MX368326B - Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]pirazin-3(2h )-ona como inhibidores de beta-secretasa (bace). - Google Patents
Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]pirazin-3(2h )-ona como inhibidores de beta-secretasa (bace).Info
- Publication number
- MX368326B MX368326B MX2015017151A MX2015017151A MX368326B MX 368326 B MX368326 B MX 368326B MX 2015017151 A MX2015017151 A MX 2015017151A MX 2015017151 A MX2015017151 A MX 2015017151A MX 368326 B MX368326 B MX 368326B
- Authority
- MX
- Mexico
- Prior art keywords
- beta
- dementia
- secretase
- dihydroimidazo
- bace
- Prior art date
Links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D487/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
- A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Abstract
La presente invención se refiere a novedosos derivados de 5,6-dihidroimidazo[1,5-a]pirazin-3(2H)-ona como inhibidores de beta-secretasa, también conocida como enzima de escisión amiloide del sitio beta, BACE, en particular BACE1 y/o BACE2 (en donde BACE1, también se conoce como Asp2 o memapsina2 y BACE2 también se conoce como Asp1, Memapsína 1 o DRAP); la invención también se dirige a composiciones farmacéuticas que comprenden dichos compuestos, a procesos para preparar dichos compuestos y composiciones y al uso de dichos compuestos y composiciones para la prevención y el tratamiento de trastornos en los que participa la beta-secretasa, tales como la enfermedad de Alzheimer (AD), deficiencia cognitiva leve, senilidad, demencia, demencia con cuerpos de Lewy, síndrome de Down, demencia asociada con accidente cerebrovascular, demencia asociada con enfermedad de Parkinson, demencia tipo Alzheimer, demencia asociada con beta-amiloide, degeneración macular relacionada con la edad, diabetes tipo 2 y otros trastornos metabólicos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP13171723 | 2013-06-12 | ||
PCT/EP2014/062283 WO2014198851A1 (en) | 2013-06-12 | 2014-06-12 | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace) |
Publications (2)
Publication Number | Publication Date |
---|---|
MX2015017151A MX2015017151A (es) | 2016-03-16 |
MX368326B true MX368326B (es) | 2019-09-27 |
Family
ID=48577639
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2015017151A MX368326B (es) | 2013-06-12 | 2014-06-12 | Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]pirazin-3(2h )-ona como inhibidores de beta-secretasa (bace). |
Country Status (12)
Country | Link |
---|---|
US (1) | US9834559B2 (es) |
EP (1) | EP3008067B1 (es) |
JP (1) | JP6387402B2 (es) |
KR (1) | KR102243135B1 (es) |
CN (1) | CN105452251B (es) |
AU (1) | AU2014280122B2 (es) |
BR (1) | BR112015030498A2 (es) |
CA (1) | CA2912156C (es) |
EA (1) | EA032662B1 (es) |
ES (1) | ES2627633T3 (es) |
MX (1) | MX368326B (es) |
WO (1) | WO2014198851A1 (es) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102933564B (zh) | 2010-06-09 | 2015-07-22 | 詹森药业有限公司 | 用作β-分泌酶(BACE)抑制剂的5,6-二氢-2H-[1,4]噁嗪-3-基-胺衍生物 |
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) |
KR102012675B1 (ko) | 2011-03-09 | 2019-08-21 | 얀센 파마슈티카 엔.브이. | 베타-세크레타제(BACE)의 억제제로서 유용한 3,4-디하이드로-피롤로[1,2-a]피라진-1-일아민 유도체 |
ES2697684T3 (es) | 2013-06-12 | 2019-01-25 | Janssen Pharmaceutica Nv | Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5 a]pirazina como inhibidores de beta-secretasa (BACE) |
AU2014280122B2 (en) | 2013-06-12 | 2017-12-21 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2H)-one derivatives as inhibitors of beta-secretase (BACE) |
CA2911693C (en) | 2013-06-12 | 2021-08-24 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
AU2015367594C1 (en) | 2014-12-18 | 2019-10-31 | Janssen Pharmaceutica Nv | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2H-pyrrol-5-amine compound inhibitors of beta-secretase |
CN111484497B (zh) * | 2019-01-25 | 2021-07-02 | 江苏恒瑞医药股份有限公司 | 咪唑并[1,5-a]吡嗪类衍生物的可药用盐、晶型及其制备方法 |
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ES2697684T3 (es) | 2013-06-12 | 2019-01-25 | Janssen Pharmaceutica Nv | Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5 a]pirazina como inhibidores de beta-secretasa (BACE) |
AU2014280122B2 (en) | 2013-06-12 | 2017-12-21 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2H)-one derivatives as inhibitors of beta-secretase (BACE) |
CA2911693C (en) | 2013-06-12 | 2021-08-24 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
AU2015367594C1 (en) | 2014-12-18 | 2019-10-31 | Janssen Pharmaceutica Nv | 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2H-pyrrol-5-amine compound inhibitors of beta-secretase |
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2014
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- 2014-06-12 JP JP2016518497A patent/JP6387402B2/ja not_active Expired - Fee Related
- 2014-06-12 EA EA201592278A patent/EA032662B1/ru not_active IP Right Cessation
- 2014-06-12 CN CN201480033513.0A patent/CN105452251B/zh active Active
- 2014-06-12 MX MX2015017151A patent/MX368326B/es active IP Right Grant
- 2014-06-12 CA CA2912156A patent/CA2912156C/en active Active
- 2014-06-12 KR KR1020157034929A patent/KR102243135B1/ko active IP Right Grant
- 2014-06-12 WO PCT/EP2014/062283 patent/WO2014198851A1/en active Application Filing
- 2014-06-12 US US14/897,420 patent/US9834559B2/en active Active
- 2014-06-12 BR BR112015030498A patent/BR112015030498A2/pt active Search and Examination
- 2014-06-12 EP EP14732131.9A patent/EP3008067B1/en active Active
- 2014-06-12 ES ES14732131.9T patent/ES2627633T3/es active Active
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CA2912156A1 (en) | 2014-12-18 |
EA201592278A1 (ru) | 2016-09-30 |
MX2015017151A (es) | 2016-03-16 |
EA032662B1 (ru) | 2019-06-28 |
KR20160018538A (ko) | 2016-02-17 |
JP6387402B2 (ja) | 2018-09-05 |
AU2014280122B2 (en) | 2017-12-21 |
CA2912156C (en) | 2021-07-20 |
ES2627633T3 (es) | 2017-07-28 |
EP3008067A1 (en) | 2016-04-20 |
KR102243135B1 (ko) | 2021-04-22 |
AU2014280122A1 (en) | 2015-11-19 |
US9834559B2 (en) | 2017-12-05 |
CN105452251A (zh) | 2016-03-30 |
WO2014198851A1 (en) | 2014-12-18 |
US20160115171A1 (en) | 2016-04-28 |
JP2016521718A (ja) | 2016-07-25 |
EP3008067B1 (en) | 2017-03-29 |
CN105452251B (zh) | 2017-12-26 |
BR112015030498A2 (pt) | 2017-07-25 |
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