Fgfr inhibitor for use in the treatment of hypophosphatemic disorders

作者: Vito Guagnano , Michaela Kneissel , Diana Graus Porta , Simon Wöhrle

DOI:

关键词:

摘要: The present invention relates generally to 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimid-4-yl}-l-methyl-urea or a pharmaceutically acceptable salt solvate thereof pharmaceutical composition comprising 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimid-4-yl}-1-methyl-urea for use in the treatment of X-linked hypophosphatemic rickets (XLH), autosomal dominant (ADHR), recessive (ARHR), tumor-induced osteomalacia, post-renal transplant hypophosphatemia, epidermal nevus syndrome, osteoglophonic dysplasia McCune-Albright syndrome.

参考文章(18)
Vito Guagnano, Diana Graus Porta, Giordano Caponigro, Yao Yao, Method for treating haematological cancers ,(2010)
Carsten Spanka, Soldermann Carole Pissot, Werner Breitenstein, Vito Guagnano, Giorgio Caravatti, Joseph Schoepfer, Paul W. Manley, Guido Bold, Pascal Furet, Nathanael Schiander Gray, Qiang Ding, Marc Lang, Tetsuo Uno, Guobao Zhang, Yi Liu, Taebo Sim, Bing Li, Pyrimidine urea derivatives as kinase inhibitors ,(2005)
Richard J. Bastin, Michael J. Bowker, Bryan J. Slater, Salt Selection and Optimisation Procedures for Pharmaceutical New Chemical Entities Organic Process Research & Development. ,vol. 4, pp. 427- 435 ,(2000) , 10.1021/OP000018U
Kenneth R. Morris, Michael G. Fakes, Ajit B. Thakur, Ann W. Newman, Ambarish K. Singh, John J. Venit, Ciro J. Spagnuolo, Abu T.M. Serajuddin, An integrated approach to the selection of optimal salt form for a new drug candidate International Journal of Pharmaceutics. ,vol. 105, pp. 209- 217 ,(1994) , 10.1016/0378-5173(94)90104-X
Simon Wöhrle, Olivier Bonny, Noemie Beluch, Swann Gaulis, Christelle Stamm, Marcel Scheibler, Matthias Müller, Bernd Kinzel, Anne Thuery, Joseph Brueggen, Nancy E Hynes, William R Sellers, Francesco Hofmann, Diana Graus-Porta, FGF receptors control vitamin D and phosphate homeostasis by mediating renal FGF-23 signaling and regulating FGF-23 expression in bone. Journal of Bone and Mineral Research. ,vol. 26, pp. 2486- 2497 ,(2011) , 10.1002/JBMR.478
Simon Wöhrle, Christine Henninger, Olivier Bonny, Anne Thuery, Noemie Beluch, Nancy E Hynes, Vito Guagnano, William R Sellers, Francesco Hofmann, Michaela Kneissel, Diana Graus Porta, Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. Journal of Bone and Mineral Research. ,vol. 28, pp. 899- 911 ,(2013) , 10.1002/JBMR.1810
Philip L. Gould, Salt selection for basic drugs International Journal of Pharmaceutics. ,vol. 33, pp. 201- 217 ,(1986) , 10.1016/0378-5173(86)90055-4
Kenneth E. White, Jose M. Cabral, Siobhan I. Davis, Tonya Fishburn, Wayne E. Evans, Shoji Ichikawa, Joanna Fields, Xijie Yu, Nick J. Shaw, Neil J. McLellan, Carole McKeown, David FitzPatrick, Kai Yu, David M. Ornitz, Michael J. Econs, Mutations that Cause Osteoglophonic Dysplasia Define Novel Roles for FGFR1 in Bone Elongation American Journal of Human Genetics. ,vol. 76, pp. 361- 367 ,(2005) , 10.1086/427956
R. Marsell, M. A. I. Mirza, H. Mallmin, M. Karlsson, D. Mellström, E. Orwoll, C. Ohlsson, K. B. Jonsson, Ö. Ljunggren, T. E. Larsson, Relation between fibroblast growth factor-23, body weight and bone mineral density in elderly men. Osteoporosis International. ,vol. 20, pp. 1167- 1173 ,(2009) , 10.1007/S00198-008-0780-2