16 results about "EP4 Receptor" patented technology

The present invention relates to a series of novel heterobicyclic amide derivatives as EP4 receptor antagonists useful in the treatment of diseases or conditions mediated by the action of PGE2 on the EP4 receptor, such as pain, inflammatory diseases and cancer. The scope of the invention also includes pharmaceutical compositions containing such compounds and methods of using these compounds to treat subjects suffering from a condition mediated by the effect of PGE2 on the EP4 receptor.

The present invention relates to compounds of formula (I) and pharmaceutical compositions comprising these compounds. The compounds provided herein can be used as prostaglandin E2 (PGE2) EP4 receptor antagonists, which makes them very useful for therapy, particularly for the treatment or prevention of cancer, neovascular eye disease, inflammatory pain or inflammatory diseases such as multiple sclerosis, rheumatoid arthritis or endometriosis. #imgabs0#

The present application relates to a compound represented by the general formula (I) (where all symbols represent the same meanings as those described in the specification) or a pharmaceutically acceptable salt thereof, which is useful as an EP4 agonist, and in particular, which has EP4 agonist activity, is selective to other PGE receptor subtypes, and has a low risk of toxicity to the circulatory system, and thus is useful as an active ingredient for preventing and / or treating diseases associated with the EP4 receptor.

Provided are a polymorph of an EP4 receptor antagonist, a preparation method therefor and a use thereof, relating in particular to a polymorph of an EP4 receptor antagonist(S)-4-(1-(2-(4-fluorobenzyl)-4, 7-dihydro-5H-thieno [2,3-c]pyran-3-carboxamido) ethyl) benzoic acid, a preparation method therefor and a use thereof. Compared with an amorphous form of a compound represented by formula I, the polymorph of the present invention has higher stability and better processing performance and is very suitable for being prepared into a medicine.

The present invention discloses the use of luteolin, isoquercetin and febuxostat in the preparation of a medicament for preventing and / or treating hyperuricemia and gout. In the composition of luteolin and isoquercetin, the mass ratio of luteolin to isoquercetin is 1:5 to 100. In the solution of the present invention, it is found that luteolin and isoquercetin are used in combination with febuxostat in a specific ratio. On the one hand, it has the effects of inhibiting XOD oxidase and reducing uric acid, and on the other hand, it can antagonize the EP4 receptor to reduce inflammation. Therefore, the dosage of febuxostat can be reduced, the inflammatory factors during the occurrence of gouty arthritis can be inhibited, the acute attack of gouty arthritis can be relieved, and it has a significant effect on the treatment of gouty arthritis without obvious toxic and side effects.

The present application provides a kind of compound shown in formula I, its tautomer, stereoisomer, hydrate, solvate, pharmaceutically acceptable salt or prodrug;The compound has effective antagonism to EP4, has good affinity with EP4 receptor, and can be used as EP4 antagonist.

The present invention provides co-crystal and salt forms, and compositions and methods thereof, useful for treating various diseases, disorders or conditions in which EP4 prostaglandin receptors are implicated in the mediation of a proliferative disorder, by the administration of small molecule therapeutics acting as inhibitors of prostaglandin EP4 receptor activity.

The invention discloses an application of a prostaglandin EP4 receptor stimulant in a preparation for preventing or treating thyroid-associated ophthalmopathy, belongs to the technical field of biological medicines, and aims to find a new and completely effective preparation for locally inhibiting orbit fat hyperplasia. The 3D cell culture technology closer to the in-vivo environment is used for exploring the influence of the prostaglandin EP4 receptor agonist L-902688 on adipogenic differentiation of TAO patient eye socket adipose-derived mesenchymal stem cells (OASCs), and the result shows that the L-902688 can significantly promote brown adipose differentiation and increase lipid hydrolysis and consumption, can effectively reduce fat accumulation and does not promote secretion of inflammatory factors. The results provide a new treatment thought for clinical treatment of TAO.

The invention discloses a new application of 6-methoxysalicylic acid, namely application of 6-methoxysalicylic acid in preparation of a medicine for relieving convulsion and soothing nerves, through systematic pharmacological experiment research, it is found for the first time that 6-methoxysalicylic acid has EP4 receptor agonistic activity and can exert the effects of relieving convulsion and soothing nerves by specifically activating an EP4 receptor, and the 6-methoxysalicylic acid can be applied to preparation of medicines for relieving convulsion and soothing nerves. The symptoms such as palpitation and restlessness, sleep disorder and the like are effectively improved, and a new way is provided for treating diseases such as insomnia and the like.

The invention is directed to a series of novel heterobicyclic amide derivatives as EP4 receptor antagonists which are useful for treating diseases or conditions mediated by the action of PGE2 at EP4 receptors, such as pain, an inflammatory disease and cancer. Also within the scope of this invention are pharmaceutical compositions containing such compounds and methods of use of these compounds for treating a subject suffering from a condition mediated by the action of PGE2 at EP4 receptors.

The invention discloses a preparation method of EP4 receptor glassine in the technical field of organic synthesis. The method comprises the following steps: (1) reacting p-toluenesulfonamide with N, N '-carbonyldiimidazole in a solvent A, and after the reaction is completed, separating, washing and drying to obtain a compound I; and (2) reacting the compound I with 2-(4-(2-ethyl-4, 6-dimethyl-1H-imidazo [4, 5-c] pyridine-1-yl) phenyl) ethylamine in a solvent B, after the reaction is finished, acidifying and filtering to obtain an intermediate solid, alkalifying, extracting and concentrating the intermediate solid, and crystallizing and purifying the obtained product in acetone to obtain the glassine. The method has the advantages that by-products are reduced, and the yield and the quality of the glassine are improved.

A compound represented by general formula (I) (wherein all symbols have the same meanings as the symbols described in the specification) or a pharmaceutically acceptable salt thereof is useful as an EP4 agonist, particularly has an EP4 agonistic activity, has selectivity for other PGE receptor subtypes, and has a smaller risk of toxicity to the circulatory system. Therefore, the compound or the pharmaceutically acceptable salt thereof is useful as a medicinal ingredient in the prevention and / or treatment of diseases associated with EP4 receptors.

The present invention relates to novel compounds of formula (I) and pharmaceutical compositions containing these compounds. The compounds provided herein can act as prostaglandin E2 (PGE2) EP4 receptor antagonists, which renders them highly advantageous for use in therapy, particularly in the treatment or prevention of cancer, a neovascular eye disease, inflammatory pain, or an inflammatory disease, such as, e.g., multiple sclerosis, rheumatoid arthritis or endometriosis.