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1.发明申请19-NOR-STEROID DERIVATIVES WITH A 15ALPHA, 16ALPHA-METHYLENE GROUP AND A SATURATED 17, 17-SPIRO-LACTONE RING, USE THEREOF, AND MEDICAMENTS CONTAINING SAID DERIVATIVES 审中-公开具有15ALPHA，16ALPHA-甲基组的饱和甾体衍生物和饱和的17,17-螺旋体环，其使用和含有所述衍生物的药物公开(公告)号：US20100311702A1
公开(公告)日：2010-12-09
申请号：US12810860
申请日：2008-12-23
申请人： Ulrich Klar , Joachim Kuhnke , Rolf Bohlmann , Jan Hubner , Sven Ring , Thomas Frenzel , Frederik Menges , Steffen Borden , Hans Peter Muhn , Katja Prelle
发明人： Ulrich Klar , Joachim Kuhnke , Rolf Bohlmann , Jan Hubner , Sven Ring , Thomas Frenzel , Frederik Menges , Steffen Borden , Hans Peter Muhn , Katja Prelle
CPC分类号： C07J21/003 , C07J53/008
摘要： The 15α,16α-methylene-17-hydroxy-19-nor-17-pregna-4-en-3-one-21-carboxylic acid γ-lactone derivatives of the present invention possess progestational efficacy. They have the general chemical formula I, in which Z is selected from the group comprising an oxygen atom, two hydrogen atoms, NOR and NNHSO2R, where R is hydrogen, C1-C10-alkyl, aryl or C7-C20-aralkyl, R4 is hydrogen or halogen, and moreover either: R6a, R6b together form methylene or 1,2-ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, C1-C10-alkyl, C2-C10-alkenyl or C2-C10-alkynyl, and R7 is selected from the group comprising hydrogen, C1-C10-alkyl, C3-C6-cycloalkyl, C2-C10-alkenyl or C2-C10-alkynyl, or: R6a is hydrogen and R6b and R7, together, denote a bond, an oxygen or form methylene, R18 represents hydrogen or C1-C3-alkyl and in addition include their solvates, hydrates, stereoisomers and salts.
摘要翻译： 本发明的15α，16α-亚甲基-17-羟基-19-去甲-17-前 - 孕-4-烯-3-酮-21-羧酸γ-内酯衍生物具有促进功效。 它们具有一般化学式I，其中Z选自氧原子，两个氢原子，NOR和NNHSO 2 R，其中R是氢，C 1 -C 10 - 烷基，芳基或C 7 -C 20 - 芳烷基，R 4是 氢或卤素，此外：R6a，R6b一起形成亚甲基或1,2-乙二基或R6a为氢，R6b选自氢，C1-C10-烷基，C2-C10-烯基或C2-C10-烯基， 炔基，R 7选自氢，C 1 -C 10 - 烷基，C 3 -C 6 - 环烷基，C 2 -C 10 - 烯基或C 2 -C 10 - 炔基，或者：R 6a是氢，R 6b和R 7一起表示 键，氧或亚甲基，R 18表示氢或C 1 -C 3 - 烷基，并且还包括它们的溶剂合物，水合物，立体异构体和盐。
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2.发明申请18-Methyl-19-norandrost-4-ene 17, 17-spiro ether (18-methyl-19-nor-20-spirox-4-en-3-one), and pharmaceutical products comprising the same 有权18-甲基-19-去雄甾-4-烯17,17-螺醚（18-甲基-19-去甲-20-螺-4-烯-3-酮）和包含它们的药物公开(公告)号：US20080153787A1
公开(公告)日：2008-06-26
申请号：US11769952
申请日：2007-06-28
申请人： Rolf BOHLMANN , Joachim Kuhnke , Jan Huebner , Norbert Gallus , Frederik Menges , Steffen Borden , Hans-Peter Muhn , Katja Prelle
发明人： Rolf BOHLMANN , Joachim Kuhnke , Jan Huebner , Norbert Gallus , Frederik Menges , Steffen Borden , Hans-Peter Muhn , Katja Prelle
CPC分类号： C07J53/008
摘要： The present invention describes the novel 18-methyl-19-norandrost-4-ene 17,17-spiro ethers of the general formula I in which Z is an oxygen atom, two hydrogen atoms, a group ═NOR or ═NNHSO2R, where R is a hydrogen atom or a straight- or branched-chain alkyl group having 1 to 4 or 3 to 4 carbon atoms, R4 is a hydrogen atom, a halogen atom or a trifluoromethyl group, and R6 and/or R7 may have a or a configuration, and R6 and R7 are independently of one another a hydrogen atom or a straight- or branched-chain alkyl group having 1 to 4 or 3 to 4 carbon atoms or a straight- or branched-chain alkenyl group having 2 to 4 or 3 to 4 carbon atoms or a saturated cycloalkyl group having 3 to 5 carbon atoms or together are a methylene group or a double bond. The novel compounds have progestational and antimineralocorticoid activity.
摘要翻译： 本发明描述了通式I的新颖的18-甲基-19-壬二酸-4-烯17,17-螺醚，其中Z是氧原子，两个氢原子，-NOR或-NNHSO - 2 R，其中R是氢原子或具有1至4或3至4个碳原子的直链或支链烷基，R 4是氢原子，卤素 原子或三氟甲基，R 6和/或R 7可以具有或其结构，并且R 6和R 6可以是 7个彼此独立地为氢原子或具有1至4或3至4个碳原子的直链或支链烷基或具有2至4或3至4个碳原子的直链或支链烯基 4个碳原子或3〜5个碳原子的饱和环烷基或一起是亚甲基或双键。 新化合物具有促孕和抗皮质激素活性。
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3.发明申请1-Phenyl-2-heteroaryl-substituted benzimidazole derivatives, their use for the production of pharmaceutical agents as well as pharmaceutical preparations that contain these derivatives 失效1-苯基-2-杂芳基取代的苯并咪唑衍生物，其用于生产药剂的用途以及含有这些衍生物的药物制剂公开(公告)号：US20050267160A1
公开(公告)日：2005-12-01
申请号：US11198098
申请日：2005-08-04
申请人： Thorsten Blume , Wolfgang Halfbrodt , Joachim Kuhnke , Ursula Moenning , Bernd Elger , Herbert Schneider
发明人： Thorsten Blume , Wolfgang Halfbrodt , Joachim Kuhnke , Ursula Moenning , Bernd Elger , Herbert Schneider
IPC分类号： C07D401/04 , C07D409/04 , C07D413/14 , C07D417/14 , A61K31/4439 , A61K31/4184 , C07D43/02 , C07D49/02
CPC分类号： C07D401/04 , C07D409/04 , C07D413/14 , C07D417/14
摘要： New benzimidazole derivatives are described, their production and their use for the production of pharmaceutical agents for treatment and prevention of diseases that are associated with a microglia activation and T-cell-mediated immunological diseases, as well as pharmaceutical preparations that contain the new benzimidazole derivatives.
摘要翻译： 描述了新的苯并咪唑衍生物，它们的生产及其用于生产用于治疗和预防与小胶质细胞激活和T细胞介导的免疫疾病相关的疾病的药物的用途，以及含有新的苯并咪唑衍生物的药物制剂 。
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4.发明授权
公开(公告)号：US5973172A
公开(公告)日：1999-10-26
申请号：US135483
申请日：1998-08-18
申请人： Klaus Schollkopf , Wolfgang Halfbrodt , Joachim Kuhnke , Wolfgang Schwede , Karl-Heinrich Fritzemeier , Rolf Krattenmacher , Hans-Peter Muhn
发明人： Klaus Schollkopf , Wolfgang Halfbrodt , Joachim Kuhnke , Wolfgang Schwede , Karl-Heinrich Fritzemeier , Rolf Krattenmacher , Hans-Peter Muhn
CPC分类号： C07J71/0005 , C07J53/00 , Y10S514/841 , Y10S514/843
摘要： The invention describes 14,17-C.sub.2 -bridged steroids of general formula (I), ##STR1## wherein the various R groups are as defined in the specification, and wherein said steroids are in contrast, with the disclaimed compound, the new compounds are available even after peroral administration with high gestagenic action and are suitable for the production of pharmaceutical agents.
摘要翻译： 本发明描述了通式（I）的14,17-C 2桥连类固醇，其中各种R基团如本说明书中所定义，并且其中所述类固醇与废弃化合物相反，即使在 口服给药具有较高的孕激素作用，适用于制药。
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5.发明申请15,16-Methylene-17-hydroxy-19-nor-21-carboxylic acid-steroid Y-lactone derivative, use thereof and medicinal products containing the derivative 审中-公开15,16-亚甲基-17-羟基-19-去甲-21-羧酸类固醇Y-内酯衍生物及其衍生物的用途公开(公告)号：US20110015162A1
公开(公告)日：2011-01-20
申请号：US12811002
申请日：2008-12-23
申请人： Ulrich Klar , Joachim Kuhnke , Rolf Bohlmann , Jan Huebner , Sven Ring , Thomas Frenzel , Frederik Menges , Steffen Borden , Hans Peter Muhn , Katja Prelle
发明人： Ulrich Klar , Joachim Kuhnke , Rolf Bohlmann , Jan Huebner , Sven Ring , Thomas Frenzel , Frederik Menges , Steffen Borden , Hans Peter Muhn , Katja Prelle
CPC分类号： C07J53/008
摘要： The invention relates to 15,16-methylene-17-hydroxy-19-nor-21-carboxylic acid-steroid γ-lactone derivatives with the general chemical formula I, and R4, R6a, R6b, R7 and Z have the meanings stated in claim 1, and their solvates, hydrates, stereoisomers and salts. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action.
摘要翻译： 本发明涉及具有一般化学式I的15,16-亚甲基-17-羟基-19-去甲-21-羧酸 - 类固醇γ-内酯衍生物，且R4，R6a，R6b，R7和Z具有以下含义： 权利要求1及其溶剂合物，水合物，立体异构体和盐。 本发明还涉及这些衍生物用于生产口服避孕用药物和用于治疗前，绝经前和绝经后的投诉和含有所述衍生物的药用产品的用途。 根据本发明的衍生物具有促孕作用，在优选情况下另外具有抗皮质激素和中性至轻度雄激素作用。
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6.发明申请Microglia inhibitors for interrupting interleukin 12 and IFNgamma-mediated immune reactions 审中-公开用于中断白细胞介素12和IFNgamma介导的免疫反应的小胶质细胞抑制剂公开(公告)号：US20060211690A1
公开(公告)日：2006-09-21
申请号：US11351603
申请日：2006-02-09
申请人： Thorsten Blume , Wolf-Dietrich Doecke , Wolfgang Halfbrodt , Joachim Kuhnke , Ursula Moenning , Bernd Elger , Herbert Schneider
发明人： Thorsten Blume , Wolf-Dietrich Doecke , Wolfgang Halfbrodt , Joachim Kuhnke , Ursula Moenning , Bernd Elger , Herbert Schneider
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4184
CPC分类号： A61K31/4184
摘要： The invention describes the use of microglia inhibitors for the production of pharmaceutical agents that inhibit immune reactions that are mediated by monocytes, macrophages and T cells, and their use for treating T-cell-mediated immunological diseases and non-T-cell-mediated inflammation reactions.
摘要翻译： 本发明描述了小胶质细胞抑制剂用于制备抑制由单核细胞，巨噬细胞和T细胞介导的免疫反应的药物的用途及其用于治疗T细胞介导的免疫疾病和非T细胞介导的炎症的用途 反应。
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公开(公告)号：US20060205803A1
公开(公告)日：2006-09-14
申请号：US11305521
申请日：2005-12-16
IPC分类号： A61K31/4184 , C07D235/16
CPC分类号： A61K31/4184 , C07D235/18 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： Benzimidazoles of general formula I and the use of benzimidazole derivatives for the production of pharmaceutical agents for treatment and prophylaxis of diseases that are associated with a microglia activation are described.
摘要翻译： 描述了通式I的苯并咪唑和苯并咪唑衍生物用于制备用于治疗和预防与小胶质细胞活化相关的疾病的药物的用途。
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8.发明授权1-Aryl-2-N-, S- or O-substituted benzimidazole derivatives, their use for the production of pharmaceutical agents as well as pharmaceutical preparations that contain these derivatives 失效1-芳基-2-N-，S-或O-取代的苯并咪唑衍生物，其用于生产药物的用途以及含有这些衍生物的药物制剂公开(公告)号：US06903126B2
公开(公告)日：2005-06-07
申请号：US10190620
申请日：2002-07-09
IPC分类号： C07D235/26 , C07D235/28 , C07D235/30 , C07D401/12 , A61K31/4184
CPC分类号： C07D401/12 , C07D235/26 , C07D235/28 , C07D235/30
摘要： The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B, Y and Z have the meanings that are indicated in the description and the claims, the use of these compounds for the production of a pharmaceutical agent for treatment and prevention of diseases associated with microglia activation as well as pharmaceutical preparations that contain these compounds
摘要翻译： 本发明涉及具有通式I的新的苯并咪唑衍生物，其中基团R 1，R 2，R 3，A，B，Y和 Z具有在说明书和权利要求书中指出的含义，这些化合物在制备用于治疗和预防与小胶质细胞活化相关的疾病的药剂中的用途以及含有这些化合物的药物制剂
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9.发明授权Process for the production of 4,4-dimethyl-5&agr;-cholesta-8,14,24-trien-3&bgr;-01 and intermediate products in process (I) 失效方法（I）中生产4,4-二甲基-5α-胆甾烯-8,14,24-三烯-3β-醇和中间产物的方法公开(公告)号：US06683197B1
公开(公告)日：2004-01-27
申请号：US09288691
申请日：1999-04-09
申请人： Thorsten Blume , Peter Esperling , Joachim Kuhnke
发明人： Thorsten Blume , Peter Esperling , Joachim Kuhnke
IPC分类号： C07J900
CPC分类号： C07J51/00 , C07J7/0095 , C07J9/00
摘要： The subject of this invention is a new process with variant embodiments for the production of compound 1.
摘要翻译： 本发明的主题是用于制备化合物1的变体实施方案的新方法。
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公开(公告)号：US5827842A
公开(公告)日：1998-10-27
申请号：US578847
申请日：1995-12-26
申请人： Klaus Schollkopf , Wolfgang Halfbrodt , Joachim Kuhnke , Wolfgang Schwede , Karl-Heinrich Fritzemeier , Rolf Krattenmacher , Hans-Peter Muhn
发明人： Klaus Schollkopf , Wolfgang Halfbrodt , Joachim Kuhnke , Wolfgang Schwede , Karl-Heinrich Fritzemeier , Rolf Krattenmacher , Hans-Peter Muhn
CPC分类号： C07J71/0005 , C07J53/00 , Y10S514/841 , Y10S514/843
摘要： The invention describes 14,17-C.sub.2 -bridged steroids of general formula (I), ##STR1## wherein the various R groups are as defined in the specification, and wherein said steroids are, in contrast with the disclaimed compound 14,17-ethano-19-norpregn-4-ene-3,20-dione bioavailable even after peroral administration with high gestagenic action and are suitable for the production of pharmaceutical agents.
摘要翻译： 本发明描述了通式（I），其中各种R基团如本说明书中所定义的通式（I），其中所述类固醇与被弃置的化合物14相反的14,17-C2-桥连类固醇， 即使在口服给药后，即使在具有高孕激素作用的情况下也能生物利用，并且适用于药物制剂的生产，17-乙醇-19-去甲孕-4-烯-3,20-二酮。
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