公开(公告)号：US20030191099A1

公开(公告)日：2003-10-09

申请号：US10305418

申请日：2002-11-27

Applicant: Schering AG

Inventor： Rolf Bohlmann ,  Nikolaus Heinrich ,  Rolf Jautelat ,  Jorg Kroll ,  Orlin Petrov ,  Andreas Reichel ,  Jens Hoffmann ,  Rosemarie Lichtner

IPC: A61K031/58 ,  A61K031/56 ,  C07J001/00

CPC classification number: C07J43/003 ,  C07J41/0072

Abstract: The invention relates to 17null-alkyl-17null-oxy-estra-1,3,5(10)-trienes that have an antiestrogenic action with general formula I. In addition, the invention also relates to 17-oxo-estra-1,3,5(10)-trienes as well as 17null-hydroxy-estra-1,3,5(10)-trienes as intermediate products in the production of the estratrienes according to the invention. The invention also relates to the use of 17null-alkyl-17null-oxy-estratrienes for the production of pharmaceutical agents as well as pharmaceutical preparations that contain at least one 17null-alkyl-17null-oxy-estratriene as well as at least one pharmaceutically compatible vehicle.

公开(公告)号：US20030166622A1

公开(公告)日：2003-09-04

申请号：US10292908

申请日：2002-11-13

Applicant: Schering AG

Inventor： Andreas Steinmeyer ,  Ulrich Zuegel

IPC: A61K031/59 ,  C07D233/54 ,  C07D213/46 ,  C07C401/00

CPC classification number: C07C401/00 ,  A61K31/59 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/24

Abstract: The invention relates to vitamin D derivatives of general formula I, 1 process for production, and the use for the production of pharmaceutical agents.

Abstract translation: 本发明涉及通式Ⅰ的维生素D衍生物，生产方法和制药用途。

公开(公告)号：US20030130249A1

公开(公告)日：2003-07-10

申请号：US10272290

申请日：2002-10-17

Applicant: Schering AG

Inventor： Walter Elger ,  Gudrun Reddersen ,  Birgitt Schneider ,  Alexander Hillisch ,  Olaf Peters ,  Dirk Kosemund ,  Gerd Muller

IPC: A61K031/56

CPC classification number: A61K31/00 ,  A61K31/56 ,  A61K31/565

Abstract: This invention describes the use of estrogen receptor (ER)null-selective agonists for the production of a pharmaceutical agent for triggering somatotropic and/or organotropic effects in the CNS, the circulatory system, the skeletal system and/or the immune system in the aging male and female organism (anticatabolic therapy).

Abstract translation: 本发明描述了雌激素受体（ER）β-选择性激动剂在生产用于在CNS，循环系统，骨骼系统和/或免疫系统中的生长激素和/或有机效应的老化中的用途 男性和女性生物体（抗分解治疗）。

公开(公告)号：US20030108486A1

公开(公告)日：2003-06-12

申请号：US10198046

申请日：2002-07-19

Applicant: Schering AG

Inventor： Johannes Platzek ,  Heribert Schmitt-Willich ,  Gunther Michl ,  Thomas Frenzel ,  Detlev Sulzle ,  Hans Bauer ,  Bernd Raduchel ,  Hanns-Joachim Weinmann ,  Heiko Schirmer

IPC: A61K049/00 ,  C07F005/00 ,  C07D257/02

CPC classification number: A61K49/10 ,  A61K47/54 ,  A61K47/547 ,  A61K49/0002 ,  A61K49/085 ,  A61K49/14 ,  A61K49/143 ,  C07D257/02

Abstract: The invention relates to macrocyclic metal complexes and their production and use for the production of conjugates with biomolecules. The conjugates are suitable as contrast media in NMR diagnosis and radiodiagnosis as well as for radiotherapy. High relaxivity is achieved by a special liganding of macrocyclic compounds, and a fine-tuning of the relaxivity is made possible.

Abstract translation: 本发明涉及大环金属络合物及其生产和用于与生物分子生产缀合物的用途。 缀合物适用于NMR诊断和放射诊断以及放射治疗中的造影剂。 通过大环化合物的特殊结合实现高的放松性，并且可以进行微调的松弛度。

公开(公告)号：US20030087913A1

公开(公告)日：2003-05-08

申请号：US10273368

申请日：2002-10-18

Applicant: Schering AG

Inventor： Heiko Kranz ,  Christoph Volkel ,  Ralph Lipp ,  Johannes Tack ,  Herbert Wiesinger

IPC: A61K009/14 ,  A61K031/495

CPC classification number: A61K31/495 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054

Abstract: A solid pharmaceutical agent formulation that contains (2R)-1-((4-chloro-2-(ureido)phenoxy)methyl)carbonyl-2-methyl-4-(4-fluorobenzyl)piperazine or a salt thereof is described.

Abstract translation: 描述了含有（2R）-1 - （（4-氯-2-（脲基）苯氧基）甲基）羰基-2-甲基-4-（4-氟苄基）哌嗪或其盐的固体药剂制剂。

公开(公告)号：US20030050324A1

公开(公告)日：2003-03-13

申请号：US10238640

申请日：2002-09-11

Applicant: Schering AG

Inventor： Rolf Bohlmann ,  Jorg Kroll ,  Hermann Kuenzer ,  Christa Hegele-Hartung ,  Monika Lessl ,  Rosemarie Lichtner ,  Yukishige Nishino

IPC: A61K031/445 ,  A61K031/137 ,  A61K031/235

CPC classification number: C07D307/38 ,  C07C217/20 ,  C07C317/18 ,  C07C317/28 ,  C07C317/44 ,  C07C323/12 ,  C07C323/25 ,  C07C323/60 ,  C07C327/28 ,  C07C2602/12 ,  C07D213/32 ,  C07D213/34 ,  C07D333/18

Abstract: This invention describes the new benzocycloheptenes of general formula I 1 in which R1, R2 and SK have the meanings that are indicated in the description. The new compounds have selective estrogenic activity on bones and are suitable for the production of pharmaceutical agents, especially for prophylaxis and therapy of osteoporosis.

Abstract translation: 本发明描述了通式I的新的苯并环庚烯，其中R1，R2和SK具有说明书中所示的含义。 新化合物对骨骼具有选择性雌激素活性，适用于生产药剂，特别是预防和治疗骨质疏松症。

公开(公告)号：US20020076379A1

公开(公告)日：2002-06-20

申请号：US09925622

申请日：2001-08-10

Applicant: Schering AG

Inventor： Johannes Platzek ,  Peter Mareski ,  Ulrich Niedballa ,  Bernd Raduechel ,  Hanns-Joachim Weinmann ,  Bernd Misselwitz

IPC: A61K049/10 ,  C07H017/02 ,  C07H015/00 ,  C07H017/00 ,  C07H023/00

CPC classification number: C07H13/10 ,  C07H15/04 ,  C07H15/26

Abstract: Perfluoroalkyl-containing complexes with sugar radicals of general formula I 1 in which R represents a monosaccharide or oligosaccharide radical that is bonded via the 1-OH position or 1-SH position, Rf means a perfluorinated carbon chain, K is a metal complex, and Y and Z represent linker groups, are suitable for intravenous lymphography, for tumor diagnosis and for infarction and necrosis imaging.

Abstract translation: 含有通式I的糖基的全氟烷基配合物，其中R表示通过1-OH位置或1-SH位置键合的单糖或寡糖基团，Rf表示全氟化碳链，K为金属络合物，Y为 和Z代表连接基团，适用于静脉内淋巴造影，肿瘤诊断和梗死和坏死成像。

公开(公告)号：US20020052475A1

公开(公告)日：2002-05-02

申请号：US09908494

申请日：2001-07-19

Applicant: Schering AG

Inventor： Stewart Leung ,  H. Daniel Perez ,  Neil Miyamoto

IPC: C07K014/705 ,  C07H021/04 ,  C12P021/04 ,  C12N005/06

CPC classification number: C07K14/7155 ,  A61K38/00 ,  C07K2319/00

Abstract: A soluble, heterodimeric interleukin 18 (IL-18) receptor molecule is described which comprises two subunits, one of which comprises an extracelluar domain, or a fragment thereof, of IL-18R, and the other of which comprises an extracelluar domain, or a fragment thereof, of AcPL. Preferably, the soluble, heterodimeric receptor binds to IL-18 with higher affinity than does either IL-18R or AcPL alone.

Abstract translation: 描述了可溶性的异二聚体白细胞介素18（IL-18）受体分子，其包含两个亚基，其中之一包含IL-18R的细胞外结构域或其片段，另一个包含胞外结构域，或 片段， 优选地，可溶性异二聚体受体以比单独的IL-18R或AcPL更高的亲和力结合IL-18。

公开(公告)号：US5986115A

公开(公告)日：1999-11-16

申请号：US239490

申请日：1999-01-28

Applicant: Rolf Bohlmann ,  Dieter Bittler ,  Josef Heindl ,  Nikolaus Heinrich ,  Helmut Hofmeister ,  Hermann Kunzer ,  Gerhard Sauer ,  Christa Hegele-Hartung ,  Rosemarie Lichtner ,  Yukishige Nishino ,  Karsten Parczyk ,  Martin Schneider

Inventor： Rolf Bohlmann ,  Dieter Bittler ,  Josef Heindl ,  Nikolaus Heinrich ,  Helmut Hofmeister ,  Hermann Kunzer ,  Gerhard Sauer ,  Christa Hegele-Hartung ,  Rosemarie Lichtner ,  Yukishige Nishino ,  Karsten Parczyk ,  Martin Schneider

IPC: C07J41/00 ,  C07J43/00 ,  C07J53/00 ,  C07D315/00 ,  C07J1/00 ,  C07J13/00 ,  C07J31/00

CPC classification number: C07J53/002 ,  C07J41/0072 ,  C07J43/006 ,  C07J53/008

Abstract: This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.

Abstract translation: 本发明描述了通式I的新的取代的7α-（xi-氨基烷基） - 三亚甲基，其中侧链SK是部分式的基团，以及它们与有机和无机酸的生理上相容的加成盐。 新化合物代表具有非常强的抗雌激素作用的化合物。 根据本发明的化合物一方面是纯抗雌激素，或者另一方面是具有雌激素部分作用的抗雌激素。 基于这一作用范围，新化合物非常适合用于肿瘤治疗和激素替代治疗药物的生产。

公开(公告)号：US5980940A

公开(公告)日：1999-11-09

申请号：US930630

申请日：1998-01-27

Applicant: Jurgen Spona ,  Bernd Dusterberg

Inventor： Jurgen Spona ,  Bernd Dusterberg

IPC: A61K31/565 ,  A61K31/57 ,  A61K31/585 ,  A61P15/08 ,  A61K31/56

CPC classification number: A61K31/57 ,  A61K31/565 ,  A61K31/585 ,  Y10S514/843

Abstract: The invention provides a pharmaceutical combination preparation with two hormone components in a packaging unit and intended for time-sequential oral administration, comprising a number of daily dosage units physically separate and individually removable in the packaging unit, whereby as a hormonal active ingredient a first hormone component contains in combination an estrogen preparation and in at least a dosage that is sufficient to inhibit ovulation a gestagen preparation, and as a hormonal active ingredient the second hormone component contains only an estrogen preparation, whereby the first hormone component comprises 23 or 24 daily units and the second hormone component comprises 4, 3 or 2 daily units, and between these two hormone components, 2 or 1 active ingredient-free daily units are present or 2 or 1 blank pill days are indicated, and the total number of hormone daily units and the active ingredient-free daily units or the blank pill days is equal to the total number of days of the desired cycle, but at least 28 days in length. This combination preparation is useful for female birth control, and allows for an estrogen content that is as low as possible in each individual dosage unit and also has a low total hormone content per administration cycle, with high contraceptive reliability, low incidence of follicular development, and satisfactory cycle control, with reliable avoidance of intracyclic menstrual bleeding as well as of undesirable side-effects.

Abstract translation: PCT No.PCT / EP96 / 01529 Sec。 371日期：1998年1月27日 102（e）日期1998年1月27日PCT提交1996年4月4日PCT公布。 出版物WO96 / 32114 日期：1996年10月17日本发明提供了包装单元中具有两种激素组分的药物组合制剂，其用于时间顺序的口服给药，其包括在包装单元中物理分离并可单独除去的多个日剂量单位，由此作为激素 活性成分第一激素成分组合含有雌激素制剂和至少一种足以抑制孕妇制剂排卵的剂量，并且作为激素活性成分，第二激素成分仅含有雌激素制剂，其中第一激素成分包含 23或24日单位，第二激素成分含有4，3或2日单位，在这两种激素组分之间，存在2或1种无活性成分的每日单位，或者指示2或1个空白药丸日， 激素每日单位数量和无活性成分的每日单位或空白药片天数等于t 期望周期的天数，但长度至少为28天。 这种组合制剂对于女性避孕是有用的，并且允许在每个单独剂量单位中尽可能低的雌激素含量，并且每个给药周期具有低的总激素含量，具有高避孕可靠性，滤泡发育发生率低， 和令人满意的循环控制，可靠地避免周期性月经出血以及不良副作用。