公开(公告)号：US06197972B1

公开(公告)日：2001-03-06

申请号：US09251989

申请日：1999-02-17

申请人： Jan Heeres ,  Leo Jacobus Jozef Backx ,  Paul August Clement Luyts

发明人： Jan Heeres ,  Leo Jacobus Jozef Backx ,  Paul August Clement Luyts

IPC分类号： C07D40506

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

摘要： The present invention concerns novel compounds of formula (I). wherein R1 is C1-10alkyl, C3-7cycloalkyl or C1-6alkyl substituted with C3-7cycloalkyl; R2 is hydrogen or C1-6alkyl; Alk represents C1-3alkanediyl; —A— represents a bivalent radical of formula —CH═CH—N═CH— (a), —N═CH—N═CH— (b), —CH═N—N═CH— (c), —CH═CH—CH═N— (d); in said bivalent radicals a hydrogen atom may be replaced by C1-6alkyl; and Ar is unsubstituted phenyl; phenyl substituted with up to two substituents selected from halo, C1-6alkyl or C1—6alkyloxy; unsubstituted naphthyl; or naphthyl substituted with up to two substituents selected from halo, C1-6alkyl or C1-6alkyloxy; the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof. The present invention further comprises the pharmaceutical compositions comprising compounds of formula (I), the preparation thereof as well as the use as a medicine in the treatment of hyperlipidemia.

摘要翻译： 本发明涉及新的式（I）化合物，其中R 1是C 1-10烷基，C 3-7环烷基或被C 3-7环烷基取代的C 1-6烷基; R2是氢或C1-6烷基; Alk表示C1-3烷二基; -A-表示式-CH = CH-N = CH-（a），-N = CH-N = CH-（b），-CH = NN = CH-（c），-CH = CH -CH = N-（d）; 在所述二价基团中，氢原子可被C 1-6烷基取代; 和Ar是未取代的苯基; 被至多两个选自卤素，C 1-6烷基或C 1-6烷氧基的取代基取代的苯基; 未取代的萘基; 或被至多两个选自卤素，C 1-6烷基或C 1-6烷氧基的取代基取代的萘基; 其立体化学异构形式及其药学上可接受的酸加成盐。 本发明还包含包含式（I）化合物，其制备方法以及用作治疗高脂血症药物的药物组合物。

公开(公告)号：US5922718A

公开(公告)日：1999-07-13

申请号：US930847

申请日：1997-10-07

申请人： Jan Heeres ,  Leo Jacobus Josef Backx ,  Paul August Clement Luyts ,  Didier Robert Guy Gabriel de Chaffoy de Courcelles

发明人： Jan Heeres ,  Leo Jacobus Josef Backx ,  Paul August Clement Luyts ,  Didier Robert Guy Gabriel de Chaffoy de Courcelles

IPC分类号： C07D405/14 ,  A61K31/495 ,  A61P3/06 ,  C07D405/06 ,  C07D521/00 ,  C07D403/14

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

摘要： The present invention concerns novel compounds of formula (I). ##STR1## wherein R.sup.1 is C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl or C.sub.1-6 alkyl substituted with C.sub.3-7 cycloalkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; Alk represents C.sub.1-3 alkanediyl; --A-- represents a bivalent radical of formula --CH.dbd.CH--N.dbd.CH-- (a), --N.dbd.CH--N.dbd.CH-- (b), --CH.dbd.N--N.dbd.CH-- (c), --CH.dbd.CH--CH.dbd.N-- (d); in said bivalent radicals a hydrogen atom may be replaced by C.sub.1-6 alkyl; and Ar is unsubstituted phenyl; phenyl substituted with up to two substituents selected from halo, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; unsubstituted naphthyl; or naphthyl substituted with up to two substituents selected from halo, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof. The present invention further comprises the pharmaceutical compositions comprising compounds of formula (I), the preparation thereof as well as the use as a medicine in the treatment of hyperlipidemia.

摘要翻译： PCT No.PCT / EP96 / 01585第 371日期1997年10月7日第 102（e）日期1997年10月7日PCT 1996年4月12日PCT PCT。 WO96 / 33193 PCT出版物 日期：1996年10月24日本发明涉及新的式（I）化合物。 其中R 1是C 1-10烷基，C 3-7环烷基或被C 3-7环烷基取代的C 1-6烷基; R2是氢或C1-6烷基; Alk表示C1-3烷二基; -A-表示式-CH = CH-N = CH-（a），-N = CH-N = CH-（b），-CH = NN = CH-（c），-CH = CH -CH = N-（d）; 在所述二价基团中，氢原子可被C 1-6烷基取代; 和Ar是未取代的苯基; 被至多两个选自卤素，C 1-6烷基或C 1-6烷氧基的取代基取代的苯基; 未取代的萘基; 或被至多两个选自卤素，C 1-6烷基或C 1-6烷氧基的取代基取代的萘基; 其立体化学异构形式及其药学上可接受的酸加成盐。 本发明还包含包含式（I）化合物，其制备方法以及用作治疗高脂血症药物的药物组合物。