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1. 发明申请

US20120178688A1 THERAPEUTIC AGENTS FOR REDUCING PARATHYROID HORMONE LEVELS 有权
标题翻译：用于减少帕拉霉素激素水平的治疗药物
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
IPC分类号： A61K38/08 , A61P5/20 , C07K7/06
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。

2. 发明申请

US20120129790A1 METHODS OF USE OF EPSILON INHIBITOR COMPOUNDS FOR THE ATTENUATION OF PAIN 失效
标题翻译：使用EPSILON抑制剂化合物减轻疼痛的方法
公开(公告)号：US20120129790A1
公开(公告)日：2012-05-24
申请号：US13230724
申请日：2011-09-12
申请人： Derek Maclean , Qun Yin
发明人： Derek Maclean , Qun Yin
IPC分类号： A61K38/17 , A61P25/00 , C07K14/435
CPC分类号： A61K38/16 , A61K38/10 , A61K38/45 , C07K2319/10
摘要： The disclosure herein relates to modified εPKC inhibitory peptides, methods of generating such peptides, and method for using εPKC inhibitory peptides for the treatment of pain.
摘要翻译：本文的公开涉及修饰的PKC抑制肽，产生这些肽的方法，以及使用PKC抑制肽治疗疼痛的方法。

3. 发明授权

US09255124B2 Modifications of peptide compositions to increase stability and delivery efficiency 有权
标题翻译：改进肽组合物以增加稳定性和递送效率
公开(公告)号：US09255124B2
公开(公告)日：2016-02-09
申请号：US13305685
申请日：2011-11-28
申请人： Derek Maclean
发明人： Derek Maclean
IPC分类号： C07K7/00 , A61K38/10 , A61K47/48
CPC分类号： C12N9/96 , A61K38/10 , A61K47/64 , A61K47/645 , C07K7/00 , C12N9/12 , C12Y207/11013
摘要： The disclosed invention relates to methods of modifying peptide compositions to increase stability and delivery efficiency. Specifically, the disclosed invention relates to methods to increase the stability and delivery efficiency of protein kinase C (PKC) modulatory peptide compositions. A “therapeutic peptide composition” comprises a “carrier peptide” and a “cargo peptide.” A “carrier peptide” is a peptide or amino acid sequence within a peptide that facilitates the cellular uptake of the therapeutic peptide composition. The “cargo peptide” is a PKC modulatory peptide. Peptide modifications to either the carrier peptide, the cargo peptide, or both, which are described herein increase the stability and delivery efficiency of therapeutic peptide compositions by reducing disulfide bond exchange, physical stability, reducing proteolytic degradation, and increasing efficiency of cellular uptake.
摘要翻译：所公开的发明涉及修饰肽组合物以提高稳定性和递送效率的方法。具体地，所公开的发明涉及增加蛋白激酶C（PKC）调节肽组合物的稳定性和递送效率的方法。 “治疗性肽组合物”包含“载体肽”和“货物肽”。“载体肽”是促进细胞摄取治疗性肽组合物的肽内的肽或氨基酸序列。 “货物肽”是PKC调节肽。通过减少二硫键交换，物理稳定性，减少蛋白水解降解和增加细胞摄取的效率，本文所述的载体肽，载体肽或两者的肽修饰增加了治疗性肽组合物的稳定性和递送效率。

4. 发明授权

US08999932B2 Therapeutic agents for reducing parathyroid hormone levels 有权
标题翻译：降低甲状旁腺激素水平的治疗剂
公开(公告)号：US08999932B2
公开(公告)日：2015-04-07
申请号：US12846724
申请日：2010-07-29
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
IPC分类号： A61K38/08 , A61P13/12 , A61P5/18 , C07K7/06 , C07K7/08 , A61K47/48 , C07K5/103 , A61K38/00
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。

5. 发明授权

US08492346B2 Methods of use of epsilon inhibitor compounds for the attenuation of pain 失效
标题翻译：使用ε抑制剂化合物减轻疼痛的方法
公开(公告)号：US08492346B2
公开(公告)日：2013-07-23
申请号：US13230724
申请日：2011-09-12
申请人： Derek Maclean , Qun Yin
发明人： Derek Maclean , Qun Yin
IPC分类号： A61K38/16 , A61K38/00 , C07K14/00
CPC分类号： A61K38/16 , A61K38/10 , A61K38/45 , C07K2319/10
摘要： The disclosure herein relates to modified εPKC inhibitory peptides, methods of generating such peptides, and method for using εPKC inhibitory peptides for the treatment of pain.
摘要翻译：本文的公开内容涉及修饰的epsilonPKC抑制肽，产生此类肽的方法，以及使用epsilonPKC抑制肽治疗疼痛的方法。

6. 发明授权

US08017583B2 Methods of use of epsilon inhibitor compounds for the attenuation of pain 失效
标题翻译：使用ε抑制剂化合物减轻疼痛的方法
公开(公告)号：US08017583B2
公开(公告)日：2011-09-13
申请号：US12018111
申请日：2008-01-22
申请人： Derek MacLean , Qun Yin
发明人： Derek MacLean , Qun Yin
IPC分类号： A61K38/16 , A61K38/00 , C07K14/00
CPC分类号： A61K38/16 , A61K38/10 , A61K38/45 , C07K2319/10
摘要： The disclosure herein relates to modified εPKC inhibitory peptides, methods of generating such peptides, and method for using εPKC inhibitory peptides for the treatment of pain.
摘要翻译：本文的公开涉及修饰的PKC抑制肽，产生这些肽的方法，以及使用PKC抑制肽治疗疼痛的方法。

7. 发明授权

US06426357B1 Antagonists of follicle stimulating hormone activity 失效
标题翻译：促卵泡激素活性的拮抗剂
公开(公告)号：US06426357B1
公开(公告)日：2002-07-30
申请号：US09629180
申请日：2000-07-31
申请人： Randall A. Scheuerman , Stephen D. Yanofsky , Christopher P. Holmes , Derek MacLean , Beatrice Ruhland , Ronald W. Barrett , Jay E. Wrobel , Ariamala Gopalsamy
发明人： Randall A. Scheuerman , Stephen D. Yanofsky , Christopher P. Holmes , Derek MacLean , Beatrice Ruhland , Ronald W. Barrett , Jay E. Wrobel , Ariamala Gopalsamy
IPC分类号： A61K31427
CPC分类号： C07D417/04 , C07D417/14
摘要： The present invention provides a compound of the formula: and methods for using the same, wherein R1, R2, R3, R4 and X are those defined herein.
摘要翻译：本发明提供下式的化合物及其使用方法：其中R1，R2，R3，R4和X为本文定义的化合物。

8. 发明申请

US20120178138A1 MODIFICATIONS OF PEPTIDE COMPOSITIONS TO INCREASE STABILITY AND DELIVERY EFFICIENCY 审中-公开
标题翻译：肽组合物的改性以提高稳定性和递送效率
公开(公告)号：US20120178138A1
公开(公告)日：2012-07-12
申请号：US13305685
申请日：2011-11-28
申请人： DEREK MACLEAN
发明人： DEREK MACLEAN
IPC分类号： C12N9/96
CPC分类号： C12N9/96 , A61K38/10 , A61K47/64 , A61K47/645 , C07K7/00 , C12N9/12 , C12Y207/11013
摘要： The disclosed invention relates to methods of modifying peptide compositions to increase stability and delivery efficiency. Specifically, the disclosed invention relates to methods to increase the stability and delivery efficiency of protein kinase C (PKC) modulatory peptide compositions. A “therapeutic peptide composition” comprises a “carrier peptide” and a “cargo peptide.” A “carrier peptide” is a peptide or amino acid sequence within a peptide that facilitates the cellular uptake of the therapeutic peptide composition. The “cargo peptide” is a PKC modulatory peptide. Peptide modifications to either the carrier peptide, the cargo peptide, or both, which are described herein increase the stability and delivery efficiency of therapeutic peptide compositions by reducing disulfide bond exchange, physical stability, reducing proteolytic degradation, and increasing efficiency of cellular uptake.
摘要翻译：所公开的发明涉及修饰肽组合物以提高稳定性和递送效率的方法。具体地，所公开的发明涉及增加蛋白激酶C（PKC）调节肽组合物的稳定性和递送效率的方法。 “治疗性肽组合物”包含“载体肽”和“货物肽”。“载体肽”是促进细胞摄取治疗性肽组合物的肽内的肽或氨基酸序列。 “货物肽”是PKC调节肽。通过减少二硫键交换，物理稳定性，减少蛋白水解降解和增加细胞摄取的效率，本文所述的载体肽，载体肽或两者的肽修饰增加了治疗性肽组合物的稳定性和递送效率。

9. 发明申请

US20090042769A1 MODIFICATIONS OF PEPTIDE COMPOSITIONS TO INCREASE STABILITY AND DELIVERY EFFICIENCY 有权
标题翻译：肽组合物的改性以提高稳定性和递送效率
公开(公告)号：US20090042769A1
公开(公告)日：2009-02-12
申请号：US12017985
申请日：2008-01-22
申请人： Derek MACLEAN
发明人： Derek MACLEAN
IPC分类号： A61K38/02 , C07K19/00 , C07K1/113
CPC分类号： C12N9/96 , A61K38/10 , A61K47/64 , A61K47/645 , C07K7/00 , C12N9/12 , C12Y207/11013
摘要： The disclosed invention relates to methods of modifying peptide compositions to increase stability and delivery efficiency. Specifically, the disclosed invention relates to methods to increase the stability and delivery efficiency of protein kinase C (PKC) modulatory peptide compositions. A “therapeutic peptide composition” comprises a “carrier peptide” and a “cargo peptide.” A “carrier peptide” is a peptide or amino acid sequence within a peptide that facilitates the cellular uptake of the therapeutic peptide composition. The “cargo peptide” is a PKC modulatory peptide. Peptide modifications to either the carrier peptide, the cargo peptide, or both, which are described herein increase the stability and delivery efficiency of therapeutic peptide compositions by reducing disulfide bond exchange, physical stability, reducing proteolytic degradation, and increasing efficiency of cellular uptake.
摘要翻译：所公开的发明涉及修饰肽组合物以提高稳定性和递送效率的方法。具体地，所公开的发明涉及增加蛋白激酶C（PKC）调节肽组合物的稳定性和递送效率的方法。 “治疗性肽组合物”包含“载体肽”和“货物肽”。 “载体肽”是促进细胞摄取治疗性肽组合物的肽内的肽或氨基酸序列。 “货物肽”是PKC调节肽。通过减少二硫键交换，物理稳定性，减少蛋白水解降解和增加细胞摄取的效率，本文所述的载体肽，载体肽或两者的肽修饰增加了治疗性肽组合物的稳定性和递送效率。

10. 发明授权

US5846839A Methods for hard-tagging an encoded synthetic library 失效
公开(公告)号：US5846839A
公开(公告)日：1998-12-08
申请号：US577203
申请日：1995-12-22
申请人： Mark A. Gallop , Eric Gordon , Zhi-Jie Ni , Derek MacLean , Christopher Holmes , William Fitch , Nikhil Shah
发明人： Mark A. Gallop , Eric Gordon , Zhi-Jie Ni , Derek MacLean , Christopher Holmes , William Fitch , Nikhil Shah
IPC分类号： C40B70/00 , G01N33/543 , G01N33/545 , G01N33/68 , G01N33/44 , G01N33/53
CPC分类号： G01N33/545 , G01N33/54306 , G01N33/68 , B01J2219/00572 , C40B70/00
摘要： Disclosed are chemical encryption methods for determining the structure of compounds formed in situ on solid supports by the use of specific amines tags which, after compound synthesis, can be deencrypted to provide the structure of the compound found on the support.

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