1031 results about "Quinolizine" patented technology

The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use.

The invention relates to the field of pharmaceutical chemistry and specifically discloses an aryl ruthenium-beta-carboline complex and its preparation method and application. The aryl ruthenium-beta-carboline complex is [Ru(Eta6-arene)(N-N)Cl](PF6), wherein Eta6-arene is aryl ligand p-cymene(p-cymene, CYM) or benzene(benzene, Ben), N-N is beta-carboline alkaloid derivative1-(2-pyridine)-9H-pyridine[3,4-b]indole(L1), 1-(2-quinoline)-9H-pyridine[3,4-b]indole(L2) or 1-(2-imidazole)-9H-pyridine[3,4-b]indole(L3). The complex provided by the invention has very outstanding activity in in-vitro antitumor screening. In addition, in comparison with cancer cell lines, toxicity of the complex to normal cells is greatly reduced, and the complex has a good potential for development of antitumor drugs.

Methods are disclosed for increasing the effectiveness of dextromethorphan in treating chronic or intractable pain, for treating tinnitus and for treating sexual dysfunction comprising administering dextromethorphan in combination with a therapeutically effective dosage of a debrisoquin hydroxylase inhibitor. A preferred combination is dextromethorphan and the oxidative inhibitor quinidine.

The present invention relates to processes for preparing solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, including Compound 1 Form A, Compound 1 Form A-HCl, Compound 1 Form B, and Compound 1 Form B-HCl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith.

The invention discloses a new gene purE1 which has high degradability on quinoline. Experiment shows that by using the purE1 gene to transform a microbe, the microbe can obtain degradation activity on quinoline, and the maximal degradation concentration of the degradation activity of the microbe provided by the purE1 gene and its coded protein is up to 850 mg/L. The invention has very important practical application value for the treatment of quinoline contaminants.

A nitrogen-phosphinonickel match catalyst system is composed of the primary catalyst, [(2-methyl)-(8-diphenylphosphino)] nickel quinolinylhalide, and secondary catalyst, methyl aluminoxyane (MAO). Its advantage are low cost, high activity, high output rate of product (norbornaene) (up to 20-100%), and wide range of adjustable molecular weights (1X10 to the power 5-3X10 to the power 6).

Compositions and methods are provided for obtaining stabilized quinol compositions, such as catecholamine drugs (e.g., epinephrine solutions), and also for obtaining stable pharmaceutical formulations that comprise a stabilized quinol composition and a second pharmacologically active component such as a local anesthetic or other active drug ingredient having a reversibly protonated amine group. Stability is achieved through the inclusion of an appropriately selected pH buffer and a thiol agent, based on redox and pH buffering principles including pKa of the buffer and of the reversibly protonated amine group.

Described herein are compounds that are useful as caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CN, CHN2, R, or CH2Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, or an aralkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; and R3 is hydrogen, an optionally substituted aryl group, an optionally substituted aralkyl group, or an optionally substituted C1-6 aliphatic group, R4 is an optionally substituted group selected from an aryl group or a heterocyclyl group, or R3 and R4 taken together with the nitrogen to which they are attached optionally form a substituted or unsubstituted monocyclic, bicyclic or tricyclic ring.

The problems of the present invention are to find a pharmaceutical composition and a method for treating cancer that exhibit excellent anti-tumor effect. Excellent anti-tumor effect is achieved when 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, an analogous compound thereof, a pharmacologically acceptable salt thereof or a solvate thereof is used in combination with taxane.

Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.

An organic light-emitting device includes a first electrode, a mixed organic layer, an emission layer, an electron transport layer, and a second electrode. The mixed organic layer contains a fluorene derivative and a pyrazine derivative, and the electron transport layer contains a lithium quinolate and a pyridine derivative.

This invention concerns compounds and a pharmaceutical composition of the structure: wherein: 1 R.sup.1 is selected from the group consisting of alkyl, substituted alkyl, aryl, and substituted aryl which group will produce a natural amino acid structure or an unnatural amino acid structure, and the carbon adjacent to R.sup.1 is in the D or L configuration; R.sup.2 is selected from the group consisting of --F and 2 wherein R.sup.3 and R.sup.4 are each selected from the group consisting of hydrogen, alkyl, fluoro, chloro, carboxyl, alkoxy, alkyl carbonyl, aryl carbonyl, and amino; R.sup.5 and R.sup.5' are each independently selected from the group consisting of hydrogen, alkyl, alkoxy, fluoro, chloro, carboxy, alkoxy, alkyl carbonyl, aryl carbonyl, and amino, R.sup.6 is selected from the group consisting of alkyl having 1 to 10 carbon atoms, aryl or substituted aryl, and m is 1, 2 or 3. These compounds are reagents and pharmaceutical compositions have pro-drug and apoptosis properties and are useful in a variety of therapies, for diseases such as arthritis, ALS, MS, and the like.

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.

The invention discloses a 3,3'-methene-difluoroquinolone derivative of a chiral oxazine quinoline ring as well as a preparation method and application of the 3,3'-methene-difluoroquinolone derivative. The 3,3'-methene-difluoroquinolone derivative has a chemical general structural formula I shown in the specification, wherein R represents cyclopropyl or ethyl or fluoroethyl; R1 represents a hydrogen atom or methyl or ethyl; R2 represents a hydrogen atom or methyl; X represents a nitrogen atom or a hydrocarbon (CH) group or a fluoro-substituted carbon atom (F-C) or a methoxyl-substituted carbon atom (CH3O-C). The 3,3'-methene-difluoroquinolone derivative of the chiral oxazine quinoline ring, disclosed by the invention, can be used for realizing the superposition of a difluoroquinolone framework and alpha, beta-unsaturated ketone pharmacophores, so that the antitumor activity of a new compound is improved, the toxic and side effects on normal cells can be reduced, and the 3,3'-methene-difluoroquinolone derivative can be used as an antitumor active substance for developing an antitumor drug of a totally new structure.

This application describes substituted 1,3,4,6,7,11b-hexahydro-benzo(a)quinolizine compounds, pharmaceutical compositions containing them, processes for making them and their therapeutic methods.

The invention provides compounds of Formula (I):

and pharmaceutically acceptable salts, solvates and stereoisomers thereof, wherein A, B, E, G, W, X, Y, Z, o, and R₁ are as disclosed herein (“Compound(s) of the Invention”), which are useful as cardio-protective and/or neuro-protective agents. The invention also provides pharmaceutical compositions comprising a Compound of the Invention and methods for treating, preventing and/or managing a vascular, cardiovascular or neurological disease or disorder, comprising administering to a patient in need thereof a Compound of the Invention.