JP2007519607A5 - - Google Patents
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- Publication number
- JP2007519607A5 JP2007519607A5 JP2006526994A JP2006526994A JP2007519607A5 JP 2007519607 A5 JP2007519607 A5 JP 2007519607A5 JP 2006526994 A JP2006526994 A JP 2006526994A JP 2006526994 A JP2006526994 A JP 2006526994A JP 2007519607 A5 JP2007519607 A5 JP 2007519607A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- group
- unsubstituted
- aryl
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 47
- 150000001875 compounds Chemical class 0.000 claims 37
- 125000003118 aryl group Chemical group 0.000 claims 23
- 125000001072 heteroaryl group Chemical group 0.000 claims 17
- 239000000203 mixture Substances 0.000 claims 16
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 14
- 125000001424 substituent group Chemical group 0.000 claims 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 125000003710 aryl alkyl group Chemical group 0.000 claims 9
- 150000002148 esters Chemical class 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 7
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 125000002947 alkylene group Chemical group 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 claims 4
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 claims 4
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 4
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 4
- 125000004350 aryl cycloalkyl group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 230000008021 deposition Effects 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- 230000005764 inhibitory process Effects 0.000 claims 4
- 230000004770 neurodegeneration Effects 0.000 claims 4
- 208000015122 neurodegenerative disease Diseases 0.000 claims 4
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000005349 heteroarylcycloalkyl group Chemical group 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- -1 1,1-ethylenedioxy Chemical group 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- DGYIJVNZSDYBOE-UHFFFAOYSA-N [CH2]C1=CC=NC=C1 Chemical group [CH2]C1=CC=NC=C1 DGYIJVNZSDYBOE-UHFFFAOYSA-N 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000003435 aroyl group Chemical group 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
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 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 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 0 CC*(C)(C(C)C1C(C)(C)*C)NC(C)C(*)C(C(C)(*)N2)C2(C)N1S(*)(=O)=O Chemical compound CC*(C)(C(C)C1C(C)(C)*C)NC(C)C(*)C(C(C)(*)N2)C2(C)N1S(*)(=O)=O 0.000 description 29
- GPASDLXNNAPVRX-UHFFFAOYSA-N CN(CC1)CCC1N1CCCCC1 Chemical compound CN(CC1)CCC1N1CCCCC1 GPASDLXNNAPVRX-UHFFFAOYSA-N 0.000 description 3
- YQOPNAOQGQSUHF-UHFFFAOYSA-N CC(C)N1CCCC1 Chemical compound CC(C)N1CCCC1 YQOPNAOQGQSUHF-UHFFFAOYSA-N 0.000 description 1
- KKBDINYFLTTZAQ-UHFFFAOYSA-N CCCCN(C)C(C)C Chemical compound CCCCN(C)C(C)C KKBDINYFLTTZAQ-UHFFFAOYSA-N 0.000 description 1
- BUHRTPXALUXAGG-UHFFFAOYSA-N CN(CC1)CCC1N1CCCC1 Chemical compound CN(CC1)CCC1N1CCCC1 BUHRTPXALUXAGG-UHFFFAOYSA-N 0.000 description 1
- GYPOLRIBHDXZAV-UHFFFAOYSA-N CN(CC1)CCN1C1CCCCC1 Chemical compound CN(CC1)CCN1C1CCCCC1 GYPOLRIBHDXZAV-UHFFFAOYSA-N 0.000 description 1
- MVSSXDKAQLWYQO-FUNVUKJBSA-N CN([C@H](CC1)C2)[C@@H]1CC2N1CCCCC1 Chemical compound CN([C@H](CC1)C2)[C@@H]1CC2N1CCCCC1 MVSSXDKAQLWYQO-FUNVUKJBSA-N 0.000 description 1
- PBKBNZLWSVHLAG-UHFFFAOYSA-N CNCCCN1CCCC1 Chemical compound CNCCCN1CCCC1 PBKBNZLWSVHLAG-UHFFFAOYSA-N 0.000 description 1
- ZPMDRIAJBDFGCZ-UHFFFAOYSA-N CNCCC[n]1cncc1 Chemical compound CNCCC[n]1cncc1 ZPMDRIAJBDFGCZ-UHFFFAOYSA-N 0.000 description 1
- SIVLSVIYONPJAK-YFNKSVMNSA-N O[C@H](CCC1)CN1C(OC1(CC1)[C@@H](CCC[C@H]1c2cc(F)cc(F)c2)N1S(c(cc1)ccc1Cl)(=O)=O)=O Chemical compound O[C@H](CCC1)CN1C(OC1(CC1)[C@@H](CCC[C@H]1c2cc(F)cc(F)c2)N1S(c(cc1)ccc1Cl)(=O)=O)=O SIVLSVIYONPJAK-YFNKSVMNSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/663,042 US20040171614A1 (en) | 2002-02-06 | 2003-09-16 | Novel gamma secretase inhibitors |
| PCT/US2004/030191 WO2005028440A1 (en) | 2003-09-16 | 2004-09-15 | Novel gamma secretase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007519607A JP2007519607A (ja) | 2007-07-19 |
| JP2007519607A5 true JP2007519607A5 (https=) | 2007-11-01 |
Family
ID=34375807
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006526994A Pending JP2007519607A (ja) | 2003-09-16 | 2004-09-15 | 新規γ−セクレターゼ阻害剤 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20040171614A1 (https=) |
| EP (1) | EP1663975A1 (https=) |
| JP (1) | JP2007519607A (https=) |
| KR (1) | KR20060106814A (https=) |
| CN (1) | CN101061097A (https=) |
| AR (1) | AR045656A1 (https=) |
| AU (1) | AU2004274449A1 (https=) |
| CA (1) | CA2538590A1 (https=) |
| IL (1) | IL174270A0 (https=) |
| MX (1) | MXPA06003058A (https=) |
| PE (1) | PE20050377A1 (https=) |
| TW (1) | TW200519087A (https=) |
| WO (1) | WO2005028440A1 (https=) |
| ZA (1) | ZA200602193B (https=) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7256186B2 (en) * | 2002-02-06 | 2007-08-14 | Schering Corporation | Gamma secretase inhibitors |
| US20040171614A1 (en) * | 2002-02-06 | 2004-09-02 | Schering-Plough Corporation | Novel gamma secretase inhibitors |
| US7521481B2 (en) | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
| MXPA06001558A (es) * | 2003-08-08 | 2006-05-15 | Schering Corp | Inhibidores de amina ciclica bace-1 que poseen un sustituyente heterociclico. |
| TWI300410B (en) * | 2004-04-05 | 2008-09-01 | Schering Corp | Novel gamma secretase inhibitors |
| PE20060481A1 (es) * | 2004-06-30 | 2006-06-19 | Schering Corp | N-arilsulfonilaminas heterociclicas sustituidas como inhibidores de gamma-secretasas |
| DE602005007245D1 (https=) * | 2004-07-28 | 2008-07-10 | Schering Corp | |
| WO2008008720A2 (en) | 2006-07-10 | 2008-01-17 | Synapsin Pharmaceuticals, Inc. | Compositions and methods relating to solenopsins and their uses in treating neurological disorders and enhancing physical performance |
| US9259419B2 (en) | 2006-07-10 | 2016-02-16 | Synapsin Pharmaceuticals, Inc. | Compositions and methods relating to solenopsins and their uses in treating neurological disorders and enhancing physical performance |
| EP2383267A1 (de) * | 2006-09-29 | 2011-11-02 | Grünenthal GmbH | Substituierte Sulfonamid-Derivate |
| EP2089383B1 (en) | 2006-11-09 | 2015-09-16 | Probiodrug AG | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
| US9126987B2 (en) | 2006-11-30 | 2015-09-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| AU2008220785B2 (en) | 2007-03-01 | 2013-02-21 | Vivoryon Therapeutics N.V. | New use of glutaminyl cyclase inhibitors |
| JP5667440B2 (ja) | 2007-04-18 | 2015-02-12 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体 |
| JP2010528036A (ja) * | 2007-05-25 | 2010-08-19 | エラン ファーマシューティカルズ,インコーポレイテッド | γセクレターゼの阻害剤としてのピラゾロピロリジン |
| JP2011523655A (ja) * | 2008-06-03 | 2011-08-18 | フレセニウス メディカル ケア ドイッチュランド ゲーエムベーハー | ガンマセクレターゼモジュレータを含む医薬組成物 |
| JP5934645B2 (ja) | 2009-09-11 | 2016-06-15 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体 |
| WO2011107530A2 (en) | 2010-03-03 | 2011-09-09 | Probiodrug Ag | Novel inhibitors |
| JP5688745B2 (ja) | 2010-03-10 | 2015-03-25 | プロビオドルグ エージー | グルタミニルシクラーゼ(qc、ec2.3.2.5)の複素環阻害剤 |
| WO2011131748A2 (en) | 2010-04-21 | 2011-10-27 | Probiodrug Ag | Novel inhibitors |
| EP2686313B1 (en) | 2011-03-16 | 2016-02-03 | Probiodrug AG | Benzimidazole derivatives as inhibitors of glutaminyl cyclase |
| AU2012338581B2 (en) | 2011-11-18 | 2016-12-08 | Nxera Pharma Uk Limited | Muscarinic M1 receptor agonists |
| WO2014122474A1 (en) | 2013-02-07 | 2014-08-14 | Takeda Pharmaceutical Company Limited | Piperidin-1 -yl and azepin-1 -yl carboxylates as muscarinic m4 receptor agonists |
| GB201404922D0 (en) | 2014-03-19 | 2014-04-30 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201513743D0 (en) | 2015-08-03 | 2015-09-16 | Heptares Therapeutics Ltd | Muscarinic agonists |
| GB201519352D0 (en) | 2015-11-02 | 2015-12-16 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201617454D0 (en) | 2016-10-14 | 2016-11-30 | Heptares Therapeutics Limited | Pharmaceutical compounds |
| EP3645008A4 (en) * | 2017-06-30 | 2020-12-09 | Bristol-Myers Squibb Company | SUBSTITUTED QUINOLINYCYCLOHEXYLPROPANAMIDE COMPOUNDS AND IMPROVED METHODS FOR THEIR PRODUCTION |
| ES2812698T3 (es) | 2017-09-29 | 2021-03-18 | Probiodrug Ag | Inhibidores de glutaminil ciclasa |
| GB201810239D0 (en) | 2018-06-22 | 2018-08-08 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201819960D0 (en) | 2018-12-07 | 2019-01-23 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201819961D0 (en) | 2018-12-07 | 2019-01-23 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB202020191D0 (en) | 2020-12-18 | 2021-02-03 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9804426D0 (en) * | 1998-03-02 | 1998-04-29 | Pfizer Ltd | Heterocycles |
| US6589978B2 (en) * | 2000-06-30 | 2003-07-08 | Hoffman-La Roche Inc. | 1-sulfonyl pyrrolidine derivatives |
| TW200302717A (en) * | 2002-02-06 | 2003-08-16 | Schering Corp | Novel gamma secretase inhibitors |
| US20040171614A1 (en) * | 2002-02-06 | 2004-09-02 | Schering-Plough Corporation | Novel gamma secretase inhibitors |
-
2003
- 2003-09-16 US US10/663,042 patent/US20040171614A1/en not_active Abandoned
-
2004
- 2004-09-14 TW TW093127793A patent/TW200519087A/zh unknown
- 2004-09-14 PE PE2004000889A patent/PE20050377A1/es not_active Application Discontinuation
- 2004-09-15 WO PCT/US2004/030191 patent/WO2005028440A1/en not_active Ceased
- 2004-09-15 MX MXPA06003058A patent/MXPA06003058A/es not_active Application Discontinuation
- 2004-09-15 EP EP04784148A patent/EP1663975A1/en not_active Withdrawn
- 2004-09-15 KR KR1020067005286A patent/KR20060106814A/ko not_active Withdrawn
- 2004-09-15 AR ARP040103301A patent/AR045656A1/es unknown
- 2004-09-15 CA CA002538590A patent/CA2538590A1/en not_active Abandoned
- 2004-09-15 JP JP2006526994A patent/JP2007519607A/ja active Pending
- 2004-09-15 AU AU2004274449A patent/AU2004274449A1/en not_active Abandoned
- 2004-09-15 CN CNA2004800335264A patent/CN101061097A/zh active Pending
-
2006
- 2006-03-12 IL IL174270A patent/IL174270A0/en unknown
- 2006-03-15 ZA ZA200602193A patent/ZA200602193B/xx unknown
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