公开(公告)号：US20240083961A1

公开(公告)日：2024-03-14

申请号：US18176172

申请日：2023-02-28

申请人： YALE UNIVERSITY

发明人： Joseph Schlessinger ,  Sangwon Lee

IPC分类号： C07K14/50

CPC分类号： C07K14/50 ,  C07K16/22

摘要： The present invention relates in one aspect to the discovery that β-Klotho is the primary cell-surface receptor for FGF21, with FGFR1c functioning as a catalytic subunit that ultimately mediates intracellular signaling. In one aspect, the invention provides compositions and methods that are useful in treating or preventing endocrine FGF-related diseases or disorders.

公开(公告)号：US10745490B2

公开(公告)日：2020-08-18

申请号：US15302342

申请日：2015-04-10

申请人： Celldex Therapeutics, Inc. ,  Yale University

发明人： Joseph Schlessinger ,  Diego Alvarado ,  Sangwon Lee

IPC分类号： C07K16/32 ,  A61K39/395 ,  G01N33/74 ,  A61K39/00

摘要： Provided herein are compositions, methods and uses involving antibodies that bind to ErbB, a receptor tyrosine kinase, and modulate the activity of ErbB. Also provided are uses and methods for treating disorders, such as cancer, by administering to subject an antibody that binds to ErbB.

公开(公告)号：US20240034762A1

公开(公告)日：2024-02-01

申请号：US18043894

申请日：2021-09-02

申请人： YALE UNIVERSITY

发明人： Joseph Schlessinger ,  Yoshihisa Suzuki ,  Irit Lax

IPC分类号： C07K14/50 ,  C12N15/63 ,  A61P5/00

CPC分类号： C07K14/50 ,  C12N15/63 ,  A61P5/00 ,  C07K2319/30

摘要： The present disclosure provides in one aspect a construct comprising the R2 region of FGF23. In other embodiments, the construct functions as a FGF23 antagonist by blocking FGF23 binding to α-Klotho and cell signaling via FGFR activation. In yet other embodiments, the construct prevents FGFR activation. In yet other embodiments, the construct of the present disclosure can be used to treat diseases or disorders related to FGF23 dysregulation and/or overexpression, such as but not limited to phosphate metabolism disorders.

公开(公告)号：US11365228B2

公开(公告)日：2022-06-21

申请号：US16624895

申请日：2018-07-05

申请人： YALE UNIVERSITY

发明人： Joseph Schlessinger ,  Sangwon Lee

IPC分类号： C07K14/50 ,  C07K16/22

摘要： The present invention relates, in one aspect, to certain mutant FGF21 polypeptide constructs. In certain non-limiting embodiments, the construct binds to β-Klotho more tightly than wild-type FGF21. In certain non-limiting embodiments, the construct has a mutation in at least one residue of SEQ ID NO:3 selected from the group consisting of V188, R203, and L194. In certain non-limiting embodiments, the construct further comprises a stability enhancing domain.

公开(公告)号：US20220112166A1

公开(公告)日：2022-04-14

申请号：US17500622

申请日：2021-10-13

申请人： YALE UNIVERSITY

发明人： William L. Jorgensen ,  Joseph Schlessinger

IPC分类号： C07D249/14 ,  A61K31/4196 ,  A61K45/06 ,  C07D401/12 ,  A61K31/4439 ,  C07D405/12 ,  C07D413/12 ,  A61K31/4245

摘要： The compounds of Formula I described herein regulate activity of JAK2 by specifically binding to the JAK2 pseudokinase domain, JH2, and are useful as therapeutic agents in the treatment or amelioration of myeloproliferative disorders. Also provided herein are methods of treating myeloproliferative disorders, and methods of making compounds of Formula I.

公开(公告)号：US20190151351A1

公开(公告)日：2019-05-23

申请号：US16150421

申请日：2018-10-03

申请人： Celldex Therapeutics, Inc. ,  Yale University

发明人： Joseph Schlessinger ,  Diego Alvarado ,  Phillip B. Murray

IPC分类号： A61K31/727 ,  A61K31/715 ,  A61K31/721 ,  C07K16/40 ,  A61K31/702 ,  G01N33/50 ,  A61K31/726 ,  A61K31/737 ,  A61K38/18 ,  C12Q1/48

摘要： Provided herein are ALK regulators for the treatment of diseases and disorders. For example, presented herein are ALK regulators, e.g., ALK activators, and methods of treatment and/or prevention of diseases, including neurodegenerative, neuromuscular and cognitive diseases or disorders, and methods of enhancing cognitive abilities using ALK regulators, e.g., ALK activators. Also provided herein are ALK regulators, e.g., ALK inhibitors, and methods of treatment and/or prevention of diseases such as hyperproliferative and neoplastic disorders associated with cells that express ALK, e.g., cells that exhibit increased or constitutive levels of ALK tyrosine phosphorylation using such ALK regulators, e.g., ALK inhibitors. Pharmaceutical compositions of said ALK regulators, e.g, ALK activators and inhibitors are likewise provided.

公开(公告)号：US12110278B2

公开(公告)日：2024-10-08

申请号：US17500622

申请日：2021-10-13

申请人： YALE UNIVERSITY

发明人： William L. Jorgensen ,  Joseph Schlessinger

IPC分类号： C07D249/14 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/4439 ,  A61K45/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12

CPC分类号： C07D249/14 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/4439 ,  A61K45/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12

摘要： The compounds of Formula I described herein regulate activity of JAK2 by specifically binding to the JAK2 pseudokinase domain, JH2, and are useful as therapeutic agents in the treatment or amelioration of myeloproliferative disorders. Also provided herein are methods of treating myeloproliferative disorders, and methods of making compounds of Formula I.

公开(公告)号：US20200331978A1

公开(公告)日：2020-10-22

申请号：US16772100

申请日：2018-12-12

申请人： YALE UNIVERSITY ,  ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI

发明人： Joseph Schlessinger ,  Sangwon Lee ,  Avner Schlessinger ,  Man-Un Ung

IPC分类号： C07K14/50

摘要： The present invention provides compositions and methods that are useful in treating or preventing endocrine FGF-related diseases or disorders, such as but not limited to dysfunctional phosphate homeostasis and chronic kidney disease (CKD).