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11. 发明授权

US06306878B1 Pharmaceutical compositions containing hydroximic acid derivatives 失效
公开(公告)号：US06306878B1
公开(公告)日：2001-10-23
申请号：US08722499
申请日：1996-09-27
申请人： Balazs Sumegi , Peter Literati Nagy , Laszlo Vigh , Bruno Maresca
发明人： Balazs Sumegi , Peter Literati Nagy , Laszlo Vigh , Bruno Maresca
IPC分类号： A61K31445
CPC分类号： A61K31/5395 , A61K31/15 , A61K31/4545 , A61K31/455 , A61K31/539
摘要： The invention refers to pharmaceutical compositions suitable for the protection of the mitochondrial genom and/or mitochondrium from damages or for the treatment of diseases connected with such damages, said compositions comprising a hydroximic acid derivative of the formula: wherein R1 represents a hydrogen or a C1-5 alkyl group, R2 stands for a hydrogen, a C1-5 alkyl group, a C3-8 cycloalkyl group or a phenyl group optionally substituted by a hydroxy or a phenyl group, or R1 or R2 together with the nitrogen atom they are attached to form a 5 to 8 membered ring optionally containing one or more further nitrogen, oxygen or sulfur atom(s) and said ring can be condensed with another alicyclic or heterocyclic ring, preferably a benzene, naphthalene, quinoline, isoquinoline, pyridine or pyrazoline ring, furthermore, if desired and chemically possible, the nitrogen and/or sulfur heteroatom(s) are present in the form of an oxide or dioxide, R3 means a hydrogen, a phenyl group, a naphthyl group or a pyridyl group wherein said groups can be substituted by one or more halo atom(s) or C1-4 alkoxy group(s), Y is a hydrogen, a hydroxy group, a C1-24 alkoxy group optionally substituted by an amino group, a C2-24 polyalkenyl-oxy group containing 1 to 6 double bond(s), a C1-25 alkanoyl group, C3-9 alkenoyl group or a group of the formula R7—COO—, wherein R7 represents a C2-30 polyalkenyl group containing 1 to 6 double bond(s), X stands for a halo, an amino group, a C1-4 alkoxy group, or X forms with B an oxygen atom, or X and Y together with the carbon atoms they are attached to and the —NR—O—CH2 group being between said carbon atoms form a ring of the formula wherein Z represents an oxygen or a nitrogen, R stands for a hydrogen or R forms with B a chemical bond, A is a C1-4 alkylene group or a chemical bond or a group of the formula wherein R4 represents a hydrogen, a C1-5 alkyl group, a C3-8 cycloalkyl group or a phenyl group optionally substituted by a halo, a C1-4 alkoxy group or a C1-5 alkyl group, R5 stands for a hydrogen, a C1-4 alkyl group or a phenyl group, m has a value of 0, 1 or 2, n has a value of 0, 1 or 2, or a pharmaceutically acceptable acid addition salt thereof as the active ingredient.

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