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
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 title abstract 3
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 101150058765 BACE1 gene Proteins 0.000 title 1
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 5
- 102100021277 Beta-secretase 2 Human genes 0.000 abstract 5
- 206010012289 Dementia Diseases 0.000 abstract 5
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract 3
- 101000894883 Homo sapiens Beta-secretase 2 Proteins 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000024827 Alzheimer disease Diseases 0.000 abstract 2
- 101710150192 Beta-secretase 1 Proteins 0.000 abstract 2
- 101710150190 Beta-secretase 2 Proteins 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- AGGPGZVKBLSAHT-UHFFFAOYSA-N 5,6-dihydro-2H-imidazo[1,5-a]pyrazin-3-one Chemical class O=c1[nH]cc2C=NCCn12 AGGPGZVKBLSAHT-UHFFFAOYSA-N 0.000 abstract 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 abstract 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 abstract 1
- 206010067889 Dementia with Lewy bodies Diseases 0.000 abstract 1
- 201000010374 Down Syndrome Diseases 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 201000002832 Lewy body dementia Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 206010039966 Senile dementia Diseases 0.000 abstract 1
- 206010044688 Trisomy 21 Diseases 0.000 abstract 1
- 206010064930 age-related macular degeneration Diseases 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- IXHBTMCLRNMKHZ-LBPRGKRZSA-N levobunolol Chemical compound O=C1CCCC2=C1C=CC=C2OC[C@@H](O)CNC(C)(C)C IXHBTMCLRNMKHZ-LBPRGKRZSA-N 0.000 abstract 1
- 208000002780 macular degeneration Diseases 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 208000027061 mild cognitive impairment Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
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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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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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- 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
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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
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Transplantation (AREA)
- Dermatology (AREA)
- Toxicology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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 (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101730937B1 (ko) | 2010-06-09 | 2017-04-27 | 얀센 파마슈티카 엔.브이. | 베타-세크레타아제(bace) 저해제로 유용한 5,6-디하이드로-2h-[1,4]옥사진-3-일-아민 유도체 |
| BR112013015430A2 (pt) | 2010-12-22 | 2016-09-20 | Janssen Pharmaceutica Nv | derivados de 5,6-diidro-imidazo[1,2-a]pirazin-8-ilamina úteis como inibidores de beta-secretase (bace) |
| PH12013501805A1 (en) | 2011-03-09 | 2013-11-18 | Janssen Pharmaceutica Nv | 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| US9751886B2 (en) | 2013-06-12 | 2017-09-05 | 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) |
| WO2014198851A1 (en) | 2013-06-12 | 2014-12-18 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace) |
| CN105283457B (zh) | 2013-06-12 | 2018-09-18 | 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]吡嗪衍生物 |
| ES2768823T3 (es) | 2014-12-18 | 2020-06-23 | Janssen Pharmaceutica Nv | Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa |
| 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 |
| US12297244B2 (en) | 2019-06-05 | 2025-05-13 | Rensselaer Polytechnic Institute | Systems and methods for inhibiting γ-secretase production of amyloid-β peptides |
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| JP4799864B2 (ja) | 2002-09-23 | 2011-10-26 | シェーリング コーポレイション | サイクリン依存性キナーゼインヒビターとしてのイミダゾピラジン |
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| PT1678172E (pt) | 2003-10-15 | 2010-03-03 | Targacept Inc | Composições farmacêuticas e métodos para alívio da dor e tratamento de perturbações do sistema nervoso central |
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| KR101730937B1 (ko) | 2010-06-09 | 2017-04-27 | 얀센 파마슈티카 엔.브이. | 베타-세크레타아제(bace) 저해제로 유용한 5,6-디하이드로-2h-[1,4]옥사진-3-일-아민 유도체 |
| EA201291413A1 (ru) | 2010-06-28 | 2013-05-30 | Янссен Фармацевтика Нв | Производные 3-амино-5,6-дигидро-1h-пиразин-2-она, применимые для лечения болезни альцгеймера и других форм деменции |
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| EP2634188A4 (en) * | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
| BR112013015430A2 (pt) | 2010-12-22 | 2016-09-20 | Janssen Pharmaceutica Nv | derivados de 5,6-diidro-imidazo[1,2-a]pirazin-8-ilamina úteis como inibidores de beta-secretase (bace) |
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| JP2012147763A (ja) | 2011-01-17 | 2012-08-09 | Toshitaka Kobayashi | 乾物穿孔具 |
| US9242943B2 (en) | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| CN103415519B (zh) | 2011-03-01 | 2016-03-02 | 詹森药业有限公司 | 作为β-分泌酶(BACE)抑制剂有用的6,7-二氢-吡唑[1,5-a]吡嗪-4-基胺衍生物 |
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| CN103608345A (zh) | 2011-04-26 | 2014-02-26 | 盐野义制药株式会社 | 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂 |
| EP2766358B1 (en) | 2011-10-13 | 2016-06-22 | Novartis AG | Novel oxazine derivatives and their use in the treatment of disease |
| UA111749C2 (uk) | 2011-12-05 | 2016-06-10 | Янссен Фармацевтика Нв | Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну |
| CA2853891C (en) | 2011-12-06 | 2020-03-10 | Janssen Pharmaceutica Nv | 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives |
| AU2013363151A1 (en) | 2012-12-20 | 2015-06-04 | Merck Sharp & Dohme Corp. | C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors |
| WO2014198851A1 (en) | 2013-06-12 | 2014-12-18 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace) |
| US9751886B2 (en) | 2013-06-12 | 2017-09-05 | 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) |
| CN105283457B (zh) | 2013-06-12 | 2018-09-18 | 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]吡嗪衍生物 |
| ES2768823T3 (es) | 2014-12-18 | 2020-06-23 | Janssen Pharmaceutica Nv | Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa |
-
2014
- 2014-06-12 WO PCT/EP2014/062283 patent/WO2014198851A1/en not_active Ceased
- 2014-06-12 ES ES14732131.9T patent/ES2627633T3/es active Active
- 2014-06-12 EP EP14732131.9A patent/EP3008067B1/en active Active
- 2014-06-12 BR BR112015030498A patent/BR112015030498A2/pt active Search and Examination
- 2014-06-12 CA CA2912156A patent/CA2912156C/en active Active
- 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 KR KR1020157034929A patent/KR102243135B1/ko not_active Expired - Fee Related
- 2014-06-12 AU AU2014280122A patent/AU2014280122B2/en not_active Ceased
- 2014-06-12 US US14/897,420 patent/US9834559B2/en not_active Expired - Fee Related
- 2014-06-12 MX MX2015017151A patent/MX368326B/es active IP Right Grant
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| Publication number | Publication date |
|---|---|
| US20160115171A1 (en) | 2016-04-28 |
| AU2014280122B2 (en) | 2017-12-21 |
| AU2014280122A1 (en) | 2015-11-19 |
| BR112015030498A2 (pt) | 2017-07-25 |
| KR102243135B1 (ko) | 2021-04-22 |
| CN105452251A (zh) | 2016-03-30 |
| EA201592278A1 (ru) | 2016-09-30 |
| US9834559B2 (en) | 2017-12-05 |
| CN105452251B (zh) | 2017-12-26 |
| WO2014198851A1 (en) | 2014-12-18 |
| CA2912156A1 (en) | 2014-12-18 |
| KR20160018538A (ko) | 2016-02-17 |
| JP6387402B2 (ja) | 2018-09-05 |
| EA032662B1 (ru) | 2019-06-28 |
| MX2015017151A (es) | 2016-03-16 |
| JP2016521718A (ja) | 2016-07-25 |
| EP3008067A1 (en) | 2016-04-20 |
| ES2627633T3 (es) | 2017-07-28 |
| EP3008067B1 (en) | 2017-03-29 |
| CA2912156C (en) | 2021-07-20 |
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