RU2442775C2 - Histamine nz-receptor antagonists - Google Patents

Histamine nz-receptor antagonists Download PDF

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Publication number
RU2442775C2
RU2442775C2 RU2007147044/04A RU2007147044A RU2442775C2 RU 2442775 C2 RU2442775 C2 RU 2442775C2 RU 2007147044/04 A RU2007147044/04 A RU 2007147044/04A RU 2007147044 A RU2007147044 A RU 2007147044A RU 2442775 C2 RU2442775 C2 RU 2442775C2
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Russia
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represented
compounds
pharmaceutically acceptable
histamine
compound
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RU2007147044/04A
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RU2007147044A (en
Inventor
Рольф ХОЛЬВЕГ (DK)
Рольф Хольвег
Кнуд Эрик АНДЕРСЕН (DK)
Кнуд Эрик Андерсен
Ян Линди СЁРЕНСЕН (DK)
Ян Линди СЁРЕНСЕН
Жан Мари ЛУНДБЕК (DK)
Жан Мари ЛУНДБЕК
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Хай Пойнт Фармасьютикалс, ЛЛС
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Abstract

FIELD: chemistry.
SUBSTANCE: present invention refers to new compounds of formula I-9
Figure 00000214
where q is represented by 1; R11 is represented by C3-8-alkyl; C3-8-cycloalkyl or C3-8-cycloalkyl-C1-3-alkyl; A is represented by phenyl substituted by one or more substituting groups independently chosen from R12; and R12 is represented by -(CH2)-NR13R14; R13 is represented by C1-6-alkylcarbanil; and R14 is represented by hydrogen; and to the pharmaceutically acceptable salts of such compounds and to the pharmaceutical compositions based on such compounds. It has been revealed that the compounds of formula I-9 are histamine NZ-receptor antagonists and thus that they can be used in treatment of diseases connected with expression of such receptors.
EFFECT: compounds of formula I-9 can be used in treatment of diseases connected with expression of histamine NZ-receptors.
6 cl, 216 ex

Description

Текст описания приведен в факсимильном виде.

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The text of the description is given in facsimile form.
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Claims (6)

1. Соединение формулы I-9:
Figure 00000213

где q представляет собой 1;
R11 представляет собой С3-8-алкил, С3-8-циклоалкил или С3-8-циклоалкил-С1-3-алкил;
А представляет собой фенил, замещенный одним или более заместителями, независимо выбранными из R12; и
R12 представляет собой -(CH2)-NR13R14;
R13 представляет собой С1-6-алкилкарбонил; и R14 представляет собой водород;
или его фармацевтически приемлемая соль.1. The compound of formula I-9:
Figure 00000213

where q is 1;
R 11 represents C 3-8 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkyl-C 1-3 alkyl;
A is phenyl substituted with one or more substituents independently selected from R 12 ; and
R 12 represents - (CH 2 ) —NR 13 R 14 ;
R 13 represents C 1-6 alkylcarbonyl; and R 14 represents hydrogen;
or a pharmaceutically acceptable salt thereof. 2. Соединение по п.1, где R13 представляет собой ацетил.2. The compound according to claim 1, where R 13 represents acetyl. 3. Соединение по п.1, где это соединение представляет собой N-{4-[2-(4-изопропилпиперазин-1-ил)пиримидин-5-ил]бензил}ацетамид, или его фармацевтически приемлемая соль.3. The compound according to claim 1, where this compound is N- {4- [2- (4-isopropylpiperazin-1-yl) pyrimidin-5-yl] benzyl} acetamide, or a pharmaceutically acceptable salt thereof. 4. Соединение по п.1, где это соединение представляет собой N-{4-[2-(4-изопропилпиперазин-1-ил)пиримидин-5-ил]бензил}изобутирамид, или его фармацевтически приемлемая соль.4. The compound according to claim 1, where this compound is N- {4- [2- (4-isopropylpiperazin-1-yl) pyrimidin-5-yl] benzyl} isobutyramide, or a pharmaceutically acceptable salt thereof. 5. Соединение по п.1, где это соединение представляет собой N-{4-[2-(4-циклопропилпиперазин-1-ил)пиримидин-5-ил]бензил}ацетамид, или его фармацевтически приемлемая соль.5. The compound according to claim 1, where this compound is N- {4- [2- (4-cyclopropylpiperazin-1-yl) pyrimidin-5-yl] benzyl} acetamide, or a pharmaceutically acceptable salt thereof. 6. Фармацевтическая композиция, обладающая способностью модулировать Н3-гистаминовый рецептор, содержащая соединение по любому из пп.1-5 и фармацевтически приемлемый носитель или эксципиент. 6. A pharmaceutical composition having the ability to modulate an H3-histamine receptor containing a compound according to any one of claims 1 to 5 and a pharmaceutically acceptable carrier or excipient.
RU2007147044/04A 2005-07-04 2006-06-30 Histamine nz-receptor antagonists RU2442775C2 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
EP05106038.2 2005-07-04
EP05106037.4 2005-07-04
EP05106037 2005-07-04
EP05106038 2005-07-04
EP05109674.1 2005-10-18
EP06114615 2006-05-29
EP06114615.5 2006-05-29

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GB1345880A (en) * 1971-06-18 1974-02-06 Cepbepe Pyridazine derivatives
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US4616014A (en) * 1981-10-22 1986-10-07 Fujisawa Pharmaceutical Co., Ltd. Triazine derivatives, and pharmaceutical compositions comprising the same
EA005160B1 (en) * 2001-07-12 2004-12-30 Ле Лаборатуар Сервье OCTAHYDRO-2H-PYRIDO [1,2-alpha]PYRAZIN COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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