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公开(公告)号：US20120264821A1
公开(公告)日：2012-10-18
申请号：US13442466
申请日：2012-04-09
IPC分类号： A61K31/353 , A61P5/16 , A61P3/04 , A61P17/00 , C07D311/58 , A61P13/08
CPC分类号： A61K31/353 , A23L33/10 , A23V2002/00 , A61K8/498 , A61K9/0014 , A61K9/0053 , A61K31/35 , A61K31/352 , A61Q7/00 , A61Q19/08
摘要： Equol (7-hydroxy-3(4′hydroxyphenyl)-chroman), the major metabolite of the phytoestrogen daidzein, specifically binds and blocks the hormonal action of 5α-dihydrotestosterone (DHT) in vitro and in vivo. Equol can bind circulating free DHT and sequester it from the androgen receptor, thus altering growth and physiological hormone responses that are regulated by androgens. These data suggest a novel model to explain equol's biological properties. The significance of equol's ability to specifically bind and sequester DHT from the androgen receptor have important ramifications in health and disease and may indicate a broad and important usage for equol in the treatment and prevention of androgen-mediated pathologies. Thus, equol can specifically bind DHT and prevent DHT's biological actions in physiological and pathophysiological processes.
摘要翻译： 洋甘菊（7-羟基-3（4'-羟基苯基） - 苯并二氢吡喃）是植物雌激素黄豆苷元的主要代谢物，在体外和体内特异性结合和阻断5α-二氢睾酮（DHT）的激素作用。 Equol可以结合循环的自由DHT并将其从雄激素受体中隔离，从而改变由雄激素调节的生长和生理激素反应。 这些数据表明了一种解释牛尿酚生物学特性的新模型。 雌激素特异性结合并从雄激素受体中螯合DHT的能力的意义在健康和疾病中具有重要的影响，并且可能表明在治疗和预防雄激素介导的病理学中雌马酚的广泛和重要用途。 因此，雌马酚可以特异性结合DHT并防止DHT在生理和病理生理过程中的生物学作用。
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2.发明申请COMPOSITIONS AND PRODUCTS CONTAINING S-EQUOL, AND METHODS FOR THEIR MAKING 有权含有S-EQUOL的组合物和产品及其制备方法公开(公告)号：US20100120705A1
公开(公告)日：2010-05-13
申请号：US12558949
申请日：2009-09-14
IPC分类号： A61K31/352 , A61P19/10 , A61P5/30 , A61P5/00 , A61P9/00 , A61P1/16 , A61P35/00 , A61P25/28 , A61K31/7048
CPC分类号： A61K31/352 , A23L33/10 , A61K8/498 , A61K9/0014 , A61K31/353 , A61K2800/10 , A61Q19/00 , C07D311/58 , C07D311/74
摘要： A composition for use in making commercial food and skin products comprising S-equol or mixtures, including both a non-racemic mixture and a racemic mixture, of S-equol and R-equol. The composition can be used to make articles of commerce such as food supplements, pharmaceuticals, and medicaments. The compositions are useful in a method of delivering S-equol to a mammal to prevent or treat a disease or associated condition, including hormone-dependent diseases or conditions such as cardiovascular disease, lipid disorder, osteopenia, osteoporosis, liver disease, and acute ovarian estrogen deficiency. The S-equol enantiomer can be produced in a biological synthesis from the metabolism of an isoflavone by an organism.
摘要翻译： 用于制备包含S-牛尿酚或S-牛尿酚和R-牛尿酚的含有非外消旋混合物和外消旋混合物的混合物的商业食品和皮肤产品的组合物。 该组合物可用于制造商品，如食品添加剂，药物和药物。 所述组合物可用于向哺乳动物递送S-牛尿酚以预防或治疗疾病或相关病症（包括激素依赖性疾病或病症如心血管疾病，脂质障碍，骨质减少，骨质疏松症，肝脏疾病和急性卵巢）的方法 雌激素缺乏症。 S-牛尿酚对映异构体可以通过生物体从异黄酮代谢产生于生物合成中。
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公开(公告)号：US20100069653A1
公开(公告)日：2010-03-18
申请号：US12435033
申请日：2009-05-04
IPC分类号： C07D311/04
CPC分类号： C07D311/58 , C07D311/04 , C07D311/38
摘要： A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.
摘要翻译： 通过在具有手性配体的Ir催化剂的存在下不对称地氢化色烯化合物来制备对映异构体色烷的方法。 该方法包括对映体雌马酚的对映选择性制备。 优选的Ir催化剂具有手性膦腈恶唑啉配体。 可以获得高立体选择性纯度的对映异构体。
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公开(公告)号：US20130116450A1
公开(公告)日：2013-05-09
申请号：US13608330
申请日：2012-09-10
IPC分类号： C07D311/58 , C07D311/38
CPC分类号： C07D311/58 , C07D311/04 , C07D311/38
摘要： A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.
摘要翻译： 通过在具有手性配体的Ir催化剂的存在下不对称地氢化色烯化合物来制备对映异构体色烷的方法。 该方法包括对映体雌马酚的对映选择性制备。 优选的Ir催化剂具有手性膦腈恶唑啉配体。 可以获得高立体选择性纯度的对映异构体。
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5.发明申请COMPOSITIONS AND PRODUCTS CONTAINING S-EQUOL, AND METHODS FOR THEIR MAKING 有权含有S-EQUOL的组合物和产品及其制备方法公开(公告)号：US20120004189A1
公开(公告)日：2012-01-05
申请号：US13150797
申请日：2011-06-01
IPC分类号： A61K31/7048 , A23L2/52 , A23L1/30 , A61K31/353
CPC分类号： A61K31/352 , A23L33/10 , A61K8/498 , A61K9/0014 , A61K31/353 , A61K2800/10 , A61Q19/00 , C07D311/58 , C07D311/74
摘要： A composition for use in making commercial food and skin products comprising S-equol or mixtures, including both a non-racemic mixture and a racemic mixture, of S-equol and R-equol. The composition can be used to make articles of commerce such as food supplements, pharmaceuticals, and medicaments. The compositions are useful in a method of delivering S-equol to a mammal to prevent or treat a disease or associated condition, including hormone-dependent diseases or conditions such as cardiovascular disease, lipid disorder, osteopenia, osteoporosis, liver disease, and acute ovarian estrogen deficiency. The S-equol enantiomer can be produced in a biological synthesis from the metabolism of an isoflavone by an organism.
摘要翻译： 用于制备包含S-牛尿酚或S-牛尿酚和R-牛尿酚的含有非外消旋混合物和外消旋混合物的混合物的商业食品和皮肤产品的组合物。 该组合物可用于制造商品，如食品添加剂，药物和药物。 所述组合物可用于向哺乳动物递送S-牛尿酚以预防或治疗疾病或相关病症（包括激素依赖性疾病或病症如心血管疾病，脂质障碍，骨质减少，骨质疏松症，肝脏疾病和急性卵巢）的方法 雌激素缺乏症。 S-牛尿酚对映异构体可以通过生物体从异黄酮代谢产生于生物合成中。
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6.发明授权公开(公告)号：US08048913B2
公开(公告)日：2011-11-01
申请号：US12558949
申请日：2009-09-14
IPC分类号： A61K31/35 , C07D311/00
CPC分类号： A61K31/352 , A23L33/10 , A61K8/498 , A61K9/0014 , A61K31/353 , A61K2800/10 , A61Q19/00 , C07D311/58 , C07D311/74
摘要： A composition for use in making commercial food and skin products comprising S-equol or mixtures, including both a non-racemic mixture and a racemic mixture, of S-equol and R-equol. The composition can be used to make articles of commerce such as food supplements, pharmaceuticals, and medicaments. The compositions are useful in a method of delivering S-equol to a mammal to prevent or treat a disease or associated condition, including hormone-dependent diseases or conditions such as cardiovascular disease, lipid disorder, osteopenia, osteoporosis, liver disease, and acute ovarian estrogen deficiency. The S-equol enantiomer can be produced in a biological synthesis from the metabolism of an isoflavone by an organism.
摘要翻译： 用于制备包含S-牛尿酚或S-牛尿酚和R-牛尿酚的含有非外消旋混合物和外消旋混合物的混合物的商业食品和皮肤产品的组合物。 该组合物可用于制造商品，如食品添加剂，药物和药物。 所述组合物可用于向哺乳动物递送S-牛尿酚以预防或治疗疾病或相关病症（包括激素依赖性疾病或病症如心血管疾病，脂质障碍，骨质减少，骨质疏松症，肝脏疾病和急性卵巢）的方法 雌激素缺乏症。 S-牛尿酚对映异构体可以通过生物体从异黄酮代谢产生于生物合成中。
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公开(公告)号：US07960573B2
公开(公告)日：2011-06-14
申请号：US12435033
申请日：2009-05-04
IPC分类号： C07D311/00
CPC分类号： C07D311/58 , C07D311/04 , C07D311/38
摘要： A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.
摘要翻译： 通过在具有手性配体的Ir催化剂的存在下不对称地氢化色烯化合物来制备对映异构体色烷的方法。 该方法包括对映体雌马酚的对映选择性制备。 优选的Ir催化剂具有手性膦腈恶唑啉配体。 可以获得高立体选择性纯度的对映异构体。
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公开(公告)号：US20100087519A1
公开(公告)日：2010-04-08
申请号：US12572791
申请日：2009-10-02
IPC分类号： A61K31/353 , A61P43/00
CPC分类号： A61K31/353 , A23L33/10 , A23V2002/00 , A61K8/498 , A61K9/0014 , A61K9/0053 , A61K31/35 , A61K31/352 , A61Q7/00 , A61Q19/08
摘要： Equol (7-hydroxy-3(4′hydroxyphenyl)-chroman), the major metabolite of the phytoestrogen daidzein, specifically binds and blocks the hormonal action of 5α-dihydrotestosterone (DHT) in vitro and in vivo. Equol can bind circulating free DHT and sequester it from the androgen receptor, thus altering growth and physiological hormone responses that are regulated by androgens. These data suggest a novel model to explain equol's biological properties. The significance of equol's ability to specifically bind and sequester DHT from the androgen receptor have important ramifications in health and disease and may indicate a broad and important usage for equol in the treatment and prevention of androgen-mediated pathologies. Thus, equol can specifically bind DHT and prevent DHT's biological actions in physiological and pathophysiological processes.
摘要翻译： 洋甘菊（7-羟基-3（4'-羟基苯基） - 苯并二氢吡喃）是植物雌激素黄豆苷元的主要代谢物，在体外和体内特异性结合和阻断5α-二氢睾酮（DHT）的激素作用。 Equol可以结合循环的自由DHT并将其从雄激素受体中隔离，从而改变由雄激素调节的生长和生理激素反应。 这些数据表明了一种解释牛尿酚生物学特性的新模型。 雌激素特异性结合并从雄激素受体中螯合DHT的能力的意义在健康和疾病中具有重要的影响，并且可能表明在治疗和预防雄激素介导的病理学中雌马酚的广泛和重要用途。 因此，雌马酚可以特异性结合DHT并防止DHT在生理和病理生理过程中的生物学作用。
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公开(公告)号：US07528267B2
公开(公告)日：2009-05-05
申请号：US11194280
申请日：2005-08-01
IPC分类号： C07D311/00
CPC分类号： C07D311/58 , C07D311/04 , C07D311/38
摘要： A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.
摘要翻译： 通过在具有手性配体的Ir催化剂的存在下不对称地氢化色烯化合物来制备对映异构体色烷的方法。 该方法包括对映体雌马酚的对映选择性制备。 优选的Ir催化剂具有手性膦腈恶唑啉配体。 可以获得高立体选择性纯度的对映异构体。
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10.发明授权公开(公告)号：US09173866B2
公开(公告)日：2015-11-03
申请号：US10625989
申请日：2003-07-24
IPC分类号： A01N43/16 , A61K31/35 , A61K31/352 , C07D311/58 , A23L1/30 , A61K8/49 , A61K9/00 , A61K31/353 , A61Q19/00 , C07D311/74
CPC分类号： A61K31/352 , A23L33/10 , A61K8/498 , A61K9/0014 , A61K31/353 , A61K2800/10 , A61Q19/00 , C07D311/58 , C07D311/74
摘要： A composition for use in making commercial food and skin products comprising R-equol. The composition can be used to make articles of commerce such as food supplements, pharmaceuticals, and medicaments. The compositions are useful in a method of delivering R-equol to a mammal to prevent or treat a disease or associated condition, including hormone-dependent diseases or conditions such as cardiovascular disease, lipid disorder, osteopenia, osteoporosis, liver disease, and acute ovarian estrogen deficiency. The R-equol enantiomer can be produced by chiral-phase column separation from a racemic mixture of equol.
摘要翻译： 一种用于制造包含R-牛尿酚的商业食品和皮肤产品的组合物。 该组合物可用于制造商品，如食品添加剂，药物和药物。 该组合物可用于向哺乳动物递送R-牛尿酚以预防或治疗疾病或相关病症（包括激素依赖性疾病或病症如心血管疾病，脂质障碍，骨质减少，骨质疏松症，肝脏疾病和急性卵巢）的方法 雌激素缺乏症。 R-牛尿酚对映异构体可以通过手性柱分离从雌马酚的外消旋混合物制备。
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