HRP20041113B1 - Stanična akumulacija fosfonatnih analoga spojeva koji su inhibitori proteaze hiv - Google Patents

Stanična akumulacija fosfonatnih analoga spojeva koji su inhibitori proteaze hiv

Info

Publication number
HRP20041113B1
HRP20041113B1 HR20041113A HRP20041113A HRP20041113B1 HR P20041113 B1 HRP20041113 B1 HR P20041113B1 HR 20041113 A HR20041113 A HR 20041113A HR P20041113 A HRP20041113 A HR P20041113A HR P20041113 B1 HRP20041113 B1 HR P20041113B1
Authority
HR
Croatia
Prior art keywords
compounds
hiv protease
protease inhibitor
cellular accumulation
phosphonate analogs
Prior art date
Application number
HR20041113A
Other languages
English (en)
Inventor
N. Arimilli Murty
M. Becker Mark
Bryant Clifford
M. Chen James
Chen Xiaowu
Dastgah Azar
Fardis Maria
He Gong-Xin
Jin Haolun
U. Kim Choung
A. Lee William
P. Lee Christopher
Lin Kuel-Ying
Liu Hongtao
L. Mackman Richard
L. Mitchell Michael
H. Nelson Peter
Pyun Hyung-Jung
D. Rowe Tanisha
Sparacino Mark
Swaminathan Sundaramoorthi
D. Tario James
Wang Jianying
A. Williams Matthew
Xu Lianhong
Yang Zheng-Yu
H. Yu Richard
Zhang Jiancun
Zhang Lijun
Original Assignee
Gilead Sciences
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 filed Critical Gilead Sciences
Publication of HRP20041113A2 publication Critical patent/HRP20041113A2/hr
Publication of HRP20041113B1 publication Critical patent/HRP20041113B1/hr

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    • 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
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • 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, i.e. RP(=X)(XH)2 (X = S, 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
    • A61K31/33—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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
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    • A61P31/18—Antivirals for RNA viruses for HIV
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    • 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
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    • 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
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    • C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
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    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
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    • C07F9/38—Phosphonic acids RP(=O)(OH)2; Thiophosphonic acids, i.e. RP(=X)(XH)2 (X = S, Se)
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    • C07F9/40—Esters thereof
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Abstract

Spoj odabran od sljedećih formula: naznačen time daY1 je neovisno O, S, N(RX), N(O)(RX), N(ORX), N(O)(ORX) ili N(N(RX)(RX)); Y2 je neovisno O, N(RX),N(O)(RX), N(ORX), N(O)(ORX), N(N(RX)(RX)), -S(O)M2- ili -S(O)M2-S(O)M2-;Rx neovisno jest H, R1, W3,zaštitna skupina ili formula: Ry neovisno jest H,W3, R2 ili zaštitna skupina; R1 neovisno jest H ili alkil od 1 do 18 atoma ugljika; R2 neovisno jest H, R1, R3 ili R4 pri čemu svaki R4 jest neovisnosupstiutiran s 0 do 3 R3 skupinama, ili uzeti zajedno na ugljikovom atomu dvije R2 skupine tvore prsten od 3 do 8 ugljika a prsten može biti supstituiran s 0 do 3 R3 skupinama; R3 jest R3a, R3b, R3c ili R3d s tim kada je R3 vezan na heteroatom, tadaR3 jest R3c ili R3d;R3a jest F, Cl, Br, I, -CN, N3 ili -NO2;R3b jest Y1;R3c jest Rx, N(RX) (Rx), -SRX, -S(O)RX, -S(O)2RX, -S(O)(ORX), -OC(Y1)RX, -OC(Y1)ORX, -OC(Y1)(N(RX)(RX)), -SC(Y1)RX, -SC(Y1)ORX,-SC(Y1)(N(RX)(RX)), -N(RX)C(Y1)RX, -N(RX)C(Y1)ORXili - N(RX)C(Y1)(N(RX)(RX));R3d jest-C(Y1)RX, -C(Y1)ORX, ili -C(Y1)(N(RX)(RX));R4 jest alkil od 1 do 18 atoma ugljika, alkenil od 2 do 18 atoma ugljika ili alkinil od 2 do 18 atoma ugljika; R5 jest R4 pri čemu je svaki R4 supstituiran s 0 do 3 R3 skupinama; W3 jest W4 ili W5;W4 jest R5, -C(Y1)R5, -C(Y1)W5, - SO2R5, ili -SO2W5;W5 je karbociklil iliheterociklil pri čemu W5 neovisno jest supstituiran s od 0-3 R2 skupinama; W6 jest W3 koji je neovinso supstituiran s 1, 2, ili 3 A3 skupinama; M2 jest 0, 1 ili 2; M12a jest1, 2, 3, 4, 5, 6, 7, 8, 9,10, 11, ili 12; M12b jest 1, 2, 3, 4, 5, 6, 7, 8,9, 10, 11, ili 12; M1a, M1c i M1d neovisno jesu 0ili 1; teM12c jest 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 ili 12, te enantiomeri i dijastereomeri kaoi fiziološki prihvatljive soli. Patent sadrži još30 patentnih zahtjeva.
HR20041113A 2002-04-26 2004-11-24 Stanična akumulacija fosfonatnih analoga spojeva koji su inhibitori proteaze hiv HRP20041113B1 (hr)

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