公开(公告)号：US20240360107A1

公开(公告)日：2024-10-31

申请号：US18687664

申请日：2022-08-30

申请人： ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA

发明人： Eli Chapman ,  Christopher Zerio

IPC分类号： C07D405/04 ,  A61K31/4709

CPC分类号： C07D405/04 ,  A61K31/4709

摘要： The present invention features inhibitors of the eIF4A enzyme. These inhibitors have a novel mechanism for inhibiting the eIF4A enzyme by occupying a binding pocket within the eIF4A RNA-binding groove, thereby perturbing RNA binding, blocking ATP hydrolysis, and, consequently, inhibiting RNA helicase activity. Thus, the compounds of the present invention are RNA-competitive, ATP-uncompetitive elF4A inhibitors that directly bind elF4A and inhibit the protein.

公开(公告)号：US20240360084A1

公开(公告)日：2024-10-31

申请号：US18633495

申请日：2024-04-11

申请人： REATA PHARMACEUTICALS, INC.

发明人： Xin JIANG ,  Melean VISNICK ,  Christopher F. BENDER ,  Gary BOLTON ,  Bradley CAPRATHE ,  Chitase LEE ,  Brian KORNBERG ,  Patrick O'BRIEN ,  Martha R. HOTEMA

IPC分类号： C07D231/54 ,  C07D235/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D409/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

CPC分类号： C07D231/54 ,  C07D235/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D409/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

摘要： Disclosed herein are compounds of the formula:




as well as analogs thereof, wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used to modulate the activity of IL-17 and RORγ. Also provided are methods of administering compounds and composition provided herein to a patient in need thereof, for example, for the treatment or prevention of diseases or disorders associated with inflammation or for autoimmune disorders.

公开(公告)号：US12129236B2

公开(公告)日：2024-10-29

申请号：US17204206

申请日：2021-03-17

申请人： CANCER RESEARCH TECHNOLOGY LIMITED

发明人： Alison E. McGonagle ,  Allan M. Jordan ,  Bohdan Waszkowycz ,  Colin P. Hutton ,  Ian D. Waddell ,  James R. Hitchin ,  Kate M. Smith ,  Niall M. Hamilton

IPC分类号： C07D235/26 ,  A61P35/00 ,  C07D307/85 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14

CPC分类号： C07D235/26 ,  A61P35/00 ,  C07D307/85 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14

摘要： The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity: wherein R1a, R1b, R1c, R1d, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.

公开(公告)号：US20240349605A1

公开(公告)日：2024-10-17

申请号：US18293874

申请日：2022-08-05

申请人： LG CHEM, LTD.

发明人： Minjun KIM ,  Dong Hoon LEE ,  Sang Duk SUH ,  Young Seok KIM ,  Da Jung LEE

IPC分类号： H10K85/60 ,  C07C211/54 ,  C07C211/61 ,  C07D209/86 ,  C07D307/91 ,  C07D333/76 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C09K11/06 ,  H10K50/11 ,  H10K101/00

CPC分类号： H10K85/6574 ,  C07C211/54 ,  C07C211/61 ,  C07D209/86 ,  C07D307/91 ,  C07D333/76 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C09K11/06 ,  H10K85/622 ,  H10K85/626 ,  H10K85/633 ,  H10K85/636 ,  H10K85/654 ,  H10K85/6576 ,  C07C2603/18 ,  C07C2603/26 ,  C07C2603/42 ,  C09K2211/1003 ,  C09K2211/1018 ,  H10K50/11 ,  H10K85/6572 ,  H10K2101/90

摘要： An organic light-emitting device. light emitting device having a light emitting layer including a compound of Chemical Formula 1 and a compound of Chemical Formula 2:




Ar1 and Ar2 are each independently a substituted or unsubstituted C6-60 aryl or C2-60 heteroaryl containing at least one of N, O and S, each Ar3 is independently hydrogen, deuterium, or a substituted or unsubstituted C6-60 aryl or C2-60 heteroaryl containing at least one of N, O and S, and at least one of Ar1, Ar2-Ar3 is a substituted or unsubstituted C16-60 aryl polycyclic aromatic ring,




Ar5 and Ar6 are each substituted or unsubstituted C6-60 aryl or C2-60 heteroaryl containing at least one of N, O and S, and the other substituents are as defined in the specification, provided that Ar3 is not




when Ar3 is an unsubstituted C16-60 aryl polycyclic aromatic ring.

公开(公告)号：US20240343752A1

公开(公告)日：2024-10-17

申请号：US18417409

申请日：2024-01-19

申请人： UNIVERSITÄT BERN

发明人： Christian Leumann ,  Damien Evequoz

IPC分类号： C07H19/048 ,  C07D405/04 ,  C07D473/18 ,  C07D473/34 ,  C07F7/18 ,  C07F9/6558 ,  C07F9/6561 ,  C07H19/16 ,  C07H21/00 ,  C12N15/113

CPC分类号： C07H19/048 ,  C07D405/04 ,  C07D473/18 ,  C07D473/34 ,  C07F7/1804 ,  C07F9/65586 ,  C07F9/65616 ,  C07H19/16 ,  C07H21/00 ,  C12N15/113 ,  C12N2310/11 ,  C12N2310/315 ,  C12N2310/3231 ,  C12N2320/33

摘要： Oligomers prepared from a bicyclic nucleoside having the formula (I) shown below:




in which each of T1 and T2 is independently OR1 or OR2; R1 is H or a hydroxyl protecting group, R2 is a phosphorus moiety; and Bx is a nucleobase. The compounds, bicyclic nucleosides and oligomers are useful for the prevention, treatment or diagnosis of muscular dystrophy.

公开(公告)号：US20240334813A1

公开(公告)日：2024-10-03

申请号：US18570822

申请日：2022-06-02

申请人： IDEMITSU KOSAN CO., LTD.

发明人： Masato MITANI ,  Tomokatsu KUSHIDA ,  Sayaka MIZUTANI ,  Masatoshi SAITO ,  Kei YOSHIDA ,  Yoshinori AOYAMA ,  Ryota TAKAHASHI

IPC分类号： H10K85/60 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  H10K50/16

CPC分类号： H10K85/622 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  H10K50/166 ,  H10K85/626 ,  H10K85/654 ,  H10K85/6574 ,  H10K85/6576

摘要： A compound represented by the following formula (1).

公开(公告)号：US20240327375A1

公开(公告)日：2024-10-03

申请号：US18560011

申请日：2022-05-13

申请人： Addex Pharma S.A.

发明人： Jean-Laurent Paparin ,  Jean-Philippe Rocher ,  Patrick Mäder ,  Tanja Stach ,  Guillaume Duvey ,  Lam Tang

IPC分类号： C07D401/04 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  C07D237/32 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D491/107 ,  C07D498/08

CPC分类号： C07D401/04 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  C07D237/32 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D491/107 ,  C07D498/08

摘要： The present invention relates to novel compounds of Formula (I), wherein A, m, Q, R1, R2, R3, R4 and R5 are defined as in Formula (I); which are negative allosteric modulators of the metabotropic glutamate receptor subtype 7 (mGlu7) and which are useful for the treatment or prevention of neurological, ear and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGlu7 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and such compositions, and to the use of such compounds for the prevention or treatment of neurological, ear and psychiatric disorders and diseases in which mGlu7 is involved.

公开(公告)号：US12108664B2

公开(公告)日：2024-10-01

申请号：US17259762

申请日：2019-07-16

申请人： Novaled GmbH

发明人： Elena Galan Garcia ,  Benjamin Schulze ,  Jens Wutke ,  Horst Hartmann

IPC分类号： H10K85/60 ,  C07D221/18 ,  C07D251/24 ,  C07D405/04 ,  H10K50/16

CPC分类号： H10K85/654 ,  C07D221/18 ,  C07D251/24 ,  C07D405/04 ,  H10K85/615 ,  H10K85/6572 ,  H10K85/6574 ,  H10K50/16

摘要： The present invention relates to an organic compound of formula (1), suitable for use as a layer material for electronic devices, and it relates to an organic semiconductor layer comprising at least one compound thereof, as well as to an organic electronic device comprising at least one organic semiconductor layer, and a method of manufacturing the same.

公开(公告)号：US20240307384A1

公开(公告)日：2024-09-19

申请号：US18593518

申请日：2024-03-01

申请人： CalciMedica, Inc.

发明人： Gonul VELICELEBI ,  Kenneth STAUDERMAN ,  Michael DUNN ,  Jack ROOS

IPC分类号： A61K31/497 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/421 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/485 ,  A61K31/506 ,  A61K45/06 ,  A61P1/18 ,  C07D401/04 ,  C07D405/04 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D491/04

CPC分类号： A61K31/497 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/421 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/485 ,  A61K31/506 ,  A61K45/06 ,  A61P1/18 ,  C07D401/04 ,  C07D405/04 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D491/04 ,  Y02A50/30

摘要： Compositions and methods related to the amelioration of pancreatitis through the pharmaceutical manipulation of calcium signaling are disclosed. Such compositions and methods may be used to ameliorate symptoms of acute or chronic pancreatitis or to reduce the chance or severity of pancreatitis in an individual at risk of the condition. In other embodiments, disclosed herein are compositions and methods related to the amelioration of viral diseases through the pharmaceutical manipulation of calcium signaling. In further embodiments, disclosed herein are compositions and methods related to the amelioration of Th17-induced diseases through the pharmaceutical manipulation of calcium signaling.

公开(公告)号：US20240300926A1

公开(公告)日：2024-09-12

申请号：US18569407

申请日：2022-05-11

申请人： LG CHEM, LTD.

发明人： Minjun KIM ,  Dong Hoon LEE ,  Sang Duk SUH ,  Young Seok KIM ,  Donghee KIM ,  Joongsuk OH ,  Da Jung LEE

IPC分类号： C07D405/04 ,  C07D405/10 ,  C07D409/14 ,  C09K11/06 ,  H10K50/11 ,  H10K85/60

CPC分类号： C07D405/04 ,  C07D405/10 ,  C07D409/14 ,  C09K11/06 ,  H10K50/11 ,  H10K85/622 ,  H10K85/654 ,  H10K85/6574 ,  C09K2211/1066

摘要： A compound of Chemical Formula 1 and an organic light emitting device including the same:




wherein: Ar1 is unsubstituted benzophenanthrenyl, chrysenyl, or fluoranthenyl; Ar2 is a substituted or unsubstituted C6-60 aryl, or a substituted or unsubstituted C6-60 heteroaryl containing any one or more of N, O and S; L1, L2, and L3 each independently is a direct bond or a substituted or unsubstituted C6-60 arylene; and R1 and R2 are each independently hydrogen, deuterium, a substituted or unsubstituted C1-12 alkyl, or a substituted or unsubstituted C6-14 aryl. The compound of Chemical Formula 1 can be used as a material for an organic material layer of an organic light emitting device for hole injection, hole transport, hole injection and transport, electron blocking, light emission, electron transport, or electron injection, and can improve the efficiency, achieve low driving voltage and/or improve lifetime characteristics of the device.