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    7ALPHA-(EPSILON-AMINOALKYL)-ESTRATRIENE, VERFAHREN ZU DEREN HERSTELLUNG, PHARMAZEUTISCHE PRÄPARATE, DIE DIESE 7ALPHA-(EPSILON-AMINOALKYL)-ESTRATRIENE ENTHALTEN SOWIE DEREN VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN
    1.
    发明公开
    7ALPHA-(EPSILON-AMINOALKYL)-ESTRATRIENE, VERFAHREN ZU DEREN HERSTELLUNG, PHARMAZEUTISCHE PRÄPARATE, DIE DIESE 7ALPHA-(EPSILON-AMINOALKYL)-ESTRATRIENE ENTHALTEN SOWIE DEREN VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN 失效
    7ALPHA-（ε-己氨基烷基） - 雌三烯，PROCESS FOR PRODUCING药物制剂THAT THIS 7ALPHA-（ε-己氨基烷基） - 雌三烯容纳和它们在药物的生产

    公开(公告)号：EP0920441A1

    公开(公告)日：1999-06-09

    申请号：EP97943814.0

    申请日：1997-08-20

    申请人： SCHERING AKTIENGESELLSCHAFT

    发明人： BOHLMANN, Rolf ,  BITTLER, Dieter ,  HEINDI, Josef ,  HEINRICH, Nikolaus ,  HOFMEISTER, Helmut ,  KÜNZER, Hermann ,  SAUER, Gerhard ,  HEGELEHARTUNG, Christa ,  LICHTNER, Rosemarie ,  NISHINO, Yukishige ,  PARCZYK, Karsten ,  SCHNEIDER, Martin

    IPC分类号： A61K31 ,  A61P5 ,  C07J41 ,  C07J43 ,  C07J53

    CPC分类号： C07J53/008 ,  C07J41/0072 ,  C07J43/006 ,  C07J53/002

    摘要： The present invention describes new substituted 7α-(κ-aminoalkyl)-estratrienes of general formula (I), in which the side chain SK is a radical of partial formula (II), where m equals 4, 5 or 6; n equals 0, 1 or 2; x equals 0, 1 or 2; A is a hydrogen atom or a C1-5-alkyl group; B and D represent each a hydrogen atom, or A and B represent together an alkylene group -(CH2)p- where p = 2, 3, 4 or 5 and D is a hydrogen atom, or A and D form together an alkylene group -(CH2)q- where q = 2, 3 or 4 and B is a hydrogen atom; and E is a non-substituted ethyl radical or an ethyl radical fluorinated one to five times; or the terminal substituent -(CH2)3-E in the side chain is substituted by an optionally substituted aryl or heteroaryl radical bonded to the sulphur atom directly or by a mono-, di- or trimethylene group; R3 is a hydrogen atom, a hydrocarbon radical with up to 8 carbon atoms or a radical of partial formula R3'-C(O)-, where R3' is a hydrogen atom or a hydrocarbon radical with up to 8 carbon atoms or a phenyl radical; R11 is a hydrogen atom, a halogen atom or a nitrooxy group -O-NO¿2?, R?14, R15α, R15β, R16α and R16β¿ represent each a hydrogen atom or R?14 and R15α¿ are an additional bond or a methylene bridge, or R15β is a methyl group and R15α is a hydrogen atom, R?15α and R15β¿ represent each a methyl group, or R?15β and R16β¿ form together a methylene bridge, or R?16α or R16β¿ are a halogen atom or R?16α and R16β¿ form together a methylidene group, and the remaining substitutents R?14, R15α, R15β, R16α and R16β¿ represent each a hydrogen atom, R17' at the α- or β-position is a hydrogen atom, a C¿1-5? alkyl, C2-5 alkenyl or C2-5 alkinyl group or a trifluoromethyl group; and R?17'¿ is a hydrogen atom or a radical of partial formula R17'''-C(O)-, where R17''' is a hydrogen atom or a hydrocarbon radical with up to 8 carbon atoms, or when R17' is at the α-position, R17' forms together with R14 an ethano bridge, provided that when A and B do not stand together for -(CH¿2?)p- or A and D stand together for -(CH2)q-, at least one of the substituents R?11, R14, R15α, R15β, R16α and R16b¿ be not a hydrogen atom. Also disclosed are the physiologically tolerable addition salts of these compounds with organic and inorganic acids. These new compounds have a very strong anti-estrogenic activity. Some of them are pure anti-estrogenes, others are anti-estrogenes with a partial estrogenic effect. Because of their spectrum of activity, these new compounds are most suitable for preparing medicaments for tumor therapy and hormone substitution therapy.

    NICHTSTEROIDALE (HETERO)ZYKLISCH-SUBSTITUIERTE ACYLANILIDE MIT GEMISCHTER GESTAGENER UND ANDROGENER WIRKSAMKEIT
    6.
    发明授权
    NICHTSTEROIDALE (HETERO)ZYKLISCH-SUBSTITUIERTE ACYLANILIDE MIT GEMISCHTER GESTAGENER UND ANDROGENER WIRKSAMKEIT 失效
    NICHTSTEROIDALE（HETERO）ZYKLISCH-SUBSTITUIERTE ACYLANILIDE MIT GEMISCHTER GERMAGENER UND ANDROGENER WIRKSAMKEIT

    公开(公告)号：EP0986545B1

    公开(公告)日：2004-12-29

    申请号：EP98928338.7

    申请日：1998-06-02

    申请人： SCHERING AKTIENGESELLSCHAFT

    发明人： LEHMANN, Manfred ,  SCHÖLLKOPF, Klaus ,  STREHLKE, Peter ,  HEINRICH, Nikolaus ,  FRITZEMEIER, Karl-Heinrich ,  MUHN, Hans-Peter ,  KRATTENMACHER, Rolf

    IPC分类号： C07D249/18 ,  A61K31/41 ,  C07D271/12 ,  C07D285/10 ,  C07C235/26 ,  A61K31/16 ,  C07D307/88 ,  A61K31/365 ,  C07D333/72 ,  A61K31/38 ,  C07D311/76 ,  C07D265/02 ,  A61K31/535 ,  C07D237/32 ,  A61K31/50

    CPC分类号： C07D285/10 ,  C07C225/22 ,  C07C235/38 ,  C07C235/84 ,  C07C255/57 ,  C07C2602/08 ,  C07D237/32 ,  C07D249/18 ,  C07D265/02 ,  C07D271/08 ,  C07D307/88 ,  C07D307/94 ,  C07D311/76 ,  C07D333/72 ,  C07D409/12

    摘要： The invention relates to non-steroidal gestagens of general formula (I), wherein R?1 and R2¿ are the same or different and stand for a hydrogen atom, a C¿1?-C5 alkyl group or a halogen atom, or together with the C atom of the chain stand for a ring with 3-7 units, R?3¿ means a C¿1?-C5 alkyl group or a partially or fully fluorinated C1-C5 alkyl group, A stands for an optionally substituted mono or bi-cyclic aromatic ring, an ester group -COOR?4¿, an alkenyl group -CR5=CR6R7, an alkinyl group -C CR5 or for a partially or fully fluorinated C¿1?-C5 alkyl group, B means a carbonyl group or a CH2 group and Ar is a ring system selected from the group of general partial formulae (2-11). When B represents a CH2 group in general formula (I), Ar additionally means a phenyl radical of partial general formula (12). The novel compounds display a very strong affinity to the gestagen receptor. They can be used on their own or in combination with oestrogen's in contraceptive preparations. They can also be used in the treatment of endometriosis. They can be used with oestrogen's in preparations for the treatment of gynaecological disorders. They can also be used to treat pre-menstrual complaints and in substitution therapy. Their androgen activity enables them to be used for male fertility control, male HRT and to treat andrological syndromes.

    摘要翻译： 本发明涉及通式（I）的非甾体孕激素，其中R 1和R 2相同或不同，代表氢原子，C1-C5烷基或卤素原子，或一起 链的C原子代表具有3-7个单元的环，R 3表示C 1 -C 5烷基或部分或全部氟化的C 1 -C 5烷基，A代表任选取代的单或双 - 环状芳环，酯基-COOR 4，烯基-CR 5 = CR 6 R 7，炔基-CCR 5或部分或全部氟化的C 1 -C 5烷基 基团，B表示羰基或CH2基团，Ar是选自通式（2-11）的环系。 当B表示通式（I）中的CH 2基时，Ar另外表示部分通式（12）的苯基。 新颖的化合物对孕激素受体表现出非常强的亲和力。 它们可以自己使用，也可以与雌激素在避孕药物中配合使用。 它们也可用于治疗子宫内膜异位症。 它们可用于治疗妇科疾病的制剂中的雌激素。 它们也可以用于治疗月经前的投诉和替代治疗。 他们的雄激素活性使他们能够用于男性生育控制，男性HRT和治疗组织学综合征。