EA201592307A1 - Производные 4-амино-6-фенил-6,7-дигидро[1,2,3]триазоло[1,5-a]пиразина в качестве ингибиторов бета-секретазы (bace) - Google Patents
Производные 4-амино-6-фенил-6,7-дигидро[1,2,3]триазоло[1,5-a]пиразина в качестве ингибиторов бета-секретазы (bace)Info
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- EA201592307A1 EA201592307A1 EA201592307A EA201592307A EA201592307A1 EA 201592307 A1 EA201592307 A1 EA 201592307A1 EA 201592307 A EA201592307 A EA 201592307A EA 201592307 A EA201592307 A EA 201592307A EA 201592307 A1 EA201592307 A1 EA 201592307A1
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- Prior art keywords
- dementia
- beta
- bace
- triazolo
- dihydro
- Prior art date
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- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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Abstract
Настоящее изобретение относится к новым производным 6,7-дигидро[1,2,3]триазоло[1,5-а]пиразин-6-ила в качестве ингибиторов бета-секретазы, также известной как фермент, расщепляющий амилоид по бета-сайту, ВАСЕ, в частности, ВАСЕ1 и/или ВАСЕ2 (где ВАСЕ1 также известен как Asp2 или мемапсин 2 и ВАСЕ2 также известен как Aspl, мемапсин 1 или DRAP). Настоящее изобретение также относится к фармацевтическим композициям, содержащим такие соединения, к способам получения таких соединений и композиций и к применению таких соединений и композиций для предупреждения и лечения расстройств, в которые вовлечена бета-секретаза, таких как болезнь Альцгеймера (AD), умеренное когнитивное нарушение, старческое слабоумие, деменция, деменция с тельцами Леви, синдром Дауна, деменция, ассоциированная с инсультом, деменция, ассоциированная с болезнью Паркинсона, деменция альцгеймеровского типа, деменция, ассоциированная с накоплением бета-амилоида, возрастная макулодистрофия, диабет 2 типа и другие метаболические расстройства.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP13171720 | 2013-06-12 | ||
EP13171720.9 | 2013-06-12 | ||
PCT/EP2014/062286 WO2014198854A1 (en) | 2013-06-12 | 2014-06-12 | 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
Publications (2)
Publication Number | Publication Date |
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EA201592307A1 true EA201592307A1 (ru) | 2016-04-29 |
EA028775B1 EA028775B1 (ru) | 2017-12-29 |
Family
ID=48577637
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201592307A EA028775B1 (ru) | 2013-06-12 | 2014-06-12 | Производные 4-амино-6-фенил-6,7-дигидро[1,2,3]триазоло[1,5-a]пиразина в качестве ингибиторов бета-секретазы (bace) |
Country Status (12)
Country | Link |
---|---|
US (1) | US9751886B2 (ru) |
EP (1) | EP3008065B1 (ru) |
JP (1) | JP6435321B2 (ru) |
KR (1) | KR102243133B1 (ru) |
CN (1) | CN105324383B (ru) |
AU (1) | AU2014280125B2 (ru) |
BR (1) | BR112015030597A2 (ru) |
CA (1) | CA2911693C (ru) |
EA (1) | EA028775B1 (ru) |
ES (1) | ES2721073T3 (ru) |
MX (1) | MX366063B (ru) |
WO (1) | WO2014198854A1 (ru) |
Families Citing this family (7)
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EP2580200B1 (en) | 2010-06-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
EP2655376B1 (en) | 2010-12-22 | 2017-08-23 | Janssen Pharmaceutica NV | 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
CN103415521B (zh) | 2011-03-09 | 2016-01-06 | 詹森药业有限公司 | 用作β分泌酶(BACE)抑制剂的3,4-二氢-吡咯并[1,2-a]吡嗪-1-基胺衍生物 |
CN105452251B (zh) | 2013-06-12 | 2017-12-26 | 詹森药业有限公司 | 作为β‑分泌酶(BACE)抑制剂的4‑氨基‑6‑苯基‑5,6‑二氢咪唑并[1,5‑A]吡嗪‑3(2H)‑酮衍生物 |
WO2014198853A1 (en) | 2013-06-12 | 2014-12-18 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
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KR20170095881A (ko) | 2014-12-18 | 2017-08-23 | 얀센 파마슈티카 엔.브이. | 베타―세크레타제의 2,3,4,5―테트라히드로피리딘―6―아민 및 3,4―디히드로―2h―피롤―5―아민 화합물 억제제 |
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ES2582473T3 (es) | 2011-12-06 | 2016-09-13 | Janssen Pharmaceutica, N.V. | Derivados de 5-(3-aminofenil)-5-alquil-5,6-dihidro-2H-[1,4]oxazin-3-amina para el tratamiento de trastornos en que está implicada la beta-secretasa |
AU2013363151A1 (en) | 2012-12-20 | 2015-06-04 | Merck Sharp & Dohme Corp. | C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors |
CN105452251B (zh) | 2013-06-12 | 2017-12-26 | 詹森药业有限公司 | 作为β‑分泌酶(BACE)抑制剂的4‑氨基‑6‑苯基‑5,6‑二氢咪唑并[1,5‑A]吡嗪‑3(2H)‑酮衍生物 |
WO2014198853A1 (en) | 2013-06-12 | 2014-12-18 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
KR20170095881A (ko) | 2014-12-18 | 2017-08-23 | 얀센 파마슈티카 엔.브이. | 베타―세크레타제의 2,3,4,5―테트라히드로피리딘―6―아민 및 3,4―디히드로―2h―피롤―5―아민 화합물 억제제 |
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CN105324383A (zh) | 2016-02-10 |
JP6435321B2 (ja) | 2018-12-05 |
KR102243133B1 (ko) | 2021-04-22 |
US9751886B2 (en) | 2017-09-05 |
EA028775B1 (ru) | 2017-12-29 |
ES2721073T3 (es) | 2019-07-26 |
AU2014280125A1 (en) | 2015-11-12 |
BR112015030597A2 (pt) | 2017-07-25 |
KR20160019893A (ko) | 2016-02-22 |
CA2911693C (en) | 2021-08-24 |
CA2911693A1 (en) | 2014-12-18 |
AU2014280125B2 (en) | 2018-03-15 |
WO2014198854A1 (en) | 2014-12-18 |
JP2016520660A (ja) | 2016-07-14 |
US20160130274A1 (en) | 2016-05-12 |
CN105324383B (zh) | 2017-10-31 |
EP3008065B1 (en) | 2019-01-30 |
MX2015017155A (es) | 2016-03-16 |
EP3008065A1 (en) | 2016-04-20 |
MX366063B (es) | 2019-06-26 |
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