Nicotinamide derivatives and their use as medicaments
A nicotinic acid amide derivative of formula (I), pharmacologically acceptable salts and pharmaceutical compositions thereof: wherein R 1 is H or lower alkyl; R 2 is optionally substituted pyridinyl, pyridinemethyl, N-benzylpiperidinyl, isoquinolyl or benzyl; R 3 is optionally substituted cyclopenty...
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Main Authors | , , , , , |
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Format | Patent |
Language | English |
Published |
24.04.2002
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Edition | 7 |
Subjects | |
Online Access | Get full text |
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Abstract | A nicotinic acid amide derivative of formula (I), pharmacologically acceptable salts and pharmaceutical compositions thereof: wherein R 1 is H or lower alkyl; R 2 is optionally substituted pyridinyl, pyridinemethyl, N-benzylpiperidinyl, isoquinolyl or benzyl; R 3 is optionally substituted cyclopentyl, cyclohexyl, cyclooctyl, norbornyl, adamantyl, piperidyl, pyridyl, isoquinolyl or azabicyclooctyl wherein the ring system is attached to the nicotinamide ring by means of an oxygen or NH group and R 4 is H or lower alkoxy. The compounds are useful for the prevention and treatment of stroke, brain edema after stroke and a variety of allergic and inflammatory diseases, e.g. asthma, chronic bronchitis, shock, rheumatoid arthritis, reperfusion injury, encephalomyelitis and multiple sclerosis. The compounds are prepared from intermediates wherein R 3 is chlorine which in turn are prepared from reaction of the corresponding acid with HNR 1 R 2 . |
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AbstractList | A nicotinic acid amide derivative of formula (I), pharmacologically acceptable salts and pharmaceutical compositions thereof: wherein R 1 is H or lower alkyl; R 2 is optionally substituted pyridinyl, pyridinemethyl, N-benzylpiperidinyl, isoquinolyl or benzyl; R 3 is optionally substituted cyclopentyl, cyclohexyl, cyclooctyl, norbornyl, adamantyl, piperidyl, pyridyl, isoquinolyl or azabicyclooctyl wherein the ring system is attached to the nicotinamide ring by means of an oxygen or NH group and R 4 is H or lower alkoxy. The compounds are useful for the prevention and treatment of stroke, brain edema after stroke and a variety of allergic and inflammatory diseases, e.g. asthma, chronic bronchitis, shock, rheumatoid arthritis, reperfusion injury, encephalomyelitis and multiple sclerosis. The compounds are prepared from intermediates wherein R 3 is chlorine which in turn are prepared from reaction of the corresponding acid with HNR 1 R 2 . |
Author | LEE LAURENCE RUBIN AKIHARU KAJIWARA MARY LOUISE MORGAN JOANNA ELIZABETH BRASHAW SATOSHI NAGATO JAMES MARTIN STADDON |
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Snippet | A nicotinic acid amide derivative of formula (I), pharmacologically acceptable salts and pharmaceutical compositions thereof: wherein R 1 is H or lower alkyl;... |
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Title | Nicotinamide derivatives and their use as medicaments |
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