Abstract: The present invention relates to compounds of formula 1, wherein R1, R2, R3 and R4 are defined as in the specification. These compounds are useful as psychotherapeutic agents.

Abstract: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-4 alkoxy optionally substituted by one or more fluorine atoms; R3 represents a 5- or 6-membered heterocyclic ring, the ring being optionally substituted; R4 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent,  or represents a cyclic group of formula Ia,  or represents a chain of formula Ib, and pharmaceutically acceptable salts thereof; are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.

Abstract: This invention provides compounds of Formula (I), having the structure where T, Z, X, A, R1, R2a, R2b, R2c, R3, R4, and n are defined herein, or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of osteoporosis and polycystic kidney disease.

Abstract: NPY antagonists, methods of using such NPY antagonists and pharmaceutical compositions containing such NPY antagonists. The NPY antagonists are useful for the treatment of NPY mediated disease/conditions including obesity.

Abstract: Fuel additives comprise a compound having a group represented by the formula >C═=N—  (1). Also disclosed are fuel compositions containing such additives. The additives have a superior detergent effect to conventional gasoline detergents and an excellent detergency of the injection nozzles of a diesel engine and is free from being sludge.

Abstract: Novell IL-8 compounds and methods of using them are provided.

Abstract: The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme.

Abstract: The invention relates to novel inhibitors of human tryptase which are used in the pharmaceutical industry for the production of medicaments.

Abstract: Compounds of formula (I) in which the substituents and symbols have the meanings indicated in the description, are suitable for the control of Helicobacter bacteria.

Abstract: A process for the preparation of organomagnesium compounds from organic halides and magnesium metal in the presence of transition metal catalysts using an activity-enhancing main group metal component. The latter is a compound of a metal of Periodic Table groups 1, 2 or 13 in which elements of Periodic Table groups 14-17 or hydrogen are bonded to the metal. Some of these additional components may also be formed in situ.

Abstract: A method is provided for evaporating cyclohexanone oxime in which cyclohexanone oxime is evaporated using a falling-film evaporator with wetting the evaporation surface of the evaporator well with the cyclohexanone oxime at a pressure of less than about 1060 Torr with a falling rate of the cyclohexanone oxime of about 170 kg/hour or more per one meter around the circumference of evaporation surface at the lowest part of the evaporator. In this method, the cyclohexanone oxime is evaporated efficiently with little decomposition thereof, while preventing the plugging of the pipes of the evaporator and continuously carrying out the operation of the evaporator for a long period of time.

Abstract: The present invention is directed to novel heterocyclic substituted pyrazolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.

Abstract: Novel thiol derivatives of formula I or of the formula Ia wherein the variables have the meanings as defined hereinbefore.

Abstract: An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, cell adhesion inhibitory activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and, therapeutic agents for treating cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases and the like and for inhibiting platelet aggregation.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as vitronectin 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: The invention relates to novel monobenzenic dyes including at least one cationic group Z, Z chosen from quaternized aliphatic chains, aliphatic chains including at least one quaternized saturated ring and aliphatic chains including at least one quaternized unsaturated ring, to their use as oxidation-dye precursors for the oxidation-dyeing of keratin fibers, to dye compositions containing them and to oxidation-dyeing processes using them.

Abstract: An electrolyte composition comprising a compound represented by the following general formula (1): wherein R represents a substituent containing a —(CR1R2—CR3R4—O)n— bond (in which R1 to R4 are independently a hydrogen atom or an alkyl group, n being an integer of 2 to 20); Q represents an atomic group forming an aromatic cation having a 5- or 6-membered ring structure with a nitrogen atom, which may have a substituent; and X− represents an anion. A photoelectric conversion device comprising the electrolyte composition and a photo-electrochemical cell composed thereof are also provided.

Abstract: Novel compounds of the formula I which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 2-(3,5-Dichlorophenyl)-7-(R*)-phenyl-7a-(R*)-tetrahydropyrrolo[1,2-c]imidazole-1,3-dione; 2-(3,5-Dichlorophenyl)-7a-(R*)-methyl-7-(R*)-phenyl-tetrahydropyrrolo[1,2-c]imidazole-1,3-dione; and, 7-(R*)-(4-Bromophenyl)-2-(3,5-dichlorophenyl)-7a-(R*)-tetrahydropyrrolo[1,2-c]imidazole-1,3-dione.

Abstract: Described are benzoxazine and benzothiazine compounds of the formula I defined herein, methods for their preparation and methods for their use in pharmaceuticals based on their activity as NO-synthases (NOS) inhibitors.

Abstract: Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.

Abstract: Compounds according to Formula (I) or a salt thereof are selective ligands for GABAA receptors useful for treatment of disorders of the central nervous system:

Abstract: Amide derivatives represented by general formula (I) or salts thereof wherein each symbol has the following meaning: ring B: an optionally substituted heteroaryl optionally fused with a benzene ring; X: a bond, lower alkylene or lower alkenylene optionally substituted by hydroxy or lower alkyl, carbonyl, or a group represented by —NH— (when X is lower alkylene optionally substituted by lower alkyl which may be bonded to the hydrogen atom bonded to a constituent carbon atom of ring B to form lower alkylene to thereby form a ring); A: a lower alkylene or a group represented by -(lower alkylene)—O—; R1a and R1b: the same or different and each hydrogen or lower alkyl; R2: hydrogen or halogeno; and Z: nitrogen or a group represented by ═CH—.

Abstract: The present invention relates to compounds of formula (I), wherein Ar1 represents (A) and (B) or (C); R12 and R13 are independently hydrogen or C1-4alkyl; Ar2 is phenyl or heteroaryl; p is 0 or 1; Ar3 is phenyl, pyridinyl, pyridazinyl, pyrimidyl or pyrazynyl, the ring being substituted on ring carbon atoms by R2 and —(CH2)nR3, and wherein Ar3 is attached to Ar1C(R12)R13CH(Ar2)O— by a ring carbon atom; R2 is a group of formula (2), or R2 represents a lactone of formula (3), the group of formula (2) or (3) having L or D configuration at the chiral alpha carbon in the corresponding free amino acid; n is 0, 1 or 2; R3 is phenyl or heteroaryl; and R5-R9, m and n are as defined in the specification; or a pharmaceutically acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use in cancer therapy.

Abstract: Compositions having a texaphyrin-lipophilic molecule conjugate loaded into a biological vesicle and methods for imaging, diagnosis and treatment using the loaded vesicle are provided. For example, liposomes or red blood cells loaded with a paramagnetic texaphyrin-lipophilic molecule conjugate have utility as a blood pool contrast agent, facilitating the enhancement of normal tissues, magnetic resonance angiography, and marking areas of damaged endothelium by their egress through fenestrations or damaged portions of the blood vascular system. Liposomes or cells loaded with a photosensitive texaphyrin-lipophilic molecule conjugate can be photolysed, allowing for a photodynamic therapy effect at the site of lysis. Availability of red blood cells loaded with a photosensitive texaphyrin-lipophilic molecule conjugate provides a method for delivering a photodynamic therapeutic agent to a desired site with a high concentration of oxygen.

Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Rx, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

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: Provided are liquid crystalline compounds having excellent physical properties and being excellent in miscibility with other liquid crystal materials; liquid crystal compositions comprising the crystalline compound; and liquid crystal display device fabricated by using the liquid crystal composition; the liquid crystalline compounds being specific chlorobenzene derivatives expressed by the general formula (1) Ra—A1—Z1—A2&Parenopenst;Z2—A3&Parenclosest;m&Parenopenst;Z3—A4&Parenclosest;nRb  (1) wherein Ra, Rb, A1 to A4, Z1 to Z3, m, and n are herein defined.

Abstract: Disclosed are novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions. Also disclosed are processes of making such compounds.

Abstract: This invention provides a novel class of substituted 6(5H)phenanthridinone compounds. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable salt, hydrate, prodrug, or mixture thereof are also described.

Abstract: Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Abstract: Compounds of the formula (I): are vitronectin receptor antagonists useful in the treatment of osteoporosis.

Abstract: The present invention relates to the use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: A process is provided for the preparation of a compound of formulae (IA) (sidenafil) and (IB) comprising reacting a compound of formula (IIA) and (IIB) respectively in the presence of —OR, wherein R in the case of formation of compound (IA) is CH2CH3 and R in the case of formation of compound (IB) is CH2CH2CH3, where X is a leaving group:

Abstract: Substituted 1H-Pyridinyl-2-ones are useful as GABAA-Alpha 2/3 ligands.

Abstract: The present invention pertains to new aminophenol derivatives of the following general formula (1), their preparation and their use as fungicides. wherein Y1, Y2, Y3, Y4, R1, and Z are as defined in the description.

Abstract: This invention is in the field of the chemistry of targeting anticancer anthracycline derivatives. More particularly, it concerns doxorubicin (DOX) or its daunosamine modified derivatives (DM-DOX) linked covalently to analogs of peptide hormones such as LH-RH, bombesin and somatostatin. These covalent conjugates are targeted to various tumors bearing receptors for the peptide hormone analogs. The compounds of this invention are represented by General Formula Q14—O—R—P wherein Q has the general formula wherein: Q14 signifies a Q moiety with a side chain at the 14 position, R— is H or —C(O)—(CH2)n—C(O)— and n=0-7, R′ is NH2 or an aromatic, saturated or partially saturated 5 or 6 membered heterocyclic compounds having at least one ring nitrogen and optionally having a butadiene moiety bonded to adjacent carbon atoms of said ring to form a bicyclic system; P is H or a peptide moiety, suitably an LHRH, somatostatin or bombesin analogs.

Abstract: Substantially non-antigenic polymers containing pI and/or pH optimum modulating moieties are disclosed. The polymers are useful as intermediates for synthesis of amine-based polymers and in the formation of activated polymers for conjugation with nucleophiles. Conjugates and methods of preparation and treatment with the conjugates are also disclosed.

Abstract: This invention is directed to a zwitterionic water-soluble imine of formula: wherein R1 is heterocyclyl, heteroaryl, aryl, arylalkyl, cycloalkyl or lower alkyl; R2 is alkyl, alkenyl, aminoalkyl, diaminoalkyl, hydroxyalkyl, alkoxyalkyl, thioalkyl, alkylthioalkyl or arylalkyl; R3 is hydrogen and lower alkyl, or R1 and R3 taken together form a cycloalkyl, p is 2, 3, 4 or 5; and Z is CO2−, OCO2−, SO3−, OSO3−, PO3− or OPO3− which are useful as ferrous metal corrosion inhibitors.

Abstract: Chlorosulfonyl substituted aromatic heterocyclic compounds, such as 2-chlorosulfonyl[1,2,4]triazolo[1,5-c]pyrimidine compounds, were prepared in good yield by chloroxidation of di(aromatic heterocyclyl) disulfide compounds in a medium containing water, a water-immiscible organic solvent, and a phase transfer catalyst, such at tetrabutylammonium chloride.

Abstract: The subject matter of the present invention relates to a reagent and a process useful for cleaving a functional group protected by an alkoxycarbonyl group during an organic synthesis. This reagent comprises: a) an aqueous phase; b) a catalyst comprising at least one group VIII element in the periodic table of elements and at least one water-soluble ligand, wherein the group VIII element in the periodic table is maintained in the aqueous phase by the formation of a complex with at least one water-soluble ligand; and c) a nucleophilic compound soluble in the aqueous phase; and optionally d) an organic phase.

Abstract: The present invention relates to a malondialdehyde-acetaldehyde adduct which acts as a specific immune-enhancing factor. In addition to its highly specific and immunogenic properties, the factor is highly fluorescent. It has an excitation frequency of about 398 nanometers and an absorbance of about 460 nanometers. The factor is also highly reactive and is also adducted to antigens including complex proteins, lipids, carbohydrates or DNA.

Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I) ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable alkoxyamide, ester, acyloxyamide, or imide thereof. Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

Abstract: Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R.sup.1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Abstract: A chromogenic receptor comprises a self-assembled chromogenic compound having at least one intrinsic binding site. The chromogenic compound is characterized by the property of producing a reversible color change responsive to binding a target substrate to the receptor. The chromogenic compound has a transition metal ion and at least one ligand bound to the transition metal ion. The ligand is selected from the group consisting of substituted phenanthroline, substituted 2,2'-bipyridine and substituted 2,2':6',2"-terpyridine. The transition metal is selected from the group consisting of Cu(I), Cu(II), Ag(I), Ni(II), Fe(II), Fe(III), Ru(II), Co(III), and Os(II). Self-assembly can be effected in the presence of Cu(I) to form receptors for dicarboxylic acids, carbohydrate, amino acids, steroids and pyrophosphates. The receptors are characterized by the formation of a 2:1 complex of the target substrate with the receptor producing a visible color change from orange to red and a measurable change in its luminescence.

Abstract: This invention relates to a compound of formula I ##STR1## These compounds are leukotriene antagonists and as such can be used in treating various diseases associated with leukotrienes.

Abstract: The present invention discloses compositions containing a transfer agent and/or bactericidal compounds, and hydrophobic materials which form, upon application to dental surfaces, adhesive, protective and bacteria-inhibiting barriers.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: Substantially non-antigenic polymers containing pI and/or pH optimum modulating moieties are disclosed. The polymers are useful as intermediates for synthesis of amine-based polymers and in the formation of activated polymers for conjugation with nucleophiles. Conjugates and methods of preparation and treatment with the conjugates are also disclosed.

Abstract: Novel ligands for use in MRI contrast agents and which have the formula ##STR1## wherein R.sub.1 -R.sub.14, M", l, m, and n are defined herein.

Abstract: This invention relates to methods, reagents, and kits utilizing metal chelates to inactivate nucleotide sequences, especially to inactivate polymerase chain reaction (PCR) and ligase chain reaction (LCR) products and to inactivate nucleotide sequences in a bioprocess and bioproduct. A novel metal chelate class is also disclosed.