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RU2225389C2 - Производные аминометилкарбоновой кислоты и фармацевтическая композиция на их основе - Google Patents

Производные аминометилкарбоновой кислоты и фармацевтическая композиция на их основе Download PDF

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RU2225389C2
RU2225389C2 RU2001105536/04A RU2001105536A RU2225389C2 RU 2225389 C2 RU2225389 C2 RU 2225389C2 RU 2001105536/04 A RU2001105536/04 A RU 2001105536/04A RU 2001105536 A RU2001105536 A RU 2001105536A RU 2225389 C2 RU2225389 C2 RU 2225389C2
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aminomethyl
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tetrahydronaphthalen
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Сэмьюэл Джордж ГИБСОН (GB)
Сэмьюэл Джордж ГИБСОН
Дэвид Роберт ДЖААП (GB)
Дэвид Роберт ДЖААП
Саймон Николас ТОРН (GB)
Саймон Николас ТОРН
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Abstract

Изобретение относится к новым производным аминометилкарбоновой кислоты формулы 1
Figure 00000001

где Z представляет собой (СН2)n, О или S; n равно 0, 1 или 2; Х представляет собой 1-3 заместителя, независимо выбранных из водорода, галогена, (С1-6)алкилокси,(С3-6)циклоалкилокси, (С6-12)арилокси, (С6-12)арила, тиенила, CN, СООR6 и (С1-4)алкила, необязательно замещенного галогеном, или 2 заместителя в смежных положениях вместе представляют собой конденсированную (С5-6)арильную группу или O-(СН2)m-O, где m равно 1 или 2; Y представляет собой 1-3 выбранных из водорода, галогена, (С1-4)алкилокси и (С1-4)алкила, необязательно замещенного галогеном; R1 представляет собой COOR7; R2 и R6 представляют собой (С1-4)алкил; R3, R4 и R5 независимо представляют собой водород; R7, R8 и R9 независимо представляют собой водород или (С1-4)алкил; или его фармацевтически приемлемым солям, а также к фармацевтической композиции на их основе, обладающей действием на центральную нервную систему. Технический результат - получение новых соединений, обладающих ценным фармацевтическим действием. 2 с. и 5 з.п. ф-лы, 1 табл.

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Claims (7)

1. Производные аминометилкарбоновой кислоты, имеющие общую формулу I
Figure 00000060
где Z представляет собой (СН2)n, О или S;
n = 0,1 или 2;
Х представляет собой 1-3 заместителя, независимо выбранных из водорода, галогена, (С1-6)алкилокси, (С3-6)циклоалкилокси, (С6-12)арилокси, (С6-12)арила, тиенила, CN, COOR6 и (С1-4)алкила, необязательно замещенного галогеном, или два заместителя в смежных положениях вместе представляют собой конденсированную (С5-6)арильную группу или O-(СН2)m-O, где m = 1 или 2;
Y представляет собой 1-3 заместителя, независимо выбранных из водорода, галогена, (С1-4)алкилокси и (С1-4)алкила, необязательно замещенного галогеном;
R1 представляет собой COOR7;
R2 и R6 представляют собой (С1-4)алкил;
R3, R4 и R5 независимо представляют собой водород;
R7, R8 и R9 независимо представляют собой водород или (С1-4)алкил;
или их фармацевтически приемлемые соли.
2. Производное аминометилкарбоновой кислоты по п.1, в котором Z представляет собой (СН2)n и n=1.
3. Производное аминометилкарбоновой кислоты по п.2, в котором R2 представляет собой метил.
4. Производное аминометилкарбоновой кислоты по любому из пп.1-4, имеющее цис-конфигурацию.
5. Производное аминометилкарбоновой кислоты по п.1, выбранное из следующих левовращающих энантиомеров:
(-)-литий цис-N-метил-N-(6-метокси-1-фенил-1,2,3,4-тетрагидронафталин-2-илметил)аминометилкарбоксилат;
(-)-натрий цис-N-метил-N-(6-метил-1-фенил-1,2,3,4-тетрагидронафталин-2-илметил)аминометилкарбоксилат;
(-)-натрий цис-N-метил-N-(6-фенокси-1-фенил-1,2,3,4-тетрагидронафталин-2-илметил)аминометилкарбоксилат;
(-)-литий N-метил-N-[1-(4-фторфенил)-6-трифторметил-1,2,3,4-тетрагидронафталин-2-илметил] аминометилкарбоксилат и
(-)-литий цис-N-метил-1N-[1-фенил-6-(2,2-диметилпропил-окси)-1,2,3,4-тетрагидронафталин-2-илметил]аминометилкарбоксилат.
6. Производные аминометилкарбоновой кислоты формулы I или их фармацевтически приемлемые соли по любому из пп.1-5 в качестве активного компонента лекарственного средства, обладающего действием на ЦНС.
7. Фармацевтическая композиция, обладающая действием на центральную нервную систему, содержащая производное аминометилкарбоновой кислоты общей формулы I или его фармацевтически приемлемую соль в смеси с фармацевтически приемлемыми вспомогательньми веществами.
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