IP Library Granted Patent US 12,433,880
Granted Patent B2
US 12,433,880 · App. 17/226,233 · Granted Oct 7, 2025

Methods for the treatment of neurological disorders

Inventors: Benjamin Matteson Vincent (Cambridge, MA); Daniel Forrest Tardiff (Arlington, MA); Jeff Scott Piotrowski (Somerville, MA); Eric Solis (Milford, MA); Robert Hughie Scannevin (Hopkinton, MA); Chee-Yeun Chung (Brookline, MA); Rebecca Aron (Cambridge, MA); Bertrand Le Bourdonnec (Northborough, MA); Matthew Lucas (Lexington, MA); Kenneth Rhodes (Belmont, MA)
Assignee: JANSSEN PHARMACEUTICA NV
A61K31/454A61K31/4545A61K45/06A61P25/14A61P25/16A61P25/28G01N33/6896G01N2333/46G01N2333/775G01N2800/28G01N2800/2814G01N2800/2821G01N2800/2828G01N2800/2835G01N2800/285
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 12,433,880
App. No.
17/226,233
Granted
Oct 7, 2025
Kind
B2
Abstract

The present disclosure provides compounds and methods useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.

Claims (23)

1. A method of treating a neurological disorder in a subject in need thereof, the method comprising administering an SCD inhibitor in an amount sufficient to suppress toxicity in a cell related to protein misfolding or aggregation, wherein the SCD inhibitor is selected from the group consisting of:

2. A method of suppressing toxicity in a cell related to protein misfolding or aggregation in a subject, the method comprising contacting a cell with an SCD inhibitor, wherein the SCD inhibitor is selected from the group consisting of:

3. The method of claim 2 , wherein the toxicity in the cell is related to protein aggregation related to misfolding of a protein.

4. The method of claim 1 , wherein the toxicity in the cell is related to misfolding or aggregation of α-synuclein or ApoE4.

5. The method of claim 2 , wherein the cell is a neural cell.

6. The method of claim 5 , wherein the neural cell is a neuron or glial cell.

7. The method of claim 1 , wherein the subject is predicted to have an elevated level of α-synuclein or ApoE4 based on genetic markers.

8. The method of claim 1 , wherein the neurological disorder is Alzheimer's disease (AD), mild cognitive impairment (MCI), cerebral amyloid angiopathy (CAA), dementia associated with Down syndrome, or other neurodegenerative diseases characterized by the formation or accumulation of amyloid plaques comprising Aβ42.

9. The method of claim 1 , wherein the neurological disorder is Alzheimer's disease (AD), Parkinson's disease (PD), dementia with Lewy bodies, amyotrophic lateral sclerosis or Lou Gehrig's disease, Alpers' disease, Leigh's disease, Pelizaeus-Merzbacher disease, Olivopontocerebellar atrophy, Friedreich's ataxia, leukodystrophies, Rett syndrome, Ramsay Hunt syndrome type II, Down's syndrome, multiple sclerosis, and mild cognitive impairment (MCI).

10. The method of claim 1 , wherein the neurological disorder is a proteopathy.

11. The method of claim 10 , wherein the proteopathy is a synucleinopathy.

12. The method of claim 11 , wherein the synucleinopathy is Parkinson's disease (PD), dementia with Lewy bodies, pure autonomic failure, multiple system atrophy, incidental Lewy body disease, pantothenate kinase-associated neurodegeneration, Alzheimer's disease, Down's Syndrome, Gaucher disease, or the Parkinsonism-dementia complex of Guam.

13. The method of claim 10 , wherein the proteopathy is AD, Alexander disease, amyotrophic lateral sclerosis (ALS), a prion disease, Huntington's disease, Machado-Joseph disease, Pick's disease, or frontotemporal dementia.

14. The method of claim 1 , wherein the method further comprises administering an additional therapeutic agent to the subject.

15. The method of claim 14 , wherein the additional therapeutic agent is a small molecule, an antibody or fragment thereof, or a nucleic acid.

16. The method of claim 14 , wherein the additional therapeutic agent is an antidepressant agent, an anxiolytic agent, an antipsychotic agent, a sedative, a dopamine promoter, or an anti-tremor agent.

17. The method of claim 1 , wherein the SCD inhibitor is:

18. The method of claim 1 , wherein the SCD inhibitor is:

19. The method of claim 1 , wherein the SCD inhibitor is:

20. The method of claim 1 , wherein the SCD inhibitor is:

21. The method of claim 1 , wherein the SCD inhibitor is:

22. The method of claim 1 , wherein the SCD inhibitor is:

23. The method of claim 1 , wherein the SCD inhibitor is:

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 19, 2022
From: YUMANITY THERAPEUTICS, INC.; YUMANITY, INC.
To: JANSSEN PHARMACEUTICA NV
Reel/Frame 062148/0414 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 13, 2022
From: VINCENT, BENJAMIN MATTESON; TARDIFF, DANIEL FORREST; PIOTROWSKI, JEFF SCOTT; SOLIS, ERIC; SCANNEVIN, ROBERT HUGHIE; CHUNG, CHEE-YEUN; ARON, REBECCA; LE BOURDONNEC, BERTRAND; LUCAS, MATTHEW; RHODES, KENNETH
To: YUMANITY THERAPEUTICS, INC.
Reel/Frame 061410/0407 →
Continuity (3)
Continuation 15863773 · Jan 5, 2018
Provisional Application 62443066 · Jan 6, 2017
Related Publication 20220040167A1 · Feb 10, 2022
References Cited (400)
US 4782071A · Butler et al. · 1988 [cited by applicant]
US 5780472A · Cho et al. · 1998 [cited by applicant]
US 6727247B2 · Flohr et al. · 2004 [cited by applicant]
US 7045290B2 · Lindquist et al. · 2006 [cited by applicant]
US 7074809B2 · Arora et al. · 2006 [cited by applicant]
US 7132424B2 · Picard · 2006 [cited by applicant]
US 7381749B2 · Malecha et al. · 2008 [cited by applicant]
US 7452670B2 · Muchowski et al. · 2008 [cited by applicant]
US 7767677B2 · Kamboj et al. · 2010 [cited by applicant]
US 7790408B1 · Ntambi et al. · 2010 [cited by applicant]
US 8044052B2 · Fay · 2011 [cited by applicant]
US 8063224B2 · Lachance et al. · 2011 [cited by applicant]
US 8129376B2 · Sundaresan et al. · 2012 [cited by applicant]
US 8207147B2 · Fyfe et al. · 2012 [cited by applicant]
US 8207199B2 · Aoki et al. · 2012 [cited by applicant]
US 8258160B2 · Dales et al. · 2012 [cited by applicant]
US 8314138B2 · Dales et al. · 2012 [cited by applicant]
US 8563539B2 · Baldino et al. · 2013 [cited by applicant]
US 8673917B2 · Zoller et al. · 2014 [cited by applicant]
US 8791136B2 · Goff et al. · 2014 [cited by applicant]
US 8822513B2 · Lu et al. · 2014 [cited by applicant]
US 8946225B2 · Dupont-Passelaigue et al. · 2015 [cited by applicant]
US 9266832B2 · Griffioen et al. · 2016 [cited by applicant]
US 9290465B2 · Derryberry et al. · 2016 [cited by applicant]
US 9296711B2 · Erickson et al. · 2016 [cited by applicant]
US 10941134B2 · Goff et al. · 2021 [cited by applicant]
US 10973810B2 · Vincent et al. · 2021 [cited by applicant]
US 20020019389A1 · Kim et al. · 2002 [cited by applicant]
US 20020133005A1 · Iino et al. · 2002 [cited by applicant]
US 20040023973A1 · Nagato et al. · 2004 [cited by applicant]
US 20040097483A1 · Zeng et al. · 2004 [cited by applicant]
US 20040127521A1 · Cai et al. · 2004 [cited by applicant]
US 20040146872A1 · Winther et al. · 2004 [cited by applicant]
US 20040167224A1 · Ozaki et al. · 2004 [cited by applicant]
US 20040226056A1 · Roch · 2004 [cited by examiner]
US 20050032859A1 · Chen · 2005 [cited by applicant]
US 20050119242A1 · DeLuca et al. · 2005 [cited by applicant]
US 20050256068A1 · McSwiggen et al. · 2005 [cited by applicant]
US 20060116382A1 · Yao et al. · 2006 [cited by applicant]
US 20060167044A1 · Arnaiz et al. · 2006 [cited by applicant]
US 20060270686A1 · Kelly et al. · 2006 [cited by applicant]
US 20070087363A1 · Bartel et al. · 2007 [cited by applicant]
US 20080015230A1 · Kamboj et al. · 2008 [cited by applicant]
US 20080021028A1 · Swinnen et al. · 2008 [cited by applicant]
US 20080132542A1 · Lachance et al. · 2008 [cited by applicant]
US 20080207587A1 · Kamboj et al. · 2008 [cited by applicant]
US 20080249100A1 · Chisholm et al. · 2008 [cited by applicant]
US 20080255130A1 · Koltun et al. · 2008 [cited by applicant]
US 20080255161A1 · Koltun et al. · 2008 [cited by applicant]
US 20080280891A1 · Kelly et al. · 2008 [cited by applicant]
US 20090098105A1 · Hopf et al. · 2009 [cited by applicant]
US 20090118296A1 · Black et al. · 2009 [cited by applicant]
US 20090149466A1 · Gillespie et al. · 2009 [cited by applicant]
US 20090163545A1 · Goldfarb · 2009 [cited by applicant]
US 20090170822A1 · DeLuca et al. · 2009 [cited by applicant]
US 20090170828A1 · Isabel et al. · 2009 [cited by applicant]
US 20090221597A1 · Hadida et al. · 2009 [cited by applicant]
US 20090239810A1 · Sundaresan et al. · 2009 [cited by applicant]
US 20090246137A1 · Hadida Ruah et al. · 2009 [cited by applicant]
US 20090253693A1 · Koltun et al. · 2009 [cited by applicant]
US 20090253738A1 · Koltun et al. · 2009 [cited by applicant]
US 20090325956A1 · Taniguchi et al. · 2009 [cited by applicant]
US 20100022486A1 · Bouillot et al. · 2010 [cited by applicant]
US 20100029722A1 · Dales et al. · 2010 [cited by applicant]
US 20100041696A1 · Daugan et al. · 2010 [cited by applicant]
US 20100160323A1 · Bischoff et al. · 2010 [cited by applicant]
US 20100210649A1 · Djaballah et al. · 2010 [cited by applicant]
US 20110319412A1 · Sakagami et al. · 2011 [cited by applicant]
US 20120010186A1 · Lachance et al. · 2012 [cited by applicant]
US 20120178678A1 · Dupont-Passelaigue et al. · 2012 [cited by applicant]
US 20120196844A1 · Alper et al. · 2012 [cited by applicant]
US 20120252850A1 · Milne et al. · 2012 [cited by applicant]
US 20120316182A1 · Whitten et al. · 2012 [cited by applicant]
US 20130011361A1 · Dales et al. · 2013 [cited by applicant]
US 20130225529A1 · Rigas · 2013 [cited by applicant]
US 20130317020A1 · Ruah et al. · 2013 [cited by applicant]
US 20140364393A1 · Yang et al. · 2014 [cited by applicant]
US 20150051206A1 · Loren et al. · 2015 [cited by applicant]
US 20150087673A1 · Hitoshi et al. · 2015 [cited by applicant]
US 20150246893A1 · Devaraj et al. · 2015 [cited by applicant]
US 20150252032A1 · Bolli et al. · 2015 [cited by applicant]
US 20160223559A1 · Devaraj et al. · 2016 [cited by applicant]
US 20160251336A1 · Yang et al. · 2016 [cited by applicant]
US 20160332989A1 · Wu et al. · 2016 [cited by applicant]
US 20170174699A1 · Hadari et al. · 2017 [cited by applicant]
US 20170226086A1 · Li et al. · 2017 [cited by applicant]
US 20180015068A1 · Inoue et al. · 2018 [cited by applicant]
US 20180193325A1 · Vincent et al. · 2018 [cited by applicant]
US 20190302121A1 · Copland, III et al. · 2019 [cited by applicant]
US 20190330198A1 · Wrona et al. · 2019 [cited by applicant]
US 20200010462A1 · Lucas et al. · 2020 [cited by applicant]
US 20200262828A1 · Lucas et al. · 2020 [cited by applicant]
US 20210139471A1 · Wrona et al. · 2021 [cited by applicant]
US 20220040167A1 · Vincent et al. · 2022 [cited by applicant]
CN 1177352 · 1998 [cited by applicant]
CN 101083994 · 2007 [cited by applicant]
CN 101128435 · 2008 [cited by applicant]
CN 101589039 · 2009 [cited by applicant]
CN 101641347 · 2010 [cited by applicant]
CN 101835776 · 2010 [cited by applicant]
CN 103221408 · 2013 [cited by applicant]
CN 103328482 · 2013 [cited by applicant]
CN 103619825 · 2014 [cited by applicant]
CN 103748087 · 2014 [cited by applicant]
CN 104163794 · 2014 [cited by applicant]
EP 1193255 · 2002 [cited by applicant]
EP 2455080 · 2012 [cited by applicant]
EP 2455081 · 2012 [cited by applicant]
EP 2598483 · 2013 [cited by applicant]
EP 2980077 · 2016 [cited by applicant]
EP 2990400 · 2016 [cited by applicant]
EP 3284738 · 2018 [cited by applicant]
EP 3381908A1 · 2018 [cited by applicant]
JP H11501021 · 1999 [cited by applicant]
JP 2005213233A · 2005 [cited by applicant]
JP 2008513514 · 2008 [cited by applicant]
JP 2008525478 · 2008 [cited by applicant]
JP 2008526796 · 2008 [cited by applicant]
JP 2008539275 · 2008 [cited by applicant]
JP 2008545760 · 2008 [cited by applicant]
JP 200919013A · 2009 [cited by applicant]
JP 2009501733 · 2009 [cited by applicant]
JP 201043052A · 2010 [cited by applicant]
JP 2010506859 · 2010 [cited by applicant]
JP 2010510993A · 2010 [cited by applicant]
JP 2010513400A · 2010 [cited by applicant]
JP 2010510272 · 2010 [cited by applicant]
JP 2010516714 · 2010 [cited by applicant]
JP 2010535847 · 2010 [cited by applicant]
JP 2011529102 · 2011 [cited by applicant]
JP 2012518603 · 2012 [cited by applicant]
JP 2013537180 · 2013 [cited by applicant]
JP 2014501274 · 2014 [cited by applicant]
JP 2014509600 · 2014 [cited by applicant]
JP 2014510708 · 2014 [cited by applicant]
JP 2014513071 · 2014 [cited by applicant]
JP 2014518240 · 2014 [cited by applicant]
KR 1020150014719A · 2015 [cited by applicant]
KR 1020150015305A · 2015 [cited by applicant]
KR 20160020616 · 2016 [cited by applicant]
WO WO9626937 · 1996 [cited by applicant]
WO WO9963979A2 · 1999 [cited by applicant]
WO WO0020414 · 2000 [cited by applicant]
WO WO0114339 · 2001 [cited by applicant]
WO WO0105769 · 2001 [cited by applicant]
WO WO0226944A2 · 2002 [cited by applicant]
WO WO02066470 · 2002 [cited by applicant]
WO WO02092087A1 · 2002 [cited by applicant]
WO WO03070885A2 · 2003 [cited by applicant]
WO WO03084948 · 2003 [cited by applicant]
WO WO2004014892 · 2004 [cited by applicant]
WO WO2005011654A2 · 2005 [cited by applicant]
WO WO2005011655A2 · 2005 [cited by applicant]
WO WO2005011656A2 · 2005 [cited by applicant]
WO WO2005011657A2 · 2005 [cited by applicant]
WO WO2005014607A2 · 2005 [cited by applicant]
WO WO2005011653 · 2005 [cited by applicant]
WO WO2005023833 · 2005 [cited by applicant]
WO WO2005026137 · 2005 [cited by applicant]
WO WO2005117867 · 2005 [cited by applicant]
WO WO2006014168A1 · 2006 [cited by applicant]
WO WO2006015621A1 · 2006 [cited by applicant]
WO WO2006012325 · 2006 [cited by applicant]
WO WO2006034279A1 · 2006 [cited by applicant]
WO WO2006034312A1 · 2006 [cited by applicant]
WO WO2006034315A2 · 2006 [cited by applicant]
WO WO2006034338A1 · 2006 [cited by applicant]
WO WO2006034341A2 · 2006 [cited by applicant]
WO WO2006034440A2 · 2006 [cited by applicant]
WO WO2006034441A1 · 2006 [cited by applicant]
WO WO2006034446A2 · 2006 [cited by applicant]
WO WO2006022442 · 2006 [cited by applicant]
WO WO2006057902A2 · 2006 [cited by applicant]
WO WO2006067531 · 2006 [cited by applicant]
WO WO2006071730 · 2006 [cited by applicant]
WO WO2006072436 · 2006 [cited by applicant]
WO WO2006074025 · 2006 [cited by applicant]
WO WO2006086445A2 · 2006 [cited by applicant]
WO WO2006086447A2 · 2006 [cited by applicant]
WO WO2006125179A1 · 2006 [cited by applicant]
WO WO2006125181A2 · 2006 [cited by applicant]
WO WO2006125194A2 · 2006 [cited by applicant]
WO WO2006116713 · 2006 [cited by applicant]
WO WO2006130986A1 · 2006 [cited by applicant]
WO WO2006137465 · 2006 [cited by applicant]
WO WO2007009236A1 · 2007 [cited by applicant]
WO WO2007044085A2 · 2007 [cited by applicant]
WO WO2007046868A2 · 2007 [cited by applicant]
WO WO2007056846A1 · 2007 [cited by applicant]
WO WO2007076055 · 2007 [cited by applicant]
WO WO2007079180 · 2007 [cited by applicant]
WO WO2007120702 · 2007 [cited by applicant]
WO WO2007130075A1 · 2007 [cited by applicant]
WO WO2007134457A1 · 2007 [cited by applicant]
WO WO2007136746A2 · 2007 [cited by applicant]
WO WO2007143597A2 · 2007 [cited by applicant]
WO WO2007143823A1 · 2007 [cited by applicant]
WO WO2007143824A1 · 2007 [cited by applicant]
WO WO2008003753A1 · 2008 [cited by applicant]
WO WO2008008059 · 2008 [cited by applicant]
WO WO2008008852 · 2008 [cited by applicant]
WO WO2008008854 · 2008 [cited by applicant]
WO WO2008017161A1 · 2008 [cited by applicant]
WO WO2008024390A2 · 2008 [cited by applicant]
WO WO2008023720 · 2008 [cited by applicant]
WO WO2008024139 · 2008 [cited by applicant]
WO WO2008029266A1 · 2008 [cited by applicant]
WO WO2008036715A1 · 2008 [cited by applicant]
WO WO2008043087A2 · 2008 [cited by applicant]
WO WO2008044767A1 · 2008 [cited by applicant]
WO WO2008046226A1 · 2008 [cited by applicant]
WO WO2008056687A1 · 2008 [cited by applicant]
WO WO2008062276A2 · 2008 [cited by applicant]
WO WO2008057280 · 2008 [cited by applicant]
WO WO2008061795 · 2008 [cited by applicant]
WO WO2008074824A2 · 2008 [cited by applicant]
WO WO2008074832A2 · 2008 [cited by applicant]
WO WO2008074833A2 · 2008 [cited by applicant]
WO WO2008074834A2 · 2008 [cited by applicant]
WO WO2008074835A1 · 2008 [cited by applicant]
WO WO2008064474 · 2008 [cited by applicant]
WO WO2008076356 · 2008 [cited by applicant]
WO WO2008089580A1 · 2008 [cited by applicant]
WO WO2008096746A1 · 2008 [cited by applicant]
WO WO2008104524A1 · 2008 [cited by applicant]
WO WO2008116898A1 · 2008 [cited by applicant]
WO WO2008120744A1 · 2008 [cited by applicant]
WO WO2008120759A1 · 2008 [cited by applicant]
WO WO2008123469A1 · 2008 [cited by applicant]
WO WO2008127349A2 · 2008 [cited by applicant]
WO WO2008128335A1 · 2008 [cited by applicant]
WO WO2008139845A1 · 2008 [cited by applicant]
WO WO2008141455A1 · 2008 [cited by applicant]
WO WO2008157844A1 · 2008 [cited by applicant]
WO WO2009010560A1 · 2009 [cited by applicant]
WO WO2009012573A1 · 2009 [cited by applicant]
WO WO2009016216A1 · 2009 [cited by applicant]
WO WO2009019566A1 · 2009 [cited by applicant]
WO WO2009021990 · 2009 [cited by applicant]
WO WO2009037542A2 · 2009 [cited by applicant]
WO WO2009056556A1 · 2009 [cited by applicant]
WO WO2009060053A1 · 2009 [cited by applicant]
WO WO2009060054A1 · 2009 [cited by applicant]
WO WO2009070533A1 · 2009 [cited by applicant]
WO WO2009073973A1 · 2009 [cited by applicant]
WO WO2009103739A1 · 2009 [cited by applicant]
WO WO2009106991A2 · 2009 [cited by applicant]
WO WO2009117659A1 · 2009 [cited by applicant]
WO WO2009124259A1 · 2009 [cited by applicant]
WO WO2009129625A1 · 2009 [cited by applicant]
WO WO2009123896 · 2009 [cited by applicant]
WO WO2009150196A1 · 2009 [cited by applicant]
WO WO2009156484A2 · 2009 [cited by applicant]
WO WO2010006962A1 · 2010 [cited by applicant]
WO WO2010007482A2 · 2010 [cited by applicant]
WO WO2010007966 · 2010 [cited by applicant]
WO WO2010013037 · 2010 [cited by applicant]
WO WO2010022055 · 2010 [cited by applicant]
WO WO2010025553A1 · 2010 [cited by applicant]
WO WO2010035052A1 · 2010 [cited by applicant]
WO WO2010037225A1 · 2010 [cited by applicant]
WO WO2010043052A1 · 2010 [cited by applicant]
WO WO2010045371A1 · 2010 [cited by applicant]
WO WO2010045374A1 · 2010 [cited by applicant]
WO WO2010039186 · 2010 [cited by applicant]
WO WO2010043052 · 2010 [cited by applicant]
WO WO2010048149 · 2010 [cited by applicant]
WO WO2010056230A1 · 2010 [cited by applicant]
WO WO2010057833 · 2010 [cited by applicant]
WO WO2010060996 · 2010 [cited by applicant]
WO WO2010094120A1 · 2010 [cited by applicant]
WO WO2010094126A1 · 2010 [cited by applicant]
WO WO2010108268A1 · 2010 [cited by applicant]
WO WO2010101964 · 2010 [cited by applicant]
WO WO2010112520A1 · 2010 [cited by applicant]
WO WO2011011506A1 · 2011 [cited by applicant]
WO WO2011011508A1 · 2011 [cited by applicant]
WO WO2011011872A1 · 2011 [cited by applicant]
WO WO2011015629A1 · 2011 [cited by applicant]
WO WO2011030312A1 · 2011 [cited by applicant]
WO WO2011025690 · 2011 [cited by applicant]
WO WO2011039358A1 · 2011 [cited by applicant]
WO WO2011047481A1 · 2011 [cited by applicant]
WO WO2011109059 · 2011 [cited by applicant]
WO WO2011131593A1 · 2011 [cited by applicant]
WO WO2011123681 · 2011 [cited by applicant]
WO WO2011157793 · 2011 [cited by applicant]
WO WO2012009134 · 2012 [cited by applicant]
WO WO2012016133 · 2012 [cited by applicant]
WO WO2012016217 · 2012 [cited by applicant]
WO WO2012035023 · 2012 [cited by applicant]
WO WO2012046681A1 · 2012 [cited by applicant]
WO WO2012066077 · 2012 [cited by applicant]
WO WO2012080729 · 2012 [cited by applicant]
WO WO2012082817 · 2012 [cited by applicant]
WO WO2012093809 · 2012 [cited by applicant]
WO WO2012123449 · 2012 [cited by applicant]
WO WO2012136492 · 2012 [cited by applicant]
WO WO2012169649 · 2012 [cited by applicant]
WO WO2013004642 · 2013 [cited by applicant]
WO WO2013026587 · 2013 [cited by applicant]
WO WO2013046136 · 2013 [cited by applicant]
WO WO2013056148 · 2013 [cited by applicant]
WO WO2013070660 · 2013 [cited by applicant]
WO WO2013085954A1 · 2013 [cited by applicant]
WO WO2013085957A1 · 2013 [cited by applicant]
WO WO2013098373 · 2013 [cited by applicant]
WO WO2013134546A1 · 2013 [cited by applicant]
WO WO2013160811A1 · 2013 [cited by applicant]
WO WO2013170072 · 2013 [cited by applicant]
WO WO2013175474 · 2013 [cited by applicant]
WO WO2014003153 · 2014 [cited by applicant]
WO WO2014031928 · 2014 [cited by applicant]
WO WO2014092104 · 2014 [cited by applicant]
WO WO2014116386A1 · 2014 [cited by applicant]
WO WO2015048547 · 2015 [cited by applicant]
WO WO2015101293 · 2015 [cited by applicant]
WO WO2015113920 · 2015 [cited by applicant]
WO WO2015132610A1 · 2015 [cited by applicant]
WO WO2015137385A1 · 2015 [cited by applicant]
WO WO2015140130 · 2015 [cited by applicant]
WO WO2016022626 · 2016 [cited by applicant]
WO WO2016022955 · 2016 [cited by applicant]
WO WO2016040794A1 · 2016 [cited by applicant]
WO WO2016049586 · 2016 [cited by applicant]
WO WO2016098005 · 2016 [cited by applicant]
WO WO2016107603 · 2016 [cited by applicant]
WO WO2017066705 · 2017 [cited by applicant]
WO WO2017093263 · 2017 [cited by applicant]
WO WO2017112777 · 2017 [cited by applicant]
WO WO2017212425 · 2017 [cited by applicant]
WO WO2018026663 · 2018 [cited by applicant]
WO WO2018081167 · 2018 [cited by applicant]
WO WO2018112077 · 2018 [cited by applicant]
WO WO2018129403 · 2018 [cited by applicant]
WO WO2018160717 · 2018 [cited by applicant]
WO WO2018161033 · 2018 [cited by applicant]
WO WO2018195450 · 2018 [cited by applicant]
WO WO2019018795 · 2019 [cited by applicant]
WO WO2019084157A1 · 2019 [cited by applicant]
WO WO2019123375 · 2019 [cited by applicant]
WO WO2019123378 · 2019 [cited by applicant]
WO WO2019140188 · 2019 [cited by applicant]
WO WO2019173394 · 2019 [cited by applicant]
WO WO2019183587 · 2019 [cited by applicant]
WO WO2019209948 · 2019 [cited by applicant]
WO WO2019209962 · 2019 [cited by applicant]
WO WO2020023657 · 2020 [cited by applicant]
WO WO2020132378 · 2020 [cited by applicant]
WO WO2020154571 · 2020 [cited by applicant]
WO WO2020198026 · 2020 [cited by applicant]
WO WO2021092240 · 2021 [cited by applicant]
WO WO2021092262 · 2021 [cited by applicant]
WO WO2021097240 · 2021 [cited by applicant]
WO WO2021139595 · 2021 [cited by applicant]
WO WO2021154571 · 2021 [cited by applicant]
Swirski et al (Evaluating the relationship between amyloid-ß and α-synuclein phosphorylated at Ser129 in dementia with Lewy bodies and Parkinson's disease, Alzheimer's Research & Therapy 2014, 6:77) (Year: 2014). [cited by examiner]
Liu et al (Apolipoprotein E and Alzheimer disease: risk, mechanisms, and therapy, Nat Rev Neurol. Feb. 2013 ; 9(2): 106-118) (Year: 2013). [cited by examiner]
Berlin et al., 16(4) Bioorg. & Med. Chem. Letts., pp. 989-994 (2006). [cited by applicant]
Dai et al., “SCD1 Confes Temozolomide Resistance to Human Glioma Cells via Akt/GSK3β/β-Catenin Signaling Axis,” Frontiers in Pharmacology, vol. 8, Art. 960 (2018). [cited by applicant]
Debenham et al., “Discovery of N-[Bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-y1)pyrimidine-5-carboxamide (MK-8617), an Orally Active Pan-Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase1-3 (HIFPHD1-3) … [cited by applicant]
Fatutta et al: “Comportamento di alcune idrazidi di fronte a composti y-dicarbonilici. (*)”, Gazzetta Chimica Italiana, Societa Chimica Italiana, It, vol. 90, Jan. 1, 1960 (Jan. 1, 1960), pp. 1645-1657, XP009532381. [cited by applicant]
Horan et al., “Piperazinyl-oxadiazoles as selective sphingosine-1-phosphate receptor agonists,” Bioorg Med Chem Lett. 24(20):4807-11 (2014) (5 pages). [cited by applicant]
Huestis et al., “The Vinyl Moiety as a Handle for regiocontrol in the Preparation of Unsymmetrical 2,3-Atiphatic-Substituted Indoles and Pyrroles,” Angew Chem Int Ed Engl. 50(6):1338-41 (2011). [cited by applicant]
Jarvis et al., “A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.” Proc Natl Acad Sci U.S.A. 104(20):8520-5 (2007). [cited by applicant]
Krasavin et al., “Antiproliferative 4-(1,2,4-oxadiazol-5-y1)piperidine-1-carboxamides, a new tubulin inhibitor chemotype,” Bioorg Med Chem Lett. 24(18): 4477-4481 (2014) (5 pages). [cited by applicant]
Kumar et al., “Design and Synthesis of 3,5-Disubstituted-1,2,4-Oxadiazoles as Potent Inhibitors of Phosphodiesterase 4 B2” Chem Biol Drug Des. 79(5):810-8 (2012). [cited by applicant]
Maya S. Salnikova, Rational Development of Protein Formulations in Solid and Solution States. [cited by applicant]
Muraglia et al., “N-(2-alkylaminoethy1)-4-(1,2,4-oxadiazol-5-y1)piperazine-1-carboxamides as highly potent smoothened antagonists,” Bioorg Med Chem Lett. 21(18): 5283-8 (2011) (6 pages). [cited by applicant]
Ng Davis et al: “Reviewing editor”,Jul. 20, 2016 (Jul. 20, 2016), pp. 1-33, XP055921015, Retrieved from the Internet: URL:https://www.ncbi.nlm.nih.gov/pmc/artic les/PMC4954757/pdf/elife-11878.pdf [retrieved on May 13, 2… [cited by applicant]
Oatman et al. “Mechanisms of stearoyl CoA desaturase inhibitor sensitivity and acquired resistance in cancer” Science Advances. Feb. 10, 2021 (Feb. 10, 2021) vol. 7, p. 1-19. [cited by applicant]
Ontoria et al., “Identification of a series of 4-[3-(quinolin-2-y1)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as potent smoothened antagonist hedgehog pathway inhibitors,” 21(18): 5274-82 (2011) (9 pages). [cited by applicant]
Shen et al., “Discovery of a Highly Potent, Selective, and Bioavailable Soluble Epoxide Hydrolase Inhibitor with Excellent Ex Vivo Target Engagement.” J Med Chem. 52(16):5009-12 (2009). [cited by applicant]
Skedelj Veronika et al: “ATP-Binding Site of Bacterial Enzymes as a Target for Antibacterial Drug Design”, Journal of Medicinal Chemistry, vol. 54, No. 4, Jan. 14, 2011 (Jan. 14, 2011), pp. 915-929, XP055922741. [cited by applicant]
Terry-Kantor et al., “Rapid Alpha-Synuclein Toxicity in a Neural Cell Model and Its Rescue by a Stearoyl-CoA Desaturase Inhibitor,” Int. J. Mol. Sci., 21, 5193, 1-16 (Jul. 22. 2020). [cited by applicant]
Tesfay et al., “Steroyl-CoA Desaturase (SCD1) protects ovarian cancer cells from ferroptotic cell death,” Cancer Res. 79(20): 5355-5366 (Oct. 15, 2019). [cited by applicant]
Tiwari et al., “Synthesis of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole analogues and their evaluation as anti-Parkinson's agents.” Med Chem Res. 17:386-398 (2008) (12 pages). [cited by applicant]
Zhang et al., “Opportunities and Challenges in Develping Stearoyl-Coenzyme A Desaturase-1 Inhibitors as Novel Therapeutics for Human Disease,” J. Med. Chem., 57, 5039-5056 (2014). [cited by applicant]
Zhou, Youping, Zhong, et al. Inhibition of stearoyl-coenzyme A desaturase 1 ameliorates hepatic steatosis by inducing AMPK-mediated lipophagy. Aging, 12(8):7350-7362 (Apr. 23, 2020). [cited by applicant]
Database Registry Chemical Abstracts Service, Columbus, Ohio, Accession No. RN 276236-86-3, Entered STN: Jul. 11, 2000. [cited by applicant]
Database Registry Chemical Abstracts Service, RN 887202-53-1, entered STN: Jun. 8, 2006 (3 pages). [cited by applicant]
PubChem CID 91412014, Create Date: Mar. 17, 2015 (Mar. 17, 2015), p. 2, Fig. [cited by applicant]
PubChem Compound Summary for CID 126485826, dated Apr. 22, 2017 (6 pages). [cited by applicant]
PubChem Compound Summary for CID 127012056, dated Jun. 2, 2017 (12 pages). [cited by applicant]
PubChem Compound Summary for CID 127868748, dated Jun. 18, 2017 (9 pages). [cited by applicant]
PubChem Compound Summary for CID 53003909, dated Jun. 21, 2011 (7 pages). [cited by applicant]
PubChem Compound Summary for CID 56980069, dated Jun. 13, 2012 (11 pages). [cited by applicant]
PubChem Compound Summary for CID 7059272, dated Jul. 29, 2006 (12 pages). [cited by applicant]
PubChem Compound Summary for CID 71908265, retrieved from <https://pubchem.ncbi.nlm.nih.gov/compound/71908265>, created Nov. 29, 2013, retrieved Jan. 4, 2021 (8 pages). [cited by applicant]
PubChem Compound Summary tor CID 15985883, “5-[5-[4-[(4-Chlorophenyl)methyl]piperidin-1-y1]-5-oxopentvll-1H-pyridin-2-one,”created Mar. 27, 2007, retrieved Mar. 25, 2020 (7 pages). [cited by applicant]
Vincent et al. “Inhibiting Stearoyl-CoA Desaturase Ameliorates a-Synuclein Cytotoxicity,” Cell Reports, 25: 2742-2754 (2018). [cited by applicant]
Madia Valentina Noemi et al., “Novel Benzazole Derivatives Endowed with Potent Antiheparanase Activity”, Journal of Medicinal Chemistry, vol. 61, No. 15, Jul. 16, 2018 (Jul. 16, 2018), pp. 6918-6936, XP093025853, US. [cited by applicant]
Trivedi Prakruti et al., “Design, synthesis and biological screening of 2-aminobenzamides as selective HDAC3 inhibitors with promising anticancer effects”, European Journal of Pharmaceutical Sciences, Elsevier Amsterdam… [cited by applicant]
Tang Qidong et al., “Discovery of novel 7-azaindole derivatives bearing dihydropyridazine moiety as c-Met kinase inhibitors”, European Journal of Medicinal Chemistry, vol. 133, Jun. 1, 2017 (Jun. 1, 2017), pp. 97-106, X… [cited by applicant]
Wang Lin Xiao et al., “Discovery of novel pyrrolo-pyridine/pyrimidine derivatives bearing pyridazinone moiety as c-Met kinase inhibitors”, European Journal of Medicinal Chemistry, vol. 141, Oct. 13, 2017 (Oct. 13, 2017)… [cited by applicant]
Byrd Katherine M. et al., “Synthesis and Biological Evaluation of Stilbene Analogues as Hsp90 C-Terminal Inhibitors”, ChemMedChem Communications, vol. 12, No. 24, Nov. 30, 2017 (Nov. 30, 2017), pp. 2022-2029, XP09302586… [cited by applicant]
RN1266245-83-3, registry database compound, 2011. [cited by applicant]
RN1358463-36-1-83-3, registry database compound, 2012. [cited by applicant]
“List of neurological conditions and disorders,” <https://en.wikipedia.org/wiki/List_of_neurological_conditions_and_disorders>, retrieved on Jun. 27, 2019 (12 pages). [cited by applicant]
Astarita et al., “Elevated stearoyl-CoA desaturase in brains of patients with Alzheimer's disease,” PLoS One. 6(10):e24777 (2011) (9 pages). [cited by applicant]