JP2006520396A5 - - Google Patents
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- Publication number
- JP2006520396A5 JP2006520396A5 JP2006507955A JP2006507955A JP2006520396A5 JP 2006520396 A5 JP2006520396 A5 JP 2006520396A5 JP 2006507955 A JP2006507955 A JP 2006507955A JP 2006507955 A JP2006507955 A JP 2006507955A JP 2006520396 A5 JP2006520396 A5 JP 2006520396A5
- Authority
- JP
- Japan
- Prior art keywords
- difluorophenyl
- oxo
- alaninamide
- acetyl
- phenyl
- 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
- 125000004211 3,5-difluorophenyl group Chemical group [H]C1=C(F)C([H])=C(*)C([H])=C1F 0.000 claims 223
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 83
- 239000004305 biphenyl Substances 0.000 claims 67
- 125000000217 alkyl group Chemical group 0.000 claims 64
- 150000001875 compounds Chemical class 0.000 claims 44
- 229940067597 azelate Drugs 0.000 claims 34
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 24
- 229910052731 fluorine Inorganic materials 0.000 claims 20
- 229910052799 carbon Inorganic materials 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 125000004434 sulfur atom Chemical group 0.000 claims 16
- 125000003118 aryl group Chemical group 0.000 claims 15
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 14
- 125000001424 substituent group Chemical group 0.000 claims 14
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 13
- 238000006467 substitution reaction Methods 0.000 claims 13
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 229910052760 oxygen Inorganic materials 0.000 claims 10
- 239000001301 oxygen Substances 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 9
- SJRJJKPEHAURKC-UHFFFAOYSA-N N-Methylmorpholine Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 8
- 125000002877 alkyl aryl group Chemical group 0.000 claims 7
- 238000004519 manufacturing process Methods 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- LMDZBCPBFSXMTL-UHFFFAOYSA-N 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide Chemical compound CCN=C=NCCCN(C)C LMDZBCPBFSXMTL-UHFFFAOYSA-N 0.000 claims 6
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 6
- 125000004430 oxygen atom Chemical group O* 0.000 claims 6
- 125000000547 substituted alkyl group Chemical group 0.000 claims 5
- WMFFVAZKIWXNQV-LURJTMIESA-N (2s)-2-[[2-(3,5-difluorophenyl)acetyl]amino]propanoic acid Chemical compound OC(=O)[C@H](C)NC(=O)CC1=CC(F)=CC(F)=C1 WMFFVAZKIWXNQV-LURJTMIESA-N 0.000 claims 3
- 125000006704 (C5-C6) cycloalkyl group Chemical group 0.000 claims 3
- PJUPKRYGDFTMTM-UHFFFAOYSA-N 1-hydroxybenzotriazole;hydrate Chemical compound O.C1=CC=C2N(O)N=NC2=C1 PJUPKRYGDFTMTM-UHFFFAOYSA-N 0.000 claims 3
- LVZWSLJZHVFIQJ-UHFFFAOYSA-N Cyclopropane Chemical compound C1CC1 LVZWSLJZHVFIQJ-UHFFFAOYSA-N 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 2
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 230000006735 deficit Effects 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- ROYNDZUEBBTIQG-ZJZGAYNASA-N (2s)-2-[[(2s)-2-hydroxy-4-methylpentanoyl]amino]-n-[(2s,6s)-1-(2-methoxyethyl)-7-oxo-2-phenyl-5,6-dihydro-2h-azepin-6-yl]-4-methylpentanamide Chemical compound C1=CC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](O)CC(C)C)C(=O)N(CCOC)[C@@H]1C1=CC=CC=C1 ROYNDZUEBBTIQG-ZJZGAYNASA-N 0.000 claims 1
- OINBCZYUQFMXGD-RTFZILSDSA-N (2s)-2-[[2-(3,5-difluorophenyl)acetyl]amino]-n-[(2s,6s)-1-(2-methoxyethyl)-7-oxo-2-phenyl-5,6-dihydro-2h-azepin-6-yl]propanamide Chemical compound N([C@@H](C)C(=O)N[C@H]1CC=C[C@H](N(C1=O)CCOC)C=1C=CC=CC=1)C(=O)CC1=CC(F)=CC(F)=C1 OINBCZYUQFMXGD-RTFZILSDSA-N 0.000 claims 1
- YGDHLLBROMDVCA-MUEKUWCCSA-N (2s)-n-[(2s,6r)-1-cyclopentyl-7-oxo-2-phenyl-5,6-dihydro-2h-azepin-6-yl]-2-[[2-(3,5-difluorophenyl)acetyl]amino]propanamide Chemical compound N([C@@H](C)C(=O)N[C@H]1C(N(C2CCCC2)[C@@H](C=CC1)C=1C=CC=CC=1)=O)C(=O)CC1=CC(F)=CC(F)=C1 YGDHLLBROMDVCA-MUEKUWCCSA-N 0.000 claims 1
- BDHCSLPVYGSDBT-CQJMVLFOSA-N (2s)-n-[(2s,6s)-1-(cyclopropylmethyl)-2-(4-methoxyphenyl)-7-oxo-5,6-dihydro-2h-azepin-6-yl]-2-[[(2s)-2-hydroxy-4-methylpentanoyl]amino]-4-methylpentanamide Chemical compound C1=CC(OC)=CC=C1[C@H]1N(CC2CC2)C(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](O)CC(C)C)CC=C1 BDHCSLPVYGSDBT-CQJMVLFOSA-N 0.000 claims 1
- YGDHLLBROMDVCA-WDNCENIBSA-N (2s)-n-[(2s,6s)-1-cyclopentyl-7-oxo-2-phenyl-5,6-dihydro-2h-azepin-6-yl]-2-[[2-(3,5-difluorophenyl)acetyl]amino]propanamide Chemical compound N([C@@H](C)C(=O)N[C@@H]1C(N(C2CCCC2)[C@@H](C=CC1)C=1C=CC=CC=1)=O)C(=O)CC1=CC(F)=CC(F)=C1 YGDHLLBROMDVCA-WDNCENIBSA-N 0.000 claims 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000000044 Amnesia Diseases 0.000 claims 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 1
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 229940125373 Gamma-Secretase Inhibitor Drugs 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 230000007000 age related cognitive decline Effects 0.000 claims 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 239000003540 gamma secretase inhibitor Substances 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 230000006984 memory degeneration Effects 0.000 claims 1
- 208000023060 memory loss Diseases 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- NXJCBFBQEVOTOW-UHFFFAOYSA-L palladium(2+);dihydroxide Chemical compound O[Pd]O NXJCBFBQEVOTOW-UHFFFAOYSA-L 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 0 *C(C(N[C@@](C(*)C(*)=C(*)C(*)N1*)C1=O)=O)NC(*)=O Chemical compound *C(C(N[C@@](C(*)C(*)=C(*)C(*)N1*)C1=O)=O)NC(*)=O 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45510003P | 2003-03-14 | 2003-03-14 | |
| US45941603P | 2003-04-01 | 2003-04-01 | |
| PCT/SE2004/000350 WO2004080983A1 (en) | 2003-03-14 | 2004-03-10 | Novel lactams and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006520396A JP2006520396A (ja) | 2006-09-07 |
| JP2006520396A5 true JP2006520396A5 (https=) | 2007-05-10 |
Family
ID=32994582
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006507955A Pending JP2006520396A (ja) | 2003-03-14 | 2004-03-10 | 新規なラクタム及びその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US7342007B2 (https=) |
| EP (1) | EP1636196A1 (https=) |
| JP (1) | JP2006520396A (https=) |
| AR (1) | AR043612A1 (https=) |
| TW (1) | TW200504036A (https=) |
| WO (1) | WO2004080983A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200502221A (en) * | 2002-10-03 | 2005-01-16 | Astrazeneca Ab | Novel lactams and uses thereof |
| EP1768960A1 (en) * | 2004-07-13 | 2007-04-04 | F.Hoffmann-La Roche Ag | Sulfonamide derivatives |
| JP2008523141A (ja) * | 2004-12-14 | 2008-07-03 | アストラゼネカ・アクチエボラーグ | 新規の分子プローブ |
| WO2007104933A1 (en) * | 2006-03-10 | 2007-09-20 | Astrazeneca Ab | Chemical compounds |
| JP5385904B2 (ja) * | 2007-08-14 | 2014-01-08 | イーライ リリー アンド カンパニー | γ−セクレターゼ阻害剤 |
| WO2012017410A2 (en) * | 2010-08-04 | 2012-02-09 | Azuravax (Proprietary) Limited | A stress or strain monitoring system and a method of monitoring stress or strain |
| US10513515B2 (en) | 2017-08-25 | 2019-12-24 | Biotheryx, Inc. | Ether compounds and uses thereof |
| CA3106239A1 (en) | 2018-07-27 | 2020-01-30 | Biotheryx, Inc. | Bifunctional compounds as cdk modulators |
| WO2021222150A2 (en) | 2020-04-28 | 2021-11-04 | Anwita Biosciences, Inc. | Interleukin-2 polypeptides and fusion proteins thereof, and their pharmaceutical compositions and therapeutic applications |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH04503073A (ja) | 1989-01-31 | 1992-06-04 | アボツト・ラボラトリーズ | アナフィラトキシン受容体リガンド |
| US5936065A (en) * | 1993-12-06 | 1999-08-10 | Cytel Corporation | CS-1 peptidomimetics, compositions and methods of using the same |
| EP0900791A1 (en) * | 1995-12-27 | 1999-03-10 | Ono Pharmaceutical Co., Ltd. | Tetrazole derivatives and drugs containing the same as the active ingredient |
| GB9621836D0 (en) | 1996-10-19 | 1996-12-11 | Zeneca Ltd | Peptide compounds |
| HUP0001232A3 (en) | 1996-12-23 | 2001-02-28 | Elan Pharmaceuticals Inc San F | Cycloalkyl, lactam, lactone derivatives and their thio analogues inhibiting betha-amyloid peptide release and/or its synthesis and pharmaceutical compositions containing the compounds |
| WO1999067221A1 (en) * | 1998-06-22 | 1999-12-29 | Elan Pharmaceuticals, Inc. | Compounds for inhibiting beta-amyloid peptide release and/or its synthesis |
| WO2000002903A1 (en) | 1998-07-10 | 2000-01-20 | Cytel Corporation | Cs-1 peptidomimetics, compositions and methods of using the same |
| HRP990246A2 (en) * | 1998-08-07 | 2000-06-30 | Du Pont Pharm Co | Succinoylamino benzodiazepines as inhibitors of a beta protein production |
| AU2001243601A1 (en) | 2000-03-10 | 2001-09-24 | Ariad Pharmaceuticals, Inc. | Caprolactam derivatives and uses thereof |
| WO2001072324A1 (en) * | 2000-03-28 | 2001-10-04 | Bristol-Myers Squibb Pharma Company | Lactams as inhibitors of a-beta protein production |
| US6495540B2 (en) * | 2000-03-28 | 2002-12-17 | Bristol - Myers Squibb Pharma Company | Lactams as inhibitors of A-β protein production |
| TW200502221A (en) | 2002-10-03 | 2005-01-16 | Astrazeneca Ab | Novel lactams and uses thereof |
-
2004
- 2004-03-10 WO PCT/SE2004/000350 patent/WO2004080983A1/en not_active Ceased
- 2004-03-10 EP EP04719166A patent/EP1636196A1/en not_active Withdrawn
- 2004-03-10 JP JP2006507955A patent/JP2006520396A/ja active Pending
- 2004-03-10 US US10/549,271 patent/US7342007B2/en not_active Expired - Fee Related
- 2004-03-12 TW TW093106669A patent/TW200504036A/zh unknown
- 2004-03-15 AR ARP040100854A patent/AR043612A1/es unknown
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