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US20040127502A1 - Use of GAL3 antagonist for treatment of depression - Google Patents

Use of GAL3 antagonist for treatment of depressionDownload PDF

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US20040127502A1
US20040127502A1US10/723,961US72396103AUS2004127502A1US 20040127502 A1US20040127502 A1US 20040127502A1US 72396103 AUS72396103 AUS 72396103AUS 2004127502 A1US2004127502 A1US 2004127502A1
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branched
straight chained
alkyl
aryl
heteroaryl
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US10/723,961
Inventor
Thomas Blackburn
Michael Konkel
Lakmal Boteju
Ian Talisman
John Wetzel
Mathivana Packiarajan
Heidi Chen
Hermo Jimenez
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H Lundbeck AS
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Synaptic Pharmaceutical Corp
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Priority claimed from US10/066,175external-prioritypatent/US20030078271A1/en
Application filed by Synaptic Pharmaceutical CorpfiledCriticalSynaptic Pharmaceutical Corp
Priority to US10/723,961priorityCriticalpatent/US20040127502A1/en
Publication of US20040127502A1publicationCriticalpatent/US20040127502A1/en
Assigned to H. LUNDBECK A/SreassignmentH. LUNDBECK A/SASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS).Assignors: SYNAPTIC PHARMACEUTICAL CORPORATION
Priority to US11/517,589prioritypatent/US7465750B2/en
Priority to US12/314,675prioritypatent/US20090318504A1/en
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Abstract

This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

Description

Claims (255)

What is claimed:
1. A method of treating a subject suffering from depression which comprises administering to the subject an amount of compound effective to treat the subject's depression wherein the compound has the structure:
Figure US20040127502A1-20040701-C00729
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is; NR11R12;
Figure US20040127502A1-20040701-C00730
Figure US20040127502A1-20040701-C00731
Figure US20040127502A1-20040701-C00732
Figure US20040127502A1-20040701-C00733
Figure US20040127502A1-20040701-C00734
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is NR11R12;
Figure US20040127502A1-20040701-C00735
Figure US20040127502A1-20040701-C00736
Figure US20040127502A1-20040701-C00737
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is N(CH3)2or
Figure US20040127502A1-20040701-C00738
Figure US20040127502A1-20040701-C00739
Figure US20040127502A1-20040701-C00740
Figure US20040127502A1-20040701-C00741
Figure US20040127502A1-20040701-C00742
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is N(CH3)2or
Figure US20040127502A1-20040701-C00743
Figure US20040127502A1-20040701-C00761
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is; NR11R12;
Figure US20040127502A1-20040701-C00762
Figure US20040127502A1-20040701-C00763
Figure US20040127502A1-20040701-C00764
Figure US20040127502A1-20040701-C00765
Figure US20040127502A1-20040701-C00766
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is NR11R12;
Figure US20040127502A1-20040701-C00767
Figure US20040127502A1-20040701-C00768
Figure US20040127502A1-20040701-C00769
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is N(CH3)2or
Figure US20040127502A1-20040701-C00770
Figure US20040127502A1-20040701-C00771
Figure US20040127502A1-20040701-C00772
Figure US20040127502A1-20040701-C00773
Figure US20040127502A1-20040701-C00774
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is N(CH3)2or
Figure US20040127502A1-20040701-C00775
Figure US20040127502A1-20040701-C00793
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is; NR11R12;
Figure US20040127502A1-20040701-C00794
Figure US20040127502A1-20040701-C00795
Figure US20040127502A1-20040701-C00796
Figure US20040127502A1-20040701-C00797
Figure US20040127502A1-20040701-C00798
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is NR11R12;
Figure US20040127502A1-20040701-C00799
Figure US20040127502A1-20040701-C00800
Figure US20040127502A1-20040701-C00801
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is N(CH3)2or
Figure US20040127502A1-20040701-C00802
Figure US20040127502A1-20040701-C00803
Figure US20040127502A1-20040701-C00804
Figure US20040127502A1-20040701-C00805
Figure US20040127502A1-20040701-C00806
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is N(CH3)2or
Figure US20040127502A1-20040701-C00807
Figure US20040127502A1-20040701-C00818
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is; NR11R12;
Figure US20040127502A1-20040701-C00819
Figure US20040127502A1-20040701-C00820
Figure US20040127502A1-20040701-C00821
Figure US20040127502A1-20040701-C00822
Figure US20040127502A1-20040701-C00823
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is NR11R12;
Figure US20040127502A1-20040701-C00824
Figure US20040127502A1-20040701-C00825
Figure US20040127502A1-20040701-C00826
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is N(CH3)2or
Figure US20040127502A1-20040701-C00827
Figure US20040127502A1-20040701-C00828
Figure US20040127502A1-20040701-C00829
Figure US20040127502A1-20040701-C00830
Figure US20040127502A1-20040701-C00831
wherein W is H, —F, —Cl, —Br, —I, CN, methyl, ethyl, propyl, methoxy or ethoxy;
wherein X is N(CH3)2or
Figure US20040127502A1-20040701-C00832
Figure US20040127502A1-20040701-C00842
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is A′, Q3, Q4, Q5, straight chained or branched C1-C7alkyl, aryl, heteroaryl, aryl(C1-C6)alkyl, heteroaryl(C1-C6)alkyl, aryl substituted with an aryl or heteroaryl, heteroaryl substituted with an aryl or heteroaryl; or (CHR17)—(CHR17)n—Z;
wherein A′ is
Figure US20040127502A1-20040701-C00843
Figure US20040127502A1-20040701-C00844
Figure US20040127502A1-20040701-C00845
Figure US20040127502A1-20040701-C00846
Figure US20040127502A1-20040701-C00847
Figure US20040127502A1-20040701-C00848
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is A′, straight chained or branched C1-C7alkyl, aryl, heteroaryl, aryl (C1-C6)alkyl or heteroaryl(C1-C6) alkyl;
Figure US20040127502A1-20040701-C00849
Figure US20040127502A1-20040701-C00850
Figure US20040127502A1-20040701-C00851
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is A′, straight chained or branched C1-C7alkyl, aryl, heteroaryl, aryl(C1-C6)alkyl or heteroaryl (C1-C6) alkyl;
wherein A′ is
Figure US20040127502A1-20040701-C00852
Figure US20040127502A1-20040701-C00853
Figure US20040127502A1-20040701-C00854
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is Q3, Q4, Q5, aryl substituted with an aryl or heteroaryl, heteroaryl substituted with an aryl or heteroaryl, or (CHR17)—(CHR17)m—Z;
wherein Q3is
Figure US20040127502A1-20040701-C00855
Figure US20040127502A1-20040701-C00856
Figure US20040127502A1-20040701-C00857
Figure US20040127502A1-20040701-C00869
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is A′, Q3, Q4, Q5, straight chained or branched C1-C7alkyl, aryl, heteroaryl, aryl(C1-C6)alkyl, heteroaryl (C1-C6)alkyl, aryl substituted with an aryl or heteroaryl, heteroaryl substituted with an aryl or heteroaryl; or (CHR17)—(CHR17)m—Z;
wherein A′ is
Figure US20040127502A1-20040701-C00870
Figure US20040127502A1-20040701-C00871
Figure US20040127502A1-20040701-C00872
Figure US20040127502A1-20040701-C00873
Figure US20040127502A1-20040701-C00874
Figure US20040127502A1-20040701-C00875
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is A′, straight chained or branched C1-C7alkyl, aryl, heteroaryl, aryl(C1-C6)alkyl or heteroaryl(C1-C6)alkyl;
wherein A′ is
Figure US20040127502A1-20040701-C00876
Figure US20040127502A1-20040701-C00877
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is A′, straight chained or branched C1-C7alkyl, aryl, heteroaryl, aryl(C1-C6)alkyl or heteroaryl(C1-C6)alkyl;
wherein A′ is
Figure US20040127502A1-20040701-C00878
Figure US20040127502A1-20040701-C00879
Figure US20040127502A1-20040701-C00880
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is Q3, Q4, Q5, aryl substituted with an aryl or heteroaryl, heteroaryl substituted with an aryl or heteroaryl, or (CHR17)—(CHR17)n—Z;
wherein Q3is
Figure US20040127502A1-20040701-C00881
Figure US20040127502A1-20040701-C00882
Figure US20040127502A1-20040701-C00883
Figure US20040127502A1-20040701-C00895
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is A′, Q3, Q4, Q5, straight chained or branched C1-C7alkyl, aryl, heteroaryl, aryl(C1-C6) alkyl, heteroaryl(C1-C6)alkyl, aryl substituted with an aryl or heteroaryl, heteroaryl substituted with an aryl or heteroaryl; or (CHR17)—(CHR17)n—Z;
wherein A′ is
Figure US20040127502A1-20040701-C00896
Figure US20040127502A1-20040701-C00897
Figure US20040127502A1-20040701-C00898
Figure US20040127502A1-20040701-C00899
Figure US20040127502A1-20040701-C00900
Figure US20040127502A1-20040701-C00901
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is A′, straight chained or branched C1-C7alkyl, aryl, heteroaryl, aryl(C1-C6)alkyl or heteroaryl(C1-C6)alkyl;
wherein A′ is
Figure US20040127502A1-20040701-C00902
Figure US20040127502A1-20040701-C00903
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is A′, straight chained or branched C1-C7alkyl, aryl, heteroaryl, aryl(C1-C6)alkyl or heteroaryl(C1-C6)alkyl;
wherein A′ is
Figure US20040127502A1-20040701-C00904
Figure US20040127502A1-20040701-C00905
Figure US20040127502A1-20040701-C00906
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or. alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is Q3, Q4, Q5, aryl substituted with an aryl or heteroaryl, heteroaryl substituted with an aryl or heteroaryl, or (CHR17)—(CHR17)n—Z;
wherein Q3is
Figure US20040127502A1-20040701-C00907
Figure US20040127502A1-20040701-C00908
Figure US20040127502A1-20040701-C00909
Figure US20040127502A1-20040701-C00916
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is A′, Q3, Q4, Q5, straight chained or branched C1-C7alkyl, aryl, heteroaryl, aryl(C1-C6)alkyl, heteroaryl(C1-C6)alkyl, aryl substituted with an aryl or heteroaryl, heteroaryl substituted with an aryl or heteroaryl; or (CHR17)—(CHR17)n—Z;
wherein A′ is
Figure US20040127502A1-20040701-C00917
Figure US20040127502A1-20040701-C00918
Figure US20040127502A1-20040701-C00919
Figure US20040127502A1-20040701-C00920
Figure US20040127502A1-20040701-C00921
Figure US20040127502A1-20040701-C00922
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is A′, straight chained or branched C1-C7alkyl, aryl, heteroaryl, aryl(C1-C6)alkyl or heteroaryl(C1-C6)alkyl;
wherein A′ is
Figure US20040127502A1-20040701-C00923
Figure US20040127502A1-20040701-C00924
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is A′, straight chained or branched C1-C7alkyl, aryl, heteroaryl, aryl(C1-C6)alkyl or heteroaryl(C1-C6)alkyl;
wherein A′ is
Figure US20040127502A1-20040701-C00925
Figure US20040127502A1-20040701-C00926
Figure US20040127502A1-20040701-C00927
wherein each of Y1, Y2, Y3, and Y4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, or C5-C7cycloalkenyl; —F, —Cl, —Br, or —I; —NO2; —N3; —CN; —OR4, —SR4, —OCOR4, —COR4, —NCOR4, —N(R4)2, —CON(R4)2, or —COOR4; aryl or heteroaryl; or any two of Y1, Y2, Y3and Y4present on adjacent carbon atoms can constitute a methylenedioxy group;
wherein each R4is independently —H; straight chained or branched C1-C7alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7alkenyl or alkynyl; C3-C7cycloalkyl, C5-C7cycloalkenyl, aryl or aryl(C1-C6)alkyl;
wherein A is Q3, Q4, Q5, aryl substituted with an aryl or heteroaryl, heteroaryl substituted with an aryl or heteroaryl, or (CHR17)—(CHR17)n—Z;
wherein Q3is
Figure US20040127502A1-20040701-C00928
Figure US20040127502A1-20040701-C00929
Figure US20040127502A1-20040701-C00930
226. A method of treating depression in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist, wherein:
(a) the GAL3 receptor antagonist binds to the human GAL3 receptor with a binding affinity at least ten-fold higher than the binding affinity with which it binds to the human GAL1 receptor;
(b) (1), the GAL3 receptor antagonist does not inhibit the activity of central monoamine oxidase A greater than 50 percent, at a concentration of 10 μM; and
(2) the GAL3 receptor antagonist does not inhibit the activity of central monoamine oxidase B greater than 50 percent, at a concentration of 10 μM; and
(c) the GAL3 receptor antagonist binds to the human GAL3 receptor with a binding affinity at least ten-fold higher than the binding affinity with which it binds to each of the following transporters: serotonin transporter, norepinephrine transporter, and dopamine transporter.
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Cited By (10)

* Cited by examiner, † Cited by third party
Publication numberPriority datePublication dateAssigneeTitle
US20030178369A1 (en)*2000-08-102003-09-25Tamiyuki EguchiImmersion type membrane filter
US20040082587A1 (en)*2002-08-072004-04-29Mathivanan Packiarajan2,4,6-Triaminopyrimidines for the treatment of depression and/or anxiety
US20040092570A1 (en)*2002-08-072004-05-13Blackburn Thomas P.GAL3 antagonists for the treatment of neuropathic pain
US20040110821A1 (en)*2002-08-072004-06-10Konkel Michael J.GAL3 receptor antagonists for the treatment of affective disorders
US20050148635A1 (en)*2002-08-072005-07-07Michael Konkel3-imino-2-indolones for the treatment of depression and/or anxiety
US7081470B2 (en)2001-01-312006-07-25H. Lundbeck A/SUse of GALR3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
US20060172989A1 (en)*2005-02-022006-08-03Michael KonkelAminoalkoxyphenyl indolone derivatives
WO2007118899A1 (en)*2006-04-192007-10-25Abbott Gmbh & Co. KgHeterocyclic arylsulphones suitable for treating disorders that respond to modulation of the serotonin 5ht6 receptor
EP1956006A1 (en)*2007-02-062008-08-13Laboratorios del Dr. Esteve S.A.Heterocyclyl-substituted-tetrahydro-naphthalen derivatives as 5-HT7 receptor ligands
EP1975161A1 (en)*2007-03-282008-10-01Laboratorios del Dr. Esteve S.A.Heterocyclyl-substituted- tetrahydro-napthalen-amine derivatives, their preparation and use as medicaments

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication numberPriority datePublication dateAssigneeTitle
US20040127502A1 (en)*2001-01-312004-07-01Synaptic Pharmaceutical CorporationUse of GAL3 antagonist for treatment of depression
US7642281B2 (en)*2002-08-072010-01-05Helicon Therapeutics, Inc.Indolone compounds useful to treat cognitive impairment
US20070135509A1 (en)*2005-12-092007-06-14Blackburn Thomas PIndolone compounds useful to treat cognitive impairment

Citations (10)

* Cited by examiner, † Cited by third party
Publication numberPriority datePublication dateAssigneeTitle
US4874687A (en)*1986-11-181989-10-17Fuji Photo Film Co., Ltd.Method for forming an image
US4921503A (en)*1988-09-121990-05-01Clairol IncorporatedNovel dyeing system
US4946956A (en)*1988-09-211990-08-07Uniroyal Chemical Company, Inc.Arylenediamine substituted pyrimidines
US5017466A (en)*1989-05-241991-05-21Fuji Photo Film Co., Ltd.Color-forming aminopyrimidine couplers and silver halide color photographic light-sensitive materials containing the coupler
US5547949A (en)*1992-06-091996-08-20Richter Gedeon Vegyeszeti Gyar Rt.Steroids with pregnane skeleton, pharmaceutical compositions containing them
US5728704A (en)*1992-09-281998-03-17Pfizer Inc.Substituted pyridmidines for control of diabetic complications
US5801150A (en)*1993-06-231998-09-01Caillot; Jean-LucAminopyri(mi)dine derivatives combined with amino acids, and pharmacological activities thereof
US5840893A (en)*1995-01-061998-11-24The Picower Institute For Medical ResearchCompounds for treating infectious diseases
US5921503A (en)*1998-02-041999-07-13Tsay; Ing-LangAssistant landing device of a troubled airplane
US6287788B1 (en)*1996-10-092001-09-11Synaptic Pharmaceutical CorporationDNA encoding galanin GALR3 receptors and uses thereof

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication numberPriority datePublication dateAssigneeTitle
GB1477349A (en)1975-09-241977-06-22Ciba Geigy AgAzo pigments
US5198461A (en)1989-12-111993-03-30Neurosearch A/SIsatine derivatives, their preparation and use
JP3374136B2 (en)1991-11-122003-02-04三洋電機株式会社 Lithium secondary battery
HUT64323A (en)1992-06-091993-12-28Richter Gedeon VegyeszetProcess for production new piperazinyl-bis(alkyl-amino)-pyrimidine derivatives
DK0640599T3 (en)1993-08-261998-09-28Ono Pharmaceutical Co 4-aminopyrimidine derivatives
US5565580A (en)1994-01-271996-10-15Neurosearch A/SGlutamate Antagonists
EP0788890A1 (en)1996-02-061997-08-13Agfa-Gevaert N.V.Dyes and dye-donor elements for thermal dye transfer recording
JP3319960B2 (en)*1996-10-172002-09-03富士通株式会社 Semiconductor device
JPH11158073A (en)1997-09-261999-06-15Takeda Chem Ind LtdAdenosine a3 antagonist
BR9908004A (en)1998-02-172001-12-18Tularik Inc Compound, composition and method for preventing or suppressing a viral infection
CZ299380B6 (en)1998-03-272008-07-09Janssen Pharmaceutica N. V.Pyrimidine compound, use of such compound for the preparation of a medicament, pharmaceutical composition containing such compound, process for preparing the pharmaceutical composition and such compound as well as combination and product containing s
EP0945442A1 (en)1998-03-271999-09-29Janssen Pharmaceutica N.V.Trisubstituted pyrimidine derivatives
WO1999065875A1 (en)1998-06-171999-12-23Geron CorporationTelomerase inhibitors
US6881740B1 (en)1998-07-082005-04-19Monash UniversityPharmaceutical agents
DE69900297T2 (en)1998-07-142002-05-02Basf Ag Acaricidal and insecticidal, substituted pyrimidines and process for their preparation
US20040127502A1 (en)*2001-01-312004-07-01Synaptic Pharmaceutical CorporationUse of GAL3 antagonist for treatment of depression
US7081470B2 (en)*2001-01-312006-07-25H. Lundbeck A/SUse of GALR3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
US6996172B2 (en)2001-12-212006-02-07Motorola, Inc.Method and structure for scalability type selection in digital video
US20040082615A1 (en)*2002-08-072004-04-29Michael Konkel3-Imino-2-indolones for the treatement of depression and/or anxiety
US7220775B2 (en)*2002-08-072007-05-22H. Lundbeck A/SCompound useful for the treatment of neuropathic pain

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication numberPriority datePublication dateAssigneeTitle
US4874687A (en)*1986-11-181989-10-17Fuji Photo Film Co., Ltd.Method for forming an image
US4921503A (en)*1988-09-121990-05-01Clairol IncorporatedNovel dyeing system
US4946956A (en)*1988-09-211990-08-07Uniroyal Chemical Company, Inc.Arylenediamine substituted pyrimidines
US5017466A (en)*1989-05-241991-05-21Fuji Photo Film Co., Ltd.Color-forming aminopyrimidine couplers and silver halide color photographic light-sensitive materials containing the coupler
US5547949A (en)*1992-06-091996-08-20Richter Gedeon Vegyeszeti Gyar Rt.Steroids with pregnane skeleton, pharmaceutical compositions containing them
US5728704A (en)*1992-09-281998-03-17Pfizer Inc.Substituted pyridmidines for control of diabetic complications
US5801150A (en)*1993-06-231998-09-01Caillot; Jean-LucAminopyri(mi)dine derivatives combined with amino acids, and pharmacological activities thereof
US5840893A (en)*1995-01-061998-11-24The Picower Institute For Medical ResearchCompounds for treating infectious diseases
US6287788B1 (en)*1996-10-092001-09-11Synaptic Pharmaceutical CorporationDNA encoding galanin GALR3 receptors and uses thereof
US6329197B2 (en)*1996-10-092001-12-11Synaptic Pharmaceutical CorporationDNA encoding galanin GALR3 receptors and uses thereof
US6368812B1 (en)*1996-10-092002-04-09Synaptic Pharmaceutical CorporationProcess for determining the agonist or antagonist of galanin receptor (GALR3)
US5921503A (en)*1998-02-041999-07-13Tsay; Ing-LangAssistant landing device of a troubled airplane

Cited By (22)

* Cited by examiner, † Cited by third party
Publication numberPriority datePublication dateAssigneeTitle
US20030178369A1 (en)*2000-08-102003-09-25Tamiyuki EguchiImmersion type membrane filter
US20090176840A1 (en)*2001-01-312009-07-09Michael KonkelUse of galr3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
US7081470B2 (en)2001-01-312006-07-25H. Lundbeck A/SUse of GALR3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
US7868034B2 (en)2001-01-312011-01-11H. Lundbeck A/SUse of GALR3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
US20040082587A1 (en)*2002-08-072004-04-29Mathivanan Packiarajan2,4,6-Triaminopyrimidines for the treatment of depression and/or anxiety
US20040092570A1 (en)*2002-08-072004-05-13Blackburn Thomas P.GAL3 antagonists for the treatment of neuropathic pain
US20040110821A1 (en)*2002-08-072004-06-10Konkel Michael J.GAL3 receptor antagonists for the treatment of affective disorders
US20050148635A1 (en)*2002-08-072005-07-07Michael Konkel3-imino-2-indolones for the treatment of depression and/or anxiety
US6936607B2 (en)2002-08-072005-08-30H. Lunobeck A/S2,4,6-Triaminopyrimidines for the treatment of depression and/or anxiety
US7166635B2 (en)2002-08-072007-01-23H. Lundbeck A/S3-imino-2-indolones for the treatment of depression and/or anxiety
US20060172989A1 (en)*2005-02-022006-08-03Michael KonkelAminoalkoxyphenyl indolone derivatives
US20090306175A1 (en)*2006-04-192009-12-10Abbott Gmbh & Co. KgHeterocyclic arylsulphones suitable for treating disorders that respond to modulation of the serotonin 5ht6 receptor
WO2007118899A1 (en)*2006-04-192007-10-25Abbott Gmbh & Co. KgHeterocyclic arylsulphones suitable for treating disorders that respond to modulation of the serotonin 5ht6 receptor
US8642642B2 (en)2006-04-192014-02-04Abbott LaboratoriesHeterocyclic arylsulphones suitable for treating disorders that respond to modulation of the serotonin 5HT6 receptor
WO2008095689A1 (en)*2007-02-062008-08-14Laboratorios Del Dr. Esteve, S.A.Heterocyclyl substituted tetrahydronaphthalene derivatives as 5-ht7 receptor ligands
EP1956006A1 (en)*2007-02-062008-08-13Laboratorios del Dr. Esteve S.A.Heterocyclyl-substituted-tetrahydro-naphthalen derivatives as 5-HT7 receptor ligands
US20100035936A1 (en)*2007-02-062010-02-11Laboratorios Del Dr. Esteve, S.A.Heterocyclyl substituted tetrahydronaphthalene derivatives as 5-ht7 receptor ligands
US8097641B2 (en)2007-02-062012-01-17Laboratorios Del Dr. Esteve, S.A.Heterocyclyl substituted tetrahydronaphthalene derivatives as 5-HT7 receptor ligands
EP1975161A1 (en)*2007-03-282008-10-01Laboratorios del Dr. Esteve S.A.Heterocyclyl-substituted- tetrahydro-napthalen-amine derivatives, their preparation and use as medicaments
WO2008116663A3 (en)*2007-03-282008-11-06Esteve Labor DrHeterocyclyl-substituted-tetrahydro-naphthalen-amine derivatives, their preparation and use as medicaments
US20100105684A1 (en)*2007-03-282010-04-29Laboratorios Del Dr. Esteve, S.A.Heterocyclyl-substituted-tetrahydro-naphthalen-amine derivatives, their preparation and use as medicaments
US8236845B2 (en)2007-03-282012-08-07Laboratorios Del Dr. Esteve, S.A.Heterocyclyl-substituted-tetrahydro-naphthalen-amine derivatives, their preparation and use as medicaments

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