Xin Chen

US Patent:

20230001215, Jan 5, 2023

Filed:

Sep 14, 2022

Appl. No.:

17/932242

Inventors:

- Minneapolis MN, US
Becky L. Dolan - Chisago MN, US
Xin Chen - West Haven CT, US
Thomas A. Anderson - New Hope MN, US
Berthold Stegemann - Kassel, DE
Maurice Verbeek - Geleen, NL
Michael D. Eggen - Chisago City MN, US

International Classification:

A61N 1/375
A61N 1/05
A61N 1/368
A61N 1/362

Abstract:

A pacemaker has a housing and a therapy delivery circuit enclosed by the housing for generating pacing pulses for delivery to a patient's heart. An electrically insulative distal member is coupled directly to the housing and at least one non-tissue piercing cathode electrode is coupled directly to the insulative distal member. A tissue piercing electrode extends away from the housing.

US Patent:

20200055825, Feb 20, 2020

Filed:

Oct 17, 2019

Appl. No.:

16/656526

Inventors:

- New Haven CT, US
Hanqing Dong - Madison CT, US
Jing Wang - Milford CT, US
Xin Chen - Trumbull CT, US
Yimin Qian - Plainsboro NJ, US
Kurt Zimmermann - Durham CT, US
Craig M. Crews - New Haven CT, US
Michael Berlin - Flemington NJ, US
Lawrence Snyder - Killingworth CT, US

International Classification:

C07D 233/86
C07D 417/14
C07D 413/12
C07D 417/12
C07D 413/14
A61K 45/06
C07D 491/107
C07D 471/10
C07D 235/02
C07D 401/04
C07D 401/08
C07C 255/54
C07D 237/24
C07C 271/24
C07D 241/28
C07D 239/42
C07D 231/14
C07D 213/82
A61K 31/4166
A61K 47/54
A61K 31/4439
A61K 31/4188
A61K 31/435
A61K 31/454
A61K 31/4184
A61K 31/277

Abstract:

The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.

US Patent:

20180346461, Dec 6, 2018

Filed:

Jul 27, 2018

Appl. No.:

16/048191

Inventors:

- New Haven CT, US
Hanqing Dong - Madison CT, US
Jing Wang - Milford CT, US
Xin Chen - Trumbull CT, US
Yimin Qian - Plainsboro NJ, US
Kurt Zimmermann - Durham CT, US
Craig M. Crews - New Haven CT, US
Michael Berlin - Flemington NJ, US
Lawrence Snyder - Killingworth CT, US

International Classification:

C07D 417/14
A61P 25/28
A61P 35/00
C07K 5/078
C07D 413/14
C07D 417/12
C07D 471/10
C07D 491/107
C07D 401/04
C07D 233/86
C07D 413/12
A61K 45/06

Abstract:

The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.

US Patent:

20170327469, Nov 16, 2017

Filed:

Jul 28, 2017

Appl. No.:

15/663273

Inventors:

- New Haven CT, US
Hanqing Dong - Madison CT, US
Jing Wang - Milford CT, US
Caterina Ferraro - Stamford CT, US
Xin Chen - Trumbull CT, US
Yimin Qian - Plainsboro NJ, US

International Classification:

C07D 233/86
C07D 471/10
C07D 401/08
C07D 401/04
C07D 241/28
C07D 239/42
C07D 237/24
C07D 235/02
C07D 231/14
C07D 213/82
C07C 271/24
C07C 255/54
A61K 45/06
A61K 31/454
A61K 31/4439
A61K 31/435
A61K 31/4188
A61K 31/4184
A61K 31/4166
A61K 31/277
A61K 47/54
C07D 491/107
C07C 2601/04

Abstract:

The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.

US Patent:

20160214972, Jul 28, 2016

Filed:

Jan 20, 2016

Appl. No.:

15/002303

Inventors:

- New Haven CT, US
Andrew P. Crew - Guilford CT, US
Hanqing Dong - Madison CT, US
Jing Wang - Milford CT, US
Kam Siu - Milford CT, US
Caterina Ferraro - Stamford CT, US
Xin Chen - Trumbull CT, US
Yimin Qian - Plainsboro NJ, US

International Classification:

C07D 417/14
C07D 413/14
A61K 31/422
A61K 31/4439
C07D 417/12
A61K 45/06
A61K 31/4545
C07D 233/86
C07D 401/04
C07D 491/107
C07D 471/10
A61K 31/427
C07D 413/12

Abstract:

The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.

US Patent:

20150291562, Oct 15, 2015

Filed:

Apr 14, 2015

Appl. No.:

14/686640

Inventors:

- New Haven CT, US
Craig Crews - New Haven CT, US
Hanqing Dong - Madison WI, US
Jing Wang - Milford CT, US
Yimin Qian - Plainsboro NJ, US
Kam Siu - Milford CT, US
Caterina Ferraro - Stamford CT, US
Meizhong Jin - East Northport NY, US
Xin Chen - Trumbull CT, US

International Classification:

C07D 401/14
C07K 14/72
G01N 33/573
C12N 9/18
A61K 47/48
A61K 45/06
C12N 9/12
C07K 14/47

Abstract:

The description relates to imide-based compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.