JP2013526610A5 - - Google Patents
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- JP2013526610A5 JP2013526610A5 JP2013512170A JP2013512170A JP2013526610A5 JP 2013526610 A5 JP2013526610 A5 JP 2013526610A5 JP 2013512170 A JP2013512170 A JP 2013512170A JP 2013512170 A JP2013512170 A JP 2013512170A JP 2013526610 A5 JP2013526610 A5 JP 2013526610A5
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- JP
- Japan
- Prior art keywords
- optionally substituted
- compound
- alkyl
- formula
- structure represented
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 15
- 239000001257 hydrogen Substances 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000000547 substituted alkyl group Chemical group 0.000 claims 5
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
- 229930195712 glutamate Natural products 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- -1 cyano, hydroxyl Chemical group 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 201000000980 schizophrenia Diseases 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- 208000027534 Emotional disease Diseases 0.000 claims 2
- 102000012777 Metabotropic Glutamate 5 Receptor Human genes 0.000 claims 2
- 108010065028 Metabotropic Glutamate 5 Receptor Proteins 0.000 claims 2
- 150000001204 N-oxides Chemical class 0.000 claims 2
- 208000028017 Psychotic disease Diseases 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
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 208000024714 major depressive disease Diseases 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 208000000044 Amnesia Diseases 0.000 claims 1
- 208000031091 Amnestic disease Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 206010048962 Brain oedema Diseases 0.000 claims 1
- 206010008748 Chorea Diseases 0.000 claims 1
- 206010010305 Confusional state Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000020401 Depressive disease Diseases 0.000 claims 1
- 208000014094 Dystonic disease Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 208000016285 Movement disease Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010033664 Panic attack Diseases 0.000 claims 1
- 208000027099 Paranoid disease Diseases 0.000 claims 1
- 230000007000 age related cognitive decline Effects 0.000 claims 1
- 230000006986 amnesia Effects 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 208000006752 brain edema Diseases 0.000 claims 1
- 208000012601 choreatic disease Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 208000010118 dystonia Diseases 0.000 claims 1
- 201000003104 endogenous depression Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 210000003292 kidney cell Anatomy 0.000 claims 1
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 201000003631 narcolepsy Diseases 0.000 claims 1
- 230000000926 neurological effect Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 208000019906 panic disease Diseases 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 230000000698 schizophrenic effect Effects 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- 208000020685 sleep-wake disease Diseases 0.000 claims 1
- 208000011117 substance-related disease Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34779510P | 2010-05-24 | 2010-05-24 | |
| US61/347,795 | 2010-05-24 | ||
| PCT/US2011/037775 WO2011149963A1 (en) | 2010-05-24 | 2011-05-24 | Substituted-6-methylnicotinamides as mglur5 positive allosteric modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013526610A JP2013526610A (ja) | 2013-06-24 |
| JP2013526610A5 true JP2013526610A5 (https=) | 2014-07-10 |
Family
ID=45004338
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013512170A Pending JP2013526610A (ja) | 2010-05-24 | 2011-05-24 | Ｍｇｌｕｒ５の正のアロステリック調節剤としての置換６−メチルニコチンアミド |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US8969389B2 (https=) |
| EP (1) | EP2575461A4 (https=) |
| JP (1) | JP2013526610A (https=) |
| KR (1) | KR20130122531A (https=) |
| CN (1) | CN103037693A (https=) |
| AU (1) | AU2011258389A1 (https=) |
| CA (1) | CA2799966A1 (https=) |
| EA (1) | EA201291327A1 (https=) |
| MX (1) | MX2012013560A (https=) |
| WO (1) | WO2011149963A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011149963A1 (en) | 2010-05-24 | 2011-12-01 | Vanderbilt University | Substituted-6-methylnicotinamides as mglur5 positive allosteric modulators |
| US20130252943A1 (en) * | 2012-02-29 | 2013-09-26 | Vanderbilt University | Bicyclic oxazole lactams as allosteric modulators of mglur5 receptors |
| CN106146391A (zh) * | 2015-04-15 | 2016-11-23 | 中国科学院上海药物研究所 | 5-芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途 |
| WO2016179351A1 (en) | 2015-05-05 | 2016-11-10 | Northwestern University | Treatment of levodopa-induced dyskinesias |
| IL287136B2 (en) | 2016-02-05 | 2023-09-01 | Denali Therapeutics Inc | Receptor inhibitors - interacting with protein kinase 1 |
| JP7208137B2 (ja) | 2016-12-09 | 2023-01-18 | デナリ セラピューティクス インコーポレイテッド | 化合物、組成物および方法 |
| CN114437025B (zh) * | 2020-11-05 | 2023-08-25 | 上海零诺生物科技有限公司 | 消旋6-甲基烟碱及其制备方法、以及应用 |
| TW202334164A (zh) | 2022-01-12 | 2023-09-01 | 美商戴納立製藥公司 | （Ｓ）－５－苄基－Ｎ－（５－甲基－４－側氧基－２，３，４，５－四氫吡啶並［３，２－ｂ］［１，４］氧氮呯－３－基）－４Ｈ－１，２，４－三唑－３－甲醯胺的晶型 |
| WO2026072192A1 (en) | 2024-09-27 | 2026-04-02 | Alto Neuroscience, Inc. | Effective treatment of depression in patients having poor cognition or impaired learning and/or memory with a mglur5 positive allosteric modulator |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0590045A1 (en) * | 1991-06-12 | 1994-04-06 | E.I. Du Pont De Nemours And Company | Substituted pyridine herbicides |
| EP0533130A1 (de) * | 1991-09-19 | 1993-03-24 | Hoechst Aktiengesellschaft | 2-Hydroxymethylpyridine, die entsprechenden Pyridin-N-oxide und ihre Derivate, Verfahren zu ihrer Herstellung sowie deren Verwendung |
| GB9417532D0 (en) | 1994-08-31 | 1994-10-19 | Zeneca Ltd | Aromatic compounds |
| AU4890301A (en) | 2000-04-17 | 2001-10-30 | Dong Wha Pharmaceutical Industrial Co., Ltd. | 6-methylnicotinamide derivatives as antiviral agents |
| WO2005033079A1 (ja) | 2003-09-30 | 2005-04-14 | Eisai Co., Ltd. | ヘテロ環化合物を含有する新規な抗真菌剤 |
| CA2555402A1 (en) * | 2004-02-12 | 2005-09-01 | Celine Bonnefous | Bipyridyl amides as modulators of metabotropic glutamate receptor-5 |
| AU2006329007A1 (en) * | 2005-12-20 | 2007-06-28 | Novartis Ag | Nicotinic acid derivatives as modulators of metabotropic glutamate receptors |
| CN101321731A (zh) * | 2005-12-20 | 2008-12-10 | 诺瓦提斯公司 | 作为代谢型谷氨酸受体调节剂的烟酸衍生物 |
| CN101600715A (zh) * | 2006-12-21 | 2009-12-09 | 辉瑞产品公司 | 具有血管紧张素II受体拮抗作用和PPARγ活化活性的化合物 |
| AU2007343139A1 (en) | 2006-12-21 | 2008-07-17 | Pfizer Products Inc. | Compounds having both angiotensin II receptor antagonism and PPARy activating activities |
| KR20100033981A (ko) * | 2007-06-03 | 2010-03-31 | 벤더르빌트 유니버시티 | 벤즈아미드 대사성 글루타민산염 수용체5 양성 알로스테릭 조절자 및 이의 제조 및 사용방법 |
| US8034806B2 (en) | 2007-11-02 | 2011-10-11 | Vanderbilt University | Bicyclic mGluR5 positive allosteric modulators and methods of making and using same |
| RU2012116124A (ru) | 2009-09-21 | 2013-10-27 | Вандербилт Юниверсити | О-БЕНЗИЛ НИКОТИНАМИДНЫЕ АНАЛОГИ КАК ПОЗИТИВНЫЕ АЛЛОСТЕРИЧЕСКИЕ МОДУЛЯТОРЫ mGluR5 |
| JP5749730B2 (ja) | 2009-11-25 | 2015-07-15 | ダイナテック エンジニアリング エーエス | シリコンの生産のための反応器および方法 |
| WO2011149963A1 (en) | 2010-05-24 | 2011-12-01 | Vanderbilt University | Substituted-6-methylnicotinamides as mglur5 positive allosteric modulators |
-
2011
- 2011-05-24 WO PCT/US2011/037775 patent/WO2011149963A1/en not_active Ceased
- 2011-05-24 JP JP2013512170A patent/JP2013526610A/ja active Pending
- 2011-05-24 EP EP11787265.5A patent/EP2575461A4/en not_active Withdrawn
- 2011-05-24 CN CN2011800335387A patent/CN103037693A/zh active Pending
- 2011-05-24 CA CA2799966A patent/CA2799966A1/en not_active Abandoned
- 2011-05-24 KR KR1020127033660A patent/KR20130122531A/ko not_active Withdrawn
- 2011-05-24 EA EA201291327A patent/EA201291327A1/ru unknown
- 2011-05-24 MX MX2012013560A patent/MX2012013560A/es not_active Application Discontinuation
- 2011-05-24 US US13/114,958 patent/US8969389B2/en not_active Expired - Fee Related
- 2011-05-24 AU AU2011258389A patent/AU2011258389A1/en not_active Abandoned
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