Patent classifications
A61P27/02
FUSED TRICYCLIC COMPOUND AND MEDICINAL USE THEREOF
The present invention provides a compound having a PDHK inhibitory activity and useful for the treatment or prophylaxis of diabetes (type 1 diabetes, type 2 diabetes etc.), insulin resistance syndrome, metabolic syndrome, hyperglycemia, hyperlactacidemia, diabetic complications (diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, cataract etc.), cardiac failure (acute cardiac failure, chronic cardiac failure), cardiomyopathy, myocardial ischemia, myocardial infarction, angina pectoris, dyslipidemia, atherosclerosis, peripheral artery disease, intermittent claudication, chronic obstructive pulmonary disease s, brain ischemia, cerebral apoplexy, mitochondrial disease, mitochondrial encephalomyopathy, cancer, pulmonary hypertension, Alzheimer disease, vascular dementia, glaucoma, diabetic retinopathy, retinopathy of prematurity, retinal vein occlusion, ischemic optic neuropathy or chronic kidney disease. The present invention relates to a compound of the formula [I-a], or a pharmaceutically acceptable salt thereof:
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wherein each symbol is as defined in the DESCRIPTION.
USE OF GP73 INHIBITOR IN PREPARATION OF MEDICINE FOR TREATING DIABETES
Embodiments of the present invention relate to use of a GP73 inhibitor in preparation of a drug for treating diabetes. In the embodiments of the present invention, the inventor finds that GP73 plays a key role in blood glucose regulation, and in particular, finds that soluble GP73 can specifically bind to glucagon to form a complex, enhances the blood glucose-rising function and gluconeogenesis function of glucagon and prolongs the half-life of glucagon; and finds soluble GP73 can activate the glucose production in liver and/or kidney and a gluconeogenesis signaling pathway in a glucagon-independent manner. Based on the blood glucose regulation effect of the GP73 described above, the inventor also proves through animal experiments: the GP73 inhibitor can reduce the blood glucose level and glycated hemoglobin level of diabetic mice and have a protective effect on islet β cells, and thereby having the effect of treating diabetes.
METHODS AND COMPOSITIONS TO PROMOTING RETINAL REGENERATION USING PROX1 MIGRATION INHIBITOR AS ACTIVE INGREDIENT
The present invention relates to a technique capable of treating a retinal neurodegenerative disease through regeneration of a retinal nerve by targeting Prox1 in the mammalian retina using an inhibitor which inhibits Prox1 expression or migration. According to the present invention, inducing the regeneration of the damaged retina in mammals, and thus can be commonly applied to the treatment of various retinal neurodegenerative diseases causing vision loss, and furthermore, when combining with a selective retinal nerve differentiation method or the like, it is expected that the method can be used for the development of an innovative retinal regeneration method capable of selectively regenerating only specific degenerating retinal neurons.
METHODS AND COMPOSITIONS TO PROMOTING RETINAL REGENERATION USING PROX1 MIGRATION INHIBITOR AS ACTIVE INGREDIENT
The present invention relates to a technique capable of treating a retinal neurodegenerative disease through regeneration of a retinal nerve by targeting Prox1 in the mammalian retina using an inhibitor which inhibits Prox1 expression or migration. According to the present invention, inducing the regeneration of the damaged retina in mammals, and thus can be commonly applied to the treatment of various retinal neurodegenerative diseases causing vision loss, and furthermore, when combining with a selective retinal nerve differentiation method or the like, it is expected that the method can be used for the development of an innovative retinal regeneration method capable of selectively regenerating only specific degenerating retinal neurons.
COMPOSITIONS OF GROWTH FACTOR FOR THE TREATMENT OF EYE DISEASE
The present disclosure relates to pharmaceutical compositions comprising a growth factor and methods of treating or preventing of eye diseases using the growth factor and compositions thereof.
COMPOSITIONS OF GROWTH FACTOR FOR THE TREATMENT OF EYE DISEASE
The present disclosure relates to pharmaceutical compositions comprising a growth factor and methods of treating or preventing of eye diseases using the growth factor and compositions thereof.
Use of a VEGF antagonist to treat angiogenic eye disorders
The present invention provides methods for treating angiogenic eye disorders by sequentially administering multiple doses of a VEGF antagonist to a patient. The methods of the present invention include the administration of multiple doses of a VEGF antagonist to a patient at a frequency of once every 8 or more weeks. The methods of the present invention are useful for the treatment of angiogenic eye disorders such as age related macular degeneration, diabetic retinopathy, diabetic macular edema, central retinal vein occlusion, branch retinal vein occlusion, and corneal neovascularization.
Ophthalmic compositions
The present disclosure provides an ophthalmic composition comprising 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate or its pharmaceutically acceptable salts; about 0.01% weight/volume to about 1.0% weight/volume of a buffer; and about 0.01% weight/volume to about 10% weight/volume of a tonicity agent.
Atropine pharmaceutical compositions
The inventive subject matter is directed to compositions and methods for sterile and storage stable low-dose atropine formulations with improved stability. Most preferably, the compositions presented herein are substantially preservative free and exhibit less than 0.35% tropic acid from degradation of atropine. Advantageously, contemplated formulations are also substantially free of preservatives.
ANTIBODIES AGAINST HUMAN ANGIOPOIETIN 2
The present invention relates to antibodies against human Angiopoietin 2 (anti-ANG-2 antibodies), methods for their production, pharmaceutical compositions containing said antibodies, and uses thereof.