RU2225389C2 - Производные аминометилкарбоновой кислоты и фармацевтическая композиция на их основе - Google Patents
Производные аминометилкарбоновой кислоты и фармацевтическая композиция на их основе Download PDFInfo
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Abstract
Изобретение относится к новым производным аминометилкарбоновой кислоты формулы 1
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.
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
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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US9051280B2 (en) | 2010-08-13 | 2015-06-09 | AbbVie Deutschland GmbH & Co. KG | Tetraline and indane derivatives, pharmaceutical compositions containing them, and their use in therapy |
US8883839B2 (en) | 2010-08-13 | 2014-11-11 | Abbott Laboratories | Tetraline and indane derivatives, pharmaceutical compositions containing them, and their use in therapy |
US9045459B2 (en) * | 2010-08-13 | 2015-06-02 | AbbVie Deutschland GmbH & Co. KG | Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy |
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JP2016533375A (ja) | 2013-10-17 | 2016-10-27 | アッヴィ・ドイチュラント・ゲー・エム・ベー・ハー・ウント・コー・カー・ゲー | アミノテトラリン誘導体およびアミノインダン誘導体、これらを含有する医薬組成物、および治療におけるこれらの使用 |
WO2015055770A1 (en) | 2013-10-17 | 2015-04-23 | AbbVie Deutschland GmbH & Co. KG | Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy |
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AU2018336171B2 (en) | 2017-09-22 | 2023-01-05 | Jubilant Epipad LLC | Heterocyclic compounds as PAD inhibitors |
PL3697785T3 (pl) | 2017-10-18 | 2023-08-07 | Jubilant Epipad LLC | Związki imidazopirydynowe jako inhibitory pad |
AU2018362046B2 (en) | 2017-11-06 | 2023-04-13 | Jubilant Prodel LLC | Pyrimidine derivatives as inhibitors of PD1/PD-L1 activation |
US11459338B2 (en) | 2017-11-24 | 2022-10-04 | Jubilant Episcribe Llc | Heterocyclic compounds as PRMT5 inhibitors |
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US5657157A (en) * | 1995-06-23 | 1997-08-12 | Sdl, Inc. | Semiconductor optical amplifying media with reduced self-focusing |
ATE221520T1 (de) * | 1995-09-29 | 2002-08-15 | Glaxo Wellcome Spa | Tetrahydrochinoline als nmda antagonisten |
EP0918767A4 (en) * | 1996-05-31 | 2000-04-26 | Allelix Neuroscience Inc | PHARMACEUTICAL PRODUCT FOR THE TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS |
CA2254833C (en) * | 1996-05-31 | 2008-04-29 | Allelix Neuroscience Inc. | Pharmaceutical for treatment of neurological and neuropsychiatric disorders |
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