JP2017523201A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017523201A5 JP2017523201A5 JP2017505456A JP2017505456A JP2017523201A5 JP 2017523201 A5 JP2017523201 A5 JP 2017523201A5 JP 2017505456 A JP2017505456 A JP 2017505456A JP 2017505456 A JP2017505456 A JP 2017505456A JP 2017523201 A5 JP2017523201 A5 JP 2017523201A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- disorders
- disorder
- compound
- monohalo
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 35
- 150000001875 compounds Chemical class 0.000 claims 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 17
- 208000035475 disorder Diseases 0.000 claims 13
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 7
- 125000001475 halogen functional group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 208000011117 substance-related disease Diseases 0.000 claims 6
- 206010012289 Dementia Diseases 0.000 claims 5
- 208000007590 Disorders of Excessive Somnolence Diseases 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 210000003169 central nervous system Anatomy 0.000 claims 5
- 206010020765 hypersomnia Diseases 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 4
- 208000024714 major depressive disease Diseases 0.000 claims 4
- -1 —C 1-4 alkyl-OH Chemical group 0.000 claims 4
- 206010012218 Delirium Diseases 0.000 claims 3
- 208000020401 Depressive disease Diseases 0.000 claims 3
- 208000037490 Medically Unexplained Symptoms Diseases 0.000 claims 3
- 208000019022 Mood disease Diseases 0.000 claims 3
- 150000001204 N-oxides Chemical class 0.000 claims 3
- 208000027626 Neurocognitive disease Diseases 0.000 claims 3
- 208000029726 Neurodevelopmental disease Diseases 0.000 claims 3
- 208000020114 Schizophrenia and other psychotic disease Diseases 0.000 claims 3
- 208000028552 Treatment-Resistant Depressive disease Diseases 0.000 claims 3
- 125000004414 alkyl thio group Chemical group 0.000 claims 3
- 208000010877 cognitive disease Diseases 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 238000002360 preparation method Methods 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 201000000980 schizophrenia Diseases 0.000 claims 3
- 208000019116 sleep disease Diseases 0.000 claims 3
- 208000000044 Amnesia Diseases 0.000 claims 2
- 208000031091 Amnestic disease Diseases 0.000 claims 2
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 2
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 2
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- 208000027674 Schizophrenia Spectrum and Other Psychotic disease Diseases 0.000 claims 2
- 230000006986 amnesia Effects 0.000 claims 2
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 2
- 208000015114 central nervous system disease Diseases 0.000 claims 2
- 230000006735 deficit Effects 0.000 claims 2
- 230000006806 disease prevention Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- GLQXAHBYDJPCHG-UHFFFAOYSA-N 6,7-dihydro-5h-pyrazolo[1,5-a]pyrazin-4-one Chemical group O=C1NCCN2N=CC=C12 GLQXAHBYDJPCHG-UHFFFAOYSA-N 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 201000001880 Sexual dysfunction Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 208000012201 sexual and gender identity disease Diseases 0.000 claims 1
- 208000015891 sexual disease Diseases 0.000 claims 1
- 231100000872 sexual dysfunction Toxicity 0.000 claims 1
- 208000020685 sleep-wake disease Diseases 0.000 claims 1
- 230000000392 somatic effect Effects 0.000 claims 1
- 238000001228 spectrum Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14179599.7 | 2014-08-01 | ||
| EP14179599 | 2014-08-01 | ||
| PCT/EP2015/067533 WO2016016381A1 (en) | 2014-08-01 | 2015-07-30 | 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017523201A JP2017523201A (ja) | 2017-08-17 |
| JP2017523201A5 true JP2017523201A5 (en:Method) | 2018-09-06 |
| JP6615864B2 JP6615864B2 (ja) | 2019-12-04 |
Family
ID=51257438
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017505456A Expired - Fee Related JP6615864B2 (ja) | 2014-08-01 | 2015-07-30 | ６，７−ジヒドロピラゾロ［１，５−ａ］ピラジン−４（５Ｈ）−オン化合物およびＭＧＬＵＲ２受容体の負のアロステリック調節因子としてのそれらの使用 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10112949B2 (en:Method) |
| EP (1) | EP3174880B1 (en:Method) |
| JP (1) | JP6615864B2 (en:Method) |
| KR (1) | KR102531693B1 (en:Method) |
| CN (1) | CN106573935B (en:Method) |
| AR (1) | AR101393A1 (en:Method) |
| AU (1) | AU2015295299B2 (en:Method) |
| BR (1) | BR112017001998A2 (en:Method) |
| CA (1) | CA2954218C (en:Method) |
| EA (1) | EA031038B1 (en:Method) |
| ES (1) | ES2702192T3 (en:Method) |
| JO (1) | JO3601B1 (en:Method) |
| MX (1) | MX2017001453A (en:Method) |
| TW (1) | TWI696625B (en:Method) |
| WO (1) | WO2016016381A1 (en:Method) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20150177B1 (ar) | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
| JOP20150179B1 (ar) | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
| ES2727158T3 (es) | 2014-12-03 | 2019-10-14 | Janssen Pharmaceutica Nv | Ligandos para PET de mGluR2 radiomarcados |
| JP6689856B2 (ja) * | 2014-12-03 | 2020-04-28 | ヤンセン ファーマシューティカ エヌ．ベー． | ６，７−ジヒドロピラゾロ［１，５−ａ］ピラジン−４（５Ｈ）−オン化合物およびＭＧＬＵＲ２受容体の負のアロステリック調節因子としてのそれらの使用 |
| PL3389727T3 (pl) * | 2015-12-18 | 2021-02-08 | Janssen Pharmaceutica Nv | RADIOZNAKOWANE LIGANDY mGluR2/3 DO PET |
| WO2017103179A1 (en) | 2015-12-18 | 2017-06-22 | Janssen Pharmaceutica Nv | Radiolabelled mglur2/3 pet ligands |
| CA3082976A1 (en) | 2017-11-24 | 2019-05-31 | Sumitomo Dainippon Pharma Co., Ltd. | 6,7-dihydropyrazolo[1,5-a]pyrazinone derivative and medical use thereof |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102004054665A1 (de) * | 2004-11-12 | 2006-05-18 | Bayer Cropscience Gmbh | Substituierte bi- und tricyclische Pyrazol-Derivate Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren |
| RU2412943C2 (ru) * | 2005-03-23 | 2011-02-27 | Ф. Хоффманн-Ля Рош Аг | ПРОИЗВОДНЫЕ АЦЕТИЛЕНИЛ-ПИРАЗОЛО-ПИРИМИДИНА В КАЧЕСТВЕ АНТАГОНИСТОВ mGluR2 |
| SG176021A1 (en) | 2009-05-12 | 2011-12-29 | Janssen Pharmaceuticals Inc | 1,2,4-triazolo [4,3-a] pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders |
| AU2011343477A1 (en) | 2010-12-17 | 2013-07-04 | Vanderbilt University | Bicyclic triazole and pyrazole lactams as allosteric modulators of mGluR5 receptors |
| WO2012172093A1 (en) * | 2011-06-17 | 2012-12-20 | Merz Pharma Gmbh & Co. Kgaa | Dihydroindolizine derivate as metabotropic glutamate receptor modulators |
| US9278960B2 (en) | 2011-11-03 | 2016-03-08 | Merck Sharp & Dohme Corp. | Quinoline carboxamide and quinoline carbonitrile derivatives as mGluR2-negative allosteric modulators, compositions, and their use |
| EP2666775A1 (en) | 2012-05-21 | 2013-11-27 | Domain Therapeutics | Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors |
| US20130345205A1 (en) * | 2012-06-20 | 2013-12-26 | Vanderbilt University | Substituted bicyclic aralkyl pyrazole lactam analogs as allosteric modulators of mglur5 receptors |
| US20130345204A1 (en) | 2012-06-20 | 2013-12-26 | Vanderbilt University | Substituted bicyclic cycloalkyl pyrazole lactam analogs as allosteric modulators of mglur5 receptors |
| RU2015101532A (ru) * | 2012-06-20 | 2016-08-20 | Вандербилт Юниверсити | Замещенные бициклические алкокси-пиразольные аналоги в качестве аллостерических модуляторов рецепторов mglur5 |
| WO2014064028A1 (en) * | 2012-10-23 | 2014-05-01 | F. Hoffmann-La Roche Ag | Mglu2/3 antagonists for the treatment of autistic disorders |
| JP6517340B2 (ja) * | 2014-08-01 | 2019-05-22 | ヤンセン ファーマシューティカ エヌ．ベー． | ６，７−ジヒドロピラゾロ［１，５−ａ］ピラジン−４（５Ｈ）−オン化合物およびＭＧＬＵＲ２受容体の負のアロステリック調節因子としてのそれらの使用 |
-
2015
- 2015-07-27 JO JOP/2015/0178A patent/JO3601B1/ar active
- 2015-07-30 WO PCT/EP2015/067533 patent/WO2016016381A1/en not_active Ceased
- 2015-07-30 ES ES15742317T patent/ES2702192T3/es active Active
- 2015-07-30 CN CN201580041306.4A patent/CN106573935B/zh not_active Expired - Fee Related
- 2015-07-30 KR KR1020177005638A patent/KR102531693B1/ko active Active
- 2015-07-30 AU AU2015295299A patent/AU2015295299B2/en not_active Ceased
- 2015-07-30 US US15/500,553 patent/US10112949B2/en active Active
- 2015-07-30 BR BR112017001998A patent/BR112017001998A2/pt not_active Application Discontinuation
- 2015-07-30 EP EP15742317.9A patent/EP3174880B1/en active Active
- 2015-07-30 JP JP2017505456A patent/JP6615864B2/ja not_active Expired - Fee Related
- 2015-07-30 EA EA201692496A patent/EA031038B1/ru not_active IP Right Cessation
- 2015-07-30 TW TW104124697A patent/TWI696625B/zh not_active IP Right Cessation
- 2015-07-30 MX MX2017001453A patent/MX2017001453A/es active IP Right Grant
- 2015-07-30 CA CA2954218A patent/CA2954218C/en active Active
- 2015-07-31 AR ARP150102462A patent/AR101393A1/es unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2017523201A5 (en:Method) | ||
| JP2017522340A5 (en:Method) | ||
| JP2017523202A5 (en:Method) | ||
| JP2017526659A5 (en:Method) | ||
| JP2017528515A5 (en:Method) | ||
| CN107438593B (zh) | 治疗化合物及其用途 | |
| CY1125460T1 (el) | Ενωσεις ιμιδαζο [4,5-d]πυρρολο [2,3-β]πυριδινης ως αναστολεις κινασων janus | |
| CN112409363B (zh) | 用于治疗认知损害的苯并二氮杂䓬衍生物、组合物和方法 | |
| AU2014272695B2 (en) | Pyrazolo-pyrrolidin-4-one derivatives as BET inhibitors and their use in the treatment of disease | |
| PH12019501355A1 (en) | Small molecule inhibitors of the jak family of kinases | |
| JP6268183B2 (ja) | Ｐｉ３キナーゼモジュレータとしてのヘテロ芳香族化合物、及びその使用方法 | |
| RU2017106489A (ru) | 6,7-дигидропиразоло[1,5-а]пиразин-4(5h)-оновые соединения и их применение в качестве отрицательных аллостерических модуляторов рецепторов mglur2 | |
| CY1119607T1 (el) | ΠΑΡΑΓΩΓΟ ΙΜΙΔΑΖΟ[1,2-b]ΠΥΡΙΔΑΖΙΝΗΣ ΩΣ ΑΝΑΣΤΟΛΕΑΣ ΚΙΝΑΣΗΣ | |
| AR087336A1 (es) | Compuestos de 2-(2,4,5-anilino sustituido)pirimidina | |
| JP2018510851A (ja) | 治療用ピリダジン化合物およびその使用 | |
| WO2013155506A1 (en) | Novel compositions and methods | |
| RU2017106100A (ru) | 6,7-ДИГИДРОПИРАЗОЛО[1,5-α]ПИРАЗИН-4(5Н)-ОНОВЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ОТРИЦАТЕЛЬНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ MGLUR2 | |
| CA2898294C (en) | Heteroaromatic compounds as pi3 kinase modulators | |
| JP6814730B2 (ja) | 治療用化合物およびその使用 | |
| HRP20171051T1 (hr) | Spojevi 6,7-dihidropirazolo[1,5-a]pirazin-4(5h)-ona i njihova uporaba kao negativnih alosternih modulatora receptora mglur2 | |
| JP2021528427A (ja) | 認知障害を処置するためのベンゾジアゼピン誘導体、組成物および方法 | |
| WO2016036954A1 (en) | Phthalazine derivatives of formula (i) as pcaf and gcn5 inhibitors for use in the treatment of cancer | |
| WO2018130869A1 (en) | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment | |
| RU2017123038A (ru) | 6,7-ДИГИДРОПИРАЗОЛО[1,5-a]ПИРАЗИН-4(5H)-ОНОВЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ОТРИЦАТЕЛЬНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ MGLUR2 | |
| JP2017536399A5 (en:Method) |