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1. 发明申请

WO2005007122A3 POLYMER STABILIZATION 审中-公开
公开(公告)号：WO2005007122A3
公开(公告)日：2005-01-27
申请号：PCT/US2004/023324
申请日：2004-07-19
申请人： OAKWOOD LABORATORIES, L.L.C. , THANOO, B., C. , MURTAGH, Jim , JOHNS, Gonto
发明人： THANOO, B., C. , MURTAGH, Jim , JOHNS, Gonto
IPC分类号： A61K9/10
摘要： Polymer and drug containing compositions and method of preparing such compositions are disclosed. The dispersed phase formulation has a polymer, a pharmaceutically or biologically active agent and a small fraction of low pKa acid additive. Stable, filter sterilizable, non-gelling solutions containing GnRH analogues at least at levels typically used in sustained release formulations and a method of increasing solubility of a high level of a GnRH analogue or a freeze-dried antagonist of GnRH in a polymer containing solution are also disclosed. The amount of the acid additive in the polymer solution is such that it is sufficient to increase the solubility of the high level of the GnRH analogue in the polymer solution without affecting the release characteristics of the microspheres prepared therefrom.

2. 发明申请

WO2006010155A2 GONADOTROPIN RELEASING HORMONE ANTAGONISTS 审中-公开
标题翻译：促性腺激素释放激素拮抗剂
公开(公告)号：WO2006010155A2
公开(公告)日：2006-01-26
申请号：PCT/US2005/025467
申请日：2005-07-18
申请人： OAKWOOD LABORATORIES, L.L.C , MURTAGH, James , THANOO, Bagavathikanun, C.
发明人： MURTAGH, James , THANOO, Bagavathikanun, C.
IPC分类号： A61K38/09
CPC分类号： A61K9/0019 , A61K9/5031 , A61K38/00 , C07K7/23
摘要： Antagonistic peptides of GnRH having improved water solubility are disclosed. These peptides are capable of suppressing serum testosterone levels in vivo to chemical castration levels of ≤0.5 ng/ml. Stable, filter sterilizable, non-gelling solutions containing the GnRH antagonists at least at levels typically used in sustained release formulations also are disclosed, as is a method of increasing the solubility of GnRH antagonist in a polymer containing dispersed phase, which method comprises addition of an acid to the dispersed phase.
摘要翻译：公开了具有改善的水溶性的GnRH的拮抗肽。这些肽能够抑制体内血清睾酮水平至化学去势水平= 0.5ng / ml。也公开了包含GnRH拮抗剂的稳定的，可过滤灭菌的非胶凝溶液，其至少在通常用于持续释放制剂中的水平下，也是提高GnRH拮抗剂在含有分散相的聚合物中的溶解度的方法，该方法包括加入一种酸到分散相。

3. 发明申请

WO2001010414A1 SLOW RELEASE MICROSPHERES 审中-公开
标题翻译：缓慢释放微球
公开(公告)号：WO2001010414A1
公开(公告)日：2001-02-15
申请号：PCT/US2000021038
申请日：2000-08-02
申请人： OAKWOOD LABORATORIES L.L.C. , THANOO, Bagavathikanun, Chithambara , MURTAGH, James
发明人： OAKWOOD LABORATORIES L.L.C.
IPC分类号： A61K9/14
CPC分类号： A61K9/1647 , A61K38/09
摘要： A continuous process for producing microspheres containing an active agent wherein the microspheres have an average cross sectional porosity of less than 5 % of the total cross sectional area. The microspheres are effective for releasing active agent at a constant and highly uniform rate into a surrounding physiological medium. The microspheres comprise a homopolymer of lactic acid or a copolymer of glycolic and lactic acids. An active agent is homogeneously distributed within a matrix of the homopolymer or copolymer wherein an average number and size of the active agent in a particular unit area is substantially the same as a second average number and size of the active agent in a different unit area of the microsphere.
摘要翻译：一种用于生产含有活性剂的微球的连续方法，其中微球的平均横截面孔隙率小于总横截面积的5％。微球对于将活性剂以恒定且高度均匀的速率释放到周围的生理介质中是有效的。微球包含乳酸的均聚物或乙醇酸和乳酸的共聚物。活性剂均匀地分布在均聚物或共聚物的基质内，其中特定单位面积中的活性剂的平均数量和大小基本上与活性剂在不同单位面积中的第二平均数和大小相同微球。

4. 发明申请

WO2006010155A3 GONADOTROPIN RELEASING HORMONE ANTAGONISTS 审中-公开
公开(公告)号：WO2006010155A3
公开(公告)日：2006-01-26
申请号：PCT/US2005/025467
申请日：2005-07-18
申请人： OAKWOOD LABORATORIES, L.L.C , MURTAGH, James , THANOO, Bagavathikanun, C.
发明人： MURTAGH, James , THANOO, Bagavathikanun, C.
IPC分类号： A61K38/24 , A61K9/14 , C07K17/00
摘要： Antagonistic peptides of GnRH having improved water solubility are disclosed. These peptides are capable of suppressing serum testosterone levels in vivo to chemical castration levels of ≤0.5 ng/ml. Stable, filter sterilizable, non-gelling solutions containing the GnRH antagonists at least at levels typically used in sustained release formulations also are disclosed, as is a method of increasing the solubility of GnRH antagonist in a polymer containing dispersed phase, which method comprises addition of an acid to the dispersed phase.

5. 发明公开

EP2462923A3 Prevention of molecular weight reduction of the polymer, impurity formation and gelling in polymer compositions 审中-公开
标题翻译：防止分子量的聚合物组合物中的减少，杂质的形成和凝胶形成
公开(公告)号：EP2462923A3
公开(公告)日：2012-08-29
申请号：EP11009427.3
申请日：2004-07-19
申请人： Oakwood Laboratories L.L.C.
发明人： Thanoo, Bagavathikanun. C. , Murtagh, James , Johns, Gonto
IPC分类号： A61K9/10 , A61K47/34 , A61K9/16 , A61K9/00
CPC分类号： A61K47/34 , A61K9/0019 , A61K9/1617 , A61K9/1647 , A61K38/08 , A61K38/09
摘要： Polymer and drug containing compositions and method of preparing such compositions are disclosed. The dispersed phase formulation has a polymer, a pharmaceutically or biologically active agent and a small fraction of low pKa acid additive. Stable, filter sterilizable, non-gelling solutions containing GnRH analogues at least at levels typically used in sustained release formulations and a method of increasing solubility of a high level of a GnRH analogue or a freeze-dried antagonist of GnRH in a polymer containing solution are also disclosed. The amount of the acid additive in the polymer solution is such that it is sufficient to increase the solubility of the high level of the GnRH analogue in the polymer solution without affecting the release characteristics of the microspheres prepared therefrom.
摘要翻译：聚合物和含药的组合物及其制备寻求成分的方法是游离缺失盘。分散相制剂具有聚合物，药学上或生物活性剂和低pKa酸添加剂的一小部分。稳定，过滤器灭菌，非凝胶溶液含有至少在持续释放制剂和灰典型使用水平GnRH类似物和增加高电平的GnRH类似物或GnRH的在聚合物含溶液冷冻干燥拮抗剂的溶解度的方法是所以游离缺失盘。在聚合物溶液中的酸添加剂的检查量这样做是足以增加高电平在聚合物溶液中的GnRH类似物的溶解性，而不会影响由其制备的微球的释放特征。

6. 发明公开

EP1962586A2 SUBLIMABLE SUSTAINED RELEASE DELIVERY SYSTEM AND METHOD OF MAKING SAME 有权
标题翻译：升华供应系统用于生产延迟释放和方法
公开(公告)号：EP1962586A2
公开(公告)日：2008-09-03
申请号：EP06846772.9
申请日：2006-12-22
申请人： Oakwood Laboratories L.L.C.
发明人： MASKIEWICZ, Richard
IPC分类号： A01N25/00 , A61K9/50 , A61M31/00 , A23J7/00
CPC分类号： A61K9/0024 , A61K9/1617 , Y10S514/957
摘要： The invention relates to compositions suitable for the delivery and/or stabilization of biologically active substances. The compositions comprise a sublimable matrix material and the biologically active agent to be delivered. The compositions can be used as drug delivery systems to treat a wide variety of diseases or as systems for the protection and stabilization of such substances. Also disclosed are methods for preparing compositions of the present invention.

7. 发明授权

EP1778278B1 GONADOTROPIN RELEASING HORMONE ANTAGONISTS 有权
标题翻译：促性腺激素释放激素拮抗剂
公开(公告)号：EP1778278B1
公开(公告)日：2014-05-21
申请号：EP05773048.3
申请日：2005-07-18
申请人： Oakwood Laboratories L.L.C.
发明人： MURTAGH, James Ph.D. , THANOO, Bagavathikanun, C.
IPC分类号： A61K38/24 , A61K9/14 , C07K17/00
CPC分类号： A61K9/0019 , A61K9/5031 , A61K38/00 , C07K7/23

8. 发明授权

EP0994695B1 CONTINUOUS MICROSPHERE PRODUCTION METHOD 失效
标题翻译：方法微球的一致制造
公开(公告)号：EP0994695B1
公开(公告)日：2013-04-03
申请号：EP98906435.7
申请日：1998-02-11
申请人： Oakwood Laboratories L.L.C.
发明人： THANOO, Bagavathikanun, Chithambara , MURTAGH, James
IPC分类号： A61K9/14 , A61K9/16
CPC分类号： B01J13/02 , A61K9/1647 , A61K9/1694

9. 发明授权

EP1962586B1 SUBLIMABLE SUSTAINED RELEASE DELIVERY SYSTEM AND METHOD OF MAKING SAME 有权
标题翻译：可升级的持续释放递送系统及其制造方法
公开(公告)号：EP1962586B1
公开(公告)日：2017-07-12
申请号：EP06846772.9
申请日：2006-12-22
申请人： Oakwood Laboratories L.L.C.
发明人： MASKIEWICZ, Richard
IPC分类号： A01N25/00 , A61K9/50 , A61M31/00 , A23J7/00
CPC分类号： A61K9/0024 , A61K9/1617 , Y10S514/957

10. 发明公开

EP2462923A2 Prevention of molecular weight reduction of the polymer, impurity formation and gelling in polymer compositions 审中-公开
标题翻译：防止分子量的聚合物组合物中的减少，杂质的形成和凝胶形成
公开(公告)号：EP2462923A2
公开(公告)日：2012-06-13
申请号：EP11009427.3
申请日：2004-07-19
申请人： Oakwood Laboratories L.L.C.
发明人： Thanoo, Bagavathikanun. C. , Murtagh, James , Johns, Gonto
IPC分类号： A61K9/10 , A61K47/34
CPC分类号： A61K47/34 , A61K9/0019 , A61K9/1617 , A61K9/1647 , A61K38/08 , A61K38/09
摘要： Polymer and drug containing compositions and method of preparing such compositions are disclosed. The dispersed phase formulation has a polymer, a pharmaceutically or biologically active agent and a small fraction of low pKa acid additive. Stable, filter sterilizable, non-gelling solutions containing GnRH analogues at least at levels typically used in sustained release formulations and a method of increasing solubility of a high level of a GnRH analogue or a freeze-dried antagonist of GnRH in a polymer containing solution are also disclosed. The amount of the acid additive in the polymer solution is such that it is sufficient to increase the solubility of the high level of the GnRH analogue in the polymer solution without affecting the release characteristics of the microspheres prepared therefrom.

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