COMPOSITIONS AND METHODS OF TREATING NEURODEGENERATIVE DISEASES Russian patent published in 2015 - IPC C07C217/20 C07C217/60 C07C217/62 C07C217/64 C07C217/72 C07C225/16 C07C229/38 C07C233/18 C07C235/08 C07C251/86 C07C279/08 C07C317/28 C07C323/25 C07D277/24 C07D309/06 A61K31/137 A61K31/155 A61K31/16 A61K31/197 A61K31/35 A61K31/10 A61P27/06 A61P27/00 

Abstract RU 2541430 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to novel compounds of general formula (A), their stereoisomers or pharmaceutically acceptable salts, possessing ability to inhibit activity of isomerase, taking part in visual cycle. Compounds can be applied for treatment of ophthalmological disease or disorder, such as age-related macular degeneration or Stargardt's macular dystrophy. In general formula (A) Z represents-C(R9)(R10)-C(R1)(R2)-; R1 and R2 each, independently on each other, are selected from hydrogen, halogen, C1-C5alkyl, or -OR6; or R1 and R2 together from oxo; R3 and R4 each, independently on each other, are selected from hydrogen; R6 is selected from a) C5-C15alkyl, optionally substituted with hydroxy, C1-C8alkoxy; or b) C5-C10carbocyclylalkyl, in which carbocycle is 4-, 5-, 6-, 7- or 8-member non-aromatic carbocycle, optionally substituted with hydroxy, halogen or R6CO2-; R9 and R10 each, independently on each other, is selected from hydrogen, halogen, C1-C5alkyl, optionally substituted with hydroxy, or -OR19; or R9 and R10 form oxo; or optionally, R9 and R1 together form direct bond to provide double bond; or optionally, R9 and R1 together form direct bond, and R10 and R2 together form direct bond to provide triple bond; R11 and R12 each, independently on each other, is selected from hydrogen, -C(=O)R23 or -C(NH)NH2, R23 is selected from C1-C8alkyl; R6, R19 and R34 are independently on each other are hydrogen or C1-C8alkyl; each R33 is independently selected from halogen, hydroxyl, C1-C5carboalkoxy, C1-C8alkyl, optionally substituted with hydroxy; and n equals 0 or 1.

EFFECT: compounds inhibit degeneration of retinal cell, in particular neuronal cell, such as photoreceptor cell, in patient's retina.

45 cl, 11 dwg, 11 tbl, 206 ex

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RU 2 541 430 C2

Authors

Skott Jen L.

Kuksa Vladimir A.

Orme Mark V.

Littl Tomas

Gehll Anna

Khong Feng

Dates

2015-02-10Published

2008-10-03Filed