Sphingosine 1-phosphate receptor agonists: a patent review (2010 – 2012)

Bibliography

• Lopez Almagro R, Tarrason G, Godessart N. Protein-coupled receptors structure signaling and physiology. CUP; Cambridge: 2011
   Google Scholar
• Blaho VA, Hla T. Regulation of mammalian physiology, development, and disease by the sphingosine 1-phosphate and lysophosphatidic acid receptors. Chem Rev 2011;111:6299-320
   PubMed Web of Science ®Google Scholar
• Pyne NJ, Pyne S. Sphingosine 1-phosphate and cancer. Nat Rev Cancer 2010;10:489-503
   PubMed Web of Science ®Google Scholar
• Marsolais D, Rosen H. Chemical modulators of sphingosine-1-phosphate receptors as barrier-oriented therapeutic molecules. Nat Rev Drug Discov 2009;8:297-307
   PubMed Web of Science ®Google Scholar
• Sanchez T, Hla T. Structural and functional characteristics of S1P receptors. J Cell Biochem 2004;92:913-22
   PubMed Web of Science ®Google Scholar
• Chun J, Goetzl EJ, Hla T. International union of pharmacology. XXXIV. Lysophospholipid receptor nomenclature. Pharmacol Rev 2002;54:265-9
   PubMed Web of Science ®Google Scholar
• Holdsworth G, Osborne DA, Pham TCT, et al. A single amino acid determines preference between phospholipids and reveals length restriction for activation of the S1P4 receptor. BMC Biochem 2004;5:12
   PubMedGoogle Scholar
• Candelore MR, Wright MJ, Tota L M, et al. Phytosphingosine 1-phosphate: a high affinity ligand for the S1P4/Edg-6 receptor. Biochem Biophys Res Commun 2002;297:600-6
   PubMed Web of Science ®Google Scholar
• Matloubian M, Lo CG, Cinamon G, et al. Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1. Nature 2004;427:355-60
   PubMed Web of Science ®Google Scholar
• Jo E, Sanna MG, Gonzalez-Cabrera PJ, et al. S1P1-selective in vivo-active agonists from high-throughput screening: off-the-shelf chemical probes of receptor interactions, signaling, and fate. Chem Biol 2005;12:703-15
   PubMed Web of Science ®Google Scholar
• Allende ML, Yamashita T, Proia RL. G-protein-coupled receptor S1P1 acts within endothelial cells to regulate vascular maturation. Blood 2003;102:3665-7
   PubMed Web of Science ®Google Scholar
• Singleton PA, Dudek SM, Chiang ET, et al. Regulation of sphingosine 1-phosphate-induced endothelial cytoskeletal rearrangement and barrier enhancement by S1P1 receptor, PI3 kinase, Tiam1/Rac1, and alpha-actinin. FASEB J 2005;19:1646-56
   PubMed Web of Science ®Google Scholar
• Wei SH, Rosen H, Matheu MP, et al. Sphingosine 1-phosphate type 1 receptor agonism inhibits transendothelial migration of medullary T cells to lymphatic sinuses. Nat Immunol 2005;6:1228-35
   PubMed Web of Science ®Google Scholar
• Ozaki H, Hla T, Lee MJ. Sphingosine-1-phosphate signaling in endothelial activation. J Atheroscler Thromb 2003;10:125-31
   PubMedGoogle Scholar
• LaMontagne K, Littlewood-Evans A, Schnell C, et al. Antagonism of Sphingosine-1-Phosphate Receptors by FTY720 Inhibits Angiogenesis and Tumor Vascularization. Cancer Res 2006;66:221-31
   PubMed Web of Science ®Google Scholar
• Uhlig S, Gulbins E. Sphingolipids in the Lung. Am J Respir Crit Care Med 2008;178:1100-14
   PubMed Web of Science ®Google Scholar
• Brinkmann V, Billich A, Baumruker T, et al. Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis. Nat Rev Drug Discov 2010;9:883-97
   PubMed Web of Science ®Google Scholar
• FDA Drug Safety Communication: revised recommendations for cardiovascular monitoring and use of multiple sclerosis drug Gilenya (fingolimod). Available from: http://www.fda.gov/Drugs/DrugSafety/ucm303192.htm [Last accessed 10 December 2012]
   Google Scholar
• Koyrakh L, Roman M I, Brinkmann V, et al. The heart rate decrease caused by acute FTY720 administration is mediated by the G protein-gated potassium channel IKACh. Am J Transplant 2005;5:529-36
   PubMed Web of Science ®Google Scholar
• Dyckman AJ. Recent advances in the discovery and development of sphingosin-1-phosphate-1 receptor agonists. Annu Rep Med Chem 2012;47:195-207
   Web of Science ®Google Scholar
• Gergely P, Wallstroum E, Nuesslein-Hildesheim B, et al. Phase I study with the selective S1P1/S1P5 receptor modulator BAF312 indicates that S1P1 rather than S1P3 mediates transient heart rate reduction in humans. Mult Scler 2009;15:S125
   Google Scholar
• Pelletier D, Hafler DA. Fingolimod for multiple sclerosis. N Engl J Med 2012;366:339-47
   PubMed Web of Science ®Google Scholar
• Sanna MG, Liao J, Jo E, et al. Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J Biol Chem 2004;279:13839-48
   PubMed Web of Science ®Google Scholar
• Forrest M, Sun S, Hajdu R, et al. Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes. J Pharmacol Exp Ther 2004;309:758-68
   PubMed Web of Science ®Google Scholar
• Nofer J, van der Giet M, Tolle M, et al. HDL induces NO-dependent vasorelaxation via the lysophospholipid receptor S1P3. J Clin Invest 2004;113:569-81
   PubMed Web of Science ®Google Scholar
• Takuwa N, Ohkura S, Takashima S, et al. S1P3-mediated cardiac fibrosis in sphingosine kinase 1 transgenic mice involves reactive oxygen species. Cardiovasc Res 2010;85:484-93
   PubMed Web of Science ®Google Scholar
• Theilmeier G, Schmidt C, Herrmann J, et al. High-density lipoproteins and their constituent, sphingosine-1-phosphate, directly protect the heart against ischemia/reperfusion injury in vivo via the S1P3 lysophospholipid receptor. Circulation 2006;114:1403-9
   PubMed Web of Science ®Google Scholar
• Means C K, Xiao C, Li Z, et al. Sphingosine 1-phosphate S1P2 and S1P3 receptor-mediated Akt activation protects against in vivo myocardial ischemia-reperfusion injury. Am J Physiol Heart Circ Phys 2007;292:H2944-51
   Web of Science ®Google Scholar
• Fischer I, Alliod C, Martinier N, et al. Sphingosine kinase 1 and sphingosine 1-phosphate receptor 3 are functionally upregulated on astrocytes under pro-inflammatory conditions. PLoS One 2011;6:e23905
   Web of Science ®Google Scholar
• Hsu A, Zhang W, Lee J, et al. Sphingosine-1-phosphate receptor-3 signaling up-regulates epidermal growth factor receptor and enhances epidermal growth factor receptor-mediated carcinogenic activities in cultured lung adenocarcinoma cells. Int J Oncol 2012;40:1619-26
   PubMed Web of Science ®Google Scholar
• Marsolais D, Hahm B, Edelmann KH, et al. Local not systemic modulation of dendritic cell S1P receptors in lung blunts virus-specific immune responses to influenza. Mol Pharmacol 2008;74:896-903
   PubMed Web of Science ®Google Scholar
• Golfier S, Kondo S, Schulze T, et al. Shaping of terminal megakaryocyte differentiation and proplatelet development by sphingosine-1-phosphate receptor S1P4. FASEB J 2010;24:4701-10
   PubMed Web of Science ®Google Scholar
• Ley S, Weigert A, Weichand B, et al. The role of TRKA signaling in IL-10 production by apoptotic tumor cell-activated macrophages. Oncogene 2012;1-10
   Web of Science ®Google Scholar
• Sekar D, Hahn C, Brune B, et al. Apoptotic tumor cells induce IL-27 release from human DCs to activate Treg cells that express CD69 and attenuate cytotoxicity. Eur J Immunol 2012;42:1585-98
   PubMed Web of Science ®Google Scholar
• Ohotski J, Long JS, Orange C, et al. Expression of sphingosine 1-phosphate receptor 4 and sphingosine kinase 1 is associated with outcome in oestrogen receptor-negative breast cancer. Br J cancer 2012;106:1453-9
   PubMed Web of Science ®Google Scholar
• Malek RL, Toman RE, Edsall LC, et al. Nrg-1 belongs to the endothelial differentiation gene family of G protein-coupled sphingosine-1-phosphate receptors. J Biol Chem 2001;276:5692-9
   PubMed Web of Science ®Google Scholar
• Jung CG, Kim HJ, Miron VE, et al. Functional consequences of S1P receptor modulation in rat oligodendroglial lineage cells. Glia 2007;55:1656-67
   PubMed Web of Science ®Google Scholar
• Walzer T, Chiossone L, Chaix J, et al. Natural killer cell trafficking in vivo requires a dedicated sphingosine 1-phosphate receptor. Nat Immunol 2007;8:1337-44
   PubMed Web of Science ®Google Scholar
• van Doorn R, Pinheiro MA, Kooij G, et al. Sphingosine 1-phosphate receptor 5 mediates the immune quiescence of the human brain endothelial barrier. J Neuroinflam 2012;9:133
   PubMed Web of Science ®Google Scholar
• Allergan, Inc. Coumarin compounds as receptor modulators with therapeutic utility. WO011050054; 2011
   Google Scholar
• Allergan, Inc. Biphenyl oxadiazole derivatives as sphingosine-1-phosphate (S1P) receptor modulators. US0110257232; 2011
   Google Scholar
• Allergan, Inc. 3-(4-((1H-imidazol-1-yl)methyl)phenyl)-5-aryl-1,2,4-oxadiazole derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO011136927; 2011
   Google Scholar
• Allergan, Inc. Novel phosphonic acids as S1P receptor Modulators. WO012071212; 2012
   Google Scholar
• Allergan, Inc. Novel azetidine derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012074703; 2012
   Google Scholar
• Allergan, Inc. Novel phenyl oxadiazole derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012074732; 2012
   Google Scholar
• Allergan, Inc. Indole derivatives as modulators of S1P receptors. WO012071184; 2012
   Google Scholar
• Allergan, Inc. Novel oxadiazole derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012074718; 2012
   Google Scholar
• Allergan, Inc. Novel pyridine derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012074719; 2012
   Google Scholar
• Allergan, Inc. Novel benzyl azetidine derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012074722; 2012
   Google Scholar
• Allergan, Inc. Oxadiazole derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012074730; 2012
   Google Scholar
• Allergan, Inc. Modulators of S1P receptos. WO012071186; 2012
   Google Scholar
• Allergan, Inc. Alkyne and alkene derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012074921; 2012
   Google Scholar
• Allergan, Inc. Novel azetidine derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012074926; 2012
   Google Scholar
• Allergan, Inc. Novel oxime azetidine derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012074780; 2012
   Google Scholar
• Allergan, Inc. Novel oxime derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012074782; 2012
   Google Scholar
• Allergan, Inc. Novel compounds as receptor modulators with therapeutic utility. WO011066179; 2011
   Google Scholar
• Allergan, Inc. Novel compounds as receptor modulators with therapeutic utility. WO012071278; 2012
   Google Scholar
• Allergan, Inc. Substituted bicyclic methyl amine derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012145236; 2012
   Google Scholar
• Allergan, Inc. Substituted bicyclic methyl azetidines as sphingosine-1-phosphate (S1P) receptor modulators. WO012142255; 2012
   Google Scholar
• Allergan, Inc. Novel compounds as receptor modulators with therapeutic utility. WO011066184; 2011
   Google Scholar
• Allergan, Inc. Aromatic compounds having sphingosine-1-phosphate (S1P) receptor activity. WO011143332; 2011
   Google Scholar
• Allergan, Inc. Bicyclic methyl amine derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012142377; 2012
   Google Scholar
• Allergan, Inc. Phenyl bicyclic methyl amine derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012142288; 2012
   Google Scholar
• Allergan, Inc. Phenyl bicyclic methyl azetidine derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012142268; 2012
   Google Scholar
• Allergan, Inc. Novel alkene derivatives as sphingosine-1-phosphate (S1P) receptor modulators. WO012074898; 2012
   Google Scholar
• Glaxo Group Ltd. 1,2,4-oxadiazol derivatives, their pharmaceutical compositions and their use as sphingosine 1-phosphate 1 receptor agonists. WO010145203; 2010
   Google Scholar
• Glaxo Group Ltd. Thiazole or thiadizaloe derivatives for use as sphingosine 1-phosphate 1 (S1P1) receptor agonists. WO010145202; 2010
   Google Scholar
• Glaxo Group Ltd. Thiadiazole derivatives and their use for the treatment of disorders mediated by SlPl receptors. WO010146104; 2010
   Google Scholar
• Glaxo Group Ltd. S1P1 agonists comprising a bicyclic N-containing ring. WO010146105; 2010
   Google Scholar
• Glaxo Group Ltd. 5-membered heteroaryl derivatives used as sphingosine 1-phosphate receptor agonists. WO010148650; 2010
   Google Scholar
• Glaxo Group Ltd. 5-membered heteroaryl derivatives used as sphingosine 1-phosphate receptor agonists. WO010148649; 2010
   Google Scholar
• Glaxo Group Ltd. Oxadiazole substituted indazole derivatives for use as sphingosine 1-phosphate 1 (s1p1) receptor agonists. WO011072488; 2011
   Google Scholar
• Glaxo Group Ltd. Pyrimidine derivatives for use as sphingosine 1-phosphate 1 (S1P1) receptor agonists. WO011113309; 2011
   Google Scholar
• Glaxo Group Ltd. Compounds as agonists of S1P1 receptors. WO011134280; 2011
   Google Scholar
• Almirall SA. New 2-amidothiadiazole derivatives. WO010043377; 2010
   Google Scholar
• Almirall SA. New thiadiazole derivatives. WO011035900; 2011
   Google Scholar
• Almirall SA. New 2-aminothiadiazole derivatives. WO011069647; 2011
   Google Scholar
• Almirall SA. 1,2,4-oxadiazole derivatives and their therapeutic use. WO010072352; 2010
   Google Scholar
• Almirall SA. New oxadiazole derivatives. WO011113578; 2011
   Google Scholar
• Almirall SA. S1P1 receptor agonists for use in the treatment of multiple sclerosis. EP2455080; 2012
   Google Scholar
• Almirall SA. S1P1 receptor agonists for use in the treatment of Crohn's disease. EP2455081; 2012
   Google Scholar
• Almirall SA. Pyrazole derivatives as S1P1 agonists. WO011144338; 2011
   Google Scholar
• Almirall SA. Oxadiazole derivatives as slpl receptor agonists. WO010081692; 2010
   Google Scholar
• Sanofi-Aventis. Heterocyclic carboxylic acid derivatives having a 2,5-substituted oxazolopyrimidine ring. WO011086080; 2011
   Google Scholar
• Sanofi-Aventis. Carboxylic acid derivatives having a 2,5-substituted oxazolopyrimidine ring. WO011086079; 2011
   Google Scholar
• Sanofi-Aventis. Heterocyclic carboxylic acid derivatives having a 2,5,7-substituted oxazolopyrimidine ring. WO011086078; 2011
   Google Scholar
• Sanofi-Aventis. Carboxylic acid derivatives having a 2,5,7-substituted oxazolopyrimidine ring. WO011086077; 2011
   Google Scholar
• Sanofi-Aventis. 2,5-substituted oxazolopyrimidine derivatives. WO011086081; 2011
   Google Scholar
• Sanofi-Aventis. 2,5,7-substituted oxazolopyrimidine derivatives. WO011086075; 2011
   Google Scholar
• Sanofi-Aventis. Oxazolopyrimidines as EDG-1 receptor agonists. WO010006704; 2010
   Google Scholar
• Merck Serono SA. Oxadiazole fused heterocyclic derivatives useful for the treatment of multiple sclerosis. WO010069949; 2010
   Google Scholar
• Merck Serono SA. Oxazole pyridine derivatives useful as S1P1 receptor agonists. WO010100142; 2010
   Google Scholar
• Merck Serono SA. Oxadiazole derivatives. WO010112461; 2010
   Google Scholar
• Merck Serono SA. Oxadiazole derivatives. WO010115751; 2010
   Google Scholar
• Merck Serono SA. Pyrazole oxadiazole derivatives as S1P1 agonists. WO010142628; 2010
   Google Scholar
• Merck Serono SA. 5-(biphenyl-4-yl)-3-phenyl-1,2,4-oxadiazolyl derivatives as ligands on the sphingosine 1-phosphate (S1P) receptors. WO012004287; 2012
   Google Scholar
• Abbott Laboratories. Novel oxadiazole compounds. WO011071570; 2011
   Google Scholar
• Abbott Laboratories. Agonists and antagonists of the S1P5 receptor, and methods of uses thereof. WO010093704; 2010
   Google Scholar
• Abbott Laboratories. (Thio)morpholine derivatives as S1P modulators. WO011023795; 2011
   Google Scholar
• Abbott Laboratories. Bisaryl(thio)morpholine derivatives as S1P modulators. WO012004375; 2012
   Google Scholar
• Abbott Laboratories. Fused heterocyclic derivatives as S1P modulators. WO012004373; 2012
   Google Scholar
• Abbott Laboratories. Spiro-cyclic amine derivatives as S1P modulators. WO012004378; 2012
   Google Scholar
• Biogen Indec Ma, Inc. Bicyclic aryl sphingosine 1-phosphate analogs. WO010051030; 2010
   Google Scholar
• Biogen Indec Ma, Inc. Heterobicyclic sphingosine 1-phosphate analogs. WO010051031; 2010
   Google Scholar
• Biogen Indec Ma, Inc. Bicyclic aryl sphingosine 1-phosphate analogs. WO011017561; 2011
   Google Scholar
• Biogen Indec Ma, Inc. S1P modulating agents. WO012109108; 2012
   Google Scholar
• Receptos, Inc. Selective heterocyclic Sphingosine 1 phosphate receptor modulators. WO011060391; 2011
   Google Scholar
• Receptos, Inc. Selective heterocyclic Sphingosine 1 phosphate receptor modulators. WO012158550; 2012
   Google Scholar
• Receptos, Inc. Sphingosine 1 phosphate receptor modulators and methods of chiral synthesis. WO011060389; 2011
   Google Scholar
• Receptos, Inc. Selective Sphingosine 1 phosphate receptor modulators and methods of chiral synthesis. WO011060392; 2011
   Google Scholar
• Novartis AG. Sphingosine 1 phosphate receptor modulators and their use to treat muscle inflammation. WO010010127; 2010
   Google Scholar
• Novartis AG. Immunosuppressant compounds and compositions. WO004103306; 2004
   Google Scholar
• Novartis AG. Immunosuppressant compounds and compositions. WO005000833; 2005
   Google Scholar
• Novartis AG. FTY720 halogenated derivatives. WO011070066; 2011
   Google Scholar
• Akaal Pharma PTY Ltd. S1P receptors modulators. WO010042998; 2010
   Google Scholar
• Akaal Pharma PTY Ltd. S1P receptors modulators and their use thereof. WO010043000; 2010
   Google Scholar
• Actelion Pharmaceuticals Ltd. 2-methoxy-pyridin-4-yl derivatives. WO012098505; 2012
   Google Scholar
• Actelion Pharmaceuticals Ltd. Pyridin-4-yl derivatives as immunomodulating agents. WO008029371; 2008
   Google Scholar
• Astellas Pharma, Inc. 2H-chromene compound and derivative thereof. US0120178735; 2012
   Google Scholar
• Bioprojet. Sun Pharma Advance Research Co. Ltd. Novel piperidinyl monocarboxylic acids as S1P1 receptor agonists. WO012140020; 2012
   Google Scholar