FI118986B - Kombinationer av retrovirushärledda proteasinhibitorer - Google Patents

Kombinationer av retrovirushärledda proteasinhibitorer Download PDF

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FI118986B
FI118986B FI964835A FI964835A FI118986B FI 118986 B FI118986 B FI 118986B FI 964835 A FI964835 A FI 964835A FI 964835 A FI964835 A FI 964835A FI 118986 B FI118986 B FI 118986B
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amino
hydroxy
phenylmethyl
methyl
propyl
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Martin L Bryant
Karen E Potts
Mary Smidt
Simon P Tucker
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Searle & Co
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Claims (16)

1. Användning av (a) en effektiv mängd av en första retroviral pro-5 teasinhibitor; och (b) en effektiv mängd av en andra retroviral pro-teasinhibitor, för framställning av ett medikament, som är avsett för behandling av retrovirusinfektioner i däggdjur, varvid nämnda andra retrovirala proteasinhibitor är effek- 10 tiv mot minst en sädan retrovirusstam, som är resistent mot nämnda första retrovirala proteasinhibitor, och varvid nämnda första retrovirala proteasinhibitor är N-(2(R)-hydroxi-1(S)-indanyl)-2(R)-fenylmetyl-4(S)-hydro-15 xi-5-(1-(4-(3-pyridylmetyl)-2(S)-N'-(t-butylkarboxamido)- piperazinyl))pentanamid; N-tert. -butyldekahydro-2-[2 (R) -hydroxi-4-fenyl-3 (S) -[[N- (2-kinolylkarbonyl) -L-asparaginyl]amino]butyl]- (4aR, 8aS) -iso-kinolin-3(s)-karboxamid; 20 (2S, 3R, 4S, 5S)-2,5-bis-[N-[N-[[N-metyl-N-(2-pyridinyl- metyl) amino]karbonyl]valinyl]amino] - 3,4 -dihydroxi -1,6-!.: : difenylhexan; • (2S, 3S, 5S)-5-[N-[N-[N-metyl-N-[ (2-isopropyl-4-tiazolyl) - ί V: me tyl]amino]karbonyl]valinyl]amino] - 2 - [N- [ (5 - tiazolyl) metoxi - *·· 25 karbonyljamino]-3-hydroxi-1,6-difenylhexan; . .·. [2-hydroxi-3-[[ (4-aminof enyl) sulfonyl]- (2-metylpropyl) - *«· amino]-IS- (fenylmetyl)propyl]karbaminsyra-3S-tetrahydro-furanylester; . . N-tert.-butyldekahydro-2-Γ2 (R) -hydroxi-4- (fenyltio) -3 (S) -ΓΓ
30 N-[ (2-metyl-3-hydroxifenyl) karbonyl]amino]butyl]- (4aR, 8aS) - • · ’···* isokinolin-3 (S) -karboxamid; ·** [4R-(4α, 5α, 6β, 7β)]-1,3-bis-[(3-aminofenyl)metyl]hexahydro- 5,6-dihydroxi-4,7-bis (fenylmetyl) -2H-1,3-diazepin-2-on; * . N-[2R-hydroxi-3-[[ (1,3-bensodioxol-5-yl) sulfonyl] (2-metyl- ] 35 propyl) amino]-lS-(fenylmetyl)propyl]-2S-[[pyrrolidin-l-yl) - acetyl]amino]-3,3-dimetylbutanamid; 118986 N-[2-R-hydroxi-3-[ (2-metylpropyl) -[ (1,3-bensodioxol-5-yl) -sulfonyl]amino]-lS- (fenylmetyl)propyl]-2S-metyl-3- (metyl-sulfonyl)propanamid; [1S-[1R* (R*), 2S*)]]-N-[2-hydroxi-3-[N1- (2-metylpropyl) -N1- (4- 5 metoxifenylsulfonyl) amino]-1- (fenylmetyl) propyl]-2-me tyl-3-(metylsulfonyl)propanamid; 2S-[[N-metylamino) acetyl]amino]-N-[2R-hydroxi-3-[[ (1,3-benso-dioxol-5-yl) sulfonyl] (2-metylpropyl) amino]-lS- (fenylmetyl) -propyl]-3,3-dimetylbutanamid; eller 10 (2R, 3S)-3-(N-metylaminoacetyl-L-tert-butylglycinyl)amino- l-(N-isoamyl-N-(tert-butylkarbomyl)) amino-4-fenyl-butanol.
2. Användning enligt patentkrav 1, där nämda för-sta och andra inhibitor administreras sä, att en effektiv mängd av bäda inhibitorerna är närvarande i nämda dägg- 15 djur.
3. Användning enligt patentkrav 1, där nämda för-sta och andra inhibitor administreras alternerat sä, att en effektiv mängd av en inhibitor i gängen är närvarande i nämda däggdjur.
4. Användning enligt patentkrav 1, där nämda andra retrovirala proteasinhibitor är • * · N- (2 (R) -hydroxi-l (S)-indanyl)-2 (R)-fenylmetyl-4 (S) - • *t! hydroxi-5- (1- (4- (3-pyridylmetyl) -2 (S) -N' - (t-butylkarbox- iV; amido)piperazinyl))pentanamid; ··· 25 N-tert-butyldekahydro-2-r2 (R) -hydroxi-4-fenyl-3 (S) -ΓΓΝ- (2- . .·. kinolylkarbonyl) -L-asparginyl]amino]butyl]- (4aR, 8aS) -iso- ··· kinolin-3 (S) -karboxamid; # · · (2S, 3S, 4S, 5S)-2,5-bis-[N-[N-[[N-metyl-N-(2-pridinylmetyl)- , , amino]karbonyl]valinyl]amino]-3,4-dihydroxi-l, 6-difenyl- ’·*·* 3 0 hexan; ··· ' *·;·* (2S, 3S, 5S) -5-bis-[N-[N-[N-metyl-N- (2-isopropyl) -4-tiazolyl) - *:* metyl]amino]karbonyl]valinyl]amino] - 2 - [N- [ (5 -1 iazolyl) metoxi - ;***; karbony ljamino - 3 -hydroxi -1,6 -di fenyl hexan; ··· * . [2-hydroxi-3-[[ (4-aminofenyl) sulfonyl]- (2-metylpropyl) - 3. amino]-lS-(fenylmetyl)propyl]karbaminsyra-3S-tetrahydro- * * furanylester; 1 1 8986 N-tert. -butyldekahydro-2-[2 (R) -hydroxi-4- (fenyltio) -3 (S) -[[ N-[ (2-metyl-3-hydroxifenyl) karbonyl]amino]butyl]- (4aR, 8aS) -isokinolin-3(S)-karboxamid; [4R- (4<χ, 5a, 6β, 7β) ]-l# 3-bis-[ (3-aminofenyl)metyl]hexa- 5 hydro-5,6-dihydroxi-4,7-bis(fenylmetyl)-2H-1,3-diazepin-2-on,- N-[2R-hydroxi-3-[[ (1,3-bensodioxol-5-yl) sulfonyl] (2-metyl-propyl)amino]-IS- (fenylmetyl) propyl]-2S-[[pyrrolidin-l-yl) -acetyl]amino]-3,3-dimetylbutanamid;
5 N-[ (2-metyl-3-hydroxifenyl) karbonyl]amino]butyl]- (4aR, 8aS)- isokinolin-3(S)-karboxamid; [4R-(4α, 5a, 6β, 7β)]-ΐ, 3-bis-[(3-aminofenyl)metyl]hexahydro- 5,6-dihydroxi-4,7-bis(fenylmetyl)-2H-1,3-diazepin-2-on; N-[2R-hydroxi-3-[[ (1,3-bensodioxol-5-yl) sulfonyl] (2-metyl-10 propyl)amino]-IS- (fenylmetyl)propyl]-2S-[[pyrrolidin-l-yl) -acetyl]amino]-3,3-dimetylbutanamid; N-[2-R-hydroxi-3-[(2-metylpropyl) -[(1,3-bensodioxol-5-yl) -sulfonyl]amino]-lS- (fenylmetyl)propyl]-2S-metyl-3- (metyl-sulfonyl)propanamid; 15 [1S-[1R* (R*), 2S*)]]-N-[2-hydroxi-3-[N1- (2-metylpropyl) -N1- (4-metoxifenylsulfony 1)amino]-1 - (fenyImety 1)propyl]-2-metyl-3-(metylsulfonyl)propanamid; eller (2R, 3 S)-3-(N-metylaminoacetyl-L-tert-butylglycinyl)amino-1- (N-isoamyl-N- (tert-butylkarbomyl) ) amino-4 - f eny 1-butanol ,-20 och ämnda andra retrovirala proteasinhibitor är 2S-[[N-metylamino) acetyl]amino]-N-[2R-hydroxi-3-[[ (1,3-benso-!*; i dioxol-5-yl) sulfonyl] (2-metylpropyl) amino]-lS- (fenylmetyl) - • propyl]-3,3-dimetylbutanamid. ί#:*ϊ
6. Användning enligt patentkrav 1, där nämnda för- *ί* 25 sta retrovirala proteasinhibitor är ···« • ·*; N- (2 (R) -hydroxi-1 (S) -indanyl) -2 (R) -fenylmetyl-4 (S) -hydroxi- ··· 5- (1- (4- (3-pyridylmetyl) - 2 (S) -N' - (t-butylkarboxamido) - • * piperazinyl))pentanamid; och .. nämnda andra retrovirala proteasinhibitor är • * * 30 (2R, 3S)-3-(N-metylaminoacetyl-L-tert-butylglycinyl) amino- • « *·;·* 1- (N-isoamyl-N- (tert-butylkarbomyl) ) amino-4-fenyl-butanol; N-[2-R-hydroxi-3-[ (2-metylpropyl) [(1,3-bensodioxol-5-yl) - :***: sulfonyl]amino]-lS- (fenylmetyl) propyl]-2S-me tyl-3 - (metyl- * . sulfonyl)propanamid; *♦**· «···· • · 118986 [1S-[1R* (R*) , 2S*)]]-N-[2-hydroxi-3-[N1-(2-metylpropyl)-N1- (4-metoxifenylsulfonyl) amino]-l- (fenylmetyl)propyl]-2-metyl-3-(metylsulfonyl)propanamid; eller 2S-[[N-raetylamino) acetyl]amino]-N-[2R-hydroxi-3-[[ (1,3-benso-5 dioxol-5-yl) sulfonyl] (2-metylpropyl) amino]-lS- (fenylmetyl) -propyl] - 3,3 - dime tylbutanamid.
5. Användning enligt patentkrav 1, där nämnda för- • f :.: : sta retrovirala proteasinhibitor är • N- (2 (R) -hydroxi-1 (S) -indanyl) -2 (R) -fenylmetyl-4 (S) -hydroxi- :V: 5-(1-(4-(3-pyridylmetyl)-2(S)-N'-(t-butylkarboxamido)- ··· 25 piperazinyl) )pentanamid; ·«·· . N-tert-butyldekahydro-2-[2 (R) -hydroxi-4-fenyl-3 (S) -[[N- (2- kinolylkarbonyl) -L-asparginyl]amino]butyl]- (4aR, 8aS) -isokinolin-3 (S)-karboxamid; .. (2S, 3S, 4S, 5S)-2,5-bis-[N-[N-[[N-metyl-N-(2-pridinylmetyl)- 30 amino]karbonyl]valinyl]amino]-3,4-dihydroxi-l, 6-difenyl- • · *···* hexan; ·;· (2S, 3S, 5S)-5-bis-[N-[N-[N-metyl-N-(2-isopropyl)-4-tiazolyl)- j*·*. metyl]amino]karbonyl]valinyl]amino] - 2 - [N- [ (5 -1 iazolyl) me toxi - • · · • . karbonyl]amino-3-hydroxi-1,6-difenylhexan; • · • · 118986 1 [2-hydroxi-3-[[ (4-aminofenyl) sulfonyl]- (2-metylpropyl) -amino]-IS- (fenylmetyl) propyljkarbaminsyra-3S-tetrahydro-furanylester; N-tert.-butyldekahydro-2-[2 (R) -hydroxi-4- (fenyltio) -3 (S) -[[
7. Användning enligt patentkrav 1, där nämnda för-sta retrovirala proteasinhibitor är (2S, 3S, 5S)-5-bis-[N-[N-[N-metyl-N-(2-isopropyl)-4-tiazolyl) -10 metyl]amino]karbonyl]valinyl]amino]- 2 -[N-[ (5 -1iazolyl) metoxi -karbonyljamino-3 -hydroxi-1,6-dif enylhexan; och nämda andra retrovirala propteasinhibitor är 2S-[[N-metylamino) acetyl]amino]-N-[2R-hydroxi-3-[[ (1,3-bensodi-oxol-5-yl) sulfonyl] (2-metylpropyl) amino]-lS- (fenylmetyl) -15 propyl]-3,3 - dimetylbutanamid,- N-[2R-hydroxi-3-[[ (1,3-bensodioxol-5-yl) sulfonyl] (2-metylpropyl) amino]-IS- (fenylmetyl)propyl]-2S-[[pyrrolidin-l-yl) acetyl]amino]-3,3 -dimetylbutanamid; eller 2S-[[N-metylamino) acetyl]amino]-N-[2R-hydroxi-3-[[ (1,3-benso-20 dioxol-5-yl) sulfonyl] (2-metylpropyl) amino]-IS- (fenylmetyl) -propyl] - 3,3 - dimetylbutanamid. Ϊ.::
8. Användning enligt patentkrav 1, där en tredje ·· · • retroviral proteasinhibitor används, varvid nämnda tredje :Y: retrovirala proteasinhibitor är effektiv mot minst en vi- ··· 25 russtam, som är resistent mot bäde den första och den and- • ••2 . ,·. ra retrovirala proteasinhibitorn. *#·
9. Användning enligt patentkrav 8, där nämda tred- • « · je retroviral proteasinhibitor är , . N-(2(R)-hydroxi-1(S)-indanyl)-2(R)-fenylmetyl-4(S)-hydroxi- t · t V.· jo 5-(1-(4-(3-pyridylmetyl)-2(S)-Ν' - (t-butylkarboxamido)-• · *·;·* piperazinyl) ) pentanamid; ·;· N-tert. -butyldekahydro-2-[2 (R) -hydroxi-4-fenyl-3 (S) -[[N- (2- ·**·. kinolylkarbonyl) -L-asparaginyl]amino]butyl]- (4aR, 8aS) -iso- ··* • . kinolin-3(S)-karboxamid; • · 118986 (2S, 3R, 4S, 5S) -2,5-bis-[N-[N-[[N-metyl-N- (2-pyridinylmetyl) -amino]karbonyl]valinyl]amino]-3,4-dihydroxi-l, 6-difenyl-hexan; (2S, 3S, 5S)-5-[N-[N-[N-metyl-N-[(2-isopropyl-4-tiazolyl) - 5 metyl]amino]karbonyl]valinyl]amino] - 2 - [N- [ (5 -1 iazolyl) metoxi -karbonyljamino] - 3 - hydroxi -1,6 - di fenylhexan ,-[2-hydroxi-3-[[ (4-aminofenyl) sulfonyl]- (2-metylpropyl) -amino]-lS- (fenylmetyl)propyl]karbaminsyra-3S-tetrahydro-furanylester;
10. Användning enligt patentkrav 1, där minst en • · *···* virustsam, som är resistent mot nämnda första retrovirala ! *:· proteasinhibitor, och minst en virusstam, som är resistent ·*’*· mot nämnda andra retrovirala proteasinhibitor, vardera ··· f , producerar retrovirala proteaser, vilka har minst en ami- \ 35 nosyrasubstitution i proteaspeptidsekvenssen, varvid denna ····· * substitution inerkar pä samma omräde i substratbindnings- 118986 stället hos proteaset och bidrar tili den observerade in-hibitorresistenssen.
10 N-tert.-butyldekahydro-2-[2 (R)-hydroxi-4-(fenyltio)-3 (S) - [[N-[ (2-metyl-3-hydroxifenyl) karbonyl]amino]butyl]- (4aR, 8aS) - j isokinolin-3(S)-karboxamid; [4R- (4a, 5«, 6β, 7β) ] -1,3-bis-[ (3- aminofenyl)metyl]hexa- hydro-5,6-dihydroxi-4,7-bis(fenylmetyl)-2H-1,3-diazepin-2-15 on,· N-[2R-hydroxi-3-[[ (1,3-bensodioxol-5-yl) sulfonyl] (2-metylpropyl) amino]-IS- (fenylmetyl)propyl]-2S-[[pyrrolidin-l-yl) -acetyl]amino]-3,3-dimetylbutanamid; N-[2-R-hydroxi-3-[ (2-metylpropyl) -[(1,3-bensodioxol-5-yl) -20 sulfonyl]amino]-lS- (fenylmetyl)propyl]-2S-metyl-3- (metyl-sulfonyl)propanamid; Ϊ.Ϊ : [1S-[1R* (R*) , 2S*)]]-N-[2-hydroxi-3-[N1- (2-metylpropyl) -N1- ·· · • (4-me toxif enyl sulfonyl) amino]-l- (fenylmetyl) propyl]-2-• · iti#: metyl-3- (metylsulfonyl)propanamid; •j· 25 2S-[[N-metylamino) acetyl]amino]-N-[2R-hydroxi-3-[[ (1,3-benso- . dioxol-5-yl) sulfonyl] (2-metylpropyl) amino]-IS- (fenylmetyl) - • M .···. propyl]-3,3-dimetylbutanamid; eller • * (2R, 3S)-3-(N-metylaminoacetyl-L-tert-butylglycinyl)amino- . . 1-(N-isoamyl-N-(tert-butylkarbomyl))amino-4-fenyl-butanol. * · «
10 N-[2-R-hydroxi-3-[ (2-metylpropyl) -[ (1,3-bensodioxol-5-yl) -sulfonyl]amino]-lS- (fenylmetyl)propyl]-2S-metyl-3- (metyl-sulfonyl)propanamid; [1S-[1R* (R*) , 2S*) ]]-N-[2-hydroxi-3-[N1-(2-metylpropyl)-N1- (4-metoxifeny 1 sulfonyl) amino]-1-(fenylmetyl) propyl]- 2 -15 metyl-3-(metylsulfonyl)propanamid; 2S-[[N-metylamino) acetyl]amino]-N-[2R-hydroxi-3-[[ (1,3-bensodioxol-5-yl) sulfonyl] (2-metylpropyl) amino]-IS -(fenylmetyl)propyl]-3,3-dimetylbutanamid; eller (2R, 3S)-3-(N-metylaminoacetyl-L-tert-butylglycinyl)amino- 20 1-(N-isoamyl-N-(tert-butylkarbomyl)) amino-4-fenyl-butanol.
11, Användning enligt patentkrav 1, där ytterliga-re ett antiviralt medel, som är annat än en proteasinhibi- 5 tor, används.
12. Användning enligt patentkrav 11, där nämnda antivirala medel är en nukleosidanalog, inhibitor för om-vänd icke-nuleosidtranskriptas, tat-antagonist eller gly-kosidasinhibitor.
13. Användning enligt patentkrav 12, där namnda nukleosidanalog är AZT, DDI, DDC, 3YC, D4T eller PMEA och nämda glykosidasinhibitor är castanospermin eller N-butyl-1-deoxinoj irmycin.
14. Användning enligt patentkrav l, där nämnda 15 däggdjur är människa, apa eller katt.
15. Användning enligt patentkrav 1, där nämda retrovirus är HIV eller HTLV.
16. Användning enligt patentkrav 15, där nämda retrovirus är HIV-1 eller HIV-2. • · • t · • · · ··· · ·· 1 • · · • · • · • · • · i • · a m 1 • ··1 ···1 • · · f · 1 ··· *·· • · « » · · • · • · · • · · • 1 ·2 3 • · • · ··· •e 2 *·· 3 • · • 1 • e1 m • · * • 1
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