AR079334A1 - Derivados de oxazin amino - Google Patents
Derivados de oxazin aminoInfo
- Publication number
- AR079334A1 AR079334A1 ARP100104543A ARP100104543A AR079334A1 AR 079334 A1 AR079334 A1 AR 079334A1 AR P100104543 A ARP100104543 A AR P100104543A AR P100104543 A ARP100104543 A AR P100104543A AR 079334 A1 AR079334 A1 AR 079334A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halogen
- alkoxy
- cyano
- group
- 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
- C07D413/02—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
-
- 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
- A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- 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
- 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
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Estos compuestos son inhibidores de la BACE2 y pueden emplearse como medicamentos para el tratamiento o prevencion de enfermedades, por ejemplo de la diabetes. Procesos de obtencion y composiciones farmacéuticas. Reivindicacion 1: Compuestos de la formula (1) en la que R1 es hidrogeno o alquilo C1-7; R2 es hidrogeno o alquilo C1-7; o R1 y R2 junto con el átomo de C al que están unidos forman un anillo cicloalquilo C3-7; R3 es alquilo C1-7 o cicloalquilo C3-7; o R2 y R3 junto con los átomos de C a los que están unidos forman un anillo cicloalquilo C3-7 o un anillo O-heterociclilo de 3 a 7 eslabones; R4 se elige entre el grupo formado por hidrogeno, alquilo C1-7, halogeno, ciano y alcoxi C1-7; R5 es arilo, sin sustituir o sustituido por uno, dos o tres restos elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7, ciano, hidroxi-alquilo C1-7, oxo y fenilo, un heteroarilo, sin sustituir o sustituido por uno, dos o tres restos elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7, ciano, hidroxi-alquilo C1-7, oxo y fenilo, alquilo C1-7, sin sustituir o sustituido por uno, dos, tres, cuatro o cinco restos elegidos individualmente entre el grupo formado por halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7, ciano e hidroxi-alquilo C1-7, anillo cicloalquilo C3-7, sin sustituir o sustituido por uno, dos o tres restos elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7, ciano e hidroxi-alquilo C1-7, un anillo O-heterociclilo de 3 a 7 eslabones, sin sustituir o sustituido por uno, dos o tres restos elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7, ciano e hidroxi-alquilo C1-7, o las sales farmacéuticamente aceptables de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09178642 | 2009-12-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR079334A1 true AR079334A1 (es) | 2012-01-18 |
Family
ID=43478012
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100104543A AR079334A1 (es) | 2009-12-10 | 2010-12-09 | Derivados de oxazin amino |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US7964594B1 (es) |
| EP (1) | EP2509966B1 (es) |
| JP (2) | JP2013513568A (es) |
| KR (1) | KR101437750B1 (es) |
| CN (1) | CN102652129A (es) |
| AR (1) | AR079334A1 (es) |
| BR (1) | BR112012013322A2 (es) |
| CA (1) | CA2780693A1 (es) |
| MX (1) | MX2012005810A (es) |
| RU (1) | RU2012126083A (es) |
| TW (1) | TW201125863A (es) |
| WO (1) | WO2011070029A1 (es) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007049532A1 (ja) | 2005-10-25 | 2007-05-03 | Shionogi & Co., Ltd. | アミノジヒドロチアジン誘導体 |
| TW200902526A (en) | 2007-04-24 | 2009-01-16 | Shionogi & Amp Co Ltd | Aminodihydrothiazin derivative substituted with a cyclic group |
| 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 |
| CA2727859C (en) | 2008-06-13 | 2016-11-01 | Shionogi & Co., Ltd. | SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY |
| WO2010047372A1 (ja) | 2008-10-22 | 2010-04-29 | 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 |
| AR077328A1 (es) | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
| WO2011044187A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | 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 |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| 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 |
| CA2783958A1 (en) | 2009-12-11 | 2011-06-16 | Shionogi & Co., Ltd. | Oxazine derivative |
| AU2011321427A1 (en) | 2010-10-29 | 2013-05-02 | Shionogi & Co., Ltd. | Naphthyridine derivative |
| US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
| US8524897B2 (en) | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
| PH12013501480A1 (en) | 2011-01-13 | 2022-10-26 | Novartis Ag | Novel heterocyclic derivatives and their use in the treatment of neurological disorders |
| WO2012138590A1 (en) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds 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 |
| 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 |
| 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 |
| US8785436B2 (en) * | 2011-05-16 | 2014-07-22 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE 1 and/or BACE2 inhibitors |
| 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 |
| RU2599256C2 (ru) * | 2011-06-07 | 2016-10-10 | Ф. Хоффманн-Ля Рош Аг | [1,3]оксазины |
| PE20140623A1 (es) * | 2011-06-07 | 2014-05-30 | Hoffmann La Roche | Halogenoalquil-1,3-oxazinas como inhibidores de la bace1 y/o bace2 |
| KR20140054295A (ko) | 2011-08-22 | 2014-05-08 | 머크 샤프 앤드 돔 코포레이션 | Bace 억제제로서의 2-스피로-치환된 이미노티아진 및 그의 모노- 및 디옥시드, 조성물 및 그의 용도 |
| UY34278A (es) | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
| US20130073953A1 (en) * | 2011-09-21 | 2013-03-21 | Timothy Onyenobi | News headline screenshot viewing system |
| US8338413B1 (en) | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| WO2013142613A1 (en) * | 2012-03-20 | 2013-09-26 | Elan Pharmaceuticals, Inc. | Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof |
| JO3143B1 (ar) * | 2012-04-03 | 2017-09-20 | Lilly Co Eli | مركبات تتراهيدرو بيرولو ثيازين |
| 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 |
| JP2016501827A (ja) * | 2012-10-24 | 2016-01-21 | 塩野義製薬株式会社 | Ｂａｃｅ１阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 |
| US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| US9489013B2 (en) | 2012-12-20 | 2016-11-08 | Merck Sharp & Dohme Corp. | C6-azaspiro iminothiadiazine dioxides as bace inhibitors, compositions, and their use |
| TW201446758A (zh) | 2013-03-01 | 2014-12-16 | Amgen Inc | 作爲β－分泌酶抑制劑的全氟化５，６－二氫－４Ｈ－１，３－□－２－胺化合物及其用途 |
| AP2015008716A0 (en) | 2013-03-08 | 2015-09-30 | Amgen Inc | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| US9045477B2 (en) * | 2013-03-15 | 2015-06-02 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| EP2989081A1 (en) * | 2013-04-26 | 2016-03-02 | F. Hoffmann-La Roche AG | Synthesis of bace inhibitors |
| 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 |
| CN106795147B (zh) | 2014-08-08 | 2020-09-22 | 美国安进公司 | 作为β-分泌酶抑制剂的环丙基稠合噻嗪-2-胺化合物和使用方法 |
| CR20170426A (es) | 2015-03-20 | 2017-10-23 | Hoffmann La Roche | Inhibidores de bace 1 |
| EP3784674B1 (en) | 2018-04-27 | 2023-02-22 | Shionogi & Co., Ltd | Tetrahydropyranooxazine derivatives having selective bace1 inhibitory activity |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60003791T2 (de) * | 1999-02-09 | 2004-02-05 | The University Of Virginia Alumni Patents Foundation | Felbamat-derivate |
| US7109217B2 (en) * | 2002-11-12 | 2006-09-19 | Merck & Co., Inc. | Phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease |
| NZ552031A (en) | 2004-06-16 | 2009-06-26 | Wyeth Corp | Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase |
| CN101084199A (zh) * | 2004-10-15 | 2007-12-05 | 阿斯利康(瑞典)有限公司 | 取代的氨基化合物及其用途 |
| TW200730523A (en) | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
| WO2007049532A1 (ja) | 2005-10-25 | 2007-05-03 | Shionogi & Co., Ltd. | アミノジヒドロチアジン誘導体 |
| TW200902526A (en) * | 2007-04-24 | 2009-01-16 | Shionogi & Amp Co Ltd | Aminodihydrothiazin derivative substituted with a cyclic group |
| AU2009205072C1 (en) | 2008-01-18 | 2016-10-13 | Eisai R & D Management Co., Ltd. | Condensed aminodihydrothiazine derivative |
| GB0912778D0 (en) * | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| 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 |
-
2010
- 2010-12-02 US US12/958,436 patent/US7964594B1/en not_active Expired - Fee Related
- 2010-12-07 CN CN2010800555310A patent/CN102652129A/zh active Pending
- 2010-12-07 CA CA2780693A patent/CA2780693A1/en not_active Abandoned
- 2010-12-07 RU RU2012126083/04A patent/RU2012126083A/ru not_active Application Discontinuation
- 2010-12-07 MX MX2012005810A patent/MX2012005810A/es active IP Right Grant
- 2010-12-07 EP EP10790920.2A patent/EP2509966B1/en not_active Not-in-force
- 2010-12-07 KR KR1020127017733A patent/KR101437750B1/ko active IP Right Grant
- 2010-12-07 WO PCT/EP2010/069098 patent/WO2011070029A1/en active Application Filing
- 2010-12-07 JP JP2012542524A patent/JP2013513568A/ja active Pending
- 2010-12-07 BR BR112012013322A patent/BR112012013322A2/pt not_active IP Right Cessation
- 2010-12-09 TW TW099143073A patent/TW201125863A/zh unknown
- 2010-12-09 AR ARP100104543A patent/AR079334A1/es unknown
-
2014
- 2014-11-07 JP JP2014227180A patent/JP2015051992A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| RU2012126083A (ru) | 2014-01-20 |
| WO2011070029A1 (en) | 2011-06-16 |
| US20110144098A1 (en) | 2011-06-16 |
| KR101437750B1 (ko) | 2014-09-03 |
| CA2780693A1 (en) | 2011-06-16 |
| TW201125863A (en) | 2011-08-01 |
| CN102652129A (zh) | 2012-08-29 |
| JP2013513568A (ja) | 2013-04-22 |
| BR112012013322A2 (pt) | 2019-09-24 |
| MX2012005810A (es) | 2012-06-12 |
| EP2509966A1 (en) | 2012-10-17 |
| EP2509966B1 (en) | 2014-10-22 |
| JP2015051992A (ja) | 2015-03-19 |
| KR20120103694A (ko) | 2012-09-19 |
| US7964594B1 (en) | 2011-06-21 |
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Legal Events
| Date | Code | Title | Description |
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| FB | Suspension of granting procedure |