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Flupirtine
Flupirtine is an aminopyridine that functions as a centrally acting non-opioid analgesic. It first became available in Europe in 1984, and is sold mainly under the names Katadolon, Trancolong, Awegal, Efiret, Trancopal Dolo, and Metanor.〔(Flupirtine ) Drugs.com. Accessed 20 September 2011.〕 Like nefopam, it is unique among analgesics in that it is a non-opioid, non-NSAID, non-steroidal centrally acting analgesic. In 2010 the chemically related drug (the difference being that the pyridine group in flupirtine is replaced with a phenyl group) retigabine (INN; ezogabine ()) was approved by the FDA as an anticonvulsant for the treatment of refractory partial-onset seizures in treatment-experienced patients. Retigabine also works by opening the neuronal KCNQ/Kv7 potassium channel, just like flupirtine.
==History==
Flupirtine was originally developed by Asta Medica, with the synthesis of the compound and the development of the drug described in patents from the 1970s to the 2000s.〔http://www.freepatentsonline.com/5721258.html Primary and secondary neuroprotective effect of flupirtine in neurodegenerative diseases ''The synthesis of flupirtine and its pharmaceutically acceptable salts is described in EP 160 865 and 199 951''. EP0199951 ''December, 1986 Process for the preparation of 2-amino-3-nitro-6-(4-fluorobenzylamino) pyridine and of 2-amino-3-carbethoxyamino-6-(4-fluorobenzylamino) pyridine''.〕〔http://patent.ipexl.com/EP/EP0199951.html#reference ''Process for the preparation of 2-amino-3-nitro-6-(4-fluorobenzylamino) pyridine and of EPO Patent EP0199951'' 1986 German.〕〔http://www.patentfish.com/2-amino-3-carbethoxyamino-6-4-fluoro-benzylamino Process for the preparation of 2-amino-3-nitro-6-(4-fluorobenzylamino) pyridine and of 2-amino-3-carbethoxyamino-6-(4-fluorobenzylamino) pyridine
EP 0199951 B1 1986. English.〕〔http://patent.ipexl.com/US/4481205.html 2-Amino-3-carbethoxyamino-6-(p-fluoro-benzylamino)-pyridine-maleate United States Patent 4481205. 1981〕〔http://www.freepatentsonline.com/3998834.html Novel N-(4-piperidinyl)-N-phenylamides and -carbamates having very potent analgesic activity, methods of preparing same and useful intermediates therefor. Patent 3998834. 1976.〕〔http://www.faqs.org/patents/app/20090306150 CARBOXYLIC ACID SALTS OF 2-AMINO-3-CARBETHOXYAMINO-6-(4-FLUORO-BENZYLAMINO)-PYRIDINE patent 20090306150. 2009. ''Flupirtine is commonly used in the form of pharmaceutically acceptable acid addition salts. Commercially, flupirtine is available as its maleate addition salt under the trademark Katadolon®. There are two known polymorphs of flupirtine maleate, designated in the art as flupirtine maleate A and B. European patentEP 0 977 736 discloses pure flupirtine maleate crystalline form A and a process for its preparation. Flupirtine and mixtures of flupirtine maleate polymorphs A and B can be synthesised according to EP 0 199 951.''〕
It was approved for the treatment of pain in 1984 in Europe. However, it has never been introduced to the United States market for any indication. In 2008, Adeona Pharmaceuticals, Inc. (now called Synthetic Biologics, Inc.) obtained an option to license issued and patent pending applications relating to flupirtine’s use in the treatment of ophthalmic indications, particularly retinitis pigmentosa.
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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