ATE483692T1 - Als beta-sekretase (bace)-hemmer nützliche 2- amino-chinazolinderivate - Google Patents
Als beta-sekretase (bace)-hemmer nützliche 2- amino-chinazolinderivateInfo
- Publication number
- ATE483692T1 ATE483692T1 AT05785256T AT05785256T ATE483692T1 AT E483692 T1 ATE483692 T1 AT E483692T1 AT 05785256 T AT05785256 T AT 05785256T AT 05785256 T AT05785256 T AT 05785256T AT E483692 T1 ATE483692 T1 AT E483692T1
- Authority
- AT
- Austria
- Prior art keywords
- beta
- bace
- secretase
- inhibitors
- amino
- Prior art date
Links
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 title abstract 3
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- CZAAKPFIWJXPQT-UHFFFAOYSA-N quinazolin-2-amine Chemical class C1=CC=CC2=NC(N)=NC=C21 CZAAKPFIWJXPQT-UHFFFAOYSA-N 0.000 title 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 2
- GQRRWNLARRRPRY-UHFFFAOYSA-N 1,4-dihydroquinazolin-2-amine Chemical class C1=CC=C2CNC(N)=NC2=C1 GQRRWNLARRRPRY-UHFFFAOYSA-N 0.000 abstract 1
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- IXHBTMCLRNMKHZ-LBPRGKRZSA-N levobunolol Chemical compound O=C1CCCC2=C1C=CC=C2OC[C@@H](O)CNC(C)(C)C IXHBTMCLRNMKHZ-LBPRGKRZSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
- C07D239/84—Nitrogen atoms
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D401/06—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 only aliphatic carbon atoms
-
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D405/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D413/06—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 carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Molecular Biology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US59981104P | 2004-08-06 | 2004-08-06 | |
| PCT/US2005/028191 WO2006017836A2 (en) | 2004-08-06 | 2005-08-08 | 2-amino-quinazoline derivatives useful as inhibitors of beta-secretase (bace) |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE483692T1 true ATE483692T1 (de) | 2010-10-15 |
Family
ID=35564387
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT05785256T ATE483692T1 (de) | 2004-08-06 | 2005-08-08 | Als beta-sekretase (bace)-hemmer nützliche 2- amino-chinazolinderivate |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8436006B2 (de) |
| EP (1) | EP1776349B1 (de) |
| JP (1) | JP4884387B2 (de) |
| CN (1) | CN101035771A (de) |
| AT (1) | ATE483692T1 (de) |
| CY (1) | CY1111086T1 (de) |
| DE (1) | DE602005024004D1 (de) |
| DK (1) | DK1776349T3 (de) |
| ES (1) | ES2351667T3 (de) |
| HR (1) | HRP20100595T1 (de) |
| PL (1) | PL1776349T3 (de) |
| PT (1) | PT1776349E (de) |
| RS (1) | RS51630B (de) |
| SI (1) | SI1776349T1 (de) |
| WO (1) | WO2006017836A2 (de) |
Families Citing this family (29)
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| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US8383637B2 (en) * | 2004-08-06 | 2013-02-26 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| US8426429B2 (en) * | 2004-08-06 | 2013-04-23 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| US8436006B2 (en) | 2004-08-06 | 2013-05-07 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| CN101228163A (zh) | 2005-06-14 | 2008-07-23 | 先灵公司 | 天冬氨酰蛋白酶抑制剂 |
| CA2610828A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Heterocyclic aspartyl protease inhibitors, preparation and use thereof |
| ATE502036T1 (de) * | 2005-10-25 | 2011-04-15 | Janssen Pharmaceutica Nv | Als inhibitoren von beta-sekretase (bace) geeignete 2-amino-3,4-dihydropyridoä3,4- düpyrimidinderivate |
| WO2007092846A2 (en) * | 2006-02-06 | 2007-08-16 | Janssen Pharmaceutica N.V. | 2-AMINO-3,4-DIHYDRO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE) |
| US7868022B2 (en) | 2006-02-06 | 2011-01-11 | Janssen Pharmaceutica Nv | 2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE) |
| WO2007092839A2 (en) * | 2006-02-06 | 2007-08-16 | Janssen Pharmaceutica N.V. | Macrocycle derivatives useful as inhibitors of beta-secretase (bace) |
| EP2032542A2 (de) | 2006-06-12 | 2009-03-11 | Schering Corporation | Heterozyklische aspartylproteasehemmer |
| JP2010512389A (ja) | 2006-12-12 | 2010-04-22 | 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阻害剤 |
| JP5450407B2 (ja) * | 2007-07-06 | 2014-03-26 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 置換アミノ−キナゾリノン、前記化合物を含む薬物、それらの使用及び製造方法 |
| CA2699787A1 (en) * | 2007-09-24 | 2009-04-02 | Comentis, Inc. | (3-hydroxy-4-amino-butan-2-yl)-3-(2-thiazol-2-yl-pyrrolidine-1-carbonyl) benzamide derivatives and related compounds as beta-secretase inhibitors for treating |
| JP5660898B2 (ja) * | 2007-11-09 | 2015-01-28 | ユニバーシティ オブ テネシー リサーチ ファウンデーション | 経口投与用の抗炎症性キナ酸誘導体 |
| NZ586831A (en) * | 2008-01-28 | 2012-02-24 | Janssen Pharmaceutica Nv | 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of beta-secretase (bace) |
| EP2240472B1 (de) * | 2008-01-29 | 2012-11-21 | Janssen Pharmaceutica NV | Als inhibitoren von beta-sekretase (bace) geeignete 2-aminochinolinderivate |
| CL2009000954A1 (es) | 2008-04-22 | 2010-12-31 | Schering Corp | Compuestos derivados de 2-imino-3-metil pirrolo pirimidinona,inhibidores de bace-1; composicion farmaceutica; y su uso para tratar, prevenir y/o retardar el inicio de una patologia de beta-amiloide seleccionada de enfermedad de alzheimer, enfermedad de parkinson, perdida de la memoria, sindrome de down, entre otras. |
| JP2012505241A (ja) * | 2008-10-10 | 2012-03-01 | パーデュー・リサーチ・ファウンデーション | アルツハイマー病の治療用組成物 |
| US8394807B2 (en) * | 2008-11-20 | 2013-03-12 | Purdue Research Foundation | Quinazoline inhibitors of BACE 1 and methods of using |
| WO2010065861A2 (en) | 2008-12-05 | 2010-06-10 | Purdue Research Foundation | Inhibitors of bace 1 and methods for treating alzheimer's disease |
| EP2504315A1 (de) | 2009-11-23 | 2012-10-03 | Amgen Inc. | Aminoheteroarylverbindungen als beta-sekretase-modulatoren und verwendungsverfahren dafür |
| CN103596939A (zh) * | 2011-04-13 | 2014-02-19 | 默沙东公司 | 作为bace抑制剂的5-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其应用 |
| MX2013011947A (es) * | 2011-04-13 | 2014-01-16 | Merck Sharp & Dohme | Iminotiazinas 5-sustituidas y sus monoxidos y dioxidos como inhibidores de la enzima que encinde la proteina precursora amiloide en el sitio beta, composiciones y su uso. |
| US9096541B2 (en) * | 2012-03-29 | 2015-08-04 | Oklahoma Medical Research Foundation | Inhibition of memapsin 1 cleavage in the treatment of diabetes |
| US9663475B2 (en) | 2013-02-25 | 2017-05-30 | Merck Patent Gmbh | 2 amino-3,4-dihydrcquinazoline derivatives and the use thereof as cathepsin D inhibitors |
| AU2019207491A1 (en) * | 2018-01-10 | 2020-07-30 | Cura Therapeutics, Llc | Pharmaceutical compositions comprising phenylsulfonamides, and their therapeutic applications |
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| RS51631B (sr) | 2004-08-06 | 2011-08-31 | Janssen Pharmaceutica N.V. | DERIVATI 2-AMINO-KVINAZOLINA KORISNI KAO INHIBITORI β-SEKRETAZE (BACE) |
| US8436006B2 (en) | 2004-08-06 | 2013-05-07 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| US8383637B2 (en) | 2004-08-06 | 2013-02-26 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| ES2403185T3 (es) | 2004-08-06 | 2013-05-16 | Janssen Pharmaceutica N.V. | Nuevos derivados de 2-amino-quinazolina útiles como inhibidores de ss-secretasa (BACE) |
| US8426429B2 (en) | 2004-08-06 | 2013-04-23 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| US20060074105A1 (en) | 2004-09-20 | 2006-04-06 | Serenex, Inc. | Substituted quinoline and quinazoline inhibitors of quinone reductase 2 |
| AU2006206654A1 (en) | 2005-01-19 | 2006-07-27 | Merck & Co., Inc. | Tertiary carbinamines having substituted heterocycles, which are active as inhibitors of beta-secretase, for the treatment of Alzheimer's disease |
| EP1895898B1 (de) | 2005-06-29 | 2011-02-16 | Compumedics Limited | Sensoranordnung mit leitfähiger brücke |
| ATE502036T1 (de) | 2005-10-25 | 2011-04-15 | Janssen Pharmaceutica Nv | Als inhibitoren von beta-sekretase (bace) geeignete 2-amino-3,4-dihydropyridoä3,4- düpyrimidinderivate |
| WO2007092839A2 (en) | 2006-02-06 | 2007-08-16 | Janssen Pharmaceutica N.V. | Macrocycle derivatives useful as inhibitors of beta-secretase (bace) |
| WO2007092846A2 (en) | 2006-02-06 | 2007-08-16 | Janssen Pharmaceutica N.V. | 2-AMINO-3,4-DIHYDRO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE) |
| US7868022B2 (en) | 2006-02-06 | 2011-01-11 | Janssen Pharmaceutica Nv | 2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE) |
| NZ586831A (en) | 2008-01-28 | 2012-02-24 | Janssen Pharmaceutica Nv | 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of beta-secretase (bace) |
| EP2240472B1 (de) | 2008-01-29 | 2012-11-21 | Janssen Pharmaceutica NV | Als inhibitoren von beta-sekretase (bace) geeignete 2-aminochinolinderivate |
-
2005
- 2005-08-04 US US11/197,615 patent/US8436006B2/en not_active Expired - Fee Related
- 2005-08-08 DE DE602005024004T patent/DE602005024004D1/de not_active Expired - Lifetime
- 2005-08-08 CN CNA2005800341221A patent/CN101035771A/zh active Pending
- 2005-08-08 RS RS20100564A patent/RS51630B/sr unknown
- 2005-08-08 HR HR20100595T patent/HRP20100595T1/hr unknown
- 2005-08-08 AT AT05785256T patent/ATE483692T1/de active
- 2005-08-08 PL PL05785256T patent/PL1776349T3/pl unknown
- 2005-08-08 ES ES05785256T patent/ES2351667T3/es not_active Expired - Lifetime
- 2005-08-08 EP EP05785256A patent/EP1776349B1/de not_active Expired - Lifetime
- 2005-08-08 JP JP2007525074A patent/JP4884387B2/ja not_active Expired - Fee Related
- 2005-08-08 PT PT05785256T patent/PT1776349E/pt unknown
- 2005-08-08 SI SI200531177T patent/SI1776349T1/sl unknown
- 2005-08-08 WO PCT/US2005/028191 patent/WO2006017836A2/en not_active Ceased
- 2005-08-08 DK DK05785256.8T patent/DK1776349T3/da active
-
2011
- 2011-01-04 CY CY20111100022T patent/CY1111086T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SI1776349T1 (sl) | 2011-01-31 |
| RS51630B (sr) | 2011-08-31 |
| DE602005024004D1 (de) | 2010-11-18 |
| DK1776349T3 (da) | 2011-01-24 |
| PT1776349E (pt) | 2010-12-06 |
| PL1776349T3 (pl) | 2011-04-29 |
| US20060178383A1 (en) | 2006-08-10 |
| JP4884387B2 (ja) | 2012-02-29 |
| ES2351667T3 (es) | 2011-02-09 |
| WO2006017836A3 (en) | 2006-06-29 |
| CN101035771A (zh) | 2007-09-12 |
| JP2008509165A (ja) | 2008-03-27 |
| WO2006017836A2 (en) | 2006-02-16 |
| EP1776349A2 (de) | 2007-04-25 |
| HRP20100595T1 (hr) | 2010-12-31 |
| EP1776349B1 (de) | 2010-10-06 |
| CY1111086T1 (el) | 2015-06-11 |
| US8436006B2 (en) | 2013-05-07 |
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