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
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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US7964192B1 (en) | 1997-12-02 | 2011-06-21 | Janssen Alzheimer Immunotherapy | Prevention and treatment of amyloidgenic disease |
US7790856B2 (en) * | 1998-04-07 | 2010-09-07 | Janssen Alzheimer Immunotherapy | Humanized antibodies that recognize beta amyloid peptide |
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 |
US20080050367A1 (en) * | 1998-04-07 | 2008-02-28 | Guriq Basi | Humanized antibodies that recognize beta amyloid peptide |
MY139983A (en) | 2002-03-12 | 2009-11-30 | Janssen Alzheimer Immunotherap | Humanized antibodies that recognize beta amyloid peptide |
RU2390350C2 (ru) * | 2003-02-01 | 2010-05-27 | Ньюралаб Лимитед | Активная иммунизация для создания антител к растворимому а-бета |
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 |
CA2590337C (en) * | 2004-12-15 | 2017-07-11 | Neuralab Limited | Humanized amyloid beta antibodies for use in improving cognition |
KR20080025079A (ko) | 2005-06-14 | 2008-03-19 | 쉐링 코포레이션 | 아스파르틸 프로테아제 억제제 |
WO2009017467A1 (en) | 2007-07-27 | 2009-02-05 | Elan Pharma International Limited | Treatment of amyloidogenic diseases |
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 |
EP2063889A4 (en) * | 2006-09-07 | 2009-09-16 | Merck & Co Inc | SPIROPIPERIDINE BETA SEKRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER 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 |
EP2091328B1 (en) | 2006-10-30 | 2011-12-28 | Merck Sharp & Dohme Corp. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
WO2008085509A1 (en) * | 2007-01-04 | 2008-07-17 | Merck & Co., Inc. | Bicyclic spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
CN101970000A (zh) * | 2007-04-18 | 2011-02-09 | 杨森阿尔茨海默氏症免疫治疗公司 | 脑淀粉样血管病的预防和治疗 |
US8003097B2 (en) * | 2007-04-18 | 2011-08-23 | Janssen Alzheimer Immunotherapy | Treatment of cerebral amyloid angiopathy |
TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
JO3076B1 (ar) * | 2007-10-17 | 2017-03-15 | Janssen Alzheimer Immunotherap | نظم العلاج المناعي المعتمد على حالة apoe |
US8158620B2 (en) * | 2008-01-18 | 2012-04-17 | Eisai R&D Management Co., Ltd. | Fused aminodihydrothiazine derivatives |
JP2011519913A (ja) * | 2008-05-05 | 2011-07-14 | ファイザー・インク | 神経変性疾患治療のための新規なクラスのスピロピペリジン |
CA2731209A1 (en) * | 2008-07-28 | 2010-02-04 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
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 |
MX2011002705A (es) | 2008-09-11 | 2011-09-09 | Amgen Inc | Compuestos con anillos espiro-triciclicos como moduladores de beta-secretasas y metodos de uso. |
AR073406A1 (es) * | 2008-09-30 | 2010-11-03 | Eisai R&D Man Co Ltd | Aminodihidrotiazinas fusionadas con tetrahidropiranos,inhibidoras de bace1 y de la produccion de abeta amiloide, composiciones farmaceuticas que las contienen y usos de las mismas para el tratamiento de enfermedades neurodegenerativas,tales como alzheimer. |
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 |
GEP20135806B (en) * | 2008-11-23 | 2013-04-10 | Pfizer | Lactams as beta secretase inhibitors |
GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
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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 |
EA022007B1 (ru) | 2009-09-11 | 2015-10-30 | Пробиодруг Аг | Гетероциклические производные в качестве ингибиторов глутаминилциклазы |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
AU2011227511B2 (en) | 2010-03-15 | 2014-02-20 | Amgen Inc. | Spiro-tetracyclic ring compounds as Beta - secretase modulators |
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 |
JP2013523806A (ja) | 2010-04-09 | 2013-06-17 | ファイザー・インク | スルタム化合物 |
EP2601197B1 (en) | 2010-08-05 | 2014-06-25 | Amgen Inc. | Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use |
US9284296B2 (en) | 2010-11-22 | 2016-03-15 | Aubergine Pharmaceuticals Llc | Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions |
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 |
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 |
WO2012100179A1 (en) | 2011-01-21 | 2012-07-26 | Eisai R&D Management Co., Ltd. | Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives |
GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
US9346827B2 (en) | 2011-02-07 | 2016-05-24 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use |
EP2675810A1 (en) | 2011-02-15 | 2013-12-25 | Amgen Inc. | Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators 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 |
US9079919B2 (en) * | 2011-05-27 | 2015-07-14 | Hoffmann-La Roche Inc. | Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors |
JP2014524472A (ja) | 2011-08-22 | 2014-09-22 | メルク・シャープ・アンド・ドーム・コーポレーション | Bace阻害剤としての2−スピロ置換イミノチアジンならびにそのモノオキシドおよびジオキシド、組成物、ならびにそれらの使用 |
US9296759B2 (en) | 2011-09-21 | 2016-03-29 | Amgen Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
JP6211509B2 (ja) | 2012-03-02 | 2017-10-11 | 武田薬品工業株式会社 | 複素環化合物およびその用途 |
WO2014078314A1 (en) | 2012-11-15 | 2014-05-22 | 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 |
EP3233077A4 (en) | 2014-12-19 | 2018-08-08 | The Broad Institute Inc. | Dopamine d2 receptor ligands |
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US7439251B2 (en) * | 2002-05-03 | 2008-10-21 | Israel Institute For Biological Research | Methods and compositions for treatment of central and peripheral nervous system disorders and novel compounds useful therefor |
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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 |
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AU2003296992A1 (en) * | 2002-12-13 | 2004-07-09 | Smithkline Beecham Corporation | Pyrrolidine and azetidine compounds as ccr5 antagonists |
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 |
AU2005295814A1 (en) * | 2004-10-13 | 2006-04-27 | Merck & Co., Inc. | Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of Alzhermer's disease |
-
2006
- 2006-07-14 AT AT06787495T patent/ATE550338T1/de active
- 2006-07-14 AU AU2006270084A patent/AU2006270084B2/en not_active Ceased
- 2006-07-14 EP EP06787495A patent/EP1910364B1/en not_active Not-in-force
- 2006-07-14 CN CNA2006800261467A patent/CN101238124A/zh active Pending
- 2006-07-14 WO PCT/US2006/027544 patent/WO2007011810A1/en active Application Filing
- 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 CA CA002615656A patent/CA2615656A1/en not_active Abandoned
- 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 |
---|---|
EP1910364B1 (en) | 2012-03-21 |
EP1910364A2 (en) | 2008-04-16 |
WO2007011833A2 (en) | 2007-01-25 |
DOP2006000169A (es) | 2007-02-28 |
WO2007011810A1 (en) | 2007-01-25 |
CN101238124A (zh) | 2008-08-06 |
TW200728305A (en) | 2007-08-01 |
CA2615656A1 (en) | 2007-01-25 |
JP2009502786A (ja) | 2009-01-29 |
US8211904B2 (en) | 2012-07-03 |
ATE550338T1 (de) | 2012-04-15 |
AU2006270084B2 (en) | 2011-08-25 |
AU2006270084A1 (en) | 2007-01-25 |
AR054560A1 (es) | 2007-06-27 |
WO2007011833A3 (en) | 2007-03-29 |
US20070021454A1 (en) | 2007-01-25 |
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Legal Events
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