JP2010529135A5 - - Google Patents
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- JP2010529135A5 JP2010529135A5 JP2010511277A JP2010511277A JP2010529135A5 JP 2010529135 A5 JP2010529135 A5 JP 2010529135A5 JP 2010511277 A JP2010511277 A JP 2010511277A JP 2010511277 A JP2010511277 A JP 2010511277A JP 2010529135 A5 JP2010529135 A5 JP 2010529135A5
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- optionally substituted
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- amino
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- Prior art date
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 201
- 239000001257 hydrogen Substances 0.000 claims description 201
- 125000004432 carbon atom Chemical group C* 0.000 claims description 177
- 150000002431 hydrogen Chemical group 0.000 claims description 149
- 229910052736 halogen Inorganic materials 0.000 claims description 125
- 150000002367 halogens Chemical group 0.000 claims description 125
- 150000001875 compounds Chemical class 0.000 claims description 120
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 104
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 104
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 104
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 94
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims description 94
- 125000001072 heteroaryl group Chemical group 0.000 claims description 93
- 125000003107 substituted aryl group Chemical group 0.000 claims description 90
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 89
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 65
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 62
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 62
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 62
- 125000004001 thioalkyl group Chemical group 0.000 claims description 62
- 229910052757 nitrogen Inorganic materials 0.000 claims description 61
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims description 58
- 125000001424 substituent group Chemical group 0.000 claims description 57
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 56
- 125000003342 alkenyl group Chemical group 0.000 claims description 54
- 125000000304 alkynyl group Chemical group 0.000 claims description 54
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 54
- QAWTYRYXDYHQNU-UHFFFAOYSA-N diazathiane Chemical class NSN QAWTYRYXDYHQNU-UHFFFAOYSA-N 0.000 claims description 53
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 52
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 49
- 125000005415 substituted alkoxy group Chemical group 0.000 claims description 48
- 125000000217 alkyl group Chemical group 0.000 claims description 44
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims description 41
- 125000000623 heterocyclic group Chemical group 0.000 claims description 40
- 150000003973 alkyl amines Chemical class 0.000 claims description 37
- 229930195712 glutamate Natural products 0.000 claims description 30
- 230000004044 response Effects 0.000 claims description 30
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims description 26
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 26
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 26
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 25
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 23
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 21
- 241000124008 Mammalia Species 0.000 claims description 21
- 238000010276 construction Methods 0.000 claims description 21
- 150000003839 salts Chemical class 0.000 claims description 21
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 20
- 150000001204 N-oxides Chemical class 0.000 claims description 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 18
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 16
- -1 bicyclic compound Chemical class 0.000 claims description 16
- 125000003545 alkoxy group Chemical group 0.000 claims description 14
- 150000003857 carboxamides Chemical class 0.000 claims description 13
- 125000005518 carboxamido group Chemical group 0.000 claims description 13
- 102000012777 Metabotropic Glutamate 5 Receptor Human genes 0.000 claims description 12
- 108010065028 Metabotropic Glutamate 5 Receptor Proteins 0.000 claims description 12
- 101001032838 Rattus norvegicus Metabotropic glutamate receptor 5 Proteins 0.000 claims description 12
- 201000010099 disease Diseases 0.000 claims description 12
- 210000003292 kidney cell Anatomy 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 125000004076 pyridyl group Chemical group 0.000 claims description 12
- 201000000980 schizophrenia Diseases 0.000 claims description 12
- 125000006729 (C2-C5) alkenyl group Chemical group 0.000 claims description 11
- 125000006730 (C2-C5) alkynyl group Chemical group 0.000 claims description 11
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims description 11
- 125000002837 carbocyclic group Chemical group 0.000 claims description 11
- 235000013922 glutamic acid Nutrition 0.000 claims description 11
- 239000004220 glutamic acid Substances 0.000 claims description 11
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 claims description 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 8
- 208000027534 Emotional disease Diseases 0.000 claims description 8
- 208000028017 Psychotic disease Diseases 0.000 claims description 8
- 208000035475 disorder Diseases 0.000 claims description 8
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims description 6
- PXXJHWLDUBFPOL-UHFFFAOYSA-N benzamidine Chemical group NC(=N)C1=CC=CC=C1 PXXJHWLDUBFPOL-UHFFFAOYSA-N 0.000 claims description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 229910052710 silicon Inorganic materials 0.000 claims description 6
- 239000010703 silicon Substances 0.000 claims description 6
- 208000012902 Nervous system disease Diseases 0.000 claims description 5
- 125000004429 atom Chemical group 0.000 claims description 5
- 230000004064 dysfunction Effects 0.000 claims description 5
- PXZQEOJJUGGUIB-UHFFFAOYSA-N isoindolin-1-one Chemical class C1=CC=C2C(=O)NCC2=C1 PXZQEOJJUGGUIB-UHFFFAOYSA-N 0.000 claims description 5
- 230000000926 neurological effect Effects 0.000 claims description 5
- XKJCHHZQLQNZHY-UHFFFAOYSA-N phthalimide Chemical class C1=CC=C2C(=O)NC(=O)C2=C1 XKJCHHZQLQNZHY-UHFFFAOYSA-N 0.000 claims description 5
- 208000020016 psychiatric disease Diseases 0.000 claims description 5
- YWPMKTWUFVOFPL-UHFFFAOYSA-N 3,4-dihydro-2h-isoquinolin-1-one Chemical class C1=CC=C2C(=O)NCCC2=C1 YWPMKTWUFVOFPL-UHFFFAOYSA-N 0.000 claims description 4
- QGNQEODJYRGEJX-UHFFFAOYSA-N 4h-isoquinoline-1,3-dione Chemical class C1=CC=C2C(=O)NC(=O)CC2=C1 QGNQEODJYRGEJX-UHFFFAOYSA-N 0.000 claims description 4
- 208000017194 Affective disease Diseases 0.000 claims description 4
- 206010001497 Agitation Diseases 0.000 claims description 4
- 208000000044 Amnesia Diseases 0.000 claims description 4
- 208000031091 Amnestic disease Diseases 0.000 claims description 4
- 208000019901 Anxiety disease Diseases 0.000 claims description 4
- 206010048962 Brain oedema Diseases 0.000 claims description 4
- 206010008748 Chorea Diseases 0.000 claims description 4
- 206010012289 Dementia Diseases 0.000 claims description 4
- 208000014094 Dystonic disease Diseases 0.000 claims description 4
- 208000030814 Eating disease Diseases 0.000 claims description 4
- 208000019454 Feeding and Eating disease Diseases 0.000 claims description 4
- 208000019695 Migraine disease Diseases 0.000 claims description 4
- 208000019022 Mood disease Diseases 0.000 claims description 4
- 208000016285 Movement disease Diseases 0.000 claims description 4
- 208000025966 Neurological disease Diseases 0.000 claims description 4
- 208000008589 Obesity Diseases 0.000 claims description 4
- 208000002193 Pain Diseases 0.000 claims description 4
- 206010033664 Panic attack Diseases 0.000 claims description 4
- 208000027099 Paranoid disease Diseases 0.000 claims description 4
- 230000032683 aging Effects 0.000 claims description 4
- 230000006986 amnesia Effects 0.000 claims description 4
- 230000036506 anxiety Effects 0.000 claims description 4
- 208000006752 brain edema Diseases 0.000 claims description 4
- 208000012601 choreatic disease Diseases 0.000 claims description 4
- 230000006999 cognitive decline Effects 0.000 claims description 4
- 208000010877 cognitive disease Diseases 0.000 claims description 4
- 206010012601 diabetes mellitus Diseases 0.000 claims description 4
- 235000014632 disordered eating Nutrition 0.000 claims description 4
- 208000010118 dystonia Diseases 0.000 claims description 4
- 206010015037 epilepsy Diseases 0.000 claims description 4
- 208000024714 major depressive disease Diseases 0.000 claims description 4
- 206010027599 migraine Diseases 0.000 claims description 4
- 201000003631 narcolepsy Diseases 0.000 claims description 4
- 235000020824 obesity Nutrition 0.000 claims description 4
- 208000019906 panic disease Diseases 0.000 claims description 4
- 230000000698 schizophrenic effect Effects 0.000 claims description 4
- 208000019116 sleep disease Diseases 0.000 claims description 4
- 208000020685 sleep-wake disease Diseases 0.000 claims description 4
- 208000011117 substance-related disease Diseases 0.000 claims description 4
- 125000006617 triphenylamine group Chemical group 0.000 claims description 3
- 150000003573 thiols Chemical group 0.000 claims 34
- 125000003118 aryl group Chemical group 0.000 claims 4
- NKSZCPBUWGZONP-UHFFFAOYSA-N 3,4-dihydroisoquinoline Chemical compound C1=CC=C2C=NCCC2=C1 NKSZCPBUWGZONP-UHFFFAOYSA-N 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 125000003396 thiol group Chemical group [H]S* 0.000 description 70
- 238000000034 method Methods 0.000 description 34
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 24
- MOIPGXQKZSZOQX-UHFFFAOYSA-N carbonyl bromide Chemical compound BrC(Br)=O MOIPGXQKZSZOQX-UHFFFAOYSA-N 0.000 description 12
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 8
- 0 CCCC*(*)*(C(C(C(C)=N)=C(*)**=C(C)C)=O)N Chemical compound CCCC*(*)*(C(C(C(C)=N)=C(*)**=C(C)C)=O)N 0.000 description 6
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 description 4
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- ODHXBMXNKOYIBV-UHFFFAOYSA-N triphenylamine Chemical compound C1=CC=CC=C1N(C=1C=CC=CC=1)C1=CC=CC=C1 ODHXBMXNKOYIBV-UHFFFAOYSA-N 0.000 description 3
- MCFDHXXQFUDVES-UHFFFAOYSA-N Cc1n[o]c([IH]C)n1 Chemical compound Cc1n[o]c([IH]C)n1 MCFDHXXQFUDVES-UHFFFAOYSA-N 0.000 description 2
- 230000019771 cognition Effects 0.000 description 2
- 230000037410 cognitive enhancement Effects 0.000 description 2
- 230000002708 enhancing effect Effects 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 229940126062 Compound A Drugs 0.000 description 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94168607P | 2007-06-03 | 2007-06-03 | |
| US60/941,686 | 2007-06-03 | ||
| US98504107P | 2007-11-02 | 2007-11-02 | |
| US60/985,041 | 2007-11-02 | ||
| PCT/US2008/065647 WO2008151184A1 (en) | 2007-06-03 | 2008-06-03 | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010529135A JP2010529135A (ja) | 2010-08-26 |
| JP2010529135A5 true JP2010529135A5 (enrdf_load_stackoverflow) | 2012-07-12 |
| JP5622568B2 JP5622568B2 (ja) | 2014-11-12 |
Family
ID=41480433
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010511277A Expired - Fee Related JP5622568B2 (ja) | 2007-06-03 | 2008-06-03 | ベンズアミドｍＧｌｕＲ５の正のアロステリック調節因子ならびにその作製および使用方法 |
Country Status (13)
Families Citing this family (76)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010513283A (ja) | 2006-12-15 | 2010-04-30 | アボット・ラボラトリーズ | 新規なオキサジアゾール化合物 |
| US8853392B2 (en) | 2007-06-03 | 2014-10-07 | Vanderbilt University | Benzamide mGluR5 positive allosteric modulators and methods of making and using same |
| US8034806B2 (en) | 2007-11-02 | 2011-10-11 | Vanderbilt University | Bicyclic mGluR5 positive allosteric modulators and methods of making and using same |
| GB0811643D0 (en) | 2008-06-25 | 2008-07-30 | Cancer Rec Tech Ltd | New therapeutic agents |
| TW201028421A (en) * | 2009-01-15 | 2010-08-01 | Abbott Lab | Novel benzenesulfonamides as calcium channel blockers |
| US8389536B2 (en) | 2009-10-27 | 2013-03-05 | Hoffmann-La Roche Inc. | Positive allosteric modulators (PAM) |
| US8586581B2 (en) | 2009-12-17 | 2013-11-19 | Hoffmann-La Roche Inc | Ethynyl compounds useful for treatment of CNS disorders |
| NZ600605A (en) | 2009-12-18 | 2013-08-30 | Janssen Pharmaceutica Nv | Bicyclic thiazoles as allosteric modulators of mglur5 receptors |
| CA2784830C (en) | 2009-12-18 | 2018-03-27 | Sunovion Pharmaceuticals Inc. | Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof |
| US9174953B2 (en) | 2009-12-18 | 2015-11-03 | Janssen Pharmaceutica Nv | Bicyclic thiazoles as allosteric modulators of mGluR5 receptors |
| EA021568B1 (ru) | 2009-12-23 | 2015-07-30 | Такеда Фармасьютикал Компани Лимитед | Конденсированные гетероароматические пирролидиноны как ингибиторы syk |
| US8420661B2 (en) * | 2010-04-13 | 2013-04-16 | Hoffmann-La Roche Inc. | Arylethynyl derivatives |
| CN103037693A (zh) * | 2010-05-24 | 2013-04-10 | 范德比尔特大学 | 作为mglur5正向变构调节剂的取代的6-甲基烟酰胺 |
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| JP6026525B2 (ja) | 2011-06-22 | 2016-11-16 | 武田薬品工業株式会社 | 置換６−アザ−イソインドリン−１−オン誘導体 |
| US20130123254A1 (en) | 2011-09-30 | 2013-05-16 | Barbara Biemans | Pharmaceutically acceptable mglur5 positive allosteric modulators and their methods of identification |
| UA110862C2 (uk) | 2011-10-07 | 2016-02-25 | Ф. Хоффманн-Ля Рош Аг | Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5 |
| UA110995C2 (uk) | 2011-10-07 | 2016-03-10 | Ф. Хоффманн-Ля Рош Аг | Етинільні похідні як модулятори метаботропного глутаматного рецептора |
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| UA113223C2 (xx) * | 2012-08-13 | 2016-12-26 | Арилетинілпіримідини | |
| CN104684911B (zh) | 2012-09-27 | 2017-05-10 | 霍夫曼-拉罗奇有限公司 | 芳基乙炔基衍生物 |
| EA025667B1 (ru) * | 2012-10-18 | 2017-01-30 | Ф. Хоффманн-Ля Рош Аг | ПРОИЗВОДНЫЕ ЭТИНИЛА В КАЧЕСТВЕ МОДУЛЯТОРОВ АКТИВНОСТИ РЕЦЕПТОРА mGluR5 |
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| US11919908B2 (en) | 2020-12-21 | 2024-03-05 | Incyte Corporation | Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors |
| US11958861B2 (en) | 2021-02-25 | 2024-04-16 | Incyte Corporation | Spirocyclic lactams as JAK2 V617F inhibitors |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法 |
| JP2024522189A (ja) | 2021-06-09 | 2024-06-11 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての三環式ヘテロ環 |
| CN116514790A (zh) * | 2022-01-24 | 2023-08-01 | 华东师范大学 | 一类靶向于stat3的三联芳香杂环哌嗪类小分子有机化合物及其应用 |
| AU2023213484A1 (en) * | 2022-01-27 | 2024-07-25 | Vivozon,Inc. | Pharmaceutical composition for preventing or treating mental disorder |
| US12084430B2 (en) | 2022-03-17 | 2024-09-10 | Incyte Corporation | Tricyclic urea compounds as JAK2 V617F inhibitors |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW544448B (en) * | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
| GB9823871D0 (en) * | 1998-10-30 | 1998-12-23 | Pharmacia & Upjohn Spa | 2-Amino-thiazole derivatives, process for their preparation, and their use as antitumour agents |
| CA2452159A1 (en) * | 2001-07-23 | 2003-02-06 | Galileo Laboratories, Inc. | Cytoprotective compounds, pharmaceutical and cosmetic formulations, and methods |
| AU2003249983A1 (en) * | 2002-07-18 | 2004-02-09 | Actelion Pharmaceuticals Ltd | Piperidines useful for the treatment of central nervous system disorders |
| WO2004087048A2 (en) * | 2003-03-26 | 2004-10-14 | Merck & Co. Inc. | Benzamide modulators of metabotropic glutamate receptors |
| AR046276A1 (es) * | 2003-10-07 | 2005-11-30 | Renovis Inc | Derivados de amida como ligandos de canales ionicos y composiciones farmaceuticas y metodos que los utilizan. |
| GB0324159D0 (en) * | 2003-10-15 | 2003-11-19 | Glaxo Group Ltd | Novel compounds |
| GB0325956D0 (en) * | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
| CN1950372A (zh) * | 2004-05-10 | 2007-04-18 | 万有制药株式会社 | 咪唑并吡啶化合物 |
| GB0503646D0 (en) * | 2005-02-22 | 2005-03-30 | Novartis Ag | Organic compounds |
| JP2008531690A (ja) * | 2005-02-28 | 2008-08-14 | レノビス， インコーポレイテッド | イオンチャネルリガンドとしてのアミド誘導体並びにそれを使用する医薬組成物及び方法 |
-
2008
- 2008-06-03 AU AU2008259776A patent/AU2008259776A1/en not_active Abandoned
- 2008-06-03 NZ NZ581817A patent/NZ581817A/en not_active IP Right Cessation
- 2008-06-03 JP JP2010511277A patent/JP5622568B2/ja not_active Expired - Fee Related
- 2008-06-03 WO PCT/US2008/065647 patent/WO2008151184A1/en active Application Filing
- 2008-06-03 KR KR1020097027281A patent/KR20100033981A/ko not_active Withdrawn
- 2008-06-03 CN CN200880100770.6A patent/CN101795689B/zh not_active Expired - Fee Related
- 2008-06-03 EA EA200971143A patent/EA200971143A1/ru unknown
- 2008-06-03 CA CA002689282A patent/CA2689282A1/en not_active Abandoned
- 2008-06-03 MX MX2009013169A patent/MX2009013169A/es not_active Application Discontinuation
- 2008-06-03 EP EP08770045A patent/EP2162136A4/en not_active Withdrawn
- 2008-06-03 SG SG2012074621A patent/SG185285A1/en unknown
- 2008-06-03 BR BRPI0812363-2A2A patent/BRPI0812363A2/pt not_active IP Right Cessation
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2009
- 2009-12-03 IL IL202508A patent/IL202508A0/en unknown
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