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1.发明公开17BETA-CYANO-18A-HOMO-19-NOR-ANDROST-4-EN-DERIVAT, DESSEN VERWENDUNG UND DAS DERIVAT ENTHALTENDE ARZNEIMITTEL 有权17β-氰基18A-HOMO-19-去甲雄甾-4-烯衍生物，其用途及药物含有该衍生物的
公开(公告)号：EP2178899A1
公开(公告)日：2010-04-28
申请号：EP08758989.1
申请日：2008-06-04
发明人： KUHNKE, Joachim , HUEBNER, Jan , BOHLMANN, Rolf , FRENZEL, Thomas , KLAR, Ulrich , MENGES, Frederik , RING, Sven , BORDEN, Steffen , MUHN, Hans-Peter , PRELLE, Katja
CPC分类号： C07J41/0094 , C07J53/007 , C07J53/008
摘要： The 17ß-cyano-18a-homo-19-nor-androst-4-ene derivatives of the present invention have gestagenic activity. They have the general chemical formula (1), in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSO2R, wherein R is hydrogen or C1-C4 alkyl, R4 is hydrogen or halogen and in addition either: R6a, R6b together form methylene or 1,2 ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, methyl and hydroxymethylene, and R7 is selected from the group comprising hydrogen, C1-C4 alkyl, C2-C3 alkenyl and cyclopropyl, or: R6a is hydrogen and R6b and R7 together either form methylene, or are omitted, whereby a double bond is formed between C6 and C7, R9 and R10 are hydrogen, or are omitted, whereby a double bond is formed between C9 and C10, R15 and R16 are hydrogen or together form methylene, R17 is selected from the group comprising hydrogen, C1-C4 alkyl and aIIyI, at least one of the substituents R4, R6a, R6b, R7, R15, R16 and R17 not being hydrogen, or R6b and R7 being omitted, whereby a double bond is formed between C6 and C7, or are omitted, whereby a double bond is formed between C1 and C2. The derivatives also comprise the solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts of the aforementioned substances.
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2.发明公开17ß-CYANO-19-ANDROST-4-EN-DERIVAT, DESSEN VERWENDUNG UND DAS DERIVAT ENTHALTENDE ARZNEIMITTEL 审中-公开17-氰基-19-雄甾-4-烯衍生物，其用途及药物含有该衍生物的
公开(公告)号：EP2167525A2
公开(公告)日：2010-03-31
申请号：EP08760962.4
申请日：2008-06-12
发明人： KUHNKE, Joachim , HUEBNER, Jan , BOHLMANN, Rolf , FRENZEL, Thomas , KLAR, Ulrich , MENGES, Frederik , RING, Sven , BORDEN, Steffen , MUHN, Hans-Peter , PRELLE, Katja
CPC分类号： C07J41/0094 , C07J53/007 , C07J53/008
摘要： The 17ß-cyano-19-androst-4-ene derivatives of the present invention have gestagenic activity. They have the general chemical formula (1), in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSO2R, wherein R is hydrogen or C1-C4 alkyl, R1 and R2 independently of one another are hydrogen or methyl, or R1 and R2 together form methylene, or are omitted, whereby a double bond is formed between C1 and C2, R4 is hydrogen or halogen and in addition either: R6a, R6b together form methylene or 1,2 ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, methyl and hydroxymethylene, and R7 is selected from the group comprising hydrogen, C1-C4 alkyl, C2-C3 alkenyl and cyclopropyl, or: R6a is hydrogen and R6b and R7 together form methylene, or are omitted, whereby a double bond is formed between C6 and C7, or: R6a is methyl and R6b and R7 are omitted, whereby a double bond is formed between C6 and C7, R15 and R16 are hydrogen, or together form methylene and R17 is selected from the group comprising hydrogen, C1-C4- alkyl and aIIyI. The derivatives also comprise the solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts of the aforementioned substances, with the proviso that certain compounds are excluded.
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3.发明公开15,16-METHYLEN-17-(1'-PROPENYL)-17,3'-OXIDOESTRA-4-EN-3-ON-DERIVAT, DESSEN VERWENDUNG UND DAS DERIVAT ENTHALTENDE ARZNEIMITTEL 有权15,16-亚甲基-17-（1'-丙烯基）-17,3'-OXIDOESTRA -4-烯-3-酮衍生物，它们的用途及药物衍生物含
公开(公告)号：EP2238148A1
公开(公告)日：2010-10-13
申请号：EP08866797.7
申请日：2008-12-23
发明人： KLAR, Ulrich , KUHNKE, Joachim , BOHLMANN, Rolf , HÜBNER, Jan , RING, Sven , FRENZEL, Thomas , MENGES, Frederik , BORDEN, Steffen , MUHN, Hans, Peter , PRELLE, Katja
CPC分类号： C07J53/008
摘要： The invention relates to 15,16-methylene-17-(1 '-propenyl)-17-3'-oxidoestra-4-en-3-one derivatives with general chemical formula (I), wherein Z, R4, R6a, R6b, R7 and R18 have the designations given in claim 1, and to the solvates, hydrates, stereoisomers and salts thereof, including all crystal modifications and all stereoisomers of said compounds. The invention also relates to the use of said derivatives for producing a medicament for oral contraception and for the treatment of premenopausal, perimenopausal and postmenopausal troubles, and medicaments containing said derivatives, especially the application thereof in the cited cases. The derivatives according to the invention have a gestagen effect, and in preferred cases, also an anti-mineral corticoid and neutral to lightly androgenous effect.
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4.发明授权1,2-DIARYLBENZIMIDAZOLE ZUR BEHANDLUNG VON ERKRANKUNGEN 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：EP1246808B1
公开(公告)日：2011-08-17
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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5.发明授权18-METHYL-19-NOR-ANDROST-4-EN-17,17-SPIROETHER (18-METHYL-19-NOR-20- SPIROX-4-EN-3-ONE), SOWIE DIESE ENTHALTENDE PHARMAZEUTISCHE PRÄPARATE 有权18-甲基-19-去甲雄甾-4-烯17,17-螺醚（18-甲基-19-去甲20蔚华-4-烯-3-酮），和药物制剂含有它们
公开(公告)号：EP2038294B1
公开(公告)日：2010-12-08
申请号：EP07765033.1
申请日：2007-06-29
发明人： BOHLMANN, Rolf , KUHNKE, Joachim , HÜBNER, Jan , GALLUS, Norbert , MENGES, Frederik , BORDEN, Steffen , MUHN,Hans-Peter , PRELLE, Katja
CPC分类号： C07J53/008
摘要： The invention relates to novel 18-methyl-19-nor-androst-4-en-17,17- spiroether of general formula (I), where Z = O, two H, =NOR or =NNHSO2R, R = H, or straight or branched chain C1-4 or C3-4alkyl, R4 = H, halogen, or CF3 and R6 and/or R7 are α- or ß-positioned and R6 and R7 independently = H or straight or branched chain C1-4 or C3-4alkyl or a straight or branched chain C2-4 or C3-4alkylene or a saturated C3-5 cycloalkyl, or together form a methylene group or a double bond. The novel compounds have gestagenic and antimineralcorticoid action.
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6.发明公开17-(1'-PROPENYL)-17-3'-OXIDOESTRA-4-EN-3-ON-DERIVAT, DESSEN VERWENDUNG UND DAS DERIVAT ENTHALTENDE ARZNEIMITTEL 有权17-（1'-丙烯基）-17-3'-OXIDOESTRA -4-烯-3-酮衍生物，它们的用途及药物衍生物含
公开(公告)号：EP2238147A2
公开(公告)日：2010-10-13
申请号：EP08867342.1
申请日：2008-12-23
发明人： KLAR, Ulrich , KUHNKE, Joachim , BOHLMANN, Rolf , HÜBNER, Jan , RING, Sven , FRENZEL, Thomas , MENGES, Frederik , BORDEN, Steffen , MUHN, Hans, Peter , PRELLE, Katja
CPC分类号： C07J21/00 , C07J41/0016 , C07J53/001 , C07J53/007
摘要： The invention relates to 17-(1'-propenyl)-17-3'-oxidoestra-4-en-3-one derivatives with general chemical formula (1) wherein the radicals Z, R
4 , R
6a , R
6b , R
7 , R
15 , R
16a , R
16b and R
18 have the designations given in claim 1, and to the solvates, hydrates and salts thereof, including all stereoisomers of said compounds. The invention also relates to the use of said derivatives for producing a medicament for oral contraception and for the treatment of premenopausal, perimenopausal and postmenopausal complaints, and medicaments containing said derivatives, especially the application thereof in the cited cases. The derivatives according to the invention have a gestagenic effect, and in preferred cases, also an anti-mineral corticoidal and neutral to lightly androgenous effect.-
7.发明授权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：EP1474415B1
公开(公告)日：2011-07-27
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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8.发明公开17-HYDROXY-19-NOR-21-CARBONSÄURE-STEROID Y-LACTON-DERIVAT, DESSEN VERWENDUNG UND DAS DERIVAT ENTHALTENDE ARZNEIMITTEL 审中-公开17-羟基-19-去甲-21-羧酸，其利用与药物含有该衍生物的类固醇的Y内酯衍生物
公开(公告)号：EP2238151A1
公开(公告)日：2010-10-13
申请号：EP08868806.4
申请日：2008-12-23
发明人： KLAR, Ulrich , KUHNKE, Joachim , BOHLMANN, Rolf , HÜBNER, Jan , RING, Sven , FRENZEL, Thomas , MENGES, Frederik , BORDEN, Steffen , MUHN, Hans, Peter , PRELLE, Katja
IPC分类号： C07J53/00 , A61P5/34 , A61K31/585
摘要： The invention relates to 17-hydroxy-19-nor-21-carboxylic acid-steroid γ-lactone derivatives with the chemical formula (I) wherein R4, R6a, R6b, R7, R15, R16a, R16b, R18 and Z have the designations given in claim 1, and to the solvates, hydrates, stereoisomers and salts thereof. The invention also relates to the use of said derivatives for producing a medicament for oral contraception and for the treatment of premenopausal, perimenopausal and postmenopausal troubles, and medicaments containing said derivatives. The derivatives according to the invention have a gestagen effect, and in preferred cases, also an anti-mineral corticoid and neutral to lightly androgenous effect.
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9.发明公开15,16-METHYLEN-17-HYDROXY-19-NOR-21-CARBONSÄURE-STEROID y-LACTON-DERIVAT, DESSEN VERWENDUNG UND DAS DERIVAT ENTHALTENDE ARZNEIMITTEL 有权15,16-亚甲基-17-羟基-19-去甲-21-羧酸-γ-内酯甾类衍生物，它们的用途及药物含有该衍生物的
公开(公告)号：EP2238150A1
公开(公告)日：2010-10-13
申请号：EP08868567.2
申请日：2008-12-23
发明人： KLAR, Ulrich , KUHNKE, Joachim , BOHLMANN, Rolf , HÜBNER, Jan , RING, Sven , FRENZEL, Thomas , MENGES, Frederik , BORDEN, Steffen , MUHN, Hans, Peter , PRELLE, Katja
CPC分类号： C07J53/008
摘要： The invention relates to a 15, 16-methylene-17-hydroxy-19-nor-21 -carboxylic acid-steroid γ-lactone derivative with general chemical formula (I) wherein R4, R6a, R6b, R7 and Z have the designations given in claim 1, and to the solvates, hydrates, stereoisomers and salts thereof. The invention also relates to the use of said derivatives for producing a medicament for oral contraception and for the treatment of premenopausal, perimenopausal and postmenopausal complaints, and medicaments containing said derivatives. The derivatives according to the invention have a gestagenic effect, and in preferred cases, also an anti-mineral corticoidal and neutral to lightly androgenous effect.
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10.发明公开ESTRATRIENE DERIVATIVES COMPRISING HETEROCYCLIC BIOISOSTERES FOR THE PHENOLIC A-RING 审中-公开随着对酚A环的杂环生物电子等排雌三烯衍生物
公开(公告)号：EP2307439A1
公开(公告)日：2011-04-13
申请号：EP09800008.6
申请日：2009-07-14
发明人： BLUME, Thorsten , HELDMANN, Dieter , SCHMEES, Norbert , OTTO, Christiane , WINTERMANTEL, Tim , KUHNKE, Joachim
CPC分类号： C07J71/0047
摘要： The present invention is directed to novel pyrazolo-estrien and triazolo-estrien-derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by an estrogen receptor such as hot flashes, vaginal dryness, osteopenia, osteoporosis, hyperlipidemia, loss of cognitive function, degenerative brain diseases, cardiovascular diseases, cerebrovascular diseases, hormone sensitive cancers and hyperplasia (in tissues including breast, endometrium, and cervix in women and prostate in men), endometriosis, uterine fibroids, osteoarthritis; and as contraceptive agents either alone or in combination with a progestogen or progestogen antagonist. The compounds of the invention are selective estrogen receptor modulators.
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