178 results about "Oxindole" patented technology

Nitric oxide releasing oxindole prodrugs are described which are useful in methods of treating or preventing pain, inflammation, fever, or gastrointestinal lesions in a patient in need of such treatment, or of modifying an inflammatory disease or condition by favorably affecting the outcome thereof in said patient, wherein there is administered to said patient a therapeutically effective amount of a compound of Formula (I): and pharmaceutically acceptable salts thereof. In preferred embodiments, X is a covalent bond; RA and RB are both hydrogen; n is the integer 4; Y is -O-; Z is -NO2; RC is a member selected from the group consisting essentially of 5-Cl and 5-F; RD is a member selected from the group consisting essentially of 6-Cl and 6-F; and RE is a member selected from the group consisting essentially of benzyl, 2-furyl, 2-thienyl, 5-chloro-2-thienyl and 5-trifluoromethyl-2-thienyl.

This invention is directed to oxindole compounds that are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of using the compounds are also disclosed.

The present invention relates to a new use of oxindole derivatives of formula I, as a free base or pharmaceutically acceptable salts thereof, in the manufacture of a medicament for the prevention and/or treatment of dementia related diseases, Alzheimer's Disease and conditions associated with glycogen synthase kinase-3. Formula (I) wherein R¹, R², R³, ring Z, m and n are as defined as in claim 1. The present invention further relates to a method of prevention and/or treatment of dementia related diseases, Alzheimer's Disease and conditions associated with glycogen synthase kinase-3, as well as a pharmaceutical composition for said use.

The present invention provides a processes, having practical utility, for preparing 2-oxindoles, N-hydroxy-2-oxindoles, or mixtures thereof comprising: catalytically hydrogenating a 2-nitroarylmalonate diester to produce a 2-(N-hydroxyamino)arylmalonate diester, a 2-aminoarylmalonate diester, or mixtures thereof as a first reaction intermediate; cyclizing, by intramolecular aminolysis of one ester group, the first reaction intermediate to produce a N-hydroxy-2-oxindole-3-carboxylate ester, 2-oxindole-3-carboxylate ester, or mixtures thereof as a second reaction intermediate; and hydrolyzing and decarboxylating the remaining ester group of the second reaction intermediate to produce the N-hydroxy-2-oxindole, the 2-oxindole, or mixtures thereof, wherein the cyclization reaction and the hydrolysis and decarboxylation reaction are conducted in situ with the catalytic hydrogenation reaction without isolation of said reaction intermediates.

Methods for preparing oxindole and thio-oxindole compounds are provided, which compounds are useful as precursors to useful pharmaceutical compounds. Specifically provided are methods for preparing 5-pyrrole-3,3-oxindole compounds and 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile. Also provided are methods for preparing iminobenzo[b]thiophene and benzo[b]thiophenone compounds.

This invention relates to compounds which are agonists of the progesterone receptor which have the general structure:

wherein:

R₁, R₂, R₃, R₄, R₅ and Q¹ are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.

The present invention relates to a new compound of formula (I)

6-(5-cyano-2-hydroxy-1H-indol-3-yl)pyridine-3-carboxylic acid or a pharmaceutically acceptable salt thereof, in an essentially pure and isolated form, pharmaceutical formulations containing said compounds, to the use of said active compounds in therapy, and methods of prevention and/or treatment of conditions associated with glycogen synthase kinase-3 related disorders, comprising administering to a mammal, including human in need of such prevention and/or treatment, a therapeutically effective amount of said compound, as well as a process for preparing said compound.

Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.

The present invention relates to inhibition of viruses, e.g., HIV using oxindoles and compounds related to oxindoles. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.

This invention is directed to methods of preparing certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

This invention is directed to spiro-oxindole compounds of formulas (I), (II), (III), as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

This invention is directed to pharmaceutical compositions for topical administration to a mammal, wherein the pharmaceutical compositions comprise a spiro-oxindole compound, as an enantiomer, a racemate or a non-racemic mixture, or a pharmaceutically acceptable salt thereof. These pharmaceutical compositions are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions.

The present invention provides methods of treating skin disorders includes delivering to a mammal a composition containing a compound of formula I, or tautomers thereof, in a regimen, wherein formula I is:

and wherein R¹–R⁵ and Q¹ are defined as described herein. Specifically, methods for treating acne, hirsutism, and a composition for conditioning the skin are described.

This invention is directed to methods of using spiro-oxindole compounds of formula (I): wherein j, k, m, Q, X, R¹, R^2a, R^2b, R^2c, R_2d and R³ are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, N-oxide, solvate or prodrug thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

This invention is directed to asymmetric syntheses of certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.

The invention belongs to urine detection reagents and particularly relates to a reagent for detecting an abnormal metabolite, namely 5-hydroxyindoleacetic acid, in a human body and a preparation method of the reagent. The reagent for detecting a tumor marker, namely 5-hydroxyindoleacetic acid, in urine comprises aqueous solutions of Hg<2+>, Hg2<2+>, Cu<2+>, WO4<2->, SO4<2-> and NO3<->. The preparation method comprises the following steps: preparing a sulfuric acid solution; preparing a nitric acid solution; preparing a solution A; preparing a solution B; preparing a solution C; preparing a solution D; preparing a solution E; mixing. According to the technical scheme provided by the invention, raw materials are easily obtained and are cheap, the preparation process is simple, the obtained reagent is stable in performance and has the characteristics of strong universality, high sensitivity, good specificity and the like when the reagent is applied to cancer detection, and the detection is simple in process, short in time and easy in judgment, so that the reagent is particularly applicable to the massive population check and the clinical auxiliary diagnosis and dynamic treatment effect check of cancers.