PE20090953A1 - Sulfonas ciclicas sustituidas por amino-bencilo utiles como inhibidores de bace - Google Patents
Sulfonas ciclicas sustituidas por amino-bencilo utiles como inhibidores de baceInfo
- Publication number
- PE20090953A1 PE20090953A1 PE2008001440A PE2008001440A PE20090953A1 PE 20090953 A1 PE20090953 A1 PE 20090953A1 PE 2008001440 A PE2008001440 A PE 2008001440A PE 2008001440 A PE2008001440 A PE 2008001440A PE 20090953 A1 PE20090953 A1 PE 20090953A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- amino
- benzyl
- halo
- halogen
- Prior art date
Links
- -1 AMINO-BENZYL Chemical group 0.000 title abstract 5
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 150000003457 sulfones Chemical group 0.000 title abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 2
- VXNQJPMCJMJOMN-UHFFFAOYSA-N 1,1-difluoroethane Chemical class C[C](F)F VXNQJPMCJMJOMN-UHFFFAOYSA-N 0.000 abstract 1
- 101000740162 Homo sapiens Sodium- and chloride-dependent transporter XTRP3 Proteins 0.000 abstract 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 102100037189 Sodium- and chloride-dependent transporter XTRP3 Human genes 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- CFHIDWOYWUOIHU-UHFFFAOYSA-N oxomethyl Chemical compound O=[CH] CFHIDWOYWUOIHU-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
- C07D335/02—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
-
- 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
- A61P25/28—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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
REFRIDA A UN DERIVADO SULFONA DE FORMULA (I), DONDE R1 ES H, HALOGENO, ALQUILO C1-C8; R2 ES H, HALOGENO, ALQUILO C1-C8, HALO-ALQUILO C1-C8, ENTRE OTROS; R3 ES H, HALO-ALQUILO C1-C8, HIDROXI-ALQUILO C1-C8, ENTRE OTROS; R4 ES H, ALQUILO C1-C8, FORMILO, ENTRE OTROS; R5 ES H, HALOGENO, ALQUILO C1-C8, ALQUENILO C2-C8, ENTRE OTROS; R6 ES OXO O ESTA AUSENTE; R7 ESTA AUSENTE O ES OXO, IMINO, BENCIL-IMINO, FORMIL-IMINO, ENTRE OTROS; R8 ES H, ALQUILO C1-C8, HIDROXI-ALQUILO C1-C8, HALO-ALQUILO C1-C8, ENTRE OTROS; R9 ES H, ALQUILO C1-C8, HALO-ALQUILO C1-C8, ENTRE OTROS; R10 ES UN GRUPO ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDO CON HALOGENO, OH, ALQUILO C1-C8, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: CLORHIDRATO DE (3S*,4S*,5R*)-3-(4-AMINO-3-FLUORO-BENCIL)-5-(3-TERBUTIL-BENCIL-AMINO)-1,1-DIOXO-HEXAHIDRO-1LAMBDA*6*-TIOPIRAN-4-OL, (3S,4S,5R)-3-(4-AMINO-3-BROMO-5-FLUORO-BENCIL)-5-[3-(1,1-DIFLUORO-ETIL)-BENCIL-AMINO]-1,1-DIOXO-HEXAHIDRO-1LAMBDA*6*-TIOPIRAN-4-OL, (3S,4S,5R)-3-(4-AMINO-3-BROMO-5-FLUORO-BENCIL)-5-[3-(2,2-DIMETIL-PROPIL)-BENCIL-AMINO]-1,1-DIOXO-HEXAHIDRO-1LAMBDA*6*-TIOPIRAN-4-OL, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE BACE Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES NEURODEGENERATIVAS, TRANSTORNOS NEUROLOGICOS, ENTRE OTRAS
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07114881 | 2007-08-23 | ||
| EP08160123 | 2008-07-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20090953A1 true PE20090953A1 (es) | 2009-08-10 |
Family
ID=39789883
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008001440A PE20090953A1 (es) | 2007-08-23 | 2008-08-25 | Sulfonas ciclicas sustituidas por amino-bencilo utiles como inhibidores de bace |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20090054427A1 (es) |
| EP (1) | EP2190833A1 (es) |
| JP (1) | JP2010536831A (es) |
| KR (1) | KR20100061805A (es) |
| CN (1) | CN101835771A (es) |
| AR (1) | AR068062A1 (es) |
| AU (1) | AU2008290561A1 (es) |
| BR (1) | BRPI0815673A2 (es) |
| CA (1) | CA2697254A1 (es) |
| CL (1) | CL2008002480A1 (es) |
| EA (1) | EA201000340A1 (es) |
| MX (1) | MX2010002007A (es) |
| PE (1) | PE20090953A1 (es) |
| TW (1) | TW200916097A (es) |
| WO (1) | WO2009024615A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011527311A (ja) * | 2008-07-10 | 2011-10-27 | ノバルティス アーゲー | Ｂａｃｅ阻害薬として有用なアミノベンジル置換環状スルホン誘導体 |
| US9066948B2 (en) | 2010-07-16 | 2015-06-30 | The United States Of America As Represented By The Secretary, Department Of Health And Human Services | Oxadiazolo[3,2-a]pyrimidines and thiadiazolo[3,2-a]pyrimidines |
| US9242943B2 (en) * | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| EP2804610B1 (en) | 2012-01-16 | 2018-10-31 | The Rockefeller University | Organic compounds |
| US10202355B2 (en) | 2013-02-12 | 2019-02-12 | Buck Institute For Research On Aging | Hydantoins that modulate bace-mediated app processing |
| CN106674264A (zh) * | 2016-12-20 | 2017-05-17 | 苏州汉德创宏生化科技有限公司 | (2,2,2‑三氟乙氧基)苯硼酸类化合物的合成方法 |
| EP3810134A4 (en) | 2018-06-19 | 2022-03-30 | Celecor Therapeutics, Inc. | DEUTERED RUC-4 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0888325B1 (en) * | 1996-02-07 | 2002-05-29 | Warner-Lambert Company | Novel cyclic amino acids as pharmaceutical agents |
| AU759392B2 (en) * | 1997-12-16 | 2003-04-10 | Warner-Lambert Company | 4(3)substituted-4(3)-aminomethyl-(thio)pyran or -piperidine derivatives (=gabapentin analogues), their preparation and their use in the treatment of neurological disorders |
| GB0602951D0 (en) * | 2006-02-14 | 2006-03-29 | Novartis Ag | Organic Compounds |
-
2008
- 2008-08-22 MX MX2010002007A patent/MX2010002007A/es not_active Application Discontinuation
- 2008-08-22 US US12/196,461 patent/US20090054427A1/en not_active Abandoned
- 2008-08-22 CA CA2697254A patent/CA2697254A1/en not_active Abandoned
- 2008-08-22 JP JP2010521442A patent/JP2010536831A/ja active Pending
- 2008-08-22 WO PCT/EP2008/061030 patent/WO2009024615A1/en not_active Ceased
- 2008-08-22 AU AU2008290561A patent/AU2008290561A1/en not_active Abandoned
- 2008-08-22 KR KR1020107006213A patent/KR20100061805A/ko not_active Withdrawn
- 2008-08-22 EP EP08787429A patent/EP2190833A1/en not_active Withdrawn
- 2008-08-22 EA EA201000340A patent/EA201000340A1/ru unknown
- 2008-08-22 BR BRPI0815673-5A2A patent/BRPI0815673A2/pt not_active Application Discontinuation
- 2008-08-22 CL CL2008002480A patent/CL2008002480A1/es unknown
- 2008-08-22 CN CN200880112386A patent/CN101835771A/zh active Pending
- 2008-08-25 AR ARP080103691A patent/AR068062A1/es unknown
- 2008-08-25 TW TW097132452A patent/TW200916097A/zh unknown
- 2008-08-25 PE PE2008001440A patent/PE20090953A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| US20090054427A1 (en) | 2009-02-26 |
| BRPI0815673A2 (pt) | 2015-02-18 |
| EA201000340A1 (ru) | 2010-08-30 |
| AU2008290561A1 (en) | 2009-02-26 |
| WO2009024615A1 (en) | 2009-02-26 |
| CN101835771A (zh) | 2010-09-15 |
| KR20100061805A (ko) | 2010-06-09 |
| CA2697254A1 (en) | 2009-02-26 |
| AR068062A1 (es) | 2009-11-04 |
| CL2008002480A1 (es) | 2009-05-15 |
| JP2010536831A (ja) | 2010-12-02 |
| EP2190833A1 (en) | 2010-06-02 |
| TW200916097A (en) | 2009-04-16 |
| MX2010002007A (es) | 2010-03-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |