Abstract: This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.

Abstract: This invention relates to compounds of formula (I): their compositions and methods of use thereof. The compounds (and compositions) are useful in modulating IL-12 production and processes mediated by IL-12.

Abstract: The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, infections, and certain immunological disorders.

Abstract: Compositions and methods for tissue-specific targeted delivery of therapeutic agents through the use of tissue-specific peptidomimetic ligands are disclosed herein. The ligand comprises a composition of formula A-scaffold-A? and one or more hydrophobic anchors covalently linked to the scaffold. The A and A? compounds linked to the scaffold comprise monovalent peptidomimetic compounds wherein each monovalent peptidomimetic compound is selected from the group consisting of fragments IKs, GKs, IDs, GSs, GTs, VSs, TKs, KTs, ARs, KIs, KEs, AEs, GRs, YSs, IRs, and morpholino.

Abstract: Provided herein are substituted pyrimidine and triazine derivatives, including bicyclic pyrimidine derivatives, their pharmaceutical compositions, their preparation, and their use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs. In one embodiment, the pyrimidine and triazine derivatives are morpholino-pyrimidine, morpholino-triazine, pyridyl-pyrimidine, and pyridyl-triazine derivatives which are selective irreversible inhibitors of the p110? isoform of PI3K.

Abstract: Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazoles of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.

Abstract: Synthesis of biguanidines and triazines, and biguanidino-aluminium complexes as intermediates Compounds of formula (I) or salts thereof, in which R1, R2, R3, R4, R5, R6, X and Y are defined as in claim 1, can be prepared by a process characterized in that a compound of the formula (II) or a salt thereof, is reacted to a compound of the formula (III) or a salt thereof, and an aluminium (III) source, optionally, in the presence of a protic additive or solvent selected from the group consisting of alcohols or amines. The compounds (I) are suitable to be used for the preparation of heterocyclic compounds corresponding to (I) where the group Al(X)(Y) is replaced with an optionally substituted carbon atom, or s-triazine derivatives thereof.

Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.

Abstract: A novel method for immunosuppressive in a mammal suffering from an immune disease, including administering to the mammal a therapeutically effective amount of a heterocyclic compound represented by the general formula (I) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is disclosed. A novel heterocyclic compound represented by the general formula (II) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is also disclosed.

Abstract: Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae IA, IB, and IC, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.

Abstract: The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, R5a, R6a A, B, Y, x, and m are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents.

Abstract: Compounds of formula (I): A-B—C and isomers, salts, solvates, chemically protected forms, and prodrugs thereof wherein: B is selected from the group consisting of formula (i) where RN is H or Me; or B is a divalent C5 heterocyclic residue containing one or two ring heteroatoms; A is formula (ii) RA3 and RA5 are independently selected from halo, ORO and RAC, where RO is H or Me, and RAC is H or C1-4 alkyl; XA is selected from N and CRA4, where RA4 is selected from H, ORO, CH2OH, CO2H, NHSO2Me and NHCOMe; RA2 and RA6 are independently selected from H, halo and ORO; or RA3 and RA4 together with the carbon atoms to which they are attached, or RA2 and RA3 together with the carbon atoms to which they are attached, may form a C5-6 heterocylic or heteroaromatic ring, containing at least one nitrogen ring atom; where if X is not N, 1, 2, or 3 of RA2 to RA6 are not H; C is formula (iii) where X is selected from N and CH, Y is selected from N and CH, and Z is selected from N and CRC6; RC3 is selected from H, halo and an

Abstract: A compound of formula (I), or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein M1, M2, L1, L2, W1, W2, X1, X2, Y1, Y2, A, R5 and R5a are as defined herein for the for treatment of conditions treatable by the blockade of an epithelial sodium channel, particularly conditions benefiting from mucosal hydration.

Abstract: Preparing dyes suitable for cosmetic use that start with known dyes and link them, for example, with 1,3,5 triazine to bulky organic groups that control solubility.

Abstract: The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention.

Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, and Ar are as defined in the specification and claims, or to pharmaceutically active acid addition salts of such compounds. Compounds of formula I are modulators for amyloid beta and may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

Abstract: Provided is a proton-conducting compound which provides proton conductivity without humidification and is suitable for electrochemical device materials such as solid electrolytes for fuel cells and electrolytes for batteries. Provided also is a proton-conducting polymer. The proton-conducting compound is composed of a melamine compound salt obtained from a melamine compound represented by the following formula (1) and a Bronsted acid and the proton-conducting polymer is obtained by homopolymerizing or copolymerizing the melamine compound salt. In formula (1), R1, R2, R3, R4, and R5 each is independently an alkyl group, an aryl group, an alkenyl group, a heterocyclic group, or a hydrogen atom; at least one of them is a group other than hydrogen; R2 and R3 or R4 and R5 may join together to form a heterocyclic structure; and the alkyl group, the aryl group, the alkenyl group, or the heterocyclic group may have a substituent.

Abstract: For the separation, removal, isolation, purification, characterisation, identification or quantification of fibrinogen or a protein that is a fibrinogen analogue, an affinity adsorbent is used that is a compound of formula II wherein one X is N and the other is N, C—Cl or C—CN; Y is O, S or NR2; 0 Z is O, S or NR3; R2 and R3 are each H, alkyl, hydroxyalkyl, benzyl or &bgr;-phenylethyl; n is 0 to 6; A is a support matrix, optionally linked to the triazine ring by a spacer; R7 is a group bearing a positive charge at neutral pH; W is an optional linker; V is an aromatic group; and R8 and R9 are each H, OH, alkyl, alkoxy, amino, NH2, acyloxy, acylamino, CO2H, sulphonic acid, carbamoyl, sulphamoyl, alkylsulphonyl or halogen or a cyclic structure such as a morpholino group, or R8 and R9 are linked to form such a cyclic structure.

Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.

Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.

Abstract: Compounds consisting of an oligomer or a polymer of a 1,3,5-triazine derivative, having the general formula I: wherein: X is selected from: or X is a heterocyclic radical containing in the ring at least one nitrogen atom which radical is linked to the triazine ring through one of such nitrogen atoms, R2 is alkyl or cycloalkyl, R1 is a divalent radical of piperazine of the formula or R2 is a divalent radical according to the formula or R2 is a radical according to the formula Y n is an integer from 2 to 30, inclusive, m is an integer from 2 to 6, inclusive, p is an integer from 2 to 12, inclusive, and X1?OH,NH2 or X whereby X and X1 may be the same or different, and, X2?H or is a C1-C4 alkyl group, and a solvent-free process for the production of the compounds of Formula I as well as the use of the self-extinguishing oligomeric or polymeric compounds as flame retardants and light stabilizers in thermoplastic polymers such as polypropylene or regenerated cellulose or polyester.

Abstract: Compounds represented by formula (1) shown below, pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising such compounds are provided.

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Abstract: The present invention relates to a compound having the formula where Z is an amine, phenoxy, or thiol-containing group, and Y is an alkyl-containing amine. Methods of producing such compounds and using them to treat patients with diabetes and obesity are also disclosed. The present invention also relates to treating such conditions with GADPH inhibitors and screening compounds useful for treating such conditions by using GADPH inhibitors. Compounds can also be screened for their effectiveness in modulating diabetes and obesity with a C. elegans strain.

Abstract: A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof: and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.

Abstract: This invention relates to a method of preparing mesylate salts of compounds that inhibit IL-12, IL-23 and/or IL-27 production.

Abstract: A composition comprising an organic fluorophore having a structure of: or a derivative thereof; as well as articles of manufacture marked with the fluorophore, methods for marking articles with the fluorophore, and methods for producing a fluorescent fiber.

Abstract: (1,3,5)-Triazinyl phenyl hydrazones are effective at controlling insects.

Abstract: A process for the separation of biological materials, such as dye-ligand affinity chromatography, wherein an adsorbent is used, which comprises a reaction product of certain reactive anthroquinone compounds and a substrate having a group capable of reaction with a reactive group in said reactive anthroquinone compounds to form a covalent bond.

Abstract: Compounds of the formula (I) or salts thereof, in which in which R1 is an optionally substituted amino group or analogous group, and R2 to R7 are each as described herein, are suitable as herbicides and crop growth regulators. The compounds (I) can be prepared by the processes described, via intermediates including novel intermediates for example of the formula (III).

Abstract: The present invention concerns concentrated aqueous solutions of anionic disazo dyes, comprising salts and or the free acids of anionic dyes of the formula and 2-(2-butoxyethoxy) ethanol wherein the substituents are each as defined in claim 1 and the use of these solutions for dyeing and/or printing hydroxyl-containing substrates and for producing inkjet inks.

Abstract: The invention provides for Triazine derivatives and their use to modulate protein kinase activity in a variety of conditions and diseases.

Abstract: The present invention provides visible light sensitive and ultraviolet (UV) light sensitive composition for DNA transfer comprising acid sensitive polyacetals developed as DNA/RNA delivery agents, a photoacid generator and optionally a photosensitizer.

Abstract: The present invention relates to a method of reducing the total organic carbon (TOC) content of waste water in the course of the preparation of concentrated solutions or suspensions of anionic organic compounds, which method comprises increasing the concentration of an aqueous solution or suspension of an anionic organic compound in the form of its free acid or its alkali metal salt, having a salt content of less than 5% of extraneous salt by weight based on the total solution or suspension, by microfiltration, ultrafiltration and/or nanofiltration, a) the membrane pore size being so selected that compounds having molecular weights in the range from 300 to 1000 Daltons or higher are retained, and b) the content of anionic compound in the concentrate being so adjusted to from 10 to 50% by weight that the total organic carbon (TOC) content of the permeate is less than 0.

Abstract: Compounds of Formula 1 [Region ?]?[Region ?]?[Region ?]?[Region ?] ??(I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.

Abstract: The present invention relates to pyrazolotriazines according to formula (I) and stereoisomers, isomers and salts thereof wherein R1-R5 are selected from certain alkyl, aryl and heteroaryl species as defined in the specification wherein all of the compounds are useful as CRF antagonists and are thus useful in the treatment of neurological disorders as well as a multitude of other CRF associated diseases or conditions.

Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, HET is an N-linked 5-membered, fully or partially unsaturated heterocyclic ring, or HET is an N-linked 6-membered di-hydro-heteroaryl ring; Q is, for example, Q1 or Q2: wherein R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example a group of the formula (TC7) wherein Rc is, for example, hydrogen, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.

Abstract: The present invention pertains to luminescent dyes and methods for covalently attaching the dyes to a component or mixture of components so that the components may be detected and/or quantified by luminescence detection methods. The dyes are cyanine and cyanine-type dyes that contain or are derivatized to contain a reactive group. The reactive group is covalently reactive with amine, hydroxy and/or sulfhydryl groups on the component so that the dye can be covalently bound to the component. In addition, the dyes are preferably soluble in aqueous or other medium in which the component is contained. The components to be labeled can be either biological materials, such as antibodies, antigens, peptides, nucleotides, hormones, drugs, or non-biological materials, such as polymers, glass, or other surfaces. Any luminescent or light absorbing detecting step can be employed in the method of the invention.

Abstract: The present invention pertains to luminescent dyes and methods for covalently attaching the dyes to a component or mixture of components so that the components may be detected and/or quantified by luminescence detection methods. The dyes are cyanine and cyanine-type dyes that contain or are derivatized to contain a reactive group. The reactive group is covalently reactive with amine, hydroxy and/or sulfhydryl groups on the component so that the dye can be covalently bound to the component. In addition, the dyes are preferably soluble in aqueous or other medium in which the component is contained. The components to be labeled can be either biological materials, such as antibodies, antigens, peptides, nucleotides, hormones, drugs, or non-biological materials, such as polymers, glass, or other surfaces. Any luminescent or light absorbing detecting step can be employed in the method of the invention.

Abstract: The present invention pertains to luminescent dyes and methods for covalently attaching the dyes to a component or mixture of components so that the components may be detected and/or quantified by luminescence detection methods. The dyes are cyanine and cyanine-type dyes that contain or are derivatized to contain a reactive group. The reactive group is covalently reactive with amine, hydroxy and/or sulfhydryl groups on the component so that the dye can be covalently bound to the component. In addition, the dyes are preferably soluble in aqueous or other medium in which the component is contained. The components to be labeled can be either biological materials, such as antibodies, antigens, peptides, nucleotides, hormones, drugs, or non-biological materials, such as polymers, glass, or other surfaces. Any luminescent or light absorbing detecting step can be employed in the method of the invention.

Abstract: This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 are each independently selected from hydrogen; hydroxy; amino; optionally substituted C1-6alkyl; C1-6alkyloxy; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; Ar1; mono- or di(C1-6alkyl)amino; mono- or di(C1-6alkyl)-aminocarbonyl; dihydro-2(3H7)-furanone; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-6alkyl)amino-C1-4alkylidene; R3 is hydrogen, Ar1, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, C1-6alkyl substituted with C1-6alkyloxycarbonyl; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C1-10alkyl; C3-10alkenyl; C3-10alkynyl; C3-7cycloalkyl; Ar1 is optionally substituted phenyl; for the manufacture of a medicine for the treatment o

Abstract: A method of improving the stability of a quaternary ammonium salt and a method of efficiently preparing the quaternary ammonium salt having improved stability.

Abstract: Sterically hindered N-substituted aryloxyamines are prepared by the Keggin polyoxometalate or the transition metal substituted polyoxometalate (TMS-POM) catalyzed decomposition of diazonium salts in the presence of a sterically hindered nitoxyl radical. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.

Abstract: Biphenyl-substituted triazines of the formulae which are notable for high thermal stability, are used as stabilizers for organic polymers to counter damage thereto caused by light, oxygen and heat, as light stabilizers for textile fiber materials and as sunscreens for the human skin.

Abstract: The present invention provides for compounds of formula (I), (Ia) and (Ib) 1

Abstract: Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the formula IA and or IB:

Abstract: A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.

Abstract: The invention relates to triazines and the use thereof to inhibit lysophosphatidic acid acyltransferase &bgr; (LPAAT-&bgr;) activity. The invention further relates to methods of treating cancer using said triazines. The invention also relates to methods for screening for LPAAT-&bgr; activity.

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.