公开(公告)号：WO2023043432A1

公开(公告)日：2023-03-23

申请号：PCT/US2021/050306

申请日：2021-09-14

Applicant: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY ,  KHDOUR, Omar ,  HECHT, Sidney ,  LIU, Jun ,  BANDYOPADHYAY, Indrajit

Inventor： KHDOUR, Omar ,  HECHT, Sidney ,  LIU, Jun ,  BANDYOPADHYAY, Indrajit

IPC: C07D279/18 ,  C07D279/20 ,  C07D417/04

Abstract: The invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 has any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as cytoprotective agents.

公开(公告)号：WO2023287793A1

公开(公告)日：2023-01-19

申请号：PCT/US2022/036829

申请日：2022-07-12

Applicant: GENENTECH, INC.

Inventor： GREEN, Samantha Alyson ,  GRANDNER, Jessica Marie ,  STABEN, Steven Thomas ,  AMARA, Neri ,  DIXIT, Vishva M. ,  VILLEMURE, Elisia

IPC: A61K31/553 ,  C07D267/14

Abstract: The invention provides a compound of formula (I): or a prodrug thereof, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 have any of the values described in the specification, as well as compositions comprising a compound of formula (I) or a prodrug thereof, or a pharmaceutically acceptable salt thereof. The compounds are agonists of glycolytic enzyme phosphofructokinase-1 liver type and are useful for treating diseases associated with the activity of glycolytic enzyme phosphofructokinase- 1 liver type, such as cancer, diabetes, sepsis, and septic shock.

公开(公告)号：WO2022182895A1

公开(公告)日：2022-09-01

申请号：PCT/US2022/017743

申请日：2022-02-24

Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY ,  REGENTS OF THE UNIVERSITY OF MICHIGAN ,  OMARY, Bishr ,  SHAVIT, Jordan Adam

Inventor： OMARY, Bishr ,  SHAVIT, Jordan Adam

IPC: A61K31/07 ,  A61K31/203 ,  A61K31/232 ,  A61P3/00

Abstract: The invention provides a method for treating or ameliorating the clinical manifestations of congenital erythropoietic porphyria in an animal (e.g. a human) by administering a retinoid to the animal.

公开(公告)号：WO2022120287A1

公开(公告)日：2022-06-09

申请号：PCT/US2021/062069

申请日：2021-12-06

Applicant: ARDELYX, INC. ,  ASTRAZENECA AB

Inventor： GUNNARSSON, Cecilia

IPC: A61K9/16 ,  A61K9/20 ,  A61K31/00

Abstract: The present invention provides a pharmaceutical tablet formulation of tenapanor that is chemically stable and soluble comprising greater than about 6% w/w of amorphous tenapanor in its bis-HCl form, an acidifying agent, an antioxidant, a disintegrant, a lubricant, a glidant, a filler, and an immediate release coating, wherein the total chloride content of the active ingredient is greater than 5.82% and the particle diameter distribution D50 is from about from about 18μm to about 22μm.

公开(公告)号：WO2022055995A1

公开(公告)日：2022-03-17

申请号：PCT/US2021/049461

申请日：2021-09-08

Applicant: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY

Inventor： WAGNER, Carl E. ,  JURUTKA, Peter W. ,  MARSHALL, Pamela A.

IPC: A01N43/90 ,  C07D213/73 ,  C07D213/74

Abstract: The invention provides compounds formula (I) and salts thereof: wherein R1-R2 have any of the values defined in the specification. The compounds are useful for treating conditions including Alzheimer' s disease, Parkinson' s disease, diabetes, cancer, inflammation, hyperresponsiveness, allergic conditions, asthma, and psychotic disorders such as schizophrenia. The compounds are also useful to lower IL-4, IL-5, or IL-15 levels in an animal.

公开(公告)号：WO2021178690A1

公开(公告)日：2021-09-10

申请号：PCT/US2021/020907

申请日：2021-03-04

Applicant: REGENTS OF THE UNIVERSITY OF MINNESOTA ,  DUDLEY, Samuel ,  GEORG, Gunda, Ingrid ,  JAKKARAJ, Sudhakar ,  CHERYALA, Narsihmulu

Inventor： DUDLEY, Samuel ,  GEORG, Gunda, Ingrid ,  JAKKARAJ, Sudhakar ,  CHERYALA, Narsihmulu

IPC: C07C205/02 ,  C07C211/03 ,  C07C233/03

Abstract: The invention provides a compound of formula (I): or a salt thereof, wherein A, B, R1, R2, R3 and X have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as therapeutic agents for treating diastolic dysfunction.

公开(公告)号：WO2020112845A1

公开(公告)日：2020-06-04

申请号：PCT/US2019/063356

申请日：2019-11-26

Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY ,  AUGERI, David J. ,  SABAAWY, Hatem ,  GILLERAN, John A.

Inventor： AUGERI, David J. ,  SABAAWY, Hatem ,  GILLERAN, John A.

IPC: A61K31/427 ,  A61K31/437 ,  C07D487/04

Abstract: The invention provides compounds of formula (16) and (17); and salts thereof, as well as compositions comprising such compounds and salts, complexes comprising such compounds and salts, and methods for treating cancer, inhibiting BMI1 expression, or treating Huntington's disease using such compounds, salts, and complexes. The compounds, salts, and complexes have potency, permeability, and oral bioavailability that make them particularly useful, for example, for the treatment of glioblastoma.

公开(公告)号：WO2019226915A1

公开(公告)日：2019-11-28

申请号：PCT/US2019/033788

申请日：2019-05-23

Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY ,  EBRIGHT, Richard H. ,  EBRIGHT, Yon W. ,  LIN, Chih-Tsung

Inventor： EBRIGHT, Richard H. ,  EBRIGHT, Yon W. ,  LIN, Chih-Tsung

IPC: A61K31/35 ,  A61K31/436 ,  A61K38/12

Abstract: The invention provides bipartite, dual-targeted inhibitors of bacterial RNA polymerase having the general structural formula (I): X-α -Y (I) wherein X is an moiety that binds to the Rif target of a bacterial RNA polymerase; Y is a moiety that binds to the bridge-helix N-terminus target of a bacterial RNA polymerase; and is a covalent bond or a linker. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.

公开(公告)号：WO2019046465A2

公开(公告)日：2019-03-07

申请号：PCT/US2018/048607

申请日：2018-08-29

Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY ,  FREUNDLICH, Joel S. ,  ALLAND, David ,  NEIDITCH, Matthew B. ,  INOYAMA, Daigo ,  CAPODAGLI, Glenn ,  KUMAR, Pradeep

Inventor： FREUNDLICH, Joel S. ,  ALLAND, David ,  NEIDITCH, Matthew B. ,  INOYAMA, Daigo ,  CAPODAGLI, Glenn ,  KUMAR, Pradeep

IPC: A61K31/541 ,  C07D417/10

CPC classification number: C07D209/42 ,  A61K31/404 ,  A61K31/4409 ,  A61K45/06 ,  C07D209/08 ,  C07D209/14 ,  C07D209/30 ,  C07D405/12 ,  A61K2300/00

Abstract: The invention provides compounds of formula I and salts thereof wherein R1-R4 have any of the meanings described in the specification. The compounds are useful for treating bacterial infections (e.g. tuberculosis).

公开(公告)号：WO2018039487A1

公开(公告)日：2018-03-01

申请号：PCT/US2017/048482

申请日：2017-08-24

Applicant: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY ,  HECHT, Sidney ,  KHDOUR, Omar ,  CHOWDHURY, Sandipan Roy ,  VISAVADIYA, Nishant P

Inventor： HECHT, Sidney ,  KHDOUR, Omar ,  CHOWDHURY, Sandipan Roy ,  VISAVADIYA, Nishant P

IPC: A61K31/54 ,  A61K31/5415 ,  A61P39/06 ,  C07D279/14

CPC classification number: C07D279/18 ,  A61K31/5415 ,  A61P3/10 ,  A61P9/00 ,  A61P25/28 ,  A61P35/00 ,  A61P39/06 ,  C07D279/14

Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables R 1 , R 2 , R 3 , R 4 , subscipt m and n, have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

Abstract translation: 本发明提供具有通式I的化合物及其药学上可接受的盐，其中变量R 1，R 2，R 4，R 5， R 3和R 4具有如本文所述的含义，以及含有这些化合物的组合物以及使用这些化合物和组合物的方法。