PE20130317A1 - Derivados de amino-tropano - Google Patents

Derivados de amino-tropano

Info

Publication number
PE20130317A1
PE20130317A1 PE2012002444A PE2012002444A PE20130317A1 PE 20130317 A1 PE20130317 A1 PE 20130317A1 PE 2012002444 A PE2012002444 A PE 2012002444A PE 2012002444 A PE2012002444 A PE 2012002444A PE 20130317 A1 PE20130317 A1 PE 20130317A1
Authority
PE
Peru
Prior art keywords
methyl
aza
benzamide
bicycle
trifluoromethyl
Prior art date
Application number
PE2012002444A
Other languages
English (en)
Inventor
Sabine Kolczewski
Emmanuel Pinard
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20130317A1 publication Critical patent/PE20130317A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/468-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular 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
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE AMINO-TROPANO DE FORMULA (I) DONDE R1, R2 Y R3 SON CADA UNO H, ALQUILO INFERIOR OPCIONALMENTE SUSTITUIDO CON HALOGENO, ALCOXI INFERIOR, CICLOALQUILO O S-ALQUILO INFERIOR. SON COMPUESTOS PREFERIDOS: 2-METOXI-N-((1S,2S,5R)-8-METIL-2-FENIL-8-AZA-BICICLO[3.2.1]OCT-2-IL)-6-METILSULFANIL-4-TRIFLUOROMETIL-BENZAMIDA; 2-CICLOPROPIL-N-((1RS,2RS,5SR)-8-METIL-2-FENIL-8-AZA-BICICLO[3.2.1]OCT-2-IL)-4-TRIFLUOROMETIL-BENZAMIDA; 2-METOXI-6-METIL-N-((1RS,2RS,5SR)-8-METIL-2-FENIL-8-AZA-BICICLO[3.2.1]OCT-2-IL)-4-TRIFLUOROMETIL-BENZAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DEL TRANSPORTADOR DE GLICINA 1 (GlyT-1) SIENDO UTILES EN EL TRATAMIENTO DE ESQUIZOFRENIA, TRASTORNOS DE DEMENCIA, ENFERMEDAD DE ALZHEIMER
PE2012002444A 2010-06-22 2011-06-17 Derivados de amino-tropano PE20130317A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10166757 2010-06-22

Publications (1)

Publication Number Publication Date
PE20130317A1 true PE20130317A1 (es) 2013-03-11

Family

ID=44310862

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2012002444A PE20130317A1 (es) 2010-06-22 2011-06-17 Derivados de amino-tropano

Country Status (24)

Country Link
US (1) US8153653B2 (es)
EP (1) EP2585456B1 (es)
JP (1) JP5546684B2 (es)
KR (1) KR101445016B1 (es)
CN (1) CN102947297B (es)
AR (1) AR081961A1 (es)
AU (1) AU2011269145A1 (es)
BR (1) BR112012032576A2 (es)
CA (1) CA2801458C (es)
CL (1) CL2012003552A1 (es)
CO (1) CO6630160A2 (es)
CR (1) CR20120614A (es)
EA (1) EA201291374A1 (es)
EC (1) ECSP12012347A (es)
ES (1) ES2550831T3 (es)
HK (1) HK1179606A1 (es)
IL (1) IL222998A0 (es)
MA (1) MA34251B1 (es)
MX (1) MX2012013820A (es)
PE (1) PE20130317A1 (es)
SG (1) SG186329A1 (es)
TW (1) TWI417097B (es)
WO (1) WO2011161006A1 (es)
ZA (1) ZA201209248B (es)

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EE04751B1 (et) * 1996-02-22 2006-12-15 Neurosearch A/S Tropaani derivaadid, nende valmistamine ja kasutamine
US5834484A (en) * 1997-03-12 1998-11-10 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Cocaine analogs
JP4563386B2 (ja) * 2003-09-09 2010-10-13 エフ.ホフマン−ラ ロシュ アーゲー 精神病の処置のためのグリシン取り込み阻害剤としての1−(2−アミノ−ベンゾール)−ピペラジン誘導体
FR2861076B1 (fr) 2003-10-17 2006-01-06 Sanofi Synthelabo Derives de n-heterocyclymethylbenzamide, leur preparation et leur application en therapeutique
US7572792B2 (en) * 2004-04-29 2009-08-11 Merck & Co., Inc. Azetidine glycine transporter inhibitors
FR2873693B1 (fr) * 2004-07-29 2006-09-15 Sanofi Synthelabo Derives d'amino-tropane, leur preparation et leur application en therapeutique
GB0428231D0 (en) * 2004-12-23 2005-01-26 Glaxo Group Ltd Compounds
MX2007008190A (es) * 2005-01-06 2007-08-07 Hoffmann La Roche Fenil metanonas sustituidas con sulfanilo como inhibidores del transportador de glicina 1 (glyt-1) para el tratamiento de trastornos neurologicos y neuropsiquiatricos.
EP2121622A1 (en) * 2007-02-01 2009-11-25 Glaxo Group Limited Glyt1 transporter inhibitors and uses thereof in treatment of neurological and neuropsychiatric disorders
WO2010020548A1 (en) * 2008-08-20 2010-02-25 F. Hoffmann-La Roche Ag Glyt1 receptor antagonists

Also Published As

Publication number Publication date
MX2012013820A (es) 2013-01-28
CO6630160A2 (es) 2013-03-01
JP5546684B2 (ja) 2014-07-09
EP2585456B1 (en) 2015-09-16
CL2012003552A1 (es) 2013-04-12
BR112012032576A2 (pt) 2016-11-22
CN102947297A (zh) 2013-02-27
MA34251B1 (fr) 2013-05-02
ECSP12012347A (es) 2013-01-31
EP2585456A1 (en) 2013-05-01
US8153653B2 (en) 2012-04-10
CA2801458C (en) 2018-10-30
CN102947297B (zh) 2015-12-16
ES2550831T3 (es) 2015-11-12
US20110312993A1 (en) 2011-12-22
AR081961A1 (es) 2012-10-31
KR101445016B1 (ko) 2014-09-26
TW201206438A (en) 2012-02-16
EA201291374A1 (ru) 2013-06-28
JP2013529607A (ja) 2013-07-22
SG186329A1 (en) 2013-01-30
IL222998A0 (en) 2013-02-03
AU2011269145A1 (en) 2012-11-08
KR20130029414A (ko) 2013-03-22
TWI417097B (zh) 2013-12-01
WO2011161006A1 (en) 2011-12-29
CR20120614A (es) 2013-01-11
HK1179606A1 (zh) 2013-10-04
ZA201209248B (en) 2013-08-28
CA2801458A1 (en) 2011-12-29

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