公开(公告)号：US07514463B2

公开(公告)日：2009-04-07

申请号：US10922747

申请日：2004-08-20

申请人： Gunda I. Georg ,  Joseph S. Tash ,  Ramappa Chakrasali ,  Sudhakar Rao Jakkaraj

发明人： Gunda I. Georg ,  Joseph S. Tash ,  Ramappa Chakrasali ,  Sudhakar Rao Jakkaraj

IPC分类号： A61K31/416 ,  C07D231/56

CPC分类号： C07D231/56 ,  C07D471/04

摘要： Novel compounds useful for inhibiting spermatogenesis and cancer treatment, and in particular as inhibitors of heat shock proteins and/or elongation factor 1 alpha.

摘要翻译： 用于抑制精子发生和癌症治疗的新型化合物，特别是作为热休克蛋白和/或延伸因子1α的抑制剂。

公开(公告)号：US08377958B2

公开(公告)日：2013-02-19

申请号：US12830681

申请日：2010-07-06

申请人： Ingrid Gunda Georg ,  Joseph S. Tash ,  Ramappa Chakrasali ,  Sudhakar Rao Jakkaraj ,  Katherine Roby

发明人： Ingrid Gunda Georg ,  Joseph S. Tash ,  Ramappa Chakrasali ,  Sudhakar Rao Jakkaraj ,  Katherine Roby

IPC分类号： A61K31/416 ,  A61K31/437

CPC分类号： C07D471/04 ,  A61K31/416 ,  A61K31/4162 ,  C07D231/56

摘要： Fertility management can include: administering to the subject one or more doses of a compound according to Formula I so as to reduce fertility in the subject. Fertility management can also include administering an effective amount of the compound to: impair Sertoli cell function in a male subject; inhibit spermatogenesis in the subject; reduce testis weight in the subject; reduce ovary weight in a female subject; reduce serum progesterone in the female subject; impair ovarian follicle function in the female subject; causing reversible fertility in the subject. In order to return fertility, the method can include ceasing administration of the compound to the subject so as to return fertility in the subject. The compound can be administered for irreversibly sterilizing the subject.

摘要翻译： 生育能力管理可以包括：向受试者施用一种或多种剂量的式I化合物，以降低受试者的生育能力。 生育能力管理还可以包括给予有效量的化合物以损害男性受试者的Sertoli细胞功能; 抑制受试者的精子发生; 减少受试者的睾丸重量; 减少女性受试者的卵巢重量; 减少女性受试者的血清孕酮; 影响女性卵巢卵泡功能; 导致受试者的可逆生育力。 为了返回生育力，该方法可以包括停止对受试者施用化合物以使受试者的生育力恢复。 该化合物可被用于不可逆地灭菌受试者。

公开(公告)号：US20090197911A1

公开(公告)日：2009-08-06

申请号：US12395521

申请日：2009-02-27

申请人： Ingrid Gunda Georg ,  Joseph S. Tash ,  Ramappa Chakrasali ,  Sudhakar Rao Jakkaraj ,  James P. Calvet

发明人： Ingrid Gunda Georg ,  Joseph S. Tash ,  Ramappa Chakrasali ,  Sudhakar Rao Jakkaraj ,  James P. Calvet

IPC分类号： A61K31/4162 ,  A61K31/416 ,  A61P13/12

CPC分类号： C07D231/56 ,  C07D471/04

摘要： Lonidamine derivatives can be useful in methods of treating, inhibiting, and/or preventing polycystic kidney disease (PKD). Accordingly, lonidamine derivatives can be administered in a therapeutically effective amount for inhibiting, and/or preventing polycystic kidney disease (PKD) in the subject. This can include administering a therapeutically effective amount of the lonidamine derivatives for inhibiting CFTR and/or Hsp90 or biological pathway thereof. Also, the method can include administering the lonidamine derivatives in a therapeutically effective amount for inhibiting ErbB2, Src, Raf-1, B-Raf, MEK, Cdk4, NKCC1, or combinations thereof. For example, the therapeutically effective amount of the lonidamine derivatives can be configured so as to provide a concentration in or adjacent to a kidney cell of about 0.25 uM or more or less.

摘要翻译： 罗丹明胺衍生物可用于治疗，抑制和/或预防多囊肾病（PKD）的方法。 因此，可以以治疗有效量的方式施用孤啡酸衍生物以抑制和/或预防受试者中的多囊肾病（PKD）。 这可以包括施用治疗有效量的用于抑制CFTR和/或Hsp90或其生物学途径的洋芋胺衍生物。 此外，该方法可以包括以治疗有效量施用用于抑制ErbB2，Src，Raf-1，B-Raf，MEK，Cdk4，NKCC1或其组合的兰酸胺衍生物。 例如，可以配置兰定胺衍生物的治疗有效量，以使其在肾细胞中或邻近肾细胞中的浓度为约0.25uM或更大或更小。

公开(公告)号：US08362031B2

公开(公告)日：2013-01-29

申请号：US12395521

申请日：2009-02-27

申请人： Ingrid Gunda Georg ,  Joseph S. Tash ,  Ramappa Chakrasali ,  Sudhakar Rao Jakkaraj ,  James P. Calvet

发明人： Ingrid Gunda Georg ,  Joseph S. Tash ,  Ramappa Chakrasali ,  Sudhakar Rao Jakkaraj ,  James P. Calvet

IPC分类号： A61K31/4162 ,  A61K31/416 ,  A61P13/12

CPC分类号： C07D231/56 ,  C07D471/04

摘要： Lonidamine derivatives can be useful in methods of treating, inhibiting, and/or preventing polycystic kidney disease (PKD). Accordingly, lonidamine derivatives can be administered in a therapeutically effective amount for inhibiting, and/or preventing polycystic kidney disease (PKD) in the subject. This can include administering a therapeutically effective amount of the lonidamine derivatives for inhibiting CFTR and/or Hsp90 or biological pathway thereof. Also, the method can include administering the lonidamine derivatives in a therapeutically effective amount for inhibiting ErbB2, Src, Raf-1, B-Raf, MEK, Cdk4, NKCC1, or combinations thereof. For example, the therapeutically effective amount of the lonidamine derivatives can be configured so as to provide a concentration in or adjacent to a kidney cell of about 0.25 uM or more or less.

摘要翻译： 兰尼达胺衍生物可用于治疗，抑制和/或预防多囊肾病（PKD）的方法。 因此，可以以治疗有效量的方式施用孤啡酸衍生物以抑制和/或预防受试者中的多囊肾病（PKD）。 这可以包括施用治疗有效量的用于抑制CFTR和/或Hsp90或其生物学途径的洋芋胺衍生物。 此外，该方法可以包括以治疗有效量施用用于抑制ErbB2，Src，Raf-1，B-Raf，MEK，Cdk4，NKCC1或其组合的兰酸胺衍生物。 例如，可以配置兰定胺衍生物的治疗有效量，以使其在肾细胞中或邻近肾细胞中的浓度为约0.25uM或更大或更小。

公开(公告)号：US20110060003A1

公开(公告)日：2011-03-10

申请号：US12830681

申请日：2010-07-06

申请人： Ingrid Gunda Georg ,  Joseph S. Tash ,  Ramappa Chakrasali ,  Sudhakar Rao Jakkaraj ,  Katherine Roby

发明人： Ingrid Gunda Georg ,  Joseph S. Tash ,  Ramappa Chakrasali ,  Sudhakar Rao Jakkaraj ,  Katherine Roby

IPC分类号： A61K31/416 ,  A61K31/437 ,  A61P3/00 ,  A61P15/00

CPC分类号： C07D471/04 ,  A61K31/416 ,  A61K31/4162 ,  C07D231/56

摘要： Fertility management can include: administering to the subject one or more doses of a compound according to Formula I so as to reduce fertility in the subject. Fertility management can also include administering an effective amount of the compound to: impair Sertoli cell function in a male subject; inhibit spermatogenesis in the subject; reduce testis weight in the subject; reduce ovary weight in a female subject; reduce serum progesterone in the female subject; impair ovarian follicle function in the female subject; causing reversible fertility in the subject. In order to return fertility, the method can include ceasing administration of the compound to the subject so as to return fertility in the subject. The compound can be administered for irreversibly sterilizing the subject.

摘要翻译： 生育能力管理可以包括：向受试者施用一种或多种剂量的式I化合物，以降低受试者的生育能力。 生育能力管理还可以包括给予有效量的化合物以损害男性受试者的Sertoli细胞功能; 抑制受试者的精子发生; 减少受试者的睾丸重量; 减少女性受试者的卵巢重量; 减少女性受试者的血清孕酮; 影响女性卵巢卵泡功能; 导致受试者的可逆生育力。 为了返回生育力，该方法可以包括停止对受试者施用化合物以使受试者的生育力恢复。 该化合物可被用于不可逆地灭菌受试者。