US 6,458,924 B2
`
`115
`GlysAsp36 Arg26
`3 4 Lys37 -(GAB-GHex) GLP-1(7-37);
`'
`34Lys3s -(GAB-GHex) GLP-1(7-38);
`Glys Asp37 Arg26•
`3 4 Lys39 -(GAB-GHex) GLP-1(7-39);
`Glys Asp3s Arg26
`'
`34Lics36-(GAB-GHex) GLP-1(7-36);
`Gly8 Asp35Ar&26
`•
`34Lys 6 -fGAB-GHex) GLP-1(7-36)amide;
`Glys Asp35 Arg26
`•
`3 4 Lys37 -(GAB-GHex) GLP-1(7-37);
`Glys Asp36 Arg2 6
`'
`34Lys38 -(GAB-GHex) GLP-1(7-38);
`Gly8 As£_37 Ar&2 6
`:
`Gly8Asp,sArg26
`4 Lys,9 -{GAB-GHex) GLP-1(7-39);
`' ,
`Gly8 Asp35 Ar~6
`34Lics36 -(GAB-GHex) GLP-1(7-36);
`•
`, 3 4Lys 6 1GAB-GHex) GLP-1(7-36)amide;
`Gly8 Asp35 Arg
`Gly8 Asp36Arg26
`34Lys 7-(GAB-GHex) GLP-1(7-37);
`•
`34Lys3 8
`GI ys Asp37 Arg26
`-( GAB-GHex) G LP-1(7-38);
`•
`Gly8 Asp38Arg26
`34Lys39-(GAB-GHex) GLP-1(7-39);
`•
`34L);s36-(GAB-GHex) GLP-1(7-36);
`Va18 Glu35 Ar~26
`•
`34Lys 6-(GAB-GHex) GLP-1(7-36)amide;
`Val8 Glu35 Arg"6
`•
`34Lys37-(GAB-GHex) GLP-1(7-37);
`Va18 Glu36 Arg26
`•
`Vai8 Glu3 7 Art 6
`34Lvs38 -(GAB-GHex) GLP-1(7-38);
`•
`34Lys19-(GAB-GHex) GLP-1(7-39);
`Va18 Glu38Arg 6
`•
`34Lvs~0 -(GAB-GHex) GLP-1(7-36);
`Vais Asp35 Art0 •
`3 4Lys1 6-{GAB-GHex) GLP-1(7-36)amide;
`Val8 Asp35 Arg'6•
`34Lys~7 -(GAB-GHex) GLP-1(7-37);
`Vais Asp3 6 Arg26 •
`Vais Asp37 Arg26 •
`34Lys38-(GAB-GHex) GLP-1(7-38);
`34Lys39-(GAB-GHex) GLP-1(7-39);
`Va18 Asp38Arg26
`•
`34Lys36-(GAB-GHex) GLP-1(7-36);
`Vais Asp35 Arg26 •
`34Lys36 -(GAB-GHex) GLP-1(7-36)amide;
`Vais Asp35 Arg26
`•
`34Lys37 -(GAB-GHex) GLP-1(7-37);
`Va18 Asp3 6 Arg26
`•
`Vais Asp37 Arg26 •
`34Lys38-(GAB-GHex) GLP-1(7-38);
`3 4Lys3 9 -(GAB-GHex) GLP-1(7-39);
`Val8 Asp38 Arg26
`'
`3 4 Lys36-(GAB-GHex) GLP-1(7-36);
`Ser8 Glu35 Arg26•
`34Lys36-(GAB-GHex) GLP-1(7-36)amide;
`Ser8 Glu35 Arg26
`'
`3 4 Lys37-(GAB-GHex) GLP-1(7-37);
`Ser8 Glu3 6 Arg26
`'
`34Lys3 s-(GAB-GHex) GLP-1(7-38);
`Ser8 Glu3 7 Arg26
`•
`34Lys39 -(GAB-GHex) GLP-1(7-39);
`Ser8 Glu3 8 Arg26
`'
`3 4 Lys36-(GAB-GHex) GLP-1(7-36);
`Ser8 Glu35 Arf 6
`'
`34Lys36-(GAB-GHex) GLP-1(7-36)amide;
`Ser8Glu35 Arg-6
`•
`SersGlu3 6Arg2 6
`34Lys37 -(GAB-GHex) GLP-1(7-37);
`'
`Ser8 Glu37 Arf6
`34Lys3 s-(GAB-GHex) GLP-1(7-38);
`•
`34Lys39 -f GAB-GHex) GLP-1(7-39);
`Ser8Glu38 Arg-6
`•
`34Lys36-(GAB-GHex) GLP-1(7-36);
`Sers Asp35 Arg26
`•
`Ser8 Asp35 Arg26
`34Lys36
`-( GAB-GHex) GLP-1(7-36)amide;
`•
`34Lys37 -(GAB-GHex) GLP-1(7-37);
`Sers Asp36 Arg2 6
`•
`Sers Asp37 Arg26
`34Lys38-(GAB-GHex) GLP-1(7-38);
`•
`SersAsp3sArg26 • 34Lys39-(GAB-GHex) GLP-1(7-39);
`34Lys36-(GAB-GHex) GLP-1(7-36);
`Sers Asp3 5 Arg26 •
`34Lys36 -(GAB-GHex) GLP-1(7-36)amide;
`Ser8 Asp35 Arg26
`•
`34Lys3 7 -(GAB-GHex) GLP-1(7-37);
`Sers Asp36 Arg26
`•
`Ser8 Asp37 Arg20
`34Lys38-(GAB-GHex) GLP-1(7-38);
`•
`34Lys39-(GAB-GHex) GLP-1(7-39);
`Ser8 Asp38 Arg26•
`34Lys36-(GAB-G Hex) GLP-1(7-36);
`Thr8 Glu35 Arg26
`·
`34Lys36-(GAB-GHex) GLP-1(7-36)amide;
`Tor8Glu35 Arg26•
`3 4 Lys37 -(GAB-GHex) GLP-1(7-37);
`Thr8 Glu36 Arg26
`'
`Thr8 Glu37 Arg26
`34Lys38-(GAB-G Hex) GLP-1(7-38);
`·
`34Lys39-(GAB-GHex) GLP- 1(7-39);
`Thr8 Glu38 Arg20 •
`34Lys36-(GAB-GHex) GLP-1(7-36);
`Thr8 Glu35 Arg26
`'
`34Lys36-(GAB-GHex) GLP-1(7-36)amide;
`Tor8Glu35 Arg26 •
`34Lys37 -(GAB-GHex) GLP- 1(7-37);
`ThrsGlu36 Arg26
`'
`34Lls38-(GAB-G Hex) GLP-1(7-38);
`Tbr8 Glu37 Ar~26
`'
`34Lys 9 -(GAB-GHex) GLP-1(7-39);
`Tor8Glu38Arg-6
`•
`Thr8 Asp35Arg26
`34Lys36-(GAB-GHex) GLP-1(7-36);
`'
`Tor8 Asp35 Arg26
`34Lys36-( GAB-GHex) GLP-1(7-36)amide;
`•
`3 4 Lys37 -(GAB-GHex) GLP-1(7-37);
`Tbr8 Asp36 Arg26
`•
`Tbr8 Asp37 Arg26
`3 4 Lys3 8 -(GAB-GHex) GLP-1(7-38);
`Tbr8 Asp38Arg26
`3 4 Lys39 -(GAB-GHex) GLP-1(7-39);
`•
`Thr8 Asp3 5 Arg26
`3 4 Lys36-(GAB-GHex) GLP-1(7-36);
`•
`34Lys36 -(GAB-GHex) GLP-1(7-36)amide;
`Tbr8 Asp35 Arg26
`•
`Tbr8 Asp36 Arg26
`3 4 Lys3 7 -(GAB-G Hex) GLP-1(7-37);
`•
`Thr8 Asp37 Arg26
`3 4 Lys38-(GAB-GHex) GLP-1(7-38);
`•
`34Lys39 -(GAB-GHex) GLP-1(7-39);
`Tor8 Asp38 Arg26
`•
`
`'
`
`'
`
`-
`
`-
`
`-
`
`-
`
`-
`
`116
`34Lys1s-(GAB-GHex) GLP-1(7-3~; Arg2 6
`3 ''Lys18
`Arg26
`'
`'
`3 4Lys1s-(GAB(cid:173)
`(GAB-GHex) GLP-1(7-36)amide; Arg2 ,
`3 4Lvs1s-(GAB-GHex) GLP-1
`GHex) GLP-1(7-37); Arg26
`'
`(7-38); Gly8Asp19Arg26
`34LJs18 -(GAB-GHex) GLP-1(7-
`•
`5 36); Gly8Asp 17An226
`34Lys1 -(GAB-GHex) GLP-1(7-36);
`'
`Gly8 Asp19 Arg26
`3'a'Lys18-(GAB-GHex) GLP-1(7-36)amide;
`•
`Glys Asp17 Arg26
`34Lys1s _( GAB-GHex) GLP-1(7-36)amide;
`•
`Glys Asp1 9 Arg26
`3 4 Lys~s-(GAB-GHex) GLP-1(7-37);
`'
`34Lvs 1s-(GAB-GHex) GLP-1(7-38);
`Gly8 Asp1 9 Arg26
`•
`34Lysis-( GAB-GHex) GLP-1(7-38);
`Glys A5P17 Arg'i6
`,
`
`10 Arg26• :l4 Lys23-(GAB-GHex) GLP-1(7-3~; Arg2 6
`34Lys23
`•
`34Lys2 3 -(GAB(cid:173)
`(GAB-GHex) GLP-1(7-36}amide; Arg2
`,
`34Lys23-(GAB-GHex) GLP-1
`GHex) GLP-1(7-37); Arg26
`•
`(7-38);
`34Lys23-(GAB-GHex) GLP-1(7-36);
`Gly8 Asp1 9 Arg26
`•
`34LJs23-(GAB-GHex) GLP-1(7-36);
`15 Gly8Asp1 7Ar&26
`,
`34Lys 3 -(GAB-GHex) GLP-1(7-36)amide;
`G!y8 A5p19 Arg"6
`•
`Glys Asp17 Arg26, 34Lys2 3-~GAB-GHex) GLP-1(7-36)amide;
`34Lys 3-(GAB-GHex) GLP-1(7-37);
`Gly8 Asp19 Arg20
`•
`34Lys2 3-(GAB-GHex) GLP-1(7-38);
`Gly8Asp1 9 Ari26
`•
`20 Glys Asp17 Arg"6 •
`34Lys~3 -(GAB-GHex) GLP-1(7-38);
`34Lys27-(GAB-GHex) GLP-1(7-36); Arg26•
`3 4Lys27
`Arg26•
`3 4Lys27 -(GAB(cid:173)
`(GAB-GHex) GLP-1(7-36)amide; Arg26
`•
`34Lys2 7 -(GAB-GHex) GLP-1
`GHex) GLP-1(7-37); Arg26•
`(7-38); Gly8Asp19Arg26
`34Lys2 7-(GAB-GHex) GLP-1(7-
`'
`25 36); Gly8 Asp 17 Arg26
`34Lys27 -(GAB-GHex) GLP-1(7-36);
`•
`34Lys27 -(GAB-GHex) GLP-1(7-36)amide;
`Glys A5p19 Arg26•
`Gly8 Asp17 Arg26
`34Lys27 -(GAB-GHex) GLP-1(7-36)amide;
`•
`3 4 Lys2 7 -(GAB-GHex) GLP-1(7-37);
`Glys Asp1 9 Arg26•
`3 4 Lys2 7 -(GAB-GHex) GLP-1(7-38);
`Gly8 Asp19 Arg26
`'
`30 Gly8 Asp17 Arg26
`3 4Lys27 -(GAB-GHex) GLP-1(7-38);
`'
`Arg26
`34Lys1s-(GAB-GHex) GLP-1(7-36); Arg2 6
`34Lys18
`•
`•
`34Lys18-(GAB(cid:173)
`(GAB-GHex) GLP-1(7-36)amide; Arg26
`'
`34Lys18-(GAB-GHex) GLP-1
`GHex) GLP-1(7-37); Arg26
`'
`(7-38);
`3 4 Lys1s-(GAB-GHex) GLP-1(7-36) ;
`35 Vais Asp 19 Arg26
`'
`34Lys1s -(GAB-GHex) GLP-1(7-36);
`Val18 Asp1 7 Arg2 6
`•
`34Lys18-(GAB-GHex) GLP-1(7-36)amide;
`Vai8 Asp19 Arg26
`•
`34Lys18-(GAB-GHex) GLP-1(7-36)amide;
`Va!8 Asp17 Arg26
`•
`34Lys1s-(GAB-GHex) GLP-1(7-37);
`ValsAsp 19Arg26
`•
`40 Va18 Asp 19 Arg26,
`34Lys1s-(GAB-GHex) GLP-1(7-38);
`Vai8Asp17 Arg26
`34Lys18-(GAB-GHex) GLP-1(7-38);
`'
`34Lys23-
`Arg26
`34Lys23-(GAB-GHex) GLP-1(7-36); Arg2 6
`•
`•
`3 4Lys23-(GAB(cid:173)
`(GAB-GHex) GLP-1(7-36)amide; Arg20
`•
`34Lys23-(GAB-GHex) GLP-1
`GHex) GLP-1(7-37); Arg26
`•
`45 (7-38);
`34Lys23-(GAB-GHex) GLP-1(7-36);
`Va18 Asp 19 Arg20
`•
`34Lys23-(GAB-GHex) GLP-1(7-36);
`Val8 Asp 17 Arg26•
`34Lys23-(GAB-GHex) GLP-1(7-36)amide;
`Vais Asp19 Arg26
`•
`Val8 A-;p17 Arg20•
`34Lys23-(GAB-GHex) GLP-1(7-36)amide;
`so Vais Asp 19 Arg26
`3 4 Lys23-(GAB-GHex) GLP-1(7-37);
`'
`3 4 Lys23-(GAB-GHex) GLP-1(7-38);
`Vais Asp 19 Arg26•
`Val8Asp17 Arg20•
`34Lys23-(GAB-GHex) GLP-1(7-38);
`34Lys27
`34Lys27-(GAB-GHex) GLP-1(7-36); Arg2 6
`Arg26
`'
`'
`-
`3 4Lys27 -(GAB-
`(GAB-GHex) GLP-1(7-36)amide; Arg26
`•
`ss GHex) GLP-1(7-37); Arg26
`3 4Lys27-(GAB-GHex) GLP-1
`'
`(7-38);
`34Lys27 -(GAB-GHex) GLP-1(7-36);
`Vais A-;p 19 Arg26
`3 4 Lys27 -(GAB-GHex) GLP-1(7-36);
`Vais Asp 17 Arg26
`'
`Val8Asp19 Arg26
`34Lys27-(GAB-GHex) GLP-1(7-36)amide;
`•
`34Lys27 -(GAB-GHex) GLP-1(7-36)amide;
`60 Val8 Asp17 Arg26
`•
`3 4 Lys27-(GAB-GHex) GLP-1(7-37) ;
`Vais Asp 19 Arg26
`'
`34L,r2 '-(GAB-GHex) GLP-1(7-38);
`Vais A-;p 19 Aro 26
`•
`Val8Asp17Arl 6
`34Lys-7-(GAB-GHex) GLP-30 1(7-38);
`•
`34Lys18-(GAB-GHex) GLP-1(7-3~; Arg26
`3 4Lys18
`Arg26
`•
`•
`34Lys18-(GAB(cid:173)
`65 (GAB-GHex) GLP-1(7-36)amide; Arg2
`,
`34Lys1s-(GAB-GHex) GLP-1
`GHex) GLP-1(7-37); Arg26
`•
`(7-38);
`
`FRESENIUS EXHIBIT 1020
`Page 61 of 129
`
`
`
`115
`GlysAsp36 Arg26
`3 4 Lys37 -(GAB-GHex) GLP-1(7-37);
`'
`34Lys3s -(GAB-GHex) GLP-1(7-38);
`Glys Asp37 Arg26•
`3 4 Lys39 -(GAB-GHex) GLP-1(7-39);
`Glys Asp3s Arg26
`'
`34Lics36-(GAB-GHex) GLP-1(7-36);
`Gly8 Asp35Ar&26
`•
`34Lys 6 -fGAB-GHex) GLP-1(7-36)amide;
`Glys Asp35 Arg26
`•
`3 4 Lys37 -(GAB-GHex) GLP-1(7-37);
`Glys Asp36 Arg2 6
`'
`34Lys38 -(GAB-GHex) GLP-1(7-38);
`Gly8 As£_37 Ar&2 6
`:
`Gly8Asp,sArg26
`4 Lys,9 -{GAB-GHex) GLP-1(7-39);
`' ,
`Gly8 Asp35 Ar~6
`34Lics36 -(GAB-GHex) GLP-1(7-36);
`•
`, 3 4Lys 6 1GAB-GHex) GLP-1(7-36)amide;
`Gly8 Asp35 Arg
`Gly8 Asp36Arg26
`34Lys 7-(GAB-GHex) GLP-1(7-37);
`•
`34Lys3 8
`GI ys Asp37 Arg26
`-( GAB-GHex) G LP-1(7-38);
`•
`Gly8 Asp38Arg26
`34Lys39-(GAB-GHex) GLP-1(7-39);
`•
`34L);s36-(GAB-GHex) GLP-1(7-36);
`Va18 Glu35 Ar~26
`•
`34Lys 6-(GAB-GHex) GLP-1(7-36)amide;
`Val8 Glu35 Arg"6
`•
`34Lys37-(GAB-GHex) GLP-1(7-37);
`Va18 Glu36 Arg26
`•
`Vai8 Glu3 7 Art 6
`34Lvs38 -(GAB-GHex) GLP-1(7-38);
`•
`34Lys19-(GAB-GHex) GLP-1(7-39);
`Va18 Glu38Arg 6
`•
`34Lvs~0 -(GAB-GHex) GLP-1(7-36);
`Vais Asp35 Art0 •
`3 4Lys1 6-{GAB-GHex) GLP-1(7-36)amide;
`Val8 Asp35 Arg'6•
`34Lys~7 -(GAB-GHex) GLP-1(7-37);
`Vais Asp3 6 Arg26 •
`Vais Asp37 Arg26 •
`34Lys38-(GAB-GHex) GLP-1(7-38);
`34Lys39-(GAB-GHex) GLP-1(7-39);
`Va18 Asp38Arg26
`•
`34Lys36-(GAB-GHex) GLP-1(7-36);
`Vais Asp35 Arg26 •
`34Lys36 -(GAB-GHex) GLP-1(7-36)amide;
`Vais Asp35 Arg26
`•
`34Lys37 -(GAB-GHex) GLP-1(7-37);
`Va18 Asp3 6 Arg26
`•
`Vais Asp37 Arg26 •
`34Lys38-(GAB-GHex) GLP-1(7-38);
`3 4Lys3 9 -(GAB-GHex) GLP-1(7-39);
`Val8 Asp38 Arg26
`'
`3 4 Lys36-(GAB-GHex) GLP-1(7-36);
`Ser8 Glu35 Arg26•
`34Lys36-(GAB-GHex) GLP-1(7-36)amide;
`Ser8 Glu35 Arg26
`'
`3 4 Lys37-(GAB-GHex) GLP-1(7-37);
`Ser8 Glu3 6 Arg26
`'
`34Lys3 s-(GAB-GHex) GLP-1(7-38);
`Ser8 Glu3 7 Arg26
`•
`34Lys39 -(GAB-GHex) GLP-1(7-39);
`Ser8 Glu3 8 Arg26
`'
`3 4 Lys36-(GAB-GHex) GLP-1(7-36);
`Ser8 Glu35 Arf 6
`'
`34Lys36-(GAB-GHex) GLP-1(7-36)amide;
`Ser8Glu35 Arg-6
`•
`SersGlu3 6Arg2 6
`34Lys37 -(GAB-GHex) GLP-1(7-37);
`'
`Ser8 Glu37 Arf6
`34Lys3 s-(GAB-GHex) GLP-1(7-38);
`•
`34Lys39 -f GAB-GHex) GLP-1(7-39);
`Ser8Glu38 Arg-6
`•
`34Lys36-(GAB-GHex) GLP-1(7-36);
`Sers Asp35 Arg26
`•
`Ser8 Asp35 Arg26
`34Lys36
`-( GAB-GHex) GLP-1(7-36)amide;
`•
`34Lys37 -(GAB-GHex) GLP-1(7-37);
`Sers Asp36 Arg2 6
`•
`Sers Asp37 Arg26
`34Lys38-(GAB-GHex) GLP-1(7-38);
`•
`SersAsp3sArg26 • 34Lys39-(GAB-GHex) GLP-1(7-39);
`34Lys36-(GAB-GHex) GLP-1(7-36);
`Sers Asp3 5 Arg26 •
`34Lys36 -(GAB-GHex) GLP-1(7-36)amide;
`Ser8 Asp35 Arg26
`•
`34Lys3 7 -(GAB-GHex) GLP-1(7-37);
`Sers Asp36 Arg26
`•
`Ser8 Asp37 Arg20
`34Lys38-(GAB-GHex) GLP-1(7-38);
`•
`34Lys39-(GAB-GHex) GLP-1(7-39);
`Ser8 Asp38 Arg26•
`34Lys36-(GAB-G Hex) GLP-1(7-36);
`Thr8 Glu35 Arg26
`·
`34Lys36-(GAB-GHex) GLP-1(7-36)amide;
`Tor8Glu35 Arg26•
`3 4 Lys37 -(GAB-GHex) GLP-1(7-37);
`Thr8 Glu36 Arg26
`'
`Thr8 Glu37 Arg26
`34Lys38-(GAB-G Hex) GLP-1(7-38);
`·
`34Lys39-(GAB-GHex) GLP- 1(7-39);
`Thr8 Glu38 Arg20 •
`34Lys36-(GAB-GHex) GLP-1(7-36);
`Thr8 Glu35 Arg26
`'
`34Lys36-(GAB-GHex) GLP-1(7-36)amide;
`Tor8Glu35 Arg26 •
`34Lys37 -(GAB-GHex) GLP- 1(7-37);
`ThrsGlu36 Arg26
`'
`34Lls38-(GAB-G Hex) GLP-1(7-38);
`Tbr8 Glu37 Ar~26
`'
`34Lys 9 -(GAB-GHex) GLP-1(7-39);
`Tor8Glu38Arg-6
`•
`Thr8 Asp35Arg26
`34Lys36-(GAB-GHex) GLP-1(7-36);
`'
`Tor8 Asp35 Arg26
`34Lys36-( GAB-GHex) GLP-1(7-36)amide;
`•
`3 4 Lys37 -(GAB-GHex) GLP-1(7-37);
`Tbr8 Asp36 Arg26
`•
`Tbr8 Asp37 Arg26
`3 4 Lys3 8 -(GAB-GHex) GLP-1(7-38);
`Tbr8 Asp38Arg26
`3 4 Lys39 -(GAB-GHex) GLP-1(7-39);
`•
`Thr8 Asp3 5 Arg26
`3 4 Lys36-(GAB-GHex) GLP-1(7-36);
`•
`34Lys36 -(GAB-GHex) GLP-1(7-36)amide;
`Tbr8 Asp35 Arg26
`•
`Tbr8 Asp36 Arg26
`3 4 Lys3 7 -(GAB-G Hex) GLP-1(7-37);
`•
`Thr8 Asp37 Arg26
`3 4 Lys38-(GAB-GHex) GLP-1(7-38);
`•
`34Lys39 -(GAB-GHex) GLP-1(7-39);
`Tor8 Asp38 Arg26
`•
`
`'
`
`'
`
`-
`
`-
`
`-
`
`-
`
`-
`
`116
`34Lys1s-(GAB-GHex) GLP-1(7-3~; Arg2 6
`3 ''Lys18
`Arg26
`'
`'
`3 4Lys1s-(GAB(cid:173)
`(GAB-GHex) GLP-1(7-36)amide; Arg2 ,
`3 4Lvs1s-(GAB-GHex) GLP-1
`GHex) GLP-1(7-37); Arg26
`'
`(7-38); Gly8Asp19Arg26
`34LJs18 -(GAB-GHex) GLP-1(7-
`•
`5 36); Gly8Asp 17An226
`34Lys1 -(GAB-GHex) GLP-1(7-36);
`'
`Gly8 Asp19 Arg26
`3'a'Lys18-(GAB-GHex) GLP-1(7-36)amide;
`•
`Glys Asp17 Arg26
`34Lys1s _( GAB-GHex) GLP-1(7-36)amide;
`•
`Glys Asp1 9 Arg26
`3 4 Lys~s-(GAB-GHex) GLP-1(7-37);
`'
`34Lvs 1s-(GAB-GHex) GLP-1(7-38);
`Gly8 Asp1 9 Arg26
`•
`34Lysis-( GAB-GHex) GLP-1(7-38);
`Glys A5P17 Arg'i6
`,
`
`10 Arg26• :l4 Lys23-(GAB-GHex) GLP-1(7-3~; Arg2 6
`34Lys23
`•
`34Lys2 3 -(GAB(cid:173)
`(GAB-GHex) GLP-1(7-36}amide; Arg2
`,
`34Lys23-(GAB-GHex) GLP-1
`GHex) GLP-1(7-37); Arg26
`•
`(7-38);
`34Lys23-(GAB-GHex) GLP-1(7-36);
`Gly8 Asp1 9 Arg26
`•
`34LJs23-(GAB-GHex) GLP-1(7-36);
`15 Gly8Asp1 7Ar&26
`,
`34Lys 3 -(GAB-GHex) GLP-1(7-36)amide;
`G!y8 A5p19 Arg"6
`•
`Glys Asp17 Arg26, 34Lys2 3-~GAB-GHex) GLP-1(7-36)amide;
`34Lys 3-(GAB-GHex) GLP-1(7-37);
`Gly8 Asp19 Arg20
`•
`34Lys2 3-(GAB-GHex) GLP-1(7-38);
`Gly8Asp1 9 Ari26
`•
`20 Glys Asp17 Arg"6 •
`34Lys~3 -(GAB-GHex) GLP-1(7-38);
`34Lys27-(GAB-GHex) GLP-1(7-36); Arg26•
`3 4Lys27
`Arg26•
`3 4Lys27 -(GAB(cid:173)
`(GAB-GHex) GLP-1(7-36)amide; Arg26
`•
`34Lys2 7 -(GAB-GHex) GLP-1
`GHex) GLP-1(7-37); Arg26•
`(7-38); Gly8Asp19Arg26
`34Lys2 7-(GAB-GHex) GLP-1(7-
`'
`25 36); Gly8 Asp 17 Arg26
`34Lys27 -(GAB-GHex) GLP-1(7-36);
`•
`34Lys27 -(GAB-GHex) GLP-1(7-36)amide;
`Glys A5p19 Arg26•
`Gly8 Asp17 Arg26
`34Lys27 -(GAB-GHex) GLP-1(7-36)amide;
`•
`3 4 Lys2 7 -(GAB-GHex) GLP-1(7-37);
`Glys Asp1 9 Arg26•
`3 4 Lys2 7 -(GAB-GHex) GLP-1(7-38);
`Gly8 Asp19 Arg26
`'
`30 Gly8 Asp17 Arg26
`3 4Lys27 -(GAB-GHex) GLP-1(7-38);
`'
`Arg26
`34Lys1s-(GAB-GHex) GLP-1(7-36); Arg2 6
`34Lys18
`•
`•
`34Lys18-(GAB(cid:173)
`(GAB-GHex) GLP-1(7-36)amide; Arg26
`'
`34Lys18-(GAB-GHex) GLP-1
`GHex) GLP-1(7-37); Arg26
`'
`(7-38);
`3 4 Lys1s-(GAB-GHex) GLP-1(7-36) ;
`35 Vais Asp 19 Arg26
`'
`34Lys1s -(GAB-GHex) GLP-1(7-36);
`Val18 Asp1 7 Arg2 6
`•
`34Lys18-(GAB-GHex) GLP-1(7-36)amide;
`Vai8 Asp19 Arg26
`•
`34Lys18-(GAB-GHex) GLP-1(7-36)amide;
`Va!8 Asp17 Arg26
`•
`34Lys1s-(GAB-GHex) GLP-1(7-37);
`ValsAsp 19Arg26
`•
`40 Va18 Asp 19 Arg26,
`34Lys1s-(GAB-GHex) GLP-1(7-38);
`Vai8Asp17 Arg26
`34Lys18-(GAB-GHex) GLP-1(7-38);
`'
`34Lys23-
`Arg26
`34Lys23-(GAB-GHex) GLP-1(7-36); Arg2 6
`•
`•
`3 4Lys23-(GAB(cid:173)
`(GAB-GHex) GLP-1(7-36)amide; Arg20
`•
`34Lys23-(GAB-GHex) GLP-1
`GHex) GLP-1(7-37); Arg26
`•
`45 (7-38);
`34Lys23-(GAB-GHex) GLP-1(7-36);
`Va18 Asp 19 Arg20
`•
`34Lys23-(GAB-GHex) GLP-1(7-36);
`Val8 Asp 17 Arg26•
`34Lys23-(GAB-GHex) GLP-1(7-36)amide;
`Vais Asp19 Arg26
`•
`Val8 A-;p17 Arg20•
`34Lys23-(GAB-GHex) GLP-1(7-36)amide;
`so Vais Asp 19 Arg26
`3 4 Lys23-(GAB-GHex) GLP-1(7-37);
`'
`3 4 Lys23-(GAB-GHex) GLP-1(7-38);
`Vais Asp 19 Arg26•
`Val8Asp17 Arg20•
`34Lys23-(GAB-GHex) GLP-1(7-38);
`34Lys27
`34Lys27-(GAB-GHex) GLP-1(7-36); Arg2 6
`Arg26
`'
`'
`-
`3 4Lys27 -(GAB-
`(GAB-GHex) GLP-1(7-36)amide; Arg26
`•
`ss GHex) GLP-1(7-37); Arg26
`3 4Lys27-(GAB-GHex) GLP-1
`'
`(7-38);
`34Lys27 -(GAB-GHex) GLP-1(7-36);
`Vais A-;p 19 Arg26
`3 4 Lys27 -(GAB-GHex) GLP-1(7-36);
`Vais Asp 17 Arg26
`'
`Val8Asp19 Arg26
`34Lys27-(GAB-GHex) GLP-1(7-36)amide;
`•
`34Lys27 -(GAB-GHex) GLP-1(7-36)amide;
`60 Val8 Asp17 Arg26
`•
`3 4 Lys27-(GAB-GHex) GLP-1(7-37) ;
`Vais Asp 19 Arg26
`'
`34L,r2 '-(GAB-GHex) GLP-1(7-38);
`Vais A-;p 19 Aro 26
`•
`Val8Asp17Arl 6
`34Lys-7-(GAB-GHex) GLP-30 1(7-38);
`•
`34Lys18-(GAB-GHex) GLP-1(7-3~; Arg26
`3 4Lys18
`Arg26
`•
`•
`34Lys18-(GAB(cid:173)
`65 (GAB-GHex) GLP-1(7-36)amide; Arg2
`,
`34Lys1s-(GAB-GHex) GLP-1
`GHex) GLP-1(7-37); Arg26
`•
`(7-38);
`
`FRESENIUS EXHIBIT 1020
`Page 61 of 129
`
`
`
`US 6,458,924 B2
`
`•
`
`118
`117
`1(7-37); Arg26' 34Lys36-(GAB-GOct) GLP-1(7-37);
`Ser8Asp19Arg26' 34Lys18-(GAB-GHex) GLP-1(7-36);
`Arg26Lys34-(GAB-G0ct) GLP-1(7-38); Arg34Lys26-(GAB-
`Ser8Asp17Arg26· 34Lys18-(GAB-G Hex) GLP-1(7-36);
`
`GOct) GLP-1(7-38); Arg26' 34Lys38 -( GAB-GOct) GLP-1(7-
`Ser8 Asp19 Arg26' 34Lys18 -(GAB-GHex) GLP-1(7-36)amide;
`38); Arg26Lys34-(GAB-GOct) GLP-1(7-39); Arg34Lys26-
`Ser8 Asp17 Arg26' 3''Lys18-(GAB-GHex) GLP-1(7-36)amide;
`Sers Asp19 Arg26· 34Lys18-(GAB-G Hex) GLP-1(7-37); s (GAB-GOct) GLP-1(7-39); Arg26· 34Lys39-(GAB-G0ct)
`Ser8 Asp19 Arg26' 34Lys18-(GAB-GHex) GLP-1(7-38);
`GLP-1(7-39);
`Ser8Asp19Arg26' 34Lys18-(GAB-GHex) GLP-1(7-38);
`G l y 8 Arg 26 Lys 3 • -(GAB -G O ct) G LP-1(7-36);
`Arg26· 34Lys23-(GAB-GHex) GLP-1(7-36); Arg26· 34Lys23-
`Giy8Arg34Lys26-(GAB-GOct) GLP-1(7-36); Gly8Arg26·
`34Lys36-(GAB-GOct) GLP-1(7-36); Gly 8 Arg26Lys34-
`(GAB-GHex) GLP-1(7-36)amide; Arg26· 34Lys23-(GAB-
`GHex) GLP-1(7-37); Arg26• 34Lys23-(GAB-GHex) GLP-1 10 (GAB-GOct) GLP-1(7-36)amide; Gly8Arg34Lys26-(GAB-
`GOct) GLP-1(7-36)amide; Gly8Arg26· 34Lys36-(GAB-
`(7-38);
`Ser8Asp19Arg26' 34Lys23-(GAB-G Hex) GLP-1(7-36);
`GOct) GLP-1(7-36)amide; Gly8Arg26Lys34-(GAB-GOct)
`GLP-1(7-37); Gly8 Art4Lys26-(GAB-G0 ct) GLP-1(7-37);
`34Lys23 -(GAB-G Hex) GLP-1(7-36);
`Sers Asp17 Art6
`Gly 8 Arg26· 34Lys 6-(GAB- GOct) G LP-1(7 -37);
`Ser8Asp19Arg-6· 34Lys23-(GAB-GHex) GLP-1(7-36)amide;
`• 34Lys23-(GAB-GHex) GLP-1(7-36)amide; 15 G l y 8 Arg26 L ys 3 4 -( GAB -G Oct) G LP- 1(7-38) ;
`Ser8 A51>17 Arg26
`Sers Asp19 Arg26· 34Lys23-(GAB-GHex) GLP-1(7-37);
`Gly8 Arg34Lys26-(GAB-GOct) GLP-1(7-38); Gly8Arg26·
`34Lys38-(GAB-GOct) GLP-1(7-38); Gly8 Arg26Lys34-
`Sers Asp19 Arg26• 34Lys23 -(GAB-GHex) GLP-1(7-38);
`34Lys23-(GAB-GHex) GLP-1(7-38);
`(GAB-GOct) GLP-1(7-39); Gly8 Arg34Lys26-(GAB-G0ct)
`Ser8 A51>17 Arg26
`Arg26· 34Lys27(GAB-GHex) GLP-1(7-36); Arg26· 34Lys27-
`GLP-1(7-39); Gly8Arg26· 34Lys39-(GAB-GOct) GLP-1(7-
`(GAB-GHex) GLP-1(7-36)amide; Arg26• 34Lys27-(GAB- 20 39);
`GHex) GLP-1(7-37); Arg26• 34Lys27-(GAB-GHex) GLP-1
`Va 18 Arg26 Lys 34 -( G AB-G O c t) G L P-1 (7-36);
`Val8Arg34Lys26-(GAB-GOct) GLP-1(7-36); Val8 Arg26
`(7-38);
`Sers Asp19 Arg26• 34Lys27-(GAB-GHex) GLP-1(7-36);
`34Lys36-(GAB-G0 ct) GLP-1(7-36); ValsArg26Lys34-(GAB-
`GOct) GLP-1(7-36)amide; Val8Arg34 Lys26-(GAB-GOct)
`Ser8 Asp17 Arg26' 34Lys27-(GAB-GHex) GLP-1(7-36);
`Sers Asp19 Arg26· 34Lys27 -(GAB-GHex) GLP-1(7-36)amide; 25 GLP-1(7-36)amide; Vais Arg26• 34Lys36-(GAB-GOct) GLP-
`Ser8 Asp17 Arg26• 34Lys27 -(GAB-GHex) GLP-1(7-36)amide;
`1(7-36)amide; Vais Arg26Lys34-(GAB-G0ct) GLP-1(7-37);
`Ser8 Asp19 Arg26' 34Lys27-(GAB-GHex) GLP-1(7-37);
`Vais Arg34 Lys26-(GAB-GOct) GLP-1(7-37); Vais Arg26'
`Sers Asp19 Arg26· 34Lys27-(GAB-GHex) GLP-1(7-38);
`34Lys36-(GAB-G0ct) GLP-1(7-37); ValsArg26Lys34-(GAB-
`Ser8Asp17Arg26' 34Lys27-(GAB-GHex) GLP-1(7-38);
`GOct) GLP-1(7-38); Val8Arg34Lys26-(GAB-G0ct) GLP-1
`Arg26' 34Lys18-(GAB-GHex) GLP-1(7-36); Arg26' 34Lys18- 30 (7-38); Val8Arg26' 34Lys38-(GAB-G0ct) GLP-1(7-38);
`Va 18 Arg26 L ys 34 - ( G AB-G Oct) G L P-1 (7-39) ;
`(GAB-GHex) GLP-1(7-36)amide; Arg26· 34Lys18-(GAB-
`GHex) GLP-1(7-37); Arg26' 34Lys18-(GAB-GHex) GLP-1
`Val8Arg34Lys26-(GAB-G0ct) GLP-1(7-39); Val8Arg26'
`34Lys39-(GAB-G0ct) GLP-1(7-39); Ser8Arg26Lys34-(GAB-
`(7-38);
`Tbrs Asp19 Arg26· 34Lys1s -(GAB-GHex) GLP-1(7-36);
`GOct) GLP-1(7-36); Sers Arg34Lys26-(GAB-G0ct) GLP-1
`Tbr8 Asp17 Arg26' 34Lys18-(GAB-GHex) GLP-1(7-36); 35 (7-36); Ser8 Arg26' 34Lys36-(GAB-G0ct) GLP-1(7-36);
`34Lys1s·(GAB-GHex) GLP-1(7-36)amide;
`Sers Arg26Lys34-(GAB-G0ct) GLP-1(7-36)amide;
`Tbr8 Asp19 Arg26
`Ser8 Arg34Ll,s26 -(GAB-G0ct) GLP- 1(7- 36)amide;
`Tors Asp17 Arg26
`• 34Lys18-(GAB-GHex) GLP-1(7-36)amide;
`TbrsAsp19Arg26' 34Lys18-(GAB-GHex) GLP-1(7-37);
`Ser8Arg26' 4Lys36-(GAB-G0ct) GLP-1(7-36)amide;
`Se rs Arg 26 Lys 3 4 -(GAB-GO ct) G L P-1(7-37);
`Tbrs Asp19 Ar~6· 34Lys1s·(GAB-GHex) GLP-1(7-38);
`, 34Lys1s-(GAB-GHex) GLP-1(7-38);
`Tur8 Asp17 Arg
`40 Sers Arg34Lys26-(GAB-GOct) GLP-1(7-37); Sers Arg26·
`34Lys23-(GAB-GHex) GLP-1(7-36); Arg26' 34Lys23-
`34Lys36-(GAB-G0ct) GLP-1(7-37); Ser8Arg26Lys34(GAB-
`Arg26
`•
`(GAB-GHex) GLP-1(7-36)amide; Arg26· 34Lys23-(GAB-
`GOct) GLP-1(7-38); Ser8Arg34Lys26-(GAB-GOct) GLP-1
`• 34Lys23-(GAB-GHex) GLP-1
`(7-38); Sers Arg26• 34Lys38 -(GAB-GOct) GLP-1(7-38);
`GHex) GLP-1(7-37); Arg26
`Ser8Arg26 L ys 34 -(GAB-G0ct) GLP-1(7-39);
`(7-38);
`Thrs Asp19 Arg26· 34Lys23-(GAB-GHex) GLP-1(7-36); 45 Sers Arg34Lys26-(GAB-GOct) GLP-1(7-39); Sers Arg26·
`34Lys39-(GAB-GOct) GLP-1(7-39);
`Thr8 Asp17 Arg26• 34Lys23 -(GAB-GHex) GLP-1(7-36);
`Tur8 Asp19 Arg26• 34Lys23-(GAB-GHex) GLP-1(7-36)amide;
`Th r 8 Arg 26 Ly s 3 4 -( GAB -GO ct) G L P-1(7-36);
`Tors Asp17Arg26 • 34Lys23-(GAB-GHex) GLP-1(7-36)amide;
`Thrs Arg34Lys26-(GAB-GOct) GLP-1(7-36); T hrs Arg26•
`34Lys36-(GAB-G0 ct) GLP-1(7-36); Tbr8Arg26Lys34-(GAB-
`Tbr8 Asp19 Arg26• 34Lys23-(GAB-GHex) GLP-1(7-37);
`Tbr8 Asp19 Arg26' 34 Lys23-(GAB-GHex) GLP-1(7-38); 50 GOct) GLP-1(7-36)amide; Thr8 Arg34Lys26-(GAB-GOct)
`Tors Asp17 Arg26 • 34Lys23 -(GAB-GHex) GLP-1(7-38);
`GLP-1(7-36)amide; Thrs Arg26 • 34Lys36-(GAB-GOct) GLP-
`Arg26• 34 Lys27-(GAB-GHex) GLP-1(7-36); Arg26• 34Lys27-
`1(7-36)amide; Tbr8Arg26 Lys34-(GAB-GOct) GLP-1(7-37);
`Thr8 Arg34Lys26 -( GAB-GOct) GLP-1(7-37); T br8 Arg26'
`( GAB-GHex) GLP-1(7-36) amide; Arg26' 34Lys27 -(GAB-
`GHex) GLP-1(7-37); Arg26• 34Lys27 -( GAB-GHex) GLP-1
`34Lys36 -(GAB-GOct) GLP-1(7-37); Tbr8 Arg26Lys34-( GAB-
`(7-38); Thr8 Asp19 Arg26' 34Lys27 -(GAB-GHex) GLP-1(7- 55 GOct) GLP-1(7-38); Tbr8 Arg34Lys2 6-(GAB-GOct) GLP-1
`36); Tor8 Aspn Arg26' 34Lys27 -(GAB-GHex) GLP-1(7-36);
`(7-38); Thr8 Arg26' 34Lys38-(GAB-G0ct) GLP-1(7-38);
`Tbr8 Asp19 Arg26
`• 34Lys27-(GAB-GHex) GLP-1(7-36)amide;
`Tb rs Arg 26 Ly s 3 4 - (GAB - GO c t ) G LP - 1(7 - 39);
`34Lys27-(GAB-GHex) GLP-1(7-36)
`Tbr8 Arg34Lys26-(GAB-GOct) GLP-1(7-39); Tbr8 Arg26'
`Thr8 Asp17&
`amide; Tbr8Asp 19Arg26· 34Lys27-(GAB-GHex) GLP-1(7-
`34Lys39-(GAB-G0ct) GLP-1(7-39);
`37); Tors Asp19 Arg26· 34Lys27 -(GAB-GHex) GLP-1(7-38); 60 Gly8Glu35 Arg26· 34Lys36 -(GAB-GOct) GLP- 1(7 -36);
`3 4Lys27-(GAB-GHex) GLP-1(7-38);
`Gly8Glu35 Arg;-6' 34Lys3 6-(GAB-G0ct) GLP-1(7-36)amide;
`Tbr8 Asp17 Arg26
`Gly8Glu36Arg26· 34Lys37-(GAB-G0ct) GLP-1(7-37);
`Arg26Lys34-(GAB-G0ct) GLP-1(7-36); Arg34Lys26-(GAB-
`GOct) GLP-1(7-36); Arg26· 34Lys36-(GAB-GOct) GLP-1(7-
`Gly8Glu37 Arg26· 34Lys38-(GAB-GOct) GLP-1(7-38);
`36); Arg26Lys34 -(GAB-G0ct) GLP- 1(7-36)amide;
`Gly8Glu38Arg26' 34Lys39-(GAB-G0ct) GLP-1(7-39);
`Arg34Lys26-(GAB-G0ct) GLP-1(7-36)amide; Arg26' 65 Gly8Glu35 Arg26 34Lys36-(GAB-G0ct) GLP-1(7-36);
`34Lys36-(GAB-GOct) GLP-1(7-36)amide; Arg26 Lys34-
`Gly8 Glu35 Arg;-6
`3 4Lys36-(GAB-GOct) GLP-1(7-36)amide;
`GJy8GJu36Arg26• 34Lys37-(GAB-G0 ct) GLP-1(7-37);
`(GAB-GOct) GLP-1(7-37); Arg34Lys26-(GAB-G0ct) GLP-
`
`826
`Ar
`'
`
`•
`
`•
`
`•
`
`1
`
`'
`
`•
`
`FRESENIUS EXHIBIT 1020
`Page 62 of 129
`
`
`
`119
`34Lys3 8 -(GAB-GOct) GLP-1(7-38);
`Gly8 Glu37 Arg26
`'
`34Lys3 9 -(GAB-GOct) GLP-1(7-39);
`Gly8 Glu3 8 Arg2 6 •
`3 4 Lys3 6 -(GAB-GOct) GLP-1(7-36);
`Gly8 A-;p3 5 Arg26
`•
`Gly8 Asp35 Arg26
`3 4 Lys36 -( GAB-GOct) GLP-1(7-36)amide;
`•
`34Lys37-(GAB-GOct) GLP-1(7-37);
`Gly8 A-;p3 6 Arg26•
`Gly8 A-;p37 Arg26
`3 4 Lys3 8 -(GAB-GOct) GLP-1(7-38);
`•
`Gly8 A-;p3 8 Arg2 6
`34Lys3 9 -(GAB-GOct) GLP-1(7-39);
`Giy8 A-;p 35 Arg26
`3 4 Lys36-(GAB-GOct) GLP-1(7-36);
`•
`Gly8 Asp35 Arg26
`34Lys36 -(GAB-GOct) GLP-1(7-36)arnide;
`•
`3 4 Lys37-(GAB-GOct) GLP-1(7-37);
`Gly8A-;p36Arg26
`•
`Gly8A-;p 37 Arg26
`3 4 Lys38-(GAB-GOct) GLP-1(7-38);
`•
`Gly8 Asp38 Arg26
`34Lys39 -(GAB-GOct) GLP-1(7-39);
`•
`3 4 Lys36-(GAB-G Oct) GLP-1(7-36);
`6
`Vai8Glu35 Art
`'
`VaJ8GJu35 Arg-6
`3 4Lys36-(GAB-GOct) GLP-1(7-36)arnide;
`•
`3 4 Lys37-(GAB-GOct) GLP-1(7-37);
`Vals Glu36 Arg26
`•
`Vals GJu37 Arg26•
`3 4 Lys38-(GAB-GOct) GLP-1(7-38);
`34Lys3 9 -(GAB-GOct) GLP-1(7-39);
`ValsGJu38 Arg2 6•
`3 4 Lys36-(GAB-GOct) GLP-1(7-36);
`Vals Glu35 Arg26
`•
`34Lys36-(GAB-GOct) GLP-1(7-36)amide;
`VaJ8GJu35 Arg2 6
`•
`3 4 Lys37-(GAB-GOct) GLP-1(7-37);
`VaJ8 GJu36 Arg2 6
`•
`Vals GJu37 Arg2 6•
`34Lys38-(GAB-GOct) GLP-1(7-38);
`3 4Lys39-(GAB-GOct) GLP-1(7-39);
`VaJ8 GJu38Arg26
`•
`34Lys36-(GAB-GOct) GLP-1(7-36);
`Val8A-;p35 Arg26•
`VaJ8 Asp35 Arg26
`34Lys36 -(GAB-GOct) GLP-1(7-36)amide;
`•
`
`34Lys37 -( GAB-GOct) GLP-1(7-37);
`Vais Asp 3 6 A rg26•
`Val8 Asp 37 Arg26•
`3 4 Lys38 -( GAB-GOct) GLP-1(7-38);
`Val8 Asp 38 Arg26
`34 Lys39 -( GAB-GOct) GLP-1(7-39);
`'
`34Lys3 6 -( GAB-GOct) GLP-1(7-36);
`Vais Asp 35 Arg26•
`Vais A-;p35 Arg2 6
`34Lys36-(GAB-GOct) GLP-1(7-36)amide;
`•
`Val8 Asp 3 6Arg26
`34 Lys37-(GAB-GOct) GLP-1(7-37);
`'
`Vais Asp 37 Arg26
`3 4 Lys38
`-( GAB-GOct) GLP-1(7-38);
`•
`3 4Lys3 9 -(GAB-GOct) GLP-1(7-39);
`Vais A-;p38 Arg2 6
`'
`Ser8 Glu35Arg26
`34Lys36-(GAB-GOct) GLP-1(7-36);
`'
`Ser8Glu35 Arg2 6
`3 4Lys36 -(GAB-GOct) GLP-1(7-36)amide;
`•
`Ser8 Glu36 Arg2 6
`
`34Lys37 -( GAB-GOct) GLP-1(7-3 7);
`'
`Ser8 Giu37 Arg26
`3 4 Lys38-(GAB-GOct) GLP-1(7-38);
`Ser8 Giu3 8 Arg26
`3 4 Lys39
`-( GAB-GOct) GLP-1(7-39);
`3 4 Lys36-(GAB-GOct) GLP-1(7-36);
`Ser8 Glu35 Arg26
`•
`Ser8Glu35 Arg2 6
`34Lys36-(GAB-GOct) GLP-1(7-36)amide;
`•
`Ser8 GJu3 6 Arg2 6
`3 4 Lys37-(GAB-GOct) GLP-1(7-37);
`•
`Sers Glu37 Arg2 6
`34Lys38-(GAB-GOct) GLP-1(7-38);
`•
`34Lys39-(GAB-GOct) GLP-1(7-39);
`Ser8GJu38Arg2 6
`•
`34Lys36-(GAB-GOct) GLP-1(7-36);
`Ser8 Asp35 Arg26
`•
`3 4Lys36 -(GAB-GOct) GLP-1(7-36)arnide;
`Ser8 Asp35 Arg26
`•
`Ser8 Asp 36 Arg26
`
`34 Lys37 -( GAB-GOct) GLP-1(7-37);
`•
`Ser8 Asp 37 Arg26
`
`3 4 Lys38 -( GAB-GOct) GLP-1(7-38);
`•
`3 4 Lys39 -( GAB-GOct) GLP-1(7-39);
`Sers Asp 38 Arg26•
`34Lys3 6 -( GAB-GOct) GLP-1(7-36);
`Sers Asp 35 Arg26•
`34Lys36-(GAB-GOct) GLP-1(7-36)amide;
`Ser:8 Asp35 Arg26•
`Ser8 Asp 3 6 Arg2 6
`34 Lys37 -( GAB-GOct) GLP-1(7-37);
`'
`Sers Asp 37 Arg26•
`34Lys3s -( GAB-GOct) GLP-1(7-38);
`34Lys39 -(GAB-GOct) GLP-1(7-39);
`Ser:8 Asp38 Arg26•
`3 4 Lys3 6 -(GAB-GOct) GLP-1(7-36);
`Thr8 Glu3 5 Arg26
`'
`34Lys36 -(GAB-GOct) GLP-1(7-36)amide;
`Tor8Giu35 Arg26•
`Thr8 Giu 3 6 Arg26
`34Lys37 -( GAB-GOct) GLP-1(7-37);
`'
`Tbr8 Glu 37 Arg26
`34Lys3 8
`-( GAB-GOct) GLP-1(7-38);
`Tbr8 Glu 38 Arg26
`
`3 4 Lys39 -( GAB-GOct) GLP-1(7-39);
`Thr8 Giu 35 Arg26
`34Lys3 6 -( GAB-GOct) GLP-1(7-36);
`'
`34Lys36-(GAB-GOct) GLP-1(7-36)amide;
`Tor8Giu35 Arg26•
`Tbr8 Glu 3 6 Arg26
`
`3 4 Ly/l7 -( GAB-GOct) GLP-1(7-37);
`•
`Tbr8 Glu 37 Arg26
`34Lys38 -(GAB-GOct) GLP-1(7 -38);
`'
`34Lys39-(GAB-GOct) GLP-1(7-39);
`Tor8Glu38Ara26
`•
`Tor8Asp3 5Arg2 6
`34Lys36-(GAB-GOct) GLP-1(7-36);
`•
`34Lys36 -(GAB-GOct) GLP-1(7-36)arnide;
`Tbr8 Asp35 Arg26
`•
`3 4 Lys37-(GAB-GOct) GLP-1(7-37);
`Thr8 Asp 36 Arg26
`•
`3 4 Lys38-(GAB-GOct) GLP-1(7-38);
`Thr8 Asp37 Arg26
`34Lys39 -(GAB-GOct) GLP-1(7-39);
`Tbrs Asp 38 Arg26
`
`•
`
`•
`
`•
`
`'
`
`•
`
`'
`
`'
`
`US 6,458,924 B2
`
`-
`
`-
`
`120
`3 4 Lys36-(GAB-GOct) GLP-1(7-36);
`Thr8 Asp35 Arg2 6
`'
`34Lys36-(GAB-GOct) GLP-t(7-36)amide;
`Tor8 Asp35 Arg26•
`3 4 Lys3 7 -(GAB-GOct) GLP-1(7-37);
`Thr8 Asp3 6 Arg2 6
`'
`3 4 Lys38 -(GAB-GOct) GLP-1(7-38);
`Thr8 Asp37 Arg2 6
`'
`s Tor8 Asp38 Arg26•
`34Lys39 -( GAB-GOct) GLP-1(7-39); Argzo.
`34Lys18 -(GAB-GOct) GLP-1(7-36); Arg26
`34Lys18-(GAB(cid:173)
`'
`3 4Lys1 8 -(GAB-GOct)
`GOct) GLP-1(7-36)arnide; Arg26
`'
`34Lys18-(GAB-GOct) GLP-1(7-38);
`GLP-1(7-37); Arg26
`•
`GJy8 Asp 19 Arg26
`34Lys1 8 -(GAB-GOct) GLP-1(7-36);
`•
`10 Gly 8 Asp 1 7 Arg26
`3 4 Lys1 8 -(GAB-GOct) GLP-1(7-36);
`•
`
`34Lys18 -( GAB-GOct) GLP-1(7-36)amide;
`Gly8 Asp19 Arg26
`•
`3 4Lys18 -(GAB-GOct) GLP-1(7-36)amide;
`Gly8 Asp1 7 Arg26
`•
`
`3 4 Lys1 8 -( GAB-GOct) G LP-1(7-37);
`G ly 8 Asp 1 9 Arg26
`•
`GJy8 Asp 1 9 Arg26
`3 4 Lys1 8 -(GAB-GOct) GLP-1(7-38);
`•
`34Lys18 -(GAB-GOct) GLP-1(7-38);
`15 Gly8Asp17Arg26
`•
`3 4Lys23
`34 Lys23-(GAB-GOct) GLP-1(7-36); Arg26
`Arg26
`•
`•
`3 4Lys23 -(GAB(cid:173)
`(GAB-GOct) GLP-1(7-36)amide; Arg26
`•
`34Lys23-(GAB-GOct) GLP-1(7-
`GOct) GLP-1(7-37); Arg26
`•
`38); GJy8 Asp19 Arg26
`34Lys23-(GAB-GOct) GLP-1(7-36);
`•
`20 Giy8 Asp 17 Arg2 6
`3 4 Lys2 3 -(GAB-GOct)-GLP-1(7-36);
`•
`34Lys23 -(GAB-GOct) GLP-1(7-36)amide;
`GJy8 Asp19 Arg26•
`GJy8 Asp17 Arg26
`3 4Lys23 -(GAB-GOct) GLP-1(7-36)amide;
`•
`3 4 Lys23-(GAB-GOct) GLP-1(7-37);
`Gly8 Asp 1 9 Arg26•
`34 Lys2 3 -(GAB-GOct) GLP-1(7-38);
`Gly8 Asp 1 9 Arg26
`•
`2s Gly8 Asp17 Arg26
`3 4Lys23 -(GAB-GOct) GLP-1(7-38);
`•
`34Lys27-(GAB-GOct) GLP-1(7-36); Arg26•
`3 4Lys27
`Arg26•
`3 4Lys2 7-(GAB(cid:173)
`(GAB-GOct) GLP-1(7-36)amide; Arg26
`'
`
`3 4Lys27 -( GAB-GOct) GLP-1(7 -
`GOct) GLP-1(7-37); Arg26•
`38); Gly8Asp19Arg2 6
`34Lys27-(GAB-GOct) GLP-1(7-36);
`'
`30 G ly8 Asp 1 7 Arg26
`
`34 Lys2 7 -( GAB-GOct) G LP-1 (7-36);
`'
`
`34Lys27 -( GAB-GOct) GLP-1(7-36)amide;
`Gly8 Asp19 Arg26
`•
`
`3 4Lys2 7 -( GAB-GOct) GLP-1(7-36)amide;
`Gly8 Asp1 7 Arg26
`•
`Gly8 A5p 1 9 Arg26
`34Lys2 7 -(GAB-GOct) GLP-1(7-37);
`•
`Gly8 Asp 1 9 Arg26
`34 Lys27 -(GAB -GOct) GLP-1(7-38);
`•
`
`3 4Lys2 7 -( GAB-GOct) GLP-1(7-38);
`35 Gly8 Asp17 Arg26
`'
`34 Lys18 -(GAB-GOct) GLP-1(7-36); Arg26
`3 4Lys18
`Arg26
`-
`•
`•
`34Lys18-(GAB(cid:173)
`(GAB-GOct) GLP-1(7-36)amide; Arg2 6
`•
`34Lys18 -(GAB-GOct) GLP-1(7-
`GOct) GLP-1(7-37); Arg26
`•
`34Lys18-(GAB-GOct) GLP-1(7-36);
`38); Vais Asp19 Arg26
`•
`40 Vais Asp 1 7 Arg26
`34Lys 18-(GAB-GOct) GLP-1(7-36);
`•
`Val8 Asp19 Arg26
`34Lys1 8 -(GAB-GOct) GLP-1(7-36)amide;
`•
`, _341:,ys18} GAB-GOct) GLP-1(7-36)amide;
`VaJ8Asp17 Arg26
`4 Lys 8 -(GAB-GOct) GLP-1(7-37);
`Vai8 Asp 19 Arg2 0 • ~
`3 4 Lys 1s-(GAB-GOct) GLP-1(7-38);
`Vais Asp 19 Arg26
`•
`45 Vai8Asp17 Arg26
`34Lys18-(GAB-GOct) GLP-1(7-38);
`•
`3 4Lys23
`34Lys23-(GAB-GOct) GLP-1(7-36); Arg26
`Arg20
`•
`•
`(GAB-GOct) GLP-1(7-36)amide; Arg26• 34Lys23-(GAB(cid:173)
`
`3 4Lys23 -( GAB-GOct) GLP-1(7-
`GOct) GLP-1(7-37); Arg26
`•
`34Lys23 -(GAB-GOct) GLP-1(7-36);
`38); Vais Asp19 Arg26•
`50 Vais Asp 1 7 Arg26
`34 Lys23-(GAB-GOct) GLP-1(7-36);
`'
`3 4Lys23 -(GAB-GOct) GLP-1(7-36)amide;
`Vais Asp19 Arg26•
`Val8 Asp17 Arg20•
`34Lys23 -(GAB-GOct) GLP-1(7-36)amide;
`Vais Asp' 9 Arg26
`34Lys23-(GAB-GOct) GLP-1(7-37);
`'
`34Lys23-(GAB-GOct) GLP- 1(7 -38);
`Val8 Asp 19 Arg26•
`55 Val8 Asp17 Arg26
`34Lys23 -(GAB-GOct) GLP-1(7-38);
`'
`34Lys2 7-(GAB-GOct) GLP-1(7-36); Arg26
`34Lys27
`Arg26
`'
`'
`-
`34Lys27-(GAB(cid:173)
`(GAB-GOct) GLP-1(7-36)amide; Arg2 6
`•
`3 4Lys27(GAB-GOct) GLP-1(7-
`GOct) GLP-1(7-37); Arg26
`'
`38); Val8 Asp19 Arg26
`34Lys27 -(GAB-GOct) GLP-1(7-36);
`•
`60 ValsAsp 1 7Arg26
`34Lys2 7 -(GAB-GOct) GLP- 1(7 -36);
`•
`Val8 Asp19 Arg26
`3 4Lys2 7 -(GAB-GOct) GLP-1(7-36)amide;
`•
`Val8,Asp17 Arg2
`3 4Lys27 iGAB-GOct) GLP-1(7-36)amide;
`:
`Val~ Asp 19 Arg-6 • 34Lys-7 -(GAB-GOct) GLP-1(7-37);
`3 4 Lys27 -(GAB-GOct) GLP-1(7-38);
`Val8 Asp 19 Arg26
`•
`65 Val8 Asp17 Arg26
`34Lys2 7 -(GAB-GOct) GLP-1(7-38);
`·
`Arg26
`34Lys18(GAB-GOct) GLP-1(7-36); Ar~· 34Lys18
`-
`•
`(GAB-GOct) GLP-1(7-36)arnide; Arg26
`34Lys1 8-(GAB-
`•
`
`-
`
`FRESENIUS EXHIBIT 1020
`Page 63 of 129
`
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`US 6,458,924 B2
`
`122
`121
`GOct) GLP-1(7-37); Arg26' 34Lys1s·(GAB-GOct) GLP-1(7-
`38); Arg26Lys34-(GAB-GLit) GLP-1(7-39); Arg34Lys26-
`(GAB-GLit) GLP-1(7-39); Arg26· 34Lys39-(GAB-GLit)
`38); Ser8 Asp19 Arg26· 34Lys18-(GAB-GOct) GLP-1(7-36);
`Sers Asp 17 Arg26· 34Lys1s -( GAB-GOct) GLP-1(7-36);
`GLP-1(7-39);
`Sers Asp19 Arg26' 34Lys's -(GAB-GOct) GLP-1(7-36)amide;
`G I y s Ar g 26 L y s 3 4 -(GAB - G Lit) G L P-1 ( 7 - 3 6);
`Ser8 Asp17 Arg26· 34Lys18-(GAB-GOct) GLP-1(7-36)amide; s Gly8Arg34Lys26-(GAB-GLit) GLP-1(7-36); Gly8 Arg26·
`Sers Asp 19 Arg26' 34Lys1s·(GAB-GOct) GLP-1(7-37);
`34Lys36-(GAB-GLit) GLP-1(7-36); Gly8 Arg26Lys34-(GAB-
`Sers Asp ' 9 Arg26' 34 Lys' s·(GAB-GOct) GLP-1(7-38);
`GLit) GLP-1(7-36)amide; GlysArg34Lys26-(GAB-GLit)
`Ser8 Asp17 Arg26· 34Lys18 -(GAB-GOct) GLP-1(7-38);
`GLP-1(7-36)amide; Glys Arg26· 34Lys36 -( GAB-GLit) GLP-
`Arg26· 34Lys23y(GAB-GOct) GLP-1(7-36); Arg26
`• 34Lys23-
`1(7-36)amide; GJy8 Arg26Lys34-(GAB-GLit) GLP-1(7-37);
`(GAB-GOct) GLP-1(7-36)amide; Arg2t, 34Lys23 -(GAB- 10 Gly8 Arg34Lys26 -(GAB-GLit) GLP-1(7-37).; Gly8 Arg26'
`GOct) GLP-1(7-37); Arg26· 34Lys23-(GAB-GOct) GLP-1(7-
`34Lys36-(GAB-GLit) GLP-1(7-37); Gly8 Arg 6Lys34-(GAB-
`38); Ser8 Asp19 Arg26· 34Lys23-(GAB-GOct) GLP-1(7-36);
`GLit) GLP-1(7-38); Gly8 Arg34Lys26-(GAB-GLit) GLP-1(7-
`Ser8 Asp 17 Art6• 34Lys23 -(GAB-GOct) GLP-1(7-36);
`38); Gly8 Arg26' 34Lys38 -(GAB-GLit) GLP- 1(7-38);
`G I ys Arg26 L ys 34 - (GAB - G Lit) G LP -1 (7 - 39);
`Ser8Asp19Arg·6· 34Lys23-(GAB-GOct) GLP-1(7-36)amide;
`Ser8 A51>17 Arg26• 34Lys23-(GAB-GOct) GLP-1(7-36)amide; 15 Gly8 Arg34Lys26-(GAB-GLit) GLP-1(7-39); G!y8 Arg26•
`Ser8 Asp 19 A rg26· 34Lys23-( GAB-GOct) GLP-1(7-37);
`34Lys39-(GAB-GLit) GLP-1(7-39);
`Sers Asp 19 A rg26• 34Lys23 -(GAB-GOct) GLP-1(7-38);
`Va Is A rg 2 6 Ly s 3 4 - ( G AB - G L it) G LP -1 (7 - 3 6);
`Ser8 A51>17 Arg26• 34Lys23-(GAB-GOct) GLP-1(7-38);
`Vais Arg34Lys26 -(~AB-GLit) GLP-H7-36); Vais Arg26'
`Arg26· 34Lys27-(GAB-GOct) GLP-1(7-36); Arg26· 34Lys27-
`34Lys36-(GAB-GLit) GLP-1(7-36); Val8Arg26Lys34-(GAB-
`(GAB-GOct) GLP-1(7-36)amide; Arg2 ' 34Lys27-(GAB- 20 GLit) GLP-1(7-36)amide; Vais Arg34Lys26-(GAB-GLit)
`GOct) GLP-1(7-37); Arg26• 34Lys27-(GAB-GOct) GLP-1(7-
`GLP-1(7-36)amide; Vais Arg26• 34Lys36-( GAB-GLit) GLP-1
`(7-36)amide; Va18 Arg26Lys34 -(GAB-GLit) GLP-1(7-37);
`38); Ser8 Asp19 Arg26· 34Lys27 -(GAB-GOct) GLP-1(7-36);
`Sers Asp 17 Arg26• 34Lys27 -( GAB-GOct) GLP-1(7-36);
`Val8 Arg34Lys26-(GAB-GLit) GLP-1(7-37); Vais Arg26•
`34Lys36-(GAB-GLit) GLP-1(7-37); Vais Arg26Lys34 -(GAB-
`Sers Asp19 Arg26' 34Lys27 -(GAB-GOct) GLP-1(7-36)amide;
`Ser8 Asp17 Arg26· 34Lys27-(GAB-GOct) GLP-1(7-36)amide; 25 GLit) GLP-1(7-38); ValsArg34Lys26-(GAB-GLit) GLP-1(7-
`Sers Asp 19 Arg26• 34Lys27 -( GAB-GOct) GLP-1(7-37);
`38); Va Is Arg26• 34Lys38 -( GAB-GLit) GLP-1(7-38);
`Va Is A rg 2 6 Ly s 3 4 - ( G AB-G L it ) G L P-1 ( 7 -3 9);
`Sers Asp 19 Arg26' 34 Lys27 -( GAB-GOct) GLP-1(7-38);
`Ser8 Asp17 Arg26· 34Lys27 -(GAB-GOct) GLP-1(7-38);
`Val8 Arg34Lys26-(GAB-GLit) GLP-1(7-39); Vais Arg26•
`Arg26· 34Lys1s·(GAB-GOct) GLP-1(7-36); Arg26
`34Lys39-(GAB-GLit) GLP-1(7-39);
`• 34Lys1s.
`(GAB-GOct) GLP-1(7-36)amide; Arg26' 34Lys1s·(GAB- 30 Ser 8 Arg26 Lys 34-(GAB-G L it) GLP-1(7-36);
`GOct) GLP-1(7-37); Arg26· 34Lys1s·(GAB-GOct) GLP-1(7-
`Ser8 Arg34Lys26-(GAB-GLit) GLP-1(7-36); SersArg26·
`38); Tors Asp19 Arg26
`
`• 34Lys18 -(GAB-GOct) GLP-1(7-36);
`34Lys36 -(GAB-GLit) GLP-1(7-36); Sers Arg26Lys34 -( GAB-
`Tbrs Aspn Art6' 34Lys' s·(GAB-GOct) GLP-1(7-36);
`GLit) GLP-1(7-36)amide; SersArif4Lys26-(GAB-GLit)
`GLP-1(7-36)amide; Ser8 Arg26· 34Lys 6-(GAB-GLit) GLP-1
`· 34Lys1s -(GAB-GOct) GLP-1(7-36)amide;
`Thr8 Asp19 Arg
`• 34Lys1s -(GAB-GOct) GLP-1(7-36)amide; 35 (7-36)amide; Ser8 Arg26Lys34 -(GAB-GLit) GLP-1(7-37);
`Tbr8 Asp" Arg26
`TbrsAsp19Arg26· 34Lys1s·(GAB-GOct) GLP-1(7-37);
`Ser8Arg34Lys26-(GAB-GLit) GLP-1(7-37); Ser8Arg26'
`TbrsAsp19Ar~26· 34Lys1s ·(GAB-GOct) GLP-1(7-38);
`34Lys36-(GAB-GLit) GLP-1(7-37); SersArg26Lys34-(GAB-
`Tbr8 As1>1' Arg"6• 34Lys18 -(GAB-GOct) GLP-1(7-38);
`GLit) GLP-1(7-38); Sers Arg34Lys26 -(GAB-GLit) GLP-1(7-
`Arg26· 34Lys23(GAB-GOct) GLP-1(7-36); Arg26· 34Lys23-
`38); Ser8Arg26' 34Lys38-(GAB-GLit) GLP-1(7-38);
`(GAB-GOct) GLP-1(7-36)amide; Arg26· 34Lys23-(GAB- 40 Ser 8 Arg2 6Lys 34-(GAB-G L it) G LP -1(7-39);
`GOct) GLP-1(7-37) ; Arg26• 34Lys23-(GAB-GOct) GLP-1(7-
`Sers Arg34Lys26 -(GAB-GLit) GLP-1(7-39) ; Ser8 Arg26·
`38); 111r8 Asp19 Arg26
`• 34Lys23-(GAB-GOct) GLP-1(7-36);
`34Lys39 -(GAB-GLit) GLP-1(7-39);
`Thrs Asp17 Arg26• 34Lys23 -(GAB-GOct) GLP-1(7-36);
`Th rs A rg 26 Ly s 3 4 -(GAB- G Lit) G LP -1 (7 -3 6);
`Tbrs Arg34Lys26-(GAB-GLit) GLP-1~7-39); Thr8 Arg26·
`Tbr8 Asp19 Arg26• 34Lys23-(GAB-GOct) GLP-1(7-36)amide;
`111r8 Asp17 Arg26
`• 34Lys23-(GAB-GOct) GLP-1(7-36)amide; 45
`34Lys36-(GAB-GLit) GLP-1(7-36); Tiu Arg26Lys34-(GAB-
`Thr8 Asp19 Arg26• 34Lys23 -(GAB-GOct) GLP-1(7-37);
`GLit) GLP-1(7-36)amide; Thrs Arg34Lys20-(GAB-GLit)
`Thr8Asp19Arg26• 34Lys23-(GAB-GOct) GLP-1(7-38);
`GLP-1(7-36)amide; Thr8Arg26• 34Lys36-(GAB-GLit) GLP-
`111r8 Asp17Arg26· 34Lys23-(GAB-GOct) GLP-1(7-38);
`1(7-36)amide; Thr8 Arg26Lys34-(GAB-GLit) GLP-1(7-37);
`Arg26• 34Lys27 -(GAB-GOct) GLP-1(7-36); Arg20• 34Lys27 -
`Thr8 Arg34Lys20 -( GAB-GLit) GLP-1(7-3 7); Thr8 Arg26•
`(GAB-GOct) GLP-1(7-36)amide; Arg26' 34Lys27-(GAB- 50 34Lys36(GAB-GLit) GLP-1(7-37); 111rs Arg26Lys34-(GAB-
`GOct) GLP-1(7-37); Arg26· 34Lys27-(GAB-GOct) GLP-1(7-
`GLit) GLP-1(7-38); Tur8 Arg34Lys26-(GAB-GLit) GLP-1(7-
`38); T hr8Arg20• 34Lys38-(GAB-GLit) GLP- 1(7-38);
`38); Tor8Asp19Arg2°• 34Lys27-(GAB-GOct) GLP-1(7-36);
`Th r s A rg 26 Ly s 3 4 -(GAB- G Lit) G L P-1 ( 7-39);
`Thrs Asp17 Arg26' 34Lys27-(GAB-GOct) GLP-1(7-36);
`Tbr8 Asp19 Arg26• 34Lys27-(GAB-GOct) GLP-1(7-36)amide;
`Tbr8 Arg34Lys26-(GAB-GLit) GLP-1(7-39); Thr8 Arg26•
`• 34Lys27 -(GAB-GOct) GLP-1(7-36)amide; 55 34Lys39 -(GAB-GLit) GLP-1(7-39);
`Tbr8 Asp' ' Arg26
`TbrsAsp19 Arg26' 34Lys27 -(GAB-GOct) GLP-1(7-37);
`Gly8 Glu35 Arf6' 34Lvs36-(GAB-GLit) GLP-1(7-36) ;
`Tbrs Asp19 Arg26· 34Lys27 -(GAB-GOct) GLP-1(7-38);
`
`Gly8Glu35 Arg--6• 34Lys36-(GAB-GLit) GLP-1(7-36)amide;
`GlysGlu36Arg26' 34Lys37-(GAB-GLit) GLP-1(7-37) ;
`34Lys27-( GAB-GOct) GLP-1(7-38);
`Tbr8Asp17Arg26
`Arg26Lys34(GAB-GLit) GLP-1(7-36); Arg34Lys26-(GAB-
`Gly8 Glu37 Arg26· 34Lys38-(GAB-GLit) GLP-1(7-38);
`GLit) GLP-1(7-36); Arg26· 34Lys36-(GAB-GLit) GLP-1(7- 60 Gly8Glu38 Arg26· 34Lys39 -(GAB-GLit) GLP- 1(7-39);
`GlysGJu35 Arg26' 34Lys36-(GAB-GLit) GLP-1(7-36) ;
`36); Arg26Lys34 -(GAB-GLit) GLP-1(7-36)amide;
`Arg 34Lys26-( GAB-GLit) GLP-1(7-36)amide; Arg 26·
`Gly8Glu35 Arg26· 34Lvs36-(GAB-GLit) GLP-L1(7-36)amide;
`Gly8Glu36Arg26· 34Lys37-(GAB-GLit) GLP-1(7-37);
`34Lys36-(GAB-GLit) GLP-1(7-36)amide; Arg26Lys34-
`Giy8 Glu37 Arg26• 34Lys3 8 -(GAB-GLit) GLP-1(7-38) ;
`(GAB-GLit) GLP-1(7-37); Arg34Lys26-(GAB-GLit) GLP-1
`(7-37); Arg26' 34Lys36-(GAB-GLit) GLP-1(7-37); 65 Gly8Glu38Arg26· 34Lys39-(GAB-GLit) GLP-3(7-39);
`Gly8 Asp35 Arg26· 34Lys36-(GAB-GLit) GLP-1(7-36);
`Arg26Lys34-(GAB-GLit) GLP-1(7-38); Arg34Lys26-(GAB-
`GLit) GLP-1(7-38); Arg26• 34Lys38-(GAB-GLit) GLP-1(7-
`Giy8Asp35 Arg26• 34Lys36-(GAB-GLit) GLP-1(7-36)amide;
`
`•
`
`FRESENIUS EXHIBIT 1020
`Page 64 of 129
`
`
`
`US 6,458,924 B2
`
`•
`
`'
`
`123
`34Lys37-(GAB-GLit) GLP-1(7-37);
`Gly 8 Asp36Arg26
`'
`34Lys38-(GAB-GLit) GLP-1(7-38);
`Gly8 Asp3 7 Arg26 ·
`34Lys39-(GAB-GLit) GLP-1(7-39);
`Giy 8 Asp38 Arg26
`'
`34L);s36-(GAB-GLit) GLP-1(7-36);
`Gly8 Asp35 Ar~26
`•
`3 4 Lys 6-(GAB-GLit) GLP-1(7-36)amide;
`Gly8 Asp35 Arg26
`•
`3 4 Lys37 -(GAB-GLit) GLP-1(7-3 7);
`Gly 8 Asp3 6 Arg2 6
`'
`34Lys38-(GAB-GLit) GLP-1(7-38);
`Glys Asp37 Ar~26
`•
`Gly8 Asp3 8 Arg26
`3 4 Lys3 9 ..(GAB-GLit) GLP-1(7-39);
`'
`34L ,s36-(GAB-GLit) GLP-1(7-36);
`Vals Glu 35 Arf/6
`•
`Val8 Glu35 Arg-6
`34Lys?6 )GAB-GLit) GLP-1(7-36)amide;
`'
`34Lys 7-(GAB-GLit) GLP-1(7-37);
`Vals Glu 36Arg2 6
`•
`Va18 Glu3 7 Arg2 6
`3 4 Lys38-(GAB-GLit) GLP-1(7-38);
`•
`3 4 Lys39-(GAB-GLit) GLP-1(7-39);
`Val8 Glu 38 Arg26
`•
`Vals GJu35 Ar 2 6
`34L s36-(GAB-GLit) GLP-1(7-36);
`•
`Val8 Glu35 Ari' 34Ly/61GAB-GLit) GLP-1(7-36)amide;
`Vals GJu36 Arg2 6 • 34Lys 7-(GAB-GLit) GLP-1(7-37);
`Vals Glu 37 Art6
`34 Lr3 s-(GAB-GLit) GLP-1(7-38);
`'
`34Lvs3 -(GAB-GLit) GLP-1(7-39);
`Va18Glu38Arg 6
`•
`34Lvs 30-(GAB-GLit) GLP-1(7-36) ;
`Vais Asp 35 Arl
`0
`•
`Val8 Asp35 ~ g'6
`34Lys'16-\GAB-GLit) GLP-1(7-36)amide;
`•
`34Lys 7-(GAB-GLit) GLP-1(7-37);
`Va18 Asp30 Arg26
`•
`34Lys 38-(GAB-GLit) GLP-1(7-38);
`Val8 Asp 37 Arg26•
`34Lys3 9 -(GAB-GLit) GLP-1(7-39) ;
`Va18 Asp3 8 Arg26
`•
`34Lys36-(GAB-GLit) GLP-1(7-36);
`Val8 Asp35 Arg26•
`Val8 Asp35 Arg26
`34Lys36-(GAB-GLit) GLP-1(7-36)amide;
`•
`34Lys37-(GAB-GLit) GLP-1(7-37) ;
`Va18 Asp3 6 Arg26
`•
`Val8 Asp37 Arg26•
`34Lys38-(GAB-GLit) GLP-1(7-38);
`Val8 Asp38 Arg26
`3 4Lys3 9 -(GAB-GLit) GLP-1(7-39);
`'
`34Lys36-(GAB-GLit) GLP-1(7 -36);
`Ser8 Glu 35 Arg26•
`Ser8 Glu35 Arg2 6
`34Lys3 6 -(GAB-GLit) GLP-1(7-36)amide;
`'
`34Lys37-(GAB-GLit) GLP-1(7-37);
`Ser8 Glu 36 Arg2 6
`'
`Sers Glu 37 Arg2 6
`34Lys3s-(GAB-GLit) GLP-1(7 -38);
`Ser8 Glu 3 8 Arg2 6
`34Lys3 9 -(GAB-GLit) GLP-1(7-39);
`34Lys36-(GAB-GLit) GLP-1(7-36);
`Ser8 Glu 35 Arg26
`'
`Ser8Glu35 Arg2 6
`34Lys3 6 -(GAB-GLit) GLP-1(7-36)amide;
`•
`Ser8 Glu 36 Arg2 6
`34Lys37-(GAB-GLit) GLP-1(7-37);
`'
`3 4 Lr3s-(GAB-GLit) GLP-1(7-38);
`Sers Glu 37 Arg26
`•
`34Lvs3 -(GAB-GLit) GLP-1(7-39);
`Ser8Glu38Arg26
`•
`34Lys 36-(GAB-GLit) GLP-1(7-36);
`Sers Asp 35 A rg26
`•
`Ser8 Asp35 Arg26
`34Lys36-(GAB-GLit) GLP-1(7-36)amide;
`•
`Sers Asp 36Arg26
`3 4 Lys 37-(GAB-GLit) GLP-1(7-37);
`•
`Sers Asp 37 Arg26
`34Lys 38-(GAB-GLit) GLP-1(7-38);
`•
`Sers Asp 38Arg26• 34Lys 39-(GAB-GLit) GLP-1(7-39) ;
`34Lys36-(GAB-GLit) GLP-1(7-36);
`Ser8 Asp35 Arg26
`•
`34Lys36-(GAB-GLit) GLP-1(7-36)amide;
`Ser8 Asp35 Arg26
`•
`Sers Asp 36 Arg26• 34Lys 37-(GAB-GLit) GLP-1(7-37) ;
`34Lys 3s-(GAB-GLit) GLP-1(7-38) ;
`Sers Asp 3 7 Arg26•
`34Lys39 -(GAB-GLit) GLP-1(7-39);
`Ser8 Asp38 Arg26•
`34Lys3 6 -(GAB-GLit) GLP-1(7-36);
`Thr8 Glu35A rg26
`•
`34Lys30-(GAB-GLit) GLP-1(7-36)amide;
`Tor8Glu35 Arg26•
`Thr8 Glu36Arg26
`34 Lys37-(GAB-GLit) GLP-1(7-37);
`'
`Thr8 Glu37 Arg26
`34Lys38-(GAB-GLit) GLP-1(7-38);
`•
`34Lys 39-(GAB-GLit) GLP-1(7-39);
`ThrsGJu 36 Arg26•
`Thr8 Glu3 5Arg26
`34Lys3 6 -(GAB-GLit) GLP-1(7-36);
`•
`34Lys36-(GAB-GLit) GLP-1(7-36)amide;
`Tor8Glu35 Arg26•
`Thr8 Giu3 6 Arg26
`34Lys3 7 -(GAB-GLit) GLP-1(7-37);
`'
`Tbr8 Glu37 Arf
`34Lys38-(GAB-GLit) GLP-1(7-38);
`6
`•
`34Lys39 -(GAB-GLit) GLP-1(7-39);
`Tor8Glu38 Arg-6
`•
`3 4 Lys36-(GAB-GLit) GLP- 1(7-36);
`Thr8 Asp35 Arg2 6
`'
`Tor8 Asp35 Arg26
`• 34Lys36-(GAB-GLit) GLP-1(7-36)amide;
`3 4 Lys 37-(GAB-GLit) GLP-1(7-37);
`TbrsAsp 36Arg2 6
`•
`34Lys38-(GAB-GLit) GLP-1(7-38);
`Tbr8 Asp37 Arg2 6
`3
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