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1. 发明授权

US4675334A Tetrazolyl compounds and their use as anti allergic agents 失效
标题翻译：四唑基化合物及其作为抗过敏剂的用途
公开(公告)号：US4675334A
公开(公告)日：1987-06-23
申请号：US629647
申请日：1984-07-11
申请人： David J. Steggles , John P. Verge
发明人： David J. Steggles , John P. Verge
IPC分类号： A61K31/41 , A61P11/00 , A61P11/06 , A61P37/08 , A61P43/00 , C07C45/71 , C07C49/84 , C07C67/00 , C07C253/00 , C07C255/32 , C07C255/37 , C07C255/53 , C07C325/00 , C07C331/02 , C07C331/10 , C07D257/04 , C07C121/52 , C07C161/02
CPC分类号： C07D257/04 , C07C255/00 , C07C331/10 , C07C45/71 , C07C49/84
摘要： Compounds of formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently selected from H, OH, C.sub.1 -C.sub.4 alkyl, R.sub.4 --CO and halogen, where R.sub.4 is C.sub.1 -C.sub.4 alkyl; R.sub.5 and R.sub.6 are each independently selected from H, C.sub.1 -C.sub.4 alkyl and optionally-substituted phenyl; R.sub.7 is an alkylene group having from 1 to 4 carbon atoms, optionally containing a substituted or unsubstituted phenyl group; p is 0 or 1; and Z is a 1H-tetrazol-5-yl or a --CN group; and salts thereof, may be prepared by reacting a compound of formula. ##STR2## with a compound of formula ##STR3## wherein R.sub.1 -R.sub.7 are as defined in claim 1, in an organic solvent at a temperature in the range of 40.degree.-120.degree. C. in the presence of a base, and reacting the resulting compound with an alkali metal cyanide or thiocyanate, and optionally reacting the resulting compound with a source of azide ions to produce pharmacologically active compounds of formula I wherein Z is 1H-tetrazol-5-yl.
摘要翻译：式（I）的化合物其中R 1，R 2和R 3各自独立地选自H，OH，C 1 -C 4烷基，R 4 -CO和卤素，其中R 4是C 1 -C 4烷基; R 5和R 6各自独立地选自H，C 1 -C 4烷基和任选取代的苯基; R7是具有1至4个碳原子的亚烷基，任选地含有取代或未取代的苯基; p为0或1; Z为1H-四唑-5-基或-CN基; 和其盐可以通过使式的化合物反应来制备。其中R 1 -R 7如权利要求1中所定义，在有机溶剂中，在碱存在的情况下，在40-120℃的温度下，使式得到的化合物与碱金属氰化物或硫氰酸盐反应，并任选地使所得化合物与叠氮离子源反应，以产生其中Z为1H-四唑-5-基的药理学活性的式I化合物。

2. 发明授权

US4675333A N-[4-[.omega.-(4-acyl-3-hydroxyphenoxy)alkoxy]-p henyl]1H-tetrazole-5-carboxamides and use thereof as anti-allergics 失效
标题翻译： N- [4- [ω-（4-酰基-3-羟基苯氧基）烷氧基] - 苯基] 1H-四唑-5-甲酰胺及其作为抗变态反应的用途
公开(公告)号：US4675333A
公开(公告)日：1987-06-23
申请号：US678445
申请日：1984-12-05
申请人： David J. Steggles , John P. Verge
发明人： David J. Steggles , John P. Verge
IPC分类号： A61K31/41 , A61P11/00 , A61P11/06 , C07C205/37 , C07D257/04
CPC分类号： C07D257/04 , C07C205/37 , Y02P20/55
摘要： There are described 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 or C.sub.3-6 alkenyl, R.sup.3 is hydrogen or C.sub.1-6 alkyl, R.sup.4 is hydrogen or an N-protecting group, n is 2, 3, 4 or 5, and X is oxygen, sulphur or --CH.sub.2 --, provided that when X is --CH.sub.2 -- n is 0; and salts thereof. The compounds in which R.sup.4 is hydrogen have pharmaceutical activity.
摘要翻译：描述了式（I）的化合物，其中R 1是氢或C 1-6烷基，R 2是氢，C 1-6烷基或C 3-6烯基，R 3是氢或C 1-6烷基，R 4是氢或N-保护基，n为2,3,4或5，并且X为氧，硫或-CH 2 - ，条件是当X为-CH 2时，n为0; 及其盐。其中R4为氢的化合物具有药物活性。

3. 发明授权

US4431589A Benzodiazepine compounds and their use as pharmaceuticals 失效
标题翻译：苯二氮卓类化合物及其作为药物的用途
公开(公告)号：US4431589A
公开(公告)日：1984-02-14
申请号：US327143
申请日：1981-12-03
申请人： Jiban K. Chakrabarti , Terrence M. Hotten , David J. Steggles
发明人： Jiban K. Chakrabarti , Terrence M. Hotten , David J. Steggles
IPC分类号： C07D243/12 , A61K31/00 , A61K31/55 , A61K31/5517 , A61P1/08 , A61P25/18 , A61P25/20 , C07D243/28 , C07D249/04 , C07D487/04
CPC分类号： C07D487/04 , C07D249/04
摘要： These are described compounds of formula (I) ##STR1## or an acid addition salt thereof; in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent 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 ##STR2## where R.sup.7 is hydrogen or C.sub.1-6 alkyl, 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; and in which R.sup.6 is attached to the 1, 2 or 3 position of the triazole ring and is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, phenyl, benzyl or acyl. These compounds are pharmaceutically active and are especially useful in the treatment of disorders of the central nervous system. They are prepared by reacting an amine of formula R.sup.5 H with a triazolobenzodiazepine intermediate appropriately substituted at the 10-position or by ring-closing the appropriate anilinotriazole.
摘要翻译：这些是式（I）化合物或其酸加成盐; 其中R 1，R 2，R 3和R 4独立地表示氢，C 1-4烷基，C 2-4烯基，卤素，C 1-4卤代烷基，硝基，C 1-4烷氧基，C 1-4卤代烷氧基，C 1-4烷硫基或苯基磺酰基。其中R 5是下式的基团，其中R 7是氢或C 1-6烷基，R 8是氢或C 1-4烷基，n是0或1，条件是当R 7是氢时，n是0; 并且其中R6连接到三唑环的1,2或3位，并且是氢，C 1-10烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基，苄基或酰基。这些化合物是药学活性的并且特别可用于治疗中枢神经系统疾病。它们通过使式R5H的胺与在10位适当取代的三唑并苯并二氮杂中间体或通过闭环合适的苯胺三唑反应来制备。

4. 发明授权

US5158971A Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US5158971A
公开(公告)日：1992-10-27
申请号：US705191
申请日：1991-05-24
申请人： Trafford Clarke , David J. Steggles
发明人： Trafford Clarke , David J. Steggles
IPC分类号： C07D333/24 , A61K31/38 , A61K31/381 , A61P37/08 , A61P43/00 , C07D333/20 , C07D333/34
CPC分类号： C07D333/34 , C07D333/20
摘要： A pharmaceutical compound of the formula ##STR1## in which R.sup.1 is halo-C.sub.1-10 alkyl, C.sub.1-10 alkylthio, halo-C.sub.1-10 alkylthio or optionally substituted phenylthio, R.sup.2 is hydrogen or C.sub.1-4 alkyl, R.sup.3 and R.sup.4 are each hydrogen or C.sub.1-4 alkyl, and X is oxygen or sulphur; and salts thereof.

5. 发明授权

US4492699A Triazolobenzodiazepine derivatives 失效
标题翻译：三唑并苯并二氮杂衍生物
公开(公告)号：US4492699A
公开(公告)日：1985-01-08
申请号：US541605
申请日：1983-10-13
申请人： Jiban K. Chakrabarti , Terrence M. Hotten , David J. Steggles
发明人： Jiban K. Chakrabarti , Terrence M. Hotten , David J. Steggles
IPC分类号： C07D243/12 , A61K31/00 , A61K31/55 , A61K31/5517 , A61P1/08 , A61P25/18 , A61P25/20 , C07D243/28 , C07D249/04 , C07D487/04 , A61K31/495
CPC分类号： C07D487/04 , C07D249/04
摘要： These are described compounds of formula (I) ##STR1## or an acid addition salt thereof; in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent 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 ##STR2## where R.sup.7 is hydrogen or C.sub.1-6 alkyl, 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; and in which R.sup.6 is attached to the 1, 2 or 3 position of the triazole ring and is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, phenyl, benzyl or acyl. These compounds are pharmaceutically active and are especially useful in the treatment of disorders of the central nervous system. They are prepared by reacting an amine of formula R.sup.5 H with a triazolobenzodiazepine intermediate appropriately substituted at the 10-position or by ring-closing the appropriate anilinotriazole.

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