EP0380217A1
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Bis-aza-bicyclic anxiolytic agents and antidepressants
Assignee: Pfizer Inc
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Filing: 1990-01-12
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Granted: —
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Expires: 2010-01-12
Abstract
Abstract An anxiolytic or antidepressant which is a racemic or optically active compound of the formula or a pharmaceutically acceptable acid addition salt thereof, wherein X is N or CH; Y is Z is SCH₂, OCH₂, -Y¹(CH₂) n or Y¹(CH₂) n substituted on carbon with up to 2 methyl groups; n is 1 or 2; and Y¹ is CH₂, NH or NCH₃.
Inventors
- 👤 Kishor Amratral Desai
- 👤 Gene Michael Bright
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-09 10:08
CPC Classifications
C; C07; C07D; C07D471/00; C07D471/02; C07D471/04; A; A61; A61P; A61P25/00; A61P25/20; A61P25/24; A61P25/26
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
163 words
A process for a racemic or optically active compound of the formula or a pharmaceutically acceptable acid addition salt thereof, wherein X is N or CH; Y is Z is SCH₂, OCH₂, -Y¹(CH₂) n or Y¹(CH₂) n substituted on carbon with up to 2 methyl groups; n is 1 or 2; and Y¹ is CH₂, NH or NCH₃; which comprises reacting a racemic or optically active compound of the formula wherein X is N or CH; Y⁴ is HO-, RSO₂O-, or H₂N-; and R is (C₁-C₃)alkyl, phenyl or tolyl; (a) when Y⁴ is HO-, with a compound YH, wherein Y is as defined above, in the presence of a coupling reagent which is an approximately 1:1 molar mixture of diethyl azodicarboxylate and triphenylphosphine; (b) when Y⁴ is RSO₂O-, with an anion of the formula Y⁻ formed by the action of a base on a compound YH; or (c) when Y⁴ is H₂N- and Y is an imide, with an anhydride of the formula
Claim 2
Dependent Claim
163 words
A process for a racemic or optically active compound of the formula or a pharmaceutically acceptable acid addition salt thereof, wherein X is N or CH; Y is Z is SCH₂, OCH₂, -Y¹(CH₂) n or Y¹(CH₂) n substituted on carbon with up to 2 methyl groups; n is 1 or 2; and Y¹ is CH₂, NH or NCH₃; which comprises reacting a racemic or optically active compound of the formula wherein X is N or CH; Y⁴ is HO-, RSO₂O-, or H₂N-; and R is (C₁-C₃)alkyl, phenyl or tolyl; (a) when Y⁴ is HO-, with a compound YH, wherein Y is as defined above, in the presence of a coupling reagent which is an approximately 1:1 molar mixture of diethyl azodicarboxylate and triphenylphosphine; (b) when Y⁴ is RSO₂O-, with an anion of the formula Y⁻ formed by the action of a base on a compound YH; or (c) when Y⁴ is H₂N- and Y is an imide, with an anhydride of the formula
Claim 3
Dependent Claim
12 words
A process of claim 1 wherein X is N and Y is
Claim 4
Dependent Claim
16 words
A process of claim 1 or 2 for an optically active compound of the formula (I).
Claim 5
Dependent Claim
22 words
A process of claim 3 wherein Z is Y¹(CH₂) n or Y¹(CH₂) n substituted on carbon with up to 2 methyl groups.
Claim 6
Dependent Claim
18 words
The process of claim 4 wherein Z is Y¹(CH₂) n , Y¹ is CH₂ and n is 1.
Claim 7
Dependent Claim
8 words
A process of claim 1 wherein Y is
Claim 8
Dependent Claim
12 words
A process of claim 1 wherein X is CH and Y is
References Cited (Backward Citations)
US3388128A
Cited
US4182763A
Cited
EP0107825A1
Cited
DE3321969A1
Cited
WO1987005022A2
Cited
US4788290A
Cited
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