
                                SEQUENCE LISTING

<110> Merck Sharp & Dohme Corp.
      Aaronson, Jeffrey G.
      Barnett, Stanley F.
      Bartz, Rene
      Colletti, Steven L.
      Jadhav, Vasant R.
      Momose, Aaron A.
      Shaw, Anthony W.
      Tellers, David M.
      Tucker, Thomas J.
      Wang, Weimin
      Yuan, Yu

<120> NOVEL SINGLE CHEMICAL ENTITIES AND
  METHODS FOR DELIVERY OF OLIGONUCLEOTIDES
  

<130> MRL-MIS-00023

<150> 61/322,422          
<151> 2010-04-09  

<160> 59

<170> FastSEQ for Windows Version 4.0

<210> 1
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 1
His Phe His His Phe Phe His His Phe Phe His Phe Phe His His Phe
 1               5                  10                  15      
Phe His His Phe
            20  


<210> 2
<211> 15
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 2
Trp His His Trp Trp His Trp Trp His His Trp Trp His His Trp
 1               5                  10                  15  


<210> 3
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 3
His Trp His His Leu Leu His His Leu Leu His Leu Leu His His Leu
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 4
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 4
His Leu His His Trp Leu His His Leu Leu His Leu Leu His His Leu
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 5
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 5
His Leu His His Leu Trp His His Leu Leu His Leu Leu His His Leu
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 6
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 6
His Leu His His Leu Leu His His Leu Trp His Leu Leu His His Leu
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 7
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 7
His Leu His His Leu Leu His His Leu Leu His Trp Leu His His Leu
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 8
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 8
His Leu His His Leu Leu His His Leu Leu His Leu Leu His His Trp
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 9
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 9
His Leu His His Leu Leu His His Leu Leu His Leu Leu His His Leu
 1               5                  10                  15      
Trp His His Leu
            20  


<210> 10
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 10
His Pro His His Leu Leu His His Leu Leu His Leu Leu His His Leu
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 11
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 11
His Leu His His Pro Leu His His Leu Leu His Leu Leu His His Leu
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 12
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 12
His Leu His His Leu Pro His His Leu Leu His Leu Leu His His Leu
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 13
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 13
His Leu His His Leu Leu His His Leu Pro His Leu Leu His His Leu
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 14
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 14
His Leu His His Leu Leu His His Leu Leu His Leu Leu His His Leu
 1               5                  10                  15      
Pro His His Leu
            20  


<210> 15
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 15
His Leu His His Leu Leu His His Leu Leu His Leu Leu His His Leu
 1               5                  10                  15      
Leu His His Pro
            20  


<210> 16
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 16
Glu Leu Glu Glu Leu Leu Glu Glu Leu Leu His Leu Leu His His Leu
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 17
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 17
Glu Leu His His Leu Leu His Glu Leu Leu His Leu Leu His Glu Leu
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 18
<211> 21
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 18
Gly Leu Trp Arg Ala Leu Trp Arg Leu Leu Arg Ser Leu Trp Arg Leu
 1               5                  10                  15      
Leu Trp Arg Ala Cys
            20      


<210> 19
<211> 33
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 19
Gly Leu Phe Glu Ala Ile Glu Gly Phe Ile Glu Asn Gly Trp Glu Gly
 1               5                  10                  15      
Met Ile Asp Gly Trp Tyr Gly Tyr Gly Arg Lys Lys Arg Arg Gln Arg
            20                  25                  30          
Arg
    


<210> 20
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 20
His Leu His His Leu Leu His His Leu Leu His Leu Leu His His Leu
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 21
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 21
His Trp His His Trp Trp His His Trp Trp His Trp Trp His His Trp
 1               5                  10                  15      
Trp His His Trp
            20  


<210> 22
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 22
His Leu His His Leu Leu His His Trp Leu His Leu Leu His His Leu
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 23
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 23
His Leu His His Leu Leu His His Leu Leu His Leu Trp His His Leu
 1               5                  10                  15      
Leu His His Leu
            20  


<210> 24
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 24
His Leu His His Leu Leu His His Leu Leu His Leu Leu His His Leu
 1               5                  10                  15      
Leu His His Trp
            20  


<210> 25
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 25
His His His His His His His His His His Leu Leu Leu Leu Leu Leu
 1               5                  10                  15      
Leu Leu Leu Leu
            20  


<210> 26
<211> 14
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 26
His His His His His His His Leu Leu Leu Leu Leu Leu Leu
 1               5                  10                  


<210> 27
<211> 15
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 27
Leu Thr Thr Leu Leu Thr Leu Leu Thr Thr Leu Leu Thr Thr Leu
 1               5                  10                  15  


<210> 28
<211> 20
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 28
Lys Leu Leu Lys Leu Leu Lys Leu Trp Leu Lys Leu Leu Lys Leu Leu
 1               5                  10                  15      
Leu Lys Leu Leu
            20  


<210> 29
<211> 29
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 29
Leu His Leu Leu His His Leu Leu His His Leu His His Leu Leu His
 1               5                  10                  15      
His Leu Leu His Leu Leu His His Leu Leu His His Leu
            20                  25                  


<210> 30
<211> 13
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 30
Phe Leu Gly Gly Ile Ile Ser Phe Phe Lys Arg Leu Phe
 1               5                  10              


<210> 31
<211> 13
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 31
Phe Ile Gly Gly Ile Ile Ser Phe Ile Lys Lys Leu Phe
 1               5                  10              


<210> 32
<211> 13
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 32
Phe Ile Gly Gly Ile Ile Ser Leu Ile Lys Lys Leu Phe
 1               5                  10              


<210> 33
<211> 21
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 33
His Leu Leu His Leu Leu Leu His Leu Trp Leu His Leu Leu His Leu
 1               5                  10                  15      
Leu Leu His Leu Leu
            20      


<210> 34
<211> 27
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 34
Gly Ile Gly Gly Ala Val Leu Lys Val Leu Thr Thr Gly Leu Pro Ala
 1               5                  10                  15      
Leu Ile Ser Trp Ile Lys Arg Lys Arg Gln Gln
            20                  25          


<210> 35
<211> 18
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 35
Arg Gln Ile Lys Ile Trp Phe Gln Asn Arg Arg Met Lys Trp Lys Lys
 1               5                  10                  15      
Gly Gly
        


<210> 36
<211> 12
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 36
Arg Lys Lys Arg Arg Gln Arg Arg Arg Pro Pro Gln
 1               5                  10          


<210> 37
<211> 24
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 37
Gly Ala Leu Phe Leu Gly Trp Leu Gly Ala Ala Gly Ser Thr Met Gly
 1               5                  10                  15      
Ala Pro Lys Lys Lys Arg Lys Val
            20                  


<210> 38
<211> 37
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 38
Gly Gly Gly Ala Arg Lys Lys Ala Ala Lys Ala Ala Arg Lys Lys Ala
 1               5                  10                  15      
Ala Lys Ala Ala Arg Lys Lys Ala Ala Lys Ala Ala Arg Lys Lys Ala
            20                  25                  30          
Ala Lys Ala Ala Lys
        35          


<210> 39
<211> 27
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 39
Gly Trp Thr Leu Asn Ser Ala Gly Tyr Leu Leu Gly Lys Ile Asn Leu
 1               5                  10                  15      
Lys Ala Leu Ala Ala Leu Ala Lys Lys Ile Leu
            20                  25          


<210> 40
<211> 9
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 40
Arg Arg Arg Arg Arg Arg Arg Arg Arg
 1               5                  


<210> 41
<211> 31
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 41
Trp Glu Ala Lys Leu Ala Lys Ala Leu Ala Lys Ala Leu Ala Lys His
 1               5                  10                  15      
Ile Leu Ala Lys Ala Leu Ala Lys Ala Leu Lys Ala Cys Glu Ala
            20                  25                  30      


<210> 42
<211> 32
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 42
Trp Glu Ala Ala Leu Ala Glu Ala Leu Ala Glu Ala Leu Ala Glu His
 1               5                  10                  15      
Leu Ala Glu Ala Leu Ala Glu Ala Glu Ala Leu Glu Ala Leu Ala Ala
            20                  25                  30          


<210> 43
<211> 12
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<221> VARIANT        
<222> 2, 4, 6, 8, 10, 12
<223> Xaa = norleucine

<221> CARBOHYD       
<222> (1)...(1)
<223> NHC12H25

<400> 43
Asp Xaa Lys Xaa Lys Xaa His Xaa Lys Xaa His Xaa
 1               5                  10          


<210> 44
<211> 21
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 44
Lys Leu Leu Lys Leu Leu Leu Lys Leu Trp Leu Lys Leu Leu Lys Leu
 1               5                  10                  15      
Leu Leu Lys Leu Leu
            20      


<210> 45
<211> 23
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 45
Gly Leu Phe Glu Ala Ile Ala Gly Phe Ile Glu Asn Gly Trp Glu Gly
 1               5                  10                  15      
Met Ile Asp Gly Trp Tyr Gly
            20              


<210> 46
<211> 24
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 46
Gly Leu Phe His Ala Ile Ala Ala His Phe Ile His Gly Gly Trp His
 1               5                  10                  15      
Gly Leu Ile His Gly Trp Tyr Gly
            20                  


<210> 47
<211> 23
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 47
Gly Leu Phe Glu Ala Ile Ala Glu Phe Ile Glu Gly Gly Trp Glu Gly
 1               5                  10                  15      
Leu Ile Glu Gly Trp Tyr Gly
            20              


<210> 48
<211> 23
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 48
Gly Leu Phe Glu Ala Ile Glu Gly Phe Ile Glu Asn Gly Trp Glu Gly
 1               5                  10                  15      
Met Ile Asp Gly Trp Tyr Gly
            20              


<210> 49
<211> 23
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 49
Gly Leu Phe Lys Ala Ile Ala Lys Phe Ile Lys Gly Gly Trp Lys Gly
 1               5                  10                  15      
Leu Ile Lys Gly Trp Tyr Gly
            20              


<210> 50
<211> 33
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 50
Gly Leu Phe Glu Ala Ile Ala Gly Phe Ile Glu Asn Gly Trp Glu Gly
 1               5                  10                  15      
Met Ile Asp Gly Trp Tyr Gly Tyr Gly Arg Lys Lys Arg Arg Gln Arg
            20                  25                  30          
Arg
    


<210> 51
<211> 41
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 51
Gly Leu Phe Glu Ala Ile Ala Gly Phe Ile Glu Asn Gly Trp Glu Gly
 1               5                  10                  15      
Met Ile Asp Gly Trp Tyr Gly Arg Gln Ile Lys Ile Trp Phe Gln Asn
            20                  25                  30          
Arg Arg Met Lys Trp Lys Lys Gly Gly
        35                  40      


<210> 52
<211> 34
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 52
Gly Leu Phe His Ala Ile Ala Ala His Phe Ile His Gly Gly Trp His
 1               5                  10                  15      
Gly Leu Ile His Gly Trp Tyr Gly Tyr Gly Arg Lys Lys Arg Arg Gln
            20                  25                  30          
Arg Arg
        


<210> 53
<211> 33
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 53
Gly Leu Phe Glu Ala Ile Ala Glu Phe Ile Glu Gly Gly Trp Glu Gly
 1               5                  10                  15      
Leu Ile Glu Gly Trp Tyr Gly Tyr Gly Arg Lys Lys Arg Arg Gln Arg
            20                  25                  30          
Arg
    


<210> 54
<211> 33
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 54
Gly Leu Phe Glu Ala Ile Glu Gly Phe Ile Glu Asn Gly Trp Glu Gly
 1               5                  10                  15      
Met Ile Asp Gly Trp Tyr Gly Tyr Gly Arg Lys Lys Arg Arg Gln Arg
            20                  25                  30          
Arg
    


<210> 55
<211> 33
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 55
Gly Leu Phe Lys Ala Ile Ala Lys Phe Ile Lys Gly Gly Trp Lys Gly
 1               5                  10                  15      
Leu Ile Lys Gly Trp Tyr Gly Tyr Gly Arg Lys Lys Arg Arg Gln Arg
            20                  25                  30          
Arg
    


<210> 56
<211> 33
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 56
Gly Phe Phe Ala Leu Ile Pro Lys Ile Ile Ser Ser Pro Leu Phe Lys
 1               5                  10                  15      
Thr Leu Leu Ser Ala Val Gly Ser Ala Leu Ser Ser Ser Gly Glu Gln
            20                  25                  30          
Glu
    


<210> 57
<211> 44
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 57
Leu His Leu Leu His His Leu Leu His His Leu His His Leu Leu His
 1               5                  10                  15      
His Leu Leu His Leu Leu His His Leu Leu His His Leu Gly Gly Gly
            20                  25                  30          
Arg Lys Lys Arg Arg Gln Arg Arg Arg Pro Pro Gln
        35                  40                  


<210> 58
<211> 44
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 58
Arg Lys Lys Arg Arg Gln Arg Arg Arg Pro Pro Gln Gly Gly Gly Leu
 1               5                  10                  15      
His Leu Leu His His Leu Leu His His Leu His His Leu Leu His His
            20                  25                  30          
Leu Leu His Leu Leu His His Leu Leu His His Leu
        35                  40                  


<210> 59
<211> 22
<212> PRT
<213> Artificial Sequence

<220> 
<223> Completely Synthetic Amino Acid Sequence

<400> 59
Leu Ile Arg Leu Trp Ser His Ile His Ile Trp Phe Gln Trp Arg Arg
 1               5                  10                  15      
Leu Lys Trp Lys Lys Lys
            20          

