CA2574218A1 - Substituted amide beta secretase inhibitors - Google Patents
Substituted amide beta secretase inhibitors Download PDFInfo
- Publication number
- CA2574218A1 CA2574218A1 CA002574218A CA2574218A CA2574218A1 CA 2574218 A1 CA2574218 A1 CA 2574218A1 CA 002574218 A CA002574218 A CA 002574218A CA 2574218 A CA2574218 A CA 2574218A CA 2574218 A1 CA2574218 A1 CA 2574218A1
- Authority
- CA
- Canada
- Prior art keywords
- compound
- alkyl
- substituted
- aryl
- mmol
- 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
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
- C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US59010204P | 2004-07-22 | 2004-07-22 | |
| US60/590,102 | 2004-07-22 | ||
| PCT/US2005/025780 WO2006014762A1 (en) | 2004-07-22 | 2005-07-20 | Substituted amide beta secretase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2574218A1 true CA2574218A1 (en) | 2006-02-09 |
Family
ID=35431616
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002574218A Abandoned CA2574218A1 (en) | 2004-07-22 | 2005-07-20 | Substituted amide beta secretase inhibitors |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US7803802B2 (https=) |
| EP (1) | EP1781625B1 (https=) |
| JP (1) | JP2008507538A (https=) |
| CN (1) | CN101014577A (https=) |
| AR (1) | AR049726A1 (https=) |
| AT (1) | ATE491693T1 (https=) |
| CA (1) | CA2574218A1 (https=) |
| DE (1) | DE602005025363D1 (https=) |
| ES (1) | ES2355733T3 (https=) |
| MX (1) | MX2007000760A (https=) |
| TW (1) | TW200621249A (https=) |
| WO (1) | WO2006014762A1 (https=) |
Families Citing this family (38)
| 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 |
| MX2007016180A (es) | 2005-06-14 | 2008-03-07 | Schering Corp | Inhibidores de aspartil proteasas. |
| JP2008543840A (ja) | 2005-06-14 | 2008-12-04 | シェーリング コーポレイション | アスパルチルプロテアーゼインヒビター |
| KR20090015967A (ko) | 2006-06-12 | 2009-02-12 | 쉐링 코포레이션 | 헤테로사이클릭 아스파르틸 프로테아제 억제제 |
| EP2089383B1 (en) | 2006-11-09 | 2015-09-16 | Probiodrug AG | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
| US9126987B2 (en) | 2006-11-30 | 2015-09-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| AU2007332754A1 (en) | 2006-12-12 | 2008-06-19 | Schering Corporation | Aspartyl protease inhibitors |
| AU2008220785B2 (en) | 2007-03-01 | 2013-02-21 | Vivoryon Therapeutics N.V. | New use of glutaminyl cyclase inhibitors |
| JP5667440B2 (ja) | 2007-04-18 | 2015-02-12 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体 |
| WO2009032277A1 (en) | 2007-09-06 | 2009-03-12 | Schering Corporation | Gamma secretase modulators |
| US8487099B2 (en) | 2007-11-05 | 2013-07-16 | Merck Sharp & Dohme Corp. | Gamma secretase modulators |
| EP2227471A1 (en) * | 2007-12-11 | 2010-09-15 | Schering Corporation | Gamma secretase modulators |
| US8450331B2 (en) | 2008-04-22 | 2013-05-28 | Merck Sharp & Dohme Corp. | Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use |
| RU2011123862A (ru) | 2008-11-13 | 2012-12-20 | Шеринг Корпорейшн | Модуляторы гамма-секретазы |
| US8759337B2 (en) | 2008-12-22 | 2014-06-24 | Merck Sharp & Dohme Corp. | Gamma secretase modulators |
| JP2012513400A (ja) | 2008-12-22 | 2012-06-14 | シェーリング コーポレイション | γ−セクレターゼ調節剤 |
| EP2443118A1 (en) | 2009-06-16 | 2012-04-25 | Schering Corporation | Gamma secretase modulators |
| WO2010147969A2 (en) | 2009-06-16 | 2010-12-23 | Schering Corporation | Gamma secretase modulators |
| US20120245158A1 (en) | 2009-06-16 | 2012-09-27 | Xianhai Huang | Gamma secretase modulators |
| JP5934645B2 (ja) | 2009-09-11 | 2016-06-15 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体 |
| US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| EP2485590B1 (en) | 2009-10-08 | 2015-01-07 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| WO2011107530A2 (en) | 2010-03-03 | 2011-09-09 | Probiodrug Ag | Novel inhibitors |
| JP5688745B2 (ja) | 2010-03-10 | 2015-03-25 | プロビオドルグ エージー | グルタミニルシクラーゼ（ｑｃ、ｅｃ２．３．２．５）の複素環阻害剤 |
| WO2011131748A2 (en) | 2010-04-21 | 2011-10-27 | Probiodrug Ag | Novel inhibitors |
| EP2686313B1 (en) | 2011-03-16 | 2016-02-03 | Probiodrug AG | Benzimidazole derivatives as inhibitors of glutaminyl cyclase |
| 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 |
| 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 |
| US20130060021A1 (en) * | 2011-09-07 | 2013-03-07 | Satori Pharmaceuticals, Inc. | Compounds useful for treating neurodegenerative disorders |
| AU2013235422B2 (en) | 2012-03-19 | 2016-12-15 | Buck Institute For Research On Aging | APP specific BACE inhibitors (ASBIs) and uses thereof |
| EP2908825B1 (en) | 2012-10-17 | 2018-04-18 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2014062553A1 (en) | 2012-10-17 | 2014-04-24 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US20140371283A1 (en) | 2013-02-12 | 2014-12-18 | Buck Institute For Research On Aging | Hydantoins that modulate bace-mediated app processing |
| ES2812698T3 (es) | 2017-09-29 | 2021-03-18 | Probiodrug Ag | Inhibidores de glutaminil ciclasa |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0395664A1 (en) * | 1987-10-21 | 1990-11-07 | The Upjohn Company | Renin inhibitors containing a (1-amino-2-hydroxy-2-heterocyclic) ethyl moiety |
| HRP990246A2 (en) | 1998-08-07 | 2000-06-30 | Du Pont Pharm Co | Succinoylamino benzodiazepines as inhibitors of a beta protein production |
| WO2000050391A1 (en) | 1999-02-26 | 2000-08-31 | Merck & Co., Inc. | Novel sulfonamide compounds and uses thereof |
| DE19934145C2 (de) * | 1999-07-26 | 2001-05-23 | Deutsche Telekom Mobil | Verfahren zur Herstellung von Kommunikationsverbindungen zu einer, einem Fahrzeug oder sonstigen mobilen oder ortsfesten Einrichtung zugeordneten, vorzugsweise mobilen Kommunikationsendeinrichtung |
| EP1299352B1 (en) | 2000-06-30 | 2005-12-28 | Elan Pharmaceuticals, Inc. | Compounds to treat alzheimer's disease |
| US6589978B2 (en) * | 2000-06-30 | 2003-07-08 | Hoffman-La Roche Inc. | 1-sulfonyl pyrrolidine derivatives |
| US6846813B2 (en) | 2000-06-30 | 2005-01-25 | Pharmacia & Upjohn Company | Compounds to treat alzheimer's disease |
| PE20020276A1 (es) | 2000-06-30 | 2002-04-06 | Elan Pharm Inc | COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER |
| WO2002088101A2 (en) | 2001-04-27 | 2002-11-07 | Vertex Pharmaceuticals Incorporated | Inhibitors of bace |
| JP2005504042A (ja) | 2001-08-03 | 2005-02-10 | シェーリング コーポレイション | γセクレターゼインヒビターのようなスルホンアミド誘導体 |
| WO2003014075A2 (en) * | 2001-08-03 | 2003-02-20 | Schering Corporation | Novel gamma secretase inhibitors |
| HUP0401241A3 (en) | 2001-08-21 | 2008-03-28 | Merck Sharp & Dohme | Novel cyclohexyl sulphones, process for their preparation and pharmaceutical compositions containing them |
| US6673821B2 (en) * | 2001-10-22 | 2004-01-06 | Enanta Pharmaceuticals, Inc. | Nitrogen heterocycle inhibitors of aspartyl protease |
| TW200302717A (en) | 2002-02-06 | 2003-08-16 | Schering Corp | Novel gamma secretase inhibitors |
| WO2003094854A2 (en) * | 2002-05-07 | 2003-11-20 | Elan Pharmaceuticals, Inc. | Succinoyl aminopyrazoles and related compounds |
| WO2004004396A1 (en) | 2002-06-26 | 2004-01-08 | Nokia Corporation | Method and network element for optimisation of radio resource utilisation in a radio access network |
| CA2505098A1 (en) * | 2002-11-12 | 2004-05-27 | Merck & Co., Inc. | Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease |
| WO2005108358A2 (en) * | 2004-04-22 | 2005-11-17 | Eli Lilly And Company | Pyrrolidine derivatives useful as bace inhibitors |
| AU2006315817A1 (en) * | 2005-11-16 | 2007-05-24 | Merck & Co., Inc. | Imidazolidinone compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease |
-
2005
- 2005-07-20 EP EP05773473A patent/EP1781625B1/en not_active Expired - Lifetime
- 2005-07-20 JP JP2007522711A patent/JP2008507538A/ja active Pending
- 2005-07-20 ES ES05773473T patent/ES2355733T3/es not_active Expired - Lifetime
- 2005-07-20 CN CNA2005800300344A patent/CN101014577A/zh active Pending
- 2005-07-20 AR ARP050103000A patent/AR049726A1/es not_active Application Discontinuation
- 2005-07-20 US US11/185,419 patent/US7803802B2/en active Active
- 2005-07-20 CA CA002574218A patent/CA2574218A1/en not_active Abandoned
- 2005-07-20 WO PCT/US2005/025780 patent/WO2006014762A1/en not_active Ceased
- 2005-07-20 AT AT05773473T patent/ATE491693T1/de not_active IP Right Cessation
- 2005-07-20 MX MX2007000760A patent/MX2007000760A/es active IP Right Grant
- 2005-07-20 DE DE602005025363T patent/DE602005025363D1/de not_active Expired - Lifetime
- 2005-07-21 TW TW094124686A patent/TW200621249A/zh unknown
-
2010
- 2010-08-23 US US12/861,347 patent/US8367712B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| WO2006014762A1 (en) | 2006-02-09 |
| EP1781625A1 (en) | 2007-05-09 |
| JP2008507538A (ja) | 2008-03-13 |
| US8367712B2 (en) | 2013-02-05 |
| MX2007000760A (es) | 2007-04-09 |
| DE602005025363D1 (de) | 2011-01-27 |
| ES2355733T3 (es) | 2011-03-30 |
| US7803802B2 (en) | 2010-09-28 |
| AR049726A1 (es) | 2006-08-30 |
| US20060040994A1 (en) | 2006-02-23 |
| ATE491693T1 (de) | 2011-01-15 |
| TW200621249A (en) | 2006-07-01 |
| US20110003825A1 (en) | 2011-01-06 |
| EP1781625B1 (en) | 2010-12-15 |
| CN101014577A (zh) | 2007-08-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| FZDE | Discontinued |
Effective date: 20130722 |