1, 5-benzodiazepine derivatives

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United States of America Patent

PATENT NO 5733867
SERIAL NO

08578534

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Compounds of general formula (I) ##STR1## wherein R.sup.1 represents a phenyl, C.sub.3-7 cycloalkyl, C.sub.7-11 bridgedcycloalkyl or C.sub.1-6 alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C.sub.1-6 alkoxycarbonyl, C.sub.3-7 cycloalkyl, or C.sub.3-7 bridgedcycloalkyl group; R.sup.2 represents phenyl substituted by a group (CH.sub.2).sub.n NR.sup.4 R.sup.5, O(CH.sub.2).sub.p R.sup.6, or (CH.sub.2).sub.n CO.sub.2 R.sup.11 ; R.sup.3 represents phenyl optionally substituted by one or 2 halogen atoms; R.sup.4 represents hydrogen or C.sub.1-4 alkyl; R.sup.5 represents acyl, or C.sub.2-4 alkyl substituted by one or more hydroxy; carboxyl and/or amino groups or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form a 5-7 saturated heterocyclic ring which contain an additional heteroatom selected from oxygen, sulphur or nitrogen and/or may be substituted by 1 or 2 C.sub.1-4 alkyl or hydroxy groups. R.sup.6 represents hydroxy, C.sub.1-4 alkoxy, CO.sub.2 R.sup.7 or NR.sup.8 R.sup.9 ; R.sup.7 represents hydrogen or C.sub.1-4 alkyl or a metabolically labile ester group; R.sup.8 represents hydrogen, C.sub.1-4, acyl or C.sub.2-6 alkyl substituted by one or more hydroxy, carboxyl and/or amino groups or R.sup.8 and R.sup.9 together with the nitrogen atom to which they are attached form a 5-7 saturated heterocyclic ring which contain an additional heteroatom selected from oxygen, sulphur or nitrogen and/or may be substituted by 1 or 2 C.sub.1-4 alkyl or hydroxy groups; R.sup.10 represents hydrogen or a halogen atom; R.sup.11 represents a metabolically labile ester group; m is zero, 1 or 2; n is zero or 1; p is an integer from 1 to 4; X represents oxygen or NH and pharmaceutically acceptable, salts thereof are antagonists of gastrin and CCK.

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Patent Owner(s)

Patent OwnerAddress
GLAXO SPAVIA ALESSANDRO FLEMING 2 37100 VERONA

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Curotto, Giovanni Verona, IT 1 0
Pellegatti, Mario Verona, IT 1 0
Polinelli, Stefano Verona, IT 1 0

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