JP2013503909A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013503909A5 JP2013503909A5 JP2012528121A JP2012528121A JP2013503909A5 JP 2013503909 A5 JP2013503909 A5 JP 2013503909A5 JP 2012528121 A JP2012528121 A JP 2012528121A JP 2012528121 A JP2012528121 A JP 2012528121A JP 2013503909 A5 JP2013503909 A5 JP 2013503909A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- alkyl
- optionally substituted
- cycloalkyl
- composition
- Prior art date
- Legal status (The legal status 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 status listed.)
- Withdrawn
Links
- 150000001875 compounds Chemical class 0.000 claims 39
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 229910052799 carbon Inorganic materials 0.000 claims 20
- 229910052760 oxygen Inorganic materials 0.000 claims 15
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 14
- 229910052757 nitrogen Inorganic materials 0.000 claims 14
- 229910052717 sulfur Inorganic materials 0.000 claims 14
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- YNQLUTRBYVCPMQ-UHFFFAOYSA-N Ethylbenzene Chemical compound CCC1=CC=CC=C1 YNQLUTRBYVCPMQ-UHFFFAOYSA-N 0.000 claims 6
- 229910005965 SO 2 Inorganic materials 0.000 claims 6
- 125000001309 chloro group Chemical group Cl* 0.000 claims 6
- 230000004064 dysfunction Effects 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 claims 4
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 4
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 4
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 4
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 4
- -1 tert- butyl acetyl Chemical group 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 3
- 102100038354 Metabotropic glutamate receptor 4 Human genes 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 108010038422 metabotropic glutamate receptor 4 Proteins 0.000 claims 3
- IUGYQRQAERSCNH-UHFFFAOYSA-N pivalic acid Chemical compound CC(C)(C)C(O)=O IUGYQRQAERSCNH-UHFFFAOYSA-N 0.000 claims 3
- 208000019901 Anxiety disease Diseases 0.000 claims 2
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- ZLTPDFXIESTBQG-UHFFFAOYSA-N isothiazole Chemical compound C=1C=NSC=1 ZLTPDFXIESTBQG-UHFFFAOYSA-N 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims 2
- 229930192474 thiophene Natural products 0.000 claims 2
- 208000031091 Amnestic disease Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 206010012218 Delirium Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- ARUKYTASOALXFG-UHFFFAOYSA-N cycloheptylcycloheptane Chemical class C1CCCCCC1C1CCCCCC1 ARUKYTASOALXFG-UHFFFAOYSA-N 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 230000000848 glutamatergic effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000002503 metabolic effect Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000001537 neural effect Effects 0.000 claims 1
- 210000002569 neuron Anatomy 0.000 claims 1
- 239000002858 neurotransmitter agent Substances 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000004083 survival effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24003109P | 2009-09-04 | 2009-09-04 | |
| US61/240,031 | 2009-09-04 | ||
| PCT/US2010/048030 WO2011029104A1 (en) | 2009-09-04 | 2010-09-07 | Mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013503909A JP2013503909A (ja) | 2013-02-04 |
| JP2013503909A5 true JP2013503909A5 (https=) | 2013-10-24 |
Family
ID=43649686
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012528121A Withdrawn JP2013503909A (ja) | 2009-09-04 | 2010-09-07 | ｍＧＬｕＲ４アロステリック増強剤、組成物、および神経機能不全を治療する方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8779157B2 (https=) |
| EP (1) | EP2473055A4 (https=) |
| JP (1) | JP2013503909A (https=) |
| CN (1) | CN102740699A (https=) |
| AU (1) | AU2010289281A1 (https=) |
| BR (1) | BR112012004919A2 (https=) |
| CA (1) | CA2773038A1 (https=) |
| IL (1) | IL218426A0 (https=) |
| IN (1) | IN2012DN02580A (https=) |
| RU (1) | RU2012114770A (https=) |
| SG (1) | SG178999A1 (https=) |
| WO (1) | WO2011029104A1 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG173465A1 (en) | 2009-01-28 | 2011-09-29 | Univ Vanderbilt | Substituted 1,1,3,3-tetraoxidobenzo[d][1,3,2]dithiazoles as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US8759377B2 (en) * | 2009-11-23 | 2014-06-24 | Vanderbilt University | Substituted dioxopiperidines and dioxopyrrolidines as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| EP3049409B1 (en) * | 2013-09-25 | 2017-05-03 | F. Hoffmann-La Roche AG | Ethynyl derivatives |
| EP2853532B1 (en) | 2013-09-28 | 2020-12-09 | Instytut Farmakologii Polskiej Akademii Nauk | 1,2,4-oxadiazole derivatives as allosteric modulators of metabotropic glutamate receptors belonging to group III |
| TWI649310B (zh) * | 2014-01-10 | 2019-02-01 | 赫孚孟拉羅股份公司 | 乙炔基衍生物 |
| MA39305A3 (fr) * | 2014-02-25 | 2018-05-31 | Hoffmann La Roche | Dérivés d'éthynyle |
| US10221172B2 (en) | 2015-01-13 | 2019-03-05 | Vanderbilt University | Benzothiazole and benzisothiazole-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US10227343B2 (en) | 2015-01-30 | 2019-03-12 | Vanderbilt University | Isoquiniline and napthalene-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US10526323B2 (en) | 2015-01-30 | 2020-01-07 | Vanderbilt University | Indazole and azaindazole substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| CN107207481B (zh) * | 2015-03-19 | 2020-03-03 | 豪夫迈·罗氏有限公司 | 作为mglur4的调节剂的3-(4-乙炔基苯基)六氢嘧啶-2,4-二酮衍生物 |
| WO2016179351A1 (en) | 2015-05-05 | 2016-11-10 | Northwestern University | Treatment of levodopa-induced dyskinesias |
| ES2733468T3 (es) | 2015-07-15 | 2019-11-29 | Hoffmann La Roche | Derivados de etinilo como moduladores de los receptores metabotrópicos de glutamato |
| WO2018015235A1 (en) | 2016-07-18 | 2018-01-25 | F. Hoffmann-La Roche Ag | Ethynyl derivatives |
| US10294222B2 (en) | 2016-09-01 | 2019-05-21 | Vanderbilt University | Benzomorpholine and benzomorpholine-substituted compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US10710997B2 (en) | 2016-09-01 | 2020-07-14 | Vanderbilt University | Isoquinoline amide and isoquinoline amide-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US11242342B2 (en) | 2016-11-08 | 2022-02-08 | Vanderbilt University | Isoquinoline amine compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US10968227B2 (en) | 2016-11-08 | 2021-04-06 | Vanderbilt University | Isoquinoline ether compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US11319304B2 (en) | 2017-06-28 | 2022-05-03 | Vanderbilt University | Pyridine quinoline compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| IL272575B2 (en) | 2017-08-16 | 2023-09-01 | Univ Vanderbilt | Indazole compounds as allosteric enhancers of mglur4, compositions and methods for treating neurological dysfunction |
| US20220089609A1 (en) | 2018-07-26 | 2022-03-24 | Domain Therapeutics | Substituted quinazolinone derivatives and their use as positive allosteric modulators of mglur4 |
| CN119504747B (zh) * | 2024-11-26 | 2025-11-21 | 上海交通大学 | 一种含氮杂季碳双环海因类衍生物及其合成方法 |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK529378A (da) | 1978-01-09 | 1979-07-10 | Shell Int Research | Anilidderivater |
| TW521073B (en) | 1994-01-05 | 2003-02-21 | Hoechst Marion Roussel Inc | New optionally substituted phenylimidazolidines, their preparation process, their use as anti-androgenic agent and the pharmaceutical compositions containing them |
| FR2725206B1 (fr) | 1994-09-29 | 1996-12-06 | Roussel Uclaf | Nouvelles imidazolidines substituees par un heterocycle, leur procede et des intermediaires de preparation, leur application comme medicaments et les compositions pharmaceutiques les renfermant |
| US6355664B1 (en) | 1997-03-03 | 2002-03-12 | Boehringer Ingelheim Pharmaceuticals, Inc. | Phenylpyrrolidines, phenylimidazolidines, 3-phenyl-1,3-oxizolidines and 3-phenyl-1,3-thiazolidines and their use in the treatment of inflammatory disease |
| USRE38132E1 (en) | 1997-03-03 | 2003-06-03 | Boehringer Ingelheim Pharmaceuticals, Inc. | Phenylpyrrolidines, phenylimidazolidines,3-phenyl-1,3-oxizolidines and 3-phenyl-1,3-thiazolidines and their use in the treatment of inflammatory disease |
| FR2764889B1 (fr) | 1997-06-20 | 2000-09-01 | Sod Conseils Rech Applic | Nouveaux derives du 2-(iminomethyl)amino-phenyle, leur preparation, leur application a titre de medicaments et les compositions pharmaceutiques les contenant |
| US6335445B1 (en) | 1997-03-24 | 2002-01-01 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) | Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them |
| US6809088B2 (en) | 1997-03-24 | 2004-10-26 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) | Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them |
| DE60034571T2 (de) | 1999-06-15 | 2007-12-27 | Aventis Pharmaceuticals Inc. | Festphasensynthese von n,n-disubstituierten diazacycloalkylcarboxy-derivaten |
| US6353013B1 (en) | 1999-07-21 | 2002-03-05 | Boehringer Ingelheim Pharmaceuticals, Inc. | Small molecules useful in the treatment of inflammatory disease |
| US6365615B1 (en) | 1999-07-21 | 2002-04-02 | Boehringer Ingelheim Pharmaceuticals, Inc. | Small molecules useful in the treatment of inflammatory disease |
| CA2393466C (en) | 1999-12-21 | 2010-01-19 | Gpi Nil Holdings, Inc. | Hydantoin derivative compounds, pharmaceutical compositions, and methods of using same |
| US6890915B2 (en) | 2001-05-25 | 2005-05-10 | Bristol-Myers Squibb Pharma Company | Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE) |
| CA2462112A1 (en) | 2001-10-01 | 2003-04-10 | Bristol-Myers Squibb Company | Spiro-hydantoin compounds useful as anti-inflammatory agents |
| US7030141B2 (en) * | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
| MXPA05000813A (es) | 2002-07-31 | 2005-04-19 | Euro Celtique Sa | Compuestos hidrantoina aril sustituidos y su uso como bloqueadores del canal de sodio. |
| US7053112B2 (en) | 2002-09-24 | 2006-05-30 | Schering Aktiengesellschaft | Imidazolidinedione analogs useful as anticoagulants and antithrombotics |
| EP2027856A1 (en) | 2003-07-11 | 2009-02-25 | Boehringer Ingelheim Vetmedica Gmbh | Method of treating or preventing central nervous system disorders with compounds having selectivity benzodiazepine receptor |
| WO2005030128A2 (en) * | 2003-09-23 | 2005-04-07 | Merck & Co., Inc. | Pyrazole modulators of metabotropic glutamate receptors |
| TWI345568B (en) * | 2004-04-02 | 2011-07-21 | Mitsubishi Tanabe Pharma Corp | Tetrahydronaphthyridine derivatives and a process for preparing the same |
| MX2007000214A (es) | 2004-07-01 | 2007-05-10 | Asubio Pharma Co Ltd | Derivado de tienopirazol que tiene actividad inhibidora de pde 7. |
| UY29896A1 (es) * | 2005-11-04 | 2007-06-29 | Astrazeneca Ab | Nuevos derivados de cromano, composiciones farmacéuticas conteniéndolos, procesos de preparación y aplicaciones |
| JP2010500300A (ja) | 2006-08-08 | 2010-01-07 | サノフィ−アベンティス | アリールアミノアリール−アルキル−置換イミダゾリジン−２，４−ジオン、それらの製造法、それらの化合物を含有する薬剤、およびそれらの使用 |
| GB0713686D0 (en) | 2007-07-13 | 2007-08-22 | Addex Pharmaceuticals Sa | New compounds 2 |
| TW200927747A (en) | 2007-10-16 | 2009-07-01 | Novartis Ag | Organic compounds |
-
2010
- 2010-09-07 RU RU2012114770/13A patent/RU2012114770A/ru not_active Application Discontinuation
- 2010-09-07 CA CA2773038A patent/CA2773038A1/en not_active Abandoned
- 2010-09-07 AU AU2010289281A patent/AU2010289281A1/en not_active Abandoned
- 2010-09-07 BR BR112012004919A patent/BR112012004919A2/pt not_active IP Right Cessation
- 2010-09-07 EP EP10814634A patent/EP2473055A4/en not_active Withdrawn
- 2010-09-07 CN CN2010800490890A patent/CN102740699A/zh active Pending
- 2010-09-07 US US13/394,309 patent/US8779157B2/en not_active Expired - Fee Related
- 2010-09-07 SG SG2012015525A patent/SG178999A1/en unknown
- 2010-09-07 WO PCT/US2010/048030 patent/WO2011029104A1/en not_active Ceased
- 2010-09-07 JP JP2012528121A patent/JP2013503909A/ja not_active Withdrawn
- 2010-09-07 IN IN2580DEN2012 patent/IN2012DN02580A/en unknown
-
2012
- 2012-03-01 IL IL218426A patent/IL218426A0/en unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013503909A5 (https=) | ||
| JP2013519684A5 (https=) | ||
| JP2013519685A5 (https=) | ||
| JP2013526544A5 (https=) | ||
| CA2798514A1 (en) | Heterocyclic sulfone mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction | |
| Erhardt et al. | The kynurenine pathway in schizophrenia and bipolar disorder | |
| DK2592081T3 (en) | TETRAHYDROCARBOLIN DERIVATIVES | |
| RU2488582C2 (ru) | Бициклозамещенные азопроизводные пиразолона, способ их получения и фармацевтическое применение | |
| CN101848908B (zh) | 激酶抑制剂的组合物及其在治疗癌症和其它与激酶相关的疾病中的用途 | |
| JP2013535408A5 (https=) | ||
| KR20170081204A (ko) | 제약 화합물 | |
| RU2012114770A (ru) | АЛЛОСТЕРИЧЕСКИЕ СРЕДСТВА ПОТЕНЦИРОВАНИЯ mGluR4, КОМПОЗИЦИИ И СПОСОБЫ ЛЕЧЕНИЯ НЕВРОЛОГИЧЕСКИХ ДИСФУНКЦИЙ | |
| CN109963854A (zh) | 杂芳基并[4,3-c]嘧啶-5-胺类衍生物、其制备方法及其在医药上的应用 | |
| RU2009126745A (ru) | Производные сульфонилфенил-2н-{1,2,4}оксадиазол-5-она, способы их получения и их применение в качестве фармацевтических средств | |
| JP2011515482A5 (https=) | ||
| RU2015120478A (ru) | Пери-карбинолы | |
| JP2007513915A5 (https=) | ||
| JPWO2005035516A1 (ja) | 新規縮合複素環化合物およびその用途 | |
| JP2010504286A5 (https=) | ||
| JP2013510178A5 (https=) | ||
| CA2702482A1 (en) | Substituted n-phenyl-bipyrrolidine carboxamides and therapeutic use thereof | |
| JP2013509392A5 (https=) | ||
| JP2017522340A5 (https=) | ||
| JP2011510992A5 (https=) | ||
| CN102458580A (zh) | 作为mek抑制剂的杂环化合物 |