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1.再颁专利Antitumoral D-homoestra-1,3,5(10)-trien-3-yl 2-substituted sulfamates 失效抗肿瘤D-高丝氨酸-1,3,5（10） - 三烯-3-基2-取代的氨基磺酸盐公开(公告)号：USRE42132E1
公开(公告)日：2011-02-08
申请号：US12351271
申请日：2004-02-19
Applicant: Alexander Hillisch , Olaf Peters , Christian Gege , Gerhard Siemeister , Eberhard Unger , Bernd Menzenbach
Inventor： Alexander Hillisch , Olaf Peters , Christian Gege , Gerhard Siemeister , Eberhard Unger , Bernd Menzenbach
IPC: A61K31/565 , C07J31/00 , C07J41/00 , A61P35/00
CPC classification number: C07J63/00
Abstract: This invention relates to 2-substituted D-homo-estra-1,3,5(10)-trien-3-yl sulfamates of general formula I (I), in which R3 means a C1-C5-alkyl or C1-C5-alkyloxy group as well as their use for the production of a pharmaceutical agent for treating tumor diseases, which can be influenced positively by the inhibition of tubulin polymerization. The compounds according to the invention are distinguished by a D-homo-substitution. They have a special action with respect to tubulin polymerization inhibition and can be used, for example, for treating prostate cancer
Abstract translation: 本发明涉及通式I（I）的2-取代的D-均 - 雌-1,3,5（10） - 三烯-3-基氨基磺酸酯，其中R 3表示C 1 -C 5 - 烷基或C 1 -C 5 - 烷氧基以及它们用于生产用于治疗肿瘤疾病的药剂的用途，其可通过抑制微管蛋白聚合而受到积极的影响。 根据本发明的化合物通过D-均取代来区分。 它们在微管蛋白聚合抑制方面具有特殊的作用，可用于例如治疗前列腺癌
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公开(公告)号：US07449459B2
公开(公告)日：2008-11-11
申请号：US11727167
申请日：2007-03-23
Applicant: Bernd Buchmann , Dirk Kosemund , Bernd Menzenbach , Martin Fritsch
Inventor： Bernd Buchmann , Dirk Kosemund , Bernd Menzenbach , Martin Fritsch
IPC: A61K31/535 , A61K31/445 , A61K31/44 , A61K31/40 , C07D413/00 , C07D401/00 , C07D209/02 , C07D209/04
CPC classification number: C07D405/12 , C07D209/42
Abstract: The invention relates to compounds of general formula I as well as the production and use thereof as a medication.
Abstract translation: 本发明涉及通式I的化合物及其作为药物的生产和用途。
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3.发明授权17-Methylene steroids, process for their production and pharmaceutical compositions that contain these compounds 失效17-亚甲基类固醇，其制备方法和含有这些化合物的药物组合物公开(公告)号：US06855836B2
公开(公告)日：2005-02-15
申请号：US09963680
申请日：2001-09-27
Applicant: Bernd Menzenbach , Peter Droescher , Walter Elger , Alexander Hillisch , Gunter Kaufmann , Hans-Udo Schweikert , Gerd Muller
Inventor： Bernd Menzenbach , Peter Droescher , Walter Elger , Alexander Hillisch , Gunter Kaufmann , Hans-Udo Schweikert , Gerd Muller
CPC classification number: C07J13/00
Abstract: The invention relates to 17-methylene steroids, process for their production and pharmaceutical compositions that contain these compounds.The compounds according to the invention have a hybrid-type profile of action in the sense that they act as inhibitors of 5α-reductase and simultaneously as gestagens. They are therefore suitable for treating diseases that are the result of elevated androgen levels in certain organs and tissues in men and women. Together with other hormonal substances, such as an estrogen, testosterone or a strong androgen, the compounds according to the invention are suitable as contraceptive agents for women and for men.
Abstract translation: 本发明涉及17-亚甲基类固醇，其生产方法和含有这些化合物的药物组合物。根据本发明的化合物具有混合型的作用特征，其意义在于它们作为5α-还原酶的抑制剂，同时作为 gestagens。 因此，它们适用于治疗男性和女性某些器官和组织中雄激素水平升高的疾病。 与其他激素物质如雌激素，睾酮或强雄激素一起，本发明的化合物适合作为妇女和男性的避孕药。
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公开(公告)号：US20080004268A1
公开(公告)日：2008-01-03
申请号：US11835164
申请日：2007-08-07
Applicant: Duy NGUYEN , Anne MENGEL , Martin FRITSCH , Gernot LANGER , Ulf BOEMER , Knut EIS , Bernd MENZENBACH , Bernd BUCHMANN , Seock-Kyu KHIM
Inventor： Duy NGUYEN , Anne MENGEL , Martin FRITSCH , Gernot LANGER , Ulf BOEMER , Knut EIS , Bernd MENZENBACH , Bernd BUCHMANN , Seock-Kyu KHIM
IPC: A61K31/5377 , A61K31/454 , A61K31/405 , C07D413/02 , C07D405/02 , C07D403/02
CPC classification number: C07D209/40 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D411/12 , C07D413/12 , C07D413/14
Abstract: The invention relates to compounds of general formula I as well as their production and use as a medication.
Abstract translation: 本发明涉及通式I的化合物及其作为药物的生产和用途。
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公开(公告)号：US20070259872A1
公开(公告)日：2007-11-08
申请号：US11727163
申请日：2007-03-23
Applicant: Bernd Buchmann , Dirk Kosemund , Bernd Menzenbach , Martin Fritsch
Inventor： Bernd Buchmann , Dirk Kosemund , Bernd Menzenbach , Martin Fritsch
IPC: A61K31/404 , A61K31/5377 , A61P15/16 , A61P15/18 , A61P3/00 , C07D209/30 , C07D413/02
CPC classification number: C07D405/12 , C07D209/04 , C07D209/42
Abstract: The invention relates to compounds of general formula I as well as the production and use thereof as a medication.
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Patent Agency Ranking
公开(公告)号：US5407928A
公开(公告)日：1995-04-18
申请号：US153558
申请日：1993-11-17
Applicant: Helmut Kasch , Gudrun Bertram , Kurt Ponsold , Gerd Schubert , Heidemarie Rohrig , Anatoli Kurischko , Bernd Menzenbach
Inventor： Helmut Kasch , Gudrun Bertram , Kurt Ponsold , Gerd Schubert , Heidemarie Rohrig , Anatoli Kurischko , Bernd Menzenbach
CPC classification number: C07J53/002 , C07J1/0085 , C07J1/0096 , C07J21/006 , C07J41/0083 , C07J71/001
Abstract: This invention relates to 11.beta.-aryl-gona-4,9-dienes of the general formula I ##STR1## wherein the variables are defined in the specification. The compounds are progesterone antagonists and are suitable for inducing labor or an abortion.
Abstract translation: 本发明涉及通式I的11α-芳基 - 腙-4,9-二烯，其中变量在说明书中定义。 这些化合物是孕酮拮抗剂，适用于诱导劳动或流产。
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公开(公告)号：US20080255117A1
公开(公告)日：2008-10-16
申请号：US12040369
申请日：2008-02-29
Applicant: Lars WORTMANN , Bernd Menzenbach , Marcus Koppitz , Dirk Kosemund , Hans Peter Muhn , Anna Schrey , Ronald Kuehne , Thomas Frenzel , Florian Peter Liesener
Inventor： Lars WORTMANN , Bernd Menzenbach , Marcus Koppitz , Dirk Kosemund , Hans Peter Muhn , Anna Schrey , Ronald Kuehne , Thomas Frenzel , Florian Peter Liesener
IPC: A61K31/4035 , C07D209/14 , A61K31/5377 , C07D413/02 , C07D403/12 , A61K31/454 , A61K31/4155 , C07D405/12 , A61K31/4709 , C07D215/36
CPC classification number: A61K31/4035 , A61K31/4155 , A61K31/454 , A61K31/4709 , A61K31/5377 , C07D209/14 , C07D215/36 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12
Abstract: The present invention relates to sulfonyltryptophanols of the general formula I, in which Q, X, W, R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as defined in the description.The compounds according to the invention are effective FSH receptor antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
Abstract translation: 本发明涉及通式I的磺酰基色氨酸，其中Q，X，W，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8具有说明书中定义的含义。 根据本发明的化合物是有效的FSH受体拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。
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8.发明授权17α-fluorosteroids, pharmaceutical compositions containing 17α-fluorosteroids and a method of making them 失效17α-含氟类固醇，含有17α-荧光素的药物组合物及其制备方法公开(公告)号：US07199115B2
公开(公告)日：2007-04-03
申请号：US11104736
申请日：2005-04-13
Applicant: Ulrich Bothe , Peter Droescher , Walter Elger , Gudrun Reddersen , Bernd Menzenbach , Hans-Udo Schweikert , Alexander Hillisch , Birgitt Schneider
Inventor： Ulrich Bothe , Peter Droescher , Walter Elger , Gudrun Reddersen , Bernd Menzenbach , Hans-Udo Schweikert , Alexander Hillisch , Birgitt Schneider
CPC classification number: C07J3/00
Abstract: New 17α-fluorosteroid compounds of formula (I) are disclosed: wherein R1 denotes H or methyl; R2 and R3 each denote H, Cl or methyl; and either a double bond or a single bond is present between C-6 and C-7 and also C-9 and C-10 of the steroid ring system respectively. These compounds have an activity profile with hybrid character so that they act as inhibitors for 5α-reductase and as high potency gestagens. Pharmaceutical compositions containing them are disclosed. They are suitable for treatment of conditions, which are caused by high levels of androgen in organs and tissues. These new compounds can be used in combination with other hormonal substances, such as estrogens, testosterone and other androgens, as contraceptives and for other applications.
Abstract translation: 公开了式（I）的新的17α-荧光素类化合物：
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9.发明申请Antitumoral d-homoestra-1,3,5 (10)-trien-3-yl 2-substituted sulfamates 有权抗肿瘤D-同型异构-1,3,5（10） - 三烯-3-基2-取代的亚磺酸盐公开(公告)号：US20060154985A1
公开(公告)日：2006-07-13
申请号：US10546230
申请日：2004-02-19
Applicant: Alexander Hillisch , Olaf Peters , Christian Gege , Gerhard Siemeister , Ebehard Unger , Bernd Menzenbach
Inventor： Alexander Hillisch , Olaf Peters , Christian Gege , Gerhard Siemeister , Ebehard Unger , Bernd Menzenbach
IPC: A61K31/255
CPC classification number: C07J63/00
Abstract: This invention relates to 2-substituted D-homo-estra-1,3,5(10)-trien-3-yl sulfamates of general formula I (I), in which R3 means a C1-C5-alkyl or C1-C5-alkyloxy group as well as their use for the production of a pharmaceutical agent for treating tumor diseases, which can be influenced positively by the inhibition of tubulin polymerization. The compounds according to the invention are distinguished by a D-homosubstitution. They have a special action with respect to tubulin polymerization inhibition and can be used, for example, for treating prostate cancer.
Abstract translation: 本发明涉及通式I（I）的2-取代的D-均 - 雌-1,3,5（10） - 三烯-3-基氨基磺酸酯，其中R 3表示C 1 -C 5 - 烷基或C 1 -C 5 - 烷氧基以及它们用于生产用于治疗肿瘤疾病的药剂的用途，其可通过抑制微管蛋白聚合而受到积极的影响。 根据本发明的化合物通过D-均质化来区分。 它们在微管蛋白聚合抑制方面具有特殊的作用，可用于例如治疗前列腺癌。
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10.发明授权Steroids with radical-attracting aromatic substituents, process for the production thereof and pharmaceutical compounds containing the said substances 失效具有自由基吸引芳族取代基的类固醇，其制备方法和含有所述物质的药物化合物
公开(公告)号：US5977096A
公开(公告)日：1999-11-02
申请号：US253650
申请日：1999-02-20
Applicant: Peter Droescher , Bernd Menzenbach , Kurt Ponsold , Bernd Undeutsch , Michael Oettel , Wolfgang Romer , Gunter Kaufmann , Jens Schroder
Inventor： Peter Droescher , Bernd Menzenbach , Kurt Ponsold , Bernd Undeutsch , Michael Oettel , Wolfgang Romer , Gunter Kaufmann , Jens Schroder
CPC classification number: C07J1/007 , C07J1/0022 , C07J1/0088 , C07J31/006 , C07J41/0044 , C07J41/0072 , C07J51/00
Abstract: Novel substituted steroid compounds are disclosed which are more effective than known radical-trapping agents in methods of prophylaxis and therapy of radical-mediated cell damage and of treatment of diseases due to radical-mediated cell damage. The novel substituted steroid compounds can be made from steroids having an estrane, androstane, pregnane or cholestane basic skeleton and have a radical-attracting aromatic substituent of the general formula --(CH.sub.2).sub.n X, or .dbd.CH--(CH.sub.2).sub.m X at the 17 or 6 position of the steroid nucleus, wherein X=Y, OY, SY, SeY or NHY; n=0 to 5; m=n-1 and Y is a phenyl group having five substituents A, B, C, D and E, wherein A to E is independently H, alkyl, Oalkyl, Oacyl, OH, or one of the substituents B, C or D is NR.sub.2 wherein R=alkyl and each of the other substituents is hydrogen. Pharmaceutical compositions containing the novel substituted steroid compounds and methods of making them are also part of the invention.
Abstract translation: 公开了新型取代的类固醇化合物，其在预防和治疗自由基介导的细胞损伤和由于自由基介导的细胞损伤引起的疾病的治疗的方法中比已知的自由基捕获剂更有效。 新型取代的类固醇化合物可以由具有雌激素，雄甾烷，孕烷或胆甾烷碱性骨架的类固醇制成，并且在17位具有通式 - （CH 2）n X或= CH-（CH 2）m X的自由基吸引芳族取代基 或6位，其中X = Y，OY，SY，SeY或NHY; n = 0〜5; m = n-1，Y是具有5个取代基A，B，C，D和E的苯基，其中A至E独立地为H，烷基，O烷基，Oacyl，OH或取代基B，C或D中的一个 是NR 2，其中R =烷基，并且每个其它取代基是氢。 含有新型取代的类固醇化合物的药物组合物及其制备方法也是本发明的一部分。
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