ES2585262T3 - Compuestos heterocíclicos de hexahidropiran[3,4-d][1,3]tiazin-2-amina sustituidos como inhibidores de PPA, BACE1 y BACE2 - Google Patents

Compuestos heterocíclicos de hexahidropiran[3,4-d][1,3]tiazin-2-amina sustituidos como inhibidores de PPA, BACE1 y BACE2 Download PDF

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Publication number
ES2585262T3
ES2585262T3 ES13725822.4T ES13725822T ES2585262T3 ES 2585262 T3 ES2585262 T3 ES 2585262T3 ES 13725822 T ES13725822 T ES 13725822T ES 2585262 T3 ES2585262 T3 ES 2585262T3
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compounds
compound
formula
hexahydropyran
thiazin
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ES13725822.4T
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Spanish (es)
Inventor
Elizabeth Mary BECK
Michael Aaron Brodney
Christopher Ryan BUTLER
Jennifer Elizabeth Davoren
Brian Thomas O'neill
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Pfizer Corp Belgium
Pfizer Inc
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Pfizer Corp Belgium
Pfizer Inc
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • A61K31/542Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/22Anxiolytics
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    • A61P25/24Antidepressants
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P27/02Ophthalmic agents
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    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
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  • Pain & Pain Management (AREA)
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  • Obesity (AREA)
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  • Ophthalmology & Optometry (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
ES13725822.4T 2012-05-04 2013-04-22 Compuestos heterocíclicos de hexahidropiran[3,4-d][1,3]tiazin-2-amina sustituidos como inhibidores de PPA, BACE1 y BACE2 Active ES2585262T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261642480P 2012-05-04 2012-05-04
US201261642480P 2012-05-04
PCT/IB2013/053178 WO2013164730A1 (en) 2012-05-04 2013-04-22 Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2.

Publications (1)

Publication Number Publication Date
ES2585262T3 true ES2585262T3 (es) 2016-10-04

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ES13725822.4T Active ES2585262T3 (es) 2012-05-04 2013-04-22 Compuestos heterocíclicos de hexahidropiran[3,4-d][1,3]tiazin-2-amina sustituidos como inhibidores de PPA, BACE1 y BACE2

Country Status (9)

Country Link
US (2) US8962616B2 (show.php)
EP (1) EP2852597B1 (show.php)
JP (1) JP6110937B2 (show.php)
AR (1) AR090928A1 (show.php)
CA (1) CA2872154C (show.php)
ES (1) ES2585262T3 (show.php)
TW (1) TW201406765A (show.php)
UY (1) UY34778A (show.php)
WO (1) WO2013164730A1 (show.php)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013030713A1 (en) 2011-08-31 2013-03-07 Pfizer Inc. Hexahydropyrano [3,4-d][1,3] thiazin-2-amine compounds
WO2013164730A1 (en) * 2012-05-04 2013-11-07 Pfizer Inc. Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2.
US9260455B2 (en) 2012-09-20 2016-02-16 Pfizer Inc. Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
WO2014091352A1 (en) 2012-12-11 2014-06-19 Pfizer Inc. Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1
WO2014097038A1 (en) * 2012-12-19 2014-06-26 Pfizer Inc. CARBOCYCLIC- AND HETEROCYCLIC-SUBSTITUTED HEXAHYDROPYRANO[3,4-d][1,3]THIAZIN-2-AMINE COMPOUNDS
US9309263B2 (en) 2013-01-29 2016-04-12 Amgen Inc. Fused multi-cyclic sulfone compounds as inhibitors of beta-secretase and methods of use thereof
EP2956458B1 (en) 2013-02-13 2017-08-09 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
AU2014223334C1 (en) 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
SG11201507196WA (en) 2013-03-08 2015-10-29 Amgen Inc Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
JO3318B1 (ar) 2013-06-18 2019-03-13 Lilly Co Eli مثبطات bace
WO2015017407A1 (en) 2013-07-30 2015-02-05 Amgen Inc. Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta- secretase
AP2016009493A0 (en) 2014-04-10 2016-10-31 Pfizer 2-AMINO-6-METHYL-4,4a,5,6-TETRAHYDROPYRANO[3,4-d][1,3]THIAZIN-8a(8H)-YL-1,3-THIAZOL-4-YL AMIDES
MX381482B (es) 2014-08-08 2025-03-12 Amgen Inc Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso.
MA41101A (fr) * 2014-12-03 2017-10-10 Lilly Co Eli Dispositif d'injection de médicament automatique comportant une indication audible de progression d'injection
WO2017024180A1 (en) 2015-08-06 2017-02-09 Amgen Inc. Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
BR112018003489A2 (pt) 2015-09-24 2018-09-25 Pfizer n-[2-(2-amino-6,6-dissubstituído-4,4a,5,6-tetra-hidropirano[3,4-d][1,3]tiazin-8a(8h)-il)-1,3-tiazol-4-il]amidas
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
EP3353182A1 (en) * 2015-09-24 2018-08-01 Pfizer Inc Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors
JP7149271B2 (ja) 2016-12-15 2022-10-06 アムジエン・インコーポレーテツド β-セクレターゼ阻害剤としての1,4-チアジンジオキシドおよび1,2,4-チアジアジンジオキシド誘導体ならびに使用方法
WO2018112084A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
JP7177773B2 (ja) 2016-12-15 2022-11-24 アムジエン・インコーポレーテツド β-セクレターゼ阻害剤としてのオキサジン誘導体および使用方法
JP7159161B2 (ja) 2016-12-15 2022-10-24 アムジエン・インコーポレーテツド β-セクレターゼ阻害剤としてのシクロプロピル縮合チアジン誘導体および使用方法
MA54100A (fr) 2016-12-15 2021-10-20 Amgen Inc Dérivés de thiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
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
WO2020087031A1 (en) 2018-10-26 2020-04-30 The Research Foundation For The State University Of New York Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia
WO2024079733A1 (en) * 2022-10-12 2024-04-18 Adama Makhteshim Ltd. Process for the preparation of aminopyridazine derivatives

Family Cites Families (71)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994017197A1 (fr) 1993-01-25 1994-08-04 Takeda Chemical Industries, Ltd. ANTICORPS DIRIGE CONTRE LE β-AMYLOIDE OU UN DERIVE DE CE DERNIER ET SON UTILISATION
US8173127B2 (en) 1997-04-09 2012-05-08 Intellect Neurosciences, Inc. Specific antibodies to amyloid beta peptide, pharmaceutical compositions and methods of use thereof
NZ337765A (en) 1997-04-09 2001-09-28 Mindset Biopharmaceuticals Usa Recombinant antibodies having specificity for beta-amyloid N-terminus and C-terminus and use in treating Alzheimer's Disease
US6743427B1 (en) 1997-12-02 2004-06-01 Neuralab Limited Prevention and treatment of amyloidogenic disease
TWI239847B (en) 1997-12-02 2005-09-21 Elan Pharm Inc N-terminal fragment of Abeta peptide and an adjuvant for preventing and treating amyloidogenic disease
SI1257584T2 (sl) 2000-02-24 2013-07-31 Washington University St. Louis Humanizirana protitelesa, ki veĹľejo amiloidni peptid beta
DE10045112A1 (de) 2000-09-11 2002-03-21 Merck Patent Gmbh Verwendung von Indolderivaten zur Behandlung von Erkrankungen des zentralen Nervensystems
CA2427661C (en) 2000-11-03 2013-05-28 Proteotech, Inc. Methods of isolating amyloid-inhibiting compounds and use of compounds isolated from uncaria tomentosa and related plants
IL157253A0 (en) 2001-02-28 2004-02-19 Merck & Co Inc Acylated piperidine derivatives as melanocortin-4 receptor agonists
US20040192898A1 (en) 2001-08-17 2004-09-30 Jia Audrey Yunhua Anti-abeta antibodies
US20030195205A1 (en) 2001-11-02 2003-10-16 Pfizer Inc. PDE9 inhibitors for treating cardiovascular disorders
EA200400980A1 (ru) 2002-02-27 2005-02-24 Пфайзер Продактс Инк. Ингибиторы асс
DE10238724A1 (de) 2002-08-23 2004-03-04 Bayer Ag Alkyl-substituierte Pyrazolpyrimidine
DE10238723A1 (de) 2002-08-23 2004-03-11 Bayer Ag Phenyl-substituierte Pyrazolyprimidine
BR0315157A (pt) 2002-10-09 2005-08-09 Rinat Neuroscience Corp Métodos de tratar doença de alzheimer empregando-se anticorpos direcionados contra peptìdeo beta amilóide e composições deste
US20040220186A1 (en) 2003-04-30 2004-11-04 Pfizer Inc. PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease
EP1638935A1 (en) 2003-06-19 2006-03-29 Pfizer Products Inc. Nk1 antagonist
CA2538220A1 (en) 2003-09-09 2005-03-24 Takeda Pharmaceutical Company Limited Use of antibody
GB0327319D0 (en) 2003-11-24 2003-12-24 Pfizer Ltd Novel pharmaceuticals
BRPI0507374A (pt) 2004-02-02 2007-07-10 Pfizer Prod Inc moduladores do receptor de histamina-3
US7456164B2 (en) 2004-05-07 2008-11-25 Pfizer, Inc 3- or 4-monosubtituted phenol and thiophenol derivatives useful as H3 ligands
EP1595881A1 (en) 2004-05-12 2005-11-16 Pfizer Limited Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands
HRP20090471T1 (hr) 2004-05-12 2009-10-31 Pfizer Products Inc. Derivati prolina i njihova upotreba kao inhibitori dipeptidil-peptidaze iv
UA84208C2 (en) 2004-05-25 2008-09-25 Пфайзер Продактс Инк. Tetraazabenzo(e)azulene derivatives and analogs thereof
US20050267009A1 (en) 2004-05-28 2005-12-01 Deagle William R Method of Treatment of Acute and Persistent Pain
MX2007000998A (es) 2004-07-30 2007-07-11 Rinat Neuroscience Corp Anticuerpos dirigidos peptido beta-amiloide y procedimientos que usan los mismos.
US20090074775A1 (en) 2004-12-22 2009-03-19 David Michael Holtzman Use Of Anti-AB Antibody To Treat Traumatic Brain Injury
PA8660701A1 (es) 2005-02-04 2006-09-22 Pfizer Prod Inc Agonistas de pyy y sus usos
MY148086A (en) 2005-04-29 2013-02-28 Rinat Neuroscience Corp Antibodies directed against amyloid-beta peptide and methods using same
US8227475B2 (en) 2005-05-12 2012-07-24 Pfizer Inc. Anhydrous crystalline forms of N-[1-(2-ethoxyethyl)-5-(N-ethyl-N-methylamino)-7-(4-methylpyridin-2-yl-amino)-1H-pyrazolo[4,3-d]pyrimidine-3-carbonyl]methanesulfonamide
WO2006126082A2 (en) 2005-05-24 2006-11-30 Pharmacia & Upjohn Company Llc Pyridine [3,4-b] pyrazinones as pde-5 inhibitors
WO2006126081A2 (en) 2005-05-24 2006-11-30 Pharmacia & Upjohn Company Llc Pyridino [2 , 3-b] pyrazinones as pde-5 inhibitors
WO2006126083A1 (en) 2005-05-24 2006-11-30 Pharmacia & Upjohn Company Llc Pyridine [3 , 4-b] pyrazinone compounds as pde-5 inhibitors
US7812040B2 (en) 2005-06-22 2010-10-12 Pfizer Inc. Histamine-3 receptor antagonists
US8158673B2 (en) 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
WO2007052124A1 (en) 2005-11-04 2007-05-10 Pfizer Limited Tetrahydronaphthyridine derivative
WO2007063385A2 (en) 2005-12-01 2007-06-07 Pfizer Products Inc. Spirocyclic amine histamine-3 receptor antagonists
WO2007069053A1 (en) 2005-12-14 2007-06-21 Pfizer Products Inc. Benzimidazole antagonists of the h-3 receptor
WO2007088450A2 (en) 2006-02-01 2007-08-09 Pfizer Products Inc. Chromane antagonist of the h-3 receptor
WO2007088462A1 (en) 2006-02-01 2007-08-09 Pfizer Products Inc. Spirochromane antagonists of the h-3 receptor
WO2007099423A1 (en) 2006-03-02 2007-09-07 Pfizer Products Inc. 1-pyrrolidine indane derivatives as histamine-3 receptor antagonists
WO2007105053A2 (en) 2006-03-13 2007-09-20 Pfizer Products Inc. Tetralines antagonists of the h-3 receptor
JP5190448B2 (ja) 2006-04-20 2013-04-24 ファイザー・プロダクツ・インク グルコキナーゼ仲介疾患を予防および治療するための縮合フェニルアミド複素環化合物
HRP20110539T1 (hr) 2006-04-21 2011-08-31 Pfizer Products Inc. PIRIDINO[3,4-b]PIRAZINONI
WO2007138431A2 (en) 2006-05-30 2007-12-06 Pfizer Products Inc. Azabicyclic ether histamine-3 antagonists
AP2009004880A0 (en) 2006-11-29 2009-06-30 Pfizer Prod Inc Spiroketone acetyl-COA carboxylase inhibitors
CA2676456C (en) 2007-01-22 2012-03-27 Pfizer Products Inc. Tosylate salt of a therapeutic compound and pharmaceutical compositions thereof
US20090036425A1 (en) 2007-08-02 2009-02-05 Pfizer Inc Substituted bicyclolactam compounds
JP4520533B2 (ja) 2008-01-18 2010-08-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 縮合アミノジヒドロチアジン誘導体
EP2297164A1 (en) 2008-05-28 2011-03-23 Pfizer Inc. Pyrazolospiroketone acetyl-coa carboxylase inhibitors
US8318762B2 (en) 2008-05-28 2012-11-27 Pfizer Inc. Pyrazolospiroketone acetyl-CoA carboxylase inhibitors
WO2010013161A1 (en) 2008-07-29 2010-02-04 Pfizer Inc. Fluorinated heteroaryls
CN102149717B (zh) 2008-08-28 2014-05-14 辉瑞大药厂 二氧杂-双环[3.2.1]辛烷-2,3,4-三醇衍生物
CN102171221B (zh) 2008-09-30 2013-11-06 卫材R&D管理有限公司 新的稠合的氨基二氢噻嗪衍生物
WO2010086820A1 (en) 2009-02-02 2010-08-05 Pfizer Inc. 4-amino-5-oxo-7, 8-dihydropyrimido [5,4-f] [1,4] oxazepin-6 (5h) -yl) phenyl derivatives, pharmaceutical compositions and uses thereof
EP2406230A1 (en) 2009-03-11 2012-01-18 Pfizer Inc. Substituted indazole amides and their use as glucokinase activators
EP2604604A1 (en) 2009-03-11 2013-06-19 Pfizer Inc Benzofuranyl derivatives used as glucokinase inhibitors
JP2012520868A (ja) 2009-03-20 2012-09-10 ファイザー・インク 3−オキサ−7−アザビシクロ[3.3.1]ノナン
WO2010128425A1 (en) 2009-05-08 2010-11-11 Pfizer Inc. Gpr 119 modulators
CA2759891A1 (en) 2009-05-08 2010-11-11 Pfizer Inc. Gpr 119 modulators
US20100285145A1 (en) 2009-05-08 2010-11-11 Pfizer Inc Gpr 119 modulators
WO2010140092A1 (en) 2009-06-05 2010-12-09 Pfizer Inc. L- ( piperidin-4-yl) -pyrazole derivatives as gpr 119 modulators
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
WO2011005611A1 (en) 2009-07-09 2011-01-13 Merck Sharp & Dohme Corp. Neuromedin u receptor agonists and uses thereof
US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
EP2511269A4 (en) 2009-12-11 2013-04-24 Shionogi & Co FUSED HETEROCYCLIC COMPOUND HAVING AN AMINO GROUP
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
WO2013030713A1 (en) * 2011-08-31 2013-03-07 Pfizer Inc. Hexahydropyrano [3,4-d][1,3] thiazin-2-amine compounds
WO2013164730A1 (en) 2012-05-04 2013-11-07 Pfizer Inc. Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2.
EP2956458B1 (en) * 2013-02-13 2017-08-09 Pfizer Inc Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
WO2015140614A1 (en) 2014-03-21 2015-09-24 Align Technology, Inc. Segmented orthodontic appliance with elastics

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US20130296308A1 (en) 2013-11-07
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US8962616B2 (en) 2015-02-24
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JP6110937B2 (ja) 2017-04-05
US20150133438A1 (en) 2015-05-14
CA2872154A1 (en) 2013-11-07
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AR090928A1 (es) 2014-12-17

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