Inotek Pharmaceuticals Corporation

Sunovion Pharmaceuticals Inc.

Sepracor, Inc.

William K McVicar

Norman N Kim

H Scott Wilkinson

Paul Mcglynn

Prakash Jagtap

Thomas Mccauley

Craig R Abolin

Rudolf A Baumgartner

Harun Takruri

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 Areceptor 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. 

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

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.

Ophthalmic formulations

The compound of formula (I) is a water-stable, long acting &#x3b2;-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like. Processes for making the compound of formula (I), as well as related intermediates, are disclosed.

Acetamide stereoisomer

The present invention is directed to a composition or a kit comprising a combination of a prostaglandin analog and an adenosine receptor Aagonist and to a method of reducing intraocular pressure (IOP) in a subject using such combination or kit. In some embodiments, the adenosine receptor Aagonist is Compound A, ((2R,3S,4R,5R)-5-(6 -(cyclopentylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl nitrate, having the structure, 

Combination, kit and method of reducing intraocular pressure

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).

Method of reducing intraocular pressure in humans

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 Areceptor 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. 

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

The present invention is directed to a combination or a kit comprising a prostaglandin analog and an adenosine receptor Aagonist and to a method of reducing intraocular pressure (IOP) in a subject using such combination or kit. In one embodiment, the prostaglandin analog is latanoprost and the adenosine receptor Aagonist is Compound A, ((2R,3S,4R,5R)-5-(6-(cyclopentylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl nitrate, having the structure, 

The compound of formula (I) is a water-stable, long acting &#x3b2;-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like.

Provided herein is a pharmaceutical composition or a kit comprising a combination of a non-selective beta-adrenergic receptor blocker and an adenosine Areceptor agonist. Also provided herein is a method of reducing intraocular pressure (IOP) in a subject using such a combination or kit. In a particular embodiment, provided herein is a combination of timolol marketed under the brand Timoptic&#x2122; and Compound A.

Combination compositions for reducing intraocular pressure

Provided herein is a pharmaceutical composition or a kit comprising a combination of a carbonic anhydrase inhibitor analog and an adenosine Areceptor agonist. Also provided herein is a method of reducing intraocular pressure (IOP) in a subject using such a combination or kit. In a particular embodiment, provided herein is a combination of dorzolamide marketed under the brand Trusopt&#x2122; and Compound A.

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Sudbury, MA, United States of America

William K McVicar