JP2013519684A5 - - Google Patents
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- Publication number
- JP2013519684A5 JP2013519684A5 JP2012553051A JP2012553051A JP2013519684A5 JP 2013519684 A5 JP2013519684 A5 JP 2013519684A5 JP 2012553051 A JP2012553051 A JP 2012553051A JP 2012553051 A JP2012553051 A JP 2012553051A JP 2013519684 A5 JP2013519684 A5 JP 2013519684A5
- Authority
- JP
- Japan
- Prior art keywords
- heteroaryl
- aryl
- optionally substituted
- alkyl
- optionally
- 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.)
- Granted
Links
- 125000003118 aryl group Chemical group 0.000 claims 62
- 125000001072 heteroaryl group Chemical group 0.000 claims 62
- 125000000217 alkyl group Chemical group 0.000 claims 44
- 229910052717 sulfur Inorganic materials 0.000 claims 40
- 229910052799 carbon Inorganic materials 0.000 claims 30
- 229910052736 halogen Inorganic materials 0.000 claims 26
- 150000002367 halogens Chemical class 0.000 claims 26
- 229910052757 nitrogen Inorganic materials 0.000 claims 25
- 229910052760 oxygen Inorganic materials 0.000 claims 25
- 229910052739 hydrogen Inorganic materials 0.000 claims 22
- 150000002431 hydrogen Chemical class 0.000 claims 22
- 239000001257 hydrogen Substances 0.000 claims 22
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 19
- 239000008194 pharmaceutical composition Substances 0.000 claims 18
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 12
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 11
- 125000000753 cycloalkyl group Chemical group 0.000 claims 11
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 10
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 9
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 9
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 230000004064 dysfunction Effects 0.000 claims 5
- 102100038354 Metabotropic glutamate receptor 4 Human genes 0.000 claims 4
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 4
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 4
- 108010038422 metabotropic glutamate receptor 4 Proteins 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 3
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 150000002825 nitriles Chemical class 0.000 claims 3
- 208000019901 Anxiety disease Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 2
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 230000002708 enhancing effect Effects 0.000 claims 2
- -1 methoxy, difluoromethoxy Chemical group 0.000 claims 2
- 201000000980 schizophrenia Diseases 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
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 239000003814 drug 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
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000002503 metabolic effect Effects 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000000203 mixture Substances 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
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 230000004083 survival effect Effects 0.000 claims 1
- 230000005062 synaptic transmission Effects 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 0 C=Cc1cnc2[n]1*ccc2 Chemical compound C=Cc1cnc2[n]1*ccc2 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30348110P | 2010-02-11 | 2010-02-11 | |
| US61/303,481 | 2010-02-11 | ||
| US201161430521P | 2011-01-06 | 2011-01-06 | |
| US61/430,521 | 2011-01-06 | ||
| PCT/US2011/024618 WO2011100607A1 (en) | 2010-02-11 | 2011-02-11 | Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as mglur4 allosteric potentiators, compounds, and methods of treating neurological dysfunction |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013519684A JP2013519684A (ja) | 2013-05-30 |
| JP2013519684A5 true JP2013519684A5 (cg-RX-API-DMAC7.html) | 2014-04-03 |
| JP5883399B2 JP5883399B2 (ja) | 2016-03-15 |
Family
ID=44368167
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012553051A Expired - Fee Related JP5883399B2 (ja) | 2010-02-11 | 2011-02-11 | ｍＧｌｕＲ４アロステリック増強剤としてのピラゾロピリジン、ピラゾロピラジン、ピラゾロピリミジン、ピラゾロチオフェンおよびピラゾロチアゾール化合物、組成物、および神経機能不全を治療する方法 |
Country Status (17)
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8658650B2 (en) | 2009-01-28 | 2014-02-25 | Vanderbilt University | Substituted 1,1,3,1-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 |
| EP2533639A4 (en) * | 2010-02-11 | 2013-08-21 | Univ Vanderbilt | PYRAZOLOPYRIDIN, PYRAZOLOPYRZIN, PYRAZOLOPYRIMIDIN, PYRAZOLOTHIOPHEN AND PYRAZOLOTHIAZOL COMPOUNDS AS ALLOSTERIC MGLUR4 POTENTRANS AND COMPOUNDS AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTIONS |
| MX339302B (es) | 2011-09-15 | 2016-05-19 | Novartis Ag | 3-(quinolin-6-il-tio)-[1,2,4]-triazolo-[4,3-a]-piridinas 6-sustituidas como cinasas de tirosina. |
| WO2013060029A1 (en) * | 2011-10-28 | 2013-05-02 | Merck Sharp & Dohme Corp | Allosteric modulators of metabotropic glutamate receptors |
| EP2791108B1 (en) | 2011-12-15 | 2016-07-27 | Pfizer Limited | Sulfonamide derivatives |
| EP2863912A4 (en) | 2012-06-20 | 2015-11-04 | Univ Vanderbilt | SUBSTITUTED BICYCLIC ALKOXYPYRAZOL ANALOGUES AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS |
| WO2014117920A1 (en) * | 2013-02-04 | 2014-08-07 | Merck Patent Gmbh | Spiro-quinazolinone derivatives useful for the treatment of neurological diseases and conditions |
| WO2014180182A1 (zh) * | 2013-05-10 | 2014-11-13 | 江苏豪森药业股份有限公司 | [1,2,4]三唑并[4,3-a]吡啶类衍生物，其制备方法或其在医药上的应用 |
| EP3626717A1 (en) | 2013-10-14 | 2020-03-25 | Eisai R&D Management Co., Ltd. | Selectively substituted quinoline compounds |
| US9663486B2 (en) | 2013-10-14 | 2017-05-30 | Eisai R&D Management Co., Ltd. | Selectively substituted quinoline compounds |
| EP3134404A1 (en) | 2014-04-25 | 2017-03-01 | Pfizer Inc. | Heteroaromatic compounds and their use as dopamine d1 ligands |
| US9980945B2 (en) | 2015-01-13 | 2018-05-29 | Vanderbilt University | Benzoisoxazole-substituted compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| 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 |
| 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 |
| 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 |
| WO2016172547A1 (en) * | 2015-04-24 | 2016-10-27 | Vanderbilt University | Substituted imidazopyridine and triazolopyridine analogs as positive allosteric modulators of muscarinic acetylcholine receptor m1 |
| UY36654A (es) | 2015-04-29 | 2016-10-31 | Janssen Pharmaceutica Nv | Azabenzimidazoles con propiedades moduladoras del receptor ampa y composiciones farmacéuticas que los contienen |
| WO2016179351A1 (en) | 2015-05-05 | 2016-11-10 | Northwestern University | Treatment of levodopa-induced dyskinesias |
| 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 |
| WO2018080918A1 (en) | 2016-10-26 | 2018-05-03 | Janssen Pharmaceutica Nv | 3-aryl-2h-pyrazolo[4,3-b]pyridine compounds and their use as ampa receptor modulators |
| WO2018085803A1 (en) * | 2016-11-07 | 2018-05-11 | Vanderbilt University | Positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
| US10968227B2 (en) | 2016-11-08 | 2021-04-06 | Vanderbilt University | Isoquinoline ether 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 |
| WO2019006157A1 (en) | 2017-06-28 | 2019-01-03 | 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 |
| CA3102326A1 (en) | 2018-07-26 | 2020-01-30 | Domain Therapeutics | Substituted quinazolinone derivatives and their use as positive allosteric modulators of mglur4 |
| CN111620874B (zh) * | 2019-02-28 | 2022-11-15 | 汇瀚医疗科技有限公司 | 取代5,6-双杂环氨基化合物作为wnt信号通路抑制剂及其治疗应用 |
| CN115605483A (zh) * | 2020-07-06 | 2023-01-13 | 莫尔根生物有限公司（Kr） | 三环双内酯化合物、其生产方法及用途 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1252418A (cg-RX-API-DMAC7.html) * | 1967-11-24 | 1971-11-03 | ||
| JP2004509115A (ja) | 2000-09-15 | 2004-03-25 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼインヒビターとして有用なピラゾール化合物 |
| US7368285B2 (en) | 2001-03-07 | 2008-05-06 | Senomyx, Inc. | Heteromeric umami T1R1/T1R3 taste receptors and isolated cells that express same |
| US7160913B2 (en) | 2002-09-13 | 2007-01-09 | Thomas Jefferson University | Methods and kit for treating Parkinson's disease |
| US20060166972A1 (en) * | 2003-07-11 | 2006-07-27 | Conn P J | Treatment of movement disorders with a metabotropic glutamate 4 receptor positive allosteric modulator |
| SE0302232D0 (sv) * | 2003-08-18 | 2003-08-18 | Astrazeneca Ab | Novel Compounds |
| SE0303180D0 (sv) | 2003-11-26 | 2003-11-26 | Astrazeneca Ab | Novel compounds |
| CN102603581B (zh) * | 2005-06-22 | 2015-06-24 | 普莱希科公司 | 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物 |
| WO2008089310A2 (en) * | 2007-01-18 | 2008-07-24 | Lexicon Pharmaceuticals, Inc. | Delta 5 desaturase inhibitors for the treatment of obesity |
| WO2008089307A2 (en) * | 2007-01-18 | 2008-07-24 | Lexicon Pharmaceuticals, Inc. | Delta 5 desaturase inhibitors for the treatment of pain, inflammation and cancer |
| GB0713686D0 (en) | 2007-07-13 | 2007-08-22 | Addex Pharmaceuticals Sa | New compounds 2 |
| NZ582879A (en) | 2007-07-31 | 2012-03-30 | Vertex Pharma | Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof |
| EP2533639A4 (en) * | 2010-02-11 | 2013-08-21 | Univ Vanderbilt | PYRAZOLOPYRIDIN, PYRAZOLOPYRZIN, PYRAZOLOPYRIMIDIN, PYRAZOLOTHIOPHEN AND PYRAZOLOTHIAZOL COMPOUNDS AS ALLOSTERIC MGLUR4 POTENTRANS AND COMPOUNDS AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTIONS |
-
2011
- 2011-02-11 EP EP20110742910 patent/EP2533639A4/en not_active Withdrawn
- 2011-02-11 BR BR112012020273A patent/BR112012020273A8/pt not_active IP Right Cessation
- 2011-02-11 AU AU2011215638A patent/AU2011215638B2/en not_active Ceased
- 2011-02-11 US US13/578,812 patent/US9163015B2/en active Active
- 2011-02-11 WO PCT/US2011/024618 patent/WO2011100607A1/en not_active Ceased
- 2011-02-11 MX MX2012009378A patent/MX2012009378A/es not_active Application Discontinuation
- 2011-02-11 CN CN201180017221.4A patent/CN102892288B/zh not_active Expired - Fee Related
- 2011-02-11 SG SG2012059325A patent/SG183263A1/en unknown
- 2011-02-11 JP JP2012553051A patent/JP5883399B2/ja not_active Expired - Fee Related
- 2011-02-11 CA CA 2789427 patent/CA2789427A1/en not_active Abandoned
- 2011-02-11 KR KR20127023699A patent/KR20130029368A/ko not_active Withdrawn
- 2011-02-11 EA EA201290774A patent/EA201290774A1/ru unknown
- 2011-02-11 PH PH1/2012/501621A patent/PH12012501621A1/en unknown
-
2012
- 2012-08-09 TN TNP2012000400A patent/TN2012000400A1/en unknown
- 2012-08-09 IL IL221390A patent/IL221390A0/en unknown
- 2012-08-10 CL CL2012002225A patent/CL2012002225A1/es unknown
- 2012-08-13 US US13/584,735 patent/US9108963B2/en active Active
- 2012-08-27 ZA ZA2012/06416A patent/ZA201206416B/en unknown