公开(公告)号：EP1490391B1

公开(公告)日：2005-12-21

申请号：EP03717244.2

申请日：2003-03-27

Applicant: Schering Aktiengesellschaft

Inventor： MÜLLER, Gerd ,  HILLISCH, Alexander ,  HOFFMANN, Jens ,  FRITZEMEIER, Karl-Heinrich

IPC: C07J1/00 ,  A61K31/585 ,  A61P35/00

CPC classification number: C07J1/0081 ,  A61K31/585

Abstract: The invention relates to novel 19-nor-17 alpha -pregna-1,3,5(10)-trien-17 beta -ols with a 21,16 alpha lactone ring and a long chain substituent in the 11 beta position of general formula (II) where R is a 6 to 17 C straight chain alkyl group and R and R have the meanings more closely given in the description. The compounds have a tissue-selective pure anti-oestrogen effect and are thus suitable for the production of medicaments.

Abstract translation: 本发明涉及在通式11β位具有21,16α内酯环和长链取代基的新型19-去甲-17α-孕烷-1,3,5（10） - 三烯-17β-醇 （II）其中R 11是6至17C的直链烷基，且R 3和R 13具有在说明书中更加紧密给出的含义。 这些化合物具有组织选择性的纯抗雌激素作用，因此适用于生产药物。

公开(公告)号：EP1594886A1

公开(公告)日：2005-11-16

申请号：EP04712555.4

申请日：2004-02-19

Applicant: Schering Aktiengesellschaft

Inventor： HILLISCH, Alexander ,  PETERS, Olaf ,  GEGE, Christian ,  SIEMEISTER, Gerhard ,  UNGER, Eberhard ,  MENZENBACH, Bernd

IPC: C07J63/00 ,  A61P35/00

CPC classification number: C07J63/00

Abstract: The invention relates to D-homoestra-1, 3, 5 (10)-trien-3-yl 2-substituted sulfamates of general formula (I), wherein R3 is C1-C5 alkyl or a C1-C5 alkyloxy group and to the use thereof for producing a drug for curing tumoral diseases which can be positively influenced by inhibiting tubulin polymerisation. The inventive compounds are characterised by a D-homosubstitution, in a particular by the effect thereof for inhibiting the tubulin polymerisation and in that they can be used, for example for curing prostate carcinomas.

公开(公告)号：EP1517914B1

公开(公告)日：2005-08-31

申请号：EP03757065.2

申请日：2003-06-11

Applicant: Schering Aktiengesellschaft

Inventor： KOSEMUND, Dirk ,  MÜLLER, Gerd ,  HILLISCH, Alexander ,  FRITZEMEIER, Karl-Heinrich ,  MUHN, Peter

IPC: C07J1/00

CPC classification number: C07J1/0055 ,  C07J1/0066 ,  C07J41/0072 ,  C07J63/008

Abstract: The invention relates to novel 9 alpha -substituted estratrienes of general formula (I) - wherein R3, R7, R7', R13, R16, R17 and R17' have the designations cited in the description, and R9 represents a linear-chain or branched-chain, optionally partially or fully halogenated alkenyl radical comprising between 2 and 6 carbon atoms, or an ethinyl radical or a prop-1-inyl radical - as pharmaceutical active ingredients which have, in vitro, a higher affinity to estrogen receptor preparations of the rat prostate than to estrogen receptor preparation of the rat uterus, and, in vivo, preferably a preferential action on the ovary compared to the uterus. The invention also relates to the production of said estratrienes, to the therapeutic application thereof and to pharmaceutical forms of administration containing the novel compounds. The invention further relates to the use of said compounds for treating illnesses and states related to estrogen deficiency.

Abstract translation: 本发明涉及通式（I）的新型9α-取代的雌三烯 - 其中R 3，R 7，R 7'，R 13，R 16，R 17和R 17'具有说明书中引用的名称，并且R 9表示直链或支链 - 链，任选地包含2至6个碳原子的部分或完全卤代的烯基，或者乙炔基或丙-1-烯基 - 作为药物活性成分，其在体外对雌激素受体制剂具有较高的亲和力 大鼠前列腺而不是大鼠子宫的雌激素受体制备，并且在体内优选对子宫相对于子宫的优先作用。 本发明还涉及所述雌三烯的生产，其治疗应用以及含有所述新化合物的药物施用形式。 本发明还涉及所述化合物用于治疗与雌激素不足有关的疾病和状态的用途。

公开(公告)号：EP1272504A1

公开(公告)日：2003-01-08

申请号：EP01931609.0

申请日：2001-04-12

Applicant: Schering Aktiengesellschaft

Inventor： PETERS, Olaf ,  HILLISCH, Alexander ,  THIEME, Ina ,  ELGER, Walter ,  HEGELE-HARTUNG, Christa ,  KOLLENKIRCHEN, Uwe ,  FRITZEMEIER, Karl-Heinrich ,  PATCHEV, Vladimir

IPC: C07J1/00 ,  A61K31/565 ,  C07J41/00 ,  A61P5/30

CPC classification number: C07J1/007 ,  C07J1/0059 ,  C07J1/0062 ,  C07J1/0074 ,  C07J41/0072

Abstract: The invention relates to novel 8ß-substituted estratrienes of the general formula (I), wherein R?2, R3, R6, R6', R7, R7', R9, R11, R11', R12, R14, R15, R15', R16, R16', R17 and R17'¿ are defined as in the description and R8 represents a straight- or branched-chained, optionally partially or completely halogenated alkyl or alkenyl group with up to 5 carbon atoms, an ethinyl or prop-1-inyl group. The inventive estratrienes are used as pharmaceutically active substances that have in vitro a higher affinity to estrogen receptor preparations of rat prostate than to estrogen receptor preparations of rat uterus and which in vivo preferably have a preferential effect on bone material as compared to uterus and/or a pronounced effect with respect to the stimulation of the expression of 5HT2a receptor and transporter. The invention further relates to the production of these novel compounds, to their use in therapy and to the pharmaceutical forms of administration that contain said novel compounds. The invention further describes the use of said compounds for treating estrogen-deficiency related diseases and conditions and to the use of an 8ß-substituted estratriene structural part in the overall structures of compounds that are characterized by a dissociation in favor of their estrogen effect on the bone as compared to the uterus.

公开(公告)号：EP1517914A2

公开(公告)日：2005-03-30

申请号：EP03757065.2

申请日：2003-06-11

Applicant: Schering Aktiengesellschaft

Inventor： KOSEMUND, Dirk ,  MÜLLER, Gerd ,  HILLISCH, Alexander ,  FRITZEMEIER, Karl-Heinrich ,  MUHN, Peter

IPC: C07J1/00

CPC classification number: C07J1/0055 ,  C07J1/0066 ,  C07J41/0072 ,  C07J63/008

Abstract: The invention relates to novel 9 alpha -substituted estratrienes of general formula (I) - wherein R3, R7, R7', R13, R16, R17 and R17' have the designations cited in the description, and R9 represents a linear-chain or branched-chain, optionally partially or fully halogenated alkenyl radical comprising between 2 and 6 carbon atoms, or an ethinyl radical or a prop-1-inyl radical - as pharmaceutical active ingredients which have, in vitro, a higher affinity to estrogen receptor preparations of the rat prostate than to estrogen receptor preparation of the rat uterus, and, in vivo, preferably a preferential action on the ovary compared to the uterus. The invention also relates to the production of said estratrienes, to the therapeutic application thereof and to pharmaceutical forms of administration containing the novel compounds. The invention further relates to the use of said compounds for treating illnesses and states related to estrogen deficiency.

公开(公告)号：EP1490391A1

公开(公告)日：2004-12-29

申请号：EP03717244.2

申请日：2003-03-27

Applicant: Schering Aktiengesellschaft

Inventor： MÜLLER, Gerd ,  HILLISCH, Alexander ,  HOFFMANN, Jens ,  FRITZEMEIER, Karl-Heinrich

IPC: C07J1/00 ,  A61K31/585 ,  A61P35/00

CPC classification number: C07J1/0081 ,  A61K31/585

Abstract: The invention relates to novel 19-nor-17α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α lactone ring and a long chain substituent in the 11β position of general formula (II) where R11 is a 6 to 17 C straight chain alkyl group and R3 and R13 have the meanings more closely given in the description. The compounds have a tissue-selective pure anti-oestrogen effect and are thus suitable for the production of medicaments.

Abstract translation: 本发明涉及在通式（II）的11β位具有21,16α内酯环和长链取代基的新型19-降-17α-孕-1,3,5（10） - 三烯-17β-醇，其中 R11是6-17个碳原子的直链烷基，R3和R13具有在说明书中更为详细的含义。 这些化合物具有组织选择性的纯抗雌激素作用，因此适用于生产药物。

公开(公告)号：EP1272505A1

公开(公告)日：2003-01-08

申请号：EP01940331.0

申请日：2001-04-12

Applicant: Schering Aktiengesellschaft

Inventor： PETERS, Olaf ,  BRAEUER, Nico ,  HILLISCH, Alexander ,  HEGELE-HARTUNG, Christa ,  FRITZEMEIER, Karl-Heinrich

IPC: C07J1/00 ,  A61K31/565 ,  C07J41/00 ,  A61P5/30

CPC classification number: C07J1/007 ,  C07J1/0059 ,  C07J1/0062 ,  C07J1/0074 ,  C07J41/0072

Abstract: The present invention relates to the novel 8β-substituted estradienes of general formula (I), wherein R?2, R3, R6, R6", R7, R7", R14, R15, R15", R16, R16", R17 and R17"¿ have the meanings given in the description, R8 means a straight-chain or branched-chain, optionally partially or entirely halogenated alkyl or alkenyl radical having up to 5 carbon atoms, an ethynyl or prop-1-inyl radical and R11 means an n-pentyl- or n-hexyl radical. Said estradienes are used as pharmaceutical active agents which, in vitro, are provided with a higher affinity of estrogen receptor preparations of rat prostate than of estrogen receptor preparations of rat uterus and, in vivo, preferably act in a preferential contraceptive manner on the ovary without stimulating the uterus. The invention also relates to the production thereof, the therapeutic use thereof and pharmaceutical administration forms which contain the novel compounds. The invention further relates to the use of said compounds for male contraception and to the use of non-malignant or malignant proliferate diseases of the ovary, such as ovarian carcinoma or granulosa cell tumours for instance.

公开(公告)号：EP1747231A1

公开(公告)日：2007-01-31

申请号：EP05747926.3

申请日：2005-05-10

Applicant: Schering Aktiengesellschaft

Inventor： WYRWA, Ralf ,  DROESCHER, Peter ,  RING, Sven ,  ELGER, Walter ,  SCHNEIDER, Birgitt ,  HILLISCH, Alexander ,  REDDERSEN, Gudrun

IPC: C07J41/00 ,  A61K31/565 ,  A61P5/30

CPC classification number: C07J41/0072

Abstract: The invention relates to estriol and estetrol prodrugs of general formula (I), in which group Y is bonded to the steroid, the method for production thereof, pharmaceutical compositions comprising said compounds and the use thereof for production of medicaments with estrogenic effect.

公开(公告)号：EP1747230A1

公开(公告)日：2007-01-31

申请号：EP05747458.7

申请日：2005-05-10

Applicant: Schering Aktiengesellschaft

Inventor： WYRWA, Ralf ,  DROESCHER, Peter ,  RING, Sven ,  ELGER, Walter ,  SCHNEIDER, Birgitt ,  HILLISCH, Alexander ,  REDDERSEN, Gudrun

IPC: C07J41/00 ,  A61K31/565 ,  A61P5/30

CPC classification number: C07J41/0072

Abstract: The invention relates to estradiol prodrugs of general formula (I), in which the group Z is bonded to the steroid. The invention further relates to methods for production thereof, pharamceutical compositions comprising said compounds and use thereof for the production of medicaments with an estrogenic effect.

公开(公告)号：EP1525215B1

公开(公告)日：2006-09-06

申请号：EP03784154.1

申请日：2003-08-01

Applicant: Schering Aktiengesellschaft

Inventor： HILLISCH, Alexander ,  ELGER, Walter ,  SCHUBERT, Gerd ,  SCHNEIDER, Birgitt ,  REDDERSEN, Gudrun

IPC: C07J41/00 ,  A61K31/565 ,  A61P5/24

CPC classification number: C07J41/0083

Abstract: The invention relates to novel compounds of general formula (I), to the production thereof and to pharmaceutical preparations containing these compounds. The inventive compounds are preferably used in female fertility testing and hormone replacement therapy.