JP2009504613A5 - - Google Patents
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- Publication number
- JP2009504613A5 JP2009504613A5 JP2008525577A JP2008525577A JP2009504613A5 JP 2009504613 A5 JP2009504613 A5 JP 2009504613A5 JP 2008525577 A JP2008525577 A JP 2008525577A JP 2008525577 A JP2008525577 A JP 2008525577A JP 2009504613 A5 JP2009504613 A5 JP 2009504613A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- aryl
- heteroaryl
- heterocyclyl
- 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
- 229910052731 fluorine Inorganic materials 0.000 claims 41
- 229910052799 carbon Inorganic materials 0.000 claims 38
- -1 diastereomers Chemical class 0.000 claims 38
- 125000001072 heteroaryl group Chemical group 0.000 claims 38
- 239000011737 fluorine Substances 0.000 claims 37
- 125000000623 heterocyclic group Chemical group 0.000 claims 37
- 125000003118 aryl group Chemical group 0.000 claims 35
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 34
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 29
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 29
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 29
- 229910052794 bromium Inorganic materials 0.000 claims 29
- 229910052801 chlorine Inorganic materials 0.000 claims 29
- 239000000460 chlorine Substances 0.000 claims 29
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 27
- 125000004093 cyano group Chemical group *C#N 0.000 claims 25
- 150000001875 compounds Chemical class 0.000 claims 24
- 229910052739 hydrogen Inorganic materials 0.000 claims 23
- 239000001257 hydrogen Substances 0.000 claims 23
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 22
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 19
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 19
- 150000002431 hydrogen Chemical class 0.000 claims 18
- 125000004043 oxo group Chemical group O=* 0.000 claims 15
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000001153 fluoro group Chemical group F* 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000004434 sulfur atom Chemical group 0.000 claims 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 239000000556 agonist Substances 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 claims 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 claims 2
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 claims 2
- 101710137189 Amyloid-beta A4 protein Proteins 0.000 claims 2
- 101710151993 Amyloid-beta precursor protein Proteins 0.000 claims 2
- 102100022704 Amyloid-beta precursor protein Human genes 0.000 claims 2
- DZHSAHHDTRWUTF-SIQRNXPUSA-N amyloid-beta polypeptide 42 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(C)C)C1=CC=CC=C1 DZHSAHHDTRWUTF-SIQRNXPUSA-N 0.000 claims 2
- 239000002439 beta secretase inhibitor Substances 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 230000003551 muscarinic effect Effects 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- MGRVRXRGTBOSHW-UHFFFAOYSA-N (aminomethyl)phosphonic acid Chemical compound NCP(O)(O)=O MGRVRXRGTBOSHW-UHFFFAOYSA-N 0.000 claims 1
- 229940124801 5-HT6 antagonist Drugs 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 229940082496 Adrenoreceptor antagonist Drugs 0.000 claims 1
- 229940124638 COX inhibitor Drugs 0.000 claims 1
- 102000018997 Growth Hormone Human genes 0.000 claims 1
- 108010051696 Growth Hormone Proteins 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 1
- 229940127523 NMDA Receptor Antagonists Drugs 0.000 claims 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 238000004220 aggregation Methods 0.000 claims 1
- 230000002776 aggregation Effects 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000006933 amyloid-beta aggregation Effects 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 229940088710 antibiotic agent Drugs 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000000544 cholinesterase inhibitor Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 229960003692 gamma aminobutyric acid Drugs 0.000 claims 1
- 239000003540 gamma secretase inhibitor Substances 0.000 claims 1
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims 1
- 229930195712 glutamate Natural products 0.000 claims 1
- 239000000122 growth hormone Substances 0.000 claims 1
- 239000003395 histamine H3 receptor antagonist Substances 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000001067 neuroprotector Effects 0.000 claims 1
- 239000002858 neurotransmitter agent Substances 0.000 claims 1
- 239000000181 nicotinic agonist Substances 0.000 claims 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 1
- 239000004031 partial agonist Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims 1
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 150000003254 radicals Chemical class 0.000 claims 1
- 229940044551 receptor antagonist Drugs 0.000 claims 1
- 239000002464 receptor antagonist Substances 0.000 claims 1
- 239000002469 receptor inverse agonist Substances 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 230000028327 secretion Effects 0.000 claims 1
- 239000000387 serotonin 5-HT4 receptor agonist Substances 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05017478 | 2005-08-11 | ||
| PCT/EP2006/065155 WO2007017510A2 (de) | 2005-08-11 | 2006-08-08 | Isophthalsäurediamide zur behandlung der alzheimer erkrankung |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009504613A JP2009504613A (ja) | 2009-02-05 |
| JP2009504613A5 true JP2009504613A5 (OSRAM) | 2009-09-24 |
Family
ID=35615569
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008525577A Pending JP2009504613A (ja) | 2005-08-11 | 2006-08-08 | アルツハイマー病の治療用化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20100168070A1 (OSRAM) |
| EP (1) | EP1915353A2 (OSRAM) |
| JP (1) | JP2009504613A (OSRAM) |
| CA (1) | CA2618474A1 (OSRAM) |
| WO (1) | WO2007017510A2 (OSRAM) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| NZ562314A (en) | 2005-04-08 | 2010-02-26 | Comentis Inc | Compounds which inhibit beta-secretase activity and methods of use thereof |
| JP2009504614A (ja) * | 2005-08-11 | 2009-02-05 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | アルツハイマー病の治療用化合物 |
| US8329897B2 (en) * | 2007-07-26 | 2012-12-11 | Vitae Pharmaceuticals, Inc. | Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 |
| CN101981003B (zh) * | 2008-02-29 | 2014-07-02 | 伊沃泰克股份公司 | 酰胺化合物、组合物及其应用 |
| JP5608655B2 (ja) | 2008-09-18 | 2014-10-15 | エヴォテック アーゲー | Ｐ２ｘ３受容体活性のモジュレーター |
| US9000047B2 (en) | 2010-05-24 | 2015-04-07 | Farmalider, S.A. | Compound inhibiting activation of the enzyme Erk 1/2 to be used in the treatment of neurodegenerative illnesses |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1991019810A1 (en) * | 1990-06-15 | 1991-12-26 | California Biotechnology Inc. | Transgenic non-human mammal displaying the amyloid-forming pathology of alzheimer's disease |
| CA2372251A1 (en) * | 1991-01-21 | 1992-08-06 | Michael John Mullan | Test and model for alzheimer's disease |
| JPH07506720A (ja) * | 1992-01-07 | 1995-07-27 | アテナ ニューロサイエンシーズ， インコーポレイテッド | アルツハイマー病のトランスジェニック動物モデル |
| US5604102A (en) * | 1992-04-15 | 1997-02-18 | Athena Neurosciences, Inc. | Methods of screening for β-amyloid peptide production inhibitors |
| JPH09507746A (ja) * | 1993-10-27 | 1997-08-12 | アテナ ニューロサイエンシズ，インコーポレイティド | Ｓｗｅｄｉｓｈ変異を有するＡＰＰ対立遺伝子を含有するトランスジェニック動物 |
| US5877399A (en) * | 1994-01-27 | 1999-03-02 | Johns Hopkins University | Transgenic mice expressing APP-Swedish mutation develop progressive neurologic disease |
| AU6383396A (en) * | 1995-06-07 | 1996-12-30 | Athena Neurosciences, Inc. | Beta-secretase, antibodies to beta-secretase, and assays for detecting beta-secretase inhibition |
| US5744346A (en) * | 1995-06-07 | 1998-04-28 | Athena Neurosciences, Inc. | β-secretase |
| EP1324859B1 (en) * | 2000-09-29 | 2011-01-26 | Strasbaugh, Inc. | Polishing pad with built-in optical sensor |
| BR0209973A (pt) * | 2001-05-25 | 2004-04-06 | Warner Lambert Co | Composição farmacêutica lìquida |
| EP1453516A2 (de) * | 2001-10-17 | 2004-09-08 | Boehringer Ingelheim Pharma GmbH & Co.KG | 5-substituierte 4-amino-2-phenylamino-pyrimdinderivate und ihre verwendung als beta-amyloid modulatoren |
| RS50504A (sr) * | 2001-11-08 | 2007-04-10 | Elan Pharmaceuticals Inc., | Derivati n,n'-supstituisanog-1,3- diamino-2-hidroksipropana |
| CH698246B1 (de) * | 2001-12-20 | 2009-06-30 | Hoffmann La Roche | Test zur Identifizierung von Inhibitoren von Beta-Sekretasen. |
| JP2005534614A (ja) * | 2002-01-04 | 2005-11-17 | イーラン ファーマスーティカルズ、インコーポレイテッド | アルツハイマー病治療のための置換アミノカルボキサミド |
| NZ538625A (en) * | 2002-09-06 | 2008-05-30 | Pharmacia & Upjohn Co Llc | 1,3-Diamino-2-hydroxypropane prodrug derivatives |
| EP1562897B1 (en) * | 2002-11-12 | 2009-09-16 | Merck & Co., Inc. | Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer s disease |
| JP2007516207A (ja) * | 2003-06-30 | 2007-06-21 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病の治療のためのＮ−アルキルフェニルカルボキサミドβ−セクレターゼ阻害剤 |
| WO2005065195A2 (en) * | 2003-12-19 | 2005-07-21 | Merck & Co., Inc. | Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of alzheimer's disease |
| CA2567223A1 (en) * | 2004-05-19 | 2005-11-24 | Boehringer Ingelheim International Gmbh | Treatment of diseases associated with altered level of amyloid beta peptides |
| WO2006050862A1 (en) * | 2004-11-10 | 2006-05-18 | Boehringer Ingelheim International Gmbh | Statine derivatives for the treatment of alzheimer's disease |
| WO2006050861A2 (en) * | 2004-11-10 | 2006-05-18 | Boehringer Ingelheim International Gmbh | Statine derivatives for the treatment of alzheimer's disease |
| WO2006103038A1 (en) * | 2005-03-30 | 2006-10-05 | Boehringer Ingelheim International Gmbh | Substituted 1,2-ethylendiamines, medicaments comprising said compound; their use and their method of manufacture |
| CA2617294A1 (en) * | 2005-08-03 | 2007-02-08 | Boehringer Ingelheim International Gmbh | Substituted ethane-1,2-diamines for the treatment of alzheimer's disease ii |
| JP2009504614A (ja) * | 2005-08-11 | 2009-02-05 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | アルツハイマー病の治療用化合物 |
| JP2009504611A (ja) * | 2005-08-11 | 2009-02-05 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | アルツハイマー病の治療用β−セクレターゼインヒビター |
| US20090042867A1 (en) * | 2005-08-11 | 2009-02-12 | Klaus Fuchs | Compounds for the treatment of alzheimer's disease |
-
2006
- 2006-08-08 CA CA002618474A patent/CA2618474A1/en not_active Abandoned
- 2006-08-08 JP JP2008525577A patent/JP2009504613A/ja active Pending
- 2006-08-08 US US12/063,317 patent/US20100168070A1/en not_active Abandoned
- 2006-08-08 EP EP06792736A patent/EP1915353A2/de not_active Withdrawn
- 2006-08-08 WO PCT/EP2006/065155 patent/WO2007017510A2/de not_active Ceased
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