TACRINE DERIVATIVES AS ACETYLCHOLINESTERASE INHIBITORS Russian patent published in 2010 - IPC C07D401/12 A61K31/473 A61K31/475 A61P25/28 

Abstract RU 2402545 C2

FIELD: chemistry.

SUBSTANCE: invention describes an amide of formula:

where A and B are independently selected from CH or N; D is H; Z is selected from hydrogen, unsubstituted C1-8alkyl, each L is independently selected from -CraRb-, -CRa=, -CO-, -O- or -NRa-; k, m, n, q, x and w are integers independently selected from 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, provided that k+m+n+q+x+w equals at least 4; R1-R6 are independently selected from hydrogen, CN or halogen; Ra and Rb are independently selected from hydrogen, unsubstituted C1-8alkyl, or its pharmaceutically acceptable salt. The invention describes a pharmaceutical composition, use of the compounds to treat AChE-mediated diseases, a treatment method, as well as an amide synthesis method and use of the formula (I) amide as a chemical agent for inhibiting acetylcholinesterase in biological research.

EFFECT: compounds have high acetylcholinesterase or butyrylcholinesterase inhibiting activity.

24 cl, 27 ex, 1 tbl

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RU 2 402 545 C2

Authors

Martines Khil' Ana

Dorronsoro Dias Isabel'

Rubio Arr'Eta Laura

Alonso Gordil'O Diana

Fuehrtes Uehrta Ana

Morales-Alselaj Susana

Del' Monte Mil'Jan Marija

Garsia Palomero Ehster

Usan Ehkhea Paola

De Austria Selija

Medina Padil'Ja Migel'

Mun'Os Ruis Pilar

Dates

2010-10-27Published

2004-07-09Filed