WO2011071057A1 - Composition pharmaceutique pour le traitement ou la prévention de la maladie d'alzheimer contenant un dérivé hétérocyclique contenant du soufre - Google Patents
Composition pharmaceutique pour le traitement ou la prévention de la maladie d'alzheimer contenant un dérivé hétérocyclique contenant du soufre Download PDFInfo
- Publication number
- WO2011071057A1 WO2011071057A1 PCT/JP2010/071957 JP2010071957W WO2011071057A1 WO 2011071057 A1 WO2011071057 A1 WO 2011071057A1 JP 2010071957 W JP2010071957 W JP 2010071957W WO 2011071057 A1 WO2011071057 A1 WO 2011071057A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- substituent
- optionally substituted
- compound
- optionally
- lower alkyl
- Prior art date
Links
- 0 CCOC(c1ncc[n]1*)=O Chemical compound CCOC(c1ncc[n]1*)=O 0.000 description 2
- UHYNYIGCGVDBTC-UHFFFAOYSA-N CCOC(c1ncc[nH]1)=O Chemical compound CCOC(c1ncc[nH]1)=O UHYNYIGCGVDBTC-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
- C07D279/06—1,3-Thiazines; Hydrogenated 1,3-thiazines not condensed with other rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Abstract
La présente invention a pour objet une composition pharmaceutique pour le traitement ou la prévention de la maladie d'Alzheimer. La présente invention concerne spécifiquement une composition pharmaceutique contenant un composé représenté par la formule (I) (dans laquelle le cycle A représente un groupe carbocyclique qui peut avoir un substituant, ou un groupe hétérocyclique qui peut avoir un substituant ; R1 représente un groupe alkyle inférieur qui peut avoir un substituant, ou analogue ; R2a et R2b représentent indépendamment un atome d'hydrogène, un groupe alkyle inférieur qui peut avoir un substituant, ou analogue ; et R3a et R3c représentent indépendamment un atome d'hydrogène, un atome d'halogène, un groupe hydroxy, un groupe alkyle inférieur qui peut avoir un substituant, ou analogue), un sel pharmaceutiquement acceptable du composé, ou un solvate du composé ou du sel pharmaceutiquement acceptable.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2011545220A JP5554346B2 (ja) | 2009-12-09 | 2010-12-08 | 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 |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2009279140 | 2009-12-09 | ||
JP2009-279140 | 2009-12-09 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2011071057A1 true WO2011071057A1 (fr) | 2011-06-16 |
Family
ID=44145601
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/JP2010/071957 WO2011071057A1 (fr) | 2009-12-09 | 2010-12-08 | Composition pharmaceutique pour le traitement ou la prévention de la maladie d'alzheimer contenant un dérivé hétérocyclique contenant du soufre |
Country Status (2)
Country | Link |
---|---|
JP (1) | JP5554346B2 (fr) |
WO (1) | WO2011071057A1 (fr) |
Cited By (36)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8168630B2 (en) | 2007-04-24 | 2012-05-01 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
WO2012057248A1 (fr) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | Dérivé de naphtyridine |
WO2012057247A1 (fr) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | Dérivé d'aminodihydropyrimidine fusionnée |
US8173642B2 (en) | 2005-10-25 | 2012-05-08 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives |
WO2012147762A1 (fr) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | Dérivé de pyridine et inhibiteur de bace-1 le contenant |
WO2012147763A1 (fr) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | Dérivé d'oxazine et inhibiteur de bace 1 le contenant |
WO2013013614A1 (fr) * | 2011-07-28 | 2013-01-31 | 南京英派药业有限公司 | 4-(3-hétéroarylarylamino)quinazoline et 1-(3-hétéroarylarylamino)isoquinoline utilisées en tant qu'inhibiteurs de la voie hedgehog et leur utilisation |
US8557826B2 (en) | 2009-10-08 | 2013-10-15 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use |
US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
US8569310B2 (en) | 2009-10-08 | 2013-10-29 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use |
US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
US8653067B2 (en) | 2007-04-24 | 2014-02-18 | Shionogi & Co., Ltd. | Pharmaceutical composition for treating Alzheimer's disease |
WO2014059185A1 (fr) | 2012-10-12 | 2014-04-17 | Amgen Inc. | Composés amino-dihydrothiazine et amino-dioxydo dihydrothiazine en tant qu'antagonistes de bêta-sécrétase et procédés d'utilisation |
US8703785B2 (en) | 2008-10-22 | 2014-04-22 | Shionogi & Co., Ltd. | 2-aminopyrimidin-4-one and 2-aminopyridine derivatives both having BACE1-inhibiting activity |
US8729071B2 (en) | 2009-10-08 | 2014-05-20 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as BACE inhibitors, compositions and their use |
WO2014078314A1 (fr) | 2012-11-15 | 2014-05-22 | Amgen Inc. | Composés d'amino-oxazine et d'amino-dihydrothiazine jouant le rôle de modulateurs de bêta-sécrétase et procédés d'utilisation |
JP2014526534A (ja) * | 2011-09-21 | 2014-10-06 | エフ.ホフマン−ラ ロシュ アーゲー | BACE1阻害剤としてのN−(3−(2−アミノ−6,6−ジフルオロ−4,4a,5,6,7,7a−ヘキサヒドロ−シクロペンタ[e][1,3]オキサジン−4−イル)−フェニル)−アミド |
US8999980B2 (en) | 2009-12-11 | 2015-04-07 | Shionogi & Co., Ltd. | Oxazine derivatives |
US9145426B2 (en) | 2011-04-07 | 2015-09-29 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
WO2015156421A1 (fr) | 2014-04-11 | 2015-10-15 | Shionogi & Co., Ltd. | Dérivés de dihydrothiazine et de dihydrooxazine présentant une activité inhibitrice de bace1 |
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 |
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 |
US9296734B2 (en) | 2013-03-01 | 2016-03-29 | Amgen Inc. | Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
US9522923B2 (en) | 2015-02-23 | 2016-12-20 | Eli Lilly And Company | Selective BACE1 inhibitors |
US9540359B2 (en) | 2012-10-24 | 2017-01-10 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity |
US9550762B2 (en) | 2014-08-08 | 2017-01-24 | Amgen, Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
US9611261B2 (en) | 2013-03-08 | 2017-04-04 | Amgen Inc. | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
WO2017061534A1 (fr) | 2015-10-08 | 2017-04-13 | Shionogi & Co., Ltd. | Dérivés de dihydrothiazine |
WO2017081615A1 (fr) | 2015-11-09 | 2017-05-18 | Wockhardt Limited | 7-oxo-6-(sulfooxy)-1,6-diazabicyclo[3.2.1] octane contenant des composés et leur utilisation dans le traitement d'infections bactériennes |
CN106795093A (zh) * | 2014-10-14 | 2017-05-31 | 先正达参股股份有限公司 | 用于制备1‑(3,5‑二氯苯基)‑2,2,2‑三氟乙酮及其衍生物的方法 |
WO2017175855A1 (fr) | 2016-04-08 | 2017-10-12 | Shionogi & Co., Ltd. | Forme posologique solide stabilisée |
US10011610B2 (en) | 2015-04-29 | 2018-07-03 | Eli Lilly And Company | Selective BACE1 inhibitors |
CN109134219A (zh) * | 2018-08-10 | 2019-01-04 | 五邑大学 | 一种合成苯偶酰类衍生物的方法 |
CN109422639A (zh) * | 2017-08-25 | 2019-03-05 | 浙江工业大学 | 一种合成1,2-二羰基类化合物的方法 |
US11629154B2 (en) | 2018-04-27 | 2023-04-18 | Shionogi & Co., Ltd. | Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity |
WO2023151642A1 (fr) * | 2022-02-10 | 2023-08-17 | Beigene , Ltd. | Composés hétérocycliques, compositions associées et méthodes de traitement faisant appel à ceux-ci |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2007049532A1 (fr) * | 2005-10-25 | 2007-05-03 | Shionogi & Co., Ltd. | Derive aminodihydrothiazine |
WO2008133274A1 (fr) * | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | Dérivés d'aminodihydrothiazine substitués par des groupes cycliques |
WO2008133273A1 (fr) * | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | Composition pharmaceutique pour le traitement de la maladie d'alzheimer |
WO2009134617A1 (fr) * | 2008-05-02 | 2009-11-05 | Eli Lilly And Company | Dérivés d’aminodihydrothiazine en tant qu’inhibiteurs de bace destinés au traitement de la maladie d’alzheimer |
WO2009151098A1 (fr) * | 2008-06-13 | 2009-12-17 | 塩野義製薬株式会社 | DÉRIVÉ HÉTÉROCYCLIQUE CONTENANT DU SOUFRE AYANT UNE ACTIVITÉ INHIBANT LA β-SÉCRÉTASE |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPWO2011058763A1 (ja) * | 2009-11-13 | 2013-03-28 | 塩野義製薬株式会社 | アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体 |
-
2010
- 2010-12-08 WO PCT/JP2010/071957 patent/WO2011071057A1/fr active Application Filing
- 2010-12-08 JP JP2011545220A patent/JP5554346B2/ja not_active Expired - Fee Related
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2007049532A1 (fr) * | 2005-10-25 | 2007-05-03 | Shionogi & Co., Ltd. | Derive aminodihydrothiazine |
WO2008133274A1 (fr) * | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | Dérivés d'aminodihydrothiazine substitués par des groupes cycliques |
WO2008133273A1 (fr) * | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | Composition pharmaceutique pour le traitement de la maladie d'alzheimer |
WO2009134617A1 (fr) * | 2008-05-02 | 2009-11-05 | Eli Lilly And Company | Dérivés d’aminodihydrothiazine en tant qu’inhibiteurs de bace destinés au traitement de la maladie d’alzheimer |
WO2009151098A1 (fr) * | 2008-06-13 | 2009-12-17 | 塩野義製薬株式会社 | DÉRIVÉ HÉTÉROCYCLIQUE CONTENANT DU SOUFRE AYANT UNE ACTIVITÉ INHIBANT LA β-SÉCRÉTASE |
Non-Patent Citations (1)
Title |
---|
HUANG, WEN-HAI ET AL.: "Pharmacophore model construction of beta-secretase inhibitors", HUAXUE XUEBAO, vol. 66, no. 16, 2008, pages 1889 - 1897 * |
Cited By (61)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8546380B2 (en) | 2005-10-25 | 2013-10-01 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives |
US9029358B2 (en) | 2005-10-25 | 2015-05-12 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives |
US8815851B2 (en) | 2005-10-25 | 2014-08-26 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives |
US8173642B2 (en) | 2005-10-25 | 2012-05-08 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives |
US8633188B2 (en) | 2005-10-25 | 2014-01-21 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives |
US8168630B2 (en) | 2007-04-24 | 2012-05-01 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
US8653067B2 (en) | 2007-04-24 | 2014-02-18 | Shionogi & Co., Ltd. | Pharmaceutical composition for treating Alzheimer's disease |
US8895548B2 (en) | 2007-04-24 | 2014-11-25 | Shionogi & Co., Ltd. | Pharmaceutical composition for treating alzheimer's disease |
US8884062B2 (en) | 2007-04-24 | 2014-11-11 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
US9273053B2 (en) | 2008-06-13 | 2016-03-01 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having Beta secretase inhibitory activity |
US9650371B2 (en) | 2008-06-13 | 2017-05-16 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
US8703785B2 (en) | 2008-10-22 | 2014-04-22 | Shionogi & Co., Ltd. | 2-aminopyrimidin-4-one and 2-aminopyridine derivatives both having BACE1-inhibiting activity |
US9428475B2 (en) | 2009-10-08 | 2016-08-30 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as BACE 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 |
US9475785B2 (en) | 2009-10-08 | 2016-10-25 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as BACE inhibitors, compositions and their use |
US9687494B2 (en) | 2009-10-08 | 2017-06-27 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
US8729071B2 (en) | 2009-10-08 | 2014-05-20 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as BACE inhibitors, compositions and their use |
US8569310B2 (en) | 2009-10-08 | 2013-10-29 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use |
US9029362B2 (en) | 2009-10-08 | 2015-05-12 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as brace inhibitors, compositions, and their use |
US8940748B2 (en) | 2009-10-08 | 2015-01-27 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
US9656974B2 (en) | 2009-12-11 | 2017-05-23 | Shionogi & Co., Ltd. | Oxazine derivatives |
US9290466B2 (en) | 2009-12-11 | 2016-03-22 | Shionogi & Co., Ltd. | Oxazine derivatives |
US8999980B2 (en) | 2009-12-11 | 2015-04-07 | Shionogi & Co., Ltd. | Oxazine derivatives |
US8927721B2 (en) | 2010-10-29 | 2015-01-06 | Shionogi & Co., Ltd. | Naphthyridine derivative |
US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
WO2012057247A1 (fr) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | Dérivé d'aminodihydropyrimidine fusionnée |
WO2012057248A1 (fr) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | Dérivé de naphtyridine |
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 |
US9145426B2 (en) | 2011-04-07 | 2015-09-29 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
CN103649082A (zh) * | 2011-04-26 | 2014-03-19 | 盐野义制药株式会社 | 吡啶衍生物和含有该吡啶衍生物的bace1抑制剂 |
WO2012147762A1 (fr) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | Dérivé de pyridine et inhibiteur de bace-1 le contenant |
US8883779B2 (en) | 2011-04-26 | 2014-11-11 | Shinogi & Co., Ltd. | Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them |
WO2012147763A1 (fr) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | Dérivé d'oxazine et inhibiteur de bace 1 le contenant |
WO2013013614A1 (fr) * | 2011-07-28 | 2013-01-31 | 南京英派药业有限公司 | 4-(3-hétéroarylarylamino)quinazoline et 1-(3-hétéroarylarylamino)isoquinoline utilisées en tant qu'inhibiteurs de la voie hedgehog et leur utilisation |
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 |
JP2014526534A (ja) * | 2011-09-21 | 2014-10-06 | エフ.ホフマン−ラ ロシュ アーゲー | BACE1阻害剤としてのN−(3−(2−アミノ−6,6−ジフルオロ−4,4a,5,6,7,7a−ヘキサヒドロ−シクロペンタ[e][1,3]オキサジン−4−イル)−フェニル)−アミド |
US9556135B2 (en) | 2012-10-12 | 2017-01-31 | Amgen, Inc. | Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use |
WO2014059185A1 (fr) | 2012-10-12 | 2014-04-17 | Amgen Inc. | Composés amino-dihydrothiazine et amino-dioxydo dihydrothiazine en tant qu'antagonistes de bêta-sécrétase et procédés d'utilisation |
US9540359B2 (en) | 2012-10-24 | 2017-01-10 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity |
US9758513B2 (en) | 2012-10-24 | 2017-09-12 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity |
WO2014078314A1 (fr) | 2012-11-15 | 2014-05-22 | Amgen Inc. | Composés d'amino-oxazine et d'amino-dihydrothiazine jouant le rôle de modulateurs de bêta-sécrétase et procédés d'utilisation |
JP2016511258A (ja) * | 2013-03-01 | 2016-04-14 | 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 |
US9296734B2 (en) | 2013-03-01 | 2016-03-29 | Amgen Inc. | Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
US9611261B2 (en) | 2013-03-08 | 2017-04-04 | Amgen Inc. | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
KR20160141849A (ko) | 2014-04-11 | 2016-12-09 | 시오노기세이야쿠가부시키가이샤 | Bace1 저해 작용을 갖는 디하이드로티아진 및 디하이드로옥사진 유도체 |
WO2015156421A1 (fr) | 2014-04-11 | 2015-10-15 | Shionogi & Co., Ltd. | Dérivés de dihydrothiazine et de dihydrooxazine présentant une activité inhibitrice de bace1 |
US9550762B2 (en) | 2014-08-08 | 2017-01-24 | Amgen, Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
CN106795093B (zh) * | 2014-10-14 | 2019-05-28 | 先正达参股股份有限公司 | 用于制备1-(3,5-二氯苯基)-2,2,2-三氟乙酮及其衍生物的方法 |
CN106795093A (zh) * | 2014-10-14 | 2017-05-31 | 先正达参股股份有限公司 | 用于制备1‑(3,5‑二氯苯基)‑2,2,2‑三氟乙酮及其衍生物的方法 |
US9522923B2 (en) | 2015-02-23 | 2016-12-20 | Eli Lilly And Company | Selective BACE1 inhibitors |
US10011610B2 (en) | 2015-04-29 | 2018-07-03 | Eli Lilly And Company | Selective BACE1 inhibitors |
WO2017061534A1 (fr) | 2015-10-08 | 2017-04-13 | Shionogi & Co., Ltd. | Dérivés de dihydrothiazine |
WO2017081615A1 (fr) | 2015-11-09 | 2017-05-18 | Wockhardt Limited | 7-oxo-6-(sulfooxy)-1,6-diazabicyclo[3.2.1] octane contenant des composés et leur utilisation dans le traitement d'infections bactériennes |
WO2017175855A1 (fr) | 2016-04-08 | 2017-10-12 | Shionogi & Co., Ltd. | Forme posologique solide stabilisée |
CN109422639A (zh) * | 2017-08-25 | 2019-03-05 | 浙江工业大学 | 一种合成1,2-二羰基类化合物的方法 |
CN109422639B (zh) * | 2017-08-25 | 2021-12-17 | 浙江工业大学 | 一种合成1,2-二羰基类化合物的方法 |
US11629154B2 (en) | 2018-04-27 | 2023-04-18 | Shionogi & Co., Ltd. | Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity |
CN109134219A (zh) * | 2018-08-10 | 2019-01-04 | 五邑大学 | 一种合成苯偶酰类衍生物的方法 |
WO2023151642A1 (fr) * | 2022-02-10 | 2023-08-17 | Beigene , Ltd. | Composés hétérocycliques, compositions associées et méthodes de traitement faisant appel à ceux-ci |
Also Published As
Publication number | Publication date |
---|---|
JPWO2011071057A1 (ja) | 2013-04-22 |
JP5554346B2 (ja) | 2014-07-23 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP5554346B2 (ja) | 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 | |
JP5572675B2 (ja) | βセクレターゼ阻害作用を有する含硫黄複素環誘導体 | |
JP5766198B2 (ja) | 縮合アミノジヒドロピリミジン誘導体 | |
JP2016028057A (ja) | オキサジン誘導体 | |
JPWO2011070781A1 (ja) | 置換アミノチアジン誘導体 | |
WO2012147763A1 (fr) | Dérivé d'oxazine et inhibiteur de bace 1 le contenant | |
WO2011058763A1 (fr) | Dérivé d'aminothiazine ou d'aminooxazine contenant un lieur amino | |
WO2011071109A1 (fr) | Composé hétérocyclique fusionné comportant un groupement amino | |
WO2012147762A1 (fr) | Dérivé de pyridine et inhibiteur de bace-1 le contenant | |
WO2010113848A1 (fr) | Dérivé isothiourée ou dérivé isourée ayant une activité inhibitrice de bace1 | |
JP2012250933A (ja) | 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 | |
JP2014101353A (ja) | 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 | |
WO2020046975A1 (fr) | Méthodes de traitement de maladies neurodégénératives |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
121 | Ep: the epo has been informed by wipo that ep was designated in this application |
Ref document number: 10835977 Country of ref document: EP Kind code of ref document: A1 |
|
WWE | Wipo information: entry into national phase |
Ref document number: 2011545220 Country of ref document: JP |
|
NENP | Non-entry into the national phase |
Ref country code: DE |
|
122 | Ep: pct application non-entry in european phase |
Ref document number: 10835977 Country of ref document: EP Kind code of ref document: A1 |