MX366063B - Derivados de 4-amino-6-fenil-6,7-dihidro[1,2,3]triazolo[1,5-a]pira zina como inhibidores de beta-secretasa (bace). - Google Patents
Derivados de 4-amino-6-fenil-6,7-dihidro[1,2,3]triazolo[1,5-a]pira zina como inhibidores de beta-secretasa (bace).Info
- Publication number
- MX366063B MX366063B MX2015017155A MX2015017155A MX366063B MX 366063 B MX366063 B MX 366063B MX 2015017155 A MX2015017155 A MX 2015017155A MX 2015017155 A MX2015017155 A MX 2015017155A MX 366063 B MX366063 B MX 366063B
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- Prior art keywords
- beta
- dementia
- secretase
- bace
- triazolo
- Prior art date
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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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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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- 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
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- A61P17/00—Drugs for dermatological disorders
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- 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
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- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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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
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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
- A61P25/08—Antiepileptics; Anticonvulsants
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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
- A61P25/14—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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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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
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- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Psychology (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Transplantation (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente invención se refiere a derivados novedosos de 6,7- dihidro[1,2,3]triazolo[1,5-a]pirazin-6-ilo bncomo 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, Memapsina 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 |
---|---|---|---|
EP13171720 | 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 |
---|---|
MX2015017155A MX2015017155A (es) | 2016-03-16 |
MX366063B true MX366063B (es) | 2019-06-26 |
Family
ID=48577637
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2015017155A MX366063B (es) | 2013-06-12 | 2014-06-12 | Derivados de 4-amino-6-fenil-6,7-dihidro[1,2,3]triazolo[1,5-a]pira zina como inhibidores de beta-secretasa (bace). |
Country Status (12)
Country | Link |
---|---|
US (1) | US9751886B2 (es) |
EP (1) | EP3008065B1 (es) |
JP (1) | JP6435321B2 (es) |
KR (1) | KR102243133B1 (es) |
CN (1) | CN105324383B (es) |
AU (1) | AU2014280125B2 (es) |
BR (1) | BR112015030597A2 (es) |
CA (1) | CA2911693C (es) |
EA (1) | EA028775B1 (es) |
ES (1) | ES2721073T3 (es) |
MX (1) | MX366063B (es) |
WO (1) | WO2014198854A1 (es) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2799640C (en) | 2010-06-09 | 2018-10-16 | Janssen Pharmaceutica Nv | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
ES2648143T3 (es) | 2010-12-22 | 2017-12-28 | Janssen Pharmaceutica Nv | Derivados de 5,6-dihidro-imidazo[1,2-a]pirazin-8-ilamina útiles como inhibidores de la beta-secretasa (BACE) |
JP5853035B2 (ja) | 2011-03-09 | 2016-02-09 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap | β−セクレターゼ(BACE)の阻害剤として有用な3,4−ジヒドロ−ピロロ[1,2−a]ピラジン−1−イルアミン誘導体 |
US9580433B2 (en) | 2013-06-12 | 2017-02-28 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-A]pyrazine derivatives as inhibitors of beta-secretase (BACE) |
MX368326B (es) | 2013-06-12 | 2019-09-27 | Janssen Pharmaceutica Nv | Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]pirazin-3(2h )-ona como inhibidores de beta-secretasa (bace). |
WO2016083425A1 (en) * | 2014-11-28 | 2016-06-02 | F. Hoffmann-La Roche Ag | Peptides |
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 |
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US9580433B2 (en) | 2013-06-12 | 2017-02-28 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-A]pyrazine derivatives as inhibitors of beta-secretase (BACE) |
MX368326B (es) | 2013-06-12 | 2019-09-27 | Janssen Pharmaceutica Nv | Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]pirazin-3(2h )-ona como inhibidores de beta-secretasa (bace). |
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 |
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2014
- 2014-06-12 BR BR112015030597A patent/BR112015030597A2/pt active Search and Examination
- 2014-06-12 EA EA201592307A patent/EA028775B1/ru not_active IP Right Cessation
- 2014-06-12 US US14/897,396 patent/US9751886B2/en active Active
- 2014-06-12 CN CN201480033508.XA patent/CN105324383B/zh active Active
- 2014-06-12 KR KR1020157034908A patent/KR102243133B1/ko active IP Right Grant
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US20160130274A1 (en) | 2016-05-12 |
JP6435321B2 (ja) | 2018-12-05 |
US9751886B2 (en) | 2017-09-05 |
AU2014280125A1 (en) | 2015-11-12 |
BR112015030597A2 (pt) | 2017-07-25 |
KR102243133B1 (ko) | 2021-04-22 |
MX2015017155A (es) | 2016-03-16 |
EP3008065B1 (en) | 2019-01-30 |
AU2014280125B2 (en) | 2018-03-15 |
WO2014198854A1 (en) | 2014-12-18 |
EA028775B1 (ru) | 2017-12-29 |
JP2016520660A (ja) | 2016-07-14 |
CN105324383A (zh) | 2016-02-10 |
CN105324383B (zh) | 2017-10-31 |
CA2911693C (en) | 2021-08-24 |
EP3008065A1 (en) | 2016-04-20 |
CA2911693A1 (en) | 2014-12-18 |
ES2721073T3 (es) | 2019-07-26 |
KR20160019893A (ko) | 2016-02-22 |
EA201592307A1 (ru) | 2016-04-29 |
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