110105-32-3Relevant academic research and scientific papers
VISUAL FUNCTION DISORDER IMPROVING AGENTS
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, (2016/09/12)
The present invention provides a visual function disorder improving agent containing a compound having Rho kinase inhibitory activity, particularly (R)-(+)-N-(1H-pyrrolo?2,3-büpyridin-4-yl)-4-(1-aminoethyl)benzamide, as an effective component. This agent
Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2- ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist
Liverton, Nigel J.,Bednar, Rodney A.,Bednar, Bohumil,Butcher, John W.,Claiborne, Christopher F.,Claremon, David A.,Cunninghan, Michael,DiLella, Anthony G.,Gaul, Stanley L.,Libby, Brian E.,Lyie, Elizabeth A.,Lynch, Joseph J.,McCauley, John A.,Mosser, Scott D.,Nguyen, Kevin T.,Stump, Gary L.,Sun, Hong,Wang, Hao,Yergey, James,Koblan, Kenneth S.
, p. 807 - 819 (2007/10/03)
The discovery of a novel series of NR2B subtype selective N-methyl-D-aspartate (NMDA) antagonists is reported. Initial optimization of a high-throughput screening lead afforded an aminopyridine derivative 13 with significant NR2B antagonist potency but limited selectivity over hERG-channel and other off-target activities. Further structure-activity studies on the aminoheterocycle moiety and optimization of the carbamate led to the highly potent 2-aminopyrimidine derivative 20j with a significantly improved off-target activity profile and oral bioavailability in multiple species coupled with good brain penetration. Compound 20j demonstrated efficacy in in vivo rodent models of antinociception, allodynia, and Parkinson's disease.
Preventives/remedies for kidney diseases
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, (2008/06/13)
A compound having a Rho kinase inhibitory activity, such as (+)-trans-4-(1-aminoethyl)-1-(4-pyridylcarbamoyl)-cyclohexane, has a renal interstitial fibrosis inhibitory action in renal interstitial fibrosis model mice and various other actions, and therefore, is useful as an agent for the prophylaxis or treatment of renal diseases.
Antitumor effect potentiators
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, (2008/06/13)
When used concurrently with an antitumor agent, a compound having a Rho kinase inhibitory activity, such as (R)-(+)-N-(4-pyridyl)-4-(1-aminoethyl)benzamide, reinforces an antitumor effect of the antitumor agent and is useful as an antitumor effect potentiator. Particularly, a compound having a Rho kinase inhibitory activity used with an antitumor agent in combination can reduce the dose of the antitumor agent, which in turn affords provision of a sufficient effect and/or reduction of side effects.
Agent for prophylaxis and treatment of glaucoma
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, (2008/06/13)
An agent for the prophylaxis and treatment of glaucoma, which contains a compound having a Rho kinase inhibitory activity, particularly an agent for the prophylaxis and treatment of glaucoma, which contains a compound of the formula (I) wherein each symbol is as defined in the specification, as the compound having a Rho kinase inhibitory activity, is provided. The agent for the prophylaxis and treatment of glaucoma of the present invention is a novel agent for the prophylaxis and treatment of glaucoma and has intraocular pressure lowering action, optic disc blood flow improving action and aqueous humor outflow promoting action.
PREVENTIVES/REMEDIES FOR ANGIOSTENOSIS
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, (2008/06/13)
An agent for the prophylaxis and treatment of vascular constriction is provided, which contains a compound having a Rho kinase inhibitory activity. In particular, a compound having a Rho kinase inhibitory activity, for example, (+)-trans-4-(1-aminoethyl)-1-(4-pyridylcarbamoyl)cyclohexane, suppresses regenerative intima proliferation after disorder of blood vessel and has various other actions. Therefore, it is useful as an agent for the prophylaxis and treatment of vascular constriction, specifically, an agent for the prophylaxis and treatment of vascular constriction induced by disorder of vascular wall, such as vascular restenosis that occurs after an operation of percutaneus transluminal coronary angioplasty, vascular restenosis that occurs after an operation of percutaneus transluminal angioplasty, vascular constriction that occurs after vascular reconstruction, such as DCA, operation of intravascular indwelling of stent and the like, and vascular constriction that occurs after organ transplantation.
PREVENTIVES/REMEDIES FOR LIVER DISEASES
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, (2008/06/13)
The invention provides an agent for the prophylaxis and treatment of liver disease and an activation inhibitor of hepatic stellate cells, which contains a compound having a Rho kinase inhibitory activity. The compound having a Rho kinase inhibitory activity, such as (+)-trans-4-(1-aminoethyl)-1-(4-pyridylcarbamoyl)cyclohexane, is useful for the prophylaxis and treatment of liver diseases, such as hepatitis, hepatic fibrosis, hepatic cirrhosis, hepatic cancer and the like, because it has various actions, such as a superior inhibitory action on the activation of hepatic stellate cell, suppressive action on hepatic fibrogenesis in liver tissues and the like.
N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists
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, (2019/08/08)
Compounds represented by Formula (I): 1or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
PREVENTIVES/REMEDIES FOR INTERSTITIAL PNEUMONIA AND PULMONARY FIBROSIS
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, (2008/06/13)
An agent for the prophylaxis and treatment of interstitial pneumonia and pulmonary fibrosis, which contains a compound having a Rho kinase inhibitory activity, particularly an agent for the prophylaxis and treatment of interstitial pneumonia and pulmonary fibrosis, which contains a compound of the formula (I) wherein each symbol is as defined in the specification, as the compound having a Rho kinase inhibitory activity, is provided.
