Method and use
First Claim
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1. A method of antagonizing GLP-1 activity in a mammalian subject, comprising administering to said subject an effective amount of a compound of the general formula I:
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whereinR1 and R2 independently of each other are C1-4alkyl, R3 is halogen, hydroxy, C1-4-alkoxy or trifluoromethoxy, R4 is hydrogen, hydroxy or C1-4-alkoxy, or a pharmacologically acceptable salt thereof.
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Abstract
The invention relates to a method of antagonizing GLP-1 activity in a mammalian patient, comprising administering to said patient an effective amount of a compound of the general formula I:
wherein
R1 and R2 independently of each other are C1-4alkyl,
R3 is halogen, hydroxy, C1-4-alkoxy or trifluoromethoxy,
R4 is hydrogen, hydroxy or C1-4-alkoxy,
or a pharmacologically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising a compound of formula I.
22 Citations
20 Claims
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1. A method of antagonizing GLP-1 activity in a mammalian subject, comprising administering to said subject an effective amount of a compound of the general formula I:
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wherein R1 and R2 independently of each other are C1-4alkyl, R3 is halogen, hydroxy, C1-4-alkoxy or trifluoromethoxy, R4 is hydrogen, hydroxy or C1-4-alkoxy, or a pharmacologically acceptable salt thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20)
4-chloro-2-{[(E)-2-(1,3-dimethyl-4-nitro-1H-pyrazol-5-yl)ethenyl]amino}phenol;
4-fluoro-1-{[(E)-2-(1,3-dimethyl-4-nitro-1H-pyrazol-5-yl)ethenyl]amino}benzene;
4-trifluoromethoxy-1-{[(E)-2-(1,3-dimethyl-4-nitro-1H-pyrazol-5-yl)ethenyl]amino}benzene;
or2,4-dimethoxy-1-{[(E)-2-(1,3-dimethyl-4-nitro-1H-pyrazol-5-yl)ethenyl]amino}benzene.
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8. The method according to claim 1, wherein the compound is:
4-chloro-2-{[(E)-2-(1,3-dimethyl-4-nitro-1H-pyrazol-5-yl)ethenyl]amino}phenol.
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9. The method according to claim 1, wherein GLP-1 is anatgonized to treat a disease selected from postprandial reactive hypoglycemia, anorexia, reduced intestinal motility and constipation, and Alzheimer'"'"'s disease.
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10. A pharmaceutical composition comprising a compound of formula I in claim 1 and optionally a pharmaceutically acceptable carrier.
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11. A method of treating a disorder where inhibition of GLP-1 activity is indicated, the method comprising administering to a mammal subject in need thereof an effective amount of a compound of formula I in claim 1.
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12. The method according to claim 11, wherein the disorder is postprandial reactive hypoglycemia.
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13. The method according to claim 11, wherein the disorder is anorexia.
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14. The method according to claim 11, wherein the disorder is reduced intestinal motility and constipation.
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15. The method according to claim 11, wherein the disorder is Alzheimer'"'"'s disease.
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16. The method according to claim 11, wherein the mammal subject is a human.
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17. A method of treating a disorder where inhibition of GLP-1 activity is indicated, the method comprising administering to a mammal subject in need thereof a pharmaceutical composition, wherein the pharmaceutical composition comprises an effective amount of a compound of formula I in claim 1 and a pharmaceutically acceptable carrier.
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18. A method of inhibiting GLP-1 activity, comprising administering to a mammal subject in need thereof an effective amount of a compound of formula I in claim 1.
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19. A method of inhibiting GLP-1 activity, comprising administering to a mammal subject in need thereof a pharmaceutical composition, wherein the pharmaceutical composition comprises an effective amount of a compound of formula I in claim 1 and a pharmaceutically acceptable carrier.
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20. The method according to claim 1, wherein R4 is hydroxy or C1-4-alkoxy.
Specification
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Current AssigneeBiovitrum AB (Swedish Orphan Biovitrum AB (publ))
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Original AssigneeBiovitrum AB (Swedish Orphan Biovitrum AB (publ))
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InventorsColca, Jerry R., Gronberg, Alvar
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Primary Examiner(s)Weddington, Kevin E.
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Application NumberUS10/006,518Publication NumberTime in Patent Office547 DaysField of Search514/407, 514/884US Class Current514/407CPC Class CodesC07D 231/16 Halogen atoms or nitro radi...
