公开(公告)号：US20220024981A1

公开(公告)日：2022-01-27

申请号：US17296679

申请日：2019-11-26

Applicant: Novartis AG

Inventor： Alec Nathanson FLYER ,  Andrei Alexandrovich GOLOSOV ,  Philipp GROSCHE ,  Ian LEWIS ,  Eugene Yuejin LIU ,  Andreas MARZINZIK ,  Lauren Gilchrist MONOVICH ,  Johannes OTTL ,  Tajesh Jayprakash PATEL ,  Patrick Crawford REID ,  Mohindra SEEPERSAUD

IPC: C07K7/64 ,  A61K38/12 ,  A61K45/06

Abstract: The disclosure relates to inhibitors of PCSK9 useful in the treatment of lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, or tautomer thereof, wherein R1, X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12, and X13 are described herein.

公开(公告)号：US20130028843A1

公开(公告)日：2013-01-31

申请号：US13649089

申请日：2012-10-10

Applicant: NOVARTIS AG

Inventor： Stefanie FLOHR ,  Stefan Andreas RANDL ,  Nils OSTERMANN ,  Ulrich HASSIEPEN ,  Frederic BERST ,  Ursula BODENDORF ,  Bernd GERHARTZ ,  Andreas MARZINZIK ,  Claus EHRHARDT ,  Josef Gottfried MEINGASSNER

IPC: C07D207/16 ,  C12N9/96 ,  A61K49/00 ,  G01N33/53 ,  G01N21/64 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/40 ,  A61K31/454 ,  C07D403/12 ,  A61K31/496 ,  C07D413/12 ,  A61K31/5377 ,  C07D217/26 ,  A61K31/472 ,  C07D211/60 ,  A61K31/445 ,  C07D405/12 ,  A61K31/4025 ,  C07D409/12 ,  C07D209/52 ,  A61K31/403 ,  A61P29/00 ,  A61P17/04 ,  A61P17/00 ,  A61P17/02 ,  A61P17/10 ,  A61P17/06 ,  A61P1/00 ,  A61P1/18 ,  A61P35/00 ,  G06F17/50 ,  C12N9/50

Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.

Abstract translation: 本发明涉及丝氨酸蛋白酶激肽释放酶7的晶体结构以及这种晶体结构在药物发现中的应用。 本发明还涉及特异性结合激素释放酶7的该活性位点的化合物。

公开(公告)号：US20250090699A1

公开(公告)日：2025-03-20

申请号：US18802972

申请日：2024-08-13

Applicant: Novartis AG

Inventor： Salvatore BONGARZONE ,  Davide CAMPORESE ,  Gonçalo dos Santos CLEMENTE ,  Takeru EHARA ,  Matteo FISCHER ,  Andrei Alexandrovich GOLOSOV ,  Philipp GROSCHE ,  Philipp HOLZER ,  Alexei KARPOV ,  Marion LACAUD-BAUMLIN ,  Lukas LEDER ,  Rafael Bermeo MALO ,  Andreas MARZINZIK ,  Yoshihide MIZUKOSHI ,  Charlie MUNSCH ,  Markus Oliver RESCHKE ,  Holger SELLNER ,  Therese-Marie STACHYRA

IPC: A61K51/08 ,  A61P35/00 ,  C07B59/00

Abstract: Described herein are cyclic peptides targeting fibroblast activation protein (FAP), and their incorporation into compounds for radioligand imaging and therapies, as well as methods and/or uses of such compounds for the imaging, treatment and/or prevention of FAP-implicated diseases and disorders.