Diaromatic substituted compounds as anti-HIV-1 agents
First Claim
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1. A diaromatic substituted compound of formula (III) ##STR31## where R1 is --CH2 -- or --CO--;
- where Z is ##STR32## where n12 is 1 and n13 is 1, ##STR33## where Y3 is --N(Y3-1)-- where Y3-1 is C1 -C4 alkyl and n12 and n13 are as defined above;
where R6 is --N═
;
where R7 is --N(R7-5)(R7-6) where R7-5 isC1 --C6 alkyl,--CH2 --cyclopropyl,--CH2 --CH2 F, and where R7-6 is --H;
where R8 is --CR8-1 ═
where R8-1 is --H or --F;
where R9 is --CR9-1 ═
where R9-1 is --H or --F;
where R10 is --CR10-1 ═
where R10-1 is --H or --F;
where Aryl/Heteroaryl is a substituent selected from the group of substituents of formula (7) ##STR34## where . . . . is a double bond;
where Q1 is --NX11 -- where X11 is --H;
where X14 is --H,--O--CH2 --φ
,--O--CH2 --COOR14-10 where R14-10 is--H,C1 -C4 alkyl,--CH2 --φ
,C1 -C6 alkyl,--F, --Cl, Br,--O--SO2 --X14-11 where X14-11 is C1 -C4 alkyl,--NO2, --NH2, --N3,--NH--SO2 --X14-1 where X14-1 is C1 -C6 alkyl,--N═
C(X14-4)--N(X14-7)(X14-8) where(a) X14-4 is --H or C1 -C4 alkyl and where X14-7 and X14-8 are the same or different and are C1 -C6 alkyl,--N(X14-2)--CO--X14-9 where X14-2 is --H or C1 -C4 alkyl and where X14-9 is--H,C1 -C4 alkyl or--φ
where X14-2 is defined above;
where n7 is 0 or 1;
where X6 is --H,--OH,--O--CH2 --φ
,--CHO,C1 -C3 alkoxy,--O--SO2 --X6-12 where X6-12 is C1 -C4 alkyl,--C.tbd.N,--O--(CH2)n3 --N(X6-3)(X6-4) where n3 is 2 thru 5, where X6-3 is --H or where X6-3 and X6-4 are taken together with the attached nitrogen atom to form a heterocyclic ring selected from the group consisting of 1-pyrrolidinyl, 1-piperidinyl, 1-piperazinyl, N-morpholinyl or 1-aziridinyl,--(CH2)n24 --OH, where n24 is 1,--NH--SO2 --X6-7 where X6-7 is C1 -C4 alkyl, enantiomers, pharmaceutically acceptable salts, hydrates and solvates thereof.
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Abstract
The present invention includes diaromatic substituted heterocyclic compounds (III) ##STR1## which are useful in treating individuals infected with the HIV virus.
34 Citations
11 Claims
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1. A diaromatic substituted compound of formula (III) ##STR31## where R1 is --CH2 -- or --CO--;
- where Z is ##STR32## where n12 is 1 and n13 is 1, ##STR33## where Y3 is --N(Y3-1)-- where Y3-1 is C1 -C4 alkyl and n12 and n13 are as defined above;
where R6 is --N═
;where R7 is --N(R7-5)(R7-6) where R7-5 is C1 --C6 alkyl, --CH2 --cyclopropyl, --CH2 --CH2 F, and where R7-6 is --H; where R8 is --CR8-1 ═
where R8-1 is --H or --F;where R9 is --CR9-1 ═
where R9-1 is --H or --F;where R10 is --CR10-1 ═
where R10-1 is --H or --F;where Aryl/Heteroaryl is a substituent selected from the group of substituents of formula (7) ##STR34## where . . . . is a double bond;
where Q1 is --NX11 -- where X11 is --H;where X14 is --H, --O--CH2 --φ
,--O--CH2 --COOR14-10 where R14-10 is --H, C1 -C4 alkyl, --CH2 --φ
,C1 -C6 alkyl, --F, --Cl, Br, --O--SO2 --X14-11 where X14-11 is C1 -C4 alkyl, --NO2, --NH2, --N3, --NH--SO2 --X14-1 where X14-1 is C1 -C6 alkyl, --N═
C(X14-4)--N(X14-7)(X14-8) where(a) X14-4 is --H or C1 -C4 alkyl and where X14-7 and X14-8 are the same or different and are C1 -C6 alkyl, --N(X14-2)--CO--X14-9 where X14-2 is --H or C1 -C4 alkyl and where X14-9 is --H, C1 -C4 alkyl or --φ
where X14-2 is defined above;where n7 is 0 or 1; where X6 is --H, --OH, --O--CH2 --φ
,--CHO, C1 -C3 alkoxy, --O--SO2 --X6-12 where X6-12 is C1 -C4 alkyl, --C.tbd.N, --O--(CH2)n3 --N(X6-3)(X6-4) where n3 is 2 thru 5, where X6-3 is --H or where X6-3 and X6-4 are taken together with the attached nitrogen atom to form a heterocyclic ring selected from the group consisting of 1-pyrrolidinyl, 1-piperidinyl, 1-piperazinyl, N-morpholinyl or 1-aziridinyl, --(CH2)n24 --OH, where n24 is 1, --NH--SO2 --X6-7 where X6-7 is C1 -C4 alkyl, enantiomers, pharmaceutically acceptable salts, hydrates and solvates thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11)
- where Z is ##STR32## where n12 is 1 and n13 is 1, ##STR33## where Y3 is --N(Y3-1)-- where Y3-1 is C1 -C4 alkyl and n12 and n13 are as defined above;
Specification
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Current AssigneePharmacia & Upjohn Company (Pfizer Inc.)
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Original AssigneeThe Upjohn Company (Pharmacia Corp.)
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InventorsThomas, Richard C., Palmer, John R., Romero, Donna L., Smith, Herman W., Aristoff, Paul A.
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Primary Examiner(s)TSANG, CECILIA J
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Application NumberUS08/198,428Time in Patent Office959 DaysField of Search544/364, 544/360, 514/253, 514/318, 546/193US Class Current514/253.09CPC Class CodesC07D 209/42 Carbon atoms having three b...C07D 213/74 Amino or imino radicals sub...C07D 295/192 from aromatic carboxylic acidsC07D 401/12 linked by a chain containin...C07D 401/14 containing three or more he...C07D 403/12 linked by a chain containin...C07D 403/14 containing three or more he...C07D 405/12 linked by a chain containin...C07D 471/04 Ortho-condensed systemsC07D 491/04 Ortho-condensed systems
