Abstract: The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is a hydrogen atom or a group containing 1 to 4 non-hydrogen atoms; RA is —COCONH2 or the like; R3 is -(L2)-(acidic group) wherein L2 is a group connecting with an acid group; R4 is a hydrogen atom or the like, its prodrug, their pharmaceutically acceptable salt, or solvate thereof.

Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: wherein one of R5, R6 or R7 is a group of general Formula B, wherein W is a —CH— group or a nitrogen atom, and the other substituents are as defined herein; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: The present invention relates to compositions and methods of achieving a therapeutic effect including, the treatment or prevention of Syndrome X in an animal, preferably a mammal including a human subject or a companion animal, using a corticotropin releasing factor (CRF) antagonist alone or together with a glucocorticoid receptor antagonist.

Abstract: The invention relates to a process for the preparation of heterocycles, characterised in that the following components: i) a propargyl derivative of the general structural formula I  a wherein Het is an optionally substituted hetero atom and A is a substituted or unsubstituted aromatic entity, a substituted or unsubstituted aromatic heterocycle, a substituted or unsubstituted vinyl arene and/or a derivative thereof, an olefin, an alkyne, an acceptor group or a nitrile; (ii) a compound of the general structural formula II, B—X  II,  wherein B is an electron-deficient substituted or unsubstituted aromatic entity with or without an acceptor group, an electron-deficient substituted or unsubstituted heteroaromatic entity with or without an acceptor group, an electron-deficient olefin and/or alkyne, a metal complex, and X is a leaving group; (iii) a nucleophile of the general structural formula III, Y—Cn—Z  III,  wherein Y and/or Z, each

Abstract: The present invention relates to novel bis-sulfonamides represented, for example, by formula I below and a pure diastereomer, a mixture of diastereomers, a diastereomeric racemate, a mixture of diastereomeric racemates and meso-forms and a pharmaceutically acceptable salt thereof, wherein R1 represents aryl; aryl-lower alkyl; aryl-lower alkenyl; heteroaryl; or heteroaryl-lower alkyl; and R2 represents lower alkyl; trifluoromethyl; lower alkoxy-lower alkyl; lower alkenyl; lower alkynyl; aryl; aryl-lower alkyl; aryl-lower alkenyl; heterocyclyl; heterocyclyl-lower alkyl; heteroaryl; heteroaryl-lower alkyl; cycloalkyl; or cycloalkyl-lower alkyl. The present invention also relates to a process for manufacturing those compounds, pharmaceutical compositions containing one or more of those compounds as endothelin antagonists, and a method of treating a subject having a disorder involving endothelin with the compounds of the invention.

Abstract: The present invention relates to a process for preparing sodium salt of cephalosporins from their corresponding hydrohalide salt, which is neutralized with trimethylsilylating agent for the first time.

Abstract: The present invention relates to a new process of extracting tetrodotoxin from the tissues of an organism. The invention provides increased yield of tetrodotoxin from animal tissues. In the invention, a lixiviated solution is obtained by soaking the tissues with water and a weak organic acid. Soluble proteins are removed by heating the lixiviated solution at a temperature below the boiling point. After pH adjustment, the solution is passed through a cation exchange column. Inorganic salts and alkaline amino acids are removed, and then the tetrodotoxin is adsorbed and eluted from activated carbon. The tetrodotoxin is crystallized by adjusting the pH to 8-10.

Abstract: The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)-1piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.

Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.

Abstract: Disclosed are novel compounds of formula (I): wherein Ar1, Ra, R4, R5, X and Y are defined below, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases associated with such kinases, for example, diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are processes for preparing these compounds, novel intermediates useful in these processes and compositions comprising compounds of the formula (I).

Abstract: Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula I, A—B—D—E—F—G   (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.

Abstract: Compounds of formula: in which R represents a CR1R2, C═C(R5)SO2R6 or C═C(R7)SO2alk radical, their preparation and the pharmaceutical compositions containing them.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketonols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, W and Y independently of one another each represent hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: This invention relates to novel isoxazolines of formula (I): or a pharmaceutically acceptable salt form thereof. This invention also relates to novel isoxazolines of formula (I) which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of 4-alkyl and cycloalkyl derivatives of dihydropyridines of Formula I. As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: The blue marine sponge Cribrochalina sp., collected in the Republic of Maldives was found to contain new cell growth inhibitors denominated cribrostatin 3, cribrostatin 4 and cribrostatin 5 which were found to be active against the NCI human melanoma panel and the P388 marine lymphocytic cell lines employed by the U.S. National Cancer Institute. Structural determination of all three substances were accomplished utilizing high yield NMR (400 MHz) and mass spectral studies. Cribrostatins 3-5 were also found to possess significant antibacterial and antifungal activity.

Abstract: The present invention provides a herbicidal compound of formula I, methods for the preparation thereof and intermediates useful therefor. ##STR1## wherein X and Y are each independently O or S; Z is N or CR.sub.4.

Abstract: The present invention refers to zinc-phthalocyanines of general formula (I) ##STR1## to processes for their preparation and to their use as phototherapeutic and photodiagnostic agents as free molecules and as conjugates with macromolecular carrier molecules.

Abstract: The invention concerns pharmaceutically useful N-heterocyclyl sulphonamide derivatives, their pharmaceutically acceptable salts, processes for their manufacture, their use for antagonising one or more actions of endothelin in a human or other warm-blooded animal, their use in methods of treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role.

Abstract: This invention relates to phosphorescent probes effective for oxygen measurement in human or animal tissue comprising a porphyrin chromophore capable of releasing absorbed energy as phosphorescent light and a dendrimer, wherein said porphyrin chromophore comprises the core of the dendrimer.