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    • 2. 发明授权
    • Tumor retarding (1,2-diphenyl-ethylenediamine)-platinum(II)-complexes
    • 抗肿瘤剂(1,2-二苯基 - 乙二胺) - 铂(II) - 复合物
    • US4730068A
    • 1988-03-08
    • US831913
    • 1986-02-21
    • Helmut SchonenbergerErwin von AngererJohann KarlMargaretha JennerweinJurgen Engel
    • Helmut SchonenbergerErwin von AngererJohann KarlMargaretha JennerweinJurgen Engel
    • A61K31/28A61P35/00C07C45/29C07C45/51C07C45/56C07C47/575C07F15/00
    • C07F15/0093C07C45/298C07C45/515C07C45/562C07C47/575
    • There are disclosed antitumor active 1,2-diphenyl-ethylenediamine)-platinum(II)-complex of the general formula ##STR1## wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.6 -alkyl and R.sub.2 is either (1) a halogen atom and the groups R.sub.1, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are the same or different and are hydrogen, halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydrogen C.sub.1 -C.sub.6 -alkoxy, a C.sub.2 -C.sub.6 -alkanoyloxy or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group, or R.sub.2 is (2) a hydroxy group, a C.sub.1 -C.sub.6 -alkoxy group, a C.sub.2 -C.sub.6 -alkanoyloxy group in the 4-position or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group and if R.sub.2 is (2) then the groups R.sub.1 and R.sub.3 which are the same or differnt are in the 2 and 6 positions of the phenyl group and are halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, a C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alklanoyloxy group or a halo or C.sub.1 -C.sub.5 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group, with the proviso that R.sub.1 can also be hydrogen and the groups R.sub.4, R.sub.5, and R.sub.6 are the same or different and are hydrogen, halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, a C.sub.2 -C.sub.6 -alkanoyloxy group or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group and X is the equivalent of a physiologically compatible anion and process of their production.
    • 公开了具有通式“IMAGE”I的抗肿瘤活性的1,2-二苯基 - 乙二胺) - 铂(II) - 复合物,其中R 7是氢或C 1 -C 6 - 烷基,R 2是(1)卤素原子, 基团R 1,R 3,R 4,R 5和R 6相同或不同,为氢,卤素,三卤甲基,C 1 -C 6 - 烷基,C 1 -C 6 - 烷氧基,C 2 -C 6 - 烷酰氧基或卤素或C 1 -C 4 - 烷磺酰氧基取代的C 2 -C 6 - 烷酰氧基,或R 2为(2)羟基,C 1 -C 6 - 烷氧基,C 4 -C 6 - 烷酰氧基或卤素或C 1 -C 4 - 烷磺酰氧取代 C 2 -C 6 - 烷酰氧基,如果R 2为(2),则相同或不同的基团R 1和R 3为苯基的2和6位,为卤素,三卤代甲基,C 1 -C 6烷基,羟基, C 1 -C 6 - 烷氧基,C 2 -C 6 - 烷酰氧基或卤素或C 1 -C 5 - 烷磺酰氧基取代的C 2 -C 6 - 烷酰氧基,条件是R 1也可以是氢,基团R 4,R 5和R 6是 相同或不同的 氢,卤素,三卤代甲基,C 1 -C 6 - 烷基,羟基,C 1 -C 6 - 烷氧基,C 2 -C 6 - 烷酰氧基或卤素或C 1 -C 4 - 烷磺酰氧基取代的C 2 -C 6 - 烷酰氧基,X等同于 生理上相容的阴离子及其生产方法。
    • 7. 发明授权
    • 2-phenylbenzo[B]furans, process for their manufacture and pharmaceutical
preparations containing them
    • 2-苯基苯并[b]呋喃,其制备方法和含有它们的药物制剂
    • US5470854A
    • 1995-11-28
    • US142462
    • 1994-04-14
    • Erwin von AngererSebastian ErberMartin Schneider
    • Erwin von AngererSebastian ErberMartin Schneider
    • A61K31/34A61K31/343A61K31/38A61K31/381A61P13/02A61P15/00A61P17/00A61P35/00C07D307/80C07D307/81C07D307/83C07D333/56C07D333/58A61K31/535C07D333/64
    • C07D333/58C07D307/80C07D307/81C07D333/56
    • 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.
    • 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。