JP2013510178A5 - - Google Patents
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- JP2013510178A5 JP2013510178A5 JP2012538064A JP2012538064A JP2013510178A5 JP 2013510178 A5 JP2013510178 A5 JP 2013510178A5 JP 2012538064 A JP2012538064 A JP 2012538064A JP 2012538064 A JP2012538064 A JP 2012538064A JP 2013510178 A5 JP2013510178 A5 JP 2013510178A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- compound
- halogen
- alkyl
- pharmaceutical 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- Withdrawn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 59
- 125000000217 alkyl group Chemical group 0.000 claims 33
- 229910052736 halogen Inorganic materials 0.000 claims 33
- 239000008194 pharmaceutical composition Substances 0.000 claims 33
- 150000002367 halogens Chemical class 0.000 claims 32
- 229910052757 nitrogen Inorganic materials 0.000 claims 32
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 28
- 229910052760 oxygen Inorganic materials 0.000 claims 28
- 229910052717 sulfur Inorganic materials 0.000 claims 28
- 229910052799 carbon Inorganic materials 0.000 claims 27
- 125000003118 aryl group Chemical group 0.000 claims 22
- 125000001072 heteroaryl group Chemical group 0.000 claims 22
- JUJWROOIHBZHMG-UHFFFAOYSA-N pyridine Substances C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 16
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 12
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 12
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical class C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 8
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 8
- 150000003222 pyridines Chemical class 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Natural products C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- BCHZICNRHXRCHY-UHFFFAOYSA-N 2h-oxazine Chemical compound N1OC=CC=C1 BCHZICNRHXRCHY-UHFFFAOYSA-N 0.000 claims 2
- AGIJRRREJXSQJR-UHFFFAOYSA-N 2h-thiazine Chemical compound N1SC=CC=C1 AGIJRRREJXSQJR-UHFFFAOYSA-N 0.000 claims 2
- 241000124008 Mammalia Species 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 class C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 2
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical class C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 230000004064 dysfunction Effects 0.000 claims 2
- 150000003230 pyrimidines Chemical class 0.000 claims 2
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims 2
- 102100038354 Metabotropic glutamate receptor 4 Human genes 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 108010038422 metabotropic glutamate receptor 4 Proteins 0.000 claims 1
- 239000002858 neurotransmitter agent Substances 0.000 claims 1
- -1 pyrazine compound Chemical class 0.000 claims 1
- 0 Cc1nc(C(Nc(cc2)ccc2S(Cc2c(*)cccc2)(=O)=O)=O)ccc1 Chemical compound Cc1nc(C(Nc(cc2)ccc2S(Cc2c(*)cccc2)(=O)=O)=O)ccc1 0.000 description 1
- APCHCMVJUVMQNL-UHFFFAOYSA-N O=C(c1ncccc1)Nc(cc1)ccc1S(Cc1ccccc1Cl)(=O)=O Chemical compound O=C(c1ncccc1)Nc(cc1)ccc1S(Cc1ccccc1Cl)(=O)=O APCHCMVJUVMQNL-UHFFFAOYSA-N 0.000 description 1
- YOKWKTDEUJJKGB-UHFFFAOYSA-N O=C(c1ncccc1F)Nc(cc1)ccc1S(Cc(cccc1)c1Cl)(=O)=O Chemical compound O=C(c1ncccc1F)Nc(cc1)ccc1S(Cc(cccc1)c1Cl)(=O)=O YOKWKTDEUJJKGB-UHFFFAOYSA-N 0.000 description 1
- VSVMWYZCNYNQMD-UHFFFAOYSA-N O=S(Cc1ccccc1Cl)(c(cc1nc(-c2ncccc2)[nH]c1c1)c1F)=O Chemical compound O=S(Cc1ccccc1Cl)(c(cc1nc(-c2ncccc2)[nH]c1c1)c1F)=O VSVMWYZCNYNQMD-UHFFFAOYSA-N 0.000 description 1
- CKHALBGUSBGGRS-UHFFFAOYSA-N OS(Cc(cccc1)c1Cl)(c(cc1)ccc1NC(c1cccc(Cl)n1)=O)=O Chemical compound OS(Cc(cccc1)c1Cl)(c(cc1)ccc1NC(c1cccc(Cl)n1)=O)=O CKHALBGUSBGGRS-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25885609P | 2009-11-06 | 2009-11-06 | |
| US61/258,856 | 2009-11-06 | ||
| PCT/US2010/055861 WO2011057208A2 (en) | 2009-11-06 | 2010-11-08 | Aryl and heteroaryl sulfones as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013510178A JP2013510178A (ja) | 2013-03-21 |
| JP2013510178A5 true JP2013510178A5 (https=) | 2013-12-26 |
Family
ID=43970815
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012538064A Withdrawn JP2013510178A (ja) | 2009-11-06 | 2010-11-08 | ｍＧｌｕＲ４アロステリック増強剤としてのアリールおよびヘテロアリールスルホン、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) | US8912336B2 (https=) |
| EP (1) | EP2498781A2 (https=) |
| JP (1) | JP2013510178A (https=) |
| KR (1) | KR20120115252A (https=) |
| CN (1) | CN103079570A (https=) |
| AU (1) | AU2010314891A1 (https=) |
| BR (1) | BR112012010738A2 (https=) |
| CA (1) | CA2780128A1 (https=) |
| IL (1) | IL219568A0 (https=) |
| MX (1) | MX2012005248A (https=) |
| RU (1) | RU2012121631A (https=) |
| WO (1) | WO2011057208A2 (https=) |
Families Citing this family (17)
| 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 |
| GB201104153D0 (en) | 2011-03-11 | 2011-04-27 | Glaxo Group Ltd | Novel compounds |
| WO2016115272A1 (en) | 2015-01-13 | 2016-07-21 | 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 |
| WO2016179351A1 (en) | 2015-05-05 | 2016-11-10 | Northwestern University | Treatment of levodopa-induced dyskinesias |
| AR105556A1 (es) * | 2015-08-03 | 2017-10-18 | Hoffmann La Roche | Derivados de 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 |
| CN108148054B (zh) * | 2016-12-05 | 2021-01-08 | 中国科学院大连化学物理研究所 | 一种吡啶基桥联手性噁唑啉化合物及其合成方法 |
| WO2019006157A1 (en) | 2017-06-28 | 2019-01-03 | Vanderbilt University | Pyridine quinoline compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US11427573B2 (en) | 2017-08-16 | 2022-08-30 | Vanderbilt University | Indazole compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| KR20210068399A (ko) * | 2018-08-06 | 2021-06-09 | 더 보드 오브 트러스티스 오브 더 리랜드 스탠포드 주니어 유니버시티 | 신경퇴행성 질병의 치료를 위한 피피에이알지씨1알파 활성제로서 2-아릴벤즈이미다졸 |
| CN112409251B (zh) * | 2020-11-26 | 2022-07-05 | 成都百泉生物医药科技有限公司 | 一种奥美拉唑工艺杂质及其制备方法 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3326753A (en) * | 1961-02-23 | 1967-06-20 | Merck & Co Inc | Benzimidazole anthelmintic compositions and method of use |
| US3429890A (en) * | 1964-12-31 | 1969-02-25 | Merck & Co Inc | Certain 2-thiazolylbenzimidazole-1-oxy derivatives |
| DE2130030A1 (de) * | 1971-06-18 | 1972-12-21 | Bayer Ag | Fungizide und bakterizide Mittel |
| PT100905A (pt) * | 1991-09-30 | 1994-02-28 | Eisai Co Ltd | Compostos heterociclicos azotados biciclicos contendo aneis de benzeno, ciclo-hexano ou piridina e de pirimidina, piridina ou imidazol substituidos e composicoes farmaceuticas que os contem |
| FR2751649B1 (fr) | 1996-07-26 | 1998-08-28 | Adir | Nouveaux derives de benzimidazole, de benzoxazole et de benzothiazole, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| GB9914825D0 (en) | 1999-06-24 | 1999-08-25 | Smithkline Beecham Spa | Novel compounds |
| US6448281B1 (en) | 2000-07-06 | 2002-09-10 | Boehringer Ingelheim (Canada) Ltd. | Viral polymerase inhibitors |
| WO2002046168A1 (en) | 2000-12-07 | 2002-06-13 | Astrazeneca Ab | Therapeutic benzimidazole compounds |
| US6897208B2 (en) | 2001-10-26 | 2005-05-24 | Aventis Pharmaceuticals Inc. | Benzimidazoles |
| WO2003066629A2 (en) | 2002-02-06 | 2003-08-14 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds useful as inhibitors of gsk-3 |
| WO2005007096A2 (en) | 2003-07-11 | 2005-01-27 | Merck & Co., Inc. | Treatment of movement disorders with a metabotropic glutamate 4 receptor positive allosteric modulator |
| BRPI0418212A (pt) | 2003-12-29 | 2007-04-27 | Banyu Pharma Co Ltd | composto ou um sal deste farmaceuticamente aceitável, ativador da glicocinase, e, medicamentos para a terapia e/ou prevenção da diabete, e da obesidade |
| ES2318556T3 (es) | 2004-11-02 | 2009-05-01 | Pfizer, Inc. | Derivados de sulfonil bencimidazol. |
| GB0505725D0 (en) | 2005-03-19 | 2005-04-27 | Merck Sharp & Dohme | Therapeutic agents |
| AU2006258842B2 (en) | 2005-06-13 | 2011-09-15 | Merck Sharp & Dohme Limited | Therapeutic agents |
| DE602007009807D1 (de) | 2006-03-06 | 2010-11-25 | Raqualia Pharma Inc | Sulfonylbenzimidazolderivate |
| CA2646755A1 (en) | 2006-03-31 | 2007-10-11 | Astrazeneca Ab | Bicyclic benzimidazole compounds and their use as metabotropic glutamate receptor potentiators |
| CN101765425A (zh) | 2007-08-02 | 2010-06-30 | 弗·哈夫曼-拉罗切有限公司 | 苯甲酰胺衍生物用于治疗cns障碍的用途 |
| PT2294066E (pt) * | 2008-04-28 | 2014-11-21 | Janssen Pharmaceutica Nv | Benzoimidazoles como inibidores da prolil-hidroxilase |
-
2010
- 2010-11-08 KR KR1020127014657A patent/KR20120115252A/ko not_active Withdrawn
- 2010-11-08 AU AU2010314891A patent/AU2010314891A1/en not_active Abandoned
- 2010-11-08 RU RU2012121631/15A patent/RU2012121631A/ru not_active Application Discontinuation
- 2010-11-08 JP JP2012538064A patent/JP2013510178A/ja not_active Withdrawn
- 2010-11-08 EP EP10829242A patent/EP2498781A2/en not_active Withdrawn
- 2010-11-08 CA CA2780128A patent/CA2780128A1/en not_active Abandoned
- 2010-11-08 MX MX2012005248A patent/MX2012005248A/es not_active Application Discontinuation
- 2010-11-08 WO PCT/US2010/055861 patent/WO2011057208A2/en not_active Ceased
- 2010-11-08 US US13/508,535 patent/US8912336B2/en active Active
- 2010-11-08 CN CN2010800589711A patent/CN103079570A/zh active Pending
- 2010-11-08 BR BR112012010738A patent/BR112012010738A2/pt not_active IP Right Cessation
-
2012
- 2012-05-03 IL IL219568A patent/IL219568A0/en unknown