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1. 发明授权

US5470854A 2-phenylbenzo[B]furans, process for their manufacture and pharmaceutical preparations containing them 失效
标题翻译： 2-苯基苯并[b]呋喃，其制备方法和含有它们的药物制剂
公开(公告)号：US5470854A
公开(公告)日：1995-11-28
申请号：US142462
申请日：1994-04-14
申请人： Erwin von Angerer , Sebastian Erber , Martin Schneider
发明人： Erwin von Angerer , Sebastian Erber , Martin Schneider
IPC分类号： A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61P13/02 , A61P15/00 , A61P17/00 , A61P35/00 , C07D307/80 , C07D307/81 , C07D307/83 , C07D333/56 , C07D333/58 , A61K31/535 , C07D333/64
CPC分类号： C07D333/58 , C07D307/80 , C07D307/81 , C07D333/56
摘要： The invention relates to new furans and thiophenes with the general Formula 1, ##STR1## in which R.sup.1 and R.sup.2 independently of one another denote a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, a benzyl group, a group C(O)R.sup.4, where R.sup.4 is an alkyl or alkoxy group having 1 to 10 carbon atoms or a phenyl radical, or a carbamoyl group --C(O)NR.sup.5 R.sup.6, where R.sup.5 and R.sup.6 independently of one another are a hydrogen atom or an alkyl group having 1 to 10 carbon atoms, and n denotes an integer from 0 to 12 if R.sup.3 is a hydrogen atom, or n denotes an integer from 4 to 12 if R.sup.3 is an amino group --NR.sup.7 R.sup.8, where R.sup.7 and R.sup.8 independently of one another represent a hydrogen atom or an alkyl group having 1 to 10 carbon atoms or R.sup.7 and R.sup.8 together represent an alkylene group --(CH.sub.2).sub.m -- or the group --(CH.sub.2).sub.2 -- or R.sup.3 denotes an amide group --C(O)NR.sup.7 R.sup. 8, where R.sup.7 and R.sup.8 have the abovementioned meanings, or R.sup.3 denotes a sulphinyl group --S(O)R.sup.3, where R.sup.9 is the radical --(CH.sub.2).sub.m (CF.sub.2).sub.o CF.sub.3 and m and o are 2, 3, 4, 5 or 6 and x denotes an oxygen or sulphur atom. These new compounds are strong and selective anti-oestrogens, and have therapeutic applications in the treatment of oestrogen-related illnesses.
摘要翻译： PCT No.PCT / DE92 / 00435 Sec。 371日期1994年04月14日 102（e）日期1994年4月14日PCT提交1992年5月25日PCT公布。 WO92 / 21669 PCT出版物本发明涉及具有通式1，其中R 1和R 2彼此独立地表示氢原子，具有1至10个碳原子的烷基的通式1的新的呋喃和噻吩，苄基，C（O）R 4，其中R 4是具有1-10个碳原子的烷基或烷氧基或苯基，或氨基甲酰基-C（O）NR 5 R 6，其中R 5和R 6独立地为一个另一个为氢原子或碳原子数为1〜10的烷基，如果R 3为氢原子，则n为0〜12的整数，如果R 3为氨基-NR 7 R 8，n为4〜12的整数，其中R 7和R 8彼此独立地表示氢原子或具有1至10个碳原子的烷基，或者R 7和R 8一起表示亚烷基 - （CH 2）m - 或基团 - （CH 2）2 - 或R 3表示酰胺基-C（O）NR 7 R 8，其中R 7和R 8具有上述含义，或R 3表示亚磺酰基-S（O）R 3，其中R 9是基团 - （CH 2）m（CF 2）o CF 3，m 和o是2,3,4,5或6，x表示氧或硫原子。这些新化合物是强和选择性的抗雌激素，并且具有治疗雌激素相关疾病的治疗应用。

2. 发明授权

US06291639B1 Metal-binding cystein-free peptides for diagnostic and therapeutical purposes, methods for their production, and pharmaceuticals containing these compounds 失效
标题翻译：用于诊断和治疗目的的金属结合半胱氨酸肽，其生产方法和含有这些化合物的药物
公开(公告)号：US06291639B1
公开(公告)日：2001-09-18
申请号：US08635928
申请日：1996-09-20
申请人： Jurgen Conrad , Ludger Dinkelborg , Sebastian Erber , Cornelius Frommel , Wolfgang Hohne , Wolfgang Kramp , Gabriele Kuttner , Reinhard Malin , Hans Martin Schier , Jens Schneider-Mergener , Renate Steinbrecher
发明人： Jurgen Conrad , Ludger Dinkelborg , Sebastian Erber , Cornelius Frommel , Wolfgang Hohne , Wolfgang Kramp , Gabriele Kuttner , Reinhard Malin , Hans Martin Schier , Jens Schneider-Mergener , Renate Steinbrecher
IPC分类号： A61K3804
CPC分类号： C07K7/06 , A61K51/08 , A61K51/088 , C07K14/57536 , C07K16/18 , C07K2319/00
摘要： These invention relates to metal-complexing, cysteine-free peptides which may be coupled to an organ-specific probe directly or via a linker and are thus enriched as conjugates specifically in tumors, organs, tissues or centers of inflammation. The organ-specific probes used are, for example, antibodies or part-sequences of antibodies against tumor-associated antigens, e.g. the carcino-embryonal antigen (CEA, which are thus specifically enriched in tumors. The invention also relates to processes for producing the metal-complexing cysteine-free peptides and their conjugates. The present invention also relates to the use of the conjugates as components of a kit for in vivo diagnosis or in vivo therapy and radio-pharmaceuticals containing these conjugates together with radio-isotopes. The organ-specific conjugates are used to image tumors, organs or centers of inflammation.
摘要翻译：这些发明涉及金属络合，不含半胱氨酸的肽，其可以直接或经由接头偶联到器官特异性探针，并因此在肿瘤，器官，组织或炎症中心中特异性地富集为缀合物。使用的器官特异性探针是例如针对肿瘤相关抗原的抗体或部分序列，例如抗体。癌胚抗原（CEA，因此特异性富集肿瘤）本发明还涉及生产金属络合半胱氨酸的肽及其缀合物的方法，本发明还涉及缀合物作为用于体内诊断或体内治疗的试剂盒和含有这些共轭物的放射性药物和放射性同位素。器官特异性缀合物用于成像肿瘤，器官或炎症中心。

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