WO2007023242A1 - Tétrahydroquinolinones et leur usage en tant que modulateurs des récepteurs de glutamate métabotropiques - Google Patents
Tétrahydroquinolinones et leur usage en tant que modulateurs des récepteurs de glutamate métabotropiques Download PDFInfo
- Publication number
- WO2007023242A1 WO2007023242A1 PCT/GB2005/003285 GB2005003285W WO2007023242A1 WO 2007023242 A1 WO2007023242 A1 WO 2007023242A1 GB 2005003285 W GB2005003285 W GB 2005003285W WO 2007023242 A1 WO2007023242 A1 WO 2007023242A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- quinolin
- dihydro
- dimethyl
- ylethynyl
- phenylethynyl
- Prior art date
Links
- FPHPAIMVSFFVBA-UHFFFAOYSA-N CC(C)(CCc1c2ccc(C#Cc3cc(C(NN=N)=N)cc(F)c3)n1)C2=O Chemical compound CC(C)(CCc1c2ccc(C#Cc3cc(C(NN=N)=N)cc(F)c3)n1)C2=O FPHPAIMVSFFVBA-UHFFFAOYSA-N 0.000 description 1
- IOZMODDHDZWFGN-UHFFFAOYSA-N CC(C)(CCc1c2ccc(C#Cc3ncc[o]3)n1)C2=O Chemical compound CC(C)(CCc1c2ccc(C#Cc3ncc[o]3)n1)C2=O IOZMODDHDZWFGN-UHFFFAOYSA-N 0.000 description 1
- ZKOPJTIDGYUNFS-UHFFFAOYSA-N CC(C)(Cc1c2ccc(C#Cc3cccc(C#N)c3)n1)CC2=O Chemical compound CC(C)(Cc1c2ccc(C#Cc3cccc(C#N)c3)n1)CC2=O ZKOPJTIDGYUNFS-UHFFFAOYSA-N 0.000 description 1
- ZINAKIAGFBYZIY-UHFFFAOYSA-N CC(C)(Cc1c2ccc(C#Cc3cccc(O)c3)n1)CC2=O Chemical compound CC(C)(Cc1c2ccc(C#Cc3cccc(O)c3)n1)CC2=O ZINAKIAGFBYZIY-UHFFFAOYSA-N 0.000 description 1
- JFWMDTILRZSYAO-UHFFFAOYSA-N O=C(CCC1)c(cc2)c1nc2C#CC(C=NC1)=CC1F Chemical compound O=C(CCC1)c(cc2)c1nc2C#CC(C=NC1)=CC1F JFWMDTILRZSYAO-UHFFFAOYSA-N 0.000 description 1
- QMEDLAZYJXJINI-UHFFFAOYSA-N O=C(CCC1)c(cc2)c1nc2C#Cc1nnc[o]1 Chemical compound O=C(CCC1)c(cc2)c1nc2C#Cc1nnc[o]1 QMEDLAZYJXJINI-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—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
- 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
- C07D215/20—Oxygen atoms
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
-
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
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- C07D401/00—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
- C07D401/02—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
- 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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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- C07D401/02—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
- C07D401/10—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 aromatic rings
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- C07D401/14—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 three or more hetero rings
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- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Definitions
- R 1 represents aryl or heteroaryl
- aryl represents an unsubstituted phenyl ring or a phenyl ring that is substituted with 1 , 2, 3, 4 or 5 substituents, that may be the same of different, which substituents are selected from the group consisting of Ci -6 alkyl, which is optionally substituted with one or more fluorine, chlorine or bromine atoms, Ci -6 alkoxy, which is optionally substituted with one or more fluorine, chlorine or bromine atoms, cycloC 3 -i 2 alkyl, hydroxyl, F, Cl 1 Br, I, CN, nitro, di-Ci -6 alkylamino, N ⁇ cycloC 3- i 2 alkyl-N- Ci-ealkylamino, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, A-
- composition comprising, together with one or more pharmaceutically acceptable excipients or vehicles, a compound of Formula I
- R 1 represents aryl or heteroaryl
- hydrohalic acids such as hydrochloric, hydrobromic and the like; sulfuric acid; nitric acid; phosphoric acid and the like; or organic acids such as acetic, propanoic, hydroxyacetic, 2-hydroxypropanoic, oxopropanoic, oxalic, malonic, succinic, maleic, fumaric, malic, tartaric, 2-hydroxy-1 ,2,3-propanetricarboxylic, methanesulfonic, ethanesulfonic, benzenesulfonic, 4-methylbenzenesulfonic, cyclohexanesulfonic, 2-hydroxybenzoic, 4-amino-2-hydroxybenzoic and the like acids.
- the salt form can be converted by treatment with alkali into the free base form.
- the active ingredients of the invention may be placed into the form of pharmaceutical compositions and unit dosages thereof, and in such form may be employed as solids, such as coated or uncoated tablets or filled capsules, or liquids, such as solutions, suspensions, emulsions, elixirs, or capsules filled with the same, all for oral use; in the form of suppositories or capsules for rectal administration or in the form of sterile injectable solutions for parenteral (including intravenous or subcutaneous) use.
- Nanoparticle formulation 10 g of polybutylcyanoacrylate nanoparticles contain:
- the medium Prior to addition of agonist or antagonist the medium was aspirated and cells were loaded for 2 h at RT with 150 ⁇ L of loading buffer consisting of Ca- sensitive dye (MD # R8033) reconstituted in sodium chloride (123 rriM), potassium chloride (5.4 mM), magnesium chloride (0.8 nriM), calcium chloride (1.8 mM), D-glucose (15 mM), and HEPES (20 mM), pH 7.3. Subsequently, plates were transferred to FLIPR to detect calcium increase with the addition of DHPG (300 ⁇ iw) or L-quisqualate (100 nM) measured as relative fluorescence units (RFU). If antagonists were tested, these compounds were pre-incubated for 10 min at RT before addition of the respective agonist.
- Ca- sensitive dye MD # R8033
Abstract
L’invention concerne des dérivés de tétrahydroquinolinone à substitution éthynyle ainsi que leurs sels pharmaceutiquement acceptables. L’invention porte également sur un procédé permettant de préparer de tels composés. Les composés de cette invention sont des modulateurs de mGIuR de groupe I et sont par conséquent utiles lors du contrôle et de la prévention de troubles neurologiques aigus et/ou chroniques.
Priority Applications (16)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/GB2005/003285 WO2007023242A1 (fr) | 2005-08-24 | 2005-08-24 | Tétrahydroquinolinones et leur usage en tant que modulateurs des récepteurs de glutamate métabotropiques |
TW095130667A TWI329635B (en) | 2005-08-24 | 2006-08-21 | Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors |
ARP060103692A AR056044A1 (es) | 2005-08-24 | 2006-08-24 | Tetrahidroquinolinonas y su uso como moduladores de receptores de glutamato metabotropicos |
JP2008527513A JP2009506018A (ja) | 2005-08-24 | 2006-08-24 | テトラヒドロキノリノン類及び代謝型グルタミン酸受容体のモジュレータとしてのその使用 |
AU2006283359A AU2006283359B2 (en) | 2005-08-24 | 2006-08-24 | Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors |
PCT/GB2006/003170 WO2007023290A1 (fr) | 2005-08-24 | 2006-08-24 | Tétrahydroquinolinones et leur utilisation comme modulateurs de récepteurs métabotropique de glutamate |
EA200800660A EA200800660A1 (ru) | 2005-08-24 | 2006-08-24 | Тетрагидрохинолиноны и их применение в качестве модуляторов метаботропных глутаматных рецепторов |
KR1020087004382A KR20080031972A (ko) | 2005-08-24 | 2006-08-24 | 테트라히드로퀴놀리논 및 향대사성 글루타메이트 수용체의조절제로서의 이들의 용도 |
CNA2006800260106A CN101223142A (zh) | 2005-08-24 | 2006-08-24 | 四氢喹诺酮以及其作为向代谢性谷氨酸受体调节剂的应用 |
EP06779201A EP1931635A1 (fr) | 2005-08-24 | 2006-08-24 | Tétrahydroquinolinones et leur utilisation comme modulateurs de récepteurs métabotropique de glutamate |
CA2610873A CA2610873C (fr) | 2005-08-24 | 2006-08-24 | Tetrahydroquinolinones et leur utilisation comme modulateurs de recepteurs metabotropique de glutamate |
MX2008001871A MX2008001871A (es) | 2005-08-24 | 2006-08-24 | Tetrahidroquinolinonas y su uso como moduladores de receptores de glutamato metabotropicos. |
BRPI0615059-4A BRPI0615059A2 (pt) | 2005-08-24 | 2006-08-24 | tetrahidroquinolinonas e seu uso como moduladores de receptores metabotrópicos de glutamato |
ZA200710668A ZA200710668B (en) | 2005-08-24 | 2007-12-06 | Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors |
IL189617A IL189617A (en) | 2005-08-24 | 2008-02-19 | Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors |
NO20081428A NO20081428L (no) | 2005-08-24 | 2008-03-18 | Tetrahydrokinolinoner og anvendelse derav som modulatorer av metabotrope glutamatreseptorer |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/GB2005/003285 WO2007023242A1 (fr) | 2005-08-24 | 2005-08-24 | Tétrahydroquinolinones et leur usage en tant que modulateurs des récepteurs de glutamate métabotropiques |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2007023242A1 true WO2007023242A1 (fr) | 2007-03-01 |
Family
ID=36273537
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/GB2005/003285 WO2007023242A1 (fr) | 2005-08-24 | 2005-08-24 | Tétrahydroquinolinones et leur usage en tant que modulateurs des récepteurs de glutamate métabotropiques |
PCT/GB2006/003170 WO2007023290A1 (fr) | 2005-08-24 | 2006-08-24 | Tétrahydroquinolinones et leur utilisation comme modulateurs de récepteurs métabotropique de glutamate |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/GB2006/003170 WO2007023290A1 (fr) | 2005-08-24 | 2006-08-24 | Tétrahydroquinolinones et leur utilisation comme modulateurs de récepteurs métabotropique de glutamate |
Country Status (15)
Country | Link |
---|---|
EP (1) | EP1931635A1 (fr) |
JP (1) | JP2009506018A (fr) |
KR (1) | KR20080031972A (fr) |
CN (1) | CN101223142A (fr) |
AR (1) | AR056044A1 (fr) |
AU (1) | AU2006283359B2 (fr) |
BR (1) | BRPI0615059A2 (fr) |
CA (1) | CA2610873C (fr) |
EA (1) | EA200800660A1 (fr) |
IL (1) | IL189617A (fr) |
MX (1) | MX2008001871A (fr) |
NO (1) | NO20081428L (fr) |
TW (1) | TWI329635B (fr) |
WO (2) | WO2007023242A1 (fr) |
ZA (1) | ZA200710668B (fr) |
Cited By (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2010084050A2 (fr) | 2009-01-13 | 2010-07-29 | Novartis Ag | Dérivés de quinazolinone utiles comme antagonistes vanilloïdes |
WO2011073339A1 (fr) | 2009-12-18 | 2011-06-23 | Janssen Pharmaceutica Nv | Thiazoles bicycliques en tant que modulateurs allostériques des récepteurs mglur5 |
WO2011073347A1 (fr) | 2009-12-18 | 2011-06-23 | Janssen Pharmaceutica Nv | Thiazoles bicycliques en tant que modulateurs allostériques des récepteurs mglur5 |
WO2011092293A2 (fr) | 2010-02-01 | 2011-08-04 | Novartis Ag | Dérivés de cyclohexylamide utilisés en tant qu'antagonistes du récepteur du crf |
WO2011092290A1 (fr) | 2010-02-01 | 2011-08-04 | Novartis Ag | Dérivés de pyrazolo[5,1-b] utilisés en tant qu'antagonistes du récepteur de crf-1 |
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WO2012139876A1 (fr) | 2011-04-14 | 2012-10-18 | Merz Pharma Gmbh & Co. Kgaa | Formulations entériques de modulateurs de récepteur de glutamate métabotropique |
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US11242338B2 (en) | 2018-05-17 | 2022-02-08 | The Wistar Institute | EBNA1 inhibitor crystalline forms, and methods of preparing and using same |
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US8772301B2 (en) | 2009-12-18 | 2014-07-08 | Sunovion Pharmaceuticals, Inc. | Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof |
WO2012052451A1 (fr) | 2010-10-18 | 2012-04-26 | Merz Pharma Gmbh & Co. Kgaa | Modulateurs des récepteurs métabotropes au glutamate |
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TWI301760B (en) * | 2004-02-27 | 2008-10-11 | Merz Pharma Gmbh & Co Kgaa | Tetrahydroquinolinones and their use as antagonists of metabotropic glutamate receptors |
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WO2011073339A1 (fr) | 2009-12-18 | 2011-06-23 | Janssen Pharmaceutica Nv | Thiazoles bicycliques en tant que modulateurs allostériques des récepteurs mglur5 |
EA020010B1 (ru) * | 2009-12-18 | 2014-07-30 | Янссен Фармацевтика Нв | БИЦИКЛИЧЕСКИЕ ТИАЗОЛЫ В КАЧЕСТВЕ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ mGluR5 РЕЦЕПТОРОВ |
US9174953B2 (en) | 2009-12-18 | 2015-11-03 | Janssen Pharmaceutica Nv | Bicyclic thiazoles as allosteric modulators of mGluR5 receptors |
US9040707B2 (en) | 2009-12-18 | 2015-05-26 | Janssen Pharmaceutica Nv | Bicyclic thiazoles as allosteric modulators of mGluR5 receptors |
CN102666552A (zh) * | 2009-12-18 | 2012-09-12 | 詹森药业有限公司 | 作为mglur5受体的变构调节剂的双环噻唑 |
CN102666551A (zh) * | 2009-12-18 | 2012-09-12 | 詹森药业有限公司 | 作为mglur5受体的变构调节剂的双环噻唑 |
CN102666552B (zh) * | 2009-12-18 | 2014-11-26 | 詹森药业有限公司 | 作为mglur5受体的变构调节剂的双环噻唑 |
WO2011073347A1 (fr) | 2009-12-18 | 2011-06-23 | Janssen Pharmaceutica Nv | Thiazoles bicycliques en tant que modulateurs allostériques des récepteurs mglur5 |
AU2010332819B2 (en) * | 2009-12-18 | 2014-02-27 | Janssen Pharmaceutica Nv | Bicyclic thiazoles as allosteric modulators of mGluR5 receptors |
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WO2012139876A1 (fr) | 2011-04-14 | 2012-10-18 | Merz Pharma Gmbh & Co. Kgaa | Formulations entériques de modulateurs de récepteur de glutamate métabotropique |
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US10081647B2 (en) | 2015-03-26 | 2018-09-25 | Merck Sharp & Dohme Corp. | Phosphate substituted quinolizine derivatives useful as HIV integrase inhibitors |
WO2016154527A1 (fr) * | 2015-03-26 | 2016-09-29 | Merck Sharp & Dohme Corp. | Dérivés de quinolizine substitués par un phosphate utiles en tant qu'inhibiteurs de l'intégrase du vih |
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US10981867B2 (en) | 2015-05-14 | 2021-04-20 | The Wistar Institute Of Anatomy And Biology | EBNA1 inhibitors and methods using same |
US11912659B2 (en) | 2015-05-14 | 2024-02-27 | The Wistar Institute Of Anatomy And Biology | EBNA1 inhibitors and methods using same |
CN111148744A (zh) * | 2017-09-26 | 2020-05-12 | 布拉格玛治疗公司 | 作为mglur7调节剂的新的杂环化合物 |
US11242338B2 (en) | 2018-05-17 | 2022-02-08 | The Wistar Institute | EBNA1 inhibitor crystalline forms, and methods of preparing and using same |
Also Published As
Publication number | Publication date |
---|---|
AU2006283359B2 (en) | 2010-05-27 |
EA200800660A1 (ru) | 2008-06-30 |
TWI329635B (en) | 2010-09-01 |
JP2009506018A (ja) | 2009-02-12 |
TW200728283A (en) | 2007-08-01 |
AR056044A1 (es) | 2007-09-12 |
IL189617A0 (en) | 2008-06-05 |
CA2610873C (fr) | 2010-08-03 |
IL189617A (en) | 2012-08-30 |
KR20080031972A (ko) | 2008-04-11 |
ZA200710668B (en) | 2009-08-26 |
CA2610873A1 (fr) | 2007-03-01 |
BRPI0615059A2 (pt) | 2011-04-26 |
NO20081428L (no) | 2008-03-18 |
MX2008001871A (es) | 2008-04-09 |
AU2006283359A1 (en) | 2007-03-01 |
WO2007023290A1 (fr) | 2007-03-01 |
CN101223142A (zh) | 2008-07-16 |
EP1931635A1 (fr) | 2008-06-18 |
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