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1. 发明授权

US07030082B2 Pharmaceutical compositions of drug-oligomer conjugates and methods of treating disease therewith 有权
标题翻译：药物 - 低聚物共轭物的药物组合物及其治疗疾病的方法
公开(公告)号：US07030082B2
公开(公告)日：2006-04-18
申请号：US10382069
申请日：2003-03-05
申请人： Richard Soltero , Nnochiri N. Ekwuribe , Foyeke Opawale , Bruce Rehlaender , Anthony Hickey , Li Li Bovet
发明人： Richard Soltero , Nnochiri N. Ekwuribe , Foyeke Opawale , Bruce Rehlaender , Anthony Hickey , Li Li Bovet
IPC分类号： A61K38/02 , A61K38/23
CPC分类号： A61K47/554 , A61K47/542 , A61K47/60
摘要： Pharmaceutical compositions that include a drug and/or drug-oligomer conjugate, a fatty acid component and a bile salt component, or a bile salt component without a fatty acid component are described. The drug can be covalently coupled to an oligomeric moiety. The fatty acid component and the bile salt component, when together, can be present in a weight-to-weight ratio of between 1:15 and 15:1 or any value between. Methods of treating diseases in a subject in need of such treatment using the pharmaceutical compositions of this invention are also provided, as well as methods of providing such pharmaceutical compositions.
摘要翻译：描述了包含药物和/或药物 - 低聚物缀合物，脂肪酸组分和胆汁盐组分的药物组合物或不含脂肪酸组分的胆汁盐组分。该药物可共价偶联至寡聚部分。当一起时，脂肪酸组分和胆汁盐组分可以以1:15至15:1的重量比或两者之间的任何值存在。还提供了使用本发明的药物组合物治疗需要这种治疗的受试者的疾病的方法以及提供这种药物组合物的方法。

2. 发明授权

US06770625B2 Pharmaceutical compositions of calcitonin drug-oligomer conjugates and methods of treating diseases therewith 有权
标题翻译：降钙素药物 - 低聚物共轭物的药物组合物及其治疗疾病的方法
公开(公告)号：US06770625B2
公开(公告)日：2004-08-03
申请号：US10235284
申请日：2002-09-05
申请人： Richard Soltero , Nnochiri N. Ekwuribe , Foyeke Opawale , Bruce Rehlaender , Anthony Hickey , Li Li Bovet
发明人： Richard Soltero , Nnochiri N. Ekwuribe , Foyeke Opawale , Bruce Rehlaender , Anthony Hickey , Li Li Bovet
IPC分类号： A61K3802
CPC分类号： A61K47/554 , A61K47/542 , A61K47/60 , Y10S514/808
摘要： Pharmaceutical compositions that include a drug-oligomer conjugate, a fatty acid component, and a bile salt component are described. The drug is covalently coupled to an oligomeric moiety. The fatty acid component and the bile salt component are present in a weight-to-weight ratio of between 1:5 and 5:1. Methods of treating diseases in a subject in need of such treatment using such pharmaceutical compositions are also provided, as are methods of providing such pharmaceutical compositions.
摘要翻译：描述了包括药物 - 低聚物缀合物，脂肪酸组分和胆汁盐组分的药物组合物。该药物与低聚部分共价偶联。脂肪酸组分和胆汁盐组分以1:5至5:1的重量比重存在。还提供了使用这种药物组合物治疗需要这种治疗的受试者的疾病的方法，以及提供这种药物组合物的方法。

3. 发明授权

US07196059B2 Pharmaceutical compositions of insulin drug-oligomer conjugates and methods of treating diseases therewith 有权
标题翻译：胰岛素药物 - 低聚物共轭物的药物组合物及其治疗疾病的方法
公开(公告)号：US07196059B2
公开(公告)日：2007-03-27
申请号：US10382155
申请日：2003-03-05
申请人： Richard Soltero , Balasingam Radhakrishan , Nnochiri N. Ekwuribe , Bruce Rehlaender , Anthony Hickey , Li Li Bovet
发明人： Richard Soltero , Balasingam Radhakrishan , Nnochiri N. Ekwuribe , Bruce Rehlaender , Anthony Hickey , Li Li Bovet
IPC分类号： A61K38/28 , C07K14/62
CPC分类号： A61K47/554 , A61K47/542 , A61K47/60
摘要： Pharmaceutical compositions that include insulin, an insulin drug-oligomer conjugate, a fatty acid component, and a bile salt component or a bile salt component without a fatty acid component are described. The insulin drug is covalently coupled to an oligomeric moiety. The fatty acid component and the bile salt component, when together, can be present in a weight-to-weight ratio of between 1:15 and 15:1. Methods of treating an insulin deficiency in a subject in need of such treatment using such pharmaceutical compositions are also provided, as are methods of providing such pharmaceutical compositions.
摘要翻译：描述了包括胰岛素，胰岛素药物 - 低聚物缀合物，脂肪酸组分和胆汁盐组分或不含脂肪酸组分的胆汁盐组分的药物组合物。胰岛素药物与低聚部分共价偶联。当一起时，脂肪酸组分和胆汁盐组分可以以1:15至15:1的重量比重存在。还提供了使用这种药物组合物治疗需要这种治疗的受试者的胰岛素缺乏症的方法，以及提供这种药物组合物的方法。

4. 发明授权

US06867183B2 Pharmaceutical compositions of insulin drug-oligomer conjugates and methods of treating diseases therewith 有权
标题翻译：胰岛素药物 - 低聚物共轭物的药物组合物及其治疗疾病的方法
公开(公告)号：US06867183B2
公开(公告)日：2005-03-15
申请号：US10235381
申请日：2002-09-05
申请人： Richard Soltero , Balasingam Radhakrishan , Nnochiri N. Ekwuribe , Bruce Rehlaender , Anthony Hickey , Li Li Bovet
发明人： Richard Soltero , Balasingam Radhakrishan , Nnochiri N. Ekwuribe , Bruce Rehlaender , Anthony Hickey , Li Li Bovet
IPC分类号： A61K47/48 , A61K38/28 , C07K14/62
CPC分类号： A61K47/554 , A61K47/542 , A61K47/60
摘要： Pharmaceutical compositions that include an insulin drug-oligomer conjugate, a fatty acid component, and a bile salt component are described. The insulin drug is covalently coupled to an oligomeric moiety. The fatty acid component and the bile salt component are present in a weight-to-weight ratio of between 1:5 and 5:1. Methods of treating an insulin deficiency in a subject in need of such treatment using such pharmaceutical compositions are also provided, as are methods of providing such pharmaceutical compositions.
摘要翻译：描述了包括胰岛素药物 - 低聚物缀合物，脂肪酸组分和胆汁盐组分的药物组合物。胰岛素药物与低聚部分共价偶联。脂肪酸组分和胆汁盐组分以1:5至5:1的重量比重存在。还提供了使用这种药物组合物治疗需要这种治疗的受试者的胰岛素缺乏症的方法，以及提供这种药物组合物的方法。

5. 发明授权

US07312192B2 Insulin polypeptide-oligomer conjugates, proinsulin polypeptide-oligomer conjugates and methods of synthesizing same 有权
标题翻译：胰岛素多肽 - 低聚物共轭物，胰岛素原多肽 - 低聚物共轭物及其合成方法
公开(公告)号：US07312192B2
公开(公告)日：2007-12-25
申请号：US10389499
申请日：2003-03-14
申请人： Balasingam Radhakrishnan , Richard Soltero , Nnochiri N. Ekwuribe , Monica Puskas , Diti Sangal
发明人： Balasingam Radhakrishnan , Richard Soltero , Nnochiri N. Ekwuribe , Monica Puskas , Diti Sangal
IPC分类号： A61K38/28 , C12P21/06 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00
CPC分类号： C07K14/62 , A61K47/60
摘要： Methods for synthesizing proinsulin polypeptides are described that include contacting a proinsulin polypeptide including an insulin polypeptide coupled to one or more peptides by peptide bond(s) capable of being cleaved to yield the insulin polypeptide with an oligomer under conditions sufficient to couple the oligomer to the insulin polypeptide portion of the proinsulin polypeptide and provide a proinsulin polypeptide-oligomer conjugate, and cleaving the one or more peptides from the proinsulin polypeptide-oligomer conjugate to provide the insulin polypeptide-oligomer conjugate. Methods of synthesizing proinsulin polypeptide-oligomer conjugates are also provided as are proinsulin polypeptide-oligomer conjugates. Methods of synthesizing C-peptide polypeptide-oligomer conjugates and other pro-polypeptide-oligomer conjugates are also provided.
摘要翻译：描述了合成胰岛素原多肽的方法，其包括通过能够被切割的肽键将包含与一个或多个肽偶联的胰岛素原多肽与足够使寡聚物与胰岛素原多肽的胰岛素多肽部分，并提供胰岛素原多肽 - 低聚物缀合物，并切割来自胰岛素原多肽 - 低聚物缀合物的一种或多种肽以提供胰岛素多肽 - 低聚物缀合物。还提供了合成胰岛素原多肽 - 低聚物缀合物的方法，胰岛素原多肽 - 低聚物缀合物。还提供了合成C-肽多肽 - 低聚物缀合物和其它前 - 多肽 - 低聚物缀合物的方法。

6. 发明授权

US06913903B2 Methods of synthesizing insulin polypeptide-oligomer conjugates, and proinsulin polypeptide-oligomer conjugates and methods of synthesizing same 有权
标题翻译：胰岛素多肽 - 低聚物共轭物的合成方法和胰岛素原多肽 - 低聚物共轭物的合成方法及其合成方法
公开(公告)号：US06913903B2
公开(公告)日：2005-07-05
申请号：US10036744
申请日：2001-12-21
申请人： Richard Soltero , Balasingam Radhakrishnan , Nnochiri N. Ekwuribe
发明人： Richard Soltero , Balasingam Radhakrishnan , Nnochiri N. Ekwuribe
IPC分类号： A61K47/48 , C07K14/62 , C12P21/06
CPC分类号： C07K14/62 , A61K47/60
摘要： Methods for synthesizing proinsulin polypeptides are described that include a contacting a proinsulin polypeptide including an insulin polypeptide coupled to one or more peptides by peptide bond(s) capable of being cleaved to yield the insulin polypeptide with an oligomer under conditions sufficient to couple the oligomer to the insulin polypeptide portion of the proinsulin polypeptide and provide a proinsulin polypeptide-oligomer conjugate, and cleaving the one or more peptides from the proinsulin polypeptide-oligomer conjugate to provide the insulin polypeptide-oligomer conjugate. Methods of synthesizing proinsulin polypeptide-oligomer conjugates are also described as are proinsulin polypeptide-oligomer conjugates. Methods of synthesizing C-peptide polypeptide-oligomer conjugates are also described.
摘要翻译：描述了合成胰岛素原多肽的方法，其包括使包含能够被切割的肽键与一个或多个肽偶联的胰岛素原多肽接触，以在足以使所述寡聚体与胰岛素原多肽的胰岛素多肽部分，并提供胰岛素原多肽 - 低聚物缀合物，并切割来自胰岛素原多肽 - 低聚物缀合物的一种或多种肽，以提供胰岛素多肽 - 低聚物缀合物。胰岛素原多肽 - 低聚物缀合物的合成方法也被描述为胰岛素原多肽 - 低聚物缀合物。还描述了合成C-肽多肽 - 低聚物缀合物的方法。

7. 发明授权

US07611864B2 Proinsulin polypeptide-oligomer conjugates 有权
标题翻译：胰岛素原多肽 - 低聚物共轭物
公开(公告)号：US07611864B2
公开(公告)日：2009-11-03
申请号：US10954787
申请日：2004-09-30
申请人： Balasingam Radhakrishnan , Richard Soltero , Nnochiri N. Ekwuribe
发明人： Balasingam Radhakrishnan , Richard Soltero , Nnochiri N. Ekwuribe
IPC分类号： A61K38/28
CPC分类号： C07K14/62 , A61K47/60
摘要： Methods for synthesizing proinsulin polypeptides are described that include a contacting a proinsulin polypeptide including an insulin polypeptide coupled to one or more peptides by peptide bond(s) capable of being cleaved to yield the insulin polypeptide with an oligomer under conditions sufficient to couple the oligomer to the insulin polypeptide portion of the proinsulin polypeptide and provide a proinsulin polypeptide-oligomer conjugate, and cleaving the one or more peptides from the proinsulin polypeptide-oligomer conjugate to provide the insulin polypeptide-oligomer conjugate. Methods of synthesizing proinsulin polypeptide-oligomer conjugates are also described as are proinsulin polypeptide-oligomer conjugates. Methods of synthesizing C-peptide polypeptide-oligomer conjugates are also described.
摘要翻译：描述了合成胰岛素原多肽的方法，其包括使包含能够被切割的肽键与一个或多个肽偶联的胰岛素原多肽接触，以在足以使所述寡聚体与胰岛素原多肽的胰岛素多肽部分，并提供胰岛素原多肽 - 低聚物缀合物，并切割来自胰岛素原多肽 - 低聚物缀合物的一种或多种肽，以提供胰岛素多肽 - 低聚物缀合物。胰岛素原多肽 - 低聚物缀合物的合成方法也被描述为胰岛素原多肽 - 低聚物缀合物。还描述了合成C-肽多肽 - 低聚物缀合物的方法。

8. 发明授权

US07368260B2 Methods of synthesizing insulin polypeptide-oligomer conjugates, and proinsulin polypeptide-oligomer conjugates and methods of synthesizing same 有权
标题翻译：胰岛素多肽 - 低聚物共轭物的合成方法和胰岛素原多肽 - 低聚物共轭物的合成方法及其合成方法
公开(公告)号：US07368260B2
公开(公告)日：2008-05-06
申请号：US11174982
申请日：2005-07-05
申请人： Balasingam Radhakrishnan , Richard Soltero , Nnochiri N. Ekwuribe
发明人： Balasingam Radhakrishnan , Richard Soltero , Nnochiri N. Ekwuribe
IPC分类号： A61K38/28
CPC分类号： C07K14/62 , A61K47/60
摘要： Methods for synthesizing proinsulin polypeptides are described that include a contacting a proinsulin polypeptide including an insulin polypeptide coupled to one or more peptides by peptide bond(s) capable of being cleaved to yield the insulin polypeptide with an oligomer under conditions sufficient to couple the oligomer to the insulin polypeptide portion of the proinsulin polypeptide and provide a proinsulin polypeptide-oligomer conjugate, and cleaving the one or more peptides from the proinsulin polypeptide-oligomer conjugate to provide the insulin polypeptide-oligomer conjugate. Methods of synthesizing proinsulin polypeptide-oligomer conjugates are also described as are proinsulin polypeptide-oligomer conjugates. Methods of synthesizing C-peptide polypeptide-oligomer conjugates are also described.
摘要翻译：描述了合成胰岛素原多肽的方法，其包括使包含能够被切割的肽键与一个或多个肽偶联的胰岛素原多肽接触，以在足以使所述寡聚体与胰岛素原多肽的胰岛素多肽部分，并提供胰岛素原多肽 - 低聚物缀合物，并切割来自胰岛素原多肽 - 低聚物缀合物的一种或多种肽，以提供胰岛素多肽 - 低聚物缀合物。胰岛素原多肽 - 低聚物缀合物的合成方法也被描述为胰岛素原多肽 - 低聚物缀合物。还描述了合成C-肽多肽 - 低聚物缀合物的方法。

9. 发明授权

US07635675B2 Micro-particle fatty acid salt solid dosage formulations for therapeutic agents 有权
标题翻译：用于治疗剂的微粒脂肪酸盐固体剂型制剂
公开(公告)号：US07635675B2
公开(公告)日：2009-12-22
申请号：US10918264
申请日：2004-08-13
申请人： Foyeke Opawale , Richard Soltero
发明人： Foyeke Opawale , Richard Soltero
IPC分类号： A61K9/14 , A61K9/20 , A61K9/26 , A61K9/16 , A61K38/02 , A61K38/16 , A61K38/23 , A61K38/28 , C07K17/00 , C07K17/02 , C07K17/08
CPC分类号： A61K9/2013 , A61K9/1617 , A61K38/23 , A61K38/28 , A61K47/12
摘要： Fatty acid salt particles having a size distribution wherein the particles are from about 1 to about 1,000 microns in diameter, use of the particles in pharmaceutical compositions, as well as methods of making and using the particles and compositions.
摘要翻译：具有尺寸分布的脂肪酸盐颗粒，其中颗粒直径为约1至约1,000微米，药物组合物中使用颗粒，以及制备和使用颗粒和组合物的方法。

10. 发明授权

US07166571B2 Insulin polypeptide-oligomer conjugates, proinsulin polypeptide-oligomer conjugates and methods of synthesizing same 有权
公开(公告)号：US07166571B2
公开(公告)日：2007-01-23
申请号：US10382022
申请日：2003-03-05
申请人： Richard Soltero , Balasingam Radhakrishnan , Nnochiri N. Ekwuribe
发明人： Richard Soltero , Balasingam Radhakrishnan , Nnochiri N. Ekwuribe
IPC分类号： A61K38/28 , C12P31/06 , C07P5/00 , C07P7/00 , C07P16/00 , C07P17/00
CPC分类号： C07K14/62 , A61K47/60
摘要： Methods for synthesizing proinsulin polypeptides are described that include contacting a proinsulin polypeptide including an insulin polypeptide coupled to one or more peptides by peptide bond(s) capable of being cleaved to yield the insulin polypeptide with an oligomer under conditions sufficient to couple the oligomer to the insulin polypeptide portion of the proinsulin polypeptide and provide a proinsulin polypeptide-oligomer conjugate, and cleaving the one or more peptides from the proinsulin polypeptide-oligomer conjugate to provide the insulin polypeptide-oligomer conjugate. Methods of synthesizing proinsulin polypeptide-oligomer conjugates are also provided as are proinsulin polypeptide-oligomer conjugates. Methods of synthesizing C-peptide polypeptide-oligomer conjugates and other pro-polypeptide-oligomer conjugates are also provided.

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