Abstract: Adhesive sticks are obtained using water-based preparations of synthetic polymers of adhesive character and soaps which act as shaping gel-forming components. Mixtures of polyurethanes and polyvinyl pyrrolidone are used as the synthetic polymers. The polyurethane may be in the form of a dispersion and produced by reacting at least one polyol, at least one polyfunctional isocyanate and a component capable of salt formation in alkaline aqueous solution and/or a nonionic hydrophilic modifying agent.

Abstract: This invention relates to a process for the preparation of the formula I compound [2-((8,9)-dioxo-2,6-diazabicyclo[5.2.0]-non-1(7)-en-2-yl)ethyl]phosphonic acid, a NMDA antagonist useful as an anticonvulsant and neuroprotectant in situations involving excess release of excitatory amino acids. ##STR1## In the process of the present invention, 3-aminopropyl carbamic acid 1,1-dimethylethyl ester is reacted with a dialkyl vinylphosphonate to obtain N-[3-(t-butyloxycarbonyl-amino)propyl]-2-aminoethylphosphonic acid dialkyl ester (d) in 80% yield. Reaction of (d) with a 3,4-dialkoxycyclobut-3-en-1,2-dione gives [3-[[2-(dialkoxyphosphoryl)ethyl]-(2-alkoxy-3,4-dioxo-1,2-cyclobuten-1-yl) amino]propyl] carbamic acid 1,1-dimethylethyl ester (e) in 96% yield. Deprotection and cyclization of (e) in trifluoroacetic acid gives [2-((8,9)-dioxo-2,6-diazabicyclo[5.2.0]-non-1(7)-en-2-yl)ethyl]phosphonic acid dialkyl ester (c) in 58% yield.

Abstract: This invention concerns peptides (I) having intracellular potassium channel modulating activity comprising the amino acid sequence shown in SEQ ID No: 2:(N terminal function) (I) Met Ile Ser Ser Val Cys Val Ser Ser 1 5} Tyr Arg Gly Arg Lys Ser Gly Asn Lys 10 15 Pro Pro Ser Lys Thr Cys Leu Lys Glu Glu 20 25 (C terminal function)in which the cysteines are optionally linked via a disulphide bridge and wherein ______________________________________ Met represents L-methionine Ile represents L-isoleucine Ser represents L-serine Val represents L-valine Cys represents L-cysteine Tyr represents L-tyrosine Arg represents L-arginine Gly represents glycine Lys represents L-lysine Asn represents L-asparagine Pro represents L-proline Thr represents L-threonine Leu represents L-leucine Glu represents L-glutamic acid ______________________________________or a variant thereof,with the proviso that excluded is the 13-Lys variant (where 13-Arg is replaced by 13-Lys) in which the cysteines are not linked via a disulphide bridge

Abstract: This invention relates to compounds of Formula I ##STR1## wherein: R.sup.1 and R.sup.2 are independently selected from hydrogen, straight-chain and branched alkyl group having up to 10 carbon atoms or --(CH.sub.2).sub.m Ar where Ar is phenyl, naphthyl or thienyl, each optionally substituted by one or two substituents selected independently from C.sub.1 -C.sub.6 alkyl, halogen, C.sub.1 -C.sub.6 alkoxide and trifluoromethyl;or NR.sup.1 R.sup.2 is 1, 2, 3, 4-tetrahydroquinolin-1-yl or 1, 2, 3, 4-tetrahydroisoquinoline-2-yl;m is 1-5;n is 1 or 2;Y is hydrogen, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkoxy;or the pharmaceutically acceptable salts thereof, which are dopamine D.sub.2 agonists and therefore useful in the treatment of psychoses and Parkinson's disease.

Abstract: The invention is a method of using Angiotensin (AII) Antagonists as inhibitors of the growth of adipose tissue, reducing adipocyte growth and body weight gain.

Abstract: Piperazine derivatives of formula (I) are useful in the treatment of cognitive disorders. In formula (I), X is a group of (IIa): --(CH.sub.2).sub.n CR.sup.2 R.sup.3 CONR.sup.4 R.sup.5 or (IIIb): --A--NR.sup.6 COR.sup.7 where n, A, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have specified meanings.

Abstract: Compounds of formula (I) and the pharmaceutically acceptable acid addition salts thereof are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics. In the formula a and b each represents 0, 1, 2 or 3 such that the sum of a+b is 0, 1, 2 or 3, the dotted line represents an optional double bond which may be present in the ring, provided that a is at least 1, A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups, R is a mono or bicyclic aryl or heteroaryl radical with the proviso that R is not an unsubstituted phenyl group, R.sup.1 is a mono or bicyclic heteroaryl radical, and R.sup.2 is cycloalkyl or cycloalkenyl.

Abstract: A process is described for preparing a compound of the formula I: ##STR1## or a salt thereof; wherein X is a protecting group and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1-6 alkyl or C.sub.1-6 perfluoroalkyl, R.sub.5 is hydrogen or when n is 1 R.sub.5 taken together with R.sub.3 comprises a double bond; m is 1, 2 or 3; n is 0 or 1, and p is 0, 1 or 2.

Abstract: The invention is a process improvement for producing N-?3-(3-cyano-pyrazolo?1,5-a!pyrimidin-7-yl)phenyl!-N-ethyl-acetamide which is useful as an anxiolytic, antiepileptic, sedative-hypnotic agent and skeletal muscle relaxant. The disclosed invention comprises reacting 3-dimethylamino-1-(3-N-ethyl-N-acetyl-aminophenyl)-2-propen-1-one or a suitable salt thereof with 3-aminopyrazole-4-carbonitrile or a suitable salt thereof in a mixture comprising water and acetic acid or a suitable salt thereof, rather than in acetic acid alone.

Abstract: This invention concerns compounds of formula (I) ##STR1## where A is a C.sub.1 or C.sub.2 alkylene chain optionally substituted by lower alkyl; Z is a bicyclic oxygen-containing aryl radical (e.g. 2,3-dihydro-1,4-benzodioxin-5-yl); R is hydrogen or lower alkyl; R.sup.1 is aryl or aryl(lower)alkyl; R.sup.2 is hydrogen or lower alkyl; and R.sup.3 is hydrogen, an alkyl group of 1 to 10 carbon atoms, cycloalkyl of 3 to 12 carbon atoms; cycloalkyl(lower)alkyl, aryl or aryl(lower)alkyl or R.sup.2 and R.sup.3 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring which may contain a further hetero atom, and the pharmaceutically acceptable acid addition salts thereof. The compounds are 5-HT.sub.1A -antagonists which may be used, for example, in treating anxiety.

Abstract: A novel asymmetric synthesis is provided for preparing optically active amides of formula (A) and their salts. ##STR1## In the formula, X represent --N-- or --CH--, R represents a mono or bicyclic aryl or heteroaryl group, R.sup.1 is an aryl or heteroaryl radical, and R.sup.2 and R.sup.3 have specified meanings. The products are useful as 5-HT.sub.1A antagonists.Novel diesters of formula D useful as intermediates in the process are also disclosed.

Abstract: This appliciation discloses a process for preparing a lactone of general formula (I), where R is an optionally substituted phenyl group or an optionally substituted mono- or bicyclic heteroaryl radical which process comprises reacting an anion of a malonate of formula (II) with an ethylene compound of formula (III) Y--CH.sub.2 --CH.sub.2 OZ, to give a compound of formula (IV) and hydrolysing the compound of formula (IV) to give a lactone of formula (I). The lactones are of use as intermediates for preparing 5-HT.sub.1A binding agents.

Abstract: Disclosed herein is an aqueous, injectable rapamycin solution comprising 40 to 75 volume percent of a concentrate solution of rapamycin in propylene glycol, at concentrations of rapamycin ranging from 0.25 mg/ml to 8 mg/ml, in combination with a diluent solution comprising water, wherein the diluent comprises 60 to 25 volume percent of the combined solution and the concentration of rapamycin in the combined solution ranges from 0.1 mg/ml to 4 mg/ml.

Abstract: Bicyclic carboxamides of formula I ##STR1## and the pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents, particularly 5-HT.sub.1A antagonists and may be used, for example, as anxiolytics. In the formulaX represents --CR.sup.2 .dbd.CR.sup.2 -- or --(CR.sup.2)q--;m represents 0,1 or 2; n represents 0,1 or 2; p represents 0,1,2 or 3 and q represents 0,1,2 or 3;A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups,R is a mono or bicyclic aryl or heteroaryl radical,R.sup.1 is an aryl or aryl(lower)alkyl radicaland each R.sup.2 is independently hydrogen or lower alkyl.

Abstract: The invention disclosed herein comprises fat compositions primarily for use in nutritionally complete infant formulas in which the constituent palmitic acid oils and lauric acid oils are corandomized. The invention additionally includes such corandomized fat compositions with medium-chain triglycerides added, particularly for use in nutritional products for preterm or low birthweight infants. The invention further includes such fat compositions in which the constituent palmitic acid oils and oleic acid oils are corandomized. Such corandomization of two or more oils yields a mixture of triglycerides having a substantially different chemical makeup than that of the native oils themselves or than the native oils when randomized individually. Corandomization of the palmitic acid oils and the lauric acid oils or of the palmitic acid oils and the oleic acid oils affords an economical means of providing a very highly absorbed fat composition.

Abstract: Amide derivatives of formula (I) and their pharmaceutically acceptable salts (where a and b each represent 0, 1, 2 or 3 such that a+b=0, 1, 2 or 3, the dotted line represents an optional double bond, A is an optionally substituted C.sub.1-2 -alkylene chain, R is mono or bicyclic aryl or heteroaryl radical, R.sup.1 is hydrogen or lower alkyl, R.sup.2 is an aryl, aralkyl, heteroaryl or heteroarylalkyl and --CONR.sup.3 R.sup.4 represents a specified amide group) are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics.

Abstract: Piperazine derivatives of formula: ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula, n is 1 or 2; R and R.sup.5 are hydrogen or lower alkyl, R.sup.1 is substituted or unsubstituted aryl or a heteroaromatic radical; R.sup.3 is substituted or unsubstituted aryl or substituted or unsubstituted arylalkyl; R.sup.9 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl or substituted or unsubstituted arylalkyl with the proviso that when R.sup.9 is hydrogen, alkyl, or arylalkyl, R.sup.5 is other than a tertiary alkyl group. The compounds of this invention are useful 5-HT.sub.1A antagonists for the treatment of CNS disorders such as anxiety.

Abstract: This invention concerns compounds of formula (I) wherein E represents hydrogen, C.sub.1 -C.sub.6 alkyl or a group Ar.sup.1 -A.sup.1 ; Ar and Ar.sup.1 when present each represent an aryl group of 6 to 10 carbon atoms or a heteroaryl group of 5 to 10 ring atoms wherein the heteroatoms are selected from oxygen, nitrogen and sulphur, which may be optionally substituted by one or more substituents selected from alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halogen, haloalkyl of 1 to 6 carbon atoms, haloalkoxy of 1 to 6 carbon atoms, cyano, amino, mono- or di-(C.sub.1 -C.sub.6) alkylamino, hydroxy and nitro; A and A.sup.1 when present are the same or different alkylene groups having one or two carbons linking Ar or Ar.sup.