Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T06093 Target Info
Target Name Rho-associated protein kinase 2 (ROCK2)
Synonyms p164 ROCK-2; Rho-associated, coiled-coil-containing protein kinase II; Rho-associated, coiled-coil-containing protein kinase 2; Rho kinase 2; ROCK-II; KIAA0619
Target Type Successful Target
Gene Name ROCK2
Biochemical Class Kinase
UniProt ID
ROCK2_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015002926
Title Tricyclic Pyrido-Carboxamide Derivatives 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
Representative Drug(s) D0E9PE Drug Info IC50 = 6 nM Click to Show More [1]
2 D06RBE Drug Info IC50 = 9.5 nM [1]
Patent ID WO2015002915
Title Tricyclic Pyri Do-Carboxam I D E Derivatives 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
Representative Drug(s) D0E1KS Drug Info IC50 = 0.6 nM Click to Show More [1]
2 D0U4LI Drug Info IC50 = 0.8 nM [1]
Patent ID WO2014055996
Title Rho Kinase Inhibitors.
Abstract The invention relates to inhibitors of ROCKl and/or ROCK2. Also provided are methods of treating diseases and disorders involving inhibiting ROCKl and/or ROCK2.
Applicant(s) Kadmon Corporation, Llc
Representative Drug(s) D0DO1U Drug Info N.A. Click to Show More [1]
2 D0QX0O Drug Info N.A. [1]
3 D0V6OK Drug Info N.A. [1]
4 D0VK6S Drug Info N.A. [1]
5 D0YV6S Drug Info N.A. [1]
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
Representative Drug(s) D0T0RV Drug Info IC50 < 100 nM [1]
Patent ID WO2013112722
Title Inhibitors of Rho Associated Protein Kinases (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
Representative Drug(s) D0CW9Q Drug Info IC50 = 670 nM [1]
Patent ID WO2016138335
Title Indazolyl Thiadiazolamines and Related Compounds for Inhibition of Rho-Associated Protein Kinase and The Treatment of Disease.
Abstract The invention provides indazolyl thiadiazolamines and related compounds, pharmaceutical compositions, methods of inhibiting Rho-associated protein kinase, and methods of treating inflammatory disorders, immune disorders, fibrotic disorders, and other medical disorders using such compounds. An exemplary indazolyl thiadiazolamine compound is an N-(5-[5-[(1H4ndazol-5-yl)amino]-1,3,4-thiadiazol-2-yl]pyridin-3-yl)acetamide compound.
Applicant(s) Lycera Corporation
Representative Drug(s) D0G3DM Drug Info N.A. [1]
Patent ID WO2015054317
Title Rho Kinase Inhibitors.
Abstract The invention provides novel inhibitors of ROCK1 and/or ROCK2. Also provided are methods of treating diseases and disorders involving inhibiting ROCK1 and/or ROCK2. The present invention includes pharmaceutical compositions comprising the compounds of the invention and a pharmaceutically acceptable carrier and/or diluents. The present invention includes compositions comprising a substantially pure compound of the invention and a pharmaceutically acceptable salt, steroisomer, or hydrate thereof: and a pharmaceutically acceptable excipient and/or diluents.
Applicant(s) Kadmon Corporation, Llc
Representative Drug(s) D0V6OK Drug Info N.A. [1]
Patent ID WO2011062765
Title 1,4-Benzodiazepine-2,5-Diones and Related Compounds with Therapeutic Properties.
Abstract The present invention provides novel chemical compounds characterized as Rho kinase (ROCK) inhibitors, methods for their discovery, and their therapeutic, research, and diagnostic use. In particular, the present invention provides 1,4-benzodiazepine-2,5-dione compounds and related compounds having ROCK inhibitory activity, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with ROCK activity.
Applicant(s) The Regents of the University of Michigan
Representative Drug(s) D0QC6H Drug Info N.A. [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
Patent ID WO2006105081
Title Pharmacokinetically Improved Compounds.
Abstract The present invention relates to inhibitors of ROCKl and R0CK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCKl and or R0CK2 that are useful for the treatment of disease.
Applicant(s) Surface Logix, Inc
References  Top
REF 1 Rho kinase inhibitors: a patent review (2014 - 2016).Expert Opin Ther Pat. 2017 Apr;27(4):507-515.

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