Abstract: The present invention relates to crystalline 2,5-dione-3-(1-methyl-1H-indol-3-yl)-4-[1-(pyridin-2-yl-methyl)piperidin-4-yl]-1H-indol-3-yl]-1H-pyrrole mono-hydrochloride salt, a pharmaceutical formulation containing said salt and to methods for treating cancer and for inhibiting tumor growth using said salt.

Abstract: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein X represents CH or N; represents a C1-C12 alkyl; R2 represents a hydrogen atom, or the like; R? represents a C1-C6 alkyl or the like; q represents 0 or an integer of 1 to 7; Y represents a C1-C6 alkyl or the like; p represents 0 or an integer of 1 to 5; R represents a 2,3-dihydroindolyl or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

Abstract: The compounds of formula (I) in which R1, R2 and R3 have the meanings as given in the description are novel effective PDE2 inhibitors.

Abstract: The present invention is directed to novel compounds of Formula (I) wherein the variables are defined as herein. The compounds of Formula (I) are useful as CRTH2 antagonists and as such would be useful in treating certain conditions and diseases, especially asthma, allergic asthma, allergic inflammation, rhinitis, allergic rhinitis or atopic dermatitis.

Abstract: The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract: The invention pertains to the use of six-membered cyclic phosphates as plant growth regulators and methods for regulating the growth of plants using such compounds.

Abstract: The invention discloses quinazoline derivatives or salts thereof, which possess PDE9-inhibiting activity and are useful as treating agents of dysuria and the like, the derivatives being represented by the formula (I) in the formula, R1 stands for phenyl or aromatic heterocyclic group which are optionally substituted with 1-3 substituents selected from halogen, C1-6 alkyl, C1-6 haloalkyl containing 1-6 halogen atoms and C1-6 alkoxy; and n is an integer of 1-3.

Abstract: This invention discloses 2?-methyl-19-nor-(20S)-vitamin D analogs, and specifically 2?-methyl-19-nor-(20S)-1?-hydroxy-bishomopregnacalciferol and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.

Abstract: This invention provides a method for treating or preventing malaria in a subject. The method includes administering to the subject an effective amount of a substituted tetracycline compound, such that malaria is treated or prevented. In one aspect, the invention relates to pharmaceutical compositions which include an effective amount of a tetracycline compound to treat malaria in a subject and a pharmaceutically acceptable carrier. The substituted tetracycline compounds of the invention can be used to in combination with one or more anti-malarial compounds or can be used to treat or prevent malaria which is resistant to one or more other anti-malarial compounds.

Abstract: The present invention relates to a compound having a leukotriene (particularly leukotriene B4) inhibitory action, and useful for the prophylaxis or treatment of diseases such as allergy, asthma, inflammation, cancer and the like.

Abstract: An improved selective herbicide, as well of methods of controlling unwanted plants using such a herbicide, are provided. A method for treating undesired vegetation can include providing a selective herbicidal composition that includes a water-soluble selective auxin-type herbicide and a chelating agent complexed with at least one transition metal, and contacting vegetation with a herbicidally effective amount of the composition such that unwanted vegetation is controlled, while desired vegetation is unaffected.

Abstract: Compounds of formula (1) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is 2-methyl-1,3-oxazol-4-yl and R4 and R5 together with the notrogen atom to which they are attached represents morpholino, process for their preparation, pharmaceutical compositions containing them and their use in medicine.

Abstract: A composition for attracting male pink hibiscus mealybugs which contains a carrier material or carrier and effective amount of (R)-lavandulyl (S)-2-methylbutanoate and (R)-maconelliyl (S)-2-methylbutanoate. Also a method for attracting male pink hibiscus mealybugs to an object or area, which method involves treating said object or area with effective amount of (R)-lavandulyl (S)-2-methylbutanoate and (R)-maconelliyl (S)-2-methylbutanoate. Cyclobutanes, 2,2-dimethyl-3-(1-methylethylidene)cyclobutanes, having the formula: wherein R1 is hydrogen, a C1-11 straight or branched alcohol, aldehyde, alkyl, ether (e.g. methanol, ethanal, 4-methylhexane, heptyloxymethane), or esters thereof with a C1-10 saturated or unsaturated, straight or branched acid (e.g., formic acid, acetic acid, 2-methylbutyric acid, 3-methyl-2-butenoic acid) and R2 is hydrogen, methyl, C1-10 saturated or unsaturated, straight or branched alkyl (e.g. hexane, isopropenyl, 4-methyl-4-pentene).

Abstract: Disclosed are 1?-hydroxy-2-(3?-hydroxypropylidene)-19-nor-vitamin D compounds, pharmaceutical compositions, and methods of making and treatment thereof. The compounds are generally directed to biologically active 2-alkylidene-19-nor-vitamin D compounds and analogs thereof characterized by the presence of a 3?-hydroxypropylidene moiety at C-2 and the presence of an abbreviated alkyl side-chain free of any hydroxyl moiety.

Abstract: The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: The present invention relates to an isoxazoline derivative having the cyclic carboxylic acid hemiketal moiety of formula (1) for use as caspase inhibitor, a process for preparing it, and a pharmaceutical composition comprising it.

Abstract: The invention relates to novel tetrahydro-1H-carbazole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to patients.

Abstract: There is provided a compound of Formula I wherein X is a ring system; R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; R2 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein when X is a steroidal structure and both of R1 and R2 are sulphamate groups, the steroidal ring system (X) represents an oestrogen; and wherein said compound is capable of inhibiting steroid sulphatase (STS) activity and/or is capable of acting as a modulator of cell cycling and/or as a modulator of apoptosis and/or as a modulator of cell growth.

Abstract: Compounds of formula 1 are provided where X1, X2, and X3 are independently selected from H or hydroxy protecting groups, and R1 and R2 have the definitions provided herein. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.

Abstract: The present invention relates to the use of 2-alkoxyestrogen sulfamates of general formula I wherein R1 and R2 independently represent H, methyl, C1-C4 acyl, benzoyl R3 represents C1-C4 alkyl or a group of formula CnFmHo, wherein n=1, 2, 3, 4, 5 or 6, m>1, and m+o=2n+1, R4 and R5 in each case represent H or, together, a methylene group or an additional double bond, R6 represents H, R7 represents OH, OC1-C4-alkyl, OC1-C11-acyl or OSO2NR1R2, the dashed lines in the B and C rings of the steroid skeleton additionally representing up to two double bonds, for the production of a medical drug for the treatment of tumor diseases which can be affected positively by inhibiting the tubulin polymerization. The inventive compounds are distinguished by the 2-alkoxy substitution in conjunction with the 17-hydroxy substitution. They have a special effect with regard to inhibiting tubulin polymerization and can be used, for example, for the treatment of prostate cancers.