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公开(公告)号：US5968955A
公开(公告)日：1999-10-19
申请号：US43906
申请日：1998-03-31
IPC分类号： A61K31/00 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61P25/00 , A61P25/04 , C07D413/06
CPC分类号： C07D413/06
摘要： A Disubstituted piperidine compounds of formula (I), wherein R.sub.1 is hydrogen; bromo; chloro; a linear or branched C.sub.1 -C.sub.5 alkyl group; a linear or branched C.sub.1 -C.sub.5 alkoxy group; or an optionally substituted phenyl group; R.sub.2 is hydrogen, a linear or branched C.sub.1 -C.sub.5 alkyl group or an optionally substituted phenyl group; X is CH.sub.2, C.dbd.O, CHOH or C.dbd.NOH; R.sub.3 is hydrogen or a linear or branched C.sub.1 -C.sub.5 alkyl group; Y is a (CH.sub.2).sub.n group in which n is an integer from 0 to 4, CHOH, C.dbd.O or CH-A wherein A is an optionally substituted phenyl group; A is an optionally substituted phenyl group; W is hydrogen or hydroxy; stereoisomers thereof and their pharmaceutically acceptable salts. The compounds possess selective neuroprotective activity and are useful in the treatment of an acute or a degenerative CNS disease. A process is described for preparing the compounds and pharmaceutical compositions containing them.
摘要翻译： PCT No.PCT / EP95 / 04075第 371日期1998年3月31日 102（e）1998年3月31日PCT PCT 1996年9月16日PCT公布。 公开号WO97 / 13769 日期1997年4月17日A式（I）的二取代哌啶化合物，其中R 1是氢; 溴 氯 直链或支链C 1 -C 5烷基; 直链或支链C 1 -C 5烷氧基; 或任选取代的苯基; R2是氢，直链或支链C1-C5烷基或任意取代的苯基; X是CH 2，C = O，CHOH或C = NOH; R3是氢或直链或支链C1-C5烷基; Y为（CH 2）n基团，其中n为0至4的整数，CHOH，C = O或CH-A，其中A为任选取代的苯基; A是任选取代的苯基; W是氢或羟基; 其立体异构体及其药学上可接受的盐。 该化合物具有选择性神经保护活性，可用于治疗急性或退行性CNS疾病。 描述了制备含有它们的化合物和药物组合物的方法。
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公开(公告)号：US5708030A
公开(公告)日：1998-01-13
申请号：US463895
申请日：1995-06-05
IPC分类号： A61K31/00 , A61K31/165 , A61K31/195 , A61K31/198 , A61K31/215 , A61K31/216 , C07C229/36 , C07C233/43 , C07C233/44 , C07C235/10 , A61K31/12 , A61K31/44 , A61K33/18
CPC分类号： C07C229/36 , A61K31/00 , A61K31/165 , A61K31/195 , A61K31/198 , A61K31/215 , A61K31/216 , C07C2101/08
摘要： The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT).
摘要翻译： 本发明涉及用于治疗与脑衰老过程相关的认知障碍和围产期脑疾病的化合物的用途，所述化合物作为犬尿氨酸转氨酶（KAT）酶的抑制剂。
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公开(公告)号：US5519055A
公开(公告)日：1996-05-21
申请号：US102843
申请日：1993-08-06
IPC分类号： A61K31/00 , A61K31/165 , A61K31/195 , A61K31/198 , A61K31/215 , A61K31/216 , C07C229/36 , C07C233/43 , C07C233/44 , C07C235/10 , A61K31/24 , C07C229/00
CPC分类号： C07C229/36 , A61K31/00 , A61K31/165 , A61K31/195 , A61K31/198 , A61K31/215 , A61K31/216 , C07C2101/08
摘要： The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT).The present invention also provides, as novel compounds, a selected class of KAT inhibitors which are the compounds of formula (IA) ##STR1## wherein R is halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.6 -C.sub.10 aryloxy, phenyl-C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, andR.sub.1 is hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, mono-C.sub.1 -C.sub.6 alkylamino, di-C.sub.1 -C.sub.6 alkylamino, hydroxylamino, C.sub.1 -C.sub.4 alkoxyamino or benzyloxyamino; with the provisos that(i) when R.sub.1 is hydroxy and, at the same time, R is halogen, then this halogen is not fluorine; and(ii) when R.sub.1 is hydroxy and, at the same time, R is C.sub.1 -C.sub.6 alkyl, then this C.sub.1 -C.sub.6 alkyl is not methyl, and the pharmaceutically acceptable salts thereof.
摘要翻译： 本发明涉及用于治疗与脑衰老过程相关的认知障碍和围产期脑疾病的化合物的用途，所述化合物作为犬尿氨酸转氨酶（KAT）酶的抑制剂。 本发明还提供作为新化合物的选定类别的KAT抑制剂，其是式（IA）化合物其中R是卤素，C 1 -C 6烷基，C 5 -C 7环烷基，苯基-C 1 -C 6烷基， C4烷基，C1-C6烷氧基，C6-C10芳氧基，苯基-C1-C4烷氧基或三氟甲基，R1为羟基，C1-C6烷氧基，氨基，单C1-C6烷基氨基，二C1-C6烷基氨基， C1-C4烷氧基氨基或苄氧基氨基; 条件是（i）当R 1是羟基，同时R是卤素时，该卤素不是氟; 和（ii）当R 1是羟基，并且同时R是C 1 -C 6烷基时，则该C 1 -C 6烷基不是甲基，及其药学上可接受的盐。
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