Patent ES-2713185-T3 (ES)
Title: Derivados de péptidos similares a GLP-1, y sus usos
Inventor: REEDTZ-RUNGE STEFFEN
IPC: C07K14/605
Filed: 2014-07-02
Granted: 2019-05-20
Abstract: Un derivado de GLP-1 seleccionado de lo siguiente: N{Épsilon-27}-[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]-[Aib8,Glu22,Arg26,Lys27,Arg34]-GLP-1-(7-37)-peptidil-Gly-Gly-Gly-Ser-N{Épsilon}[2-[2-[2-[[2-[2-[2- [[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]Lys, Quím. 21: **Fórmula** N{Épsilon-31}-[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]-[Aib8,Glu22,Arg26,Lys31,Arg34]-GLP-1-(7-37)-peptidil-Gly-Gly-Gly-Ser-N{Épsilon}[2-[2-[2-[[2-[2-[2- [[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]Lys, Quím. 22: **Fórmula** Nα([Aib8,Glu22,Arg26,Arg34]-GLP-1-(7-37)-peptidil)-N{épsilon}[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]Lys-Gly-Gly-Ser-N{épsilon}[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]Lys, **Fórmula** N{Épsilon-23}-[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] 20 acetil]-[Aib8,Glu22,Lys23,Arg26,Arg34]-GLP-1-(7-37)-peptidil-Gly-Gly-Gly-Ser-N{Épsilon}[2-[2-[2-[[2-[2-[2- [[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]Lys, Quím. 24: **Fórmula** N{Épsilon-36}-[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]-[Aib8,Glu22,Arg26,Arg34,Lys36]-GLP-1-(7-37)-peptidil-Gly-Gly-Gly-Ser-N{Épsilon}[2-[2-[2-[[2-[2-[2- [[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoylamino)metil]cyclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etox i]acetil]Lys, Quím. 25: **Fórmula** N{Épsilon-18}-[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] 20 acetil]-[Aib8,Lys18,Glu22,Arg26,Arg34]-GLP-1-(7-37)-peptidil-Gly-Gly-Gly-Ser-N{Épsilon}[2-[2-[2-[[2-[2-[2- [[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]Lys, Quím. 26: **Fórmula** Nα([Aib8,Glu22,Arg26,Arg34]-GLP-1-(7-37)-peptidil)-N{Épsilon}[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4- carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]hexanoil]amino]hexanoil]Lys-Gly- Gly-Ser-N{Épsilon}[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]hexanoil]amino]hexanoil]Lys, Quím. 27: **Fórmula** N{Épsilon-27}-[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxi-4-(19- carboxinonadecanoilamino)butanoil]amino]hexanoil]amino]hexanoil]-[Aib8,Glu22,Arg26,Lys27,Arg34]-GLP-1- (7-37)-peptidil-Gly-Gly-Gly-Ser-N{Épsilon}[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxi-4-(19- carboxinonadecanoilamino)butanoil]amino]hexanoil]amino]hexanoil]Lys, Quím. 28: **Fórmula** Nα([Aib8,Glu22,Arg26,Arg34]-GLP-1-(7-37)-peptidil)-N{Épsilon}[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(21- carboxihenicosanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi]a cetil]Lys-Gly-Gly-Ser-N{Épsilon}[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(21- carboxihenicosanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi]a cetil]Lys, Quím. 29: **Fórmula** Nα([Aib8,Glu22,Arg26,Arg34]-GLP-1-(7-37)-peptidil)-N{Épsilon}3-[2-[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]etoxi]etoxi]propanoilLys -Gly-Gly-Ser-N{Épsilon}3-[2-[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]etoxi]etoxi]propanoilLys , Quím. 30: **Fórmula** Nα([Aib8,Glu22,Arg26,Arg34]-GLP-1-(7-37)-peptidil)-N{Épsilon}[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]Lys-Ser-Pro-Glu-N{Épsilon}[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]Lys, Quím. 31: **Fórmula** Nα([Aib8,Glu22,Arg26,Arg34]-GLP-1-(7-37)-peptidil)-N{Épsilon}[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]Lys-Pro-Glu-Gly-N{Épsilon}[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]Lys, Quím. 32: **Fórmula** Nα([Aib8,Glu22,Arg26,Arg34]-GLP-1-(7-37)-peptidil)-N{Épsilon}[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]Lys-Ser-Ala-Glu-N{Épsilon}[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]Lys, Quím. 33: **Fórmula** N{Épsilon-36}-[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] 20 acetil]-[Aib8,Glu22,Arg26,Arg34,Lys36]-GLP-1-(7-37)-peptidil-Ala-Glu-Ser-Pro-N{Épsilon}[2-[2-[2-[[2-[2-[2- [[(4S)-4-carboxi-4-[[4-[(19- carboxinonadecanoilamino)metil]ciclohexanecarbonil]amino]butanoil]amino]etoxi]etoxi]acetil]amino]etoxi]etoxi] acetil]Lys, Quím. 34: **Fórmula**