322 results about "Quinolinium Compounds" patented technology

A stable solid pharmaceutical composition consisting essentially of an effective amount of a salt of formula (II) together with an alkaline-reacting component maintaining the pH preferably above 8, or a salt with a divalent metal cation; and at least one pharmaceutical excipient; said salt of formula (II) being essentially stable during storage at room temperature for a period of at least 3 years. A process for stabilizing the salt of formula (II). A crystalline salt of formula (II) and a process for preparing said salt.

The present invention provides novel substituted quinoline compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.

Compound of formula (I):wherein:R1 represents hydrogen orwherein A is as defined in the description,R2 and R3 each independently represents alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl,or optionally substituted aminoalkyl or R2 and R3, together with the carbon atom carrying them, form cycloalkyl or monocyclic heterocyclic group, substituted or unsubstituted,R40 represents hydrogen or a group selected from optionally substituted alkyl, optionally substituted alkenyl and optionally substituted alkynyl or Q or -V-Q wherein V represents alkylene, alkenylene or alkynylene and Q represents optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heterocycloalkyl,or optionally substituted heteroaryl,R41 and R5 together form a bond or each represents hydrogen,R6, R7, R8 and R9 each independently represents hydrogen, halogen, alkyl, (C3-C8)cycloalkyl,or -OW wherein W is as defined in the description, and medicinal products containing the same which are useful as antioxidative agents.

A stable solid pharmaceutical composition consisting essentially of an effective amount of a salt of formula (II)together with an alkaline-reacting component maintaining the pH preferably above 8, or a salt with a divalent metal cation; andat least one pharmaceutical excipient;said salt of formula (II) being essentially stable during storage at room temperature for a period of at least 3 years. A process for stabilizing the salt of formula (II).A crystalline salt of formula (II) and a process for preparing said salt.

The present invention provides an azolylacylquanidine compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.

The present invention belongs to gas producing technology. The absorbing liquid for eliminating sulfide from gas mixture includes main absorbent comprising steric hindrance amine and N-methyl diethanolamine; cosolvent of one or several of sulfolane, N-methyl pyrrolidine, polyglycol dialkyl ether, morpholine and its derivative; catalyst of one or several of C2-C12 alkanolamine, piperazine and its derivative, quinoline, urea and metal phthalocyanine complex. Using the absorbing liquid can eliminate H2S, COS, mercaptan, thioether and other sulfide in less steps.

A serious of nitro heterocyclic derivatives including a structure of formula (I) are provided. In formula (I), P, Q and R1 to R8 are defined in the specification. The derivatives disclosed in the present invention are characterized in inhibiting tubulin polymerization, and treating cancers and other tubulin polymerization-related disorders with a suitable pharmaceutical acceptable carrier.

The invention concerns the production of quinoline compounds containing sulfonic acid groups, the said quinoline compounds and their conversion into dyes containing sulfonic acid groups. The dyes according to the invention are used especially to label analytes, for example to label biomolecules.

An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I]wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.

Certain tetrahydroisoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.

The invention provides compounds which exert excellent fungicidal activities against various plant diseases and are useful as active ingredients of pesticides permitting the control of rice blast and so on even in low dosages. Compounds represented by the general formula wherein R<1> and R<2> are each C1-6 alkyl or the like; R<3> and R<4> are each hydrogen, halogeno, or the like; R<5> is hydrogen, C1-6 alkyl, or the like; X is halogeno, C1-6 alkyl, or the like; Y is halogeno, C1-6 alkyl, or the like; n is an integer of 0 to 4; and m is an integer of 0 to 6.

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.

A chemiluminescent substrate of a hydrolytic enzyme having the following general Formula I is disclosed, as follows:Lumi-M-PFormula Iwhere “Lumi” is a chemiluminescent moiety capable of producing light (a) by itself, (b) with MP attached and (c) with M attached. Examples of Lumi include chemiluminescent acridinium compounds, benzacridinium compounds, quinolinium compounds, isoquinolinium compounds, phenanthridinium compounds, and lucigenin compounds, spiroacridan compounds, luminol compounds and isoluminol compounds. M is a multivalent heteroatom having at least one lone pair of electrons selected from oxygen, nitrogen and sulfur, directly attached to the light emitting moiety of Lumi at one end and to P at the other end. P is a group that can be readily removed by hydrolytic enzymes. An enzymatic reaction utilizing the above compound is the following:where HE is a hydrolytic enzyme. Lumi-M is a chemiluminescent product having physical and / or chemical properties different from those of Lumi-M-P.

The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, the present invention provides, for example, compounds represented by the formulas (6), (7-1), (7-2) and (8):wherein R is a fluorine atom or a methoxy group, R1 is a C1-C4 alkyl group, R2 is a hydroxyl-protecting group, and X2 is a halogen atom, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.

This is to provide a plant disease control composition having a broad spectrum against various plant pathogens, and shows excellent controlling effects (synergistic controlling effects) which cannot be expected from a single component alone.A plant disease control composition comprising (Group a) at least one quinoline compound represented by the formula:(wherein R1, R2: an alkyl which may be substituted, an aryl which may be substituted, etc.; R3, R4: H, an alkyl which may be substituted, etc.; X: halogen, an alkyl which may be substituted, etc.; Y: halogen, alkyl, etc.; n: 0 to 4; m: 0 to 6) or a salt thereof, and at least one of fungicidal compounds selected from the group consisting of a Strobilurin series compound, a triazole series compound, etc., as effective ingredients.

Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and / or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.

The present invention relates to a compound represented by the following formula [I]wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical composition, an anti-HIV agent and an HIV integrase inhibitor containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an anti-HIV agent, or as an agent for the prophylaxis or treatment of AIDS. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Because it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.

A quaternary nitrogen-containing corrosion inhibitor of formulawhereinis an aromatic, nitrogen-containing ring of 5 to 14 ring atoms, optionally containing an additional N, O or S ring atom and optionally substituted with one or more alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, amino, aminoalkyl, alkoxy, hydroxylalkyl, or cyano groups, or a mixture thereof, Y is a group of formula —OC(O)R1 or —C(O)R1; L is C1-C10 alkyl, C2-C10 alkenyl or a group of formula CH2CH(OR2)CH2—; R1 is C8-C20 alkyl or C8-C20 alkenyl; R2 is H or C(O)R1; R3 and R4 are independently selected from H, alkyl, alkenyl, amino, alkoxy, hydroxylalkyl and cyano; and X is Br, Cl or I is particularly useful for inhibiting corrosion in oil and gas field applications.

Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and / or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.

This invention involves involves the use of compounds having the following structure:wherein:(a) R is unsubstituted C1-C3 alkanyl or alkenyl; and(b) R' is selected from hydrogen; unsubstituted C1-C3 alkanyl or alkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thiol; cyano; and halo;for preventing or treating of disorders modulated by alpha-2 adrenoceptors.The subject invention also involves novel compounds and compositions.

A soil treating agent or a seed treating agent having excellent prevention effects against various plant pathogens (particularly against rice blast) is provided. A soil treating agent or seed treating agent, comprising one or more compounds of the general formula (Ia), (Ib) or (Ic):(wherein R1, R2: C1-C6 alkyl (may be substituted), aryl (may be substituted), heteroaryl (may be substituted), aralkyl (may be substituted) and the like; R3, R4: H, C1-C6 alkyl (may be substituted), halogen, C1-C6 alkoxy and the like; X: halogen, C1-C6 alkyl (may be substituted), C2-C6 alkenyl (may be substituted), C2-C6 alkynyl (may be substituted), aryl (may be substituted), heteroaryl (may be substituted), C1-C6 alkoxy and the like; Y: halogen, C1-C6 alkyl, C1-C6 alkoxy, OH; n: 0 to 4; m: 0 to 6) or salts thereof as an active ingredient.

This invention relates to MTP / Apo-B secretion inhibitors of Formula (I) wherein R1-R7, X1, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the compounds, and methods of use of the compounds and compositions. The compounds of the invention are useful in treating obesity and associated diseases, conditions or disorders.

The subject invention provides a mechanism by which steroidal quinol compounds confer beneficial ophthalmic effects. The subject compounds possess a lipophilic-hydrophilic balance for transcorneal penetration and are readily reduced into parent phenolic A-ring steroid compounds to provide protection or treatment against various ocular symptoms and disorders. The compounds according to the subject invention appear to be highly advantageous as prodrugs to provide protection and / or treatment against ocular disorders. These prodrugs confer lipid solubility optimal for transocorneal penetration and are readily converted to endogenous reducing agents into active phenolic A-ring steroid compounds. To the extent that these prodrugs have reduced feminizing effects and systemic toxicity, they would be expected to be quite advantageous for protecting or treating the eye against ocular disorders such as cataract or glaucoma without undesired (systemic) side effects).