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公开(公告)号：US08435973B2
公开(公告)日：2013-05-07
申请号：US12892351
申请日：2010-09-28
申请人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Michael Weske , Pasi Koskimies , Lila Pirkkala
发明人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Michael Weske , Pasi Koskimies , Lila Pirkkala
IPC分类号： A61K31/566 , A61K31/58 , C07J1/00 , C07J17/00 , C07J43/00
CPC分类号： C07J43/00
摘要： Substituted steroid compounds which represent selective inhibitors of 17β-hydroxysteroid dehydrogenase type I (17β-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17β-estradiol concentration.
摘要翻译： 代表17β-羟基类固醇脱氢酶I型（17β-HSD1）的选择性抑制剂的替代类固醇化合物，另外可以代表类固醇硫酸酯酶的抑制剂，其盐，含有这些化合物的药物制剂及其制备方法 化合物。 还公开了使用这种取代的类固醇化合物的治疗方法，特别是在治疗，抑制，预防或预防类固醇激素依赖性疾病或病症例如类固醇激素依赖性疾病或需要抑制I型17β-羟类固醇脱氢酶的病症和 /或类固醇硫酸酯酶和/或需要降低内源性17β-雌二醇浓度。
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2.发明申请Amidomethyl-substituted 1-(carboxyalkyl)-cyclopentyl-carbonylamino-benzazepine-N-acetic acid compounds, process and intermediate products for their preparation and pharmaceutical compositions containing them 有权甲基取代的1-（羧基烷基） - 环戊基 - 羰基氨基 - 苯并氮杂-N-乙酸化合物，其制备方法和中间产物以及含有它们的药物组合物公开(公告)号：US20060281732A1
公开(公告)日：2006-12-14
申请号：US11404775
申请日：2006-04-17
申请人： Dagmar Hoeltje , Yvan Fischer , Dieter Ziegler , Michael Weske , Katrin Michaelis , Yasmin Karimi-Nejad , Josef Messinger , Axel Pahl , Constanze Hoefer , Hrissanthi Ikonomidou , Lechoslaw Turski
发明人： Dagmar Hoeltje , Yvan Fischer , Dieter Ziegler , Michael Weske , Katrin Michaelis , Yasmin Karimi-Nejad , Josef Messinger , Axel Pahl , Constanze Hoefer , Hrissanthi Ikonomidou , Lechoslaw Turski
IPC分类号： A61K31/55
CPC分类号： C07D223/16 , C07D401/12 , C07K5/0222 , C07K5/06139
摘要： Compounds having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity corresponding to the formula I, wherein the substituents R1, R2, R3 and R4 have the meanings given in the description and also pharmaceutical compositions containing these compounds, in particular pharmaceutical compositions suitable for treating or inhibiting cardiovascular diseases, sexual dysfunction and/or adverse conditions associated with apoptosis.
摘要翻译： 具有对应于式I的中性内肽酶（NEP）和/或人可溶内肽酶（hSEP）抑制活性的化合物，其中取代基R 1，R 2，R SUP > 3和R 4具有说明书中给出的含义，并且还含有这些化合物的药物组合物，特别是适用于治疗或抑制心血管疾病，性功能障碍和/或不利条件的药物组合物 与凋亡相关。
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公开(公告)号：US20050176742A1
公开(公告)日：2005-08-11
申请号：US11011744
申请日：2004-12-15
申请人： Leena Hirvelae , Nina Johansson , Pasi Koskimies , Olli Pentikaeinen , Tommi Nyroenen , Tiina Salminen , Mark Johnson , Pekka Lehtovuori , Pauli Saarenketo , Bartholomeus Van Steen , Heinrich-Hubert Thole , Mikko Unkila , Josef Messinger , Johanna Kiviniemi , Lila Pirkkala , Bettina Husen
发明人： Leena Hirvelae , Nina Johansson , Pasi Koskimies , Olli Pentikaeinen , Tommi Nyroenen , Tiina Salminen , Mark Johnson , Pekka Lehtovuori , Pauli Saarenketo , Bartholomeus Van Steen , Heinrich-Hubert Thole , Mikko Unkila , Josef Messinger , Johanna Kiviniemi , Lila Pirkkala , Bettina Husen
IPC分类号： A61K31/519 , C07D495/04 , C07D498/02
CPC分类号： C07D495/04 , A61K31/519
摘要： Thiophenepyrimidinone compounds and their use in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring inhibition of 17β-hydroxysteroid dehydrogenase enzymes.
摘要翻译： 噻吩并嘧啶酮化合物及其在治疗中的用途，特别是用于治疗和/或预防类固醇激素依赖性疾病或病症，例如类固醇激素依赖性疾病或需要抑制17β-羟基类固醇脱氢酶的病症。
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4.发明授权17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases 失效17β-羟类固醇脱氢酶1型抑制剂用于治疗激素相关疾病公开(公告)号：US08546392B2
公开(公告)日：2013-10-01
申请号：US12593134
申请日：2008-03-27
申请人： Rolf Hartmann , Martin Frotscher , Sandrine Oberwinkler , Erika Ziegler , Josef Messinger , Heinrich-Hubert Thole
发明人： Rolf Hartmann , Martin Frotscher , Sandrine Oberwinkler , Erika Ziegler , Josef Messinger , Heinrich-Hubert Thole
IPC分类号： A61K31/5375 , A61K31/192 , A61K31/405 , A61K31/47 , A61K31/505 , C07C65/24 , C07C59/40 , C07D209/12 , C07D215/14 , C07D239/26 , C07D265/30
CPC分类号： A61K31/015 , A61K31/498
摘要： The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases. The invention further relates to suitable inhibitors and to a method for the production thereof.
摘要翻译： 本发明涉及非甾体17β-羟类固醇脱氢酶1型抑制剂用于治疗和预防激素依赖性，特别是雌激素依赖性疾病的用途。 本发明进一步涉及合适的抑制剂及其生产方法。
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公开(公告)号：US07524853B2
公开(公告)日：2009-04-28
申请号：US11011744
申请日：2004-12-15
申请人： Leena Hirvelae , Nina Johansson , Pasi Koskimies , Olli Taneli Pentikaeinen , Tommi Nyroenen , Tiina Annamaria Salminen , Mark Stuart Johnson , Pekka Lehtovuori , Pauli Saarenketo , Bartholomeus Johannes Van Steen , Heinrich-Hubert Thole , Mikko Unkila , Josef Messinger , Johanna Kiviniemi , Lila Pirkkala , Bettina Husen
发明人： Leena Hirvelae , Nina Johansson , Pasi Koskimies , Olli Taneli Pentikaeinen , Tommi Nyroenen , Tiina Annamaria Salminen , Mark Stuart Johnson , Pekka Lehtovuori , Pauli Saarenketo , Bartholomeus Johannes Van Steen , Heinrich-Hubert Thole , Mikko Unkila , Josef Messinger , Johanna Kiviniemi , Lila Pirkkala , Bettina Husen
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： C07D495/04 , A61K31/519
摘要： Thiophenepyrimidinone compounds and their use in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring inhibition of 17β-hydroxysteroid dehydrogenase enzymes.
摘要翻译： 噻吩并嘧啶酮化合物及其在治疗中的用途，特别是用于治疗和/或预防类固醇激素依赖性疾病或病症，例如类固醇激素依赖性疾病或需要抑制17β-羟基类固醇脱氢酶的病症。
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公开(公告)号：US07452875B2
公开(公告)日：2008-11-18
申请号：US11833430
申请日：2007-08-03
申请人： Dagmar Hoeltje , Yvan Fischer , Dieter Ziegler , Michael Weske , Katrin Michaelis , Yasmin Karimi-Nejad , Josef Messinger , Axel Pahl , Constanze Hoefer , Hrissanthi Ikonomidou , Lechoslaw Turski
发明人： Dagmar Hoeltje , Yvan Fischer , Dieter Ziegler , Michael Weske , Katrin Michaelis , Yasmin Karimi-Nejad , Josef Messinger , Axel Pahl , Constanze Hoefer , Hrissanthi Ikonomidou , Lechoslaw Turski
IPC分类号： C07D223/16 , A61K38/05 , A61P9/12
CPC分类号： C07D223/16 , C07D401/12 , C07K5/0222 , C07K5/06139
摘要： Compounds having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity corresponding to the formula I, wherein the substituents R1, R2, R3 and R4 have the meanings given in the description and also pharmaceutical compositions containing these compounds, in particular pharmaceutical compositions suitable for treating or inhibiting cardiovascular diseases, sexual dysfunction and/or adverse conditions associated with apoptosis.
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7.发明申请公开(公告)号：US20080249075A1
公开(公告)日：2008-10-09
申请号：US12051937
申请日：2008-03-20
申请人： Josef Messinger , Christiane Boecker , Heinrich-Hubert Thole , Bettina Husen , Maria Hinaje , Monika Buchholz
发明人： Josef Messinger , Christiane Boecker , Heinrich-Hubert Thole , Bettina Husen , Maria Hinaje , Monika Buchholz
CPC分类号： C07J15/005
摘要： Retrosteroidal compounds corresponding to formula I, representing progesterone receptor modulators, and their production, and pharmaceutical preparations containing these compounds. These compounds are useful in the treatment of benign gynecological disorders such as endometriosis and uterine fibroids, as well as for female birth control and for hormone replacement therapy.
摘要翻译： 对应于式I的代替孕酮受体调节剂的反式甾体化合物及其制备，以及含有这些化合物的药物制剂。 这些化合物可用于治疗良性妇科疾病，如子宫内膜异位症和子宫肌瘤，以及女性避孕和激素替代治疗。
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8.发明授权Amidomethyl-substituted 1-(carboxyalkyl) cyclopentyl-carbonylamino-benzazepine-N-acetic acid compounds, process and intermediate products for their preparation and pharmaceutical compositions containing them 有权酰胺甲基取代的1-（羧基烷基）环戊基 - 羰基氨基 - 苯并氮杂-N-乙酸化合物，其制备方法和中间产物以及含有它们的药物组合物公开(公告)号：US07410962B2
公开(公告)日：2008-08-12
申请号：US11773231
申请日：2007-07-03
申请人： Dagmar Hoeltje , Yvan Fischer , Dieter Ziegler , Michael Weske , Katrin Michaelis , Yasmin Karimi-Nejad , Josef Messinger , Axel Pahl , Constanze Hoefer , Hrissanthi Ikonomidou , Lechoslaw Turski
发明人： Dagmar Hoeltje , Yvan Fischer , Dieter Ziegler , Michael Weske , Katrin Michaelis , Yasmin Karimi-Nejad , Josef Messinger , Axel Pahl , Constanze Hoefer , Hrissanthi Ikonomidou , Lechoslaw Turski
IPC分类号： C07D223/16 , A61K38/05 , A61P9/12
CPC分类号： C07K5/06139 , C07K5/0222
摘要： Compounds having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity corresponding to the formula I, wherein the substituents R1, R2, R3 and R4 have the meanings given in the description and also pharmaceutical compositions containing these compounds, in particular pharmaceutical compositions suitable for treating or inhibiting cardiovascular diseases, sexual dysfunction and/or adverse conditions associated with apoptosis.
摘要翻译： 具有对应于式I的中性内肽酶（NEP）和/或人可溶内肽酶（hSEP）抑制活性的化合物，其中取代基R 1，R 2，R SUP > 3和R 4具有说明书中给出的含义，并且还含有这些化合物的药物组合物，特别是适用于治疗或抑制心血管疾病，性功能障碍和/或不利条件的药物组合物 与凋亡相关。
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公开(公告)号：US20080146531A1
公开(公告)日：2008-06-19
申请号：US11856768
申请日：2007-09-18
申请人： Josef Messinger , Uwe Schoen , Heinrich-Hubert Thole , Bettina Husen , Pasi Koskimies , Lila KALLIO nee Pirkkala
发明人： Josef Messinger , Uwe Schoen , Heinrich-Hubert Thole , Bettina Husen , Pasi Koskimies , Lila KALLIO nee Pirkkala
CPC分类号： C07J43/00 , Y10S514/825 , Y10S514/826 , Y10S514/863 , Y10S514/866 , Y10S514/903
摘要： Estratrien-triazoles corresponding to formula (I) (shown below) which are useful in therapy, especially for the treatment and/or prevention or inhibition of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17β-hydroxysteroid dehydrogenase (17β-HSD) such as 17β-HSD type 1, type 2 or type 3 enzyme.
摘要翻译： 对应于式（I）（如下所示）的依那他三唑可用于治疗，特别是用于治疗和/或预防或抑制类固醇激素依赖性病症，优选需要抑制17β的类固醇激素依赖性疾病或病症 - 类固醇脱氢酶（17β-HSD），如17β-HSD 1型，2型或3型酶。
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10.发明申请AMIDOMETHYL-SUBSTITUTED 1-(CARBOXYALKYL) CYCLOPENTYL-CARBONYLAMINO-BENZAZEPINE-N-ACETIC ACID COMPOUNDS, PROCESS AND INTERMEDIATE PRODUCTS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权氨基取代的1-（羧基甲基）环戊烯基 - 亚磺酰氨基 - 苯甲腈-N-乙酸化合物，其制备和其包含它们的药物组合物的方法和中间产物公开(公告)号：US20070265244A1
公开(公告)日：2007-11-15
申请号：US11773231
申请日：2007-07-03
申请人： Dagmar Hoeltje , Yvan Fischer , Dieter Ziegler , Michael Weske , Katrin Michaelis , Yasmin Karimi-Nejad , Josef Messinger , Axel Pahl , Constanze Hoefer , Hrissanthi Ikonomidou , Lechoslaw Turski
发明人： Dagmar Hoeltje , Yvan Fischer , Dieter Ziegler , Michael Weske , Katrin Michaelis , Yasmin Karimi-Nejad , Josef Messinger , Axel Pahl , Constanze Hoefer , Hrissanthi Ikonomidou , Lechoslaw Turski
IPC分类号： A61K31/55 , A61P9/00 , C07D487/00
CPC分类号： C07K5/06139 , C07K5/0222
摘要： Compounds having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity corresponding to the formula I, wherein the substituents R1, R2, R3 and R4 have the meanings given in the description and also pharmaceutical compositions containing these compounds, in particular pharmaceutical compositions suitable for treating or inhibiting cardiovascular diseases, sexual dysfunction and/or adverse conditions associated with apoptosis.
摘要翻译： 具有对应于式I的中性内肽酶（NEP）和/或人可溶内肽酶（hSEP）抑制活性的化合物，其中取代基R 1，R 2，R SUP > 3和R 4具有说明书中给出的含义，并且还含有这些化合物的药物组合物，特别是适用于治疗或抑制心血管疾病，性功能障碍和/或不利条件的药物组合物 与凋亡相关。
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