PE20090280A1 - Pirazol-pirrolidinas como inhibidores de gamma secretasa - Google Patents
Pirazol-pirrolidinas como inhibidores de gamma secretasaInfo
- Publication number
- PE20090280A1 PE20090280A1 PE2008000888A PE2008000888A PE20090280A1 PE 20090280 A1 PE20090280 A1 PE 20090280A1 PE 2008000888 A PE2008000888 A PE 2008000888A PE 2008000888 A PE2008000888 A PE 2008000888A PE 20090280 A1 PE20090280 A1 PE 20090280A1
- Authority
- PE
- Peru
- Prior art keywords
- pyrazole
- pyrrolidines
- gamma secretase
- secretase inhibitors
- phenylsulfonil
- Prior art date
Links
- 239000003540 gamma secretase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Substances C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 3
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical group F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 abstract 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 abstract 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 abstract 1
- DZHSAHHDTRWUTF-SIQRNXPUSA-N amyloid-beta polypeptide 42 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(C)C)C1=CC=CC=C1 DZHSAHHDTRWUTF-SIQRNXPUSA-N 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical group F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
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)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
REFERIDA A UN COMPUESTO DERIVADO DE PIRAZOL-PIRROLIDINA DE FORMULA (I), DONDE A ES ALQUILO C1-C6, CILCOALQUILO C3-C6, ARILO, ENTRE OTROS; R1, R1a, R2 Y R2a SON H, ALQUILO C1-C6, ALQUENILO C2-C6, CICLOALQUILO C3-C6, ENTRE OTROS; Y ES SO2, SO2-O, SO2-NR10. SON COMPUESTOS PREFERIDOS: 4-CICLOPROPILO-6-(FLUOROMETIL)-5-(4-(TRIFLUOROMETIL)FENILSULFONIL)-1,4,5,6-TETRAHIDROPIRROLO[3,4-c]PIRAZOL, 5-(4-CLOROFENILSULFONIL)-1,4,5,6-TETRAHIDROPIRROLO[3,4-c]PIRAZOL, 4,6-DICICLOPROPILO-5-(4-(TRIFLUOROMETIL)FENILSULFONIL)-1,4,5,6-TETRAHIDROPIRROLO[3,4-c]PIRAZOL, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN LA LIBERACION DE GAMMA-SECRETASA Y EL PEPTIDO BETA-AMILOIDE Y SON UTILES EN EL TRATAMIENTO DE TRANSTORNOS COGNITIVOS, PARTICULARMENTE, LA ENFERMEDAD DE ALZHEIMER
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US93184007P | 2007-05-25 | 2007-05-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20090280A1 true PE20090280A1 (es) | 2009-03-19 |
Family
ID=39679310
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008000888A PE20090280A1 (es) | 2007-05-25 | 2008-05-23 | Pirazol-pirrolidinas 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 |
|---|---|---|---|---|
| TW201014856A (en) * | 2008-09-05 | 2010-04-16 | Elan Pharm Inc | N-sulfonamido polycyclic pyrazolyl compounds |
| US8350052B2 (en) * | 2009-08-03 | 2013-01-08 | Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. | Process for the preparation of 1-benzyl-3-hydroxymethyl-1H-indazole and its derivatives and required magnesium intermediates |
| ES2548913T3 (es) | 2009-09-11 | 2015-10-21 | Probiodrug Ag | Derivados heterocíclicos como inhibidores de glutaminil ciclasa |
| US8481541B2 (en) | 2010-03-22 | 2013-07-09 | Hoffmann-La Roche Inc. | Pyrrolopyrazine kinase inhibitors |
| US8518945B2 (en) | 2010-03-22 | 2013-08-27 | Hoffmann-La Roche Inc. | Pyrrolopyrazine kinase inhibitors |
| RU2012152352A (ru) | 2010-05-20 | 2014-06-27 | Ф. Хоффманн-Ля Рош Аг | ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-b]ПИРАЗИН-7-КАРБОКСАМИДА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ JAK И SYK |
| EP2571881A1 (en) | 2010-05-20 | 2013-03-27 | F.Hoffmann-La Roche Ag | Pyrrolopyrazine derivatives as syk and jak inhibitors |
| 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 |
| EP3461819B1 (en) | 2017-09-29 | 2020-05-27 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999033785A1 (fr) * | 1997-12-27 | 1999-07-08 | Kaneka Corporation | PROCEDES POUR PRODUIRE DES ACIDES β-HALOGENO-α-AMINOCARBOXYLIQUES AINSI QUE DES DERIVES DE PHENYLCYSTEINE ET LEURS INTERMEDIAIRES |
| 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 |
| US20040171614A1 (en) * | 2002-02-06 | 2004-09-02 | Schering-Plough Corporation | Novel gamma secretase inhibitors |
| TW200302717A (en) * | 2002-02-06 | 2003-08-16 | Schering Corp | Novel gamma secretase inhibitors |
| CA2493625A1 (en) * | 2002-07-25 | 2004-02-19 | Pharmacia Italia S.P.A. | Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| US20060264380A1 (en) * | 2003-07-21 | 2006-11-23 | Mats Hellstrom | Compounds and Methods for Promoting Angiogenesis |
| WO2005030776A1 (en) * | 2003-09-23 | 2005-04-07 | Vertex Pharmaceuticals Incorporated | Pyrazolopyrrole derivatives as protein kinase inhibitors |
| JP2009506988A (ja) | 2005-08-19 | 2009-02-19 | 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 | ガンマセクレターゼの架橋ｎ−環状スルホンアミド阻害剤 |
| KR20080073359A (ko) * | 2005-12-01 | 2008-08-08 | 엘란 파마슈티칼스, 인크. | 5(아릴설포닐)피라졸로피페리딘 |
| UY30377A1 (es) | 2006-06-02 | 2008-01-02 | Elan Pharm Inc | Inhibidores triciclicos fusionados de sulfonamida de gama-secretasa |
-
2008
- 2008-05-21 ES ES08756023T patent/ES2373253T3/es active Active
- 2008-05-21 NZ NZ582039A patent/NZ582039A/en not_active IP Right Cessation
- 2008-05-21 US US12/124,358 patent/US7977368B2/en not_active Expired - Fee Related
- 2008-05-21 AU AU2008256940A patent/AU2008256940A1/en not_active Abandoned
- 2008-05-21 WO PCT/US2008/064324 patent/WO2008147800A1/en not_active Ceased
- 2008-05-21 EP EP08756023A patent/EP2152713B1/en active Active
- 2008-05-21 JP JP2010509514A patent/JP2010528036A/ja active Pending
- 2008-05-21 CA CA002687765A patent/CA2687765A1/en not_active Abandoned
- 2008-05-21 BR BRPI0812014-5A2A patent/BRPI0812014A2/pt not_active Application Discontinuation
- 2008-05-21 MX MX2009012525A patent/MX2009012525A/es active IP Right Grant
- 2008-05-21 AT AT08756023T patent/ATE523511T1/de not_active IP Right Cessation
- 2008-05-23 PE PE2008000888A patent/PE20090280A1/es not_active Application Discontinuation
- 2008-05-23 AR ARP080102194A patent/AR066712A1/es not_active Application Discontinuation
- 2008-05-23 TW TW097119221A patent/TW200904413A/zh unknown
- 2008-05-23 CL CL200801516A patent/CL2008001516A1/es unknown
-
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 |
|---|---|
| CL2008001516A1 (es) | 2008-10-10 |
| TW200904413A (en) | 2009-02-01 |
| JP2010528036A (ja) | 2010-08-19 |
| AR066712A1 (es) | 2009-09-09 |
| NZ582039A (en) | 2012-02-24 |
| MX2009012525A (es) | 2009-12-09 |
| CA2687765A1 (en) | 2008-12-04 |
| EP2152713A1 (en) | 2010-02-17 |
| BRPI0812014A2 (pt) | 2014-11-18 |
| EP2152713B1 (en) | 2011-09-07 |
| CO6241122A2 (es) | 2011-01-20 |
| WO2008147800A1 (en) | 2008-12-04 |
| ZA200908919B (en) | 2010-08-25 |
| US7977368B2 (en) | 2011-07-12 |
| ES2373253T3 (es) | 2012-02-01 |
| US20090099235A1 (en) | 2009-04-16 |
| ATE523511T1 (de) | 2011-09-15 |
| AU2008256940A1 (en) | 2008-12-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |