MX2013003246A - Derivados de 4, 7-dihidro-pirazolo [1, 5-a] pirazin-6-ilamina utiles como inhibidores de beta-secretasa (bace). - Google Patents

Derivados de 4, 7-dihidro-pirazolo [1, 5-a] pirazin-6-ilamina utiles como inhibidores de beta-secretasa (bace).

Info

Publication number
MX2013003246A
MX2013003246A MX2013003246A MX2013003246A MX2013003246A MX 2013003246 A MX2013003246 A MX 2013003246A MX 2013003246 A MX2013003246 A MX 2013003246A MX 2013003246 A MX2013003246 A MX 2013003246A MX 2013003246 A MX2013003246 A MX 2013003246A
Authority
MX
Mexico
Prior art keywords
beta
dementia
bace
secretase
pyrazin
Prior art date
Application number
MX2013003246A
Other languages
English (en)
Inventor
Andres Avelino Trabanco-Suarez
Francisca Delgado-Jimenez
Gary John Tresadern
Original Assignee
Janssen Pharmaceutica Nv
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
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of MX2013003246A publication Critical patent/MX2013003246A/es

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Classifications

    • 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
    • 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

Landscapes

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

Abstract

La presente invención se refiere a derivados novedosos de 4, 7-dihidro-pirazolo[1 ,5-a]pirazin-6-il-amina como inhibidores de beta-secretasa, también conocida como la enzima de corte de amiloide en el sitio beta, BACE, BACE1, Asp2 o memapsin2; la invención también está dirigida a composiciones farmacéuticas que comprenden estos compuestos, a procedimientos para preparar estos compuestos y composiciones, y al uso de estos compuestos y composiciones para la prevención y tratamiento de trastornos en los que está implicada la beta-secretasa, tales como la enfermedad de Alzheimer (AD), deterioro cognitivo leve, senilidad, demencia, demencia con cuerpos de Lewy, síndrome de Down, demencia asociada con derrame cerebral, demencia asociada con enfermedad de Parkinson o demencia asociada con beta-amiloide.
MX2013003246A 2010-09-22 2011-09-20 Derivados de 4, 7-dihidro-pirazolo [1, 5-a] pirazin-6-ilamina utiles como inhibidores de beta-secretasa (bace). MX2013003246A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10178315 2010-09-22
EP11157858 2011-03-11
PCT/EP2011/066343 WO2012038438A1 (en) 2010-09-22 2011-09-20 4,7-DIHYDRO-PYRAZOLO[1,5-a]PYRAZIN-6-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)

Publications (1)

Publication Number Publication Date
MX2013003246A true MX2013003246A (es) 2013-05-22

Family

ID=45873470

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2013003246A MX2013003246A (es) 2010-09-22 2011-09-20 Derivados de 4, 7-dihidro-pirazolo [1, 5-a] pirazin-6-ilamina utiles como inhibidores de beta-secretasa (bace).

Country Status (21)

Country Link
US (1) US8609660B2 (es)
EP (1) EP2619207B1 (es)
JP (1) JP5797756B2 (es)
KR (1) KR101962216B1 (es)
CN (1) CN103097389B (es)
AU (1) AU2011306941B2 (es)
BR (1) BR112013006353A2 (es)
CA (1) CA2807904C (es)
CL (1) CL2013000782A1 (es)
CO (1) CO6660450A2 (es)
EA (1) EA021723B1 (es)
ES (1) ES2529641T3 (es)
HK (1) HK1182391A1 (es)
IL (1) IL225349A (es)
IN (1) IN2013MN00782A (es)
MX (1) MX2013003246A (es)
MY (1) MY160138A (es)
NZ (1) NZ606848A (es)
SG (1) SG188338A1 (es)
WO (1) WO2012038438A1 (es)
ZA (1) ZA201302128B (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2612854B1 (en) 2005-10-25 2015-04-29 Shionogi&Co., Ltd. Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors
JP5383483B2 (ja) 2007-04-24 2014-01-08 塩野義製薬株式会社 アルツハイマー症治療用医薬組成物
TW200902526A (en) 2007-04-24 2009-01-16 Shionogi & Amp Co Ltd Aminodihydrothiazin derivative substituted with a cyclic group
NZ589590A (en) 2008-06-13 2012-05-25 Shionogi & Co Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
JPWO2010047372A1 (ja) 2008-10-22 2012-03-22 塩野義製薬株式会社 Ｂａｃｅ１阻害活性を有する２−アミノピリミジン−４−オンおよび２−アミノピリジン誘導体
US8999980B2 (en) 2009-12-11 2015-04-07 Shionogi & Co., Ltd. Oxazine derivatives
TWI537263B (zh) 2010-06-09 2016-06-11 健生藥品公司 使用作為β－分泌酶抑制劑之５，６－二氫－２Ｈ－［１，４］－３－基－胺衍生物
EP2634186A4 (en) 2010-10-29 2014-03-26 Shionogi & Co naphthyridine
US9018219B2 (en) 2010-10-29 2015-04-28 Shionogi & Co., Ltd. Fused aminodihydropyrimidine derivative
AU2011347377B2 (en) 2010-12-22 2016-03-03 Janssen Pharmaceutica Nv 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (BACE)
SG193342A1 (en) 2011-03-09 2013-10-30 Janssen Pharmaceutica Nv 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
WO2012147763A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤
KR102082016B1 (ko) 2011-06-27 2020-02-26 에자이 알앤드디 매니지먼트 가부시키가이샤 알츠하이머병을 나타내는 마이크로rna 바이오마커들
JP2016501827A (ja) 2012-10-24 2016-01-21 塩野義製薬株式会社 Ｂａｃｅ１阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体
EP3008066B1 (en) 2013-06-12 2018-08-15 Janssen Pharmaceutica N.V. 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine 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)
EA032662B1 (ru) 2013-06-12 2019-06-28 Янссен Фармацевтика Нв ПРОИЗВОДНЫЕ 4-АМИНО-6-ФЕНИЛ-5,6-ДИГИДРОИМИДАЗО[1,5-а]ПИРАЗИН-3(2H)-ОНА В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (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
WO2018165520A1 (en) 2017-03-10 2018-09-13 Vps-3, Inc. Metalloenzyme inhibitor compounds
WO2019025250A1 (en) 2017-08-04 2019-02-07 Basf Se SUBSTITUTED TRIFLUOROMETHYLOXADIAZOLES FOR COMBATING PHYTOPATHOGENIC FUNGI
CN108440320A (zh) * 2018-05-09 2018-08-24 上海凌凯医药科技有限公司 一种高手性选择性合成α-双取代α-氨基酸的方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003297431A1 (en) * 2002-12-20 2004-07-22 Pharmacia Corporation Mitogen activated protein kinase-activated protein kinase-2 inhibiting compounds
KR20080028881A (ko) * 2005-06-14 2008-04-02 쉐링 코포레이션 헤테로사이클릭 아스파르틸 프로테아제 억제제, 이의제조방법 및 용도
TW200804290A (en) * 2005-11-15 2008-01-16 Astrazeneca Ab Compounds and uses thereof
WO2011002409A1 (en) * 2009-07-02 2011-01-06 Astrazeneca Ab 5h-pyrrolo[3,4-£>]pyrazin-7-amine derivatives inhibitors of beta-secretase

Also Published As

Publication number Publication date
IN2013MN00782A (es) 2015-06-12
BR112013006353A2 (pt) 2024-01-16
EA201390419A1 (ru) 2013-07-30
NZ606848A (en) 2015-01-30
CL2013000782A1 (es) 2013-08-09
ZA201302128B (en) 2014-08-27
JP5797756B2 (ja) 2015-10-21
IL225349A0 (en) 2013-06-27
CA2807904C (en) 2018-09-11
AU2011306941A1 (en) 2013-02-28
MY160138A (en) 2017-02-28
CA2807904A1 (en) 2012-03-29
HK1182391A1 (zh) 2013-11-29
WO2012038438A1 (en) 2012-03-29
CN103097389B (zh) 2015-10-14
EP2619207B1 (en) 2014-11-12
JP2013540740A (ja) 2013-11-07
IL225349A (en) 2016-07-31
US8609660B2 (en) 2013-12-17
KR101962216B1 (ko) 2019-03-26
CO6660450A2 (es) 2013-04-30
SG188338A1 (en) 2013-04-30
CN103097389A (zh) 2013-05-08
US20130190318A1 (en) 2013-07-25
EA021723B1 (ru) 2015-08-31
AU2011306941B2 (en) 2014-06-12
EP2619207A1 (en) 2013-07-31
ES2529641T3 (es) 2015-02-24
KR20130110161A (ko) 2013-10-08

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