Abstract: The present invention relates to therapeutically active novel aminoindanes of formula (I). Also provided is a method of preparing compounds of formula (I), and pharmaceutical compositions comprising the compounds. The novel compounds act as modulators of metabotropic glutamate receptors and, as such, are useful in treating diseases of the central nervous system related to the metabotropic glutamate receptor system.

Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.

Abstract: A description is given of an extrusion process for the preparation of a low-dust stabiliser, using a subcooled melt as granulation liquid, as well as of novel amorphous modifications of different stabilisers, including 2,2′-methylenebis(4-[1,1,3,3-tetramethylbutyl]-6-benzotriazol-2-yl-phenol), and of the &bgr;-crystalline modification of 2-(2-hydroxy-3,5-di-tert-butylphenyl)-5-chlorobenzotriazole and of the preparation thereof. The novel process affords products which are easy to handle and which are flowable, and the novel modifications have advantages as regards their preparation, processing and their use as stabiliser.

Abstract: Compounds of the formula (I) in which R1, R2 and X1 have the meanings given in the specification, modulate metabotopic glotamate receptor function and are useful in treating disorders of the central nervous system.

Abstract: Compounds of formula I or II 1

Abstract: The invention provides a method for preparing a 1-benzotriazolylcarbonate ester of a water-soluble and non-peptidic polymer by reacting a terminal hydroxyl group of a water-soluble and non-peptidic polymer with di(1-benzotriazolyl)carbonate in the presence of an amine base and an organic solvent. The polymer backbone can be poly(ethylene glycol). The 1-benzotriazolylcarbonate ester can then be reacted directly with a biologically active agent to form a biologically active polymer conjugate or reacted with an amino acid, such as lysine, to form an amino acid derivative.

Abstract: Compounds having the formula: wherein R1 represents hydrogen, C1-C20 alkyl which is unsubstituted or substituted by one or more ammonium, mono-, di-, tri or tetra-C1-C12 alkylammonium groups or by one or more sulphonium groups or represents an aralkyl residue having a total of from 7 to 10 carbon atoms and, in which, the aryl group is unsubstituted or substituted by C1-C4alkyl, C1-C4 alkoxy or halogen and Z is a group selected from R2, R3 and R4, independently, representing hydrogen, C1-C4alkyl, C1-C4 alkoxy, halogen, NHCOC1-C4 alkyl or phenyl which is unsubstituted or substituted by. C1-C4 alkyl, C1-C4 alkoxy or halogen, a process for their preparation and use of the compounds of formula (1) as UV-absorbers which have improved absorption spectrum characteristics, superior resistance to exposure to UV light and excellent thermal stability, relative to known benzophenone compounds.

Abstract: The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.

Abstract: The present application describes novel amides and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein these compounds are useful as inhibitors of matrix metalloproteinases, TNF-&agr;, and aggrecanase.

Abstract: A process for the preparation of compounds of formula (I): wherein the general symbols are as defined in claim 1, which comprises reacting a compound of formula (V): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R18 are as defined in claim 1, and R18 is especially nitro, chlorine or bromine, with an azide compound of formula (IX): wherein M and n are as defined in claim 1, especially with sodium azide.

Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof.

Abstract: Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists.

Abstract: The present invention relates to three crystalline solid forms of lansoprazole denominated as forms D, E and F. Processes for preparing these crystalline solid forms of lansoprazole are disclosed.

Abstract: The invention relates to novel biphenyl derivatives of the general formula (I), wherein R4 represents an aromatic heterocycle, and to the physiologically acceptable salts or solvates thereof. The inventive compounds are integrin inhibitors and are used for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections and restenosis following angioplasty or for pathological processes that are maintained or propagated by angiogenesis.

Abstract: Photostable, silylated benzotriazole compounds of formula (I) or (II) where at least one of E1, E2, E5, E8, E9, G2 and G7 is a silylated group; and G2 and/or G7 is an electron withdrawing moiety or E1 is &agr;-cumyl, are both photostable and particularly compatible in high performance coatings such as organopolysiloxanes.

Abstract: A compound of formula 1a 1

Abstract: This invention relates to novel amorphous losartan potassium, novel losartan potassium in a crystalline form that is a hydrate, novel crystalline losartan potassium Form IV and solvates thereof, novel crystalline losartan potassium Form V and solvates thereof, to processes for their preparation, to compositions containing them and to their use in medicine. This invention further relates to a novel process for preparing crystalline losartan potassium Form I and Form II.

Abstract: The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.

Abstract: The present invention relates to compounds of general formula (I), processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory diseases.

Abstract: The present invention relates to novel benzotriazoles of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; s is an integer from 0-5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

Abstract: Novel compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, type 1 diabetes, type 2 diabetes, disorders of the lipid metabolism and obesity.

Abstract: Provided herein are novel heteroaromatic substituted cyclopropanes of the Formula (I): 1

Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented.

Abstract: Alkenyldiarylmethane (ADAM) compounds have been found effective as anti-HIV agents. Novel ADAM compounds, their pharmaceutical formulations and a method of using same to treat viral infections are described.

Abstract: Compounds of formula I or II 1

Abstract: Improved organophotoreceptors have:

Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.

Abstract: This invention describes the new, nonsteroidal gestagens of general formula I 1

Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors.

Abstract: The invention provides a method for preparing a 1-benzotriazolylcarbonate ester of a water-soluble and non-peptidic polymer by reacting a terminal hydroxyl group of a water-soluble and non-peptidic polymer with di(1-benzotriazolyl)carbonate in the presence of an amine base and an organic solvent. The polymer backbone can be poly(ethylene glycol). The 1-benzotriazolylcarbonate ester can then be reacted directly with a biologically active agent to form a biologically active polymer conjugate or reacted with an amino acid, such as lysine, to form an amino acid derivative.

Abstract: The invention provides compounds of formula (I) wherein n, A, R1, R2 and R3 are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.

Abstract: A recording medium having an ink receiving layer comprising a porous pigment and a binder, wherein the ink receiving layer contains at least one benzotriazole compound represented by formula (I): wherein R represents hydrogen atom or an alkyl group; X represents a hydrogen atom, a sodium atom, a potassium atom or a primary, secondary or tertiary amino group. Also disclosed is an aqueous ink composition containing a compound of formula (I) and an ink jet recording method using the recording medium or the aqueous ink composition.

Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.

Abstract: The present invention relates to a method for preparing 5- and 6-halomethyl quinoxalines. The method comprises contacting a 5- or 6-methyl quinoxaline with a halogenating agent in the presence of a radical initiator in a solvent selected from the group consisting of fluorobenzene, difluorobenzenes, trifluorobenzenes, chlorobenzene, dichlorobenzenes, trichlorobenzenes, &agr;, &agr;, &agr;-trifluorotoluene and &agr;, &agr;, &agr;-trichlorotoluene. The invention also relates to preparing 6-bromomethyl quinoxaline with N-bromosuccinimide in the presence of a radical initiator in 1,2-dichloroethane. The method for halogenating benzylic methyl groups may also be employed to halogenate a wide variety of halomethyl heterocyclic compounds.

Abstract: The present invention relates to novel benzotriazoles of the formula I 1

Abstract: This invention provides a method for preparing 2-(2-hydroxyphenyl)-2H-benzotriazole of formula (I) below, consisting of steps of a) performing a first reduction in which hydrazine hydrate is added to a compound of formula (II) below with or without a phase transition catalyst in the presence of solvents which include a nonpolar solvent, water, and an alkaline compound, thereby preparing a compound of formula (III) below, and b) performing a second reduction in which water is added to the compound of formula (III) prepared in step a), and then zinc powder and sulfuric acid are added thereto with or without the phase transition catalyst, wherein, X is halogen or hydrogen, R is hydrogen, C1-C12 alkyl, C5-C8 cycloalkyl, phenyl, or phenyl-C1-C4 alkyl; and R′ is C1-C12 alkyl, C5-C8 cycloalkyl, phenyl, or phenyl-C1-C4 alkyl 1

Abstract: The present invention relates to a method for preparing 5- and 6-halomethyl quinoxalines. The method comprises contacting a 5- or 6-methyl quinoxaline with a halogenating agent in the presence of a radical initiator in a solvent selected from the group consisting of fluorobenzene, difluorobenzenes, trifluorobenzenes, chlorobenzene, dichlorobenzenes, trichlorobenzenes, &agr;, &agr;, &agr;-trifluorotoluene and &agr;, &agr;, &agr;-trichlorotoluene. The method for halogenating benzylic methyl groups may also be employed to halogenate a wide variety of halomethyl heterocyclic compounds.

Abstract: A compound represented by the following general formula: wherein R1 and R2 represent amino groups present at adjacent positions each other on the phenyl ring; R3, R4, R5 and R6 independently represent a C1-6 alkyl group; R7, R8, R9 and R10 independently represent a hydrogen atom, a C1-6 alkyl group, an allyl group, or a halogen atom; R11 represents a hydrogen atom or a C1-18 alkyl group; and X− represents an anion, and an agent for nitric oxide measurement comprising said compound. The compound efficiently reacts with nitric oxide to give a fluorescent compound that emits strong fluorescence by irradiation with excitation light of a long wavelength. This fluorescent compound is characterized in that said compound is detectable in a fluorescence wavelength range hardly influenced by autofluorescence of cells, and its fluorescence intensity is not attenuated under an acidic condition.

Abstract: Compounds with heterocyclic-hydroxyimino-fluorene nuclei that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

Abstract: 1. A 1-naphthol compound represented by formula (I) below: wherein A represents the moiety of a compound having an acidic proton the pKa of a corresponding protonated form (AH) of which is 0 to 14, R1 represents an aliphatic group, aryl group, or heterocyclic group, R2 represents a substituent, n represents an integer of 0 to 5, X represents a hydrogen atom, halogen atom, R11—, R11O—, R11S—, R11OCOO—, R12COO—, R12(R13)NCOO—, R12CON(R13)—, —NO, —NO2, or —N═N—R11, wherein R11 represents an aliphatic group, aryl group, or heterocyclic group, and each of R12 and R13 independently represents a hydrogen atom, aliphatic group, aryl group, or heterocyclic group, and Y represents an oxygen atom or sulfur atom.

Abstract: Novel benzotriazoles of the formula 1

Abstract: Benzotriazole UV absorbers which are substituted at the 5-position of the benzo ring by an electron withdrawing group exhibit enhanced durability and very low loss rates when incorporated into automotive coatings. This is particularly the case when the 3-position of the phenyl ring is also substituted by phenyl or phenylalkyl such as &agr;-cumyl. Compounds where the 5-position of the benzo ring are substituted by perfluoroalkyl such as trifluoromethyl are particularly of interest for both their enhanced durability and for their excellent solubility and excellent color properties in some thermoplastic compositions when the phenyl ring is substituted at the 3-position by hydrogen or tert-alkyl.

Abstract: A novel compound suitable for use as an ultraviolet absorber is provided. Further provided are a resin composition and a coating material each containing the novel compound. A bis(benzotriazolyl phenol) compound represented by the following general formula (1), a resin composition containing the compound, and an ultraviolet-absorbing polymer prepared by copolymerization of the compound: [wherein A represents a methylene group, a (CH3)2C group or a C2H5(CH3)C group; R1 and R6, either identical to or different from each other, represent a hydrogen atom, an alkyl group having 1-4 carbon atoms, an aryl group, an alkoxy group having 1-4 carbon atoms or a halogen atom; R2 and R4, either identical to or different from each other, represent a straight-chain or branched alkylene group having 1-6 carbon atoms; R3 and R5each represents a hydrogen atom or a methyl group; and 1, m and n each indicates 0 or 1].

Abstract: The invention pertains to a process for the preparation of a novel UV absorbing diol of the general formula: 1

Abstract: A catalyst is for use in a reaction using an oxygen-atom-containing reactant and includes a nitrogen-containing heterocyclic compound of the following formula (1): wherein each of R1 and R2 is, identical to or different from each other, a hydrogen atom, a halogen atom, an alkyl group, a haloalkyl group, an aryl group, a cycloalkyl group, a hydroxyl group, an alkoxy group, a carboxyl group, an alkoxycarbonyl group, or an acyl group, and R1 and R2 may be combined to form a double bond or to form an aromatic or non-aromatic ring with the adjacent two carbon atoms, where one or two of heterocyclic ring containing three nitrogen atoms indicated in the formula may be further formed on the R1 or R2, or on the double bond or aromatic or non-aromatic ring formed by R1 and R2; X is an oxygen atom or a hydroxyl group; and Y is a single bond, a methylene group, or a carbonyl group. This catalyst can introduce an oxygen-atom-containing group into an organic substrate under mild conditions.

Abstract: A compound of formula 1a 1

Abstract: Novel benzotriazoles of the formula in which R, X1, X2, X3, X4 and Y have the meanings given in the description, and their acid addition salts and metal salt complexes, a process for the preparation of these substances and their use as microbicides in crop protection and in material protection.

Abstract: The invention provides compounds having the formula: wherein Rf is CnF2n+1—(CH2)m—, wherein n is 1 to 22 and m is 0, or an integer from 1 to 3; X is —CO2—, —SO3—, —CONH—, —O—, —S— a covalent bond, —SO2NR—, or —NR—, wherein R is H or C1 to C5 alkylene; Y is —CH2— wherein z is 0 or 1; and R1 is H, lower alkyl or Rf—X—Yz— with the provisos that when X is —S—, or —O—, m is 0, sand z is 0, n is ≧7 and when X is a covalent bond, m or z is at least 1, and uses thereof.

Abstract: The invention provides a method for preparing a 1-benzotriazolylcarbonate ester of a water-soluble and non-peptidic polymer by reacting a terminal hydroxyl group of a water-soluble and non-peptidic polymer with di(1-benzotriazolyl) carbonate in the presence of an amine base and an organic solvent. The polymer backbone can be poly(ethylene glycol). The 1-benzotriazolylcarbonate ester can then be reacted directly with a biologically active agent to form a biologically active polymer conjugate or reacted with an amino acid, such as lysine, to form an amino acid derivative.

Abstract: An organometallic luminescent material selected from the group consisting of the compounds of formulae (I) to (V) of the present invention can emit blue, green and red lights.