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公开(公告)号：US5041461A
公开(公告)日：1991-08-20
申请号：US412686
申请日：1989-09-26
IPC分类号： A61K31/38 , A61K31/381 , A61K31/40 , A61P25/00 , C07C69/708 , C07D333/38 , C07D409/12
CPC分类号： C07D409/12 , C07D333/38
摘要： A pharmaceutically-active compound of the formula ##STR1## in which R.sup.1 is C.sub.1-4 alkythio, C.sub.1-4 alkylsulphinyl or C.sub.1-4 alkylsulphonyl, R.sup.2 is C.sub.1-4 alkyl, R.sup.3 is C.sub.1-4 alkyl or C.sub.2-4 alkenyl, and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.2 --, and n is 1, 2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a C.sub.1-3 alkylene chain; and salts thereof.
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公开(公告)号：US5021449A
公开(公告)日：1991-06-04
申请号：US412685
申请日：1989-09-26
IPC分类号： A61K31/40 , A61K31/4025 , A61P1/08 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D409/12
CPC分类号： C07D409/12
摘要： A pharmaceutical compound of the formula ##STR1## in which R.sup.1 is --CHO, CH.sub.2 OH, --CH.sub.2 OC.sub.1-4 alkyl, --COC.sub.1-3 alkyl, --CH(OH)C.sub.1-3 alkyl or --COOH, R.sup.2 is C.sub.1-4 alkyl, --CHO, --CH.sub.2 OH, --CH.sub.2 OC.sub.1-4 alkyl, --COC.sub.1-3 alkyl, --CH(OH)C.sub.1-3 alkyl or --COOH, R.sup.3 is C.sub.1-4 alkyl and X is pyrrolidinyl or pyrrolidinylmethyl; and salts and esters thereof.
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公开(公告)号：US5015656A
公开(公告)日：1991-05-14
申请号：US412691
申请日：1989-09-26
IPC分类号： A61K31/38 , A61K31/381 , A61K31/40 , A61P1/08 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D333/38 , C07D409/12
CPC分类号： C07D409/12 , C07D333/38
摘要： A pharmaceutical compound of the formula ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen, hydroxy, halo, nitro, amino, C.sub.2-5 acylamino, C.sub.1-4 alkyl, --CHO, --CH.sub.2 OH, --CH.sub.2 OC.sub.1-4 alkyl, --COOH, --COC.sub.1-3 alkyl, --CH(OH)C.sub.1-3 alkyl, C.sub.1-4 alkoxy, C.sub.2-4 alkenyloxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphinyl, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene bridge; provided that at least one of R.sup.2 and R.sup.3 is C.sub.1-4 alkoxy or C.sub.2-4 alkenyloxy; and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.2 --, and n is 1, 2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a C.sub.1-3 alkylene chain; and salts and esters thereof.
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公开(公告)号：US5631250A
公开(公告)日：1997-05-20
申请号：US410474
申请日：1995-03-24
IPC分类号： C07D495/04 , A61K31/55 , C07D243/10
CPC分类号： C07D495/04
摘要： The invention provides lower alcohol solvates of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine (olanzapine) and a process for making such lower alcohol solyates of olanzapine. The invention provides a method for using such solyates of olanzapine to prepare substantially pure anhydrous Form I 2-methyl-thieno-benzodiazepine.
摘要翻译： 本发明提供2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂（奥氮平）的低级醇溶剂化物和制备这种低级醇的方法 奥氮平的盐酸盐。 本发明提供了使用这种奥氮平醋酸盐制备基本上纯的无水形式I 2-甲基 - 噻吩并 - 苯并二氮杂的方法。
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公开(公告)号：US5605897A
公开(公告)日：1997-02-25
申请号：US387498
申请日：1995-02-13
IPC分类号： A61K31/551 , A61K31/5513 , A61K31/55
CPC分类号： A61K31/5513 , A61K31/551
摘要： Olanzapine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system. The compound has the following structure: ##STR1##
摘要翻译： 奥氮平或其酸式盐具有药物性质，并且特别用于治疗中枢神经系统疾病。 该化合物具有以下结构：
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6.发明授权Pyrazolo-[3,4-g]isoquinoline derivatives useful to treat CNS disorders 失效吡唑并[3,4-g]异喹啉衍生物可用于治疗CNS疾病
公开(公告)号：US4963558A
公开(公告)日：1990-10-16
申请号：US447319
申请日：1989-12-07
CPC分类号： C07D471/04
摘要： Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 is hydrogen or C.sub.1-6 alkyl, R.sup.2 is hydrogen, C.sub.1-6 alkyl optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, C.sub.3-9 cycloalkyl, optionally substituted phenyl, or --SR.sup.4 where R.sup.4 is C.sub.1-6 alkyl optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, or C.sub.3-9 cycloalkyl, R.sup.3 is hydrogen, C.sub.1-6 alkyl optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, c.sub.3-9 cycloalkyl, or optionally phenyl, and either X and Y are both hydrogen or together are .dbd.O; and acid addition salts thereof. These compounds show useful effects on the central nervous system.
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公开(公告)号：US5627178A
公开(公告)日：1997-05-06
申请号：US387997
申请日：1995-02-13
IPC分类号： A01N43/62 , A61K31/551 , A61K31/5513 , C07D243/10 , A61K31/55
CPC分类号： A61K31/551 , A61K31/5513
摘要： 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system. The compound has the following structure: ##STR1##
摘要翻译： 2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂或其酸式盐具有药物性质，具有特别的用途 在治疗中枢神经系统疾病。 该化合物具有以下结构：
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公开(公告)号：US5229382A
公开(公告)日：1993-07-20
申请号：US890348
申请日：1992-05-22
IPC分类号： C07D333/38 , C07D495/04
CPC分类号： C07D495/04 , C07D333/38
摘要： 2-Methyl-10-(4-methyl-1-piperazinyl)-4H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system. The compound has the following structure: ##STR1##
摘要翻译： 2-甲基-10-（4-甲基-1-哌嗪基）-4H-噻吩并[2,3-b] [1,5]苯并二氮杂或其酸式盐具有药物性质，具有特别的用途 在治疗中枢神经系统疾病。 该化合物具有以下结构：
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公开(公告)号：US4904686A
公开(公告)日：1990-02-27
申请号：US179601
申请日：1988-04-11
IPC分类号： C07D333/10 , A61K31/38 , A61K31/381 , A61K31/41 , A61K31/415 , A61P25/00 , C07D333/38 , C07D333/42 , C07D409/12 , C07D409/14
CPC分类号： C07D409/12 , C07D333/38 , C07D409/14
摘要： Compounds of the following formula have pharmacutical properties: ##STR1## in which R.sup.1 and R.sup.2 independently are hydrogen, halo, nitro, amino, C.sub.2-5 acylamino, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene bridge, R.sup.3 is C.sub.1-4 alkyl or C.sub.2-4 alkenyl, and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.2 --, and n is 1, 2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a C.sub.1-3 alkylene chain; and salts thereof.
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公开(公告)号：US5051516A
公开(公告)日：1991-09-24
申请号：US562055
申请日：1990-08-02
IPC分类号： C07D277/20 , A61K31/00 , A61K31/55 , A61P25/18 , A61P25/20 , C07D277/56 , C07D513/04
CPC分类号： C07D513/04 , C07D277/56
摘要： Pharmaceutical thiazolo-[1,5]benzodiazepines of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, halogen, C.sub.1-4 haloalkyl, nitro, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio or phenylsulphonyl; in which R.sup.5 is a group of the formula formula ##STR2## where R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, benzyl or ZO--C.sub.2-6 alkyl where Z is hydrogen or an acyl group, R.sup.8 is hydrogen or C.sub.1-4 alkyl and n is 0 or 1, provided that when R.sup.7 is hydrogen n is 0; in which R.sup.6 is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkylthio; and in which ##STR3## represents a thiazole ring selected from ##STR4## and acid addition salts thereof. The compounds have central nervous system activity.
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