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![Anhydrous polymorphs of [(2R,3S,4R,5R)-5-(6-(cyclopentylamino)-9H-purin-9-YL)-3,4-dihydroxytetrahydrofuran-2-YL)] methyl nitrate and processes of preparation thereof](/abs-image/US/2017/08/01/US09718853B2/abs.jpg.150x150.jpg)
公开(公告)号：US09718853B2
公开(公告)日：2017-08-01
申请号：US15005697
申请日：2016-01-25
发明人： William K. McVicar
IPC分类号： A01N43/04 , A61K31/70 , C07H19/20 , C07H19/167 , C07H19/173 , C07H19/16 , C07H1/06
CPC分类号： C07H19/16 , C07H1/06 , C07H19/167
摘要： The present invention provides novel anhydrous polymorph forms of [(2R,3S,4R,5R)-5-(6-(cyclopentylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)]methyl nitrate (compound A), a selective adenosine A1 receptor agonist with a number of therapeutic uses including the treatment of elevated intra-ocular pressure. Also provided are methods for the preparation of the anhydrous polymorphic forms of compound A, pharmaceutical compositions and methods of treatment.
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公开(公告)号：US09289383B2
公开(公告)日：2016-03-22
申请号：US14552160
申请日：2014-11-24
IPC分类号： A61K31/70 , A61K9/00 , A61K31/495 , A61K31/7076 , C07H19/167 , A61K45/06 , C07H19/16
CPC分类号： A61K31/7076 , A61K9/0048 , A61K31/495 , A61K45/06 , C07H19/16 , C07H19/167
摘要： Provided herein is a method of reducing intraocular pressure (IOP) in humans using N6-cyclopentyladenosine (CPA), CPA derivatives or prodrugs or enhanced cornea permeability formulations of CPA. In one embodiment, the invention is directed to CPA derivatives or prodrugs that are permeable to the cornea. In another embodiment, the invention is directed to uses of certain compounds in human subjects for reducing and/or controlling elevated or abnormally fluctuating IOPs in the treatment of glaucoma or ocular hypertension (OHT).
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公开(公告)号：US09370530B2
公开(公告)日：2016-06-21
申请号：US14517509
申请日：2014-10-17
IPC分类号： A61K31/70 , A61K31/7076 , A61K9/00 , A61K31/165 , A61K31/19 , A61K31/216 , A61K45/06 , C07H19/16
CPC分类号： A61K31/7076 , A61K9/0048 , A61K31/165 , A61K31/19 , A61K31/216 , A61K31/5575 , A61K45/06 , C07H19/16 , A61K2300/00
摘要： The present invention is directed to a composition or a kit comprising a combination of a prostaglandin analog and an adenosine receptor A1 agonist and to a method of reducing intraocular pressure (IOP) in a subject using such combination or kit. In some embodiments, the adenosine receptor A1 agonist is Compound A, ((2R,3S,4R,5R)-5-(6 -(cyclopentylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl nitrate, having the structure,
摘要翻译： 本发明涉及包含前列腺素类似物和腺苷受体A1激动剂的组合的组合物或试剂盒，以及使用这种组合或试剂盒降低受试者的眼内压（IOP）的方法。 在一些实施方案中，腺苷受体A1激动剂是化合物A，（（2R，3S，4R，5R）-5-（6-（环戊基氨基）-9H-嘌呤-9-基）-3,4-二羟基四氢呋喃-2-基 吡啶基）甲基硝酸盐，具有结构，
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公开(公告)号：US08895530B2
公开(公告)日：2014-11-25
申请号：US13909288
申请日：2013-06-04
IPC分类号： A61K31/70 , C07H19/167 , A61K31/7076 , A61K31/495
CPC分类号： A61K31/7076 , A61K9/0048 , A61K31/495 , A61K45/06 , C07H19/16 , C07H19/167
摘要： Provided herein is a method of reducing intraocular pressure (IOP) in humans using N6-cyclopentyladenosine (CPA), CPA derivatives or prodrugs or enhanced cornea permeability formulations of CPA. In one embodiment, the invention is directed to CPA derivatives or prodrugs that are permeable to the cornea. In another embodiment, the invention is directed to uses of certain compounds in human subjects for reducing and/or controlling elevated or abnormally fluctuating IOPs in the treatment of glaucoma or ocular hypertension (OHT).
摘要翻译： 本文提供了使用N6-环戊基腺苷（CPA），CPA衍生物或前药或CPA增强的角膜通透性制剂降低人眼内压（IOP）的方法。 在一个实施方案中，本发明涉及可透过角膜的CPA衍生物或前药。 在另一个实施方案中，本发明涉及某些化合物在人受试者中用于减少和/或控制治疗青光眼或高眼压症（OHT）的升高或异常波动的IOP的用途。
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公开(公告)号：US09522160B2
公开(公告)日：2016-12-20
申请号：US14211516
申请日：2014-03-14
发明人： William K. McVicar , Harun Takruri
IPC分类号： A61K31/7076 , A61K31/14 , A61K9/10 , A61K45/06 , A61K9/00 , A61K31/5575 , A61K47/38
CPC分类号： A61K31/7076 , A61K9/0048 , A61K9/10 , A61K31/14 , A61K31/5575 , A61K45/06 , A61K47/02 , A61K47/26 , A61K47/38 , A61K2300/00
摘要： The present invention relates to an ophthalmic formulation which comprises a fine particle of Compound A in an aqueous suspension and a manufacturing process thereof. More specifically, the present invention relates to a topically applied ophthalmic aqueous suspension which is obtainable by suspending fine particles of Compound A in an aqueous vehicle containing a surfactant and boric acid. The invention also provides processes for making the ophthalmic formulations and to methods of use thereof.
摘要翻译： 本发明涉及在水性悬浮液中含有化合物A的细颗粒的眼用制剂及其制造方法。 更具体地说，本发明涉及一种局部施用的眼用水性悬浮液，其通过将化合物A的细颗粒悬浮在含有表面活性剂和硼酸的水性载体中而获得。 本发明还提供了制备眼用制剂的方法及其使用方法。
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6.发明授权Anhydrous polymorphs of [(2R,3S,4R,5R)-5-(6-(cyclopentylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)} methyl nitrate and processes of preparation thereof 有权[（2R，3S，4R，5R）-5-（6-（环戊基氨基）-9H-嘌呤-9-基）-3,4-二羟基四氢呋喃-2-基）}甲基硝酸酯的无水多晶型物及其制备方法公开(公告)号：US09278991B2
公开(公告)日：2016-03-08
申请号：US13750389
申请日：2013-01-25
发明人： William K. McVicar
IPC分类号： A01N43/04 , A61K31/70 , C07H19/167 , C07H19/173 , C07H19/16 , C07H1/06
CPC分类号： C07H19/16 , C07H1/06 , C07H19/167
摘要： The present invention provides novel anhydrous polymorph forms of 2R,3S,4R,5R)-5-(6-(cyclopentylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl) methyl nitrate (Compound A), a selective adenosine A1 receptor agonist with a number of therapeutic uses including the treatment of elevated intra-ocular pressure. Also provided are methods for the preparation of the anhydrous polymorphic forms of compound A, pharmaceutical compositions and methods of treatment.
摘要翻译： 本发明提供2R，3S，4R，5R）-5-（6-（环戊基氨基）-9H-嘌呤-9-基）-3,4-二羟基四氢呋喃-2-基）甲基硝酸酯（化合物 A），具有许多治疗用途的选择性腺苷A1受体激动剂，包括治疗眼内压升高。 还提供了制备化合物A的无水多晶型物的方法，药物组合物和治疗方法。
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