AR081154A1 - Compuestos de amino-oxazinas y amino-dihidrotiazina como moduladores de beta-secretasa y metodos de uso - Google Patents
Compuestos de amino-oxazinas y amino-dihidrotiazina como moduladores de beta-secretasa y metodos de usoInfo
- Publication number
- AR081154A1 AR081154A1 ARP110100821A AR081154A1 AR 081154 A1 AR081154 A1 AR 081154A1 AR P110100821 A ARP110100821 A AR P110100821A AR 081154 A1 AR081154 A1 AR 081154A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- independently
- alkynyl
- oxo
- alkenyl
- Prior art date
Links
Classifications
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- 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
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- 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
- 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
-
- 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
- C07D498/12—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 three hetero rings
- C07D498/20—Spiro-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
- C07D513/12—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
- C07D513/20—Spiro-condensed systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente comprende una clase de compuestos para la modulación de actividad de enzima beta-secretasa y para el tratamiento de enfermedades mediadas por beta-secretasa, incluyendo enfermedad de Alzheimer (AD) y afecciones relacionadas. También incluye el uso de estos compuestos en las composiciones farmacéuticas para tratamiento, profiláctico o terapéutico, de trastornos y afecciones relacionadas con la actividad de proteína beta-secretasa. Tales trastornos incluyen, por ejemplo, enfermedad de Alzheimer, déficits cognitivos, deterioro cognitivo, esquizofrenia y otras afecciones del sistema nervioso central relacionadas a y/o causadas por la formación y/o deposición de placa en el cerebro. También comprende además modalidades de la fórmula (1), intermediarios y procesos útiles para la preparación de compuestos de la fórmula (1). Reivindicación 1: Un compuesto de la fórmula (1), o un estereoisómero, tautómero, hidrato, solvato o sal farmacéuticamente aceptable del mismo, caracterizado porque: A1 es CR6 o N; A2 es CR5 o N; A3 es CR4 o N; A4 es CR3 o N; A5 es CR1 o N; A6 es CR8 o N, con la condición de que no más de uno de A1, A2, A3, A4, A5 y A6 es N; cada uno de R1, R4, R5 y R8, independientemente, es H, F, Cl, Br, CF3, OCF3, -alquilo C1-6, CN, OH, -O-alquilo C1-6-, -S(O)o-alquilo C1-6, -NH-alquilo C1-6 o -C(O)-alquilo C1-6, en donde el -alquilo C1-6 y porción -alquilo C1-6 de -O-alquilo C1-6-, -S(O)o-alquilo C1-6, -NH-alquilo C1-6 y -C(O)-alquilo C1-6 se sustituyen opcionalmente con 1 - 3 sustituyentes de F, oxo u OH; cada uno de R2 y R7, independientemente, es F, Cl, Br, l, haloalquilo, haloalcoxilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, CN, -O-alquilo C1-6, -S-alquilo C1-6, -NH-alquilo C1-6, -N(alquilo C1-3)2, -NH-fenilo, -NH-bencilo, -Si(CH3)3 o un anillo seleccionado del grupo que consiste de fenilo, piridilo, pirimidilo, pirazinilo, piridazinilo, triazinilo, tienilo, pirazolilo, imidazolilo, oxazolilo, isoxazolilo, tiazolilo, isotiazolilo, diazolilo, triazolilo, tetrazolilo, piranilo, dihidropiranilo, tetrahidropiranilo, furanilo, dihidrofuranilo, tetrahidrofuranilo, pirrolilo, dihidropirrolilo, pirrolidinilo, piperidinilo, piperazinilo, morfolinilo, azetidinilo, 8-oxo-3-aza-biciclo[3.2.1]oct-3-ilo, aza-biciclo[2.2.1]hept-5-ilo, 2-oxo-7-aza-[3,5]-espironon-7-ilo, ciclopropilo, ciclobutilo, ciclopentilo y ciclohexilo, en donde el alquilo C1-6, alquenilo C2-4, alquinilo C2-4, -O-alquilo C1-6, -S-alquilo C1-6, -NH-alquilo C1-6, -N(alquilo C1-3)2, -NH-fenilo, -NH-bencilo y un anillo están opcionalmente sustituidos, independientemente, con 1 - 3 sustituyentes de R9; cada uno de R3 y R6, independientemente, es H, halo, haloalquilo, haloalcoxilo, -alquilo C1-6, CN, OH, O-alquilo C1-6. S(O)o-alquilo C1-6, NH-alquilo C1-6 o C(O)-alquilo C1-6; cada R9, independientemente, es halo, haloalquilo, haloalcoxilo, CN, OH, NO2, NH2, acetilo, -C(O)NHCH3, oxo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, alquilamino C1-6-, dialquilamino C1-6-, alcoxilo C1-6, tioalcoxilo C1-6, morfolinilo, pirazolilo, isoxazolilo, dihidropiranilo, pirrolidinilo, piperazinilo, oxetanilo o dioxolilo, en donde cada uno del alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, alquilamino C1-6-, dialquilamino C1-6-, alcoxilo C1-6, tioalcoxilo C1-6, morfolinilo, pirazolilo, isoxazolilo, dihidropiranilo, pirrolidinilo, oxetanilo o dioxolilo, está opcionalmente sustituido independientemente con 1 - 5 sustituyentes de F, Cl, CN, NO2, NH2, OH, oxo, metilo, metoxilo, etilo, etoxilo, propilo, propoxilo, isopropilo, isopropoxilo, ciclopropilo, ciclopropilmetoxilo, butilo, butoxilo, isobutoxilo, tert-butoxilo, isobutilo, sec-butilo, tert-butilo, alquilamino C1-3-, dialquilamino C1-3, tioalcoxilo C1-3, u oxetanilo; X es -CR10R10-, -O- ó -S-, en donde cada R10, independientemente, es H, halo, haloalquilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6 o un anillo seleccionado del grupo que consiste de morfolinilo, piperidinilo, piperizinilo, tetrahidrofuranilo, furanilo, tienilo, fenilo, piridinilo, pirimidinilo, piridazinilo, pirazinilo, piranilo, dihidropiranilo, tetrahidropiranilo, pirrolilo, dihidropirrolilo, tetrahidropirrolilo y oxetanilo; Y es -O-, -S- o -CH2-, con la condición de que (i) cuando X es -O- ó -S-, entonces Y es -CH2-, o (ii) cuando X es -CR10R10-, entonces Y es -O- ó -S-; y Z es CH2, CHF, CF2, CH(CH3), C(CH3)2 o CH(CF3).
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US31402410P | 2010-03-15 | 2010-03-15 |
Publications (1)
Publication Number | Publication Date |
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AR081154A1 true AR081154A1 (es) | 2012-07-04 |
Family
ID=43982433
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110100821 AR081154A1 (es) | 2010-03-15 | 2011-03-15 | Compuestos de amino-oxazinas y amino-dihidrotiazina como moduladores de beta-secretasa y metodos de uso |
Country Status (11)
Country | Link |
---|---|
US (2) | US8497264B2 (es) |
EP (1) | EP2547686B1 (es) |
JP (1) | JP5584352B2 (es) |
AR (1) | AR081154A1 (es) |
AU (1) | AU2011227501B9 (es) |
CA (1) | CA2791389C (es) |
ES (1) | ES2450568T3 (es) |
MX (1) | MX2012010657A (es) |
TW (1) | TW201144323A (es) |
UY (1) | UY33276A (es) |
WO (1) | WO2011115928A1 (es) |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
WO2012071279A1 (en) | 2010-11-23 | 2012-05-31 | Amgen Inc. | Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use |
WO2012109165A1 (en) * | 2011-02-07 | 2012-08-16 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use |
EP2694489B1 (en) | 2011-04-07 | 2017-09-06 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
AU2012298983A1 (en) | 2011-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | 2-spiro-substituted iminothiazines and their mono-and dioxides as BACE inhibitors, compositions and their use |
WO2013044092A1 (en) | 2011-09-21 | 2013-03-28 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
EP2650284A1 (en) * | 2012-04-10 | 2013-10-16 | Merz Pharma GmbH & Co. KGaA | Heterocyclic derivatives as metabotropic glutamate receptor modulators |
MX2014014066A (es) * | 2012-05-30 | 2015-03-19 | Comentis Inc | Compuestos de cromano. |
US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
CN103012355B (zh) * | 2012-11-18 | 2016-02-10 | 中北大学 | 一种活性口山酮化合物及其制备方法 |
WO2015027021A1 (en) | 2013-08-22 | 2015-02-26 | Bristol-Myers Squibb Company | Imide and acylurea derivatives as modulators of the glucocorticoid receptor |
US9796720B2 (en) | 2013-08-22 | 2017-10-24 | Bristol-Myers Squibb Company | Imidazole-derived modulators of the glucocorticoid receptor |
Family Cites Families (89)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US355019A (en) | 1886-12-28 | Geoege joedaist | ||
US2683718A (en) | 1952-01-11 | 1954-07-13 | Searle & Co | Spiro-[xanthene-9, 4'-imidazolidine]-2, 5-dione |
US3185696A (en) | 1959-03-12 | 1965-05-25 | Jack M Tien | 3', 6'-diaminofluoran derivatives of gamma-lactam |
FR2576178B1 (fr) | 1985-01-24 | 1987-04-17 | Furodet Philippe | Procede de fabrication pour un enfumoir a chargement par-dessous |
DE3601492A1 (de) | 1986-01-20 | 1987-07-23 | Vacuumschmelze Gmbh | Verfahren zur herstellung eines stabilisierten filament-supraleiters mit hohem anteil an stabilisierungsmaterial |
US5441870A (en) | 1992-04-15 | 1995-08-15 | Athena Neurosciences, Inc. | Methods for monitoring cellular processing of β-amyloid precursor protein |
SI9300303A (en) | 1993-06-08 | 1994-12-31 | Krka Tovarna Zdravil | Process for isolation of hypolipemic effective substance |
US5629322A (en) | 1994-11-15 | 1997-05-13 | Merck & Co., Inc. | Cyclic amidine analogs as inhibitors of nitric oxide synthase |
EP0871720A2 (en) | 1995-06-07 | 1998-10-21 | Athena Neurosciences, Inc. | Beta-secretase, antibodies to beta-secretase, and assays for detecting beta-secretase inhibition |
KR100768381B1 (ko) | 1998-09-24 | 2007-10-18 | 파마시아 앤드 업존 캄파니 엘엘씨 | 알츠하이머병 세크레타제 |
MY138097A (en) | 2000-03-22 | 2009-04-30 | Du Pont | Insecticidal anthranilamides |
DE60112942T2 (de) | 2000-06-30 | 2006-06-22 | Elan Pharmaceuticals, Inc., South San Francisco | Verbindungen zur behandlung der alzheimerischen krankheit |
US7196163B2 (en) | 2001-05-22 | 2007-03-27 | Merk & Co., Inc. | Assays using amyloid precursor proteins with modified β-secretase cleavage sites to monitor β-secretase activity |
MXPA04000140A (es) | 2001-06-27 | 2004-06-03 | Elan Pharm Inc | Derivados de beta-hidroxiamina utiles en el tratamiento de enfermedad de alzheimer. |
KR100713137B1 (ko) | 2001-06-28 | 2007-05-02 | 동화약품공업주식회사 | 신규의 2,4-디플루오로벤즈아미드 유도체 |
EP1404328A1 (en) | 2001-07-10 | 2004-04-07 | Elan Pharmaceuticals, Inc. | Alpha-hydroxyamide statine derivatives for the treatment of alzheimer's disease |
CA2453444A1 (en) | 2001-07-10 | 2003-01-23 | Elan Pharmaceuticals, Inc. | Diaminediols for the treatment of alzheimer's disease |
US20030109559A1 (en) | 2001-07-11 | 2003-06-12 | Andrea Gailunas | N-(3-amino-2-hydroxy-propyl)substituted alkylamide compounds |
CA2462851A1 (en) | 2001-10-04 | 2003-04-10 | Elan Pharmaceuticals, Inc. | Hydroxypropylamines |
BR0213138A (pt) | 2001-10-05 | 2004-08-24 | Elan Pharm Inc | Métodos de tratar ou prevenir mal de alzheimer e uma doença distinguida por depósito de beta-amilóide no cérebro, de tratar um paciente que tenha, ou de prevenir um paciente de contrair uma doença ou condição, de produzir um complexo de beta-secretase e de inibir a produção de placa beta-amilóide em um animal, composição e uso de um composto |
WO2003037325A1 (en) | 2001-10-29 | 2003-05-08 | Elan Pharmaceuticals, Inc. | Hydroxy substituted amides for the treatment of alzheimer's disease |
MXPA04004428A (es) | 2001-11-08 | 2004-09-10 | Elan Pharm Inc | Derivados de 2,3-diamino-2-hidroxipropano n,n`-sustituidos. |
TW200304374A (en) | 2001-11-30 | 2003-10-01 | Smithkline Beecham Plc | Novel compounds |
CA2469622A1 (en) | 2001-12-06 | 2003-06-19 | Elan Pharmaceuticals, Inc. | Substituted hydroxyethylamines |
BR0306724A (pt) | 2002-01-04 | 2006-04-11 | Elan Pharm Inc | carboxamidas amino substituìdas para tratamento de doença de alzheimer |
MXPA04006882A (es) | 2002-01-17 | 2004-12-06 | Neurogen Corp | Analogos substituidos de quinazolin-4-ilamina como moduladores de receptores de capsaicina. |
US6806283B2 (en) * | 2002-05-06 | 2004-10-19 | Virginia Commonwealth University | Selective serotonin receptor antagonists and therapeutic applications thereof |
US7115652B2 (en) | 2002-06-17 | 2006-10-03 | Sunesis Pharmaceuticals, Inc. | Aspartyl protease inhibitors |
JP2005529953A (ja) | 2002-06-17 | 2005-10-06 | サネシス ファーマシューティカルズ, インコーポレイテッド | アスパルチルプロテアーゼインヒビター |
CA2489988A1 (en) | 2002-06-20 | 2003-12-31 | Michael R. Reeder | Process for preparing 5-(1,3-oxazol-2-yl) benzoic acid derivatives |
UY27967A1 (es) | 2002-09-10 | 2004-05-31 | Pfizer | Acetil 2-hindroxi-1,3-diaminoalcanos |
CA2505098A1 (en) | 2002-11-12 | 2004-05-27 | Merck & Co., Inc. | Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease |
GB0228410D0 (en) | 2002-12-05 | 2003-01-08 | Glaxo Group Ltd | Novel Compounds |
CA2512111A1 (en) | 2003-01-07 | 2004-07-29 | Merck And Co., Inc. | Macrocyclic beta-secretase inhibitors for treatment of alzheimer's disease |
GB0305918D0 (en) | 2003-03-14 | 2003-04-23 | Glaxo Group Ltd | Novel compounds |
MXPA05009850A (es) | 2003-03-14 | 2005-12-06 | Merck Sharp & Dohme | Metodo para tratar el deterioro cognitivo leve y para prevenir o atrasar la enfermedad de alzheimer. |
AR044044A1 (es) | 2003-04-21 | 2005-08-24 | Elan Pharm Inc | 2-hidroxi-3-diaminoalcanos de benzamida |
CL2004000848A1 (es) | 2003-04-21 | 2005-01-28 | Elan Pharmaceuticals Inc Pharm | Compuestos derivados de fenacil-2-hidroxi-3-diaminoalcanos, inhibidores de la enzima betasecretasa, utiles para preparar un medicamento para tratar alzheimer, sindrome de down, hemorragia cerebral hereditaria con amiloidosis de tipo holandes, y otras |
CN100430377C (zh) | 2003-06-30 | 2008-11-05 | 麦克公司 | 用于治疗阿尔茨海默病的N-烷基苯基甲酰胺β分泌酶抑制剂 |
WO2005004803A2 (en) | 2003-07-01 | 2005-01-20 | Merck & Co., Inc. | Phenylcarboxylate 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 |
US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
GB0402143D0 (en) | 2004-01-30 | 2004-03-03 | Smithkline Beecham Corp | Novel compounds |
WO2005097767A1 (en) | 2004-03-30 | 2005-10-20 | Merck & Co., Inc. | 2-aminothiazole compounds useful as aspartyl protease inhibitors |
AU2005264915A1 (en) | 2004-06-16 | 2006-01-26 | Wyeth | Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase |
US20090221579A1 (en) | 2004-10-15 | 2009-09-03 | Jeffrey Scott Albert | Substituted Amino-Compounds and Uses Thereof |
EP2264036A1 (en) | 2005-01-14 | 2010-12-22 | Wyeth LLC (Formerly Known As Wyeth) | Amino-imidazolones for the inhibition of beta-secretase |
AU2006211159A1 (en) | 2005-02-01 | 2006-08-10 | Wyeth | Amino-pyridines as inhibitors of beta-secretase |
US7759337B2 (en) | 2005-03-03 | 2010-07-20 | Amgen Inc. | Phthalazine compounds and methods of use |
US8594320B2 (en) | 2005-04-19 | 2013-11-26 | (Epfl) Ecole Polytechnique Federale De Lausanne | Hybrid echo and noise suppression method and device in a multi-channel audio signal |
WO2006138265A2 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Heterocyclic aspartyl protease inhibitors, preparation and use thereof |
JP2008543846A (ja) | 2005-06-14 | 2008-12-04 | シェーリング コーポレイション | プロテアーゼ阻害剤として化合物の調製およびその使用 |
WO2006138528A2 (en) | 2005-06-16 | 2006-12-28 | Janssen Pharmaceutica N.V | Tricyclic opioid modulators |
WO2007005404A1 (en) * | 2005-06-30 | 2007-01-11 | Wyeth | AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION |
TW200738683A (en) | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
ATE550338T1 (de) | 2005-07-18 | 2012-04-15 | Merck Sharp & Dohme | Spiropiperidininhibitoren von beta-secretase zur behandlung von alzheimer-krankheit |
TW200730523A (en) | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
KR20080050430A (ko) | 2005-09-26 | 2008-06-05 | 와이어쓰 | 베타-세크레타제 (bace) 억제제로서아미노-5-[4-(디플루오로메톡시)페닐]-5-페닐이미다졸론화합물 |
BRPI0617852A2 (pt) | 2005-10-25 | 2011-08-09 | Shionogi & Co | compostos derivados de aminodi-hidrotiazina assim como composições contendo os mesmos |
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 |
WO2007114771A1 (en) | 2006-04-05 | 2007-10-11 | Astrazeneca Ab | 2-AMINOPYRIMIDIN-4-ONES AND THEIR USE FOR TREATING OR PREVENTING Aβ-RELATED PATHOLOGIES |
TW200808751A (en) | 2006-04-13 | 2008-02-16 | Astrazeneca Ab | New compounds |
AR061264A1 (es) | 2006-06-12 | 2008-08-13 | Schering Corp | Inhibidores de aspartil-proteasas derivados de pirimidina, composiciones farmaceuticas que los contienen y usos para tratar enfermedades cognitivas o neurodegenerativas, y como inhibidores del virus vih. |
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 |
IL177552A (en) | 2006-08-17 | 2014-08-31 | Ron Keren | Irrigation Pipe |
AU2007314338A1 (en) | 2006-10-30 | 2008-05-08 | Merck & Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's Disease |
TW200831091A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
TW200831484A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
RU2473545C2 (ru) | 2007-02-02 | 2013-01-27 | Ф.Хоффманн-Ля Рош Аг | Новые 2-аминооксазолины в качестве лигандов taar1 для заболеваний цнс |
US20080207900A1 (en) | 2007-02-28 | 2008-08-28 | Teiji Kimura | Two cyclic oxomorphorin derivatives |
AR065814A1 (es) | 2007-03-23 | 2009-07-01 | Wyeth Corp | Derivados de 5-fenilimidazolona,inhibidores de beta-secretasa,composiciones farmaceuticas que los contienen y usos para prevenir y/o tratar trastornos asociados a niveles beta-amiloides elevados. |
AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
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 |
TW200902503A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
US20100317850A1 (en) | 2008-01-18 | 2010-12-16 | Yuichi Suzuki | Condensed aminodihydrothiazine derivative |
BRPI0907563A2 (pt) | 2008-02-18 | 2015-08-04 | Hoffmann La Roche | Derivados de 4,5-di-hidro-xazol-2-il amina |
WO2009131975A1 (en) | 2008-04-22 | 2009-10-29 | Schering Corporation | Phenyl-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 |
WO2009151098A1 (ja) | 2008-06-13 | 2009-12-17 | 塩野義製薬株式会社 | βセクレターゼ阻害作用を有する含硫黄複素環誘導体 |
WO2010010014A1 (en) | 2008-07-24 | 2010-01-28 | 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 |
US8450308B2 (en) * | 2008-08-19 | 2013-05-28 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
PE20110805A1 (es) * | 2008-09-11 | 2011-11-09 | Amgen Inc | Compuestos con anillos espiro-triciclicos como moduladores de beta-secretasas y metodos de uso |
AR077328A1 (es) | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
US8188079B2 (en) | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
WO2011115938A1 (en) * | 2010-03-15 | 2011-09-22 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta - secretase modulators |
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2011
- 2011-03-14 US US13/047,693 patent/US8497264B2/en active Active
- 2011-03-14 WO PCT/US2011/028401 patent/WO2011115928A1/en active Application Filing
- 2011-03-14 JP JP2013500133A patent/JP5584352B2/ja not_active Expired - Fee Related
- 2011-03-14 ES ES11714873T patent/ES2450568T3/es active Active
- 2011-03-14 CA CA 2791389 patent/CA2791389C/en not_active Expired - Fee Related
- 2011-03-14 MX MX2012010657A patent/MX2012010657A/es not_active Application Discontinuation
- 2011-03-14 AU AU2011227501A patent/AU2011227501B9/en not_active Ceased
- 2011-03-14 EP EP20110714873 patent/EP2547686B1/en active Active
- 2011-03-15 UY UY33276A patent/UY33276A/es not_active Application Discontinuation
- 2011-03-15 TW TW100108813A patent/TW201144323A/zh unknown
- 2011-03-15 AR ARP110100821 patent/AR081154A1/es not_active Application Discontinuation
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2013
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US8497264B2 (en) | 2013-07-30 |
EP2547686B1 (en) | 2014-01-22 |
UY33276A (es) | 2011-09-30 |
EP2547686A1 (en) | 2013-01-23 |
TW201144323A (en) | 2011-12-16 |
CA2791389A1 (en) | 2011-09-22 |
AU2011227501B2 (en) | 2013-08-15 |
US20140045828A1 (en) | 2014-02-13 |
CA2791389C (en) | 2014-04-29 |
JP2013522304A (ja) | 2013-06-13 |
WO2011115928A1 (en) | 2011-09-22 |
ES2450568T3 (es) | 2014-03-25 |
AU2011227501A1 (en) | 2012-09-20 |
US9012446B2 (en) | 2015-04-21 |
MX2012010657A (es) | 2013-02-07 |
JP5584352B2 (ja) | 2014-09-03 |
US20110251186A1 (en) | 2011-10-13 |
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