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    • 3. 发明授权
    • Pharmaceutical compositions containing hydroximic acid derivatives
    • US06306878B1
    • 2001-10-23
    • US08722499
    • 1996-09-27
    • Balazs SumegiPeter Literati NagyLaszlo VighBruno Maresca
    • Balazs SumegiPeter Literati NagyLaszlo VighBruno Maresca
    • A61K31445
    • A61K31/5395A61K31/15A61K31/4545A61K31/455A61K31/539
    • 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.
    • 8. 发明申请
    • Alicyclic-amine-substituted 4-carboxamido-benzimidazoles as parp-inhibitors and antioxidants
    • 脂环胺 - 胺取代的4-甲酰氨基 - 苯并咪唑作为对位抑制剂和抗氧化剂
    • US20070072912A1
    • 2007-03-29
    • US10553937
    • 2004-04-27
    • Kalman HidegTamas KalaiBalazs Sumegi
    • Kalman HidegTamas KalaiBalazs Sumegi
    • A61K31/4439A61K31/4184C07D403/02
    • C07D401/04C07D403/04C07D403/10C07D405/14C07D495/04
    • Compounds of the formula (I) and their pharmaceutically acceptable or technically applicable acid salts—where in the formula R1 represents hydrogen, C(1-4)alkyl or C(1-4)alkoxy R2 represents hydrogen, C(1-4)alkyl, carboxyl, C(1-4)alkoxycarbonyl, carboxamido, aryl or hetero-aryl R3 represents hydrogen, C(1-4)alkyl, aryl-methylene, or aryl, Y is a valency bond, a straight or branched chain C(1-4)alkene, a carbonyl-amino-C(1-4)alkene, or a —S—(CH2)m— group, where all alkene groups above may be spaced by an arylene group, n represents zero or the integer 1 m represents the integer 1, 2 or 3 Q represents hydrogen, hydroxyl or the oxygen radical (0) or together with the N atom of the adjacent ring forms a +N=O (oxoimmonium) group Z represents a single or double bond and their pharmaceutically acceptable or technically useful salts, processes for their preparation and their biological use as PARP inhibitors and antioxidants.
    • 式(I)化合物及其药学上可接受的或技术上可应用的酸盐 - 其中在式R 1表示氢,C 1-4(1-4) - 烷基或C (1-4)烷氧基R 2表示氢,C 1-4(1-4)烷基,羧基,C 1-4(1-4) 烷氧基羰基,甲酰胺基,芳基或杂芳基R 3表示氢,C 1-4(1-4)烷基,芳基 - 亚甲基或芳基,Y是 直链或支链C 1-4(1-4)烯烃,羰基 - 氨基-C 1-4(1-4) - 烯烃或-S-(CH 其中所有上述烯烃基团可以被亚芳基间隔开,n表示0或整数1m表示整数1,2或3个Q 表示氢,羟基或氧自由基(0)或与相邻环的N原子一起形成a + N = O(有机基元素)基团Z表示单键或双键及其药学上可接受或技术上有用的盐, 准备 n及其生物用作PARP抑制剂和抗氧化剂。