MX366855B - Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso. - Google Patents
Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso.Info
- Publication number
- MX366855B MX366855B MX2015011313A MX2015011313A MX366855B MX 366855 B MX366855 B MX 366855B MX 2015011313 A MX2015011313 A MX 2015011313A MX 2015011313 A MX2015011313 A MX 2015011313A MX 366855 B MX366855 B MX 366855B
- Authority
- MX
- Mexico
- Prior art keywords
- compounds
- beta
- bace
- methods
- oxazin
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
- C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
- C07D265/08—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic System
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
Abstract
La presente invención da a conocer una nueva clase de compuestos útiles para la modulación de la actividad de la enzima beta-secretasa (BACE). Los compuestos poseen una Fórmula general I: (ver Fórmula) donde las variables A4, A5, A6, A8, cada uno de R1 y R2, R3 y R7 de la Fórmula I, en forma independiente, se definen en la presente descripción. La invención también da a conocer composiciones farmacéuticas que comprenden los compuestos, y los correspondientes usos de los compuestos y composiciones para el tratamiento de trastornos y/o condiciones asociadas con la formación y deposición de placa A-beta que resulta de la actividad biológica de BACE. Dichos trastornos mediados por BACE incluyen, por ejemplo, la enfermedad de Alzheimer, déficits cognitivos, deterioro cognitivo, esquizofrenia y otras condiciones del sistema nervioso central. La invención asimismo da a conocer compuestos de Fórmulas II y III, y sub-Fórmulas de los mismos, y compuestos intermediarios, así como procesos y métodos útiles para la preparación de los compuestos de Fórmulas I-III.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361771615P | 2013-03-01 | 2013-03-01 | |
US201361826431P | 2013-05-22 | 2013-05-22 | |
US201461928898P | 2014-01-17 | 2014-01-17 | |
PCT/US2014/019100 WO2014134341A1 (en) | 2013-03-01 | 2014-02-27 | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
Publications (2)
Publication Number | Publication Date |
---|---|
MX2015011313A MX2015011313A (es) | 2015-12-03 |
MX366855B true MX366855B (es) | 2019-07-26 |
Family
ID=50349866
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2015011313A MX366855B (es) | 2013-03-01 | 2014-02-27 | Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso. |
Country Status (9)
Country | Link |
---|---|
US (1) | US9296734B2 (es) |
EP (1) | EP2961749B1 (es) |
JP (1) | JP6389830B2 (es) |
AU (2) | AU2014223334C1 (es) |
CA (1) | CA2902212C (es) |
MX (1) | MX366855B (es) |
TW (1) | TW201446758A (es) |
UY (1) | UY35361A (es) |
WO (1) | WO2014134341A1 (es) |
Families Citing this family (26)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20130018370A (ko) | 2008-06-13 | 2013-02-20 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
WO2011071135A1 (ja) † | 2009-12-11 | 2011-06-16 | 塩野義製薬株式会社 | オキサジン誘導体 |
WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
WO2014134341A1 (en) | 2013-03-01 | 2014-09-04 | Amgen Inc. | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
EP2964644B1 (en) | 2013-03-08 | 2018-12-26 | Amgen, Inc. | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
WO2014166906A1 (en) * | 2013-04-11 | 2014-10-16 | F. Hoffmann-La Roche Ag | Bace1 inhibitors |
UA117695C2 (uk) | 2014-02-19 | 2018-09-10 | Х. Луннбек А/С | 2-аміно-3,5,5-трифтор-3,4,5,6-тетрагідропіридини як інгібітори bace1 для лікування хвороби альцгеймера |
TW201623295A (zh) | 2014-04-11 | 2016-07-01 | 塩野義製藥股份有限公司 | 具有bace1抑制活性之二氫噻及二氫衍生物 |
MX2017001794A (es) | 2014-08-08 | 2017-06-29 | Amgen Inc | Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso. |
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 |
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 |
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 |
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 |
EP3334720A1 (en) | 2015-08-12 | 2018-06-20 | H. Lundbeck A/S | 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridins as bace1 inhibitors |
TW201726651A (zh) | 2015-09-23 | 2017-08-01 | 健生藥品公司 | 2,3,4,5-四氫吡啶-6-胺衍生物 |
WO2017061534A1 (en) | 2015-10-08 | 2017-04-13 | Shionogi & Co., Ltd. | Dihydrothiazine derivatives |
CN108430982A (zh) | 2015-12-25 | 2018-08-21 | 盐野义制药株式会社 | 用于制备噻嗪衍生物的方法和中间体 |
CN108699051B (zh) * | 2016-03-01 | 2021-12-24 | 豪夫迈·罗氏有限公司 | Bace1抑制剂 |
MX2019007103A (es) * | 2016-12-15 | 2019-11-05 | Amgen Inc | Derivados de tiazina condensados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso. |
US11124528B2 (en) * | 2017-04-27 | 2021-09-21 | Basf Se | Process for preparing optically active 2,3-dihydrothiazolo[3,2-A]pyrimidin-4-ium compounds |
US11629154B2 (en) | 2018-04-27 | 2023-04-18 | Shionogi & Co., Ltd. | Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity |
TWI797167B (zh) * | 2018-09-28 | 2023-04-01 | 德商巴地斯顏料化工廠 | 用於製備光學活性嘧啶鎓化合物之方法 |
TWI780230B (zh) * | 2018-09-28 | 2022-10-11 | 德商巴地斯顏料化工廠 | 用於製備含硫之嘧啶鎓化合物之方法 |
TW202237119A (zh) | 2020-12-10 | 2022-10-01 | 美商住友製藥腫瘤公司 | Alk﹘5抑制劑和彼之用途 |
CN113979993B (zh) * | 2021-11-29 | 2023-10-13 | 云南萃精生物科技有限责任公司 | 一种不对称合成(s)-烟碱的方法 |
CN114561435B (zh) * | 2022-04-27 | 2022-08-30 | 南京科力硕生物科技有限公司 | 利用磁性碳纳米管固定化酶催化制备4-氯-3-乙基-1-甲基吡唑-5-甲酸的方法 |
Family Cites Families (77)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5441870A (en) | 1992-04-15 | 1995-08-15 | Athena Neurosciences, Inc. | Methods for monitoring cellular processing of β-amyloid precursor protein |
SI9300303A (en) | 1993-06-08 | 1994-12-31 | Krka Tovarna Zdravil | Process for isolation of hypolipemic effective substance |
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 |
SG113454A1 (en) | 1998-09-24 | 2005-08-29 | Upjohn Co | Alzheimer's disease secretase |
US20040234976A1 (en) | 1998-09-24 | 2004-11-25 | Gurney Mark E. | Alzheimer's disease secretase, app substrates therefor, and uses therefor |
US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
EP1699455B1 (en) | 2003-12-15 | 2013-05-08 | Merck Sharp & Dohme Corp. | Heterocyclic aspartyl protease inhibitors |
US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
CN103936690B (zh) | 2005-10-25 | 2016-06-08 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
MX2009011498A (es) | 2007-04-24 | 2009-11-10 | Shionogi & Co | Derivados de aminodihidrotiazina sustituida con un grupo ciclico. |
AU2008276521B2 (en) | 2007-07-17 | 2011-11-03 | Amgen Inc. | Heterocyclic modulators of PKB |
AP2010005167A0 (en) | 2007-08-01 | 2010-02-28 | Pfizer | Pyrazole compounds and their use as RAF inhibitors |
RU2476431C2 (ru) | 2008-01-18 | 2013-02-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Конденсированное производное аминодигидротиазина |
TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
KR20130018370A (ko) | 2008-06-13 | 2013-02-20 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
AU2009277485B2 (en) | 2008-07-28 | 2013-05-02 | 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 |
US8461160B2 (en) | 2009-05-08 | 2013-06-11 | Hoffmann-La Roche, Inc. | Dihydropyrimidinones |
AR077277A1 (es) * | 2009-07-09 | 2011-08-17 | Lilly Co Eli | Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer |
GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
US8188079B2 (en) | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
US20110065695A1 (en) | 2009-09-11 | 2011-03-17 | Jeremy Beauchamp | Use of aminodihydrothiazines for the treatment or prevention of diabetes |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
US20120238557A1 (en) | 2009-11-13 | 2012-09-20 | Shionogi & Co., Ltd. | Aminothiazine or aminooxazine derivative having amino linker |
US20120245154A1 (en) | 2009-12-09 | 2012-09-27 | Shionogi & Co., Ltd. | Substituted aminothiazine derivative |
JP5554346B2 (ja) | 2009-12-09 | 2014-07-23 | 塩野義製薬株式会社 | 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物 |
US7964594B1 (en) | 2009-12-10 | 2011-06-21 | Hoffmann-La Roche Inc. | Amino oxazine derivatives |
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 |
WO2011071135A1 (ja) | 2009-12-11 | 2011-06-16 | 塩野義製薬株式会社 | オキサジン誘導体 |
WO2011071109A1 (ja) | 2009-12-11 | 2011-06-16 | 塩野義製薬株式会社 | アミノ基を有する縮合ヘテロ環化合物 |
JP2013544894A (ja) | 2010-12-09 | 2013-12-19 | ヤンセン ファーマシューティカ エヌ.ベー. | Trpm8モジュレータとしてのイミダゾ[1,2−a]ピリジンスルホンアミド |
CN103429589A (zh) | 2011-01-12 | 2013-12-04 | 诺瓦提斯公司 | 噁嗪衍生物及其在治疗神经障碍中的用途 |
US20140128385A1 (en) | 2011-01-13 | 2014-05-08 | Novartis Ag | Bace-2 inhibitors for the treatment of metabolic disorders |
CA2824220C (en) | 2011-01-13 | 2020-09-01 | Novartis Ag | Novel heterocyclic derivatives and their use in the treatment of neurological disorders |
US8404680B2 (en) | 2011-02-08 | 2013-03-26 | Hoffmann-La Roche Inc. | N-[3-(5-amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides as BACE1 and/or BACE2 inhibitors |
US9221839B2 (en) | 2011-04-07 | 2015-12-29 | Merck Sharp & Dohme Corp. | C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
US8754075B2 (en) | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
RU2013150349A (ru) | 2011-04-13 | 2015-05-20 | Мерк Шарп И Доум Корп. | 5-замещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов васе, содержащие их композиции и их применение |
WO2012147762A1 (ja) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | ピリジン誘導体およびそれを含有するbace1阻害剤 |
WO2012147763A1 (ja) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するbace1阻害剤 |
US8785436B2 (en) * | 2011-05-16 | 2014-07-22 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE 1 and/or BACE2 inhibitors |
US8604024B2 (en) | 2011-05-24 | 2013-12-10 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
WO2012162334A1 (en) | 2011-05-24 | 2012-11-29 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
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 |
JP2012250933A (ja) | 2011-06-03 | 2012-12-20 | Shionogi & Co Ltd | オキサジン誘導体を含有するアルツハイマー症治療用または予防用医薬組成物 |
RU2599256C2 (ru) | 2011-06-07 | 2016-10-10 | Ф. Хоффманн-Ля Рош Аг | [1,3]оксазины |
WO2012168164A1 (en) * | 2011-06-07 | 2012-12-13 | F. Hoffmann-La Roche Ag | Halogen-alkyl-1,3 oxazines as bace1 and/or bace2 inhibitors |
US8927535B2 (en) | 2011-07-06 | 2015-01-06 | Hoffman-La Roche Inc. | Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors |
US9181236B2 (en) | 2011-08-22 | 2015-11-10 | Merck Sharp & Dohme Corp. | 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use |
UY34278A (es) | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
EP2751116B1 (en) | 2011-08-31 | 2016-10-12 | Pfizer Inc | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds |
US8476264B2 (en) | 2011-09-21 | 2013-07-02 | Hoffmann-La Roche Inc. | N-(3-(2-amino-6,6-difluoro-4,4A,5,6,7,7A-hexahydro-cyclopenta[E][1,3]oxazin-4-yl)-phenylamides as BACE1 inhibitors |
AU2012322329A1 (en) | 2011-10-13 | 2014-05-01 | Novartis Ag | Novel oxazine derivatives and their use in the treatment of disease |
CA2853221A1 (en) | 2011-10-24 | 2013-05-02 | Tohru Yamashita | Bicyclic compound |
CN104066727B (zh) * | 2012-01-26 | 2019-04-26 | 霍夫曼-拉罗奇有限公司 | 氟甲基-5,6-二氢-4h-[1,3]噁嗪类 |
JP2015514073A (ja) | 2012-03-20 | 2015-05-18 | エラン ファーマシューティカルズ, リミテッド・ライアビリティ・カンパニー | スピロ環式ジヒドロ−チアジンおよびジヒドロ−オキサジンbace阻害剤、ならびにその組成物および使用 |
ES2585262T3 (es) | 2012-05-04 | 2016-10-04 | Pfizer Inc | Compuestos heterocíclicos de hexahidropiran[3,4-d][1,3]tiazin-2-amina sustituidos como inhibidores de PPA, BACE1 y BACE2 |
WO2013182638A1 (en) | 2012-06-08 | 2013-12-12 | H. Lundbeck A/S | 2 -aminothiazinylheteroaryls as bace1 inhibitors for the treatment alzheimer's disease |
CA2872181A1 (en) | 2012-06-26 | 2014-01-03 | F. Hoffmann-La Roche Ag | Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors |
GB201212871D0 (en) | 2012-07-20 | 2012-09-05 | Eisai Ltd | Novel compounds |
EP2897964A1 (en) | 2012-09-20 | 2015-07-29 | Pfizer Inc. | Alkyl-substituted hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds |
EP2908824B1 (en) | 2012-10-17 | 2018-05-02 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
US9422277B2 (en) | 2012-10-17 | 2016-08-23 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use |
WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
JP6243921B2 (ja) | 2012-10-26 | 2017-12-06 | イーライ リリー アンド カンパニー | Bace阻害剤 |
US9447085B2 (en) | 2012-12-14 | 2016-09-20 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxides containing a thioamide, amidine, or amide oxime group as BACE inhibitors, compositions, and their use |
WO2014098831A1 (en) | 2012-12-19 | 2014-06-26 | Bristol-Myers Squibb Company | 4,6-diarylaminothiazines as bace1 inhibitors and their use for the reduction of beta-amyloid production |
EP2935282A1 (en) | 2012-12-19 | 2015-10-28 | Pfizer Inc. | CARBOCYCLIC- AND HETEROCYCLIC-SUBSTITUTED HEXAHYDROPYRANO[3,4-d][1,3]THIAZIN-2-AMINE COMPOUNDS |
US9365589B2 (en) | 2012-12-20 | 2016-06-14 | Merck Sharp & Dohme Corp. | C5, C6 oxacyclic-fused thiazine dioxide compounds as BACE inhibitors, compositions, and their use |
EP2934534B1 (en) | 2012-12-21 | 2017-12-13 | Merck Sharp & Dohme Corp. | C5-spiro iminothiadiazine dioxides as bace inhibitors |
CA2896185A1 (en) * | 2013-01-22 | 2014-07-31 | F. Hoffmann-La Roche Ag | Fluoro-[1,3]oxazines as bace1 inhibitors |
WO2014134341A1 (en) | 2013-03-01 | 2014-09-04 | Amgen Inc. | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
EP2964644B1 (en) | 2013-03-08 | 2018-12-26 | Amgen, Inc. | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
WO2014166906A1 (en) | 2013-04-11 | 2014-10-16 | F. Hoffmann-La Roche Ag | Bace1 inhibitors |
EP2989081A1 (en) | 2013-04-26 | 2016-03-02 | F. Hoffmann-La Roche AG | Synthesis of bace inhibitors |
-
2014
- 2014-02-27 WO PCT/US2014/019100 patent/WO2014134341A1/en active Application Filing
- 2014-02-27 AU AU2014223334A patent/AU2014223334C1/en active Active
- 2014-02-27 MX MX2015011313A patent/MX366855B/es active IP Right Grant
- 2014-02-27 EP EP14712418.4A patent/EP2961749B1/en active Active
- 2014-02-27 US US14/192,710 patent/US9296734B2/en active Active
- 2014-02-27 JP JP2015560325A patent/JP6389830B2/ja active Active
- 2014-02-27 TW TW103106910A patent/TW201446758A/zh unknown
- 2014-02-27 CA CA2902212A patent/CA2902212C/en active Active
- 2014-03-05 UY UY0001035361A patent/UY35361A/es not_active Application Discontinuation
-
2018
- 2018-06-25 AU AU2018204589A patent/AU2018204589A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
US9296734B2 (en) | 2016-03-29 |
CA2902212C (en) | 2020-10-13 |
EP2961749B1 (en) | 2019-10-09 |
MX2015011313A (es) | 2015-12-03 |
AU2014223334B2 (en) | 2018-04-05 |
CA2902212A1 (en) | 2014-09-04 |
JP2016511258A (ja) | 2016-04-14 |
WO2014134341A1 (en) | 2014-09-04 |
TW201446758A (zh) | 2014-12-16 |
UY35361A (es) | 2014-09-30 |
JP6389830B2 (ja) | 2018-09-12 |
AU2014223334A1 (en) | 2015-09-10 |
US20140249104A1 (en) | 2014-09-04 |
AU2014223334C1 (en) | 2018-10-18 |
EP2961749A1 (en) | 2016-01-06 |
AU2018204589A1 (en) | 2018-07-12 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
MX366855B (es) | Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso. | |
TN2015000382A1 (en) | Perfluorinated cyclopropyl fused 1,3- oxazin -2- amine compounds as beta- secretase inhibitors and methods of use | |
MX2017001794A (es) | Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso. | |
MX2019007104A (es) | Derivados de dioxido de 1,4-tiazina y dioxido de 1,2,4-tiadiazina como inhibidores de beta-secretasa y metodos de uso. | |
MX2019007101A (es) | Derivados de oxazina como inhibidores de beta secretasa y metodos de uso. | |
MX2012010658A (es) | Compuestos de anillo espiro tetraciclico como moduladores de beta-secretasa. | |
MY148558A (en) | Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use | |
MX2019007102A (es) | Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso. | |
MX2019007100A (es) | Derivados de tiazina y oxazina biciclicos como inhibidores de beta-secretasa y metodos de uso. | |
MX2012010657A (es) | Compuestos de espiro amino-dihidrooxazina y amino-dihidrotiazina como moduladores de beta-secretasa y su uso medico. | |
MX2019007103A (es) | Derivados de tiazina condensados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso. | |
EA201000332A1 (ru) | 1,3-двузамещенные 4-фенил-1н-пиридин-2-оны | |
MX2011003691A (es) | Derivados de indol y benzomorfolina como moduladores de los receptores de glutamato metabotropico. | |
MX2009012608A (es) | Compuestos de hidroxietil amina substituidos como moduladores de beta-secretasa y metodos de uso. | |
MX2010002538A (es) | 4-(aril-x-fenil)-1h-piridin-2-onas 1,3-disubstituidas. | |
EA017914B8 (ru) | 1,4-ДВУЗАМЕЩЕННЫЕ 3-ЦИАНОПИРИДОНОВЫЕ ПРОИЗВОДНЫЕ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ПОЗИТИВНЫХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ mGluR2 | |
ATE534625T1 (de) | Substituierte n-phenyl-bipyrrolidinharnstoffe und deren therapeutische verwendung | |
ATE525350T1 (de) | Substituierte n-phenyl- bipyrrolidincarbonsäureamide und deren therapeutische verwendung | |
IL202236A0 (en) | Prolinamide derivatives as nk3 antagonists | |
MX2018014164A (es) | Intermedios para la sintesis de derivados de acido biliar, en particular, de acido obeticolico. | |
MX2017008083A (es) | Compuestos 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2h-pirrol-5-amina inhibidores de beta-secretasa. | |
EA201691831A1 (ru) | Гетероароматические соединения и их применение в качестве допаминовых d1 лигандов | |
MD20160109A2 (ro) | Compuşi heteroaromatici şi utilizarea lor ca liganzi ai dopaminei D1 | |
PH12014502780A1 (en) | Azetidine and piperidine compounds useful as pde10 inhibitors | |
AU2008258664A8 (en) | Prolinamide-tetrazole derivatives as NK3 receptor antagonists |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG | Grant or registration |