BRPI0606730A2 - derivados de fenil metanona 2,5-di-substituìdos como inibidores do transportador de glicina 1 (glyt-1) para o tratamento de distúbios neurológicos e neuropsiquiátricos - Google Patents

derivados de fenil metanona 2,5-di-substituìdos como inibidores do transportador de glicina 1 (glyt-1) para o tratamento de distúbios neurológicos e neuropsiquiátricos

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Publication number
BRPI0606730A2
BRPI0606730A2 BRPI0606730-1A BRPI0606730A BRPI0606730A2 BR PI0606730 A2 BRPI0606730 A2 BR PI0606730A2 BR PI0606730 A BRPI0606730 A BR PI0606730A BR PI0606730 A2 BRPI0606730 A2 BR PI0606730A2
Authority
BR
Brazil
Prior art keywords
glyt
treatment
inhibitors
neurological
glycine transporter
Prior art date
Application number
BRPI0606730-1A
Other languages
English (en)
Inventor
Synese Jolidon
Roger David Norcross
Emmanuel Pinard
Robert Narquizian
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 BRPI0606730A2 publication Critical patent/BRPI0606730A2/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/12Oxygen or sulfur atoms
    • 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
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • 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
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/46Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • 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
    • C07D401/12Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

DERIVADOS DE FENIL METANONA 2,5-DISUBSTITUìDOS COMO INIBIDORES DO TRANSPORTADOR DE GLICINA 1 (GLYT-1) PARA O TRATAMENTO DE DISTúBIOS NEUROLóGICOS E NEUROPSIQUIáTRICOS. A presente invenção se refere a compostos da fórmula geral em que R¹ é - 0R¹', -SR¹' ou é um grupo heterocicloalquila; R¹' é alquila inferior, alquila inferior substituído por halogênio, ou é - (CH2 22)2 n2-cicIoalquiIa; R² é - S(O)2 22-alquila inferior ou - S(O)2 22NH-alquila inferior; R³ é arila ou heteroarila, os quais são não-substituidas ou substituidos por um a três substituintes, selecionados do grupo consistindo em alquila inferior, alcóxi inferior, CN, NO2 22, -C(O)-alquila inferior, -0(0)0-alquila inferior, halogênio ou alquila inferior substituída(o) por halogênio; n é 1 ou 2; m é 1 ou 2; e a sais de adição de ácido farmaceuticamente aceitáveis dos mesmos. Foi visto que os compostos de fórmula geral (1) são bons inibidores do transportador de glicina 1 (GIyT-1).
BRPI0606730-1A 2005-01-18 2006-01-10 derivados de fenil metanona 2,5-di-substituìdos como inibidores do transportador de glicina 1 (glyt-1) para o tratamento de distúbios neurológicos e neuropsiquiátricos BRPI0606730A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP05100280 2005-01-18
PCT/EP2006/000127 WO2006077026A1 (en) 2005-01-18 2006-01-10 2, 5-disubstituted phenyl methanone derivatives as glycine transporter 1 (glyt-i) inhibitors for the treatment of neurological and neuropsychiatry disorders

Publications (1)

Publication Number Publication Date
BRPI0606730A2 true BRPI0606730A2 (pt) 2009-07-14

Family

ID=35985447

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0606730-1A BRPI0606730A2 (pt) 2005-01-18 2006-01-10 derivados de fenil metanona 2,5-di-substituìdos como inibidores do transportador de glicina 1 (glyt-1) para o tratamento de distúbios neurológicos e neuropsiquiátricos

Country Status (14)

Country Link
US (1) US7790763B2 (pt)
EP (1) EP1843767B1 (pt)
JP (1) JP2008527016A (pt)
KR (1) KR100935256B1 (pt)
CN (1) CN101141959B (pt)
AT (1) ATE435650T1 (pt)
AU (1) AU2006207650B2 (pt)
BR (1) BRPI0606730A2 (pt)
CA (1) CA2601326A1 (pt)
DE (1) DE602006007682D1 (pt)
ES (1) ES2326833T3 (pt)
IL (1) IL184439A (pt)
MX (1) MX2007008616A (pt)
WO (1) WO2006077026A1 (pt)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2406085T3 (es) * 2006-06-22 2013-06-05 F. Hoffmann-La Roche Ag Derivados de fenil-metanona sustituida y su empleo como inhibidores de receptores de GlyT1 y GlyT2
EP2202223B1 (en) 2007-10-18 2017-01-25 Takeda Pharmaceutical Company Limited Heterocyclic compound as blood rbp4 lowering agent
EP3215500A1 (en) 2014-11-05 2017-09-13 Dart NeuroScience (Cayman) Ltd. Substituted azetidinyl compounds as glyt1 inhibitors
WO2025198588A1 (en) * 2024-03-20 2025-09-25 Bridgene Biosciences, Inc. Preparation of compound and crystalline forms thereof

Family Cites Families (21)

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Publication number Priority date Publication date Assignee Title
DE2423847A1 (de) 1973-05-28 1975-01-02 Ciba Geigy Ag Neue sulfamoylbenzoesaeureamide
DE2611705A1 (de) 1976-03-18 1977-09-22 Josef Dipl Chem Dr Rer N Klosa N-5-(nitrofurfuryliden-)-1-amino- hydantoin enthaltende kristalloesungsmittel
IT1176613B (it) 1984-08-14 1987-08-18 Ravizza Spa Derivati piperazinici farmacologicamente attivi e processo per la loro preparazione
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US6001854A (en) * 1996-05-31 1999-12-14 Allelix Neuroscience Inc. Pharmaceutical for treating of neurological and neuropsychiatric disorders
WO1997045423A1 (en) * 1996-05-31 1997-12-04 Trophix Neuroscience Inc. Pharmaceutical for treating of neurological and neuropsychiatric disorders
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CA2322164A1 (en) * 1998-03-06 1999-09-10 Ludo Edmond Josephine Kennis Glycine transport inhibitors
EP1296950A2 (en) * 2000-04-20 2003-04-02 NPS Allelix Corp. Aminopiperidines for use as glyt-1 inhibitors
DOP2001000189A (es) * 2000-06-30 2002-03-30 Pfizer Prod Inc Benzofenonas y sulfonas como inhibidores de la captación de glicina
GB0021419D0 (en) 2000-08-31 2000-10-18 Oxford Glycosciences Uk Ltd Compounds
JP2005502623A (ja) 2001-07-02 2005-01-27 ノボ ノルディスク アクティーゼルスカブ 置換ピペラジンおよびジアゼパン
WO2003035602A1 (en) 2001-10-25 2003-05-01 Sankyo Company, Limited Lipid modulators
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SE0302116D0 (sv) * 2003-07-21 2003-07-21 Astrazeneca Ab Novel compounds
AU2004263306B2 (en) 2003-08-11 2010-04-22 F. Hoffmann-La Roche Ag Piperazine with or-substituted phenyl group and their use as GLYT1 inhibitors
DK1663232T3 (da) 2003-09-09 2008-02-04 Hoffmann La Roche Benzimidazolderivater som human chymase-inhibitorer
JP4563387B2 (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−ベンゾイル−ピペラジン誘導体
GB0329362D0 (en) * 2003-12-18 2004-01-21 Glaxo Group Ltd Compounds
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ES2406085T3 (es) * 2006-06-22 2013-06-05 F. Hoffmann-La Roche Ag Derivados de fenil-metanona sustituida y su empleo como inhibidores de receptores de GlyT1 y GlyT2

Also Published As

Publication number Publication date
WO2006077026A1 (en) 2006-07-27
US20060160788A1 (en) 2006-07-20
CN101141959B (zh) 2010-12-15
DE602006007682D1 (de) 2009-08-20
MX2007008616A (es) 2007-09-11
IL184439A (en) 2011-11-30
ATE435650T1 (de) 2009-07-15
AU2006207650A1 (en) 2006-07-27
JP2008527016A (ja) 2008-07-24
AU2006207650B2 (en) 2011-01-27
EP1843767A1 (en) 2007-10-17
EP1843767B1 (en) 2009-07-08
KR20070094971A (ko) 2007-09-27
US7790763B2 (en) 2010-09-07
CA2601326A1 (en) 2006-07-27
IL184439A0 (en) 2007-10-31
ES2326833T3 (es) 2009-10-20
KR100935256B1 (ko) 2010-01-06
CN101141959A (zh) 2008-03-12

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Legal Events

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B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 8A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2260 DE 29/04/2014.