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1.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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2.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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3.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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4.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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5.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.-
6.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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7.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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8.发明公开C-RING-SUBSTITUIERTE PREGN-4-EN-21,17-CARBOLACTONE, SOWIE DIESE ENTHALTENDE PHARMAZEUTISCHE PRÄPARATE 有权C-环取代的孕-4- EN-21,17-carbolactones和药物制剂含有它们
公开(公告)号：EP2297177A1
公开(公告)日：2011-03-23
申请号：EP09757194.7
申请日：2009-05-26
发明人： RING, Sven , BOHLMANN, Rolf , KUHNKE, Joachim , ZORN, Ludwig , BORDEN, Steffen , PRELLE, Katja
CPC分类号： C07J53/008
摘要： The present invention relates to C-ring-substituted pregn-4-ene-21,17-carbolactones of the general formula I in which R
6,7 is an α- or β-methylene and R
9 is a hydrogen atom and R
11 is a bromine, chlorine or fluorine atom or R
9 and R
11 together are a bond. The novel compounds are gestagenic antimineralocorticoids.-
9.发明公开19-NOR-STEROIDDERIVATE MIT EINER 15 ,16 -METHYLENGRUPPE UND EINEM GESÄTTIGTEN 17,17-SPIROLACTONRING, DEREN VERWENDUNG SOWIE DIESE DERIVATE ENTHALTENDE ARZNEIMITTEL 有权WITH A 15ALPHA，16alpha甲基GROUP和饱和17,17-螺内酯，它们的用途和它们的衍生物及药物含19-NOR-甾类衍生物
公开(公告)号：EP2238149A2
公开(公告)日：2010-10-13
申请号：EP08867523.6
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 , A61K31/585 , A61P5/34
CPC分类号： C07J21/003 , C07J53/008
摘要： The invention relates to 15α,16α-methylene-17-hydroxy-19-nor-17-pregna-4-en-3-one-21-carboxylic acid γ-lactone derivatives having a gestagen effect. They are of general chemical formula (I) wherein Z is selected from the group comprising an oxygen atom, two hydrogen atoms, NOR and NNHSO
2 R wherein R is hydrogen, C
1 -C
10 alkyl, aryl or C
7 -C
20 -aralkyl ist, R
4 is hydrogen or halogen, and additionally either: R
6a , R
6b together form methylene or 1,2-ethanediyl or R
6a is hydrogen and R
6b is selected from the group comprising hydrogen, C
1 -C
10 alkyl, C
2 -C
10 alkenyl or C
2 - C
10 alkinyl, and R
7 is selected from the group comprising hydrogen, C
1 -C
10 alkyl, C
3 -C
6 cycloalkyl, C
2 -C
10 alkenyl or C
2 -C
10 alkinyl, or: R
6a is hydrogen and R
6b and R
7 together form a bond, an oxygen or methylene, and R
18 is hydrogen or C
1 -C
3 alkyl. The invention also relates to the solvates, hydrates, stereoisomers and salts of said derivatives.-
10.发明公开17ß-CYANO-19-NOR-ANDROST-4-EN-DERIVAT, DESSEN VERWENDUNG UND DAS DERIVAT ENTHALTENDE ARZNEIMITTEL 有权17-氰基-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：EP2170925A2
公开(公告)日：2010-04-07
申请号：EP08758990.9
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： C07J53/008 , C07J41/0094 , C07J53/007
摘要： The 17ß-cyano-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 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. The derivatives also comprise the solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts of the aforementioned substances.
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