CO6241122A2 - Pirazolpirrolidinas como inhibidores de gamma secretasa - Google Patents
Pirazolpirrolidinas como inhibidores de gamma secretasaInfo
- Publication number
- CO6241122A2 CO6241122A2 CO09147608A CO09147608A CO6241122A2 CO 6241122 A2 CO6241122 A2 CO 6241122A2 CO 09147608 A CO09147608 A CO 09147608A CO 09147608 A CO09147608 A CO 09147608A CO 6241122 A2 CO6241122 A2 CO 6241122A2
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- aryl
- heterocyclyl
- heteroaryl
- alkoxy
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (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)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
1.- Compuestos de la fórmula:estereoisómeros, tautómeros, mezclas de estereoisómeros y/o tautómeros o sales farmacéuticamente aceptables de los mismos, en donde: A es alquilo C1-C6, arilo, cicloalquilo C3-C6, heteroarilo o heterociclilo, donde cada anillo se sustituye opcionalmente, en una posición sustituible, con uno o más entre halógeno, alquilo C1-C6, alquenilo C2-C6, alquinilo C2-C6, alcoxi C1-C6, haloalquilo C1-C6, haloalcoxi C1-C6, hidroxilo, hidroxialquilo, CN, ariloxi, arilalquiloxi, -SO2-(alquilo C1-C6), -NR'R", alcanoilo C1-C6, alquil C0-C3-C(O)OR', heteroarilo, heterociclilo, arilo, arilalquilo, o -SO2-NR'R", y en dondecuando A es alquilo C1-C6, el grupo alquilo C1-C6 se sustituye opcionalmente en una posición sustituible con uno o más entre halógeno, alquenilo C2-C6, alquinilo C2-C6, alcoxi C1-C6, haloalquilo C1-C6, haloalcoxi C1-C6, haloalcoxi C1-C6, hidroxilo, hidroxialquilo, CN, ariloxi, arilalquiloxi, -SO2-(alquilo C1-C6), -NR'R", alcanoilo C1-C6, alquilo C0-C3-C(C)OR', heteroarilo, heterociclilo, arilo, arilalquilo, o -SO2-NR'R", R1, R1a, R2, y R2a, son independientemente hidrógeno,Alquilo C1-C6, alquenilo C2-C6, alquinilo C2-C6, cicloalquiloC3-C6, cicloalquilo C3-C6 alquilo C1-C6, haloalquilo C1-C6, arilo, aril alquilo C1-C6, heteroarilo, heterociclilo, -C(O)OR', -CONR'R", haloalcoxialquilo C1-C4, hidroxi alquilo C1-C6, alcoxi C1-C6, alcanoilo C2-C6, ariloxi alquilo C1-C6, heteroariloxi alquilo C1-C6, alquil-C0-C6-OC(O)NR'R", alquil-C0-C6 -NR'R", hidroxilo, CN, o alquilo-C0-C6-OC(O)-heterociclilo, donde cada grupo arilo, heteroarilo y heterociclilo es sustituido opcionalmente con uno o más grupos que son independientemente halógeno, alquilo C1-C6, alcoxi C1-C6, alcanoilo C1-C6, halo alquilo C1-C4, halo alcoxi C1-C4, -C(O)NR'R", -NR'R", hidroxilo, CN, o -C(O)OR´; o R1 y R1a, o R2 y R2a junto con el carbono al cual se unen forman el grupo cicloalquilo C3-C6 en donde uno de los carbonos es sustituido opcionalmente con un heteroátomo seleccionado entre N, O ó S y en donde dicho anillo puede ser sustituido opcionalmente con alquilo C1-C6; o R1 y R1a, o R2 y R2a junto con el carbono sI cual se unen forman un grupo oxo;R' y R" son independientemente H o alquilo C1-C6; o R' y R" junto con el átomo al cual se unen pueden formar un anillo compuesto por 3-8 miembros que incluye opcionalmente un heteroátomo adicional tal como N, O o S;Y es -SO2-, -SO2-O- o SO2-NR10-; y R10 es H o alquilo C1-C6.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US93184007P | 2007-05-25 | 2007-05-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO6241122A2 true CO6241122A2 (es) | 2011-01-20 |
Family
ID=39679310
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO09147608A CO6241122A2 (es) | 2007-05-25 | 2009-12-24 | Pirazolpirrolidinas como inhibidores de gamma secretasa |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US7977368B2 (es) |
| EP (1) | EP2152713B1 (es) |
| JP (1) | JP2010528036A (es) |
| AR (1) | AR066712A1 (es) |
| AT (1) | ATE523511T1 (es) |
| AU (1) | AU2008256940A1 (es) |
| BR (1) | BRPI0812014A2 (es) |
| CA (1) | CA2687765A1 (es) |
| CL (1) | CL2008001516A1 (es) |
| CO (1) | CO6241122A2 (es) |
| ES (1) | ES2373253T3 (es) |
| MX (1) | MX2009012525A (es) |
| NZ (1) | NZ582039A (es) |
| PE (1) | PE20090280A1 (es) |
| TW (1) | TW200904413A (es) |
| WO (1) | WO2008147800A1 (es) |
| ZA (1) | ZA200908919B (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2009289579A1 (en) * | 2008-09-05 | 2010-03-11 | Elan Pharmaceuticals, Inc. | N-sulfonamido polycyclic pyrazolyl compounds |
| MX2012001520A (es) * | 2009-08-03 | 2012-06-01 | Acraf | Proceso para la preparacion de 1-bencil-3-hidroximetil-1h-indazol y sus derivados e intermediarios de magnesio requeridos. |
| ES2548913T3 (es) | 2009-09-11 | 2015-10-21 | Probiodrug Ag | Derivados heterocíclicos como inhibidores de glutaminil ciclasa |
| US8518945B2 (en) | 2010-03-22 | 2013-08-27 | Hoffmann-La Roche Inc. | Pyrrolopyrazine kinase inhibitors |
| US8481541B2 (en) | 2010-03-22 | 2013-07-09 | Hoffmann-La Roche Inc. | Pyrrolopyrazine kinase inhibitors |
| TWI496785B (zh) | 2010-05-20 | 2015-08-21 | Hoffmann La Roche | 吡咯并吡激酶抑制劑 |
| CN103003281A (zh) | 2010-05-20 | 2013-03-27 | 弗·哈夫曼-拉罗切有限公司 | 作为JAK和SYK抑制剂的吡咯并[2，3-b]吡嗪-7-甲酰胺衍生物和它们的用途 |
| JP6644017B2 (ja) * | 2017-03-30 | 2020-02-12 | 長弘生物科技股▲ふん▼有限公司 | ブチリデンフタリドの用途、その使用方法及びそれを使用して医薬組成物を製造する方法 |
| DK3461819T3 (da) | 2017-09-29 | 2020-08-10 | Probiodrug Ag | Inhibitorer af glutaminylcyklase |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999033785A1 (en) * | 1997-12-27 | 1999-07-08 | Kaneka Corporation | PROCESSES FOR PRODUCING β-HALOGENO-α-AMINO-CARBOXYLIC ACIDS AND PHENYLCYSTEINE DERIVATIVES AND INTERMEDIATES THEREOF |
| US6887898B1 (en) * | 1999-10-22 | 2005-05-03 | Darrick S. H. L. Kim | Pharmaceutical compositions useful in prevention and treatment of beta-Amyloid protein-induced disease |
| US6559174B2 (en) | 2001-03-20 | 2003-05-06 | Merck & Co., Inc. | N-arylsulfonyl aryl aza-bicyclic derivatives as potent cell adhesion inhibitors |
| US7256186B2 (en) | 2002-02-06 | 2007-08-14 | Schering Corporation | Gamma secretase inhibitors |
| 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 |
| BR0312924A (pt) * | 2002-07-25 | 2005-07-12 | Pharmacia Italia Spa | Biciclo-pirazóis ativos como inibidores de quinase, processo para sua preparação e composições farmacêuticas compreendendo os mesmos |
| US20060264380A1 (en) | 2003-07-21 | 2006-11-23 | Mats Hellstrom | Compounds and Methods for Promoting Angiogenesis |
| AU2004276341B2 (en) | 2003-09-23 | 2011-04-14 | Vertex Pharmaceuticals Incorporated | Pyrazolopyrrole derivatives as protein kinase inhibitors |
| WO2007024651A2 (en) * | 2005-08-19 | 2007-03-01 | Elan Pharmaceuticals, Inc. | Bridged n-bicyclic sulfonamido inhibitors of gamma secretase |
| EA014906B1 (ru) * | 2005-12-01 | 2011-02-28 | Элан Фармасьютикалз, Инк. | 5-(арилсульфонил)пиразолопиперидины |
| UY30377A1 (es) | 2006-06-02 | 2008-01-02 | Elan Pharm Inc | Inhibidores triciclicos fusionados de sulfonamida de gama-secretasa |
-
2008
- 2008-05-21 EP EP08756023A patent/EP2152713B1/en active Active
- 2008-05-21 ES ES08756023T patent/ES2373253T3/es active Active
- 2008-05-21 JP JP2010509514A patent/JP2010528036A/ja active Pending
- 2008-05-21 AU AU2008256940A patent/AU2008256940A1/en not_active Abandoned
- 2008-05-21 US US12/124,358 patent/US7977368B2/en not_active Expired - Fee Related
- 2008-05-21 MX MX2009012525A patent/MX2009012525A/es active IP Right Grant
- 2008-05-21 BR BRPI0812014-5A2A patent/BRPI0812014A2/pt not_active Application Discontinuation
- 2008-05-21 AT AT08756023T patent/ATE523511T1/de not_active IP Right Cessation
- 2008-05-21 WO PCT/US2008/064324 patent/WO2008147800A1/en active Application Filing
- 2008-05-21 CA CA002687765A patent/CA2687765A1/en not_active Abandoned
- 2008-05-21 NZ NZ582039A patent/NZ582039A/en not_active IP Right Cessation
- 2008-05-23 CL CL200801516A patent/CL2008001516A1/es unknown
- 2008-05-23 PE PE2008000888A patent/PE20090280A1/es not_active Application Discontinuation
- 2008-05-23 TW TW097119221A patent/TW200904413A/zh unknown
- 2008-05-23 AR ARP080102194A patent/AR066712A1/es not_active Application Discontinuation
-
2009
- 2009-12-15 ZA ZA200908919A patent/ZA200908919B/xx unknown
- 2009-12-24 CO CO09147608A patent/CO6241122A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| PE20090280A1 (es) | 2009-03-19 |
| ZA200908919B (en) | 2010-08-25 |
| US20090099235A1 (en) | 2009-04-16 |
| MX2009012525A (es) | 2009-12-09 |
| EP2152713A1 (en) | 2010-02-17 |
| US7977368B2 (en) | 2011-07-12 |
| ES2373253T3 (es) | 2012-02-01 |
| AU2008256940A1 (en) | 2008-12-04 |
| JP2010528036A (ja) | 2010-08-19 |
| BRPI0812014A2 (pt) | 2014-11-18 |
| ATE523511T1 (de) | 2011-09-15 |
| EP2152713B1 (en) | 2011-09-07 |
| WO2008147800A1 (en) | 2008-12-04 |
| TW200904413A (en) | 2009-02-01 |
| AR066712A1 (es) | 2009-09-09 |
| CL2008001516A1 (es) | 2008-10-10 |
| NZ582039A (en) | 2012-02-24 |
| CA2687765A1 (en) | 2008-12-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Application granted | ||
| FD | Application lapsed |