Abstract: The fumaric acid salt of 2-{3-[4-(2-t-butyl-6-trifluoromethyl-4-pyrimidinyl)-1-piperazinyl]propylthio}-4-pyrimidinol is useful for treating disorders which respond to dopamine D3 ligands. It has higher stability at low pH and is therefore particularly suitable for oral administration in pharmaceutical compositions comprising this salt.

Abstract: The present invention provides structure-based combinatorial libraries of compounds containing the functional group minima of picornaviruses including poliovirus and rhinovirus. The libraries can be used to screen for therapeutical antiviral compounds, e.g., anti-picornaviral capsid-binding compounds.

Abstract: This invention relates to compounds which are IP receptor antagonists and which are represented by Formula (I): 1

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.

Abstract: Treatment of Protozoan Infections with new diphenylurea derivatives.

Abstract: Piperazinylalkylthiopyrimidine derivatives of formula (I), a process for preparing them, and pharmaceutical compositions containing them as active substances. The compounds are useful for the treatment of central nervous system disorders, especially anxiety.

Abstract: Novel pyridin-4-yl or pyrimidin-4-yl substituted pyridine compounds and compositions for use in therapy.

Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):

Abstract: Anti-diarrheal, anti-secretory, nitric oxide agonist, nitric oxide synthase activating or gastrointestinal anti-spasmodic compounds of the formula:  R1—N1H—(CH2)3—N2H—(C2)3—N3H—(CH2)4—N4H—(CH2)3—N5H—(CH2)3—N6H—R6  (II); or wherein: R1 and R6 may be the same or different and are H, alkyl or aralkyl having from 1 to 12 carbon atoms; R2-R5 may be the same or different and are H, R1 or R6; R7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms; m is an integer from 3 to 6, inclusive; and n is an integer from 3 to 6, inclusive; or (IV) a salt thereof with a pharmaceutically acceptable acid; and a pharmaceutically acceptable carrier therefor. Methods of treatment utilizing the composition are also disclosed.

Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula 1

Abstract: The invention relates to compounds represented by the following general formula (1): wherein A is an aromatic compound which may be substituted, or the like, B is a nitrogen atom or CH, X is a lower alkylene group which may be substituted, or the like, Y is a single bond or the like; Z is a divalent residue of benzene which may be substituted, or the like, and m and n are independently an integer of 1 to 4, and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.

Abstract: The invention relates to novel substituted aryluracils of the formula (I): to processes for their preparation and to their use as crop protection agents.

Abstract: The present invention relates to the use of pyrimidine compounds of the following formula: where R1, R2, R3, A, B and Ar have the meanings indicated in the description. The compounds according to the invention have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.

Abstract: Compounds described by the chemical structural formula or a pharmaceutically acceptable salt thereof, are useful in the treatment of pain, migraine, depression, anxiety, schizophrenia, Parkinson's disease, stroke, and in the treatment of neuropathies including postherpetic neuralgia, central pain from spinal cord injury, and phantom limb pain.

Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) in which the radicals n, Q, R1 to R6 are each as defined in the description, and to processes for this preparation and to their use as herbicides.

Abstract: Novel and efficient syntheses create novel piperazinone intermediates which facilitate the production and use of PNAs. Such syntheses and the products enhance the feasibility of a system which permits the rapid identification of PNA oligomers useful as therapeutics, diagnostics and/or gene characterization tools. A first component of the system is a universal PNA library that most preferably incorporates one or more universal nucleotide bases into carefully selected positions within each oligomer species thereby providing the library with the screening ability of a much larger library. The second component of the system is a high throughput screening system that includes a number of assays designed to provide information on the binding activities of the different PNAs to a target nucleotide sequence (generally, a DNA or RNA sequence).

Abstract: The invention relates to compounds of the formula 1

Abstract: The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods.

Abstract: The invention relates to novel aminouracils of the general formula (I) in which, Q, R1, R2, R3, R4, R5, R6 and R7 are each as defined in the description, to their use as herbicides and to novel intermediates.

Abstract: A group of novel pyrimidone compounds are inhibitors of the enzyme LDL PLA2 and therefore of use in treating atherosclerosis.

Abstract: Compounds of the formula (I) and salts thereof in which R1-R9, W and A are as defined in formula (I) of claim 1 are suitable as herbicides and plant growth regulators. They can be prepared by processes according to claim 5 via intermediates according to claim 9, some of which are novel.

Abstract: (Het)Arylsulfonylureas having an imino function, their preparation, and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof in which A is a (hetero)aromatic or heterocyclic bridge linked to the group SO2 by a direct bond, or via O, S, NH, CH2 or via alkylated NH or alkylated methylene, B is a group having an imino-containing fragment N═C—N, N═C—S, N═C—O or N═C—C which is linked to A by one of the nitrogen atoms of the fragment, R═H or an aliphatic radical, W═O or S and X, Y and Z are as defined in claim 1 are suitable as herbicides and plant growth regulators. The preparation is carried out for example similarly to known processes via novel intermediates of the formula (XII) (cf.

Abstract: There are described cycloalkyl derivatives of the formula (I) R1—Y—A—B—D—E—F—G  (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.

Abstract: Arylpyrimidinone compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided.

Abstract: Compounds of Formula I are disclosed, having activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4, and accordingly useful for treating diseases whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.

Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Abstract: Compounds of formula I, 1

Abstract: The invention relates to substituted phenyluracils of the general formula (I) in which the radicals R1 to R5, Q and n are each as defined in the description, and to processes for their preparation and to their use as herbicides.

Abstract: The invention relates to novel soluble pigment precursors possessing not only higher thermal stability but also improved solubility characteristics and to a process for mass coloration of high temperature polymers that utilizes these novel soluble pigment precursors. The pigment precursors of the invention are essentially of the formula A(B)x  (I) where x is an integer from 1 to 8, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, indanthrone, isoindolinone, isoindoline, dioxazine, azo, phthalocyanine or diketopyrrolopyrrole series, this radical being linked with xB groups via one or more heteroatoms, these heteroatoms being selected from the group consisting of N, O and S and forming part of the radical A, and B is hydrogen or a group of the formula although at least one B group is not hydrogen and when x is from 2 to 8 the B groups may be identical or different.

Abstract: 8,8a-Dihydroindeno[1,2-d]thiazole derivatives which carry in the 2-position a substituent having a sulfonamide structure or sulfone structure; processes for their preparation and their use as medicaments The invention relates to polycyclic dihydrothiazoles and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of formula I, in which the radicals are as defined above, and their physiologically acceptable salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.

Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis.

Abstract: The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.

Abstract: The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are rapidly metabolized by blood and tissue enzymes to form polar metabolites with no hypnotic activity and which are rapidly eliminated.

Abstract: The present invention relates to acylguanidine derivatives of the formula I in which R1, R2, R4, Ar, X and n have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of the formula I are valuable pharmacologically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion. They inhibit, for example, bone resorption by osteoclasts and are suitable for the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example osteoporosis. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceutical preparations, and pharmaceutical preparations comprising them.

Abstract: Diaryl ether compounds useful in the control of weeds are described. An exemplary compound is represented by the general formula (I): In this formula Q is represented by Q9: X and Y represent a hydrogen atom, halogen atom, cyano group, nitro group or (C1-6)haloalkyl group. A1 and A2 are independently oxygen or sulfur atoms. R9 and R10 represent a hydrogen atom, a (C1-6)alkyl group, an acyl group, or a (C1-6)alkylsulfonyl group; or R9 and R10 may form a ring consisting of polymethylene, (CH2)m groups, where m is an integer of 2, 3, 4 or 5, together with the nitrogen atom of NR9R10, which may or may not have a (C1-6)alkyl substituent. Methods of making the compounds are also described.

Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.

Abstract: The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.

Abstract: Disubstituted methylidenehydrazinophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof in which R1 to R6, W, X, Y, Z are as defined in claim 1 and the group R2R3C is a carbon atom which is subsituted by at least one electron-withdrawing radical R2 or R3 are suitable as herbicides and plant growth regulators. They can be prepared in accordance with known processes via intermediates, some of which are novel.

Abstract: Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of proteins tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.

Abstract: Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of protein tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.

Abstract: The novel compounds of formula I: (A, B, R1, R2, R3, X and m are defined in the specification) show selective herbicidal activity. The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.

Abstract: 2-(O-[pyrimidin-4-yl]methylenoxy)phenylacetic acid derivatives of the general formula I and the salts and N-oxides thereof where the radicals R1 to R4 and Q have the following meanings: R1 is hydrogen or alkyl; R2 is halogen, alkyl or haloalkyl; R3 is hydrogen; amino; hydroxyl; mercapto; halogen; unsubstituted or phenyl-substituted alkyl; haloalkyl; alkoxyalkyl; alkoxy; monoalkylamino; dialkylamino; alkylthio; alkylsulfoxyl; alkylsulfonyl; cycloalkyl; trialkylsilyloxy, or: phenyl, phenoxy, phenoxymethyl, benzyloxy or hetaryl, unsubstituted or substituted in the aromatic ring; R4 is hydrogen; cyano; halogen; alkyl; haloalkyl or alkoxy; Q is C(═NOCH3)—CONHCH3, C(═NOCH3)—COOCH3 or N(OCH3)—COOCH3, the salts and N-oxides thereof, and their use for controlling harmful fungi and animal pests.

Abstract: The present invention relates to a novel pyrimidinone compounds and the pharmaceutical acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, thereby, being useful in treating cardiovascular disease caused by binding angiotensin II to its receptor.

Abstract: The fumaric acid salt of 2-{3-[4-(2-t-butyl-6-trifluoromethyl-4-pyrimidinyl)-1-piperazinyl]propylthio}-4-pyrimidinol is useful for treating disorders which respond to dopamine D3 ligands. It has higher stability at low pH and is therefore particularly suitable for oral administration in pharmaceutical compositions comprising this salt.

Abstract: The invention relates to substituted phenyluracils of the general formula (I) in which the radicals R1 to R5, Q and n are each as defined in the description, and to processes for their preparation and to their use as herbicides.

Abstract: Compounds of formula A(B)x  (I), wherein x is an integer from 1 to 8, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, indanthrone, isoindolinone, isoindoline, dioxazine, azo, phthalocyanine or diketopyrrolopyrrole series that is bonded to x groups B via one or more hetero atoms, those hetero atoms being selected from the group consisting of N, O and S and forming part of the radical A, each group B independently of any other(s) is hydrogen or a group of the formula  at least one group B being a group of the formula The compounds according to the invention are used in high-molecular-weight organic materials, thermo-, photo- or chemo-sensitive recording materials, light-sensitive negative or positive resist compositions, ink compositions for ink-jet printing and color tapes for thermal transfer printing.

Abstract: The invention provides compounds of the formula wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R1 and R2 may together be —CH═CH—CH═CH—, wherein R1 and R2 together with the two carbon ring atoms to which they are attached form a fused ring; R3 is halogen, trifluoromethyl, lower alkyl or lower alkoxy; R4/R4′ are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, phenyl, hydroxy-lower alkyl, cyano-lower alkyl, carbamoyl-lower alkyl, pyridyl, pyrimidyl, —(CH2)n-piperazinyl, which is optionally substituted by one or two lower alkyl groups or by hydroxy-lower alkyl, —(CH2)n-morpholinyl, —(CH2)n-piperidinyl, —(CH2)n+1-imidazolyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl or —O&

Abstract: Compositions capable of simultaneous two-photon absorption and higher order absorptivities are disclosed. Many of these compositions are compounds satisfying the formulae D-Π-D, A-Π-A, D-A-D and A-D-A, wherein D is an electron donor group, A is an electron acceptor group and Π comprises a bridge of &pgr;-conjugated bonds connecting the electron donor groups and electron acceptor groups. In A-D-A and D-A-D compounds, the &pgr; bridge is substituted with electron donor groups and electron acceptor groups, respectively. Also disclosed are methods that generate an electronically excited state of a compound, including those satisfying one of these formulae. The electronically excited state is achieved in a method that includes irradiating the compound with light. Then, the compound is converted to a multi-photon electronically excited state upon simultaneous absorption of at least two photons of light.

Abstract: This invention provides a drug which has inhibitory activities against thymidine phosphorylase and inhibits metastasis of a cancer. Specifically, this invention relates to a cancerous metastasis inhibitor comprising, as an active ingredient, a uracil derivative represented by the following formula (1): wherein R1 represents a chlorine, bromine or iodine atom or a cyano or lower alkyl group and R2 represents a substituted or unsubstituted 4-8 membered hetero-cyclic group having nitrogen atoms or a substituted or unsubstituted amidinothio, guanidino, (lower alkyl)amidino, amino or like group, or a salt thereof.

Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to processes for their preparation, to novel intermediates and to their use as herbicides.