JP2007513913A5 - - Google Patents
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- Publication number
- JP2007513913A5 JP2007513913A5 JP2006543488A JP2006543488A JP2007513913A5 JP 2007513913 A5 JP2007513913 A5 JP 2007513913A5 JP 2006543488 A JP2006543488 A JP 2006543488A JP 2006543488 A JP2006543488 A JP 2006543488A JP 2007513913 A5 JP2007513913 A5 JP 2007513913A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- hydroxy
- propyl
- phenylmethyl
- tetrahydro
- 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.)
- Withdrawn
Links
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 88
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 87
- VGPKJZKKCPUOEF-UHFFFAOYSA-N 10,10-dioxo-10lambda6-thia-3,9-diazatricyclo[6.4.1.04,13]trideca-1(13),2,4,6,8,11-hexaene-6-carboxamide Chemical compound N=1S(C=CC=2C=NC3=CC(=CC1C23)C(=O)N)(=O)=O VGPKJZKKCPUOEF-UHFFFAOYSA-N 0.000 claims 79
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 61
- -1 cyano, hydroxy Chemical group 0.000 claims 47
- 125000000217 alkyl group Chemical group 0.000 claims 41
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 11
- 125000002877 alkyl aryl group Chemical group 0.000 claims 11
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 125000000304 alkynyl group Chemical group 0.000 claims 6
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 125000004367 cycloalkylaryl group Chemical group 0.000 claims 5
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 4
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 125000005215 cycloalkylheteroaryl group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 208000037259 Amyloid Plaque Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- TYABZJINIKXMCL-LBNVMWSVSA-N 1,6-diethyl-n-[(1s,2r)-2-hydroxy-1-(phenylmethyl)-3-(tetrahydro-2h-pyran-4-ylamino)propyl]-1,3,4,6-tetrahydro[1,2]thiazepino[5,4,3-cd]indole-8-carboxamide 2,2-dioxide Chemical compound C([C@H](NC(=O)C=1C=C2N(S(CCC3=CN(CC)C(=C23)C=1)(=O)=O)CC)[C@H](O)CNC1CCOCC1)C1=CC=CC=C1 TYABZJINIKXMCL-LBNVMWSVSA-N 0.000 claims 1
- CYWIMYQJZNCIBU-LBNVMWSVSA-N 1,6-diethyl-n-[(1s,2r)-2-hydroxy-1-(phenylmethyl)-3-(tetrahydro-2h-pyran-4-ylamino)propyl]-1,6-dihydro[1,2]thiazepino[5,4,3-cd]indole-8-carboxamide 2,2-dioxide Chemical compound C([C@H](NC(=O)C=1C=C2N(S(C=CC3=CN(CC)C(=C23)C=1)(=O)=O)CC)[C@H](O)CNC1CCOCC1)C1=CC=CC=C1 CYWIMYQJZNCIBU-LBNVMWSVSA-N 0.000 claims 1
- 125000006433 1-ethyl cyclopropyl group Chemical group [H]C([H])([H])C([H])([H])C1(*)C([H])([H])C1([H])[H] 0.000 claims 1
- HNEGJTWNOOWEMH-UHFFFAOYSA-N 1-fluoropropane Chemical group [CH2]CCF HNEGJTWNOOWEMH-UHFFFAOYSA-N 0.000 claims 1
- 125000006432 1-methyl cyclopropyl group Chemical group [H]C([H])([H])C1(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- 125000004778 2,2-difluoroethyl group Chemical group [H]C([H])(*)C([H])(F)F 0.000 claims 1
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000006176 2-ethylbutyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(C([H])([H])*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000004777 2-fluoroethyl group Chemical group [H]C([H])(F)C([H])([H])* 0.000 claims 1
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 1
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000006309 butyl amino group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 125000006311 cyclobutyl amino group Chemical group [H]N(*)C1([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000006317 cyclopropyl amino group Chemical group 0.000 claims 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 125000000031 ethylamino group Chemical group [H]C([H])([H])C([H])([H])N([H])[*] 0.000 claims 1
- 125000004705 ethylthio group Chemical group C(C)S* 0.000 claims 1
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000000040 m-tolyl group Chemical group [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000003261 o-tolyl group Chemical group [H]C1=C([H])C(*)=C(C([H])=C1[H])C([H])([H])[H] 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- 125000006308 propyl amino group Chemical group 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0328900.6A GB0328900D0 (en) | 2003-12-12 | 2003-12-12 | Novel compounds |
| PCT/EP2004/014076 WO2005058915A1 (en) | 2003-12-12 | 2004-12-09 | Tricyclic indole hydroxyethylamine derivatives and their use in the treatment of alzheimer's disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007513913A JP2007513913A (ja) | 2007-05-31 |
| JP2007513913A5 true JP2007513913A5 (https=) | 2008-01-17 |
Family
ID=30130158
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006543488A Withdrawn JP2007513913A (ja) | 2003-12-12 | 2004-12-09 | 三環式インドールヒドロキシエチルアミン誘導体およびアルツハイマー病の治療におけるそれらの使用 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US20070073060A1 (https=) |
| EP (1) | EP1692143B1 (https=) |
| JP (1) | JP2007513913A (https=) |
| KR (1) | KR20060121164A (https=) |
| CN (1) | CN1914214A (https=) |
| AT (1) | ATE414090T1 (https=) |
| AU (1) | AU2004299231A1 (https=) |
| BR (1) | BRPI0417476A (https=) |
| CA (1) | CA2549072A1 (https=) |
| DE (1) | DE602004017777D1 (https=) |
| GB (1) | GB0328900D0 (https=) |
| IL (1) | IL175819A0 (https=) |
| IS (1) | IS8521A (https=) |
| MA (1) | MA28241A1 (https=) |
| NO (1) | NO20063137L (https=) |
| RU (1) | RU2006124863A (https=) |
| WO (1) | WO2005058915A1 (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050239836A1 (en) | 2004-03-09 | 2005-10-27 | Varghese John | Substituted hydroxyethylamine aspartyl protease inhibitors |
| EP1773756A2 (en) | 2004-07-09 | 2007-04-18 | Elan Pharmaceuticals, Inc. | Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors |
| BRPI0515383A (pt) * | 2004-09-21 | 2008-07-22 | Pfizer Prod Inc | n-etil hidroxietilamina útil no tratamento de condições do snc |
| GB0422765D0 (en) * | 2004-10-13 | 2004-11-17 | Glaxo Group Ltd | Novel compounds |
| GB0422766D0 (en) * | 2004-10-13 | 2004-11-17 | Glaxo Group Ltd | Novel compounds |
| WO2007047305A1 (en) * | 2005-10-12 | 2007-04-26 | Elan Pharmaceuticals, Inc. | Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors |
| US7872009B2 (en) | 2005-11-21 | 2011-01-18 | Amgen Inc. | Beta-Secretase modulators and methods of use |
| US7838676B2 (en) * | 2005-11-21 | 2010-11-23 | Amgen Inc. | Beta-secretase modulators and methods of use |
| PT2185561E (pt) * | 2007-07-27 | 2011-09-07 | Sanofi Aventis | Derivados de 1,2,3,4-tetra-hidropirrolo(1,2-a)pirazina-6- carboxamidas e de 2,3,4,5-tetra-hidropirrolo(1,2-a)-diazepina-7- carboxamidas, sua preparação e sua aplicação em terapia |
| FR2919289B1 (fr) * | 2007-07-27 | 2009-09-04 | Sanofi Aventis Sa | Derives de 2,3,4,5-tetrahydropyrrolo[1,2-a][1,4]- diazepine-7-carboxamides, leur preparation et leur application en therapeutique. |
| FR2919288B1 (fr) * | 2007-07-27 | 2009-09-04 | Sanofi Aventis Sa | Derives de 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-6- carboxamides, leur preparation et leur application en therapeutique. |
| FR2919286A1 (fr) | 2007-07-27 | 2009-01-30 | Sanofi Aventis Sa | Derives de derives de 1-oxo-1,2-dihydroisoquinoleine-5- carboxamides et de 4-oxo-3,4-dihydroquinazoline-8- carboxamides,leur preparation et leur application en therapeutique. |
| FR2919285B1 (fr) | 2007-07-27 | 2012-08-31 | Sanofi Aventis | Derives de 1-oxo-isoindoline-4-carboxamides et de 1-oxo- 1,2,3,4-tetrahydroisoquinoleine-5-carboxamides, leur preparation et leur application en therapeutique. |
| EP2310019A4 (en) * | 2008-05-29 | 2011-06-01 | Albany Molecular Res Inc | 5-HT3 RECEPTOR MODULATORS, MANUFACTURING METHOD AND ITS USE |
| FR2960876B1 (fr) | 2010-06-03 | 2012-07-27 | Sanofi Aventis | Derives de 3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1h)-dicarboxamide leur preparation et leur application en therapeutique. |
| AU2011261375B2 (en) | 2010-06-04 | 2016-09-22 | Albany Molecular Research, Inc. | Glycine transporter-1 inhibitors, methods of making them, and uses thereof |
| CN104768949A (zh) * | 2012-08-24 | 2015-07-08 | 特温蒂斯公司 | 苯并呋咱抗淀粉样蛋白化合物和方法 |
| US12043631B2 (en) | 2017-10-13 | 2024-07-23 | Purdue Research Foundation | BACE1 inhibitors for the treatment of Alzheimer's disease |
| WO2019075358A1 (en) * | 2017-10-13 | 2019-04-18 | Ghosh Arun K | BACE1 INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2280096A1 (en) * | 1997-02-04 | 1998-08-06 | The Regents Of The University Of California | Nanomolar, non-peptide inhibitors of cathepsin d |
| US6207664B1 (en) * | 1998-11-25 | 2001-03-27 | Pfizer Inc. | Squalene synthetase inhibitor agents |
| DE60124080T2 (de) * | 2000-03-23 | 2007-03-01 | Elan Pharmaceuticals, Inc., San Francisco | Verbindungen und verfahren zur behandlung der alzheimerschen krankheit |
| EP1299352B1 (en) * | 2000-06-30 | 2005-12-28 | Elan Pharmaceuticals, Inc. | Compounds to treat alzheimer's disease |
| NZ533107A (en) * | 2001-11-08 | 2007-04-27 | Upjohn Co | N, N'-substituted-1,3-diamino-2-hydroxypropane derivatives |
| GB0228410D0 (en) * | 2002-12-05 | 2003-01-08 | Glaxo Group Ltd | Novel Compounds |
| GB0309221D0 (en) * | 2003-04-23 | 2003-06-04 | Glaxo Group Ltd | Novel compounds |
-
2003
- 2003-12-12 GB GBGB0328900.6A patent/GB0328900D0/en not_active Ceased
-
2004
- 2004-12-09 DE DE602004017777T patent/DE602004017777D1/de not_active Expired - Fee Related
- 2004-12-09 EP EP04803724A patent/EP1692143B1/en not_active Expired - Lifetime
- 2004-12-09 AT AT04803724T patent/ATE414090T1/de not_active IP Right Cessation
- 2004-12-09 JP JP2006543488A patent/JP2007513913A/ja not_active Withdrawn
- 2004-12-09 US US10/596,296 patent/US20070073060A1/en not_active Abandoned
- 2004-12-09 CA CA002549072A patent/CA2549072A1/en not_active Abandoned
- 2004-12-09 AU AU2004299231A patent/AU2004299231A1/en not_active Abandoned
- 2004-12-09 RU RU2006124863/04A patent/RU2006124863A/ru not_active Application Discontinuation
- 2004-12-09 BR BRPI0417476-3A patent/BRPI0417476A/pt not_active IP Right Cessation
- 2004-12-09 WO PCT/EP2004/014076 patent/WO2005058915A1/en not_active Ceased
- 2004-12-09 CN CNA2004800416435A patent/CN1914214A/zh active Pending
- 2004-12-09 KR KR1020067011376A patent/KR20060121164A/ko not_active Withdrawn
-
2006
- 2006-05-22 IL IL175819A patent/IL175819A0/en unknown
- 2006-06-26 MA MA29143A patent/MA28241A1/fr unknown
- 2006-06-26 IS IS8521A patent/IS8521A/xx unknown
- 2006-07-06 NO NO20063137A patent/NO20063137L/no not_active Application Discontinuation
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