PE20121640A1 - Derivados de pirazina como inhibidores de bace - Google Patents

Derivados de pirazina como inhibidores de bace

Info

Publication number
PE20121640A1
PE20121640A1 PE2012000897A PE2012000897A PE20121640A1 PE 20121640 A1 PE20121640 A1 PE 20121640A1 PE 2012000897 A PE2012000897 A PE 2012000897A PE 2012000897 A PE2012000897 A PE 2012000897A PE 20121640 A1 PE20121640 A1 PE 20121640A1
Authority
PE
Peru
Prior art keywords
alkyl
halogen
pyridin
tetrahydro
bromo
Prior art date
Application number
PE2012000897A
Other languages
English (en)
Inventor
Marina Tintelnot-Blomley
Siem Jacob Veenstra
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43598456&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20121640(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20121640A1 publication Critical patent/PE20121640A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61P25/28—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

REFERIDA A UN DERIVADO DE PIRAZINA DE FORMULA (I), DONDE R1 ES H, CIANO, HALOGENO, ALQUILO C1-C8, ENTRE OTROS; R2 ES ARILO, HETEROARILO, ENTRE OTROS; R3 ES H, CIANO, HALOGENO, ALQUILO C1-C8, ENTRE OTROS; R4 ES H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS; R5 ES H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS; R6 ES H, ALQUILO C1-C8, HALOALQUILO C1-C8, ENTRE OTROS; R7 ES H, ALQUILO C1-C8, HALOALQUILOC1-C8, ENTRE OTROS; E1 ES C(R8)(R9) O C(R8)(R9)-C(R10)(R11); E2 ES C(R12)(R13) O C(R12)(R13)-C(R14)(R15); R8 Y R9 SON H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS; R10 Y R11 SON H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS; R12 Y R13 SON H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS; R14 Y R15 SON H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: [3-(6-AMINO-2,4-DIMETIL-3-OXO-2,3,4,5-TETRAHIDRO-PIRAZIN-2-IL)-4-FLUORO-FENIL]-AMIDA DEL ACIDO 5-BROMO-PIRIDIN-2-CARBOXILICO, [3-(6-AMINO-2,4-DIMETIL-2,3,4,5-TETRAHIDRO-PIRAZIN-2-IL)-4-FLUORO-FENIL]-AMIDA DEL ACIDO 5-BROMO-PIRIDIN-2-CARBOXILICO,[3-(6-AMINO-2,4-DIMETIL-3-OXO-2,3,4,5-TETRAHIDRO-PIRAZIN-2-IL)-4-FENIL]-AMIDA DEL ACIDO 5-BROMO-PIRIDIN-2-CARBOXILICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE BACE Y SON UTILES EN EL TRATAMIENTO DE TRASTORNOS NEUROLOGICOS TALES COMO LA ENFERMEDAD DE ALZHEIMER
PE2012000897A 2009-12-31 2010-12-22 Derivados de pirazina como inhibidores de bace PE20121640A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US29172409P 2009-12-31 2009-12-31

Publications (1)

Publication Number Publication Date
PE20121640A1 true PE20121640A1 (es) 2012-12-17

Family

ID=43598456

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2012000897A PE20121640A1 (es) 2009-12-31 2010-12-22 Derivados de pirazina como inhibidores de bace

Country Status (27)

Country Link
US (2) US20120277244A1 (es)
EP (1) EP2519515B1 (es)
JP (1) JP5600754B2 (es)
KR (1) KR101419157B1 (es)
CN (1) CN102712621B (es)
AU (1) AU2010338365B2 (es)
BR (1) BR112012015916A2 (es)
CA (1) CA2785341A1 (es)
CL (1) CL2012001762A1 (es)
CR (1) CR20120332A (es)
CU (1) CU20120099A7 (es)
EA (1) EA201200952A1 (es)
EC (1) ECSP12012065A (es)
ES (1) ES2445536T3 (es)
GT (1) GT201200219A (es)
HK (1) HK1172023A1 (es)
HN (1) HN2012001413A (es)
IL (1) IL220268A0 (es)
MX (1) MX2012007754A (es)
NZ (1) NZ600136A (es)
PE (1) PE20121640A1 (es)
PL (1) PL2519515T3 (es)
PT (1) PT2519515E (es)
SG (1) SG181431A1 (es)
TN (1) TN2012000249A1 (es)
WO (1) WO2011080176A1 (es)
ZA (1) ZA201203614B (es)

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JP5853033B2 (ja) 2011-03-01 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６，７−ジヒドロ−ピラゾロ［１，５−ａ］ピラジン−４−イルアミン誘導体
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
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EA028775B1 (ru) 2013-06-12 2017-12-29 Янссен Фармацевтика Нв Производные 4-амино-6-фенил-6,7-дигидро[1,2,3]триазоло[1,5-a]пиразина в качестве ингибиторов бета-секретазы (bace)
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Also Published As

Publication number Publication date
JP5600754B2 (ja) 2014-10-01
AU2010338365A1 (en) 2012-06-07
GT201200219A (es) 2013-10-10
HK1172023A1 (en) 2013-04-12
NZ600136A (en) 2013-09-27
JP2013516395A (ja) 2013-05-13
EP2519515B1 (en) 2013-11-06
IL220268A0 (en) 2012-07-31
ECSP12012065A (es) 2012-08-31
SG181431A1 (en) 2012-07-30
WO2011080176A1 (en) 2011-07-07
AU2010338365B2 (en) 2014-01-30
BR112012015916A2 (pt) 2017-04-25
PL2519515T3 (pl) 2014-04-30
KR101419157B1 (ko) 2014-07-11
CL2012001762A1 (es) 2012-12-21
TN2012000249A1 (en) 2013-12-12
CN102712621A (zh) 2012-10-03
HN2012001413A (es) 2015-03-23
MX2012007754A (es) 2012-08-01
CU20120099A7 (es) 2012-07-31
ZA201203614B (en) 2013-01-30
CR20120332A (es) 2012-07-12
EP2519515A1 (en) 2012-11-07
PT2519515E (pt) 2014-02-17
US20150322038A1 (en) 2015-11-12
KR20120102795A (ko) 2012-09-18
ES2445536T3 (es) 2014-03-03
US20120277244A1 (en) 2012-11-01
CN102712621B (zh) 2015-03-11
EA201200952A1 (ru) 2013-02-28
CA2785341A1 (en) 2011-07-07

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