423 results about "Geometric isomer" patented technology

Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

The invention relates to novel therapeutic agents and diagnostic probes. The invention also relates to phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor triazine-, pyrimidine- and pyridine-based compoundŝ Formula (I), their stereoisomers, geometric isomers, tautomers, solvates, metabolites, N-oxide derivatives, pharmaceutically acceptable salts, and prodrugs thereof compositions of the new compounds; either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, for treating disorders mediated by lipid kinases. •Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. (Formula I)

The invention relates to novel ligands of 5-HT₆ receptor, to a pharmaceutical composition containing said novel ligands of 5-HT₆ receptor as active component and to novel medicaments used for humans and warm-blooded animals for treating diseases and conditions of central nervous system, in pathogenesis of which neuromediator systems induced by 5-HT₆ receptors are playing an essential role.

Azaheterocyclic compounds of the general formula 1 or racemates, or optical or geometrical isomers, or pharmaceutically acceptable salts and/or hydrates thereof are used as 5-HT₆ ligands.

Wherein R2 and R3 independently of each other represent an amino group substituent selected from hydrogen; substituted carbonyl; substituted aminocarbonyl; substituted aminothiocarbonyl; substituted sulphonyl; C₁-C₅-alkyl optionally substituted by: C₆-C₁₀-arylaminocarbonyl, heterocyclyl, C₆-C₁₀-arylaminocarbonyl, C₆-C₁₀-arylaminothiocarbonyl, C₅-C₁₀-azaheteroaryl, optionally substituted carboxyl, nitryl group, optionally substituted aryl; R¹_k represents from 1 to 3 substituents of cyclic system, independent of each other and selected from hydrogen, optionally substituted C₁-C₅-alkyl, C₁-C₅-alkoxy, C₁-C₅-alkenyl, C₁-C₅-alkynyl, halogen, trifluoromethyl, CN-group, carboxyl, optionally substituted aryl, optionally substituted heterocyclyl, substituted sulfonyl, optionally substituted carboxyl; the solid line accompanied by the dotted line represents a single or a double bond; n=1, 2 or 3.

A food product containing an effective amount of an active agent which is hydroxymatairesinol, a geometric isomer or stereoisomer thereof, or an acceptable salt thereof, or a mixture thereof, where the food product is selected from the group consisting of a nutritional supplement and a nutrient. The food product can increase the level of enterolactone or another metabolite of hydroxymatairesinol in a person's serum thereby causing prevention of a cancer or a certain non-cancer, hormone dependent disease in a person, based on the administration of hydroxymatairesinol to the person.

Disclosed are electrophosphorescent organic metal complexes with formula (I), (H), (III) or (IV), of either geometrical isomers, comprising two bidentate NN-type ligands, or two NO-type ligands, or a tetradentate NNNN-type ligand or a tetradentate NOON-type ligand, and a transition metal. These electrophosphorescent materials are valuable to the application in organic light-emitting devices (OLEDs), including red-, orange-, or yellow-light OLEDs.

Compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof, are useful for inhibiting receptor tyrosine kinases and for treating hyperproliferative disorders mediated thereby. Methods of using compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).

Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

The invention discloses hetero-aromatic compounds and applications thereof in pharmacy. Specifically, the invention provides hetero-aromatic compounds, and steric isomers, geometric isomers, tautomers, racemic bodies, nitrogen oxides, hydrates, solvates, metabolism products, and pharmaceutically acceptable salts or prodrug thereof. The compounds mentioned above can be used to treat autoimmune diseases or proliferative diseases. The invention also discloses a pharmaceutical composition comprising the compounds mentioned above, and an application of the compounds or the pharmaceutical composition in the preparation of drugs for treating autoimmune diseases or proliferative diseases.

Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions.

Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

The present invention relates to novel tricyclic compounds which can bind to FXR and act as modulators of the FXR, or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and the uses of the compounds for the treatment of diseases and/or conditions mediated by FXR. The invention further provides a pharmaceutical composition containing the compound disclosed herein and a method of treatment of diseases and/or conditions mediated by FXR comprising administering the compound or the pharmaceutical composition.

The invention belongs to the technical field of medicine, and relates to semicarbazone derivatives disclosed as general formula I, and geometrical isomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein the substituent groups M, R1, R2, R and n are defined in the specification. The invention also relates to a method for preparing compounds disclosed as Formula I, a pharmaceutical composition containing the compounds and application of the compounds and pharmaceutical composition in preparing drugs for treating and/or preventing cancers and other hyperplastic diseases.

The invention discloses a compound. The compound is a compound shown as a formula I or a stereoisomer, a geometric isomer, a tautomer, nitrogen oxide, hydrate, a solvate, a metabolite and a pharmaceutically acceptable salt of the compound shown as the formula I, wherein Cbz represents benzyloxycarbonyl; Bn represents benzyl; Boc represents tert-butoxycarbonyl. The compound has stable physiochemical properties; compared with XJB-5-131, the compound has the advantages of improved water solubility, stable physiochemical properties, good bioactivity, small medicinal dosage, improved in-vivo stability, high bioavailability, small side effect and prominent target anti-oxidization property; the compound can be used for effectively repairing oxidization injuries of mitochondria, and preventing or treating neurodegenerative diseases including age-related macular degeneration and the like. The formula I is shown in the description.

Compounds of Formulas (Ia) and (Ib), and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).

This invention relates to a liquid or semisolid oral drug formulation comprising a therapeutically active compound of the formula (I)

or a geometric isomer, a stereoisomer, a mixture of isomers, a pharmaceutically acceptable salt, an ester thereof or a metabolite thereof, in combination with a pharmaceutically acceptable carrier.

The invention provides compounds used as a JAK inhibitor, and a use of the compounds, and concretely provides compounds (represented by formula (I)) with JAK inhibition activity or a stereoisomer, a geometric isomer, a tautomer, a racemate, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and a medicinal composition including the compounds. The invention also discloses a use of the compounds or the medicinal composition thereof in the preparation of medicines used for treating autoimmune diseases or proliferative diseases.

The invention relates to an andrographolide derivative the structure of which is shown in a formula (I) or (II) and a stereoisomer, a stereomer, a tautomer, a solvate, a polymorph, a metabolin, ester, a pharmaceutically acceptable salt or a prodrug of the derivative. The andrographolide compound provided by the invention has the advantages of good solubility, high purity and good antipyretic property; and the andrographolide compound is especially suitable to be used as an effective component for preparing antipyretic, anti-inflammatory and antimicrobial medicaments.