AR054560A1 - Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer - Google Patents
Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimerInfo
- Publication number
- AR054560A1 AR054560A1 ARP060103053A ARP060103053A AR054560A1 AR 054560 A1 AR054560 A1 AR 054560A1 AR P060103053 A ARP060103053 A AR P060103053A AR P060103053 A ARP060103053 A AR P060103053A AR 054560 A1 AR054560 A1 AR 054560A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- beta
- phenyl
- group
- Prior art date
Links
- 208000024827 Alzheimer disease Diseases 0.000 title abstract 2
- JUXAVSAMVBLDKO-UHFFFAOYSA-N 1-(1-azabicyclo[2.2.2]octan-3-yl)-3-[3-(1h-indol-3-yl)-1-oxo-1-spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylpropan-2-yl]urea Chemical compound C1N(CC2)CCC2C1NC(=O)NC(C(=O)N1CCC2(C3=CC=CC=C3CC2)CC1)CC1=CNC2=CC=CC=C12 JUXAVSAMVBLDKO-UHFFFAOYSA-N 0.000 title 1
- 239000002439 beta secretase inhibitor Substances 0.000 title 1
- -1 -OH Chemical group 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 abstract 3
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000006413 ring segment Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 1
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 abstract 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000003884 phenylalkyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
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)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Vascular Medicine (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
Son inhibidores de la enzima beta-secretasa y que son utiles en el tratamiento de enfermedades en las que está implicada la enzima beta- secretasa, tales como la enfermedad de Alzheimer. Composiciones farmacéuticas que comprenden estos compuestos y al uso de estos compuestos en el tratamiento de enfermedades en las que está implicada la enzima beta-secretasa. Reivindicacion 1: Un compuesto de formula (1) o su tautomero en las que R1 se selecciona del grupo constituido por H, alquilo C1-10, cicloalquilo C3-12, un grupo heterocíclico que tiene 4 a 8 átomos de anillo, en el que un átomo de anillo es un heteroátomo seleccionado del grupo constituido por N. S u O, y fenilo, en el que dicho resto R1 alquilo cicloalquilo, heterocíclico o fenilo está opcionalmente sustituido con uno o más de H, halo, -OH, -CN, -alquilo C1-10, -cicloalquilo C3-12, -O-alquilo C1-10, o fenilo; R2 está opcionalmente presente en uno o más de los átomos de C de anillo, y se selecciona del grupo constituido por halo, -OH, -CN, y -alquilo C1-10; R3 se selecciona del grupo constituido por H, - alquilo C1-10, -cicloalquilo C3-12, fenilo, y heteroarilo, en los que dicho resto R3 alquilo, cicloalquilo, fenilo o heteroarilo está opcionalmente sustituido con uno o más de halo, -OH, -CN, -alquilo C1-10, -cicloalquilo C3-12, -O-cicloalquilo C3-12, -O-alquilo C1-10, y dicho resto alquilo y cicloalquilo está opcionalmente sustituido con uno o más de halo, -OH, -CN, -cicloalquilo C3-12, -alquilo C1-10, o -O- alquilo C1-10, y sales farmacéuticamente aceptables de los mismos, y enantiomeros y diastereomeros individuales de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US70009005P | 2005-07-18 | 2005-07-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR054560A1 true AR054560A1 (es) | 2007-06-27 |
Family
ID=37491690
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060103053A AR054560A1 (es) | 2005-07-18 | 2006-07-17 | Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer |
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) | WO2007011833A2 (es) |
Families Citing this family (61)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7964192B1 (en) | 1997-12-02 | 2011-06-21 | Janssen Alzheimer Immunotherapy | Prevention and treatment of amyloidgenic disease |
| US20080050367A1 (en) | 1998-04-07 | 2008-02-28 | Guriq Basi | 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 |
| US7790856B2 (en) * | 1998-04-07 | 2010-09-07 | Janssen Alzheimer Immunotherapy | 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 |
| ES2545765T3 (es) * | 2003-02-01 | 2015-09-15 | Janssen Sciences Ireland Uc | Inmunización activa para generar anticuerpos para A-beta soluble |
| 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 |
| JP2008523815A (ja) * | 2004-12-15 | 2008-07-10 | エラン ファーマ インターナショナル リミテッド | 認知の改善における使用のためのヒト化アミロイドβ抗体 |
| MX2007016182A (es) | 2005-06-14 | 2008-03-07 | Schering Corp | Inhibidores de aspartil proteasas. |
| 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 |
| ATE549923T1 (de) * | 2006-10-06 | 2012-04-15 | Merck Sharp & Dohme | Makrozyklische spiropiperidin-beta-sekretase- hemmer zur behandlung von morbus alzheimer |
| EP2091328B1 (en) * | 2006-10-30 | 2011-12-28 | Merck Sharp & Dohme Corp. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
| 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 |
| EP2146746A4 (en) * | 2007-04-18 | 2011-03-23 | Janssen Alzheimer Immunotherap | PREVENTIVE AND TREATING ZEREBRALER AMYLOID ANGIOPATHY |
| 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 |
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| ES2375913T3 (es) * | 2008-05-05 | 2012-03-07 | Pfizer Inc. | Nueva clase de espiropiperidinas para el tratamiento de enfermedades neurodegenerativas. |
| 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 |
| CN102209721A (zh) | 2008-09-11 | 2011-10-05 | 安姆根有限公司 | 作为β-分泌酶调节剂的螺四环化合物及其使用方法 |
| KR20110076965A (ko) | 2008-09-30 | 2011-07-06 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 신규한 축합 아미노 디하이드로티아진 유도체 |
| 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 |
| US20110224231A1 (en) * | 2008-11-23 | 2011-09-15 | Pfizer Inc. | Novel Lactams as Beta Secretase Inhibitors |
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| WO2011029920A1 (en) | 2009-09-11 | 2011-03-17 | Probiodrug Ag | Heterocylcic derivatives as inhibitors of glutaminyl cyclase |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| 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 |
| MX2012010658A (es) | 2010-03-15 | 2012-12-05 | Amgen Inc | Compuestos de anillo espiro tetraciclico como moduladores de beta-secretasa. |
| EP2556076A2 (en) | 2010-04-09 | 2013-02-13 | 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 |
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| GB201101139D0 (en) * | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
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| 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 |
| 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 |
| US9145426B2 (en) | 2011-04-07 | 2015-09-29 | 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 |
| 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 |
| US9296759B2 (en) | 2011-09-21 | 2016-03-29 | Amgen Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| EP2821401B1 (en) | 2012-03-02 | 2020-09-09 | Takeda Pharmaceutical Company Limited | Dihydroquinolinone compounds as modulators of the muscarininc m1 receptor |
| 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 |
| WO2016100940A1 (en) | 2014-12-19 | 2016-06-23 | The Broad Institute, Inc. | Dopamine d2 receptor ligands |
| WO2016100823A1 (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 |
| DK3461819T3 (da) | 2017-09-29 | 2020-08-10 | Probiodrug Ag | Inhibitorer af glutaminylcyklase |
| JP2023516235A (ja) * | 2019-12-03 | 2023-04-19 | キャリーオペ,インク. | Sstr5アンタゴニスト |
| CN117143004B (zh) * | 2023-08-30 | 2026-01-09 | 安徽农业大学 | 一种手性氮杂螺环类化合物及其制备方法和应用 |
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| 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 AU AU2006270084A patent/AU2006270084B2/en not_active Ceased
- 2006-07-14 JP JP2008522854A patent/JP2009502786A/ja active Pending
- 2006-07-14 CN CNA2006800261467A patent/CN101238124A/zh active Pending
- 2006-07-14 CA CA002615656A patent/CA2615656A1/en not_active Abandoned
- 2006-07-14 AT AT06787495T patent/ATE550338T1/de active
- 2006-07-14 WO PCT/US2006/027594 patent/WO2007011833A2/en not_active Ceased
- 2006-07-14 US US11/487,229 patent/US8211904B2/en active Active
- 2006-07-14 EP EP06787495A patent/EP1910364B1/en not_active Not-in-force
- 2006-07-14 WO PCT/US2006/027544 patent/WO2007011810A1/en not_active Ceased
- 2006-07-17 AR ARP060103053A patent/AR054560A1/es not_active Application Discontinuation
- 2006-07-17 PE PE2006000854A patent/PE20070367A1/es not_active Application Discontinuation
- 2006-07-17 DO DO2006000169A patent/DOP2006000169A/es unknown
- 2006-07-18 TW TW095126228A patent/TW200728305A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2006270084B2 (en) | 2011-08-25 |
| TW200728305A (en) | 2007-08-01 |
| WO2007011833A3 (en) | 2007-03-29 |
| JP2009502786A (ja) | 2009-01-29 |
| CN101238124A (zh) | 2008-08-06 |
| US8211904B2 (en) | 2012-07-03 |
| WO2007011833A2 (en) | 2007-01-25 |
| EP1910364B1 (en) | 2012-03-21 |
| DOP2006000169A (es) | 2007-02-28 |
| ATE550338T1 (de) | 2012-04-15 |
| CA2615656A1 (en) | 2007-01-25 |
| US20070021454A1 (en) | 2007-01-25 |
| WO2007011810A1 (en) | 2007-01-25 |
| PE20070367A1 (es) | 2007-05-12 |
| AU2006270084A1 (en) | 2007-01-25 |
| EP1910364A2 (en) | 2008-04-16 |
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