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(19)

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2 482 107

(13)

(51)

IPC

C07C215/64(2006-01-01)

C07C227/14(2006-01-01)

C07C229/28(2006-01-01)

C07C237/48(2006-01-01)

A61K31/197(2006-01-01)

A61K31/216(2006-01-01)

A61P1/00(2006-01-01)

(21) (22)

Application

2010128542/04, 2008-12-10

(24)

Start date

2008-12-10

(22)

Actual filing date

2008-12-10

(45)

Published

2013-05-20

(72)

Inventor

Trehpp Shon Dzh.Lidbetter Majkl R.Long Dehniel D.Dzhekobsen Dzhon R.Van Dajk PristsillaKol'Son P'Er-ZhanRapta MiroslavJuj In

(73)

Holder

Terevans, Ink.

3-CARBOXYPROPYL-AMINOTETRALINE DERIVATIVES AND RELATED COMPOUNDS AS MU-OPIOID RECEPTOR ANTAGONISTS Russian patent published in 2013 - IPC C07C215/64 C07C227/14 C07C229/28 C07C237/48 A61K31/197 A61K31/216 A61P1/00

Abstract RU 2482107 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (I) or pharmaceutically acceptable salts thereof having mu-opioid receptor antagonist activity. In formula (I), R¹ means -OR^a or -C(O)NR^bR^c; R², R³ and R⁴mean, each independently, C_1-3alkyl; R⁵ is specified in C_1-6alkyl, cyclohexyl, -(CH₂)_1-3-cyclohexyl and -(CH₂)_1-3-phenyl; R^a, R^b and R^cmean, each independently, hydrogen; and R⁶ means hydrogen or C_1-3alkyl; and substitutes in the starred chiral centres are found in a trans configuration. The invention also refers to a method for preparing compounds of formula (I), to intermediate compounds used in the synthesis of the compounds of formula (1) and a method for preparing them. Furthermore, the invention refers to a pharmaceutical composition comprising the compounds of formula (I), and to the use of such compounds for treating the diseases or conditions associated with mu-opioid receptor activity.

EFFECT: new pharmaceutical composition is presented.

25 cl, 19 ex

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RU 2 482 107 C2

Authors

Trehpp Shon Dzh.

Lidbetter Majkl R.

Long Dehniel D.

Dzhekobsen Dzhon R.

Van Dajk Pristsilla

Kol'Son P'Er-Zhan

Rapta Miroslav

Juj In

Dates

2013-05-20—Published

2008-12-10—Filed