JP2015518048A5 - - Google Patents
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- Publication number
- JP2015518048A5 JP2015518048A5 JP2015515133A JP2015515133A JP2015518048A5 JP 2015518048 A5 JP2015518048 A5 JP 2015518048A5 JP 2015515133 A JP2015515133 A JP 2015515133A JP 2015515133 A JP2015515133 A JP 2015515133A JP 2015518048 A5 JP2015518048 A5 JP 2015518048A5
- Authority
- JP
- Japan
- Prior art keywords
- dimethyldispiro
- carboxamide
- amino
- salt
- compound
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 30
- 150000003839 salts Chemical class 0.000 claims 27
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 229910052736 halogen Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical group 0.000 claims 14
- 208000010877 cognitive disease Diseases 0.000 claims 8
- 208000027061 mild cognitive impairment Diseases 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- FVLGCKAZTKQUNT-NRFANRHFSA-N n-[(4'r)-2''-amino-2',2'-dimethyldispiro[cyclopropane-1,3'-chromene-4',4''-[1,3]oxazol]-6'-yl]-5-methoxypyrazine-2-carboxamide Chemical compound C1=NC(OC)=CN=C1C(=O)NC1=CC=C(OC(C)(C)C2(CC2)[C@@]23N=C(N)OC3)C2=C1 FVLGCKAZTKQUNT-NRFANRHFSA-N 0.000 claims 2
- INWIVMOTHPFWNU-NRFANRHFSA-N n-[(4s)-2-amino-2',2'-dimethyldispiro[1,3-oxazole-4,4'-chromene-3',3''-oxetan]-6'-yl]-5-chloropyrid ine-2-carboxamide Chemical compound C1OCC1([C@@]1(N=C(N)OC1)C1=C2)C(C)(C)OC1=CC=C2NC(=O)C1=CC=C(Cl)C=N1 INWIVMOTHPFWNU-NRFANRHFSA-N 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- GPWZMCGYHYETLO-UHFFFAOYSA-N C1=C2C3(N=C(N)OC3)C3(COC3)C(C)(C)OC2=CC=C1NC(=O)C1=CC=C(C#N)C=N1 Chemical compound C1=C2C3(N=C(N)OC3)C3(COC3)C(C)(C)OC2=CC=C1NC(=O)C1=CC=C(C#N)C=N1 GPWZMCGYHYETLO-UHFFFAOYSA-N 0.000 claims 1
- FSJTVQBTRXXXMC-UHFFFAOYSA-N C1=C2C3(N=C(N)OC3)C3(COC3)C(C)(C)OC2=CC=C1NC(=O)C1=CC=C(F)C=N1 Chemical compound C1=C2C3(N=C(N)OC3)C3(COC3)C(C)(C)OC2=CC=C1NC(=O)C1=CC=C(F)C=N1 FSJTVQBTRXXXMC-UHFFFAOYSA-N 0.000 claims 1
- OKNLKKUCXCACGI-UHFFFAOYSA-N C1=C2C3(N=C(N)OC3)C3(COC3)C(C)(C)OC2=CC=C1NC(=O)C1=NC=C(Br)C=N1 Chemical compound C1=C2C3(N=C(N)OC3)C3(COC3)C(C)(C)OC2=CC=C1NC(=O)C1=NC=C(Br)C=N1 OKNLKKUCXCACGI-UHFFFAOYSA-N 0.000 claims 1
- NNCFJTIUQAEALJ-UHFFFAOYSA-N C1=C2C3(N=C(N)OC3)C3(COC3)C(C)(C)OC2=CC=C1NC(=O)C1=NC=C(Cl)C=C1F Chemical compound C1=C2C3(N=C(N)OC3)C3(COC3)C(C)(C)OC2=CC=C1NC(=O)C1=NC=C(Cl)C=C1F NNCFJTIUQAEALJ-UHFFFAOYSA-N 0.000 claims 1
- SUARPGUFOBBSJS-NRFANRHFSA-N C1CC1([C@@]1(N=C(N)OC1)C1=C2)C(C)(C)OC1=CC=C2NC(=O)C1=CC=C(Cl)C=N1 Chemical compound C1CC1([C@@]1(N=C(N)OC1)C1=C2)C(C)(C)OC1=CC=C2NC(=O)C1=CC=C(Cl)C=N1 SUARPGUFOBBSJS-NRFANRHFSA-N 0.000 claims 1
- KFVQLLMGMYDUOM-NRFANRHFSA-N C1CC1([C@@]1(N=C(N)OC1)C1=C2)C(C)(C)OC1=CC=C2NC(=O)C1=CC=C(F)C=N1 Chemical compound C1CC1([C@@]1(N=C(N)OC1)C1=C2)C(C)(C)OC1=CC=C2NC(=O)C1=CC=C(F)C=N1 KFVQLLMGMYDUOM-NRFANRHFSA-N 0.000 claims 1
- CWCLNAMDVBTHAU-NRFANRHFSA-N C1OCC1([C@@]1(N=C(N)OC1)C1=C2)C(C)(C)OC1=CC=C2NC(=O)C1=CC=C(Br)C=N1 Chemical compound C1OCC1([C@@]1(N=C(N)OC1)C1=C2)C(C)(C)OC1=CC=C2NC(=O)C1=CC=C(Br)C=N1 CWCLNAMDVBTHAU-NRFANRHFSA-N 0.000 claims 1
- WTTPTTMLIGTSRC-UHFFFAOYSA-N CC1=CC(Cl)=CN=C1C(=O)NC1=CC=C(OC(C)(C)C2(COC2)C23N=C(N)OC3)C2=C1 Chemical compound CC1=CC(Cl)=CN=C1C(=O)NC1=CC=C(OC(C)(C)C2(COC2)C23N=C(N)OC3)C2=C1 WTTPTTMLIGTSRC-UHFFFAOYSA-N 0.000 claims 1
- -1 N-[(4S) -2-amino-2 ′, 2′-dimethyldispiro [1,3-oxazol-4,4′-chromene-3 ′, 3 ′′ -oxetane] -6′-yl] -5 -Chloropyridine-2-carboxamide hydrate Chemical compound 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000036571 hydration Effects 0.000 claims 1
- 238000006703 hydration reaction Methods 0.000 claims 1
- INWIVMOTHPFWNU-UHFFFAOYSA-N n-(2-amino-2',2'-dimethyldispiro[1,3-oxazole-4,4'-chromene-3',3''-oxetan]-6'-yl)-5-chloro pyridine-2-carboxamide Chemical compound C1=C2C3(N=C(N)OC3)C3(COC3)C(C)(C)OC2=CC=C1NC(=O)C1=CC=C(Cl)C=N1 INWIVMOTHPFWNU-UHFFFAOYSA-N 0.000 claims 1
- WZWNQLAVZZUSHH-NRFANRHFSA-N n-[(4s)-2-amino-2',2'-dimethyldispiro[1,3-oxazole-4,4'-chromene-3',3''-oxetan]-6'-yl]-5-methoxypy razine-2-carboxamide Chemical compound C1=NC(OC)=CN=C1C(=O)NC1=CC=C(OC(C)(C)C2(COC2)[C@@]23N=C(N)OC3)C2=C1 WZWNQLAVZZUSHH-NRFANRHFSA-N 0.000 claims 1
- WZWNQLAVZZUSHH-UHFFFAOYSA-N n-[2-amino-2',2'-dimethyldispiro[1,3-oxazole-4,4'-chromene-3',3''-oxetan]-6'-yl]-5-methoxypyrazine-2-carboxamide Chemical compound C1=NC(OC)=CN=C1C(=O)NC1=CC=C(OC(C)(C)C2(COC2)C23N=C(N)OC3)C2=C1 WZWNQLAVZZUSHH-UHFFFAOYSA-N 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261653321P | 2012-05-30 | 2012-05-30 | |
| US61/653,321 | 2012-05-30 | ||
| US201361782038P | 2013-03-14 | 2013-03-14 | |
| US61/782,038 | 2013-03-14 | ||
| PCT/US2013/043016 WO2013181202A2 (en) | 2012-05-30 | 2013-05-29 | Chromane compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015518048A JP2015518048A (ja) | 2015-06-25 |
| JP2015518048A5 true JP2015518048A5 (https=) | 2016-07-14 |
Family
ID=49674034
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015515133A Pending JP2015518048A (ja) | 2012-05-30 | 2013-05-29 | クロマン化合物 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US8975415B2 (https=) |
| EP (1) | EP2854797A4 (https=) |
| JP (1) | JP2015518048A (https=) |
| KR (1) | KR20150023536A (https=) |
| CN (1) | CN104394862A (https=) |
| AR (1) | AR091203A1 (https=) |
| AU (1) | AU2013267555A1 (https=) |
| BR (1) | BR112014029597A2 (https=) |
| CA (1) | CA2873678A1 (https=) |
| EA (1) | EA026380B1 (https=) |
| HK (1) | HK1208817A1 (https=) |
| MX (1) | MX2014014066A (https=) |
| SG (1) | SG11201407796YA (https=) |
| TW (1) | TW201408672A (https=) |
| WO (1) | WO2013181202A2 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015518048A (ja) | 2012-05-30 | 2015-06-25 | コメンティス， インコーポレイテッド | クロマン化合物 |
| TW201629025A (zh) * | 2014-10-07 | 2016-08-16 | 阿斯特捷利康公司 | 化合物及其作為ｂａｃｅ抑制劑之用途 |
| CN110818694B (zh) * | 2019-11-18 | 2023-04-21 | 上海医药工业研究院有限公司 | 艾拉普林中间体及其应用 |
| CN110724135B (zh) * | 2019-11-18 | 2023-04-28 | 上海医药工业研究院有限公司 | 一种艾拉普林中间体及其制备方法 |
| CN110713483B (zh) * | 2019-11-18 | 2023-04-07 | 上海医药工业研究院 | 艾拉普林中间体及艾拉普林的制备方法 |
| CN110790753B (zh) * | 2019-11-18 | 2023-04-07 | 上海医药工业研究院 | 艾拉普林对甲苯磺酸盐、其制备方法和应用 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1196609A2 (en) | 1999-06-28 | 2002-04-17 | Oklahoma Medical Research Foundation | Catalytically active recombinant memapsin and methods of use thereof |
| US20040121947A1 (en) | 2000-12-28 | 2004-06-24 | Oklahoma Medical Research Foundation | Compounds which inhibit beta-secretase activity and methods of use thereof |
| CA2464736A1 (en) | 2001-10-23 | 2003-05-15 | Oklahoma Medical Research Foundation | Beta-secretase inhibitors and methods of use |
| PT1699455E (pt) | 2003-12-15 | 2013-08-27 | Merck Sharp & Dohme | Inibidores de protease de aspartilo heterocíclicos |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| WO2007100536A1 (en) | 2006-02-24 | 2007-09-07 | Wyeth | DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE |
| EP2318416B1 (en) | 2008-07-28 | 2013-09-04 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
| WO2010013302A1 (ja) * | 2008-07-28 | 2010-02-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | スピロアミノジヒドロチアジン誘導体 |
| JP5444240B2 (ja) * | 2008-07-28 | 2014-03-19 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | スピロアミノジヒドロチアジン誘導体 |
| US8450308B2 (en) * | 2008-08-19 | 2013-05-28 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| CA2736130C (en) * | 2008-09-11 | 2014-01-14 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use |
| CA2753730C (en) * | 2009-03-13 | 2020-12-22 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| US8461160B2 (en) | 2009-05-08 | 2013-06-11 | Hoffmann-La Roche, Inc. | Dihydropyrimidinones |
| WO2011072064A1 (en) * | 2009-12-08 | 2011-06-16 | Array Biopharma Inc. | S piro [chroman - 4, 4 ' - imidazol] ones as beta - secretase inhibitors |
| CN102812005B (zh) * | 2010-02-24 | 2014-12-10 | 生命医药公司 | β-分泌酶抑制剂 |
| EP2547685A1 (en) * | 2010-03-15 | 2013-01-23 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta - secretase modulators |
| MX2012010657A (es) * | 2010-03-15 | 2013-02-07 | Amgen Inc | Compuestos de espiro amino-dihidrooxazina y amino-dihidrotiazina como moduladores de beta-secretasa y su uso medico. |
| US20120065195A1 (en) * | 2010-03-31 | 2012-03-15 | Clark Christopher T | Compounds for treating neurodegenerative diseases |
| WO2011130741A1 (en) | 2010-04-16 | 2011-10-20 | Array Biopharma Inc. | Compounds for treating neurodegenerative diseases |
| US20120083501A1 (en) | 2010-09-24 | 2012-04-05 | Hunt Kevin W | Compounds for treating neurodegenerative diseases |
| TW201300380A (zh) | 2010-10-19 | 2013-01-01 | Comentis Inc | 抑制β－分泌酶活性之噁二唑化合物及其使用方法 |
| WO2012071458A1 (en) | 2010-11-22 | 2012-05-31 | Array Biopharma Inc. | Heterocyclic inhibitors of beta - secretase for the treatment of neurodegenerative diseases |
| EP2643325A1 (en) | 2010-11-23 | 2013-10-02 | Amgen Inc. | Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use |
| US8415483B2 (en) | 2010-12-22 | 2013-04-09 | Astrazeneca Ab | Compounds and their use as BACE inhibitors |
| EP2673279A1 (en) | 2011-02-07 | 2013-12-18 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use |
| EP2675810A1 (en) | 2011-02-15 | 2013-12-25 | Amgen Inc. | Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use |
| US9079919B2 (en) | 2011-05-27 | 2015-07-14 | Hoffmann-La Roche Inc. | Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors |
| WO2013044092A1 (en) | 2011-09-21 | 2013-03-28 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| EP2780321B1 (en) | 2011-10-10 | 2015-12-30 | Astrazeneca AB | Mono-fluoro beta-secretase inhibitors |
| JP2015518048A (ja) | 2012-05-30 | 2015-06-25 | コメンティス， インコーポレイテッド | クロマン化合物 |
| EP2669286A1 (en) | 2012-05-31 | 2013-12-04 | Ares Trading S.A. | Spiro tetrahydro-benzothiophen derivatives useful for the treatment of neurodegenerative diseases |
-
2013
- 2013-05-29 JP JP2015515133A patent/JP2015518048A/ja active Pending
- 2013-05-29 SG SG11201407796YA patent/SG11201407796YA/en unknown
- 2013-05-29 KR KR20147036874A patent/KR20150023536A/ko not_active Withdrawn
- 2013-05-29 CA CA2873678A patent/CA2873678A1/en not_active Abandoned
- 2013-05-29 BR BR112014029597A patent/BR112014029597A2/pt not_active IP Right Cessation
- 2013-05-29 CN CN201380028374.8A patent/CN104394862A/zh active Pending
- 2013-05-29 MX MX2014014066A patent/MX2014014066A/es unknown
- 2013-05-29 EA EA201492271A patent/EA026380B1/ru not_active IP Right Cessation
- 2013-05-29 HK HK15109582.8A patent/HK1208817A1/xx unknown
- 2013-05-29 EP EP13797843.3A patent/EP2854797A4/en not_active Withdrawn
- 2013-05-29 AR ARP130101885 patent/AR091203A1/es unknown
- 2013-05-29 AU AU2013267555A patent/AU2013267555A1/en not_active Abandoned
- 2013-05-29 WO PCT/US2013/043016 patent/WO2013181202A2/en not_active Ceased
- 2013-05-30 TW TW102119181A patent/TW201408672A/zh unknown
-
2014
- 2014-02-27 US US14/192,667 patent/US8975415B2/en not_active Expired - Fee Related
-
2015
- 2015-01-22 US US14/603,110 patent/US9242973B2/en not_active Expired - Fee Related
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