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Details for Patent: 5,468,743

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Patent 5,468,743 protects LASTACAFT and is included in one NDA. There has been one Paragraph IV challenge on Lastacaft.

This patent has forty-four patent family members in thirty countries.

Summary for Patent: 5,468,743

Title: Imidazo[2,1-b]benzazepine derivatives, compositions and method of use
Abstract:The present invention is concerned with novel imidazo[2, 1-b][3]benzazepines of formula ##STR1## the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; R.sup.1 represents hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 alkyloxy; R.sup.2 represents hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 alkyloxy; R.sup.3 represents hydrogen, C.sub.1-4 alkyl, ethenyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxyC.sub.1-4 alkyl, formyl or hydroxycarbonyl; R.sup.4 represents hydrogen, C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl, phenyl or halo; R.sup.5 represents hydrogen, C.sub.1-4 alkyl or halo; L represents hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C.sub.1-4 alkyloxy, hydroxycarbonyl, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyloxycarbonyl-C.sub.1-4 alkyloxy, hydroxycarbonylC.sub.1-4 alkyloxy, C.sub.1-4 alkyloxycarbonylamino, C.sub.1-4 alkylaminocarbonyl, C.sub.1-4 alkylaminocarbonylamino, C.sub.1-4 alkylaminothiocarbonylamino, aryl, aryloxy and arylcarbonyl; C.sub.1-6 alkyl substituted with both hydroxy and aryloxy; C.sub.3-6 alkenyl; C.sub.3-6 alkenyl substituted with aryl; or, L represents a radical of formula --Alk--Y--Het.sup.1 (a-1),--Alk--NH--CO--Het.sup.2 (a-2)or --Alk--Het.sup.3 (a-3); provided that 6,11-dihydro-11-(4-piperidinylidene)-5H-imidazo[2,1-b][3]benzazepine is ecxluded, which are useful antiallergic compounds. Compositions comprising said compounds, methods of using and processes for preparing the same.
Inventor(s): Janssens; Frans E. (Bonheiden, BE), Diels; Gaston S. M. (Ravels, BE), Leenaerts; Joseph E. (Rijkevorsel, BE)
Assignee: Janssen Pharmaceutica N.V. (Beerse, BE)
Application Number:08/142,474
Patent Claim Types:
see list of patent claims
Compound; Composition; Use;
Patent PDF download available with subscription

Applicant Tradename Generic Name Dosage NDA Approval Date Type RLD Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use
Allergan
LASTACAFT
alcaftadine
SOLUTION/DROPS;OPHTHALMIC022134-001Jul 28, 2010RXYes5,468,743<disabled>YY
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Foreign Priority and PCT Information for Patent: 5,468,743

PCT Information
PCT FiledJune 09, 1992PCT Application Number:PCT/EP92/01330
PCT Publication Date:December 23, 1992PCT Publication Number: WO92/22551

International Patent Family for Patent: 5,468,743

Country Document Number Publication Date Supplementary Protection Certificate SPC Country SPC Expiration
Poland170771Jan 31, 1997
Yugoslavia61292Sep 09, 1994
Norway934492Dec 09, 1993
South Africa9204326Dec 13, 1993
Singapore47823Apr 17, 1998
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Preferred citation:

Friedman, Y. Location of pharmaceutical innovation: 2000–2009 Nature Reviews Drug Discovery 9, 835–836 (2010).

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