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1.发明申请AZAHETEROCYCLYL DERIVATIVES OF ANDROSTANES AND ANDROSTENES AS MEDICAMENTS FOR CARDIOVASCULAR DISORDERS 有权安非他酮和安慰剂作为心血管疾病药物的偶氮胆碱衍生物公开(公告)号：US20090275542A1
公开(公告)日：2009-11-05
申请号：US12296532
申请日：2007-04-11
申请人： Alberto Cerri , Giorgio Fedrizzi , Alessandra Benicchio , Giuseppe Bianchi , Patrizia Ferrari , Mauro Gobbini , Rosamaria Micheletti , Marco Pozzi , Piero Enrico Scotti
发明人： Alberto Cerri , Giorgio Fedrizzi , Alessandra Benicchio , Giuseppe Bianchi , Patrizia Ferrari , Mauro Gobbini , Rosamaria Micheletti , Marco Pozzi , Piero Enrico Scotti
CPC分类号： C07J43/003
摘要： Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. They are useful for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.
摘要翻译： 式（I）化合物其中：所述基团如说明书中所定义，可用于制备用于治疗心血管疾病，特别是心力衰竭和高血压的药物。 这些化合物是Na +，K + -ATP酶的酶活性的抑制剂。 它们可用于制备用于治疗由内源性哇巴因的高血压作用引起的疾病的药物，例如常染色体显性多囊肾病（ADPKD）的肾衰竭进展，先兆子痫高血压和蛋白尿以及肾衰竭进展 adducin多态性。
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2.发明授权Azaheterocyclyl derivatives of androstanes and androstenes as medicaments for cardiovascular disorders 有权雄激素和雄激素的氮杂环基衍生物作为心血管疾病的药物公开(公告)号：US08536160B2
公开(公告)日：2013-09-17
申请号：US12296532
申请日：2007-04-11
申请人： Alberto Cerri , Giorgio Fedrizzi , Alessandra Benicchio , Giuseppe Bianchi , Patrizia Ferrari , Mauro Gobbini , Rosamaria Micheletti , Marco Pozzi , Piero Enrico Scotti
发明人： Alberto Cerri , Giorgio Fedrizzi , Alessandra Benicchio , Giuseppe Bianchi , Patrizia Ferrari , Mauro Gobbini , Rosamaria Micheletti , Marco Pozzi , Piero Enrico Scotti
CPC分类号： C07J43/003
摘要： Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. They are useful for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.
摘要翻译： 式（I）化合物其中：所述基团如说明书中所定义，可用于制备用于治疗心血管疾病，特别是心力衰竭和高血压的药物。 这些化合物是Na +，K + -ATP酶的酶活性的抑制剂。 它们可用于制备用于治疗由内源性哇巴因的高血压作用引起的疾病的药物，例如常染色体显性多囊肾病（ADPKD）的肾衰竭进展，先兆子痫高血压和蛋白尿和肾衰竭进展 adducin多态性。
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3.发明申请AMINOOXIME DERIVATIVES OF 2- AND/OR 4-SUBSTITUTED ANDROSTANES AND ANDROSTENES AS MEDICAMENTS FOR CARDIOVASCULAR DISORDERS 失效2-和/或4-取代的安慰剂和安慰剂作为心血管疾病药物的氨基酸衍生物公开(公告)号：US20100324003A1
公开(公告)日：2010-12-23
申请号：US12680988
申请日：2008-09-18
申请人： Alberto Cerri , Giuseppe Bianchi , Giorgio Fedrizzi , Patrizia Ferrari , Mauro Gobbini , Giuseppe Marazzi , Marco Torri , Walter Cabri
发明人： Alberto Cerri , Giuseppe Bianchi , Giorgio Fedrizzi , Patrizia Ferrari , Mauro Gobbini , Giuseppe Marazzi , Marco Torri , Walter Cabri
IPC分类号： A61K31/58 , C07J41/00 , C07J43/00 , C07J71/00 , C07J53/00 , A61K31/5685 , A61P9/12 , A61P9/00
CPC分类号： C07J41/0016 , C07J43/003
摘要： New aminooxime derivatives at position 3 of 2- and/or 4-substituted androstanes and androstenes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.
摘要翻译： 2-和/或4-取代的雄甾烷和雄甾烯-3的位置3上的新的氨基肟衍生物，其制备方法以及含有它们用于治疗心力衰竭和高血压的心血管疾病的药物组合物。 特别地描述了具有通式（I）的化合物，其中基团具有本申请中详细描述的含义。
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4.发明授权Aminooxime derivatives of 2- and/or 4-substituted androstanes and androstenes as medicaments for cardiovascular disorders 失效作为心血管疾病药物的2-和/或4-取代的雄甾烷和雄激素的氨基肟衍生物公开(公告)号：US08664210B2
公开(公告)日：2014-03-04
申请号：US12680988
申请日：2008-09-18
申请人： Alberto Cerri , Giuseppe Bianchi , Giorgio Fedrizzi , Patrizia Ferrari , Mauro Gobbini , Marco Torri , Giuseppe Marazzi , Walter Cabri
发明人： Alberto Cerri , Giuseppe Bianchi , Giorgio Fedrizzi , Patrizia Ferrari , Mauro Gobbini , Marco Torri , Giuseppe Marazzi , Walter Cabri
CPC分类号： C07J41/0016 , C07J43/003
摘要： New aminooxime derivatives at position 3 of 2- and/or 4-substituted androstanes and androstenes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.
摘要翻译： 2-和/或4-取代的雄甾烷和雄甾烯-3的位置3上的新的氨基肟衍生物，其制备方法以及含有它们用于治疗心力衰竭和高血压的心血管疾病的药物组合物。 特别地描述了具有通式（I）的化合物，其中基团具有本申请中详细描述的含义。
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5.发明申请AMINO DERIVATIVES OF ANDROSTANES AND ANDROSTENES AS MEDICAMENTS FOR CARDIOVASCULAR DISORDERS 有权安非他明的氨基酸衍生物和作为心血管疾病药物的安慰剂公开(公告)号：US20110053902A1
公开(公告)日：2011-03-03
申请号：US12295497
申请日：2007-04-11
申请人： Alberto Cerri , Marco Torri , Silvia Armaroli , Leonardo Banfi , Giuseppe Bianchi , Giulio Carzana , Patrizia Ferrari , Rosamaria Michaeletti , Simona Sputore , Maria Pia Zappavigna
发明人： Alberto Cerri , Marco Torri , Silvia Armaroli , Leonardo Banfi , Giuseppe Bianchi , Giulio Carzana , Patrizia Ferrari , Rosamaria Michaeletti , Simona Sputore , Maria Pia Zappavigna
CPC分类号： C07J41/0038 , C07J41/0016 , C07J43/003
摘要： Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. Said compounds are used for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.
摘要翻译： 式（I）化合物其中：所述基团如说明书中所定义，可用于制备用于治疗心血管疾病，特别是心力衰竭和高血压的药物。 这些化合物是Na +，K + -ATP酶的酶活性的抑制剂。 所述化合物用于制备用于治疗由内源性哇巴因的高血压作用引起的疾病的药物，例如常染色体显性多囊肾病（ADPKD）的肾衰竭进展，先兆子痫高血压和蛋白尿以及患者肾衰竭进展 与adducin多态性。
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6.发明授权1,5-disubstituted 7A-methylperhydroinden-3A-ol derivatives, useful in treating cardiovascular disorders, processes for their preparation and pharmaceutical compositions containing the same 失效可用于治疗心血管疾病的1,5-二取代的7A-甲基多氢茚-3-醇衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5705531A
公开(公告)日：1998-01-06
申请号：US556854
申请日：1995-11-02
IPC分类号： A61K31/155 , A61K31/195 , A61P9/00 , A61P9/12 , C07C47/267 , C07C47/46 , C07C217/18 , C07C239/10 , C07C239/20 , C07C251/36 , C07C251/38 , C07C251/40 , C07C251/58 , C07C279/08 , C07C279/10 , C07C281/16 , C07C281/18 , C07C281/20 , C07D233/52 , C07D239/22 , C07C279/02
CPC分类号： C07D239/22 , C07C239/20 , C07C251/36 , C07C251/38 , C07C251/58 , C07C279/08 , C07C279/10 , C07C281/16 , C07C281/18 , C07D233/52 , C07B2200/09 , C07C2101/14 , C07C2102/24
摘要： 1,5-Disubstituted 5a-methylperhydroinden-3a-ol derivatives of formula (I): ##STR1## where either the symbol - - - - represents a single bond, the group A is in cis configuration with respect to the 3a-hydroxy, 7a-methyl and 1-L groups, and A is (CH.dbd.CH).sub.m (CH.sub.2).sub.n OR, (CH.dbd.CH).sub.m (CH.sub.2).sub.n NR.sup.1 R.sup.2, (CH.dbd.CH).sub.m (CH.sub.2).sub.p B, OH, O(CH.sub.2).sub.q OR, O(CH.sub.2).sub.q NR.sup.1 R.sup.2 or O(CH.sub.2).sub.r B; q is an integer from 2 to 5; r is an integer from 1 to 2; or the symbol - - - - represents a double bond, A is oxygen, CH(CH.dbd.CH).sub.s (CH.sub.2).sub.n OR, CH(CH.dbd.CH).sub.s (CH.sub.2).sub.n NR.sup.1 R.sup.2 or CH(CH.dbd.CH).sub.s (CH.sub.2).sub.p B; and L is �CH.dbd.C(R.sup.3)!.sub.s CH.dbd.NR.sup.4 or �CH.dbd.C(R.sup.3)!.sub.s CH.sub.2 NHR.sup.4, in the E configuration, are useful for treating cardiovascular disorders such as heart failure and hypertension.
摘要翻译： 式（I）的1,5-二取代的5α-甲基氢化茚-3α-醇衍生物：其中符号+ E，非 - - - EE代表单键，A组为顺式 A为（CH = CH）m + Z（CH 2）nOR，（CH = CH）m + Z（CH 2）n NR 1 R 2，（CH = CH） CH）m + Z（CH2）pB，OH，O（CH2）qOR，O（CH2）qNR1R2或O（CH2） q是2至5的整数; r为1〜2的整数; 或符号+ E，不 - - - + EE表示双键，A是氧，CH + Z（CH = CH）s + Z（CH 2）nOR，CH + Z（CH = CH）s + Z CH2）nNR1R2或CH + Z（CH = CH）s + Z（CH2）pB; 并且L是[CH = C（R3）] sCH = NR4或[CH = C（R3）] sCH2NHR4，在E构型中，可用于治疗心血管疾病如心力衰竭和高血压。
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公开(公告)号：US20090209506A1
公开(公告)日：2009-08-20
申请号：US12305571
申请日：2007-05-31
申请人： Alberto Cerri , Barbara Moro , Maco Torri , Giulio Carzana , Giuseppe Bianchi , Mara Ferrandi , Patrizia Ferrari , Maria Pia Zappavigna , Leonardo Banfi , Giuseppe Giacalone
发明人： Alberto Cerri , Barbara Moro , Maco Torri , Giulio Carzana , Giuseppe Bianchi , Mara Ferrandi , Patrizia Ferrari , Maria Pia Zappavigna , Leonardo Banfi , Giuseppe Giacalone
IPC分类号： A61K31/566 , C07J41/00
CPC分类号： C07J73/005 , C07J63/004 , C07J73/003
摘要： New aminoalkoxyimino derivatives at position 3 of substituted B-homoandrostanes and B-heteroandrostanes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.
摘要翻译： 取代的β-异雄甾烷砜和B-异雄甾烷砜的3位的新的氨基烷氧基亚氨基衍生物，其制备方法以及含有它们用于治疗心力衰竭和高血压的心血管疾病的药物组合物。 特别地描述了具有通式（I）的化合物，其中基团具有本申请中详细描述的含义。
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8.发明授权17-(3-imino-2-alkylpropenyl)-5.beta., 14.beta.-androstane derivatives active on the cardiovascular system, processes for their preparation and pharmaceutical compositions containing same 失效对心血管系统有活性的17-（3-亚氨基-2-烷基丙烯基）-5β，14β-雄甾烷衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5705662A
公开(公告)日：1998-01-06
申请号：US559291
申请日：1995-11-15
CPC分类号： C07J43/003 , C07J41/0055
摘要： New 17-�3-imino-2-alkyl propenyl!-14.beta.-hydroxy-5.beta.-androstane derivatives active on the cardiovascular system by inhibiting Na+,K+-ATPase, a process for their preparation, and to pharmaceutical compositions for the treatment of cardiovascular disorders, such as heart failure and hypertension.
摘要翻译： 通过抑制Na +，K + -ATP酶，其制备方法和用于治疗的药物组合物，对心血管系统上活性的新的17- [3-亚氨基-2-烷基丙烯基]-14β-羟基-5β-雄甾烷衍生物 的心血管疾病，如心力衰竭和高血压。
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9.发明授权Hydrazono-5.beta., 14.beta.-androstane derivatives active on the cardiovascular system, and pharmaceutical compositions containing same 失效对心血管系统有活性的肼基-5β，14β-雄甾烷衍生物和含有它们的药物组合物
公开(公告)号：US5538960A
公开(公告)日：1996-07-23
申请号：US106638
申请日：1993-08-16
申请人： Alberto Cerri , Luigi Bernardi , Giuseppe Bianchi , Patrizia Ferrari , Elena Folpini , Piero Melloni
发明人： Alberto Cerri , Luigi Bernardi , Giuseppe Bianchi , Patrizia Ferrari , Elena Folpini , Piero Melloni
IPC分类号： A61K31/565 , A61K31/58 , A61P9/00 , A61P9/12 , C07J31/00 , C07J41/00 , C07J43/00 , C07J75/00 , C07D43/00 , A61K31/57
CPC分类号： C07J41/0088 , C07J41/0005 , C07J41/0038 , C07J43/003
摘要： The present invention relates to new 17-hydrazonomethyl- and 17-hydrazono-14.beta.-hydroxy-5.beta.-androstane derivatives active on the cardiovascular system, to a process for their preparation and to pharmaceutical compositions containing same for the treatment of cardiovascular disorders, such as heart failure and hypertension.
摘要翻译： 本发明涉及在心血管系统上活性的新的17-亚肼基甲基和17-亚肼基-14β-羟基-5β-雄甾烷衍生物，其制备方法以及含有其用于治疗心血管疾病的药物组合物， 如心力衰竭和高血压。
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10.发明授权Amino derivatives of androstanes and androstenes as medicaments for cardiovascular disorders 有权雄激素和雄激素的氨基衍生物作为心血管疾病的药物公开(公告)号：US08609644B2
公开(公告)日：2013-12-17
申请号：US12295497
申请日：2007-04-11
申请人： Alberto Cerri , Marco Torri , Silvia Armaroli , Leonardo Banfi , Giuseppe Bianchi , Giulio Carzana , Patrizia Ferrari , Rosamaria Michaeletti , Simona Sputore , Maria Pia Zappavigna
发明人： Alberto Cerri , Marco Torri , Silvia Armaroli , Leonardo Banfi , Giuseppe Bianchi , Giulio Carzana , Patrizia Ferrari , Rosamaria Michaeletti , Simona Sputore , Maria Pia Zappavigna
IPC分类号： A61K31/566 , C07J41/00
CPC分类号： C07J41/0038 , C07J41/0016 , C07J43/003
摘要： Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. Said compounds are used for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.
摘要翻译： 式（I）化合物其中：所述基团如说明书中所定义，可用于制备用于治疗心血管疾病，特别是心力衰竭和高血压的药物。 这些化合物是Na +，K + -ATP酶的酶活性的抑制剂。 所述化合物用于制备用于治疗由内源性哇巴因的高血压作用引起的疾病的药物，例如常染色体显性多囊肾病（ADPKD）的肾衰竭进展，先兆子痫高血压和蛋白尿以及患者肾衰竭进展 与adducin多态性。
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