Title:
DEALKYLATED DERIVATIVES OF PYRROLO[2,1-B]BENZOTHIAZEPINES WITH ATYPICAL ANTIPSYCHOTIC ACTIVITY
Document Type and Number:
WIPO Patent Application WO2005108403
Kind Code:
A3
Abstract:
Derivatives of pyrrolo[2,1-b]benzothiazepines with formula (I) where A is CH-CH2C=CH; R is hydrogen, halogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, C5-C6 cycloalkyl; R1 is 1-peperazinyl, 1-homopiperazinyl and 1-piperidinyl; R2 is hydrogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, CHO, CH=NOH,CH2OH. The formula (I) compounds are endowed with characteristic atypical anti-psychotic activity, and are therefore useful as medicaments, in particular for the treatment and prevention of schizophrenia, paranoid states, manic-depressive states, disorders of the affective sphere, social regression, personality regression, and hallucinations. Said compounds also present advantageous pharmacokinetic properties.
Inventors:
MINETTI PATRIZIA (IT)
DI CESARE MARIA ASSUNTA (IT)
GHIRARDI ORLANDO (IT)
TINTI MARIA ORNELLA (IT)
CARMINATI PAOLO (IT)
DI CESARE MARIA ASSUNTA (IT)
GHIRARDI ORLANDO (IT)
TINTI MARIA ORNELLA (IT)
CARMINATI PAOLO (IT)
Application Number:
PCT/IT2005/000246
Publication Date:
December 29, 2005
Filing Date:
April 28, 2005
Export Citation:
Assignee:
SIGMA TAU IND FARMACEUTI (IT)
MINETTI PATRIZIA (IT)
DI CESARE MARIA ASSUNTA (IT)
GHIRARDI ORLANDO (IT)
TINTI MARIA ORNELLA (IT)
CARMINATI PAOLO (IT)
MINETTI PATRIZIA (IT)
DI CESARE MARIA ASSUNTA (IT)
GHIRARDI ORLANDO (IT)
TINTI MARIA ORNELLA (IT)
CARMINATI PAOLO (IT)
International Classes:
A61K31/407; C07D513/00; C07D513/04; (IPC1-7): C07D513/04; A61K31/407
Domestic Patent References:
| WO2002010175A1 | 2002-02-07 | |||
| WO2000006579A2 | 2000-02-10 |
Other References:
CAMPIANI, GIUSEPPE ET AL: "Pyrrolo[1,3]benzothiazepine-Based Serotonin and Dopamine Receptor Antagonists. Molecular Modeling, Further Structure-Activity Relationship Studies, and Identification of Novel Atypical Antipsychotic Agents", JOURNAL OF MEDICINAL CHEMISTRY , 47(1), 143-157 CODEN: JMCMAR; ISSN: 0022-2623, 2004, XP002354023
CAMPIANI, GIUSEPPE ET AL: "Pyrrolo[1,3]benzothiazepine-Based Atypical Antipsychotic Agents. Synthesis, Structure-Activity Relationship, Molecular Modeling, and Biological Studies", JOURNAL OF MEDICINAL CHEMISTRY , 45(2), 344-359 CODEN: JMCMAR; ISSN: 0022-2623, 2002, XP002354024
CAMPIANI, GIUSEPPE ET AL: "New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure", JOURNAL OF MEDICINAL CHEMISTRY , 41(20), 3763-3772 CODEN: JMCMAR; ISSN: 0022-2623, 1998, XP002354025
CAMPIANI, GIUSEPPE ET AL: "Pyrrolo[1,3]benzothiazepine-Based Atypical Antipsychotic Agents. Synthesis, Structure-Activity Relationship, Molecular Modeling, and Biological Studies", JOURNAL OF MEDICINAL CHEMISTRY , 45(2), 344-359 CODEN: JMCMAR; ISSN: 0022-2623, 2002, XP002354024
CAMPIANI, GIUSEPPE ET AL: "New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure", JOURNAL OF MEDICINAL CHEMISTRY , 41(20), 3763-3772 CODEN: JMCMAR; ISSN: 0022-2623, 1998, XP002354025
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