Abstract: Disclosed is a process for preparing a compound having the formula: wherein R, R1, R2, R3, and R4 are independently selected from the group consisting of H, Br, Cl, F, alkyl, or alkoxy.

Abstract: A method of eliminating, reducing or preventing parasites in a fish population is provided by feeding emamectin or a salt thereof to the fish population at a daily dose of 25 &mgr;g to 400 &mgr;g per kg of fish biomass per day for a period of 3-14 days. Also provided is a kit for preparing a medicated fish feed for eliminating, reducing or preventing parasites in a fish population, the kit having a supply of emamectin or a salt thereof and printed instructions for feeding the emamectin or emamectin salt at a daily dose of 25 &mgr;g to 400 &mgr;g per kg of fish biomass per day for a period of 3-14 days.

Abstract: A method for treating obsessive-compulsive disorders, somatoform disorders, dissociative disorders, eating disorders, impulse control disorders, and autism is disclosed. These disorders are treated by administering an effective amount of a D1/D5 antagonist.

Abstract: A process is provided for preparing an S-enantiomer compound having the formula in enantiomeric excess, or an R-enantiomer compound having the formula in enantiomeric excess, said process comprising hydrolyzing a compound having the formula with: (a) an enzyme capable of producing an enantiomeric excess of the S-enantiomer compound of formula (IA) of at least 70%, or (b) an enzyme capable of producing an enantiomeric excess of the R-enantiomer compound of formula (IB) of at least 70%, wherein R1 is selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl, or cycloalkylalkyl.

Abstract: Disclosed is a process for preparing a compound having the formula: wherein R, R1, R2, R3, and R4 are independently selected from the group consisting of H, Br, Cl, F, alkyl, or alkoxy, by (A) reacting a compound having the formula  wherein RA, RC, RD, and RE are independently selected from the group consisting of H, halo, alkyl, or alkoxy, and R5 is aryl or heteroaryl, with a dehydrating agent to produce an imine having the formula: (B) hydrolyzing the imine produced in step (A) to produce the compound having formula (I). Also disclosed are novel intermediates having the formula:  wherein RA, RB, RC, RD, and RE are independently selected from the group consisting of H, halo, alkyl, or alkoxy, and R5 is aryl or heteroaryl.

Abstract: A process is provided for producing a compound having the formula: by: (a) reacting a compound having the formula  with a compound having the formula  in the presence of an organic base selected from the group consisting of: triethylamine; N,N-diisopropylethylamine; 1,8-diazabicyclo[5.4.0]undec-7-ene(1,5-5); 1,5-diazabicyclo[4.3.0]non-5-ene; or 1,4-diazabicyclo[2.2.2]octane to form a compound having the formula (b) reducing the compound of formula (4.0) to form the compound of formula (1.0), wherein X is Cl, Br, I or F.

Abstract: A method for treating a patient afflicted with cancer is provided, in which temozolomide is administered to the patient for at least two cycles of a cyclical dosing schedule, wherein each cycle has a dosing period of 5 to 25 days, in which temozolomide is administered daily, at a dose of 40 to 150 mg/m2/day, followed by a rest period of 5 to 14 days in which temozolomide is not administered. Also provided is a medical kit for administering temozolomide, having printed instructions for administering temozolomide according to the cyclical dosing schedule set forth above, and a supply of temozolomide in dosage units for at least one cycle, wherein each dosage unit contains 5 to 250 mg of temozolomide and a pharmaceutically acceptable carrier.

Abstract: Aqueous nasal spray compositions comprising a medicament and an aqueous carrier comprising water soluble polymers selected from the group consisting of polyvinylpyrrolidone and mixtures thereof.

Abstract: Disclosed is a process for preparing a compound of the formula: wherein X1, X2, X3, X4, and X5 are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having the formula wherein X1, X2, X3, X4, and X5 are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having the formula wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase.

Abstract: Disclosed is a process for preparing a compound having the formula: wherein R1 is selected from the group consisting of: alkyl, alkenyl, alkynyl, aryl, aralkyl, cycloalkyl, and cycloalkylalkyl, R1 being optionally substituted by substituents selected from halo, —OH, alkyl, alkoxy, or —CF3, said process comprising the following steps: (a) reacting a ketone having the formula with a carbanion having the formula wherein R1 is as defined above, and R2 and R3 are independently selected from the group consisting of —ORA and —RA, wherein RA is alkyl, phenyl, substituted phenyl, cycloalkyl, substituted cycloalkyl, cycloalkylalkyl, or substituted cycloalkylalkyl; (b) treating the reaction mixture from step (a) with a protonating agent; and (c) thermally decomposing the product of 16, to form the compound of formula (I). The compounds made by this process have antihistaminic activity, e.g., loratadine.

Abstract: Intermediates having the formula wherein BI is —CH2OH or —CH2ORP, and RP is an alcohol protecting group; a is 1, 2, or 3; TI is —OH or QI is phenyl, naphthyl ohr heteroaryl having 1-3 substituents; Ra and Rc are the same, and are H, or are selected from alkyl, cycloalkyl and aryl groups, the groups being optionally substituted with one or more substituents selected from alkyl cycloalkyl, aryl, or —OH; or Ra and Rc together with the C—N—C chain to which they are bound, form a 5-7 membered ring; Rb and Rd are the same, and are H, or are selected from alkyl, cycloalkyl and aryl groups, the groups being optionally substituted with one or more substituents selected from alkyl, cycloalkyl, aryl, or —OH; and D is a directing group capable of directing lithiation alpha to a nitrogen atom of a nitrogen compound having D as a substituent bound to the nitrogen atom when the nitrogen compound is reacted with s-butyl lithium, are disclosed

Abstract: The present invention provides compounds having the formula: wherein n is 0 or 1; R is —NH2 or wherein R1 and R2 are independently selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, carboxy, carboxyalkyl, and carbamoyl; Q is R3C(O)— or wherein R5 is selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, and carbamoylalkyl, and R3 and R4 are selected from the group consisting of H, alkyl, alkoxy, arylalkoxy, aralkyl, heteroaralkyl, and carbamoylalkyl; the Q—NH—(CH2)n— and the —C(O)R substituents of the compound of formula I are independently positioned ortho, meta, orpara relative to the carbon atoms that form the bond between the two phenyl groups to which said substituents are bound, with the proviso that said substituents are not both positioned ortho; and the Q—NH—(CH2)n and the —C(O)R substituents of the compound of formula II are positioned meta orpara t

Abstract: Novel compounds of formula are disclosed. Also disclosed is a method of inhibiting farnesyl protein transferase function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the above formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Also disclosed is a method of effecting an anti-allergic response by administering the compounds.

Abstract: The present invention provides compounds having the formula wherein n, p, q and r are each independently selected from 0 or 1; a, b, c, and d each independently represents a carbon or nitrogen atom, with the proviso that no more than two of a, b, c, and d are nitrogen atoms; Y and Y1 each independently represents 1-4 optional substituents selected from alkyl, alkoxy, halo, —CF3, and —C(O)OH; R1, R2, R3 and R4 are as defined herein; R5, R6, R7, R8, R9, R10, R11 and R12 are independently selected from H or C1-C3 alkyl; and wherein are positioned meta or para relative to each other; or a biolabile ester thereof, or a pharmaceutically acceptable salt thereof. Also provided are methods of using these compounds for treating vitronectin-mediated disorders, e.g., cancer, retinopathy, artherosclerosis, vascular restenosis, and osteoporosis.

Abstract: Aminomethyl-phenylimidazoles are produced by reaction of an ester of a hydroxymethyl-phenylimidazole with an amine. A particularly preferred ester is the acetate ester. The aminomethyl-phenylimidazoles have useful properties as highly selective partial agonists or antagonists at brain dopamine receptor subtypes. A preferred compound prepared is 5-fluoro-2-?4-?(2-phenyl-1H-imidazol-5-yl)methyl!-1-piperazinyl!pyrimidine . Esters of the hydroxymethyl-phenylimidazoles are useful intermediates.

Abstract: Aqueous nasal spray compositions containing:0.001-2% by weight/volume of a medicament selected from the group consisting of chlorpheniramine maleate, oxymetazoline hydrochloride and mixtures thereof;0.50 to 15.00% by weight/volume of a water soluble polymer selected from the group consisting of polyvinylpyrrolidone having an average molecular weight of about 10,000 to 360,000 and mixtures thereof;2.5 to 10.00% by weight/volume of polyethylene glycol;1.00 to 10.00% by weight/volume of a moisturizing agent other than polyethylene glycol;0.01 to 0.05% by weight/volume of disodium edetate;0.001 to 0.3% by weight/volume of an antimicrobial preservative;0.20 to 5.00% by weight/volume of an aromatic alcohol;a sufficient amount of a pharmaceutically acceptable buffer to maintain the pH of the composition within the range of about 4.0 to 8.0; andQS water.

Abstract: The invention provides an improved process for the preparation of 17-esters of 9.alpha.,21 -dihalo-pregnane-11.beta.,17.alpha.-diol-20-ones, and in particular for the preparation of 17-esters of anti-inflammatory steroids according to the following scheme: ##STR1## wherein RCO, R.sup.1, X, Y and the dotted line are as defined in the specification. The novel process is especially suitable for the preparation of Mometasone Furoate.

Abstract: The invention discloses a vaccine and methods for the treatment of porcine reproductive and respiratory syndrome. The vaccine is derived from the viral agent NEB-l-P94, deposited at the American Type Culture Collection under accession number VR-2525.Further, the invention discloses a vaccine virus with phenotypic characteristics which can be distinguished from wild type PRRS virus.

Abstract: An aqueous nasal decongestant composition containing oxymatazoline is disclosed which does not contain mercurial preservatives.

Abstract: A process is described for preparing 3-exomethylene cephalosporanic acid derivatives for use in the synthesis of cephalosporin antibiotics such as ceftibuten. The process comprises electrochemical reduction of a compound of the formula (IV) ##STR1## wherein: R.sup.3 is ##STR2## is an optional sulfoxide group; n is 2 or 3; R.sup.1 is H and R is H or NHR.sup.2, where R.sup.2 is H or a protecting group selected from C.sub.6 H.sub.5 CH.sub.2 OC(O)--, C.sub.6 H.sub.5 C(O)-- or C.sub.1 -C.sub.6 alkoxy-C(O)--; or wherein R and R.sup.1 together with the carbon atom to which they are attached comprise --C(O)--, and produces the desired 3-exomethylene compounds with low levels of the corresponding 3-methyl tautomers.