CY1108036T1 - Κυτταρικη συσσωρευση φωσφονικων αναλογων ενωσεων αναστολεα πρωτεασης του ιου ανοσολογικης ανεπαρκειας του ανθρωπου (hiv) και οι ενωσεις ως τετοιες - Google Patents

Κυτταρικη συσσωρευση φωσφονικων αναλογων ενωσεων αναστολεα πρωτεασης του ιου ανοσολογικης ανεπαρκειας του ανθρωπου (hiv) και οι ενωσεις ως τετοιες

Info

Publication number
CY1108036T1
CY1108036T1 CY20071101320T CY071101320T CY1108036T1 CY 1108036 T1 CY1108036 T1 CY 1108036T1 CY 20071101320 T CY20071101320 T CY 20071101320T CY 071101320 T CY071101320 T CY 071101320T CY 1108036 T1 CY1108036 T1 CY 1108036T1
Authority
CY
Cyprus
Prior art keywords
hiv
phosphone
human
cellular accumulation
protective protection
Prior art date
Application number
CY20071101320T
Other languages
English (en)
Inventor
Murty N Arimilli
Mark W Becker
Clifford Bryant
James M Chen
Xiaowu Chen
Azar Dastgah
Maria Fardis
Gong-Xin He
Haolun Jin
Choung U Kim
William A Lee
Christopher P Lee
Kuei-Ying Lin
Hongtao Liu
Richard L Mackman
Michael L Mitchell
Peter H Nelson
Hyung-Jung Pyun
Tanisha D Rowe
Sundaramoorthi Swaminathan
James D Tario
Lijun Zhang
Mark Sparacino
Jianying Wang
Matthew A Williams
Lianhong Xu
Zheng-Yu Yang
Richard H Yu
Jiancun Zhang
Original Assignee
Gilead Sciences, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Gilead Sciences, Inc. filed Critical Gilead Sciences, Inc.
Publication of CY1108036T1 publication Critical patent/CY1108036T1/el

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • C07D213/84—Nitriles
    • C07D213/85—Nitriles in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18—One oxygen or sulfur atom
    • C07D231/20—One oxygen atom attached in position 3 or 5
    • 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
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/42—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—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
    • C07D239/28—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/04—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/18—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in position 2
    • 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
    • C07D307/56—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 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
    • C07D307/68—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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006—Esters of acyclic acids which can have further substituents on alkyl
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/58—Pyridine rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503—Five-membered rings
    • C07F9/6506—Five-membered rings having the nitrogen atoms in positions 1 and 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/650905—Six-membered rings having the nitrogen atoms in the positions 1 and 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/650905—Six-membered rings having the nitrogen atoms in the positions 1 and 2
    • C07F9/650947—Six-membered rings having the nitrogen atoms in the positions 1 and 2 condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3
    • C07F9/65128—Six-membered rings having the nitrogen atoms in positions 1 and 3 condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07F9/6533—Six-membered rings
    • C07F9/65335—Six-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
    • C07F9/65515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/16—Hydrolases (3) acting on ester bonds (3.1)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/02—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving viable microorganisms
    • C12Q1/18—Testing for antimicrobial activity of a material
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/37—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/44—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving esterase
    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00—Libraries per se, e.g. arrays, mixtures
    • C40B40/04—Libraries containing only organic compounds
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/502—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing non-proliferative effects
    • G01N33/5038—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing non-proliferative effects involving detection of metabolites per se
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/005—Assays involving biological materials from specific organisms or of a specific nature from viruses
    • G01N2333/08—RNA viruses
    • G01N2333/15—Retroviridae, e.g. bovine leukaemia virus, feline leukaemia virus, feline leukaemia virus, human T-cell leukaemia-lymphoma virus
    • G01N2333/155—Lentiviridae, e.g. visna-maedi virus, equine infectious virus, FIV, SIV
    • G01N2333/16—HIV-1, HIV-2
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Biomedical Technology (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • General Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biophysics (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Toxicology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Food Science & Technology (AREA)
  • Cell Biology (AREA)
  • Virology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)

Abstract

Αποκαλύπτονται φωσφονικές υποκαθιστάμενες ενώσεις με ανασταλτικές ιδιότητες πρωτεάσης του ΗIV που χρησιμοποιούνται ως θεραπευτικές και για άλλους βιομηχανικούς σκοπούς. Οι συνθέσεις αναστέλλουν τη δραστηριότητα πρωτεάσης του HIV και/ή είναι χρήσιμες θεραπευτικά για τη θεραπεία του AIDS και άλλων αντιϊκών μολύνσεων, καθώς επίσης σε δοκιμασίες για την ανίχνευση της πρωτεάσης του HIV.
CY20071101320T 2002-04-26 2007-10-15 Κυτταρικη συσσωρευση φωσφονικων αναλογων ενωσεων αναστολεα πρωτεασης του ιου ανοσολογικης ανεπαρκειας του ανθρωπου (hiv) και οι ενωσεις ως τετοιες CY1108036T1 (el)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US37583402P 2002-04-26 2002-04-26
US37562202P 2002-04-26 2002-04-26
US37566502P 2002-04-26 2002-04-26
US37577902P 2002-04-26 2002-04-26
EP03747326A EP1509537B9 (en) 2002-04-26 2003-04-25 Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds and the compounds as such

Publications (1)

Publication Number Publication Date
CY1108036T1 true CY1108036T1 (el) 2013-09-04

Family

ID=29273807

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20071101320T CY1108036T1 (el) 2002-04-26 2007-10-15 Κυτταρικη συσσωρευση φωσφονικων αναλογων ενωσεων αναστολεα πρωτεασης του ιου ανοσολογικης ανεπαρκειας του ανθρωπου (hiv) και οι ενωσεις ως τετοιες

Country Status (28)

Country Link
US (7) US20070010489A1 (el)
EP (4) EP1575486A4 (el)
JP (5) JP4942915B2 (el)
KR (2) KR100987815B1 (el)
CN (4) CN1656109A (el)
AT (1) ATE367394T1 (el)
AU (4) AU2003231766A1 (el)
BR (2) BR0309573A (el)
CA (3) CA2481261C (el)
CY (1) CY1108036T1 (el)
DE (1) DE60315023T2 (el)
DK (1) DK1509537T3 (el)
EA (2) EA008775B1 (el)
ES (1) ES2290485T3 (el)
HK (1) HK1073467A1 (el)
HR (2) HRP20041114A2 (el)
IL (2) IL164491A0 (el)
IS (2) IS7555A (el)
MX (2) MXPA04010527A (el)
NO (2) NO20045152L (el)
NZ (1) NZ535828A (el)
PL (2) PL211979B1 (el)
PT (1) PT1509537E (el)
SI (1) SI1509537T1 (el)
TW (2) TWI332956B (el)
UA (1) UA80819C2 (el)
WO (4) WO2003090690A2 (el)
ZA (2) ZA200409376B (el)

Families Citing this family (130)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003231766A1 (en) * 2002-04-26 2003-11-10 Gilead Sciences, Inc. Non nucleoside reverse transcriptase inhibitors
US20050239054A1 (en) * 2002-04-26 2005-10-27 Arimilli Murty N Method and compositions for identifying anti-HIV therapeutic compounds
WO2004050609A1 (en) * 2002-11-27 2004-06-17 Elan Pharmaceutical, Inc. Substituted ureas and carbamates
SI1583542T1 (sl) 2003-01-14 2008-12-31 Gilead Sciences Inc Sestavki in postopki za kombinacijsko antivirusnoterapijo
US7452901B2 (en) 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
US7407965B2 (en) * 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
US20090247488A1 (en) * 2003-04-25 2009-10-01 Carina Cannizzaro Anti-inflammatory phosphonate compounds
US7432261B2 (en) * 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
US7273716B2 (en) * 2003-04-25 2007-09-25 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds with GS-7340 ester hydrolase
WO2005002626A2 (en) * 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
US20050261237A1 (en) * 2003-04-25 2005-11-24 Boojamra Constantine G Nucleoside phosphonate analogs
WO2004096287A2 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
WO2004096237A2 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
WO2004096233A2 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Nucleoside phosphonate conjugates
CA2522845A1 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
CN101410120A (zh) * 2003-04-25 2009-04-15 吉里德科学公司 抗炎的膦酸酯化合物
WO2004096285A2 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Anti-infective phosphonate conjugates
US7470724B2 (en) * 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
EP1620110A2 (en) * 2003-04-25 2006-02-01 Gilead Sciences, Inc. Immunomodulator phosphonate conjugates
MXPA05011297A (es) 2003-04-25 2006-05-25 Gilead Sciences Inc Analogos antivirales de fosfonato.
US7491794B2 (en) * 2003-10-14 2009-02-17 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
WO2005044308A1 (en) * 2003-10-24 2005-05-19 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
WO2005044279A1 (en) * 2003-10-24 2005-05-19 Gilead Sciences, Inc. Purine nucleoside phosphonate conjugates
US20050153990A1 (en) * 2003-12-22 2005-07-14 Watkins William J. Phosphonate substituted kinase inhibitors
BRPI0418031A (pt) * 2003-12-22 2007-04-17 Gilead Sciences Inc inibidores de quinase fosfonato-substituìdos
WO2005063258A1 (en) * 2003-12-22 2005-07-14 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
WO2005063751A1 (en) * 2003-12-22 2005-07-14 Gilead Sciences, Inc. 4’-substituted carbovir-and abacavir-derivatives as well as related compounds with hiv and hcv antiviral activity
MXPA06007906A (es) * 2004-01-12 2007-02-14 Gilead Sciences Inc Compuestos antivirales de fosfonato de pirimidilo y metodos de uso.
PT1742642E (pt) * 2004-04-14 2009-01-23 Gilead Sciences Inc Análogos de fosfonato de compostos inibidores da integrase do hiv
DK2258376T3 (en) * 2004-07-27 2019-04-15 Gilead Sciences Inc Phosphonate analogues of HIV inhibitor compounds
AU2011218664B2 (en) * 2004-07-27 2014-08-21 Gilead Sciences, Inc. Antiviral compounds
NZ554232A (en) * 2004-09-17 2010-09-30 Idenix Pharmaceuticals Inc Phosphoindoles as HIV inhibitors
ES2354338T3 (es) * 2004-09-17 2011-03-14 Idenix Pharmaceuticals, Inc. Fosfoindoles como inhibidores de vih.
AU2005294123C1 (en) 2004-10-07 2010-01-21 Vitae Pharmaceuticals, Inc. Diaminoalkane aspartic protease inhibitors
EP1812012A4 (en) 2004-11-15 2010-02-17 Ceptyr Inc PROTEIN TYROSINE PHOSPHATASE INHIBITOR AND METHOD FOR THEIR USE
WO2006066074A2 (en) 2004-12-16 2006-06-22 The Regents Of The University Of California Lung-targeted drugs
ES2331257T3 (es) 2005-02-25 2009-12-28 Tibotec Pharmaceuticals Sintesis de precursores de inhibidores de proteasas.
US20070003608A1 (en) * 2005-04-08 2007-01-04 Almond Merrick R Compounds, compositions and methods for the treatment of viral infections and other medical disorders
JP2008535862A (ja) * 2005-04-08 2008-09-04 キメリクス，インコーポレイテッド ポックスウイルス感染の治療のための化合物、組成物および方法
AR053845A1 (es) 2005-04-15 2007-05-23 Tibotec Pharm Ltd 5-tiazolilmetil[(1s,2r)-3-[[(2-amino-6-benzoxazolil)sulfonil)](2-metilpropil)amino]-2-hidroxi-1-(fenilmetil)propil]carbamato como mejorador de farmacos metabolizados por el citocromo p450
TWI471145B (zh) 2005-06-13 2015-02-01 Bristol Myers Squibb & Gilead Sciences Llc 單一式藥學劑量型
TWI375560B (en) 2005-06-13 2012-11-01 Gilead Sciences Inc Composition comprising dry granulated emtricitabine and tenofovir df and method for making the same
AU2006276246B2 (en) 2005-07-25 2012-09-27 Intermune, Inc. Novel macrocyclic inhibitors of hepatitis C virus replication
WO2007014352A2 (en) * 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of hiv
CN101415705B (zh) * 2005-10-11 2011-10-26 因特蒙公司 抑制丙型肝炎病毒复制的化合物和方法
TWI411607B (zh) 2005-11-14 2013-10-11 Vitae Pharmaceuticals Inc 天門冬胺酸蛋白酶抑制劑
AR058238A1 (es) 2005-11-28 2008-01-23 Tibotec Pharm Ltd Compuestos y derivados de aminofenilsulfonamida sustituida como inhibidores de proteasa del vih
TWI385173B (zh) 2005-11-28 2013-02-11 Tibotec Pharm Ltd 作為ｈｉｖ蛋白酶抑制劑之經取代的胺基苯基磺醯胺化合物
WO2007068934A2 (en) * 2005-12-14 2007-06-21 Cipla Limited Pharmaceutical combination comprising nucleotide and nucleoside reverse transcriptase inhibitors (such as tenofovir and lamivudine) in different parts of the dosage unit
US20070167422A1 (en) * 2006-01-18 2007-07-19 Yu Kwok S Pharmaceutical compositions comprising 17-allylamino-17-demethoxygeldanamycin
SG170794A1 (en) 2006-03-29 2011-05-30 Gilead Sciences Inc Process for preparation of hiv protease inhibitors
AU2007277253A1 (en) * 2006-07-24 2008-01-31 Gilead Sciences, Inc. Bisfuranyl protease inhibitors
CL2007002689A1 (es) 2006-09-18 2008-04-18 Vitae Pharmaceuticals Inc Compuestos derivados de piperidin-1-carboxamida, inhibidores de la renina; compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como hipertension, insuficiencia cardiaca, fibrosis cardiaca, entre otras.
EP2078029B1 (en) 2006-09-29 2014-05-14 IDENIX Pharmaceuticals, Inc. Enantiomerically pure phosphoindole as hiv inhibitor
WO2008077070A2 (en) * 2006-12-18 2008-06-26 University Of Massachusetts Crystal structures of hiv-1 protease inhibitors bound to hiv-1 protease
EP2134336B1 (en) 2007-03-16 2013-12-11 Sequoia Pharmaceuticals Benzofuran-derived hiv protease inhibitors
EP2139883A4 (en) * 2007-03-23 2011-06-22 Univ Massachusetts INHIBITORS OF HIV-1 PROTEASE
BRPI0811020A2 (pt) * 2007-05-03 2015-07-21 Intermune Inc Composto, composição farmacêutica e métodos de inibição da atividade da protease ns3/ns4, de tratamento da fibrose hepática, de intensificação da função hepática em indivíduo com infecção do vírus da hepatite c e métodos de síntese de compostos, de administração de inibidor da infecção do vírus da hepatite c (hcv) e de distribuição de forma de dosagem oral.
WO2008151306A1 (en) * 2007-06-05 2008-12-11 Arizona Board Of Regents, A Body Corporate Of The State Of Arizona, Acting For And On Behalf Of Arizona State University Synthesis of cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity
AR067181A1 (es) 2007-06-29 2009-09-30 Gilead Sciences Inc Inhibidores de transcriptasa inversa de hiv, composicion farmaceutica, uso del compuesto para preparar un medicamento, agente de combinacion farmaceutica y metodo de inhibicion de la replicacion de un retrovirus
WO2009005693A1 (en) 2007-06-29 2009-01-08 Gilead Sciences, Inc. Novel hiv reverse transcriptase inhibitors
US8901487B2 (en) * 2007-07-20 2014-12-02 George Washington University Subcellular analysis by laser ablation electrospray ionization mass spectrometry
US20100285446A1 (en) * 2007-07-20 2010-11-11 Akos Vertes Methods for Detecting Metabolic States by Laser Ablation Electrospray Ionization Mass Spectrometry
US8067730B2 (en) 2007-07-20 2011-11-29 The George Washington University Laser ablation electrospray ionization (LAESI) for atmospheric pressure, In vivo, and imaging mass spectrometry
US7964843B2 (en) 2008-07-18 2011-06-21 The George Washington University Three-dimensional molecular imaging by infrared laser ablation electrospray ionization mass spectrometry
US8119800B2 (en) 2007-12-21 2012-02-21 Korea Research Institute Of Chemical Technology Processes for preparing HIV reverse transcriptase inhibitors
JP5562255B2 (ja) * 2008-01-25 2014-07-30 キメリクス，インコーポレイテッド ウイルス感染を治療する方法
EP2282762A2 (en) * 2008-04-15 2011-02-16 Intermune, Inc. Novel macrocyclic inhibitors of hepatitis c virus replication
ES2645689T3 (es) * 2008-05-21 2017-12-07 Ariad Pharmaceuticals, Inc. Derivados de fósforo como inhibidores de quinasas
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
US8173621B2 (en) 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
JP2011525933A (ja) * 2008-06-26 2011-09-29 ヴァイティー ファーマシューティカルズ，インコーポレイテッド メチル２−（（ｒ）−（３−クロロフェニル）（（ｒ）−１−（（ｓ）−２−（メチルアミノ）−３−（（ｒ）−テトラヒドロ−２ｈ−ピラン−３−イル）プロピルカルバモイル）ピペリジン−３−イル）メトキシ）エチルカルバメートの塩
MX2011000306A (es) 2008-07-08 2011-03-15 Gilead Sciences Inc Sales de compuestos inhibidores de hiv.
CN102216321A (zh) * 2008-10-15 2011-10-12 因特蒙公司 治疗性抗病毒肽
CL2009002206A1 (es) 2008-12-23 2011-08-26 Gilead Pharmasset Llc Compuestos derivados de pirrolo -(2-3-d]-pirimidin-7(6h)-tetrahidrofuran-2-il fosfonamidato, composicion farmaceutica; y su uso en el tratamiento de enfermedades virales.
MX2011006891A (es) 2008-12-23 2011-10-06 Pharmasset Inc Fosforamidatos de nucleosidos.
AU2009329917B2 (en) 2008-12-23 2016-03-31 Gilead Pharmasset Llc Nucleoside analogs
AR075584A1 (es) * 2009-02-27 2011-04-20 Intermune Inc COMPOSICIONES TERAPEUTICAS QUE COMPRENDEN beta-D-2'-DESOXI-2'-FLUORO-2'-C-METILCITIDINA Y UN DERIVADO DE ACIDO ISOINDOL CARBOXILICO Y SUS USOS. COMPUESTO.
TWI598358B (zh) 2009-05-20 2017-09-11 基利法瑪席特有限責任公司 核苷磷醯胺
EP2270021A1 (en) 2009-06-18 2011-01-05 Centre National de la Recherche Scientifique Phosphonates synthons for the synthesis of phosphonates derivatives showing better bioavailability
US20120232038A1 (en) 2009-06-25 2012-09-13 Gilead Sciences, Inc. Crystalline forms of (3r, 3as, 6ar) - hexahydrofuro [2,3-b] furan-3-yl (1s,2r) - (1-{4-[ (diethoxyphosphoryl) methoxy] pheny1}-3-hydroxy-4- [4-methoxy-n- (2-methylpropyl) benzenesul - fonamido] butan-2-yl) carbamate
US7924650B2 (en) * 2009-06-30 2011-04-12 Oracle America, Inc. Dynamically controlled voltage regulator for a memory
CN102711472B (zh) 2009-07-02 2015-12-02 江苏康缘药业股份有限公司 含磷的喹唑啉化合物及其使用方法
US8614200B2 (en) 2009-07-21 2013-12-24 Chimerix, Inc. Compounds, compositions and methods for treating ocular conditions
AR077692A1 (es) 2009-08-06 2011-09-14 Vitae Pharmaceuticals Inc Sales de 2-((r)-(3-clorofenil) ((r)-1-((s) -2-(metilamino)-3-((r)-tetrahidro-2h-piran-3-il) propilcarbamoil) piperidin -3-il) metoxi) etilcarbamato de metilo
DE102009041443A1 (de) * 2009-09-16 2011-03-31 Archimica Gmbh Salze des 6-Chlor-4-(cyclopropylethinyl)-1,4-dihydro-4-(trifluormethyl)-2H-3,1-benzoxazin-2-ons und deren Synthese, Aufreinigung und Anwendung als Vorstufen für Efavirenz
EP2483273A4 (en) * 2009-09-28 2013-05-01 Hoffmann La Roche NOVEL MACROCYCLIC INHIBITORS FOR HEPATITIS C VIRUS REPLICATION
US20110082182A1 (en) * 2009-10-01 2011-04-07 Intermune, Inc. Therapeutic antiviral peptides
JP2013509433A (ja) * 2009-10-30 2013-03-14 キメリクス，インコーポレイテッド ウイルス関連疾患を処置する方法
US9006218B2 (en) 2010-02-12 2015-04-14 Chimerix Inc. Nucleoside phosphonate salts
PE20130151A1 (es) 2010-03-31 2013-02-21 Gilead Pharmasset Llc Sintesis estereoselectiva de activos que contienen fosforo
US8563530B2 (en) 2010-03-31 2013-10-22 Gilead Pharmassel LLC Purine nucleoside phosphoramidate
PL2609923T4 (pl) 2010-03-31 2017-11-30 Gilead Pharmasset Llc Proces krystalizacji 2-(((s)-(perfluorofenoksy) (fenoksy)fosforylo)amino)propanianu (s)-izopropylu
US9278135B2 (en) 2010-04-26 2016-03-08 Chimerix Inc. Methods of treating retroviral infections and related dosage regimes
US8884027B2 (en) 2010-10-22 2014-11-11 University Of Rochester Melampomagnolide B derivatives as antileukemic and cytotoxic agents
TW201242974A (en) 2010-11-30 2012-11-01 Gilead Pharmasset Llc Compounds
CN102127030B (zh) * 2011-01-21 2013-05-22 天津大学 4-(取代-1,3-二炔基)-4-(三氟甲基)苯并-1,4-二氢噁嗪-2-酮类化合物及其制备方法和应用
EA201391626A1 (ru) 2011-05-04 2014-03-31 Ариад Фармасьютикалз, Инк. Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака
PT2710019T (pt) 2011-05-19 2017-07-21 Gilead Sciences Inc Processos e intermediários para preparar agentes anti-hiv
US8829426B2 (en) 2011-07-14 2014-09-09 The George Washington University Plume collimation for laser ablation electrospray ionization mass spectrometry
ES2467145T3 (es) * 2011-07-18 2014-06-12 Essilor International (Compagnie Générale d'Optique) Máquina para revestir un artículo óptico con una composición de revestimiento antisuciedad y procedimiento para utilizar la máquina
WO2013082476A1 (en) 2011-11-30 2013-06-06 Emory University Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections
US9919939B2 (en) 2011-12-06 2018-03-20 Delta Faucet Company Ozone distribution in a faucet
AU2013204563B2 (en) 2012-05-05 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
CN103665043B (zh) 2012-08-30 2017-11-10 江苏豪森药业集团有限公司 一种替诺福韦前药及其在医药上的应用
PT2970346T (pt) 2013-03-15 2018-11-09 Univ California Diésteres de fosfonato nucleosídico acíclico
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
KR102448455B1 (ko) 2014-03-14 2022-09-28 올텍 법인회사 셀레노유기 화합물의 조성물 및 이의 사용 방법
EP3192794A4 (en) * 2014-09-11 2018-06-27 Shionogi & Co., Ltd. Sustained hiv protease inhibitor
BR112017005111B1 (pt) 2014-09-15 2023-02-14 The Regents Of The University Of California Compostos análogos de nucleotídeo acíclico, composição farmacêutica contendo tais compostos, e usos da composição no tratamento de uma infecção por papilomavírus
WO2016069955A1 (en) * 2014-10-29 2016-05-06 Wisconsin Alumni Research Foundation Boronic acid inhibitors of hiv protease
JP7381190B2 (ja) 2014-12-26 2023-11-15 エモリー・ユニバーシテイ Ｎ４－ヒドロキシシチジン及び誘導体並びにそれに関連する抗ウイルス用途
WO2016187788A1 (en) 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection
WO2017048252A1 (en) 2015-09-15 2017-03-23 Alltech, Inc. Compositions of selenoorganic compounds and methods of use thereof
US10377782B2 (en) 2015-09-15 2019-08-13 The Regents Of The University Of California Nucleotide analogs
KR20180069067A (ko) 2015-10-30 2018-06-22 엔비이-테라퓨틱스 아게 안티-ror1 항체
US10548910B2 (en) 2015-11-17 2020-02-04 Merck Sharp & Dohme Corp. Amido-substituted pyridotriazine derivatives useful as HIV integrase inhibitors
CN115093008B (zh) 2015-12-21 2024-05-14 德尔塔阀门公司 包括消毒装置的流体输送***
WO2017127664A1 (en) 2016-01-20 2017-07-27 The Scripps Research Institute Ror1 antibody compositions and related methods
WO2017133517A1 (zh) * 2016-02-03 2017-08-10 四川海思科制药有限公司 一种磷酰胺衍生物及制备方法和用途
CN106045874B (zh) * 2016-05-20 2017-12-05 大连医科大学 二苯甲酮‐二酮酸类化合物，组合物及用途
JOP20190130A1 (ar) 2016-12-02 2019-06-02 Merck Sharp & Dohme مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv)
EP3548031B1 (en) 2016-12-02 2023-07-19 Merck Sharp & Dohme LLC Tricyclic heterocycle compounds useful as hiv integrase inhibitors
WO2018165766A1 (en) * 2017-03-16 2018-09-20 Therapure Biopharma Inc. Method for purification of albumin
CN109305989B (zh) * 2017-07-28 2021-02-26 四川海思科制药有限公司 一种磷酰胺衍生物及制备方法和用途
CN109305990B (zh) * 2017-07-28 2021-02-26 四川海思科制药有限公司 一种磷酸衍生物及制备方法和用途
PL3661937T3 (pl) 2017-08-01 2021-12-20 Gilead Sciences, Inc. Formy krystaliczne ((s)-((((2r,5r)-5-(6-amino-9h-puryn-9-ylo)-4-fluoro-2,5-dihydrofuran-2-ylo)oksy)metylo)(fenoksy)fosforylo)-l-alaninianu etylu (gs-9131) do leczenia zakażeń wirusowych
SG11202000846WA (en) 2017-08-07 2020-02-27 Nbe Therapeutics Ag Anthracycline-based antibody drug conjugates having high in vivo tolerability
CA3082191C (en) 2017-12-07 2021-09-21 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
US11542288B2 (en) * 2020-06-01 2023-01-03 University Of Massachusetts Antiviral compounds

Family Cites Families (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE63869B1 (en) 1986-11-06 1995-06-14 Res Dev Foundation Aerosols containing liposomes and method for their preparation
FR2611203B1 (fr) 1987-02-20 1989-06-09 Sturtz Georges Analogues gem-diphosphoniques d'amethopterine (methotrexate) et de derives deaza-n-10 amethopterine. leur preparation et les compositions pharmaceutiques qui les contiennent
US5631370A (en) * 1988-01-20 1997-05-20 Regents Of The University Of Minnesota Optically-active isomers of dideoxycarbocyclic nucleosides
DE4003574A1 (de) * 1990-02-07 1991-08-08 Bayer Ag Neue dipeptide, verfahren zu ihrer herstellung und ihre verwendung als renininhibitoren in arzneimitteln
EP0533833B1 (en) 1990-06-13 1995-12-20 GLAZIER, Arnold Phosphorous produgs
EP0465297B1 (en) 1990-07-04 1996-01-31 Merrell Dow Pharmaceuticals Inc. 9-Purinyl phosphonic acid derivatives
US5177064A (en) 1990-07-13 1993-01-05 University Of Florida Targeted drug delivery via phosphonate derivatives
DE4111730A1 (de) 1991-04-10 1992-10-15 Knoll Ag Neue cytarabin-derivate, ihre herstellung und verwendung
EP0531597A1 (en) 1991-09-12 1993-03-17 Merrell Dow Pharmaceuticals Inc. Novel unsaturated acyclic phosphonate derivatives of purine and pyrimidine
US5610294A (en) 1991-10-11 1997-03-11 The Du Pont Merck Pharmaceutical Company Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors
GB9126144D0 (en) 1991-12-10 1992-02-12 British Bio Technology Compounds
FR2692265B1 (fr) 1992-05-25 1996-11-08 Centre Nat Rech Scient Composes biologiquement actifs de type phosphotriesters.
IS2334B (is) 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
DE69426904T2 (de) 1993-06-29 2001-10-11 Mitsubishi Chem Corp Phosphonat-Nukleotid Ester-Derivate
JPH09500120A (ja) * 1993-07-14 1997-01-07 チバ−ガイギー アクチェンゲゼルシャフト 環式ヒドラジン化合物
US5446137B1 (en) 1993-12-09 1998-10-06 Behringwerke Ag Oligonucleotides containing 4'-substituted nucleotides
US5854227A (en) 1994-03-04 1998-12-29 Hartmann; John F. Therapeutic derivatives of diphosphonates
WO1997011092A1 (fr) 1994-04-07 1997-03-27 Nippon Shinyaku Co., Ltd. Derives de phosphates de cyclosporine et composition medicinale
DE69532245T2 (de) * 1994-09-26 2004-09-16 Shionogi & Co., Ltd. Imidazolderivat
US5705524A (en) * 1994-11-04 1998-01-06 Gilead Sciences, Inc. Thiepane compounds
AU710492B2 (en) * 1994-11-04 1999-09-23 Gilead Sciences, Inc. Thiepane compounds inhibiting and detecting HIV protease
US5750493A (en) * 1995-08-30 1998-05-12 Raymond F. Schinazi Method to improve the biological and antiviral activity of protease inhibitors
US5914332A (en) * 1995-12-13 1999-06-22 Abbott Laboratories Retroviral protease inhibiting compounds
US5874577A (en) 1996-04-03 1999-02-23 Medichem Research, Inc. Method for the preparing 9-12-(Diethoxyphosphonomethoxy)ethyl!adenine and analogues thereof
WO1998004569A1 (en) 1996-07-26 1998-02-05 Gilead Sciences, Inc. Nucleotide analogs
KR20000029952A (ko) 1996-08-13 2000-05-25 미우라 아끼라 포스포네이트뉴클레오티드화합물
EP0948341A4 (en) * 1996-09-17 2003-05-21 Supergen Inc DERIVATIVES OF PHOSPHOLIPIDIC DRUGS
US6436989B1 (en) * 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
JP2001527062A (ja) * 1997-12-24 2001-12-25 バーテックス ファーマシューティカルズ インコーポレイテッド アスパルチルプロテアーゼインヒビターのプロドラッグ
US6312662B1 (en) * 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
AU4125099A (en) 1998-06-01 1999-12-20 S & T Science And Technology Inc. Antiviral phosphorus derivatives of 4'-thio-5-ethyl-2'-deoxyuridine
GB9815567D0 (en) * 1998-07-18 1998-09-16 Glaxo Group Ltd Antiviral compound
TWI260322B (en) * 1999-02-12 2006-08-21 Vertex Pharma Inhibitors of aspartyl protease
US6258831B1 (en) * 1999-03-31 2001-07-10 The Procter & Gamble Company Viral treatment
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
EP1210121A2 (en) 1999-08-24 2002-06-05 Cellgate Inc. Enhancing drug delivery across and into epithelial tissues using oligo arginine moieties
GB9920872D0 (en) 1999-09-04 1999-11-10 Glaxo Group Ltd Benzophenones as inhibitors of reverse transcriptase
IL131887A0 (en) 1999-09-14 2001-03-19 Dpharm Ltd Phospholipid prodrugs of anti-proliferative drugs
ES2300281T3 (es) * 1999-12-03 2008-06-16 The Regents Of The University Of California At San Diego Compuestos de fosfonato.
JP2003518128A (ja) 1999-12-22 2003-06-03 メルク フロスト カナダ アンド カンパニー タンパク質チロシンホスファターゼ１ｂ（ｐｔｐ−１ｂ）のインヒビターとなる芳香族ホスホネート
WO2001064693A1 (fr) 2000-02-29 2001-09-07 Mitsubishi Pharma Corporation Compose de nucleotide de phosphonate
PL359364A1 (en) 2000-06-13 2004-08-23 Shionogi & Co, Ltd. Medicinal compositions containing propenone derivatives
FR2810322B1 (fr) * 2000-06-14 2006-11-10 Pasteur Institut PRODUCTION COMBINATOIRE D'ANALOGUES DE NUCLEOTIDES ET NUCLEOTIDES (XiTP)
UA72612C2 (en) 2000-07-06 2005-03-15 Pyrido[2.3-d]pyrimidine and pyrimido[4.5-d]pyrimidine nucleoside analogues, prodrugs and method for inhibiting growth of neoplastic cells
US6617310B2 (en) 2000-07-19 2003-09-09 Bristol-Myers Squibb Pharma Company Phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines
PL213214B1 (pl) 2000-07-21 2013-01-31 Gilead Sciences Diastereoizomerycznie wzbogacone proleki fosfonianowych analogów nukleotydowych oraz kompozycje zawierajace takie zwiazki
US6420586B1 (en) * 2000-08-15 2002-07-16 University Of Kansas Amino acid-derived cyclic phosphonamides and methods of synthesizing the same
MY134070A (en) 2001-01-22 2007-11-30 Isis Pharmaceuticals Inc Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
GB0114286D0 (en) 2001-06-12 2001-08-01 Hoffmann La Roche Nucleoside Derivatives
EP1402024B1 (en) * 2001-06-20 2007-08-22 Nuevolution A/S Templated molecules and methods for using such molecules
KR20020097384A (ko) 2001-06-20 2002-12-31 미쯔비시 도꾜 세이야꾸 가부시끼가이샤 기존의 약제에 내성변이를 가지는 바이러스에 유효한 약제
JP2005508924A (ja) 2001-08-30 2005-04-07 三菱ウェルファーマ株式会社 抗ウイルス剤
AU2002343556A1 (en) 2001-12-07 2003-06-23 Eli Lilly And Company Use of phosphonate nucleotide analogue for treating hepatitis b virus infections
ATE423563T1 (de) 2001-12-21 2009-03-15 Guilford Pharm Inc Verfahren zur herstellung von wasserlöslichen phosphonooxymethyl-derivaten aus alkohol und phenol
JP4547911B2 (ja) 2002-02-01 2010-09-22 アリアド・ファーマシューティカルズ・インコーポレイテッド リン含有化合物およびその用途
AU2003217393B8 (en) 2002-02-08 2009-06-25 Conforma Therapeutics Corporation Ansamycins having improved pharmacological and biological properties
AU2003216523A1 (en) 2002-03-18 2003-10-08 Mitsubishi Pharma Corporation Treatment of pre-core hepatitis b virus mutant infections
AU2003231766A1 (en) * 2002-04-26 2003-11-10 Gilead Sciences, Inc. Non nucleoside reverse transcriptase inhibitors
US20050239054A1 (en) * 2002-04-26 2005-10-27 Arimilli Murty N Method and compositions for identifying anti-HIV therapeutic compounds
BRPI0407374A (pt) 2003-02-19 2006-01-10 Univ Yale Análogos de nucleosìdeo antiviral e métodos para tratar infecções virais, especialmente infecções de hiv
CA2522845A1 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates

Also Published As

Publication number Publication date
NO20045152L (no) 2005-01-24
AU2003291998A8 (en) 2004-11-23
KR100987815B1 (ko) 2010-10-18
WO2003091264A2 (en) 2003-11-06
TW200408645A (en) 2004-06-01
US20050197320A1 (en) 2005-09-08
US20040121316A1 (en) 2004-06-24
AU2003231766A1 (en) 2003-11-10
AU2003228707A1 (en) 2003-11-10
IS2714B (is) 2011-01-15
CA2481285A1 (en) 2003-11-06
CN101074242A (zh) 2007-11-21
CA2481261C (en) 2011-11-01
IL164490A (en) 2010-11-30
UA80819C2 (en) 2007-11-12
NO20045150L (no) 2005-01-26
JP2006524487A (ja) 2006-11-02
US20070190523A1 (en) 2007-08-16
WO2003091264A3 (en) 2004-03-11
EP1509537A2 (en) 2005-03-02
EA200401436A1 (ru) 2005-04-28
EA008775B1 (ru) 2007-08-31
BR0309557A (pt) 2005-03-01
BR0309573A (pt) 2005-02-01
WO2004096818A2 (en) 2004-11-11
WO2003090690A2 (en) 2003-11-06
WO2004096818A3 (en) 2005-04-07
JP2005523912A (ja) 2005-08-11
AU2003231765A1 (en) 2003-11-10
EP1575486A4 (en) 2007-02-28
CN1649885A (zh) 2005-08-03
JP4942915B2 (ja) 2012-05-30
US20070010489A1 (en) 2007-01-11
EP1509537B9 (en) 2007-11-14
ATE367394T1 (de) 2007-08-15
ZA200409376B (en) 2005-11-30
HRP20041113B1 (en) 2008-09-30
IS7555A (is) 2004-11-25
NO336469B1 (no) 2015-08-31
PT1509537E (pt) 2007-11-02
WO2003090690A3 (en) 2004-06-24
DE60315023T2 (de) 2008-04-03
PL374968A1 (en) 2005-11-14
IL164491A0 (en) 2005-12-18
TW200404075A (en) 2004-03-16
ES2290485T3 (es) 2008-02-16
US20050209197A1 (en) 2005-09-22
MXPA04010527A (es) 2004-12-13
US20060115815A1 (en) 2006-06-01
CN1656109A (zh) 2005-08-17
HRP20041113A2 (en) 2005-08-31
PL374522A1 (en) 2005-10-31
HRP20041114A2 (en) 2005-08-31
KR20040108757A (ko) 2004-12-24
KR20040108756A (ko) 2004-12-24
EP1509537B1 (en) 2007-07-18
HK1073467A1 (en) 2005-10-07
WO2003090691A3 (en) 2006-02-09
EP1575486A2 (en) 2005-09-21
AU2003231765B9 (en) 2010-01-28
JP2006508634A (ja) 2006-03-16
NZ535828A (en) 2007-10-26
ZA200409377B (en) 2006-03-29
US7649015B2 (en) 2010-01-19
IS7556A (is) 2004-11-25
CN1313472C (zh) 2007-05-02
WO2003090691A2 (en) 2003-11-06
JP2005523922A (ja) 2005-08-11
EA200401437A1 (ru) 2005-04-28
IL164490A0 (en) 2005-12-18
CN101041669A (zh) 2007-09-26
TWI332956B (en) 2010-11-11
CA2481449A1 (en) 2003-11-06
SI1509537T1 (sl) 2008-02-29
EP1620445A2 (en) 2006-02-01
CA2481261A1 (en) 2003-11-06
EP1501841A2 (en) 2005-02-02
PL211979B1 (pl) 2012-07-31
AU2003231765B2 (en) 2009-12-10
US20060128692A1 (en) 2006-06-15
AU2003291998A1 (en) 2004-11-23
DE60315023D1 (de) 2007-08-30
JP2009112319A (ja) 2009-05-28
MXPA04010528A (es) 2005-05-27
US7462608B2 (en) 2008-12-09
DK1509537T3 (da) 2007-11-12

Similar Documents

Publication Publication Date Title
CY1108036T1 (el) Κυτταρικη συσσωρευση φωσφονικων αναλογων ενωσεων αναστολεα πρωτεασης του ιου ανοσολογικης ανεπαρκειας του ανθρωπου (hiv) και οι ενωσεις ως τετοιες
TR200201187T2 (tr) Ters transkriptazın inhibitörleri olarak benzofenonlar
ECSP088258A (es) Inhibidores de serina proteasas
CY1111225T1 (el) Νεα πεπτιδια ως αναστολεις πρωτεασης νs3-σερινης ιου ηπατiτιδας c
EA200600498A1 (ru) Макроциклические пептиды, проявляющие противовирусную активность в отношении вируса гепатита с
CY2013043I1 (el) Ενωσεις 4-οξοκινολινης και χρησιμοποιηση αυτων ως αναστολεις της ενσωματασης του hiv
CR20120356A (es) Nuevos compuestos heterocíclicos activos como inhibidores de beta-lactamasas
EA200700488A1 (ru) S-ТРИАЗОЛИЛ-α-МЕРКАПТОАЦЕТАНИЛИДЫ КАК ИНГИБИТОРЫ ОБРАТНОЙ ТРАНСКРИПТАЗЫ ВИЧ
BRPI0410456A (pt) compostos inibidores de hepatite c, composição farmacêutica, uso dos mesmos, bem como artigo de fabricação
NO20051082L (no) Antimikrobielle kinoloner, deres sammensetninger og anvendelser
ATE373005T1 (de) Thienopyrrole als antivirale mittel
ECSP055844A (es) Nuevos compuestos triciclicos
ATE349448T1 (de) Pyrazol-3,4-d-pyrimidinderivate und ihre verwendung bei der behandlung von h.pylori- infektionen
SE0302304D0 (sv) Novel compounds
BRPI0509667A (pt) azaquinazolinas substituìdas com eficácia antiviral
SE0100733D0 (sv) Non-nucleoside reverse transcriptase inhibitors
DE602004013011D1 (de) Haarbehandlungszusammensetzungen
BR0313400A (pt) N-aril-2-oxazolidinonas e seus derivados
PT1358182E (pt) Derivados de diazocinas e sua utilizacao como inibidores de triptase
DOP2002000405A (es) 1-biaril-1,8-naftiridin-4-ona inhibidores de la fosfodisterasa-4.