JP2005522437A5 - - Google Patents
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- Publication number
- JP2005522437A5 JP2005522437A5 JP2003565966A JP2003565966A JP2005522437A5 JP 2005522437 A5 JP2005522437 A5 JP 2005522437A5 JP 2003565966 A JP2003565966 A JP 2003565966A JP 2003565966 A JP2003565966 A JP 2003565966A JP 2005522437 A5 JP2005522437 A5 JP 2005522437A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- group
- alkylene
- unsubstituted
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 46
- 150000001875 compounds Chemical class 0.000 claims 22
- 125000003118 aryl group Chemical group 0.000 claims 21
- 125000001072 heteroaryl group Chemical group 0.000 claims 18
- 239000008194 pharmaceutical composition Substances 0.000 claims 13
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 12
- 125000002947 alkylene group Chemical group 0.000 claims 11
- 125000001424 substituent group Chemical group 0.000 claims 10
- 125000003710 aryl alkyl group Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 6
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 5
- 125000004350 aryl cycloalkyl group Chemical group 0.000 claims 4
- 125000005349 heteroarylcycloalkyl group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 2
- 125000002993 cycloalkylene group Chemical group 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
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 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
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 claims 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 claims 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 1
- 108010090849 Amyloid beta-Peptides Proteins 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
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 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
- 230000008021 deposition Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35561802P | 2002-02-06 | 2002-02-06 | |
| US60/355,618 | 2002-02-06 | ||
| PCT/US2003/003471 WO2003066592A1 (en) | 2002-02-06 | 2003-02-05 | Gamma secretase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005522437A JP2005522437A (ja) | 2005-07-28 |
| JP2005522437A5 true JP2005522437A5 (https=) | 2006-04-06 |
| JP4758609B2 JP4758609B2 (ja) | 2011-08-31 |
Family
ID=27734543
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003565966A Expired - Fee Related JP4758609B2 (ja) | 2002-02-06 | 2003-02-05 | γ−セクレターゼ阻害剤 |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US7208602B2 (https=) |
| EP (1) | EP1472223A1 (https=) |
| JP (1) | JP4758609B2 (https=) |
| KR (1) | KR20040081489A (https=) |
| CN (1) | CN1628100A (https=) |
| AR (1) | AR038482A1 (https=) |
| AU (1) | AU2003210865B2 (https=) |
| BR (1) | BR0307492A (https=) |
| CA (1) | CA2478423A1 (https=) |
| CO (1) | CO5611195A2 (https=) |
| EC (1) | ECSP045218A (https=) |
| MX (1) | MXPA04007659A (https=) |
| MY (1) | MY141504A (https=) |
| NO (1) | NO329067B1 (https=) |
| NZ (1) | NZ534223A (https=) |
| PE (1) | PE20030977A1 (https=) |
| PL (1) | PL371735A1 (https=) |
| RU (1) | RU2004126864A (https=) |
| TW (1) | TW200302717A (https=) |
| WO (1) | WO2003066592A1 (https=) |
| ZA (1) | ZA200406237B (https=) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100562516C (zh) | 2001-12-27 | 2009-11-25 | 第一制药株式会社 | β-淀粉样蛋白产生和分泌的抑制剂 |
| US20040171614A1 (en) * | 2002-02-06 | 2004-09-02 | Schering-Plough Corporation | Novel gamma secretase inhibitors |
| US7256186B2 (en) | 2002-02-06 | 2007-08-14 | Schering Corporation | Gamma secretase inhibitors |
| US7521481B2 (en) | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
| WO2004080966A1 (ja) | 2003-03-14 | 2004-09-23 | Ono Pharmaceutical Co., Ltd. | 含窒素複素環誘導体およびそれらを有効成分とする薬剤 |
| CA2526487A1 (en) | 2003-06-30 | 2005-01-06 | Daiichi Pharmaceutical Co., Ltd. | Heterocyclic methyl sulfone derivative |
| MXPA06001558A (es) | 2003-08-08 | 2006-05-15 | Schering Corp | Inhibidores de amina ciclica bace-1 que poseen un sustituyente heterociclico. |
| ES2323068T3 (es) | 2003-08-08 | 2009-07-06 | Schering Corporation | Inhibidores de bace-1 de aminas ciclicas con un sustituyente de benzamida. |
| RU2364587C2 (ru) * | 2003-10-29 | 2009-08-20 | Элан Фармасьютикалз, Инк. | N-замещенные бензолсульфонамиды |
| TWI300410B (en) * | 2004-04-05 | 2008-09-01 | Schering Corp | Novel gamma secretase inhibitors |
| CA2567343A1 (en) * | 2004-05-20 | 2005-12-01 | Elan Pharmaceuticals, Inc. | N-cyclic sulfonamido inhibitors of gamma secretase |
| PE20060481A1 (es) * | 2004-06-30 | 2006-06-19 | Schering Corp | N-arilsulfonilaminas heterociclicas sustituidas como inhibidores de gamma-secretasas |
| KR100880972B1 (ko) * | 2004-07-13 | 2009-02-03 | 에프. 호프만-라 로슈 아게 | 설폰아마이드 유도체 |
| EP1781625B1 (en) | 2004-07-22 | 2010-12-15 | Schering Corporation | Substituted amide beta secretase inhibitors |
| EP1790637B1 (en) | 2004-09-13 | 2014-01-29 | Ono Pharmaceutical Co., Ltd. | Derivatives of N-4-piperidyl urea and medicaments containing them as active ingredient |
| GB0423356D0 (en) * | 2004-10-21 | 2004-11-24 | Merck Sharp & Dohme | Therapeutic agents |
| BRPI0614944A2 (pt) * | 2005-08-19 | 2011-04-26 | Elan Pharm Inc | inibidores sulfonamido n-bicìclicos ponte de gama-secretase |
| KR20090008217A (ko) | 2006-03-10 | 2009-01-21 | 오노 야꾸힝 고교 가부시키가이샤 | 질소 함유 복소환 유도체 및 이들을 유효 성분으로 하는 약제 |
| ATE509956T1 (de) * | 2006-06-08 | 2011-06-15 | Helmholtz Zentrum Muenchen | Spezifische proteaseinhibitoren und ihre verwendung in der krebstherapie |
| 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 |
| CA2669917A1 (en) * | 2006-11-17 | 2008-05-22 | Dawn M. George | Aminopyrrolidines as chemokine receptor antagonists |
| US9126987B2 (en) | 2006-11-30 | 2015-09-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| US8080549B2 (en) * | 2007-01-12 | 2011-12-20 | Concert Pharmaceuticals, Inc. | Endothelin receptor antagonists |
| 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 |
| 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 |
| ES2812698T3 (es) | 2017-09-29 | 2021-03-18 | Probiodrug Ag | Inhibidores de glutaminil ciclasa |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2687146B1 (fr) * | 1992-02-12 | 1994-04-01 | Adir Cie | Nouveaux derives de pyrrolidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| US6166037A (en) * | 1997-08-28 | 2000-12-26 | Merck & Co., Inc. | Pyrrolidine and piperidine modulators of chemokine receptor activity |
| GB9800750D0 (en) * | 1998-01-14 | 1998-03-11 | Lilly Co Eli | Pharmaceutical compound |
| GB9804426D0 (en) * | 1998-03-02 | 1998-04-29 | Pfizer Ltd | Heterocycles |
| TW575561B (en) * | 1999-03-25 | 2004-02-11 | Hoffmann La Roche | 1-arenesulfonyl-2-aryl-pyrrolidine and piperidine derivatives |
| US6589978B2 (en) * | 2000-06-30 | 2003-07-08 | Hoffman-La Roche Inc. | 1-sulfonyl pyrrolidine derivatives |
-
2003
- 2003-01-30 TW TW092102236A patent/TW200302717A/zh unknown
- 2003-02-04 PE PE2003000130A patent/PE20030977A1/es not_active Application Discontinuation
- 2003-02-04 AR ARP030100346A patent/AR038482A1/es unknown
- 2003-02-05 EP EP03737650A patent/EP1472223A1/en not_active Withdrawn
- 2003-02-05 CN CNA038032686A patent/CN1628100A/zh active Pending
- 2003-02-05 JP JP2003565966A patent/JP4758609B2/ja not_active Expired - Fee Related
- 2003-02-05 PL PL03371735A patent/PL371735A1/xx not_active Application Discontinuation
- 2003-02-05 WO PCT/US2003/003471 patent/WO2003066592A1/en not_active Ceased
- 2003-02-05 AU AU2003210865A patent/AU2003210865B2/en not_active Ceased
- 2003-02-05 BR BR0307492-7A patent/BR0307492A/pt not_active IP Right Cessation
- 2003-02-05 RU RU2004126864/04A patent/RU2004126864A/ru not_active Application Discontinuation
- 2003-02-05 NZ NZ534223A patent/NZ534223A/en unknown
- 2003-02-05 US US10/358,898 patent/US7208602B2/en not_active Expired - Fee Related
- 2003-02-05 KR KR10-2004-7012102A patent/KR20040081489A/ko not_active Ceased
- 2003-02-05 MY MYPI20030381A patent/MY141504A/en unknown
- 2003-02-05 CA CA002478423A patent/CA2478423A1/en not_active Abandoned
- 2003-02-05 MX MXPA04007659A patent/MXPA04007659A/es active IP Right Grant
-
2004
- 2004-08-03 EC EC2004005218A patent/ECSP045218A/es unknown
- 2004-08-04 ZA ZA200406237A patent/ZA200406237B/en unknown
- 2004-08-06 CO CO04076759A patent/CO5611195A2/es not_active Application Discontinuation
- 2004-09-03 NO NO20043696A patent/NO329067B1/no not_active IP Right Cessation
-
2005
- 2005-10-03 US US11/242,337 patent/US20060100427A1/en not_active Abandoned
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