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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Prior art keywords
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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    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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

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  • Organic Chemistry (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Addiction (AREA)
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  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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 (enExample)
EP (1) EP2852597B1 (enExample)
JP (1) JP6110937B2 (enExample)
AR (1) AR090928A1 (enExample)
CA (1) CA2872154C (enExample)
ES (1) ES2585262T3 (enExample)
TW (1) TW201406765A (enExample)
UY (1) UY34778A (enExample)
WO (1) WO2013164730A1 (enExample)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6043355B2 (ja) * 2011-08-31 2016-12-14 ファイザー・インク ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物
JP6110937B2 (ja) 2012-05-04 2017-04-05 ファイザー・インク ＡＰＰ、ＢＡＣＥ１、およびＢＡＣＥ２の阻害剤としての複素環式置換ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物
US9260455B2 (en) 2012-09-20 2016-02-16 Pfizer Inc. Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
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
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
JP2016507551A (ja) 2013-02-13 2016-03-10 ファイザー・インク ヘテロアリール置換ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物
US9233981B1 (en) * 2013-02-15 2016-01-12 Pfizer Inc. Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
TW201446758A (zh) 2013-03-01 2014-12-16 Amgen Inc 作爲β－分泌酶抑制劑的全氟化５，６－二氫－４Ｈ－１，３－□－２－胺化合物及其用途
KR20150124985A (ko) 2013-03-08 2015-11-06 암젠 인크 베타-세크레타제 억제제로서 퍼플루오르화된 사이클로프로필 융합된 1,3-옥사진-2-아민 화합물 및 그의 사용 방법
JO3318B1 (ar) 2013-06-18 2019-03-13 Lilly Co Eli مثبطات bace
US9096615B2 (en) 2013-07-30 2015-08-04 Amgen Inc. Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof
CR20160455A (es) 2014-04-10 2016-12-16 Pfizer 2-AMINO-6-METIL-4,4a,5,6-TETRAHIDROPIRANO[3,4-d][1,3]TIAZIN-8a(8H)-IL-1,3-TIAZOL-4-ILA
CA2957544C (en) 2014-08-08 2023-01-24 Amgen Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
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
WO2017051303A1 (en) * 2015-09-24 2017-03-30 Pfizer Inc. Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors
EP3353174A1 (en) 2015-09-24 2018-08-01 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
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
EP3555106B1 (en) 2016-12-15 2022-03-09 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
US11021493B2 (en) 2016-12-15 2021-06-01 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
MA54100A (fr) 2016-12-15 2021-10-20 Amgen Inc Dérivés de thiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
US10889581B2 (en) 2016-12-15 2021-01-12 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
US10947223B2 (en) 2016-12-15 2021-03-16 Amgen Inc. Substituted oxazines as beta-secretase inhibitors
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
US20250353832A1 (en) * 2022-10-12 2025-11-20 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
EP1308461A3 (en) 1993-01-25 2004-02-11 Takeda Chemical Industries, Ltd. Antibodies to beta-amyloids or their derivatives and use thereof
US8173127B2 (en) 1997-04-09 2012-05-08 Intellect Neurosciences, Inc. Specific antibodies to amyloid beta peptide, pharmaceutical compositions and methods of use thereof
CA2286305A1 (en) 1997-04-09 1998-10-15 Mindset Ltd. Recombinant antibodies specific for beta-amyloid ends, dna encoding and methods of use thereof
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
US6905686B1 (en) 1997-12-02 2005-06-14 Neuralab Limited Active immunization for treatment of alzheimer's disease
SK288723B6 (sk) 2000-02-24 2020-01-07 Univ Washington Farmaceutický prostriedok a použitie tohto farmaceutického prostriedku
DE10045112A1 (de) 2000-09-11 2002-03-21 Merck Patent Gmbh Verwendung von Indolderivaten zur Behandlung von Erkrankungen des zentralen Nervensystems
AU2002239764B2 (en) 2000-11-03 2007-06-21 Proteotech, Inc. Methods of isolating amyloid-inhibiting compounds and use of compounds isolated from uncaria tomentosa and related plants
GEP20053710B (en) 2001-02-28 2005-12-26 Merck & Co Inc Acylated Piperidine Derivatives as Melanocortin-4 Receptor Agonists
JP2005503789A (ja) 2001-08-17 2005-02-10 イーライ・リリー・アンド・カンパニー 抗Ａβ抗体
US20030195205A1 (en) 2001-11-02 2003-10-16 Pfizer Inc. PDE9 inhibitors for treating cardiovascular disorders
EP1478437B1 (en) 2002-02-27 2005-08-31 Pfizer Products Inc. Acc inhibitors
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
MXPA05003621A (es) 2002-10-09 2005-10-19 Rinat Neuroscience Corp Metodos de tratamiento de la enfermedad de alzheimer usando anticuerpos dirigidos contra el peptido beta amiloide y composiciones de los mismos.
US20040220186A1 (en) 2003-04-30 2004-11-04 Pfizer Inc. PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease
JP2006527756A (ja) 2003-06-19 2006-12-07 ファイザー・プロダクツ・インク Ｎｋ１拮抗薬
WO2005025616A1 (ja) 2003-09-09 2005-03-24 Takeda Pharmaceutical Company Limited 抗体の用途
GB0327319D0 (en) 2003-11-24 2003-12-24 Pfizer Ltd Novel pharmaceuticals
JP2007519707A (ja) 2004-02-02 2007-07-19 ファイザー・プロダクツ・インク ヒスタミン−３受容体モジュレーター
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
WO2005116014A1 (en) 2004-05-12 2005-12-08 Pfizer Products Inc. Proline derivatives and their use as dipeptidyl peptidase iv inhibitors
EP1753766A1 (en) 2004-05-25 2007-02-21 Pfizer Products Inc. 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
BRPI0513959A (pt) 2004-07-30 2008-05-20 Rinat Neuroscience Corp anticorpos dirigidos contra o peptìdeo beta-amilóide, suas composições farmacêuticas, kit e métodos de fabricação dos mesmos
WO2006069081A2 (en) 2004-12-22 2006-06-29 Washington University In St. Louis USE OF ANTI-Aβ ANTIBODY TO TREAT TRAUMATIC BRAIN INJURY
PA8660701A1 (es) 2005-02-04 2006-09-22 Pfizer Prod Inc Agonistas de pyy y sus usos
PE20061323A1 (es) 2005-04-29 2007-02-09 Rinat Neuroscience Corp Anticuerpos dirigidos contra el peptido amiloide beta y metodos que utilizan los mismos
CA2608018C (en) 2005-05-12 2010-07-13 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
WO2006126083A1 (en) 2005-05-24 2006-11-30 Pharmacia & Upjohn Company Llc Pyridine [3 , 4-b] pyrazinone compounds as pde-5 inhibitors
WO2006126082A2 (en) 2005-05-24 2006-11-30 Pharmacia & Upjohn Company Llc Pyridine [3,4-b] pyrazinones as pde-5 inhibitors
CA2603830A1 (en) 2005-05-24 2006-11-30 Pharmacia & Upjohn Co Llc PYRIDINE [2,3-B] PYRAZINONES
JP2008543923A (ja) 2005-06-22 2008-12-04 ファイザー・プロダクツ・インク ヒスタミン−３受容体アンタゴニスト
US8158673B2 (en) 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
CA2624625A1 (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
CA2643055A1 (en) 2006-03-13 2007-09-20 Pfizer Products Inc. Tetralines antagonists of the h-3 receptor
WO2007122482A1 (en) 2006-04-20 2007-11-01 Pfizer Products Inc. Fused phenyl amido heterocyclic compounds for the prevention and treatment of glucokinase-mediated diseases
CN101454320B (zh) 2006-04-21 2012-12-19 辉瑞产品公司 吡啶并[3，4-b]吡嗪酮
WO2007138431A2 (en) 2006-05-30 2007-12-06 Pfizer Products Inc. Azabicyclic ether histamine-3 antagonists
US20090270435A1 (en) 2006-11-29 2009-10-29 Jeffrey Wayne Corbett Spiroketone Acetyl-CoA Carboxylase Inhibitors
EP2124933B1 (en) 2007-01-22 2012-10-17 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
HUE026064T2 (en) 2008-01-18 2016-05-30 Eisai R&D Man Co Ltd Condensed aminodihydrothiazine derivatives
CA2724603A1 (en) 2008-05-28 2009-12-03 Pfizer Inc. Pyrazolospiroketone acetyl-coa carboxylase inhibitors
CA2724774C (en) 2008-05-28 2013-06-25 Pfizer Inc. Pyrazolospiroketone acetyl-coa carboxylase inhibitors
EP2318370A1 (en) 2008-07-29 2011-05-11 Pfizer Inc. Fluorinated heteroaryls
PE20110288A1 (es) 2008-08-28 2011-05-26 Pfizer Derivados de dioxa-biciclo[3.2.1]octano-2,3,4-triol
ES2539859T3 (es) 2008-09-30 2015-07-06 Eisai R&D Management Co., Ltd. Nuevo derivado de aminodihidrotiazina condensado
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
AP3179A (en) 2009-03-11 2015-03-31 Pfizer Benzofuranyl derivatives used as glucokinase inhibitors
WO2010103438A1 (en) 2009-03-11 2010-09-16 Pfizer Inc. Substituted indazole amides and their use as glucokinase activators
EP2408780A2 (en) 2009-03-20 2012-01-25 Pfizer Inc. 3-oxa-7-azabicycloý3.3.1¨nonanes
WO2010128414A1 (en) 2009-05-08 2010-11-11 Pfizer Inc. Gpr 119 modulators
WO2010128425A1 (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
EP2438051A1 (en) 2009-06-05 2012-04-11 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
JP6043355B2 (ja) * 2011-08-31 2016-12-14 ファイザー・インク ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物
JP6110937B2 (ja) * 2012-05-04 2017-04-05 ファイザー・インク ＡＰＰ、ＢＡＣＥ１、およびＢＡＣＥ２の阻害剤としての複素環式置換ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物
JP2016507551A (ja) * 2013-02-13 2016-03-10 ファイザー・インク ヘテロアリール置換ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物
CN111772834B (zh) 2014-03-21 2022-07-15 阿莱恩技术有限公司 具有弹性体的分段的正畸矫正器

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CA2872154A1 (en) 2013-11-07
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