| Patent(s) and the Corresponding Patented Drug(s) |
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| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2015165342 |
| Title |
Isoquinolinesulfonamide Derivative, and Pharmaceutical Composition and Pharmaceutical Use Thereof. |
| Abstract |
The present invention discloses a class of isoquinolinesulfonamide derivatives as RHO kinase inhibitors, and pharmaceutical compositions thereof, and relates to pharmaceutically acceptable uses thereo. |
| Applicant(s) |
Medshine Discovery Inc |
| Representative Drug(s) |
D0N0YE |
Drug Info
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N.A. |
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[1] |
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2
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D0OS9O
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Drug Info
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N.A.
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[1] |
| Patent ID |
WO2015165341 |
| Title |
Isoquinolinesulfonyl Derivative As Rho Kinase Inhibitor. |
| Abstract |
The present invention discloses a class of isoquinolinesulfonyl derivatives as RHO kinase inhibitors, and pharmaceutical compositions thereof, and relates to pharmaceutically acceptable uses thereof. |
| Applicant(s) |
Medshine Discovery Inc |
| Representative Drug(s) |
D0FX7I |
Drug Info
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N.A. |
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[1] |
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2
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D0P6GJ
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Drug Info
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N.A.
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[1] |
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3
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D0VX0H
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Drug Info
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N.A.
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[1] |
| Patent ID |
WO2014068035 |
| Title |
Novel Rock Inhibitors. |
| Abstract |
The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases. Compounds of the invention display soft drug characteristics, i.e. they are rapidly inactivated upon entry in the systemic circulation. Therefore, they allow for reduced systemic exposure to functionally active ROCK inhibitors. |
| Applicant(s) |
Amakem Nv |
| Representative Drug(s) |
D0IF5M |
Drug Info
|
N.A. |
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[1] |
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2
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D0QF4V
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Drug Info
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N.A.
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[1] |
| Patent ID |
WO2015124877 |
| Title |
Derivatives of 5-Benzylisoquinoline for The Treatment of Cardiovascular Diseases. |
| Abstract |
The invention relates to novel isoquinoline derivatives of formula (I), to the synthesis thereof, and to the use of same in the prevention and/or treatment of pathologies resulting from the activation of the RhoA/ROCK pathway and the phosphorylation of the light chain of myosin. X represents a group -C(=0)-, -CH(OH)- or -CH2-, and the other substituents represent various groups such as those defined in claim 1. |
| Applicant(s) |
Les Laboratoires Servier |
| Patent ID |
WO2014177699 |
| Title |
Rhoa (Rock) Inhibitors for The Treatment of Enflammatory Bowel Disease. |
| Abstract |
The inventors now identified that TTC7A deficiency is a novel cause of IBD. It results from inappropriate activation of the RhoA signaling pathway, and thus inhibition of said pathway represents a novel therapeutic strategy for the treatment of IBD. Accordingly, the present invention relates to a RhoA kinase (ROCK) inhibitor for use in the treatment of an inflammatory bowel disease in a subject in need thereof. |
| Applicant(s) |
Inserm Inst Nat De La Sant et De La Rech M Dicale |
| Patent ID |
WO2014118133 |
| Title |
Pyridine Derivatives As Soft Rock Inhibitors. |
| Abstract |
The present invention relates to new kinase inhibitors of Formula (I) or a stereoisomer, tautomer, racemic, salt, hydrate, or solvate thereof, and more specifically to ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including Respiratory and Gastro-lntestinal diseases. |
| Applicant(s) |
Amakem Nv |
| Patent ID |
WO2014113620 |
| Title |
Phthalazinones and Isoquinolinones As Rock Inhibitors. |
| Abstract |
The present invention provides compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same. |
| Applicant(s) |
Bristol-Myers Squibb Company |
| Patent ID |
WO2013135596 |
| Title |
Rho Kinase Inhibitors for Use In Treating Amyotrophic Lateral Sclerosis. |
| Abstract |
The invention relates to a new use of a known Rho kinase inhibitor, fasudil or a fasudil derivative selected from hydroy-fasudil or dimethylfasudil, in the treatment of amyotrophic lateral sclerosis (ALS). |
| Applicant(s) |
Georg August Uni Goettingen Stiftung Oeffent Lichen Rechts Universitaet Semedizin |
| Patent ID |
WO2012146724 |
| Title |
Novel Rock Inhibitors. |
| Abstract |
The present invention relates to new kinase inhibitors of Formula (I), wherein X is oxygen, -NH-, or a direct bond; Y is -NH- or a direct bond; n is an integer from 0 to 4; m is an integer from 0 to 4; Cy represents a bivalent radical consisting of a satured (poly)cycle, including fused, bi-, spiro or bridged carbocycles and heterocycles; in particular selected from the group consisting of:Formula (II), Ar is selected from the group comprising: Formula (III), R2 is hydrogen or methyl; R8 is hydrogen, methyl, halogen, or alkynyl; R1 is an aryl or heteroaryl more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases. |
| Applicant(s) |
Amakem Nv |
| Patent ID |
WO2012135697 |
| Title |
Novel Rho Kinase Inhibitors and Methods of Use. |
| Abstract |
The subject invention concerns materials and methods for treating diseases and disorders associated with expression of Rho associated kinases (ROCKs). Examples of diseases and disorders contemplated within the scope of the invention include, but are not limited to, oncological disorders, cardiovascular diseases, CNS disorders, and inflammatory disorders. In one embodiment, a method of the invention comprises administering a therapeutically effective amount of one or more compounds of the present invention, or a composition comprising the compounds, to a person or animal in need of treatment. The subject invention also concerns compounds that inhibit ROCKs, and compositions that comprise the inhibitor compounds of the invention. Compounds contemplated within the scope of the invention include, but are not limited to, those compounds shown in Table (5). |
| Applicant(s) |
H. Lee Moffitt Cancer Center and Research Institute |
| Patent ID |
WO2012067965 |
| Title |
Nampt and Rock Inhibitors. |
| Abstract |
Disclosed are compounds of formula (1c) which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. Disclosed are compounds which inhibit the activity of ROCK, compositions containing the compounds and methods of treating diseases during which ROCK is expressed. |
| Applicant(s) |
Abbvie Inc |
| Patent ID |
WO2012015760 |
| Title |
Method for Treating Ophthalmic Diseases Using Kinase Inhibitor Compounds In Prodrug forms. |
| Abstract |
This invention is directed to prodrugs of rho kinase (ROCK) inhibitors. These prodrugs are in general the ester or the amide derivatives of the parent compounds. These prodrugs are often weak inhibitors of ROCK, but their parent compounds have good activities. Upon instillation into the eyes, the ester or the amide group of these prodrugs is rapidly hydrolyzed into alcohol, amine, or acid, and the prodrugs are converted into the active base compounds. The prodrugs of ROCK inhibitors provide several advantages such as delivery of higher concentrations of the active species into the target site and reduction of ocular discomfort. The invention is also directed to a method of treating ophthalmic diseases such as glaucoma, allergic conjunctivitis, macular edema, macular degeneration, and blepharitis, by administering an effective amount of a ROCK prodrug compound of Formula (I) to the eyes of the patient in need of. |
| Applicant(s) |
Inspire Pharmaceuticals, Inc |
| Patent ID |
WO2012012282 |
| Title |
Bifunctional Rho Kinase Inhibitor Compounds, Composition and Use. |
| Abstract |
This invention relates to synthetic bifunctional compounds comprising a first rho-associated kinase (ROCK) inhibiting compound and a second pharmaceutically active compound with complementary activity; the first and the second compounds are covalently linked by a biologically labile bond. This invention also relates to methods of making such compounds. The invention also relates to methods of using such bifunctional compounds in the prevention or treatment of diseases or conditions that are affected or can be assisted by altering the integrity or rearrangement of the cytoskeleton. Particularly, this invention relates to methods of treating ophthalmic diseases such as disorders in which intraocular pressure is elevated, for example primary open-angle glaucoma, using the bifunctional compounds. |
| Applicant(s) |
Inspire Pharmaceuticals, Inc |
| Patent ID |
WO2011130740 |
| Title |
Pyridylthiazole-Based Ureas As Inhibitors of Rho Associated Protein Kinase (Rock) and Methods of Use. |
| Abstract |
Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed. |
| Applicant(s) |
H. Lee Moffitt Cancer Center and Research Institute |
| Patent ID |
WO2011107608 |
| Title |
Heterocyclic Amides As Rock Inhibitors. |
| Abstract |
The present invention relates to new kinase inhibitors of formula (I), more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases. |
| Applicant(s) |
Amakem Nv |
| Patent ID |
WO2009155209 |
| Title |
Ophthalmic formulation of Rho Kinase Inhibitor Compound. |
| Abstract |
The present invention relates to an aqueous pharmaceutical formulation comprising at least one inhibitor of Rho-associated protein kinase (ROCK). The aqueous pharmaceutical formulation comprises 0.01-0.4% w/v of ROCK inhibitor(s), a non-ionic surfactant in an amount of 0.01-2% w/v, and a tonicity agent to maintain a tonicity between 220-360 mOsm/kG, at a pH between 6.3 to 7.8, wherein the ROCK inhibitor, the surfactant, and the tonicity agent are compatible in the formulation. The aqueous ophthalmic formulations of this invention have an increased ocular bioavailability and/or aqueous humor concentrations without a concomitant increase in systemic concentrations. The present invention further provides a method of reducing intraocular pressure, particularly a method of treating glaucoma, by administering the aqueous pharmaceutical formulation to a subject. |
| Applicant(s) |
Inspire Pharmaceuticals, Inc |
| Patent ID |
WO2008077057 |
| Title |
Cytoskeletal Active Rho Kinase Inhibitor Compounds, Composition and Use. |
| Abstract |
The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions. |
| Applicant(s) |
Inspire Pharmaceuticals, Inc |
| Patent ID |
WO2004106325 |
| Title |
Prodrugs of 1-(1-Hydroxy-5-Isoquinolinesulfonyl)Homopiperazine. |
| Abstract |
The present invention provides for novel prodrugs of 1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazine of the following Formula (I) wherein R1 is as defined herein. |
| Applicant(s) |
Schering Aktiengesellschaft |
| United States Patent and Trademark Office (USPTO) |
| Patent ID |
US20160213664 |
| Title |
Treatment of Cerebral Cavernous Malformations and Cerebral Aneurysms with Rho Kinase Inhibitors. |
| China National Intellectual Property Administration (CNIPA) |
| Patent ID |
CN104803914 |
| Title |
Hexahydro-Azepine Oxy-Benzamide Compounds Serving As Rho Kinase Inhibitor. |
| Representative Drug(s) |
D05OEZ |
Drug Info
|
IC50 < 1000 nM |
[1] |
