公开(公告)号：US20240270780A1

公开(公告)日：2024-08-15

申请号：US17922514

申请日：2021-04-29

申请人： TAI BI DI PHARMACEUTICAL TECHNOLOGY (SHIJIAZHUANG) CO. LTD

发明人： Jinxu Wang ,  Xiangdong Su ,  Mingjie Bai

IPC分类号： C07H15/26 ,  A61K31/7056 ,  A61K31/7064 ,  A61P35/00

CPC分类号： C07H15/26 ,  A61K31/7056 ,  A61K31/7064 ,  A61P35/00

摘要： The present invention is based on the discovery of a proteolysis targeting compound having tissue targeting capability and use thereof, relating to medicinal products, and to such a compound or a pharmaceutically acceptable salt thereof, a stereoisomer, a solvate, or a polymorph. The compound is a proteolysis targeting chimera (PROTAC) with specific tissue targeting ability. The compound structure comprises three parts, i.e., A-BD-CON, wherein the part A is a PROTAC, one end of the structure thereof is a target protein ‘binding ligand, and the other end is a ubiquitin ligase ligand; and the part CON is a ligand of an asialoglycoprotein receptor (ASGPR), enabling the specific tissue targeting function. The compound enriches in liver tissue and is able to target cells in the tissue. The invention achieves improved druggability of the PROTAC with higher solubility and cellular membrane permeability, therefore produces enhanced pharmaceutical effect on the specific target tissue.

公开(公告)号：US20240247030A1

公开(公告)日：2024-07-25

申请号：US18509211

申请日：2023-11-14

申请人： Seagen Inc.

发明人： Patrick J. BURKE ,  Scott JEFFREY ,  Joseph Z. HAMILTON

IPC分类号： C07K7/06 ,  A61K45/06 ,  A61K47/54 ,  A61K47/64 ,  A61K47/68 ,  C07H15/26 ,  C07K5/117 ,  C07K7/02 ,  C07K16/28

CPC分类号： C07K7/06 ,  A61K45/06 ,  A61K47/545 ,  A61K47/6415 ,  A61K47/6817 ,  A61K47/6849 ,  A61K47/6889 ,  C07H15/26 ,  C07K5/1024 ,  C07K7/02 ,  C07K16/2875 ,  C07K16/2878 ,  C07K16/2881 ,  C07K2317/24

摘要： Compounds and compositions are disclosed in which a quaternized drug unit is linked to a targeting ligand unit from which a tertiary amine-containing drug is released at the targeted site of action.
Methods for treating diseases characterized by the targeted abnormal cells, such as cancer or an autoimmune disease using the compounds and compositions of the invention are also disclosed.

公开(公告)号：US11884672B2

公开(公告)日：2024-01-30

申请号：US15931256

申请日：2020-05-13

申请人： Vertex Pharmaceuticals Incorporated

发明人： Upul Keerthi Bandarage ,  Cavan McKeon Bligh ,  Diane Boucher ,  Michael John Boyd ,  Michael Aaron Brodney ,  Michael Philip Clark ,  Veronique Damagnez ,  Lev Tyler Dewey Fanning ,  Robert Francis Fimognari ,  Gabrielle Simone Fleming ,  Kevin James Gagnon ,  Pedro Manuel Garcia Barrantes ,  Robert Daniel Giacometti ,  Simon Giroux ,  Ronald Lee Grey, Jr. ,  Samantha Guido ,  Amy Beth Hall ,  Sarah Carol Hood ,  Dennis James Hurley ,  Mac Arthur Johnson, Jr. ,  Peter Jones ,  Sarathy Kesavan ,  Mei-Hsiu Lai ,  Siying Liu ,  Adam Looker ,  Brad Maxwell ,  John Patrick Maxwell ,  Ales Medek ,  Philippe Marcel Nuhant ,  Kirk Alan Overhoff ,  Setu Roday ,  Stefanie Roeper ,  Steven M. Ronkin ,  Rupa Sawant ,  Yi Shi ,  Muna Shrestha ,  Marisa Sposato ,  Kathy Stavropoulos ,  Rebecca Jane Swett ,  Timothy Lewis Tapley ,  Qing Tang ,  Stephen Thomson ,  Jinwang Xu ,  Mariam Zaky ,  Kevin Michael Cottrell

IPC分类号： C07D487/04 ,  A61K9/16 ,  A61K31/4162 ,  C07D491/18 ,  C07D513/04 ,  C07D519/00 ,  C07F9/6561 ,  C07H15/26

CPC分类号： C07D487/04 ,  A61K9/1635 ,  A61K9/1652 ,  A61K31/4162 ,  C07D491/18 ,  C07D513/04 ,  C07D519/00 ,  C07F9/6561 ,  C07H15/26 ,  C07B2200/13

摘要： The disclosure provides compounds useful for treating alpha-1 antitrypsin deficiency (AATD), according to formula (I):




tautomers thereof, pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable salts of the tautomers, deuterated derivatives of the compounds, deuterated derivatives of the tautomers, and deuterated derivatives of the salts, solid forms of those compounds and processes for making those compounds.

公开(公告)号：US11858954B2

公开(公告)日：2024-01-02

申请号：US17392970

申请日：2021-08-03

申请人： H. Lundbeck A/S

发明人： Klaus Gjervig Jensen ,  Lisbet Kværnø ,  Morten Jørgensen ,  Martin Juhl ,  Heidi Lopez de Diego ,  Karin Fredholt ,  Frans Dennis Therkelsen ,  Tobias Gylling Frihed ,  Mikkel Fog Jacobsen

IPC分类号： C07H15/26

CPC分类号： C07H15/26 ,  C07B2200/13

摘要： The present invention relates to new solid forms of the compound (2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(((4aR,10aR)-7-hydroxy-1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinolin-6-yl)oxy)tetrahydro-2H-pyran-2-carboxylic acid with the formula (Id) below.




The compound of formula (Id) is a prodrug of a catecholamine for use in treatment of neurodegenerative diseases and disorders such as Parkinson's Disease.

公开(公告)号：US11827665B2

公开(公告)日：2023-11-28

申请号：US17385166

申请日：2021-07-26

申请人： H. Lundbeck A/S

发明人： Martin Juhl ,  Lisbet Kværnø ,  Mikkel Fog Jacobsen

IPC分类号： C07H15/26

CPC分类号： C07H15/26

摘要： The present invention relates to a process for manufacturing (2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(((4aR,10aR)-7-hydroxy-1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinolin-6-yl)oxy)tetrahydro-2H-pyran-2-carboxylic acid with the formula (Id) below and pharmaceutically acceptable salts thereof




The compound of formula (Id) is a prodrug of a catecholamine for use in treatment of neurodegenerative diseases and disorders such as Parkinson's Disease.
The invention also relates to a new intermediate of said process.

公开(公告)号：US11793823B2

公开(公告)日：2023-10-24

申请号：US17699784

申请日：2022-03-21

申请人： SyneuRx International (Taiwan) Corp.

发明人： Guochuan Emil Tsai ,  Yi-Wen Mao ,  Lu-Ping Lu ,  Wei-Hua Chang ,  Han-Yi Hsieh ,  Jhe Wei Hu ,  Tsai-Miao Shih ,  ChanHui Huang

IPC分类号： C07D207/34 ,  A61K31/7048 ,  A23L33/10 ,  A23L33/00 ,  A61P25/18 ,  A61K31/235 ,  A61K31/36 ,  A61K31/40 ,  A61K31/415 ,  A61K31/7034 ,  C07C69/90 ,  C07D231/14 ,  C07D317/68 ,  C07H15/22 ,  C07H15/26

CPC分类号： A61K31/7048 ,  A23L33/10 ,  A23L33/40 ,  A61K31/235 ,  A61K31/36 ,  A61K31/40 ,  A61K31/415 ,  A61K31/7034 ,  A61P25/18 ,  C07C69/90 ,  C07D207/34 ,  C07D231/14 ,  C07D317/68 ,  C07H15/22 ,  C07H15/26 ,  A23V2002/00

摘要： A compound of Formula (I):




or a pharmaceutically acceptable salt thereof, in which Ring X is a 3 to 7 membered monocyclic ring, at least one of R1, R2, R3, and R4 is OR5 or CH2OR5 and the other R1, R2, R3, and R4 each independently are halogen, OH, OR5, CH2OR5, CO2H, OC═OR6, (C═O)R6, R6, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, H, or absent. Also provided herein are therapeutic uses of the compound of Formula (I).

公开(公告)号：US20230331767A1

公开(公告)日：2023-10-19

申请号：US17758492

申请日：2021-01-07

申请人： Purdue Research Foundation

发明人： Spencer S. Gardeen ,  Philip Stewart Low

IPC分类号： C07J43/00 ,  C07H15/26 ,  C07J51/00 ,  A61P1/04

CPC分类号： C07J43/003 ,  A61P1/04 ,  C07H15/26 ,  C07J51/00

摘要： A compound of the formula (I): G1-L-G2, or a pharmaceutically acceptable salt, polymorph, prodrug, solvate or clathrate thereof, wherein G1 is a folate radical, an antifolate radical, or a folate analog radical; L is a linker; and G2 is a radical of a steroid; compositions comprising such compounds; and the use of such compounds and compositions to treat, for example, inflammation associated with a disease or disorder.

公开(公告)号：US11780873B2

公开(公告)日：2023-10-10

申请号：US17347744

申请日：2021-06-15

申请人： GLYCOMIMETICS, INC.

发明人： John L. Magnani ,  John M. Peterson ,  Myung-Gi Baek

IPC分类号： C07H15/207 ,  A61K31/7034 ,  A61P35/04 ,  A61P1/04 ,  C07H7/06 ,  C07H15/26 ,  A61K47/60 ,  C07H7/04

CPC分类号： C07H7/06 ,  A61K31/7034 ,  A61K47/60 ,  A61P1/04 ,  A61P35/04 ,  C07H7/04 ,  C07H15/207 ,  C07H15/26

摘要： Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, highly potent multimeric E-selectin antagonist are desorbed and pharmaceutical compositions comprising at least one of the same.

公开(公告)号：US11780863B2

公开(公告)日：2023-10-10

申请号：US16183583

申请日：2018-11-07

申请人： Ventana Medical Systems, Inc.

发明人： Christopher Bieniarz ,  Julia Ashworth-Sharpe ,  Brian D. Kelly ,  Nathan Polaske

IPC分类号： C07F9/12 ,  C07H15/203 ,  C07H17/02 ,  C07H15/207 ,  C07F9/6561 ,  C07F9/6518 ,  C07F9/6558 ,  C07D209/14 ,  C07H15/26 ,  C07F9/58 ,  C07F9/6503 ,  C12Q1/42 ,  G01N33/58 ,  C07D403/06 ,  C07F9/6533 ,  C07F9/06

CPC分类号： C07F9/6561 ,  C07D209/14 ,  C07D403/06 ,  C07F9/06 ,  C07F9/12 ,  C07F9/58 ,  C07F9/6518 ,  C07F9/65031 ,  C07F9/65335 ,  C07F9/65583 ,  C07H15/203 ,  C07H15/207 ,  C07H15/26 ,  C07H17/02 ,  C12Q1/42 ,  G01N33/581

摘要： Disclosed herein are novel quinone methide analog precursors and embodiments of a method and a kit of using the same for detecting one or more targets in a biological sample. The method of detection comprises contacting the sample with a detection probe, then contacting the sample with a labeling conjugate that comprises an enzyme. The enzyme interacts with a quinone methide analog precursor comprising a detectable label, forming a reactive quinone methide analog, which binds to the biological sample proximally to or directly on the target. The detectable label is then detected. In some embodiments, multiple targets can be detected by multiple quinone methide analog precursors interacting with different enzymes without the need for an enzyme deactivation step.

公开(公告)号：US20230279041A1

公开(公告)日：2023-09-07

申请号：US18065503

申请日：2022-12-13

申请人： Hongene Biotech Corporation

发明人： Wing C. Poon ,  Xiaoyang Guan ,  David Yu ,  Ruiming Zou ,  Xiaojun Li ,  Michael Su ,  Gang Zhao ,  Gengyu Du ,  Yun-Chiao Yao

IPC分类号： C07H15/26 ,  C07H21/00

CPC分类号： C07H15/26 ,  C07H21/00

摘要： Embodiments of the present application relate to functionalized N-acetylgalactosamine-analogs, methods of making, and uses of the same. In particular, mono or trivalent N-acetylgalactosamine analogs may be prepared by utilizing a wide variety of linkers containing functional groups. These functionalized N-acetylgalactosamine-analogs may be used in the preparation of targeted delivery of oligonucleotide-based therapeutics.