CA2660441A1 - Imidazolamines en tant qu'inhibiteurs de beta-secretase - Google Patents
Imidazolamines en tant qu'inhibiteurs de beta-secretase Download PDFInfo
- Publication number
- CA2660441A1 CA2660441A1 CA002660441A CA2660441A CA2660441A1 CA 2660441 A1 CA2660441 A1 CA 2660441A1 CA 002660441 A CA002660441 A CA 002660441A CA 2660441 A CA2660441 A CA 2660441A CA 2660441 A1 CA2660441 A1 CA 2660441A1
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- CA
- Canada
- Prior art keywords
- compound
- formula
- optionally substituted
- phenyl
- group
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
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- -1 Imidazole amines Chemical class 0.000 title claims description 30
- 239000003112 inhibitor Substances 0.000 title description 13
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 title description 10
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- 125000001072 heteroaryl group Chemical group 0.000 claims description 20
- 238000000034 method Methods 0.000 claims description 20
- 229910052757 nitrogen Inorganic materials 0.000 claims description 19
- 125000003118 aryl group Chemical group 0.000 claims description 15
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 15
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 14
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- SCODXNNXABJQIY-UHFFFAOYSA-N 8-[3-(2-fluoropyridin-3-yl)phenyl]-8-[4-(trifluoromethoxy)phenyl]-3,4-dihydroimidazo[5,1-c][1,2,4]oxadiazin-6-amine Chemical compound C12=NOCCN2C(N)=NC1(C=1C=C(C=CC=1)C=1C(=NC=CC=1)F)C1=CC=C(OC(F)(F)F)C=C1 SCODXNNXABJQIY-UHFFFAOYSA-N 0.000 claims description 2
- QIQBZQYBYKQPSP-UHFFFAOYSA-N 8-[3-(5-fluoropyridin-3-yl)phenyl]-8-[4-(trifluoromethoxy)phenyl]-3,4-dihydroimidazo[5,1-c][1,2,4]oxadiazin-6-amine Chemical compound C12=NOCCN2C(N)=NC1(C=1C=C(C=CC=1)C=1C=C(F)C=NC=1)C1=CC=C(OC(F)(F)F)C=C1 QIQBZQYBYKQPSP-UHFFFAOYSA-N 0.000 claims description 2
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- RRDVLXWUXDSNDZ-UHFFFAOYSA-N 8-(2,6-diethylpyridin-4-yl)-8-[3-(2-fluoropyridin-3-yl)phenyl]-3,4-dihydro-2h-imidazo[1,5-a]pyrimidin-6-amine Chemical compound CCC1=NC(CC)=CC(C2(C3=NCCCN3C(N)=N2)C=2C=C(C=CC=2)C=2C(=NC=CC=2)F)=C1 RRDVLXWUXDSNDZ-UHFFFAOYSA-N 0.000 claims 1
- BTKIVAGPTLXEER-UHFFFAOYSA-N 8-[3-(2-fluoropyridin-3-yl)phenyl]-8-[1-(2,2,2-trifluoroethyl)pyrazol-4-yl]-3,4-dihydro-2h-imidazo[1,5-a]pyrimidin-6-amine Chemical compound C12=NCCCN2C(N)=NC1(C=1C=C(C=CC=1)C=1C(=NC=CC=1)F)C=1C=NN(CC(F)(F)F)C=1 BTKIVAGPTLXEER-UHFFFAOYSA-N 0.000 claims 1
- SIFXKACBEOUPOD-UHFFFAOYSA-N 8-[3-(2-fluoropyridin-3-yl)phenyl]-8-pyridin-4-yl-3,4-dihydro-2h-imidazo[1,5-a]pyrimidin-6-amine Chemical compound C12=NCCCN2C(N)=NC1(C=1C=C(C=CC=1)C=1C(=NC=CC=1)F)C1=CC=NC=C1 SIFXKACBEOUPOD-UHFFFAOYSA-N 0.000 claims 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/20—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/20—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US83835706P | 2006-08-17 | 2006-08-17 | |
| US60/838,357 | 2006-08-17 | ||
| PCT/US2007/075690 WO2008022024A2 (fr) | 2006-08-17 | 2007-08-10 | Imidazolamines en tant qu'inhibiteurs de bêta-secrétase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2660441A1 true CA2660441A1 (fr) | 2008-02-21 |
Family
ID=38988046
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002660441A Abandoned CA2660441A1 (fr) | 2006-08-17 | 2007-08-10 | Imidazolamines en tant qu'inhibiteurs de beta-secretase |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP2054414A2 (fr) |
| JP (1) | JP2010500999A (fr) |
| AR (1) | AR062409A1 (fr) |
| CA (1) | CA2660441A1 (fr) |
| CL (1) | CL2007002288A1 (fr) |
| MX (1) | MX2009001699A (fr) |
| PE (1) | PE20080744A1 (fr) |
| TW (1) | TW200817406A (fr) |
| WO (1) | WO2008022024A2 (fr) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| AU2006259572A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Aspartyl protease inhibitors |
| EP2345411B1 (fr) | 2005-06-14 | 2013-10-02 | Merck Sharp & Dohme Corp. | Inhibiteurs hétérocycliques d'aspartyl protéase, leurs préparations et utilisations |
| CA2628074C (fr) | 2005-10-25 | 2014-01-14 | Shionogi & Co., Ltd. | Derive aminodihydrothiazine |
| US8168641B2 (en) | 2006-06-12 | 2012-05-01 | Schering Corporation | Aspartyl protease inhibitors |
| CA2683887A1 (fr) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | Derives d'aminodihydrothiazine substitues par un groupe cyclique ayant une activite inhibitoire contre la production de proteine beta amyloide |
| EP2151435A4 (fr) | 2007-04-24 | 2011-09-14 | Shionogi & Co | Composition pharmaceutique pour le traitement de la maladie d'alzheimer |
| BRPI0911356A2 (pt) | 2008-04-22 | 2019-09-24 | Schering Corp | compositos de 2-imino-3-metil pirrol pirimidina substituída por fenila como inibidores de bace-1, composições, e seu uso |
| JP5490692B2 (ja) | 2008-06-13 | 2014-05-14 | 塩野義製薬株式会社 | βセクレターゼ阻害作用を有する含硫黄複素環誘導体 |
| EP2360155A4 (fr) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-aminopyridin-4-one et dérivé de 2-aminopyridine dont l'activité inhibe la bace1 |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| EP2511268B2 (fr) | 2009-12-11 | 2021-02-17 | Shionogi & Co., Ltd. | Dérivé d'oxazine |
| EP2634186A4 (fr) | 2010-10-29 | 2014-03-26 | Shionogi & Co | Dérivé de naphtyridine |
| US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
| EP2694489B1 (fr) | 2011-04-07 | 2017-09-06 | Merck Sharp & Dohme Corp. | Composés de dioxyde de thiadiazine condensés avec des dérivés oxacycliques en c5-c6 comme inhibiteurs de bace, compositions, et utilisation use |
| WO2012138590A1 (fr) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | Composés de dioxyde de thiadiazine fusionnée à la pyrrolidine en tant qu'inhibiteurs de bace, compositions et leur utilisation |
| EP2703399A4 (fr) | 2011-04-26 | 2014-10-15 | Shionogi & Co | Dérivé d'oxazine et inhibiteur de bace 1 le contenant |
| RU2014111055A (ru) | 2011-08-22 | 2015-09-27 | Мерк Шарп И Доум Корп. | 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение |
| WO2014065434A1 (fr) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dérivés de dihydrooxazine ou d'oxazépine ayant une activité inhibitrice de bace1 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200602048A (en) * | 2004-06-16 | 2006-01-16 | Wyeth Corp | Diphenylimidazopyrimidine and -imidazole amines as inhibitors of β -secretase |
| DE602005017033D1 (de) * | 2004-06-16 | 2009-11-19 | Wyeth Corp | Amino-5,5-diphenylimidazolon-derivate zur beta-sekretase-hemmung |
| BRPI0606690A2 (pt) * | 2005-01-14 | 2009-07-14 | Wyeth Corp | composto; uso do composto para o tratamento de uma doença ou distúrbio associado com uma atividade excessiva de bace; e composição farmacêutica |
| WO2007005404A1 (fr) * | 2005-06-30 | 2007-01-11 | Wyeth | DÉRIVÉS D'IMIDAZOLONE PORTANT UN GROUPEMENT HÉTÉROARYLE À 6 CHAÎNONS EN POSITION 5 ET UN GROUPEMENT AMINO, ET LEUR EMPLOI DANS LA RÉGULATION DE LA β-SECRÉTASE |
| TW200738683A (en) * | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
-
2007
- 2007-07-24 TW TW096126963A patent/TW200817406A/zh unknown
- 2007-08-07 PE PE2007001049A patent/PE20080744A1/es not_active Application Discontinuation
- 2007-08-07 CL CL200702288A patent/CL2007002288A1/es unknown
- 2007-08-10 WO PCT/US2007/075690 patent/WO2008022024A2/fr active Application Filing
- 2007-08-10 CA CA002660441A patent/CA2660441A1/fr not_active Abandoned
- 2007-08-10 JP JP2009524746A patent/JP2010500999A/ja not_active Withdrawn
- 2007-08-10 MX MX2009001699A patent/MX2009001699A/es not_active Application Discontinuation
- 2007-08-10 EP EP07840855A patent/EP2054414A2/fr not_active Withdrawn
- 2007-08-16 AR ARP070103654A patent/AR062409A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PE20080744A1 (es) | 2008-05-24 |
| AR062409A1 (es) | 2008-11-05 |
| MX2009001699A (es) | 2009-02-25 |
| EP2054414A2 (fr) | 2009-05-06 |
| TW200817406A (en) | 2008-04-16 |
| WO2008022024A2 (fr) | 2008-02-21 |
| WO2008022024A3 (fr) | 2008-05-22 |
| CL2007002288A1 (es) | 2008-02-08 |
| JP2010500999A (ja) | 2010-01-14 |
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