BR112015030678A2 - derivados 4-amino-6-fenil-5,6-di-hidroimidazo [1,5-a] pirazina como inibidores de beta-secretase (bace) - Google Patents

derivados 4-amino-6-fenil-5,6-di-hidroimidazo [1,5-a] pirazina como inibidores de beta-secretase (bace)

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Publication number
BR112015030678A2
BR112015030678A2 BR112015030678A BR112015030678A BR112015030678A2 BR 112015030678 A2 BR112015030678 A2 BR 112015030678A2 BR 112015030678 A BR112015030678 A BR 112015030678A BR 112015030678 A BR112015030678 A BR 112015030678A BR 112015030678 A2 BR112015030678 A2 BR 112015030678A2
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Prior art keywords
beta
secretase
dementia
dihydroimidazo
bace
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BR112015030678A
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English (en)
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BR112015030678A8 (pt
Inventor
Oehlrich Daniel
Jacobus Maria Gijsen Henricus
Surkyn Michel
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Janssen Pharmaceutica Nv
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Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of BR112015030678A2 publication Critical patent/BR112015030678A2/pt
Publication of BR112015030678A8 publication Critical patent/BR112015030678A8/pt

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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
    • 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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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
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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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
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    • 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]
    • A—HUMAN NECESSITIES
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    • 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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  • Orthopedic Medicine & Surgery (AREA)
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  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

resumo patente de invenção: "derivados 4-amino-6-fenil-5,6-di-hidroimidazo [1,5-a] pirazina como inibidores de beta-secretase (bace)". a presente invenção refere-se a novos derivados 5,6-di-hidroimidazo [1,5-a] pirazinila como inibidores de beta-secretase, também conhecida como enzima de clivagem de amiloide de local beta, bace, em particular bace1 e/ou bace2 (em que bace1 também é conhecida como asp2, ou memapsina2, e bace2 também é conhecida como asp1, memapsina 1 ou drap). a invenção também é dirigida a composições farmacêuticas compreendendo tais compostos, a processos para a preparação de tais compostos e composições, e ao uso de tais compostos e composições para a prevenção e tratamento de distúrbios nos quais está envolvida a beta-secretase, como doença de alzheimer (ad), defeito cognitivo ligeiro, senilidade, demência, demência com corpos de lewy, síndrome de down, demência associada a derrame cerebral, demência associada a doença de parkinson, demência do tipo alzheimer, demência associada a beta-amiloide, degeneração macular relacionada à idade, diabetes do tipo 2 e outros distúrbios metabólicos.
BR112015030678A 2013-06-12 2014-06-12 derivados 4-amino-6-fenil-5,6-di-hidroimidazo [1,5-a] pirazina como inibidores de beta-secretase (bace), composição farmacêutica, processo para preparação da mesma, e usos na fabricação de medicamentos BR112015030678A8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13171730 2013-06-12
PCT/EP2014/062285 WO2014198853A1 (en) 2013-06-12 2014-06-12 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace)

Publications (2)

Publication Number Publication Date
BR112015030678A2 true BR112015030678A2 (pt) 2017-07-25
BR112015030678A8 BR112015030678A8 (pt) 2020-01-07

Family

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BR112015030678A BR112015030678A8 (pt) 2013-06-12 2014-06-12 derivados 4-amino-6-fenil-5,6-di-hidroimidazo [1,5-a] pirazina como inibidores de beta-secretase (bace), composição farmacêutica, processo para preparação da mesma, e usos na fabricação de medicamentos

Country Status (12)

Country Link
US (1) US9580433B2 (pt)
EP (1) EP3008066B1 (pt)
JP (1) JP6325092B2 (pt)
KR (1) KR102243134B1 (pt)
CN (1) CN105283457B (pt)
AU (1) AU2014280124B2 (pt)
BR (1) BR112015030678A8 (pt)
CA (1) CA2911690C (pt)
EA (1) EA032816B1 (pt)
ES (1) ES2697684T3 (pt)
MX (1) MX369629B (pt)
WO (1) WO2014198853A1 (pt)

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CN110312718B (zh) 2017-01-10 2023-02-28 拜耳公司 作为害虫防治剂的杂环烯衍生物

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ES2697684T3 (es) 2019-01-25
BR112015030678A8 (pt) 2020-01-07
WO2014198853A1 (en) 2014-12-18
EP3008066A1 (en) 2016-04-20
CA2911690A1 (en) 2014-12-18
EA201592277A1 (ru) 2016-09-30
US9580433B2 (en) 2017-02-28
KR102243134B1 (ko) 2021-04-22
CN105283457B (zh) 2018-09-18
US20160115170A1 (en) 2016-04-28
EA032816B1 (ru) 2019-07-31
MX369629B (es) 2019-11-14
KR20160018537A (ko) 2016-02-17
EP3008066B1 (en) 2018-08-15
CA2911690C (en) 2021-08-24
CN105283457A (zh) 2016-01-27
JP2016520659A (ja) 2016-07-14
MX2015017153A (es) 2016-03-16
AU2014280124B2 (en) 2018-11-01
AU2014280124A1 (en) 2015-11-12
JP6325092B2 (ja) 2018-05-16

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