JP2009514802A5 - - Google Patents
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- Publication number
- JP2009514802A5 JP2009514802A5 JP2008534914A JP2008534914A JP2009514802A5 JP 2009514802 A5 JP2009514802 A5 JP 2009514802A5 JP 2008534914 A JP2008534914 A JP 2008534914A JP 2008534914 A JP2008534914 A JP 2008534914A JP 2009514802 A5 JP2009514802 A5 JP 2009514802A5
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- oxy
- prolinamide
- methyl
- fluorophenyl
- 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
- -1 4-{[(3-Fluorophenyl) methyl] oxy} phenyl Chemical group 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 13
- 201000010099 disease Diseases 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 7
- 239000012453 solvate Substances 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 208000020925 Bipolar disease Diseases 0.000 claims 2
- 208000019022 Mood disease Diseases 0.000 claims 2
- 102000016913 Voltage-Gated Sodium Channels Human genes 0.000 claims 2
- 108010053752 Voltage-Gated Sodium Channels Proteins 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 208000011117 substance-related disease Diseases 0.000 claims 2
- JESCETIFNOFKEU-ZYMOGRSISA-N (2r)-5-[4-[(2-fluorophenyl)methoxy]phenyl]pyrrolidine-2-carboxamide Chemical compound N1[C@@H](C(=O)N)CCC1C(C=C1)=CC=C1OCC1=CC=CC=C1F JESCETIFNOFKEU-ZYMOGRSISA-N 0.000 claims 1
- OKBUYONUIPCSBT-DLBZAZTESA-N (2r,5s)-5-(4-phenylmethoxyphenyl)pyrrolidine-2-carboxamide Chemical compound N1[C@@H](C(=O)N)CC[C@H]1C(C=C1)=CC=C1OCC1=CC=CC=C1 OKBUYONUIPCSBT-DLBZAZTESA-N 0.000 claims 1
- QNXQSFGSRNYTGG-ZWKOTPCHSA-N (2r,6s)-6-[4-[(3-fluorophenyl)methoxy]phenyl]piperidine-2-carboxamide Chemical compound N1[C@@H](C(=O)N)CCC[C@H]1C(C=C1)=CC=C1OCC1=CC=CC(F)=C1 QNXQSFGSRNYTGG-ZWKOTPCHSA-N 0.000 claims 1
- IWTDYHZQFARTCR-WBAXXEDZSA-N (2s,3as,6as)-2-[4-[(2-fluorophenyl)methoxy]phenyl]-2,3,3a,4,5,6a-hexahydro-1h-pyrrolo[2,3-c]pyrrol-6-one Chemical compound FC1=CC=CC=C1COC1=CC=C([C@H]2N[C@@H]3C(=O)NC[C@@H]3C2)C=C1 IWTDYHZQFARTCR-WBAXXEDZSA-N 0.000 claims 1
- ZZDYMRPEDUYFJR-SJORKVTESA-N (2s,5r)-5-[3-cyano-4-[(2-fluorophenyl)methoxy]phenyl]pyrrolidine-2-carboxamide Chemical compound N1[C@H](C(=O)N)CC[C@@H]1C(C=C1C#N)=CC=C1OCC1=CC=CC=C1F ZZDYMRPEDUYFJR-SJORKVTESA-N 0.000 claims 1
- AXWAKFGUSYJBPY-MSOLQXFVSA-N (2s,5r)-5-[4-(2-phenylethyl)phenyl]pyrrolidine-2-carboxamide Chemical compound N1[C@H](C(=O)N)CC[C@@H]1C(C=C1)=CC=C1CCC1=CC=CC=C1 AXWAKFGUSYJBPY-MSOLQXFVSA-N 0.000 claims 1
- QNXQSFGSRNYTGG-MSOLQXFVSA-N (2s,6r)-6-[4-[(3-fluorophenyl)methoxy]phenyl]piperidine-2-carboxamide Chemical compound N1[C@H](C(=O)N)CCC[C@@H]1C(C=C1)=CC=C1OCC1=CC=CC(F)=C1 QNXQSFGSRNYTGG-MSOLQXFVSA-N 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 208000032841 Bulimia Diseases 0.000 claims 1
- 206010006550 Bulimia nervosa Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 0 C*C(*1)C(*)CC(C)CC1C(C(C)C(C)C1*)NC1C(N(*)*)=O Chemical compound C*C(*1)C(*)CC(C)CC1C(C(C)C(C)C1*)NC1C(N(*)*)=O 0.000 description 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0520561A GB0520561D0 (en) | 2005-10-10 | 2005-10-10 | Novel compounds |
| GB0520561.2 | 2005-10-10 | ||
| GB0523028A GB0523028D0 (en) | 2005-11-11 | 2005-11-11 | Novel compounds |
| GB0523028.9 | 2005-11-11 | ||
| GB0603899.6 | 2006-02-27 | ||
| GB0603899A GB0603899D0 (en) | 2006-02-27 | 2006-02-27 | Novel compounds |
| GB0618336.2 | 2006-09-18 | ||
| GB0618336A GB0618336D0 (en) | 2006-09-18 | 2006-09-18 | Novel compounds |
| PCT/EP2006/009746 WO2007042250A1 (en) | 2005-10-10 | 2006-10-06 | Prolinamide derivatives as sodium channel modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009514802A JP2009514802A (ja) | 2009-04-09 |
| JP2009514802A5 true JP2009514802A5 (enExample) | 2009-11-26 |
| JP5139307B2 JP5139307B2 (ja) | 2013-02-06 |
Family
ID=37546927
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008534914A Expired - Fee Related JP5139307B2 (ja) | 2005-10-10 | 2006-10-06 | ナトリウムチャネルモジュレーターとしてのプロリンアミド誘導体 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US7855218B2 (enExample) |
| EP (1) | EP1943216B1 (enExample) |
| JP (1) | JP5139307B2 (enExample) |
| AT (1) | ATE472529T1 (enExample) |
| DE (1) | DE602006015215D1 (enExample) |
| WO (1) | WO2007042250A1 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7855218B2 (en) | 2005-10-10 | 2010-12-21 | Convergence Pharmaceuticals Limited | Compounds |
| TW200730494A (en) * | 2005-10-10 | 2007-08-16 | Glaxo Group Ltd | Novel compounds |
| US8143306B2 (en) * | 2005-10-10 | 2012-03-27 | Convergence Pharmaceuticals Limited | Methods of treating bipolar disorders |
| GB0701365D0 (en) * | 2007-01-24 | 2007-03-07 | Glaxo Group Ltd | Novel pharmaceutical compositions |
| GB0701366D0 (en) * | 2007-01-24 | 2007-03-07 | Glaxo Group Ltd | Novel pharmaceutical compositions |
| JP5121346B2 (ja) * | 2007-08-07 | 2013-01-16 | 国立大学法人 長崎大学 | 光学活性プロリンエステル誘導体およびｎ−ホルミル光学活性プロリン誘導体の製造方法 |
| GB0808747D0 (en) * | 2008-05-14 | 2008-06-18 | Glaxo Wellcome Mfg Pte Ltd | Novel compounds |
| WO2011015537A1 (en) * | 2009-08-05 | 2011-02-10 | Glaxo Group Limited | Co-therapy for the treatment of epilepsy and related disorders |
| HRP20150491T1 (hr) | 2009-09-14 | 2015-08-14 | Convergence Pharmaceuticals Limited | PROCES PRIPREME DERIVATA α-KARBOKSAMIDA |
| CN102180823B (zh) * | 2011-03-12 | 2016-03-02 | 浙江华海药业股份有限公司 | 一种精制脯氨酰胺的方法 |
| GB201122113D0 (en) | 2011-12-22 | 2012-02-01 | Convergence Pharmaceuticals | Novel compounds |
| GB201209015D0 (en) | 2012-05-22 | 2012-07-04 | Convergence Pharmaceuticals | Novel compounds |
| CN106255679B (zh) | 2014-02-27 | 2019-09-06 | 默克专利有限公司 | 用作nav通道抑制剂的杂环化合物及其用途 |
| ES2912881T3 (es) | 2014-12-23 | 2022-05-30 | Convergence Pharmaceuticals | Procedimiento para preparar derivados de alfa-carboxamida pirrolidina |
| US9624169B2 (en) * | 2015-03-27 | 2017-04-18 | Scifluor Life Sciences, Inc. | Aryl- and heteroaryl-pyrrolidine-2-carboxamide compounds |
| CA3062884A1 (en) * | 2017-05-19 | 2018-11-22 | Biogen Ma Inc. | Novel crystalline forms |
| EP3691634A4 (en) | 2017-10-05 | 2021-03-31 | Biogen Inc. | PROCESS FOR THE PREPARATION OF PYRROLIDINE ALPHA-CARBOXAMIDE DERIVATIVES |
| CA3077088A1 (en) | 2017-10-10 | 2019-04-18 | Biogen Inc. | Process for preparing spiro derivatives |
| AU2020320034A1 (en) | 2019-07-30 | 2022-03-03 | Karl-Franzens-Universität Graz | Inhibitors of human ATGL |
| CN112679407B (zh) * | 2021-03-17 | 2021-06-04 | 南京桦冠生物技术有限公司 | 一种手性5-取代脯氨酸类化合物的制备方法 |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL94466A (en) * | 1989-05-25 | 1995-01-24 | Erba Carlo Spa | Pharmaceutical preparations containing the history of A-amino carboxamide N-phenylalkyl are converted into such new compounds and their preparation |
| US6201016B1 (en) * | 1994-06-27 | 2001-03-13 | Cytomed Incorporated | Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders |
| GB9727523D0 (en) * | 1997-12-31 | 1998-02-25 | Pharmacia & Upjohn Spa | Alpha-aminoamide derivatives useful as analgesic agents |
| RU2001129155A (ru) | 1999-03-26 | 2003-08-10 | Еро-Сельтик С.А. (Lu) | Соединения с арильными заместителями (варианты), фармацевтическая композиция и способ лечения расстройства, чувствительного к блокаде натриевых каналов у млекопитающего, способ лечения, профилактики различных заболеваний или уменьшения интенсивности гибели или потери нейронов (варианты), способ облегчения или предупреждения эпилептических припадков у животного (варианты), соединение - радиоактивный лиганд для участка связывания в натриевом канале |
| GB9923748D0 (en) * | 1999-10-07 | 1999-12-08 | Glaxo Group Ltd | Chemical compounds |
| GB0115517D0 (en) * | 2001-06-25 | 2001-08-15 | Ferring Bv | Novel antidiabetic agents |
| TW200404796A (en) * | 2002-08-19 | 2004-04-01 | Ono Pharmaceutical Co | Nitrogen-containing compound |
| MY134480A (en) * | 2002-09-20 | 2007-12-31 | Hoffmann La Roche | 4-pyrrolidino-phenyl-benzyl ether derivatives |
| AR044503A1 (es) | 2003-03-18 | 2005-09-14 | Merck & Co Inc | Triazoles sustituidos con biarilo como bloqueantes del canal de sodio |
| CN101333192A (zh) | 2003-04-03 | 2008-12-31 | 默克公司 | 作为钠通道阻滞剂的联芳基取代吡唑 |
| JP2006523701A (ja) | 2003-04-18 | 2006-10-19 | メルク エンド カムパニー インコーポレーテッド | ナトリウムチャネルブロッカーとしてのビアリール置換チアゾール、オキサゾール、およびイミダゾール |
| WO2005000309A2 (en) | 2003-06-27 | 2005-01-06 | Ionix Pharmaceuticals Limited | Chemical compounds |
| EP1524265A1 (en) * | 2003-10-15 | 2005-04-20 | Newron Pharmaceuticals S.p.A. | Prolinamide derivatives as sodium and/or calcium channel blockers or selective MAO-B inhibitors |
| WO2005100334A1 (en) * | 2004-04-14 | 2005-10-27 | Pfizer Products Inc. | Dipeptidyl peptidase-iv inhibitors |
| WO2006119451A1 (en) | 2005-05-04 | 2006-11-09 | Vertex Pharmaceuticals Incorporated | Pyrimidines and pyrazines useful as modulators of ion channels |
| JP2008540438A (ja) | 2005-05-04 | 2008-11-20 | 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 | イオンチャネルのモジュレーターとして有用なピリジン |
| JP2008540665A (ja) | 2005-05-19 | 2008-11-20 | 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 | イオンチャネルのモジュレーターとして有用なビアリール |
| PT1928886E (pt) * | 2005-09-09 | 2011-07-14 | Glaxosmithkline Llc | Derivados de piridina e sua utilização para o tratamento de distúrbios psicóticos |
| TW200730494A (en) * | 2005-10-10 | 2007-08-16 | Glaxo Group Ltd | Novel compounds |
| US7855218B2 (en) | 2005-10-10 | 2010-12-21 | Convergence Pharmaceuticals Limited | Compounds |
| TW200728258A (en) * | 2005-10-10 | 2007-08-01 | Glaxo Group Ltd | Novel compounds |
| EP2117538A1 (en) | 2007-01-24 | 2009-11-18 | Glaxo Group Limited | Pharmaceutical compositions comprising 2-methoxy-5- (5-trifluoromethyl-tetrazol-i-yl-benzyl) - (2s-phenyl-piperidin-3s-yl-) |
| GB0701366D0 (en) | 2007-01-24 | 2007-03-07 | Glaxo Group Ltd | Novel pharmaceutical compositions |
| GB0701365D0 (en) | 2007-01-24 | 2007-03-07 | Glaxo Group Ltd | Novel pharmaceutical compositions |
| GB0706630D0 (en) | 2007-04-04 | 2007-05-16 | Glaxo Group Ltd | Novel compounds |
-
2006
- 2006-10-06 US US11/570,556 patent/US7855218B2/en active Active
- 2006-10-06 JP JP2008534914A patent/JP5139307B2/ja not_active Expired - Fee Related
- 2006-10-06 DE DE602006015215T patent/DE602006015215D1/de active Active
- 2006-10-06 WO PCT/EP2006/009746 patent/WO2007042250A1/en not_active Ceased
- 2006-10-06 EP EP06792409A patent/EP1943216B1/en active Active
- 2006-10-06 AT AT06792409T patent/ATE472529T1/de not_active IP Right Cessation