JP2012508734A5 - - Google Patents
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- Publication number
- JP2012508734A5 JP2012508734A5 JP2011536289A JP2011536289A JP2012508734A5 JP 2012508734 A5 JP2012508734 A5 JP 2012508734A5 JP 2011536289 A JP2011536289 A JP 2011536289A JP 2011536289 A JP2011536289 A JP 2011536289A JP 2012508734 A5 JP2012508734 A5 JP 2012508734A5
- Authority
- JP
- Japan
- Prior art keywords
- disease
- dementia
- pharmaceutically acceptable
- alzheimer
- acceptable salt
- 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
- 208000024827 Alzheimer disease Diseases 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 9
- 206010012289 Dementia Diseases 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 208000010877 cognitive disease Diseases 0.000 claims 4
- 230000001575 pathological effect Effects 0.000 claims 4
- 230000002792 vascular Effects 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- -1 2- (difluoromethyl) pyridin-4-yl Chemical group 0.000 claims 2
- 208000000044 Amnesia Diseases 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
- 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
- 208000026139 Memory disease 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
- 210000004227 basal ganglia Anatomy 0.000 claims 2
- 230000006735 deficit Effects 0.000 claims 2
- 230000007850 degeneration Effects 0.000 claims 2
- 230000003412 degenerative effect Effects 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000006984 memory degeneration Effects 0.000 claims 2
- 208000023060 memory loss Diseases 0.000 claims 2
- 208000027061 mild cognitive impairment Diseases 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 230000000750 progressive effect Effects 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- MRXBCEQZNKUUIP-UHFFFAOYSA-N 3-[2-(difluoromethyl)pyridin-4-yl]-7-fluoro-3-(3-pyrimidin-5-ylphenyl)isoindol-1-amine Chemical compound C12=CC=CC(F)=C2C(N)=NC1(C=1C=C(N=CC=1)C(F)F)C(C=1)=CC=CC=1C1=CN=CN=C1 MRXBCEQZNKUUIP-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11463408P | 2008-11-14 | 2008-11-14 | |
| US61/114,634 | 2008-11-14 | ||
| US13976708P | 2008-12-22 | 2008-12-22 | |
| US61/139,767 | 2008-12-22 | ||
| US22165309P | 2009-06-30 | 2009-06-30 | |
| US61/221,653 | 2009-06-30 | ||
| PCT/SE2009/051295 WO2010056196A1 (en) | 2008-11-14 | 2009-11-13 | New compounds 578 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012508734A JP2012508734A (ja) | 2012-04-12 |
| JP2012508734A5 true JP2012508734A5 (enExample) | 2012-12-20 |
Family
ID=42170158
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011536289A Pending JP2012508734A (ja) | 2008-11-14 | 2009-11-13 | Ｂａｃｅ阻害剤としての置換イソインドール類及びそれらの使用 |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US8030500B2 (enExample) |
| EP (1) | EP2367814A4 (enExample) |
| JP (1) | JP2012508734A (enExample) |
| KR (1) | KR20110091540A (enExample) |
| CN (1) | CN102282140A (enExample) |
| AR (1) | AR074341A1 (enExample) |
| AU (1) | AU2009314664A1 (enExample) |
| BR (1) | BRPI0921879A2 (enExample) |
| CA (1) | CA2743938A1 (enExample) |
| CL (1) | CL2011001098A1 (enExample) |
| CO (1) | CO6362004A2 (enExample) |
| CR (1) | CR20110255A (enExample) |
| CU (1) | CU20110106A7 (enExample) |
| DO (1) | DOP2011000138A (enExample) |
| EA (1) | EA201190020A1 (enExample) |
| EC (1) | ECSP11011051A (enExample) |
| IL (1) | IL212590A0 (enExample) |
| MX (1) | MX2011004918A (enExample) |
| NI (1) | NI201100099A (enExample) |
| PE (1) | PE20110875A1 (enExample) |
| TW (1) | TW201020244A (enExample) |
| UY (1) | UY32241A (enExample) |
| WO (1) | WO2010056196A1 (enExample) |
| ZA (1) | ZA201104396B (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101346357B (zh) | 2005-10-25 | 2014-04-02 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
| TW200815349A (en) * | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
| JP5383483B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | アルツハイマー症治療用医薬組成物 |
| EP2689780A1 (en) | 2007-04-24 | 2014-01-29 | Shionogi & Co., Ltd. | Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group |
| KR101324426B1 (ko) | 2008-06-13 | 2013-10-31 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
| 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 |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| EP2485591B1 (en) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| KR20120104570A (ko) | 2009-12-11 | 2012-09-21 | 시오노기세야쿠 가부시키가이샤 | 옥사진 유도체 |
| US20110281894A1 (en) * | 2010-05-12 | 2011-11-17 | Astrazeneca Ab | Hemifumarate salt |
| EP2601197B1 (en) | 2010-08-05 | 2014-06-25 | Amgen Inc. | Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use |
| CN103261199A (zh) | 2010-10-29 | 2013-08-21 | 盐野义制药株式会社 | 萘啶衍生物 |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
| US20120165346A1 (en) * | 2010-12-22 | 2012-06-28 | Astrazeneca Ab | Compounds and their use as BACE inhibitors |
| CN103608345A (zh) | 2011-04-26 | 2014-02-26 | 盐野义制药株式会社 | 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂 |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| EP3353844B1 (en) | 2015-03-27 | 2022-05-11 | Mason K. Harrup | All-inorganic solvents for electrolytes |
| CN105272884B (zh) * | 2015-11-02 | 2017-05-24 | 浙江大学 | 一种邻氰基二苯甲酮衍生物的制备方法 |
| US10707531B1 (en) | 2016-09-27 | 2020-07-07 | New Dominion Enterprises Inc. | All-inorganic solvents for electrolytes |
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| US5877399A (en) | 1994-01-27 | 1999-03-02 | Johns Hopkins University | Transgenic mice expressing APP-Swedish mutation develop progressive neurologic disease |
| DE4419849A1 (de) | 1994-06-07 | 1995-12-14 | Hoechst Ag | Isoindolinpigmente |
| NZ284846A (en) | 1994-06-16 | 1998-12-23 | Pfizer | 1-substituted-pyrazolo[3,4-b]pyridin-5-carboxylic acid derivatives, preparation, use, intermediates and pharmaceutical compositions thereof |
| DE19516804A1 (de) | 1995-05-08 | 1996-11-14 | Hoechst Ag | Isoindolinpigmente auf Basis von Aminochinoxalindionen |
| JPH11507538A (ja) | 1995-06-07 | 1999-07-06 | アテナ ニューロサイエンシズ インコーポレイティド | β−セクレターゼ、β−セクレターゼに対する抗体、及びβ−セクレターゼ阻害を検出するためのアッセイ |
| US6211235B1 (en) | 1996-11-22 | 2001-04-03 | Elan Pharmaceuticals, Inc. | Compounds for inhibiting β-amyloid peptide release and/or its synthesis |
| GB9701684D0 (en) | 1997-01-28 | 1997-03-19 | Smithkline Beecham Plc | Novel compounds |
| ATE221886T1 (de) | 1997-09-02 | 2002-08-15 | Bristol Myers Squibb Pharma Co | Heterocyclyl-substituierte annellierte pyridine und pyrimidine als antagonisten des corticotropin freisetzenden hormons (crh), verwendbar für die behandlung von cns und stress |
| US5981168A (en) | 1998-05-15 | 1999-11-09 | The University Of British Columbia | Method and composition for modulating amyloidosis |
| NZ510708A (en) | 1998-09-24 | 2003-12-19 | Upjohn Co | Alzheimer's disease and Asp1 and Asp2 cleaving APP site (beta secretase) |
| US6245884B1 (en) | 1998-10-16 | 2001-06-12 | Vivian Y. H. Hook | Secretases related to alzheimer's dementia |
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| EP1194449B1 (en) | 1999-06-28 | 2010-09-22 | Oklahoma Medical Research Foundation | Inhibitors of memapsin 2 and use thereof |
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| GB9924957D0 (en) | 1999-10-21 | 1999-12-22 | Smithkline Beecham Plc | Novel treatment |
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| DE60116313T2 (de) | 2000-06-30 | 2006-08-31 | Elan Pharmaceuticals, Inc., San Francisco | Verbindungen zur behandlung der alzheimerischen krankheit |
| US6846813B2 (en) | 2000-06-30 | 2005-01-25 | Pharmacia & Upjohn Company | Compounds to treat alzheimer's disease |
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| WO2002025276A1 (en) | 2000-09-22 | 2002-03-28 | Wyeth | Crystal structure of bace and uses thereof |
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| ATE444962T1 (de) | 2004-06-16 | 2009-10-15 | Wyeth Corp | Amino-5,5-diphenylimidazolon-derivate zur beta- sekretase-hemmung |
| TW200613272A (en) * | 2004-08-13 | 2006-05-01 | Astrazeneca Ab | Isoindolone compounds and their use as metabotropic glutamate receptor potentiators |
| EP1805171A4 (en) | 2004-09-21 | 2009-05-13 | Wyeth Corp | CRTH2 RECEPTOR ANTAGONISM DISPLAYING INDIGENOUS ACIDS AND APPLICATIONS THEREOF |
| EP1802587A4 (en) | 2004-10-15 | 2010-02-17 | Astrazeneca Ab | SUBSTITUTED AMINO BINDINGS AND THEIR APPLICATIONS |
| WO2006041405A1 (en) | 2004-10-15 | 2006-04-20 | Astrazeneca Ab | Substituted amino-pyrimidones and uses thereof |
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| EP2264036A1 (en) * | 2005-01-14 | 2010-12-22 | Wyeth LLC (Formerly Known As Wyeth) | Amino-imidazolones for the inhibition of beta-secretase |
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| EP1896032B1 (en) | 2005-06-14 | 2012-10-31 | Merck Sharp & Dohme Corp. | The preparation and use of compounds as protease inhibitors |
| EP1896406A2 (en) | 2005-06-14 | 2008-03-12 | Shering Corporation | The preparation and use of compounds as protease inhibitors |
| CA2609562A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Macrocyclic heterocyclic aspartyl protease inhibitors |
| AU2006259574A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | The preparation and use of compounds as aspartyl protease inhibitors |
| SG162790A1 (en) | 2005-06-14 | 2010-07-29 | Schering Corp | Aspartyl protease inhibitors |
| US7759353B2 (en) | 2005-06-14 | 2010-07-20 | Schering Corporation | Substituted spiro iminopyrimidinones as aspartyl protease inhibitors, compositions, and methods of treatment |
| TW200738683A (en) | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
| JP2009500329A (ja) | 2005-06-30 | 2009-01-08 | ワイス | アミノ−５−（６員）ヘテロアリールイミダゾロン化合物およびβ−セレクターゼ調節のためのその使用 |
| WO2007011810A1 (en) | 2005-07-18 | 2007-01-25 | Merck & Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
| US7601751B2 (en) | 2005-09-01 | 2009-10-13 | Bristol-Myers Squibb Company | Indole acetic acid acyl guanidines as β-secretase inhibitors |
| CN101346357B (zh) | 2005-10-25 | 2014-04-02 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
| ATE478070T1 (de) | 2005-10-27 | 2010-09-15 | Schering Corp | Heterozyklische aspartyl-proteasehemmer |
| EP1943246A1 (en) | 2005-10-31 | 2008-07-16 | Schering Corporation | Aspartyl protease inhibitors |
| CN101360720A (zh) | 2005-11-15 | 2009-02-04 | 阿斯利康(瑞典)有限公司 | 新颖的2-氨基嘧啶酮衍生物及其用途 |
| EP1951682A4 (en) | 2005-11-15 | 2011-06-15 | Astrazeneca Ab | NEW 2-AMINOPYRIMIDONE OR 2-AMINOPYRIDINONE DERIVATIVES AND THEIR USE |
| CN101360722A (zh) | 2005-11-15 | 2009-02-04 | 阿斯利康(瑞典)有限公司 | 新颖的2-氨基嘧啶衍生物及其用途 |
| TW200804290A (en) | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
| TW200734311A (en) | 2005-11-21 | 2007-09-16 | Astrazeneca Ab | New compounds |
| CN101360716A (zh) | 2005-11-21 | 2009-02-04 | 阿斯利康(瑞典)有限公司 | 新颖的2-氨基-咪唑-4-酮化合物及其在制备用于治疗认知缺损、阿尔茨海默病、神经变性和痴呆的药物中的用途 |
| 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 |
| TW200808751A (en) | 2006-04-13 | 2008-02-16 | Astrazeneca Ab | New compounds |
| US8168641B2 (en) | 2006-06-12 | 2012-05-01 | Schering Corporation | Aspartyl protease inhibitors |
| TW200815447A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds IV |
| TW200815449A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds II |
| TW200815443A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds I |
| TW200808796A (en) | 2006-06-14 | 2008-02-16 | Astrazeneca Ab | New compounds III |
| TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
| WO2008063114A1 (en) | 2006-11-20 | 2008-05-29 | Astrazeneca Ab | Amino- imidazolones and their use as medicament for treating cognitive impairment alzheimer disease, neurodegeneration and dementia |
| WO2008076043A1 (en) | 2006-12-20 | 2008-06-26 | Astrazeneca Ab | Novel 2-amino-5,5-diaryl-imidazol-4-ones |
| TW200831484A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| TW200831091A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| TW200902503A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| WO2009005470A1 (en) * | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
| WO2009005471A1 (en) * | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
| WO2010056195A1 (en) | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 575 |
| US20100125081A1 (en) | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 574 |
| EP2485591B1 (en) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace 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 |
| US8557826B2 (en) | 2009-10-08 | 2013-10-15 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use |
-
2009
- 2009-11-12 TW TW098138485A patent/TW201020244A/zh unknown
- 2009-11-13 PE PE2011001034A patent/PE20110875A1/es not_active Application Discontinuation
- 2009-11-13 UY UY0001032241A patent/UY32241A/es not_active Application Discontinuation
- 2009-11-13 US US12/618,212 patent/US8030500B2/en not_active Expired - Fee Related
- 2009-11-13 EP EP09826375A patent/EP2367814A4/en not_active Withdrawn
- 2009-11-13 JP JP2011536289A patent/JP2012508734A/ja active Pending
- 2009-11-13 WO PCT/SE2009/051295 patent/WO2010056196A1/en not_active Ceased
- 2009-11-13 CA CA2743938A patent/CA2743938A1/en not_active Abandoned
- 2009-11-13 BR BRPI0921879A patent/BRPI0921879A2/pt not_active Application Discontinuation
- 2009-11-13 CN CN2009801545281A patent/CN102282140A/zh active Pending
- 2009-11-13 AR ARP090104400A patent/AR074341A1/es unknown
- 2009-11-13 EA EA201190020A patent/EA201190020A1/ru unknown
- 2009-11-13 AU AU2009314664A patent/AU2009314664A1/en not_active Abandoned
- 2009-11-13 KR KR1020117013516A patent/KR20110091540A/ko not_active Withdrawn
- 2009-11-13 MX MX2011004918A patent/MX2011004918A/es not_active Application Discontinuation
-
2011
- 2011-04-28 IL IL212590A patent/IL212590A0/en unknown
- 2011-04-28 CO CO11052264A patent/CO6362004A2/es not_active Application Discontinuation
- 2011-05-13 CL CL2011001098A patent/CL2011001098A1/es unknown
- 2011-05-13 NI NI201100099A patent/NI201100099A/es unknown
- 2011-05-13 EC EC2011011051A patent/ECSP11011051A/es unknown
- 2011-05-13 DO DO2011000138A patent/DOP2011000138A/es unknown
- 2011-05-13 CR CR20110255A patent/CR20110255A/es unknown
- 2011-05-13 CU CU20110106A patent/CU20110106A7/es unknown
- 2011-06-13 ZA ZA2011/04396A patent/ZA201104396B/en unknown
- 2011-09-06 US US13/225,707 patent/US20110319426A1/en not_active Abandoned
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