throbber
WO 99/43706
`
`PCT/DK99/00082
`
`99
`
`Arg”*™“Lys'*-(Aspa-AOct)-GLP-1(7-36)amide;
`Arg”*™Lys"®-(Aspa-AOct)-GLP-1 (7-36);
`Arg?®*Lys'®-(Aspa-AOct)-GLP-1(7-38);
`Arg?**4Lys'®-(Aspa-AOct)-GLP-1 (7-37):
`Val’Asp"Arg”™Lys"*-(Aspa-AOct)-GLP-1(7-36); Val®Asp'’Arg”**Lys"*-(Aspa-AOct)-GLP-1(7-
`36); ValAsp"Arg”*Lys"®-(Aspa-AOct)-GLP-1(7-36)amide; Val’Asp'’Arg”™Lys*-(Aspa-AOct)-
`GLP-1(7-36)amide; Val®Asp"*Arg’**“Lys"*-(Aspa-AOct)-GLP-1(7-37),_Val’Asp*Arg”*“Lys’*-
`(Aspa-AOct)-GLP-1 (7-38); Val’Asp'’Arg*™Lys'®-(Aspa-AOct)-GLP-1 (7-38);
`Arg”**_ys**-(Aspa-AOct)-GLP-1 (7-36);
`Arg”*™“Lys**-(Aspa-AOct)-GLP-1(7-36)amide;
`Arg”**Lys**-(Aspa-AOct)-GLP-1 (7-37);
`Arg®™Lys**-(Aspa-AOct)-GLP-1 (7-38);
`Val’Asp**Arg*™Lys”*-(Aspa-AOct)-GLP-1(7-36); Val’Asp"Arg”*Lys”°-(Aspa-AOct)-GLP-1(7-
`36); Val’Asp*Arg””™Lys”*-(Aspa-AOct)-GLP-1(7-36)amide; Val’Asp"’Arg”™Lys”-(Aspa-AOct)-
`GLP-1(7-36)amide; Val®Asp“*Arg*®*Lys”*-(Aspa-AOct)-GLP-1(7-37), Val’Asp'*Arg”*Lys”°-
`(Aspa-AOct)-GLP-1(7-38); Val’Asp"’Arg**™“Lys”-(Aspa-AOct)-GLP-1 (7-38);
`Arg”*™“Lys”’-(Aspa-AOct)-GLP-1 (7-36);
`Arg”*Lys*’-(Aspa-AOct)-GLP-1(7-36)amide;
`Arg”*™Lys”’-(Aspa-AOct)-GLP-1 (7-37);
`Arg”®*Lys?’-(Aspa-AOct)-GLP-1 (7-38);
`Val’Asp®Arg**“Lys*”-(Aspa-AOct)-GLP-1(7-36);
` Val’Asp"’Arg?*“Lys?’-(Aspa-AOct)-GLP-1(7-
`36); Val’Asp'*Arg**“Lys*’-(Aspa-AOct)-GLP-1(7-36)amide; Val’Asp"’Arg*™Lys”’-(Aspa-AOct)-
`GLP-1(7-36)amide; Val°Asp**Arg”®™Lys”’-(Aspa-AOct)-GLP-1(7-37);
` Val’Asp"*Arg”*™“Lys?”-
`(Aspa-AOct)-GLP-1(7-38); Val’Asp"Arg**™Lys?’-(Aspa-AOct)-GLP-1 (7-38);
`Arg”*™“Lys"®-(Aspa-AOct)-GLP-1(7-36);
`Arg®™Lys'®-(Aspa-AOct)-GLP-1(7-36)amide;
`Arg”*™Lys"*-(Aspa-AOct)-GLP-1 (7-37);
`Arg”**Lys'*-(Aspa-AOct)-GLP-1 (7-38);
`Ser’Asp"*Arg”™Lys"*-(Aspa-AOct)-GLP-1(7-36); Ser’Asp’Arg”*“Lys'®-(Aspa-AOct)-GLP-1(7-
`36);
`Ser’Asp'*Arg”**“Lys'*-(Aspa-AOct)-GLP-1(7-36)amide;
` Ser®*Asp*’Arg”*™“Lys"®-(Aspa-
`AOct)-GLP-1(7-36)amide;
`Ser’Asp*Arg”*™Lys'®-(Aspa-AOct)-GLP-1 (7-37);
`Ser*Asp'*Arg”*™Lys'*-(Aspa-AOct)-GLP-1(7-38); Ser®Asp"7Arg*“Lys"*-(Aspa-AOct)-GLP-1(7-
`
`20
`
`25
`
`30
`
`38);
`Arg”®**Lys?*-(Aspa-AOct)-GLP-1(7-36)amide;
`Arg”**“Lys”*.(Aspa-AOct)-GLP-1 (7-36);
`Arg”**Lys*-(Aspa-AOct)-GLP-1 (7-38);
`Arg”*“Lys**-(Aspa-AOct)-GLP-1 (7-37);
`SerAsp*Arg”™Lys*-(Aspa-AOct)-GLP-1(7-36); SerAsp"Arg”“Lys”*-(Aspa-AOct)-GLP-1(7-
`36);
`Ser’Asp'°Arg**“Lys*-(Aspa-AOct)-GLP-1(7-36)amide;
` Ser’Asp'’Arg**™Lys”*-(Aspa-
`
`SerAsp*Arg”***Lys”-(Aspa-AOct)-GLP-1 (7-37);
`AOct)-GLP-1(7-36)amide;
`SerAspArg”®™Lys”*-(Aspa-AOct)-GLP-1 (7-38); SerAsp"”Arg®“Lys”-(Aspa-AOct)-GLP-1(7-
`38);
`Arg”**“Lys?’-(Aspa-AOct)-GLP-1 (7-36):
`Arg”*“Lys”’-(Aspa-AOct)-GLP-1(7-37);
`
`Arg”®™Lys??-(Aspa-AOct)-GLP-1(7-36)amide;
`Arg”*™“Lys?’-(Aspa-AOct)-GLP-1 (7-38);
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 101 of 270
`
`

`

`WO 99/43706
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`PCT/DK99/00082
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`100
`
`SerAspArg™Lys’-(Aspa-AOct)-GLP-1(7-36); Ser’Asp'’Arg**“Lys”’-(Aspa-AOct)-GLP-1(7-
`36);
` SerAsp'*Arg”*™“Lys”’-(Aspa-AOct)-GLP-1(7-36)amide;
` Ser®Asp'’Arg”®™Lys”’-(Aspa-
`AOct)-GLP-1(7-36)amide;
`SerAsp*Arg”™Lys””-(Aspa-AOct)-GLP-1(7-37);
`Ser’Asp*Arg**Lys?’-(Aspa-AOct)-GLP-1(7-38); Ser’Asp'’Arg**™“Lys”’-(Aspa-AOct)-GLP-1(7-
`
`38);
`Arg”***Lys'®-(Aspa-AOct)-GLP-1(7-36)amide;
`Arg”™Lys'*-(Aspa-AOct)-GLP-1 (7-36);
`Arg*™Lys"*-(Aspa-AOct)-GLP-1(7-38);
`Arg”**Lys"®-(Aspa-AOct)-GLP-1 (7-37);
`ThreAsp"*Arg™Lys'®-(Aspa-AOct)-GLP-1(7-36); ThrAsp'’Arg”™“Lys"-(Aspa-AOct)-GLP-1(7-
`36); ThrAsp*Arg”*™Lys"*-(Aspa-AOct)-GLP-1(7-36)amide; Thr’Asp'’Arg**“Lys'*-(Aspa-AOct)-
`GLP-1(7-36)amide;
`Thr’Asp'*Arg”““Lys'®-(Aspa-AOct)-GLP-1(7-37);
`ThrAsp"*Arg™“Lys"®-
`(Aspa-AOct)-GLP-1 (7-38); Thr’Asp"Arg**“Lys"*-(Aspa-AOct)-GLP-1 (7-38);
`
`Arg*™Lys”*-(Aspa-AOct)-GLP-1 (7-36):
`
`Arg***Lys”-(Aspa-AOct)-GLP-1 (7-36)amide;
`
`Arg®*™Lys**-(Aspa-AOct)-GLP-1(7-38);
`Arg”’Lys”°-(Aspa-AOct)-GLP-1 (7-37);
`ThrAsp*Arg”*™“Lys*-(Aspa-AOct)-GLP-1(7-36); ThrAsp’’Arg”™“Lys*-(Aspa-AOct)-GLP-1(7-
`36); Thr’Asp"*Arg***Lys*-(Aspa-AOct)-GLP-1(7-36)amide; Thr’Asp'’Arg”*™“Lys”*-(Aspa-AOct)-
`GLP-1(7-36)amide; ThréAsp'*Arg”*™Lys*-(Aspa-AOct)-GLP-1(7-37);
` Thr’Asp"’Arg”*™“Lys*-
`(Aspa-AOct)-GLP-1 (7-38); Thr’Asp"Arg?*“Lys®-(Aspa-AOct)-GLP-1 (7-38):
`Arg”®**“Lys”’-(Aspa-AOct)-GLP-1 (7-36);
`Arg’*Lys*”-(Aspa-AOct)-GLP-1(7-36)amide;
`Arg”®*™Lys?’-(Aspa-AOct)-GLP-1 (7-37);
`Arg”®™Lys?’-(Aspa-AOct)-GLP-1(7-38);
`
`ThrAsp"Arg?*™Lys?”-(Aspa-AOct)-GLP-1(7-36);
` ThrAsp'”Arg?*Lys?”-(Aspa-AOct)-GLP-1(7-
`36); Thr’Asp"*Arg**™Lys?’-(Aspa-AOct)-GLP-1(7-36)amide; ThrAsp'’Arg”*™Lys?’-(Aspa-AOct)-
`GLP-1(7-36)amide;
`Thr°Asp'°Arg’®*“Lys?’-(Aspa-AOct)-GLP-1(7-37);
` ThrAsp*Arg”*™Lys?’-
`(Aspa-AOct)-GLP-1 (7-38); Thr’Asp'’Arg”™Lys?”-(Aspa-AOct)-GLP-1 (7-38);
`Arg*Lys™-(Aspa-ALit)-GLP-1(7-36); Arg™Lys?°-(Aspa-ALit)-GLP-1(7-36); Arg’®*Lys*®-(Aspa-
`ALit)-GLP-1(7-36); Arg*Lys™-(Aspa-ALit)-GLP-1(7-36)amide; Arg™ Lys”*-(Aspa-ALit)-GLP-1(7-
`36)amide; Arg***“Lys**-(Aspa-ALit)-GLP-1(7-36)amide; Arg” Lys*-(Aspa-ALit)-GLP-1 (7-37).
`Arg™Lys”**-(Aspa-ALit)-GLP-1(7-37); Arg?®“Lys*®-(Aspa-ALit)-GLP-1(7-37); Arg*Lys*-(Aspa-
`ALit)-GLP-1(7-38); Arg“Lys”-(Aspa-ALit)-GLP-1(7-38) ; Arg®Lys®°-(Aspa-ALit)-GLP-1(7-38):
`Arg”*Lys™-(Aspa-ALit)-GLP-1(7-39); Arg™Lys”®-(Aspa-ALit)-GLP-1(7-39); Arg”***Lys**-(Aspa-
`
`ALit)-GLP-1(7-39):
`Gly*’Arg™Lys”°-(Aspa-ALit)-GLP-1 (7-36);
`Gly°Arg“Lys*-(Aspa-ALit)-GLP-1(7-36);
`Gly*Arg#*Lys™-(Aspa-ALit)-GLP-1(7-36)amide;
`Gly*Arg”*™“Lys**-(Aspa-ALit)-GLP-1 (7-36);
`Gly®Arg***Lys**-(Aspa-ALit)-GLP-1(7-
`Gly®Arg™Lys”*-(Aspa-ALit)-GLP-1(7-36)amide;
`36)amide; Gly*°Arg”Lys*-(Aspa-ALit)-GLP-1(7-37); Gly’Arg™Lys”°-(Aspa-ALit)-GLP-1 (7-37);
`
`15
`
`20
`
`25
`
`30
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 102 of 270
`
`

`

`WO 99/43706
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`PCT/DK99/00082
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`101
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`Gly*Arg”*Lys*-(Aspa-ALit)-GLP-1 (7-38);
`Gly*Arg?®“Lys®-(Aspa-ALit)-GLP-1 (7-38);
`Gly’Arg*Lys”°-(Aspa-ALit)-GLP-1 (7-39);
`
`Gly*Arg***Lys**-(Aspa-ALit)-GLP-1 (7-37);
`Gly*Arg*Lys**-(Aspa-ALit)-GLP-1(7-38)
`Gly*Arg”Lys™-(Aspa-ALit)-GLP-1(7-39);
`Gly*Arg?™“Lys®-(Aspa-ALit}-GLP-1(7-39);
`ValArg*Lys*-(Aspa-ALit)-GLP-1(7-36);
`Val’Arg”®™Lys**-(Aspa-ALit)-GLP-1 (7-36);
`Val’Arg™Lys”-(Aspa-ALit)-GLP-1(7-36)amide;
`36)amide; Val’Arg*Lys™-(Aspa-ALit)-GLP-1(7-37);
`Val’Arg?™Lys**-(Aspa-ALit)-GLP-1 (7-37);
`Val’Arg™Lys”*-(Aspa-ALit)-GLP-1 (7-38)
`Val’Arg”Lys*-(Aspa-ALit)-GLP-1 (7-39);
`Val’Arg”™Lys**-(Aspa-ALit)-GLP-1(7-39);
`Ser’Arg”Lys*-(Aspa-ALit)-GLP-1(7-36):
`SerArg”*™Lys*®-(Aspa-ALit)-GLP-1 (7-36);
`Ser®Arg™Lys”°-(Aspa-ALit)-GLP-1(7-36)amide;
`36)amide;
`Ser®Arg**Lys*-(Aspa-ALit)-GLP-1(7-37);
`Ser’Arg”*™Lys*®-(Aspa-ALit)-GLP-1 (7-37),
`
`Val’Arg™Lys”°-(Aspa-ALit)-GLP-1 (7-36);
`Val’Arg*Lys*-(Aspa-ALit)-GLP-1 (7-36)amide;
`Val’Arg*™Lys**-(Aspa-ALit)-GLP-1(7-
` Val’Arg™Lys”-(Aspa-ALit)-GLP-1 (7-37);
`Val’Arg*Lys*-(Aspa-ALit)-GLP-1 (7-38);
`Val’Arg?*4Lys®*-(Aspa-ALit}-GLP-1 (7-38);
`ValArg™Lys”*-(Aspa-ALit)-GLP-1 (7-39);
`
`;
`
`Ser’Arg™Lys*-(Aspa-ALit)-GLP-1(7-36):
`SerArg*Lys™-(Aspa-ALit)-GLP-1 (7-36)amide;
`SerArg”™Lys*°-(Aspa-ALit)-GLP-1(7-
`Ser’Arg™“Lys”-(Aspa-ALit)-GLP-1(7-37);
`SerArg”*Lys™-(Aspa-ALit)-GLP-1 (7-38);
`
`SerArg”™Lys*-(Aspa-ALit)-GLP-1 (7-38);
`Ser’Arg™Lys”-(Aspa-ALit)-GLP-1 (7-39);
`
`:
`
`.
`
`SerArg™Lys”*-(Aspa-ALit)-GLP-1(7-38)
`Ser®Arg”*Lys™-(Aspa-ALit)-GLP-1(7-39);
`Ser’Arg”™Lys*°-(Aspa-ALit)-GLP-1 (7-39);
`ThrArg*Lys*-(Aspa-ALit)-GLP-1 (7-36);
`ThrArg™Lys”°-(Aspa-ALit)-GLP-1 (7-36);
`ThrArg**Lys**-(Aspa-ALit)-GLP-1 (7-36);
`ThrArg“Lys™-(Aspa-ALit)~-GLP-1(7-36)amide;
`ThrArg™Lys”-(Aspa-ALit)-GLP-1(7-36)amide:;
`ThrArg™Lys®-(Aspa-ALit)-GLP-1(7-
`36)amide; Thr’Arg”Lys*-(Aspa-ALit)-GLP-1(7-37); Thr°Arg™Lys”°-(Aspa-ALit)-GLP-1 (7-37);
`Thr’Arg*™Lys**-(Aspa-ALit)-GLP-1 (7-37);
`ThrArg*Lys*-(Aspa-ALit)-GLP-1 (7-38);
`ThrArg™Lys*-(Aspa-ALit)-GLP-1(7-38)
`ThreArg?™Lys*®-(Aspa-ALit)-GLP-1(7-38);
`ThrArg*Lys*-(Aspa-ALit)-GLP-1 (7-39);
`ThrArg™Lys”*-(Aspa-ALit)-GLP-1 (7-39);
`ThrArg®™“Lys**-(Aspa-ALit)-GLP-1 (7-39);
`Gly®Glu*Arg**“Lys**-(Aspa-ALit)-GLP-1 (7-
`Gly®Glu*Arg”™Lys**-(Aspa-ALit)-GLP-1 (7-36);
`36)amide; Gly*®Glu**Arg”“Lys*”-(Aspa-ALit)-GLP-1(7-37); Gly®Glu*’Arg”Lys*-(Aspa-ALit)-
`GLP-1(7-38); Gly®Glu®*Arg**“Lys**-(Aspa-ALit)-GLP-1(7-39); Gly®Glu*Arg*™“Lys**-(Aspa-ALit)-
`GLP-1(7-36);
` Gly®Glu®=Arg**“Lys*°-(Aspa-ALit)-GLP-1(7-36)amide;
` Gly®Glu**Arg”**“Lys®”-
`(Aspa-ALit)-GLP-1 (7-37); Gly®’Glu*”Arg”*“Lys**-(Aspa-ALit)-GLP-1 (7-38); Gly®Glu*Arg*™Lys**-
`
`(Aspa-ALit)-GLP-1 (7-39);
`
`15
`
`20
`
`25
`
`30
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 103 of 270
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`

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`PCT/DK99/00082
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`102
`
` Gly’Asp**Arg?*Lys**-(Aspa-ALit)-GLP-1(7-
`Gly*Asp*Arg*“Lys**-(Aspa-ALit)-GLP-1(7-36);
`36)amide; Gly®Asp**Arg”Lys’”-(Aspa-ALit)-GLP-1(7-37); Gly*Asp*’Arg”*™“Lys*-(Aspa-ALit)-
`GLP-1(7-38); Gly®Asp*Arg”*4Lys®-(Aspa-ALit)-GLP-1(7-39);
`Gly*Asp*Arg”*™“Lys**-(Aspa-
`ALit)-GLP-1(7-36);
`Gly®Asp*Arg”™Lys**-(Aspa-ALit)-GLP-1 (7-36)amide;
`Gly’Asp**Arg”™“Lys°’-(Aspa-ALit)-GLP-1(7-37);
` Gly*Asp*’Arg”**Lys**-(Aspa-ALit)-GLP-1(7-
`38); Gly’Asp*Arg”™Lys**-(Aspa-ALit)-GLP-1 (7-39);
`Val’Glu**Arg?*“Lys°*-(Aspa-ALit)-GLP-1(7-36);_Val®Glu*=Arg?®**Lys®*-(Aspa-ALit)-GLP-1(7-
`36)amide; Val®Glu**Arg?*Lys*”-(Aspa-ALit)-GLP-1(7-37); Val®Glu®’Arg**“Lys*-(Aspa-ALit)-
`GLP-1(7-38); Val’Glu®Arg”*™Lys®*-(Aspa-ALit)-GLP-1 (7-39); Val°Glu*Arg”*“Lys®*-(Aspa-ALit)-
`
`GLP-1(7-36); Val®GluArg’*“Lys®°-(Aspa-ALit)-GLP-1(7-36)amide;—Val®Glu**Arg”**“Lys*”-
`(Aspa-ALit)-GLP-1(7-37); Val’Glu®’Arg*“Lys®*-(Aspa-ALit)-GLP-1 (7-38); Val®Glu**Arg”™Lys**-
`
`15
`
`(Aspa-ALit)-GLP-1 (7-39);
` Val®Asp*Arg”*“Lys**-(Aspa-ALit)-GLP-1(7-
`Val’Asp*Arg”*“Lys**-(Aspa-ALit)-GLP-1(7-36);
`36)amide; Val’Asp*Arg®Lys*”-(Aspa-ALit)-GLP-1(7-37), Val®Asp*’Arg”™“Lys**-(Aspa-ALit)-
`GLP-1(7-38);
`Val’Asp**Arg’®*4Lys°°-(Aspa-ALit)-GLP-1(7-39);
` Val®@Asp*Arg*“Lys**-(Aspa-
`ALit)-GLP-1(7-36); Val’Asp“Arg”**4Lys*°-(Aspa-ALit)-GLP-1(7-36)amide; Val’Asp*Arg”*“Lys*’-
`(Aspa-ALit)-GLP-1 (7-37);
`Val’Asp*’Arg”*“Lys**-(Aspa-ALit)-GLP-1 (7-38);
`Val’Asp*Arg”*™Lys*®-(Aspa-ALit)-GLP-1 (7-39);
`Ser’Glu®Arg*™Lys**-(Aspa-ALit)-GLP-1 (7-
`SerGlu*Arg*™Lys*®-(Aspa-ALit)-GLP-1 (7-36);
`36)amide; Ser®Glu*Arg”*“Lys*”-(Aspa-ALit)-GLP-1(7-37); Ser®Glu®’Arg**“Lys**-(Aspa-ALit)-
`
`GLP-1(7-38); Ser®Glu**Arg”**“Lys**-(Aspa-ALit)-GLP-1(7-39);|Ser’Glu**Arg”*“Lys**-(Aspa-
`ALit)-GLP-1 (7-36); Ser’Glu*Arg?**Lys°*-(Aspa-ALit)-GLP-1(7-36)amide; Ser’Glu*Arg*™Lys*”-
`
`20
`
`Ser’Glu*Arg”™Lys**-(Aspa-ALit)-GLP-1 (7-38);
`
`25
`
`30
`
`(Aspa-ALit)-GLP-1 (7-37);
`SerGlu*Arg*™Lys**-(Aspa-ALit)-GLP-1 (7-39);
` Ser’Asp*Arg”*“Lys*°-(Aspa-ALit)-GLP-1 (7-
`Ser’Asp*Arg”™Lys*-(Aspa-ALit)-GLP-1(7-36);
`36)amide; Ser’Asp*Arg”*“Lys*’-(Aspa-ALit)-GLP-1(7-37); Ser’Asp*’Arg”™“Lys*-(Aspa-ALit)-
`GLP-1(7-38);
`SerAsp*Arg’®“Lys**-(Aspa-ALit)-GLP-1(7-39);
`Ser’Asp*Arg”**Lys**-(Aspa-
`ALit)-GLP-1(7-36);
`Ser’Asp*Arg?*Lys°*-(Aspa-ALit)-GLP-1(7-36)amide;
`Ser’Asp*Arg*™Lys*”-(Aspa-ALit)-GLP-1(7-37);
` Ser®Asp*’Arg”®*4Lys®®-(Aspa-ALit)-GLP-1(7-
`38); Ser’Asp*Arg**™“Lys*®-(Aspa-ALit)-GLP-1 (7-39):
` Thr®Glu°5Arg”**“Lys®*-(Aspa-ALit)-GLP-1(7-
`ThrGlu*Arg?*Lys**-(Aspa-ALit)-GLP-1(7-36),
`36)amide; ThrGlu*Arg”*™Lys*’-(Aspa-ALit)-GLP-1(7-37); Thr°Glu*’Arg**Lys*-(Aspa-ALit)-
`GLP-1(7-38); Thr’Giu*Arg?*“Lys®*-(Aspa-ALit)-GLP-1(7-39); Thr°’Glu*Arg”™Lys*-(Aspa-ALit)-
`
`GLP-1(7-36); Thr®Glu**Arg”*“Lys*°-(Aspa-ALit)-GLP-1(7-36)amide;—Thr°Glu**Arg?*“Lys*”-
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 104 of 270
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`

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`103
`
`15
`
`(Aspa-ALit)-GLP-1(7-37), Thr°'Glu*“Arg?™Lys*-(Aspa-ALit)-GLP-1(7-38); Thr°Glu*Arg”™Lys*-
`(Aspa-ALit)-GLP-1(7-39);
` ThrAsp*Arg”**Lys**-(Aspa-ALit)-GLP-1(7-
`ThreAsp*Arg”“Lys®*-(Aspa-ALit)-GLP-1(7-36);
`36)amide; ThAsp*Arg’*Lys*”-(Aspa-ALit)-GLP-1(7-37); ThrAsp*’Arg”™“Lys*-(Aspa-ALit)-
`GLP-1(7-38);
` Thr®Asp*Arg”**Lys®*-(Aspa-ALit)-GLP-1(7-39);
` Thr’Asp*Arg”*Lys**-(Aspa-
`ALit)-GLP-1 (7-36);
`ThrAsp*Arg=™Lys*°-(Aspa-ALit)-GLP-1(7-36)amide;
`TheAsp*Arg”“Lys*’-(Aspa-ALit)-GLP-1(7-37);
` Thr’Asp*’Arg”*™Lys*°-(Aspa-ALit)-GLP-1(7-
`38); ThFeAsp*Arg”*™Lys*?-(Aspa-ALit)-GLP-1 (7-39);
`Arg”**“Lys"*-(Aspa-ALit)-GLP-1 (7-36);
`Arg”*™Lys"*-(Aspa-ALit)-GLP-1(7-36)amide;
`Arg**Lys'*-(Aspa-ALit)-GLP-1 (7-37);
`Ara®“Lys"®-(Aspa-ALit)-GLP-1(7-38);
`Gly*Asp*Arg*“Lys'®-(Aspa-ALit)-GLP-1(7-36);
` Gly*Asp'’Arg”*“Lys'*-(Aspa-ALit)-GLP-1(7-
`36); Gly’Asp*Arg”*Lys'®-(Aspa-ALit)-GLP-1(7-36)amide; Gly*Asp'’Arg”™Lys"*-(Aspa-ALit)-
`GLP-1(7-36)amide;
`Gly*Asp"°Arg”*Lys'®-(Aspa-ALit)-GLP-1(7-37);
` Gly*Asp'°Arg”*“Lys®-
`(Aspa-ALit)-GLP-1 (7-38); Gly’Asp"“Arg“Lys"-(Aspa-ALit)-GLP-1 (7-38);
`Arg”®™Lys”*-(Aspa-ALit)-GLP-1 (7-36);
`Arg®*Lys**-(Aspa-ALit)-GLP-1 (7-36)amide;
`Arg?®4Lys®°-(Aspa-ALit)-GLP-1 (7-37);
`Arg?®“Lys”*-(Aspa-ALit)-GLP-1(7-38);
`Gly*Asp"Arg”“Lys”-(Aspa-ALit)-GLP-1(7-36);
` Gly®Asp"’Arg**Lys®-(Aspa-ALit)-GLP-1(7-
`36); Gly*Asp"*Arg?**“Lys”*-(Aspa-ALit)-GLP-1(7-36)amide; Gly°Asp'’Arg”™Lys”-(Aspa-ALit)-
`
`GLP-1(7-36)amide;—Gly’Asp"Arg?*™Lys*-(Aspa-ALit)-GLP-1(7-37); Gly®Asp'*Arg”*™Lys”°-
`20
`(Aspa-ALit)-GLP-1 (7-38); Gly’Asp’’Arg**™Lys”*-(Aspa-ALit)-GLP-1 (7-38);
`Arg”*“Lys’’-(Aspa-ALit)-GLP-1 (7-36);
`Arg’**Lys?’-(Aspa-ALit)-GLP-1(7-36)amide;
`Arg?®*4Lys*”-(Aspa-ALit)-GLP-1 (7-37);
`Arg?®*4Lys?”-(Aspa-ALit)-GLP-1(7-38);
`Gly*Asp"*Arg*Lys?’-(Aspa-ALit)-GLP-1(7-36);
` Gly®Asp"’Arg”*“Lys””-(Aspa-ALit)-GLP-1(7-
`36); Gly’Asp"Arg**“Lys?’-(Aspa-ALit)-GLP-1(7-36)amide; Gly*Asp"’Arg”Lys*’-(Aspa-ALit)-
`
`GLP-1(7-36)amide;—Gly’Asp"°Arg”***Lys?’-(Aspa-ALit)-GLP-1(7-37),; Gly*Asp'*Arg”*™Lys?’-
`25
`(Aspa-ALit)-GLP-1(7-38); Gly’Asp'’Arg”*“Lys?’-(Aspa-ALit)-GLP-1 (7-38);
`Arg”®**Lys"®-(Aspa-ALit)-GLP-1 (7-36);
`Arg?®™Lys'®-(Aspa-ALit)-GLP-1 (7-36)amide;
`Arg”*™“Lys"*-(Aspa-ALit)-GLP-1 (7-37);
`Arg®Lys'®-(Aspa-ALit)-GLP-1 (7-38);
`Val’Asp'*Arg?*™Lys'*-(Aspa-ALit)-GLP-1 (7-36); Val’Asp'’Arg”™“Lys'*-(Aspa-ALit)-GLP-1 (7-36);
`ValAsp'°Arg”*“Lys'®-(Aspa-ALit)-GLP-1(7-36)amide; Val’Asp'’Arg”Lys'*-(Aspa-ALit)-GLP-
`1(7-36)amide; Val®Asp'Arg”*Lys'®-(Aspa-ALit)-GLP-1(7-37); Val®Asp"*Arg”*“Lys'®-(Aspa-
`ALit)-GLP-1(7-38); Val®Asp'’Arg”™Lys"®-(Aspa-ALit)-GLP-1 (7-38);
`Arg?**4Lys”°-(Aspa-ALit)-GLP-1 (7-36);
`Arg®Lys?3-(Aspa-ALit)-GLP-1(7-36)amide;
`Arg**“Lys”-(Aspa-ALit)-GLP-1(7-37);
`Arg’6“L_ys?8-(Aspa-ALit)-GLP-1 (7-38);
`
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`Val’Asp"Arg”4Lys**-(Aspa-ALit)-GLP-1 (7-36); Val’Asp""Arg”™Lys”*-(Aspa-ALit)-GLP-1 (7-36);
`Val’Asp*Arg”*4Lys*-(Aspa-ALit)-GLP-1(7-36)amide; Val’Asp"7Arg”**“Lys**-(Aspa-ALit)-GLP-
`1(7-36)amide; Val®Asp‘*Arg”***Lys”*-(Aspa-ALit)-GLP-1(7-37); Val’Asp‘*Arg”*™“Lys”*-(Aspa-
`ALit)-GLP-1(7-38), Val’Asp'’Arg”™Lys”-(Aspa-ALit)-GLP-1 (7-38);
`Arg”*™Lys?’-(Aspa-ALit)-GLP-1 (7-36);
`Arg”54Lys?’-(Aspa-ALit)-GLP-1 (7-36)amide;
`Arg?®**Lys?”-(Aspa-ALit)-GLP-1(7-37);
`Arg?®‘Lys””-(Aspa-ALit)-GLP-1 (7-38);
`Val®AspArg**Lys?”-(Aspa-ALit)-GLP-1(7-36); Val®Asp'’Arg”™Lys*’-(Aspa-ALit)-GLP-1 (7-36),
`Val’Asp"*Arg”“Lys”’-(Aspa-ALit)-GLP-1(7-36)amide; Val*Asp"’Arg**™Lys”’-(Aspa-ALit)-GLP-
`1(7-36)amide; Val’Asp"*Arg”*™“Lys””-(Aspa-ALit)-GLP-1(7-37);
`Val®Asp‘*Arg’”*™“Lys*”-(Aspa-
`ALit)-GLP-1(7-38); Val’Asp'"Arg™Lys?”-(Aspa-ALit)-GLP-1(7-38);
`Arg***Lys"*-(Aspa-ALit)-GLP-1 (7-36);
`Arg”*4Lys'*-(Aspa-ALit)-GLP-1(7-36)amide;
`Arg”*™Lys"®-(Aspa-ALit)-GLP-1 (7-37);
`Arg®®™“Lys'®-(Aspa-ALit)-GLP-1 (7-38);
`Ser’Asp'°Arg*“Lys'®-(Aspa-ALit)-GLP-1(7-36);
` Ser’Asp'’Arg’®*“Lys'®-(Aspa-ALit)-GLP-1(7-
`36); SerAsp'*Arg**“Lys'®-(Aspa-ALit)-GLP-1(7-36)amide; Ser®Asp'’Arg*™“Lys"*-(Aspa-ALit)-
`
`GLP-1(7-36)amide; Ser’Asp"°Arg?**Lys'®-(Aspa-ALit)-GLP-1(7-37);|Ser®Asp"*Arg**™“Lys"*-
`15
`(Aspa-ALit)-GLP-1(7-38); Ser’Asp'’Arg”*™Lys'®-(Aspa-ALit)-GLP-1 (7-38);
`Arg”***Lys”*-(Aspa-ALit)-GLP-1 (7-36);
`Arg**4Lys”*-(Aspa-ALit)-GLP-1(7-36)amide;
`Arg?**4Lys®-(Aspa-ALit)-GLP-1(7-37):
`Arg?®*Lys®-(Aspa-ALit)-GLP-1 (7-38);
`Ser’Asp'*Arg*“Lys**-(Aspa-ALit)-GLP-1(7-36),
` Ser®Asp'’Arg”**“Lys*-(Aspa-ALit)-GLP-1(7-
`36); Ser’Asp"*Arg”*“Lys”-(Aspa-ALit)-GLP-1(7-36)amide; Ser®Asp"’Arg”*™“Lys”*-(Aspa-ALit)-
`GLP-1(7-36)amide;
`Ser®Asp"Arg?*“Lys”*-(Aspa-ALit)-GLP-1(7-37);
`SerAsp'*Arg”™Lys”-
`(Aspa-ALit)-GLP-1 (7-38); Ser’Asp'’Arg**Lys”*-(Aspa-ALit)-GLP-1 (7-38);
`Arg***Lys?’-(Aspa-ALit)-GLP-1 (7-36);
`Arg’*“Lys’-(Aspa-ALit)-GLP-1 (7-36)amide;
`Arg’*4Lys’-(Aspa-ALit)-GLP-1 (7-37);
`Arg”*™Lys?’-(Aspa-ALit)-GLP-1 (7-38);
`Ser’Asp"*Arg”™Lys?’-(Aspa-ALit)-GLP-1(7-36);
` Ser’Asp'’Arg”*Lys”’-(Aspa-ALit)-GLP-1 (7-
`36); Ser®Asp*Arg**“Lys?’-(Aspa-ALit)-GLP-1(7-36)amide; Ser’Asp'’Arg*™“Lys?’-(Aspa-ALit)-
`GLP-1(7-36)amide;
`Ser’Asp"*Arg**“Lys?’-(Aspa-ALit)-GLP-1(7-37);
`SerAsp"*Arg**™Lys?’-
`
`20
`
`25
`
`30
`
`(Aspa-ALit)-GLP-1(7-38); Ser’Asp'’Arg”*™“Lys?’-(Aspa-ALit)-GLP-1 (7-38);
`Arg”*™Lys'*-(Aspa-ALit)-GLP-1 (7-36),
`Arg*™Lys'®-(Aspa-ALit)-GLP-1 (7-36)amide;
`Arg”*™Lys"®-(Aspa-ALit)-GLP-1 (7-37);
`Arg>4Lys"*-(Aspa-ALit)-GLP-1 (7-38);
`Thr’Asp*Arg”*™Lys'*-(Aspa-ALit)-GLP-1(7-36);
` Thr’Asp"’Arg”*™Lys"*-(Aspa-ALit)-GLP-1(7-
`36); Thr’Asp'*Arg”*“Lys'®-(Aspa-ALit)-GLP-1(7-36)amide; ThréAsp’’Arg”“Lys"’-(Aspa-ALit)-
`GLP-1(7-36)amide;
` Thr’Asp'*Arg”**“Lys"®-(Aspa-ALit)-GLP-1(7-37);
`ThrAsp'*Arg”®“Lys"-
`(Aspa-ALit)-GLP-1(7-38); Thr’Asp‘’Arg*“Lys"*-(Aspa-ALit)-GLP-1(7-38);
`
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`Arg”*“Lys?3-(Aspa-ALit)-GLP-1(7-36)amide;
`Arg”*“Lys*-(Aspa-ALit)-GLP-1 (7-36);
`Arg”“Lys”*-(Aspa-ALit)-GLP-1 (7-38);
`Arg**“Lys**-(Aspa-ALit)-GLP-1(7-37);
` ThreAsp’’Arg”**Lys”*-(Aspa-ALit)-GLP-1(7-
`ThrAsp*Arg”*™“Lys”-(Aspa-ALit)-GLP-1(7-36);
`36); ThrAsp'*Arg”*Lys”*-(Aspa-ALit)-GLP-1(7-36)amide; Thr’Asp'’Arg”™Lys*-(Aspa-ALit)-
`GLP-1(7-36)amide;
`ThrAsp"’Arg®**Lys”-(Aspa-ALit)-GLP-1(7-37);
` Thr’Asp"*Arg”**Lys*-
`(Aspa-ALit)-GLP-1(7-38); ThrAsp"Arg”*“Lys*-(Aspa-ALit)-GLP-1 (7-38);
`Arg”**4Lys??-(Aspa-ALit)-GLP-1 (7-36);
`Arg**™Lys?’-(Aspa-ALit)-GLP-1(7-36)amide;
`Arg”™Lys”’-(Aspa-ALit)-GLP-1 (7-37);
`Arg?*™Lys?’-(Aspa-ALit)-GLP-1 (7-38);
`ThrAsp"Arg’*“Lys?”-(Aspa-ALit)-GLP-1(7-36);
` Thr’Asp'”Arg”*™Lys””-(Aspa-ALit)-GLP-1(7-
`36); Thr’AspArg®Lys?’-(Aspa-ALit)-GLP-1(7-36)amide; Thr’Asp'’Arg”™“Lys’’-(Aspa-ALit)-
`GLP-1(7-36)amide;
`Thr’Asp"*Arg?®Lys’-(Aspa-ALit)-GLP-1(7-37);
` Thr’Asp"?Arg”*™Lys?’-
`(Aspa-ALit)-GLP-1 (7-38); ThrAspArg”*Lys””-(Aspa-ALit)-GLP-1 (7-38);
`Arg*Lys*-(Glyc-ADod)-GLP-1(7-36); Arg™“Lys”-(Glyc-ADod)-GLP-1(7-36); Arg”*™“Lys**-(Glyc-
`ADod)-GLP-1(7-36); Arg**Lys**-(Glyc-ADod)-GLP-1(7-36)amide; Arg™ Lys”°-(Giyc-ADod)-GLP-
`1(7-36)amide; Arg?°*Lys**-(Glyc-ADod)-GLP-1(7-36)amide; Arg* Lys*-(Glyc-ADod)-GLP-1(7-
`37); Arg™“Lys”-(Glyc-ADod)-GLP-1 (7-37); Arg”**Lys**-(Glyc-ADod)-GLP-1(7-37); Arg”Lys*-
`(Glyc-ADod)-GLP-1(7-38); Arg*Lys?*-(Glyc-ADod)-GLP-1(7-38)
`; Arg’®*Lys®-(Glyc-ADod)-
`GLP-1(7-38);
`Arg®*Lys“4-(Glyc-ADod)-GLP-1(7-39);
` Arg**Lys”°-(Glyc-ADod)-GLP-1 (7-39);
`Arg?®*4Lys®°-(Glyc-ADod)-GLP-1 (7-39);
`Gly*’Arg™Lys”-(Glyc-ADod)-GLP-1 (7-36);
`Gly*’Arg”*Lys™-(Glyc-ADod)-GLP-1 (7-36);
` Gly’Arg**Lys*-(Glyc-ADod)-GLP-1(7-36)amide;
`Gly*’Arg?*Lys**-(Glyc-ADod)-GLP-1(7-36),
`Gly®Arg”*™Lys**-(Glyc-ADod)-GLP-1(7-
`Gly*Arg™Lys”*-(Glyc-ADod)-GLP-1(7-36)amide;
`36)amide; Gly*Arg?Lys*-(Glyc-ADod)-GLP-1 (7-37); Gly*Arg*Lys®-(Glyc-ADod)-GLP-1(7-37):
`Gly*Arg”™™Lys**-(Glyc-ADod)-GLP-1 (7-37);
`Gly*Arg”Lys™-(Glyc-ADod)-GLP-1 (7-38);
`Gly*Arg™Lys”°-(Glyc-ADod)-GLP-1 (7-38)
`Gly*Arg”*™Lys**-(Glyc-ADod)-GLP-1 (7-38):
`
`:
`
`10
`
`20
`
`25
`
`Gly’Arg*Lys’°-(Glyc-ADod)-GLP-1(7-39);
`
`Gly®Arg*Lys*-(Glyc-ADod)-GLP-1(7-39);
`Gly*Arg®Lys*°-(Glyc-ADod)-GLP-1(7-39);
`Val®Arg™Lys°-(Glyc-ADod)-GLP-1 (7-36);
`Val’Arg?*Lys*-(Glyc-ADod)-GLP-1(7-36):
`Val’ArgLys*-(Glyc-ADod)-GLP-1(7-36)amide;
`Val’Arg**™Lys**-(Glyc-ADod)-GLP-1 (7-36);
`Val®Arg?®“Lys*®-(Glyc-ADod)-GLP-1(7-
`Val’Arg™Lys”°-(Glyc-ADod)-GLP-1(7-36)amide;
`36)amide; Val®Arg*Lys*-(Glyc-ADod)-GLP-1(7-37); Val®Arg™Lys”°-(Glyc-ADod)-GLP-1(7-37);
`Val’Arg®™Lys**-(Glyc-ADod)-GLP-1 (7-37);
`Val’Arg*Lys™-(Glyc-ADod)-GLP-1 (7-38);
`
`Val’Arg*Lys’-(Glyc-ADod)-GLP-1(7-38) :_Val’Arg’**Lys®°-(Glyc-ADod)-GLP-1 (7-38);
`
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`Val’Arg™Lys”°-(Glyc-ADod)-GLP-1(7-39);
`
`;
`
`Val’Arg®Lys*-(Glyc-ADod)-GLP-1(7-39);
`Val’Arg”*™Lys**-(Glyc-ADod)-GLP-1(7-39):
`Ser’Arg™Lys”°-(Glyc-ADod)-GLP-1(7-36);
`SerArg”Lys™-(Glyc-ADod)-GLP-1 (7-36);
` Ser°Arg’**Lys*-(Glyc-ADod)-GLP-1 (7-36)amide,
`SerArg**™“Lys*®-(Glyc-ADod)-GLP-1(7-36);
`Ser’Arg”™Lys*°-(Glyc-ADod)-GLP-1(7-
`Ser’Arg™Lys**-(Glyc-ADod)-GLP-1 (7-36)amide;
`36)amide; Ser’Arg”*Lys*-(Glyc-ADod)-GLP-1 (7-37); Ser’Arg™Lys*°-(Glyc-ADod)-GLP-1 (7-37);
`SerArg”“Lys*®-(Glyc-ADod)-GLP-1(7-37);
`SerArg*Lys™*-(Glyc-ADod)-GLP-1 (7-38);
`SerArg™Lys”*-(Glyc-ADod)-GLP-1(7-38)
` Ser®Arg®*4Lys®®-(Glyc-ADod)-GLP-1 (7-38);
`SerArg”*Lys™-(Glyc-ADod)-GLP-1 (7-39);
`Ser’Arg™Lys”-(Glyc-ADod)-GLP-1(7-39);
`SerArg”>™Lys*®-(Glyc-ADod)-GLP-1 (7-39);
`Thr’Arg*Lys”*-(Glyc-ADod)-GLP-1 (7-36);
`ThrArg”*Lys**-(Glyc-ADod)-GLP-1 (7-36);
` Thr*Arg”*Lys**-(Glyc-ADod)-GLP-1(7-36)amide;
`ThrArg?“Lys®*-(Glyc-ADod)-GLP-1(7-36);
`ThrArg”**“*Lys*°-(Glyc-ADod)-GLP-1(7-
`ThrArg™Lys**-(Glyc-ADod)-GLP-1(7-36)amide;
`36)amide; ThrArg*Lys*-(Glyc-ADod)-GLP-1(7-37); ThrArg™*Lys**-(Glyc-ADod)-GLP-1(7-37);
`ThrArg”*™Lys*°-(Glyc-ADod)-GLP-1 (7-37);
`Thr’Arg”Lys*-(Glyc-ADod)-GLP-1 (7-38);
`
`TheArg™‘Lys*-(Glyc-ADod)-GLP-1(7-38) :—Thr’Arg***4Lys°*-(Glyc-ADod)-GLP-1(7-38);
`ThrArg”Lys*-(Glyc-ADod)-GLP-1 (7-39),
`ThreArg“Lys”°-(Glyc-ADod)-GLP-1(7-39);
`ThrArg?Lys*-(Glyc-ADod)-GLP-1(7-39);
` Gly*®Glu®°Arg**“Lys**-(Glyc-ADod)-GLP-1(7-
`Gly’Glu“Arg”>™“Lys*°-(Glyc-ADod)-GLP-1(7-36);
`36)amide; Gly®Glu**Arg”*“Lys*’-(Glyc-ADod)-GLP-1(7-37); Gly®Glu*’Arg”*“Lys**-(Glyc-ADod)-
`GLP-1(7-38);
` Gly®Glu*Arg?**Lys°*-(Glyc-ADod)-GLP-1(7-39);
` Gly®Glu**Arg”™Lys**-(Glyc-
`ADod)-GLP-1(7-36):
`Gly’Glu*Arg’*Lys®-(Glyc-ADod)-GLP-1(7-36)amide;
`Gly®Glu*Arg**“Lys*”-(Glyc-ADod)-GLP-1(7-37),;
` Gly®Glu®’Arg”*™“Lys*®-(Glyc-ADod)-GLP-1(7-
`38); Gly’Glu*Arg*™Lys*°-(Glyc-ADod)-GLP-1 (7-39);
`Gly*Asp*Arg”™Lys*-(Glyc-ADod)-GLP-1(7-36); Gly’Asp**Arg”*™Lys**-(Glyc-ADod)-GLP-1(7-
`36)amide; Gly*Asp**Arg”“Lys*”-(Glyc-ADod)-GLP-1 (7-37); Gly’Asp*”Arg”*™Lys**-(Glyc-ADod)-
`GLP-1(7-38); Gly’Asp*Arg”*“Lys*°-(Glyc-ADod)-GLP-1(7-39); Gly’Asp*Arg”*“Lys*-(Glyc-
`ADod)-GLP-1(7-36);
`Gly®Asp*Arg*4Lys*°-(Glyc-ADod)-GLP-1(7-36)amide;
`Gly*Asp*Arg”*“Lys*”-(Glyc-ADod)-GLP-1(7-37); Gly’Asp*’Arg”*™Lys**-(Glyc-ADod)-GLP-1(7-
`38); Gly*Asp*Arg”*“Lys**-(Glyc-ADod)-GLP-1 (7-39);
`Val’Glu®Arg*™Lys®®.(Glyc-ADod)-GLP-1(7-36);
` Val’Glu*Arg”**Lys**-(Glyc-ADod)-GLP-1(7-
`36)amide; Val°Glu*Arg”*™“Lys*”-(Glyc-ADod)-GLP-1(7-37); Val’Glu*’Arg”™Lys*-(Glyc-ADod)-
`GLP-1(7-38);
` Val’Glu®*Arg’*“Lys®°-(Glyc-ADod)-GLP-1(7-39);
` Val®Glu*Arg’®Lys®*-(Glyc-
`ADod)-GLP-1 (7-36):
`Val’Glu*Arg?Lys®-(Glyc-ADod)-GLP-1 (7-36)amide;
`
`15
`
`20
`
`25
`
`30
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` Val’Glu*”Arg’*“Lys*-(Glyc-ADod)-GLP-1(7-
`Val’Glu**Arg?*™“Lys*’-(Glyc-ADod)-GLP-1(7-37);
`38); Val’Glu**Arg”*™Lys**-(Glyc-ADod)-GLP-1 (7-39);
`ValtAsp*Arg*™Lys**-(Glyc-ADod)-GLP-1(7-36); Val®Asp*Arg**“Lys**-(Glyc-ADod)-GLP-1(7-
`36)amide; ValAsp*Arg?*4Lys°’-(Glyc-ADod)-GLP-1 (7-37); Val’Asp”Arg”*“Lys*-(Glyc-ADod)-
`GLP-1(7-38); Val’Asp*Arg’*™“Lys*°-(Glyc-ADod)-GLP-1(7-39); Val’Asp**Arg”“Lys*-(Glyc-
`ADod)-GLP-1 (7-36),
`Val’Asp*Arg”™Lys*®-(Glyc-ADod)-GLP-1(7-36)amide;
`Val’Asp*Arg*™Lys*’-(Glyc-ADod)-GLP-1(7-37); Val’Asp*’Arg®™Lys*-(Glyc-ADod)-GLP-1(7-
`
`10
`
`38); Val’Asp™*Arg”*™Lys**-(Glyc-ADod)-GLP-1(7-39);
`SerGluArg*™“Lys**-(Glyc-ADod)-GLP-1(7-36);
`Ser’Glu**Arg”**Lys**-(Glyc-ADod)-GLP-1(7-
`36)amide; Ser®’Glu*Arg”*™Lys*”-(Glyc-ADod)-GLP-1(7-37); Ser’Glu”’Arg”“Lys*-(Glyc-ADod)-
`GLP-1(7-38);
`Ser®Glu*Arg?*™“Lys**-(Glyc-ADod)-GLP-1(7-39);
` Ser®Glu**Arg”**Lys**-(Glyc-
`ADod)-GLP-1(7-36);
`SerGlu*Arg”™Lys**-(Glyc-ADod)-GLP-1(7-36)amide;
`
`Ser®Glu®’Arg”*™“Lys*-(Glyc-ADod)-GLP-1(7-
`Se?Glu*Arg*™Lys*”-(Glyc-ADod)-GLP-1(7-37);
`38); Ser’Glu*Arg”*™Lys**-(Glyc-ADod)-GLP-1 (7-39);
`SerAsp*Arg*™Lys®-(Glyc-ADod)-GLP-1(7-36); Ser’Asp*Arg?*™“Lys*°-(Glyc-ADod)-GLP-1(7-
`
`36)amide; Ser’Asp*Arg’*“Lys*”-(Glyc-ADod)-GLP-1(7-37);|Ser®Asp*’Arg”®*“*Lys*?-(Glyc-
`ADod)-GLP-1(7-38); Ser’Asp*Arg”**“Lys**-(Glyc-ADod)-GLP-1(7-39); Ser®Asp*Arg”®“Lys*-
`(Glyc-ADod)-GLP-1 (7-36);
`SerAsp”Arg*™Lys*®-(Glyc-ADod)-GLP-1(7-36)amide;
`
`15
`
`20
`
`25
`
`30
`
`SerAsp*Arg”™Lys*’-(Glyc-ADod)-GLP-1(7-37); Ser’Asp*’Arg”*™“Lys®*-(Glyc-ADod)-GLP-1(7-
`38); Ser’Asp*Arg”™Lys**-(Glyc-ADod)-GLP-1 (7-39);
`Thr’Glu*Arg*™Lys**-(Glyc-ADod)-GLP-1(7-36);
` Thr®Glu**Arg”**“Lys*°-(Glyc-ADod)-GLP-1(7-
`36)amide; Thr’Glu**Arg®*Lys*’-(Glyc-ADod)-GLP-1 (7-37); Thr®Glu*’Arg**“Lys**-(Glyc-ADod)-
`GLP-1(7-38);
` ThrGlu**Arg”*“Lys®®-(Glyc-ADod)-GLP-1(7-39);
` Thr’Glu*®*Arg”*“Lys*°-(Glyc-
`ADod)-GLP-1(7-36);
`Thr’Glu*Arg”*“Lys*-(Glyc-ADod)-GLP-1(7-36)amide;
`ThrGlu*Arg**Lys?”-(Glyc-ADod)-GLP-1(7-37);
` Thr°Glu®’Arg”**Lys**-(Glyc-ADod)-GLP-1(7-
`38); Thr’Glu*Arg?*™Lys*°-(Glyc-ADod)-GLP-1 (7-39);
`Thr’Asp*Arg*™Lys®-(Glyc-ADod)-GLP-1(7-36); ThrAspArg”*“Lys®*-(Glyc-ADod)-GLP-1(7-
`36)amide; Thr’Asp*Arg”*™Lys*’-(Glyc-ADod)-GLP-1(7-37); Thr’Asp*’Arg”™“Lys**-(Glyc-ADod)-
`GLP-1(7-38);
` Thr’Asp**Arg”*“*Lys**-(Giyc-ADod)-GLP-1(7-39);
` Thr’Asp*Arg”*™“Lys**-(Glyc-
`ADod)-GLP-1(7-36);
`Thr’Asp*Arg“Lys*®-(Glyc-ADod)-GLP-1(7-36)amide;
`ThrAsp*Arg*™Lys*”-(Glyc-ADod)-GLP-1(7-37);
` Thr’Asp*”Arg?*“Lys*®-(Glyc-ADod)-GLP-1(7-
`38); Thr’Asp*Arg®™Lys**-(Glyc-ADod)-GLP-1 (7-39);
`Arg”*™Lys'®-(Glyc-ADod)-GLP-1 (7-36);
`Arg”*™Lys"*-(Glyc-ADod)-GLP-1 (7-36)amide;
`Arg?®™Lys'®-(Glyc-ADod)-GLP-1(7-37):
`Arg?**4Lys"®-(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
`
`Gly*Asp"*Arg™Lys'®-(Glyc-ADod)-GLP-1(7-36); Gly*Asp'’Arg”*™“Lys'*-(Glyc-ADod)-GLP-1(7-
`36); GlySAsp*Arg”*™Lys"®-(Glyc-ADod)-GLP-1(7-36)amide; Gly*Asp’’Arg”*™Lys'°-(Glyc-ADod)-
`GLP-1(7-36)amide; Gly®Asp"’Arg”™Lys'®-(Glyc-ADod)-GLP-1(7-37);
`_Gly*Asp'*Arg**Lys"°-
`(Glyc-ADod)-GLP-1 (7-38); Gly’Asp”Arg”*™Lys'*-(Glyc-ADod)-GLP-1(7-38);
`Arg***Lys?°-(Glyc-ADod)-GLP-1 (7-36);
`Arg?*“Lys*-(Glyc-ADod)-GLP-1(7-36)amide;
`Arg”*™Lys”*-(Glyc-ADod)-GLP-1(7-37);
`Arg***Lys”*-(Glyc-ADod)-GLP-1 (7-38);
`Gly*Asp"Arg”™“Lys’*-(Glyc-ADod)-GLP-1(7-36); Gly*Asp'’Arg”*™Lys**-(Glyc-ADod)-GLP-1(7-
`36); Gly®Asp°Arg”*™4Lys”-(Glyc-ADod)-GLP-1(7-36)amide; Gly*Asp'7Arg”™Lys”*-(Glyc-ADod)-
`GLP-1(7-36)amide; Gly®Asp"°Arg”**‘Lys”*-(Glyc-ADod)-GLP-1(7-37);
`Gly*Asp‘*Arg”*™“Lys”-
`(Glyc-ADod)-GLP-1(7-38); Gly’Asp'’Arg*™Lys*-(Glyc-ADod)-GLP-1 (7-38);
`Arg®“Lys?’-(Glyc-ADod)-GLP-1(7-36);
`Arg?**4Lys??-(Glyc-ADod)-GLP-1(7-36)amide;
`Arg?***Lys?”-(Glyc-ADod)-GLP-1(7-37);
`Arg?*“Lys?’-(Glyc-ADod)-GLP-1(7-38);
`Gly*AspArg”*™Lys*’-(Glyc-ADod)-GLP-1(7-36); Gly’Asp'’Arg”*Lys”’-(Glyc-ADod)-GLP-1(7-
`36); Gly*Asp"*Arg”>™Lys?”-(Glyc-ADod)-GLP-1(7-36)amide; Gly’Asp"’Arg”™Lys*’-(Glyc-ADod)-
`GLP-1(7-36)amide; Gly®Asp"Arg**™*Lys”’-(Glyc-ADod)-GLP-1(7-37); Gly®Asp'*Arg”*“Lys”’-
`(Glye-ADod)-GLP-1(7-38); Gly*Asp"”Arg2“Lys?”-(Glyc-ADod)-GLP-1 (7-38);
`Arg”*™Lys'®-(Glyc-ADod)-GLP-1 (7-36);
`Arg”**Lys'*-(Glyc-ADod)-GLP-1(7-36)amide;
`Arg?®*Lys'®-(Glyc-ADod)-GLP-1 (7-37);
`Arg?®*Lys'®-(Glyc-ADod)-GLP-1(7-38);
`Val’Asp*Arg”*4Lys"®-(Glyc-ADod)-GLP-1(7-36); Val@Asp"’Arg?®*Lys"®.(Glyc-ADod)-GLP-1 (7-
`36); ValAsp"Arg”*“Lys'®-(Glyc-ADod)-GLP-1(7-36)amide; Val*Asp"’Arg”**™Lys"*-(Glyc-ADod)-
`GLP-1(7-36)amide; Val®Asp'°Arg?***Lys’®-(Glyc-ADod)-GLP-1(7-37);
`Val®Asp‘*Arg**™“Lys'*-
`(Glyc-ADod)-GLP-1 (7-38); Val®Asp"’Arg*™Lys"*-(Glyc-ADod)-GLP-1 (7-38);
`Arg”*“Lys”*-(Glyc-ADod)-GLP-1 (7-36);
`Arg*™“Lys”*-(Glyc-ADod)-GLP-1 (7-36)amide;
`Arg?***Lys”°-(Glyc-ADod)-GLP-1 (7-37):
`Arg?**Lys?-(Glyc-ADod)-GLP-1 (7-38);
`Val’Asp"*Arg*™Lys?*-(Glyc-ADod)-GLP-1(7-36); Val’Asp*’Arg”*“Lys*-(Glyc-ADod)-GLP-1(7-
`36); Val’Asp"Arg”“Lys”-(Glyc-ADod)-GLP-1(7-36)amide; Val°Asp"’Arg”*™Lys”*-(Glyc-ADod)-
`GLP-1(7-36)amide; Val®Asp"*Arg”*“Lys**-(Glyc-ADod)-GLP-1(7-37);
` Val®Asp**Arg’”*“Lys”*-
`(Glyc-ADod)-GLP-1 (7-38); Val®Asp'’Arg”*™Lys”-(Glyc-ADod)-GLP-1 (7-38);
`Arg”™Lys?’-(Glyc-ADod)-GLP-1 (7-36);
`Arg’°Lys*’-(Glyc-ADod)-GLP-1(7-36)amide;
`Arg®®**Lys?”-(Glyc-ADod)-GLP-1(7-37);
`Arg?**4Lys?’-(Glyc-ADod)-GLP-1 (7-38);
`Val’Asp"*Arg™Lys?’-(Glyc-ADod)-GLP-1(7-36);
` Val®Asp"’Arg”**Lys?”-(Glyc-ADod)-GLP-1(7-
`36); Val*Asp"*Arg**“Lys*”-(Glyc-ADod)-GLP-1(7-36)amide; Val’Asp*’Arg”*™Lys”’-(Glyc-ADod)-
`GLP-1(7-36)amide; Val’Asp"*Arg’*Lys?”-(Glyc-ADod)-GLP-1(7-37);
`Val’Asp**Arg”*™“Lys””-
`(Glyc-ADod)-GLP-1(7-38); Val’Asp'’Arg**Lys*”-(Glyc-ADod)-GLP-1 (7-38);
`
`10
`
`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
`
`Arg?®*4Lys"*-(Glyc-ADod)-GLP-1(7-36)amide;
`Arg?®*Lys'®-(Glyc-ADod)-GLP-1 (7-36);
`Arg?**Lys'®-(Glyc-ADod)-GLP-1 (7-38);
`Arg’*™“Lys'8-(Glyc-ADod)-GLP-1 (7-37);
`SerAsp'*Arg”*™Lys'®-(Glyc-ADod)-GLP-1(7-36); Ser’Asp'’Arg”*™Lys'*-(Glyc-ADod)-GLP-1(7-
`
`36); Ser’Asp'’Arg’**Lys"*-(Glyc-ADod)-GLP-1(7-36)amide;—Ser®Asp'’Arg*™“Lys"*-(Glyc-
`ADod)-GLP-1(7-36)amide;
`Ser’Asp*Arg”™Lys'*-(Glyc-ADod)-GLP-1(7-37);
`SerAsp*Arg“Lys'®-(Glyc-ADod)-GLP-1(7-38); Ser’Asp"’Arg**“Lys"*-(Glyc-ADod)-GLP-1(7-
`
`10
`
`15
`
`20
`
`25
`
`30
`
`38);
`Arg?**4Lys®-(Glyc-ADod)-GLP-1(7-36)amide;
`Arg?**Lys*-(Glyc-ADod)-GLP-1(7-36);
`Arg?®*Lys”°-(Glyc-ADod)-GLP-1 (7-38);
`Arg?®*4Lys**-(Glye-ADod)-GLP-1(7-37):
`SerAsp*Arg”™“Lys”-(Glyc-ADod)-GLP-1(7-36); Ser’Asp'’Arg**™“Lys*-(Glyc-ADod)-GLP-1(7-
`36);
` Ser’Asp'°Arg’*“Lys”°-(Glyc-ADod)-GLP-1(7-36)amide;
` Ser’Asp‘’Arg”*“Lys*-(Glyc-
`ADod)-GLP-1(7-36)amide;
`SerAsp"*Arg”™Lys”-(Glyc-ADod)-GLP-1 (7-37);
`Ser’Asp"Arg>“Lys*-(Glyc-ADod)-GLP-1(7-38); Ser’Asp'’Arg*“Lys**-(Glyc-ADod)-GLP-1(7-
`
`38);
`Arg”*™Lys?’-(Glyc-ADod)-GLP-1 (7-36),
`Arg”*™Lys’-(Glyc-ADod)-GLP-1 (7-37);
`
`Arg’**Lys*’-(Glyc-ADod)-GLP-1(7-36)amide;
`Arg?®*4Lys?’-(Glyc-ADod)-GLP-1(7-38);
`
`SerAspArg”*™Lys*’-(Glyc-ADod)-GLP-1(7-36); Ser’Asp'’Arg”*™Lys?’-(Glyc-ADod)-GLP-1(7-
`36);
`SerAsp"*Arg”®4Lys?’-(Glyc-ADod)-GLP-1(7-36)amide;
` Ser®’Asp‘’Arg”*™Lys*’-(Glyc-
`ADod)-GLP-1(7-36)amide;
`Ser*Asp'*Arg”*™4Lys””-(Glyc-ADod)-GLP-1 (7-37);
`Ser’AspArg***™Lys*’-(Glyc-ADod)-GLP-1(7-38); Ser®Asp'’Arg”*™Lys?’-(Glyc-ADod)-GLP-1(7-
`
`38);
`
`Arg”®*Lys'®-(Glyc-ADod)-GLP-1 (7-36)amide;
`Arg***Lys'®-(Glyc-ADod)-GLP-1 (7-36);
`Arg”™Lys'®-(Glyc-ADod)-GLP-1 (7-38);
`Arg”®*“Lys'®-(Glyc-ADod)-GLP-1 (7-37);
`Thr’Asp*Arg”®™Lys"*-(Glyc-ADod)-GLP-1 (7-36); Thr’Asp'’Arg”*™Lys"*-(Glyc-ADod)-GLP-1(7-
`36); ThrAsp*Arg?*™Lys'*-(Glyc-ADod)-GLP-1(7-36)amide; Thr’Asp'’Arg”™Lys'®-(Glyc-ADod)-
`GLP-1(7-36)amide; Thr°Asp'*Arg*“Lys'®-(Glyc-ADod)-GLP-1(7-37);
` Thr’Asp'*Arg”™“Lys®*-
`(Glyc-ADod)-GLP-1 (7-38); Thr’Asp"’Arg”*™“Lys-(Glyc-ADod)-GLP-1(7-38);
`Arg’®*“_ys*-(Glyc-ADod)-GLP-1 (7-36);
`Arg®™Lys**-(Glyc-ADod)-GLP-1(7-36)amide;
`Arg**™Lys”-(Glyc-ADod)-GLP-1(7-37);
`Arg’®’*Lys-(Glyc-ADod)-GLP-1 (7-38);
`ThrAsp*Arg*™Lys*-(Glyc-ADod)-GLP-1(7-36); ThrAsp"Arg”*Lys*-(Glyc-ADod)-GLP-1(7-
`36); Thr’Asp*Arg*™Lys”-(Glyc-ADod)-GLP-1(7-36)amide; ThrAsp’Arg*™Lys”-(Glyc-ADod)-
`GLP-1(7-36)amide;
`ThrAsp‘*Arg**“Lys’°-(Glyc-ADod)-GLP-1(7-37);
`Thr’Asp"*Arg”®*™Lys”°-
`(Glyc-ADod)-GLP-1(7-38); Thr?Asp"”Arg”*“4Lys*-(Glyc-ADod)-GLP-1 (7-38);
`
`M
`
`M
`
` PFIZER, INC. v. NOVO NORDISK A/S - IPR2020-01252, Ex. 1033, p. 111 of 270
`
`

`

`WO 99/43706
`
`PCT/DK99/00082
`
`110
`
`Arg’°*4Lys?’-(Glyc-ADod)-GLP-1(7-36)amide;
`Arg*“Lys”’-(Glyc-ADod)-GLP-1 (7-36);
`Arg”*4Lys?’-(Glyc-ADod)-GLP-1 (7-38);
`Arg*4Lys?’-(Glyc-ADod)-GLP-1 (7-37);
` Thr’Asp'’Arg”™Lys?’-(Glyc-ADod)-GLP-1 (7-
`ThrAsp'*Arg*™“Lys?’-(Glyc-ADod)-GLP-1(7-36);
`36); ThrFAsp*Arg?**4Lys?’-(Glyc-ADod)-GLP-1(7-36)amide; Thr’Asp'’Arg”*™Lys?’-(Glyc-ADod)-
`GLP-1(7-36)amide; Thr’Asp"°Arg”*Lys?’-(Glyc-ADod)-GLP-1(7-37);
` Thr’Asp'®Arg”*“Lys?’-
`(Glyc-ADod)-GLP-1 (7-38); Thr’Asp"“Arg?®“Lys?”-(Glyc-ADod)-GLP-1 (7-38);
`Arg*Lys*-(Glyc-ATet)-GLP-1 (7-36); Arg*Lys*°-(Glyc-ATet)-GLP-1(7-36); Arg”**Lys**-(Glyc-
`ATet)-GLP-1(7-36); Arg”*Lys*-(Glyc-ATet)-GLP-1(7-36)amide; Arg™ Lys”-(Glyc-ATet)-GLP-
`1(7-36)amide; Arg”*“Lys*°*-(Glyc-ATet)-GLP-1(7-36)amide; Arg”® Lys*-(Glyc-ATet)-GLP-1(7-
`37), Arg™Lys”*-(Glyc-ATet)-GLP-1(7-37); Arg”®*“Lys*-(Glyc-ATet)-GLP-1 (7-37); Arg”*Lys™-
`
`(Glyc-ATet)-GLP-1(7-38); Arg®Lys”*-(Glyc-ATet)-GLP-1(7-38) ; Arg®**Lys®*-(Glyc-ATet)-GLP-
`1(7-38); Arg”*Lys*-(Glyc-ATet)-GLP-1(7-39); Arg™Lys*-(Glyc-ATet)-GLP-1 (7-39); Arg**“Lys**-
`
`;
`
`(Glyc-ATet)-GLP-1 (7-39);
`Gly*Arg™Lys”°-(Glyc-ATet)-GLP-1 (7-36);
`Gly*Arg*Lys*-(Glyc-ATet)-GLP-1(7-36);
`Gly*Arg*Lys**-(Glyc-ATet)-GLP-1 (7-36)amide;
`Gly*Arg”*™Lys*°-(Glyc-ATet)-GLP-1 (7-36):
`Gly’Arg*“Lys*°-(Glyc-ATet)-GLP-1(7-
`Gly’Arg™Lys”-(Glyc-ATet)-GLP-1(7-36)amide;
`36)amide; Gly*Arg*Lys*-(Glyc-ATet)-GLP-1(7-37); Gly’Arg™Lys”°-(Glyc-ATet)-GLP-1 (7-37);
`Gly*Arg”4Lys®*-(Glyc-ATet)-GLP-1 (7-37):
`Gly*Arg?Lys*-(Glyc-ATet)-GLP-1 (7-38);
`Gly*Arg™‘Lys®-(Glyc-ATet)-GLP-1(7-38)
`Gly*Arg®*“Lys®-(Glyc-ATet)-GLP-1(7-38):
`Gly’Arg*Lys*-(Glyc-ATet)-GLP-1(7-39);
`Gly*Arg™Lys”°-(Glyc-ATet)-GLP-1 (7-39);
`Gly’Arg”*™Lys**-(Glyc-ATet)-GLP-1 (7-39);
`ValArg™Lys”*-(Glyc-ATet)-GLP-1 (7-36);
`Val’Arg*Lys™-(Glyc-ATet)-GLP-1 (7-36):
`Val’Arg*Lys™-(Glyc-ATet)-GLP-1 (7-36)amide;
`Val’Arg***Lys*°-(Glyc-ATet)-GLP-1 (7-36);
`Val’Arg”*Lys*-(Glyc-ATet)-GLP-1 (7-
`Val’Arg™Lys”°-(Glyc-ATet)-GLP-1 (7-36)amide;
`36)amide; Val*Arg”Lys*-(Glyc-ATet)-GLP-1(7-37); Val’Arg™Lys”°-(Glyc-ATet)-GLP-1 (7-37);
`Val’Arg***Lys**-(Glyc-ATet)-GLP-1 (7-37);
`Val’Arg**Lys*-(Glyc-ATet)-GLP-1 (7-38);
`Val’Arg™Lys”-(Glyc-ATet)-GLP-1

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