1,5-BENZODIAZEPINE DERIVATIVES USEFUL AS CCK OR GASTRIN ANTAGONISTS

PCT No. PCT/EP94/02352 Sec. 371 Date Nov. 4, 1996 Sec. 102(e) Date Nov. 4, 1996 PCT Filed Jul. 18, 1994 PCT Pub. No. WO95/03284 PCT Pub. Date Feb. 2, 1995Compounds of general formula (I) (I) wherein R1 represents a phenyl, C3-7cycloalkyl, C7-11bridgedcycloalkyl or C1-6alkyl group which alkyl group m...

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Hauptverfasser: POLINELLI, STEFANO, PELLEGATTI, MARIO, CUROTTO, GIOVANNI
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PELLEGATTI, MARIO
CUROTTO, GIOVANNI
description PCT No. PCT/EP94/02352 Sec. 371 Date Nov. 4, 1996 Sec. 102(e) Date Nov. 4, 1996 PCT Filed Jul. 18, 1994 PCT Pub. No. WO95/03284 PCT Pub. Date Feb. 2, 1995Compounds of general formula (I) (I) wherein R1 represents a phenyl, C3-7cycloalkyl, C7-11bridgedcycloalkyl or C1-6alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl, or C3-7bridgedcycloalkyl group; R2 represents phenyl substituted by a group (CH2)nNR4R5, O(CH2)pR6, or (CH2)nCO2R11; R3 represents phenyl optionally substituted by one or 2 halogen atoms; R4 represents hydrogen or C1-4alkyl; R5 represents acyl, or C2-4alkyl substituted by one or more hydroxy; carboxyl and/or amino groups or R4 and R5 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 C1-4alkyl or hydroxy groups. R6 represents hydroxy, C1-4alkoxy, CO2R7 or NR8R9; R7 represents hydrogen or C1-4alkyl or a metabolically labile ester group; R8 represents hydrogen, C1-4, acyl or C2-6alkyl substituted by one or more hydroxy, carboxyl and/or amino groups or R8 and R9 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 C1-4alkyl or hydroxy groups; R10 represents hydrogen or a halogen atom; R11 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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No. WO95/03284 PCT Pub. Date Feb. 2, 1995Compounds of general formula (I) (I) wherein R1 represents a phenyl, C3-7cycloalkyl, C7-11bridgedcycloalkyl or C1-6alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl, or C3-7bridgedcycloalkyl group; R2 represents phenyl substituted by a group (CH2)nNR4R5, O(CH2)pR6, or (CH2)nCO2R11; R3 represents phenyl optionally substituted by one or 2 halogen atoms; R4 represents hydrogen or C1-4alkyl; R5 represents acyl, or C2-4alkyl substituted by one or more hydroxy; carboxyl and/or amino groups or R4 and R5 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 C1-4alkyl or hydroxy groups. 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No. WO95/03284 PCT Pub. Date Feb. 2, 1995Compounds of general formula (I) (I) wherein R1 represents a phenyl, C3-7cycloalkyl, C7-11bridgedcycloalkyl or C1-6alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl, or C3-7bridgedcycloalkyl group; R2 represents phenyl substituted by a group (CH2)nNR4R5, O(CH2)pR6, or (CH2)nCO2R11; R3 represents phenyl optionally substituted by one or 2 halogen atoms; R4 represents hydrogen or C1-4alkyl; R5 represents acyl, or C2-4alkyl substituted by one or more hydroxy; carboxyl and/or amino groups or R4 and R5 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 C1-4alkyl or hydroxy groups. 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No. WO95/03284 PCT Pub. Date Feb. 2, 1995Compounds of general formula (I) (I) wherein R1 represents a phenyl, C3-7cycloalkyl, C7-11bridgedcycloalkyl or C1-6alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl, or C3-7bridgedcycloalkyl group; R2 represents phenyl substituted by a group (CH2)nNR4R5, O(CH2)pR6, or (CH2)nCO2R11; R3 represents phenyl optionally substituted by one or 2 halogen atoms; R4 represents hydrogen or C1-4alkyl; R5 represents acyl, or C2-4alkyl substituted by one or more hydroxy; carboxyl and/or amino groups or R4 and R5 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 C1-4alkyl or hydroxy groups. R6 represents hydroxy, C1-4alkoxy, CO2R7 or NR8R9; R7 represents hydrogen or C1-4alkyl or a metabolically labile ester group; R8 represents hydrogen, C1-4, acyl or C2-6alkyl substituted by one or more hydroxy, carboxyl and/or amino groups or R8 and R9 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 C1-4alkyl or hydroxy groups; R10 represents hydrogen or a halogen atom; R11 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.</abstract><edition>6</edition><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title 1,5-BENZODIAZEPINE DERIVATIVES USEFUL AS CCK OR GASTRIN ANTAGONISTS
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