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1. 发明授权

US06300452B1 Block copolymers and preparation thereof 有权
标题翻译：嵌段共聚物及其制备方法
公开(公告)号：US06300452B1
公开(公告)日：2001-10-09
申请号：US09442403
申请日：1999-11-18
申请人： Harri Jukarainen , Jarkko Ruohonen , Matti Lehtinen , Juha Ala-Sorvari , Jukka Seppälä
发明人： Harri Jukarainen , Jarkko Ruohonen , Matti Lehtinen , Juha Ala-Sorvari , Jukka Seppälä
IPC分类号： C08G7746
CPC分类号： C08G77/46 , C08F290/062 , C08F290/068
摘要： The invention relates to a new polysiloxane-based block copolymer having a formula T(AB)xAT (I) wherein A=—(SiR′R″O)nSiR′R″—, wherein R′ and R″ are the the same or different and represent a lower alkyl group or a phenyl group, wherein said alkyl or phenyl group may be substituted or unsubstituted; B is polyalkylene oxide of formula wherein R is hydrogen, lower alkyl, or phenyl; R1 is hydrogen or lower alkyl; y is 2-6; m is 1-30; n is 1-3000; and x is 0-100.
摘要翻译：本发明涉及一种新的聚硅氧烷基嵌段共聚物，其具有式（A） - （SiR'R''O）nSiR'R“ - ，其中R'和R”相同或不同，表示低级烷基或苯基，其中所述烷基或苯基可以是取代的或未取代的; B是式（Ⅳ）的聚环氧烷，R是氢，低级烷基或苯基; R 1是氢或低级烷基; y为2-6; m为1-30; n为1-3000; x为0-100。

2. 发明授权

US06794464B2 Membrane or matrix for controlling the permeation rate of drugs 有权
标题翻译：用于控制药物渗透速率的膜或基质
公开(公告)号：US06794464B2
公开(公告)日：2004-09-21
申请号：US10298195
申请日：2002-11-18
申请人： Harri Jukarainen , Tommi Markkula , Juha Ala-Sorvari , Matti Lehtinen , Jarkko Ruohonen
发明人： Harri Jukarainen , Tommi Markkula , Juha Ala-Sorvari , Matti Lehtinen , Jarkko Ruohonen
IPC分类号： C08L8310
CPC分类号： C08L83/12 , A61K9/0024 , A61K9/0036 , A61K9/0039 , A61K9/2027 , A61K9/2031
摘要： A membrane or matrix for controlling the permeation rate of a drug, where the membrane or matrix includes a siloxane-based elastomer composition which contains at least one elastomer and optionally a non-crosslinked polymer. The elastomer composition includes poly(alkylene oxide) groups, and the poly(alkylene oxide) groups are present as blocks in a chain of the elastomer or the polymer, or as blocks and alkoxy-terminated grafts of polysiloxane units, the blocks or blocks and grafts being linked to the polysiloxane units by silicon-carbon bonds, with at least three blocks being present in the elastomer or polymer chain. Methods for the preparation of the elastomer composition are also disclosed.
摘要翻译：用于控制药物渗透速率的膜或基质，其中膜或基质包括含有至少一种弹性体和任选的非交联聚合物的硅氧烷基弹性体组合物。弹性体组合物包括聚（环氧烷）基团，聚（环氧烷）基团作为嵌段存在于弹性体或聚合物的链中，或作为聚硅氧烷单元的嵌段和烷氧基封端的接枝物，嵌段或嵌段接枝物通过硅 - 碳键与聚硅氧烷单元连接，至少有三个嵌段存在于弹性体或聚合物链中。还公开了制备弹性体组合物的方法。

3. 发明授权

US6117442A Drug delivery device, especially for the delivery of androgens 有权
标题翻译：药物输送装置，特别是用于输送雄激素
公开(公告)号：US6117442A
公开(公告)日：2000-09-12
申请号：US190607
申请日：1998-11-12
申请人： Tommi Markkula , Juha Ala-Sorvari , Harri Jukarainen , Matti Lehtinen , Jarkko Ruohonen
发明人： Tommi Markkula , Juha Ala-Sorvari , Harri Jukarainen , Matti Lehtinen , Jarkko Ruohonen
IPC分类号： A61K9/52 , A61K9/00 , A61K31/565 , A61K31/568 , A61K47/34 , A61P15/16 , A61P15/18 , A61F13/00
CPC分类号： A61K9/0024
摘要： The invention relates to a delivery device for the controlled release of a therapeutically active agent, especially an androgen, over a prolonged period of time, said device including a core containing the therapeutically active agent, and a membrane encasing the core wherein the membrane is made of an elastomer. According to the invention, the elastomer is a siloxane-based elastomer which includes 3,3,3-trifluoropropyl groups attached to the Si-atoms of the siloxane units.
摘要翻译：本发明涉及用于在更长时间内控制释放治疗活性剂，特别是雄激素的递送装置，所述装置包括含有治疗活性剂的核心和包围核心的膜，其中制成膜的弹性体。根据本发明，弹性体是包含连接到硅氧烷单元的Si原子上的3,3,3-三氟丙基的硅氧烷类弹性体。

4. 发明授权

US06476079B1 Devices for the delivery of drugs having antiprogestinic properties 有权
标题翻译：用于输送具有抗过药性质的药物的装置
公开(公告)号：US06476079B1
公开(公告)日：2002-11-05
申请号：US09472126
申请日：1999-12-23
申请人： Harri Jukarainen , Tommi Markkula , Juha Ala-sorvari , Matti Lehtinen , Jarkko Ruohonen
发明人： Harri Jukarainen , Tommi Markkula , Juha Ala-sorvari , Matti Lehtinen , Jarkko Ruohonen
IPC分类号： A16K4732
CPC分类号： A61K9/0024 , A61K9/0039 , A61K31/122 , A61K31/277 , A61K31/4418 , A61K31/50 , A61K31/502 , A61K31/565 , A61K31/569 , A61K31/575 , A61K31/58 , C08G77/18 , C08G77/44 , C08G77/46 , C08G77/50 , C08G77/70 , C08L83/04 , C08L83/12 , Y10S514/843 , C08L2666/14
摘要： A device for the controlled release over a prolonged period of time of a drug having antiprogestinic properties, the device including a core containing the drug, optionally a membrane encasing the core, where at least one of the core and membrane, when present, is made of a siloxane-based elastomer composition including at least one elastomer and optionally a non-crosslinked polymer. The device is characterized in that the elastomer composition includes poly(alkylene oxide) groups and that the poly(alkylene oxide) groups are present in the elastomer or polymer as alkoxy-terminated grafts of polysiloxane units, or as blocks, the grafts or blocks being linked to the polysiloxane units by silicon-carbon bonds, or as a mixture of these forms.
摘要翻译：一种用于具有抗过药性质的药物在长时间内控制释放的装置，该装置包括含有该药物的核心，任选地包含核心的膜，其中存在核心和膜中的至少一个的包含至少一种弹性体和任选的非交联聚合物的硅氧烷基弹性体组合物。该装置的特征在于，弹性体组合物包括聚（环氧烷）基团，并且聚（环氧烷）基团作为烷氧基封端的聚硅氧烷单元的接枝物存在于弹性体或聚合物中，或作为嵌段，所述接枝物或嵌段是通过硅 - 碳键与聚硅氧烷单元连接，或作为这些形式的混合物。

5. 发明授权

US06299894B1 Drug delivery device, especially for the delivery of gestodene 有权
标题翻译：药物输送装置，特别是用于递送吉司他丁
公开(公告)号：US06299894B1
公开(公告)日：2001-10-09
申请号：US09568027
申请日：2000-05-10
申请人： Tommi Markkula , Juha Ala-Sorvari , Harri Jukarainen , Matti Lehtinen , Jarkko Ruohonen
发明人： Tommi Markkula , Juha Ala-Sorvari , Harri Jukarainen , Matti Lehtinen , Jarkko Ruohonen
IPC分类号： A61F1300
CPC分类号： A61K9/0039
摘要： The invention relates to a delivery device for the controlled release of the therapeutically active agent gestodene, over a prolonged period of time, at a release rate of 0,1-300 &mgr;g/day, said device comprising a core comprising at least said therapeutically active agent, and a membrane encasing said core wherein said membrane is made of an elastomer. According to the invention, the elastomer is a siloxane-based elastomer comprising 3,3,3-trifluoropropyl groups attached to the Si-atoms of the siloxane units, and the release rate of said therapeutically active agent of said delivery device is regulated by the amount of said 3,3,3-trifluoropropyl groups.
摘要翻译：本发明涉及一种递送装置，用于在更长的时间内以0.01至300杯/天的释放速率控制释放治疗活性剂甘露聚糖，所述装置包含至少包含所述治疗活性物质的核心试剂和包封所述芯的膜，其中所述膜由弹性体制成。根据本发明，弹性体是包含连接到硅氧烷单元的Si原子上的3,3,3-三氟丙基的硅氧烷基弹性体，并且所述递送装置的所述治疗活性剂的释放速率由所述3,3,3-三氟丙基的量。

6. 发明授权

US06887948B2 Method for preparing a siloxane-based elastomer composition 有权
标题翻译：硅氧烷类弹性体组合物的制造方法
公开(公告)号：US06887948B2
公开(公告)日：2005-05-03
申请号：US10298197
申请日：2002-11-18
申请人： Harri Jukarainen , Tommi Markkula , Juha Ala-Sorvari , Pirkko Lehtinen , Jarkko Ruohonen
发明人： Matti Lehtinen
IPC分类号： A61K9/00 , A61K9/20 , C08L83/12 , C08L83/10
CPC分类号： A61K9/2027 , A61K9/0024 , A61K9/0036 , A61K9/0039 , A61K9/2031 , C08L83/12
摘要： The invention relates to a method for the preparation of a siloxane-based elastomer composition comprising at least one elastomer, said elastomer composition comprising poly(alkylene oxide) groups present in the elastomer as alkoxy-terminated grafts of polysiloxane units and linked to the polysiloxane units by silicon-carbon bonds wherein at least one vinyl functional polymer component is crosslinked in the presence of a peroxide catalyst.
摘要翻译：本发明涉及一种制备包含至少一种弹性体的硅氧烷基弹性体组合物的方法，所述弹性体组合物包含存在于弹性体中的聚（烯化氧）基团，作为聚硅氧烷单元的烷氧基封端的接枝物并与聚硅氧烷单元连接通过其中至少一种乙烯基官能聚合物组分在过氧化物催化剂存在下进行交联的硅 - 碳键。

7. 发明授权

US06056976A Elastomer, its preparation and use 有权
标题翻译：弹性体，其制备和使用
公开(公告)号：US06056976A
公开(公告)日：2000-05-02
申请号：US190608
申请日：1998-11-12
申请人： Tommi Markkula , Juha Ala-Sorvari , Harri Jukarainen , Matti Lehtinen , Jarkko Rughonen
发明人： Tommi Markkula , Juha Ala-Sorvari , Harri Jukarainen , Matti Lehtinen , Jarkko Rughonen
IPC分类号： A61L27/00 , A61K9/00 , A61K9/20 , A61K9/52 , A61K9/58 , C08G77/24 , C08J5/18 , C08K3/36 , C08K5/54 , C08L83/04 , C08L83/08 , A61K9/14
CPC分类号： A61K9/0039 , A61K9/009 , A61K9/2036
摘要： The invention relates to a siloxane-based elastomer intended for controlling the permeation of drugs, wherein the elastomer includes 3,3,3,-trifluoropropyl groups attached to the Si-atoms of the siloxane units.The invention relates also to a method for the preparation of a siloxane-based elastomer including 3,3,3,-trifluoropropyl substituents, where the elastomer is intended for controlling the permeation of drugs.In the method eitheri) a 3,3,3,-trifluoropropyl-substituted vinyl-functional polysiloxane component and a silicon hydride-functional crosslinking agent are crosslinked in the presence of a catalyst, orii) a 3,3,3,-trifluoropropyl-substituted polysiloxane component is crosslinked in the presence of a peroxide catalyst.
摘要翻译：本发明涉及一种旨在控制药物渗透性的硅氧烷基弹性体，其中弹性体包括连接到硅氧烷单元的Si原子上的3,3,3-三氟丙基。本发明还涉及制备包含3,3,3-三氟丙基取代基的硅氧烷基弹性体的方法，其中弹性体用于控制药物的渗透。在该方法中，i）3,3,3,3-三氟丙基取代的乙烯基官能聚硅氧烷组分和硅氢化物官能的交联剂在催化剂存在下进行交联，或ii）3,3,3，三氟丙基取代的聚硅氧烷组分在过氧化物催化剂存在下交联。

8. 发明授权

US6063395A Drug delivery device especially for the delivery of progestins and estrogens 有权
标题翻译：药物输送装置特别适用于输送孕激素和雌激素
公开(公告)号：US6063395A
公开(公告)日：2000-05-16
申请号：US190606
申请日：1998-11-12
申请人： Tommi Markkula , Juba Ala-Sorvari , Harri Jukarainen , Matti Lehtinen , Jarkko Ruohonen
发明人： Tommi Markkula , Juba Ala-Sorvari , Harri Jukarainen , Matti Lehtinen , Jarkko Ruohonen
IPC分类号： A61K9/32 , A61K9/00 , A61K31/565 , A61K31/57 , A61K45/00 , A61P15/18 , A61F13/00
CPC分类号： A61K9/0092 , A61K31/565 , A61K31/569 , A61K31/57 , A61K31/575 , A61K9/0039 , A61K9/0024 , A61K9/0036
摘要： The invention relates to a delivery device for the controlled release of a therapeutically active agent, especially a progestin or an estrogen, over a prolonged period of time, said device including a core which contains the therapeutically active agent, and a membrane encasing the core wherein said membrane is made of an elastomer. According to the invention, the elastomer is a siloxane-based elastomer which includes 3,3,3-trifluoropropyl groups attached to the Si-atoms of the siloxane units.
摘要翻译：本发明涉及用于在更长时间内控制释放治疗活性剂，特别是孕激素或雌激素的递送装置，所述装置包括含有治疗活性剂的核心和包裹核心的膜，其中所述膜由弹性体制成。根据本发明，弹性体是包含连接到硅氧烷单元的Si原子上的3,3,3-三氟丙基的硅氧烷类弹性体。

9. 发明授权

US07053077B1 Use of biogenic estrogen sulfamates for hormone replacement therapy 有权
标题翻译：使用生物源性雌激素氨基磺酸盐治疗激素替代疗法
公开(公告)号：US07053077B1
公开(公告)日：2006-05-30
申请号：US09744574
申请日：1999-05-13
申请人： Walter Elger , Pekka Lähteenmäki , Matti Lehtinen , Gudrun Reddersen , Holger Zimmermann , Michael Oettel , Sigfrid Schwarz
发明人： Walter Elger , Pekka Lähteenmäki , Matti Lehtinen , Gudrun Reddersen , Holger Zimmermann , Michael Oettel , Sigfrid Schwarz
IPC分类号： A61K31/56
CPC分类号： A61K31/566 , A61K31/565 , A61K31/57 , Y10S514/874 , A61K2300/00
摘要： The invention relates to the use of biogenic estrogen sulfamates for the oral discontinuous application for hormone replacement therapy (HRT). The discontinuous administration takes place in intervals ranging from 2 to 40 days. The invention also provides the additional application of gestagens, preferably continuously in the form of an implant or in the form of an intrauterine releasing system (IUD). Estrone sulfamate, estradiol sulfamate or an N-acyl sulfamate of estrone, estradiol or estriol having up to 7 C-atoms in the acyl chain, or a combination comprised of two or more of said active ingredients are used as biogenic estrogen sulfamates.
摘要翻译：本发明涉及用于激素替代治疗（HRT）的口服不连续应用的生物源性雌激素氨基磺酸盐的用途。不连续给药时间间隔为2至40天。本发明还提供了孕妇的额外应用，优选连续地以植入物的形式或以子宫内释放系统（IUD）的形式。氨基磺酸氨基磺酸酯，氨基磺酸雌二醇酯或酰基链中具有至多7个C原子的雌酮，雌二醇或雌三醇的N-酰基氨基磺酸酯或由两种或更多种所述活性成分组成的组合物用作生物来源的雌激素亚磺酸盐。

10. 发明授权

US5626148A Device for intrauterine use 失效
标题翻译：子宫内使用装置
公开(公告)号：US5626148A
公开(公告)日：1997-05-06
申请号：US167792
申请日：1994-02-22
申请人： Matti Lehtinen
发明人： Matti Lehtinen
IPC分类号： A61F6/14 , A61F6/06
CPC分类号： A61F6/14
摘要： Device for intrauterine use comprising means (7, 8) for attaching the device to the interior wall of the uterus, as well as a member (1) releasing active agent and connected to the said attachment means. The invention is characterized in that the active agent releasing member (1) is in the form of a closed container enclosing the active agent, the walls of the container being at least partly permeable to the active agent.
摘要翻译： PCT No.PCT / FI92 / 00189 Sec。 371日期：1994年2月22日 102（e）日期1994年2月22日PCT提交1992年6月17日PCT公布。第WO93 / 00055号公报日期1993年1月7日用于子宫内使用的装置包括用于将装置附接到子宫内壁的装置（7,8），以及释放活性剂并连接到所述附接装置的构件（1）。本发明的特征在于活性剂释放构件（1）为封闭容器的形式，其包围活性剂，容器的壁至少部分地可渗透活性剂。

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