JP2008516945A5 - - Google Patents
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- Publication number
- JP2008516945A5 JP2008516945A5 JP2007536655A JP2007536655A JP2008516945A5 JP 2008516945 A5 JP2008516945 A5 JP 2008516945A5 JP 2007536655 A JP2007536655 A JP 2007536655A JP 2007536655 A JP2007536655 A JP 2007536655A JP 2008516945 A5 JP2008516945 A5 JP 2008516945A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- heterocyclyl
- nhc
- tautomer
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 152
- 125000003118 aryl group Chemical group 0.000 claims 62
- 125000000623 heterocyclic group Chemical group 0.000 claims 57
- 150000001875 compounds Chemical class 0.000 claims 33
- 238000001727 in vivo Methods 0.000 claims 27
- 239000002243 precursor Substances 0.000 claims 27
- 150000003839 salts Chemical class 0.000 claims 27
- 229910052799 carbon Inorganic materials 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 150000002367 halogens Chemical class 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 11
- 208000024827 Alzheimer disease Diseases 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 206010012289 Dementia Diseases 0.000 claims 6
- -1 S (═O) NH Inorganic materials 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000006720 (C1-C6) alkyl (C6-C10) aryl group Chemical group 0.000 claims 5
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims 5
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 5
- 125000006717 (C3-C10) cycloalkenyl group Chemical group 0.000 claims 4
- 125000001831 (C6-C10) heteroaryl group Chemical group 0.000 claims 4
- 125000005466 alkylenyl group Chemical group 0.000 claims 4
- 208000010877 cognitive disease Diseases 0.000 claims 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 230000002792 vascular Effects 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 2
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 2
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 2
- 206010059245 Angiopathy Diseases 0.000 claims 2
- 102100021257 Beta-secretase 1 Human genes 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 2
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 2
- 208000028698 Cognitive impairment Diseases 0.000 claims 2
- 201000010374 Down Syndrome Diseases 0.000 claims 2
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 claims 2
- 206010033799 Paralysis Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 206010036631 Presenile dementia Diseases 0.000 claims 2
- 206010039966 Senile dementia Diseases 0.000 claims 2
- 206010044688 Trisomy 21 Diseases 0.000 claims 2
- 230000001054 cortical effect Effects 0.000 claims 2
- 230000007850 degeneration Effects 0.000 claims 2
- 230000003412 degenerative effect Effects 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 206010027175 memory impairment Diseases 0.000 claims 2
- 208000027061 mild cognitive impairment Diseases 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 230000007170 pathology Effects 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- XEXHWKWBGQYXIL-UHFFFAOYSA-N 2-amino-6-[2-[3-(3-methoxyphenyl)phenyl]-3-bicyclo[2.2.1]hept-5-enyl]-3-methylpyrimidin-4-one Chemical compound COC1=CC=CC(C=2C=C(C=CC=2)C2C(C3CC2C=C3)C=2N=C(N)N(C)C(=O)C=2)=C1 XEXHWKWBGQYXIL-UHFFFAOYSA-N 0.000 claims 1
- MPIIEWIMHZUOBG-UHFFFAOYSA-N 2-amino-6-[[3-(3-methoxyphenyl)phenoxy]methyl]-3-methylpyrimidin-4-one Chemical compound COC1=CC=CC(C=2C=C(OCC=3N=C(N)N(C)C(=O)C=3)C=CC=2)=C1 MPIIEWIMHZUOBG-UHFFFAOYSA-N 0.000 claims 1
- 229940122041 Cholinesterase inhibitor Drugs 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000000544 cholinesterase inhibitor Substances 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000003695 memory enhancer Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 230000001777 nootropic effect Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US61930904P | 2004-10-15 | 2004-10-15 | |
| PCT/SE2005/001533 WO2006041404A1 (en) | 2004-10-15 | 2005-10-14 | Substituted amino-compounds and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008516945A JP2008516945A (ja) | 2008-05-22 |
| JP2008516945A5 true JP2008516945A5 (https=) | 2008-11-20 |
Family
ID=36148580
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007536655A Pending JP2008516945A (ja) | 2004-10-15 | 2005-10-14 | 置換されたアミノ化合物およびそれらの使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20090221579A1 (https=) |
| EP (1) | EP1802587A4 (https=) |
| JP (1) | JP2008516945A (https=) |
| CN (1) | CN101084199A (https=) |
| WO (1) | WO2006041404A1 (https=) |
Families Citing this family (72)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| PE20070135A1 (es) | 2005-06-14 | 2007-03-09 | Schering Corp | Compuestos heterociclicos como inhibidores de aspartil proteasas |
| ATE489370T1 (de) | 2005-06-14 | 2010-12-15 | Schering Corp | Herstellung und verwendung von verbindungen als aspartylproteasehemmer |
| WO2006138265A2 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Heterocyclic aspartyl protease inhibitors, preparation and use thereof |
| KR20080025079A (ko) | 2005-06-14 | 2008-03-19 | 쉐링 코포레이션 | 아스파르틸 프로테아제 억제제 |
| AU2006259675A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Aspartyl protease inhibitors |
| CA2628074C (en) | 2005-10-25 | 2014-01-14 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| JP2009515950A (ja) * | 2005-11-15 | 2009-04-16 | アストラゼネカ・アクチエボラーグ | 新規な２−アミノピリミジン誘導体およびその使用 |
| CN101360721A (zh) * | 2005-11-15 | 2009-02-04 | 阿斯利康(瑞典)有限公司 | 新颖的2-氨基嘧啶酮衍生物或2-氨基吡啶酮衍生物及其用途 |
| AR058381A1 (es) * | 2005-12-19 | 2008-01-30 | Astrazeneca Ab | Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica |
| CN101460480A (zh) * | 2006-04-05 | 2009-06-17 | 阿斯利康(瑞典)有限公司 | 2-氨基嘧啶-4-酮类化合物及其用于治疗或预防Aβ相关病理的用途 |
| PE20080155A1 (es) * | 2006-06-12 | 2008-03-10 | Schering Corp | Compuestos heterociclicos como inhibidores de aspartil-proteasa |
| TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
| CN100439343C (zh) * | 2006-08-04 | 2008-12-03 | 复旦大学 | 2-烷基硫-5-烷基-6-(1-氰基芳甲基)取代尿嘧啶类化合物及其制备方法和用途 |
| US20100016341A1 (en) * | 2006-12-12 | 2010-01-21 | Zhaoning Zhu | Aspartyl protease inhibitors containing a tricyclic ring system |
| JP2010512389A (ja) | 2006-12-12 | 2010-04-22 | シェーリング コーポレイション | アスパルチルプロテアーゼ阻害剤 |
| US8653067B2 (en) | 2007-04-24 | 2014-02-18 | Shionogi & Co., Ltd. | Pharmaceutical composition for treating Alzheimer's disease |
| JP5383484B2 (ja) * | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | 環式基で置換されたアミノジヒドロチアジン誘導体 |
| US8222264B2 (en) * | 2007-07-06 | 2012-07-17 | Boehringer Ingelheim International Gmbh | Substituted amino-quinazolinones, medicaments comprising said compound, their use and their method of manufacture |
| PL2233474T3 (pl) | 2008-01-18 | 2015-12-31 | Eisai R&D Man Co Ltd | Skondensowana pochodna aminodihydrotiazyny |
| TWI431004B (zh) * | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Ｂａｃｅ抑制劑 |
| KR101324426B1 (ko) | 2008-06-13 | 2013-10-31 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
| CN102105475B (zh) | 2008-07-28 | 2014-04-09 | 卫材R&D管理有限公司 | 螺氨基二氢噻嗪衍生物 |
| MY148558A (en) | 2008-09-11 | 2013-04-30 | Amgen Inc | Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use |
| JP5666304B2 (ja) | 2008-09-30 | 2015-02-12 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 新規な縮合アミノジヒドロチアジン誘導体 |
| CN102186841A (zh) | 2008-10-22 | 2011-09-14 | 盐野义制药株式会社 | 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物 |
| TW201020244A (en) | 2008-11-14 | 2010-06-01 | Astrazeneca Ab | New compounds |
| EP2415756A4 (en) | 2009-03-31 | 2012-08-29 | Shionogi & Co | ISOTHIOROUS DERIVATIVES OR ISO-HARVEST DERIVATIVES WITH BACE1-HEMMENDER EFFECT |
| US8461160B2 (en) * | 2009-05-08 | 2013-06-11 | Hoffmann-La Roche, Inc. | Dihydropyrimidinones |
| GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| GB0912777D0 (en) * | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
| EP2281824A1 (en) | 2009-08-07 | 2011-02-09 | Noscira, S.A. | Furan-imidazolone derivatives, for the treatment of cognitive, neurodegenerative or neuronal diseases or disorders |
| EP2485590B1 (en) | 2009-10-08 | 2015-01-07 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| WO2011044187A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US7964594B1 (en) * | 2009-12-10 | 2011-06-21 | Hoffmann-La Roche Inc. | Amino oxazine derivatives |
| MX2012006491A (es) | 2009-12-11 | 2012-07-03 | Shionogi & Co | Derivados de oxazina. |
| UA103272C2 (uk) * | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2 |
| EP2547685A1 (en) | 2010-03-15 | 2013-01-23 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta - secretase modulators |
| US8497264B2 (en) | 2010-03-15 | 2013-07-30 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| US8815881B2 (en) | 2010-08-09 | 2014-08-26 | Hoffmann-La Roche Inc. | 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds |
| JP5816630B2 (ja) | 2010-10-29 | 2015-11-18 | 塩野義製薬株式会社 | ナフチリジン誘導体 |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
| EP2643299B1 (en) | 2010-11-22 | 2016-06-22 | Noscira, S.A. | Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions |
| US8957083B2 (en) | 2010-11-23 | 2015-02-17 | Amgen Inc. | Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use |
| 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 |
| ES2624288T3 (es) | 2011-01-21 | 2017-07-13 | Eisai R&D Management Co., Ltd. | Métodos y compuestos útiles en la síntesis de derivados de aminodihidrotiazina condensados |
| US8399459B2 (en) * | 2011-02-02 | 2013-03-19 | Hoffmann-La Roche Inc. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| 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 |
| EP2675810A1 (en) | 2011-02-15 | 2013-12-25 | Amgen Inc. | Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use |
| EP2694489B1 (en) | 2011-04-07 | 2017-09-06 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| BR112013026341A2 (pt) * | 2011-04-13 | 2019-09-24 | Merck Sharp & Dohe Corp | composto, composição farmacêutica, e, método para tratar, prevenir e/ou atrasar o início de uma doença ou patologia |
| US8883779B2 (en) | 2011-04-26 | 2014-11-11 | Shinogi & Co., Ltd. | Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them |
| CN103874496A (zh) | 2011-08-22 | 2014-06-18 | 默沙东公司 | 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途 |
| ES2861268T3 (es) | 2011-09-20 | 2021-10-06 | Basf Se | Moduladores de bajo peso molecular del receptor de mentol frío TRPM8 y su uso |
| WO2013044092A1 (en) | 2011-09-21 | 2013-03-28 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| UA113438C2 (xx) * | 2012-05-24 | 2017-01-25 | 5-аміно$1,4]тіазини як інгібітори бета-секретази 1 | |
| WO2014010748A1 (en) * | 2012-07-10 | 2014-01-16 | Shionogi & Co., Ltd. | Cyclopropane derivative having bace1 inhibiting activity |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| WO2014078314A1 (en) | 2012-11-15 | 2014-05-22 | Amgen Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| ES2942308T3 (es) | 2015-04-21 | 2023-05-31 | Allgenesis Biotherapeutics Inc | Compuestos y su uso como inhibidores de BACE1 |
| CN108290860B (zh) | 2015-11-25 | 2021-08-10 | Ucb生物制药有限责任公司 | 作为plasmepsin v抑制剂的亚氨基四氢嘧啶酮衍生物 |
| CN107892697B (zh) | 2016-12-26 | 2020-11-03 | 郑州泰基鸿诺医药股份有限公司 | 一种[1,3]噻嗪-2-胺类化合物及应用，药物组合物 |
| JP7592069B2 (ja) | 2019-08-19 | 2024-11-29 | ユーシービー バイオファルマ エスアールエル | 抗マラリア性ヘキサヒドロピリミジン類似体 |
| GB202010606D0 (en) | 2020-07-10 | 2020-08-26 | Ucb Biopharma Sprl | Therapeutic agents |
| WO2023152042A1 (en) | 2022-02-08 | 2023-08-17 | UCB Biopharma SRL | Antimalarial hexahydropyrimidine analogues |
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| WO2001019801A1 (en) * | 1999-09-16 | 2001-03-22 | Rimma Iliinichna Ashkinazi | Bioactive substance containing derivatives of 2-amino-6-aryloxypyrimidines and intermediary products of synthesis thereof |
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| US20030114445A1 (en) * | 2001-06-15 | 2003-06-19 | Chengxin Zhi | N3-substituted 6-anilinopyrimidines and methods to treat-Gram-positive bacterial and mycoplasmal infections |
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| AU2002950853A0 (en) * | 2002-08-19 | 2002-09-12 | Fujisawa Pharmaceutical Co., Ltd. | Aminopyrimidine compound and pharmaceutical use thereof |
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| TWI357408B (en) * | 2003-03-26 | 2012-02-01 | Mitsubishi Tanabe Pharma Corp | 3-substituted-4-pyrimidone derivatives |
| KR20080025079A (ko) * | 2005-06-14 | 2008-03-19 | 쉐링 코포레이션 | 아스파르틸 프로테아제 억제제 |
| AR053902A1 (es) * | 2005-06-14 | 2007-05-23 | Schering Corp | Inhibidores de aspartil proteasa heterociclicos macrociclicos |
| ATE478070T1 (de) * | 2005-10-27 | 2010-09-15 | Schering Corp | Heterozyklische aspartyl-proteasehemmer |
| JP2009513670A (ja) * | 2005-10-31 | 2009-04-02 | シェーリング コーポレイション | アスパルチルプロテアーゼインヒビター |
-
2005
- 2005-10-14 JP JP2007536655A patent/JP2008516945A/ja active Pending
- 2005-10-14 WO PCT/SE2005/001533 patent/WO2006041404A1/en not_active Ceased
- 2005-10-14 CN CNA2005800431529A patent/CN101084199A/zh active Pending
- 2005-10-14 US US11/577,155 patent/US20090221579A1/en not_active Abandoned
- 2005-10-14 EP EP05793318A patent/EP1802587A4/en not_active Withdrawn