公开(公告)号：US07186728B2

公开(公告)日：2007-03-06

申请号：US10487862

申请日：2002-08-28

申请人： Bernd Menzenbach ,  Peter Droescher ,  Alexander Hillisch ,  Walter Elger ,  Hans-Udo Schweikert ,  Klaus Schoellkopf

发明人： Bernd Menzenbach ,  Peter Droescher ,  Alexander Hillisch ,  Walter Elger ,  Hans-Udo Schweikert ,  Klaus Schoellkopf

IPC分类号： A61K31/473 ,  C07D221/18

CPC分类号： C07J73/005

摘要： 17-methylene-4-azasteroid compounds of formula I: wherein R20 denotes fluoro, chloro or bromo R20a denotes hydrogen, R10 and R4 each denote a hydrogen atom or a methyl group, and R1 and R2 each denote a hydrogen atom or together denote an additional bond, are useful for treating diseases or conditions caused by excessive androgen levels, such as acne, prostate diseases, alopecia and hirsutism, as well as gynecological conditions. Methods of synthesizing the new 17-methylene-4-azasteroid compounds are described.

摘要翻译： 式I的17-亚甲基-4-氮杂甾族化合物：其中R 20表示氟，氯或溴R 20a表示氢，R 10和 R 4各自表示氢原子或甲基，R 1和R 2各自表示氢原子或一起表示附加键 可用于治疗由过度雄激素水平引起的疾病或病症，如痤疮，前列腺疾病，脱发和多毛症以及妇科病症。 描述了合成新的17-亚甲基-4-氮杂甾族化合物的方法。

公开(公告)号：US20050282793A1

公开(公告)日：2005-12-22

申请号：US11134617

申请日：2005-05-23

申请人： Ralf Wyrwa ,  Sven Ring ,  Peter Droescher ,  Alexander Hillisch ,  Walter Elger ,  Birgitt Schneider ,  Gudrun Reddersen

发明人： Ralf Wyrwa ,  Sven Ring ,  Peter Droescher ,  Alexander Hillisch ,  Walter Elger ,  Birgitt Schneider ,  Gudrun Reddersen

IPC分类号： A61K31/56 ,  C07J1/00

CPC分类号： C07J1/00

摘要： This invention relates to steroid prodrugs with androgenic action of general formula (I), in which group Z is bonded to the steroid, pharmaceutical compositions that contain these compounds as well as their use for the production of pharmaceutical agents with androgenic action.

摘要翻译： 本发明涉及具有通式（I）的雄激素作用的类固醇前药，其中Z基团与类固醇结合，含有这些化合物的药物组合物及其用于制备具有雄激素作用的药剂的用途。

公开(公告)号：US06777409B2

公开(公告)日：2004-08-17

申请号：US09916195

申请日：2001-07-27

申请人： Stefan Jaroch ,  Manfred Lehmann ,  Norbert Schmees ,  Bernd Buchmann ,  Harmur Rehwinkel ,  Peter Droescher ,  Werner Skuballa ,  Konrad Krolikiewicz ,  Hartwig Hennekes ,  Heike Schaecke ,  Arndt Schottelius

发明人： Stefan Jaroch ,  Manfred Lehmann ,  Norbert Schmees ,  Bernd Buchmann ,  Harmur Rehwinkel ,  Peter Droescher ,  Werner Skuballa ,  Konrad Krolikiewicz ,  Hartwig Hennekes ,  Heike Schaecke ,  Arndt Schottelius

IPC分类号： A61K31536

CPC分类号： C07D413/12 ,  A61K31/365 ,  A61K31/536 ,  C07D265/02 ,  C07D307/88

摘要： The compound of formula 1 useful in the treatment of inflammation.

摘要翻译： 式1化合物用于治疗炎症。

公开(公告)号：US06517078B2

公开(公告)日：2003-02-11

申请号：US09990266

申请日：2001-11-23

申请人： Andreas Schruefer ,  Werner Wolf ,  Guenther Lederer ,  Peter Droescher ,  Josef Nosowicz ,  Georg Steigenberger

发明人： Andreas Schruefer ,  Werner Wolf ,  Guenther Lederer ,  Peter Droescher ,  Josef Nosowicz ,  Georg Steigenberger

IPC分类号： F16J1516

CPC分类号： F16J15/3468 ,  F16J15/3472

摘要： A face seal device for use with components rotating at a high rotational speed includes a non-rotating face seal ring (5) and a rotary face seal ring (11). The rotary face seal ring is mounted in a loose fit for common rotation with a rotating component and includes a sealing face (6) which, in operation, is essentially radially aligned for cooperation with an opposite sealing face (16) of the non-rotating face seal ring. A heavy-mass-contributing element (22) is arranged to rotate in common with the rotating component and engages a portion of the rotary face seal ring. The center of gravity of the heavy-mass-contributing element is axially spaced from that of the rotary face seal ring, whereby, in operation, a torque directed towards the non-rotating face seal ring is applied to the rotary face seal ring. This torque arises from the centrifugal forces that correspond to the mass-contributing element and the spacing between the centers of gravity.

公开(公告)号：US07129270B2

公开(公告)日：2006-10-31

申请号：US11253690

申请日：2005-10-20

申请人： Stefan JaRoch ,  Manfred Lehmann ,  Norbert Schmees ,  Bernd Buchmann ,  Harmur Rehwinkel ,  Peter Droescher ,  Werner Skuballa ,  Konrad Krolikiewicz ,  Hartwig Hennekes ,  Heike Schaecke ,  Arndr Schottelius

发明人： Stefan JaRoch ,  Manfred Lehmann ,  Norbert Schmees ,  Bernd Buchmann ,  Harmur Rehwinkel ,  Peter Droescher ,  Werner Skuballa ,  Konrad Krolikiewicz ,  Hartwig Hennekes ,  Heike Schaecke ,  Arndr Schottelius

IPC分类号： C07D307/85 ,  A61K31/343

CPC分类号： C07D413/12 ,  A61K31/365 ,  A61K31/536 ,  C07D265/02 ,  C07D307/88

摘要： Compounds of Formula 1 are useful in the treatment of inflammation.

摘要翻译： 式1的化合物可用于治疗炎症。

公开(公告)号：US20090099250A1

公开(公告)日：2009-04-16

申请号：US12249056

申请日：2008-10-10

申请人： Ralf WYRWA ,  Olaf Peters ,  Rolf Bohlmann ,  Peter Droescher ,  Katja Prelle ,  Karl Heinrich Fritzemeier ,  Hans Peter Muhn

发明人： Ralf WYRWA ,  Olaf Peters ,  Rolf Bohlmann ,  Peter Droescher ,  Katja Prelle ,  Karl Heinrich Fritzemeier ,  Hans Peter Muhn

IPC分类号： A61K31/381 ,  C07C39/17 ,  A61K31/122 ,  A61K31/05 ,  A61P5/00 ,  C07C49/747 ,  C07D333/16

CPC分类号： C07C39/23 ,  C07C39/17 ,  C07C43/23 ,  C07D333/16

摘要： The present invention describes non-steroidal compounds of the general formula (I) in which A is in which X1 means one or more groups on the phenyl ring and represents independently of one another a halogen, OH, (C1-C4)alkyl, (C1-C4)alkyl-O, (C3-C6)cycloalkyl-O, (C1-C14)acyl-O, (C1-C4)alkenyl, (C1-C4)alkynyl, perfluoro(C1-C4)alkyl radical, —CHO or CN, and X2 means one or more groups on the phenyl ring and represents independently of one another an H, halogen, OH, (C1-C4)alkyl, (C1-C4)alkyl-O, (C1-C4)alkenyl, (C1-C4)alkynyl, perfluoro-(C1-C4)alkyl radical, —CHO or CN, as Estrogens.

摘要翻译： 本发明描述了通式（I）的非甾体化合物，其中A是其中X 1表示苯基上的一个或多个基团并且彼此独立地表示卤素，OH，（C 1 -C 4）烷基，（ C1-C4）烷基-O，（C3-C6）环烷基-O，（C1-C14）酰基-O，（C1-C4）烯基，（C1-C4）炔基，全氟（C1-C4）烷基， CHO或CN，X2表示苯基上的一个或多个基团，并且彼此独立地表示H，卤素，OH，（C1-C4）烷基，（C1-C4）烷基-O，（C1-C4）烯基 ，（C 1 -C 4）炔基，全氟 - （C 1 -C 4）烷基，-CHO或CN作为雌激素。

公开(公告)号：US07378522B2

公开(公告)日：2008-05-27

申请号：US10896961

申请日：2004-07-23

申请人： Peter Strehlke ,  Peter Droescher ,  Ulrich Buehmann ,  Norbert Schmees ,  Peter Muhn ,  Holger Hess-Stumpp ,  Roland Kühne ,  Eckhard Guenther ,  Emmanuel Polymeropoulos ,  Antonius M. Ter Laak

发明人： Peter Strehlke ,  Peter Droescher ,  Ulrich Buehmann ,  Norbert Schmees ,  Peter Muhn ,  Holger Hess-Stumpp ,  Roland Kühne ,  Eckhard Guenther ,  Emmanuel Polymeropoulos ,  Antonius M. Ter Laak

IPC分类号： C07D239/72

CPC分类号： C07D401/04 ,  A61K31/47 ,  C07D215/56 ,  C07D237/32 ,  C07D401/12 ,  C07D409/04

摘要： The invention relates to new quinoline, isoquinoline and phthalazine derivatives as antagonists of the gonadotropin-releasing hormone.

摘要翻译： 本发明涉及作为促性腺激素释放激素拮抗剂的新喹啉，异喹啉和酞嗪衍生物。

公开(公告)号：US07199115B2

公开(公告)日：2007-04-03

申请号：US11104736

申请日：2005-04-13

申请人： Ulrich Bothe ,  Peter Droescher ,  Walter Elger ,  Gudrun Reddersen ,  Bernd Menzenbach ,  Hans-Udo Schweikert ,  Alexander Hillisch ,  Birgitt Schneider

发明人： Ulrich Bothe ,  Peter Droescher ,  Walter Elger ,  Gudrun Reddersen ,  Bernd Menzenbach ,  Hans-Udo Schweikert ,  Alexander Hillisch ,  Birgitt Schneider

IPC分类号： A61K31/56 ,  C07J3/00

CPC分类号： C07J3/00

摘要： 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.

摘要翻译： 公开了式（I）的新的17α-荧光素类化合物：

公开(公告)号：US20050277625A1

公开(公告)日：2005-12-15

申请号：US11134618

申请日：2005-05-23

申请人： Ralf Wyrwa ,  Sven Ring ,  Peter Droescher ,  Alexander Hillisch ,  Walter Elger ,  Birgitt Schneider ,  Gudrun Reddersen

发明人： Ralf Wyrwa ,  Sven Ring ,  Peter Droescher ,  Alexander Hillisch ,  Walter Elger ,  Birgitt Schneider ,  Gudrun Reddersen

IPC分类号： A61K31/56 ,  C07J1/00

CPC分类号： C07J1/00

摘要： This invention provides estriol and estetrol prodrugs of general formula (I), in which group Y is bonded to the steroid process for their production, pharmaceutical compositions that contain these compounds, as well as their use for the production of pharmaceutical agents with estrogenic action.

摘要翻译： 本发明提供了通式（I）的雌三醇和雌酮前体药物，其中Y基团与类固醇过程结合用于其生产，含有这些化合物的药物组合物以及其用于生产具有雌激素作用的药剂的用途。

公开(公告)号：US5977096A

公开(公告)日：1999-11-02

申请号：US253650

申请日：1999-02-20

申请人： Peter Droescher ,  Bernd Menzenbach ,  Kurt Ponsold ,  Bernd Undeutsch ,  Michael Oettel ,  Wolfgang Romer ,  Gunter Kaufmann ,  Jens Schroder

发明人： Peter Droescher ,  Bernd Menzenbach ,  Kurt Ponsold ,  Bernd Undeutsch ,  Michael Oettel ,  Wolfgang Romer ,  Gunter Kaufmann ,  Jens Schroder

IPC分类号： A61K31/56 ,  A61P29/00 ,  C07J1/00 ,  C07J31/00 ,  C07J41/00 ,  C07J51/00 ,  C07J3/00 ,  C07J53/00

CPC分类号： C07J1/007 ,  C07J1/0022 ,  C07J1/0088 ,  C07J31/006 ,  C07J41/0044 ,  C07J41/0072 ,  C07J51/00

摘要： 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.

摘要翻译： 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。