277 results about "Retinopathy" patented technology

The present disclosure relates to novel sustained-release intraocular drug delivery systems and improvements in the treatment of retinopathies. In particular, fibronectin scaffold domain proteins that selectively inhibit VEGFR-2 are contemplated.

The invention discloses and claims benzimidazole compounds of formula (I):

wherein X is C—R2; Y is C—R2 or C—R3; W and Z are each C—R3; R1 is an optionally substituted aryl, heteroaryl or a saturated 5- or 6-membered monocyclic heterocyclic radical or a bicyclic heterocyclic radical; and A5 is H or alkyl; or a stereoisomer, a racemate, an enantiomer or a diastereoisomer of said compound of formula (I) or a pharmaceutically acceptable salt thereof; the use of compounds of formula (I) for the treatment of a disorder of proliferation of blood vessels, uncontrolled angiogenesis, a fibrotic disorder, a disorder of proliferation of mesangial cells, a metabolic disorder, allergy, asthma, thrombosis, a disease of the nervous system, retinopathy, psoriasis, rheumatoid arthritis, diabetes, muscle degeneration, solid tumors and cancers, pharmaceutical compositions comprising a compound of formula (I) and one or more pharmaceutically acceptable adjuvants or diluents and pharmaceutical compositions comprising a compound of formula (I) and one or more. antimitiotic agents.

The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

Methods and compositions for treating retinal diseases comprising therapeutic amounts of a compound selected from a normal Puf-A gene product, an active polypeptide fragment thereof, an analog thereof or a peptidomimetic thereof. Vectors, including AAV vectors comprising the therapeutic compound are provided. Puf-A compositions suitable for subretinal, intravitreal, topical, subconjunctival, retrobulbar, periocular, suprachoroidal, or intraocular administration are provided. Methods for screening siRNA, RNAi and shRNA, small molecules and monoclonal antibodies that inhibit Puf-A target activity and reduce apoptosis are provided.

A compound of formula:

where Ar₁, Ar₂, X, R₃, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Tetrahydropiperidyl Compound”); compositions comprising an effective amount of a Tetrahydropiperidyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Tetrahydropiperidyl Compound are disclosed herein.

The invention relates to highly concentrated DHA and EPA formulations in a soft gel capsule. A capsule may contain at least 80% omega-3 fatty acids, salts or derivatives thereof, where EPA and DHA are present in relative amounts of greater than or equal to 3:1 or less than or equal to 1:3, and constitute at least 75% to greater than 95% of the total fatty acids present in the capsule. Capsules of the invention may be provided in a blister package so as to provide clean and protected oils that are easy to travel with. Compliance is improved with one-pill-a-day dosing and the days of the week imprinted on the foil packing. Anitoxidant protection may be provided by rosemary and vitamin C. The invention also provides a methods of treatment, modulation or prophalaxis of coronary disease, altering serum LDL-cholesterol and/or HDL-cholesterol, lowering serum triglycerides, lowering blood pressure, pulse rate, altering the activity of the blood coagulation factor VII complex, mild hypertension, protection from cyclosporine toxicity in kidney transplant, rheumatoid arthritis, development and progression of retinopathy, hypertriglyceridemia, and neurological disorders in a subject.

Methods for the treatment or prevention of a number of ocular diseases or disorders are disclosed. In particular, methods are disclosed for the amelioration of macular degeneration, diabetic retinopathy and other retinopathies, as well as uveitis, presbyopia, dry eye, glaucoma, blepharitis and rosacea of the eye. The methods comprise administration of a compositions comprising an ophthalmologically acceptable carrier or diluent and a hydoxylamine compound in a therapeutically sufficient amount to prevent, retard the development or reduce the symptoms of one or more of the ophthalmic conditions.

The present invention relates to a method of making novel dipeptidyl peptidase-IV ("DPP-IV') inhibitor compounds useful for treating, inter alia, diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes mellitus, metabolic syndrome (Syndrome X or insulin resistance syndrome), hyperglycemia, impaired glucose tolerance, glucosuria, metabolic acidosis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome and to prevent disease progression in Type 2 diabetes. The invention also relates to a method of making 3,3,4,4-tetrafluoropyrrolidine, a starting material utilized in the afore-mentioned method for preparing DPP-IV compounds.

Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, leukemias, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocyctosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.

Piperidine Compounds; compositions comprising a Piperidine Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperidine Compound are disclosed. In one embodiment, the Piperidine Compound has the formula:

and pharmaceutically acceptable salts thereof, wherein Ar₁, Ar₂, X, R₃, R₄, and m are as disclosed herein.

The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

The present invention provides a method for lowering intraocular pressure and providing neuroprotection to a patient in need thereof by administering a therapeutically effective amount of at least one non-nucleotide or non-protein agent that inhibits expression and/or signaling of lysyl oxidase (LOX) or a lysyl oxidase-like protease (LOXL).

The invention discloses a lutein ester health care product for protecting eyesight. The lutein ester health care product is prepared by taking lutein ester as a main material, and adding any one or more materials including taurine, selenium, zinc, alpha-lipoic acid, docosahexaenoic acid (DHA), vitamin A, vitamin E, vitamin B1, vitamin B2 and bilberry extract, and pharmaceutically acceptable formulation accessories. The outstanding innovation of the invention is the implementation of the method for preparing a functional eye health care product with the lutein ester instead of lutein, so that the bioavailability, the stability and the health care effect of the product are improved, and production cost can be greatly reduced. The health care product can be prepared into common dosage forms, such as tablets, capsula, granules and soft capsules. The lutein ester health care product is mainly used for the treatment on diseases, such as myopia, amblyopia, hyperopia, presbyopia, cataract, vitreous opacity, retinal pigment degeneration, macular degeneration, asthenopia, and retinopathy caused by diabetes, and the like. The lutein ester health care product adopts a unique formulation of multiple constituents, measures and mechanisms, and has significant treatment effects and excellent social and economic benefits.

The invention provides peptide derivatives designed to deliver peptides having growth factor inhibitory activity, especially somatostatin analogs, to the retina by sequential metabolism. The peptide derivatives, which comprise a dihydropyridine<CUSTOM-CHARACTER FILE="US06440933-20020827-P00900.TIF" ALT="custom character" HE="20" WI="20" ID="CUSTOM-CHARACTER-00001"/>pyridinium salt-type redox targetor moiety, a bulky lipophilic function and an amino acid/dipeptide/tripeptide spacer, are used in the prevention and treatment of diabetic retinopathy.

Ophthalmically acceptable compositions used in arresting the development of cataract, presbyopia, macular degeneration and other retinopathies, glaucoma, uveitis and various corneal disorders are disclosed. The compositions are also useful as a prophylactic treatment to prevent or delay development of age-related ocular disorders, which include cataracts, presbyopia, glaucoma and macular degeneration. The compositions comprise a pharmaceutically acceptable carrier or diluent and at least one compound having the formula:

[0001]
• where R₁ and R₂ are, independently, H or C₁ to C₃ alkyl;
[0002]
• R₃ and R₄ are, independently C₁ to C₃ alkyl; and
[0003]
• where R₁ and R₂, taken together, or R₃ and R₄, taken together, or both may be cycloalkyl;
[0004]
• R₅ is H, OH, or C₁ to C₆ alkyl;
[0005]
• R₆ is or C₁ to C₆ alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl;
[0006]
• R₇ is C₁ to C₆ alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl or where R₆ and R₇, or R₅, R₆ and R₇, taken together, form a carbocycle or heterocycle having from 3 to 7 atoms in the ring.