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公开(公告)号：EP0799238A2
公开(公告)日：1997-10-08
申请号：EP95943195.0
申请日：1995-12-23
发明人： SCHÖLLKOPF, Klaus , HALFBRODT, Wolfgang , KUHNKE, Joachim , SCHWEDE, Wolfgang , FRITZEMEIER, Karl-Heinrich , KRATTENMACHER, Rolf , MUHN, Hans-Peter
CPC分类号： C07J71/0005 , C07J53/00 , Y10S514/841 , Y10S514/843
摘要： The invention concerns 14,17-C2-bridged steroids of general formula (I), wherein: R3 represents an oxygen atom, the hydroxy amino group or two hydrogen atoms; R6 represents either a hydrogen, fluorine, chlorine or bromine atom or a C¿1?-C4 alkyl group at the α or β position, R?6' and R7¿ then representing hydrogen atoms; or alternatively, R6 represents a hydrogen, fluorine, chlorine or bromine atom or a C¿1?-C4 alkyl group, R?6' and R7¿ then representing a common additional bond; R7 represents a C¿1?-C4 alkyl group at the α or β position, R?6 and R6'¿ then representing hydrogen atoms; or alternatively R?6 and R7¿ together represent a methylene group at the α or β position and R6' represents a hydrogen atom; or R?6 and R6'¿ together represent an ethylene or methylene group and R7 represents a hydrogen atom; R?9 and R10¿ each represent a hydrogen atom or a common bond; R?11 and R12¿ each represent a hydrogen atom or a common bond; R13 represents a methyl or ethyl group; R15 represents a hydrogen atom or a C¿1?-C3 alkyl group; R?16 and R16'¿ independently of one another represent a hydrogen atom, a C¿1?-C3 alkyl group, or a C2-C4 alkenyl group, or together represent a C1-C3 alkylidene group; R?15 and R16¿ represent a common bond and R16' represents a hydrogen atom or a C¿1?-C3 alkyl group, or alternatively R?15 and R16¿ together represent a ring of the partial formula (i) shown, in which n = 1 and 2 and X represents a methylene group or an oxygen atom; and R16' represents a hydrogen atom; R171 represents a hydrogen atom or a C¿1?-C3 alkyl group; R17?2¿ represents a hydrogen atom, a C¿1?-C3 alkyl group or a C2-C4 alkenyl group; R17?1'¿ and R172' each represent a hydrogen atom or a common bond; R21 represents a hydrogen atom or a C¿1?-C3 alkyl group; and R?21'¿ represents a hydrogen atom, C¿1?-C3 alkyl group or hydroxy group. The claimed compounds do not include 14,17-ethano-19-norpregn-4-en-3,20-dione. The novel compounds, unlike the one disclaimed, show a high level of gestagenic activity even after peroral administration and are suitable for use in the production of medicaments.
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公开(公告)号：EP0664811B1
公开(公告)日：1997-08-13
申请号：EP93922949.8
申请日：1993-10-13
发明人： OTTOW, Eckhard , SCHWEDE, Wolfgang , HALFBRODT, Wolfgang , FRITZEMEIER, Karl-Heinrich , KRATTENMACHER, Rolf
CPC分类号： C07J53/002
摘要： Described are etheno- and ethano-19,11-bridged 4-estrenes of general formula (I), in which W, R?1, R2, R6a, R6b, R7, R14, R15, R16, R11, R11' and R19¿ are as defined in the description. Also described is a method of preparing them. These compounds exhibit a marked gestagenic action and are suitable for use in the production of drugs.
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公开(公告)号：EP0664811A1
公开(公告)日：1995-08-02
申请号：EP93922949.0
申请日：1993-10-13
发明人： OTTOW, Eckhard , SCHWEDE, Wolfgang , HALFBRODT, Wolfgang , FRITZEMEIER, Karl-Heinrich , KRATTENMACHER, Rolf
CPC分类号： C07J53/002
摘要： Described are etheno- and ethano-19,11-bridged 4-estrenes of general formula (I), in which W, R , R , R , R , R , R , R , R , R , R and R are as defined in the description. Also described is a method of preparing them. These compounds exhibit a marked gestagenic action and are suitable for use in the production of drugs.
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4.发明公开1-PHENYL-2-HETEROARYL-SUBSTITUIERTE BENZIMIDAZOLDERIVATE, DEREN VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN ZUR BEHANDLUNG VON IMMUNOLOGISCHEN ERKRANKUNGEN 有权1-苯基-2-杂芳基取代的苯并咪唑衍生物，它们在药物的生产免疫疾病的治疗
公开(公告)号：EP1474415A1
公开(公告)日：2004-11-10
申请号：EP03702464.3
申请日：2003-01-17
发明人： BLUME, Thorsten , HALFBRODT, Wolfgang , KUHNKE, Joachim , MÖNNING, Ursula , ELGER, Bernd , SCHNEIDER, Herbert
IPC分类号： C07D401/04 , C07D409/04 , C07D413/14 , C07D417/14 , A61K31/415
CPC分类号： C07D401/04 , C07D409/04 , C07D413/14 , C07D417/14
摘要： The invention relates to the novel benzimidazole derivatives of formula (I), to the production and use thereof in the treatment and prophylaxis of diseases that are associated with microglial activation, and of T-cell mediated immunological diseases. The invention also relates to the pharmaceutical preparations that contain the novel benzimidazole derivatives.
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5.发明公开BENZIMIDAZOLDERIVATE ZUR BEHANDLUNG VON MIT MIKROGLIA-AKTIVIERUNG ASSOZIIERTEN ERKRANKUNGEN WIE INFLAMMATORISCHE, ALLERGISCHE, INFEKTIÖSE ODER AUTOIMMUNE ERKRANKUNGEN 有权苯并咪唑衍生物与小胶质细胞活化有关的病症AS炎性，过敏性,,传染性或自身免疫性疾病TREAT
公开(公告)号：EP1404656A1
公开(公告)日：2004-04-07
申请号：EP02740766.7
申请日：2002-07-05
发明人： BLUME, Thorsten , HALFBRODT, Wolfgang , KUHNKE, Joachim , MOENNING, Ursula , SCHNEIDER, Herbert
IPC分类号： C07D235/26 , C07D235/28 , C07D235/30 , A61K31/4184 , A61P31/00 , A61P37/06 , A61P37/08 , C07D401/12
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 the radicals R?1, R2, R3¿, A, B, Y and Z have the meanings as cited in the description and in the claims. The invention also relates to the use of these compounds for producing a medicament used for the treatment and prophylaxis of diseases associated with a microglia-activation, and to pharmaceutical preparations containing these compounds.
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6.发明公开1-ALKYL-2-ARYL-BENZIMIDAZOLDERIVATE, DEREN VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN SOWIE DIESE DERIVATE ENTHALTENDE PHARMAZEUTISCHE PRÄPARATE 审中-公开1-烷基-2-芳基 - 苯并咪唑衍生物，它们在药物的生产和它们的衍生物药物制剂
公开(公告)号：EP1404321A1
公开(公告)日：2004-04-07
申请号：EP02762333.9
申请日：2002-07-06
发明人： BLUME, Thorsten , HALFBRODT, Wolfgang , KUHNKE, Joachim , MOENNING, Ursula , ELGER, Bernd , SCHNEIDER, Herbert
IPC分类号： A61K31/4184 , C07D235/18 , C07D401/04 , C07D409/04 , C07D403/04 , C07D405/04 , C07D413/04 , C07D403/06 , C07D401/06 , C07D401/14 , C07D403/14 , C07D405/14
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D235/18 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04
摘要： The invention relates to novel benzimidazole derivatives of general formula (I), wherein the groups R?1, R2, R3¿, A, B and Y are defined as per the definition and the claims. The invention also relates to the use of these compounds for producing a medicament for the prophylaxis and treatment of diseases linked to the activation of microglia and to pharmaceutical preparations containing said compounds.
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7.发明授权BENZIMIDAZOLDERIVATE ZUR BEHANDLUNG VON MIT MIKROGLIA-AKTIVIERUNG ASSOZIIERTEN ERKRANKUNGEN WIE INFLAMMATORISCHE, ALLERGISCHE, INFEKTIÖSE ODER AUTOIMMUNE ERKRANKUNGEN 有权BENZIMIDAZOLDERIVATE ZUR BEHANDLUNG VON MIT MIKROGLIA-AKTIVIERUNG ASSOZIIERTEN ERKRANKUNGEN WIE INFLAMMATORISCHE，ALLERGISCHE，INFEKTIÖSEODER AUTOIMMUNE ERKRANKUNGEN
公开(公告)号：EP1404656B9
公开(公告)日：2005-10-19
申请号：EP02740766.7
申请日：2002-07-05
发明人： BLUME, Thorsten , HALFBRODT, Wolfgang , KUHNKE, Joachim , MOENNING, Ursula , SCHNEIDER, Herbert
IPC分类号： C07D235/26 , C07D235/28 , C07D235/30 , A61K31/4184 , A61P31/00 , A61P37/06 , A61P37/08 , C07D401/12
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 the radicals R?1, R2, R3¿, A, B, Y and Z have the meanings as cited in the description and in the claims. The invention also relates to the use of these compounds for producing a medicament used for the treatment and prophylaxis of diseases associated with a microglia-activation, and to pharmaceutical preparations containing these compounds.
摘要翻译： 本发明涉及具有通式（I）的新型苯并咪唑衍生物，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引用的含义。 本发明还涉及这些化合物在制备用于治疗和预防与小胶质细胞活化有关的疾病的药物中的用途，以及含有这些化合物的药物制剂。
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8.发明授权BENZIMIDAZOLDERIVATE ZUR BEHANDLUNG VON MIT MIKROGLIA-AKTIVIERUNG ASSOZIIERTEN ERKRANKUNGEN WIE INFLAMMATORISCHE, ALLERGISCHE, INFEKTIÖSE ODER AUTOIMMUNE ERKRANKUNGEN 有权苯并咪唑衍生物与小胶质细胞活化有关的病症AS炎性，过敏性,,传染性或自身免疫性疾病TREAT
公开(公告)号：EP1404656B1
公开(公告)日：2005-05-18
申请号：EP02740766.7
申请日：2002-07-05
发明人： BLUME, Thorsten , HALFBRODT, Wolfgang , KUHNKE, Joachim , MOENNING, Ursula , SCHNEIDER, Herbert
IPC分类号： C07D235/26 , C07D235/28 , C07D235/30 , A61K31/4184 , A61P31/00 , A61P37/06 , A61P37/08 , C07D401/12
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 the radicals R?1, R2, R3¿, A, B, Y and Z have the meanings as cited in the description and in the claims. The invention also relates to the use of these compounds for producing a medicament used for the treatment and prophylaxis of diseases associated with a microglia-activation, and to pharmaceutical preparations containing these compounds.
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9.发明公开MIKROGLIA-INHIBITOREN ZUR UNTERBRECHUNG VON INTERLEUKIN 12 UND IFN-GAMMA VERMITTELTEN IMMUNREAKTIONEN 审中-公开是否中断白细胞介素12和小胶质细胞抑制剂IFN-γ介导的免疫反应
公开(公告)号：EP1474138A1
公开(公告)日：2004-11-10
申请号：EP03739380.8
申请日：2003-01-17
发明人： BLUME, Thorsten , DÖCKE, Wolf-Dietrich , HALFBRODT, Wolfgang , KUHNKE, Joachim , MÖNNING, Ursula , ELGER, Bernd , SCHNEIDER, Herbert
IPC分类号： A61K31/4184 , A61P1/04 , A61P3/10 , A61P11/06 , A61P17/06 , A61P19/02 , A61P31/12 , A61P37/00
CPC分类号： A61K31/4184
摘要： The invention relates to the use of microglia inhibitors for producing medicaments that inhibit the monocyte, macrophage and T cell-induced immune reactions, and to their use for treating T cell-induced immunological diseases and inflammatory reactions that are not T-cell induced.
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10.发明公开1,2-DIARYLBENZIMIDAZOLE ZUR BEHANDLUNG VON KRANKUNGEN DIE MIT EINER MICROGLIA-AKTIVIERUNG ASSOZIIERT SIND 有权1,2- DIARYLBENZIMIDAZOLE用于疾病相关联的小胶质细胞活化于治疗
公开(公告)号：EP1246808A1
公开(公告)日：2002-10-09
申请号：EP01915133.1
申请日：2001-01-12
IPC分类号： C07D235/18 , A61K31/415 , A61P25/28 , C07D405/04 , C07D401/04 , A61K31/44 , C07D417/04 , C07D401/12 , C07D403/12
CPC分类号： C07D231/12 , C07D233/56 , C07D235/18 , C07D249/08 , C07D401/04 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04
摘要： The invention relates to 1,2-diaryl benzimidazoles of general formula (I) and to the use of benzimidazole derivatives for producing medicaments utilized for the treatment and prophylaxis of illnesses that are associated with a microglia activation.
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