AR036332A1 - SUBSTITUTED DERIVATIVES OF NAFTO [1,8-DE] - [1,3] TIAZIN-1,1-DIOXIDE, PROCEDURES FOR PREPARATION, YOUR EMPLOYMENT FOR THE PREPARATION OF A MEDICINAL PRODUCT, AND PHARMACEUTICAL PREPARATIONS CONTAINING SUCH COMPOUNDS IN QUALITY OF ACTIVE SUBSTANCES - Google Patents
SUBSTITUTED DERIVATIVES OF NAFTO [1,8-DE] - [1,3] TIAZIN-1,1-DIOXIDE, PROCEDURES FOR PREPARATION, YOUR EMPLOYMENT FOR THE PREPARATION OF A MEDICINAL PRODUCT, AND PHARMACEUTICAL PREPARATIONS CONTAINING SUCH COMPOUNDS IN QUALITY OF ACTIVE SUBSTANCESInfo
- Publication number
- AR036332A1 AR036332A1 ARP020101827A ARP020101827A AR036332A1 AR 036332 A1 AR036332 A1 AR 036332A1 AR P020101827 A ARP020101827 A AR P020101827A AR P020101827 A ARP020101827 A AR P020101827A AR 036332 A1 AR036332 A1 AR 036332A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- nr6r7
- group
- so2h
- optionally substituted
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/02—1,2-Thiazines; Hydrogenated 1,2-thiazines
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Abstract
Se describen derivados sustituidos de nafto[1,8-de]-[1,3]tiazin-1,1-dióxido, de fórmula general (1), en donde: R1 significa un radical elegido del grupo consistente en hidrógeno, un grupo alquilo C1-6 eventualmente sustituido con uno o varios átomos de halógeno, -SO2H, -SO2- -alquilo C1-6, -SO-alquilo C1-6, -CO-alquiloC1-6, -O, fenil-alquilo C1-4, -alquil C1-4-NR6R7 y -alquil C1-4-O-alquilo C1-4, y cicloalquilo C3-6; R2 y R3, iguales o diferentes, significan un radical elegido del grupo consistente en hidrógeno, un grupo alquilo C1-6 eventualmente sustituido con uno o varios átomos de halógeno, halógeno, -NO2, -SO2H, -SO2-alquilo C1-6, -SO-alquilo C1-6, -CO-alquilo C1-6, -OH, -O-alquilo C1-6, -S-alquilo C1-6, alquil C1-4-NR6R7 y -alquil C1-4-O-alquilo C1-4, y cicloalquilo C3-6; o R1 y R2, juntos, significan un puente de alquileno C4-6; R6, R7, iguales o diferentes, significan hidrógeno, alquilo C1-4 o -CO-alquilo C1-4; R4, iguales o diferentes, significa un radical elegido del grupo consistente en un grupo alquilo C1-6 eventualmente sustituido con uno o varios átomos de halógeno, fenil-alquilo C1-4, halógeno, -CN, -NO2, -SO2H, -SO3H, -SO2-alquilo C1-6, -SO-alquilo C1-6, -SO2-NR6R7, -COOH, -CO-alquilo C1-6, -O-CO-alquilo C1-4, -CO-O-alquilo C1-4, -O-CO-O-alquilo C1-4, -CO-NR6R7, -OH, -O-alquilo C1-6, -S-alquilo C1-6, -NR6R7 y un radical arilo, eventualmente sustituido, una vez o varias veces, con átomos de halógeno, -NO2, -SO2H o alquilo C1-4; R5, iguales o diferentes, significa un radical elegido del grupo consistente en un grupo alquilo C1-6 eventualmente sustituido con uno o varios átomos de halógeno, fenil-alquilo C1-4, halógeno, -CN, -NO2, -SO2H, -SO3H, -SO2-alquilo C1-6, -SO-alquilo C1-6, -SO2-NR6R7, -COOH, -CO-alquilo C1-6, -O-CO-alquilo C1-4, -CO-O-alquilo C1-4, -O-CO-O-alquilo C1-4, -CO-NR6R7, -OH, -O-alquilo C1-6, -S-alquilo C1-6, -NR6R7 y un radical arilo, eventualmente sustituido, una vez o varias veces, con átomos de halógeno, -NO2, -SO2H o alquilo C1-4; y n, m, iguales o diferentes, significan 0, 1, 2 ó 3; con la condición de que esté excluida nafto[1,8-de]-2,3-dihidro-1,1-dióxido-1,2-tiazina, eventualmente en forma de sus distintos enantiómeros y diastereoisómeros, así como sus sales farmacológicamente inocuas. Los compuestos de fórmula (1) son moduladores de receptores AMPA alostéricos positivos. También se describen los preparados farmacéuticos que contienen dichos compuestos en calidad de sustancias activas y el empleo de los mismos para preparar un medicamento destinado al tratamiento y/o la prevención de enfermedades y alteraciones neurodegenerativas o psicóticas, enfermedades de demencia e isquemias cerebrales de diferente génesis, preferentemente la esquizofrenia o los trastornos del aprendizaje y la memoria.Substituted derivatives of naphtho [1,8-de] - [1,3] thiazin-1,1-dioxide, of general formula (1) are described, wherein: R1 means a radical chosen from the group consisting of hydrogen, a group C1-6 alkyl optionally substituted with one or more halogen atoms, -SO2H, -SO2- -C1-6 alkyl, -SO-C1-6 alkyl, -CO-C1-6 alkyl, -O, phenyl-C1-4 alkyl , -C 1-4 alkyl-NR6R7 and -C 1-4 alkyl-O-C 1-4 alkyl, and C 3-6 cycloalkyl; R2 and R3, the same or different, mean a radical chosen from the group consisting of hydrogen, a C1-6 alkyl group optionally substituted with one or more halogen atoms, halogen, -NO2, -SO2H, -SO2-C1-6 alkyl, -SO-C1-6 alkyl, -CO-C1-6 alkyl, -OH, -O-C1-6 alkyl, -S-C1-6 alkyl, C1-4-NR6R7 alkyl and -C1-4-O-alkyl C1-4 alkyl, and C3-6 cycloalkyl; or R1 and R2, together, mean a C4-6 alkylene bridge; R6, R7, the same or different, mean hydrogen, C1-4 alkyl or -CO-C1-4 alkyl; R4, the same or different, means a radical chosen from the group consisting of a C1-6 alkyl group optionally substituted with one or more halogen atoms, phenyl-C1-4 alkyl, halogen, -CN, -NO2, -SO2H, -SO3H , -SO2-C1-6 alkyl, -SO-C1-6 alkyl, -SO2-NR6R7, -COOH, -CO-C1-6 alkyl, -O-CO-C1-4 alkyl, -CO-O-C1 alkyl -4, -O-CO-O-C1-4 alkyl, -CO-NR6R7, -OH, -O-C1-6 alkyl, -S-C1-6 alkyl, -NR6R7 and an aryl radical, optionally substituted, a once or several times, with halogen atoms, -NO2, -SO2H or C1-4 alkyl; R5, the same or different, means a radical chosen from the group consisting of a C1-6 alkyl group optionally substituted with one or more halogen atoms, phenyl-C1-4 alkyl, halogen, -CN, -NO2, -SO2H, -SO3H , -SO2-C1-6 alkyl, -SO-C1-6 alkyl, -SO2-NR6R7, -COOH, -CO-C1-6 alkyl, -O-CO-C1-4 alkyl, -CO-O-C1 alkyl -4, -O-CO-O-C1-4 alkyl, -CO-NR6R7, -OH, -O-C1-6 alkyl, -S-C1-6 alkyl, -NR6R7 and an aryl radical, optionally substituted, a once or several times, with halogen atoms, -NO2, -SO2H or C1-4 alkyl; and n, m, the same or different, mean 0, 1, 2 or 3; with the proviso that naphtho [1,8-de] -2,3-dihydro-1,1-dioxide-1,2-thiazine is excluded, possibly in the form of its various enantiomers and diastereoisomers, as well as its pharmacologically safe salts . The compounds of formula (1) are positive allosteric AMPA receptor modulators. Also described are pharmaceutical preparations containing said compounds as active substances and their use to prepare a medicament for the treatment and / or prevention of neurodegenerative or psychotic diseases and disorders, dementia diseases and cerebral ischemia of different genesis. , preferably schizophrenia or learning and memory disorders.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10123952A DE10123952A1 (en) | 2001-05-17 | 2001-05-17 | New naphtho-1,2-thiazine compounds, useful as neuroprotectants for treating e.g. epilepsy or Alzheimer's disease, are allosteric modulators of AMPA receptors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR036332A1 true AR036332A1 (en) | 2004-09-01 |
Family
ID=7685080
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020101827A AR036332A1 (en) | 2001-05-17 | 2002-05-17 | SUBSTITUTED DERIVATIVES OF NAFTO [1,8-DE] - [1,3] TIAZIN-1,1-DIOXIDE, PROCEDURES FOR PREPARATION, YOUR EMPLOYMENT FOR THE PREPARATION OF A MEDICINAL PRODUCT, AND PHARMACEUTICAL PREPARATIONS CONTAINING SUCH COMPOUNDS IN QUALITY OF ACTIVE SUBSTANCES |
Country Status (26)
| Country | Link |
|---|---|
| EP (1) | EP1404340A1 (en) |
| JP (1) | JP2004529980A (en) |
| KR (1) | KR20040007572A (en) |
| CN (1) | CN1533278A (en) |
| AR (1) | AR036332A1 (en) |
| BG (1) | BG108324A (en) |
| BR (1) | BR0209796A (en) |
| CA (1) | CA2449189A1 (en) |
| CO (1) | CO5550460A2 (en) |
| CZ (1) | CZ20033112A3 (en) |
| DE (1) | DE10123952A1 (en) |
| EA (1) | EA006608B1 (en) |
| EC (1) | ECSP034852A (en) |
| EE (1) | EE200300566A (en) |
| HR (1) | HRP20030933A2 (en) |
| HU (1) | HUP0401273A3 (en) |
| IL (1) | IL158642A0 (en) |
| MX (1) | MXPA03010373A (en) |
| NO (1) | NO20035088L (en) |
| NZ (1) | NZ530154A (en) |
| PL (1) | PL364053A1 (en) |
| SK (1) | SK14222003A3 (en) |
| UY (1) | UY27290A1 (en) |
| WO (1) | WO2002100411A1 (en) |
| YU (1) | YU90403A (en) |
| ZA (1) | ZA200308466B (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8039468B2 (en) * | 2006-08-31 | 2011-10-18 | The Governors Of The University Of Alberta | Method of inhibition of respiratory depression using positive allosteric AMPA receptor modulators |
| CN111518058B (en) * | 2020-05-29 | 2021-03-09 | 四川大学华西医院 | Oxathiazine compound and application thereof |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU4345297A (en) * | 1996-09-17 | 1998-04-14 | Regents Of The University Of California, The | Benzothiadiazide derivatives and their use as allosteric up-modulators of the ampa receptor |
| US6346526B1 (en) * | 1998-06-25 | 2002-02-12 | Merck & Co., Inc. | Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment |
| DE10004572A1 (en) * | 2000-02-02 | 2001-08-09 | Boehringer Ingelheim Pharma | New positive allosteric AMPA receptor modulators (PAARM), processes for their production and their use as medicines |
-
2001
- 2001-05-17 DE DE10123952A patent/DE10123952A1/en not_active Withdrawn
-
2002
- 2002-05-15 IL IL15864202A patent/IL158642A0/en unknown
- 2002-05-15 MX MXPA03010373A patent/MXPA03010373A/en unknown
- 2002-05-15 NZ NZ530154A patent/NZ530154A/en unknown
- 2002-05-15 PL PL02364053A patent/PL364053A1/en not_active Application Discontinuation
- 2002-05-15 BR BR0209796-6A patent/BR0209796A/en not_active IP Right Cessation
- 2002-05-15 CZ CZ20033112A patent/CZ20033112A3/en unknown
- 2002-05-15 CA CA002449189A patent/CA2449189A1/en not_active Abandoned
- 2002-05-15 KR KR10-2003-7014965A patent/KR20040007572A/en not_active Withdrawn
- 2002-05-15 EP EP02750931A patent/EP1404340A1/en not_active Withdrawn
- 2002-05-15 YU YU90403A patent/YU90403A/en unknown
- 2002-05-15 EA EA200301167A patent/EA006608B1/en not_active IP Right Cessation
- 2002-05-15 JP JP2003503232A patent/JP2004529980A/en not_active Abandoned
- 2002-05-15 WO PCT/EP2002/005338 patent/WO2002100411A1/en not_active Ceased
- 2002-05-15 EE EEP200300566A patent/EE200300566A/en unknown
- 2002-05-15 HR HR20030933A patent/HRP20030933A2/en not_active Application Discontinuation
- 2002-05-15 CN CNA028100832A patent/CN1533278A/en active Pending
- 2002-05-15 HU HU0401273A patent/HUP0401273A3/en unknown
- 2002-05-15 SK SK1422-2003A patent/SK14222003A3/en unknown
- 2002-05-15 UY UY27290A patent/UY27290A1/en not_active Application Discontinuation
- 2002-05-17 AR ARP020101827A patent/AR036332A1/en unknown
-
2003
- 2003-10-30 ZA ZA200308466A patent/ZA200308466B/en unknown
- 2003-11-07 BG BG108324A patent/BG108324A/en unknown
- 2003-11-14 NO NO20035088A patent/NO20035088L/en not_active Application Discontinuation
- 2003-11-17 EC EC2003004852A patent/ECSP034852A/en unknown
- 2003-12-01 CO CO03105591A patent/CO5550460A2/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| NO20035088D0 (en) | 2003-11-14 |
| KR20040007572A (en) | 2004-01-24 |
| YU90403A (en) | 2006-05-25 |
| WO2002100411A1 (en) | 2002-12-19 |
| HUP0401273A3 (en) | 2006-11-28 |
| EA200301167A1 (en) | 2004-06-24 |
| NO20035088L (en) | 2003-11-14 |
| ZA200308466B (en) | 2004-05-24 |
| HUP0401273A2 (en) | 2004-10-28 |
| SK14222003A3 (en) | 2004-05-04 |
| BR0209796A (en) | 2004-06-01 |
| CZ20033112A3 (en) | 2004-03-17 |
| JP2004529980A (en) | 2004-09-30 |
| CA2449189A1 (en) | 2002-12-19 |
| EA006608B1 (en) | 2006-02-24 |
| EP1404340A1 (en) | 2004-04-07 |
| BG108324A (en) | 2004-12-30 |
| HRP20030933A2 (en) | 2004-04-30 |
| CN1533278A (en) | 2004-09-29 |
| MXPA03010373A (en) | 2004-03-16 |
| CO5550460A2 (en) | 2005-08-31 |
| UY27290A1 (en) | 2002-12-31 |
| IL158642A0 (en) | 2004-05-12 |
| EE200300566A (en) | 2004-02-16 |
| NZ530154A (en) | 2005-09-30 |
| PL364053A1 (en) | 2004-12-13 |
| ECSP034852A (en) | 2003-12-24 |
| DE10123952A1 (en) | 2002-11-21 |
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