PE20110805A1 - Compuestos con anillos espiro-triciclicos como moduladores de beta-secretasas y metodos de uso - Google Patents
Compuestos con anillos espiro-triciclicos como moduladores de beta-secretasas y metodos de usoInfo
- Publication number
- PE20110805A1 PE20110805A1 PE2011000606A PE2011000606A PE20110805A1 PE 20110805 A1 PE20110805 A1 PE 20110805A1 PE 2011000606 A PE2011000606 A PE 2011000606A PE 2011000606 A PE2011000606 A PE 2011000606A PE 20110805 A1 PE20110805 A1 PE 20110805A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds
- spiro
- beta
- secretases
- modulators
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 108091007737 beta-secretases Proteins 0.000 title 1
- -1 2- (2,2-DIMETHYLPROPOXY) -7 '- (5-PYRIMIDINYL) SPIRO [1,3-OXAZOL-4,9'-XANTHEN] -2-AMINE Chemical compound 0.000 abstract 3
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 abstract 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 abstract 1
- 231100000876 cognitive deterioration Toxicity 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
-
- 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
- C07D498/10—Spiro-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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- 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
- C07D513/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychology (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)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
REFERIDA A UN COMPUESTO DE FORMULA I, DONDE A1 ES CR6, N; A2 ES CR5, N; A3 ES CR4, N; A5 ES CR1, N; A6 ES CR8, N; T1 ES CR2, N; T2 ES CR7, N; R1, R4, R5 Y R8 SON CADA UNO H, F, Cl, Br, CF3, OCF3, ALQUILO C1-C6, ENTRE OTROS; R2 Y R7 SON CADA UNO H, HALO, HALOALQUILO HALOALCOXILO,ALQUINILO C1-C6, ENTRE OTROS; R3 Y R6 SON CADA UNO HALO, HALOALQUILO, CN, OH, O(ALQUILO C1-C6), CO-(ALQUILO C1-C6), ENTRE OTROS; W ES R1R1; X ES O, S; Y ESTA AUSENTE O ES CR1R1, C(=O), O, NR1, ENTRE OTROS; Z ESTA AUSENTE O ES CR1R1, C(=O), O, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-(2,2-DIMETILPROPOXI)-7'-(5-PIRIMIDINIL)ESPIRO[1,3-OXAZOL-4,9'-XANTEN]-2-AMINA; (4R)-2'-PROPOXI-7'-(5-PIRIMIDINIL)ESPIRO[1,3-OXAZOL-4,9-XANTEN]-2-AMINA; (4R)-2'-(3,3-DIMETIL-1-BUTIN-1-IL)-7'-(5-PIRIMIDINIL)ESPIRO[1,3-OXAZOL-4,9'-XANTEN]-2-AMINA; ENTRE OTROS. REFERIDA ADEMAS A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE BETA SECRETASA SIENDO UTILES EN EL TRATAMIENTO DE ALZHEIMER, DETERIORO COGNITIVO
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9608208P | 2008-09-11 | 2008-09-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20110805A1 true PE20110805A1 (es) | 2011-11-09 |
Family
ID=41319591
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011000606A PE20110805A1 (es) | 2008-09-11 | 2009-09-11 | Compuestos con anillos espiro-triciclicos como moduladores de beta-secretasas y metodos de uso |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8426447B2 (es) |
| EP (1) | EP2328903B1 (es) |
| JP (1) | JP5579720B2 (es) |
| KR (1) | KR20110073511A (es) |
| CN (1) | CN102209721A (es) |
| AU (1) | AU2009291602B2 (es) |
| BR (1) | BRPI0918449A2 (es) |
| CA (1) | CA2736130C (es) |
| CL (1) | CL2011000516A1 (es) |
| CO (1) | CO6362014A2 (es) |
| CR (1) | CR20110134A (es) |
| EA (1) | EA201100461A1 (es) |
| ES (1) | ES2459195T3 (es) |
| IL (1) | IL211440A0 (es) |
| MA (1) | MA32705B1 (es) |
| MX (1) | MX2011002705A (es) |
| MY (1) | MY148558A (es) |
| PE (1) | PE20110805A1 (es) |
| TW (1) | TWI385175B (es) |
| WO (1) | WO2010030954A1 (es) |
| ZA (1) | ZA201102674B (es) |
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| US8889703B2 (en) | 2010-02-24 | 2014-11-18 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
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| WO2011130741A1 (en) * | 2010-04-16 | 2011-10-20 | Array Biopharma Inc. | Compounds for treating neurodegenerative diseases |
| US8921363B2 (en) | 2010-08-05 | 2014-12-30 | Amgen Inc. | Derivatives of 1 H-isoindol-3-amine, 1 H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as beta-secretase inhibitors |
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| US9346827B2 (en) | 2011-02-07 | 2016-05-24 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use |
| US8962859B2 (en) * | 2011-02-15 | 2015-02-24 | Amgen Inc. | Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use |
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| KR20140041590A (ko) | 2011-06-07 | 2014-04-04 | 에프. 호프만-라 로슈 아게 | [1,3]옥사진 |
| BR112014004181A2 (pt) | 2011-08-22 | 2017-06-13 | Merck Sharp & Dohme | composto, composição farmacêutica, e, método de tratamento, prevenção, e / ou retardo do início de uma doença ou patologia |
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| ES2566373T3 (es) * | 2011-10-10 | 2016-04-12 | Astrazeneca Ab | Inhibidores monofluoro beta-secretasa |
| TWI557112B (zh) | 2012-03-05 | 2016-11-11 | 百靈佳殷格翰國際股份有限公司 | β-分泌酶抑制劑 |
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| JP2015518048A (ja) | 2012-05-30 | 2015-06-25 | コメンティス, インコーポレイテッド | クロマン化合物 |
| US9000183B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cyclohexane-1,2′-indene-1′,2″-imidazol compounds and their use as BACE inhibitors |
| US9000184B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cyclohexane-1,2′-naphthalene-1′,2″-imidazol compounds and their use as BACE inhibitors |
| US9000182B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | 2H-imidazol-4-amine compounds and their use as BACE inhibitors |
| US9000185B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cycloalkyl ether compounds and their use as BACE inhibitors |
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| AU2006307314C1 (en) | 2005-10-25 | 2011-08-25 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| WO2007100536A1 (en) | 2006-02-24 | 2007-09-07 | Wyeth | DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE |
| JP2009532464A (ja) | 2006-04-05 | 2009-09-10 | アストラゼネカ・アクチエボラーグ | 2−アミノピリミジン−4−オン及びAβ−関連の病理を治療又は予防するためのその使用 |
| TW200808751A (en) | 2006-04-13 | 2008-02-16 | Astrazeneca Ab | New compounds |
| CA2653650A1 (en) | 2006-06-12 | 2007-12-21 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| TW200815447A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds IV |
| TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
| EP2091328B1 (en) | 2006-10-30 | 2011-12-28 | Merck Sharp & Dohme Corp. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
| TW200831484A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| TW200831091A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| EP2114906B1 (en) | 2007-02-02 | 2014-08-06 | F. Hoffmann-La Roche AG | 2-aminooxazolines as taar1 ligands for cns disorders |
| PE20090617A1 (es) | 2007-03-23 | 2009-05-08 | Wyeth Corp | Compuestos amino-5-[-4-(difluorometoxi)fenil]-5-fenilimidazolona para la inhibicion de -secretasa |
| WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
| EP2147914B1 (en) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivatives substituted with cyclic groups |
| UY31083A1 (es) | 2007-05-15 | 2009-01-05 | Astrazeneca Ab | Derivados de sulfoximinas para la inhibicion de b-secretasa |
| MY160690A (en) | 2008-01-18 | 2017-03-15 | Eisai R&D Man Co Ltd | Condensed aminodihydrothiazine derivative |
| CA2712228C (en) | 2008-02-18 | 2013-04-16 | F. Hoffmann-La Roche Ag | 4,5-dihydro-oxazol-2-yl amine derivatives |
| MX2010011563A (es) | 2008-04-22 | 2010-11-12 | Schering Corp | Compuestos 2-imino-3-metil pirrolo pirimidinona fenil-sustituidos como inhibidores de enzima de escision de proteina precursora amiloide sitio beta-1, composiciones y su uso. |
| TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
| EP2321287B1 (en) | 2008-07-24 | 2015-11-11 | F. Hoffmann-La Roche AG | 4,5-dihydro-oxazol-2-yl derivatives |
| AU2009277485B2 (en) * | 2008-07-28 | 2013-05-02 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
-
2009
- 2009-09-11 CN CN2009801456428A patent/CN102209721A/zh active Pending
- 2009-09-11 CA CA2736130A patent/CA2736130C/en not_active Expired - Fee Related
- 2009-09-11 JP JP2011527012A patent/JP5579720B2/ja not_active Expired - Fee Related
- 2009-09-11 MY MYPI2011001092A patent/MY148558A/en unknown
- 2009-09-11 EP EP09737222.1A patent/EP2328903B1/en active Active
- 2009-09-11 ES ES09737222.1T patent/ES2459195T3/es active Active
- 2009-09-11 KR KR1020117008316A patent/KR20110073511A/ko not_active Withdrawn
- 2009-09-11 EA EA201100461A patent/EA201100461A1/ru unknown
- 2009-09-11 TW TW098130795A patent/TWI385175B/zh not_active IP Right Cessation
- 2009-09-11 AU AU2009291602A patent/AU2009291602B2/en not_active Ceased
- 2009-09-11 PE PE2011000606A patent/PE20110805A1/es not_active Application Discontinuation
- 2009-09-11 WO PCT/US2009/056748 patent/WO2010030954A1/en not_active Ceased
- 2009-09-11 US US12/558,426 patent/US8426447B2/en active Active
- 2009-09-11 MX MX2011002705A patent/MX2011002705A/es active IP Right Grant
- 2009-09-11 BR BRPI0918449A patent/BRPI0918449A2/pt not_active IP Right Cessation
-
2011
- 2011-02-27 IL IL211440A patent/IL211440A0/en unknown
- 2011-03-10 CL CL2011000516A patent/CL2011000516A1/es unknown
- 2011-03-14 CR CR20110134A patent/CR20110134A/es unknown
- 2011-03-25 CO CO11036742A patent/CO6362014A2/es not_active Application Discontinuation
- 2011-04-11 MA MA33762A patent/MA32705B1/fr unknown
- 2011-04-11 ZA ZA2011/02674A patent/ZA201102674B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW201022280A (en) | 2010-06-16 |
| JP2012502112A (ja) | 2012-01-26 |
| BRPI0918449A2 (pt) | 2019-09-24 |
| CL2011000516A1 (es) | 2011-08-26 |
| CA2736130C (en) | 2014-01-14 |
| IL211440A0 (en) | 2011-05-31 |
| ES2459195T3 (es) | 2014-05-08 |
| CA2736130A1 (en) | 2010-03-18 |
| EA201100461A1 (ru) | 2011-10-31 |
| CO6362014A2 (es) | 2012-01-20 |
| CN102209721A (zh) | 2011-10-05 |
| AU2009291602B2 (en) | 2013-02-14 |
| JP5579720B2 (ja) | 2014-08-27 |
| EP2328903B1 (en) | 2014-03-05 |
| US20100087429A1 (en) | 2010-04-08 |
| ZA201102674B (en) | 2011-12-28 |
| MX2011002705A (es) | 2011-09-09 |
| US8426447B2 (en) | 2013-04-23 |
| MY148558A (en) | 2013-04-30 |
| WO2010030954A1 (en) | 2010-03-18 |
| EP2328903A1 (en) | 2011-06-08 |
| MA32705B1 (fr) | 2011-10-02 |
| TWI385175B (zh) | 2013-02-11 |
| KR20110073511A (ko) | 2011-06-29 |
| AU2009291602A1 (en) | 2010-03-18 |
| CR20110134A (es) | 2011-08-04 |
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