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1. 发明申请

WO1986003488A1 INDENE ANALOGS OF MEVALONOLACTONE AND DERIVATIVES THEREOF 审中-公开
标题翻译：梅洛酮及其衍生物的衍生物类似物
公开(公告)号：WO1986003488A1
公开(公告)日：1986-06-19
申请号：PCT/EP1985000653
申请日：1985-11-29
申请人： SANDOZ AG
发明人： SANDOZ AG , KATHAWALA, Faizulla, G. , WATTANASIN, Sompong
IPC分类号： C07C69/738
CPC分类号： C07D309/30 , C07C17/2632 , C07C45/00 , C07C47/24 , C07C47/57 , C07C25/22
摘要： Compounds of formula (I), wherein R is hydrogen or primary or secondary C1-6alkyl, R1 is primary or secondary C1-6alkyl or R and R1 together are (CH2)m or (Z)-CH2-CH=CH-CH2- wherein m is 2, 3, 4, 5 or 6, Ro is C1-6alkyl, C3-7cycloalkyl or ring A (II) each or R2 and R4 is independently hydrogen, C1-4alkyl, C1-4alkoxy (except t-butoxy), trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, each of R3 and R5 is independently hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R6 is hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, with the proviso that there may only be one each of trifluoromethyl, phenoxy or benzyloxy on each of the phenyl and indene rings X is -(CH2)n - or - (CH2)qCH=CH(CH2)q- wherein n is 1, 2 or 3 and both q's are 0 or one is 0 and the other is 1, and Z is (III) wherein Q is (IV) wherein each R7 is the same primary or secondary C1-6alkyl or together they represent -(CH2)2-, -(CH2)3-, R10 is hydrogen or C1-3alkyl, with the proviso that Q may be other than (V) only when X is -CH=CH- or -CH2-CH=CH- and/or R10 is C1-3alkyl, in free acid form, or in the form of an ester or -lactone thereof or in salt form as appropriate, which are indicated for use as hypolipoproteinemic and anti-atherosclerotic agents.
摘要翻译：式（I）化合物，其中R是氢或伯或仲C 1-6烷基，R 1是伯或仲C 1-6烷基或R和R 1一起是（CH 2）m或（Z）-CH 2 -CH = CH-CH 2 - 其中m为2,3,4,5或6，Ro为C 1-6烷基，C 3-7环烷基或环A（II）或R 2和R 4独立地为氢，C 1-4烷基，C 1-4烷氧基（除了叔丁氧基）三氟甲基，氟，氯，苯氧基或苄氧基，R3和R5各自独立地是氢，C1-3烷基，C1-3烷氧基，三氟甲基，氟，氯，苯氧基或苄氧基，R6是氢，C1-2烷基，C1-2烷氧基，氟或氯，条件是每个苯基和茚环中只有一个三氟甲基，苯氧基或苄氧基，X是 - （CH 2）n - 或 - （CH 2）q CH = CH（CH 2）q-，其中 n为1,2或3，q为0或1为0，另一个为1，Z为（III）其中Q为（Ⅳ），其中每个R 7为相同的伯或仲C 1-6烷基或一起代表 - （CH 2）2 - ， - （CH 2）3 - ，R 10是氢或C 1-3烷基，条件是或者以酯或内酯的形式，当X是-CH = CH-或-CH 2 -CH = CH-和/或R 10是C 1-3烷基时，Q可以不同于（V）或适当的盐形式，其被指示用作低脂蛋白血症和抗动脉粥样硬化剂。

2. 发明申请

WO1988001997A2 AZAINDOLE AND INDOLIZINE DERIVATIVES, PROCESSES FOR THEIR PRODUCTION AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译：吖啶和吲哚啉衍生物，其生产方法及其作为药物的用途
公开(公告)号：WO1988001997A2
公开(公告)日：1988-03-24
申请号：PCT/EP1987000511
申请日：1987-09-09
申请人： SANDOZ AG
发明人： SANDOZ AG , ANDERSON, Paul, LeRoy , KATHAWALA, Faizulla, Gulamhusein , PAOLELLA, Nicholas, Andrew , WATTANASIN, Sompong
IPC分类号： C07D41/04
CPC分类号： C07D471/04
摘要： Compounds of formula (I), wherein: either one Y is -N- and the remainder are -CH-; X is a compound of formula (II); X is a compound of formula (III), with appropriate bond formation; R1 is a primary or secondary alkyl, free of asymmetric carbon atoms; R2 is a substituted or unsubstituted phenyl, primary or secondary C1-6 alkyl, free of asymmetric carbon atoms, C3-6 cycloalkyl or phenylalkyl as defined in the specification; A is a) a compound of formula (IV) or (V), b) -(CH2)n-, wherein n is 1, 2 or 3; Z is a) a compound of formula (VI), b) a compound of formula (VII), in which R8 is hydrogen, R9 or M, wherein R9 is a physiologically acceptable and hydrolysable ester group, and M is a pharmaceutically acceptable cation; or: each Y is -CH-, X is -N-, X is a compound of formula (VIII), with appropriate bond formation; R1 and R2 are independently as defined under R2 above and R2 may additionally be hydrogen; A and Z are as defined above. Said compounds are obtained by multi-step processes and are useful as hypolipoproteinemic and anti-atherosclerotic agents.
摘要翻译：式（I）的化合物，其中：Y中的一个为-N-，其余为-CH-; X是式（II）的化合物; X 1是式（III）的化合物，具有适当的键形成; R1是不含不对称碳原子的伯或仲烷基; R2是取代或未取代的苯基，不含不对称碳原子的伯或仲C 1-6烷基，如说明书中定义的C 3-6环烷基或苯基烷基; A是a）式（IV）或（V）的化合物，b） - （CH 2）n - ，其中n是1,2或3; Z是a）式（VI）化合物，b）式（VII）化合物，其中R 8是氢，R 9或M，其中R 9是生理上可接受和可水解的酯基，M是药学上可接受的阳离子 ; 或：每个Y是-CH-，X是-N-，X 1是式（VIII）的化合物，具有适当的键形成; R1和R2独立地如上述R2所定义，R2可以另外是氢; A和Z如上所定义。所述化合物通过多步法获得，可用作低脂蛋白血症和抗动脉粥样硬化剂。

3. 发明授权

EP0216785B1 INDENE ANALOGS OF MEVALONOLACTONE AND DERIVATIVES THEREOF 失效
标题翻译：甲氧基酮及其衍生物的衍生物类似物
公开(公告)号：EP0216785B1
公开(公告)日：1991-01-30
申请号：EP86900099.2
申请日：1985-11-29
申请人： SANDOZ AG , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN Verwaltungsgesellschaft m.b.H.
发明人： KATHAWALA, Faizulla, G. , WATTANASIN, Sompong
IPC分类号： C07C69/738 , C07C69/732 , C07C59/90 , C07C59/56 , C07C59/54 , C07D309/30 , A61K31/365 , A61K31/22 , A61K31/19
CPC分类号： C07D309/30 , C07C17/2632 , C07C45/00 , C07C47/24 , C07C47/57 , C07C25/22
摘要： Compounds of formula (I), wherein R is hydrogen or primary or secondary C1-6alkyl, R1 is primary or secondary C1-6alkyl or R and R1 together are (CH2)m or (Z)-CH2-CH=CH-CH2- wherein m is 2, 3, 4, 5 or 6, Ro is C1-6alkyl, C3-7cycloalkyl or ring A (II) each or R2 and R4 is independently hydrogen, C1-4alkyl, C1-4alkoxy (except t-butoxy), trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, each of R3 and R5 is independently hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R6 is hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, with the proviso that there may only be one each of trifluoromethyl, phenoxy or benzyloxy on each of the phenyl and indene rings X is -(CH2)n - or - (CH2)qCH=CH(CH2)q- wherein n is 1, 2 or 3 and both q's are 0 or one is 0 and the other is 1, and Z is (III) wherein Q is (IV) wherein each R7 is the same primary or secondary C1-6alkyl or together they represent -(CH2)2-, -(CH2)3-, R10 is hydrogen or C1-3alkyl, with the proviso that Q may be other than (V) only when X is -CH=CH- or -CH2-CH=CH- and/or R10 is C1-3alkyl, in free acid form, or in the form of an ester or -lactone thereof or in salt form as appropriate, which are indicated for use as hypolipoproteinemic and anti-atherosclerotic agents.

4. 发明公开

EP0216785A1 INDENE ANALOGS OF MEVALONOLACTONE AND DERIVATIVES THEREOF 失效
标题翻译： INDEN类似物MEVALONOLAKTON及其衍生物。
公开(公告)号：EP0216785A1
公开(公告)日：1987-04-08
申请号：EP86900099.0
申请日：1985-11-29
申请人： SANDOZ AG , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN Verwaltungsgesellschaft m.b.H.
发明人： KATHAWALA, Faizulla, G. , WATTANASIN, Sompong
IPC分类号： C07C , C07D , C07C43 , A61K31 , C07C17 , C07C27 , C07C33 , C07C41 , C07C45 , C07C47 , C07C51 , C07C57 , C07C59 , C07C67 , C07C69 , C07D309 , C07F7
CPC分类号： C07D309/30 , C07C17/2632 , C07C45/00 , C07C47/24 , C07C47/57 , C07C25/22
摘要： Des composés ont la formule générale (I), dans laquelle R est hydrogène ou C1-6alcoyle primaire ou secondaire, R1 est C1-6 alcoyle primaire ou secondaire ou R et R1 ensemble sont (CH2)m ou (Z)-CH2-CH=CH-CH2-, m étant égal à 2, 3, 4, 5 ou 6, Ro est C1-6alcoyle, C3-7 cycloalcoyle ou un anneau A (II), R2 et R4 sont indépendamment de l'hydrogène, C1-4alcoyle, C1-4alkoxy (sauf t-butoxy), trifluorométhyle, fluor, chlore, phénoxy ou benzyloxy, R3 et R5 sont indépendamment de l'hydrogène, C1-3alcoyle, C1-3alkoxy, trifluorométhyle, fluor, chlore ou benzyloxy, R6 est de l'hydrogène, C1-2alcoyle, C1-2alkoxy, fluor ou chlore, à condition qu'il y ait un seul trifluorométhyle, phénoxy ou benzyloxy dans chaque anneau phényle ou indène, X est - (CH2)n - ou - (CH2)q CH=CH(CH2)q- dans laquelle n est égal à 1,2 ou 3 et les deux q sont égaux à 0, ou un q est égal à 0 et l'autre est égal à 1, et Z a la formule (III), dans laquelle Q est égal à (IV) dans laquelle chaque R7 représente le même C1-6alcoyle primaire ou secondaire, ou ensemble ils représentent -(CH2)2-, -(CH2)3-, R10 est de l'hydrogène ou C1-3alcoyle, à condition que Q soit différent de (V) uniquement lorsque X est égal à -CH=CH- ou -CH2-CH=CH-et/ou R10 est égal à C1-3alcoyle sous forme acide libre, ou sous forme d'un ester ou d'une lactone de ces composés, ou sous forme d'un sel, selon ce qui convient. Ces composés sont indiqués comme agents hypolipoprotéinémiques ou comme agents anti-artériosclérotiques.

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