Abstract: A process for preparing a morphinan derivative, by providing a dihydrofuranyl bridged tetracycle halide of the formula (19) wherein X is halogen, R is an alkyl group of from 1 to about 10 carbon atoms, and R1 is a protecting group; and converting the pentacycle halide into a morphinan derivative of formula (20) wherein R is as defined above.

Abstract: The present invention is directed to the use of 2,4,5-trisubstituted imidazole compounds and compositions in the treatment of CNS injuries to the brain.

Abstract: Compounds having Formula I are useful for treating inflammation. Also disclosed are pharmaceutical compositions comprising compounds of Formula I, and methods of inhibiting/treating inflammatory diseases in a mammal.

Abstract: A novel 4-acylamino-2,2,6,6-tetramethylpiperidine derivatives and antioxidants comprising the same. The 4-acylamino-2,2,6,6-tetramethylpiperidine derivatives are represented by formula (A): wherein R1 represents a hydrogen atom, a hydroxyl group, an oxyradical group, an aliphatic group, an acyl group, an aliphatic oxy group or an acyloxy group; and R2 represents an aliphatic group having at least 3 carbon atoms and at least two hydroxyl groups.

Abstract: The present invention provides compounds of Formula I: wherein A and R1-R8 are defined herein. The compounds of Formula I inhibit the polymerization of tubulin and possess antimitotic activity. The compounds of Formula I may be useful for the treatment of psoriasis, gout, papiloma, warts, and a variety of tumors.

Abstract: Pharmaceutically/cosmetically-active adamantyl-substituted retinoid compounds have the structural formula (I): wherein Ar is a radical having one of the formulae (a)-(d): and are useful for the treatment of disorders and/or ailments manifesting an overregulation of PAR receptors and/or a hypervitaminosis A.

Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

Abstract: Compounds of general formula (I) in which U represents a group of general formula (A) or (B) in which formulae V represents a hydrogen or halogen atom, a (C1-C3)alkyl group or one or two (C1-C3)alkoxy groups, W and X each represent, respectively, either two oxygen atoms, or an oxygen atom and a CH2 group, or a CH2 group and an oxygen atom, or an oxygen atom and a CO group, n represents the number 0 or 1, R represents either a propyl group when U represents a group of general formula (A), or a hydrogen atom or a (C1-C3)alkyl group when U represents a group of general formula (B), Y represents one or more atoms or groups chosen from the following: hydrogen, halogen, (C1-C3)alkyl and (C1-C3)alkoxy, Z represents two hydrogen atoms or an oxygen atom.

Abstract: Novel heterocyclic compounds which generate chemiluminescence on reaction with a phosphatase enzyme are provided as well as a process for their preparation and intermediates useful therein. The compounds comprise a nitrogen, oxygen or sulfur-containing heterocyclic ring system bearing an exocyclic carbon-carbon double bond. The double bond is further substituted at the distal carbon with a phosphate group and an oxygen or sulfur atom-containing group. Novel compositions further comprising a cationic aromatic compound (CAC) in addition to the heterocyclic phosphate compound are provided. The addition of the CAC in the composition greatly increases the production of chemiluminescence and provides improved detection sensitivity. Compositions further comprising an anionic surfactant and a non-ionic surfactant provide additional improvements in detection sensitivity.

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

Abstract: This invention provides compounds of Formula I having the structure wherein: B, C, D, and R1 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Abstract: Substituted 4-benzoylpyrazole of the formula I where: Q is a pyrazole of the formula II X1 is a straight-chain or branched C1-C6-alkylene, a C2-C6-alkenylene or a C2-C6-alkynylene chain which is interrupted by a hetero atom selected from the group consisting of: oxygen and sulfur, Het is a three- to six-membered partially or fully saturated heterocyclic group or a three- to six-membered heteroaromatic group having up to three hetero atoms selected from the following three groups: nitrogen, oxygen in combination with at least one nitrogen or sulfur in combination with at least one nitrogen; and agriculturally useful salts thereof, processes and intermediates for preparing compounds of the formula I, compositions comprising them and the use of the compounds of the formula I and of compositions comprising them for controlling harmful plants are described.

Abstract: The invention relates to polycyclic thiazolidin-2-ylidene amines and their physiologically tolerated salts and physiologically functional derivatives. Polycyclic thiazolidin-2-ylidene amines of the formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example as anorectics and in the treatment or prophylaxis of type II diabetes.

Abstract: The present invention provides a compound of formula (I) wherein R is phenyl, C3-C7 cycloalkyl or heteroaryl, each of which being optionally benzo- or C3-C7 cycloalkyl-fused and optionally substituted, including in the benzo- or C3-C7 cycloalkyl-fused portion, by from 1 to 3 substituents each independently selected from C1-C4 alkyl, fluoro(C1-C4)alkyl, C1-C4 alkoxy, fluoro(C1-C4)alkoxy, phenoxy, C2-C4 alkanoyl, halo, C1-C4 alkoxycarbonyl, C3-C7 cycloalkyl, —S(O)m(C1-C4 alkyl), cyano, —NR2R3, —S(O)mNR2R3, —NR4(C1-C4 alkanoyl) and —CONR2R3, or R is 2,3-dihydrobenzo[b]furanyl or chromanyl; R1 is H or C1-C6 alkyl; W is a direct link, methylene or ethylene; X is unbranched C2-C4 alkylene; Y is phenyl, naphthyl, benzyl, pyridyl, thienyl or C3-C7 cycloalkyl, each of which being optionally substituted by from 1 to 3 substituents each independently selected from C1-C4 alkyl, fluoro(C1-C4)alkyl, C1-C4 alkoxy, fluoro(C1-C4)alkoxy, halo and cyano; Ar is phenyl, naphthyl, benzyl, th

Abstract: Novel compounds that are anti-angiogenic or immunosuppressive are described. Also described are methods for determining if an animal is at risk for a disease involving abnormal angiogenesis or an immune reaction resulting in pathology comprising evaluating an aspect of MetAP2 metabolism or structure; methods for identifying agents that are anti-angiogenic or immunosuppressive comprising evaluating the effect of the agent on an aspect of MetAP2 metabolism; methods for treating a cell having an abnormality in metabolism or structure of MetAP2; and methods for treating abnormal angiogenesis or an immune reaction which results in pathology in an animal. Pharmaceutical compositions are also provided.

Abstract: Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.

Abstract: The invention provides adamantane derivatives, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.

Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula I and to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering the compounds of Formula I to said mammal.

Abstract: Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, suchas pain and diabetes. The inventin encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermedates useful in such processes.

Abstract: Compound corresponding to the general formula (I) in which R1 represents a hydrogen atom, a (C1-C4)alkyl group or a phenyl(C1-C4)alkyl group, R2 represents a hydrogen atom or a (C1-C4) alkyl group, and R3, R4 and R5 each represent a hydrogen or halogen atom or a trifluoromethyl, cyano, hydroxyl, (C1-C6)alkyl or (C1-C6) alkoxy group.