ES2261699T3 - Macrociclos utiles en el tratamiento de la enfermedad de alzheimer. - Google Patents
Macrociclos utiles en el tratamiento de la enfermedad de alzheimer.Info
- Publication number
- ES2261699T3 ES2261699T3 ES02752056T ES02752056T ES2261699T3 ES 2261699 T3 ES2261699 T3 ES 2261699T3 ES 02752056 T ES02752056 T ES 02752056T ES 02752056 T ES02752056 T ES 02752056T ES 2261699 T3 ES2261699 T3 ES 2261699T3
- Authority
- ES
- Spain
- Prior art keywords
- ethyl
- oxa
- hydroxy
- fluoro
- diaza
- 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.)
- Expired - Lifetime
Links
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- 229920001296 polysiloxane Polymers 0.000 description 1
- LPNYRYFBWFDTMA-UHFFFAOYSA-N potassium tert-butoxide Chemical compound [K+].CC(C)(C)[O-] LPNYRYFBWFDTMA-UHFFFAOYSA-N 0.000 description 1
- MICLTPPSCUXHJT-UHFFFAOYSA-M potassium;4-[3-(6-oxo-3h-purin-9-yl)propanoylamino]benzoate Chemical compound [K+].C1=CC(C(=O)[O-])=CC=C1NC(=O)CCN1C(NC=NC2=O)=C2N=C1 MICLTPPSCUXHJT-UHFFFAOYSA-M 0.000 description 1
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- 102000004169 proteins and genes Human genes 0.000 description 1
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- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 description 1
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 description 1
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- 229960001404 quinidine Drugs 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
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- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
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- NCDNCNXCDXHOMX-XGKFQTDJSA-N ritonavir Chemical compound N([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1SC=NC=1)CC=1C=CC=CC=1)C(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-XGKFQTDJSA-N 0.000 description 1
- 229960000311 ritonavir Drugs 0.000 description 1
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- 235000019204 saccharin Nutrition 0.000 description 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
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- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
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- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 description 1
- 229960002930 sirolimus Drugs 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 239000007892 solid unit dosage form Substances 0.000 description 1
- 238000000638 solvent extraction Methods 0.000 description 1
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- 229960001603 tamoxifen Drugs 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- ILMRJRBKQSSXGY-UHFFFAOYSA-N tert-butyl(dimethyl)silicon Chemical group C[Si](C)C(C)(C)C ILMRJRBKQSSXGY-UHFFFAOYSA-N 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
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- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
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Classifications
-
- 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
-
- 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
- C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
- C07D273/02—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and only one oxygen atom
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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29754601P | 2001-06-12 | 2001-06-12 | |
| US297546P | 2001-06-12 | ||
| US33308301P | 2001-11-19 | 2001-11-19 | |
| US333083P | 2001-11-19 |
Publications (1)
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|---|---|
| ES2261699T3 true ES2261699T3 (es) | 2006-11-16 |
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| Application Number | Title | Priority Date | Filing Date |
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| ES02752056T Expired - Lifetime ES2261699T3 (es) | 2001-06-12 | 2002-06-12 | Macrociclos utiles en el tratamiento de la enfermedad de alzheimer. |
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| EP (1) | EP1404671B1 (enExample) |
| JP (1) | JP2004534064A (enExample) |
| AT (1) | ATE323084T1 (enExample) |
| BR (1) | BR0210392A (enExample) |
| CA (1) | CA2450202A1 (enExample) |
| DE (1) | DE60210614T2 (enExample) |
| ES (1) | ES2261699T3 (enExample) |
| MX (1) | MXPA03011466A (enExample) |
| WO (1) | WO2002100856A1 (enExample) |
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| CA2469622A1 (en) * | 2001-12-06 | 2003-06-19 | Elan Pharmaceuticals, Inc. | Substituted hydroxyethylamines |
| EP1583750B1 (en) | 2003-01-07 | 2013-02-27 | Merck Sharp & Dohme Corp. | Macrocyclic beta-secretase inhibitors for treatment of Alzheimer's disease |
| US7521481B2 (en) | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
| ATE457995T1 (de) | 2003-06-18 | 2010-03-15 | Tranzyme Pharma Inc | Makrozyklische motilin rezeptorantagonisten |
| GB0325830D0 (en) * | 2003-11-05 | 2003-12-10 | Novartis Ag | Organic compounds |
| US7652003B2 (en) * | 2004-07-28 | 2010-01-26 | Schering-Plough Corporation | Macrocyclic β-secretase inhibitors |
| GB0500683D0 (en) | 2005-01-13 | 2005-02-23 | Novartis Ag | Organic compounds |
| CA2593268A1 (en) * | 2005-01-13 | 2006-07-20 | Novartis Ag | Macrocyclic compounds useful as bace inhibitors |
| AU2006235344B2 (en) | 2005-04-08 | 2012-07-26 | Comentis, Inc. | Compounds which inhibit beta-secretase activity and methods of use thereof |
| US7338974B2 (en) | 2005-08-12 | 2008-03-04 | Bristol-Myers Squibb Company | Macrocyclic diaminopropanes as beta-secretase inhibitors |
| GB0526614D0 (en) * | 2005-12-30 | 2006-02-08 | Novartis Ag | Organic compounds |
| CN101484431A (zh) * | 2006-07-20 | 2009-07-15 | 诺瓦提斯公司 | 大环内酰胺 |
| RU2009105762A (ru) * | 2006-07-20 | 2010-08-27 | Новартис АГ (CH) | Макроциклические соединения, применимые в качестве ингибиторов васе |
| US7678784B2 (en) | 2006-11-20 | 2010-03-16 | Bristol-Myers Squibb Company | Oxime-containing macrocyclic acyl guanidines as β-secretase inhibitors |
| US7772221B2 (en) | 2007-02-09 | 2010-08-10 | Bristol-Meyers Squibb Company | Diaminopropane derived macrocycles as inhibitors of β amyloid production |
| US20100063013A1 (en) * | 2007-03-26 | 2010-03-11 | Renata Oballa | Cathepsin cysteine protease inhibitors |
| US7732434B2 (en) | 2007-04-20 | 2010-06-08 | Bristol-Myers Squibb Company | Macrocyclic acyl guanidines as beta-secretase inhibitors |
| WO2014144346A1 (en) * | 2013-03-15 | 2014-09-18 | The Board Of Regents Of The University Of Texas System | Use of inhibitors of mtor to improve vascular functions in apoe4 carriers |
| DK3089737T3 (da) | 2013-12-31 | 2021-12-13 | Rapamycin Holdings Llc | Orale rapamycin-nanopartikelpræparater og anvendelse. |
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| AUPM982594A0 (en) * | 1994-12-02 | 1995-01-05 | University Of Queensland, The | HIV protease inhibitors |
| EP1192177A1 (en) * | 1999-06-15 | 2002-04-03 | Elan Pharmaceuticals, Inc. | Statine-derived tetrapeptide inhibitors of beta-secretase |
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2002
- 2002-06-12 AT AT02752056T patent/ATE323084T1/de not_active IP Right Cessation
- 2002-06-12 CA CA002450202A patent/CA2450202A1/en not_active Abandoned
- 2002-06-12 WO PCT/US2002/019076 patent/WO2002100856A1/en not_active Ceased
- 2002-06-12 MX MXPA03011466A patent/MXPA03011466A/es active IP Right Grant
- 2002-06-12 EP EP02752056A patent/EP1404671B1/en not_active Expired - Lifetime
- 2002-06-12 JP JP2003503623A patent/JP2004534064A/ja active Pending
- 2002-06-12 DE DE60210614T patent/DE60210614T2/de not_active Expired - Fee Related
- 2002-06-12 US US10/171,182 patent/US6969709B2/en not_active Expired - Fee Related
- 2002-06-12 BR BR0210392-3A patent/BR0210392A/pt not_active IP Right Cessation
- 2002-06-12 ES ES02752056T patent/ES2261699T3/es not_active Expired - Lifetime
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2005
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Also Published As
| Publication number | Publication date |
|---|---|
| US7442691B2 (en) | 2008-10-28 |
| JP2004534064A (ja) | 2004-11-11 |
| CA2450202A1 (en) | 2002-12-19 |
| EP1404671B1 (en) | 2006-04-12 |
| US6969709B2 (en) | 2005-11-29 |
| WO2002100856A1 (en) | 2002-12-19 |
| US20030236199A1 (en) | 2003-12-25 |
| EP1404671A1 (en) | 2004-04-07 |
| DE60210614D1 (de) | 2006-05-24 |
| MXPA03011466A (es) | 2004-07-01 |
| DE60210614T2 (de) | 2007-03-01 |
| BR0210392A (pt) | 2004-10-13 |
| ATE323084T1 (de) | 2006-04-15 |
| US20060040910A1 (en) | 2006-02-23 |
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