PE20110307A1 - Derivados de aminodihidrotiazina fusionada con actividad sobre la proteina beta-amiloide - Google Patents
Derivados de aminodihidrotiazina fusionada con actividad sobre la proteina beta-amiloideInfo
- Publication number
- PE20110307A1 PE20110307A1 PE2011000781A PE2011000781A PE20110307A1 PE 20110307 A1 PE20110307 A1 PE 20110307A1 PE 2011000781 A PE2011000781 A PE 2011000781A PE 2011000781 A PE2011000781 A PE 2011000781A PE 20110307 A1 PE20110307 A1 PE 20110307A1
- Authority
- PE
- Peru
- Prior art keywords
- beta
- group
- azanaftalen
- oxa
- carboxamide
- Prior art date
Links
- 102000013455 Amyloid beta-Peptides Human genes 0.000 title abstract 3
- 108010090849 Amyloid beta-Peptides Proteins 0.000 title abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 201000010374 Down Syndrome Diseases 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 206010044688 Trisomy 21 Diseases 0.000 abstract 1
- 230000004927 fusion Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003462 sulfoxides Chemical class 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
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
- C07D513/02—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
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
REFERIDA A UN COMPUESTO DERIVADO DE AMINODIHIDROTIAZINA FUSIONADA DE FORMULA (I), DONDE A ES UN GRUPO ARILO C6-C14, UN GRUPO HETEROARILO DE 5 A 6 MIEMBROS CON HETEROATOMOS TALES COMO N, S Y O, UN GRUPO HETEROCICLICO BENZO-FUSIONADO DE 9 A 10 MIEMBROS, ENTRE OTROS; L ES UN ENLACE, UN ATOMO DE OXIGENO, ENTRE OTROS; B ES CICLOALQUILO C3-C8, ARILO C6-C14, UN GRUPO HETEROCICLICO DE 5 A 10 MIEMBROS CON HETEROATOMOS TALES COMO N, S Y O, ENTRE OTROS; X ES UN ENLACE, ALQUILENO C1-C3, ENTRE OTROS; Y ES ALQUILENO C1-C3, ALQUENILENO C2-C3, ENTRE OTROS; Z ES O, S, SULFOXIDO, ENTRE OTROS; R1 Y R2 SON H, ALQUILO C1-C6, ALQUILCARBONILO C1-C6, ENTRE OTROS; R3, R4, R5 Y R6 SON H, OH, ALQUILO C1-C6, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-[3-((4aR*,8aS*)-2-AMINO-4,4a,5,6-TETRAHIDRO-7-OXA-3-TIA-1-AZANAFTALEN-8a-IL)-4-FLUOROFENIL]-5-CIANOPIRIDINA-2-CARBOXAMIDA, N-[3-((8S*,8aR*)-2-AMINO-4,4a,5,6-TETRAHIDRO-7-OXA-3-TIA-1-AZANAFTALEN-8a-IL)-4-FLUOROFENIL]-5-FLUOROMETOXIPIRAZINA-2-CARBOXAMIDA, N-[3-((4aR*,8aS*)-2-AMINO-4,4a,5,6-TETRAHIDRO-7-OXA-3-TIA-1-AZANAFTALEN-8a-IL)-4-FLUOROFENIL]-5-DIFLUOROMETOXIPIRAZINA-2-CARBOXAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN LA PRODUCCION DE PROTEINA BETA-AMILOIDE O LA ENZIMA 1 DE ESCISION DE LA PROTEINA PRECURSORA BETA-AMILOIDE, SIENDO UTILES EN EL TRATAMIENTO DE ENFERMEDADES NEURODEGENERATIVAS TALES COMO ALZHEIMER, SINDROME DE DOWN, ENTRE OTRAS
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10135908P | 2008-09-30 | 2008-09-30 | |
| JP2008252062 | 2008-09-30 | ||
| US17017909P | 2009-04-17 | 2009-04-17 | |
| JP2009100457 | 2009-04-17 | ||
| US22636509P | 2009-07-17 | 2009-07-17 | |
| JP2009168490 | 2009-07-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20110307A1 true PE20110307A1 (es) | 2011-05-21 |
Family
ID=42073450
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011000781A PE20110307A1 (es) | 2008-09-30 | 2009-09-28 | Derivados de aminodihidrotiazina fusionada con actividad sobre la proteina beta-amiloide |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US20110207723A1 (es) |
| EP (1) | EP2332943B1 (es) |
| JP (1) | JP5666304B2 (es) |
| KR (1) | KR20110076965A (es) |
| CN (1) | CN102171221B (es) |
| AR (1) | AR073406A1 (es) |
| AU (1) | AU2009300836B2 (es) |
| CA (1) | CA2738150A1 (es) |
| ES (1) | ES2539859T3 (es) |
| IL (1) | IL211933A (es) |
| MX (1) | MX2011003189A (es) |
| NZ (1) | NZ591878A (es) |
| PE (1) | PE20110307A1 (es) |
| TW (1) | TW201016708A (es) |
| WO (1) | WO2010038686A1 (es) |
| ZA (1) | ZA201102172B (es) |
Families Citing this family (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US8722708B2 (en) | 2005-06-14 | 2014-05-13 | Merck Sharp & Dohme Inc. | Substituted isoindolines as aspartyl protease inhibitors |
| AU2006259572A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Aspartyl protease inhibitors |
| ES2537898T3 (es) * | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
| KR20090015967A (ko) | 2006-06-12 | 2009-02-12 | 쉐링 코포레이션 | 헤테로사이클릭 아스파르틸 프로테아제 억제제 |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| KR20100017255A (ko) * | 2007-04-24 | 2010-02-16 | 시오노기 앤드 컴파니, 리미티드 | 환식기로 치환된 아미노다이하이드로싸이아진 유도체 |
| SI2233474T1 (sl) * | 2008-01-18 | 2015-11-30 | Eisai R&D Management Co., Ltd. | Kondenziran derivat aminodihidrotiazina |
| US8450331B2 (en) | 2008-04-22 | 2013-05-28 | Merck Sharp & Dohme Corp. | Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use |
| EP2305672B1 (en) * | 2008-06-13 | 2019-03-27 | Shionogi & Co., Ltd. | SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY |
| WO2010013794A1 (en) * | 2008-07-28 | 2010-02-04 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
| ES2539859T3 (es) * | 2008-09-30 | 2015-07-06 | Eisai R&D Management Co., Ltd. | Nuevo derivado de aminodihidrotiazina condensado |
| CN102186841A (zh) * | 2008-10-22 | 2011-09-14 | 盐野义制药株式会社 | 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物 |
| 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 |
| GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
| WO2011044184A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | 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 | |
| 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 |
| 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 |
| RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
| JP5766198B2 (ja) | 2010-10-29 | 2015-08-19 | 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 |
| CN103261199A (zh) | 2010-10-29 | 2013-08-21 | 盐野义制药株式会社 | 萘啶衍生物 |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| ES2624288T3 (es) | 2011-01-21 | 2017-07-13 | Eisai R&D Management Co., Ltd. | Métodos y compuestos útiles en la síntesis de derivados de aminodihidrotiazina condensados |
| 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 |
| US8877744B2 (en) * | 2011-04-04 | 2014-11-04 | Hoffmann-La Roche Inc. | 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors |
| WO2012138590A1 (en) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2012138734A1 (en) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| 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 |
| TW201302763A (zh) * | 2011-05-24 | 2013-01-16 | 必治妥美雅史谷比公司 | 用於減少β-類澱粉產生之化合物 |
| US8604024B2 (en) | 2011-05-24 | 2013-12-10 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
| EP2747769B1 (en) | 2011-08-22 | 2017-08-02 | Merck Sharp & Dohme Corp. | 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use |
| EP2751116B1 (en) * | 2011-08-31 | 2016-10-12 | Pfizer Inc | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds |
| JO3143B1 (ar) | 2012-04-03 | 2017-09-20 | Lilly Co Eli | مركبات تتراهيدرو بيرولو ثيازين |
| US9227942B2 (en) | 2012-04-27 | 2016-01-05 | Eisai R&D Management Co., Ltd. | Method for producing 5-(difluoromethyl)pyrazine-2-carboxylic acid and production intermediate thereof |
| CA2872154C (en) * | 2012-05-04 | 2016-08-23 | Pfizer Inc. | Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin-2-amine compounds as inhibitors of app, bace1 and bace2 |
| US9260455B2 (en) | 2012-09-20 | 2016-02-16 | Pfizer Inc. | Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| PL2912041T3 (pl) | 2012-10-26 | 2017-06-30 | Eli Lilly And Company | Pochodne tetrahydropirolotiazyny stanowiące inhibitory BACE |
| EP2931731A1 (en) | 2012-12-11 | 2015-10-21 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1 |
| US9403846B2 (en) | 2012-12-19 | 2016-08-02 | Pfizer Inc. | Carbocyclic- and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| CA2897678A1 (en) | 2013-02-13 | 2014-08-21 | Pfizer Inc. | Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| US9233981B1 (en) * | 2013-02-15 | 2016-01-12 | Pfizer Inc. | Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| 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 |
| CN106459088A (zh) * | 2014-04-10 | 2017-02-22 | 辉瑞公司 | 2‑氨基‑6‑甲基‑4,4a,5,6‑四氢吡喃并[3,4‑d][1,3]噻嗪‑8a(8H)‑基‑1,3‑噻唑‑4‑基酰胺 |
| AR103680A1 (es) | 2015-02-23 | 2017-05-24 | Lilly Co Eli | Inhibidores selectivos de bace1 |
| CN107257795A (zh) * | 2015-03-19 | 2017-10-17 | 伊莱利利公司 | 选择性bace1抑制剂 |
| AR104241A1 (es) | 2015-04-29 | 2017-07-05 | Lilly Co Eli | Derivados de tetrahidrofuro tiazina como inhibidores de bace1 selectivos |
| EP3353183A1 (en) | 2015-09-24 | 2018-08-01 | Pfizer Inc | N-[2-(2-amino-6,6-disubstituted-4, 4a, 5, 6-tetrahydropyrano [3,4-d][1,3]thiazin-8a (8h)-yl) -1, 3-thiazol-4-yl]amides |
| WO2017051294A1 (en) | 2015-09-24 | 2017-03-30 | Pfizer Inc. | N-[2-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2h-1,2,4-thiadiazin-5-yl)-1,3-thiazol-4-yl] amides useful as bace inhibitors |
| WO2017051303A1 (en) | 2015-09-24 | 2017-03-30 | Pfizer Inc. | Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors |
| US20210355138A1 (en) | 2016-08-11 | 2021-11-18 | Eli Lilly And Company | Aminothiazinies and their use as bace1 inhibitors |
| MX388697B (es) | 2016-12-15 | 2025-03-20 | Amgen Inc | Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso. |
| WO2018112086A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| WO2018112081A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| CA3047290A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use |
| WO2018112084A1 (en) * | 2016-12-15 | 2018-06-21 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| CN107892697B (zh) | 2016-12-26 | 2020-11-03 | 郑州泰基鸿诺医药股份有限公司 | 一种[1,3]噻嗪-2-胺类化合物及应用,药物组合物 |
| CN111808057B (zh) * | 2019-04-10 | 2023-05-09 | 四川大学 | 利用α-O-烯基砜作为亲电试剂的铃木反应及其应用 |
Family Cites Families (28)
| 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 |
| KR20020097484A (ko) | 2000-05-19 | 2002-12-31 | 다케다 야쿠힌 고교 가부시키가이샤 | β-씨크리타아제 억제제 |
| US6562783B2 (en) | 2001-05-30 | 2003-05-13 | Neurologic, Inc. | Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors |
| NZ560368A (en) | 2002-05-03 | 2008-11-28 | Israel Inst Biolog Res | Methods and compostions for treatment of central and peripheral nervous system disorders and novel compounds useful therefor |
| WO2004014843A1 (ja) | 2002-08-09 | 2004-02-19 | Takeda Chemical Industries, Ltd. | 置換アミノ化合物およびその用途 |
| 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 |
| MY149978A (en) | 2003-12-15 | 2013-11-15 | Merck Sharp & Dohme | Heterocyclic aspartyl protease inhibitors |
| WO2005097767A1 (en) | 2004-03-30 | 2005-10-20 | Merck & Co., Inc. | 2-aminothiazole compounds useful as aspartyl protease inhibitors |
| CN1938288A (zh) * | 2004-03-30 | 2007-03-28 | 默克公司 | 可用作天冬氨酰蛋白酶抑制剂的2-氨基噻唑化合物 |
| EP1802587A4 (en) | 2004-10-15 | 2010-02-17 | Astrazeneca Ab | SUBSTITUTED AMINO BINDINGS AND THEIR APPLICATIONS |
| US20090062282A1 (en) * | 2004-10-15 | 2009-03-05 | Astrazeneca Ab | Substituted Amino-Pyrimidones and Uses Thereof |
| US8338614B2 (en) | 2005-01-19 | 2012-12-25 | Merck, Sharp & Dohme Corp. | Tertiary carbinamines having substituted heterocycles which are active as β-secretase inhibitors for the treatment of alzheimer's disease |
| WO2007011810A1 (en) | 2005-07-18 | 2007-01-25 | Merck & Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
| ES2537898T3 (es) | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
| JP2009184924A (ja) | 2006-05-31 | 2009-08-20 | Eisai R & D Management Co Ltd | 生物学的試薬用化合物 |
| KR20100017255A (ko) | 2007-04-24 | 2010-02-16 | 시오노기 앤드 컴파니, 리미티드 | 환식기로 치환된 아미노다이하이드로싸이아진 유도체 |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| SI2233474T1 (sl) * | 2008-01-18 | 2015-11-30 | Eisai R&D Management Co., Ltd. | Kondenziran derivat aminodihidrotiazina |
| TWI431004B (zh) * | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
| 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 |
| WO2010013794A1 (en) | 2008-07-28 | 2010-02-04 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
| ES2539859T3 (es) * | 2008-09-30 | 2015-07-06 | Eisai R&D Management Co., Ltd. | Nuevo derivado de aminodihidrotiazina condensado |
| 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 |
| GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
-
2009
- 2009-09-28 ES ES09817719.9T patent/ES2539859T3/es active Active
- 2009-09-28 NZ NZ591878A patent/NZ591878A/en not_active IP Right Cessation
- 2009-09-28 EP EP20090817719 patent/EP2332943B1/en active Active
- 2009-09-28 JP JP2010531835A patent/JP5666304B2/ja not_active Expired - Fee Related
- 2009-09-28 CA CA2738150A patent/CA2738150A1/en not_active Abandoned
- 2009-09-28 PE PE2011000781A patent/PE20110307A1/es not_active Application Discontinuation
- 2009-09-28 US US13/121,062 patent/US20110207723A1/en not_active Abandoned
- 2009-09-28 AU AU2009300836A patent/AU2009300836B2/en not_active Ceased
- 2009-09-28 TW TW098132702A patent/TW201016708A/zh unknown
- 2009-09-28 MX MX2011003189A patent/MX2011003189A/es active IP Right Grant
- 2009-09-28 US US12/568,151 patent/US8198269B2/en not_active Expired - Fee Related
- 2009-09-28 WO PCT/JP2009/066728 patent/WO2010038686A1/ja not_active Ceased
- 2009-09-28 CN CN2009801383817A patent/CN102171221B/zh not_active Expired - Fee Related
- 2009-09-28 KR KR1020117009408A patent/KR20110076965A/ko not_active Withdrawn
- 2009-09-28 AR ARP090103718A patent/AR073406A1/es not_active Application Discontinuation
-
2011
- 2011-03-23 ZA ZA2011/02172A patent/ZA201102172B/en unknown
- 2011-03-24 IL IL211933A patent/IL211933A/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| CN102171221A (zh) | 2011-08-31 |
| IL211933A0 (en) | 2011-06-30 |
| US20100093999A1 (en) | 2010-04-15 |
| EP2332943A4 (en) | 2012-03-14 |
| NZ591878A (en) | 2012-06-29 |
| IL211933A (en) | 2015-03-31 |
| JPWO2010038686A1 (ja) | 2012-03-01 |
| ZA201102172B (en) | 2012-10-31 |
| AR073406A1 (es) | 2010-11-03 |
| AU2009300836A1 (en) | 2010-04-08 |
| US8198269B2 (en) | 2012-06-12 |
| US20110207723A1 (en) | 2011-08-25 |
| ES2539859T3 (es) | 2015-07-06 |
| JP5666304B2 (ja) | 2015-02-12 |
| KR20110076965A (ko) | 2011-07-06 |
| AU2009300836B2 (en) | 2014-02-27 |
| WO2010038686A1 (ja) | 2010-04-08 |
| EP2332943A1 (en) | 2011-06-15 |
| CA2738150A1 (en) | 2010-04-08 |
| MX2011003189A (es) | 2011-04-27 |
| EP2332943B1 (en) | 2015-04-22 |
| TW201016708A (en) | 2010-05-01 |
| CN102171221B (zh) | 2013-11-06 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20110307A1 (es) | Derivados de aminodihidrotiazina fusionada con actividad sobre la proteina beta-amiloide | |
| PE20091438A1 (es) | Derivados fusionados de aminodihidrotiazina | |
| PE20090276A1 (es) | Compuestos derivados de imidazoquinolina como moduladores de tlr7 | |
| PE20171341A1 (es) | Compuestos de pirazina para el tratamiento de enfermedades infecciosas | |
| PE20140623A1 (es) | Halogenoalquil-1,3-oxazinas como inhibidores de la bace1 y/o bace2 | |
| PE20140690A1 (es) | Benzoxazepinonas fusionadas como moduladoras de canales ionicos | |
| PE20070602A1 (es) | Compuestos de carboxiamina como moduladores de histona desacetilasa | |
| PE20141205A1 (es) | Spiro-[1,3]-oxacinas y spiro-[1,4]-oxacepinas como inhibidores de bace1 y/o bace2 | |
| PE20141004A1 (es) | 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2 | |
| PE20070002A1 (es) | Compuestos derivados de heteroaril como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa tipo i | |
| PE20091095A1 (es) | Moduladores de gamma secretasa | |
| PE20120505A1 (es) | Derivados de 1-heterociclil-1,5-dihidro-pirazolo[3,4-d]pirimidin-4-ona como moduladores de pde9a | |
| PE20090188A1 (es) | Compuestos heterociclicos como moduladores de la senda de hedgehog | |
| PE20081753A1 (es) | Compuestos y composiciones como inhibidores de la proteasa activadora de canal | |
| JO2962B1 (en) | Aminopronic derivatives substituted as niprilicin inhibitors | |
| PE20090649A1 (es) | DERIVADOS DE PIRAZOL COMO INHIBIDORES DE LA ENZIMA 11ßHSD1 | |
| AR077935A1 (es) | Derivados de 3-amino-5 fenil-5,6-dihidro-2h-(1,4)oxazina | |
| PE20141005A1 (es) | 1,3-oxazinas como inhibidores de bace1 y/o bace2 | |
| PE20142376A1 (es) | Fluormetil-5,6-dihidro-4h-[1,3]oxazinas | |
| DK2123271T3 (da) | Lægemiddel til behandling af influenza | |
| PE20150021A1 (es) | 5-amino[1,4]tiazinas como inhibidores de bace1 | |
| PE20091811A1 (es) | DERIVADOS DE IMIDAZOLIDINONA COMO INHIBIDORES DE 11b-HSD1 | |
| EA201290632A1 (ru) | Производные бетулина | |
| PE20121522A1 (es) | Derivados de acido 5-alquinil-3-amida-2-tiofeno-carboxilico como inhibidores del virus flaviviridae | |
| PE20140703A1 (es) | Derivados de heteroarilo como moduladores de nachr alfa 7 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |