PE20070367A1 - Compuestos de espiropiperidina como inhibidores de la enzima beta secretasa - Google Patents
Compuestos de espiropiperidina como inhibidores de la enzima beta secretasaInfo
- Publication number
- PE20070367A1 PE20070367A1 PE2006000854A PE2006000854A PE20070367A1 PE 20070367 A1 PE20070367 A1 PE 20070367A1 PE 2006000854 A PE2006000854 A PE 2006000854A PE 2006000854 A PE2006000854 A PE 2006000854A PE 20070367 A1 PE20070367 A1 PE 20070367A1
- Authority
- PE
- Peru
- Prior art keywords
- inhibitors
- compounds
- secretase enzyme
- beta secretase
- triazaespiro
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
- A61P25/28—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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
SE REFIERE A COMPUESTOS DE FORMULA (I) O SU TAUTOMERO DE FORMULA (I') DONDE R1 ES H, ALQUILO(C1-C10), CICLOALQUILO(C3-C12), ENTRE OTROS, OPCIONALMENTE SUSTITUIDOS CON H, HALO, OH, ENTRE OTROS; R2 ES HALO, CN, ALQUILO(C1-C10), ENTRE OTROS; R3 ES H, ALQUILO(C1-C10), FENILO, ENTRE OTROS, OPCIONALMENTE SUSTITUIDOS CON HALO, OH, CN, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 5(R,S),7(R,S)-8-BENCIL-4-(CICLOHEXILAMINO)-1-(3-FLUOROFENIL)-7-METIL-1,3,8-TRIAZAESPIRO[4,5]DEC-3-EN-2-ONA RACEMICA (DIASTEREOMERO A), 5(R,S),7(S,R)-8-BENCIL-4-(CICLOHEXILAMINO)-1-(3-FLUOROFENIL)-7-METIL-1,3,8-TRIAZAESPIRO[4,5]DEC-3-EN-2-ONA RACEMICA (DIASTEREOMERO B), 5(R,S),7(R,S)-4-(CICLOHEXILAMINO)-1-(3-FLUOROFENIL)-8-(3-ISOPROPOXIBENCIL)-7-METIL-1,3,8-TRIAZAESPIRO[4,5]DEC-3-EN-2-ONA RACEMICA (DIASTEREOMERO A), ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ENZIMA BETA SECRETASA SIENDO UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US70009005P | 2005-07-18 | 2005-07-18 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20070367A1 true PE20070367A1 (es) | 2007-05-12 |
Family
ID=37491690
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2006000854A PE20070367A1 (es) | 2005-07-18 | 2006-07-17 | Compuestos de espiropiperidina como inhibidores de la enzima beta secretasa |
Country Status (12)
Country | Link |
---|---|
US (1) | US8211904B2 (es) |
EP (1) | EP1910364B1 (es) |
JP (1) | JP2009502786A (es) |
CN (1) | CN101238124A (es) |
AR (1) | AR054560A1 (es) |
AT (1) | ATE550338T1 (es) |
AU (1) | AU2006270084B2 (es) |
CA (1) | CA2615656A1 (es) |
DO (1) | DOP2006000169A (es) |
PE (1) | PE20070367A1 (es) |
TW (1) | TW200728305A (es) |
WO (2) | WO2007011810A1 (es) |
Families Citing this family (60)
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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 |
US7790856B2 (en) * | 1998-04-07 | 2010-09-07 | Janssen Alzheimer Immunotherapy | Humanized antibodies that recognize beta amyloid peptide |
US20080050367A1 (en) | 1998-04-07 | 2008-02-28 | Guriq Basi | Humanized antibodies that recognize beta amyloid peptide |
US7964192B1 (en) | 1997-12-02 | 2011-06-21 | Janssen Alzheimer Immunotherapy | Prevention and treatment of amyloidgenic disease |
MY139983A (en) | 2002-03-12 | 2009-11-30 | Janssen Alzheimer Immunotherap | Humanized antibodies that recognize beta amyloid peptide |
US20060188512A1 (en) * | 2003-02-01 | 2006-08-24 | Ted Yednock | Active immunization to generate antibodies to solble a-beta |
US7521481B2 (en) | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
TW200635607A (en) * | 2004-12-15 | 2006-10-16 | Elan Pharm Inc | Humanized Aβ antibodies for use in improving cognition |
US7759353B2 (en) | 2005-06-14 | 2010-07-20 | Schering Corporation | Substituted spiro iminopyrimidinones as aspartyl protease inhibitors, compositions, and methods of treatment |
US8784810B2 (en) * | 2006-04-18 | 2014-07-22 | Janssen Alzheimer Immunotherapy | Treatment of amyloidogenic diseases |
TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
CA2662776A1 (en) * | 2006-09-07 | 2008-03-13 | Merck And Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
US8399473B2 (en) * | 2006-10-06 | 2013-03-19 | Merck, Sharp & Dohme, Corp. | Macrocyclic spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's disease |
JP2010508272A (ja) | 2006-10-30 | 2010-03-18 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病を治療するためのスピロピペリジンβセクレターゼ阻害剤 |
JP2010515681A (ja) * | 2007-01-04 | 2010-05-13 | メルク・シャープ・エンド・ドーム・コーポレイション | アルツハイマー病治療用の二環式スピロピペリジンベータ−セクレターゼ阻害剤 |
US8003097B2 (en) * | 2007-04-18 | 2011-08-23 | Janssen Alzheimer Immunotherapy | Treatment of cerebral amyloid angiopathy |
BRPI0810118A8 (pt) * | 2007-04-18 | 2015-09-29 | Janssen Alzheimer Immunotherap | Método para tratar doença, método para efetuar profilaxia contra caa, uso de um agente, método para reduzir amilóide vascular em um paciente, e, kit para tratamento |
TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
PT2182983E (pt) | 2007-07-27 | 2014-09-01 | Janssen Alzheimer Immunotherap | Tratamento de doenças amiloidogénicas com anticorpos anti-abeta humanizados |
JO3076B1 (ar) * | 2007-10-17 | 2017-03-15 | Janssen Alzheimer Immunotherap | نظم العلاج المناعي المعتمد على حالة apoe |
WO2009091016A1 (ja) | 2008-01-18 | 2009-07-23 | Eisai R & D Management Co., Ltd. | 縮合アミノジヒドロチアジン誘導体 |
ATE537178T1 (de) * | 2008-05-05 | 2011-12-15 | Pfizer | Neue klasse von spiro-piperidinen zur behandlung neurodegenerativer krankheiten |
JP5444240B2 (ja) * | 2008-07-28 | 2014-03-19 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | スピロアミノジヒドロチアジン誘導体 |
AU2009277485B2 (en) * | 2008-07-28 | 2013-05-02 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
ES2459195T3 (es) | 2008-09-11 | 2014-05-08 | Amgen Inc. | Compuestos de anillo espiro-tetracíclico como moduladores de beta-secretasa y métodos de uso |
US8198269B2 (en) * | 2008-09-30 | 2012-06-12 | Eisai R&D Management Co., Ltd. | Fused aminodihydrothiazine derivative |
US9067981B1 (en) | 2008-10-30 | 2015-06-30 | Janssen Sciences Ireland Uc | Hybrid amyloid-beta antibodies |
TW201020244A (en) | 2008-11-14 | 2010-06-01 | Astrazeneca Ab | New compounds |
AU2009318855A1 (en) * | 2008-11-23 | 2010-05-27 | Pfizer Inc. | Lactams as beta secretase inhibitors |
GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
EP2281824A1 (en) | 2009-08-07 | 2011-02-09 | Noscira, S.A. | Furan-imidazolone derivatives, for the treatment of cognitive, neurodegenerative or neuronal diseases or disorders |
PL2475428T3 (pl) | 2009-09-11 | 2015-12-31 | Probiodrug Ag | Pochodne heterocykliczne jako inhibitory cyklazy glutaminowej |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
JP2013522305A (ja) | 2010-03-15 | 2013-06-13 | 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スピロ−四環式環化合物 |
EP2547686B1 (en) | 2010-03-15 | 2014-01-22 | Amgen Inc. | Amino-dihydrooxazine and amino-dihydrothiazine spiro compounds as beta-secretase modulators and their medical use |
WO2011125006A2 (en) | 2010-04-09 | 2011-10-13 | Pfizer Inc. | Novel sultam compounds |
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 |
EP2643299B1 (en) | 2010-11-22 | 2016-06-22 | Noscira, S.A. | Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions |
US8957083B2 (en) | 2010-11-23 | 2015-02-17 | Amgen Inc. | Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use |
GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
JP5993875B2 (ja) | 2011-01-21 | 2016-09-14 | 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の合成に有用な方法および化合物 |
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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 |
WO2012112462A1 (en) | 2011-02-15 | 2012-08-23 | Amgen Inc. | Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use |
WO2012138590A1 (en) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their 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 |
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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 |
WO2013044092A1 (en) | 2011-09-21 | 2013-03-28 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
WO2013129622A1 (ja) | 2012-03-02 | 2013-09-06 | 武田薬品工業株式会社 | 複素環化合物およびその用途 |
US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
US8742111B1 (en) * | 2013-02-21 | 2014-06-03 | The United States Of America As Represented By The Secretary Of The Army | Synthesis of intermediate anilino methyl esters used in the production of synthetic opioid analgesics |
US10752588B2 (en) | 2014-12-19 | 2020-08-25 | The Broad Institute, Inc. | Dopamine D2 receptor ligands |
WO2016100940A1 (en) | 2014-12-19 | 2016-06-23 | The Broad Institute, Inc. | Dopamine d2 receptor ligands |
WO2016139501A1 (en) * | 2015-03-04 | 2016-09-09 | Tfchem | Gem difluorocompounds as depigmenting or lightening agents |
ES2812698T3 (es) | 2017-09-29 | 2021-03-18 | Probiodrug Ag | Inhibidores de glutaminil ciclasa |
UY38976A (es) * | 2019-12-03 | 2021-06-30 | Kallyope Inc | Antagonistas de sstr5 |
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US5221675A (en) * | 1989-12-15 | 1993-06-22 | Abbott Laboratories | Aza-spirocyclic compounds that enhance cholinergic neurotransmission |
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US20040067950A1 (en) | 1998-07-27 | 2004-04-08 | Schering-Plough Corporation | High affinity ligands for nociceptin receptor ORL-1 |
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JP2006512404A (ja) | 2002-10-22 | 2006-04-13 | グラクソ グループ リミテッド | H3受容体リガンドとしてのアリールオキシアルキルアミン誘導体 |
WO2004050039A2 (en) | 2002-12-04 | 2004-06-17 | Merck & Co., Inc. | Spirocyclic ureas, compositions containing such compounds and methods of use |
ATE402176T1 (de) * | 2002-12-13 | 2008-08-15 | Smithkline Beecham Corp | Pyrrolidin- und azetidinverbindungen alsccr5- antagonisten |
EP1644322A1 (en) | 2003-06-16 | 2006-04-12 | Sunesis Pharmaceuticals, Inc. | Aspartyl protease inhibitors |
GB0323204D0 (en) * | 2003-10-03 | 2003-11-05 | Novartis Ag | Organic compounds |
CN101068545A (zh) | 2004-10-13 | 2007-11-07 | 默克公司 | 作为β-分泌酶抑制剂用于治疗阿尔茨海默病的螺哌啶化合物 |
-
2006
- 2006-07-14 WO PCT/US2006/027544 patent/WO2007011810A1/en active Application Filing
- 2006-07-14 CA CA002615656A patent/CA2615656A1/en not_active Abandoned
- 2006-07-14 EP EP06787495A patent/EP1910364B1/en not_active Not-in-force
- 2006-07-14 AU AU2006270084A patent/AU2006270084B2/en not_active Ceased
- 2006-07-14 WO PCT/US2006/027594 patent/WO2007011833A2/en active Application Filing
- 2006-07-14 US US11/487,229 patent/US8211904B2/en active Active
- 2006-07-14 CN CNA2006800261467A patent/CN101238124A/zh active Pending
- 2006-07-14 AT AT06787495T patent/ATE550338T1/de active
- 2006-07-14 JP JP2008522854A patent/JP2009502786A/ja active Pending
- 2006-07-17 PE PE2006000854A patent/PE20070367A1/es not_active Application Discontinuation
- 2006-07-17 DO DO2006000169A patent/DOP2006000169A/es unknown
- 2006-07-17 AR ARP060103053A patent/AR054560A1/es not_active Application Discontinuation
- 2006-07-18 TW TW095126228A patent/TW200728305A/zh unknown
Also Published As
Publication number | Publication date |
---|---|
AR054560A1 (es) | 2007-06-27 |
CN101238124A (zh) | 2008-08-06 |
ATE550338T1 (de) | 2012-04-15 |
TW200728305A (en) | 2007-08-01 |
CA2615656A1 (en) | 2007-01-25 |
US8211904B2 (en) | 2012-07-03 |
EP1910364A2 (en) | 2008-04-16 |
AU2006270084B2 (en) | 2011-08-25 |
US20070021454A1 (en) | 2007-01-25 |
DOP2006000169A (es) | 2007-02-28 |
WO2007011810A1 (en) | 2007-01-25 |
WO2007011833A3 (en) | 2007-03-29 |
EP1910364B1 (en) | 2012-03-21 |
JP2009502786A (ja) | 2009-01-29 |
AU2006270084A1 (en) | 2007-01-25 |
WO2007011833A2 (en) | 2007-01-25 |
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