公开(公告)号：US5735810A

公开(公告)日：1998-04-07

申请号：US708332

申请日：1996-09-04

申请人： Burton H. Sage, Jr. ,  Philip G. Green

发明人： Burton H. Sage, Jr. ,  Philip G. Green

IPC分类号： A61N1/30

CPC分类号： A61N1/30

摘要： The present invention relates to a method and device for the iontophoretic delivery of a therapeutic dose range of bisphosphonate to be delivered to a patient over a period of lime to prevent the onset for advancement of osteoporosis and other metabolic bone diseases for a selected period of time.

摘要翻译： 本发明涉及一种用于离子电渗传递治疗剂量范围的二膦酸盐的方法和装置，其在石灰期间递送至患者以防止在选定的时间段内促进骨质疏松症和其它代谢性骨疾病的发生 。

公开(公告)号：US5935598A

公开(公告)日：1999-08-10

申请号：US877602

申请日：1997-06-18

申请人： Burton H. Sage ,  Carl Randolph Bock ,  Philip G. Green

发明人： Burton H. Sage ,  Carl Randolph Bock ,  Philip G. Green

IPC分类号： A61K9/00 ,  A61K9/70 ,  A61K31/42 ,  A61K31/4439 ,  A61K31/4545 ,  A61N1/30

CPC分类号： A61K31/4545 ,  A61K31/42 ,  A61K31/4439 ,  A61K9/0009

摘要： This invention relates to novel methods and devices for iontophoretically administering therapeutic doses of cell adhesion receptor antagonists in a controlled manner through the skin. Such antagonist compounds include but are not limited to antagonists of the IIb/IIIa and .alpha..sub.v .beta..sub.3 inter and related cell surface adhesive protein receptors. The present invention includes iontophoretic delivery devices comprising cell adhesion receptor antagonists. Such methods and devices are useful, alone or in combination with other therapeutic agents, for the treatment of thromboembolic disorders, angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

摘要翻译： 本发明涉及以受控方式通过皮肤离子电渗施用治疗剂量的细胞粘附受体拮抗剂的新方法和装置。 这种拮抗剂化合物包括但不限于IIb / IIIa和αvβ3内相和相关细胞表面粘附蛋白受体的拮抗剂。 本发明包括包含细胞粘附受体拮抗剂的离子电渗疗法递送装置。 这些方法和装置单独或与其它治疗剂组合用于治疗血栓栓塞障碍，血管生成障碍，炎症，骨退化，癌转移，糖尿病性视网膜病变，再狭窄，黄斑变性和由细胞粘附介导的其它病症， /或细胞迁移和/或血管发生。

公开(公告)号：US06858018B1

公开(公告)日：2005-02-22

申请号：US09162301

申请日：1998-09-28

申请人： Philip G. Green ,  Ronald J. Pettis ,  Michelle R. Brosnan-Cook

发明人： Philip G. Green ,  Ronald J. Pettis ,  Michelle R. Brosnan-Cook

IPC分类号： A61K9/00 ,  A61K9/70 ,  A61K31/445 ,  A61K31/4468 ,  A61K47/32 ,  A61N1/30 ,  A61P23/00 ,  A61P25/04 ,  C07D211/58

CPC分类号： A61K9/0009 ,  A61N1/30

摘要： Iontophoretic devices for the delivery of N-phenyl-N-(4-piperidinyl)amide esters are provided. The N-phenyl-N-(4-piperidinyl)amide esters are compounds of the 1. A reservoir comprising a matrix material and, distributed in said matrix material, a pharmaceutically acceptable amount of at least one compound selected from compounds of the formula (I) wherein: X is a member selected from the group consisting of alkoxy-carbonyl-lower alkyl, lower alkyl-carbonyloxy-lower alkyl, alkenyloxy-carbonyl-lower alkyl, and (C1-2)alkoxy-(C1-2)alkoxy-carbonyl-lower alkyl; Ar is a member selected from the group consisting of phenyl, and mono-, di- and tri-substituted phenyl, wherein each substituent is independently selected from the group consisting of halo, lower alkyl, lower alkoxy and trifluoromethyl; R is a member selected from the group consisting of lower alkyl, and lower alkoxy-lower alkyl,; R1 is a member selected from the group consisting of hydrogen, lower alkoxy-carbonyl; and R2 is a member selected from the group consisting of hydrogen and methyl; and the optically active and cis-trans isomers thereof, and the acid addition salts, of said compounds and isomers.

摘要翻译： 提供用于递送N-苯基-N-（4-哌啶基）酰胺酯的离子电渗装置。 N-苯基-N-（4-哌啶基）酰胺酯是1.含有基质材料并且在所述基质材料中分布有药学上可接受量的至少一种选自以下化合物的化合物的储库的化合物（ I）其中：X是选自烷氧基 - 羰基 - 低级烷基，低级烷基 - 羰氧基 - 低级烷基，烯氧基 - 羰基 - 低级烷基和（C1-2）烷氧基 - （C1-2）烷氧基 - 羰基 - 低级烷基; Ar是选自苯基和单 - ，二 - 和三取代的苯基的成员，其中每个取代基独立地选自卤素，低级烷基，低级烷氧基和三氟甲基 ; R是选自低级烷基和低级烷氧基 - 低级烷基的成员; R 1是选自氢，低级烷氧基 - 羰基， 和R 2是选自氢和甲基的成员; 及其光学活性和顺式 - 反式异构体，以及所述化合物和异构体的酸加成盐。

公开(公告)号：US5682726A

公开(公告)日：1997-11-04

申请号：US730948

申请日：1996-10-16

申请人： Philip G. Green ,  Ronald J. Clark ,  Bernt Fredrik Julius Broberg

发明人： Philip G. Green ,  Ronald J. Clark ,  Bernt Fredrik Julius Broberg

IPC分类号： A61K9/00 ,  A61K9/70 ,  B65B29/00 ,  B65B31/02 ,  B65B55/00

CPC分类号： A61K9/7023 ,  A61K9/0009 ,  A61F2013/0296

摘要： A method for forming and packaging an iontophoretic patch in an inert atmosphere to provide increased shelf-life. The method includes a number of sub-assemblies for forming a well in a laminate material, forming the reservoir and dosing the reservoir, sealing the laminate material and another laminate material together to form a continuous web from which the individual patches are cut. In addition, the patch can be subsequently enclosed in an individual package. In this way, the patch and/or package provides a commercially suitable shelf-life to the drug-filled patch stored therein.

摘要翻译： 一种用于在惰性气氛中形成和包装离子电渗贴剂以提高保质期的方法。 该方法包括用于在层压材料中形成井的多个子组件，形成储存器并计量储存器，将层压材料和另一层压材料密封在一起以形成连续的腹板，各个贴片从该连续腹板切割。 此外，贴片可以随后封装在单个包装中。 以这种方式，贴片和/或包装为储存在其中的药物填充贴片提供商业上合适的保质期。

公开(公告)号：US5961483A

公开(公告)日：1999-10-05

申请号：US878493

申请日：1997-06-18

申请人： Burton H. Sage ,  Carl Randolph Bock ,  Philip G. Green ,  Munir A. Hussain ,  Arnold J. Repta

发明人： Burton H. Sage ,  Carl Randolph Bock ,  Philip G. Green ,  Munir A. Hussain ,  Arnold J. Repta

IPC分类号： A61K9/00 ,  A61K9/70 ,  A61K31/42 ,  A61K31/4439 ,  A61K31/4545 ,  A61N1/30

CPC分类号： A61K31/4545 ,  A61K31/42 ,  A61K31/4439 ,  A61K9/0009

摘要： This invention relates to novel methods and devices for iontophoretically administering therapeutic doses of cell adhesion receptor antagonists in a controlled manner through the skin. Such antagonist compounds include but are not limited to antagonists of the IIb/IIIa and .alpha..sub.v .beta..sub.3 integrins and related cell surface adhesive protein receptors. The present invention includes iontophoretic delivery devices comprising cell adhesion receptor antagonists. Such methods and devices are useful, alone or in combination with other therapeutic agents, for the treatment of thromboembolic disorders, angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

摘要翻译： 本发明涉及以受控方式通过皮肤离子电渗施用治疗剂量的细胞粘附受体拮抗剂的新方法和装置。 这种拮抗剂化合物包括但不限于IIb / IIIa和αvβ3整联蛋白和相关细胞表面粘附蛋白受体的拮抗剂。 本发明包括包含细胞粘附受体拮抗剂的离子电渗疗法递送装置。 这些方法和装置单独或与其它治疗剂组合用于治疗血栓栓塞障碍，血管生成障碍，炎症，骨退化，癌转移，糖尿病性视网膜病变，再狭窄，黄斑变性和由细胞粘附介导的其它病症， /或细胞迁移和/或血管发生。

公开(公告)号：US5730715A

公开(公告)日：1998-03-24

申请号：US665181

申请日：1996-06-14

申请人： Burton H. Sage, Jr. ,  Philip G. Green

发明人： Burton H. Sage, Jr. ,  Philip G. Green

IPC分类号： A61N1/30

CPC分类号： A61N1/30

摘要： A method for preventing the onset or advancement of osteoporosis or other metabolic bone disorders in a patient by iontophoretically administering to the patient an effective amount of a bisphosphonate which would be effective for preventing the onset or advancement of osteoporosis or other bone disorders and wherein the effective amount of bisphosphonate is delivered over a period of from about four (4) hours to about forty-eight (48) hours, at intervals of from about once a week to about twice a year and wherein the effective amount of bisphosphonate also contains an agent capable of chelating calcium.

摘要翻译： 一种通过对患者进行离子电渗治疗来预防骨质疏松症或其他代谢性骨骼疾病发作或进展的方法，该方法有效量地对于预防骨质疏松症或其他骨病发生或进展有效的双膦酸盐，并且其中有效 二膦酸盐的量在约四（4）小时至约四十八（48）小时的时间内以每周约一次至约两次的间隔递送，并且其中双膦酸盐的有效量还含有一种试剂 能螯合钙。