EA201100461A1 - Спиро-трициклические соединения как модуляторы бета-секретазы и способы их использования - Google Patents
Спиро-трициклические соединения как модуляторы бета-секретазы и способы их использованияInfo
- Publication number
- EA201100461A1 EA201100461A1 EA201100461A EA201100461A EA201100461A1 EA 201100461 A1 EA201100461 A1 EA 201100461A1 EA 201100461 A EA201100461 A EA 201100461A EA 201100461 A EA201100461 A EA 201100461A EA 201100461 A1 EA201100461 A1 EA 201100461A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- beta
- compounds
- secretase
- diseases
- present
- Prior art date
Links
Classifications
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- 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
Abstract
Предметом настоящего изобретения является новый класс соединений, которые могут использоваться для модуляции ферментной активности бета-секретазы и для лечения заболеваний, в развитии которых принимает участие бета-секретаза, включая болезнь Альцгеймера и связанные с ней состояния. В одном из вариантов осуществления этого изобретения соединения имеют общую формулу Iв которой А, А, А, А, А, А, Т, Т, W, X, Y и Z определяются в этом описании изобретения. Предметом настоящего изобретения является также использование таких соединений в фармацевтических препаратах для лечения и профилактики заболеваний и состояний, связанных с активностью белка бета-секретазы. К таким заболеваниям относится, например, болезнь Альцгеймера, недостаточность когнитивной функции, когнитивные нарушения, шизофрения и другие заболевания центральной нервной системы, связанные и/или вызываемые образованием и/или отложением бляшек в головном мозге. Предметом настоящего изобретения являются также другие варианты воплощения соединений формулы I, промежуточных соединений и процессов, которые могут применяться для получения соединений формулы I.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US9608208P | 2008-09-11 | 2008-09-11 | |
PCT/US2009/056748 WO2010030954A1 (en) | 2008-09-11 | 2009-09-11 | Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use |
Publications (1)
Publication Number | Publication Date |
---|---|
EA201100461A1 true EA201100461A1 (ru) | 2011-10-31 |
Family
ID=41319591
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201100461A EA201100461A1 (ru) | 2008-09-11 | 2009-09-11 | Спиро-трициклические соединения как модуляторы бета-секретазы и способы их использования |
Country Status (21)
Country | Link |
---|---|
US (1) | US8426447B2 (ru) |
EP (1) | EP2328903B1 (ru) |
JP (1) | JP5579720B2 (ru) |
KR (1) | KR20110073511A (ru) |
CN (1) | CN102209721A (ru) |
AU (1) | AU2009291602B2 (ru) |
BR (1) | BRPI0918449A2 (ru) |
CA (1) | CA2736130C (ru) |
CL (1) | CL2011000516A1 (ru) |
CO (1) | CO6362014A2 (ru) |
CR (1) | CR20110134A (ru) |
EA (1) | EA201100461A1 (ru) |
ES (1) | ES2459195T3 (ru) |
IL (1) | IL211440A0 (ru) |
MA (1) | MA32705B1 (ru) |
MX (1) | MX2011002705A (ru) |
MY (1) | MY148558A (ru) |
PE (1) | PE20110805A1 (ru) |
TW (1) | TWI385175B (ru) |
WO (1) | WO2010030954A1 (ru) |
ZA (1) | ZA201102674B (ru) |
Families Citing this family (35)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
AR075854A1 (es) | 2009-03-13 | 2011-05-04 | Vitae Pharmaceuticals Inc | Inhibidores de beta- secretasa |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
CN102812005B (zh) | 2010-02-24 | 2014-12-10 | 生命医药公司 | β-分泌酶抑制剂 |
JP5584352B2 (ja) * | 2010-03-15 | 2014-09-03 | アムジエン・インコーポレーテツド | β−セクレターゼ調節剤としてのアミノ−ジヒドロオキサジン系およびアミノ−ジヒドロチアジン系スピロ化合物ならびにそれらの医学的用途 |
US8883782B2 (en) * | 2010-03-15 | 2014-11-11 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use |
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 |
CA2808590A1 (en) | 2010-08-23 | 2012-03-01 | Amgen Inc. | Sulfonylpiperazine derivatives that interact with glucokinase regulatory protein for the treatment of diabetes |
TW201307357A (zh) * | 2010-11-22 | 2013-02-16 | Array Biopharma Inc | 治療神經退化性疾病之化合物 |
KR20140032948A (ko) | 2010-11-22 | 2014-03-17 | 이데미쓰 고산 가부시키가이샤 | 산소 함유 축합환 유도체 및 그것을 포함하여 이루어지는 유기 전계 발광 소자 |
EP2643325A1 (en) | 2010-11-23 | 2013-10-02 | Amgen Inc. | Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use |
US8415483B2 (en) | 2010-12-22 | 2013-04-09 | Astrazeneca Ab | Compounds and their use as BACE inhibitors |
EP2673279A1 (en) | 2011-02-07 | 2013-12-18 | 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 |
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 |
EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
RU2599256C2 (ru) | 2011-06-07 | 2016-10-10 | Ф. Хоффманн-Ля Рош Аг | [1,3]оксазины |
US9181236B2 (en) | 2011-08-22 | 2015-11-10 | 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 |
US9650336B2 (en) | 2011-10-10 | 2017-05-16 | Astrazeneca Ab | Mono-fluoro beta-secretase inhibitors |
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 |
EP2650284A1 (en) * | 2012-04-10 | 2013-10-16 | Merz Pharma GmbH & Co. KGaA | Heterocyclic derivatives as metabotropic glutamate receptor modulators |
EA026380B1 (ru) * | 2012-05-30 | 2017-04-28 | Коментис, Инк. | Соединения хроманов |
US9000185B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cycloalkyl ether 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 |
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 |
US10548882B2 (en) | 2012-06-21 | 2020-02-04 | Astrazeneca Ab | Camsylate salt |
TW201422592A (zh) | 2012-08-27 | 2014-06-16 | Boehringer Ingelheim Int | β-分泌酶抑制劑 |
EP2900650A1 (en) | 2012-09-28 | 2015-08-05 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
MX2020003488A (es) | 2015-02-02 | 2022-05-24 | Forma Therapeutics Inc | Acidos 3-alquil-4-amido-biciclico [4,5,0] hidroxamicos como inhibidores de histona desacetilasas (hdac). |
AR103598A1 (es) | 2015-02-02 | 2017-05-24 | Forma Therapeutics Inc | Ácidos bicíclicos[4,6,0]hidroxámicos como inhibidores de hdac |
EP3472131B1 (en) | 2016-06-17 | 2020-02-19 | Forma Therapeutics, Inc. | 2-spiro-5- and 6-hydroxamic acid indanes as hdac inhibitors |
Family Cites Families (76)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
JPH11507538A (ja) | 1995-06-07 | 1999-07-06 | アテナ ニューロサイエンシズ インコーポレイティド | β−セクレターゼ、β−セクレターゼに対する抗体、及びβ−セクレターゼ阻害を検出するためのアッセイ |
SG113454A1 (en) | 1998-09-24 | 2005-08-29 | Upjohn Co | Alzheimer's disease secretase |
MY138097A (en) | 2000-03-22 | 2009-04-30 | Du Pont | Insecticidal anthranilamides |
CN1217920C (zh) | 2000-06-30 | 2005-09-07 | 艾兰制药公司 | 治疗早老性痴呆的化合物 |
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 |
WO2003006021A1 (en) | 2001-07-10 | 2003-01-23 | Elan Pharmaceuticals, Inc. | Alpha-hydroxyamide statine derivatives for the treatment of alzh eimer's disease |
WO2003006013A1 (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 |
WO2003029169A2 (en) | 2001-10-04 | 2003-04-10 | Elan Pharmaceuticals, Inc. | Hydroxypropylamines |
WO2003030886A2 (en) | 2001-10-05 | 2003-04-17 | Elan Pharmaceuticals, Inc | Allylamides useful in the treatment of alzheimer's disease |
MXPA04004079A (es) | 2001-10-29 | 2005-07-05 | Pharmacia & Upjohn Co Llc | Amidas hidroxi sustituidas para tratamiento de enfermedad de alzheimer. |
AP2004003049A0 (en) | 2001-11-08 | 2004-06-30 | Elan Pharm Inc | N,N' -substituted-1,3-diamino -2-hydroxypropane derivatives. |
TW200304374A (en) | 2001-11-30 | 2003-10-01 | Smithkline Beecham Plc | Novel compounds |
BR0214736A (pt) | 2001-12-06 | 2004-11-23 | Elan Pharm Inc | Composto e seus sais farmaceuticamente aceitáveis, composição farmacêutica e método de tratar seres humanos ou animais que sofrem de doenças ou condições |
JP2005534614A (ja) | 2002-01-04 | 2005-11-17 | イーラン ファーマスーティカルズ、インコーポレイテッド | アルツハイマー病治療のための置換アミノカルボキサミド |
TW200406390A (en) | 2002-01-17 | 2004-05-01 | Neurogen Corp | Substituted quinazolin-4-ylamine analogues |
US7115652B2 (en) | 2002-06-17 | 2006-10-03 | Sunesis Pharmaceuticals, Inc. | Aspartyl protease inhibitors |
AU2003276047A1 (en) | 2002-06-17 | 2003-12-31 | Sunesis Pharmaceuticals, Inc. | Aspartyl protease inhibitors |
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 |
DE60329316D1 (de) | 2002-11-12 | 2009-10-29 | Merck & Co Inc | Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer |
GB0228410D0 (en) | 2002-12-05 | 2003-01-08 | Glaxo Group Ltd | Novel Compounds |
AU2004204692B2 (en) | 2003-01-07 | 2009-07-09 | Merck & 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 |
WO2004080459A1 (en) | 2003-03-14 | 2004-09-23 | Merck Sharp & Dohme Limited | Method for treating mild cognitive impairment and for preventing or delaying alzheimer’s disease |
CL2004000849A1 (es) | 2003-04-21 | 2005-01-28 | Elan Pharmaceuticals Inc Pharm | Compuestos derivados de benzamidas-2-hidroxi-3-diaminoalcanos, utiles para el tratamiento o la prevencion de alzheimer, sindrome de down, hemorragia cerebral hereditaria, demencias degenerativas y otras. |
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 |
EP1699455B1 (en) | 2003-12-15 | 2013-05-08 | Merck Sharp & Dohme Corp. | 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 |
US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
GB0402143D0 (en) | 2004-01-30 | 2004-03-03 | Smithkline Beecham Corp | Novel compounds |
EP1732906A4 (en) | 2004-03-30 | 2007-11-21 | Merck & Co Inc | 2-AMINOTHIAZOLE COMPOUNDS USEFUL AS ASPARTYLE-PROTEASE INHIBITORS |
EP1756087B1 (en) | 2004-06-16 | 2009-10-07 | Wyeth | Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase |
WO2006041404A1 (en) | 2004-10-15 | 2006-04-20 | Astrazeneca Ab | Substituted amino-compounds and uses thereof |
WO2006076284A2 (en) | 2005-01-14 | 2006-07-20 | Wyeth | AMINO-IMIDAZOLONES FOR THE INHIBITION OF ß-SECRETASE |
US7759337B2 (en) | 2005-03-03 | 2010-07-20 | Amgen Inc. | Phthalazine compounds and methods of use |
AR054618A1 (es) | 2005-06-14 | 2007-07-04 | Schering Corp | Compuestos de azetidina y su uso como inhibidores de proteasas |
ES2436795T3 (es) | 2005-06-14 | 2014-01-07 | Merck Sharp & Dohme Corp. | Inhibidores heterocíclicos de aspartil proteasa, preparación y uso de los mismos |
JP2008543866A (ja) * | 2005-06-16 | 2008-12-04 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 三環式オピオイドモジュレーター |
TW200738683A (en) | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
US20070020316A1 (en) * | 2005-07-13 | 2007-01-25 | Raviv Laor | Personal topical disinfectant device |
WO2007011810A1 (en) | 2005-07-18 | 2007-01-25 | Merck & Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
TW200730523A (en) | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
JP2009509957A (ja) | 2005-09-26 | 2009-03-12 | ワイス | β−セクレターゼ阻害剤としてのアミノ−5−[4−(ジフルオロメトキシ)フェニル]−5−フェニルイミダゾロン化合物 |
CN103936690B (zh) | 2005-10-25 | 2016-06-08 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
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 |
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 |
EP2091328B1 (en) | 2006-10-30 | 2011-12-28 | Merck Sharp & Dohme Corp. | 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 |
CA2675221C (en) | 2007-02-02 | 2016-02-23 | F. Hoffmann-La Roche Ag | Novel 2-aminooxazolines as taar1 ligands |
CL2008000791A1 (es) | 2007-03-23 | 2008-05-30 | Wyeth Corp | Compuestos derivados de 2-amino-5-(4-difluorometoxi-fenil)-5-fenil-imidazolidin-4-ona; composicion farmaceutica que comprende a dichos compuestos; y su uso en el tratamiento de una enfermedad asociada con la actividad bace excesiva, tales como enferm |
MX2009011498A (es) | 2007-04-24 | 2009-11-10 | Shionogi & Co | Derivados de aminodihidrotiazina sustituida con un grupo ciclico. |
EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
UY31083A1 (es) | 2007-05-15 | 2009-01-05 | Astrazeneca Ab | Derivados de sulfoximinas para la inhibicion de b-secretasa |
RU2476431C2 (ru) | 2008-01-18 | 2013-02-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Конденсированное производное аминодигидротиазина |
BRPI0907563A2 (pt) | 2008-02-18 | 2015-08-04 | Hoffmann La Roche | Derivados de 4,5-di-hidro-xazol-2-il amina |
JP2011518225A (ja) | 2008-04-22 | 2011-06-23 | シェーリング コーポレイション | Bace−1阻害剤としてのフェニル置換2−イミノ−3−メチルピロロピリミジノン化合物、組成物、およびそれらの使用 |
TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
KR101307007B1 (ko) | 2008-07-24 | 2013-09-11 | 에프. 호프만-라 로슈 아게 | 4,5-다이하이드로-옥사졸-2-일 유도체 |
AU2009277485B2 (en) * | 2008-07-28 | 2013-05-02 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
-
2009
- 2009-09-11 US US12/558,426 patent/US8426447B2/en active Active
- 2009-09-11 EA EA201100461A patent/EA201100461A1/ru unknown
- 2009-09-11 KR KR1020117008316A patent/KR20110073511A/ko not_active Application Discontinuation
- 2009-09-11 BR BRPI0918449A patent/BRPI0918449A2/pt not_active IP Right Cessation
- 2009-09-11 EP EP09737222.1A patent/EP2328903B1/en active Active
- 2009-09-11 MX MX2011002705A patent/MX2011002705A/es active IP Right Grant
- 2009-09-11 ES ES09737222.1T patent/ES2459195T3/es active Active
- 2009-09-11 TW TW098130795A patent/TWI385175B/zh not_active IP Right Cessation
- 2009-09-11 MY MYPI2011001092A patent/MY148558A/en unknown
- 2009-09-11 AU AU2009291602A patent/AU2009291602B2/en not_active Ceased
- 2009-09-11 CN CN2009801456428A patent/CN102209721A/zh active Pending
- 2009-09-11 JP JP2011527012A patent/JP5579720B2/ja not_active Expired - Fee Related
- 2009-09-11 CA CA2736130A patent/CA2736130C/en not_active Expired - Fee Related
- 2009-09-11 PE PE2011000606A patent/PE20110805A1/es not_active Application Discontinuation
- 2009-09-11 WO PCT/US2009/056748 patent/WO2010030954A1/en active Application Filing
-
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 ZA ZA2011/02674A patent/ZA201102674B/en unknown
- 2011-04-11 MA MA33762A patent/MA32705B1/fr unknown
Also Published As
Publication number | Publication date |
---|---|
JP5579720B2 (ja) | 2014-08-27 |
KR20110073511A (ko) | 2011-06-29 |
MA32705B1 (fr) | 2011-10-02 |
ZA201102674B (en) | 2011-12-28 |
JP2012502112A (ja) | 2012-01-26 |
BRPI0918449A2 (pt) | 2019-09-24 |
EP2328903A1 (en) | 2011-06-08 |
WO2010030954A1 (en) | 2010-03-18 |
CA2736130C (en) | 2014-01-14 |
CR20110134A (es) | 2011-08-04 |
US8426447B2 (en) | 2013-04-23 |
MX2011002705A (es) | 2011-09-09 |
PE20110805A1 (es) | 2011-11-09 |
CO6362014A2 (es) | 2012-01-20 |
TW201022280A (en) | 2010-06-16 |
IL211440A0 (en) | 2011-05-31 |
CL2011000516A1 (es) | 2011-08-26 |
TWI385175B (zh) | 2013-02-11 |
EP2328903B1 (en) | 2014-03-05 |
US20100087429A1 (en) | 2010-04-08 |
AU2009291602B2 (en) | 2013-02-14 |
ES2459195T3 (es) | 2014-05-08 |
MY148558A (en) | 2013-04-30 |
CA2736130A1 (en) | 2010-03-18 |
CN102209721A (zh) | 2011-10-05 |
AU2009291602A1 (en) | 2010-03-18 |
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