IP Library › Granted Patent US 12,440,468
Granted Patent B2
US 12,440,468 · App. 18/582,320 · Granted Oct 14, 2025

Pharmaceutical compositions of dimethyl fumarate

Inventors: Sami Karaborni (Cupertino, CA); Wei Chen (Cupertino, CA); Suresh Kumar Manthati (Sunnyvale, CA)
Assignee: ARBOR PHARMACEUTICALS, LLC
A61K31/336A61J1/035A61K31/194A61K31/215A61K31/225A61K31/343A61K31/381A61K31/403A61K9/4825
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Quick Facts
Patent No.
US 12,440,468
App. No.
18/582,320
Granted
Oct 14, 2025
Kind
B2
Abstract

Pharmaceutical compositions and dosage forms of dimethyl fumarate containing low levels of certain impurities are disclosed.

Claims (17)

1. A dosage form for treating multiple sclerosis, comprising:

(a) a therapeutically effective amount of dimethyl fumarate in solid form;

(b) one or more compounds of Formula (V):

isomers thereof and salts of any of the foregoing, wherein:

each of R 13 and R 14 is independent chosen from hydrogen and methyl; and wherein the one or more compounds of Formula (V) are present in a combined total amount of about 0.0010% to 2% by weight based on total weight of the dimethyl fumarate; and

(c) a pharmaceutically acceptable vehicle.

2. The dosage form of claim 1 , wherein the one or more compounds of Formula (V) are present in a combined total amount of about 0.001% to 1% by weight based on total weight of the dimethyl fumarate.

3. The dosage form of claim 1 , wherein each of the one or more compounds of Formula (V) is present in an amount of about 0.001% to 0.3% by weight based on total weight of the dimethyl fumarate.

4. The dosage form of claim 1 , wherein each of the one or more compounds of Formula (V) is present in an amount of about 0.0010% to 0.2% weight based on total weight of the dimethyl fumarate.

5. The dosage form of claim 1 , wherein the one or more compounds of Formula (V) are selected from: 2,3-dihydroxysuccinic acid dimethyl ester, 2,3-dihydroxysuccinic acid monomethyl ester, 2,3-dihydroxysuccinic acid, isomers thereof and salts of any of the foregoing.

6. The dosage form of claim 5 , wherein the one or more compounds of Formula (V) is 2,3-dihydroxysuccinic acid dimethyl ester, isomers thereof, or salts thereof.

7. The dosage form of claim 5 , wherein the one or more compounds of Formula (V) is 2,3-dihydroxysuccinic acid monomethyl ester, isomers thereof, or salts thereof.

8. The dosage form of claim 5 , wherein the one or more compounds of Formula (V) is 2,3-dihydroxysuccinic acid, isomers thereof, or salts thereof.

9. The dosage form of claim 1 , in the form of a tablet or capsule.

10. The dosage form of claim 1 , wherein the pharmaceutically acceptable vehicle is selected from a carrier, a diluent, an excipient, a wetting agent, an emulsifier, a buffer, a stabilizer, a thickener, a lubricant, a coloring agent and combinations thereof.

11. The dosage form of claim 1 , wherein the dosage form is substantially free of PVP, PEG and polysorbate surfactant.

12. The dosage form of claim 1 , further comprising a free radical scavenger.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 16, 2025
From: KARABORNI, SAMI; CHEN, WEI; MANTHATI, SURESH KUMAR
To: XENOPORT, INC.
Reel/Frame 071422/0508 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 16, 2025
From: XENOPORT, INC.
To: ARBOR PHARMACEUTICALS, LLC
Reel/Frame 071422/0546 →
CONFIRMATORY GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded Mar 17, 2025
From: ARBOR PHARMACEUTICALS, LLC; AZURITY PHARMACEUTICALS, INC.; AZURITY PHARMACEUTICALS IRELAND LIMITED; SILVERGATE PHARMACEUTICALS, INC.
To: HPS INVESTMENT PARTNERS, LLC, AS ADMINISTRATIVE AGENT
Reel/Frame 070531/0487 →
Continuity (9)
Division 17551550 · Dec 15, 2021
Division 16749427 · Jan 22, 2020
Continuation 16206521 · Nov 30, 2018
Division 14223026 · Mar 24, 2014
Provisional Application 61805869 · Mar 27, 2013
Provisional Application 61805516 · Mar 26, 2013
Provisional Application 61805137 · Mar 25, 2013
Provisional Application 61804725 · Mar 24, 2013
Related Publication 20240189271A1 · Jun 13, 2024
References Cited (391)
US 2532579A · Thomas · 1950 [cited by applicant]
US 3139395A · Griffin · 1964 [cited by applicant]
US 3336364A · Robert · 1967 [cited by applicant]
US 3751277A · Small et al. · 1973 [cited by applicant]
US 4851439A · Speiser et al. · 1989 [cited by applicant]
US 4863916A · Habich et al. · 1989 [cited by applicant]
US 4959389A · Speiser et al. · 1990 [cited by applicant]
US 5073641A · Bundgaard et al. · 1991 [cited by applicant]
US 5145684A · Liversidge et al. · 1992 [cited by applicant]
US 5149695A · Speiser et al. · 1992 [cited by applicant]
US 5424332A · Speiser et al. · 1995 [cited by applicant]
US 5451667A · Speiser et al. · 1995 [cited by applicant]
US 5534250A · Klaveness et al. · 1996 [cited by applicant]
US 6130248A · Nudelman et al. · 2000 [cited by applicant]
US 6277882B1 · Joshi et al. · 2001 [cited by applicant]
US 6355676B1 · Joshi et al. · 2002 [cited by applicant]
US 6359003B1 · Joshi et al. · 2002 [cited by applicant]
US 6379697B1 · Gregoriadis et al. · 2002 [cited by applicant]
US 6436992B1 · Joshi et al. · 2002 [cited by applicant]
US 6509376B1 · Joshi et al. · 2003 [cited by applicant]
US 6613800B1 · Smith · 2003 [cited by applicant]
US 6709868B2 · Law et al. · 2004 [cited by applicant]
US 6723508B2 · Sprenger et al. · 2004 [cited by applicant]
US 6858750B2 · Joshi et al. · 2005 [cited by applicant]
US 7157423B2 · Joshi et al. · 2007 [cited by applicant]
US 7320999B2 · Joshi et al. · 2008 [cited by applicant]
US 7432240B2 · Joshi et al. · 2008 [cited by applicant]
US 7612110B2 · Joshi et al. · 2009 [cited by applicant]
US 7619001B2 · Joshi et al. · 2009 [cited by applicant]
US 7638118B2 · Flachsmann et al. · 2009 [cited by applicant]
US 7790916B2 · Joshi et al. · 2010 [cited by applicant]
US 7803840B2 · Joshi et al. · 2010 [cited by applicant]
US 7906659B2 · Joshi et al. · 2011 [cited by applicant]
US 7915310B2 · Joshi et al. · 2011 [cited by applicant]
US 8067467B2 · Joshi et al. · 2011 [cited by applicant]
US 8148414B2 · Gangakhedkar et al. · 2012 [cited by applicant]
US 8399514B2 · Lukashev et al. · 2013 [cited by applicant]
US 8524773B2 · Joshi et al. · 2013 [cited by applicant]
US 8669281B1 · Zeidan et al. · 2014 [cited by applicant]
US 8759393B2 · Joshi et al. · 2014 [cited by applicant]
US 8778991B2 · Gangakhedkar et al. · 2014 [cited by applicant]
US 8785443B2 · Gangakhedkar et al. · 2014 [cited by applicant]
US 8906420B2 · Nilsson et al. · 2014 [cited by applicant]
US 8952006B2 · Cundy et al. · 2015 [cited by applicant]
US 9421182B2 · Mao et al. · 2016 [cited by applicant]
US 10179118B2 · Karaborni et al. · 2019 [cited by applicant]
US 10576055B2 · Karaborni et al. · 2020 [cited by applicant]
US 10716760B2 · Karaborni et al. · 2020 [cited by applicant]
US 11229621B2 · Karaborni et al. · 2022 [cited by applicant]
US 11938111B2 · Karaborni et al. · 2024 [cited by applicant]
US 20040054001A1 · Joshi et al. · 2004 [cited by applicant]
US 20040102525A1 · Kozachuk · 2004 [cited by applicant]
US 20050095292A1 · Benjamin et al. · 2005 [cited by applicant]
US 20050096369A1 · Hoang · 2005 [cited by applicant]
US 20050101779A1 · Sagi et al. · 2005 [cited by applicant]
US 20050208133A1 · Tsutsumi et al. · 2005 [cited by applicant]
US 20060269925A1 · Nunes et al. · 2006 [cited by applicant]
US 20070027076A1 · Joshi et al. · 2007 [cited by applicant]
US 20070213300A1 · Liu et al. · 2007 [cited by applicant]
US 20070231382A1 · Karnachi et al. · 2007 [cited by applicant]
US 20070253902A1 · Lobb et al. · 2007 [cited by applicant]
US 20080004344A1 · Nilsson et al. · 2008 [cited by applicant]
US 20080033199A1 · Lai et al. · 2008 [cited by applicant]
US 20080089861A1 · Went et al. · 2008 [cited by applicant]
US 20080089896A1 · Wang et al. · 2008 [cited by applicant]
US 20080103172A1 · Yu · 2008 [cited by examiner]
US 20080227847A1 · Nilsson et al. · 2008 [cited by applicant]
US 20080233185A1 · Joshi et al. · 2008 [cited by applicant]
US 20080299196A1 · Nilsson et al. · 2008 [cited by applicant]
US 20080300217A1 · Nilsson · 2008 [cited by applicant]
US 20090304790A1 · Nilsson et al. · 2009 [cited by applicant]
US 20100099907A1 · Raillard et al. · 2010 [cited by applicant]
US 20100105784A1 · Remon et al. · 2010 [cited by applicant]
US 20100130607A1 · Gold · 2010 [cited by applicant]
US 20100144651A1 · Nilsson et al. · 2010 [cited by applicant]
US 20100226981A1 · Karaborni et al. · 2010 [cited by applicant]
US 20100247642A1 · Wu et al. · 2010 [cited by applicant]
US 20100260755A1 · Gammans et al. · 2010 [cited by applicant]
US 20110112196A1 · Lukashev · 2011 [cited by applicant]
US 20110124615A1 · Joshi et al. · 2011 [cited by applicant]
US 20110212169A1 · Bae et al. · 2011 [cited by applicant]
US 20120034274A1 · Nilsson et al. · 2012 [cited by applicant]
US 20120165404A1 · Lukashev · 2012 [cited by applicant]
US 20120196931A1 · Lukashev · 2012 [cited by examiner]
US 20130065909A1 · Milne et al. · 2013 [cited by applicant]
US 20130172391A1 · Kahrs · 2013 [cited by applicant]
US 20130259856A1 · Kaye · 2013 [cited by applicant]
US 20130259906A1 · Nilsson et al. · 2013 [cited by applicant]
US 20130295169A1 · Goldman et al. · 2013 [cited by applicant]
US 20130302410A1 · Gold · 2013 [cited by applicant]
US 20130317103A1 · Lukashev · 2013 [cited by applicant]
US 20130324539A1 · Virsik et al. · 2013 [cited by applicant]
US 20140051705A1 · Cundy et al. · 2014 [cited by applicant]
US 20140056973A1 · Ma · 2014 [cited by examiner]
US 20140056978A1 · Karaborni et al. · 2014 [cited by applicant]
US 20140057917A1 · Cundy et al. · 2014 [cited by applicant]
US 20140057918A1 · Wustrow et al. · 2014 [cited by applicant]
US 20140065211A1 · Karaborni et al. · 2014 [cited by applicant]
US 20140066505A1 · Joshi et al. · 2014 [cited by applicant]
US 20140099364A2 · Nilsson et al. · 2014 [cited by applicant]
US 20140163100A1 · Dawson et al. · 2014 [cited by applicant]
US 20140179778A1 · Mao et al. · 2014 [cited by applicant]
US 20140179779A1 · Chao · 2014 [cited by applicant]
US 20140193386A1 · Preiss-Bloom et al. · 2014 [cited by applicant]
US 20140193387A1 · Gruskin et al. · 2014 [cited by applicant]
US 20140193388A1 · Velders et al. · 2014 [cited by applicant]
US 20140193390A1 · Valenzano et al. · 2014 [cited by applicant]
US 20140193392A1 · Annunziata et al. · 2014 [cited by applicant]
US 20140193393A1 · Gulati · 2014 [cited by applicant]
US 20140193495A1 · Nilsson et al. · 2014 [cited by applicant]
US 20140194427A1 · Chao · 2014 [cited by applicant]
US 20140200272A1 · Nilsson et al. · 2014 [cited by applicant]
US 20140200273A1 · Nilsson et al. · 2014 [cited by applicant]
US 20140200363A1 · Guzowski et al. · 2014 [cited by applicant]
US 20140205659A1 · Nilsson et al. · 2014 [cited by applicant]
US 20140275048A1 · Zeidan et al. · 2014 [cited by applicant]
US 20140275250A1 · Cundy · 2014 [cited by applicant]
US 20140323570A1 · Gold · 2014 [cited by applicant]
US 20140329818A1 · Gangakhedkar et al. · 2014 [cited by applicant]
US 20140336151A1 · Chao · 2014 [cited by applicant]
US 20140364604A1 · Raillard et al. · 2014 [cited by applicant]
US 20150038499A1 · Virsik · 2015 [cited by applicant]
US 20150073049A1 · Mao et al. · 2015 [cited by applicant]
US 20150079180A1 · Karaborni et al. · 2015 [cited by applicant]
US 20150190360A1 · Cundy · 2015 [cited by applicant]
US 20150265707A1 · Manthati et al. · 2015 [cited by applicant]
CN 1616400A · 2005 [cited by applicant]
CN 101318901A · 2008 [cited by applicant]
CN 101774913A · 2010 [cited by applicant]
DE 1165586B · 1964 [cited by applicant]
DE 10360869A1 · 2005 [cited by applicant]
EP 2692344A1 · 2014 [cited by applicant]
GB 1153927A · 1969 [cited by applicant]
GB 1404989A · 1975 [cited by applicant]
GB 2285805A · 1995 [cited by applicant]
JP S60181047A · 1985 [cited by applicant]
JP H03294245A · 1991 [cited by applicant]
JP 2001158760A · 2001 [cited by applicant]
JP 2002027998A · 2002 [cited by applicant]
WO WO9636613A1 · 1996 [cited by applicant]
WO WO9829114A1 · 1998 [cited by applicant]
WO WO9852549A2 · 1998 [cited by applicant]
WO WO9853803A1 · 1998 [cited by applicant]
WO WO9921559A1 · 1999 [cited by applicant]
WO WO9949858A1 · 1999 [cited by applicant]
WO WO9951191A1 · 1999 [cited by applicant]
WO WO9962973A1 · 1999 [cited by applicant]
WO WO0010560A1 · 2000 [cited by applicant]
WO WO0012072A2 · 2000 [cited by applicant]
WO WO02055063A2 · 2002 [cited by applicant]
WO WO02055066A1 · 2002 [cited by applicant]
WO WO02055067A2 · 2002 [cited by applicant]
WO WO03087174A2 · 2003 [cited by applicant]
WO WO2005023241A1 · 2005 [cited by examiner]
WO WO2005027899A1 · 2005 [cited by applicant]
WO WO2006037342A2 · 2006 [cited by applicant]
WO WO2006050730A1 · 2006 [cited by applicant]
WO WO2006122652A2 · 2006 [cited by applicant]
WO WO2007006307A2 · 2007 [cited by applicant]
WO WO2007006308A1 · 2007 [cited by applicant]
WO WO2007042034A1 · 2007 [cited by applicant]
WO WO2007042035A2 · 2007 [cited by applicant]
WO WO2008096271A2 · 2008 [cited by applicant]
WO WO2008097596A2 · 2008 [cited by applicant]
WO WO2010022177A2 · 2010 [cited by applicant]
WO WO2010079221A1 · 2010 [cited by applicant]
WO WO2010079222A1 · 2010 [cited by applicant]
WO WO2010126605A1 · 2010 [cited by applicant]
WO WO2011080344A1 · 2011 [cited by applicant]
WO WO2011100589A1 · 2011 [cited by applicant]
WO WO2012162669A1 · 2012 [cited by applicant]
WO WO2012170923A1 · 2012 [cited by applicant]
WO WO2013022882A1 · 2013 [cited by applicant]
WO WO2013076216A1 · 2013 [cited by applicant]
WO WO2013119677A1 · 2013 [cited by applicant]
WO WO2013119791A1 · 2013 [cited by applicant]
WO WO2014020156A1 · 2014 [cited by applicant]
WO WO2014031894A1 · 2014 [cited by applicant]
WO WO2014031897A1 · 2014 [cited by applicant]
WO WO2014071371A1 · 2014 [cited by applicant]
WO WO2014096425A2 · 2014 [cited by applicant]
WO WO2014100728A1 · 2014 [cited by applicant]
WO WO2014190056A2 · 2014 [cited by applicant]
WO WO2015028472A1 · 2015 [cited by applicant]
WO WO2015028473A1 · 2015 [cited by applicant]
Acids—pH Values. The Engineering ToolBox. Retrieved from URL:https://www.engineeringtoolbox.com/acids-ph-d_401.html pp. 1-8. [cited by applicant]
Altmeyer, Peter J. et al.: Antipsoriatic Effect of Fumaric Acid Derivatives. Results of a Multicenter Double-blind Study in 100 Patients. Journal of the American Academy of Dermatology 30(6):977-981 (1994). [cited by applicant]
Altschul, Stephen F. et al.: Gapped BLAST and PSI-BLAST: a new Generation of Protein Database Search Programs. Nucleic Acids Research 25(17):3389-3402 (1997). [cited by applicant]
Ashe, Karen Hsiao: Learning and Memory in Transgenic Mice Modeling Alzheimer's Disease. Learning & Memory 8(6):301-308 (2001). [cited by applicant]
Atreya, I. et al.: NF-κB in Inflammatory Bowel Disease. Journal of Internal Medicine 263(6):591-596 (2008). [cited by applicant]
Bardgett, Mark E. et al.: NMDA Receptor Blockade and Hippocampal Neuronal Loss Impair Fear Conditioning and Position Habit Reversal in C57BI/6 Mice. Brain Research Bulletin 60(1-2):131-142 (2003). [cited by applicant]
Barnes, Peter J.: Mediators of chronic obstructive pulmonary disease. Pharmacological reviews 56(4):515-548 (2004). [cited by applicant]
Bar-Or, Amit. et al.: Clinical Efficacy Of Bg-12 (Dimethyl Fumarate) In Patients With Relapsing-remitting Multiple Sclerosis: Subgroup Analyses Of The DEFINE Study. Journal of Neurology 260(9):2297-2305 (2013). [cited by applicant]
Bertone, Joseph J.: Prevalence of Gastric Ulcers In Elite, Heavy Use Western Performance Horses. AAEP Proceedings 46:256-259 (2000). [cited by applicant]
BG 12: BG 00012, BG 12/Oral Fumarate, FAG-201, Second-generation Fumarate Derivative—Fumapharm/Biogen Idec. Drugs in R&D 6(4):229-230 (2005). [cited by applicant]
Bhagavathula, Narasimharao. et al.: 7-chloro-5-(4-hydroxyphenyl)-1-methyl-3-(Naphthalen-2-ylmethyl)-4,5-dihydro-1H-benzo[B][1,4]Diazepin-2(3H)-one (Bz-423), A Benzodiazepine, Suppresses Keratinocyte Proliferation And Ha… [cited by applicant]
Bhagiyalakshmi, M. et al.: Selective epoxidation of dimethyl maleate to cis-epoxydimethyl succinate over solid acid catalysts. Catalysis Today 141(1-2):234-241 (2009). [cited by applicant]
Bhattacharya, Sisir et al.: Chapter 9: Thermoanalytical and Crystallographic Methods. Polymorphism in Pharmaceutical Solids, 2nd edition. Informa Healthcare (pp. 318-346) (2009). [cited by applicant]
Blad, Clara C. et al.: Biological and Pharmacological Roles of HCA Receptors. Advances in Pharmacology 62:219-250 (2011). [cited by applicant]
Blandini, Fabio. et al.: Glutamate and Parkinson's Disease. Molecular Neurobiology 12(1):73-94 (1996). [cited by applicant]
Boehncke, W H. Chapter 12: The Psoriasis SCIO Mouse Model: A Tool for Drug Discovery?. Ernst Schering Research Foundation Workshop 50:213-234 (2005). [cited by applicant]
Booth, Laurence. et al.: Regulation of Dimethyl-fumarate Toxicity by Proteasome Inhibitors. Cancer Biology and Therapy 15(12):1646-1657 (2014). [cited by applicant]
Booth, Lawrence et al.: Regulation of dimethyl-fumarate toxicity by proteasome inhibitors. Cancer Biology & Therapy 15(12):1646-1657 (2014). [cited by applicant]
Boros, M. et al.: Methods for syntheses of N-methyl-DL-aspartic acid derivatives. Amino Acids 33(4):709-717 (2007). [cited by applicant]
Brewer, L, and S. Rogers.: Fumaric Acid Esters In The Management Of Severe Psoriasis. Clinical Experimental Dermatology 32:246-249 (2007). [cited by applicant]
Bruhn, Claudia et al.: Concordance Between Enzyme Activity and Genotype of Glutathione S-transferase Theta (GSTT1). Biochemical Pharmacology 56(9):1189-1193 (1998). [cited by applicant]
Bundgaard, H. et al.: Esters of N,N-Disubstituted 2-Hydroxyacetamides as a Novel Highly Biolab le Prodrug Type for Carboxylic Acid Agents. Journal of Medicinal Chemistry 30(3):451-454 (1987). [cited by applicant]
Bundgaard, Hans: and Niels Mark Nielsen. Glycolamide Esters as a Novel Biolabile Prodrug Type for Non-steroidal Anti-inflammatory Carboxylic Acid Drugs. International Journal of Pharmaceutics 43:101-110 (1988). [cited by applicant]
Buyukcoskun, N I, and K Ozluk: Role Of Intracerebroventricular Vasopressin In The Development Of Stress-induced Gastric Lesions In Rats. Physiological Research 48(6):451-455 (1999). [cited by applicant]
Buyukcoskun, Naciye Isbil. et al.: Central Effects Of Glucagon-like Peptide-1 On Cold-restraint Stress-induced Gastric Mucosal Lesions. Turkish Journal of Gastroenterology 18(3):150-156 (2007). [cited by applicant]
Caira, Mino R.: Crystalline Polymorphism of Organic Compounds. In: Design of Organic Solids, Topics in Current Chemistry. Springer 198:163-208 (1998). [cited by applicant]
Camandola, Simonetta et al.: NF-κB as a Therapeutic Target in Neurodegenerative Diseases. Expert Opinion on Therapeutic Targets 11(2):123-132 (2007). [cited by applicant]
Capello, E. et al.: Marburg Type And Bald's Concentric Sclerosis: Rare And Acute Variants Of Multiple Sclerosis. Neurological Sciences 25 Suppl 4:S361-S363 (2004). [cited by applicant]
Carter, Stephen K.: Chemotherapy of Cancer, 2nd edition. John Wiley and Sons :362-365 (1981). [cited by applicant]
Cavarra, Eleonora. et al.: Effects Of Cigarette Smoke In Mice With Different Levels Of Alpha(1)-proteinase Inhibitor and Sensitivity To Oxidants. American Journal Of Respiratory And Critical Care Medicine 164(5):886-890… [cited by applicant]
Chaudhary, Amit. et al.: Enhancement of Solubilization and Bioavailability of Poorly Soluble Drugs By Physical and Chemical Modifications: A Recent Review. Journal of Advanced Pharmacy Education & Research 2(1):32-67 (2… [cited by applicant]
Chen, Huabing. et al.: Nanonization Strategies For Poorly Water-soluble Drugs. 16(7-8):354-360 (2011). [cited by applicant]
Cockcroft, D W. et al. Bronchial Reactivity To Inhaled Histamine: A Method And Clinical Survey. Clinical Allergy 7(3):235-243 (1977). [cited by applicant]
Cross, Stephanie A. et al.: Dimethyl Fumarate, An Immune Modulator And Inducer Of The Antioxidant Response, Suppresses HIV Replication And Macrophage-mediated Neurotoxicity: A Novel Candidate For HIV Neuroprotection. Jo… [cited by applicant]
D'Acquisto, Fulvio et al. Inhibition Of Nuclear Factor Kappa B (NF-B): An Emerging Theme In Anti-inflammatory Therapies. Molecular Interventions 2(1):22-35 (2002). [cited by applicant]
Damasio, Antonio R.: Alzheimer's Disease and Related Dementias. Cecil Textbook of Medicine, 20th edition 2:1992-1996 (1996). [cited by applicant]
De Jong, Rolien. et al.: Selective Stimulation of T Helper 2 Cytokine Responses by the Anti-psoriasis Agent Monomethylfumarate. European Journal of Immunology 26(9):2067-2074 (1996). [cited by applicant]
Dibbert, Stefan. et al.: Detection of Fumarate-glutathione Adducts in the Portal Vein Blood Of Rats: Evidence For Rapid Dimethylfumarate Metabolism. Archives of Dermatological Research 305(5):447-451 (2013). [cited by applicant]
Dymicky, Michael: Preparation of Monomethyl Fumarate. Organic Preparations and Procedures International 15(4): 233-238 (1983). [cited by applicant]
Eberle, Franziska C. et al.: Fumaric Acid Esters in Severe Ulcerative Necrobiosis Lipoidica: A Case Report And Evaluation of Current Therapies. Acta Dermato-Venereologica 90(1):104-106 (2010). [cited by applicant]
Ellrichmann, Gisa. et al.: Efficacy of Fumaric Acid Esters in the R6/2 And Yac128 Models of Huntington's Disease. PLoS One 6(1):e16172, 1-11 (2011). [cited by applicant]
Etter, Margaret C. et al.: Graph-set Analysis of Hydrogen-bond Patterns in Organic Crystals. Acta Crystallographica Section B46 (Pt 2):256-262 (1990). [cited by applicant]
Etter, Margaret C. et al.: Hydrogen Bond Directed Cocrystallization and Molecular Recognition Properties of Diarylureas. Journal of the American Chemical Society 112:8415-8426 (1990). [cited by applicant]
Etter, Margaret C. et al.: The Use of Cocrystallization as a Method of Studying Hydrogen Bond Preferences of 2-aminopyrimidine. Journal Of The Chemical Society 8:589-591 (1990). [cited by applicant]
Eugster, Hans-Pietro. et al.: Superantigen Overcomes Resistance of II-6-deficient Mice Towards MOG-induced EAE by a TNFR1 Controlled Pathway. European Journal of Immunology 31(8):2302-2312 (2001). [cited by applicant]
Feinstein, Douglas L. et al.: Anti-Inflammatory and Pro-Metabolic Effects of BG-12 in Glial Cells. Poster Presented at 26th Congress of the European Committee for Treatment and Research in Multiple Sclerosis (ECTRIMS) (… [cited by applicant]
Fox, Robert J. et al.: Placebo-controlled Phase 3 Study of Oral BG-12 or Glatiramer in Multiple Sclerosis. The New England Journal of Medicine 367(12):1087-1097 (2012). With Erratum 367(17):1673 (2012). [cited by applicant]
Frycak, Petr. et al.: Evidence of Covalent Interaction of Fumaric Acid Esters with Sulfhydryl Groups in Peptides. Journal of Mass Spectrometry 40(10):1309-1318 (2005). [cited by applicant]
Gadad, Andanappa K. et al.: Synthesis, Spectral Studies and Anti-inflammatory Activity of Glycolamide Esters of Niflumic Acid as Potential Prodrugs. Arzneimittelforschung 52(11):817-821 (2002). [cited by applicant]
Gambichler, T. et al.: Clearance of Necrobiosis Lipoidica with Fumaric Acid Esters. Dermatology 207(4):422-424 (2003). [cited by applicant]
Gesser, Borbala. et al.: Dimethylfumarate Specifically Inhibits The Mitogen and Stress-activated Kinases 1 and 2 (MSK1/2): Possible Role for its Anti-psoriatic Effect. Journal of Investigative Dermatology 127(9):2129-21… [cited by applicant]
Ghoreschi, Kamran. et al.: Fumarates Improve Psoriasis and Multiple Sclerosis by Inducing Type II Dendritic Cells. Journal of Experimental Medicine 208(11):2291-2303 (2011). [cited by applicant]
Goke, B. et al.: Effect of a Specific Serine Protease Inhibitor on the Rat Pancreas: Systemic Administration of Camostate and Exocrine Pancreatic Secretion. Digestion 30(3):171-178 (1984). [cited by applicant]
Gold, Ralf. et al.: Placebo-controlled Phase 3 Study of oral BG-12 for Relapsing Multiple Sclerosis. The New England Journal of Medicine 367(12):1098-1107 (2012). With Erratum 367(24):2362 (2012). [cited by applicant]
Gorbitz, Carl Henrik, and Hans-Petter Hersleth: On the Inclusion of Solvent Molecules in the Crystal Structures of Organic Compounds. Acta Crystallographica Section B56(Pt 3):526-534 (2000). [cited by applicant]
Griffin, G W. et al.: The Chemistry of Photodimers of Maleic and Fumaric Acid Derivatives. I. Dimethyl Fumarate Dimer. Journal of the American Chemical Society 83(12):2725-2728 (1961). [cited by applicant]
Grigorian, Ani: Control of T Cell-mediated Autoimmunity by Metabolite Flux To N-glycan Biosynthesis. Journal of Biological Chemistry 282(27):20027-20035 (2007). [cited by applicant]
Guenther, Claudia H. et al.: Macular Exanthema Due to Fumaric Acid Esters. Annals of Pharmacotherapy 37(2):234-236 (2003). [cited by applicant]
Gurney, Mark E. et al.: Motor Neuron Degeneration in Mice that Express a Human Cu,Zn Superoxide Dismutase Mutation. Science 264(5166):1772-1775 (1994). [cited by applicant]
Hanson, Julien. et al.: Nicotinic Acid- And Monomethyl Fumarate-induced Flushing Involves GPR109A Expressed by Keratinocytes and COX-2-dependent Prostanoid Formation In Mice. Journal of Clinical Investigation 120(8):291… [cited by applicant]
Heiligenhaus, .A et al.: Improvement of Herpetic Stromal Keratitis with Fumaric Acid Derivate is Associated with Systemic Induction of T Helper 2 Cytokines. Clinical and Experimental Immunology 142(1):180-187 (2005). [cited by applicant]
Heiligenhaus, A. et al.: Influence of Dimethylfumarate on Experimental HSV-1 Necrotizing Keratitis. Graefe's Archive for Clinical and Experimental Ophthalmology 242(10):870-877 (2004). [cited by applicant]
Hoefnagel, J.J. et al.: Long-term Safety Aspects of Systemic Therapy with Fumaric Acid Esters in Severe Psoriasis. British Journal of Dermatology 149(2):363-369 (2003). [cited by applicant]
Hoxtermann, S. et al.: Fumaric Acid Esters Suppress Peripheral CD4- and CD8-positive Lymphocytes in Psoriasis. Dermatology 196(2):223-230 (1998). [cited by applicant]
Hörig, Heidi et al.: From Bench to Clinic and Back: Perspective on the 1st IQPC Translational Research Conference. Journal of Translational Medicine 2:1-8 (2004). [cited by applicant]
Hurd, Charles D. et al.: Vinylation and the Formation of Acylals. Journal of the American Chemical Society 78(1):104-106 (1956). [cited by applicant]
Šilhavý, Jan. et al.: Fumaric Acid Esters can Block pro-inflammatory Actions of Human CRP and Ameliorate Metabolic Disturbances in Transgenic Spontaneously Hypertensive Rats. PLoS One 9(7): e101906, 1-9 (2014). [cited by applicant]
Iyer, Radhakrishnan P. et al.: Synthesis of lodoalkylacylates and their Use in the Preparation of S-alkyl Phosphorothiolates. Synthetic Communications 25(18):2739-2749 (1995). [cited by applicant]
Jamil, N. et al.: Studies on the Photostability of Reserpine in Parenteral Solutions. Die Pharmazie 38(7):467-469 (1983) Abstract. [cited by applicant]
Jennings, L, and GM Murphy: Squamous Cell Carcinoma as a Complication of Fumaric Acid Ester Immunosuppression. Journal of the European Academy of Dermatology and Venereology 23(12):1451 (2009). [cited by applicant]
Jurjus, Abdo R. et al.: Animal Models of Inflammatory Bowel Disease. Journal of Pharmacological and Toxicological Methods 50(2):81-92 (2004). [cited by applicant]
Kamimura, Akio. et al. Stereoselective Formation of Optically Active 2-oxy-1,3-oxazolidin-4-ones from Chiral 0-acylmandelamides or Lactamides. Tetrahedron 58:8763-8770 (2002). [cited by applicant]
Kappos, Ludwig. et al. Efficacy and Safety of Oral Fumarate in Patients with Relapsing-remitting Multiple Sclerosis: A Multicentre, Randomised, Double-blind, Placebo-controlled Phase IIb Study. Lancet 372(9648):1463-147… [cited by applicant]
Khan, M S Y etal: Synthesis and Biological Evaluation of Glycolamide Esters as Potential Prodrugs of Some Non-steroidal Anti-inflammatory Drugs. Indian Journal of Chemistry-Section B 41(10):2172-2175(2002). [cited by applicant]
Killestein, Joep. et al.: Oral Treatment for Multiple Sclerosis. Lancet Neurology 10(11):1026-1034 (2011). [cited by applicant]
Klein, A. et al.: Off-label Use of Fumarate Therapy for Granulomatous and Inflammatory Skin Diseases Other than Psoriasis Vulgaris: A Retrospective Study. Journal of the European Academy of Dermatology and Venereology 2… [cited by applicant]
Kreuter, A. et al.: Fumaric Acid Esters in Necrobiosis Lipoidica: Results of a Prospective Noncontrolled Study. British Journal of Dermatology 153(4):802-807 (2005). [cited by applicant]
Kumar, Senthil V S. et al.: Molecular Complexes of Some Mono- and Dicarboxylic Acids with trans-1,4-Dithiane-1,4-dioxide. Crystal Growth & Design 2(4):313-318 (2002). [cited by applicant]
Layzer, Robert B.: Second Five—Degenerative Diseases of the Nervous System. Cecil Textbook of Medicine 2:2050-2057 (1996). [cited by applicant]
Lee, De-Hyung. et al.: Spotlight on Fumarates. International MS Journal 15(1):12-18 (2008). [cited by applicant]
Lehmann, Joachim C U. et al.: Dimethylfumarate Induces Immunosuppression Via Glutathione Depletion and Subsequent Induction of Heme Oxygenase 1. Journal of Investigative Dermatology 127(4):835-845 (2007). [cited by applicant]
Lehmann, Manfred. et al.: Fumaric Acid Esters Are Potent Immunosuppressants: Inhibition of Acute and Chronic Rejection in Rat Kidney Transplantation Models by Methyl Hydrogen Fumarate. Arch Dermatol Res 294(9):399-404 (… [cited by applicant]
Linker, Ralf A. et al.: Fumaric Acid Esters Exert Neuroprotective Effects in Neuroinflammation via Activation of the Nrf2 Antioxidant Pathway. Brain 134(3):678-692 (2011). [cited by applicant]
Linker, Ralf A. et al.: Identification and Development of New Therapeutics For Multiple Sclerosis. Trends in Pharmacological Sciences 29(11):558-565 (2008). [cited by applicant]
Litjens, N H R. et al.: Effects Of Monomethylfumarate On Dendritic Cell Differentiation. British Journal of Dermatology 154(2):211-217 (2006). [cited by applicant]
Litjens, Nicolle H R. et al.: Monomethylfumarate Affects Polarization of Monocyte-derived Dendritic Cells Resulting in Down-regulated Th1 Lymphocyte Responses. European Journal of Immunology 34(2):565-575 (2004). [cited by applicant]
Litjens, Nicolle HR. et al.: Pharmacokinetics of Oral Fumarates in Healthy Subjects. British journal of clinical pharmacology 58(4):429-432 (2004). [cited by applicant]
Loewe, Robert. et al.: Dimethylfumarate Impairs Melanoma Growth And Metastasis. Cancer Research 66(24):11888-11896 (2006). [cited by applicant]
Loewe, Robert. et al.: Dimethylfumarate Inhibits TNF-induced Nuclear Entry of NF-κB/P65 in Human Endothelial Cells. The Journal of Immunology 168(9):4781-4787 (2002). [cited by applicant]
Lopez-Diego, Rocio S. et al.: Novel Therapeutic Strategies For Multiple Sclerosis—A Multifaceted Adversary. Nature Reviews Drug Discovery 7(11):909-925 (2008). [cited by applicant]
Los, M. et al.: New Esters of Substituted Anilinonicotinic and Phenylanthranilic Acids. Il Farmaco; Edizione Scientifica 36(5):372-385 (1981). [cited by applicant]
Mandhane, Sanjay N. et al.: Adenosine A2 Receptors Modulate Haloperidol-induced Catalepsy In Rats. European Journal of Pharmacology 328(2-3):135-141 (1997). [cited by applicant]
Mannervik, Bengt. et al.: Identification of Three Classes of Cytosolic Glutathione Transferase Common to Several Mammalian Species: Correlation Between Structural Data and Enzymatic Properties. Proceedings of the Nation… [cited by applicant]
Martin, Joseph B.: Molecular Basis of the Neurodegenerative Disorders. New England Journal of Medicine 340(25):1970-1980 (2005). [cited by applicant]
Martorana, Piero A. et al.: Roflumilast Fully Prevents Emphysema In Mice Chronically Exposed To Cigarette Smoke. American Journal of Respiratory and Critical Care Medicine 172(7):848-853 (2005). [cited by applicant]
Meissner, Markus. et al.: Dimethyl Fumarate-only an Anti-psoriatic Medication?. JDDG: Journal der Deutschen Dermatologischen Gesellschaft 10(11):793-801 (2012). [cited by applicant]
Menter, Alan. et al.: Guidelines of Care for the Management of Psoriasis and Psoriatic Arthritis. Journal of the American Academy of Dermatology 61(3):451-485 (2009). [cited by applicant]
Merisko-Liversidge, Elaine. et al.: Nanosizing: A Formulation Approach For Poorly-water-soluble Compounds. European Journal of Pharmaceutical Sciences 18(2):113-120 (2003). [cited by applicant]
Miller, Stephen D, and William J Karpus: Chapter 15 Experimental Autoimmune Encephalomyelitis in the Mouse. Current Protocols in Immunology 88(1):15.1.1-15.1.18, 1-18 (2007). [cited by applicant]
Milo, Ron, and Hillel Panitch: Combination Therapy in Multiple Sclerosis. Journal of Neuroimmunology 231(1-2):23-31 (2011). Published online Dec. 15, 2010. [cited by applicant]
Mosmann, TRt, and R. L. Coffman: TH1 and TH2 cells: Different Patterns of Lymphokine Secretion Lead to Different Functional Properties. Annual Review of Immunology 7(1):145-173 (1989). [cited by applicant]
Mrowietz, Ulrich, and Khusru Asadullah: Dimethylfumarate for Psoriasis: More than a Dietary Curiosity. Trends in Molecular Medicine 11(1):43-48 (2005). [cited by applicant]
Mrowietz, Ulrich. et al.: Treatment of Psoriasis with Fumaric Acid Esters (Fumaderm). Journal of the German Dermatological Society 5(8):716-717 (2007). [cited by applicant]
Mrowietz, Ulrich. et al.: Treatment of Psoriasis with Fumaric Acid Esters: Results of a Prospective Multicentre Study. German Multicentre Study. British Journal of Dermatology 138(3):456-460 (1998). [cited by applicant]
Mrowietz, Ulrich. et al.: Treatment of Severe Psoriasis With Fumaric Acid Esters: Scientific Background and Guidelines for Therapeutic Use. British Journal of Dermatology 141(3):424-429 (1999). [cited by applicant]
Muller, Michael. et al.: High-performance Liquid Chromatography/fluorescence Detection of S-methylglutathione Formed by Glutathione-s-transferase T1 in Vitro. Archives of Toxicology 74(12):760-767 (2001). [cited by applicant]
Murakami, Akira. et al.: Suppression of Dextran Sodium Sulfate-induced Colitis in Mice by Zerumbone, A Subtropical Ginger Sesquiterpene, and Nimesulide: Separately and in Combination. Biochemical Pharmacology 66(7):1253… [cited by applicant]
Naldi, Luigi, and Berthold Rzany: Psoriasis (Chronic Plaque). BMJ Clinical Evidence 2009:1706, 1-109 (2009). [cited by applicant]
Nelson, Kasey C. et al.: Effect of Dietary Inducer Dimethylfumarate on Glutathione in Cultured Human Retinal Pigment Epithelial Cells. Investigative Ophthalmology & Visual Science 40(9):1927-1935 (1999). [cited by applicant]
Neymotin, Arie. et al.: Neuroprotective Effect of Nrf2/ARE Activators, CDDO Ethylamide and CDDO Trifluoroethylamide, in a Mouse Model Of Amyotrophic Lateral Sclerosis. Free Radical Biology and Medicine 51(1):88-96 (2011… [cited by applicant]
Nibbering, P H. et al.: Intracellular Signalling by Binding Sites for the Antipsoriatic Agent Monomethylfumarate on Human Granulocytes. British Journal Of Dermatology 137(1):65-75 (1997). [cited by applicant]
Nielsen, Niels Mrk, and Hans Bundgaard: Glycolamide Esters as Biolabile Prodrugs of Carboxylic Acid Agents: Synthesis, Stability, Bioconversion, and Physicochemical Properties. Journal of Pharmaceutical Sciences 77(4):2… [cited by applicant]
O'Donnell et al.: Remington The Science and Practice of Pharmacy, 21st Edition, 2005, Chapter 52, pp. 1025-1036. [cited by applicant]
Offermanns, Stefan: The Nicotinic Acid Receptor GPR109A (HM74A or PUMA-G) as a New Therapeutic Target. Trends in Pharmacological Sciences 27(7):384-390 (2006). [cited by applicant]
O'Toole, Dermot. et al.: Treatment of Carcinoid Syndrome: A Prospective Crossover Evaluation of Lanreotide Versus Octreotide in Terms of Efficacy, Patient Acceptability, and Tolerance. Cancer 88(4):770-776 (2000). [cited by applicant]
Panagiotou, Thomai, and Robert J Fisher: Form Nanoparticles Via Controlled Crystallization. Chemical Engineering Progress 104(10):33-39 (2008). [cited by applicant]
Pathak, Pankaj. et al.: Supercritical Fluid Technology for Enhanced Drug Delivery. Expert Opinion On Drug Delivery 2(4):747-761 (2005). [cited by applicant]
Peeters, A J. et al.: Fumaric Acid Therapy for Psoriatic Arthritis. A Randomized, Double-blind, Placebo-Controlled Study. Rheumatology 31(7):502-504 (1992). [cited by applicant]
Pemble, Sally. et al.: Human Glutathione S-transferase Theta (GSTT1): cDNA Cloning and the Characterization of a Genetic Polymorphism. Biochemical Journal 300(1):271-276 (2004). [cited by applicant]
Rantanen, Tapio: The Cause of the Chinese Sofa/Chair Dermatitis Epidemic is Likely to be Contact Allergy to Dimethylfumarate, A Novel Potent Contact Sensitizer. British Journal Of Dermatology 159(1):218-221 (2008). [cited by applicant]
Reddingius, Wiebrandus Gerardus: Bioanalysis and Pharmacokinetics of Fumarates in Humans. Diss. ETH Zurich (1997). [cited by applicant]
Reich, Kristian. et al.: Efficacy and Safety of Fumaric Acid Esters in the Long-Term Treatment of Psoriasis—A Retrospective Study (Future). JDDG: Journal Der Deutschen Dermatologischen Gesellschaft 7(7):603-610 (2009). [cited by applicant]
Richman, Jeremy G. et al.: Nicotinic Acid Receptor Agonists Differentially Activate Downstream Effectors. Journal of Biological Chemistry 282(25):18028-18036 (2007). [cited by applicant]
Roll, Antonie. et al.: Use of Fumaric Acid Esters in Psoriasis. Indian J Dermatol Venereol Leprol 73(2):133-137 (2007). [cited by applicant]
Rostami-Yazdi, Martin. et al.: Detection of Metabolites of Fumaric Acid Esters in Human Urine: Implications for their Mode of Action. The Journal of Investigative Dermatology 129(1):231-234 (2009). [cited by applicant]
Rostami-Yazdi, Martin. et al.: Pharmacokinetics of Anti-psoriatic Fumaric Acid Esters in Psoriasis Patients. Archives of Dermatological Research 302:531-538 (2010). [cited by applicant]
Rowland, Lewis P, and Neil A. Shneider: Amyotrophic lateral sclerosis. New England Journal of Medicine 344(22):1688-1700 (2001). [cited by applicant]
Rubant, Simone A. et al.: Dimethylfumarate Reduces Leukocyte Rolling in Vivo Through Modulation of Adhesion Molecule Expression. Journal of Investigative Dermatology 128(2):326-331 (2008). [cited by applicant]
Sawant, Kamlesh D, and Tushar A. Naik: Necessity of Establishing Chemical Integrity of Polymorphs of Drug Substance Using a Combination of NMR, HPLC, Elemental Analysis, and Solid-state Characterization Techniques: case… [cited by applicant]
Schafer, Stefan et al.: Failure is an Option: Learning from Unsuccessful Proof-of-concept Trials. Drug Discovery Today 13(21-22):913-916 (2008). [cited by applicant]
Schilling, S. et al.: Fumaric Acid Esters are Effective in Chronic Experimental Autoimmune Encephalomyelitis and Suppress Macrophage Infiltration. Clinical and Experimental Immunology 145(1):101-107 (2006). [cited by applicant]
Schimrigk, S. et al.: Oral fumaric acid esters for the treatment of active multiple sclerosis: an open-label, baseline-controlled pilot study. European journal of neurology 13(6):604-610 (2006). [cited by applicant]
Schmidt, Thomas J. et al.: Reactivity of Dimethyl Fumarate and Methylhydrogen Fumarate Towards Glutathione and N-acetyl-L-cysteine-preparation of S-substituted Thiosuccinic Acid Esters. Bioorganic and Medicinal Chemistr… [cited by applicant]
Seder, Robert A, and William E. Paul.: Acquisition of Lymphokine-producing Phenotype by Cd4+ T Cells. Annual Review of Immunology 12:635-673 (1994). [cited by applicant]
Shan, Ning, and Michael J. Zaworotko: The Role of Cocrystals in Pharmaceutical Science. Drug Discovery Today 13(9-10):440-446 (2008). [cited by applicant]
Sharma, Pritam Dev, et al.: Distal Effect on Mass Spectral Fragmentations of Glycolamide Esters of 6-methoxy-2-naphthylacetic Acid (6-mna) and the Crystal Structure of N, N′-dimethylglycolamide Ester of 6-MNA. Indian Jo… [cited by applicant]
Sheikh, Sarah. et al.: Safety, Tolerability, and Pharmacokinetics of Bg-12 Administered with and Without Aspirin: Key Findings From a Randomized, Double-blind, Placebo-controlled Trial in Healthy Volunteers. Poster PO4.… [cited by applicant]
Sorensen, Per Soelberg, and Finn Sellebjerg: Oral Fumarate for Relapsing-remitting Multiple Sclerosis. Lancet 372(9648):1447-1448 (2008). [cited by applicant]
Spatz, Sydney M. et al.: Methyl Hydrogen Fumarate. The Journal of Organic Chemistry 23(10):1559-1560 (1958). [cited by applicant]
Spencer, Roxanne P. Tecfidera: An Approach for Repurposing. Pharmaceutical Patent Analyst 3(2):183-198 (2014). [cited by applicant]
Spencer, Sharon R. et al.: Induction of Glutathione Transferases and Nad(P)H:Quinone Reductase by Fumaric Acid Derivatives in Rodent Cells and Tissues. Cancer Research 50(24):7871-7875 (1990). [cited by applicant]
Sprenger, Raimund. et al.: Characterization of the Glutathione S-transferase GSTT1 Deletion: Discrimination of all Genotypes by Polymerase Chain Reaction Indicates a Trimodular Genotype-phenotype Correlation. Pharmacoge… [cited by applicant]
Steckel, Hartwig, and Katrin Jess: The extrusion and Speronization of Chitosan. Pharmaceutical Technology Europe, Jul. 2, 1989; [retrieved on Aug. 6, 2024]. Retrieved at URL:https://www.pharmtech.com/view/extrusion-and-… [cited by applicant]
Stoof, T J. et al.: The Antipsoriatic Drug Dimethylfumarate Strongly Suppresses Chemokine Production in Human Keratinocytes and Peripheral Blood Mononuclear Cells. British Journal Of Dermatology 144(6):1114-1120 (2001). [cited by applicant]
Tabruyn, Sebastien P, and Arjan W Griffioen: NF-κB: a New Player in Angiostatic Therapy. Angiogenesis 11(1):101-106 (2008). [cited by applicant]
Talath, Sirajunisa. et al.: Stability Studies of Some Glycolamide Ester Prodrugs of Niflumic Acid in Aqueous Buffers and Human Plasma by HPLC With UV Detection. Arzneimittelforschung 56(09):631-639 (2006). [cited by applicant]
Talath; Sirajunisa et al.: Synthesis, Stability Studies, Anti-inflammatory Activity and Ulcerogenicity of Morpholinoalkyl Ester Prodrugs of Niflumic Acid. Arzneimittelforschung 56(11):744-752 (2006). DOI: 10.1055/s-0031… [cited by applicant]
Tammara, Vijay K. et al.: Morpholinoalkyl Ester Prodrugs of Diclofenac: Synthesis, In Vitro and In Vivo Evaluation. Journal of Pharmaceutical Sciences 83(5):644-648 (1994). [cited by applicant]
Tammara; V.K. et al.: Morpholinoalkyl ester prodrugs of diclofenac: synthesis, in vitro and in vivo evaluation. J. Pharm. Sci. 83(5):644-8 (1994). doi: 10.1002/jps.2600830510. (Abstract). [cited by applicant]
Tang, Hua. et al.: The Psoriasis Drug Monomethylfumarate is a Potent Nicotinic Acid Receptor Agonist. Biochemical and Biophysical Research Communications 375(4):562-565 (2008). [cited by applicant]
Thing, Mette. et al.: Prolonged Naproxen Joint Residence Time After Intra-articular Injection of Lipophilic Solutions Comprising a Naproxen Glycolamide Ester Prodrug in the Rat. International Journal of Pharmaceutics 45… [cited by applicant]
Thomson, A. W. et al.: FK 506: A Novel Immunosuppressant for Treatment of Autoimmune Disease: Rationale and Preliminary Clinical Experience at the University of Pittsburgh. Springer Seminars in Immunopathology 14(4):323… [cited by applicant]
Tracey, Daniel. et al.: Tumor Necrosis Factor Antagonist Mechanisms of Action: a Comprehensive Review. Pharmacology and Therapeutics 117(2):244-279 (2008). [cited by applicant]
Treumer, Felix. et al.: Dimethylfumarate is a Potent Inducer of Apoptosis in Human T Cells. Journal of investigative dermatology 121(6):1383-1388 (2003). [cited by applicant]
U.S. Appl. No. 14/223,026 Notice of Allowance dated Aug. 30, 2018. [cited by applicant]
U.S. Appl. No. 14/223,026 Office Action dated Aug. 22, 2017. [cited by applicant]
U.S. Appl. No. 14/223,026 Office Action dated Dec. 2, 2015. [cited by applicant]
U.S. Appl. No. 14/223,026 Office Action dated Feb. 10, 2017. [cited by applicant]
U.S. Appl. No. 14/223,026 Office Action dated Jun. 2, 2016. [cited by applicant]
U.S. Appl. No. 14/223,026 Office Action dated Mar. 9, 2018. [cited by applicant]
U.S. Appl. No. 16/206,521 Notice of Allowance dated Oct. 23, 2019. [cited by applicant]
U.S. Appl. No. 16/749,427 Notice of Allowance dated Sep. 24, 2021. [cited by applicant]
U.S. Appl. No. 16/749,427 Office Action dated Oct. 20, 2020. [cited by applicant]
U.S. Appl. No. 17/551,550 Corrected Notice of Allowability dated Jan. 19, 2024. [cited by applicant]
U.S. Appl. No. 17/551,550 Notice of Allowance dated Jan. 8, 2024. [cited by applicant]
U.S. Appl. No. 17/551,550 Office Action dated Jul. 3, 2023. [cited by applicant]
Van Der Fits, Leslie. et al.: Imiquimod-induced Psoriasis-like Skin Inflammation in Mice is Mediated via the II-23/II-17 Axis. Journal of Immunology 182(9):5836-5845 (2009). [cited by applicant]
Van Schoor, Jan. et al.: Effect of Inhaled Fluticasone on Bronchial Responsiveness to Neurokinin A in Asthma. European Respiratory Journal 19(6):997-1002 (2002). [cited by applicant]
Van Schoor, Jan. et al.: The Effect of the NK2 Tachykinin Receptor Antagonist SR 48968 (saredutant) on Neurokinin A-induced Bronchoconstriction in Asthmatics. European Respiratory Journal 12(1):17-23 (1998). [cited by applicant]
Vandermeeren, Marc. et al.: Dimethylfumarate is an Inhibitor of Cytokine-induced E-selectin, VCAM-1, and ICAM-1 Expression in Human Endothelial Cells. Biochemical and Biophysical Research Communications 234(1):19-23 (19… [cited by applicant]
Villegas, Isabel. et al.: A New Flavonoid Derivative, Dosmalfate, Attenuates the Development of Dextran Sulphate Sodium-induced Colitis in Mice. International Immunopharmacology 3(13-14):1731-1741 (2003). [cited by applicant]
Virley, David J.: Developing Therapeutics for the Treatment of Multiple Sclerosis. NeuroRx : the Journal of the American Society for Experimental Neuro Therapeutics 2(4):638-649 (2005). [cited by applicant]
Vishweshwar, Peddy. et al.: Pharmaceutical Co-crystals. Journal of Pharmaceutical Sciences 95(3):499-516 (2006). [cited by applicant]
Wain, E M. et al.: Treatment of Severe, Recalcitrant, Chronic Plaque Psoriasis With Fumaric Acid Esters: a Prospective Study. British Journal of Dermatology 162(2):427-434 (2010). [cited by applicant]
Wakkee, Marlies, and H.: Bing Thio. Abstract: Drug evaluation: BG-12, an immunomodulatory dimethylfumarate. Current Opinion in Investigational Drugs 8(11):955-962 (2007). [cited by applicant]
Weber, H. et al.: Synthesis, in Vitro Skin Permeation Studies, and PLS-analysis of New Naproxen Derivatives. Pharmaceutical Research 18(5):600-607 (2001). [cited by applicant]
Weber, H Oliver. et al.: Treatment of Disseminated Granuloma Annulare With Low-dose Fumaric Acid. Acta Dermato-venereologica 89(3):295-298 (2009). [cited by applicant]
Werdenberg, D. et al.: Presystemic Metabolism and Intestinal Absorption of Antipsoriatic Fumaric Acid Esters. Biopharmaceutics & Drug Disposition 24(6):259-273 (2003). [cited by applicant]
Whiteley, P E, and S A Dalrymple: Models of Inflammation: Measuring Gastrointestinal Ulceration in the Rat. Current Protocols in Pharmacology 10:10.2.1_10.2.4 (1998). [cited by applicant]
Wingerchuk, Dean M. et al.: Multiple Sclerosis: Current Pathophysiological Concepts. Laboratory Investigation 81(3):263-281 (2001). [cited by applicant]
Winkler, B S. et al.: Oxidative Damage and Age-related Macular Degeneration. Molecular Vision 5:32, 1-15 (1999). [cited by applicant]
Wu, Kuei-meng, and James G Farrelly: Regulatory Perspectives of Type II Prodrug Development and Time-dependent Toxicity Management: Nonclinical Pharm/Tox Analysis and the Role of Comparative Toxicology. Toxicology 236(1… [cited by applicant]
Yamada. et al.: Synthesis and Polymerization of Unsaturated Dibasic Acid Derivatives. Yuki Gosei Kaqaku Kvokaishi 23(2):1-19 (1965). [cited by applicant]
Yang, Lichuan. et al.: Neuroprotective Effects of the Triterpenoid, CDDO Methyl Amide, a Potent Inducer of Nrf2-mediated Transcription. Public Library of Science one 4(6):e5757, 1-13 (2009). [cited by applicant]
Yazdi, Martin Rostami, and Ulrich Mrowietz: Fumaric acid esters. Clinics in Dermatology 26(5):522-526 (2008). [cited by applicant]
Zhu, K, and U Mrowietz: Inhibition of Dendritic Cell Differentiation by Fumaric Acid Esters. Journal of Investigative Dermatology 116(2):203-208 (2001). [cited by applicant]
Behari, Madhuri et al.: Baseline Characteristics of a Subpopulation of Indian Patients Enrolled in Two Phase 3 Trials for Oral BG-12 in Relapsing-Remitting Multiple Sclerosis. Poster Presented at 62nd Annual Meeting Ame… [cited by applicant]
Benoit, P. et al.: Clinical Study of the Beta-morpholinoethylester of Niflumic Acid in Children's Dentistry. Revue D'odonto-stomatologie Du Midi De La France 4:249-261 (1975). [cited by applicant]
Dawson, K.T. et al.: Bioequivalence of BG-12 (Dimethyl Fumarate) Administered as a Single 240 mg Capsule and Two 120 mg Capsules: Findings from a Randomized, Two-period Crossover Study. Poster P913 presented at the 28th… [cited by applicant]
European Commission Health & Consumer Protection Directorate-General, Report of the scientific committee on animal nutrition on the safety of fumaric acid (2003). [cited by applicant]
FDA mulls drug to slow late-stage Alzheimer's, Associated CNN press, Sep. 24, 2003. Retrieved from URL: http://www.cnn.com/2003/HEALTH/conditions/09/24/alzheimers.drug.apfmd ex.html. pp. 1-2. [cited by applicant]
FDA-Department of Health and Human Services, International Conference on Harmonisation; Guidelines for the Photostability Testing of New Drug Substances and Products. Federal Register 62(95):27116-27122 (1997). [cited by applicant]
Fox, Robert et al.: Baseline characteristics of patients in a randomized, multicenter, placebo- controlled and active comparator trial evaluating efficacy and safety of BG-12 in relapsing-remitting multiple sclerosis: t… [cited by applicant]
Gogas, K. et al.: Comparison of the efficacy and tolerability of a novel methyl hydrogen fumarate prodrug with dimethyl fumarate in rodent EAR and GI Irritation models. Multiple Sclerosis 16(10 Suppl):S230-S231 (2010). [cited by applicant]
Gold, Ralf et al.: Baseline characteristics of patients in the DEFINE trial: a randomized, multicenter, double blind, placebo-controlled, phase 3 study of BG-12 in relapsing-remitting multiple sclerosis. Poster Presente… [cited by applicant]
Lei et al.: Novel Technology of Dimethyl Fumarate Synthesis. Ziyuan Kaifa Yu Shichang 27(9):787-789 (2011). [cited by applicant]
McGinity, J.W. et al.: Aqueous Polymeric Coatings for Pharmaceutical Dosage Forms. Third Edition, CRC Press, 2008. pp. 1-488 (abstract). [cited by applicant]
Pharmapedia (http://pharmapedia.wikidot.com/film-coating-materials-and-their-properties) accessed Aug. 8, 2017, pp. 1-25. [cited by applicant]
Wadhwa, L K, and P D Sharma: Glycolamide Esters of 6-methoxy-2-naphthylacetic Acid as Potential Pro-drugs-synthetic and Spectral Studies. Indian Journal Of Chemistry Section B-organic Chemistry Including Medicinal Chemi… [cited by applicant]
Wang, W.P. et al.: Evidence-Based Treatment of Chronic Leg Ulcers in A Patient with Necrobiosis Lipoidica Diabeticorum. Chinese Journal of Evidence-Based Medicine 7(11):830-835 (2007). [cited by applicant]
Woodworth, J. et al.: Oral Bg-12 in Combination with interferon Beta-1A or Glatiramer Acetate: Pharmacokinetics, Safety and Tolerability. Poster P478 Presented at: European Committee for Treatment and Research in Multip… [cited by applicant]
Woodworth, James et al.: Pharmacokinetics of Oral BG-12 Alone Compared with BG-12 and Interferon beta-1a or Glatiramer Acetate Administered Together, Studied in Healthy Volunteers. Poster P04.207 presented at the 62nd A… [cited by applicant]
Xenoport, Inc.: XenoPort announces presentation of preclinical data for novel fumarate analog XP23829 at ECTRIMS. Biospace, Oct. 13, 2010. Available at URL:https://www.biospace.com/xenoport-inc-announces-presentation-of… [cited by applicant]
Zhang, Ming et al.: Synthesis of Dimethyl Fumarate with Orthogonal Test. Jingxi Huaqonq Zhongjian 36(6):71-72 (2006). [cited by applicant]
Zhao, Wen-Xiu et al.: Synthesis and antimicrobial active of monomethyl fumarate. Shipin Gonqye Keii 29(6):259-262 (2008). [cited by applicant]
Zheng, Chao et al.: Improved Preparation of Monomethyl Fumarate. Huaxue Shiiie 45(4):207-208, 217 (2004). [cited by applicant]