PE20090953A1 - Sulfonas ciclicas sustituidas por amino-bencilo utiles como inhibidores de bace - Google Patents

Sulfonas ciclicas sustituidas por amino-bencilo utiles como inhibidores de bace

Info

Publication number
PE20090953A1
PE20090953A1 PE2008001440A PE2008001440A PE20090953A1 PE 20090953 A1 PE20090953 A1 PE 20090953A1 PE 2008001440 A PE2008001440 A PE 2008001440A PE 2008001440 A PE2008001440 A PE 2008001440A PE 20090953 A1 PE20090953 A1 PE 20090953A1
Authority
PE
Peru
Prior art keywords
alkyl
amino
benzyl
halo
halogen
Prior art date
Application number
PE2008001440A
Other languages
English (en)
Inventor
Emmanuelle Briard
Rainer Martin Lueoend
Rainer Machauer
Henrik Moebitz
Olivier Rogel
Jean-Michel Rondeau
Heinrich Rueeger
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
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20090953A1 publication Critical patent/PE20090953A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D335/00Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/02Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)

Abstract

REFRIDA A UN DERIVADO SULFONA DE FORMULA (I), DONDE R1 ES H, HALOGENO, ALQUILO C1-C8; R2 ES H, HALOGENO, ALQUILO C1-C8, HALO-ALQUILO C1-C8, ENTRE OTROS; R3 ES H, HALO-ALQUILO C1-C8, HIDROXI-ALQUILO C1-C8, ENTRE OTROS; R4 ES H, ALQUILO C1-C8, FORMILO, ENTRE OTROS; R5 ES H, HALOGENO, ALQUILO C1-C8, ALQUENILO C2-C8, ENTRE OTROS; R6 ES OXO O ESTA AUSENTE; R7 ESTA AUSENTE O ES OXO, IMINO, BENCIL-IMINO, FORMIL-IMINO, ENTRE OTROS; R8 ES H, ALQUILO C1-C8, HIDROXI-ALQUILO C1-C8, HALO-ALQUILO C1-C8, ENTRE OTROS; R9 ES H, ALQUILO C1-C8, HALO-ALQUILO C1-C8, ENTRE OTROS; R10 ES UN GRUPO ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDO CON HALOGENO, OH, ALQUILO C1-C8, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: CLORHIDRATO DE (3S*,4S*,5R*)-3-(4-AMINO-3-FLUORO-BENCIL)-5-(3-TERBUTIL-BENCIL-AMINO)-1,1-DIOXO-HEXAHIDRO-1LAMBDA*6*-TIOPIRAN-4-OL, (3S,4S,5R)-3-(4-AMINO-3-BROMO-5-FLUORO-BENCIL)-5-[3-(1,1-DIFLUORO-ETIL)-BENCIL-AMINO]-1,1-DIOXO-HEXAHIDRO-1LAMBDA*6*-TIOPIRAN-4-OL, (3S,4S,5R)-3-(4-AMINO-3-BROMO-5-FLUORO-BENCIL)-5-[3-(2,2-DIMETIL-PROPIL)-BENCIL-AMINO]-1,1-DIOXO-HEXAHIDRO-1LAMBDA*6*-TIOPIRAN-4-OL, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE BACE Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES NEURODEGENERATIVAS, TRANSTORNOS NEUROLOGICOS, ENTRE OTRAS
PE2008001440A 2007-08-23 2008-08-25 Sulfonas ciclicas sustituidas por amino-bencilo utiles como inhibidores de bace PE20090953A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07114881 2007-08-23
EP08160123 2008-07-10

Publications (1)

Publication Number Publication Date
PE20090953A1 true PE20090953A1 (es) 2009-08-10

Family

ID=39789883

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008001440A PE20090953A1 (es) 2007-08-23 2008-08-25 Sulfonas ciclicas sustituidas por amino-bencilo utiles como inhibidores de bace

Country Status (15)

Country Link
US (1) US20090054427A1 (es)
EP (1) EP2190833A1 (es)
JP (1) JP2010536831A (es)
KR (1) KR20100061805A (es)
CN (1) CN101835771A (es)
AR (1) AR068062A1 (es)
AU (1) AU2008290561A1 (es)
BR (1) BRPI0815673A2 (es)
CA (1) CA2697254A1 (es)
CL (1) CL2008002480A1 (es)
EA (1) EA201000340A1 (es)
MX (1) MX2010002007A (es)
PE (1) PE20090953A1 (es)
TW (1) TW200916097A (es)
WO (1) WO2009024615A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2011000390A (es) * 2008-07-10 2011-03-01 Novartis Ag Sulfonas ciclicas con sustitucion de amino-bencilo utiles coimo inhibidores de bace.
US9066948B2 (en) 2010-07-16 2015-06-30 The United States Of America As Represented By The Secretary, Department Of Health And Human Services Oxadiazolo[3,2-a]pyrimidines and thiadiazolo[3,2-a]pyrimidines
US9242943B2 (en) * 2011-01-18 2016-01-26 Siena Biotech S.P.A. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
WO2013109632A2 (en) 2012-01-16 2013-07-25 The Rockefeller University Organic compounds
CA2899938C (en) 2013-02-12 2021-10-19 Buck Institute For Research On Aging Hydantoins that modulate bace-mediated app processing
CN106674264A (zh) * 2016-12-20 2017-05-17 苏州汉德创宏生化科技有限公司 (2,2,2‑三氟乙氧基)苯硼酸类化合物的合成方法
WO2019246085A1 (en) * 2018-06-19 2019-12-26 Celecor Therapeutics, Inc. Deuterated ruc-4

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA001534B1 (ru) * 1996-02-07 2001-04-23 Варнер-Ламберт Компани Производные циклической аминокислоты или их фармацевтически приемлемые соли, фармацевтическая композиция и способ лечения депрессии, состояний паники, страха и болевых ощущений
PL341231A1 (en) * 1997-12-16 2001-03-26 Warner Lambert Co 4(3)-substitute derivatives of 4(3)aminomethyl(thio)pyrane or piperidine derivatives (analogues of garbapentin), their production and application in treating neurological disorders
GB0602951D0 (en) * 2006-02-14 2006-03-29 Novartis Ag Organic Compounds

Also Published As

Publication number Publication date
KR20100061805A (ko) 2010-06-09
EA201000340A1 (ru) 2010-08-30
JP2010536831A (ja) 2010-12-02
MX2010002007A (es) 2010-03-10
US20090054427A1 (en) 2009-02-26
TW200916097A (en) 2009-04-16
CA2697254A1 (en) 2009-02-26
CL2008002480A1 (es) 2009-05-15
AR068062A1 (es) 2009-11-04
BRPI0815673A2 (pt) 2015-02-18
EP2190833A1 (en) 2010-06-02
AU2008290561A1 (en) 2009-02-26
CN101835771A (zh) 2010-09-15
WO2009024615A1 (en) 2009-02-26

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