公开(公告)号：US20240317676A1

公开(公告)日：2024-09-26

申请号：US18433950

申请日：2024-02-06

申请人： REATA PHARMACEUTICALS HOLDINGS, LLC

发明人： Eric ANDERSON ,  Xin JIANG ,  Melean VISNICK

IPC分类号： C07C255/47 ,  C07C271/24 ,  C07C275/26 ,  C07C275/34 ,  C07C311/07 ,  C07C311/09 ,  C07C311/10 ,  C07D209/56 ,  C07D211/44 ,  C07D231/12 ,  C07D261/08 ,  C07D261/20 ,  C07D295/195 ,  C07D295/215 ,  C07D307/20 ,  C07D333/34 ,  C07D487/08 ,  C07J63/00

CPC分类号： C07C255/47 ,  C07C271/24 ,  C07C275/26 ,  C07C275/34 ,  C07C311/07 ,  C07C311/09 ,  C07C311/10 ,  C07D209/56 ,  C07D211/44 ,  C07D231/12 ,  C07D261/08 ,  C07D261/20 ,  C07D295/195 ,  C07D295/215 ,  C07D307/20 ,  C07D333/34 ,  C07D487/08 ,  C07J63/008 ,  C07C2603/52

摘要： This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula:




wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

公开(公告)号：US12091389B2

公开(公告)日：2024-09-17

申请号：US17232321

申请日：2021-04-16

申请人： Temple University—Of The Commonwealth System of Higher Education ,  CONSEJO SUPERIOR DE INVESTIGACIONES CIENTÍFICAS ,  University of North Carolina Greensboro

发明人： Mary Ellen Abood ,  Eugen Brailoiu ,  Luciana Magalhaes Leo ,  Pingwei Zhao ,  Nadine Jagerovic ,  Ana Lago Fernández ,  Paula Morales Lazaro ,  Patricia Hodapp Reggio ,  Dow Preston Hurst ,  Nouroddin Sotoudeh Chafi

IPC分类号： C07D231/12 ,  C07D401/04

CPC分类号： C07D231/12 ,  C07D401/04

摘要： The present invention relates to pyrazolylbenzene-1,3-diols as cannabidiol derivatives, its use for the manufacture of a medicament, and more particularly, to the use of this medicament for the treatment and/or prevention of a disorder associated with the GPR18 and/or TRPV1 receptors and the use of these compounds for pharmacological assays related to GPR18 and/or TRPV1.

公开(公告)号：US12054493B2

公开(公告)日：2024-08-06

申请号：US17143326

申请日：2021-01-07

申请人： ENANTA PHARMACEUTICALS, INC.

发明人： Yao-Ling Qiu ,  Xuri Gao ,  Wei Li ,  Hui Cao ,  Meizhong Jin ,  Jorden Kass ,  Xiaowen Peng ,  Yat Sun Or

IPC分类号： C07D493/08 ,  A61K31/167 ,  A61K31/18 ,  A61K31/196 ,  A61K31/215 ,  A61K31/223 ,  A61K31/277 ,  A61K31/325 ,  A61K31/335 ,  A61K31/336 ,  A61K31/341 ,  A61K31/351 ,  A61K31/357 ,  A61K31/365 ,  A61K31/39 ,  A61K31/401 ,  A61K31/41 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4164 ,  A61K31/421 ,  A61K31/426 ,  A61K31/439 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/4425 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/655 ,  C07B59/00 ,  C07C235/56 ,  C07C311/53 ,  C07C317/32 ,  C07C317/44 ,  C07C323/42 ,  C07C323/62 ,  C07D207/16 ,  C07D211/54 ,  C07D213/52 ,  C07D213/81 ,  C07D213/89 ,  C07D231/12 ,  C07D233/64 ,  C07D257/04 ,  C07D261/02 ,  C07D261/08 ,  C07D261/20 ,  C07D263/52 ,  C07D277/26 ,  C07D295/088 ,  C07D303/26 ,  C07D303/34 ,  C07D307/32 ,  C07D307/33 ,  C07D309/08 ,  C07D313/04 ,  C07D317/72 ,  C07D327/10 ,  C07D401/04 ,  C07D451/04 ,  C07D493/04

CPC分类号： C07D493/08 ,  A61K31/167 ,  A61K31/18 ,  A61K31/196 ,  A61K31/215 ,  A61K31/223 ,  A61K31/277 ,  A61K31/325 ,  A61K31/335 ,  A61K31/336 ,  A61K31/341 ,  A61K31/351 ,  A61K31/357 ,  A61K31/365 ,  A61K31/39 ,  A61K31/401 ,  A61K31/41 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4164 ,  A61K31/421 ,  A61K31/426 ,  A61K31/439 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/4425 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/655 ,  C07B59/001 ,  C07C235/56 ,  C07C311/53 ,  C07C317/32 ,  C07C317/44 ,  C07C323/42 ,  C07C323/62 ,  C07D207/16 ,  C07D211/54 ,  C07D213/52 ,  C07D213/81 ,  C07D213/89 ,  C07D231/12 ,  C07D233/64 ,  C07D257/04 ,  C07D261/02 ,  C07D261/08 ,  C07D261/20 ,  C07D263/52 ,  C07D277/26 ,  C07D295/088 ,  C07D303/26 ,  C07D303/34 ,  C07D307/32 ,  C07D307/33 ,  C07D309/08 ,  C07D313/04 ,  C07D317/72 ,  C07D327/10 ,  C07D401/04 ,  C07D451/04 ,  C07D493/04 ,  C07B2200/05 ,  C07B2200/07 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/44 ,  C07C2602/46 ,  C07C2603/74

摘要： The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:

X-A-Y-L-R  (I)

which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

公开(公告)号：US20240226026A1

公开(公告)日：2024-07-11

申请号：US18551704

申请日：2022-03-23

申请人： ModernaTX, Inc.

发明人： Kerry E. BENENATO ,  Mark CORNEBISE ,  Edward HENNESSY ,  Mohindra SEEPERSAUD ,  Michael W. DANNEMAN

IPC分类号： A61K9/51 ,  C07C233/36 ,  C07C233/62 ,  C07C233/78 ,  C07C311/32 ,  C07D205/04 ,  C07D207/16 ,  C07D213/74 ,  C07D231/12 ,  C07D271/07 ,  C07D285/10 ,  C07D307/24 ,  C07D309/08

CPC分类号： A61K9/5123 ,  C07C233/36 ,  C07C233/62 ,  C07C233/78 ,  C07C311/32 ,  C07D205/04 ,  C07D207/16 ,  C07D213/74 ,  C07D231/12 ,  C07D271/07 ,  C07D285/10 ,  C07D307/24 ,  C07D309/08

摘要： The disclosure features novel lipids and compositions involving the same. Lipid nanoparticles (e.g., empty LNPs or loaded LNPs) include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Lipid nanoparticles (e.g., empty LNPs or loaded LNPs) further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

公开(公告)号：US12030877B2

公开(公告)日：2024-07-09

申请号：US17538442

申请日：2021-11-30

申请人： University of Kentucky Research Foundation

发明人： Chang-Guo Zhan ,  Fang Zheng ,  Kai Ding ,  Ziyuan Zhou

IPC分类号： C07D417/06 ,  C07C205/42 ,  C07C255/41 ,  C07D207/452 ,  C07D231/12 ,  C07D251/20 ,  C07D277/34 ,  C07D403/06 ,  C07D417/04

CPC分类号： C07D417/06 ,  C07C205/42 ,  C07C255/41 ,  C07D207/452 ,  C07D231/12 ,  C07D251/20 ,  C07D277/34 ,  C07D403/06 ,  C07D417/04

摘要： Compounds and compositions are provided that can inhibit microsomal prostaglandin E synthase-1 (mPGES-1). The compounds and compositions can reduce inflammation in a subject, such as inflammation caused by an inflammation disorder or symptoms thereof. Pharmaceutical compositions comprising the compound are also provided. Furthermore, methods are provided for reducing inflammation and/or inhibiting mPGES-1. The methods can comprise administering an effective amount of the composition to a subject.

公开(公告)号：US12023333B2

公开(公告)日：2024-07-02

申请号：US17609177

申请日：2020-05-07

申请人： GREY WOLF THERAPEUTICS LIMITED

发明人： Martin Quibell ,  Jason John Shiers ,  Michael Sparenberg

IPC分类号： A61K31/505 ,  A61K31/192 ,  A61K31/277 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/402 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/422 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/50 ,  A61K45/06 ,  A61P37/02 ,  C07C311/29 ,  C07D207/325 ,  C07D207/327 ,  C07D207/335 ,  C07D213/42 ,  C07D213/56 ,  C07D213/57 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D249/08 ,  C07D257/04 ,  C07D263/32 ,  C07D275/02 ,  C07D277/28 ,  C07D277/30 ,  C07D307/52 ,  C07D333/20 ,  C07D333/22 ,  C07D333/24 ,  C07D333/38 ,  C07D401/10 ,  C07D403/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

CPC分类号： A61K31/505 ,  A61K31/192 ,  A61K31/277 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/402 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/422 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/50 ,  A61K45/06 ,  A61P37/02 ,  C07C311/29 ,  C07D207/325 ,  C07D207/327 ,  C07D207/335 ,  C07D213/42 ,  C07D213/56 ,  C07D213/57 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D249/08 ,  C07D257/04 ,  C07D263/32 ,  C07D275/02 ,  C07D277/28 ,  C07D277/30 ,  C07D307/52 ,  C07D333/20 ,  C07D333/22 ,  C07D333/24 ,  C07D333/38 ,  C07D401/10 ,  C07D403/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO2— or —SO2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R1 is H or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, C land alkyl; R4 is selected from H and halo; R5 is selected from H, alkyl, haloalkyl, SO2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl, SO2NR12R13, heteroaryl, CONR10R11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R8 is selected from H, alkyl, haloalkyl and halo; and R9 is H, alkyl or halo; R10 and R11 are each independently H or alkyl; and R12 and R13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (1a) and (1b).

公开(公告)号：US12006293B1

公开(公告)日：2024-06-11

申请号：US18545056

申请日：2023-12-19

申请人： KING FAISAL UNIVERSITY

发明人： Saad Shaaban ,  Amr Negm

IPC分类号： C07D231/12 ,  A61K31/4155 ,  A61K31/4375 ,  C07D213/65 ,  C07D401/14

CPC分类号： C07D231/12 ,  A61K31/4155 ,  A61K31/4375 ,  C07D213/65 ,  C07D401/14

摘要： Diselenide organo compounds, their synthesis, and their use as deubiquitination signaling pathway modulators and anti-cancer agents.

公开(公告)号：US20240182426A1

公开(公告)日：2024-06-06

申请号：US18482475

申请日：2023-10-06

申请人： Epizyme, Inc.

发明人： Richard CHESWORTH ,  Lorna Helen Mitchell ,  Gideon Shapiro ,  Kerren Kalai Swinger

IPC分类号： C07D231/12 ,  A61K31/415 ,  A61K31/4155 ,  C07D401/04 ,  C07D403/04 ,  C07D403/08 ,  C07D405/04 ,  C07D405/08 ,  C07D405/12 ,  C07D493/10

CPC分类号： C07D231/12 ,  A61K31/415 ,  A61K31/4155 ,  C07D401/04 ,  C07D403/04 ,  C07D403/08 ,  C07D405/04 ,  C07D405/08 ,  C07D405/12 ,  C07D493/10

摘要： Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.

公开(公告)号：US20240166612A1

公开(公告)日：2024-05-23

申请号：US18275880

申请日：2022-02-18

申请人： X-Biotix Therapeutics, Inc.

发明人： Michael Dominic RYAN ,  Alastair PARKES ,  Olivier Rémi BARBEAU ,  Adele FAULKNER ,  Maisie HOLBROW-WILSHAW ,  Michelle SOUTHEY ,  Angelo SANZONE ,  Christophe BOLDRON ,  Elise GADOULEAU ,  Timothy GORMAN ,  Kate SPEAR ,  Thomas Martin KRULLE ,  Vasileios ROUMPELAKIS ,  Spencer Charles Robert NAPIER

IPC分类号： C07D271/113 ,  A61P31/04 ,  C07C323/41 ,  C07D205/04 ,  C07D211/58 ,  C07D231/12 ,  C07D231/56 ,  C07D233/64 ,  C07D249/14 ,  C07D257/04 ,  C07D263/32 ,  C07D265/30 ,  C07D271/06 ,  C07D285/135 ,  C07D295/185 ,  C07D413/12 ,  C07D413/14

CPC分类号： C07D271/113 ,  A61P31/04 ,  C07C323/41 ,  C07D205/04 ,  C07D211/58 ,  C07D231/12 ,  C07D231/56 ,  C07D233/64 ,  C07D249/14 ,  C07D257/04 ,  C07D263/32 ,  C07D265/30 ,  C07D271/06 ,  C07D285/135 ,  C07D295/185 ,  C07D413/12 ,  C07D413/14 ,  C07B2200/05

摘要： The invention provides arylthioether acetamide and related compounds, pharmaceutical compositions, and their use in the treatment of medical conditions, such as bacterial infections, and in inhibiting LpxA activity.

公开(公告)号：US20240158414A1

公开(公告)日：2024-05-16

申请号：US17767465

申请日：2020-10-09

申请人： Janssen Biotech, Inc.

发明人： Justin Cisar ,  Scott Kuduk ,  Lindsey DeRatt ,  Yvan Rene Ferdinand Simonnet

IPC分类号： C07D498/04 ,  A61P35/02 ,  C07D213/56 ,  C07D213/61 ,  C07D213/81 ,  C07D231/12 ,  C07D233/64 ,  C07D233/90 ,  C07D237/08 ,  C07D241/12 ,  C07D241/18 ,  C07D249/08 ,  C07D263/32 ,  C07D271/10 ,  C07D277/30 ,  C07D285/08 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

CPC分类号： C07D498/04 ,  A61P35/02 ,  C07D213/56 ,  C07D213/61 ,  C07D213/81 ,  C07D231/12 ,  C07D233/64 ,  C07D233/90 ,  C07D237/08 ,  C07D241/12 ,  C07D241/18 ,  C07D249/08 ,  C07D263/32 ,  C07D271/10 ,  C07D277/30 ,  C07D285/08 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： Disclosed are compounds, compositions and methods for treating diseases, disorders, or medical conditions that are affected by the modulation of DHODH. Such compounds are represented by Formula I as follows:




wherein R1, R2, R3, and Q are defined herein.