JP2004534064A5 - - Google Patents
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- Publication number
- JP2004534064A5 JP2004534064A5 JP2003503623A JP2003503623A JP2004534064A5 JP 2004534064 A5 JP2004534064 A5 JP 2004534064A5 JP 2003503623 A JP2003503623 A JP 2003503623A JP 2003503623 A JP2003503623 A JP 2003503623A JP 2004534064 A5 JP2004534064 A5 JP 2004534064A5
- Authority
- JP
- Japan
- Prior art keywords
- ethyl
- alkyl
- optionally substituted
- diaza
- oxa
- 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.)
- Pending
Links
- -1 —OH Chemical group 0.000 claims 166
- 229910052736 halogen Inorganic materials 0.000 claims 69
- 150000002367 halogens Chemical class 0.000 claims 69
- 125000000753 cycloalkyl group Chemical group 0.000 claims 52
- 125000003118 aryl group Chemical group 0.000 claims 47
- 125000004663 dialkyl amino group Chemical group 0.000 claims 42
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 42
- 125000003545 alkoxy group Chemical group 0.000 claims 40
- 125000000217 alkyl group Chemical group 0.000 claims 40
- 150000001875 compounds Chemical class 0.000 claims 35
- 125000001072 heteroaryl group Chemical group 0.000 claims 30
- 229910052739 hydrogen Inorganic materials 0.000 claims 30
- 229910052799 carbon Inorganic materials 0.000 claims 29
- 125000000623 heterocyclic group Chemical group 0.000 claims 26
- 125000000304 alkynyl group Chemical group 0.000 claims 24
- 239000001257 hydrogen Substances 0.000 claims 20
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 15
- 125000003275 alpha amino acid group Chemical group 0.000 claims 15
- 125000002837 carbocyclic group Chemical group 0.000 claims 10
- 229910052760 oxygen Inorganic materials 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 208000024827 Alzheimer disease Diseases 0.000 claims 6
- 125000004429 atom Chemical group 0.000 claims 6
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 6
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 6
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 150000001721 carbon Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 208000010877 cognitive disease Diseases 0.000 claims 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 208000027061 mild cognitive impairment Diseases 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 150000002431 hydrogen Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 2
- 206010012289 Dementia Diseases 0.000 claims 2
- 201000010374 Down Syndrome Diseases 0.000 claims 2
- 125000002877 alkyl aryl group Chemical group 0.000 claims 2
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 2
- 210000004556 brain Anatomy 0.000 claims 2
- 230000003412 degenerative effect Effects 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 210000004558 lewy body Anatomy 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 208000019553 vascular disease Diseases 0.000 claims 2
- XSTLZQUIZYEJPU-UHFFFAOYSA-N 3-[2-[(3-ethylphenyl)methylamino]-1-hydroxyethyl]-16-fluoro-13-oxa-4,7-diazabicyclo[12.3.1]octadeca-1(18),14,16-triene-5,8-dione Chemical compound CCC1=CC=CC(CNCC(O)C2NC(=O)CNC(=O)CCCCOC=3C=C(F)C=C(C=3)C2)=C1 XSTLZQUIZYEJPU-UHFFFAOYSA-N 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 150000002366 halogen compounds Chemical class 0.000 claims 1
- 239000007943 implant Substances 0.000 claims 1
- 238000007913 intrathecal administration Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 0 CNC(C(C(CBO*C(N(C)C1*)=O)NC1=O)O)=* Chemical compound CNC(C(C(CBO*C(N(C)C1*)=O)NC1=O)O)=* 0.000 description 3
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29754601P | 2001-06-12 | 2001-06-12 | |
| US33308301P | 2001-11-19 | 2001-11-19 | |
| PCT/US2002/019076 WO2002100856A1 (en) | 2001-06-12 | 2002-06-12 | Macrocycles useful in the treatment of alzheimer's disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004534064A JP2004534064A (ja) | 2004-11-11 |
| JP2004534064A5 true JP2004534064A5 (enExample) | 2006-01-05 |
Family
ID=26970209
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003503623A Pending JP2004534064A (ja) | 2001-06-12 | 2002-06-12 | アルツハイマー病の治療に有用な大環状分子 |
Country Status (10)
| 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) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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
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