UY35361A - COMPUESTOS PERFLUORADOS DE 5,6-DIHIDRO-4H-1,3-OXAZIN-2-AMINA COMO INHIBIDORES DE BETA-SECRETASA y MÉTODOS DE USO - Google Patents
COMPUESTOS PERFLUORADOS DE 5,6-DIHIDRO-4H-1,3-OXAZIN-2-AMINA COMO INHIBIDORES DE BETA-SECRETASA y MÉTODOS DE USOInfo
- Publication number
- UY35361A UY35361A UY0001035361A UY35361A UY35361A UY 35361 A UY35361 A UY 35361A UY 0001035361 A UY0001035361 A UY 0001035361A UY 35361 A UY35361 A UY 35361A UY 35361 A UY35361 A UY 35361A
- Authority
- UY
- Uruguay
- Prior art keywords
- compounds
- beta
- dihidro
- amina
- oxazin
- Prior art date
Links
Classifications
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- 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 invención da a conocer una nueva clase de compuestos útiles para la modulación de la actividad d e la enzima beta-secretasa (BACE). Los compuestos poseen una Fórmula general I: 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 e n la memoria. También se dan a conocer composiciones farmacéuticas que comprenden los compuestos, y usos de los compuestos y composiciones para el t ratamiento de trastornos y/o condiciones asociadas con la formación y deposición de placa A-beta qu e resulta de la actividad biológica de BACE.
Applications Claiming Priority (3)
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 |
Publications (1)
Publication Number | Publication Date |
---|---|
UY35361A true UY35361A (es) | 2014-09-30 |
Family
ID=50349866
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
UY0001035361A UY35361A (es) | 2013-03-01 | 2014-03-05 | COMPUESTOS PERFLUORADOS DE 5,6-DIHIDRO-4H-1,3-OXAZIN-2-AMINA COMO INHIBIDORES DE BETA-SECRETASA y MÉTODOS 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)
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US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
BR112012013854A2 (pt) | 2009-12-11 | 2019-09-24 | Shionogi & Co | derivados de oxazina. |
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 |
CA2900433C (en) * | 2013-04-11 | 2021-06-22 | F. Hoffmann-La Roche Ag | Bace1 inhibitors |
MA39225A1 (fr) | 2014-02-19 | 2017-04-28 | H Lundbeck As | 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tétrahydropyridines utilisées en tant qu'inhibiteurs de bace1 dans le traitement de la maladie d'alzheimer |
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 |
WO2016022724A1 (en) | 2014-08-08 | 2016-02-11 | 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 |
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 |
MX2018001699A (es) | 2015-08-12 | 2018-05-07 | H Lundbeck As | 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidr opiridinas como inhibidores de bace1. |
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 |
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EP3423450B1 (en) * | 2016-03-01 | 2019-11-27 | H. Hoffnabb-La Roche Ag | Bace 1 inhibitors |
CA3047287A1 (en) * | 2016-12-15 | 2018-06-21 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
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 |
KR20210003872A (ko) | 2018-04-27 | 2021-01-12 | 시오노기 앤드 컴파니, 리미티드 | 선택적 bace1 억제 활성을 갖는 테트라하이드로피라노옥사진 유도체 |
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 |
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2014
- 2014-02-27 WO PCT/US2014/019100 patent/WO2014134341A1/en active Application Filing
- 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 AU AU2014223334A patent/AU2014223334C1/en active Active
- 2014-02-27 CA CA2902212A patent/CA2902212C/en active Active
- 2014-02-27 TW TW103106910A patent/TW201446758A/zh unknown
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AU2018204589A1 (en) | 2018-07-12 |
AU2014223334C1 (en) | 2018-10-18 |
AU2014223334B2 (en) | 2018-04-05 |
JP6389830B2 (ja) | 2018-09-12 |
US9296734B2 (en) | 2016-03-29 |
WO2014134341A1 (en) | 2014-09-04 |
TW201446758A (zh) | 2014-12-16 |
MX366855B (es) | 2019-07-26 |
MX2015011313A (es) | 2015-12-03 |
CA2902212C (en) | 2020-10-13 |
CA2902212A1 (en) | 2014-09-04 |
JP2016511258A (ja) | 2016-04-14 |
EP2961749A1 (en) | 2016-01-06 |
EP2961749B1 (en) | 2019-10-09 |
US20140249104A1 (en) | 2014-09-04 |
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