BR112013016856A2 - composto, uso de um composto, composição farmacêutica e produto farmacêutico - Google Patents
composto, uso de um composto, composição farmacêutica e produto farmacêuticoInfo
- Publication number
- BR112013016856A2 BR112013016856A2 BR112013016856A BR112013016856A BR112013016856A2 BR 112013016856 A2 BR112013016856 A2 BR 112013016856A2 BR 112013016856 A BR112013016856 A BR 112013016856A BR 112013016856 A BR112013016856 A BR 112013016856A BR 112013016856 A2 BR112013016856 A2 BR 112013016856A2
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- alkyl
- optionally substituted
- pharmaceutical
- inhibitory effect
- Prior art date
Links
Classifications
-
- 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
- C07D513/12—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 three hetero rings
- C07D513/14—Ortho-condensed systems
-
- 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
- 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
- A61K31/542—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 ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- C07D279/08—1,3-Thiazines; Hydrogenated 1,3-thiazines condensed with carbocyclic rings or ring 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
Abstract
composto, uso de um composto, composição farmacêutica e produto farmacêutico a presente invenção diz respeito a um derivado de aminodi-hidrotiazina fundida da fórmula (i): em que r é hidrogênio ou alquila c~ 1~-~ 6~, opcionalmente substituídos por um até cinco átomos de halógeno; n é 0,1,2 ou 3; ar é fenila ou um grupo heteroaromático de 5 ou 6 membros que contêm de 1,2, ou 3 átomos n, ar este que é opcionalmente substituído por um até três substituintes selecionados de hal, hidroxila, -cn, alquila c~ 1-~ 6~, alquila c~ 1~-~ 6~ e alcóxi c~ 1~-~ 6~ são opcionalmente substituídos por um até três átomos de halógeno; e seus sais farmaceuticamente aceitáveis; composto este que tem um efeito inibidor da produção a<225> ou um efeito inibidor de bace1 e é útil como um agente profilático ou terapêutico para uma doença neurodegenarativa causada por a<225> e tipificada pela demência do tipo de alzheimer.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB1100181.5A GB201100181D0 (en) | 2011-01-06 | 2011-01-06 | Fused aminodihydrothiazine derivatives |
PCT/EP2012/050122 WO2012093148A1 (en) | 2011-01-06 | 2012-01-05 | Fused aminodihydrothiazine derivatives |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112013016856A2 true BR112013016856A2 (pt) | 2017-08-01 |
Family
ID=43663873
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112013016856A BR112013016856A2 (pt) | 2011-01-06 | 2012-01-05 | composto, uso de um composto, composição farmacêutica e produto farmacêutico |
Country Status (12)
Country | Link |
---|---|
US (1) | US8822455B2 (pt) |
EP (1) | EP2661267A1 (pt) |
JP (1) | JP2014501769A (pt) |
KR (1) | KR20130131399A (pt) |
CN (1) | CN103429244A (pt) |
AU (1) | AU2012204890A1 (pt) |
BR (1) | BR112013016856A2 (pt) |
CA (1) | CA2822777A1 (pt) |
GB (1) | GB201100181D0 (pt) |
MX (1) | MX2013007490A (pt) |
RU (1) | RU2013136542A (pt) |
WO (1) | WO2012093148A1 (pt) |
Families Citing this family (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2537898T3 (es) | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
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 |
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 |
CA2711655C (en) | 2008-01-18 | 2013-03-05 | Eisai R&D Management Co., Ltd. | Condensed aminodihydrothiazine derivative |
US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 塩野義製薬株式会社 | Bace1阻害活性を有する2−アミノピリミジン−4−オンおよび2−アミノピリジン誘導体 |
GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
BR112012013854A2 (pt) | 2009-12-11 | 2019-09-24 | Shionogi & Co | derivados de oxazina. |
WO2012057247A1 (ja) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
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 |
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 |
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 |
GB201212816D0 (en) * | 2012-07-19 | 2012-09-05 | Eisai Ltd | Novel compounds |
GB201212871D0 (en) * | 2012-07-20 | 2012-09-05 | Eisai Ltd | Novel compounds |
WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
EP2912041B1 (en) | 2012-10-26 | 2016-12-14 | Eli Lilly and Company | Tetrahydropyrrolothiazine derivatives as bace inhibitors |
TWI593692B (zh) | 2013-03-12 | 2017-08-01 | 美國禮來大藥廠 | 四氫吡咯并噻嗪化合物 |
JO3318B1 (ar) | 2013-06-18 | 2019-03-13 | Lilly Co Eli | مثبطات bace |
AR103680A1 (es) | 2015-02-23 | 2017-05-24 | Lilly Co Eli | Inhibidores selectivos de bace1 |
AR104241A1 (es) | 2015-04-29 | 2017-07-05 | Lilly Co Eli | Derivados de tetrahidrofuro tiazina como inhibidores de bace1 selectivos |
AR118235A1 (es) * | 2019-03-05 | 2021-09-22 | Eisai R&D Man Co Ltd | Heterociclos pentacíclicos |
Family Cites Families (46)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3227713A (en) | 1966-01-04 | Azine derivatives | ||
US3235551A (en) | 1966-02-15 | Novel derivatives of | ||
JPH0967355A (ja) | 1995-08-31 | 1997-03-11 | Tokyo Tanabe Co Ltd | チアジン誘導体、チアゾール誘導体及びそれらの製造方法 |
US6642237B1 (en) | 1999-11-24 | 2003-11-04 | Merck & Co., Inc. | Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof |
AU2001258771A1 (en) | 2000-05-19 | 2001-11-26 | Takeda Chemical Industries Ltd. | -secretase inhibitors |
US6562783B2 (en) | 2001-05-30 | 2003-05-13 | Neurologic, Inc. | Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors |
AU2003223093B2 (en) | 2002-05-03 | 2010-02-04 | Israel Institute For Biological Research | Methods and compositions for treatment of central and peripheral nervous system disorders and novel compounds useful therefor |
AU2003254844A1 (en) | 2002-08-09 | 2004-02-25 | Takeda Chemical Industries, Ltd. | Substituted amino compounds and use thereof |
AU2003285012A1 (en) | 2002-10-24 | 2004-05-13 | Sepracor, Inc. | Compositions comprising zopiclone derivatives and methods of making and using the same |
JP2004149429A (ja) | 2002-10-29 | 2004-05-27 | Takeda Chem Ind Ltd | インドール化合物およびその用途 |
EP1562897B1 (en) | 2002-11-12 | 2009-09-16 | Merck & Co., Inc. | Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer s disease |
JP5020638B2 (ja) | 2003-12-15 | 2012-09-05 | シェーリング コーポレイション | 複素環式アスパルチルプロテアーゼインヒビター |
US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
CA2561267A1 (en) | 2004-03-30 | 2005-10-20 | Merck & Co., Inc. | 2-aminothiazole compounds useful as aspartyl protease inhibitors |
PE20060664A1 (es) | 2004-09-15 | 2006-08-04 | Novartis Ag | Amidas biciclicas como inhibidores de cinasa |
WO2006041405A1 (en) | 2004-10-15 | 2006-04-20 | Astrazeneca Ab | Substituted amino-pyrimidones and uses thereof |
JP2008516945A (ja) | 2004-10-15 | 2008-05-22 | アストラゼネカ・アクチエボラーグ | 置換されたアミノ化合物およびそれらの使用 |
JP2008526999A (ja) | 2005-01-19 | 2008-07-24 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病治療用ベータ−セクレターゼインヒビターとして活性な置換へテロ環含有三級カルビナミン |
TWI332005B (en) | 2005-06-14 | 2010-10-21 | Schering Corp | Aspartyl protease inhibitors |
JP2009502786A (ja) | 2005-07-18 | 2009-01-29 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病を治療するためのスピロピペリジンβ−セクレターゼ阻害剤 |
ES2537898T3 (es) | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
EP2004630A4 (en) | 2006-04-05 | 2010-05-19 | Astrazeneca Ab | 2-AMINOPYRIMIDIN-4-ONES AND THEIR USE FOR THE TREATMENT OR PREVENTION OF PATHOLOGIES RELATED TO PROTEIN A |
JP5117382B2 (ja) | 2006-05-31 | 2013-01-16 | 第一三共株式会社 | 7員環化合物の製造方法 |
US8168641B2 (en) | 2006-06-12 | 2012-05-01 | Schering Corporation | Aspartyl protease inhibitors |
WO2008073365A1 (en) | 2006-12-12 | 2008-06-19 | Schering Corporation | Aspartyl protease inhibitors |
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 |
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 |
PE20091236A1 (es) | 2007-11-22 | 2009-09-16 | Astrazeneca Ab | Derivados de pirimidina como immunomoduladores de tlr7 |
CA2711655C (en) | 2008-01-18 | 2013-03-05 | Eisai R&D Management Co., Ltd. | Condensed aminodihydrothiazine derivative |
AU2009239535A1 (en) * | 2008-04-22 | 2009-10-29 | Schering Corporation | Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use |
TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
US8501733B2 (en) | 2008-07-28 | 2013-08-06 | 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 |
US8450308B2 (en) | 2008-08-19 | 2013-05-28 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
KR20110076965A (ko) | 2008-09-30 | 2011-07-06 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 신규한 축합 아미노 디하이드로티아진 유도체 |
SG173466A1 (en) | 2009-03-13 | 2011-09-29 | Vitae Pharmaceuticals Inc | Inhibitors of beta-secretase |
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 |
GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
EP2588467A1 (en) | 2010-07-01 | 2013-05-08 | Amgen Inc. | Heterocyclic compounds and their use as inhibitors of pi3k activity |
GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
BR112013016241A2 (pt) | 2011-01-21 | 2016-07-12 | Eisai R&D Man Co Ltd | composto, e, método para fabricar um composto |
-
2011
- 2011-01-06 GB GBGB1100181.5A patent/GB201100181D0/en not_active Ceased
-
2012
- 2012-01-05 RU RU2013136542/04A patent/RU2013136542A/ru not_active Application Discontinuation
- 2012-01-05 KR KR1020137018349A patent/KR20130131399A/ko not_active Application Discontinuation
- 2012-01-05 US US13/978,062 patent/US8822455B2/en not_active Expired - Fee Related
- 2012-01-05 BR BR112013016856A patent/BR112013016856A2/pt not_active IP Right Cessation
- 2012-01-05 EP EP12700259.0A patent/EP2661267A1/en not_active Withdrawn
- 2012-01-05 WO PCT/EP2012/050122 patent/WO2012093148A1/en active Application Filing
- 2012-01-05 AU AU2012204890A patent/AU2012204890A1/en not_active Abandoned
- 2012-01-05 CN CN2012800048141A patent/CN103429244A/zh active Pending
- 2012-01-05 JP JP2013547855A patent/JP2014501769A/ja active Pending
- 2012-01-05 MX MX2013007490A patent/MX2013007490A/es unknown
- 2012-01-05 CA CA2822777A patent/CA2822777A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
CA2822777A1 (en) | 2012-07-12 |
JP2014501769A (ja) | 2014-01-23 |
WO2012093148A1 (en) | 2012-07-12 |
RU2013136542A (ru) | 2015-02-20 |
AU2012204890A1 (en) | 2013-08-01 |
GB201100181D0 (en) | 2011-02-23 |
US8822455B2 (en) | 2014-09-02 |
US20140011802A1 (en) | 2014-01-09 |
MX2013007490A (es) | 2013-08-15 |
CN103429244A (zh) | 2013-12-04 |
KR20130131399A (ko) | 2013-12-03 |
EP2661267A1 (en) | 2013-11-13 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
BR112013016856A2 (pt) | composto, uso de um composto, composição farmacêutica e produto farmacêutico | |
BR112013018601A2 (pt) | composto, uso de composto, composição farmacêutica, e, produto farmacêutico | |
GEP20207105B (en) | 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2yl carbamate derivatives as magl inhibitors | |
BR112014001801A2 (pt) | indazóis | |
SG10201805033XA (en) | Glyoxamide substituted pyrrolamide derivatives and the use thereof as medicaments for the treatment of hepatitis b | |
BR112015021983A2 (pt) | compostos heterocíclicos e usos dos mesmos | |
MY174042A (en) | Fused bicyclic sulfamoyl derivative and the use thereof as medicaments for the treatment of hepatitis b. | |
PH12014501283A1 (en) | 4`-azido, 3``-fluoro substituted nucleoside derivatives as inhibitors of hcv rna replication | |
MX2015014033A (es) | Derivados de n-fenil-carboxamida y su uso como medicamentos para el tratamiento de la hepatitis b. | |
BR112015001502A2 (pt) | derivados de tipo azaindazol ou diazaindazol para tratamento de dor | |
EA201001683A1 (ru) | Производные фенил- или пиридинилзамещенных индазолов | |
CO7280475A2 (es) | Derivados de azaindol que actuan como inhibidores de pi3k | |
EA201390163A1 (ru) | Гетеробициклические производные в качетстве ингибиторов hcv | |
GEP20176631B (en) | Alkoxy pyrazoles as soluble guanylate cyclase activators | |
JO3115B1 (ar) | مركبات بيريدازينون واستخدامها كمثبطات daao | |
MX340033B (es) | Derivados heterobiciclicos como inhibidores del virus de la hepatitis c. | |
BR112013001632A2 (pt) | composto, composição farmacêutica, método de inibir uma atividade uma jak quinase in vitro, uso de um composto, ou da composição farmacêutica, e, método de fabricar um composto | |
UY33191A (es) | Derivados de pirazina | |
BR112015031878A2 (pt) | composição farmacêutica | |
GEP20207108B (en) | Substituted 2,4 diamino-quinoline as new anticancer agents | |
BR112013030264A2 (pt) | ácidos acéticos de benzociclohepteno | |
WO2013177534A3 (en) | New salicylic acid derivatives, pharmaceutically acceptable salt thereof, composition thereof and method of use thereof | |
BR112016011778A8 (pt) | pirazol fluorofenila, seus usos, e composição farmacêutica | |
AU2012360910A8 (en) | Quinazolinone derivatives as HCV inhibitors | |
BR112015006243A2 (pt) | agentes antibacterianos de fenicol |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] | ||
B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |