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 |
| AR045219A1 (es) * | 2003-08-08 | 2005-10-19 | Pharmacopeia Inc | Aminas ciclicas inhibidoras de base - 1 que poseen un sustiuyente heterociclico |
| WO2005097768A2 (en) * | 2004-04-05 | 2005-10-20 | Schering Corporation | Novel gamma secretase inhibitors |
| PE20060481A1 (es) * | 2004-06-30 | 2006-06-19 | Schering Corp | N-arilsulfonilaminas heterociclicas sustituidas como inhibidores de gamma-secretasas |
| CA2575340A1 (en) * | 2004-07-28 | 2006-02-09 | Schering Corporation | Macrocyclic beta-secretase inhibitors |
| US8524741B2 (en) * | 2006-07-10 | 2013-09-03 | Synapsin Pharmaceuticals, Inc. | Compositions and methods relating to solenopsins and their uses in treating neurological disorders and enhancing cognitive and 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 |
| RU2462464C2 (ru) * | 2006-09-29 | 2012-09-27 | Грюненталь Гмбх | Замещенные сульфамидные производные |
| US8278345B2 (en) | 2006-11-09 | 2012-10-02 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| ATE554085T1 (de) | 2006-11-30 | 2012-05-15 | Probiodrug Ag | Neue inhibitoren von glutaminylcyclase |
| JP5930573B2 (ja) | 2007-03-01 | 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の新規使用 |
| EP2142514B1 (en) | 2007-04-18 | 2014-12-24 | Probiodrug AG | Thiourea derivatives as glutaminyl cyclase inhibitors |
| AU2008256940A1 (en) * | 2007-05-25 | 2008-12-04 | Elan Pharmaceuticals, Inc. | Pyrazolopyrrolidines as inhibitors of gamma secretase |
| 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 |
| JP6026284B2 (ja) | 2010-03-03 | 2016-11-16 | プロビオドルグ エージー | グルタミニルシクラーゼの阻害剤 |
| NZ602312A (en) | 2010-03-10 | 2014-02-28 | Probiodrug Ag | Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5) |
| 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 |
| EP2780015B1 (en) | 2011-11-18 | 2017-01-04 | Heptares Therapeutics Limited | Muscarinic m1 receptor agonists |
| JP6478923B2 (ja) | 2013-02-07 | 2019-03-06 | ヘプタレス セラピューティクス リミテッドＨｅｐｔａｒｅｓ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｌｉｍｉｔｅｄ | ムスカリンｍ４受容体アゴニストとしてのピペリジン−１−イル及びアゼピン−１−イルカルボキシレート |
| 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 |
| JP7315483B2 (ja) * | 2017-06-30 | 2023-07-26 | ブリストル－マイヤーズ スクイブ カンパニー | 置換キノリニルシクロヘキシルプロパンアミド化合物および改良されたその製造方法 |
| 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 JP JP2006526994A patent/JP2007519607A/ja active Pending
- 2004-09-15 WO PCT/US2004/030191 patent/WO2005028440A1/en not_active Ceased
- 2004-09-15 CA CA002538590A patent/CA2538590A1/en not_active Abandoned
- 2004-09-15 AU AU2004274449A patent/AU2004274449A1/en not_active Abandoned
- 2004-09-15 AR ARP040103301A patent/AR045656A1/es unknown
- 2004-09-15 CN CNA2004800335264A patent/CN101061097A/zh active Pending
- 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
-
2006
- 2006-03-12 IL IL174270A patent/IL174270A0/en unknown
- 2006-03-15 ZA ZA200602193A patent/ZA200602193B/xx unknown
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