blank Quick help
blank Maintenance news

Scheduled maintenance

Regular maintenance outages:
between 05.00 and 05.15 hrs CET (Monday to Sunday).

Other outages
Availability

2022.02.11

More...
blank News flashes

News Flashes

New version of the European Patent Register – SPC proceedings information in the Unitary Patent Register.

2024-07-24

More...
blank Related links

Release notes
European Patent Register Assistant
European Patent Register Resource Book
European Patent Register – pocket guide
FAQ - European Patent Register
Federated Register (Flyer)
Global Dossier (Flyer)
Register events
Deep link coverage
Federated Register content
The Patent Information Tour
Fair use charter

Extract from the Register of European Patents

EP About this file: EP2128158

EP2128158 - Heterocyclic cyclopropyl-substituted FXR binding compounds [Right-click to bookmark this link]
StatusThe application is deemed to be withdrawn
Status updated on  19.11.2010
Database last updated on 01.10.2024
Most recent event   Tooltip19.11.2010Application deemed to be withdrawnpublished on 22.12.2010  [2010/51]
Applicant(s)For all designated states
Phenex Pharmaceuticals AG
J542N, Werksgelände BASF
67056 Ludwigshafen / DE
[2009/49]
Inventor(s)01 / Abel, Ulrich
Spitzwegstrasse 4
69126 Heidelberg / DE
02 / Kremoser, Claus
Gugenmusweg 20
69121 Heidelberg / DE
 [2009/49]
Representative(s)Grünecker Patent- und Rechtsanwälte PartG mbB
Leopoldstrasse 4
80802 München / DE
[N/P]
Former [2009/49]Grünecker, Kinkeldey, Stockmair & Schwanhäusser Anwaltssozietät
Leopoldstrasse 4
80802 München / DE
Application number, filing date08009576.326.05.2008
[2009/49]
Filing languageEN
Procedural languageEN
PublicationType: A1 Application with search report 
No.:EP2128158
Date:02.12.2009
Language:EN
[2009/49]
Search report(s)(Supplementary) European search report - dispatched on:EP20.11.2008
ClassificationIPC:C07D413/12, A61K31/4439, A61P1/16, A61P3/10, A61P7/02, A61P9/10
[2009/49]
CPC:
C07D413/12 (EP); A61P1/16 (EP); A61P3/10 (EP);
A61P7/02 (EP); A61P9/10 (EP)
Designated contracting states(deleted) [2010/32]
Former [2009/49]AT,  BE,  BG,  CH,  CY,  CZ,  DE,  DK,  EE,  ES,  FI,  FR,  GB,  GR,  HR,  HU,  IE,  IS,  IT,  LI,  LT,  LU,  LV,  MC,  MT,  NL,  NO,  PL,  PT,  RO,  SE,  SI,  SK,  TR 
TitleGerman:Heterocyclische Cyclopropyl-substituierte FXR-bindende Verbindungen[2009/49]
English:Heterocyclic cyclopropyl-substituted FXR binding compounds[2009/49]
French:Composés de liaison FXR substitués de cyclopropyle hétérocyclique[2009/49]
Examination procedure03.06.2010Application deemed to be withdrawn, date of legal effect  [2010/51]
09.07.2010Despatch of communication that the application is deemed to be withdrawn, reason: examination fee not paid in time  [2010/51]
Fees paidPenalty fee
Additional fee for renewal fee
31.05.201003   M06   Not yet paid
Opt-out from the exclusive  Tooltip
competence of the Unified
Patent Court		 See the Register of the Unified Patent Court for opt-out data
Responsibility for the accuracy, completeness or quality of the data displayed under the link provided lies entirely with the Unified Patent Court.
Documents cited:Search[DX]WO2007140174  (LILLY CO ELI [US], et al) [DX] 1-23 * claims 1,16-23 * * compounds 5,46,65,67,69,72,93 *;
 [DA]WO2008025540  (PHENEX PHARMACEUTICALS AG [DE], et al) [DA] 1-23 * claims 1,14-38 * * compound 28 *
by applicantWO2008051942
 WO2008025539
 WO2008025540
 WO2007140183
 WO2007092751
 WO2007140174
 WO2004048349
 WO03015771
 WO0037077
 WO2004087076
 WO03080803
    - D. MANGELSDORF ET AL., "The nuclear receptor superfamily: the second decade", CELL, (1995), vol. 83, no. 6, doi:doi:10.1016/0092-8674(95)90199-X, pages 835 - 839, XP000929729

DOI:   http://dx.doi.org/10.1016/0092-8674(95)90199-X
    - R EVANS, "The nuclear receptor superfamily: a rosetta stone for physiology", MOL. ENDOCRINOL, (2005), vol. 19, no. 6, pages 1429 - 1438
    - M. SCHENA, "Mammalian glucocorticoid receptor derivatives enhance transcription in yeast", SCIENCE, (1988), vol. 241, no. 4868, pages 965 - 967
    - A. BRZOZOWSKI ET AL., "Molecular basis of agonism and antagonism in the oestrogen receptor", NATURE, (1997), vol. 389, no. 6652, doi:doi:10.1038/39645, pages 753 - 758, XP002248702

DOI:   http://dx.doi.org/10.1038/39645
    - D. HEERY ET AL., "A signature motif in transcriptional co-activators mediates binding to nuclear receptors", NATURE, (1997), vol. 387, no. 6634, doi:doi:10.1038/42750, pages 733 - 6, XP002162222

DOI:   http://dx.doi.org/10.1038/42750
    - T. HEINZEL ET AL., "A complex containing N-CoR, mSin3 and histone deacetylase mediates transcriptional repression", NATURE, (1997), vol. 387, no. 6628, pages 16 - 17
    - K. NETTLES; G. GREENE, "Ligand control of coregulator recruitment to nuclear receptors", ANNU. REV. PHYSIOL, (2005), vol. 67, pages 309 - 33
    - A. ARANDA, "A. Pascual "Nuclear hormone receptors and gene expression", PHYSIOL. REV, (2001), vol. 81, no. 3, pages 1269 - 1304
    - B. FORMAN ET AL., "Identification of a nuclear receptor that is activated by farnesol metabolites", CELL, (1995), vol. 81, no. 5, doi:doi:10.1016/0092-8674(95)90530-8, pages 687 - 693, XP000919168

DOI:   http://dx.doi.org/10.1016/0092-8674(95)90530-8
    - D. PARKS ET AL., "Bile acids: natural ligands for an orphan nuclear receptor", SCIENCE, (1999), vol. 284, no. 5418, doi:doi:10.1126/science.284.5418.1365, pages 1365 - 1368, XP002927559

DOI:   http://dx.doi.org/10.1126/science.284.5418.1365
    - M. MAKISHIMA ET AL., "Identification of a nuclear receptor for bile acids", SCIENCE, (1999), vol. 284, no. 5418, doi:doi:10.1126/science.284.5418.1362, pages 1362 - 1365, XP002927558

DOI:   http://dx.doi.org/10.1126/science.284.5418.1362
    - J. HOLT ET AL., "Definition of a novel growth factor-dependent signal cascade for the suppression of bile acid biosynthesis", GENES DEV., (2003), vol. 17, no. 13, pages 1581 - 91
    - T. INAGAKI ET AL., "Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis", CELL METAB, (2005), vol. 2, no. 4, doi:doi:10.1016/j.cmet.2005.09.001, pages 217 - 225, XP055000838

DOI:   http://dx.doi.org/10.1016/j.cmet.2005.09.001
    - P. ANANDET, "Downregulation of TACO gene transcription restricts mycobacterial entry/survival within human macrophages", FEMS MICROBIOL. LETT., (2005), vol. 250, no. 1, pages 137 - 144
    - R. C. BUIJSMAN ET AL., "Non-Steroidal Steroid Receptor Modulators", CURR. MED. CHEM, (2005), vol. 12, pages 1017 - 1075
    - R. PRENTIS ET AL., "Pharmaceutical innovation by seven UK-owned pharmaceutical companies (1964-1985", BR. J. CLIN. PHARMACOL, (1988), vol. 25, pages 387 - 396, XP000943342
    - J. LIN; A. LU, "Role of pharmacokinetics and Metabolism in Drug Discovery and Development", PHARMACOL. REV., (1997), vol. 49, no. 4, pages 404 - 449, XP000943339
    - C. A. LIPINSKI, "Drug-like properties and the causes of poor solubility and poor permeability", J. PHARMACOL. TOXICOL. METHODS, (2000), vol. 44, doi:doi:10.1016/S1056-8719(00)00107-6, pages 235 - 249, XP001097602

DOI:   http://dx.doi.org/10.1016/S1056-8719(00)00107-6
    - L. DI; E. KERNS, "Profiling drug-like properties in discovery research", CURR. OPIN. CHEM. BIOL., (2003), vol. 7, pages 402 - 408
    - A.M. MARINO ET AL., "Validation of the 96-well Caco-2 cell culture model for high-throughput permeability and assessment of discovery compounds", INT. J. PHARMACEUTICS, (2005), vol. 297, pages 235 - 241
    - F. WOHNSLAND; B. FALLER, "High-throughput Permeability pH Profile and High-throughput Alkane/Water Log P With Artificial Membranes", J. MED. CHEM., (2001), vol. 44, doi:doi:10.1021/jm001020e, pages 923 - 930, XP002413495

DOI:   http://dx.doi.org/10.1021/jm001020e
    - T. IWATSUBO ET AL., "Prediction of in vivo drug metabolism in the human liver from in vitro metabolism data", PHARM. THER, (1997), vol. 73, pages 147 - 171
    - T. CLAUDEL ET AL., "The Farnesoid X receptor: a molecular link between bile acid and lipid and glucose metabolism", ARTERIOSCLER. THROMB. VASC. BIOL., (2005), vol. 25, no. 10, pages 2020 - 2030
    - S. WESTIN ET AL., "FXR, a therapeutic target for bile acid and lipid disorders", MINI REV. MED. CHEM., (2005), vol. 5, no. 8, pages 719 - 727
    - B. GOODWIN ET AL., "A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis", MOL. CELL, (2000), vol. 6, no. 3, doi:doi:10.1016/S1097-2765(00)00051-4, pages 517 - 526, XP002209573

DOI:   http://dx.doi.org/10.1016/S1097-2765(00)00051-4
    - T. LU ET AL., "Molecular basis for feedback regulation of bile acid synthesis by nuclear receptors", MOL. CELL, (2000), vol. 6, no. 3, doi:doi:10.1016/S1097-2765(00)00050-2, pages 507 - 515, XP002209572

DOI:   http://dx.doi.org/10.1016/S1097-2765(00)00050-2
    - C. SINAL ET AL., "Targeted disruption of the nuclear receptor FXR/BAR impairs bile acid and lipid homeostasis", CELL, (2000), vol. 102, no. 6, doi:doi:10.1016/S0092-8674(00)00062-3, pages 731 - 744, XP055059110

DOI:   http://dx.doi.org/10.1016/S0092-8674(00)00062-3
    - M. ANANTHANARAYANANET, "Human bile salt export pump promoter is transactivated by the farnesoid X receptor/bile acid receptor", J. BIOL. CHEM., (2001), vol. 276, no. 31, doi:doi:10.1074/jbc.M011610200, pages 28857 - 28865, XP002430664

DOI:   http://dx.doi.org/10.1074/jbc.M011610200
    - J. PLASS ET AL., "Farnesoid X receptor and bile salts are involved in transcriptional regulation of the gene encoding the human bile salt export pump", HEPATOLOGY, (2002), vol. 35, no. 3, doi:doi:10.1053/jhep.2002.31724, pages 589 - 96, XP008021676

DOI:   http://dx.doi.org/10.1053/jhep.2002.31724
    - N. URIZAR ET AL., "The farnesoid X-activated receptor mediates bile acid activation of phospholipid transfer protein gene expression", J. BIOL. CHEM., (2000), vol. 275, no. 50, doi:doi:10.1074/jbc.M007998200, pages 39313 - 39317, XP002948685

DOI:   http://dx.doi.org/10.1074/jbc.M007998200
    - H. KAST ET AL., "Regulation of multidrug resistance-associated protein 2 (ABCC2) by the nuclear receptors pregnane X receptor, farnesoid X-activated receptor, and constitutive androstane receptor", J. BIOL. CHEM., (2002), vol. 277, no. 4, pages 2908 - 2915
    - L. HUANG ET AL., "Farnesoid X receptor activates transcription of the phospholipid pump MDR3", J. BIOL. CHEM., (2003), vol. 278, no. 51, pages 51085 - 51090
    - M. MIYATA, "Role of farnesoid X receptor in the enhancement of canalicular bile acid output and excretion of unconjugated bile acids: a mechanism for protection against cholic acid-induced liver toxicity", J. PHARMACOL. EXP. THER, (2005), vol. 312, no. 2, pages 759 - 766
    - G. RIZZO ET AL., "Role of FXR in regulating bile acid homeostasis and relevance for human diseases", CURR. DRUG TARGETS IMMUNE ENDOCR. METABOL. DISORD, (2005), vol. 5, no. 3, pages 289 - 303
    - P. MALONEY ET AL., "Identification of a chemical tool for the orphan nuclear receptor FXR", J. MED. CHEM., (2000), vol. 43, no. 16, doi:doi:10.1021/jm0002127, pages 2971 - 2974, XP002421612

DOI:   http://dx.doi.org/10.1021/jm0002127
    - T. WILLSON ET AL., "Chemical genomics: functional analysis of orphan nuclear receptors in the regulation of bile acid metabolism", MED. RES. REV., (2001), vol. 21, no. 6, doi:doi:10.1002/med.1023, pages 513 - 22, XP009013154

DOI:   http://dx.doi.org/10.1002/med.1023
    - R. PELLICCIARI ET AL., "6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity", J. MED. CHEM., (2002), vol. 45, no. 17, doi:doi:10.1021/jm025529g, pages 3569 - 3572, XP002370635

DOI:   http://dx.doi.org/10.1021/jm025529g
    - Y. LIU ET AL., "Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis", J. CLIN. INVEST, (2003), vol. 112, no. 11, doi:doi:10.1172/JCI200318945, pages 1678 - 1687, XP002992678

DOI:   http://dx.doi.org/10.1172/JCI200318945
    - S. FIORUCCI ET AL., "The nuclear receptor SHP mediates inhibition of hepatic stellate cells by FXR and protects against liver fibrosis", GASTROENTEROLOGY, (2004), vol. 127, no. 5, doi:doi:10.1053/j.gastro.2004.08.001, pages 1497 - 1512, XP005313108

DOI:   http://dx.doi.org/10.1053/j.gastro.2004.08.001
    - S. FIORUCCI ET AL., "A farnesoid x receptor-small heterodimer partner regulatory cascade modulates tissue metalloproteinase inhibitor-1 and matrix metalloprotease expression in hepatic stellate cells and promotes resolution of liver fibrosis", J. PHARMACOL. EXP. THER, (2005), vol. 314, no. 2, doi:doi:10.1124/jpet.105.084905, pages 584 - 595, XP008060974

DOI:   http://dx.doi.org/10.1124/jpet.105.084905
    - S. FIORUCCI ET AL., "Cross-talk between farnesoid-X-receptor (FXR) and peroxisome proliferator-activated receptor gamma contributes to the antifibrotic activity of FXR ligands in rodent models of liver cirrhosis", J. PHARMACOL. EXP. THER., (2005), vol. 315, no. 1, doi:doi:10.1124/jpet.105.085597, pages 58 - 68, XP008060972

DOI:   http://dx.doi.org/10.1124/jpet.105.085597
    - A. GALLI ET AL., "Antidiabetic thiazolidinediones inhibit collagen synthesis and hepatic stellate cell activation in vivo and in vitro", GASTROENTEROLOGY, (2002), vol. 122, no. 7, doi:doi:10.1053/gast.2002.33666, pages 1924 - 1940, XP055075611

DOI:   http://dx.doi.org/10.1053/gast.2002.33666
    - I. PINEDA TORRA ET AL., "Bile acids induce the expression of the human peroxisome proliferator-activated receptor alpha gene via activation of the farnesoid X receptor", MOL. ENDOCRINOL., (2003), vol. 17, no. 2, pages 259 - 272
    - S. FIORUCCI ET AL., "Protective effects of 6-ethyl chenodeoxycholic acid, a farnesoid X receptor ligand, in estrogen-induced cholestasis", J. PHARMACOL. EXP. THER., (2005), vol. 313, no. 2, doi:doi:10.1124/jpet.104.079665, pages 604 - 612, XP008060973

DOI:   http://dx.doi.org/10.1124/jpet.104.079665
    - F. CHEN ET AL., "Progressive familial intrahepatic cholestasis, type 1, is associated with decreased farnesoid X receptor activity", GASTROENTEROLOGY, (2004), vol. 126, no. 3, doi:doi:10.1053/j.gastro.2003.12.013, pages 756 - 64, XP005314485

DOI:   http://dx.doi.org/10.1053/j.gastro.2003.12.013
    - L. ALVAREZ ET AL., "Reduced hepatic expression of farnesoid X receptor in hereditary cholestasis associated to mutation in ATP8B1", HUM. MOL. GENET, (2004), vol. 13, no. 20, pages 2451 - 60
    - G. RIZZO ET AL., CURR. DRUG TARGETS IMMUNE ENDOCR. METABOL. DISORD, (2005), vol. 5, no. 3, pages 289 - 303
    - G. ZOLLNER, "Role of nuclear receptors in the adaptive response to bile acids and cholestasis: pathogenetic and therapeutic considerations", MOL. PHARM, (2006), vol. 3, no. 3, pages 231 - 51
    - S. CAI ET AL., "FXR: a target for cholestatic syndromes", EXPERT OPIN. THER. TARGETS, (2006), vol. 10, no. 3, pages 409 - 421
    - H. WITTENBURG, "FXR and ABCG5/ABCG8 as determinants of cholesterol gallstone formation from quantitative trait locus mapping in mice", GASTROENTEROLOGY, (2003), vol. 125, no. 3, doi:doi:10.1016/S0016-5085(03)01053-9, pages 868 - 881, XP005313511

DOI:   http://dx.doi.org/10.1016/S0016-5085(03)01053-9
    - A. MOSCHETTA ET AL., "Prevention of cholesterol gallstone disease by FXR agonists in a mouse model", NATURE MEDICINE, (2004), vol. 10, no. 12, pages 1352 - 1358
    - S. DOGGRELL, "New targets in and potential treatments for cholesterol gallstone disease", CURR. OPIN. INVESTIG. DRUGS, (2006), vol. 7, no. 4, pages 344 - 348, XP008175325
    - P. MALONEY ET AL., J. MED. CHEM., (2000), vol. 43, no. 16, pages 2971 - 2974
    - T. WILLSON ET AL., MED. RES. REV, (2001), vol. 21, no. 6, pages 513 - 22
    - H. KAST ET AL., "Farnesoid X-activated receptor induces apolipoprotein C-II transcription: a molecular mechanism linking plasma triglyceride levels to bile acids", MOL. ENDOCRINOL, (2001), vol. 15, no. 10, doi:doi:10.1210/me.15.10.1720, pages 1720 - 1728, XP001157555

DOI:   http://dx.doi.org/10.1210/me.15.10.1720
    - N.URIZAR ET AL., "A natural product that lowers cholesterol as an antagonist ligand for FXR", SCIENCE, (2002), vol. 296, no. 5573, doi:doi:10.1126/science.1072891, pages 1703 - 1706, XP002358293

DOI:   http://dx.doi.org/10.1126/science.1072891
    - G. LAMBERT ET AL., "The farnesoid X-receptor is an essential regulator of cholesterol homeostasis", J. BIOL. CHEM., (2003), vol. 278, pages 2563 - 2570
    - M. WATANABE ET AL., "Bile acids lower triglyceride levels via a pathway involving FXR, SHP, and SREBP-1c", J. CLIN. INVEST, (2004), vol. 113, no. 10, pages 1408 - 1418
    - A. FIGGE ET AL., "Hepatic overexpression of murine Abcbll increases hepatobiliary lipid secretion and reduces hepatic steatosis", J. BIOL. CHEM., (2004), vol. 279, no. 4, pages 2790 - 2799
    - S. BILZ ET AL., "Activation of the farnesoid X receptor improves lipid metabolism in combined hyperlipidemic hamsters", AM. J. PHYSIOL. ENDOCRINOL. METAB, (2006), vol. 290, no. 4, pages 716 - 22
    - K. STAYROOK ET AL., "Regulation of carbohydrate metabolism by the farnesoid X receptor", ENDOCRINOLOGY, (2005), vol. 146, no. 3, doi:doi:10.1210/en.2004-0965, pages 984 - 91, XP008109012

DOI:   http://dx.doi.org/10.1210/en.2004-0965
    - Y. ZHANG ET AL., "Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice", PROC. NATL. ACAD. SCI. USA, (2006), vol. 103, no. 4, pages 1006 - 1011
    - B. CARIOU ET AL., "The farnesoid X receptor modulates adiposity and peripheral insulin sensitivity in mice", J. BIOL. CHEM., (2006), vol. 281, pages 11039 - 11049
    - K. MA ET AL., "Farnesoid X receptor is essential for normal glucose homeostasis", J. CLIN. INVEST., (2006), vol. 116, no. 4, pages 1102 - 1109
    - D. DURAN-SANDOVAL ET AL., "Potential regulatory role of the farnesoid X receptor in the metabolic syndrome", BIOCHIMIE, (2005), vol. 87, no. 1, doi:doi:10.1016/j.biochi.2004.11.018, pages 93 - 98, XP004768698

DOI:   http://dx.doi.org/10.1016/j.biochi.2004.11.018
    - J. HOLT ET AL., GENES DEV., (2003), vol. 17, no. 13, pages 1581 - 1591
    - E. TOMLINSON ET AL., "Transgenic mice expressing human fibroblast growth factor-19 display increased metabolic rate and decreased adiposity", ENDOCRINOLOGY, (2002), vol. 143, no. 5, doi:doi:10.1210/en.143.5.1741, pages 1741 - 1747, XP002972819

DOI:   http://dx.doi.org/10.1210/en.143.5.1741
    - E. HANNIMAN ET AL., "Loss of functional farnesoid X receptor increases atherosclerotic lesions in apolipoprotein E-deficient mice", J. LIPID RES, (2005), vol. 46, no. 12, pages 2595 - 2604
    - F. HE ET AL., "Down regulation of endothelin-1 by farnesoid X receptor in vascular endothelial cells", CIRC. RES, (2006), vol. 98, no. 2, pages 192 - 9
    - E. NIESOR ET AL., "The nuclear receptors FXR and LXRalpha: potential targets for the development of drugs affecting lipid metabolism and neoplastic diseases", CURR. PHARM. DES, (2001), vol. 7, no. 4, doi:doi:10.2174/1381612013398185, pages 231 - 59, XP008004861

DOI:   http://dx.doi.org/10.2174/1381612013398185
    - D. BISHOP-BAILEY ET AL., "Expression and activation of the farnesoid X receptor in the vasculature", PROC. NATL. ACAD. SCI. USA., (2004), vol. 101, no. 10, doi:doi:10.1073/pnas.0400046101, pages 3668 - 3673, XP002358294

DOI:   http://dx.doi.org/10.1073/pnas.0400046101
    - J. SILVA, "Lipids isolated from bone induce the migration of human breast cancer cells", J. LIPID RES, (2006), vol. 47, no. 4, pages 724 - 733
    - G. DE GOTTARDI ET AL., "The bile acid nuclear receptor FXR and the bile acid binding protein IBABP are differently expressed in colon cancer", DIG. DIS. SCI., (2004), vol. 49, no. 6, doi:doi:10.1023/B:DDAS.0000034558.78747.98, pages 982 - 989, XP019237067

DOI:   http://dx.doi.org/10.1023/B:DDAS.0000034558.78747.98
    - D. DURAN-SANDOVAL ET AL., J. BIOL. CHEM., (2005), vol. 280, no. 33, pages 29971 - 29979
    - Y. ZHANG ET AL., PROC. NATL. ACAD. SCI. USA., (2006), vol. 103, no. 4, pages 1006 - 1011
    - T. INAGAKI ET AL., "Regulation of antibacterial defense in the small intestine by the nuclear bile acid receptor", PROC. NATL. ACAD. SCI. U S A., (2006), vol. 103, no. 10, pages 3920 - 3905
    - "March's Advanced Organic Chemistry: Reactions, Mechanisms, and Structure", JOHN WILEY & SONS
    - MALONEY ET AL., J. MED. CHEM., (2000), vol. 43, no. 16, pages 2971 - 2974
    - DOLEY ET AL., J. CHEM. SOC., (1963), pages 5838 - 5845
    - HIMBERT ET AL., LIEBIGS ANN. CHEM, (1990), vol. 4, pages 403 - 407
    - BEYER ET AL., JUSTUS LIEBIGS ANN CHEM, (1970), pages 45 - 54
    - J. PIET ET AL., BULL. SOC. CHIM. BELG, (1996), vol. 105, no. 1, pages 33 - 44
    - A. CWIKLICKI ET AL., ARCH. PHARM, (2004), vol. 337, no. 3, pages 156 - 163
    - March's Advanced Organic Chemistry: Reactions, Mechanisms, and Structure, JOHN WILEY & SONS
    - "Database", Database accession no. 005123
    - GROBER ET AL., JBC, (1999), vol. 174, pages 29749 - 29754
    - DYER ET AL., ANAL BIOCHEM, (2000), no. 282, pages 158 - 161
The EPO accepts no responsibility for the accuracy of data originating from other authorities; in particular, it does not guarantee that it is complete, up to date or fit for specific purposes.