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公开(公告)号：US20120178688A1
公开(公告)日：2012-07-12
申请号：US13365213
申请日：2012-02-02
申请人： FELIX KARIM , AMOS BARUCH , DEREK MACLEAN , KANAD DAS , QUN YIN
发明人： FELIX KARIM , AMOS BARUCH , DEREK MACLEAN , KANAD DAS , QUN YIN
CPC分类号： C07K7/06 , A61K9/0019 , A61K9/08 , A61K38/00 , A61K47/60 , C07K5/1013 , C07K7/08
摘要： Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X1-X2-X3-X4-X5-X6-X7, wherein the X1 subunit comprises a thiol-containing moiety and the distribution of charge on the X2-X7 subunits provides the desired activity. Methods of using the compounds for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders are also described, and in particular, methods for lowering plasma PTH and serum calcium are provided. The compounds can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.
摘要翻译： 描述了具有降低甲状旁腺激素水平的活性的化合物。 在一个实施方案中，化合物由亚单位X1-X2-X3-X4-X5-X6-X7的连续序列组成，其中X1亚基包含含巯基的部分，并且X2-X7亚基上的电荷分布 提供所需的活动。 还描述了使用该化合物治疗甲状旁腺功能亢进，骨疾病和/或高钙血症的方法，特别是提供降低血浆PTH和血清钙的方法。 这些化合物可用于治疗患有例如：原发性，继发性或甲状腺功能亢进的受试者; 恶性高钙血症; 转移性骨病; 或骨质疏松。
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2.发明授权Polycationic calcium modulator peptides for the treatment of hyperparathyroidism and hypercalcemic disorders 有权用于治疗甲状旁腺功能亢进和高钙血症的多阳离子钙调节肽公开(公告)号：US08987200B2
公开(公告)日：2015-03-24
申请号：US11941857
申请日：2007-11-16
申请人： Gregory Bell , Sarah Walter , Felix Karim
发明人： Gregory Bell , Sarah Walter , Felix Karim
IPC分类号： A61K38/29 , C07K14/635 , A61K38/17
CPC分类号： A61K38/17
摘要： The present invention provides methods and kits for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders. In particular, methods for lowering serum PTH and serum calcium using polycationic calcium modulator peptides are provided. The calcium modulator peptides can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.
摘要翻译： 本发明提供了用于治疗甲状旁腺功能亢进，骨疾病和/或高钙血症的方法和试剂盒。 特别地，提供了使用聚阳离子钙调节剂肽降低血清PTH和血清钙的方法。 钙调节肽可用于治疗患有例如：原发性，继发性或次级甲状旁腺功能亢进的受试者; 恶性高钙血症; 转移性骨病; 或骨质疏松。
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公开(公告)号：US08377880B2
公开(公告)日：2013-02-19
申请号：US13365213
申请日：2012-02-02
申请人： Felix Karim , Amos Baruch , Derek MacLean , Kanad Das , Qun Yin
发明人： Felix Karim , Amos Baruch , Derek MacLean , Kanad Das , Qun Yin
CPC分类号： C07K7/06 , A61K9/0019 , A61K9/08 , A61K38/00 , A61K47/60 , C07K5/1013 , C07K7/08
摘要： Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X1—X2—X3—X4—X5—X6—X7, wherein the X1 subunit comprises a thiol-containing moiety and the distribution of charge on the X2—X7 subunits provides the desired activity. Methods of using the compounds for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders are also described, and in particular, methods for lowering plasma PTH and serum calcium are provided. The compounds can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.
摘要翻译： 描述了具有降低甲状旁腺激素水平的活性的化合物。 在一个实施方案中，化合物由亚单位X1-X2-X3-X4-X5-X6-X7的连续序列组成，其中X1亚基包含含巯基的部分，并且X2-X7亚基上的电荷分布 提供所需的活动。 还描述了使用该化合物治疗甲状旁腺功能亢进，骨疾病和/或高钙血症的方法，特别是提供降低血浆PTH和血清钙的方法。 这些化合物可用于治疗患有例如：原发性，继发性或甲状腺功能亢进的受试者; 恶性高钙血症; 转移性骨病; 或骨质疏松。
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4.发明申请公开(公告)号：US20100311671A1
公开(公告)日：2010-12-09
申请号：US12732091
申请日：2010-03-25
CPC分类号： A61K47/645 , A61K47/62
摘要： Disclosed herein are methods for transdermal delivery of PKC modulatory peptides. Generally, methods comprise the delivery of an isozyme specific PKC peptide modulator through skin that has been microporated, e.g., with an array of microneedles. Such methods may be used to administer therapeutically effective amounts of an isozyme selective PKC peptide inhibitor or activator.
摘要翻译： 本文公开了用于透皮递送PKC调节肽的方法。 通常，方法包括通过已被微孔化的皮肤（例如用微针阵列）递送同工酶特异性PKC肽调节剂。 这种方法可用于施用治疗有效量的同工酶选择性PKC肽抑制剂或活化剂。
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5.发明申请公开(公告)号：US20090023652A1
公开(公告)日：2009-01-22
申请号：US11941857
申请日：2007-11-16
申请人： Gregory Bell , Sarah Walter , Felix Karim
发明人： Gregory Bell , Sarah Walter , Felix Karim
CPC分类号： A61K38/17
摘要： The present invention provides methods and kits for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders. In particular, methods for lowering serum PTH and serum calcium using polycationic calcium modulator peptides are provided. The calcium modulator peptides can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.
摘要翻译： 本发明提供了用于治疗甲状旁腺功能亢进，骨疾病和/或高钙血症的方法和试剂盒。 特别地，提供了使用聚阳离子钙调节剂肽降低血清PTH和血清钙的方法。 钙调节肽可用于治疗患有例如：原发性，继发性或次级甲状旁腺功能亢进的受试者; 恶性高钙血症; 转移性骨病; 或骨质疏松。
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6.发明申请公开(公告)号：US20070269378A1
公开(公告)日：2007-11-22
申请号：US10556440
申请日：2004-06-18
申请人： Gregory Plowman , Felix Karim , Candace Swimmer , Hinrich Habeck , Thomas Koblizek , Stefan Schulte-Merker , Ulrike Eisenmann , Gordon Stott , Torsten Trowe , Andreas Vogel , Joerg Odenthal , Jochen Scheel , Torsten Will , Yinsheng Jin , Lynn Bjerke , Timothy Heuer
发明人： Gregory Plowman , Felix Karim , Candace Swimmer , Hinrich Habeck , Thomas Koblizek , Stefan Schulte-Merker , Ulrike Eisenmann , Gordon Stott , Torsten Trowe , Andreas Vogel , Joerg Odenthal , Jochen Scheel , Torsten Will , Yinsheng Jin , Lynn Bjerke , Timothy Heuer
CPC分类号： G01N33/574 , A01K67/0275 , A01K2217/058 , A01K2227/40 , A01K2267/03 , A61K49/0008 , C12N9/1205 , C12Q1/485 , G01N33/5008 , G01N33/5011 , G01N33/5041
摘要： Human NADK genes are identified as modulators of branching morphogenesis, and thus are therapeutic targets for disorders associated with defective branching morphogenesis function. Methods for identifying modulators of branching morpho-genesis, comprising screening for agents that modulate the activity of NADK are provided.
摘要翻译： 人NADK基因被鉴定为分支形态发生的调节剂，因此是与缺陷支链形态发生功能相关的病症的治疗靶点。 提供用于鉴定分支形态发生的调节剂的方法，包括筛选调节NADK活性的试剂。
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公开(公告)号：US08969299B2
公开(公告)日：2015-03-03
申请号：US13492778
申请日：2012-06-08
申请人： Felix Karim , Gregory Bell
发明人： Felix Karim , Gregory Bell
摘要： Methods for modulating serum phosphorus levels are described, wherein calcimimetic agents are administered to a subject in need thereof. In one embodiment, the compound is cinacalcet, and in other embodiments the compound is comprised of a contiguous sequence of subunits, X1—X2—X3—X4—X5—X6—X7, wherein the X1 subunit comprises a thiol-containing moiety and the distribution of charge on the X2-X7 subunits. The compound, when administered at selected times to a patient undergoing dialysis, lowers serum phosphorus levels, relative to pre-dosing levels, and achieves a sustained reduced level for a period of time after administration.
摘要翻译： 描述了调节血清磷水平的方法，其中向有需要的受试者施用拟拟剂。 在一个实施方案中，化合物是西那卡塞，在其它实施方案中，该化合物由亚单位X1-X2-X3-X4-X5-X6-X7的连续序列组成，其中X1亚基包含含硫醇的部分， X2-X7亚基上的电荷分布。 该化合物在选定的时间对经历透析的患者施用时，相对于给药前水平降低血清磷水平，并且在施用后达到持续降低水平一段时间。
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公开(公告)号：US20130150301A1
公开(公告)日：2013-06-13
申请号：US13492778
申请日：2012-06-08
申请人： Felix Karim , Gregory Bell
发明人： Felix Karim , Gregory Bell
摘要： Methods for modulating serum phosphorus levels are described, wherein calcimimetic agents are administered to a subject in need thereof. In one embodiment, the compound is cinacalcet, and in other embodiments the compound is comprised of a contiguous sequence of subunits, X1—X2—X3—X4—X5—X6—X7, wherein the X1 subunit comprises a thiol-containing moiety and the distribution of charge on the X2-X7 subunits. The compound, when administered at selected times to a patient undergoing dialysis, lowers serum phosphorus levels, relative to pre-dosing levels, and achieves a sustained reduced level for a period of time after administration.
摘要翻译： 描述了调节血清磷水平的方法，其中向有需要的受试者施用拟拟剂。 在一个实施方案中，化合物是西那卡塞，在其它实施方案中，该化合物由亚单位X1-X2-X3-X4-X5-X6-X7的连续序列组成，其中X1亚基包含含硫醇的部分， X2-X7亚基上的电荷分布。 该化合物在选定的时间对经历透析的患者施用时，相对于给药前水平降低血清磷水平，并且在施用后达到持续降低水平一段时间。
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公开(公告)号：US20110028394A1
公开(公告)日：2011-02-03
申请号：US12846724
申请日：2010-07-29
申请人： Felix KARIM , Amos Baruch , Derek MaClean
发明人： Felix KARIM , Amos Baruch , Derek MaClean
CPC分类号： C07K7/06 , A61K9/0019 , A61K9/08 , A61K38/00 , A61K47/60 , C07K5/1013 , C07K7/08
摘要： Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X1-X2-X3-X4-X5-X6-X7, wherein the X1 subunit comprises a thiol-containing moiety and the distribution of charge on the X2-X7 subunits provides the desired activity. Methods of using the compounds for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders are also described, and in particular, methods for lowering plasma PTH and serum calcium are provided. The compounds can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.
摘要翻译： 描述了具有降低甲状旁腺激素水平的活性的化合物。 在一个实施方案中，化合物由亚单位X1-X2-X3-X4-X5-X6-X7的连续序列组成，其中X1亚基包含含巯基的部分，并且X2-X7亚基上的电荷分布 提供所需的活动。 还描述了使用该化合物治疗甲状旁腺功能亢进，骨疾病和/或高钙血症的方法，特别是提供降低血浆PTH和血清钙的方法。 这些化合物可用于治疗患有例如：原发性，继发性或甲状腺功能亢进的受试者; 恶性高钙血症; 转移性骨病; 或骨质疏松。
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公开(公告)号：US5747275A
公开(公告)日：1998-05-05
申请号：US909984
申请日：1997-08-12
申请人： Gerry Rubin , Marc Therrien , Henry Chang , Felix Karim , David Wassarman
发明人： Gerry Rubin , Marc Therrien , Henry Chang , Felix Karim , David Wassarman
IPC分类号： C12N15/09 , A61K31/00 , A61K38/00 , A61K45/00 , A61P43/00 , C12N1/15 , C12N5/10 , C12N9/12 , C12N15/54 , C12Q1/48 , C07H21/04 , C07K1/00 , C12P21/06
CPC分类号： C12N9/1205 , A61K38/00
摘要： The kinase suppressor of Ras (Ksr), a novel protein kinase involved in the regulation of cell growth and differentiation, provides an important target for therapeutic intervention. The subject compositions also include nucleic acids which encode a Ksr kinase, and hybridization probes and primers capable of hybridizing with a Ksr gene. Such probes are used to identify mutant Ksr alleles associated with disease. The invention includes methods, including phosphorylation and binding assays, for screening chemical libraries for lead compounds for a pharmacological agent useful in the diagnosis or treatment of disease associated Ksr activity or Ksr-dependent signal transduction.
摘要翻译： 参与调节细胞生长和分化的新蛋白激酶Ras（Ksr）的激酶抑制剂为治疗干预提供了重要的靶标。 主题组合物还包括编码Ksr激酶的核酸，以及能够与Ksr基因杂交的杂交探针和引物。 这样的探针用于鉴定与疾病相关的突变体Ksr等位基因。 本发明包括用于筛选用于诊断或治疗与疾病相关的Ksr活性或Ksr依赖性信号转导的药理学试剂的化合物的化学文库的方法，包括磷酸化和结合测定。
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