US 4202876A
· Monks et al.
· 1980
[cited by applicant]
US 5466815A
· Enhsen et al.
· 1995
[cited by applicant]
US 5512558A
· Enhsen et al.
· 1996
[cited by applicant]
US 5541348A
· Ayra et al.
· 1996
[cited by applicant]
US 5571809A
· Hargrave et al.
· 1996
[cited by applicant]
US 5646316A
· Jacobson et al.
· 1997
[cited by applicant]
US 5656277A
· Berlati et al.
· 1997
[cited by applicant]
US 6974830B2
· Giegrich et al.
· 2005
[cited by applicant]
US 7319109B2
· Boggs et al.
· 2008
[cited by applicant]
US 7846960B2
· Bell et al.
· 2010
[cited by applicant]
US 7858608B2
· Pellicciari et al.
· 2010
[cited by applicant]
US 7863302B2
· Bell et al.
· 2011
[cited by applicant]
US 7897773B2
· Aletru et al.
· 2011
[cited by applicant]
US 7902373B2
· Blake et al.
· 2011
[cited by applicant]
US 8952042B2
· Kremoser et al.
· 2015
[cited by applicant]
US 9751874B2
· Gege et al.
· 2017
[cited by applicant]
US 20050054559A1
· Gallop et al.
· 2005
[cited by applicant]
US 20060287374A1
· Barf et al.
· 2006
[cited by applicant]
US 20070054902A1
· Fukui et al.
· 2007
[cited by applicant]
US 20090131384A1
· Uysal et al.
· 2009
[cited by applicant]
US 20090163474A1
· Zhang et al.
· 2009
[cited by applicant]
US 20100063697A1
· Lindgren et al.
· 2010
[cited by applicant]
US 20100099703A1
· Garcia-López et al.
· 2010
[cited by applicant]
US 20100120775A1
· Bass et al.
· 2010
[cited by applicant]
US 20100184809A1
· Kremoser et al.
· 2010
[cited by applicant]
US 20100249179A1
· Deaton et al.
· 2010
[cited by applicant]
US 20110034507A1
· Akwabi-Ameyaw et al.
· 2011
[cited by applicant]
US 20130034536A1
· Gedulin
· 2013
[cited by applicant]
US 20130261108A1
· Tully et al.
· 2013
[cited by applicant]
US 20140057953A1
· Hartmann et al.
· 2014
[cited by applicant]
US 20140187633A1
· Manku et al.
· 2014
[cited by applicant]
US 20140206657A1
· Yu et al.
· 2014
[cited by applicant]
US 20150112089A1
· Finch et al.
· 2015
[cited by applicant]
US 20150366856A1
· Mutnick et al.
· 2015
[cited by applicant]
US 20160176917A1
· Wang et al.
· 2016
[cited by applicant]
US 20170368038A1
· Badman et al.
· 2017
[cited by applicant]
US 20180148470A1
· Li et al.
· 2018
[cited by applicant]
CN 105669811A
· 2016
[cited by applicant]
CN 106478759A
· 2017
[cited by applicant]
CN 106518946
· 2017
[cited by applicant]
CN 105669811
· 2020
[cited by applicant]
EP 0583566A2
· 1994
[cited by applicant]
EP 1364645A1
· 2003
[cited by applicant]
EP 1947108A1
· 2008
[cited by applicant]
JP H1160594A
· 1999
[cited by applicant]
JP H11109628A
· 1999
[cited by applicant]
KR 20090104622A
· 2009
[cited by applicant]
WO 8702367A2
· 1987
[cited by applicant]
WO 9526325A1
· 1995
[cited by applicant]
WO 0037077A1
· 2000
[cited by applicant]
WO 0228881A1
· 2002
[cited by applicant]
WO 03030612A2
· 2003
[cited by applicant]
WO 03086303A2
· 2003
[cited by applicant]
WO 2004046162A2
· 2004
[cited by applicant]
WO 2005042513A1
· 2005
[cited by applicant]
WO 2005089316A2
· 2005
[cited by applicant]
WO 2007089907A2
· 2007
[cited by applicant]
WO 2007095174A2
· 2007
[cited by applicant]
WO 2008009407A2
· 2008
[cited by applicant]
WO 2008091540A2
· 2008
[cited by applicant]
WO 2010093845A1
· 2010
[cited by applicant]
WO 2011020615A1
· 2011
[cited by applicant]
WO 2013007387A1
· 2013
[cited by applicant]
WO 2013020108A2
· 2013
[cited by applicant]
WO 2013166176A1
· 2013
[cited by applicant]
WO 2013192097A1
· 2013
[cited by applicant]
WO 2014036379A2
· 2014
[cited by applicant]
WO 2014184271A1
· 2014
[cited by applicant]
WO 2015017813A2
· 2015
[cited by applicant]
WO 2015181275A1
· 2015
[cited by applicant]
WO 2016073767A1
· 2016
[cited by applicant]
WO 2016086169A1
· 2016
[cited by applicant]
WO 2016130809A1
· 2016
[cited by applicant]
WO 2016173493A1
· 2016
[cited by applicant]
WO 2016173524A1
· 2016
[cited by applicant]
WO 2016205475A2
· 2016
[cited by applicant]
WO 2017027396A1
· 2017
[cited by applicant]
WO 2017053826A1
· 2017
[cited by applicant]
WO 2017129125A1
· 2017
[cited by applicant]
WO 2018085148A1
· 2018
[cited by applicant]
WO 2018091540A1
· 2018
[cited by applicant]
Mosesin-4 at www.chemspider.com/Chemical-Structure.10375019.html (retrieved from the internet Oct. 11, 2016).
[cited by applicant]
“PubChem-CID-122592927, Create Date: Dec. 8, 2016”.
[cited by applicant]
“PubChem-CID-122592945, Create Date: Dec. 8, 2016”.
[cited by applicant]
Ali , “Recent advances in the development of farnesoid X receptor agonists”, Ann Transl Med, 3(1), 2015, 1-16.
[cited by applicant]
Ballatore, C. , “Carboxylic Acid (Bio)Isosteres in Drug Design”, ChemMedChem., 8(3), 2013, 385-395.
[cited by applicant]
Banker, G. S, “Prodrugs”, Modern Pharmaceutics, 3rd., Marcel Dekker, Inc., NY, 1996, 2 pgs.
[cited by applicant]
Briere, D. A, “Novel small molecule agonist of TGR5 possesses anti-diabetic effects but causes gallbladder filling in mice”, PLoS, one, vol. 10(8), Cited in 1284-Cited in Some Related Cases—Didn't Remove—Take Out on a C…
[cited by applicant]
Bundgaard, H. , “Design of Prodrugs: Bioreversible derivatives for various functional groups and chenmical entitites”, Hans Bundgaard: “Design of Prodrugs”, Elsevier, Amsterdam, New York, Oxford; Chapeter 1, 1985.
[cited by applicant]
Coleman, J. P, “Metabolic Fate and Hepatocyte Toxicity of Reverse Amide Analogs of Conjugated Ursodeoxycholate in the Rat”, J. Steroid Biochem. Molec. Biol., vol. 64, No. 1/2, 1998, 91-101.
[cited by applicant]
Crawley , “Farnesoid X Receptor Modulators: a patent review”, Expert Opinion on Therapeutic Patents, 20(8), 2010, 1047-1057.
[cited by applicant]
Dyck, L. E, “Effects of Deuterium Substitution on the Catabolismof beta-Phenylethylamine: An In Vivo Study”, J. of Neurochemistry, 46, Cite in 1284 Only, 1986, 399-404.
[cited by applicant]
Fini, A. , “Basic Cholane Derivatives. XI: Comparison between Acid and Basic Derivatives”, Journal of Pharmaceutical Sciences, vol. 81, No. 7, 1992, 726-730.
[cited by applicant]
Fini, A. , “Quantitative Structure-Antimicrobial Activity Relationship in 5B-Cholanyl-24-benzylamine Derivatives”, Journal of Pharmaceutical Sciences, vol. 79, No. 7, 1990, 603-605.
[cited by applicant]
Gioiello, A , “Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3[alpha], 7[alpha]dihydroxy-6[alpha]-ethyl-24-nor-5[beta]-ch o I an-23-amine”, Bioorganic & Medicinal Chem., 19(8), Apr. 15…
[cited by applicant]
Griffiths, W. J, “Charge-remote fragmentation of bile acids derivatized with amino-sulphonic acids”, Rapid Communications in Mass Spectrometry, vol. 7, No. 3, Mar. 1, 1993, 235-240.
[cited by applicant]
Herr, R. J, “5-Substituted-1-H-tetrazoles as Carboxylic Acid Isosteres: Medicinal Chemistry and Synthetic Methods”, Bioorganic & Medicinal Chemistry 10(11), 2002, 3379-3393.
[cited by applicant]
Honorio, K. M, “Hologram QSAR Studies on Farnesoid X Receptor Activators”, Letters in Drug Design & Discovery, 3(4), DOI: 10.2174/157018006776743206, 2006, 261-267.
[cited by applicant]
Kim, H-S , “Synthesis and Antimicrobial Activity of New 3a-Hydroxy-23,24-bisnorcholane Polyamine Carbamates”, Bioorganic & Medicinal Chemistry Letters, 11(23), , DOI: 10.1016/S0960-894X(01)00632-1, 2001, 3065-3068.
[cited by applicant]
Klinoi, J , “Isolation of (23r) 3a, 7a,23-Trihydroxy-5b-Cholan-24-OIC . . . ”, Collection Czechoslovak Chem. Commun., 51, 1986, 1722-1730.
[cited by applicant]
Klinot, J. , “Isolation of (23R) 3α, 7α,23-trihydroxy-5β-cholan-24-oic (β-phocaecholic) acid from duck bile. 1H NMR spectra of its derivatives”, Collect. Czech. Chem. Commun., 51(8), , DOI: 10.1135/cccc19861722, Aug. 1,…
[cited by applicant]
Macchiarulo, A. , “Charting the chemical space of target sites: insights into the binding modes of amine and amidine groups”, Journal of chemical information and modeling, 49(4):, Mar. 18, 2009, 900-912.
[cited by applicant]
Macchiarulo, A. , “Probing the Binding Site of Bile Acids in TGR5”, ACS Medicinal Chemistry Letters, 4(12), , DOI: 10.1021/ml400247k, Oct. 15, 2013, 1158-1162.
[cited by applicant]
Mayorquin-Torres, M. C, “application of palladium-catalyzed carboxyl anhydride-boronic acid cross coupling in the synthesis of novel bile acids analogs and modified side chains”, Steroids, vol. 101, 2015, 21-27.
[cited by applicant]
Meijide, F. , “Spontaneous Formation in the Solid State of Carbamate Derivatives of Bile Acids”, Crystal Growth and Design, 11(1), DOI: 10.1021/cg101424a, 2011, 356-361.
[cited by applicant]
Montero, J-L. , “Selective synthesis of sulfonylureas and carboxysulfamides a novel route to oxazolidinones”, Tetrahedron Letters, 24(30), Dec. 31, 1983, 3091-3094.
[cited by applicant]
Nikolaienko, P. V, “Rapid way to fluorescent cholic-based chemosensor precursors”, International Electronic Conference on Synthetic Organic Chemistry, 2011, 1-4.
[cited by applicant]
Okada, J. , “Preparation of bile acid derivatives and their use as nasal absorption enhancers”, Database CA [Online] Chemical Abstracts Service, Columbus, Ohio, US; retrieved from STN Database accession No. 1999:142390.
[cited by applicant]
Okahata , “Base-catalyzed proton abstraction from.beta.-(p-nitrophenoxy) propiophenone in the presence of Single-chain, double-chain, and triple-chain ammonium bilayer membrane aggregates”, The Chemical Society of Japan…
[cited by applicant]
Okahata, Y. , “Base-catalyzed proton abstraction from .beta.-(p-nitrophenoxy)propiophenone in the presence of single-chain, double-chain, and triple-chain ammonium bilayer membrane aggregates”, Database CA [Online] Chem…
[cited by applicant]
Okahata, Y. , “Catalytic Hydrolysis of p-Nitrophenyl Esters in the Presence of Representative Ammonium Aggregates. Specific u Activation of a Cholesteryl Nucleophile Bound to a Dialkylammonium Bilayer Membrane”, Bulleti…
[cited by applicant]
Opsenica, I. M, “4-Amino-7-chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity”, J. Med. Chem., vol. 56, 2013, 5860-5871.
[cited by applicant]
Pellicciari, R. , “6α-Ethyl-Chenodeoxycholic Acid (6-ECDCA), a Potent and Selective FXR Agonist Endowed with Anticholestatic Activity”, Journal of Medicinal Chemistry, 45(17), 2002, 3569-3572.
[cited by applicant]
Pellicciari, R. , “Back Door Modulation of the Farnesoid X Receptor: Design, Synthesis and Biological Evaluation of a Series of Side Chain Modified Chenodeoxycholic Acid Derivatives”, J. Med. Chem., 49(14), DOI: 10.1021…
[cited by applicant]
Pellicciari, R., “Bile Acid Derivatives as Ligands of the Farnesoid X Receptor. Synthesis, Evaluation, and Structure-Activity Relationship of a Series of Body and Side Chain Modified Analogues of Chenodeoxycholic Acid”,…
[cited by applicant]
Pore, V. S, “Design and synthesis of fluconazole/bile acid conjugate using click reaction”, Tetrahedron, vol. 62, 2006, 11178-11186.
[cited by applicant]
Roda, A. , “Effect of Basic Cholane Derivatives on Intestinal Cholic Acid Metabolism: In Vitro and In Vivo Activity”, Journal of Pharmaceutical Sciences, vol. 81, No. 3, 1992, 237-240.
[cited by applicant]
Sajisha , “Remarkable isomer-selective gelation of aromatic solvents by a polymorph of a urea-linked bile acid-amino acid conjugate”, ZCAPLUS Accession No. 2014:1448647, 2014, 2 pgs.
[cited by applicant]
Sajisha, V. S, “Remarkable isomer-selective gelation of aromatic solvents by a polymorph of a urea-linked bile acid-amino acid conjugate”, RSC Advances, 4(81), DOI:10.1039/C4RA08957J., 2014, 43167-43171.
[cited by applicant]
Sato , “Novel Potent and Selective Bile Acid Derivatives as TGR5 Agonists: Biological Screening, Structure- Activity Relationships, and Molecular Modeling Studies”, J. Med. Chem., 51(6), 2008, 1831-1841.
[cited by applicant]
Sepe , “Farnesoid X receptor modulators (2011-2014): a patent review”, Expert Opinion on Therapeutic Patents, 25:8, 2015, 885-896.
[cited by applicant]
Silverman, R. B, “Prodrugs and Drug Delivery Systems”, The Organic Chemistry of Drug Design and Drug Action. Published by Academic Press, Chapter 8, 1992, 352-397.
[cited by applicant]
Solaja, B. A, “Novel 4-Aminoquinolines Active against Chloroquine-Resistant and Sensitive P. falciparum Strains that also Inhibit Botulinum Serotype A”, J. Med. Chem., vol. 51, 2008, 4388-4391.
[cited by applicant]
Videnovic, M. , “Second Generation Steroidal 4-Aminoquinolines Are Potent, Dual-Target Inhibitors . . . ”, J. Med. Chem., 57(10), doi.org/10.1021/jm500033r, Apr. 17, 2014, 4134-4153.
[cited by applicant]
Willemen, H. M, “Alkyl Derivatives of Cholic Acid as Organogelators: One-Component and Two-Component Gels”, Langmuir, 18(19), DOI: 10.1021/la0255141, 2002, 7102-7106.
[cited by applicant]
Wolff, M. E, “, Burger's Medicinal Chemistry and Drug Discovery, Fifth Edition, vol. 5(1): Principles and Practice” published by John Wiley and Sons, 1994, 975-977.
[cited by applicant]
Zaragoza Dorwald, F. , “Side Reactions in Organic Synthesis”, WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim, Preface. p. IX, 2005.
[cited by applicant]