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1. (WO1992010479) AMIDIC DERIVATIVES OF GLUTAMIC, ASPARTIC AND 2-AMINO ADIPIC ACIDS WITH ANTIGASTRIN ACTIVITY
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1992/010479 International Application No.: PCT/EP1991/002342
Publication Date: 25.06.1992 International Filing Date: 06.12.1991
Chapter 2 Demand Filed: 09.06.1992
IPC:
C07C 237/22 (2006.01) ,C07D 209/54 (2006.01) ,C07D 217/06 (2006.01) ,C07D 221/20 (2006.01) ,C07D 491/10 (2006.01) ,C07D 495/10 (2006.01) ,C07D 497/10 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
237
Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02
having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
22
having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
54
Spiro-condensed
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
217
Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
02
with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
06
with the ring nitrogen atom acylated by carboxylic or carbonic acids, or with sulfur or nitrogen analogues thereof, e.g. carbamates
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
221
Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/-C07D219/187
02
condensed with carbocyclic rings or ring systems
20
Spiro-condensed ring systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02
in which the condensed system contains two hetero rings
10
Spiro-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
495
Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
10
Spiro-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
497
Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
10
Spiro-condensed systems
Applicants:
ROTTA RESEARCH LABORATORIUM S.P.A. [IT/IT]; Via Valosa di Sopra, 7 I-20052 Monza, IT (AllExceptUS)
MAKOVEC, Francesco [IT/IT]; IT (UsOnly)
ROVATI, Luigi, Angelo [IT/IT]; IT (UsOnly)
ROVATI, Claudio, Lucio [IT/IT]; IT (UsOnly)
Inventors:
MAKOVEC, Francesco; IT
ROVATI, Luigi, Angelo; IT
ROVATI, Claudio, Lucio; IT
Agent:
RAMBELLI, Paolo ; Jacobacci-Casetta & Perani S.p.A. Via Alfieri, 17 I-10121 Torino, IT
Priority Data:
67995 A/9011.12.1990IT
Title (EN) AMIDIC DERIVATIVES OF GLUTAMIC, ASPARTIC AND 2-AMINO ADIPIC ACIDS WITH ANTIGASTRIN ACTIVITY
(FR) DERIVES AMIDIQUES PRESENTANT L'ACTIVITE ANTIGASTRINE DES ACIDES GLUMATIQUE, ASPARTIQUE ET 2-AMINO ADIPEUX
Abstract:
(EN) Bicyclic and polycyclic amidic derivatives of glumatic, aspartic and 2-amino adipic acids having activities antagonistic to gastrin, of general formula (I) in which r is between 1 and 3 and R1 is selected from mono- and disubstituted phenyl groups, and in which the substituents are selected from chlorine, linear and branched C1-C4 alkyl groups, cyano, nitro, methoxy, and trifluoromethyl groups, and the 2(beta)-naphthyl group, and heterocyclic, monocyclic or bicyclic groups containing one heteroatom such as nitrogen, oxygen or sulphur and selected from furyl, thiophenyl, pirrolyl, pyridinyl, and pyridinyl-N-oxide unsubstituted or mono- or disubstituted with methyl and chlorine, indolyl, thionaphthyl, benzofuranyl, quinolinyl, or isoquinolinyl groups, and in which R2 is selected independently from a heterocyclic spiro group, a bicyclic spiro amino group, a bicyclic amino group (condensed) and an adamantyl alkyl amino group.
(FR) Dérivés amidiques bicycliques et polycycliques des acides glutamique, aspartique et 2-amino adipeux, présentant des activités antagonistes de la gastrine et répondant à la formule générale (I), dans laquelle r est compris entre 1 et 3; R1 est sélectionné parmi les groupes phényle mono- et disubstitués; les substituants sont sélectionnés parmi le chlore, les groupes alkyle C1-4 linéaires ou ramifiés, les groupes cyano, nitro, méthoxy, et trifluorométhyle, et le groupe 2(bêta)-naphtyle, ainsi que les groupes hétérocycliques, monocycliques ou bicycliques comprenant un hétéroatome tel que l'azote, l'oxygène ou le soufre, et sélectionnés parmi furyle, thiophényle, pirrolyle, pyridinyle et pyridinyl-N-oxyde non substitué ou mono- ou disubstitué par méthyle et des groupes chlore, indolyle, thionaphtyle, benzofuranyle, quinolinyle ou isoquinolinyle; et R2 est sélectionné indépendamment parmi un groupe spiro hétérocyclique, un groupe amino spiro bicyclique, un groupe amino bicyclique (condensé) et un groupe amino alkyle adamantyle.
Designated States: AU, CA, JP, US
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, MC, NL, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0561863US5500430JPH06503557CA2097069DE000069104996PT99745
AU1991090456DK0561863