Abstract: This invention encompasses a novel process for synthesizing the compound represented by formula I: ##STR1## These compounds are useful as non-steroidal anti-inflammatory agents.

Abstract: Described is a process of preparing 3-aryl, 4-aryloxy furan-5-ones which are useful as inhibitors of cyclooxygenase-2 (COX-2). Such compounds are useful as anti-inflammatory agents. The process is directed to an asymmetric synthesis which involves: a trisubstituted styrene derivative preparation via Horner-Wadsworth-Emmons reaction and subsequent one pot trifluoromethylation of the allylic alcohol; preparation of the .alpha.-hydroxyl ketone using Sharpless asymmetric dihydroxylation and Swern oxidation; the esterification of the .alpha.-hydroxyl ketone with the phenoxy acetic acid; and the Dieckman condensation of the resulting ester.

Abstract: The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.

Abstract: The present invention relates to the use of a tachykinin antagonist and a muscarinic antagonist and/or an antihistamine for the treatment or prevention of motion sickness. There is also provided pharmaceutical compositions and products comprising a tachykinin antagonist and a muscarinic antagonist and/or an antihistamine.

Abstract: A class of compounds of formula (I) wherein Z, E, Q, T, U, V, W, M, R.sup.1, R.sup.7 and R.sup.8 are as defined herein; are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.

Abstract: Sulfurpentafluorophenylpyrazoles of formula I are highly potent against flea and tick infestations in animals. The compounds may be formulated to provide products with long duration of action and low potential for inducing vomition and other adverse reactions in treated animals.

Abstract: The present invention relates compounds of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 each independently represents a phenyl group optionally substituted by a variety of substituents;R.sup.3 represents a variety of substituents;R.sup.4, R.sup.5, R.sup.6, and R.sup.7 each independently represents hydrogen or C.sub.1-6 alkyl;A represents --O-- or --S--;B represents --O--, --S--, --NR.sup.a -- or --CHR.sup.a --; andn is zero, 1, 2, 3, 4 or 5;or a pharmaceutically acceptable salt or a prodrug thereof.The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.

Abstract: PURPOSE: To produce a novel antibiotic substance zofimarin having antimicrobial activity against fungi and obtain an antimicrobial agent containing the antibiotic substance zofimarin as an active constituent, by cultivating a microorganism, belonging to the genus Zopfiella and capable of producing the zofimarin.CONSTITUTION: An ascomycete belonging to the genus Zopfiella, e.g. Zopfiella marina; is cultivated. The cultivation is carried out according to general fungi, but artifical seawater is used in place of tap water in a liquid culture medium. A carbon source, nitrogen source, inorganic salt, etc., are added, and a defoaming agent is suitably used to carry out the cultivation at 20-30.degree. C. by the spinner culture method with aeration. After completing the cultivation, microbial cells are removed, and the resultant product in the supernatant liquid or filtrate is extracted and purified to afford the aimed zofimarin.

Abstract: The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.

Abstract: The present invention is directed to the use of a soluble polyvalent support for the preparation of combinatorial libraries of compounds. The resultant combinatorial libraries are useful in screening for biologically active moieties in the drug discovery process or in developing compounds with desired physical and chemical properties.

Abstract: The invention encompasses compounds of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I ##STR1## e.g. (5R)-3-(3,4-difluorophenyl)-5-ethyl-5-methyl-4-[4-(methylsulfonyl)phenyl]- 2,5-dihydro-2-furanone.

Abstract: Tricyclic pyridin-2-one analogues which are ligands for GABA.sub.

Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.

Abstract: The present invention relates to a process for the preparation of substantially pure N-((S)-(-)-.alpha.-methylbenzyl)-3-(S)-(4-fluorophenyl)-1,4-oxazin-2-one hydrochloride, which comprises selectively crystallising the (S,S)-diastereomer as the hydrochloride salt from a mixture of the (S,R)- and (S,S)-diastereomers in an organic solvent, and collecting the resultant crystalline product.

Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.

Abstract: The present invention is directed to compounds of the formula (I): ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9a, R.sup.9b, m and n are as defined herein) which are tachykinin antagonists and which are particularly useful in the treatment of pain, inflammation, migraine, emesis and postherpetic neuralgia.

Abstract: A class of substituted azetidine, pyrrolidine and piperidine derivatives of Formula I are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.

Abstract: The present invention relates to a pharmaceutical composition and a process for the preparation of a tablet containing a growth hormone secretagogue as the active ingredient. The tablet is prepared by forming a powder blend of the active ingredient N-[1(R)-[(1,2-dihydro-1-methanesulfonyl-spiro[3H-indole-3,4'-piperdin]-1'- yl)carbonyl]-2-(phenylmethyl-oxy)ethyl]-2-amino-2-methyl-propanamide, or a pharmaceutically acceptable salt thereof, in particular the methanesulfonate salt, with a binder/diluent, a first diluent, a second diluent, a first portion of a disintegrant, and a lubricant; wet granulating the powder blend with a solution of ethanol/water to form granules; drying the granules to remove the ethanol/water; adding a second portion of a disintegrant; lubricating the granules; and compressing the dried granules into the desired tablet form.

Abstract: The present invention is directed to 3,3-disubstituted piperidines of the formula I: ##STR1## (wherein X, Y, Z, Ar, R, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.

Abstract: A tachykinin receptor antagonist is useful for treating or preventing attention deficit disorder, optionally associated with hyperactivity, in a patient.