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ECSP11010882A - Derivados de piperazina que se unen a las placas amiloides para obtener imágenes de las mismas y su uso - Google Patents

Derivados de piperazina que se unen a las placas amiloides para obtener imágenes de las mismas y su uso

Info

Publication number
ECSP11010882A
ECSP11010882A EC2011010882A ECSP11010882A ECSP11010882A EC SP11010882 A ECSP11010882 A EC SP11010882A EC 2011010882 A EC2011010882 A EC 2011010882A EC SP11010882 A ECSP11010882 A EC SP11010882A EC SP11010882 A ECSP11010882 A EC SP11010882A
Authority
EC
Ecuador
Prior art keywords
amiloid
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Prior art date
Application number
EC2011010882A
Other languages
English (en)
Inventor
Ulf Bomer
Matthias Friebe
Lutz Lehmann
Andrea Thiele
Tobias Heinrich
Heribert Schmitt-Willich
Ulrike Rohn
Ansgar Fitzner
Sabine Krause
Damian Brockschnieder
Thomas Dyrks
Original Assignee
Bayer Schering Pharma A G
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=40289401&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ECSP11010882(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Schering Pharma A G filed Critical Bayer Schering Pharma A G
Publication of ECSP11010882A publication Critical patent/ECSP11010882A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/24Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/185Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La invención se relaciona con compuestos de fórmula I, su síntesis y su uso, en particular para la detección de depósitos amiloides en un paciente.
EC2011010882A 2008-09-12 2011-03-11 Derivados de piperazina que se unen a las placas amiloides para obtener imágenes de las mismas y su uso ECSP11010882A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08164279A EP2163541A1 (en) 2008-09-12 2008-09-12 Piperazine derivatives for binding and imaging amyloid plaques and their use

Publications (1)

Publication Number Publication Date
ECSP11010882A true ECSP11010882A (es) 2011-04-29

Family

ID=40289401

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2011010882A ECSP11010882A (es) 2008-09-12 2011-03-11 Derivados de piperazina que se unen a las placas amiloides para obtener imágenes de las mismas y su uso

Country Status (23)

Country Link
US (1) US20110250135A1 (es)
EP (2) EP2163541A1 (es)
JP (1) JP2012502070A (es)
KR (1) KR20110069005A (es)
CN (1) CN102149681A (es)
AR (1) AR075079A1 (es)
AU (1) AU2009291251A1 (es)
BR (1) BRPI0918442A2 (es)
CA (1) CA2736530A1 (es)
CL (1) CL2011000520A1 (es)
CO (1) CO6341559A2 (es)
CR (1) CR20110133A (es)
DO (1) DOP2011000078A (es)
EA (1) EA201100448A1 (es)
EC (1) ECSP11010882A (es)
IL (1) IL211212A0 (es)
MX (1) MX2011002724A (es)
PE (1) PE20110795A1 (es)
SV (1) SV2011003854A (es)
TW (1) TW201014843A (es)
UY (1) UY32112A (es)
WO (1) WO2010028776A1 (es)
ZA (1) ZA201102689B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201201846A (en) * 2010-02-08 2012-01-16 Bayer Schering Pharma Ag Iodo precursor for a PET imaging agent of amyloid plaques
WO2011110511A1 (en) * 2010-03-11 2011-09-15 Bayer Pharma Aktiengesellschaft Spect imaging agents of amyloid plaques
CN103724207B (zh) * 2013-12-20 2016-07-06 北京智博高科生物技术有限公司 苯基苄基醚类衍生物及其制备方法和应用
AU2016340237A1 (en) 2015-10-14 2018-05-31 Bristol-Myers Squibb Company Selective NR2B antagonists
US10703711B2 (en) 2017-11-06 2020-07-07 Acelot, Inc. Small molecule drugs and related methods for treatment of diseases related to Aβ42 oligomer formation
CN107989600B (zh) * 2017-12-13 2023-09-12 捷贝通石油技术集团股份有限公司 一种水基痕量化学示踪剂及用于测量注水井井间连通性的方法
CN111511732A (zh) * 2017-12-21 2020-08-07 豪夫迈·罗氏有限公司 放射性标记化合物

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6387900B1 (en) * 1999-08-12 2002-05-14 Pharmacia & Upjohn S.P.A. 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents
UY27003A1 (es) * 2000-11-06 2002-07-31 Schering Ag Productos radiofarmacéuticos para el diagnóstico de la enfermedad de alzheimer
EP1411052B1 (en) * 2001-07-05 2011-10-05 Takeda Pharmaceutical Company Limited Benzo-fused 5-membered hetrocycle compounds,process for preparation of the same, and use thereof
TWI289141B (en) * 2003-03-11 2007-11-01 Hoffmann La Roche F. Ag. Quinolinone derivatives and uses thereof
JP2006056884A (ja) * 2004-07-23 2006-03-02 Tanabe Seiyaku Co Ltd 医薬組成物
TW200804347A (en) * 2006-01-10 2008-01-16 Janssen Pharmaceutica Nv Urotensin II receptor antagonists
GB0623258D0 (en) * 2006-11-22 2007-01-03 Remynd Nv Thiadiazole derivatives for the treatment of neuro-degenerative diseases

Also Published As

Publication number Publication date
IL211212A0 (en) 2011-04-28
BRPI0918442A2 (pt) 2015-11-24
PE20110795A1 (es) 2011-10-30
WO2010028776A8 (en) 2011-03-17
DOP2011000078A (es) 2011-04-30
US20110250135A1 (en) 2011-10-13
CL2011000520A1 (es) 2011-07-08
AR075079A1 (es) 2011-03-09
WO2010028776A1 (en) 2010-03-18
CO6341559A2 (es) 2011-11-21
EP2350000A1 (en) 2011-08-03
JP2012502070A (ja) 2012-01-26
UY32112A (es) 2010-04-30
AU2009291251A1 (en) 2010-03-18
TW201014843A (en) 2010-04-16
CR20110133A (es) 2011-04-28
EA201100448A1 (ru) 2011-10-31
KR20110069005A (ko) 2011-06-22
SV2011003854A (es) 2011-07-27
EP2163541A1 (en) 2010-03-17
AU2009291251A8 (en) 2011-05-12
MX2011002724A (es) 2011-04-11
ZA201102689B (en) 2013-09-25
CN102149681A (zh) 2011-08-10
CA2736530A1 (en) 2010-03-18

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