JP2012520324A5 - - Google Patents
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- JP2012520324A5 JP2012520324A5 JP2011554237A JP2011554237A JP2012520324A5 JP 2012520324 A5 JP2012520324 A5 JP 2012520324A5 JP 2011554237 A JP2011554237 A JP 2011554237A JP 2011554237 A JP2011554237 A JP 2011554237A JP 2012520324 A5 JP2012520324 A5 JP 2012520324A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- halo
- cycloalkyl
- heteroaryl
- 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
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- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 73
- 125000001072 heteroaryl group Chemical group 0.000 claims 63
- 125000004093 cyano group Chemical group *C#N 0.000 claims 49
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 46
- 125000003118 aryl group Chemical group 0.000 claims 45
- 125000001424 substituent group Chemical group 0.000 claims 40
- 229910052736 halogen Inorganic materials 0.000 claims 38
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 36
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 32
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 31
- 125000000217 alkyl group Chemical group 0.000 claims 28
- 150000001875 compounds Chemical class 0.000 claims 23
- 150000002367 halogens Chemical class 0.000 claims 23
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 22
- -1 halo (C1-C6) Alkyl Chemical group 0.000 claims 20
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 19
- 229910052757 nitrogen Inorganic materials 0.000 claims 16
- 125000001246 bromo group Chemical group Br* 0.000 claims 15
- 125000001309 chloro group Chemical group Cl* 0.000 claims 15
- 125000005843 halogen group Chemical group 0.000 claims 15
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 14
- 125000005154 alkyl sulfonyl amino alkyl group Chemical group 0.000 claims 13
- 125000005842 heteroatom Chemical group 0.000 claims 13
- 229910052717 sulfur Inorganic materials 0.000 claims 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 8
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 239000011593 sulfur Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 7
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 6
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000006554 (C4-C8) cycloalkenyl group Chemical group 0.000 claims 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 5
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000002619 bicyclic group Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000002950 monocyclic group Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 125000003367 polycyclic group Chemical group 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 208000024827 Alzheimer disease Diseases 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- DMEGYFMYUHOHGS-UHFFFAOYSA-N heptamethylene Natural products C1CCCCCC1 DMEGYFMYUHOHGS-UHFFFAOYSA-N 0.000 claims 3
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 125000001544 thienyl group Chemical group 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- RGSFGYAAUTVSQA-UHFFFAOYSA-N Cyclopentane Chemical compound C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 claims 2
- 208000010412 Glaucoma Diseases 0.000 claims 2
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 2
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- HGCIXCUEYOPUTN-UHFFFAOYSA-N cyclohexene Chemical compound C1CCC=CC1 HGCIXCUEYOPUTN-UHFFFAOYSA-N 0.000 claims 2
- NNBZCPXTIHJBJL-UHFFFAOYSA-N decalin Chemical compound C1CCCC2CCCCC21 NNBZCPXTIHJBJL-UHFFFAOYSA-N 0.000 claims 2
- PQNFLJBBNBOBRQ-UHFFFAOYSA-N indane Chemical compound C1=CC=C2CCCC2=C1 PQNFLJBBNBOBRQ-UHFFFAOYSA-N 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000005493 quinolyl group Chemical group 0.000 claims 2
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 2
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 claims 1
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims 1
- VDFVNEFVBPFDSB-UHFFFAOYSA-N 1,3-dioxane Chemical compound C1COCOC1 VDFVNEFVBPFDSB-UHFFFAOYSA-N 0.000 claims 1
- XXOQJWXDRPURJK-UHFFFAOYSA-N 2,3,4,5-tetrahydro-1-benzoxepine Chemical compound O1CCCCC2=CC=CC=C21 XXOQJWXDRPURJK-UHFFFAOYSA-N 0.000 claims 1
- GKNLVRYWFYXZFU-UHFFFAOYSA-N 2,3-dihydro-1h-phenalene Chemical compound C1=CC(CCC2)=C3C2=CC=CC3=C1 GKNLVRYWFYXZFU-UHFFFAOYSA-N 0.000 claims 1
- HTMGQIXFZMZZKD-UHFFFAOYSA-N 5,6,7,8-tetrahydroisoquinoline Chemical compound N1=CC=C2CCCCC2=C1 HTMGQIXFZMZZKD-UHFFFAOYSA-N 0.000 claims 1
- YQDGQEKUTLYWJU-UHFFFAOYSA-N 5,6,7,8-tetrahydroquinoline Chemical compound C1=CC=C2CCCCC2=N1 YQDGQEKUTLYWJU-UHFFFAOYSA-N 0.000 claims 1
- HEOQXHNKRXRCTO-UHFFFAOYSA-N 6,7,8,9-tetrahydro-5h-benzo[7]annulene Chemical compound C1CCCCC2=CC=CC=C21 HEOQXHNKRXRCTO-UHFFFAOYSA-N 0.000 claims 1
- 208000024667 ABeta amyloidosis, Dutch type Diseases 0.000 claims 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 206010039966 Senile dementia Diseases 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 235000018936 Vitellaria paradoxa Nutrition 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 1
- 230000006999 cognitive decline Effects 0.000 claims 1
- 230000003412 degenerative effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000036536 dutch type ABeta amyloidosis Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- UHHKSVZZTYJVEG-UHFFFAOYSA-N oxepane Chemical compound C1CCCOCC1 UHHKSVZZTYJVEG-UHFFFAOYSA-N 0.000 claims 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- CXWXQJXEFPUFDZ-UHFFFAOYSA-N tetralin Chemical compound C1=CC=C2CCCCC2=C1 CXWXQJXEFPUFDZ-UHFFFAOYSA-N 0.000 claims 1
- 150000003852 triazoles Chemical class 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21014609P | 2009-03-13 | 2009-03-13 | |
| US61/210,146 | 2009-03-13 | ||
| US30754210P | 2010-02-24 | 2010-02-24 | |
| US61/307,542 | 2010-02-24 | ||
| PCT/US2010/027173 WO2010105179A2 (en) | 2009-03-13 | 2010-03-12 | Inhibitors of beta-secretase |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015080118A Division JP2015147792A (ja) | 2009-03-13 | 2015-04-09 | β−セクレターゼ阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012520324A JP2012520324A (ja) | 2012-09-06 |
| JP2012520324A5 true JP2012520324A5 (enExample) | 2013-04-25 |
| JP5731414B2 JP5731414B2 (ja) | 2015-06-10 |
Family
ID=42664888
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011554237A Expired - Fee Related JP5731414B2 (ja) | 2009-03-13 | 2010-03-12 | β−セクレターゼ阻害剤 |
| JP2015080118A Pending JP2015147792A (ja) | 2009-03-13 | 2015-04-09 | β−セクレターゼ阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015080118A Pending JP2015147792A (ja) | 2009-03-13 | 2015-04-09 | β−セクレターゼ阻害剤 |
Country Status (28)
| Country | Link |
|---|---|
| US (3) | US8633212B2 (enExample) |
| EP (2) | EP2406240B1 (enExample) |
| JP (2) | JP5731414B2 (enExample) |
| KR (2) | KR101908255B1 (enExample) |
| CN (1) | CN102348698B (enExample) |
| AP (1) | AP2866A (enExample) |
| AR (1) | AR075854A1 (enExample) |
| AU (1) | AU2010223937B2 (enExample) |
| BR (1) | BRPI1009333B8 (enExample) |
| CA (1) | CA2753730C (enExample) |
| CO (1) | CO6450683A2 (enExample) |
| DK (1) | DK2406240T3 (enExample) |
| EA (1) | EA020875B1 (enExample) |
| EC (1) | ECSP11011398A (enExample) |
| ES (1) | ES2571057T3 (enExample) |
| GE (1) | GEP20135964B (enExample) |
| IL (1) | IL214226A (enExample) |
| MA (1) | MA33240B1 (enExample) |
| MX (1) | MX2011009571A (enExample) |
| NZ (1) | NZ594230A (enExample) |
| PE (1) | PE20120219A1 (enExample) |
| PT (1) | PT2406240E (enExample) |
| SG (1) | SG173466A1 (enExample) |
| TN (1) | TN2011000400A1 (enExample) |
| TW (1) | TWI464153B (enExample) |
| UY (1) | UY32490A (enExample) |
| WO (1) | WO2010105179A2 (enExample) |
| ZA (2) | ZA201106002B (enExample) |
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2324032B1 (en) | 2008-08-19 | 2014-10-01 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| EA020875B1 (ru) | 2009-03-13 | 2015-02-27 | Вайтаи Фармасьютиклз, Инк. | Ингибиторы бета-секретазы |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| US8889703B2 (en) | 2010-02-24 | 2014-11-18 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| 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 |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| US9346827B2 (en) | 2011-02-07 | 2016-05-24 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use |
| US8962859B2 (en) | 2011-02-15 | 2015-02-24 | Amgen Inc. | Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use |
| JP2014526560A (ja) | 2011-09-21 | 2014-10-06 | アムジエン・インコーポレーテツド | β‐セクレターゼ調節因子としてのアミノオキサジン化合物およびアミノジヒドロチアジン化合物および使用方法 |
| WO2013054108A1 (en) | 2011-10-10 | 2013-04-18 | Astrazeneca Ab | Mono-fluoro beta-secretase inhibitors |
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| AR091203A1 (es) | 2012-05-30 | 2015-01-21 | Astellas Pharma Inc | Compuestos de cromano |
| EP2669286A1 (en) * | 2012-05-31 | 2013-12-04 | Ares Trading S.A. | Spiro tetrahydro-benzothiophen derivatives useful for the treatment of neurodegenerative diseases |
| US9000184B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cyclohexane-1,2′-naphthalene-1′,2″-imidazol compounds and their use as BACE inhibitors |
| US9000182B2 (en) * | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | 2H-imidazol-4-amine compounds and their use as BACE inhibitors |
| US9000185B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cycloalkyl ether compounds and their use as BACE inhibitors |
| US9000183B2 (en) * | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cyclohexane-1,2′-indene-1′,2″-imidazol compounds and their use as BACE inhibitors |
| US10548882B2 (en) * | 2012-06-21 | 2020-02-04 | Astrazeneca Ab | Camsylate salt |
| TW201422592A (zh) | 2012-08-27 | 2014-06-16 | Boehringer Ingelheim Int | β－分泌酶抑制劑 |
| EP2900639B1 (en) | 2012-09-27 | 2017-08-16 | Portola Pharmaceuticals, Inc. | Bicyclic dihydropyridone kinase inhibitors |
| EP2900650A1 (en) | 2012-09-28 | 2015-08-05 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| WO2014078314A1 (en) | 2012-11-15 | 2014-05-22 | Amgen Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| US10550327B2 (en) | 2012-11-21 | 2020-02-04 | Merck Patent Gmbh | Polymerisable compounds and the use thereof in liquid-crystal displays |
| WO2014081558A1 (en) | 2012-11-21 | 2014-05-30 | Boehringer Ingelheim International Gmbh | PROCESS FOR MAKING N-SULFINYL a-AMINO AMIDES |
| EP2759310B2 (en) | 2013-01-28 | 2023-11-08 | Mölnlycke Health Care AB | Suction device |
| US9353089B2 (en) | 2013-03-26 | 2016-05-31 | Saint Louis University | Compositions and methods for the treatment of malaria |
| AR102202A1 (es) | 2014-10-07 | 2017-02-08 | Astrazeneca Ab | Compuestos de oxazol y su uso como inhibidores de bace de oxazol |
| JP6319805B2 (ja) * | 2014-10-08 | 2018-05-09 | 田岡化学工業株式会社 | スピロビフルオレン骨格を有するジオール化合物およびその製造方法 |
| CN106083764B (zh) * | 2016-07-11 | 2018-09-18 | 上海皓元生物医药科技有限公司 | 一种用于制备axl抑制剂的高纯度中间体的手性拆分方法 |
| US11505534B2 (en) | 2017-05-16 | 2022-11-22 | The University Of Chicago | Highly diastereoselective construction of the 4,5-spirocycle via palladium-catalyzed intramolecular alkenylation |
| WO2018230555A1 (ja) * | 2017-06-14 | 2018-12-20 | 日本曹達株式会社 | オキサジアゾリン化合物および有害生物防除剤 |
| KR101969528B1 (ko) | 2017-09-29 | 2019-04-16 | 에스케이텔레콤 주식회사 | 터치 디스플레이를 제어하는 장치와 방법 및 터치 디스플레이 시스템 |
| US11760701B2 (en) | 2018-02-27 | 2023-09-19 | The Research Foundation For The State University Of New Yrok | Difluoromethoxylation and trifluoromethoxylation compositions and methods for synthesizing same |
| CN108675922B (zh) * | 2018-06-27 | 2021-04-27 | 沅江华龙催化科技有限公司 | 一种螺环化合物及其合成方法 |
| CN108675923B (zh) * | 2018-06-27 | 2021-04-27 | 沅江华龙催化科技有限公司 | 一种由环酮化合物与2-芳基丙烯及二甲亚砜共同构建螺环化合物的方法 |
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- 2010-03-12 WO PCT/US2010/027173 patent/WO2010105179A2/en not_active Ceased
- 2010-03-12 JP JP2011554237A patent/JP5731414B2/ja not_active Expired - Fee Related
- 2010-03-12 AP AP2011005913A patent/AP2866A/xx active
- 2010-03-12 PT PT107086845T patent/PT2406240E/pt unknown
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