83results about "Heterocyclic compound active ingredients" patented technology

The present invention provides prodrug compounds of diaryldiazepine drug compounds.

Macrolide compounds, such as the FK506 Substance and its related compounds, are provided for the prevention or treatment of eye diseases, particularly glaucoma. Composition containing such compounds is also disclosed.

This application provides methods and compositions for the treatment of cancer. The application provides compositions comprising hyaluronic acid and a chemotherapeutic agent such as irinotecan that are useful in the treatment of cancer.

The biodegradable drug delivery systems described here are formulated for implantation into the nail unit and its surrounding tissues for the treatment of various nail unit conditions. The systems include non-temperature dependent phase change compositions that may be formulated as solutions, solids, semisolids, microparticles, or crystals.

The invention relates to a method of treatment of resistance to platelet inhibitors, i.e. a method to overcome resistance of treatment with platelet inhibitors, said method comprising administering a therapeutically effective amount of dipyridamole in combination with a platelet inhibitor and, optionally, in combination with a third antithrombotic component such as direct thrombin inhibitors, factor Xa inhibitors, combined thrombin/factor Xa inhibitors, heparin, low molecular weight heparin, argatroban, bivalrudin, hirulog or polyglycans to a patient in need thereof. The invention further relates to the use of dipyridamole for the manufacture of a pharmaceutical composition for treatment of resistance to platelet inhibitors. The invention also relates to a method to diagnose resistance to treatment with platelet inhibitors, said method comprising measurement of the density of binding of Annexin V on platelets.

A process is provided for preparing spiro-hydantoin compounds of the formula II

wherein Z is N or CR_4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A₂ is a linker, G′ is a linker; Q is a linker; and R₂, R_4a, R_4c, and R_h are defined in the specification. The process optionally includes the enantiomeric separation of intermediates to allow preparation of enantiomers of the spiro-hydantoin compounds of formula II. Substituted spiro-hydantoin compounds may be prepared from the spiro-hydantoin compounds of formula II. The spiro-hydantoin compound of formula II and the substituted spiro-hydantoin compounds are useful in the treatment of immune or inflammatory diseases. Also, provided are products made by the instant inventive process and crystalline forms (prepared by any process) of the substituted spiro-hydantoin compound, 5-[(5S, 9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-ylmethyl]-thiophene-3-carboxylic acid, including solvates and salts thereof, as well as methods of use thereof. Crystalline forms of certain intermediates are provided.

This application relates to the use of one or more parasympathomimetic drugs in combination with one or more alpha agonists to create optically beneficial miosis to, for example, temporarily treat presbyopia. The invention provides a pharmaceutical preparation comprising a therapeutically effective amount of one or more parasympathomimetic drugs or cholinesterase inhibitors, or a pharmaceutically acceptable salt thereof, in combination with one or more alpha agonists or antagonists, or a pharmaceutically acceptable salt thereof. The invention further provides for a method for treating, ameliorating or reducing presbyopia of a patient having an eye, comprising administering to said eye a pharmaceutically effective amount of the ophthalmic preparation.

The present invention relates to methods of treating, preventing, or lessening the severity of resistant bacterial infections in mammals, utilizing compounds of formula I or formula VII or pharmaceutically salts thereof. The present invention also relates to methods of using compounds of formula I or formula VII in combination with one or more additional antibacterial agents and/or one or more additional therapeutic agents that increase the susceptibility of bacterial organisms to antibiotics.

Disclosed are compounds having the structure:

wherein Z is —OH or —O•; and

A is:

wherein

• • • X and Y are independently NR₁ or O, where
    • R₁ is H or C₁-C₄ alkyl; and
    • R₂ is H, C₁-C₄ alkyl or t-butoxycarbonyl,
    • wherein W is C₃-C₄ alkynyl; and
    • R₁ is H or C₁-C₄ alkyl, or
    • wherein R₁ is H, C₁-C₄ alkyl, or C₃-C₄ alkynyl; and
      • R₃ is H, OH, O(C₁-C₄ alkyl), or a halogen,

optically active enantiomers, pharmaceutically acceptable salts of the compounds, pharmaceutical compositions containing such compounds or salts, and processes for their preparation. The subject invention also provides methods of alleviating symptoms of neurologic, autoimmune, and inflammatory disorders caused by the presence of reactive oxygen species, methods of preventing oxidation of lipids, proteins, or deoxyribonucleic acids on a cellular level, and methods of protecting human red blood cells from lysis by O₂ radicals.

The present invention refers to the use of phthalimide and/or sulphonamide derivatives with nitric oxide donor properties, which have important activities in increasing the gamma-globin gene expression and anti-inflammatory and analgesic activities, effective in the treatment of hematologic diseases which require reducing the TNF-α levels and an exogenous source of nitric oxide. More particularly, the present invention describes the use of such phthalimide and/or sulphonamide derivatives for the treatment of sickle-cell disease. The invention also has as a novel characteristic the disclosure of new functionalized phthalimide derivatives designed from the prototypes thalidomide and hydroxyurea, and designed rationally through the strategy of molecular hybridization for the treatment of said diseases. The invention still discloses a new method for obtaining a specific sulphonamide derivative which can be used in the preparation of a drug for the treatment of diseases which require reducing the levels of the TNF-α factor and an exogenous source of nitric oxide.

Disclosed are compounds based on lactone ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.

The present invention provides a compound of Formula (I) or pharmaceutical acceptable thereof, wherein ‘R’ is herein described. In addition, the invention relates to composition comprising effective therapeutic amount of compound of formula (I) and methods of using the compounds for treating or prevention disorder such as nonalcoholic fatty liver disease (NAFLD) including fatty liver (steatosis), nonalcoholic steatohepatitis (NASH), and cirrhosis (advanced scarring of the liver).

The present invention is to provide an imidazolidinedione derivative and oxazolidinedione derivative represented by the following general Formula (I) having the chymase and/or tryptase inhibition activity [wherein R<1 >and R<2 >are the same or different, and denote a lower alkyl group or a phenyl group, or R<1 >and R<2 >are taken together to form a ring, R<3 >denotes an optionally substituted naphthyl group or heterocyclic group, A denotes oxygen or NR<4 >(R<4 >is hydrogen or optionally substituted lower alkyl group), or NB<2>R<5 >(R<5 >is aryl group, and B<2 >is carbonyl group or sulfonyl group), and B<1 >denotes a carbonyl group or a sulfonyl group], or a pharmaceutically acceptable salt thereof.

The presently disclosed subject matter relates generally to the fields of molecular biology and medicine. More particularly, it concerns methods involving the use of GSK3 inhibitors in combination with radiation therapies. In some embodiments, administration of a GSK3 inhibitor to a subject results in an amelioration of cognitive decline, toxicity to vascular endothelial cells, and/or neuron death associated with radiation therapy alone.

The subject invention is directed to a pharmaceutical composition comprising an open matrix network carrying a pharmaceutically active ingredient, wherein the open matrix network comprises both the polysaccharides levan and inulin.

A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the following general formula (I):

wherein X represents a single bond or a C₁ to C₆ alkylene group which may be substituted; A represents a C₁ to C₆ alkyl group which may be substituted, a C₆ to C₁₀ aryl group which may be substituted, or a 4 to 10-membered monocyclic or bicyclic and unsaturated, partly saturated, or completely saturated heterocyclic group which may be substituted, wherein said heterocyclic group comprises as ring-constituting atoms 1 to 4 hetero atoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom.

In part, the present invention is directed to compositions having a FabI inhibitor and at least one other bioactive agent. In another part, the present invention is directed to antibacterial compositions having a compound of formulas I-III and at least one other antibacterial agent.

Methods for producing moxifloxacin hydrochloride compounds having very low levels of impurities are provided. Compounds produced using such methods and pharmaceutical compositions including such compounds are also provided.

The invention discloses acne-removing liquid containing a tea tree flower extract. The acne-removing liquid comprises the following components in percentage by weight: 20.0-50.0 percent of tea tree flower extract, 0.2-5.0 percent of plant essential oil, 0.5-5.0 percent of a natural plant source antibacterial agent, 0.2-2.0 percent of salicylic acid, 0.2-2.0 percent of vitamin E and the balance of water. The acne-removing liquid disclosed by the invention realizes the purposes of efficient and multi-effect treatment of acnes on the premise of taking natural plant ingredients without toxic and side effects as raw materials at the most extent: 1) inhibiting excessive secretion of sebum, regulating the oil balance of skin, converging oily and acne skin and improving skin immunity; 2) inhibiting the reproduction of propionibacterium acnes and controlling pathogens; 3) controlling inflammation, preventing the destruction of a hair follicle sebaceous gland structure and reducing the acnes; 4) desalting and removing the acnes, and improving the moisturizing effect of the skin; 5) adopting an antibacterial agent and a preservative serving as natural plants to reduce skin allergy symptoms.