JP2014505688A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2014505688A5 JP2014505688A5 JP2013548830A JP2013548830A JP2014505688A5 JP 2014505688 A5 JP2014505688 A5 JP 2014505688A5 JP 2013548830 A JP2013548830 A JP 2013548830A JP 2013548830 A JP2013548830 A JP 2013548830A JP 2014505688 A5 JP2014505688 A5 JP 2014505688A5
- Authority
- JP
- Japan
- Prior art keywords
- disease
- bace
- present
- treating
- patent document
- 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.)
- Ceased
Links
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 18
- 201000010099 disease Diseases 0.000 description 11
- 239000003814 drug Substances 0.000 description 10
- 239000003795 chemical substances by application Substances 0.000 description 7
- 208000035475 disorder Diseases 0.000 description 7
- 229940124597 therapeutic agent Drugs 0.000 description 6
- 208000024827 Alzheimer disease Diseases 0.000 description 5
- 210000004556 brain Anatomy 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 108090000765 processed proteins & peptides Proteins 0.000 description 4
- 102000003908 Cathepsin D Human genes 0.000 description 3
- 108090000258 Cathepsin D Proteins 0.000 description 3
- 208000010877 cognitive disease Diseases 0.000 description 3
- 230000001404 mediated effect Effects 0.000 description 3
- 208000027061 mild cognitive impairment Diseases 0.000 description 3
- 208000024891 symptom Diseases 0.000 description 3
- 102000013455 Amyloid beta-Peptides Human genes 0.000 description 2
- 108010090849 Amyloid beta-Peptides Proteins 0.000 description 2
- 102100021257 Beta-secretase 1 Human genes 0.000 description 2
- 101710150192 Beta-secretase 1 Proteins 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- 238000004220 aggregation Methods 0.000 description 2
- 230000002776 aggregation Effects 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 230000037396 body weight Effects 0.000 description 2
- 238000002648 combination therapy Methods 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 230000004770 neurodegeneration Effects 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 230000006641 stabilisation Effects 0.000 description 2
- 238000011105 stabilization Methods 0.000 description 2
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 description 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 description 1
- 102000035101 Aspartic proteases Human genes 0.000 description 1
- 108091005502 Aspartic proteases Proteins 0.000 description 1
- 208000024806 Brain atrophy Diseases 0.000 description 1
- 206010012289 Dementia Diseases 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000006978 adaptation Effects 0.000 description 1
- 230000003044 adaptive effect Effects 0.000 description 1
- 239000003696 aspartic proteinase inhibitor Substances 0.000 description 1
- 230000019771 cognition Effects 0.000 description 1
- 239000013066 combination product Substances 0.000 description 1
- 229940127555 combination product Drugs 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 230000002121 endocytic effect Effects 0.000 description 1
- 238000012224 gene deletion Methods 0.000 description 1
- 210000002288 golgi apparatus Anatomy 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000015654 memory Effects 0.000 description 1
- 230000001394 metastastic effect Effects 0.000 description 1
- 206010061289 metastatic neoplasm Diseases 0.000 description 1
- 230000000926 neurological effect Effects 0.000 description 1
- 210000002569 neuron Anatomy 0.000 description 1
- 230000008506 pathogenesis Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 230000007505 plaque formation Effects 0.000 description 1
- 102000004196 processed proteins & peptides Human genes 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 210000000225 synapse Anatomy 0.000 description 1
- 230000000946 synaptic effect Effects 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161432037P | 2011-01-12 | 2011-01-12 | |
| US61/432,037 | 2011-01-12 | ||
| PCT/EP2012/050387 WO2012095463A1 (en) | 2011-01-12 | 2012-01-11 | Oxazine derivatives and their use in the treatment of neurological disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014505688A JP2014505688A (ja) | 2014-03-06 |
| JP2014505688A5 true JP2014505688A5 (enExample) | 2015-03-05 |
Family
ID=45476523
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013548830A Ceased JP2014505688A (ja) | 2011-01-12 | 2012-01-11 | オキサジン誘導体および神経障害の処置におけるその使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20130281449A1 (enExample) |
| EP (1) | EP2663559B1 (enExample) |
| JP (1) | JP2014505688A (enExample) |
| KR (1) | KR20140051822A (enExample) |
| CN (1) | CN103429589A (enExample) |
| AU (1) | AU2012206555A1 (enExample) |
| BR (1) | BR112013017779A2 (enExample) |
| CA (1) | CA2824097A1 (enExample) |
| EA (1) | EA201391029A1 (enExample) |
| MX (1) | MX2013008111A (enExample) |
| WO (1) | WO2012095463A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101324426B1 (ko) | 2008-06-13 | 2013-10-31 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
| UY32799A (es) | 2009-07-24 | 2011-02-28 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos |
| EP2485591B1 (en) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| KR20120104570A (ko) | 2009-12-11 | 2012-09-21 | 시오노기세야쿠 가부시키가이샤 | 옥사진 유도체 |
| KR101730937B1 (ko) | 2010-06-09 | 2017-04-27 | 얀센 파마슈티카 엔.브이. | 베타-세크레타아제(ｂａｃｅ) 저해제로 유용한 5,6-디하이드로-2ｈ-[1,4]옥사진-3-일-아민 유도체 |
| BR112013015430A2 (pt) | 2010-12-22 | 2016-09-20 | Janssen Pharmaceutica Nv | derivados de 5,6-diidro-imidazo[1,2-a]pirazin-8-ilamina úteis como inibidores de beta-secretase (bace) |
| DK2663561T3 (en) | 2011-01-13 | 2016-06-06 | Novartis Ag | New heterocyclic derivatives and their use in treating neurological disorders |
| PH12013501805A1 (en) | 2011-03-09 | 2013-11-18 | Janssen Pharmaceutica Nv | 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| EP2766358B1 (en) | 2011-10-13 | 2016-06-22 | Novartis AG | Novel oxazine derivatives and their use in the treatment of disease |
| UA111749C2 (uk) * | 2011-12-05 | 2016-06-10 | Янссен Фармацевтика Нв | Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| JP6389830B2 (ja) | 2013-03-01 | 2018-09-12 | アムジエン・インコーポレーテツド | ベータ−セクレターゼ阻害剤としてのパーフルオロ化５，６−ジヒドロ−４ｈ−１，３−オキサジン−２−アミン化合物および使用方法 |
| JP6374889B2 (ja) | 2013-03-08 | 2018-08-15 | アムジエン・インコーポレーテツド | β−セクレターゼ阻害剤としての過フッ素化シクロプロピル縮合１，３−オキサジン−２−アミン化合物、及び使用方法 |
| WO2014198851A1 (en) | 2013-06-12 | 2014-12-18 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace) |
| US9751886B2 (en) | 2013-06-12 | 2017-09-05 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-A]pyrazine derivatives as inhibitors of beta-secretase (BACE) |
| GEAP201814248A (en) * | 2014-02-19 | 2018-04-10 | H Lundbeck As | 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease |
| US9550762B2 (en) | 2014-08-08 | 2017-01-24 | Amgen, Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| MA40941A (fr) | 2014-11-10 | 2017-09-19 | H Lundbeck As | 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1 |
| JO3458B1 (ar) | 2014-11-10 | 2020-07-05 | H Lundbeck As | 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 |
| CR20170187A (es) | 2014-11-10 | 2018-02-01 | H Lundbeck As | 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer |
| ES2768823T3 (es) | 2014-12-18 | 2020-06-23 | Janssen Pharmaceutica Nv | Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa |
| TW201717948A (zh) | 2015-08-10 | 2017-06-01 | Ｈ 朗德貝克公司 | 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療 |
| JP2018531889A (ja) | 2015-08-12 | 2018-11-01 | ハー・ルンドベック・アクチエゼルスカベット | Ｂａｃｅ１阻害剤としての２−アミノ−３−フルオロ−３−（フルオロメチル）−６−メチル−６−フェニル−３，４，５，６−テトラヒドロピリジン |
| US10399995B2 (en) | 2016-08-26 | 2019-09-03 | Eli Lilly And Company | 1,4-Oxazines useful as selective BACE1 inhibitors |
| MX388697B (es) | 2016-12-15 | 2025-03-20 | Amgen Inc | Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso. |
| MA52722A (fr) | 2016-12-15 | 2021-04-14 | Amgen Inc | Dérivés d'oxazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation |
| MX386618B (es) | 2016-12-15 | 2025-03-19 | Amgen Inc | Derivados de tiazina condensados con ciclopropilo como inhibidores de beta-secretasa y métodos de uso. |
| MA54101A (fr) | 2016-12-15 | 2021-10-27 | Amgen Inc | Dérivés de thiazine et d'oxazine bicycliques en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation |
| EP3555086B1 (en) | 2016-12-15 | 2021-09-01 | Amgen Inc. | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use |
| KR102093540B1 (ko) | 2017-08-11 | 2020-03-25 | 주식회사 엘지화학 | 할로겐 치환된 스티렌 모노머의 제조방법 |
| CN111675708A (zh) * | 2020-06-10 | 2020-09-18 | 南京合巨药业有限公司 | 一种6-氰基-7-氮杂吲哚及其衍生物的制备方法 |
| CN111943947B (zh) * | 2020-07-24 | 2021-04-30 | 重庆文理学院 | 1H-吡咯[2,3-b]吡啶衍生物及其合成方法与应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL6911868A (enExample) | 1968-08-31 | 1970-03-03 | ||
| DE19725802A1 (de) | 1996-07-10 | 1998-01-15 | Lonza Ag | Verfahren zur Herstellung von (S)- oder (R)-3,3,3-trifluor-2-hydroxy-2-methylpropionsäure |
| CA2514733A1 (en) | 2003-02-28 | 2004-09-16 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
| JP4707560B2 (ja) | 2003-12-29 | 2011-06-22 | Ｍｓｄ株式会社 | 新規２−ヘテロアリール置換ベンズイミダゾール誘導体 |
| 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 |
| BRPI0906962B8 (pt) | 2008-01-18 | 2021-05-25 | Eisai R&D Man Co Ltd | composto de aminodiidrotiazina fundido |
| 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 |
| UY32799A (es) * | 2009-07-24 | 2011-02-28 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos |
| BR112012004154A2 (pt) * | 2010-07-13 | 2017-05-30 | Novartis Ag | "derivados de oxazina e seu uso no tratamento de distúrbios neurológicos" |
-
2012
- 2012-01-11 KR KR20137021073A patent/KR20140051822A/ko not_active Withdrawn
- 2012-01-11 WO PCT/EP2012/050387 patent/WO2012095463A1/en not_active Ceased
- 2012-01-11 BR BR112013017779A patent/BR112013017779A2/pt not_active IP Right Cessation
- 2012-01-11 US US13/978,885 patent/US20130281449A1/en not_active Abandoned
- 2012-01-11 MX MX2013008111A patent/MX2013008111A/es not_active Application Discontinuation
- 2012-01-11 CA CA 2824097 patent/CA2824097A1/en not_active Abandoned
- 2012-01-11 CN CN2012800128201A patent/CN103429589A/zh active Pending
- 2012-01-11 AU AU2012206555A patent/AU2012206555A1/en not_active Abandoned
- 2012-01-11 EP EP12700232.7A patent/EP2663559B1/en not_active Not-in-force
- 2012-01-11 JP JP2013548830A patent/JP2014505688A/ja not_active Ceased
- 2012-01-11 EA EA201391029A patent/EA201391029A1/ru unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2014505688A5 (enExample) | ||
| Maciejewska et al. | A review of the mechanisms underlying selected comorbidities in Alzheimer’s disease | |
| Sikiric et al. | Brain-gut axis and pentadecapeptide BPC 157: Theoretical and practical implications | |
| Wei et al. | Direct activation of protein phosphatase 2A (PP2A) by tricyclic sulfonamides ameliorates Alzheimer's disease pathogenesis in cell and animal models | |
| KR102547164B1 (ko) | 특정 환자 집단에서 신경퇴행성 장애를 치료하는 방법 | |
| EA201490163A1 (ru) | Ингибиторы кинуренин-3-монооксигеназы, фармацевтические композиции и способы их применения | |
| EA201790406A1 (ru) | Ингибиторы кинуренин-3-монооксигеназы, фармацевтические композиции и способы их применения | |
| Palhegyi et al. | Biomedical implications of autophagy in macromolecule storage disorders | |
| CN105267235A (zh) | 纳米金属在促进神经突生长和治疗和/或预防神经病症中的用途 | |
| KR20160111013A (ko) | 신경질환의 치료를 위한 바클로펜, 아캄프로세이트 및 중쇄 트리-글리세리드의 조합 | |
| PH12021552905A1 (en) | 1,3,4-oxadiazole homophthalimide derivative compounds as histone deacetylase 6 inhibitor, and the pharmaceutical composition comprising the same | |
| US12527781B2 (en) | Treatment of neurodegenerative conditions by disruption of Rhes | |
| MX2023000610A (es) | Inhibidor de trpv4 como agente terapeutico para enfermedades oculares. | |
| JP5856725B2 (ja) | うつ病治療用または予防用医薬組成物 | |
| CN102218091A (zh) | 肉桂油、桂皮醛及其衍生物在制备组胺h3受体拮抗剂或反向激动剂药物中的用途 | |
| US11318122B2 (en) | Pharmaceutical combination and its use for treating synucleinopathties | |
| JP2015522601A5 (enExample) | ||
| US11376277B2 (en) | Synergistic medicinal compositions for treating dysfunctional D-serine signaling | |
| EP3106161A1 (en) | Prevention or treatment agent for cerebral amyloid beta storage diseases | |
| CN111315373A (zh) | 用于预防和/或治疗以神经元可塑性下降为特征、特别是突触可塑性下降为特征的中枢神经系统疾病的化合物和组合物 | |
| Emran et al. | Autophagy and Alzheimer’s disease: How far science has to be progressed?− correspondence | |
| US20200297662A1 (en) | Ketamine for treatment of adnp syndrome and sensory processing deficits | |
| KR102633592B1 (ko) | 자폐 스펙트럼 장애의 예방 또는 치료용 약학적 조성물 및 이를 이용한 자폐 스펙트럼 장애 치료방법 | |
| Adnan | Clinical Aspects and Treatment of Parkinson Disease: A Biochemical Perspective | |
| Nobili et al. | Autophagy Mechanisms for Brain Recovery. Keep It Clean, Keep It Alive |