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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- 210000003061 neural cell Anatomy 0.000 description 1
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- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 description 1
- XKJCHHZQLQNZHY-UHFFFAOYSA-N phthalimide Chemical compound C1=CC=C2C(=O)NC(=O)C2=C1 XKJCHHZQLQNZHY-UHFFFAOYSA-N 0.000 description 1
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- 125000003386 piperidinyl group Chemical group 0.000 description 1
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- 239000004626 polylactic acid Substances 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- 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
- 230000002335 preservative effect Effects 0.000 description 1
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- 229960003387 progesterone Drugs 0.000 description 1
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- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 230000017854 proteolysis Effects 0.000 description 1
- 230000002797 proteolythic effect Effects 0.000 description 1
- 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
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 125000001422 pyrrolinyl group Chemical group 0.000 description 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 description 1
- 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
- 238000012552 review Methods 0.000 description 1
- 238000007142 ring opening reaction Methods 0.000 description 1
- 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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- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 229940081974 saccharin Drugs 0.000 description 1
- 235000019204 saccharin Nutrition 0.000 description 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 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
- 238000011895 specific detection Methods 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
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- 208000011580 syndromic disease Diseases 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 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
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 description 1
- 125000005329 tetralinyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
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- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
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- 125000001544 thienyl group Chemical group 0.000 description 1
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- 125000001425 triazolyl group Chemical group 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 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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- IHOVFYSQUDPMCN-QKUIIBHLSA-N zosuquidar Chemical compound C([C@H](COC=1C2=CC=CN=C2C=CC=1)O)N(CC1)CCN1C1C2=CC=CC=C2C2C(F)(F)C2C2=CC=CC=C12 IHOVFYSQUDPMCN-QKUIIBHLSA-N 0.000 description 1
- 125000004933 β-carbolinyl group Chemical group C1(=NC=CC=2C3=CC=CC=C3NC12)* 0.000 description 1
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)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (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)
| Publication Number | Publication Date |
|---|---|
| ES2261699T3 true ES2261699T3 (es) | 2006-11-16 |
Family
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Family Applications (1)
| 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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| Country | Link |
|---|---|
| US (2) | US6969709B2 (enExample) |
| 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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| US7312360B2 (en) | 2001-12-06 | 2007-12-25 | Elan Pharmaceuticals, Inc. | Substituted hydroxyethylamines |
| JP4673833B2 (ja) | 2003-01-07 | 2011-04-20 | メルク・シャープ・エンド・ドーム・コーポレイション | アルツハイマー病の治療用大環状β−セクレターゼ阻害剤 |
| 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 |
| ES2306200T3 (es) * | 2004-07-28 | 2008-11-01 | Schering Corporation | Inhibidores macrociclicos de beta-secretasa. |
| 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 |
| WO2007021793A1 (en) * | 2005-08-12 | 2007-02-22 | Bristol-Myers Squibb Company | Macrocyclic diaminopropanes as beta-secretase inhibitors |
| GB0526614D0 (en) | 2005-12-30 | 2006-02-08 | Novartis Ag | Organic compounds |
| RU2009105764A (ru) * | 2006-07-20 | 2010-08-27 | Новартис АГ (CH) | Макроциклические соединения, применимые в качестве ингибиторов васе |
| CN101490018A (zh) * | 2006-07-20 | 2009-07-22 | 诺瓦提斯公司 | 用作bace抑制剂的大环化合物 |
| 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 |
| EP2139876A4 (en) * | 2007-03-26 | 2011-07-20 | Merck Canada Inc | Cathepsin cysteine protease inhibitor |
| US7732434B2 (en) | 2007-04-20 | 2010-06-08 | Bristol-Myers Squibb Company | Macrocyclic acyl guanidines as beta-secretase inhibitors |
| US20160022649A1 (en) * | 2013-03-15 | 2016-01-28 | The Board Of Regents Of The University Of Texas System | Use of inhibitors of mtor to improve vascular functions in apoe4 carriers |
| EP3089737B1 (en) | 2013-12-31 | 2021-11-03 | Rapamycin Holdings, LLC | Oral rapamycin nanoparticle preparations and use |
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| AUPM982594A0 (en) * | 1994-12-02 | 1995-01-05 | University Of Queensland, The | HIV protease inhibitors |
| CA2376420A1 (en) * | 1999-06-15 | 2000-12-21 | Elan Pharmaceuticals, Inc. | Statine-derived tetrapeptide inhibitors of beta-secretase |
-
2002
- 2002-06-12 BR BR0210392-3A patent/BR0210392A/pt not_active IP Right Cessation
- 2002-06-12 JP JP2003503623A patent/JP2004534064A/ja active Pending
- 2002-06-12 MX MXPA03011466A patent/MXPA03011466A/es active IP Right Grant
- 2002-06-12 AT AT02752056T patent/ATE323084T1/de not_active IP Right Cessation
- 2002-06-12 EP EP02752056A patent/EP1404671B1/en not_active Expired - Lifetime
- 2002-06-12 CA CA002450202A patent/CA2450202A1/en not_active Abandoned
- 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 ES ES02752056T patent/ES2261699T3/es not_active Expired - Lifetime
- 2002-06-12 WO PCT/US2002/019076 patent/WO2002100856A1/en not_active Ceased
-
2005
- 2005-09-02 US US11/218,879 patent/US7442691B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| ATE323084T1 (de) | 2006-04-15 |
| DE60210614D1 (de) | 2006-05-24 |
| EP1404671A1 (en) | 2004-04-07 |
| JP2004534064A (ja) | 2004-11-11 |
| WO2002100856A1 (en) | 2002-12-19 |
| US7442691B2 (en) | 2008-10-28 |
| US20060040910A1 (en) | 2006-02-23 |
| EP1404671B1 (en) | 2006-04-12 |
| DE60210614T2 (de) | 2007-03-01 |
| BR0210392A (pt) | 2004-10-13 |
| MXPA03011466A (es) | 2004-07-01 |
| US20030236199A1 (en) | 2003-12-25 |
| US6969709B2 (en) | 2005-11-29 |
| CA2450202A1 (en) | 2002-12-19 |
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