522 results about "Benzimidazole derivative" patented technology

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 discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Disclosed are compounds of the formula Iand pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.

A light emitting element comprises a first electrode, a second electrode configured to transmitting light, an organic layer arranged between the first and the second electrodes, comprising a light emitting layer, and a capping layer arranged on the second electrode and made of a material with a higher refractive index than the refractive index of the material constituting the second electrode. The material constituting the capping layer comprises at least one selected from the group consisting of triarylamine derivative, carbazole derivative, benzimidazole derivative and triazole derivative.

The invention belongs to the technical field of the pharmaceutical chemistry, and concretely discloses benzimidazole derivatives, and a preparation method and a medicinal use thereof. The benzimidazole derivatives comprise ligustrazine and NO donor derivatives, and the benzimidazole derivatives can rapidly release ligustrazine or NO in vivo, so there is an effective synergistic effect between the benzimidazole derivatives and azilsartan, thereby the benzimidazole derivatives enhances the antihypertension effect, reduces untoward effects, has an ideal protection effect on the liver and kidney of a patient, and fills a gap in the prior art.

The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I:and pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein W1, W2, W3, W4, U, G, m, R1, and R2 are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II to V as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.

This invention relates to a family of benzimidazole analogs, which are inhibitors of the IgE response to allergens. These compounds are useful in the treatment of allergy, asthma, or any diseases where IgE is pathogenic.

The present invention relates to a compound of the Formula Ior a pharmaceutically acceptable salt thereof, wherein R1, R2, R3A, R3B, R4, R5, X, m, and n are as defined herein. Such novel benzamidazole derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.

The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).

Provided herein are drug delivery systems, such as self-nanoemulsifying drug delivery systems, self-emulsifying drug delivery systems and parenteral microemulsion formulations, suitable for parenteral or oral delivery to a subject. The drug delivery systems may comprise a benzimidazole derivative, e.g., mebendazole, an oil, a surfactant, a cosurfactant and a dipolar aprotic solvent in a microemulsion formulation. Also provided are methods for improving the bioavailability of a benzimidazole derivative during treatment of a pathophysiological condition by using a formulation combining a particular emulsion droplet diameter and ratio of the surfactant:cosurfactant therein, for increasing concentration and retention of a benzimidazole derivative in the lung via a parenterally administerable microemulsion with droplet size of about 35 nm to less than 100 nm and for defining hemolytically safe microemulsions of a benzimidazole derivative during a therapeutic treatment via a parenterally administerable microemulsion with a surfactant:cosurfactant content by weight of about 6% to 48%.

This invention relates to a family of benzimidazole analogs, which are inhibitors of the IgE response to allergens. These compounds are useful in the treatment of allergy, asthma, or any diseases where IgE is pathogenic.

The invention provides compounds of the formula (I):The compounds have activity against cyclin dependent kinases, glycogen synthase kinase and Auroa kinases and are therefore useful to treat cancer and viral diseases.

The present invention relates to indole derivatives or benzimidazole derivatives, to processes for preparing such compounds, to pharmaceutical compositions comprising such compounds, and methods for the prophylaxis and therapy of a disease associated with an increased activity of IκB kinase comprising administering such compounds.

An organic electroluminescence device including: an anode (10), a cathode (70), an emitting layer (40) including an organic compound, which is between the anode (10) and the cathode (70), two or more layers arranged in a hole injection and transport region which is between the anode (10) and the emitting layer (40), and one or more layers arranged in an electron injection and transport region which is between the emitting layer (40) and the cathode (70), wherein a layer in the hole injection and transport region, which is in contact with the emitting layer (40), includes an aromatic amine derivative having a carbazole skeleton, one of the layers other than the layer in contact with the emitting layer (40) in the hole injection and transport region includes one or more materials selected from the group consisting of thiophene derivatives, tricyclic or more cyclic fused aromatic derivatives, amine derivatives excluding the compound represented by the following formula (A), conductive polymers, CFx, CuPc, transition metal oxides, fullerenes and acceptor materials, and a layer in the electron injection and transport region includes a benzimidazole derivative.

This invention relates to novel carboxyl- or hydroxyl-substituted benzimidazole derivatives of formula (I)wherein R1 to R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to FXR and can be used as medicaments.

A rubber composition comprising 100 parts by weight of a rubber ingredient comprising natural rubber and / or a synthetic rubber, 0.1 to 50 parts by weight of at least one nitrogenous compound selected among benzimidazole derivatives having a specific structure and hydrazide derivatives having a specific structure, and 0.1 to 50 parts by weight of a protonic acid; and a pneumatic tire including a member formed from this rubber composition. The rubber composition enables excellent gripping performance while attaining intact productivity. The pneumatic tire produced from this rubber composition, in particular, the tire whose tread has been formed from the composition, has significantly improved gripping performance in high-speed driving, etc.

This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated.

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. antimitotic agents.

This invention provides compounds which are represented by a general formula [I][in which X stands for hydrogen or halogen; B stands for halogen, cyano or optionally fluorine-substituted lower alkyl; D stands for a 3–10 membered aliphatic nitrogen-containing heterocyclic group; R3, R4 and R5 may be same or different, and each stands for hydrogen, lower alkyl optionally having substituent group(s) and the like; and a is 0 or 1]. These compounds exhibit high affinity to nociceptin receptors and whereby inhibit actions of nociceptin, and are useful as an analgesic, antiobestic, agent for ameliorating brain function, treating agents for Alzheimer's disease and dementia, and therapeutic agents for schizophrenia, neurodegenerative diseases, depression, diabetes insipidus, polyuria, hypotension and the like.

Stabilized substituted benzimidazole modified release pharmaceutical formulations with at least two drug-containing fractions, wherein the release from a first fraction precedes the release from a second fraction, pharmaceutical excipients, processes for preparing the stable formulations, packaging therefor, and their use in treatment of erosive esophagitis and heartburn associated with non-erosive gastroesophageal reflux disease.

An organic electroluminescent device includes an anode; a cathode; an organic layer including a light-emitting layer and disposed between the anode and the cathode; and an electron transport layer constituting the organic layer, disposed between the cathode and the light-emitting layer, and having a stacked structure including a layer containing a benzimidazole derivative and a layer containing a dibenzimidazole derivative represented by general formula (1):wherein Y1 to Y8 each represent a substituted or unsubstituted aryl group having 6 to 60 carbon atoms, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted pyridyl group, a substituted or unsubstituted quinolyl group, a substituted or unsubstituted alkyl group having 1 to 20 carbon atoms, a substituted or unsubstituted alkoxy group having 1 to 20 carbon atoms, or a substituted or unsubstituted aliphatic cyclic group, and Y7 and Y8 may form a ring through a linking group.

An enteric formulation containing at least one benzimidazole derivative, said formulation comprising: a core containing at least one benzimidazole derivative and at least one lipophilic antioxidant, and an enteric envelope protecting the core at least at a pH of 3 to 5, preferably at a pH of 1 to 5.

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.

Compounds of formula (I) are inhibitors of PDK1 and CHK1 activity, and of use in the treatment of cancer and autoimmune disorders (I): wherein R2 is a radical of formula R7—(CH2)n−, or a radical of formula -Alk-N(—R5)—R9 wherein n is 0, 1, 2 or 3 and Alk is C1-C6 alkylene; R7 is (i) a heterocyclic ring of 5 or 6 ring atoms coupled via a ring carbon wherein the sole heteroatom is nitrogen, optionally substituted by C1-C6 alkyl or aryl C1-C6 alkyl, (ii) 1-aza-bicyclo[2.2.2]oct-3-yl, or (iii) 8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl; R8 and R9 are independently selected from hydrogen or C1-C3 alkyl; and the remaining substituents are as defined in the claims.