JP2013503909A5 - - Google Patents
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- 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- Withdrawn
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- 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 (enExample) | 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 (enExample) |
| EP (1) | EP2473055A4 (enExample) |
| JP (1) | JP2013503909A (enExample) |
| CN (1) | CN102740699A (enExample) |
| AU (1) | AU2010289281A1 (enExample) |
| BR (1) | BR112012004919A2 (enExample) |
| CA (1) | CA2773038A1 (enExample) |
| IL (1) | IL218426A0 (enExample) |
| IN (1) | IN2012DN02580A (enExample) |
| RU (1) | RU2012114770A (enExample) |
| SG (1) | SG178999A1 (enExample) |
| WO (1) | WO2011029104A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2010208176A1 (en) | 2009-01-28 | 2011-09-15 | Vanderbilt University | 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 |
| KR101757603B1 (ko) * | 2013-09-25 | 2017-07-12 | 에프. 호프만-라 로슈 아게 | 에틴일 유도체 |
| 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 |
| PL3110802T3 (pl) * | 2014-02-25 | 2019-03-29 | F. Hoffmann-La Roche Ag | Pochodne etynylowe |
| 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 |
| WO2016123629A1 (en) | 2015-01-30 | 2016-08-04 | Vanderbilt University | Indazole and azaindazole substituted compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| JP6539749B2 (ja) * | 2015-03-19 | 2019-07-03 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | ｍＧｌｕＲ４のモジュレーターとしての３−（４−エチニルフェニル）ヘキサヒドロピリミジン−２，４−ジオン誘導体 |
| US9987242B2 (en) | 2015-05-05 | 2018-06-05 | Northwestern University | Treatment of Levodopa-induced Dyskinesias |
| LT3322701T (lt) | 2015-07-15 | 2019-07-10 | F. Hoffmann-La Roche Ag | Etinilo dariniai kaip metabotropinių glutamato receptorių moduliatoriai |
| CR20190014A (es) | 2016-07-18 | 2019-03-04 | Hoffmann La Roche | Derivados etinilo |
| 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 |
| 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 |
| US10968227B2 (en) | 2016-11-08 | 2021-04-06 | Vanderbilt University | Isoquinoline ether compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| WO2018089544A1 (en) | 2016-11-08 | 2018-05-17 | Vanderbilt University | Isoquinoline amine 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 |
| BR112020003292A2 (pt) | 2017-08-16 | 2020-08-18 | Vanderbilt University | compostos indazol como potencializadores alostéricos de mglur4 e seus usos terapêuticos, bem como composição farmacêutica e método para fabricação de medicamento para potenciar a atividade do receptor mglur4 |
| 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 |
| 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 |
| 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 |
| 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 |
| ATE360818T1 (de) | 1999-06-15 | 2007-05-15 | Aventis Pharma Inc | Festphasensynthese von n,n-disubstituierten diazacycloalkylcarboxy-derivaten |
| US6365615B1 (en) | 1999-07-21 | 2002-04-02 | Boehringer Ingelheim Pharmaceuticals, Inc. | Small molecules useful in the treatment of inflammatory disease |
| US6353013B1 (en) | 1999-07-21 | 2002-03-05 | Boehringer Ingelheim Pharmaceuticals, Inc. | Small molecules useful in the treatment of inflammatory disease |
| AU1464101A (en) | 1999-12-21 | 2001-07-03 | Gpi Nil Holdings, Inc. | Hydantoin derivative compounds, pharmaceutical compositions, and methods of using same |
| EP1397137B1 (en) | 2001-05-25 | 2009-10-14 | Bristol-Myers Squibb Company | Hydantion derivatives as inhibitors of matrix metalloproteinases |
| BR0213025A (pt) | 2001-10-01 | 2004-10-05 | Bristol Myers Squibb Co | Compostos de espiro-hidantoìna úteis como agentes antiinflamatórios |
| US7030141B2 (en) * | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
| JP2005538101A (ja) | 2002-07-31 | 2005-12-15 | ユーロ−セルティーク エス．エイ． | アリール置換ヒダントイン化合物及びナトリウムチャネルブロッカーとしてのその使用 |
| US7053112B2 (en) | 2002-09-24 | 2006-05-30 | Schering Aktiengesellschaft | Imidazolidinedione analogs useful as anticoagulants and antithrombotics |
| UA87982C2 (ru) | 2003-07-11 | 2009-09-10 | Берингер Ингельхайм Ветмедика Гмбх | Способ лечения или предотвращения расстройств центральной нервной системы производными 1-ар(алк)-4-пиперидиноимидазолин-2-она, фармацевтическая композиция |
| JP2007506741A (ja) * | 2003-09-23 | 2007-03-22 | メルク エンド カムパニー インコーポレーテッド | 向代謝性グルタミン酸受容体のピラゾール系調節剤 |
| MY139887A (en) * | 2004-04-02 | 2009-11-30 | Mitsubishi Tanabe Pharma Corp | Tetrahydronaphthyridine derivatives and a process for preparing the same. |
| EP1775298B1 (en) * | 2004-07-01 | 2013-03-20 | Daiichi Sankyo Company, Limited | Thienopyrazole derivative having pde7 inhibitory activity |
| UY29896A1 (es) * | 2005-11-04 | 2007-06-29 | Astrazeneca Ab | Nuevos derivados de cromano, composiciones farmacéuticas conteniéndolos, procesos de preparación y aplicaciones |
| AU2007283113A1 (en) | 2006-08-08 | 2008-02-14 | Sanofi-Aventis | Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, processes for preparing them, medicaments comprising these compounds, and their use |
| 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 WO PCT/US2010/048030 patent/WO2011029104A1/en not_active Ceased
- 2010-09-07 RU RU2012114770/13A patent/RU2012114770A/ru not_active Application Discontinuation
- 2010-09-07 US US13/394,309 patent/US8779157B2/en not_active Expired - Fee Related
- 2010-09-07 BR BR112012004919A patent/BR112012004919A2/pt not_active IP Right Cessation
- 2010-09-07 JP JP2012528121A patent/JP2013503909A/ja not_active Withdrawn
- 2010-09-07 EP EP10814634A patent/EP2473055A4/en not_active Withdrawn
- 2010-09-07 AU AU2010289281A patent/AU2010289281A1/en not_active Abandoned
- 2010-09-07 CN CN2010800490890A patent/CN102740699A/zh active Pending
- 2010-09-07 CA CA2773038A patent/CA2773038A1/en not_active Abandoned
- 2010-09-07 SG SG2012015525A patent/SG178999A1/en unknown
- 2010-09-07 IN IN2580DEN2012 patent/IN2012DN02580A/en unknown
-
2012
- 2012-03-01 IL IL218426A patent/IL218426A0/en unknown
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