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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 SUBSTANCES

Info

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
Application number
ARP020101827A
Other languages
Spanish (es)
Inventor
Ceci Angelo Dr
Klinder Klaus Dr
Weiser Thomas Dr
Winter Karin Dr
Original Assignee
Boehringer Ingelheim Pharma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma
Publication of AR036332A1 publication Critical patent/AR036332A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D279/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/021,2-Thiazines; Hydrogenated 1,2-thiazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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

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  • 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.

ARP020101827A 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 AR036332A1 (en)

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)

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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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

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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