ECSP045218A - "novedosos inhibidores de la gamma secretasa" - Google Patents
"novedosos inhibidores de la gamma secretasa"Info
- Publication number
- ECSP045218A ECSP045218A EC2004005218A ECSP045218A ECSP045218A EC SP045218 A ECSP045218 A EC SP045218A EC 2004005218 A EC2004005218 A EC 2004005218A EC SP045218 A ECSP045218 A EC SP045218A EC SP045218 A ECSP045218 A EC SP045218A
- Authority
- EC
- Ecuador
- Prior art keywords
- alkyl
- secretasa
- gamma
- new inhibitors
- group
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000004350 aryl cycloalkyl group Chemical group 0.000 abstract 1
- -1 arylheterocycloalkyl Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003540 gamma secretase inhibitor Substances 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000005349 heteroarylcycloalkyl group Chemical group 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
- C07D211/96—Sulfur atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
La presente invención revela novedosos inhibidores de la gamma secretasa, de la Fórmula: en la cual: R1 es un grupo arilo sustituido ó heteroarilo sustituido; R2 es es un grupo R1 , alquilo, -X(CO)Y, ó alquileno-X(CO)Y, siendo X e Y como anteriormente definidos: cada uno de los R3 y cada uno de los R3A es independientemente entre sí Hó alquilo; R11 es alquilo, heteroarilo, alquilo, cicloalquilo, arilalquilo, arilcicloalquilo, heteroarilalquilo, heteroarilcicloalquilo, arilheterocicloalquilo, ó alcoxialquilo.También se revela un método para tratar la Enfermedad de Alzheirmer mediante uno ó más compuestos de la invención.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35561802P | 2002-02-06 | 2002-02-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP045218A true ECSP045218A (es) | 2004-09-28 |
Family
ID=27734543
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2004005218A ECSP045218A (es) | 2002-02-06 | 2004-08-03 | "novedosos inhibidores de la gamma secretasa" |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US7208602B2 (es) |
| EP (1) | EP1472223A1 (es) |
| JP (1) | JP4758609B2 (es) |
| KR (1) | KR20040081489A (es) |
| CN (1) | CN1628100A (es) |
| AR (1) | AR038482A1 (es) |
| AU (1) | AU2003210865B2 (es) |
| BR (1) | BR0307492A (es) |
| CA (1) | CA2478423A1 (es) |
| CO (1) | CO5611195A2 (es) |
| EC (1) | ECSP045218A (es) |
| MX (1) | MXPA04007659A (es) |
| MY (1) | MY141504A (es) |
| NO (1) | NO329067B1 (es) |
| NZ (1) | NZ534223A (es) |
| PE (1) | PE20030977A1 (es) |
| PL (1) | PL371735A1 (es) |
| RU (1) | RU2004126864A (es) |
| TW (1) | TW200302717A (es) |
| WO (1) | WO2003066592A1 (es) |
| ZA (1) | ZA200406237B (es) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7399775B2 (en) | 2001-12-27 | 2008-07-15 | Daiichi Pharmaceutical Co., Ltd. | β-amyloid protein production/secretion inhibitor |
| 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 |
| RU2336270C2 (ru) | 2003-06-30 | 2008-10-20 | Дайити Фармасьютикал Ко., Лтд. | Гетероциклические метилсульфоновые производные |
| EP1660443B1 (en) | 2003-08-08 | 2009-03-04 | Schering Corporation | Cyclic amine bace-1 inhibitors having a benzamide substituent |
| MXPA06001558A (es) | 2003-08-08 | 2006-05-15 | Schering Corp | Inhibidores de amina ciclica bace-1 que poseen un sustituyente heterociclico. |
| CA2544350A1 (en) | 2003-10-29 | 2005-05-12 | Elan Pharmaceuticals, Inc. | N-substituted benzene sulfonamides |
| KR20070010144A (ko) * | 2004-04-05 | 2007-01-22 | 쉐링 코포레이션 | 신규한 감마 세크레타제 억제제 |
| EP1758884A2 (en) * | 2004-05-20 | 2007-03-07 | Elan Pharmaceuticals, Inc. | N-cyclic sulfonamido inhibitors of gamma secretase |
| CN101602741A (zh) * | 2004-06-30 | 2009-12-16 | 先灵公司 | 作为γ-分泌酶抑制剂的取代的N-芳基磺酰基杂环胺 |
| AU2005261932B2 (en) * | 2004-07-13 | 2011-10-13 | F. Hoffmann-La Roche Ag | Sulfonamide derivatives |
| ATE491693T1 (de) | 2004-07-22 | 2011-01-15 | Schering Corp | Substituierte amide als inhibitoren der beta- sekretase |
| NZ553696A (en) | 2004-09-13 | 2010-02-26 | Ono Pharmaceutical Co | Nitrogenous heterocyclic derivative and medicine containing the same as an active ingredient |
| GB0423356D0 (en) * | 2004-10-21 | 2004-11-24 | Merck Sharp & Dohme | Therapeutic agents |
| EP1916985A4 (en) * | 2005-08-19 | 2010-06-09 | Elan Pharm Inc | BRIDGED N-CYCLIC SULPHONAMIDE INHIBITORS OF THE GAMMED CRYSTETRY |
| WO2007105637A1 (ja) | 2006-03-10 | 2007-09-20 | 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 |
| EP2041181B1 (en) * | 2006-06-08 | 2011-05-18 | Helmholtz Zentrum München Deutsches Forschungszentrum für Gesundheit und Umwelt (GmbH) | Specific protease inhibitors and their use in cancer therapy |
| MX2009003382A (es) * | 2006-09-29 | 2009-04-08 | Gruenenthal Gmbh | Derivados de sulfonamidas sustituidos. |
| US8278345B2 (en) | 2006-11-09 | 2012-10-02 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| CN101534824A (zh) * | 2006-11-17 | 2009-09-16 | 艾博特公司 | 作为化学活素受体拮抗剂的氨基吡咯烷 |
| JP5523107B2 (ja) | 2006-11-30 | 2014-06-18 | プロビオドルグ エージー | グルタミニルシクラーゼの新規阻害剤 |
| US8080549B2 (en) * | 2007-01-12 | 2011-12-20 | Concert Pharmaceuticals, Inc. | Endothelin receptor antagonists |
| EP2481408A3 (en) | 2007-03-01 | 2013-01-09 | Probiodrug AG | New use of glutaminyl cyclase inhibitors |
| WO2008128985A1 (en) | 2007-04-18 | 2008-10-30 | Probiodrug Ag | Thiourea derivatives as glutaminyl cyclase inhibitors |
| NZ582039A (en) * | 2007-05-25 | 2012-02-24 | Elan Pharm 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 |
| MX2012002993A (es) | 2009-09-11 | 2012-04-19 | Probiodrug Ag | Derivados heterociclicos como inhibidores de ciclasa glutaminilo. |
| 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 |
| US8269019B2 (en) | 2010-03-10 | 2012-09-18 | Probiodrug Ag | Inhibitors |
| WO2011131748A2 (en) | 2010-04-21 | 2011-10-27 | Probiodrug Ag | Novel inhibitors |
| ES2570167T3 (es) | 2011-03-16 | 2016-05-17 | Probiodrug Ag | Derivados de benzimidazol como inhibidores de glutaminil ciclasa |
| CN105189482A (zh) | 2013-02-07 | 2015-12-23 | 武田药品工业株式会社 | 作为毒蕈碱m4受体激动剂的哌啶-1-基羧酸酯和氮杂卓-1-基羧酸酯 |
| PL3461819T3 (pl) | 2017-09-29 | 2020-11-30 | Probiodrug Ag | Inhibitory cyklazy glutaminylowej |
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 KR KR10-2004-7012102A patent/KR20040081489A/ko not_active Ceased
- 2003-02-05 PL PL03371735A patent/PL371735A1/xx not_active Application Discontinuation
- 2003-02-05 MY MYPI20030381A patent/MY141504A/en unknown
- 2003-02-05 WO PCT/US2003/003471 patent/WO2003066592A1/en not_active Ceased
- 2003-02-05 EP EP03737650A patent/EP1472223A1/en not_active Withdrawn
- 2003-02-05 NZ NZ534223A patent/NZ534223A/en unknown
- 2003-02-05 BR BR0307492-7A patent/BR0307492A/pt not_active IP Right Cessation
- 2003-02-05 US US10/358,898 patent/US7208602B2/en not_active Expired - Fee Related
- 2003-02-05 JP JP2003565966A patent/JP4758609B2/ja not_active Expired - Fee Related
- 2003-02-05 CA CA002478423A patent/CA2478423A1/en not_active Abandoned
- 2003-02-05 CN CNA038032686A patent/CN1628100A/zh active Pending
- 2003-02-05 RU RU2004126864/04A patent/RU2004126864A/ru not_active Application Discontinuation
- 2003-02-05 AU AU2003210865A patent/AU2003210865B2/en not_active Ceased
- 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
Also Published As
| Publication number | Publication date |
|---|---|
| US20040048848A1 (en) | 2004-03-11 |
| MXPA04007659A (es) | 2005-06-08 |
| NO20043696L (no) | 2004-11-05 |
| US20060100427A1 (en) | 2006-05-11 |
| JP2005522437A (ja) | 2005-07-28 |
| AU2003210865B2 (en) | 2008-01-31 |
| BR0307492A (pt) | 2004-11-23 |
| JP4758609B2 (ja) | 2011-08-31 |
| PE20030977A1 (es) | 2003-12-04 |
| PL371735A1 (en) | 2005-06-27 |
| AU2003210865A1 (en) | 2003-09-02 |
| US7208602B2 (en) | 2007-04-24 |
| KR20040081489A (ko) | 2004-09-21 |
| CN1628100A (zh) | 2005-06-15 |
| NO329067B1 (no) | 2010-08-16 |
| NZ534223A (en) | 2007-05-31 |
| EP1472223A1 (en) | 2004-11-03 |
| CA2478423A1 (en) | 2003-08-14 |
| MY141504A (en) | 2010-05-14 |
| TW200302717A (en) | 2003-08-16 |
| ZA200406237B (en) | 2005-09-22 |
| AR038482A1 (es) | 2005-01-19 |
| WO2003066592A1 (en) | 2003-08-14 |
| RU2004126864A (ru) | 2005-07-10 |
| CO5611195A2 (es) | 2006-02-28 |
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