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RU2007143509A - Производные ацетилена - Google Patents

Производные ацетилена Download PDF

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RU2007143509A
RU2007143509A RU2007143509/04A RU2007143509A RU2007143509A RU 2007143509 A RU2007143509 A RU 2007143509A RU 2007143509/04 A RU2007143509/04 A RU 2007143509/04A RU 2007143509 A RU2007143509 A RU 2007143509A RU 2007143509 A RU2007143509 A RU 2007143509A
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compound
alkyl
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hydrogen
unsubstituted
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Ральф ГЛАТТАР (DE)
Ральф ГЛАТТАР
Томас Й. ТРОКСЛЕР (CH)
Томас Й. ТРОКСЛЕР
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Новартис АГ (CH)
Новартис Аг
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Abstract

1. Соединение формулы (I) ! ! в которой ! R1 обозначает водород или C1-С4алкил и ! R2 обозначает незамещенный или замещенный гетероцикл, или ! R1 обозначает водород или C1-С4алкил и ! R2 обозначает арил или замещенный арил, или ! R1 обозначает водород или C1-С4алкил и ! R2 обозначает C(О)R21, где R21 обозначает незамещенный или замещенный алкил, незамещенную или замещенную алкоксигруппу, незамещенный или замещенный гетероцикл, незамещенный или замещенный арил, или ! R1 и R2 совместно с атомом азота образуют незамещенный или замещенный гетероцикл; ! R3 обозначает (С1-С4)алкил, (С1-С4)алкоксигруппу, трифторметил, галоген, цианогруппу, нитрогруппу, -СНО, -СОО(C1-С4)алкил, -СО(C1-С4)алкил; ! n равно 0, 1, 2, 3, 4 или 5; ! R4 обозначает ОН и ! R5 и R6 обозначают Н или C1-С4алкил, или ! R4 и R5 образуют связь и ! R6 обозначает И или C1-С4алкил, или ! R4 и R6 образуют связь и ! R5 обозначает И или C1-С4алкил, ! в форме свободного основания или соли присоединения с кислотой. ! 2. Соединение формулы (I') ! ! в которой R1, R2, R3 являются такими, как определено в п.1. ! 3. Способ получения соединения формулы (I) по п.1 или его соли, который включает стадии ! а) получения соединения формулы (I), в которой R4 обозначает гидроксигруппу, R5 и R6 обозначают водород или С1-С4алкил, по реакции соединения формулы (II) ! ! в которой R1, R2, R3, R4 являются такими, как определено выше, с соединением формулы (III) ! ! в которой R3 и n являются такими, как определено выше, или ! b) получения соединения формулы (I), в которой R4 и R5 образуют связь и R6 обозначает водород или С1-С4алкил или в которой R4 и R6 образуют связь и R5 обозначает водород, с помощью дегидратации соединения формулы (I), в которой R4 обозначает гидроксигруппу, R5 и R6 обозначают водород или С1-�

Claims (9)

1. Соединение формулы (I)
Figure 00000001
в которой
R1 обозначает водород или C1-С4алкил и
R2 обозначает незамещенный или замещенный гетероцикл, или
R1 обозначает водород или C1-С4алкил и
R2 обозначает арил или замещенный арил, или
R1 обозначает водород или C1-С4алкил и
R2 обозначает C(О)R21, где R21 обозначает незамещенный или замещенный алкил, незамещенную или замещенную алкоксигруппу, незамещенный или замещенный гетероцикл, незамещенный или замещенный арил, или
R1 и R2 совместно с атомом азота образуют незамещенный или замещенный гетероцикл;
R3 обозначает (С1-С4)алкил, (С1-С4)алкоксигруппу, трифторметил, галоген, цианогруппу, нитрогруппу, -СНО, -СОО(C1-С4)алкил, -СО(C1-С4)алкил;
n равно 0, 1, 2, 3, 4 или 5;
R4 обозначает ОН и
R5 и R6 обозначают Н или C1-С4алкил, или
R4 и R5 образуют связь и
R6 обозначает И или C1-С4алкил, или
R4 и R6 образуют связь и
R5 обозначает И или C1-С4алкил,
в форме свободного основания или соли присоединения с кислотой.
2. Соединение формулы (I')
Figure 00000002
в которой R1, R2, R3 являются такими, как определено в п.1.
3. Способ получения соединения формулы (I) по п.1 или его соли, который включает стадии
а) получения соединения формулы (I), в которой R4 обозначает гидроксигруппу, R5 и R6 обозначают водород или С1-С4алкил, по реакции соединения формулы (II)
Figure 00000003
в которой R1, R2, R3, R4 являются такими, как определено выше, с соединением формулы (III)
Figure 00000004
в которой R3 и n являются такими, как определено выше, или
b) получения соединения формулы (I), в которой R4 и R5 образуют связь и R6 обозначает водород или С1-С4алкил или в которой R4 и R6 образуют связь и R5 обозначает водород, с помощью дегидратации соединения формулы (I), в которой R4 обозначает гидроксигруппу, R5 и R6 обозначают водород или С1-С4алкил, или
c) получения соединения формулы (I), в которой i) R4 обозначает гидроксигруппу,
R1 обозначает водород или С1-С4алкил и R2 обозначает незамещенный или замещенный гетероцикл или ii) R1 обозначает водород или С1-С4алкил и R обозначает арил или замещенный арил, с помощью восстановительного аминирования соединения формулы (IV)
Figure 00000005
в которой R6, R5, R3, n являются такими, как определено выше, соединением формулы (V)
Figure 00000006
в которой R1 и R2 являются такими, как определено выше, или
d) получения соединения формулы (I), в которой R4 обозначает гидроксигруппу, R1 и R2 совместно с атомом азота образуют незамещенный или замещенный гетероцикл, с помощью циклоконденсации соединения формулы (VI)
Figure 00000007
и выделения полученного соединения формулы (I) в форме свободного основания или соли присоединения с кислотой.
4. Соединение по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой, предназначенное для применения в качестве фармацевтического средства.
5. Соединение по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой, предназначенное для применения для предупреждения, лечения или задержки прогрессирования нарушений, связанных с нерегулярностью глутаматергической передачи сигнала, нарушений желудочно-кишечного тракта и мочевых путей, и нервной системы, полностью или частично опосредуемых mGluR5.
6. Фармацевтическая композиция, включающая соединение по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой совместно с фармацевтическим носителем или разбавителем.
7. Применение соединения по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой для предупреждения, лечения или задержки прогрессирования нарушений, связанных с нерегулярностью глутаматергической передачи сигнала, нарушений желудочно-кишечного тракта и мочевых путей, и нервной системы, полностью или частично опосредуемых mGluR5.
8. Применение соединения по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой для приготовления фармацевтической композиции, предназначенной для предупреждения, лечения или задержки прогрессирования нарушений, связанных с нерегулярностью глутаматергической передачи сигнала, нарушений желудочно-кишечного тракта и мочевых путей, и нервной системы, полностью или частично опосредуемых mGluR5.
9. Способ лечения нарушений, связанных с нерегулярностью глутаматергической передачи сигнала и нарушений нервной системы, полностью или частично опосредуемых mGluR5, способ включает введение субъекту, нуждающемуся в таком лечении, терапевтически эффективного количества соединения по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой.
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2688677C2 (ru) * 2014-10-24 2019-05-22 Лэндос Байофарма, Инк. Лекарственные средства на основе лантионинсинтетаза с-подобного белка

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0220581D0 (en) 2002-09-04 2002-10-09 Novartis Ag Organic Compound
PE20060437A1 (es) 2004-06-18 2006-06-08 Novartis Ag COMPUESTOS AZA-BICICLONONANOS COMO LIGANDOS COLINERGICOS DE nAChR
GB0415746D0 (en) * 2004-07-14 2004-08-18 Novartis Ag Organic compounds
GB0503646D0 (en) * 2005-02-22 2005-03-30 Novartis Ag Organic compounds
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GB0525672D0 (en) * 2005-12-16 2006-01-25 Novartis Ag Organic compounds
GB0525673D0 (en) * 2005-12-16 2006-01-25 Novartis Ag Organic compounds
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
CN102762572A (zh) 2010-02-01 2012-10-31 诺瓦提斯公司 作为CRF-1受体拮抗剂的吡唑并[5,1b]*唑衍生物
WO2011092293A2 (en) 2010-02-01 2011-08-04 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
CN102753527B (zh) 2010-02-02 2014-12-24 诺华股份有限公司 用作crf受体拮抗剂的环己基酰胺衍生物
EA202091325A1 (ru) 2017-11-30 2020-08-28 Лэндос Байофарма, Инк. Способы лечения с помощью лигандов лантионин c-подобного белка 2 и подготовленных с их помощью клеток
JP7430852B2 (ja) 2019-12-20 2024-02-14 エヌイミューン バイオファーマ インコーポレイテッド ランチオニンｃ様タンパク質２リガンド、それを用いて調製される細胞、およびそれを使用する療法

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3991064A (en) * 1975-01-17 1976-11-09 Warner-Lambert Company Benzonaphthyridines
EP0689535B1 (en) * 1993-03-18 1998-09-23 MERCK SHARP & DOHME LTD. Benzimidazole derivatives
AU6215594A (en) * 1993-03-18 1994-10-11 Merck Sharp & Dohme Limited Indole derivatives as dopamine d4 antagonists
US5521297A (en) * 1993-06-04 1996-05-28 Salk Institute Biotechnology/Industrial Associates Nucleic acids encoding human metabotropic glutamate receptors
CA2188949A1 (en) * 1994-04-28 1995-11-09 Janusz Jozef Kulagowski Benzofuran derivatives as d4 receptor antagonists
US5830901A (en) * 1994-08-10 1998-11-03 Merch Sharp & Dohme Ltd Tetrahydropyridinylmethyl derivatives of pyrrolo 2,3-B!pyridine
US5688798A (en) * 1995-10-10 1997-11-18 Hoffmann-La Roche Inc. Pyrimidine compounds
AUPR201600A0 (en) * 2000-12-11 2001-01-11 Fujisawa Pharmaceutical Co., Ltd. Quinazolinone derivative
GB0128996D0 (en) * 2001-12-04 2002-01-23 Novartis Ag Organic compounds
US6806279B2 (en) * 2001-12-17 2004-10-19 Sunesis Pharmaceuticals, Inc. Small-molecule inhibitors of interleukin-2
US6995144B2 (en) * 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
GB0503646D0 (en) * 2005-02-22 2005-03-30 Novartis Ag Organic compounds
GB0508318D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0508319D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2688677C2 (ru) * 2014-10-24 2019-05-22 Лэндос Байофарма, Инк. Лекарственные средства на основе лантионинсинтетаза с-подобного белка

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