusprotease Inhibitoren
EP0607334B1 (en) 1991-10-11 1997-07-30 The Du Pont Merck Pharmaceutical Company Cyclic ureas and analogues useful as retroviral protease inhibitiors
WO1993008184A1 (en) 1991-10-23 1993-04-29 Merck & Co., Inc. Hiv protease inhibitors
EP0541168B1 (en) 1991-11-08 1998-03-11 Merck & Co. Inc. HIV protease inhibitors useful for the treatment of aids
US5413999A (en) 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
DE69300043T2 (de) 1992-03-13 1995-05-24 Bio Mega Boehringer Ingelheim Substituierte Pipecoline-Säurederivate als HIV-Protease-Hemmer.
ES2091000T3 (es) 1992-05-20 1996-10-16 Searle & Co Metodo para elaborar intermedios utiles en la sintesis de inhibidores de proteasas retroviricas.
US5559256A (en) 1992-07-20 1996-09-24 E. R. Squibb & Sons, Inc. Aminediol 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
ES2123065T3 (es) 1992-08-25 1999-01-01 Searle & Co Hidroxietilamino-sulfonamidas utiles como inhibidores de proteasas retroviricas.
US5968942A (en) * 1992-08-25 1999-10-19 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
WO1994004491A1 (en) 1992-08-25 1994-03-03 G.D. Searle & Co. N-(alkanoylamino-2-hydroxypropyl)-sulfonamides useful as retroviral protease inhibitors
RU2146668C1 (ru) 1992-08-25 2000-03-20 Джи Ди Сирл энд Компани Сульфонилалканоиламино-гидроксиэтиламино-сульфонамидное соединение, фармацевтические композиции и способы лечения и ингибирования ретровирусных протеаз
US6022994A (en) 1992-08-25 2000-02-08 G. D. Searle &. Co. Succinoylamino 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
US5830897A (en) 1992-08-27 1998-11-03 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
WO1994005300A1 (en) 1992-09-03 1994-03-17 Biochem Pharma Inc. Use of rapamycin in the treatment of aids
US5783701A (en) 1992-09-08 1998-07-21 Vertex Pharmaceuticals, Incorporated Sulfonamide inhibitors of aspartyl protease
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
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
EP0715618B1 (en) 1993-08-24 1998-12-16 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
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
PL186473B1 (pl) 1996-01-26 2004-01-30 Virco Nv Sposób oceny in vitro chemioterapii HIV u pacjentów HIV dodatnich oraz sposób oznaczania fenotypowej wrażliwości lekowej poszczególnych szczepów HIV u pacjenta na inhibitory co najmniej dwóch enzymówkodowanych przez gen pol HIV
CA2216126C (en) 1996-01-29 2009-03-31 Virologic, Inc. Compositions and methods for determining anti-viral drug susceptibility and resistance and anti-viral drug screening
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
ATE500823T1 (de) 1998-06-23 2011-03-15 Us Of America Represented By The Secretary Dept Of Health And Human Services Arzneimittel zur behandlung von hiv-infizierten säugetieren
US6538006B1 (en) 1998-07-08 2003-03-25 Pharmacia Corporation Retroviral protease inhibitors
JP2003501051A (ja) 1999-05-28 2003-01-14 ビルコ・エヌ・ブイ 表現型薬物耐性と相関するｈｉｖ−１逆転写酵素における新規な変異プロフィル
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0264795A2 (de) * 1986-10-22 1988-04-27 MERCK PATENT GmbH Aminosäurederivate

Also Published As

Publication number Publication date
ATE172717T1 (de) 1998-11-15
ES2123065T3 (es) 1999-01-01
USRE43596E1 (en) 2012-08-21
JP3657002B2 (ja) 2005-06-08
US6846954B2 (en) 2005-01-25
EP0656887A1 (en) 1995-06-14
US6534493B1 (en) 2003-03-18
US20040044047A1 (en) 2004-03-04
US7320983B2 (en) 2008-01-22
US6500832B1 (en) 2002-12-31
FI950650L (fi) 1995-02-14
EP0810209B1 (en) 2002-06-05
US20040229922A1 (en) 2004-11-18
FI20012317L (fi) 2001-11-27
EP0810209A3 (en) 1998-12-02
NO307047B1 (no) 2000-01-31
US5744481A (en) 1998-04-28
USRE43802E1 (en) 2012-11-13
CA2140929A1 (en) 1994-02-26
EP0810209A2 (en) 1997-12-03
NO983099L (no) 1995-02-13
NL300283I1 (nl) 2007-09-03
LU91339I2 (fr) 2007-07-23
RU95106624A (ru) 1996-12-10
US7115618B2 (en) 2006-10-03
FI119427B (fi) 2008-11-14
DE69321845T2 (de) 1999-04-29
AU680635B2 (en) 1997-08-07
NO950533D0 (no) 1995-02-13
NO983099D0 (no) 1998-07-03
JPH08501288A (ja) 1996-02-13
AU680635C (en) 2007-05-17
FI950650A0 (fi) 1995-02-14
AU5347494A (en) 1994-03-15
FR07C0034I2 (fr) 2008-05-09
FI112471B (fi) 2003-12-15
CA2140929C (en) 2006-09-12
DE69332002T2 (de) 2002-12-19
US20070078173A1 (en) 2007-04-05
KR100336699B1 (ko) 2002-05-13
WO1994004492A1 (en) 1994-03-03
DE122007000045I1 (de) 2007-08-16
US20090023664A1 (en) 2009-01-22
KR950702960A (ko) 1995-08-23
DE69321845D1 (en) 1998-12-03
US5786483A (en) 1998-07-28
US7829564B2 (en) 2010-11-09
EP0656887B1 (en) 1998-10-28
NO305478B1 (no) 1999-06-07
DK0810209T3 (da) 2002-08-12
US6335460B1 (en) 2002-01-01
DE69332002D1 (de) 2002-07-11
PT810209E (pt) 2002-09-30
NO950533L (no) 1995-02-13
FR07C0034I1 (enExample) 2007-06-07
US6172082B1 (en) 2001-01-09
DK0656887T3 (da) 1999-07-05
US6472407B1 (en) 2002-10-29
US6060476A (en) 2000-05-09
US6455581B1 (en) 2002-09-24
ES2177868T3 (es) 2002-12-16
DE122007000045I2 (de) 2011-07-21
US5843946A (en) 1998-12-01
ATE218541T1 (de) 2002-06-15

Similar Documents

Publication Publication Date Title
KR100296463B1 (ko) 레트로바이러스프로테아제저해제로서유용한히드록시에틸아미노술폰아미드
US6646010B2 (en) α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
EP0666842B1 (en) Hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors
US7232817B2 (en) α- and β-amino acid hydroxyethlamino sulfonyl urea derivatives useful as retroviral protease inhibitors
EP0715618A1 (en) Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
USRE42889E1 (en) α- and β- amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US20050004043A1 (en) Succinoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
RU2173680C2 (ru) Гидроксиэтиламиносульфонамиды, промежуточные соединения, фармацевтическая композиция, способ ингибирования ретровирусных протеаз, способ лечения ретровирусных инфекций, способ лечения спида

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 19950214

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 19980824

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20000629

Patent event code: PE09021S01D

A107 Divisional application of patent
PA0104 Divisional application for international application

Comment text: Divisional Application for International Patent

Patent event code: PA01041R01D

Patent event date: 20001117

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20010223

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20010510

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20010511

End annual number: 3

Start annual number: 1

PG1601 Publication of registration
PR1001 Payment of annual fee

Payment date: 20040406

Start annual number: 4

End annual number: 4

PR1001 Payment of annual fee

Payment date: 20050408

Start annual number: 5

End annual number: 5

PR1001 Payment of annual fee

Payment date: 20060502

Start annual number: 6

End annual number: 6

PR1001 Payment of annual fee

Payment date: 20070406

Start annual number: 7

End annual number: 7

PR1001 Payment of annual fee

Payment date: 20080407

Start annual number: 8

End annual number: 8

PR1001 Payment of annual fee

Payment date: 20090409

Start annual number: 9

End annual number: 9

PR1001 Payment of annual fee

Payment date: 20100429

Start annual number: 10

End annual number: 10

PR1001 Payment of annual fee

Payment date: 20110428

Start annual number: 11

End annual number: 11

PR1001 Payment of annual fee

Payment date: 20120427

Start annual number: 12

End annual number: 12

FPAY Annual fee payment

Payment date: 20130429

Year of fee payment: 13

PR1001 Payment of annual fee

Payment date: 20130429

Start annual number: 13

End annual number: 13

EXPY Expiration of term
PC1801 Expiration of term

Termination date: 20140224

Termination category: Expiration of duration