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)
- Biomedical Technology (AREA)
- Neurosurgery (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 |
---|---|---|---|---|
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 |
JP4523914B2 (ja) | 2003-06-30 | 2010-08-11 | 第一三共株式会社 | 複素環メチルスルホン誘導体 |
ATE424383T1 (de) | 2003-08-08 | 2009-03-15 | Schering Corp | Cyclische amine mit benzamidsubstituent als bace- 1-inhibitoren |
US7598250B2 (en) | 2003-08-08 | 2009-10-06 | Schering Corporation | Cyclic amine BACE-1 inhibitors having a heterocyclic substituent |
WO2005042489A1 (en) * | 2003-10-29 | 2005-05-12 | Elan Pharmaceuticals, Inc. | N-substituted benzene sulfonamides |
CN1950358A (zh) * | 2004-04-05 | 2007-04-18 | 先灵公司 | 新颖的γ分泌酶抑制剂 |
WO2005113542A2 (en) * | 2004-05-20 | 2005-12-01 | Elan Pharmaceuticals, Inc. | N-cyclic sulfonamido inhibitors of gamma secretase |
ATE461926T1 (de) * | 2004-06-30 | 2010-04-15 | Schering Corp | Substituierte n-arylsulfonylheterocyclische amine als gamma-sekretase-hemmer |
CN101747324A (zh) * | 2004-07-13 | 2010-06-23 | 弗·哈夫曼-拉罗切有限公司 | 磺酰胺衍生物 |
MX2007000760A (es) | 2004-07-22 | 2007-04-09 | Schering Corp | Amida sustituida inhibidora de b secretasa. |
MX2007002886A (es) | 2004-09-13 | 2007-05-16 | Ono Pharmaceutical Co | Derivado heterociclico que contiene nitrogeno y un farmaco que contiene el mismo como el ingrediente activo. |
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 |
CA2644368A1 (en) | 2006-03-10 | 2007-09-20 | Ono Pharmaceutical Co., Ltd. | Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient |
US20100226922A1 (en) * | 2006-06-08 | 2010-09-09 | Dorothea Maetzel | Specific protease inhibitors and their use in cancer therapy |
CN101553481A (zh) * | 2006-09-29 | 2009-10-07 | 格吕伦塔尔有限公司 | 取代的磺酰胺衍生物 |
JP5379692B2 (ja) | 2006-11-09 | 2013-12-25 | プロビオドルグ エージー | 潰瘍、癌及び他の疾患の治療のためのグルタミニルシクラーゼの阻害薬としての3−ヒドロキシ−1,5−ジヒドロ−ピロール−2−オン誘導体 |
EP2099454A4 (en) * | 2006-11-17 | 2010-11-10 | Abbott Lab | AMINOPYRROLIDINES AS CHEMOKINE RECEPTOR ANTAGONISTS |
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 |
ZA200905537B (en) | 2007-03-01 | 2010-10-27 | Probiodrug Ag | New use of glutaminyl cyclase inhibitors |
ES2533484T3 (es) | 2007-04-18 | 2015-04-10 | Probiodrug Ag | Derivados de tiourea como inhibidores de la glutaminil ciclasa |
BRPI0812014A2 (pt) * | 2007-05-25 | 2014-11-18 | Elan Pharm Inc | Pirazolopirrolidinas como inibidores de gama secretase, composição farmacêutica compreendendo as mesmas e uso dos referidos compostos |
CN102137669A (zh) * | 2008-06-03 | 2011-07-27 | 弗雷森纽斯医疗护理德国有限责任公司 | 包含γ分泌酶调节剂的药物组合物 |
EA022007B1 (ru) | 2009-09-11 | 2015-10-30 | Пробиодруг Аг | Гетероциклические производные в качестве ингибиторов глутаминилциклазы |
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 |
KR101790806B1 (ko) | 2010-03-10 | 2017-11-20 | 프로비오드룩 아게 | 글루타미닐 사이클라제(qc, ec 2.3.2.5)의 헤테로사이클릭 억제제 |
EP2560953B1 (en) | 2010-04-21 | 2016-01-06 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
WO2012123563A1 (en) | 2011-03-16 | 2012-09-20 | Probiodrug Ag | Benz imidazole 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 |
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 PL PL03371735A patent/PL371735A1/xx not_active Application Discontinuation
- 2003-02-05 KR KR10-2004-7012102A patent/KR20040081489A/ko not_active Application Discontinuation
- 2003-02-05 BR BR0307492-7A patent/BR0307492A/pt not_active IP Right Cessation
- 2003-02-05 MY MYPI20030381A patent/MY141504A/en unknown
- 2003-02-05 CN CNA038032686A patent/CN1628100A/zh active Pending
- 2003-02-05 CA CA002478423A patent/CA2478423A1/en not_active Abandoned
- 2003-02-05 EP EP03737650A patent/EP1472223A1/en not_active Withdrawn
- 2003-02-05 NZ NZ534223A patent/NZ534223A/en unknown
- 2003-02-05 MX MXPA04007659A patent/MXPA04007659A/es active IP Right Grant
- 2003-02-05 WO PCT/US2003/003471 patent/WO2003066592A1/en active Application Filing
- 2003-02-05 RU RU2004126864/04A patent/RU2004126864A/ru not_active Application Discontinuation
- 2003-02-05 US US10/358,898 patent/US7208602B2/en not_active Expired - Fee Related
- 2003-02-05 AU AU2003210865A patent/AU2003210865B2/en not_active Ceased
- 2003-02-05 JP JP2003565966A patent/JP4758609B2/ja not_active Expired - Fee Related
-
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 |
---|---|
AU2003210865A1 (en) | 2003-09-02 |
MXPA04007659A (es) | 2005-06-08 |
TW200302717A (en) | 2003-08-16 |
BR0307492A (pt) | 2004-11-23 |
JP2005522437A (ja) | 2005-07-28 |
JP4758609B2 (ja) | 2011-08-31 |
CN1628100A (zh) | 2005-06-15 |
MY141504A (en) | 2010-05-14 |
NO329067B1 (no) | 2010-08-16 |
US20060100427A1 (en) | 2006-05-11 |
AU2003210865B2 (en) | 2008-01-31 |
RU2004126864A (ru) | 2005-07-10 |
ZA200406237B (en) | 2005-09-22 |
NO20043696L (no) | 2004-11-05 |
EP1472223A1 (en) | 2004-11-03 |
NZ534223A (en) | 2007-05-31 |
CO5611195A2 (es) | 2006-02-28 |
PL371735A1 (en) | 2005-06-27 |
PE20030977A1 (es) | 2003-12-04 |
WO2003066592A1 (en) | 2003-08-14 |
AR038482A1 (es) | 2005-01-19 |
US20040048848A1 (en) | 2004-03-11 |
CA2478423A1 (en) | 2003-08-14 |
KR20040081489A (ko) | 2004-09-21 |
US7208602B2 (en) | 2007-04-24 |
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