WO 99/43706
`
`PCT/DK99/00082
`
`99
`
`Argzs's‘Lys‘B-(Aspa-AOct)-GLP-1 (7-36);
`
`ArgZS-“Lys‘B—(Aspa-AOct)-GLP-1 (7-36)amide;
`
`Argzs'uLys‘B—(Aspa—AOct)—GLP—1 (7-37);
`
`Argzs'“Lys‘8-(Aspa-AOct)-GLP-‘l (7-38);
`
`VaIBAsp‘gArgzs'MLys‘8-(Aspa-AOct)-GLP—1 (7-36); ValsAsp‘7Argzs'34Lys‘a-(Aspa-AOct)-G LP—1 (7-
`
`36); ValaAsp‘QArgzs'MLys‘8-(Aspa-AOct)-GLP-1(7-36)amide; ValaAsp‘7Argzs'34Lys“’-(Aspa-AOct)—
`
`GLP-1(7-36)amide; ValeAsp‘9Ar926'3“Lys‘B-(Aspa-AOct)-GLP-1(7-37); ValBAspmArgzs'MLys‘e-
`
`(Aspa-AOct)—GLP-1(7—38); VaI8ASp17Ar926'34Lys18—(Aspa-AOct)-GLP—1 (7-38);
`
`Arg26'34Ly523—(Aspa-A0ct)-GLP-1 (7-36);
`
`Argze'MLyszs-(Aspa-AOct)—GLP-1 (7-36)amide;
`
`Arg26'34Ly523-(Aspa-A0ct)-GLP-1 (7-37);
`
`ArgZG'MLysza-(Aspa-AOct)—GLP-1 (7-38);
`
`VaIBAsp‘9Argzs'34Ly523-(Aspa-AOct)-GLP-1 (7-36); ValaAsp‘7ArgZG'MLysza-(Aspa-AOctyGLP-1(7-
`
`36); ValaAsp‘gArgzs'MLysza-(Aspa-AOct)—GLP-1(7-36)amide; ValsAsp17Argze'uLy523-(Aspa-A0ct)-
`
`GLP-1(7—36)amide; Va|8Asp19Arg25-34Ly523-(Aspa-A0ct)-GLP-1(7-37);
`
`VaIBAsp‘gArgzs'MLysza-
`
`(Aspa-AOct)—GLP-1 (7-38); VaIsAsp17Argz‘5'34Lysza-(Aspa-AOct)-GLP-1 (7-38);
`
`ArgZG-“Lys27-(Aspa-AOct)-GLP-1 (7-36);
`
`Arg26'34Ly327-(Aspa-A0ct)-GLP-1 (7-36)amide;
`
`Argzs'“LysZ7-(Aspa-AOct)-GLP-1 (7—37);
`
`ArgZG'MLysfl—(Aspa-AOct)-GLP—1 (7—38);
`
`ValsAsp19Ar926-34Lys”—(Aspa-AOct)-GLP-1 (7-36); ValeAsp17Arg25'34Ly327-(Aspa-AOct)-GLP-1 (7-
`
`36); VaIBAsp‘9Ar925'3‘Ly527-(Aspa-AOct)-GLP-1(7—36)amide; ValaAsp‘7Argzs'3“LysZ7—(Aspa-A0ct)-
`
`GLP-1(7-36)amide; ValaAsp‘gArgzs'S“Lys”-(Aspa—AOct)—GLP—1(7-37); VaIBAsp‘gArgze's‘Lysfl-
`
`(Aspa-AOct)—GLP-1(7-38); VaIBAsp17Argzs'3“LysZ7-(Aspa—A0ct)-GLP-1 (7-38);
`
`Argze'MLys‘8-(Aspa-A0ct)-GLP—1 (7-36);
`
`ArgZS'S‘Lys15-(Aspa-AOct)—GLP-1(7-36)amide;
`
`Argzs-“Lys‘8-(Aspa-AOct)-GLP-1 (7-37);
`
`Argzs-“Lys‘8-(Aspa-AOct)-GLP-1 (7-38);
`
`SerBAsp‘9Ar925'34Lys‘B-(Aspa-AOct)-GLP—1 (7—36); SerBAsp‘7Argzs'3‘Lys‘5-(AspahAOct)-GLP-1 (7-
`
`36);
`
`SeraAsp19Argze'34Lys18—(Aspa-AOct)-GLP—1(7-36)amide;
`
`SersAsp‘7Argz‘5'34Lys‘8-(Aspa-
`
`AOct)-GLP-1 (7-36)amide;
`
`SersAsp‘9Argzs-34Lys‘s—(Aspa-AOct)-GLP-1 (7-37);
`
`SerBAsp‘9Argzs'34Lys1B—(Aspa-AOct)—GLP-1 (7-38); SerBAsp‘7Argzev34Lys‘B—(Aspa-AOct)—GLP-1 (7-
`
`1O
`
`15
`
`20
`
`25
`
`33);
`
`Argze'uLysm-(Aspa-AOct)-GLP-1 (7—36);
`
`ArgZB'MLysza-(Aspa-AOctrGLP-1 (7-36)amide;
`
`Argze'“Lys”-(Aspa-AOct)-GLP-1 (7-37);
`
`Argzs'MLysn-(Aspa-AOct)-GLP-1 (7-38);
`
`SereAsp‘9Ar926‘3“Lysza-(Aspa-AOct)-GLP-1 (7-36); SersAsp‘7Ar926'“Lyszs-(Aspa-AOct)-GLP-1 (7-
`
`36);
`
`SeraAsp19Arg25'3‘Ly523-(Aspa-AOct)-GLP-1(7-36)amide;
`
`SeraAsp17Argze'34Ly523-(Aspa—
`
`30
`
`AOct)-GLP-1 (7-36)amide;
`
`SeraAsp‘9Ar926-34Lysza-(Aspa-AOct)-GLP-1 (7-37);
`
`SersAsp‘9Argzs'uLysza-(Aspa-AOctyGLP-1 (7—38); SerBAsp17Ar926'“Ly523-(Aspa—AOct)-GLP-1 (7-
`
`38);
`
`Argze-“Lysm-(Aspa-AOct)-GLP-1 (7-36);
`
`Argzs'MLysfi-(Aspa-AOct)-GLP-1 (7-36)amide;
`
`Argze'a‘Lysfl-(Aspa-AOct)-GLP-1 (7-37);
`
`Ar926'34Ly527-(Aspa-A0ct)-GLP-1 (7-38);
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 101 of 270
`
`

`

`WO 99/43706
`
`PCT/DK99/00082
`
`100
`
`SerBAsp'9Arg26'34Ly527-(Aspa-A0ct)-GLP-1 (7-36); SeraAsp17Argz‘5'34LySZ7-(Aspa-AOct)-GLP-1 (7-
`
`36);
`
`SetBAsp‘9Argzs'3“LysZ7-(Aspa-AOct)-GLP-‘I(7-36)amide;
`
`SeraAsp17Argzs-34Ly327-(Aspa-
`
`AOct)-GLP-1(7-36)amide;
`
`SerfiAsp‘9Argzav34Lys27-(Aspa-A0ct)-GLP-1(7-37);
`
`SeraAsp‘gArgzs'“Ly327-(Aspa-AOct)-GLP-1 (7-38); SeraAsp17Argzs'34Lysz7-(Aspa-AOct)—GLP-1 (7-
`
`38);
`
`Argza-“Lys‘3-(Aspa-AOct)-GLP-1 (7—36);
`
`ArgZG'MLys‘B-(Aspa-AOct)—GLP-‘I (7-36)amide;
`
`ArgZS'MLys‘a—(Aspa-AOct)—GLP—1 (7-37);
`
`Argzs'“Lys‘B—(Aspa-AOct)—GLP-1 (7-38);
`
`ThraAsp‘9Argzs‘34Lys‘B-(Aspa-AOct)—GLP-1 (7-36); Thr’sAsp‘7Argzs'34Lys‘8-(Aspa-AOct)-GLP—1 (7-
`
`36); ThrBAsp‘9Argze'3“Lys‘B-(Aspa-AOct)-GLP-1(7-36)amide; ThraAsp17Argz‘5'3‘Lys‘8-(Aspa-AOct)-
`
`GLP-1(7-36)amide;
`
`ThrBAsp'9Argze'3‘Lys‘B-(Aspa-AOct)-GLP-1(7-37);
`
`Thl‘Asp‘QArgze'MLysw-
`
`(Aspa-AOct)—GLP—1 (7—38); Thr8Asp17Argze'34Lys‘B-(Aspa—AOct)—GLP-1 (7—38);
`
`Argzs'MLysza-(Aspa-AOct)-GLP-1 (7-36);
`
`ArgZG'MLysfl-(Aspa-AOct)-GLP-1 (7—36)amide;
`
`Argze'MLysza-(Aspa-AOct)—GLP-1 (7-37);
`
`Argzs'MLysza-(Aspa-AOct)—GLP-1 (7-38);
`
`Th rBAsp‘9ArgZS'MLysza-(Aspa-AOctyGLP-1 (7-36); Th rBAsp17Argze'34Ly523-(Aspa-AOct)-GLP-1 (7-
`
`36); ThrBAsp19Argze'34Lysza-(Aspa-AOct)—GLP—1(7—36)amide; ThrfiAsp17Argze'34Ly523-(Aspa—AOct)-
`
`GLP-1(7-36)amide; ThrsAsp‘9Arg26'“Lysza-(Aspa-A0ct)-GLP-1(7-37); ThraAsprrgze'MLyszs-
`
`(Aspa-AOct)-GLP-1 (7-38); ThrsAsp17Argze'34Lysza-(Aspa-AOct)-G LP-1 (7-38);
`
`Argzs'MLysfl-(Aspa-AOct)-G LP-1 (7-36);
`
`ArgZG-“Ly827-(Aspa-AOct)-GLP-1 (7-36)amide;
`
`ArgZG'MLysfl-(Aspa-AOct)-GLP—1 (7-37);
`
`Argze'MLysfl-(Aspa-AOct)—GLP-1 (7-38);
`
`Thr‘Asp‘9Argze'34Ly327—(Aspa-AOct)-GLP-1 (7-36); ThrsAsp17Arg25'34Ly527-(Aspa-AOct)-GLP-1(7-
`
`36); ThraAsp‘QArgzs'MLysy-(Aspa-AOct)-GLP-1(7-36)amide; ThraAsp17Argza-34Ly327-(Aspa-AOct)-
`
`GLP-1(7-36)amide;
`
`ThrsAsp19Arg26'34Ly527-(Aspa-AOct)-GLP-1(7-37);
`
`ThrBAsp‘aArgze'MLysfl—
`
`(Aspa-AOct)—GLP—1 (7-38); ThrsAsp1 7Argz‘5'3"Ly527-(Aspa1-AOct)-G LP-1 (7-38);
`
`ArgzeLysu-(Aspa-ALityGLP—1(7-36); ArQMLyszs-(Aspa-ALityGLP-1(7-36); Argze'MLysas-(Aspa-
`
`ALit)-GLP-1(7-36); ArgZGLysu-(Aspa-ALit)-GLP-1(7-36)amide; Arg3“ Lyszs-(Aspa—ALit)-GLP-1(7-
`
`36)amide; Argzs'MLysw—(Aspa-ALit)-GLP-1(7-36)amide; Arg26 Lys“-(Aspa—ALit)—GLP-‘l(7-37);
`
`Arg“LysZG—(Aspa-ALit)-GLP-1(7-37); Argzs'MLysae-(Aspa-ALit)—GLP-1(7-37); ArgzeLySM-(Aspa-
`
`ALit)-GLP-1(7-38); Arg34Lyszs-(Aspa—ALit)—GLP-1(7-38) ; Argzs'a“Lyssa-(Aspa-ALit)-GLP-1(7-38);
`
`ArgzsLysu-(Aspa-ALityGLP-1(7-39); ArguLyszs-(Aspa—ALityGLP-1(7-39); Argzs'uLysag—(Aspa-
`
`1O
`
`15
`
`20
`
`25
`
`30
`
`ALit)—GLP-1(7-39);
`
`GlyBArgzeLyss‘L(Aspa-ALit)-GLP-1 (7-36);
`
`GlysArgmLyszs-(Aspa-ALit)-GLP-‘I (7-36);
`
`GlyaArgze'MLysss-(Aspa-ALit)-GLP—1 (7—36);
`
`GIyBArgzeLySM-(Aspa-ALit)—GLP-1 (7-36)amide;
`
`G|y8Arga4Lysze—(Aspa-ALit)-GLP-1 (7-36)amide;
`
`GlyBArgzs'uLysss-(Aspa-ALit)-GLP-1(7—
`
`36)amide; GIyBArgz“Lys“—(Aspa-ALit)—GLP-1(7-37); GIyBArQMLysze-(Aspa-ALit)-GLP-1(7-37);
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 102 of 270
`
`

`

`WO 99/43706
`
`PCT/DK99/00082
`
`101
`
`GlyaArgze'MLys36-(Aspa-ALit)-GLP—1 (7—37);
`
`GlyaArgzeLySM-(Aspa-ALit)—GLP-1 (7-38);
`
`GlyaArQMLyszs-(Aspa-ALit)-GLP-1(7-38)
`
`;
`
`G|yaArg26'34Lys38—(Aspa-ALit)-GLP-1(7-38);
`
`GIyBArgzeLys“-(Aspa-ALit)—G LP-1 (7-39);
`
`Gly8Ar934Lysze-(Aspa-ALit)—GLP-1 (7—39);
`
`GlyaArgze'MLysw-(Aspa-ALit)—GLP—1(7—39);
`
`VaI3ArgzsLysu—(Aspa—ALit)—GLP-1 (7—36);
`
`VaIBArg34Lysze-(Aspa-ALit)-GLP-1 (7-36);
`
`ValBArgze'MLysss-(Aspa-ALit)-GLP-1 (7-36);
`
`VaIBArgzsLys“-(Aspa—ALit)—GLP-1 (7—36)amide;
`
`VaIBArQMLysze-(Aspa-ALit)—GLP-1 (7-36)amide;
`
`ValaArgzs-“Lysae-(Aspa-ALit)—GLP-1 (7—
`
`36)amide; VaIBArgzsLysm-(Aspa—ALit)—GLP-1(7-37); ValaArg“Lysza-(Aspa-ALit)-GLP-1(7-37);
`
`ValaArgze'MLysas-(Aspa-ALit)-GLP-1 (7-37);
`
`ValaArgzeLys“—(Aspa-ALit)-GLP-1(7-38);
`
`VaIBArguLysze-(Aspa-ALit)-GLP-1(7-38)
`
`;
`
`VaIBArgzs‘MLys35-(Aspa-ALit)—GLP-1(7-38);
`
`VaIBArgzaLys“-(Aspa-ALit)—GLP-1 (7-39);
`
`VaISArg34Lyszs-(Aspa-ALit)-GLP-1(7-39);
`
`VaIBArgza'uLyse‘g-(Aspa-ALit)-GLP-1(7-39);
`
`SersArgzeLySM-(Aspa-ALit)—GLP-1 (7-36);
`
`SeraArg“Lyszs-(Aspa-ALit)—GLP-1 (7—36);
`
`SeI’BArgze'MLysae-(Aspa-ALit)-GLP-1 (7-36);
`
`SeraArg26Lys“—(Aspa-ALit)—GLP-1 (7-36)amide;
`
`SerBArgmLysze-(Aspa-ALit)-GLP-1 (7-36)amide;
`
`SeraArg26-34Ly536-(A3pa-ALit)-GLP-1 (7-
`
`36)amide;
`
`SerBArgzeLysu—(Aspa—ALit)-GLP-1 (7-37); SePArgs‘Lysze-(Aspa-ALityGLP-1 (7-37);
`
`SeraArgzs'MLysas-(Aspa-ALit)-GLP-1 (7-37);
`
`SeraArgzsLys“-(Aspa-ALit)—GLP-1 (7-38);
`
`SeraArguLyszs-(Aspa-ALit)-GLP-‘I (7-38)
`
`;
`
`SerBArgze'“Lyssa-(Aspa-ALit)-GLP—1 (7-38);
`
`SerBArgzeLySM-(Aspa-ALit)-GLP-1 (7-39);
`
`SeraArgmLysze-(Aspa-ALityGLP-1 (7-39);
`
`SerBArgza'MLyssg-(Aspa-ALit)—GLP-1 (7—39);
`
`Thr8Ar926Lys34-(Aspa-ALit)-GLP-1 (7-36);
`
`Th rBArguLyszs-(Aspa—ALityGLP—1 (7-36);
`
`ThrBArgze'a“Lyssa-(Aspa—ALit)—G LP-‘I (7-36);
`
`ThrBArgzeLySM-(Aspa-ALityGLP-1 (7—36)amide;
`
`ThreArguLysze-(Aspa-ALit)-GLP-1(7-36)amide;
`
`ThraArgZSv“LysBG-(Aspa-ALityGLP-1(7-
`
`36)amide; ThrBArgzsLysu-(Aspa-ALityGLP-1(7-37); Th rBArguLysze—(Aspa—ALityGLP-1 (7-37);
`
`ThraArgzs'MLysas-(Aspa-ALit)—GLP-1 (7-37);
`
`ThraArgzsLysu-(Aspa-ALit)-GLP-1 (7—38);
`
`ThraArg34Ly526-(Aspa-ALit)-GLP-1 (7-38)
`
`;
`
`ThrBArgze'MLysae-(Aspa-ALit)-GLP-1 (7-38);
`
`ThraArgzeLySM-(Aspa-ALit)-GLP-1 (7-39);
`
`Th rBArguLyszs-(Aspa-ALityGLP-1 (7-39);
`
`ThlfiArgze'MLys39-(ASpa-ALit)—G LP-1 (7-39);
`
`GlyaGIu35Argze'34Ly336-(Aspa-ALit)-GLP-1 (7-36);
`
`Gly8G|u35Argze'34Lysae-(Aspa-ALit)-G LP—1 (7-
`
`36)amide; GlyBGIuseArgzs'MLyss7-(Aspa-ALit)—GLP-1(7-37); GlyaGlu37Argze'3‘Ly538-(Aspa-ALit)-
`
`GLP—1(7-38); GlyaGIu38Arg26'34Lys39-(Aspa-ALit)-GLP-1(7-39); G|y8GIu35Argze'34Ly536-(Aspa-ALit)-
`
`GLP-1(7—36);
`
`GlyaG|u35ArgZG‘MLysse-(Aspa-ALityGLP-1(7-36)amide;
`
`GlyBGluaeArgzs-“Lys37-
`
`(Aspa-ALit)—GLP-1(7-37); GIyBG|u37Argzs'34Lysaa-(Aspa-ALit)-GLP-1(7-38); GlyaGlusaArgzs‘MLysag-
`
`(Aspa-ALit)-GLP-1(7-39);
`
`1O
`
`15
`
`20
`
`25
`
`30
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 103 of 270
`
`

`

`WO 99/43706
`
`PCT/DK99/00082
`
`102
`
`GIyaAspfiArgzs'MLysae-(Aspa-ALit)-GLP-1 (7-36);
`
`GlyaAsp35Argze'MLysae-(Aspa-ALityGLP-1 (7—
`
`36)amide; GlyBAsp36Ar925'34Lys37~(Aspa-ALit)-GLP-‘l(7—37); GlyaAsp37Argzs-3“Lyssa-(Aspa-ALity
`
`GLP-1(7-38); Gly8Asp“ArgmLy339-(Aspa-ALit)—GLP-1(7-39);
`
`Gly8Asp35Argzs'34Ly536-(Aspa-
`
`ALit)-GLP—1 (7-36);
`
`GlysAspSSArgzs'MLysw-(Aspa-ALit)-GLP-1 (7-36)amide;
`
`GlyflAspaeArgzs'a‘Lysw-(Aspa-ALit)-GLP-1 (7-37);
`
`GlyaAsp37Arg26'34Lysas-(Aspa-ALit)-GLP-1 (7-
`
`38); GlyBAspasArg26'34Lys39-(Aspa-ALit)-GLP-1(7-39);
`
`VaIBGlU35Argzs'3‘Ly336-(Aspa-ALit)-GLP-1 (7-36);
`
`ValsGlu35Argzs'34Lysae-(Aspa-ALit)-GLP—1 (7-
`
`36)amide; ValsGlU35Argzs'34Lysa7-(Aspa-ALit)-GLP-1(7-37); ValBG|u37Ar925'34Lysaa-(Aspa-ALit)-
`
`GLP-1(7-38); VaIBG|u”Arg25'3“Lysa9-(Aspa-ALit)-GLP-1(7-39); Val8G|u35Argze'34Lysae-(Aspa-ALit)-
`
`GLP-1(7—36);
`
`VaIBGlu35Argzs'3“Lys36—(Aspa-ALit)-GLP-1(7-36)amide;
`
`ValaGluaeArgzs'MLysm-
`
`(Aspa-ALit)-GLP-1(7-37); ValaG|U37Argze'34Lysaa-(Aspa-ALit)-GLP-1(7—38); Val8G|u3BArgza'3“Ly539-
`
`(Aspa-ALit)-GLP-1 (7-39);
`
`Va|8Asp35Argze'3“Ly536-(Aspa-ALit)-G LP-1 (7-36);
`
`Valf‘Asp35Argze'3‘Ly836-(Aspa-ALit)—GLP-1 (7-
`
`36)amide; ValaAsp36Arg26'“Lys37-(Aspa—ALit)—GLP-1(7—37); VaIaAsp37Argze’34Lyssa-(Aspa-ALit)-
`
`GLP—1(7-38);
`
`ValaAspsaArgzs'MLysw-(Aspa-ALit)-GLP-1(7-39);
`
`ValaAsp35Argzs'34Lysae-(Aspa-
`
`ALit)-GLP-1(7-36); ValeAspafiArgzs-“LySB‘S—(Aspa-ALit)-GLP-1(7-36)amide; ValsAspasArgzs'“Lys37-
`
`(Aspa-ALit)-GLP—1 (7-37);
`
`VaIBAsp37Argzs'3‘Lysaa-(Aspa-ALit)—GLP-1 (7-38);
`
`VaIRAsp38Argze'3“Lyssg-(Aspa-ALit)-G LP-1 (7-39);
`
`SerBG|u35Argzs-3“Lysae-(Aspa-ALit)-GLP-1 (7-36);
`
`SereGIu35Argze'3‘Lysas-(Aspa—ALit)—GLP-1 (7-
`
`36)amide; SerBG|u35Argzs'3“Lyss7-(Aspa-ALit)-GLP-1(7-37);
`
`SeraGlU37Argze'34Lysae-(Aspa-ALit)-
`
`GLP—1(7-38);
`
`SerBGlusBArgze'uLys39—(Aspa-ALit)—GLP-1(7—39);
`
`SeraGlu35Argze-“Ly535-(Aspa-
`
`ALit)-GLP—1(7-36); Ser’SGIu35Arg25-34Ly336—(Aspa—ALit)—GLP—1(7—36)amide; SerBGluaeArgzs'MLys37—
`
`(Aspa-ALit)-GLP-1 (7-37);
`
`SeF’G|u37Argze'34Lysaa-(Aspa-ALit)-GLP-1 (7-38);
`
`Ser°G|umArgzs'“LysaQ-(Aspa-ALit)~G LP-1 (7-39);
`
`SeraAspssArgzs'“Lysas-(Aspa-ALit)-GLP-1 (7-36);
`
`SerBAsp35Argzs'34Ly535-(Aspa-ALit)—GLP-1 (7-
`
`36)amide; SersAsp35Arg26'34Lysa7-(Aspa-ALit)-GLP-1(7-37); SeFAsp37ArgZS'MLysaa-(Aspa-ALit}
`
`GLP-1(7-38);
`
`SerBAspaeArgza'MLysag-(Aspa-ALit)-GLP-1(7-39);
`
`SeraAsp35Arg26'34Ly536-(Aspa-
`
`ALit)—GLP—1(7-36);
`
`Ser8Asp35Argze'3“Lys36-(Aspa-ALit)-GLP-1(7-36)amide;
`
`SersAspaeArg26'34Ly537-(Aspa-ALit)-GLP-1 (7-37);
`
`Ser’SAsp37Argzs'34Lys38-(Aspa—ALit)-GLP—1 (7—
`
`38); SePAspaaArgze~34Lysa9-(Aspa-ALit)-GLP-‘l (7-39);
`
`ThrBGIuasArgZWLysas-(Aspa-ALit)-GLP-1 (7-36);
`
`Th raGlu35Argze'3“Lyssa—(Aspa-ALityGLP-1 (7-
`
`36)amide; ThrBGluasArgz‘3'S4Lysa7-(Aspa-ALit)-GLP-1(7-37); ThraGlu37Argze'3‘Lys38-(Aspa-ALit)-
`
`GLP-1 (7-38); ThrsGlumArgze'S‘Lysa9-(Aspa-ALit)-GLP-1(7-39); ThrBGlu35Ar926-3“Lysas-(Aspa-ALit)-
`
`GLP-1(7-36);
`
`ThPG!U35Ar926'34Lys35—(Aspa-ALit)—GLP-1(7—36)amide;
`
`ThPGIUBGArgZG'MLySW-
`
`10
`
`15
`
`20
`
`25
`
`30
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 104 of 270
`
`

`

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`PCT/DK99/00082
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`103
`
`(Aspa-ALit)-GLP-1(7-37); ThreGlu37Argzs'34Lys3a-(Aspa-ALit)-GLP-1(7-38); ThrBGluasArgzs'uLyssg-
`
`(Aspa-ALit)-GLP-1 (7-39);
`
`ThraAsp35ArgZG'MLysae-(Aspa-ALit)-GLP-1 (7-36);
`
`ThrBAsp35Argza'MLysae-(Aspa-ALit)-GLP-1(7-
`
`36)amide; ThrBAsp36Argze'3“Lys37-(Aspa-ALit)—GLP-1(7-37); ThrBAsp37Argz‘3'3‘Lysae-(Aspa-ALit)-
`
`GLP-1(7—38);
`
`ThrBAspaaArgze-“Lysae-(Aspa-ALit)-GLP-1(7—39);
`
`ThrBAsp35Argzs-34Ly535-(Aspa-
`
`ALit)—GLP-1 (7—36);
`
`Thr5Asp35ArgZS'34Lysae-(Aspa-ALit)-G LP-1 (7—36)amide;
`
`ThrBAspasArgzs'“Lys37~(Aspa-ALit)-GLP-1 (7-37);
`
`ThrBAsp37ArgZG'MLyssa-(Aspa-ALityGLP-1 (7-
`
`38); ThraASpseArgze'MLysgg-(Aspa-ALit)-GLP—1(7-39);
`
`Argze'MLys‘B-(Aspa-ALit)-GLP-1 (7-36);
`
`Argze'“Lys‘8-(Aspa-ALit)-GLP—1 (7—36)amide;
`
`Argzs'a‘Lys‘3—(Aspa—ALit)—GLP—1 (7-37);
`
`Argze'MLys‘B-(Aspa-ALit)-GLP-1 (7-38);
`
`GlyaAsp‘9Argzs'3“Lys18-(Aspa—ALit)-G LP-1 (7-36);
`
`GlysAsp‘7Argzs'34Lys'B-(Aspa-ALit)-GLP-1(7-
`
`36); GIyBAsp‘9Argz‘5'34Lys‘B-(Aspa-ALit)-GLP-1(7-36)amide; GIySAspWArgzs'MLys‘B—(Aspa-ALit)—
`
`GLP-1(7-36)amide;
`
`GlyaAsp‘9Ar926'3“Lys‘”-(Aspa-ALit)-GLP~‘1(7-37);
`
`GlySAsp19Argze'3‘Lys‘8-
`
`(Aspa—ALit)—G LP-1 (7-38); GIysAsp17Argze’34Lys‘8—(Aspa—ALit)-GLP-1 (7-38);
`
`Argzs'“Lysza-(Aspa-ALit)-GLP—1 (7-36);
`
`Argzs'“Lyeza-(Aspa~ALit)-GLP-1 (7-36)amide;
`
`Ar926~34Lys23-(Aspa-ALit)-GLP-1 (7—37);
`
`Arg25'34Ly323-(Aspa—ALit)-GLP—1 (7-38);
`
`GlysAsp‘sArgze'MLysza-(Aspa-ALit)-GLP-1 (7-36);
`
`GlyBAsp17Argzs'3‘Lyszs-(Aspa-ALit)-GLP-1 (7-
`
`36); GIyaAsp‘9ArgZB'MLyszs-(Aspa-ALityGLP—1(7-36)amide; GIyBAsp‘7Argzs-34Ly323-(Aspa-ALit)-
`
`GLP-1(7-36)amide;
`
`GIyaAsp‘9Argze'3“LysZ3-(Aspa-ALit)-GLP—1(7-37);
`
`GIyBAsp19Argzs-34Lyszs-
`
`(Aspa-ALit)-GLP-1 (7-38); GlyBAsp‘7Argze'34Lys”—(Aspa-ALit)—GLP-1 (7-38);
`
`Arg25'3“Ly527-(Aspa-ALit)-G LP-1 (7-36);
`
`Arg26'34Ly527-(Aspa-ALit)-GLP-1(7-36)amide;
`
`Argze'MLysv-(Aspa-ALit)—GLP—‘I (7—37);
`
`ArgZS'S‘LySN-(Aspa-ALit)—GLP-1 (7-38);
`
`GlyaAsp1 9Argz‘i's‘lysw-(Aspa-ALit)-GLP-1 (7-36);
`
`GlyBAsp‘7Argze'34LySZ7—(Aspa-ALit)-G LP-1 (7—
`
`36); GlyeAsp19ArgZS'MLysfl-(Aspa-ALityGLP-1(7-36)amide; GlyaAsp17Argze'34Ly327-(Aspa-ALit)-
`
`GLP-1(7-36)amide;
`
`GIyBAsp19Arg25'34LySZ7-(Aspa-ALit)-GLP-1(7-37);
`
`GlyeAsp‘QArgzs'“Ly527-
`
`(Aspa-ALit)—GLP-1(7—38); Gly"Asp1 7Argze""“‘Lys”-(Aspa-ALit)—G LP—1 (7-38);
`
`ArQZG'MLys‘a-(Aspa-ALit)-GLP-1 (7-36);
`
`Argze-“Lys‘B-(Aspa-ALit)—G LP-1 (7—36)amide;
`
`Argzs'S‘Lys‘B-(Aspa-ALit)-GLP-1 (7-37);
`
`Argzs'MLys‘8-(Aspa-ALit)-GLP-1 (7-38);
`
`Va|aAsp19Argze'34Lys1a-(Aspa-ALit)-GLP-1 (7—36); ValsAspWArgzs'MLys‘8-(Aspa-ALit)—GLP-1(7-36);
`
`ValaAsp‘9Ar926'3‘Lys13-(Aspa-ALit)-GLP-1(7-36)amide; ValsAsp‘7Argzs'34Lys‘B—(Aspa-ALit)-GLP-
`
`1(7-36)amide; ValBAsp‘gArgzs'MLys‘5-(Aspa-ALit)-GLP-1(7-37); ValBAsp‘9Argz‘5'34Lys‘a-(Aspa-
`
`ALit)-GLP-1 (7-38); VaIBAsp‘7Ar926'34Lys‘8-(Aspa-ALit)—GLP-1 (7-38);
`
`Arg26-34Ly323-(Aspa-ALit)-GLP-1 (7-36);
`
`Argzs-“Lysza-(Aspa-ALit)-GLP-1 (7—36)amide;
`
`Argzs'“Lysza-(Aspa-ALit)—GLP-1 (7-37);
`
`Argze'MLysza-(Aspa-ALit)-GLP-1 (7-38);
`
`10
`
`15
`
`20
`
`25
`
`30
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 105 of 270
`
`

`

`WO 99/43706
`
`PCT/DK99/00082
`
`104
`
`VaIaAsp19Argza'3‘Lyszs-(Aspa-ALit)-GLP-1(7-36); VaISAsp‘7Argze'3“Lysza-(Aspa-ALit)-GLP-1 (7-36);
`
`ValaAsp‘9Argze'34LySZ3—(Aspa-ALit)-GLP—1(7—36)amide; ValaAsp‘7Argze'3‘Ly523-(Aspa-ALit)-GLP-
`
`1(7-36)amide; ValaAs'p19Arg26'34Ly323-(Aspa—ALit)-GLP-1(7-37); ValBAsp‘9Argze'3‘Lysza-(Aspa-
`
`ALit)-GLF’-1(7-38); ValsAsp‘7Argzs'3“LysZ3-(Aspa-ALit)-GLP-1 (7-38);
`
`ArgZS'MLysfl-(Aspa-ALit)-GLP-1 (7-36);
`
`ArgZS-“LySZ7-(Aspa-ALit)-GLP-1 (7-36)amide;
`
`Argzs-“LySZ7-(Aspa—ALit)-GLP-1 (7-37);
`
`Ar9265“LysZ7-(Aspa-ALit)-GLP-1 (7-38);
`
`ValsAsp‘9Arg25-3‘Ly327-(Aspa-ALit)-GLP-1 (7-36); VaI8Asp‘7Ar926'34LysZ7-(Aspa-ALit)-GLP-1 (7-36);
`
`VaIBAsp19Argzs'3‘LySZ7-(Aspa-ALit)-GLP-1(7-36)amide; VaIBAsp‘7Argzs'34Ly527-(Aspa-ALit)-GLP-
`
`1(7—36)amide; VaIBAsp19Ar926'3‘Ly827-(Aspa-ALit)—GLP—1(7-37); VaIBAsp'9Argze'34Ly527-(Aspa-
`
`ALit)-GLP-1 (7-38); ValgAsp17Arg26'34Ly527—(Aspa-ALit)-GLP-1 (7-38);
`
`ArgzwLys‘B-(Aspa-ALit)-GLP-1(7-36);
`
`ArgZB'MLys18-(Aspa—ALit)-GLP—1 (7-36)amide;
`
`Argzs‘MLys‘B-(Aspa-ALit)-GLP-1(7-37);
`
`Argzs'MLys‘8-(Aspa-ALit)-GLP-1 (7-38);
`
`SerSAsp‘9Argzfi'34Lys‘8—(Aspa-ALit)-GLP-1 (7-36);
`
`SerBAsp‘7Argzs'34Lys‘8-(Aspa-ALit)-GLP-1 (7-
`
`36); SeraAsp‘9Argze‘34Lys‘8-(Aspa-ALit)-GLP-1(7-36)amide; SerBAsp‘7Argz‘5'3‘Lys‘8-(Aspa—ALit)—
`
`GLP-1(7-36)amide;
`
`SerBAsp‘9Argzs-34Lys‘3-(Aspa-ALit)-GLP-1(7-37);
`
`SeraASp19Argzs'34Lys18-
`
`(Aspa-ALit)-GLP-1 (7-38); SereAsp17Ar926'34Lys‘B—(Aspa-ALit)-GLP-1 (7-38);
`
`Argzs'a“LysZ3-(Aspa-ALit)—GLP-1 (7-36);
`
`Argzsg‘Lyszs-(Aspa-ALit)-GLP-1 (7-36)amide;
`
`Argze'a“Ly523—(Aspa-ALit)-G LP-1 (7-37);
`
`ArgmLysz3-(Aspa-ALit)-GLP-1 (7-33);
`
`SerEAsp19ArgZS'MLysza-(Aspa-ALityGLP-1 (7-36);
`
`SerBAsp‘7Arg26'34Ly323-(Aspa-ALit)-GLP-1 (7—
`
`36); SerBAsp‘9ArgZG'MLysza-(Aspa-ALityGLP-‘l(7-36)amide; SersAsp17Argze'3‘Lys23-(Aspa-ALit)-
`
`GLP~1(7—36)amide;
`
`SeraAsp‘9Argze'3‘Lys”~(Aspa—ALit)-GLP—1(7-37);
`
`SeraAsp‘gArgza'MLysza-
`
`(Aspa—ALit)—GLP—1 (7-38); SerBAsp‘7Argze'34Ly323—(Aspa-ALit)—GLP-1(7-38);
`
`Argze'MLysy-(Aspa-ALit)-GLP-1 (7-36);
`
`Arg26'34Ly527-(Aspa-ALit)-GLP-1 (7-36)amide;
`
`Argze'MLysfl-(Aspa-ALit)-GLP-1 (7-37);
`
`Arg26-“Lysz7-(Aspa-ALit)-GLP-1 (7-38);
`
`SeraAsp‘9Ar9263“LySZ7-(Aspa-ALit)-GLP-1 (7-36);
`
`SerfiAsp17Argzs'34LysZ7-(Aspa-ALit)-GLP-1 (7-
`
`36); SeraAsp‘9Argzs-34Ly327-(Aspa-ALit)-GLP-1(7-36)amide; SeraAsp‘7Argze'34Ly327-(Aspa—ALit)-
`
`GLP-1(7-36)amide;
`
`SeraAsp‘gArgza'MLysm-(Aspa-ALit)-GLP-1(7-37);
`
`SerBAsp‘gArQZG'MLysfl-
`
`(Aspa-ALit)-GLP—1(7-38); SeraAsp‘7ArgZG'MLysfi—(Aspa—ALityGLP-1 (7—38);
`
`Argze'uLys‘8-(Aspa-ALit)—GLP-‘| (7-36);
`
`Argze'“Lys‘“-(Aspa-ALit)-GLP—1(7-36)amide;
`
`Argzs'MLys13-(Aspa-ALit)-GLP-1 (7-37);
`
`Argzs'34Lys1a-(Aspa-ALit)-GLP-1 (7-38);
`
`ThrBAsp‘9Argzs-34Lys15—(Aspa-ALit)-GLP-1 (7-36);
`
`ThrBAsp‘7Argza'34Lys‘B-(Aspa-ALit)-GLP-1 (7-
`
`36); ThraAsp‘9Argze'34Lys‘8-(Aspa-ALit)-GLP-1(7-36)amide; ThrBAsp‘7Argzs'34Lys18—(Aspa-ALit)-
`
`GLP-1(7-36)amide;
`
`ThrBAsp‘9Argze'34Lys‘B-(Aspa-ALit)-GLP-1(7-37);
`
`ThrBAsp19Argzs'34Lys‘8-
`
`(Aspa-ALit)-GLP-1 (7-38); ThrBAsp‘7Argzs'34Lys1B—(Aspa-ALit)-GLP-1 (7-38);
`
`1O
`
`15
`
`20
`
`25
`
`30
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 106 of 270
`
`

`

`WO 99/43706
`
`PCT/DK99/00082
`
`105
`
`Argze'MLysfi-(Aspa—ALit)—GLP—1 (7-36);
`
`ArgZG*“Ly523-(Aspa-ALit)-GLP-1 (7-36)amide;
`
`ArgzaMLysn-(Aspa-ALit)-GLP-1 (7-37);
`
`ArgzevuLysza-(Aspa-ALityGLP-1 (7-38);
`
`Th rBAsp19Arg26'34Lys23-(Aspa-ALit)-GLP-1 (7-36);
`
`ThrBAsp17Argz‘5'3“LysZS-(Aspa-ALit)-GLP-1 (7-
`
`36); ThraAsp‘9Ar925'3‘Ly523-(Aspa-ALit)—GLP-1(7-36)amide; ThrBAsp‘7Arg”'3‘Ly523-(Aspa-ALit)-
`
`GLP—1(7-36)amide;
`
`ThrsAsp‘gArgzs's‘lySB-(Aspa-ALit)-GLP-1(7-37);
`
`ThrBAsp1°Arg25‘34Lys”-
`
`(Aspa-ALit)—GLP-1 (7-38); ThrsAsp17Ar926'34LysZ3—(Aspa-ALit)—GLP-1 (7—38);
`
`Argzs'MLysfl-(Aspa-ALit)-GLP-1 (7-36);
`
`ArgZB'S‘Lysfi-(Aspa-ALit)-GLP-1 (7—36)amide;
`
`Argzs-S“Lysz7-(Aspa-ALit)-GLP-1 (7-37);
`
`ArgZG'MLysfl-(Aspa-ALit)-G LP-1 (7-38);
`
`Thr8Asp‘9Argzs‘34Ly527-(Aspa-ALit)—GLP-1(7—36);
`
`ThrsAsp‘7Argze'3“Ly527-(Aspa-ALit)-GLP-1(7-
`
`36); ThrgAsp‘9Argze'34LysZ7-(Aspa-ALit)-GLP-1(7-36)amide; ThrsAsp‘7Arg26'34Ly527-(Aspa—ALit)-
`
`GLP-1(7-36)amide;
`
`ThrsAsp‘QArgze'MLysfl-(Aspa-ALit)-GLP-1(7—37);
`
`ThrSAsprrgzs'MLysfl-
`
`(Aspa-ALit)-G LP-1 (7-38); ThrBAsp‘7Argze'3“Lys”—(Aspa-ALit)-GLP-1 (7-38);
`
`ArgZGLySM-(Glyc—ADod)-GLP-1(7-36); ArguLyszs—(Glyc-ADodyGLP-1(7—36); Argze's‘Lysae-(Glyc-
`
`ADOd)-GLP-1(7-36); ArgzsLySM-(Glyc—ADod)—GLP-1(7-36)amide; Arg34 Lyszs—(Glyc-ADod)-GLP—
`
`1(7-36)amide; Argze-“Lysae-(Gch-ADod)-GLP-1(7-36)amide; Arg26 Lys“-(Gch-ADod)-GLP-1(7—
`
`37); ArgMLySQG-(GIyC-ADOd)-GLP-1(7-37); Argzs'“Lysse-(Gch—ADod)-GLP—1(7-37); ArgzeLysu-
`
`(Glyc-ADod)—GLP-1(7-38); ArgMLysze-(Glyc-AoodyeLP-1(7-38)
`
`; ArgzwLysss-(Glyc-ADod}
`
`GLP—1(7-38);
`
`ArgzsLys34-(G|yc-ADod)-GLP—1(7-39);
`
`ArgMLySZB-(Glyc-AoodyeLP-1(7-39);
`
`Argzs-“Lys39-(Gch-ADod)-GLP-1(7-39);
`
`GlyBArg25Lys34-(Glyc-ADod)-GLP-1 (7-36);
`
`GIySArgyLysza-(Glyc-ADod)-GLP-1 (7-36);
`
`GIyBArgZG'MLysae—(Giyc-ADodyGLP—1 (7—36);
`
`GlyaArgzeLys“—(G|yc—ADOd)—GLP-1 (7-36)amide;
`
`GlyBArg34Lyszs-(Glyc-ADod)-GLP-1 (7-36)amide;
`
`GlyBArgzs'“Lysafi—(Glyc-ADod)-GLP-1 (7—
`
`36)amide; GlyaArgzsLySM-(G|yc-ADod)-GLP-1(7-37); GlySArQMLyszs-(G|yc-ADod)-GLP-1(7-37);
`
`GIyBArgzs'MLysae-(Gch-ADod)—GLP-1 (7-37);
`
`GlyeArgzsLys“-(Glyc—ADod)-GLP-1 (7-38);
`
`GlysArQMLysze—(Gch—ADod)—GLP-1 (7-38)
`
`;
`
`GIyBArgzs'a“Lys38-(Glyc-ADod)-GLP-1 (7-38);
`
`GIyBArgzsLysu-(G|yc-ADod)-GLP-1 (7-39);
`
`GlySArQMLyszs-(G|yc-ADod)-GLP—1 (7-39);
`
`GIyBArgzs's“Lyssa-(Glyc-ADod)-GLP-1(7-39);
`
`VaIBArgzaLySM-(Gch—ADod)-GLP-1 (7-36);
`
`Va|8Arg34Lys26-(Glyc—ADod)—GLP-1 (7-36);
`
`VaIBArgze-“Lys36-(Gch—ADod)—GLP-1 (7-36);
`
`VaIBArgzsLysy-(G|yc-ADod)-GLP-1 (7-36)amide;
`
`Va|BArguLysze-(Glyc-ADodyGLP-1 (7-36)amide;
`
`VaIBArgze'MLysae-(Glyc-ADod)-GLP-1 (7—
`
`36)amide; ValBArgzeLySM-(Glyc—ADod)—GLP-1(7-37); ValsArQMLyszs-(G|yc-ADod)—GLP-1(7-37);
`
`ValsArgzs'“Lys36-(Gch-ADod)-GLP-1 (7-37);
`
`ValaArgzsLySM-(Gch-ADod)—GLP-1 (7-38);
`
`VaIBArguLyszs-(G|yc—ADod)-GLP-1(7-38)
`
`;
`
`ValBArgze'MLysaa-(Gch-ADod)-GLP-1(7-38);
`
`10
`
`15
`
`20
`
`25
`
`30
`
`M
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 107 of 270
`
`

`

`WO 99/43706
`
`PCT/DK99/00082
`
`106
`
`VaIBArgzsLysu—(G|yc-ADod)-GLP-1(7-39);
`
`ValsArg“Lysze-(Glyc-ADod)-GLP-1(7-39);
`
`VaIBArgzs'MLysag-(Glyc-ADod)-GLP-1 (7-39);
`
`SerBArgzeLysu-(Gch-ADod)-GLP—1 (7—36);
`
`SerBArgMLysze-(Glyc-ADodyGLP-1 (7-36);
`
`SeraArgze'MLysw—(G|yc-ADod)—GLP—1 (7-36);
`
`SeraArgzaLySM-(Gch-ADod)-GLP-1 (7-36)amide;
`
`SeFArQMLysze-(Glyc-ADodyGLP-1 (7—36)amide;
`
`SerBArgzs'MLys36-(Gch—ADod)-GLP-1 (7-
`
`36)amide; SerBArgzeLySM-(Glyc-ADodyGLP-1(7-37); SeraArg“Lyszs—(Glyc-ADod)-GLP-1(7—37);
`
`SeraArgze'MLysas-(Glyc-ADod)-GLP-1 (7-37);
`
`SeraArgzsLysu-(Glyc-ADod)-GLP-1 (7-38);
`
`SerflArQMLyszs—(Glyc-ADod)—GLP-1(7—38)
`
`;
`
`SersArgzs'a“Lys”-(Glyc-ADod)-GLP-1(7-38);
`
`SerBArgzeLySM-(Glyc-ADodyGLP-1 (7-39);
`
`SerBArgyLysze-(Glyc-ADodyGLP—1 (7-39);
`
`SeraArgzs'MLysag-(Gch-ADod)-GLP-1 (7-39);
`
`ThraArgZSLysu-(Glyc-ADodyG LP-1 (7-36);
`
`Th rBArgMLysZG-(Glyc-Aoodye LP—‘I (7-36);
`
`ThraArgZWLysSG-(Gch-ADod)-GLP—1(7—36);
`
`ThrBArgzeLySM—(Glyc-ADod)-GLP-1(7-36)amide;
`
`ThrsArguLysze-(G|yc-ADod)-G LP-1 (7—36)amide;
`
`ThraArgzs'“Lysa‘s—(Glyc-ADod)—GLP-1 (7—
`
`36)amide; ThraArgzeLysm-(Glyc-ADodyGLP-1(7-37); ThrBArgmLyszs-(Glyc-ADodyGLP—1(7—37);
`
`ThraArgza'MLysae-(Gch-ADod)—GLP—1 (7-37);
`
`ThPArgzeLySM-(Glyc-ADodyGLP-1 (7-38);
`
`ThraArguLysze—(Glyc-ADodyGLP-1(7—38)
`
`;
`
`ThrBArgze'MLysaa-(Gch—ADod)-GLP-1(7-38);
`
`ThrsArgzsLysu-(Glyc-ADodyGLP-1 (7-39);
`
`Th PArQMLyszs-(Glyc—ADodyGLP-1 (7-39);
`
`ThrBArgZS-“Lyssg-(Gch-ADod)-GLP-1 (7-39);
`
`GlyBGlU35Argz‘3'34Ly535-(Glyc—ADod)-GLP-1 (7-36);
`
`GlyBG|u35Argzs'34Lysse-(Glyc-ADod)-GLP-1 (7-
`
`36)amide; GIyBGlu3sArgzs'34Lys37-(Glyc—ADod)—GLP—1(7-37); GlysG|u37Argze'34Lysa"-(Glyc—ADod)-
`
`GLP-1(7-38);
`
`GIyBGlusaArgzs-“Lysag-(G|yc-ADod)-GLP-‘I(7—39);
`
`GlyeGlU35Argz‘3'34Ly336—(Glyc-
`
`ADod)—GLP-1(7-36);
`
`GlysGlu35Argze'34Ly536-(Gch-ADod)-GLP-1(7—36)amide;
`
`GIyBGluaeArgze'MLysfl-(Gch-ADod)-GLP-1 (7-37);
`
`GIyBG|u37Argze'34Lys38-(G|yc-ADod)-GLP-1 (7-
`
`38); GIyBGIUSSArgze'MLysw—(Glyc-ADod)-GLP—1(7-39);
`
`GlysAsp35Argzs-34Lysse-(G|yc-ADod)-G LP-1 (7-36); GlyaAspasArgza'MLys36-(Gch—ADod)-GLP-1 (7—
`
`36)amide; GlyBAsp36Arg26'34Ly537-(Glyc-ADod)-GLP-1(7-37); GIyaAsp37Argze'34Lys38-(G|yc-ADod)-
`
`GLP-1(7-38); GlyaAsprrgze'uLysw-(Gch—ADod)-GLP-1(7-39); Gly8Asp35Argzs'34Lysae-(Glyc-
`
`ADod)—GLP—1 (7—36);
`
`GlyaAsp35Argzs'34Lysae-(Gch-ADod)-GLP-1 (7-36)amide;
`
`GIyBAspmArgze'MLysm-(Glyc-ADod)-GLP-1(7-37); GIyBAsp37Argze'3‘Lysae-(Glyc-ADod)-GLP-1(7-
`
`38); GlyaAspuArgzs'MLyssg-(Gch-ADod)-GLP—1(7-39);
`
`ValsGlu35Argzs434Lysae-(G|yc—ADod)-GLP-1 (7-36);
`
`VaIBG|u35Arg26'34Lyssa-(Glyc-ADod)-GLP-1(7-
`
`36)amide; VaIBGluaaArgzwLysm-(G|yc-ADod)-GLP-1(7—37); ValaGlu37Argze-“Lys3a-(Gch-ADod)-
`
`GLP-1(7-38);
`
`ValsGlU38Argza'34Lys39-(Gch—ADod)—GLP-1(7-39);
`
`ValsGlu35Argzs-“Lysss-(Glyc-
`
`ADod)-GLP-1(7-36);
`
`ValaGlussArgze-“Lysas-(G|yc-ADod)-GLP—1 (7-36)amide;
`
`10
`
`15
`
`20
`
`25
`
`30
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 108 of 270
`
`

`

`WO 99/43706
`
`PCT/DK99/00082
`
`107
`
`ValaGIu36Argze'3‘Lyss7-(Glyc-ADod)-GLP-1 (7-37);
`
`ValaGlu37Ar926'34Lys3a-(Glyc-ADod)-GLP-1 (7-
`
`38); ValaGlusaArgzs'“Lys39-(Glyc-ADod)-GLP-1(7-39);
`
`ValaAspasArgzs'MLySSS-(G|yc-ADod)—GLP-1 (7-36); Va|”Asp35ArgZS'MLysw-(Glyc-ADodyGLP-1 (7-
`
`36)amide; VaIBAspaeArgze'“Ly537-(Glyc-ADod)-GLP—1(7-37); Va|8Asp37Argzs'34Lys”-(Gch—ADod)-
`
`GLP—1(7-38); ValsAspssArg26'“Ly539-(Glyc-ADod)-GLP-1(7-39);
`
`ValaAsp35Ar926'34Lys35-(Glyc-
`
`ADod)—GLP-1(7-36);
`
`VaIBAsp35Argze'34Ly336-(Glyc-ADod)—GLP-1 (7-36)amide;
`
`ValeAspasArgzs-“Lysy-(Gch-ADod)-GLP-1 (7-37); Va|8Asp37Argzs'34Lyssa-(G|yc-ADod)-GLP—1 (7-
`
`38); VaIBAspaaArgze-“Lys39-(Gch-ADod)-GLP-1(7-39);
`
`SerBG|u35Argze'3‘LysaS—(Glyc—ADod)-GLP-1 (7—36);
`
`SeraG|U35Argze'34Ly536-(Glyc-ADod)-GLP-1 (7-
`
`36)amide; SerBG|U36Arg25'34Ly337-(Glyc—ADod)—GLP-1(7-37); Ser8G|u37Argzs'34Lys“-(G|yc-ADod)—
`
`GLP—1(7-38);
`
`SereGluaeArgze-“Lyssg-(G|yc-ADod)-GLP-1(7-39);
`
`SeraGlU35Argzs'3‘Lys35-(Glyc-
`
`ADOd)—GLP—1(7-36);
`
`SerBGlussArgza'MLysas-(Glyc-ADod)-GLP-1(7-36)amide;
`
`SereGluaeArgze'MLysy—(Gch—ADod)-GLP-1 (7—37);
`
`SerBG|u37Argze'3‘Lysaa-(Glyc—ADod)-GLP-1 (7-
`
`38); SeraG|u38Argz‘5'34Lysag-(Gch—ADod)—GLP-1(7-39);
`
`SersAspasArgzs'MLysae-(Glyc-ADod)—GLP-1 (7-36); SerBAspasArgze'MLysae-(Gch—ADod)-GLP—1 (7-
`
`36)amide;
`
`Ser8Asp36Argza'3“Ly537-(Glyc-ADod)-GLP-1(7-37);
`
`SeI‘Asp37Argzs'34Lysaa-(Glyc-
`
`ADod)-GLP-1(7-38);
`
`SerBAspuArgza'uLysag—(Gch-ADod)-GLP—1(7—39); SeraASpasArgzs'uLysss-
`
`(Glyc—ADod)—GLP—1(7—36);
`
`SergAsp35Argzs'34Lys35-(Glyc-ADod)-G LP-1 (7-36)amide;
`
`Ser‘AspaaArgzs'MLysw-(G|yc-ADod)-GLP-1 (7-37); SerBAsp37Argze'34Ly838—(G|yc-ADod)-GLP-1 (7-
`
`38); SeraAspasArgze'MLysag-(G|yc—ADod)-GLP-1(7-39);
`
`Th FGluasArgze'“Lys3G-(Gch-ADod)—GLP-1 (7-36);
`
`ThraGlu3sArgzs'34Lys35-(Gch—ADod)—GLP—1 (7-
`
`36)amide; ThraGlusBArg26*“Lys37-(Glyc-ADod)-GLP-1(7-37); ThrEGlu37Argze'34Lysas-(Gch—ADod)—
`
`GLP-1(7-38);
`
`ThrBG|uwArQZG'MLysa9-(G|yc—ADod)-GLP-1(7-39);
`
`ThPGlufiArgze'MLysw-(Glyc-
`
`ADod)-G LP-1 (7-36);
`
`Th raGIuasArgzs'MLysae—(Glyc-ADod)-G LP-1 (7-36)amide;
`
`ThrBGluasArgzs'MLysw-(G|yc-ADod)-GLP-1 (7—37);
`
`Thr8G|u37Argzs'34Lyssa-(Gch—ADod)—GLP-1 (7—
`
`38); ThraG|uaaArgze-“Lysae-(Gch-ADod)-GLP-1(7-39);
`
`10
`
`15
`
`20
`
`25
`
`ThraAsp3sArgzs’34Lysae-(Glyc-ADod)-GLP-1 (7-36); ThFAspasArgze'MLysse-(G|yc-ADod)-GLP-1(7-
`
`36)amide; ThrBAsp3’3Argzs’3“Lys37-(Glyc—ADod)-GLP-1(7-37); ThraAsp37Argze'34Lys38-(Glyc—ADod)—
`
`GLP-1(7-38);
`
`ThraAspasArgze'MLysw-(Glyc-ADod)-GLP-1(7-39);
`
`ThrBAspasArgze'MLysas-(Glyc-
`
`30
`
`ADod)-GLP-1(7-36);
`
`ThrSAspssArgzs-“Lysas-(Gch-ADod)-GLP-1 (7-36)amide;
`
`ThraAspaeArgzs'a‘Lysa7-(Glyc—ADod)-GLP~1 (7-37); ThrBAsp37Argzs'34Lysas—(Glyc-ADod)-GLP-1 (7—
`
`38); Thr’sAsp38Argzs-34Lys39-(Glyc—ADod)—GLP-1(7-39);
`
`Argzs'MLys‘5-(Gch-ADod)-G LP-1 (7-36);
`
`Argze-MLySW-(GIyoADod)-GLP-1 (7-36)amide:
`
`Argzs'uLys‘B-(G|yc~ADod)—GLP-1(7—37);
`
`Argzs'MLys‘a—(Glyc—ADod)-GLP—1(7-38);
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 109 of 270
`
`

`

`WO 99/43706
`
`PCT/DK99/00082
`
`108
`
`GIyBAsp‘9Argzs'3‘Lys18—(Glyc—ADod)—GLP-1 (7-36); GIyBAsp17Argze'3‘Lys‘8-(Glyc-ADod)-GLP-1 (7-
`
`36); GlyBAsp‘gArgze'MLys‘B-(Gch-ADod)-GLP-1(7-36)amide; GIysAsp17Argze'34Lys1B—(G|yc-ADod)-
`
`GLP-1(7-36)amide; GlySAsp‘9Argzs'3“Lys‘B-(Glyc-ADod)-GLP-1(7-37); GlyaAsp‘gArgze'uLys‘B-
`
`(Gch—ADod)—GLP-1 (7~38); GlyBAspnArgze'a“Lys‘a-(G|yc-ADod)-GLP-1(7-38);
`
`Argzs'MLysza—(Glyc—ADod)—GLP-1 (7—36);
`
`Argze'S‘Lysza-(Glyc—ADod)-GLP-1 (7-36)amide;
`
`Argze'“Lys”—(G|yc—ADOd)-GLP-‘l (7-37);
`
`Argzs'MLysza-(Glyc~ADod)-GLP—1 (7-38);
`
`GlysAsp‘gArg26-34Ly323-(Glyc-ADod)-GLP—1 (7-36); GIyBAsp‘7Argzs'34Lysza-(Gch-ADod)—GLP-1 (7-
`
`36); GlyBAsp‘gArgz‘s'“Lys”-(G|yc-ADod)—GLP-1(7-36)amide; GlyBAsp‘7Argze'34Ly523-(Glyc-ADod)-
`
`GLP-1(7-36)amide; GlysAsp‘gArgzs'MLysza-(Gch—ADod)-GLP-1(7—37); GlyaAsp‘gArgze'“Lysza-
`
`(GIyC-ADod)—GLP-1 (7-38); GlyBAsp‘7Argzs'3‘Ly523-(Gch-ADod)-GLP-1 (7-38)‘,
`
`Arg26~34Lysz7—(Glyc-ADod)-G LP-1 (7-36);
`
`ArgZB'MLysfl-(Gch—ADod)-GLP-1 (7-36)amide;
`
`ArgZG'MLysfi—(Glyc—ADod)—GLP—1(7-37);
`
`Argza'a“LysZ7-(Glyc-ADod)-GLP-1(7-38);
`
`GlysAsp19Argze-“LySZ7-(Glyc-ADod)-GLP-1(7-36); GlyBAsp17Argze'34LySZ7—(Glyc-ADod)-GLP—1 (7—
`
`36); GIyBAsp19Argzs'3“LysZ7-(Glyc-ADod)-GLP-1(7-36)amide; GlysAsp‘7Argza'3“LysZ7-(Glyc-ADod)-
`
`GLP-1(7-36)amide; GIyBAsp‘9Argzs'3‘Lysz7-(Gch-ADod)-GLP-1(7-37);
`
`GIyBAsp19Argzs'34LySZ7-
`
`(Glyc—ADod)-GLP-1(7-38); GIyBAsp17Arg26-34Lys27—(Gch-ADod)—GLP-1(7-38);
`
`Argzs'MLys‘8-(Glyc-ADod)-GLP-1(7-36);
`
`Argzs‘MLys‘8-(Glyc-ADod)-GLP-1(7-36)amide;
`
`Argzs'MLys‘a-(Gch-ADod)-GLP-1(7-37);
`
`Argze'34Lys‘8-(Glyc-ADod)—GLP-1(7-38);
`
`VaIBAsp‘gArgzs'MLys‘a-(Gch—ADod)-GLP-1 (7-36); ValaAsp17Argze'3‘Lys‘8-(G|yc-ADod)-GLP-1 (7-
`
`36); ValBAsp‘9Ar926'34Lys18—(Glyc-ADod)-GLP—1(7-36)amide; VaIBAsp‘7Argzs'34Lys‘8-(G|yc-ADod)-
`
`GLP—1(7-36)amide; ValaAsp‘9Argze'34Lys18-(Glyc-ADod)-GLP-1(7—37);
`
`VaIBAsp‘9Argzs'3‘Lys‘8-
`
`(Gch-ADod)-GLP-1 (7-38); ValaAsp17Argzs'34Lys1a-(Gch-ADod)-GLP-1 (7-38);
`
`Argze'MLyszs-(Gch-ADod)-GLP-1 (7-36);
`
`ArgZG-“Ly523-(Glyc-ADod)-G LP-1 (7-36)amide;
`
`Argze'MLyszs—(Gch-ADod)-GLP-1(7—37);
`
`ArgZG'MLysn—(Gch—ADod)—GLP-1(7-38);
`
`ValaAsp19Argze'34Lysza-(Gch—ADod)—GLP-1 (7-36); VaIBAsp17Argzs'34Lysza—(Glyc-ADod)-GLP-1(7-
`
`36); VaIBAsp‘g’ArgZG'MLysm-(Gch-ADod)-GLP-1(7-36)amide; ValBAsp‘7Argze-34Lysz3-(G|yc-ADod)-
`
`GLP-1(7—36)amide; VaIBAsp19Ar926'34Ly523-(Gch—ADod)-GLP-1(7-37);
`
`VaIBAsp‘gArgzs-“Lysza-
`
`(Glyc-ADod)-GLP-1(7-38); ValsAsp17Ar926-3“Lysza-(Glyc-ADod)-GLP-1(7-38);
`
`Argzs'MLysfl-(GIyc—ADod)-G LP-1 (7-36);
`
`Argze'MLysn-(Glyc-ADod)-GLP-1 (7-36)amide;
`
`Argzs'MLysfl-(Gch-ADod)—GLP-1(7-37);
`
`Argze'MLysfl-(Gch-ADod)-GLP-1(7-38);
`
`VaIBAsp‘9Arg25'34Ly527-(Glyc-ADod)-GLP-1(7-36); ValsAsp‘7Argzs'34LySZ7-(Glyc-ADod)-GLP-1(7-
`
`36); VaIBAsp19Ar926'3‘Ly527-(Gch-ADod)-GLP-1(7-36)amide; VaIBASp17AI'926‘34LySZ7-(Gch-ADOd)-
`
`GLP-1(7-36)amide; ValaAsp‘gArgzs'MLysfl-(Glyc—ADod)-GLP—1(7-37);
`
`VaIBAsp19Argze'3‘Ly527-
`
`(Glyc—ADod)—GLP-1(7-38); ValsAspnArgZB-“Lysm-(G|yc-ADod)—GLP—1 (7—38);
`
`10
`
`15
`
`20
`
`25
`
`30
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 110 of 270
`
`

`

`WO 99/43706
`
`PCT/DK99/00082
`
`109
`
`Argzs-“Lysw-(Gch-ADod)-GLP-1 (7-36);
`
`ArgZWLys‘a-(Gch-ADod)-G LP-1 (7—36)amide;
`
`Argzs'a‘Lys‘a-(Glyc-ADod)-GLP-1 (7-37);
`
`Argzs'MLys‘8-(Glyc-ADod)-GLP-1 (7—38);
`
`SerBAsp19Argza'MLys‘5-(Glyc-ADod)-GLP-1 (7-36); SePAsp17Argzs-“Lys‘8-(Gch-ADod)-GLP-1 (7-
`
`36);
`
`SerBAsp‘gArgzs'“Lys‘”-(Gch-ADod)-GLP-1(7-36)amide;
`
`SeraAsp'7Argze'3‘Lys‘5-(Glyc-
`
`ADod)-GLP-1 (7-36)amide;
`
`SeraAsp‘9Argz‘5'3“Lys‘B-(Glyc-ADod)-GLP-1 (7-37);
`
`SeraAsp‘9Argzs'34Lys‘B—(Gch-ADod)-GLP-1 (7-38); SeraAspWArgzs'MLys‘s-(Gch-ADod)-GLP-1(7—
`
`38);
`
`ArgZS-“Lysza-(Gch-ADod)-GLP-1 (7-36);
`
`ArgZWLyszs-(Gch-ADod)-GLP-1 (7-36)amide;
`
`ArgZS'MLyszs-(G|yc-ADod)—GLP-1 (7-37);
`
`Argze'“Lysza-(Gch-ADod)-GLP—1 (7-38);
`
`SeraAsp‘gArgzemeysza-(Glyc-ADod)—GLP-1 (7-36); SeraAsp17Argze‘34Ly523-(Gch—ADod)-GLP-1 (7-
`
`36);
`
`SerfiAsprrgze'MLysn—(G|yc-ADod)—GLP-1(7—36)amide;
`
`SerflAsp‘7Argze‘34Ly523-(Glyc-
`
`ADod)—GLP-1(7—36)amide;
`
`Ser8Asp‘9Argza'34Lysz3-(G|yc-ADod)—GLP-1 (7-37);
`
`SersAsp‘gArgzs'MLySZ3-(G|yc-ADod)-GLP—1 (7-38); SerJaAsp1 7Argz‘5'34Lyszs-(G|yc-ADod)—GLP-1 (7—
`
`38);
`
`Argze'MLysfl—(Glyc—ADod)—GLP—1 (7—36);
`
`Argze'a‘Lysfl-(Glyc-ADod)-GLP-1 (7-36)amide;
`
`Argzs'MLysm—(Glyc-ADod)-GLP-1 (7-37);
`
`ArgZS'S‘Lysfl-(G|yc~ADod)—GLP-1 (7-38);
`
`SerBAsp‘9Argze-34Ly327-(Glyc-ADod)-GLP-1 (7-36); SerBAsp‘7Argzs'34LySZ7-(Gch—ADod)—GLP-1 (7—
`
`36);
`
`SeraAsp‘9Ar925-34Ly527-(Glyc-ADod)-GLP-1(7-36)amide;
`
`SereAsp‘7Argzs'34Ly527-(Glyc-
`
`ADod)—GLP—1(7-36)amide;
`
`SersAsp‘9Argzs'3‘LySZ7-(Gch-ADod)-GLP-1(7-37);
`
`SerBAsp‘gArgzs'uLysy—(Glyc—ADod)-GLP-1 (7-38); SerBAsp‘7Argzs'34Ly527-(Gch-ADod)-GLP-1(7-
`
`38);
`
`Argze'MLys‘5-(Glyc-ADod)-GLP-1(7-36);
`
`ArgZG’MLys‘s-(Glyc—ADod)-GLP—1(7-36)amide;
`
`Argzs'“Lys‘a-(Glyc-ADod)-GLP-1 (7-37);
`
`Argze'MLys‘B-(Glyc-ADod)-GLP-1(7-38);
`
`ThraAsprrgZG-“Lys‘a—(Gch—ADod)-GLP-1 (7-36); ThrsAsp17Argzs'34Lys1a—(Gch-ADod)-GLP-1 (7-
`
`36); ThrBAsp‘9Argze-34Lys18—(Gch-ADod)-GLP-1(7-36)amide; ThrBAsp17Argzs'34Lys‘B-(Gch-ADod)-
`
`GLP-1(7-36)amide;
`
`ThraAsp‘QArgzs'MLys‘B-(Glyc-ADod)-GLP-1(7-37);
`
`ThrBAsp19Argzs'34Lys‘8-
`
`(Gch-ADod)—GLP-1 (7—38); ThrBAsp‘7Argzs'34Lys18—(Gch-ADod)—GLP-1(7-38);
`
`Arg25-34Ly523-(Glyc-ADod)-GLP-1 (7-36);
`
`Argzs-“Lysm-(Glyc-ADod)-GLP-1 (7-36)amide;
`
`Argm“Lysza-(Glyc-ADod)-GLP-1 (7-37);
`
`Argzs'a‘Lysza-(Gch-ADod)-GLP-1 (7-38);
`
`ThraAsp‘QArgze'MLySZ3—(Glyc-ADod)—GLP-1 (7-36); ThrsAsp‘7Ar926’34Ly523—(Glyc-ADod)-G LP—1 (7-
`
`36); ThreAsp19ArgZS'MLysza-(Glyc-ADodyGLP-1(7-36)amide; ThrBAsp‘7Arg25-34Ly523-(Glyc-ADod)-
`
`GLP—1(7-36)amide;
`
`Thr8Asp19Argzs-3“Lys”-(G|yc-AD0d)-GLP-1(7-37);
`
`ThrBAsp‘gArgze'MLysza-
`
`(Gch-ADod)-GLP-1 (7-38); ThrBAsp‘7Argze'34Lysza-(Glyc-ADod)-GLP-1 (7-38);
`
`10
`
`15
`
`20
`
`25
`
`30
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 111 of 270
`
`

`

`WO 99/43706
`
`PCT/DK99/00082
`
`110
`
`Argzs'a“LysZ7-(Glyc-ADod)—GLP—1 (7-36);
`
`Argzs'MLysm-(Glyc-ADod)-GLP-1 (7-36)amid_e;
`
`Argzs's‘Lysfl-(Glyc—ADod)-GLP-1 (7-37);
`
`ArgZG'MLysfl-(Gch-ADod)—GLP-1 (7-38);
`
`ThrsAsp‘9Argzs'34LySZ7-(G|yc-ADod)—GLP-1 (7-36); ThraAsp‘7Ar925'3‘Ly527—(Glyc-