JP2009544597A5 - - Google Patents
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- Publication number
- JP2009544597A5 JP2009544597A5 JP2009519989A JP2009519989A JP2009544597A5 JP 2009544597 A5 JP2009544597 A5 JP 2009544597A5 JP 2009519989 A JP2009519989 A JP 2009519989A JP 2009519989 A JP2009519989 A JP 2009519989A JP 2009544597 A5 JP2009544597 A5 JP 2009544597A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- tetrahydro
- dioxo
- cycloalkyl
- lambda
- 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- Withdrawn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
- 150000001875 compounds Chemical class 0.000 claims description 24
- 239000002253 acid Substances 0.000 claims description 12
- 239000012458 free base Substances 0.000 claims description 12
- 229910052739 hydrogen Inorganic materials 0.000 claims description 12
- 239000001257 hydrogen Substances 0.000 claims description 12
- 150000003839 salts Chemical group 0.000 claims description 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 7
- 229910052799 carbon Inorganic materials 0.000 claims description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 6
- 238000002360 preparation method Methods 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 3
- 239000002243 precursor Substances 0.000 claims description 3
- 239000003054 catalyst Substances 0.000 claims description 2
- 238000003776 cleavage reaction Methods 0.000 claims description 2
- 238000007306 functionalization reaction Methods 0.000 claims description 2
- 238000005649 metathesis reaction Methods 0.000 claims description 2
- 230000003647 oxidation Effects 0.000 claims description 2
- 238000007254 oxidation reaction Methods 0.000 claims description 2
- 125000006239 protecting group Chemical group 0.000 claims description 2
- 238000007363 ring formation reaction Methods 0.000 claims description 2
- 230000007017 scission Effects 0.000 claims description 2
- -1 chroman-4-yl Chemical group 0.000 claims 35
- 125000000217 alkyl group Chemical group 0.000 claims 29
- 125000000753 cycloalkyl group Chemical group 0.000 claims 19
- 125000003118 aryl group Chemical group 0.000 claims 14
- 125000001072 heteroaryl group Chemical group 0.000 claims 14
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 4
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 4
- 208000012902 Nervous system disease Diseases 0.000 claims 4
- 208000025966 Neurological disease Diseases 0.000 claims 4
- 238000004220 aggregation Methods 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 230000000926 neurological effect Effects 0.000 claims 4
- 208000019553 vascular disease Diseases 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 230000006933 amyloid-beta aggregation Effects 0.000 claims 3
- 230000003941 amyloidogenesis Effects 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 2
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 239000008186 active pharmaceutical agent Substances 0.000 claims 1
- 230000002776 aggregation Effects 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000005085 alkoxycarbonylalkoxy group Chemical group 0.000 claims 1
- 125000005194 alkoxycarbonyloxy group Chemical group 0.000 claims 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 1
- 125000005237 alkyleneamino group Chemical group 0.000 claims 1
- 125000005529 alkyleneoxy group Chemical group 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229940088679 drug related substance Drugs 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000008024 pharmaceutical diluent Substances 0.000 claims 1
- 125000006413 ring segment Chemical group 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- ZOKXTWBITQBERF-UHFFFAOYSA-N Molybdenum Chemical compound [Mo] ZOKXTWBITQBERF-UHFFFAOYSA-N 0.000 description 1
- KJTLSVCANCCWHF-UHFFFAOYSA-N Ruthenium Chemical compound [Ru] KJTLSVCANCCWHF-UHFFFAOYSA-N 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 229910052750 molybdenum Inorganic materials 0.000 description 1
- 239000011733 molybdenum Substances 0.000 description 1
- 229910052707 ruthenium Inorganic materials 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- WFKWXMTUELFFGS-UHFFFAOYSA-N tungsten Chemical compound [W] WFKWXMTUELFFGS-UHFFFAOYSA-N 0.000 description 1
- 229910052721 tungsten Inorganic materials 0.000 description 1
- 239000010937 tungsten Substances 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06117583 | 2006-07-20 | ||
| PCT/EP2007/057492 WO2008009734A1 (en) | 2006-07-20 | 2007-07-19 | Macrocyclic lactams |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009544597A JP2009544597A (ja) | 2009-12-17 |
| JP2009544597A5 true JP2009544597A5 (enExample) | 2010-09-02 |
Family
ID=37451237
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009519989A Withdrawn JP2009544597A (ja) | 2006-07-20 | 2007-07-19 | 大環状ラクタム |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20090170878A1 (enExample) |
| EP (1) | EP2046760A1 (enExample) |
| JP (1) | JP2009544597A (enExample) |
| KR (1) | KR20090041387A (enExample) |
| CN (1) | CN101484431A (enExample) |
| AU (1) | AU2007275132A1 (enExample) |
| BR (1) | BRPI0715437A2 (enExample) |
| CA (1) | CA2656869A1 (enExample) |
| MX (1) | MX2009000768A (enExample) |
| RU (1) | RU2009105764A (enExample) |
| WO (1) | WO2008009734A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0325830D0 (en) * | 2003-11-05 | 2003-12-10 | Novartis Ag | Organic compounds |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| EP1851208A1 (en) * | 2005-01-13 | 2007-11-07 | Novartis AG | Macrocyclic compounds useful as bace inhibitors |
| GB0500683D0 (en) * | 2005-01-13 | 2005-02-23 | Novartis Ag | Organic compounds |
| GB0526614D0 (en) | 2005-12-30 | 2006-02-08 | Novartis Ag | Organic compounds |
| MX2009000710A (es) * | 2006-07-20 | 2009-01-30 | Novartis Ag | Compuestos macrociclicos utiles como inhibidores de bace. |
| CN104995176B (zh) | 2013-02-12 | 2019-02-22 | 巴克老龄化研究所 | 调节bace所介导的app加工的乙内酰脲 |
| WO2019075259A1 (en) * | 2017-10-11 | 2019-04-18 | Cornell University | MACROCYCLIC COMPOUNDS AS PROTEASE INHIBITORS |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2450167A1 (en) * | 2001-06-12 | 2002-12-19 | Elan Pharmaceuticals, Inc. | Macrocycles useful in the treatment of alzheimer's disease |
| MXPA03011466A (es) * | 2001-06-12 | 2004-07-01 | Elan Pharm Inc | Macrociclos utiles en tratamiento de enfermedades de alzheimer. |
| GB0325830D0 (en) * | 2003-11-05 | 2003-12-10 | Novartis Ag | Organic compounds |
| AR050184A1 (es) * | 2004-07-28 | 2006-10-04 | Schering Corp | Inhibidores macrociclicos de beta-secretasa |
| EP1851208A1 (en) * | 2005-01-13 | 2007-11-07 | Novartis AG | Macrocyclic compounds useful as bace inhibitors |
| GB0500683D0 (en) * | 2005-01-13 | 2005-02-23 | Novartis Ag | Organic compounds |
| GB0526614D0 (en) * | 2005-12-30 | 2006-02-08 | Novartis Ag | Organic compounds |
| MX2009000710A (es) * | 2006-07-20 | 2009-01-30 | Novartis Ag | Compuestos macrociclicos utiles como inhibidores de bace. |
-
2007
- 2007-07-19 CN CNA2007800255206A patent/CN101484431A/zh active Pending
- 2007-07-19 US US12/374,469 patent/US20090170878A1/en not_active Abandoned
- 2007-07-19 CA CA002656869A patent/CA2656869A1/en not_active Abandoned
- 2007-07-19 EP EP07819907A patent/EP2046760A1/en not_active Withdrawn
- 2007-07-19 JP JP2009519989A patent/JP2009544597A/ja not_active Withdrawn
- 2007-07-19 WO PCT/EP2007/057492 patent/WO2008009734A1/en not_active Ceased
- 2007-07-19 KR KR1020097001068A patent/KR20090041387A/ko not_active Withdrawn
- 2007-07-19 AU AU2007275132A patent/AU2007275132A1/en not_active Abandoned
- 2007-07-19 RU RU2009105764/04A patent/RU2009105764A/ru not_active Application Discontinuation
- 2007-07-19 MX MX2009000768A patent/MX2009000768A/es unknown
- 2007-07-19 BR BRPI0715437-2A patent/BRPI0715437A2/pt not_active Application Discontinuation
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