TWI328578B - Acetylene derivatives having mglur5 antagonistic activity - Google Patents

Acetylene derivatives having mglur5 antagonistic activity Download PDF

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Publication number
TWI328578B
TWI328578B TW091134933A TW91134933A TWI328578B TW I328578 B TWI328578 B TW I328578B TW 091134933 A TW091134933 A TW 091134933A TW 91134933 A TW91134933 A TW 91134933A TW I328578 B TWI328578 B TW I328578B
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Taiwan
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hydroxy
phenylethynyl
cyclohexyl
octahydro
carboxylic acid
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TW091134933A
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English (en)
Chinese (zh)
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TW200304910A (en
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Gasparini Fabrizio
Auberson Yves
Ofner Silvio
Zimme Rmann Kaspar
W Hart Terance
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Novartis Ag
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Publication of TW200304910A publication Critical patent/TW200304910A/zh
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    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/16—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
    • A—HUMAN NECESSITIES
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    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/24—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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    • 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
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    • A61P25/32—Alcohol-abuse
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07C233/23—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
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    • C07D209/04—Indoles; Hydrogenated indoles
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    • C07D215/08—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
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    • C07D401/04—Heterocyclic 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
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    • C07D401/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
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    • C07D405/12—Heterocyclic 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

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  • Hospice & Palliative Care (AREA)
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  • Cardiology (AREA)
  • Heart & Thoracic Surgery (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)
  • Indole Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
TW091134933A 2001-12-04 2002-12-02 Acetylene derivatives having mglur5 antagonistic activity TWI328578B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0128996.6A GB0128996D0 (en) 2001-12-04 2001-12-04 Organic compounds

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TW200304910A TW200304910A (en) 2003-10-16
TWI328578B true TWI328578B (en) 2010-08-11

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US (4) US7348353B2 (enExample)
EP (1) EP1453512B8 (enExample)
JP (2) JP4176020B2 (enExample)
KR (2) KR100980901B1 (enExample)
CN (2) CN101366714B (enExample)
AR (2) AR037682A1 (enExample)
AT (1) ATE327755T1 (enExample)
AU (1) AU2002358585B2 (enExample)
BR (1) BR0214666A (enExample)
CA (1) CA2466560C (enExample)
CO (1) CO5590929A2 (enExample)
CY (1) CY1105460T1 (enExample)
DE (1) DE60211944T2 (enExample)
DK (1) DK1453512T3 (enExample)
EC (1) ECSP045139A (enExample)
EG (1) EG24936A (enExample)
ES (1) ES2263842T3 (enExample)
GB (1) GB0128996D0 (enExample)
HU (1) HU229429B1 (enExample)
IL (1) IL161990A0 (enExample)
MX (1) MXPA04005456A (enExample)
MY (1) MY137774A (enExample)
NO (1) NO327005B1 (enExample)
NZ (1) NZ533266A (enExample)
PE (1) PE20030640A1 (enExample)
PL (1) PL212996B1 (enExample)
PT (1) PT1453512E (enExample)
RU (1) RU2341515C2 (enExample)
TW (1) TWI328578B (enExample)
WO (1) WO2003047581A1 (enExample)
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GB0503646D0 (en) * 2005-02-22 2005-03-30 Novartis Ag Organic compounds
GB0508318D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0508319D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0508314D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0514296D0 (en) * 2005-07-12 2005-08-17 Novartis Ag Organic compounds
KR20090061041A (ko) * 2006-09-11 2009-06-15 노파르티스 아게 대사성 글루타메이트 수용체의 조절제로서의 니코틴산 유도체
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AU2012254934B2 (en) * 2007-10-12 2013-10-17 Novartis Ag Metabotropic glutamate receptor modulators for the treatment of Parkinson's disease
EP2810951B1 (en) 2008-06-04 2017-03-15 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
EP2826478A1 (en) * 2008-06-30 2015-01-21 Novartis AG Combinations comprising mglur modulators for the treatment of parkinson's disease
NZ590753A (en) * 2008-08-12 2012-06-29 Novartis Ag Processes for the preparation of 4-oxo-octahydro-indole-1-carbocylic acid methyl ester and derivatives thereof
US8334287B2 (en) 2009-07-17 2012-12-18 Hoffmann-La Roche Inc. Imidazoles
WO2011009890A2 (en) 2009-07-23 2011-01-27 Novartis Ag Use of azabicycloalkyl derivatives or pyrrolidine-2-one derivatives
JO3250B1 (ar) 2009-09-22 2018-09-16 Novartis Ag إستعمال منشطات مستقبل نيكوتينيك أسيتيل كولين ألفا 7
EP2490691A1 (en) 2009-10-20 2012-08-29 Novartis AG Use of 1h-quinazoline-2,4-diones
BR112012027816A2 (pt) * 2010-04-30 2017-08-08 Novartis Ag marcadores preditivos úteis no tratamento da síndrome do x frágil (fxs).
RU2013103001A (ru) 2010-06-24 2014-07-27 Новартис Аг Применение 1н-хиназолин-2,4-дионов
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EP2668159A1 (en) 2011-01-24 2013-12-04 Novartis AG 4-tolyl-ethynyl-octahydro-indole-1-ester derivatives
US20140171448A1 (en) 2011-01-27 2014-06-19 Novartis Ag Use of nicotinic acetylcholine receptor alpha 7 activators
CA2830458A1 (en) 2011-03-18 2012-09-27 Novartis Ag Combinations of alpha 7 nicotinic acetylcholine receptor activators and mglur5 antagonists for use in dopamine induced dyskinesia in parkinson's disease
WO2013036224A1 (en) 2011-09-07 2013-03-14 Novartis Ag Use of 1h-quinazoline- 2, 4 -diones for use in the prevention or treatment photosensitive epilepsy
WO2013131981A1 (en) 2012-03-08 2013-09-12 Novartis Ag Predictive markers useful in the diagnosis and treatment of fragile x syndrome (fxs)
GB201215033D0 (en) 2012-08-23 2012-10-10 Novartis Ag Diazepinone derivatives
BR112015016994A8 (pt) 2013-01-15 2018-01-23 Novartis Ag uso de agonistas do receptor alfa 7 nicotínico de acetilcolina
WO2014111837A1 (en) 2013-01-15 2014-07-24 Novartis Ag Use of alpha 7 nicotinic acetylcholine receptor agonists
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CA3066711A1 (en) 2017-07-31 2019-02-07 Novartis Ag Use of mavoglurant in the reduction of cocaine use or in preventing relapse into cocaine use
US12201612B2 (en) 2017-07-31 2025-01-21 Novartis Ag Use of mavoglurant in the reduction of alcohol use or in preventing relapse into alcohol use
KR20210120011A (ko) 2019-01-29 2021-10-06 노파르티스 아게 오피오이드 진통제 내약성을 치료하기 위한 mglur5 길항제의 용도
US20220387410A1 (en) * 2019-11-05 2022-12-08 Claes Thulin 4-[5-[(rac)-1-[5-(3-Chlorophenyl)-3-isoxazolyl]ethoxy]-4-methyl-4H-1,2,4-triazol-3-yl]pyridine for use in prevention and/or treatment of surmenage in a mammal
MX2023000664A (es) 2020-07-17 2023-02-27 Novartis Ag Uso de antagonistas de mglur5.
WO2022123482A1 (en) 2020-12-11 2022-06-16 Novartis Ag Use of mglur5 antagonists for treating amphetamine addiction
CA3204360A1 (en) 2020-12-14 2022-06-23 Novartis Ag Use of mglur5 antagonists for treating gambling disorder

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